Chalcogen Bonded Directly To Ring Carbon Of The Tricyclo Ring System Patents (Class 546/86)
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Patent number: 5834481Abstract: Heterotricyclically substituted phenyl-cyclohexanecarboxylic acid derivatives are prepared by reacting the heterocyclic compounds with cyclohexanecarboxylic acid derivatives which are substituted by benzyl halide radicals. The compounds can be employed as active compounds in medicaments.Type: GrantFiled: July 8, 1997Date of Patent: November 10, 1998Assignee: Bayer AktiengesellschaftInventors: Ulrich E. Muller, Jurgen Dressel, Peter Fey, Rudolf H. Hanko, Walter Hubsch, Thomas Kramer, Matthias Muller-Gliemann, Martin Beuck, Stanislav Kazda, Stefan Wohlfeil, Andreas Knorr, Johannes-Peter Stasch, Siegfried Zaiss
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Patent number: 5834482Abstract: A compound of formula (I). The present invention relates to therapeutically active .beta.-carboline derivatives, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a central nervous system ailment related to the inhibition of GABA uptake via the GAT-4 subtype carrier.Type: GrantFiled: October 21, 1997Date of Patent: November 10, 1998Assignee: Novo Nordisk A/SInventors: Jane Marie Lundbeck, Birgitte Soekilde, Per Olaf Huusfeldt
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Patent number: 5817668Abstract: A compound of the general formula 1; ##STR1## is disclosed as useful in treating disorders of the central nervous system. Pharmaceutical compositions and methods of treatment are also disclosed.Type: GrantFiled: October 3, 1997Date of Patent: October 6, 1998Assignee: Ortho Pharmaceutical CorporationInventors: Allen B. Reitz, Alfonzo D. Jordan, Pauline J. Sanfilippo, Malcolm K. Scott, Anna Vavouyios-Smith
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Patent number: 5808067Abstract: The present invention pertains to a method of preparing substituted and unsubstituted N-hydroxy-2-aminobutane diacid derivatives which can be dehydrated to 2-aminobut-2-ene dioic acid derivatives, which can be subsequently converted to pyridine and quinoline derivatives.Type: GrantFiled: December 21, 1994Date of Patent: September 15, 1998Assignee: Hoechst Celanese CorporationInventors: John Saukaitis, Franklin B. Gupton
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Patent number: 5783575Abstract: The present invention relates to therapeutically active non competitive antagonists, acting selectively at the metabotropic glutamate receptor. The novel compounds are useful in treating diseases in the central nervous system by modulating synaptic transmission via the metabotropic glutamate receptor.Type: GrantFiled: July 31, 1995Date of Patent: July 21, 1998Assignee: Novo Nordisk A/SInventors: Palle Jakobsen, Anders Kanstrup, Peter Faarup, Preben H. Olesen, Jane Marie Lundbech
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Patent number: 5760051Abstract: Tetrahydro-beta-carboline compounds having useful central nervous system activity are enclosed.Type: GrantFiled: June 7, 1995Date of Patent: June 2, 1998Assignee: Eli Lilly and CompanyInventors: James E. Audia, James J. Droste, Deborah A. Evrard, Pawel Fludzinski, Gwyn L. Murdoch, David L. Nelson
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Patent number: 5700761Abstract: Compounds of Formula I having herbicidal utility are disclosed: ##STR1## wherein Q, R.sup.1, R.sup.2, V, m and p are defined in the text, including compositions containing such compounds, and a method for controlling weeds employing such compounds.Type: GrantFiled: August 15, 1996Date of Patent: December 23, 1997Assignees: E. I. Du Pont de Nemours and Company, Degussa AktiengesellschaftInventor: John Jolly Kilama
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Patent number: 5700808Abstract: 5- or 6-substituted .beta.-carboline-3-carboxylic acid esters of Formula I ##STR1## wherein R.sup.1 is hydrogen, nitrilo, halogen, lower alkyl or lower alkoxy, andR.sup.3 is a branched C.sub.3-6 alkyl group which is optionally substituted by halogen, or a C.sub.3-6 cycloalkyl group which is optionally methyl-substituted, are valuable pharmaceuticals.Type: GrantFiled: May 18, 1994Date of Patent: December 23, 1997Assignee: Schering AktiengesellschaftInventors: Helmut Biere, Andreas Huth, Dieter Rahtz, Ralph Schmiechen, Dieter Seidelmann, Wolfgang Kehr, Herbert Hans Schneider, Mogens Engelstoft, Bondo John Hansen, Frank Waetjen, Tage Honore
