Inventors list

Assignees list

Classification tree browser

Top 100 Inventors

Top 100 Assignees


Chalcogen bonded directly to pyrimidine at 2-position

Subclass of:

514 - Drug, bio-affecting and body treating compositions

514001000 - DESIGNATED ORGANIC ACTIVE INGREDIENT CONTAINING (DOAI)

514183000 - Heterocyclic carbon compounds containing a hetero ring having chalcogen (i.e., O,S,Se or Te) or nitrogen as the only ring hetero atoms DOAI

514247000 - Hetero ring is six-membered consisting of two nitrogens and four carbon atoms (e.g., pyridazines, etc.)

514256000 - 1,3-diazines (e.g., pyrimidines, etc.)

514269000 - Pyrimidines with chalcogen bonded directly to a ring carbon of said pyrimidine moiety

Patent class list (only not empty are listed)

Deeper subclasses:

Entries
DocumentTitleDate
20130045985N-(5-FLUORO-2-((4-METHYLBENZYL)OXY)PYRIMIDIN-4-YL)BENZAMIDE DERIVATIVES - This present disclosure is related to the field of N-(5-fluoro-2-((4-methylbenzyl)oxy)pyrimidin-4-yl)benzamides and their derivatives and to the use of these compounds as fungicides.02-21-2013
201300459845-FLUORO-4-IMINO-3,4-DIHYDROPYRIMIDIN-2-(1H)-ONES DERIVATIVES - This present disclosure is related to the field of 5-fluoro-4-imino-3-(substituted)-3,4-dihydropyrimidin-2(1H)ones and their derivatives and to the use of these compounds as fungicides.02-21-2013
20120184573 PROCESS FOR THE PREPARATION OF AMBRISENTAN AND NOVEL INTERMEDIATES THEREOF - The invention relates to improved processes for the preparation of ambrisentan. The invention also relates to a novel intermediate useful in the preparation of ambrisentan and a process for the preparation of the intermediate. The invention also relates to new polymorphic form of ambrisentan. In particular, it relates to a polymorphic form, designated as Form I of ambrisentan and a process for the preparation of the Form I.07-19-2012
20100152217METHOD FOR TREATING A PULMONARY HYPERTENSION CONDITION - A method for treating a pulmonary hypertension condition such as pulmonary arterial hypertension (PAH) in a subject comprises administering to the subject a therapeutically effective amount of ambrisentan, wherein, at baseline, time from first diagnosis of the condition in the subject is not greater than about 2 years.06-17-2010
20110190326IMIDAZO[1,5]NAPHTHYRIDINE COMPOUNDS, THEIR PHARMACEUTICAL USE AND COMPOSITIONS - The present invention is directed to compounds of Formula (I),08-04-2011
20090192179CHROMAN DERIVATIVES - The invention relates to novel chroman derivatives, stereoisomers and pharmaceutically acceptable salts of Formula I07-30-2009
20100113491SYNTHESIS OF NOVEL TUBULIN POLYMERIZATION INHIBITORS: BENZOYLPHENYLUREA (BPU) SULFUR ANALOGS - A novel series of BPU analogues were synthesized and evaluated for antitumor activity. In particular, BPU sulfur analogues 6n and 7d were shown to possess up to 10-fold increased potency, when compared to compound 1, against cancer cell lines. 6n was more effective than compound 1 in causing apoptosis of MCF-7 cells. When compared to other drugs with a similar mechanism of action, 6n retained significant ability to inhibit tubulin assembly, with an IC50 of 2.1 μM.05-06-2010
20120245188METHODS OF TREATING MEMORY LOSS AND ENHANCING MEMORY PERFORMANCE - The present invention provides methods and compositions for enhancing working memory impaired due to aging, Alzheimer's disease, amyotrophic lateral sclerosis (ALS), Parkinson's disease, alcoholism or alcohol withdrawal or Huntington's disease using p38 MAPK inhibitor such as SB239063.09-27-2012
20130035351Oximes For Treatment Of Peripheral And Central Nervous System Exposure To Acetyl Cholinesterase Inhibitors - The present invention relates to non-charged oxime compounds which are acetyl cholinesterase (AChE) reactivators of inhibited AChE and which protect against organophosphate poisoning both peripherally and in the central nervous system. Also disclosed are pharmaceutical compositions and methods for preparing the reactivator compounds and associated intermediates.02-07-2013
20130079361NOVEL IODO PYRIMIDINE DERIVATIVES USEFUL FOR THE TREATMENT OF MACROPHAGE MIGRATION INHIBITORY FACTOR (MIF)-IMPLICATED DISEASES AND CONDITIONS - Compounds useful for the inhibition of macrophage migration inhibitory factor (MIF) are provided herein, having the Formula (I): wherein A is selected from the group consisting of aromatic or non-aromatic rings, bicyclic rings, polycyclic rings, alkenes or alkynes; B is H, OH, OR, SR, NH2, NHR, or alkyl; R is H or alkyl, and X and Y are independently N or CH, but one of X and Y must be N. Also provided are pharmaceutical compositions comprising a Formula I compound and methods for the treatment of MIF-implicated diseases or conditions, comprising administering a safe and effective amount of a Formula I compound.03-28-2013
20100022567Compositions containing pufa and/or uridine and methods of use thereof - This invention provides methods of enhancing brain development; increasing or enhancing intelligence; increasing or enhancing synthesis and levels of phospholipids, synapses, synaptic proteins, and synaptic membranes by a neural cell or brain cell, comprising contacting a subject or a pregnant or nursing mother thereof with a composition comprising an omega-3 fatty acid, an omega-6 fatty acid, and/or uridine, a metabolic precursor thereof, or a combination thereof.01-28-2010
20100063080CXCR2 inhibitors - The present invention relates to compounds of formula (I) and the use of these compounds as pharmaceuticals, e.g. in preventing or treating a CXCR2 receptor mediated condition or disease.03-11-2010
20130079362CYCLOPROPANE AMIDES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES - Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including, but not limited to, malignant melanomas, solid tumors, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, hepatic cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, chronic myelogenous leukemia, leukemias, papillary thyroid carcinoma, non-small cell lung cancer, mesothelioma, hypereosinophilia syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, diabetic retinopathy, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocytosis, mast cell leukemia, and diseases caused by PDGFR-α kinase, PDGFR-β kinase, c-KIT kinase, cFMS kinase, c-MET kinase, and oncogenic forms, aberrant fusion proteins and polymorphs of any of the foregoing kinases.03-28-2013
20100105710SOLID PREPARATION COMPRISING 2-[[6-[(3R)-3-AMINO-1-PIPERIDINYL]-3,4-DIHYDRO-3-METHYL-2,4-DIOXO-1(2H)-P- YRIMIDINYL]METHYL]-4-FLUOROBENZONITRILE - The present invention provides a solid preparation containing 21[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-4-fluorobenzonitrile (compound (A)) or a salt thereof as a pharmaceutically active ingredient. Specifically, the present invention provides a solid preparation containing a granule composed of compound (A) or a salt thereof and an additive (excluding microcrystalline cellulose) and a tablet containing (a) a granule containing compound (A) or a salt thereof and microcrystalline cellulose, and (b) a tableting aid containing magnesium stearate and microcrystalline cellulose.04-29-2010
20090306111Pharmaceutical Comprising PPAR Agonist - An object of the present invention is to provide an agent for promoting proliferation of a meibomian gland epithelial cell and a corneal epithelial cell, as well as provide an agent for treating an ocular disease such as meibomian gland dysfunction or evaporative dry eye.12-10-2009
20090306114Polymorphic and Other Crystalline Forms of Cis-FTC - Solid phases of (−)-cis-FTC, which are designated herein as amorphous (−)-FTC and Forms II and III (−)-cis-FTC) are provided that can be distinguished from Form I (−)-cis-FTC by X-ray powder diffraction patterns, thermal properties, and methods of manufacture. A hydrated crystalline form of (±)-cis-FTC (i.e. racemic cis-FTC), and a dehydrated form of the hydrate, are also provided, and can similarly be distinguished from other forms of FTC by X-ray powder diffraction patterns, thermal properties, and methods of manufacture. These FTC forms can be used in the manufacture of other forms of FTC, or in pharmaceutical compositions. Particularly preferred uses of these forms are in the treatment of HIV or hepatitis B.12-10-2009
20090306113PHARMACEUTICAL FORMULATION - The present invention provides enteric polymer coated tablet formulations for oral administration which comprise a phospholipase A2 enzyme Lipoprotein Associated Phospholipase A2 (Lp-PLA2) inhibitor, processes for preparing such formulations and their use in therapy, in particular the treatment of atherosclerosis.12-10-2009
20090306112ANTIVIRAL PROTEASE INHIBITORS - The invention is related to compounds of Formula I or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.12-10-2009
20130072508SOLID PHARMACEUTICAL DOSAGE FORM - A solid pharmaceutical dosage form providing improved oral bioavailability is disclosed for inhibitors of HIV protease. In particular, the dosage form comprises a solid dispersion of at least one HIV protease inhibitor and at least one pharmaceutically acceptable water-soluble polymer and at least one pharmaceutically acceptable surfactant, said pharmaceutically acceptable water-soluble polymer having a Tg of at least about 50° C. Preferably, the pharmaceutically acceptable surfactant has an HLB value of from about 4 to about 10.03-21-2013
20130059872POLYMORPHS OF ALOGLIPTIN BENZOATE - The present invention provides new amorphous forms of alogliptin benzoate, pharmaceutical compositions comprising same, methods for their preparation and use thereof in treating conditions mediated by DPP-IV, in particular, type 2 diabetes.03-07-2013
20110015216Solid Pharmaceutical Dosage Form - A solid pharmaceutical dosage form providing improved oral bioavailability is disclosed for inhibitors of HIV protease. In particular, the dosage form comprises a solid dispersion of at least one HIV protease inhibitor and at least one pharmaceutically acceptable water-soluble polymer and at least one pharmaceutically acceptable surfactant, said pharmaceutically acceptable water-soluble polymer having a Tg of at least about 50° C. Preferably, the pharmaceutically acceptable surfactant has an HLB value of from about 4 to about 10.01-20-2011
