Chalcogen Attached Indirectly To The Piperazine Ring By Nonionic Bonding Patents (Class 544/398)
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Patent number: 5696123Abstract: The invention relates to new compounds of general formula I ##STR1## and the pharmaceutically acceptable salts thereof, wherein A, B, Z, R.sup.1, R.sup.2, R.sup.3 and m are defined as in the specification, processes for preparing them and pharmaceutical compositions containing these compounds. The compounds are valuable neurokinin (tachykinin) antagonists.Type: GrantFiled: June 7, 1995Date of Patent: December 9, 1997Assignee: Boehringer Ingelheim KGInventors: Horst Dollinger, Gerd Schorrenberg, Hans Briem, Birgit Jung, Georg Speck
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Patent number: 5691340Abstract: A compound selected from those of formula (I): ##STR1## where RA, RB, RC, RD, A, n, X, Y and Ar are defined in the description, and a medicinal product comprising the same for treating a mammal afflicted with a disease associated with sigma receptors.Type: GrantFiled: September 14, 1995Date of Patent: November 25, 1997Assignee: Adir et CompagnieInventors: Genevieve Baziard-Mouysset, Sallouma Younes, Youssef Labssita, Marc Payard, Daniel-Henri Caignard, Pierre Renard, Marie-Claire Rettori
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Patent number: 5686609Abstract: The invention relates to compounds of the formula ##STR1## in which: m is 2 or 3;Ar and Ar' independently are a thienyl group; a substituted or unsubstituted phenyl group; or an imidazolyl group; it also being possible for Ar' to be a benzothienyl group which is unsubstituted or substituted by a halogen; a naphthyl group which is unsubstituted or substituted by a halogen; a biphenyl group; or a substituted or unsubstituted indolyl;X is hydrogen;X' is hydrogen or a hydroxyl group or is joined to X" below to form a carbon-carbon bond, or X and X' together form an oxo group or a dialkylaminoalkoxyimino group of the formula .dbd.N--O--(CH.sub.2).sub.p --Am, in which p is 2 or 3 and Am is a dialkylamino group;Y is a nitrogen atom or a group C(X"), in which X" is hydrogen or forms a carbon-carbon bond with X';Q is hydrogen, a C.sub.1 -C.sub.4 alkyl group or an aminoalkyl group of the formula --(CH.sub.2).sub.Type: GrantFiled: March 11, 1994Date of Patent: November 11, 1997Assignee: SanofiInventors: Xavier Emonds-Alt, Pierre Goulaouic, Vincenzo Proietto, Didier Van Broeck
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Patent number: 5670546Abstract: N-arylalkylphenylacetamide compounds of formula (I), and pharmaceutically acceptable salts thereof, possess potent analgesic and anti-inflammatory activities.Type: GrantFiled: January 11, 1996Date of Patent: September 23, 1997Assignee: Korean Research Institute of Chemical TechnologyInventors: No-Sang Park, Young-Sik Jung, Churl-Min Seong, Jong-Cheol Lee, Jin-Il Choi, Seung-Won Choi, Yeon-Joo Choi, Kwang-Sook Lee
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Patent number: 5668138Abstract: A compound selected from those of formula (I): ##STR1## where RA, RB, RC, RD, A, n, X, Y and Ar are defined in the description, and a medicinal product comprising the same for treating a mammal afflicted with a disease associated with sigma receptors.Type: GrantFiled: July 10, 1996Date of Patent: September 16, 1997Assignee: Adir Et CompagnieInventors: Genevieve Baziard-Mouysset, Sallouma Younes, Youssef Labssita, Marc Payard, Daniel-Henri Caignard, Pierre Renard, Marie-Claire Rettori
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Patent number: 5668136Abstract: A benzene, pyridine or pyrimidine derivative having the below shown formula is novel and useful as an anti-arteriosclerotic agent. ##STR1## wherein R.sup.1 stands for a lower alkyl group, an amino group which may be substituted, or the like; R.sup.2 stands for a group represented by the formula: ##STR2## (wherein R.sup.16 stands for an alkyl group having 1 to 6 carbon atoms, or the like) or the like; R.sup.3 stands for a group represented by the formula: --O--(CH.sub.2).sub.m --Y (Y stands for an imidazolyl or piperazinyl group, or the like and m is 1 to 6) or the like; R.sup.5 stands for