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Patent number: 5698555Abstract: Hetaryloxy-.beta.-carbolines of formula I ##STR1## in which R.sup.A means a triazine or benzocondensed hetaryl radical with 1-2 nitrogen atoms optionally substituted with halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, trifluoromethyl or SO.sub.2 --R.sup.1 or a 5- or 6-membered hetaryl radical with 1-2 nitrogen atoms substituted with halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, trifluoromethyl or SO.sub.2 --R.sup.1are useful pharmaceutical agents.Type: GrantFiled: July 11, 1994Date of Patent: December 16, 1997Assignee: Schering AktiengesellschaftInventors: Martin Kruger, Andreas Huth, Dieter Seidelmann, Herbert Schneider, Lechoslaw Turski, David Norman Stephens
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Patent number: 5688807Abstract: The present invention provides methods for binding a 5-HT.sub.2B receptor in mammals using a both known and novel compounds. Further, the invention provides a method for treating or preventing 5-HT.sub.2B related conditions. Finally, the invention provides an article of manufacture.Type: GrantFiled: February 6, 1995Date of Patent: November 18, 1997Assignee: Eli Lilly and CompanyInventors: James E. Audia, Marlene L. Cohen, Jaswant S. Gidda, David L. G. Nelson
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Patent number: 5684014Abstract: Cycloalkano-indole and -azaindole derivatives are prepared by reaction of appropriately substituted carboxylic acids with amines. The cycloalkano-indole and -azaindole derivatives are suitable as active compounds for medicaments, preferably antiatherosclerotic medicaments.Type: GrantFiled: September 28, 1995Date of Patent: November 4, 1997Assignee: Bayer AktiengesellschaftInventors: Ulrich Muller, Richard Connell, Siegfried Goldmann, Rudi Grutzmann, Martin Beuck, Hilmar Bischoff, Dirk Denzer, Anke Domdey-Bette, Stefan Wohlfeil
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Patent number: 5652245Abstract: Tricyclic nitrogen containing compounds, having anxiolytic and anti-depressant activity and central nervous system activity of the following structural formula: ##STR1## and pharmaceutically acceptable salts thereof wherein R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl or R.sub.1 and R.sub.2 are joined to form pyrrolidine, piperidine, morpholine or imidazole. X is OCH.sub.3, SO.sub.2 R.sub.3, SO.sub.2 CF.sub.3 or CN where R.sub.3 is C.sub.1-6 alkyl or an Aryl; and Y is hydrogen, Cl, Br, F, CN, CONR.sub.1 R.sub.2, CF.sub.3, OCH.sub.3, SO.sub.2 NR.sub.1 R.sub.2. These new compounds are suitable for treating anxiolytic disorder, schizophrenia, Parkinson's disease, anxiety, depression or as compounds for lowering blood pressure or treating migraine headaches in patients in need of such treatment.Type: GrantFiled: January 23, 1996Date of Patent: July 29, 1997Assignee: Pharmacia & Upjohn CompanyInventor: Arthur G. Romero
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Patent number: 5646150Abstract: The invention provides lavendamycin analogs having the following formula: ##STR1## wherein X, Y and R.sup.1 through R.sup.9 are defined in the specification, and salts of these analogs. The invention also provides a method of making the lavendamycin analogs. The lavendamycin analogs have antitumor and antimicrobial activity. Also, methods of treating cancer using lavendamycin methyl ester, 7-butyramido-2-methylquinoline-5,8-dione or 7-butyramido-2-formylquinoline-5,8-dione.Type: GrantFiled: November 28, 1994Date of Patent: July 8, 1997Assignee: Ball State UniversityInventors: Mohammad Behforouz, Ronald L. Merriman
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Patent number: 5646149Abstract: Compounds having both calcium antagonist and antioxidant activity are disclosed. The compounds are useful in preventing or alleviating damage to tissues at the cellular level. Methods of treatment which employ these properties of the compounds and corresponding pharmaceutical compositions are also disclosed.Type: GrantFiled: June 7, 1995Date of Patent: July 8, 1997Assignee: Alcon Laboratories, Inc.Inventors: Mark R. Hellberg, George Barnes, Robert J. Collier, Jr.
