公开(公告)号：US20180230112A1

公开(公告)日：2018-08-16

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

IPC分类号： C07D265/38 ,  C07D413/04 ,  C07D291/08 ,  C07D419/04 ,  C07D285/01 ,  C07D417/04 ,  C07D498/04 ,  C07D301/14 ,  C07D309/28

CPC分类号： C07D265/38 ,  C07B2200/07 ,  C07D209/86 ,  C07D275/06 ,  C07D285/01 ,  C07D291/08 ,  C07D301/14 ,  C07D307/30 ,  C07D309/28 ,  C07D401/04 ,  C07D405/04 ,  C07D413/04 ,  C07D417/04 ,  C07D419/04 ,  C07D498/04 ,  Y02P20/582

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：US20180251456A1

公开(公告)日：2018-09-06

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 ,  C07D405/04 ,  C07D413/14 ,  C07D401/04

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：US20180105485A1

公开(公告)日：2018-04-19

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

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：US20160200666A1

公开(公告)日：2016-07-14

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

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.

摘要翻译： 公开了式I的环状野生型酰胺。该化合物可用于治疗由含有乙酰赖氨酸的蛋白质的不适当活性引起的疾病。 所述组合物包含作为溴结构域抑制剂的环状野生型酰胺属。

公开(公告)号：US20220402880A1

公开(公告)日：2022-12-22

申请号：US17753980

申请日：2020-09-23

申请人： Icahn School of Medicine At Mount Sinai

发明人： Nilesh ZAWARE ,  Ming-Ming ZHOU ,  Chunyan REN ,  Claudia KIM ,  Sudeh IZADMEHR ,  Matthew GALSKY

IPC分类号： C07D235/30 ,  C07D209/08 ,  C07D403/06 ,  A61P35/00

摘要： A genus of bicyclic inhibitors of CBX chromodomains is disclosed. The compounds are of the following genus: The compounds inhibit CBX proteins and, as a consequence, they are useful for treating prostate cancer, ovarian cancer, and B-cell lymphoma.

公开(公告)号：US20180251444A1

公开(公告)日：2018-09-06

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 ,  C07D405/04 ,  C07D417/04 ,  C07D401/14 ,  C07D417/14 ,  A61P35/00

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

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.