Z Radical Contains Two Or More Nitrogen Atoms At Least One Of Which Forms A C(=x)n Group (x Is Chalcogen) Patents (Class 514/542)
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Patent number: 5614539Abstract: Novel urea derivatives are provided which inhibit platelet aggregation. This invention also pertains to pharmaceutical compositions and methods of using such derivatives.Type: GrantFiled: June 1, 1995Date of Patent: March 25, 1997Assignee: G. D. Searle & Co.Inventors: Steven P. Adams, Foe S. Tjoeng, Mark E. Zupec
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Patent number: 5612373Abstract: The invention concerns acid derivatives of formula IR.sup.1 --CON(R.sup.2)--N(R.sup.3)CO--X.sup.1 --Q--X.sup.2 --GIand pharmaceutically acceptable metabolically labile esters or amides thereof, and pharmaceutically acceptable salts thereof, in which R.sup.1, R.sup.2, R.sup.3, X.sup.1, Q, X.sup.2 and G have the meanings given in the specification. The invention also concerns processes for the preparation of the acid derivatives of formula I, pharmaceutical compositions containing them and their use as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa.Type: GrantFiled: June 27, 1994Date of Patent: March 18, 1997Assignee: Zeneca LimitedInventors: Andrew G. Brewster, Peter W. R. Caulkett, Alan W. Faull, Robert J. Pearce, Richard E. Shute
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Patent number: 5602277Abstract: A compound of the Formula (I): ##STR1## or pharmaceutically-suitable salts or prodrug forms thereof, wherein: n is 0-1;m is 0;p is 0-1;R.sup.1 is --CO.sub.2 H;R.sup.2 is selected from the group consisting of H, --OH, and --NH.sub.2 ;R.sup.3 is H;R.sup.4 is --C(O)NHR.sup.8 ;R.sup.5 is --NHC(R.sup.6)NH.sub.2R.sup.6 is selected from the group consisting of .dbd.NH, .dbd.NOH, .dbd.NCN, .dbd.O, and .dbd.S; andR.sup.8 is selected from the group consisting of C.sub.1 -C.sub.4 linear or branched alkyl substituted with 0-3 halogens on each carbon.Type: GrantFiled: March 30, 1995Date of Patent: February 11, 1997Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, Pooran Chand, David A. Walsh
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Patent number: 5602175Abstract: Hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: May 25, 1995Date of Patent: February 11, 1997Assignee: G.D. Searle & Co.Inventors: John J. Talley, Kathryn L. Reed
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Patent number: 5574064Abstract: The present invention provides an agricultural or horticultural fungicide including an effective amount of an amino-acid derivative represented by the formula: ##STR1## wherein R.sup.1 represents a lower alkyl group (optionally having at least one same or different substituent of a halogen atom, an alkoxy group, and a cyano group), R.sup.2 represents an ethyl group, or an n-propyl group, R.sup.3 represents a hydrogen atom or a lower alkyl group, R.sup.4 represents a hydrogen atom, R.sup.5, R.sup.6, and R.sup.7 independently represent a hydrogen atom or a lower alkyl group, R.sup.8 represents a hydrogen atom, or a lower alkyl group, Z.sup.1 and Z.sup.2 independently represent an oxygen atom or a sulfur atom, Z.sup.3 represents an oxygen atom, or a sulfur atom, Q represents a phenyl group, m represents an integer from 0 to 2, and n represents 0 or 1.Type: GrantFiled: December 28, 1994Date of Patent: November 12, 1996Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Masaru Shibata, Kazuhiko Sugiyama, Norihisa Yonekura, Junetsu Sakai, Yoshiyuki Kojima, Shigeru Hayashi
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Patent number: 5565430Abstract: Disclosed are compounds, compositions and methods for inhibiting interleukinprotease activity. The compounds, .alpha.-substituted acetamides a ##STR1## wherein: R.sub.2 =H or alkyl;R.sup.3 =halo, O(CO).sub.0-1 aryl, OPOR.sup.4 R.sup.5 ; ##STR2## where R.sup.4 and R.sup.5 =aryl;R.sup.6 =H, aryl or aralkyl;R.sup.7 =independently selected from R.sup.6, CF.sub.3 and CF.sub.2 CF.sub.3 ;R.sup.1 =R.sup.6 -CO, heteroaryl-CO, heteroaralkyl-CO and amino acid.Type: GrantFiled: August 2, 1994Date of Patent: October 15, 1996Assignee: Sterling Winthrop Inc.Inventors: Roland E. Dolle, Todd L. Graybill
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Patent number: 5561162Abstract: Fluorinated alkene compounds useful for and methods of controlling nematodes, insects, and acarids that prey on agricultural crops. Polar compounds, for example, 3,4,4-trifluoro-3-butene-1-amine or 3,4,4-trifluoro-3-butenoic acid, are particularly useful for systemic control of pests. Novel method and intermediates for the preparation of 3,4,4-trifluoro-3-butene-1-amine are also provided.Type: GrantFiled: March 8, 1995Date of Patent: October 1, 1996Assignee: Monsanto CompanyInventor: Peter G. Ruminski
