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公开(公告)号：US20190062311A1
公开(公告)日：2019-02-28
申请号：US15766887
申请日：2016-10-07
发明人： Patrick Rene Angibaud , Olivier Alexis Georges Querolle , Didier Jean-Claude Berthelot , Christophe Meyer , Matthieu Philippe Victor Willot , Lieven Meerpoel , Thierry Francois Alain Jean Jousseaume
IPC分类号： C07D403/10 , C07D487/04 , C07D495/10 , C07D498/10 , C07D471/04 , C07D241/42 , C07D403/12 , C07D403/14 , C07D413/10
CPC分类号： C07D403/10 , C07D241/14 , C07D241/42 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D413/04 , C07D413/06 , C07D413/10 , C07D417/04 , C07D471/04 , C07D487/02 , C07D487/04 , C07D491/10 , C07D495/10 , C07D498/10 , C07D513/10
摘要： The present invention relates to substituted quinoxaline and pyridopyrazine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as pI3Kβ inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
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公开(公告)号：US20180155299A1
公开(公告)日：2018-06-07
申请号：US15833494
申请日：2017-12-06
申请人： Nagaraju Birudukota , David Becker
发明人： Nagaraju Birudukota , David Becker
IPC分类号： C07D255/02 , C07D403/14 , C07D487/04 , C07C251/20 , C07C321/06 , C07C49/675 , C07B43/04 , C07B45/02
CPC分类号： C07D255/02 , A61P5/26 , C07B43/04 , C07B45/02 , C07C49/675 , C07C243/18 , C07C251/20 , C07C321/06 , C07C2603/06 , C07D249/08 , C07D257/10 , C07D261/08 , C07D271/08 , C07D403/14 , C07D487/02 , C07D487/04
摘要： An azasteroid mimic or an intermediate for the preparation of an azasteroid and azasteroid mimic is formed via an oxocycloalkenyl isoxazolium anhydrobase and its dimer. The dimer can be used to form mono- and dihydrazones, which can be an azasteroid mimic or an intermediate for the preparation of an azasteroid and azasteroid mimic. A method of preparation of the dimer and the azasteroid mimic or an intermediate for the preparation of an azasteroid and azasteroid mimic occurs with hydrazonation and, optionally, a subsequent dehydrazonation. The dimer can be converted by inserting a nitrogen atom into the six membered ring of to a C-17 position cyclohexenone moiety of the dimer to yield a reduced tetrazolo[1,5-a]azepin-8-yl group. A subsequent hydrozone formation at a benzylic ketone can be carried out to generate an azasteroid mimic with a (triazol-4-yl)imino substituent. Monohydrazones can be converted to their thione equivalents.
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公开(公告)号：US20170267672A1
公开(公告)日：2017-09-21
申请号：US15505758
申请日：2015-08-18
发明人： Andre Stoller , Andre Jeanguenat , Andrew Edmunds , Pierre Joseph Marcel Jung , Daniel Emery , Michel Muehlebach , Peter Renold
IPC分类号： C07D417/10 , C07F5/02 , C07D487/02 , A01N43/90 , C07D471/04
CPC分类号： C07D417/10 , A01N43/90 , C07D471/04 , C07D487/02 , C07D487/04 , C07F5/02 , C07F5/025 , A01N25/00 , A01N2300/00
摘要： Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.
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公开(公告)号：US09331290B2
公开(公告)日：2016-05-03
申请号：US13809913
申请日：2011-06-17
IPC分类号： H01L51/00 , C07D487/02 , C07D487/12 , C07F15/00 , C09K11/06 , H05B33/14 , H01L51/50
CPC分类号： H01L51/0085 , C07D487/02 , C07D487/12 , C07F15/0033 , C09K11/06 , C09K2211/1029 , C09K2211/1044 , C09K2211/1059 , C09K2211/1092 , C09K2211/185 , H01L51/0059 , H01L51/0067 , H01L51/0072 , H01L51/0077 , H01L51/0087 , H01L51/5016 , H05B33/14 , Y02E10/549
摘要： The present invention relates to metal complexes and to electronic devices, in particular organic electro-luminescent devices, comprising these metal complexes. M(L)n(L′)m formula (1), where the compound contains a moiety M(L)n of the formula (2).
