Five-membered Hetero Ring Consisting Of One Nitrogen And Four Carbons Patents (Class 544/372)
  • Patent number: 5428037
    Abstract: Compounds of the formula: ##STR1## wherein A, R.sup.1, R.sup.2, R.sup.3 and m are defined as in the specification or a pharmaceutically acceptable acid addition salt or N-oxide thereof, are calcium and sodium channel antagonists useful for treating mammals having a variety of disease states, such as stroke, epilepsy, hypertension, angina, migraine, arrhythmia, thrombosis, embolism, and also for treatment of spinal injuries.
    Type: Grant
    Filed: April 9, 1993
    Date of Patent: June 27, 1995
    Assignee: Syntex Pharmaceuticals, Ltd.
    Inventors: Jean-Claude Pascal, Gary McCort, Dominique Blondet, Francoise Gellibert
  • Patent number: 5424451
    Abstract: Aminoalkylcarbamic esters of eseroline suitable for use as cholinesterase activity inhibitors, having general formula (I) ##STR1## where R stands for an amine selected out of the group consisting of ##STR2## and n, R1, R2, R3, and R4 are as defined in the text.
    Type: Grant
    Filed: January 4, 1994
    Date of Patent: June 13, 1995
    Assignee: Mediolanum Farmaceutici S.p.A.
    Inventors: Maria A. Alisi, Mario Brufani, Maria C. Cesta, Luigi Eieocamo, Gianluca Gostoli, Sperandina Lappa, Pier Giuseppe Pagella, Enrico Ferrari, Stefano Maiorana, Donata Marchesini
  • Patent number: 5418236
    Abstract: Aroyl(piperidinyl and piperazinyl)acyl pyrroles of the following formula have anxiolytic activity: ##STR1## wherein, Y is selected from the group consisting of N, CH or COH;A.sup.1 is selected from the group consisting of ##STR2## n is an integer from 1 to 5;R.sup.1 is selected from the group consisting of H and C.sub.1-4 alkyl;R.sup.2 and R.sup.3 are selected from the group consisting of H and C.sub.1-4 alkyl;R.sup.4 is selected from the group consisting of halo, C.sub.1-4 alkyl, hydroxy, C.sub.1-4 alkoxy, nitro, amino, C.sub.1-4 acylamino, cyano, trihaloC.sub.1-4 alkyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylsulfinyl and C.sub.1-4 acyl; andR.sup.5 is selected from the group consisting of halo, C.sub.1-4 alkyl, hydroxy, C.sub.1-4 alkoxy, nitro, amino, C.sub.1-4 acylamino, cyano, trihaloC.sub.1-4 alkyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylsulfinyl and C.sub.1-4 acyl; and acid addition salts thereof.
    Type: Grant
    Filed: December 23, 1993
    Date of Patent: May 23, 1995
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Richard J. Carmosin, John R. Carson, Philip Pitis
  • Patent number: 5413999
    Abstract: Compounds of formula ##STR1## where R.sup.1 and R.sup.2 are independently hydrogen or optionally-substituted C.sub.1-4 alkyl or aryl, or R.sup.1 and R.sup.2 are joined together to form a monocyclic or bicyclic ring system, are HIV protease inhibitors. These compounds are useful in the treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of treating infection by HIV are also described.
    Type: Grant
    Filed: May 7, 1993
    Date of Patent: May 9, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Joseph P. Vacca, Bruce D. Dorsey, James P. Guare, M. Katharine Holloway, Randall W. Hungate, Rhonda B. Levin
  • Patent number: 5414082
    Abstract: A process for producing pharmacologically active 1-unsubstituted 3-aminopyrroles of the formula ##STR1## by ring transformation of a corresponding 1,2-thiazolium pyrrole in a single step, without producing harmful byproducts.
    Type: Grant
    Filed: August 11, 1993
    Date of Patent: May 9, 1995
    Assignee: Arzneimittelwerk Dresden GmbH
    Inventors: Andreas Rolfs, Jurger Liebscher, Klaus Unverferth, Gottfried Faust
  • Patent number: 5413997
    Abstract: A triphenylmethane derivative represented by the following general formula: ##STR1## exhibits bone absorption inhibiting effects and is useful as a medicament for treating osteoporosis.
