On January 6, 2011, Guzzo, Peter R.; Surman, Matthew David; Henderson, Alan John; Jiang, May Xiaowu published a patent.Name: (6-(Trifluoromethyl)pyridin-3-yl)methanol The title of the patent was Preparation of azinone-substituted azapolycycles as MCH-1 receptor antagonists and use in the treatment of diseases. And the patent contained the following:
Title compounds I [R1 = H, (un)substituted alkyl, alkenyl, alkynyl, etc; R2 and R4 independently = H, CONH2 and derivatives, (un)substituted alkyl, aryl, etc.; R2 and R3 or R3 and R4 taken together to form an (un)substituted 3- to 7-membered heterocycle; at least one of R2 and R3 or R3 and R4 taken together to form an (un)substituted 3- to 7-membered heterocycle; each R5 independently = H, halo, NH2 and derivatives, (un)substituted alkyl, aryl, etc.; R6 = H, halo, (un)substituted aryl, heteroaryl, etc.; A = (CH2)m; B = (un)substituted aryl, heteroaryl, cycloalkyl, etc.; D = (CH2)n; L = (CH2)pO, (CH2)p, CH=CH, or bond; X = CR12, C(R12)2, N, or NR12; Y = CR12, C, or N; Z = CH, C, or N; R12 = H, halo, NH2 and derivatives, (un)substituted alkyl, aryl, etc.; m and n = 0 or 1, wherein m + n = 1; p = 1 to 4; q = 0 to 3; dash bond represents an optional double bound], and their pharmaceutically acceptable salts, oxides, solvates, or prodrugs, are prepared and disclosed as MCH-1 receptor antagonists and useful in the treatment of obesity, anxiety, depression, non-alc. fatty liver disease, and psychiatric disorders. Thus, e.g., II·HCl was prepared by acylation of 2-(6-bromo-1-methyl-1H-indol-3-yl)ethanamine with 4-bromobutyryl chloride followed by intramol. cyclization, intramol. reductive N-alkylation, amination with 4-(benzyloxy)pyridin-2(1H)-one, and addition of hydrochloric acid. Select I were evaluated for their MCH-1 antagonistic activity, e.g., II·HCl demonstrated a Ki value of 14.9 nM. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Name: (6-(Trifluoromethyl)pyridin-3-yl)methanol
The Article related to azinone azapolycycle preparation mch receptor antagonist treatment disease, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Name: (6-(Trifluoromethyl)pyridin-3-yl)methanol
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