首页> 外国专利> HETEROCYCLIC COMPOUNDS, USEFUL AS ALLOSTERIC EFFECTORS AT MUSCARINIC RECEPTORS USEFUL AS ALLOSERIC EFFECT IN MUSCARIN SINGLE RECEPTORS

HETEROCYCLIC COMPOUNDS, USEFUL AS ALLOSTERIC EFFECTORS AT MUSCARINIC RECEPTORS USEFUL AS ALLOSERIC EFFECT IN MUSCARIN SINGLE RECEPTORS

机译:杂环化合物,用作肌肉受体上的异位效应物用作麝香单药中异位效应的化合物

摘要

The compounds of formula (I) and their pharmaceutically acceptable salts and esters thereof are allosteric effectors at muscarinic receptors and are useful for the treatment and prevention of diseases associated with muscarinic receptors:;(Wherein Z is a methylene group, a methine group, a formula NH or a formula = N- group, W is a methylene group, a methine group, a sulfur atom or a group represented by the formula S (O) v wherein v is 1 or 2 ) And if W is a group of formula S (O) v then Z is not a group of formula NH; Each Ao represents a double bond to turn a single bond, Y 1, Y 2, Y 3 and Y 4 in at least one is a carboxyl group, a protected carboxyl group, a sulfonamide group, a protected sulfonamide group or a group represented by the formula - (A) pB 1 -T 1 wherein A is an oxygen atom or a sulfur atom, T 1 is a carboxyl group, a thiocarboxy group, a dithiocarboxy group, a protected carboxyl group, a protected thiocarboxy group, a protected dithiocarboxy group, A tetrazolyl group, B1 is a direct bond, an alkylene group which may be substituted, and p is 0 or 1; The groups Y 1 , Y 2 , Y 3 and Y 4 which are not defined hereinbefore may be the same or different and are each a hydrogen atom, a halogen atom, a nitro group, a hydroxyl group, a thiol group, an amino group, An alkylthio group, an alkylsulfinyl group, an alkylsulfonyl group, an aryl group, an aralkyloxy group, an aralkylthio group, Y 1 may together with Y 2 represent a lactone group or a keto group; R a 1 and R 2 are a hydrogen atom, an alkyl group, an alkanoyl group, an aralkyl group, an aralkyl group, an aralkyl group, a carboxyl group, a protected carboxyl group, a sulfonamide group, a protected sulfonamide group, or a group represented by the formula - (O) qB 2 -T 2 group (wherein, T 2 is a carboxyl group, a protected carboxyl group, a sulfonamide group, a protected sulfonamide group, or a tetrazolyl group, B 2 is an alkylene group or an amino group, a protected amino group, hydroxyl group protection and And q is 0 or 1; and R 2 is an alkylene group having at least one substituent selected from a hydrogen atom, The other of R 1 and R 2 is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, an aryl group or an aralkyl group, or the other of R 1 and R 2 is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, An aralkyl group, or R 1 and R 2 together form a group of the formula (Ib '):;Wherein R 10 , R 11 and R 12 are the same or different and each represents a hydrogen atom, a hydroxyl group, a halogen atom, a haloalkyl group, an alkyl group, an alkyl group which may be substituted, an alkoxy group, an alkylthio group, , An alkylsulfonyl group; R 3 is a hydrogen atom or an amino protecting group.
机译:式(I)化合物及其药学上可接受的盐和酯是毒蕈碱受体的变构效应物,可用于治疗和预防与毒蕈碱受体相关的疾病:(其中Z为亚甲基,次甲基,式NH或式= N-,W为亚甲基,次甲基,硫原子或式S(O)v表示的基团v其中v为1或2)并且如果W为式S(O)v则Z不是式NH的基团;每个Ao代表一个双键变成一个单键,Y 1, Y 2, Y 3 和Y 4 至少一个是羧基,被保护的羧基,磺酰胺基,被保护的磺酰胺基或式-(A)pB 1 -T 1 < / Sup>其中A是氧原子或硫原子,T 1 是羧基,硫代羧基,​​二硫代羧基,​​被保护的羧基,被保护的硫代羧基,​​被保护的二硫代羧基,四唑基,B1是直接键,可以被取代的亚烷基,p是0或1;之前未定义的组Y 1 ,Y 2 ,Y 3 和Y 4 可能相同分别为氢原子,卤素原子,硝基,羟基,硫醇基,氨基,烷硫基,烷基亚磺酰基,烷基磺酰基,芳基,芳烷氧基, Y 1 和芳烷基硫基可以与Y 2 一起代表内酯基或酮基。 R a 1 和R 2 是氢原子,烷基,烷酰基,芳烷基,芳烷基,芳烷基,羧基,a保护的羧基,磺酰胺基,保护的磺酰胺基或由式-(O)qB 2 -T 2 基表示的基团(其中,T 2 是羧基,被保护的羧基,磺酰胺基,保护的磺酰胺基或四唑基,B 2 是亚烷基或氨基,被保护的氨基,羟基保护基,且q为0或1;且R 2为具有至少一个选自氢原子的取代基的亚烷基,R 1 和R 2 是氢原子,碳原子数为1-6的烷基,芳基或芳烷基,或R 1 和R 2 是氢原子,碳数为1-6的烷基,芳烷基或R 1 和R 2 一起组成一组式(Ib'):;其中R 10 ,R 11 和R 12 相同或不同,分别表示氢原子,羟基,卤原子,卤代烷基,烷基,可被取代的烷基,烷氧基,烷硫基,烷基磺酰基; R 3 是氢原子或氨基保护基。

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