The Other Ring Nitrogen Has A Substituent Which Includes Chalcogen Single Bonded To Acyclic Carbon Patents (Class 544/394)
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Patent number: 5523302Abstract: This invention relates to novel compounds containing basic and acidic termini, pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.Type: GrantFiled: November 24, 1993Date of Patent: June 4, 1996Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Gary A. Cain, Charles J. Eyermann
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Patent number: 5504087Abstract: A hypotensive agent and antiglaucoma agent which comprise a compound represented by the following formula: ##STR1## (wherein R.sub.1 is hydrogen, or a lower alkyl or lower alkoxy group; R.sub.2 is an isopropylamino, tert-butylamino, 2-(2-methoxyphenyl)ethyl-1-amino, 4-(2-methoxyphenyl)!-1-piperazinyl or 4-piperonyl-1-piperazinyl group, provided however that in the case of R.sub.1 being hydrogen, R.sub.2 is neither isopropylamino nor tert-butylamino group) or its pharmacologically acceptable salt.Type: GrantFiled: February 8, 1994Date of Patent: April 2, 1996Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Kazumi Ogata, Takahiro Sakaue, Yuuichi Isowaki, Takaaki Deguchi
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Patent number: 5420278Abstract: 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 functionalized 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: May 24, 1994Date of Patent: May 30, 1995Assignee: John Wyeth & Brother, LimitedInventor: Ian A. Cliffe
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Patent number: 5382687Abstract: An enamine derivative containing a fluoroalkyl group, a fluoroaryl group or a fluoroaralkyl group is effective as a charge transport material in an electrophotographic member excellent in sensitivity, residual potential, durability and the like electrophotographic properties.Type: GrantFiled: August 2, 1993Date of Patent: January 17, 1995Assignee: Hitachi Chemical Company Ltd.Inventors: Yoshii Morishita, Shigeru Hayashida, Yasushi Sugimoto, Hiroko Ishikawa, Hiroshi Kobayashi, Takaaki Sonoda
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Patent number: 5352677Abstract: Cinnamamide derivatives and the salts thereof are provided. An antihyperlipidemic composition is also provided. The composition comprises an active ingredient which is at least one selected from the group consisting of the above-mentioned cinnamamide derivative and the pharmaceutically acceptable salt thereof.Type: GrantFiled: July 15, 1992Date of Patent: October 4, 1994Assignee: Kanegafuchi Kagaku Kogyo Kabushiki KaishaInventors: Yoshihide Fuse, Kenji Fujii, Keiji Kameyama, Taizo Kawabe, Toshiaki Miwa, Ikuo Katsumi
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Patent number: 5346896Abstract: Disclosed herein are piperazine derivatives of the formula ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein W is (CH.sub.2).sub.m, CHOH or O,m is one of the integers 1 or 2,A is an alkylene chain of 1 to 3 carbon atoms optionally substituted by one or more (lower)alkyl groups,R is hydrogen or lower alkyl,R.sup.1 and R.sup.2 are each, independently, aryl or heteroaryl radicals with the proviso that R.sup.1 is not an optionally substituted indolyl radical,R.sup.3 is hydrogen or lower alkyl andR.sup.4 is an aryl or heteroaryl radical.The compounds are 5HT.sub.1A binding agents which may be used, for example, in the treatment of CNS disorders such as anxiety.Type: GrantFiled: June 3, 1992Date of Patent: September 13, 1994Assignee: John Wyeth & Brother, LimitedInventors: Terence J. Ward, Graham J. Warrellow
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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
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Patent number: 5322846Abstract: The present invention relates to novel 4-methylthiazole derivatives, to tr methods of preparation and to the pharmaceutical compositions in which they are present.According to the invention, these derivatives have the general formula ##STR1## in which n is equal to 0 or 1 and R.sub.1 and R.sub.2, which are identical or different, are selected from a hydrogen atom, a halogen, a hydroxyl group, a trifluoromethyl group, an alkyl group having from 1 to 4 carbon atoms and an alkoxy group having from 1 to 5 carbon atoms and are useful in the treatment of cardiovascular diseases associated with hyperactivity of the sympathetic nervous system.Type: GrantFiled: October 19, 1992Date of Patent: June 21, 1994Assignee: Institut de Recherches Chimiques et Biologiques Appliquees (I.R.C.E.B.A.)Inventors: Fabienne Jobard-Rouppert, Patrick Houziaux, Jean-Pierre Riffaud, Jean-Yves Lacolle, Patrick Saur, Bernard Danree
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Patent number: 5317020Abstract: Aromatic amine derivatives of the general formula (I) ##STR1## or salts of the derivatives with mineral or organic acids are useful as neurokinin receptor antagonists.Type: GrantFiled: November 5, 1990Date of Patent: May 31, 1994Assignee: SanofiInventors: Xavier Emonds-Alt, Pierre Goulaouic, Vincenzo Proietto, Didier Van Broeck
