Five-membered Hetero Ring Consisting Of One Nitrogen And Four Carbons Patents (Class 544/372)
-
Patent number: 5428037Abstract: 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: GrantFiled: April 9, 1993Date of Patent: June 27, 1995Assignee: Syntex Pharmaceuticals, Ltd.Inventors: Jean-Claude Pascal, Gary McCort, Dominique Blondet, Francoise Gellibert
-
Patent number: 5424451Abstract: 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: GrantFiled: January 4, 1994Date of Patent: June 13, 1995Assignee: 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: 5418236Abstract: 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: GrantFiled: December 23, 1993Date of Patent: May 23, 1995Assignee: Ortho Pharmaceutical CorporationInventors: Richard J. Carmosin, John R. Carson, Philip Pitis
-
Patent number: 5413999Abstract: 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: GrantFiled: May 7, 1993Date of Patent: May 9, 1995Assignee: Merck & Co., Inc.Inventors: Joseph P. Vacca, Bruce D. Dorsey, James P. Guare, M. Katharine Holloway, Randall W. Hungate, Rhonda B. Levin
-
Patent number: 5414082Abstract: 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: GrantFiled: August 11, 1993Date of Patent: May 9, 1995Assignee: Arzneimittelwerk Dresden GmbHInventors: Andreas Rolfs, Jurger Liebscher, Klaus Unverferth, Gottfried Faust
-
Patent number: 5413997Abstract: 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: GrantFiled: January 21, 1993Date of Patent: May 9, 1995Assignee: 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: 5387593Abstract: Novel piperazinyl- and piperidinyl-cyclohexanols of the following formula are useful as anxiolytic agents and have other psychotropic properties ##STR1##Type: GrantFiled: February 17, 1994Date of Patent: February 7, 1995Assignee: Briston-Myers SquibbInventors: Ronald J. Mattson, John D. Catt
-
Patent number: 5384319Abstract: 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: GrantFiled: December 20, 1993Date of Patent: January 24, 1995Assignee: Ciba-Geigy CorporationInventor: Pier G. Ferrini
-
Patent number: 5382583Abstract: 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: GrantFiled: December 29, 1992Date of Patent: January 17, 1995Assignee: John Wyeth & Brother, LimitedInventor: Ian A. Cliffe
-
Patent number: 5380726Abstract: 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: GrantFiled: December 20, 1993Date of Patent: January 10, 1995Assignee: Ciba-Geigy CorporationInventor: Pier G. Ferrini
-
Patent number: 5373008Abstract: 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: GrantFiled: January 27, 1993Date of Patent: December 13, 1994Assignee: The Boots Compant plc.Inventor: Balasubramanian Gopalan
-
Patent number: 5369103Type: GrantFiled: June 19, 1992Date of Patent: November 29, 1994Assignee: John Wyeth & Brother, LimitedInventors: Ian A. Cliffe, Alan C. White, Anderson D. Ifill
-
Patent number: 5364849Abstract: 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: GrantFiled: July 10, 1992Date of Patent: November 15, 1994Assignee: John Wyeth & Brother, LimitedInventor: Ian A. Cliffe
-
Patent number: 5356893Abstract: 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: GrantFiled: September 17, 1992Date of Patent: October 18, 1994Assignee: Glaxo Group LimitedInventors: John Bradshaw, John W. Clitherow, Ian B. Campbell
-
Patent number: 5350762Abstract: 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: GrantFiled: March 8, 1993Date of Patent: September 27, 1994Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Lawrence L. Martin, Larry Davis
-
Patent number: 5344830Abstract: 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: GrantFiled: December 10, 1992Date of Patent: September 6, 1994Assignee: Merck & Co., Inc.Inventors: Sander G. Mills, Richard J. Budhu, Conrad P. Dorn, William J. Greenlee, Malcolm MacCoss, Mu T. Wu
-
Patent number: 5340812Abstract: 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: GrantFiled: January 7, 1993Date of Patent: August 23, 1994Assignee: John Wyeth & Brother, LimitedInventor: Ian A. Cliffe
-
Patent number: 5340809Abstract: 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: GrantFiled: August 13, 1992Date of Patent: August 23, 1994Assignee: ADIR et CompagnieInventors: Michel Gaudry, Bruno Pfeiffer, Pierre Renard, Jean-Francois Renaud de la Faverie, Gerard Adam
