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公开(公告)号：US20240174611A1
公开(公告)日：2024-05-30
申请号：US18273476
申请日：2022-02-07
发明人： George L. Trainor , Maria Obdulia Rabal Gracia , Laura Fourmois , Olga Gherbovet , Frederic Cachoux
IPC分类号： C07D211/96 , C07C311/29 , C07D205/04 , C07D205/12 , C07D207/09 , C07D207/14 , C07D207/48 , C07D209/52 , C07D211/28 , C07D211/56 , C07D211/58 , C07D211/76 , C07D231/56 , C07D261/10 , C07D309/14 , C07D311/68 , C07D311/96 , C07D401/04 , C07D401/12 , C07D405/04 , C07D409/04 , C07D417/04 , C07D451/04
CPC分类号： C07D211/96 , C07C311/29 , C07D205/04 , C07D205/12 , C07D207/09 , C07D207/14 , C07D207/48 , C07D209/52 , C07D211/28 , C07D211/56 , C07D211/58 , C07D211/76 , C07D231/56 , C07D261/10 , C07D309/14 , C07D311/68 , C07D311/96 , C07D401/04 , C07D401/12 , C07D405/04 , C07D409/04 , C07D417/04 , C07D451/04 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/08 , C07C2602/10 , C07C2603/74
摘要： The present disclosure relates in part to chemical modulators of protein phosphatase 2A (PP2A). The compounds of the present disclosure are useful in treating, preventing, and/or ameliorating cancer, diabetes, autoimmune disease, solid organ transplant rejection, graft vs host disease, chronic obstructive pulmonary disease (COPD), non-alcoholic fatty liver disease, abdominal aortic aneurysm, chronic liver disease, heart failure, neurodegenerative disease, and cardiac hypertrophy.
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公开(公告)号：US20230312471A1
公开(公告)日：2023-10-05
申请号：US18022644
申请日：2021-08-26
申请人： UNIVERSITÄT KONSTANZ
发明人： Thomas BÖTTCHER , Lilian PENALVER
IPC分类号： C07D211/28 , C07C237/22 , C07D311/74 , C12Q1/37
CPC分类号： C07D211/28 , C07C237/22 , C07D311/74 , C12Q1/37
摘要： The present invention relates to a compound which can be used in the treatment of infections caused by SARS coronaviruses, e.g. by blocking the active site of the proteases 3CLpro and PLpro. The compound can be used as inhibitor or label as such or can be used in screening methods for profiling other inhibitors. Moreover, the present invention relates to a method of producing the compound.
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公开(公告)号：US20230181742A1
公开(公告)日：2023-06-15
申请号：US17821122
申请日：2022-08-19
IPC分类号： A61K47/54 , C07C227/06 , C07D211/28 , C07D211/58 , C12N15/88 , A61K48/00 , C07C229/08 , C12N15/113
CPC分类号： A61K47/54 , C07C227/06 , C07D211/28 , C07D211/58 , C12N15/88 , A61K48/0008 , C07C229/08 , C12N15/1137 , A61K47/543 , C12N2310/11 , C12N2310/141
摘要： There are provided for herein novel amine-containing transfection compounds and methods for making and using same. The compounds are generally obtained by reacting a primary amine with an unsaturated compound. Transfection complexes made using the amine-containing transfection compounds in combination with additional compounds to encapsulate biologically active agents such as nucleic acids are also provided for herein. Methods of using the transfection complexes for the in vivo or in vitro delivery of biologically active agents are also described. The transfection complexes of the present invention are highly potent, thereby allowing effective modulation of a biological activity at relatively low doses compared to analogous transfection compounds known in the art.
