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Polycyclo ring system having the additional 1,3-diazine ring as one of the cyclos

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.)

514252100 - 1,4 diazines

514252120 - Piperazines (i.e., fully hydrogenated 1,4-diazines)

514252130 - Additional hetero ring attached directly or indirectly to the piperazine ring by nonionic bonding

514252140 - The additional hetero ring is a 1,3 diazine ring

Patent class list (only not empty are listed)

Deeper subclasses:

Class / Patent application numberDescriptionNumber of patent applications / Date published
514252170 The polycyclo ring system is quinazoline (including hydrogenated) 54
Entries
DocumentTitleDate
20090247538Ortho-Condensed Pyridine and Pyrimidine Derivatives (e.g., Purines) as Protein Kinases Inhibitors - The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR10-01-2009
20100069395Pyrazolo[1,5-a]pyrimidine-3-carboxylic acid compounds as protein kinase inhibitors - Compounds of formula03-18-2010
20130079350Substitute 2-amino-3-(Sulfony)pyrazol[1,5-a]pyramidines - serotonin 5-ht6 receptor antagonists, method for us thereof - The present invention relates to novel substituted 2-amino-3-(arylsulfonyl)pyrazolo[1,5-a]pyrimidines of general formula 1, to serotonin 5-HT03-28-2013
20130035342Compound Suitable for the Treatment of Synucleopathies - The present invention relates to a compound of formula (I): Wherein R02-07-2013
20100069397SEXUAL DYSFUNCTION COMPOUNDS - The present invention provides for a sexual dysfunction compound comprising a rapid-onset pharmaceutical composition that further comprises cocoa powder. The invention also provides for a process for manufacturing the composition, and use of the composition in sexual dysfunction therapy.03-18-2010
20090306093METHOD FOR TREATING PATIENT HAVING BENIGN PROSTATE HYPERPLASIA - A method for treating a patient having lower urinary tract symptoms is provided. The method comprises a step of administering to the patient a therapeutically effective amount of one selected from a group consisting of a treating compound of 7-[2-[4-(2-Chlorobenzene)piperazinyl]ethyl]-1,3-dimethyl xanthine, a salt of the treating compound, a solvate of the treating compound and a combination thereof, wherein the compound has an effect on treating the benign prostate hyperplasia via a mechanism selected from a group consisting of an activation of PKG pathway, a blockage of an adrenoceptor, an opening of a potassium channel and an inhibition of PDE activity.12-10-2009
20130072498TRANSDERMAL DELIVERY OF BENEFICIAL SUBSTANCES EFFECTED BY A HOSTILE BIOPHYSICAL ENVIRONMENT - The present invention generally relates to the transdermal delivery of substances and, in some embodiments, to the transdermal delivery of beneficial substances by a hostile biophysical environment. In one aspect, various methods for the transdermal delivery of beneficial substances are disclosed. By creating a hostile biophysical environment, beneficial substances may be delivered, according to certain embodiments, through the stratum corneum of the skin into the body. Beneficial substances include, but are not limited to, pharmaceutical agents, drugs, vitamins, co-factors, peptides, dietary supplements, and others. The beneficial effects disclosed include, for instance, relief of pain and inflammation, prevention and healing of ulcers of the skin, relief of headache, improved sexual function and enjoyment, growth of hair on the scalp, improving muscle size and/or function, removing body fat and/or cellulite, treating cancer, treating viral infections and others.03-21-2013
20130059859PREDICTIVE BIOMARKERS FOR PI3K/AKT KINASE PATHWAY INHIBITOR EFFICACY - A method of predicting the sensitivity of tumor cell growth to inhibition by a PI3K/AKT kinase pathway inhibitor, comprising: determining the localization profile of FOXO3a in a tumor cell, wherein a cytoplasmic localization profile of FOXO3a correlates with sensitivity to inhibition by a PI3K/AKT kinase inhibitor and a nuclear localization profile of FOXO3a correlates with resistance to inhibition by a PI3K/AKT kinase inhibitor.03-07-2013
20110015204PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS - The present invention provides compounds of Formula (I), including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.01-20-2011
20130065908DIHYDROFURO PYRIMIDINES AS AKT PROTEIN KINASE INHIBITORS - The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula:03-14-2013
20090325976PROSTACYCLIN DERIVATIVES - This invention relates to novel prostacyclin 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 prostacyclin, and in particular those diseases and conditions beneficially treated by dilators of systemic and pulmonary arterial vascular beds or by platelet aggregation inhibitors.12-31-2009
20080293734PHARMACEUTICAL COMPOSITIONS - Disclosed are useful pharmaceutical compositions.11-27-2008
20080293733AXL KINASE INHIBITORS - Axl kinase inhibitory compounds are disclosed, as well as compositions and methods of using the same in the treatment of cancer and other conditions mediated by and/or associated with Axl kinase.11-27-2008
