Derivatives Indan - 1 - trees replaced in C2, Process for their Preparation and their use as Drugs, Medicine, Process for the preparation of a Medicine, and use of said derivatives alone or in combination with another active substance, for the preparation of medicaments

摘要

1. The indan-1-ole derivative is replaced in C2 equation (1), which means (a) R1 to R4, h; X is s, so, or SO2; y is (CH2) P, where p can be equal to 0, 1, 2 or 3; R5 is CF3, c12-18, cyclo-4, cyclo-c6-8, which can be converted into fluorine by one to seven hydrogen atoms in tar group; (CH2) r-cor6, may be r = 1-6, may be R6, equivalent to Oh, o-tar C1-6 or NH2; ch2-ch (nhr7) - cor8, may be R7, equivalent to h, C (or) - C1-4 or C (or) C1-4 tar, and may be R8, equivalent to Oh, o-tar C1-6 or NH2; phenyl, 1-o-2-naftio, biphenyl or a heterosexual radical substance,the rings or ring systems may be substituted up to twice with O-C 1-8 alkyl, O-C 3-8 cycloalkyl, O-CO-C 1-8 alkyl, O-CO-C 3-8 cycloalkyl, S (O) 0 -2-C1-8-alkyl, S (O) 0-2-C3-8-cycloalkyl, NH2, NH-C1-8-alkyl, NH-C3-8-cycloalkyl, N [C1-8-alkyl] 2, N [C3-cycloalkyl -8] 2, NH-CO-C2-8-alkyl, NH-CO-C3-8-cycloalkyl, SO3H, SO2-NH2, SO2-NH-C1-8-alkyl, SO2-NH-C3-8-cycloalkyl, NH-SO2 -NH2, NH-SO2-C1-8-alkyl, NH-SO2-C3-8 cycloalkyl, O-CH2-COOH, O-CH2-CO-O-C1-8-alkyl, COOH, CO-O-C1-8-alkyl , CO-O-C3-8cycloalkyl, CO-NH2, CO-NH-C1-8alkyl, CO-N- [C1-8alkyl] 2, C1-8alkyl, C3-8cycloalkyl,In each case, as many as seven hydrogen atoms in the tar group can be replaced by fluorine; F, Cl, Br, I, CN; but excluding the meaning of unsubstituted phenyl, 4-fluoroofenenio, 4-bromophenyl, 4-chlorophenyl, 3-methylphenyl, 4-methylphenyl, 4-methoxyphenyl, 4-n-butylphenyl, 4-t-butylphenyl, 2-amino, 2. C12; or (b) R1, R4, which are independent of each other, are h; F, Cl, Br, I; CN; N3, NO2, oh, o-c1-8, o-cycloquilo (C3-4 and c6-8),O-CH2-phenyl, O-phenyl, O-CO-C1-8-alkyl, O-CO-C3-8-cycloalkyl, S (O) 0-2-C1-8-alkyl, S (O) 0-2-cycloalkyl C3-8, NH2, NH-C1-8-alkyl, NH-C3-8-cycloalkyl, N [C1-8-alkyl] 2, N [C3-8-cycloalkyl] 2, NH-CO-C1-8-alkyl, NH-CO -C3-8cycloalkyl, SO3H, SO2-NH2, SO2-NH-C1-8alkyl, SO2-NH-C3-8cycloalkyl, NH-SO2-NH2, NH-SO2-C1-8alkyl, NH-SO2-cycloalkyl C3-8, O-CH2-COOH, O-CH2-CO-O-C1-8-alkyl, COOH, CO-O-C1-8-alkyl, CO-O-C3-8-cycloalkyl, CO-NH2, CO-NH -C1-8alkyl, CO-N- [C1-8alkyl] 2, C1-8alkyl, C3-8cycloalkyl, C2-8alkenyl, or C2-8alkynyl, being able to be substituted in the alkyl groups,3 - [lil] - 3 - [3] - 3,2-3,2-3 - [3-3-2-3] - 3-3 - [seamless 2 - or 3-folio, 23-or 4-pyridine, 2-4-or 5-oxazolilo, 3-4-or 5-isoxazolilo, 2-4-or 5-thiazole, 34- or 5-isothiazolyl, the aryl or heterocycle radical may be substituted up to twice with F, Cl, Br, CN, OH, C1-4 alkyl, CF3, O-C1-4 alkyl, S (O) 0-2 -C1-6alkyl, NH2, NH-SO2-C1-4alkyl, COOH, CO-O-C1-4alkyl, or CO-NH2 and one to seven hydrogen atoms may