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4365 results about "Pyrazole" patented technology

Pyrazole is an organic compound with the formula C₃H₃N₂H. It is a heterocycle characterized by a 5-membered ring of three carbon atoms and two adjacent nitrogen atoms. Pyrazole is a weak base, with pKb 11.5 (pKₐ of the conjugated acid 2.49 at 25 °C). Pyrazoles are also a class of compounds that have the ring C₃N₂ with adjacent nitrogen atoms. Notable drugs containing a pyrazole ring are celecoxib (Celebrex) and the anabolic steroid stanozolol.

Substituted pyrrolopyridines and pyrazolopyridines as kinase modulators

Provided herein are substituted pyrrolopyridine heterocycles and substituted pyrazolopyridine heterocycles, pharmaceutical compositions comprising said heterocycles and methods of using said heterocycles in the treatment of disease. The heterocycles disclosed herein function as kinase modulators and have utility in the treatment of diseases such as cancer, allergy, asthma, inflammation, obstructive airway disease, autoimmune diseases, metabolic disease, infection, CNS disease, brain tumor, obesity, asthma, hematological disorder, degenerative neural disease, cardiovascular disease, or disease associated with angiogenesis, neovascularization, or vasculogenesis.
Owner:SGX PHARMA INC

Synergistic Mixtures of Anthranilamide Invertebrate Pest Control Agents

ActiveUS20080027046A1BiocideOrganic chemistryRyanodine receptorPyrazole-5-carboxamide
Disclosed are mixtures and compositions for controlling invertebrate pests relating to combinations comprising (a) 3-bromo-N-[4-chloro-2-methyl-6-[(methylamino)carbonyl]phenyl]-1-(3-chloro-2-pyridinyl)-1H-pyrazole-5-carboxamide, and its N-oxides, and suitable salts thereof and a component (b) wherein the component (b) is at least one compound or agent selected from neonicotinoids, cholinesterase inhibitors, sodium channel modulators, chitin synthesis inhibitors, ecdysone agonists, lipid biosynthesis inhibitors, macrocyclic lactones, GABA-regulated chloride channel blockers, juvenile hormone mimics, ryanodine receptor ligands, octopamine receptor ligands, mitochondrial electron transport inhibitors, nereistoxin analogs, pyridalyl, flonicamid, pymetrozine, dieldrin, metaflumizone, biological agents, and suitable salts of the foregoing. Also disclosed are methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a mixture or composition of the invention.
Owner:FMC CORP

Pyrazolopyrimidines as protein kinase inhibitors

In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of protein and / or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or checkpoint kinases using such compounds or pharmaceutical compositions. The invention also relates to the inhibition of hepatitis C virus (HCV) replication. In particular, embodiments of the invention provide compounds and methods for inhibiting HCV RNA-dependent RNA polymerase enzymatic activity. The invention also provides compositions and methods for the prophylaxis and treatment of HCV infection.
Owner:MERCK SHARP & DOHME LLC

Oligonucleotides including pyrazolo[3,4-D]pyrimidine bases, bound in double stranded nucleic acids

A triplex forming oligonucleotide is complementary pursuant to the G / T or A / G recognition motif to a homopurine, or substantially homopurine target sequence in double stranded nucleic acids, and at least one and preferably all of the guanine bases are replaced by their pyrazolo[3,4-d]pyrimidine analog, namely by 6-amino-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one. The oliginucleotides containing the pyrazolo[3,4-d]pyrimidine analog of guanine exhibit a lesser degree of self-association, and lack the nucleophilic nitrogen atom in the 7 position of guanine. The latter feature results in a diminished extent of self-crosslinking in ODNs which also have a covalently attached cross-linking agent.
Owner:EPOCH PHARMA

Crystalline form of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate

A novel crystalline form of (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide, pharmaceutical compositions containing said crystalline form and the use of said crystalline form in the treatment of pain, cancer, inflammation, neurodegenerative disease or Trypanosoma cruzi infection are disclosed. In some embodiments, the novel crystalline form comprises a stable polymorph of (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate. The present invention is further directed to a process for the preparation of the novel crystalline form.
Owner:ARRAY BIOPHARMA

Pyrazole amide compound containing diphenyl ether, and application and pesticide composition of pyrazole amide compound

Disclosed are a pyrazole amide compound containing diphenyl ether as represented by formula I and / or formula II, application thereof in the prevention and treatment of rice sheath blight and cucumber powdery mildew, and pesticide composition containing the compound. The pyrazole amide compound of the present invention containing diphenyl ether as represented by formula I and / or formula II, and a bactericide containing the pyrazole amide compound as an active ingredient have good prevention and treatment effects on rice sheath blight and cucumber powdery mildew.
Owner:燕化永乐(乐亭)生物科技有限公司 +1

Pyrazolo[1,5-a]pyrimidines useful as inhibitors of protein kinases

The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing the compounds of the invention.
Owner:VERTEX PHARMA INC

Cannabinoid receptor antagonists/inverse agonists useful for treating obesity

The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, and / or cardiometabolic disorders.
Owner:JENRIN DISCOVERY

RAF inhibitor compounds and methods

Pyrazolyl compounds of Formulas Ia and Ib are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using pyrazolyl compounds for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
Owner:GENENTECH INC +1

Novel pyrazolopyrimidines as cyclin dependent kinase inhibitors

In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
Owner:MERCK SHARP & DOHME LLC

Nicotinamide acids, amides, and their mimetics active as inhibitors of PDE4 isozymes

Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: wherein j is 0 or 1, k is 0 or 1, m is 0, 1, or 2; n is 1 or 2; A is selected from the partial Formulas: where q is 1, 2, or 3, W3 is -O-; -N(R9)-; or -OC(=O)-; R7 is selected from -H; -(C1-C6) alkyl, -(C2-C6) alkenyl, or -(C2-C6) alkynyl substituted by 0 to 3 substituents R10; -(CH2)u-(C3-C7) cycloalkyl where u is 0, 1 or 2, substituted by 0 to 3 R10; and phenyl or benzyl substituted by 0 to 3 R14; R8 is tetrazol-5-yl; 1,2,4-triazol-3-yl; 1,2,4-triazol-3-on-5-yl; 1,2,3-triazol-5-yl; imidazol-2-yl; imidazol-4-yl; imidazolidin-2-on-4-yl; 1,3,4-oxadiazolyl; 1,3,4-oxadiazol-2-on-5-yl; 1,2,4-oxadiazol-3-yl; 1,2,4-oxadiazol-5-on-3-yl; 1,2,4-oxadiazol-5-yl; 1,2,4-oxadiazol-3-on-5-yl; 1,2,5-thiadiazolyl; 1,3,4-thiadiazolyl; morpholinyl; parathiazinyl; oxazolyl; isoxazolyl; thiazolyl; isothiazolyl; pyrrolyl; pyrazolyl; succinimidyl; glutarimidyl; pyrrolidonyl; 2-piperidonyl; 2-pyridonyl; 4-pyridonyl; pyridazin-3-onyl; pyridyl; pyrimidinyl; pyrazinyl; pyridazinyl; indolyl; indolinyl; isoindolinyl; benzo[b]furanyl; 2,3-dihydrobenzofuranyl; 1,3-dihydroisobenzofuranyl; 2H-1-benzopyranyl; 2-H-chromenyl; chromanyl; benzothienyl; 1H-indazolyl; benzimidazolyl; benzoxazolyl; benzisoxazolyl; benzothiazolyl; benzotriazolyl; benzotriazinyl; phthalazinyl; 1,8-naphthyridinyl; quinolinyl; isoquinolinyl; quinazolinyl; quinoxalinyl; pyrazolo[3,4-d]pyrimidinyl; pyrimido[4,5-d]pyrimidinyl; imidazo[1,2-a]pyridinyl; pyridopyridinyl; pteridinyl; or 1H-purinyl; or A is selected from phosphorous and sulfur acid groups; W is -O-; -S(=O)t-, where t is 0, 1, or 2; or -N(R3)-; Y is =C(R1a)-, or -[N<custom-character file="US20020111495A1-20020815-P00900.TIF" wi="20" he="20" id="custom-character-00001" / >(O)k] where k is 0 or 1; R4, R5 and R6 are (1) -H; provided that R5 and R6 are not both -H at the same time, -F; -Cl; -(C2-C4) alkynyl; -R16; -OR16; -S(=O)pR16; -C(=O)R16, -C(=O)OR16, -C(=O)OR<highlight><sup
Owner:PFIZER INC

Pyrazole compositions useful as inhibitors of ERK

Described herein are compounds that are useful as protein kinase inhibitors having the formula: where R1, R2, T and Ht are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.
Owner:VERTEX PHARMA INC

Pyrazole compositions useful as inhibitors of erk

Described herein are compounds that are useful as protein kinase inhibitors having the formula:where R1-4, Q, and T are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.
Owner:VERTEX PHARMA INC

3-Pyrrol-pyridopyrazoles and 3-pyrrolyl-indazoles as novel kinase inhibitors

Compounds of Formula I are useful as mediators of protein kinases and have activity as cell proliferation inhibitors:where X, R1–R7 and R9 are as defined herein.
Owner:SUGEN INC

4-phenylpiperidines, their preparation and use

The present invention provides a compound having the structure: (structurally represented) wherein R1, R2, R3, R4, and R5 are each independently H, halogen, CF3 or C1-C4 alkyl; R6 is H, OH, or halogen; B is a substituted or unsubstituted heterobicycle, pyridazine, pyrazole, pyrazine, thiadiazole, or triazole, wherein the heterobicycle is other than chloro substituted indole; and the pyrazole, when substituted, is substituted with other than trifluoromethyl, or a pharmaceutically acceptable salt thereof.
Owner:THE TRUSTEES OF COLUMBIA UNIV IN THE CITY OF NEW YORK

Polishing fluid and polishing method

ActiveUS20050181609A1Increase chanceSuperior in dimensional accuracy and electric characteristicOther chemical processesSemiconductor/solid-state device manufacturingDevice materialSlurry
A polishing slurry including an oxidant, a metal oxide dissolver, a metal inhibitor and water and having a pH from 2 to 5. The metal oxide dissolver contains one or more types selected from one or more acids (A-group) selected from acids of which the dissociation constant (pKa) of a first dissociable acid group is less than 3.7 and from which five acids of lactic acid, phthalic acid, fumaric acid, maleic acid and aminoacetic acid are excluded, ammonium salts of the A-group and esters of the A-group, and one or more types selected from one or more acids (B-group) selected from acids of which the dissociation constant (pKa) of a first dissociable acid group is 3.7 or more and the five acids, ammonium salts of the B-group and esters of the B-group. The metal inhibitor contains one or more types selected from the group consisting of aromatic compounds having a triazole skeleton and one or more types selected from the group consisting of aliphatic compounds having a triazole skeleton and compounds having any one of pyrimidine skeleton, imidazole skeleton, guanidine skeleton, thiazole skeleton and pyrazole skeleton. The polishing slurry having a high metal-polishing rate, reducing etching rate and polishing friction, results in the production, with high productivity, of semiconductor devices reduced in dishing and erosion in metal wiring.
Owner:HITACHI CHEM CO LTD
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