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Patent number: 5545640Abstract: Disclosed herein are compounds which inhibit human immunodeficiency virus (HIV) protease activity and inhibit HIV replication in human cells. Thus, the compounds are indicated for the treatment of HIV infections. The compounds can be represented by the formula ##STR1## wherein X is a terminal group, for example, an aryloxycarbonyl, an alkanoyl or an arylalkyl carbamoyl; A is absent or an amino acid or a derived amino acid; either R.sup.1 or R.sup.2 is hydrogen while the other is alkyl or R.sup.1 and R.sup.2 are joined to form a cyclohexane; Q is hydrogen, hydroxy, halo or lower alkoxy; and Y is a terminal group, for example, an alkylamino, alkoxy or an optionally substituted anilino.Type: GrantFiled: April 4, 1995Date of Patent: August 13, 1996Assignee: Bio-Mega/Boehringer Ingeleheim Research Inc.Inventors: Pierre L. Beaulieu, Ingrid Guse
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Patent number: 5543425Abstract: This invention relates to a method of inhibiting platelet aggregation comprising administering compounds having the following formula ##STR1##Type: GrantFiled: October 28, 1994Date of Patent: August 6, 1996Assignee: G. D. Searle & Co.Inventors: Steven P. Adams, Richard J. Lindmark, Masateru Miyano, Joseph G. Rico
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Patent number: 5525629Abstract: Hydroxamic acid derivatives of formula (I): ##STR1## wherein R.sup.1 represents hydrogen or an (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxycarbonyl(C.sub.1 -C.sub.6)alkyl, phenyl, substituted phenyl, phenyl(C.sub.1 -C.sub.6)alkyl, heterocyclyl, (C.sub.1 -C.sub.6)alkylcarbonyl, phenacyl or substituted phenacyl group;R.sup.2 represents hydrogen or a (C.sub.1 -C.sub.6)alkyl, (C.sub.2 -C.sub.6)alkenyl, phenyl(C.sub.1 -C.sub.6)alkyl, cycloalkyl(C.sub.1 -C.sub.6)alkyl or cycloalkenyl(C.sub.1 -C.sub.6)alkyl group,R.sup.3 represents a group --CH.sub.2 CO.sub.2 (C.sub.1 -C.sub.4)alkyl or --CH.sub.2 CH.sub.2 CO.sub.2 (C.sub.1 -C.sub.4)alkyl;R.sup.4 represents hydrogen or a (C.sub.1 -C.sub.6)alkyl or phenyl(C.sub.1 -C.sub.6)alkyl group;R.sup.5 represents hydrogen or a methyl group;n is 0, 1 or 2;and A represents a (C.sub.1 -C.sub.6)hydrocarbon chain optionally substituted with one or more (C.sub.1 -C.sub.Type: GrantFiled: November 4, 1993Date of Patent: June 11, 1996Assignee: British Bio-Technology LimitedInventors: Michael J. Crimmin, William A. Galloway, Andrew J. Gearing
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Patent number: 5491169Abstract: Compounds having the properties of morphinic substances, particularly anasia, with beneficial effects on behaviour and with peripheral effects without their major drawbacks (tolerence, addiction), the blood-brain barrier and having the following formula :H.sub.2 N--CH(R.sub.1)--CH(R.sub.2)--S--S--CH(R.sub.3)--CH(R.sub.4)--A--B--Zwherein: AB preferably represents a CO amide bond, R.sub.2 et R.sub.3 preferably represent a hydrogen atom, R.sub.1 et R.sub.4 preferably represent, independently of each other, a benzyl grouping, --CH.sub.2 CH.sub.2 SCH.sub.3, --CH.sub.2 --CH.sub.2 --S(O)--CH.sub.3 or --CH.sub.2 --CH(CH.sub.3) .sub.2, Z may represent a --CH(R.sub.5)[CH(R.sub.6)].sub.n --COO(R.sub.7) grouping wherein: R.sub.5 may represent a hydrogen atom, a methyl grouping, a benzyl grouping or a phenyl grouping, R.sub.6 may represent a hydrogen atom and may also form a hydrocarbon cycle with R.sub.5, or Z may represent a heterocyclic grouping, and preferably a morpholinyl grouping. No drawings.Type: GrantFiled: September 26, 1994Date of Patent: February 13, 1996Assignee: Institut National de la Sante et de la Recherche Medicale (INSERM)Inventors: Bernard Roques, Marie C. Fournie-Zaluski
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Patent number: 5475013Abstract: Urea-containing hydroxyethylamine peptide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: May 20, 1992Date of Patent: December 12, 1995Assignee: Monsanto CompanyInventors: 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: 5472978Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q represents optionally substituted phenyl, naphthyl, indolyl, benzothiophenyl, benzofuranyl, benzyl or indazolyl; Z represents O, S or NR.sup.8 ; X and Y are H or are together .dbd.O; R.sup.1 and R.sup.2 are H; optionally substituted C.sub.1-6 alkyl; optionally substituted phenyl(C.sub.1-4 alkyl); COR.sup.c ; CO.sub.2 R.sup.c ; CONR.sup.c R.sup.d ; CONR.sup.c COOR.sup.d ; or SO.sub.2 R.sup.c ; R.sup.3 is H or C.sub.1-6 alkyl, R.sup.4 is H , C.sub.1-6 alkyl or optionally substituted phenyl; and R.sup.5 represents optionally substituted phenyl; are tachykinin antagonists. They and compositions thereof are useful in therapy.Type: GrantFiled: December 10, 1993Date of Patent: December 5, 1995Assignee: Merck Sharp & Dohme Ltd.Inventors: Raymond Baker, Angus M. MacLeod, Kevin J. Merchant, Christopher J. Swain
