Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Acyclic Nitrogen Patents (Class 546/265)
  • Patent number: 5962479
    Abstract: 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: Grant
    Filed: December 6, 1996
    Date of Patent: October 5, 1999
    Assignee: Pfizer Inc.
    Inventor: Yuhpyng Liang Chen
  • Patent number: 5948778
    Abstract: 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: Grant
    Filed: May 19, 1998
    Date of Patent: September 7, 1999
    Assignee: Merrel Pharmaceuticals Inc.
    Inventors: Viviane Van Dorsselaer, Daniel Schirlin, Celine Tarnus
  • Patent number: 5932734
    Abstract: 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: Grant
    Filed: August 7, 1997
    Date of Patent: August 3, 1999
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Xi Chen
  • Patent number: 5874584
    Abstract: 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: Grant
    Filed: November 5, 1997
    Date of Patent: February 23, 1999
    Assignee: Eastman Kodak Company
    Inventors: Trevor John Wear, Christopher Peter Moore, Alistair J. Goulden, Paul D. Beer, Nicholas C. Fletcher
  • Patent number: 5827827
    Abstract: 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: Grant
    Filed: June 20, 1996
    Date of Patent: October 27, 1998
    Assignee: The Scripps Research Institute
    Inventors: Kim D. Janda, Peter Wirsching
  • Patent number: 5801175
    Abstract: 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: Grant
    Filed: September 13, 1996
    Date of Patent: September 1, 1998
    Assignees: 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
  • Patent number: 5767085
    Abstract: Compounds of the formula A--B--C--D(--E).sub.p are used to stimulate the release of growth hormone from the pituitary.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: June 16, 1998
    Assignee: Novo Nordisk A/S
    Inventors: Nils Langeland Johansen, Jesper Lau, Kjeld Madsen, Behrend Friedrich Lundt, Henning Th.o slashed.gersen, Birgit Sehested Hansen, Bernd Peschke
  • Patent number: 5760246
    Abstract: 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: Grant
    Filed: December 17, 1996
    Date of Patent: June 2, 1998
    Inventors: 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
  • Patent number: 5760231
    Abstract: 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: Grant
    Filed: October 22, 1996
    Date of Patent: June 2, 1998
    Assignee: Eastman Kodak Company
    Inventors: Trevor John Wear, Christopher Peter Moore, Alistair J. Goulden, Paul D. Beer, Nicholas C. Fletcher
  • Patent number: 5747505
    Abstract: 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: Grant
    Filed: September 20, 1996
    Date of Patent: May 5, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Richard Connell, Siegfried Goldmann, Ulrich Muller, Martin Beuck, Hilmar Bischoff, Dirk Denzer, Rudi Grutzmann, Stefan Wohlfeil
  • Patent number: 5733931
    Abstract: 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: Grant
    Filed: March 8, 1996
    Date of Patent: March 31, 1998
    Assignee: Nissin Food Products Co., Ltd.
    Inventors: Toshihiro Yamada, Yoichi Nobuhara, Ichinari Takagi, Shiho Furumoto, Kazuhiro Kobayashi, Kiyohito Ikemoto
  • Patent number: 5723646
    Abstract: 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: Grant
    Filed: January 16, 1992
    Date of Patent: March 3, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Thomas Seitz, Heinz-Wilhelm Dehne
  • Patent number: 5712294
    Abstract: 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: Grant
    Filed: May 25, 1995
    Date of Patent: January 27, 1998
    Assignee: Adir Et Compagnie
    Inventors: Jean-Michel Robert, Odile Rideau, Sylvie Robert-Piessard, Jacqueline Courant, Guillaume Le Baut, Daniel-Henri Caignard, Pierre Renard, Gerard Adam
  • Patent number: 5672615
    Abstract: 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: Grant
    Filed: March 11, 1996
    Date of Patent: September 30, 1997
    Assignee: Novartis Corporation
    Inventors: Lawrence J. MacPherson, David Thomas Parker
  • Patent number: 5658907
    Abstract: 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: Grant
    Filed: May 31, 1995
    Date of Patent: August 19, 1997
    Assignee: Medivir A/B
    Inventors: John M. Morin, Jr., Robert J. Ternansky, Rolf Noreen, Peter Tomas Lind
  • Patent number: 5659033
    Abstract: 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: Grant
    Filed: September 13, 1995
    Date of Patent: August 19, 1997
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Xi Chen
  • Patent number: 5618826
    Abstract: 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: Grant
    Filed: May 30, 1995
    Date of Patent: April 8, 1997
    Assignee: University of Florida
    Inventors: Richard H. Hammer, Nicholas S. Bodor
  • Patent number: 5616776
    Abstract: 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: Grant
    Filed: April 7, 1995
    Date of Patent: April 1, 1997
    Assignee: Abbott Laboratories
    Inventors: 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
  • Patent number: 5614634
    Abstract: 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: Grant
    Filed: June 5, 1995
    Date of Patent: March 25, 1997
    Assignee: Schering Aktiengesellschaft