20120190699PYRIDONES USEFUL AS INHIBITORS OF KINASES - The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing the compounds of the invention and intermediate compounds useful in these processes.07-26-2012
20120115894IMIDAZOLE DERIVATIVES USEFUL AS MODULATORS OF FAAH AND AS FAAH IMAGING AGENTS - The present invention is directed to certain Inidazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.05-10-2012
201000416864,5-DIHYDRO-OXAZOL-2YL DERIVATIVES - The invention relates to compounds of formula I02-18-2010
20090012106Methods, compositions, and kits for organ protection during systemic anticancer therapy - Methods, compositions, and kits are presented for local tissue protection during systemic administration of anticancer therapeutic agents.01-08-2009
20130165460SULFUR DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS - The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.06-27-2013
20120270890Methods of Pancreatic Beta Cell Regeneration - Disclosed are new methods for pancreatic β-cell regeneration and the methods for identifying adult pancreatic endocrine stem cells and the methods for identifying the existence of differentiation processes from adult pancreatic endocrine stem cells toward pancreatic β-cell fate and a new animal model for pancreatic β-cell regeneration. The present invention can be utilized in screening and development of new medicines and therapy protocols for diabetes.10-25-2012
20110034494REVERSIBLE INHIBITION OF SPERM RECEPTOR SYNTHESIS FOR CONTRACEPTION - Methods are disclosed for reversibly inhibiting sperm receptor activity in animals. Nicarbazin, its derivatives and modifications which retain pharmacological activity are shown to inhibit activity of zona pellucida proteins and concomitant synthesis and/or assembly of the sperm receptor on the oocyte surface necessary for fertilization. Nicarbazin is easily administered, for example by simple addition to feed of an animal and is and non-toxic to the animals, providing a safe and efficient means for controlling populations of mammals and avian species.02-10-2011
20110294839NOVEL POLYMORPHS OF LOPINAVIR - The present invention provides a novel cyclohexane solvate form of lopinavir, and a process for its preparation thereof. The present invention also provides a novel desolvated crystalline form of lopinavir, process for its preparation and to pharmaceutical composition containing it. Thus, for example, lopinavir cyclohexane solvate was heated at 100° C. for 10 hours to give lopinavir desolvated crystalline form H1.12-01-2011
20110281900Crystalline Pharmaceutical - New crystalline forms of lopinavir are disclosed.11-17-2011
20090186912ANTI-INFECTIVE AGENTS AND USES THEREOF - This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.07-23-2009
20090149485PYRIMIDINEDIONES AS TYROSINE KINASE INHIBITORS - The present invention relates to a compound of formula (I)06-11-2009
20120289526IMIDAZOLIDINEDIONE DERIVATIVES - The invention provides a compound of formula (Ia), and pharmaceutically acceptable salts thereof. The invention also provides use of the compounds or salts as modulators of Kv3.1 and/or Kv3.2, and in the treatment of diseases or disorders where a modulator of Kv3.1 and/or Kv3.2 is required, such as depression and mood disorders, hearing disorders, schizophrenia, substance abuse disorders, sleep disorders or epilepsy.11-15-2012
20110112124FUNGICIDAL COMPOSITIONS - A method of controlling phytopathogenic diseases on useful plants or on propagation material thereof, which comprises applying to the useful plants, the locus thereof or propagation material thereof a combination of components A) and B) in a synergistically effective amount, wherein component A) is a compound of formula (I) wherein R05-12-2011
20110172257(POLY) AMINOALKYLAMINOALKYLAMIDE, ALKYL-UREA, OR ALKYL-SULFONAMIDE DERIVATIVES OF EPIPODOPHYLLOTOXIN, A PROCESS FOR PREPARING THEM, AND APPLICATION THEREOF IN THERAPY AS ANTICANCER AGENTS - The present invention relates to new derivatives of epipodophyllotoxin 4-substituted with an optionally substituted (poly)aminoalkylaminoalkylamide, or alkyl-urea or alkyl-sulfonamide chain, a process for preparing them and their use as a medicine as an anticancer agent. Formula (1) wherein: —R represents hydrogen or C07-14-2011
20120088783CHROMAN DERIVATIVES - The invention relates to novel chroman derivatives, stereoisomers and pharmaceutically acceptable salts of Formula I04-12-2012
20080312262ARYLOXYALKYLCARBAMATE-TYPE DERIVATIVES, PREPARATION METHOD THEREOF AND USE OF SAME IN THERAPEUTICS - The invention relates to a compound of formula (I):12-18-2008
20100035905Hydrates of 2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1-(2H)-pyr- imidinyl]-4-fluoro-N-[[methyl(1-methylethyl)amino]sulfonyl]benzamide - The present invention relates to hydrates of 2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1-(2H)pyrimidinyl]-4-fluoro-N-[[methyl(1-methylethyl)amino]-sulfonyl]benzamide. The invention also relates to a process for the preparation of these hydrates and to plant protection formulations which comprise hydrates of the phenyluracil I.02-11-2010
20110201634DIHYDROPYRIDIMIDINONE COMPOUNDS FOR THE TREATMENT OF CARDIOVASCULAR DISEASES AND PROCESS FOR PREPARING THE SAME - The present invention relates to a dihydropyrimidinone compound of formula (I) wherein X represents O, S, etc. and R′ represents alkyl, alkoxy, thioalkyl, thioalkyloxy, phenyl, substituted phenyl, phenyloxy, substituted phenyloxy, amino, monosubstitutedamino, disubstitutedamino, aryl, heteroaryl, aryloxy, heteroaryloxy, halo; R″ represents alkoxy, phenyloxy, substituted phenyloxy, aryloxy, heteroaryloxy, halo, NR08-18-2011
20120035196CARBOXYLIC ACID COMPOUND02-09-2012
20120108616SUBSTITUTED OXAZOLE DERIVATIVES AND THEIR USE AS TYROSINE KINASE INHIBITORS - The present invention relates to novel compounds selected from substituted oxazole derivatives of formula (I) that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective c-kit, bcr-abl and Flt-3 inhibitors.05-03-2012
20100125084DOSING REGIMENS FOR TREATMENT OF PROLIFERATIVE DISORDERS COMPRISING ADMINISTRATION OF SAPACITABINE - One aspect of the present invention relates to the use of sapacitabine, or a metabolite thereof, in the preparation of a medicament for treating a proliferative disorder, wherein the sapacitabine or metabolite thereof is administered in a dosing regimen comprising at least one treatment cycle, wherein said treatment cycle comprises administering a therapeutically effective amount of sapacitabine or metabolite thereof for about 2 to about 6 days per week, for 2 weeks out of 3 weeks. Another aspect of the invention relates to the use of sapacitabine, or a metabolite thereof, in the preparation of a medicament for treating cutaneous T-cell lymphoma (CTCL).05-20-2010
20090105286Low-molecular inhibitors of cytohesin-family guanine nucleotide exchange factors - The invention relates to drugs and the use thereof, wherein said drugs contain compounds selected from a group comprising general formulas (1), (2), (3) and (4) and/or enantiomers, diastereomers or the pharmaceutically acceptable salts thereof. Said drugs are used for treating autoimmune and tumoral diseases and/or for immunosuppresion.04-23-2009
20080318986Ddc Compositions - A composition comprising from 1% to 3% dDC which is aqueous and ophthalmically acceptable is disclosed herein.12-25-2008
20080207656Methods, compositions, and kits for organ protection during systemic anticancer therapy - Methods, compositions, and kits are presented for local tissue protection during systemic administration of anticancer therapeutic agents.08-28-2008
20090275600MODIFIED PYRIMIDINE GLUCOCORTICOID RECEPTOR MODULATORS - The present invention provides a novel class of modified pyrimidine compounds and compositions and methods of using the compounds as glucocorticoid receptor modulators.11-05-2009
20090281132Pharmaceutical formulation for use in hiv therapy - The invention discloses a formulation prepared by granulating at least one anti-retro viral drug and at least one pharmaceutically acceptable additive, using an organic solvent; milling the product; finally processing the milled product to form tablets or capsules.11-12-2009
20090286818Pyridine Non-Classical Cannabinoid Compounds and Related Methods of Use11-19-2009
20120295930NOVEL PROCESS FOR THE PREPARATION OF CIS-NUCLEOSIDE DERIVATIVE - The present invention relates to an improved process for the preparation of cis-nucleoside derivative of formula-1 involving chlorination of the compound of formula-2 followed by reaction with compound of formula-3 in presence of a base to get compound of formula-4, reacting the compound of formula-4 with an alkyl halide (RiX) to get a quaternary ammonium salt then with cytosine derivative of formula-5 to provide the compound of formula-6, optionally de-protecting the compound of formula-6 to the compound of formula-7, reducing compound of formula-7 with metal catalyst in presence of a buffer solution, then adding an organic acid to get the compound of formula-8, and converting the compound of formula-8 to cis-nucleoside derivative of formula-1. The present invention further relates to novel cis-nucleoside derivative of formula-8. The present invention also relates to a pharmaceutical composition comprising cis-nucleoside derivative of formula-1 with excipients.11-22-2012
20120295929COMPOSITIONS AND METHODS FOR TREATING AND PREVENTING DERMATOSES - The invention encompasses protectant agents including uracil or a metabolite thereof that effectively prevent and/or treat the cutaneous toxicities and dermatological side-effects associated with chemotherapeutic agents. Additionally, and surprisingly compositions including uracil or a metabolite thereof are effective for treating or preventing various dermatoses.11-22-2012
