146552-71-8Relevant articles and documents
NOVEL NICOTINAMIDE DERIVATIVES OR SALTS THEREOF
-
Paragraph 1232; 1235; 1236, (2018/09/08)
An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. Th e present invention provides a nicotinamide derivative represented by the follo wing formula (I) (wherein R 1 represents a halogen atom; R 2 represents a C 1-12 alkyl group, a C 2-12 alkenyl group, a C 2-12 alkynyl group, a C 3-8 cycloalkyl g roup, an aryl group, an ar-C 1-6 alkyl group or a heterocyclic group, each opti onally having at least one substituent; R 3 represents an aryl group or a hetero cyclic group each optionally having at least one substituent; and R 4 and R 5 e ach independently represent a hydrogen atom; and R 2 and R 4 may form a cyc lic amino group optionally having at least one substituent together with the ni trogen atom to which they bind) or a salt thereof, and a pharmaceutical comp osition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.
CARBAZOLE-CONTAINING AMIDES, CARBAMATES, AND UREAS AS CRYPTOCHROME MODULATORS
-
, (2015/10/28)
The subject matter herein is directed to carbazole-containing amide, carbamate, and urea derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I wherein the variable R1, R2, R3, R4, R5, R6, R7, A, D, E, G, J, L, M, Q, a, and b are accordingly described. Also provided are pharmaceutical compositions containing the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, complications associated with diabetes, Cushing's syndrome, NASH, NAFLD, asthma, and COPD.
Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering
Johannes, Jeffrey W.,Almeida, Lynsie,Daly, Kevin,Ferguson, Andrew D.,Grosskurth, Shaun E.,Guan, Huiping,Howard, Tina,Ioannidis, Stephanos,Kazmirski, Steven,Lamb, Michelle L.,Larsen, Nicholas A.,Lyne, Paul D.,Mikule, Keith,Ogoe, Claude,Peng, Bo,Petteruti, Philip,Read, Jon A.,Su, Nancy,Sylvester, Mark,Throner, Scott,Wang, Wenxian,Wang, Xin,Wu, Jiaquan,Ye, Qing,Yu, Yan,Zheng, Xiaolan,Scott, David A.
, p. 5743 - 5747 (2015/11/24)
The propensity for cancer cells to accumulate additional centrosomes relative to normal cells could be exploited for therapeutic benefit in oncology. Following literature reports that suggested TNKS1 (tankyrase 1) and PARP16 may be involved with spindle s