Bicyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/567)
- Chalcogen bonded directly to ring carbon of the hetero ring (Class 540/570)
- Nitrogen bonded directly to ring carbon of the hetero ring (Class 540/571)
- Chalcogen or nitrogen attached indirectly to ring carbon of the hetero ring by acyclic nonionic bonding (Class 540/573)
- Formation of the 1,4-benzodiazepine ring system (Class 540/574)
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Patent number: 5958920Abstract: Certain aralkyl diazabicycloalkyl compounds are disclosed for treatment of CNS disorders, such as cerebral ischemia, psychosis and convulsions.Type: GrantFiled: October 20, 1997Date of Patent: September 28, 1999Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Wayne Bowen, Brian R. de Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
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Patent number: 5942506Abstract: This invention relates to new 1-?2-(substituted vinyl)!-5H-2,3-benzodiazepine derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, to the use of the said benzodiazepine derivatives for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases. The compounds according to the invention correspond to the general formula (I), ##STR1## wherein the variables are herein below defined, and the compounds possess central nervous activities.Type: GrantFiled: February 9, 1996Date of Patent: August 24, 1999Assignee: GIS Gyogyszergyar Rt.Inventors: Pal Vago, Jozsef Reiter, Istvan Gyertyan, Istvan Gacsalyi, Andras Bilkei-Gorzo, Andras Egyed, Ferenc Andrasi, Anna Bakonyi, Pal Berzsenyi, Hilda Botka, Tamas Hamori, Cecilia Salamon Haskane, Edit Horvath, Katalin Horvath, Peter Korosi, Gyorgyne Mate, Imre Moravcsik, Eszter Szentkuti, Gabor Zolyomi, Gabor Blasko, Klara Daroczi Kazone, Gyula Simig, Karoly Tihanyi, Judit Bajnogel
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Patent number: 5922869Abstract: The process for the preparation of bicyclic amidines of the general formula: ##STR1## wherein A is selected from the group consisting of --CR.sup.1 R.sup.2 --CR.sup.3 R.sup.4 --CR.sup.5 R.sup.6 --, --CR.sup.1 R.sup.2 --CR.sup.3 R.sup.4 --CR.sup.5 R.sup.6 --CR.sup.7 R.sup.8 -- and --CR.sup.1 R.sup.2 --CR.sup.3 R.sup.4 --CR.sup.5 R.sup.6 --CR.sup.7 R.sup.8 --CR.sup.9 R.sup.10 --, wherein the substituents in A are in each case numbered starting from the nitrogen atom, and B is selected from the group consisting of --CR.sup.11 R.sup.12 --CR.sup.13 R.sup.14 --, --CR.sup.11 R.sup.12 --CR.sup.15 R.sup.16 --CR.sup.13 R.sup.14 -- and --CR.sup.11 R.sup.12 --CR.sup.15 R.sup.16 --CR.sup.17 R.sup.18 --CR.sup.13 R.sup.14 --, and R.sup.1, R.sup.2 and R.sup.11 to R.sup.14 are, in each case independently of one another, hydrogen, C.sub.1 -C.sub.4 -alkyl, aryl, or are C.sub.1 -C.sub.4 -alkyl which is substituted with hydroxyl, amino, C.sub.1 -C.sub.4 -alkylamino or mercapto, and R.sup.3 to R.sup.10 and R.sup.15 to R.sup.Type: GrantFiled: October 3, 1997Date of Patent: July 13, 1999Assignee: Lonza Ltd.Inventors: Oleg Werbitzky, Ulrich Daum, Rachel Bregy
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Patent number: 5854239Abstract: The present invention relates to diazabicyclic compounds and, specifically, to compounds of the formula ##STR1## wherein A, G, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are as defined in the specification. The compounds of formula I are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.Type: GrantFiled: June 20, 1996Date of Patent: December 29, 1998Assignee: Pfizer Inc.Inventors: Harry R. Howard, Kevin D. Shenk
