Nitrogen Attached Directly Or Indirectly To The Hetero Ring By Acyclic Nonionic Bonding Patents (Class 549/467)
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Patent number: 5811582Abstract: Dimethyl-(3-aryl-but-3-enyl)-amine compounds, a method of preparing them, and the use of the compounds as pharmaceutical active ingredients are described.Type: GrantFiled: March 12, 1997Date of Patent: September 22, 1998Assignee: Gruenenthal GmbHInventors: Helmut Heinrich Buschmann, Wolfgang Werner Alfred Strassburger, Elmar Josef Friderichs, Babette-Yvonne Koegel
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Patent number: 5798382Abstract: Disclosed are a 2,3-dihydrobenzofuran derivative represented by formula (1) or a salt thereof, a method for producing the same, and use thereof: ##STR1## wherein R.sup.1 represents a hydrogen atom or a lower alkyl group; R.sup.2 represents a naphthyl group, a pyridyl group, a furyl group or a thienyl group; n is an integer of from 2 to 6; A represents a carbonyl group or a sulfonyl group; and * represents an asymmetric carbon atom. The 2,3-dihydrobenzofuran derivatives of the present invention and the non-toxic salts thereof have a strong affinity for serotonin 1A receptors. Therefore, are useful as pharmaceutical composition containing the 2,3-dihydrobenzofuran derivatives and the non-toxic salts thereof are especially useful for treating a serotonergic neuron-related disease, such as anxiety, depression, eating disorder, high blood pressure, emesis (including emesis induced by motion sickness, space sickness, dizziness and drug, etc.) and the like.Type: GrantFiled: December 12, 1996Date of Patent: August 25, 1998Assignee: Asahi Kasei Kogyo Kabushiki KaishaInventors: Yuji Kogami, Naomi Aono, Daisuke Mochizuki
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Patent number: 5792763Abstract: This invention provides novel 5-HT.sub.1F agonists of formula ##STR1## where X, Y, Z,and R are defined in the specification, which are useful for the prevention and treatment of migraine and associated disorders.Type: GrantFiled: September 26, 1997Date of Patent: August 11, 1998Assignee: Eli Lilly and CompanyInventors: James E. Fritz, Stephen W. Kaldor, Sidney Xi Liang, Upinder Singh, Yao-Chang Xu
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Patent number: 5792791Abstract: Disclosed are a 2,3-dihydrobenzofuran derivative represented by formula (1) or a salt thereof, a method for producing the same, and use thereof: ##STR1## wherein R.sup.1 represents a hydrogen atom or a lower alkyl group; n is an integer of from 2 to 6; A represents a carbonyl group or a sulfonyl group; R.sup.2 represents a hydrogen atom, a halogen atom, a lower alkyl group (which is unsubstituted or substituted with at least one halogen atom), a lower alkoxy group, a hydroxyl group, a nitro group or a cyano group; and * represents an asymmetric carbon atom.A 2,3-dihydrobenzofuran derivative of the present invention or a salt thereof has a strong affinity for a serotonin 1A receptor, and, therefore, is useful for prevention and treatment of serotonergic neuron-related diseases, such as anxiety, depression, high blood pressure, emeses (including emeses induced by motion sickness, space sickness and dizziness, etc.) and the like.Type: GrantFiled: June 28, 1996Date of Patent: August 11, 1998Assignee: Asahi Kasei Kogyo Kabushiki KaishaInventors: Yuji Kogami, Daisuke Mochizuki
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Patent number: 5780629Abstract: The invention relates to chiral compounds containing at least one divalent or polyvalent chiral group, at least one polymerizable group, at least one spacer and at least one mesogenic group, and to their use as polymerizable, chiral dopes for the preparation of cholesteric networks. The novel compounds are suitable for use in electro-optical displays or as chiral dopes for nematic or cholesteric liquid crystals in order to produce layers which reflect in colors.Type: GrantFiled: June 6, 1996Date of Patent: July 14, 1998Assignee: BASF AktiengesellschaftInventors: Karl-Heinz Etzbach, Paul Delavier, Karl Siemensmeyer, Gerhard Wagenblast, Lothar Laupichler, Volkmar Vill