    Type: Grant
    Filed: January 21, 1993
    Date of Patent: May 9, 1995
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Iwao Kinoshita, Daisuke Machii, Yasuo Onoda, Haruki Takai, Nobuo Kosaka, Katsuichi Shuto, Katsushige Gomi, Makoto Morimoto, Akio Ishii
  • Patent number: 5387593
    Abstract: Novel piperazinyl- and piperidinyl-cyclohexanols of the following formula are useful as anxiolytic agents and have other psychotropic properties ##STR1##
    Type: Grant
    Filed: February 17, 1994
    Date of Patent: February 7, 1995
    Assignee: Briston-Myers Squibb
    Inventors: Ronald J. Mattson, John D. Catt
  • Patent number: 5384319
    Abstract: Aminoalkylphenyl derivatives of formula I ##STR1## wherein alk, R.sub.1 -R.sub.6, X and Y are as defined in the description, and salts thereof, exhibit properties inhibiting the biosynthesis of interleukin-1 (IL-1) and analgesic properties and can therefore be used as active ingredients in medicaments. They are prepared in a manner known per se.
    Type: Grant
    Filed: December 20, 1993
    Date of Patent: January 24, 1995
    Assignee: Ciba-Geigy Corporation
    Inventor: Pier G. Ferrini
  • Patent number: 5382583
    Abstract: Piperazine derivatives of formula: ##STR1## and their pharmaceutically acceptable acid addition salts are disclosed. In the formula, n is 1 or 2; R and R.sup.5 are hydrogen or lower alkyl, R.sup.1 is substituted or unsubstituted aryl or a heteroaromatic radical; R.sup.3 is substituted or unsubstituted aryl or substituted or unsubstituted arylalkyl; R.sup.9 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl or substituted or unsubstituted arylalkyl with the proviso that when R.sup.9 is hydrogen, alkyl, or arylalkyl, R.sup.5 is other than a tertiary alkyl group. The compounds of this invention are useful 5-HT.sub.1A antagonists for the treatment of CNS disorders such as anxiety.
    Type: Grant
    Filed: December 29, 1992
    Date of Patent: January 17, 1995
    Assignee: John Wyeth & Brother, Limited
    Inventor: Ian A. Cliffe
  • Patent number: 5380726
    Abstract: Substituted dialkylthio ethers of formula I ##STR1## wherein R.sub.1 -R.sub.6, alk, X and Y are as defined in the description, and salts thereof, exhibit properties inhibiting the biosynthesis of interleukin-1 (IL-1) and analgesic properties and can therefore be used as active ingredients in medicaments. They are prepared in a manner known per se.
    Type: Grant
    Filed: December 20, 1993
    Date of Patent: January 10, 1995
    Assignee: Ciba-Geigy Corporation
    Inventor: Pier G. Ferrini
  • Patent number: 5373008
    Abstract: Compounds of formula I ##STR1## and their salts in which n=0 or 1, R.sub.1 and R.sub.2 are each aliphatic or cycloalkyl or NR.sub.1 R.sub.2 is an optionally substituted heterocyclic ring, R.sub.3 is alkyl, cycloalkyl or optionally substituted amino, R.sub.5 is an aliphatic group, R.sub.6 is H, an optionally substituted aliphatic group or a cycloalkyl group, or R.sub.3 and R.sub.5 together with the nitrogen and carbon atoms to which they are attached form an optionally substituted heterocyclic ring or R.sub.5 and R.sub.6 together with the nitrogen to which they are attached form a heterocyclic ring optionally substituted by alkyl and R.sub.7 is optionally substituted alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkoxycarbonyl, trifluoromethyl or cyano have utility as hypoglycemic agents.
    Type: Grant
    Filed: January 27, 1993
    Date of Patent: December 13, 1994
    Assignee: The Boots Compant plc.
    Inventor: Balasubramanian Gopalan
  • Patent number: 5369103
    Type: Grant
    Filed: June 19, 1992
    Date of Patent: November 29, 1994
    Assignee: John Wyeth & Brother, Limited
    Inventors: Ian A. Cliffe, Alan C. White, Anderson D. Ifill
  • Patent number: 5364849
    Abstract: Piperazine derivatives of formula ##STR1## and their pharmaceutically acceptable acid addition salts are disclosed. In the formula n is 1 or 2, R is hydrogen or lower alkyl, R.sup.1 is an aryl or nitrogen containing heteroaryl radical, R.sup.2 is hydrogen or lower alkyl, R.sup.3 is aryl, C.sub.4-8 alkyl or aryl(lower)alkyl and X is a functionalised group of specified meaning. The compounds exhibit activity as 5-HT.sub.1A antagonists and can be used, into alia, for the treatment of CNS disorders, such as anxiety.
