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1. 发明授权

US10376514B2 Therapeutic thiophene-, furan-, and pyridine-fused azolopyrimidin-5-(6H)-ones 有权
公开(公告)号：US10376514B2
公开(公告)日：2019-08-13
申请号：US16164726
申请日：2018-10-18
申请人： Dart Neuroscience (Cayman) Ltd.
发明人： Bryan Branstetter , James Breitenbucher , Brian Dyck , Laurent Gomez , Andrew Richard Hudson , Tami Jo Marrone , Marco Peters , Troy Vickers , Michael I. Weinhouse
IPC分类号： C07D495/14 , C07D495/22 , C07D471/14 , C07D471/22 , C07D487/14 , C07D487/22 , C07D491/22 , A61K31/519 , C07D498/08 , C07D491/147 , C07D491/107 , C07D519/00 , C07D495/12 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/551 , A61K31/553 , A61K31/5386 , A61P25/00 , A61P9/00
摘要： Described herein are compounds of Formula I and Formula II, methods of their synthesis, compositions comprising the compounds, and use of the compounds and compositions in treating numerous diseases and disorders, including cognitive deficits associated with CNS diseases and disorders.

2. 发明授权

US5286858A Optically active thienotriazolodiazepine compounds 失效
标题翻译：光学活性噻吩并三唑并噻嗪化合物
公开(公告)号：US5286858A
公开(公告)日：1994-02-15
申请号：US774945
申请日：1991-10-11
申请人： Minoru Moriwaki , Syuji Yuasa , Hiroyuki Kitani , Michio Terasawa
发明人： Minoru Moriwaki , Syuji Yuasa , Hiroyuki Kitani , Michio Terasawa
IPC分类号： A61K31/55 , A61K31/00 , A61K31/554 , A61P7/02 , A61P9/00 , A61P11/00 , A61P29/00 , A61P37/00 , A61P37/08 , A61P43/00 , C07D495/14 , C07D495/12
CPC分类号： C07D495/14
摘要： Stable crystals of an acid addition salt of an optically active thienotriazolodiazepine compound or its hydrate of the formula ##STR1## wherein R.sup.1 is hydrogen, R.sup.2 is 2-phenylethyl substituted by alkyl having 1 to 5 carbon atoms, 2-morpholinocarbonylethyl or alkyl having 6 to 12 carbon atoms, or R.sup.1 and R.sup.2 may combinedly form a saturated 5-membered ring having one substituent selected from the group consisting of morpholinomethyl, morpholinocarbonyl and N,N-dipropylcarbamoyl, R.sup.3 is halogen, alkyl having 1 to 5 carbon atoms or alkoxy having 1 to 5 carbon atoms, R.sup.4 is trifluoromethyl or alkyl having 1 to 5 carbon atoms, R.sup.5 is hydrogen or methyl, m is 1-2, and n is 0-2. The present invention provides optically active thienotriazolodiazepine compounds having strong PAF-antagonistic activity as markedly stable crystals which are excellent in crystalline property, permit purification by recrystallization, and have high chemical purity and optical purity, thereby rendering industrial large-scale synthesis attainable. In addition, crystallization thereof facilitates medicinal standardization and pharmaceutical formulation.
摘要翻译：光学活性噻吩并三唑并噻嗪类化合物或其水合物（*化学结构*）（I）的酸加成盐的稳定晶体，其中R 1为氢，R 2为被具有1至5个碳原子的烷基取代的2-苯乙基，吗啉代羰基乙基或具有6至12个碳原子的烷基，或者R 1和R 2可以组合形成具有一个选自吗啉代甲基，吗啉代羰基和N，N-二丙基氨基甲酰基的一个取代基的饱和五元环，R 3是卤素， 5个碳原子或具有1至5个碳原子的烷氧基，R4是三氟甲基或具有1-5个碳原子的烷基，R5是氢或甲基，m是1-2，n是0-2。本发明提供具有优异结晶性的显色稳定结晶的具有强PAF拮抗作用的光学活性噻吩并三唑并氮杂化合物，可以通过重结晶进行纯化，化学纯度高，光学纯度高，从而可实现工业化的大规模合成。此外，其结晶有助于药物标准化和药物制剂。

3. 发明申请

US20230135894A1 MK2 DEGRADERS AND USES THEREOF 有权
公开(公告)号：US20230135894A1
公开(公告)日：2023-05-04
申请号：US17855336
申请日：2022-06-30
申请人： Kymera Therapeutics, Inc.
发明人： Bin YANG , Matthew M. WEISS , Xiao ZHU , Huijun DONG , Isaac MARX
IPC分类号： C07D471/22 , C07D405/14 , C07D495/12 , C07D401/04 , C07D519/00 , C07D491/048 , C07D471/14 , C07D471/04
摘要： The present invention provides compounds, compositions thereof, and methods of using the same.

