Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Acyclic Nitrogen Patents (Class 546/265)
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Patent number: 5962479Abstract: Corticotropin-releasing factor (CRF) antagonists having formulae (I), (II) or (III) wherein the dashed lines, A, B, Y, Z, G, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.16 and R.sub.17 are as defined in the description, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment of CNS and stress-related disorders.Type: GrantFiled: December 6, 1996Date of Patent: October 5, 1999Assignee: Pfizer Inc.Inventor: Yuhpyng Liang Chen
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Patent number: 5948778Abstract: This invention relates to novel statone antiviral analogs, to the processes and intermediates useful for their preparation and to their use as antiviral agents.Type: GrantFiled: May 19, 1998Date of Patent: September 7, 1999Assignee: Merrel Pharmaceuticals Inc.Inventors: Viviane Van Dorsselaer, Daniel Schirlin, Celine Tarnus
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Patent number: 5932734Abstract: Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein: G represents a group of the formula ##STR2## where R.sub.a and R.sub.b represent hydrogen, or organic or inorganic substituents;A is an optionally substituted alkylene;R.sub.1, R.sub.2, R.sub.3, R.sub.4 represent organic or inorganic substituents;R.sub.5 is hydrogen or lower alkyl;R.sub.6 and R.sub.7 independently represent hydrogen, lower alkyl; or together form a ring of 5-8 members;Z is nitrogen or carbon; andW is optionally substituted aryl or heteroaryl. Compounds of the present invention demonstrate high affinity and selectivity in binding to the D.sub.3 receptor subtype.Type: GrantFiled: August 7, 1997Date of Patent: August 3, 1999Assignee: Neurogen CorporationInventors: Jun Yuan, Xi Chen
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Patent number: 5874584Abstract: An ion-sensitive calix(4)arene compound having the formula A.sup.2 +B.sup.2 - wherein A represents a cation capable of forming a receptor-substrate complex with an anion, and B represents sulfate, nitrate or borate, characterized in that the cation is an anion receptor represented by the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each independently a substituted or unsubstituted alkyl group or a substituted or unsubstituted aryl group wherein substituents are selected from alkyl C(O)NH--, aryl C(O)NH--, alkoxy, aryloxy, alkoxycarbonyl, aryloxycarbonyl, alkylsulfonamido, arylsulfonamido, alkylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, cyano and nitro;R.sup.5 and R.sup.6 are each independently H or a lower alkyl group having from 1 to 4 carbon atoms, or R.sup.3 and R.sup.4 taken together represent an ethylene bridging group; and,n is 0 or 1.Type: GrantFiled: November 5, 1997Date of Patent: February 23, 1999Assignee: Eastman Kodak CompanyInventors: Trevor John Wear, Christopher Peter Moore, Alistair J. Goulden, Paul D. Beer, Nicholas C. Fletcher
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Patent number: 5827827Abstract: A series of novel oxirane derivatives, which are useful for inhibiting HIV are disclosed. Particularly of value are peptidomimetic compounds, containing a terminal epoxide group on a peptide or psuedopeptide backbone, which are believed to inhibit HIV protease by extruding enzyme-bound water molecules from the active site of the enzyme.Type: GrantFiled: June 20, 1996Date of Patent: October 27, 1998Assignee: The Scripps Research InstituteInventors: Kim D. Janda, Peter Wirsching
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Patent number: 5801175Abstract: Novel compounds of Formula ##STR1## are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering a compound of the above formula to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.Type: GrantFiled: September 13, 1996Date of Patent: September 1, 1998Assignees: Schering Corporation, Pharmacopeia, Inc.Inventors: Adriano Afonso, John J. Baldwin, Ronald J. Doll, Ge Li, Alan K. Mallams, F. George Njoroge, Dinanath F. Rane, John C. Reader, Randall R. Rossman
