Invention Grant
US09561290B2 Functionalized thieno-indole derivatives for the treatment of cancer
有权
用于治疗癌症的功能化噻吩并吲哚衍生物
- Patent Title: Functionalized thieno-indole derivatives for the treatment of cancer
- Patent Title (中): 用于治疗癌症的功能化噻吩并吲哚衍生物
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Application No.: US14390216Application Date: 2013-03-28
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Publication No.: US09561290B2Publication Date: 2017-02-07
- Inventor: Italo Beria , Michele Caruso , Vittoria Lupi , Paolo Orsini , Matteo Salsa
- Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
- Applicant Address: IT Nerviano (MI)
- Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
- Current Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
- Current Assignee Address: IT Nerviano (MI)
- Agency: Scully, Scott, Murphy & Presser, P.C.
- Priority: EP12163437 20120405
- International Application: PCT/EP2013/056733 WO 20130328
- International Announcement: WO2013/149946 WO 20131010
- Main IPC: C07D495/04
- IPC: C07D495/04 ; A61K47/48 ; A61K31/496 ; A61K45/06 ; A61K31/407 ; A61P35/00

Abstract:
The invention relates to new functionalized thieno-indole derivatives of formula (I) or (II) which have cytotoxic activity and are useful in treating diseases such as cancer and cellular proliferation disorders. The invention also relates to the use of these functionalized thieno-indole derivatives in the preparation of conjugates. Formula (I) or (II) wherein R1 and R2 taken together form a group (D) or (G): wherein R5 is hydrogen or C1-C4 alkyl; R3 and R4 are independently hydrogen, C1-C4 alkyl or C1-C4 hydroxyalkyl; n is 0, 1 or 2; each of X is independently —O—, —S— or —NR4—; each of Y is independently —CH═ or —N═; R7 and R8 are independently hydrogen, halogen, hydroxy, C1-C4 alkoxy, cyano, —NHCOOR3, —C(NH)NH2 or —NR3R4; A is —O—, —NH— or —CO—; L is null or a conditionally-cleavable moiety; W is null or a self-immolative moiety comprising one or more self-immolative groups; Z is null or a peptidic, non peptidic or hybrid peptidic and non peptidic linker; RM is null or a reactive moiety; R6 is a leaving group; A1 is null or A; L1 is hydrogen or L.
Public/Granted literature
- US20150080316A1 FUNCTIONALIZED THIENO-INDOLE DERIVATIVES FOR THE TREATMENT OF CANCER Public/Granted day:2015-03-19
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