Benzene Ring Bonded Directly To Ring Carbon Of The Hetero Ring Patents (Class 540/595)
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Patent number: 9072749Abstract: Methods and compounds are disclosed for treating dry age-related macular degeneration, and preventing or delaying the onset of wet age-related macular degeneration.Type: GrantFiled: November 30, 2009Date of Patent: July 7, 2015Inventors: Joseph Weinstock, Sarah Jane Paikowsky
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Publication number: 20140316130Abstract: This invention relates to the miniaturisation of radiosyntheses onto microfabricated devices, and in particular to use of microfabricated devices for radiosynthesis, isolation, and analysis of radiotracers for use in Positron Emission Tomography (PET).Type: ApplicationFiled: April 15, 2014Publication date: October 23, 2014Applicant: HAMMERSMITH IMANET LIMITEDInventors: FRANK BRADY, SAJINDER KAUR LUTHRA, JAMES MILLAR GILLIES, NICHOLAS TOBY JEFFREY
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Patent number: 8859001Abstract: Formulations of fenoldopam are disclosed for repeated administration or continued slow release administration, over prolonged periods of time or targeted slow and regulated delivery. The formulations include those formulations that increase the bioavailability of fenoldopam after oral intake, particularly lipid based nano dispersions and pronanodispersions and surfactant rich formulations. This may be accomplished by entrapment in nanoparticles or liposomal formulations or conjugation to a polymer or small molecule via a soft bond.Type: GrantFiled: October 20, 2008Date of Patent: October 14, 2014Inventors: Mia Levite, Avi Domb
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Publication number: 20140296514Abstract: The compounds of the present invention are represented by the following aryl- and heteroaryl-substituted tetrahydrobenzazepine and dihydrobenzazapine derivatives having formulae I(A-E) and formula (II): where the carbon atom designated * is in the R or S configuration, and the substituents X and R1-R9 are as defined herein.Type: ApplicationFiled: June 13, 2014Publication date: October 2, 2014Inventors: Bruce F. Molino, Shuang Liu, Aruna Sambandam, Peter R. Guzzo, Min Hu, Congxiang Zha, Kassoum Nacro, David D. Manning, Matthew L. Isherwood, Kristen N. Fleming, Wenge Cui, Richard E. Olson
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Patent number: 8754073Abstract: Piperidinodihydrothienopyrimidines of formula 1 wherein X is SO or SO2 (preferably SO), and R1, R2, R3, and R4 may have the meanings given in the disclosure and claims, pharmacologically acceptable salts thereof, and pharmaceutical compositions containing these compounds. These piperidinodihydrothienopyrimidines are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system, or cancers.Type: GrantFiled: October 16, 2008Date of Patent: June 17, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Pascale Pouzet, Ralf Anderskewitz, Horst Dollinger, Dennis Fiegen, Thomas Fox, Rolf Goeggel, Christoph Hoenke, Domnic Martyres, Peter Nickolaus, Klaus Klinder
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Patent number: 8741890Abstract: The present invention relates to new substituted prolinamides of general formula (I) wherein D, Y, A, B, R3, R4 and R5 are defined as in the specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.Type: GrantFiled: November 14, 2008Date of Patent: June 3, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Kai Gerlach, Herbert Nar, Henning Priepke, Annette Schuler-Metz, Wolfgang Wienen
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Patent number: 8633184Abstract: The invention is directed to compounds of Formula (I) useful as PPAR agonists. Pharmaceutical compositions and methods of treating one or more conditions including, but not limited to, diabetes, nephropathy, neuropathy, retinopathy, polycystic ovary syndrome, hypertension, ischemia, stroke, irritable bowel disorder, inflammation, cataract, cardiovascular diseases, Metabolic X Syndrome, hyper-LDL-cholesterolemia, dyslipidemia (including hypertriglyceridemia, hypercholesterolemia, mixed hyperlipidemia, and hypo-HDL-cholesterolemia), atherosclerosis, obesity, and other disorders related to lipid metabolism and energy homeostasis complications thereof, using compounds of the invention are also described.Type: GrantFiled: January 19, 2010Date of Patent: January 21, 2014Assignee: Janssen Pharmaceutica N.V.Inventors: Gee-Hong Kuo, Yan Zhang, Lan Shen, Songfeng Lu, Keith T. Demarest, Patricia Pelton
