Abstract: This invention is directed generally to pyrazoles that, inter alia, inhibit p38 kinase, TNF, and/or cyclooxygenase-2 activity.

Abstract: The present invention relates to compounds of the formula I, wherein Z1, Z2, R1, R2 and R3 are defined as in the specification, pharmaceutical compositions containing such compounds the use of such compounds to treat neurological and gastrointestinal disorders.

Abstract: Described herein are compounds useful in the treatment of migraine, which have the general formula: wherein: W is a CH group or a N atom; Z is N or C—R4; B and D are selected independently from CH and N, with the proviso that at least one of B and D is CH and with the further proviso that one of B and D can represent N only when W and Z are both other than N; A is a group of Formula II, III or IV, such that group A contains at least 1 N atom; NR7 is either —NH— or —N═; is a single or double bond; X is a N atom, a CH group or a C(OH) group when is a single bond; or, when is a double bond, a C atom; Y is an NH, N-alkyl, N-benzyl or CH2 group; U and V each represent a N atom or a CH group, with the proviso that both cannot be N; a and b are, independently, 0 or 1; c is an integer from 0 to 3; d is an integer from 1 to 3; e is an integer from 1 to 2; f is an integer from 0 to 3; g is an integer from 3 to 6 and h is an integer from 2 to 3; such that the sum of c a

Abstract: The present application describes modulators of CCR3 of formula (I): 1

Abstract: The present invention relates to compounds having the general formula 1

Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein R1, R2, T, n and Q are as described in the specification. The compounds are useful for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases, such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.

Abstract: 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.

Abstract: N-Piperidino-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethylpyrazole-3-carboxamide and its salts and solvates are powerful antagonists of the CB1 cannabinoid receptors. They are prepared by reacting a functional derivative of 5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethylpyrazole-3-carboxylic acid with 1-aminopiperidine, optionally followed by salification.

Abstract: Certain compounds which contain a piperidine moiety flanked by aryl groups are inhibitors of p38-&agr; kinase and thus useful in the treatment of a variety of conditions characterized by inappropriate p38-&agr; kinase activity.

Abstract: The present invention discloses compounds which, are novel receptor antagonists for NPY Y5 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y5 receptor antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

Abstract: This invention is directed to aromatic sulfone hydroxamates (also known as “aromatic sulfone hydroxamic acids”) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.

Abstract: A compound represented in general formula (X) and (XI):

Abstract: This invention is directed towards novel compounds as opioid receptor modulators, antagonists, and agonists useful for the treatment of opioid modulated disorders such as pain and gastrointestinal disorders.

Abstract: The present invention provides pyrazole and pyrazolone derivatives. Preferred compounds of the invention are useful as RNA polymerase inhibitors. Further preferred compounds of the invention are useful as antimicrobial agents.

Abstract: The present invention provides a method of treatment of a subject suffering from a disease, such as schizophrenia, for which the administration of an NK-3 antagonist is indicated which comprises administering to that subject a therapeutically effective amount of a compound of formula I: 1

Abstract: Compounds of the formula (I), are described in which X is halogen, cyano, nitro, (C1-C4)-alkyl, (C1-C4)-alkoxy, (C1-C4)-alkylthio or (C1-C4)-alkylsulfinyl; R1 is halogen, (C1-C4)-haloalkyl, (C1-C4)-alkyl, (C1-C4)-alkoxy, (C1-C4)-haloalkoxy or cyano; m is 0 to 3; n is 1 to 5; Z is oxygen, sulfur, CH2 or NR2; R2 is CN, (C1-C4)-alkoxy-(C1-C4)-alkyl, CHO, (C1-C6)-alkylcarbonyl, (C1-C6)-alkoxycarbonyl or (CW)NR3R4; R3, R4 are H or (C1-C6)-alkyl; W is O or S; G is mono- to tetrasubstituted isoxazoline which is attached in the 3-, 4- or 5-position to the adjacent phenyl ring. The compounds are suitable for use as pesticides.