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Patent number: 5643916Abstract: The present invention provides novel tetrahydro-beta-carboline compounds having useful central nervous system activity. Further, there is provided tetrahydro-beta-carboline related compounds which are useful intermediates and have beneficial central nervous system activity. The invention provides formulations and methods for using the novel tetrahydro-beta-carboline and related compounds. Such compounds are particularly useful for the modulation of a 5-HT.sub.2B receptor.Type: GrantFiled: May 19, 1995Date of Patent: July 1, 1997Assignee: Eli Lilly and CompanyInventors: James E. Audia, Stephen Richard Baker, Jesus Ezquerra Carrera, Carlos Lamas Peteira, Concepcion Pedregal Tercero
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Patent number: 5639760Abstract: The present invention is directed to compounds of the following formula I: ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, A, n, X, and Y are as defined hereinafter. The compounds of formula I are useful in treating central nervous system disorders. The compounds are ligands for the BZD binding site on GABA-A receptors, and are thus useful as muscle relaxants, hypnotics/sedatives including sleep-aids, anxiolytics, anticonvulsants/antiepileptics, anti-inebriants, and antidotes for drug overdose (particularly benzodiazepine overdose).Type: GrantFiled: February 16, 1995Date of Patent: June 17, 1997Inventors: Bruce E. Maryanoff, David F. McComsey, Winston Ho
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Patent number: 5635513Abstract: 056355134 ##STR1## This invention relates to the novel salt 6-fluoro-2,3,4,5-tetrahydro-5-methyl-2[(5-methyl-1H-imidazol-4-yl)methyl]- 1H-pyrido[4,3-b]indol-1-one methane sulphonate, to solvates of this salt, to pharmaceutical compositions containing it and to its use in medicine as 5-HT3 receptor antagonists.Type: GrantFiled: January 26, 1995Date of Patent: June 3, 1997Assignee: Glaxo Group LimitedInventors: Peter L. Hartley, Tony G. Roberts, Leonard G. Whitesell
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Patent number: 5631265Abstract: The present invention provides novel tetrahydro-beta-carboline compounds and intermediates having useful central nervous system activity. The invention provides formulations and methods for using the tetrahydro-beta-carboline and related intermediate compounds. Finally, the invention provides an article of manufacture.Type: GrantFiled: February 6, 1995Date of Patent: May 20, 1997Assignee: Eli Lilly and CompanyInventors: James E. Audia, James J. Droste, Jeffrey S. Nissen
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Patent number: 5629317Abstract: The present invention provides novel tetrahydro-beta-carboline compounds having useful central nervous system activity. Further, there is provided tetrahydro-beta-carboline related compounds which are useful intermediates and have beneficial central nervous system activity. The invention provides formulations and methods for using the novel tetrahydro-beta-carboline and related compounds. Such compounds are particularly useful for the modulation of a 5-HT.sub.2B receptor.Type: GrantFiled: May 19, 1995Date of Patent: May 13, 1997Assignee: Eli Lilly and CompanyInventors: James E. Audia, Stephen R. Baker, Jesus E. Carrera, Carlos L. Peteira, Concepcion P. Tercero
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Patent number: 5606060Abstract: Azatoxin and derivatives thereof are illustrative of a new class of antitumor drugs that are topoisomerase II (top 2) inhibitors. The pharmacophore inhibits the catalytic activity of the purified enzyme but does not unwind relaxed or supercoiled DNA. It is nonintercalative and has at least two domains: a quasiplanar polycyclic ring system, which may bind between DNA base pairs, and a pendant substituent thought to interact with the enzyme, with the DNA grooves or with both. In SV40 and c-myc DNA, azatoxin induces numerous double-strand breaks according to a cleavage pattern which differs from those of known top 2 inhibitors. Azatoxin also is a potent inhibitor of tubulin polymerization.Type: GrantFiled: June 2, 1995Date of Patent: February 25, 1997Assignee: The United States of America as represented by the Department of Health & Human ServicesInventors: Yves Pommier, Timothy L. MacDonald, Jose S. Madalengoitia