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公开(公告)号：US10071964B2
公开(公告)日：2018-09-11
申请号：US15560580
申请日：2016-03-22
申请人： Univerza V Ljubljani
发明人： Boris Brus , Urban Kosak , Damijan Knez , Nicolas Coquelle , Jacques-Philippe Colletier , Stanislav Gobec
IPC分类号： A61K31/445 , C07D211/06 , C07D211/28 , A61K31/4523 , A61K31/453 , A61K31/4709 , C07D401/12 , C07D405/12 , C07D211/26
CPC分类号： C07D211/28 , A61K31/445 , A61K31/4523 , A61K31/453 , A61K31/4709 , C07D211/26 , C07D401/12 , C07D405/12
摘要： This invention relates to new inhibitors of butyrylcholinesterase with general formulas I and II, where substituents are described in patent description. Compounds can be in the form of pure enantiomers or as racemic mixtures, or in the form of pharmaceutically acceptable salts. The present invention relates to the use of these inhibitors for the treatment of Alzheimer's disease and other forms of dementia.
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公开(公告)号：US09974762B2
公开(公告)日：2018-05-22
申请号：US15632412
申请日：2017-06-26
发明人： Zhiyuan Zhang , Xiaodong Wang , Xiaoguang Lei , Yaning Su , Sudan He , Hanying Ruan , Liming Sun
IPC分类号： A61K31/165 , A61K31/10 , C07C25/13 , C07C25/02 , C07C233/05 , C07C233/01
CPC分类号： A61K31/165 , A61K31/10 , C07C25/02 , C07C25/13 , C07C233/01 , C07C233/05 , C07C233/13 , C07C233/18 , C07C233/47 , C07C233/59 , C07C235/10 , C07C237/06 , C07C237/22 , C07C255/60 , C07C259/06 , C07C275/24 , C07C311/14 , C07C313/06 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2603/74 , C07D211/28 , C07D213/40 , C07D213/61 , C07D213/64 , C07D217/14 , C07D231/12 , C07D277/28 , C07D307/14 , C07D307/52 , C07D333/20
摘要： The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
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公开(公告)号：US20170183307A1
公开(公告)日：2017-06-29
申请号：US15320488
申请日：2014-12-19
发明人： Asami MURAYAMA , Takaaki KANO
IPC分类号： C07D211/56 , C07D211/02 , C07K1/12 , C07D211/28
CPC分类号： C07D211/56 , C07D211/02 , C07D211/28 , C07K1/128 , C07K5/1016 , C07K7/06
摘要： Provided are a method for industrially advantageously producing a highly purified pentapeptide and an intermediate thereof.A compound represented by the following formula (1) or a salt thereof: wherein R1 represents an alkyl group or an aralkyl group.
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公开(公告)号：US20170107208A1
公开(公告)日：2017-04-20
申请号：US15128829
申请日：2015-03-24
发明人： Jianliang XIAO , Jianjun WU
IPC分类号： C07D409/04 , C07D211/22 , C07D211/18 , C07D401/04 , C07D211/32 , C07D211/26 , C07D405/04 , C07D211/34 , C07D211/14 , C07D211/28
CPC分类号： C07D409/04 , C07B2200/13 , C07D211/02 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/26 , C07D211/28 , C07D211/32 , C07D211/34 , C07D401/04 , C07D405/04
摘要： The present invention relates to a process for preparing substituted piperidine compounds and especially chiral substituted piperidine compounds. The process involves reacting a substituted pyridinium ion with an amine as defined herein, in the presence of a hydrogen donor, a catalysts and a suitable solvent.
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公开(公告)号：US20150094474A1
公开(公告)日：2015-04-02
申请号：US14383777
申请日：2013-03-13
申请人： Redx Pharma Ltd.