a hydrogen atom, a lower alkyl group, or the like; A stands for a group represented by the formula: ##STR3## (wherein R.sup.6 stands for a hydrogen atom, a lower alkyl group, or the like), --N.dbd., or the like; and B stands for a group represented by the formula: ##STR4## (wherein R.sup.4 stands for a hydrogen or the like), --N.dbd., or the like.Type: GrantFiled: September 11, 1991Date of Patent: September 16, 1997Assignee: Eisai Co., Ltd.Inventors: Teiji Kimura, Nobuhisa Watanabe, Yasutaka Takase, Kenji Hayashi, Makoto Matsui, Hironori Ikuta, Youji Yamagishi, Kozo Akasaka, Hiroshi Tanaka, Issei Ohtsuka, Takao Saeki, Motoji Kogushi, Tohru Fujimori, Isao Saito
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Patent number: 5659065Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aromatic or heteroaromatic radical, a hydroxy group that is aliphatically, araliphatically or heteroarylaliphatically etherified or protected by a hydroxy-protecting group, or an aliphatically etherified mercapto group, andR.sub.2 is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic or heteroarylaliphatic radical, orR.sub.1 and R.sub.2 together form a divalent aliphatic radical,R.sub.3 is free or aliphatically, araliphatically or aromatically esterified carboxy, formyl or hydroxymethyl,R.sub.4 is hydrogen, an aliphatic or araliphatic radical or an amino-protecting group, andR.sub.5 is hydrogen or an aliphatic radical,and the salts thereof can be used as intermediates in the preparation of medicinal active ingredients.Type: GrantFiled: April 4, 1995Date of Patent: August 19, 1997Assignee: Novartis CorporationInventor: Richard Goschke
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Patent number: 5622953Abstract: This invention relates to 1-amino-3-phenoxy-propane-derivatives of formula 1: ##STR1## (in which A, B, R, R.sup.x, X and Z are defined as in the specification described) and methods for their preparation.These compounds may be used as modulators of multidrug resistance in cancer chemotherapy and for circumvention of resistance in the treatment of malaria.Type: GrantFiled: June 6, 1995Date of Patent: April 22, 1997Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Andreas Kling, Stefan Mueller, Kurt Ritter, Rainer Schlecker, Gerhard Keilhauer, Cynthia Romerdahl, Ulrich Traugott
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Patent number: 5618938Abstract: Compounds of the formula ##STR1## and their salts with mineral or organic acids are useful as neurokinin receptor antagonists. Methods of preparing the compounds, especially pure STEREO ISOMERS thereof, are provided.Type: GrantFiled: June 7, 1995Date of Patent: April 8, 1997Assignee: SanofiInventors: Xavier Emonds-Alt, Pierre Goulaouic, Vincenzo Proietto, Didier Van Broeck
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Patent number: 5614548Abstract: Quaternary amine-containing ether lipid analogs of the formulaR.sub.1 --X--R.sub.2 --N.sup.+ (R.sub.3) (R.sub.4) (R.sub.5) Z.sup.-are disclosed. R.sub.1 represents a hydrophobic group and R.sub.2 represents the backbone of the molecule, with the quaternary amine being linked directly to the backbone. Pharmaceutical compositions including these compounds and methods of combating tumors with these compounds are disclosed. Also disclosed is a method of combating viral infections with both these compounds and ET-18-OMe and its analogs.Type: GrantFiled: September 8, 1994Date of Patent: March 25, 1997Assignee: Wake Forest UniversityInventors: Claude Piantadosi, Khalid S. Ishaq, Canio J. Marasco, Jr., Larry W. Daniel, Louis S. Kucera, Edward J. Modest, Barry P. Goz
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Patent number: 5614536Abstract: Substituted N-aminoalkylmethane sulfanilide of formula (I), their solutions and pharmaceutically acceptable addition salts, their pharmaceutical compositions and their therapeutic use. In formula (I) Y represents hydrogen, cyano, nitro, amino, acetamide or halogen; n is an integer between 2 and 4, R.sup.1 and R.sup.2 equal or different are alkyl-(C1-C4) or they are connected together and with the N-atom thereby forming a 1-pyrrolidinyl, 1-piperidinyl, 1-piperazinyl, 4-methyl-1-piperazinyl, 4-ethylpiperazinyl, 4-propylpiperazinyl, 1-homopiperidinyl or 4-morpholine residue. The products of formula (I) are used as antispasmodic agents.Type: GrantFiled: January 7, 1994Date of Patent: March 25, 1997Assignee: Roemmers S.A.I.C.F.Inventors: Carlos E. A. Monti, Gustavo E. Aldom a
