Plural Hetero Atoms In The Polycyclo Ring System Patents (Class 540/521)
-
Patent number: 5484783Abstract: The present invention relates to the use of certain mercaptoacetylamide and benzazapine derivatives in treating patients suffering from hypertriglyceridemia, atherosclerosis and hypercholesterolemia.Type: GrantFiled: March 24, 1994Date of Patent: January 16, 1996Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Gary A. Flynn, John F. French, Richard C. Dage
-
Patent number: 5476933Abstract: Disclosed are methods of preparing azepines by a multistep synthesis including a Diels-Alder reaction. Also disclosed are methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, inducing anesthesia and treating or preventing opiate tolerance are disclosed by administering to an animal in need of such treatment an azepine which has high binding to the NMDA glycine site.Type: GrantFiled: November 16, 1994Date of Patent: December 19, 1995Assignees: State of Oregon, acting by and through The Oregon State Board of Higher Education, acting for and on behalf of The Oregon health Sciences University and The University of Oregon, Acea Pharmaceuticals, Inc.Inventors: John F. W. Keana, Anthony P. Guzikowski, Daniel F. Nogales, Sui X. Cai
-
Patent number: 5470975Abstract: Novel A-II receptor antagonists have the formula ##STR1## and its isomer ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are as defined herein.Type: GrantFiled: January 11, 1994Date of Patent: November 28, 1995Assignee: E.R. Squibb & Sons, Inc.Inventor: Karnail Atwal
-
Patent number: 5468745Abstract: The present invention relates to compounds of the formula ##STR1## wherein A is methylene, oxygen, sulfur or N--B wherein B is R.sub.1 or COR.sub.2 wherein R.sub.1 is hydrogen, a C.sub.1 -C.sub.4 alkyl or an Ar--Z--group wherein Ar is aryl and Z is a C.sub.0 -C.sub.4 alkyl and R.sub.2 is a --CF.sub.3, a C.sub.1 -C.sub.10 alkyl or an Ar--Z group;R is hydrogen or a C.sub.1 -C.sub.4 alkyl; andX and Y are each independently hydrogen, nitro or amino, with the proviso that when X is nitro or amino, Y must be hydrogen, and when Y is nitro or amino, X must be hydrogen; andpharmaceutically acceptable salts thereof, which are inhibitors of Angiotensin Converting Enzyme.Type: GrantFiled: August 18, 1994Date of Patent: November 21, 1995Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Gary A. Flynn, Douglas W. Beight
-
Patent number: 5457196Abstract: The present invention relates to novel 2-substituted indane-2-carboxyalkyl derivatives useful as inhibitors of enkephalinase and ACE.Type: GrantFiled: December 6, 1993Date of Patent: October 10, 1995Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Alan M. Warshawsky, Gary A. Flynn
-
Patent number: 5455242Abstract: The present invention relates to compounds of the formula ##STR1## wherein B.sub.1 and B.sub.2 are each independently hydrogen; hydroxy; --OR.sub.2 wherein R.sub.2 is a C.sub.1 -C.sub.4 alkyl or an Ar--Y group wherein Ar is aryl and Y is a hydrogen or C.sub.1 -C.sub.4 alkyl; or, where B.sub.1 and B.sub.2 are attached to adjacent carbon atoms, B.sub.1 and B.sub.2 can be taken together with said adjacent carbons to form a benzene ring or methylenedioxy;A is a bond, methylene or oxygen, sulfur or NR.sub.4 or NCOR.sub.5 wherein R.sub.4 is hydrogen, a C.sub.1 -C.sub.4 alkyl or an Ar--Y-- group and R.sub.5 is --CF.sub.3, a C.sub.1 -C.sub.10 alkyl or an Ar--Y-- group;R.sub.3 is hydrogen or --CH.sub.2 OC(O)C(CH.sub.3).sub.3 ;R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl or --CH.sub.2 OC(O)--C(CH.sub.3).sub.3 ; andn is an integer 1 to 3,which are useful as inhibitors of enkephalinase and ACE.Type: GrantFiled: November 2, 1993Date of Patent: October 3, 1995Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Alan M. Warshawsky, Gary A. Flynn
-
Patent number: 5436250Abstract: A compound having the formula ##STR1## wherein R.sup.4 and R.sup.5 independently are hydrogen, halogen, CF.sub.3, CN, NO.sub.2 or SO.sub.2 NR.sup.1 R.sup.2 whereinR.sup.1 is hydrogen or C.sub.1-6 -alkyl which may be straight, branched or cyclic,R.sup.2 is hydrogen or C.sub.1-6 -alkyl which may be straight, branched or cyclic, or wherein R.sup.1 and R.sup.2 together represent --(CH.sub.2).sub.n --A--(CH.sub.2).sub.m --, wherein A is O, S, CH.sub.2 or NR.sup.I, wherein R.sup.I is H, C.sub.1-6 -alkyl which may be straight, branched or cyclic, n is 0, 1, 2, 3, 4, 5 and m is 0, 1, 2, 3, 4, 5;R.sup.II is hydrogen, benzyl, (C.dbd.O)CF.sub.3, C.sub.1-6 -carboxylic acid acyl, C.sub.1-6 -alkoxy which may be branched or cyclic, or C.sub.1-6 -alkyl which may be straight, branched or cyclic, CH.sub.2 CO.sub.2 R.sup.VI wherein R.sup.VI is hydrogen or C.sub.Type: GrantFiled: July 7, 1993Date of Patent: July 25, 1995Assignee: NeuroSearch A/SInventors: Frank Watjen, Bjarne H. Dahl, Jorgen Drejer, Lein H. Jensen
-
Patent number: 5434261Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.Type: GrantFiled: July 26, 1993Date of Patent: July 18, 1995Assignee: Merck & Co., Inc.Inventors: William R. Schoen, Matthew J. Wyvratt, Jr.