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Patent number: 5284850Abstract: Novel terpene amino alcohols having an antiallergic activity or an activity of improving cerebral function are provided. Also provided are medicinal uses of the alcohols.Type: GrantFiled: June 5, 1992Date of Patent: February 8, 1994Assignee: Kuraray Co., Ltd.Inventors: Koichi Kanehira, Katsushi Eziri, Manzo Shiono, Yoshiji Fujita, Johji Yamahara
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Patent number: 5246935Abstract: Piperazinyl derivatives of the general formula I ##STR1## wherein R.sup.1 represents substituted phenyl, 1- or 2-diazanaphthyl, azadiazanaphtyl or diazanaphtyl groups; n is 1, 2, 3 or 4; X is --O-- or ##STR2## wherein R.sup.2 is hydrogen, C.sub.1-6 -alkyl or C.sub.3-8 -cycloalkyl; Y is .dbd.O or .dbd.S or .dbd.NZ wherein Z is hydrogen, C.sub.1-6 -alkyl or --CN and R.sup.3 is selected from a group consisting of various structures have been found to exhibit high affinity for various receptor subtypes including the 5-HT.sub.2 receptor, the 5-HT.sub.1A receptor, the alpha.sub.1 receptor the dopamine receptor or a combination of these and may therefore be useful for treating CNS system, cardiovascular system and gastrointestinal disorders.Type: GrantFiled: August 13, 1991Date of Patent: September 21, 1993Assignee: Novo Nordisk A/SInventors: Lone Jeppesen, Marit Kristiansen, John B. Hansen
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Patent number: 5245034Abstract: Novel quinoline sulfonamino derivatives having a vessel smooth muscle relaxation activity as well as a platelet agglutination inhibitory activity and inhibitory activity to protein kinase A, myosin light chain kinase, proteinkinase C, and calmodulindependent proteinkinase II, but having little action or cardio function; a process for the production of the derivatives, and a pharmaceutical composition containing the derivative.Type: GrantFiled: March 23, 1992Date of Patent: September 14, 1993Assignee: Kiroyoshi HidakaInventors: Hiroyoshi Hidaka, Tomohiko Ishikawa, Masatoshi Hagiwara, Tsutomu Inoue, Kenji Naitoh, Osamu Sakuma, Masayuki Yuasa, Tadashi Morita, Tadashi Toshioka, Isao Umezawa, Takashi Inaba
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Patent number: 5234934Abstract: The invention relates to novel racemic or optically active aminopropanol derivatives of formula I ##STR1## wherein R and R.sup.1 are independently hydrogen atom, halogen atom, lower alkoxy, or together represent a methylene dioxy group,R.sup.2 and R.sup.3 together represent a chemical bond or independently stand for a hydrogen atom,R.sup.4 and R.sup.5 are independently hydrogen atom, C.sub.3-7 cycloalkyl group or straight or branched, saturated or unsaturated C.sub.1-12 alkyl group optionally substituted by one or more dialkyl-aminoalkyl, dimethoxyphenyl or phenyl groups, orR.sup.4 and R.sup.5 together with the adjacent nitrogen atom form a 4 to 7 membered ring optionally comprising an oxygen, sulfur or a further nitrogen atom, which ring is optionally substituted by a phenyl, benzyl or C.sub.1-3 alkyl group and the said substituents may carry a hydroxyl group, one or two methoxy groups, halogen atoms or trifluoromethyl groups, orR.sup.4 and R.sup.Type: GrantFiled: April 30, 1992Date of Patent: August 10, 1993Assignee: Egis GyogyszergyarInventors: Zoltan Budai, Klara Reiter nee Esses, Eniko Sziri nee Kiszelly, Gizella Zsila, Gabor Gigler, Lujza Petocz, Maria Szecsey nee Hegedus, Marton Fekete, Valeria Hoffmann, Laszlo Kapolnai
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Patent number: 5223623Abstract: This invention relates to novel 2-substituted-1(4)-aryl piperazines and to a process for their preparation. The compounds of this invention have been found to have cardiovascular, primarily antiarrhythmic effects.Type: GrantFiled: September 11, 1991Date of Patent: June 29, 1993Assignee: Schering AGInventor: Gary B. Phillips
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Patent number: 5216150Abstract: Novel quinoline sulfonamino derivatives having a vessel smooth muscle relaxation activity as well as a platelet agglutination inhibitory activity and inhibitory activity to protein kinase A, myosin light chain kinase, proteinkinase C, and calmodulindependent proteinkinase II, but having little action or cardio function; a process for the production of the derivatives, and a pharmaceutical composition containing the derivative.Type: GrantFiled: September 12, 1991Date of Patent: June 1, 1993Assignees: Hiroyoshi Hidaka, Tobishi Yakuhin Kogyo Kabushiki KaishaInventors: Hiroyoshi Hidaka, Tomohiko Ishikawa, Masatoshi Hagiwara, Tsutomu Inoue, Kenji Naitoh, Osamu Sakuma, Masayuki Yuasa, Tadashi Morita, Tadashi Toshioka, Isao Umezawa, Takashi Inaba
