The Additional Cyclo Consists Of Two Nitrogens And Three Carbons (e.g., Imidazobenzodiazepines, Etc.) Patents (Class 540/562)
  • Patent number: 9156842
    Abstract: The invention concerns a new process for preparing 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]-propionic acid methyl ester or 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]propionic acid methyl ester benzene sulfonate (P) which comprises reacting 3-[(S)-7-bromo-2-((R and/or S)-2-hydroxy-propylamino)-5-pyridin-2-yl-3H-benzo[e][1,4]diazepin-3-yl]-propionic acid methyl ester of formula (EM) with an oxidizing agent and optionally treating the reaction product under acidic conditions, such as to produce the compound of formula (F) or the compound (P), and new compounds useful as starting material or as intermediate for performing that process.
    Type: Grant
    Filed: September 15, 2010
    Date of Patent: October 13, 2015
    Assignee: PAION UK LIMITED
    Inventors: Gary Stuart Tilbrook, Andreas Schumacher, René Emmenegger
  • Patent number: 9006233
    Abstract: Described herein are ?3 or ?2 or ?2/?3 GABAergic receptor subtype selective ligands, pharmaceutical compositions, and methods of use of such ligands and compositions in treatment of anxiety disorders, epilepsy and schizophrenia with reduced sedative and ataxic side effects. In embodiments, such as ?3 or ?2 or ?2/?3 GABAergic receptor subtype selective ligands lack ester linkages and may be thus relatively insensitive to hydrolysis by esterases.
    Type: Grant
    Filed: April 27, 2012
    Date of Patent: April 14, 2015
    Assignee: UWM Research Foundation, Inc.
    Inventors: James M. Cook, Terry S. Clayton, Hiteshkumar D. Jain, Sundari K. Rallipalli, Yun Teng Johnson, Jie Yang, Michael Ming-jin Poe, Ojas A. Namjoshi, Zhi-jian Wang
  • Patent number: 8981083
    Abstract: The invention features compositions and methods for treating or preventing a neoplasia. More specifically, the invention provides compositions and methods for disrupting the interaction of a BET family polypeptide comprising a bromodomain with chromatin (e.g., disrupting a bromodomain interaction with an acetyl-lysine modification present on a histone N-terminal tail).
    Type: Grant
    Filed: May 16, 2011
    Date of Patent: March 17, 2015
    Assignee: Dana Farber Cancer Institute, Inc.
    Inventors: James Elliott Bradner, Jun Qi
  • Patent number: 8835424
    Abstract: In preferred embodiments, the present invention provides methods of treatment and pharmaceutical compositions for the suppression, alleviation and prevention of the often chronic, severe and debilitating pain that can accompany inflammatory diseases and neuropathic insults, pain that is often unresponsive to conventional analgesic treatment. The preferred embodiments of the present invention further relate to methods of treatment and pharmaceutical compositions using benzodiazepine derivatives that provide suppression, alleviation and prevention of neuropathic pain, migraine-related pain and inflammatory pain with reduced sedative and ataxic side effects.
    Type: Grant
    Filed: May 13, 2010
    Date of Patent: September 16, 2014
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: James Cook, Shengming Huang, Rahul Edwankar, Ojas A. Namjoshi, Zhi-Jian Wang
  • Publication number: 20140228320
    Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia or so on represented by the formula (I):
    Type: Application
    Filed: April 15, 2014
    Publication date: August 14, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Takahiko TANIGUCHI, Masato YOSHIKAWA, Kasei MIURA, Tomoaki HASUI, Eiji HONDA, Keisuke IMAMURA, Makoto KAMATA, Haruhi KAMISAKI, John F. QUINN, Joseph RAKER, Fatoumata CAMARA, Yi WANG
  • Publication number: 20140081018
    Abstract: Disclosed is the synthesis of [18F]flumazenil that is useful in imaging epileptic lesions by PET (positron emission tomography). A method for preparing [18F]flumazenil by reacting a diaryliodonium salt precursor with the positron-emitting radionuclide fluorine-18. [18F]flumazenil can be prepared from the diaryliodonium salt precursor in the presence of kryptofix2.2.2./potassium carbonate(K2.2.2./K2CO3) and TEMPO in dimethylformamide (DMF) at a high yield.
