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1.发明申请NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES 有权用于治疗衰老和炎症疾病的新型化合物公开(公告)号：US20150031706A1
公开(公告)日：2015-01-29
申请号：US14457071
申请日：2014-08-11
IPC分类号： C07D471/04 , A61K45/06 , A61K31/496
CPC分类号： A61K31/496 , A61K31/437 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D471/04 , C07D491/107
摘要： A pyrazolopyridine compound according to Formula I, able to inhibit JAK is disclosed, as well as pharmaceutically acceptable salts, a solvate thereof, solvates of the pharmaceutically acceptable salts and biologically active metabolites thereof. The compound may be prepared as a pharmaceutical composition, and may be used for the treatment or prophylaxis of a variety of conditions in mammals including humans, and particularly, such conditions as may be associated with aberrant JAK activity, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6.
摘要翻译： 公开了能够抑制JAK的式I的吡唑并吡啶化合物，以及其药学上可接受的盐，其溶剂化物，其药学上可接受的盐和其生物活性代谢物的溶剂合物。 该化合物可以制备为药物组合物，并且可以用于治疗或预防包括人在内的哺乳动物中的各种病症，特别是可能与异常JAK活性相关的病症，包括以非限制性的方式 例如，过敏，炎性病症，自身免疫性疾病，增殖性疾病，移植排斥，涉及软骨周转损伤的疾病，先天性软骨畸形和/或与IL6分泌过多相关的疾病。
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2.发明授权公开(公告)号：US08802682B2
公开(公告)日：2014-08-12
申请号：US13459055
申请日：2012-04-27
IPC分类号： A61K31/496 , C07D471/04
CPC分类号： A61K31/496 , A61K31/437 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D471/04 , C07D491/107
摘要： A pyrazolopyridine compound according to Formula I, able to inhibit JAK is disclosed, as well as pharmaceutically acceptable salts, a solvate thereof, solvates of the pharmaceutically acceptable salts and biologically active metabolites thereof. The compound may be prepared as a pharmaceutical composition, and may be used for the treatment or prophylaxis of a variety of conditions in mammals including humans, and particularly, such conditions as may be associated with aberrant JAK activity, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6.
摘要翻译： 公开了能够抑制JAK的式I的吡唑并吡啶化合物，以及其药学上可接受的盐，其溶剂化物，其药学上可接受的盐和其生物活性代谢物的溶剂合物。 该化合物可以制备为药物组合物，并且可以用于治疗或预防包括人在内的哺乳动物中的各种病症，特别是可能与异常JAK活性相关的病症，包括非限制性地 例如，过敏，炎性病症，自身免疫性疾病，增殖性疾病，移植排斥，涉及软骨周转损伤的疾病，先天性软骨畸形和/或与IL6分泌过多相关的疾病。
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3.发明申请NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES 有权用于治疗衰老和炎症疾病的新型化合物公开(公告)号：US20120277247A1
公开(公告)日：2012-11-01
申请号：US13459055
申请日：2012-04-27
IPC分类号： A61K31/496 , A61P37/08 , A61P19/02 , A61P37/06 , A61P35/00 , C07D471/04 , A61P29/00
CPC分类号： A61K31/496 , A61K31/437 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D471/04 , C07D491/107
摘要： A pyrazolopyridine compound according to Formula I, able to inhibit JAK is disclosed, as well as pharmaceutically acceptable salts, a solvate thereof, solvates of the pharmaceutically acceptable salts and biologically active metabolites thereof. The compound may be prepared as a pharmaceutical composition, and may be used for the treatment or prophylaxis of a variety of conditions in mammals including humans, and particularly, such conditions as may be associated with aberrant JAK activity, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6.
