Nitrogen Bonded Directly To The -c(=x)- Group Patents (Class 546/175)
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Patent number: 5643926Abstract: Novel substituted pyrazolidinones have been found to exhibit significant binding to cholecystokinin (CCK) receptors and gastrin receptors in the brain and/or peripheral sites such as the pancreas, stomach, and ileum. The pyrazolidinones are CCK and gastrin receptor antagonists and find therapeutic application in the treatment of gastrointestinal disorders, central nervous system disorders and for appetite regulation in warm-blood vertebrates. Pharmaceutical formulations for such indications are described.Type: GrantFiled: January 19, 1994Date of Patent: July 1, 1997Assignee: Eli Lilly and CompanyInventors: Raymond F. Brown, J. Jeffry Howbert, Karen L. Lobb, David A. Neel, Jon K. Reel, Beverley Greenwood
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Patent number: 5633380Abstract: The invention is substituted quinoline intermediates useful in the synthesis of the herbicide 2-(4-isopropyl-4-methyl 5-oxo 2-imidazolidinyl)-5-methoxymethylnicotinic acid and a process for preparing the herbicide intermediate 3-methoxymethyl-7- or 8-hydroxyquinoline.Type: GrantFiled: June 5, 1995Date of Patent: May 27, 1997Assignee: American Cyanamid CompanyInventor: Wen-Xue Wu
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Patent number: 5633231Abstract: The present invention relates to valine-containing, substituted pseudopeptides of the general formula (I) ##STR1## in which the substituents have the meaning given in the description, to processes for their preparation, and to their use as anti-viral agents, in particular against cytomegaloviruses.Type: GrantFiled: September 7, 1994Date of Patent: May 27, 1997Assignee: Bayer AktiengesellschaftInventors: Dieter Habich, Thomas J. Schulze, Jurgen Reefschlager, Jutta Hansen, Rainer Neumann, Gert Streissle, Arnold Paessens
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Patent number: 5631279Abstract: This invention relates to perhydroisoindole derivatives of 08/448,402 formula (I), wherein radicals R are phenyl radicals optionally 2-or 3-substituted by a halogen atom or a methyl radical; R.sub.1 is optionally substituted phenyl, cyclohexadienyl, naphthyl, indenyl or optionally substituted heterocyclyl; R.sub.2 is H, halogen, OH, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxy, alkylthio, acyloxy, acyloxy, carboxy, optionally substituted alkyloxycarbonyl, benzyloxycarbonyl, amino or acylamino; and R.sub.3 is optionally 2-substituted phenyl; optionally salts thereof where applicable; and preparation thereof. Said derivatives are particularly useful as neurokinin A antagonists.Type: GrantFiled: June 7, 1995Date of Patent: May 20, 1997Assignee: Rhone-Poulenc Rorer, S.A.Inventors: Andre Crespo, Veronique Fardin, Jean-Marc Guillaume, Jean-Luc Malleron, Jean-Francois Peyronel
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Patent number: 5616605Abstract: This invention is directed to a collagenase inhibitor of the formula: ##STR1##Type: GrantFiled: August 8, 1994Date of Patent: April 1, 1997Assignee: Research Corporation Tech., Inc.Inventors: Robert D. Gray, Arno F. Spatola, Krzysztof Darlak
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Patent number: 5605896Abstract: This invention provides bicyclic heterocyclic derivatives and their pharmaceutically acceptable salts useful for the treatment of hypertension, urethral and lower urinary tract contractions, and other disorders. The compounds are also useful for binding .alpha..sub.1 -adrenergic and 5HT.sub.1A serotonergic receptors, in vitro or in vivo.Type: GrantFiled: August 31, 1994Date of Patent: February 25, 1997Assignee: Recordati S.A., Chemical and Pharmaceutical CompanyInventors: Amedeo Leonardi, Gianni Motta, Carlo Riva, Rodolfo Testa