    Inventors: Josef Heindl, Werner Skuballa, Bernd Buchmann, Wolfgang Frohlich, Roland Ekerdt, Claudia Giesen
  • Patent number: 5614548
    Abstract: 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: Grant
    Filed: September 8, 1994
    Date of Patent: March 25, 1997
    Assignee: Wake Forest University
    Inventors: Claude Piantadosi, Khalid S. Ishaq, Canio J. Marasco, Jr., Larry W. Daniel, Louis S. Kucera, Edward J. Modest, Barry P. Goz
  • Patent number: 5552419
    Abstract: 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: Grant
    Filed: November 3, 1994
    Date of Patent: September 3, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Lawrence J. MacPherson, David T. Parker
  • Patent number: 5545608
    Abstract: 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: Grant
    Filed: April 25, 1994
    Date of Patent: August 13, 1996
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Katsushi Morimoto, Masatoshi Ohnari, Tsutomu Nawamaki, Shigeomi Watanabe, Kimihiro Ishikawa
  • Patent number: 5519132
    Abstract: 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: Grant
    Filed: February 21, 1995
    Date of Patent: May 21, 1996
    Assignee: The Du Pont Merck Pharmaceutical Company
    Inventor: Christopher A. Teleha
  • Patent number: 5506227
    Abstract: 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: Grant
    Filed: April 13, 1992
    Date of Patent: April 9, 1996
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Robert Zamboni, Daniel Guay, Jacques-Yves Gauthier
  • Patent number: 5506242
    Abstract: 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: Grant
    Filed: June 24, 1994
    Date of Patent: April 9, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Lawrence J. MacPherson, David T. Parker, Arco Y. Jeng
  • Patent number: 5463124
    Abstract: 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: Grant
    Filed: June 22, 1994
    Date of Patent: October 31, 1995
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Detlef Jacobi, Heiner Jendralla, Bernhard Kammermeier
  • Patent number: 5455258
    Abstract: 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: Grant
    Filed: January 6, 1993
    Date of Patent: October 3, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Lawrence J. MacPherson, David T. Parker
  • Patent number: 5430155
    Abstract: 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: Grant
    Filed: December 17, 1993
    Date of Patent: July 4, 1995
    Assignee: The Du Pont Merck Pharmaceutical Company
    Inventors: Prabhakar K. Jadhav, Lawrence R. McGee, Ashok Shenvi, Carl N. Hodge
  • Patent number: 5416117
    Abstract: 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: Grant
    Filed: February 28, 1994
    Date of Patent: May 16, 1995
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Ryoichi Ando, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
  • Patent number: 5384425
    Abstract: 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: Grant
    Filed: October 7, 1993
    Date of Patent: January 24, 1995
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Noriki Ito, Tomoyuki Yasunaga, Yuichi Iizumi, Tomio Araki
  • Patent number: 5364853
    Abstract: 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: Grant
    Filed: August 20, 1992
    Date of Patent: November 15, 1994
    Assignee: Rhone-Poulenc Rorer Limited
    Inventors: Malcolm N. Palfreyman, Nigel Vicker
  • Patent number: 5358955
    Abstract: 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: Grant
    Filed: June 2, 1993
    Date of Patent: October 25, 1994
    Assignee: Abbott Laboratories
    Inventors: Dee W. Brooks, Teodozy J. Kolasa
  • Patent number: 5354866
    Abstract: 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: Grant
    Filed: September 14, 1993
    Date of Patent: October 11, 1994
    Assignee: Abbott Laboratories
    Inventors: Dale J. Kempf, Daniel W. Norbeck, Lynn M. Codacovi, Jacob J. Plattner, Hing L. Sham, Chen Zhao
  • Patent number: 5344836
    Abstract: 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: Grant
    Filed: November 5, 1992
    Date of Patent: September 6, 1994
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Nobuyuki Hamanaka, Kanji Takahashi, Hidekado Tokumoto
  • Patent number: 5328909
    Abstract: 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: Grant
    Filed: June 25, 1992
    Date of Patent: July 12, 1994
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Ryoichi Ando, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
  • Patent number: 5326759
    Abstract: 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: Grant
    Filed: November 1, 1993
    Date of Patent: July 5, 1994
    Assignee: American Cyanamid Company
    Inventors: Joseph J. Hlavka, Phaik-Eng Sum, Yakov Gluzman, Ving J. Lee
  • Patent number: 5318989
    Abstract: 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: Grant
    Filed: December 18, 1992
    Date of Patent: June 7, 1994
    Assignee: Bristol-Myers Squibb Company
    Inventors: John F. Kadow, Mark D. Wittman
  • Patent number: 5294720
    Abstract: 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: Grant
    Filed: May 31, 1991
    Date of Patent: March 15, 1994
    Assignee: The DuPont Merck Pharmaceutical Co.
