Design and synthesis of bridged γ-lactams as analogues of β-lactam antibiotics
摘要:
Anti-Bredt bridged bicyclo[3.2.1] gamma-lactams were designed as inhibitors of penicillin binding proteins (PBPs). The compounds were prepared by a carbenoid insertion into a lactam N-H bond. Their weak antibacterial activity could either be explained by a poor chemical stability or by unfavorable steric interactions of the methylene bridge of the gamma-lactam with the targeted enzymes. (C) 2004 Elsevier Ltd. All rights reserved.
Design and synthesis of bridged γ-lactams as analogues of β-lactam antibiotics
摘要:
Anti-Bredt bridged bicyclo[3.2.1] gamma-lactams were designed as inhibitors of penicillin binding proteins (PBPs). The compounds were prepared by a carbenoid insertion into a lactam N-H bond. Their weak antibacterial activity could either be explained by a poor chemical stability or by unfavorable steric interactions of the methylene bridge of the gamma-lactam with the targeted enzymes. (C) 2004 Elsevier Ltd. All rights reserved.
This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of defined compounds of formula I as thrombin inhibitors.
Novel substituted 4-(1H-benzimidazol-2-yl) [1,4]diazepanes useful for the treatment of allergic diseases
申请人:——
公开号:US20010034343A1
公开(公告)日:2001-10-25
The present invention relates to novel 4-(1H-benzimidazol-2-yl)[1,4]diazepane derivatives of formula
1
and stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.
Compounds Comprising a Lactam or a Lactam Derivative Moiety, Processes for Making Them, and Their Uses
申请人:Celanire Sylvain
公开号:US20090023708A1
公开(公告)日:2009-01-22
The present invention relates to compounds of formula (I) comprising a lactam or a lactam derivative moiety, processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as pharmaceuticals.
1-Benzoyl-2-pyrrolidinonderivat, Verfahren zu seiner Herstellung und dieses enthaltende Arzneimittel
申请人:F. HOFFMANN-LA ROCHE & CO.
Aktiengesellschaft
公开号:EP0005143A1
公开(公告)日:1979-11-14
1-(p-Methoxybenzoyl)-2-pyrrolidinon, verwendbar bei der Bekämpfung bzw. Verhütung der cerebralen Insuffizienz bzw. bei der Verbesserung der intellektuellen Leistungsfähigkeit.
1-(对甲氧基苯甲酰基)-2-吡咯烷酮,可用于治疗或预防脑功能不全或提高智力。
Pyrrolidone, piperidone and azetidinone terminated and functionalizes dendritic polymers
申请人:Tomalia A. Donald
公开号:US20050171298A1
公开(公告)日:2005-08-04
Heterocycle terminated dendritic polymers. More specifically, the production of 2-pyrrolidone, 2-piperidone, 2-aza-cycloheptanone or 2-azetidinone-terminated dendritic polymers obtained by reacting precursor primary amine,(e.g., —NH
2
)-terminated dendritic polymers with certain functionalized methacrylate reagents to produce new and novel dendritic polymers terminated with ester substituted 2-pyrrolidone, 2-piperidone, 2-aza-cycloheptanone or 2-azetidinone groups.