The Diazine Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 544/115)
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Patent number: 5162320Abstract: Compounds of formula I are described, ##STR1## wherein: R.sub.1 and R.sub.2, that can be the same or different, are hydrogen or acyl groups;R.sub.3 and R.sub.4, that can be the same or different, are hydrogen or optionally substituted alkyl groups.The compounds of formula I are prepared by oxydation of the compounds of formula II: ##STR2## wherein the groups R'.sub.1, R'.sub.2, R'.sub.3 and R'.sub.4 have the same meanings as R.sub.1, R.sub.2, R.sub.3 and R.sub.4 or groups convertible to the latter.The compounds of formula I have remarkable antitumor activity.Type: GrantFiled: October 25, 1990Date of Patent: November 10, 1992Assignee: Boehringer Biochemia Robin S.p.A.Inventors: Carmelo A. Gandolfi, Francis Johnson, Ernesto Menta, Silvano Spinelli, Sergio Tognella
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Patent number: 5143915Abstract: A compound of the formula ##STR1## (symbols defined in the specification), its 3,4-dihydropyrimidine tautomer form and pharmaceutically acceptable salts thereof have calcium entry blocking activity. A process of preparation, pharmaceutical composition and method of using the compound to reduce blood pressure are also provided.Type: GrantFiled: July 25, 1990Date of Patent: September 1, 1992Assignee: E. R. Squibb & Sons, Inc.Inventors: George C. Rovnyak, Spencer D. Kimball
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Patent number: 5137879Abstract: Compounds of the formula ##STR1## R.sup.1 is H, C.sub.1 -C.sub.4 alkyl, or phenyl optionally substituted with halo, (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkoxy, halo (C.sub.1 -C.sub.4) alkyl, or halo (C.sub.1 -C.sub.4) alkoxy;R.sup.2 is H, (C.sub.1 -C.sub.4) alkyl, nitro, halo; orR.sup.1 and R.sup.2 combine to form --(CH.sub.2).sub.4 --;R.sup.3 is H, (C.sub.1 -C.sub.4) alkyl, halo (C.sub.1 -C.sub.4 alkyl, phenyl, or substituted phenyl;Y is a bivalent hydrocarbon radical two to six carbon atoms long, optionally substituted with (C.sub.1 -C.sub.4) alkyl, (C.sub.2 -C.sub.4) alkenyl or -alkynyl, branched (C.sub.3 -C.sub.7) alkyl, (C.sub.3 -C.sub.7) cycloalkyl or cycloalkenyl, halo, halo (C.sub.1 -C.sub.4) alkyl, halo (C.sub.1 -C.sub.4) alkoxy, hydroxy, or (C.sub.1 -C.sub.4) acyl; andZ is an optionally substituted cycloalkyl, cycloalkenyl, phenyl, naphtyl, or pyridyl group;are useful as fungicides and as intermediates in making other pesticides.Type: GrantFiled: March 30, 1990Date of Patent: August 11, 1992Assignee: DowElancoInventors: Ronnie G. Edie, Eriks V. Krumkalns, Ronald E. Hackler
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Patent number: 5130426Abstract: Bis(morpholinomethyl) derivatives of tricyclic bisdioxopyperzaines of the formula ##STR1## wherein R is H, ##STR2## R' is H, lower alkyl groups (straight or branched chain of 1 to 6 carbon atoms) and the processes for the syntheses thereof are provided.Type: GrantFiled: June 27, 1985Date of Patent: July 14, 1992Assignee: Ohio State UniversityInventors: Donald T. Witiak, Bharat K. Trivedi
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Patent number: 5130430Abstract: The invention encompasses compounds of the formula: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 represent organic or inorganic substituents; X represents hydrogen, halogen, hydroxy or amino and W represents phenyl, thienyl or pyridyl, each of which may be unsubstituted or mono or disubstituted with organic or inorganic substituents.These compounds are highly selective agonists, antagonists or inverse agonists for GABA a brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine drugs, and enhancement of memory.Type: GrantFiled: October 31, 1990Date of Patent: July 14, 1992Assignee: Neurogen CorporationInventor: Kenneth Shaw
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Patent number: 5128338Abstract: New imidazo [1,2-c] quinazoline compounds useful as coronary smooth muscle relaxants and corresponding to the formula: ##STR1## in which: Y is oxygen or sulfur;R.sub.1 is (C.sub.1 -C.sub.6) alkyl optionally substituted by a phenyl itself optionally substituted, a (C.sub.3 -C.sub.6) cycloalkyl, optionally substituted phenyl, furyl, thienyl or acyl;R.sub.2 is hydrogen, a halogen or a (C.sub.1 -C.sub.6) alkyl optionally substituted by amino or dialkylamino;R.sub.3 is hydrogen, (C.sub.1 -C.sub.6) alkyl optionally substituted by an aryl, or R--CO--(CH.sub.2).sub.n -- [n being 1, 2 or 3, and R being (C.sub.1 -C.sub.6) alkoxy, amino, (alkyl or dialkyl)amino, morpholino or methylpiperazinyl]; andX is hydrogen or a halogen.These compounds and their physiologically tolerated salts can be used in medical treatment of coronary smooth-muscle dysfunctions.Type: GrantFiled: March 8, 1991Date of Patent: July 7, 1992Assignee: Adir et CompagnieInventors: Jean-Jacques Bourguignon, Camille-Georges Wermuth, de la Faverie Renaud, Catherine Thollon, Alain Lombet
