Patents Examined by C. S. Aulakh
  • Patent number: 6174915
    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
  • Patent number: 6169097
    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
  • Patent number: 6166051
    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.
    Type: Grant
    Filed: June 23, 1998
    Date of Patent: December 26, 2000
    Assignee: Zambon Group S.p.A.
    Inventors: Franco Pellacini, Stefano Romagnano, Gabriele Norcini, Francesco Santangelo, Claudio Semeraro
  • Patent number: 6150540
    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
  • Patent number: 6143905
    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
  • Patent number: 6143894
    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
  • Patent number: 6124455
    Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning defined in the specification have retinoid-like biological activity.
    Type: Grant
    Filed: January 25, 2000
    Date of Patent: September 26, 2000
    Assignee: Allergan Sales, Inc.
    Inventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna
  • Patent number: 5663352
    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
  • Patent number: 5635517
    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