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1,3-thiazoles (including hydrogenated)

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

514359000 - Five-membered hetero ring containing at least one nitrogen ring atom (e.g., 1,2,3-triazoles, etc.)

Patent class list (only not empty are listed)

Deeper subclasses:

Class / Patent application numberDescriptionNumber of patent applications / Date published
514366000 Polycyclo ring system having the thiazole ring as one of the cyclos 121
514370000 Nitrogen bonded directly to ring carbon of the thiazole ring 86
514369000 Chalcogen bonded directly to ring carbon of the thiazole ring 71
Entries
DocumentTitleDate
20130030028DESFERRITHIOCIN POLYETHER ANALOGUES - Compounds represented by structural formulas described herein, such as Structural Formula (I):01-31-2013
20130030027HEMI-PHORBOXAZOLE A DERIVATIVES AND METHODS OF THEIR USE - The present invention is directed to hemi phorboxazole A: and its stereoisomers, as well as derivatives of hemi phorboxazole A of formula I: wherein ring A is aryl or a 5- or 6-membered heteroaryl optionally substituted with one or more of halogen, —OH, or —C01-31-2013
20120184586DESFERRITHIOCIN POLYETHER ANALOGUES AND USES THEREOF - Desferrithiocin analogues represents by the structural formulae described here, such as formula (I), are useful in treating conditions such as metal overload (e.g., iron overload from transfusion therapy), oxidative stress, and neoplastic and preneoplastic conditions.07-19-2012
20090105317VEGF Inhibition - The present invention provides methods for inhibiting VEGF production or secretion in a subject comprising administering to the subject an effective amount of a compound of Formula I. The invention also provides methods for the treatment or prevention of conditions associated with abnormal levels of VEGF production or secretion.04-23-2009
20100113538N-HYDROXY-4- BENZAMIDINE 2 ETHANSULFONIC ACID SALT, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}benzamidine 2 ethansulfonic acid salt, a process for the preparation thereof, a pharmaceutical composition for preventing and treating osteoporosis, bone fractures or allergic inflammatory diseases, comprising the same, and an oral formulation for preventing and treating osteoporosis, bone fractures or allergic inflammatory diseases, comprising the same are described.05-06-2010
20100076035Transdermal Drug Delivery using an Osmolyte and Vasoactive Agent - A formulation and method for delivery of bioactive substances when applied to, or within, the skin or other exterior region of a mammal. for example, a patient, includes a vasoactive agent; an osmolyte; and an active ingredient. The formulation is sufficiently hygroscopic so as to create a condition of hypertonicity when absorbed by the skin. When the formulation is applied to the skin, the vasoactive agent can be delivered to the dermis so as to contact the vasculature of a patient.03-25-2010
201000760342-ARYL-2-FLUOROPROPANOIC ACIDS AND DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - The present invention relates to (R,S) 2-aryl-2-fluoropropanoic acids, their single enantiomers (R) and (S), their derivatives amides and acylsulfonamides and to pharmaceutical compositions containing them, which are used in the prevention and treatment of tissue damage due to the exacerbated recruitment of polymorphonucleated neutrophils (PMN leukocytes) at inflammation sites. The present invention provides compounds for use in the treatment of psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigo, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the treatment of damages caused by ischemia and reperfusion.03-25-2010
20100331378AMINOTRIAZOLE DERIVATIVES AS ALX AGONISTS - The invention relates to aminotriazole derivatives of formula (I),12-30-2010
20100041723Thiazole Compound (as PPAR delta) Ligand and Pharmaceutical, Cosmetic and Health Food Comprised Thereof - The present invention relates to a thiazole compound as a peroxisome proliferator activated receptor δ (PPARδ) activator or pharmaceutically acceptable salts thereof, and a pharmaceutical composition, a functional cosmetic composition, a health food, health beverages, a food additive and animal feeds containing the same.02-18-2010
20090156651Heterocyclylethylbenzamide Derivatives - A compound of general formula (I):06-18-2009
20100105744SUBSTITUTED 7-SULFANYLMETHYL-, 7-SULFINYLMETHYL- AND 7-SULFONYLMETHYLINDOLES AND THE USE THEREOF - The present application relates to novel 7-sulfanylmethyl-, 7-sulfinylmethyl- and 7-sulfonylmethylindole derivatives, processes for the preparation thereof, the use thereof alone or in combinations for the treatment and/or prevention of diseases, and the use thereof for the manufacture of medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular disorders.04-29-2010
20120214853ITE for Cancer Intervention and Eradication - A method of cancer intervention or eradication by administering an effective amount of an endogenous ligand for the aryl hydrocarbon (Ah) receptor (AhR) named ITE or one of its analogs (the active ingredient) to a subject with cancer is disclosed. An effective dose and dosing frequency of the active ingredient are determined by measuring its blood levels of the subject after dosing. The active ingredient formulated with a carrier system is applied topically, enterally, or parenterally to the subject. The formulated drug can also be administered together with one or more of other cancer therapeutic agents. A maintenance dosing is provided after the subject is free of cancer to insure the cancer eradication. Subjects with cancers of prostate, liver, lung, ovarian, and breast are preferably accepted for treatment.08-23-2012
20090124673Method for treating diabetic nephropathy - Provided, among other things, is a method of treating or ameliorating or preventing an indication of the invention in an animal, including a human comprising administering an effective amount of a compound of the formula I:05-14-2009
20100069448HUMAN PROTEIN TYROSINE PHOSPHATASE INHIBITORS AND METHODS OF USE - The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-β) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising said human protein tyrosine phosphatase beta (HPTP-β) inhibitors, and to methods for regulating angiogenesis.03-18-2010
20130045999SUBSTITUTED (THIAZOLYL-CARBONYL)IMIDAZOLIDINONES AND USE THEREOF - The present invention relates to novel substituted furancarboxamides, methods for their production, their use for the treatment and/or prevention of diseases, as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially retroviral diseases, in humans and/or animals.02-21-2013
20090306155THIAZOLES, IMIDAZOLES, AND PYRAZOLES USEFUL AS INHIBITORS OF PROTEIN KINASES - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and the compositions in the treatment of various disease, conditions, or disorders. The invention also relates to processes for preparing compounds of the inventions.12-10-2009
20130072528Methods for Treating HCV - The present invention features interferon-free therapies for the treatment of HCV. The therapies comprise administering Compound I (or a pharmaceutically acceptable salt thereof) and another anti-HCV agent. Preferably, the therapies are both interferon- and ribavirin-free.03-21-2013
