COMPOUNDS AND PHARMACEUTICAL COMPOSITION POSSESSING PROPERTY FOR GROWTH HORMONE RELEASING, METHOD FOR STIMULATION OF SECRETION OF GROWTH HORMONE FROM MAMMAL HYPOPHYSIS Russian patent published in 2007 - IPC C07C237/22 C07K14/60 C07K5/06 A61K38/25 A61P5/02 

FIELD: organic chemistry, medicine, endocrinology, pharmacy.

SUBSTANCE: invention relates to novel compounds of the formula (I): or their pharmaceutically acceptable salts and composition containing thereof that possess activity with respect to release of growth hormone. In the formula (I) R¹ represents hydrogen atom or (C₁-C₆)-alkyl; R² represents hydrogen atom or (C₁-C₆)-alkyl; L represents compound of the formula: wherein R⁴ represents hydrogen atom or (C₁-C₆)-alkyl; p = 0 or 1; r = 1; q, s, t and u = 0, 1, 2, 3 or 4 being independently of one another; the sum q + r + s + t + u = 0, 1, 2, 3 or 4; R⁹, R¹⁰, R¹¹ and R¹² represent independently of one another hydrogen atom or (C₁-C₆)-alkyl; Q represents >N-R¹² wherein R¹³ represents hydrogen atom or (C₁-C₆); or L represents compound of the formula: , wherein r = 0 or 1; q, s, t and u independently of one another = 0, 1, 2, 3 or 4; the sum q + r + s + t + u = 0, 1, 2, 3 or 4; R⁹, R¹⁰, R¹¹ and R¹² represent independently of one another hydrogen atom or (C₁-C₆)-alkyl; Q represents >N-R¹³ or compound of the formula: , wherein o = 0, 1 or 2; T represents -N(R¹⁵)(R¹⁶) or hydroxyl; R¹³, R¹⁵ and R¹⁶ represent independently of one another hydrogen atom or (C₁-C₆); R¹⁴ represents hydrogen atom; G represents compounds of the formula or wherein R¹⁷, R¹⁸, R¹⁹, R²⁰ and R²¹ represent independently of one another hydrogen atom or aryl; J represents compounds of the formula or wherein R²², R²³, R²⁴, R²⁵ and R²⁶ represent independently of one another hydrogen or halogen atom; a = 0, 1 or 2; b = 0, 1 or 2; c = 0, 1 or 2; d = 0 or 1; e = 0, 1, 2 or 3; f = 0 or 1; R⁵ represents hydrogen atom; R⁶ and R⁷ represent independently of one another hydrogen atom or (C₁-C₆)-alkyl; or R⁶ and R⁷ can form -(CH₂)_i-U-(CH₂)_j- optionally wherein i and j = 1, 2 or 3 independently one another, and U represent a valence bond; R⁸ represents hydrogen atom or (C₁-C₆)-alkyl; M represents arylene or -CR²⁷=CR²⁸- wherein R²⁷ and R²⁸ represent independently one another hydrogen atom or (C₁-C₆)-alkyl. Also, invention relates to a pharmaceutical composition comprising compounds of the formula (I) or its pharmaceutically acceptable salt as an active component in common with a pharmaceutically acceptable carrier or excipient. Also, invention relates to a method for stimulation of growth hormone secretion from mammalian hypophysis that involves administration to mammal the effective dose of compound or its pharmaceutically acceptable salt. Invention provides synthesis of novel compounds and their composition containing thereof that can be used in treatment of diseases associated with the growth hormone deficiency.

EFFECT: improve stimulating method, valuable medicinal properties of compounds and pharmaceutical composition.

13 cl, 29 ex