20130165448AILDENAFIL CITRATE CRYSTAL FORM O, PREPARATION METHOD AND USE THEREOF - The invention provides a 1-[3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d] pyridine-5-group)-4-ethoxy-benzenesulfonyl]-cis-3,5-dimethylpiperazine citrate or an Aildenafil citrate crystal form O and a preparation method thereof. And the invention also provides pharmaceutical compositions containing the Aildenafil citrate crystal form O and the use thereof in preparing drugs for treating Male Erectile Dysfunction (ED). The above crystal form O can be prepared through the steps of: dissolving a raw material, namely, the Aildenafil citrate in a mixture of distilled water and tetrahydrofuran, stirring, heating, filtering, stirring a filtrate, cooling, insulating heat, crystallizing, filtering and the like. The crystal form O can be adopted to prepare drugs with pharmaceutically acceptable excipients, so as to treat the male sexual dysfunction diseases.06-27-2013
20120225888Inhibitors of Human Immunodeficiency Virus Replication - The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.09-06-2012
20110190312Combinations Comprising Epothilones and Protein Tyrosine Kinase Inhibitors and Pharmaceutical Uses Thereof - The invention relates to a combination which comprises: 08-04-2011
20100056538Pro-drugs of A2B Adenosine Receptor Antagonists - Disclosed are prodrugs of A03-04-2010
20110281884FUSED DERIVATIVES AS PI3KDELTA INHIBITORS - The present invention provides fused derivatives that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.11-17-2011
20100267735METHODS AND COMPOSITIONS TO ENHANCE THE EFFICACY OF PHOSPHODIESTERASE INHIBITORS - Methods for treatment of sexual dysfunction in men and women using combination of phosphodiesterase (PDE) type 5 inhibitors and 1-deprenyl or propargylamine compounds are described. Methods of reducing the dosage and preventing the side effects of PDE type5 inhibitors are also described. The methods comprise administering a therapeutically effect amount of 1-deprenyl or propargylamine compounds (also called monoamine oxidase [MAO] inhibitors) in combination with PDE inhibitors. Stimulation of nitric oxide production and vasodilation by 1-deprenyl and propargylamine compounds augments the actions of PDE inhibitors or other drugs and methods used in the treatment of sexual dysfunction. The composition described here enhances the actions of PDE inhibitors primarily by increasing the generation of cyclic GMP by stimulating the nitric oxide pathway and secondarily by providing several additional benefits such as enhanced dopamine activity. Methods of enhancing the efficacy of various PDE inhibitors in the treatment of a number of disorders other than sexual dysfunction are also disclosed.10-21-2010
20110039859SUSCEPTIBILITY TO BONE DAMAGE - In one aspect, the present invention provides methods for determining susceptibility to bone damage in a subject. In some embodiments, the methods comprise screening for polymorphisms in the MTHFR and collagen Iα1 genes that are associated with susceptibility to bone damage. In some embodiments, the methods comprise screening for elevated levels of homocysteine in a subject, wherein elevated levels of homocysteine are associated with an increased risk of bone damage. The methods of the invention may be used in predicting the response of a patient to treatment. Also provided are methods for prevention or reducing the risk of bone damage in a subject.02-17-2011
20100292245(EN) SUBSTITUTED 2-AMINO-3-SULFONYL-PYRAZOLO[1,5-A] PYRIMIDINES/ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS, METHODS FOR THE PRODUCTION AND THE USE THEREOF - The present invention relates to novel substituted 2-amino-3-(arylsulfonyl)pyrazolo[1,5-a]pyrimidines of general formula 1, to serotonin 5-HT11-18-2010
20100035891Pharmaceutically Active Compounds - Compounds of the formula (I):02-11-2010
20110201618KMUPS INHIBITING PROLIFERATION AND OBLITERATION OF PULMONARY ARTERY - An obstructive pulmonary disease inhibiting pharmaceutical composition is provided. The obstructive pulmonary disease inhibiting pharmaceutical composition includes:08-18-2011
20100267736METHODS AND COMPOSITIONS TO ENHANCE THE EFFICACY OF PHOSPHODIESTERASE INHIBITORS - Methods for treatment of sexual dysfunction in men and women using combination of phosphodiesterase (PDE) type 5 inhibitors and 1-deprenyl or propargylamine compounds are described. Methods of reducing the dosage and preventing the side effects of PDE type5 inhibitors are also described. The methods comprise administering a therapeutically effect amount of 1-deprenyl or propargylamine compounds (also called monoamine oxidase [MAO] inhibitors) in combination with PDE inhibitors. Stimulation of nitric oxide production and vasodilation by 1-deprenyl and propargylamine compounds augments the actions of PDE inhibitors or other drugs and methods used in the treatment of sexual dysfunction. The composition described here enhances the actions of PDE inhibitors primarily by increasing the generation of cyclic GMP by stimulating the nitric oxide pathway and secondarily by providing several additional benefits such as enhanced dopamine activity. Methods of enhancing the efficacy of various PDE inhibitors in the treatment of a number of disorders other than sexual dysfunction are also disclosed.10-21-2010
20090143400PURINE DERIVATIVES HAVING IMMUNO-MODULATING PROPERTIES - The present invention provides compounds of formula06-04-2009
201000874439-SUBSTITUTED-8-OXO-ADENINE COMPOUNDS AS TOLL-LIKE RECEPTOR (TLR7) MODULATORS - The present invention provides compounds of formula04-08-2010