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Patent number: 5455274Abstract: The invention relates to the compounds of the formula ##STR1## wherein the C(=NOH)-NH.sub.2 group may be in tautomeric form, and pharmaceutically acceptable salts thereof, in which:R.sub.1 is amino or amino which is mono- or disubstituted by a substituent selected from an aliphatic hydrocarbon radical, an araliphatic hydrocarbon radical, an aromatic radical, and a cycloaliphatic hydrocarbon radical or is amino which is disubstituted by a divalent aliphatic hydrocarbon radical or a said radical interrupted by oxygen;R.sub.2 is hydrogen, halogen, trifluoromethyl, an aliphatic hydrocarbon radical or hydroxy; or R.sub.2 is hydroxy which is etherified by an aliphatic alcohol, araliphatic alcohol, or aromatic alcohol or which is esterified by an aliphatic or araliphatic carboxylic acid; or R.sub.2 is hydroxy which is etherified by an aliphatic alcohol which is substituted by carboxy, by esterified carboxy or by amidated carboxy;X.sub.1 and X.sub.Type: GrantFiled: December 9, 1992Date of Patent: October 3, 1995Assignee: Ciba-Geigy CorporationInventor: Hongsuk Suh
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Patent number: 5455273Abstract: The invention relates to N,N-disubstituted arylcycloalkylamines of general formula ##STR1## wherein n, m, A, X and R.sup.1 to R.sup.7 are defined as in claim 1, the isomers, isomer mixtures and salts thereof, which have valuable properties, particularly an inhibitory effect on cholesterol biosynthesis.Type: GrantFiled: November 19, 1993Date of Patent: October 3, 1995Assignee: Karl Thomae GmbHInventors: Roland Maier, Peter Muller, Eberhard Woitun, Rudolf Hurnaus, Michael Mark, Bernhard Eisele, Ralph-Michael Budzinski, Gerhard Hallermayer
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Patent number: 5453440Abstract: This invention relates to compounds having the following formula ##STR1## or pharmaceutically acceptable salt thereof which are useful in the inhibition of platelet aggregation, to pharmaceutical compositions of such phenylamidines derivatives, and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.Type: GrantFiled: October 15, 1993Date of Patent: September 26, 1995Assignee: G. D. Searle & Co.Inventors: Philippe R. Bovy, Robert B. Garland, Masateru Miyano, Joseph G. Rico, Thomas E. Rogers, Jeffery A. Zablocki
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Patent number: 5420165Abstract: There are provided substituted acid amide, arylhydrazone compounds (amidrazones) of formula I ##STR1## the use thereof for the control of insect and acarid pests and methods and compositions for the protection of crops from the damage and loss caused by said pests.Type: GrantFiled: December 29, 1992Date of Patent: May 30, 1995Assignee: American Cyanamid CompanyInventors: Joseph A. Furch, David G. Kuhn, David A. Hunt
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Patent number: 5411964Abstract: A phenylalanine-glycine compound of formula (I): ##STR1## wherein R represents a residue of an antitumor substance, or a salt or ester thereof, a process for preparation thereof, and a pharmaceutical composition containing the same are described. The novel conjugate of the phenylalanine-glycine compound and the antitumor substance exhibits superior antitumor activity in comparison with the case wherein an antitumor substance is administered alone or as a mixture with phenylalanine.Type: GrantFiled: March 15, 1993Date of Patent: May 2, 1995Assignee: Kureha Chemical Industry Co., Ltd.Inventors: Koichi Niimura, Takako Kawabe, Takao Ando, Kenichi Saito
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Patent number: 5387591Abstract: Compounds of formula (I): ##STR1## in which: R.sub.1 represents:optionally substituted alkyl,optionally substituted phenyl,pyridyl,optionally substituted phenylsulfonyl,acyl,optionally substituted benzoyl or pyridylcarbonyl,alkylaminocarbonyl or phenylaminocarbonyl,acylamino or benzoylamino,R2 represents:hydrogen,optionally substituted phenyl,optionally substituted 3-pyridyl or 2-pyridyl,R.sub.3 represents any one of the following groups: ##STR2## in which m is equal to 2, 3 or 4,n is equal to 4, 5, 6 or 7, and R represents hydrogen or alkyl.Type: GrantFiled: February 11, 1993Date of Patent: February 7, 1995Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Thierry Dubuffet, Olivier Muller, Michel Laubie, Tony Verbeuren
