Polycyclo-carbocyclic Ring System Having At Least Three Cyclos Patents (Class 544/380)
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Patent number: 5607937Abstract: The present invention relates to D,L-, L- and D-phenylalanine piperazides of formula (I) defined in claim 1 that inhibit blood coagulation, and thrombin and/or trypsin, respectively. The compounds are extraordinarily absorbable after oral, intraduodenal and in particular rectal administration and show only a low toxicity.Type: GrantFiled: January 5, 1995Date of Patent: March 4, 1997Assignee: Pentapharm AGInventors: Joerg Stuerzebecher, Helmut Vieweg, Peter Wikstroem, Christoph Adler
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Patent number: 5565457Abstract: The compounds are N-(2,3,4-trimethoxybenzyl)piperazines N'-substituted by a radical containing a sulfonamide group, and pharmaceutically tolerable salts thereof, useful for treating myocardial ischaemic pathologies, cerebral vascular accident and manifestations of deficiency associated with chronic cerebral circulatory disorders.A compound disclosed is : N-benzyl-N-{3,3-dimethyl-4-[4-(2,3,4-trimethoxybenzyl) piperazin-1-yl]butyl}-(isoquinolin-5-yl)sulfonamide and its fumarate.Type: GrantFiled: February 23, 1995Date of Patent: October 15, 1996Assignee: Adir et CompagnieInventors: Jean-Louis Peglion, Jean-Paul Vilaine, Nicole Villeneuve, Jean-Pierre Iliou, Jean-Pierre Bidouard
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Patent number: 5508280Abstract: This invention relates to novel derivatives of 5H-dibenzo (a,d)cycloheptenes, to the processes for their preparation, to their muscarinic receptor antagonist properties and to their end-use application for treating Parkinson's Disease, tardive dyskinesia, and motion sickness.Type: GrantFiled: January 30, 1995Date of Patent: April 16, 1996Assignee: Merrell Pharmaceuticals, Inc.Inventors: Marcel Hibert, Luc Van Hijfte, Mary Richards, Paul Moser
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Patent number: 5493036Abstract: The invention relates to fibre-reactive anthraquinone dyes of formula ##STR1## wherein R.sub.1, R.sub.2, B, U, R and n are as defined in claim 1. The anthraquinone dyes of formula (1) are suitable for dyeing or printing hydroxyl group containing or nitrogen-containing fibre materials and give dyeings or prints of good allround fastness properties.Type: GrantFiled: September 19, 1994Date of Patent: February 20, 1996Assignee: Ciba-Geigy CorporationInventor: Jean-Marie Adam
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Patent number: 5488119Abstract: Compounds of formulae I and II ##STR1## wherein D is H or --OR wherein R is phenyl and R.sub.1 to R.sub.4 are H or a substituent such as phenylthio, and one of the substituents R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is a group of formula III--E-CR.sub.5 =C(R.sub.6).sub.2 (III)or R is substituted by a group of formula III, wherein E is a direct bond or --X-C(O)-- wherein X is a linking group, and R.sub.5 and R.sub.6 are each independently of the other H, halogen, C.sub.1 -C.sub.12 alkyl or C.sub.6 -C.sub.10 aryl, can be polymerised to homopolymers or copolymers. The monomers and polymers are reversible photochromic systems which can be used as color indicators, as photochemically modifiable color filters, or for the optical storage of information.Type: GrantFiled: October 12, 1993Date of Patent: January 30, 1996Assignee: Ciba-Geigy CorporationInventors: Evelyn Fischer-Reimann, Walter Fischer
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Patent number: 5446146Abstract: A therapeutic agent for liver disease containing as an active ingredient a piperazine derivative having the formula: ##STR1## wherein, A represents a phenyl, p-benzoquinonyl or cumarinyl group which may have at least one substituent selected from the group consisting of halogen, alkyl, fluoroalkyl, formyl, alkoxycarbonyl, acyl, hydroxy, alkoxy, acyloxy, glycosyloxy, amino, alkylamino, mercapto, alkylthio and nitro; B represents a single bond or a straight chain alkylene group containing 1-4 carbon atoms which may have at least one substituent selected from the group consisting of alkyl, aryl, aralkyl, hydroxy and oxo; R represents an atom or a group selected from the group consisting of hydrogen, alkali metal, alkaline earth metal, alkyl, cycloalkyl, aralkyl and aryl; and n is 2 or 8, or its pharmaceutically acceptable salt is diclosed.Type: GrantFiled: June 7, 1994Date of Patent: August 29, 1995Assignee: Nippon Chemiphar Co., Ltd.Inventors: Mitsuo Masaki, Tomio Yamakawa, Masaru Satoh, Hiromitsu Takeda, Yasushi Yoshino, Hitoshi Matsukura