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Patent number: 5767085Abstract: Compounds of the formula A--B--C--D(--E).sub.p are used to stimulate the release of growth hormone from the pituitary.Type: GrantFiled: June 6, 1995Date of Patent: June 16, 1998Assignee: Novo Nordisk A/SInventors: Nils Langeland Johansen, Jesper Lau, Kjeld Madsen, Behrend Friedrich Lundt, Henning Th.o slashed.gersen, Birgit Sehested Hansen, Bernd Peschke
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Patent number: 5760246Abstract: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure ##STR1## including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0, 1 or 2;R.sup.x is H, alkyl, aryl or halogen;A is(1) a bond;(2) --O--; or(3) ##STR2## B is: ##STR3## and wherein L.sup.2, L.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.3', R.sup.3a, R.sup.3b, R.sup.4, R.sup.4', R.sup.5, X, ##STR4## are as defined herein.Type: GrantFiled: December 17, 1996Date of Patent: June 2, 1998Inventors: Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Jeffrey A. Robl, William A. Slusarchyk, Richard B. Sulsky, Joseph A. Tino
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Patent number: 5760231Abstract: An ion-sensitive calix(4)arene compound having the formula A.sup.2 +B.sup.2- wherein A represents a cation capable of forming a receptor-substrate complex with an anion, and B represents sulfate, nitrate or borate, characterized in that the cation is an anion receptor represented by the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each independently a substituted or unsubstituted alkyl group or a substituted or unsubstituted aryl group wherein substituents are selected from alkyl C(O)NH--, aryl C(O)NH--, alkoxy, aryloxy, alkoxycarbonyl, aryloxycarbonyl, alkylsulfonamido, arylsulfonamido, alkylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, cyano and nitro;R.sup.5 and R.sup.6 are each independently H or a lower alkyl group having from 1 to 4 carbon atoms, or R.sup.3 and R.sup.4 taken together represent an ethylene bridging group; and,n is 0 or 1.Type: GrantFiled: October 22, 1996Date of Patent: June 2, 1998Assignee: Eastman Kodak CompanyInventors: Trevor John Wear, Christopher Peter Moore, Alistair J. Goulden, Paul D. Beer, Nicholas C. Fletcher
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Patent number: 5747505Abstract: The heterocyclic aryl-, alkyl- and cycloalklacetamides are prepared by reacting the appropriately substituted acetic acids with amines, if appropriate in complexed form. The heterocyclic aryl-, alkyl- and cycloalkylacetamides can be used as active compounds in medicaments, in particular in antiatherosclerotic medicaments.Type: GrantFiled: September 20, 1996Date of Patent: May 5, 1998Assignee: Bayer AktiengesellschaftInventors: Richard Connell, Siegfried Goldmann, Ulrich Muller, Martin Beuck, Hilmar Bischoff, Dirk Denzer, Rudi Grutzmann, Stefan Wohlfeil
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Patent number: 5733931Abstract: The present invention provides a cyclohexanediurea derivative, inclusive of its salt, represented by the following formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and they each represent a straight-chain or branched alkyl group having at least 3 carbons, a cycloalkyl group, a cycloalkyl group having a bridge head, a furyl group, a furyl lower alkyl group or an aralkyl group, A.sub.1 and A.sub.2 are the same or different and they each represent a phenyl, pyridyl, quinolyl, isoquinolyl or indolyl group which may have substituents; a process for production thereof; an intermediate thereof; pharmaceutical use, a method for treatment and use thereof.Type: GrantFiled: March 8, 1996Date of Patent: March 31, 1998Assignee: Nissin Food Products Co., Ltd.Inventors: Toshihiro Yamada, Yoichi Nobuhara, Ichinari Takagi, Shiho Furumoto, Kazuhiro Kobayashi, Kiyohito Ikemoto
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Patent number: 5723646Abstract: There are described new amino acid amide derivatives, some of which are known, of the formula (I) ##STR1## in which R.sup.1 to R.sup.8 have the meaning given in the description, and a process for their preparation. The amino acid amide derivatives of the formula (I) are used for the preparation of pesticides.Type: GrantFiled: January 16, 1992Date of Patent: March 3, 1998Assignee: Bayer AktiengesellschaftInventors: Thomas Seitz, Heinz-Wilhelm Dehne