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Patent number: 5374656Abstract: This invention relates to compounds of formula: ##STR1## in which R.sub.1 represents a hydrogen atom or an alkyl or alkoxycarbonyl radical or an unsubstituted or substituted phenyl radical,R.sub.2 represents an alkyl (1-8 C) or polyfluoroalkyl radical or an unsubstituted or substituted cycloalkyl radical,R.sub.3 represents an unsubstituted or substituted phenyl radical, a naphthyl, indolyl, quinolyl or phenylamino radical in which the phenyl ring is optionally substituted, or a quinolylamino radical, andm is 0 or 1, the process for preparing them and the medicaments containing them.Type: GrantFiled: June 25, 1992Date of Patent: December 20, 1994Assignee: Rhone-Poulenc Rorer, S.A.Inventors: Jean-Dominique Bourzat, Marc Capet, Claude Cotrel, Claude Guyon, Franco Manfre, Gerard Roussel
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Patent number: 5356931Abstract: Alpha-Arylacrylic acid derivatives of the general formula I ##STR1## where X is ethylene or ethenylene; n is 0 or 1;m is 0, 1, 2, 3 or 4;R.sup.1 is cyano, cyanato, thiocyanato, nitro, hydroxyl, carboxyl, haloalkyl, haloalkoxy, unsubstituted or substituted cycloalkyl, cycloalkenyl, cycloalkadienyl, alkenyl, alkynyl or amino, alkylcarbonyl, alkoxycarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, unsubstituted or substituted benzyloxycarbonyl, benzoyl, phenylalkyl, phenylalkoxy or phenoxyalkyl,or R.sup.1 together with one of the radicals R.sup.2 forms an unsubstituted or substituted 1,3-butadiene-1,4-diyl group or an unsubstituted or substituted chain consisting of carbon members and an oxygen member, andR.sup.2 is halogen, unsubstituted or substituted alkyl, alkoxy, alkenyloxy, alkynyloxy, alkadienyloxy, benzyloxy or benzylthio, are used for controlling pests.Type: GrantFiled: January 4, 1993Date of Patent: October 18, 1994Assignee: BASF AktiengesellschaftInventors: Reinhard Kirstgen, Rainer Otter, Christoph Kuenast, Uwe Kardorff, Wolfgang Steglich, Gunda Bertram
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Patent number: 5352440Abstract: A method for inducing melanin synthesis in melanocytes, thereby increasing the melanin content of melanocytes and, thus, increasing pigmentation, melanocytes with increased melanin content produced by these methods, and uses thereof.Type: GrantFiled: August 21, 1992Date of Patent: October 4, 1994Assignee: Trustees of Boston UniversityInventors: Barbara A. Gilchrest, Philip R. Gordon
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Patent number: 5346887Abstract: A method and a composition for treating or reducing and/or controlling intraocular pressure comprising administering an effective amount of a renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; W is CO or CHOH and U is CH.sub.2 or NR.sub.2 wherein R.sub.2 is hydrogen or loweralkyl; with the proviso that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloalkylmethyl, benzyl, (alpha, alpha) -dimethylbenzyl, 4-hydroxybenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, 1-benzyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R.sub.3 is loweralkyl, loweralkenyl, ((alkoxy)alkoxy)loweralkyl, (thioalkoxy)alkyl, benzyl or heterocyclic ring substituted methyl; and R.sub.4 is substituted hydroxyalkylamino.Type: GrantFiled: April 23, 1991Date of Patent: September 13, 1994Assignee: Abbott LaboratoriesInventors: Herman H. Stein, Jacob J. Plattner, Steven R. Crowley
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Patent number: 5326770Abstract: This invention relates to monoamine oxidase-B (MAO-B) inhibitory 5-substituted 2,4-thiazolidinediones, such as Formula I, to pharmaceutical compositions thereof, process of preparation, and methods of use in mammals to treat cognitive disorders, neurological dysfunction, and/or mood disturbances such as, but not limited to degenerative nervous system diseases.Type: GrantFiled: July 17, 1992Date of Patent: July 5, 1994Assignee: The Du Pont Merck Pharmaceutical CompanyInventor: Wendell W. Wilkerson
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Patent number: 5314916Abstract: Compounds having beta-2 adrenergic agonist activity and the use of these compounds in controlling intraocular pressure are disclosed. The compounds are believed to be useful in controlling intraocular pressure by increasing the outflow of aqueous humor. The compounds are considered to be less likely to cause cardiovascular side effects and various other side effects associated with stimulation of beta-1 receptors, relative to epinephrine.Type: GrantFiled: April 19, 1993Date of Patent: May 24, 1994Assignee: Alcon Laboratories, Inc.Inventors: Billie M. York, Evan P. Kyba