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Patent number: 5124331Abstract: 3,4-Dihydrothieno[2,3-d]pyrimidine compounds having immunoregulating and carcinostatic actions of the general formula ##STR1## wherein A represents a C.sub.1-4 alkylene; R.sup.1 represents hydrogen, an alkyl, an aryl which may be substituted or --N(R.sup.7)(R.sup.8); R.sup.2, R.sup.3 and R.sup.4 represent hydrogen, a halogen, hydroxy, an alkyl which may be substituted by a halogen, an alkoxy, nitro, cyano or --N(R.sup.9)(R.sup.10); R.sup.5 represents hydrogen, a halogen, nitro, amino, cyano, an alkyl or an alkoxycarbonyl; R.sup.6 represents hydrogen, a halogen, nitro, amino, cyano, an alkyl, an alkoxycarbonyl, a halogenosulfonyl or --SO.sub.2 N(R.sup.12)(R.sup.13); or R.sup.5 and R.sup.6 may, taken together, form a C.sub.3-6 alkylene chain, and their pharmaceutical use.Type: GrantFiled: November 2, 1989Date of Patent: June 23, 1992Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Masafumi Arita, Yoshitaka Fukumasu, Mitsuharu Sano, Yukio Hoshino, Hirotsugu Komatsu
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Patent number: 5120845Abstract: The present invention relates to novel positive inotropic and lusitropic 3,5-dihydroimidazo[2,1-b]quinazolin-2(1H)-one derivatives having positive inotropic and lusitropic properties which are useful in the treatment of warm-blooded animals suffering from Congestive Heart Failure. Pharmaceutical compositions containing said compounds as an active ingredient. Methods of preparing said compounds and pharmaceutical compositions.Type: GrantFiled: July 24, 1991Date of Patent: June 9, 1992Assignee: Janssen Pharmaceutica N.V.Inventors: Eddy J. E. Freyne, Alfons H. M. Raeymaekers
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Patent number: 5114934Abstract: The compounds of the formula ##STR1## wherein R.sub.a, R.sub.b, R.sub.c, R.sub.d are defined in the specification and pharmaceutically acceptable addition salts are disclosed. The compounds of formula I have valuable pharmacological properties and can be used for the control of prevention of illnesses. In particular, they have muscle relaxant, seditive-hypnotic, anxiolytic and/or anticonvulsive activity and can accordingly be used in the control or prevention of muscle tensions, stress conditions, isomnia, anxiety states and/or convulsions.Type: GrantFiled: June 1, 1989Date of Patent: May 19, 1992Assignee: Hoffman-La Roche, Inc.Inventors: Ulf Fischer, Fernand Schneider, Ulrich Widmer
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Patent number: 5082842Abstract: The compounds of the formula ##STR1## wherein Ra, Rb, Rc, Rd, Re and Rf are defined in the specification, and the pharmaceutically acceptable acid addition salts of compounds of formula A which have one or more basic substituents are described. The compounds of formula A have valuable pharmacological properties and can be used for the control or prevention of illnesses. In particular, they have muscle relaxant, sedative-hypnotic, anxiolytic and/or anticonvulsive activity and can accordingly be used in the control or prevention of muscle tensions, stress conditions, insomnia, anxiety states and/or convulsions.Type: GrantFiled: October 16, 1989Date of Patent: January 21, 1992Assignee: Hoffmann-La Roche Inc.Inventor: Ulrich Widmer
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Patent number: 5075304Abstract: New imidazoquinoxaline compounds having the general formula ##STR1## wherein R.sup.3 is ##STR2## or CO.sub.2 R' wherein R' isC.sub.3-7 -cycloalkyl;R.sup.5 is methyl, which is substituted with hydrogen, alkoxycarbonyl, heteroaryl, morpholino, C.sub.3-7 -cycloalkyl, C.sub.1-6 -alkenyl, arylacyl, alkylacyl, alkoxyalkyl, alkoxy, phthalimidophenyl, aralkyl or aryl, all of which are substituted with hydrogen, halogen, C.sub.1-6 -alkyl, amino, azido, or C.sub.1-6 -alkoxy;and R.sup.6 is H, C.sub.1-6 -alkyl, halogen, or CF.sub.3.The compounds are useful in psychopharmaceutical preparations as anticonvulsants, anxiolytics, hypnotics, and in improving the cognitive function of the brain of mammals.Type: GrantFiled: May 18, 1989Date of Patent: December 24, 1991Assignee: Novo Nordisk A/SInventors: Holger C. Hansen, Frank Watjen