20120108604PROCESSES FOR PREPARING AMINE SALTS OF SILDENAFIL-ANALOGUES AND USE THEREOF - A series of amine salts including a structure of formula (I) and formula (III) have provided. In formula I or formula (III), R05-03-2012
20100093748SUBSTITUTED PIPERIDINES HAVING PROTEIN KINASE INHIBITING ACTIVITY - The invention provides PKA and PKB kinase-inhibiting compounds of the formula (I):04-15-2010
20130190320HETEROCYCLIC COMPOUNDS AND USES AS ANTICANCER AGENTS - The present disclosure provides pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment of tumors and related diseases related to the dysregulation of kinase (such as EGFR (including HER), Alk, PDGFR, but not limited to) pathways.07-25-2013
200902755933 Substituted N-(aryl- or heteroaryl)-pyrazolo[1,5-a]pyrimidines as Kinase Inhibitors - The invention relates to 3-substituted N-(aryl- or heteroaryl)-pyrazolo[1,5-a]pyrimidine compounds, their use as kinase inhibitors, new pharmaceutical formulations comprising said compounds, said compounds for use in the diagnostic or therapeutic treatment of warm-blooded animals, especially humans, their use in the treatment of diseases or for the manufacture of pharmaceutical formulations useful in the treatment of diseases that respond to modulation of kinase, especially tie-2 kinase, activity, methods of treatment comprising administration of said compounds to a warm-blooded animal, especially a human, and processes for the manufacture of said compounds.11-05-2009
20090286802High Dose Folic Acid Compositions for Vascular Dysfunction - The present invention relates to treatments for hypertension and more particularly, to the use of high dose folic acid in treating dysfunctional conditions associated with vascular function. High dose folic acid can increase vasodilator-stimulated myocardial blood flow and acutely lower arterial pressure independently of homocysteine lowering.11-19-2009
20100216807HETEROCYCLIC COMPOUNDS AS SEROTONERGIC AND / OR DOPAMINERGIC AGENTS AND USES THEREOF - Novel heterocyclic compounds of formula I:08-26-2010
200802750543-(Substituted Amino)-Pyrazolo[3, 4-D]Pyrimidines as Ephb and Vegfr2 Kinase Inhibitors - The invention relates to novel pyrazolo[3,4-d]pyrimidines of the formula11-06-2008
20080261991Reducing Side Effects of Tramadol - The invention provides methods of reducing the side effects of tramadol. Accordingly, in one embodiment, the invention provides a method of reducing the incidence of newly-discovered side effects related to sexual function in human males taking a tramadol material. The method comprises administering a phosphodiesterase inhibitor to a male taking the tramadol material. The invention also provides pharmaceutical compositions. In one embodiment, the composition comprises a tramadol material and a phosphodiesterase inhibitor. The invention further provides kits. In one embodiment, the kit comprises a tramadol material and a phosphodiesterase inhibitor.10-23-2008
20080287456Oral Therapeutic Compound Delivery System - The present invention relates generally to therapeutic formulations. More particularly, this present invention provides an oral delivery system for a therapeutic compound that is a base, a salt of a base or an amphoteric compound or a salt of a amphoteric compound with pharmacological, physiological or biochemical activity or a proactive form thereof. The present invention even more particularly provides a swallow formulation comprising a therapeutic compound that is a base, a salt of a base, an amphoteric compound or a salt of an amphoteric compound which facilitates the rapid delivery of the therapeutic compound to the circulatory system.11-20-2008
20080269238Thiazolopyrimidine Derivative - The present invention provides a compound represented by the following Formula:10-30-2008
20080269240Novel Adenine Compound - An adenine compound useful as a medicine represented by the following formula (1):10-30-2008
20120295916ORODISPERSIBLE TABLET CONTAINING COMPACTED SILDENAFIL BASE - The invention relates to a process for the preparation of a pharmaceutical intermediate, comprising the steps of (i) mixing (a-i) sildenafil base, (b-i) wicking agent, (c-i) disintegrant, (d-i) optionally glidant; (ii) compacting the mixture; and (iii) milling the compacted material; and to an intermediate obtainable by that process. In addition, the invention relates to a process for the preparation of an orally dispersible tablet (hereinafter also referred to as an “orodispersible tablet”) comprising the intermediate of the invention, and to orodispersible tablets obtainable by that process.11-22-2012
20120295915AZABENZIMIDAZOLES AS FATTY ACID SYNTHASE INHIBITORS - Disclosed are compounds having Formula (I),11-22-2012
20110207740PHARMACEUTICAL COMPOSITIONS - Disclosed are useful pharmaceutical compositions.08-25-2011
20080242672ADENOSINE A2A RECEPTOR ANTAGONISTS - The present invention provides compounds of the formula10-02-2008
20080242673ADENOSINE A2A RECEPTOR ANTAGONISTS - The present invention provides compounds of the formula10-02-2008
20080269239Pyrimidine Compounds as Histamine Modulators - The present invention relates to novel pyrimidine compounds, for the modulation of the histamine H4 receptor and the treatment or prevention of conditions mediated by the histamine H4 receptor. The invention also relates to the preparation of such compounds.10-30-2008
20110269773DIHYDROFURO PYRIMIDINES AS AKT PROTEIN KINASE INHIBITORS - The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula (I): Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.11-03-2011