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Patent number: 7858618Abstract: The present invention relates to compounds of general formula I wherein A, B, D, Y, R1, R2, R3, R4 and R5 are defined as in the specification, the enantiomers, the diastereomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and the use thereof.Type: GrantFiled: August 17, 2007Date of Patent: December 28, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Iris Kauffmann-Hefner, Norbert Hauel, Rainer Walter, Heiner Ebel, Henri Doods, Angelo Ceci, Annette Schuler-Metz, Ingo Konetzki
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Publication number: 20100316731Abstract: Methods and compounds are disclosed for treating dry age-related macular degeneration, and preventing or delaying the onset of wet age-related macular degeneration.Type: ApplicationFiled: May 30, 2008Publication date: December 16, 2010Inventors: Joseph Weinstock, Sarah Jane Paikowsky
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Publication number: 20100311728Abstract: Provided herein methods of screening for potential antidepressant compounds effective to increase production of cellular CDP-diacylglycerol and synthesis of inositol phospholipid in depression-related areas of the brain. Also, provided are methods of diagnosing and treating depressive or mood disorders in a subject by administering these screened antidepressant compounds. Further provided is a method of determining the therapeutic efficacy of an antidepressant drug regimen by comparing the ratio of CDP-diacylglycerol/inositol phosphate after treatment to a basal ratio in a subject.Type: ApplicationFiled: July 23, 2010Publication date: December 9, 2010Inventor: Ashiwel S. Undieh
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Publication number: 20100075926Abstract: The invention provides methods and compounds for the treatment of neurological disorders, including Alzheimer's disease, Parkinson's disease, Huntington's disease, ALS (Amyotrophic Lateral Sclerosis), traumatic brain injury, ischemic brain injury or a stroke. In one aspect the compounds are HDAC1 activators. Exemplary HDAC1 activators include metal chelators, iron chelators, deferoxamin, flavonoids, compounds comprising a catechol moity, ginkgetin K, Chembridge 5104434, sciadopilysin, tetrahydrogamboic acid, TAM-11, LY 235959, CGS 19755, SK&F 97541, etidronic acid, levonordefrin, methyldopa, ampicillin trihydrate, D-aspartic acid, gamma-D-glutamylaminomethylsulfonic acid, phenazopyridine to hydrochloride, oxalamine citrate salt, podophyllotoxin, SK&F 97541, (+-)-4-amino-3-(5-chloro-2-thienyl)-butanoic acid, (RS)-(tetrazol-5-yl) glycine, R(+)-SKF-81297, gambogic acid, and derivatives thereof.Type: ApplicationFiled: July 23, 2009Publication date: March 25, 2010Inventors: Li-Huei Tsai, Stephen J. Haggarty, Dohoon Kim
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Patent number: 7678786Abstract: The invention is directed to compounds of Formula (I) useful as PPAR agonists. Pharmaceutical compositions and methods of treating one or more conditions including, but not limited to, diabetes, nephropathy, neuropathy, retinopathy, polycystic ovary syndrome, hypertension, ischemia, stroke, irritable bowel disorder, inflammation, cataract, cardiovascular diseases, Metabolic X Syndrome, hyper-LDL-cholesterolemia, dyslipidemia (including hypertriglyceridemia, hypercholesterolemia, mixed hyperlipidemia, and hypo-HDL-cholesterolemia), atherosclerosis, obesity, and other disorders related to lipid metabolism and energy homeostasis complications thereof, using compounds of the invention are also described.Type: GrantFiled: April 17, 2007Date of Patent: March 16, 2010Assignee: Janssen Pharmaceutica NVInventors: Gee-Hong Kuo, Yan Zhang, Lan Shen, Songfeng Lu, Keith T. Demarest, Patricia Pelton
