At Least One Of The Ring Hetero Atoms Is Chalcogen Patents (Class 546/83)
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Patent number: 5075442Abstract: Oxophthalazinyl acetic acids having benzothiazole side chains are prepared by reacting an oxophthalazinyl thioacetamide acetate with hydrogen sulfide and a nitrophenyl compound having a reactive group such that the benzothiazole side chain may be formed by ring closure involving the thiocaetamide group. The oxophthalazinyl thioacetamide may be prepared by reacting the corresponding cyanomethyloxophthalazinyl acetate with hydrogen sulfide in the presence of tertiary amines. Analogous indazole and oxopyridopyridazinone acetic acids may be prepared similarly, as well as oxophthalazinyl, indazole and oxopyridopyridazinone acetic acids having thiazolopyridinyl side chains.Type: GrantFiled: June 15, 1990Date of Patent: December 24, 1991Assignee: Pfizer Inc.Inventors: Banavara L. Mylari, William J. Zembrowski
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Patent number: 5071848Abstract: Isothiazolo-quinoline derivatives are described which are cytotoxic for various tumor cell lines and are useful in the treatment of neoplastic diseases.Type: GrantFiled: October 23, 1989Date of Patent: December 10, 1991Assignee: Abbott LaboratoriesInventors: Daniel Tim-Wo Chu, Jacob J. Plattner, Linus L. Shen, Larry L. Klein
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Patent number: 5071853Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.Type: GrantFiled: February 27, 1990Date of Patent: December 10, 1991Inventors: Christopher F. Bigge, Sheryl J. Hays, Graham Johnson, Perry M. Novak, Daniel F. Ortwine
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Patent number: 5062881Abstract: 2-(1-Substituted-2-imidazolin-2-yl)benzoic and nicotinic acids, and derivatives thereof, which are effective in the control of undesirable plant species are described. Also described are a method for the herbicidal use of the compounds and a method for their preparation.Type: GrantFiled: December 20, 1989Date of Patent: November 5, 1991Assignee: American Cyanamid CompanyInventor: Michael A. Guaciaro
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Patent number: 5036075Abstract: This invention relates to a compound of the formula: ##STR1## in which R.sub.1 representsa 1,2,3,6-tetrahydro-1-pyridyl radical substituted in the 4-position.a 1-piperazinyl radical substituted in the 4-position.a piperidino radical substituted in the 4-positioneither:R.sub.2 and R.sub.3, which are identical, represent a hydrogen or halogen atom and R.sub.4 represents a hydrogen atom orR.sub.2 and R.sub.4 represent a hydrogen atom and R.sub.3 represents a halogen atom or an acetylamino radical orR.sub.2 and R.sub.3 represent a hydrogen atom and R.sub.4 represents a halogen atom and R.sub.5 represents a --CH.dbd. group.or R.sub.2, R.sub.3 and R.sub.4 represent a hydrogen atom and R.sub.5 represents a nitrogen atom.R.sub.Type: GrantFiled: November 6, 1990Date of Patent: July 30, 1991Assignee: Rhone-Poulenc SanteInventors: Marie-Therese Comte, Claude Gueremy, Jean-Luc Malleron, Serge Mignani, Jean-Francois Peyronel, Alain Truchon
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Patent number: 5034531Abstract: Novel polycyclic pyranyl compounds, pharmaceutical compositions, and their use as anti-viral agents are disclosed.Type: GrantFiled: December 23, 1988Date of Patent: July 23, 1991Assignee: Schering CorporationInventors: Richard J. Friary, John H. Schwerdt, Ashit K. Ganguly
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Patent number: 5026856Abstract: Isoindoline derivatives represented by the formula (I) and their salts are disclosed. ##STR1## There are many varieties for the compound depending on the types of residues R.sup.1 -R.sup.9 and X. The compounds can be prepared from quinoline derivatives of the formula (II) and an isoindoline derivatives of the formula (III). The compounds of formula (I) and their salts have excellent antibacterial activities against both gram positive and gram negative microorganisms. They can be used as a medicine, an agrichemical, and a food preservative.Type: GrantFiled: May 23, 1989Date of Patent: June 25, 1991Assignee: Wakunaga Seiyaku Kabushiki KaishaInventors: Takashi Yatsunami, Akira Yazaki, Satoshi Inoue, Hitoshi Yamamoto, Masaharu Yokomoto, Jun Nomiyama, Shuichiro Noda