摘要翻译： 本发明涉及金属络合物和包含这些金属络合物的电子器件，特别是有机电致发光器件。 M（L）n（L'）m式（1），其中化合物含有式（2）的部分M（L）n。
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公开(公告)号：US08895580B2
公开(公告)日：2014-11-25
申请号：US13499335
申请日：2010-10-01
IPC分类号： A61K31/4745 , A61K31/5377 , C07D519/00 , C07D471/04 , C07D473/00 , C07D487/02 , C07D495/04 , A61K31/535
CPC分类号： C07D405/04 , A61K31/535 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D473/00 , C07D487/02 , C07D491/056 , C07D495/04 , C07F7/0812
摘要： The present invention is directed to quinolinone-pyrazolone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
摘要翻译： 本发明涉及式（I）的喹啉酮 - 吡唑啉酮化合物，其为M1受体阳性变构调节剂，可用于治疗涉及M1受体的疾病，例如阿尔茨海默氏病，精神分裂症，疼痛或睡眠障碍 。 本发明还涉及包含该化合物的药物组合物，以及该化合物和组合物在治疗由M1受体介导的疾病中的用途。
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6.发明申请N-substituted hetero-bicyclic compounds and derivatives for combating animal pests 有权N-取代的杂双环化合物和用于对抗动物害虫的衍生物公开(公告)号：US20140024659A1
公开(公告)日：2014-01-23
申请号：US14009606
申请日：2012-04-05
IPC分类号： A01N43/90 , C07D513/04 , C07D403/04 , C07D498/04
CPC分类号： A01N43/90 , C07D403/04 , C07D487/02 , C07D498/04 , C07D513/04
摘要： The invention relates to N-substituted hetero-bicyclic compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted hetero-bicyclic compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted hetero-bicyclic compounds.The N-substituted hetero-bicyclic compounds of the present invention are defined by the following formula I: wherein A, B, X, Het, R1, R2, W1, W2, W3 and W4 are defined as in the description.
摘要翻译： 本发明涉及式（I）的N-取代杂双环化合物，其对映异构体，非对映异构体和盐以及包含这些化合物的组合物。 本发明还涉及这些N-取代的杂双环化合物及其组合物的方法和用途，用于对抗和控制动物害虫。 此外，本发明还涉及施用这种N-取代的杂双环化合物的杀虫方法。 本发明的N-取代杂双环化合物由下式I定义：其中A，B，X，Het，R 1，R 2，W 1，W 2，W 3和W 4如在说明书中所定义。
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公开(公告)号：US20120196845A1
公开(公告)日：2012-08-02
申请号：US13499335
申请日：2010-10-01
IPC分类号： A61K31/4745 , A61K31/5377 , A61K31/496 , A61K31/506 , A61K31/519 , C07D519/00 , A61K31/498 , A61K31/52 , A61P25/28 , A61P25/18 , A61P29/00 , A61P25/00 , C07D471/04 , A61K31/501
CPC分类号： C07D405/04 , A61K31/535 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D473/00 , C07D487/02 , C07D491/056 , C07D495/04 , C07F7/0812
摘要： The present invention is directed to quinolinone-pyrazolone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
摘要翻译： 本发明涉及式（I）的喹啉酮 - 吡唑啉酮化合物，其为M1受体阳性变构调节剂，可用于治疗涉及M1受体的疾病，例如阿尔茨海默氏病，精神分裂症，疼痛或睡眠障碍 。 本发明还涉及包含该化合物的药物组合物，以及该化合物和组合物在治疗由M1受体介导的疾病中的用途。
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公开(公告)号：US20120142925A1
公开(公告)日：2012-06-07
申请号：US12300068
申请日：2007-05-25
IPC分类号： C07D489/02 , C07D489/00
CPC分类号： C07D487/02 , C07D487/04 , Y02P20/55
摘要： A process is provided for the N-demethylation of certain morphinans by reaction with α-chloroethyl chloroformate followed by hydrolysis of the resulting intermediate.