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Patent number: 5439940Abstract: The invention relates to novel, pharmaceutically active benz[e]indene derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, further to the use of the said benz[e]indene derivatives in the treatment of certain diseases and in the preparation of pharmaceutical compositions suitable for the treatment of said diseases.The new benz[e]indene derivatives according to the invention correspond to the general formula ##STR1## wherein A represents a group of the formula alk-NR.sup.1 R.sup.2, wherein alk represents a C.sub.2-7 alkylene group optionally carrying a hydroxy substituent,R.sup.1 and R.sup.2 are independently hydrogen, C.sub.1-7 alkyl, C.sub.2-7 alkenyl, C.sub.2-7 alkynyl, mono(C.sub.1-7)alkylamino(C.sub.1-7)alkyl, di(C.sub.1-7)alkylamino(C.sub.1-7)alkyl or C.sub.3-7 cycloalkyl; orR.sup.1 and R.sup.Type: GrantFiled: October 28, 1993Date of Patent: August 8, 1995Assignee: EGIS Gyogyszergyar Rt.Inventors: Klara Reiter nee Eszes, Zoltan Budai, Tibor Mezei, Gabor Blasko, Gyula Simig, Istvan Gyertyan, Luiza Petocz, Marton Fekete, Katalin Szemeredi, Istvan Gacsalyi, Gabor Gigler, Ludmilla Rohacas nee Zamkovaja, Maria Szecsey nee Hegedus, Eniko Szirt nee Kiszelly
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Patent number: 5436243Abstract: Potentiating agents inhibit the development of multidrug resistance, reduce drug-resistance in drug-resistant tumors, or sensitize tumors to antineoplastic drugs, thereby potentiating the effect of antineoplastic agents. The potentiating agents are aminoanthraquinones, preferably 1,4-bis(N-substituted) amino anthraquinones, and pharmaceutically acceptable salts thereof.Type: GrantFiled: November 17, 1993Date of Patent: July 25, 1995Assignees: Research Triangle Institute Duke University, Pharmaceuticals CorporationInventors: Clifford W. Sachs, Robert L. Fine, Lawrence M Ballas, R. Ivy Carroll, Robert Bell
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Patent number: 5401729Abstract: The invention provides compounds of the formula: ##STR1## wherein R, R.sup.3, R.sup.4 and W are defined in the specification. These compounds are useful as antibiotic agents.Type: GrantFiled: February 24, 1994Date of Patent: March 28, 1995Assignee: American Cyanamid CompanyInventors: Phaik-Eng Sum, Ving J. Lee, Raymond T. Testa
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Patent number: 5380725Abstract: There are disclosed compounds of the formula (I) ##STR1## wherein R.sup.1 is 1-adamantyl, 3-methyl-1-adamantyl, 3-noradamantyl, unsubstituted or substituted-2-indolyl, 3-indolyl, 2-benzofuranyl and 3-benzofuranyl wherein the substituents are selected from lower alkyl, lower alkoxy and halo; R.sup.2 is unsubstituted or substituted phenyl, benzyl, pyridinyl, pyrimidinyl or pyrazinyl, wherein the substituents are selected from lower alkyl, lower alkoxy, trifluoromethyl and halo; R.sup.3 is H or lower alkyl of 1 to 3 carbon atoms; n is the integer 0 or 1; m is the integer from 2 to 5; and the pharmaceutically acceptable salts thereof.Type: GrantFiled: July 14, 1993Date of Patent: January 10, 1995Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, John P. Yardley, Wayne E. Childers, Jr.
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Patent number: 5292726Abstract: Diacylpiperazines of general structure ##STR1## are: angiotensin II (A-II) antagonists selective for the type 2 (AT.sub.2) subtype useful in the treatment of cerebrovascular, cognitive, and CNS disorders; tachykinin receptor antagonists useful in the treatment of inflammatory diseases and pain or migraine; and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.Type: GrantFiled: May 19, 1992Date of Patent: March 8, 1994Assignee: Merck & Co., Inc.Inventors: Wallace T. Ashton, Conrad P. Dorn, William J. Greenlee, Malcolm MacCoss, Sander G. Mills, Mu T. Wu
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Patent number: 5254552Abstract: There are disclosed compounds of the formula (I) ##STR1## wherein R.sup.1 is 1-adamantyl, 3-methyl-1-adamantyl, 3-noradamantyl, unsubstituted or substituted-2-indolyl, 3-indolyl, 2-benzofuranyl and 3-benzofuranyl wherein the substituents are selected from lower alkyl, lower alkoxy and halo; R.sup.2 is unsubstituted or substituted phenyl, benzyl, pyridinyl, pyrimidinyl or pyrazinyl, wherein the substituents are selected from lower alkyl, lower alkoxy, trifluoromethyl and halo; R.sup.3 is H or lower alkyl of 1 to 3 carbon atoms; n is the integer 0 or 1; m is the integer from 2 to 5; and the pharmaceutically acceptable salts thereof.The compounds of this invention which demonstrate selectivity at the 5-HT.sub.1A and 5-HT.sub.2 versus D.sub.2 receptor binding sites are useful as potential anxiolytic-antidepressant agents.Compounds of this invention with equal high affinity for the 5-HT.sub.1A and D.sub.2 -receptor binding sites are useful as mixed antipsychotic-anxiolytic agents.Type: GrantFiled: March 16, 1992Date of Patent: October 19, 1993Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, John P. Yardley, Wayne E. Childers, Jr.