    Type: Application
    Filed: November 22, 2013
    Publication date: March 20, 2014
    Applicant: BIO IMAGING KOREA CO., LTD.
    Inventors: Byung Chul Lee, Byung Seok Moon, Ji Sun Kim
  • Patent number: 8642588
    Abstract: The invention relates to esylate salts of the compound of formula (I): Methods of preparing the salts, and their use as medicaments, in particular for sedative or hypnotic, anxiolytic, muscle relaxant, or anticonvulsant purposes is also described.
    Type: Grant
    Filed: July 10, 2007
    Date of Patent: February 4, 2014
    Assignee: PAION UK Limited
    Inventors: Gary Stuart Tilbrook, Louisa Jane Cubitt
  • Patent number: 8557981
    Abstract: The present invention refers to a process for the preparation of 4H-imidazo[1,5-a][1,4]benzodiazepines, in particular Midazolam, through an efficient and selective decarboxylation reaction of the derivative compound of the 5-aminomethyl-1-phenyl-1H-imidazole-4-carboxylic acid of formula (II) avoiding the formation of the 6H-imidazo[1,5-a][1,4]benzodiazepines by-products and the ensuing process for the isomerization of a 4H-imidazo[1,5-a][1,4]benzodiazepine product.
    Type: Grant
    Filed: May 3, 2011
    Date of Patent: October 15, 2013
    Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.
    Inventors: Andrea Castellin, Michele Maggini, Paola Donnola
  • Publication number: 20130172328
    Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia or so on represented by the formula (I):
    Type: Application
    Filed: June 22, 2011
    Publication date: July 4, 2013
    Applicant: CROSSWING INC.
    Inventors: Takahiko Taniguchi, Masato Yoshikawa, Kasei Miura, Tomoaki Hasui, Eiji Honda, Keisuke Imamura, Makoto Kamata, Haruhi Kamisaki, John F. Quinn, Joseph Raker, Fatoumata Camara, Yi Wang
  • Patent number: 8455479
    Abstract: The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising compounds of Formula I and methods of treating or preventing one or more conditions that may be regulated or normalized via inhibition of dipeptidyl peptidase IV (DPP-IV).
    Type: Grant
    Filed: January 23, 2009
    Date of Patent: June 4, 2013
    Assignee: Panacea Biotec Limited
    Inventors: Rajesh Jain, Sanjay Trehan, Jagattaran Das, Nishan Singh, Gurmeet Kaur Nanda, Sitaram Kumar Magadi, Sudhir Kumar Sharma
  • Publication number: 20130023524
    Abstract: Tricyclic indazole compound and its pharmaceutically acceptable salts of acid addition, use thereof, method and intermediates for preparing them, and a pharmaceutical composition containing them. The tricyclic indazole compound has the following general Formula (I): in which R1, R2, L1, L2, X1, X2, X3, X4, X5, Y, W, m, and n have the meanings stated in the description.
    Type: Application
    Filed: March 4, 2011
    Publication date: January 24, 2013
    Applicant: AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.
    Inventors: Maria Alessandra Alisi, Nicola Cazzolla, Guido Furlotti, Beatrice Garrone, Gabriele Magaro', Giorgina Mangano
  • Publication number: 20120330007
    Abstract: The invention concerns a new process for preparing 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]-propionic acid methyl ester or 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]propionic acid methyl ester benzene sulfonate (P) which comprises reacting 3-[(S)-7-bromo-2-((R and/or S)-2-hydroxy-propylamino)-5-pyridin-2-yl-3H-benzo[e][1,4]diazepin-3-yl]-propionic acid methyl ester of formula (EM) with an oxidizing agent and optionally treating the reaction product under acidic conditions, such as to produce the compound of formula (F) or the compound (P), and new compounds useful as starting material or as intermediate for performing that process.