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Patent number: 5604236Abstract: Selected acid functional beta-carboline type derivatives effective as thromboxane synthase inhibitors having the formula: ##STR1## where R.sub.1 and R.sub.2 are monovalent radicals, --(L.sub.a)-- is a linking group of 4 to 8 chain atoms, and A is an acidic group.Type: GrantFiled: May 5, 1995Date of Patent: February 18, 1997Assignee: Eli Lilly and CompanyInventors: Joseph A. Jakubowski, Alan D. Palkowitz
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Patent number: 5580878Abstract: This invention relates to novel substituted tryptamine and phenalkylamine and related compounds, pharmaceutical compositions thereof and methods of using said compounds.Type: GrantFiled: June 7, 1995Date of Patent: December 3, 1996Assignee: Interneuron Pharmaceuticals, Inc.Inventors: Kay J. D'Orlando, Kenneth W. Locke, Emile M. Bellott, Richard L. Gabriel, Michael D. Nohrden, Yesh P. Sachdeva, Salah A. Zahr, Emile Al-Farhan, Subramaniam Krishnananthan
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Patent number: 5563147Abstract: This invention provides novel, optionally substituted tetrahydropyridoindoles which are useful serotonergic agents for the treatment of central nervous system disorders.Type: GrantFiled: June 5, 1995Date of Patent: October 8, 1996Assignee: Eli Lilly and CompanyInventors: Jeremy Gilmore, Peter T. Gallagher, Martin V. Miles, William M. Owton, Colin W. Smith
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Patent number: 5550118Abstract: Selected acid functional polyhydronorharman type derivatives effective as thromboxane synthase inhibitors having the formula: ##STR1## where R.sub.1 and R.sub.2 are monovalent radicals, --(L.sub.a)-- is a linking group of 4 to 8 chain atoms, and A is an acidic group.Type: GrantFiled: January 31, 1994Date of Patent: August 27, 1996Assignee: Eli Lilly and CompanyInventors: Joseph A. Jakubowski, Alan D. Palkowitz, Sandra K. Sigmund
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Patent number: 5543519Abstract: Compounds of formula I are described ##STR1## in which R.sup.3 represents a C.sub.6-12 -aryl or hetaryl radical, optionally substituted singly or multiply with C.sub.1-4 -alkyl, C.sub.3-7 -cycloalkyl, halogen, C.sub.1-4 -alkoxy-C.sub.1-2 -alkyl, phenyl or amino, the process for their production and their use in pharmaceutical agents.Type: GrantFiled: October 25, 1994Date of Patent: August 6, 1996Assignee: Schering AktiengesellschaftInventors: Andreas Huth, Dieter Seidelmann, Ralph Schmiechen, Herbert Schneider, Lechoslaw Turski
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Patent number: 5538981Abstract: The present invention provides novel tetrahydrobeta-carboline compounds and intermediates having useful central nervous system activity. The invention further provides formulations and methods for using the novel tetrahydrobeta-carboline compounds.Type: GrantFiled: May 10, 1995Date of Patent: July 23, 1996Assignee: Eli Lilly and CompanyInventors: James E. Audia, James J. Droste, Deborah A. Evrard
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Patent number: 5525611Abstract: The invention provides lavendamycin analogs having the following formula: ##STR1## wherein X, Y and R.sup.1 through R.sup.9 are defined in the specification, and salts of these analogs. The invention also provides a method of making the lavendamycin analogs. The lavendamycin analogs have antitumor and antimicrobial activity.Type: GrantFiled: June 4, 1993Date of Patent: June 11, 1996Inventors: Mohammad Behforouz, Ronald L. Merriman
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Patent number: 5512566Abstract: Compounds represented by the general formula I: ##STR1## are disclosed as useful in treating diseases of the central nervous system.Type: GrantFiled: October 25, 1993Date of Patent: April 30, 1996Assignee: Ortho Pharmaceutical CorporationInventors: Ellen W. Baxter, Allen B. Reitz
