Ring Nitrogen Is Shared By Two Of The Cyclos Patents (Class 514/294)
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Patent number: 5143912Abstract: The novel pyridone derivatives of the formula ##STR1## wherein Ra is hydrogen or halogen, Rb is --NR.sup.2 R.sup.3 wherein R.sup.2 and R.sup.3 taken together with the nitrogen atom to which they are attached is a 1-azetidinyl, 1-pyrrolidinyl, 1-piperidinyl which is unsubstituted or mono- or disubstituted by lower alkyl, hydroxy, lower alkoxy, lower hydroxyalkyl, lower alkoxyalkyl or phenyl; B and the carbon atom denoted by .alpha. taken together is a group of the formula >C.sub..alpha. --CR.sup.4 .dbd.CH--CH.dbd.CH-- and R.sup.4 is hydrogen, fluorine or chlorine, 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: August 2, 1991Date of Patent: September 1, 1992Assignee: Hoffmann-La Roche, Inc.Inventors: Serge Burner, Ulrich Widmer
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Patent number: 5141945Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkyl or lower alkenyl, R.sup.2 is hydrogen, lower alkyl, or halogen, R.sup.3 is imidazolyl or pyridyl, each of which may have suitable substituents, and R.sup.4 is hydrogen, lower alkyl, lower alkenyl or hydroxy (lower) alkyl and R.sup.5 is hydrogen, hydroxy, or alkanoyloxy, or R.sup.4 and R.sup.5 are linked together to form an additional bond or novel pyridoindole derivatives which are useful as potent in selective antagonists of 5-HT receptors.Type: GrantFiled: September 20, 1989Date of Patent: August 25, 1992Assignee: Fujisawa Pharmaceutical Company, Ltd.Inventors: Masayuki Kato, Kiyotaka Ito, Hisashi Takasugi
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Patent number: 5140023Abstract: An azatetracycle compound useful as 5 HT.sub.3 antagonists of the general formula ##STR1## wherein D is a tetracycle of the structure ##STR2## wherein Ar is an aromatic moiety and B is either NH or O.Type: GrantFiled: April 12, 1991Date of Patent: August 18, 1992Assignee: G. D. Searle & Co.Inventors: Daniel P. Becker, Daniel L. Flynn, Roger Nosal, Dale P. Spangler, Daniel L. Zabrowski
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Patent number: 5114950Abstract: The invention provides amide derivatives of the general formula (I) ##STR1## wherein R.sup.1 is a hydrogen atom or a C.sub.1-6 alkyl group; Y represents a group --(CH.sub.2).sub.m --, where m represents 2, 3 or 4 or a group --X(CH.sub.2).sub.p, where p represents 2 or 3, X represents an oxygen or a sulphur atom or a group NR.sup.5, where R.sup.5 is a C.sub.1-6 alkyl group, and X is attached to the benzene ring moiety of the molecule; and Im represents an imidazolyl group of the formula: ##STR2## wherein one of the groups represented by R.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group; and physiologically acceptable salts and solvates thereof.The compounds of formula (I) are potent and selective antagonists of 5-hydroxytryptamine at 5-HT.sub.Type: GrantFiled: June 13, 1990Date of Patent: May 19, 1992Assignee: Glaxo Group LimitedInventors: Alexander W. Oxford, David E. Bays, David J. Cavalla, Peter C. North
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Patent number: 5114949Abstract: Compounds are disclosed of formula:R.sub.1 --(CH.sub.2).sub.n --Hetin which R.sub.1 represents a residue of formula ##STR1## X represents a hydrogen atom or an alkyl radical, Y represents a hydrogen atom or an alkyl or alkoxy radical,Z represents an alkyl radical,n is equal to 2 or 3,Het represents a substituted piperidino (substituted at the 4-position with a 1-indenylidene, 1-indenyl or 1-indanyl radical or with a chain --(CH.sub.2).sub.m --R.sub.2 or .dbd.CH--R.sub.2), substituted 1,2,3,6-tetrahydro-1-pyridyl (substituted at the 4-position with a chain --(CH.sub.2).sub.m --R.sub.2),m is equal to 1 or 2, andR.sub.2 represents an optionally substituted 2- or 3-indolyl radical, a 1- or 2-indanyl, 1- or 2-indenyl, an optionally substituted 1,2,3,4-tetrahydro-5H-pyrido[4,3-b]indol-2-yl radical, a 1,2,3,4-tetrahydro-3-quinolyl radical, an optionally substituted 1,2,3,4-tetrahydro-2-naphthyl radical or a 1-indolyl radical, their preparation and medicinal products containing them.Type: GrantFiled: November 19, 1990Date of Patent: May 19, 1992Assignee: Rhone-Poulenc SanteInventors: Claude Gueremy, Jean-Luc Malleron, Serge Mignani