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Patent number: 5773463Abstract: This invention describes the use of aminoindane and amino-tetrahydronaphthalene derivatives of general formula (I) ##STR1## in which Ar, X, R.sub.1, R.sub.2 and n are defined in claim 1, for the manufacture of a medicament for the treatment of disorders in which a calcium channel antagonist is indicated. Novel compounds falling within formula (I) are also claimed.Type: GrantFiled: January 22, 1996Date of Patent: June 30, 1998Assignee: SmithKline Beecham p.l.c.Inventors: John David Harling, Barry Sidney Orlek
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Patent number: 5773467Abstract: Benzofuran carboxides and sulphonamides have therapeutic utility, e.g. in the treatment of inflammation and asthma, by virtue of their ability to inhibit phosphodiesterases and tumor necrosis factor.Type: GrantFiled: December 5, 1996Date of Patent: June 30, 1998Assignee: Chiroscience, Ltd.Inventors: Hazel Joan Dyke, Hannah Jayne Kendall, Christopher Lowe, John Gary Montana
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Patent number: 5760071Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which A, R.sub.1, R'.sub.1, R.sub.2, R.sub.3 and n are as defined in the description, and medicinal product containing the same useful for treating a mammal afflicted with a disorder of the melatoninergic system.Type: GrantFiled: March 10, 1997Date of Patent: June 2, 1998Assignee: Adir et CompagnieInventors: Daniel Lesieur, Veronique Leclerc, Patrick Depreux, Philippe Delagrange, Pierre Renard
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Patent number: 5756769Abstract: A method for producing a propargylamine compound represented by the general formula (I): ##STR1## which comprises reacting a propargyl compound represented by the general formula (II): ##STR2## with an aromatic aldehyde represented by the general formula (III):ArCHO (III)and ammonia to obtain an imine compound represented by the general formula (IV): ##STR3## and hydrolyzing the resultant imine compound. It is to provide a method for producing a propargylamine compound from a propargyl compound by a simple operation without using a special facility, using ammonia as a reaction reagent, without producing a dipropatygylamine compound and a tripropargylamine compound as by-products.Type: GrantFiled: May 30, 1997Date of Patent: May 26, 1998Assignee: Sumitomo Chemical Company, Ltd.Inventors: Shinzo Seko, Akihiko Nakamura, Motoo Hazama
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Patent number: 5750564Abstract: Compounds having anti-inflammatory and anti-oxidant activity are disclosed. The compounds are useful in preventing and treating inflammatory disorders through several mechanisms. Methods of treatment employing these properties of the compounds and corresponding pharmaceutical compositions are disclosed.Type: GrantFiled: September 12, 1995Date of Patent: May 12, 1998Inventors: Mark Hellberg, Pete Delgado, Jon C. Nixon
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Patent number: 5747508Abstract: This patent application describes new amidinohydrazones of ketones derived from benzo?b!furan having the general formula I ##STR1## and their pharmaceutically acceptable salts, a method for their production, and pharmaceuticals containing these compounds.The compounds described show improved effects of class III antiarrhythmic agents.Type: GrantFiled: December 6, 1996Date of Patent: May 5, 1998Assignee: Helopharm G. Petrik GmbHInventors: Peter Richter, Martin Elsner, Barbara Vogt
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Patent number: 5744481Abstract: .alpha.- and .beta.-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: April 25, 1997Date of Patent: April 28, 1998Assignee: G.D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Patent number: 5731352Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which A, R.sub.1, R'.sub.1, R.sub.2, R.sub.3 and n are as defined in the description, and medicinal product containing the same useful for treating a mammal afflicted with a disorder of the melatoninergic system.Type: GrantFiled: May 30, 1996Date of Patent: March 24, 1998Assignee: Adir Et CompagnieInventors: Daniel Lesieur, Veronique Leclerc, Patrick Depreux, Philippe Delagrange, Pierre Renard