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Patent number: 5478836Abstract: Heterotricyclically substituted phenyl-cyclohexane-carboxylic acid derivatives are prepared by reacting the heterocyclic compounds with cyclohexanecarboxylic acid derivatives which are substituted by benzyl halide radicals. The compounds can be employed as active compounds in medicaments.Type: GrantFiled: March 11, 1994Date of Patent: December 26, 1995Assignee: Bayer AktiengesellschaftInventors: Ulrich E. Muller, Jurgen Dressel, Peter Fey, Rudolf H. Hanko, Walter Hubsch, Thomas Kramer, Matthias Muller-Gliemann, Martin Beuck, Stanislav Kazda, Stefan Wohlfeil, Andreas Knorr, Johannes-Peter Stasch, Siegfried Zaiss
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Patent number: 5466688Abstract: The compound of the formula: ##STR1## where R.sub.1 and R.sub.5 are independently hydrogen, fluorine, chlorine, bromine, iodine, trifluoromethyl, cyano, nitro, CO.sub.2 H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.8 cycloalkyl, cycloalkylalkyl, C.sub.3 -C.sub.8 cycloalkyloxy, C.sub.2 -C.sub.7 alkylcarbonyl, C.sub.2 -C.sub.7 alkylcarbonyloxy, C.sub.2 -C.sub.7 alkoxycarbonyl, mono- or di-alkylaminocarbonyl, tetrazolyl, --OH, --(CH.sub.2).sub.1-6 OH, --SH, --NH.sub.2 or --(CH.sub.2).sub.1-6 NR.sub.8 R.sub.9 where R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.7 alkylcarbonyl, C.sub.2 -C.sub.7 alkoxycarbonyl and R.sub.9 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.2 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.3 and R.sub.4 are hydrogen or taken together with the carbon atoms to which they are attached form a double bond; R.sub.6 and R.sub.7 are independently H, C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.3 -C.sub.Type: GrantFiled: October 20, 1994Date of Patent: November 14, 1995Assignee: American Home Products CorporationInventors: Thomas J. Commons, Christa M. LaClair, Susan Christman
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Patent number: 5434264Abstract: Cognitive defeciencies or neurological dysfunction in mammals are treated with .alpha.,.alpha.-disubstituted aromatic or heteroaromatic compounds. The compounds have the formula: ##STR1## or a salt thereof wherein X and Y are taken together to form a saturated or unsaturated carbocyclic or heterocyclic first ring and the shown carbon in said ring is .alpha. to at least one additional aromatic ring or heteroaromatic ring fused to the first ring;one of Het.sup.1 or Het.sup.2 is 2, 3, or 4-pyridyl or 2, 4, or 5-pyrimidinyl and the other is selected from(a) 2, 3, or 4-pyridyl,(b) 2, 4, or 5-pyrimidinyl,(c) 2-pyrazinyl,(d) 3, or 4-pyridazinyl,(e) 3, or 4-pyrazolyl,(f) 2, or 3-tetrahydrofuranyl, and(g) 3-thienyl.Type: GrantFiled: September 30, 1992Date of Patent: July 18, 1995Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Richard A. Earl, Melvyn J. Myers, Victor J. Nickolson
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Patent number: 5430038Abstract: Novel 2-(4-piperidinyl)-1H-pyrido[4,3-b]indol-1-ones and related compounds, intermediates and processes for the preparation thereof, and methods of treating psychoses employing compounds and compositions thereof are disclosed.Type: GrantFiled: November 8, 1993Date of Patent: July 4, 1995Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Lawrence L. Martin, Denise M. Flanagan, Joseph F. Payack
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Patent number: 5424321Abstract: Compounds having both calcium antagonist and antioxidant activity are disclosed. The compounds are useful in preventing or alleviating damage to tissues at the cellular level. Methods of treatment which employ these properties of the compounds and corresponding pharmaceutical compositions are also disclosed.Type: GrantFiled: December 8, 1993Date of Patent: June 13, 1995Assignee: Alcon Laboratories, Inc.Inventors: Mark R. Hellberg, George Barnes, Robert J. Collier, Jr.