-
Patent number: 5430145Abstract: The present invention relates to certain novel mercaptoacetylamide derivatives useful as inhibitors of enkephalinase and of ACE.Type: GrantFiled: November 9, 1993Date of Patent: July 4, 1995Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Gary A. Flynn, Philippe Bey, Alan M. Warshawsky, Douglas W. Beight, Shujaath Mehdi, Eugene L. Giroux, Timothy P. Burkholder, Edward D. Daugs, John F. French
-
Patent number: 5430144Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.Type: GrantFiled: July 26, 1993Date of Patent: July 4, 1995Assignee: Merck & Co., Inc.Inventors: William R. Schoen, Matthew J. Wyvratt, Jr., Paul J. Hodges
-
2-substituted indane-2-mercaptoacetylamide derivatives useful as inhibitors of enkephalinase and ace
Patent number: 5428158Abstract: The present invention relates to novel 2-substituted indane-2-mercaptoacetylamide derivatives which are useful as inhibitors of enkephalinase and ACE.Type: GrantFiled: November 1, 1993Date of Patent: June 27, 1995Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Alan M. Warshawsky, Gary A. Flynn -
Patent number: 5424425Abstract: The present invention relates to novel aminoacetylmercapto derivatives useful as inhibitors of enkephalinase and ACE.Type: GrantFiled: September 10, 1993Date of Patent: June 13, 1995Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Gary A. Flynn, Robert J. Cregge, Thomas L. Fevig, Shyam Sunder, Patrick W. Shum
-
Patent number: 5420271Abstract: The present invention relates to novel 2-substitited indane-2-mercaptoacetylamide tricyclic derivatives which are useful as inhibitors of Enkephalise.Type: GrantFiled: June 17, 1993Date of Patent: May 30, 1995Assignee: Merrell Dow Pharmaceuticals, Inc.Inventors: Alan M. Warshawsky, Gary A. Flynn
-
Patent number: 5416082Abstract: Disclosed herein are pyrroloazepine derivatives having anti-.alpha..sub.1 activity and anti-serotonin activity represented by the following formula (I): ##STR1## wherein R means a hydrogen atom, a linear or branched C.sub.1-6 alkyl group or a C.sub.7-10 aralkyl group, A denotes a linear or branched C.sub.2-10 alkylene, alkenylene or alkynylene group, Z stands for O, NOR.sub.1 or NOCOR.sub.5 in which R.sub.1 and R.sub.5 is a hydrogen atom or an alkyl, aryl or aralkyl group, and Y means a particular piperidinyl or pyrrolidinyl group; and salts thereof. Their preparation processes are also disclosed.Type: GrantFiled: February 14, 1994Date of Patent: May 16, 1995Assignee: Suntory LimitedInventors: Akira Mizuno, Hidetsura Cho, Mikiko Hamaguchi, Toshio Tatsuoka, Takafumi Ishihara
-
Patent number: 5399557Abstract: This invention provides a pyrroloazepine compound represented by the following formula (I) or (II): ##STR1## wherein Z.sub.1, Z.sub.2, R, A and Y are defined in the claims. The pyrroloazepine compounds according to the present invention are drugs having excellent anti-serotonin action. Coupled with their high safety, they can therefore be used as novel therapeutics for ischemic heart diseases. In addition, the compounds of the present invention include those having anti-.alpha..sub.1 action. Such compounds are effective as hypotensive drugs. Pyrroloazepine compounds according to the present invention are therefore extremely useful as therapeutics for a wide variety of circulatory diseases.Type: GrantFiled: April 7, 1993Date of Patent: March 21, 1995Assignee: Suntory LimitedInventors: Akira Mizuno, Mikiko Miya, Norio Inomata, Toshio Tatsuoka, Takafumi Ishihara
-
Patent number: 5391731Abstract: Disclosed herein are pyrroloazepine derivatives, which are useful as therapeutics for circulatory diseases, represented by the following formula (I): ##STR1## wherein R means a hydrogen atom, a linear or branched C.sub.1-6 alkyl group or a C.sub.7-10 aralkyl group, A denotes a linear or branched C.sub.2-10 alkylene, alkenylene or alkynylene group, Z stands for O, NOR.sub.1 or NOCOR.sub.5 in which R.sub.1 and R.sub.5 is a hydrogen atom or an alkyl, aryl or aralkyl group, and Y means a particular piperidinyl or pyrrolidinyl group; and salts thereof. Their preparation processes are also disclosed.Type: GrantFiled: December 9, 1992Date of Patent: February 21, 1995Assignee: Suntory LimitedInventors: Akira Mizuno, Hidetsura Cho, Mikiko Hamaguchi, Toshio Tatsuoka, Takafumi Ishihara
