Second generation 2-aminoimidazole based advanced glycation end product inhibitors and breakers
摘要:
The formation of advanced glycation end-products (AGE) as a result of the action of reducing sugars on host macromolecules plays a role in increased morbidity of diabetic patients. There are currently no clinically available therapeutics for the prevention or eradication of AGEs. Following our previous identification of 2-aminoimidazole (2-AI) based AGE inhibitors and breakers, we now report the use of a rapid, scalable, two-step procedure to access a second generation of 2-AI based anti-AGE compounds from commercially available amino acids. Several second generation compounds exhibit increased AGE inhibition and breaking activty compared to the first generation compounds and to the known AGE inhibitor aminoguanidine. (C) 2015 Elsevier Ltd. All rights reserved.
Mandelic acid derivatives and their use as throbin inhibitors
申请人:——
公开号:US20040019033A1
公开(公告)日:2004-01-29
There is provided a compound of formula I
1
wherein R
a
, R
1
, R
2
, Y and R
3
have meanings given in the description and pharmaceutically acceptable derivatives (including prodrugs) thereof, which compounds and derivatives are useful as, or are useful as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.
提供了一种公式I的化合物
1
其中R
a
, R
1
, R
2
, Y和R
3
具有说明书中给出的含义以及药学上可接受的衍生物(包括前药),这些化合物和衍生物可用作竞争性胰蛋白酶样蛋白酶抑制剂,如凝血酶,因此,特别是用于需要抑制凝血酶的情况(例如血栓形成)或作为抗凝剂。
Composition for the treatment of damaged tissue
申请人:Pfizer Inc.
公开号:US20030199440A1
公开(公告)日:2003-10-23
A pharmaceutical for use in damaged tissue, such as wound, treatment (e.g. healing) is described. The pharmaceutical comprising a composition which comprises: (a) a growth factor; and (b) an inhibitor agent; and optionally (c) a pharmaceutically acceptable carrier, diluent or excipient; wherein the inhibitor agent can inhibit the action of at least one specific adverse protein (e.g. a specific protease) that is upregulated in a damaged tissue, such as a wound, environment.
Base-substituted benzylamine analogs for use as coagulation factor xa inhibitors, the production and use thereof
申请人:Stürzebecher Jörg
公开号:US20070066539A1
公开(公告)日:2007-03-22
The invention relates to the novel base-substituted benzylamine analogs of general formula (I), wherein A represents P
2
-P
1
with P
1
=(A) and P
2
=(B), for use as coagulation factor Xa inhibitors. The invention also relates to the production and use of said analogs in the therapy and prophylaxis of cardiovascular diseases and thromboembolic events.
Thiochromane derivatives and their use as thrombin inhibitors
申请人:——
公开号:US20030220317A1
公开(公告)日:2003-11-27
There is provided compounds of formulae I and IA
1
wherein Y, R
1
, R
2
, R
3
, D
1
and D
2
have meanings given in the description which are useful as, or as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.
New amidino derivatives and their use as thormbin inhibitors
申请人:——
公开号:US20020068730A1
公开(公告)日:2002-06-06
There is provided compounds of formula I,
1
wherein Y and R
1
have meanings given in the description, and pharmaceutically acceptable derivatives (including prodrugs) thereof, which compounds and derivatives are useful as, or are useful as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.