Patent RU-2298547-C2 (RU)
Title: Compounds and pharmaceutical composition possessing property for growth hormone releasing, method for stimulation of secretion of growth hormone from mammal hypophysis
Inventor: PESHKE BERND
IPC: C07K5/06
Filed: 1999-06-29
Granted: 2007-05-10
Abstract: 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) R 1  represents hydrogen atom or (C 1 -C 6 )-alkyl; R 2  represents hydrogen atom or (C 1 -C 6 )-alkyl; L represents compound of the formula:   wherein R 4  represents hydrogen atom or (C 1 -C 6 )-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; R 9 , R 10 , R 11  and R 12  represent independently of one another hydrogen atom or (C 1 -C 6 )-alkyl; Q represents >N-R 12  wherein R 13  represents hydrogen atom or (C 1 -C 6 ); 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; R 9 , R 10 , R 11  and R 12  represent independently of one another hydrogen atom or (C 1 -C 6 )-alkyl; Q represents >N-R 13  or compound of the formula:  , wherein o = 0, 1 or 2; T represents -N(R 15 )(R 16 ) or hydroxyl; R 13 , R 15  and R 16  represent independently of one another hydrogen atom or (C 1 -C 6 ); R 14  represents hydrogen atom; G represents compounds of the formula   or   wherein R 17 , R 18 , R 19 , R 20  and R 21  represent independently of one another hydrogen atom or aryl; J represents compounds of the formula   or   wherein R 22 , R 23 , R 24 , R 25  and R 26  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; R 5  represents hydrogen atom; R 6  and R 7  represent independently of one another hydrogen atom or (C 1 -C 6 )-alkyl; or R 6  and R 7  can form -(CH 2 ) i -U-(CH 2 ) j - optionally wherein i and j = 1, 2 or 3 independently one another, and U represent a valence bond; R 8  represents hydrogen atom or (C 1 -C 6 )-alkyl; M represents arylene or -CR 27 =CR 28 - wherein R 27  and R 28  represent independently one another hydrogen atom or (C 1 -C 6 )-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