Abstract: The present invention provides compounds of formula I wherein X and R1–R7 are as defined herein.

Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.

Abstract: The present invention relates to compounds having the general formula or a pharmaceutically acceptable salt thereof. Also included is a method of prophylaxis or treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic ? cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs.

Abstract: This invention relates to a compound of Formula I, a method for its preparation and its use in the preparation of a compound of Formula II wherein R1, R2, R3, X and n are as defined in the disclosure. This invention also discloses preparation of compounds of Formula III wherein R1, R2, R6, R7, R8 and n are as defined in the disclosure. Also disclosed are certain intermediates of Formula 4 for the preparation of compounds of Formula I wherein X is N and R2, R3 and n are as defined in the disclosure.

Abstract: Novel pyrazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-? signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer, and fibrotic diseases.

Abstract: This invention relates to a compound of the formula: or a pharmaceutically acceptable salt thereof, wherein A and R1 are each an optionally substituted 5 to 6-membered heteroaryl, wherein the heteroaryl is optionally fused to a carbocyclic ring or 5 to 6-heteroaryl; R2 is NH2; R3 and R4 are each hydrogen, halo, (C1-C4)alkyl optionally substituted with halo and the like; and X1 to X4 are each hydrogen, halo, hydroxy, (C1-C4)alkyl optionally substituted with halo and the like. These compounds have COX-2 inhibiting activity and thus useful for treating or preventing inflammation or other COX-2 related diseases.

Abstract: The present invention relates to compounds of the formula wherein R1, R3, R5, R6, and A are defined as in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment of inflammation and other inflammation associated disorders, such as osteoarthritis, rheumatoid arthritis, colon cancer and Alzheimer's disease, in mammals (preferably humans, dogs, cats and livestock).

Abstract: The invention relates method of combating undesired plant growth at a locus, comprising application to the locus of an effective amount of at least one compound of formula (I): wherein R1, R3, A, X, Z and m have the meaning given in claim 1, and the agronomically acceptable salts or N-oxides thereof, and to novel compounds of formula I as well as to herbicidal compositions containing such compounds as active ingredients.

Abstract: The present invention relates to hydrazinyl and nitrogen oxide pyrazoles of the formula I: wherein the ring of the formula (R5)-A-(SOmR4), m, X, R1 through R5 are as defined in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock animals.

Abstract: A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula I wherein Q, R1, R2, R3 and R4 are as described in the specification.

Abstract: The present invention relates to 5-(alkylidene-cycloalkyl)-pyrazoles and 5-(alkylidene-heterocyclyl)-pyrazoles of the formula I: wherein the ring of the formula (R5)-A-(SOmR4), m, B, ring G, R1 through R7 are as defined in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer, and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock animals.

Abstract: Compounds of formula (I), wherein the variables and the index have the following meanings: R1 H, halogen, alkyl, haloalkyl, alkenyl, haloalkenyl, alkylthio, alkoxyalkyl, alkylthioalkyl, or optionally substituted phenyl; R2 H, halogen, alkyl, haloalkyl, alkenyl, haloalkenyl or optionally substituted phenyl; A H, OH, CN, NO2, halogen, SCN, alkoxy, haloalkoxy, alkenyloxy, alkylthio, haloalkylthio, alkylsulfinyl, alkylsulfonyl, aminothiocarbonyl, hydroxycarbonyl, alkoxycarbonyl, or aminocarbonyl; B H, OH, NH2, CN, NO2, halogen, optionally substituted alkyl, optionally substituted alkoxy, optionally substituted alkenyl, alkenyloxy, alkylthio, haloalkylthio, alkoxythiocarbonylthio, alkoxycarbonylalkoxy, alkoxycarbonylalkylthio, alkylsulfinyl, alkylsulfonyl, aminothiocarbonyl, NR3R4, N═CHOR5, or N═CHNR5; R3, R4 H, alkyl, alkoxycarbonylalkyl, [(alkoxycarbonyl)(alkenyl)]alkyl, alkoxycarbonylalkenyl, alkylcarbonyl, cycloalkylcarbonyl, alkylaminocarbonyl, diaminocarbonyl, alkoxycarbonyl, alkoxyaminos

Abstract: A process for the preparation of a compound of the formula (I): wherein R1 is CN or CSNH2; X is N or CR4; R2 and R4 are each independently hydrogen or chloro; R3 is halo, haloalkyl, haloalkoxy or —SF5; R5 and R6 are each independently alkyl and n is 0, 1 or 2; said process comprising reacting a compound of the formula (II): wherein the symbols are as defined above and W is H, with an alkylating agent of the formula (III): R6—Y  (III) wherein R6 is as defined above and Y is a leaving group. The process may also be conducted by reacting a compound of formula (II) initially with an inorganic salt or an organic base, and reacting the resultant salt of the compound of formula (II) with the alkylating agent.