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Patent number: 5721233Abstract: Derivatives of 2,3-dihydro-5-benzofuranol, intermediates thereof, and processes useful for their preparation. These compounds are free radical scavengers and are useful in the treatment of conditions capable of being treated by free radical scavengers, such as stroke, nervous system trauma and reperfusion damage.Type: GrantFiled: December 22, 1994Date of Patent: February 24, 1998Assignee: Merrell Pharmaceuticals Inc.Inventors: J. Martin Grisar, Margaret A. Petty, Frank Bolkenius
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Patent number: 5721276Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which A, B, X and R.sub.1 are as defined in the description, and medicinal product containing the same useful for treating a disorder of the melatoninergic system.Type: GrantFiled: May 30, 1996Date of Patent: February 24, 1998Assignee: Adir et CompagnieInventors: Isabelle Lesieur, Patrick Depreux, Veronique Leclerc, Philippe Delagrange, Pierre Renard, Beatrice Guardiola Lemaitre
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Patent number: 5718845Abstract: Nonlinear optical compounds which contain a heteroaromatic ring and may further comprise a tricyanovinyl group attached to the heteroaromatic ring.Type: GrantFiled: January 18, 1995Date of Patent: February 17, 1998Assignee: Enichem S.p.A.Inventors: Kevin J. Drost, Pushkara Rao Varanasi, Kwan-Yue Alex Jen, Michael Anthony Drzewinski
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Patent number: 5719287Abstract: The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of their use.Type: GrantFiled: May 24, 1995Date of Patent: February 17, 1998Assignee: Eli Lilly and CompanyInventors: Stephen W. Kaldor, Marlys Hammond
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Patent number: 5708020Abstract: A compound which is selected from those of formula (I) : ##STR1## in which A, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are as defined in the description,its optical isomers,and its addition salts thereof with a pharmaceutically-acceptable acid or base,and medicinal products containing the same which are useful for treating a disorder of the melatoninergic system.Type: GrantFiled: March 11, 1996Date of Patent: January 13, 1998Assignee: Adir Et CompagnieInventors: Michel Langlois, Pierre Renard, Gerard Adam
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Patent number: 5705507Abstract: This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 3-benzyl-benzofurans which are .alpha.-substituted with ether, thioether, amino, hydrazino, cyano or halo that are useful for the treatment of the various medical indications associated with post-menopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus and cervix. The present invention further relates to intermediate compounds and processes useful for preparing the pharmaceutically active compounds of the present invention, and pharmaceutical compositions.Type: GrantFiled: September 29, 1995Date of Patent: January 6, 1998Assignee: Eli Lilly and CompanyInventor: Brian S. Muehl
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Patent number: 5705500Abstract: Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: June 7, 1995Date of Patent: January 6, 1998Assignee: G.D. Searle & Co.Inventors: Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, Joseph J. McDonald
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Patent number: 5703121Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which: R.sub.1, R.sub.2, R.sub.3 and A are as defined in the description,and Medicinal product containing the same useful for treating a disorder of the melatoninergic system.Type: GrantFiled: January 11, 1996Date of Patent: December 30, 1997Assignee: Adir Et CompagnieInventors: Daniel Lesieur, Eric Fourmaintraux, Patrick Depreux, Philippe Delagrange, Pierre Renard, Beatrice Guardiola-Lemaitre
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Patent number: 5698696Abstract: This invention relates to a novel process for preparing 2,3-dihydro-benzofuranol derivatives and to the novel intermediates produced thereby.Type: GrantFiled: March 7, 1996Date of Patent: December 16, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Gilbert Marciniak, Richard A. Schnettler, Timothy A. Ayers, Damian J. Krysan