Abstract: N-Piperidino-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethylpyrazole -3-carboxamide and its salts and solvates are powerful antagonists of the CB1 cannabinoid receptors. They are prepared by reacting a functional derivative of 5-(4-bromophenyl)-1-(2,4-dichlorophenyl) -4-ethylpyrazole-3-carboxylic acid with 1-aminopiperidine, optionally followed by salification.

Abstract: Compounds of formula (I), (IIa) or (IIb) wherein R1-R6, Z, Q and n are as defined in claim 1 and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors. Compositions comprising a compound of formula (I), (IIa) or (IIb) are also described.

Abstract: Described are piperidines of Formula I and pharmaceutically acceptable salts thereof. The compounds of Formula I are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, stroke, cerebral ischemia, central nervous system disorders, depression, trauma, hypoglycemia, neurodegenerative disorders, anxiety, migraine headache, convulsions, Parkinson's disease, aminoglycoside antibiotics-induced hearing loss, psychosis, glaucoma, CMV retinitis, opioid tolerance or withdrawal, pain, especially chronic pain, neuropathic pain, or surgical pain, or urinary incontinence.

Abstract: A class of phenylsulphonyl derivatives wherein the sulphonyl moiety is also attached to an N-arylalkyl-substituted azetidine, pyrrolidine or piperidine ring are selective antagonists of the human 5-HT2A receptor and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse conditions of the central nervous system, including schizophrenia and depression.

Abstract: The present invention describes a method of purifying a pesticide that includes: a) melting a pesticide, wherein the pesticide includes at least one active ingredient and at least one impurity capable of inhibiting crystallization; b) coating the pesticide on a substrate to form a pesticide particle; c) substantially reducing the amount of crystallization inhibiting impurity by an azeotropic method; and d) crystallizing the pesticide. In another embodiment, the present invention includes a method of purifying a pesticide as described above, such that the pesticide has a melting point of not more than about 90° C. Also included in the invention is the product produced by the above process for the pesticide, methyl N-(2-{[1-(4-chlorophenyl)-1H-pyrazol-3-yl]oxymethyl}phenyl)N-methoxy carbamate.

Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.

Abstract: Compounds of formula (I) wherein Y represents a group (CH2)n, wherein n represents 0, 1 or 2; R1 is phenyl, naphthyl, a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S; or a group NR3R4 wherein one of R3 and R4 is hydrogen or optionally substituted (C1-4)alkyl and the other is phenyl, naphthyl or a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S, or R3 and R4 together with the N atom to which they are attached form a 5 to 7-membered cyclic amine which has an optionally fused phenyl ring; any of which R1 groups may be optionally substituted; R2 represents phenyl or a 5- or 6-membered hereroaryl group containing up to 3 heteroatoms selected from N, O and S, wherein the phenyl or heteroaryl group is substituted by R5, and further optional substituents; or R2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing up to 3 heteroatoms selected from N, O and S; R5 represents an optionally s

Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.

Abstract: The present invention relates to 5-heterocyclo-pyrazoles of the formula I: wherein ring W, m, n, and 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: Compounds of formula (1), and pharmaceutically acceptable salts thereof, are capable of blockading voltage-dependent sodium channels and are useful in particular, in treating glaucoma and multiple sclerosis.

Abstract: The invention concerns compounds of formula (I), and their use in therapy, particularly in the modulation of CCR3 activity.

Abstract: The present invention relates to substituted diphenyl heterocycle compounds and pharmaceutical compositions thereof that inhibit replication of HCV virus. The present invention also relates to the use of the compounds and/or compositions to inhibit HCV replication and/or proliferation and to treat or prevent HCV infections.

Abstract: The present invention is directed to novel heterocyclic substituted pyrazolones, including pharmaceutical compositions, diagnostic kits, assay standards or reagents containing the same, and methods of using the same as therapeutics. The invention is also directed to intermediates and processes for making these novel compounds.

Abstract: Novel compounds having general formula (I), and pharmaceutically and veterinarily acceptable salts thereof wherein R1, R2, R3, W, Y1, Y2, X, n and y are as defined above and processes for their preparation and intermediate compounds prepared therein. The novel compounds are useful for having utility in the treatment of pruritic dermatoses including allergic dermatitis and atopy in animals and humans.