-
Patent number: 5389628Abstract: The present invention relates to compounds of the formula ##STR1## wherein A is methylene, oxygen, sulfur or N--B wherein B is R.sub.1 or COR.sub.2 wherein R.sub.1 is hydrogen, a C.sub.1 -C.sub.4 alkyl or an Ar--Z-- group wherein Ar is aryl and Z is a C.sub.0 -C.sub.4 alkyl and R.sub.2 is a --CF.sub.3, a C.sub.1 -C.sub.10 alkyl or an Ar--Z group;R is hydrogen or a C.sub.1 -C.sub.4 alkyl; andX and Y are each independently hydrogen, nitro or amino, with the proviso that when X is nitro or amino, Y must be hydrogen, and when Y is nitro or amino, X must be hydrogen; andpharmaceutically acceptable salts thereof, which are inhibitors of Angiotensin Converting Enzyme.Type: GrantFiled: December 8, 1993Date of Patent: February 14, 1995Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Gary A. Flynn, Douglas W. Beight
-
Patent number: 5328912Abstract: The invention encompasses compounds of the formula: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof wherein n is 0, 1, or 2, X is ##STR2## Z is H.sub.2, oxygen or sulfur, and R.sub.1, R.sub.2, R.sub.3, R.sub.4, T, W, and Y are defined variables.These compounds are highly selective agonists or inverse agonists for the GABAa brain receptors and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine type drugs, and enhancement of alertness.Type: GrantFiled: February 1, 1993Date of Patent: July 12, 1994Assignee: Neurogen CorporationInventor: Pamela Albaugh
-
Patent number: 5317101Abstract: The invention relates to tricyclic heterocycles of the formula I ##STR1## wherein X is oxy, thio, sulphinyl, sulphonyl, amino, (1-4C)alkylamino or methylene;Y is carbonyl or methylene;each R.sup.1 includes hydrogen, halogeno and various other substituents;each of m and n is 1 or 2;A.sup.1, alkylene, alkenylene or alkynylene;Het is a 5 or 6 membered heteroaryl group optionally bearing particular substituents; andG is carboxy, 1H-tetrazol-5-yl or a group of the formula:--CONH--SO.sub.2 R.sup.2wherein R.sup.2 is (1-4C)alkyl, benzyl or phenyl;and pharmaceutically-acceptable salts thereof, which possess anti-hyperalgesic properties. The invention also relates to processes for the manufacture of said tricyclic heterocycles; and to novel pharmaceutical compositions containing them.Type: GrantFiled: September 25, 1992Date of Patent: May 31, 1994Assignee: Imperial Chemical Industries PLCInventors: John Oldfield, Howard Tucker
-
Patent number: 5308841Abstract: The present invention relates to compounds of the formula ##STR1## wherein A is methylene, oxygen, sulfur or N-B wherein B is R.sub.1 or COR.sub.2 wherein R.sub.1 is hydrogen, a C.sub.1 -C.sub.4 alkyl or an Ar-Z-group wherein Ar is aryl and Z is a C.sub.0 -C.sub.4 alkyl and R.sub.2 is a --CF.sub.3, a C.sub.1 -C.sub.10 alkyl or an Ar-Z group;R is hydrogen or a C.sub.1 -C.sub.Type: GrantFiled: April 12, 1993Date of Patent: May 3, 1994Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Gary A. Flynn, Douglas W. Beight
-
Patent number: 5294611Abstract: The invention provides novel 2,3,6 substituted quinazolinones having the formula: ##STR1## wherein R.sup.6, R and X are as described in the specification, which have activity as angiotensin II (AII) antagonists.Type: GrantFiled: April 23, 1993Date of Patent: March 15, 1994Assignee: American Cyanamid CompanyInventors: Aranapakam M. Venkatesan, Jeremy I. Levin
-
Patent number: 5258511Abstract: Heterocyclic compounds of the formula ##STR1## in which R represents hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted hetaryl,A represents C--R.sup.1, N,R.sup.1 represents substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted hetaryl,X, Y represent O, NH,Z represents hydrogen, --CN, substituted or unsubstituted aryl, substituted or unsubstituted hetaryl,W represents O, N--R.sup.5,R.sup.5 represents hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, a substituted or unsubstituted heterocyclic radical andB represents a substituted or unsubstituted carbocyclic-aromatic or heterocyclic ring onto which one or more further rings can be fused,and the use of these compounds as dyestuffs or pigments.Type: GrantFiled: July 20, 1992Date of Patent: November 2, 1993Assignee: Bayer AktiengesellschaftInventor: Hans Hochstetter