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Patent number: 5612378Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds of structure: ##STR1## wherein each R.sup.1 is independently one of alkyl, substituted alkyl, cycloalkyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl;each R.sup.2 and R.sup.3 is independently one of hydrogen, alkyl, aryl or arylalkyl;Y is a bond, or is one of --(CH.sub.2).sub.p --, cycloalkyl, aryl or C.sub.2-10 heterocycle; andm, n and p are each independently 1 to 10.Type: GrantFiled: June 6, 1995Date of Patent: March 18, 1997Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Lu Tianbao, Richard M. Soll
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Patent number: 5599933Abstract: The reaction product of:(a) a compound of the formula: ##STR1## wherein X is a member selected from the group consisting of N, O and S; R.sub.1 and R.sub.2 are independently a straight or branched, saturated or unsaturated non-aromatic hydrocarbon of four to eighteen carbon atoms; m is 1 or 2; and n is 0, 1 or 2; and(b) a compound selected from the group consisting of primary, secondary, tertiary and higher amines, which are liquid at room temperature.The reaction product of the present invention has excellent surfactant properties, and is suitable for use in coloring compositions to improve the fugitivity from skin and clothing. The reaction product is also useful as a cleansing agent.Type: GrantFiled: March 15, 1995Date of Patent: February 4, 1997Assignee: Binney & Smith Inc.Inventor: Richard J. Kaiser
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Patent number: 5595993Abstract: Piperidinyl-substituted cyclohexanes of Formula I have anti-ischemic properties: ##STR1## wherein R=R.sub.1 and is independently H or halogen; or R and R.sub.1 may be taken together to form an --O(CH.sub.2).sub.m O-- (m=1 or 2);X=a phenyl residue;R.sub.2 =R.sub.3 and is independently H or C.sub.1-4 alkyl; andR.sub.4 =phenyl or substituted phenyl wherein the phenyl group is mono-, or di-substituted with groups selected from: F, Cl, I and C.sub.1-4 alkoxy.Type: GrantFiled: September 14, 1994Date of Patent: January 21, 1997Assignee: Bristol-Myers Squibb CompanyInventors: Ronald J. Mattson, John D. Catt
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Patent number: 5596099Abstract: A process for the preparation of N-(2-sulfatoethyl)-piperazine in high purity, which comprises reacting N-(2-hydroxyethyl)piperazine in a mixture of highly--or relatively highly--concentrated sulfuric acid and oleum or chlorosulfonic acid at temperatures of from about 80.degree. to about 250.degree. C., transferring the resulting sulfonation mixture to a water-miscible aliphatic alcohol, isolating the N-(2-sulfatoethyl)piperazine sulfate formed, treating the N-(2-sulfatoethyl)piperazine sulfate, still moist with alcohol, at temperatures of from about 35.degree. to about 90.degree. C. with a basic compound in a mixture of a (C.sub.1 -C.sub.2)-alkanol and water, separating off the precipitated sulfate of the basic compound employed, and isolating the N-(2-sulfatoethyl)piperazine formed, by the addition of (C.sub.1 -C.sub.2)-alkanol.Type: GrantFiled: March 15, 1995Date of Patent: January 21, 1997Assignee: Hoechst AktiengesellschaftInventors: Michael Meier, Heinz-Georg Kautz
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Patent number: 5585378Abstract: The present invention relates to an oxindole compound having the formula 5-cyclohexyl-1,3-dihydro-1-[2-[4-(phenylmethyl)-1-piperazinyl]ethyl]-2H-in dol-2-one for the prevention or treatment of cognitive dysfunctions.Type: GrantFiled: June 6, 1995Date of Patent: December 17, 1996Assignee: Aktiebolaget AstraInventors: Bernard R. Boar, Alan J. Cross