201300598952',2-DITHIAZOL NON-NUCLEOSIDE COMPOUNDS, PREPARATION METHODS, PHARMACEUTICAL COMPOSITIONS AND USES AS HEPATITIS VIRUS INHIBITORS THEREOF - The present disclosure belongs to the field of pharmaceutical chemistry, and relates to a class of 2′,2-bisthiazole non-nucleoside compounds of following formula I, the preparation method and the pharmaceutical composition thereof. The compounds have both the anti-HBV and anti-HCV activities and are useful in treating hepatitides B and C. Pharmacokinetic tests showed the compounds have good bioavailability.03-07-2013
20090270466Epothilones C, D, E, and F, Preparation and Compositions - The present invention relates to epothilones C, D, E, and F, their preparation and their use for the production of therapeutic compositions and compositions for plant protection.10-29-2009
20090270465USE OF EPOTHILONE D IN TREATING TAU-ASSOCIATED DISEASES INCLUDING ALZHEIMER'S DISEASE - Methods of treating Tau-associated diseases, preferably tauopathies, are described using epothilone D that exhibit good brain penetration, long half-life, and high selective retention in brain, and provides effective therapies in treating tauopathies including Alzheimer's disease.10-29-2009
20090069394CANCER TREATMENT WITH EPOTHILONES - The present invention relates to an in vivo regimen for the treatment of a proliferative disease, including non small cell lung carcinoma, where an epothilone, including epothiline B, is administered in a loading dose followed by at least one maintenance doses.03-12-2009
20090326020COMPOUNDS FOR TREATMENT OF CANCER - Compounds according to formula (I) are disclosed12-31-2009
20090012133Polymorphic Form of -Acetic Acid - The present invention relates to a novel polymorphic form of the compound {2-methyl-4-[4-methyl-2-(4-trifluoromethylphenyl)thiazol-5-ylmethylthio]phenoxy}-acetic acid, methods of preparing it, pharmaceutical compositions and medicaments containing the same, and use of such polymorphs, compositions and medicaments in the treatment of PPAR mediated diseases or conditions.01-08-2009
20080293784EPOTHILONES C, D, E AND F, PREPARATION AND COMPOSITIONS - The present invention relates to epothilones C, D, E and F, their preparation and their use for the production of therapeutic compositions and compositions for plant protection.11-27-2008
20130165487Seed Treatment Formulations - The present invention generally relates to aqueous seed treatment formulations comprising from about 0.2 to about 15% of at least one pesticidal agent, from about 0.1 to about 0.45% of at least one graft copolymer, at least one polyvinyl alcohol (PVA), and from about 5 to about 30% of at least one plasticizer. The present invention also relates to aqueous seed treatment formulations wherein the pesticidal agents are clothianidin, metconazole, and metalaxyl.06-27-2013
20130165488Novel Thromboxane A2 (TP) Receptor Antagonists - The present invention relates to novel TP receptor antagonists, which optionally cross the blood-brain barrier of a mammal. The invention also provides methods for treating a disorder related to activation of TP receptor utilizing the compounds of the invention.06-27-2013
20080207708Oxazole and Thiazole Compounds and Their Use in the Treatment of Pge2 Mediated Disorders - Compounds of formula (I) or a pharmaceutically acceptable derivative thereof:08-28-2008
20110281918Antifungal Composition - A pharmaceutical composition for oral administration which is self-emulsifying on contact with an aqueous phase, in particular gastrointestinal fluids, and which comprises: (a) an antifungally active compound of formula (I) wherein R11-17-2011
20110281919AGENT FOR TREATING OR PREVENTING DIGESTIVE ULCER - An object of the present invention is to provide an agent for treating or preventing digestive ulcer that is effective even to ulcer of small intestine and others, for which gastric acid secretion inhibitors such as proton pump inhibitors are ineffective, and is superior to allopurinol in the efficaciousness and the safety.11-17-2011
20110301209METHODS AND COMPOSITIONS FOR THE TREATMENT OF CANCER, TUMORS, AND TUMOR-RELATED DISORDERS - Described herein are compositions and methods for using these compositions in the treatment of cancer, tumors, and tumor-related disorders in a subject.12-08-2011
20100144804Polymorph of a Pharmaceutical - A new crystalline polymorph of ritonavir and methods for its use and preparation are disclosed.06-10-2010
20100137382Therapeutic formulations of desoxyepothilones - Formulations of desoxyepothilones are stable before and after dilution into aqueous media. 06-03-2010
20100035944COMPOUNDS AND METHODS FOR MODULATING G PROTEIN-COUPLED RECEPTORS - The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating G protein-coupled receptor 20 (GPR20), and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated GPR20.02-11-2010
20090099243ORGANIC COMPOUNDS - The invention relates to compound of the formula (I)04-16-2009
20100120875USE OF 4-[(4-THIAZOLYL)PHENOXY]ALKOXY-BENZAMIDINE DERIVATIVES FOR TREATMENT OF OSTEOPOROSIS - A method of treating osteoporosis comprising administering to a subject a composition comprising a compound, 4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}-benzamidine or a salt thereof, is described. A method of inhibiting osteoclast activity and stimulating osteoblast activity in a subject also is described.05-13-2010
20120065235COMPOUNDS FOR TREATING PROLIFERATIVE DISORDERS - Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.03-15-2012
20100249199Hard Surface Treatment Compositions with Improved Mold or Fungi Remediation Properties - Provided are hard surface treatment compositions which provide improved mold and/or fungi remediation properties which compositions are formed from two aqueous mixtures which are admixed immediately prior to use or upon use. The hard surface treatment compositions contain an oxidizing agent, preferably a hypochlorite. In addition to a mold and/or fungi remediation effect, the composition may also be useful in the cleaning treatment and/or disinfection or sanitization treatment of hard surfaces. Methods for the remediation of mold and/or mold spores and/or fungi on surfaces are also disclosed.09-30-2010
20120035227DEUTERIUM-ENRICHED IXABEPILONE - The present application describes deuterium-enriched ixabepilone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.02-09-2012
20090088461Methods of Treating or Preventing Cardiac Disease Associated With a High Fat Diet - The present invention relates to a method of treating or preventing cardiac disorders, myocardial inflammation or myocardial oxidative stress associated with a high fat diet or in a patient subjected to a high fat diet using the thiazolium compounds and compositions of the invention. The present invention also relates to a method of ameliorating weight gain, myocardial AGE accumulation associated, mitochondrial superoxide production, RAGE expression or PPARα expression with a high fat diet or in a patient subjected to a high fat diet using the thiazolium compounds and compositions of the invention.04-02-2009