    Inventors: Prabhakar K. Jadhav, Lawrence R. McGee, Ashok Shenvi, Carl N. Hodge
  • Patent number: 5227492
    Abstract: 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: Grant
    Filed: June 30, 1992
    Date of Patent: July 13, 1993
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Noriki Ito, Tomoyuki Yasunaga, Yuichi Iizumi, Tomio Araki
  • Patent number: 5216169
    Abstract: 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: Grant
    Filed: September 18, 1990
    Date of Patent: June 1, 1993
    Assignee: Fuji Photo Film Co., Ltd.
    Inventor: Shigeru Yamazaki
  • Patent number: 5204359
    Abstract: 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: Grant
    Filed: September 11, 1991
    Date of Patent: April 20, 1993
    Assignee: Nihon Bayer Agrochem K.K.
    Inventors: Kozo Shiokawa, Shinichi Tsuboi, Koichi Moriya, Yumi Hattori, Ikuro Honda, Katsuhiko Shibuya
  • Patent number: 5185375
    Abstract: 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: Grant
    Filed: March 30, 1990
    Date of Patent: February 9, 1993
    Assignee: May & Baker Limited
    Inventors: David C. Cook, Terance W. Hart, Iain M. McLay, Malcolm N. Palfreyman, Roger J. A. Walsh
  • Patent number: 5177089
    Abstract: 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: Grant
    Filed: July 25, 1990
    Date of Patent: January 5, 1993
    Assignee: Eisai Co., Ltd.
    Inventors: Norio Minami, Fumihiro Ozaki, Keiji Ishibashi, Yasuhiro Kabasawa, Megumi Ikemori, Toshiaki Ogawa, Takanori Kawamura
  • Patent number: 5153199
    Abstract: 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: Grant
    Filed: December 19, 1990
    Date of Patent: October 6, 1992
    Assignee: Imperial Chemical Industries PLC
    Inventors: Don R. Baker, Patrick J. Crowley, Paul A. Worthington, Ian R. Matthews
  • Patent number: 5153208
    Abstract: 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: Grant
    Filed: July 1, 1991
    Date of Patent: October 6, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Martin Bickel, Dietrich Brocks, Harald Burghard, Volkmar Gunzler, Stephan Henke, Hartmut Hanauske-Abel, Jurgen Mohr, Georg Tschank
  • Patent number: 5151436
    Abstract: 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: Grant
    Filed: August 23, 1990
    Date of Patent: September 29, 1992
    Assignee: Rhone-Poulenc Sante
    Inventors: David C. Cook, Terance W. Hart, Iain M. Mc Lay, Malcolm N. Palfreyman, Brian W. Sharp, Roger J. A. Walsh
  • Patent number: 5142056
    Abstract: 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: Grant
    Filed: May 9, 1990
    Date of Patent: August 25, 1992
    Assignee: Abbott Laboratories
    Inventors: Dale J. Kempe, Daniel W. Norbeck, John W. Erickson
  • Patent number: 5126358
    Abstract: 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: Grant
    Filed: December 21, 1990
    Date of Patent: June 30, 1992
    Assignee: Ciba-Geigy Corporation
    Inventor: Walter Kunz
  • Patent number: 5126357
    Abstract: 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: Grant
    Filed: November 8, 1990
    Date of Patent: June 30, 1992
    Assignee: A. Nattermann & Cie. GmbH
    Inventors: Michel Evers, Michael Parnham, Axel Romer, Hartmut Fischer, Norbert Dereu
  • Patent number: 5120747
    Abstract: 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: Grant
    Filed: May 1, 1990
    Date of Patent: June 9, 1992
    Assignee: Pfizer Inc.
    Inventors: Kelvin Cooper, Michael Fray, Kenneth Richardson, John Steele