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Patent number: 5216178Abstract: Novel aminoalkylthiodibenzoxepins, physiologically tolerable acid addition salts thereof, a method of preparing same, pharmaceutical and veterinary preparations including same and methods of treating by administering same are disclosed. These compounds are useful as analgesic, antidepressant and anticonvulsant agents. A process for selectively reducing olefins by alkaline earth metals in loweralkanols is also disclosed.Type: GrantFiled: August 15, 1991Date of Patent: June 1, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Helen H. Ong, Vernon B. Anderson, James A. Profitt
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Patent number: 5215992Abstract: Certain ethanobicyclic amine compounds are described for treatment of CNS disorders such as psychotic disorders, convulsions, dystonia and cerebral ischemia. Compounds of particular interest are of the formula ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y and Z is independently selected from hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, phenalkyl, phenyl, alkoxy, phenoxy, phenalkoxy, alkoxyalkyl, halo, haloalkyl and hydroxyalkyl; wherein R.sup.3 and R.sup.4 may be taken together to form oxo;wherein each of R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9 and R.sup.10 is independently selected from hydrido, alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl, cycloalkylalkyl, alkoxyalkyl, phenalkyl and phenyl; wherein G within the nitrogen-containing cyclohetero moiety is selected from ##STR2## wherein R.sup.11 is selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, phenalkyl, alkoxyalkyl and hydroxyalkyl; wherein each of R.sup.12 and R.sup.Type: GrantFiled: December 2, 1991Date of Patent: June 1, 1993Assignee: G. D. Searle & Co.Inventors: Nancy M. Gray, Brian K. Cheng
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Patent number: 5192766Abstract: Compounds of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 is each --R.sup.5, --CH.dbd.CH--R.sup.5 or --C.tbd.C--R.sup.5, wherein R.sup.5 is optionally substituted aryl or aromatic heterocyclic; R.sup.3 is hydrogen, alkyl, cyano or --R.sup.5 ; X is oxygen or sulfur; A is 1,4-piperazin-1,4-diyl or a 1,4-homopiperazin-1,4-diyl; B' is alkylene, carbonyl, thiocarbonyl, sulfinyl or sulfonyl; and R.sup.4 is optionally substituted phenyl and pharmaceutically acceptable salts thereof have valuable PAF antagonist activity, and may be prepared by reacting a compound containing the piperazine or homopiperazine part of the molecular with a compound containing the other part of the molecule.Type: GrantFiled: August 28, 1991Date of Patent: March 9, 1993Assignee: Sankyo Company, LimitedInventors: Norio Nakamura, Nobuyuki Ohkawa, Takeshi Oshima, Masaaki Miyamoto, Yasuteru Iijima
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Patent number: 5143922Abstract: Novel tricyclic compounds having a TXA.sub.2 antagonizing activity represented by formula (I): ##STR1## possess a potent antagonizing action against thromboxane A.sub.2 and also an antiallergic and/or antihistaminic acitvity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.Type: GrantFiled: November 20, 1990Date of Patent: September 1, 1992Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii, Hidee Ishii, Kenji Ohmori
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Patent number: 5141960Abstract: A class of tricyclic glycinamide derivatives is described having use in treatment of CNS dysfunctions such as epilepsy and convulsive disorders. Compounds of most interest are those of the formula ##STR1## wherein each of X and Y is hydrido; wherein Z is selected from methylene, ethylene, ethenylene, thiomethylene and thioethylene; and wherein each of R.sup.1, R.sup.2 and R.sup.3 is hydrido; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: June 25, 1991Date of Patent: August 25, 1992Assignee: G. D. Searle & Co.Inventors: Alexis A. Cordi, Claude L. Gillet