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Patent number: 5698569Abstract: Urea-containing hydroxyethylamine peptide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: June 7, 1995Date of Patent: December 16, 1997Assignee: G. D. Searle & Co.Inventors: John J. Talley, Daniel P. Getman, John N. Freskos, Ko-Chung Lin, Robert M. Heintz, Donald J. Rogier, Jr., Deborah E. Bertenshaw
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Patent number: 5693831Abstract: The novel compound (2,3-dihydro-5-benzofuranyl)-acetonitrile is prepared by chloromethylating 2,3-dihydro-benzofuran and reacting the resulting 2,3-dihydro-5-chloromethyl-benzofuran with a cyanide. (2,3-Dihydro-5-benzofuranyl)-acetonitrile can be converted by saponification to (2,3-dihydro-5-benzofuranyl)-acetic acid, an important intermediate for the manufacture of various pharmaceutical active substances. This intermediate has hitherto been obtainable only by a laborious procedure and in low yields.Type: GrantFiled: February 27, 1997Date of Patent: December 2, 1997Assignee: Bayer AktiengesellschaftInventors: Nikolaus Muller, Guido Steffan
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Patent number: 5684033Abstract: This invention provides a novel series of non-peptidyl compounds which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This invention also provides methods for the treatment of such physiological disorders as well as pharmaceutical formulations which employ these novel compounds.Type: GrantFiled: June 5, 1995Date of Patent: November 4, 1997Assignee: Eli Lilly and CompanyInventors: Sung Y. Cho, Thomas A. Crowell, Bruce D. Gitter, Philip A. Hipskind, J. Jeffry Howbert, Joseph H. Krushinski, Jr., Karen L. Lobb, Brian S. Muehl, James A. Nixon
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1,2-ethanediol derivative and salt thereof and cerebral function-improving agent comprising the same
Patent number: 5658904Abstract: 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: June 6, 1995Date of Patent: August 19, 1997Assignee: Toyama Chemical Co., Ltd.Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita -
Patent number: 5646313Abstract: New amino acid derivatives, processes for their preparation, and their therapeutic application are described.These amino acid derivatives correspond to the general formulae ##STR1## These derivatives may be used as medicaments which exhibit an enkephalinase-inhibitory activity.Type: GrantFiled: June 5, 1995Date of Patent: July 8, 1997Assignee: Societe Civile BioprojetInventors: Denis Danvy, Thierry Monteil, Christophe Lusson, Jean-Charles Schwartz, Claude Gros, Nadine Noel, Jeanne-Marie LeComte, Pierre Duhamel, Lucette Duhamel
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Patent number: 5643958Abstract: The present invention relates to a compound of the formula (I): ##STR1## wherein Ar.sup.1, Ar.sup.2 and Ar.sup.3 represent an aryl group or a heteroaromatic ring group; A represents a hydrocarbon group which may be substituted; Q represents a group of the formula --(CH.sub.2).sub.m -- (m is an integer of from 1 to 6) or --(CH.sub.2).sub.n --W--(CH.sub.2).sub.p -- (W is an oxygen atom, a sulfur atom, a vinylene group or an ethynylene group; n and p are a integer of from 0 to 3); R.sup.1 represents a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group, a lower alkoxy group, an aryl or heteroaromatic ring group which may be substituted; R.sup.2, R.sup.7 and R.sup.8 represent a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a lower alkoxy group; R.sup.3 and R.sup.Type: GrantFiled: March 15, 1996Date of Patent: July 1, 1997Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Yoshikazu Iwasawa, Tetsuya Aoyama, Kumiko Kawakami, Sachie Arai, Toshihiko Satoh, Yoshiaki Monden