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Patent number: 5109007Abstract: A method is provided for attenuating the intoxicating effects of ethyl alcohol in a patient, by administering to a patient in need thereof, an alpha-2 adrenoceptor antagonist compound. Two preferred compounds useful in the present invention, each being a highly potent and selective alpha-2 adrenoceptor antagonist, are atipamezole and idazoxan.Type: GrantFiled: May 10, 1990Date of Patent: April 28, 1992Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Markku Linnoila, Richard G. Lister, Michael J. Durcan
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Patent number: 5104868Abstract: This invention relates to novel tricyclic derivatives of 7-substituted-6-fluoro-1,4-dihydroquinol-4-one-3-carboxylic acids and certain esters and cation salts thereof. The compounds of this invention are substituted at the 7-position by vinyl, W--CH.dbd.CH--, CH.sub.3 C.tbd.C--, W--CH.sub.2 C.tbd.C-- or ##STR1## where W is selected from certain substituted alkyl groups. This invention also relates to antibacterial compositions containing the compounds and methods of using the compounds to treat bacterial disease.Type: GrantFiled: August 29, 1990Date of Patent: April 14, 1992Assignee: Pfizer Inc.Inventor: Paul R. McGuirk
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Patent number: 5102901Abstract: The invention relates to a group of new 3-N substituted carbamoyl-indole derivatives of the formula ##STR1## having an antagonistic activity on 5-HT receptors. The compounds can be used for the treatment of symptoms which are caused by excessive stimulation of said receptors in the gastrointestinal system, the central nervous system, the cardiovascular system, the respiratory system, and for alleviating or preventing withdrawal symptoms which are induced by abuse of drugs.Type: GrantFiled: April 13, 1990Date of Patent: April 7, 1992Assignee: Duphar International Research B.V.Inventors: Ineke van Wijngaarden, Hans H. Haeck, Derk Hamminga, Wouter Wouters
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Patent number: 5086060Abstract: The effects of acne and psoriasis are relived by applying either topically or by oral adminstration, a compound having the structure: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are independently selected from the group consisting of H, Cl, straight or branched alkyl of 1 to 10 carbon atoms, NO.sub.2, COOR.sub.6, CN, OR.sub.6, NR.sub.6 R.sub.7, NR.sub.6 C(.dbd.S)NR.sub.7 R.sub.8, NF.sub.6 COR.sub.7, SO.sub.2 NR.sub.6 R.sub.7, CH(CH.sub.3)COOH, CONR.sub.6 R.sub.7, COR.sub.6, OCONR.sub.6 R.sub.7, NR.sub.6 COONR.sub.7, R.sub.9 OR.sub.6, NR.sub.6 SO.sub.2 R.sub.7, Si(CH.sub.3).sub.3, and NR.sub.6 CONR.sub.7 R.sub.8,R.sub.3 together with R.sub.4 forms a benzo ring or taken together with R.sub.2 forms a benzo or tetrahydrobenzo ring or together with R.sub.2 and R.sub.1 forms a: ##STR2## moiety or together with R.sub.2 forms a ##STR3## moiety or R.sub.2 together with R.sub.1 forms a benzo ring or R.sub.2 together with R.sub.3 forms a ##STR4## moiety, or R.sub.Type: GrantFiled: July 16, 1990Date of Patent: February 4, 1992Assignee: Eastman Kodak CompanyInventors: Neil F. Haley, Xina Nair, Gerard J. Gendimenico, F. Christopher Zusi, R. Thomas Swann
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Patent number: 5084452Abstract: Use of 2-azabicyclo[2.2.2]octane-3-carboxylic acid derivatives and their salts for the production of medicinal products intended for the treatment of arteritis and more especially arteritis of the lower limbs, disorders of the cerebral circulation and more especially disorders of cerebral senescence and migraine, and disorders of vision such as retinal disorders of vascular origin, diabetic retinopathy, chorioretinal atrophy and chorioretinal degeneration.Type: GrantFiled: April 24, 1990Date of Patent: January 28, 1992Assignee: Adir et CompagnieInventor: Bernard Teisseire