20090143399Protein Kinase Inhibitors - Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure:06-04-2009
20110224220SUBSTITUTED TRICYCLIC DERIVATIVES - Compounds of formula (I):09-15-2011
20130217697ORAL PHARMACEUTICAL FILM FORMULATION FOR BITTER TASTING DRUGS - The invention relates to a pharmaceutical film formulation comprising one or more bitter-tasting drug(s) or pharmaceutically acceptable salts thereof, one or more film formers, a bitterness masker containing one or more inorganic and/or organic salt(s) and at least two monocyclic monoterpenes, and one or more sweetening agent(s).08-22-2013
20090062298DEUTERIUM-ENRICHED SILDENAFIL - The present application describes deuterium-enriched sildenafil, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-05-2009
20090137604TRI-HETEROCYCLIC COMPOUNDS AND A PHARMACEUTICAL COMPRISING THEM AS AN ACTIVE INGREDIENT - Tri-heterocyclic compound of formula (I)05-28-2009
20120077819USE OF KINASE INHIBITOR FOR THE TREATMENT OF THYMOMA - The invention provides a low molecular weight ATP-competitive CDK inhibitor and TRKA inhibitor of formula (I) for use in the treatment of thymoma and thymic carcinoma. The compound can be administered together with one or more cytotoxic or cytostatic agents.03-29-2012
20090247539Novel Pharmaceuticals - This invention relates to compounds of formula (I)10-01-2009
20090197892ANHYDROUS COMPOSITIONS USEFUL FOR ATTAINING ENHANCED SEXUAL WELLNESS - The invention relates to an anhydrous composition comprising a vasodilator and an acceptable carrier wherein the vasodilator is present in an amount effective to increase the blood flow when the composition is applied to human tissue. The compositions according to the invention are non-flushing.08-06-2009
20100016330Novel Derivatives - The present invention relates to novel piperazine derivatives; to processes for their preparation; to pharmaceutical compositions containing the derivatives; and to the use of the derivatives in therapy to treat diseases for which blocking the Ca01-21-2010
20100261729METHODS FOR THE TREATMENT OF ERECTILE DYSFUNCTION USING FISPEMIFENE - A method of treatment of erectile dysfunction (ED) comprises the step of administering fispemifene to a subject in need thereof in an amount effective to raise the subject's testosterone level. Fispemifene may be used in combination with a PDE-5 inhibitor in individuals who have failed to respond sufficiently to conventional ED treatment. Methods are also disclosed of treating ED by administering clomifene, enclomifene, ospemifene, toremifene and mixtures thereof in combination with a PDE-5 inhibitor.10-14-2010
20100234393USE OF A VASOPEPTIDASE INHIBITOR FOR THE TREATMENT OF PULMONARY ARTERIAL HYPERTENSION - The present invention relates to the use of a vasopeptidase inhibitor for the preparation of a medicament for use in the treatment and/or prevention of PAH.09-16-2010
20130217698SALT(S) OF 7-CYCLOPENTYL-2-(5-PIPERAZIN-1-YL-PYRIDIN-2-YLAMINO)-7H-PYRROLO- [2,3-D]PYRIMIDINE-6-CARBOXYLIC ACID DIMETHYLAMIDE AND PROCESSES OF MAKING THEREOF - This invention relates to (1) process of making 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and salts thereof; (2) novel salt(s) of 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide; (3) pharmaceutical compositions comprising the same; and (4) methods of treatment using the same.08-22-2013
20090111827ARYLINDENOPYRIMIDINES COMPOUND AND USE AS AN ADENOSINE A2a RECEPTOR ANTAGONISTS - This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses. Disorders treated and/or prevented include Parkinson's Disease.04-30-2009
20090069336PYRIMIDOTHIOPHENE COMPOUNDS - Compounds of formula (I) are inhibitors of HSP90, and useful in the treatment of, for example, cancers:03-12-2009
20130143896ISOXAZOLO-QUINAZOLINES AS MODULATORS OF PROTEIN KINASE ACTIVITY - The present invention relates to substituted isoxazolo-quinazolines which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular human MPS1 and PERK. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.06-06-2013
20100324062COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, Aurora-A, Axl, BMX, CHK2, c-RAF, cSRC, Fes, FGFR3, Flt3, IKKα, IR, JNK2α2, Lck, Met, MKK6, MST2, p70S6K, PDGFRα, PKA, PKD2, ROCK-II, Ros, Rsk1, SAPK2α, SAPK2β, SAPK3, SAPK4, Syk, Tie2 and TrkB kinases.12-23-2010
20110118276METHODS OF TREATING ATHEROSCLEROSIS - The present invention relates to adenosine A05-19-2011
20090215791NEW THERAPEUTIC USE OF 4-(2-FLUOROPHENYL)-6-METHYL-2-(1-PIPERAZINYL)THIENO[2,3-D]PYRIMIDINE - 4-(2-Fluorophenyl)-6-methyl-2-(1-piperazinyl)thieno[2,3-D]pyrimidine or a salt thereof is useful for the treatment of pain.08-27-2009
201000693964-AMINO-3-(IMIDAZOLYL)-PYRAZOLO[3,4-D]PYRIMIDINES - Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are 4-amino-3-imidazoyl-pyrazolo[3,4-d]pyrimidine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.03-18-2010
20110034476GENETIC POLYMORPHISMS AND INFERTILITY - Methods of screening for a cause of low sperm motility and/or for mitochondrial impairment in subjects are provided, comprising determining a genotype of the subject with respect to at least one choline metabolism gene and comparing the genotype of the subject with at least one reference choline metabolism genotype associated with low sperm motility and/or impaired mitochondrial function, wherein a similarity between the subject and reference genotypes indicates a cause of low sperm motility and/or impaired mitochondrial function in the subject. In another aspect, methods for treating subjects having low sperm motility and/or impaired mitochondrial function are provided, comprising administering to the subject an effective amount of a choline metabolism supplement composition to at least partially ameliorate the low sperm motility and/or impaired mitochondrial function.02-10-2011