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Patent number: 5214045Abstract: Novel acrylic amide derivatives of the Formula (I) ##STR1## wherein R.sup.1 represents a hydrogen or a halogen atom or a C.sub.1-4 alkyl, a C.sub.1-4 alkoxy or a nitro group.n is an integer of 0 to 2,A represents an amino acid residue derived from a naturally occurring amino acid or an antipode thereof which is bonded to the acrylic acyl residue through its amino group; or a residue derived from thiazolidinecarboxylic acid, bonded to the acrylic acyl group through its nitrogen, or a derivative of the above residues wherein any free carboxy group is esterified with a C.sub.1-4 alkyl group or is amidated; or A represents a group of the formula ##STR2## wherein R.sub.2 is a hydrogen atom or a phenyl, C.sub.1-4 alkyl or C.sub.1-4 alkoxycarbonyl group,and their salts which have cytoprotective and antiulcer to activities. A process is also described for the preparation of said compounds.Type: GrantFiled: July 11, 1990Date of Patent: May 25, 1993Assignee: Richter Gedeon Vegyeszeti Gyar RTInventors: Tamas Fodor, Janos Fischer, Laszlo Dobay, Elemer Ezer, Judit Matuz, Laszlo Szporny, Gyorgy Hajos
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Patent number: 5166157Abstract: Compounds of formula I: ##STR1## in which: N=1-4,R represents hydrogen, halogen, alkyl, hydroxyl or alkoxy, R.sub.1 represents a radical -NHCOR2 (A.sub.1); (in which R.sub.2 represents alkyl, cycloalkyl, phenyl, optionally substituted-, -O-alkyl, 3-pyridyl, 2-pyrrolyl, quinolyl, 1-isoquinolyl, 2-thienyl or 3-indolyl); a radical of --NHSO2R3 (A.sub.2) (in which R.sub.3 represents alkyl, cycloalkyl or phenyl optionally substituted); a radical --NHCONHR4 (A.sub.3) (in which R.sub.4 represents alkyl or phenyl-optionally substituted); a phthalimido radical (A.sub.4); an o-sulfobenzoic imido radical (A.sub.5); a di(benzoyl)amino radical (A.sub.6) optionally substituted; a radical of formula A.sub.7 : ##STR2## (in which R.sub.5 represents carbamoyl, cyano, carboxy or alkoxycarbonyl); or a radical of formula A.sub.8 : ##STR3## their stereoisomers and their addition salts with a pharmaceutically-acceptable inorganic or organic acid, are disclosed to be useful as 5-HT.sub.Type: GrantFiled: August 27, 1991Date of Patent: November 24, 1992Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Michel Laubie, Francis Colpaert
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Patent number: 5166156Abstract: Compounds of formula I: ##STR1## in which: n=1-4,R represents hydrogen, halogen, alkyl, hydroxyl or alkoxy, R.sub.1 represents a radical --NHCOR2 (A.sub.1); (in which R.sub.2 represents alkyl, cycloalkyl, phenyl optionally substituted, -O-alkyl, 3-pyridyl, 2-pyrrolyl, quinolyl, 1-isoquinolyl, 2-thienyl or 3-indolyl); a radical of -NHSO2R3 (A.sub.2) (in which R.sub.3 represents alkyl, cycloalkyl or phenyl optionally substituted); a radical --NHCONHR4 (A.sub.3) (in which R.sub.4 represents alkyl or phenyl-optionally substituted); a phthalimido radical (A.sub.4); an o-sulfobenzoic imido radical (A.sub.5); a di(benzoyl)amino radical (A.sub.6) optionally substituted; a radical of formula A.sub.7 : ##STR2## (in which R.sub.5 represents carbamoyl, cyano, carboxy or alkoxycarbonyl); or a radical of formula A.sub.8 : ##STR3## their stereoisomers and their addition salts with a pharmaceutically-acceptable inorganic or organic acid, are disolosed to be useful as 5-HT.sub.Type: GrantFiled: August 29, 1991Date of Patent: November 24, 1992Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Michel Laubie, Francis Colpaert
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Patent number: 5166218Abstract: Tertiary and secondary amines of the formulas ##STR1## and ##STR2## wherein n is the integer 1 or 2,R is hydrogen, lower-alkanoyl or phenyl-lower-alkanoyl,X.sup.1 is phenoxymethyl optionally mono-fluorinated or mono-chlorinated in the ortho-position,X.sup.2 is lower-alkyl, phenoxymethyl optionally mono-fluorinated or mono-chlorinated in the ortho-position or phenyl optionally monosubstituted by fluorine, chlorine, trifluoromethyl or lower-alkoxy,Y is hydrogen or methyl, andZ is a phenyl or thienyl residue substituted as hereinafter described,and the physiologically and pharmaceutically compatible salts are described. The compounds of formulas I and V-1 have catabolic activity and can be used for the treatment of obesity and diabetes mellitus or for the treatment of conditions which are associated with an increased protein breakdown, or as feed additives for fattening animals. The compounds of formulas I and V-1 can be prepared starting from corresponding primary amines.Type: GrantFiled: August 12, 1991Date of Patent: November 24, 1992Assignee: Hoffmann-La Roche Inc.Inventors: Leo Alig, Marcel Muller
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Patent number: 5162324Abstract: Compounds of formula I: ##STR1## in which: n=1-4,R represents hydrogen, halogen, alkyl, hydroxyl or alkoxy, R.sub.1 represents a radical --NHCOR2 (A.sub.1); (in which R.sub.2 represents alkyl, cycloalkyl, phenyl optionally substituted-, -O-alkyl, 3-pyridyl, 2-pyrrolyl, quinolyl, 1-isoquinolyl, 2-thienyl or 3-indolyl); a radical of --NHSO2R3 (A.sub.2) (in which R.sub.3 represents alkyl, cycloalkyl or phenyl optionally substituted); a radical --NHCONHR4 (A.sub.3) (in which R.sub.4 represents alkyl or phenyl-optionally substituted); a phthalimido radical (A.sub.4); an o-sulfobenzoic imido radical (A.sub.5); a di(benzoyl)amino radical (A.sub.6) optionally substituted; a radical of formula A.sub.7 : ##STR2## (in which R.sub.5 represents carbamoyl, cyano, carboxy or alkoxycarbonyl); or a radical of formula A.sub.8 : ##STR3## their stereoisomers and their addition salts with a pharmaceutically-acceptable inorganic or organic acid, are disclosed to be useful as 5-HT.sub.Type: GrantFiled: August 29, 1991Date of Patent: November 10, 1992Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Michel Laubie, Francis Colpaert
