6311-73-5Relevant academic research and scientific papers
Pyrimidine fused ring derivatives and application thereof in medicine
-
, (2021/05/26)
The invention relates to compounds shown in a general formula (I) or stereoisomers, deuterated compounds, solvates, prodrugs, metabolites, pharmaceutically acceptable salts or co-crystal of the compounds, an intermediate and a preparation method of the compounds, and application of the compounds in preparation of drugs for treating diseases related to activity or expression quantity of KRas-G12C.
INHIBITORS OF KRAS G12C MUTANT PROTEINS
-
, (2018/04/17)
Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I), or a pharmaceutically acceptable salt, tautomer, stereoisomer or prodrug thereof, wherein B, W, X, Y, R1, R2a, R2b, R3a, R3b, R4a, R4b, G1, G2, m1, m2, L1, L2 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
CARBAZOLE AND CARBOLINE KINASE INHIBITORS
-
Page/Page column 163, (2010/08/04)
The present invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) compounds inhibit tyrosine kinase activity of Jak2, thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.
KINASE INHIBITORS
-
Page/Page column 45; 46, (2010/11/08)
Disclosed are protein kinase inhibitors of Formula Ia and Ib, compositions comprising such inhibitors, and methods of use, thereof. More particularly, these compounds and compositions are inhibitors of Aurora-A (Aurora-2) and Aurora-B (Aurora-1) protein k
Effect of a-ring modifications on the DNA-binding behavior and cytotoxicity of pyrrolo[2,1-c][1,4]benzodiazepines
Thurston, David E.,Bose, D. Subhas,Howard, Philip W.,Jenkins, Terence C.,Leoni, Alberto,Baraldi, Pier G.,Guiotto, Andrea,Cacciari, Barbara,Kelland, Lloyd R.,Foloppe, Marie-Paule,Rault, Sylvain
, p. 1951 - 1964 (2007/10/03)
Several A-ring-modified analogues of the DNA-binding antitumor agent DC- 81 (5) have been synthesized in order to study structure- reactivity/cytotoxicity relationships. For two molecules (23 and 30) the modifications required the addition of a fourth rin
FUSED HETEROCYCLIC COMPOUNDS, HAVING ANGIOTENSIN II ANTAGONISTIC ACTIVITY
-
, (2008/06/13)
Fused heterocyclic compounds of the formula (I): STR1 wherein R. sup.1 is an optionally substituted hydrocarbon residue which may be attached through a hetero atom; R 2 is a group capable of forming an anion or a group convertible thereinto; R 3 is an optionally substituted aromatic hydrocarbon or heterocyclic residue which contains at least one hetero atom; X is a direct bond or a spacer having an atomic length of two or less between the R 3 group and the ring W group; W is an optionally substituted aromatic hydrocarbon or heterocyclic residue which contains at least one hereto atom; a,c and d are independently selected from the group consisting of one or two optionally substituted carbon atoms and one or two optionally substituted hetero atoms; b and e are independently selected from the group consisting of one optionally substituted carbon atom and one optionally substituted nitrogen atom wherein one of b or e must be nitrogen; the dotted line is a bond to form one double bond; n is an integer of 1 or 2 and when a, which is an optionally substituted carbon atom, is taken together with R 1, the following group: STR2 may form a ring group; provided that when STR3 is a benzimidazole, thieno[3,4-d] imidazole, or thieno[2,3-d] imidazole ring, at least one of the group: STR4 and R 3 is an optionally substituted heterocyclic residue; and the pharmaceutically acceptable salts thereof, have potent angiotensin II antagonistic activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases (e.g. hypercardia, heart failure, cardiac infarction, etc.), strokes, cerebral apoplexy, nephritis, etc.