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Patent number: 5834463Abstract: Compounds represented by the formula: ##STR1## wherein ring A is benzene; Ar is aromatic group; R.sup.1, R.sup.2 and R.sup.3 each stands for H, acyl, hydrocarbon or heterocyclic, or R.sup.2 and R.sup.3, taken together, may form non-aromatic cyclic hydrocarbon; X is methylene or carbonyl; ......... is single bond or double bond; when ......... is single bond, Y is --NR.sup.4 -- (R.sup.4 is H, acyl, hydrocarbon or heterocyclic), when ......... is double bond, Y is N; n is 1-3, provided that, X is carbonyl and, at the same time, R.sup.2 and R.sup.3, taken together, form non-aromatic cyclic hydrocarbon, ......... is double bond or R.sup.4 is a heterocyclic or --Z(CH.sub.2).sub.m --W (Z is methylene or carbonyl, W is optionally substituted amino, and m denotes 0-5), or salts thereof have an excellent GnRH receptor antagonistic action and/or an action of improving sleep disturbances.Type: GrantFiled: June 26, 1995Date of Patent: November 10, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigenori Ohkawa, Nobuhiro Fujii, Koichi Kato, Masaomi Miyamoto
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Patent number: 5807851Abstract: Derivatives of 2,3-benzodiazepine are substituted by one or two halogen atom(s) and have the general formula ##STR1## These derivatives are non-competitive AMPA antagonists and are used in pharmaceutical compositions.Type: GrantFiled: April 4, 1997Date of Patent: September 15, 1998Assignee: Egis Gyogyszergyar Rt.Inventors: Istvan Ling, Gizella Abraham, Pal Berzsenyi, Istvan Tarnawa, Sandor Solyom, Ferenc Andrasi, Tamas Hamori, Emese Csuzdi, Katalin Horvath, Melinda Gal, Imre Moravcsik, Marta Szollosy
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Patent number: 5750690Abstract: A process for the asymmetric hydrogenation of a compound of the formula ##STR1## wherein each R, independently, is alkyl, arylmethyl, aryl, alkoxy, arylmethoxy or aryloxy or both R's, taken together, are methylene, ethylene or 1,2-phenylene and n is 1,2 or 3,or of a salt thereof to a compound of the formula ##STR2## in the form of an (S) or (R) enantiomer, wherein R and n have the significances given above, using an optically active ruthenium-diphosphine complex as catalyst, is described. The preparation of the compounds of formula II, as well as the compounds of formula II, which form a further object of the invention, are also described.Type: GrantFiled: July 26, 1996Date of Patent: May 12, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Emil Albin Broger, Yvo Crameri, Marquard Imfeld, Fran.cedilla.ois Montavon, Erich Widmer
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Patent number: 5723605Abstract: The process for the preparation of bicyclic amidines of the general formula: ##STR1## wherein A is selected from the group consisting of --CR.sup.1 R.sup.2 --CR.sup.3 R.sup.4 --CR.sup.5 R.sup.6 --, --CR.sup.1 R.sup.2 --CR.sup.3 R.sup.4 --CR.sup.5 R.sup.6 --CR.sup.7 R.sup.8 -- and --CR.sup.1 R.sup.2 --CR.sup.3 R.sup.4 --CR.sup.5 R.sup.6 --CR.sup.7 R.sup.8 --CR.sup.9 R.sup.10 --, wherein the substituents in A are in each case numbered starting from the nitrogen atom, and B is selected from the group consisting of --CR.sup.11 R.sup.12 --CR.sup.13 R.sup.14 --, --CR.sup.11 R.sup.12 --CR.sup.15 R.sup.16 --CR.sup.13 R.sup.14 -- and --CR.sup.11 R.sup.12 --CR.sup.15 R.sup.16 --CR.sup.17 R.sup.18 --CR.sup.13 R.sup.14 --, and R.sup.1, R.sup.2 and R.sup.11 to R.sup.14 are, in each case independently of one another, hydrogen, C.sub.1 -C.sub.4 -alkyl, aryl, or are C.sub.1 -C.sub.4 -alkyl which is substituted with hydroxyl, amino, C.sub.1 -C.sub.4 -alkylamino or mercapto, and R.sup.3 to R.sup.10 and R.sup.15 to R.sup.Type: GrantFiled: November 10, 1994Date of Patent: March 3, 1998Assignee: Lonza Ltd.Inventors: Oleg Werbitzky, Ulrich Daum, Rachel Bregy