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Patent number: 5055465Abstract: This invention relates to novel imidazoquinoxalinones and their aza analogs and to a process for their preparation. The compounds of this invention have been found to have inodilatory, vasodilatory, venodilatory and other pharmacologic effects.Type: GrantFiled: May 31, 1989Date of Patent: October 8, 1991Assignee: Berlex Laboratories, Inc.Inventor: David D. Davey
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Patent number: 5045541Abstract: Fused pyridazine compounds ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and respectively hydrogen, a halogen, hydroxy, nitro, amino, cyano, trifluoromethyl, and alkyl, an alkoxy or an alkanoylamino; one of R.sub.a and R.sub.b is a group of the formula--O--Y--NR.sup.5 R.sup.6wherein R.sup.5 and R.sup.6 are the same or different and respectively hydrogen, an alkyl, a phenylalkyl or a substituted phenylalkyl or a group forming a heterocycle together with the adjacent nitrogen atom and Y stands for a straight- or branched-chain alkylene which may have hydroxy group as a substituent on the chain, and the other is hydrogen, or both of R.sub.a and R.sub.b are the same or different and respectively a group of the formula--O--Y--NR.sup.5 R.sup.6wherein R.sup.5 and R.sup.6 are of the same meanings as defined above; W is .dbd.CH-- or .dbd.N; X is CH.sub.2, S, SO, SO.sub.Type: GrantFiled: July 2, 1989Date of Patent: September 3, 1991Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Toru Nakao, Minoru Kawakami, Masao Hisadome, Tetsuya Tahara
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Patent number: 5043327Abstract: The present invention relates to novel positive inotropic and lusitropic 3,5-dihydroimidazo[2,1-b]quinazolin-2(1H)-one derivatives having positive inotropic and lusitropic properties which are useful in the treatment of warm-blooded animals suffering from Congestive Heart Failure. Pharmaceutical compositions containing said compounds as an active ingredient. Methods of preparing said compounds and pharmaceutical compositions.Type: GrantFiled: November 16, 1990Date of Patent: August 27, 1991Assignee: Janssen Pharmaceutica N.V.Inventors: Eddy J. E. Freyne, Alfons H. M. Raeymaekers
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Patent number: 4992442Abstract: Pyrrolo[3,2-e]pyrazolo[1,5-a]pyrimidine derivatives are disclosed. The compounds are represented by the formula (I), ##STR1## wherein R.sub.1 and R.sub.2 individually represent a hydrogen atom, a linear or branched alkyl group which may have a substituent, a cycloalkyl or phenyl group which may have a substituent, or a heterocyclic group which may have a substituent, and R.sub.3 is a hydrogen atom or a cyano group. The compounds have excellent circulatory disease curing activities as well as bronchodilation activities.Type: GrantFiled: October 3, 1989Date of Patent: February 12, 1991Assignee: Pola Chemical Industries Inc., JapanInventors: Michihiko Tsujitani, Kenichi Kishii, Masato Inazu, Toshihiro Morimoto, Yoshiaki Motoki, Ichiro Matsuo
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Patent number: 4985560Abstract: The compound of the formula: ##STR1## in which R.sup.1 is hydrogen, alkoxy, cyano, halo, nitro, amino, or mono- or dialkylamino; R.sup.2 is hydrogen, alkyl, phenyl, benzyl, 2-thienyl, 3-thienyl or 2-,3- or 4-pyridinyl; R.sup.3 is hydrogen, alkyl or phenyl; R.sup.4 is N-methyl-pyrrolidin-2yl, 2-, 3- or 4-pyridinyl, 3-quinuclidinyl or ##STR2## where n is 1 to 5; m is 0 to 3; and R.sup.8 is hydrogen or alkyl of 1 to 6 carbon atoms; or R.sup.4 is ##STR3## wherein: (a) n is 2, R.sup.5 taken with R.sup.3 is ethylene and R.sup.6 is --CHO, alkyl, unsubstituted or substituted phenyl, pyrimidinyl, pyridinyl, or pyrazinyl, where the substituents are alkyl, alkoxyl, halo, cyano, nitro or trifluoromethyl; (b) n is 1 to 5, and R.sup.5 and R.sup.6 taken together are polymethylene which may be alkyl substituted or R.sup.5 nd R.sup.6 are morpholino, 3-azabicyclo[3.2.Type: GrantFiled: January 12, 1990Date of Patent: January 15, 1991Assignee: American Home Products CorporationInventors: Annmarie L. Sabb, Magid A. Abou-Gharbia, Gervais Dionne
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Patent number: 4983603Abstract: The invention relates to novel tricyclic derivatives which are agonists of cholinergic receptors.These derivatives have the formula ##STR1## in which X=O, S, --OCH.sub.2 -- or --SCH.sub.2 --; R.sub.1 =H or halogen; and R.sub.2 = ##STR2## in which Alk is an alkylene group and R.sub.3, an R.sub.4, which are identical or different, are hydrogen or a lower alkyl group, or R.sub.3 and R.sub.4, with the nitrogen atom to which they are bonded, form a 5- or 6-membered cyclic amino group optionally containing a second heteroatom; or R.sub.2 is a group ##STR3## where R.sub.5 =C.sub.1 -C.sub.4 -alkyl. Application: agonists of cholinergic receptors.Type: GrantFiled: December 23, 1988Date of Patent: January 8, 1991Assignee: Societe Anonyme: SANOFIInventors: Camille G. Wermuth, Paul Worms, Jean-Jacques Bourguignon, Roger Brodin