    Type: Application
    Filed: September 15, 2010
    Publication date: December 27, 2012
    Applicant: PAION UK Limited
    Inventors: Gary Stuart Tilbrook, Andreas Schumacher, René Emmengger
  • Publication number: 20120295892
    Abstract: Described herein are ?3 or ?2 or ?2/?3 GABAergic receptor subtype selective ligands, pharmaceutical compositions, and methods of use of such ligands and compositions in treatment of anxiety disorders, epilepsy and schizophrenia with reduced sedative and ataxic side effects. In embodiments, such as ?3 or ?2 or ?2/?3 GABAergic receptor subtype selective ligands lack ester linkages and may be thus relatively insensitive to hydrolysis by esterases.
    Type: Application
    Filed: April 27, 2012
    Publication date: November 22, 2012
    Applicant: UWM RESEARCH FOUNDATION, INC.
    Inventors: James M. Cook, Terry S. Clayton, Hiteshkumar D. Jain, Sundari K. Rallipalli, Yun Teng Johnson, Jie Yang, Michael Ming-Jin Poe, Ojas A. Namjoshi, Zhi-jian Wang
  • Patent number: 8278297
    Abstract: In one aspect, the invention provides compounds of Formula I or pharmaceutically acceptable salts thereof. In another aspect, the invention provides methods for treatment of diseases or disorders mediated by a protein kinase, comprising administering a therapeutically effective amount of a compound of this invention.
    Type: Grant
    Filed: December 23, 2010
    Date of Patent: October 2, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steven Durrant
  • Patent number: 8252787
    Abstract: In one aspect, the invention provides compounds of Formula I or pharmaceutically acceptable salts thereof. In another aspect, the invention provides methods for treatment of diseases or disorders mediated by a protein kinase, comprising administering a therapeutically effective amount of a compound of this invention.
    Type: Grant
    Filed: December 23, 2010
    Date of Patent: August 28, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steven Durrant
  • Publication number: 20120184536
    Abstract: The present invention encompasses compositions comprising UGT inhibitors. Additionally, the invention encompasses methods of reducing the glucuronidation of a compound using a UGT inhibitor.
    Type: Application
    Filed: February 27, 2012
    Publication date: July 19, 2012
    Applicant: The Board of Trustees of the University of Arkansas
    Inventor: Anna Radominska-Pandya
  • Patent number: 8202858
    Abstract: The present invention concerns compounds inter alia according to general formula 1a. Compounds according to the invention are vasopressin V1a receptor antagonists. Pharmaceutical compositions of the compounds are useful as treatment of dysmenorrhoea.
    Type: Grant
    Filed: August 24, 2005
    Date of Patent: June 19, 2012
    Assignee: Vantia Limited
    Inventors: Andrzej Roman Batt, Martin Lee Stockley, Michael Bryan Roe, Celine Marguerite Simone Heeney, Andrew John Baxter, Peter Hudson, Rachel Handy
  • Patent number: 8119629
    Abstract: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.
    Type: Grant
    Filed: September 29, 2008
    Date of Patent: February 21, 2012
    Assignee: Bristol-Meyers Squibb Company
    Inventor: Ronald J. Mattson
  • Publication number: 20110319394
    Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia. The compound is represented by the formula (I): wherein the symbols are defined in the specification.
