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.
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
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
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.
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
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.
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.
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.
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
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
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