885950-46-9Relevant articles and documents
Imidazole-containing condensed tricyclic compound and application thereof
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Paragraph 0222, (2018/03/01)
The invention discloses an imidazole-containing condensed tricyclic compound adopting the structure as shown in the formula (I) or pharmaceutically acceptable salts, stereisomers or prodrug molecules thereof. The imidazole-containing condensed tricyclic compound has the IDO1 activity regulation function, can enhance T-cell activation through blocking immune checkpoints IDO1, is used for treating IDO1-mediated immunosuppression, and therefore, can become an effective medicine for treating malignant tumors. When used together with checkpoint protein anti-body drugs or other anti-cancer drugs, the imidazole-containing condensed tricyclic compound can enhance the anti-cancer effect. Meanwhile, the imidazole-containing condensed tricyclic compound has the potential of effectively treating IDO1 abnormity related immunosuppressive diseases and has a high application value.
Development of a safe and economical synthesis of methyl 6-chloro-5-(trifluoromethyl)nicotinate: Trifluoromethylation on kilogram scale
Mulder, Jason A.,Frutos, Rogelio P.,Patel, Nitinchandra D.,Qu, Bo,Sun, Xiufeng,Tampone, Thomas G.,Gao, Joe,Sarvestani, Max,Eriksson, Magnus C.,Haddad, Nizar,Shen, Sherry,Song, Jinhua J.,Senanayake, Chris H.
, p. 940 - 945 (2013/07/26)
Reported herein is a safe and economical synthesis of methyl 6-chloro-5-(trifluoromethyl)nicotinate, an intermediate in the synthesis of novel anti-infective agents. The key to this process is the trifluoromethylation of an aryl iodide using an inexpensive methyl chlorodifluoroacetate (MCDFA)/KF/CuI system, with an emphasis on the development work which led to this effective process.
PROCESS FOR THE PREPARATION OF NICOTINAMIDE DERIVATIVES
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Page/Page column 12-13, (2012/05/05)
The present invention relates to a process for the preparation of nicotinamide derivatives of the formula (I) R1 to R7 are as defined in the and to pharmaceutically acceptable salts thereof. The compounds of formula (I) are useful for the treatment and / or prophylaxis of diseases which are associated with the modulation of cannabinoid 1 receptors (CB 1 receptors) as described in the PCT Publ. WO 2006/106054.
PROCESS FOR THE PREPARATION OF NICOTINAMIDE DERIVATIVES
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Page/Page column 6, (2012/05/04)
The present invention relates to a process for the preparation of nicotinamide derivatives of formula I, wherein R1 to R7 are as defined above and to pharmaceutically acceptable salts thereof. The compounds of formula I are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of cannabinoid 1 receptors (CB1 receptors) as described in the PCT Publ. WO 2006/106054.
Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5- carboxamide, an agonist of the α7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: Synthesis and structure-activity relationship
Wishka, Donn G.,Walker, Daniel P.,Yates, Karen M.,Reitz, Steven C.,Jia, Shaojuan,Myers, Jason K.,Olson, Kirk L.,Jacobsen, E. Jon,Wolfe, Mark L.,Groppi, Vincent E.,Hanchar, Alexander J.,Thornburgh, Bruce A.,Cortes-Burgos, Luz A.,Wong, Erik H. F.,Staton, Brian A.,Raub, Thomas J.,Higdon, Nicole R.,Wall, Theron M.,Hurst, Raymond S.,Walters, Rodney R.,Hoffmann, William E.,Hajos, Mihaly,Franklin, Stanley,Carey, Galen,Gold, Lisa H.,Cook, Karen K.,Sands, Steven B.,Zhao, Sabrina X.,Soglia, John R.,Kalgutkar, Amit S.,Arneric, Stephen P.,Rogers, Bruce N.
, p. 4425 - 4436 (2007/10/03)
N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide (14, PHA-543,613), a novel agonist of the α7 neuronal nicotinic acetylcholine receptor (α7 nAChR), has been identified as a potential treatment of cognitive deficits in schizophrenia. Compound 14 is a potent and selective a7 nAChR agonist with an excellent in vitro profile. The compound is characterized by rapid brain penetration and high oral bioavailability in rat and demonstrates in vivo efficacy in auditory sensory gating and, in an in vivo model to assess cognitive performance, novel object recognition.