Two Of The Cyclos Share At Least Three Ring Members Or A Ring Member Is Shared By Three Of The Cyclos (e.g., Bridged, Peri-fused, Etc.) Patents (Class 540/556)
  • Patent number: 5166341
    Abstract: Indazole-3-carboxylic acid derivatives represented by the following general formula (I) and their physiologically acceptable acid addition salts or quaternary ammonium salts, ##STR1## are useful as a potent and selective antagonist of serotonin 3 (5-HT.sub.3) receptor. Also disclosed are compounds of the formula ##STR2## which are useful as intermediates in the production of the disclosed final product compounds.
    Type: Grant
    Filed: March 11, 1991
    Date of Patent: November 24, 1992
    Assignee: Dainippon Pharmaceutical Co., Ltd.
    Inventors: Tatsuya Kon, Shiro Kato, Toshiya Morie, Tadahiko Karasawa, Naoyuki Yoshida
  • Patent number: 5140033
    Abstract: Antibacterial 5-alkylquinolonecarboxylic acids of the formula ##STR1## in which R.sup.3 is C.sub.1 -C.sub.4 -alkyl,R.sup.1 is optionally substituted alkyl or cycloalkyl, alkenyl, alkoxy, amino or alkylamino or optionally substituted phenyl,R.sup.2 is hydrogen or optionally substituted alkyl,R.sup.4 is a nitrogen-containing heterocyclic radical, andA is hydrogen, halogen, methyl, cyano or nitro, or forms a bridge with R.sup.1.and hydrates and salts thereof.
    Type: Grant
    Filed: October 1, 1990
    Date of Patent: August 18, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Michael Schriewer, Klaus Grohe, Andreas Krebs, Uwe Petersen, Thomas Schenke, Ingo Haller, Karl G. Metzger, Rainer Endermann, Hans-Joachim Zeiler
  • Patent number: 5135930
    Abstract: Novel hydrogenated heterocyclic compounds, containing two nitrogen atoms, of the formula ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.5 and R.sub.7 are each, independently of the others, hydrogen or lower alkyl, m is 2 or 3, n is 1 or 2, and either R.sub.4 and R.sub.6 are each hydrogen or R.sub.4 and R.sub.6 together form an additional bond, in free form or in form of a salt, can be used as pharmaceutical active ingredients for memory improvement and can be manufactured in a manner known per se.
    Type: Grant
    Filed: December 3, 1990
    Date of Patent: August 4, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Wolfgang Frostl, Cesare Mondadori, Dietrich Strub, Armin Zust
  • Patent number: 5095103
    Abstract: Heterocyclic compounds of the formula ##STR1## with the substituent meanings given in the description, and derivatives thereof are suitable for dyeing and pigmenting the most diverse substrates.
    Type: Grant
    Filed: December 12, 1990
    Date of Patent: March 10, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventor: Hans Hochstetter
  • Patent number: 5091383
    Abstract: Antibacterial compounds have the formula ##STR1## wherein R.sup.1 is hydrogen, a pharmaceutically acceptable cation, or alkyl; A is CH, CF, CCl or N; Y is alkyl, haloalkyl, cyclopropyl, vinyl, methoxy, N-methylamino, p-fluorophenyl, p-hydroxyphenyl or p-aminophenyl; or A is carbon and is taken together with Y and the carbon and nitrogen to which A and Y are attached to form a five to seven membered ring which is optionally substituted; and R.sup.2 is a bridged-diazabicycloalkyl group.
    Type: Grant
    Filed: February 16, 1988
    Date of Patent: February 25, 1992
    Assignee: Pfizer Inc.