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Patent number: 5112826Abstract: The dihydrodibenzocycloheptyliden-ethylpiperazine derivative has the formula: ##STR1## wherein R represents a substituent selected from the group consisting of --CH.dbd.CH.sub.2 ; --CO.sub.2 C.sub.2 H.sub.5 ; --CH.dbd.CH--CO.sub.2 CH.sub.Type: GrantFiled: April 12, 1989Date of Patent: May 12, 1992Inventors: Xavier D. Cirera, Romeo R. Andreoli, Pedro P. Lloveras, Leonida Bruseghini, Jose P. Irurre
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Patent number: 5098916Abstract: Certain propanobicyclic amine compounds are described for treatment of CNS disorders such as psychotic disorders, convulsions, dystonia and cerebral ischemia. Compounds of particular interest are of the formula ##STR1## wherein each R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y and Z is independently selected from hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, phenalkyl, phenyl, alkoxy, phenoxy, phenalkoxy, alkoxyalkyl, halo, haloalkyl and hydroxyalkyl; wherein R.sup.3 and R.sup.4 may be taken together to form oxo;wherein each of R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13 and R.sup.14 is independently selected from hydrido, alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl, cycloalkylalkyl, alkoxyalkyl, henalkyl and phenyl; wherein G within the nitrogen-containing cyclohetero moiety is selected from ##STR2## wherein R.sup.15 is selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, phenalkyl, alkoxyalkyl and hydroxyalkyl; wherein each of R.sup.16 and R.sup.Type: GrantFiled: March 29, 1990Date of Patent: March 24, 1992Assignee: G. D. Searle & Co.Inventors: Nancy M. Gray, Brian K. Cheng
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Patent number: 5091526Abstract: Biologically active, enantiomerically substantially pure intermediates of trans-hexahydro-benzo[d]naphtho[2,1-b]azepines are prepared.The present invention involves a process for preparing compounds of the general formula 3: ##STR1## wherein: R* is ##STR2## Each R.sup.1 is independently H or alkyl; Q is methylene, --O-- or --S--;m and n are independently variable and may each have a value of 0, 1 or 2, with the provisos that the sum of m and n is not greater than 3, that m may not equal zero when Q is --O-- or --S--, and that when Q is --CH.sub.2 --, m and n cannot both be zero;X is hydrogen, halo, alkyl, alkylthio, alkylsulfinyl, alkylsufonyl, hydroxy, alkoxy or trifluoromethyl;Y is hydrogen, hydroxy, alkoxy, --OC(O)NR.sup.2 R.sup.3, --OC(O)--R.sup.9, --N(R.sup.1).sub.2, --NHC(O)R.sup.1 or --OP(O)(OH)OR.sup.1,R.sup.2 and R.sup.3 are the same or different and each is hydrogen (provided that both are not hydrogen), alkyl, aralkyl, cycloalkyl, aryl, hydroxyalkyl, or alkoxyalkyl;in addition, when one of R.sup.Type: GrantFiled: January 8, 1991Date of Patent: February 25, 1992Assignee: Schering CorporationInventors: Joel G. Berger, John W. Clader
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Patent number: 5030631Abstract: Novel tricyclic arylsulfonamides useful for treating hypertension and bronchoconstiction, as well as to their pharmaceutical compositions and methods for using the same.Type: GrantFiled: November 27, 1989Date of Patent: July 9, 1991Assignee: Schering CorporationInventor: Barr E. Bauer
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Patent number: 5010078Abstract: There are disclosed compounds of the formula (I) ##STR1## wherein R.sup.1 is 1-adamantyl, 3-methyl-1-adamantyl, 3-noradamantyl, unsubstituted or substituted-2-indolyl, 3-indolyl, 2-benzofuranyl and 3-benzofuranyl wherein the substituents are selected from lower alkyl, lower alkoxy and halo; R.sup.2 is unsubstituted or substituted phenyl, benzyl, pyridinyl, pyrimidinyl or pyrazinyl, wherein the substituents are selected from lower alkyl, lower alkoxy, trifluoromethyl and halo; R.sup.3 is H or lower alkyl of 1 to 3 carbon atoms; n is the integer 0 or 1; m is the integer from 2 to 5; and the pharmaceutically acceptable salts thereof.Type: GrantFiled: March 14, 1990Date of Patent: April 23, 1991Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, John P. Yardley, Wayne E. Childers, Jr.