20120202826Tetrahydropyrrolopyrimidinediones And Their Use In Therapy - The subject invention provides compounds of formula (I):08-09-2012
20120202825Soluble Salts of Thieno [2,3-d] Pyrimidine Derivatives - The present invention is directed to novel salts of thieno[2,3-d]pyrimidine derivatives, including 4-(2-fluorophenyl)-6-methyl-2-(piperazin-1-yl)thieno[2,3-d]pyrimidine salts. The present invention is also directed to compositions including such polymorphs and methods for using such salts, e.g., in the treatment of gastrointestinal and/or genitourinary disorders.08-09-2012
20090137603HETEROCYCLIC AMIDE COMPOUND AND USE THEREOF - The present invention provides a novel amide compound represented by the following formula, which has a matrix metalloproteinase inhibitory activity and is useful as a pharmaceutical agent.05-28-2009
20110190311USE OF CDK INHIBITOR FOR THE TREATMENT OF GLIOMA - The invention provides a low molecular weight ATP-competitive CDK inhibitor able to cross the blood brain barrier for use in the treatment of malignant glioma and, in particular, of glioblastoma. The compound can be administered together with one or more agents selected from the group consisting of cytotoxic or cytostatic agents and ionizing radiation.08-04-2011
20100022552KMUP-1 CAPABLE OF TREATING HYPERTENSION - A method for treating a spontaneous hypertension or a cardiomyocyte hypertrophy is provided. The method comprises a step of administering to a mammal a therapeutically effective amount of a compound of 7-[2-[4-(2-chlorobenzene)piperazinyl]ethyl]-1,3-dimethyl xanthine.01-28-2010
20100016329XANTHINE-BASED CYCLIC GMP-ENHANCING RHO-KINASE INHIBITOR INHIBITS PHYSIOLOGICAL ACTIVITIES OF LUNG EPITHELIAL CELL LINE - The present invention provides a pharmaceutical composition including a compound of 7-[2-[4-(2-chlorophenyl)piperazinyl]-ethyl]-1,3-dimethylxanthine (KMUP-1), wherein the compound is a Rho-kinase inhibitor, and the pharmaceutical composition inhibits a physiological activity of a lung epithelial cell.01-21-2010
20080312249KMUP-1 CAPABLE OF TREATING HYPERTENSION - A pharmaceutical composition for treating the hypertension is provided. The pharmaceutical composition comprises a chemical compound of 7-[2-[4-(2-Chlorobenzene)piperazinyl]ethyl]-1,3-dimethyl xanthine and one of a pharmaceutical acceptable salt thereof and a solvate thereof, wherein the chemical compound treats the hypertension by cGMP-dependent inhibition on Rho kinase.12-18-2008
20120232090ARYLPIPERAZINE-CONTAINING PURINE DERIVATIVES AND USES THEREOF - A novel arylpiperazine-containing purine derivatives and a pharmaceutical composition comprising the same as an active ingredient, which are useful for preventing or treating depressive disorders, are provided.09-13-2012
20120157468PLK INHIBITOR SALTS - The present invention relates to novel crystalline, water-soluble salts of a plk inhibitor. Such crystal salts are for example L-tartrate, succinate, phosphate, mesylate, maleate, L-malate, hydrochloride, fumarate (half mole of counterion), fumarate, citrate (half mole of counterion), benzenesulfonate and L-aspartate (half mole of counterion). New crystal forms of the base as well as solvates and hydrates of such new salt forms, a process for their preparation, their utility in therapy and to the pharmaceutical compositions containing them are also claimed and described in the present application.06-21-2012
20120157467COMPOSITION AND USE FOR PHOSPHODIESTERASE INHIBITORS - Compositions and methods for enhancing the aesthetic appearance of the lip or lips of a human achieved by applying to the surface of the lip a composition containing a phosphodiesterase inhibitor, preferably a pyrazolopyrimidinone such as sildenafil or its citrate salt.06-21-2012
20120157466HETEROCYCLIC COMPOUNDS WITH CXCR3 ANTAGONIST ACTIVITY - The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1 or Formula 5:06-21-2012
20120115878SALT(S) OF 7-CYCLOPENTYL-2-(5-PIPERAZIN-1-YL-PYRIDIN-2-YLAMINO)-7H-PYRROLO- [2,3-D]PYRIMIDINE-6-CARBOXYLIC ACID DIMETHYLAMIDE AND PROCESSES OF MAKING THEREOF - This invention relates to (1) process of making 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and salts thereof; (2) novel salt(s) of 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide; (3) pharmaceutical compositions comprising the same; and (4) methods of treatment using the same.05-10-2012
20120071490P70 S6 KINASE INHIBITORS - The present invention provides p70 S6 kinase inhibitors of the formula:03-22-2012
20120071489DERIVATIVES OF N-ACYL-N'-PHENYLPIPERAZINE USEFUL (INTER ALIA) FOR THE PROPHYLAXIS OR TREATMENT OF DIABETES - The present invention relates to a compound represented by the formula wherein each symbol is as defined in the present specification, which has a superior RBP4-lowering action and is useful as a pharmaceutical composition for the prophylaxis or treatment of a disease or condition mediated by an increase in RBP4.03-22-2012
