1017599-17-5Relevant articles and documents
DIARYL KETIMINE DERIVATIVE HAVING ANTAGONISM AGAINST MELANIN-CONCENTRATING HORMONE RECEPTOR
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Page/Page column 23, (2010/12/31)
[Problems] To provide an antagonist of a melanin-concentrating hormone receptor, which is useful as a medicine for a central nervous system disease, a cardiovascular disease or a metabolic disease. [Means for Solving Problems] The antagonist comprises, as an active ingredient, a compound represented by the formula (I) wherein R1a and R1b independently represent a hydrogen atom or a C1-6 alkyl group; R2a, R2b, R3a and R3b independently represent a hydrogen atom, a C1-6 alkyl group, or the like; Y represents H or —OH; Z represents —OR8, or the like; R8 represents a hydrogen atom, a C1-6 alkyl group which may have a substituent, or the like; R9a and R9b independently represent a hydrogen atom, a C1-6 alkyl group, or the like; Ar1 represents an aromatic carbon ring group, or an aromatic heteroring group; Ar2 represents a group produced by removing two hydrogen atoms from an aromatic carbon ring, or the like; and the ring group A represents an unsaturated heteroring group.
Discovery of novel diarylketoxime derivatives as selective and orally active melanin-concentrating hormone 1 receptor antagonists
Suzuki, Takao,Kameda, Minoru,Ando, Makoto,Miyazoe, Hiroshi,Sekino, Etsuko,Ito, Satoru,Masutani, Kouta,Kamijo, Kaori,Takezawa, Akihiro,Moriya, Minoru,Ito, Masahiko,Ito, Junko,Nakase, Kazuho,Matsushita, Hiroko,Ishihara, Akane,Takenaga, Norihiro,Tokita, Shigeru,Kanatani, Akio,Sato, Nagaaki,Fukami, Takehiro
scheme or table, p. 5339 - 5345 (2010/06/16)
Optimization of the lead 2a led to the identification of a novel diarylketoxime class of melanin-concentrating hormone 1 receptor (MCH-1R) antagonists. Our focus was directed toward improvement of hERG activity and metabolic stability. The representative derivative 4b showed potent and dose-dependent body weight reduction in diet-induced obese (DIO) C57BL/6J mice after oral administration. The synthesis and structure-activity relationships of the novel diarylketoxime MCH-1R antagonists are described.
DIARYL KETIMINE DERIVATIVE
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Page/Page column 30-31, (2009/07/17)
Provided is a compound of a formula (I): [wherein R1a and R1b are the same or different, representing a hydrogen atom, etc.; R2a and R2b are the same or different, representing a hydrogen atom, etc., or R2a and R2b, taken together, form -CH2CH2-, R3a and R3b are the same or different, representing a hydrogen atom, etc.; or R3a and R3b, taken together, form - CH2CH2-etc.; Y1 and Y2 represent -C(R)2-, etc.; Z represents OR, NR2, etc.; R represents a hydrogen atom, a C1-6 alkyl group, etc.; Ar1 represents a 6-membered aromatic carbocyclic group, etc.; Ar2 represents a 6-membered aromatic carbocyclic group, etc; A3 represents a 6-membered aromatic carbocyclic group etc.]. The compound is useful as a medicine for central disorders, cardiovascular disorders, metabolic disorders.