    Type: Grant
    Filed: July 10, 1992
    Date of Patent: November 15, 1994
    Assignee: John Wyeth & Brother, Limited
    Inventor: Ian A. Cliffe
  • Patent number: 5356893
    Abstract: The invention provides compounds of formula (I): ##STR1## or a physiologically acceptable salt or solvate thereof wherein R.sup.1 represents a halogen or hydrogen atom or a C.sub.1-6 alkyl or C.sub.1-6 alkoxy group;R.sup.2 represents a phenyl group optionally substituted by one or two substituents;R.sup.3 represents the group ##STR2## R.sup.4 and R.sup.5, which may be the same or different, each independently represent a hydrogen atom or a halogen atom, or a group selected from hydroxy, C.sub.1-6 alkoxy or C.sub.1-6 alkyl.The compounds may be used in the treatment or prophylaxis of depression and other CNS disorders.
    Type: Grant
    Filed: September 17, 1992
    Date of Patent: October 18, 1994
    Assignee: Glaxo Group Limited
    Inventors: John Bradshaw, John W. Clitherow, Ian B. Campbell
  • Patent number: 5350762
    Abstract: There are disclosed various compounds of the formula below, ##STR1## where the various parameters R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, m and n are as defined in the specification, which show activities as a monoamine oxidase inhibitor demonstrating a utility for the treatment of depression, and activities as a cholinesterase inhibitor demonstrating a utility for the treatment of various memory dysfunctions such as Alzheimer's disease.
    Type: Grant
    Filed: March 8, 1993
    Date of Patent: September 27, 1994
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Lawrence L. Martin, Larry Davis
  • Patent number: 5344830
    Abstract: Diacylpiperazines of general structure ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, and asthma, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
    Type: Grant
    Filed: December 10, 1992
    Date of Patent: September 6, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Sander G. Mills, Richard J. Budhu, Conrad P. Dorn, William J. Greenlee, Malcolm MacCoss, Mu T. Wu
  • Patent number: 5340812
    Abstract: Piperazine derivatives of formula ##STR1## and their pharmaceutically acceptable acid addition salts are disclosed. In the formula n is 1 or 2, R is hydrogen or lower alkyl, R.sup.1 is an aryl or nitrogen containing heteroaryl radical, R.sup.2 is hydrogen or lower alkyl, R.sup.3 is aryl, C.sub.4-8 alkyl or aryl(lower)alkyl, and X is a functionalised group of specified meaning. The compounds exhibit activity as 5-HT.sub.1A antagonists and can be used, inter alia, for the treatment of CNS disorders, such as anxiety.
    Type: Grant
    Filed: January 7, 1993
    Date of Patent: August 23, 1994
    Assignee: John Wyeth & Brother, Limited
    Inventor: Ian A. Cliffe
  • Patent number: 5340809
    Abstract: A compound selected from those of formula (I): ##STR1## with R.sub.1, R.sub.2 and n as defined in the description, and medicinal products containing the same useful in treating or in preventing a disorder resulting from cellular damages following upon ischemia, hypoxia, or anoxia.
    Type: Grant
    Filed: August 13, 1992
    Date of Patent: August 23, 1994
    Assignee: ADIR et Compagnie
    Inventors: Michel Gaudry, Bruno Pfeiffer, Pierre Renard, Jean-Francois Renaud de la Faverie, Gerard Adam
  • Patent number: 5340822
    Abstract: The invention relates to polycyclic amine compounds of formula (I) ##STR1## where Y. m. Ar', n, p, Q, T, q and Z are defined herein. The invention also relates to methods of making the compounds of formula (I) and pharmaceutical compositions which contain the compounds of formula (I). The inventive compounds are useful as neurokinin receptor antagonists, and are useful for the treatment of any substance P-dependent and neurokinin-dependent pathological condition.
    Type: Grant
    Filed: May 4, 1992
    Date of Patent: August 23, 1994
    Assignee: Elf Sanofi
    Inventors: Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto, Pierre Goulaouic, deceased, by Marie Bousquet, heir, by Catherine M. L. Goulaouic, heir
  • Patent number: 5332732
    Abstract: Compounds of the general formula I ##STR1## wherein A is N; Ar is aryl, substituted aryl or benzofuranyl, wherein the substituents are selected from C.sub.1 -C.sub.8 alkoxy; B is CO or CH.sub.2 and HET is selected from any of piperizine, piperidine, hexahydroazepine, morpholine, thiomorpholine or pyrrolidine, which may be substituted with one of more oxo groups are disclosed as novel antipsychotic agents. Pharmaceutical compositions and methods of treating convulsions employing such compounds of formula I are also disclosed.
    Type: Grant
    Filed: September 11, 1992
    Date of Patent: July 26, 1994
    Assignee: McNeilab, Inc.
    Inventors: Malcolm K. Scott, Allen B. Reitz, Frank J. Villani, Jr., C. Royce Rasmussen
  • Patent number: 5324725
    Abstract: Pharmacologically active compounds having anti-allergic properties corresponding to the formula I ##STR1## which can be mono- or disubstituted in the phenyl ring and their acid addition salts and/or S-mono- or dioxides of sulfur-containing compounds of the formula I are described, together with processes and intermediates for their preparation.
