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    • 5. 发明申请
    • DIAMINO THIAZOLOINDAN DERIVATIVES AND THEIR USE
    • DIAMINO THIAZOLOINDAN DERIVATIVES及其使用
    • WO2005084205A3
    • 2005-10-20
    • PCT/US2005005921
    • 2005-02-25
    • TEVA PHARMATEVA PHARMA
    • STERLING JEFFREYHAYARDENY-NISIMOV LIATLERNER DAVIDHERZIG YAACOVFALB ELIEZERTOTH GYORGYMOLNAR SANDORPINKERT DALIA
    • A61K31/428C07D277/60
    • A61K31/428C07D277/60
    • The subject invention provides a compound having the structure: wherein Y is O, NR3R4 or NOR6; R3 is H, alkyl, aralkyl, alkynyl, trifluoroacetyl, t-butoxycarbonyl or an acyl group; R4 is H, alkyl, aralkyl, or alkynyl; R6 is H or C1-C4 alkyl; R1and R2 are each independently H, alkyl, aralkyl, or alkynyl; the curved line drawn from S to the center of the phenyl ring and the straight line drawn from N to the center of the ring indicate that S and N are part of a 5 membered ring which shares two carbons with the phenyl ring; and the dashed line drawn from the carbon atom on the cyclopentyl ring to Y represents a bond when Y is O or NOR6 and is absent when Y is NR3R4 and wherein wherein X is H or O; and R5 is H, alkyl, trifluoroacetyl, t-butoxycarbonyl or an acyl group, or an enantiomer, or a tautomer, or a pharmaceutically acceptable salt thereof, a process for preparing the compounds and a method of treating Parknison's disease, multiple sclerosis or depression with the compounds of the invention.
    • 本发明提供具有以下结构的化合物:其中Y为O,NR 3 R 4或NOR 6; R3是H,烷基,芳烷基,炔基,三氟乙酰基,叔丁氧羰基或酰基; R4是H,烷基,芳烷基或炔基; R6是H或C1-C4烷基; R 1和R 2各自独立地为H,烷基,芳烷基或炔基; 从S到苯环中心的曲线和从N到环的中心的直线表示S和N是与苯环共享两个碳的5元环的一部分; 在Y为O或NOR6时,从环戊基环上的碳原子取代的虚线表示Y,当Y为NR3R4且X为H或O时,不存在。 R5是H,烷基,三氟乙酰基,叔丁氧基羰基或酰基,或其对映异构体或其互变异构体或其药学上可接受的盐,该化合物的制备方法以及治疗帕金森病,多发性硬化或抑郁症的方法 与本发明的化合物。