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Patent number: 5001160Abstract: Compounds are disclosed having the formula: ##STR1## in which R.sub.1 is a C.sub.1 l to C.sub.12 alkyl, said alkyl being straight or branched chain, saturated or unsaturated, monosubstituted or unsubstituted, said substituents being selected from piperidine, pyrrolidine, morpholine, thiomorpholine or cycloalkyl of 3 to 7 carbons, a cycloalkyl of 3 to 9 carbons, a lower alkylcycloalkyl of 4 to 9 carbons, or a polycycloalkyl of 2 to 3 rings containing 7 to 12 carbons;R.sub.Type: GrantFiled: June 27, 1989Date of Patent: March 19, 1991Assignee: Marion Laboratories, Inc.Inventors: Daniel W. McPherson, John P. Carter
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Patent number: 4997836Abstract: Novel trisubstituted piperazine compounds of the formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.Type: GrantFiled: November 9, 1989Date of Patent: March 5, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Kohei Nishikawa
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Patent number: 4994463Abstract: Novel tricyclic compounds having a TXA.sub.2 antagonizing activity represented by formula (I): ##STR1## possess a potent antagonizing action against thromboxane A.sub.2 and also an antiallergic and/or antihistaminic activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.Type: GrantFiled: December 8, 1988Date of Patent: February 19, 1991Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii, Hidee Ishii, Kenji Ohmori
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Patent number: 4940709Abstract: Diseases caused by platelet activating factor are prevented and treated by administration to a subject of a therapeutically effective amount of a piperazine compound of the formula: ##STR1## wherein R.sup.1 to R.sup.4 are as defined in the specification.Type: GrantFiled: November 20, 1987Date of Patent: July 10, 1990Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Norihiko Shimazaki, Keiji Hemmi, Osamu Nakaguti, Yoshio Miyazaki, Masashi Hashimoto
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Patent number: 4933344Abstract: Ethanone oximes represented by the following general formula: ##STR1## wherein R.sup.1 represents a cycloalkyl group, aryl group, aralkyl group, aryloxy group, aralkyloxy group, arylthio group or aryl sulfonyl group, those groups being optionally substituted with a substituent selected from an alkyl group having 1 to 3 carbon atoms, an alkoxy group having 1 to 3 carbon atoms and a halogen atom, piperidino group, piperazino group, 4-alkyl substituted piparazino group, imidazolyl group, 4-alkyl substituted imidazolyl group or substituted amino group,R.sup.2 represents a hydrogen atom or an alkoxy group having 1 to 3 carbon atoms, andR.sup.3 represents a piperidino group, piperazino group or 4-alkyl substituted piperazino group, orR.sup.1 and R.sup.2 together with a phenyl group to which they are attached may form a phenothiazin-2-yl group, N-acetyl-phenothiazin-2-yl group, thianthren-2-yl group, dibenzothiophen-3-yl group, dibenzofuran-3-yl group or a group of the formula: ##STR2## wherein R.sup.Type: GrantFiled: August 31, 1988Date of Patent: June 12, 1990Assignee: Mitsubishi Kasei CorporationInventors: Shinichiro Fujimori, Satoshi Yamazaki, Mamoru Sugano, Makoto Kawamura, Kunihiro Ninomiya, Akihiro Tobe, Issei Nitta
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Patent number: 4921958Abstract: The compounds of the formula: ##STR1## wherein Ad is 1-adamantyl, 2-adamantyl or 3-noradamantyl; n is 1,2,3,4 or 5; R.sup.1 hydrogen, alkyl, phenyl, benzyl, or substituted phenyl or benzyl in which the substituent is alkyl, alkoxy, halo, cyano, nitro or trifluoromethyl; R.sup.2 is phenyl, benzyl or substituted phenyl or benzyl in which the substituent is alkyl, alkoxy, halo, nitro, cyano or perhalomethyl, 2-, 3-, or 4-pyridinyl, 2-, 4- or 5-pyrimidinyl or 2- or 3-pyrazinyl; R.sup.3 and R.sup.4 are, independently, hydrogen, methyl, phenyl or benzyl; or a pharmaceutically acceptable salt thereof, are useful anxiolytic/antidepressant agents, with elements of antipsychotic activity.Type: GrantFiled: September 27, 1989Date of Patent: May 1, 1990Assignees: American Home Products Corporation, John Wyeth & Brother LimitedInventors: Magid A. Abou-Gharbia, John P. Yardley, Wayne E. Childers, Jr., Ian A. Cliffe
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Patent number: 4917826Abstract: Provided are cyclic hydrocarbons of Formula I ##STR1## with an aminoalkyl sidechain that are useful for treating phospholipase A2 mediated conditions, diabetes, and obesity.Type: GrantFiled: June 16, 1987Date of Patent: April 17, 1990Assignee: The Upjohn CompanyInventors: Roy A. Johnson, Gordon L. Bundy, Gilbert A. Youngdale, Douglas R. Morton, Donald P. Wallach, deceased