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Patent number: 5719156Abstract: The invention relates to compounds of the formulas ##STR1## wherein Z, R.sub.c, y, x, l.sub.1, l.sub.2, l.sub.3, u, R.sub.4,R.sub.c', n, R.sub.1, R.sub.2, and R.sub.3, are as described herein. These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.Type: GrantFiled: May 2, 1995Date of Patent: February 17, 1998Assignee: Schering CorporationInventors: Ho-Jane Shue, Neng-Yang Shih, John Piwinski, Xiao Chen, David J. Blythin
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Patent number: 5698691Abstract: Disclosed is a squalene synthetase inhibitor which comprises the compound represented by the formula ##STR1## wherein R.sub.1 is hydrogen or an optionally substituted hydrocarbon group; R.sub.2 is hydrogen, an optionally substituted alkyl group, an optionally substituted phenyl group or an optionally substituted aromatic heterocyclic ring group; X' is a substituent comprising an optionally esterified carboxyl group, an optionally substituted carbamoyl group, an optionally substituted hydroxyl group, an optionally substituted amino group or an optionally substituted heterocyclic radical having a protonizable hydrogen; Ring A is an optionally substituted benzene ring or an optionally substituted aromatic heterocyclic ring; Ring J' is a 7- to 8-membered heterocyclic ring containing at most three ring constituting hetero atoms; D is C or N; the Ring J' optionally having, besides R.sub.1, R.sub.Type: GrantFiled: September 26, 1994Date of Patent: December 16, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Hidefumi Yukimasa, Ryuichi Tozawa, Yasuo Sugiyama, Masakuni Kori
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Patent number: 5691332Abstract: This invention is concerned with novel compounds represented by structural formula I ##STR1## which are useful in the treatment of arrhythmia.Type: GrantFiled: August 19, 1996Date of Patent: November 25, 1997Assignee: Merck & Co., Inc.Inventors: David A. Claremon, Roger M. Freidinger, Nigel Liverton, Harold G. Selnick, Garry R. Smith
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Patent number: 5639745Abstract: Disclosed are compounds, compositions and methods for inhibiting interleukin-1.beta. protease activity. The compounds, bicyclic derivatives of aldehydes and .alpha.-substituted methyl ketones, have the formula (A) set out herein.Type: GrantFiled: May 25, 1995Date of Patent: June 17, 1997Assignee: SanofiInventors: Roland E. Dolle, Prasad V. Chaturvedula, Tina Morgan Ross, Stanley J. Schmidt
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Patent number: 5631372Abstract: A process for producing 1-substituted-4-fluoro-1,4-diazoniabicyclo[2.2.2]octane salts having the formula ##STR1## wherein the Z substituent is OH, OR, OC(O)R, SO.sub.3, SO.sub.2 R, NO.sub.2, NO, or PO(OR).sub.2, wherein R is an aryl or C.sub.1 -C.sub.8 alkyl group; n is 0, 1 or 2; each of R.sub.1, R.sub.2, R.sub.3, P.sub.4 and R.sub.5 independently represent hydrogen, C.sub.1 to C.sub.8 alkyl, or aryl 1-substituted-1,4-diazoniabicyclo[2.2.2]octane or 1,4-diazoniabicyclo[2.2.2]octane mono-N-oxide is reacted to attach the Z group and then the result is reacted with molecular fluorine in the presence of a solvent that substantially does not react with fluorine and a fluoride scavenger that results in an X counter ion. These compounds are useful as fluorinating agents for the introduction of fluorine into organic compounds.Type: GrantFiled: May 6, 1996Date of Patent: May 20, 1997Assignee: AlliedSignal Inc.Inventors: Andrew J. Poss, George A. Shia, Dennis M. Lavery