Abstract: An efficient synthesis of sulfonyl pyrazoles of formula I: wherein the ring of the formula (R5)-A-(SOmR4), m, R1 through R9 are as defined in the specification, comprising reacting a compound of formula II: wherein the ring of the formula (R5)-A-(SOmR4), m R1 through R9 are as defined above and wherein R10 is halo, (C1-C6)alkyl-SO3—, (C6-C10)aryl-SO3—, (C1-C6)alkyl-SO2—, or (C6-C10)aryl-SO2—; wherein each of said (C1-C6)alkyl component of said (C1-C6)alkyl-SO3— and (C1-C6)alkyl-SO2— radicals may optionally be substituted on any carbon atom by one to six fluoro substituents per (C1-C6)alkyl component; with a compound of formula R3—H, wherein R3 is as defined above, in the presence of a fluoride containing salt and in the presence of a solvent.

Abstract: The present invention relates to a compound of the formula (I) or salt thereof in which R1 is identical or different at each occurrence and is H, halogen, CN, nitro, SF5, (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, (C1-C8)alkoxy, [(C1-C8)alkyl]-carbonyl or (C1-C8)alkylsulfonyl, each of the radicals being unsubstituted or substituted,  or is S(O)p—R7, where p=0, 1 or 2 and R7 is (C1-C8)alkyl, (C1-C8)haloalkyl or NR8R9, where  R8 and R9 independently of one another are identical or different and are H, (C1-C8)alkyl, (C2-C8)alkenyl, (C7-C10)arylalkyl, (C7-C10)alkylaryl or (C6-C10)aryl, each of the last-mentioned five radicals being unsubstituted or substituted,  or is a group of the formula where R10 is (C1-C8)alkyl which is unsubstituted or substituted, and W=O or S, A is optionally substituted aryl or an optionally substituted heterocyclic radical, X is O or S, R2,R3,R4, and R5 are identical or different and are H, hal

Abstract: 1

Abstract: The invention relates to the use of compounds of formula (I) as medicaments, to the novel compounds of formula (I) themselves, and to a method for the production thereof.

Abstract: There is provided a compound of formula I: wherein X represents O or NR5 R4 represents H, halo, cyano, nitro, halo(loweralkyl), OR6, OC(O)R7, C(O)R8, C(O)OR9, C(O)NR10R11, NR12R13, NR16Y(O)R17, N[Y(O)R17]2, SOR18, SO2R19, C(O)AZ, lower alkyl, lower alkenyl, lower alkynyl, Het, alkylHet, aryl, alkylaryl (which latter seven groups are all optionally substituted with one or more substituents selected from halo, cyano, nitro, lower alkyl, halo(loweralkyl), OR6, OC(O)R7, C(O)R8, C(O)OR9, C(O)NR10R11, NR12R13 and SO2NR14R15) which are useful in the curative and prophylactic treatment of a medical condition for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g., cGMP PDE5) is desired.

Abstract: This invention relates to a novel process of preparing selected 5-substituted pyrazoles useful as p38 kinase and COX-2 inhibitors.

Abstract: A process for the preparation of a compound of general formula (I), wherein R1 is CN or CSNH2; R2 is hydrogen or chloride; and R3 is halogen or haloalkyl or haloalkoxy or SF5 which process comprises reacting a compound of formula (II), where R1, R2 and R3 are as defined above; with a proton source.

Abstract: The present invention comprises novel and known pyrazole derivatives having anti-HIV activity, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the compounds of formula I are inhibitors of the human immunodeficiency virus reverse transcriptase enzyme which is involved in viral replication. Consequently the compounds of this invention may be advantageously used as therapeutic agents for HIV infection.

Abstract: A process for the preparation of a compound of formula (I) 1

Abstract: The present invention is directed to compounds useful in the treatment of diseases associated with prenylation of proteins and pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising same, and to methods for inhibiting protein prenylation in an organism using the same.

Abstract: A process for the preparation of a compound of formula (I) comprising oxidizing a compound of formula (II) with trifluoroperacetic acid in the presence of a corrosion inhibiting compound such as boric acid. Also, a process for preparing a compound of formula (II) by adding sulfur dioxide to a mixture of the corresponding disulfide, a formate salt, trifluoromethyl bromide and a polar solvent; and a process for preparing the disulfide comprising adding S2Cl2 to a solution, in an organic solvent, of the corresponding 4-unsubstituted pyrazole.

Abstract: A process for the preparation of a compound of the formula (I): 1

Abstract: This invention describes novel pyrazole compositions comprising a pharmaceutically acceptable carrier and a compound of formula V: wherein Z1 is N, CRa, or CH, and Z2 is N or CH, provided one of Z1 and Z2 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from —R1; Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T—R3, or Rx and Ry are taken together with their intervening atoms to form a fused ring; and R1, R2, R2′, R3, and T are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.