    Inventors: Martin R. Jefson, Paul R. McGuirk
  • Patent number: 5086178
    Abstract: Fluorinated diazabicycloalkane derivative of the following Formula I: ##STR1## wherein n represents 0, 1 or 2; R represents a quaternizing organic group; each R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 independently represents hydrogen, C.sub.1 -C.sub.6 alkyl, aryl, C.sub.1 -C.sub.6 alkyl-substituted aryl or aryl-substituted C.sub.1 -C.sub.6 alkyl and each X.sup.- independently represents a conterion or 2X.sup.- represents a single divalent counterion, are electrophilic fluorinating agents.
    Type: Grant
    Filed: September 20, 1990
    Date of Patent: February 4, 1992
    Assignee: Air Products and Chemicals, Inc.
    Inventor: Ronald E. Banks
  • Patent number: 5036153
    Abstract: (R,R)-2,5-Diazabicyclo[ 2.2.1]heptanes are prepared from a compound of the formula ##STR1## wherein X and R.sub.2 are as defined herein, by heating with tosylchloride in pyridine, reacting the formed compound of the formula ##STR2## with a C.sub.1 -C.sub.6 alkylamine or ammonia, and reducing or hydrolyzing the formed compound of the formula ##STR3## wherein R.sub.1 is hydrogen or C.sub.1 -C.sub.6 alkyl.
    Type: Grant
    Filed: October 18, 1989
    Date of Patent: July 30, 1991
    Inventors: Tamim F. Braish, Darrell E. Fox
  • Patent number: 5026856
    Abstract: Isoindoline derivatives represented by the formula (I) and their salts are disclosed. ##STR1## There are many varieties for the compound depending on the types of residues R.sup.1 -R.sup.9 and X. The compounds can be prepared from quinoline derivatives of the formula (II) and an isoindoline derivatives of the formula (III). The compounds of formula (I) and their salts have excellent antibacterial activities against both gram positive and gram negative microorganisms. They can be used as a medicine, an agrichemical, and a food preservative.
    Type: Grant
    Filed: May 23, 1989
    Date of Patent: June 25, 1991
    Assignee: Wakunaga Seiyaku Kabushiki Kaisha
    Inventors: Takashi Yatsunami, Akira Yazaki, Satoshi Inoue, Hitoshi Yamamoto, Masaharu Yokomoto, Jun Nomiyama, Shuichiro Noda
  • Patent number: 5015645
    Abstract: Disclosed are the compounds of formula I ##STR1## wherein R and R.sub.1 -R.sub.3 independently represent hydrogen or lower alkyl, and m represents the integer 2 or 3; their methods of preparation; pharmaceutical compositions thereof, and their use for treating cognitive disorders in mammals.
    Type: Grant
    Filed: October 19, 1989
    Date of Patent: May 14, 1991
    Assignee: Ciba-Geigy Corporation
    Inventor: Jan W. F. Wasley
  • Patent number: 5015738
    Abstract: Novel benzo[b]pyrrolo[3,2,1-jk]benzodiazepines, intermediates and processes for the preparation thereof, and methods for alleviating pain utilizing the compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: September 21, 1990
    Date of Patent: May 14, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Edward J. Glamkowski, Barbara E. Kurys
  • Patent number: 4983601
    Abstract: Novel benzo[b]pyrrolo[3,2,1-jk]benzodiazepines, intermediates and processes for the preparation thereof, and methods for alleviating pain utilizing the compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: August 7, 1989
    Date of Patent: January 8, 1991
    Assignee: Hoechst-Roussel Pharmaceutical Inc.
    Inventors: Edward J. Glamkowski, Barbara E. Kurys
  • Patent number: 4965273
    Abstract: There are disclosed new naphthyridine- and quinoline-carboxylic acids having a 1-tertiary-alkyl substituent, compositions containing them, and their use in treating bacterial infections in warm-blooded animals. Also disclosed are novel amines and intermediates used in the preparation of the naphthyridine- and quinoline-carboxylic acids.
