acid catalytic system has been established, providing a direct approach for the preparation of diversesubstituted quinoline derivatives in high yields with wide functional group tolerance. Practically, the protocol can be easily scaled up to gram-scale and was utilized in the concise formal synthesis of a promising herbicide candidate.
The invention relates to compounds of formula (I):
or a salt thereof, wherein R
1
, G, L
1
, L
2
, L
3
, and Y are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are inhibitors of one, or both of, αvβ
1
integrin and αvβ
6
integrin that are useful for treating fibrosis such as in nonalcoholic steatohepatitis (NASH), idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP).
LACTAM-CONTAINING COMPOUNDS AND DERIVATIVES THEREOF AS FACTOR XA INHIBITORS
申请人:Bristol-Myers Squibb Company
公开号:US20170050964A1
公开(公告)日:2017-02-23
The present application describes lactam-containing compounds and derivatives thereof of Formula I:
P
4
—P-M-M
4
I
or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
There are provided o-carboxy-(5-oxo-2-imidazolin-2-yl)benzo-(6-membered)-heterocyclic compounds which contain one, two or three heteroatoms and derivatives thereof and a method for the use therewith to control monocotyledenous and dicotyledenous plant species.
A sultam derivative of Formula (1) described below having inhibitory action for aggrecanase activity is provided. The sultam derivative of Formula (1) and a salt thereof exhibit strong inhibitory action for aggrecanase activity in a living body of a mammalian animal including human, and is useful, for example, as an active ingredient of a pharmaceutical agent for preventing and/or treating various diseases caused by degradation of aggrecan.