20120071488MELTING TABLET CONTAINING A SILDENAFIL SALT - The invention relates to an orodispersible tablet comprising the components pharmaceutically acceptable sildenafil salt (a), polymeric adsorbent (b), in particular cation exchanger resin, sweetener (c), and flavoring (d) and, preferably, mucilage (e) and glidant (f). The invention furthermore relates to a process for the preparation of orodispersible tablets comprising a pharmaceutically acceptable sildenafil salt and to the use of a combination of cation exchanger resin and mucilage for masking the flavor of medicaments for treating erectile dysfunction03-22-2012
20110065716HYDROXYLATED PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS - The present invention provides compounds, including pharmaceutically acceptable salts thereof, comprising the Formula (I): Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases, such as cancer.03-17-2011
20110105519Pharmaceutical Compositions for the Treatment of Sexual Disorders II - The invention relates to new pharmaceutical compositions for the treatment of sexual disorders and methods for the preparation thereof. In a preferred embodiment, the instant invention is directed to pharmaceutical combinations comprising flibanserin as one active ingredient in combination with at least one additional active ingredient for the treatment of sexual disorders and methods for the preparation thereof.05-05-2011
20120172370PREPARATION OF CRYSTALLINE FORMS OF DIHYDROPYRAZOLOPYRIMIDINONE - The instant invention relates to crystalline forms of MK-1775, an inhibitor of Weel kinase. Specifically, the instant invention relates to hemihydrates of MK-1775.07-05-2012
20110183992THERAPEUTIC AGENT FOR MIGRAINE - Provided are therapeutic and/or preventive agents for migraine which comprise, as an active ingredient, a compound having a selective adenosine A07-28-2011
20120129868POLY (ADP-RIBOSE) POLYMERASE (PARP) INHIBITORS - Compounds of the following formula are provided for use with PARP:05-24-2012
20100280041RHOKINASE-DEPENDENT INHIBITION ACTIVITY ON PULMONARY ARTERY ENDOTHELIUM DYSFUNCTION, MEDIAL WALL THICKNESS AND VASCULAR OBSTRUCTION OF PULMODIL AND PULMODIL-1 - A pharmaceutical composition for treating one of a cardiovascular disease and a pulmonary artery disease, comprising one of a first compound having a Formula I and a second compound having a Formula II.11-04-2010
20120232089METHOD OF TREATING AN ANXIETY DISORDER - Anxiety disorders, such as panic disorder, agoraphobia, obsessive-compulsive disorder, social phobia, post-traumatic stress disorder, generalized anxiety disorder, specific phobia, or the like, are treated by administering an effective amount of at least one adenosine A09-13-2012
20100010005 Renal Function with Quercetin-Containing Compositions - This invention relates to a method of improving renal function by administering to a subject in need thereof an effective amount of a composition containing quercetin, vitamin C, vitamin B3, and folic acid.01-14-2010
20100292244HYDROXYLATED PYRIMIDYL CYCLOPENTANE AS AKT PROTEIN KINASE INHIBITOR - The present invention provides a compound and pharmaceutically acceptable salts thereof, comprising the Formula I. Also provided are methods of using the compound of this invention as an AKT protein kinase inhibitor and for the treatment of hyperproliferative diseases such as cancer.11-18-2010
20120258970Compositions and Methods for the Treatment of Drug-Induced Hand-Foot Syndrome - The present invention provides methods of treating, ameliorating or preventing hand-foot syndrome in a subject in need thereof comprising administering to the subject a therapeutically effective amount of a phosphodiesterase inhibitor.10-11-2012
20110124655KMUP-1 CAPABLE OF TREATING HYPERTENSION - A cardiomyocyte hypertrophy inhibiting pharmaceutical composition is provided. The composition comprises an effective amount of a compound of 7-[2-[4-(2-chlorobenzene)piperazinyl]ethyl]-1,3-dimethylxanthine; and a pharmaceutically acceptable carrier.05-26-2011
20110124654DIAZACARBAZOLES AND METHODS OF USE - The invention relates to 1,5-diazacarbazole compounds of Formula (I), (I-a), (I-b), (I-c), (I-d), (I-e), (I-f), (I-g) and (I-h) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.05-26-2011
20090005395SILDENAFIL N-OXIDE AS PRODRUG - Embodiments of the present invention relate to a compound of formula (101-01-2009
20120329808DIHYDROTHIENO PYRIMIDINES AS AKT PROTEIN KINASE INHIBITORS - The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula:12-27-2012
201100461492-AMINO-3-SULPHONYL-TETRAHYDRO-PYRAZOLO[1,5-A]PYRIDO-PYRIMIDINE ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS, METHODS FOR THE PRODUCTION AND USE THEREOF - The invention relates to serotonin 5-HT02-24-2011
20110237599HETEROCYCLIC INHIBITORS OF HISTAMINE RECEPTORS FOR THE TREATMENT OF DISEASE - The present invention relates to compounds and methods which may be useful as inhibitors of H09-29-2011
20120329809PURINE COMPOUNDS USED AS CB2 AGONISTS - A compound of the formula (I) and pharmaceutical compositions for the treatment of pain.12-27-2012
20090099195Therapeutic Compounds 570 - Compounds of formula I or pharmaceutically acceptable salts thereof:04-16-2009
20100168122XANTHINE DERIVATIVES AS SELECTIVE HM74A AGONISTS - The present invention relates to compounds of formula (I) which are xanthine derivatives, processes for manufacture of said derivatives, pharmaceutical formulations containing these compounds and the use of the compounds in therapy, for example, in the treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial07-01-2010