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Patent number: 5563271Abstract: Preparation of N-(2-sulfatoethyl)piperazine sulfate by reacting N-(2-hydroxyethyl)piperazine in a mixture of high- or relatively high-percentage sulfuric acid and oleum or chlorosulfonic acid at temperatures of about 80.degree. C. to about 250.degree. C., introducing the sulfation mixture formed into a water-miscible aliphatic alcohol and isolating the N-(2-sulfatoethyl)piperazine sulfate formed.Type: GrantFiled: March 15, 1995Date of Patent: October 8, 1996Assignee: Hoechst AG.Inventors: Michael Meier, Heinz-Georg Kautz, Andreas Schrell
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Patent number: 5554641Abstract: The small nonpeptides of the instant invention are tachykinin antagonists. The compounds are highly selective and functional NK.sub.3 antagonists expected to be useful in the treatment of pain, depression, anxiety, panic, schizophrenia, neuralgia, addiction disorders, inflammatory diseases, gastrointestinal disorders, vascular disorders, and neuropathological disorders.Type: GrantFiled: March 20, 1995Date of Patent: September 10, 1996Inventors: David C. Horwell, Martyn C. Pritchard, Jennifer Raphy
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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: 5523303Abstract: The invention relates to novel, pharmaceutically active trisubstituted cycloalkane derivatives, a process for the preparation thereof and pharmaceutical compositions comprising the same. The invention also encompasses the use of the said cycloalkane derivatives for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases.The compounds according to the invention are characterized by the general formula (I), ##STR1## wherein R represents hydrogen, C.sub.1-4 alkyl or hydroxyl,R.sup.1 stands for C.sub.1-12 alkyl,R.sup.2 and R.sup.3 each represents hydrogen, C.sub.1-12 alkyl or C.sub.2-12 alkenyl, orR.sup.2 and R.sup.3 together with the adjacent nitrogen atom form a 4- to 7-membered ring optionally comprising an oxygen, sulfur or a further nitrogen atom, which latter may carry a phenyl, benzyl or C.sub.1-4 alkyl substituent,R.sup.4 and R.sup.5 each stands for hydrogen, halogen or C.sub.Type: GrantFiled: April 11, 1994Date of Patent: June 4, 1996Assignee: Egis Gyogyszergyar Rt.Inventors: Judit Bajnogel, Gabor Blasko, Zoltan Budai, Andras Egyed, Marton Fekete, Erika Karaffa, Tibor Mezei, Klara Reiter nee Esses, Gyula Simig, Katalin Szemeredi, Eniko Szirt nee Kiszelly
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Patent number: 5520829Abstract: Lube oils of improved properties contain ethylene-propylene copolymer bearing moieties derived from the reaction product of allyl glycidyl ether and a heterocyclic amine such as N-(3-aminopropyl) morpholine.Type: GrantFiled: January 10, 1995Date of Patent: May 28, 1996Assignee: Texaco Inc.Inventors: Maria M. Kapuscinski, Christopher S. Liu, Larry D. Grina, Ronald E. Jones
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Patent number: 5492913Abstract: The compounds are N-(unsubstituted or substituted) N'-benzylpiperazine compounds and pharmaceutically tolerable salts thereof, useful for treating neuronal disorders resulting from the dysfunctioning of oxidative metabolism.A compound disclosed is: N-ethyl N'-(2-hydroxy-3,4- dimethoxybenzyl)-piperazine and its dihydrochloride.Type: GrantFiled: March 23, 1994Date of Patent: February 20, 1996Assignee: Adir et CompagnieInventors: Michel Wierzbicki, Jean Lepagnol, Jean-Paul Tillement, Bernard Testa, Yves Rolland
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Patent number: 5486528Abstract: Novel basic ether of general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, halogen or C.sub.1-4 alkoxy, or together they represent a 3,4-methylenedioxy group,R stands for C.sub.1-8 alkyl,R.sup.3 represents hydrogen, C.sub.1-4 alkyl or hydroxy,A is a valency bond or methylene group,R.sup.4 and R.sup.5 are independently hydrogen, C.sub.1-12 alkyl or C.sub.1-12 alkenyl, orR.sup.4 and R.sup.5 form together with the adjacent nitrogen atom 1-pyrrolidinyl, 1-piperidinyl, morpholino or 1-piperazinyl groups, stereo and optically active isomers and their possible mixtures, acid-addition salts and quaternary ammonium derivatives thereof. The basic ethers have antiulceric and anxiolytic activities.Type: GrantFiled: April 11, 1994Date of Patent: January 23, 1996Assignee: Egis Gyogyszergyar Rt.Inventors: Judit Bajnogel, Gabor Blasko, Zoltan Budai, Eva Schmidt, Andras Egyed, Marton Fekete, Istvan Gacsalyi, Istvan Gyertyan, Tibor Mezei, Kalara Reiter nee Esses, Gyula Simig, Katalin Szemeredi, Enik Szirt nee Kiszelly