20100280055Flavoring Systems for Pharmaceutical Compositions and Methods of Making Such Compositions - A flavoring system for a liquid pharmaceutical composition and pharmaceutical compositions containing such flavoring systems are disclosed. Flavoring systems of the invention include at least one sweetening agent, at least two flavored ingredients, and at least one flavor modifier selected from the group consisting of citric acid, sodium citrate, sodium chloride, and mixtures thereof. At least two of the flavored ingredients are selected from the group consisting of a vanilla flavored ingredient, a peppermint flavored ingredient, a menthol flavored ingredient, a cotton candy flavored ingredient, and mixtures thereof. The one or more sweetening agents comprise glycerin, monoammonium glycyrrhizinate, saccharin sodium, acesulfame potassium, high fructose corn syrup, and/or mixtures thereof. Pharmaceutical compositions of the invention include a flavoring system of the invention, a solvent system, and at least one pharmaceutically active agent, such as lopinavir or derivatives thereof, ritonavir or derivatives thereof, or mixtures thereof. Methods for making such liquid pharmaceutical compositions are also disclosed.11-04-2010
20080275072WEEKLY ADMINISTRATION OF DIPEPTIDYL PEPTIDASE INHIBITORS - Pharmaceutical compositions comprising 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile and pharmaceutically acceptable salts thereof are provided as well as kits and articles of manufacture comprising the pharmaceutical compositions as well as methods of using the pharmaceutical compositions.11-06-2008
20080280930Pyrimidinone Compounds and Preparation and Use Thereof - Disclosed are pyrimidinone compounds having formula (I), a preparation and use thereof. The compounds are inhibitors of HMG-CoA reductase, and therefore have antivirus activities and are useful for preventing and treating cardiovascular and cerebrovascular disorders, senile dementia, diabetes mellitus, osteoporosis and tumors, and enhancing immune functions in a subject, and especially useful for treating diseases associated with hyperlipaemia.11-13-2008
20080287476ADMINISTRATION OF DIPEPTIDYL PEPTIDASE INHIBITORS - Pharmaceutical compositions comprising 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile and pharmaceutically acceptable salts thereof are provided as well as kits and articles of manufacture comprising the pharmaceutical compositions as well as methods of using the pharmaceutical compositions.11-20-2008
20080306098Pharmacokinetics of protease inhibitors and other drugs - A method for modulating at least one pharmacokinetic property of a protease inhibitor upon administration to a host is provided. One administers to the host an effective amount of a bifunctional compound of less than about 5000 daltons comprising the protease inhibitor or an active derivative thereof and a pharmacokinetic modulating moiety. The pharmacokinetic modulating moiety binds to at least one intracellular protein. The bifunctional compound has at least one modulated pharmacokinetic property upon administration to the host as compared to a free drug control that comprises the protease inhibitor.12-11-2008
20080275071Radiotherapy Enhancer - The present invention relates to a radiotherapy enhancer that can reduce the radiation dose and adverse drug reactions when used in combination with a cancer radiotherapy. A radiotherapy enhancer comprising (A) tegafur and (B) gimeracil.11-06-2008
200901494864,5-DIPHENYL-PYRIMIDINYL-OXY OR -MERCAPTO SUBSTITUTED CARBOXYLIC ACIDS, METHOD FOR THE PRODUCTION AND USE THEREOF AS MEDICAMENTS - This invention relates to a compound of formula I,06-11-2009
20080269267KINASE INHIBITORS USEFUL FOR THE TREATMENT OF MYLEOPROLIFIC DISEASES AND OTHER PROLIFERATIVE DISEASES - Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanomas, solid tumors, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, hepatic cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, chronic myelogenous leukemia, leukemias, papillary thyroid carcinoma, non-small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, diabetic retinopathy, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocytosis, mast cell leukemia, a disease caused by c-Abl kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, a disease caused by c-Kit kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, a disease caused by c-Met kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, or a disease caused by a Raf kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof.10-30-2008
20090005405COMPOSITIONS AND METHODS FOR TREATING AND PREVENTING DERMATOSES - The invention encompasses protectant agents including uracil or a metabolite thereof that effectively prevent and/or treat the cutaneous toxicities and dermatological side-effects associated with chemotherapeutic agents. Additionally, and surprisingly compositions including uracil or a metabolite thereof are effective for treating or preventing various dermatoses.01-01-2009
20090186913Tetrahalogenated compounds useful as inhibitors of angiogenesis - Methods for inhibiting a neoplasm in a subject and methods of inhibiting undesired angiogenesis that include administering to a subject a therapeutically effective amount of at least one novel tetrahalogenated compound, or a pharmaceutically acceptable salt thereof.07-23-2009
20080318987METHODS FOR MODULATING BONE FORMATION AND MINERALIZATION - Methods and compositions for modulating bone formation and mineralization are described.12-25-2008
20090209563Pyridinoylpiperidines as 5-HT1F agonists - The present invention relates to compounds of formula I:08-20-2009
20090209565THERAPEUTIC AGENT FOR INFLAMMATORY BOWEL DISEASE - The present invention relates to a therapeutic agent for inflammatory bowel disease comprising 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione or a pharmaceutically acceptable salt thereof as an active ingredient.08-20-2009
20090209564Glucagon Receptor Antagonist Compounds, Compositions Containing Such Compounds And Methods Of Use - Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.08-20-2009
20090023763Condensed Pyridine Derivatives Useful as A2B Adenosine Receptor Antagonists - New antagonists of the A01-22-2009
20090082376DEUTERIUM-ENRICHED ALOGLIPTIN - The present application describes deuterium-enriched alogliptin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-26-2009
20090082377Matrix Metalloproteinase Inhibitors - The present invention relates to compounds of Formula (I):03-26-2009
20080262005Uracil-Type Gonadotropin-Releasing Hormone Receptor Antagonists and Methods Related Thereto - Compounds having utility as GnRH receptor antagonists and for treatment of a variety of sex-hormone related conditions in both men and women. Such compounds have the following structure (I): (I) wherein R10-23-2008
20090221618AZABICYCLO (3, 1, 0) HEXAN DERIVATIVES USEFUL AS MODULATORS OF DOPAMINE D3 RECEPTORS - The present invention relates to novel compounds of formula (I) or a salt thereof:09-03-2009
20090221617LEAD COMPOUND OF ANTI-HYPERTENSIVE DRUG AND METHOD FOR SCREENING THE SAME - A system for screening a small molecule library with 250,000 molecules to find out a compound of an anti-hypertensive drug aiming at human Angiotensin II type IA receptor is provided. The system includes a first database having a three-dimensional structure datum of a human Angiotensin II type IA receptor, a second database having molecular data of a plurality of small molecules, and a computer acquiring the three-dimensional structure datum and the molecular data from the first database and the second database respectively, wherein the computer has a molecular docking software for calculating a free energy of the human Angiotensin II type IA receptor bound to each of the plurality of small molecules, ranks the plurality of small molecules according to the respective free energy so as to select a top small molecule in the ranking as the compound of the drug.09-03-2009
20100184788HETEROCYCLIC DERIVATIVES - The invention relates to novel heterocyclic derivatives of the general formula (I), processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction, and heart failure development.07-22-2010
200901708833-ARYLPHENYL SULFIDE DERIVATIVE AND INSECTICIDE AND MITICIDE - 3-Arylphenyl sulfide derivatives represented by general formula (I):07-02-2009
20080214589Thrombin Inhibiting 2,4-Dioxo-3,4-Dihydropyrimidine Derivatives - There is provided a compound of formula I wherein R09-04-2008
20100216826Polymorphisms in Voltage-Gated Sodium Channel Alpha 1-Subunit as Markers for Therapy Selection - A method for determining whether a patient in need thereof will respond to chemotherapy by screening a suitable sample isolated from the patient for a pre-selected polymorphism present in the VGSC gene.08-26-2010
20120196884UREA SUBSTITUTED SULPHONAMIDE DERIVATIVES - The present invention relates to sulphonamide derivatives, whith a urea moiety. The invention also relates to the use of the derivatives as inhibitors of collagen receptor integrins, especially α2β1 integrin inhibitors e.g. in connection with diseases and medical conditions that involve the action of cells and platelets expressing collagen receptors, their use as a medicament, e.g. for the treatment of thrombosis, inflammation, cancer and vascular diseases, pharmaceutical compositions containing them and a process for preparing them. The sulphonamide derivatives have the general formula (I) or (I′).08-02-2012
20110112123Compositions for Intratumoral Administration - The present disclosure describes compositions for intratumoral administration which include a tissue-stabilizing agent and a therapeutic agent.05-12-2011
201002406852-S-Benzyl Substituted Pyrimidines As CRTH2 Antagonists - Provided herein are 2-S-benzyl pyrimidine compounds having CRTH2 (G-protein-coupled chemoattractant receptor, expressed on Th2 cells) antagonistic activity, useful for the prophylaxis and treatment of diseases associated with CRTH2 activity, including the treatment of allergic diseases, eosinophil-related diseases and basophil-related diseases.09-23-2010
20090076045Non-nucleoside reverse transcriptase inhibitors - Compounds of formula I, wherein R03-19-2009