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Patent number: 5624922Abstract: Aryl-fused- and hetaryl-fused-2,4-diazepines of formula XXXVI, benzodiazocines of formula XXX, benzodiazepines of formula II ##STR1## .delta.-aminoamides of formula III and aryldimethanamines of formula XXXVII ##STR2## wherein A is an aryl or hetaryl ring;R.sup.1 is hydrogen, alkyl, aryl or hetaryl;R.sup.2 is hydrogen, alkyl, substituted alkyl, or aryl;R.sup.3 is alkyl, aryl, aralkyl or heteroatom substituted alkyl or aralkyl;R.sup.4 is hydrogen or alkyl;R.sup.5 is hydrogen, alkyl, aryl or hetaryl;R.sup.6 is hydrogen, alkyl, alkoxy, halogen or a fused benzene ring;R.sup.9 is hydrogen, alkyl, or substituted alkyl; andR.sup.10 is hydrogen, alkyl, or substituted alkyl the invention further relates to processes for the preparation of, pharmaceutical compositions containing, and methods of treating cardiac arrhythmia with the compounds of formulas XXXVI, XXX, II, III, and XXXVII.Type: GrantFiled: May 24, 1995Date of Patent: April 29, 1997Assignee: Sterling Winthrop Inc.Inventors: Robert E. Johnson, Donald C. Schlegel, Alan M. Ezrin
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Patent number: 5534633Abstract: Aminoketone-substituted coumarin sensitizers having tethered tertiary amino groups are described which have extremely good photosensitivity. The sensitizers of the instant invention have the formula: ##STR1## wherein R.sub.1 and R.sub.2 each represent an alkyl group having 1 to 6 carbon atoms, and R.sub.3 and R.sub.4 each represent hydrogen; or at least one of R.sub.1 and R.sub.3 or R.sub.2 and R.sub.4 together represent an alkylene group having 2 to 4 carbon atoms,R.sub.5 represents an alkyl group having 1 to 6 carbon atoms or H,R.sub.6 represents an alkylene group having 1 to 6 carbon atoms, andR.sub.7 and R.sub.8 each independently represent an alkyl group having 1 to 6 carbon atoms, both of R.sub.7 and R.sub.8 taken together represent an alkylene group having 4 to 6 carbon atoms, or R.sub.5 or R.sub.6 taken together with R.sub.7 or R.sub.8 represent a five, six, or seven membered heterocyclic ring group.Type: GrantFiled: February 3, 1995Date of Patent: July 9, 1996Assignee: Minnesota Mining and Manufacturing CompanyInventor: M. Zaki Ali
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Patent number: 5510346Abstract: Novel 4,5-dihydro-4-heteroaryl-3H-1,3-benzodiazepines, intermediates, processes for the preparation thereof, and methods for treating depression, inhibiting convulsions and treating anxiety utilizing compounds and compositions thereof are disclosed.Type: GrantFiled: October 24, 1991Date of Patent: April 23, 1996Assignee: Hoechst Marion Roussel, Inc.Inventors: Lawrence L. Martin, Joseph F. Payack, Salvatore M. Brucato
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Patent number: 5489681Abstract: A compound of the formula ##STR1## is prepared by reacting an N-acylated-o-toluidine of the formula ##STR2## with n-alkyllithium to form a dilithio intermediate of the formula ##STR3## which can then be quenched with N-benzylidenemethylamine to fore compound II. Hydrolysis of compound(II) yields the free base ##STR4## or its salt, which can be cyclized to form 4,5-dihydro-2,3-dimethyl-4-phenyl-3H-1,3-benzodiazepine or its physiologically acceptable salts, which are useful as pharmacological agents.Type: GrantFiled: September 9, 1994Date of Patent: February 6, 1996Assignee: Hoeschst-Roussel Pharmaceuticals, Inc.Inventors: Thomas B. K. Lee, George E. Lee
