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

Subclass of:

514 - Drug, bio-affecting and body treating compositions

514001000 - DESIGNATED ORGANIC ACTIVE INGREDIENT CONTAINING (DOAI)

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

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

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

Patent class list (only not empty are listed)

Deeper subclasses:

Class / Patent application numberDescriptionNumber of patent applications / Date published
514274000 Chalcogen bonded directly to pyrimidine at 2-position 225
514272000 Nitrogen bonded directly to the 1,3-diazine at 2-position 71
514270000 Barbituric acid or derivative (including thioanalogs) 16
Entries
DocumentTitleDate
20100063076Endothelin receptor antagonists - This invention relates to novel endothelin receptor antagonists, derivatives, acceptable acid addition salts 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.03-11-2010
20120172383FUNGICIDAL COMPOSITIONS BASED ON PYRIDYLMETHYLBENZAMIDE DERIVATIVES AND AT LEAST ONE COMPLEX III INHIBITING COMPOUND - 1) Fungicidal compositions comprising: a) at least one pyridylmethylbenzamide derivative of Formula (I), in which the various radicals are as defined in the description; and b) at least one compound (II) capable of inhibiting the transport of electrons of the respiratory chain of mitochondrial ubiquinol:ferricytochrome-c oxidoreductase or complex III in phytopathogenic fungal organisms. 2) Process for curatively or preventively controlling the phytopathogenic fungi of crops, characterized in that an effective and nonphytotoxic quantity of one of these fungicidal compositions is applied to the aerial parts of plants.07-05-2012
20100160358Pyridylsulfonamidyl-Pyrimidines for the Prevention of Blood Vessel Graft Failure - The present invention relates to the use of a compound of formula (I), wherein R06-24-2010
20130079360RALTEGRAVIR SALTS AND CRYSTALLINE FORMS THEREOF - The present invention includes new salts of Raltegravir and crystalline forms thereof, pharmaceutical compositions containing the salts or crystalline forms, methods of using the salts or crystalline forms or the compositions to treat HIV infection or to prepare medicament for treating HIV infection, and a process for preparing Raltegravir potassium.03-28-2013
20130040975GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO - GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure:02-14-2013
20100016342SOLID FORMS COMPRISING 3-(2,5-DIMETHYL-4-OXO-4H-QUINAZOLIN-3-YL)-PIPERIDINE-2,6-DIONE, COMPOSITIONS COMPRISING THE SAME, AND METHODS OF USING THE SAME - Provided herein are solid forms comprising 3-(2,5-dimethyl-4-oxo-4H-quinazolin-3-yl)-piperidine-2,6-dione. Pharmaceutical compositions comprising the solid forms and methods for treating, preventing and managing various disorders are also disclosed.01-21-2010
20100041682Ternary Pesticidal Mixtures - Ternary pesticidal mixtures comprising, as active components, an anthranilamid compound of the formula (I) wherein the variables are defined according to the description, and two fungicidal compounds II and III selected from the following groups: azoles, strobilurins, carboxamides, heterocylic compounds, carbamates, guanidines, antibiotics, nitrophenyl derivates, sulfur-containing heterocyclyl compounds, organometal compounds and other active compounds according to the description, in a synergistically effective amount, methods for controlling pests, and harmful fungi, methods of protecting plants from attack or infestation by insects, acarids or nematodes, methods for treating, controlling, preventing or protecting an animal against infestation or infection by parasites, compositions containing these mixtures, and methods for their preparation.02-18-2010
20100105709HETEROMONOCYCLIC COMPOUND AND USE THEREOF - A compound represented by the formula (I):04-29-2010
20100331352NOVEL CRYSTALLINE FORMS OF BOSENTAN - The present invention relates to novel crystalline forms of bosentan and processes for their preparation. Further, the invention relates to pharmaceutical compositions comprising said crystalline forms and use of said compositions in the treatment of patients suffering from endothelin receptor mediated disorders, for example, cardiovascular disorders such as hypertension, pulmonary hypertension, ischemia, vasospasm and angina pectoris.12-30-2010
20090005403Alkinyl-Oxypyrimidines Used in the Form of Pesticides - The invention relates to compounds of the formula (I),01-01-2009
20090306109FUNGICIDE ACTIVE SUBSTANCE COMBINATIONS - The novel active compound combinations comprising 2-[2-(1-chlorocyclopropyl)-3-(2-chlorophenyl)-2-hydroxypropyl]-2,4-dihydro-[1,2,4]-triazole-3-thione of the formula12-10-2009
20090306108SUBSTITUTED PYRIMIDINONES - Disclosed are compounds Formula I12-10-2009
20090306110N-(2-ARYLETHYL)BENZYLAMINES AS ANTAGONISTS OF THE 5-HT6 RECEPTOR - The present invention provides compounds of formula (I), which are antagonists of the 5-HT12-10-2009
200901118386-ARYLAMINO-5-CYANO-4-PYRIMIDINONES AS PDE9A INHIBITORS - The invention relates to novel 6-arylamino-5-cyano-4-pyrimidinones of formula (I)04-30-2009
