- PYRAZOLOCHLOROPHENYL COMPOUNDS, COMPOSITIONS AND METHODS OF USE THEREOF
-
Compounds of Formula (I) and methods of use as Janus kinase inhibitors are described herein.
- -
-
Page/Page column 89-90
(2018/10/19)
-
- Synthesis of 4-Quinolones: N,O-Bis(trimethylsilyl)acetamide-Mediated Cyclization with Cleavage of Aromatic C-O Bond
-
The synthesis of 1,4-dihydro-4-oxoquinoline derivatives (4-quinolones) based on a BSA [N,O-bis(trimethylsilyl)acetamide]-mediated cyclization of substituted 1-(2-methoxyphenyl)-3-(alkyl/arylamino)prop-2-en-1-ones is described. The reaction belongs to a rare set of cyclizations in which a methoxy group serves as the leaving group. Reaction takes place by the action of silylating agent under mild conditions and provides high yields of pure products following simple aqueous work-up. The versatility of the approach is exemplified by a wide range of 1-alkyl/aryl 3-carboxylates and 3-nitriles that have been prepared. A crucial advantage of this approach is the facile availability of starting methoxy compounds enabling new synthetic possibilities as well as improved cost efficiency. A new approach to the synthesis of 1,4-dihydro-4-oxoquinoline (4-quinolone) derivatives using a BSA-mediated reaction was developed; this entails an example of rare cyclizations in which an OMe group serves as a leaving group. This transformation has great synthetic potential due to the phenolic framework of starting materials and the mildness of the reagent.
- Pí?a, Ond?ej,Rádl, Stanislav
-
p. 2336 - 2350
(2016/05/19)
-
- 5-CHLORO-2-DIFLUOROMETHOXYPHENYL PYRAZOLOPYRIMIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE THEREOF
-
Compounds of Formula (00A) and methods of use as Janus kinase inhibitors are described herein.
- -
-
Paragraph 0652
(2015/12/05)
-
- 2-Thiopyrimidinones
-
Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.
- -
-
Paragraph 0239; 0240; 0241
(2013/05/22)
-
- PYRAZOLOPYRIMIDINE JAK INHIBITOR COMPOUNDS AND METHODS
-
A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical
- -
-
Page/Page column 73-74
(2011/02/24)
-
- Pyrimidines and uses thereof
-
The invention relates to pyrimidines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase β (LPAAT-β) activity and/or proliferation of cells such as tumor-cells.
- -
-
-