20130190337SOLID DOSAGE FORMS OF HIV PROTEASE INHIBITORS - The present invention relates to a solid dosage form comprising a solid dispersion composition of at least one HIV protease inhibitor and a water-soluble polymer having a glass transition temperature (Tg) of at least about 50° C. in an amount of less than 50% by weight of the dosage form. It also relates to a process of preparation for such solid dosage forms.07-25-2013
20100144771Novel Hydantoin Derivatives for the Treatment of Obstructive Airway Diseases - The invention provides compounds of formula (I):06-10-2010
20100144770Pyrimidinones as Casein Kinase II (CK2) Modulators - A compound having Formula I: or a pharmaceutically acceptable salt thereof, wherein X, R, R and R are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof. The compounds of Formula I are inhibitors of Casein kinase II (CK2) pathways.06-10-2010
20100120806CYCLOPROPANE AMIDES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES - Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including, but not limited to, malignant melanomas, solid tumors, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, hepatic cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, chronic myelogenous leukemia, leukemias, papillary thyroid carcinoma, non-small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, diabetic retinopathy, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocytosis, mast cell leukemia, and diseases caused by PDGFR-α kinase, PDGFR-β kinase, c-KIT kinase, cFMS kinase, c-MET kinase, and oncogenic forms, aberrant fusion proteins and polymorphs of any of the foregoing kinases.05-13-2010
20100222372THERAPEUTIC AGENT FOR INFLAMMATORY BOWEL DISEASE COMPRISING URACIL DERIVATIVE AS ACTIVE INGREDIENT - To provide a therapeutic agent for inflammatory bowel disease.09-02-2010
201201427164-PYRIMIDINESULFAMIDE DERIVATIVE - The invention relates to the compound of structural formula (I) and the salts thereof. Said compound is useful as endothelin receptor antagonist. The invention further relates to a process for preparing said compound.06-07-2012
20120142717COMPOUNDS - The present invention relates to novel compounds that inhibit Lp-PLA06-07-2012
20090318483Potentiators Of Glutamate Receptors - This application relates to a substituted hydroxyphenyl ketone compound of formula I, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof and its use in treating migraine.12-24-2009
20130131092NOVEL AMIDO DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS - The present invention relates to novel compounds of Formula (I), wherein X05-23-2013
20100311773NOVEL ANABASEINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE THEREOF - Disclosed are novel anabaseine derivatives that act as agonists of the α7 nAChR. Also disclosed are pharmaceutical compositions, methods of treating inflammatory conditions, methods of treating CNS disorders, methods for inhibiting cytokine release from mammalian cells and methods for the preparation of the novel compounds.12-09-2010
20100311774Combination Comprising Paclitaxel for Treating Ovarian Cancer - The invention relates to the combination of an endothelin receptor antagonist of formula (I) with paclitaxel, and in particular to this combination for therapeutic use, simultaneously, separately or over a period of time, in the treatment of ovarian cancer.12-09-2010
20130143907PYRAZOLOQUINOLINE DERIVATIVES - A compound and/or pharmacologically acceptable salt thereof represented by the formula (I) has PDE9 inhibitory action, so that the intracerebral cGMP concentration is anticipated to be elevated. The PDE9 inhibitory action and the increase in cGMP lead to the improvement of learning and memory behaviors, and the compound (I) has applicability as a therapeutic agent for cognitive dysfunctions in Alzheimer's disease.06-06-2013
20110009438SUBSTITUTED ISOXAZOLINE COMPOUND AND PEST CONTROL AGENT - There is provided a novel pest control agent, particularly an insecticide or miticide. A substituted isoxazoline compound of General Formula (1):01-13-2011
20110034490N1-acyl-5-fluoropyrimidinone derivatives - This present disclosure is related to the field of N1-acyl-5-fluoropyrimidinones and their derivatives and to the use of these compounds as fungicides.02-10-2011
20110034488METHOD OF ASSAYING 5-FU - The present invention provides methods, compositions, devices and kits for assaying 5-FU.02-10-2011
20110034492N1-SUBSTITUTED-5-FLUORO-2-OXOPYRIMIDINONE-1(2H)-CARBOXAMIDE DERIVATIVES - This present disclosure is related to the field of N1-substituted-5-fluoro-2-oxopyrimidinone-1-(2H)-carboxamides and their derivatives and to the use of these compounds as fungicides.02-10-2011
20110034489SOLID DOSAGE FORMS OF HIV PROTEASE INHIBITORS - The present invention relates to a solid dosage form comprising a solid dispersion composition of at least one HIV protease inhibitor and water soluble polymer having a glass transition temperature (Tg) of at least about 50° C. in an amount of less than 50% by weight of the dosage form. It also relates to a process of preparation of such solid dosage forms.02-10-2011
20110034493N1-SULFONYL-5-FLUOROPYRIMIDINONE DERIVATIVES - This present disclosure is related to the field of N1-sulfonyl-5-fluoropyrimidinones and their derivatives and to the use of these compounds as fungicides.02-10-2011
201100344915-FLUORO-2-OXOPYRIMIDINE- 1(2H)-CARBOXYLATE DERIVATIVES - This present disclosure is related to the field of 5-fluoro-2-oxopyrimidine-1-(2H)-carboxylates and their derivatives and to the use of these compounds as fungicides.02-10-2011
20130150392IMINOPROPENE COMPOUND AND USE THEREOF - The compound (I) or a salt thereof has an excellent controlling activity against pests. Then the compound (I) or a salt thereof is useful for an active ingredient of a pesticidal composition.06-13-2013
20110082163NOVEL URACIL COMPOUND OR SALT THEREOF HAVING HUMAN DEOXYURIDINE TRIPHOSPHATASE INHIBITORY ACTIVITY - Provided is a uracil compound or a salt thereof, which has potent human dUTPase inhibitory activity and is useful as, for example, an antitumor drug.04-07-2011
20090312352COMPOSITIONS AND METHODS FOR TREATMENT OF DISEASE CAUSED BY YERSINIA SPP INFECTION - The invention generally relates to compositions and methods for treatment of disease caused by 12-17-2009
20090062319METHODS OF INHIBITING THE INTERACTION BETWEEN S100 AND THE RECEPTOR FOR ADVANCED GLYCATION END-PRODUCTS - A method of inhibiting an interaction between a S100 protein and the receptor for advanced glycation end-products is provided comprising administering to a subject a therapeutically effective amount of cromolyn, C5, or salt, hydrate, or solvate thereof. In some embodiments, the S100 protein is S100P. In some embodiments, the S100 protein is S100P. In addition, the present invention provides a method of treating a cancer comprising administering to a mammal a therapeutically effective amount of cromolyn, C5, or salt, hydrate, or solvate thereof. Additional methods are also provided.03-05-2009
20110152301Compounds that Inhibit HIV Particle Formation - The present invention describes novel methods of identifying compounds which inhibit HIV particle formation and Rev-dependent HIV production. The present invention also provides methods and compounds for inhibiting HIV particle formation and or treating patients infected with HIV.06-23-2011
20100069416Azabicyclo [3.1.0] Hexyl Derivatives as Modulators of Dopamine D3 Receptors - The present invention relates to certain azabicyclo compounds of formula (I)′:03-18-2010
20090215803Pyrimidinones as Casein Kinase II (CK2) Modulators - A compound having Formula (I) or a pharmaceutically acceptable salt thereof, wherein X, R08-27-2009
20100063078SPIROCOMPOUNDS USEFUL AS MODULATORS FOR DOPAMINE D3 RECEPTORS - The present invention relates to novel compounds of formula (I) or salts thereof:03-11-2010
20130158055Prevention Of Pancreatic Beta Cell Degeneration - The present invention relates to compounds and pharmaceutically acceptable salts thereof and formulations comprising the compounds or a pharmaceutically acceptable salts thereof that are useful in methods of preventing pancreatic beta cell degeneration or methods of treating a disorder associated with pancreatic beta cell degeneration, such as type I diabetes.06-20-2013
20110046169FUSED HETEROCYCLIC DERIVATIVES AND USE THEREOF - The present invention provides a fused heterocyclic derivative having a strong kinase inhibitory activity and use thereof.02-24-2011
20110251220Pharmaceutical compositions comprising gamma secretase modulators - The present invention relates to pharmaceutical compositions comprising gamma secretase modulators as well as to the use of gamma secretase modulators for treating renal disorders, cancer, neurodegenerative disorders as well as related disorders.10-13-2011
20110098313POSITIVE ALLOSTERIC MODULATORS (PAM) - The present invention relates to phenylethynyl compounds of formula I04-28-2011
20110077260METHODS, COMPOSITIONS, AND KITS FOR ORGAN PROTECTION DURING SYSTEMIC ANTICANCER THERAPY - Methods, compositions, and kits are presented for local tissue protection during systemic administration of anticancer therapeutic agents.03-31-2011
201101523002-ALDOXIMINO-5-FLUOROPYRIMIDINE DERIVATIVES - This present disclosure is related to the field of 2-aldoximino-5-fluoropyrimidines and their derivatives and to the use of these compounds as fungicides.06-23-2011
20110077259COMPOSITIONS AND METHODS FOR TREATING AND PREVENTING DERMATOSES - The invention encompasses protectant agents including uracil or a metabolite thereof that effectively prevent and/or treat the cutaneous toxicities and dermatological side-effects associated with chemotherapeutic agents. Additionally, and surprisingly compositions including uracil or a metabolite thereof are effective for treating or preventing various dermatoses.03-31-2011