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Patent number: 5414002Abstract: 5- or 6-substituted .beta.-carboline-3-carboxylic acid esters of Formula I ##STR1## wherein R.sup.1 is hydrogen, nitrilo, halogen, lower alkyl or lower alkoxy, andR.sup.3 is a branched C.sub.3-6 alkyl group which is optionally substituted by halogen, or a C.sub.3-6 cycloalkyl group which is optionally methyl-substituted, are valuable pharmaceuticals.Type: GrantFiled: October 3, 1989Date of Patent: May 9, 1995Assignee: Schering AktiengesellschaftInventors: Helmut Biere, Andreas Huth, Dieter Rahtz, Ralph Schmiechen, Dieter Seidelmann, Wolfgang Kehr, Herbert H. Schneider, Mogens Engelstoft, Bondo J. Hansen, Frank Waetjen, Tage Honore
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Patent number: 5405852Abstract: The present invention relates to certain novel amide ##STR1## derivatives which are pyrido[3,4-b]indol-2-ylacetamides which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these amide derivatives, processes for preparing the amide derivatives, pharmaceutical compositions containing such amide derivatives and methods for their use.Type: GrantFiled: June 3, 1993Date of Patent: April 11, 1995Assignee: Zeneca LimitedInventors: Chris A. Veale, Peter Warner, Donald J. Wolanin
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Patent number: 5360800Abstract: The invention relates to tricyclic lactams of the general formula (I) ##STR1## wherein Im represents an imidazolyl group of the formula: ##STR2## and R.sup.1 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, phenyl C.sub.1-3 alkyl, phenylmethoxymethyl, phenoxyethyl or phenoxymethyl,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 phenyl C.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 alkhyl group;n represents 2 or 3; and physiologically acceptable salts and solvates thereof.The compounds are potent and selective antagonists of the effect of 5-HT at 5-HT.sub.3 receptors and are useful, for example, in the treatment of psychotic disorders, anxiety, and nausea and vomiting.Type: GrantFiled: August 7, 1991Date of Patent: November 1, 1994Assignee: Glaxo Group LimitedInventors: Ian H. Coates, Peter C. North, Alexander W. Oxford
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Patent number: 5350750Abstract: .beta.-carboline-3-hydroxyalkylcarboxylic acid ester derivatives of formula I ##STR1## in which R.sup.A, n, R.sup.4 and R.sup.3, have the meaning indicated in the claims, as well as their production and their use in pharmaceutical agents are described.Type: GrantFiled: March 1, 1993Date of Patent: September 27, 1994Assignee: Schering AktiengesellschaftInventors: Andreas Huth, Martin Kruger, Dieter Seidelmann, Ralph Schmiechen, Werner Krause, Herbert Schneider, Lechoslaw Turski
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Patent number: 5348958Abstract: Hetaryloxy-.beta.-carbolines of formula I ##STR1## in which R.sup.A means a benzocondensed hetaryl radical with 1-2 nitrogen atoms optionally substituted with halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, trifluoromethyl or SO.sub.2 --R.sup.1 or a 5- or 6-membered hetaryl radical with 1-2 nitrogen atoms substituted with halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, trifluoromethyl or SO.sub.2 --R.sup.1 are useful pharmaceutical agents.Type: GrantFiled: June 5, 1992Date of Patent: September 20, 1994Assignee: Schering AktiengesellschaftInventors: Martin Kruger, Andreas Huth, Dieter Seidelmann, Herbert Schneider, Lechoslaw Turski, David N. Stephens
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Patent number: 5329009Abstract: Disclosed is chemoselective phenylation of 5-hydroxy-.beta.-carbolines in the presence of weak bases while adding water.Type: GrantFiled: March 19, 1992Date of Patent: July 12, 1994Assignee: Schering AktiengesellschaftInventors: Gregor Haffer, Helmut Borner, Klaus Nickisch, Julius Deutsch
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Patent number: 5300645Abstract: The present invention provides a new Pictet-Spengler process useful for preparing tetrahydro-beta-carboline compounds.Type: GrantFiled: April 14, 1993Date of Patent: April 5, 1994Assignee: Eli Lilly and CompanyInventors: James E. Audia, James J. Droste, Deborah A. Evrard
