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公开(公告)号：US11504377B2
公开(公告)日：2022-11-22
申请号：US17038353
申请日：2020-09-30
发明人： Gerard M. Housey
IPC分类号： A61K31/5377 , C07D213/81 , C07D213/87 , C07D215/50 , C07D231/14 , C07D239/42 , C07D239/84 , C07D253/065 , C07D401/12 , C07D405/12 , C07D409/12 , G01N33/574 , C07D239/48 , C07C243/38 , C07D213/77 , C07D213/86 , C07D215/38 , C07D253/075 , C07D403/12 , G01N33/573 , A61K31/47 , A61K31/4709 , A61K31/505 , A61K31/506 , A61K31/53 , G01N33/50 , A61K31/166 , A61K31/175 , A61K31/195 , A61K31/27 , A61K31/415 , A61K31/4196 , A61K31/44 , A61K31/4436 , A61K31/444 , A61K31/495 , A61K31/517
摘要： This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.
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公开(公告)号：US20210015948A1
公开(公告)日：2021-01-21
申请号：US16990368
申请日：2020-08-11
发明人： Eric M. Gale , Peter Caravan
IPC分类号： A61K49/08 , A61K49/10 , A61K49/14 , C07D213/87 , C07D233/58 , C07D213/40 , C07K7/08 , C07D213/65 , C07D213/80 , C07D217/14 , C07D235/14 , C07D213/68 , C07K7/06 , G16H10/40
摘要： Provided herein are examples of metal chelating ligands that have high affinity for manganese. The resultant metal complexes can be used as MRI contrast agents, and can be functionalized with moieties that bind to or cause relaxivity change in the presence of biochemical targets.
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公开(公告)号：US20200046718A1
公开(公告)日：2020-02-13
申请号：US16656271
申请日：2019-10-17
发明人： Gerard M. Housey
IPC分类号： A61K31/5377 , A61K31/517 , A61K31/495 , A61K31/444 , A61K31/4436 , A61K31/44 , A61K31/4196 , A61K31/415 , A61K31/27 , A61K31/195 , A61K31/175 , A61K31/166 , G01N33/50 , A61K31/53 , A61K31/506 , A61K31/505 , A61K31/4709 , A61K31/47 , G01N33/573 , C07D403/12 , C07D253/075 , C07D215/38 , C07D213/86 , C07D213/77 , C07C243/38 , C07D239/48 , G01N33/574 , C07D409/12 , C07D405/12 , C07D401/12 , C07D253/065 , C07D239/84 , C07D239/42 , C07D231/14 , C07D215/50 , C07D213/87 , C07D213/81
摘要： This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.
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公开(公告)号：US10471065B2
公开(公告)日：2019-11-12
申请号：US15789476
申请日：2017-10-20
发明人： Gerard M. Housey
IPC分类号： C07D213/81 , A61K31/5377 , C07D213/87 , C07D215/50 , C07D231/14 , C07D239/42 , C07D239/48 , C07D239/84 , C07D253/065 , C07D401/12 , C07D405/12 , C07D409/12 , G01N33/574 , C07C243/38 , C07D213/77 , C07D213/86 , C07D215/38 , C07D253/075 , C07D403/12 , G01N33/573 , A61K31/47 , A61K31/4709 , A61K31/505 , A61K31/506 , A61K31/53 , G01N33/50 , A61K31/166 , A61K31/175 , A61K31/195 , A61K31/27 , A61K31/415 , A61K31/4196 , A61K31/44 , A61K31/4436 , A61K31/444 , A61K31/495 , A61K31/517
摘要： This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.
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公开(公告)号：US10227339B2
公开(公告)日：2019-03-12
申请号：US15573061
申请日：2016-10-25
发明人： Peng Li , Bailing Yang , Fei Hao , Zheng Wang , Zongbin Li , Haiying He , Shuhui Chen , Wei Xiao , Wang Shen , Zhenzhong Wang
IPC分类号： C07D417/14 , C07D213/87 , C07D401/04 , C07D417/04 , C07B41/02 , C07B43/04
摘要： The present invention discloses a salt form, crystal form and intermediate of the compound 1, and preparation method thereof.