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Patent number: 5162321Abstract: Compounds of formula I: ##STR1## in which: n=1-4;R represents hydrogen, halogen, alkyl, hydroxyl or alkoxy, R.sub.1 represents a radical --NHCOR2 (A.sub.1); (in which R.sub.2 represents alkyl, cycloalkyl, phenyl optionally substituted-, --O-alkyl, 3-pyridyl, 2-pyrrolyl, quinolyl, 1-isoquinolyl, 2-thienyl or 3-indolyl); a radical of --NHSO2R3 (A.sub.2) (in which R.sub.3 represents alkyl, cycloalkyl or phenyl optionally substituted); a radical --NHCONHR4 (A.sub.3) (in which R.sub.4 represents alkyl or phenyl-optionally substituted); a phthalimido radical (A.sub.4); an o-sulfobenzoic imido radical (A.sub.5); a di(benzoyl)amino radical (A.sub.6) optionally substituted; a radical of formula A.sub.7 : ##STR2## (in which R.sub.5 represents carbamoyl, cyano, carboxy or alkoxycarbonyl); or a radical of formula A.sub.8 : ##STR3## their stereoisomers and their addition salts with a pharamaceutically-acceptable inorganic or organic acid, are disclosed to be useful as 5-HT.sub.Type: GrantFiled: August 29, 1991Date of Patent: November 10, 1992Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Michel Laubie, Francis Colpaert
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Patent number: 5143916Abstract: Compounds of the formula I: ##STR1## in which: n=1-4,R represents hydrogen, halogen, alkyl, hydroxyl or alkoxy, R.sub.1 represents a radical --NHCOR2 (A.sub.1); (in which R.sub.2 represents alkyl, cycloalkyl, phenyl optionally substituted-, --O-alkyl, 3-pyridyl, 2-pyrrolyl, quinolyl, 1-isoquinolyl, 2-thienyl or 3-indolyl); a radical of --NHS02R3 (A.sub.2) (in which R.sub.3 represents alkyl, cycloalkyl or phenyl optionally substituted); a radical --NHCONHR4 (A.sub.3) (in which R.sub.4 represents alkyl or phenyl-optionally substituted); a phthalimido radical (A.sub.4); an o-sulfobenzoic imido radical (A.sub.5); a di(benzoyl)amino radical (A.sub.6) optionally substituted; a radical of formula A.sub.7 : ##STR2## (in which R.sub.5 represents carbamoyl, cyano, carboxy or alkoxycarbonyl); or a radical of formula A.sub.8 : ##STR3## their stereoisomers and their addition salts with a pharmaceutically-acceptable inorganic or organic acid, are disclosed to be useful as 5-HT.sub.Type: GrantFiled: December 19, 1990Date of Patent: September 1, 1992Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Michel Laubie, Francis Colpaert
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Patent number: 5128348Abstract: Certain hexane and heptane amines including geometric and stereoisomers, agricultural compositions containing them and their use as fungicides.Type: GrantFiled: September 12, 1990Date of Patent: July 7, 1992Assignee: E. I. Du Pont de Nemours and CompanyInventor: Gregory S. Basarab
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Patent number: 5112867Abstract: A triphenylmethane derivative represented by the following general formula: ##STR1## exhibits born absorption inhibiting effects and is useful as a medicament for treating osteoporosis.Type: GrantFiled: April 27, 1990Date of Patent: May 12, 1992Assignee: Kyowa Hakko Gogyo Co., Ltd.Inventors: Iwao Kinoshita, Daisuke Machii, Yasuo Onoda, Haruki Takai, Nobuo Kasaka, Katsuichi Shuto, Katsushige Gomi, Makoto Morimoto, Akio Ishii
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Patent number: 5110928Abstract: N-Aryl-substituted 2-amino-alkyl-2-hydroxyalkylamines and N-aryl-substituted piperazines Ia and Ib respectively ##STR1## (Ar=aryl; R.sup.1 =hydrogen, methyl, identical or different, R.sup.2 =hydrogen, alkyl) are prepared by reacting an N,N-di(2-hydroxyalkyl)-N-arylamine II ##STR2## with ammonia or a primary amine IIIH.sub.2 N-R.sup.2 IIIat elevated temperature and under elevated pressure in the presence of hydrogen and of a catalyst which is a supported catalyst whose active mass predominantly contains copper and/or nickel and/or cobalt in the form of the metal or an oxide.Type: GrantFiled: March 15, 1991Date of Patent: May 5, 1992Assignee: BASF AktiengesellschaftInventors: Wolfgang Schroeder, Guenther Ruider
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Patent number: 5110816Abstract: The present invention relates to the products of general formula (I): ##STR1## in which R.sub.1 and R.sub.2 are identical or different and are selected om a hydrogen atom, a halogen atom, a hydroxyl radical, an alkyl radical having from 1 to 5 (sic) carbon atoms, an alkoxy radical having from 1 to 5 carbon atoms or a phenoxy, benzyloxy, trifluoromethyl or acetyl radical.It further relates toa method of preparing said productsand the drugs in which said products are present.Type: GrantFiled: December 12, 1990Date of Patent: May 5, 1992Assignee: Institut de Recherches Chimiques et Biologiques Appliquees (I.R.C.E.B.A.)Inventors: Patrick Houziaux, Jean-Pierre Riffaud, Jean-Yves Lacolle, Bernard Danree
