Ring Sulfur In The Polycyclo Ring System Patents (Class 546/202)
-
Patent number: 5446052Abstract: The invention relates to aromatic amino derivatives of formula ##STR1## wherein, R, T, Z, Ar', T', Z' are defined in the specification and their enantiomers, processes for their production and their use for the treatment of substance p- and neurokinin-dependent pathology.Type: GrantFiled: February 4, 1994Date of Patent: August 29, 1995Assignee: SanofiInventors: Xavier Emonds-Alt, Isabelle Grossriether, Vincenzo Proietto, Didier Van Broeck
-
Patent number: 5428043Abstract: Compounds of the formula ##STR1## wherein ring A, ring B, ring D, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6,R.sup.11, R.sup.12, R.sup.13, E, G, X and P are as defined below. The compounds of formula I are cholinesterase inhibitors and are useful in enhancing memory in patients suffering from dementia and Alzheimer's disease.Type: GrantFiled: October 29, 1992Date of Patent: June 27, 1995Assignee: Pfizer Inc.Inventor: Yuhpyng L. Chen
-
Patent number: 5428027Abstract: Certain substituted semicarbazones, including all geometric and stereoisomers thereof, agricultural compositions containing them and their use as arthropodicides.Type: GrantFiled: October 28, 1993Date of Patent: June 27, 1995Assignee: E. I. Du Pont de Nemours and CompanyInventors: John P. Daub, George P. Lahm, Bradford S. Marlin
-
Patent number: 5420132Abstract: A compound of formula (I): ##STR1## wherein: X represents O, S or H.sub.2,R and R' each represents hydrogen or together form a bond,R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in the description.useful in the treatment or prevention of disorders involving oxidative processes.Type: GrantFiled: May 6, 1994Date of Patent: May 30, 1995Assignee: Adir et CompagnieInventors: Gerald Guillaumet, Gerard Coudert, Valerie Thiery, Gerard Adam, Jean-Guy Bizot-Espiard, Bruno Pfeiffer, Pierre Renard
-
Patent number: 5405976Abstract: Dyes comprising an inner salt of a compound of the formula:Q.sup.1 =Z-Q.sup.2wherein:Q.sup.1 is a 4-(benz[b]-4H-pyrylium)methylidene, 4-(benz[b]-4H-thiopyrylium)methylidene or 4-(benz[b]-4H-selenopyrylium)methylidene grouping;Z is a 1,3-(2-hydroxy-4-oxo-2-cyclobutylidene) hydroxide or 1,3-(2-hydroxy-4,5-dioxo-2-cyclopentylidene) hydroxide ring; andQ.sup.2 is a 4-(benz[b]-4H-pyran-4-ylidene)methyl, 4-(benz[b]-4H-thiopyran-4-ylidene)methyl or 4-(benz[b]-4H-selenopyran-4-ylidene)methyl grouping;wherein at least one of the groupings Q.sup.1 and Q.sup.Type: GrantFiled: September 24, 1993Date of Patent: April 11, 1995Assignee: Polaroid CorporationInventors: Stephen J. Telfer, Robert P. Short, Stephen G. Stroud, Anthony J. Puttick, Socorro Ramos, Michael J. Zuraw
-
Patent number: 5403842Abstract: The invention relates to benzopyranone and benzothiopyranone compounds, compositions and methods of use which have adrenergic and serotonergic activity.Type: GrantFiled: May 26, 1992Date of Patent: April 4, 1995Assignee: Recordati S.A., Chemical and Pharmaceutical CompanyInventors: Amedeo Leonardi, Gianni Motta, Carlo Riva, Rodolfo Testa
-
Patent number: 5399360Abstract: A ketotifen pharmaceutical composition adapted for once-a-day oral administration e.g. based on a fat matrix.Type: GrantFiled: August 11, 1993Date of Patent: March 21, 1995Assignee: Sandoz Pharmaceuticals Corp.Inventors: Hansruedi Surer, Aldo Riva
-
Patent number: 5393890Abstract: A piperidine compound of the formula (I): ##STR1## wherein A is a fused aromatic ring; R is hydrogen, chloro or methoxy; X is (CH.sub.2).sub.n, which may be substituted, in which n is 0 or an integer of 1 to 10, --CH.dbd.CH--, --C.dbd.C--, --O--, --S--, --NH--, --N(COCH.sub.3)--, --N(COOC.sub.2 H.sub.5)--, --N(CHO)--, --N(CH.sub.3)--, --CO--, --SO--, or --SO.sub.2 --; Y is --CH.dbd.CH--, --CH.sub.2 CH.sub.2 --, --CH.sub.2 CO--, --O--, --S--, --NH--, --OCH.sub.2 --, --SCH.sub.2 --, --NHCH.sub.2 --, --CH(OH)CH.sub.2 -- or --CH(OH)CH(OH)--; and Q is substituted or unsubstituted n-hexyl, carboxypropyl, ethoxycarbonylpropyl, cyanopropyl, cyclohexyl, phenyl, indanyl, naphthyl, tetrahydronaphthyl, benzocycloheptyl, piperidinyl, tetrahydroisoquinolinyl, indolyl, pyrolyl, furyl, thienyl, thiazolyl, oxazolyl or N-methylpyrolyl, wherein any one or more of the --(CH.sub.2)-groups of the hexyl, carboxypropyl, ethoxycarbonylpropyl and cyanopropyl groups may be replaced by --CH.dbd.CH--, --C.dbd.Type: GrantFiled: July 1, 1994Date of Patent: February 28, 1995Assignee: Ajinomoto Co., Inc.Inventors: Masataka Syoji, Kozo Toyota, Chikahiko Eguchi, Ryoto Yoshimoto, Yoshikatsu Koyama, Hideki Domoto, Akira Kamimura