    Type: Grant
    Filed: December 1, 1988
    Date of Patent: October 23, 1990
    Assignee: Bristol-Myers Company
    Inventors: Abraham Weber, Daniel Bouzard, Munir Essiz, Pierre Di Cesare, Jean-Pierre Jacquet, Philippe Remuzon
  • 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: 4912258
    Abstract: Fluorinated aniline derivatives of the general formula I are described ##STR1## in which R.sup.1 represents H or (CH.sub.2).sub.n -X, n is a whole number from 1 to 3, X is H, OH, NH.sub.2, CH.sub.3 CONH, CH.sub.3 SO.sub.2 NH, SO.sub.3 H or ArSO.sub.3 H, Ar is optionally substituted arylene radical, R.sup.1 is alternatively also a --(CH.sub.2).sub.3 -- group, which is bonded to the free o-position next to the N-atom, Y is H, --O--, --NH--, --S-- or a C--C single bond, R.sup.2, in the event that Y=H, is the same as or different from R.sup.1 and means one of the radicals shown for R.sup.1, and in the event that Y is a C--C single bond or --O--, --NH-- or --S--, is an alkylene group having 1 to 3 carbon atoms linked with Y, and R.sup.3 =H, alkyl having 1 to 3 carbon atoms, OCH.sub.3, CH.sub.3 CONH, CO.sub.2 H or SO.sub.3 H.
    Type: Grant
    Filed: February 5, 1988
    Date of Patent: March 27, 1990
    Assignee: Boehringer Mannheim GmbH
    Inventors: Hans-Georg Batz, Rupert Herrmann
  • Patent number: 4895943
    Abstract: Processes and intermediates for preparing 1,4-diazabicyclo[3.2.2.]nonane including a process for the preparation of a compound of the formula ##STR1## wherein R.sup.1 is C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkyl substituted with 1 to 6 halo groups; and R.sup.2 is hydrogen, naphthoyl, substituted naphthoyl, benzyl, substituted benzyl, benzoyl or substituted benzoyl, wherein each of said substituted naphthoyl, substituted benzyl, and substituted benzoyl is substituted with one to three substituents selected from the group consisting of halo, C.sub.1 -C.sub.4 alkoxy and C.sub.1 -C.sub.4 alkyl, comprising reacting a compound of the formula ##STR2## wherein R.sup.1 and R.sup.3 are independently selected from C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkyl substituted with 1 to 6 halo groups with an alkyl stannane or a trialkyl aluminum and, if desired, reacting the resulting compound of the formula III wherein R.sup.
    Type: Grant
    Filed: October 25, 1988
    Date of Patent: January 23, 1990
    Assignee: Pfizer Inc.
    Inventors: Robert C. Friedmann, John W. Lackey, Brian T. O'Neill
  • Patent number: 4861779
    Abstract: Antibacterial compounds have the formula ##STR1## wherein R.sup.1 is hydrogen, a pharmaceutically acceptable cation, or alkyl; A is CH, CF, CCl or N; Y is alkyl, haloalkyl, cyclopropyl, vinyl, methoxy, N-methylamino, p-fluorophenyl, p-hydroxyphenyl or p-aminophenyl; or A is carbon and is taken together with Y and the carbon and nitrogen to which A and Y are attached to form a five to seven membered ring which is optionally substituted; and R.sup.2 is a bridged-diazabicycloalkyl group.
    Type: Grant
    Filed: August 19, 1986
    Date of Patent: August 29, 1989
    Assignee: Pfizer Inc.
    Inventors: Martin R. Jefson, Paul R. Mc Guirk
  • Patent number: 4826839
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: j is 0 or 1;q is 0, 1 or 2;p is 0 and r is 2 or 3, orp is 1 and r is 2;X is O, S, SO or NR where R is hydrogen, C.sub.1-6 alkyl or C.sub.1-10 carboxylic acyl;Y is NH; or O when R.sub.1 is hydrogen; either R.sub.1 is C.sub.1-6 alkoxy and one of R.sub.2, R.sub.3 and R.sub.4 is hydrogen and the other two are selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-10 carboxylic acylamino, C.sub.1-6 alkyl S(O) n wherein n is 0, 1 or 2, nitro or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl or phenyl C.sub.1-4 alkyl groups any of which phenyl moieties may be substituted by one or two groups selected from halogen, CF.sub.3, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; or R.sub.1 is hydrogen and R.sub.2, R.sub.3 and R.sub.4 are independently selected from hydrogen, C.sub.