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Patent number: 5061712Abstract: Process for the preparation of antibacterial compounds of the formula ##STR1## comprises condensing an oxo compound of the formula ##STR2## with an amino compound of the formula ##STR3## to produce a compound of the formula ##STR4## reacting the compound of the formula (III) with a compound of the formula ##STR5## to give a compound of the formula ##STR6## and then eliminating the amino-protective group ##STR7##Type: GrantFiled: May 25, 1990Date of Patent: October 29, 1991Assignee: Bayer AktiengesellschaftInventors: Uwe Petersen, Andreas Krebs, Thomas Schenke, Klaus Grohe, Michael Schriewer, Ingo Haller, Karl G. Metzger, Rainer Endermann, Hans-Joachim Zeiler
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Patent number: 5059597Abstract: 7-(1-Pyrrolidinyl)-3-quinolone- and -naphthyridone-carboxylic acid derivatives as antibacterial agents and feed additives, of the formula ##STR1## in which X.sup.1 is halogen,X.sup.2 is hydrogen, halogen, amino or other radical,R.sup.1 is alkyl, cycloalkyl, optionally substituted phenyl or other radical,R.sup.2 is hydrogen, alkyl or a dioxolylmethyl radical,R.sup.3 is ##STR2## and A is N, CH, C-halogen, or the like, or forms a bridge with R.sup.1,and addition products thereof.Type: GrantFiled: September 10, 1990Date of Patent: October 22, 1991Assignee: Bayer AktiengesellschaftInventors: Uwe Petersen, Thomas Schenke, Andreas Krebs, Klaus Grohe, Michael Schriewer, Ingo Haller, Karl G. Metzger, Rainer Endermann, Hans-Joachim Zeiler
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Patent number: 5026696Abstract: The invention relates to compounds of the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 together form a C.sub.3-5 alkylene chain and R.sup.3 is a hydrogen atom; orR.sup.1 and R.sup.3 together form a C.sub.2-4 alkylene chain and R.sup.2 is a hydrogen atom;A-B represents the group R.sup.4 R.sup.5 C--CH.sub.2 or R.sup.4 C.dbd.CH;R.sup.4 and R.sup.5, which may be the same or different, each represent a hydrogen atom or a C.sub.1-6 alkyl group; andIm represents an imidazolyl group of formula: ##STR2## wherein one of the groups represented by R.sup.6, R.sup.7 and R.sup.8 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl group and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group; and physiologically acceptable salts and solvates thereof.The compounds are potent and selective antagonists of the effect of 5-HT at 5-HT.sub.Type: GrantFiled: July 18, 1990Date of Patent: June 25, 1991Assignee: Glaxo Group LimitedInventors: Peter C. North, Alexander W. Oxford, David J. Cavalla
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Patent number: 5011846Abstract: The present invention is directed to the use of esters of hexahydro-8-hydroxy-2,6-methano-2H-quinolizin-3(4H)-one and hexahydro-8-hydroxy-2,6-methano-2H-quinolizines in the manufacture of a medicament for the treatment of anxiety, psychosis, glaucoma and for the stimulation of gastric motility.Type: GrantFiled: May 16, 1990Date of Patent: April 30, 1991Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Maurice W. Gittos, Francis P. Miller, Stephen M. Sorensen, John R. Fozard, Paul Moser, Michael G. Palfreyman, Hsien Cheng
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Patent number: 4992446Abstract: Tricyclic quinolizine amides, which have activity as Class III antiarrhythmic agents, acting by prolonging cardiac action potential repolarization. The invention further provides for compositions incorporating the compounds and methods of their use, as well as providing for pharmaceutically acceptable salts of the compounds.Type: GrantFiled: September 5, 1989Date of Patent: February 12, 1991Assignee: G. D. Searle & Co.Inventor: Kerry W. Fowler