-
Patent number: 5385930Abstract: The invention relates to compounds of the formula I: ##STR1## in which R.sub.1 is as defined in the description, their optical isomers and their addition salts with a pharmaceutically-acceptable acid or base, and medicinal products which are useful for treating Central Nervous System disorders.Type: GrantFiled: January 14, 1994Date of Patent: January 31, 1995Assignee: Adir et CompagnieInventors: Gerald Guillaumet, Gerard Coudert, Tchao Podona, Beatrice Guardiola-Lemaitre, Pierre Renard, Gerard Adam, Daniel Henri-Caignard
-
Patent number: 5376677Abstract: The invention relates to novel compounds of the formula ##STR1## in which R is as defined in the description, to their preparation, to fungicidal compositions which contain such compounds as active substances, and to the use of the active substances or compositions for controlling fungi in agriculture and horticulture.Type: GrantFiled: March 22, 1993Date of Patent: December 27, 1994Assignee: Ciba-Geigy CorporationInventor: Stephan Trah
-
Patent number: 5371093Abstract: Piperidinyl thiacyclic derivatives ##STR1## wherein X, Y, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are defined in the specification. useful in the treatment of allergic diseases and diseases responding to antagonism of 5HT.sub.2 receptors, pharmaceutical compositions and a methods of treatment using these compounds.Type: GrantFiled: February 24, 1994Date of Patent: December 6, 1994Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Albert A. Carr, George D. Maynard, John M. Kane, Hsien C. Cheng, Mark W. Dudley
-
Patent number: 5356907Abstract: A compound selected from the group consisting of all possible racemic, enantiomeric and diastereoisomeric forms of a compound of the formula ##STR1## wherein E and G together form a group selected from the group: ##STR2## consisting of a) ##STR3## wherein, A is a cycloalkyl of 3-6 carbon optionally substituted, R, R.sub.1, R.sub.2 and Y are defined in the specification.Type: GrantFiled: October 1, 1992Date of Patent: October 18, 1994Assignee: Roussel UCLAFInventors: Francois Clemence, Michel Fortin, Odile Le Martret
-
Patent number: 5346908Abstract: Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower alkyl, benzyl, and haloloweralkyl; wherein each of R.sup.2, R.sup.3 and R.sup.8 through R.sup.11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is an integer of from four to six; wherein m is an integer of from two to four; wherein A is selected from phenyl, naphthyl, benzothienyl, benzofuranyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 25, 1992Date of Patent: September 13, 1994Assignees: National Institutes of Health, Brown UniversityInventors: Wayne Bowen, Brian R. de Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
-
Patent number: 5344835Abstract: According to the invention there is provided a compound of formula (I): R.sup.1 --O(CH.sub.2).sub.m A(CH.sub.2).sub.n XR or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is a group of formula (a or b) where Z is --(CH.sub.2).sub.2-, --CH.dbd.CH--, --CH.sub.2 --S-- or --CH.sub.2 --O--; R is a group of formula (c, d or Het) and A is a group of formula (e, f or g) in which the N atom is attached to the group (CH.sub.2)n; m is 1 or 2; n is an integer of from 1 to 4; p is 1, 2 or 3; R.sup.2 and R.sup.3 are each independently hydrogen, C.sub.1 -C.sub.4 alkyl, hydroxy-(C.sub.1 -C.sub.4 alkyl), hydroxy, C.sub.1 -C.sub.4 alkoxy, halo, trifluoromethyl, nitro, cyano, sulphamoyl, --CO(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.4 alkyl), carboxy, --CO.sub.2 (C.sub.1 -C.sub.4 alkyl), --CH.sub.2).sub.q CONR.sup.4 R.sup.5, -- (CH.sub.2).sub.q OCONR.sup.4 R.sup.5, --CH.sub.2).sub.q NR.sup.6 R.sup.7 or --NHSO.sub.2 NH.sub.2 in which R.sup.4 and R.sup.5 are each independently H or C.sub.1 -C.sub.Type: GrantFiled: July 2, 1992Date of Patent: September 6, 1994Assignee: Pfizer Inc.Inventors: David Alker, Peter E. Cross
-
