165947-55-7Relevant articles and documents
Identification of 2-substituted pyrrolo[1,2-b]pyridazine derivatives as new PARP-1 inhibitors
Xiang, Hao-Yue,Chen, Jian-Yang,Huan, Xia-Juan,Chen, Yi,Gao, Zhao-bing,Ding, Jian,Miao, Ze-Hong,Yang, Chun-Hao
, (2021)
A library of new 2-substituted pyrrolo[1,2-b]pyridazine derivatives were rapidly assembled and identified as PARP inhibitors. Structure-activity relationship for this class of inhibitor resulted in the discovery of most potent compounds 15a and 15b that e
Design and synthesis of 2-(4,5,6,7-tetrahydrothienopyridin-2-yl)-benzoimidazole carboxamides as novel orally efficacious Poly(ADP-ribose)polymerase (PARP) inhibitors
Chen, Xuxing,Huan, Xiajuan,Liu, Qiufeng,Wang, Yuqin,He, Qian,Tan, Cun,Chen, Yi,Ding, Jian,Xu, Yechun,Miao, Zehong,Yang, Chunhao
supporting information, p. 389 - 403 (2018/01/17)
The nuclear protein poly(ADP-ribose) polymerases-1/2 (PARP-1/2) are involved in DNA repair damaged by endogenous or exogenous process. And PARP-1/2 inhibitors have been proved to be clinically efficacious for DNA repair deficient tumors in the past decade
SUBSTITUTED SULFONAMIDE DERIVATIVES
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, (2009/11/29)
The invention relates to substituted sulfonamide derivatives, processes for the preparation thereof, medicaments containing these compounds and the use of substituted sulfonamide derivatives for the preparation of medicaments.
Structure-activity relationship of 6-methylidene penems bearing 6,5 bicyclic heterocycles as broad-spectrum β-lactamase inhibitors: Evidence for 1,4-thiazepine intermediates with C7 R stereochemistry by computational methods
Venkatesan, Aranapakam M.,Agarwal, Atul,Abe, Takao,Ushirogochi, Hideki,Yamamura, Itsuka,Ado, Mihira,Tsuyoshi, Takasaki,Dos Santos, Osvaldo,Gu, Yansong,Sum, Fuk-Wah,Li, Zhong,Francisco, Gerry,Lin, Yang-I.,Petersen, Peter J.,Yang, Youjun,Kumagai, Toshio,Weiss, William J.,Shlaes, David M.,Knox, James R.,Mansour, Tarek S.
, p. 4623 - 4637 (2007/10/03)
The design and synthesis of a series of 6-methylidene penems containing [6,5]-fused bicycles (thiophene, imidazole, or pyrazle-fused system) as novel class A, B, and C β-lactamase inhibitors is described. These penems proved to be potent inhibitors of the TEM-1 (class A) and AmpC (class C) β-lactamases and less so against the class B metallo-β-lactamase CcrA. Their in vitro and in vivo activities in combination with piperacillin are discussed. On the basis of the crystallographic structures of a serine-bound reaction intermediate of 2 with SHV-1 (class A) and GC1 (class C) enzymes, compounds 14a-1 were designed and synthesized. Penems are proposed to form a seven-membered 1,4 thiazepine ring in both class A and C β-lactamases. The interaction energy calculation for the enzyme-bound intermediates favor the formation of the C7 R enantiomer over the S enantiomer of the 1,4-thiazepine in both β-lactamases, which is consistent with those obtained from the crystal structure of 2 with SHV-1 and GC1.
Bicyclic 6-alkylidene-penems as class-D beta-lactamases inhibitors
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Page/Page column 15, (2010/11/25)
This invention relates to certain bicyclic 6-alkylidene penems which act as a inhibitor of class-D enzymes. β-Lactamases hydrolyze β-lactam antibiotics, and as such serve as the primary cause of bacterial resistance. The compounds of the present invention when combined with β-lactam antibiotics will provide an effective treatment against life threatening bacterial infections. In accordance with the present invention there are provided compounds of general formula I or a pharmaceutically acceptable salt or in vivo hydrolyzable ester R5 thereof: wherein: One of A and B denotes hydrogen and the other an optionally substituted fused bicyclic heteroaryl group; and X═O or S.
BICYCLIC 6-ALKYLIDENE-PENEMS AS ?-LACTAMASES INHIBITORS
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Page/Page column 57, (2008/06/13)
The present invention provides a compound of Formula (I), pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.
PROCESS FOR PREPARING 6-ALKYLIDENE PENEM DERIVATIVES
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Page/Page column 76, (2010/02/07)
The present invention provides a process of making compounds of Formula (I), which are useful for the treatment of bacterial infection or disease.
γ-Diketone compounds with inhibitory activity against platelet aggregation
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, (2008/06/13)
A γ-diketone compound represented by the following formula (I) and a pharmaceutically acceptable salt and solvate thereof having platelet aggregation inhibitory activity is disclosed: STR1 wherein B is --Z--(CH2)q COOR7 an
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.