20090182022Treatment of Fatty Liver - Methods and compositions comprising peroxisomal and/or mitochondrial beta oxidation stimulating agents to reverse or resolve, slow the progression of, treat or prevent the development of fatty liver and conditions stemming from fatty liver, such as NASH, liver inflammation, cirrhosis and liver failure. An active agent that by itself is associated with an increased risk of fatty liver development and conditions stemming from fatty liver, such as NASH, liver inflammation, cirrhosis and liver failure, may be administered in combination with peroxisomal and/or mitochondrial beta oxidation stimulating agents. A combination regimen involving such agents, as simultaneous or concomitant therapy, or as a fixed dosage form, is also provided.07-16-2009
20080207709Thiazole Derivatives for Treating Dyskinesias Caused by a Chemical Treatment - The invention relates to the use of derivatives of thiazoles having general formula (I) for the preparation of a medicament for the treatment or prevention of dyskinesias caused by a chemical treatment. The invention also relates to a combination of thiazole derivatives having general formula (I) and at least one compound selected from among neuroleptics or products that act on the dopaminergic system for the treatment or prevention of dyskinesias caused by a chemical treatment.08-28-2008
20090275622NIZATIDINE FORMULATIONS - Pharmaceutical formulations comprising nizatidine or salts thereof. Further the invention relates to liquid pharmaceutical formulations comprising nizatidine or salts thereof.11-05-2009
20090281152Indole Compounds Having Affinity to the EP1 Receptor - Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: formula (I) wherein R11-12-2009
20090286838TREATMENT FOR CANCER - The present invention provides methods for the treatment of tumors, comprising administration of an effective amount of at least one taxoid and an effective amount of at least one benzimidazol carbamate compound of formula (I). The invention also provides a method for the treatment of tumors insensitive to one or more anti-mitotic drugs, the method comprising administering an effective amount of at least one benzimidazole carbamate compound of formula (I). Also provide are compositions for carrying out methods of the invention.11-19-2009
20100113539COMPOUNDS FOR TREATING OPHTHALMIC DISEASES AND DISORDERS - Provided are compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.05-06-2010
20080287509Pharmaceutical Composition for the Treatment of Bone Fracture - Disclosed herein is a composition for the treatment bone fracture comprising N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxyl-benzamidine, 4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}-benzamidine or pharmaceutically acceptable salts thereof as a medicinally effective ingredient. The composition of the present invention can significantly reduce the volume of bony callus, and increase bony density and strength of bony callus, and decrease the contents of connective tissue and cartilage tissue in bony callus, and thus promote loss and ossification of the bony callus formed during the fracture healing process. Therefore, the composition of the present invention is useful for the treatment of bone fracture.11-20-2008
20080312300Processes for the Preparation of Stable Polymorphic Form I of Ritonavir - The invention relates to processes for the preparation of a polymorphic form of ritonavir. More particularly, it relates to the preparation of a stable polymorphic Form I of ritonavir. The invention also relates to pharmaceutical compositions that include the stable Form I of ritonavir and use of the compositions for treatment of HIV infections in combination with other antiretro viral agents.12-18-2008
20080242708Biphenyl-Thiazolo-Carboxamides - Novel biphenyl thiazole carboxamides of Formula (I)10-02-2008
20090030050Heterocyclic Compounds, Compositions Comprising Them and Methods of Their Use - Heterocyclic compounds, compositions comprising them, and methods of their use for the treatment, prevention and management of inflammatory and autoimmune diseases and disorders are disclosed. Particular compounds are of formula I:01-29-2009
20080234337Preventive and/or Remedy for Hyperkalemia Containing Ep4 Agonist - The present invention relates to a preventive and/or therapeutic agent for hyperkalemia, and a potassium excretion promoter containing EP09-25-2008
200903260193,4-BICYCLIC PYRROLIDINE ANTIVIRALS - The present invention discloses compounds of formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:12-31-2009
20090326021THIAZOLO NAPHTHYL ACIDS - The present invention relates to thiazolo-naphthyl acids of the formula12-31-2009
200903260182-Phenyl indene derivatives useful as estrogen receptor ligands - The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity. Formula (I), wherein R12-31-2009
20130217734ACTIVATING AGENT FOR PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR DELTA - A compound represented by the following general formula (II) or a salt thereof is used as an activator of PPARδ.08-22-2013
20130217735FUNGICIDAL COMPOSITIONS AND METHODS OF USE - Disclosed are compositions and methods of preparing compositions of active fungicidal ingredients. Also disclosed are methods of using the compositions described herein to improve fungicide penetration into the plant tissue, reduce fungicide volatility and drift, decrease water solubility of the fungicides, and introduce additional biological function to fungicides.08-22-2013
20110230528Use of Epothilone D in Treating Tau-Associated Diseases Including Alzheimer's Disease - Methods of treating Tau-associated diseases, preferably tauopathies, are described using epothilone D that exhibit good brain penetration, long half-life, and high selective retention in brain, and provides effective therapies in treating tauopathies including Alzheimer's disease.09-22-2011
20090192203COMPOUNDS AND COMPOSITIONS AS PPAR MODULATORS - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families.07-30-2009
20090105316Biphenyl Thiazole Carboxamides - Novel biphenyl thiazole carboxamides of Formula (I)04-23-2009
20090105318Amidoethylthioether Orexin Receptor Antagonists - The present invention is directed to amidoethylthioether compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.04-23-2009
20120077855CRYSTALLINE TRIPEPTIDE EPOXY KETONE PROTEASE INHIBITORS - The disclosure features crystalline tripeptide keto epoxide compounds, methods of their preparation, and related pharmaceutical compositions.03-29-2012
20090247592Epothilones C, D, E, and F, Preparation and Compositions - The present invention relates to epothilones C, D, E, and F, their preparation and their use for the production of therapeutic compositions and compositions for plant protection.10-01-2009
20100160393CRYSTAL FORM OF EPOTHILONE B AND USE IN PHARMACEUTICAL COMPOSITIONS - The invention relates to new crystal forms of epothilone B.06-24-2010
20090298896ACTIVATING AGENT FOR PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR DELTA - A compound represented by the following general formula (II) or a salt thereof is used as an activator of PPARδ.12-03-2009
20090298895USE OF THIOPROLINE IN BODY WEIGHT REDUCTION TREATMENTS - The invention relates to thioproline, pharmaceutically acceptable salts and/or prodrugs thereof that can be used as anorexia-inducing agents in both therapeutic and cosmetic treatments to reduce body weight.12-03-2009