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Patent number: 4977152Abstract: The invention relates to novel tricyclic derivatives which are agonists of cholinergic receptors and to drugs containing them.These derivatives have the following formula: ##STR1## in which: X represents a group (CH.sub.2).sub.n, n representing an integer equal to 2, 3 or 4, or alternatively a vinylene group or a methylvinylene group;R.sub.1 and R.sub.2, considered independently, represent hydrogen or a substituent occupying one of the free positions of the benzene ring and selected from the group comprising halogens, a lower alkyl group, a lower alkoxy group, a hydroxyl group, a thiol group, a nitro group and an optionally substituted amino group;Y represents oxygen, sulfur or a group --NH--; andR.sub.3 is an amino groupApplication: agonists of the cholinergic receptors.Type: GrantFiled: January 25, 1990Date of Patent: December 11, 1990Assignee: Societe Anonyme: SanofiInventors: Kathleen Biziere, Camille G. Wermuth, Paul Worms, Jean-Jacques Bourguignon
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Patent number: 4971967Abstract: Novel quinolinecarboxylic acid derivatives of the formula: ##STR1## wherein Z is ##STR2## in which R.sup.1 and R.sup.2 are each hydrogen atom or a lower alkyl, R.sup.3 is hydrogen atom, hydroxy or a lower alkyl and R.sup.4 is hydrogen atom, hydroxy, amino, aminomethyl, a (lower alkyl)aminomethyl or a di(lower alkyl)aminomethyl, and a pharmaceutically acceptable salt thereof. The compounds have excellent antibacterial activities and are useful as an antibacterial agent.Type: GrantFiled: March 14, 1990Date of Patent: November 20, 1990Assignee: Kanebo LtdInventors: Hirosato Kondo, Masahiro Taguchi, Yoshimasa Inoue, Fumio Sakamoto
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Patent number: 4916137Abstract: This disclosure described novel 5-(substituted-amino)-8-(substituted-phenyl)-3H,6H, -1,-4,5a,8a-tetraazaacenaphthylen-3-ones useful for the treatment of cognitive and related neural behavioral disorders in mammals.Type: GrantFiled: November 30, 1988Date of Patent: April 10, 1990Assignee: American Cyanamid CompanyInventors: Joseph W. Epstein, Jeremy I. Levin, Shin S. Tseng
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Patent number: 4904658Abstract: Substituted-6H,8H-pyrimido[1,2,3-cd]purine-8,10(9H)-diones and substituted-6H,10H-pyrimido[1,2-cd]purin-10-ones which are useful as cognition enhancing agents, anxiolytic agents and/or antihypertensive agents in the treatment of cognitive and relative neutral behavioral problems, anxiety and hypertension in mammals.Type: GrantFiled: April 15, 1988Date of Patent: February 27, 1990Assignee: American Cyanamid CompanyInventors: Shin S. Tseng, Joseph W. Epstein, Jeremy I. Levin
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Patent number: 4889854Abstract: The compounds of the formula ##STR1## wherein Ra, Rb, Rc, Rd, Re and Rf are as hereinafter described, compounds of formula A which have one or more basic substituents are described and have valuable pharmacological properties. In particular, they have muscle relaxant, sedative-hypnotic, anxiolytic and/or anticonvulsive activity and can be used for the control or prevention of muscle tensions, stress conditions, insomnia, anxiety states and/or convulsions.Type: GrantFiled: May 25, 1988Date of Patent: December 26, 1989Assignee: Hoffman-La Roche Inc.Inventor: Ulrich Widmer
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Patent number: 4871732Abstract: The present invention is directed to a group of compounds which are imidazo[2,1-b]quinazolin-5(3H)-ones, related tricyclic compounds, and pharmaceutically acceptable salts thereof. These compounds are useful as bronchodilators. These compounds are prepared by the reaction of an appropriate hydrazine with an appropriate 1-substituted-2-methyl-2-imidazoline or chemically equivalent compound.Type: GrantFiled: September 22, 1988Date of Patent: October 3, 1989Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Norton P. Peet, Shyam Sunder
