Publication number: 20030225059
Abstract: The present invention relates compounds of the formula (I): wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of: (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k), (l) and R1, R2, R3, R4, R5, R6, R7, R13, R14, R15, R16, R?17, R18, R19, R21a and R21b are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.
Type:
Application
Filed:
November 13, 2002
Publication date:
December 4, 2003
Inventors:
Jose Luis Castro Pineiro, Kevin Dinnell, Jason Matthew Elliott, Gregory John Hollingworth, Duncan Edward Shaw, Christopher John Swain, Lihu Yang
Publication number: 20030207865
Abstract: This invention relates to 2-arylimino heterocycles, including 2-arylimino-1,3-thiazolidines, 2-arylimino-2,3,4,5-tetrahydro-1,3-thiazines, 2-arylimino-1,3-thiazolidin-4-ones, 2-arylimino-1,3-thiazolidin-5-ones, and 2-arylimino-1,3-oxazolidines, and their use in modulating progesterone receptor mediated processes, and pharmaceutical compositions for use in such therapies.
Type:
Application
Filed:
October 23, 2001
Publication date:
November 6, 2003
Inventors:
Brian R. Dixon, Cedo M. Bagi, Catherine R. Brennan, David R. Brittelli, William H. Bullock, Jinshan Chen, William L. Collibee, Robert Dally, Jeffrey S. Johnson, Harold C. E. Kluender, William F. Lathrop, Peiying Liu, Carol Ann Mase, Aniko M. Redman, William J. Scott, Klaus Urbahns, Donald J. Wolanin
Patent number: 6613776
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.
Type:
Grant
Filed:
September 14, 2001
Date of Patent:
September 2, 2003
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Ronald Knegtel, David Bebbington, Hayley Binch, Julian Golec, Sanjay Patel, Jean-Damien Charrier, David Kay, Robert Davies, Pan Li, Marion Wannamaker, Cornelia Forster, Albert Pierce
Patent number: 6593322
Abstract: Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective for ER-&bgr; over ER-&agr;. Methods are disclosed for modulating ER-&bgr; in cell and/or tissues expressing the same, including cells and/or tissue that preferentially ER-&bgr;. Methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natureal hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.
Type:
Grant
Filed:
September 21, 2000
Date of Patent:
July 15, 2003
Assignee:
Signal Pharmaceuticals, Inc.
Inventors:
Shripad S. Bhagwat, Leah Marie Gayo-Fung, Bernd M. Stein, Qi Chao, Anthony R. Gangloff, Jeffrey A. McKie, Kenneth D. Rice
Publication number: 20020169156
Abstract: The present invention discloses compounds of formula (1) or (2), any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein n is 0, or 1; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; and R1 is aryl which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl and a monocyclic 5 to 6-membered heteroaryl group a monocyclic 5 to 6-membered heteroaryl group which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl and a monocyclic 5 to 6-membered heteraryl group, or a bicyclic heteroaryl group composed of a monocyclic
Type:
Application
Filed:
April 30, 2002
Publication date:
November 14, 2002
Applicant:
Neurosearch A/S
Inventors:
Dan Peters, Gunnar M. Olsen, Simon F. Nielsen, Elsebet O. Nielsen
Patent number: 6420395
Abstract: The present invention discloses compounds of formula (1) or (2), any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein n is 0, or 1; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalky-alkyl, aryl or aralkyl; and R1 is aryl which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cyloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl and a monocyclic 5 to 6-membered heteroaryl group a monocyclic 5 to 6-membered heteroaryl group which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3.
Type:
Grant
Filed:
November 29, 1999
Date of Patent:
July 16, 2002
Assignee:
Neurosearch A/S
Inventors:
Dan Peters, Gunnar M. Olsen, Simon F. Nielsen, Elsebet O. Nielsen