    Type: Grant
    Filed: July 17, 1986
    Date of Patent: May 2, 1989
    Assignee: Beecham Group p.l.c.
    Inventors: Francis D. King, Michael S. Hadley, Roger T. Martin
  • Patent number: 4762831
    Abstract: A process for the preparation of a 1,8-bridged 4-quinolone-3-carboxylic acid of the formula ##STR1## wherein the substituents are defined hereinbelow. Some of the compound are new. The old and new compounds are antibacterials and promote animal growth.
    Type: Grant
    Filed: June 13, 1986
    Date of Patent: August 9, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus Grohe, Michael Schriewer
  • Patent number: 4761412
    Abstract: The invention relates to benzopyrrolobenzodiazepines and quinobenzodiazepines of the formula ##STR1## where X and Y may be the same or different and each is hydrogen, halogen, CF.sub.3, lower alkyl, lower alkoxy, lower alkylthio and lower alkylsulfonyl, p and q are independently 1 or 2; R.sub.1 is hydrogen when R.sub.2 is bonded to R.sub.3 to form a --(CH.sub.2).sub.m --CH.sub.2 -- group or a --CH.dbd.CH-- group; R.sub.3 is hydrogen when R.sub.1 is bonded to R.sub.2 to form a --(CH.sub.2).sub.m --CH.sub.2 -- group or a --CH.dbd.CH-- group; m is 1 or 2; R.sub.4 is NR.sub.5 R.sub.6 wherein R.sub.5 is hydrogen or lower alkyl and R.sub.6 is hydrogen, lower alkyl or a group of the formula (CH.sub.2).sub.n NR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are lower alkyl, and n is 2 or 3, ##STR2## wherein R.sub.9 is lower alkyl, ##STR3## wherein R.sub.10 is CH.sub.2 CH.sub.2 OH, lower alkyl, phenyl, phenyl substituted by halogen, CF.sub.
    Type: Grant
    Filed: November 12, 1986
    Date of Patent: August 2, 1988
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 4761411
    Abstract: The invention relates to dihydrobenzopyrrolobenzodiazepines of the formula ##STR1## where X and Y may be the same or different and each is hydrogen, halogen, CF.sub.3, lower alkyl, lower alkoxy, lower alkylthio and lower alkylsulfonyl; R.sub.1 is hydrogen when R.sub.2 is bonded to R.sub.3 to form a --CH.sub.2 CH.sub.2 -- group; and R.sub.3 is hydrogen when R.sub.1 is bonded to R.sub.2 to form a --CH.sub.2 CH.sub.2 -- group and the pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: May 18, 1983
    Date of Patent: August 2, 1988
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 4751223
    Abstract: There are disclosed compounds of the formula ##STR1## where X and Y are independently hydrogen, loweralkyl, trifluoromethyl or halogen; Z is --CH.sub.2 CH.sub.2 --, --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 CH.sub.2 --; n is 1, 2 or 3; R.sub.1 is hydrogen, loweralkanoyl, aroyl, ethoxycarbonyl, phenoxycarbonyl, loweralkylaminocarbonyl, arylaminocarbonyl, loweralkyl or arylmethyl; R.sub.2 is hydrogen or loweralkyl; R.sub.3 is hydrogen, loweralkyl, ethoxycarbonyl, loweralkanoyl or arylloweralkyl, or R.sub.2 and R.sub.3 taken together is isopropylidene; with the proviso that when n is 3, X, Y and R.sub.1 are all hydrogen and Z is --CH.sub.2 CH.sub.2 --, R.sub.2 and R.sub.3 can not both be methyl. These compounds display antiinflammatory and analgesic activities.
