Polycyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/555)
  • Patent number: 5070086
    Abstract: Imidazo- and pyrimido-quinoline, naphthyridine and pyridopyrazine compounds, methods of making said compounds and their use as anti-allergy, antiinflammatory and/or agents for the treatment of hyperproliferative skin disease are disclosed.
    Type: Grant
    Filed: June 15, 1990
    Date of Patent: December 3, 1991
    Assignee: Schering Corporation
    Inventor: Richard Friary
  • Patent number: 5049559
    Abstract: The invention relates to thieno-triazolo-diazepine derivatives of the formula ##STR1## wherein Y stands for oxygen or sulphur and R stands for various substituents, to a preparation process of said compounds and to therapeutic compositions containing the same. The compounds are particularly interesting in the treatment of ischemia.
    Type: Grant
    Filed: May 11, 1990
    Date of Patent: September 17, 1991
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Pierre Braquet, Andre Esanu, Jean-Pierre Laurent, Jacques Pommier
  • Patent number: 5049560
    Abstract: This invention relates to thieno-triazolo-diazepine derivatives of the formula ##STR1## wherein R represents various substituents, to a preparation process of these compounds consisting in reacting the thieno-triazolo-diazepine compound of the formula ##STR2## on RSO.sub.2 Cl and to therapeutic compositions containing the same. The compounds are particularly interesting as anti-PAF and anti-ischemic agents.
    Type: Grant
    Filed: March 20, 1990
    Date of Patent: September 17, 1991
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Andre Esanu, Pierre Braquet, Christiane Martin, Jean-Pierre Laurent
  • Patent number: 5008263
    Abstract: Platelet activating factor antagonists of formula (I), (II) or (III): ##STR1## where A is optionally substituted benzene, pyridine, naphthalene, quinoline, thiophene, benzothiophene, pyrazole or isothiazole,X is O, S or NHY is 1,4 phenylene or a group of formula ##STR2## R.sup.1 is H or optionally substituted C.sub.1 -C.sub.4 alkyl, R.sup.2 and R.sup.3 are H or C.sub.1 -C.sub.4 alkyl,B is an optionally fused 5- or 6-membered ring containing nitrogen atoms,Het is an optionally substituted 5-membered heterocyclic ring containing nitrogen or a pyridine ring, the ring optionally being fused to benzene or nitrogen-containing heterocyclic ring.
    Type: Grant
    Filed: March 20, 1990
    Date of Patent: April 16, 1991
    Assignee: Pfizer Inc.
    Inventors: Kelvin Cooper, Michael J. Fray
  • Patent number: 4997831
    Abstract: The invention provides lactam derivatives of the general formula (I) ##STR1## wherein n represents 2 or 3; Im represents an imidazolyl group of the formula: ##STR2## wherein one of the groups represented by R.sup.1, R.sup.2 and R.sup.3 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl- group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group; Y represents a group --(CH.sub.2).sub.m --, wherein m represents 2, 3 or 4; or Y represents a group --X(CH.sub.2).sub.p --, wherein p represents 2 or 3, X represents an oxygen or a sulphur atom or a group NR.sup.4, where R.sup.4 is a C.sub.1-6 alkyl group, and X is attached to the benzene ring moiety of the molecule; and physiologically acceptable salts and solvates thereof.The compounds of formula (I) are potent and selective antagonists of 5-hydroxytryptamine at 5-HT.sub.
    Type: Grant
    Filed: August 31, 1989
    Date of Patent: March 5, 1991
    Assignee: Glaxo Group Limited
    Inventors: David E. Bays, Ian H. Coates, Alexander W. Oxford, Peter C. North
  • Patent number: 4985423
    Abstract: The invention relates to a group of new 1,4-diazepine derivatives of the formula ##STR1## wherein A represents a group of the formulae 2-10 ##STR2## These compounds have a strong anti-ulcer activity after oral administration.
    Type: Grant
    Filed: July 3, 1989
    Date of Patent: January 15, 1991
    Assignee: Duphar International Research B.V.
    Inventors: Jacobus A. J. den Hartog, Herman H. van Stuivenberg, Ineke van Wijngaarden
  • Patent number: 4963685
    Abstract: Novel Tetrahydroisoquino[2,1-c][1,3]benzodiazepines are disclosed having the formula ##STR1## where X and Y are each independently hydrogen, halogen, loweralkyl, loweralkoxy or --CF.sub.3, and R is hydrogen or loweralkyl, and the pharmaceutically acceptable acid addition salts thereof and where applicable the geometric and optical isomers and racemic mixtures thereof. The compounds of this invention display utility in enhancing memory.
    Type: Grant
    Filed: December 21, 1989
    Date of Patent: October 16, 1990
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Lawrence L. Martin, Richard C. Allen
  • Patent number: 4929615
    Abstract: Novel 7H-benzo[b]pyrazino[1,2-d]pyrrolo[3,2,1-jk][1,4]benzodiazepines, processes for the preparation thereof, and a method of treating depression utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: June 12, 1989
    Date of Patent: May 29, 1990
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Edward J. Glamkowski, Barbara E. Kurys
  • Patent number: 4908361
    Abstract: Novel Tetrahydroisoquino[2,1-c][1,3]benzodiazepines are disclosed having the formula ##STR1## where X and Y are each independently hydrogen, halogen, loweralkyl, loweralkoxy or --CF.sub.3, and R is hydrogen or loweralkyl, and the pharmaceutically acceptable acid addition salts thereof and where applicable the geometric and optical isomers and racemic mixtures thereof. The compounds of this invention display utility in enhancing memory.