4. 发明申请

US20210387998A1 TRICYCLIC FUSED THIOPHENE DERIVATIVES AS JAK INHIBITORS 有权
公开(公告)号：US20210387998A1
公开(公告)日：2021-12-16
申请号：US17400861
申请日：2021-08-12
申请人： Incyte Corporation , Incyte Holdings Corporation
发明人： Yun-Long Li , Wenyu Zhu , Song Mei , Joseph Glenn
IPC分类号： C07D495/14 , C07D495/12 , A61K31/437
摘要： The present invention provides tricyclic fused thiophene derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.

5. 发明授权

US10370387B2 Tricyclic fused thiophene derivatives as JAK inhibitors 有权
公开(公告)号：US10370387B2
公开(公告)日：2019-08-06
申请号：US15874140
申请日：2018-01-18
申请人： Incyte Corporation , Incyte Holdings Corporation
发明人： Yun-Long Li , Wenyu Zhu , Song Mei
IPC分类号： A61K31/437 , C07D495/12 , C07D495/14
摘要： The present invention provides tricyclic fused thiophene derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.

6. 发明授权

US09320741B2 Compositions and methods for treating neoplasia, inflammatory disease and other disorders 有权
公开(公告)号：US09320741B2
公开(公告)日：2016-04-26
申请号：US14502840
申请日：2014-09-30
申请人： Dana-Farber Cancer Institute, Inc.
发明人： James Elliott Bradner , Jun Qi
IPC分类号： A61K31/5517 , A61K31/551 , C07D487/04 , C07D495/12 , C07D519/00 , C07D495/14
CPC分类号： C07D495/14 , A61K31/551 , A61K31/5517 , C07D487/04 , C07D495/12 , C07D519/00 , Y02A50/411
摘要： The invention features compositions and methods for treating or preventing a neoplasia. More specifically, the invention provides compositions and methods for disrupting the interaction of a BET family polypeptide comprising a bromodomain with chromatin (e.g., disrupting a bromodomain interaction with an acetyl-lysine modification present on a histone N-terminal tail).

7. 发明申请

US20070160871A1 MATERIAL FOR ORGANIC ELECTROLUMINESCENT DEVICE AND ORGANIC ELECTROLUMINESCENT DEVICE 审中-公开
标题翻译：有机电致发光器件和有机电致发光器件的材料
公开(公告)号：US20070160871A1
公开(公告)日：2007-07-12
申请号：US11616545
申请日：2006-12-27
申请人： Hironobu Morishita , Chishio Hosokawa , Hisayuki Kawamura
发明人： Hironobu Morishita , Chishio Hosokawa , Hisayuki Kawamura
IPC分类号： H01L51/54 , C07D487/12 , C07D495/12
CPC分类号： H01L51/0072 , C07D335/12 , C07D487/04 , C09K11/06 , C09K2211/1011 , C09K2211/1044 , H01L51/0059 , H01L51/006 , H01L51/0081 , H01L51/5088 , H05B33/14
摘要： A material for an organic electroluminescent device represented by the following formula (I): wherein X1 and X2 are independently one of specific divalent groups; Y1 to Y4 are independently a carbon atom or a nitrogen atom; R1 to R4 are independently a hydrogen atom, an alkyl group, an aryl group, a heterocyclic group, a halogen atom, a fluoroalkyl group, or a cyano group; and R1 and R2, and R3 and R4 may be bonded together to form a ring, respectively.
摘要翻译：由下式（I）表示的有机电致发光器件的材料：其中X 1和X 2独立地是特定二价基团之一; Y 1至Y 4独立地为碳原子或氮原子; R 1至R 4独立地为氢原子，烷基，芳基，杂环基，卤素原子，氟代烷基或氰基; R 1和R 2，R 3和R 4和R 4可以结合在一起形成环，分别。