Patent number: 5338735Abstract: Compounds of the formula: ##STR1## in which each R.sup.1 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or nitro, and n is 0, 1, 2 or 3, R.sup.2 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkenyl, R.sup.3 and R.sup.4 are each hydrogen, C.sub.1-4 alkyl, optionally substituted phenyl or C.sub.6-9 cycloalkyl optionally substituted by 1 to 4 C.sub.1-4 alkyl groups, R.sup.5 is optionally substituted phenyl, tetrahydronaphthyl, phthalimido, saccharinyl, glutaramido, C.sub.6-10 cycloalkyl optionally substituted with 1 to 4 C.sub.1-4 alkyl groups or a phenyl group, or C.sub.4-9 heterosubstituted cycloalkyl optionally substituted with 1 to 4 alkyl groups, x is 1, 2 or 3, y is 0 or 1 and z is 0, 1, 2 or 3; and salts thereof.The compounds are indicated for use in the treatment of disorders of the central nervous system.Type: GrantFiled: August 12, 1993Date of Patent: August 16, 1994Assignee: Lilly Industries LimitedInventors: John Fairhurst, David E. Tupper
-
Patent number: 5332741Abstract: The invention relates to compounds of the formula I: ##STR1## in which R.sub.1 is as defined in the description, their optical isomers and their addition salts with a pharmaceutically-acceptable acid or base, andmedicinal products which are useful for treating Central Nervous System disorders.Type: GrantFiled: May 17, 1993Date of Patent: July 26, 1994Assignee: Adir et CompagnieInventors: Gerald Guillaumet, Gerard Coudert, Tchao Podona, Beatrice Guardiola-Lemaitre, Pierre Renard, Gerard Adam, Daniel Henri-Caignard
-
Patent number: 5332743Abstract: Compounds of the general formula I: ##STR1## are disclosed as potent antipsychotic agents. Novel methods of use and intermediates used to make the compounds of formula I are also disclosed.Type: GrantFiled: June 12, 1992Date of Patent: July 26, 1994Assignee: McNeilab, Inc.Inventors: Ellen W. Baxter, Allen B. Reitz
-
Patent number: 5322848Abstract: A compound, or solvate or salt thereof, of formula ##STR1## R.sub.1 is hydrogen, halogen, or C.sub.1-6 alkyl; R.sub.2 and R.sub.3 are hydrogen or C.sub.1-6 alkyl;R.sub.5 together with R.sub.4 forms a --(CH).sub.2).sub.2 -- group optionally substituted by one or two C.sub.1-6 alkyl;W is halogen or when A is gem-dimethyl substituted piperidine, is OH;a is 1 or 2,useful in the treatment of pain.Type: GrantFiled: May 22, 1992Date of Patent: June 21, 1994Assignee: Dr. Lo Zembeletti S.p.A.Inventors: Robert Colle, Giulio Dondio, Giuseppe Giardina, Lorenzo Leurini, Vittorio Vecchietti
-
Patent number: 5306823Abstract: Novel compounds according to formula I ##STR1## are disclosed, as well as processes for their production and methods for their use.These compounds are useful as light stabilizers for polymeric materials, particularly in acid catalyzed stoving finishes such as those encountered in the top coat of two layer metallic finishes.Type: GrantFiled: February 14, 1992Date of Patent: April 26, 1994Assignee: Sandoz Ltd.Inventor: Lajos Avar
-
Patent number: 5300648Abstract: The invention relates to intermediates in the production of dialkylenepiperidino compounds and their enantiomers and their use for the treatment of substance p- and neurokinin-dependent pathology.Type: GrantFiled: May 4, 1992Date of Patent: April 5, 1994Assignee: Societe Anonyme: Elf SanofiInventors: Xavier Emonds-Alt, Isabelle Grossriether, Vincenzo Proietto, Didier Van Broeck
-
Patent number: 5286735Abstract: The application discloses pharmacologically-active derivatives of 4-aminomethyl piperidine having the general formula 1 ##STR1## wherein the symbols have the meanings set forth in the Specification, as well as pharmaceutically-acceptable acid addition salts thereof, the use of the compounds as serotoninergic receptor ligands and for the treatment of anxiety, depression, and other related serotoninergic system disorders, pharmaceutical compositions thereof, and a method for their preparation.Type: GrantFiled: September 14, 1992Date of Patent: February 15, 1994Assignee: Pierre Fabre MedicamentInventors: Bernard Bonnaud, Dennis Bigg
-
Patent number: 5280032Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.Type: GrantFiled: September 8, 1992Date of Patent: January 18, 1994Assignee: Toyama Chemical Co., Ltd.Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita
-
Patent number: 5278174Abstract: Sigma binding site agents having the formula ##STR1## which are useful to inhibit sigma binding site-induced activity, pharmaceutical compositions including these agents, and methods of using these agents to inhibit sigma binding site-induced activity in mammals. Also disclosed are novel intermediates useful in preparing the presently invented agents.Type: GrantFiled: May 17, 1991Date of Patent: January 11, 1994Assignee: Scios Nova, Inc.Inventors: Ronald H. Erickson, Kenneth J. Natalie, Jr., Michael J. Pontecorvo, Waclaw J. Rzeszotarski
