Synthesis of 4-(4-guanidinobenzoyloxy)benzamides and 1-(4-guanidinobenzoyloxy)benzoyloxy acetamides as trypsin inhibitors
摘要:
Seventeen new compounds of 4-(4-guanidinobenzoyloxy)benzamides and 4-(4-guanidinobenzoyloxy)benzoyloxyacetamides were prepared and their inhibitory activities on trypsin, thrombin and porcine pancreatic elastase were measured. These compounds were found to be selective trypsin inhibitors with inhibiting activities from 0.44 to 43 mu M.
PYRIMIDINE COMPOUND, PREPARATION METHOD THEREOF AND MEDICAL USE THEREOF
申请人:Ancureall Pharmaceutical (Shanghai) Co., Ltd.
公开号:US20210101881A1
公开(公告)日:2021-04-08
The present invention discloses a pyrimidine compound, a preparation method thereof and a medical use thereof. Specifically, the present invention discloses a pyrimidine compound represented by formula (I), pharmaceutically acceptable salts thereof, a preparation method thereof, and a use thereof as a cyclin-dependent kinase 9 (CDK9) inhibitor, particularly for the treatment of cancer. The definition of each group in formula (I) is the same as that in the specification.
The invention relates to novel imidazopyridine derivatives and to their use in the treatment of diseases and disorders which may e.g. involve angiogenesis and/or pain, including autoimmune and inflammatory diseases.
Process for Isomerization of CIS-2-Pentenenitrile to 3-Pentenenitriles
申请人:BASF SE
公开号:US20130289299A1
公开(公告)日:2013-10-31
The present invention relates to an improved process for batchwise or continuous isomerization of cis-2-pentenenitrile to 3-pentenenitriles in the presence of 1,4-diazabicyclo[2.2.2]octane as catalyst.
The invention provides a compound of formula I:
wherein A
1
, A
2
, A
3
, R
1
, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.
The present invention relates to compounds of formula I
wherein s, R
1a
and R
1
to R
3
are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.