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: 4400385Abstract: 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: August 23, 1983Assignee: Pfizer Inc.Inventor: Michael R. Johnson
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Patent number: 4399134Abstract: 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: November 10, 1981Date of Patent: August 16, 1983Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hiroshi Ishikawa, Testuyuki Uno, Masanobu Kano, Kazuyuki Nakagawa
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Patent number: 4380542Abstract: 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.Type: GrantFiled: December 9, 1981Date of Patent: April 19, 1983Assignee: PfizerInventor: Michael R. Johnson
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Patent number: 4374984Abstract: Compounds of the formula ##STR1## wherein the substituents A, Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, n and m are defined hereinbeloware effective photoinitiators, especially for the photopolymerization of ethylenically unsaturated compounds and for the curing of printing inks.Type: GrantFiled: March 4, 1981Date of Patent: February 22, 1983Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Jurgen Eichler, Claus Herz, Karl-Heinz Neisius, Gregor Wehner
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Patent number: 4351833Abstract: 9-Amino-1-hydroxyoctahydrobenzo[c]quinoline derivatives of formula ##STR1## and pharmaceutically acceptable acid addition salts thereof wherein R is hydrogen, COR.sub.7 or SO.sub.2 R.sub.8 where R.sub.7 is hydrogen, alkyl, having from one to five carbon atoms; alkenyl and alkynyl each having from two to six carbon atoms; trifluoromethyl, benzyl, furyl, thienyl, pyridyl or R.sub.9 C.sub.6 H.sub.4 where R.sub.9 is H, NH.sub.2, F, Cl, Br, Ch.sub.3 or OCH.sub.3 ; R.sub.8 is alkyl having from one to five carbon atoms or R.sub.9 C.sub.6 H.sub.4 ; 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.Type: GrantFiled: August 27, 1981Date of Patent: September 28, 1982Assignee: Pfizer Inc.Inventor: Michael R. Johnson
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Patent number: 4349678Abstract: Neuroleptically active octahydro-1H-pyrrolo[2,3-g]isoquinolines of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and X are as hereinafter set forth, are described.Type: GrantFiled: December 12, 1980Date of Patent: September 14, 1982Assignee: Hoffmann-La Roche Inc.Inventors: Leo Berger, Gary L. Olson
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Patent number: 4342871Abstract: An antiphlogistic compound of the formula (I) ##STR1## or a pharmaceutically effective salt thereof wherein R.sup.1 and R.sup.2 are hydrogen or C.sub.1-4 alkoxy or together form a methylenedioxy group;R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are hydrogen or a group of the formula --CH.sub.2 --(CH.sub.2).sub.n -R.sup.7 with the proviso that at least one of R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is other than hydrogen;R.sup.7 is a carboxylic group or a carboxylic acid derivative group; n=0, 1 or 2, provided that if R.sup.3, R.sup.4 and R.sup.5 are hydrogen and R.sup.7 in the group R.sup.6 is cyano or alkoxycarbonyl, and n=1, then R.sup.1 and R.sup.2 are hydrogen, C.sub.2-4 alkoxy, or together form a methylenedioxy group.Type: GrantFiled: November 24, 1976Date of Patent: August 3, 1982Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara RtInventors: Csaba Szantay, Lajos Szabo, Laszlo Toke, Istvan Toth, Sandor Virag, Erzsebet Kanyo, Agoston David
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Patent number: 4340737Abstract: 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- to 6-membered heterocyclic ring (piperidino, pyrrolo, pyrrolidino, morpholine and N-alkylpiperazino having from one to four carbon atoms in the alkyl group); R.sub.Type: GrantFiled: October 3, 1980Date of Patent: July 20, 1982Assignee: Pfizer Inc.Inventor: Michael R. Johnson