20080249118Silencing of Tumor-Suppressive Genes by Cpg-Methylation in Prostate Cancer - The present invention relates to method and kits for diagnosing and/or treating prostate cancer. The method and kit relate to the determination and/or modulation of the methylation degree of tumor suppressive genes in biological samples. More particularly, CpG-methylation of 14-3-3σ was found in all primary PCa samples analysed, but not in matching normal prostate epithelial cells or benign prostate hyperplasia (BPH). CpG-methylation was accompanied by a decrease or loss of 14-3-3σ protein expression in primary PCa and PCa cell lines. PCa-precursor lesions, known as prostatic intraepithelial neoplasia (PIN), also displayed decreased levels of 14-3-3σ expression, whereas normal prostate epithelial cells and BPH showed high levels of 14-3-3σ protein expression. The generality of CpG-methylation in PCa suggests that silencing of 14-3-3σ significantly contributes to the formation of PCa. Furthermore, the CpG-methylation of 14-3-3σ in PCa may be exploited for diagnostic purposes.10-09-2008
20110212982Administration of Dipeptidyl Peptidase Inhibitors - Pharmaceutical compositions comprising 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile and pharmaceutically acceptable salts thereof are provided as well as kits and articles of manufacture comprising the pharmaceutical compositions as well as methods of using the pharmaceutical compositions.09-01-2011
20100004273Compounds And Methods For Treating Disorders Related To Glucose Metabolism - The present invention relates to compounds and pharmaceutically acceptable salts thereof, and compositions comprising the same, that are useful in modulating lyn kinase activity, treating obesity, type II diabetes, metabolic syndrome, and in reducing blood glucose level, weight gain, or fat depot level, or treating a disease or condition associated with the same.01-07-2010
200802211401-[2',3' -Dideoxy-3' C-(Hydroxymethyl) - Beta-D-Erythro-Pentofuranosyl] Cytosine Derivatives as Hiv - Compounds of the formula (I) wherein: R09-11-2008
20110212981Method of Determining a Chemotherapeutic Regimen Based on ERCC1 and TS Expression - The present invention relates to prognostic methods which are useful in medicine, particularly cancer chemotherapy. The object of the invention to provide a method for assessing TS and/or ERCC1 expression levels in fixed or fixed and paraffin embedded tissues and prognosticate the Probable resistance of a patient's tumor to treatment with 5-FU and oxaliplatin-based therapies by examination of the amount of TS and/or ERCC1 mRNA in a Patient's tumor cells and comparing it to a predetermined threshold expression level for those genes. More specifically, the invention provides to oligonucleotide prither pairs ERCC1 and TS and methods comprising their use for detecting levels of ERCC1 and TS mRNA, respectively.09-01-2011
20090118315Methods of Treatment Using Sapacitabine - A first aspect of the invention relates to a method of treating leukaemia or myelodysplastic syndromes (MDS), said method comprising administering a therapeutically effective amount of sapacitabine, or a metabolite thereof, to a subject in accordance with a dosing regimen comprising at least one treatment cycle, wherein said treatment cycle comprises administering a therapeutically effective amount of sapacitabine, or a metabolite thereof, for 7 consecutive days every 21 days or 14 consecutive days every 21 days.05-07-2009
20110178110Genotype and Expression Analysis for Use in Predicting Outcome and Therapy Selection - The invention provides compositions and methods for determining the likelihood of successful treatment with a various treatment regimens available to gastrointestinal cancer patients. After determining if a patient is likely to be successfully treated, the invention also provides methods for treating these patients.07-21-2011
20110053967(POLY) AMINOACETAMIDE DERIVATIVES OF EPIPODOPHYLLOTOXIN THEIR PROCESS OF PREPARATION AND THEIR APPLICATIONS IN THERAPEUTICS AS ANTICANCER AGENTS - The present invention relates to novel podophyllotoxin derivatives substituted in the 4-position by a substituted (poly)aminoalkylaminoacetamide chain, to their process of preparation and to their use as medicament as anticancer agents.03-03-2011
20110053966SYNERGISTIC FUNGICIDAL COMPOSITIONS CONTAINING A 5-FLUOROPYRIMIDINE DERIVATIVE FOR FUNGAL CONTROL IN CEREALS - A fungicidal composition containing a fungicidally effective amount of a) a compound of Formula IA and/or IB and (b) at least one fungicide selected from the group consisting of epoxiconazole, prothioconazole, azoxystrobin, pyraclostrobin, penthiopyrad, isopyrazam, bixafen, boscalid, prochloraz, chlorothalanil, isobutyric acid (3S,6S,7R,8R)-8-benzyl-3-[(3-isobutyryloxymethoxy-4-methoxypyridine-2-carbonyl)-amino]-6-methyl-4,9-dioxo-[1,5]dioxonan-7-yl ester, and (5,8-difluoroquinazolin-4-yl)-{2-[2-fluoro-4-(4-trifluoromethylpyridin-2-yloxy)-phenyl]-ethyl}-amine provides synergistic control of selected fungi.03-03-2011
20110053965SULFONATED PRECURSORS OF THYMIDINE FOR THE TREATMENT OF EPITHELIAL HYPERPLASIAS - This invention relates to pharmaceutical compositions comprising a sulfonated biological precursor of thymidine, such as a precursor of 4-thiothymidine (4-TT), and their use in the photodynamic treatment of skin hyperplasias, including cancer, psoriasis, actinic keratosis and keloids, by topical or systemic administration.03-03-2011
20110028502DIHYDROPYRIMIDONE AMIDES AS P2X7 MODULATORS - Compounds of the formula I:02-03-2011
20100286178COMPOUNDS AND USES THEREOF11-11-2010
20110257210BENZIMIDAZOLE DERIVATIVES AND THEIR USE FOR MODULATING THE GABAA RECEPTOR COMPLEX - The present application discloses novel benzimidazole derivatives of general formula (I) or an N-oxide thereof, any of its stereoisomers or any mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein R represents a pyridyl or pyrimidyl group; which pyridyl or pyrimidyl group is optionally substituted with one or more substituents independently selected from the group consisting of: halo, trifluoromethyl, trifluoromethoxy, cyano, nitro, alkyl, hydroxy, hydroxyalkyl and alkoxy, and their use as modulators of the GABA10-20-2011
20100298363Use of carboxyamidotriazole (CAI) orotate in macular degeneration - Method and composition of Carboxyamidotriazole orotate for treating age-related macular degeneration and other angiogenesis-dependent diseases.11-25-2010
20100152215METHODS OF IDENTIFYING ACTIVATORS OF LYN KINASE - The present invention relates to methods of identifying activators of lyn kinase by preincubating a test compound in the presence of lyn kinase; adding ATP and substrate to the lyn kinase and test compound; incubating the test compound, lyn kinase, ATP, and substrate; and measuring phosphorylation level of the substrate, whereby an increase in the phosphorylation of the substrate indicates that the test compound is an activator of lyn kinase.06-17-2010
20090176812HETEROMONOCYCLIC COMPOUND AND USE THEREOF - A compound represented by the formula (I):07-09-2009
20100190810COMPOSITION AND METHOD FOR TREATMENT OF WARTS - Provided is a composition comprising 5-FU and salicylic acid. This composition is useful as a treatment for warts. As opposed to conventional compositions and methods, this composition need only be applied once a day. Also provided are methods for the preparation and use of the composition for treatment of warts.07-29-2010
20100029699MATRIX METALLOPROTEINASE INHIBITORS - The present invention relates to compounds of Formula (I):02-04-2010
20100022568ENDOTHELIN RECEPTOR ANTAGONISTS FOR EARLY STAGE IDIOPATHIC PULMONARY FIBROSIS - This present invention relates to the use of an endothelin receptor antagonist for the preparation of a medicament for the treatment of early stage idiopathic pulmonary fibrosis.01-28-2010
20100016343ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTOR INHIBITORS - The present invention provides compounds and compositions, methods of making them, and methods of using them to modulate α7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other things, neurological, psychiatric and/or inflammatory system.01-21-2010
20090318482TABLET PREPARATION WITHOUT CAUSING A TABLETING TROUBLE - The present invention provides a tablet without causing a tableting trouble, which is superior in the tablet formability, dissolution property of pharmaceutically active ingredient, and the like.12-24-2009
20080262006Selective endothelin type-a antagonists - This invention relates to novel endothelin receptor antagonists that selectively inhibit the interaction between Endothelin-1 (ET-1) and endothelin type-A receptors, their derivatives, acceptable acid addition salts. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by endothelin receptor antagonists, particularly those diseases and conditions that are beneficially treated by selective inhibitors of endothelin type-A receptors.10-23-2008
20100197711BENZOTHIAZOLE COMPOUNDS - The present invention relates to benzothiazole compounds that mimic the activity of BH3 only proteins and are capable of binding to and neutralizing pro survival Bcl 2 proteins. The invention also relates to the use of such compounds in the regulation of cell death or cell survival and the treatment and/or prophylaxis of diseases or conditions associated with the deregulation of cell death or cell survival.08-05-2010
201201497235-METHYL-PIPERIDINE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS FOR THE TREATMENT OF SLEEP DISORDER - This invention relates to heteroaryloxy 5-methyl substituted piperidine derivatives and their use as pharmaceuticals.06-14-2012
20100286179EGFR POLYMORPHISMS PREDICT GENDER-RELATED TREATMENT - The invention provides compositions and methods for identifying a gender-specific cancer patient suitable for treatment with various treatment regimens available to cancer patients. After determining if a patient is suitable for therapy, the invention also provides methods for treating these patients.11-11-2010
20110306624GLUCAGON RECEPTOR ANTAGONIST COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF USE - Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.12-15-2011
20100137345PROPHYLACTIC AND THERAPEUTIC USE OF SIRTUIN INHIBITORS IN TNF-ALPHA MEDIATED PATHOLOGIES - The invention relates to the use of sirtuin inhibitors for reducing TNF-alpha production by cells and organisms. The invention also concerns prophylactic and therapeutic applications of sirtuin inhibitors in TNF-alpha mediated pathologies, such as various inflammatory and autoimmune disorders.06-03-2010
