Benzene Ring Bonded Directly To Ring Carbon Of The Hetero Ring Patents (Class 540/595)
  • Patent number: 9072749
    Abstract: 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: Grant
    Filed: November 30, 2009
    Date of Patent: July 7, 2015
    Inventors: Joseph Weinstock, Sarah Jane Paikowsky
  • Publication number: 20140316130
    Abstract: 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: Application
    Filed: April 15, 2014
    Publication date: October 23, 2014
    Applicant: HAMMERSMITH IMANET LIMITED
    Inventors: FRANK BRADY, SAJINDER KAUR LUTHRA, JAMES MILLAR GILLIES, NICHOLAS TOBY JEFFREY
  • Patent number: 8859001
    Abstract: 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: Grant
    Filed: October 20, 2008
    Date of Patent: October 14, 2014
    Inventors: Mia Levite, Avi Domb
  • Publication number: 20140296514
    Abstract: 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: Application
    Filed: June 13, 2014
    Publication date: October 2, 2014
    Inventors: 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
  • Patent number: 8754073
    Abstract: 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: Grant
    Filed: October 16, 2008
    Date of Patent: June 17, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Pascale Pouzet, Ralf Anderskewitz, Horst Dollinger, Dennis Fiegen, Thomas Fox, Rolf Goeggel, Christoph Hoenke, Domnic Martyres, Peter Nickolaus, Klaus Klinder
  • Patent number: 8741890
    Abstract: 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: Grant
    Filed: November 14, 2008
    Date of Patent: June 3, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Kai Gerlach, Herbert Nar, Henning Priepke, Annette Schuler-Metz, Wolfgang Wienen
  • Patent number: 8633184
    Abstract: 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: Grant
    Filed: January 19, 2010
    Date of Patent: January 21, 2014
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Gee-Hong Kuo, Yan Zhang, Lan Shen, Songfeng Lu, Keith T. Demarest, Patricia Pelton
  • Patent number: 7858618
    Abstract: 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: Grant
    Filed: August 17, 2007
    Date of Patent: December 28, 2010
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Iris Kauffmann-Hefner, Norbert Hauel, Rainer Walter, Heiner Ebel, Henri Doods, Angelo Ceci, Annette Schuler-Metz, Ingo Konetzki
  • Publication number: 20100316731
    Abstract: 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: Application
    Filed: May 30, 2008
    Publication date: December 16, 2010
    Inventors: Joseph Weinstock, Sarah Jane Paikowsky
  • Publication number: 20100311728
    Abstract: 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: Application
    Filed: July 23, 2010
    Publication date: December 9, 2010
    Inventor: Ashiwel S. Undieh
  • Publication number: 20100075926
    Abstract: 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: Application
    Filed: July 23, 2009
    Publication date: March 25, 2010
    Inventors: Li-Huei Tsai, Stephen J. Haggarty, Dohoon Kim
  • Patent number: 7678786
    Abstract: 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: Grant
    Filed: April 17, 2007
    Date of Patent: March 16, 2010
    Assignee: Janssen Pharmaceutica NV
    Inventors: Gee-Hong Kuo, Yan Zhang, Lan Shen, Songfeng Lu, Keith T. Demarest, Patricia Pelton
  • Patent number: 7662956
    Abstract: 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: Grant
    Filed: February 1, 2005
    Date of Patent: February 16, 2010
    Assignee: Bayer Shering Pharma AG
    Inventors: Nils Griebenow, Timo Flessner, Michael Härter, Martin Raabe, Anja Buchmüller, Hilmar Bischoff, Peter Ellinghaus, Peter Kolkhof
  • Patent number: 7504391
    Abstract: 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: Grant
    Filed: May 20, 2004
    Date of Patent: March 17, 2009
    Assignee: Schering Corporation
    Inventors: Duane A. Burnett, William J. Greenlee, Brian McKittrick, Jing Su, Zhaoning Zhu, Thavalakulamgara K. Sasikumar, Robert Mazzola, Li Qiang, Yuanzan Ye
  • Publication number: 20080166298
    Abstract: 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: Application
    Filed: January 5, 2006
    Publication date: July 10, 2008
    Inventor: Christophe Plisson
  • Publication number: 20070281920
    Abstract: 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: Application
    Filed: May 31, 2007
    Publication date: December 6, 2007
    Inventors: Ryan Craig Schoenfeld, Robert James Weikert
  • Patent number: 7008938
    Abstract: 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: Grant
    Filed: July 29, 2004
    Date of Patent: March 7, 2006
    Assignee: Nokia Corporation
    Inventors: Kazuyuki Ohmoto, Iori Itagaki
  • Patent number: 6919332
    Abstract: 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: Grant
    Filed: April 28, 2003
    Date of Patent: July 19, 2005
    Assignee: Pfizer Inc.