    Type: Application
    Filed: June 22, 2011
    Publication date: December 29, 2011
    Inventors: Takahiko TANIGUCHI, Masato YOSHIKAWA, Kasei MIURA, Tomoaki HASUI, Eiji HONDA, Keisuke IMAMURA, Makoto KAMATA, Haruhi KAMISAKI, John F. QUINN, Joseph RAKER, Fatoumata CAMARA, Yi WANG
  • Patent number: 8063032
    Abstract: Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Grant
    Filed: February 11, 2010
    Date of Patent: November 22, 2011
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Milan Chytil, Qun Kevin Fang, Kerry L. Spear
  • Publication number: 20110224195
    Abstract: The present invention is directed to substituted six-membered heterocyclic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as obesity and diabetes, particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Application
    Filed: August 18, 2008
    Publication date: September 15, 2011
    Inventors: Tesfaye Biftu, Danqing Feng, Ann E. Weber, Jason M. Cox, Xiaoxia Qian, Jinyou Xu
  • Patent number: 7947678
    Abstract: Compounds of formula I: (where variables R2, R7, D, W, X, Y and Z are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Grant
    Filed: July 25, 2006
    Date of Patent: May 24, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Theresa M. Williams
  • Publication number: 20100311732
    Abstract: The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising compounds of Formula I and methods of treating or preventing one or more conditions that may be regulated or normalized via inhibition of dipeptidyl peptidase IV (DPP-IV).
    Type: Application
    Filed: January 23, 2009
    Publication date: December 9, 2010
    Inventors: Rajesh Jain, Sanjay Trehan, Jagattaran Das, Nishan Singh, Gurmeet Kaur Nanda, Sitaram Kumar Magadi, Sudhir Kumar Sharma
  • Publication number: 20100298287
    Abstract: There is provided a compound of the formula (I?): wherein X is a nitrogen or CRx, Rx is a hydrogen, etc., R1 is an optionally substituted hydrocarbon group, etc., R2 is an optionally substituted hydrocarbon group, etc., ring A is 5- to -8-membered heterocyclic ring, etc., and each of Y1, Y2 and Y3 is an optionally substituted carbon or a nitrogen, etc.; or ‘a salt thereof or a prodrug thereof, which have CRF receptor antagonistic activity and use thereof.
    Type: Application
    Filed: January 21, 2009
    Publication date: November 25, 2010
    Inventors: Kazuyoshi Aso, Katsumi Kobayashi, Takafumi Takai, Takuto Kojima, Kazuyuki Tokumaru, Michiyo Mochizuki, Yasutaka Hoashi
  • Publication number: 20100234417
    Abstract: A hetero-dimeric or hetero-oligomeric receptor, comprising at least one thyrotropin releasing hormone receptor subunit associated with at least one orexin receptor subunit.
    Type: Application
    Filed: November 9, 2007
    Publication date: September 16, 2010
    Applicant: DIMERIX BIOSCIENCE PTY LTD.
    Inventors: Kevin Donald George Pfleger, Ruth Marie Seeber, Heng See Boon, Karin Ann Eidne
  • Patent number: 7776852
    Abstract: Provided is a process for producing highly pure midazolam and salts thereof, and a pharmaceutical composition containing the highly pure midazolam and/or a salt thereof.
    Type: Grant
    Filed: September 11, 2007
    Date of Patent: August 17, 2010
    Assignee: CHEMAGIS Ltd.
    Inventors: Sonia Krivonos, Yana Sery
  • Publication number: 20100204214
    Abstract: Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Application
    Filed: February 11, 2010
    Publication date: August 12, 2010
    Inventors: Milan Chytil, Sharon R. Engel, Qun Kevin Fang, Kerry L. Spear
  • Patent number: 7700588
    Abstract: Compositions of midazolam, a benzodiazapine, in concentrations of 35-100 mg/ml are disclosed for the treatment of anxiety, epilepsy and epileptic seizures, invasive surgical procedures and diagnostic procedures and sedation. These compositions are particularly characterized by a solubilizer such an propylene glycol. Preferably, the compositions are aqueous solutions for intranasal administration.
