公开(公告)号：US11530237B2

公开(公告)日：2022-12-20

申请号：US16748117

申请日：2020-01-21

申请人： Sage Therapeutics, Inc.

发明人： Gabriel Martinez Botella ,  Francesco G. Salituro ,  Albert Jean Robichaud ,  Boyd L. Harrison

IPC分类号： C07J43/00 ,  C07J1/00 ,  C07J7/00 ,  A61K31/58 ,  A61K31/575 ,  A61P23/00 ,  A61P25/00 ,  A61P25/06 ,  A61P25/08 ,  A61P25/14 ,  A61P25/18 ,  A61P25/20 ,  A61K45/06 ,  C07J9/00 ,  C07J3/00 ,  C07J5/00 ,  C07J11/00 ,  C07J13/00 ,  C07J21/00 ,  C07J31/00 ,  C07J41/00 ,  C07J51/00 ,  C07J71/00

摘要： Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein , A, R1, R2, R3a, R4a, R4b, R5, R7a, and R7b are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia.

公开(公告)号：US11512034B2

公开(公告)日：2022-11-29

申请号：US17303462

申请日：2021-05-28

申请人： McMaster University

发明人： Jakob Magolan ,  Nicholas Jentsch ,  Xiong Zhang ,  Mathew Piotrowski

IPC分类号： C07C37/14 ,  C07J7/00 ,  B01J21/04 ,  C07D209/08 ,  C07C41/26 ,  C07D307/80 ,  C07C201/12 ,  C07J1/00 ,  C07D311/30 ,  C07D311/32 ,  C07C253/30

摘要： The present application describes process for preparing an ortho-allylated hydroxy aryl compounds such as compounds of Formula (I) by reacting an allylic alcohol with a hydroxy aryl compound in the presence of aluminum compound selected from alumina and aluminum alkoxides and in a non-protic solvent wherein at least one carbon atom ortho to the hydroxy group in the hydroxy aryl compound is unsubstituted. The present application also includes compounds of Formula (I).

公开(公告)号：US20220296609A1

公开(公告)日：2022-09-22

申请号：US17639206

申请日：2020-09-02

申请人： RICHTER GEDEON NYRT.

发明人： Róbert LOVAS ,  Sándor MAHÓ ,  Ildikó BACSA ,  Beatrix MAYER

IPC分类号： A61K31/566 ,  C07J1/00 ,  A61K31/585

摘要： The invention relates to the preparation of estetrol of formula (I), derivatives thereof protected at positions 3,15α,16α,17β of general formula (III), and 3-hydroxy derivatives thereof protected at positions 15α,16α,17β of general formula (IV), and to the intermediates of general formulae (III) and (IV) applied in the process. Another aspect of the invention is the use of estetrol of formula (I) obtained by the process of the invention for the preparation of a pharmaceutical composition.

公开(公告)号：US20220204464A1

公开(公告)日：2022-06-30

申请号：US17618110

申请日：2020-06-12

申请人： Arxada AG

发明人： Christoph TAESCHLER ,  Matthias BELLER ,  Helfried NEUMANN ,  Florian FISCHER ,  Shaoke ZHANG ,  Fei YE ,  Stefan ELLINGER ,  Florencio ZARAGOZA DOERWALD

IPC分类号： C07D295/073 ,  C07D295/067 ,  C07C45/68 ,  C07D317/72 ,  C07C67/343 ,  C07J1/00 ,  C07D451/06 ,  C07D335/02

摘要： The invention discloses a method for fluoroalkylation of enamines with a fluoro alkyl halide in the presence of a base.

公开(公告)号：US11344563B2

公开(公告)日：2022-05-31

申请号：US16507214

申请日：2019-07-10

申请人： Sage Therapeutics, Inc.

发明人： Gabriel Martinez Botella ,  Boyd L. Harrison ,  Albert Jean Robichaud ,  Francesco G. Salituro ,  Richard Thomas Beresis

IPC分类号： A61K31/58 ,  C07J7/00 ,  C07J3/00 ,  C07J9/00 ,  C07J17/00 ,  C07J33/00 ,  C07J15/00 ,  C07J43/00 ,  A61K31/573 ,  C07J1/00 ,  C07J13/00 ,  C07J21/00 ,  C07J41/00 ,  C07J5/00 ,  C07J31/00

摘要： Provided herein are 19-nor C3,3-disubstituted steroids of Formula (I): and pharmaceutically acceptable salts thereof; wherein , R1, R2, R3a, R3b, R4a, and R4b are as defined herein, and A is a carbon bound substituted or unsubstituted 5- to 6-membered heteroaryl ring as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.

公开(公告)号：US11280795B2

公开(公告)日：2022-03-22

申请号：US16099017

申请日：2017-05-03

申请人： Indiana University Research and Technology Corporation

发明人： Avinash Shivaputrappa Patil

IPC分类号： G01N33/74 ,  G01N33/68 ,  G01N33/48 ,  G01N33/53 ,  C07J7/00 ,  C07J1/00 ,  C07J5/00 ,  G01N33/487 ,  G01N33/566 ,  C07K16/26

摘要： Disclosed are methods for identifying a pregnant female who is susceptible to spontaneous preterm delivery. In particular, disclosed are methods for identifying a pregnant female who is susceptible to spontaneous preterm delivery based on ratios of steroids in samples obtained from the pregnant female.

