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21. 发明申请

US20200277275A1 MODULATORS OF THE CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR PROTEIN AND METHODS OF USE 审中-公开
公开(公告)号：US20200277275A1
公开(公告)日：2020-09-03
申请号：US16878430
申请日：2020-05-19
申请人： AbbVie Overseas S.Á.R.L. , Galapagos NV
发明人： Robert J. Altenbach , Andrew Bogdan , Sylvain Couty , Nicolas Desroy , Gregory A. Gfesser , Christopher Gaëtan Housseman , Philip R. Kym , Bo Liu , Thi Thu Trang Mai , Karine Fabienne Malagu , Nuria Merayo Merayo , Olivier Laurent Picolet , Mathieu Rafaël Pizzonero , Xenia B. Searle , Steven Emiel Van der Plas , Xueqing Wang , Ming C. Yeung
IPC分类号： C07D401/04 , A61P1/00 , C07D401/14 , C07D213/30 , C07D215/36 , A61P11/00 , C07D231/56 , C07C311/45 , C07D471/04 , C07D235/28 , C07D213/64 , C07D213/71 , C07D401/12
摘要： The invention discloses compounds of Formula (I), wherein A1, R1, R2, R3, R4, and n are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention.

22. 发明授权

US10676455B2 Methods and compositions for treatment of muscle wasting, muscle weakness, and/or cachexia 有权
公开(公告)号：US10676455B2
公开(公告)日：2020-06-09
申请号：US14335853
申请日：2014-07-18
申请人： Baylor College of Medicine
发明人： David J. Tweardy , Moses M. Kasembeli , Marvin X. Xu , Thomas Kristian Eckols
IPC分类号： C07D333/34 , A61K31/47 , A61K31/44 , A61K31/194 , C07C311/21 , C07D215/36 , A61K31/4406 , A61K31/415 , A61K31/381 , A61K31/357 , A61K31/145 , C07D213/71 , C07D231/18 , C07D319/18 , C07C311/08 , C07C311/10 , C07C311/13 , C07C311/24 , C07C311/29 , C07C311/44 , C07C323/49 , C07C381/06 , A61K45/06 , A61K31/18 , A61K31/4035 , A61K31/404 , A61K31/4164 , A61K31/4196 , A61K31/42 , A61K31/428 , A61K31/45 , A61K31/454 , A61K31/4704 , A61K31/4709 , A61K31/513
摘要： Embodiments of the invention include methods of treating, preventing, and/or reduce the risk or severity of a condition selected from the group consisting of muscle wasting, muscle weakness, cachexia, and a combination thereof in an individual in need thereof. In some embodiments, particular small molecules are employed for treatment, prevention, and/or reduction in the risk of muscle wasting. In at least particular cases, the small molecules are inhibitors of STAT3.

23. 发明授权

US10676439B2 Pentafluorosulfanyl pyridine 有权
公开(公告)号：US10676439B2
公开(公告)日：2020-06-09
申请号：US15778920
申请日：2016-11-25
申请人： UBE INDUSTRIES, LTD.
发明人： Norio Shibata , Kohei Matsuzaki , Norimichi Saito
IPC分类号： C07D213/71 , C07D213/74 , C07D213/73 , C07D213/76 , C07D213/84
摘要： A pyridine compound having a SF5 group on position-3 and position-4 of a pyridine ring is provided. Pentafluorosulfanyl pyridine represented by formula (d): wherein a SF5 group binds to either one of position-3 or position-4 of a pyridine ring, and R2 binds to the other one of position-3 or position-4; and R1, R2, R3, and R4 are independently a hydrogen atom, a halogen atom, a substituted or non-substituted alkyl group having 1 to 18 carbon atoms, a substituted or non-substituted aryl group having 6 to 30 carbon atoms, a nitro group, a cyano group, a substituted or non-substituted alkanesulfonyl group having 1 to 18 carbon atoms, a substituted or non-substituted arenesulfonyl group having 6 to 30 carbon atoms, a substituted or non-substituted alkoxy group having 1 to 18 carbon atoms, a substituted or non-substituted aryloxy group having 6 to 30 carbon atoms, an acyloxy group having 1 to 18 carbon atoms, a substituted or non-substituted alkanesulfonyloxy group having 1 to 18 carbon atoms, a substituted or non-substituted arenesulfonyloxy group having 6 to 30 carbon atoms, a substituted or non-substituted alkoxycarbonyl group having 2 to 18 carbon atoms, a substituted or non-substituted aryloxycarbonyl group having 7 to 30 carbon atoms, a substituted carbamoyl group having 2 to 18 carbon atoms, a substituted amino group having 1 to 18 carbon atoms, an amino group, an azide group, a substituted or non-substituted aralkyloxy group having 7 to 30 carbon atoms, a substituted or non-substituted aralkylsulfide group having 7 to 30 carbon atoms, or a SF5 group.