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Patent number: 4912220Abstract: Nitroaryl carbonyl Formula (IIA) compounds, their nitrodihydroaryl carbonyl Formula (I) intermediates, processes for preparing Formula (II) compounds, and a process for preparing Formula (I) compounds, wherein each process comprises the reaction of a nitroaryl compound with a silane.Type: GrantFiled: February 3, 1988Date of Patent: March 27, 1990Assignee: E. I. Du Pont de Nemours and CompanyInventor: Thaliyil V. Rajanbabu
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Patent number: 4898876Abstract: A benzopylpiperazine ester of the following formula: ##STR1## wherein A represents a single bond or an alkylene group, vinylene group, --O--alkylene group or methine group, R.sub.1 represents a bicyclic carbon ring residue which may be substituted with a lower alkyl group, lower alkoxy group, oxo group or nitro group or a halogen atom, or may be partially saturated; a fluorene residue which may contain an oxo group; a fluorenylidene group; an anthracene residue; a phenanthrene residue which may be substituted with a lower alkyl group, or may be partially saturated; a benzofuran residue or thianaphthene residue which may be substituted with a lower alkyl group or lower alkoxy group; a benzopyran residue or benzoazine residue which may be substituted with an oxo group or phenyl group and partially saturated; a phthalimide residue; a benzodiazine residue; an isozazole residue which may be substituted with a lower alkyl group or phenyl group; or an alkylene dioxybenzene residue or xanthene residue; and R.sub.Type: GrantFiled: November 12, 1985Date of Patent: February 6, 1990Assignee: Kowa Co., Ltd.Inventors: Setsuro Fujii, Eizou Hattori, Mitsuteru Hirata, Koichiro Watanabe, Kazuhiro Onogi, Masahiko Nagakura
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Patent number: 4882432Abstract: The compounds of the formula: ##STR1## wherein Ad is 1-adamantyl, 2-adamantyl or 3-noradamantyl; X is --O-- or ##STR2## n is 1,2,3 or 4; R.sup.1 and R.sup.2 are, independently, hydrogen, alkyl, phenyl, benzyl, or substituted phenyl or benzyl in which the substituent is alkyl, alkoxy, halo, cyano, nitro or trifluoromethyl; and R.sup.3 is phenyl, benzyl or substituted phenyl or benzyl in which the substituent is alkyl, alkoxy, halo, nitro, cyano or perhalomethyl, 2-, 3-, or 4-pyridinyl, 2-, 4-or 5-pyrimidiny; or 2- or 3-pyrazinyl; R.sup.4 and R.sup.5 are independently, hydrogen, methyl, phenyl or benzyl; or a pharmaceutically acceptable salt thereof, are useful anxiolytic/antidepressant agents, with elements of antipsychotic activity.Type: GrantFiled: January 9, 1989Date of Patent: November 21, 1989Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, John P. Yardley, Wayne E. Childers, Jr.
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Patent number: 4876345Abstract: The invention provides an indene compound represented by the following general formula (I): ##STR1## wherein R.sub.1 means a lower alkyl group, R.sub.2 and R.sub.3 denote a lower alkyl group individually or an alkylenedioxy group in combination, and R.sub.4 and R.sub.5 mean individually a substituted or unsubstituted lower alkyl or aryl group or in combination a substituted or unsubstituted piperidino, piperazinyl or homopiperazinyl group together with the adjacent nitrogen atom, with a proviso that not both R.sub.4 and R.sub.5 are a methyl group at the same time.Type: GrantFiled: June 6, 1988Date of Patent: October 24, 1989Assignee: Taiyo Pharmaceutical Industry Co., Ltd.Inventors: Shozo Nakaoku, Kazuhiko Sakuma, Yasuhiro Oshika, Kazuo Ohira
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Patent number: 4871740Abstract: A glycyrrhetic acid derivative of the formula ##STR1## wherein X and Y are hydrogen atom, respectively or X is oxygen atom together with Y, A.sub.1 is methylene or carbonyl radical, A.sub.2 is hydrogen atom, cyano, carbamoyl, carboxyl radical or alkoxycarbonyl group, m and n are an integer, respectively, R.sub.1 is a radical of ##STR2## in which R.sub.2 is an alkyl, alkenyl group, phenyl radical or a substituted phenyl radical, A.sub.3 is S, O or NH, and l is an integer, a process for the preparation of the derivatives, and use of the derivative as a pharmaceutical agent.Type: GrantFiled: November 24, 1987Date of Patent: October 3, 1989Assignee: Sanwa Kagaku Kenkyusho Co., Ltd.Inventors: Masayasu Kurono, Ryoichi Unno, Hiromoto Kimura, Mitsuru Oka, Keiko Hasegawa, Shinichi Ikeda, Noboru Kuboyama, Takashi Ito, Kiichi Sawai, Shunshuke Ito