Abstract: The invention relates to novel 1-arylpyrazole oxime derivatives, of general formula (I) or (I bis) 1

Abstract: This invention relates to a compound of the formula: 1

Abstract: The present invention relates to 5-heteroatom-substituted pyrazoles of the formula I: 1

Abstract: This invention relates to pyrazole derivatives of formula (I) 1

Abstract: The present invention provides a compound of the formula (I):   wherein A ring, B ring and C ring are each independently optionally substituted aromatic carbocycle or optionally substituted 5- or 6-membered heterocycle which may fuse with benzene ring, W1, W2 and/or W3 represents a bond when A ring, B ring and/or C ring is optionally substituted 5-membered heterocycle, X is —O—, —NR1— wherein R1 is hydrogen, lower alkyl etc. or the like, Y is hydrogen, lower alkyl, lower alkenyl or the like, one of V1 and V2 is a bond, and the other is a bond, —O— or the like, and a pharmaceutical composition comprising the same.

Abstract: The invention is concerned with novel pyrazole derivatives, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the compounds of formula I are inhibitors of the human immunodeficiency virus reverse transcriptase enzyme which is involved in viral replication. Consequently the compounds of this invention may be advantageously used as therapeutic agents for HIV mediated process.

Abstract: A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula I wherein Q, R1, R2, R3 and R4 are as described in the specification.

Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.

Abstract: Thiazole-indole compounds useful as cyclin dependent kinase 11 inhibitors, for preventing/reducing the severity of epithelial cytotoxicity side-effects (e.g., alopecia, plantar-palmar syndrome, mucositis) induced by chemoptherapy and/or radiation therapy in a patient receiving such therapy.

Abstract: This invention relates to a novel process of preparing selected 5-substituted pyrazoles useful as p38 kinase and COX-2 inhibitors.

Abstract: The novel compounds of formula I: wherein A has the meaning set forth in the description, and herbicidal compositions containing such compounds as active ingredients.

Abstract: Benzoylcyclohexanediones and benzoylpyrazoles, their preparation and their use as herbicides and plant growth regulators. There are described benzoyl compounds of the formula (I), their preparation and their use as herbicides and plant growth regulators. In this formula (I), R1, R2, R3 and R4 are various radicals, X is an alkylene chain which may contain a hetero atom and Het is a heterocycle or heteroaromatic ring.

Abstract: The invention relates to novel arylpyrazoles of the formula (I): wherein R1, R3, R7, R14, R15, R16, and R17 are as defined in the description, and to their use as pesticides.

Abstract: The present invention relates to compounds of the formula 1

Abstract: The invention relates to novel 1-arylpyrazole oxime derivatives, of general formula (I) or (I bis) 1

Abstract: Compounds of the formula I and salts thereof, in which the substituents and the index n have the following meanings: Q is —C(═CHCH3)—COOCH3, —C(═CHOCH3)—COOCH3, —C(═NOCH3)—COOCH3 or —C(═NOCH3)—CONH(CH3); R1 is hydrogen, halogen, C1-C4-alkyl, C1-C2-haloalkyl, C1-C4-alkoxy or C1-C2-haloalkoxy; R2 is halogen, C1-C4-alkyl, C1-C2-haloalkyl, C1-C4-alkoxy; n is 0, 1 or 2, where the substituents R2 may be different if n=2; R3 is phenyl, pyridyl or pyrimidyl, compositions comprising them and the use of the compounds I and the compositions for controlling harmful fungi and animal pests are described.

Abstract: Compounds of formula (I) 1

Abstract: The invention relates to 1-arylpyrazole-3-thiocarboxamide derivatives of formula (I): 1

Abstract: This invention relates to a novel process of preparing selected 5-substituted pyrazoles useful as p38 kinase and COX-2 inhibitors.

Abstract: A 1-aryl-3-cyano-5-(het)arylalkylaminopyrazole derivative represented by the general formula (1): process of making, intermediate thereof and pesticide therewith.

Abstract: Compounds of the following formula I wherein wherein all variables are as defined in the specification and the pyrazoleN-oxides, agrochemically acceptable salts and stereisomers thereof useful as herbisdes.

Abstract: A process for the preparation of arylamides of heteroaromatic carboxylic acids of the formula: in which each An is nitrogen or CRn(n=1 to 5), with the proviso that at least one of the ring members is nitrogen and that two nitrogen atoms are not bonded directly to one another; R1 to R5, if present, independently of one another are hydrogen, C1-4-alkyl or aryl, one of the substituents R1 to R5 being a group of the formula —OR, in which R is an optionally substituted aromatic or heteroaromatic radical; R6 is hydrogen or C1-4-alkyl; and R7 is an optionally substituted aromatic or heteroaromatic radical. The amides are obtained from the corresponding heteroaromatic halogen compounds, the corresponding aromatic amines and carbon monoxide in the presence of a palladium phosphine complex. Compounds of this class are important herbicides.

Abstract: Benzylidenepyrazolones of the formula I, Useful as herbicides.

Abstract: The invention relates to new substituted 1-arylpyrazoles of the general formula (I) to a plurality of processes for their preparation, and to their use as pesticides.