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1. 发明申请

US20040067950A1 High affinity ligands for nociceptin receptor ORL-1 审中-公开
标题翻译：伤害感受器受体ORL-1的高亲和力配体
公开(公告)号：US20040067950A1
公开(公告)日：2004-04-08
申请号：US10464580
申请日：2003-06-17
申请人： Schering-Plough Corporation
发明人： Deen Tulshian , Ginny D. Ho , Lisa S. Silverman , Julius J. Matasi , Robbie L. McLeod , John A. Hey , Richard W. Chapman , Ana Bercovici , Francis M. Cuss
IPC分类号： A61K031/517 , A61K031/498 , A61K031/4439 , C07D43/02
CPC分类号： A61K31/4535 , A61K31/00 , A61K31/438 , A61K31/439 , A61K31/451 , A61K31/454 , A61K45/06
摘要： The present invention relates to the method of treating cough with ORL-1 agonists, alone or in combination with additional agents for treating symptoms of cough, allergy or asthma, pharmaceutical compositions comprising the combinations, and to compounds of the formula 1 or a pharmaceutically acceptable salt or solvate thereof, wherein: the dotted line represents an optional double bond; X1 is optionally substituted alkyl, cycloalkyl, aryl, heteroaryl or heterocycloalkyl; X2 is nullCHO, nullCN, optionally substituted amino, alkyl, or aryl; or X1 is optionally substituted benzofused heterocyclyl and X2 is hydrogen; or X1 and X2 together form an optionally benzofused spiro heterocyclyl group R1, R2, R3 and R4 are independently H and alkyl, or (R1 and R4) or (R2 and R3) or (R1 and R3) or (R2 and R4) together can form an alkylene bridge of 1 to 3 carbon atoms; Z1 is optionally substituted alkyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl, or nullCO2(alkyl or substituted amino) or CN ; Z2 is H or Z1; Z3 is H or alkyl; or Z1, Z2 and Z3, together with the carbon to which they are attached, form bicyclic saturated or unsaturated rings; pharmaceutical compositions therefore, and the use of said compounds as nociceptin receptor inhibitors useful in the treatment of pain, anxiety, cough, asthma, depression and alcohol abuse.
摘要翻译：本发明涉及用ORL-1激动剂治疗咳嗽的方法，其单独或与另外用于治疗咳嗽，过敏或哮喘症状的药物组合，包含该组合的药物组合物，以及下式的化合物或其药学上可接受的盐或其溶剂合物，其中：虚线表示任选的双键; X 1是任选取代的烷基，环烷基，芳基，杂芳基或杂环烷基; X 2是-CHO，-CN，任选取代的氨基，烷基或芳基; 或X 1是任选取代的苯并稠合的杂环基，X 2是氢; 或X 1和X 2一起形成任选的苯并稠合的螺杂环基R 1，R 2，R 3和R 4独立地为H和烷基，或（R 1和 R 4）或（R 2和R 3）或（R 1和R 3）或（R 2和R 4）可以形成1至 3个碳原子; Z 1是任选取代的烷基，芳基，杂芳基，环烷基或杂环烷基，或-CO 2（烷基或取代的氨基）或CN; Z 2是H或Z 1; Z 3是H或烷基; 或Z 1，Z 2和Z 3与它们所连接的碳一起形成双环饱和或不饱和环; 因此，药物组合物以及所述化合物用作疼痛，焦虑，咳嗽，哮喘，抑郁和酒精滥用的伤害感受肽受体抑制剂的用途。

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