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Patent number: 5272162Abstract: This invention relates to compounds having the following formula ##STR1## or a pharmaceutically acceptable salt thereof which are useful in the inhibition of platelet aggregation, to pharmaceutical compositions including the compounds and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.Type: GrantFiled: July 2, 1992Date of Patent: December 21, 1993Assignee: G. D. Searle & Co.Inventors: Foe S. Tjoeng, Jeffery A. Zablocki
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Patent number: 5262436Abstract: Mercapto-acylamino acids useful in the treatment of hypertension and combinations of mercapto-acylamino acids and atrial natriuretic factors or angiotensin converting enzyme inhibitors useful for treating hypertension are disclosed.Type: GrantFiled: August 6, 1991Date of Patent: November 16, 1993Assignee: Schering CorporationInventors: Martin F. Haslanger, Bernard R. Neustadt, Elizabeth M. Smith
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Patent number: 5258398Abstract: This invention relates to novel diaminoalkanoic acid derivatives that inhibit platelet aggregation and thrombus formation in mammalian blood thereby being useful in the prevention and treatment of thrombosis associated with disease states such as myocardial infarction, stroke, peripheral arterial disease and disseminated intravascular coagulation, to pharmaceutical compositions including such compounds, and to their use in inhibiting thrombus formation and platelet aggregation in mammals.Type: GrantFiled: December 16, 1991Date of Patent: November 2, 1993Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: Scott I. Klein, Bruce F. Molino
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Patent number: 5232920Abstract: Novel N-(mercaptoalkyl)amides of the formula ##STR1## wherein R.sub.1 is lower alkyl, cyclolower alkyl, aryl or heteroaryl;R.sub.2 is (COR.sub.3)-aryl, heteroaryl, substituted (COR.sub.3)-aryl or substituted heteroaryl, wherein the substituents are 1-3 substituents selected from the group consisting of carboxy, alkoxycarbonyl, lower alkyl, hydroxy, halo, lower alkoxy, cyclolower alkyl, cyano, trifluoromethyl, phenyl, phenoxy and phenylthio;R.sub.3 is --OR.sub.4 or --NR.sub.4 R.sub.5 ;R.sub.4 and R.sub.5 are independently selected from the group consisting of hydrogen, lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl and aryl lower alkyl, or R.sub.4 and R.sub.5 together with the nitrogen to which they are attached form a 5-, 6- or 7-membered ring;Q is hydrogen or R.sub.6 CO--;R.sub.Type: GrantFiled: December 21, 1990Date of Patent: August 3, 1993Assignee: Schering CorporationInventor: Bernard R. Neustadt
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Patent number: 5223509Abstract: This invention relates to certain .beta.-carbolines, which are antagonists of the functions of cholecystokinin (CCK) and gastrin, to pharmaceutical compositions comprising these compounds, and to the use of these compounds in the prevention and treatment of disorders of the gastrointestinal, central nervous and appetite-regulatory systems of mammals, especially of humans.Type: GrantFiled: February 21, 1992Date of Patent: June 29, 1993Assignee: Merck & Co., Inc.Inventor: Ben E. Evans
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Patent number: 5219842Abstract: A .beta.-glucooligosaccharide-containing composition comprising at least one material selected from food, drink and medicine, and at least one selected from a glucooligosaccharide comprising at least one .beta.-1,6 bond and a reduced product thereof. A method of improving intestinal floras, comprising administering to a human or animal for ingestion a physiologically effective amount of at least one selected from a glucooligosaccharide comprising at least one .beta.-1,6 bond and a reduced product thereof. The ingestion of the .beta.-glucooligosaccharide and/or the reduced product thereof can bring about promotion of the selective growth of useful bacteria such as Bifidobacteria and lactic acid bacteria, inhibition of the growth of harmful bacteria or putrefactive bacteria, and hence improvement in the intestinal floras.Type: GrantFiled: August 9, 1990Date of Patent: June 15, 1993Assignee: Nihon Shokuhin Kako Co., Ltd.Inventors: Gentaro Okada, Teruo Nakakuki, Seishiro Kainuma, Takehiro Unno
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Patent number: 5220050Abstract: This invention relates to 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 amidines derivatives.Type: GrantFiled: November 12, 1991Date of Patent: June 15, 1993Assignee: G. D. Searle & Co.Inventors: Philippe R. Bovy, Dudley E. McMackins, Joseph G. Rico, Foe S. Tjoeng, Mihaly V. Toth, Robert B. Garland, Masateru Miyano, Jeffery A. Zablocki