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Patent number: 5635527Abstract: A novel carboxylic acid compound having a condensed ring, which is represented by the formula (I) ##STR1## wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a pharmaceutical composition thereof and pharmaceutical use thereof. The novel carboxylic acid compound having a condensed ring and pharmacologically acceptable salt thereof of the present invention have superior GPIIb/IIIa antagonism in mammals inclusive of human; can be administered orally; have long life in blood and low toxicity; and show less side-effects. Accordingly, they are extremely useful for the prophylaxis and treatment of thrombotic diseases and other diseases.Type: GrantFiled: February 6, 1996Date of Patent: June 3, 1997Assignee: The Green Cross CorporationInventors: Shinichiro Ono, Tomohiro Yoshida, Atsuyuki Ashimori, Keigo Kosaka, Takehiro Okada, Kazuhiro Maeda, Masahiro Eda, Fumio Mori, Yoshihisa Inoue, Hajime Ebisu, Teruaki Imada, Ruriko Ikegawa, Feng Wang, Norifumi Nakamura
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Patent number: 5631253Abstract: Compounds having the formula (I): ##STR1## and stereoisomers thereof, wherein A is hydrogen, halo, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl, phenoxy, nitro or cyano; R.sup.1 and R.sup.2, which may be the same or different, are hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocyclylalkyl, optionally substituted cycloalkylalkyl, optionally substituted aralkyl, optionally substituted heteroarylalkyl, optionally substituted aryloxyalkyl, optionally substituted heteroaryloxyalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkoxy, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aryloxy, optionally substituted heteroaryloxy, nitro, halo, cyano, --NR.sup.3 R.sup.4, --CO.sub.2 R.sup.3, --CONR.sup.3 R.sup.4, --COR.sup.3, --S(O).sub.n R.sup.3 wherein n is 0, 1 or 2, (CH.sub.2).sub.m PO(OR.Type: GrantFiled: December 2, 1994Date of Patent: May 20, 1997Assignee: Zeneca LimitedInventors: Paul J. de Fraine, Anne Martin
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Patent number: 5631208Abstract: The present invention relates to novel cyclohexane-1,3-dione derivatives of formula (I) useful as herbicides and plant-growth regulants. ##STR1## wherein, X is selected from the group consisting of hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkoxy, halogen, C.sub.1 -C.sub.6 haloalkyl, nitro, cyano, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylsulfinyl, C.sub.1 -C.sub.6 alkylsulfonyl, sulfamoyl, N-(C.sub.1 -C.sub.6 alkyl) sulfamoyl and N,N-di(C.sub.1 -C.sub.6 alkyl) sulfamoyl group;(X)n represents number of X substituents which may be the same or different on benzene ring, where n is 1, 2 or 3.Also, cyclohexyl moiety, one of the substituents on benzofuran ring, is substituted at 4, 5, 6 or 7 position. The (X)n can't be filled only with hydrogens and the (X)n can substitute position where cyclohexyl moiety is not substituted;R.sup.1 is selected from hydrogen and C.sub.1 -C.sub.4 alkyl group;R.sup.2 is selected from C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl and C.sub.2 -C.sub.Type: GrantFiled: April 24, 1995Date of Patent: May 20, 1997Assignee: Korea Research Institute of Chemical TechnologyInventors: Eung K. Ryu, Kyoung M. Kim, Hyoung R. Kim, Jong H. Song, Jae N. Kim, Jin S. Kim
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Patent number: 5625083Abstract: The present invention relates to novel dinitroglycerol esters of fatty acids, hydroxy fatty acids and prostaglandins, and methods for producing them. Dinitroglycerol esters provided by this invention have an improved biological specificity and/or a greater specific activity than the parent compound. The novel prostanoids produced herein may be used as vasodilators, antihypertensive cardiovascular agents, bronchodilators, and they may have uses in obstetrics and gynecology. The dinitroglycerol esters of fatty acids and hydroxy fatty acids may be useful as platelet antiaggregating agents.Type: GrantFiled: June 2, 1995Date of Patent: April 29, 1997Inventors: Vladimir V. Bezuglov, Igor V. Serkov
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Patent number: 5622974Abstract: This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 3-benzyl-benzofurans which are .alpha.-substituted with ether, thioether amino, cyano or halo that are useful for the treatment of the various medical indications associated with post-menopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus and cervix. The present invention further relates to intermediate compounds and processes useful for preparing the pharmaceutically active compounds of the present invention, and pharmaceutical compositions.Type: GrantFiled: March 10, 1995Date of Patent: April 22, 1997Assignee: Eli Lilly and CompanyInventor: Brian S. Muehl