20110015215CRYSTALLINE FORMS OF 4-[6-(6-METHANESULFONYL-2-METHYL-PYRIDIN-3-YLAMINO)-5-METHOXY-PYRIMIDIN-4- -YLOXY]-PIPERIDINE-1-CARBOXYLIC ACID ISOPROPYL ESTER - The present invention is directed to a novel crystalline forms of 4-[6-(6-methanesulfonyl-2-methyl-pyridin-3-ylamino)-5-methoxy-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid isopropyl ester, pharmaceutical compositions containing said crystalline form and the use of said crystalline forms in the treatment of metabolic related disorders. The present invention is further directed to processes for the preparation of the crystalline forms of 4-[6-(6-methanesulfonyl-2-methyl-pyridin-3-ylamino)-5-methoxy-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid isopropyl ester.01-20-2011
20090069352DEUTERIUM-ENRICHED CLAZOSENTAN - The present application describes deuterium-enriched clazosentan, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-12-2009
20130065915NOVEL FORMULATION - The present invention provides a liquid formulation comprising a strobilurin fungicide, such as azoxystrobin, at least one non-ionic surfactant, at least one anionic surfactant and a solvent/carrier.03-14-2013
20110021547Substantially Pure and a Stable Crystalline Form of Bosentan - Described is a highly stable crystalline form of bosentan having a water content in the range of about 3-4% by weight, based on the total weight of the bosentan, (bosentan crystalline form A5), a process for preparation thereof, and pharmaceutical compositions comprising the bosentan crystalline form A01-27-2011
20100041683NOVEL CHAIN-BREAKING ANTIOXIDANTS - Compounds, preferably 5-pyrimidinol and 3-pyridinol derivatives, that act as effective chain breaking antioxidants of both the lipid and water-soluble variety (analogous to the natural Vitamins E and C), many of which are more reactive toward peroxyl radicals than the most potent form of Vitamin E. These compounds may exhibit many chemopreventive effects associated with conditions in which free radical-mediated cellular damage or disruption is implicated and Vitamins E and C are shown to have protective effects. Additionally, these compounds should be excellent oxidation inhibitors as additives to fuels, lubricants, rubber, polymers, chemicals, solvents and foodstuffs.02-18-2010
20080280929Antifungal Wallboards and Building Materials and Methods for the Production Thereof - The present invention relates to, inter alia, methods for the treatment of wallboards and the treated wallboards. In particular, the invention relates to the treatment of wallboards with a fungicidally effective amount of a strobilurin or strobilurin-type fungicide. In a particular embodiment the fungicide is azoxystrobin. The invention also provides for the treatment of wallboards and building materials with combinations of fungicides present in synergistic amounts.11-13-2008
20110294835Muscarinic Agonists as Cognitive Enhancers - A method of treating a mental condition in a subject in need thereof, comprising: administering to a subject in need thereof an effective amount of compound CDD-102A.12-01-2011
20110281897HETEROCYCLIC COMPOUNDS AND THEIR USES - Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity. The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.11-17-2011
20110144140PYRIDINYL-PYRIMIDINE DERIVATIVES USEFUL AS POTASSIUM CHANNEL MODULATING AGENTS - This invention relates to novel pyridinyl-pyrimidine derivatives and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels.06-16-2011
20110281898PHENOXIACETIC ACID DERIVATIVES - The invention relates to substituted phenoxyacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.11-17-2011
20080214587Processes For the Preparation of Azoxystrobin Using Dabco as a Catalyst and Novel Intermediates Used in the Processes - The present invention relates, inter alia, to a process for preparing a compound of formula (I): which comprises either (a) reacting a compound of formula (II): with 2-cyanophenyl, or a salt thereof, in the presence of between 0.1 and 2 mol % of 1,4-diazabicyclo[2.2.2]octane, or (b) reacting a compound of the formula (III): with a compound of the formula (IV): in the presence of between 0.1 and 2 mol % of 1,4-diazabicyclo[2.2.2]octane; where W is the methyl (E)-2-(3-methoxy)acrylate group C(CO09-04-2008
20090023761Heterocyclic compounds and their uses - Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.01-22-2009
20110294836ARYL GPR119 AGONISTS AND USES THEREOF - Aryl GPR119 agonists are provided. These compounds are useful for the treatment of diabetic diseases, including Type II diabetes and other diseases associated with poor glycemic control.12-01-2011
20100249162PROCESS FOR THE INTRODUCTION OF HYDROXYETHOXY SIDE CHAIN IN BOSENTAN - The present invention relates to an improved process for the preparation of bosentan. In particular it relates to a process for preparing bosentan substantially free from the dimer impurity of formula (II) and the 6-hydroxy impurity of formula (III). The invention also relates to a pharmaceutical composition comprising bosentan and its use in the treatment of endothelin-receptor mediated disorders.09-30-2010
