The Additional Six-membered Hetero Ring Is One Of The Cyclos In A Tricyclo Ring System Patents (Class 544/126)
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Patent number: 4767762Abstract: This invention relates to novel isoxazolo-naphthyridine, isoxazolo-quinoline, isothiazolo-naphthyridine, and isothiazolo-quinoline, derivatives having antibacterial properties.Type: GrantFiled: December 11, 1986Date of Patent: August 30, 1988Assignee: Abbott LaboratoriesInventor: Daniel T. Chu
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Patent number: 4757070Abstract: Compounds of formula I ##STR1## wherein n is 0 or 1,R.sup.1 is hydrogen or lower alkyl,R.sup.2 and R.sup.3 each independently is hydrogen, optionally substituted lower alkyl, acyl or aryl, or together with the nitrogen atom form a 5-6-member heterocycle,R.sup.4 is hydrogen, lower alkyl or lower alkoxyalkyl andX is COOR.sup.6, CO--NR.sup.7 R.sup.8, or an oxadiazolyl radical of the formula ##STR2## wherein R.sup.5 is H, lower alkyl or cycloalkyl,R.sup.6 is H or lower alkyl,R.sup.7 and R.sup.8 each independently is hydrogen, optionally substituted lower alkyl, acyl or aryl, orR.sup.7 and R.sup.8 together with the nitrogen atom can form a 5-6-member heterocycle,are valuable drugs, e.g., have psychotropic activity.Type: GrantFiled: December 8, 1987Date of Patent: July 12, 1988Assignee: Schering AktiengesellschaftInventors: Helmut Biere, Andreas Huth, Dieter Rahtz, Ralph Schmiechen, Dieter Seidelmann, David N. Stephens
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Patent number: 4751305Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 is pyridl, quinolinyl, pyrazinyl, pyridinyl, pyridazinyl, pyrimidinyl, quinoxalinyl, quinazolinyl or any of the foregoing substituted with halo, lower alkyl, lower alkyl carbonyl, benzoyl, carboxy, lower alkoxycarbonyl, OR.sup.2, N(R.sup.2).sub.2, CON(R.sup.2).sub.2, SO.sub.3 R.sup.2, SO.sub.2 N(R.sup.2).sub.2, phenylsulfonyl, lower alkylsulfonyl, cyano, nitro or trifluoromethyl;R.sup.2 is hydrogen, lower alkyl or phenyl;R.sup.3 is halo, morpholino, 4-methylpiperazino, R.sup.4 NNHR.sup.5, NR.sup.4 R.sup.5, OR.sup.5, SR.sup.5, R.sup.4 NCH.sub.2 CH.sub.2 OCH.sub.3, SCH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2, or ##STR2## R.sup.4 is hydrogen or lower alkyl; R.sup.5 is hydrogen, lower alkyl, lower alkanoyl, lower cycloalkylor phenyl; andR.sup.6 and R.sup.Type: GrantFiled: May 7, 1987Date of Patent: June 14, 1988Assignee: American Home Products CorporationInventors: Jerauld S. Skotnicki, Steven C. Gillman
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Patent number: 4745115Abstract: Compounds of the general formula I ##STR1## in which: R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl or together are a group X which is C.sub.3-6 polymethylene optionally in which one carbon atom is replaced by O, S or NR.sub.6 wherein R.sub.6 is hydrogen or C.sub.1-6 alkyl;R.sub.3 is a mono- or fused bi-cyclic heteroaromatic group having up to ten atoms in the aromatic ring(s), not more than four of which are selected from nitrogen, oxygen or sulphur, optionally C-substituted by one or more substituents selected from halogen, CF.sub.3, nitro, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.2-7 alkanoyl or cyano; or is phenyl or naphthyl, optionally substituted by one or more substituents selected from halogen, CF.sub.3, nitro, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.2-7 alkanoyl, carboxyl, C.sub.1-6 alkoxycarbonyl, cyano, CONR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are selected from hydrogen or C.sub.1-6 alkyl or together are a group X; NR.sub.9 R.sub.Type: GrantFiled: October 18, 1985Date of Patent: May 17, 1988Assignee: Beecham Group p.l.c.Inventors: Roger E. Markwell, Stephen A. Smith, David J. Hunter
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Patent number: 4735940Abstract: Compounds of the formula ##STR1## or a pharmaceutically acceptable acid addition salt of a compound of formula I which has one or more basic substituents, are described.The compounds of formula I possess pronounced muscle relaxant, sedative-hypnotic, anticonvulsive and anxiolytic properties and have low toxicity.Type: GrantFiled: October 31, 1985Date of Patent: April 5, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Ulf Fischer, Fernand Schneider, Ulrich Widmer