20130190366SUBSTANTIALLY PURE SALTS OF FEBUXOSTAT AND PROCESSES FOR PREPARATION THEREOF - Substantially pure salts of febuxostat of Formula (IA): wherein Y is Na07-25-2013
20130190367FLUORINATED THIAZOLES FOR USE IN TREATING CANCER - Compounds of formula (I) or their pharmaceutically acceptable salts, or their stereoisomers or mixtures of stereoisomers, where: R07-25-2013
20110060018INSECTICIDAL N-SUBSTITUTED (2-SUBSTITUTED-1,3-THIAZOL)ALKYL SULFOXIMINES - N-Substituted (2-substituted-1,3-thiazol)alkyl sulfoximines are effective at controlling insects.03-10-2011
20100152255Organic Compounds - Compounds of the formula06-17-2010
20100240721SYNTHESIS OF EPOTHILONES, INTERMEDIATES THERETO, ANALOGUES AND USES THEREOF - The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype.09-23-2010
20100160394USE OF 4-[(4- THIAZOLYL)PHENOXY]ALKOXY-BENZAMIDINE DERIVATIVES FOR THE PROPHYLAXIS AND TREATMENT OF OSTEOPOROSIS - This invention relates to a pharmaceutical composition containing 4-[(4-thiazolyl)phenoxyl]alkoxy-benzamidine derivatives expressed by the following formula 1 for the prophylaxis and treatment of osteoporosis and more particularly, to the use of 4-{5-[4-(5-isoproply-2-methyl-1,3-thiazol-4-yl)phenoxyl]pentoxy}-benzamidine or N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxyl]pentoxy}-benzamidine expressed by the following formula 1 as a pharmaceutical composition for the prophylaxis and treatment of osteoporosis.06-24-2010
20090076101Thiophene and Thiazole Substituted Trifluoroethanone Derivatives as Histone Deacetylase (HDAC) Inhibitors - The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts and tautomers thereof. Compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative diseases, including cancer. They are also useful for treating neurodegenerative diseases, mental retardation, 10 schizophrenia, inflammatory diseases, restenosis, immune disorders, diabetes, cardiovascular disorders and asthma.03-19-2009
20090076100DEUTERIUM-ENRICHED GSK625433 - The present application describes deuterium-enriched GSK625433, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-19-2009
20090076098METHODS, KITS, AND COMPOUNDS FOR DETERMINING RESPONSIVENESS TO TREATMENT OF A PATHOLOGICAL DISORDER BY EPOTHILONES - The invention provides methods, kits and compounds for determining the potential responsiveness of a subject suffering from a pathological disorder, including non-small cell lung cancer (NSCLC), to treatment with an epothilone by analyzing the gene expression profile and/or certain molecular markers in a sample obtained from said subject. The invention further relates to methods, compounds and uses of said compounds for treating subjects suffering from said pathologic disorder, optionally in combination with other therapeutic agents. Also provided are genes and/or proteins encoded by them whose expression level have been determined to differ between epothilone responders and epothilone non-responders.03-19-2009
20110112155METHODS FOR TREATING CANCER IN PATIENTS HAVING BREAST CANCER RESISTANCE PROTEIN OVEREXPRESSION - A method for treating cancer comprising identifying a mammal that overexpresses breast cancer resistance protein; and administering to said mammal a pharmaceutical composition comprising a therapeutically effective amount of ixabepilone. In one aspect, the mammal is not administered an agent that is susceptible to breast cancer resistance protein overexpression resistance. In another aspect, the cancer is breast and/or lung cancer.05-12-2011
20100261769Topical Compositions Comprising Non-Proteogenic Amino Acids and Methods of Treating Skin - Cosmetic compositions comprising non-natural, non-proteogenic amino acids and methods of using such compositions to impart antiaging benefits to the skin are disclosed. The non-natural, non-proteogenic amino acids are believed to have modulatory activity against one or more biochemical pathways implicated in skin aging, and in particular, are enhancers of LOXL-1.10-14-2010
20090176846N-hydroxy-4- {5- [4- (5-isopropyl-2-methyl-1, 3-thiazol-4-yl) phenoxy] pentoxy} benzamidine 2 methanesulfonic acid salt - Disclosed is an N-Hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy} benzamidine 2 methansulfonic acid salt, which has excellent bioavailability. Also disclosed are a method of preparing the compound and a pharmaceutical composition comprising the compound.07-09-2009
20090149517NOVEL 2-SUBSTITUTED TIAZOLE-4-CARBOXAMIDE DERIVATIVES, THEIR PREPARATION AND USE AS PHARMACEUTICALS - The present invention relates to 2-substituted thiazole-4-carboxamide derivatives of the formula (I), the use thereof as medicament for the treatment of various disorders, and processes for the preparation thereof06-11-2009
20110130430Materials Having Embedded Insecticides And Additives - The present invention concerns polymeric material containing at least an embedded insecticidally active ingredient and an additive, which are released at room temperature. It similarly concerns materials produced from this polymer, for example in the form of self-supporting film/sheet, threads, wovens, fabrics, textiles, nets, curtains and pellets. The invention further concerns processes for producing such polymeric material and also the use of the self-supporting film/sheet, threads, wovens, fabrics, textiles and nets and curtains produced from the material for protecting humans, animals and plants and buildings, machines and packaging against arthropods, particularly for controlling insects.06-02-2011
20130137734Polymorphs of an Active Pharmaceutical Ingredient - The present invention relates to crystalline form I of Febuxostat as well as to pharmaceutical compositions camprising crystalline form I as an active pharmaceutical ingredient. Furthermore the present invention relates to a further polymorphic form of Febuxostat designated as form II and to a novel solvate of Febuxostat. The present invention also relates to methods of making crystalline form I, form II and the novel solvate of Febuxostat.05-30-2013
20090069393PARENTERAL FORMULATION FOR EPOTHILONE ANALOGS - A process for formulating certain epothilone analogs for parenteral administration is disclosed wherein the analog is dissolved in a mixture of at least 03-12-2009
20100311796 METHOD FOR THE SEPARATION AND PURIFICATION OF EPOTHILONES - The invention discloses a method for the separation and purification of epothilones, especially discloses a method for the separation and purification of epothilones B and A using normal phase silica gel chromatography, which comprises loading the sample after dissolving the sample containing epothilones B and A with C12-09-2010
20110082178METHODS OF TREATING AUTOIMMUNE AND INFLAMMATORY DISEASES AND DISORDERS - Heterocyclic compounds, compositions comprising them, and methods of their use for the treatment, prevention and management of inflammatory and autoimmune diseases and disorders are disclosed. Particular compounds are of formula I:04-07-2011
20090076099DEUTERIUM-ENRICHED IXABEPILONE - The present application describes deuterium-enriched ixabepilone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-19-2009