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Patent number: 5026711Abstract: Compounds represented by the general formula: ##STR1## in which R.sub.1 and R.sub.2 are selected from hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkenyl , phenyl or benzyl or R.sub.1 and R.sub.2 form together with the nitrogen atom to which they are attached a C.sub.4 -C.sub.8 saturated heterocycle, R.sub.3 is selected from hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl or C.sub.7 -C.sub.9 phenyl-alkyl, R.sub.4 is selected from hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.5 and R.sub.6 are selected from hydrogen or halogen, C.sub.1 -C.sub.3 or alkoxy, nitro or trifluoromethyl; Z is selected from OH, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.4 alkyl, benzyl, C.sub.4 -C.sub.6 aryl with or without a heteroatom, or NR.sub.8 R.sub.9, R.sub.8 and R.sub.9 being selected from hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl or benzyl; R.sub.10 is selected from hydrogen, C.sub.1 -C.sub.Type: GrantFiled: June 6, 1989Date of Patent: June 25, 1991Assignee: SanofiInventors: Etienne Mendes, Jean-Claude Vernieres, Peter E. Keane, Andre Bachy
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Patent number: 5025096Abstract: Indole and indole derivatives are prepared by contacting under mild reaction conditions an N-(2-toly)formidate, N-(3-methyl-2-pyridyl)formimidate, or N-methyldiazyl formimidate with an alkali metal amide.Type: GrantFiled: August 22, 1985Date of Patent: June 18, 1991Assignee: Mine Safety Appliances CompanyInventors: Kuen-Wai Chiu, Lin-Chen Yu, John R. Strickler
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Patent number: 4985430Abstract: There are disclosed a 9-acylamino-tetrahydroacridine derivative represented by the following formula (I): ##STR1## wherein R ##STR2## are as defined in the specification, its optical antipode or pharmaceutically acceptable acid addition salt thereof and a memory enhancing agent containing the same as an active ingredient.Type: GrantFiled: December 2, 1988Date of Patent: January 15, 1991Assignee: Mitsubishi Kasei CorporationInventors: Shuji Morita, Ken-Ichi Saito, Kunihiro Ninomiya, Akihiro Tobe, Issei Nitta, Mamoru Sugano
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Patent number: 4977160Abstract: 7- or 8-Substituted, partially hydrogenated pyrazolo[3,4-g]quinoline, thiazolo[4,5-g]quinoline, oxazolo[4,5-g]quinoline, and pyrrolo[3,4-g]quinoline derivatives, and 8- or 9-substituted, partially hydrogenated pyrido[2,3-g]quinazoline derivatives are D-2 dopamine agonists. 6-Oxo-1-substituted-octahydroquinolines and 6-oxo-1-substituted-decahydroquinolines which are additionally substituted in the 3- or 4-position are intermediates useful in preparation of the dopamine agonists. Acetals of 4,6-dioxo-1-substituted-decahydroquinoline 3-carboxylic acid esters enable synthesis of the foregoing compounds.Type: GrantFiled: February 16, 1989Date of Patent: December 11, 1990Assignee: Eli Lilly and CompanyInventors: Diane L. Huser, John M. Schaus
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Patent number: 4975435Abstract: The present invention comprises certain quinoline lactams of formula I; pharmaceutically acceptable salts of the compounds of formula I; pharmaceutical compositions containing a compound of formula I, or a pharmaceutically acceptable salt thereof, for use in the treatment of anxiety; and processes for the manufacture of the compounds of formula I, as well as intermediates for use in such manufacture.Type: GrantFiled: April 29, 1987Date of Patent: December 4, 1990Assignee: ICI Americas Inc.Inventors: James B. Campbell, Edward J. Warawa
