A novel cationic [IrH(THF)(P,N)(imine)] [BArF] catalyst containing a P-stereogenic MaxPHOX ligand is described for the direct asymmetrichydrogenation of N-methyl and N-alkyl imines. This is the first catalytic system to attain high enantioselectivity (up to 94% ee) in this type of transformation. The labile tetrahydrofuran ligand allows for effective activation and reactivity, even at low temperatures
PROCESS FOR PRODUCING (S)-3-[(1-DIMETHYLAMINO)ETHYL] PHENYL-N-ETHYL-N-METHYL-CARBAMATE VIA NOVEL INTERMEDIATES
申请人:Dubey Shailendra Kumar
公开号:US20120022281A1
公开(公告)日:2012-01-26
Disclosed herein are novel intermediates and process for large scale production of (S)-3-[(1-dimethylamino)ethyl]phenyl-N-ethyl-N-methyl-carbamate (rivastigmine) or its pharmaceutically acceptable salts employing the novel intermediates. Further provided are methods for producing the novel intermediates thereof.
The invention relates to compounds of formula (I)
Z-C(R
1
R
2
)—C(R
3
NH
2
)—C(R
4
R
5
)—X—N(R
6
R
7
) (I),
wherein Z, R
1-7
and X have the meaning as cited in the description and the claims. Said compounds are useful as DPP-IV inhibitors. The invention also relates to the preparation of such compounds as well as the production and use thereof as medicament.
TRICYCLIC PYRIDO-CARBOXAMIDE DERIVATIVES AS ROCK INHIBITORS
申请人:BRISTOL-MYERS SQUIBB COMPANY
公开号:US20160152628A1
公开(公告)日:2016-06-02
The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.