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Patent number: 4731365Abstract: Compounds of formula I ##STR1## wherein n is 0 or 1,R.sup.1 is hydrogen or lower alkyl,R.sup.2 and R.sup.3 each independently is hydrogen, optionally substituted lower alkyl, acyl or aryl, or together with the nitrogen atom form a 5-6-member heterocycle,R.sup.4 is hydrogen, lower alkyl or lower alkoxyalkyl andX is COOR.sup.6, CO--NR.sup.7 R.sup.8, or an oxadiazolyl radical of the formula ##STR2## wherein R.sup.5 is H, lower alkyl or cycloalkyl,R.sup.6 is H or lower alkyl,R.sup.7 and R.sup.8 each independently is hydrogen, optionally substituted lower alkyl, acyl or aryl, orR.sup.7 and R.sup.8 together with the nitrogen atom can form a 5-6-member heterocycle,are valuable drugs, e.g., have psychotropic activity.Type: GrantFiled: December 22, 1986Date of Patent: March 15, 1988Assignee: Schering AktiengesellschaftInventors: Helmut Biere, Andreas Huth, Dieter Rahtz, Ralph Schmiechen, Dieter Seidelmann, David N. Stephens
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Patent number: 4719210Abstract: Compounds of formula I ##STR1## wherein R.sup.1 is hydrogen or a protecting group,R.sup.2 is --CH.dbd.CR.sub.2.sup.4 or --C.tbd.CR.sup.4,R.sup.4 is hydrogen or halogen,R.sup.3 is hydrogen, lower alkyl or lower alkoxyalkyl,R.sup.A is, inter alia, hydrogen, OR.sup.7, lower alkyl, which optionally is substituted with aryl, lower alkoxy or NR5R6,R.sup.5 and R.sup.6 can be the same or different and in each case is hydrogen, lower alkyl or together with the nitrogen atom a 5-6 member ring, which can contain another heteroatom,R.sup.7 is lower alkyl, optionally substituted aryl or aralkyl, andeach compound can contain one or more R.sup.A radicals which are not hydrogen, have valuable pharmacological properties.Type: GrantFiled: October 6, 1986Date of Patent: January 12, 1988Assignee: Schering AktiengesellschaftInventors: Dieter Seidelmann, Andreas Huth, Ralph Schmiechen, Rudolf Wiechert, Herbert Schneider, David N. Stephens
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Patent number: 4719211Abstract: This invention concerns tetrahydropyridoindoles of the formula: ##STR1## wherein Q represents ##STR2## in which R.sub.3 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, or --COO(C.sub.1-2) alkyl, and n is an integer from 1 to 7; R.sub.1 is hydrogen, halogen, hydroxy, or C.sub.1-3 alkyl; and R.sub.2 is hydrogen, C.sub.1-4 alkyl or --(CH.sub.2).sub.m --A where A is --N(CH.sub.3).sub.2,--N(C.sub.2 H.sub.5).sub.2, ##STR3## in which Ar is 2-pyrimidinyl, 2-pyrazinyl, phenyl, or phenyl substituted by a methyl, ethyl, methoxy, ethoxy, or trifluoromethyl group; and m is an integer from 1-4, or physiologically acceptable salts thereof, providing however that when n is 1, Q may not be quinolinyl. These compounds exhibit antihypertensive properties. Four of the disclosed compounds also exhibit antipsychotic properties.Also disclosed are compounds of Formula XX in which Q of Formula I is replaced by Q.sub.1, wherein Q.sub.1 is 2- or 3-pyridinyl, and R.sub.2 of Formula I is restricted to hydrogen.Type: GrantFiled: March 7, 1986Date of Patent: January 12, 1988Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, Meier E. Freed
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Patent number: 4716168Abstract: The present invention involves compounds of the class of imidazo[4,5-f]quinolines and methods for enhancing the immune response system of mammals which comprises systemically administering to mammals having a depressed immune function an effective but nontoxic amount of a composition comprising such a compound.Type: GrantFiled: April 29, 1986Date of Patent: December 29, 1987Assignee: Norwich Eaton Pharmaceuticals, Inc.Inventors: Robert J. Alaimo, Jon A. Andersen
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Patent number: 4711889Abstract: The invention relates to acridanone derivatives of the formula ##STR1## wherein the dotted line is an optional bond, R.sup.1 is hydrogen, halogen or nitro,R.sup.2 is hydrogen or lower alkyl,one of R.sup.3 and R.sup.4 is hydrogen or lower alkyl and the other together with R is an additional bond,A is lower alkylene,R.sup.5 is a 5-membered nitrogen-containing, optionally lower alkyl-substituted aromatic heterocycle, amino or the group ##STR2## the symbol is a 5- or 6-membered, optionally lower alkyl-substituted saturated heterocycle which can contain as a ring member oxygen or sulfur or the group >NH or >N(B).sub.n --A.sup.1 --R.sup.6, B is the group --CO--, --COO-- or --SO.sub.2 --, n is the number 0 or 1, A.sup.1 is lower alkylene, R.sup.6 is hydrogen, amino, lower alkylamino or di(lower alkyl)amino and R.sup.7 is hydrogen or lower alkyl, and pharmaceutically acceptable acid addition salts thereof, their preparation and pharmaceutical compositions based thereon.Type: GrantFiled: July 18, 1986Date of Patent: December 8, 1987Assignee: Hoffman-La Roche Inc.Inventors: Urs Brombacher, Helmut Link, Marc Montavon