-
Patent number: 5252749Abstract: The compounds of the invention having the formula: ##STR1## in which: A, which is a ring condensed with cyclopentane, represents a substituted or unsubstituted thiophene ring, Q represents an alkylene chain, R.sub.1 and R.sub.2 each represent H or an alkyl, or they form, with the nitrogen atom to which they are linked, a saturated nitrogenous heterocyclic ring containing 5 to 7 atoms, R.sub.3 and R.sub.4 each represent H, alkyl, cycloalkyl, trifluoromethyl or an optionally substituted phenyl, thienyl or furyl group or R.sub.3 and R.sub.4 together form a (C.sub.5 -C.sub.8) cycloalkyl, as well as their addition salts with an acid and their quaternary ammonium derivatives.They can be used as medicines.Type: GrantFiled: September 23, 1992Date of Patent: October 12, 1993Assignee: Elf SanofiInventors: Alain Badorc, Jean Courregelongue, Daniel Ducros, Daniel Frehel, Antonina Giudice, Claudine Serradeil-Legal
-
Patent number: 5250681Abstract: A piperidine compound of the formula (I): ##STR1## wherein A is a fused aromatic ring; R is hydrogen, chloro or methoxy; X is (CH.sub.2).sub.n, which may be substituted, in which n is 0 or an integer of 1 to 10, --CH.dbd.CH--, --C.dbd.C--, --O--, --S--, --NH--, --N(COCH.sub.3)--, --N(COOC.sub.2 H.sub.5)--, --N(CHO)--, --N(CH.sub.3)--, --CO--, --SO--, or --SO.sub.2 --; Y is --CH.dbd.CH--, --CH.sub.2 CH.sub.2 --, --CH.sub.2 CO--, --O--, --S--, --NH--, --OCH.sub.2 --, --SCH.sub.2 --, --NHCH.sub.2 --, --CH(OH)CH.sub.2 -- or --CH(OH)CH(OH)--; and Q is substituted or unsubstituted n-hexyl, carboxypropyl, ethoxycarbonylpropyl, cyanopropyl, cyclohexyl, phenyl, indanyl, naphthyl, tetrahydronaphthyl, benzocycloheptyl, piperidinyl, tetrahydroisoquinolinyl, indolyl, pyrolyl, furyl, thienyl, thiazolyl, oxazolyl or N-methylpyrolyl, wherein any one or more of the --(CH.sub.2)-groups of the hexyl, carboxypropyl, ethoxycarbonylpropyl and cyanopropyl groups may be replaced by --CH.dbd.CH--, --C.dbd.Type: GrantFiled: February 15, 1991Date of Patent: October 5, 1993Assignee: Ajinomoto Co., Inc.Inventors: Masataka Shoji, Kozo Toyota, Chikahiko Eguchi, Ryota Yoshimoto, Yoshikatsu Koyama, Hideki Domoto, Akira Kamimura
-
Patent number: 5248686Abstract: The invention relates to substituted arylamines and heteroarylamines, their preparation process and the pharmaceutical composition containing them. Said substituted amine is in accordance with the formula: ##STR1## in which R.sup.1 and R.sup.2 are optionally substituted alkyl radicals or form with N an optionally substituted piperazine or piperidine cycle, R.sup.3 and R.sup.4 represent a hydrogen atom or an organic radical, Y represents CR.sup.6 or N and R.sup.5 is an optionally substituted benzothiophenyl, benzofuranyl or naphthyl radical.These amines can be used in pharmaceutical compositions for the treatment of nervous depression or for stimulating vigilance.Type: GrantFiled: May 12, 1992Date of Patent: September 28, 1993Assignee: Centre National de la Recherche ScientifiqueInventors: Jean-Marc Kamenka, Alain Privat, Robert Chicheportiche, Jean Costentin
-
Patent number: 5244893Abstract: New compounds of the formula (I) ##STR1## in which R.sup.1 -R.sup.6 have the meanings given in the description, their preparation and use in plant protection, the protection of materials and in the field of human and veterinary medicine.Formula (I) gives a definition of the compounds which can be prepared by analogous processes, for example from suitable benzothiophene derivatives by oxidation.Type: GrantFiled: April 29, 1992Date of Patent: September 14, 1993Assignee: Bayer AktiengesellschaftInventors: Hans-Ludwig Elbe, Dieter Berg, Heinz-Wilhelm Dehne, Stefan Dutzmann, Georg-Wilhelm Ludwig, Manfred Plempel
-
Patent number: 5227388Abstract: Novel naphtho[2,3-b]thiophen-9(4H)-ones of the formula ##STR1## wherein R is loweralkyl or arylloweralkyl; X and Y are independently hydrogen, loweralkyl, halogen, loweralkoxy, or trifluoromethyl; W is CH.sub.2, CHOH, or C.dbd.O; n is 1 or 2; an optical isomer or pharmaceutically acceptable salt thereof, processes for the preparation thereof, and methods of alleviating pain utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: January 30, 1991Date of Patent: July 13, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Effland, David G. Wettlaufer