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Patent number: 5620998Abstract: The invention relates to N-acyl-N-heterocyclylalkylamino acids of the formula ##STR1## wherein Y.sub.1 is O, S or N(R) and R is hydrogen or C.sub.1 -C.sub.7 alkyl;X.sub.1 is --CO-- or --S(O).sub.m -- and the index m is 0, 1 or 2;one of the variables X.sub.2 and X.sub.4 is C.sub.1 -C.sub.4 alkylene and the other of the variables X.sub.2 and X.sub.4 is a bond; or each of the variables X.sub.2 and X.sub.4 is a bond;X.sub.3 is C.sub.3 -C.sub.7 cycloalkylidene or the structural element --C(X.sub.a)(X.sub.b)-- and X.sub.a is hydrogen or C.sub.1 -C.sub.7 alkyl and X.sub.b is C.sub.1 -C.sub.7 alkyl;and the rings A, B and C, with the exception of the substituents indicated in the formula, and also aromatic substituents are, independently of one another, unsubstituted or mono- or poly-substituted by substituents selected from the group consisting of halogen, C.sub.1 -C.sub.7 alkyl, C.sub.1 -C.sub.7 alkoxy, C.sub.2 -C.sub.7 alkenyloxy, phenoxy, benzyloxy, trifluoromethyl and S(O).sub.Type: GrantFiled: June 7, 1995Date of Patent: April 15, 1997Assignee: Ciba-Geigy CorporationInventors: Tibur Schmidlin, Paul Zbinden, Peter B uhlmayer
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Patent number: 5616738Abstract: N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal motility stimulating properties, compositions containing these compounds as active ingredient and methods of treating warm-blooded animals suffering from the decreased peristalsis of the gastrointestinal system.Type: GrantFiled: March 31, 1995Date of Patent: April 1, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Georges H. P. Van Daele, Frans M. A. Van den Keybus
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Patent number: 5616718Abstract: A compound having the formula: ##STR1## wherein W, X, Y, and Z are as defined in the specification is useful for making 2,4-diaminoquinazolines.Type: GrantFiled: April 20, 1995Date of Patent: April 1, 1997Assignee: FMC CorporationInventors: Robert N. Henrie, II, Clinton J. Peake, Thomas G. Cullen, Walter H. Yeager, John W. Buser, James J. Fiordeliso, John A. Dixson
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Patent number: 5612368Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which Ar, X, R.sub.1 and R.sub.2 are as defined in the description and a medicinal product containing the same in order to treat a disorder of the melatoninergic system.Type: GrantFiled: October 25, 1995Date of Patent: March 18, 1997Assignee: Adir et CompagnieInventors: Jean Andrieux, Michel Langlois, Pierre Renard, Philippe Delagrange
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Patent number: 5612371Abstract: New amino acid derivatives, processes for their preparation and their therapeutic application.Amino acid derivatives corresponding to the general formulae ##STR1## These derivatives may be used as medicaments which exhibit an enkephalinase-inhibitory activity.Type: GrantFiled: July 18, 1994Date of Patent: March 18, 1997Assignee: Societe Civile BioprojectInventors: Denis Danvy, Thierry Monteil, Christophe Lusson, Jean-Charles Schwartz, Claude Gros, Nadine Noel, Jeanne-Marie Lecomte, Pierre Duhamel, Lucette Duhamel
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Patent number: 5604256Abstract: Compounds of formula (I): ##STR1## (in which: R is hydrogen, methyl or hydroxy; X is alkyl, alkenyl, cycloalkyl, aryl, aralkyl, or a heterocyclic group; A is a single bond, or an alkylene, alkenylene, alkynylene or alkadienylene group; Y is hydrogen, aryl, cycloalkyl or a heterocyclic group) have the ability to inhibit the biosynthesis of cholesterol, and can thus be used for the treatment and prophylaxis of diseases relating to high blood cholesterol levels.Type: GrantFiled: December 14, 1994Date of Patent: February 18, 1997Assignee: Sankyo Company, LimitedInventors: Hiroshi Kogen, Masaaki Kurabayashi, Teiichiro Koga, Toru Komai, Haruo Iwabuchi