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Patent number: 5712294Abstract: A compound selected from those of formula (I): ##STR1## where m is equal to 0 or 1andHet, A, X, R, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and the ring ##STR2## are defined in the description, and a medicinal product comprising the same for treating an inflammatory disorder.Type: GrantFiled: May 25, 1995Date of Patent: January 27, 1998Assignee: Adir Et CompagnieInventors: Jean-Michel Robert, Odile Rideau, Sylvie Robert-Piessard, Jacqueline Courant, Guillaume Le Baut, Daniel-Henri Caignard, Pierre Renard, Gerard Adam
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Patent number: 5672615Abstract: Disclosed are the compounds of formula I ##STR1## wherein R and R.sub.1 together with the chain to which they are attached or R.sub.1 and R.sub.2 together with the carbon atom to which they are attached form a ring; pharmaceutically acceptable prodrug derivatives and pharmaceutically salts thereof; methods of 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: March 11, 1996Date of Patent: September 30, 1997Assignee: Novartis CorporationInventors: Lawrence J. MacPherson, David Thomas Parker
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Patent number: 5658907Abstract: Treatment of AIDS, inhibition of the replication of HIV and related viruses thereof, and formulations using thiourea derivative compounds or salts thereof is disclosed. Also disclosed are novel thiourea derivative compounds.Type: GrantFiled: May 31, 1995Date of Patent: August 19, 1997Assignee: Medivir A/BInventors: John M. Morin, Jr., Robert J. Ternansky, Rolf Noreen, Peter Tomas Lind
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Patent number: 5659033Abstract: Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein: G represents a group of the formula ##STR2## where R.sub.a and R.sub.b represent hydrogen, or organic or inorganic substituents;A is an optionally substituted alkylene;R.sub.1, R.sub.2, R.sub.3, R.sub.4 represent organic or inorganic substituents;R.sub.5 is hydrogen or lower alkyl;R.sub.6 and R.sub.7 independently represent hydrogen, lower alkyl; or together form a ring of 5-8 members;Z is nitrogen or carbon; andW is optionally substituted aryl or heteroaryl.Compounds of the present invention demonstrate high affinity and selectivity in binding to the D.sub.3 receptor subtype.Type: GrantFiled: September 13, 1995Date of Patent: August 19, 1997Assignee: Neurogen CorporationInventors: Jun Yuan, Xi Chen
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Patent number: 5618826Abstract: Compounds of the formula ##STR1## wherein the variables are defined in the specification; and acid addition and quaternary ammonium salts of formula (I) compounds are described. The compounds and their salts are soft anticholinergic/antisecretory agents especially useful as mydriatics and as antiperspirants.Type: GrantFiled: May 30, 1995Date of Patent: April 8, 1997Assignee: University of FloridaInventors: Richard H. Hammer, Nicholas S. Bodor
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Patent number: 5616776Abstract: Intermediates and processes are disclosed which are useful for the preparation of a substantially pure compound of the formula: ##STR1## wherein R.sub.6 and R.sub.7 are each hydrogen or R.sub.6 and R.sub.7 are independently selected from ##STR2## wherein R.sub.a and R.sub.b are independently selected from hydrogen, loweralkyl and phenyl and R.sub.c, R.sub.d and R.sub.e are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and ##STR3## wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; orR.sub.6 is as defined above and R.sub.7 is R.sub.7a OC(O)-- wherein R.sub.7a is loweralkyl or benzyl; orR.sub.6 and R.sub.7 taken together with the nitrogen atom to which they are bonded are ##STR4## wherein R.sub.f, R.sub.g, R.sub.h and R.sub.i are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl and R.sub.Type: GrantFiled: April 7, 1995Date of Patent: April 1, 1997Assignee: Abbott LaboratoriesInventors: Timothy L. Stuk, Anthony R. Haight, Francis A. J. Kerdesky, M. Robert Leanna, Howard E. Morton, Timothy A. Robbins, David Scarpetti, Jien-Heh J. Tien