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Patent number: 5478828Abstract: Novel piperazinyl- and piperidinyl-cyclohexanols are useful as anxiolytic agents and have other psychotropic properties.Type: GrantFiled: January 24, 1995Date of Patent: December 26, 1995Assignee: Bristol-Myers Squibb CompanyInventors: Ronald J. Mattson, John D. Catt
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1,2-ethanediol derivative and salt thereof and cerebral function-improving agent comprising the same
Patent number: 5472984Abstract: 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: December 29, 1993Date of Patent: December 5, 1995Assignee: Toyama Chemical Co., Ltd.Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita -
Patent number: 5466690Abstract: Retinoid-like activity is exhibited by compounds of the formula ##STR1## where R is hydrogen or lower alkyl; A is pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl or pyrazinyl; n is 0-5; and B is H, --COOH or an ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative thereof, or --CHO or an acetal derivative thereof, or --COR.sub.1 or a ketal derivative thereof where R.sub.1 is --(CH.sub.2).sub.m CH.sub.3 where m is 0-4; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 18, 1994Date of Patent: November 14, 1995Assignee: Allergan, Inc.Inventor: Roshantha A. S. Chandraratna
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Patent number: 5464941Abstract: The present invention provides novel substituted biphenyl pyrazines or pyrazine derivatives ("BPD") which are functional and have useful application as a monomer for a variety of high performance polymers such as polyester, polyarylate, polycarbonate, polyetherketones, epoxides, polyimides, polyamides, and polyamides-imides; and as pigments for coating compositions such as paints.Type: GrantFiled: October 19, 1994Date of Patent: November 7, 1995Assignee: Hoechst Celanese CorporationInventors: Richard Vicari, George Kvakovszky, Olan S. Fruchey, Hans J. Metz
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Patent number: 5409931Abstract: 1,3-Substituted cycloalkenes and cycloalkanes are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.Type: GrantFiled: February 4, 1994Date of Patent: April 25, 1995Assignee: Warner-Lambert CompanyInventors: Bradley W. Caprathe, Dennis M. Downing, Juan C. Jaen, Stephen J. Johnson, William J. Smith, III, Lawrence D. Wise, Jonathan Wright, David J. Wustrow
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Patent number: 5389630Abstract: Diamine compounds of formula (I) or an addition salt thereof are provided: ##STR1## These compounds have an excellent cerebral protective action, are very safe, and exhibit a strong action when orally administered, and therefore, medicines containing such compounds are effective for treating disorders caused by cerebral hemorrhage, cerebral infarction, subarachnoid hemorrhage, transient ischemic attack, cerebrovascular disorders and the like, or preventing progress of such disorders.Type: GrantFiled: January 22, 1993Date of Patent: February 14, 1995Assignee: Kowa Co., Ltd.Inventors: Seiichi Sato, Kiyoshi Kawamura, Yoshio Takahashi, Koichiro Watanabe, Sadahiro Shimizu, Tomio Ohta
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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
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Patent number: 5371088Abstract: Compounds of the formula ##STR1## where Ar, R.sup.1, R.sup.2, P and Q have the meanings indicated in the description, and the preparation thereof are described. The compounds have antihypoxic and antiischemic action and are suitable for treating acute and chronic degenerative processes of the CNS and other organs.Type: GrantFiled: September 14, 1993Date of Patent: December 6, 1994Assignee: BASF AktiengesellschaftInventors: Hans-Joerg Treiber, Hans P. Hofmann, Laszlo Szabo