be replaced by fluorine in the alkyl groups; R2, R3 independently of one another are H; F, Cl, Br, I; CN; N3, NO2, O-C1-8-alkyl, O-C3-8-cycloalkyl, O-CO-C1-8-alkyl, O-CO-C3-8-cycloalkyl, S (O) 0-2-C1-8-alkyl, S (O) 0-2-C3-8cycloalkyl, NH2, NH-C1-8alkyl, NH-C3-8cycloalkyl, N [C1-8alkyl] 2, N [C3-8cycloalkyl] 2, NH-CO- C1-8alkyl, NH-CO-C3-8cycloalkyl, SO3H, SO2-NH2,SO2-NH-C5-8-alkyl, SO2-NH-C3-8-cycloalkyl, NH-SO2-NH2, NH-SO2-C1-8-alkyl, NH-SO2-C5-8-cycloalkyl, O-CH2-COOH, O- CH2-CO-O-C1-8-alkyl, COOH, CO-O-C1-8-alkyl, CO-O-C3-8-cycloalkyl, CO-NH2, CO-NH-C1-8-alkyl, CO-N [C1-alkyl -8] 2, C1-8-alkyl, C3-8-cycloalkyl, C2-8-alkenyl, C2-8-alkynyl, the alkyl, alkenyl and alkynyl groups being able to be substituted in each case one to seven hydrogen atoms by fluorine; or a hydrogen may be replaced by OH, OC (O) CH3, O-CH2-Ph, NH2, NH-CO-CH3 or N (COOCH2Ph) 2; phenyl, 1- or 2-naphthyl, 5-tetrazolyl, 1- [C1-6alkyl] -5-tetrazolyl, 2- [C1-6alkyl] -5-tetrazolyl, 1-imidazolyl, 1- or 4- [1 2,4] triazolyl,2 Three, two, three, fuliou, two3-or 4-pyridine, 2-4-or 5-oxazolilo, 3-4-or 5-isoxazolilo, 2-4-or 5-thiazole, 34-O 5-isothiocyanides can be replaced by F, Cl, Br, CN, oh, C1-4 tar, CF3, or C1-4, s (o) 0-2-tar C1-6, NH2, nh-so2-c1-4, COOH, co-O C1-4 or co-nh2 for two heterocycles, and one to seven hydrogen atoms can be replaced by fluorine in tar group; O R2 and R3 constitute an o-ch2-o group;At least one of the R1, R2, R3 and R4 type radicals does not contain hydrogen; X is s, so, so or SO2 type; and it is (CH2) P type radical, whose quantity is equivalent to 0, 1, 2 or 3; R5 is c1-18 asphalt, or cyclomequillo (C3-4 and c6-8),in the alkyl groups, one to seven hydrogen atoms may be replaced by fluorine; (CH2) r-COR6, where r = 1-6 can be and R6 can be equal to OH, O-C1-6 alkyl or NH2; CH2-CH (NHR7) -COR8, R7 being equal to H, C (O) -C1-6 alkyl or C (O) O-C1-6 alkyl and R8 being equal to OH, O-C1-6 alkyl or NH2; phenyl, 1- or 2-naphthyl, biphenyl or a heterocyclic radical, the rings or ring systems may be substituted up to twice with O-C 1-8 alkyl, O-C 3-8 cycloalkyl, O-CO-C 1-8 alkyl , O-CO-C3-8 cycloalkyl, S (O) 0-2-C1-8-alkyl, S (O) 0-2-C3-8-cycloalkyl, NH2, NH-C1-8-alkyl, NH-C3-cycloalkyl 8, N [C1-8 alkyl] 2, N [C3-8 cycloalkyl] 2,Or or or or or or or or or or or or or or or or or or or or or or or or or or or or or or or or or or or or or or or or or or or lo C3-8, co-nh2, co-nh-tar c1-8, Co-N [c1-8 tar] 2, c1-8 tar, cycloquinolo C3-8, may already exist In each case, up to seven hydrogen atoms are replaced by fluorine in each group of aspha F, Cl, Br, I or CN and their physiologically compatible salts; their preparation and procedures for use as drugs, drugs and drugs;Use of these derivatives or in combination with other active substances for the prevention or treatment of obesity and type II diabetes.