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Patent number: 5614634Abstract: Leukotriene-B.sub.4 analogs of formula I ##STR1## in which R.sup.1 means radical COOR.sup.2 with R.sup.2 meaning a hydrogen atom or a (C.sub.1 -C.sub.4)-alkyl group or R.sup.1 means radical CH.sub.2 OH,B means an alkylene group with 1-3 C atoms in the chain, a radical ##STR2## or a radical ##STR3## with R.sup.3 meaning a hydrogen atom, a carboxy or methoxycarbonyl group, A means groups ##STR4## --NH--CO--, --CO--NH--, --OCH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, --COCH.sub.2 -- or --CHOH--CH.sub.2 --,X means N or CH,D means groups or ##STR5## and . . . . . means a single or double bond, as well as optionally their salts with physiologically harmless bases, process for their production and their pharmaceutical use.Type: GrantFiled: June 5, 1995Date of Patent: March 25, 1997Assignee: Schering AktiengesellschaftInventors: Josef Heindl, Werner Skuballa, Bernd Buchmann, Wolfgang Frohlich, Roland Ekerdt, Claudia Giesen
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Patent number: 5614548Abstract: Quaternary amine-containing ether lipid analogs of the formulaR.sub.1 --X--R.sub.2 --N.sup.+ (R.sub.3) (R.sub.4) (R.sub.5) Z.sup.-are disclosed. R.sub.1 represents a hydrophobic group and R.sub.2 represents the backbone of the molecule, with the quaternary amine being linked directly to the backbone. Pharmaceutical compositions including these compounds and methods of combating tumors with these compounds are disclosed. Also disclosed is a method of combating viral infections with both these compounds and ET-18-OMe and its analogs.Type: GrantFiled: September 8, 1994Date of Patent: March 25, 1997Assignee: Wake Forest UniversityInventors: Claude Piantadosi, Khalid S. Ishaq, Canio J. Marasco, Jr., Larry W. Daniel, Louis S. Kucera, Edward J. Modest, Barry P. Goz
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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: 5545608Abstract: Pyrazole-glycolic acid amides of the following formula (1) (in which R.sup.1 to R.sup.5 each represent a hydrogen atom or a substituent having a broad definition), and herbicides containing them. The compounds have a high herbicidal effect against paddy weeds, especially Echinochloa crus-galli, while highly safe for paddy rice plants.Type: GrantFiled: April 25, 1994Date of Patent: August 13, 1996Assignee: Nissan Chemical Industries, Ltd.Inventors: Katsushi Morimoto, Masatoshi Ohnari, Tsutomu Nawamaki, Shigeomi Watanabe, Kimihiro Ishikawa
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Patent number: 5519132Abstract: Compounds of Formula I have been shown to enhance the release of the neurotransmitter acetylcholine, and thus may be useful as chemical intermediates and as pharmacological agents in the treatment of diseases of man, such as in Alzheimer's Disease and other conditions involving learning and cognition, where subnormal levels of this neurochemical are found.Type: GrantFiled: February 21, 1995Date of Patent: May 21, 1996Assignee: The Du Pont Merck Pharmaceutical CompanyInventor: Christopher A. Teleha
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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: 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: 5463124Abstract: Process for the diastereoselective reductive pinacol coupling of homochiral .alpha.-aminoaldehydesA process for the preparation of optically pure symmetrical compounds of the formula I ##STR1## is described in which R.sup.1, R.sup.2 and R.sup.3 are explained in the description, with simultaneous control of the four centers of chirality marked by *.Type: GrantFiled: June 22, 1994Date of Patent: October 31, 1995Assignee: Hoechst AktiengesellschaftInventors: Detlef Jacobi, Heiner Jendralla, Bernhard Kammermeier
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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: 5430155Abstract: There are provided novel 1,4 Diamine 2,3 Dihydroxybutanes useful as antiviral agents, pharmaceutical compositions containing them and processes for preparing such compounds.Type: GrantFiled: December 17, 1993Date of Patent: July 4, 1995Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Prabhakar K. Jadhav, Lawrence R. McGee, Ashok Shenvi, Carl N. Hodge