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Patent number: 4855297Abstract: The compounds of the formula ##STR1## wherein Ra,R.sub.b,R.sub.c R.sub.d are defined in the specification and pharmaceutically acceptable addition salts are disclosed.The compounds of formula I have valuable pharmacological properties and can be used for the control or prevention of illnesses. In particular, they have muscle relevant, seditive-hypnotic, anxiolytic and/or anticonvulsive activity and can accordingly be used in the control or prevention of muscle tensions, stress conditions, isomnia, anxiety states and/or convulsions.Type: GrantFiled: December 4, 1986Date of Patent: August 8, 1989Assignee: Hoffman-La Roche Inc.Inventors: Ulf Fischer, Fernand Schneider, Widmer Ulrich
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Patent number: 4838925Abstract: This invention relates to novel heterocyclic carbonyl sulfonamides which are particularly useful as agricultural chemicals.Type: GrantFiled: September 25, 1987Date of Patent: June 13, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventor: Chi-Ping Tseng
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Patent number: 4837239Abstract: This invention is directed to a formulation of cardiotonic phosphodiesterase inhibitors with a water-soluble vitamin, comprising a lyophilization step performed on a solution of the complex in an aqueous/organic solvent system. The formulation results in a complex that has been found to have enhanced solubility (over the compound alone) in a parenterally or orally acceptable solvent, and the lyophilization process yields a product with superior stability permitting an extended shelf life.Type: GrantFiled: October 14, 1986Date of Patent: June 6, 1989Assignee: Syntex (U.S.A.) Inc.Inventors: Eric J. Benjamin, Gary C. Visor
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Patent number: 4831029Abstract: The invention relates to condensed cyclic triazole derivatives of the general Formula I ##STR1## and pharmaceutically acceptable salts thereof. The compounds of the general Formula I possess useful sedative and tranquillant properties and exhibit particularly spasmolytic, motility inhibiting, and narcosis potentiating, yohimbine potentiating and local anaesthetic and also weak reserpine ptosis inhibiting effect.Type: GrantFiled: November 5, 1987Date of Patent: May 16, 1989Inventors: Jozsef Reiter, Endre Rivo, Klara Reiter nee Esess, Marton Fekete, Frigyes Gogenyi, Lujza Petocz, Istvan Gacsalyi, Istvan Gyertyan
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Patent number: 4788186Abstract: The present invention refers to new s-triazolo[3,4-a]phthalazine derivatives, to the process for their preparation and to the pharmaceutical compositions containing them.Type: GrantFiled: October 20, 1987Date of Patent: November 29, 1988Assignee: Gruppo Lepetit S.p.A.Inventors: Emilio Occelli, Domenico Barone, Giorgio Tarzia, Adele Giunta
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Patent number: 4783461Abstract: The present invention is directed to new 3,6-disubstituted-1,2,4-triazolo[3,4-a]phthalazine derivatives of formula I ##STR1## wherein R represents phenyl or substituted phenyl, n is 1 or 2, R.sup.1 is an amino group of formula NR.sup.4 R.sup.5, or an alkoxy of cycloalkoxy group of formula OR.sup.6, and R.sup.2 and R.sup.3 represent hydrogen, halogen, (C.sub.1 -C.sub.4)alkyl or (C.sub.1 -C.sub.4)alkoxy, to the process for their preparation and to the pharmaceutical compositions containing them. The compounds of the present invention are as active as anti-anxiety substances.Type: GrantFiled: July 11, 1984Date of Patent: November 8, 1988Assignee: Gruppo Lepetit S.p.A.Inventors: Emilio Occelli, Giorgio Tarzia
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Patent number: 4762840Abstract: Novel pyrimido[2,1-b]benzothiazoles of the formula ##STR1## wherein R and R.sub.3 are individually selected from the group consisting of hydrogen and alkyl of 1 to 6 carbon atoms or taken together with the carbon to which they are attached form a cycloalkyl of 3 to 6 carbon atoms, R.sub.1 is selected from the group consisting of hydroxy, alkoxy of 1 to 12 carbon atoms, cycloalkyl of 7 to 12 carbon atoms, and ##STR2## R.sub.5 and R.sub.6 are individually selected from the group consisting of hydrogen and alkyl of 1 to 6 carbon atoms or taken together with the nitrogen form piperidino or morpholino, R.sub.Type: GrantFiled: July 31, 1986Date of Patent: August 9, 1988Assignee: Roussel UclafInventors: David A. Rowlands, Julian M. C. Golec, Saroop S. Matharu, Peter W. Hairsine
