Naphthalenylsulfonyl-hydantoins as aldose reductase inhibitors
摘要:
Accumulation of intracellular sorbitol, formed from glucose by aldose reductase, is believed to play an important role in the development of certain chronic complications of diabetes mellitus. Several 1-(naphthalenylsulfonyl)hydantoins inhibit aldose reductase isolated from bovine lens in vitro, and decrease galactitol formation in sciatic nerves of galactosemic rats in vivo. The 5-bromo analogue (entry 12, table I) was found to be the most orally active aldose reductase inhibitor of this series with an ED50 value of 8.1 mg/kg po. The 1-(naphthalenylsulfonyl)-2-thiohydantoin analogues with the exception of entry 11 (table I) which showed good in vivo activity, were either inactive or had only marginal activity.
Aminoheterocyclic derivatives as antithrombotic or anticoagulant agents
申请人:ZENECA LIMITED
公开号:US20030207882A1
公开(公告)日:2003-11-06
Compounds of formula (I), wherein G
1
is CH or N; G
2
is CH or N; R
1
is a variety of optional substituents, L
1
is (1-4C)alkylene; T
1
is CH or N; R
2
and R
3
are independently hydrogen or (1-4C)alkyl or are joined to form a ring; X
1
and X
2
represent various linking groups; Ar is phenylene or certain heteroaryl rings and Q represents a variety of aromatic or heterocyclic rings systems, and pharmaceutically acceptable salts thereof are described as useful antithrombotic and anticoagulant agents, and are selective Factor Xa inhibitors. Processes for their preparation and pharmaceutical compositions containing them are also described.
1
Carbamate derivatives, process for producing the same and use thereof
申请人:——
公开号:US20040038986A1
公开(公告)日:2004-02-26
Novel carbamate derivatives which are useful as drugs because of inhibiting activated blood coagulation factor X and thus exerting an anticoagulant effect. Compounds represented by the formula:
1
wherein R
1
represents a group represented by the formula:
2
(wherein Y
1
represents CH═CH, etc.), which may be substituted, etc.; the ring A represents an oxo-substituted nitrogen-containing heterocyclic ring which may be further substituted; R
2
represents a hydrogen atom, optionally substituted C
1-4
alkyl, etc.; R
3
represents optionally substituted C
1-4
alkyl, etc.; and Z represents an optionally substituted nitrogen containing heterocyclic group, etc., or salts thereof.