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Patent number: 5416117Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.Type: GrantFiled: February 28, 1994Date of Patent: May 16, 1995Assignee: Mitsubishi Kasei CorporationInventors: Ryoichi Ando, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
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Patent number: 5384425Abstract: Diurea derivatives are provided which can be represented by the following general formula and salts thereof: ##STR1## wherein, R.sup.1 and R.sup.2 are the same or different, and each represents C.sup.1 -10 alkyl group, a C.sup.3 -18 cycloalkyl group, or a lower alkyl group substituted by cycloalkyl radical(s);R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different, and each represents a hydrogen atom, a lower alkyl group, a cycloalkyl group, hydrocarbyl aralkyl group, a pyridyl group, or an unsubstituted or substituted phenyl group, the substituents of the phenyl group being selected from a group consisting of lower alkyl radical, halogen atom-substituted lower alkyl radical, halogen atom, nitro radical, amino radical, mono- or di-lower alkylamino radical, lower acylamino radical, hydroxyl radical, lower alkoxy radical and lower acyloxy radical;X represents an oxygen atom or a sulfur atom, and n.sup.1 and n.sup.2 represent an integer of 1 to 6; and wherein at least one of R.sup.3 -R.sup.Type: GrantFiled: October 7, 1993Date of Patent: January 24, 1995Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Noriki Ito, Tomoyuki Yasunaga, Yuichi Iizumi, Tomio Araki
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Patent number: 5364853Abstract: Thioformamide compounds of formula (I) are disclosed in which R is alkyl, Y is methylene, ethylene or a direct bond, A is optionally substituted phenyl or pyridyl, R.sup.1 is hydrogen and R.sup.2 is N-alkylsulphonyl-, N-phenylsulphonyl-N'-alkylamidino or an arylsulphonyl group; R.sup.1 and R.sup.2 may both independently represent alkyl- or arylsulphonyl groups.Type: GrantFiled: August 20, 1992Date of Patent: November 15, 1994Assignee: Rhone-Poulenc Rorer LimitedInventors: Malcolm N. Palfreyman, Nigel Vicker
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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: 5354866Abstract: A retroviral protease inhibiting compound of the formula A--X--B is disclosed. Also disclosed are a composition and method for inhibiting a retroviral protease and for treating an HIV infection. Also disclosed are processes and intermediates useful for the preparation of the retroviral protease inhibitors.Type: GrantFiled: September 14, 1993Date of Patent: October 11, 1994Assignee: Abbott LaboratoriesInventors: Dale J. Kempf, Daniel W. Norbeck, Lynn M. Codacovi, Jacob J. Plattner, Hing L. Sham, Chen Zhao
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Patent number: 5344836Abstract: A fused benzenoxyacetic acid derivative of the formula (I): ##STR1## and salts thereof possess an agonistic on PGI.sub.2 receptor, so it is useful for prevention and/or treatment of thrombosis, arteriosclerosis, ischemic heart diseases, gastric ulcer and hypertention.Type: GrantFiled: November 5, 1992Date of Patent: September 6, 1994Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Nobuyuki Hamanaka, Kanji Takahashi, Hidekado Tokumoto
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Patent number: 5328909Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.Type: GrantFiled: June 25, 1992Date of Patent: July 12, 1994Assignee: Mitsubishi Kasei CorporationInventors: Ryoichi Ando, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
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Patent number: 5326759Abstract: Novel 9-amino-7-(substituted amino)-6-demethyl-6-deoxytetracyclines having activity against a wide spectrum of organisms including organisms which are resistant to tetracyclines are disclosed. Also disclosed are intermediates and methods for making the novel compounds of the present invention.Type: GrantFiled: November 1, 1993Date of Patent: July 5, 1994Assignee: American Cyanamid CompanyInventors: Joseph J. Hlavka, Phaik-Eng Sum, Yakov Gluzman, Ving J. Lee
