Polycyclo-carbocyclic Ring System Having At Least Three Cyclos Patents (Class 544/154)
  • Patent number: 4727072
    Abstract: 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: Grant
    Filed: February 12, 1986
    Date of Patent: February 23, 1988
    Assignee: McNeilab, Inc.
    Inventors: Philip P. Grous, Richard J. Mohrbacher
  • Patent number: 4670435
    Abstract: 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: Grant
    Filed: December 2, 1985
    Date of Patent: June 2, 1987
    Assignee: BASF Aktiengesellschaft
    Inventors: Albrecht Franke, deceased, Claus D. Mueller, Dieter Lenke
  • Patent number: 4658061
    Abstract: 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: Grant
    Filed: December 24, 1984
    Date of Patent: April 14, 1987
    Assignee: Eli Lilly and Company
    Inventors: William B. Lacefield, Richard L. Simon
  • Patent number: 4642373
    Abstract: 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: Grant
    Filed: July 6, 1984
    Date of Patent: February 10, 1987
    Assignee: Pfizer Inc.
    Inventors: James F. Eggler, Michael R. Johnson, Lawrence S. Melvin, Jr.
  • Patent number: 4610986
    Abstract: 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: Grant
    Filed: October 12, 1984
    Date of Patent: September 9, 1986
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Kikuo Ishizumi, Michihisa Muramatsu, Norihiko Tanno, Hiromi Sato, Noboru Yoshida
  • Patent number: 4605673
    Abstract: 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: Grant
    Filed: December 19, 1983
    Date of Patent: August 12, 1986
    Assignee: Warner-Lambert Company
    Inventors: Gerhard Satzinger, Edgar Fritschi, Manfred Herrmann
  • Patent number: 4564698
    Abstract: The present invention relates to new tricyclic compounds of the formula: ##STR1## having valuable CNS and cardiovascular properties.
    Type: Grant
    Filed: January 24, 1983
    Date of Patent: January 14, 1986
    Assignee: Akzo N.V.
    Inventors: Johannes H. Wieringa, Frans A. van der Vlugt
  • Patent number: 4486598
    Abstract: Novel compounds of the following general formula: ##STR1##
    Type: Grant
    Filed: February 22, 1982
    Date of Patent: December 4, 1984
    Assignee: The Upjohn Company
    Inventor: Paul A. Aristoff
  • Patent number: 4473704
    Abstract: 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: Grant
    Filed: March 16, 1982
    Date of Patent: September 25, 1984
    Assignee: Pfizer Inc.
    Inventors: James F. Eggler, Michael R. Johnson, Lawrence S. Melvin, Jr.
  • Patent number: 4452745
    Abstract: 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: Grant
    Filed: September 29, 1982
    Date of Patent: June 5, 1984
    Assignee: Eli Lilly and Company
    Inventors: William B. Lacefield, Richard L. Simon
  • Patent number: 4376773
    Abstract: 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: Grant
    Filed: February 25, 1981
    Date of Patent: March 15, 1983
    Assignee: BASF Aktiengesellschaft
    Inventors: Gerd Steiner, Hans P. Hofmann, Horst Kreiskott, Hans-Juergen Teschendorf
  • Patent number: 4374984
    Abstract: 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: Grant
    Filed: March 4, 1981
    Date of Patent: February 22, 1983
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Jurgen Eichler, Claus Herz, Karl-Heinz Neisius, Gregor Wehner
  • Patent number: 4323691
    Abstract: 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: Grant
    Filed: December 1, 1980
    Date of Patent: April 6, 1982
    Assignee: Abbott Laboratories
    Inventors: Carroll W. Ours, Cheuk M. Lee
  • Patent number: 4317910
    Abstract: 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: Grant
    Filed: August 14, 1978
    Date of Patent: March 2, 1982
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Frederic P. Hauck, Joyce Reid
  • Patent number: 4306075
    Abstract: 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: Grant
    Filed: December 22, 1980
    Date of Patent: December 15, 1981
    Assignee: The Upjohn Company
    Inventor: Paul A. Aristoff
  • Patent number: 4277473
    Abstract: 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: Grant
    Filed: December 12, 1979
    Date of Patent: July 7, 1981
    Assignees: Kao Soap Co., Ltd., Sumitomo Chemical Industries Ltd.
    Inventors: Yoshiaki Inamoto, Motoyoshi Osugi, Eiji Kashihara
  • Patent number: 4272536
    Abstract: 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: Grant
    Filed: December 12, 1979
    Date of Patent: June 9, 1981
    Assignees: Kao Soap Co., Ltd., Sumitomo Chemical Industries Ltd.
    Inventors: Yoshiaki Inamoto, Motoyoshi Osugi, Eiji Kashihara
  • Patent number: 4208326
    Abstract: 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: Grant
    Filed: June 5, 1978
    Date of Patent: June 17, 1980
    Assignee: Sandoz Ltd.
    Inventors: Helmut Egger, Hellmuth Reinshagen
  • Patent number: 4169146
    Abstract: 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: Grant
    Filed: June 30, 1977
    Date of Patent: September 25, 1979
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Junki Katsube, Atsuyuki Kojima, Makoto Sunagawa, Yoshinori Takashima, Yoshito Kameno, Hisao Yamamoto
  • Patent number: 4127717
    Abstract: 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: Grant
    Filed: March 20, 1978
    Date of Patent: November 28, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Frederic P. Hauck, Joyce Reid
  • Patent number: 4113726
    Abstract: 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: Grant
    Filed: February 28, 1974
    Date of Patent: September 12, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Frederic Peter Hauck, Christopher Michael Cimarusti
  • Patent number: 4107206
    Abstract: 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: Grant
    Filed: October 26, 1976
    Date of Patent: August 15, 1978
    Assignee: Akzona Incorporated
    Inventors: Colin Leslie Hewett, David Samuel Savage
  • Patent number: 4096267
    Abstract: [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: Grant
    Filed: June 10, 1975
    Date of Patent: June 20, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
  • Patent number: 4085210
    Abstract: 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: Grant
    Filed: January 6, 1976
    Date of Patent: April 18, 1978
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Junki Katsube, Atsuyuki Kojima, Makoto Sunagawa, Yoshinori Takashima, Yoshito Kameno, Hisao Yamamoto
  • Patent number: 4061774
    Abstract: 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: Grant
    Filed: April 9, 1975
    Date of Patent: December 6, 1977
    Assignee: Lilly Industries, Limited
    Inventors: Jiban Kumar Chakrabarti, Terrence Michael Hotten, David Edward Tupper
  • Patent number: 4045432
    Abstract: 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: Grant
    Filed: March 15, 1976
    Date of Patent: August 30, 1977
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Roy Teruyuki Uyeda
  • Patent number: 4045560
    Abstract: 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: Grant
    Filed: July 7, 1976
    Date of Patent: August 30, 1977
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Makoto Sunagawa, Hiromi Sato, Junki Katsube, Hisao Yamamoto
  • Patent number: 4041173
    Abstract: 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: Grant
    Filed: October 6, 1975
    Date of Patent: August 9, 1977
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Peter H. Nelson, Karl G. Untch