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Patent number: 5194447Abstract: A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen or --CONHSO.sub.2 -Ar; andAr is phenyl, naphthyl, pyridyl, quinolyl, isoquinolyl, quinoxalyl, thienyl, thionaphthyl, furyl, benzofuryl, benzodioxyl, benzoxazolyl, benzoisoxazolyl, or benzodioxolyl; wherein the Ar group may be optionally mono-, di, or tri-substituted; with the provision that R.sup.1 and R.sup.2 are not hydrogen; oror a pharmaceutically acceptable salt thereof which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host vs. graft disease, autoimmune diseases and diseases of inflammation; by virtue of its antitumor activity is useful in treating solid tumors; and by virtue of its antifungal activity is useful in treating fungal infections.Type: GrantFiled: February 18, 1992Date of Patent: March 16, 1993Assignee: American Home Products CorporationInventor: Wenling Kao
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Patent number: 5187189Abstract: This invention discloses novel sulfoximines having the formula: ##STR1## where Z is C.sub.1 -C.sub.6 alkylene and Y is alkyl, arylalkyl, acyl, carbamoyl, sulfonyl or alkoxycarbonyl. The invention compounds are useful in the treatment of Class II arrhythmia.Type: GrantFiled: January 22, 1991Date of Patent: February 16, 1993Assignee: American Home Products CorporationInventors: Mark R. Hellberg, James R. Shanklin, Jr.
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Patent number: 5187183Abstract: The invention relates to novel S-nitroso derivatives of ACE inhibitors and to pharmaceutical compositions comprising the S-nitrosothiol derivatives of the invention together with a pharmaceutically acceptable carrier.The invention also relates to methods for treating various pathophysiological conditions including acute myocardial infarction, left ventricular dysfunction without overt heart failure, hypertension, pulmonary hypertension, congestive heart failure, angina pectoris, vascular thrombosis, Raynauds syndrome, scleroderma, toxemia of pregnancy, acute renal failure, diabetic nephropathy, and renal artery stenosis, and to methods of inhibiting ACE and effecting vasodilation comprising administering the S-nitrosothiol derivatives of the ACE inhibitors of the invention to an animal.Type: GrantFiled: June 14, 1991Date of Patent: February 16, 1993Assignee: Brigham & Women's HospitalInventors: Joseph Loscalzo, John Cooke
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Patent number: 5185375Abstract: Therapeutically useful thioformamide derivatives of the formula: ##STR1## wherein R represents alkyl, Ar represents optionally substituted phenyl group, Y represents ethylene, methylene or a valency bond, and X represents carbonyl, hydroxymethylene, >C.dbd.NOR.sup.1, >C.dbd.NN(R.sup.1).sub.2 or >C.dbd.NN(R.sup.1)CON(R.sup.1).sub.2 in which R.sup.1 represents hydrogen or optionally substituted alkyl, benzyl, phenethyl, 1-naphthylmethyl, 2-naphthylmethyl or pyrid-3-ylmethyl or two R.sup.1 substituents on the same nitrogen atom may together form optionally substituted alkylene, and salts thereof, processes for their preparation and compositions containing them are described.Type: GrantFiled: March 30, 1990Date of Patent: February 9, 1993Assignee: May & Baker LimitedInventors: David C. Cook, Terance W. Hart, Iain M. McLay, Malcolm N. Palfreyman, Roger J. A. Walsh
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Patent number: 5180744Abstract: Non-peptidyl compounds characterized generally as aralkyl-N-terminal amino hydroxy .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are of the formula ##STR1## wherein R.sub.1 is selected from ##STR2## wherein each of Y and Z is independently selected from hydrido, chloro, fluoro, methoxy and dimethylamino; wherein n is a number selected from zero through four, inclusive; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is methyl or ethyl; wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 is hydroxy; wherein R.sub.7 is isobutyl or ethyl; and wherein each of R.sub.8 and R.sub.9 is hydrido; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: July 29, 1991Date of Patent: January 19, 1993Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran, Dave Weissing, Mark Russell
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Patent number: 5177106Abstract: Novel 4-amino substituted phenoxyalkyl carboxylic acid, ester, and alcohol derivatives are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful in preventing the intestinal absorption of cholesterol and thus are useful in the treatment of hypercholesterolemia and atherosclerosis.Type: GrantFiled: June 21, 1991Date of Patent: January 5, 1993Assignee: Warner-Lambert CompanyInventor: Paul L. Creger
