- IMPROVED METHODS, KITS, COMPOSITIONS AND DOSING REGIMENS FOR THE USE OF HETEROCYCLIC INHIBITORS OF ERK1 AND ERK2
-
The present application provides improved compositions, methods, kits and dosing regimens for the use of heterocyclic compounds and pharmaceutically acceptable salts, prodrugs, solvates, hydrates, or stereoisomers thereof. These compositions, methods, kit
- -
-
Page/Page column 125-126
(2021/05/07)
-
- HETEROCYCLIC INHIBITORS OF ERK1 AND ERK2 AND THEIR USE IN THE TREATMENT OF CANCER
-
The present application provides novel heterocyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful for inhibiting ERK1/2. By administering to a patient in need a
- -
-
Paragraph 0532-0533
(2017/01/02)
-
- 2-hydroxy-4-amino-5-picoline heterocyclic compounds
-
The invention discloses a 2-hydroxy-4-amino-5-methylpyridine heterocyclic compound which can be used as an intermediate for synthesizing an omeprazole compound. The invention further discloses a synthesis method of a 2-hydroxy-4-amino-5-methylpyridine heterocyclic compound. The synthesis method comprises four steps of synthesis of 2-chloro-5-methylpyridine nitrogen oxide, synthesis of 2-chloro-4-nitro-5-methylpyridine nitrogen oxide, synthesis of 2-chloro-4-amino-5-methylpyridine and synthesis of 2-hydroxy-4-amino-5-methylpyridine. The synthesis method of the 2-hydroxy-4-amino-5-methylpyridine heterocyclic compound disclosed by the invention is simple, reaction raw materials are low in price, and a synthesis route is environment-friendly.
- -
-
Paragraph 0025; 0030-0034
(2017/01/23)
-
- HETEROARYLS AND USES THEREOF
-
This invention provides compounds of formula IB: and also provides compounds of formulas ID, IIB, VB, and IIC: wherein HY, R1, R2, G5, G6, G7, G8, and G9 are as described in the specification. The compounds are inhibitors of VPS34 and/or PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
- -
-
Paragraph 0843
(2013/07/05)
-
- Synthesis of heteroaryl-fused pyrazoles as P38 kinase inhibitors
-
The synthesis of pyrazolo-pyridine, pyrimidine, pyrazine and pyridazine heterocycles is described. In addition, we report the utilization of 2,4-difluorophenoxide as a leaving group, to facilitate formation of the desired pyrazole adducts.
- Abbot, Sarah C.,Billedeau, Roland J.,Dewdney, Nolan J.,Gabriel, Tobias,Goldstein, David M.,McCaleb, Kristen L.,Soth, Michael,Trejo-Martin, Teresa Alejandra,Zecic, Hasim
-
experimental part
p. 2811 - 2826
(2010/04/25)
-
- FUSED PYRAZOLE AS p38 MAP KINASE INHIBITORS
-
Fused pyrazoles effective as p38 MAP kinase inhibitors, methods of making the compounds, and methods of using the compounds for treatment of p38 MAP kinase-mediated diseases.
- -
-
Page/Page column 43
(2008/06/13)
-
- AMINOPYRIMIDINE COMPOUNDS AND THEIR SALTS, PROCESS FOR PREPARATION AND PHARMACEUTICAL USE THEREOF
-
The present invention provides aminopyrimidine compounds of formula (I) and their salts, wherein R1, R2, R3, R4, R5, R6, Q, Z, L, m, n are defined as the description, the methods for preparation thereof, the uses thereof and the pharmaceutical compositions comprising the effective amount of compounds of formula (I). The compounds of formula (I) and their salts can be used as protein kinase inhibitors.
- -
-
Page/Page column 13
(2008/06/13)
-
- PYRIDINE DERIVATIVES AND THEIR USE AS MEDICAMENTS FOR TREATING DISEASES RELATED TO MCH RECEPTOR
-
The present invention encompasses novel substituted pyridine compounds of Formula (I), which act as MCH receptor antagonists. These compositions and pharmaceutical compositions thereof are useful in the prophylaxis or treatment of improving memory function, sleeping and arousal, anxiety, depression, mood disorders, seizure, obesity, diabetes, appetite and eating disorders, cardiovascular disease, hypertension, dyslipidemia, myocardial infarction, binge eating disorders including bulimia, anorexia, mental disorders including manic depression, schizophrenia, delirium, dementia, stress, cognitive disorders, attention deficit disorder, substance abuse disorders and dyskinesias including Parkinson's disease, epilepsy, and addiction.
- -
-
Page/Page column 54
(2010/10/20)
-
- Heteroaryl-fused pyrazolo derivatives and methods for using the same
-
Compounds of the formula I: where A, B, X, Y, Z, k, R1, R2 and R3 are those defined herein, and compositions comprising the same. The present invention also provides methods for preparing compounds of formula I and using t
- -
-
Page/Page column 35; 44
(2010/02/13)
-
- PYRIDINE INHIBITORS OF ERK2 AND USES THEREOF
-
The present invention relates to compounds useful of inhibitors of protein kinases of formula (I). The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of var
- -
-
Page/Page column 24; 39
(2008/06/13)
-
- PYRROLE COMPOUNDS AS INHIBITORS OF ERK PROTEIN KINASE, SYNTHESIS THEREOF AND INTERMEDIATES THERETO
-
The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
- -
-
Paragraph 0091
(2010/02/14)
-
- PYRROLE DERIVATIVES AS INHIBITORS OF ERK2 AND USES THEREOF
-
Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein A1, A2, TmR1, X, R2, R3, R9, R12, and R13 Are as described in t
- -
-
Page/Page column 48-49
(2010/02/07)
-