-
Patent number: 5242918Abstract: A compound having the formula ##STR1## wherein R.sup.4 and R.sup.5 independently are hydrogen, halogen, CF.sub.3, CN, NO.sub.2 or SO.sub.2 NR.sup.1 R.sup.2 whereinR.sup.1 is hydrogen or straight, C.sub.1-6 -alkyl which may be branched or cyclic,R.sup.2 is hydrogen or straight, C.sub.1-6 -alkyl which may be branched or cyclic,or wherein R.sup.1 and R.sup.2 together represent --(CH.sub.2).sub.n --A--(CH.sub.2).sub.m --, wherein A is O, S, CH.sub.2 or NR.sup.I, wherein R.sup.I is H, C.sub.1-6 -alkyl which may be straight, branched or cyclic, n is 0, 1, 2, 3, 4, 5 and m is 0, 1, 2, 3, 4, 5;Q is NOH or O;Z=O, S, N--R.sup.II, ##STR2## wherein R.sup.II, R.sup.III, R.sup.IV and R.sup.V independently are hydrogen, benzyl, C.sub.1-6 carboxylic acid-acyl, C.sub.1-6 -alkoxy which may be branched or cyclic, or C.sub.1-6 -alkyl which may be branched or cyclic;X is --(CH.sub.2).sub.o -- wherein o is 0, 1, 2, or 3;Y is --(CH.sub.2).sub.p -- wherein p is 0, 1, 2 or 3;.alpha. and .beta.Type: GrantFiled: August 27, 1992Date of Patent: September 7, 1993Assignee: NeuroSearch A/SInventors: Frank Watjen, Bjarne H. Dahl, Jorgen Drejer, Leif H. Jensen
-
Patent number: 5240934Abstract: Quinoline derivatives of the formula, ##STR1## wherein >A represents a group >N--(CH.sub.2).sub.n --, >C.dbd., >C.dbd.CH(CH.sub.2).sub.n --, or >CH(CH.sub.2).sub.n --, wherein n is an integer of 0-7; Y represents a group >C.dbd.O or >CHOH, R.sup.1 is a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, or an alkylthio group, R.sup.2 is a hydrogen atom, a halogen atom, an alkyl group, a hydroxy group, an alkoxy group, a phenyl group which may have a substituent, a phenoxy group, an alkanoyloxy group, or an amino group which may have a substituent, R.sup.3 is a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group, and m is an integer of 1-3. The compounds and their salts exhibit a superior anti-acetylcholinesterase activity with no side effects and are effective for the prevention or cure of senile dementia or memory disturbance.Type: GrantFiled: September 18, 1992Date of Patent: August 31, 1993Assignee: SS Pharmaceutical Co., Ltd.Inventors: Hiroshi Hasegawa, Kazuo Isomae, Takeshi Kotsugai, Noriaki Shioiri, Kumiko Sekine, Naokata Taido, Susumu Sato, Tadayuki Kuraishi
-
Patent number: 5238932Abstract: The present invention relates to novel mercaptoacetylamide tricyclic derivatives useful as inhibitors of enkephalinase.Type: GrantFiled: May 20, 1992Date of Patent: August 24, 1993Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Gary A. Flynn, Alan M. Warshawsky
-
Patent number: 5212177Abstract: Novel compounds having the formula ##STR1## and its isomer ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and X are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, an antihypertensive agents.Type: GrantFiled: December 16, 1991Date of Patent: May 18, 1993Assignee: E. R. Squibb & Sons, Inc.Inventors: Michael A. Poss, Karnail S. Atwal
-
Patent number: 5208230Abstract: The present invention relates to compounds of the formula ##STR1## wherein A is methylene, oxygen, sulfur or N-B wherein B is R.sub.1 or COR.sub.2 wherein R.sub.1 is hydrogen, a C.sub.1 -C.sub.4 alkyl or an Ar--Z-- group wherein Ar is aryl and Z is a C.sub.0 -C.sub.4 alkyl and R.sub.2 is a --CF.sub.3, a C.sub.1 -C.sub.10 alkyl or an Ar--Z group;R is hydrogen or a C.sub.1 -C.sub.4 alkyl; andX and Y are each independently hydrogen, nitro or amino, with the proviso that when X is nitro or amino, Y must be hydrogen, and when Y is nitro or amino, X must be hydrogen; andpharmaceutically acceptable salts thereof, which are inhibitors of Angiotensin Converting Enzyme.Type: GrantFiled: June 25, 1992Date of Patent: May 4, 1993Assignee: Merrell Dow PharmaceuticalsInventors: Gary A. Flynn, Douglas W. Beight
-