    Type: Grant
    Filed: August 21, 1992
    Date of Patent: June 28, 1994
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Daniel Jasserand, Dominique Paris, Patrice Demonchaux, Michel Cottin, Francois Floc'H, Pierre Dupassieux, Richard White
  • Patent number: 5322943
    Abstract: Disclosed are .DELTA..sup.9(11) -steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C.sub.17 -side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), .DELTA..sup.16 -steroids (IIIa and IIIb), reduced A-ring steroids (IV), .DELTA..sup.17(20) -steroids (Va and Vb) and .DELTA..sup.9(11) -steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.
    Type: Grant
    Filed: August 26, 1991
    Date of Patent: June 21, 1994
    Assignee: The Upjohn Company
    Inventors: John M. McCall, E. Jonathan Jacobsen, Frederick J. VanDoornik, John R. Palmer
  • Patent number: 5314889
    Abstract: A 2-Acylaminothiazole of formula: ##STR1## in which R.sub.1 is H, an alkyl or a substituted alkyl; R.sub.IV is a cycloalkyl, an aromatic group such as phenyl or a heterocyclic group which are unsubstituted or substituted; R.sub.V is a substituted alkyl, a substituted carboxy such as an ester or an amide; or R.sub.IV and R.sub.V together represent a phenoxyalkylene group which may be substituted on the phenyl; and Z is a heterocyclic e.g. indolyl group; or a salt of compound (I).
    Type: Grant
    Filed: May 29, 1992
    Date of Patent: May 24, 1994
    Assignee: Elf Sanofi
    Inventors: Robert Boigegrain, Roger Brodin, Danielle Gully, Jean-Charles Molimard, Dominique Olliero
  • Patent number: 5314885
    Abstract: Compounds of the general formula I ##STR1## are disclosed as novel antipsychotic agents. Pharmaceutical compositions and methods of treating convulsions employing such compounds of formula I are also disclosed.
    Type: Grant
    Filed: September 11, 1992
    Date of Patent: May 24, 1994
    Assignee: McNeilab, Inc.
    Inventors: Malcolm K. Scott, Allen B. Reitz, Cynthia A. Maryanoff, Frank J. Villani, Jr.
  • Patent number: 5302593
    Abstract: Aminoalkylcarbamic esters of eseroline suitable for use as cholinesterase activity inhibitors, having general formula (I) ##STR1## where R stands for an amine selected out of the group consisting of ##STR2## and n, R1, R2, R3, and R4 are as defined in the text.
    Type: Grant
    Filed: June 23, 1993
    Date of Patent: April 12, 1994
    Assignee: Mediolanum Farmaceutici S.p.A.
    Inventors: Maria A. Alisi, Mario Brufani, Maria C. Cesta, Luigi Filocamo, Gianluca Gostoli, Sperandina Lappa, Pier Giuseppe Pagella, Enrico Ferrari, Stefano Maiorana, Donata Marchesini
  • Patent number: 5292739
    Abstract: The present invention relates to heterocyclic compounds, characterized in that they have the general formula I ##STR1## Wherein Ar, n and Z.sub.1 -Z.sub.6 are defined in the specification, are disclosed to have pharmaceutical activity on the central nervous system.
    Type: Grant
    Filed: January 27, 1992
    Date of Patent: March 8, 1994
    Assignee: Laboratorios del Dr. Esteve, S.A.
    Inventors: Ramon Merce-Vidal, Jordi Frigola-Constansa, Juan Pares-Corominas
  • Patent number: 5292726
    Abstract: Diacylpiperazines of general structure ##STR1## are: angiotensin II (A-II) antagonists selective for the type 2 (AT.sub.2) subtype useful in the treatment of cerebrovascular, cognitive, and CNS disorders; tachykinin receptor antagonists useful in the treatment of inflammatory diseases and pain or migraine; and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
    Type: Grant
    Filed: May 19, 1992
    Date of Patent: March 8, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Wallace T. Ashton, Conrad P. Dorn, William J. Greenlee, Malcolm MacCoss, Sander G. Mills, Mu T. Wu
  • Patent number: 5292756
    Abstract: A series of non-peptide derivatives of the formula ##STR1## that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet anti-aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.
    Type: Grant
    Filed: March 25, 1992
    Date of Patent: March 8, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, Melissa S. Egbertson, Wasyl Halczenko, George D. Hartman
  • Patent number: 5286728
    Abstract: Amino-substituted piperazine derivatives of formula I ##STR1## wherein R.sub.1 -R.sub.6, X and Y are as defined in the description, and salts thereof, have properties inhibiting the biosynthesis of interleukin-1 (IL-1) as well as analgesic properties and can therefore be used as active ingredients in medicaments. They are prepared in a manner known per se.