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Patent number: 5354904Abstract: The sulfonamides have the formula ##STR1## where R.sup.1 is C.sub.1 -C.sub.13 -lkyl, substituted or unsubstituted phenyl, C.sub.1 -C.sub.8 -alkanoyl or substituted or unsubstituted benzoyl, andR.sup.2 and R.sup.3 are each independently of one another substituted or unsubstituted C.sub.1 -C.sub.13 -alkyl, substituted or unsubstituted C.sub.5 -C.sub.7 -cycloalkyl or substituted or unsubstituted piperidinyt, or R.sup.2 may also be hydrogen.Type: GrantFiled: October 8, 1992Date of Patent: October 11, 1994Assignee: BASF AktiengesellschaftInventors: Udo Mayer, Ulrike Schloesser
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Patent number: 5352678Abstract: Certain piperazinyl- and piperidinyl-substituted cyclohexanes have anti-ischemic properties.Type: GrantFiled: June 25, 1993Date of Patent: October 4, 1994Assignee: Bristol-Myers Squibb Co.Inventors: Ronald J. Mattson, John D. Catt
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Patent number: 5344845Abstract: Disclosed herein is a specific cinnamic acid derivative such as methyl 4-(4-acetoxy-3-methoxycinnamanide)-1-cyclohexanecarboxylate, or a pharmaceutically acceptable salt thereof. These compounds are useful as IV-type allergic reaction-suppressive drugs.Type: GrantFiled: December 4, 1992Date of Patent: September 6, 1994Assignee: Tsumura & Co.Inventors: Akihide Koda, Koji Waragai, Yutaka Ono, Hideyuki Ozawa, Hideki Kawamura, Masao Maruno, Takeshi Wakamatsu
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Patent number: 5332816Abstract: The present invention relates to novel piperazine-piperidine compounds of the general formula (I) ##STR1## in which R.sub.1 is e.g. hydrogen or methyl, R.sub.2 is e.g. ethylene, m is zero or 1 and n is e.g. 1, and when n is 1, A is e.g. 2,2-dimethyl-1-propanoyl, n-butoxycarbonyl, n-tetradecyloxycarbonyl or 2,4-bis[N-butyl-(2',2',6',6'-pentamethyl-4'-piperidyl)amino]triazin-6-yl.The said compounds are effective as light stabilizers, heat stabilizers and oxidation stabilizers for organic materials.Type: GrantFiled: July 19, 1990Date of Patent: July 26, 1994Assignee: Ciba-Geigy CorporationInventors: Graziano Vignali, Valerio Borzatta
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Patent number: 5328906Abstract: Hydroximic acid derivatives of the formula ##STR1## These compounds are useful for treating diabetes angiopathy.Type: GrantFiled: June 7, 1993Date of Patent: July 12, 1994Assignee: Biorex Kutato-Fejleszto KFTInventors: Peter L. Nagy, Bela Balazs, Maria Boross, Jeno Szilbereky, Gizella Zsila, Lajos Abraham, Gyorgy Blasko, Bela Gachalyi, Attila Almasi, Gabor Nemet
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Patent number: 5326762Abstract: Amides of the formula ##STR1## wherein R.sub.1 and R.sub.2 are independently heteroaryl, X-substituted heteroaryl, X-substituted phenyl, N-substituted triazinyl or N-substituted imidazolyl;and in addition, one of R.sub.1 and R.sub.2 can be as defined above and the other can be phenyl;R.sub.3 is an alkyl chain of 2 to 25 carbon atoms, saturated or unsaturated; an alkyl chain as defined substituted by one or more substituents selected from the group consisting of phenyl, X-substituted phenyl, heteroaryl and X-substituted heteroaryl; an alkyl chain as defined interrupted by one or more groups independently selected from the group consisting of --O--, --S--, --SO--, --SO.sub.2 --, --NH--, --N(lower alkyl)--, --C(O)--, phenylene, X-substituted phenylene, heteroarylene and X-substituted heteroarylene; or an interrupted alkyl chain as defined substituted by one or more substituents selected form the group consisting of phenyl, X-substituted phenyl, heteroaryl and X-substituted heteroaryl;R.sub.Type: GrantFiled: May 19, 1992Date of Patent: July 5, 1994Assignee: Schering CorporationInventors: John Clader, Sundeep Dugar, Timothy Kogan, Bradley Tait, Wayne Vaccaro
