New phenothiazine derivative for use in preparing medicine for blood sugar lowering and for treatment of diabetes, nicotine dependence, alcohol dependence, central nervous system disorders, schizophrenia, and Alzheimer's disease

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专利权人:

SANOFI-AVENTIS

发明人:

申请号：

DE200710005045

公开号：

DE102007005045(A1)

申请日:

2007.01.26

申请国别(地区):

德国

年份:

2008

代理人:

摘要：

A phenothiazine derivative is new. A phenothiazine derivative of formula (I) is new. R1 : H, 1-6C alkyl, 0-6C alkylaryl, CO-1-6C alkyl, 2-6C alkyl-COO-0-6C alkyl, or 2-6C alkyl-O-1-6C alkyl; R2, R3 : H, F, Cl, Br, CN, NO 2, 0-6C alkyl-COO-0-6C alkyl, 0-6C alkyl-O-0-6C alkyl, 1-6C alkyl, 0-6C alkyl-CO-1-6C alkyl, 0-6C alkylphenyl, SCF 3, SF 5, or SCH 3; R4, R5 : H, F, Cl, Br, CN, SCN, NO 2, =O, 0-6C alkyl-COO-0-6C alkyl, -CO-COO-0-6C alkyl, 0-6C alkyl-O-0-6C alkyl, 1-6C alkyl, 0-6C alkyl-CO-1-6C alkyl, 0-6C alkyl-CONH-0-6C alkyl, 0-6C alkyl-CON[0-6C alkyl] 2, 0-6C alkyl-NH-0-6C alkyl, 0-6C alkyl-NH-COO-0-6C alkyl, 0-6C alkyl-CON[0-6C alkyl]-O-0-6C alkyl, 0-6C alkyl-N[0-6C alkyl] 2, 0-6C alkylaryl, SF 5, 0-6C alkyl-S(O) x-1-6C alkyl, S(O) x-1-6C alkyl-COO-0-6C alkyl, S(O) x-2-6C alkyl-O-0-6C alkyl, -SO 2-NH-0-6C alkyl, -SO 2-N-[0-6C alkyl] 2, S(O) x-0-6C alkyl-heterocycle, S(O) x-1-6C alkyl-CO-heterocycle, -NH-SO 2-1-6C alkyl, 0-6C alkylcycloalkyl, or 0-6C alkyl-heterocycle; x : 0-2; R6, R7 : H, F, Cl, Br, CN, NO 2, =O, =S, =N-O-0-6C alkyl, 0-6C alkyl-COO-0-6C alkyl, 0-6C alkyl-O-0-6C alkyl, 0-6C alkyl-O-CO-1-6C alkyl, 1-6C alkyl, 0-6C alkyl-CO-1-6C alkyl, 0-6C alkylaryl, SF 5, or S(O) x-1-6C alkyl; Ring A : 5-10-membered heterocyclic ring optionally with another 5-10-membered ring; and Ring B : 4-8-membered cycloalkyl ring, 4-10-membered heterocyclic ring or 6-10-membered cycloaryl. Independent claims are included for: (1) a medicament comprising (I) and further active ingredients; and (2) production of medicine by mixing (I) with carrier and preparing into a form suitable for administration. [Image] - ACTIVITY : Antialcoholic; Neuroprotective; Nootropic; Hypoglycemic; CNS-Gen; Antidiabetic; Antismoking; Neuroleptic. - MECHANISM OF ACTION : Glucokinase activator. 2-(10-Methyl-5,5-dioxo-5,10-dihydro-phenothiaz in-2-yl)-3-(tetrahydro-pyrany-4-yl)-N-thiazol-2-yl-propionamide was tested for activation of human glucokinase in an enzymatic test. Effective concentration at 150% (EC 1 5 0) was 4.2 mu M and fold induction was 2.0.

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