    Type: Grant
    Filed: July 14, 1992
    Date of Patent: February 15, 1994
    Assignee: Ciba-Geigy Corporation
    Inventor: Pier G. Ferrini
  • Patent number: 5273982
    Abstract: Acetic acid derivatives of formulaH.sub.2 N(NH)C--X--Y--CO--Z--CH(Q.sup.1)COOQ.sup.2 Iand hydrates, solvates and physiologically acceptable salts thereof are useful to inhibit the binding of adhesive proteins to blood platelets and also to inhibit blood platelet aggregation and cell-cell adhesion.
    Type: Grant
    Filed: March 5, 1991
    Date of Patent: December 28, 1993
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Albrecht Edenhofer, Marcel Muller, Arnold Trzeciak, Thomas Weller
  • Patent number: 5268477
    Abstract: The claimed invention is to triazin-2-yl and triazin-3-yl piperazines which are useful intermediates in the preparation of amino substituted steroid (XI) which are useful pharmaceutical agents.
    Type: Grant
    Filed: November 19, 1992
    Date of Patent: December 7, 1993
    Assignee: The Upjohn Company
    Inventors: John M. McCall, Donald E. Ayer, E. Jon Jacobsen, Frederick J. VanDoornik, John R. Palmer, Harold A. Karnes
  • Patent number: 5254550
    Abstract: A novel prolinal derivative of the general formula: ##STR1## [wherein A represents alkylene or alkenylene group of from 1 to 8 carbon atom(s) or a saturated hydrocarbon ring of from 3 to 7 carbon atoms,R represents hydrogen atom, phenyl group, benzyl group, alkyl group of from 1 to 8 carbon atom(s) or cycloalkyl group of from 3 to 7 carbon atoms,B represents alkylene group of from 1 to 8 atom(s) unsubstituted or substituted by phenyl group or benzyl group, or a single bond,D represents carbocyclic or heterocyclic ring unsubstituted or substituted by from one to three of halogen atom, alkyl or alkoxy group of from 1 to 4 carbon atom(s), nitro group or trifluoromethyl group]posses inhibitory activity on prolyl endopeptidase, and therefore are useful for treating and/or preventing agent for amnesia.
    Type: Grant
    Filed: December 6, 1991
    Date of Patent: October 19, 1993
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Masaaki Toda, Shuichi Ohuchida, Hiroyuki Ohno
  • Patent number: 5250528
    Abstract: This invention relates to new aminopiperazine derivatives having the potentiation of the cholinergic activity and represented by the general formula [I]: ##STR1## wherein R.sup.1 is lower alkyl, aryl, ar(lower)alkoxy or a heterocyclic group, each of which may be substituted with halogen,R.sup.2 is hydrogen or lower alkyl,R.sup.3 is cyclo(lower)alkyl, aryl or ar(lower)-alkyl, each of which may be substituted with halogen,A is ##STR2## or lower alkylene, and Y is ##STR3## and pharmaceutically acceptable salts thereof, to processes for the preparation thereof and to a pharmaceutical composition comprising the same.
    Type: Grant
    Filed: October 8, 1992
    Date of Patent: October 5, 1993
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Teruo Oku, Eishiro Todo, Yoshihiro Yokota, Hiroshi Kayakiri, Masashi Hashimoto
  • Patent number: 5248692
    Abstract: Novel DC-89 derivatives as shown below have an excellent anti-tumor activity, and thus are useful as anti-tumor agent ##STR1## wherein L represents chlorine or bromine; R represents ##STR2## (wherein n represents an integer of 4 to 7) or ##STR3## (wherein Y represents oxygen or N--M).
    Type: Grant
    Filed: March 1, 1993
    Date of Patent: September 28, 1993
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Hiromitsu Saito, Akira Asai, Satoru Nagamura, Eiji Kobayashi, Katsushige Gomi
  • Patent number: 5227486
    Abstract: The present invention relates to a process for the preparation of aryl (or heteroaryl) piperazinyl-butylazole derivatives corresponding to the general formula I ##STR1## in which Ar denotes a nitrogenous or other aromatic radical chosen from differently substituted aryls, differently substituted 2-pyrimidine, 2-N-methyl-imidazole and 3-(1,2-benzisothiazole)Z.sub.1 denotes a nitrogen atom or an optionally substituted carbon atom which may be denoted by: C-R.sub.1Z.sub.2 denotes a nitrogen atom or an optionally substituted carbon atom which may be denoted by: C-R.sub.2Z.sub.4 denotes a nitrogen atom or an optionally substituted carbon atom which may be denoted by: C-R.sub.4 and R.sub.1, R.sub.2, R.sub.3 and R.sub.