-
Patent number: 5179092Abstract: A compound having the formula (I): ##STR1## wherein A is --CH.sub.2 --, --O--, or --S--; R.sup.1 is CH.sub.3 or OCH.sub.3 ; R.sup.2 is hydroxy or carboxy which may be optionally esterized or amidated; R.sup.3 is H or a lower alkyl; and n is 0 or an integer of 1 to 6 or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 30, 1991Date of Patent: January 12, 1993Assignee: Suntory LimitedInventors: Toshio Tatsuoka, Kenji Suzuki, Fumio Satoh, Seiji Miyano, Kunihiro Sumoto
-
Patent number: 5169856Abstract: The present invention relates to unsaturated carboxylic acid amide derivatives of the formula ##STR1## wherein ring A stands for an optionally substituted aromatic ring; R.sup.1 stands for a hydrogen atom or an optionally substituted hydrocarbon residue or forms an optionally substituted carbocyclic ring with the adjacent group --CH.dbd.C-- together with two carbon atoms constituting the ring A; R.sup.2 stands for a hydrogen atom, an optionally substituted hydrocarbon residue or an optionally substituted acyl group; R.sup.3 stands for an optionally substituted hydrocarbon residue; and n denotes an integer ranging from 2 to 6, and salts thereof, as well as the production thereof.The compounds of the present invention act on the central nervous system of mammals and has a strong anti-cholinesterase activity, which can be used for the prophylaxis and therapy of, for example, senile dementia, Alzheimer's diseases, Huntington's chorea, et., and are useful as medicines.Type: GrantFiled: February 6, 1989Date of Patent: December 8, 1992Assignee: Takeda Chemical Industries, Inc.Inventors: Giichi Goto, Akinobu Nagaoka
-
Patent number: 5145967Abstract: The present invention is directed to a method for preparing a 4-alkoxyalkyl-4-phenylaminopiperidine compound which comprises the steps of (a) reacting an N-substituted-4-piperidone compound with an aniline compound to form a Schiff base compound, (b) reacting the Schiff base compound with an anionic reagent having an anion stabilizing group to form an amine compound, and (c) reducing the amine compound in step (b) with a reducing agent to displace the anion stabilizing group.The anionic reagent in step (b) above has the general formula:X--CYM--Zwherein X is an anion stabilizing group, Y is hydrogen or lower-alkyl, Z is lower-alkoxy or phenylmethoxy, M is an alkali or alkaline earth metal, and C is a carbon atom.Type: GrantFiled: November 2, 1990Date of Patent: September 8, 1992Assignee: Anaquest, Inc.Inventors: Bor-Sheng Lin, H. Kenneth Spencer, Joseph W. Scheblein
-
Patent number: 5143922Abstract: Novel tricyclic compounds having a TXA.sub.2 antagonizing activity represented by formula (I): ##STR1## possess a potent antagonizing action against thromboxane A.sub.2 and also an antiallergic and/or antihistaminic acitvity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.Type: GrantFiled: November 20, 1990Date of Patent: September 1, 1992Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii, Hidee Ishii, Kenji Ohmori
-
Patent number: 5126356Abstract: The compounds disclosed are 1-R'-4-RS-piperidines in which R' and R, which are different, may each represent: (1) (alkoxybenzyl)-alkyl or -alkenyl, or (2) (optionally-substituted chromanyl-, thiochromanyl-, chromenyl- or thiochromenyl)-alkyl or -alkenyl. The compounds are useful in the treatment of disorders associated with tissue ischaemia and of peripheral vascular disorders or in the treatment of disorders in which lipid peroxidation plays an initiating and/or aggravating role. A typical disclosed compound is: 4-(2,3,4-tirmethoxybenzylthio)-1-(3,5-di- tert-butyl-4-hydroxybenzyl)piperidine. ,3,4-trimethoxybenzylthio)-1-(3,5-di-tert-butyl-4-hydroxybenzyl)piperidine .Type: GrantFiled: December 11, 1990Date of Patent: June 30, 1992Assignee: Adir et CompagnieInventors: Gilbert Regnier, J. F. Benaud De La Faverie, Alain Lombet, Jean-Pierre Iliou, Jean-Paul Vilaine, Jean-Pierre Bidouard, Albert Lenaers
-
Patent number: 5098915Abstract: Substituted N-benzylpiperidine amides, which have activity as Class III antiarrhythmic agents, acting by prolonging cardiac action potential repolarization. The invention further provides for compositions incorporating the compunds and methods of their use, as well as providing for pharmaceutically acceptable salts of the compounds.Type: GrantFiled: September 5, 1989Date of Patent: March 24, 1992Assignee: G. D. Searle & Co.Inventors: Bipinchandra N. Desai, Kerry W. Fowler, Alan E. Moormann