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Patent number: 4987137Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof; ##STR1## wherein: R.sub.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen;R.sub.2 and R.sub.3 are both hydrogen or together represent a bond;R.sub.4 is hydrogen and R.sub.5 is hydrogen or R.sub.4 and R.sub.5 together represent an oxo group;R.sub.6 is C.sub.1-7 alkyl substituted by NR.sub.8 R.sub.9 where R.sub.8 and R.sub.9 are independently hydrogen or C.sub.1-4 alkyl or together are C.sub.3-7 polymethylene optionally containing a further heteroatom which is oxygen, sulphur or nitrogen substituted by R.sub.10 where R.sub.10 is hydrogen, C.sub.1-4 alkyl or benzyl, and optionally substituted by one or two C.sub.1-4 alkyl, C.sub.2-5 alkanoyl, C.sub.1-4 alkoxycarbonyl, aminocarbonyl optionally substituted by one or two C.sub.1-6 alkyl groups or by a benzyl group, cyano, phenyl or benzyl and wherein any phenyl or benzyl group is optionally substituted in the phenyl ring by one or two halo, CF.sub.3, C.sub.1-4 alkyl, C.sub.Type: GrantFiled: April 20, 1989Date of Patent: January 22, 1991Assignee: Beecham Wuelfing GmbH & Co., KGInventors: Dagmar Hoeltje, Dietrich Thielke
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Patent number: 4973590Abstract: Known quinolone carboxylic acid derivatives of the formula ##STR1## are treated so as to become readily administrable parenterally, the treatment comprising dissolving the active compound using an acid, allowing the solution to stand for about 0.15 to 150 hours at a temperature from room temperature to the boiling point of the solution, filtering the solution, precipitating the active compound from the solution using a basic reagent, and converting the precipitated active compound into a form which can be administered parenterally.Type: GrantFiled: April 15, 1988Date of Patent: November 27, 1990Assignee: Bayer AktiengesellschaftInventors: Michael Preiss, Ulrich Schorsch, Arthur Haaf, Paul Naab, Rudolf Zerbes
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Patent number: 4968699Abstract: A pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen;R.sub.2 and R.sub.3 are both hydrogen or together represent a bond;R.sub.4 is hydrogen and R.sub.5 is hydrogen or R.sub.4 and R.sub.5 together represent an oxo group;R.sub.6 is phenyl C.sub.1-7 alkanoyl in which the phenyl moiety is optionally substituted by one or two of halogen, nitro, meta- or para-methoxy, methyl or NR.sub.8 R.sub.9 wherein R.sub.8 and R.sub.9 are independently hydrogen or C.sub.1-6 alkyl or R.sub.8 and R.sub.9 together are C.sub.2-6 polymethylene, or 3,4-disubstituted by methylenedioxy or ethylenedioxy; or C.sub.1-7 alkanoyl substituted by NR.sub.10 R.sub.11 where R.sub.10 and R.sub.11 are independently hydrogen or C.sub.1-4 alkyl or together are C.sub.3-7 polymethylene optionally containing a further heteroatom which is oxygen, sulphur or nitrogen substituted by R.sub.12 where R.sub.Type: GrantFiled: December 21, 1987Date of Patent: November 6, 1990Assignee: Beecham-Wuelfing GmbH & Co.Inventors: Dagmar Hoeltje, Ljerka Jozic, Dietrich Thielke
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Patent number: 4933350Abstract: Pyrrolo[2,1-a]isoquinoline derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 each represent cycloalkyl or alkyl, alkenyl or alkynyl which may be halogen-substituted, or optionally substituted aryl or heteroaryl, X represents ethylene or vinylene, R.sup.3 represents a group of the formula:--Y--CH.sub.2 --CH(OH)--CH.sub.2 --COOR.sup.5 IIwherein Y represents carbonyl or hydroxymethylene and R.sup.5 represents hydrogen or optionally substituted alkyl, or R.sup.3 represents a lactone ring, and the symbols R.sup.4 represent hydrogen, halogen, optionally substituted alkyl, alkenyl or alkynyl, optionally substituted aryl or heteroaryl, or a group of the formula R.sup.6 O--, wherein R.sup.6 represents alkyl, aryl or arylalkyl and pharmaceutical properties.Type: GrantFiled: August 9, 1988Date of Patent: June 12, 1990Assignee: May & Baker LimitedInventors: Michael J. Ashton, Donald I. Dron, Garry Fenton, David J. Lythgoe, Christopher G. Newton, David Riddell
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Patent number: 4923879Abstract: Novel quinoline-, naphthyridine-, and benzoxazine-carboxylic acid derivatives with bridged sidechains useful as antibacterial agents are described. Methods for their preparation, formulation, and use in treatment of bacterial infections is also described.Type: GrantFiled: July 31, 1987Date of Patent: May 8, 1990Assignee: Warner-Lambert CompanyInventors: Marland P. Hutt, Jr., John S. Kiely