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Patent number: 4716159Abstract: The present invention is directed to pyridazino[4,3-c]isoquinolines of Formula I ##STR1## wherein R represents methyl, phenyl or substituted phenyl groups, R.sub.1 represents inter alia amino or substituted amino, alkoxy or cycloalkoxy groups, having pharmacological activity, to process for preparing them and to the pharmaceutical compositions containing them. The compounds of the invention possess anti-anxiety activity.Type: GrantFiled: July 30, 1986Date of Patent: December 29, 1987Assignee: Gruppo Lepetit, S.p.A.Inventor: Emilio Toja
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Patent number: 4678499Abstract: Benzenesulfonamide compounds such as N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl-4 -oxo-1-phenyl-indeno[1,2-C]-pyrazole-5-sulfonamide and N-[(4-methoxy-6-methyl-pyrimidin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl- 4-oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide, agricultural compositions containing them, and their herbicidal utility are disclosed.Type: GrantFiled: January 30, 1986Date of Patent: July 7, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventors: Robert J. Pasteris, Ramaurthi Muthukrishnan
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Patent number: 4670434Abstract: This invention relates to compounds of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein the various substituents are defined herein. These compounds are cyclic AMP phosphodiesterase inhibitors useful as antithrombotic and inotropic agents in mammals.Type: GrantFiled: November 14, 1985Date of Patent: June 2, 1987Assignee: Syntex (U.S.A.) Inc.Inventor: Michael C. Venuti
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Patent number: 4652646Abstract: Novel triazolopyrimidine compounds represented by the formula (I) and physiologically acceptable salts thereof are disclosed. These compounds have an excellent anti-allergic activity in oral administration and are useful for treatment and prophylaxis of allergic diseases such as bronchial asthma, allergic gastro-intestinal disorders, allergic rhinitis, hay fever, urticaria and the like.Type: GrantFiled: April 25, 1985Date of Patent: March 24, 1987Assignee: Daiichi Seiyaku Co., Ltd.Inventors: Sumiro Isoda, Norio Suzuki, Tamotsu Miwa, Shunzo Aibara
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Patent number: 4638066Abstract: Compounds of formula (I), ##STR1## or an N-oxide or pharmaceutically acceptable salt thereof, wherein R.sub.1 is hydrogen, C.sub.1-7 alkyl, C.sub.3-7 cycloalkyl, C.sub.4-7 cycloalkenyl or C.sub.1-4 alkyl substituted by C.sub.2-7 alkenyl, C.sub.2-7 alkynyl, C.sub.3-7 cycloalkyl, hydroxy, thiol, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, carboxy, C.sub.1-4 alkoxycarbonyl, C.sub.1-4 alkanoyl, amino optionally substituted by one or two C.sub.1-4 alkyl or by C.sub.4-6 polymethylene optionally containing an oxygen or nitrogen atom, aminocarbonyl optionally N-substituted by one or two C.sub.1-4 alkyl, or benzoyl or phenyl either being optionally ring-substituted by C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or trifluoromethyl, R.sub.2 and R.sub.3 are the same or different and are hydrogen, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, halogen or trifluoromethyl, m is 1 to 3 and n is 1 or 2, the hydrogen atom bonded to the C.sub.a carbon atom being trans to the hydrogen atom bonded to the C.sub.Type: GrantFiled: December 20, 1984Date of Patent: January 20, 1987Assignee: Beecham Group p.l.c.Inventors: Laramie M. Gaster, Barry S. Orlek
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Patent number: 4610987Abstract: Imidazoquinazolin-2-one compounds having platelet aggregation inhibitory activity is disclosed. These compounds have high water-solubility and reduced influences on the circulatory system and are useful for treatment and prophylaxis of intravascular thromboembolism and temporary ischemia as well as prevention of thrombus upon use of prosthetic apparatus.Type: GrantFiled: July 16, 1984Date of Patent: September 9, 1986Assignee: Daiichi Seiyaku Co., Ltd.Inventor: Fumiyoshi Ishikawa
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Patent number: 4602019Abstract: Substituted 2,5-dihydro- and 2,4,4a,5-tetrahydro-3H-indeno[1,2-c]pyridazin-3-ones and pharmaceutically acceptable salts thereof are useful as cardiotonic and antihypertensive agents.Type: GrantFiled: February 2, 1984Date of Patent: July 22, 1986Assignee: Warner-Lambert CompanyInventors: Ila Sircar, James A. Bristol
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Patent number: 4598148Abstract: What are disclosed are pyrimido(6,1-a)isoquinolin-4-one compounds useful as hypotensive agents, bronchodilators, and anti-allergenics, intermediates useful in their preparation, and method for making the compounds and intermediates.Type: GrantFiled: September 19, 1984Date of Patent: July 1, 1986Assignee: Hoechst AktiengesellschaftInventors: Bansi Lal, Horst Dornauer, Bani K. Bhattacharya, Alihussein N. Dohadwalla, Noel J. de Souza