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Patent number: 5599826Abstract: Compounds of formula I ##STR1## in which A denotes a carbocyclic ring with 5 or 6 carbon atoms or a heterocyclic ring with a maximum of 4 heteroatoms in which the heteroatoms can be the same or different and denote oxygen, nitrogen or sulphur and the heterocycles can if desired carry an oxygen atom on one or several nitrogen atoms,B denotes --CH.dbd.CH--, --N.dbd.CH--, --CH.dbd.N--, O or S,W denotes CH.sub.2, O, CH(OH), CO or --CH.dbd.CH--,X denotes S, O or NR.sup.2 in which the residue R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl,Y is CH or N,R denotes naphthyl, pyridyl, furyl, thienyl or phenyl which if desired is mono- or disubstituted with C.sub.1 -C.sub.3 alkyl, CF.sub.3, C.sub.1 -C.sub.3 alkoxy, F, Cl or bromine,R.sup.1 denotes hydrogen or C.sub.1 -C.sub.6 alkyl andn equals 1-3as well as their tautomers, enantiomers, diastereomers and physiologically tolerated salts,processes for their production as well as pharmaceutical agents that contain these compounds for the treatment of diabetes.Type: GrantFiled: November 21, 1995Date of Patent: February 4, 1997Assignee: Boehringer Mannheim GmbHInventors: Alfred Mertens, Hans-Peter Wolff, Peter Freund
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Patent number: 5587388Abstract: The present invention provides cis-epoxide compounds represented by formula (I-1), (I-2) or (I-3) which are useful for treating or preventing diseases caused by HIV infection: ##STR1## wherein: A, B, D, E, R.sup.1, R.sup.10, R.sup.11, K, G, Q, r and J have the meanings as defined in the specification.Type: GrantFiled: November 30, 1993Date of Patent: December 24, 1996Assignee: Lucky LimitedInventors: Sung C. Kim, Nakyen Choy, Chang S. Lee, Young C. Son, Ho I. Choi, Jong S. Koh, Heungsik Yoon, Chi H. Park, Sang S. Kim
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Patent number: 5578608Abstract: An HIV protease inhibiting compound of formula I ##STR1## wherein: R is C.sub.1 -C.sub.6 alkyl, cycloalkyl, heterocycle, unsaturated heterocycle, aryl, cycloalkyl (C.sub.1 -C.sub.4)alkyl, heterocycle(C.sub.1 -C.sub.4)alkyl, unsaturated heterocycle (C.sub.1 -C.sub.4)alkyl, aryl(C.sub.1 -C.sub.4)alkyl, or --A--(CH.sub.2).sub.q --R.sup.0, where A is --O--, --NH-- or --S--; q is 0, 1, 2 or 3; and R.sup.0 is cycloalkyl, aryl, heterocycle or unsaturated heterocycle; ##STR2## where R.sup.1 is aryl, cycloalkyl, heterocycle or unsaturated heterocycle; R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.3 is an amino acid side chain, --CH.sub.2 CH.sub.3, --CH.sub.2 CH.sub.2 CH.sub.3, --CH.sub.2 (CH.sub.2).sub.2 CH.sub.3, --C(CH.sub.3).sub.3, cyano(C.sub.1 -C.sub.4)alkyl, unsaturated heterocycle (C.sub.1 -C.sub.4)alkyl, aryl(C.sub.1 -C.sub.4)alkyl, --(CH.sub.2).sub.s --A.sup.0 --(CH.sub.2).sub.r --R.sup.4, or --CH.sub.2 --C(O)--NR.sup.2 --(CH.sub.2).sub.r --R.sup.5, where s is 1, 2, 3 or 4; r is 0, 1, 2 or 3; A.sup.Type: GrantFiled: January 17, 1995Date of Patent: November 26, 1996Assignee: Eli Lilly and CompanyInventors: William J. Hornback, John E. Munroe
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Patent number: 5574164Abstract: Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth are disclosed.Type: GrantFiled: April 21, 1995Date of Patent: November 12, 1996Assignee: Hoescht Roussel Pharmaceuticals Inc.Inventors: John J. Tegeler, Barbara S. Rauckman, Russell R. L. Hamer, Brian S. Freed, Gregory H. Merriman
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Patent number: 5565473Abstract: Compounds having the formula I: ##STR1## are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.Type: GrantFiled: February 23, 1995Date of Patent: October 15, 1996Assignee: Merck Frosst Canada, Inc.Inventors: Michel L. Belley, Serge Leger, Marc Labelle, Patrick Roy, Yi B. Xiang, Daniel Guay
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Patent number: 5563154Abstract: Compounds characterized generally as tetrahydro-quinolinyl or tetrahydro-isoquinolinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein G is a tetrahydro-quinolinyl or tetrahydro-isoquinolinyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from--(CH.sub.2).sbsb.q--C.tbd.C-Vwherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: June 1, 1995Date of Patent: October 8, 1996Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, Robert E. Manning
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Patent number: 5557006Abstract: Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth fire disclosed.Type: GrantFiled: April 20, 1995Date of Patent: September 17, 1996Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: John J. Tegeler, Barbara S. Rauckman, Russell R. L. Hamer, Brian S. Freed, Gregory H. Merriman
