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1. 发明申请

US20170360784A1 TRIZOL-1-OL ANALOGS ANTI-RETROVIRAL LATENCY DRUGS 审中-公开
公开(公告)号：US20170360784A1
公开(公告)日：2017-12-21
申请号：US15639575
申请日：2017-06-30
申请人： University of Utah Research Foundation
发明人： Vincente Planelles , Alberto Bosque-Pardos , Chris M. Ireland , Ryan Van Wagoner , Mary Kay Harper-Ireland , John Alan Maschek
IPC分类号： A61K31/501 , C07D403/04 , C07D253/08 , C07D249/18 , C07D231/54 , A61K31/416 , A61K45/06 , A61K31/53 , A61K31/437 , A61K31/4192 , C07D471/04 , C07D249/04
CPC分类号： A61K31/501 , A61K31/416 , A61K31/4192 , A61K31/437 , A61K31/53 , A61K45/06 , C07D231/54 , C07D249/04 , C07D249/18 , C07D253/08 , C07D403/04 , C07D471/04 , A61K2300/00
摘要： In one aspect, the invention relates to triazol-1-ol compounds, analogs thereof, compositions comprising same, and methods of using same, alone or in combination with other agents, to reactivate latent retroviruses, and more particularly to reactivate latent HIV-1. Such compounds, compositions, and methods can be used, for example, in connection with diagnosing and/or treating a retrovirus, and more specifically HIV-1. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

2. 发明申请

US20170355664A1 NEPRILYSIN INHIBITORS 审中-公开
公开(公告)号：US20170355664A1
公开(公告)日：2017-12-14
申请号：US15581327
申请日：2017-04-28
申请人： THERAVANCE BIOPHARMA R&D IP, LLC
发明人： Melissa Fleury , Adam D. Hughes
IPC分类号： C07C229/22 , A61K31/4439 , C07D401/04 , C07D405/14 , C07C271/22 , C07D249/12 , C07D231/20 , C07D261/18 , A61K31/4192 , A61K31/415 , C07D257/04 , A61K31/42 , C07D207/26 , A61K31/675 , A61K31/41 , A61K31/4155 , A61K45/06 , C07D249/18 , C07F9/6503 , C07D249/04 , C07D263/38 , A61K31/4196 , C07D253/08 , C07D231/18 , C07D405/12 , C07D231/14
CPC分类号： C07C229/22 , A61K31/41 , A61K31/415 , A61K31/4155 , A61K31/4192 , A61K31/4196 , A61K31/42 , A61K31/4439 , A61K31/675 , A61K45/06 , C07C271/22 , C07D207/26 , C07D231/14 , C07D231/18 , C07D231/20 , C07D249/04 , C07D249/12 , C07D249/18 , C07D253/08 , C07D257/04 , C07D261/18 , C07D263/38 , C07D401/04 , C07D405/12 , C07D405/14 , C07F9/65031
摘要： In one aspect, the invention relates to compounds having the formula XII: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.

3. 发明授权

US09670140B2 Neprilysin inhibitors 有权
公开(公告)号：US09670140B2
公开(公告)日：2017-06-06
申请号：US14792810
申请日：2015-07-07
申请人： Adam D. Hughes
发明人： Adam D. Hughes
IPC分类号： C07C229/22 , C07C271/22 , C07D249/18 , A61K31/4192 , A61K45/06 , C07D231/20 , A61K31/415 , C07D405/12 , A61K31/4155 , A61K31/4439 , C07D401/04 , C07D405/14 , C07D231/14 , C07D261/18 , A61K31/42 , C07D249/04 , C07D249/12 , A61K31/4196 , C07D257/04 , A61K31/41 , A61K31/675 , C07F9/6503 , C07D231/18 , C07D253/08 , C07D207/26 , C07D263/38
CPC分类号： C07C229/22 , A61K31/41 , A61K31/415 , A61K31/4155 , A61K31/4192 , A61K31/4196 , A61K31/42 , A61K31/4439 , A61K31/675 , A61K45/06 , C07C271/22 , C07D207/26 , C07D231/14 , C07D231/18 , C07D231/20 , C07D249/04 , C07D249/12 , C07D249/18 , C07D253/08 , C07D257/04 , C07D261/18 , C07D263/38 , C07D401/04 , C07D405/12 , C07D405/14 , C07F9/65031
摘要： In one aspect, the invention relates to compounds having the formula XII: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.

4. 发明申请

US20170095480A1 4-OXO-3,4-DIHYDRO-1,2,3-BENZOTRIAZINE AS MODULATORS OF GPR139 有权
公开(公告)号：US20170095480A1
公开(公告)日：2017-04-06
申请号：US15382490
申请日：2016-12-16
申请人： Takeda Pharmaceutical Company Limited
发明人： Stephen Hitchcock , Betty Lam , Holger Monenschein , Holly Reichard
IPC分类号： A61K31/53
CPC分类号： A61K31/53 , C07D253/08
摘要： The present invention provides a method for treating a disease, disorder or condition associated with GPR139 using compounds of formula 1: which are agonists of GPR139, certain compounds encompassed by formula 1, pharmaceutical compositions thereof, processes for making the compounds, and intermediates thereof.