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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: 5302720Abstract: Compounds of formula I ##STR1## and their salts in which R.sub.1 is optionally substituted phenyl, R.sub.2 is alkyl, cycloalkyl or optionally substituted amino, or R.sub.2 and R.sub.3 together with the nitrogen and carbon atoms to which they are attached form an optionally substituted heterocyclic ring or R.sub.3 and R.sub.4 together with the nitrogen atom to which they are attached form an optionally substituted heterocyclic ring and R.sub.5 is H, halo, alkyl, alkoxy, trifluoromethyl or a group of formula S(O).sub.m R.sub.8 in which m is 0, 1 or 2 and R.sub.8 is alkyl have utility in the treatment of diabetes particularly in the treatment of hyperglycaemia.Type: GrantFiled: June 17, 1992Date of Patent: April 12, 1994Assignee: The Boots CompanyInventor: Balasubramanian Gopalan
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Patent number: 5298513Abstract: For treatment of disorders of the central nervous system, the cardiovascular system or the intestinal tract, the new substituted basic 2-aminotetralins of the formula ##STR1## in which R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen, alkyl or acyl, andR.sup.3 represents quinuclidine ora group of the formula --(CH.sub.2).sub.a --R.sup.4, --CH.sub.2 --CH.dbd.CH--(CH.sub.2).sub.b --R.sup.4, --CH.sub.2 --C.tbd.C--(CH.sub.2).sub.b --R.sup.4, ##STR2## wherein a denotes a number from 1 to 10,b denotes a number 0, 1, 2, 3 or 4,c denotes a number 0, 1 or 2,d denotes a number 2 or 3, andX denotes oxygen, sulphur or NR.sup.5,and their salts.Type: GrantFiled: May 29, 1992Date of Patent: March 29, 1994Assignee: Bayer AktiengesellschaftInventors: Rudolf Schohe, Thomas Glaser, Jorg Traber, George S. Allen
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Patent number: 5294616Abstract: A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.Type: GrantFiled: March 25, 1992Date of Patent: March 15, 1994Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, Melissa S. Egbertson, Wasyl Halczenko, George D. Hartman, Laura M. Turchi, William L. Laswell
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Patent number: 5283246Abstract: The compounds are substituted trimetazidine useful for the treatment of ischaemic pathologies and peripheral vascular pathology.A compound disclosed is 4-(2,3,4-trimethoxybenzyl)-1-[3-(4-hydroxy-2,3,5-trimethylphenoxy)propyl]p iperazine.Type: GrantFiled: September 17, 1992Date of Patent: February 1, 1994Assignee: Adir et CompagnieInventors: Gilbert Regnier, Jean-Paul Vilaine, Nicole Villeneuve, Jean-Pierre Bidouard, Jean-Pierre Iliou, Albert Lenaers
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Patent number: 5281598Abstract: The invention relates to a piperazine derivative having the formula ##STR1## wherein each .phi. is a phenyl group which may independently be substituted by one or more substituents selected from the group consisting of lower alkyl, lower alkoxy, CF.sub.3, and halogen, and Y is O or S, or a pharmaceutically acceptable salt thereof. The piperazine derivatives have sigma receptor affinity, and may be used for the treatment of psychosis.Type: GrantFiled: April 9, 1993Date of Patent: January 25, 1994Assignee: Akzo N.V.Inventors: Franciscus H. A. Van Bakel, Gerhardus J. Heeres, Ralf Plate, Johannes H. Wieringa
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Patent number: 5281595Abstract: The invention relates to compounds having anti-ischaemic activity, memory enhancing activity and anti-convulsive activity of the formulae 1A and 1B ##STR1## wherein R.sub.1 +R.sub.2 together form an alkylene group having 1-3 C-atoms which may be substituted with one or more alkyl group(s) having 1-3 C-atoms and the remaining R and Z variables are defined as disclosed herein, or a pharmacologically acceptable salt thereof.Type: GrantFiled: March 17, 1992Date of Patent: January 25, 1994Assignee: Duphar International Research B.V.Inventors: Josephus H. M. Lange, Gerrit P. Toorop, Ineke v. Wijngaarden, Jacobus A. J. den Hartog