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Patent number: 5552419Abstract: The invention relates to the compounds of formula I ##STR1## pharmaceutically acceptable prodrug derivatives and pharmaceutically acceptable salts thereof; methods for preparation thereof; pharmaceutical compositions comprising said compounds; and a method of inhibiting matrix-degrading metalloproteinase and of treating matrix-degrading metalloproteinase dependent conditions in mammals using such compounds.Type: GrantFiled: November 3, 1994Date of Patent: September 3, 1996Assignee: Ciba-Geigy CorporationInventors: Lawrence J. MacPherson, David T. Parker
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Patent number: 5543423Abstract: The present invention relates to compounds that can maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for treatment of multi-drug resistant cells, for prevention of the development of multi-drug resistance, and for use in multi-drug resistant cancer therapy.Type: GrantFiled: January 23, 1995Date of Patent: August 6, 1996Assignee: Vertex Pharmaceuticals, IncorporatedInventors: Robert E. Zelle, Matthew W. Harding
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Patent number: 5536731Abstract: The compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are, independent from each other, hydrogen, alkyl, or cyclic or bicyclic alkyl; R.sub.3 is an acyl substituent selected from the group consisting of formyl, alkanoyl, alkenoyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; A is selected from the group consisting of: ##STR2## wherein R.sub.4 is hydrogen, alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, amino, alkylamino, dialkylamino, alkylsulfonamido, alkylcarboxamido, nitro, cyano or carboxyl; or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.Type: GrantFiled: May 31, 1995Date of Patent: July 16, 1996Assignee: American Home Products CorporationInventors: Madelene M. Antane, John A. Butera, Bradford H. Hirth, Schuyler A. Antane
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Patent number: 5529978Abstract: Certain N-acetonyl-substituted-amides of the formula: ##STR1## wherein A is a heterocycle, a phenylalkyl, a phenylalkoxy, naphthyl, cycloalkyl, alkoxyalkyl, alkyl, haloalkyl or alkenyl group; X, Y and Z are selected from the group consisting of hydrogen, halo, cyano, thiocyano, isothiocyano, methylsulfonyloxy, thio(C.sub.1 -C.sub.2)alkyl, (C.sub.1 -C.sub.2)alkoxy, carbamoyl, dithiocarbamoyl, hydroxy, azide, trifluoromethylcarboxy, (C.sub.1 -C.sub.4)alkylcarbonyloxy, phenylcarbonyloxy, phenoxy, thiophenyl, imidazolyl or triazolyl group as described herein; R.sup.1 and R.sup.2 are each independently a hydrogen atom or a (C.sub.1 -C.sub.6)alkyl group; and compositions containing these amides are fungicidally active, particularly against phytopathogenic fungi.Type: GrantFiled: May 3, 1994Date of Patent: June 25, 1996Assignee: Rohm and Haas CompanyInventor: Ashok K. Sharma
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Patent number: 5521179Abstract: The present invention relates to certain novel heterocyclic amides which are 1-pyridylacetamide compounds of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these heterocyclic amides, processes for preparing the heterocyclic amides, pharmaceutical compositions containing such heterocyclic amides and methods for their use.Type: GrantFiled: April 8, 1993Date of Patent: May 28, 1996Assignee: Zeneca LimitedInventors: Peter R. Bernstein, Andrew Shaw, Royston M. Thomas, Peter Warner, Donald J. Wolanin
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Patent number: 5514694Abstract: A novel class of peptide .alpha.-ketoamides useful for selectively inhibiting serine proteases, selectively inhibiting cysteine proteases, generally inhibiting all serine proteases, and generally inhibiting all cysteine proteases, having the formula Y--CO--AA.sup.2 --AA.sup.1 --CO--NH--X. Processes for the synthesis of peptidyl .alpha.-ketoamide derivatives.Type: GrantFiled: June 24, 1993Date of Patent: May 7, 1996Assignee: Georgia Tech Research CorpInventors: James C. Powers, Zhaozhao Li, Girish S. Patil, Der-Lun Chu
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Patent number: 5512581Abstract: The present invention relates to a compound of formulaW--X--Q--Y--CH(R.sup.1)--O--N.dbd.C(R.sup.2)--A--COMor a pharmaceutically acceptable salt thereof wherein W is optionally substituted aryl or heteroaryl; X is a valence bond, or methylene, divalent alkylene, alkenylene, alkynylene or alkyloxy; Q is a valence bond, or --O--, --S--, >NR.sup.4 or >NCOR.sup.5 ; Y is optionally substituted phenyl, biphenyl, naphthyl, tetrahydronaphthyl, indolyl, pyridyl, or benzo b!thienyl, thienyl, thiazolyl, or thiazolylphenyl; R.sup.1 is alkyl, cycloalkyl, alkoxyalkyl, aryl or arylalkyl, heteroaryl or heteroarylalkyl; R.sup.2 is hydrogen, alkyl or hydroxyalkyl; A is a valence bond or is selected from alkylene, alkenylene, alkynylene, cycloalkylene, phenylene, pyridylene, thienylene and furylene; and M is a pharmaceutically acceptable, metabolically cleavable group, --OR.sup.6, --NR.sup.6 R.sup.Type: GrantFiled: May 1, 1995Date of Patent: April 30, 1996Assignee: Abbott LaboratoriesInventors: Dee W. Brooks, Pramila Bhatia, Teodozyi Kolasa