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Patent number: 5087698Abstract: A process for the optical resolution of racemic dropropizine, carried out using L(+)tartaric acid as the optical resolution agent in aqueous medium, is described.Type: GrantFiled: July 19, 1990Date of Patent: February 11, 1992Assignee: Dompe' Farmaceutici S.p.A.Inventor: Roberto Giani
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Patent number: 5081246Abstract: Novel quinoline sulfonamino derivatives having a vessel smooth muscle relaxation activity as well as a platelet agglutination inhibitory activity and inhibitory activity to protein kinase A, myosin light chain kinase, proteinkinase C, and calmodulindependent proteinkinase II, but having little action or cardio function; a process for the production of the derivatives, and a pharmaceutical composition containing the derivative.Type: GrantFiled: December 20, 1989Date of Patent: January 14, 1992Assignees: Hiroyoshi Hidaka, Tobishi Yakuhin Kogyo Kabushiki KaishaInventors: Horoyoshi Hidaka, Tomohiko Ishikawa, Masatoshi Hagiwara, Tsutomu Inoue, Kenji Naitoh, Osamu Sakuma, Masayuki Yuasa, Tadashi Morita, Tadashi Toshioka, Isao Umezawa, Takashi Inaba
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Patent number: 5064863Abstract: Tertiary and secondary amines of the formulas ##STR1## wherein n is the integer 1 or 2, p0 R is hydrogen, lower-alkanoyl or phenyl-lower-alkanoyl,X.sup.1 is phenoxymethyl optionally mono-fluorinated or mono-chlorinated in the ortho-position,X.sup.2 is lower-alkyl, phenoxymethyl optionally mono-fluorinated or mono-chlorinated in the ortho-position or phenyl optionally monosubstituted by fluorine, chlorine, trifluoromethyl or lower-alkoxy,Y is hydrogen or methyl, andZ is a phenyl or thienyl residue substituted as hereinafter described,and the physiologically and pharmaceutically compatible salts are described. The compounds of formulas I and V-1 have catabolic activity and can be used for the treatment of obesity and diabetes mellitus or for the treatment of conditions which are associated with an increased protein breakdown, or as feed additives for fattening animals. The compounds of formulas I and V-1 can be prepared starting from corresponding primary amines.Type: GrantFiled: December 10, 1987Date of Patent: November 12, 1991Assignee: Hoffmann-La Roche Inc.Inventors: Leo Alig, Marcel Muller
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Patent number: 5053409Abstract: There is disclosed an aminobenzenesulfonic acid derivative of the formula: ##STR1## wherein R.sub.1 represents hydrogen atom, a C.sub.1 -C.sub.6 alkyl group, a C.sub.3 -C.sub.7 cycloalkyl group, a C.sub.1 -C.sub.4 halogenated alkyl group, a halogen atom or a C.sub.6 -C.sub.12 aryl group, R.sub.2 represents hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a C.sub.7 -C.sub.12 aralkyl group which may have at least one substituent selected from cyano group, nitro group, C.sub.1 -C.sub.6 alkoxy groups, halogen atoms, C.sub.1 -C.sub.6 alkyl groups and amino groups, and n represents an integer of 1 to 4, of a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 22, 1990Date of Patent: October 1, 1991Assignee: Mitsubishi Kasei CorporationInventors: Hiromi Okushima, Akihiro Narimatsu, Makio Kobayashi, Naoya Satoh, Miyuki Morita
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Patent number: 5051423Abstract: Novel derivatized alkanolamines of the following structural formula ##STR1## are described as useful cardiovascular agents. Most especially described is their usefulness as cardiovascular agents exhibiting an antiarrhythmic effect. Said antiarrhythmic effect is of a combination Class II/Class III variety. Pharmaceutical formulations containing such compounds are also described.Type: GrantFiled: July 13, 1988Date of Patent: September 24, 1991Assignee: Schering AGInventors: Randall E. Lis, William C. Lumma, Jr., Thomas K. Morgan, Jr., Klaus Nickisch, Ronald A. Wohl
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Patent number: 5037828Abstract: The present invention provides compounds of the general formula: ##STR1## wherein R.sub.1 is a hydroxyl group or a methoxy radical, R.sub.2 is a hydrogen atom or a hyroxyl group and R.sub.3 is a hydrogen atom or a hydroxyl group, with the proviso that R.sub.2 and R.sub.3 are not simultaneously hydrogen atoms when R.sub.1 is a methoxy radical; and the pharmacologically acceptable salts thereof.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.Type: GrantFiled: June 6, 1990Date of Patent: August 6, 1991Assignee: Boehringer Mannheim GmbHInventors: Gisbert Sponer, Harald D. Borbe-Volmer, Jurgen Engel, Bernhard Kutscher, Georg Niebch, Marianne Siebert-Weigel
