公开(公告)号：US10759790B2

公开(公告)日：2020-09-01

申请号：US15758045

申请日：2016-09-08

申请人： ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI

发明人： Michael Ohlmeyer ,  Nilesh Zaware

IPC分类号： C07D413/04 ,  C07D413/14 ,  C07D401/04 ,  C07D498/04 ,  C07D403/04 ,  C07D405/04

摘要： A genus of arylsulfonamide derivatives of heterocyclic constrained tricyclic compounds is disclosed. The compounds are of the following genus: The compounds induce FOXO1 transcription factor translocation to the nucleus by modulating PP2A and, as a consequence, exhibit anti-proliferative effects. They are useful in the treatment of a variety of disorders, including as a therapy in cancer treatment, or used in combination with other drugs to restore sensitivity to chemotherapy where resistance has developed.

公开(公告)号：US09884806B2

公开(公告)日：2018-02-06

申请号：US14914672

申请日：2014-08-29

申请人： ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI

发明人： Ming-Ming Zhou ,  Michael Ohlmeyer ,  Adam Vincek ,  Nilesh Zaware

IPC分类号： A61K31/136 ,  A61K31/166 ,  A61K31/18 ,  A61K31/195 ,  A61K31/196 ,  A61K31/245 ,  A61K31/277 ,  A61K31/404 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4468 ,  A61K31/47 ,  A61K31/4965 ,  A61K31/498 ,  A61K31/517 ,  A61K31/5375 ,  A61K45/06 ,  C07D209/08 ,  C07D209/40 ,  C07D211/58 ,  C07D213/74 ,  C07D213/75 ,  C07D213/76 ,  C07D215/06 ,  C07D215/38 ,  C07D217/02 ,  C07D239/74 ,  C07D241/20 ,  C07D241/42 ,  C07D249/04 ,  C07D249/06 ,  C07D295/16 ,  C07D295/21 ,  C07C225/20 ,  C07C229/48 ,  C07C229/56 ,  C07C229/60 ,  C07C229/68 ,  C07C237/30 ,  C07C237/40 ,  C07C255/58 ,  C07C311/38 ,  C07D235/26

CPC分类号： C07C225/20 ,  A61K31/136 ,  A61K31/166 ,  A61K31/18 ,  A61K31/195 ,  A61K31/196 ,  A61K31/245 ,  A61K31/277 ,  A61K31/404 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4468 ,  A61K31/47 ,  A61K31/4965 ,  A61K31/498 ,  A61K31/517 ,  A61K31/5375 ,  A61K45/06 ,  C07C229/48 ,  C07C229/56 ,  C07C229/60 ,  C07C229/68 ,  C07C237/30 ,  C07C237/40 ,  C07C255/58 ,  C07C311/38 ,  C07D209/08 ,  C07D209/40 ,  C07D211/58 ,  C07D213/74 ,  C07D213/75 ,  C07D213/76 ,  C07D215/06 ,  C07D215/38 ,  C07D217/02 ,  C07D235/26 ,  C07D239/74 ,  C07D241/20 ,  C07D241/42 ,  C07D249/04 ,  C07D249/06 ,  C07D295/16 ,  C07D295/21 ,  A61K2300/00

摘要： Cyclic vinylogous amides of Formula I are disclosed The compounds are useful for treating diseases that arise from inappropriate activity of proteins containing an acetyl-lysine. The compositions comprise a genus of cyclic vinylogous amides that are inhibitors of bromodomain.

公开(公告)号：US10450282B2

公开(公告)日：2019-10-22

申请号：US15750388

申请日：2016-08-05

申请人： ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI

发明人： Michael Ohlmeyer ,  Nilesh Zaware ,  David Kastrinsky

IPC分类号： C07D498/04 ,  C07D209/86 ,  C07D209/88 ,  C07D275/06 ,  C07D291/08 ,  C07D265/38 ,  C07D401/04 ,  C07D405/04 ,  C07D413/04 ,  C07D417/04 ,  C07D307/30 ,  C07D285/01 ,  C07D301/14 ,  C07D309/28 ,  C07D419/04

摘要： A process for the stereoselective synthesis of chiral 3-heterocyclyl-1,2-dihydroxy cyclohexanes is disclosed. The process involves reacting a tricyclic nitrogenous heterocycle with an allyl carbonate in the presence of a chiral palladium catalyst followed by oxidation of the olefinic bond to provide 3-heterocyclyl-1,2-dihydroxy cyclohexanes, cyclopentanes and corresponding alicyclic heterocycles. Also disclosed are methods for converting the heterocyclyl-1,2-dihydroxy cyclohexanes to 2-amino-6-(heteroaryl)cyclohexanols (and related cyclic compounds).

公开(公告)号：US10351511B2

公开(公告)日：2019-07-16

申请号：US15842032

申请日：2017-12-14

申请人： ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI

发明人： Ming-Ming Zhou ,  Michael Ohlmeyer ,  Adam Vincek ,  Nilesh Zaware

IPC分类号： A61K31/136 ,  A61K31/166 ,  A61K31/18 ,  A61K31/195 ,  A61K31/196 ,  A61K31/245 ,  A61K31/277 ,  A61K31/404 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4468 ,  A61K31/47 ,  A61K31/4965 ,  A61K31/498 ,  A61K31/517 ,  A61K31/5375 ,  C07C225/20 ,  C07C229/48 ,  C07C229/56 ,  C07C229/60 ,  C07C229/68 ,  C07C237/30 ,  C07C237/40 ,  C07C255/58 ,  C07C311/38 ,  C07D209/08 ,  C07D211/58 ,  C07D213/74 ,  C07D215/06 ,  C07D217/02 ,  C07D235/26 ,  C07D239/74 ,  C07D241/20 ,  C07D241/42 ,  C07D249/04 ,  C07D295/16 ,  A61K45/06 ,  C07D213/75 ,  C07D213/76 ,  C07D215/38 ,  C07D249/06 ,  C07D209/40 ,  C07D295/21

摘要： Cyclic vinylogous amides of Formula I are disclosed The compounds are useful for treating diseases that arise from inappropriate activity of proteins containing an acetyl-lysine. The compositions comprise a genus of cyclic vinylogous amides that are inhibitors of bromodomain.

公开(公告)号：US10221158B2

公开(公告)日：2019-03-05

申请号：US15758038

申请日：2016-09-08

申请人： ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI

发明人： Michael Ohlmeyer ,  Nilesh Zaware

IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D417/04 ,  C07D417/14 ,  A61P35/00

摘要： A genus of arylsulfonamide derivatives of heterocyclic constrained tricyclic compounds is disclosed. The compounds are of the following genus: The compounds induce FOXO1 transcription factor translocation to the nucleus by modulating PP2A and, as a consequence, exhibit anti-proliferative effects. They are useful in the treatment of a variety of disorders, including as a therapy in cancer treatment, or used in combination with other drugs to restore sensitivity to chemotherapy where resistance has developed.