20100190833PHARMACEUTICAL CONTAINING PPARA AGONIST - Provision of an agent for promoting proliferation of meibomian gland epithelial cells or corneal epithelial cells, and a therapeutic agent for ocular diseases such as meibomian gland dysfunction, dry eye and the like.07-29-2010
20100048649COMBINATIONS COMPRISING BICYCLIC S1P LYASE INHIBITORS - Methods and compositions for treating immunological and inflammatory diseases and disorders are disclosed. Particular methods and compositions comprise the administration of an agent that inhibits S1P lyase activity and at least one additional immunosuppressive and/or anti-inflammatory agent.02-25-2010
201100983262-FLUOROTHIAZOLE DERIVATIVES USEFUL AS IMAGING AGENTS; METHODS OF SYNTHESIS, AND METHODS OF USE04-28-2011
20110251246SMALL MOLECULE INHIBITORS OF MUC1 AND METHODS OF IDENTIFYING THE SAME - The invention provides methods for the identification of small molecules that inhibit MUC1 oligomerization, and the functions flowing therefrom. In addition, small molecules that prevent MUC1 oligomerization are disclosed. Identified molecules will find use in treating a variety of MUC1-related inflammatory conditions, including MUC1-related cancers.10-13-2011
20080269303HETEROCYCLIC DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF - The invention concerns compounds of formula (I):10-30-2008
20110009459EPOTHILONE DERIVATIVES - Epothilone derivatives of Formula (I) and their use as a pharmaceutical.01-13-2011
20110213003SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF - This invention provides compounds of formula (I):09-01-2011
20110178141Thiazoliums and Their Use for Treating Protein Aging Associated Diseases - The present invention relates to a composition of a thiazolium compound of formula I or a solvate thereof, wherein the definitions of groups in the formula I are as those given in the claims:07-21-2011
20090069392COMPOSITION THAT PREVENTS DAMAGE TO TREES BY HARMFUL INSECTS AND A PREVENTION METHOD THEREOF - The present invention relates to a composition comprising a neonicotinoid-based compound having a high degree of insecticidal activity, a surfactant, and an organic solvent, which is capable of demonstrating stable effects and in which the types and amounts of surfactant and organic solvent are adjusted so as to prevent chemical damage in numerous types of trees. In addition, the present invention relates to a method for preventing damage to trees by harmful insects of numerous types of trees by injecting this composition into a tree trunk and allowing the chemical to circulate within the tree body.03-12-2009
20120202858Solid 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 10.08-09-2012
20120202859Macrocyclic Inhibitors of Hepatitis C Virus - Inhibitors of HCV replication of formula (I)08-09-2012
20090170912AGENTS FOR COMBATING PLANT PESTS - The present invention relates to compositions for controlling plant pests containing the compound of formula (I)07-02-2009
20120202857NOVEL SALTS AND POLYMORPHS OF DESAZADESFERRITHIOCIN POLYETHER ANALOGUES AS METAL CHELATION AGENTS - Disclosed herein are new salts and polymorphs of desazadesferrithiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.08-09-2012
20110053993PRODRUGS OF DESAZADESFERROTHIOCIN POLYETHER ANALOGUES AS METAL CHELATION AGENTS - Disclosed herein are new compounds of desazadesferrothiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.03-03-2011
20110263663SYNTHESIS OF EPOTHILONES, INTERMEDIATES THERETO, ANALOGUES AND USES THEREOF - The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype.10-27-2011
201102636621,2-DIAMIDO-ETHYLENE DERIVATIVES AS OREXIN ANTAGONISTS - The invention relates to 1,2-diamido-ethylene derivatives of the formula (I) wherein R10-27-2011
20110118322BIPHENYL CARBOXYLIC ACIDS AND BIOISOSTERES AS GLYCOGEN SYNTHASE ACTIVATORS - Provided herein are compounds of the formula (I):05-19-2011
20100305172Methods for Concomitant Administration of Colchicine and a Second Active Agent - Methods for concomitant administration of colchicine together with one or more second active agents, e.g., ketoconazole and ritonavir, are disclosed. Such methods reduce the dangers commonly associated with such concomitant administration and provide additional benefits. Methods of notifying health care practitioners and patients regarding appropriate dosing for concomitant administration of colchicine together with second active agents are also provided.12-02-2010
20100305170Agents for Combating Plant Pests - The present invention relates to compositions for controlling plant pests, which contain the compound of the formula (I)12-02-2010
20100305171Methods for Concomitant Administration of Colchicine and a Second Active Agent - Methods for concomitant administration of colchicine together with one or more second active agents, e.g., ketoconazole and ritonavir, are disclosed. Such methods reduce the dangers commonly associated with such concomitant administration and provide additional benefits. Methods of notifying health care practitioners and patients regarding appropriate dosing for concomitant administration of colchicine together with second active agents are also provided.12-02-2010
20110124690COMPOSITIONS AND METHODS FOR TREATING CANCER OR A NEUROTROPHIC DISORDER - The present invention relates to compositions comprising an effective amount of a Panaxytriol Compound and a tubulin-binding drug, methods for treating or preventing cancer or a neurotrophic disorder comprising administering to a subject in need thereof an effective amount of a Panaxytriol Compound and a tubulin-binding drug, and methods for making a Panaxytriol Compound.05-26-2011
20100197746SYNTHESIS OF EPOTHILONES, INTERMEDIATES THERETO AND ANALOGUES THEREOF - The present invention provides compounds of formula (I):08-05-2010
20110152328Combination Therapy For Glaucoma - Disclosed herein is method of treating glaucoma or ocular hypertension comprising administering a prostaglandin agonist and a second therapeutically active agent to a mammal in need thereof, wherein said second therapeutically active agent is selected from: β-Blockers, Adrenergic Agonists, non-selective adrenergic agonists, α2-selective adrenergic agonists, Carbonic Anhydrase Inhibitors, Cholinergic Agonists, direct acting cholinergic agonists, chlolinesterase inhibitors, Glutamate Antagonists, Ca06-23-2011
20110178142PHARMACEUTICAL COMPOSITION FOR THERAPEUTIC OR PROPHYLACTIC TREATMENT OF BACTERIAL INFECTIONS AND ASSOCIATED DISEASES - The present invention provides a pharmaceutical composition comprising 3-{5-[4-Oxo-2-thioxo-3-(3-trifluoromethyl-phenyl)-thiazolidin-5-ylidenemethyl]-furan-2-yl}-benzoic acid or a pharmaceutically acceptable salt thereof and pharmaceutically acceptable excipients for therapeutic or prophylactic treatment of bacterial infections and diseases associated thereof.07-21-2011
201002106965-MEMBERED HETEROCYCLIC COMPOUND - Provided is a compound having a superior acid secretion suppressive action, which shows an antiulcer activity and the like.08-19-2010
20090176847Dicyclooctane Derivatives, Preparation Processes and Medical Uses Thereof - The present invention relates to new dicyclooctane derivates represented by general formula (I), preparation processes and pharmaceutical compositions containing them, and to uses for treatment especially for dipeptidyl peptidase inhibitor (DPPIV), in which each substituent group of general formula (I) is as defined in specification.07-09-2009