-
Patent number: 5089505Abstract: A series of novel 1-(phenethyl) and 1-(1-heteroarylethyl)-3-substituted piperidine derivatives have been prepared, including their pharmaceutically acceptable salts and various novel key intermediates therefor. The 3-substituent present in these compounds is an unsubstituted or substituted diphenylmethoxy group or a diphenylmethoxy-derived group, while the 1-substituent is unsubstituted or substituted phenethyl or 1-(2-heteroarylethyl) wherein the heteroaryl moiety is thienyl, pyridyl or pyrazinyl. These compounds in the form of both their racemates and 3R-isomers, are useful in therapy as smooth muscle muscarinic receptor antagonists and therefore, are of value in the treatment diseases associated with altered motility and/or smooth muscle tone. The most preferred compound is (3R)-diphenylmethoxy-1-(3,4-methylenedioxyphenethyl)piperidine. Methods for preparing these compounds from known starting materials are provided.Type: GrantFiled: July 6, 1989Date of Patent: February 18, 1992Assignee: Pfizer Inc.Inventors: David Alker, Peter E. Cross, Robert M. Wallis
-
Patent number: 5086179Abstract: This invention is directed to certain dibenzofurancarboxamides and dibenzofurancarboxamide acids and their use as 5HT.sub.3 antagonists having unique CNS, anti-emetic and gastric prokinetic activity void of any significant D.sub.2 receptor binding properties. Further, this invention relates to a process for the synthesis of stereoisomeric compounds having such CNS, anti-emetic and gastric prokinetic activity.Type: GrantFiled: September 24, 1990Date of Patent: February 4, 1992Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: Matthew R. Powers, Raymond D. Youssefyeh, William L. Studt, Frederick A. Golec
-
Patent number: 5071858Abstract: Disclosed are 3,4-dihydro-2H-1-benzothiopyran-3-yl-methyl- and ethylamines useful as antipsychotics, processes for the preparation of said compounds, pharmaceutical compositions containing same, and a method of treating psychotic disorders by administering said compounds.Type: GrantFiled: October 12, 1990Date of Patent: December 10, 1991Assignee: Ciba-Geigy CorporationInventor: Alan J. Hutchison
-
Patent number: 5071841Abstract: The present invention provides a sulfur-containing heterocyclic compound of the formula (I) ##STR1## wherein ring A is a benzene ring which may be substituted; R is a hydrogen atom or a hydrocarbon group which may be substituted; B is a carboxyl group which may be esterified or amidated; X is --CH(OH)-- or --CO--; k is 0 or 1; and k' is 0, 1 or 2 or a pharmaceutically acceptable salt thereof.Also, it provides a process for producing the compound (I) or a salt thereof and a pharmaceutical preparation for use in the treatment of osteoporosis comprising the compound (I) or salt thereof.The compounds (I) and salts thereof show excellent bone resorption inhibitory activity.Type: GrantFiled: December 28, 1989Date of Patent: December 10, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Masao Tsuda, Iwao Yamazaki
-
Patent number: 5053411Abstract: This invention pertains to novel substituted N-aryl-N-[4-(1-heterocyclicalkyl)piperidinyl]amides useful as analgesics, and methods of administering analgesia, which comprises the systemic administration to mammals of such compounds, and pharmaceutical compositions containing such compounds, wherein the novel compounds have the general formula: ##STR1## including optically active isomeric forms, and the pharmaceutically acceptable acid addition salts thereof, wherein R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are defined in the disclosure.Type: GrantFiled: April 20, 1989Date of Patent: October 1, 1991Assignee: Anaquest, Inc.Inventors: Jerome R. Bagley, Nhora L. Lalinde, Bao-Shan Huang, H. Kenneth Spencer
-
