165948-23-2Relevant articles and documents
Substituted oxazolidinone compounds and method and use thereof
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Paragraph 0286; 0288; 0289, (2017/02/02)
The invention provides a substituted oxazolidinone compound represented by a formula (I) shown in specifications, or stereoisomers, tautomers, nitrogen oxides, solvates, metabolites and pharmaceutically acceptable salts or prodrugs thereof. The compound i
PRMT5 INHIBITORS AND USES THEREOF
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Paragraph 00651; 00652, (2016/04/20)
Described herein are compounds of Formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof:wherein Y1 is of formula (?) or formula (y):Ring Y is a 5- to 6-membered heteroaryl ring; and V4, V5, Rx, x, y, and n are as defined herein. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
Orally active factor Xa inhibitors: 4,5,6,7-tetrahydrothiazolo[5,4-c] pyridine derivatives
Haginoya, Noriyasu,Kobayashi, Syozo,Komoriya, Satoshi,Hirokawa, Yumiko,Furugori, Taketoshi,Nagahara, Takayasu
, p. 2935 - 2939 (2007/10/03)
In our investigation of factor Xa inhibitors, a series of 1-(6-chloronaphthalen-2-yl)sulfonyl-4-(4,5,6,7-tetrahydrothiazolo[5,4-c] pyridine-2-carbonyl)piperazines 3a-i were synthesized. In vitro inhibitory activities of the compounds against factor Xa and coagulation are summarized. Among the compounds, 3c and 3d, possessing a carbamoyl or N-methylcarbamoyl moiety, showed potent inhibitory activities when administered orally to rats.
Synthesis and conformational analysis of a non-amidine factor Xa inhibitor that incorporates 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine as S4 binding element
Haginoya, Noriyasu,Kobayashi, Syozo,Komoriya, Satoshi,Yoshino, Toshiharu,Suzuki, Makoto,Shimada, Takashi,Watanabe, Kengo,Hirokawa, Yumiko,Furugori, Taketoshi,Nagahara, Takayasu
, p. 5167 - 5182 (2007/10/03)
Our exploratory study was based on the concept that a non-amidine factor Xa (fXa) inhibitor is suitable for an orally available anticoagulant. We synthesized and evaluated a series of N-(6-chloronaphthalen-2-yl) sulfonylpiperazine derivatives incorporating various fused-bicyclic rings containing an aliphatic amine expected to be S4 binding element. Among this series, 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine type 61 displayed orally potent anti-fXa activity and evident prolongation of prothrombin time (PT) with the moderate bioavailability in rats. The X-ray crystal analysis afforded an obvious binding mode that 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c] pyridine and 6-chloronaphthalene respectively bound to S4 and S1 subsites. In this X-ray study, we discovered a novel intramolecular S-O close contact. Ab initio energy calculations of model compounds deduced that conformers with the most close S-O proximity were most stable. The Mulliken population analysis proposed that this energy profile was caused by both of electrostatic S-O affinity and N-O repulsion. The results of these calculations and X-ray analysis suggested a possibility that the restricted conformation effected the affinity to S4 subsite of fXa.
Compound with platelet aggregation inhibitor activity
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, (2008/06/13)
A compound represented by the general formula (I) and a pharmaceutically acceptable salt and solvate thereof having an effect for inhibiting the agglutination of platelets is disclosed: STR1 wherein R1 represents a group --W--(CH2)i --COOR3, R2 represents a hydrogen atom or a group --W--(CH2)i --COOR3 or --OR4, X represents --CH= or --N=, Y represents (i) a group --(CO)k --N(R5)--Z--, wherein Z represents a bond or a group --(CH2)m --CO-- or a group --(CH2)m --CHR6 --, (ii) a group --(CH2)m --N(R5)--(CO)k --, or (iii) a group --(CO)k -Het, wherein Het represents a five- or six-membered heterocyclic ring comprising a nitrogen atom, A represents (i) the following groups (III) or (IV) STR2 B represents a bond, C1-6 alkylene or C2-6 alkenylen.