摘要翻译： 通过与氯甲酸α-氯乙酯反应，然后水解所得中间体，提供某些吗啡喃的N-去甲基化方法。
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![Alkynyl pyrrolo[2,3-d]pyrimidines and related analogs as HSP90-inhibitors](/abs-image/US/2012/01/10/US08093229B2/abs.jpg.150x150.jpg)
9.发明授权Alkynyl pyrrolo[2,3-d]pyrimidines and related analogs as HSP90-inhibitors 有权炔基吡咯并[2,3-d]嘧啶和相关类似物作为HSP90-抑制剂公开(公告)号：US08093229B2
公开(公告)日：2012-01-10
申请号：US12471298
申请日：2009-05-22
IPC分类号： A61K31/519 , A61K31/661 , A61P35/00 , C07F9/113 , C07D487/04
CPC分类号： C07D487/02 , C07D487/04
摘要： Alkynyl pyrrolo [2,3-d] pyrimidines of Formula I are described and demonstrated to have utility as Heat Shock Protein 90 (HSP90) inhibiting agents used in the treatment and prevention of various HSP90 mediated disorders. Methods of synthesis and use of such compounds are also described and claimed.
摘要翻译： 描述了式I的炔基吡咯并[2,3-d]嘧啶，并证明其可用作用于治疗和预防各种HSP90介导的病症的热休克蛋白90（HSP90）抑制剂。 还描述和要求保护这些化合物的合成和使用方法。
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![Substituted pyrrolo[2.3-B]pyridines](/abs-image/US/2008/12/16/US07465726B2/abs.jpg.150x150.jpg)
公开(公告)号：US07465726B2
公开(公告)日：2008-12-16
申请号：US11194158
申请日：2005-08-01
申请人： Saleh Ahmed , Oscar Barba , Jason Bloxham , Graham Dawson , William Gattrell , John Kitchin , Neil Anthony Pegg , Imaad Saba , Shazia Sadiq , Colin Peter Sambrook Smith , Don Smyth , Amo G. Steinig , Robin Wilkes , Bijoy Panicker , Paula Tavares , Matthew Cox , An-Hu Li , Hanqing Dong , Lifu Ma , Kenneth (‘Ken’) Foreman , Qinghua (‘Felix’) Weng , Kathryn Stolz
发明人： Saleh Ahmed , Oscar Barba , Jason Bloxham , Graham Dawson , William Gattrell , John Kitchin , Neil Anthony Pegg , Imaad Saba , Shazia Sadiq , Colin Peter Sambrook Smith , Don Smyth , Amo G. Steinig , Robin Wilkes , Bijoy Panicker , Paula Tavares , Matthew Cox , An-Hu Li , Hanqing Dong , Lifu Ma , Kenneth (‘Ken’) Foreman , Qinghua (‘Felix’) Weng , Kathryn Stolz
IPC分类号： A61K31/437 , A61K31/496 , A61K31/5355 , A61K31/541 , A61K31/5513 , A61K31/551 , C07D471/04 , C07D223/04 , C07D243/08 , C07D241/04 , C07D413/10 , C07D413/06 , C07D413/08 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/14 , A61K31/04 , A61K31/519 , C07D487/04
CPC分类号： C07D471/02 , C07D487/02 , C07D487/04
摘要： Compounds represented by Formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, are inhibitors of least two of the Abl, Aurora-A, Blk, c-Raf, cSRC, Src, PRK2, FGFR3, Flt3, Lck, Mek1, PDK-1, GSK3β, EGFR, p70S6K, BMX, SGK, CaMKII, Tie-2, IGF-1R, Ron, Ret, and KDR kinases in animals, including humans, for the treatment and/or prevention of various diseases and conditions such as cancer.
摘要翻译： 由式（I）表示的化合物或其立体异构体或其药学上可接受的盐是Abl，Aurora-A，Blk，c-Raf，cSRC，Src，PRK2，FGFR3，Flt3，Lck，Mek1，PDK中的至少两种的抑制剂 -1，GSK3beta，EGFR，p70S6K，BMX，SGK，CaMKII，Tie-2，IGF-1R，Ron，Ret和KDR激酶，用于治疗和/或预防各种疾病和病症， 癌症。
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