Patent number: 5206239Abstract: Disclosed herein are pyrroloazepine derivatives, which are useful as therapeutics for circulatory diseases, represented by the following formula (I): ##STR1## wherein R means a hydrogen atom, a linear or branched C.sub.1-6 alkyl group or a C.sub.7-10 aralkyl group, A denotes a linear or branched C.sub.2-10 alkylene, alkenylene or alkynylene group, Z stands for O, NOR.sub.1 or NOCOR.sub.5 in which R.sub.1 and R.sub.5 is a hydrogen atom or an alkyl, aryl or aralkyl group, and Y means a particular piperidinyl or pyrrolidinyl group; and salts thereof. Their preparation processes are also disclosed.Type: GrantFiled: February 7, 1991Date of Patent: April 27, 1993Assignee: Suntory LimitedInventors: Akira Mizuno, Hidetsura Cho, Mikiko Hamaguchi, Toshio Tatsuoka, Takafumi Ishihara
-
Patent number: 5200406Abstract: Imidazole derivatives are described which are useful in restoring learning and treating memory difficulties. A compound of the invention is 2,5-dioxohexahydro-1H-pyrrolo[1,2-a]imidazole.Type: GrantFiled: April 3, 1992Date of Patent: April 6, 1993Assignee: I.S.F. Societa per AzioniInventors: Mario Pinza, Alberto Cerri, Carlo Farina, Maria T. Riccaboni
-
Patent number: 5183820Abstract: The invention provides potent and selective antagonists of 5-HT at 5-HT.sub.3 receptors which are tricyclic lactams of the formula (I) ##STR1## wherein Im represents an imidazolyl group of the formula: ##STR2## and R.sup.1 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, phenylC.sub.1-3 alkyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CONR.sup.5 R.sup.6 or --SO.sub.2 R.sup.5 ;one of the groups represented by R.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl group, and each of the other two groups, which may be same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group;Y represents the group CH.dbd.CH or (CH.sub.2).sub.n, wherein n represents 2 or 3;Q represents a halogen atom, or a group selected from hydroxy, C.sub.1-4 alkoxy, phenylC.sub.1-3 alkoxy, C.sub.Type: GrantFiled: April 26, 1991Date of Patent: February 2, 1993Assignee: Glaxo Group LimitedInventors: Ian H. Coates, Alexander W. Oxford, Peter C. North, Barry J. Price
-
Patent number: 5175157Abstract: Disclosed are new cyclic amine derivatives of the formula I ##STR1## wherein the substituents are defined in the specification. These compounds are useful as for treating sinus tachycardia.Type: GrantFiled: July 3, 1991Date of Patent: December 29, 1992Assignee: Boehringer Ingelheim GmbHInventors: Manfred Psiorz, Joachim Heider, Andreas Bomhard, Manfred Reiffen, Norbert Hauel, Klaus Noll, Berthold Narr, Christian Lillie, Walter Kobinger, Jurgen Dammgen
-
Patent number: 5149699Abstract: This invention relates to pyrrolo-, pyrido-, azepino-, and azocinopyrimidines of the general formula I ##STR1## useful for treating hypertension and congestive heart failure, to pharmaceutical compositions, and to methods for production thereof.Type: GrantFiled: October 24, 1991Date of Patent: September 22, 1992Assignee: American Home Products CorporationInventors: John W. Ellingboe, Madelene Nikaido, Jehan Bagli
-
Patent number: 5141930Abstract: A fused thiophene compound of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt thereof. In the above formula, one of E.sup.1, E.sup.2 and E.sup.3 is sulfur atom and other two of them are C--R.sup.1 and C--R.sup.2 respectively. R.sup.1 and R.sup.2 are the same or different and each is hydrogen, halogen, nitro, amino, cyano, hydroxyl, formyl, alkyl, alkoxy, haloalkyl, arylalkyl, acyl, alkoxyalkyl, acyloxyalkyl, hydroxyalkyl, acyloxyalkanoyl, alkoxyalkanoyl, hydroxyalkanoyl, aryloxyalkanoyl, haloalkanoyl, alkylthio, alkylsulfinyl, alkylsulfonyl, arylthio, arylsulfinyl, arylsulfonyl, hydroxysulfonyl, halosulfonyl, sulfamoyl, substituted sulfamoyl, carboxyl, acylamino, alkoxycharbonyl, carbamoyl, substituted carbamoyl or substituted amino. D is --CH.sub.2 -- or --S(O).sub.m -- (m is 0, 1 or 2). Q is straight or branched chain alkylene. T is primary amino, secondary amino or tertiary amino.Type: GrantFiled: July 8, 1991Date of Patent: August 25, 1992Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Tohru Nakao, Hiroshi Tanaka, Hirotake Yamato, Takeshi Akagi, Shuzo Takehara
-
Patent number: 5095015Abstract: The invention encompasses compounds of the formula: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof where n is 0, 1, or 2 and x is ##STR2## and R.sub.1, R.sub.2, R.sub.3, Y, Z, W, T are defined variables. These compounds are highly selective agonists or inverse agonists for the GABAa brain receptors and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine type drugs, and enhancement of alertness.Type: GrantFiled: July 24, 1990Date of Patent: March 10, 1992Assignee: Neurogen CorporationInventor: Pamela Albaugh