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Patent number: 5508408Abstract: Compounds of formula I ##STR1## wherein R.sub.1 -R.sub.5, X, Ar and Y are as defined in the description, have valuable pharmaceutical properties and are especially effective as leukotriene antagonists. They are prepared in a manner known per se.Type: GrantFiled: August 10, 1994Date of Patent: April 16, 1996Assignee: Ciba-Geigy CorporationInventors: Andreas von Sprecher, Andreas Beck, Marc Gerspacher
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Patent number: 5506242Abstract: The invention relates to a method of inhibiting metalloellastase activity, of inhibiting the degradation of elastin, or of treating macrophage metalloelastase dependent conditions in mammals which comprises administering to a mammal in need thereof an effective macrophage metalloelastase inhibiting amount of a compound of formula I ##STR1## wherein Ar, R, R.sub.1 and R.sub.2 have meanings as defined, or of a pharmaceutically acceptable prodrug derivative thereof, or of a pharmaceutically acceptable salt thereof, or of pharmaceutical compositions comprising a said compound.Type: GrantFiled: June 24, 1994Date of Patent: April 9, 1996Assignee: Ciba-Geigy CorporationInventors: Lawrence J. MacPherson, David T. Parker, Arco Y. Jeng
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Patent number: 5506227Abstract: Compounds having the formula I: ##STR1## are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.Type: GrantFiled: April 13, 1992Date of Patent: April 9, 1996Assignee: Merck Frosst Canada, Inc.Inventors: Robert Zamboni, Daniel Guay, Jacques-Yves Gauthier
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Patent number: 5492915Abstract: This invention relates to compounds having selective LTB.sub.4 antagonist properties. Therapeutic compositions comprising said compounds and methods for the treatment of disorders involving LTB.sub.4 agonist-mediated activity utilizing said compositions wherein the compounds are described by the formula ##STR1## wherein R.sub.4, X, R, Y, R', Q, m and n are herein defined, and pharmaceutically acceptable salts thereof.Type: GrantFiled: October 6, 1994Date of Patent: February 20, 1996Assignee: Rhone-Poulenc Rorer S.A.Inventors: Norbert Dereu, Wolfram Hendel, Richard Labaudiniere
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Patent number: 5488149Abstract: A compound of the formula (I) or its pharmaceutically acceptable salt or ester: ##STR1## wherein each of the substituents are herein defined.Type: GrantFiled: June 6, 1995Date of Patent: January 30, 1996Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takashi Nomoto, Masahiro Hayashi, Jun Shibata, Yoshikazu Iwasawa, Morihiro Mitsuya, Yoshiaki Iida, Katsumasa Nonoshita, Yasufumi Nagata
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Patent number: 5461055Abstract: Compounds of the formula ##STR1## wherein R.sub.3, R.sub.4, J, K, Z, and Het are as set forth herein are described.The compounds of formula I are useful as agents in the treatment of fungal infections.Type: GrantFiled: June 3, 1994Date of Patent: October 24, 1995Assignee: Schering CorporationInventors: Alan B. Cooper, Anil K. Saksena, Raymond Lovey, Viyyoor Girijavallabhan, Ashit Ganguly
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Azacyclic compounds, processes for their preparation and pharmaceutical compositions containing them
Patent number: 5459270Type: GrantFiled: February 16, 1994Date of Patent: October 17, 1995Assignee: Merck Sharp & Dohme LimitedInventors: Brian Williams, Raymond Baker, Timothy Harrison, Christopher J. Swain -