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Patent number: 4705856Abstract: .beta.-carbolines of formula I ##STR1## can be prepared by reacting an indole of formula II: ##STR2## with an azabutadiene of formula III ##STR3## in the presence of an acid at 50.degree.-200.degree. C.Type: GrantFiled: October 28, 1983Date of Patent: November 10, 1987Assignee: Schering AktiengesellschaftInventor: Helmut Biere
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Patent number: 4704459Abstract: This invention relates to a process for industrially producing a 1-substituted aryl-1,4-dihydro-4-oxonaphthyridine derivative and a salt thereof which are useful as an antibacterial agent, and also to intermediates therefor and processes for producing the intermediates.Type: GrantFiled: January 17, 1986Date of Patent: November 3, 1987Assignee: Toyama Chemical Co., Ltd.Inventors: Yozo Todo, Tetsuo Yamafuji, Katsuyuki Nagumo, Isao Kitayama, Hideyoshi Nagaki, Mikako Miyajima, Yoshinori Konishi, Hirokazu Narita, Shuntaro Takano, Isamu Saikawa
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Patent number: 4701459Abstract: Novel series of 2,3-dihydro-2-oxo-1H-imidazo[4,5-b]quinolinyl amine derivatives of Formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl; R.sub.2 is hydrogen, lower alkyl, lower alkoxy, halogen; R.sub.3 is hydrogen, lower alkyl; R.sub.4 is hydrogen, lower alkyl, alkanoyl, phenylalkanoyl wherein phenyl is optionally substituted with halogen, lower alkyl, lower alkoxy; R.sub.3 and R.sub.4 are joined together to form morpholinyl, piperidinyl or pyrrolidinyl optionally substituted with --CO.sub.2 R.sub.5 or ##STR2## wherein R.sub.5 is hydrogen or lower alkyl, and R.sub.6 is hydrogen, lower alkyl, cycloalkyl; 4-R.sub.7 -piperazinyl wherein R.sub.7 is --CO.sub.2 R.sub.8 wherein R.sub.8 is lower alkyl, phenyl optionally substituted with up to 2 halogen, lower alkyl or lower alkoxy; phenylalkanoyl of 7 to 10 carbon wherein phenyl is unsubstituted or independently substituted with up to 2 halogen, lower alkyl, lower alkoxy.Type: GrantFiled: July 8, 1986Date of Patent: October 20, 1987Assignee: Bristol-Myers CompanyInventors: Nicholas A. Meanwell, John J. Wright
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Patent number: 4698348Abstract: 1H-imidazo[4,5-c]quinoline which are bronchodilators. Pharmacological methods of using the compounds as bronchodilators, pharmaceutical compositions containing the compounds, and synthetic intermediate for preparing the compounds are also described.Type: GrantFiled: November 15, 1985Date of Patent: October 6, 1987Assignee: Riker Laboratories, Inc.Inventor: John F. Gerster
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Patent number: 4690928Abstract: Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective .alpha..sub.6 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives, antidiabetics, antiobesity and platelet aggregation inhibitors.Type: GrantFiled: July 14, 1986Date of Patent: September 1, 1987Assignee: Merck & Co., Inc.Inventors: Joel R. Huff, Joseph P. Vacca, John J. Baldwin
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Patent number: 4686227Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is lower alkyl,R.sup.3 is hydrogen, halogen or ar(lower)alkoxy, andR is lower alkanoyl, nitroso, amino, carboxy, esterified carboxy, carbamoyl, hydroxycarbamoyl, haloformyl, aminomethyleneamino which may be substituted with cyano or lower alkyl, iminomethylamino which may be substituted with cyano or lower alkyl, or a group of the formula: --A--R.sup.2 in whichA is lower alkylene andR.sup.2 is di(lower)alkylamino, cyano, lower alkoxy, N-containing heterocyclic group which may have suitable substituent(s), lower alkynyloxy, lower alkenyloxy, lower alkylthio, amino(lower)alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, carboxy, esterified carboxy, carbamoyl, hydroxycarbamoyl, hydroxy, lower alkanoyloxy, heterocyclicamino (lower)alkylthio having two oxo groups, hydrogen or a group of the formula: ##STR2## in which R.sup.4, R.sup.5 and R.sup.6 are each lower alkyl andX is an acid residue,and pharmaceutically acceptable salts thereof.Type: GrantFiled: June 17, 1985Date of Patent: August 11, 1987Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Ikuo Ueda, Youichi Shiokawa, Masayuki Kato, Nobukiyo Konishi, Atsushi Akahane
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Patent number: 4675323Abstract: Compounds which are imidazo[1,2-a]quinoline derivatives of general formula (I) ##STR1## in which X is hydrogen, halogen, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, (C.sub.1-4) alkylthio, methylsulphonyl, amino, (C.sub.1-4)alkylamino, di-(C.sub.1-4)alkylamino, nitro or trifluoromethyl, Y is hydrogen, halogen or methyl in position 6, 7 or 8, R.sub.1 and R.sub.2, which may be the same or different, are hydrogen or (C.sub.1-6) alkyl, or R.sub.1 and R.sub.2 together form a tetramethylene, pentamethylene, 3-methyl-3-azapentamethylene, 3-ethoxycarbonyl-3-azapentamethylene group, and A and B both are hydrogen or together form a carbon-carbon bond, and their pharmacologically acceptable acid addition salts have anxiolytic, sleep-inducing, hypnotic, anticonvulsant, analgesic and anti-ulcer properties.Type: GrantFiled: February 7, 1986Date of Patent: June 23, 1987Assignee: SynthelaboInventors: Pascal George, Danielle De Peretti