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Patent number: 5318989Abstract: The present invention relates to a novel and efficient process for the preparation of 8-hydroxybicyclo[7.3.1]tridec-4-ene-2,6-diyne ring system which is part of the aglycone of esperemicin and to novel cytotoxic antitumor agents having said bicyclic ring system. The present invention also provides a method for treating mammalian malignant tumors by administering to an animal in need of such treatment an antitumor effective amount of a compound of the present invention.Type: GrantFiled: December 18, 1992Date of Patent: June 7, 1994Assignee: Bristol-Myers Squibb CompanyInventors: John F. Kadow, Mark D. Wittman
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Patent number: 5294720Abstract: There are provided novel 1,4 Diamine 2,3 Dihydroxybutanes useful as antiviral agents, pharmaceutical compositions containing them and processes for preparing such compounds.Type: GrantFiled: May 31, 1991Date of Patent: March 15, 1994Assignee: The DuPont Merck Pharmaceutical Co.Inventors: Prabhakar K. Jadhav, Lawrence R. McGee, Ashok Shenvi, Carl N. Hodge
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Patent number: 5227492Abstract: Diurea derivatives are provided which can be represented by the following general formula and salts thereof: ##STR1## Illustrative derivatives include 1,3-bis[[1-cycloheptyl-3-(3-pyridyl)ureido]-methyl]benzene, 1,3-bis[[1-cycloheptyl-3-(2-pyridyl)ureido]-methyl]benzene, and 1,3-bis[[1-cycloheptyl-3-(4-pyridyl)ureido]-methyl]benzene.The above compounds inhibit acyl-coenzyme A cholesterol acyltransferase (ACAT enzyme), and thereby control the accumulation of cholesterol ester to the smooth muscle of arterial wall in the blood vessel.Type: GrantFiled: June 30, 1992Date of Patent: July 13, 1993Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Noriki Ito, Tomoyuki Yasunaga, Yuichi Iizumi, Tomio Araki
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Patent number: 5216169Abstract: A 3-hydroxypyridineazomethine dye represented by general formula (I) ##STR1## wherein R.sub.1 represents an aliphatic group, an aromatic group, or a heterocyclic group; R.sub.2 represents an aliphatic group, an aromatic group, a heterocyclic group, an alkoxy group, an aryloxy group, an alkenyloxy group, an amino group, an acyl group, an ester group, an amido group, a carbamoylamino group, a sulfamoylamino group, a sulfamido group, an imido group, a ureido group, an aliphatic or an aromatic sulfonyl group, an aliphatic or an aromatic thio group, a hydroxyl group, a cyano group, a carboxy group, or a halogen atom; R.sub.3 represents an aryl group; Y represents a bivalent linking group containing at least one of amide bond and ester bond; n represents 0, 1 or 2; where n is 2, the two R.sub.2 groups may be the same group or atom or may be mutually different groups or atoms, or the two R.sub.2 groups may form a ring; where n is 1 or more, R.sub.1 and R.sub.2 may form a ring; and at least one of R.sub.1 and R.sub.Type: GrantFiled: September 18, 1990Date of Patent: June 1, 1993Assignee: Fuji Photo Film Co., Ltd.Inventor: Shigeru Yamazaki
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Patent number: 5204359Abstract: Insecticidally active nitro compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, cyano or alkyl,R.sup.2 is hydrogen or an organic radical,R.sup.3 is ##STR2## R.sup.4 is an organic radical, R.sup.5 and R.sup.6 are hydrogen or organic radicals,Y is CH or N, andZ is an optionally substituted 5- or 6-membered heterocyclic group,with certain conditions and exceptions.Type: GrantFiled: September 11, 1991Date of Patent: April 20, 1993Assignee: Nihon Bayer Agrochem K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Koichi Moriya, Yumi Hattori, Ikuro Honda, Katsuhiko Shibuya