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Patent number: 5272269Abstract: Polycyclic cognition enhancers having the general formula (1a), (1b) or (1c) are provided: ##STR1## wherein: R.sub.1 is a heterocyclic aromatic moiety such as a 4-pyridyl, 2-pyridyl, 4-pyrimidyl, or pyrazinyl group;R.sub.2 and R.sub.3 are independently H, F, Cl, Br, NO.sub.2, CONH.sub.2, CON(R.sub.4)(R.sub.4 '), S(O).sub.m R.sub.4, CF.sub.3, or N(R.sub.4)(R.sub.4 ');R.sub.4 and R.sub.4 ' are independently H, alkyl having from 1 to 4 carbon atoms, CH.sub.2 Phe--W, or Phe--W;Phe is a phenyl group;R.sub.5 is --(CH.sub.2).sub.n --Y or --OCOR.sub.4 ;Y is H, OH, NH.sub.2, NHR.sub.4, N(R.sub.4)(R.sub.4 '), NHCOR.sub.4, NHCO.sub.2 R.sub.4, NHS(O).sub.2 R.sub.4, F, Cl, Br, OR.sub.4, S(O).sub.m R.sub.4, CO.sub.2 H, CO.sub.2 R.sub.4, CN, CON(R.sub.4)(R.sub.4 '), CONHR.sub.4, CONH.sub.2, COR.sub.4, Phe, Phe--W, --C.tbd.CCO.sub.2 R.sub.4, --CH.dbd.CHR.sub.4, --C.tbd.CR.sub.4, or a heterocyclic aromatic moiety such as a 4-pyridyl, 2-pyridyl, 4-pyrimidyl, or pyrazinyl group;W is F, Cl, Br, R.sub.4, OR.sub.4, NO.sub.2, NH.Type: GrantFiled: January 16, 1992Date of Patent: December 21, 1993Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: James H. Jensen, Timothy D. Costello, Leon De Brabander, Jr., Matthew E. Voss
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Patent number: 5254563Abstract: Compounds of formula I ##STR1## in which R.sup.A, B (which is CR.sup.4) and R.sup.3 and have the meaning indicated in the application, as well as their production and their use in pharmaceutical agents, are described.Type: GrantFiled: October 23, 1991Date of Patent: October 19, 1993Assignee: Schering AktiengesellschaftInventors: Andreas Huth, Martin Kruger, Dieter Rahtz, Dieter Seidelmann, Ralph Schmiechen, Lechoslaw Turski, John S. Andrews, Herbert H. Schneider
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Patent number: 5252580Abstract: Disclosed are indole derivatives of formula (I) ##STR1## wherein Y represents H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy or halogen;Z represents --CH.sub.2 N(R.sub.5)--;R represents H or --CH.sub.2 CH.sub.2 X where X represents pyridyl, aralkyloxy or substituted amino of NR.sub.6 R.sub.7 where R.sub.6 represents H, C.sub.1 -C.sub.6 alkyl, aralkyl, C.sub.1 -C.sub.6 alkoxycarbonyl, aralkyloxycarbonyl or halogenated C.sub.1 -C.sub.6 alkoxycarbonyl and R.sub.7 represents H, C.sub.1 -C.sub.6 alkyl or aralkyl, or together with R.sub.2 may form a ring of --(CH.sub.2).sub.n -- (n is 1-4) or ##STR2## R.sub.1 represents H, C.sub.1 -C.sub.6 alkyl, aralkyl or arylsulfonyl; R.sub.2 represents C.sub.1 -C.sub.6 alkyl, hydroxy, C.sub.1 -C.sub.6 alkoxy or aralkyloxy;R.sub.3 represents H, C.sub.1 -C.sub.6 alkyl, aralkyl or halogenated C.sub.1 -C.sub.6 alkyl;R.sub.4 and R.sub.5 may be the same or different and each represents H, C.sub.1 -C.sub.6 alkyl or aralkyl or both may together form a ring of --(CH.sub.2).sub.Type: GrantFiled: September 18, 1992Date of Patent: October 12, 1993Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Toshihiro Takahashi, Hitoshi Inoue, Masato Horigome, Kenichi Momose, Masanori Sugita, Kouichi Katsuyama, Chikako Suzuki, Shinji Nagai, Masao Nagase, Koichi Nakamaru
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Patent number: 5244905Abstract: Novel substituted polyhydro-.beta.-carboline derivatives useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, or as antipsychotic agents are disclosed. Further the compounds are antianxiety agents and antiulcer agents. Further, the compounds are useful for treating and/or preventing panic attacks. They are agents useful for preventing the response to withdrawal from chronic treatment with or use of nicotine, caffeine, diazepam, alcohol, cocaine or opioids. Also disclosed are pharmaceutical compositions and methods of treatment using the compounds as well as processes for preparing them and novel intermediates useful in their preparation. An additional feature of the invention is the use of the subject compounds in diagnostic compositions.Type: GrantFiled: July 12, 1991Date of Patent: September 14, 1993Assignee: Warner-Lambert CompanyInventors: David C. Horwell, Edward Roberts, Uwe Trostmann
