Compounds 4 - 4 - tetrazolil - phenylpiperidine opioid receptors agonists as therapeutic agents useful for treating Pain and Pharmaceutical compositions containing them as active Principle in combination with other therapeutic agents.

摘要

The compound of 4-tetrazolil-4-fenilpiperidine is composed of the effective compound of 4-tetrazolil-4-fenilpiperidine, which is used to treat or prevent pain or diarrhea in animals and stimulate the function of opioid receptor in cells. Item 1: a compound (1a) with formula characteristics or table salt acceptable from the formula, wherein AR1 is CYCLOPROPYLENE C3-8, phenyl, naftirol, antril, styrene or isobutylene (5-7 members),1. Each substance is undesirable or replaced by one or more R2 groups; ar2 is phenyl, nafos, antrilo, styrene or isobutylene (5 to 7 members);1. Each substance is subject to one or more R2; ges-h, L - (CH2) Nr4, - L - (CH2) NR5, - C1-5) co2r4, or - (C1-5) R5; les-c (o) -,-SO2-O-SOR1 es-h, - C (o) NH2, - C (o) NHO, - co2r4, - CHO, - CN, - (C1-4 tar),-C (o) NH (C1-4 tar),-C (o) n (C1-4 tar) 2 or other parts (2) selected from the preparation group;R2 and R3 are halogen, c1-3 tar or (c1-3 tar) that are independent of each other,-NH (c1-3 tar) o-n (c1-3 tar) 2; R4 = - H, c1-10-ch2o (C1-4 tar),-CH2n (C1-4 tar) 2 o-ch2nh (C1-4 tar);R5 = - NH2, - nhso2r4, - C (o) NH2, - C (o) NHO, - so2nh2, - C (o) NH (pitch C1-4),-C (o) n (C1-4 tar) 2,-So2nh (C1-4 tar),-So2n (C1-4 tar) 2, - H, - Oh, - CN, - cycloquilo C3-8, phenyl, naftyl, antrilo, fenantrilo, o-heaterilo (5-7 members),Each group is replaced or not used by one or more R2 groups; integer m = 0 to 4; integer n = 1 to 4; integer P = 0 or 1; integer q = 0 to 3; integer r = 1 to 6. Item 21: a compound (1b) with formulation characteristics,Or a pharmaceutically acceptable salt, wherein AR1 is C3-8 cyclopentanediol, phenyl, naphthalene, antrilo, phenylenediene or isobutylene (5-7 members),1. Each substance is undesirable or replaced by one or more R2 groups; ar2 is phenyl, nafos, antrilo, styrene or isobutylene (5 to 7 members);1. Each substance is subjected to one or more R2; ges-h, L - (CH2) NC (o) R4, L - (CH2) N5, - (C1-5 tar) cour4, or - (C1-5 tar) R5; les-c (o) -,-SO2-O-SOR1 es-h, - C (o) NH2, - C (o) NHO, - co2r4, - CHO, - CN, - (C1-4 tar),-C (o) NH (C1-4 tar),-C (o) n (C1-4 tar) 2 or other parts (2) selected from the preparation group;R2 and R3 are halogen, c1-3 tar or (c1-3 tar) that are independent of each other,-NH (c1-3 tar) o-n (c1-3 tar) 2; R4 = - H, c1-10-ch2o (C1-4 tar),-CH2n (C1-4 tar) 2 o-ch2nh (C1-4 tar);R5 = - NH2, - nhso2r4, - C (o) NH2, - C (o) NHO, - so2nh2, - C (o) NH (pitch C1-4),-C (o) n (C1-4 tar) 2-so2nh (C1-4 tar),-So2n (C1-4 tar) 2, - H, - Oh, - CN, - cycloquilo C3-8, phenyl, naftyl, antrilo, fenantrilo, o-heaterilo (5-7 members),Each group is replaced or not used by one or more R2 groups; integer m = 0 to 4; integer n = 1 to 4; integer P = 0 or 1; integer q = 0 to 3; integer r = 1 to 6. Item 41: a compound with the characteristics of formula (1c) or a salt acceptable to the drug in the formula, wherein Ar3 is phenyl, nafil, antril, styrene or isopropene (5-7 members),1. Each substance is subject to one or more R2, g = - H, - L - (CH2) NC (o), R4, - L - (CH2) N5, - C1-5 tar) cor4, or - (C1-5 tar) R5, les-c (o) -,-SO2-O-SOR1 es-h, - C (o) NH2, - C (o) NHO, - co2r4, - CHO, - CN, - (C1-4 tar),-C (o) NH (C1-4 tar),-C (o) n (C1-4 tar) 2 or other parts (2) selected from the preparation group;R2 and R3 are halogen, c1-3 tar or (c1-3 tar) that are independent of each other,-NH (c1-3 tar) o-n (c1-3 tar) 2; R4 = - H, c1-10-ch2o (C1-4 tar),-CH2n (C1-4 tar) 2 o-ch2nh (C1-4 tar);R5 = - NH2, - nhso2r4, - C (o) NH2, - C (o) NHO, - so2nh2, - C (o) NH (pitch C1-4),-C (o) n (C1-4 tar) 2-so2nh (C1-4 tar),-So2n (C1-4 tar) 2, - H, - Oh, - CN, - cycloquilo C3-8, phenyl, naftyl, antrilo, fenantrilo, o-heaterilo (5-7 members),Each group is replaced or not used by one or more R2 groups; integer m = 0 to 4; integer n = 1 to 4; integer P = 0 or 1; integer q = 0 to 3; integer r = 1 to 6. Item 61: a compound (1D) with formulation characteristics or a pharmaceutically acceptable formulation, wherein Ar3 is phenyl, nanophilic, antril, styrene or isopropene (5-7 members),1. Each substance is subject to one or more R2, g = - H, - L - (CH2) NC (o), R4, - L - (CH2) N5, - C1-5 tar) cor4, or - (C1-5 tar) R5, les-c (o) -,-SO2-O-SOR1 es-h, - C (o) NH2, - C (o) NHO, - co2r4, - CHO, - CN, - (C1-4 tar),-C (o) NH (C1-4 tar),-C (o) n (C1-4 tar) 2 or other parts (2) selected from the preparation group;R2 and R3 are halogen, c1-3 tar or (c1-3 tar) that are independent of each other,-NH (c1-3 tar) o-n (c1-3 tar) 2; R4 = - H, c1-10-ch2o (C1-4 tar),-CH2n (C1-4 tar) 2 o-ch2nh (C1-4 tar);R5 = - NH2, - nhso2r4, - C (o) NH2, - C (o) NHO, - so2nh2, - C (o) NH (pitch C1-4),-C (o) n (C1-4 tar) 2-so2nh (C1-4 tar),-So2n (C1-4 tar) 2, - H, - Oh, - CN, - cycloquilo C3-8, phenyl, naftyl, antrilo, fenantrilo, o-heaterilo (5-7 members),Each group is replaced or not used by one or more R2 groups; integer m = 0 to 4; integer n = 1 to 4; integer P = 0 or 1; integer q = 0 to 3; integer r = 1 to 6. Requirement No. 110: a compound characterized by formula (3) or formula salt. Requirement No. 111: a compound having the characteristics of formula (4) or formula salt.