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Patent number: 5001160Abstract: Compounds are disclosed having the formula: ##STR1## in which R.sub.1 is a C.sub.1 l to C.sub.12 alkyl, said alkyl being straight or branched chain, saturated or unsaturated, monosubstituted or unsubstituted, said substituents being selected from piperidine, pyrrolidine, morpholine, thiomorpholine or cycloalkyl of 3 to 7 carbons, a cycloalkyl of 3 to 9 carbons, a lower alkylcycloalkyl of 4 to 9 carbons, or a polycycloalkyl of 2 to 3 rings containing 7 to 12 carbons;R.sub.Type: GrantFiled: June 27, 1989Date of Patent: March 19, 1991Assignee: Marion Laboratories, Inc.Inventors: Daniel W. McPherson, John P. Carter
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Patent number: 4988814Abstract: Compounds of the formula: ##STR1## in which R.sup.1 is alkyl; R.sup.2 and R.sup.3 are alkyl or taken together they are polymethylene, R.sup.2 and R.sup.3 complete a 5-norbornen-2-yl moiety; X is --CO.sub.2 --, --OCO--, --OCO.sub.2 --, --N(R.sup.7)CO--, --NHNHCO--, --ON(R.sup.7)CO--, --CON(R.sup.7)--, --N(R.sup.7)CO.sub.2 --, --OCON(R.sup.7)-- or --N(R.sup.7)CON(R.sup.8)--, wherein R.sup.7 and R.sup.8 are, independently, hydrogen, alkyl, phenyl, benzyl, substituted phenyl or substituted benzyl in which the substituents are halo, alkyl alkoxy, cyano, nitro or perhalomethyl; R.sup.4 is hydrogen or alkyl; R.sup.5 is hydrogen, alkyl, hydroxyalkyl, phenyl, benzyl, substituted phenyl or substituted benzyl in which the substituents are hydroxy, halo, alkyl alkoxy, trifluoromethyl, nitro, cyano, carbalkoxy, carboxamido, amino, alkylamino or dialkylamino; R.sup.Type: GrantFiled: October 27, 1989Date of Patent: January 29, 1991Assignees: American Home Products Corp., John Wyeth & Bro.Inventors: Magid A. Abou-Gharbia, John P. Yardley, Ian A. Cliffe
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Patent number: 4963680Abstract: A piperazine derivative of formula (I) ##STR1## in which: R is hydrogen or a straight or branched (C.sub.1 -.sub.4) alkoxycarbonyl group; andA is a 7-methoxy-1-naphthalenyl, 6-methoxy-2,3-dihydro-1-(1H)-indenyl or 7-methoxy-1,2,3,4-tetrahydro-1-naphthalenyl group, or an optically active isomer thereof, or a salt thereof.Type: GrantFiled: August 2, 1989Date of Patent: October 16, 1990Assignee: SynthelaboInventors: Philippe Manoury, Jean Binet, Daniel Obitz, Gerard Defosse, Elisabeth Dewitte, Corinne Veronique
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Patent number: 4954498Abstract: The present invention provides tricyclic benzimidazoles of the formula: ##STR1## wherein R.sub.1 is a phenyl radical of the general formula: ##STR2## wherein R.sub.2, R.sub.3 and R.sub.4 can be the same or diferent as in claim 1. For A, B, C and D are understood those compounds where one or two of A, B, C or D are nitrogen. These compounds are useful to inhibit the aggregation of thrombocytes and erythrocytes, lower blood pressure and can increase the power of the heart.Type: GrantFiled: January 15, 1988Date of Patent: September 4, 1990Assignee: Boehringer Mannheim GmbHInventors: Alfred Mertens, Wolfgang von der Saal, Erwin Boehm, Klaus Strein
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Patent number: 4948892Abstract: A sulfonamide compound represented by the following formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are identical or different, and each represents a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group; R.sup.4 represents a hydrogen atom, a lower alkyl group, or a substituted or unsubstituted aralykyl group; R.sup.5 represents a substituted or unsubstituted aryl group or a substituted or unsubstituted aralkyl group; R.sup.6 and R.sup.7 are identical or different and each represents a hydrogen atom, a lower alkyl group or a lower alkoxy group; and n is an integer of 1 to 8,and an acid addition salt thereof. The compounds of formula (I) provided by this invention have some useful biological activities such as the spasmolytic activity on the vascular smooth muscles and anti-platelet aggregatory activity and are useful as drugs for treating cardiovascular disorders such as angina pectoris, cerebral circulation disorder and thrombosis.Type: GrantFiled: February 15, 1989Date of Patent: August 14, 1990Assignee: Kowa Comp., Ltd.Inventors: Sohei Tanabe, Seiichi Sato, Yoshinori Kyotani, Tomio Ohta, Yasumi Uchida
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Patent number: 4935426Abstract: N,N'-disubstituted piperazines of the general formula I ##STR1## where the group is unsaturated (.dbd.) or saturated (--) and the substituents R.sup.1, R.sup.2 and A have the following meanings:A is --, --CH.dbd., --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --,R.sup.1 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, alkylcycloalkyl, cycloalkenylalkyl, alkylcycloalkenyl, bicycloalkyl, bicycloalkylalkyl or alkylbicycloalkyl, these radicals being unsubstituted or substituted by hydroxy, halogen, alkoxy or trialkylsilyl,R.sup.1 is further heterocycloalkyl with oxygen and/or sulfur, heterocycloalkylmethyl with oxygen and/or sulfur, alkyl-substituted heterocycloalkylmethyl with oxygen and/or sulfur, andR.sup.2 is alkyl, alkoxy, trimethylsilyl, cycloalkyl, alkylthio,and plant-physiologically tolerated salts thereof, and fungicides containing these compounds.Type: GrantFiled: February 8, 1989Date of Patent: June 19, 1990Assignee: BASF AktiengesellschaftInventors: Matthias Zipplies, Hubert Sauter, Franz Roehl, Thomas Kuekenhoehner, Lothar Janitschke, Eberhard Ammermann, Gisela Lorenz