    Type: Grant
    Filed: October 14, 1986
    Date of Patent: June 14, 1988
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang, Frederick J. Ehrgott, Jr.
  • Patent number: 4725595
    Abstract: Antibacterially active new 1,8-bridged 4-quinolone-3-carboxylic acid derivatives of the formula ##STR1## in which Y is carboxyl or a derivative thereofR.sup.1, R.sup.2, R.sup.3, R.sup.4, X.sup.1, X.sup.2 and X.sup.5 are H or various radicals,Z is O, NH, substituted NH, --CON< or --SO.sub.2 N<,m and n are 0 or 1, andA, B, D and E are CH or substituted C or up to three of them are N,and physiologically acceptable salts thereof. Novel intermediates are described as well as processes for making the intermediates and end products.
    Type: Grant
    Filed: January 8, 1987
    Date of Patent: February 16, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Michael Schriewer, Klaus Grohe, Hans-Joachim Zeiler, Karl G. Metzger
  • Patent number: 4663453
    Abstract: The invention relates to benzopyrrolobenzodiazepines and quinobenzodiazepines of the formula ##STR1## where X and Y may be the same or different and each is hydrogen, halogen, CF.sub.3, lower alkyl, lower alkoxy, lower alkylthio and lower alkylsulfonyl, p and q are independently 1 or 2; R.sub.1 is hydrogen when R.sub.2 is bonded to R.sub.3 to form a --(CH.sub.2).sub.m --CH.sub.2 -- group or a --CH.dbd.CH-- group; R.sub.3 is hydrogen when R.sub.1 is bonded to R.sub.2 to form a --(CH.sub.2).sub.m --CH.sub.2 -- group or a --CH.dbd.CH-- group; m is 1 or 2; R.sub.4 is NR.sub.5 R.sub.6 wherein R.sub.5 is hydrogen or lower alkyl and R.sub.6 is hydrogen, lower alkyl or a group of the formula (CH.sub.2).sub.n NR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are lower alkyl, and n is 2 or 3, ##STR2## wherein R.sub.9 is lower alkyl, ##STR3## wherein R.sub.10 is CH.sub.2 CH.sub.2 OH, lower alkyl, phenyl, phenyl substituted by halogen, CF.sub.
    Type: Grant
    Filed: August 28, 1985
    Date of Patent: May 5, 1987
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 4638066
    Abstract: Compounds of formula (I), ##STR1## or an N-oxide or pharmaceutically acceptable salt thereof, wherein R.sub.1 is hydrogen, C.sub.1-7 alkyl, C.sub.3-7 cycloalkyl, C.sub.4-7 cycloalkenyl or C.sub.1-4 alkyl substituted by C.sub.2-7 alkenyl, C.sub.2-7 alkynyl, C.sub.3-7 cycloalkyl, hydroxy, thiol, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, carboxy, C.sub.1-4 alkoxycarbonyl, C.sub.1-4 alkanoyl, amino optionally substituted by one or two C.sub.1-4 alkyl or by C.sub.4-6 polymethylene optionally containing an oxygen or nitrogen atom, aminocarbonyl optionally N-substituted by one or two C.sub.1-4 alkyl, or benzoyl or phenyl either being optionally ring-substituted by C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or trifluoromethyl, R.sub.2 and R.sub.3 are the same or different and are hydrogen, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, halogen or trifluoromethyl, m is 1 to 3 and n is 1 or 2, the hydrogen atom bonded to the C.sub.a carbon atom being trans to the hydrogen atom bonded to the C.sub.
    Type: Grant
    Filed: December 20, 1984
    Date of Patent: January 20, 1987
    Assignee: Beecham Group p.l.c.
    Inventors: Laramie M. Gaster, Barry S. Orlek