发明人： William Thompson , Peter Jackson , Derek Lindsay , Thomas Screen , Benjamin Moulton , Christopher Urch
IPC分类号： A01N53/00 , C07C255/44 , C07C255/61 , A01N37/34 , C07C255/40 , A01N43/56 , A01N35/02 , C07D211/32 , A01N47/16 , C07D211/34 , C07D401/04 , C07C69/743 , C07C49/255
CPC分类号： A01N53/00 , A01N35/02 , A01N37/34 , A01N43/40 , A01N43/56 , A01N43/76 , A01N47/16 , A01N47/36 , C07C49/255 , C07C49/577 , C07C69/743 , C07C255/31 , C07C255/37 , C07C255/40 , C07C255/43 , C07C255/44 , C07C255/61 , C07C2601/02 , C07D211/28 , C07D211/32 , C07D211/34 , C07D213/643 , C07D239/52 , C07D401/04
摘要： The present invention relates to derivatives of compounds which are known to be of use in the field of agriculture. These derivatives are differentiated from the parent active compound by virtue of being redox derivatives of the active compound. This means that one or more of the functional groups in the active compound has been converted to another group in one or more changes one or more of which may be considered to represent a change of oxidation state relative to the groups in the original compound. We refer to these compounds generally as redox derivatives. The compounds are of use as insecticides, herbicides and insect repellents.
摘要翻译： 本发明涉及已知在农业领域中使用的化合物的衍生物。 由于活性化合物的氧化还原衍生物，这些衍生物与母体活性化合物不同。 这意味着活性化合物中的一个或多个官能团已经在一个或多个变化中转化为另一个基团，其中一个或多个可被认为代表相对于原始化合物中基团的氧化态变化。 我们通常将这些化合物称为氧化还原衍生物。 该化合物可用作杀虫剂，除草剂和驱虫剂。
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公开(公告)号：US20140011996A1
公开(公告)日：2014-01-09
申请号：US14013934
申请日：2013-08-29
申请人： Hassan Pajouhesh , Ramesh Kaul , Yanbing Ding , Yongbao Zhu , Lingyun Zhang , Nagasree Chakka , MIchael Edward Grimwood , Jason Tan , Yuanxi Zhou
发明人： Hassan Pajouhesh , Ramesh Kaul , Yanbing Ding , Yongbao Zhu , Lingyun Zhang , Nagasree Chakka , MIchael Edward Grimwood , Jason Tan , Yuanxi Zhou
IPC分类号： C07D211/28 , C07D401/06 , C07D211/62 , C07D409/12 , C07D405/06 , C07D413/12 , C07D211/26 , C07D401/12 , C07D211/66 , C07D405/14 , C07D211/46 , C07D211/38 , C07D405/12 , C07D417/12
CPC分类号： A61K31/5377 , A61K31/445 , A61K31/4525 , A61K31/453 , A61K31/4535 , A61K31/454 , A61K31/4545 , C07D211/26 , C07D211/28 , C07D211/38 , C07D211/46 , C07D211/62 , C07D211/66 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12
摘要： Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing N-piperidinyl acetamide derivatives as shown in formula (1).
摘要翻译： 公开了有助于改善由不希望的钙通道活性，特别是不希望的T型钙通道活性表征的病症的方法和化合物。 具体而言，是一系列含有式（1）所示的N-哌啶基乙酰胺衍生物的化合物。
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公开(公告)号：US08569344B2
公开(公告)日：2013-10-29
申请号：US13601357
申请日：2012-08-31
申请人： Hassan Pajouhesh , Ramesh Kaul , Yanbing Ding , Yongbao Zhu , Lingyun Zhang , Nagasree Chakka , Mike Grimwood , Jason Tan , Yuanxi Zhou
发明人： Hassan Pajouhesh , Ramesh Kaul , Yanbing Ding , Yongbao Zhu , Lingyun Zhang , Nagasree Chakka , Mike Grimwood , Jason Tan , Yuanxi Zhou
IPC分类号： A61K31/445 , A61P29/00
CPC分类号： A61K31/5377 , A61K31/445 , A61K31/4525 , A61K31/453 , A61K31/4535 , A61K31/454 , A61K31/4545 , C07D211/26 , C07D211/28 , C07D211/38 , C07D211/46 , C07D211/62 , C07D211/66 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12
摘要： Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing N-piperidinyl acetamide derivatives as shown in formula (1).
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