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Patent number: 4863522Abstract: A composition comprising(a) a dianthraquinonyl pigment of formula I ##STR1## (b) a compound of formula II ##STR2## wherein X.sup..sym. is H.sup..sym. or a group of formula M.sup.n.sym. /n or N.sup..sym. (R)(R.sub.1)(R.sub.2)(R.sub.3), M.sup.n.sym. is a monovalent metal cation of valency n, n is 1, 2 or 3, each of R, R.sub.1, R.sub.2 and R.sub.3 independently is hydrogen, C.sub.1 -C.sub.18 alkyl, C.sub.5 -C.sub.6 cycloalkyl, phenyl or phenyl which is substituted by C.sub.1 -C.sub.18 alkyl, or R.sub.2 and R.sub.3, together with the linking nitrogen atom, are a pyrrolidine, imidazolidine, piperidine, piperazine or morpholine radical, or R.sub.1, R.sub.2 and R.sub.3, together with the linking nitrogen atom, are a pyrrole, pyridine, picoline, pyrazine, quinoline or isoquinoline radical, r and t are each independently of the other 0 or 1, with the proviso that at least one of r and t must be 1.Type: GrantFiled: December 22, 1987Date of Patent: September 5, 1989Assignee: Ciba-Geigy CorporationInventors: Max Jost, Edward E. Jaffe, Philippe Bugnon
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Patent number: 4857644Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, lower alkyl or phenyl; or R.sup.1 and R.sup.2 taken together represent --(CH.sub.2).sub.4 --or ##STR2## where the dotted line represents an optional double bond; R.sup.3 is hydrogen, lower alkyl, lower alkoxy or halo;R.sup.4 is pyridinyl, pyrimidinyl, pyrazinyl, benzyl, phenyl or phenyl substituted by lower alkyl, lower alkoxy, or halo;Z is --SO.sub.2 --or ##STR3## where R.sup.5 is hydrogen or lower alkyl; m is 0-4;n is 0-2; andthe pharmaceutically acceptable salts thereof, and their use as anti-inflammatory agents.Type: GrantFiled: June 9, 1988Date of Patent: August 15, 1989Assignee: American Home Products CorporationInventor: Magid A. Abou-Gharbia
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Patent number: 4835156Abstract: A dihydrodibenzocycloheptyliden-ethyl-piperazine derivative of the general formula: ##STR1## in which, R=--CH.dbd.CH.sub.2 ; --CH.sub.2 OH; --COOH; --CO.sub.2 C.sub.2 H.sub.5 ; --CH.dbd.CH--CO.sub.2 CH.sub.3 ; --CH.dbd.CH--CO.sub.2 CH.sub.3, --C.sub.6 H.sub.5, ##STR2## or pharmaceutically acceptable salts thereof, are disclosed. The compounds of the invention are useful in pharmaceutical compositions for the treatment of pathologies responsive to vasodilatory agents.Type: GrantFiled: May 26, 1987Date of Patent: May 30, 1989Assignee: Sociedad Espanola De Especialidades Terepeuticas, S.A.Inventors: Xavier D. Cirera, Romeo R. Andreoli, Pedro P. Lloveras, Leonida Bruseghini, Jose P. Irrure
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Patent number: 4826996Abstract: The invention concerns 1,8-dihydroxy-9-anthrones substituted in the 10-position of the formula: ##STR1## in which R.sub.1 represents a group taken from the set constituted by: ##STR2## wherein R.sub.2 represents H, C.sub.1-8 alkyl, C.sub.1-3 mono- or poly-hydroxyalkyl, carbamoyl or phenyl,R.sub.3, R.sub.4, and R.sub.5 represent H, C.sub.1-8 alkyl, C.sub.3-8 mono- or poly-hydroxyalkyl, possibly interrupted by an oxygen, C.sub.3-6 cycloalkyl, or R.sub.3 and R.sub.4 form a divalent group: --(CH.sub.2).sub.(4 or 5) --, --(CH.sub.2).sub.2 --O--(CH.sub.2).sub.2 --, or --(CH.sub.2).sub.2 --N(R.sub.8)--(CH.sub.2).sub.2 --, R.sub.8 being H, --CH.sub.3, or --CH.sub.2 CH.sub.2 OH,R.sub.6 represents --CO.sub.2 R.sub.5, --CN, CHO, --CONH.sub.2, or --CONH--CH.sub.2 OH,and R.sub.7 and R'.sub.7 are H or --CH.sub.3, and their optical isomers.Utilization of the compounds (I) in human or veterinary medicine, in particular in the treatment of psoriasis and of warts, in cosmetics.Type: GrantFiled: December 9, 1985Date of Patent: May 2, 1989Assignee: Groupement d'Interet Economique dit Centre International De Recherches Dermatologioues C.I.R.D.Inventors: Braham Shroot, Jean Maignan, Gerard Lang
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Patent number: 4792551Abstract: Compounds useful for treating inflammation, pain and swelling, represented by the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein: Y and Z are each independently halo, alkyl or alkoxy;l and m are each independently integers of 0-4;b is an integer of 2-12; andX is selected from the group consisting of:--NR.sup.1 R.sup.2, --NR.sup.1 (CH.sub.2 CH.sub.2 OH), ##STR2## in which R.sup.1 and R.sup.2 are independently H, alkyl or cycloalkyl;R.sup.3 is H, alkyl or CH.sub.2 CH.sub.2 OH; andn is an integer of 3-7.Type: GrantFiled: July 15, 1983Date of Patent: December 20, 1988Assignee: Syntex (U.S.A.) Inc.Inventors: Peter H. Nelson, Stefan H. Unger, Thomas R. Thieme