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Patent number: 5594028Abstract: This invention provides certain sulfonamide derivatives, their pharmaceutical formulations, and their use in the treatment of susceptible neoplasms in mammals.Type: GrantFiled: November 21, 1994Date of Patent: January 14, 1997Assignee: Eli Lilly and CompanyInventors: Richard W. Harper, J. Jeffry Howbert, Gerald A. Poore, Brent J. Rieder, Eddie V. P. Tao, James A. Aikins
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Patent number: 5576332Abstract: New soft .beta.-adrenergic blocking agents, useful in the treatment or prevention of cardiovascular disorders and in the treatment of glaucoma, have the formula ##STR1## wherein n is an integer from 0 to 10; R is C.sub.6 -C.sub.12 cycloalkyl-C.sub.p H.sub.2p --, C.sub.6 -C.sub.18 polycycloalkyl-C.sub.p H.sub.2p --, C.sub.6 -C.sub.18 polycycloalkenyl-C.sub.p H.sub.2p -- or C.sub.6 -C.sub.12 cycloalkenyl-C.sub.p H.sub.2p -- (wherein p is 0, 1, 2 or 3), or together with the adjacent ##STR2## group represents a variety of other complex ester groupings; R.sub.1 is C.sub.1 -C.sub.7 alkyl; and Ar is a divalent radical containing at least one aromatic nucleus. The corresponding pharmaceutically acceptable acid addition salts are also described.Type: GrantFiled: May 31, 1995Date of Patent: November 19, 1996Inventor: Nicholas S. Bodor
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Patent number: 5569669Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which R.sub.1, R.sub.2, R.sub.2', R.sub.2", R.sub.2'", R.sub.3 and n are as defined in the description, an optical isomer, and an addition salt thereof with a pharmaceutically-acceptable acid or base,and medicinal product containing the same useful for treating a mammal afflicted with a disorder associated to 5-HT.sub.1A or 5-HT.sub.2C receptors.Type: GrantFiled: March 10, 1995Date of Patent: October 29, 1996Assignee: Adir et CompagnieInventors: G erald Guillaumet, Marie-Claude Viaud, Pierre Renard, G erard Adam, Daniel-Henri Caignard, B eatrice Guardiola-Lemaitre, Marie-Claire Rettori
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Patent number: 5567828Abstract: The present invention provides compounds with nitrogen-containing non-basic side chains of formula II ##STR1## wherein R.sup.1 and R.sup.2, independently, are H, OH, O(C.sub.1 -C.sub.6 alkyl), O--C(O)--(C.sub.1 -C.sub.6 alkyl), O--C(O)--O(C.sub.1 -C.sub.6 alkyl), O--C(O)--Ar, O--C(O)--O--Ar, O--SO.sub.2 --(C.sub.4 -C.sub.6 alkyl), chloro, fluoro, or bromo;W is CHOH, C(O), or CH.sub.2 ;Y is (CH.sub.2).sub.n, or CH(C.sub.1 -C.sub.4 alkyl);V is S, 0, or CH.sub.2 CH.sub.2 ;n is 1, 2, or 3; andAr is optionally substituted phenyl.The present invention also provides pharmaceutical compositions containing compounds of formula II, optionally containing estrogen or progestin, and the use of such compounds, alone, or in combination with estrogen or progestin, for alleviating the symptoms of post-menopausal symptoms, particularly osteoporosis, cardiovascular related pathological conditions, and estrogen-dependent cancer.Type: GrantFiled: June 7, 1995Date of Patent: October 22, 1996Assignee: Eli Lilly and CompanyInventor: Jeffrey A. Dodge
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Patent number: 5554633Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q is optionally substituted phenyl or benzhydryl; X and Y are each H or together form a group=O; Z is O, S or NR.sup.9, where R.sup.9 is H or C.sub.1-6 alkyl; R.sup.1 represents H or C.sub.1-6 alkyl; R.sup.2 represents C.sub.1-6 alkyl substituted by CONR.sup.7 (CH.sub.2).sub.p R.sup.8 (where R.sup.7 is H or C.sub.1-6 alkyl, R.sup.8 is optionally substituted heteroaryl and p is 0, 1, 2, 3, 4, 5 or 6); R.sup.3 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkynyl; R.sup.4 represents H, C.sub.1-6 alkyl or optionally substitute phenyl; R.sup.5 represents optionally substituted phenyl; R.sup.6 is H or C.sub.1-6 alkyl; and q is 0, 1, 2 or 3; are tachykinin antagonists useful in therapy.Type: GrantFiled: January 27, 1995Date of Patent: September 10, 1996Assignee: Merck, Sharp & Dohme, Ltd.Inventor: Martin R. Teall