20130012518BICYCLIC COMPOUNDS AND THEIR USES AS DUAL C-SRC / JAK INHIBITORS - The present invention relates to substituted aromatic bicyclic compounds containing pyrimidine and pyridine rings of formula (I) having the structure as well as pharmaceutically acceptable salts thereof. The compounds of the present invention are useful as tyrosine kinase inhibitors, preferably SRC family kinases (SFKs) inhibitors, in particular as multi SFK/JAK. kinases inhibitors and even preferably as dual c-SRC/JAK kinases inhibitors, thereby inhibiting the STAT3 activation and therefore abnormal growth of particular cell types. Notably, the compounds of the present invention are useful for the treatment or inhibition of certain diseases that are the result of deregulation of STAT3.01-10-2013
20130018057Quinoline and Quinoxaline Derivatives as Kinase InhibitorsAANM Burli; RolandAACI Saffron Walden EssexAACO GBAAGP Burli; Roland Saffron Walden Essex GBAANM Haughan; Alan FindlayAACI Saffron Walden EssexAACO GBAAGP Haughan; Alan Findlay Saffron Walden Essex GBAANM Matteucci; M zioAACI Saffron Walden EssexAACO GBAAGP Matteucci; M zio Saffron Walden Essex GBAANM Owens; Andrew PateAACI Saffron Walden EssexAACO GBAAGP Owens; Andrew Pate Saffron Walden Essex GBAANM Raphy; GillesAACI Saffron Walden EssexAACO GBAAGP Raphy; Gilles Saffron Walden Essex GBAANM Sharpe; AndrewAACI Saffron Walden EssexAACO GBAAGP Sharpe; Andrew Saffron Walden Essex GB - A series of quinoline and quinoxaline derivatives, substituted by a fused bicyclic pyridine or pyrimidine moiety attached via an alkylene chain optionally linked to a heteroatom, being selective inhibitors of P13 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.01-17-2013
20110160222MODULATORS OF GLUCOSE HOMEOSTASIS FOR THE TREATMENT OF DIABETES AND METABOLIC DISORDERS - Aryl 119 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.06-30-2011
20110160221PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS - The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.06-30-2011
20080234284Pyrazolo[1,5-a]Pyrimidin-7-Yl Amine Derivatives as Protein Kinase Inhibitors - The invention relates to pyrazolo[1,5a]pyrimidin-7-yl amine derivatives of formula (I)09-25-2008
20130116265COMPOUND FOR INHIBITING TYPE 5 PHOSPHODIESTERASE AND PREPARATION METHOD THEREOF - The present invention discloses a compound of formula (I) and citrate thereof as type 5 phosphodiesterase inhibitor, a preparation method thereof, and a pharmaceutical composition including the compound of formula (I) and citrate thereof. The experimental results of the present invention prove that the compound of formula (I) and citrate thereof can inhibit activity of type 5 phosphodiesterase, and can be used for treating erectile dysfunction, inhibiting platelet aggregation and treating thrombosis, decreasing pulmonary hypertension and treating cardiovascular diseases, treating asthma and treating diabetes gastroparesis.05-09-2013
20090221600PYRIDO-PYRIDIMIDINE DERIVATIVES USEFUL AS ANTIINFLAMMATORY AGENTS - Provided are novel pyrido-pyrimidine derivatives, having the structure of Formula (I): which can be used as anti-inflammatory agents. Also provided are pharmaceutical compositions comprising one or more pyrido-pyrimidine derivatives, as well as methods of treating autoimmune diseases, inflammation or associated pathologies, including for example, sepsis, rheumatoid arthritis, inflammatory bowel disease, type-1 diabetes, asthma, chronic obstructive pulmonary disorder, organ transplant rejection and psoriasis, comprising administering such compounds or pharmaceutical compositions comprising them.09-03-2009
20090005394Endothelin receptor antagonists - This invention relates to novel endothelin receptor antagonists, derivatives, 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 that are beneficially treated by compounds that block the endothelin signaling pathway that leads to vasoconstriction and in particular those diseases or conditions beneficially treated by endothelin receptor antagonists.01-01-2009
20130143894ORAL SPRAY FORMULATIONS AD METHODS FOR ADMINISTRATION OF SILDENAFIL - The present disclosure is directed to chemically-stable and pharmaceutically-acceptable sildenafil oral spray formulations for the treatment of male erectile dysfunction, wherein the oral spray formulation has a pH of about 1.5 to less than 3.0. The present disclosure is also directed to methods for treating male erectile dysfunction.06-06-2013
20130143895BICYCLIC COMPOUNDS AND THEIR USES AS DUAL C-SRC / JAK INHIBITORS - The present invention relates to substituted aromatic bicyclic compounds containing pyrimidine and pyridine rings of formula (I) having the structure as well as pharmaceutically acceptable salts thereof. The compounds of the present invention are useful as tyrosine kinase inhibitors, preferably SRC family kinases (SFKs) inhibitors, in particular as multi SFK/JAK. kinases inhibitors and even preferably as dual c-SRC/JAK kinases inhibitors, thereby inhibiting the STAT3 activation and therefore abnormal growth of particular cell types. Notably, the compounds of the present invention are useful for the treatment or inhibition of certain diseases that are the result of deregulation of STAT3.06-06-2013