20100041685STAT3 INHIBITORS - Small molecule inhibitors of Stat3 and their derivatives are disclosed. Also described are methods to inhibit cell growth by use of Stat3 inhibitors, and the use of Stat3 inhibitors for the prevention and/or treatment of cancer. Further, inhibitors of Stat3 that also do not inhibit Stat1 are described as well as their derivatives. Methods of screening additional compounds for Stat3 inhibition activity and/or non-inhibition of Stat1 activity are also described herein.02-18-2010
20090054473THERAPY FOR COMPLICATIONS OF DIABETES - A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelin A (ET02-26-2009
20090082378DERIVATIVES OF 4-(2-AMINO-1-HYDROXIETHYL)PHENOL AS AGONISTS OF THE B2 ADRENERGIC RECEPTOR - This present disclosure relates to compounds of formula (I):03-26-2009
20120041009PYRIMIDINE COMPOUND AND ITS USE IN PEST CONTROL - A pyrimidine compound represented by below formula (I) has excellent control activity against pests and is useful as an active ingredient of a pest controlling agent.02-16-2012
20090239887Method of resolution and antiviral activity of 1,3-oxathiolane nucleoside enantiomers - A process for the resolution of a racemic mixture of nucleoside enantiomers that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers. The nucleoside enantiomer (−)-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane is an effective antiviral agent against HIV, HBV, and other viruses replicating in a similar manner.09-24-2009
20110082162SYNERGISTIC FUNGICIDAL COMPOSITION CONTAINING 5-FLUOROCYTOSINE FOR FUNGAL CONTROL IN CEREALS - A fungicidal composition containing a fungicidally effective amount of a) a compound of Formula I and (b) at least one fungicide selected from the group consisting of epoxiconazole, prothioconazole, azoxystrobin, pyraclostrobin, penthiopyrad, isopyrazam, bixafen, boscalid, chlorothalonil and isobutyric acid (3S,6S,7R,8R)-8-benzyl-3-[(3-isobutyryloxymethoxy-4-methoxypyridine-2-carbonyl)-amino]-6-methyl-4,9-dioxo-[1,5]dioxonan-7-yl ester provides synergistic control of selected fungi.04-07-2011
20090023764Use of Pyrimidinedione Derivative for Preventing or Treating Hepatitis C - A pyrimidinedione derivative of formula (I) or a pharmaceutically acceptable salt thereof exhibits excellent inhibitory activity against hepatitis C virus.01-22-2009
20100152216MONOCYCLIC ANILIDE SPIROLACTAM CGRP RECEPTOR ANTAGONISTS - The present invention is directed to compounds of Formula I:06-17-2010
20090099218SYNTHESIS OF NOVEL TUBULIN POLYMERIZATION INHIBITORS: BENZOYLPHENYLUREA (BPU) SULFUR ANALOGS - This invention provides a series of BPU analogues; their synthesis and evaluated biological activity. BPU sulfur analogues were found to possess up to 20 fold increased potency, when compared to compound 1, in various cancerous cell lines.04-16-2009
20090325988Glucocorticoid Mimetics, Methods of Making Them, Pharmaceutical Compositions and Uses Thereof - Compounds of Formula (I)12-31-2009
20120010227FORMULATION FOR NAIL AND NAIL BED DISEASES - The invention relates to a pharmaceutical composition with a content in active ingredient that can be an antimycotic, so that the composition is suitable for the treatment of onychomycoses, in particular severe onychomycoses. The inventive formulation is an ointment-like thermogel at body temperature and an inviscid thermogel at lower temperatures and facilitates the permeation of sufficient active ingredient quantities through human fingernails and toenails, in order to also treat severe onychomycoses.01-12-2012
20120015966PPAR ACTIVE COMPOUNDS - Compounds are described that are active on at least one of PPARα, PPARδ, and PPARγ, which are useful for therapeutic and/or prophylactic methods involving modulation of at least one of PPARα, PPARδ, and PPARγ.01-19-2012
20120022089Solid Pharmaceutical Dosage Form - A solid pharmaceutical dosage form providing improved oral bioavailability is disclosed for inhibitors of HIV protease. In particular, the dosage form comprises a solid dispersion of at least one HIV protease inhibitor and at least one pharmaceutically acceptable water-soluble polymer and at least one pharmaceutically acceptable surfactant, said pharmaceutically acceptable water-soluble polymer having a Tg of at least about 50° C. Preferably, the pharmaceutically acceptable surfactant has an HLB value of from about 4 to about 10.01-26-2012
20120022088PHARMACEUTICAL COMBINATION OF 5-FLUOROURACIL AND DERIVATE OF 1,4-DIHYDROPYRIDINE AND ITS USE IN THE TREATMENT OF CANCER - New compounds of 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid ester type having general formula I01-26-2012
20120022087AMORPHOUS AMBRISENTAN - The invention relates to amorphous ambrisentan, preferably together with a surface stabiliser in the form of a stable intermediate. The invention further relates to methods of producing stable amorphous ambrisentan and pharmaceutical formulations containing stable amorphous ambrisentan.01-26-2012
20120122907Novel Pyrazole Derivatives and their use as Positive Allosteric Modulators of Metabotropic Glutamate Receptors - The present invention relates to novel compounds of Formula (I), wherein M, P, X05-17-2012
20120309777SUBSTITUTED 2-IMIDAZOLIDONES AND ANALOGS - Compounds of formula (I): wherein R12-06-2012
20110039872DEUTERIUM-ENRICHED CAPECITABINE - The present application describes deuterium-enriched capecitabine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.02-17-2011
20110065739NOVEL ISOXAZOLE DRIVATIVE - Disclosed is a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, which has an agonistic activity on GPR120 and is therefore useful for the treatment of diabetes, obesity or hyperlipemia. [In formula (I), the A represents a phenyl group which may be substituted by a lower alkoxy group or the like; the 13 represents a bivalent group produced by removing two hydrogen atoms from a benzene ring which may be substituted by a halogen atom or the like; X represents a lower alkylene group having 2 to 4 carbon atoms in its main chain or the like, wherein a carbon atom constituting the main chain may be substituted by an oxygen atom or the like; and Y represents a hydrogen atom or the like.]03-17-2011
20120157487SULFUR DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS - The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.06-21-2012
20120157486SYNERGISTIC FUNGICIDAL INTERACTIONS OF AMINOPYRIMIDINES AND OTHER FUNGICIDES - A fungicidal composition containing a fungicidally effective amount of a) a compound of Formula I and (b) at least one fungicide selected from the group consisting of myclobutanil, fenbuconazole, difenoconazole, trifloxystrobin, penthiopyrad, fluopyram, boscalid, mancozeb, pyrimethanil, and bixafen provides synergistic control of selected fungi.06-21-2012
20120157485SYNERGISTIC FUNGICIDAL INTERACTIONS OF 5-FLUOROCYTOSINE AND OTHER FUNGICIDES - A fungicidal composition containing a fungicidally effective amount of a) a compound of Formula I and (b) at least one fungicide selected from the group consisting of myclobutanil, fenbuconazole, difenoconazole, trifloxystrobin, pentiopyrad, fluopyram, boscalid, mancozeb, and pyrimethanil provides synergistic control of selected fungi.06-21-2012
20090069353DEUTERIUM-ENRICHED AMBRISENTAN - The present application describes deuterium-enriched ambrisentan, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-12-2009
20090131462Fungicidally Active Agent - The invention relates to a fungicidally active agent containing at least one other defined fungicide in addition to the fungicide N-[2-(1,3-dimethylbutyl)-3-thienyl]-1-methyl-3-(trifluormethyl)-1H-pyrazol-4-carboxamide (penthiopyrad). The invention also relates to a method for controlling pathogenic fungi using one such agent, and to the use of said agent for controlling pathogenic fungi.05-21-2009
20120258978NITROGEN-CONTAINING SIX-MEMBERED AROMATIC RING DERIVATIVES AND PHARMACEUTICAL PRODUCTS CONTAINING THE SAME - Compounds of Formula (I) promote axonal outgrowth angiogenesis and can therefore be used to reduce central nerve injuries such as head injury and spinal cord injury, cerebral infarction, ischemic heart diseases, peripheral arterial occlusive diseases, or after-effects of these diseases.10-11-2012
20110184006METHOD AND COMPOSITION FOR THERMALLY STABILIZING VITAMIN C WITHIN NANO LAYERS OF MONTMORILLONITE CLAY - A thermally stable Vitamin C composition containing montmorillonite, an organic acid containing L-ascorbic acid or a derivative thereof, a divalent cation present within nanolayers of the montmorillonite, wherein the organic acid is combined with the divalent cation within the nanolayers to form an organic acid-montmorillonite chelate.07-28-2011
20120129878TABLET - Provided is a tablet having a high content of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-4-fluorobenzonitrile (compound (A)) or a salt thereof as a pharmaceutically active component. A tablet containing compound (A) or a salt thereof, and a fluidizer, which has a compound (A) content of 35-50 weight %.05-24-2012
20120214831METHOD FOR DETERMINATION OF SENSITIVITY TO ANTI-CANCER AGENT - To provide a marker for determining sensitivity of a patient to an anti-cancer agent, and novel cancer therapeutic means employing the marker.08-23-2012
20100204253Ribosome Structure and Protein Synthesis Inhibitors - The invention provides methods for producing high resolution crystals of ribosomes and ribosomal subunits as well as crystals produced by such methods. The invention also provides high resolution structures of ribosomal subunits either alone or in combination with protein synthesis inhibitors. The invention provides methods for identifying ribosome-related ligands and methods for designing ligands with specific ribosome-binding properties as well as ligands that may act as protein synthesis inhibitors. Thus, the methods and compositions of the invention may be used to produce ligands that are designed to specifically kill or inhibit the growth of any target organism.08-12-2010
