126370-67-0Relevant academic research and scientific papers
NEW BENZAMIDE DERIVATIVES AS PPAR-GAMMA MODULATORS
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Paragraph 0097-0098; 0102-0103, (2019/06/27)
The present invention relates to novel benzamides derivatives of formula (I) as modulators of PPAR-gamma receptor, to processes for their preparation, to pharmaceutical compositions comprising said compounds and to said compound for use in the treatment of pathological conditions, disorders or diseases that can improve by modulation of PPAR-gamma receptor, such as cancer; metabolic diseases, inflammatory diseases, respiratory disorders, autoimmune diseases, neurodegenerative diseases, cardiovascular diseases and renal diseases.
METHODS OF USING INDAZOLE-3-CARBOXAMIDES AND THEIR USE AS WNT/B-CATENIN SIGNALING PATHWAY INHIBITORS
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Paragraph 0303; 0305; 0320; 0322; 0326; 0328, (2018/05/16)
This disclosure features the use of one or more indazole-3-carboxamide compounds or salts or analogs thereof, in the treatment of one or more diseases or conditions independently selected from the group consisting of a tendinopathy, dermatitis, psoriasis, morphea, ichthyosis, Raynaud's syndrome, and Darier's disease; and/or for promoting wound healing. The methods include administering to a subject (e.g., a subject in need thereof) a therapeutically effective amount of one or more indazole-3-carboxamide compounds or salts or analogs thereof as described anywhere herein.
Pd-Catalyzed Suzuki coupling reactions of aryl halides containing basic nitrogen centers with arylboronic acids in water in the absence of added base
Li, Zhao,Gelbaum, Carol,Campbell, Zachary S.,Gould, Paul C.,Fisk, Jason S.,Holden, Bruce,Jaganathan, Arvind,Whiteker, Gregory T.,Pollet, Pamela,Liotta, Charles L.
supporting information, p. 15420 - 15432 (2017/12/15)
The Pd-catalyzed Suzuki coupling reactions of a series of aryl chlorides and aryl bromides containing basic nitrogen centers with arylboronic acids in water in the absence of added base are reported. The reactions proceed either partially or entirely under acidic conditions. After surveying twenty-two phosphorus ligands, high yields of products were obtained with aryl chlorides only when a bulky ligand, 2-(di-tert-butyl-phosphino)-1-phenyl-1H-pyrrole (cataCXiumPtB) was used. In contrast, aryl bromides produced high yields of products in the absence of both added base and added ligand. In order to explore the Suzuki coupling process entirely under acidic conditions, a series of reactions were conducted in buffered acidic media using several model substrates. 4-Chlorobenzylamine, in the presence of cataCXiumPtB, produced high yields of product at buffered pH 6.0; the yields dropped off precipitously at buffered pH 5.0 and lower. The fall-off in yield was attributed to the decomposition of the Pd-ligand complex due to the protonation of the ligand in the more acidic aqueous media. In contrast, in the absence of an added ligand, 4-amino-2-chloropyridine produced quantitative yields at buffered pH 3.5 and 4.5 while 4-amino-2-bromopyridine produced quantitative yields in a series of buffered media ranging from pH 4.5 to 1.5. These substrates are only partially protonated in acidic media and can behave as active Pd ligands in the Suzuki catalytic cycle.
A novel graphene-supported palladium catalyst for suzuki-miyaura coupling of less reactive heteroaryl halides in water
Taher, Abu,Lee, Dong-Jin,Lee, Ik-Mo,Rahman, Md. Lutfor,Sarker, Md Shaheen
, p. 1478 - 1485 (2016/10/11)
An efficient reduced graphene oxide-supported heterogenized palladium complex with pyrene-tagged ketoiminato ligand has been developed and used for cross-coupling of less reactive heteroaryl halides in water. Desirable catalytic activity was observed with high (up to 98%) conversion of the less reactive reactants under relatively mild conditions. The efficiency and green nature of the catalyst were confirmed without significant loss of activity.
