603306-58-7Relevant academic research and scientific papers
Ruthenium(II)-Catalyzed Highly Chemo- And Regioselective Oxidative C6 Alkenylation of Indole-7-carboxamides
Jadhav, Pankaj P.,Kahar, Nilesh M.,Dawande, Sudam G.
supporting information, p. 8673 - 8677 (2021/11/20)
We disclosed the first efficient method for highly chemo- and regioselective C6 alkenylation of indole-7-carboxamides using inexpensive Ru(II) catalyst through chelation assisted C-H bond activation. Electronically diverse indole-7-carboxamides and alkenes react efficiently to produce a wide range of C6 alkenyl indole derivatives. Further the C6 alkenyl indole-7-carboxamides modified to their derivatives through simple chemical transformations. The observed regioselectivity and kinetics has been evidenced by deuterium incorporation and intermolecular competitive studies. In addition, for mechanistic insights, the intermediates were analyzed by HRMS.
METHODS FOR HAIR FOLLICLE STEM CELL PROLIFERATION
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Paragraph 0431-0433, (2020/05/06)
The present invention relates to compositions of minoxidil and Sonic Hedgehog (Shh) pathway activators and optionally, Wnt agonists and methods of using them to induce self-renewal of hair follicle stem cells, including inducing the hair follicle stem cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into hair follicle epithelial cells.
1,2-DIHYDRO-3H-PYRAZOL-3-ONE COMPOUNDS AND METHODS OF USING SAME
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Paragraph 0341; 0342, (2020/11/27)
The present disclosure relates to 1,2-dihydro-3H-pyrazol-3-one compounds and methods of using them to induce self-renewal of stem/progenitor supporting cells, including inducing the stem/progenitor cells to proliferate while maintaining, in the daughter c
1,2-DIHYDRO-3H-PYRAZOL-3-ONE COMPOUNDS AND METHODS OF USING SAME
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Paragraph 0292, (2019/07/13)
The present disclosure relates to l,2-dihydro-3H-pyrazol-3-one compounds and methods of using them to induce self-renewal of stem/progenitor supporting cells (e.g. cochlear cells), including inducing the stem/progenitor cells to proliferate while maintain
1,5-DIHYDRO-2H-PYRROL-2-ONE COMPOUNDS AND METHODS OF USING SAME
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Paragraph 0333-0335, (2018/08/20)
The present invention relates to 1,5-dihydro-2H-pyrrol-2-one compounds and methods of using them to induce self-renewal of stem/progenitor supporting cells, including inducing the stem/progenitor cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into tissue cells.
1H-PYRROLE-2,5-DIONE COMPOUNDS AND METHODS OF USING THEM TO INDUCE SELF-RENEWAL OF STEM/PROGENITOR SUPPORTING CELLS
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Paragraph 0288; 0289, (2018/07/29)
The present invention relates to 1H-pyrrole-2,5-dione compounds and methods of using them to induce self-renewal of stem/progenitor supporting cells, including inducing the stem/progenitor cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into tissue cells.
METHODS FOR HAIR FOLLICLE STEM CELL PROLIFERATION
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Paragraph 0284; 0334; 0335, (2018/11/10)
The present invention relates to compositions of Sonic Hedgehog (Shh) pathway activators and Wnt agonists and methods of using them to induce self-renewal of hair follicle stem cells, including inducing the hair follicle stem cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into hair follicle epithelial cells.
POTENTIATION OF CANCER CHEMOTHERAPY
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Paragraph 0040, (2015/12/19)
An improved method for treating gastric cancer, ovarian cancer, non-small cell lung cancer, or colorectal cancer in a patient is described, as well as pharmaceutical compositions useful for the method and a process for preparing said compositions.
Discovery of the dual orexin receptor antagonist [(7 R)-4-(5-chloro-1,3- benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2 H -1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia
Cox, Christopher D.,Breslin, Michael J.,Whitman, David B.,Schreier, John D.,McGaughey, Georgia B.,Bogusky, Michael J.,Roecker, Anthony J.,Mercer, Swati P.,Bednar, Rodney A.,Lemaire, Wei,Bruno, Joseph G.,Reiss, Duane R.,Harrell, C. Meacham,Murphy, Kathy L.,Garson, Susan L.,Doran, Scott M.,Prueksaritanont, Thomayant,Anderson, Wayne B.,Tang, Cuyue,Roller, Shane,Cabalu, Tamara D.,Cui, Donghui,Hartman, George D.,Young, Steven D.,Koblan, Ken S.,Winrow, Christopher J.,Renger, John J.,Coleman, Paul J.
supporting information; experimental part, p. 5320 - 5332 (2010/10/20)
Despite increased understanding of the biological basis for sleep control in the brain, few novel mechanisms for the treatment of insomnia have been identified in recent years. One notable exception is inhibition of the excitatory neuropeptides orexins A and B by design of orexin receptor antagonists. Herein, we describe how efforts to understand the origin of poor oral pharmacokinetics in a leading HTS-derived diazepane orexin receptor antagonist led to the identification of compound 10 with a 7-methyl substitution on the diazepane core. Though 10 displayed good potency, improved pharmacokinetics, and excellent in vivo efficacy, it formed reactive metabolites in microsomal incubations. A mechanistic hypothesis coupled with an in vitro assay to assess bioactivation led to replacement of the fluoroquinazoline ring of 10 with a chlorobenzoxazole to provide 3 (MK-4305), a potent dual orexin receptor antagonist that is currently being tested in phase III clinical trials for the treatment of primary insomnia.
HEMATOPOIETIC NEOPLASM CHEMOTHERAPY
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, (2010/11/03)
A method and medicament for treating mixed lineage leukemia; translocated mixed lineage leukemia; translocated mixed lineage leukemia based acute myelogenous leukemia; translocated mixed lineage leukemia based acute lymphoid leukemia; a non-MLL based chronic myeloproliferative disorder, or non-MLL based acute lymphoid leukemia is provided.
