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1. 发明申请

WO2023021026A1 A SYNTHETIC PATHWAY TO ESTRA-1,3,5(10)-TRIENE-3,15A,16A,17B-TETROL 审中-公开
公开(公告)号：WO2023021026A1
公开(公告)日：2023-02-23
申请号：PCT/EP2022/072847
申请日：2022-08-16
申请人： ASPEN OSS B.V.
发明人： BOTMAN, Petrus Nicolaas Maria , STOCK, Herman Thijs
IPC分类号： C07J1/00 , C07J31/00 , C07J51/00
摘要： A method of preparing a compound of Formula (VI) is provided wherein: R1, R2 and R3 are independently selected from H, halogen or methyl; and, Pr2 is -Q2, -C(O)Q2 or -Si(Q2)3 wherein each Q2 is independently selected from C1-C6 alkyl, C1-C6 heteroalkyl, C3-C8 heterocycloalkyl, C6-C10 aryl, C7-C18 alkylaryl or C7-C18 aralkyl; and, said method comprising the steps of: a) reacting a compound of Formula (I) with a compound of Formula (II) to form a product of Formula (III), wherein: Z is OR4 or SR5; R4 is C1-C4 alkyl or C6-C10 aryl; R5 is C1-C4 alkyl or C6-C10 aryl; T1 is C1-C6 alkyl or a 5- or 6-membered aromatic ring having 0, 1 or 2 heteroatoms, said aromatic ring being substituted with n substituents X; each X is independently selected from halogen, cyano, C1-C4 alkyl, C1-C4 alkoxy or C(O)R6; R6 is C1-C4 alkyl; and, n is 0, 1 or 2; b) reacting said compound of Formula (III) with compound Pr2-A to yield a compound of Formula (IV) wherein A is halogen or -OSO2CF; c) desulfiny lation of the compound of Formula (IV) to form a compound of Formula (V), under heating in the presence of a non-polar aprotic solvent and at least one of a base and a tri(C1-C2)alkylphosphite; d) subjecting the compound of Formula (V) to a reduction to form said compound of Formula (VI), wherein said reduction comprises treating said compound of Formula (V) in the presence of a solvent with a hydride donor selected from borohydrides and aluminium hydride compounds.

2. 发明申请

WO2022198191A1 ANDROGEN RECEPTOR MODULATORS 审中-公开
公开(公告)号：WO2022198191A1
公开(公告)日：2022-09-22
申请号：PCT/US2022/071130
申请日：2022-03-14
申请人： TRUSTEES OF DARTMOUTH COLLEGE
发明人： MICALIZIO, Glenn C.
IPC分类号： C07J1/00 , C07J3/00
摘要： The present disclosure relates to polycyclic (e.g., tetracyclic) androgen receptor (AR) modulators, synthetic methods for preparing such AR modulators, and methods of using such AR modulators to treat an androgen-dependent condition, such as prostate cancer or BPH. Exemplary compounds have quaternary centers at C10 and C13 and a fused cyclic ring comprising C14 and C15.

3. 发明申请

WO2021262836A1 3.ALPHA.-HYDROXY, 17.BETA.-C(O)-N-ARYL SUBSTITUTED NEUROACTIVE STEROIDS AND COMPOSITIONS THEREOF 审中-公开
公开(公告)号：WO2021262836A1
公开(公告)日：2021-12-30
申请号：PCT/US2021/038661
申请日：2021-06-23
申请人： SAGE THERAPEUTICS, INC.
发明人： HAN, Bingsong , BLANCO-PILLADO, Maria Jesus
IPC分类号： C07J43/00 , C07J63/00 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/28 , A61P25/30 , A61K31/58 , A61K31/56 , C07J1/00 , C07J3/00 , C07J7/00 , C07J41/00 , C07J51/00 , C07J1/0011 , C07J3/005 , C07J41/005 , C07J41/0066 , C07J43/003 , C07J63/008 , C07J7/002
摘要： Provided herein is a compound of the Formula (I) or a pharmaceutically acceptable salt thereof, wherein R2a, R2b, R3a, R4a, R4b, R5, R6, R7, R11a, R11b, R15a, R15b, R16, R17, R19, RX, RY, and t are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds, e.g., in the treatment of CNS-related disorders.