摘要翻译： 公开了能够抑制JAK的式I的吡唑并吡啶化合物，以及其药学上可接受的盐，其溶剂化物，其药学上可接受的盐和其生物活性代谢物的溶剂合物。 该化合物可以制备为药物组合物，并且可以用于治疗或预防包括人在内的哺乳动物中的各种病症，特别是可能与异常JAK活性相关的病症，包括非限制性地 例如，过敏，炎性病症，自身免疫性疾病，增殖性疾病，移植排斥，涉及软骨周转损伤的疾病，先天性软骨畸形和/或与IL6分泌过多相关的疾病。
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4.发明授权公开(公告)号：US09241931B2
公开(公告)日：2016-01-26
申请号：US14457071
申请日：2014-08-11
IPC分类号： A61K31/496 , C07D471/04 , A61K31/437 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D491/107
CPC分类号： A61K31/496 , A61K31/437 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D471/04 , C07D491/107
摘要： A pyrazolopyridine compound according to Formula I, able to inhibit JAK is disclosed, as well as pharmaceutically acceptable salts, a solvate thereof, solvates of the pharmaceutically acceptable salts and biologically active metabolites thereof. The compound may be prepared as a pharmaceutical composition, and may be used for the treatment or prophylaxis of a variety of conditions in mammals including humans, and particularly, such conditions as may be associated with aberrant JAK activity, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6.
摘要翻译： 公开了能够抑制JAK的式I的吡唑并吡啶化合物，以及其药学上可接受的盐，其溶剂化物，其药学上可接受的盐和其生物活性代谢物的溶剂合物。 该化合物可以制备为药物组合物，并且可以用于治疗或预防包括人在内的哺乳动物中的各种病症，特别是可能与异常JAK活性相关的病症，包括非限制性地 例如，过敏，炎性病症，自身免疫性疾病，增殖性疾病，移植排斥，涉及软骨周转损伤的疾病，先天性软骨畸形和/或与IL6分泌过多相关的疾病。
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公开(公告)号：US20080269206A1
公开(公告)日：2008-10-30
申请号：US12058371
申请日：2008-03-28
申请人： Michael Geoffrey Neil Russell , Huw David Vater , Jacqueline Anne Macritchie , Kevin James Doyle , David Brown , Joanne Peach
发明人： Michael Geoffrey Neil Russell , Huw David Vater , Jacqueline Anne Macritchie , Kevin James Doyle , David Brown , Joanne Peach
IPC分类号： A61K31/5415 , C07C243/32 , A61K31/165 , A61K31/47 , A61P1/12 , C12N5/06 , C07D215/52 , C07D279/26
CPC分类号： C07C251/86 , C07C271/22 , C07C311/08 , C07C311/21 , C07C317/44 , C07C323/60 , C07C2601/14 , C07C2602/08 , C07D207/325 , C07D207/327 , C07D209/08 , C07D209/42 , C07D213/74 , C07D213/81 , C07D213/82 , C07D215/36 , C07D215/52 , C07D231/06 , C07D231/14 , C07D237/04 , C07D239/28 , C07D239/92 , C07D263/34 , C07D277/06 , C07D277/30 , C07D277/56 , C07D279/22 , C07D285/06 , C07D295/192 , C07D307/79 , C07D333/22 , C07D333/38 , C07D333/70 , C07D339/06 , C07D401/04 , C07D405/06 , C07D409/04 , C07D495/04
摘要： The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-6 or encompassed by formulas I-VI) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.
摘要翻译： 本发明涉及用于治疗动物疾病的组合物和方法，该疾病通过对有需要的哺乳动物施用有效量的本文定义的化合物来对功能性囊性纤维化跨膜传导调节因子（CFTR）多肽的抑制作出反应 包括表1-6所示或由式I-VI所包括的那些化合物或其组合物，从而治疗疾病。 本发明特别涉及一种治疗腹泻和多囊肾病的方法。
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公开(公告)号：US20180078547A1
公开(公告)日：2018-03-22
申请号：US15694454
申请日：2017-09-01
IPC分类号： A61K31/496 , C07D491/107 , C07D471/04 , A61K31/437 , A61K31/541 , A61K31/5377 , A61K45/06
CPC分类号： A61K31/496 , A61K31/437 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D471/04 , C07D491/107
摘要： A pyrazolopyridine compound according to Formula I, able to inhibit JAK is disclosed, as well as pharmaceutically acceptable salts, a solvate thereof, solvates of the pharmaceutically acceptable salts and biologically active metabolites thereof. The compound may be prepared as a pharmaceutical composition, and may be used for the treatment or prophylaxis of a variety of conditions in mammals including humans, and particularly, such conditions as may be associated with aberrant JAK activity, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6.