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Patent number: 5474974Abstract: There are provided new 3-hydroxy-4-aryl-5-oxo-pyrazoline derivatives of the formula (I) ##STR1## The new 3-hydroxy-4-aryl-5-oxo-pyrazoline derivatives of the formula (I) have a particularly pronounced activity against animal pests, in particular against insects and arachnids, and against weeds.Type: GrantFiled: April 28, 1994Date of Patent: December 12, 1995Assignee: Bayer AktiengesellschaftInventors: Bernd-Wieland Kruger, Reiner Fischer, Heinz-Jurgen Bertram, Thomas Bretschneider, Stefan Bohm, Andreas Krebs, Thomas Schenke, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt, Christoph Erdelen, Ulrike Wachendorff-Neumann, Wilhelm Stendel
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Patent number: 5380721Abstract: Aryl-fused- and hetaryl-fused-2,4-diazepines of formula XXXVI, benzodiazocines of formula XXX, benzodiazepines of formula II ##STR1## .delta.-aminoamides of formula III and aryldimethanamines of formula XXXVII ##STR2## wherein A is an aryl or hetaryl ring;R.sup.1 is hydrogen, alkyl, aryl or hetaryl;R.sup.2 is hydrogen, alkyl, substituted alkyl, or aryl;R.sup.3 is alkyl, aryl, aralkyl or heteroatom substituted alkyl or aralkyl;R.sup.4 is hydrogen or alkyl;R.sup.5 is hydrogen, alkyl, aryl or hetaryl;R.sup.6 is hydrogen, alkyl, alkoxy, halogen or a fused benzene ring;R.sup.9 is hydrogen, alkyl, or substituted alkyl; andR.sup.10 is hydrogen, alkyl, or substituted alkyl.The invention further relates to processes for the preparation of, pharmaceutical compositions containing, and methods of treating cardiac arrhythmia with the compounds of formulas XXXVI, XXX, II, III, and XXXVII.Type: GrantFiled: May 31, 1994Date of Patent: January 10, 1995Assignee: Sterling Winthrop Inc.Inventors: Robert E. Johnson, Donald C. Schlegel, Alan M. Ezrin
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Patent number: 5292760Abstract: Novel 4,5-dihydro-4-heteroaryl-3H-1,3-benzodiazepines, intermediates, processes for the preparation thereof, and methods for treating depression, inhibiting convulsions and treating anxiety utilizing compounds and compositions thereof are disclosed.Type: GrantFiled: April 22, 1992Date of Patent: March 8, 1994Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Lawrence L. Martin, Joseph F. Payack, Salvatore M. Brucato
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Patent number: 5288863Abstract: The invention relates to a process for the preparation of 1-(3-chlorophenyl)-4-methyl-7,8-dimethoxy-5 H-2,3-benzodiazepine of formula (I) ##STR1## in high purity and in a quality suitable for pharmaceutical purposes. According to the invention the reaction of 1 mole of 2-acetonyl-3'-chloro-4,5-dimethoxybenzophenone of formula (II) ##STR2## with 3-7 moles of hydrazine hydrate in an organic solvent or in a mixture of organic solvents at a temperature between 15.degree. C. and 85.degree. C. is carried out in the absence of air oxygen, optionally in the presence of water. The crude product is then recrystallized from an aliphatic alcohol containing 1 to 5 carbon atom(s).Type: GrantFiled: May 4, 1992Date of Patent: February 22, 1994Assignee: Egis Gyogyszergyar Rt.Inventors: Gyorgy Somogyi, Peter Botka, Gyula Horvath, Antal Simay, Roozsa Gyenge, Imre Moravcsik, Erno Orban, Tamas Hamori, Jeno Korosi, Csilla Kiss, Tibor Balogh, Maria Bidlo nee Igloi, nee Dievald Uskert