20100280040SYNTHESIS AND PHARMACOKINETIC ACTIVITIES OF PULMODIL AND PULMODIL-1, TWO CHLOROPHENYLPIPERAZINE SALT DERIVATIVES - A compound including a salt derivative of the chlorophenylpiperazine moiety is provided, wherein the chlorophenylpiperazine moiety is derived from the reaction of a xanthine and a piperazine. The salt derivative thereof is non-toxic to the tracheal smooth muscle cells (TSMCs) and can be intravenously-, orally- or sublingually-dosed into the mammals.11-04-2010
20100280039PHARMACEUTICAL COMPOSITIONS COMPRISING CHLOROPHENYL PIPERAZINE DERIVED COMPOUNDS AND USE OF THE COMPOUNDS IN PRODUCING MEDICAMENTS - The invention relates to a pharmaceutical composition for treating serotonergic neurotransmission related disease or condition, including an effective amount of a chlorophenylpiperazine derived compound of Formula (I),11-04-2010
200802004754-Piperazinothieno[2,3-D] Pyrimidine Compounds As Platelet Aggregation Inhibitors - Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: (I) wherein A08-21-2008
20110212972Compositions and Methods for Treating Female Sexual Dysfunction - This invention relates to methods, pharmaceutical compositions and kits useful in treating female sexual dysfunction and the use of an estrogen agonist/antagonist for the manufacture of a medicament for the treatment of female sexual dysfunction. The compositions are comprised of an estrogen agonist/antagonist as a first active ingredient and a cyclic guanosine 3′,5′-monophosphate elevator as a second active component and a pharmaceutically acceptable vehicle, carrier or diluent. The compositions and methods of treatment are effective while substantially reducing the concomitant liability of adverse effects associated with estrogen administration.09-01-2011
20110224221HEMATOPOIETIC PROTECTION AGAINST IONIZING RADIATION USING SELECTIVE CYCLIN-DEPENDENT KINASE 4/6 INHIBITORS - Methods for reducing or preventing the effects of ionizing radiation in healthy cells arc provided. The methods relate to the use of selective cyclin-dependent kinase (CDK) 4/6 inhibitors to induce transient quiescence in CDK4/6 dependent cells, such as hematopoietic stem cells and/or hematopoietic progenitor cells. Radioprotection can be effected in mammals by treatment with selective CDK4/6 inhibitor compounds either before, at the same time as, or after exposure to the ionizing radiation.09-15-2011
20100317671XANTHINE-BASED CYCLIC GMP-ENHANCING RHO-KINASE INHIBITOR INHIBITS PHYSIOLOGICAL ACTIVITIES OF LUNG EPITHELIAL CELL LINE - A pharmaceutical composition for a treatment of an interstitial lung disease is provided. The pharmaceutical composition comprises an effective amount of an active component being one selected from a group consisting of a KMUP compound, a KMUP monoquaternary ammonium salt and a KMUP monoquaternary ammonium complex salt, wherein the KMUP monoquaternary ammonium complex salt is synthesized by the KMUP compound and a carboxylic acid derivative of one selected from a group consisting of a statin, a non-steroid anti-inflammatory (NSAIDs) and an anti-asthmatic drug.12-16-2010
20130184285PYRROLOPYRIMIDINE COMPOUNDS AND THEIR USES - The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.07-18-2013
20130158043PAK INHIBITORS FOR THE TREATMENT OF CANCER - Provided herein are methods of utilizing PAK inhibitors for the treatment of cancer. Further provided herein are compounds and formulations utilized for the treatment of cancer.06-20-2013
20130203767Treatment of Pulmonary Hypertension - This invention relates to the use of certain cyclic guanosine 3′,5′-monophosphate phosphodiesterase type five (cGMP PDE5) inhibitors, including in particular the compound sildenafil, for the treatment of pulmonary hypertension.08-08-2013
20130203765DEUTERATED PYRROLOPYRIMIDINE COMPOUNDS AS INHIBITORS OF CDK4/6 - The invention is directed to novel deuterated pyrrolopyrimidine compounds of formula (I) wherein R08-08-2013
20130203766Pharmaceutical Compositions for the Treatment of Sexual Disorders II - The invention relates to new pharmaceutical compositions for the treatment of sexual disorders and methods for the preparation thereof. In a preferred embodiment, the instant invention is directed to pharmaceutical combinations comprising flibanserin as one active ingredient in combination with at least one additional active ingredient for the treatment of sexual disorders and methods for the preparation thereof.08-08-2013
20130203768N-HETEROARYL COMPOUNDS WITH CYCLIC BRIDGING UNIT FOR THE TREATMENT OF PARASITIC DISEASES - This invention relates to certain N-heteroaryl compounds that are generally useful as medicaments, more specifically as medicaments for animals. The medicament can preferably be used for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to the preparation of the N-heteroaryl compounds. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.08-08-2013
20120088775Pyrazolo-[1,5-a]-Pyrimidones Derivatives and Pharmaceutical Compositions and Uses Thereof - The present invention provides new pyrazolo-[1,5-04-12-2012
20120095013USE OF KMUP-3 FOR MYOCARDIAL INFARCTION - A pharmaceutical composition for improving a cardiac function is provided. The pharmaceutical composition comprises an effective amount of an active component being one of a KMUP-3 compound and a salt thereof.04-19-2012

Patent applications in class Polycyclo ring system having the additional 1,3-diazine ring as one of the cyclos

Patent applications in all subclasses Polycyclo ring system having the additional 1,3-diazine ring as one of the cyclos