- HETEROCYCLIC COMPOUNDS AS MUTANT IDH INHIBITORS
-
The present disclosure relates generally to compounds useful in treatment of conditions associated with mutant isocitrate dehydrogenase (mt-IDH), particularly mutant IDH1 enzymes. Specifically, the present invention discloses compound of formula (IA), which exhibits inhibitory activity against mutant IDH1 enzymes. Method of treating conditions associated with excessive activity of mutant IDH1 enzymes with such compound is disclosed. Uses thereof, pharmaceutical composition, and kits are also disclosed.
- -
-
Paragraph 0238-0239
(2020/07/16)
-
- Asymmetric Synthesis of Chiral Primary Amines by Ruthenium-Catalyzed Direct Reductive Amination of Alkyl Aryl Ketones with Ammonium Salts and Molecular H2
-
A ruthenium/C3-TunePhos catalytic system has been identified for highly efficient direct reductive amination of simple ketones. The strategy makes use of ammonium acetate as the amine source and H2 as the reductant and is a user-friendly and operatively simple access to industrially relevant primary amines. Excellent enantiocontrol (>90% ee for most cases) was achieved with a wide range of alkyl aryl ketones. The practicability of this methodology has been highlighted by scalable synthesis of key intermediates of three drug molecules. Moreover, an improved synthetic route to the optimal diphosphine ligand C3-TunePhos is also presented.
- Tan, Xuefeng,Gao, Shuang,Zeng, Weijun,Xin, Shan,Yin, Qin,Zhang, Xumu
-
supporting information
p. 2024 - 2027
(2018/02/19)
-
- 3-PYRIMIDIN-4-YL-OXAZOLIDIN-2-ONES AS INHIBITORS OF MUTANT IDH
-
The invention is directed to a formula (I), or a pharmamceutically acceptable salt thereof, wherein R1, R2a, R2b and R3-R7 are herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.
- -
-
Page/Page column 158; 159; 172
(2014/09/29)
-
- AMINO-ALKYL-AMIDE DERIVATIVES AS CCR3 RECEPTOR LIQUIDS
-
The present invention relates to the CCR3 receptor ligands of the general formula (I), within them favourably to antagonists and to the salts, solvates and isomers thereof, to the pharmaceutical compositions containing them, to the use of the compounds of the general formula (I) and their salts, solvates and isomers and to the preparation of the compounds of the general formula (I) and their salts, solvates and isomers and to the new intermediates of the general formula (IIa).
- -
-
Page/Page column 26
(2010/11/26)
-
- 2-Mercaptoimidazoles, a new class of potent CCR2 antagonists
-
We describe the synthesis and SAR of a new class of CCR2 antagonists based on a 2-mercaptoimidazole scaffold. The initial lead 1a was optimized to the 3,4-disubstituted analogues 1p-(S) and 1q-(S), which have IC50 values in the MCP-1 induced Ca
- Van Lommen, Guy,Doyon, Julien,Coesemans, Erwin,Boeckx, Staf,Cools, Marina,Buntinx, Mieke,Hermans, Bart,VanWauwe, Jean
-
p. 497 - 500
(2007/10/03)
-
- AMIDE COMPOUND AND METHOD OF CONTROLLING PLANT DISEASE WITH THE SAME
-
A amid compound of the formula (1): wherein, in the formula, R51 represents a halogen atom, a C1-C6 alkyl group and the like; R52 represents a hydrogen atom, a halogen atom, a C1-C6 alkyl group and the like; R53 represents a halogen atom and the like; R56 represents a halogen atom and the like; R57 represents a hydrogen atom and the like; R58 and R59 independently represent a hydrogen atom, a C1-C3 alkyl group and the like; R60 represents a C1-C4 alkyl group, a C1-C4 haloalkyl group, a C3-C4 alkenyl group, or a C3-C6 alkynyl group; R61 represents a C1-C4 alkyl group, a C1-C4 haloalkyl group, a C3-C4 alkenyl group or a C3-C6 alkynyl group or a C2-C4 cyanoalkyl group; R62, R63 and R64 represent a hydrogen atom, a halogen atom and the like; X represents a oxygen atom or a sulfur atom; has an excellent activity against plant diseases.
- -
-
Page/Page column 107
(2010/02/14)
-
- N-(α-alkylbenzylidene)-α-phenylalkylamine, its use and process for producing the same and process for producing intermediate therefor
-
There is disclosed an N-(α-alkylbenzylidene)-α-phenylalkylamine represented by the general formula (1): STR1 wherein R1 represents a lower alkyl group, R2 represents a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group and X represents a halogen atom or a lower alkoxy group, its use and a process for producing the same and processes for producing intermediates therefor.
- -
-
-
- Triazine derivatives, a process for preparing the derivatives, and herbicides containing the derivatives as the effective component
-
A triazine derivative represented by the general formula: STR1 wherein R1 and R2 are each an alkyl group having 1 to 4 carbon atoms, and X1 and X2 are each a halogen atom, an alkyl group having 1 to 4 carbon atoms, an alkoxyl group having 1 to 4 carbon atoms, or an alkylthio group having 1 to 4 carbon atoms. This invention also provides a process for efficiently preparing said triazine derivative and a herbicide containing said triazine derivative as effective component.
- -
-
-