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Patent number: 5175170Abstract: Non-peptidyl compounds characterized generally as cycloalkyl/cycloalkylkyl-N-terminal amino hydroxy .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest of the formula ##STR1## wherein R.sub.1 is selected from cycloalkyl and cycloakylalkyl groups, wherein said cycloalkyl group contains three to about eight carbon atoms and the acyclic alkyl portion of said cycloakylalkyl group contains one to about eight carbon atoms; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is methyl or ethyl; wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 is hydroxy; and wherein R.sub.7 is isobutyl or ethyl; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: July 29, 1991Date of Patent: December 29, 1992Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran, Dave Weissing, Mark Russell
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Patent number: 5166212Abstract: Disclosed are compound of the formula ##STR1## wherein X and Y independently represent hydroxymethyl; cyano; carboxy; functionally modified carboxy selected from esterified carboxy, carbamoyl, and N-substituted carbamoyl; 5-tetrazolyl; 2-oxazolyl, 4,5-dihydro-2-oxazolyl, or each said grouping substituted by lower alkyl; R and R.sub.o independently represent lower alkyl, (C.sub.3 -C.sub.7)-cycloalkyl-lower alkyl, or aryl-lower alkyl; A represents methylene; or A represents methylene substituted by lower alkyl, by lower alkylthio-lower alkyl, by aryl-lower alkylthio-lower alkyl, by arylthio-lower alkyl, by hydroxy-lower alkyl, by acyloxy-lower alkyl, by lower alkoxy-lower alkyl, by alkyloxy-lower alkyl, by aryloxy-lower alkyl, by amino-lower alkyl by acylamino-lower alkyl, by guanidino-lower amino-lower alkyl, by (C.sub.3 -C.sub.7)-cycloalkyl, by (C.sub.3 -C.sub.Type: GrantFiled: April 25, 1991Date of Patent: November 24, 1992Assignee: Ciba-Geigy CorporationInventor: Gary M. Ksander
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Patent number: 5140044Abstract: A UCN-1028D derivative represented by the formula: ##STR1## has protein kinase C inhibitory activity and is expected to be used as an active ingredient in anti-tumor agents, etc.Type: GrantFiled: March 27, 1990Date of Patent: August 18, 1992Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Teruo Kishi, Hiromitsu Saito, Hiroshi Sano, Isami Takahashi, Tatsuya Tamaoki
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Patent number: 5132312Abstract: Disclosed are novel 3-hydroxy-3-methylglutarylcoenzyme A reductase inhibitors useful as antihypercholesterolemic agents represented by the formula ##STR1## and the corresponding ring-opened hydroxy acids derived therefrom and pharmaceutically acceptable salts thereof.Pharmaceutical compositions containing said compounds and method of inhibiting the biosynthesis of cholesterol therewith are also disclosed.Type: GrantFiled: November 27, 1990Date of Patent: July 21, 1992Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: John R. Regan, Kent E. Neuenschwander
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Patent number: 5130119Abstract: Fluorosubstituted benzene derivatives of Formula I ##STR1## wherein Y, R.sup.2, R.sup.3 and R.sup.4 are defined herein, are NMR diagnostic agents.Type: GrantFiled: October 6, 1989Date of Patent: July 14, 1992Assignee: Schering AktiengesellschaftInventors: Peter Blaszkiewicz, Ulrich Niedballa, Heinz Gries, Hans Bauer, Hanns-Joachim Weinmann
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Patent number: 5124322Abstract: Novel compounds of formula (I), salts, solvates and hydrates thereof: ##STR1## in which: R.sub.1 and R.sub.2 are independently hydrogen; alkyl; alkoxy; halogen; or CF.sub.3 ;R.sub.3 is hydrogen; acyl, such as ##STR2## where Z is optionally substituted aryl; or a group R--S-- where R is an organic residue such that the group R--S-- provides an in vivo-cleavable disulphide bond;R.sub.4 is C.sub.3-6 alkyl;R.sub.5 is hydrogen; alkyl; --CH.sub.2 --R.sub.10 where R.sub.10 is optionally substituted phenyl or heteroaryl; or a group ##STR3## where R.sub.11 is hydrogen; alkyl; or --CH.sub.2 --Ph is optionally substituted phenyl; and R.sub.12 is hydrogen or alkyl; andR.sub.6 is hydrogen; alkyl; or a group ##STR4## where R.sub.13 is hydrogen; or alkyl; and R.sub.14 is hydroxy; alkoxy; or --NR.sub.7a R.sub.8 where each of R.sub.7a and R.sub.8 is hydrogen or alkyl, or R.sub.7a and R.sub.Type: GrantFiled: June 19, 1989Date of Patent: June 23, 1992Assignee: Beecham Group p.l.c.Inventor: Ian Hughes
