Invention Grant
- Patent Title: Substituted pyrrolo[2,1-a]phthalazines and benzo[g]pyrrolo[2,1-a]phthalazines for the treatment of cancer
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Application No.: US16764873Application Date: 2018-11-16
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Publication No.: US11066412B2Publication Date: 2021-07-20
- Inventor: Te-Chang Lee , Tsann-Long Su , Tai-Lin Chen
- Applicant: Academia Sinica
- Applicant Address: TW Taipei
- Assignee: Academia Sinica
- Current Assignee: Academia Sinica
- Current Assignee Address: TW Taipei
- Agency: NZ Carr Law Office PLLC
- International Application: PCT/US2018/061400 WO 20181116
- International Announcement: WO2019/099755 WO 20190523
- Main IPC: C07D487/14
- IPC: C07D487/14 ; C07D487/22 ; C07D487/04 ; A61P35/02 ; A61K45/06
![Substituted pyrrolo[2,1-a]phthalazines and benzo[g]pyrrolo[2,1-a]phthalazines for the treatment of cancer](/abs-image/US/2021/07/20/US11066412B2/abs.jpg.150x150.jpg)
Abstract:
Disclosed herein are novel bifunctional compounds and their uses for the treatment and/or prophylaxis of cancers. The bifunctional compound disclosed herein has the structure of formula (I), wherein, optionally substituted with one or more substituents independently selected from the group consisting of halo, alkyl, haloalkyl, alkenyl, C(O)H, OH, O(alkyl), O(CO)alkyl, O(aryl), aryl, and —O(CH2)xN(Rb)2; R1 is an alkyl optionally substituted with one or more substituents independently selected from the group consisting of halo, —OR, —O(CO)CH3, —OSO2R, and —OCONHR; R is hydrogen, alkyl, cycloalkyl, or aryl; R2 is hydrogen, alkyl, cycloalkyl, aryl or heteroaryl, in which the aryl or heteroaryl is optionally substituted with one or more substituents independently selected from the group consisting of C1-6 alkyl, O(alkyl), halo, cyano, nitro, —N(Rc)2, OCH2O—, O(CH2)2O—, pyrrolidinyl, piperidinyl, piperazinyl, morpholino, and 4—(piperido)piperidinyl; R3 is -NRARB, or -NHPhRC, or -NRARB are taken together to form pyrrolidin-l-yl, piperidin-l-yl, piperazin-l-yl, morpholin-4-yl, 4-(piperidin-l-y)piperidin-l-yl, or 4-(piperidin-4-yl)piperidin-l-yl, wherein the piperazin-l-yl or 4-(piperidin-4-yl) piperidin-l-yl is optionally substituted with one or more substituents independently selected from the group consisting of alky, and —(CH2)nCONH(CH2)mNRARB; RA and RB are independently H or C1-C6 alkyl; RC is hydrogen, halo, alkyl, alkenyl, alknyl, O(alkyl), —NHCORa, —NHC(O)ORa, heterocyclyl or aryl, in which the alkyl is optionally substituted with one or more substituents independently selected from the group consisting of halo, alkyl, haloalkyl, alkenyl C(O)H, OC(O)alkyl, O(aryl), and aryl, in which the aryl is optionally substituted with one or more substituents independently selected from the group consisting of halo, CN, C1-6 alkyl, N(Rc)2, NO2, O(alkyl), —OCH2O—, —O(CH2)2O—,pyrrolidinyl, pepiridinyl, piperazinyl, morpholino, and 4-(piperido)piperidinyl; Ra is C1-6 alkyl or aryl; Rb is C1-10 alkyl, pyrrolidin-l-yl, piperidin-l-yl, piperazin-l-yl, morpholin-4-yl, 4-(piperidin-l-yl)piperidin-l-yl, or 4-(piperidin-4-yl)piperidin-l-yl; Rc, is hydrogen or C1-10 alkyl; and. x, n and m are independently an integral between 1 to 5.
Public/Granted literature
- US20200339584A1 BIS(HYDROXYMETHYL)PYRROLOPHTHALAZINE HYBRIDS, PREPARATION METHODS AND USES THEREOF Public/Granted day:2020-10-29
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