8. 发明申请

US20050004099A1 Spiroazabicyclic heterocyclic compounds 失效
标题翻译：螺环双环杂环化合物
公开(公告)号：US20050004099A1
公开(公告)日：2005-01-06
申请号：US10801085
申请日：2004-03-15
申请人： Eifion Phillips , Robert Mack , John Macor , Simon Semus
发明人： Eifion Phillips , Robert Mack , John Macor , Simon Semus
IPC分类号： C07D491/22 , A61K20060101 , A61K31/395 , A61K31/435 , A61K31/4353 , A61K31/4355 , A61K31/436 , A61K31/4365 , A61K31/438 , A61K31/439 , A61K31/44 , A61K31/444 , A61K31/4738 , A61K31/4745 , A61K31/496 , A61K31/5377 , A61K31/695 , A61P20060101 , A61P1/00 , A61P1/04 , A61P25/00 , A61P25/04 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/34 , A61P43/00 , C07D20060101 , C07D491/12 , C07D491/20 , C07D495/12 , C07D499/21 , C07F5/02 , C07F7/18 , A61K31/55 , C07D487/14
CPC分类号： C07D491/22
摘要： A pharmaceutical composition comprising a compound of formula wherein n, m, p, X, Y, W, A, G and D are as defined in the specification, enantiomers thereof, or pharmaceutically acceptable salts thereof, its use in therapy, especially in the treatment or prophylaxis of psychotic disorders and intellectual impairment disorders.
摘要翻译：一种药物组合物，其包含下式化合物其中n，m，p，X，Y，W，A，G和D如说明书中所定义，其对映体或其药学上可接受的盐，其用于治疗，治疗或预防精神病和智力障碍。

9. 发明授权

US4816461A 7,8,9,10-tetrahydrothieno[3,2-e]pyrido[4,3-b] indole, a process for their preparation and medicaments containing them 失效
标题翻译： 7,8,9,10-四氢噻吩并[3,2-e]吡啶并[4,3-b]吲哚，其制备方法和含有它们的药物
公开(公告)号：US4816461A
公开(公告)日：1989-03-28
申请号：US61255
申请日：1987-06-10
申请人： Peter-Rudolf Seidel , Gunter Schollnhammer
发明人： Peter-Rudolf Seidel , Gunter Schollnhammer
IPC分类号： C07D333/62 , A61K31/435 , A61K31/44 , A61P25/18 , A61P25/24 , A61P25/26 , C07C205/56 , C07D333/54 , C07D333/66 , C07D495/12 , C07D495/14
CPC分类号： C07D333/54 , C07C205/45 , C07C205/56 , C07C323/00 , C07D495/14
摘要： The invention concerns the provision of 7,8,9,10-tetrahydrothieno[3,2-e]pyrido[4,3-b] indoles, useful, inter alia, as antidepressants, and intermediates for the preparation thereof. Also included in the invention are compositions containing said indoles and methods for the use of said indoles and indole compositions as antidepressants.
摘要翻译：本发明涉及提供7,8,9,10-四氢噻吩并[3,2-e]吡啶并[4,3-b]吲哚，尤其可用作抗抑郁剂，以及其制备的中间体。本发明还包括含有所述吲哚的组合物和使用所述吲哚和吲哚组合物作为抗抑郁药的方法。

10. 发明授权

US4496725A Substituted 1,2,3-triazino[4',5':4,5]-thieno[2,3-B]quinolin-4(3H)-ones 失效
标题翻译：取代的1,2,3-三嗪并[4'，5'：4,5]噻吩并[2,3-b]喹啉-4（3H） - 酮
公开(公告)号：US4496725A
公开(公告)日：1985-01-29
申请号：US496800
申请日：1983-05-23
申请人： James R. McCarthy , Paul J. Widner
发明人： James R. McCarthy , Paul J. Widner
IPC分类号： A61K31/53 , A61P37/08 , C07D215/20 , C07D215/54 , C07D495/04 , C07D495/14 , C07D495/22 , C07D495/12
CPC分类号： C07D495/04 , C07D215/20 , C07D215/54 , C07D495/14
摘要： Substituted 1,2,3-triazino[4',5':4,5]thieno[2,3-b]quinolin-4(3H)-ones useful as antiallergic agents are described herein. The compounds are prepared by the reaction of an appropriate substituted 3-aminothieno[2,3-b]quinoline-2-carboxamide with sodium nitrite in an acid such as acetic acid.
摘要翻译：本文描述了可用作抗过敏剂的取代的1,2,3-三嗪[4'，5'：4,5]噻吩并[2,3-b]喹啉-4（3H） - 酮。通过在酸如乙酸中将适当的取代的3-氨基噻吩并[2,3-b]喹啉-2-甲酰胺与亚硝酸钠反应来制备化合物。

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