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Patent number: 4585772Abstract: The invention relates to pharmaceutical compositions containing active ingredients of Formula (I) and methods for the use of said compositions to treat cardiac insufficiencies. Also included in the invention are methods of the manufacture of said active ingredients of Formula (I). The invention includes, additionally, compounds of Formula (I).Type: GrantFiled: July 11, 1983Date of Patent: April 29, 1986Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Siegfried Goldmann, Gunter Thomas, Bernward Garthoff
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Patent number: 4584374Abstract: 4-Thioxobenzopyrano[2,3-d]-pyrimidine derivatives of the general formulae Ia or Ib ##STR1## are described. Compounds Ia and Ib are tautomers and are valuable intermediates for the preparation of 5H-[1]-benzopyrano[2,3-d]pyrimidine derivatives having ulcer-protective action without inhibition of secretion.Type: GrantFiled: September 24, 1984Date of Patent: April 22, 1986Assignee: Warner-Lambert CompanyInventors: Gerhard Satzinger, Hubert Barth, Johannes Hartenstein, Manfred Herrmann, Edgar Fritschi, Ilse-Dore Schutt
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Patent number: 4579847Abstract: Amino derivatives of benzylidene-Pyrrolo[2,1-b] Quinazolines are provided, together with pharmaceutical compositions containing them. The compounds and the compositions have pharmaceutical utility and are particularly useful as anti allergy agents.Type: GrantFiled: December 14, 1984Date of Patent: April 1, 1986Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Gianfederico Doria, Carlo Passarotti, Maria L. Corno
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Patent number: 4578380Abstract: The invention relates to 5H-[1]benzopyrano-[2,3-d]pyrimidine derivatives of the general formula I ##STR1## which may be prepared by means of a new chemical process and have a protective effect similar to that of cimetidine, but do not exhibit the undesired side effects of antisecretory agents. The invention is based on a new mucoprotective mode of action which prevents lesions of the mucous membrane epithelium to arise.Type: GrantFiled: September 24, 1984Date of Patent: March 25, 1986Assignee: Warner-Lambert CompanyInventors: Gerhard Satzinger, Hubert Barth, Johannes Hartenstein, Manfred Herrmann, Edgar Fritschi, Ilse-Dore Schutt
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Patent number: 4564610Abstract: Substituted 5H-pyrimido[5,4-b]indoles of Formula I ##STR1## wherein R.sup.2 is halogen; the oxadiazolyl group ##STR2## wherein R" is lower alkyl with up to 3 carbon atoms; C.sub.1-5 -alkyl, cycloalkyl, aralkyl, or aryl; OR.sup.I, SO.sub.n R.sup.I with n being 0, 1, or 2, or ##STR3## wherein R.sup.I is hydrogen, C.sub.1-5 -alkyl, cycloalkyl, aralkyl, or aryl; ##STR4## wherein R.sup.II and R.sup.III are hydrogen, C.sub.1-5 -alkyl, C.sub.3-5 -alkenyl, cycloalkyl, aralkyl, aryl, or, with the connecting N-atom, a 5- or 6-membered heterocyclic ring; andR.sup.A is hydrogen; the oxadiazolyl group ##STR5## wherein R" is lower alkyl with up to 3 carbon atoms; halogen, nitro, OR.sup.I, SO.sub.n R.sup.I with n being 0, 1, or 2, ##STR6## wherein R.sup.I is hydrogen, C.sub.1-5 -alkyl, cycloalkyl, aralkyl, or aryl; ##STR7## wherein R.sup.II and R.sup.III are hydrogen, C.sub.1-5 -alkyl, cycloalkyl, C.sub.3-5 -alkenyl, aralkyl, aryl, or, with the connecting N-atom, a 5- or 6-membered heterocyclic ring; orPO(OR).sub.Type: GrantFiled: December 16, 1983Date of Patent: January 14, 1986Assignee: Schering AktiengesellschaftInventors: Dieter Rahtz, Andreas Huth, Ralph Schmiechen, Dieter Seidelmann, Wolfgang Kehr, Herbert H. Schneider, Claus T. Braestrup
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Patent number: 4539318Abstract: Novel tertiary aminohydroxypropoxy substituted thiadiazole compounds exhibit .alpha..sub.1 -adrenoceptor and serotonin antagonism and are also useful as antihypertensive agents.Type: GrantFiled: June 4, 1984Date of Patent: September 3, 1985Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Gerald S. Ponticello