20110195984PEST CONTROL COMPOSITION AND PEST CONTROL METHOD - A pest controlling composition comprising, as active ingredients, a pyrimidine compound represented by Formula (1) and an anthranilamide compound represented by Formula (2).08-11-2011
20100081677HETEROARYLAMIDE PYRIMIDONE DERIVATIVES - The present invention discloses a series of pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof:04-01-2010
20100099692HARMFUL ORGANISM CONTROL COMPOSITION - This invention provides a harmful organism control composition having an excellent harmful organism control effect and comprising as an effective ingredient the following 4-(2-butynyloxy)-5-fluoro-6-(3,5-dimethylpiperidino)-pyrimidine (X):04-22-2010
20080207654HETEROMONOCYCLIC COMPOUND AND USE THEREOF - A compound represented by the formula (I):08-28-2008
20090286816MODULATORS OF METABOLISM AND THE TREATMENT OF DISORDERS RELATED THERETO - The present invention relates to 4-[5-Methoxy-6-(2-methyl-6-[1,2,4]triazol-1-yl-pyridin-3-ylamino)-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid isopropyl ester, pharmaceutically acceptable salts, solvates and hydrates thereof that are modulators of glucose metabolism. Accordingly, compounds of the present invention are useful in the treatment of metabolic-related disorders and complications thereof,11-19-2009
20090291974BOSENTAN SALTS - Stable acid addition salts of bosentan useful for the purification of bosentan base; the salts are in solid state and the starting acid has a pKa lower than 3.11-26-2009
20080275070Aryl Ether Compounds and Their Preparation and Use Thereof - The invention relates to aryl ether compounds and its preparation method and use thereof. The aryl ether compounds of the invention having general formula (I):11-06-2008
20080269265Inhibition Of Raf Kinase Using Symmetrical And Unsymmetrical Substituted Diphenyl Ureas - This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.10-30-2008
20120046308NOVEL ALPHA-PHENOXYBENZENEACETIC ACID DERIVATIVE AND PHARMACEUTICAL PREPARATION COMPRISING SAME - An α-phenoxybenzeneacetic acid derivative represented by general formula (I), which has both an angiotensin II receptor antagonistic activity and a PPARγ activation activity and is useful as a prophylactic and/or therapeutic agent for hypertension, metabolic syndrome or the like, a salt of the derivative, or a solvate of the derivative or the salt; and a pharmaceutical composition containing the derivative, the salt or the solvate. [In the formula, Q represents a group represented by formula (II) or (III) [wherein R02-23-2012
20120196882COMPOUNDS THAT TREAT MALARIA AND PREVENT MALARIA TRANSMISSION - The invention provides methods and compounds for the treatment and prevention of malaria infection and transmission in a mammal by administering compounds of the invention to a mammal having or suspected of having a malaria infection. The invention also provides pharmaceutical compositions that can kill or arrest the growth of 08-02-2012
20100004272Modulators of metabolism and the treatment of disorders related thereto - The present invention relates to 4-[6-(6-methanesulfonyl-2-methyl-pyridin-3-ylamino)-5-methyl-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid isopropyl ester, pharmaceutically acceptable salts, solvates and hydrates thereof that are modulators of glucose metabolism. Accordingly, compounds of the present invention are useful in the treatment of metabolic-related disorders and complications thereof, such as, diabetes and obesity.01-07-2010
20090005404Pyridylsulfonamido pyrimidines for treating diabetic nephropathy - The present invention relates to the use of a compound of formula (I) wherein R01-01-2009
20090143416Method of Inducing Tolerance of Plants Against Bacterioses - A method of inducing tolerance of plants against bacterioses which comprises treating the plants, the soil or seeds with an effective amount of a combination of a compound of the formula I06-04-2009
20090197902Use of Pyrimidine Compounds in the Preparation of Parasiticides - The invention relates to the use of compounds of the general formula (I), wherein R08-06-2009
20110224241ISOTHIAZOLE AND PYRAZOLE DERIVATIVES AS FUNGICIDES - The present invention relates to compounds of Formula (I) wherein R09-15-2011
20120196881Treatment Of Pulmonary Hypertension With Carbonic Anhydrase Inhibitors - This disclosure relates generally to methods and pharmaceutical compositions useful in treating pulmonary hypertension. In one embodiment, for example, the disclosure provides a method for treating pulmonary hypertension comprising administering a therapeutically effective dose of a carbonic anhydrase inhibitor to a patient in need of treatment. The disclosure finds utility in the fields of medicine and pharmacology.08-02-2012
