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1. 发明申请

US20220144821A1 AKT INHIBITOR 有权
公开(公告)号：US20220144821A1
公开(公告)日：2022-05-12
申请号：US17426047
申请日：2020-01-22
申请人： Nanjing Chia Tai Tianqing Pharmaceutical Co., Ltd.
发明人： Changyou Ma , He Tian , Jie An , Jianliang Zhao , Donghui Chen , Jian Wu , Dan Xu , Chunxia Zhu , Zhoushan Tian
IPC分类号： C07D471/04 , C07D519/00 , C07D475/06 , C07D498/04
摘要： The present invention discloses an AKT inhibitor, and specifically relates to a compound represented by formula I or a pharmaceutically acceptable salt thereof. The present invention further provides a preparation method thereof, and the use thereof in prevention and/or treatment of a disease mediated by AKT protein kinase.

2. 发明申请

US20220009928A1 SOLID FORMS OF A TOLL-LIKE RECEPTOR MODULATOR 有权
公开(公告)号：US20220009928A1
公开(公告)日：2022-01-13
申请号：US17353462
申请日：2021-06-21
申请人： GILEAD SCIENCES, INC.
发明人： Krista Marie Diaz , Patricia Andres , Valeriya N. Smolenskaya
IPC分类号： C07D475/06 , A61K31/519 , C07D487/04 , A61K45/06
摘要： The present invention provides crystalline forms, solvates and hydrates of 4-amino-2-butoxy-8-(3-(pyrrolidin-1-ylmethyl)benzyl)-7,8-dihydropteridin-6(5H)-one, and methods of making.

3. 发明申请

US20210292327A1 DEUTERATED TOLL-LIKE RECEPTOR MODULATORS 有权
公开(公告)号：US20210292327A1
公开(公告)日：2021-09-23
申请号：US15753845
申请日：2016-08-24
申请人： Gilead Sciences, Inc.
发明人： Steven S. Bondy , Ryan McFadden
IPC分类号： C07D475/06
摘要： The present invention provides deuterated analogs of toll like receptor modulator compounds having the structures of formula (X) or (Y), processes for making those analogs, and their therapeutic methods of use.

4. 发明授权

US10508117B2 Solid forms of a toll-like receptor modulator 有权
公开(公告)号：US10508117B2
公开(公告)日：2019-12-17
申请号：US16229460
申请日：2018-12-21
申请人： GILEAD SCIENCES, INC.
发明人： Patricia Andres , Krista Marie Diaz , Valeriya N. Smolenskaya
IPC分类号： C07D401/10 , C07D475/06 , C07D487/04 , A61K31/519 , A61K45/06
摘要： The present invention provides crystalline forms, solvates and hydrates of 4-amino-2-butoxy-8-(3-(pyrrolidin-1-ylmethyl)benzyl)-7,8-dihydropteridin-6(5H)-one, and methods of making.

5. 发明授权

US10144736B2 Substituted pteridines useful for the treatment and prevention of viral infections 有权
公开(公告)号：US10144736B2
公开(公告)日：2018-12-04
申请号：US12374457
申请日：2007-07-20
申请人： Piet AndréMaurits Maria Herdewijn , Steven Cesar Alfons De Jonghe , William John Watkins , Lee Shun Chong
发明人： Piet AndréMaurits Maria Herdewijn , Steven Cesar Alfons De Jonghe , William John Watkins , Lee Shun Chong
IPC分类号： C07D487/00 , C07D475/02 , C07D475/00 , C07D475/04 , C07D475/06 , C07D475/08
摘要： The invention provides 4,6-di- and 2,4,6-tri-substituted pteridine derivatives with a specific substitution pattern which exhibit a significant and selective activity against certain types of viral infections, in particular selectively inhibit replication of Flaviridae such as the hepatitis C virus, and are useful for the prevention and treatment of such viral infections.

6. 发明授权

US09327006B2 Extraction of B-vitamins from plant matter 有权
标题翻译：从植物物质中提取B族维生素
公开(公告)号：US09327006B2
公开(公告)日：2016-05-03
申请号：US14131262
申请日：2012-07-30
申请人： Ramaswamy Rajendran , Kamala Rajendran
发明人： Ramaswamy Rajendran , Kamala Rajendran
IPC分类号： A01N65/00 , A61K36/752 , C07D475/06 , A61K36/53 , A61K36/61
CPC分类号： A61K36/752 , A61K31/16 , A61K31/4406 , A61K31/4415 , A61K31/51 , A61K31/519 , A61K31/525 , A61K36/53 , A61K36/61 , C07D415/00 , C07D475/06 , C07D475/14 , C07H1/08 , C07H23/00
摘要： A process for the extraction of the B group of vitamins from a first plant matter is disclosed wherein, prior to the said extraction operation, the first plant matter is treated with a second plant matter comprising acidic compounds. The acidification converts the vitamins into more water-soluble forms and increases the yield thereof. In one example, the first plant matter comprises guava fruit matter, holy basil leaves and lemon peels, the two last-mentioned plant species being the source of the acidic compounds. The vitamins extracted and the proportions thereof may be controlled by suitable choice of the plant species constituting the first and second plant matters and their quantities, such as to give a substantially ready formulation conforming to RDA values or other requirements. The vitamins extracted are B1, B2, B3, B5, B6 and B9, the above combination of plant matters giving a higher yield than others. The process is of general applicability to other plant constituents.
摘要翻译：公开了从第一植物物质中提取B族维生素的方法，其中在所述提取操作之前，用包含酸性化合物的第二植物物质处理第一植物物质。酸化将维生素转化为更多的水溶性形式并提高其产率。在一个实例中，第一植物物质包括番石榴果实物质，圣罗勒叶和柠檬皮，两种最后提到的植物物种是酸性化合物的来源。提取的维生素及其比例可以通过合适选择构成第一和第二植物物质及其数量的植物物种来进行控制，例如给出符合RDA值或其它要求的基本准备的制剂。提取的维生素是B1，B2，B3，B5，B6和B9，上述植物物质组合比其他物质产量高。该方法对其他植物成分具有普遍适用性。