Patent number: 5459149Abstract: The present Application discloses pesticidally active compounds of formula (I):Q(CH.sub.2).sub.a (O).sub.b Q.sup.1 CR.sup.2 =CR.sup.3 CR.sup.4 =CR.sup.5 CXNR.sup.1 R.sup.xor a salt or propesticide thereof, wherein Q is an optionally substituted aromatic monocyclic or fused bicyclic ring system in which at least one ring is aromatic, or Q is a dihalovinyl group or a group R.sup.6 --C=C--where R.sup.6 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halo or hydrogen; Q.sup.1 is a 1,2-cyclopropyl ring optionally substituted by one or more groups selected from C.sub.1-3 alkyl, halo, C.sub.1-3 haloalkyl, C.sub.2-3 alkynyl, or cyano; or Q.sup.1 is (CH.sub.2).sub.7 ; a=0 or 1; b=0 or 1; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 haloalkyl; X is oxygen or sulphur;R.sup.1 is phenyl optionally substituted by 1-5 substituents chosen from: a) C.sub.1-4 alkyl, C.sub.Type: GrantFiled: September 20, 1994Date of Patent: October 17, 1995Assignee: Roussel UclafInventors: John E. Robinson, George S. Cockerill
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Patent number: 5455258Abstract: Particularly the invention relates to the compounds of formula I ##STR1## (a) wherein Ar is carbocyclic or heterocyclic aryl;R is hydrogen, lower alkyl, carbocyclic aryl-lower alkyl, carbocyclic aryl, heterocyclic aryl, biaryl, biaryl-lower alkyl, heterocyclic aryl-lower alkyl, mono- or poly-halo-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, hydroxy-lower alkyl, acyloxy-lower alkyl, lower alkoxy-lower alkyl, lower alkyl-(thio, sulfinyl or sulfonyl)-lower alkyl, amino, mono- or di-lower alkylamino)-lower alkyl, acylamino-lower alkyl, (N-lower alkyl-piperazino or N-aryl-lower alkylpiperazino)-lower alkyl, or (morpholino, thiomorpholino, piperidino, pyrrolidino, piperidyl or N-lower alkylpiperidyl)-lower alkyl;R.sub.1 is hydrogen, lower alkyl, carbocyclic aryl-lower alkyl, carbocyclic aryl, heterocyclic aryl, biaryl, biaryl-lower alkyl, heterocyclic aryl-lower alkyl, mono- or poly-halo-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.3 -C.sub.Type: GrantFiled: January 6, 1993Date of Patent: October 3, 1995Assignee: Ciba-Geigy CorporationInventors: Lawrence J. MacPherson, David T. Parker
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Patent number: 5451605Abstract: Compounds of the formula ##STR1## where R.sub.1 -R.sub.5 are hydrogen, lower alkyl of 1-6 carbons, or halogen; A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.2, or CR.sub.7 OR.sub.13 O, where R.sub.7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R.sub.8 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.8 is phenyl or lower alkylphenyl, R.sub.9 and R.sub.10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R.sub.11 is lower alkyl, phenyl or lower alkylphenyl, R.sub.Type: GrantFiled: December 30, 1993Date of Patent: September 19, 1995Assignee: Allergan, Inc.Inventors: Roshantha A. Chandraratna, Richard L. Beard
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Patent number: 5434162Abstract: Compounds characterized as quinolinyl- or isoquinolinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension and are of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; X is selected from oxygen atom and methylene; G is a quinolinyl or isoquinolinyl group; R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; R.sub.2 is phenylmethyl; each of R.sub.3 and R.sub.5 is hydrido; R.sub.4 is--(CH.sub.2).sub.q --C--V;V is selected from hydrido and methyl; R.sub.6 is cyclohexylmethyl; R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; q is a number selected from zero through three, inclusive; and n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: September 13, 1993Date of Patent: July 18, 1995Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, Robert E. Manning
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Patent number: 5428171Abstract: Compounds having the formula: ##STR1## are antagonists of leukotrienes and inhibitors of their biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents.Type: GrantFiled: May 26, 1989Date of Patent: June 27, 1995Assignee: Merck Frosst Canada, Inc.Inventors: Robert N. Young, Robert Zamboni, Serge Leger
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Patent number: 5424442Abstract: A water-soluble methine compound represented by the following general formula (I): ##STR1## wherein Z.sub.1 and Z.sub.2, which may be the same or different, each represents a non-metallic atomic group required for forming a 5-membered or 6-membered nitrogen-containing heterocyclic ring; R.sub.1 and R.sub.2, which may be the same or different, each represents an alkyl group; Q.sub.1 and Q.sub.2 each represents an atomic group required, in combination, for forming a 4-thiazolidinone ring, a 5-thiazolidinone ring, a 4-imidazolidinone ring, a 4-oxazolidinone ring, a 5-oxazolidinone ring, a 5-imidazolidinone ring or a 4-dithiolanone ring; L.sub.1, L.sub.2, L.sub.3, L.sub.4 and L.sub.5, which may be the same or different, each represents a methine group; R represents a hydrogen atom, an alkyl group, an aryl group or a heterocyclic group; m represents 1 or 2; i and h each represents 0 or 1; l represents 1 or 2; and j and k each represents 0, 1, 2 or 3.Type: GrantFiled: June 18, 1993Date of Patent: June 13, 1995Assignee: Fuji Photo Film Co., Ltd.Inventors: Keizo Koya, Toshinao Ukai, Haruo Takei