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Patent number: 4666910Abstract: Compounds of the formula ##STR1## wherein one of R.sub.1 and R.sub.2 is hydrogen, halogen, methyl, methoxy, amino or nitro and the other is hydrogen; orR.sub.1 and R.sub.2 are both halogen;R.sub.3 is hydrogen, halogen or methyl;R.sub.4 and R.sub.5 are each independently hydrogen or alkyl or 1 to 2 carbon atoms; orR.sub.4 and R.sub.5, together with each other and the nitrogen atom to which they are attached, are pyrrolidino or morpholino; andX is --O--, --NH--, or --S--;and non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful anti-depressants.Type: GrantFiled: August 28, 1984Date of Patent: May 19, 1987Assignee: Boehringer Ingelheim KGInventors: Claus Schneider, Gerhard Walther, Karl-Heinz Weber, Wolf D. Bechtel, Karin Boke-Kuhn
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Patent number: 4666917Abstract: This invention concerns novel substituted acridine compounds which are useful as modulators of the immune system in warm-blooded animals.Type: GrantFiled: November 9, 1984Date of Patent: May 19, 1987Assignee: American Cyanamid CompanyInventors: Raymond G. Wilkinson, Yang-I Lin
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Patent number: 4656268Abstract: There are described novel cationic quinophthalone compounds of the formula I ##STR1## wherein the symbols have the meanings defined in claim 1, and also processes for producing them. These novel quinophthalone compounds can be used in particular as dyes for dyeing and printing paper, greenish-yellow dyeings having good fastness to water and to light being obtained.Type: GrantFiled: October 18, 1985Date of Patent: April 7, 1987Assignee: Ciba-Geigy CorporationInventor: Jean-Marie Adam
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Patent number: 4642310Abstract: Tetrahydrothienopyridines of the formula ##STR1## in which R is optionally substituted aryl or heterocyclyl,R.sup.1 is an organic radical, andR.sup.2, R.sup.3 and R.sup.4 each independently is hydrogen or an organic radical, or pharmaceutically acceptable salts thereof, which are coronary active, hypotensive, anti-diabetic and salt balance restoring.Type: GrantFiled: March 28, 1985Date of Patent: February 10, 1987Assignee: Bayer AktiengesellschaftInventors: Siegfried Goldmann, Matthias Schramm, Gunter Thomas, Rainer Gross
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Patent number: 4624954Abstract: Herein is disclosed 6,7,8,9-tetrahydro-10-methylpyrido[1,2-a]indol-9-amines and derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions. The derivatives are chemically novel agents with cerebroactive and cognition activating properties.Type: GrantFiled: December 20, 1985Date of Patent: November 25, 1986Assignee: American Home Products CorporationInventors: Ivo Jirkovsky, Gary King, Reinhardt Baudy, Victor DeNoble
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Patent number: 4623380Abstract: Compounds of the formula ##STR1## in which A denotes C-R.sup.4 or N; X denotes alkyl and Y denotes alkyl, cycloalkyl, alkenyl, alkynyl, phenyl or benzoyl, or, together with X, cycloalkyl; R.sup.1 -R.sup.4 denote H, alkyl, alkoxy, alkoxycarbonyl, halogen, NO.sub.2, CN, phenoxy or (substituted) phenyl; R.sup.5 denotes H or alkyl; and R.sup.6 denotes H, (substituted) alkyl, halogenoalkenyl, cycloalk(en)yl, alkynyl, (substituted) phenyl or carboxylic acid ester, carboxylic acid amide, sulfo-ester or acyl radicals, are effective plant treatment agents, in particular herbicides.Type: GrantFiled: February 1, 1985Date of Patent: November 18, 1986Assignee: Hoechst AktiengesellschaftInventors: Roland Schmierer, Reinhard Handte, Hilmar Mildenberger, Klaus Bauer, Hermann Bieringer, Helmut Burstell
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Patent number: 4614820Abstract: Chemical compounds are provided that are novel 3,6-disubstituted-1,8-naphthalimides (I), as well as methods for their production, pharmaceutical compositions comprising the compounds, and methods of treatment using the compounds in dosage form. Compounds of the invention have pharmacological properties and are useful antimicrobial agents and antitumor agents. ##STR1## .Type: GrantFiled: February 13, 1986Date of Patent: September 30, 1986Assignee: Warner-Lambert Co.Inventors: Robert K. Zee-Cheng, Chia C. Cheng