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公开(公告)号：US09688616B2
公开(公告)日：2017-06-27
申请号：US15219478
申请日：2016-07-26
发明人： Erik Fenster , Melissa Fleury , Adam D. Hughes
IPC分类号： A61K31/40 , A61K31/42 , A61K31/44 , A61K31/197 , A61K31/397 , A61K31/5375 , C07D205/04 , C07D207/09 , C07D207/14 , C07D213/56 , C07C235/34 , C07D261/04 , C07D295/32 , C07C243/38 , C07D491/107 , C07D213/75 , C07C259/04 , C07D309/08 , C07D233/06 , C07D401/04 , C07D405/06 , C07D239/36 , C07D261/02 , C07C233/56 , C07C235/12 , C07C235/20 , C07C235/74 , C07C235/78 , C07D265/30 , C07D207/08 , C07D207/12 , C07D207/16 , C07D493/10 , C07C243/24 , C07C243/32 , C07D211/22 , C07D211/38 , C07D211/42 , C07D211/46 , C07D211/48 , C07D211/60 , C07D211/62 , C07D213/61 , C07D307/68 , A61K31/4015 , A61K31/495 , A61K45/06 , A61K31/192 , A61K31/4406 , C07C235/80 , C07D213/65 , A61K31/341 , A61K31/4409 , C07D213/86 , C07D213/87
CPC分类号： C07C243/38 , A61K31/192 , A61K31/197 , A61K31/341 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/42 , A61K31/44 , A61K31/4406 , A61K31/4409 , A61K31/495 , A61K31/5375 , A61K45/06 , C07C233/56 , C07C235/12 , C07C235/20 , C07C235/34 , C07C235/74 , C07C235/78 , C07C235/80 , C07C243/24 , C07C243/32 , C07C259/04 , C07C2601/08 , C07C2601/16 , C07D205/04 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/14 , C07D207/16 , C07D211/22 , C07D211/38 , C07D211/42 , C07D211/46 , C07D211/48 , C07D211/60 , C07D211/62 , C07D213/56 , C07D213/61 , C07D213/65 , C07D213/75 , C07D213/86 , C07D213/87 , C07D233/06 , C07D239/36 , C07D261/02 , C07D261/04 , C07D265/30 , C07D295/32 , C07D307/68 , C07D309/08 , C07D401/04 , C07D405/06 , C07D491/107 , C07D493/10
摘要： In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
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7.发明申请Diacylhydrazine Ligands for Modulating the Expression of Exogenous Genes in Mammalian Systems via an Ecdysone Receptor Complex 有权用于通过蜕皮激素受体复合物调节哺乳动物系统中外源基因表达的二酰基肼配体公开(公告)号：US20150005256A1
公开(公告)日：2015-01-01
申请号：US14254291
申请日：2014-04-16
申请人： Intrexon Corporation
IPC分类号： C07C243/38 , C12N15/85 , C07D319/20 , C07D213/87 , C07F7/18
CPC分类号： C07C243/38 , C07D213/87 , C07D311/58 , C07D311/66 , C07D319/20 , C07F7/1896 , C12N9/0069 , C12N15/85 , C12N2830/002
摘要： The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.
摘要翻译： 本发明涉及用于基于核受体的诱导型基因表达系统的非甾体配体，以及调节外源基因表达的方法，其中蜕皮激素受体复合物包含：DNA结合结构域; 配体结合域; 反式激活域 并且配体与包含以下的DNA构建体接触：外源基因和应答元件; 其中外源基因处于响应元件的控制之下，并且在配体存在下DNA结合结构域与响应元件的结合导致基因的激活或抑制。
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8.发明申请Bioavailable Diacylhydrazine Ligands for Modulating the Expression of Exogenous Genes via an Ecdysone Receptor Complex 审中-公开用于通过蜕皮激素受体复合物调节外源基因表达的生物可利用的二酰基肼配体公开(公告)号：US20140045903A1
公开(公告)日：2014-02-13
申请号：US13954376
申请日：2013-07-30
申请人： Intrexon Corporation
发明人： Robert Eugene HORMANN , David W. Potter , Orestes Chortyk , Colin M. Tice , Glenn Richard Carlson , Andrew Meyer , Thomas R. Opie
IPC分类号： C07D319/18 , C07D213/87 , C07C243/18
CPC分类号： C07C241/04 , A61K31/166 , A61K31/222 , A61K31/357 , A61K31/404 , A61K31/415 , A61K31/4184 , A61K31/455 , A61K31/4965 , C07C243/18 , C07C243/24 , C07C243/38 , C07C251/08 , C07C251/38 , C07C255/66 , C07C281/10 , C07C309/59 , C07C315/02 , C07C317/44 , C07C317/46 , C07D209/42 , C07D213/81 , C07D213/82 , C07D213/86 , C07D213/87 , C07D231/14 , C07D231/56 , C07D235/06 , C07D235/24 , C07D237/24 , C07D239/52 , C07D241/24 , C07D271/12 , C07D317/68 , C07D319/08 , C07D319/18 , C07D319/20 , C07D405/12 , C12N9/0069 , C12N15/635 , C12P21/00 , Y02A50/471
摘要： The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.