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Patent number: 7662956Abstract: The present application relates to novel tetrahydrobenzo[d]azepin-2-one derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders, especially of dyslipidaemias, arteriosclerosis, restenosis and ischaemias.Type: GrantFiled: February 1, 2005Date of Patent: February 16, 2010Assignee: Bayer Shering Pharma AGInventors: Nils Griebenow, Timo Flessner, Michael Härter, Martin Raabe, Anja Buchmüller, Hilmar Bischoff, Peter Ellinghaus, Peter Kolkhof
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Patent number: 7504391Abstract: The present invention provides compounds, which, are novel antagonists for D1/D5 receptors as well as methods for preparing such compounds. In another embodiment, the invention provides pharmaceutical compositions comprising such D1/D5 receptor antagonists as well as methods of using them to treat CNS disorders, obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: GrantFiled: May 20, 2004Date of Patent: March 17, 2009Assignee: Schering CorporationInventors: Duane A. Burnett, William J. Greenlee, Brian McKittrick, Jing Su, Zhaoning Zhu, Thavalakulamgara K. Sasikumar, Robert Mazzola, Li Qiang, Yuanzan Ye
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Publication number: 20080166298Abstract: The present invention relates to radiolabelled compounds of formula (I), which are useful for the labelling and diagnostic imaging of histamine H3 receptor functionality.Type: ApplicationFiled: January 5, 2006Publication date: July 10, 2008Inventor: Christophe Plisson
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Publication number: 20070281920Abstract: Compounds of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ar, R1 and R2 are defined herein. Also provided are pharmaceutical compositions, methods of preparing the compounds, and method of using the compounds for treatment of monoamine reuptake inhibitor-mediated diseases.Type: ApplicationFiled: May 31, 2007Publication date: December 6, 2007Inventors: Ryan Craig Schoenfeld, Robert James Weikert
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Patent number: 7008938Abstract: A benzene-fused heteroring derivative of formula (I) wherein all symbols are the same as described in the specification, and a non-toxic salt thereof. The compound of formula (I) has an inhibitory activity against cysteine protease and therefore it is useful as an agent for the prophylaxis and/or treatment of immune diseases (autoimmune diseases, infectious diseases, etc.), inflammatory diseases (inflammatory bowel diseases, multiple cerebrosclerosis, arthritis, etc.), nerve degeneration diseases (Alzheimer's disease, muscular dystrophy, etc.), bone resorption diseases (osteoporosis, etc.), respiratory system diseases, diabetes, shock, etc.Type: GrantFiled: July 29, 2004Date of Patent: March 7, 2006Assignee: Nokia CorporationInventors: Kazuyuki Ohmoto, Iori Itagaki
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Patent number: 6919332Abstract: The present invention relates to N-substituted-heteroaryloxy-aryloxy-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, A, Y, B, G, and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.Type: GrantFiled: April 28, 2003Date of Patent: July 19, 2005Assignee: Pfizer Inc.Inventors: Mark C. Noe, Lilli Ann Wolf-Gouveia
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Patent number: 6602864Abstract: The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.Type: GrantFiled: June 3, 1998Date of Patent: August 5, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Yong Mi Choi-Sledeski, Henry W. Pauls, Jeffrey N. Barton, William R. Ewing, Daniel M. Green, Michael R. Becker, Yong Gong
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Patent number: 6534496Abstract: The object of the present invention is to provide a prophylactic and/or therapeutic drug for obesity and obesity-associated diseasestor diabetes with a reduced risk for central side effects and high universality in usage. Another object of the present invention is to provide a pharmaceutical composition comprising a compound of the following formula: wherein Ar represents phenyl which may be substituted and/or condensed; n represents an integer of 1 to 10; R represents hydrogen or a hydrocarbon group which may be substituted, which may not be the same in its n occurrences; R may be bound to either Ar or a substituent for Ar; Y represents an amino group which may be subsituted or a nitrogen-containing saturated heterocyclic group which may be substituted, or a salt thereof, which can be used for a thermogenic agent, an antiobesity agent, a lipolytic agent, or a prophylactic and/or treating drug for obesity-associated diseases.Type: GrantFiled: October 7, 1999Date of Patent: March 18, 2003Assignee: Takeda Chemical Industries, Inc.Inventors: Yuji Ishihara, Yukio Fujisawa, Naoki Furuyama