4. 发明申请

WO2021252761A2 MONOMERIC AND OLIGOMERIC COMPOUND EMBODIMENTS AS CONTRACEPTIVES AND THERAPIES AND METHODS OF MAKING AND USING THE SAME 审中-公开
公开(公告)号：WO2021252761A2
公开(公告)日：2021-12-16
申请号：PCT/US2021/036809
申请日：2021-06-10
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , ASH STEVENS, LLC
发明人： KASKAR, Bashir , LIN, Ming-Teh , LEE, Min , BLITHE, Diana , GUPTA, Pranab
IPC分类号： A61P1/00 , A61P3/00 , A61P7/06 , A61P9/00 , A61P11/00 , A61P15/00 , A61P15/08 , A61P21/06 , A61P31/04 , A61P31/10 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/00 , C07J1/00 , C07J3/00 , C07J5/00 , C07J31/00 , C07J41/00 , C07J43/00 , C07J1/0025 , C07J1/0074 , C07J1/0096 , C07J3/005 , C07J31/006 , C07J41/0038 , C07J41/0044 , C07J41/0072 , C07J43/003 , C07J5/0053 , C07J5/0076
摘要： Disclosed herein are monomeric and oligomeric compound embodiments for use as contraceptive agents. Monomeric compound embodiments disclosed herein comprise substituents that facilitate the ability of the compounds to exhibit progestogenic, androgenic, and estrogenic activity, which can prevent or inhibit bone density loss in subjects. Oligomeric compound embodiments disclosed herein provide the ability to control receptor activation and/or treatment by incorporating a tunable linker group which couples steroidal-based compounds to one another or with therapeutic agents and facilitates selective cleavage of the monomeric components of the oligomeric compound.

5. 发明申请

WO2020264495A1 COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS 审中-公开
公开(公告)号：WO2020264495A1
公开(公告)日：2020-12-30
申请号：PCT/US2020/040119
申请日：2020-06-29
申请人： SAGE THERAPEUTICS, INC.
发明人： ROBICHAUD, Albert, Jean , SALITURO, Francesco, G. , BLANCO-PILLADO, Maria, Jesus , LA, Daniel , HARRISON, Boyd, L. , MORNINGSTAR, Marshall, Lee
IPC分类号： C07J43/00 , C07J7/00 , C07J1/00 , C07J63/00 , C07J67/00 , A61K31/58 , A61K31/57 , A61K31/573 , A61P25/00 , C07J13/00 , C07J15/00 , C07J21/00 , C07J31/00 , C07J41/00 , C07J51/00 , C07J53/00 , C07J71/00 , C07C13/00
摘要： Provided herein is a compound of Formula (1-I): or a pharmaceutically acceptable salt thereof, wherein R 2a , R 2b , R 3 , R 4a , R 4b , R 5 , R 6a , R 6b , R 11a , R 11b , R 16a , R 16b , R 19 , R 18 , X, q, r, s, t, u, and n are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (1-I) and methods of using the compounds, e.g, in the treatment of CNS -related disorders.

6. 发明申请

WO2020053509A1 COMPOSES ANALOGUES DE LA SQUALAMINE ET LEUR UTILISATION MEDICALE 审中-公开
公开(公告)号：WO2020053509A1
公开(公告)日：2020-03-19
申请号：PCT/FR2019/052064
申请日：2019-09-09
申请人： CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE , ASSISTANCE PUBLIQUE - HOPITAUX DE MARSEILLE , UNIVERSITE D'AIX-MARSEILLE , INSERM (INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE) , INSTITUT JEAN PAOLI & IRENE CALMETTES
发明人： BLIN, Olivier , KRAUS, Jean Louis , RAOULT, Didier , BRUNEL, Jean Michel , ROLAIN, Jean-Marc , SAKR, Adèle
IPC分类号： A61K31/57 , A61P31/04 , A61P31/10 , A61P31/06 , A61P33/00 , A61P35/00 , A61P31/12 , C07J41/00 , C07J1/00
摘要： L'invention concerne une famille de composés analogues de la squalamine pour leur utilisation comme médicament, en particulier pour le traitement ou la prévention d'infections mycobactériennes, notamment de la tuberculose. La présente invention a également pour objet de nouveaux composés analogues de la squalamine et leur utilisation comme médicament, notamment pour le traitement ou la prévention d'infections bactériennes, fongiques, virales, parasitaires ou dans le traitement du cancer chez l'homme ou l'animal, ainsi que des compositions pharmaceutiques ou vétérinaires les comprenant. L'invention concerne enfin l'utilisation de ces nouveaux composés comme agents désinfectant et/ou décontaminant.