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Patent number: 4963677Abstract: A compound of the formula ##STR1## and pharmaceutically acceptable salts thereof, in which A is --N.dbd.N--NH--, --X--C(R.sub.2).dbd.N--, --N.dbd.C(R.sub.2)--X--, --X--C(R.sub.2)--CH(R.sub.2).dbd.N-- or --N.dbd.C(R.sub.2)--CH(R.sub.2)--X--, wherein X is sulphur, oxygen or nitrogen and R.sub.2 is provided that where two R.sub.2 -groups are present in the A group one of the R.sub.2 groups is hydrogen, amino, substituted amino, C.sub.1-6 alkyl, substituted acylamino or one of the following groups: ##STR2## wherein R.sub.a is hydrogen, amino, substituted amino, C.sub.1-6 alkoxy, heterocyclic five membered ring or --NHCOR', wherein R' is C.sub.1-6 alkyl, aryl or heterocyclic five membered ring, R.sub.b is hydrogen, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio or hydroxy, R.sub.c is hydrogen, C.sub.1-6 alkyl or oxygen and R.sub.d is C.sub.1-6 alkyl or oxygen, R.sub.e is hydrogen, hydroxy or C.sub.1-6 alkoxy, R.sub.f is C.sub.1-6 alkyl, provided that where two R.sub.2 -groups are present in the A group, one of the R.sub.Type: GrantFiled: November 8, 1988Date of Patent: October 16, 1990Assignee: Orion Corporation Ltd.Inventors: Lawrence Sellin, Reijo J. Backstrom, Kalevi E. Heinola, Erkki J. Honkanen, Tord K. W. Langenskiold, Irma O. Ojala, Aino K. Pippuri, Jarmo J. Pystynen
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Patent number: 4954629Abstract: Oxophthalazinyl acetic acids having benzothiazole side chains are prepared by reacting an oxophthalazinyl thioacetamide acetate with hydrogen sulfide and a nitrophenyl compound having a reactive group such that the benzothiazole side chain may be formed by ring closure involving the thioacetamide group. The oxophthalazinyl thioacetamide may be prepared by reacting the corresponding cyanomethyloxophthalazinyl acetate with hydrogen sulfide in the presence of tertiary amines. Analogous indazole and oxopyridopyridazinone acetic acids may be prepared similarly, as well as oxophthalazinyl, indazole and oxopyridopyridazinone acetic acids having thiazolopyridinyl side chains.Type: GrantFiled: May 11, 1989Date of Patent: September 4, 1990Assignee: Pfizer Inc.Inventors: Banavara L. Mylari, William J. Zembrowski
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Patent number: 4929623Abstract: A benzothiazol compound having the formula is disclosed and is effective to inhibit the production of leukotriene. It is useful against allergy, asthma, affections of the skin, allergic rhinitis and affection of a cardiovascular system. ##STR1## in which R20 is ester or amide and --NR5R6 is amino in variety.Type: GrantFiled: June 16, 1988Date of Patent: May 29, 1990Assignee: Eisai Co., Ltd.Inventors: Shinya Abe, Mitsuaki Miyamoto, Masayuki Tanaka, Kozo Akasaka, Kenji Hayashi, Tetsuya Kawahara, Satoshi Katayama, Yoshinori Sakuma, Takeshi Suzuki, Isao Yamatsu
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Patent number: 4927933Abstract: A fogged direct positive photographic silver halide emulsion containing a sensitizing amount of at least one cyanine dye defined above, e.g., cyanine dye containing a 1-phenylindole nucleus substituted in the 2-position with the 3-pyridyl group. The said cyanine dye is also covered. The dye useful in sensitizing the silver halide emulsion useful for fogged direct-positive films.Type: GrantFiled: January 31, 1989Date of Patent: May 22, 1990Assignee: E. I. Du Pont de Nemours and CompanyInventor: Thomas D. Weaver
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Patent number: 4904669Abstract: The invention relates to new thiazolo[4,5-c]quinoline derivatives of the general Formula I ##STR1## and acid addition salts thereof, a process for the preparation of the same and pharmaceutical compositions comprising the said compounds.The substituent definition of the general Formula I is as follows:R stands for hydrogen; a straight or branched chained alkyl group having 2-5 carbon atoms optionally substituted by one or more halogen atom(s); phenyl or phenyl-(lower alkyl) optionally bearing one or more substituent(s) on the phenyl ring;R.sup.1 and R.sup.2 are identical or different and stand for hydrogen, halogen or lower alkyl).The compounds of the general Formula I possess valuable central nervous depressive properties.Type: GrantFiled: November 12, 1986Date of Patent: February 27, 1990Assignee: EGIS GyogyszergyarInventors: Jozsef Knoll, Edit Berenyi nee Poldermann, Katain Budainee Simonyi, Berta Knoll, Zsuzsa Furts, Julia Timar, Gabriella Zsila, Ildiko Niklya, Lujza Petocz, Attila Mandi