20100160359Modulators of Metabolism and the Treatment of Disorders Related Thereto - The present invention relates to 4-[5-methyl-6-(2-methyl-pyridin-3-yloxy)-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid isopropyl ester, pharmaceutically acceptable salts, solvates and hydrates thereof that are modulators of glucose metabolism. Accordingly, compounds of the present invention are useful in the treatment of metabolic-related disorders and complications thereof, such as, diabetes and obesity.06-24-2010
20130123287CONTROL AGENT FOR SOFT ROT AND CONTROL METHOD FOR THE SAME - Providing a novel control agent for soft rot and a novel control method for the same. A compound having no antibacterial activity against 05-16-2013
20120142714BICYCLIC COMPOUND - The present invention provides a compound having an ACC inhibitory action, which is useful as an agent for the prophylaxis or treatment of obesity, diabetes and the like, and having superior efficacy.06-07-2012
20100144768KINASE INHIBITOR COMPOUNDS - Pyrimidinone derivatives have enhanced and unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as inflammatory diseases and certain types of cancer.06-10-2010
20110112122EPIMINOCYCLOALKYL[b] INDOLE DERIVATIVES AS SEROTONIN SUB-TYPE 6 (5-HT6) MODULATORS AND USES THEREOF - The present invention relates to epiminocycloalkyl[b]indole derivatives as serotonin sub-type 6 (5-HT05-12-2011
20110112121Pharmaceutical Compositions and Solid Forms - The present invention relates to pharmaceutical compositions of 6-(6-hydroxymethyl-pyrimidin-4-yloxy)-naphthalene-1-carboxylic acid (3-trifluoromethyl-phenyl)-amide, to the use of 6-(6-hydroxymethyl-pyrimidin-4-yloxy)-naphthalene-1-carboxylic acid (3-trifluoromethyl-phenyl)-amide and compositions of 6-(6-hydroxymethyl-pyrimidin-4-yloxy)-naphthalene-1-carboxylic acid (3-trifluoromethyl-phenyl)-amide in therapeutic applications, especially indications with a dysregulation/overexpression of VEFG, (neo)-vascularisation and VEGF driven angiogenesis and to methods for manufacturing such compositions, the invention further relates to specific forms of 6-(6-hydroxymethyl-pyrimidin-4-yloxy)-naphthalene-1-carboxylic acid (3-trifluoromethyl-phenyl)-amide and to the manufacturing and use of such forms. The present invention also relates to a new process to produce 6-(6-hydroxymethyl-pyrimidin-4-yloxy)-naphthalene-1-carboxylic acid (3-trifluoromethyl-phenyl)-amide.05-12-2011
20120142715POLYMORPH OF [4,6-BIS(DIMETHYLAMINO)-2-(4-BENZYL)PYRIMIDIN-5-YL] - Provided is a crystalline form of the ethylenediamine salt of [4,6-bis(dimethylamino)-2-(4-{[4-(trifluoromethyl)benzoyl]amino}benzyl)pyrimidin-5-yl]acetic acid, processes for its preparation, pharmaceutical compositions comprising it, and methods of its use for treating, preventing, or ameliorating one or more symptoms of a CRTH2-mediated disorder or disease.06-07-2012
20090069351DEUTERIUM-ENRICHED BOSENTAN - The present application describes deuterium-enriched bosentan, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-12-2009
20110112120HETEROMONOCYCLIC COMPOUND AND USE THEREOF - A compound represented by the formula (I):05-12-2011
20110009437CARBOXAMIDE-HETEROARYL DERIVATIVES FOR THE TREATMENT OF DIABETES - Novel heterocyclic compounds of the formula I01-13-2011
20110039871PROCESS FOR PREPARING BOSENTAN - The present invention relates to a novel intermediate useful in the preparation of bosentan and to processes for the preparation of said intermediate and bosentan. The invention further relates to compositions comprising bosentan prepared according to the processes of the invention and their use in the treatment of endothelin-receptor mediated disorders.02-17-2011
20110118290Novel Amides and Thioamides as Pesticides - The present application relates to novel amides and thioamides, to processes for preparation thereof and to use thereof for controlling animal pests, in particular arthropods and especially insects.05-19-2011
20110082160SYNERGISTIC FUNGICIDAL MIXTURES FOR FUNGAL CONTROL IN CEREALS - A fungicidal composition containing a fungicidally effective amount of a compound of Formula I-V and at least one fungicide selected from the group consisting of epoxiconazole, prothioconazole, azoxystrobin, pyraclostrobin, penthiopyrad, isopyrazam, bixafen, boscalid, prochloraz, and chlorothalonil provides synergistic control of selected fungi.04-07-2011
20100216825FUNGICIDAL COMPOSITIONS - A composition for control of diseases on useful plants or on propagation material thereof caused by phytopathogens, comprising (A) a compound of formula (I) or a tautomer of such a compound; and component (B) and component (C) are pesticides as described in claim 08-26-2010
20110152299SUBSTITUTED BENZAMIDE ANALOGS AS MGLUR5 NEGATIVE ALLOSTERIC MODULATORS AND METHODS OF MAKING AND USING THE SAME - Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention06-23-2011
20110077258TREATMENT OF MALARIA - The invention contemplates compositions for the treatment of malaria comprising an anti-malaria drug and an adjuvant which promotes vasodilation and methods of using same.03-31-2011
20110071175Indoles and Their Therapeutic Use - Compound of formula (I) are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions. Wherein X is —SO03-24-2011