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Patent number: 4600715Abstract: .beta.-carboline derivatives of general Formula I ##STR1## wherein R.sup.3 is ##STR2## wherein R.sup.5 is C.sub.1-5 alkyl, R.sup.6 is lower alkyl, aralkyl, or alkoxyalkyl of up to 7 carbon atoms, and R.sup.7 and R.sup.8 are hydrogen C.sub.1-5 alkyl, or, collectively with the amido nitrogen atom, piperidino,R.sup.4 is hydrogen, C.sub.1-3 alkyl, or CH.sub.2 OR.sup.9 wherein R.sup.9 is C.sub.1-3 alkyl, atoms, andR.sup.A is --COOR.sup.10 ##STR3## wherein R.sup.10 is hydrogen, lower alkyl, alkoxyalkyl or alkenyl of up to 5 carbon atoms, or benzyl, or X is oxygen or sulfur, and R.sup.11 and R.sup.12 each are hydrogen, lower alkyl or alkenyl or, collectively with the amido nitrogen atom, represent a hetero ring, are prepared by conventional methods and exhibit, inter alia, an effect on the central nervous system and are suitable for use as psychopharmaceuticals.Type: GrantFiled: June 22, 1984Date of Patent: July 15, 1986Assignee: Shering AktiengesellschaftInventors: Andreas Huth, Ralph Schmiechen, Dieter Seidelmann, Dieter Rahtz, Mogens Engelstoft, Claus T. Braestrup
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Patent number: 4599409Abstract: The present invention relates to new bisamidine derivatives of polycyclic compounds such as 5,10-dioxo-4,5,9,10-tetrahydro-4,9-dioxapyrene-6(5H)-phenanthridone and 5,10-dioxo-4,5,9,10-tetrahydro-4,9-dioxapyrenephenanthridine and to a process for their preparation. The polycyclic bisamidines according to the invention are distinguished by valuable chemotherapeutic properties, such as, for example, an action against amoebas and trichomonads.Type: GrantFiled: February 15, 1984Date of Patent: July 8, 1986Assignee: Hoechst AktiengesellschaftInventors: Balbir S. Bajwa, deceased, Dipak K. Chatterjee, Bimal N. Ganguli, Jurgen Reden, Noel J. de Souza
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Patent number: 4596809Abstract: Substituted 1,8-naphthyridinones are anti-allergic, anti-inflammatory and cytoprotective agents. Methods for their preparation and use are disclosed.Type: GrantFiled: March 25, 1985Date of Patent: June 24, 1986Assignee: Schering CorporationInventor: Margaret H. Sherlock
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Patent number: 4575508Abstract: 2-Substituted 1-(3'-aminoalkyl)-1,2,3,4-tetrahydro-.beta.-carbolines of the formula ##STR1## where n, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the meanings given in the description, and their preparation and use.The novel substances are useful for treating arrhythmia.Type: GrantFiled: August 5, 1983Date of Patent: March 11, 1986Assignee: BASF AktiengesellschaftInventors: Gerd Steiner, Claus D. Mueller, Dieter Lenke
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Patent number: 4565818Abstract: A 6- and/or 7-oxy-trans-1,2,3,4,4a,5,10,10a-octahydro-benzo[g]quinoline in which the 3-position is substituted by an optionally amidated carboxy group, an optionally etherified hydroxymethyl group, a cyanomethyl group, an alkyl- or aryl-thiomethyl group or a sulfamoylamino or carbamoylamino group, or a physiologically-hydrolysable and -acceptable ester thereof. The subject compounds are useful as pharmaceuticals, in particular as prolactin secretion inhibitors, dopaminergic agents ad dopamine receptor stimulating agents.Type: GrantFiled: October 14, 1982Date of Patent: January 21, 1986Assignee: Sandoz Ltd.Inventors: Rene Nordmann, Trevor J. Petcher
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Patent number: 4564613Abstract: Pyridoindoles of the formula ##STR1## in which R.sub.1 represents hydrogen or C.sub.1 -C.sub.4 -alkyl, which is optionally substituted by the radical ##STR2## R.sub.2 and R.sub.3 represent H or form a bond, or R.sub.1 and R.sub.2 together represent O, --O--CH.sub.2 --CH.sub.2 --O-- or --S--CH.sub.2 --CH.sub.2 --S--,R.sub.4 represents H or the ##STR3## or R.sub.3 and R.sub.4 represent O, orR.sub.1 and R.sub.4 are members of an N-containing six-membered ring andR.sub.8 and R.sub.9 represent H or C.sub.1 -C.sub.4 -alkyl, or optionally form, with the N atom, a heterocyclic 5-membered or 6-membered ring, which can optionally also contain a further hetero-atom from the series comprising N, O or S,R.sub.5 represents H, C.sub.1 -C.sub.4 -alkyl or the group ##STR4## or R.sub.5 and R.sub.3 form a bond, andR.sub.10 and R.sub.11 represent C.sub.1 -C.sub.4 -alkyl or are members of an N-containing 5-membered or 6-membered ring,R.sub.6 represents H or C.sub.1 -C.sub.4 -alkyl andR.sub.Type: GrantFiled: September 14, 1984Date of Patent: January 14, 1986Assignee: Troponwerke GmbH & Co.Inventors: Karl-Heinz Boltze, Margaret A. Davies, Bodo Junge, Teunis Schuurman, Jorg Traber