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Patent number: 4880814Abstract: The present invention includes compounds represented by the formula: ##STR1## wherein R.sub.1 is a hydroxy, a C.sub.1 to C.sub.6 alkoxy, benzoxy, or an alkylcarbonyloxymethoxy group, or R.sub.3 together with R.sub.1 forms a group of the formula --Y--NH-- where Y is oxygen or sulfur; or R.sub.3 is hydrogen; A is nitrogen or CR.sub.2, where R.sub.2 is hydrogen, or halogen, or R.sub.2 together with R forms a group of the formula --X--CH.sub.2 --CH(R.sub.6)-- or --X--CH.sub.2 --CH.dbd.CH.sub.2, wherein X is CH.sub.2, O, S, NH, or NCH.sub.3, and R.sub.6 is hydrogen, alkyl, or C.sub.1 -C.sub.3 haloalkyl; or R is (1) a C.sub.1 to C.sub.4 alkyl, (2) lower cycloalkyl, (3) alkylamino, (4) haloalkyl, (5) an aromatic heterocyclic ring or (6) a substituted phenyl group; and Z is a carbocyclic group;or a pharmaceutically acceptable salt thereof. The compounds of the present invention are useful as antibacterial agents.Type: GrantFiled: November 13, 1987Date of Patent: November 14, 1989Assignee: Abbott LaboratoriesInventors: Daniel T. Chu, Terry J. Rosen, Curt S. Cooper
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Patent number: 4866061Abstract: Aryl-substituted naphthyridines and pyridopyrazines are disclosed which are useful in treating allergic reactions, inflammation, peptic ulcers and/or hyperproliferative skin disease. Pharmaceutical compositions and methods of treatment employing such compounds are also disclosed.Type: GrantFiled: May 12, 1988Date of Patent: September 12, 1989Assignee: Schering CorporationInventors: David J. Blythin, Ho-Jane Shue
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Patent number: 4826986Abstract: 7- or 8-Substituted, partially hydrogenated pyrazolo[3,4-g]quinoline, thiazolo[4,5-g]quinoline, oxazolo[4,5-g]quinoline, and pyrrolo[3,4-g]quinoline derivatives, and 8- or 9-substituted, partially hydrogenated pyrido[2,3-g]quinazoline derivatives are D-2 dopamine agonists. 6-Oxo-1-substituted-octahydroquinolines and 6-oxo-1-substituted-decahydroquinolines which are additionally substituted in the 3- or 4-position are intermediates useful in preparation of the dopamine agonists. Acetals of 4,6-dioxo-1-substituted-decahydroquinoline 3-carboxylic acid esters enable synthesis of the foregoing compounds.Type: GrantFiled: June 16, 1986Date of Patent: May 2, 1989Assignee: Eli Lilly and CompanyInventors: Diane L. Huser, John M. Schaus
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Patent number: 4810708Abstract: Novel polycyclic quinoline, naphthyridine and pyrazinopyridine derivatives are disclosed which are useful for treating allergic reactions, inflammation, peptic ulcers, hypertension, and hyperproliferative skin diseases and for suppressing the immune response in mammals. Methods for preparing said compounds are also disclosed.Type: GrantFiled: February 17, 1987Date of Patent: March 7, 1989Assignee: Schering CorporationInventors: Ashit K. Ganguly, Richard J. Friary, John H. Schwerdt, Marvin I. Siegel, Sidney R. Smith, Vera A. Seidl, Edmund J. Sybertz
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Patent number: 4803210Abstract: Tricyclic oxazolones enhance myocardial contractile force and are useful as cardiotonics in the treatment of heart failure.Type: GrantFiled: April 14, 1988Date of Patent: February 7, 1989Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Winton D. Jones, Richard A. Schnettler, George P. Claxton, Richard C. Dage
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Patent number: 4778801Abstract: A compound of the formula ##STR1## wherein X is hydrogen, halogen or nitro; Ar is phenyl or naphthyridinyl which may optionally be substituted; and either one of Z.sup.1 and Z.sup.2 is hydrogen and the other is lower alkanoyloxy or hydroxy, each of Z.sup.1 and Z.sup.2 is lower alkoxy, or Z.sup.1 and Z.sup.2 combinedly represent hydroxyimino or oxo; and a salt thereof, act on the central nervous system but are weak in adverse effects such as hypnotic and muscle relaxant effects.Type: GrantFiled: June 29, 1987Date of Patent: October 18, 1988Assignee: Takeda Chemical Industries, Ltd.Inventors: Giichi Goto, Yoshiaki Saji
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Patent number: 4778892Abstract: 3-7-Diheterabicylo[3.3.1]nonanes and derivatives thereof are disclosed. Their method of preparation and use as antiarrhythmic agents is given.Type: GrantFiled: May 11, 1987Date of Patent: October 18, 1988Assignee: Oklahoma State UniversityInventors: Kenneth D. Berlin, Mark D. Thompson, Benjamin J. Scherlag, Gary S. Smith