7. 发明申请

WO2020051329A1 C19 SCAFFOLDS AND STEROIDS AND METHODS OF USE AND MANUFACTURE THEREOF 审中-公开
公开(公告)号：WO2020051329A1
公开(公告)日：2020-03-12
申请号：PCT/US2019/049743
申请日：2019-09-05
申请人： TRUSTEES OF DARTMOUTH COLLEGE
发明人： MICALIZIO, Glenn C. , GAUR, Arti B.
IPC分类号： C07J1/00 , C07J3/00 , C07J75/00
摘要： The present disclosure relates to stereodefined polycyclic (e.g., tetracyclic) compounds that contain quaternary centers at one or multiple ring fusions, synthetic methods for preparing such compounds, and methods of using such compounds to treat a disease, such as a brain tumor and, particularly, a glioma.

8. 发明申请

WO2018197296A1 PROCESS FOR THE PREPARATION OF DES-A-STEROIDS, INTERMEDIATES USEFUL FOR THE SYNTHESIS OF 9BETA,10ALFA-STEROIDS 审中-公开
公开(公告)号：WO2018197296A1
公开(公告)日：2018-11-01
申请号：PCT/EP2018/059890
申请日：2018-04-18
申请人： NEWCHEM S.P.A.
发明人： LOPOPOLO, Gianfranco , FABRIS, Francesco , MONTORSI, Mauro , MERLO, Massimo , GAMBARIN, Luca , DI BRISCO, Roberto , ZAUPA, Giovanni , GENONI, Andrea , ANDRIOLO, Erika
IPC分类号： C07J1/00
CPC分类号： C07D317/72 , C07C49/553 , C07D317/00
摘要： The present invention relates to a process for the synthesis of intermediates of general formula (I): by means of a simultaneous protection and hydrogenation reaction of an intermediate of formula (II), according to the scheme below: Compounds (I) are intermediates useful for the preparation of steroidal compounds with a (9β,10α) configuration, which are an important group of molecules with known pharmacological activity.

9. 发明申请

WO2017192668A1 QUANTITATIVE PROFILING OF PROGESTERONE METABOLITES FOR THE PREDICTION OF SPONTANEOUS PRETERM DELIVERY 审中-公开
标题翻译：孕酮代谢物定量分析预测自发前体递送
公开(公告)号：WO2017192668A1
公开(公告)日：2017-11-09
申请号：PCT/US2017/030759
申请日：2017-05-03
申请人： INDIANA UNIVERSITY RESEARCH & TECHNOLOGY CORPORATION
发明人： PATIL, Dr. Avinash Shivaputrappa
IPC分类号： C07J1/00 , C07J5/00 , C07J51/00 , G01N33/48 , G01N33/53 , G01N33/74
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.
摘要翻译：公开了用于鉴定易于自发性早产的怀孕女性的方法。具体而言，公开了用于基于从怀孕女性获得的样品中的类固醇比率来鉴定对自发性早产易感的怀孕女性的方法。

10. 发明申请

WO2017112904A1 INHIBITORS OF GLUCOCORTICOID RECEPTOR 审中-公开
标题翻译：糖皮质激素受体的抑制剂
公开(公告)号：WO2017112904A1
公开(公告)日：2017-06-29
申请号：PCT/US2016/068435
申请日：2016-12-22
申请人： ORIC PHARMACEUTICALS, INC.
发明人： SUN, Daqing , MCGEE, Lawrence R. , DU, Xiaohui , ZHU, Liusheng , YAN, Xuelei , REW, Yosup , EKSTEROWICZ, John , MEDINA, Julio C. , ZHOU, Haiying , BALBAS, Minna Delarae , FANTIN, Valeria R.
IPC分类号： C07J1/00 , C07J31/00 , C07J41/00 , C07J43/00 , C07J51/00 , A61K31/565 , A61K31/567 , A61K31/58
CPC分类号： A61K31/565 , A61K31/567 , A61K31/58 , C07B2200/05 , C07J1/0096 , C07J17/00 , C07J21/006 , C07J31/006 , C07J41/0083 , C07J41/0094 , C07J43/003 , C07J71/001
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.
摘要翻译：本发明一般涉及用于治疗癌症和皮质醇增多症的组合物和方法。本文提供取代的甾族衍生物化合物和包含所述化合物的药物组合物主题化合物和组合物可用于抑制糖皮质激素受体。此外，主题化合物和组合物可用于治疗癌症和皮质醇增多症。

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