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公开(公告)号:US20180282285A1
公开(公告)日:2018-10-04
申请号:US15973655
申请日:2018-05-08
申请人: Dow AgroSciences LLC
发明人: Qiang YANG , Beth LORSBACH , Gregory WHITEKER , Gary ROTH , Carl DeAMICIS , Thomas CLARK , Kaitlyn GRAY , Belgin CANTURK , Elisabeth J. KANE , Yu ZHANG , Joseck M. MUHUHI
IPC分类号: C07D231/38 , C07C321/16 , C07D401/04 , A01N43/56 , C07D231/40 , C07C321/14
CPC分类号: C07D231/38 , A01N43/56 , C07C321/14 , C07C321/16 , C07C2601/02 , C07D231/40 , C07D401/04
摘要: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.
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公开(公告)号:US10000459B2
公开(公告)日:2018-06-19
申请号:US14776954
申请日:2014-03-17
IPC分类号: C07D261/14 , C07D231/38 , C07D231/52 , C07D233/88 , C07D401/04 , C07D239/42 , C07D413/04 , C07D263/48
CPC分类号: C07D261/14 , C07D231/38 , C07D231/52 , C07D233/88 , C07D239/42 , C07D263/48 , C07D401/04 , C07D413/04
摘要: Heterocyclic compounds are described that are lysophosphatidic acid receptor ligands that are useful in the treatment of lysophosphatidic acid receptor-dependent diseases and conditions, including but not limited to diseases involving fibrosis, such as fibrosis of the heart, kidney, liver and lung, and scleroderma; inflammatory diseases such as diabetic nephropathy and inflammatory bowel disease; ocular diseases such as diseases involving retinal degeneration; nerve diseases such as pruritus and pain. Non-limiting examples of those compounds include (RS)-3-Cyclopropyl-2-{4-[3-methyl-4-((R)-1-phenyl-ethoxycarbonylamino)-isoxazol-5-yl]-benzyloxy}-propionic acid and (R)-1-(4′-{5-[1-(2-Chloro-phenyl)-ethoxycarbonylamino]-4-fluoro-pyrazol-1-yl}-2-fluoro-biphenyl-4-yl)-cyclopropanecarboxylic acid.
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公开(公告)号:US20180133221A1
公开(公告)日:2018-05-17
申请号:US15522715
申请日:2015-10-23
发明人: Neil BENCE , Jessica HUCK , Marc HYER , Michael MILHOLLEN , Judy Qiuji SHI , Tary TRAORE
IPC分类号: A61K31/519 , A61K31/337 , A61K31/282 , A61K33/24 , A61P35/00
CPC分类号: A61K31/519 , A61K31/282 , A61K31/337 , A61K31/52 , A61K31/555 , A61K33/24 , A61K2300/00 , A61P35/00 , C07D231/38 , C07D405/12 , C07D487/04
摘要: Disclosed are methods for the treatment of cancer in patients in need of such treatment. The methods comprise administering to such a patient an ubiquitin-activating enzyme (UAE) inhibitor such as ((1R,2R,3S,4R)-2,3-dihydroxy-4-(2-(3-(tri-fluoromethylthio)phenyl)pyrazolo [1,5-a]pyrimidin-7-ylamino)cyclopentyl)methyl sulfamate (Compound 1) or a pharmaceutically acceptable salt in combination with one or more chemotherapeutic agents. Also disclosed are medicaments for use in the treatment of cancer.
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公开(公告)号:US20180105509A1
公开(公告)日:2018-04-19
申请号:US15567668
申请日:2016-04-20
申请人: ALMIRALL, S.A.
发明人: James DUFFY , Mark Stuart CHAMBERS , Alastair RAE , James OSBORNE , Isabelle Anne LEMASSON , Michael Daniel GOLDSMITH , Andrew SHARPE , Silvia FONQUERNA POU
IPC分类号: C07D401/12 , C07D231/38 , C07D249/06 , C07D401/14 , C07D403/10 , C07D403/12 , A61P25/02
CPC分类号: C07D401/12 , A61P25/02 , C07D231/38 , C07D249/06 , C07D249/14 , C07D401/04 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/14
摘要: The present invention relates to novel aminoindazolyl derivative compounds of Formula (I), the use of said compounds in treating diseases mediated by modulation of voltage-gated sodium channels in particular Nav1.7 AND to compositions containing said derivatives.
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公开(公告)号:US20180042234A1
公开(公告)日:2018-02-15
申请号:US15551352
申请日:2016-03-16
IPC分类号: A01N43/56 , C07D231/18 , A01N43/80 , C07D231/12 , C07D413/04 , C07D231/38 , C07D405/04
CPC分类号: A01N43/56 , A01N43/80 , C07D231/12 , C07D231/18 , C07D231/20 , C07D231/38 , C07D405/04 , C07D413/04 , A01N25/00
摘要: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein Q1, X, R1, R1a, R2 and R3 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
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公开(公告)号:US20180036294A1
公开(公告)日:2018-02-08
申请号:US15553593
申请日:2016-02-26
发明人: Shaomeng WANG , Yujun ZHAO , Bing ZHOU , Angelo AGUILAR
IPC分类号: A61K31/437 , C07D487/14 , C07D231/38 , C07D471/04 , C07D261/06 , A61K31/519 , C07D487/04
CPC分类号: A61K31/437 , A61K31/519 , C07D231/38 , C07D261/06 , C07D471/04 , C07D487/04 , C07D487/14
摘要: The present disclosure provides substituted 9H-pyrimido [4,5-b] indoles and 5H-pyrido [4,3-b] indoles and related analogs represented by Formula I and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, W, B1, B2, G, X1, Y1, Y2, and Y3 are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a condition or disorder responsive to inhibition of BET bromodomains such as cancer. The present disclosure is also directed to the use of compound of Formula I as synthetic intermediates.