POPd/TBAB co-catalyzed Suzuki cross-coupling reaction of heteroaryl chlorides/bromides with 4-fluorophenylboronic acid in water
Li, Ben,Zhang, Zhiqiang
, p. 637 - 644 (2016/02/19)
An organic solvent free and efficient heterogeneous synthesis for bridging heteroaryl halides and 4-fluorophenylboronic acid was studied in aqueous media according to the Suzuki cross-coupling protocol. High yields of heteroaryl-aryl fluorides were successfully obtained with: chloro-/bromo-substituted pyridine, thiophene, indole, and inzole in neat water using palladium phosphinous acid complexes (POPd)/tetrabutylammonium bromide (TBAB) as co-catalysts. A possible mechanism for the heterogeneous coupling reaction is proposed and discussed according to the function of the TBAB interphases. The notable properties of the reported method are highly co-catalytic activity, hetero-atom tolerance, simple separating procedure and little environmental disposal impact.
5-SUBSTITUTED INDAZOLE-3-CARBOXAMIDES AND PREPARATION AND USE THEREOF
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Paragraph 1279; 1281; 1314; 1316, (2015/11/09)
Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, fibrotic disorders, cartilage (chondral) defects, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, and neurological conditions/disorders/diseases linked to overexpression of DYRK1A.
Structure-activity relationship study of E6 as a novel necroptosis inducer
Mou, Jianfeng,Park, Ann,Cai, Yu,Yuan, Junying,Yuan, Chengye
supporting information, p. 3057 - 3061 (2015/06/22)
Necroptosis inducers represent a promising potential treatment for drug-resistant cancer. We herein describe the structure modification of E6, which was identified recently as a potent and selective necroptosis inducer. The studies described herein demonstrate for the first time that functionalized biphenyl derivatives possess necroptosis inducer activity. Furthermore, these studies have led to the identification of two promising compounds (5h and 5j) that can be used for further optimization studies as well as mechanism of action investigations.
NAPHTHALENE DERIVATIVE
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Paragraph 0179, (2013/06/27)
The present invention provides compounds which can regulate VCP activity. The present invention provides the compound of formula (I) (R is as defined in the description) or oxides, esters, prodrugs, pharmaceutically acceptable salts or solvates thereof. The compounds can regulate VCP activity, and thus are useful for treating VCP-mediated diseases such as neurodegenerative diseases.
AGENT FOR TREATMENT OF EYE DISEASES
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Paragraph 0081, (2013/08/15)
The present invention provides agents effective to treat eye diseases, pharmaceutical compositions comprising them, methods for preparing pharmaceuticals for treatment of eye diseases comprising using the agents, use of the agents in manufacture of pharma
Ortho-(Dimesitylboryl)phenylphosphines: Positive boryl effect in the palladium-catalyzed suzuki-miyaura coupling of 2-chloropyridines
Malacea, Raluca,Chahdoura, Faouzi,Devillard, Marc,Saffon, Nathalie,Gomez, Montserrat,Bourissou, Didier
, p. 2274 - 2284 (2013/10/01)
Catalytic systems combining ortho-(dimesitylboryl) phenylphosphines and palladium precursors have been evaluated in the Suzuki-Miyaura couplings of chloro-N-heterocycles, in particular 2-chloro pyridines, with arylboronic acids. The Lewis basic character of the substrates does not interfere with the Lewis acidic site of the ligands, even for a substrate featuring free NH2 groups. The influence of several reaction parameters has been studied and the ortho-dimesitylboryl moiety was actually found to substantially enhance the catalytic performance. The role of this group has been examined using preformed phosphine-borane/Pd complexes and the formation of an original phosphine/h4-boratabutadiene complex has been identified as a possible deactivation pathway. Regioselective coupling of 2,6-dichloro-3-nitropyridine with phosphine-borane/Pd catalysts has also been explored, and sequential double cross-couplings were found to give a direct and efficient access to unsymmetrical 2,6-diarylpyridines.