20080214590Zalcitabine (Ddc) Boosted Lamivudine (3Tc) Compositions for Antiretroviral Therapy - Boosted cytidine analogue reverse transcriptase inhibitor antiretroviral compound is a new therapeutic anti HIV option, in combination with another drug such as a NRTI or a protease inhibitor. It's heightened and sustained antiretroviral potency is due to the increased intracellular level of 3TC triphosphate, the active form of 3TC. This effect is obtained by combining 3TC, in usual doses, with a reduced dose of ddC, in the same pharmaceutical formulation. The product could be administered twice or even once daily, which is convenient, and does not increase the pill burden for the patient. The reduced ddC dosage prevents the occurrence of ddC related side effects. Other cytidine derivatives (racemic or negative enantiomers) could have the same effects as ddC and could probably be combined with 3TC, and have the same effect. On the other hand, low dose ddC may also increase the intracellular levels of other cytidine derivatives as it does for 3TC. Boosted cytidine analogue reverse transcriptase inhibitor antiretroviral compound could also be formulated in combination with another drug such as another NRTI (e.g. abacavir) or any protease inhibitor in the same capsule or tablet. This approach offers a dual anti-HIV therapy that is as efficacious as the routine triple therapy. In this way the HIV treatment cost could be significantly reduced which is imperative for resource-poor settings. This new formulation is convenient and well tolerated with no additional toxicity than that of the combining drug (NRTI or protease inhibitor) and 3TC. Moreover, this will enable a larger number of patients to benefit from the already known 3TC effects. It will also increase the 3TC effects in those organs or HIV sanctuaries with usually reduced 3TC concentrations or activity. It could be indicated in both the initial as well as in salvage HIV therapy. It could also be used for therapy optimization or simplification. Moreover, in combination with another NRTI such as abacavir, or even alone, it could be beneficial for reducing the HIV harm in resource-poor settings.09-04-2008
20120136017USE OF 4'-THIO-2'-DEOXYNUCLEOSIDES AS ANTI ORTHOPOXVIRUS AGENTS - Compound represented by the formulae:05-31-2012
20100173921Antiretroviral Solid Oral Composition - The present invention provides an antiretroviral solid oral composition comprising one or more antiretroviral drugs, for example protease inhibitors such as lopinavir, ritonavir or a combination thereof with one or more excipients. The invention provides a composition which is smaller for a given amount of said active substance and possesses taste masking property and a process for preparing the composition. The present invention also provides an antiretroviral solid oral composition comprising one or more antiretroviral drugs, for example protease inhibitors such as lopinavir, ritonavir or a combination thereof with at least one water insoluble polymer, wherein the ratio of drug to polymer in the composition ranges from about 1:1 to about 1:6, and a process for preparing the composition.07-08-2010
20120252830Substituted Aminobutyric Derivatives as Neprilysin Inhibitors - The present invention provides a compound of formula I′;10-04-2012
20100048594USE OF CYTOHESIN INHIBITORS FOR CHEMICALLY INDUCING LONGEVITY - The invention relates to compounds selected from among the group comprising general formulas (1), (2), (3), and/or (4) and/or the enantiomers, diastereomers, and derivatives thereof, and the pharmaceutically acceptable salts thereof for producing a medicament used for therapeutically and/or preventively treating disease and pathological conditions linked to regulation of the insulin and/or insulin-like growth factor (IGF) signalling pathway and/or for chemically inducing longevity.02-25-2010
20100197710Methods Of Activating IRS-1 And AKT - The present invention provides methods of activating IRS-1 and/or AKT and methods of treating or preventing IRS-1- and/or AKT-related disease, condition, or disorder.08-05-2010
20100010024USE OF1,4-DIARYL-DIHYDROPYRIMIDINE-2-ON DERIVATIVES FOR TREATING PULMONARY ARTERIAL HYPERTENSION - The present application relates to the use of 1,4-diaryldihydropyrimidin-2-one derivatives of the formula (I) for the treatment and/or prophylaxis of pulmonary arterial hypertension and other types of pulmonary hypertension, and to the use thereof for the manufacture of medicaments for the treatment and/or prophylaxis of pulmonary arterial hypertension and other types of pulmonary hypertension.01-14-2010
20090069355Bicyclic pyrazolone cytokine inhibitors - The present invention relates to 6,7-dihydro-5H-pyrazolo[1,2a]pyrazol-1-ones which inhibit the extracellular release of inflammatory cytokines, said cytokines responsible for one or more human or higher mammalian disease states. The present invention further relates to compositions comprising said 6,7-dihydro-5H-pyrazolo[1,2a]pyrazol-1-ones and methods for preventing, abating, or otherwise controlling enzymes which are understood to be the active components responsible for the herein described disease states.03-12-2009
20120220612PHARMACEUTICAL COMPRISING PPAR AGONIST - An object of the present invention is to provide an agent for promoting proliferation of a meibomian gland epithelial cell and a corneal epithelial cell, as well as provide an agent for treating an ocular disease such as meibomian gland dysfunction or evaporative dry eye.08-30-2012
20120220614SUBSTITUTED BIARYL DERIVATIVES AND METHODS OF USE THEREOF - The present invention relates to Substituted Biaryl Derivatives, compositions comprising a Substituted Biaryl Derivative, and methods of using the Substituted Biaryl Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.08-30-2012
20120220613METHOD FOR DETERMINING SENSITIVITY TO AN ANTICANCER AGENT - To provide a marker for determining sensitivity of a patient to an anti-cancer agent, and novel cancer therapeutic means employing the marker.08-30-2012
20120083503METHOD FOR PREDICTING THERAPEUTIC EFFICACY OF CHEMOTHERAPY ON NON-SMALL-CELL LUNG CANCER - This invention relates to an antitumor agent comprising carboplatin and a combination drug of tegafur/gimeracil/oteracil potassium to be administered to a cancer patient selected according to an expression level of thymidylate synthase gene.04-05-2012
20110124668NOVEL INDOLE DERIVATIVE HAVING, CARBAMOYL GROUP, UREIDO GROUP AND SUBSTITUTED OXY GROUP - The present invention relates to synthetic studies on novel indole derivatives having a carbamoyl group, a ureido group and a substituted oxy group or a salt thereof, and pharmaceutical actions of the derivatives. The compound and a salt thereof represented by the general formula (1) has an IKKβ inhibitory activity and is useful as a preventive and/or therapeutic agent for diseases considered to be associated with IKKβ. In the formula, R05-26-2011
20120232104NOVEL SULFONAMIDES AS L-CPT1 INHIBITORS - The invention is concerned with novel sulfonamide derivatives of formula (I)09-13-2012
20120232103NOVEL 5-FLUOROURACIL DERIVATIVE - The present invention provides a novel antimetabolic anticancer agent that has an excellent balance between antitumor effect and toxicity. Specifically, the present invention provides a medicament containing, as an active ingredient, a 5-fluorouracil derivative represented by Formula (I) or a salt thereof:09-13-2012
20080300265ANTIVIRAL DRUGS FOR TREATMENT OF ARENAVRUS INFECTION - Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to, Arenaviridae (Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, Pichinde, and LCMV), Filoviridae (Ebola and Marburg viruses), Flaviviridae (yellow fever, Omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever and Crimean-Congo hemorrhagic fever).12-04-2008
20080280931POLYMORPHS OF SUCCINATE SALT OF 2-[6-(3-AMINO-PIPERIDIN-1-YL)-3-METHYL-2,4-DIOXO-3,4-DIHYDRO-2H-PYRIMIDIN-1-YLMETHY]-4-FLUOR-BENZONITRILE AND METHODS OF USE THEREFOR - Compositions comprising the succinate salt of 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile (referred to herein as Compound I) which has the formula:11-13-2008
20100249163RENIN INHIBITORS - The present invention relates to piperidinyl-based renin inhibitor compounds having the formula09-30-2010
20100234405PYRIMIDINE NUCLEOSIDE DERIVATIVES AND SALTS THEREOF - A novel pyrimidine nucleoside derivative represented by the following formula (1) and a salt thereof, as well as a pharmaceutical composition comprising the same as an active ingredient have excellent antiviral properties and are useful as antiviral therapeutic agents:09-16-2010
20110245282Compounds - The invention provides a compound according to formula (I): wherein: X is O or S; Y is O or S; each Ar and Ar′ is independently a mono-, bi- or tricyclic aryl or heteroaryl group optionally substituted with one or more substituents selected from halo, alkyl, aryl, heteroaryl, hydroxyl, nitro, amino, alkoxy, alkylthio, cyano, thio, ester, acyl and amido; each R10-06-2011
20120329821PESTICIDAL COMPOSITIONS - The invention disclosed in this document is related to field of pesticides and their use in controlling pests.12-27-2012
20120329820Pyridinoylpiperidines As 5-HT1F Agonists - The present invention relates to compounds of formula I:12-27-2012
20110319439AZA PYRIDONE ANALOGS USEFUL AS MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS - MCHR1 antagonists are provided having the following Formula I:12-29-2011
20110319438NOVEL SULFONAMIDES AS L-CPT1 INHIBITORS - The invention is concerned with novel sulfonamide derivatives of formula (I)12-29-2011
20110319437IMINOPROPENE COMPOUND AND USE THEREOF - The compound (I) or a salt thereof has an excellent controlling activity against pests. Then the compound (I) or a salt thereof is useful for an active ingredient of a pesticidal composition.12-29-2011
20100137344INDUCTION OF ANALGESIA IN NEUROPATHIC PAIN - The present invention relates to agents which are capable of inducing analgesia in chronic neuropathic pain, associated methods and uses thereof. In particular, the present invention provides compounds capable of activating the TRPM8 receptor for the treatment of chronic neuropathic pain.06-03-2010
