发明名称 PERIPHERALLY ACTING OPIOID COMPOUNDS
摘要 The invention relates to a compound of Formula I, II, III, IV or a pharmaceutically acceptable ester or prodrug thereof:;
申请公布号 US2017007609(A1) 申请公布日期 2017.01.12
申请号 US201615207731 申请日期 2016.07.12
申请人 Alkermes, Inc. 发明人 Blumberg Laura Cook;Arnelle Derrick
分类号 A61K31/513;A61K31/485 主分类号 A61K31/513
代理机构 代理人
主权项 1. A method of treating or preventing a side effect associated with an opioid, comprising the step of: administering to a patient in need thereof, a composition comprising an effective amount of a compound of Formula I, or a pharmaceutically acceptable salt thereof, or Formula II: wherein: u is 0, 1 or 2; t is 0, 1, 2, 3, 4, 5, 6, or 7; X is S or O; Y⊖ is a pharmaceutically acceptable counterion; R1 is selected from aliphatic, substituted aliphatic, aryl, substituted aryl, heterocyclyl or substituted heterocyclyl; Each R2, R3, R4, R6, R8, and R11 is independently selected from absent, hydrogen, halogen, —OR20, —SR20, —NR20R21, —C(O)R20, —C(O)OR20, —C(O)NR20R21, —N(R20)C(O)R21, —CF3, —CN, —NO2, —N3, acyl, alkoxy, substituted alkoxy, alkylamino, substituted alkylamino, dialkylamino, substituted dialkylamino, alkylthio, substituted alkylthio, alkylsulfonyl, substituted alkylsulfonyl, aliphatic, substituted aliphatic, aryl, substituted aryl, heterocyclyl or substituted heterocyclyl; alternatively R2 and R3 together with the carbon they are attached to form a C═X group or a vinyl group; alternatively, two R11 groups together with the carbon atom to which they are attached form a C═X or a vinyl group; wherein each R20 and R21 is independently selected from hydrogen, halogen, alkyl, substituted alkyl, aryl or substituted aryl; R5 is alkyl, substituted alkyl, aryl or substituted aryl; R7 is hydrogen, alkyl, substituted alkyl, aryl or substituted aryl; R9 is selected from hydrogen, aliphatic, substituted aliphatic, aryl, substituted aryl, heterocyclyl or substituted heterocyclyl; and R10 is selected from wherein s is 0, 1, 2, or 3; p is 0, 1, 2, 3, 4, 5, 6, or 7; q is 0, 1, 2, 3, 4, or 5; each R100, R101, R102, R103, R104, and R105 is independently selected from hydrogen, halogen, —OR20, —SR20, —NR20R21, —C(O)R20, —C(O)OR20, —C(O)NR20R21, —N(R20)C(O)R21, —CF3, —CN, —NO2, —N3, acyl, alkoxy, substituted alkoxy, alkylamino, substituted alkylamino, dialkylamino, substituted dialkylamino, substituted or unsubstituted alkylthio, substituted or unsubstituted alkylsulfonyl, optionally substituted aliphatic, optionally substituted aryl, heterocyclyl or substituted heterocyclyl; wherein the term “substituted” refers to the replacement of one or more hydrogen radicals in a given structure with the radical selected from halogen, alkyl, alkenyl, alkynyl, aryl, heterocyclyl, thiol, alkylthio, arylthio, alkylthioalkyl, arylthioalkyl, alkylsulfonyl, alkylsulfonylalkyl, arylsulfonylalkyl, alkoxy, aryloxy, aralkoxy, aminocarbonyl, alkylaminocarbonyl, arylaminocarbonyl, alkoxycarbonyl, aryloxycarbonyl, haloalkyl, amino, trifluoromethyl, cyano, nitro, alkylamino, arylamino, alkylaminoalkyl, arylaminoalkyl, aminoalkylamino, hydroxy, alkoxyalkyl, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, acyl, aralkoxycarbonyl, carboxylic acid, sulfonic acid, sulfonyl, phosphonic acid, heteroaryl, and aliphatic.
地址 Waltham MA US