- COMPOUNDS FOR THE TREATMENT OF MEDICAL DISORDERS
-
Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula (I), or a pharmaceutically acceptable salt or composition thereof The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduce the excessive activation of complement.
- -
-
-
- AMIDE COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS
-
Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an amide substituent (R32) are provided. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein are capable of reducing the excessive activation of complement.
- -
-
-
- Dihydro pyridine compound, its composition, preparation method and use
-
Disclosed dihydropyridine compounds are the compounds possessing the following general formula (I) as shown in the specification, wherein R1 is selected from hydrogen, halogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, alkylamino, substituted alkylamino, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclic groups, substituted heterocyclic groups, ester group and amide group; R2 is selected from hydrogen, cyanogroup, alkyl, substituted alky, alkenyl, substituted alkenyl and acyl; or R2 and R3 form a fused ring; R3 is selected from alkyl, substituted alkyl, aryl, substituted aryl, heteroaryl and substituted heteroaryl; or R3 and R2 or R4 form a fused ring; R4 is selected from hydrogen, alkyl and substituted alkyl; or R4 and R3 or R5 form a fused ring; R5 is selected form alkyl, substituted alky, aryl, substituted aryl, heteroaryl and substituted heteroaryl; or R5 and R4 form a fused ring. The invention also discloses a preparation method of the compounds of the general formula (I), compositions containing the compounds of the general formula (I), and applications of the compositions to medicaments for treating cancers.
- -
-
-
- BICYCLIC HETEROCYCLIC COMPOUNDS AS ROR GAMMA MODULATORS
-
The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as modulator of retinoid-related orphan receptor gamma t (RORγt). These compounds prevent, inhibit, or suppress the action of RORγt and are therefore useful in the treatment of RORγt mediated disease, disorder, syndrome or condition such as pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, neurodegenerative diseases or cancer.
- -
-
-
- Discovery of (S)-1-(1-(Imidazo[1,2- a ]pyridin-6-yl)ethyl)-6-(1-methyl-1 H -pyrazol-4-yl)-1 H -[1,2,3]triazolo[4,5- b ]pyrazine (Volitinib) as a Highly Potent and Selective Mesenchymal-Epithelial Transition Factor (c-Met) Inhibitor in Clinical Development for Treatment of Cancer
-
HGF/c-Met signaling has been implicated in human cancers. Herein we describe the invention of a series of novel triazolopyrazine c-Met inhibitors. The structure-activity relationship of these compounds was investigated, leading to the identification of compound 28, which demonstrated favorable pharmacokinetic properties in mice and good antitumor activities in the human glioma xenograft model in athymic nude mice.
- Jia, Hong,Dai, Guangxiu,Weng, Jianyang,Zhang, Zhulin,Wang, Qing,Zhou, Feng,Jiao, Longxian,Cui, Yumin,Ren, Yongxin,Fan, Shiming,Zhou, Jinghong,Qing, Weiguo,Gu, Yi,Wang, Jian,Sai, Yang,Su, Weiguo
-
p. 7577 - 7589
(2014/12/11)
-
- CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR
-
Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.
- -
-
-
- CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR
-
Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.
- -
-
-
- FUSED HETEROCYCLIC COMPOUND
-
The present invention aims to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like. A glucokinase activator containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.
- -
-
Page/Page column 39
(2009/07/18)
-
- TEC KINASE INHIBITORS
-
Disclosed are compounds of formula (I): (F) wherein Ri, R2, X and Ar are defined herein. The compounds of the invention inhibit Itk kinase and are therefore useful for treating diseases and pathological conditions involving inflammation, immunological disorders and allergic disorders. Also disclosed are processes for preparing these compounds and to pharmaceutical compositions comprising these compounds.
- -
-
Page/Page column 24
(2010/11/27)
-
- THIENOPYRAZOLES
-
Thienopyrazoles, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical uses in the treatment of disease states capable of being modulated by the inhibition of the protein kinases, in particular interleukin-2 inducible tyrosine kinase (ITK).
- -
-
Page/Page column 75-76
(2008/06/13)
-
- MODULATORS OF CELLULAR ADHESION
-
The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1-R4, n, p, A, B, D, E, L and AR1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders mediated by the CD11/CD18 family of cellular adhesion molecules (e.g., LFA-1).
- -
-
Page/Page column 139
(2010/02/11)
-
- Diacid-substituted heteroaryl derivatives as matrix metalloproteinase inhibitors
-
The invention provides dicarboxylic acid-substituted heteroaryl derivatives of the formula G1-(C(R1)R2)n-Q1-B-Q2-(C(R3)R4)m-G2??I or a pharmaceutically acceptable salt thereof, wherein G1, G2, R1, R2, R3, R4, n, m, Q1, Q2, and B are as defined in the specification. The invention compounds are inhibitors of matrix metalloproteinase enzymes, including MMP-13. This invention also provides pharmaceutical compositions and methods of treating diseases mediated by MMP-13, including arthritis, asthma, heart disease, atherosclerosis, and osteoporosis, or a pharmaceutically acceptable salt thereof.
- -
-
-