7. 发明申请

US20160108045A1 SOLID FORMS OF A TOLL-LIKE RECEPTOR MODULATOR 有权
标题翻译：类似感受器调制器的固体形式
公开(公告)号：US20160108045A1
公开(公告)日：2016-04-21
申请号：US14853855
申请日：2015-09-14
申请人： Gilead Sciences, Inc.
发明人： Patricia Andres , Brandon Heath Brown , Krista Marie Diaz , Yoo Joong Kim , Paul Roethle , Fang Wang , Valeriya Smolenskaya
IPC分类号： C07D475/06 , A61K45/06 , A61K31/519
CPC分类号： C07D475/06 , A61K31/519 , A61K45/06 , C07D487/04 , A61K2300/00
摘要： The present invention provides crystalline forms, solvates and hydrates of 4-amino-2-butoxy-8-(3-(pyrrolidin-1-ylmethyl)benzyl)-7,8-dihydropteridin-6(5H)-one, and methods of making.
摘要翻译：本发明提供4-氨基-2-丁氧基-8-（3-（吡咯烷-1-基甲基）苄基）-7,8-二氢蝶啶-6（5H） - 酮的结晶形式，溶剂合物和水合物，以及制造。

8. 发明授权

US08809527B2 Modulators of toll-like receptors 有权
标题翻译： toll样受体的调节剂
公开(公告)号：US08809527B2
公开(公告)日：2014-08-19
申请号：US14089633
申请日：2013-11-25
申请人： Gilead Sciences, Inc.
发明人： Manoj C. Desai , Randall L. Halcomb , Paul Hrvatin , Hon Chung Hui , Ryan McFadden , Paul A. Roethle , Hong Yang
IPC分类号： C07D475/06 , C07D475/08 , C07D475/12 , C07D487/04
CPC分类号： A61K31/519 , A61K31/527 , A61K31/5377 , A61K31/551 , A61K31/573 , A61K31/683 , A61K31/7056 , A61K31/7072 , A61K31/708 , A61K38/16 , A61K38/21 , A61K38/212 , A61K45/06 , C07D403/12 , C07D475/06 , C07D475/08 , C07D475/10 , C07D475/12 , C07D487/04 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/391 , Y02A50/393 , Y02A50/395
摘要： Provided are modulators of TLRs of Formula II: pharmaceutically acceptable salts thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
摘要翻译：提供了式II的TLR的调节剂：其药学上可接受的盐，含有这些化合物的组合物和包括施用这些化合物的治疗方法。

9. 发明授权

US06875868B2 Pteridine compounds for the treatment of psoriasis 失效
公开(公告)号：US06875868B2
公开(公告)日：2005-04-05
申请号：US10204814
申请日：2001-02-20
申请人： Roger Bonnert , Stewart Gardiner , Fraser Hunt , Iain Walters
发明人： Roger Bonnert , Stewart Gardiner , Fraser Hunt , Iain Walters
IPC分类号： C07D487/08 , A61K31/439 , A61K31/4427 , A61K31/4709 , A61K31/519 , A61K31/5377 , A61K31/542 , A61P1/00 , A61P7/00 , A61P9/10 , A61P11/06 , A61P17/06 , A61P19/02 , A61P25/00 , A61P25/04 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/34 , A61P29/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07D453/02 , C07D453/06 , C07D475/00 , C07D475/06 , C07D513/04 , C07D487/04
CPC分类号： C07D513/04 , C07D453/02 , C07D475/06
摘要： The invention provides pteridine compounds of formula (I), processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy. Formula (I) in which A is a group of formula (a) or (b).

10. 发明授权

US06858612B1 Use of tetrahydropteridine derivatives as no synthase inhibitors 失效
标题翻译：四氢喋啶衍生物作为合成酶抑制剂的使用
公开(公告)号：US06858612B1
公开(公告)日：2005-02-22
申请号：US09357212
申请日：1999-07-20
申请人： Wolfgang Pfleiderer , Harald Schmidt , Rainer Henning
发明人： Wolfgang Pfleiderer , Harald Schmidt , Rainer Henning
IPC分类号： A61K31/505 , A61K31/519 , A61P7/00 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/28 , A61P43/00 , C07D475/04 , C07D475/06 , C07D475/08 , A61K31/495 , A61K31/50
CPC分类号： C07D475/08 , C07D475/04
摘要： The present invention relates to the use of pteridine derivatives of the formula I in which X is O or NH and R4, for example, is hydrogen, phenyl or the radical R4a—CH2— and R4a, for example, is hydrogen, (C1-C4)-alkylmercapto, the radical —NR11R12 or the radical —OR13, and in which R1, R2, R3, R5, R6, R7, R11, R12 and R13 have the meanings given in claim 1, which are nitric oxide synthase inhibitors, for the treatment of diseases which are caused by an increased nitric oxide level.
摘要翻译：本发明涉及式Iin的蝶啶衍生物，其中X为O或NH，R 4为例如氢，苯基或基团R 4a -CH 2 - 和R 4a的基团，用于例如，是氢，（C 1 -C 4） - 烷基巯基，基团-NR 11 R 12或基团-OR 13，其中R 1，R 2，R 3， R 5，R 6，R 7，R 11，R 12和R 13具有权利要求1中给出的含义，其为一氧化氮合酶抑制剂，用于治疗疾病这是由一氧化氮水平升高引起的。

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