    Inventors: Mark C. Noe, Lilli Ann Wolf-Gouveia
  • Patent number: 6602864
    Abstract: 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: Grant
    Filed: June 3, 1998
    Date of Patent: August 5, 2003
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Yong Mi Choi-Sledeski, Henry W. Pauls, Jeffrey N. Barton, William R. Ewing, Daniel M. Green, Michael R. Becker, Yong Gong
  • Patent number: 6534496
    Abstract: 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: Grant
    Filed: October 7, 1999
    Date of Patent: March 18, 2003
    Assignee: Takeda Chemical Industries, Inc.
    Inventors: Yuji Ishihara, Yukio Fujisawa, Naoki Furuyama
  • Publication number: 20030018024
    Abstract: A compound of the formulae (I) or (II): 1
    Type: Application
    Filed: April 11, 2002
    Publication date: January 23, 2003
    Applicant: Wyeth
    Inventors: Amedeo Arturo Failli, Thomas Joseph Caggiano, Jay Scott Shumsky, Eugene J. Trybulski, Kevin A. Memoli, John P. Dusza
  • Publication number: 20030013873
    Abstract: Secondary amines of the formula 1
    Type: Application
    Filed: June 19, 2002
    Publication date: January 16, 2003
    Inventors: Peter Neumann, Johann-Peter Melder, Christoph Benisch, Arthur Hohn, Joachim Pfeffinger
  • Patent number: 6489354
    Abstract: 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: Grant
    Filed: March 1, 2000
    Date of Patent: December 3, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Jianming Bao, Robert K. Baker, William H. Parsons, Kathleen Rupprecht
  • Patent number: 6372764
    Abstract: 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: Grant
    Filed: March 1, 2000
    Date of Patent: April 16, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Jianming Bao, Robert K. Baker, William H. Parsons, Kathleen Rupprecht
  • Patent number: 6362201
    Abstract: 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: Grant
    Filed: March 1, 2000
    Date of Patent: March 26, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Robert K. Baker, William H. Parsons, Kathleen Rupprecht
  • Patent number: 6346527
    Abstract: 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: Grant
    Filed: October 24, 2000
    Date of Patent: February 12, 2002
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Kohei Takenaka, Yoshikazu Inoue, Masatoshi Minagawa, Atsushi Akahane
  • Patent number: 6281227
    Abstract: 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: Grant
    Filed: December 2, 1999
    Date of Patent: August 28, 2001
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Yong Mi Choi-Sledeski, Heinz W. Pauls, Jeffrey N. Barton, William R. Ewing, Daniel M. Green, Michael R. Becker, Yong Gong, Julian Levell
  • Patent number: 6166037
    Abstract: 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: Grant
    Filed: August 27, 1998
    Date of Patent: December 26, 2000
    Assignee: 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
  • Patent number: 5914319
    Abstract: 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: Grant
    Filed: September 1, 1995
    Date of Patent: June 22, 1999
    Assignee: Eli Lilly and Company
    Inventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
  • Patent number: 5910494
    Abstract: 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: Grant
    Filed: February 7, 1997
    Date of Patent: June 8, 1999
    Assignee: Glaxo Wellcome Inc.
