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公开(公告)号：US20240180916A1
公开(公告)日：2024-06-06
申请号：US18433881
申请日：2024-02-06
发明人： Gerard M. HOUSEY
IPC分类号： A61K31/5377 , A61K31/166 , A61K31/175 , A61K31/195 , A61K31/27 , A61K31/415 , A61K31/4196 , A61K31/44 , A61K31/4436 , A61K31/444 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/505 , A61K31/506 , A61K31/517 , A61K31/53 , C07C243/38 , C07D213/77 , C07D213/81 , C07D213/86 , C07D213/87 , C07D215/38 , C07D215/50 , C07D231/14 , C07D239/42 , C07D239/48 , C07D239/84 , C07D253/065 , C07D253/075 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , G01N33/50 , G01N33/573 , G01N33/574
CPC分类号： A61K31/5377 , A61K31/166 , A61K31/175 , A61K31/195 , A61K31/27 , A61K31/415 , A61K31/4196 , A61K31/44 , A61K31/4436 , A61K31/444 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/505 , A61K31/506 , A61K31/517 , A61K31/53 , C07C243/38 , C07D213/77 , C07D213/81 , C07D213/86 , C07D213/87 , C07D215/38 , C07D215/50 , C07D231/14 , C07D239/42 , C07D239/48 , C07D239/84 , C07D253/065 , C07D253/075 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , G01N33/5011 , G01N33/502 , G01N33/5041 , G01N33/573 , G01N33/574 , G01N2500/00 , G01N2500/10
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：US11925647B2
公开(公告)日：2024-03-12
申请号：US17857478
申请日：2022-07-05
发明人： Gerard M. Housey
IPC分类号： A61K31/5377 , A61K31/166 , A61K31/175 , A61K31/195 , A61K31/27 , A61K31/415 , A61K31/4196 , A61K31/44 , A61K31/4436 , A61K31/444 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/505 , A61K31/506 , A61K31/517 , A61K31/53 , C07C243/38 , C07D213/77 , C07D213/81 , C07D213/86 , C07D213/87 , C07D215/38 , C07D215/50 , C07D231/14 , C07D239/42 , C07D239/48 , C07D239/84 , C07D253/065 , C07D253/075 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , G01N33/50 , G01N33/573 , G01N33/574
CPC分类号： A61K31/5377 , A61K31/166 , A61K31/175 , A61K31/195 , A61K31/27 , A61K31/415 , A61K31/4196 , A61K31/44 , A61K31/4436 , A61K31/444 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/505 , A61K31/506 , A61K31/517 , A61K31/53 , C07C243/38 , C07D213/77 , C07D213/81 , C07D213/86 , C07D213/87 , C07D215/38 , C07D215/50 , C07D231/14 , C07D239/42 , C07D239/48 , C07D239/84 , C07D253/065 , C07D253/075 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , G01N33/5011 , G01N33/502 , G01N33/5041 , G01N33/573 , G01N33/574 , G01N2500/00 , G01N2500/10
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：US20180194718A1
公开(公告)日：2018-07-12
申请号：US15806722
申请日：2017-11-08
发明人： Erik Fenster , Melissa Fleury , Adam D. Hughes
IPC分类号： C07C243/38 , C07D493/10 , C07D491/107 , A61K31/192 , C07D405/06 , C07D401/04 , C07D309/08 , C07D307/68 , C07D295/32 , C07D265/30 , C07D261/04 , C07D261/02 , C07D239/36 , C07D233/06 , C07D213/87 , C07D213/86 , C07D213/75 , C07D213/65 , C07D213/61 , C07D213/56 , C07D211/62 , C07D211/60 , C07D211/48 , C07D211/46 , C07D211/42 , C07D211/38 , C07D211/22 , C07D207/16 , C07D207/14 , C07D207/12 , C07D207/09 , C07D207/08 , C07D205/04 , C07C259/04 , C07C243/32 , C07C243/24 , C07C235/80 , C07C235/78 , C07C235/74 , C07C235/34 , C07C235/20 , C07C235/12 , C07C233/56 , A61K45/06 , A61K31/5375 , A61K31/495 , A61K31/4409 , A61K31/4406 , A61K31/44 , A61K31/42 , A61K31/4015 , A61K31/40 , A61K31/397 , A61K31/341 , A61K31/197
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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公开(公告)号：US09579326B2
公开(公告)日：2017-02-28
申请号：US14297863
申请日：2014-06-06
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
CPC分类号： A61K31/5377 , A61K31/166 , A61K31/175 , A61K31/195 , A61K31/27 , A61K31/415 , A61K31/4196 , A61K31/44 , A61K31/4436 , A61K31/444 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/505 , A61K31/506 , A61K31/517 , A61K31/53 , C07C243/38 , C07D213/77 , C07D213/81 , C07D213/86 , C07D213/87 , C07D215/38 , C07D215/50 , C07D231/14 , C07D239/42 , C07D239/48 , C07D239/84 , C07D253/065 , C07D253/075 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , G01N33/5011 , G01N33/502 , G01N33/5041 , G01N33/573 , G01N33/574 , G01N2500/00 , G01N2500/10
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.