    Type: Grant
    Filed: March 6, 1992
    Date of Patent: July 13, 1993
    Assignee: Laboratorios Del Dr. Esteve, S.A.
    Inventors: Ramon Merce-Vidal, Jordi Frigola-Constansa, Juan Pares-Corominas
  • Patent number: 5223517
    Abstract: Heterocyclically substituted cycloalkano[b]-indolesulphonamides can be prepared by reaction of appropriate N-unsubstituted indoles with acrylonitrile, followed by hydrolysis, esterification or amidation, or by reaction of heterocyclically substituted hydrazines with cycloalkanones or by subsequent introduction of the heterocyclic group into appropriate indole derivatives. The heterocyclically substituted cycloalkano[b]-indolesulphonamides can be employed for the treatment of thromboembolic disorders, ischaemias, arteriosclerosis, asthma, allergies and for the prophylaxis of myocardial infarcts.
    Type: Grant
    Filed: August 23, 1991
    Date of Patent: June 29, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich E. Muller, Ulrich Niewohner, Elisabeth Perzborn, Erwin Bischoff, Hans-Georg Dellweg
  • Patent number: 5210193
    Abstract: 7-(substituted)piperazinyl-1-ethyl-6-fluoro-4-oxo-3-quinolinecarboxylic acids, the pharmacologically acceptable salts thereof, compositions containing them, processes and intermediates for producing them, and methods of using them to treat bacterial infections in warm-blooded animals.
    Type: Grant
    Filed: March 16, 1990
    Date of Patent: May 11, 1993
    Assignee: American Cyanamid Company
    Inventors: Phaik-Eng Sum, Joseph P. Joseph, Carl B. Ziegler, Jr., Daniel B. Moran, Yang-I Lin
  • Patent number: 5204341
    Abstract: 1-arylsulphonyl-2-pyrrolidone derivatives for treating spasmodic disorders in gastro-enterology, in gynaecology, in obstetrics, in urology; intermediates in the preparation of such products; methods for preparing such products and pharmaceutical preparations containing such products.
    Type: Grant
    Filed: December 11, 1991
    Date of Patent: April 20, 1993
    Assignee: Roussel Uclaf
    Inventors: Emilio Toja, Carla Bonetti, Fernando Barzaghi, Giulio Galliani
  • Patent number: 5202345
    Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is hydrogen, or C.sub.1 14 C.sub.6 alkyl; n is an integer of from 2 to 3; Z.sup.1 is phenyl, benzyl, or isoxazolyl and each is optionally substituted by a halogen, a methoxy, or a methyl group; Z.sup.2 is hydrogen, C.sub.1 -C.sub.5 alkyl, allyl, unsubstituted phenyl, or phenyl substituted by halogen, methyl, or methoxy; orZ.sub.1 and Z.sub.2 are taken together with the adjacent nitrogen atom to form triazolyl, imidazolyl or pyrazolyl; or a pharmaceutically acceptable acid addition salt thereof.
    Type: Grant
    Filed: February 7, 1992
    Date of Patent: April 13, 1993
    Assignee: Shionogi & Co., Ltd.
    Inventors: Hiromu Matsumura, Toshisada Yano, Akira Matsushita, Masami Eigyo
  • Patent number: 5202321
    Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, psoriasis, uveitis and allograft rejection and in preventing the formation of atherosclerotic plaques.
    Type: Grant
    Filed: June 13, 1991
    Date of Patent: April 13, 1993
    Assignee: Merck Frosst Canada, Inc.
    Inventors: John H. Hutchinson, Yves Girard, Rejean Fortin, Dwight MacDonald, John Scheigetz, Daniel Delorme, Michel Therien, Pierre Hamel
  • Patent number: 5202437
    Abstract: The present invention concerns intermediates in the preparation of novel 3-pyrrolidinylthio-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid compounds and pharmaceutically acceptable salts thereof. The novel 3-pyrrolidinylthio-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid compounds and pharmaceutically acceptable salts thereof show antimicrobial activity.
    Type: Grant
    Filed: March 6, 1990
    Date of Patent: April 13, 1993
    Assignee: Fujisawa Pharmaceutical Company, Ltd.