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Publication number: 20030018024Abstract: A compound of the formulae (I) or (II): 1Type: ApplicationFiled: April 11, 2002Publication date: January 23, 2003Applicant: WyethInventors: Amedeo Arturo Failli, Thomas Joseph Caggiano, Jay Scott Shumsky, Eugene J. Trybulski, Kevin A. Memoli, John P. Dusza
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Publication number: 20030013873Abstract: Secondary amines of the formula 1Type: ApplicationFiled: June 19, 2002Publication date: January 16, 2003Inventors: Peter Neumann, Johann-Peter Melder, Christoph Benisch, Arthur Hohn, Joachim Pfeffinger
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Patent number: 6489354Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.Type: GrantFiled: March 1, 2000Date of Patent: December 3, 2002Assignee: Merck & Co., Inc.Inventors: Jianming Bao, Robert K. Baker, William H. Parsons, Kathleen Rupprecht
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Patent number: 6372764Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.Type: GrantFiled: March 1, 2000Date of Patent: April 16, 2002Assignee: Merck & Co., Inc.Inventors: Jianming Bao, Robert K. Baker, William H. Parsons, Kathleen Rupprecht
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Patent number: 6362201Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.Type: GrantFiled: March 1, 2000Date of Patent: March 26, 2002Assignee: Merck & Co., Inc.Inventors: Robert K. Baker, William H. Parsons, Kathleen Rupprecht
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Patent number: 6346527Abstract: A compound of the formula: wherein R1 is hydrogen or halogen, R2 is hydroxy, acyl(lower)alkoxy, hydroxy(lower)alkyl, lower alkoxy(lower)alkyl, lower alkylthio(lower)alkyl, mono(or di or tri)halo(lower)alkyl, (ethoxycarbonyl)amino, sulfamoylamino, (dimethylsulfamoyl)amino, N,N-di(lower)alkylamino(lower)alkyl, hydroxyimino(lower)alkyl, lower alkoxyimino(lower)alkyl, acyl, lower alkoxycarbonyl, carbamoyl, di(lower)alkylcarbamoyl, (amino(lower)alkyl)carbamoyl, N,N-di(lower)alkylamino(lower)alkylcarbamoyl, guanidinocarbonyl, morpholinylsulfonyl, sulfamoyl, lower alkylsulfamoyl, (lower alkylsulfonyl)(lower)alkyl, guanidinocarbonyl(lower)alkenyl, lower alkylthio, cyano, acyl(lower)alkyl, acyl(lower)alkenyl, aryl which has one or more substituent(s) or a heterocyclic group which has one or more substituent(s), and X is —O—, or a salt thereof.Type: GrantFiled: October 24, 2000Date of Patent: February 12, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kohei Takenaka, Yoshikazu Inoue, Masatoshi Minagawa, Atsushi Akahane
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Patent number: 6281227Abstract: The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, for treating a patient suffering from, or subject to, a physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.Type: GrantFiled: December 2, 1999Date of Patent: August 28, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Yong Mi Choi-Sledeski, Heinz W. Pauls, Jeffrey N. Barton, William R. Ewing, Daniel M. Green, Michael R. Becker, Yong Gong, Julian Levell
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Patent number: 6166037Abstract: The present invention is directed to pyrrolidine and piperidine compounds of the formula I: ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4a, R.sup.4b, R.sup.4c, R.sup.4d, R.sup.4e, R.sup.4f, R.sup.4g, R.sup.4h, m, n, x and y are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.Type: GrantFiled: August 27, 1998Date of Patent: December 26, 2000Assignee: Merck & Co., Inc.Inventors: Richard J. Budhu, Edward Holson, Jeffrey J. Hale, Christopher Lynch, Malcolm Maccoss, Scott C. Berk, Sander G. Mills, Christopher A. Willoughby