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Patent number: 4337250Abstract: Derivatives of 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]-indole and of (+)enantiomeric, mixtures of (+) and (-)enantiomeric or (.+-.)racemic 2,3,4,4a,5,9b-hexahydro-4a,9b-trans-1H-pyrido[4,3-b]indole, substituted at the 5-position with an aryl group and at the 2-position with a carbonylaminoalkyl group or an aminoalkyl group, are neuroleptic agents useful in the treatment of certain psychoses and neuroses.Type: GrantFiled: January 16, 1981Date of Patent: June 29, 1982Assignee: Pfizer Inc.Inventors: Willard M. Welch, Charles A. Harbert
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Patent number: 4335129Abstract: Nitrogen containing heterocyclic compounds shown by the formula ##STR1## wherein Y represents an oxygen atom, a sulfur atom, or a group shown by ##STR2## (wherein m is 1 or 2); n represents 0 or 1; R.sub.1 and R.sub.4, which may be the same or different, each represents a hydrogen atom, a lower alkyl group, or a lower alkenyl group; R.sub.2 and R.sub.3, which may be the same or different, each represents a hydrogen atom, a hydroxyl groups, a lower alkanoyloxy group, a lower alkyl group or a lower alkenyl group; said R.sub.2 and R.sub.3 may further form together a double bond; R.sub.5 and R.sub.6, which may be the same or different, each represents by hydrogen atom, a halogen atom, a hydroxyl group, a nitro group, an amino group, a lower alkoxy group, a mono or di lower alkylamino group, or a lower alkyl group; said R.sub.5 and R.sub.6 may further form together a lower alkylenedioxy group; and R.sub.Type: GrantFiled: January 28, 1981Date of Patent: June 15, 1982Assignee: Yamanouchi Pharmaceutical Co. Ltd.Inventors: Kazuo Kubo, Noriki Ito, Isao Souzu, Yasuo Isomura, Hiroshige Homma
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Patent number: 4322418Abstract: This invention relates to substituted 1-(.alpha.-aminocarbonyl-benzyl)-3,4-dihydro-isoquinolines in the racemic or optically active form and the non-toxic pharmacologically acceptable salts thereof. These compounds are useful in the promotion of blood circulation in warm-blooded animals.Type: GrantFiled: April 3, 1981Date of Patent: March 30, 1982Assignee: C. H. Boehringer SohnInventors: Walter Losel, Franz Esser, Otto Roos, Richard Reichl, Franz J. Kuhn, Werner Traunecker
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Patent number: 4321382Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, a straight or branched chain alkyl of 1-5 carbon atoms or a straight or branched chain alkanoyl of 1-5 carbon atoms;R.sub.2 is hydrogen, a straight or branched chain alkyl of 1-5 carbon atoms, phenyl, phenyl substituted with halogen, a straight or branched chain alkoxy of 1-5 carbon atoms, a straight or branched chain alkyl of 1-5 carbon atoms or trifluoromethyl or, when R.sub.1 is hydrogen, R.sub.2 can also be a straight or branched chain alkanoyl of 1-5 carbon atoms; orR.sub.1 and R.sub.2 taken together with the nitrogen atom to which they are attached form a saturated heterocyclic ring of 4-7 total ring atoms and 0 or 1 hetero N or O atom in addition to the connecting N atom; or the corresponding heterocyclic ring substituted by a C.sub.1-5 straight or branched chain alkyl group, aryl or aralkyl;R.sub.Type: GrantFiled: August 10, 1979Date of Patent: March 23, 1982Assignee: Richardson-Merrell Inc.Inventors: Charles A. Lundberg, Jr., Robert A. Farr
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Patent number: 4309545Abstract: 9-Amino-1-hydroxyoctahydrobenzo[c]quinoline derivatives of formula ##STR1## and pharmaceutically acceptable acid addition salts thereof wherein R is hydrogen, COR.sub.7 or SO.sub.2 R.sub.8 where R.sub.7 is hydrogen, alkyl, having from one to five carbon atoms; alkenyl and alkynyl each having from two to six carbon atoms; trifluoromethyl, benzyl, furyl, thienyl, pyridyl or R.sub.9 C.sub.6 H.sub.4 where R.sub.9 is H, NH.sub.2, F, Cl, Br, CH.sub.3 or OCH.sub.3 ; R.sub.8 is alkyl having from one to five carbon atoms or R.sub.9 C.sub.6 H.sub.4 ; 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.Type: GrantFiled: July 28, 1980Date of Patent: January 5, 1982Assignee: Pfizer Inc.Inventor: Michael R. Johnson
