Biaryl diacid inhibitors of human s-PLA 2 with anti-inflammatory activity
摘要:
Twenty-four hydrophobic dicarboxylic acids are described which were evaluated as inhibitors of 14 kDa human platelet phospholipase A(2) (HP-PLA(2)). In general, biarylacetic acid derivatives were found to be more active than biaryl acids or biaryl-propanoic acids. More potent inhibitors were obtained when hydrophobic groups were attached to the biaryl acid nucleus using an olefin linkage as compared to an ether linkage. Compounds with larger hydrophobic groups were usually more potent inhibitors of HP-PLA(2). Five of the compounds disclosed in this report (2, 4, 28, 36b and 36i) were found to possess significant anti-inflammatory activity in a phorbol ester induced mouse ear edema model of chronic inflammation. (C) 2000 Elsevier Science Ltd. All rights reserved.
Certain novel biaryl compounds are effective phospholipase A.sub.2 (PLA.sub.2) inhibitors.
某些新型联苯化合物是有效的磷脂酶A.sub.2(PLA.sub.2)抑制剂。
Pyridine compounds which are useful as angiotensin II receptor
申请人:Imperial Chemical Industries PLC
公开号:US05236936A1
公开(公告)日:1993-08-17
The invention concerns pharmaceutically useful compounds of the formula I, in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X and Z have the various meanings defined herein, and their non-toxic salts, and pharmaceutical compositions containing them. The novel compounds are of value in treating conditions such as hypertension and congestive heart failure. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.
Novel indane and indene derivatives are described which are endothelin receptor antagonists.
本文描述了一种新型的吲哚烷和吲哚烯衍生物,它们是内皮素受体拮抗剂。
Endothelin receptor anatagonists
申请人:SmithKline Beecham Corporation
公开号:US05719182A1
公开(公告)日:1998-02-17
Novel indane and indene derivatives are described which are endothelin receptor antagonists.
本文描述了一种新的吲哚烷和吲哚烯衍生物,它们是内皮素受体拮抗剂。
Tosylates in palladium-catalysed coupling reactions. Application to the synthesis of arylcoumarin inhibitors of gyrase B
作者:Laurent Schio、Fabienne Chatreaux、Michel Klich
DOI:10.1016/s0040-4039(99)02351-5
日期:2000.3
The palladium-catalysed coupling reaction between tosylate derivatives and organostannanes has been investigated as a methodology for carbon-carbon bond formation. Aryl substituents have been successfully incorporated even in highly functionalised coumarin structures to afford new analogues of the antibiotic novobiocin. (C) 2000 Elsevier Science Ltd. All rights reserved.