    Inventor: Lawrence Edward Brieaddy
  • Patent number: 5726159
    Abstract: 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: Grant
    Filed: September 1, 1995
    Date of Patent: March 10, 1998
    Assignee: Eli Lilly and Company
    Inventors: Aaron L. Schacht, Robert T. Shuman, Gerald F. Smith, Michael R. Wiley
  • Patent number: 5710130
    Abstract: 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: Grant
    Filed: September 1, 1995
    Date of Patent: January 20, 1998
    Assignee: Eli Lilly and Company
    Inventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
  • Patent number: 5707966
    Abstract: 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: Grant
    Filed: September 1, 1995
    Date of Patent: January 13, 1998
    Assignee: Eli Lilly and Company
    Inventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
  • Patent number: 5705487
    Abstract: 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: Grant
    Filed: September 1, 1995
    Date of Patent: January 6, 1998
    Assignee: Eli Lilly and Company
    Inventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
  • Patent number: 5658899
    Abstract: 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: Grant
    Filed: March 14, 1995
    Date of Patent: August 19, 1997
    Assignee: Novo Nordisk A/S
    Inventors: Louis Brammer Hansen, Rolf Emil Amsler, Scott Eugene McGraw
  • Patent number: 5599793
    Abstract: 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: Grant
    Filed: March 2, 1995
    Date of Patent: February 4, 1997
    Assignee: Eli Lilly and Company
    Inventors: Nickolay Y. Chirgadze, Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
  • Patent number: 5530125
    Abstract: 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: Grant
    Filed: August 19, 1994
    Date of Patent: June 25, 1996
    Assignee: Schering Corportion
    Inventors: Joel G. Berger, Wei K. Chang, Joseph A. Kozlowski, Guowei Zhou
  • Patent number: 5470850
    Abstract: 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: Grant
    Filed: May 6, 1994
    Date of Patent: November 28, 1995
    Assignee: Novo Nordisk A/S
    Inventors: Christian Foged, Rolf Holweg, Erik Nielsen
  • Patent number: 5461148
    Abstract: 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: Grant
    Filed: September 27, 1993
    Date of Patent: October 24, 1995
    Assignee: Schering Corporation
    Inventors: Guang-Zhong Wu, Martin Steinman, Yee-Shing Wong
  • Patent number: 5446147
    Abstract: 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: Grant
    Filed: April 3, 1992
    Date of Patent: August 29, 1995
    Assignee: Trustees of the University of Pennsylvania
    Inventors: Hank F. Kung, Sumalee Chumpradit, Mei Ping Kung
  • Patent number: 5273974
    Abstract: 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: Grant
    Filed: November 22, 1991
    Date of Patent: December 28, 1993
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Giichi Goto, Yuji Ishihara, Masaomi Miyamoto
  • Patent number: 5244881
    Abstract: 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: Grant
    Filed: November 22, 1991
    Date of Patent: September 14, 1993
    Assignee: Rhone-Poulenc Sante
    Inventor: Anne Coutel-Egros
  • Patent number: 5216150
    Abstract: 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: Grant
    Filed: September 12, 1991
    Date of Patent: June 1, 1993
    Assignees: Hiroyoshi Hidaka, Tobishi Yakuhin Kogyo Kabushiki Kaisha
    Inventors: Hiroyoshi Hidaka, Tomohiko Ishikawa, Masatoshi Hagiwara, Tsutomu Inoue, Kenji Naitoh, Osamu Sakuma, Masayuki Yuasa, Tadashi Morita, Tadashi Toshioka, Isao Umezawa, Takashi Inaba
  • Patent number: 5079243
    Abstract: 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: Grant
    Filed: February 8, 1990
    Date of Patent: January 7, 1992
    Assignee: Novo Nordisk A/S
    Inventors: Louis B. Hansen, Kristian T. Hansen
  • Patent number: 5017571
    Abstract: 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: Grant
    Filed: February 28, 1989
    Date of Patent: May 21, 1991
    Assignee: Novo Nordisk A/S
    Inventors: Kristian T. Hansen, Hans Bundgaard, Peter Faarup
  • Patent number: 5015639
    Abstract: 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: Grant
    Filed: March 13, 1989
    Date of Patent: May 14, 1991
    Assignee: Schering Corporation
    Inventors: Joel G. Berger, Wei K. Chang, Marjorie Peters
  • Patent number: 5010074
    Abstract: 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: Grant
    Filed: June 12, 1989
    Date of Patent: April 23, 1991
    Assignee: Novo Nordisk A/S
    Inventors: Frederik Gronwald, Peter H. Andersen, Peter Faarup, Erling Guddal, Kristian T. Hansen, Louis B. Hansen, Erik B. Nielsen
  • Patent number: 4861771
    Abstract: 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: Grant
    Filed: January 27, 1989
    Date of Patent: August 29, 1989
    Assignee: SmithKline Beckman Corporation
    Inventors: Dimitri Gaitanopoulos, Bruce Mico, Joseph Weinstock
  • Patent number: 4824839
    Abstract: 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: Grant
    Filed: March 14, 1988
    Date of Patent: April 25, 1989
    Assignee: SmithKline Beckman Corporation
    Inventors: William E. Bondinell, Herbert S. Ormsbee, III
  • Patent number: 4751222
    Abstract: 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: Grant
    Filed: April 21, 1986
    Date of Patent: June 14, 1988
    Assignee: Novo Industri A/S
    Inventors: Claus Braestrup, Peter H. Andersen, Poul Borrevang, Frederik C. Gr nvald, Louis B. Hansen, Rolf Hohlweg