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21. 发明申请

US20180297955A1 N-(4-HYDROXY-4-METHYL-CYCLOHEXYL)-4-PHENYL-BENZENESULFONAMIDE AND N-(4-HYDROXY-4-METHYL-CYCLOHEXYL)-4-(2-PYRIDYL)-BENZENESULFONAMIDE COMPOUNDS AND THEIR THERAPEUTIC USE 审中-公开
公开(公告)号：US20180297955A1
公开(公告)日：2018-10-18
申请号：US16011718
申请日：2018-06-19
申请人： PIMCO 2664 LIMITED
发明人： Stephen Allan Smith , Lisa Patel , Iain Robert Greig
IPC分类号： C07D213/85 , C07C311/20
摘要： The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain substituted N-(4-hydroxy-4-methyl-cyclohexyl)-4-phenyl-benzenesulfonamide and N-(4-hydroxy-4-methyl-cyclohexyl)-4-(2-pyridyl)benzenesulfonamide compounds (collectively referred to herein as HMC compounds) that are useful, for example, in the treatment of disorders (e.g., diseases) including, inflammation and/or joint destruction and/or bone loss; disorders mediated by excessive and/or inappropriate and/or prolonged activation of the immune system; inflammatory and autoimmune disorders, for example, rheumatoid arthritis; psoriasis; psoriatic arthritis; chronic obstructive pulmonary disease (COPD); asthma; atherosclerosis; inflammatory bowel disease; ankylosing spondylitis; multiple sclerosis; systemic lupus erythematosus; Sjogren's syndrome; a disorder associated with bone loss, such as bone loss associated with excessive osteoclast activity in rheumatoid arthritis, osteoporosis, cancer-associated bone disease, or Paget's disease; cancer, such as a haematological malignancy, such as multiple myeloma, leukemia, or lymphoma, or a solid tumour cancer, such as bladder cancer, breast cancer (female and/or male), colon cancer, renal cell carcinoma, kidney cancer, lung cancer, pancreatic cancer, gastric cancer, prostate cancer, brain cancer, skin cancer, thyroid cancer, basal cell ameloblastoma, or melanoma; a disorder associated with fibrosis, such as systemic sclerosis or scleroderma; or a rare vasculitide, such as Behçet's disease. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, for example, in therapy.

22. 发明申请

US20180258025A1 LABILE ESTERS OF AGROCHEMICALS FOR CONTROLLED RELEASE AND REDUCTION OF OFF-SITE MOVEMENT 审中-公开
公开(公告)号：US20180258025A1
公开(公告)日：2018-09-13
申请号：US15913030
申请日：2018-03-06
申请人： Monsanto Technology LLC
发明人： David A. Morgenstern
IPC分类号： C07C65/21 , C07D237/26 , A01N37/40 , A01N37/38 , C07D241/44 , C07D213/64 , C07D213/85 , C07D237/32 , A01N43/60 , A01N43/58 , A01N43/42 , A01N43/40 , C07D213/69 , C07D213/63 , C07D241/18 , C07D237/16 , C07D215/32 , C07D213/84 , C07C205/56 , C07C205/43 , C07C255/55 , C07C69/92 , C07C69/712 , C07C205/42 , C07C205/37 , C07C205/34 , A01N39/04
CPC分类号： C07C65/21 , A01N37/38 , A01N37/40 , A01N39/04 , A01N43/40 , A01N43/42 , A01N43/58 , A01N43/60 , C07C69/712 , C07C69/92 , C07C205/34 , C07C205/37 , C07C205/42 , C07C205/43 , C07C205/56 , C07C255/55 , C07D213/63 , C07D213/64 , C07D213/69 , C07D213/84 , C07D213/85 , C07D215/32 , C07D237/16 , C07D237/26 , C07D237/32 , C07D241/18 , C07D241/44 , Y02P20/55 , Y02P20/582
摘要： The present invention relates to esters of carboxylic acid agrochemicals comprising a labile protecting group and having formula (I). Certain of the esters of carboxylic acid agrochemicals do not undergo hydrolysis to a significant degree in the dark, but are cleaved to regenerate the parent carboxylic acid agrochemical when exposed to light. Others of the esters of carboxylic acid agrochemicals undergo hydrolysis under both light and dark conditions. The present invention further relates to methods for the controlled release of a carboxylic acid agrochemicals, and to methods of controlling unwanted plants comprising applying to the unwanted plants an ester of a carboxylic acid agrochemical.