20100261742NOVEL POLYMORPHIC FORMS - Novel polymorphic forms of bosentan and processes for their preparation are disclosed. Further, pharmaceutical compositions comprising said polymorphic forms and the use of said compositions in the treatment of patients suffering from endothelin receptor mediated disorders, for example, cardiovascular disorders such as hypertension, pulmonary hypertension, ischemia, vasospasm and angina pectoris are disclosed.10-14-2010
20110178109PEST CONTROL COMPOSITION AND PEST CONTROL METHOD - A pest controlling composition comprising, as active ingredients, a pyrimidine compound represented by Formula (1):07-21-2011
20100087461ARYLAMIDE PYRIMIDONE COMPOUNDS - The present invention discloses a series of pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof:04-08-2010
20090137616METHOD FOR THE CONTROL OF PHYTOPATHOGENIC FUNGI - The present invention provides a method of controlling 05-28-2009
20080221139Novel Compounds - The invention provides compounds of formula (I):09-11-2008
20090118314TUMOR SUPPRESSOR - A compound having a sructure of propanedioic acid represented by the following formula (05-07-2009
20090082375SOLID FORMS COMPRISING 3-(2,5-DIMETHYL-4-OXO-4H-QUINAZOLIN-3-YL)-PIPERIDINE-2,6-DIONE, COMPOSITIONS COMPRISING THE SAME, AND METHODS OF USING THE SAME - Provided herein are solid forms comprising 3-(2,5-dimethyl-4-oxo-4H-quinazolin-3-yl)-piperidine-2,6-dione. Pharmaceutical compositions comprising the solid forms and methods for treating, preventing and managing various disorders are also disclosed.03-26-2009
20110178108Group of amino substituted benzoyl derivatives and their preparation and their use - A group of amino substituted benzoyl derivatives, their preparation and their use. The screening and research on an antiviral drug with hA3G/Vif as a target point proves that the 3-amino benzoyl derivatives not only have the combined activity for the hA3G/Vif, but also have a function of inhibiting replication of viruses. The present invention provides the possible breakthrough progress for the problem of HIV drug resistance, thereby providing a novel clinical antiviral drug which has higher efficiency.07-21-2011
20110028501SUBSTITUTED CYCLOPROPYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT - Substituted cyclopropyl compounds of formula (I) are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.02-03-2011
20100286176FLOWERS - The present invention relates to methods for reducing the incidence of 11-11-2010
20100298361Alkylthio Pyrimidines As CRTH2 Antagonists - Provided herein are alkylthio substituted pyrimidine compounds having CRTH2 (G-protein-coupled chemoattractant receptor, expressed on Th2 cells) antagonistic activity, useful for the treatment or prophylaxis of diseases associated with CRTH2 activity, including the treatment of allergic diseases, eosinophil-related diseases and basophil-related diseases.11-25-2010
20100298362PROCESS FOR THE PREPARATION OF 4-[6-(6-METHANESULFONYL-2-METHYL-PYRIDIN-3-YLAMINO)-5-METHOXY-PYRIMIDIN-4- -YLOXY]-PIPERIDINE-1-CARBOXYLIC ACID ISOPROPYL ESTER - The present invention is directed to a process for the preparation of 4-[6-(6-methanesulfonyl-2-methyl-pyridin-3-ylamino)-5-methoxy-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid isopropyl ester, useful as glucose dependent insulinotropic receptor agonist, for the treatment of metabolic-related disorders and complications thereof, such as, diabetes and obesity.11-25-2010
20100179177HETEROCYCLIC COMPOUNDS AND THEIR USES - Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.07-15-2010
20110028500PLANT PATHOGEN INHIBITOR COMBINATIONS AND METHODS OF USE - Combinations, compositions and methods of use for modulating plant pathogen infection using plant extracts containing anthraquinone derivatives which induce resistance to plant phytopathogens and an antimicrobial agent, a biological control agent and/or a surfactant having fungicidal activity02-03-2011
20110306623NOVEL COMPOUNDS COMPRISING A 3-(5-ALKOXYPYRIMIDIN-2-YL) PYRIMIDIN-4(3H)-ONE STRUCTURE AND DRUGS THAT COMPRISE SAME - Provided are novel compounds that have both angiotensin II receptor-antagonist effects and PPAR-activating effects that are useful as agents for preventing and/or treating hypertension, heart disease, angina, cerebral vascular accident, cerebrovascular disorder, ischemic peripheral circulatory disorder, kidney disease, atherosclerosis, inflammatory disease, type 2 diabetes mellitus, diabetic complication, insulin resistance syndrome, Syndrome X, metabolic syndrome, and hyperinsulinemia. Disclosed are 3-(5-alkoxypyrimidin-2-yl)pyrimidin-4(3H)-one derivatives represented by the General formula (I): [wherein R represents a C12-15-2011
20100197708INDOLE COMPOUNDS - Indole derivatives that are useful for treating pain, inflammation and other conditions are described. Certain of the compounds are benzyl derivatives and others are benzoyl derivatives. The compounds are substituted at least at the 3 position of the indole.08-05-2010