-
Patent number: 5053422Abstract: Imidazole derivatives are described which are useful in restoring learning and treating memory difficulties. A compound of the invention is 2,5-dioxohexahydro-1H-pyrrolo[1,2-a]imidazole.Type: GrantFiled: February 6, 1989Date of Patent: October 1, 1991Assignee: I.S.F. Societa per AzioniInventors: Mario Pinza, Alberto Cerri, Carlo Farina, Maria T. Riccaboni
-
Patent number: 5015638Abstract: This invention relates to substituted pyridooxazinone and naphtheridone pyridones which are useful as cardiotonic agents for the treatment of congestive heart failure, to methods for increasing cardiac contractility using said compounds, and pharmaceutical compositions including the same.Type: GrantFiled: November 3, 1989Date of Patent: May 14, 1991Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: Alfred P. Spada, William L. Studt, Henry F. Campbell, Donald E. Kuhla, Thomas Tucker
-
Patent number: 4985422Abstract: Compounds which are potent and selective antagonists of the effect of 5-HT.sub.3 receptors and are useful in the treatment of psychotic disorders, anxiety, and nausea and vomiting, of the general formula (I) ##STR1## wherein Im represents an imidazolyl group of the formula (a), (b) or (c): ##STR2## one of the groups represented by R.sup.1, R.sup.2 and R.sup.3 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenyl C.sub.1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group;n represents 1 or 2;Q represents a hydrogen atom, a halogen atom, or a hydroxy, C.sub.1-4 alkoxy, phenyl C.sub.1-3 alkoxy or C.sub.1-6 alkyl group, or a group --NR.sup.4 R.sup.5 or --CONR.sup.4 R.sup.5 ; andX represents an oxygen or a sulphur atom, and, when Im represents an imidazolyl group of formula (c), X may also represent the group NR.sup.6, where R.sup.Type: GrantFiled: April 26, 1989Date of Patent: January 15, 1991Assignee: Glaxo Group LimitedInventors: Peter C. North, Alexander W. Oxford, Ian H. Coates, Paul J. Beswick
-
Patent number: 4973585Abstract: This invention relates to derivatives of fused bicyclic or tricyclic lactams, to the intermediates and processes useful for their preparation and to their pharmacological effect in inhibiting the angiotensin converting enzyme and to their end-use application in the treatment of hypertension.Type: GrantFiled: May 10, 1989Date of Patent: November 27, 1990Assignee: Merrell Dow PharmaceuticalsInventors: Gary A. Flynn, Douglas W. Beight
-
Patent number: 4960784Abstract: Certain substituted indazoles, including all geometric and stereoisomers thereof, agricultural compositions containing the indazoles and use of the indazoles as insecticides.Type: GrantFiled: October 2, 1989Date of Patent: October 2, 1990Assignee: E. I. Du Pont de Nemours and CompanyInventor: George P. Lahm
-
Patent number: 4959368Abstract: A pharmaceutical composition comprising a pyrimidine represented by the following formula ##STR1## wherein R.sup.1 represents a hydrogen atom, an acyl group having 2 to 4 carbon atoms, an alkoxycarbonyl group having 2 to 5 carbon atoms, an alkoxycarbonylmethyl group having 3 to 5 carbon atoms, a 3,4-dimethoxybenzoyl group or a 3,4-methylenedioxybenzyl group,R.sup.2 represents a hydrogen atom, an amino group, a monoalkylamino group having 1 to 4 carbon atoms, an alkoxy group having 1 to 5 carbon atoms or an alkoxycarbonyl group having 2 to 4 carbon atoms,R.sup.3 represents a hydrogen atom, an alkoxycarbonyl group having 2 to 4 carbon atoms, a dialkylaminocarbonyl group having 1 to 9 carbon atoms in each alkyl moiety, an alkoxy group having 1 to 5 carbon atoms, or a hydroxyethyl group, R.sup.2 and R.sup.3, together with the carbon atoms to which they are bonded, may form a 5- to 7-membered carbocyclic ring or a heterocyclic ring having N, O or S as the hetero atom, and R.sup.Type: GrantFiled: October 22, 1987Date of Patent: September 25, 1990Assignees: Mitsui Petrochemical Industries Ltd., Mitsui Pharmaceuticals, Inc.Inventors: Akira Awaya, Takuo Nakano, Hisashi Kobayashi, Ken E. Tan, Kazutoshi Horikomi, Tadayuki Sasaki, Keiichi Yokoyama, Hiroyasu Ohno, Kozi Kato, Takumi Kitahara, Ikuo Tomino, Shigeru Isayama
