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公开(公告)号：US20230242486A1
公开(公告)日：2023-08-03
申请号：US18007840
申请日：2021-05-28
发明人： Jianqi LI , Yangli QI , Xiaowen CHEN , Junwei XU , Ruixiang YUAN , Qiang PU
IPC分类号： C07D213/74 , C07D213/87 , C07D401/04 , C07D405/14 , C07D405/12 , C07D405/04 , C07D409/04 , C07D409/14
CPC分类号： C07D213/74 , C07D213/87 , C07D401/04 , C07D405/14 , C07D405/12 , C07D405/04 , C07D409/04 , C07D409/14
摘要： Disclosed in the present invention are a pyridinyl morpholine compound, a preparation method therefor, and an application thereof. The present invention provides a pyridinyl morpholine compound as represented by formula I, a pharmaceutically acceptable salt thereof or a hydrate of the pharmaceutically acceptable salt thereof. The compound can be used as an antagonist for one or more of D2, D3 or 5-HT2A, and is used for preparing a drug for treating schizophrenia.
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公开(公告)号：US20220370469A1
公开(公告)日：2022-11-24
申请号：US17857478
申请日：2022-07-05
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：US10053417B2
公开(公告)日：2018-08-21
申请号：US15806722
申请日：2017-11-08
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 , A61K31/341 , A61K31/4409 , C07D213/86 , C07D213/87 , C07C235/80 , A61K31/4406 , A61K31/192 , C07D213/65 , A61K45/06 , A61K31/495 , A61K31/4015 , C07D307/68 , C07D213/61 , C07D211/62 , C07D211/60 , C07D211/48 , C07D211/46 , C07D211/42 , C07D211/38 , C07D211/22 , C07C243/32 , C07C243/24 , C07D493/10 , C07D207/16 , C07D207/12 , C07D207/08 , C07D265/30 , C07C235/78 , C07C235/74 , C07C235/20 , C07C235/12 , C07C233/56 , C07D261/02 , C07D239/36 , C07D405/06 , C07D401/04 , C07D233/06 , C07D309/08 , C07C259/04 , C07D213/75 , C07D491/107
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：US20180042935A1
公开(公告)日：2018-02-15
申请号：US15789476
申请日：2017-10-20
发明人： Gerard M. Housey
IPC分类号： A61K31/5377 , C07D403/12 , C07D253/075 , C07D215/38 , C07D213/86 , C07D213/77 , C07C243/38 , A61K31/444 , A61K31/415 , A61K31/4196 , A61K31/44 , A61K31/4436 , A61K31/517 , A61K31/495 , A61K31/166 , A61K31/175 , A61K31/195 , A61K31/27 , A61K31/4709 , A61K31/505 , A61K31/506 , A61K31/53 , G01N33/50 , A61K31/47 , G01N33/574 , C07D409/12 , C07D405/12 , C07D401/12 , C07D253/065 , C07D239/84 , C07D239/48 , C07D239/42 , C07D231/14 , C07D215/50 , C07D213/87 , G01N33/573 , C07D213/81
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：US20170327459A1
公开(公告)日：2017-11-16
申请号：US15600998
申请日：2017-05-22
发明人： Erik Fenster , Melissa Fleury , Adam D. Hughes
IPC分类号： C07C243/38 , 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 , C07D493/10 , C07C2601/16 , C07C2601/08
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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76.发明授权Bioavailable diacylhydrazine ligands for modulating the expression of exogenous genes via an ecdysone receptor complex 有权生物可利用的二酰肼配体，用于通过蜕皮激素受体复合物调节外源基因的表达公开(公告)号：US09359289B2
公开(公告)日：2016-06-07
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： C07C243/24 , C07D319/18 , C07C241/04 , 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 , C07D405/12 , C07C243/18 , C07D213/87 , C07D319/20 , C12N9/02 , C12N15/63 , C12P21/00 , A61K31/166 , A61K31/222 , A61K31/357 , A61K31/404 , A61K31/415 , A61K31/4184 , A61K31/455 , A61K31/4965 , C07C315/02 , C07D213/86 , C07D235/24 , C07D319/08
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DNA构建体接触，所述DNA构建体包含： 外源基因和响应元件; 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：US20110257199A1
公开(公告)日：2011-10-20
申请号：US13162907
申请日：2011-06-17
申请人： Richard R. Tidwell , David W. Boykin , W. David Wilson , Reto Brun , Karl Werbovetz , Mohamed A. Ismail , Reem K. Arafa , Laixing Hu
发明人： Richard R. Tidwell , David W. Boykin , W. David Wilson , Reto Brun , Karl Werbovetz , Mohamed A. Ismail , Reem K. Arafa , Laixing Hu
IPC分类号： A61K31/506 , A61K31/444 , C07D239/42 , A61K31/505 , C07D213/87 , A61P33/00 , C07D401/14 , C07D401/10 , C07C279/18 , A61K31/155 , C07D405/14 , A61K31/4178 , C07D401/04 , A61K31/4418
CPC分类号： C07C257/18 , C07C259/18 , C07C279/18 , C07C279/24 , C07D213/58 , C07D239/26 , C07D307/68 , C07D401/04 , C07D401/14 , C07D405/04 , C07D405/14
摘要： Novel dicationic terphenyl compounds and their aza analogues. Methods for combating microbial infections with novel dicationic terphenyl compounds and their aza analogues. Processes for synthesizing novel dicationic terphenyl compounds and their aza analogues.