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Patent number: 5914319Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: September 1, 1995Date of Patent: June 22, 1999Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 5910494Abstract: The invention is concerned with novel hypolipidemic compounds of formula (I), with processes and novel intermedites for their preparation, pharmaceutical compositions containing them and with their use in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions, such as atherosclerosis.Type: GrantFiled: February 7, 1997Date of Patent: June 8, 1999Assignee: Glaxo Wellcome Inc.Inventor: Lawrence Edward Brieaddy
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Patent number: 5726159Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: September 1, 1995Date of Patent: March 10, 1998Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Robert T. Shuman, Gerald F. Smith, Michael R. Wiley
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Patent number: 5710130Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: September 1, 1995Date of Patent: January 20, 1998Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 5707966Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: September 1, 1995Date of Patent: January 13, 1998Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 5705487Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: September 1, 1995Date of Patent: January 6, 1998Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 5658899Abstract: The invention provides a series of crystalline salts of (S)-8-chloro-5-(5-bromo-2,3-dihydrobenzofuran-7-yl)-3-methyl-2,3,4,5-tetra hydro-1H-3-benzazepine-7-ol, their preparation and use as therapeutic agents.Type: GrantFiled: March 14, 1995Date of Patent: August 19, 1997Assignee: Novo Nordisk A/SInventors: Louis Brammer Hansen, Rolf Emil Amsler, Scott Eugene McGraw
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Patent number: 5599793Abstract: This invention relates to L-arginine aldehyde derivatives, having the Formula I ##STR1## where X and Y have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: March 2, 1995Date of Patent: February 4, 1997Assignee: Eli Lilly and CompanyInventors: Nickolay Y. Chirgadze, Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 5530125Abstract: A novel process for the preparation of .alpha.-substituted arylacetamides wherein the substituent is an aromatic group or a 1-alkenyl or 1-cycloalkenyl group and wherein the nitrogen atom carries no hydrogen atoms comprises the reaction of an arylacetamide having one or two hydrogen atoms on the .alpha.-carbon atom, wherein the nitrogen atom carries no hydrogen atoms, with a strong base in an inert aprotic organic solvent, followed by reaction with a zerovalent transition metal catalyst and then with a compound of the formula R.sup.4 --X, wherein R.sup.4 is selected from aromatic groups, 1-alkenyl groups and 1-cycloalkenyl groups and X is a particular leaving group, especially a triflate group. The .alpha.-substituted arylacetamides are useful as intermediates in the preparation (by reduction) of .alpha.-substituted arylethylamines, e.g., 1-substituted-2,3,4,5-tetrahydro-1H-3-benzazepines, having pharmacological activity. Certain benzazepines wherein the 1-substituent R.sup.4 is 1-(1-cycloalkenyl) are novel.Type: GrantFiled: August 19, 1994Date of Patent: June 25, 1996Assignee: Schering CorportionInventors: Joel G. Berger, Wei K. Chang, Joseph A. Kozlowski, Guowei Zhou
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Patent number: 5470850Abstract: 2,3,4,5-Tetrahydro-1H-3-benzazepines having the general formula ##STR1## wherein R.sup.1 is Cl or Br; R.sup.3 and R.sup.4 are hydrogen, halogen, CF.sup.3, CN, NO.sub.2, or NH.sub.2.The compounds are useful in treatment of certain disorders in the central nervous system.Type: GrantFiled: May 6, 1994Date of Patent: November 28, 1995Assignee: Novo Nordisk A/SInventors: Christian Foged, Rolf Holweg, Erik Nielsen
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Patent number: 5461148Abstract: Disclosed are a process and intermediates of the formulae ##STR1## wherein R is --CH.sub.2 OH or --OH and R.sup.3 is H or C.sub.1 -C.sub.6 alkyl; useful for preparing benzazepines of the formula ##STR2## having activity as selective D1 antangonists.Type: GrantFiled: September 27, 1993Date of Patent: October 24, 1995Assignee: Schering CorporationInventors: Guang-Zhong Wu, Martin Steinman, Yee-Shing Wong
