Monsanto Company

Pharmacia Corporation

University of Oklahoma

Pfizer Products Inc.

Gopichand Yalamanchili

Dennis Paul Phillion

Peter Gerrard Ruminski

Michael Mao

Jerry D Clark

Jodi L Moe

Partha Mudipalli

Christine B Seymour

Tobin C Schilke

Kimberley C Allen

Shaun Raj Selness

Sarath P Gunasekera

Jon P Lawson

Sastry A Kunda

Dennis K Anderson

Win Naing

John Walker

Lisa L McDermott

Patrick H Lau

Francis J Schmitz

Clay Little

Dick Van Der Helm

M Bilayet Hossain

Patricia S Miyake

Shekhar Viswanath

John E Baldus

Thomas P Fraher

Dan R Dukesherer

Albert D Edney

Tom Fevig

Rajappa Vaidyanathan

Jason A Hanko

Todd Boehlow

Kimberly L Kolbert

Ahmad Y Sheikh

Ronald Vanderroest

George Klemm

Daniel Dukeshereer

Randy Geurink

Richard Vonder Embse

Brian Chekal

This invention is directed generally to a process for making substituted pyrazoles, tautomers of the substituted pyrazoles, and salts of the substituted pyrazoles and tautomers. The substituted pyrazoles correspond in structure to Formula (I): wherein R, R, R, Y, Y, Y, Y, and Yare as defined in the specification.

Process for making substituted pyrazoles

Crystalline forms of the p38 kinase inhibitor N-(2-hydroxyacetyl)-5-(4-piperidyl)-4-(4-pyrimidinyl)-3-(4-chlorophenyl)pyrazole are provided. These crystalline forms include (a) a first anhydrous crystalline form possessing improved physical stability relative to other solid-state forms of the compound; (b) a second anhydrous crystalline form possessing unique properties relative to other solid-state forms of the compound; (c) a third anhydrous crystalline form possessing unique properties relative to other solid-state forms of the compound; and (d) solvated crystalline forms, hydrated crystalline forms, and crystalline salt forms of the compound that are useful, for example, as intermediate solid-state forms in the preparation of other crystalline forms of the compound. Also provided are combinations and pharmaceutical compositions comprising at least one of these crystalline forms, processes for preparing these crystalline forms and for preparing compositions comprising these 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 at least one of these crystalline forms.

Solid-state forms of N-(2-hydroxyacetyl)-5-(4-piperidyl)-4-(4-pyrimidinyl)-3-(4-chlorophenyl) pyrazole

Fluorinated alkene compounds useful for and methods of controlling nematodes, insects, and acarids that prey on agricultural crops. Polar compounds are particularly useful for systemic control of pests.

Fluoroalkenyl compounds and their use as pest control agents

Fluorinated alkene compounds useful for and methods of controlling nematodes, insects, and acards that prey on agricultural crops. Polar compounds are particularly useful for systemic control of pests.

Novel 3,4,4-trifluorobutenoic acid derivatives of the formula ##STR1## wherein Q is --(C.dbd.W)--R.sub.2 wherein W is O or S, and R.sub.2 is an aliphatic or aromatic group when W.dbd.O; --OR.sub.50 ; --SR.sub.50 ; or --NR.sub.50 R.sub.60 wherein R.sub.60 is hydrogen or R.sub.50 ; NR.sub.7 R.sub.8 ; a heterocyclic group; phenyl substituted by alkyl; or any agronomically acceptable salt thereof having usefulness as nematocides, insecticides and acaricides.

Fluorinated alkene compounds useful for and methods of controlling nematodes, insects, and acarids that prey on agricultural crops, these compounds having the structure: ##STR1## where Q is --(C.dbd.S)--R.sub.1 and R.sub.1 is --OR.sub.5, --SR.sub.5, halogen, --NHOH or --NR.sub.5 R.sub.6. Each of R.sub.5 and R.sub.6 is independently hydrogen; an aliphatic or an aromatic group; a C.sub.1 -C.sub.12 aliphatic amine group; a C.sub.2 -C.sub.12 aliphatic carboxylic acid group; or R.sub.5 and R.sub.6 when taken together with the N of R.sub.1 are a protein amino acid or a cyclic group. Polar compounds are particularly useful for systemic control of pests.

Fluorinated alkene compounds useful for controlling nematodes, insects, and acarids that prey on agricultural crops, these compounds having the formula BrCF.sub.2 CFClCH.sub.2 CO--R where R is R.sub.1 or R.sub.2. R.sub.1 is --SR.sub.5, halogen, --NHOH or --NR.sub.5 R.sub.6, where R.sub.5 and R.sub.6 are independently H; an aliphatic or aromatic group; an aliphatic amine group; an aliphatic carboxylic acid group; or R.sub.5 and R.sub.6 when taken with the N of R.sub.1 are an amino acid or a cyclic group or R.sub.1 is --OR.sub.5, where R.sub.5 is an aliphatic or aromatic group; an aliphatic amine group; or an aliphatic carboxylic acid group. R.sub.2 is --SR.sub.5 or --NR.sub.5 R.sub.6, where R.sub.5 and R.sub.6 are independently H; an aliphatic, aromatic or heterocyclic group; an aliphatic amine group; an aliphatic carboxylic acid group; R.sub.5 and R.sub.6 when taken with the N of R.sub.2 are an amino acid or a cyclic group; R.sub.5 and R.sub.6 when taken with the N of R.sub.2 are pyrazole, imidazole, or triazole; a heterocyclic group; or phenyl or NR.sub.7 R.sub.8 or R.sub.2 is --OR.sub.5, where R.sub.5 is an aliphatic, aromatic or heterocyclic group; an aliphatic amine group; an aliphatic carboxylic acid group; a heterocyclic group; or phenyl or NR.sub.7 R.sub.8. R.sub.7 is H or an aliphatic or aromatic group. R.sub.8 is phenyl, substituted phenyl, --OR.sub.9, --C(O)R.sub.9, --NR.sub.9 R.sub.10, --S(O).sub.2 R.sub.11 or --P(.dbd.O)R.sub.12 R.sub.13. R.sub.9 and R.sub.10 are independently H, alkyl or aryl. R.sub.11 is H, alkyl, haloalkyl or aryl. R.sub.12 and R.sub.13 are independently H, alkyl, aryl, alkoxy, aryloxy, alkylthio, alkylthio, arylthio, alkylamino, dialkylamino, arylamino or --OR.sub.14, where R.sub.14 is H, alkyl or aryl. These polar compounds are particularly useful for systemic control of pests.

Fluorinated alkene compounds useful for and methods of controlling nematodes, insects, and acarids that prey on agricultural crops, these compounds having the general structure: ##STR1## These Polar compounds are particularly useful for systemic control of pests.

A compound having cytotoxic activity of the formula: ##STR1## and a composition comprising such compound in a suitable pharmaceutical carrier.

Tedanolide

Growing community of inventors

St. Louis, MO, United States of America

Gopichand Yalamanchili