Polycyclo-carbocyclic Ring System Having At Least Three Cyclos Patents (Class 544/154)
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Patent number: 4727072Abstract: Propylamines of the formula (I): ##STR1## and isomers thereof, particularly those enantiomers and racemates relative to the chiral carbon indicated by an asterisk (*). The propylamines can be used for the treatment of hypertension or angina in humans. A is pyrrolidine, piperidine or morpholine and B is an aromatic heterocycle, aromatic carbocycle or saturated carbocycle.Type: GrantFiled: February 12, 1986Date of Patent: February 23, 1988Assignee: McNeilab, Inc.Inventors: Philip P. Grous, Richard J. Mohrbacher
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10,11-dihydro-5H-dibenzo[a,d]cycloheptadiene derivatives in a method for treating cardiac arrhythmia
Patent number: 4670435Abstract: 10,11-Dihydro-5H-dibenzo[a,d]cycloheptadiene derivatives of the formula I ##STR1## where R.sup.1 and R.sup.2 have the meanings stated in the description, and their preparation are described. The novel substances are useful for the treatment of disorders.Type: GrantFiled: December 2, 1985Date of Patent: June 2, 1987Assignee: BASF AktiengesellschaftInventors: Albrecht Franke, deceased, Claus D. Mueller, Dieter Lenke -
Patent number: 4658061Abstract: Fluorenes bearing a 9-aminoalkyl substituent are useful antiarrhythmic agents. Pharmaceutical formulations containing such compounds are provided, as well as a method of treatment.Type: GrantFiled: December 24, 1984Date of Patent: April 14, 1987Assignee: Eli Lilly and CompanyInventors: William B. Lacefield, Richard L. Simon
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Patent number: 4642373Abstract: 1,2,3,4,4a,4b,5,6,7,8,8a,12b-Dodecahydro-7-(oxo, hydroxy or amino)-9-hydroxy-11-(alkyl, alkoxy or alkoxyalkyl)triphenylenes, 2,3,3a,3b,4,5,6,7,7a,11b-decahydro-6-(oxo, hydroxy or amino)-8-hydroxy-10-(alkyl, alkoxy or alkoxyalkyl)-1H-cyclopenta[1]-phenanthrenes, 2,3,4,4a,4b,5,6,7,8,8a-decahydro-7-(oxo, hydroxy or amino)-9-hydroxy-11-(alkyl, alkoxy, alkoxyalkyl, aralkyl, aralkoxy, aryloxyalkyl or aralkoxyalkyl)-1H-pyrido[1,2-f]phenanthridines, and 1,2,3,3a,3b,4,5,6,7,7a-decahydro-6-(oxo, hydroxy or amino)-8-hydroxy-10-(alkyl, alkoxy or alkoxyalkyl)pyrrolo[1,2-f]phenanthridines and derivatives are valuable as central nervous system active agents or as intermediates to compounds having such activity.Type: GrantFiled: July 6, 1984Date of Patent: February 10, 1987Assignee: Pfizer Inc.Inventors: James F. Eggler, Michael R. Johnson, Lawrence S. Melvin, Jr.