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Patent number: 4916138Abstract: This invention relates to a solid dispersion composition comprising FR-900506 substance and water-soluble hydroxypropyl methylcellulose which is capable of dispersing the FR-900506 substance, the FR-900506 substance and hydroxypropyl methylcellulose being in the ratio of 1:0:1 to 1:20 by weight.Type: GrantFiled: July 25, 1988Date of Patent: April 10, 1990Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Yoshio Ueda, Fumio Shimojo, Yasuo Shimazaki, Kazutake Kado, Toshiyasu Honbo
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Patent number: 4910193Abstract: Use of a mono or dicyclic carboxylic or heterocyclic carboxylic acid ester or amide of an alcohol or amine nitrogen as a ring atom in free base form or in acid addition or quaternary ammonium salt form as a 5-HT.sub.3 antagonist in the manufacture of a medicament suitable for the treatment of serotonin induced gastrointestinal disturbances.Type: GrantFiled: August 28, 1987Date of Patent: March 20, 1990Assignee: Sandoz Ltd.Inventor: Karl-Heinz Buchheit
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Patent number: 4897391Abstract: Isoquinolinone and isothiochromone derivatives of the general formula ##STR1## are disclosed. These compounds display anti-allergy, antiinflammatory and anti-hyperproliferative activity, which makes them useful for treating related disorders.Type: GrantFiled: June 17, 1988Date of Patent: January 30, 1990Assignee: Schering CorporationInventor: Richard J. Friary
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Patent number: 4889848Abstract: Compounds of the formula ##STR1## wherein Q.sup.1 and the nitrogen atom taken together are a group of the formula >N--CH.sub.2 CH.sub.2 -- (a), >N--CH.sub.2 CH.sub.2 CH.sub.2 -- (b), >N--CH.dbd.CH-- (c), >N--CH.sub.2 --CH.dbd.CH-- (d), >N--CH.sub.2 --S(O).sub.p -- (e), >N--CH.sub.2 CH.sub.2 --S(O).sub.p -- (f) or >N--CH.dbd.CH--S(O).sub.p -- (g), p is the integer 0, 1 or 2, Ra is a phenyl, pyridyl or thienyl group which is optionally substituted by halogen, trifluoromethyl, nitro, lower alkyl or lower alkoxy, Rb and Rc each, independently, are hydrogen, halogen, trifluoromethyl, lower alkyl, lower alkoxy or nitro and the dotted line signifies an optional bond, or Rb and Rc together with the carbon atom denoted by .alpha. are a group of the formula >C.alpha.--S--CH.dbd.CH-- (h), >C.alpha.--CH.dbd.CH--S-- (i) or >C.alpha.--CH.dbd.CH--CH.dbd.Type: GrantFiled: January 5, 1988Date of Patent: December 26, 1989Assignee: Hoffmann-La Roche Inc.Inventors: Ulf Fischer, Fernand Schneider, Ulrich Widmer
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Patent number: 4861782Abstract: Circulation active compounds of the formula ##STR1## in which R.sup.1 is phenyl or heterocyclyl substituted by nitro, trifluoromethyl or other radicals,R.sup.2 is optionally substituted alkyl or other radicalR.sup.3 and R.sup.5 are hydrogen, methyl or other radicals,R.sup.4 is hydrogen or optionally substituted alkyl,X is from 2 to 15, andR.sup.6 is ##STR2## and physiologically acceptable salts thereof.Type: GrantFiled: February 25, 1987Date of Patent: August 29, 1989Assignee: Bayer AktiengesellschaftInventors: Eckhard Schwenner, Hartmut Stegelmeier, Stanislav Kazda, Andreas Knorr
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Patent number: 4853391Abstract: A pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen;R.sub.2 and R.sub.3 are both hydrogen or together represent a bond;R.sub.4 is hydrogen and R.sub.5 is hydrogen or R.sub.4 and R.sub.5 together represent an oxo group;R.sub.6 is hydrogen; C.sub.1-6 alkyl; C.sub.3-7 cycloalkyl; C.sub.3-7 cycloalkyl-C.sub.1-4 alkyl; phenyl or phenyl C.sub.1-7 alkyl in which the phenyl moiety is optionally substituted by one or two of halogen, ortho-nitro, meta-or para-methoxy, methyl or NR.sub.8 R.sub.9 wherein R.sub.8 and R.sub.9 are independently hydrogen or C.sub.1-6 alkyl or R.sub.8 and R.sub.9 together are C.sub.2-6 polymethylen, or 3,4-disubstituted by methylenedioxy or ethylenedioxy; or monocyclic heteroaryl-C.sub.1-4 alkyl or aliphatic heterocyclyl-C.sub.Type: GrantFiled: June 28, 1985Date of Patent: August 1, 1989Inventors: Guy Nadler, Jean-Bernard Le Polles, Marie-Noelle Legave