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Patent number: 5420131Abstract: The present invention relates to new cyanomethylpyridine dervatives of formula I ##STR1## wherein Y represents N or CH; R.sub.1 represents hydrogen, fluoro, chloro, difluoro or dichloro; R.sub.2 represents hydrogen or C.sub.1-4 alkyl; n is 0 or 1; p is 0 or 1; A represents a covalent bond or a group of formula --CONHCH(Ar)--, --NHCH(Ar)--, --SO.sub.2 NHCH(Ar)--, --NHCONHCH(Ar)-- or --OCONHCH(Ar)--, and when p is 1, A can also represent --CH(Ar)NH--; and Ar represents phenyl or phenyl substituted with halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or trifluoromethyl. These compounds are PAF antagonist and/or 5-lipoxygenase inhibitors.Type: GrantFiled: March 23, 1994Date of Patent: May 30, 1995Assignee: J. Uriach & Cia, S.A.Inventors: Elena Carceller, Pere J. Jimenez, Carmen Almansa, Javier Bartroli
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Patent number: 5407945Abstract: The invention concerns a cyclic ether derivative of the formula I ##STR1## wherein Ar.sup.1 is optionally substituted phenyl, naphthyl or a 9- or 10-membered bicyclic heterocyclic moiety;A.sup.1 is a direct link to X.sup.1 or (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl, sulphonyl or imino;Ar.sup.2 is optionally substituted phenylene or pyridylene;R.sup.1 includes hydrogen, (1-4C)alkyl, (1-4C)alkoxycarbonyl and (1-4C)alkylthio; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 5 to 7 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl;or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.Type: GrantFiled: July 30, 1993Date of Patent: April 18, 1995Assignees: Imperial Chemical Industries, Inc., ICI-PharmaInventors: Pierre A. R. Bruneau, Robert I. Dowell, David Waterson
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Patent number: 5399565Abstract: Novel substituted pyrazolidinones have been found to exhibit significant binding to cholecystokinin (CCK) receptors and gastrin receptors in the brain and/or peripheral sites such as the pancreas, stomach, and ileum. The pyrazolidinones are CCK and gastrin receptor antagonists and find therapeutic application in the treatment of gastrointestinal disorders, central nervous system disorders and for appetite regulation in warm-blood vertebrates. Pharmaceutical formulations for such indications are described.Type: GrantFiled: November 12, 1993Date of Patent: March 21, 1995Assignee: Eli Lilly and CompanyInventors: Beverley Greenwood, David R. Helton, J. Jeffry Howbert, Steven J. Mitan, Kurt Rasmussen
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Patent number: 5399703Abstract: A compound of the formula [I] useful for treating allergic symptoms, cardiovascular disorders, cerebrovascular disorders, inflammation or other conditions mediated by SRS-A in humans and animals is disclosed.Type: GrantFiled: February 4, 1993Date of Patent: March 21, 1995Assignee: Nippon Shinyaku Company, LimitedInventors: Yoshihiko Yoshimoto, Shoji Yasufuku, Yoshihiko Makita, Kichiro Inoue, Kei Nakanouchi
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Patent number: 5395849Abstract: The present invention provides novel antitumor agents which are hybrid molecules consisting of a cyclic enediyne unit attached to a DNA-binding unit via a linker unit, and having the general formula (I)D--(OCH.sub.2).sub.m --O--(CH.sub.2).sub.n --Ar--Y--CONH--B(I)wherein D is a cyclic enediyne; B is a residue capable of binding to the minor groove of DNA; n is 0 and m is 1, is or n is 1 and m is 0 or 1; Ar is an aromatic residue selected from the group consisting of phenyl, naphthyl, pyridyl, quinolinyl and indolyl; and Y is a direct bond, --CH.sub.2 -- or --CH.dbd.CH--; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 5, 1993Date of Patent: March 7, 1995Assignee: Bristol-Myers Squibb CompanyInventors: Mark D. Wittman, David Langley, John F. Kadow