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Patent number: 4305938Abstract: The present invention provides 2,8-disubstituted-10-hydroxy-5,5-dimethyl-tetrahydro-and hexahydro-5H-[1]-benzopyrano[4,3-c]pyridines represented by Formulae I-III: ##STR1## wherein: R is selected from the group consisting of C.sub.4 -C.sub.20 straight or branched chain alkyl, C.sub.8 14 C.sub.20 straight or branched chain arylalkyl; n is an integer from 1-4 inclusive; and X is OH, NR.sub.1 R.sub.2, R.sub.1 and R.sub.2 being the same or different members of the group consisting of hydrogen and loweralkyl, and ##STR2## wherein Y is CH.sub.2, S, O or NR.sub.1 ; and the pharmaceutically acceptable salts thereof. The compounds are useful as antihypertensive agents.Type: GrantFiled: June 9, 1980Date of Patent: December 15, 1981Assignee: Abbott LaboratoriesInventor: Harold E. Zaugg
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Patent number: 4279912Abstract: Novel imidazoquinolines of the formula ##STR1## wherein X and Y are individually selected from the group consisting of hydrogen, halogen and alkoxy of 1 to 5 carbon atoms, Z is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms optionally substituted with at least two hydroxyls or protected hydroxyls and ##STR2## n is an integer from 1 to 6 and R.sub.1 and R.sub.2 are individually alkyl of 1 to 5 carbon atoms and taken together with the nitrogen to which they are attached form a saturated heterocyclic ring containing 4 to 6 carbon atoms and optionally interrupted by another heteroatom which further heteroatom is optionally substituted with alkyl of 1 to 5 carbon atoms and non-toxic, pharmaceutically acceptable salts thereof having antiallergic and bronchodilatory activity and their preparations.Type: GrantFiled: January 16, 1978Date of Patent: July 21, 1981Assignee: Roussel UclafInventors: Ian R. Ager, Peter J. Ramm
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Patent number: 4260764Abstract: 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: May 29, 1979Date of Patent: April 7, 1981Assignee: Pfizer Inc.Inventor: Michael R. Johnson
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Patent number: 4260762Abstract: Neuroleptically active octahydro-1H-pyrrolo[2,3-g]isoquinolines of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and X are as hereinafter set forth,are described.Type: GrantFiled: September 10, 1979Date of Patent: April 7, 1981Assignee: Hoffmann-La Roche Inc.Inventors: Leo Berger, Gary L. Olson
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Patent number: 4254116Abstract: 5H-[1]Benzopyrano[3,4-d]pyridines represented by the formula ##STR1## wherein each R.sub.1 is loweralkyl, R.sub.2 is alkyl, cycloalkyl or ##STR2## wherein Y is a straight or branched chain alkylene group having from 1 to 10 carbon atoms and each R.sub.4, R.sub.5 and R.sub.6 are the same or different members of the group consisting of hydrogen, halo, trifluoromethyl or loweralkyl; and R.sub.3 is hydroxy, acyloxy, loweralkoxy, loweralkenyloxy, loweralkynyloxy or ##STR3## X is a straight or branched chain alkylene group having from one to eight carbon atoms, and wherein R.sub.7 and R.sub.8 are the same or different members of the group consisting of hydrogen or loweralkyl, or ##STR4## wherein X is a straight or branched chain alkylene group having from one to eight carbon atoms, a is an integer from 1 to 4, b is an integer from 1 to 4, Z is CH.sub.2, O, S or NR.sub.10 with R.sub.10 being hydrogen or loweralkyl, with the limitation that when Z is O or S, the sum of a and b is 3 or 4; and when Z is NR.sub.Type: GrantFiled: April 8, 1974Date of Patent: March 3, 1981Assignee: Abbott LaboratoriesInventor: Cheuk M. Lee