20100029730THIAZOLYL BIPHENYL AMIDES - The invention relates to novel thiazolylbiphenylamides of the formula (I)02-04-2010
20100022605N-HYDROXYAMIDE DERIVATIVES POSSESSING ANTIBACTERIAL ACTIVITY - Described herein are N-hydroxyamlde antibacterial compounds, methods for making the compounds, pharmaceutical compositions containing the compounds and methods of treating bacterial infections utilizing the compounds and pharmaceutical compositions compound of Formula (I): or a salt, solvate ti hydrate thereof, wherein A is (a) each01-28-2010
20100016385PROCESS AND FORMULATION CONTAINING EPOTHILONES AND ANALOGS THEREOF - A process for formulating certain epothilones and analogs thereof for parenteral administration is provided wherein the pH of the formulation for administration can be controlled to enhance the stability and thus, potency of the epothilone, or analog thereof.01-21-2010
20100016384PESTICIDAL COMPOSITION AND METHOD FOR CONTROLLING A PEST - A pesticidal composition containing 4-methoxymethyl-2,3,5,6-tetrafluorobenzyl 3-(2-cyano-1-propenyl)-2,2-dimethylcyclopropanecarboxylate and 1-(2-chloro-1,3-thiazolyl)methyl-3-methyl-2-nitroguanidine has a high pesticidal activity.01-21-2010
20090054503COMPOSITION - Pharmaceutical compositions and methods for the treatment of neoplastic disease and comprising the combination of a taxane, such as docetaxel, with a CYP3A4 inhibitor, such as ritonavir. Methods of treatment of neoplastic disease incorporating the administration of a taxane and the administration of a CYP3A4 inhibitor, either simultaneously or separately, are also included. Further, kits for carrying out the methods are included. Solid pharmaceutical taxane compositions for oral administration comprising a substantially amorphous taxane, a carrier and a surfactant are also included.02-26-2009
20100240720ALLOSTERIC JNK INHIBITORS - The disclosure provides compounds and compositions, and methods of using these compounds and compositions, for the targeted delivery of chemotherapeutic agents.09-23-2010
20110306646FUNGICIDAL N-(PHENYLCYCLOALKYL)CARBOXAMIDE, N-(BENZYLCYCLOALKYL)CARBOXAMIDE AND THIOCARBOXAMIDE DERIVATIVES - The present invention relates to a N-(Phenylcycloalkyl)carboxamide or N-(Benzylcycloalkyl)carboxamide or its thiocarboxamide derivative of formula (I) wherein A represents a carbo-linked, unsaturated or partially saturated, substituted or non-substituted 5-membered heterocyclyl group, T represents an oxygen or a sulphur atom, B represents a non aromatic carbocycle that can be substituted by one to four C12-15-2011
20100197747Synergistic Insecticidal Mixtures - The invention relates to insecticide mixtures comprising thiodicarb and at least one other known active ingredient from the category of chloronicotinyls, as well as the use of these mixtures to control animal pests.08-05-2010
20090215840METHODS FOR TREATING SCHIZOPHRENIA - Treatment of schizophrenia or humans suffering from conditions associated with high dopamine levels in ventral striatum or caudate nucleus administers the compound (2S)-2-{3-[3-({[(2R,4R)-4-tert-Butoxycarbonyl-2-(2-fluorophenyl)]-3-thiazolidinyl}carbonylmethyl) ureido]phenyl} propionic acid and its physiological acceptable salts.08-27-2009
20120022120ANTIMYCOTIC PHARMACEUTICAL COMPOSITION - In a pharmaceutical composition for external use containing a compound such as luliconazole and/or a salt thereof, comprised are a higher alcohol which is in a liquid state at 1 atm and 25° C. and/or a diester of a dibasic acid, provided that a diester carbonate is excluded, and a polyoxyethylene alkyl ether and/or a polyoxyethylene alkenyl ether. Provided is a preparation using a solvent other than crotamiton, propylene carbonate, and N-methyl-2-pyrroridone as a solvent for solubilization and steric stabilization and having the following properties: 1) when a compound represented by the general formula (1) and/or a salt thereof has a stereoisomer, the amount of the stereoisomer of the compound and/or a salt thereof produced under a preservation condition of 60 degrees C. for 3 weeks is 1% by mass or less with respect to the total mass of the compound and/or a salt thereof at the beginning of preservation; 2) the preparation is in a clear liquid state when preserved at a constant temperature of 20° C. immediately after manufacture; and 3) no crystal is deposited when the preparation is preserved at 5° C. for 2 weeks after manufacture.01-26-2012
20120065236METHODS FOR CONCOMITANT TREATMENT OF THEOPHYLLINE AND FEBUXOSTAT - The present disclosure relates to a method of treating hyperuricemia in a patient that also suffers from a second disease state requiring treatment with theophylline, wherein the patient receives concomitant treatment with a xanthine oxidoreductase inhibitor and theophylline without resulting in theophylline toxicity to the patient and without substantial adjustments to the manufacturer's recommended dosage of theophylline.03-15-2012
20120071523BENZOFURAN-4,5-DIONES AS SELECTIVE PEPTIDE DEFORMYLASE INHIBITORS - The instant invention provides novel benzofuran-4,5-diones and pharmaceutical compositions thereof useful for inhibiting PDF and for treating proliferative and infectious diseases. Compounds may be selective for eukaryotic (e.g., human) PDF or prokaryotic PDF.03-22-2012
20120136032Fungicidal Active Substance Combinations Containing Trifloxystrobin - What are described are novel active compound combinations comprising a known oxime ether derivative (trifloxystrobin) and imidacloprid, which combinations are highly suitable for controlling phytopathogenic fungi and insects.05-31-2012
20120122938Alkoxy Compounds for Disease Treatment - The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.05-17-2012
20100093812DESFERRITHIOCIN POLYETHER ANALOGUES - A relatively non-toxic desazadesferrithiocin analog having the formula (I): wherein: R04-15-2010
20120129895METHODS OF TREATMENT - The invention relates to combinations comprising a vascular disrupting agent (VDA) with IAP antagonists, for simultaneous, concurrent, separate or sequential use, especially for use in the treatment of proliferative diseases.05-24-2012
20120129894Alkoxy Compounds for Disease Treatment - The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.05-24-2012
20120214852Alkoxy Compounds for Disease Treatment - The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.08-23-2012
20100204286METHOD FOR REDUCING GASTROINTESTINAL ADVERSE EFFECTS OF CYTOTOXIC AGENTS - A method for moderating a gastrointestinal adverse effect induced by at least one cytotoxic agent, for example ionizing radiation and/or at least one chemotherapeutic agent, in a subject comprises administering to the subject a therapeutically effective amount of an ACE2 inhibitor or a compound selected from (S,S)-2-[1-carboxy-2-[3-(3,5-dichlorobenzyl)-3H-imidazol-4-yl]-ethylaminol-4-methylpentanoic acid (ORE1001), pharmaceutically acceptable salts thereof and prodrugs thereof. A method for treating a cancerous condition in a subject comprises administering to the subject (a) at least one cytotoxic anticancer agent, for example ionizing radiation and/or at least one chemotherapeutic agent; and (b) an ACE2 inhibitor or a compound selected from ORE1001, pharmaceutically acceptable salts thereof and prodrugs thereof in an amount effective to moderate a gastrointestinal adverse effect induced by the anticancer agent.08-12-2010
