Invention Grant
- Patent Title: Lysine specific demethylase-1 inhibitors and their use
- Patent Title (中): 赖氨酸特异性脱甲基酶-1抑制剂及其用途
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Application No.: US14228083Application Date: 2014-03-27
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Publication No.: US09149447B2Publication Date: 2015-10-06
- Inventor: Alberto Ortega Muñoz , Julio Castro-Palomino Laria , Matthew Colin Thor Fyfe
- Applicant: ORYZON GENOMICS S.A.
- Applicant Address: ES Barcelona
- Assignee: Oryzon Genomics S.A.
- Current Assignee: Oryzon Genomics S.A.
- Current Assignee Address: ES Barcelona
- Agency: Finnegan, Henderson, Farabow, Garrett & Dunner, LLP
- Priority: EP10160315 20100419
- Main IPC: A61K31/165
- IPC: A61K31/165 ; A61K31/135 ; C07C211/35 ; C07C211/42 ; C07C217/52 ; C07C237/24 ; A61K45/06 ; C07C211/40 ; C07C217/74

Abstract:
The present invention relates to a compound of Formula 1, wherein: (A) is heteroaryl or aryl; each (A′), if present, is independently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A′) is substituted with 0, 1, 2, or 3 substituents independently chosen from halo, haloalkyl, haloalkoxy, aryl, arylalkoxy, alkyl, alkoxy, amido, —CH2C(═0)NH2, heteroaryl, cyano, sulfonyl, 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 —NH—; (L) is chosen from a single bond, —CH2—, —CH2CH2—, —CH2CH2CH2—, and —CH2CH2CH2CH2—; and (D) is an aliphatic carbocyclic group or benzocycloalkyl, wherein said aliphatic carbocyclic group or said benzocycloalkyl has 0, 1, 2, or 3 substituents independently chosen from —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)(C1-C6 alkyl), alkyl, halo, amido, cyano, alkoxy, haloalkyl, and haloalkoxy. (A′)X-(A)-(B)—(Z)-(L)-(D) formula (I) The compounds of the invention show activity for inhibiting LSD1, which makes them useful in the treatment or prevention of diseases such as cancer.
Public/Granted literature
- US20140213657A1 LYSINE SPECIFIC DEMETHYLASE-1 INHIBITORS AND THEIR USE Public/Granted day:2014-07-31
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