cas 161886-21-1, Benzonitrile, 2-fluoro-5-hydrazino- (9CI)

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FACTOR XA COMPOUNDS
The present invention is directed to novel compounds of Formula (I) and forms and pharmaceutical compositions thereof, and the use thereof as inhibitors of Factor Xa.
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Page/Page column 33; 42

(2008/06/13)

1-[3-Aminobenzisoxazol-5′-yl]-3-trifluoromethyl-6-[2′-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1′]-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa
Attempts to further optimize the pyrazole factor Xa inhibitors centered on masking the aryl aniline P4 moiety. Scaffold optimization resulted in the identification of a novel bicyclic pyrazolo-pyridinone scaffold which retained fXa potency. The novel bicyclic scaffold preserved all binding interactions observed with the monocyclic counterpart and importantly the carboxamido moiety was integrated within the scaffold making it less susceptible to hydrolysis. These efforts led to the identification of 1-[3-aminobenzisoxazol-5′-yl]-3-trifluoromethyl-6-[2′-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1′]-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one 6f (BMS-740808), a highly potent (fXa Ki = 30 pM) with a rapid onset of inhibition (2.7 × 107 M-1 s-1) in vitro, selective (>1000-fold over other proteases), efficacious in the AVShunt thrombosis model, and orally bioavailable inhibitor of blood coagulation factor Xa.
Pinto, Donald J.P.,Orwat, Michael J.,Quan, Mimi L.,Han, Qi,Galemmo Jr., Robert A.,Amparo, Eugene,Wells, Brian,Ellis, Christopher,He, Ming Y.,Alexander, Richard S.,Rossi, Karen A.,Smallwood, Angela,Wong, Pancras C.,Luettgen, Joseph M.,Rendina, Alan R.,Knabb, Robert M.,Mersinger, Lawrence,Kettner, Charles,Bai, Steven,He, Kan,Wexler, Ruth R.,Lam, Patrick Y.S.
p. 4141 - 4147
(2007/10/03)

Process for the preparation of 1,3,5-trisubstituted pyrazoles via [3+2] cycloaddition
A process for the preparation of 1,3,5-trisubstituted pyrazole compounds, which are useful intermediates in the synthesis of factor Xa inhibitors.
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Page/Page column 4-5

(2008/06/13)

Structure-based design of novel guanidine/benzamidine mimics: Potent and orally bioavailable factor Xa inhibitors as novel anticoagulants
As part of an ongoing effort to prepare orally active factor Xa inhibitors using structure-based drug design techniques and molecular recognition principles, a systematic study has been performed on the pharmacokinetic profile resulting from replacing the
Lam, Patrick Y. S.,Clark, Charles G.,Li, Renhua,Pinto, Donald J. P.,Orwat, Michael J.,Galemmo, Robert A.,Fevig, John M.,Teleha, Christopher A.,Alexander, Richard S.,Smallwood, Angela M.,Rossi, Karen A.,Wright, Matthew R.,Bai, Stephen A.,He, Kan,Luettgen, Joseph M.,Wong, Pancras C.,Knabb, Robert M.,Wexler, Ruth R.
p. 4405 - 4418
(2007/10/03)

Herbicides
The invention provides compounds of formula: wherein R and R1 independently represent hydrogen, optionally halogenated alkyl alkenyl or alkynyl;, -(-CR3R4)n-(optionally subtituted phenyl); -(-CR3R4)nHet; or, -(-CR3R4)n-Ar, wherein Ar is an optionally substituted bicycle;, wherein at least one of the groups R and R1 represents -(-CR3R4)n-Ar;, R2 represents R5 or optionally substituted phenyl;, X is oxygen or sulphur; m is 0, 1, 2 or 3;, R3 and R4, independently represent hydrogen, alkyl or haloalkyl;, R5 is halogen, optionally halogenated alkyl, alkenyl or alkynyl;, or a group selected from cyano, nitro, -CO2R6, -S(O)pR6, -NR3R4, -COR6, -S(O)pR7, -CO2R7, -OR7, -CONR3R4, -OSO2R7, -OSO2R8, -OCH2R7, -N(R3)COR8, -N(R3)SO2R8, -N(R3)SO2R7, -SO2NR3R4, -Si(R8)3 and -OR6;, n is zero, 1 or 2; q is zero or an integer from 1 to 5;, Het represents an optionally substituted heterocycle;, R6 represents hydrogen, alkyl or haloalkyl;, p is zero, one or two; r is one or two;, R7 represents optionally substituted phenyl;, R8 represents alkyl or haloalkyl;, R61 and R62 independently represent hydrogen, halogen, alkyl or haloalkyl;, and agriculturally acceptable salts thereof;, which possess utility as herbicides.
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(2008/06/13)