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Patent number: 4837240Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen;R.sub.2 and R.sub.3 are both hydrogen or together represent a bond;R.sub.4 is hydrogen and R.sub.5 is hydrogen or R.sub.4 and R.sub.5 together represent an oxo group;R.sub.6 is phenyl, phenyl C.sub.1-7 alkyl or phenyl C.sub.1 -7 alkanoyl, in which the phenyl moiety is substituted by NR.sub.8 R.sub.9 wherein R.sub.8 is C.sub.1-6 alkyl substituted by a group R.sub.10 selected from hydroxy, halo, CF.sub.3 or COR.sub.11 where R.sub.11 is hydroxy, C.sub.1-4 alkoxy or amino optionally substituted by one or two C.sub.1-4 alkyl groups, and R.sub.9 is hydrogen, C.sub.1-6 alkyl or R.sub.8 ; andR.sub.7 is hydrogen or C.sub.1-4 alkyl.Type: GrantFiled: June 30, 1987Date of Patent: June 6, 1989Assignee: Beecham-Wuelfing GmbH & Co. KGInventors: Dietrich Thielke, Dagmar Holtje, Guy Nadler
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Analgesic carbocyclic and heterocyclic carbonylmethylene-and carbonylmethypipidines and-pyrrolidines
Patent number: 4826838Abstract: Carbocyclic and heterocyclic carbonylmethylene- and carbonylmethylpiperidines and -pyrrolidines are serotonin antagonists.Type: GrantFiled: July 7, 1987Date of Patent: May 2, 1989Assignee: Sandoz Ltd.Inventors: Brian P. Richardson, Rudolf K. A. Giger, Gunter Engel, Roland Furler -
Patent number: 4731385Abstract: An insecticidal and fungicidal composition comprising (1) An insecticidally effective amount of a nitromethylene derivative of the formula ##STR1## in which X is a lower alkyl group, a lower alkoxy group, or a halogen atom,n is 0, 1 or 2 andm is 2 or 3,and a fungicidally effective amount of at least one fungicide selected from the group consisting of(2) O-ethyl S,S-diphenyl phosphorodithioate,(3) 4,5,6,7-tetrachlorophthalide,(4) 1-(4-chlorobenzyl)-1-cyclopentyl-3-phenylurea,(5) Validamycin A, 3'-iso-propoxy-2-methylbenzenilide, o-trifluoromethyl-m'-isopropoxybenzoylanilide or 6-(3,5-dichloro-4-methylphenyl-3(2H)pyridazinone, and(6) di-isopropyl-1,3-dithiolan-2-ylidenemalonate, 5-methyl-1,2,4-triazo[3,4-b]-benzothiazole, 3-allyloxy-1,2-benzisothiazole 1,1-dioxide, and 1,2,5,6-tetrahydro-4H-pyrrolo-[3,2,1-i,j]quinolin-4-one, [5-amino-2-methyl-6-(2,3,4,5,6-pentahydroxycyclohexyloxy)tetrahydropyran-3 -yl]amino-.alpha.-iminoacetic acid or S-benzyl diisopropylphosphorothiolate.Type: GrantFiled: October 21, 1986Date of Patent: March 15, 1988Assignee: Nihon Tokushu Noyaku Seizo K.K.Inventors: Shinichi Tsuboi, Shoko Sasaki, Yumi Hattori, Yoshio Kurahashi, Shinji Sakawa, Toshihito Kondo
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Patent number: 4729997Abstract: Invention relates to nasal administration of known anti-nausea and anti-emetic therapeutic agents and dosage forms useful for such administration.Type: GrantFiled: August 19, 1986Date of Patent: March 8, 1988Assignee: Nastech Pharmaceutical Co., Inc.Inventor: Jeffrey Wenig
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Patent number: 4713386Abstract: Tetrahydroazeto[2,1-a]isoquinoline of the formula (I): ##STR1## wherein R, R.sup.1, R.sup.2 and R.sup.3 are substituents and x and y are 0-2. Also pharmaceutical compositions for relieving depression in mammals, e.g. in humans, and methods for synthesis and use of formula (I) compounds as well as novel intermediates in the synthesis.Type: GrantFiled: September 22, 1986Date of Patent: December 15, 1987Assignee: McNeilab, Inc.Inventor: Bruce E. Maryanoff
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Patent number: 4654337Abstract: A novel compound of the formula, ##STR1## wherein k is zero or an integer of 1 to 2, j is an integer of from 1 or 3, l and m are each zero or an integer of from 1 to 3, and n is an integer of from 1 to 4, the rings A, B and C being optionally substituted with at least one trifluoromethyl group or tetrafluoroethyl group is prepared by reacting the perhydro compound corresponding thereto with fluorine. The compound is useful as a material capable of carrying oxygen in an aqueous emulsion for lifesaving a patient suffering from massive hemorrhage and for preserving internal organs in transplantation.Type: GrantFiled: July 5, 1985Date of Patent: March 31, 1987Assignee: The Green Cross CorporationInventors: Kazumasa Yokoyama, Chikara Fukaya, Yoshio Tsuda, Taizo Ono, Yoshio Arakawa, Yoshihisa Inoue, Youichiro Naito, Tadakazu Suyama