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Patent number: 4778811Abstract: It has been found that 2-methyl-thiazolo[4,5-c]quinoline and pharmaceutically acceptable acid addition salts and hydrates thereof possess valuable central nervous depressive properties being different from those of benzodiazepines. The invention relates to pharmaceutical compositions comprising as active ingredient 2-methyl-thiazolo[4,5-c]quinoline of the Formula I ##STR1## or a pharmaceutically acceptable acid addition salt or hydrate thereof.Type: GrantFiled: November 12, 1986Date of Patent: October 18, 1988Assignee: EGIS GyogyszergyarInventors: Jozsef Knoll, Lujza Petocz, Attila Mandi, Edit Berenyi nee Poldermann, Katalin Budai nee Simonyi, Berta Knoll, Zsuzsa Furts, Julia Timar, Gabriella Zsila, Ildiko Niklya
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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: 4764518Abstract: The present invention relates to novel antibacterial agents, corresponding to the following general formula I ##STR1## in which: Q represents an aromatic ring,X represents a hydrogen atom or a linear or branched alkyl group,Y represents a linkage or an alkyl group,Z represents a hydrogen atom, an alkyl, aralkyl or heteroalkyl group.These compounds constitute anti-bacterial agents with multiple pharmacological activity.Type: GrantFiled: June 13, 1986Date of Patent: August 16, 1988Assignee: PanmedicaInventors: Claude Laruelle, Marcel Lepant, Bernard Raynier
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Patent number: 4762843Abstract: Hetero [f] fused carbocyclic pyridines are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as dopamine agonists with selectivity for the presynaptic dopamine receptor and are useful as dopaminergic, antipsychotic and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.Type: GrantFiled: July 17, 1987Date of Patent: August 9, 1988Assignee: Warner-Lambert CompanyInventors: Bradley W. Caprathe, Juan C. Jaen, Lawrence D. Wise
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Patent number: 4760073Abstract: Aryl-substituted naphthyridines and pyridopyrazines are disclosed which are useful in treating allergic reactions, inflammation, peptic ulcers and/or hyperproliferative skin disease. Pharmaceutical compositions and methods of treatment employing such compounds are also disclosed.Type: GrantFiled: December 23, 1986Date of Patent: July 26, 1988Assignee: Schering CorporationInventors: David J. Blythin, Ho-Jane Shue
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Patent number: 4753951Abstract: A compound of the formula: ##STR1## (wherein R is phenyl optionally substituted by one or two members selected from the group consisting of trifluoromethyl, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, C.sub.1 -C.sub.5 alkylthio, nitro, amino C.sub.1 -C.sub.5 alkanoylamino and C.sub.1 -C.sub.5 alkoxycarbonyl or 5- or 6-membered heterocyclic group optionally substituted by one or two members selected from the group consisting of halogen, C.sub.1 -C.sub.5 alkyl and C.sub.1 -C.sub.5 alkoxy,Q is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.10 acyl, C.sub.1 -C.sub.5 alkylsulfonyl or C.sub.6 -C.sub.10 arylsulfonyl, ##STR2## R.sup.1, R.sup.2, R.sup.3, and R.sup.4 each is hydrogen, halogen C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy or C.sub.1 -C.sub.Type: GrantFiled: October 17, 1986Date of Patent: June 28, 1988Assignee: Shionogi & Co., Ltd.Inventors: Susumu Takada, Toshio Fujishita, Takashi Sasatani, Akira Matsushita, Masami Eigyo
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Patent number: 4749702Abstract: Novel substituted N-[(4-piperidinyl)alkyl] bicyclic condensed oxazol- and thiazolamines useful as anti-depressives, in the treatment of Parkinson's disease and in the treatment of diseases related with disturbed enterokinesia.Type: GrantFiled: June 23, 1987Date of Patent: June 7, 1988Assignee: Janssen Pharmaceutica N. V.Inventors: Frans E. Janssens, Theophilus T. J. M. Van Offenwert, Raymond A. Stokbroekx, Bernard R. Boar