24. 发明申请

US20200085051A1 HETEROCYCLIC COMPOUND AND COMPOSITION CONTAINING SAME 审中-公开
公开(公告)号：US20200085051A1
公开(公告)日：2020-03-19
申请号：US16617211
申请日：2018-06-01
申请人： Sumitomo Chemical Company, Limited
发明人： Ayaka TANAKA , Naoya SUGIMOTO , Takeshi TSURUDA
IPC分类号： A01N43/40 , C07D213/70 , C07D401/04 , A01N43/54 , C07D213/71 , C07D239/52 , A01N43/58 , C07D401/14 , A01N43/653
摘要： A heterocyclic compound is represented by formula (I): in which R2 represents a C1-C6 alkyl group optionally having one or more halogen atoms, n is 0, R3 represents a C1-C6 chain hydrocarbon group optionally having one or more substituents selected from Group B, q is 0, Het represents a group represented by the formulae Het 1 or Het 2, A1 represents a nitrogen atom, and Q2 represents an oxygen atom. The compound has excellent efficacy for controlling harmful arthropods. A composition is provided which contains the compound of formula (I) and one or more additional ingredients.

25. 发明授权

US10538487B2 Sulfonylureas and related compounds and use of same 有权
公开(公告)号：US10538487B2
公开(公告)日：2020-01-21
申请号：US15551264
申请日：2016-02-16
申请人： THE UNIVERSITY OF QUEENSLAND , THE PROVOST, FELLOWS, FOUNDATION SCHOLARS, AND THE OTHER MEMBERS OF THE BOARD OF THE COLLEGE OF THE HOLY AND UNDIVIDED TRINITY OF QUEEN ELIZABETH NEAR DUBLIN
发明人： Luke O'Neill , Rebecca Coll , Matthew Cooper , Avril Robertson , Kate Schroder
IPC分类号： C07C311/56 , C07D307/18 , C07D307/64 , C07D407/12 , C07D493/04 , C07D405/12 , C07D333/34 , C07D277/36 , C07D249/12 , C07D249/04 , C07D231/18 , C07D403/12 , C07C311/60 , C07D333/52 , C07D249/06 , C07D413/12 , C07D495/04 , C07D401/12 , C07D241/24 , C07D307/68 , C07D271/12 , C07D311/16 , C07D317/62 , C07D487/04 , C07D215/36 , C07D217/02 , C07D241/42 , C07D498/04 , C07D307/82 , C07D333/62 , C07D217/24 , C07D207/38 , C07D261/18 , C07D213/71 , C07D221/18 , C07D309/08 , A61P1/00 , C07D417/12 , C07D495/06 , C07D311/60 , A61P35/00 , A61P3/00 , C07D235/02 , C07D311/18 , A61P17/00 , A61P5/00 , C07D401/06 , A61P37/00 , A61P25/00 , C07D217/22 , C07D241/44
摘要： The present invention provides for certain sulfonyl ureas and related compounds which have advantageous properties and show useful activity in the inhibition of activation of the NLRP3 inflammasome. Such compounds are useful in the treatment of a wide range of disorders in which the inflammation process, or more specifically the NLRP3 inflammasome, have been implicated as being a key factor.

26. 发明授权

US10322107B2 N-methyl-N-(1-phenyl-2-(1-pyrrolidinyl)ethyl)-2-aminophenylacetamide derivatives agonists for the kappa opioid receptor 有权
公开(公告)号：US10322107B2
公开(公告)日：2019-06-18
申请号：US15539061
申请日：2015-12-18
申请人： Nektar Therapeutics
发明人： Franco J. Duarte , Neel K. Anand , Wen Zhang , Pankaj Sharma , Devendrapratap Singh
IPC分类号： A61K31/4025 , C07D213/71 , C07D231/18 , C07D333/34 , C07D239/60 , C07D261/10 , C07D207/12 , C07D207/14 , C07D295/13 , C07D295/135 , C07D207/04
摘要： Compounds and pharmaceutically acceptable salts and solvates thereof are described. The compounds relate to and/or have application(s) in (among others) the fields of drug discovery, pharmacotherapy, physiology and organic chemistry.

