-
公开(公告)号：US20170319695A1
公开(公告)日：2017-11-09
申请号：US15660114
申请日：2017-07-26
IPC分类号： A61K45/06 , C07J43/00 , C07J41/00 , C07J13/00 , C07J7/00 , C07J3/00 , C07J51/00 , A61K31/00 , A61K45/00
CPC分类号： A61K45/06 , A61K31/00 , A61K45/00 , C07J3/00 , C07J3/005 , C07J7/002 , C07J7/007 , C07J7/0085 , C07J7/009 , C07J9/00 , C07J13/007 , C07J41/0044 , C07J43/003 , C07J51/00
摘要： Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein , A, R1, R2, and R3 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, e.g., for treating a subject suffering from a disease or disorder described herein.
-
公开(公告)号：US09296780B2
公开(公告)日：2016-03-29
申请号：US14367886
申请日：2012-12-19
CPC分类号： C07J75/00 , C07J1/0011 , C07J1/0059 , C07J1/0081 , C07J1/0096 , C07J7/00 , C07J7/0055 , C07J7/0075 , C07J7/009 , C07J31/006 , C07J51/00
摘要： A process ethynylates 16-methylene-17-keto steroids to the corresponding 16-methylene-17α-ethynyl-17β-hydroxy steroids by treatment with silyl-protected lithium acetylides followed by further desilylation. The resulting products are useful intermediates in the preparation of several pharmaceutically active agents, such as e.g. Nestorone® or melengestrol acetate.
摘要翻译： 通过用甲硅烷基保护的乙炔化锂处理，然后进一步脱甲硅烷，将16-亚甲基-17-酮类固醇乙炔化为相应的16-亚甲基-17α-乙炔基-17β-羟基类固醇。 所得产物是制备几种药物活性剂的有用的中间体，例如 Nestorone®或醋酸美伦他林。
-
公开(公告)号：US20150005518A1
公开(公告)日：2015-01-01
申请号：US14367886
申请日：2012-12-19
CPC分类号： C07J75/00 , C07J1/0011 , C07J1/0059 , C07J1/0081 , C07J1/0096 , C07J7/00 , C07J7/0055 , C07J7/0075 , C07J7/009 , C07J31/006 , C07J51/00
摘要： A process ethynylates 16-methylene-17-keto steroids to the corresponding 16-methylene-17α-ethynyl-17β-hydroxy steroids by treatment with silyl-protected lithium acetylides followed by further desilylation. The resulting products are useful intermediates in the preparation of several pharmaceutically active agents, such as e.g. Nestorone® or melengestrol acetate.
摘要翻译： 通过用甲硅烷基保护的乙炔化锂处理，然后进一步脱甲硅烷，将16-亚甲基-17-酮类固醇乙炔化为相应的16-亚甲基-17α-乙炔基-17β-羟基类固醇。 所得产物是制备几种药物活性剂的有用的中间体，例如 Nestorone®或醋酸美伦他林。
-
公开(公告)号：US08716479B2
公开(公告)日：2014-05-06
申请号：US12810600
申请日：2008-12-24
申请人： Brian C. Austad , Andre Lescarbeau , Lin-Chen Yu
发明人： Brian C. Austad , Andre Lescarbeau , Lin-Chen Yu
IPC分类号： C07D471/02 , C07D311/96
CPC分类号： C07J7/009 , C07B2200/09 , C07D471/10 , C07D491/22 , C07J1/0011 , C07J5/0053 , C07J9/00 , C07J21/00 , C07J43/006 , C07J63/00 , C07J65/00 , C07J69/00 , C07J71/0005
摘要： The invention is directed to a method to reduce a C—C double bond of an enone of a steroidal compound to produce a mixture of β ketone product and α ketone product, comprising treating a solution or suspension of the steroidal compound in a solvent with hydrogen gas in the presence of a catalyst and a substituted pyridine.
摘要翻译： 本发明涉及一种降低甾族化合物的烯酮的C-C双键以产生“bgr”的混合物的方法。 酮产物和α-酮产物，包括在催化剂和取代的吡啶的存在下，用氢气处理溶剂中的甾族化合物的溶液或悬浮液。
-
5.发明申请Preparations of Hydrophobic Therapeutic Agents, Methods of Manufacture and Use Thereof 有权疏水治疗剂的制备方法，制造和使用方法公开(公告)号：US20130303502A1
公开(公告)日：2013-11-14
申请号：US13735973
申请日：2013-01-07
发明人： Thomas Cavanagh , Shikha P. Barman
IPC分类号： C07J3/00
CPC分类号： C07J7/009 , C07B2200/13 , C07J3/005 , C07J31/006 , C07J71/0005 , C07J71/0031 , Y10T428/2982
摘要： The present invention further provides method of preparing nanocrystals of a hydrophobic therapeutic agent such as fluticasone, pharmaceutical compositions (e.g., topical or intranasal compositions) thereof and methods for treating and/or preventing the signs and/or symptoms of disorders such as blepharitis, meibomian gland dysfunction or skin inflammation or a respiratory disease (e.g., asthma).
