Guzzo, Peter R. et al. published their patent in 2011 |CAS: 386704-04-7

The Article related to azinone azabicycloalkyl indole preparation mch1 receptor antagonist treatment disease, azabicycloalkyl pyridoindole preparation, 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.Application In Synthesis of (6-(Trifluoromethyl)pyridin-3-yl)methanol

On January 6, 2011, Guzzo, Peter R.; Surman, Matthew David; Zhu, Lei published a patent.Application In Synthesis of (6-(Trifluoromethyl)pyridin-3-yl)methanol The title of the patent was Preparation of azinone-substituted (azabicycloalkyl)indoles and (azabicycloalkyl)pyridoindoles 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, cycloalkyl, heteroaryl, etc; each R2 independently = H, NH2 and derivatives, (un)substituted alkyl, aryl, etc.; R3 = H, halo, (un)substituted aryl, heteroaryl, etc.; A = (CH2)n; B = (un)substituted aryl, heteroaryl, cycloalkyl, etc.; L = (CH2)pO, (CH2)p, CH=CH, or bond; X = CR9, C(R9)2, N, or NR9; Y = CR9, C, or N; Z = CH, C, or N; R9 = H, halo, NH2 and derivatives, (un)substituted alkyl etc.; m = 0 to 3, n = 1 or 2; p = 1 to 4; 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 methylation of 3-bromophenylhydrazine hydrochloride with Me iodide followed by heterocyclization with 1-azabicyclo[3,2,1]octan-4-one, 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 6.4 nM. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Application In Synthesis of (6-(Trifluoromethyl)pyridin-3-yl)methanol

The Article related to azinone azabicycloalkyl indole preparation mch1 receptor antagonist treatment disease, azabicycloalkyl pyridoindole preparation, 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.Application In Synthesis of (6-(Trifluoromethyl)pyridin-3-yl)methanol

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