Patent number: 4994450Abstract: A compound, or a solvate or salt thereof, of formula (I) ##STR1## in which: R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4-12 cycloalkylalkyl groups, or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group optionally substituted with a hetero-atom, provided that R.sub.1 and R.sub.2 are not simultaneously hydrogen;R.sub.3 is hydrogen, C.sub.1-6 alkyl, preferably methyl or ethyl, or phenyl, or R.sub.3 together with R.sub.1 form a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- group;p is 1, 2, 3 or 4, andR is a group of formula (II) ##STR2## in which the group --(CHR.sub.4).sub.n --X-- is in the meta- or para-position with respect to YR.sub.5 or R.sub.6, R.sub.4 is hydrogen or C.sub.1-6 alkyl, preferably hydrogen;n is 0, 1 or 2, preferably 1;X is a direct bond, or O, S or NR.sub.a in which R.sub.a is hydrogen or C.sub.1-6 alkyl, and is preferably a direct bond;Y is >C.dbd.O, >CHOH, --S.dbd.O or --SO.Type: GrantFiled: February 10, 1989Date of Patent: February 19, 1991Assignee: Dr. Lo. Zambeletti S.p.A.Inventors: Vittorio Vecchietti, Antonio Giordani
-
Patent number: 4994463Abstract: Novel tricyclic compounds having a TXA.sub.2 antagonizing activity represented by formula (I): ##STR1## possess a potent antagonizing action against thromboxane A.sub.2 and also an antiallergic and/or antihistaminic activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.Type: GrantFiled: December 8, 1988Date of Patent: February 19, 1991Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii, Hidee Ishii, Kenji Ohmori
-
Patent number: 4988727Abstract: A compound selected from the group consisting of all enantiomeric and diastereoisomeric forms possible of compounds of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, halogen, and alkyl and alkoxy of 1 to 5 carbon atoms, R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, one of A and B being ##STR2## and the other being ##STR3## R is hydrogen or alkyl of 1 to 5 carbon atoms, Z is --(CH.sub.2).sub.n -- or branched alkylene of 2 to 8 carbon atoms, n is an integer from 0 to 5, Y is selected from the group consisting of naphthyl, indenyl, heterobicyclics and heteromonocyclic containing 5 to 6 ring members, all optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, halogen, --OH, --CF.sub.3, --NO.sub.2, --NH.sub.Type: GrantFiled: September 19, 1989Date of Patent: January 29, 1991Assignee: Roussel UclafInventors: Francois Clemence, Michel Fortin
-
Patent number: 4977151Abstract: Ethanone oximes represented by the following general formula: ##STR1## wherein R.sup.1 represents a cycloalkyl group, aryl group, aralkyl group, aryloxy group, aralkyloxy group, arylthio group or aryl sulfonyl group, those groups being optionally substituted with a substituent selected from an alkyl group having 1 to 3 carbon atoms, an alkoxy group having 1 to 3 carbon atoms and a halogen atom, piperidino group, piperazino group, 4-alkyl substituted piperazino group, imidazolyl group 4-alkyl substituted imidazolyl group or substituted amino group,R.sup.2 represents a hydrogen atom or an alkoxy group having 1 to 3 carbon atoms, andR.sup.3 represents a piperidino group, piperazino group or 4-alkyl substituted piperazino group, orR.sup.1 and R.sup.2 together with a phenyl group to which they are attached may form a phenothiazin-2-yl group, N-acetyl-phenothiazin-2-yl group, thianthren-2-yl group, dibenzothiophen-3-yl group, dibenzofuran-3-yl group or a group of the formula: ##STR2## wherein R.sup.Type: GrantFiled: March 29, 1990Date of Patent: December 11, 1990Assignee: Mitsubishi Kasei CorporationInventors: Shinichiro Fujimori, Satoshi Yamazaki, Mamoru Sugano, Makoto Kawamura, Kunihiro Ninomiya, Akihiro Tobe, Issei Nitta
-
Patent number: 4939144Abstract: The invention relates to ketones of the general formula (I): ##STR1## wherein Im represents an imidazolyl group of the formula: ##STR2## 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 phenyl C.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;n represents 1, 2 or 3;Q represents a hydrogen atom, a halogen atom, or a hydroxy, C.sub.1-4 alkoxy, phenyl C.sub.1-3 alkoxy or C.sub.1-6 alkyl group, or a group --NR.sup.4 R.sup.5 or --CONR.sup.4 R.sup.5, (wherein R.sup.4 and R.sup.5, which may be the same or different, each represents a hydrogen atom or a C.sub.1-4 alkyl or C.sub.Type: GrantFiled: October 21, 1988Date of Patent: July 3, 1990Assignee: Glaxo Group LimitedInventors: Ian H. Coates, David C. Humber, James A. Bell, George B. Ewan, Alexander W. Oxford, William L. Mitchell
-