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7.发明申请NOVEL COMPOUND USEFUL FOR THE TREATEMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES 有权用于治疗衰老和炎症疾病的新型化合物公开(公告)号：US20160213666A1
公开(公告)日：2016-07-28
申请号：US15005442
申请日：2016-01-25
IPC分类号： A61K31/496 , A61K45/06 , C07D471/04
CPC分类号： A61K31/496 , A61K31/437 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D471/04 , C07D491/107
摘要： A pyrazolopyridine compound according to Formula I, able to inhibit JAK is disclosed, as well as pharmaceutically acceptable salts, a solvate thereof, solvates of the pharmaceutically acceptable salts and biologically active metabolites thereof. The compound may be prepared as a pharmaceutical composition, and may be used for the treatment or prophylaxis of a variety of conditions in mammals including humans, and particularly, such conditions as may be associated with aberrant JAK activity, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6.
摘要翻译： 公开了能够抑制JAK的式I的吡唑并吡啶化合物，以及其药学上可接受的盐，其溶剂化物，其药学上可接受的盐和其生物活性代谢物的溶剂合物。 该化合物可以制备为药物组合物，并且可以用于治疗或预防包括人在内的哺乳动物中的各种病症，特别是可能与异常JAK活性相关的病症，包括以非限制性的方式 例如，过敏，炎性病症，自身免疫性疾病，增殖性疾病，移植排斥，涉及软骨周转损伤的疾病，先天性软骨畸形和/或与IL6分泌过多相关的疾病。
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公开(公告)号：US09987272B2
公开(公告)日：2018-06-05
申请号：US15005442
申请日：2016-01-25
IPC分类号： A61K31/496 , C07D471/04 , A61K31/437 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D491/107
CPC分类号： A61K31/496 , A61K31/437 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D471/04 , C07D491/107
摘要： A pyrazolopyridine compound according to Formula I, able to inhibit JAK is disclosed, as well as pharmaceutically acceptable salts, a solvate thereof, solvates of the pharmaceutically acceptable salts and biologically active metabolites thereof. The compound may be prepared as a pharmaceutical composition, and may be used for the treatment or prophylaxis of a variety of conditions in mammals including humans, and particularly, such conditions as may be associated with aberrant JAK activity, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6.
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9.发明授权公开(公告)号：US08975406B2
公开(公告)日：2015-03-10
申请号：US14114218
申请日：2012-04-26
IPC分类号： A61K31/44 , C07D471/02 , A61K31/437 , C07D471/04 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D491/107
CPC分类号： A61K31/496 , A61K31/437 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D471/04 , C07D491/107
摘要： Novel pyrrazolopyridines according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prophylaxis and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons.
摘要翻译： 公开了能够抑制JAK的根据式I的新的吡唑并吡啶，这些化合物可以制备成药物组合物，并且可以用于预防和治疗哺乳动物包括人的各种病症，包括以非限制性方式 例如过敏，炎性病症，自身免疫性疾病，增殖性疾病，移植排斥，涉及软骨周转损伤的疾病，先天性软骨畸形和/或与IL6或干扰素分泌过多相关的疾病。
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10.发明申请NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES 有权用于治疗衰老和炎症疾病的新型化合物公开(公告)号：US20140051677A1
公开(公告)日：2014-02-20
申请号：US14114218
申请日：2012-04-26
IPC分类号： A61K31/541 , A61K31/437 , A61K45/06 , A61K31/5377 , C07D491/107 , C07D471/04 , A61K31/496
CPC分类号： A61K31/496 , A61K31/437 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D471/04 , C07D491/107
摘要： Novel pyrrazolopyridines according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prophylaxis and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons.
摘要翻译： 公开了能够抑制JAK的根据式I的新的吡唑并吡啶，这些化合物可以制备成药物组合物，并且可以用于预防和治疗哺乳动物包括人的各种病症，包括以非限制性方式 例如过敏，炎性病症，自身免疫性疾病，增殖性疾病，移植排斥，涉及软骨周转损伤的疾病，先天性软骨畸形和/或与IL6或干扰素分泌过多相关的疾病。
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