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Patent number: 4622327Abstract: The invention relates to new 2H-azeto[2,1-a]isoquinoline derivatives of formula (I) ##STR1## wherein R.sup.1 and R.sup.2 represent hydroxyl or alkoxy having from 1 to 6 carbon atoms,R.sup.3 is hydroxyl, halogen or an ##STR2## group, whereinX is oxygen or sulfur,R.sup.4 is optionally substituted phenyl,and acid addition, metal and quaternary salts thereof.According to the invention the new compounds are prepared by cyclization of the corresponding compounds of formula (II), ##STR3## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, and Hal is halogen.Compounds of formula (I) are pharmaceutically active, in particular are potent analgesic and antipyretic agents.Type: GrantFiled: October 25, 1984Date of Patent: November 11, 1986Assignee: Richter Gedeon Vegyeszeti Gyar R.T.Inventors: Gabor Bernath, Jeno Kobor, Alajos Kalman, Pal Sohar, Ferenc Fulop, Elemer Ezer, Gyorgy Hajos, Eva Palosi, Laszlo Denes, Laszlo Szporny
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Patent number: 4613605Abstract: A novel compound of the formula, ##STR1## wherein k is zero or an integer of 1 to 2, j is an integer of from 1 or 3, l and m are each zero or an integer of from 1 to 3, and n is an integer of from 1 to 4, the rings A, B and C being optionally substituted with at least one trifluoromethyl group or tetrafluoroethyl group is prepared by reacting the perhydro compound corresponding thereto with fluorine. The compound is useful as a material capable of carrying oxygen in an aqueous emulsion for lifesaving a patient suffering from massive hemorrhage and for preserving internal organs in transplantation.Type: GrantFiled: July 5, 1985Date of Patent: September 23, 1986Assignee: The Green Cross CorporationInventors: Kazumasa Yokoyama, Chikara Fukaya, Yoshio Tsuda, Taizo Ono, Yoshio Arakawa, Yoshihisa Inoue, Youichiro Naito, Tadakazu Suyama
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Patent number: 4604398Abstract: The invention concerns benzoquinolizines of general formula ##STR1## or their pharmaceutically acceptable acid addition salts. In the formula R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, lower alkyl, lower alkoxy or halogen, R.sup.3 represents lower alkyl and R.sup.4 is lower alkoxy or lower alkoxy carbonyl. The compounds possess .alpha..sub.2 -adrenoceptor antagonistic activity in warm blooded animals.Type: GrantFiled: June 13, 1985Date of Patent: August 5, 1986Assignee: John Wyeth & Brother LimitedInventor: Terence J. Ward
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Patent number: 4595688Abstract: Novel compounds are disclosed, which are derivatives of 1,2,3,5,6,10b-hexahydropyrrolo[2,1-a]-isoquinolines, represented by general formula (I): ##STR1## as well as pharmaceutical compositions and methods for the treatment of depression in warm-blooded animals, e.g., man. Novel intermediates are also part of the invention.Type: GrantFiled: May 18, 1984Date of Patent: June 17, 1986Assignee: McNeilab, Inc.Inventor: Bruce E. Maryanoff
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Patent number: 4567177Abstract: Imidazoline derivatives of formula (I) ##STR1## in which n is 1 or 2, R is hydrogen, C.sub.1 -C.sub.3 alkyl or allyl group, and X is hydrogen, halogen atom, methyl or methoxy, in the form of enantiomers or mixtures thereof, and their pharmaceutically acceptable acid addition salts are useful as .alpha..sub.2 -antagonists.Type: GrantFiled: October 16, 1984Date of Patent: January 28, 1986Assignee: SynthelaboInventors: Dennis Bigg, Claude Morel, Mireille Sevrin
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Patent number: 4562195Abstract: A class of novel saturated, fused-ring, tricyclic, nitrogen-containing diones are useful as agents in treating electro-convulsive shock-induced amnesia. A method of preparing the compounds, pharmaceutical compositions including the compounds, and a method of treating amnesia are disclosed.Type: GrantFiled: January 7, 1985Date of Patent: December 31, 1985Assignee: Warner-Lambert CompanyInventors: Donald E. Butler, Yvon J. L'Italien