Patent number: 4933344Abstract: Ethanone oximes represented by the following general formula: ##STR1## wherein R.sup.1 represents a cycloalkyl group, aryl group, aralkyl group, aryloxy group, aralkyloxy group, arylthio group or aryl sulfonyl group, those groups being optionally substituted with a substituent selected from an alkyl group having 1 to 3 carbon atoms, an alkoxy group having 1 to 3 carbon atoms and a halogen atom, piperidino group, piperazino group, 4-alkyl substituted piparazino group, imidazolyl group, 4-alkyl substituted imidazolyl group or substituted amino group,R.sup.2 represents a hydrogen atom or an alkoxy group having 1 to 3 carbon atoms, andR.sup.3 represents a piperidino group, piperazino group or 4-alkyl substituted piperazino group, orR.sup.1 and R.sup.2 together with a phenyl group to which they are attached may form a phenothiazin-2-yl group, N-acetyl-phenothiazin-2-yl group, thianthren-2-yl group, dibenzothiophen-3-yl group, dibenzofuran-3-yl group or a group of the formula: ##STR2## wherein R.sup.Type: GrantFiled: August 31, 1988Date of Patent: June 12, 1990Assignee: Mitsubishi Kasei CorporationInventors: Shinichiro Fujimori, Satoshi Yamazaki, Mamoru Sugano, Makoto Kawamura, Kunihiro Ninomiya, Akihiro Tobe, Issei Nitta
-
Patent number: 4921955Abstract: The invention relates to a process for the preparation of 1,5-disubstituted imidazoles of the formula ##STR1## by alkylation of an N-cyanoformamidine of the formula IIX--NH--CH.dbd.N--CH (II)to form an N,N-disubstituted N'-cyanoformamidine of the formula ##STR2## which is cyclised under the action of bases to form a 4-aminoimidazole of the formula ##STR3## and then reduced to form the product of the formula I. The invention relates also to a special process for the reduction of the aminoimidazole V to I, and to intermediate compounds for carrying out this process and to processes for the preparation of the intermediate compounds.The meaning of the substituents X and L is explained in detail in the text.Type: GrantFiled: December 18, 1987Date of Patent: May 1, 1990Assignee: Ciba-Geigy CorporationInventor: Werner Topfl
-
Patent number: 4904688Abstract: The present invention deals with dibenzo-oxocin-, dibenzo-thiocin-, dibenzo-azocin- and dibenzocyclo-octenamine derivatives suitable for use as antipsychotic compounds without extra-pyrimidal side-effects.Type: GrantFiled: March 8, 1989Date of Patent: February 27, 1990Assignee: Akzo N.V.Inventors: Duncan R. Rae, James Cairns
-
Patent number: 4904686Abstract: Compounds of the following formula have pharmacutical properties: ##STR1## in which R.sup.1 and R.sup.2 independently are hydrogen, halo, nitro, amino, C.sub.2-5 acylamino, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulphonyl, N-substituted heterocyclyl, optionally substituted phenyl, optionally substituted phenylthio, optionally substituted phenylsulphonyl or optionally substituted phenylsulphonamido, or R.sup.1 and R.sup.2 together form a C.sub.3-5 alkylene bridge, R.sup.3 is C.sub.1-4 alkyl or C.sub.2-4 alkenyl, and X is (i) --(CH.sub.2).sub.n N(R.sup.4).sub.2 where each R.sup.4 independently is C.sub.1-4 alkyl, C.sub.2-4 alkenyl or optionally substituted C.sub.6 H.sub.5 CH.sub.2 --, and n is 1, 2 or 3, or (ii) a 5- to 8-membered alicyclic group containing one or two nitrogen atoms and directly attached to the amido nitrogen or attached by a C.sub.1-3 alkylene chain; and salts thereof.Type: GrantFiled: April 11, 1988Date of Patent: February 27, 1990Assignee: Lilly Industries LimitedInventors: Maria I. F. Fernandez, Terrence M. Hotten, David E. Tupper
-
Patent number: 4897402Abstract: Novel HMG-CoA reductase inhibitors are useful as antihypercholesterolemic agents and are represented by stuctural formulae (I) and (II): ##STR1## wherein A is O, S(O).sub.n or N--R.sub.13.Type: GrantFiled: June 29, 1988Date of Patent: January 30, 1990Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman
-
Patent number: RE34201Abstract: This invention pertains to novel substituted N/aryl-N-[4-(1-heterocyclicalkyl)piperidinyl]amides useful as analgesics, and methods of administering analgesia, which comprises the systemic administration to mammals of such compounds, and pharmaceutical compositions containing such compounds, wherein the novel compounds have the general formula: ##STR1## including optically active isomeric forms, and the pharmaceutically acceptable acid addition salts thereof, wherein R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are defined in the disclosure.Type: GrantFiled: April 14, 1992Date of Patent: March 23, 1993Assignee: Anaquest, Inc.Inventors: Jerome R. Bagley, Nhora L. Lalinde, Bao-Shan Huang, H. Kenneth Spencer