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Patent number: 5393782Abstract: Thioamides of the formula I ##STR1## where A, B, R' are hydrogen, cyano, alkyl, alkoxy or halogen,X is .dbd.CHCH.sub.3 or .dbd.N--OCH.sub.3,R.sup.1, R.sup.2 are hydrogen or alkyl,Y is a group ##STR2## and R is hydrogen, unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl or unsubstituted or substituted hetaryl,and pesticides containing these compounds.Type: GrantFiled: November 29, 1993Date of Patent: February 28, 1995Assignee: BASF AktiengesellschaftInventors: Horst Wingert, Hubert Sauter, Herbert Bayer, Klaus Oberdorf, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5391747Abstract: A (quinolin-2-yl-methoxy) phenylacyl-sulphonamide or -cyanamide of the formula ##STR1## and physiologically acceptable salts thereof. The (quinolin-2-yl-methoxy)phenylacylsulphonamide or -cyanamide is useful as an active compound in medicaments, particularly as a lipoxygenase inhibitor.Type: GrantFiled: September 23, 1991Date of Patent: February 21, 1995Assignee: Bayer AktiengesellschaftInventors: Siegfried Raddatz, Klaus-Helmut Mohrs, Romanis Fruchtmann, Christian Kohlsdorfer, Pia Theisen-Popp, Reiner Muller-Peddinghaus
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Patent number: 5389649Abstract: Oxathiane derivatives of formula ##STR1## in which R represents alkyl and A represents optionally substituted phenyl or a heteroaromatic group containing 1 or 2 nitrogen atoms optionally substituted by alkyl, alkoxy or halogen, and salts thereof possess pharmacological activity and are also useful in inhibiting head hair loss.Type: GrantFiled: July 20, 1992Date of Patent: February 14, 1995Assignee: Rhone-Poulenc Rorer LimitedInventors: Iain M. McLay, Roger J. A. Walsh
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Patent number: 5384318Abstract: Compounds of the formula ##STR1## and pharmaceutical compositions comprising them, wherein R.sup.1, R.sup.2, R.sup.3, W, X and Z are as defined below. The compounds are inhibitors of 5-lipoxygenase enzyme and antagonists of leukotriene B4, leukotriene C4, leukotriene D4 and leukotriene E4.Type: GrantFiled: February 21, 1992Date of Patent: January 24, 1995Assignee: Pfizer Inc.Inventors: James F. Eggler, Anthony Marfat, Lawrence S. Melvin, Jr., Hiroko Masamune
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Patent number: 5380852Abstract: Disclosed are compounds of the formula (I): ##STR1## The substituents are disclosed in the specification. The compounds are herbicidal safenets. Accordingly, processes for the preparation and use of the compounds of formula (I) are also disclosed.Type: GrantFiled: December 19, 1991Date of Patent: January 10, 1995Assignee: Hoechst AktiengesellschaftInventors: Rainer Schutze, Heinz-Josef Loher, Frank Ziemer, Klaus Bauer, Hermann Bieringer
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Patent number: 5360811Abstract: Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols of the formulaRCH(OR.sup.1)CH(NR.sup.2 R.sup.3)R.sup.4 or RCH.sub.2 CR.sup.35 (NR.sup.2 R.sup.3)R.sup.4wherein R is ##STR1## wherein R.sup.5 is CH.sub.3 (CH.sub.2).sub.m C.tbd.C, CH.sub.3 (CH.sub.2).sub.m CH.dbd.CH,CH.sub.3 (CH.sub.2).sub.m CH.sub.2 CH.sub.2, ##STR2## wherein m is 3 to 15, n is 0 to 12, and W and X are independently hydrogen, hydroxy, alkyl, alkoxy, halogen, or trifluoromethyl, ##STR3## wherein R.sup.23 loweralkyl; Z is S, O, or C.dbd.O; and A is S or O; R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.35 and R.sup.40 are as defined in the specification, the optical isomers thereof, or the pharmaceutically acceptable salts thereof, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth are disclosed.Type: GrantFiled: September 10, 1992Date of Patent: November 1, 1994Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: John J. Tegeler, Barbara S. Rauckman, Russell R. L. Hamer, Brian S. Freed, Gregory H. Merriman
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Patent number: 5358955Abstract: The present invention relates to a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein W is selected from optionally substituted pyridyl, naphthyl, and quinolyl; which inhibits lipoxygenase enzyme activity and leukotriene biosynthesis and is useful in the treatment of inflammatory disease states; also disclosed are leukotriene biosynthesis inhibiting compositions and a method for inhibiting lipoxygenase enzyme activity and leukotriene biosynthesis.Type: GrantFiled: June 2, 1993Date of Patent: October 25, 1994Assignee: Abbott LaboratoriesInventors: Dee W. Brooks, Teodozy J. Kolasa