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Patent number: 4244954Abstract: 9-Phenyl(or benzyl)acridines, 9-phenyl(or benzyl)-9-acridinols and acridinium compounds, useful as trypanosomacidal and antibacterial agents, are prepared from aminoalkoxy substituted 9-acridinones via reaction with the appropriate Grignard reagents or aryllithium. The intermediate aminoalkoxy substituted 9-acridinones, prepared from the corresponding halo or hydroxy substituted 9-acridinones, are useful as antiviral agents.Type: GrantFiled: October 2, 1978Date of Patent: January 13, 1981Assignee: Sterling Drug Inc.Inventor: John W. Schulenberg
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Patent number: 4242513Abstract: Chromogenic compounds of normally colorless form are disclosed having the following structural formula: ##STR1## wherein E represents a six-membered aromatic or heterocyclic ring which may have an aromatic condensed ring and both the E ring and the condensed ring may be substituted, A represents an optionally substituted aminophenyl, indolyl, benzoindolyl, julolidinyl or kairolyl radical or the radical represented by B, and B represents a family of heterocyclic radicals. The compounds of this invention are eligible for use in pressure-sensitive and heat sensitive record materials and manifold marking systems.Type: GrantFiled: March 5, 1979Date of Patent: December 30, 1980Assignee: Appleton Papers Inc.Inventors: Troy E. Hoover, Sheldon Farber, William J. Becker
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Patent number: 4206225Abstract: A compound of the formula ##STR1## wherein Q is CH.sub.2, C.dbd.O, CHOH or CHCH.sub.2 OH; M is O or NR.sub.6 ; where R.sub.6 is hydrogen, or certain alkyl, aralkyl, acyl or carboalkoxy substituted alkyl groups; R.sub.1 is hydrogen, or certain alkanoyl or amino substituted alkanoyl groups; R.sub.4 and R.sub.5 are each hydrogen or alkyl having from 1 to 4 carbon atoms; Z is alkylene having from 1 to 9 carbon atoms or --(alk.sub.1)--X--(alk.sub.2).sub.n -- where (alk.sub.1) and (alk.sub.2) are certain alkylene groups and X is O, S, SO or SO.sub.2 ; W is a methyl, phenyl, substituted phenyl, pyridyl, piperidyl, cycloalkyl or substituted cycloalkyl group and the pharmaceutically acceptable and addition salts of said compounds having a basic nitrogen atoms. Said compounds are useful as analgesics and as intermediates therefore.Type: GrantFiled: September 22, 1978Date of Patent: June 3, 1980Assignee: Pfizer Inc.Inventor: Michael R. Johnson
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Patent number: 4204063Abstract: N-substituted-3-substituted naphthalimides are prepared by reacting 3-substituted naphthalic acid with a compound having a primary amino group. The naphthalimides possess cytotoxic properties.Type: GrantFiled: June 2, 1978Date of Patent: May 20, 1980Assignee: Laboratorios Made, S.A.Inventors: Miguel F. Brana, Antonio M. Sanz, Rafael P. Alvarez-Ossorio, Cristobal M. Roldan, Cristina R. Fernandez de Gamboa
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Patent number: 4200751Abstract: Lactone electron donative color-forming agents of quinoline-carboxylic acid are disclosed having the general formulae (I) and (II) ##STR1## wherein A and B represent a variety of chemical moieties, X represents halo- or nitro- and n.sup.1 is an integer of 0-4. The color-forming agents are useful in recording materials of the pressure-sensitive and heat-sensitive varieties, and the like.Type: GrantFiled: November 21, 1977Date of Patent: April 29, 1980Assignee: Yamamoto Kagaku Gosei Co., Ltd.Inventors: Seiji Ikegami, Yoshihiro Hatano