20080269264Crystalline Forms of 3-[5-Chloro-4-[(2,4-Difluorobenzyl) Oxy]-6-Oxopyrimidin-1(6H)-Yl]-N-(2-Hydroxyethyl)-4-Methylbenzamide - Crystalline forms of the p38 kinase inhibitor 3-[5-chloro-4-[(2,4-difluorobenzyl)oxy]-6-oxopyrimidin-1(6H)-yl]-N-(2-hydroxyethyl)-4-methylbenzamide is provided. Also provided are combinations and pharmaceutical compositions comprising the crystalline forms, and methods for the prophylaxis and/or treatment of a p38 kinase-mediated condition comprising administering to a subject a therapeutically effective amount of the crystalline forms.10-30-2008
20100173920POLYMORPHS OF 3-(E)-2--3-METHOXYACRYLATE - The present invention relates to novel crystalline polymorphic and amorphous forms of the compound (E)-2-{2-[6-(2-cyanophenoxy)pyrimidin-4-yloxy]phenyl}-3-methoxy-acrylate(azoxystrobin). Infrared Raman spectra, X-ray powder diffraction pattern and differential scanning calorimetry thermogram of two polymorphs “A” and “B” are provided. Further, the present invention also provides methods for preparing the novel polymorphic forms “A” and “B”, as well as processes for producing mixtures of the polymorphs, and a process for preparing amorphous azoxystrobin. Yet further, the present invention provides anti-fungal compositions comprising the novel crystalline polymorphs “A” and “B” or amorphous azoxystrobin, which are useful for controlling and combating fungi grown on agricultural and horticultural crops and up-land, and methods of using the same as pesticidal agents for combating fungi on agricultural and horticultural crops.07-08-2010
20090298859METHOD FOR TREATING PLANTS - The present invention relates to the use of a fungicide selected from the group consisting of (i) a strobilurin or strobilurin-type fungicide or (ii) a triazole or an insecticide selected from the group consisting of (i) an avermectin, (ii) an organophosphate, (iii) a benzoylurea or (iv) a neonicotinoid in the production of a crop plant having raised levels of anti-oxidants.12-03-2009
20120059020PROPHYLACTIC OR THERAPEUTIC AGENT FOR PULMONARY FIBROSIS - Disclosed is a compound which has an inhibitory activity on plasminogen activator inhibitor-1 (PAI-1) and has a propanedioic acid structure represented by formula (1) [wherein R03-08-2012
20100029698Pesticidal Mixtures - The present invention relates to mixtures comprising, as active components, 1) an insecticidal compound I selected from fipronil and ethiprole; and 2) a fungicidal compound IIA selected from azoles, strobilurins, carboxamides, heterocylic compounds, carbamates, and other active compounds, and optionally 3) one or two fungicidal compounds IIB selected from List B which is defined as List A plus triticonazole, orysastrobin, in synergistically effective amounts, all as further defined in the description.02-04-2010
20120157482COMPOUNDS AND METHODS - Disclosed are compounds having the formula:06-21-2012
20130012529HETEROBICYCLIC CARBOXAMIDES AS INHIBITORS FOR KINASES - The invention relates to novel organic compounds of formula (I)01-10-2013
201201360164, 5, 6-TRISUBSTITUTED PYRIMIDINE DERIVATIVES AS FACTOR IXA INHIBITORS - The present invention relates to novel heterocyclic compounds of Formulae (I): (Chemical formula should be inserted here as it appears on abstract in paper form) Formula (I) as disclosed herein, or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder.05-31-2012
20120136015PROCESS FOR PREPARATION OF ENDOTHELIAL RECEPTOR ANTAGONIST (BOSENTAN) - The present invention relates to processes for the preparation of an endothelial receptor antagonist. The present invention particularly relates to synthesis of 4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-(2-pyrimidinyl)-4-pyrimidinyl]benzene sulfonamide (bosentan).05-31-2012
20120172382PYRIDONE AMIDES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES - Compounds useful in the treatment of mammalian cancers and especially human cancers according to Formula I are disclosed.07-05-2012
20100292259PYRIMIDYL INDOLINE COMPOUND - It is intended to provide a pyrimidyl indoline compound which structurally differs from compounds used as active ingredients in conventional oral hypoglycemic agents and has excellent hypoglycemic effect. The present invention provides a compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof:11-18-2010
20100292258SUBSTITUTED AROMATIC HETEROCYCLIC COMPOUNDS AS FUNGICIDES - The present invention relates to compounds of formula (I) wherein R11-18-2010
201202206095-HYDROXYPYRIMIDINE-4-CARBOXAMIDE DERIVATIVE - The present invention provides a compound which enhances the production of erythropoietin. The present invention provides a compound represented by formula (1):08-30-2012
201202258951-HETERODIENE DERIVATIVE AND PEST CONTROL AGENT - The present invention provides a pest control agent having a novel skeleton, which can be synthesized industrially, and also has excellent biological activity and residual effects. Specifically, the present invention provides a 1-heterodiene derivative represented by Formula (1) or a salt thereof, and a pest control agent including, as an active ingredient, a 1-heterodiene derivative or a salt thereof.09-06-2012