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Patent number: 4610986Abstract: A (7S,9S) isomer or its racemic modification of the aminonaphthacene derivative of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom, a hydroxyl group or a lower alkoxy group, R.sup.2 is a hydrogen atom or a hydroxyl group, R.sup.3 and R.sup.4 are each a lower alkoxy group or, when taken together, represent an ethylenedioxy group or an oxo group, A is an ethylene group optionally bearing at least one lower alkyl and Q is a hydroxyl group, a lower alkoxy group or a dimethylamino group, or an acid addition salt thereof, which is useful as an anti-tumor agent.Type: GrantFiled: October 12, 1984Date of Patent: September 9, 1986Assignee: Sumitomo Chemical Company, LimitedInventors: Kikuo Ishizumi, Michihisa Muramatsu, Norihiko Tanno, Hiromi Sato, Noboru Yoshida
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Patent number: 4605673Abstract: The invention is concerned with 7H-dibenzo(a,c)-cyclohepten-5-one-(7) derivatives of general formula I ##STR1## wherein R.sup.1 and R.sup.2 can be the same or different, a hydrogen atom, an alkyl radical containing 1 to 3 carbon atoms, or, together with the nitrogen atom to which they are attached form a heterocyclic ring containing 3 to 6 carbon atoms,n is 2 or 3R.sup.3 is a hydrogen atom or a halogen atom andX is either a methylene radical or an oxygen atomand the pharmacologically acceptable salts thereof with inorganic and organic acids.The invention is furthermore concerned with analogous processes for the preparation thereof and their application for controlling psychic diseases and gastric and/or intestinal ulcers.Type: GrantFiled: December 19, 1983Date of Patent: August 12, 1986Assignee: Warner-Lambert CompanyInventors: Gerhard Satzinger, Edgar Fritschi, Manfred Herrmann
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Patent number: 4564698Abstract: The present invention relates to new tricyclic compounds of the formula: ##STR1## having valuable CNS and cardiovascular properties.Type: GrantFiled: January 24, 1983Date of Patent: January 14, 1986Assignee: Akzo N.V.Inventors: Johannes H. Wieringa, Frans A. van der Vlugt
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Patent number: 4486598Abstract: Novel compounds of the following general formula: ##STR1##Type: GrantFiled: February 22, 1982Date of Patent: December 4, 1984Assignee: The Upjohn CompanyInventor: Paul A. Aristoff
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Patent number: 4473704Abstract: 1,2,3,4,4a,4b,5,6,7,8,8a,12b-Dodecahydro-7-(oxo, hydroxy or amino)-9-hydroxy-11-(alkyl, alkoxy or alkoxyalkyl)triphenylenes, 2,3,3a,3b,4,5,6,7,7a,11b-decahydro-6-(oxo, hydroxy or amino)-8-hydroxy-10-(alkyl, alkoxy or alkoxyalkyl)-1H-cyclopenta[1]phenanthrenes, 2,3,4,4a,4b,5,6,7,8,8a-decahydro-7-(oxo, hydroxy or amino)-9-hydroxy-11-(alkyl, alkoxy, alkoxyalkyl, aralkyl, aralkoxy, aryloxyalkyl or aralkoxyalkyl)-1H-pyrido[1,2-f]phenanthridines, and 1,2,3,3a,3b,4,5,6,7,7a-decahydro-6-(oxo, hydroxy or amino)-8-hydroxy-10-(alkyl, alkoxy or alkoxyalkyl)pyrrolo[1,2-f]phenanthridines and derivatives are valuable as central nervous system active agents or as intermediates to compounds having such activity.Type: GrantFiled: March 16, 1982Date of Patent: September 25, 1984Assignee: Pfizer Inc.Inventors: James F. Eggler, Michael R. Johnson, Lawrence S. Melvin, Jr.
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Patent number: 4452745Abstract: Fluorenes bearing a 9-aminoalkyl substituent are useful antiarrhythmic agents. Pharmaceutical formulations containing such compounds are provided, as well as a method of treatment.Type: GrantFiled: September 29, 1982Date of Patent: June 5, 1984Assignee: Eli Lilly and CompanyInventors: William B. Lacefield, Richard L. Simon
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Patent number: 4376773Abstract: 10-Substituted 5-cyanomethylene-10,11-dihydro-dibenzo[a,d]-cycloheptenes, their pharmaceutically tolerated addition salts with acids, processes for their preparation, and their use as drugs, especially as sedatives, hypnotics or tranquilizers.Type: GrantFiled: February 25, 1981Date of Patent: March 15, 1983Assignee: BASF AktiengesellschaftInventors: Gerd Steiner, Hans P. Hofmann, Horst Kreiskott, Hans-Juergen Teschendorf