23. 发明申请

US20180155279A1 ARYL ETHERS AND USES THEREOF 审中-公开
公开(公告)号：US20180155279A1
公开(公告)日：2018-06-07
申请号：US15805390
申请日：2017-11-07
申请人： Peloton Therapeutics, Inc.
发明人： Darryl David Dixon , Jonas Grina , John A. Josey , James P. Rizzi , Stephen T. Schlachter , Eli M. Wallace , Bin Wang , Paul Wehn , Rui Xu , Hanbiao Yang
IPC分类号： C07C311/29 , C07D231/56 , C07D213/89 , A61K31/09 , A61K31/10 , C07C43/205 , C07D213/85 , C07D213/65 , C07C381/10 , C07C323/22 , C07C317/48 , C07C317/46 , C07C317/44 , C07C317/42 , C07C317/40 , C07C317/36 , C07C317/34 , C07C317/32 , C07C317/24 , C07C317/22 , C07C313/06 , C07C255/56 , C07C255/54 , C07C205/22 , C07C43/285 , C07C43/263 , C07C43/23 , C07C43/225
CPC分类号： C07D213/85 , A61K31/09 , A61K31/10 , A61K41/0038 , A61P35/00 , C07C43/205 , C07C43/225 , C07C43/23 , C07C43/263 , C07C43/275 , C07C43/285 , C07C43/29 , C07C205/22 , C07C255/54 , C07C255/56 , C07C311/29 , C07C313/06 , C07C317/22 , C07C317/24 , C07C317/32 , C07C317/34 , C07C317/36 , C07C317/40 , C07C317/42 , C07C317/44 , C07C317/46 , C07C317/48 , C07C323/22 , C07C381/10 , C07C2602/04 , C07C2602/08 , C07C2602/10 , C07C2603/94 , C07D213/65 , C07D213/89 , C07D231/56
摘要： The present disclosure relates to HIF-2α inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2α scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo.

24. 发明申请

US20180086742A1 SUBSTITUTED OXOPYRIDINE DERIVATIVES AND USE THEREOF IN THE TREATMENT OF CARDIOVASCULAR DISORDERS 审中-公开
公开(公告)号：US20180086742A1
公开(公告)日：2018-03-29
申请号：US15786352
申请日：2017-10-17
申请人： Bayer Pharma Aktiengesellschaft
发明人： Susanne RÖHRIG , Alexander HILLISCH , Julia STRASSBURGER , Stefan HEITMEIER , Martina Victoria SCHMIDT , Karl-Heinz SCHLEMMER , Adrian TERSTEEGEN , Anja BUCHMÜLLER , Christoph GERDES , Martina SCHÄFER , Tom KINZEL , Henrik TELLER , Harmut SCHIROK , Jürgen KLAR , Eloisa Jimenez NUNEZ
IPC分类号： C07D405/06 , C07D213/84 , C07D213/85 , C07D401/12 , C07D413/14 , C07D413/12 , C07D417/12 , C07D213/64 , C07D213/69 , C07D409/06
CPC分类号： C07D405/06 , C07B2200/05 , C07D213/64 , C07D213/69 , C07D213/84 , C07D213/85 , C07D401/12 , C07D409/06 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The invention relates to substituted oxopyridine derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.