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Patent number: 4698346Abstract: New quinoline compound, and the corresponding 1,2-; 1,3-; and 1,4-benzodiazines, the quinoline compounds being of the formula: ##STR1## and salts thereof, wherein R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl, halo, trifluoromethyl, amino, lower alkyl amino, lower acylamino, cyano, aryl, aryl/lower alkylene, nitro, lower alkynyl, lower alkenyl, lower alkyl sulfinyl, lower alkyl sulfonyl, lower alkoxycarbonyl, carboxyl, lower alkoxy, lower alkanoyl, or lower alkenoyl,Y is oxygen, sulfur, nitrogen or R.sub.3 N wherein R.sub.3 is hydrogen, lower alkyl, alkenyl, alkynyl, aryl, aralkyl, acyl, aminoalkyl, or carboxyalkyl,Z is oxygen, sulfur or nitrogen,X is cyano, carbalkoxyl, carboxyl, formyloximino, tetrazolyl, carbalkoxyalkyl or carboxyalkyl, andm is 0 or 1, are useful as medicinals, especially for treatment of asthma, and/or as intermediates in the preparation of compounds useful for treating asthma.Type: GrantFiled: July 24, 1986Date of Patent: October 6, 1987Assignee: USV Pharmaceutical CorporationInventors: John H. Musser, Richard E. Brown
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Patent number: 4698347Abstract: Trans-(.+-.)-2- and/or -5-permissibly substituted octahydro-oxazolo[4,5-g]quinolines, acid addition salts thereof and individual enantiomers thereof, useful as dopamine agonists or intermediates of the preparation of dopamine agonists.Type: GrantFiled: December 11, 1986Date of Patent: October 6, 1987Assignee: Eli Lilly and CompanyInventors: John M. Schaus, Robert D. Titus
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Patent number: 4686226Abstract: Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective .alpha..sub.2 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives, ocular antihypertensives, antidiabetics, antiobesity and platelet aggregation inhibitors and modifiers of gastrointestinal motility.Type: GrantFiled: September 3, 1985Date of Patent: August 11, 1987Assignee: Merck & Co., Inc.Inventors: Joel R. Huff, John J. Baldwin, Yojiro Sakurai, Joseph P. Vacca, James P. Guare, Jr.
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Patent number: 4680298Abstract: Substituted quinoline, [1,5]- and [1,8]-naphthyridine and pyrido[2,3-b]pyrazine derivatives are anti-allergic, anti-inflammatory and cytoprotective agents. Methods for their preparation and use are disclosed.Type: GrantFiled: April 9, 1984Date of Patent: July 14, 1987Assignee: Schering CorporationInventor: David J. Blythin
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Patent number: 4675370Abstract: Resins are obtained by Diels-Alder polymerization of a monomer of the formula ##STR1## where R is a hydrogen atom or an aryl group; andL is an aromatic linking group.Type: GrantFiled: April 29, 1986Date of Patent: June 23, 1987Assignee: University of DaytonInventors: Loon-Seng Tan, Fred E. Arnold
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Patent number: 4668671Abstract: This invention describes tricyclic derivatives which are useful as histamine H.sub.1 -antagonists. A particular compound of this invention is 3-[3-(pyrido[3,2-b][1,4]-benzothiazin-10-yl)propylamino]-4-(pyrid-4-ylmeth ylamino)-1,2,5-thiadiazole-1-oxide.Type: GrantFiled: April 23, 1986Date of Patent: May 26, 1987Assignee: Smith Kline & French Laboratories LimitedInventors: Andrew D. Gribble, Robert J. Ife
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Patent number: 4659832Abstract: Trans-(.+-.)-2- and/or -5-permissibly substituted octahydro-oxazolo[4,5-g]quinolines, acid addition salts thereof and individual enantiomers thereof, useful as dopamine agonists or intermediates of the preparation of dopamine agonists.Type: GrantFiled: June 10, 1985Date of Patent: April 21, 1987Assignee: Eli Lilly and CompanyInventors: John M. Schaus, Robert D. Titus