    Inventors: Masayoshi Murata, Hideo Tsutsumi, Keiji Matsuda, Kohji Hattori, Takashi Nakajima
  • Patent number: 5192763
    Abstract: [(1-Arylpyrrolidin-2-yl)methyl]piperazine compounds corresponding to the formula ##STR1## in which Z denotes a group of formula N-R.sub.1 in which R.sub.1 is either a hydrogen atom or a C.sub.1-3 alkyl group or a group of formula Ar--C.sub.n H.sub.2n in which n denotes 0, 1 or 2 and Ar denotes a phenyl group optionally substituted by one or more halogen atoms and/or C.sub.1-3 alkyl or C.sub.1-3 alkoxy radicals, or a group of formula COR.sub.2 in which R.sub.2 denotes the CH.sub.3, C.sub.6 H.sub.5, CH.sub.2 C.sub.6 H.sub.5 or OC.sub.2 H.sub.5 group and their salts of addition to pharmaceutically acceptable acids. The compounds are useful for the treatment of neurological disorders.
    Type: Grant
    Filed: June 6, 1991
    Date of Patent: March 9, 1993
    Assignee: Synthelabo
    Inventors: Pascal George, Jacques Menin, Jean-Pierre Merly, Dennis Bigg, Daniel Obitz, Michel Peynot, Corinne Veronique
  • Patent number: 5180418
    Abstract: Cycloalkanecarboxylic acid derivatives of formula I ##STR1## wherein W is ##STR2## and A is CO--R.sub.3 or CN; R.sub.1 is hydrogen or fluorine; R.sub.2 is halogen or cyano; R.sub.3 is chlorine, X--R.sub.5, amino, C.sub.1 -C.sub.4 alkylamino, d-C.sub.1 -C.sub.4 alkylamino, C.sub.2 -C.sub.4 haloalkylamino, di-C.sub.2 -C.sub.4 haloalkylamino, C.sub.1 -C.sub.4 hydroxyalkylamino, di-C.sub.1 -C.sub.4 hydroxyalkylamino, C.sub.3 -C.sub.4 alkenylamino, diallylamino, --N-pyrrolidino, --N-piperidino, --N-morpholino, --N-thiomorpholino, --N-piperidazino, the group --O--N.dbd.C--(R.sub.9)R.sub.10 or the group --N--R.sub.6 (OR.sub.6); each of R.sub.4 and R.sub.14, independently of the other, is hydrogen, fluorine, chlorine, bromine, C.sub.1 -C.sub.4 alkyl or trifluoromethyl; R.sub.5 is hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.4 alkoxy-C.sub.1 -C.sub.4 alkyl, halo-C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.10 alkylthio-C.sub.1 -C.sub.4 alkyl, di-C.sub.1 -C.sub.4 alkylamino-C.sub.1 -C.sub.4 alkyl, cyano-C.sub.1 -C.sub.
    Type: Grant
    Filed: July 19, 1991
    Date of Patent: January 19, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Georg Pissiotas, Hans Moser, Hans-Georg Brunner, Eginhard Steiner
  • Patent number: 5177078
    Abstract: Compounds of formula ##STR1## where A is an alkylene chain of 1 or 2 carbon atoms optionally substituted by one or more lower alkyl groups,R is hydrogen or lower alkyl,R.sup.1 is an aryl or heteroaryl radical,R.sup.2 is a mono- or bicyclic heterocyclic radical,R.sup.3 is hydrogen, lower alkyl or hydroxy andR.sup.4 is a aryl or heteroaryl radical,and their pharmaceutically acceptable acid addition salts are 5-HT.sub.1A binding agents which may be used, for example, for the treatment of CNS--disorders such as anxiety.
    Type: Grant
    Filed: September 30, 1991
    Date of Patent: January 5, 1993
    Assignee: John Wyeth & Brother Limited
    Inventors: Terence J. Ward, Graham J. Warrellow
  • Patent number: 5175285
    Abstract: A conversion product of polysuccinimide useful as coating material for medicinal preparations and foodstuffs having the structure: ##STR1## wherein A is hydrogen or a straight or branched alkyl or alkylene group of 1 to 8 carbon atoms, optionally substituted by cycloaliphatic or aromatic groups, wherein the cyclic substituent can also contain heteroatoms, or by R--O--, ##STR2## or R.sub.3 R.sub.4 N groups, wherein R, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are hydrogen or branched alkyl or cycloalkyl groups each of which may contain oxygen and nitrogen atoms in the chain or in the ring of 1 to 10 carbon atoms;B is hydrogen or straight or branched chain alkyl or alkenyl, and is the same or different from A;D is hydrogen, NH.sub.4, ##STR3## wherein A and B have the aforementioned meanings, or an alkali metal ion; anda is 0.2 to 1 and b is 0.8 to 0.