20120264772ANTIHYPERTENSIVE PHARMACEUTICAL COMPOSITION - Provided is an antihypertensive pharmaceutical composition containing Fimasartan, a pharmaceutically acceptable salt thereof, a solvate thereof or a hydrate thereof as an angiotensin II receptor blocker, and Amlodipine, an isomer thereof, a pharmaceutically acceptable salt thereof, a solvate thereof or a hydrate thereof as a calcium channel blocker.10-18-2012
20120232101Novel Compounds - The invention provides compounds of formula (I):09-13-2012
20130018064Amino Heteroaryl Compounds as Beta-Secretase Modulators and Methods of UseAANM Paras; Nick A.AACI San FranciscoAAST CAAACO USAAGP Paras; Nick A. San Francisco CA USAANM Cheng; YuanAACI Newbury ParkAAST CAAACO USAAGP Cheng; Yuan Newbury Park CA USAANM Powers; TimothyAACI MalibuAAST CAAACO USAAGP Powers; Timothy Malibu CA USAANM Brown; JamesAACI MoorparkAAST CAAACO USAAGP Brown; James Moorpark CA USAANM Hitchcock; Stephen A.AACI JupiterAAST FLAACO USAAGP Hitchcock; Stephen A. Jupiter FL USAANM Judd; TedAACI Simi ValleyAAST CAAACO USAAGP Judd; Ted Simi Valley CA USAANM Lopez; PatriciaAACI West HillsAAST CAAACO USAAGP Lopez; Patricia West Hills CA USAANM Xue; QiufenAACI Newbury ParkAAST CAAACO USAAGP Xue; Qiufen Newbury Park CA USAANM Yang; BryantAACI Simi ValleyAAST CAAACO USAAGP Yang; Bryant Simi Valley CA US - The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I, wherein ring A, B01-17-2013
20120322819COMPOUND CONTAINING A NOVEL 4-ALKOXYPYRIMIDINE STRUCTURE AND MEDICINE CONTAINING SAME - Disclosed is novel compound and medicinal formulation containing same, possessing both angiotensin II receptor blocking and PPARγ activation effect, of use as a medicine for prevention and/or treatment of hypertension, heart disease, angina pectoris, cerebrovascular disorder, cerebral circulatory disturbances, post-ischemic peripheral circulatory damage, renal disease, arteriosclerosis, inflammatory disorder, type 2 diabetes, diabetic complications, insulin resistance syndrome, syndrome X, metabolic syndrome and hyperinsulinaemia. Further disclosed is the general formula I (where one or both of R12-20-2012
20120270888PHARMACEUTICAL COMPOSITIONS OF RALTEGRAVIR, METHODS OF PREPARATION AND USE THEREOF - Disclosed are pharmaceutical compositions comprising HIV integrase strand transfer inhibitor. More particularly, oral pharmaceutical compositions of raltegravir or its pharmaceutically acceptable salts and process for preparing and use of the same are disclosed.10-25-2012
20110224242STYRLYQUINOLINES, THEIR PROCESS OF PREPARATION AND THEIR THERAPEUTIC USES - The present disclosure concerns new substituted styrylquinolines, the process of their preparation and their therapeutic uses as integrase inhibitors and/or for the treatment and/or prevention of HIV.09-15-2011
20110245281DISPERSIBLE BOSENTAN TABLET - The invention relates to dispersible tablets comprising the compound 4-tert-butyl-N-[6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-2-(pyrimidin-2-yl)-pyrimidin-4-yl]-benzenesulfonamide.10-06-2011
20100173919PHARMACEUTICAL COMPOSITION USING ALISKIREN AND AVOSENTAN - The present invention relates to a pharmaceutical composition and method of achieving a therapeutic effect including, but not limited to, the treatment of hypertension, kidney or heart disease in an animal, preferably a mammal including a human subject, using (i) SPP100/aliskiren or a pharmaceutically acceptable salt thereof in combination with (ii) SPP301/avosentan or a pharmaceutically acceptable salt thereof and (iii) a pharmaceutically acceptable carrier.07-08-2010
20130023547DISPERSIBLE TABLET - The invention relates to dispersible tablets comprising the compound 4-tert-butyl-N-[6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-2-(pyrimidin-2-yl)-pyrimidin-4-yl]-benzenesulfonamide.01-24-2013
20080255166Dithiocarbamate derivatives and their use as antibacterial agents - The invention relates to the use of dithiocarbamate derivatives for the therapeutic or prophylactic treatment of infectious diseases in mammals (humans and animals) caused by bacteria, especially diseases like tuberculosis (TB) and lepra caused by mycobacteria and infectious diseases caused by staphylococci. The invention further relates to novel dithiocarbamate derivatives of the formula (I), wherein X is a bivalent residue selected from the group consisting of formulae having excellent antibacterial activities, and to pharmaceutical preparations containing the same.10-16-2008
20100087460ARYLAMIDE PYRIMIDONE DERIVATIVES - The present invention discloses a series of pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof:04-08-2010
20080234301Alpha-4 Integrin Mediated Cell Adhesion Inhibitors for the Treatment or Prevention of Inflammatory Diseases - The present invention relates to novel compounds of formula (I), processes for their preparation, compositions comprising them and their use in the treatment or prevention of diseases capable of being modulated by the inhibition of cell adhesion.09-25-2008
20130172375PHARMACEUTICAL COMPOSITION - The present invention relates to a pharmaceutical composition comprising a solid dispersion of a drug. In the composition, the drug is in substantially amorphous form.07-04-2013