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Patent number: 5270157Abstract: A colour photographic silver halide material having at least one silver halide emulsion layer which contains at least one colour coupler and in which the silver halide grains contain from 40 to 90 mol. % of AgCl and at least two zones differing in halide composition, the chloride content of the outer zone being at least 10 mol. % higher than that of the inner zone, which silver halide emulsion layer is associated with a DIR compound whose reaction with the oxidized colour developer has a rate constant k>2000 [1/mol.s] is distinguished by excellent sharpness and colour reproduction even when processed by a high speed process.Type: GrantFiled: September 28, 1992Date of Patent: December 14, 1993Assignee: Bayer AktiengesellschaftInventors: Peter Bell, Cuong Ly
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Patent number: 5212301Abstract: Introduction of a fluoro substituent into an aromatic ring adjacent an electron donating group is difficult producing mixed isomers and low yields of desired products.A process for the introduction of a fluoro substituent into a substantially adjacent position to an electron-donating group into an aromatic compound in high yield is disclosed.The fluoroaromatic compounds are useful as synthetic intermediates for example in the manufacture of agrochemicals, pharmaceuticals and dyestuffs.Type: GrantFiled: May 8, 1992Date of Patent: May 18, 1993Assignee: Imperial Chemical Industries PLCInventors: John S. Moilliet, Richard D. Chambers, Michael H. Rock
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Patent number: 5204343Abstract: The invention relates to the new 1-(3-chlorophenyl)-4-hydroxymethyl-7,8-dimethoxy-5H-2,3-benzodiazepine of formula (I) ##STR1## and pharmaceutically acceptable acid addition salts thereof, furthermore to a process for preparing these compounds.The compounds according to the invention possess valuable anxiolytic, antiaggressive and antidepressant effects and have at the same time favorable acute toxicity values, so they can be used to advantage in therapy.Type: GrantFiled: October 17, 1991Date of Patent: April 20, 1993Assignee: Egis GyogyszergyarInventors: Ferenc Andrasi, Peter Botka, Katalin Goldschmidt nee Horvath, Tamas Hamori, Gyula Horvath, Jeno Korosi, Imre Moravcsik, Marta Rusz nee Patfalusi, Eva Tomori nee Joszt, Gabor Zolyomi
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Patent number: 5168103Abstract: A compound of the formula: ##STR1## in which R.sup.1 is hydrogen, alkyl or phenylalkyl; R.sup.2 is hydrogen, alkyl, alkenyl or phenylalkyl; or R.sup.1 and R.sup.2 taken together are --Ch.sub.2 CH.sub.2 --, --CH.sub.2 C(R.sup.6)(R.sup.7)CH.sub.2 --or --CH.sub.2 C(R.sup.8)(R.sup.9)--C(R.sup.10)(R.sup.11)CH.sub.2 --, where R.sup.6, R.sup.8 and R.sup.10 are, independently, hydrogen, alkyl of 1 to 6 carbon atoms or hydroxyl and R.sup.7, R.sup.9 and R.sup.11 are, independently, hydrogen or alkyl of 1 to 6 carbon atoms; A is alkylene or alkenylene; X is CO.sub.2 R.sup.3 in which R.sup.3 is hydrogen or alkyl, P(O)(OR.sup.4)(OR.sup.5) in which R.sup.4 and R.sup.5 are, independently, hydrogen or alkyl, 3,5-dioxo-1,2,4-oxadiazolindin-2-yl or 5-tetrazolyl; or a pharmaceutically acceptable salt thereof are useful as neuroprotectants.Type: GrantFiled: December 17, 1991Date of Patent: December 1, 1992Assignee: American Home Products CorporationInventors: William A. Kinney, Deanna C. Garrison
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Patent number: 5036153Abstract: (R,R)-2,5-Diazabicyclo[ 2.2.1]heptanes are prepared from a compound of the formula ##STR1## wherein X and R.sub.2 are as defined herein, by heating with tosylchloride in pyridine, reacting the formed compound of the formula ##STR2## with a C.sub.1 -C.sub.6 alkylamine or ammonia, and reducing or hydrolyzing the formed compound of the formula ##STR3## wherein R.sub.1 is hydrogen or C.sub.1 -C.sub.6 alkyl.Type: GrantFiled: October 18, 1989Date of Patent: July 30, 1991Inventors: Tamim F. Braish, Darrell E. Fox