    Type: Grant
    Filed: July 5, 1990
    Date of Patent: December 29, 1992
    Assignee: Rohm GmbH Chemische Fabrik
    Inventors: Klaus Lehmann, Rdiger Jelitte, Joachim Knebel
  • Patent number: 5169845
    Abstract: Piperazine derivative of formula ##STR1## and the pharmaceutically acceptable acid addition salts, where A is an alkylene chain of 1 or 2 carbon atoms optionally substituted by one or more lower alkyl groups, m is 0, 1 or 2, R is hydrogen or lower alkyl, R.sup.1 is aryl or a mono- or bicyclic heteroaryl radical, R.sup.2 is hydrogen or lower alkyl, R.sup.3 is a heteroaryl radical, R.sup.4 is hydrogen, lower alkyl or aryl, and R.sup.5 is hydrogen, lower alkyl, cycloalkyl, cycloalkyl(lower)alkyl, aryl, or aryl(lower)alkyl or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are both attached represent a saturated heterocyclic ring which may contain a further hetero atom are 5--HT.sub.1A -binding agents and may be used, for example, as anxiolytics.
    Type: Grant
    Filed: September 30, 1991
    Date of Patent: December 8, 1992
    Assignee: John Wyeth & Brother Limited
    Inventors: Ian A. Cliffe, Graham J. Warrellow
  • Patent number: 5166359
    Abstract: An optical recording medium contains novel azulenemethine dyes of the formula ##STR1## where R is unsubstituted or substituted C.sub.1 -C.sub.6 -alkyl, X.sup..crclbar. is an anion, A.sup..sym. is heterocyclic radical, of the formula ##STR2## wherein R.sup.1, R.sup.2, R.sup.3, Y, Z and W are as defined, with the proviso that, when A.sup..sym. is a radical of the formula II f, II g, II i or II k, m is 2, A is 1, 2 or 3 and M is 1 or 2.
    Type: Grant
    Filed: March 28, 1991
    Date of Patent: November 24, 1992
    Assignee: BASF Aktiengesellschaft
    Inventors: Michael Acker, Peter Neumann, Wolfgang Schrott, Matthias Dust
  • Patent number: 5166204
    Abstract: A novel isoindole derivative represented by general formula [1] or a salt thereof: ##STR1## which has an excellent antitumor activity and low toxicity.
    Type: Grant
    Filed: October 30, 1990
    Date of Patent: November 24, 1992
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Takashi Nagai, Isao Myoukan, Keishi Funaki, Kenji Ohta, Nobuhisa Taya, Shinji Miyabara, Masaaki Shibata, Hidetada Mikami, Takako Hori
  • Patent number: 5166205
    Abstract: The present invention relates to novel derivatives of 1-diphenylmethyl piperazinyl, characterized in that they correspond to the general formula I, and their therapeutically acceptable salts, ##STR1## in which: R.sub.1 and R.sub.2, equal or different, represent a hydrogen atom, a halogen, a lower alkyl radical, a hydroxy radical, an alkoxy radical, an alkyl carboxylate radical, an aryl or substituted aryl radical,n may have the values 2 to 4,X, Y, Z and W, equal or different, represent a nitrogen atom or a carbon atom linked to a hydrogen atom, a halogen or to another alkyl, aryl, carboxyalkyl, carbonyl, hydroxyl, sulfonyl and alkylsulfonyl radical.The present invention also relates to the process of preparing these compounds and their use for the manufacture of medicaments intended for prophylaxis and for the treatment of various allergic disorders caused by histamine.
    Type: Grant
    Filed: July 25, 1991
    Date of Patent: November 24, 1992
    Assignee: Laboratorios Del Dr. Esteve, S. A.
    Inventors: Maria R. Cuberes-Altisent, Jordi Frigola-Constansa, Juan Pares-Corominas
  • Patent number: 5149808
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 4 carbon atoms; R.sub.2 is 2-, 3- or 4-pyridyl, phenyl or mono- or di-substituted phenyl, where the substituents are each individually alkoxy of 1 to 2 carbon atoms, fluorine, chlorine, bromine, trifluoromethyl, alkyl or 1 to 4 carbon atoms, hydroxyl or nitro; andR.sub.3 and R.sub.4 are each independently hydrogen or alkyl of 1 to 4 carbon atoms; orR.sub.3 and R.sub.4, together with each other and the nitrogen atom to which they are attached, form an unsubstituted or methyl-substituted, saturated 5- or 6-membered heterocycle which may contain an additional oxygen or nitrogen heteroatom, or form an imidazole ring;where the aminomethyl substituent is attached to the 4- or 5-position or the pyrrolidine ring, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as the salts are useful as nootropics and antihypoxics.
    Type: Grant
    Filed: September 4, 1991
    Date of Patent: September 22, 1992
    Assignee: Boehringer Ingelheim KG
    Inventors: Karl-Heinz Weber, Gerhard Walther, Claus Schneider, Dieter Hinzen, Franz J. Kuhn, Erich Lehr