27. 发明授权

US10322104B2 Disulfur bridge linkers for conjugation of a cell-binding molecule 有权
公开(公告)号：US10322104B2
公开(公告)日：2019-06-18
申请号：US15479859
申请日：2017-04-05
申请人： Suzhou M-Conj Biotech Co., Ltd.
发明人： Robert Yongxin Zhao
IPC分类号： A61K31/5365 , A61K31/337 , A61K45/06 , C07C243/28 , C07D207/452 , C07C275/50 , C07C311/55 , C07D213/71 , C07K5/065 , C07D403/14 , C07K5/078 , C07D405/14 , C07D413/14 , C07D417/14 , C07D493/08 , C07D498/14 , C07D519/00 , A61K31/404 , A61K31/5513 , A61K31/551 , A61K49/00 , A61K47/68
摘要： The present invention relates to novel disulfur bridge linkers containing hydrazine used for the specific conjugation of compounds/cytotoxic agents to a cell-binding molecule, through bridge linking a pair of thiols on the cell-binding molecule. The invention also relates to methods of making such linkers, and of using such linkers in making homogeneous conjugates, as well as of application of the conjugates in treatment of cancers, infections and autoimmune disorders.

28. 发明授权

US10315990B2 Isothiocyanate compounds and isothiocyanate XPO1 protein inhibitor drugs thereof 有权
公开(公告)号：US10315990B2
公开(公告)日：2019-06-11
申请号：US15550783
申请日：2016-02-03
申请人： DRIVINGFORCE THERAPEUTICS Co., Ltd.
发明人： Yongliang Yang
IPC分类号： A61K31/26 , A61K31/428 , C07C331/22 , C07C331/24 , C07D213/71 , C07D215/36 , C07D235/28 , C07D239/74 , C07D257/04 , C07D277/76 , C07D311/14 , C07D295/096
摘要： The present invention provides an isothiocyanate compound and its application. The compound is an aryl-substituted isothiocyanate compound that has a structure of the general formula I. The isothiocyanate compound of the present invention has very good solubility in water, far better inhibitory activity for XPO1 protein than other non-aryl substituted congeneric compounds, little side effects, and good biological safety and bioavailability, and is quite suitable for clinical application. Therefore, the isothiocyanate compound would have tremendous potential market space and economic benefits.

29. 发明授权

US10301320B2 Compositions and methods of modulating 15-PGDH activity 有权
公开(公告)号：US10301320B2
公开(公告)日：2019-05-28
申请号：US15359330
申请日：2016-11-22
申请人： CASE WESTERN RESERVE UNIVERSITY , Board of Regents of the University of Texas System , University of Kentucky Research Foundation
发明人： Sanford Markowitz , James K. V. Willson , Bruce Posner , Joseph Ready , Youngyou Zhang , Hsin-Hsiung Tai , Monika Antczak , Stanton Gerson , KiBeom Bae , Sung Yeun Yang , Amar Desai
IPC分类号： A61K31/4365 , C07D495/04 , C07D213/71 , C07D213/73 , C07D213/75 , C07D213/76 , C07D215/08 , C07D237/20 , C07D405/12 , C07D239/42 , C07D241/20 , C07D261/14 , C07D207/263 , C07D275/03 , C07D209/08 , C07D277/46 , C07D295/185 , C07C311/21 , A61K31/519
摘要： Compounds and methods of modulating 15-PGDH activity, modulating tissue prostaglandin levels, treating disease, diseases disorders, or conditions in which it is desired to modulate 15-PGDH activity and/or prostaglandin levels include 15-PGDH inhibitors and 15-PGDH activators described herein.

30. 发明授权

US10292961B2 Disulfur bridge linkers for conjugation of a cell-binding molecule 有权
公开(公告)号：US10292961B2
公开(公告)日：2019-05-21
申请号：US14799712
申请日：2015-07-15
申请人： Suzhou M-Conj Biotech Co., Ltd.
发明人： Robert Yongxin Zhao
IPC分类号： A61K47/48 , A61K31/337 , A61K45/06 , C07C243/28 , C07D207/452 , C07C275/50 , C07C311/55 , C07D213/71 , C07K5/065 , C07D403/14 , C07K5/078 , C07D405/14 , C07D413/14 , C07D417/14 , C07D493/08 , C07D498/14 , C07D519/00 , A61K31/404 , A61K31/5365 , A61K31/5513 , A61K31/551 , A61K49/00 , A61K47/68
摘要： The present invention relates to novel disulfur bridge linkers containing hydrazine used for the specific conjugation of compounds/cytotoxic agents to a cell-binding molecule, through bridge linking a pair of thiols on the cell-binding molecule. The invention also relates to methods of making such linkers, and of using such linkers in making homogeneous conjugates, as well as of application of the conjugates in treatment of cancers, infections and autoimmune disorders.

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