Formation Of The 1,4-benzodiazepine Ring System Patents (Class 540/574)
  • Patent number: 8242264
    Abstract: The present invention relates to a process for preparing 4-acetyl-2,3,4,5-tetrahydro-benzo[1,4]diazepine and the intermediates thereof. The present invention provides a compound represented by formula I and a compound represented by formula II, and processes for preparing 4-acetyl-2,3,4,5-tetrahydro-benzo[1,4]diazepine by using the compound represented by formula I, the compound represented by formula II and o-nitrobenzaldehyde. The invention has the advantages of the shorter synthesis steps, easily available raw materials and simple operation. Moreover, the process is economic and safe by avoiding the use of expensive and dangerous lithium aluminum hydride.
    Type: Grant
    Filed: May 22, 2008
    Date of Patent: August 14, 2012
    Assignees: Topharman Shanghai Co., Ltd., Weifang Tehua Chemical Co., Ltd.
    Inventors: Fuqiang Zhu, Haihong Li, Wenzhong Wang, Hui Zhang, Jingshan Shen
  • Patent number: 7074921
    Abstract: Methods for the synthesis of benzodiazepine compounds having farnesyl protein transferase inhibitory activity.
    Type: Grant
    Filed: November 12, 2002
    Date of Patent: July 11, 2006
    Assignee: Bristol Myers Squibb Company
    Inventors: David R. Kronenthal, Rao S. Bhandaru, Zhongping Shi, Boguslaw M. Mudryk
  • Patent number: 6737421
    Abstract: Compounds of the formula I or II and their tautomeric forms, possible enantiomeric and diastereomeric forms, possible cistrans isomers on the rings in A and prodrugs thereof, pharmaceutical compositions containing these compounds and methods of treating neurodegenerative diseases or neuronal damage with these compounds.
    Type: Grant
    Filed: April 4, 2002
    Date of Patent: May 18, 2004
    Assignee: Abbott GmbH & Co. KG
    Inventors: Wilfried Lubish, Michael Kock, Thomas Hoeger, Roland Grandel, Sabine Schult, Reinhold Mueller
  • Patent number: 6703387
    Abstract: The invention is concerned with novel benzodiazepine derivatives, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the compounds are inhibitors of the human papillomavirus E1 helicase enzyme which is involved in viral replication. Consequently the compounds of this invention may be advantageously used as therapeutic agents for HPV mediated diseases.
    Type: Grant
    Filed: June 26, 2001
    Date of Patent: March 9, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: David N. Hurst, Philip Stephen Jones, Kevin Edward Burdon Parkes, Martin John Parratt, Francis Xavier Wilson
  • Patent number: 6545000
    Abstract: The present invention relates to [1,2,4]triazolo[1,5-c]pyrimidine compounds represented by formula (I): wherein na and nb independently represent an integer of 0 to 4 and Q represents a hydrogen atom or 3,4-dimethoxybenzyl, or salts thereof exhibit activity as adenosine A2A receptor antagonists.
    Type: Grant
    Filed: March 22, 2001
    Date of Patent: April 8, 2003
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Junichi Shimada, Hironori Imma, Naoto Osakada, Shizuo Shiozaki, Tomoyuki Kanda, Yoshihisa Kuwana
  • Publication number: 20020065270
    Abstract: N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed.
    Type: Application
    Filed: December 22, 2000
    Publication date: May 30, 2002
    Inventors: Kevin Joseph Moriarty, Yvonne Shimshock, Gulzar Ahmed, Junjun Wu, James Wen, Wei Li, Shawn David Erickson, Jeffrey John Letourneau, Edward McDonald, Katerina Leftheris, Stephen T. Wrobleski
  • Patent number: 6362174
    Abstract: The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke, cerebral ischemia, pain, epilepsy, and head trauma.
    Type: Grant
    Filed: August 9, 2001
    Date of Patent: March 26, 2002
    Assignee: Warner-Lambert Company
    Inventors: Michael Francis Rafferty, Yuntao Song
  • Patent number: 6316440
    Abstract: The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke, cerebral ischemia, pain, epilepsy, and head trauma.
    Type: Grant
    Filed: December 27, 1999
    Date of Patent: November 13, 2001
    Assignee: Warner-Lambert Company
    Inventors: Michael Francis Rafferty, Yuntao Song
  • Patent number: 5466799
    Abstract: A general method is provided for the synthesis of substituted 2,3-dihydro-5-phenyl-1H-1,4-benzodiazepines by the reaction of bis-trifiated-2,5-dihydroxy benzophenones with 1,2-bisaminoethanes, followed by displacement of the 7-trifloxy group.
    Type: Grant
    Filed: August 8, 1994
    Date of Patent: November 14, 1995
    Assignee: Iowa State University Research Foundation, Inc.
    Inventor: George A. Kraus
  • Patent number: 5395934
    Abstract: Racemic or optically active new 3(2H)-pyridazinone derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, to the use of the said 3(2H)-pyridazinone derivatives for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases.
    Type: Grant
    Filed: December 21, 1992
    Date of Patent: March 7, 1995
    Assignee: EGIS Gyogyszergyar
    Inventors: Peter Matyus, Klara Czako, Ildiko Varga, Andrea Jednakovics, Agnes Papp, Ilona Bodi, Gyorgy Rabloczky, Andras Varro, Laszlo Jaszlits, Aniko Miklos, Luca Levay, Gvorgy Schmidt, Marton Fekete, Maria Kurthy, Katalin Szemeredi, Erzsebet Zara
  • Patent number: 4751298
    Abstract: There is disclosed a process for the production of 1,4-bis-[3-(3,4,5-trimethoxybenzyloxy)-propyl]-diazepane which consists of first reacting 3-aminopropanol with acrylonitrile and subsequently reacting in aqueous solution with formaldehyde and hydrocyanic acid or with formaldehyde and an alkali cyanide in the presence of alkali hydrogen sulfite to form cyanomethyl-(2-cyano-ethyl)-(3-hydroxy-propyl)-amine; hydrogenating the thus obtained reaction product in the presence of a hydrogenating catalyst and ammonia to 1 (3-hydroxy-propyl)-1,4-diazepane and reacting the latter compound for example with 3-halogen propanol or with allyl alcohol and introducing two 3,4,5-trimethoxy-benzoyl groups into the thus obtained reaction product by esterification.
    Type: Grant
    Filed: January 22, 1985
    Date of Patent: June 14, 1988
    Assignee: Degussa Aktiengesellschaft
    Inventors: Axel Kleemann, Bernd Lehmann, Klaus Deller
  • Patent number: RE37781
    Abstract: This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors, to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating viral infection. A representative compound of the invention is the compound of formula: wherein R22 and R23 are allyl.
    Type: Grant
    Filed: March 10, 1999
    Date of Patent: July 2, 2002
    Assignee: DuPont Pharmaceuticals Company
    Inventors: Patrick Y. Lam, Prabhakar K. Jadhav, Charles J. Eyermann, Carl N. Hodge, George V. De Lucca, James D. Rodgers