公开(公告)号：US11242314B2

公开(公告)日：2022-02-08

申请号：US15403954

申请日：2017-01-11

申请人： Dong Zhou ,  Wenhua Chu

发明人： Dong Zhou ,  Wenhua Chu

IPC分类号： C07C315/04 ,  C07D213/52 ,  C07D213/71 ,  C07H3/02 ,  C07H19/06 ,  C07D233/91 ,  C07D207/09 ,  C07C247/04 ,  C07C67/307 ,  C07C45/63 ,  C07C303/22 ,  C07J1/00 ,  C07B59/00

摘要： The present disclosure relates to the methods for the preparation of reactive [F-18]fluoride in a form of [F-18]sulfonyl fluoride suitable for efficient radiolabeling without an azeotropic evaporation step by the use of anion exchange resin and sulfonyl chloride, and its applications in the manufacturing of PET radiopharmaceuticals.

公开(公告)号：US11208432B2

公开(公告)日：2021-12-28

申请号：US16065627

申请日：2016-12-22

申请人： ORIC Pharmaceuticals, Inc.

发明人： Daqing Sun ,  Lawrence R. McGee ,  Xiaohui Du ,  Liusheng Zhu ,  Xuelei Yan ,  Yosup Rew ,  John Eksterowicz ,  Julio C. Medina ,  Haiying Zhou ,  Minna Delarae Balbas ,  Valeria R. Fantin

IPC分类号： C07J1/00 ,  A61P5/44 ,  A61P5/46 ,  A61P35/00 ,  C07J17/00 ,  C07J41/00 ,  C07J43/00 ,  A61K45/06 ,  C07K16/28

摘要： The present invention relates generally to compositions and methods for treating cancer and hypercortisolism. Provided herein are substituted steroidal derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of glucocorticoid receptors. Furthermore, the subject compounds and compositions are useful for the treatment of cancer and hypercortisolism.

公开(公告)号：US20210380630A1

公开(公告)日：2021-12-09

申请号：US17403899

申请日：2021-08-17

申请人： Atia-tul- Wahab ,  Muhammad Iqbal Choudhary ,  Rabia Farooq ,  Nimra Naveed Shaikh ,  Atta-ur- Rahman

发明人： Atia-tul- Wahab ,  Muhammad Iqbal Choudhary ,  Rabia Farooq ,  Nimra Naveed Shaikh ,  Atta-ur- Rahman

IPC分类号： C07J1/00

摘要： The present invention identifies new steroidal analogues of formestane synthesized through biotransformation with significant aromatase inhibitory activity, and thus can serve as possible safe, effective, and selective anti-cancer agent towards estrogen-responsive (ER+) breast cancer. Four new derivatives of anticancer drug formestane (1), 4α,5α,7α-trihydroxyandrostane-3,17-dione (2), 3β,7β-dihydroxyandrostane-4,17-dione (3), 3β,5α,7β-trihydroxyandrostane-4,17-dione (4), and 4,11α-dihydroxyandrosta-1,4-diene-3,17-dione (5) were synthesized through bio-catalyzed structural modifications by Cunninghamella. blakesleeana and Fusarium lini. The new derivatives showed varying degree of inhibition of aromatase enzyme. Metabolite 4 (IC50=0.386±0.072 μM), showed a significant inhibitory potential, comparable to substrate 1 (IC50=0.335±0.011 μM) and standard aromatase inhibitory anti-cancer drug exemestane (IC50=0.232±0.031 μM). Metabolites 3 (IC50=1.37±0.029 μM), and 2 (IC50=5.229±0.094 μM) showed significant inhibition, while metabolite 5 (IC50=34.27±0.532 μM) showed a weak inhibitory activity as compared to standard.

公开(公告)号：US20210379084A1

公开(公告)日：2021-12-09

申请号：US17381430

申请日：2021-07-21

申请人： ORIC Pharmaceuticals, Inc.

发明人： Daqing SUN ,  Lawrence R. McGEE ,  Xiaohui DU ,  Liusheng ZHU ,  Xuelei YAN ,  Yosup REW ,  John EKSTEROWICZ ,  Julio C. MEDINA ,  Haiying ZHOU ,  Minna Delarae BALBAS ,  Valeria R. FANTIN

IPC分类号： A61K31/58 ,  A61K31/567 ,  A61K45/06 ,  C07J1/00 ,  C07J21/00 ,  C07J43/00

摘要： The present invention relates generally to compositions and methods for treating cancer and hypercortisolism. Provided herein are substituted steroidal derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of glucocorticoid receptors. Furthermore, the subject compounds and compositions are useful for the treatment of cancer and hypercortisolism.