20120214854CARBOXY OXAZOLE OR THIAZOLE COMPOUNDS AS DGAT- 1 INHIBITORS USEFUL FOR THE TREATMENT OF OBESITY - Heteroaryl compounds, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or disorders mediated by Diacylglycerol acyltransferase (DGAT) enzyme, particularly DGAT-1 is described.08-23-2012
20100137383NOVEL SALTS AND POLYMORPHS OF DESAZADESFERROTHIOCIN POLYETHER ANALOGUES AS METAL CHELATION AGENTS - Disclosed herein are new salts and polymorphs of desazadesferrithiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.06-03-2010
20100010054THERAPEUTIC AGENT FOR AMYOTROPHIC LATERAL SCLEROSIS - A novel therapeutic agent for amyotrophic lateral sclerosis. A therapeutic agent for amyotrophic lateral sclerosis, including a compound having xanthine dehydrogenase inhibitory action and not acting as a substrate for the purine salvage pathway.01-14-2010
201202206385-Iodotriazole derivatives - The present invention relates to novel 5-iodotriazole derivatives, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators.08-30-2012
20110124691Organic Compounds - Pharmaceutical formulations comprising an epothilone in the form of an infusion concentrate or a lyophilised composition, and methods of administration of an epothilone in suitable form for parenteral administration.05-26-2011
20120264793Pharmaceutical Use of 2',2-Bis-Thiazole Non-Nucleoside Compounds as Hepatitis C Virus Inhibitor - The present invention discloses the pharmaceutical use of a 2′,2-bis-thiazole non-nucleoside compound of formula I as an inhibitor of hepatitis C virus (HCV). The 2′,2-bis-thiazole non-nucleoside compound can inhibit the replication of HCV, and thus has an anti-HCV activity and is useful for treating hepatitis C.10-18-2012
20120322838Epothilone Compounds, Preparation Method and Use Thereof - Epothilone compounds represented by formula (I), their preparation methods and their use for preparing medicines are disclosed. The epothilone compounds are prepared by bioconversion and chemosynthesis or chemical modifications using epothilones or their derivatives as starting materials. Said epothilone compounds can be sued to treat proliferative diseases.12-20-2012
20110046190COMBINATIONS COMPRISING A SELECTIVE CYCLOOXYGENASE-2 INHIBITOR - A combination therapy for treating patients suffering from pre-malignant colon lesions (e.g. polyps) and colon cancer, as well as other malignancies, is disclosed. The patient is treated concurrently with a cycloocygenase-2 inhibitor and at least one compound selected from the group consisting of a microtubule interfering agent, an epithelial growth factor receptor tyrosine protein kinase inhibitor and a vascular endothelial growth factor receptor tyrosine kinase inhibitor.02-24-2011
20110046189HETEROARYL-SUBSTITUTED BICYCLIC SMAC MIMETICS AND THE USES THEREOF - The invention relates to heteroaryl-substituted bicyclic mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.02-24-2011
20120270911NOVEL SALTS AND POLYMORPHS OF DESAZADESFERRITHIOCIN POLYETHER ANALOGUES AS METAL CHELATION AGENTS - Disclosed herein are new salts and polymorphs of desazadesferrithiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.10-25-2012
20120277274EPOTHILONE COMPOUND FORMULATIONS - The present application relates to compositions for parenteral administration of epothilone compounds, such as ixabepilone.11-01-2012
20100204287HETEROCYCLIC AMIDE DERIVATIVES USEFUL AS MICROBIOCIDES - The invention relates to a fungicidally active compound of formula (I):08-12-2010
20100204285TRANS-3-AZA-BICYCLO[3.1.0]HEXANE DERIVATIVES - The invention relates to novel trans-3-aza-bicyclo[3.1.0]hexane derivatives of formula (I), wherein A, B, n and R08-12-2010
20120329842SMALL MOLECULE COMPOUNDS AS BROAD-SPECTRUM INHIBITORS OF METALLO-BETA-LACTAMASES - The present invention concerns methods and/or compositions for treatment and/or prevention of bacterial infection wherein the bacteria has at least one metallo-β-lactamase. The bacteria are provided with an inhibitor of the metallo-β-lactamase, for example in conjunction with an antibiotic that targets the bacteria. The bacteria may be a drug-resistant strain or susceptible to becoming a drug-resistant strain. In specific embodiments, the bacteria is 12-27-2012
20120329841TREATING CANCER WITH DESTHIAZOLYL RITONAVIR - Treatment of cancer includes administering a compound of formula I, for example desritonavir, to a subject. In particular, treatment of breast cancer is described.12-27-2012
20120101138FLUORINATED AMINOTRIAZOLE DERIVATIVES - The invention relates to fluorinated aminotriazole derivatives of formula (I),04-26-2012
20120289556Methods for Treating Conditions Caused by Higher-Than-Normal Dopaminergic Activity In Basal Ganglia - Treatment of humans suffering from conditions caused by higher-than-normal dopaminergic activity in basal ganglia includes administering the compound (2S)-2-{3-[3-({[(2R,4R)-4-tert-Butoxycarbonyl-2-(2-fluorophenyl)]-3-thiazolidinyl}carbonylmethyl)ureido]phenyl}propionic acid and its physiological acceptable salts.11-15-2012
20130012553METHODS FOR STABILIZING JOINT DAMAGE IN SUBJECTS USING XANTHINE OXIDOREDUCTASE INHIBITORS - The present invention relates to methods for preventing the progression of joint damage in a subject having hyper-uricemia and who has gout thereof by administering a therapeutically effective amount of at least one xanthine oxidoreductase inhibiting compound or salt thereof. Moreover, the present invention also relates to methods of preventing joint damage in a subject having hyperuricemia and who has gout by administering a therapeutically effective amount of at least one xanthine oxidoreductase inhibiting compound or salt thereof.01-10-2013
20100130568TOPICAL COMPOSITIONS COMPRISING TELMESTEINE FOR TREATING DERMATOLOGICAL DISORDERS - This invention relates to topical compositions, such as creams and lotions, that comprise or consist essentially of Telmesteine, or a pharmaceutically acceptable salt thereof, as the active ingredient, and methods for their use in treating a variety of dermatological diseases and disorders, including atopic, dermatitis (eczema), allergic contact dermatitis, seborrheic dermatitis, radiation dermatitis, psoriasis, xerosis and atopy.05-27-2010
20110160257NOVEL SALTS AND POLYMORPHS OF DESAZADESFERROTHIOCIN POLYETHER ANALOGUES AS METAL CHELATION AGENTS - Disclosed herein are new salts and polymorphs of desazadesferrithiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.06-30-2011
20110160256INHIBITORS OF AKT ACTIVITY - Invented are novel hetero-pyrrole compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.06-30-2011
20110160255INHIBITORS OF AKT ACTIVITY - Invented are novel hetero-pyrrole compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.06-30-2011