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Patent number: 4374984Abstract: Compounds of the formula ##STR1## wherein the substituents A, Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, n and m are defined hereinbeloware effective photoinitiators, especially for the photopolymerization of ethylenically unsaturated compounds and for the curing of printing inks.Type: GrantFiled: March 4, 1981Date of Patent: February 22, 1983Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Jurgen Eichler, Claus Herz, Karl-Heinz Neisius, Gregor Wehner
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Patent number: 4323691Abstract: Described are compounds of the formula ##STR1## wherein ##STR2## wherein Z is hydrogen or loweralkyl, R.sub.5 and R.sub.6 may be the same or different and are hydrogen, loweralkyl or together are alkylene of 4 or 5 carbon atoms,R.sub.2 is hydrogen, halo, haloloweralkyl, loweralkyl, loweralkoxy, loweralkylthio or ##STR3## wherein R.sub.5 and R.sub.6 are previously defined, R.sub.3 is hydroxy, alkoxy, branched alkoxy, adamantyloxy, morpholino, amino or amino substituted by loweralkyl or alkylene of 4 or 5 carbon atoms,R.sub.4 is hydrogen or loweralkyl, andX.sub.1 and X.sub.2 are hydrogen, loweralkyl, halo or when substituted on adjacent carbon atoms of the benzene ring form a 1,3-butadienylene linkage, Y is oxygen or sulfur, and pharmaceutically acceptable salts thereof. The compounds are effective as diuretic agents in increasing urinary excretion.Type: GrantFiled: December 1, 1980Date of Patent: April 6, 1982Assignee: Abbott LaboratoriesInventors: Carroll W. Ours, Cheuk M. Lee
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Patent number: 4317910Abstract: Compounds having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein n is 1 or 2; m is 2, 3 or 4; and R.sub.2 is a tertiary amino group; are intermediates useful in the preparation of compounds having hypotensive activity.Type: GrantFiled: August 14, 1978Date of Patent: March 2, 1982Assignee: E. R. Squibb & Sons, Inc.Inventors: Frederic P. Hauck, Joyce Reid
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Patent number: 4306075Abstract: The present specification provides novel analogs of carbacyclin (CBA.sub.2), 6a-carba-prostacyclin (6a-carba-PGI.sub.2), which have pronounced prostacyclin-like pharmacological activity, e.g., as platelet antiaggregatory agents. Specifically the novel chemical analogs of CBA.sub.2 are those substituted by fluoro (C-5), alkyl (C-9), interphenylene (C-5), and methano (C-6a,9). Further provided are benzindene analogs of CBA.sub.2 and substituted forms thereof, i.e., 9-deoxy-2',9-methano (or 2',9-metheno)-3-oxa-4,5,6-trinor-3,7-(1',3'-interphenylene)-PGF.sub.1 compounds. Also provided are a variety of novel chemical intermediates, e.g., substituted bicyclo[3.3.0]octane intermediates, and chemical process utilizing such intermediates which are useful in the preparation of the novel CBA.sub.2 analogs.Type: GrantFiled: December 22, 1980Date of Patent: December 15, 1981Assignee: The Upjohn CompanyInventor: Paul A. Aristoff
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Patent number: 4277473Abstract: Compounds having the formula ##STR1## wherein a is 0 or 1, R.sub.1 is hydrogen or lower alkyl, A is lower alkylene or lower alkylidene, and R.sub.2 and R.sub.3, which can be the same or different, are hydrogen, lower alkyl, cycloalkyl, benzyl or substituted benzyl, or ##STR2## is a saturated heterocyclic ring, and acid addition salts thereof, possess anti-viral activity and reduced activity on the central nervous system.Type: GrantFiled: December 12, 1979Date of Patent: July 7, 1981Assignees: Kao Soap Co., Ltd., Sumitomo Chemical Industries Ltd.Inventors: Yoshiaki Inamoto, Motoyoshi Osugi, Eiji Kashihara
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Patent number: 4272536Abstract: A compound having the formula ##STR1## wherein a is 0 or 1, R.sub.1 is hydrogen or lower alkyl, A is lower alkylene or lower alkylidene, and R.sub.2 and R.sub.3, which can be the same or different, are hydrogen, lower alkyl, cycloalkyl, benzyl or substituted benzyl, or ##STR2## form a saturated heterocyclic ring, and pharmacologically acceptable acid addition salt thereof, exhibits anti-viral activity and is free from significant effect on the central nervous system.Type: GrantFiled: December 12, 1979Date of Patent: June 9, 1981Assignees: Kao Soap Co., Ltd., Sumitomo Chemical Industries Ltd.Inventors: Yoshiaki Inamoto, Motoyoshi Osugi, Eiji Kashihara