    Type: Grant
    Filed: January 13, 2005
    Date of Patent: April 20, 2010
    Inventor: Franciscus Wilhelmus Henricus Maria Merkus
  • Publication number: 20100081647
    Abstract: The invention relates to besylate salts of the compound of formula (I): Methods of preparing the salts, and their use as medicaments, in particular for sedative or hypnotic, anxiolytic, muscle relaxant, or anticonvulsant purposes is also described.
    Type: Application
    Filed: July 10, 2007
    Publication date: April 1, 2010
    Applicant: PAION UK Limited
    Inventors: Gary Stuart Tilbrook, Louisa Jane Cubitt
  • Publication number: 20100075955
    Abstract: The invention relates to esylate salts of the compound of formula (I): Methods of preparing the salts, and their use as medicaments, in particular for sedative or hypnotic, anxiolytic, muscle relaxant, or anticonvulsant purposes is also described.
    Type: Application
    Filed: July 10, 2007
    Publication date: March 25, 2010
    Inventors: Gary Stuart Tilbrook, Louisa Jane Cubitt
  • Patent number: 7625888
    Abstract: The present invention is directed to novel fused triazole derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: August 19, 2005
    Date of Patent: December 1, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Ann E. Weber, Wallace T. Ashton
  • Patent number: 7618958
    Abstract: The present invention provides compositions and methods of using stereospecific benzodiazepine derivatives, their salts and prodrugs for the treatment of anxiolytic or convulsant disorders having the side effects of reduced alcohol craving in human alcoholics and a concomitant reduced sedative, hypnotic, muscle relaxant and ataxic side-effects. The invention further provides pharmaceutical compositions for treatment of anxiolytic and convulsant disorders in subjects in need thereof, comprising a compound, prodrug or a salt having a chemical structure represented by any one of Formula I-XXI and a pharmaceutically-acceptable carrier.
    Type: Grant
    Filed: June 30, 2005
    Date of Patent: November 17, 2009
    Assignee: WISYS Technology Foundation, Inc.
    Inventors: James M. Cook, Hao Zhou, Shengming Huang, P.V.V. Srirama Sarma, Chunchun Zhang
  • Publication number: 20090093466
    Abstract: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.
    Type: Application
    Filed: September 29, 2008
    Publication date: April 9, 2009
    Inventor: Ronald J. Mattson
  • Publication number: 20090069306
    Abstract: Provided is a process for producing highly pure midazolam and salts thereof, and a pharmaceutical composition containing the highly pure midazolam and/or a salt thereof.
    Type: Application
    Filed: September 11, 2007
    Publication date: March 12, 2009
    Applicant: CHEMAGIS LTD.
    Inventors: Sonia KRIVONOS, Yana SERY
  • Patent number: 7485635
    Abstract: The present invention provides a compound of formula (I): wherein all variables are as defined herein, pharmaceutical formulations containing the same, processes for preparing the same and their use therapy.
    Type: Grant
    Filed: December 5, 2006
    Date of Patent: February 3, 2009
    Assignee: CeNes Limited
    Inventors: Paul L. Feldman, David Kendall Jung, Istvan Kaldor, Gregory J. Pacofsky, Jeffrey A. Stafford, Jeffrey H. Tidwell
  • Patent number: 7459414
    Abstract: Compounds of formula wherein the substituents have the meanings given in claim 1, and agronomically tolerable salts, isomers and enantiomers of those compounds, are suitable for use as herbicides.
    Type: Grant
    Filed: March 18, 2005
    Date of Patent: December 2, 2008
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Thomas Maetzke, André Stoller, Sebastian Wendeborn, Henry Szczepanski
  • Patent number: 7435730
    Abstract: The present invention provides a compound of formula (I): wherein all variables are as defined herein, pharmaceutical formulations containing the same, processes for preparing the same and their use therapy.
