Constrained amino acids. The synthesis of glutamine mimetics
摘要:
The preparation and utility of conformationally constrained homoserines trans- 8a and cis-8b as intermediates for the synthesis of constrained glutamine mimetics Irans-la and cis-lb is presented. (C) 1997 Elsevier Science Ltd.
Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds
申请人:——
公开号:US20020045747A1
公开(公告)日:2002-04-18
Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
The present invention relates to compounds of the formula
which are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as, cancer, cognative and CNS disorders and inflammatory/autoimmune diseases.
Cobalt (II) complexes of porphyrins are effective catalysts for intramolecular nitrene insertion of C—H bonds with arylsulfonyl azides. The cobalt-catalyzed process can proceed efficiently under mild and neutral conditions in low catalyst loading without the need of other reagents or additives, generating nitrogen gas as the only byproduct. Using the simple tetraphenylporphyrin (TPP) as the ligand, the cobalt-catalyzed intramolecular amidation can be applied to primary, secondary, and tertiary C—H bonds and suitable for a broad range of arylsulfonyl azides, leading to the syntheses of various benzosultam derivatives in excellent yields
This invention is concerned with novel compounds represented by structural formula I ##STR1## which are useful in the treatment of arrhythmia.
这项发明涉及由结构式I代表的新化合物,这些化合物在治疗心律失常方面很有用。
[EN] 4- BROMO - 5 - (2- CHLORO - BENZOYLAMINO) - 1H - PYRAZOLE - 3 - CARBOXYLIC ACID AMIDE DERIVATIVES AND RELATED COMPOUNDS AS BRADYKININ B1 RECEPTOR ANTAGONISTS FOR THE TREATMENT OF INFLAMMATORY DISEASES<br/>[FR] DERIVES AMIDES DE L'ACIDE CARBOXYLIQUE DE 4- BROMO - 5 - (2- CHLORO - BENZOYLAMINO) - 1H - PYRAZOLE 3 ET COMPOSES ASSOCIES EN TANT QU'ANTAGONISTES DE RECEPTEUR DE B1 DE LA BRADYKININE POUR LE TRAITEMENT DE MALADIES INFLAMMATOIRES
申请人:ELAN PHARM INC
公开号:WO2004098589A1
公开(公告)日:2004-11-18
Disclosed are compounds of formula I and II that are bradykinin B1 receptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin B1 receptor. Certain of the compounds exhibit increased potency and are also expected to exhibit increased duration of action.