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リジン特異的デメチラーゼ-1阻害剤およびその使用
专利权人:
オリゾン・ジェノミックス・ソシエダッド・アノニマ
发明人:
アルベルト・オルテガ・ムニョス,フリオ・カストロ-パロミノ・ラリア,マシュー・コリン・ソーア・ファイフ
申请号:
JP2012530181
公开号:
JP2013505903A
申请日:
2010.04.19
申请国别(地区):
JP
年份:
2013
代理人:
摘要:
The invention relates to a compound of Formula (I): (A&prime)x-(A)-(B)-(Z)-(L)-(D), wherein: (A) is heteroaryl or aryl each (A&prime), if present, is independently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A&prime) is substituted with 0, 1, 2, or 3 substituents independently chosen from halo, haloalkyl, aryl, arylalkoxy, alkyl, alkoxy, cyano, sulfonyl, amido, and sulfinyl X is 0, 1, 2, or 3 (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B) (Z) is &mdashNH&mdash (L) is chosen from &mdashCH2CH2&mdash, &mdashCH2CH2CH2&mdash, and &mdashCH2CH2CH2CH2&mdash and (D) is chosen from &mdashN(&mdashR1)-R2, &mdashO&mdashR3, and &mdashS&mdashR3, wherein: R1 and R2 are mutually linked to form a heterocyclic ring together with the nitrogen atom that R1 and R2 are attached to, wherein said heterocyclic ring has 0, 1, 2, or 3 substituents independently chosen from &mdashNH2, &mdashNH(C1-C6 alkyl), &mdashN(C1-C6 alkyl)(C1-C6 alkyl), alkyl, halo, cyano, alkoxy, haloalkyl, and haloalkoxy, or R1 and R2 are independently chosen from &mdashH, alkyl, cycloalkyl, haloalkyl, and heterocyclyl, wherein the sum of substituents on R1 and R2 together is 0, 1, 2, or 3, and the substituents are independently chosen from &mdashNH2, &mdashNH(C1-C6 alkyl), &mdashN(C1-C6 alkyl)(C1-C6 alkyl), and fluoro and R3 is chosen from &mdashH, alkyl, cycloalkyl, haloalkyl, and heterocyclyl, wherein R3 has 0, 1, 2, or 3 substituents independently chosen from &mdashNH2, &mdashNH(C1-C6 alkyl), &mdashN(C1-C6 alkyl)(C1-C6 alkyl), and fluoro or an enantiomer, diastereomer, or mixture thereof, or a pharmaceutically acceptable salt or solvate thereof. The compounds of the invention show inhibitory LSD1 activity, which makes them useful in the treatment or prevention of diseases such as cancer.本願発明は、式I:(A’)x-(A)-(B)-(Z)-(L)-(D)(式中:(A)はヘテロアリールまたはアリールであり;(A’)は、各々、存在するならば、アリール、アリー
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