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Patent number: 5185375Abstract: Therapeutically useful thioformamide derivatives of the formula: ##STR1## wherein R represents alkyl, Ar represents optionally substituted phenyl group, Y represents ethylene, methylene or a valency bond, and X represents carbonyl, hydroxymethylene, >C.dbd.NOR.sup.1, >C.dbd.NN(R.sup.1).sub.2 or >C.dbd.NN(R.sup.1)CON(R.sup.1).sub.2 in which R.sup.1 represents hydrogen or optionally substituted alkyl, benzyl, phenethyl, 1-naphthylmethyl, 2-naphthylmethyl or pyrid-3-ylmethyl or two R.sup.1 substituents on the same nitrogen atom may together form optionally substituted alkylene, and salts thereof, processes for their preparation and compositions containing them are described.Type: GrantFiled: March 30, 1990Date of Patent: February 9, 1993Assignee: May & Baker LimitedInventors: David C. Cook, Terance W. Hart, Iain M. McLay, Malcolm N. Palfreyman, Roger J. A. Walsh
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Patent number: 5177089Abstract: A butenoic or propenoic acid derivative having the following formula in which G is an aryl or a heterocyclic ring, R11 and R12 are hydroben or an alkyl, X is sulfur or oxygen, R2 and R3 are hydrogen, an substituent such as an alkyl and J is pyridyl or phenyl having substituents and a heterocyclic ring may be formed between R2, R3 and J is provided here and is useful in the pharmacological field.Type: GrantFiled: July 25, 1990Date of Patent: January 5, 1993Assignee: Eisai Co., Ltd.Inventors: Norio Minami, Fumihiro Ozaki, Keiji Ishibashi, Yasuhiro Kabasawa, Megumi Ikemori, Toshiaki Ogawa, Takanori Kawamura
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Patent number: 5153199Abstract: Compounds having the general formula (I): ##STR1## and optical isomers thereof, wherein X is oxygen or sulphur; R.sup.1 is halogen, C.sub.1-4 alkoxy or C.sub.1-4 haloalkoxy; R.sup.2 and R.sup.3, which are the same or different, are hydrogen, --CO.sub.2 R.sup.5 or C.sub.1-4 alkyl; R.sup.4 is hydrogen, cyano, C.sub.1-4 alkyl (optionally substituted with cyano or halogen), --(CH.sub.2).sub.n CO.sub.2 R.sup.6, --CONR.sup.6 R.sup.7, C.sub.3-6 cycloalkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, optionally substituted phenyl or optionally substituted heteroaromatic; or the group CR.sup.2 R.sup.3 R.sup.4 can form an allene moiety optionally substituted with C.sub.1-4 alkyl; R.sup.5, R.sup.6 and R.sup.7, which are the same or different, are hydrogen or C.sub.1-4 alkyl; n is 0, 1, 2, 3 or 4; and metal complexes thereof are active as fungicides.Type: GrantFiled: December 19, 1990Date of Patent: October 6, 1992Assignee: Imperial Chemical Industries PLCInventors: Don R. Baker, Patrick J. Crowley, Paul A. Worthington, Ian R. Matthews
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Patent number: 5153208Abstract: The invention relates to pyridine-2,4- and -2,5-dicarboxylic acid derivatives of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and X have the meanings given, a process for the preparation of these compounds and their use, in particular in medicaments for influencing the metabolism of collagen and collagen-like substances or the biosynthesis of Cl.sub.q.Type: GrantFiled: July 1, 1991Date of Patent: October 6, 1992Assignee: Hoechst AktiengesellschaftInventors: Martin Bickel, Dietrich Brocks, Harald Burghard, Volkmar Gunzler, Stephan Henke, Hartmut Hanauske-Abel, Jurgen Mohr, Georg Tschank
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Patent number: 5151436Abstract: Therapeutically useful thioformamide derivatives of the formula: ##STR1## wherein R represents alkyl, Het represents pyrid-3-yl, isoquinolin-4-yl, tetrahydroquinolin-3-yl, quinolin-3-yl, pyridazin-4-yl, pyrimid-5-yl, thiazol-5-yl, thieno[2,3-b]-pyridin-5-yl, pyrazin-2-yl, indol-3-yl and thieno[3,2-b]-pyridin-6-yl, Y represents ethylene, methylene or a valency bond, and X represents carbonyl, hydroxymethylene, >C.dbd.NOR.sup.1, >C.dbd.NN(R.sup.1).sub.2 or >C.dbd.NN(R.sup.1)CON(R.sup.1).sub.2 in which R.sup.1 represents hydrogen or optionally substituted alkyl, benzyl, phenethyl, 1-naphthylmethyl, 2-naphthylmethyl or pyrid-3-ylmethyl, or two R.sup.1 substituents on the same nitrogen atom may together form an optionally substituted alkylene radical chain and salts thereof, processes for their preparation and compositions containing them are described.Type: GrantFiled: August 23, 1990Date of Patent: September 29, 1992Assignee: Rhone-Poulenc SanteInventors: David C. Cook, Terance W. Hart, Iain M. Mc Lay, Malcolm N. Palfreyman, Brian W. Sharp, Roger J. A. Walsh