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Patent number: 4176184Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is lower alkyl; phenyl-lower alkyl; cycloalkyl of 3 to 6 carbon atoms; phenyl; mono- or di-substituted phenyl, where the substituents, which may be identical to or different from each other, are each halogen, hydroxyl, methoxy, methylmercapto, methylsulfinyl, methylsulfonyl or benzyloxy; andA is hydrogen or ##STR2## where R.sub.2 is hydrogen or lower alkyl;R.sub.3 is lower alkyl or dimethoxyphenyl-lower alkyl; orR.sub.2 and R.sub.3, together with each other and the nitrogen atom to which they are attached, are piperidino, morpholino or N'-lower alkyl-piperazino; andn is 2 or 3;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as cardiotonics, hypotensives, antithrombotics and antiarrhythmics.Type: GrantFiled: July 17, 1978Date of Patent: November 27, 1979Assignee: Boehringer Ingelheim GmbHInventors: Volkhard Austel, Eberhard Kutter, Joachim Heider, Wolfgang Eberlein, Walter Kobinger, Christian Lillie, Willi Diederen, Walter Haarmann
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Patent number: 4172943Abstract: A compound of the formula ##STR1## wherein R.sub.1 is H or loweralkyl; R.sub.2 is H, loweralkyl, phenyl or substituted phenyl; R is C.sub.3 -C.sub.20 alkyl, phenyl alkyl or substituted phenyl alkyl; R.sub.3 is H or ##STR2## where X is a straight or branched chain alkylene group of 3 to 4 carbon atoms, and R.sub.4 and R.sub.5 are the same or different members of the group consisting of H or loweralkyl; or R.sub.4 and R.sub.5 taken together form a 6- or 6- member heterocyclic ring and containing no more than one additional heterocyclic atom, with or without .alpha.-loweralkyl substituents, and the acid addition salts thereof.The compounds of this invention are useful as analgesics, tranquilizers, sedative-hypnotics and anti-glaucoma agents.Type: GrantFiled: August 4, 1978Date of Patent: October 30, 1979Assignee: Abbott LaboratoriesInventors: Harold E. Zaugg, Cheuk M. Lee
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Patent number: 4172202Abstract: N-substituted amides or optionally N-substituted hydrazides of 4-amino-naphthalic acids which may be substituted in 3-position by a sulfo group are obtained by reacting 4-halo-1,8-naphthalic anhydride with a primary amine or an optionally N-substituted hydrazine having a pK.sub.a -value of at least 8, exchanging in the so-obtained 4-halo-naphthalimide the halogen for the amino group by reacting it with ammonia and, optionally, subsequent sulfonation. The products are dyeing matters useful for the coloration of synthetic fibers, plastics, oils, waxes, resins, paper, printing pastes, lacquers or natural polyamides, especially for daylight-fluorescence pigments.Type: GrantFiled: January 9, 1978Date of Patent: October 23, 1979Assignee: Hoechst AktiengesellschaftInventor: Theodor Papenfuhs
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Patent number: 4163844Abstract: Novel nitrogen-containing heterocyclic compounds shown by the formula ##STR1## wherein Y represents an oxygen atom, a sulfur atom, or a group shown by ##STR2## (wherein m is 1 or 2); n represents 0 or 1; R.sub.1 and R.sub.4, which may be the same or different, each represents a hydrogen atom, a lower alkyl group, or a lower alkenyl group; R.sub.2 and R.sub.3, which may be the same or different, each represents a hydrogen atom, a hydroxyl group, a lower alkanoyloxy group, a lower alkyl group or a lower alkenyl group; said R.sub.2 and R.sub.3 may further form together a double bond; R.sub.5 and R.sub.6, which may be the same or different, each represents a hydrogen atom, a halogen atom, a hydroxyl group, a nitro group, an amino group, a lower alkoxy group, a mono or di lower alkylamino group, or a lower alkyl group; said R.sub.5 and R.sub.6 may further form together a lower alkylenedioxy group; and R.sub.Type: GrantFiled: December 19, 1977Date of Patent: August 7, 1979Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Kazuo Kubo, Noriki Ito, Isao Souzu, Yasuo Isomura, Hiroshige Homma