25. 发明申请

US20180057455A1 COMPOUNDS USEFUL AS IMMUNOMODULATORS 审中-公开
公开(公告)号：US20180057455A1
公开(公告)日：2018-03-01
申请号：US15689115
申请日：2017-08-29
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： KAP-SUN YEUNG , Katharine A. Grant-Young , Juliang Zhu , Mark G. Saulnier , David B. Frennesson , David R. Langley , Piyasena Hewawasam , Tao Wang , Zhongxing Zhang , Zhaoxing Meng , Li-Qiang Sun , Eric Mull , Paul Michael Scola
IPC分类号： C07D207/12 , C07D211/66 , C07D207/16 , C07D403/12 , C07D401/12 , C07D207/14 , C07D211/22 , C07D213/38 , C07D401/14 , C07C237/06 , C07D295/088 , C07D205/04 , C07D213/85 , C07C217/18 , C07D213/73 , C07D405/12 , C07C255/24 , C07D413/14 , C07D405/14 , C07D213/79 , C07D231/12 , C07D239/26 , C07D277/28 , C07D211/90
CPC分类号： C07D207/12 , C07C217/18 , C07C217/28 , C07C217/58 , C07C229/14 , C07C235/08 , C07C237/04 , C07C237/06 , C07C255/24 , C07C255/25 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D205/04 , C07D207/14 , C07D207/16 , C07D211/22 , C07D211/46 , C07D211/58 , C07D211/60 , C07D211/66 , C07D211/90 , C07D213/38 , C07D213/42 , C07D213/55 , C07D213/73 , C07D213/79 , C07D213/85 , C07D231/12 , C07D239/26 , C07D277/28 , C07D295/088 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/14 , C07D417/12
摘要： The present disclosure generally relates to compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.

26. 发明授权

US09884823B2 Oxime ether acetate compound, preparation method therefor and weeding application thereof 有权
公开(公告)号：US09884823B2
公开(公告)日：2018-02-06
申请号：US15125540
申请日：2015-02-13
申请人： ZHEJIANG UNIVERSITY OF TECHNOLOGY
发明人： Xiaohua Du , Dajie Mao , Zhenyuan Xu
IPC分类号： C07D213/61 , C07D213/64 , C07D213/65 , C07D213/85 , A01N43/40 , C07D213/55 , C07D213/84 , C07D213/30 , C07D213/57 , C07D213/76
CPC分类号： C07D213/55 , A01N43/40 , C07D213/30 , C07D213/57 , C07D213/61 , C07D213/64 , C07D213/65 , C07D213/76 , C07D213/84 , C07D213/85
摘要： The present invention discloses an oxime ether acetate compound containing a phenylpyridine moiety of formula (I), whose preparation method is as follows: (1) mixing a compound of formula (IV), a compound of formula (V), an alkaline substance A, a palladium catalyst and a solvent A; subjecting the mixture to a reaction at the temperature ranging from −10° C. to the reflux temperature for 0.5-20 hours to obtain a reaction solution A; post-treating the solution A to obtain a compound of formula (II); (2) mixing the compound of formula (II), an alkaline substance B, a phase transfer catalyst and a solvent B; subjecting the mixture to a reaction at the temperature ranging from −10° C. to the reflux temperature for 0.1-2 hours; then adding a compound of formula (III), continuing to react at the temperature ranging from −10° C. to the reflux temperature for 0.5-20 hours to obtain a reaction solution B; and post-treating the solution B to obtain the compound of formula (I). The oxime ether acetate compound containing a phenylpyridine moiety of formula (I) can be used for weeding in crops.

27. 发明授权

US09856279B2 Therapeutically active compositions and their methods of use 有权
公开(公告)号：US09856279B2
公开(公告)日：2018-01-02
申请号：US15130358
申请日：2016-04-15
申请人： AGIOS PHARMACEUTICALS, INC
发明人： Sheldon Cao , Janeta Popovici-Muller , Francesco G. Salituro , Jeffrey O. Saunders , Xuefei Tan , Jeremy M. Travins , Shunqi Yan , Zhixiong Ye
IPC分类号： C07D401/04 , C07D401/14 , C07D407/14 , C07D413/14 , C07D471/04 , A61K31/496 , C07F9/6509 , C07D405/14 , C07D213/85 , C07D401/12 , C07D405/12 , C07D409/14 , C07D417/14 , C07F9/6558 , A61K31/498 , A61K31/4985 , A61K31/501 , A61K31/502 , A61K31/506 , A61K31/517 , C07D487/04 , C07D498/04 , A61K31/5377 , A61K31/675
CPC分类号： C07F9/650952 , A61K31/496 , A61K31/498 , A61K31/4985 , A61K31/501 , A61K31/502 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/675 , C07D213/85 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D498/04 , C07F9/65583
摘要： Provided are piperazine compounds of Formula I useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described here.