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Patent number: 4931443Abstract: A piperazine compound represented by the general formula: ##STR1## (wherein each of the symbols is as defined above) or a pharmaceutically acceptable acid addition salt thereof, and pharmaceutical uses thereof as well as intermediates thereof are disclosed. The above piperazine compounds possess antipsychotic activities with less adverse reaction on the extrapyramidal system and are useful as drugs.Type: GrantFiled: June 24, 1988Date of Patent: June 5, 1990Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Toru Nakao, Kenji Morita, Minoru Obata, Yasuto Morimoto
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Patent number: 4873331Abstract: The compounds of the following structural formula posses useful anxiolytic, antidepressant, antipsychotic and learning and memory enhancement properties: ##STR1## in which R.sup.1 is 3-noradamantyl;n is 0 or 1;X is --CO.sub.2 --, --O.sub.2 C-- or --OCO.sub.2 --;m is 1, 2, 3, 4, or 5;andR.sup.2 is phenyl, benzyl, pyridinyl, pyrimidinyl, pyrazinyl or substituted phenyl or benzyl in which the substituent is alkyl, alkoxy, halo, cyano, nitro or trifluoromethyl;or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 9, 1988Date of Patent: October 10, 1989Assignee: American Home Products CorporationInventors: Wayne E. Childers, Jr., Magid A. Abou-Gharbia
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Patent number: 4870078Abstract: The present invention provides a taurine-type compound of the formula ##STR1## wherein R is a phenyl group optionally having substituent(s) selected from lower alkyl, halogen-substituted lower alkyl, lower alkoxy, lower alkanoyl and halogen atom; and n is 2 or 3. The above compound is useful as an agent for improving microcirculation.Type: GrantFiled: April 4, 1988Date of Patent: September 26, 1989Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Kiyoshi Eshima, Kazuo Ogawa, Shigeru Kaneko
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Patent number: 4826844Abstract: Compounds of the formula: ##STR1## in which m is one of the integers 1, 2 or 3; n is one of the integers 0, 1 or 2; o is one of the integers 0, 1 or 2; R.sub.1 and R.sub.2 are, independently, hydrogen, hydroxyl, alkyl, alkoxy, alkanoyloxy, trifluoromethyl, halo, or, when taken together, 3,4-methylenedioxy; R.sub.3 is alkyl, ##STR2## where R.sub.4 and R.sub.5 are, independently, hydrogen, hydroxyl, alkyl, alkoxy, alkanoyloxy, halo or trifluoromethyl; and R.sub.6 is hydrogen or halo; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: September 30, 1987Date of Patent: May 2, 1989Assignee: American Home Products CorporationInventors: G. E. M. Husbands, Gary P. Stack
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Patent number: 4814507Abstract: A novel sulfone compound represented by the general formula (I) ##STR1## wherein R.sup.1 is cyclohexyl, phenyl; or a phenyl substituted with a group selected from nitro, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are respectively hydrogen, halogen, cyano or carbonyl, wherein R.sup.1 and R.sup.2 may form an o-phenylene or an o-phenylene substituted with at least one group selected from nitro C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen; X is oxygen or methylkene; Y is -(CH.sub.2).sub.n --, wherein n is an integer of 0, 5 or 6, or ##STR2## wherein m is an integer 1-3; R.sup.6 is hydrogen, C.sub.1 -C.sub.3 alkyl, .omega.-alkylaminoalkyl, wherein each alkyl has 1-3 carbon atoms, or .omega.-dialkylaminoalkyl, wherein each alkyl has 1-3 carbon atoms; R.sup.7 is hydrogen or C.sub.1 -C.sub.3 alkyl; and R.sup.6 and R.sup.7 may form a ring together with N, or ##STR3## wherein R.sup.8 is hydrogen, C.sub.1 -C.sub.Type: GrantFiled: September 14, 1987Date of Patent: March 21, 1989Assignee: Mitsubishi Chemical Industries, LimitedInventors: Akihiro Tobe, Shinichiro Fujimori, Tomoshi Yamazaki, Mamoru Sugano, Ryoji Kikumoto, Issei Nitta
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Patent number: 4797401Abstract: Antiarrhythmic agents of the formula: ##STR1## and their pharmaceutically acceptable salts, wherein R and R.sup.1, which are the same or different, are C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.7 cycloalkyl, --CH.sub.2 CH.sub.3, --CH.sub.2 Cl, --CF.sub.3 or --NH.sub.2 ;R.sup.2 and R.sup.3, which are the same or different, are H, halo, CF.sub.3, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy; andX is --CH.sub.2 --, ##STR2## or --CH(OH)--.Type: GrantFiled: July 15, 1987Date of Patent: January 10, 1989Assignee: Pfizer Inc.Inventors: John E. G. Kemp, Peter E. Cross