20130012530New Positive allosteric modulators of nicotinic acetylcholine receptor - The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine α7 receptor.01-10-2013
20100173922Polymorphisms for Predicting Disease and Treatment Outcome - The invention provides compositions and methods for determining the increased risk for recurrence of certain cancers and the likelihood of successful treatment with one or both of chemotherapy and radiation therapy. The methods comprising determining the type of genomic polymorphism present in a predetermined region of the gene of interest isolated from the subject or patient. Also provided are nucleic acid probes and kits for determining a patient's cancer risk and treatment response.07-08-2010
20100130521METHOD OF TREATMENT USING FUSED AROMATIC COMPOUNDS HAVING ANTI-DIABETIC ACTIVITY - Fused aromatic compounds of Formula I are PPAR gamma agonists or partial agonists and are useful for weekly dosing in the treatment or control of type II diabetes, including hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.05-27-2010
20110160235TRIAZOLYL TROPANE DERIVATIVES - This invention relates to novel triazolyl tropane derivatives, their acceptable acid addition salts, solvates, hydrates and polymorphs thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by blocking or reducing the binding ability of the CCR5 receptor.06-30-2011
20080255168METHODS FOR ADMINISTERING DPD INHIBITORS IN COMBINATION WITH 5-FU AND 5-FU PRODRUGS - Methods for improved administration and dosing of DPD inhibitors in combination with 5-FU and/or 5-FU prodrugs are provided, comprising first administering to a patient in need thereof a DPD inhibitor that substantially eliminates activity of the enzyme and thereafter administering 5-FU or a 5-FU prodrug, wherein the level of 5-FU or 5-FU prodrug is in substantial excess of DPD inhibitor in the patient. Also provided are topical formulations comprising DPD, TP and/or UP inhibitors and methods of using same.10-16-2008
20100063079Pyrimidyl Sulphone Amide Derivatives as Chemokine Receptor Modulators - A compound of formula (I), pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof for the treatment of asthma, allergic rhinitis, COPD, inflammatory bowel disease, irritable bowel syndrome, osteoarthritis, osteoporosis, rheumatoid arthritis, psoriasis or cancer.03-11-2010
20080249119Homogemcitabines - The invention relates to homogemcitabines of general formula (2), with the meanings for the substituents as given in claim 10-09-2008
20080227798POLYMORPHS OF SUCCINATE SALT OF 2-[6-(3-AMINO-PIPERIDIN-1-YL)-3-METHYL-2,4-DIOXO-3,4-DIHYDRO-2H-PYRIMIDIN-1-YLMETHY]-4-FLUOR-BENZONITRILE AND METHODS OF USE THEREFOR - Compositions comprising the succinate salt of 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile (referred to herein as Compound I) which has the formula:09-18-2008
20110263627N3-SUBSTITUTED-N1-SULFONYL-5-FLUOROPYRIMIDINONE DERIVATIVES - This present disclosure is related to the field of N3-substituted-N1-sulfonyl-5-fluoropyrimidinones and their derivatives and to the use of these compounds as fungicides.10-27-2011
20110263626NOVEL BRADYKININ B1-ANTAGONISTS - The present invention relates to compounds of general formula I10-27-2011
20120252829TIVOZANIB AND CAPECITABINE COMBINATION THERAPY - A method of treating a tumor in a subject using a combination of tivozanib and capecitabine is disclosed.10-04-2012
20110269785Substituted 2-Aminoacetamides and the Use Thereof - The invention is directed to substituted 2-aminoacetamides represented by formula (II):11-03-2011
20130172377ADMINISTRATION OF DIPEPTIDYL PEPTIDASE INHIBITORS - Pharmaceutical compositions and methods comprising 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile or a pharmaceutically acceptable salt thereof administered once weekly.07-04-2013
20130116269CYCLIC N,N'-DIARYLTHIOUREAS AND N,N'-DIARYLUREAS - ANDROGEN RECEPTOR ANTAGONISTS, ANTICANCER AGENT, METHOD FOR PREPARATION AND USE THEREOF - The present invention relates to novel cyclic N,N′-diarylureas and N,N′-diarylthioureas—androgen receptor antagonists, anti-cancer agent, pharmaceutical composition, medicament, and method for treatment of cancerous diseases, among them prostate cancer.05-09-2013
20130158056ALKOXY PYRIMIDINE PDE10 INHIBITORS - The present invention is directed to 2-alkoxy pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.06-20-2013
20080200485Kinase Inhibitors - Disclosed are protein kinase inhibitors, compositions comprising such inhibitors, and methods of use, thereof. More particularly, disclosed are inhibitors of Aurora-2 (Aurora-A) protein kinase. Also disclosed are methods of treating diseases associated with protein kinases, especially diseases associated with Aurora-2, such as cancer.08-21-2008
20090069354DEUTERIUM-ENRICHED GEMCITABINE - The present application describes deuterium-enriched gemcitabine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-12-2009
20100292261QUORUM SENSING ANTAGONIST, METHOD OF PREVENTING A BIOFILM FORMATION USING THE QUORUM SENSING ANTAGONIST AND METHOD OF REDUCING A BACTERIAL CONTAMINATION USING THE QUORUM SENSING ANTAGONIST - In the quorum sensing antagonist blocking the communication in bacteria, the method for preventing biofilm formation using this quorum sensing antagonist and the method for reducing the bacterial contamination, the quorum sensing antagonist contains the homoserine lactone moiety and sulfanylethanoyl group, and has a similar chemical structure to that of the autoinducer which is produced by bacteria as a signal, whereby the quorum sensing antagonist can inhibit the formation of biofilm and reduce the bacterial contamination as well.11-18-2010
20130131093Novel Dihydropyrimidin-2(1H)-One Compounds As Neurokinin-3 Receptor Antagonists - The present invention is directed to novel dihydropyrimidin-2(1H)-one compounds useful as Neurokinin-3 (NK3) receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of making and using the same.05-23-2013
20100305145Substituted Aminobutyric Derivatives as Neprilysin Inhibitors - The present invention provides a compound of formula I′;12-02-2010
20130131091HARMFUL ORGANISM CONTROL AGENT - The present invention provides a composition for use as a harmful organism control agent comprising as an active ingredient one or more of compounds represented by formula (I) or salts thereof and an agriculturally or zootechnically acceptable carrier.05-23-2013
20120283281NEW (POLY)AMINOALKYLAMINOALKYLAMIDE, ALKYL-UREA, OR ALKYL-SULFONAMIDE DERIVATIVES OF EPIPODOPHYLLOTOXIN, A PROCESS FOR PREPARING THEM, AND APPLICATION THEREOF IN THERAPY AS ANTICANCER AGENTS - The present invention relates to new derivatives of epipodophyllotoxin 4-substituted with an optionally substituted (poly)aminoalkylaminoalkylamide, or alkyl-urea or alkyl-sulfonamide chain, a process for preparing them and their use as a medicine as an anticancer agent.11-08-2012
20130123288POLYSUBSTITUTED DERIVATIVES OF 2-HETEROARYL-6-PHENYLIMIDAZO[1,2-a]PYRIDINES, AND PREPARATION AND THERAPEUTIC USE THEREOF - Compounds of formula (I):05-16-2013
20110312984STAT3 INHIBITORS - Small molecule inhibitors of Stat3 and their derivatives are disclosed. Also described are methods to inhibit cell growth by use of Stat3 inhibitors, and the use of Stat3 inhibitors for the prevention and/or treatment of cancer. Further, inhibitors of Stat3 that also do not inhibit Stat1 are described as well as their derivatives. Methods of screening additional compounds for Stat3 inhibition activity and/or non-inhibition of Stat1 activity are also described herein.12-22-2011
20110312983DEUTERIUM-ENRICHED ALOGLIPTIN - The present application describes deuterium-enriched alogliptin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.12-22-2011
20130190336STABLE PHARMACEUTICAL COMPOSITIONS COMPRISING A PYRIMIDINE-SULFAMIDE - The invention relates to stable pharmaceutical compositions comprising the compound of the below formula, or pharmaceutically acceptable salts, solvates, hydrates or morphological forms thereof07-25-2013
20130190338SULFUR DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS - The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.07-25-2013
20120004252NEW CCR2 RECEPTOR ANTAGONISTS AND USES THEREOF - The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.01-05-2012
20120029000PROCESS FOR THE PREPARATION OF ALOGLIPTIN - The present invention is based on the discovery of a process for preparing pyrimidin-dione compounds, especially alogliptin and its derivatives, which comprises the reaction of a urea derivative of formula (VIII) with a malonic acid or its derivatives to form intermediates of formulae (VII) or (VII-A), which are subsequently converted to a compound of formula (II) upon introduction of a leaving group X. Compound (II) then reacts with an amine to form compound (I), which is optionally converted to its salts of formula (IV).02-02-2012
20130203790SULFUR-CONTAINING COMPOUNDS AS ANTI-PROLIFERATIVE AGENTS - Novel sulphur-containing compounds and pharmaceutically acceptable salts thereof are disclosed, which have utility as anti-proliferative agents against mammalian cells. The invention provides a method for synthesizing the sulphur-containing compounds.08-08-2013
20130203791Tablets and Preparation Thereof - The present invention features processes of making tablets having reduced internal fractures. In one aspect, the processes comprise the steps of (1) compressing a pre-tabletting material in a die to form a tablet, where an internal surface of the die is lubricated with at least one lubricant, and the pre-tabletting material comprises at least one therapeutic agent and at least one pharmaceutically acceptable polymer; and (2) ejecting said tablet from said die. In another aspect, the processes employ a granular or powdery pre-tabletting material which comprises at least one therapeutic agent and at least one pharmaceutically acceptable polymer, wherein 90% of the particles in the pre-tabletting material are smaller than 400 μm.08-08-2013

Patent applications in class Chalcogen bonded directly to pyrimidine at 2-position