    Type: Grant
    Filed: April 28, 1989
    Date of Patent: March 13, 1990
    Assignee: Hoechst-Roussel Incorporated
    Inventors: Lawrence L. Martin, Richard C. Allen
  • Patent number: 4897392
    Abstract: There are disclosed compounds having the formula ##STR1## where X is H, halogen, --OH,--OCH.sub.3,--NO.sub.2 or --CF.sub.3 ; Y is H, Cl or Br; Z is H, halogen, --OH or --OCH.sub.3 ; and R is H, loweralkyl, --CH.sub.2 OH or diloweralkylaminomethyl, which compounds are useful as analgesic agents.
    Type: Grant
    Filed: July 3, 1989
    Date of Patent: January 30, 1990
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: John J. Tegeler, Eileen M. Gardenhire, Grover C. Helsley
  • Patent number: 4840947
    Abstract: There are disclosed compounds of the formula ##STR1## where X and Y are independently hydrogen, loweralkyl, halogen or trifluoromethyl; Z is --CH.sub.2 CH.sub.2 --, --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 CH.sub.2 --; R is ##STR2## R.sub.2 being hydrogen, loweralkyl, ethoxycarbonyl, 2,2,2-trichloroethoxycarbonyl or phenoxycarbonyl; and R.sub.1 is hydrogen, loweralkanoyl, loweralkyl, ethoxycarbonyl, 2,2,2-trichloroethoxycarbonyl or phenoxycarbonyl; the dotted line within the seven-membered ring and the dotted line between R.sub.1 and the ring nitrogen being optional bonds such that the former is absent and the latter present when R is ##STR3## whereas the former is present and the latter absent when R is ##STR4## These compounds display antiinflammatory activities and analgesic activities.
    Type: Grant
    Filed: October 14, 1986
    Date of Patent: June 20, 1989
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang, Frederick J. Ehrgott, Jr.
  • Patent number: 4737496
    Abstract: The invention relates to 1,3,4,16b-tetrahydro-2H,10H-indolo[2,1-c]pyrazino[1,2-a][1,4]benzodiazepin e derivatives of the formula I, ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, C.sub.3-7 -alkenyl, C.sub.3-7 -alkynyl, 3 to 7 ring-membered cycloalkyl, C.sub.2-7 -alkyl substituted by a substituent selected from hydroxy, amino, N-mono-lower alkyl-amino and N,N-di-lower alkyl-amino; or R.sup.1 is lower alkyl substituted by a substituent selected from 3 to 7 ring-membered cycloalkyl, carboxy, lower alkoxycarbonyl, carbamoyl, N-mono-lower alkyl-carbamoyl, N,N-di-lower alkyl-carbamoyl and lower alkanoyl; or R.sup.1 is lower alkyl substituted by either phenyl or benzoyl each of said phenyl or benzoyl radicals being unsubstituted or substituted by up to three members selected from lower alkyl, lower alkoxy, lower alkylthio, halogen and trifluoromethyl; R.sup.2 and R.sup.3 represent hydrogen, lower alkyl, hydroxy, lowr alkoxy, halogen or trifluoromethyl; and R.sup.
    Type: Grant
    Filed: October 1, 1986
    Date of Patent: April 12, 1988
    Assignee: Ciba-Geigy Corporation
    Inventor: Jan W. F. Wasley
  • Patent number: 4678784
    Abstract: Fused tetracyclic benzodiazepines of the formula (I): ##STR1## where R.sup.1 is a cyclic amine such as 1-piperazine and R.sup.2 is H or a substituent as defined herein are useful as LHRH antagonizing agents. Also, methods for their synthesis, intermediates used in such synthesis, methods for use as medicaments and pharmaceutical compositions are described.
    Type: Grant
    Filed: October 7, 1985
    Date of Patent: July 7, 1987
    Assignee: McNeilab, Inc.
    Inventor: Chih Y. Ho
  • Patent number: 4636499
    Abstract: Novel compounds of the formula IIIa ##STR1## wherein R.sup.1a, R.sup.2a, R.sup.3a and R.sup.4a are the same or different and are hydrogen, an alkyl, alkoxy optionally completely or predominantly substituted by fluorine or chlorine, halogen, --CN, --CF.sub.3, --NO.sub.2, --COR, --COOR, aryl, aryloxy or arylalkoxy group, or adjacent groups R.sup.1a, R.sup.2a, R.sup.3a and R.sup.4a together with the adjacent carbon atoms in the benzimidazole ring form a 5-, 6- or 7-membered monocyclic ring or a 9-, 10- or 11-membered bicyclic ring, which rings may be saturated or unsaturated and may contain 0-3 heteroatoms selected from N and O and which rings may be optionally substituted with 1-4 substitutents selected from alkyl groups with 1-3 carbon atoms, halogen perferably F or Cl, alkylene radicals containing 4-5 carbon atoms giving spiro compounds, or two or four of these substituents together form one or two oxy groups ##STR2## whereby if R.sup.1a, R.sup.2a, R.sup.3a and R.sup.
    Type: Grant
    Filed: May 30, 1985
    Date of Patent: January 13, 1987
    Assignee: Aktiebolaget Hassle
    Inventors: Arne E. Brandstrom, Per L. Lindberg, Bjorn Wallmark