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Patent number: 4526890Abstract: 3,6,7,8-Substituted-s-triazolo-pyridazine compounds such as 7,8-dimethyl-6-morpholino-3-methyl-s-triazolo[4,3-b]pyridazine or 7,8-dimethyl-6-(1-pyrrolidinyl)-3-(isopropyl)-s-triazolo-[4,3-b]pyridazine are prepared by the reaction of a carboxylic acid with a substituted 3-hydrazino-6-halo-pyridazine followed by the reaction of the resulting 6-halotriazolopyridazine with a corresponding base. The compounds have pharmacological activity as bronchodilators.Type: GrantFiled: April 7, 1981Date of Patent: July 2, 1985Assignee: The Dow Chemical CompanyInventors: Norton P. Peet, Shyam Sunder
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Patent number: 4510141Abstract: The invention relates to novel polycyclic polyazaheterocycles having psychopharmacological properties, especially antidepressive and anxiolytic activity, corresponding to the formula I ##STR1## in which R.sub.1 and R.sub.2 each represents, independently of the other, hydrogen, lower alkyl or hydroxy-lower alkyl, or together represent lower alkylene or ethyleneoxyethylene, ethyleneazaethylene or N-lower alkyl- or N-(2-hydroxy-lower alkyl)-ethyleneazaethylene, R.sub.3 represents hydrogen or a lower aliphatic hydrocarbon radical or a saturated lower cycloaliphatic hydrocarbon radical or unsubstituted or substituted phenyl, R.sub.4 and R.sub.Type: GrantFiled: September 13, 1982Date of Patent: April 9, 1985Assignee: Ciba-Geigy CorporationInventor: Roland Heckendorn
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Patent number: 4503227Abstract: The invention relates to chromogenic dihydroquinazolines of the general formula ##STR1## wherein the ring A is a monocyclic or polycyclic, unsubstituted or substituted heterocyclic radical which may contain further heteroatoms as ring members,each of X.sub.1, X.sub.2 and Y independently of one another is hydrogen, halogen, lower alkyl, lower alkanoylamino, or a group of the formula ##STR2## X.sub.3 is hydrogen, halogen, lower alkyl or lower alkoxy; each of R.sub.1, R.sub.2, R.sub.3, R.sub.4, Z.sub.1 and Z.sub.2 independently of one another is C.sub.1 -C.sub.12 alkyl which is unsubstituted or substituted by halogen, hydroxyl, cyano or lower alkoxy, or is cycloalkyl, phenyl, or phenyl or benzyl each substituted by halogen, nitro, lower alkyl or lower alkoxy, and the radicals R may also be hydrogen; oreach pair of substituents (R.sub.1 and R.sub.2), (R.sub.3 and R.sub.4) and (Z.sub.1 and Z.sub.Type: GrantFiled: April 18, 1983Date of Patent: March 5, 1985Assignee: Ciba-Geigy CorporationInventors: Heinz Balli, Sigmund Gunzenhauser, Ian J. Fletcher, Davor Bedekovic
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Patent number: 4490371Abstract: Compounds according to the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein: n is an integer of 1 to 6;R.sub.1 is hydrogen or alkyl of 1 to 4 carbons;R.sub.2 is hydrogen or R.sub.1 and R.sub.2 are combined to form an oxo group;R.sub.3 is hydrogen, alkyl of 1 to 6 carbons, phenyl, benzyl or hydroxy lower alkyl;R.sub.4 is hydrogen, alkyl of 1 to 6 carbons, benzyl, or hydroxy lower alkyl;Y is hydrogen, alkyl of 1 to 4 carbon atoms, halo or lower alkoxy;A is an amide forming group wherein the nitrogen substituents are: hydrogen; alkyl of 1 to 6 carbon atoms; hydroxyalkyl of 1 to 6 carbon atoms and its aliphatic acylates of 1 to 6 carbon atoms or aryl acylates of 7 to 12 carbon atoms; cycloalkyl of 3 to 7 carbon atoms or cycloalkyl lower alkyl of 4 to 11 carbon atoms wherein the cycloalkyl ring is unsubstituted or substituted with a lower alkyl, lower alkoxy, OH, --OCOR.sub.5, halo, --NH.sub.2, --N(R.sub.5).sub.2, --NHCOR.sub.5, --COOH, or --COO(R.sub.5) group wherein R.sub.Type: GrantFiled: February 16, 1983Date of Patent: December 25, 1984Assignee: Syntex (U.S.A.) Inc.Inventors: Gordon H. Jones, Michael C. Venuti, Robert Alvarez, John J. Bruno
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Patent number: 4486221Abstract: Thiazolo[2,3-b]quinazolones of the formula ##STR1## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the meanings given in the description, are used for influencing plant growth and for controlling undesirable plant growth.Type: GrantFiled: October 20, 1982Date of Patent: December 4, 1984Assignee: BASF AktiengesellschaftInventors: Guenther Seybold, Bruno Wuerzer
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Patent number: 4482556Abstract: What are disclosed are pyrimido (6,1-a)isoquinolin-4-one compounds useful as hypotensive agents, bronchodilators, and anti-allergenics, intermediates useful in their preparation, and methods for making the compounds and intermediates.Type: GrantFiled: March 26, 1980Date of Patent: November 13, 1984Assignee: Hoechst AktiengesellschaftInventors: Bansi Lal, Horst Dornauer, Bani K. Bhattacharya, Alihussein N. Dohadwalla, Noel J. de Souza