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Patent number: 4208326Abstract: This invention relates to new pleuromutilins of the formula: ##STR1## wherein either R.sub.1 is ethyl or vinyl,n is an integer from 2 to 5,X is sulphur,a group ##STR2## or a group .dbd.N--R.sub.4.sup.I, whereineither Y and Z are both sulphur, orone of Y and Z is oxygen and the other is sulphur, andR.sub.4.sup.I is hydrogen or a group of the formula: ##STR3## wherein R.sub.1 is as defined above, each of R.sub.2 and R.sub.3 is alkyl of 1 to 10 carbon atoms, orR.sub.2 and R.sub.3 together with the nitrogen atom form a heterocycle of 5 to 7 ring members, and pharmaceutically acceptable acid addition salts and quaternary salts thereof.Processes for the preparation of such compounds are described.The compounds are antibiotics with an antibacterial effect.Type: GrantFiled: June 5, 1978Date of Patent: June 17, 1980Assignee: Sandoz Ltd.Inventors: Helmut Egger, Hellmuth Reinshagen
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Patent number: 4169146Abstract: Novel morpholine compounds of the formula: ##STR1## wherein R.sub.1 represents hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.2 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.5 alkenyl, C.sub.3 -C.sub.5 alkynyl, aryl-(C.sub.1 -C.sub.4)alkyl, (C.sub.3 -C.sub.6)cycloalkyl(C.sub.1 -C.sub.4)alkyl, polyhalo(C.sub.2 -C.sub.4) alkyl or hydroxy(C.sub.2 -C.sub.4)alkyl, A represents straight or branched C.sub.2 -C.sub.4 alkylene, B represents a divalent radical selected from the group consisting of --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 --O--, --CH.sub.2 --S--, --S-- and --O--, >D--E-- represents a trivalent radical selected from the group consisting of >CH--CH.sub.2 -- and >C.dbd.CH-- and C.sub.1 and C.sub.2 each represent 1,2-phenylene optionally substituted with one or more substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.Type: GrantFiled: June 30, 1977Date of Patent: September 25, 1979Assignee: Sumitomo Chemical Company, LimitedInventors: Junki Katsube, Atsuyuki Kojima, Makoto Sunagawa, Yoshinori Takashima, Yoshito Kameno, Hisao Yamamoto
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Patent number: 4127717Abstract: Compounds having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein n is 1 or 2; m is 2, 3 or 4; R.sub.1 is alkanoyl; and R.sub.2 is a tertiary amino group; have hypotensive activity.Type: GrantFiled: March 20, 1978Date of Patent: November 28, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: Frederic P. Hauck, Joyce Reid
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Patent number: 4113726Abstract: Compounds are provided having the structure ##STR1## wherein n is 1 or 2, n.sup.1 is 0, 1 or 2 and n.sup.2 is 0, 1, 2 or 3, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 may be the same or different and can be hydrogen, lower alkyl, halolower alkyl, acyl, lower alkoxy-carbonyl ##STR2## amido ##STR3## or lower alkoxyalkylene, R can be lower alkoxy, lower alkyl or cycloalkyl, R.sub.8 can be hydrogen, lower alkyl, cycloalkyl, hydroxy, dialkylaminoalkyl or R.sub.9 O(CH.sub.2)q-. X is a single bond or a straight or branched bivalent aliphatic radical and Y is ##STR4## These compounds are useful in the treatment of hypertension.Type: GrantFiled: February 28, 1974Date of Patent: September 12, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: Frederic Peter Hauck, Christopher Michael Cimarusti
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Patent number: 4107206Abstract: The present invention relates to novel biologically active tricyclic compounds of the general formula: ##STR1## and salts thereof, IN WHICHR.sub.1 and R.sub.2 stand for hydroge, alkyl or alkenyl, an optionally substituted aralkyl group or an acyl group orR.sub.1 + r.sub.2 together with the nitrogen atom represent a heterocyclic 5- or 6-membered ring, andX and Y stand for hydrogen, hydroxy, halogen, alkyl or alkoxy of 1-6 carbon atoms, nitro, trifluoromethyl or an acyloxy group,Which compounds have valuable biological activities, particularly anorectic activity.Type: GrantFiled: October 26, 1976Date of Patent: August 15, 1978Assignee: Akzona IncorporatedInventors: Colin Leslie Hewett, David Samuel Savage
