454-15-9Relevant academic research and scientific papers
(PYRIDIN-2-YL)AMINE DERIVATIVES AS TGF-BETA R1 (ALK5) INHIBITORS FOR THE TREATMENT OF CANCER
-
Paragraph 00305-00306, (2020/07/15)
The present invention relates to pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment and/or prevention of a proliferation disorder associated with ΤGFβR1 activity, such as a cancer or fibrosis. The invention provides compounds of Formula (I) and Formula (II) as further described herein having an acidic moiety that enhances tissue specificity for targeted tissues and organs. The invention includes pharmaceutical compositions, pharmaceutical combinations, and methods of use of these compounds for treating conditions including cancer or fibrosis.
CK2 INHIBITORS, COMPOSITIONS AND METHODS THEREOF
-
Paragraph 0453; 0466, (2018/02/01)
The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula (I), or a stereoisomer, a tautomer or a pharmaceutically acceptable salt thereof. For Formula (I) compounds R1, R2, R3, Ar and Z are as defined in the specification. The inventive Formula (I) compounds are inhibitors of CK2 and find utility in any number of therapeutic applications, including but not limited to treatment of proliferative disorders such as cancer, inflammation and immunological disorders.
THERAPEUTIC COMPOUNDS
-
Paragraph 0395; 0403; 0404, (2017/01/23)
The invention provides compounds of formula (I): wherein, A, C, D, X, and Y have any of the values defined in the specification, and salts thereof. The compounds are SIRT2 inhibitors and are useful for treating SIRT2 associated conditions.
NOVEL 4,6-DISUBSTITUTED AMINOPYRIMIDINE DERIVATIVES HAVING BOTH AROMATIC AND HALOGENIC SUBSTITUENTS
-
Paragraph 0356; 0357, (2014/03/24)
Certain 4,6-disubstituted aminopyrimidine derivatives having both aromatic and halogenic substituents.
METHOD FOR PRODUCING SUBSTITUTED PYRIDIN-2-ONE
-
Paragraph 0117; 0118, (2013/05/21)
The present invention relates to a process for the preparation of substituted 3-(2-hydroxyethyl)-1-[4-nitrophenyl]pyridin-2(1H)-ones which serve as important intermediate compounds for producing drugs.
Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
-
Page/Page column 69, (2013/06/27)
The invention relates to dihydronaphthyridines and related compounds; compositions comprising an effective amount of a dihydronaphthyridine or a related compound; and methods for treating or preventing proliferative diseases comprising the administration of an effective amount of a dihydronaphthyridine or a related compound.
DIHYDRONAPHTHYRIDINES AND RELATED COMPOUNDS USEFUL AS KINASE INHIBITORS FOR THE TREATMENT OF PROLIFERATIVE DISEASES
-
Paragraph 0372, (2014/01/08)
The invention relates to dihydronaphthyridines and related compounds; compositions comprising an effective amount of a dihydronaphthyridine or a related compound; and methods for treating or preventing proliferative diseases comprising the administration of an effective amount of a dihydronaphthyridine or a related compound. The present invention discloses the unexpected utility of compounds that inhibit cKIT kinase across a broad range of c-KIT mutations, including complex occurrences of primary mutations (KIT exon 9 or 11) and secondary KIT mutations (exons 13, 14, 17 and 18) that may arise in individual, refractory GIST patients. Also unexpected is the utility of compounds of the present invention to inhibit the problematic exon 17 D816V c-KIT mutation, for which there is currently no effective therapy.
SUBSTITUTED OXAZOLIDINONES AND THEIR USE
-
, (2010/11/03)
The invention relates to novel substituted oxazolidinones, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of thromboembolic disorders.
SUBSTITUTED OXAZOLIDINONES AND THEIR USE
-
Page/Page column 30-31, (2010/08/07)
The invention relates to novel substituted oxazolidinones, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in parti
SUBSTITUTED OXAZOLIDINONES AND THEIR USE
-
Page/Page column 23, (2010/12/29)
The invention relates to novel substituted oxazolidinones, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases, and to the use thereof for producing medicaments for treatment and/or prophylaxis of diseases