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Patent number: 5223509Abstract: This invention relates to certain .beta.-carbolines, which are antagonists of the functions of cholecystokinin (CCK) and gastrin, to pharmaceutical compositions comprising these compounds, and to the use of these compounds in the prevention and treatment of disorders of the gastrointestinal, central nervous and appetite-regulatory systems of mammals, especially of humans.Type: GrantFiled: February 21, 1992Date of Patent: June 29, 1993Assignee: Merck & Co., Inc.Inventor: Ben E. Evans
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Patent number: 5196534Abstract: The invention relates to a process for the preparation of a compound of formula (I) ##STR1## wherein R represent a hydrogen atom or a methyl or ethyl group, which comprises cyclising a compound of formul (IV) ##STR2## Where R represents a hydrogen atom, the compound of formula (IV) may optionally be alkylated to produce a compound in whcich R is methyl or ethyl.The compound of formula (I) is useful as an intermediate in the preparation of 2,3,4,5-tetrahydro-2-[(imidazol-4(or 5)-yl)methyl]-1H-pyrido[4,3-b]indol-1-ones having 5-HT.sub.3 antagonist activity.Type: GrantFiled: May 22, 1991Date of Patent: March 23, 1993Assignee: Glaxo Group LimitedInventors: John W. F. Whitehead, Keith Mills, Ian H. Coates, Alexander W. Oxford, Peter C. North
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Patent number: 5189041Abstract: 5-HT.sub.3 receptor antagonist compounds of the formula ##STR1## in which Z is --O--, --S-- or --N(R.sup.2)--; R.sup.1 and R.sup.2 are independently selected from hydrogen and lower alkyl or are together --(CH.sub.2).sub.n -- wherein n is 2 to 4; and R.sup.3 is selected from ##STR2## and the pharmaceutically acceptable salts, individual isomers, compositions, and methods of use thereof.Type: GrantFiled: November 16, 1990Date of Patent: February 23, 1993Assignee: Syntex (U.S.A.) Inc.Inventors: Jacob Berger, Robin D. Clark
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Patent number: 5185447Abstract: Ketones having formulas (1)-(3) are provided by improved methods which involve the treatment of compounds having formulas (9)-(11) with aqueous base. ##STR1## wherein R.sub.x is NO.sub.2.Type: GrantFiled: January 29, 1992Date of Patent: February 9, 1993Assignee: Du Pont Merck Pharmaceutical CompanyInventor: Edward C. Crapps
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Patent number: 5183820Abstract: The invention provides potent and selective antagonists of 5-HT at 5-HT.sub.3 receptors which are tricyclic lactams of the formula (I) ##STR1## wherein Im represents an imidazolyl group of the formula: ##STR2## and R.sup.1 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, phenylC.sub.1-3 alkyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CONR.sup.5 R.sup.6 or --SO.sub.2 R.sup.5 ;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 same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group;Y represents the group CH.dbd.CH or (CH.sub.2).sub.n, wherein n represents 2 or 3;Q represents a halogen atom, or a group selected from hydroxy, C.sub.1-4 alkoxy, phenylC.sub.1-3 alkoxy, C.sub.Type: GrantFiled: April 26, 1991Date of Patent: February 2, 1993Assignee: Glaxo Group LimitedInventors: Ian H. Coates, Alexander W. Oxford, Peter C. North, Barry J. Price
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Patent number: 5162336Abstract: Disclosed are tetrahydro-pyrido-indoles having the general formula ##STR1## which are antagonists towards the neuropeptides cholexystokinin and gastrin processing valuable activities for the treatment of cholecystokinin or gastrin-related disorders of the gastrointestinal, central nervous and appetite regulatory systems and their pharmaceutical compositions and processes for their preparation.Type: GrantFiled: August 24, 1990Date of Patent: November 10, 1992Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: Bruce F. Molino, Paul R. Darkes, William R. Ewing