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Patent number: 4780466Abstract: There are disclosed compounds of the formula ##STR1## wherein the group A is ##STR2## where R.sub.1 and R.sub.2 are each independently hydrogen or loweralkyl, or R.sub.1 +R.sub.2 =(CH.sub.2).sub.m, m being 2 to 6, p is 1 or 2, and each X is independently hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro, amino, loweralkylamino, diloweralkylamino, trifluoromethyl or loweralkylthio; W is O, H.sub.2 or [H, OH]; n is 2, 3 or 4; and R.sub.3 is ##STR3## where q is 1 or 2 and each Y is independently hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro, amino, loweralkylamino, diloweralkylamino, trifluoromethyl or loweralkylthio, which are useful as antipsychotic, anxiolytic and analgesic agents.Type: GrantFiled: March 17, 1988Date of Patent: October 25, 1988Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Nicholas J. Hrib, John G. Jurcak
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Patent number: 4734500Abstract: A novel sulfone compound represented by the general formula (I) ##STR1## wherein R.sup.1 is cyclohexyl, phenyl; or a phenyl substituted with a group selected from nitro, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are respectively hydrogen, halogen, cyano or carbonyl, wherein R.sup.1 and R.sup.2 may form an o-phenylene or an o-phenylene substituted with at least one group selected from nitro C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen; X is oxygen or methylene; Y is --(CH.sub.2).sub.n --, wherein n is an integer of 0, 5 or 6, or ##STR2## wherein m is an integer 1-3; R.sup.6 is hydrogen, C.sub.1 -C.sub.3 alkyl, .omega.-alkylaminoalkyl, wherein each alkyl has 1-3 carbon atoms, or .omega.-dialkylaminoalkyl, wherein each alkyl has 1-3 carbon atoms; R.sup.7 is hydrogen or C.sub.1 -C.sub.3 alkyl; and R.sup.6 and R.sup.7 may form a ring together with N, or ##STR3## wherein R.sup.8 is hydrogen, C.sub.1 -C.sub.Type: GrantFiled: March 11, 1986Date of Patent: March 29, 1988Assignee: Mitsubishi Chemical Industries LimitedInventors: Akihiro Tobe, Shinichiro Fujimori, Tomoshi Yamazaki, Mamoru Sugano, Ryoji Kikumoto, Issei Nitta
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Patent number: 4721715Abstract: Compounds of the formula (I): ##STR1## wherein n is 0 or 1, R.sub.1 is H or a lower alkyl of 1 to 6 carbon atoms, R.sub.2 is an unsubstituted phenyl group or a phenyl group substituted by one or more of the same or different substituents selected from the group consisting of hydroxy, lower alkyl of 1 to 6 carbon atoms, lower alkoxy of 1 to 6 carbon atoms, chloro, fluoro, trifluoromethyl or a 2-, 3- or 4- pyridyl ring, in the form of a free base or a pharmaceutically acceptable acid addition salt thereof.The compounds of the present invention are useful in cardiovascular, antiallergy, psychotropic and hypolipidemic therapy.Type: GrantFiled: August 7, 1985Date of Patent: January 26, 1988Assignee: Societe Cortial, S.A.Inventors: Marie-Helene Creuzet, Claude Feniou, Francoise Guichard, Henri Pontagnier, Gisele Prat
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Patent number: 4698343Abstract: A compound of the formula ##STR1## wherein R.sub.1 is C.sub.3 -C.sub.6 branched alkyl group, e.g., an isopropyl group or a tert-butyl group, R.sub.2 is a C.sub.1 -C.sub.6 alkoxy group, e.g., a methoxy, an ethoxy or a propoxy group, and X is a CHOH group or a (CH.sub.2).sub.n --group where n=0, 1 or 2 and a process for making this compound are disclosed.This compound is useful in human and veterinary therapeutics.Type: GrantFiled: September 19, 1985Date of Patent: October 6, 1987Assignee: Societe Cortial, S.A.Inventors: Marie-Helene Creuzet, Claude Feniou, Francoise Guichard, Henri Pontagnier, Gisele Prat
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Patent number: 4616017Abstract: Novel tertiary aminohydroxypropoxy substituted aryl compounds exhibit .alpha..sub.1 -adrenoceptor and serotonin antagonism and are also useful as antihypertensive agents.Type: GrantFiled: June 4, 1984Date of Patent: October 7, 1986Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Gerald S. Ponticello
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Patent number: 4613598Abstract: A piperazine derivative according to the present invention has the following general formula [I]: ##STR1## wherein R.sup.1 is --OH, --OR.sup.3, --SR.sup.3, --SOR.sup.3 or --SO.sub.2 R.sup.3 wherein R.sup.3 is alkyl group having 1 to 3 carbon atoms;R.sup.2 is --SO.sub.2 NH.sub.2, --SO.sub.2 NHR.sup.4, --SO.sub.2 NR.sup.4 R.sup.5, --COOH, --COOR.sup.4, --CONH.sub.2, --CONHR.sup.4, --CONR.sup.4 R.sup.5, --NHCONH.sub.2, --NHCSNH.sub.2, --NHCONHR.sup.4, --NHCOR.sup.4 or --NHSO.sub.2 R.sup.4 wherein R.sup.4 and R.sup.5 are independently alkyl group having 1 to 3 carbon atoms; orR.sup.1 and R.sup.2 together with carbon atoms to which they are attached form ##STR2## Z is --CO-- or --CH(OH)--; Ar is pyridyl or substituted or unsubstituted phenyl; andn is an integer of 3 to 5.An acid addition salt of the piperazine derivative having the above formula [I] is included in the present invention.Type: GrantFiled: March 6, 1985Date of Patent: September 23, 1986Assignee: Mitsubishi Chemical Industries LimitedInventors: Harukazu Fukami, Shinya Inoue, Issei Nitta, Kenichiro Nakao, Ryoji Kikumoto