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Patent number: 5446147Abstract: This invention relates to novel dopamine D-1 and D-2 imaginging agents which are both fluorinated and iodinated and can appropriately labelled for use in both PET and SPECT imaging. Compounds include S-(-)-2-fluoroethoxy-3-methyl-N-[(1-ethyl-2-pyrrolidinyl)methyl]-5-iodoben zamide and R(+)-2,3-dimethoxy-N-[(1-(4'-fluorobenzyl)-2-pyrrolidinyl)methyl]-5-iodobe nzamide.Type: GrantFiled: April 3, 1992Date of Patent: August 29, 1995Assignee: Trustees of the University of PennsylvaniaInventors: Hank F. Kung, Sumalee Chumpradit, Mei Ping Kung
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Patent number: 5273974Abstract: A condensed heterocyclic derivative of the formula (I): ##STR1## wherein X is an oxygen atom, a sulfur atom or R.sup.1 --N< wherein R.sup.1 is a hydrogen atom, a hydrocarbon group which may be substituted or an acyl group which may be substituted; R.sup.2 is a hydrogen atom or a hydrocarbon group which may be substituted; ring A is a benzene ring which may be substituted, k is a whole number of 0 to 3; m is a whole number of 1 to 8; and n is a whole number of 1 to 6, or a pharmaceutically acceptable salt thereof exhibiting high colinesterase inhibitory activity, and a method for producing the same.Type: GrantFiled: November 22, 1991Date of Patent: December 28, 1993Assignee: Takeda Chemical Industries, Ltd.Inventors: Giichi Goto, Yuji Ishihara, Masaomi Miyamoto
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Patent number: 5244881Abstract: The invention provides new inclusion compounds based on imipramine and cyclodextrin and pharmaceutical compositions which can be administered orally and are based on these new inclusion compounds.Type: GrantFiled: November 22, 1991Date of Patent: September 14, 1993Assignee: Rhone-Poulenc SanteInventor: Anne Coutel-Egros
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Patent number: 5216150Abstract: Novel quinoline sulfonamino derivatives having a vessel smooth muscle relaxation activity as well as a platelet agglutination inhibitory activity and inhibitory activity to protein kinase A, myosin light chain kinase, proteinkinase C, and calmodulindependent proteinkinase II, but having little action or cardio function; a process for the production of the derivatives, and a pharmaceutical composition containing the derivative.Type: GrantFiled: September 12, 1991Date of Patent: June 1, 1993Assignees: Hiroyoshi Hidaka, Tobishi Yakuhin Kogyo Kabushiki KaishaInventors: Hiroyoshi Hidaka, Tomohiko Ishikawa, Masatoshi Hagiwara, Tsutomu Inoue, Kenji Naitoh, Osamu Sakuma, Masayuki Yuasa, Tadashi Morita, Tadashi Toshioka, Isao Umezawa, Takashi Inaba
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Patent number: 5079243Abstract: Novel 2, 3, 4, 5-tetrahydro-1H-3-benzazepines, which in the 7-position have a methoxymethyloxy group, in the 8-position hydrogen, halogen, or a nitro group and in the 5-position have an optionally substituted phenyl ortho-fused ring-system, with interesting effects on the central nervous system.Type: GrantFiled: February 8, 1990Date of Patent: January 7, 1992Assignee: Novo Nordisk A/SInventors: Louis B. Hansen, Kristian T. Hansen
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Patent number: 5017571Abstract: Compounds having the formula ##STR1## wherein R.sup.1, R.sup.4, R.sup.6, R.sup.7, and R.sup.8 are hydrogen or a substituent, R.sup.2 is a substituent, R.sup.5 is an optionally-substituted bicyclic ring system, especially a 7-benzofuranyl or 2,3-dihydrobenzofuran-7-yl substituent, R.sup.9 is hydrogen, alkyl, alkoxycarbonyl or, together with R.sup.8, forms the remainder of a heterocyclic ring, their pharmaceutically-accceptable salts, as well as their pharmaceutical compositions and use as prodrugs for compounds active for the treatment of mental disorders, are disclosed.Type: GrantFiled: February 28, 1989Date of Patent: May 21, 1991Assignee: Novo Nordisk A/SInventors: Kristian T. Hansen, Hans Bundgaard, Peter Faarup