5. 发明申请

US20170022171A1 2,5-DISUBSTITUTED CYCLOPENTANECARBOXYLIC ACIDS AND THEIR USE 审中-公开
标题翻译： 2,5-DISUBSTITUTED CYPOPENTANECARBOXYLIC ACIDS AND THEE USE
公开(公告)号：US20170022171A1
公开(公告)日：2017-01-26
申请号：US15301392
申请日：2015-03-31
申请人： Bayer Pharma Aktiengesellschaft
发明人： Hartmut BECK , Volkhart Min-Jian LI , Yolanda CANCHO GRANDE , Andreas TIMMERMANN , Dirk BROHM , Hannah JÖRISSEN , Pamela BOGNER , Michael GERISCH , Dieter LANG
IPC分类号： C07D253/08 , A61K31/53 , C07D413/12 , A61K45/06
CPC分类号： C07D253/08 , A61K31/53 , A61K45/06 , C07D413/12
摘要： The present application relates to novel 2,5-disubstituted cyclopentanecarboxylic acid derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of respiratory, pulmonary and cardiovascular disorders.
摘要翻译：本申请涉及新的2,5-二取代的环戊烷羧酸衍生物，其制备方法，单独使用或组合用于治疗和/或预防疾病及其用于生产用于治疗和/ 或预防疾病，特别是用于治疗和/或预防呼吸，肺和心血管疾病。

6. 发明申请

US20160340323A1 AZAQUINAZOLINE CARBOXAMIDE DERIVATIVES 审中-公开
公开(公告)号：US20160340323A1
公开(公告)日：2016-11-24
申请号：US15227638
申请日：2016-08-03
申请人： Merck Patent GmbH
发明人： Bayard R. HUCK , Ruoxi LAN , Justin POTNICK , Lizbeth Celeste DESELM , Mark W. CRONIN, JR. , Constantin NEAGU , Xiaoling CHEN , Roch BOIVIN , Theresa L. JOHNSON , Andreas GOUTOPOULOS
IPC分类号： C07D253/08 , C07D403/12 , C07D401/12
CPC分类号： C07D253/08 , A61K31/519 , A61K31/53 , A61K45/06 , C07D401/12 , C07D403/12 , C07D471/04
摘要： Novel azaquinazoline carboxamide derivatives of formula (I) wherein W1, W2, W3, W4, R1, R2, R3 and m which are defined above, are p70S6K inhibitor, and can be employed, inter alia, for the treatment of hyperproliferative disorders.
摘要翻译：其中上述定义的W1，W2，W3，W4，R1，R2，R3和m是p70S6K抑制剂，并且可以用于治疗过度增殖性疾病。

7. 发明申请

US20160250233A1 ANTIVIRAL DRUGS FOR TREATMENT OR PREVENTION OF DENGUE INFECTION 审中-公开
标题翻译：用于治疗或预防登革热感染的药物
公开(公告)号：US20160250233A1
公开(公告)日：2016-09-01
申请号：US15148241
申请日：2016-05-06
申请人： Siga Technologies, Inc.
发明人： Chelsea OLSEN , Robert JORDAN , Dongcheng DAI , Tove BOLKEN , Dennis E. HRUBY
IPC分类号： A61K31/635 , A61K31/18 , A61K31/53 , A61K31/517 , A61K31/63 , A61K9/00
CPC分类号： A61K31/635 , A61K9/0019 , A61K31/18 , A61K31/473 , A61K31/502 , A61K31/517 , A61K31/519 , A61K31/522 , A61K31/53 , A61K31/63 , C07C311/46 , C07D221/14 , C07D237/32 , C07D239/88 , C07D239/96 , C07D241/44 , C07D253/08 , C07D401/12 , C07D403/06 , C07D405/12 , C07D409/12 , C07D417/12 , C07D473/08 , C07D491/048 , C07D495/04 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/393 , Y02A50/395
摘要： Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.
摘要翻译：公开了通过施用治疗有效量的某些化合物来治疗病毒感染的化合物，方法和药物组合物。还公开了制备化合物的方法和使用该化合物的方法及其药物组合物。特别地，公开了由黄病毒引起的病毒感染的治疗和预防，即包括但不限于登革病毒，西尼罗河病毒，黄热病病毒，日本脑炎病毒和蜱传脑炎病毒。