-
Patent number: 4959361Abstract: The invention relates to compounds of the formula ##STR1## wherein X is --CH.dbd.CH-- or S; R.sub.1 is lower alkyl, lower alkoxy or trifluoromethyl;R.sub.2 is hydrogen, lower alkyl, lower alkoxy, hydroxy or alkanoyloxy;R.sub.3 and R.sub.4, independently, are hydrogen, chlorine, fluorine, lower alkyl or lower alkoxy;s is an integer from 0 to 1, provided that when s is 1,R.sub.2 cannot be hydroxy, lower alkoxy or alkanoyloxy;R.sub.5 is a radical of the formula R.sub.6 --(CH.sub.2).sub.n -- or R.sub.7 --O--(CH.sub.2).sub.m --wherein R.sub.6 and R.sub.7 are aryl or a heterocyclic radical, n is an integer of from 0 to 2 and m is an integer of from 1 to 2, provided that, when n is 0, R.sub.6 must be attached through a carbon to carbon bond, and provided that R.sub.7 is always attached through a carbon to oxygen bond,and, when at least one asymmetric carbon is present, its enantiomers and racemates, and pharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: October 3, 1988Date of Patent: September 25, 1990Assignee: Hoffmann-La Roche Inc.Inventor: Armin Walser
-
Patent number: 4954625Abstract: Novel compounds of the formula: ##STR1## [wherein A is an .alpha.-amino acid residue; B is a group represented by the formula: ##STR2## wherein R.sup.4 is hydrogen, lower alkyl, aralkyl or amino-lower alkyl), whereby the linkage between the symbols A and B designates a peptide bond and the group R.sup.4 in B may be linked with A; R.sup.1 is hydrogen, lower alkyl or aralkyl; R.sup.2 is hydrogen, lower alkyl, aralkyl or acyl; X is alkylene] and salts thereof posses, for example, inhibitory activity on angiotensin converting enzyme, and are useful as an agent for diagnosis, prevention or treatment of hypertension as well as circulatory diseases such as cardiopathy and cerebral apoplexy.Type: GrantFiled: August 30, 1989Date of Patent: September 4, 1990Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Kohei Nishikawa, Katsumi Ito
-
Patent number: 4946847Abstract: Tetracyclic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, X, Y, Z and n are as hereinafter described, and salts thereof, prepared starting from corresponding tricyclic compounds, are described. The compounds I and some of the said tricyclic compounds have antibacterial activity, and are therefore useful as antibacterial agents.Type: GrantFiled: November 21, 1988Date of Patent: August 7, 1990Assignee: Hoffmann-La Roche Inc.Inventors: Synese Jolidon, Rita Locher, Ivan Kompis, Ekkehard Weiss, Pierre-Charles Wyss
-
Patent number: 4927819Abstract: The present invention provides a compound of formula I: ##STR1## or a salt thereof, wherein: the dotted lines represent optional double bonds;R.sup.1 represents hydrogen, hydroxy, alkenyl, alkyl, aminoalkyl or hydroxyalkyl;R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 independently represet hydrogen, hydroxy, fluoro, alkenyl, aryl, alkyl, or alkyl substituted with aryl, amino, hydroxy, carboxy or fluoro; andR.sup.7, R.sup.8, R.sup.9 and R.sup.10 independently represent hydrogen, hydrocarbon or a heterocyclic group provided that R.sup.7, R.sup.8, R.sup.9 and R.sup.10 are not simultaneously hydrogen; orR.sup.7 and R.sup.8 and/or R.sup.9 and R.sup.10 may complete a saturated or unsaturated C.sub.4-9 hydrocarbon or heterocyclic ring; which compounds are useful as anticonvulsant agents and in the treatment and/or prevention of neurodegenerative disorders.Type: GrantFiled: November 22, 1988Date of Patent: May 22, 1990Assignee: Merck Sharp & Dohme LimitedInventors: Raymond Baker, William R. Carling, Kim James, Paul D. Leeson
-
Patent number: 4927831Abstract: This invention relates to spiro-isoquinoline-pyrrolidine tetrones and their pharmaceutically acceptable salts thereof, to processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneficial for the prevention of diabetes mellitus associated complications.Type: GrantFiled: May 26, 1989Date of Patent: May 22, 1990Assignee: American Home ProductsInventor: Michael S. Malamas
-