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Patent number: 5008263Abstract: Platelet activating factor antagonists of formula (I), (II) or (III): ##STR1## where A is optionally substituted benzene, pyridine, naphthalene, quinoline, thiophene, benzothiophene, pyrazole or isothiazole,X is O, S or NHY is 1,4 phenylene or a group of formula ##STR2## R.sup.1 is H or optionally substituted C.sub.1 -C.sub.4 alkyl, R.sup.2 and R.sup.3 are H or C.sub.1 -C.sub.4 alkyl,B is an optionally fused 5- or 6-membered ring containing nitrogen atoms,Het is an optionally substituted 5-membered heterocyclic ring containing nitrogen or a pyridine ring, the ring optionally being fused to benzene or nitrogen-containing heterocyclic ring.Type: GrantFiled: March 20, 1990Date of Patent: April 16, 1991Assignee: Pfizer Inc.Inventors: Kelvin Cooper, Michael J. Fray
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Patent number: 4977155Abstract: Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.2 is hydrogen, NO.sub.2, NH.sub.2, CN, halogen, or SO.sub.2 NH.sub.2 ; --X--Y--Z-- is selected from --N.dbd.N--N.sup.3 --,--NR.sup.3 --N.dbd.N--,.dbd.N--NR.sup.3 --N.dbd., wherein R.sup.3 is hydrogen, lower alkyl, or CF.sub.3.The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use.The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters.Type: GrantFiled: June 22, 1989Date of Patent: December 11, 1990Assignee: A/S FerrosanInventors: Poul Jacobsen, Flemming E. Nielsen, Tage Honore, Jorgen Drejer
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Patent number: 4906630Abstract: A method for increasing cardiotonic contractility in humans or other animals using a class of benzodiazinone-pyridazinone and hydroxy-pyrazolyl compounds and pharmaceutical compositions including the same.Type: GrantFiled: October 11, 1988Date of Patent: March 6, 1990Assignee: Rorer Pharmaceutical CorporationInventors: William L. Studt, William C. Faith, Bruce F. Molino
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Patent number: 4895943Abstract: Processes and intermediates for preparing 1,4-diazabicyclo[3.2.2.]nonane including a process for the preparation of a compound of the formula ##STR1## wherein R.sup.1 is C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkyl substituted with 1 to 6 halo groups; and R.sup.2 is hydrogen, naphthoyl, substituted naphthoyl, benzyl, substituted benzyl, benzoyl or substituted benzoyl, wherein each of said substituted naphthoyl, substituted benzyl, and substituted benzoyl is substituted with one to three substituents selected from the group consisting of halo, C.sub.1 -C.sub.4 alkoxy and C.sub.1 -C.sub.4 alkyl, comprising reacting a compound of the formula ##STR2## wherein R.sup.1 and R.sup.3 are independently selected from C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkyl substituted with 1 to 6 halo groups with an alkyl stannane or a trialkyl aluminum and, if desired, reacting the resulting compound of the formula III wherein R.sup.Type: GrantFiled: October 25, 1988Date of Patent: January 23, 1990Assignee: Pfizer Inc.Inventors: Robert C. Friedmann, John W. Lackey, Brian T. O'Neill