    Type: Grant
    Filed: January 5, 2007
    Date of Patent: October 14, 2008
    Assignee: CeNeS Limited
    Inventors: Paul L. Feldman, David Kendall Jung, Istvan Kaldor, Gregory J. Pacofsky, Jeffrey A. Stafford, Jeffrey H. Tidwell
  • Patent number: 7407949
    Abstract: Novel compounds according to general formula 1, wherein G1 is NR5R6 or a fused polycyclic group that are specific OT receptor agonists and/or V1a receptor antagonists. Pharmaceutical compositions comprising such compounds are useful in the treatment of, inter alia, primary dysmenorrhoea.
    Type: Grant
    Filed: February 12, 2004
    Date of Patent: August 5, 2008
    Assignee: Ferring B.V.
    Inventors: Peter Hudson, Andrzej Roman Batt, Celine Marguerite Simone Heeney, Andrew John Baxter, Michael Bryan Roe, Peter Andrew Robson
  • Patent number: 7238685
    Abstract: The invention relates to novel benzo-fused heterocycles and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as endothelin receptor antagonists.
    Type: Grant
    Filed: July 31, 2002
    Date of Patent: July 3, 2007
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Martin Bolli, Christoph Boss, Martine Clozel, Walter Fischli, Thomas Weller, Judith Marfurt
  • Patent number: 7119196
    Abstract: Orally active benzodiazepine derivatives and their salts are disclosed. These compounds and their salts have anxiolytic and anticonvulsant activity with reduced sedative/hypnotic/muscle relaxant/ataxic effects.
    Type: Grant
    Filed: March 28, 2003
    Date of Patent: October 10, 2006
    Assignee: Wisys Technology Foundation, Inc.
    Inventors: James M. Cook, Qi Huang, Xiaohui He, Xioayan Li, Jianming Yu, Dongmei Han, Snjezana Lelas, John F. McElroy
  • Patent number: 7105509
    Abstract: A novel class of 1,4- and 1,5-benzodiazepines of formula (I) is disclosed.
    Type: Grant
    Filed: May 21, 2001
    Date of Patent: September 12, 2006
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Jose Luis Castro Pineiro, Ian Churcher, Alexander Richard Guiblin, Timothy Harrison, Sonia Kerrard, Andrew Madin, Alan John Nadin, Andrew Pate Owens, Timothy Jason Sparey, Martin Richard Teall, Susannah Williams
  • Patent number: 6894005
    Abstract: Compounds of formula wherein the substituents have the meanings given in claim 1, and agronomically tolerable salts, isomers and enantiomer of those compounds, are suitable for use as herbicides.
    Type: Grant
    Filed: September 5, 2000
    Date of Patent: May 17, 2005
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Thomas Maetzke, André Stoller, Sebastian Wendeborn, Henry Szczepanski
  • Patent number: 6784292
    Abstract: The invention relates to a method for the preparation of compound of formula (1). The invention further relates to the previously unknown compounds of formulas (5 and 6) as intermediates in the production of benzodiazepines of formula (1).
    Type: Grant
    Filed: August 21, 2003
    Date of Patent: August 31, 2004
    Assignee: Schering AG
    Inventors: Eric Winter, Matthias Schneider, Ulf Tilstam
  • Patent number: 6512114
    Abstract: The present invention provides a process for the synthesis of Midazolam I from a compound of formula II, using thermodynamic, basic workup conditions. Additional steps to isolate the pure bulk product follow.
    Type: Grant
    Filed: June 30, 1999
    Date of Patent: January 28, 2003
    Assignee: Abbott Laboratories
    Inventors: Madhup K. Dhaon, Grant L. Esser, Deborah A. Davis, Ashok V. Bhatia
  • Patent number: 6511974
    Abstract: This invention relates to new compounds selected from those of the general formula (I), or a pharmaceutically acceptable salt, ester or prodrug form thereof: wherein D, E and G are N or CH, which serve as vasopressin agonists and are useful in treating disorders such as diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders, and the inability to temporarily delay urination and pharmaceutical compositions and methods for same.