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Patent number: 5262535Abstract: The reaction product of:(a) a compound of the formula: ##STR1## wherein X is a member selected from the group consisting of N, O and S; R.sub.1 and R.sub.2 are independently a straight or branched, saturated or unsaturated non-aromatic hydrocarbon of four to eighteen carbon atoms; m is 1 or 2; and n is 0, 1 or 2; and(b) a compound selected from the group consisting of primary, secondary, tertiary and higher amines, which are liquid at room temperature.The reaction product of the present invention has excellent surfactant properties, and is suitable for use in coloring compositions to improve the fugitivity from skin and clothing. The reaction product is also useful as a cleansing agent.Type: GrantFiled: February 20, 1992Date of Patent: November 16, 1993Assignee: Binney & Smith Inc.Inventor: Richard J. Kaiser
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Patent number: 5254689Abstract: Compounds of the formula: ##STR1## in which R.sup.1 is alkylsulfonamido of 1 to 6 carbon atoms, arylsulfonamido of 6 to 10 carbon atoms, --NO.sub.2, --CN, 1-imidazolyl or 1,2,4-triazol-1-yl;Y is ##STR2## --CH.sub.2 --, --O--, --S--, or --SO.sub.2 --; X is --CH.dbd. or --N.dbd.;R.sup.2 is hydrogen when n is 0, otherwise it is hydrogen or --OH;n is one of the integers 0, 1, 2, 3, 4, 5 or 6;A is ##STR3## where R.sup.3 is alkylsulfonamido of 1 to 6 carbon atoms, arylsulfonamido of 6 to 10 carbon atoms, --NO.sub.2, --CN, 1-imidazolyl or 1,2,4-triazol-1-yl; or ##STR4## where R.sup.4 is hydrogen or alkyl of 1 to 6 carbon atoms; with the provisos that:a) X is --CH.dbd. when Y is ##STR5## --O-- or --S-- and when Y is ##STR6## and R.sup.2 is --OH; b) X is --N.dbd. when A is ##STR7## and c) A is ##STR8## when Y is --S-- or --SO.sub.2 -- and X is --CH.dbd., and their pharmaceutically acceptable salts are Class III antiarrhythmic agents.Type: GrantFiled: October 7, 1992Date of Patent: October 19, 1993Assignee: American Home Products CorporationInventors: John A. Butera, Jehan F. Bagli, John W. Ellingboe
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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
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Patent number: 5164388Abstract: A renin inhibiting compound of the formula ##STR1## wherein X is N, O or CH; R.sub.1 is absent or a functional group; A and L are independently selected from absent, C.dbd.O, SO.sub.2 and CH.sub.2 ; D is C.dbd.O, SO.sub.2 or CH.sub.2 ; Y is N or CH; R.sub.2 is hydrogen, loweralkyl or substituted alkyl; Z is a functional group; R.sub.3 is loweralkyl or substituted alkyl; n is 0 or 1; and T is a mimic of the Leu-Val cleavage site of angiotensinogen; or a pharmaceutically acceptable salt, ester or prodrug thereof.Type: GrantFiled: April 18, 1991Date of Patent: November 17, 1992Assignee: Abbott LaboratoriesInventors: Biswanath De, Thomas N. Zydowsky, William R. Baker, Joseph F. Dellaria, Saul H. Rosenberg, Hwan S. Jae
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Patent number: 5153225Abstract: For treatment of disorders of the central nervous system, the cardiovascular system or the intestinal tract, the new substituted basic 2-aminotetralins of the formula ##STR1## in which R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen, alkyl or acyl, andR.sup.3 represents quinuclidine or a group of the formula --(CH.sub.2).sub.a --R.sup.4, --CH.sub.2 --CH.dbd.CH--(CH.sub.2).sub.b --R.sup.4, --CH.sub.2 --C.tbd.C--(CH.sub.2).sub.b --R.sup.4, ##STR2## wherein a denotes a number from 1 to 10,b denotes a number 0, 1, 2, 3 or 4,c denotes a number 0, 1 or 2,d denotes a number 2 or 3, andx denotes oxygen, sulphur or NR.sup.5,and their salts.Type: GrantFiled: April 9, 1991Date of Patent: October 6, 1992Assignee: Bayer AktiengesellschaftInventors: Rudolf Schohe, Thomas Glaser, Jorg Traber, George S. Allen
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Patent number: 5153198Abstract: A compound of the formula [II] or pharmaceutically acceptable salt thereof, ##STR1## wherein R.sup.1 is hydrogen or fluorine;R.sup.2 is hydrogen or fluorine;R.sup.3 is hydrogen, lower alkyl, lower alkoxy, halogen or lower alkylenedioxy;A is straight or branched lower alkylene having 1 to 6 carbon atoms; and n is 0 or 1,provided that at least one of R.sup.1 or R.sup.2 is fluorine. Such compound is useful for treatment of disorders of the cerebro-neural transmission system.Type: GrantFiled: October 23, 1991Date of Patent: October 6, 1992Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Takakazu Morita, Tadashi Iso, Hideyasu Yamauchi