摘要翻译： 本发明还提供了制备疏水性治疗剂如氟替卡松，药物组合物（例如，局部或鼻内组合物）的纳米晶体的方法和用于治疗和/或预防诸如睑板炎，睑板炎 腺体功能障碍或皮肤炎症或呼吸系统疾病（如哮喘）。
-
公开(公告)号：US4588530A
公开(公告)日：1986-05-13
申请号：US502449
申请日：1983-06-09
申请人： Henry J. Lee
发明人： Henry J. Lee
CPC分类号： C07J7/0095 , C07J41/005 , C07J7/009
摘要： Derivatives of prednisolone of the formula ##STR1## wherein CR.sub.1 is C.dbd.O, .alpha.-HCOH, .beta.-HCOH, or a mixture of .alpha.-HCOH and .beta.-HCOH CR.sub.2 is HC(OH) OR.sub.6 or HCO when CR.sub.1 is C.dbd.O;CR.sub.2 is COOR.sub.3 or CONHR.sub.4 when CR.sub.1 is .alpha.-HCOH, .beta.-HCOH, or a mixture of .alpha.-HCOH and .beta.-HCOH:R.sub.3 is alkyl of 1-5 carbon atoms;R.sub.4 is alkyl of 1-5 carbon atoms, benzyl, or phenethyl;R.sub.5 is hydrogen, acetyl, or benzoyl;R.sub.6 is alkyl of 1-5 carbon atoms;R.sub.7 is .alpha.- or .beta.-position of hydrogen, hydroxyl, methyl, acetate esters of 1-5 carbon atoms, or alkoxy of 1-5 carbon atoms; andX and Y are hydrogen, halogen or methyl;and process for preparing these compounds. The compounds are useful as anti-inflammatory agents which have reduced side effects.
摘要翻译： 其中CR1为C = O，α-HCOH，β-HCOH或α-HCOH和β-HCOH CR2的混合物的泼尼松龙衍生物为CR（C = O）时为HC（OH）OR 6或HCO ; 当CR 1为α-HCOH，β-HCOH或α-HCOH和β-HCOH的混合物时，CR2为COOR3或CONHR4：R3为1-5个碳原子的烷基; R4是1-5个碳原子的烷基，苄基或苯乙基; R5是氢，乙酰基或苯甲酰基; R6是1-5个碳原子的烷基; R7是1-5个碳原子的氢，羟基，甲基，乙酸酯或1-5个碳原子的烷氧基的α-或β-位; X和Y是氢，卤素或甲基; 和这些化合物的制备方法。 这些化合物可用作具有减少的副作用的抗炎剂。
-
公开(公告)号：US2389325A
公开(公告)日：1945-11-20
申请号：US42766942
申请日：1942-01-21
申请人： TADEUS RELCHSTEIN
发明人： TADEUS RELCHSTEIN
-
公开(公告)号：US20190169226A1
公开(公告)日：2019-06-06
申请号：US16269779
申请日：2019-02-07
CPC分类号： C07J41/005 , C07J1/0011 , C07J5/0015 , C07J7/002 , C07J7/007 , C07J7/0085 , C07J7/009 , C07J13/007 , C07J17/00 , C07J21/00 , C07J21/006 , C07J21/008
摘要： Described herein are steroids of Formula (I): and pharmaceutically acceptable salts thereof; wherein R1, R2a, R2b, R3, R4, R5a, R5b, R6, and Z are 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.
-
9.发明申请公开(公告)号：US20180022775A1
公开(公告)日：2018-01-25
申请号：US15660470
申请日：2017-07-26
CPC分类号： C07J7/009 , C07B2200/13 , C07J3/005 , C07J31/006 , C07J71/0005 , C07J71/0031 , Y10T428/2982
摘要： The present invention further provides method of preparing nanocrystals of a hydrophobic therapeutic agent such as fluticasone or triamcinolone, pharmaceutical compositions (e.g., topical or intranasal compositions) thereof and methods for treating and/or preventing the signs and/or symptoms of disorders such as blepharitis, meibomian gland dysfunction or skin inflammation or a respiratory disease (e.g., asthma).
-
公开(公告)号：US20170340754A1
公开(公告)日：2017-11-30
申请号：US15523325
申请日：2015-10-29
发明人： Zheng-Yi Chen , David Liu
IPC分类号： A61K48/00 , C07J7/00 , C07K7/06 , C12N9/22 , C07K7/08 , C12N15/11 , C12N9/52 , C07K19/00 , C07K14/47 , C07K14/46 , A61K9/127 , C12N15/113 , C12N2310/20
CPC分类号： A61K48/0008 , A61K9/1272 , A61K38/00 , A61K38/10 , A61K47/64 , A61K47/6911 , A61K48/0075 , A61K48/0083 , C07J7/009 , C07K7/06 , C07K7/08 , C07K14/463 , C07K14/47 , C07K19/00 , C07K2319/06 , C07K2319/21 , C07K2319/33 , C07K2319/60 , C12N5/062 , C12N9/00 , C12N9/22 , C12N9/52 , C12N15/11 , C12N15/113 , C12N15/87 , C12N15/88 , C12N15/907 , C12N2310/20 , C12N2310/3513 , C12N2510/00 , C12Y304/2207
摘要： Compositions are described for direct protein delivery into multiple cell types in the mammalian inner ear. The compositions are used to deliver protein(s) (such as gene editing factors) editing of genetic mutations associated with deafness or associated disorders thereof. The delivery of genome editing proteins for gene editing and correction of genetic mutations protect or restore hearing from genetic deafness. Methods of treatment include the intracellular delivery of these molecules to a specific therapeutic target.
-
-
-
-
-
-
-
-
-
搜索结果
49 条记录 (耗时 0.032 秒)