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Patent number: 4552879Abstract: A benzoheterocyclic compound of the formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and n are as defined, and its pharmaceutically acceptable salts, processes for preparing same and antibacterial composition containing the benzoheterocyclic compound as an active ingredient and a pharmaceutically acceptable carrier are disclosed.Type: GrantFiled: May 25, 1983Date of Patent: November 12, 1985Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hiroshi Ishikawa, Testuyuki Uno, Masanobu Kano, Kazuyuki Nakagawa
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Patent number: 4552881Abstract: Novel substituted and bridged pyridines useful as calcium channel blockers, pharmaceutical compositions thereof and methods of treatment are disclosed.Type: GrantFiled: August 1, 1984Date of Patent: November 12, 1985Assignee: Merck & Co., Inc.Inventor: David A. Claremon
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Patent number: 4550205Abstract: The invention relates to new diphenyl ethers of the general formula ##STR1## wherein X is a hydrogen atom, a halogen atom, a nitro group, an optionally halogenated alkyl, alkoxy or alkylthio group having 1-6 carbon atoms, or an alkanoyl group having 1-4 carbon atoms;Y is a nitrogen atom or a group of the formula CH or CCl;Z is a hydrogen atom, a halogen atom, a nitro group, an optionally halogenated alkyl group having 1-4 carbon atoms, or an alkanoyl group having 1-4 carbon atoms; n is 0-2;R.sub.1 is a hydrogen atom, or an alkyl or alkanoyl group having 1-4 carbon atoms;R.sub.2 and R.sub.3 are equal or different and represent hydrogen atoms or alkyl groups having 1-4 carbon atoms; andA is a group of the general formula ##STR2## wherein R.sub.4 is a hydrogen atom, an alkyl group having 1-6 carbon atoms, or a cation of an alkali metal, alkaline earth metal or an alkylated or non-alkylated ammonium group, andR.sub.5 and R.sub.Type: GrantFiled: November 4, 1982Date of Patent: October 29, 1985Assignee: Duphar International Research B.V.Inventors: Gerard B. Paerels, Cornelis W. Raven
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Patent number: 4548941Abstract: There are disclosed novel substituted and bridged pyridines which are useful as calcium channel blockers.Type: GrantFiled: July 30, 1984Date of Patent: October 22, 1985Assignee: Merck & Co., Inc.Inventors: Wasyl Halczenko, George D. Hartman
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Patent number: 4547496Abstract: A novel [1] benzepino[3,4-b]pyridine derivative having antiulcer activity is represented by the formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl group, a halogenated alkyl group, an alkoxy group or a halogen atom; R.sup.2 represents ##STR2## wherein Y represents an amino group, a substituted amino group, a heterocyclic group or a substituted heterocyclic group; Z represents a hydrogen atom, an alkyl group or an acyl group; and m is an integer of 1-3, ##STR3## wherein Z' represents a hydrogen atom or an alkyl group; Y has the same meaning as defined above, and n is 0, 1 or 2; or ##STR4## wherein Z and n have the same meanings as defined above; X represents an oxygen atom or a sulfur atom. Also disclosed are pharmaceutically acceptable acid addition salts of the compound represented by the formula (I).Type: GrantFiled: June 21, 1984Date of Patent: October 15, 1985Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Toshiaki Kumazawa, Yoshimasa Oiji, Hiroshi Tanaka, Katsuichi Shuto
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Patent number: 4543354Abstract: Benzo[f]quinoline derivatives which are useful as antihypertensive agents and are represented by the formula: ##STR1## wherein R.sup.1 is hydrogen or lower alkyl, R.sup.2 is hydrogen, lower alkyl, hydroxy-lower-alkyl or lower-alkoxy-lower-alkyl, R.sup.3 and R.sup.4 are the same or different and each is hydrogen, lower alkyl, halogen, lower alkoxy, benzyloxy or hydroxy, R.sup.5 and R.sup.6 are the same or different and each is hydrogen, straight or branched alkyl, aralkyl or cycloalkyl, or R.sup.5 and R.sup.6 together with the adjacent nitrogen atom form a heterocycle, and the dotted line in the ring is an optional bond between 1- and 2-positions, and pharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: November 10, 1983Date of Patent: September 24, 1985Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Toru Nakao, Tsuguo Ikebe, Tetsuya Tahara, Yutaka Maruyama, Osamu Yaoka