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Patent number: 4869772Abstract: In a process for priming a non-polar substrate such as a polyolefin for bonding with a cyanoacrylate adhesive, the use of an adhesion-promoting primer comprising at least one diazabicyclo or triazabicyclo compound selected from1,5-diazabicyclo[4.3.0]non-5-ene having the formula: ##STR1## 1,8-diazabicyclo[5.4.0]undec-7-ene having the formula: ##STR2## and 1,5,7-triazabicyclo[4.4.0]dec-5-ene having the formula: ##STR3## The primer also contains a solvent.Type: GrantFiled: June 14, 1988Date of Patent: September 26, 1989Assignee: Loctite (Ireland) Ltd.Inventors: Patrick F. McDonnell, Brendan J. Kneafsey
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Patent number: 4840948Abstract: This invention relates to new 1-(hydroxystyryl)-5H-2,3-benzodiazepine derivatives of the general formula (I) and to a process for the preparation thereof, furthermore to pharmaceutical compositions containing the same, ##STR1## wherein R stands for a hydrogen or halogen atom, or a C.sub.1-4 alkoxy group,R.sup.1 represents a hydrogen atom or a C.sub.1-4 alkyl group,R.sup.2 and R.sup.3 are identical and denote a C.sub.1-4 alkyl group, or combined they denote a methylene group.The compounds of the general formula (I) possess valuable positive inotropic (cardiotonic) potency, are capable to increase the myocardiac contractile force (heart performance in cardiac insufficiency), thus they can be applied in the therapy of chronic heart failure and coronary ailments.Type: GrantFiled: May 20, 1987Date of Patent: June 20, 1989Assignee: EGIS GyogyszergyarInventors: Tibor Lang, Jeno Korosi, Gyorgy Rabloczky, Tamas Hamori, Maria Kuhar nee Kurthy, Istvan Polgari, Istvan Elekes, Gabor Zolyomi, Krisztina Heltai, Judit Sarossy nee Kincsesy, Zsuzsanna Lang nee Rihmer, Imre Moravcsik
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Patent number: 4785101Abstract: Benzodiazinone-pyridazinone and -hydroxypyrazolyl compounds possess cardiotonic activity and are included in therapeutic cardiotonic compositions useful in methods for increasing cardiac contractility and for the treatment of congestive heart failure.Type: GrantFiled: June 17, 1987Date of Patent: November 15, 1988Assignee: Rorer Pharmaceutical CorporationInventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt, William C. Faith, Bruce F. Molino
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Patent number: 4650797Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is alkyl, alkenyl, alkynyl, cycloalkyl, or substituted alkyl, and R.sub.4 is aryl or heterocyclo are disclosed. These compounds are useful as cardiovascular agents and especially as anti-hypertensive agents.Type: GrantFiled: July 18, 1986Date of Patent: March 17, 1987Assignee: E. R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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Patent number: 4647561Abstract: Compounds of formula ##STR1## wherein R.sub.4 is aryl or heterocyclo are disclosed. These compounds are useful as cardiovascular agents and especially as anti-hypertensive agents.Type: GrantFiled: August 5, 1985Date of Patent: March 3, 1987Assignee: E. R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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Patent number: 4614740Abstract: The invention relates to new 5H-2,3-benzodiazepine derivatives and a process for the preparation thereof, furthermore to pharmaceutical compositions containing the same.The new 5H-2,3-benzodiazepine derivatives of the invention possess valuable central nervous effect and in particular exert antiaggressive, anxiolytic, narcosis potentiating and soporific properties.Type: GrantFiled: July 26, 1985Date of Patent: September 30, 1986Assignee: Egis GyogyszergyarInventors: Tibor Lang, Jeno Korosi, Ferenc Andrasi, Peter Botka, Tamas Hamori, Pal Berzsenyi, Katalin Goldschmidt, Gabor Zolyomi, Istvan Elekes, Zsuzsanna Lang nee Rihmer