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Patent number: 5142056Abstract: A retroviral protease inhibiting compound of the formulaA--X--Bor a pharmaceutically acceptable salt, prodrug or ester thereof, wherein X is a linking group; A is(1) substituted amino,(2) substituted carbonyl,(3) functionalized imino,(4) functionalized alkyl,(5) functionalized acyl,(6) functionalized heterocyclic or(7) functionalized (heterocyclic)alkyl; and B is(1) substituted carbonyl independently defined as herein,(2) substituted amino independently defined as herein,(3) functionalized imino independently defined as herein,(4) functionalized alkyl independently defined as herein,(5) functionalized acyl independently defined as herein,(6) functionalized heterocyclic independently defined as herein or(7) functionalized (heterocyclic)alkyl independently defined as herein.Type: GrantFiled: May 9, 1990Date of Patent: August 25, 1992Assignee: Abbott LaboratoriesInventors: Dale J. Kempe, Daniel W. Norbeck, John W. Erickson
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Patent number: 5126358Abstract: The invention relates to novel isonicotinoylpyridinyl hydrazine derivatives of formula I ##STR1## wherein Hal is halogen,R.sub.1 is hydrogen, methyl or --COR.sub.5,R.sub.2 is hydrogen, C.sub.1 -C.sub.4 alkyl, or a radical selected from --COR.sub.5 and --CO--Z--R.sub.6,R.sub.3 is hydrogen, halogen, trifluoromethyl, trichloromethyl, --COOH, --COOCH.sub.3, --OH or nitro.R.sub.4 is hydrogen, halogen, methoxy or methyl,R.sub.5,R.sub.6, Z are as defined hereinafter.with the exception of 1-(pyridin-2'-yl)-2-(2,6-dichloroisonicotinoyl) hydrazine.The novel compounds have plant-protective properties and are especially suitable for protecting plants from attack by phytopathogenic microorganisms such as fungi, bacteria and viruses.Type: GrantFiled: December 21, 1990Date of Patent: June 30, 1992Assignee: Ciba-Geigy CorporationInventor: Walter Kunz
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Patent number: 5126357Abstract: A compound or a pharmaceutically acceptable salt thereof, having anti-inflammatory activity, is disclosed according to the Formula (I) ##STR1## wherein R is hydrogen, methyl or ethyl,R.sub.1 is a 2-pyridyl, 3-pyridyl or 4-pyridyl group or is phenyl, chlorophenyl or fluorophenyl,R.sub.2 is a 2-pyridyl, 3-pyridyl or 4-pyridyl group,R.sub.3 and R.sub.4 are identical or different and, taken separately, are hydrogen, fluorine, chlorine, bromine, C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkoxy, hydroxy, cyano or nitro or, taken together, are methylenedioxy, and n is 0 or 1.Type: GrantFiled: November 8, 1990Date of Patent: June 30, 1992Assignee: A. Nattermann & Cie. GmbHInventors: Michel Evers, Michael Parnham, Axel Romer, Hartmut Fischer, Norbert Dereu
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Patent number: 5120747Abstract: Platelet activating factor antagonists of formula (I): ##STR1## wherein R is phenyl or phenyl substituted by one or more substituents selected from nitro, halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl(C.sub.1 -C.sub.4)alkoxy, fluoro(C.sub.1 -C.sub.4)alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulphonyl, hydroxy, trifluoromethyl and cyano, or is phenyl fused to a dioxole ring;R.sup.1 and R.sup.2 are each independently H or C.sub.1 -C.sub.6 alkyl, or R.sup.1 and R.sup.2 together complete a pyrrolidinyl, piperidino, morpholino, piperazinyl, N-(C.sub.1 -C.sub.4 alkyl)piperazinyl or N-(C.sub.2 -C.sub.4 alkanoyl)-piperazinyl group;R.sup.2 is H or C.sub.1 -C.sub.4 alkyl and R.sup.1 is CN, C.sub.3 -C.sub.7 cycloalkyl, aryl, heteroaryl or a C.sub.1 -C.sub.4 alkyl group substituted by one or more substituents selected from C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.4 alkoxycarbonyl, aryl or heteroaryl;Z is selected from C.sub.1 -C.sub.6 alkoxy, aryl(C.sub.1 -C.sub.Type: GrantFiled: May 1, 1990Date of Patent: June 9, 1992Assignee: Pfizer Inc.Inventors: Kelvin Cooper, Michael Fray, Kenneth Richardson, John Steele