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Patent number: 4542215Abstract: A method for preparing 8-acylthio-1,2,3,4,5,6-hexahydro-2,6-methano-3,6(e),11(a)-trimethyl-3-benz azocines represented by general formula (I) below ##STR1## wherein R represents an alkyl group, a phenyl group or a heterocyclic group, which comprises reacting 1,2,3,4,5,6-hexahydro-2,6-methano-3,6(e),11(a)-trimethyl-3-benzazocine represented by the formula (II) below ##STR2## or its salt with chlorosulfonic acid, heating the reaction product in the presence of a reducing agent, and reacting the reaction mixture with an acyl halide represented by the general formula (III)RCOX (III)wherein R has the same meaning as defined above and X represents a halogen atom is disclosed.Type: GrantFiled: May 19, 1983Date of Patent: September 17, 1985Assignee: Wako Pure Chemical Industries, Ltd.Inventors: Mikio Hori, Hajime Fujimura
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Patent number: 4535161Abstract: Benzoquinolizine derivatives of formula (I) ##STR1## wherein: X.sub.1 represents a hydrogen atom or a halogen atom,R.sub.1 represents a cyclic amino group which may contain additional hetero atom(s) of N,S and O and may be substituted with one or more substituents selected from the group consisting of hydroxyl, amino, alkyl, mono- or di-alkylamino, hydroxyalkyl and aminoalkyl, and physiologically acceptable salts thereof, having antibacterial activity.Type: GrantFiled: June 27, 1983Date of Patent: August 13, 1985Assignee: Daiichi Seiyaku Co., Ltd.Inventor: Isao Hayakawa
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Patent number: 4530927Abstract: New isoxazole[5,4-b]pyridines having antiinflammatory, CNS-depressant and cardiovascular activity.Type: GrantFiled: March 28, 1983Date of Patent: July 23, 1985Assignee: Gruppo Lepetit S.p.A.Inventors: Giorgio Winters, Alberto Sala
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Patent number: 4499266Abstract: Chemical compounds are provided that are novel 3,6-dinitro-1,8-naphthalimides (I), as well as a method for their production, pharmaceutical compositions comprising the compounds, and methods of treatment using the compounds in dosage form. Compounds of the invention have pharmacological properties and are useful antimicrobial agents and antitumor agents.Type: GrantFiled: April 1, 1983Date of Patent: February 12, 1985Assignee: Warner-Lambert CompanyInventors: Chia C. Cheng, Robert K. Zee-Cheng
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Patent number: 4481200Abstract: The invention concerns benzoquinolizines of formula ##STR1## and their pharmaceutically acceptable acid addition salts. In the formula R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, lower alkyl, lower alkoxy or halogen, R.sup.3 represents methyl or ethyl, A represents a direct bond between the S and N atoms or a lower alkylene group having 1 to 3 carbon atoms in the chain between the S and N atoms, R.sup.4 and R.sup.5 each independently represent hydrogen, lower alkyl, aryl or aryl(lower)alkyl or together with the nitrogen atom to which they are attached represent a five or six membered heterocyclic ring. The compounds possess .alpha..sub.2 -adrenoceptor antagonistic activity and can be incorporated into pharmaceutical compositions.Type: GrantFiled: March 3, 1983Date of Patent: November 6, 1984Assignee: John Wyeth & Brother, LimitedInventors: Terence J. Ward, John F. White
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Patent number: 4478834Abstract: New dihydropyridines are described. These compounds are useful in the treatment of asthma.Type: GrantFiled: February 11, 1983Date of Patent: October 23, 1984Assignee: USV Pharmaceutical CorporationInventors: James R. Shroff, Bernard Loev
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Patent number: 4469696Abstract: The invention relates to 4-,5-and 6-substituted 2-amino pyridines of Formula (I) and methods for their preparation. Also included in the invention are compositions containing said 2-amino pyridines of Formula (I) and the use of said compounds and compositions for use inter alia, as lipid absorption inhibitors.Type: GrantFiled: June 3, 1982Date of Patent: September 4, 1984Assignee: Bayer AktiengesellschaftInventors: Ulrich Rosentreter, Walter Puls, Hilmar Bischoff
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Patent number: 4446321Abstract: Novel 4-aryl-or heteroaryl-2,6-bis[(substituted-amino)phenyl]pyridines which are useful as color formers in pressure-sensitive carbonless duplicating systems and thermal marking systems are prepared by reacting a 2-, 3- or 4-R.sub.1 R.sub.2 N-acetophenone with an aryl or heteroaryl aldehyde in the present of ammonia or an ammonia-releasing agent.Type: GrantFiled: June 3, 1982Date of Patent: May 1, 1984Assignee: Sterling Drug Inc.Inventors: Paul J. Schmidt, William M. Hung
