Abstract: The present invention is directed to compound of the formula I:
wherein R1, R2, R3, R4, R5, X, Y, and
are as defined herein.
These compounds are useful for inhibiting the activity of a metalloproteinase by contacting the metalloproteinase with an effective amount of the inventive compounds.
Type:
Grant
Filed:
May 11, 1999
Date of Patent:
January 16, 2001
Assignees:
Agouron Pharmaceuticals, Inc., Syntex (U.S.A.) Inc.
Inventors:
Steven L. Bender, Arlindo L. Castelhano, Wesley K. M. Chong, Melwyn A. Abreo, Roland J. Billedeau, Jian Jeffrey Chen, Judith G. Deal
Abstract: The present invention concerns compounds of formula
the N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein n is 0, 1 or 2; m is 1 or 2, provided that if m is 2, then n is 1; p is 0, 1 or 2; ═Q is ═O or ═NR3; X is a covalent bond or a bivalent radical of formula —O—, —S—, —NR3—; R1 is Ar1; Ar1C1-6alkyl or di(Ar1)C1-6alkyl, wherein each C1-6alkyl group is optionally substituted with hydroxy, C1-4alkyloxy, oxo or a ketalized oxo substituent of formula —O—CH2—CH2—O— or —O—CH2—CH2—CH2—O—; R2 is Ar2; Ar2C1-6alkyl; Het or HetC1-6alkyl; R3 is hydrogen or C1-6alkyl; R4 is hydrogen; C1-4alkyl; C1-4aklyloxyC1-4alkyl; hydroxyC1-4alkyl; carboxyl; C1-4aklyloxycarbonyl or Ar3; R5 is hydrogen; hydroxy; Ar3; Ar3C1-6alkyloxy; di(Ar3)C1-6alkyloxy; Ar3C1-6alkylthio; di(Ar3)C1-6alkylthio; Ar3C1-6alkylsulfoxy; di(Ar3)C1-6alkylsulfoxy;
Type:
Grant
Filed:
June 22, 1998
Date of Patent:
January 2, 2001
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Frans Eduard Janssens, François Maria Sommen, Dominique Louis Nestor Ghislaine Surleraux, Yves Emiel Maria Van Roosbroeck
Abstract: Compounds of formula (I) wherein R, R.sub.1, R.sub.2, R.sub.3 have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients are described. The compounds of formula (I) are endowed with a mixed ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases.
Abstract: A tetrahydrofuran (THF) epoxide and method of its preparation according to a novel stereoselective synthetic method. The compounds of the invention are used to prepare therapeutically active mono-THF and bis-THF containing Annonaceous Acetogenins.
Type:
Grant
Filed:
November 2, 1998
Date of Patent:
November 21, 2000
Assignee:
Hughes Institute
Inventors:
Fatih M. Uckun, Keqiang Li, Shyi-Tai Jan
Abstract: 1,7-Disubstituted perylene-3,4,9,10-tetracarboxylic dianhydrides I and perylene-3,4,9,10-tetracarboxylic acids Ia ##STR1## where R is substituted or unsubstituted aryloxy, arylthio, hetaryloxy or hetarylthio,their preparation and use as pigments, laser dyes and precursors for preparing fluorescent dyes, polymeric colorants, pigments and pigment additives, and 1,7-disubstituted perylene-3,4,9,10-tetracarboxylic diimides (VI) as intermediates thereof.
Type:
Grant
Filed:
June 18, 1998
Date of Patent:
November 7, 2000
Assignee:
BASF Aktiengesellschaft
Inventors:
Arno Bohm, Harald Arms, Georg Henning, Peter Blaschka
Abstract: This invention is directed to methods for the preparation of [1S-[1a,2b,3b,4a(S*)]]-4-[7-[[1-(3-chloro-2-thienyl) methyl]propyl]amino]-3H-imidazo[4,5-b]pyridin-3-yl]-N-ethyl-2,3-dihydroxyc yclopentanecarboxamide, methods for the preparation of intermediates thereto, and to said intermediates themselves.
Type:
Grant
Filed:
January 19, 1999
Date of Patent:
November 7, 2000
Assignee:
Aventis Pharmaceuticals Products Inc.
Inventors:
Michael K. O'Brien, Herve Garcia, Patrick Leon, Tory H. Powner, Laurence W. Reilly, Harshavadan C. Shah, Michael D. Thompson, Ching T. Tsuei, Benoit J. Vanasse, Francis L. Walther
Abstract: The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts and prodrugs thereof, wherein X represents a propylene or propenylene chain optionally substituted by one or more of R.sup.4, R.sup.5, R.sup.6 and R.sup.7 ; m is 2, 3 or 4; n is 0, 1 or 2 when m is 2 or 3, and n is 0 or 1 when m is 4; R.sup.1 represents optionally substituted phenyl; R.sup.2 represents optionally substituted phenyl, heteroaryl, benzhydryl or benzyl; R.sup.3 represents H, COR.sup.9, CO.sub.2 R.sup.10, COCONR.sup.10 R.sup.11, COCO.sub.2 R.sup.10, SO.sub.2 R.sup.15, CONR.sup.10 SO.sub.2 R.sup.15, C.sub.1-6 alkyl optionally substituted by a group selected from (CO.sub.2 R.sup.10, CONR.sup.10 R.sup.11, hydroxy, cyano, COR.sup.9, NR.sup.10 R.sup.11, C(NOH)NR.sup.10 R.sup.11, CONHphenyl(C.sub.1-4 alkyl), COCO.sub.2 R.sup.10, COCONR.sup.10 R.sup.11, SO.sub.2 R.sup.15, CONR.sup.10 SO.sub.2 R.sup.15 and optionally substituted phenyl), Y--R.sup.8 or CO--Z--(CH.sub.2).sub.q --R.sup.12 ; R.sup.4 and R.sup.
Type:
Grant
Filed:
January 19, 1996
Date of Patent:
September 2, 1997
Assignee:
Merck Sharp & Dohme Limited
Inventors:
Angus Murray MacLeod, Kevin John Merchant, Graeme Irvine Stevenson
Abstract: 1-Oxo- and 1,3-dioxo-2-(2,6-dioxopiperidin-3-yl) isoindolines substituted with amino in the benzo ring reduce the levels of TNF.alpha. in a mammal. A typical embodiment is 1,3-dioxo-2-(2,6-dioxopiperidin-3-yl)-5-aminoisoindoline.
Type:
Grant
Filed:
July 24, 1996
Date of Patent:
June 3, 1997
Assignee:
Celgene Corporation
Inventors:
George W. Muller, David I. Stirling, Roger S. -C. Chen