Patent number: 4910302Abstract: Compounds of the formula: ##STR1## in which Z is ##STR2## wherein X is alkylene, ethanylene or alkylidene; Q is alkylene, alkylidene, ##STR3## or Q, taken together with the carbon atoms to which it is attached forms a benzene ring or a substituted benzene ring, in which said substituents are --OH, --OCH.sub.3, alkyl, halo, --CF.sub.3, --NH.sub.2, monoalkylamino, dialkylamino or alkanoylamino; R.sup.1 is hydrogen or alkyl; R.sup.2 and R.sup.3 are, independently, hydrogen or alkyl or taken together with the carbon atoms to which they are attached, they form a cycloalkane or cycloalkene ring; m is one of the integers 2-5; R.sup.4 is hydrogen, hydroxy, cyano, alkyl, alkoxy, halo, amino, alkylamino, phenylamino, tolylamino, xylylamino, mesitylamino, methoxyphenylamino, or halophenylamino; and the dotted lines represent optional unsaturation; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 19, 1988Date of Patent: March 20, 1990Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, Gary P. Stack
-
Patent number: 4880924Abstract: This invention relates to a selective process for preparing bicyclic lactam-lactone compounds wherein the rings are fused, i.e. the rings share at least two carbon atoms, or are isolated. In particular, the present invention provides a process for selectively reacting novel 1-hydrocarbylamino (or heteroatom-substituted hydrocarbylamino); 1,1-dicarboxylic acid, alkylesters; 1-alkanolactonyl or hydrocarbyl (or heteroatom-substituted hydrocarbyl) alkanonylactonyl methane, as the salt of an acid having a pKa of 0 or more, to provide bicyclic lactam-lactone compounds. The selectively of the reaction to either fused or isolated bicyclic compounds is controlled by cyclizing the novel salts, in the absence of a base, a cyclizing said novel salts, in the presence of an amount of base substantially equivalent to said acid, respectively.Type: GrantFiled: April 3, 1986Date of Patent: November 14, 1989Assignee: Nelson Research & Development Co.Inventors: James V. Peck, Gevork Minaskanian
-
Patent number: 4871842Abstract: Novel compounds of the formula: ##STR1## [wherein A is an .alpha.-amino acid residue; B is a group represented by the formula: ##STR2## (wherein R.sup.4 is hydrogen, lower alkyl, aralkyl or amino-lower alkyl), whereby the linkage between the symbols A and B designates a peptide bond and the group R.sup.4 in B may be linked with A; R.sup.1 is hydrogen, lower alkyl or aralkyl; R.sup.2 is hydrogen, lower alkyl, aralkyl or acyl; X is alkylene] and salts thereof possess, for example, inhibitory activity on angiotensin converting enzyme, and are useful as an agent for diagnosis, prevention or treatment of hypertension as well as circulatory diseases such as cardiopathy and cerebral apoplexy.Type: GrantFiled: July 14, 1988Date of Patent: October 3, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Kohei Nishikawa, Katsumi Ito
-
Patent number: 4812565Abstract: This invention is directed to compounds having the formula: ##STR1## wherein: A represents an aromatic or heterocyclic ring having two of its carbon atoms held mutually with the oxazepine, thiazepine or diazepine moiety selected from the group consisting of benzene, naphthalene, a quinoline, a pyridine in any of its four positions, any of which rings are optionally substituted by one or two Y radicals selected from the group consisting of halo, loweralkyl, loweralkoxy, diloweralkylamino, nitro, amino, lower acylamino, trilfuoromethyl, phenyl or phenyl substituted by one to three Y' groups selected from halo, loweralkyl, loweralkoxy, diloweralkylamino, nitro, amino, loweracylamino or trifluoromethyl,E is selected from oxygen, sulfur or ##STR2## B is selected from the group consisting of loweralkyl, cycloalkyl or phenyl-loweralkyl wherein phenyl is optionally substituted by one or two radicals selected from halo, loweralkyl, loweralkoxy, nitro or trifuoromethyl,N is 1 or 2,R.sup.4 and R.sup.Type: GrantFiled: February 25, 1987Date of Patent: March 14, 1989Assignee: A. H. Robins Company, IncorporatedInventor: Albert D. Cale, Jr.
-
Patent number: 4797397Abstract: Certain .alpha.-[(2-nitro-1H-imidazol-1-yl)methyl]-aziridinylethanols and the corresponding aziridine-ring opened analogs are useful as radiation sensitizers for X-irradiation therapy of tumors.Type: GrantFiled: July 31, 1987Date of Patent: January 10, 1989Assignee: Warner-Lambert CompanyInventors: Mark J. Suto, Leslie M. Werbel