-
Patent number: 5340822Abstract: 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: GrantFiled: May 4, 1992Date of Patent: August 23, 1994Assignee: Elf SanofiInventors: Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto, Pierre Goulaouic, deceased, by Marie Bousquet, heir, by Catherine M. L. Goulaouic, heir
-
Patent number: 5332732Abstract: 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: GrantFiled: September 11, 1992Date of Patent: July 26, 1994Assignee: McNeilab, Inc.Inventors: Malcolm K. Scott, Allen B. Reitz, Frank J. Villani, Jr., C. Royce Rasmussen
-
Patent number: 5324725Abstract: 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: GrantFiled: August 21, 1992Date of Patent: June 28, 1994Assignee: Kali-Chemie Pharma GmbHInventors: Daniel Jasserand, Dominique Paris, Patrice Demonchaux, Michel Cottin, Francois Floc'H, Pierre Dupassieux, Richard White
-
Patent number: 5322943Abstract: 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: GrantFiled: August 26, 1991Date of Patent: June 21, 1994Assignee: The Upjohn CompanyInventors: John M. McCall, E. Jonathan Jacobsen, Frederick J. VanDoornik, John R. Palmer
-
Patent number: 5314889Abstract: 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: GrantFiled: May 29, 1992Date of Patent: May 24, 1994Assignee: Elf SanofiInventors: Robert Boigegrain, Roger Brodin, Danielle Gully, Jean-Charles Molimard, Dominique Olliero
-
Patent number: 5314885Abstract: 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: GrantFiled: September 11, 1992Date of Patent: May 24, 1994Assignee: McNeilab, Inc.Inventors: Malcolm K. Scott, Allen B. Reitz, Cynthia A. Maryanoff, Frank J. Villani, Jr.
-
Patent number: 5302593Abstract: 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: GrantFiled: June 23, 1993Date of Patent: April 12, 1994Assignee: 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: 5292739Abstract: 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: GrantFiled: January 27, 1992Date of Patent: March 8, 1994Assignee: Laboratorios del Dr. Esteve, S.A.Inventors: Ramon Merce-Vidal, Jordi Frigola-Constansa, Juan Pares-Corominas
-
Patent number: 5292726Abstract: 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: GrantFiled: May 19, 1992Date of Patent: March 8, 1994Assignee: Merck & Co., Inc.Inventors: Wallace T. Ashton, Conrad P. Dorn, William J. Greenlee, Malcolm MacCoss, Sander G. Mills, Mu T. Wu
-
Patent number: 5292756Abstract: 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: GrantFiled: March 25, 1992Date of Patent: March 8, 1994Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, Melissa S. Egbertson, Wasyl Halczenko, George D. Hartman
-
Patent number: 5286728Abstract: 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: GrantFiled: July 14, 1992Date of Patent: February 15, 1994Assignee: Ciba-Geigy CorporationInventor: Pier G. Ferrini
-
Patent number: 5273982Abstract: 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: GrantFiled: March 5, 1991Date of Patent: December 28, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Leo Alig, Albrecht Edenhofer, Marcel Muller, Arnold Trzeciak, Thomas Weller
-
Patent number: 5268477Abstract: 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: GrantFiled: November 19, 1992Date of Patent: December 7, 1993Assignee: The Upjohn CompanyInventors: John M. McCall, Donald E. Ayer, E. Jon Jacobsen, Frederick J. VanDoornik, John R. Palmer, Harold A. Karnes
-
Patent number: 5254550Abstract: 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: GrantFiled: December 6, 1991Date of Patent: October 19, 1993Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Masaaki Toda, Shuichi Ohuchida, Hiroyuki Ohno
-
Patent number: 5250528Abstract: 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: GrantFiled: October 8, 1992Date of Patent: October 5, 1993Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Teruo Oku, Eishiro Todo, Yoshihiro Yokota, Hiroshi Kayakiri, Masashi Hashimoto
-
Patent number: 5248692Abstract: 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: GrantFiled: March 1, 1993Date of Patent: September 28, 1993Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Hiromitsu Saito, Akira Asai, Satoru Nagamura, Eiji Kobayashi, Katsushige Gomi
