630382-44-4

Upstream product

• 545445-40-7 3-morpholin-4-yl-5,6-dihydro-1H-pyridin-2-one 
• 116853-79-3 trifluoroacetaldehyde 4-methoxyphenylhydrazone 
• 207976-92-9 3-chloro-5,6-dihydro-1H-pyridin-2-one 
• 41419-12-9 3,3-dichloro-piperidin-2-one 
• 675-20-7 piperidin-2-one 

Downstream Products

• 630382-45-5 1-{4-[1-(4-methoxyphenyl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]phenyl}cyclopropanecarboxylic acid 
• 630384-47-3 6-{4-[1-(4,5-dihydro-1H-imidazol-2-yl)cyclopropyl]phenyl}-1-(4-methoxyphenyl)-3-trifluoromethyl-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-7-one 

Relevant academic research and scientific papers

HYDRAZINE COMPOUND AS BLOOD COAGULATION FACTOR Xa INHIBITOR

Provided is a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein X is selected from a 3-9 membered carbon ring or its phenyl ring, and a 4-10 membered heterocyclic ring or its benzo ring; Y and Z are independently selected from 4-9 membered saturated heterocyclic rings respectively; RI-3 are independently selected from H, F, Cl, Br, I, CN, OH, SH,NH2, CHO, COOH respectively, or selected from C1-10 alkyls or heteroalkyls optionally substituted by R01, C3-10 alkyls ring hydrocarbon groups or heterocyclic hydrocarbon groups, C1-10 alkyls or heteroalkyls substituted by C3-10 ring hydrocarbon groups or heterocyclic hydrocarbon group. The compound can be used as an anticoagulant for treating and preventing thrombotic disorders, and can meet the real needs of selectivity and a potent inhibitor for coagulation Xa.

Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: Discovery of novel, highly potent inhibitors of Factor Xa

Ortho-substituted biphenyl moieties are widely used in drug design. We herein report a successful use of the perpendicular conformation of the alpha-substituted phenylcyclopropyl groups to mimic the aplanar, biologically active conformation of the ortho-substituted biphenyl moieties to achieve structural diversity. This is exemplified by the design and synthesis of a series of highly potent pyrazole bicyclic-based Factor Xa (FXa) inhibitors bearing alpha-substituted phenylcyclopropyl P4 moieties. The designed perpendicular conformation was confirmed by the X-ray structure of FXa-bound compound 2r. The potential structural basis for the high FXa potency in the phenylcyclopropyl P4 analogs and their improved FXa inhibitory activities compared with the biphenyl P4 counterparts are discussed.

LINEAR CHAIN SUBSTITUTED MONOCYCLIC AND BICYCLIC DERIVATIVES AS FACTOR XA INHIBITORS

The present application descirbes linear chain subtituted monocyclic and byciclic compounds and derivatives thereof of formula (I): P4-P-M-M4 or pharmaceutically acceptable salts from thereof, P-M are rings substituted by a linear group. Compounds of the present invention are useful as inhibitors of trypsin like serine proteases, specifically factor Xa.