20110263624BICYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF - The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a GPCR in a patient.10-27-2011
20110263623PROCESS FOR PREPARATION OF BOSENTAN - The present invention provides improved processes for preparing Bosentan. The present invention provides novel intermediates like 4,6-dihydroxy-5-(2-methoxy phenoxy)[2,2′]bipyrimidine of formula (II) and N-(6-Chloro-5-(2-ethoxyphenoxy)[2,2′-bipyrimidinyl]-4-t-butyl benzenesulfonamide cesium salt and process for preparation thereof. The invention also disclosed novel polymorphic form of the intermediates.10-27-2011
20110263622TETRAHYDROPHENANTHRIDINONES AND TETRAHYDROCYCLOPENTAQUINOLINONES AS PARP AND TUBULIN POLYMERIZATION INHIBITORS - The present invention provides compounds of formula (I), their use as inhibitors of tubulin polymerization and their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I)10-27-2011
20130184299CCR2 ANTAGONISTS AND USES THEREOF - The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.07-18-2013
20110269784USE OF TETRAHYDROPYRIMIDINES - Tetrahydropyrimidines of the formula11-03-2011
20130096147Raltegravir Salts and Crystalline Forms Thereof - The present invention includes new salts of Raltegravir and crystalline forms thereof, pharmaceutical compositions containing the salts or crystalline forms, methods of using the salts or crystalline forms or the compositions to treat HIV infection or to prepare medicament for treating HIV infection, and a process for preparing Raltegravir potassium.04-18-2013
20130143905NOVEL ANTAGONISTS FOR CCR2 AND USES THEREOF - The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (I) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.06-06-2013
20130143906SUBSTITUTED PYRIMIDINONE-PHENYL-PYRIMIDINYL COMPOUNDS - The present disclosure provides pyrimidinone-phenyl-pyrimidinyl compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and inflammatory disease, having the structure of Formula (I):06-06-2013
20130158054POLYMORPHS OF 3-(E)-2--3-METHOXYACRYLATE - The present invention relates to novel crystalline polymorphic and amorphous forms of the compound (E)-2-{2-[6-(2-cyanophenoxy)pyrimidin-4-yloxy]phenyl}-3-methoxy-acrylate (azoxystrobin). Infrared Raman spectra, X-ray powder diffraction pattern and differential scanning calorimetry thermogram of two polymorphs “A” and “B” are provided. Further, the present invention also provides methods for preparing the novel polymorphic forms “A” and “B”, as well as processes for producing mixtures of the polymorphs, and a process for preparing amorphous azoxystrobin. Yet further, the present invention provides anti-fungal compositions comprising the novel crystalline polymorphs “A” and “B” or amorphous azoxystrobin, which are useful for controlling and combating fungi grown on agricultural and horticultural crops and up-land, and methods of using the same as pesticidal agents for combating fungi on agricultural and horticultural crops.06-20-2013
20130158053CRYSTALLINE FORMS OF 3-[5-CHLORO-4-[(2,4-DIFLUOROBENZYL) OXY]-6-OXOPYRIMIDIN-1(6H)-YL]-N-(2-HYDROXYETHYL)-4-METHYLBENZAMIDE - Crystalline forms of the p38 kinase inhibitor 3-[5-chloro-4-[(2,4-difluorobenzyl)oxy]-6-oxopyrimidin-1(6H)-yl]-N-(2-hydroxyethyl)-4-methylbenzamide is provided. Also provided are combinations and pharmaceutical compositions comprising the crystalline forms, and methods for the prophylaxis and/or treatment of a p38 kinase-mediated condition comprising administering to a subject a therapeutically effective amount of the crystalline forms.06-20-2013
20110275653HETEROCYCLIC COMPOUNDS AND THEIR USES - Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.11-10-2011
20130150388INHIBITORS OF NEDD8-ACTIVATING ENZYME - Disclosed are chemical entities which are inhibitors of Nedd8-activating enzyme (NAE), namely, the compound {(1S,2S,4R)-4-[(6-{[(1R,2S)-5-chloro-2-methoxy-2,3-dihydro-1H-inden-1-yl]amino}pyrimidin-4-yl)oxy]-2-hydroxycyclopentyl}methyl sulfamate and pharmaceutically acceptable salts thereof; solid state forms thereof; and prodrugs thereof. Also disclosed are methods of using the chemical entities to treat disorders such as cancer.06-13-2013
20120028996NOVEL OXIME DERIVATIVES - The present invention relates to novel oxime derivatives of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation.02-02-2012
20080242687SUBSTITUTED PYRIMIDINES - Disclosed herein are substituted pyrimidine-based endothelin modulators of Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.10-02-2008
20120095031CYCLOPROPANE COMPOUND - A cyclopropane compound represented by the following formula (A) or a pharmaceutically acceptable salt thereof has orexin receptor antagonism, and therefore has a potencial of usefulness for the treatment of sleep disorder for which orexin receptor antagonism is effective, for example, insomnia:04-19-2012

Patent applications in class Pyrimidines with chalcogen bonded directly to a ring carbon of said pyrimidine moiety

Patent applications in all subclasses Pyrimidines with chalcogen bonded directly to a ring carbon of said pyrimidine moiety