79538-29-7Relevant academic research and scientific papers
PROCESSES AND INTERMEDIATE FOR THE LARGE-SCALE PREPARATION OF 2,4,6-TRIFLUORO-N-[6-(1-METHYL-PIPERIDINE-4-CARBONYL)-PYRIDIN-2-YL]-BENZAMIDE HEMISUCCINATE, AND PREPARATION OF 2,4,6-TRIFLUORO-N-[6-(1-METHYL-PIPERIDINE-4-CARBONYL)-PYRIDIN-2-YL]-BENZAMIDE ACE
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Page/Page column 35-37, (2021/01/29)
The embodiments of present invention provide processes and an intermediate for the large-scale preparation of 2,4,6-trifluoro-N-[6-(1-methylpiperidine-4-carbonyl)-2-pyridyl]benzamide hemisuccinate, and formulations and product forms made by these processe
Synthesis, structural characterization and antimycobacterial evaluation of several halogenated non-nitro benzothiazinones
Madikizela, Balungile,Eckhardt, Tamira,Goddard, Richard,Richter, Adrian,Lins, Anika,Lehmann, Christoph,Imming, Peter,Seidel, Rüdiger W.
, p. 1523 - 1533 (2021/06/14)
8-Nitro-1,3-benzothiazin-4-ones (BTZs), with BTZ043 and PBTZ169 as the most advanced compounds, represent a new class of potent antitubercular agents, which irreversibly inhibit decaprenylphosphoryl-β-d-ribose-2′-epimerase (DprE1), an enzyme crucial for c
PROCESS FOR PREPARATION OF LASMIDITAN
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Paragraph 0098, (2021/08/06)
The present invention relates to a process for the preparation of lasmiditan, a compound of formula I, or pharmaceutically acceptable salts thereof, the process comprising reacting a compound of formula IV with morpholine to obtain a compound of formula II, reacting the of formula III with a compound of formula IIA to obtain lasmiditan or salt thereof.
PROCESS FOR PREPARATION OF LASMIDITAN
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Paragraph 0164; 0167; 0172, (2020/06/01)
The present invention relates to a process for the preparation of lasmiditan, a compound of formula I, or pharmaceutically acceptable salts thereof, the process comprising reacting a compound of formula IX with N-methoxymethylamine or salt thereof to obtain a compound of formula VII; reacting the compound of formula VII with a compound of formula XIV to obtain lasmiditan or salts thereof.
COMBINATION THERAPY WITH 2,3-DIHYDRO-ISOINDOLE-1-ONE COMPOUNDS AND METHODS FOR TREATING PATIENTS WITH VARIOUS MUTATIONS
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Paragraph 00292, (2020/06/19)
The present disclosure comprises a method for administering 2,3-dihydro-isoindole-1-one compound or a pharmaceutically acceptable salt, ester, solvate and/or prodrug thereof, alone or in combination with an anticancer agent, for the treatment of hematolog
Synthesis, structure-activity relationship and in vitro pharmacodynamics of A-ring modified caged xanthones in a preclinical model of inflammatory breast cancer
Chantarasriwong, Oraphin,Milcarek, Andrew T.,Morales, Theodore Habarth,Settle, Aspen L.,Rezende, Celso O.,Althufairi, Bashayer D.,Theodoraki, Maria A.,Alpaugh, Mary L.,Theodorakis, Emmanuel A.
supporting information, p. 405 - 413 (2019/03/05)
Inflammatory breast cancer (IBC) is a highly metastatic, lethal form of breast cancer that lacks targeted therapeutic strategies. Inspired by the promising cytotoxicity of gambogic acid and related caged xanthones in spheroidsMARY-X, an in vitr
Design, synthesis and biological study of potent and covalent HER-2 tyrosine kinase inhibitors with low cytotoxicity in vitro
Jin, Shuyu,Sun, Xiuyun,Liu, Dan,Xie, Hua,Rao, Yu
, p. 1333 - 1345 (2019/05/06)
The discovery and development of a novel HER-2 tyrosine kinase inhibitor for the treatment of HER2-positive breast cancer are presented in this article. EGFR family has been recognized as a crucial meditator in the cancer progression; HER-2 tyrosine kinase was one of the members among them. In the effort to explore potent HER-2 inhibitors, a novel series of 4-anilino-3-cyanoquinoline derivatives have been designed, synthesized and evaluated. Most compounds possessed modest proliferation inhibition on SK-BR-3 cell line and HER-2 kinase. Compound 16 appeared to be the most potent compound (HER-2 kinase IC50: 19.4?nM, SK-BR-3 IC50: 94?nM). In the experiment of cellular cytotoxicity assay, compound 16 shows a much lower cytotoxicity than neratinib on Beas-2b cell line (Human bronchial epithelial cells). In conclusion, compound 16 would be a promising lead compound for further anti-breast cancer drug discovery.
INHIBITORS OF BRUTON'S TYROSINE KINASE
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Page/Page column 27; 58, (2014/06/23)
This application discloses the Btk inhibitor compounds 6-tert-Butyl-8-fluoro-2-{3- hydroxymethyl-4-[1-methyl-5-(1'-methyl-1',2',3',4',5',6'-hexahydro-[3,4']bipyridinyl-6-ylamino)- 6-oxo-1,6-dihydro-pyridazin-3-yl]-pyridin-2-yl}-2H-phthalazin-1-one, 2-(2-{3-[5-(5-Azetidin-1- ylmethyl-1-methyl-1H-pyrazol-3-ylamino)-1-methyl-6-oxo-1,6-dihydro-pyridazin-3-yl]-2- hydroxymethyl-phenyl}-8-fluoro-1-oxo-1,2-dihydro-isoquinolin-6-yl)-2-methyl-propionitrile, and 6-tert-Butyl-2-[2-hydroxymethyl-3-(5-{5-[(2-methoxy-ethylamino)-methyl]-pyridin-2- ylamino}-6-oxo-1,6-dihydro-pyridin-3-yl)-phenyl]-3,4-dihydro-2H-isoquinolin-1-one, formulations thereof, and methods of treatment of asthma, as described herein.
Inhibitors of Bruton's Tyrosine Kinase
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Page/Page column 73, (2012/03/08)
This application discloses 6-(2-Hydroxymethyl-phenyl)-2-methyl-2H-pyridazin-3-one derivatives according to generic Formula I: wherein, variables X, R, and Y4, are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation, such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
P38 KINASE INHIBITING AGENTS
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Page/Page column 31, (2010/11/18)
Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: Formula (I); are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of asthma, COPD, ARDS, rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.