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Patent number: 5350754Abstract: The invention concerns a heterocyclic cycloalkane of the formula I ##STR1## wherein Q is an optionally substituted 6-membered monocyclic or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen atoms;A is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene;X is oxy, thio, sulphinyl, sulphonyl or imino;Ar is phenylene which may optionally bear one or two substituents orAr is an optionally substituted 6-membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 is hydrogen, (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted benzoyl;and R.sup.2 and R.sup.3 together form a (3-6C)alkylene group which, together with the carbon atom to which R.sup.2 and R.sup.3 are attached, defines a ring having 4 to 7 ring atoms, and which ring may bear one or two substituents; or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.Type: GrantFiled: March 1, 1993Date of Patent: September 27, 1994Assignees: Zeneca Limited, ICI PharmaInventors: Graham C. Crawley, Jean-Marc M. M. Girodeau
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Patent number: 5348976Abstract: The present invention provides a condensed heterocyclic derivative represented by a formula: ##STR1## wherein R.sup.1 represents a lower alkyl group, an alkenyl group, or the like, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 independently represent a hydrogen atom, a lower alkyl, or the like, W is represented by --OC(O)--, --SC(O)--, or the like, and Z represents a 2-indolyl group or the like. The present invention also provides an agricultural or horticultural fungicide which comprises an amount of the condensed derivative known to be effective as a fungicide. The agricultural or horticultural fungicide according to the present invention exhibits a superior control effect for downy mildew and late blight, without harm to nonfungal, photosynthesizing plants.Type: GrantFiled: September 7, 1993Date of Patent: September 20, 1994Assignees: Kumai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Masaru Shibata, Shigekazu Ito, Jun-etsu Sakai, Shigeru Hayashi
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Patent number: 5326770Abstract: This invention relates to monoamine oxidase-B (MAO-B) inhibitory 5-substituted 2,4-thiazolidinediones, such as Formula I, to pharmaceutical compositions thereof, process of preparation, and methods of use in mammals to treat cognitive disorders, neurological dysfunction, and/or mood disturbances such as, but not limited to degenerative nervous system diseases.Type: GrantFiled: July 17, 1992Date of Patent: July 5, 1994Assignee: The Du Pont Merck Pharmaceutical CompanyInventor: Wendell W. Wilkerson
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Patent number: 5324839Abstract: Novel bicyclic compounds in all possible racemic, enantiomeric and diasteroisomeric forms of the formula ##STR1## having antagonistic properties for angiotensin II receptors and novel intermediates and process for their preparation.Type: GrantFiled: February 6, 1992Date of Patent: June 28, 1994Assignee: Roussel-UclafInventors: Francois Clemence, Michel Fortin, Jean-Luc Haesslein
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Patent number: 5310743Abstract: 1-Acylpiperidine compound of the formula I ##STR1## in which R.sub.1 is an optionally substituted aralkyl, aryloxyalkyl, heteroaralkyl, aroyl, heteroaroyl, cycloalkylcarbonyl, aralkanoyl, heteroarylalkanoyl, aralkoxycarbonyl or arylcarbamoyl radical or the acyl radical of an .alpha.-amino acid which is optionally N-substituted by lower alkanoyl or carbamoyl-lower-alkanoyl, R.sub.2 is cycloalkyl or an optionally substituted aryl or heteroaryl radical, R.sub.3 is hydrogen, alkyl, carbamoyl or an alkanoyl or alkenoyl radical which is optionally substituted by carboxyl or esterified or amidated carboxyl, R.sub.4 is an optionally substituted aryl or optionally partially hydrogenated heteroaryl radical, X.sub.1 is methylene, ethylene, a direct linkage, an optionally ketalised carbonyl group or an optionally etherified hydroxymethylene group, X.sub.2 is alkylene, carbonyl or a direct linkage, and X.sub.Type: GrantFiled: August 11, 1992Date of Patent: May 10, 1994Assignee: Ciba-Geigy Corp.Inventors: Walter Schilling, Silvio Ofner, Siem J. Veenstra