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Patent number: 4786721Abstract: The reactive dyes are useful, in particular, for dyeing or printing cellulose-containing fiber materials by the cold pad-batch method and produce, with a high dyeing yield, dyeings and prints having good fastness properties.Type: GrantFiled: August 13, 1986Date of Patent: November 22, 1988Assignee: Ciba-Geigy CorporationInventors: Athanassios Tzikas, Peter Aeschlimann, Paul Herzig
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Patent number: 4749703Abstract: Compounds of the formula: ##STR1## wherein A means an alkylene; Y--Z means ##STR2## --CH.dbd.CH--, --CH.sub.2 CH.sub.2 --, or ##STR3## R.sub.1 and R.sub.2 are each a substituent; R.sub.3 is hydrogen atom, alkyl, or alkoxy; R.sub.4 is phenyl, phenylalkyl, phenylalkenyl, diphenylmethyl, naphthyl, thiazolyl, optionally substituted pyridyl, optionally substituted pyrimidinyl, quinolyl, benzoylalkyl, benzoyl, furoyl, thenoyl, phenyloxycarbonyl, phenyloxysulfonyl, or phenylsulfonyl; a is 2 or 3, b and c are each 1 or 2, and d is an integer of 0 to 2, provided that the phenyl, phenyl moiety and naphthyl may optionally be substituted, and a pharmaceutically acceptable salt thereof, process for the preparation thereof, and pharmaceutical composition containing the same. The compounds and salt thereof show potent calcium antagonistic activity and are useful for prophylaxis and treatment of hypertension and/or ischemic heart disease.Type: GrantFiled: April 10, 1986Date of Patent: June 7, 1988Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Hitoshi Uno, Mikio Kurokawa, Fuminori Sato, Naonobu Hatano
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Patent number: 4743690Abstract: Nitroaryl carbonyl Formula (IIA) compounds, their nitrodihydroaryl carbonyl Formula (I) intermediates, processes for preparing Formula (II) compounds, and a process for preparing Formula (I) compounds, wherein each process comprises the reaction of a nitroaryl compound with a silane.Type: GrantFiled: January 16, 1987Date of Patent: May 10, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventor: Thaliyil V. Rajanbabu
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Patent number: 4683330Abstract: A compound of the formula ##STR1## and intermediates useful in preparing same.Type: GrantFiled: January 11, 1985Date of Patent: July 28, 1987Assignee: The Upjohn CompanyInventor: Paul A. Aristoff
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Patent number: 4668814Abstract: A compound of the formula ##STR1## and intermediates useful in preparing same.Type: GrantFiled: January 11, 1985Date of Patent: May 26, 1987Assignee: The Upjohn CompanyInventor: Paul A. Aristoff
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Patent number: 4659862Abstract: Nitroaryl carbonyl Formula (IIA) compounds, their nitrodihydroaryl carbonyl Formula (I) intermediates, processes for preparing Formula (II) compounds, and a process for preparing Formula (I) compounds, wherein each process comprises the reaction of a nitroaryl compound with a silane.Type: GrantFiled: May 3, 1984Date of Patent: April 21, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventor: Thaliyil V. Rajanbabu
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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: 4652649Abstract: A new class of anti-spasmodic compounds having two branch chains is provided. The compounds have the general formula: ##STR1## wherein the substituents are defined hereinbelow.Type: GrantFiled: February 20, 1985Date of Patent: March 24, 1987Assignee: United Pharmaceuticals, Inc.Inventor: William M. Davis
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Patent number: 4647562Abstract: A new class of anti-spasmodic compounds having three branch chains is provided. These compounds have the general formula: ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are saturated straight chain or branched alkyl groups contained from 1 to 8 carbon atoms, and are separated or linked to one another to form an aliphatic ring system. k is an integer from 0 to 5, and the total number of carbon atoms in R.sub.1 plus R.sub.2 plus R.sub.3 plus k are equal to or less than 12. Furthermore, l is an integer from 1 to 3, m is an integer from 1 to 3, n is an integer from 1 to 3, and X may be nonexistent or may be O, S, NH or CH.sub.2 or salts thereof. However, when X is nonexistent the terminal group in both the m chain and the n chain is a methyl group.Type: GrantFiled: February 20, 1985Date of Patent: March 3, 1987Assignee: United Pharmaceuticals, Inc.Inventor: William M. Davis
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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