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Patent number: 4552879Abstract: A benzoheterocyclic compound of the formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and n are as defined, and its pharmaceutically acceptable salts, processes for preparing same and antibacterial composition containing the benzoheterocyclic compound as an active ingredient and a pharmaceutically acceptable carrier are disclosed.Type: GrantFiled: May 25, 1983Date of Patent: November 12, 1985Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hiroshi Ishikawa, Testuyuki Uno, Masanobu Kano, Kazuyuki Nakagawa
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Patent number: 4550114Abstract: The invention concerns benzoquinolizines of general formula ##STR1## and their pharmaceutically acceptable acid addition salts. In the formula R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, lower alkyl, lower alkoxy or halogen, R.sup.3 represents hydrogen or lower alkyl and R.sup.4 represents a heterocyclic radical attached to the SO.sub.2 group through a carbon atom of the heterocyclic ring. The compounds possess .alpha..sub.2 -adrenoceptor antagonistic activity in warm blooded animals.Type: GrantFiled: January 3, 1984Date of Patent: October 29, 1985Assignee: John Wyeth & Brother limitedInventor: John F. White
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Patent number: 4550103Abstract: Novel 10-amino-9-fluoro- and 9-fluoro-6,7-dihydro-5-methyl-1-oxo-8-(heterocyclyl)1H,5H-benzo (ij)-2-carboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections.Type: GrantFiled: July 20, 1984Date of Patent: October 29, 1985Assignee: Warner-Lambert CompanyInventors: Thomas F. Mich, Townley P. Culbertson
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Patent number: 4542147Abstract: A novel compound of the formula, ##STR1## wherein k is zero or an integer of 1 to 2, j is an integer of from 1 to 3, l and m are each zero or an integer of from 1 to 3, and n is an integer of from 1 to 4, the rings A, B and C being optionally substituted with at least one trifluoromethyl group or tetrafluoroethyl group is prepared by reacting the perhydro compound corresponding thereto with fluorine. The compound is useful as a material capable of carrying oxygen in an aqueous emulsion for lifesaving a patient suffering from massive hemorrhage and for preserving internal organs in transplantation.Type: GrantFiled: June 17, 1983Date of Patent: September 17, 1985Assignee: The Green Cross CorporationInventors: Kazumasa Yokoyama, Chikara Fukaya, Yoshio Tsuda, Taizo Ono, Yoshio Arakawa, Yoshihisa Inoue, Youichiro Naito, Tadakazu Suyama
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Patent number: 4530926Abstract: A novel compound of the formula, ##STR1## wherein k, j, l and m are zero or an integer of from 1 to 3, and n is an integer of from 1 to 3, the rings A, B and C being optionally substituted with at least one trifluoromethyl group, prepared by reacting the corresponding perhydro compound with fluorine is useful as a material capable of carrying oxygen in an aqueous emulsion for lifesaving a patient suffering from massive hemorrhage and for preserving internal organs in transplantation.Type: GrantFiled: June 17, 1983Date of Patent: July 23, 1985Assignee: The Green Cross CorporationInventors: Kazumasa Yokoyama, Chikara Fukaya, Yoshio Tsuda, Taizo Ono, Yoshio Arakawa, Yoshihisa Inoue, Youichiro Naito, Tadakazu Suyama
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Patent number: 4524148Abstract: The compounds 8-bromo-6,7-dihydro-9-fluoro-5-methyl-1-oxo-1H,5H-benzo[ij]quiniolizine-2- carboxylic acid and 8-chloro-6,7-dihydro-9-fluoro-5-methyl-1-oxo-1H,5H,-benzo[ij]quinolizine-2 -carboxylic acid are disclosed as potent antimicrobials. Pharmaceutically-acceptable carboxylate salts, acyl chlorides, esters and alkylaminoalkyl ester salts of the acids are also disclosed.Type: GrantFiled: November 6, 1981Date of Patent: June 18, 1985Assignee: Riker Laboratories, Inc.Inventor: Richard M. Stern