摘要翻译： 新型的二联三联苯化合物及其杂环类似物。 用新型双极化三联苯化合物及其氮杂类似物对抗微生物感染的方法。 合成新型双线性三联苯化合物及其氮杂类似物的方法。
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公开(公告)号：US20110046088A1
公开(公告)日：2011-02-24
申请号：US12528198
申请日：2008-02-20
IPC分类号： A01N55/10 , C07D213/74 , A01N43/40 , C07F7/10 , C07D401/12 , C07D213/87 , A01N43/50 , A01N43/56 , A01N43/713 , A01P1/00
CPC分类号： C07D213/74 , A01N43/40 , A01N43/42 , A01N43/50 , A01N43/54 , A01N43/653 , A01N43/713 , A01N43/72 , A01N43/84 , A01N55/00 , C07D213/16 , C07D213/85 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D407/04 , C07D407/10 , C07D409/10 , C07D413/12 , C07D417/10 , C07F7/0812
摘要： Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as microbiocides.
摘要翻译： 其中取代基如权利要求1中所定义的式（I）化合物适合用作杀微生物剂。
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79.发明申请Pharmaceutical Combinations Comprising Specified Age Breaker and Further Drugs, I.A. Antihypertensive Drugs, Antidiabetic Drugs Etc. 审中-公开药物组合包括特定的破碎者和其他药物，I.A. 抗高血压药物，抗糖尿病药物等公开(公告)号：US20110034378A1
公开(公告)日：2011-02-10
申请号：US12735472
申请日：2009-01-21
申请人： Chaitanya Dutt , Deepa Joshi , Ram Gupta , Kumarprafull Chandra
发明人： Chaitanya Dutt , Deepa Joshi , Ram Gupta , Kumarprafull Chandra
IPC分类号： A61K31/4425 , A61K31/4545 , A61K31/4439 , A61K31/4436 , A61K31/55 , A61K31/472 , A61K31/675 , A61K31/549 , A61K31/397 , A61K38/26 , A61K38/28 , A61K31/704 , A61P9/04 , A61P9/12 , A61P9/10 , A61P9/00 , A61P13/12 , A61P3/10 , A61P3/04 , A61P7/02 , C07D213/86 , C07D213/87 , C07D405/14 , C07D401/12 , C07D401/06 , C07D409/06 , C07D417/06
CPC分类号： A61K31/155 , A61K31/00 , A61K31/40 , A61K31/44 , A61K31/4422 , A61K31/4436 , A61K31/4439 , A61K31/7048 , A61K45/06 , A61K2300/00
摘要： The present invention relates to a combination, such as a combined preparation or pharmaceutical composition comprising: (a) compound of formula (I), and/or (II) or a pharmaceutically acceptable salt thereof; (b) at least one therapeutic agent selected from the group consisting of: an antihypertensive agent; an antidiabetics agent; a hypolipidemic agent; an antiplatelet agent; an antiobesity agent; an antithrombotic agent; an agent for diabetic vascular complications; and an agent for treatment of heart failure; or a pharmaceutically acceptable salts thereof, optionally in presence of a pharmaceutically acceptable carrier for separate, simultaneous or sequential use. The present invention also relates to a use of such combination for the treatment of mammal including human being. R1, R2, R3, R1, R2, R3, R4, R5, X, Y, A and B and m are as defined in the specification.
摘要翻译： 本发明涉及组合，例如组合制剂或药物组合物，其包含：（a）式（I）和/或（II）化合物或其药学上可接受的盐; （b）至少一种选自以下的治疗剂：抗高血压药; 抗糖尿病药; 降血脂药; 抗血小板药; 抗生素; 抗血栓剂; 糖尿病血管并发症的药剂; 和治疗心力衰竭的药剂; 或其药学上可接受的盐，任选地在用于分离，同时或顺序使用的药学上可接受的载体的存在下。 本发明还涉及这种组合用于治疗包括人的哺乳动物的用途。 R1，R2，R3，R1，R2，R3，R4，R5，X，Y，A和B和m如说明书中所定义。
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公开(公告)号：US20050182103A1
公开(公告)日：2005-08-18
申请号：US10508043
申请日：2003-03-24
申请人： Paul Finke , Laura Meurer , John Debenham , Richard Toupence , Thomas Walsh
发明人： Paul Finke , Laura Meurer , John Debenham , Richard Toupence , Thomas Walsh
IPC分类号： C07D213/64 , A61K31/44 , A61K31/4418 , A61K31/4439 , A61K31/4545 , A61K31/455 , A61K31/496 , A61K31/5377 , A61K45/00 , A61K47/02 , A61K47/10 , A61K47/26 , A61K47/34 , A61P1/04 , A61P1/10 , A61P1/16 , A61P3/04 , A61P9/00 , A61P11/06 , A61P25/00 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/30 , A61P29/00 , A61P43/00 , C07D213/56 , C07D213/65 , C07D213/79 , C07D213/80 , C07D213/81 , C07D213/82 , C07D213/85 , C07D213/86 , C07D213/87 , C07D401/12 , C07D41/02
CPC分类号： C07D213/79 , C04B35/632 , C07D213/65 , C07D213/80 , C07D213/81 , C07D213/82 , C07D213/85 , C07D213/86 , C07D213/87 , C07D401/12
摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
摘要翻译： 结构式（I）的新型化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，可用于治疗，预防和抑制由CB1受体介导的疾病。 本发明的化合物可用作治疗精神病，记忆缺陷，认知障碍，偏头痛，神经病，包括多发性硬化和神经 - 巴利综合征的神经炎症性疾病以及病毒性脑炎的炎症性后遗症，脑血管 事故和头部创伤，焦虑障碍，压力，癫痫，帕金森病，运动障碍和精神分裂症。 这些化合物还可用于治疗药物滥用障碍，治疗肥胖或进食障碍，以及治疗哮喘，便秘，慢性肠假性梗阻和肝硬化。
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