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Patent number: 5098934Abstract: Novel .omega.-mercaptopropanamides and their homologs of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen and ##STR2## R.sub.1 ' is selected from the group consisting of alkyl of 1 to 5 carbon atoms and aryl optionally substituted with at least one member of the group consisting of --OH, alkyl and alkoxy of 1 to 5 carbon atoms, --NO.sub.2 and halogen, n is an integer from 1 to 5, R.sub.2 is selected from the group consisting of hydrogen alkyl of 1 to 5 carbon atoms and aryl and aralkyl of 6 to 15 carbon atoms optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, --OH, halogen and --CF.sub.3, R.sub.3 is selected from the group consisting of a) hydrogen, b) phenyl optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, --OH, --NO.sub.2, halogen, --CF.sub.Type: GrantFiled: June 22, 1990Date of Patent: March 24, 1992Assignee: Roussel UclafInventors: Jean-Paul Vevert, Francoise Delevallee, Rogert Deraedt
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Patent number: 5096700Abstract: The subject invention involves halogenated amino acid derivatives useful as antimicrobial agents having the structure: ##STR1## wherein --R is hydrogen or 2-aminoethyl; --R' is hydroxy, alkoxy, aryloxy, or an amino acid residue bonded at the amino nitrogen; --R" is hydrogen or an amino acid residue bonded at the carbonyl carbon; --X is halogen; and --Y is hydrogen or halogen.Type: GrantFiled: September 28, 1990Date of Patent: March 17, 1992Assignee: The Procter & Gamble CompanyInventors: William L. Seibel, Joseph H. Gardner
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Patent number: 5077309Abstract: Novel compounds have the formula (I) ##STR1## where ##STR2## represents one of the divalent cyclic groups ##STR3## the letters a and b indicating in each case the points of attachment of the substituents R.sup.1 and CV(R.sup.2)-NV'R, respectively; R.sup.1 is a group --(CH.sub.2).sub.b --(A).sub.a --(CH.sub.2).sub.c --B--CH.sub.2 --CO.sub.2 R' in which A and B are each separately oxygen or sulphur, a is 0, b is 0 and c is an integer from 3 to 10, or a is 1, b is 0 or an integer from 1 to 7 and c is an integer from 2 to 9 with the sum of b and c being from 2 to 9, and CO.sub.2 R' is a carboxy group or an amide, ester or salt derivative thereof; V and V' either each separately is hydrogen or together are the second bond of a carbon-nitrogen double bond; R.sup.2 is hydrogen, an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted by an aromatic group directly or through an oxygen or sulphur atom; and R is a group --OR.sup.3, --OR.sup.4, --D--R.sup.3, --N.dbd. R.sup.5 or --NW.G.Type: GrantFiled: March 28, 1990Date of Patent: December 31, 1991Assignee: National Research Development CorporationInventors: Robert L. Jones, Norman H. Wilson
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Patent number: 5066680Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is aryl which may have one or more suitable substituent(s),R.sup.2 is aryl which may have one or more suitable substituent(s), lower alkyl or cyclo(lower)alkyl,R.sup.3 is hydrogen, hydroxy, halogen, lower alkenyl, amino or protected amino,R.sup.4 is a group of the formula: ##STR2## wherein R.sup.5 is lower alkyl which may have one or more suitable substituent(s), cyclo(lower)alkyl, aryl, ar(lower)alkyl which may have one or more suitable substituent(s), andR.sup.6 is hydrogen or lower alkyl; or N-containing heterocyclic group which may have one or more suitable substituent(s), andA is lower alkylene or lower alkynylene, in which R.sup.1 and R.sup.2 may be linked through oxygen atom, their preparation and use in treatment of dysuria, and starting materials for their preparation.Type: GrantFiled: February 5, 1990Date of Patent: November 19, 1991Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Youichi Shiokawa, Kazuo Okumura, Kazuhiko Take, Kazunori Tsubaki
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Patent number: 5053430Abstract: Novel compounds having the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein. These compounds are useful in the treatment of schizophrenia.Type: GrantFiled: September 22, 1989Date of Patent: October 1, 1991Assignee: Boehringer Ingelheim KGInventors: Matthias Grauert, Herbert Merz, Joachim Mierau, Gunter Schingnitz, Claus Schneider
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Patent number: 5051446Abstract: The present invention relates to new compounds of the formula I ##STR1## as well as their preparation, pharmaceutical preparations containing same, and method of treating acute myocardial infarction.The compounds which possess beta-adrenoceptor blocking activity are very shortacting and are preferably intended for treatment of acute myocardial infarction by administration by means of injection.Type: GrantFiled: March 13, 1989Date of Patent: September 24, 1991Assignee: E. I. du Pont de Nemours & Co.Inventors: Enar I. Carlsson, Bill B. Gustafsson, Bo T. Lungren