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Patent number: 4647566Abstract: Compounds of the formula formula IA or IB ##STR1## wherein A represents an optionally substituted saturated divalent grouping which together with the two carbon atoms to which it is attached represents a fused 5-, 6- or 7-membered carbocyclic or heterocyclic ring selected from optionally substituted fused cyclopenteno, cyclohexeno, cyclohepteno, dihydrothieno, dihydrothiopyrano, tetrahydrothiepino, dihydrofuro, dihydropyrano, tetrahydrooxepino, dihydropyrrolo, tetrahydropyrido and tetrahydroazepino; R.sub.1 represents lower alkyl, phenyl, or phenyl mono- or disubstituted by lower alkyl, lower alkoxy, halogen or trifluoromethyl; or R.sub.1 represents an aromatic heterocyclic radical selected from e.g. optionally substituted pyridyl, quinolyl, isoquinolyl, pyrimidyl and thiazolyl; R.sub.2, R.sub.3, R.sub.3 ' are hydrogen or lower alkyl; and pharmaceutically acceptable salts; are useful as benzodiazepine receptor modulators for the treatment of nervous system disorders.Type: GrantFiled: January 8, 1986Date of Patent: March 3, 1987Assignee: Ciba-Geigy CorporationInventor: Naokata Yokoyama
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Patent number: 4624955Abstract: There are disclosed compounds having the formula ##STR1## wherein R.sub.1 is hydrogen, loweralkyl, arylloweralkyl, aryl or heteroaryl; R.sub.2 is hydrogen or loweralkyl; R.sub.3 is loweralkyl, loweralkoxyloweralkyl, cycloalkyl, arylloweralkyl or heteroarylmethyl; and R.sub.4 is hydrogen or loweralkyl; or a pharmaceutically acceptable acid addition salt thereof, which are useful as anxiolytic agents, methods for synthesizing them, and pharmaceutical compositions comprising an effective amount of such a compound.Type: GrantFiled: December 23, 1985Date of Patent: November 25, 1986Assignee: Hoechst-Roussel PharmaceuticalsInventor: Gregory M. Shutske
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Patent number: 4622326Abstract: There are disclosed compounds having the formula ##STR1## wherein R.sub.1 is hydrogen, loweralkyl, arylloweralkyl, aryl or heteroaryl; R.sub.2 is hydrogen or loweralkyl; R.sub.3 is loweralkyl, loweralkoxyloweralkyl, cycloalkyl, arylloweralkyl or heteroarylmethyl; and R.sub.4 is hydrogen or loweralkyl; or a pharmaceutically acceptable acid addition salt thereof, which are useful for alleviating pain and lowering blood pressure, methods for synthesizing them, and pharmaceutical compositions comprising an effective amount of such a compound.Type: GrantFiled: December 23, 1985Date of Patent: November 11, 1986Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventor: Gregory M. Shutske
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Patent number: 4621088Abstract: The present invention relates to new N-acyl derivatives of amino acids.These derivatives correspond to the general formula I below: ##STR1## in which A represents a linear or branched, saturated hydrocarbon radical containing from 1 to 6 carbon atoms or a saturated ring containing 6 carbon atoms,X represents a --COOH radical, a --COOAlkyl radical (alkyl from C.sub.1 to C.sub.4), a hydrogen atom or a --CH.sub.3 group when Y is --COOH or --COOAlkyl,Y represents a --COOH radical, a --COOAlkyl radical (alkyl from C.sub.1 to C.sub.4), an --NH.sub.2 group, an --SH group, an --SCH.sub.3 group, a --NH--CH(.dbd.NH)--NH.sub.2 group, a substituted or unsubstituted phenyl group, an indolin-3-yl group or a 5-hydroxyindolin-3-yl group, andQ represents an optionally substituted aromatic ring or an optionally substituted heterocycle containing 1 or 2 nitrogen atoms.Drugs having an antiallergic action.Type: GrantFiled: May 23, 1985Date of Patent: November 4, 1986Assignee: PanmedicaInventors: Claude Laruelle, Marcel Lepant, Bernard Raynier
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Patent number: 4617395Abstract: Quinoline and substituted quinolines are prepared by reacting aniline or a substituted aniline with an .alpha., .beta.-monounsaturated aldehyde in a high-boiling mineral oil by a method in which the high-boiling mineral oil is replaced when it becomes enriched with by-products, and the said mineral oil enriched with by-products is removed.Type: GrantFiled: October 15, 1984Date of Patent: October 14, 1986Assignee: BASF AktiengesellschaftInventors: Toni Dockner, Helmut Hagen, Herbert Krug
