185836-35-5Relevant articles and documents
Development of a practical synthesis to PI3K α-selective inhibitor GDC-0326
Koenig, Stefan G.,Green, Keena L.,Müller, Barbara,Sowell, C. Gregory,Askin, David,Gosselin, Francis
, (2020/12/29)
A practical route to PI3K α-selective inhibitor GDC-0326 is reported. The synthesis leverages an existing scheme to a key tetracyclic benzoxazepine intermediate and optimizes it for robustness and scalability, including removing numerous undesired conditions and reagents, as well as eliminating chromatographic purification steps. The process endgame is streamlined to utilize a single-step, stereocontrolled alkylation of the key phenol with a chiral lactamide mesylate, followed by recrystallization of the lactamide ether product, to deliver the desired enantiomer of the active pharmaceutical ingredient (API) GDC-0326.
SSAO INHIBITOR
-
Paragraph 0150-0152; 0489; 0490; 0491, (2020/04/02)
The present invention provides an SSAO inhibitor and an application thereof in preparing a drug for treating a disease related to SSAO. In particular, the present invention provides a compound shown in formula (IV) and a pharmaceutically acceptable salt thereof.
FUSED HETEROCYCLIC COMPOUND
-
Paragraph 0277, (2017/03/08)
The present invention provides a fused heterocyclic compound that has CDK 8 and/or CDK 19 inhibitory activity. The present invention provides a compound represented by formula (I) (wherein the symbols are as defined in the description) or a salt thereof.
The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (
Heffron, Timothy P.,Heald, Robert A.,Ndubaku, Chudi,Wei, BinQing,Augistin, Martin,Do, Steven,Edgar, Kyle,Eigenbrot, Charles,Friedman, Lori,Gancia, Emanuela,Jackson, Philip S.,Jones, Graham,Kolesnikov, Aleksander,Lee, Leslie B.,Lesnick, John D.,Lewis, Cristina,McLean, Neville,M?rtl, Mario,Nonomiya, Jim,Pang, Jodie,Price, Steve,Prior, Wei Wei,Salphati, Laurent,Sideris, Steve,Staben, Steven T.,Steinbacher, Stefan,Tsui, Vickie,Wallin, Jeffrey,Sampath, Deepak,Olivero, Alan G.
, p. 985 - 1002 (2016/02/23)
Inhibitors of the class I phosphoinositide 3-kinase (PI3K) isoform PI3Kα have received substantial attention for their potential use in cancer therapy. Despite the particular attraction of targeting PI3Kα, achieving selectivity for the inhibition of this
SELECTIVELY SUBSTITUTED QUINOLINE COMPOUNDS
-
Paragraph 0174; 0349, (2015/04/21)
Embodiments of the disclosure relate to selectively substituted quinoline compounds that act as antagonists or inhibitors for Toll-like receptors 7 and/or 8, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (SLE) and lupus nephritis.
Compounds as syk kinase inhibitors
-
Paragraph 0138; 0139, (2013/03/26)
The present invention relates to a compound of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by inhibition of Syk kinase.
COMPOSITION FOR AGRICULTURAL USE FOR CONTROLLING OR PREVENTING PLANT DISEASES CAUSED BY PLANT PATHOGENS
-
Page/Page column 225-226, (2010/11/19)
Disclosed is a composition for agricultural use, which is used for controlling or preventing plant diseases caused by plant pathogens. The composition for agricultural use contains a compound represented by formula (1), a salt thereof or a hydrate of the compound or the salt. (1) [In the formula, Z represents an oxygen atom, a sulfur atom or NRz; and E represents a furyl group, a thienyl group, a pyrrolyl group, a tetrazolyl group, a thiazolyl group, a pyrazolyl group, a phenyl group or the like.]
Indazoles, benzisoxazoles and benzisothiazoles as estrogenic agents
-
Page/Page column 15, (2008/06/13)
The present invention relates to compounds of formula (I): in which R1, R2, R3, X, Y and A are as defined in the specification. The compounds are modulators of the estrogen receptors.
5-5-MEMBERED FUSED HETEROCYCLIC COMPOUND AND USE THEREOF AS HCV POLYMERASE INHIBITOR
-
Page/Page column 126, (2008/06/13)
The present invention relates to a fused ring compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and
Compositions and methods using compounds having cytochrome P450RAI inhibitory activity co-administered with vitamin A
-
, (2008/06/13)
vitamin A, or a derivative of vitamin A having vitamin A like activity is co-administered with inhibitors of the CP450RAI1 and/or of CP450RAI2 enzymes for the purpose of treating diseases and conditions in mammals, including humans, which diseases or conditions are prevented, treated, ameliorated, or the onset of which is delayed by administration of retinoid compounds or by the mammalian organism's naturally occurring retinoic acid.