8. 发明授权

US08569304B2 Active esters of N-substituted piperazine acetic acids, including isotopically enriched versions thereof 有权
标题翻译： N-取代哌嗪乙酸的活性酯，包括同位素富集的形式
公开(公告)号：US08569304B2
公开(公告)日：2013-10-29
申请号：US12398920
申请日：2009-03-05
申请人： Subhakar Dey , Darryl J. C. Pappin , Subhasish Purkayastha , Sasi Pillai , James M. Coull
发明人： Subhakar Dey , Darryl J. C. Pappin , Subhasish Purkayastha , Sasi Pillai , James M. Coull
IPC分类号： A61K31/497 , C07D241/04 , C07D295/00 , C07D403/00
CPC分类号： C07D207/46 , C07D241/08 , C07D253/08 , C07D295/03 , C07D295/15
摘要： In some embodiments, this invention pertains to active esters of N-substituted piperazine acetic acid, including isotopically enriched versions thereof. In some embodiments, this invention pertains to methods for the preparation of active esters of N-substituted piperazine acetic acid, including isotopically enriched versions thereof.
摘要翻译：在一些实施方案中，本发明涉及N-取代的哌嗪乙酸的活性酯，包括同位素富集的形式。在一些实施方案中，本发明涉及制备N-取代的哌嗪乙酸的活性酯的方法，包括同位素富集的形式。

9. 发明授权

US07932388B2 Isotopically enriched N-substituted piperazines and methods for the preparation thereof 有权
标题翻译：同位素富集的N-取代哌嗪及其制备方法
公开(公告)号：US07932388B2
公开(公告)日：2011-04-26
申请号：US12001734
申请日：2007-12-11
申请人： Darryl J. C. Pappin , Sasi Pillai , James M. Coull
发明人： Darryl J. C. Pappin , Sasi Pillai , James M. Coull
IPC分类号： C07D241/04 , C07D295/067
CPC分类号： C07D207/46 , C07D241/08 , C07D253/08 , C07D295/03 , C07D295/15
摘要： In some embodiments, this invention pertains to isotopically enriched N-substituted piperazines. In some embodiments, this invention pertains to methods for the preparation of isotopically enriched N-substituted piperazines.
摘要翻译：在一些实施方案中，本发明涉及同位素富集的N-取代的哌嗪。在一些实施方案中，本发明涉及制备同位素富集的N-取代哌嗪的方法。

10. 发明授权

US07816521B2 1,2,4-benzotriazine-1,4-dioxides 有权
标题翻译： 1,2,4-苯并三嗪-1,4-二氧化物
公开(公告)号：US07816521B2
公开(公告)日：2010-10-19
申请号：US10590796
申请日：2005-03-01
申请人： William Alexander Denny , Michael Patrick Hay , Kevin Owen Hicks , Frederik Pruijn , William Robert Wilson , Karin Pchalek
发明人： William Alexander Denny , Michael Patrick Hay , Kevin Owen Hicks , Frederik Pruijn , William Robert Wilson , Karin Pchalek
IPC分类号： C07D253/10 , C07D413/12 , A61K31/53 , A61P35/00
CPC分类号： C07D253/10 , C07D253/08 , C07D401/12
摘要： The compound 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide and pharmacologically acceptable salts thereof. A method of treating cancer in a subject is also described in which 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide or a pharmacologically acceptable salt thereof is administered to tumor cells in a hypoxic environment. Also described is a method of radiosensitising in a subject tumor cells of solid tumors in hypoxic conditions by administering to the subject a pharmaceutical composition containing 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide or a pharmacologically acceptable salt thereof in an amount sufficient to produce radiosensitivity in the tumor cells, and subjecting the tumor cells to radiation. A pharmaceutical composition is additionally provided containing a therapeutically effective amount of 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide or a pharmacologically acceptable salt thereof and a pharmaceutically acceptable excipient, adjuvant, carrier, buffer or stabiliser.
摘要翻译：化合物3-乙基-6- [3-（4-吗啉基）丙氧基] -1,2,4-苯并三嗪1,4-二氧化物及其药理学上可接受的盐。还描述了在受试者中治疗癌症的方法，其中给予3-乙基-6- [3-（4-吗啉基）丙氧基] -1,2,4-苯并三嗪1,4-二氧化物或其药理学上可接受的盐到缺氧环境中的肿瘤细胞。还描述了通过向受试者施用含有3-乙基-6- [3-（4-吗啉基）丙氧基] -1,2,4-恶二唑的药物组合物，在缺氧条件下的实体瘤的受试肿瘤细胞中放射增敏的方法，苯并三嗪1,4-二氧化物或其药理学上可接受的盐，其量足以在肿瘤细胞中产生放射敏感性，并对肿瘤细胞进行辐射。另外提供含有治疗有效量的3-乙基-6- [3-（4-吗啉基）丙氧基] -1,2,4-苯并三嗪1,4-二氧化物或其药学上可接受的盐和药学上可接受的盐的药物组合物可接受的赋形剂，佐剂，载体，缓冲液或稳定剂。

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