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Patent number: 4139532Abstract: Compounds of the formula: ##STR1## in which one R is identical with or different from the other R and each is alkyl, hydroxyalkyl, alkoxyalkyl, haloalkyl, cycloalkyl, aralkyl, aryl, N,N-dialkylaminoalkyl or quaternized N,N-dialkylaminoalkyl; A is ##STR2## or ##STR3## R.sup.1 is hydrogen, substituted or unsubstituted alkyl, cycloalkyl, aralkyl, aryl or heteroaryl;B is --CH.dbd.CH--, --CCl.dbd.CH--, --CCl.dbd.CCl--, --CH.dbd.CBr--, --CH.sub.2 --CH.sub.2 --,1,2-phenylene, 1,8-naphthylene or 1,2-phenylene or 1,8-naphthylene bearing chloro, bromo, methoxy or ethoxy as a substituent; and T is acyl.The compounds are eminently suitable as optical brighteners, particularly for polyesters and blends of polyester and cotton.Type: GrantFiled: May 14, 1976Date of Patent: February 13, 1979Assignee: BASF AktiengesellschaftInventors: Horst Scheuermann, Albert Hettche
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Patent number: 4133885Abstract: Organic chemical compounds based upon the naphthyridine molecule are disclosed which have potent gastric secretion inhibitory properties. The naphthyridinone is substituted with a substituted amino alkyl group at the 1-position, and variously substituted at the remaining positions. The compounds have profound effects on the inhibition of gastric secretions in the gastro-intestinal tract, and compositions for such uses are also disclosed.Type: GrantFiled: July 18, 1977Date of Patent: January 9, 1979Assignee: Merck & Co., Inc.Inventors: William A. Bolhofer, Edward J. Cragoe, Jr., Jacob M. Hoffman, Jr.
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Patent number: 4126620Abstract: 2,4,5,6-Tetrahydrocyclopenta[c]pyrrole-4-carboxamide and 4-thiocarboxamide derivatives useful as antisecretory and anti-ulcer agents are prepared by hydrolysis or thiohydrolysis of the corresponding 2,4,5,6-tetrahydrocyclopenta[c]pyrrole-4-carbonitriles or, in the case of the thiocarboxamides, by reaction of the 4-carboxamide with phosphorus pentasulfide.Type: GrantFiled: February 25, 1977Date of Patent: November 21, 1978Assignee: Sterling Drug Inc.Inventors: Malcolm R. Bell, Rudolf Oesterlin
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Patent number: 4108998Abstract: Furo[3,4-b]quinoline derivatives, having both an alkyl substituent and an alkyl or alkylene amide substituent at position 3 are disclosed. The derivatives can be further substituted at positions 1 and 9. The furo[3,4-b]quinoline derivatives of this invention are useful antihypertensive and antimicrobial agents. Methods for the preparation and use of these derivatives are also disclosed.Type: GrantFiled: November 8, 1976Date of Patent: August 22, 1978Assignee: American Home Products Corp.Inventors: Christopher A. Demerson, Leslie G. Humber
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Patent number: 4102886Abstract: A process for the preparation of a compound of the formula I or a salt thereof ##STR1## wherein R.sup.1 and R.sup.2 each represent hydrogen or a C.sub.1-4 alkoxy group, or together form a methylenedioxy group;R.sup.3, r.sup.4, r.sup.5 and R.sup.6 are the same or different and are hydrogen or a group of the formula --CH.sub.2 --(CH.sub.2).sub.n --R.sup.7 with the proviso that at least one of the members R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is other than hydrogen; R.sup.7 is carboxyl or a carboxylic acid derivative group;N = 0.1 or 2 which comprises reacting a compound of the formula II ##STR2## with an organic secondary amine and reacting the N-amine of the formula III ##STR3## thus obtained wherein R.sup.8 and R.sup.9 each represent a C.sub.1-5 alkyl group, or together with the adjacent nitrogen atom form a 5- or 6-membered heterocyclic ring which can contain a further heteroatom, with a compound of the formula IVch.sub.2 .dbd. ch -- (ch.sub.2).sub.n -- R.sup.10 (IV)wherein R.sup.Type: GrantFiled: October 21, 1975Date of Patent: July 25, 1978Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.Inventors: Csaba Szantay, Lajos Szabo, Laszlo Toke, Istvan Toth, Sandor Virag, Erzsebet Kanyo, Agoston David