摘要翻译： 本发明涉及用于基于核受体的可诱导基因表达系统的非甾体配体和调节外源基因表达的方法，其中包含DNA结合结构域的蜕皮激素受体复合物; 配体结合域; 反式激活域 并且配体与包含以下的DNA构建体接触：外源基因和应答元件; 其中外源基因处于响应元件的控制之下，并且在配体存在下DNA结合结构域与响应元件的结合导致基因的激活或抑制。
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公开(公告)号：US06887863B2
公开(公告)日：2005-05-03
申请号：US10782502
申请日：2004-02-19
申请人： Richard A. Craig , Megumi Kawai , Linda M. Lynch , Jyoti R. Patel , George S. Sheppard , Jieyi Wang , Fan Yang , Nwe Ba-Maung , Xenia Beebe Searle
发明人： Richard A. Craig , Megumi Kawai , Linda M. Lynch , Jyoti R. Patel , George S. Sheppard , Jieyi Wang , Fan Yang , Nwe Ba-Maung , Xenia Beebe Searle
IPC分类号： C07C243/34 , C07C243/38 , C07C251/86 , C07C255/44 , C07C255/57 , C07C259/06 , C07C281/02 , C07C323/48 , C07C323/60 , C07C323/63 , C07D207/40 , C07D207/416 , C07D207/50 , C07D209/14 , C07D211/98 , C07D213/42 , C07D213/77 , C07D213/81 , C07D213/86 , C07D213/87 , C07D215/42 , C07D231/38 , C07D237/20 , C07D239/28 , C07D239/42 , C07D241/44 , C07D261/18 , C07D277/54 , C07D277/56 , C07D277/82 , C07D295/15 , C07D295/32 , C07D307/68 , C07D307/84 , C07D317/68 , C07D333/38 , C07D333/68 , C07D333/72 , A61K31/33 , A61K31/16 , A61K31/20
CPC分类号： C07D207/416 , C07B2200/07 , C07C243/34 , C07C243/38 , C07C251/86 , C07C255/44 , C07C255/57 , C07C259/06 , C07C281/02 , C07C323/48 , C07C323/60 , C07C323/63 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07D207/50 , C07D209/14 , C07D211/98 , C07D213/42 , C07D213/77 , C07D213/81 , C07D213/86 , C07D213/87 , C07D215/42 , C07D231/38 , C07D237/20 , C07D239/28 , C07D239/42 , C07D241/44 , C07D261/18 , C07D277/54 , C07D277/56 , C07D277/82 , C07D295/15 , C07D295/32 , C07D307/68 , C07D307/84 , C07D317/68 , C07D333/38 , C07D333/68 , C07D333/72
摘要： Compounds having the formula are methionine aminopeptidase type 2 (MetAP2) inhibitors and are useful for inhibiting angiogenesis. Also disclosed are MetAP2-inhibiting compositions and methods of inhibiting angiogenesis in a mammal.
摘要翻译： 具有下式的化合物是甲硫氨酸氨基肽酶2（MetAP2）抑制剂，可用于抑制血管发生。 还公开了抑制哺乳动物血管生成的MetAP2抑制组合物和方法。
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10.发明申请Use of tetra-azapentamethine compounds as direct dyeing agents and novel tetraazapentamethine compounds 失效使用四氮杂异丙酮化合物作为直接染色剂和新的四氮代五甲基化合物公开(公告)号：US20050028300A1
公开(公告)日：2005-02-10
申请号：US10489855
申请日：2003-07-04
IPC分类号： A61K8/00 , A61K8/49 , A61Q5/00 , A61Q5/08 , A61Q5/10 , C07D213/76 , C07D213/77 , C07D213/87 , C07D233/88 , C07D237/20 , C07D237/22 , C07D401/14 , C09B50/10 , C09B56/10 , D06P1/41 , D06P3/04 , A61K7/13
CPC分类号： C07D213/77 , C07D213/87 , C07D233/88 , C07D237/20 , C07D237/22 , C07D401/14 , C09B50/10
摘要： The invention concerns the use as direct dyeing agent of at least one tetraazapentamethine compound, a dyeing composition comprising at least such a compound, as well as a method for dyeing keratinous fibers, in particular human keratinous fibers and more particularly hair, which consists in applying at least one composition comprising such a compound. The composition also concerns tetra-azapentamethine compounds of formula (I). The invention further concerns a method for bleaching such compounds, as well as bleaching keratinous fibers previously dyed therewith.
摘要翻译： 本发明涉及作为至少一种四氮代十五指肠化合物的直接染色剂，至少包含这种化合物的染色组合物的用途，以及用于染色角质纤维，特别是人角质纤维，更特别是毛发的方法，其包括施用 至少一种包含这种化合物的组合物。 该组合物还涉及式（I）的四氮杂异戊肾上药化合物。 本发明还涉及漂白这些化合物的方法，以及漂白预先染色的角质纤维。
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