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Patent number: 5015639Abstract: Disclosed herein are novel 1-substituted-2,3,4,5-tetrahydro-1H-3-benzazepines of the general formula I: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are specified substituents.R.sup.1 is preferably --X.sup.6, --CHR.sup.7 R.sup.8, cycloalkyl, cycloalkenyl, ##STR2## or pyrrolyl where m is 1, R.sup.6 represents .dbd.H, phenyl, substituted phenyl, aralkyl, alkyl, cycloalkyl, haloalkyl or alkoxyalkyl, R.sup.7 represents H or alkyl preferably H, R.sup.8 represents cycloalkyl, cycloalkenyl, haloalkyl, alkoxyalkyl, alkenyl or alkynyl and R.sup.9 represents alkyl, aloxy or alkoxyalkyl.R.sup.2 preferably represents --H and R.sup.3 --CH.sub.3, and R.sup.4 is preferably halogen and R.sup.5 is preferably OH, OCO.R.sup.9 or --O(CR.sup.7).sub.2.OCO.R.sup.13 where R.sup.7 represents hydrogen, R.sup.9 is as defined above and R.sup.13 represents alkyl. The compounds of the formula I are indicated as being useful in the treatment of psychoses, depression and pain.Type: GrantFiled: March 13, 1989Date of Patent: May 14, 1991Assignee: Schering CorporationInventors: Joel G. Berger, Wei K. Chang, Marjorie Peters
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Patent number: 5010074Abstract: Novel 2,3,4,5-tetrahydro-1H-3-benzazepines having the formula ##STR1## wherein R.sup.3 represents H, C.sub.1-3 -alkyl or C.sub.3-7 -cycloalkyl; R.sup.4 represents hydrogen or R.sup.4 together with R.sup.10 represents a bridge which connects the positions to which R.sup.4 and R.sup.10 are linked, said bridge being --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --O--CH.sub.2 -- or --S--CH.sub.2 --;R.sup.7 represent hydroxy, lower alkoxy;R.sup.10, R.sup.11, R.sup.12 independently represent hydrogen or halogen or alkyl or alkoxy or trifluoromethyl, or R.sup.10 together with R.sup.4 represents a bridge as described in connection with the definition of R.sup.4 ; or R.sup.10 together with R.sup.11 represents a bridge or R.sup.11 together with R.sup.12 represents a bridge, the bridge in both cases being chosen among --O--CH.sub.2 --CH.sub.2 --, --O--CH.sub.2 --CH.sub.2 --CH.sub.2 --, --O-CH.dbd.CH--, --CH.sub.2 -CH.sub.2 -CH.sub.2 --, --CH.sub.2 -CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2 --;R.sup.Type: GrantFiled: June 12, 1989Date of Patent: April 23, 1991Assignee: Novo Nordisk A/SInventors: Frederik Gronwald, Peter H. Andersen, Peter Faarup, Erling Guddal, Kristian T. Hansen, Louis B. Hansen, Erik B. Nielsen
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Patent number: 4861771Abstract: Prodrug carbamate derivatives of fenoldopam which provide fenoldopam plasma levels of similar magnitude and over a much longer period of time than the parent compound. An absence of a high initial peak effect associated with the parent compound is noted. A lead compound of the series is 6-chloro-7,8-diethylcarbamoyl-1-(4'-ethylcarbamoylphenyl)-2,3,4,5-tetrahyd ro-1H-3-benzazepine. The R-enantiomers are the most biologically active and preferred compounds.Type: GrantFiled: January 27, 1989Date of Patent: August 29, 1989Assignee: SmithKline Beckman CorporationInventors: Dimitri Gaitanopoulos, Bruce Mico, Joseph Weinstock
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Patent number: 4824839Abstract: Sulfinyl and sulfonyl substituted 3-benzazepine compounds are useful in treating gastrointestinal motility disorders and emesis. A particular compound of this invention is 7-methylsulfonyl-2,3,4,5-tetrahydro-1H-3-benzazepine.Type: GrantFiled: March 14, 1988Date of Patent: April 25, 1989Assignee: SmithKline Beckman CorporationInventors: William E. Bondinell, Herbert S. Ormsbee, III
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Patent number: 4751222Abstract: Novel 2,3,4,5-tetrahydro-1H-3-benzazepines which in the 5-position have furyl, thienyl, pyridyl, or ring systems consisting of phenyl ortho condensed with a benzen, cyclohexan, cyclohexen, cyclopentan or cyclopenten ring wherein one of the carbon atoms may be exchanged with oxygen, sulphur or nitrogen, have interesting central nervous system and cardiovascular effects.Type: GrantFiled: April 21, 1986Date of Patent: June 14, 1988Assignee: Novo Industri A/SInventors: Claus Braestrup, Peter H. Andersen, Poul Borrevang, Frederik C. Gr nvald, Louis B. Hansen, Rolf Hohlweg