    Type: Grant
    Filed: July 24, 1998
    Date of Patent: January 28, 2003
    Assignee: Wyeth
    Inventors: John P. Dusza, Peter S. Chan, Jay D. Albright, Jehan F. Bagli, Amedeo A. Failli, Mark A. Ashwell, Albert J. Molinari, Thomas J. Caggiano, Eugene J. Trybulski
  • Patent number: 6482819
    Abstract: 2,3-Benzodiazepines of formula (I), their stereoisomers and acid addition salts, wherein the variables have the meaning given in the specification, and pharmaceutical compositions containing them which are suitable for treating conditions associated with muscle spasms, epilepsy as well as acute and chronic forms of neurodegenerative diseases are disclosed.
    Type: Grant
    Filed: April 10, 2000
    Date of Patent: November 19, 2002
    Assignee: Gyogyszerkutato Intezet Kft.
    Inventors: Gizella Ábrahám, Emese Csuzdi, Sándor Sólyom, Pál Berzsenyi, István Tarnawa, Ferenc Andrási, István Ling, Tamás Hámori, Katalin Horváth, Imre Moravcsik, István Pallagi, Antal Simay
  • Patent number: 6413956
    Abstract: Disclosed are compounds of Formula I: or the pharmaceutically acceptable salts thereof where, R1, R2, and W are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.
    Type: Grant
    Filed: May 5, 2000
    Date of Patent: July 2, 2002
    Assignee: Neurogen Corporation
    Inventors: Pamela A. Albaugh, Kevin S. Currie, Dan Rosewater, Guolin Cai
  • Patent number: 6323197
    Abstract: The invention concerns compounds of formula (I), in which R1, R2, R3 and R4 mean hydrogen or different substituents; X means hydrogen or halogen; Y means C1-6 alkoxy or X and Y together mean —O—(CH2)n—O—; n means 1, 2 or 3; and A together with nitrogen forms a saturated or unsaturated five-member heterocycle which can contain between 1 and 3 nitrogen atoms and/or an oxygen atom and/or one or two carbonyl groups. Owing to their non-competitive inhibiting of the AMPA receptors, these compounds can be used as medicaments for treating diseases of the central nervous system.
    Type: Grant
    Filed: November 5, 1998
    Date of Patent: November 27, 2001
    Assignee: Schering Aktiengesellschaft
    Inventors: Ernese Csuzdi, Tamas Hámori, Gizella Ábrahám, Sändor Sólyom, István Tarnawa, Pál Berzsenyi, Ferenc Andrási, István Ling, Antal Simay, Melinda Gál, Katalin Horváth, Eszter Szentkuti, Márta Szöllosy, István Pallagi
  • Publication number: 20010014738
    Abstract: The present invention relates to a process for the synthesis of a compound having the formula I, 1
    Type: Application
    Filed: June 30, 1999
    Publication date: August 16, 2001
    Inventors: MADHUP K. DHAON, PARVIZ LABIB, DEBORAH A. DAVIS, GRANT L. ESSER
  • Patent number: RE47475
    Abstract: In preferred embodiments, the present invention provides methods of treatment and pharmaceutical compositions for the suppression, alleviation and prevention of the often chronic, severe and debilitating pain that can accompany inflammatory diseases and neuropathic insults, pain that is often unresponsive to conventional analgesic treatment. The preferred embodiments of the present invention further relate to methods of treatment and pharmaceutical compositions using benzodiazepine derivatives that provide suppression, alleviation and prevention of neuropathic pain, migraine-related pain and inflammatory pain with reduced sedative and ataxic side effects.
    Type: Grant
    Filed: September 16, 2016
    Date of Patent: July 2, 2019
    Assignee: WISYS TECHNOLOGY FOUNDATION, INC.
    Inventors: James M. Cook, Shengming Huang, Rahul Edwankar, Ojas A. Namjoshi, Zhi-Jian Wang, Qi Huang, Xiaohui He, Xiaoyan Li, Jianming Yu, Dongmei Han