Abstract: Compounds of formulae I and I′, methods of making them, pharmaceutical compositions containing them, and methods for their use. The compounds are antagonists of IL-2/IL-2R binding; and are useful for the treatment of interleukin-2 mediated diseases, such as autoimmune diseases (such as rheumatoid arthritis, multiple sclerosis, uveitis, and psoriasis), allograft rejection, and graft-versus-host disease.

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

Abstract: A “one-pot” process is described herein for the production of pyrazole compounds of general formula (II) 1

Abstract: A compound of general formula (I) 1

Abstract: 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.

Abstract: The invention provides compounds of general formula (I) wherein R1, R2, R3, R4, A, Q, U, V, W, X, Y and n are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, especially for the treatment of chemokine receptor related diseases and conditions.

Abstract: Compounds of general formula (I) 1

Abstract: 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.

Abstract: Compounds of formula (I) and pharmaceutically-acceptable derivatives thereof, are matrix metalloprotease inhibitors, useful in treatment of conditions mediated by matrix metalloproteases, such as chronic dermal ulcers.

Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: and physiologically acceptable salts thereof.

Abstract: The present invention relates to compounds of the formula I, wherein Z1, Z2, X, Q, R1, R2 and R3 are defined as in the specification, pharmaceutical compositions containing such compounds the use of such compounds to treat neurological and gastrointestinal disorders.

Abstract: Benzylidenepyrazolones of the formula I, where the substituents and the index n have the following meanings: R1 is unsubstituted or substituted C1-C6-alkyl; R2 is unsubstituted or substituted C1-C6-alkyl, unsubstituted or substituted C1-C6-alkoxy, halogen, nitro, cyano; R3 is hydrogen, halogen, nitro, cyano, a group NR5R6, OCOR5, NR5COR6, CO2R5, —COSR5, —CONR5R6, C1-C4-alkoxyiminoalkyl, C1-C6-alkylcarbonyl, unsubstituted or substituted C1-C6-alkyl, unsubstituted or substituted C1-C6-alkoxy, unsubstituted or substituted C1-C6-alkylthio, unsubstituted or substituted C2-C6-alkenyl, unsubstituted or substituted C2-C6-alkynyl, unsubstituted or substituted phenyl, unsubstituted or substituted phenoxy, an unsubstituted or substituted 5- or 6-membered saturated or unsaturated heterocycle which may contain up to 4 nitrogen atoms and/or up to 2 oxygen or sulfur atoms as ring members; R4 is C1-C6-alkyl, C1-C4-haloalkyl; R3 and R4 form an optionally substituted saturated or unsaturated

Abstract: N-Piperidino-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethylpyrazole-3-carboxamide and its salts and solvates are powerful antagonists of the CB1 cannabinoid receptors. They are prepared by reacting a functional derivative of 5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethylpyrazole-3-carboxylic acid with 1-aminopiperidine, optionally followed by salification.

Abstract: Disclosed are compounds that are highly selective partial agonists or antagonists at human CRF1 receptors that are useful in the diagnosis and treatment of treating stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety. The compounds have the formula or the pharmaceutically acceptable salts thereof wherein Ar, R1, R2, A, and Z are various organic and inorganic substituents.

Abstract: A substituted 4-, 5-, 6-, and 7-indole derivative of Formula (I) 1

Abstract: A “one-pot” process is described herein for the production of pyrazole compounds of general formula (II) 1

Abstract: N-Piperidino-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethylpyrazole-3-carboxamide and its salts and solvates are powerful antagonists of the CB1 cannabinoid receptors. They are prepared by reacting a functional derivative of 5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethylpyrazole-3-carboxylic acid with 1-aminopiperidine, optionally followed by salification.

Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R2, R3, R4, R5, R7, R8, X, n, x and y are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.

Abstract: The invention provides compounds of formula 1 1

Abstract: The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises a thiazolium compound capable of inhibiting, and to some extent reversing, the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated. A novel immunoassay for detection of the reversal of the nonenzymatic crosslinking is also disclosed.