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Patent number: 5504213Abstract: The Benzofuranyl- and -thiophenyl-alkane-carboxylic acid derivatives are prepared Tby cyclisation of hydroxy acetophenones and related compounds or by Wittig-reaction of benzofuranyl aldehydes. The compounds can be used to prepared medicaments.Type: GrantFiled: April 29, 1994Date of Patent: April 2, 1996Assignee: Bayer AktiengesellschaftInventors: Rudiger Fischer, Gabriele Braunlich, Klaus-Helmut Mohrs, Rudolf Hanko, John-Edward Butler-Ransohoff, Mazen Es-Sayed, Graham Sturton, Steve Tudhope, Trevor Abram, Wendy J. McDonald-Gibson
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Patent number: 5496853Abstract: Pharmaceutical compositions containing a benzoxazole compound and a 2,3-dihydrobenzofuran compound represented by the following formula (I) and its pharmaceutically acceptable salt: ##STR1## In the formula, any one of P, Q, R and S is a group represented by the formula: ##STR2## and R.sub.1, R.sub.2 and the reining three substituents out of the substituents P to S each independently stand for various substituents. These compositions are used as an ATCAT inhibitor or for treating hyperlipidemia and atherosclerosis.Type: GrantFiled: April 26, 1995Date of Patent: March 5, 1996Assignee: Teijin LimitedInventors: Tatsuki Shiota, Takumi Takeyasu, Kenichiro Kataoka, Tsutomu Mochizuki, Hirofumi Tanabe, Mikio Ota, Masatoshi Kano, Hisao Yamaguchi
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Patent number: 5492929Abstract: Novel compound represented by the formula: ##STR1## wherein ring A, ring B and ring C each stands for an optionally substituted benzene ring; X stands for --NR-- wherein R stands for hydrogen atom or an optionally substituted hydrocarbon group, --O-- or --S--; Y stands for --(CH.sub.2)n-- wherein n denotes 1 or 2 or --NH--; and R.sup.a stands for a hydrogen atom or an optionally substituted hydrocarbon group, provided that when ring C is unsubstituted or substituted only at para-position, ring B is substituted at least at ortho-position or a salt thereof which have an excellent acyl-CoA: cholesterol acyltransferase inhibiting action and cholesterol-lowering activity, their production and medicinal use.Type: GrantFiled: December 14, 1993Date of Patent: February 20, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideaki Natsugari, Yasuo Sugiyama, Yoshinori Ikeura
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Patent number: 5491152Abstract: The present invention provides compounds of Formula I, ##STR1## or a pharmaceutically acceptable salt forms thereof, which are inhibitors of acyl-Coenzyme A: cholesterol O-acyltransferase (ACAT), pharmaceutical compositions containing such compounds, processes for the preparation of such compounds, and the use of such compounds as antihypercholesterolemic and/or antiatherosclerotic agents.Type: GrantFiled: March 23, 1994Date of Patent: February 13, 1996Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Richard G. Wilde, Soo S. Ko, Jeffrey T. Billheimer
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Patent number: 5482966Abstract: The invention concerns oxime derivatives of the formula I ##STR1## wherein R.sup.4 includes hydrogen, carboxy, carbamoyl, amino, cyano, trifluoromethyl, (1-4C)alkylamino, di-(1-4C)alkylamino and (1-4C)alkyl;R.sup.5 includes hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, (2-5C)alkanoyl, halogeno-(2-4C)alkyl and hydroxy-(2-4C)alkyl;Ar.sup.1 is phenylene or a heteroaryl diradical;A.sup.1 is a direct link to X.sup.1, or A.sup.1 is (1-4C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is phenylene or a heteroaryl diradical;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which together with the carbon atom to which A.sup.2 and A.sup.3 are attached define a ring having 5 or 6 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.Type: GrantFiled: June 13, 1994Date of Patent: January 9, 1996Assignees: Zeneca Limited, Zeneca Pharma S.A.Inventors: Thomas G. C. Bird, Patrick Ple
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Patent number: 5481021Abstract: This invention relates to phenyl amidine derivatives having the following formula ##STR1## or a pharmaceutically acceptable salt which are useful in the inhibition of platelet aggregation. This invention also relates to pharmaceutical compositions of such phenyl amidine derivatives.Type: GrantFiled: December 22, 1994Date of Patent: January 2, 1996Assignee: G. D. Searle & Co.Inventors: Robert B. Garland, Masateru Miyano, Jeffery A. Zablocki, Lori A. Schretzman