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Patent number: 4442291Abstract: The present invention is directed to a compound having the formula ##STR1## which is used as an intermediate in the preparation of octahydro-1H-pyrrolo[2,3-g]isoquinolines.Type: GrantFiled: March 28, 1983Date of Patent: April 10, 1984Assignee: Hoffmann-La Roche Inc.Inventors: Leo Berger, Gary L. Olson
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Patent number: 4440768Abstract: Pyrrolo [3,4-c]quinolines are described which have various substitutions at the 2, 4, 5, 6, 7, 8 and 9 positions. The group of compounds has been found to possess unexpected pharmaceutical utilities including antipsychotic, analgesic and antidepressant activities. Also set forth are various methods of making the compounds as well as pharmaceutical compositions containing them.Type: GrantFiled: July 8, 1982Date of Patent: April 3, 1984Assignee: ICI Americas inc.Inventor: Howard S. Shapiro
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Patent number: 4439437Abstract: This invention relates to 2-amino-3-hydroxy, and 3-carboxy pyridine derivatives, in which the amino group is substituted by a methylthioethyl, butyl or oxypropyl group bearing a terminal heterocyclic group. The compounds have histamine H.sub.2 -antagonist activity. A specific compound of this invention is 2-[2-(2-guanidino-4-thiazolylmethylthio)ethyl]amino pyridine 3-carboxylic acid.Type: GrantFiled: April 5, 1982Date of Patent: March 27, 1984Assignee: Smith Kline & French Laboratories LimitedInventors: Martin Jones, Rodney C. Young
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Patent number: 4430333Abstract: Dihydropyridine anti-ischaemic and antihypertensive agents of the formula: ##STR1## where Y is --(CH.sub.2).sub.2 -- or --(CH.sub.2).sub.3 --;R is aryl or heteroaryl;R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl or 2-methoxyethyl;andR.sup.3 and R.sup.4 are each independently C.sub.1 -C.sub.4 alkyl or aryl-(C.sub.1 -C.sub.4 alkyl); or R.sup.3 and R.sup.4 taken together with the nitrogen atom to which they are attached represent a group of the formula: ##STR2## where R.sup.5 is C.sub.1 -C.sub.4 alkyl, aryl, aryl-(C.sub.1 -C.sub.4 alkyl), benzhydryl; 2-methoxyethyl, 2-(N,N-di[C.sub.1 -C.sub.4 alkyl]amino) ethyl, or cyclopropylmethyl;their pharmaceutically acceptable acid addition salts, processes for the preparation of the compounds, and pharmaceutical compositions containing them.Type: GrantFiled: March 11, 1982Date of Patent: February 7, 1984Assignee: Pfizer Inc.Inventors: Simon F. Campbell, Peter E. Cross, John K. Stubbs
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Patent number: 4419352Abstract: There are described compounds of formula I, ##STR1## in which an adjacent pair of R.sub.5, R.sub.6, R.sub.7 and R.sub.8 form a chain --CZC(G.sub.1).dbd.(G.sub.2)--Z--,R.sub.4, R.sub.9 and the remainder of R.sub.5, R.sub.6, R.sub.7 and R.sub.8, which may be the same or different, each represent hydrogen, alkyl, halogen, alkenyl, --NO.sub.2, --NR.sub.1 R.sub.2, --OR.sub.3, --S(O).sub.n R.sub.3 ; or alkyl substituted by hydroxy, amino, alkoxy or carbonyl oxygen,n is 0, 1 or 2,R.sub.1 and R.sub.2, which may be the same or different, each represent hydrogen, alkyl, --CONHR.sub.3, phenyl or phenyl substituted by alkyl or halogen, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form a 5 or 6 membered heterocyclic ring,R.sub.3 represents hydrogen, alkyl, alkenyl or phenyl,one of G.sub.1 and G.sub.Type: GrantFiled: February 20, 1981Date of Patent: December 6, 1983Assignee: Fisons LimitedInventors: David Cox, Hugh Cairns, Nigel Chadwick, John L. Suschitzky
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Patent number: 4405626Abstract: 1,9-Dihydroxyoctahydrobenzo[c]quinolines (I), 1-hydroxyhexahydrobenzo[c]quinoline-9(8H)-ones (II), and 1-hydroxy-tetrahydrobenzo[c]quinolines (IV) useful as CNS agents, especially as analgesics and tranquilizers, as hypotensives, as agents for the treatment of glaucoma and as diuretics; intermediates therefor (III) and derivatives thereof having the formulae ##STR1## wherein R is hydroxy, alkanoyloxy having from one to five carbon atoms and hydroxymethyl;R.sub.1 is hydrogen, benzyl, benzoyl, alkanoyl having from one to five carbon atoms or --CO--(CH.sub.2).sub.p --NR.sub.2 R.sub.3 wherein p is 0 or an integer from 1 to 4; each of R.sub.2 and R.sub.3 when taken individually is hydrogen or alkyl having from one to four carbon atoms; R.sub.2 and R.sub.3 when taken together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclic ring (piperidino, pyrrolo, pyrrolidino, morpholino and N-alkylpiperazino having from one to four carbon atoms in the alkyl group); R.sub.Type: GrantFiled: December 9, 1981Date of Patent: September 20, 1983Assignee: Pfizer Inc.Inventor: Michael R. Johnson