20110160254COMBINATION OF A BIS-THIAZOLIUM SALT OR A PRECURSOR THEREOF AND ARTEMISININ OR A DERIVATIVE THEREOF FOR TREATING ACUTE MALARIA - The present invention relates to a combination of antimalarial active ingredients, namely a bisthiazolium salt or a precursor thereof and artemisinin or derivatives thereof. The invention also relates to a pharmaceutical composition comprising such a combination and use thereof in the treatment and/or prevention of malaria.06-30-2011
20130023570POLYMORPHS OF DARUNAVIR - The present invention provides new pseudopolymorphic forms of darunavir as well as a novel amorphous form of darunavir, pharmaceutical compositions comprising these compounds, methods for their preparation and use thereof in treating retroviral infections, in particular, HIV infection.01-24-2013
20080255213THIAZOLIDINONE AMIDES, THIAZOLIDINE CARBOXYLIC ACID AMIDES, AND SERINE AMIDES, INCLUDING POLYAMINE CONJUGATES THEREOF, AS SELECTIVE ANTI-CANCER AGENTS - Substituted thiazolidinone carboxylic acid amides and substituted thiazolidine carboxylic acid amides having a structure10-16-2008
20080249144Preventive or Therapeutic Agent for Chronic Inflammatory Lung Disease - Not only acute or chronic interstitial pneumonia and plumonary fibrosis but also chronic obstructive plumonary diseases, such as plumonary emphysema and chronic bronchitis, can be effectively prevented or treated by inhalation administration to the lung tissue of 2-{N-[4-(4-chlorobenzenesulfonylamino)butyl]-N-{3-[(4-isopropyl 2-thiazolyl)methoxy]benzyl}}-sulfamoylbenzoic acid or a pharmacologically acceptable salt thereof.10-09-2008
20080227835Heterocyclic Amide Derivatives Useful as Microbiocides - The invention relates to a fungicidally active compound of formula (I): where Het is a 5- or 6-membered heterocyclic ring containing one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, the ring being substituted by the groups R09-18-2008
20130178504CRYSTALLINE FORMS OF FEBUXOSTAT - New forms of Febuxostat have been prepared and characterized. These forms are useful, for example, in the chronic management of hyperuricemia in patients with gout.07-11-2013
20080214630Desferrithiocin polyether analogues - Compounds represented by structural formulas described herein, such as Structural Formula (I):09-04-2008
20130096166CAMALEXIN AS A TREATMENT FOR PROSTATE CANCER - Compositions and methods to treat prostate cancer with the compound camalexin and its structural analogs. Camalexin increases ROS production and decreases the proliferation of prostate cancer cells, especially aggressive prostate cancer cells.04-18-2013
20130123311MODULATORS OF PHARMACOKINETIC PROPERTIES OF THERAPEUTICS - The present application provides for a compound of Formula I,05-16-2013
20130131128ASSOCIATION OF XANTHINE OXIDASE INHIBITORS AND ANGIOTENSIN II RECEPTOR ANTAGONISTS AND USE THEREOF - The present invention relates to an association of active principles, i.e. of a xanthine oxidase inhibitor with one or more angiotensin II receptor antagonists, pharmaceutical compositions comprising said active principles, for use in a therapeutic treatment in humans or animals, and methods for the preparation thereof.05-23-2013
20100280084Cyp1B1 Genotype - The invention relates to pharmacology, pharmacokinetics and toxicology, and more specifically to methods of identifying and predicting inter-patient differences in response to drugs in order to achieve superior efficacy and safety in selected patient populations. It further related to the genetic basis of inter-patient variation in response to therapy, including drug therapy, and to methods for determining and exploiting such differences to improve medical outcomes.11-04-2010
20080200526Composition for the Prevention and Treatment of Allergic Inflammatory Disease - Disclosed herein is a composition for the treatment and prevention of allergic inflammatory diseases comprising N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}-benzamidine, 4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}-benzamidine or pharmaceutically acceptable salts. The composition exhibits excellent medicinal effects on allergic inflammatory diseases, with a great reduction in typical chronic inflammation symptoms, such as an increase of eosinophil level in bronchoalveolar lavage fluid, total leukocyte level and eosinophil level in blood, the hypertrophy or hyperplasia of bronchial epithelium due to an increase in the number of mucus cells, a reduction in alveolar surface area resulting from the hyptertrophy of alveolar walls, and the infiltration of inflammatory cells.08-21-2008
20090312375HETEROCYCLIC COMPOUNDS, COMPOSITIONS COMPRISING THEM AND METHODS OF THEIR USE - Heterocyclic compounds, compositions comprising them, and methods of their use for the treatment, prevention and management of inflammatory and autoimmune diseases and disorders are disclosed. Particular compounds are of formula I:12-17-2009
20100317703METHOD FOR INHIBITING BRASSININ OXIDASE - The present disclosure relates to a method for inhibiting brassinin oxidase comprising treating a pathogen that is producing BO with an effective amount of selected Paldoxin compounds.12-16-2010
20100317702CRYSTALLINE FORM OF FEBUXOSTAT - New forms of Febuxostat have been prepared and characterized. These forms are useful, for example, in the chronic management of hyperuricemia in patients with gout.12-16-2010
20130190368NOVEL POLYMORPHS OF FEBUXOSTAT - The present invention provides a novel 1,4-dioxane solvate form of febuxostat and process for its preparation. The present invention also provides novel crystalline forms of febuxostat, processes for their preparation and pharmaceutical compositions comprising them.07-25-2013
20090149516Synthesis of Epothilones, Intermediates Thereto, Analogues and Uses Thereof - The present invention provides compounds of formula (I):06-11-2009
20130197043USE OF THE FETAL REPROGRAMMING OF A PPAR AGONIST - Disclosed is a novel use of a PPAR δ agonist, and more particularly, a fetal reprogramming effect of a PPAR δ agonist. A PPAR δ agonist adjusts calcium ion during embryo genesis and a early fetal development period to increase slow muscle fiber and to thus improve muscle endurance, thereby improving lipid and glucose metabolism and reprogramming the metabolism of the entire body, thus preventing/inhibiting the occurrence of metabolic diseases, such as obesity and diabetes in an adult body caused by a high-fat diet and a lack of exercise, and improving memory for an adult.08-01-2013
20130210870DESFERRITHIOCIN POLYETHER ANALOGUES - A relatively non-toxic desazadesferrithiocin analog having the formula:08-15-2013
20130210871Clothianidin, Metofluthrin, and Piperonyl Butoxide Mixture for Bed Bug Control - The invention relates to a mixture comprising clothianidin, metofluthrin, and piperonyl butoxide which provides superior insect knockdown and mortality rates, and is especially effective against bed bugs. This mixture of actives may be formulated with adjuvants, such as solvents, anti-caking agents, stabilizers, defoamers, slip agents, humectants, dispersants, wetting agents, thickening agents, emulsifiers, and/or preservatives which increase the activity of the mixture. Mixtures of the present invention have long lasting residual control.08-15-2013

Patent applications in class 1,3-thiazoles (including hydrogenated)

Patent applications in all subclasses 1,3-thiazoles (including hydrogenated)