摘要翻译： 本发明涉及作为内源性蛋白质的变体形式的抑制剂或活化剂的试剂，以及鉴定这些变体的新方法。 特别令人感兴趣的是内源性蛋白质变体的抑制剂和活化剂，其由具有突变的基因编码，所述变体经常出现或至少首先被鉴定为在暴露于化学试剂之后产生，已知其是相应的抑制剂或活化剂 未突变的内源蛋白
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公开(公告)号：US20170015619A1
公开(公告)日：2017-01-19
申请号：US15219478
申请日：2016-07-26
发明人： Erik Fenster , Melissa Fleury , Adam D. Hughes
IPC分类号： C07C243/38 , A61K31/44 , C07D213/86 , A61K45/06 , A61K31/4406 , C07D307/68 , A61K31/341 , A61K31/192 , C07D213/87 , A61K31/4409
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.
摘要翻译： 其中R1-R5和X如说明书中所定义，或其药学上可接受的盐。 这些化合物具有去血清抑制活性。 另一方面，本发明涉及包含这些化合物的药物组合物; 使用这些化合物的方法; 以及制备这些化合物的方法和中间体。
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公开(公告)号：US09255273B2
公开(公告)日：2016-02-09
申请号：US13604001
申请日：2012-09-05
申请人： Robert Eugene Hormann , David W. Potter , Orestes Chortyk , Colin M. Tice , Glenn Richard Carlson , Andrew Meyer , Thomas R. Opie
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： C12P21/06 , C12N15/63 , C07C243/24 , C07C243/38 , C07C251/08 , C07C251/38 , C07C255/66 , C07C281/10 , C07C309/59 , C07C317/44 , C07C317/46 , C07D209/42 , C07D213/81 , C07D213/82 , C07D231/14 , C07D231/56 , C07D235/06 , C07D237/24 , C07D239/52 , C07D241/24 , C07D271/12 , C07D317/68 , C07D319/18 , C07D405/12 , C07C243/18 , C07D213/87 , C07D319/20 , C12N9/02 , C12P21/00
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.
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公开(公告)号：US09102648B1
公开(公告)日：2015-08-11
申请号：US11841617
申请日：2007-08-20
申请人： Robert Eugene Hormann , David W. Potter , Orestes Chortyk , Colin M. Tice , Glenn Richard Carlson , Andrew Meyer , Thomas R. Opie
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： C12P21/06 , C07D319/20 , C12N9/02
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.
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公开(公告)号：US08846677B2
公开(公告)日：2014-09-30
申请号：US13472090
申请日：2012-05-15
IPC分类号： A61K31/501 , C07D401/00 , C07D409/00
CPC分类号： C07D213/74 , C07D213/84 , C07D213/87 , C07D237/20 , C07D403/04 , C07D403/12 , C07D417/10
摘要： Novel compounds which interact with the histamine H3 receptor are defined. These compounds are particularly useful in the treatment of a variety of diseases or conditions in which histamine H3 interactions are beneficial. Thus, the compounds may find use, e.g., in the treatment of diseases of the central nervous system, the peripheral nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system. The novel compounds have a core consisting of a 6 membered aromatic ring containing at least one nitrogen atom and two carbon atoms in the ring and, at the remaining positions in the ring, there is either a carbon or a nitrogen atom.
摘要翻译： 定义与组胺H3受体相互作用的新型化合物。 这些化合物特别可用于治疗组胺H3相互作用有益的各种疾病或病症。 因此，该化合物可用于例如治疗中枢神经系统，周围神经系统，心血管系统，肺系统，胃肠系统和内分泌系统的疾病。 该新化合物具有由在环中含有至少一个氮原子和两个碳原子的6元芳香环组成的核心，并且在该环的其余位置上有碳原子或氮原子。
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公开(公告)号：US08633323B2
公开(公告)日：2014-01-21
申请号：US12934903
申请日：2009-03-31
申请人： Shoujun Chen , Jun Jiang , Lijun Sun , Keizo Koya
发明人： Shoujun Chen , Jun Jiang , Lijun Sun , Keizo Koya
IPC分类号： C07D213/44 , C07C327/00
CPC分类号： C07C327/56 , C07C2601/02 , C07D213/86 , C07D213/87
摘要： Disclosed herein are methods of preparing a bis(thio-hydrazide amides) compounds of the following structural formula: wherein R1, R2, R3, R4, R5, R6 and R13 are defined herein.
摘要翻译： 本文公开了制备以下结构式的双（硫代酰肼酰胺）化合物的方法：其中R1，R2，R3，R4，R5，R6和R13如本文所定义。
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公开(公告)号：US08501739B2
公开(公告)日：2013-08-06
申请号：US11917823
申请日：2006-06-30
IPC分类号： A61K31/50 , C07D401/00
CPC分类号： C07D213/74 , C07D213/84 , C07D213/87 , C07D237/20 , C07D403/04 , C07D403/12 , C07D417/10
摘要： Novel compounds which interact with the histamine H3 receptor are defined. These compounds are particularly useful in the treatment of a variety of diseases or conditions in which histamine H3 interactions are beneficial. Thus, the compounds may find use, e.g., in the treatment of diseases of the central nervous system, the peripheral nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system. The novel compounds have a core consisting of a 6 membered aromatic ring containing at least one nitrogen atom and two carbon atoms in the ring and, at the remaining positions in the ring, there is either a carbon or a nitrogen atom.
摘要翻译： 定义与组胺H3受体相互作用的新型化合物。 这些化合物特别可用于治疗组胺H3相互作用有益的各种疾病或病症。 因此，该化合物可用于例如治疗中枢神经系统，周围神经系统，心血管系统，肺系统，胃肠系统和内分泌系统的疾病。 该新化合物具有由在环中含有至少一个氮原子和两个碳原子的6元芳香环组成的核心，并且在该环的其余位置上有碳原子或氮原子。
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