- PROCESS FOR THE PREPARATION OF APIXABAN
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The present invention relates to an improved process for the preparation of Apixaban and its intermediates.
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Paragraph 0061; 0062
(2017/11/16)
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- AN IMPROVED PROCESS FOR THE PREPARATION OF APIXABAN
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The present invention relates to an improved process for the preparation of Apixaban and its intermediates.
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Page/Page column 11; 12
(2017/12/09)
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- NOVEL PROCESS FOR THE PREPARATION OF A LACTAM-CONTAINING COMPOUND
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Provided herein is a novel, commercially viable and industrially advantageous process for the preparation of 1-(4-Methoxyphenyl)-7-oxo-6-[4-(2-oxo-1-piperidinyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazole-[3,4-c]pyridine-3-carboxamide, in high yield and with high purity, using a novel intermediate 3-chloro-1-(4-iodophenyl)-5,6-dihydropyridin-2(1H)-one.
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Page/Page column 24
(2015/12/08)
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- Novel intermediate and polymorphs of 1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetra hydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide and process thereof
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The present invention provides a novel intermediate as well as novel polymorphs of 1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide compound represented by the following structural formula-1 and processes for their preparation.
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Paragraph 0127
(2016/01/10)
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- PYRAZOLE CARBOXAMIDE INHIBITORS OF FACTOR XA
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The present invention relates to new pyrazole carboxamide inhibitors of factor Xa, pharmaceutical compositions thereof, and methods of use thereof.
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Page/Page column 29
(2010/04/06)
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- Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties
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The bicyclic dihydropyrazolopyridinone scaffold allowed for incorporation of multiple P1 moieties with subnanomolar binding affinities for blood coagulation factor Xa. The compound 3-[6-(2′-dimethylaminomethyl-biphenyl-4-yl)-7-oxo-3-trifluoro-methyl-4,5,6,7-tetrahydro-pyrazolo[3,4-c]pyridine-l-yl]-benzamide 6d shows good fXa potency, selectivity, in vivo efficacy and oral bioavailability. Compound 6d was selected for further pre-clinical evaluations.
- Pinto, Donald J.P.,Galemmo Jr., Robert A.,Quan, Mimi L.,Orwat, Michael J.,Clark, Charles,Li, Renhua,Wells, Brian,Woerner, Francis,Alexander, Richard S.,Rossi, Karen A.,Smallwood, Angela,Wong, Pancras C.,Luettgen, Joseph M.,Rendina, Alan R.,Knabb, Robert M.,He, Kan,Wexler, Ruth R.,Lam, Patrick Y.S.
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p. 5584 - 5589
(2007/10/03)
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- 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
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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.
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p. 4141 - 4147
(2007/10/03)
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