-
Patent number: 5227486Abstract: 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: GrantFiled: March 6, 1992Date of Patent: July 13, 1993Assignee: Laboratorios Del Dr. Esteve, S.A.Inventors: Ramon Merce-Vidal, Jordi Frigola-Constansa, Juan Pares-Corominas
-
Patent number: 5223517Abstract: 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: GrantFiled: August 23, 1991Date of Patent: June 29, 1993Assignee: Bayer AktiengesellschaftInventors: Ulrich E. Muller, Ulrich Niewohner, Elisabeth Perzborn, Erwin Bischoff, Hans-Georg Dellweg
-
Patent number: 5210193Abstract: 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: GrantFiled: March 16, 1990Date of Patent: May 11, 1993Assignee: American Cyanamid CompanyInventors: Phaik-Eng Sum, Joseph P. Joseph, Carl B. Ziegler, Jr., Daniel B. Moran, Yang-I Lin
-
Patent number: 5204341Abstract: 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: GrantFiled: December 11, 1991Date of Patent: April 20, 1993Assignee: Roussel UclafInventors: Emilio Toja, Carla Bonetti, Fernando Barzaghi, Giulio Galliani
-
Patent number: 5202345Abstract: 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: GrantFiled: February 7, 1992Date of Patent: April 13, 1993Assignee: Shionogi & Co., Ltd.Inventors: Hiromu Matsumura, Toshisada Yano, Akira Matsushita, Masami Eigyo
-
Patent number: 5202321Abstract: 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: GrantFiled: June 13, 1991Date of Patent: April 13, 1993Assignee: Merck Frosst Canada, Inc.Inventors: John H. Hutchinson, Yves Girard, Rejean Fortin, Dwight MacDonald, John Scheigetz, Daniel Delorme, Michel Therien, Pierre Hamel
-
Patent number: 5202437Abstract: 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: GrantFiled: March 6, 1990Date of Patent: April 13, 1993Assignee: Fujisawa Pharmaceutical Company, Ltd.Inventors: Masayoshi Murata, Hideo Tsutsumi, Keiji Matsuda, Kohji Hattori, Takashi Nakajima
-
Patent number: 5192763Abstract: [(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: GrantFiled: June 6, 1991Date of Patent: March 9, 1993Assignee: SynthelaboInventors: Pascal George, Jacques Menin, Jean-Pierre Merly, Dennis Bigg, Daniel Obitz, Michel Peynot, Corinne Veronique
-
Patent number: 5180418Abstract: 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: GrantFiled: July 19, 1991Date of Patent: January 19, 1993Assignee: Ciba-Geigy CorporationInventors: Georg Pissiotas, Hans Moser, Hans-Georg Brunner, Eginhard Steiner
-
Patent number: 5177078Abstract: 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: GrantFiled: September 30, 1991Date of Patent: January 5, 1993Assignee: John Wyeth & Brother LimitedInventors: Terence J. Ward, Graham J. Warrellow
-
Patent number: 5175285Abstract: 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: GrantFiled: July 5, 1990Date of Patent: December 29, 1992Assignee: Rohm GmbH Chemische FabrikInventors: Klaus Lehmann, Rdiger Jelitte, Joachim Knebel
-
Patent number: 5169845Abstract: 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: GrantFiled: September 30, 1991Date of Patent: December 8, 1992Assignee: John Wyeth & Brother LimitedInventors: Ian A. Cliffe, Graham J. Warrellow
-
Patent number: 5166359Abstract: 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: GrantFiled: March 28, 1991Date of Patent: November 24, 1992Assignee: BASF AktiengesellschaftInventors: Michael Acker, Peter Neumann, Wolfgang Schrott, Matthias Dust
-
Patent number: 5166204Abstract: A novel isoindole derivative represented by general formula [1] or a salt thereof: ##STR1## which has an excellent antitumor activity and low toxicity.Type: GrantFiled: October 30, 1990Date of Patent: November 24, 1992Assignee: 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: 5166205Abstract: 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: GrantFiled: July 25, 1991Date of Patent: November 24, 1992Assignee: Laboratorios Del Dr. Esteve, S. A.Inventors: Maria R. Cuberes-Altisent, Jordi Frigola-Constansa, Juan Pares-Corominas
-
Patent number: 5149808Abstract: 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: GrantFiled: September 4, 1991Date of Patent: September 22, 1992Assignee: Boehringer Ingelheim KGInventors: Karl-Heinz Weber, Gerhard Walther, Claus Schneider, Dieter Hinzen, Franz J. Kuhn, Erich Lehr