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Patent number: 4602014Abstract: Compounds of the formula formula IA or IB ##STR1## wherein A represents an optionally substituted saturated divalent grouping which together with the two carbon atoms to which it is attached represents a fused 5-, 6- or 7-membered carbocyclic or heterocyclic ring selected from optionally substituted fused cyclopenteno, cyclohexeno, cyclohepteno, dihydrothieno, dihydrothiopyrano, tetrahydrothiepino, dihydrofuro, dihydropyrano, tetrahydrooxepino, dihydropyrrolo, tetrahydropyrido and tetrahydroazepino; R.sub.1 represents lower alkyl, phenyl, or phenyl mono- or disubstituted by lower alkyl, lower alkoxy, halogen or trifluoromethyl; or R.sub.1 represents an aromatic heterocyclic radical selected from e.g. optionally substituted pyridyl, quinolyl, isoquinolyl, pyrimidyl and thiazolyl; R.sub.2, R.sub.3, R.sub.3 ' are hydrogen or lower alkyl; and pharmaceutically acceptable salts; are useful as benzodiazepine receptor modulators for the treatment of nervous system disorders.Type: GrantFiled: June 19, 1985Date of Patent: July 22, 1986Assignee: Ciba-Geigy CorporationInventor: Naokata Yokoyama
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Patent number: 4599410Abstract: Methine dyes are disclosed which contain a 2-halo or pseudohalo substituted 1,2,5-oxatellurazole ring fused with an aromatic nucleus, the aromatic nucleus being substituted with a methine linkage terminating in an auxochrome providing a conjugated resonance chromophore. The dyes can be formed by condensing a methine linkage precursor with a compound containing an oxatellurazole ring fused with an aromatic nucleus. The dyes are useful in optical recording elements and in photographic elements.Type: GrantFiled: February 19, 1985Date of Patent: July 8, 1986Assignee: Eastman Kodak CompanyInventor: Wolfgang H. H. Gunther
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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: 4588731Abstract: Novel isoxazoloquinolinones of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, fluorine, chlorine, bromine, alkyl and alkoxy of 1 to 5 carbon atoms, --NO.sub.2 and CF.sub.3 -- and R.sub.1 is phenyl optionally substituted by at least one member selected from the group consisting of halogen and alkyl and alkoxy of 1 to 5 carbon atoms having anxiolytic activity and their preparation and novel intermediates.Type: GrantFiled: June 21, 1985Date of Patent: May 13, 1986Assignee: Roussel UclafInventors: Daniel Humbert, Jean-Claude Gasc, Peter F. Hunt
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Patent number: 4581455Abstract: (1H-Tetrazol-5-yl)tetrazolo[1,5-a]thienopyridines and related compounds which are useful as antiallergic agents are described herein. The compounds are prepared by the reaction of an appropriate halocyano-quinoline with ammonium chloride and an azide such as sodium azide in an inert solvent such as dimethylformamide.Type: GrantFiled: October 10, 1984Date of Patent: April 8, 1986Assignee: Merrell Dow Pharmaceuticals Inc.Inventor: Terry L. Wright
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Patent number: 4575504Abstract: Compounds of the formula ##STR1## wherein A is ##STR2## and R is hydrogen, alkyl of 1 to 5 carbon atoms, alkanoyl of 1 to 5 carbon atoms, alkenyl of 3 to 5 carbon atoms, (alkoxy of 1 to 4 carbon atoms)carbonyl, or aralkyl of 7 to 11 carbon atoms optionally halo-substituted,and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as bradycardiacs.Type: GrantFiled: September 12, 1984Date of Patent: March 11, 1986Assignee: Dr. Karl Thomae GmbHInventors: Robert Sauter, Gerhart Griss, deceased, Wolfgang Grell, Rudolf Hurnaus, Walter Kobinger, Ludwig Pichler
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Patent number: 4563463Abstract: New quinoline compound, and the corresponding 1,2-; 1,3-; and 1,4-benzodiazines, the quinoline compounds being of the formulae: ##STR1## and salts thereof, wherein R is hydrogen, acyl, carboethoxy,(3-methoxyphen)acetyl,(2-phenyl)propionyl, dimethylcarbamoyl or methyl,R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl, halo, trifluoromethyl, amino, lower alkyl amino, lower acylamino, cyano, aryl, aryl/lower alkylene, nitro, lower alkynyl, lower alkenyl, lower alkyl sulfinyl, lower alkyl sulfonyl, lower alkoxycarbonyl, carboxyl, lower alkoxy, lower alkanoyl, or lower alkenoyl,Y is oxygen, sulfur, nitrogen or R.sub.3 N wherein R.sub.Type: GrantFiled: November 2, 1984Date of Patent: January 7, 1986Assignee: USV Pharmaceutical Corp.Inventors: John H. Musser, Richard E. Brown