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公开(公告)号:US20170355712A1
公开(公告)日:2017-12-14
申请号:US15601888
申请日:2017-05-22
申请人: Epizyme, Inc.
发明人: John Emmerson Campbell , Kenneth William Duncan , Megan Alene Foley , Darren Martin Harvey , Kevin Wayne Kuntz , James Edward John Mills , Michael John Munchhof
IPC分类号: C07D498/04 , C07D405/14 , C07D405/12 , C07D215/38 , C07D487/04 , C07D491/044 , C07D401/14 , C07D401/12 , C07D213/74 , C07D473/32 , C07D239/49 , C07D403/14 , C07D239/48 , C07D413/12 , C07D471/04 , C07D413/14 , C07D403/12 , C07D409/14
CPC分类号: C07D498/04 , C07D213/74 , C07D215/38 , C07D231/38 , C07D239/48 , C07D239/49 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D471/04 , C07D473/32 , C07D487/04 , C07D491/044
摘要: The present disclosure relates to amine-substituted aryl or heteroaryl compounds. The present disclosure also relates to pharmaceutical compositions containing these compounds and methods of treating a disorder (e.g., sickle cell anemia) via inhibition of a methyltransferase enzyme selected from EHMT1 and EHMT2, by administering an amine-substituted aryl or heteroaryl compound disclosed herein or a pharmaceutical composition thereof to subjects in need thereof. The present disclosure also relates to the use of such compounds for research or other non-therapeutic purposes.
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公开(公告)号:US20170267644A1
公开(公告)日:2017-09-21
申请号:US15610324
申请日:2017-05-31
IPC分类号: C07D231/38
CPC分类号: C07D231/38
摘要: An electrically conducting organic oligomer comprising 4-nitro-1H-pyrazole-3-yl-amine, 4-trifluoromethyl-1H-pyrazol-3-yl-amine, 4-trichloromethyl-1H-pyrazol-3-yl-amine, 4-tribromomethyl-1H-pyrazol-3-yl-amine, 4-ammonium-1H-pyrazol-3-yl-amine, 4-trimethylammonium-1H-pyrazol-3-yl-amine, 4-triethylammonium-1H-pyrazol-3-yl-amine, or 4-tripropylammonium-1H-pyrazol-3-yl-amine. An electrically conducting organic oligomer made from the steps of preparing an acidic aqueous solution with a monomer, preparing the acidic aqueous solution by mixing water with a monomer (3-amino-1H-pyrazole-4-carbonitrile), forming a solution preparing a second aqueous solution, mixing the acidic aqueous solution with the second aqueous solution, and allowing a reaction to proceed at about 40° C.
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公开(公告)号:US20170223959A1
公开(公告)日:2017-08-10
申请号:US15496048
申请日:2017-04-25
IPC分类号: A01N43/56 , C07D231/20 , C07D231/12 , C07D231/38
CPC分类号: A01N43/56 , C07D231/12 , C07D231/20 , C07D231/38 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D407/12 , C07D409/04 , C07D417/12
摘要: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein Q1 is a phenyl ring, naphthalenyl ring system, a 5- to 6-membered fully unsaturated heterocyclic ring or an 8- to 10-membered heteroaromatic bicyclic ring system, each as described with optional substituents as defined in the disclosure; Q2 is a phenyl ring, a naphthalenyl ring system, a 5- to 6-membered saturated, partially unsaturated or fully unsaturated heterocyclic ring, or an 8- to 10-membered heteroaromatic bicyclic ring system, each as described with optional substituents as defined in the disclosure; X is O, S(O)m, NR4, CR15R16, C(═O) or C(═S); and R1, R1a, R2, R4, R15, R16 and m are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention. Also disclosed are compounds of Formula 2, including all geometric and stereoisomers, and salts thereof, wherein X is NH; and Q1, Q2 and R2 are as defined for Formula 1; which are useful as intermediates for preparing compounds of Formula 1.
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公开(公告)号:US09725415B2
公开(公告)日:2017-08-08
申请号:US15037564
申请日:2014-11-25
发明人: Sergii Pazenok , Norbert Lui , Christian Funke , Arnd Neeff , Vadim Mikhailovich Timoshenko , Elena Ivanovna Kaminskaya , Yuriy Grigorievich Shermolovich
IPC分类号: C07D231/16 , C07D403/04 , C07D231/14 , C07D231/38
CPC分类号: C07D231/16 , C07D231/14 , C07D231/38 , C07D403/04
摘要: A new process for the preparation of 5-fluoro-1H-pyrazoles of the general formula (I) as described herein, resulting from the reaction of an olefin with hydrazine in the presence of water and a base.
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