121404-83-9Relevant academic research and scientific papers
RET INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
-
Paragraph 00298, (2020/07/06)
Provided herein are a RET inhibitor, a pharmaceutical composition thereof and uses thereof. In particular, provided is a compound having Formula (I) or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof. Provided is a pharmaceutical composition comprising the compound, and uses of the compound and pharmaceutical composition thereof for the preparation of a medicament, in particular for treatment and prevention of RET-related diseases and conditions, including cancer, irritable bowel syndrome, and/or pain associated with irritable bowel syndrome.
IRAK4 INHIBITORS AND USES THEREOF
-
Paragraph 0128, (2019/05/22)
Compounds of Formula I as IRAK4 inhibitors are disclosed. The pharmaceutical compositions comprising compounds of formula I, methods of synthesis of these compounds, methods of treatment for diseases associated with IRAK-4 such as inflammatory diseases an
Bicyclic-Fused Heteroaryl or Aryl Compounds
-
Paragraph 0381, (2015/10/28)
Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
Modular C-H Functionalization Cascade of Aryl Iodides
Shi, Hang,Babinski, David J.,Ritter, Tobias
supporting information, p. 3775 - 3778 (2015/04/14)
We report the first example of ipso-borylation for the modular 1,2-bisfunctionalization of aryl iodides via C-H functionalization. The carbon-boron bond is used as a lynchpin to access ipso carbon-carbon, carbon-nitrogen, carbon-oxygen, and carbon-halogen (Cl, Br, I) bonds. The utility of our methodology is illustrated through quick, modular syntheses of the pharmaceuticals Abilify and Flunixin.
Mild and selective organocatalytic iodination of activated aromatic compounds
Jakab, Gergely,Hosseini, Abolfazl,Hausmann, Heike,Schreiner, Peter R.
supporting information, p. 1635 - 1640 (2013/07/27)
We describe an organocatalytic iodination of activated aromatic compounds using 1,3-diiodo-5,5-dimethylhydantoin (DIH) as the iodine source with thiourea catalysts in acetonitrile. The protocol is applicable to a number of aromatic substrates with significantly different steric and electronic properties. The iodination is generally highly regioselective and provides high yields of isolated products. NMR kinetic investigations conducted in THF-d 8indicate the role of sulfur in the thiourea motif as a nucleophile that is assisted by H-bonding in the key steps of the reaction. Georg Thieme Verlag Stuttgart . New York.
Synthesis and preliminary evaluation of curcumin analogues as cytotoxic agents
Zhang, Qin,Zhong, Ying,Yan, Lin-Na,Sun, Xun,Gong, Tao,Zhang, Zhi-Rong
scheme or table, p. 1010 - 1014 (2011/03/21)
A series of curcumin analogues with different substituents at the 4-position of the phenyl group were synthesized and screened for in vitro cytotoxicity against a panel of human cancer cell lines. Several novel curcumin analogues, especially 32 and 34, exhibited selective and potent cytotoxic activity against human epidermoid carcinoma cell line A-431 and human glioblastoma cell line U-251, implying their specific potential in the chemoprevention and chemotherapy of skin cancer and glioma. The preliminary SAR information extracted from the results suggested that introduction of appropriate substituents to the 4′-positions could be a promising approach for the development of new cytotoxic curcumin analogues with special selectivity for A-431 and U-251 cell lines.
Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties
Oost, Thorsten,Backfisch, Gisela,Bhowmik, Swati,Van Gaalen, Marcel M.,Geneste, Herve,Hornberger, Wilfried,Lubisch, Wilfried,Netz, Astrid,Unger, Liliane,Wernet, Wolfgang
scheme or table, p. 3828 - 3831 (2011/08/02)
Herein we report the discovery of a novel series of vasopressin 1b (V1b) receptor antagonists, starting from potent but metabolically labile oxindole SSR149415. Masking the proline N,N-dimethyl amide moiety as an oxazole and attaching a benzylic amine moiety to the northern phenyl ring resulted in potent and selective V1b receptor antagonists with improved metabolic stability and improved pharmacokinetic properties in rat. Compound 18c was found to be efficacious in a rat model of anti-depressant activity.
GAMMA SECRETASE MODULATORS
-
Page/Page column 362, (2010/06/15)
In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
Syntheses of macrocyclic bis(bibenzyl) compounds derived from perrottetin e
Speicher, Andreas,Groh, Matthias,Hennrich, Markus,Huynh, Anh-Minh
experimental part, p. 6760 - 6778 (2011/03/18)
Macrocyclic bis(bibenzyl) compounds are natural products from liverworts and are of growing interest due to recent reports on new isolated compounds and on their remarkable biological activities. We report here on a flexible and general approach to the to
GAMMA SECRETASE MODULATORS
-
Page/Page column 140-141, (2010/06/15)
In its many embodiments, the present invention provides a novel class of heterocyclic compounds of Group A or Group, as defined herein, as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions