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Patent number: 4096145Abstract: Compounds of the formula ##STR1## where A is a heterocyclic group containing a pyridone moiety and R to R.sup.5 are each hydrogen or substituents conventionally encountered in dyes. The compounds are eminently suitable for coloring resins and for dyeing textile materials, particularly polyester textile materials.Type: GrantFiled: March 14, 1977Date of Patent: June 20, 1978Assignee: BASF AktiengesellschaftInventor: Ernst Schefczik
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Patent number: 4085111Abstract: 1H-Tetrazole derivatives of the formula: ##STR1## and pharmaceutically acceptable salts thereof, wherein the ring P is pyridine ring; A is carbonyl, methylene or C.sub.2-4 alkylidene; Y is oxygen, sulfur or --N(R.sup.1)-- wherein R.sup.1 is hydrogen or C.sub.1-4 alkyl; each of X.sup.1 and X.sup.2 is hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, phenyl or substituted phenyl, any substitutent on the phenyl being halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or trifluoromethy; and R is hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, hydroxy-C.sub.1-4 alkyl, C.sub.1-4 alkoxy-C.sub.1-4 alkyl, carboxy-C.sub.1-4 alkyl, C.sub.1-4 alkoxycarbonyl-C.sub.1-4 alkyl or substituted or unsubstituted amino-C.sub.1-4 alkyl, any substituted amino being C.sub.1-4 alkyl- or di-C.sub.1-4 alkyl-amino, piperidino, 1-pyrrolidinyl, morpholino, 1-piperazinyl and 4-C.sub.1-4 alkyl-1-piperazinyl; are useful as antiallergic agents.Type: GrantFiled: May 20, 1975Date of Patent: April 18, 1978Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Takanori Oe, Mineo Tsuruda
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Patent number: 4081449Abstract: Heterocyclic esters of alkylphenyl benzopyranopyridines represented by the formula ##STR1## wherein R.sub.1 is hydrogen, loweralkyl, loweralkanoyl, cycloalkylloweralkyl, cycloalkylloweralkanoyl, loweralkenyl, loweralkynyl, haloloweralkenyl, phenylloweralkyl, phenylloweralkenyl or phenylloweralkynyl; R.sub.2 is loweralkyl; R.sub.3 is ##STR2## WHEREIN X is a straight or branched chain alkylene group having from one to eight carbon atoms, a is an integer from 1 to 4, b is an integer from 1 to 4 and Z is CH.sub.2, O, S or NR.sub.7, with R.sub.7 being hydrogen or loweralkyl, with the limitation that when X is O, S or NR.sub.7, the sum of a and b is 3 or 4; and R.sub.8 is hydrogen or loweralkyl; Y is a straight or branched chain alkylene group having from one to ten carbon atoms; and each R.sub.4 and R.sub.5 and R.sub.6 are the same or different members of the group consisting of hydrogen, halo, trifluoromethyl or loweralkyl; and the pharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: April 5, 1973Date of Patent: March 28, 1978Assignee: Abbott LaboratoriesInventor: Martin Winn
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Patent number: 4075211Abstract: Compounds of the naphthalimide series which in the dissolved condition exhibit a characteristic blue, violet or bluish violet fluorescence, and a process for their production. The compounds are outstandingly suitable for the optical brightening of synthetic fibers.Type: GrantFiled: January 2, 1976Date of Patent: February 21, 1978Assignee: BASF AktiengesellschaftInventors: Horst Scheuermann, Albert Hettche
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Patent number: 4051134Abstract: Reactive dyestuffs of the formula ##STR1## wherein W, T, T', n, R, R.sub.1, R.sub.2, p and Z have the meaning given in the description, their preparation and their use for dyeing and printing materials containing N and materials containing hydroxyl groups, especially fibre materials. The dyestuffs are particularly suitable as fluorescent dyestuffs for dyeing or printing natural and synthetic polyamides and natural and regenerated cellulose, especially cotton. They combine a high fixing yield with outstanding wet fastness properties.Type: GrantFiled: November 20, 1975Date of Patent: September 27, 1977Assignee: Bayer AktiengesellschaftInventors: Adolf Friedrich, Horst Harnisch, Roderich Raue