28. 发明申请

US20170298020A1 METHODS AND COMPOUNDS FOR TREATING PROLIFERATIVE DISORDERS AND VIRAL INFECTIONS 审中-公开
公开(公告)号：US20170298020A1
公开(公告)日：2017-10-19
申请号：US15631796
申请日：2017-06-23
申请人： UNIVERSITY COLLEGE DUBLIN, NATIONAL UNIVERSITY OF IRELAND, DUBLIN
发明人： B. Therese Kinsella , Helen Reid
IPC分类号： C07D213/71 , C07D305/08 , C07D295/192 , C07D277/34 , C07D261/08 , A61K31/18 , C07D231/12 , C07D213/85 , C07D213/34 , C07D205/04 , C07D307/42 , C07D263/48
摘要： The invention generally relates to methods and compounds for treating proliferative disorders, viral infections, or both. In some embodiments, the invention provides an anticancer or antiviral compound including a substituted nitro phenoxy phenyl, a sulfonylurea, and an alkyl group. In some embodiments, the invention provides a method of treating a proliferative disorder or a viral infection including administering an anticancer or antiviral compound that binds to a thromboxane receptor, has preferential binding for either TPalpha (TPα) or TPbeta (TPβ) receptor subtype.

29. 发明申请

US20170066721A1 PROCESS FOR FLUORINATING COMPOUNDS 有权
标题翻译：氟化合物的方法
公开(公告)号：US20170066721A1
公开(公告)日：2017-03-09
申请号：US15228188
申请日：2016-08-04
申请人： Dow AgroSciences LLC , The Regents of the University of Michigan
发明人： Melanie Sanford , Sarah Ryan , Sydonie Schimler , Yang Cheng , Douglas Bland
IPC分类号： C07D213/79 , C07D215/04 , C07D213/76 , C07D237/08 , C07D213/84 , C07D213/85 , C07D213/803 , C07D217/02
CPC分类号： C07D213/79 , C07D213/26 , C07D213/76 , C07D213/803 , C07D213/84 , C07D213/85 , C07D215/04 , C07D217/02 , C07D237/08
摘要： Disclosed are mild temperature (e.g., from 0 to 80° C.) SNAr fluorinations of a variety of halide and sulfonate substituted aryl and heteroaryl substrates using NMe4F.
摘要翻译：公开了温和的温度（例如，0至80℃）。使用NMe4F对各种卤化物和磺酸酯取代的芳基和杂芳基底物进行SNAr氟化。

30. 发明申请

US20160326126A1 AMYLOID TARGETING AGENTS AND METHODS OF USING THE SAME 有权
标题翻译： AMYLOID瞄准剂及其使用方法
公开(公告)号：US20160326126A1
公开(公告)日：2016-11-10
申请号：US14915883
申请日：2015-03-19
申请人： AMYDIS DIAGNOSTICS , THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
发明人： Jerry Yang , Emmanuel A. Theodorakis , Stella Sarraf
IPC分类号： C07D295/155 , C07H19/056 , C07D213/85
CPC分类号： C07D295/155 , C07C255/42 , C07C255/58 , C07C255/59 , C07C311/35 , C07D211/06 , C07D213/57 , C07D213/85 , C07D241/04 , C07D265/30 , C07D295/04 , C07D307/52 , C07D333/22 , C07D401/04 , C07D401/14 , C07D405/04 , C07D405/10 , C07D407/10 , C07D409/04 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/12 , C07H19/056
摘要： Provided herein is the design and synthesis of novel molecular rotor fluorophores useful for detection of amyloid or amyloid like proteins. The fluorophores are designed to exhibit enhanced fluorescence emission upon associating with amyloid or amyloid like proteins as compared to unbound compound. Also disclosed herein are the methods for treating of diseases associated with an amyloid or amyloid like proteins.
摘要翻译：本文提供了可用于检测淀粉样蛋白或类淀粉样蛋白的新型分子转子荧光团的设计和合成。与未结合的化合物相比，荧光团被设计为在与淀粉样蛋白或淀粉样蛋白样蛋白相关联时表现出增强的荧光发射。本文还公开了治疗与淀粉样蛋白或类淀粉样蛋白相关的疾病的方法。

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