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Patent number: 4096267Abstract: [1-Oxo-2-aryl or thienyl-2-substituted-5-indanyloxy (or thio)]aklanoic acid, derivatives thereof, their salts, esters and amides are disclosed. The products display a dual pharmaceutical utility in that they exhibit diuretic, saluretic and uricosuric activity. Also disclosed are processes for the preparation of such [1-oxo-2-aryl or thienyl-2-substituted-5-indanyloxy (or thio)]alkanoic acids, pharmaceutical compositions comprising therapeutically effective amounts of such compounds and methods of treatment comprising administering such compounds and compositions.Type: GrantFiled: June 10, 1975Date of Patent: June 20, 1978Assignee: Merck & Co., Inc.Inventors: Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
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Patent number: 4085210Abstract: Novel morpholine compounds of the formula: ##STR1## wherein R.sub.1 represents hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.2 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.5 alkenyl, C.sub.3 -C.sub.5 alkynyl, aryl-(C.sub.1 -C.sub.4)alkyl, (C.sub.3 -C.sub.6)cycloalkyl(C.sub.1 -C.sub.4)alkyl, polyhalo(C.sub.2 -C.sub.4)alkyl or hydroxy(C.sub.2 -C.sub.4)alkyl, A represents straight or branched C.sub.2 -C.sub.4 alkylene, B represents a divalent radical selected from the group consisting of --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 --O--, --CH.sub.2 --S--, --S-- and --O--, >D --E-- represents a trivalent radical selected from the group consisting of >CH--CH.sub.2 -- and >C.dbd.CH-- and C.sub.1 and C.sub.2 each represent 1,2-phenylene optionally substituted with one or more substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.Type: GrantFiled: January 6, 1976Date of Patent: April 18, 1978Assignee: Sumitomo Chemical Company, LimitedInventors: Junki Katsube, Atsuyuki Kojima, Makoto Sunagawa, Yoshinori Takashima, Yoshito Kameno, Hisao Yamamoto
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Patent number: 4061774Abstract: Novel 2-substituted-1-methylamino adamantanes of formula: ##STR1## where X is hydroxyl or halogeno, and R.sup.1, R.sup.2 and R.sup.3 are hydrogen or C.sub.1-4 alkyl or R.sup.2 and R.sup.3 together with the nitrogen form a heterocyclic ring, having anti-Parkinsonian activity, pharmaceutical formulations containing the active adamantanes and novel 4-protoadamantane spiro oxirane and 1,2-difunctionalized intermediates useful in the preparation of the final products of the invention.Type: GrantFiled: April 9, 1975Date of Patent: December 6, 1977Assignee: Lilly Industries, LimitedInventors: Jiban Kumar Chakrabarti, Terrence Michael Hotten, David Edward Tupper
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Patent number: 4045432Abstract: Antidepressant 1,1a,6,10b-tetrahydrodibenzo-[a,e]-cyclopropa-[c]-cyclohepten-6-substitute d oximes and their pharmaceutically suitable salts useful for alleviating depression in mammals.Type: GrantFiled: March 15, 1976Date of Patent: August 30, 1977Assignee: E. I. Du Pont de Nemours and CompanyInventor: Roy Teruyuki Uyeda
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Patent number: 4045560Abstract: Novel morpholine compounds of the formula: ##STR1## wherein R.sub.1 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.5 alkenyl, aryl(C.sub.1 -C.sub.4)alkyl or (C.sub.3 -C.sub.6)cycloalkyl(C.sub.1 -C.sub.4)alkyl and n represents 1 or 2, and their non-toxic salts, which are useful as antidepressants and can be produced by various methods.Type: GrantFiled: July 7, 1976Date of Patent: August 30, 1977Assignee: Sumitomo Chemical Company, LimitedInventors: Makoto Sunagawa, Hiromi Sato, Junki Katsube, Hisao Yamamoto
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Patent number: 4041173Abstract: A compound selected from the group of compounds represented by the formula ##STR1## R is hydrogen, alkyl having 1 to 12 carbon atoms, or ##STR2## where n is an integer of 2 to 4 inclusive and R.sup.4 and R.sup.5 are independently lower alkyl of 1 to 6 carbon atoms inclusive or together R.sup.4 and R.sup.5 and the nitrogen atom to which they are attached form a heterocyclic ring having 5 to 6 total ring atoms;R.sup.1 is at the 7, 8 or 9 position and is halogen, hydroxy, lower alkoxy of 1 to 6 carbon atoms inclusive, or lower alkyl of 1 to 4 carbons atoms, inclusive;The dotted lines may be an additional, optional bond between the carbon atoms at the 10- and 11 positions; andThe pharmaceutically acceptable salts thereof. The compounds are used pharmaceutically to treat allergic reactions and autoimmune diseases.Type: GrantFiled: October 6, 1975Date of Patent: August 9, 1977Assignee: Syntex (U.S.A.) Inc.Inventors: Peter H. Nelson, Karl G. Untch