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公开(公告)号：US09018207B2
公开(公告)日：2015-04-28
申请号：US14229746
申请日：2014-03-28
IPC分类号： A61K31/50 , A61K31/495 , A61K31/44 , A61K31/47 , A61K31/41 , C07D471/04 , A61K31/517 , A61K38/08 , G01N33/74 , C07D409/14 , C07D239/90 , C07D401/06 , C07D403/10 , C07D403/14 , C07D409/06 , C07D413/12
CPC分类号： C07D471/04 , A61K31/517 , A61K38/08 , C07D239/90 , C07D401/06 , C07D403/10 , C07D403/14 , C07D409/06 , C07D409/14 , C07D413/12 , G01N33/74 , G01N2500/00
摘要： The present invention is directed to methods and agents that are useful in the prevention and amelioration of signs and symptoms associated with neuropathic conditions. More particularly, the present invention discloses the use of angiotensin II receptor 2 (AT2 receptor) antagonists for the treatment, prophylaxis, reversal and/or symptomatic relief of neuropathic pain, including mechanical hyperalgesia, thermal or mechanical allodynia, diabetic pain and entrapment pain, in vertebrate animals and particularly in human subjects. The AT2 receptor antagonists may be provided alone or in combination with other compounds such as those that are useful in the control of neuropathic conditions.
摘要翻译： 本发明涉及可用于预防和改善与神经病变相关的体征和症状的方法和试剂。 更具体地，本发明公开了血管紧张素II受体2（AT2受体）拮抗剂用于治疗，预防，逆转和/或症状缓解神经性疼痛，包括机械性痛觉过敏，热或机械异常性疼痛，糖尿病性疼痛和包埋性疼痛， 在脊椎动物，特别是在人类受试者。 AT2受体拮抗剂可以单独提供或与其它化合物组合提供，例如可用于控制神经病症的化合物。
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公开(公告)号：US20150105422A1
公开(公告)日：2015-04-16
申请号：US14573774
申请日：2014-12-17
发明人： Thomas David McCarthy , Craig James Stewart Boyle , Alexander Redvers Eberlin , Peter Michael Kelly
IPC分类号： C07D217/26
CPC分类号： C07D217/26 , A61K31/47
摘要： (S)-2-(Diphenylacetyl)-1,2,3,4-tetrahydro-6-methoxy-5-(phenylmethoxy)-3-isoquinoline carboxylic acid in substantially pure form is described together with its sodium salt and solvates. Methods for preparing the compound, its sodium salt and its solvates and pharmaceutical compositions comprising them are also described.
摘要翻译： 与其钠盐和溶剂化物一起描述基本上纯的形式的（S）-2-（二苯基乙酰基）-1,2,3,4-四氢-6-甲氧基-5-（苯基甲氧基）-3-异喹啉羧酸。 还描述了制备化合物，其钠盐及其溶剂合物的方法和包含它们的药物组合物。
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公开(公告)号：US09162985B2
公开(公告)日：2015-10-20
申请号：US14573774
申请日：2014-12-17
发明人： Thomas David McCarthy , Craig James Stewart Boyle , Alexander Redvers Eberlin , Peter Michael Kelly
IPC分类号： C07D217/26 , A61K31/47
CPC分类号： C07D217/26 , A61K31/47
摘要： (S)-2-(Diphenylacetyl)-1,2,3,4-tetrahydro-6-methoxy-5-(phenylmethoxy)-3-isoquinoline carboxylic acid in substantially pure form is described together with its sodium salt and solvates. Methods for preparing the compound, its sodium salt and its solvates and pharmaceutical compositions comprising them are also described.
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公开(公告)号：US20150011565A1
公开(公告)日：2015-01-08
申请号：US14373355
申请日：2013-01-25
发明人： Thomas David McCarthy , Alan Naylor
IPC分类号： C07D295/185 , C07D231/12
CPC分类号： C07D241/04 , C07D231/12 , C07D243/08 , C07D295/185 , C07D403/04 , C07D413/04 , C07D413/06
摘要： The present invention relates to heterocyclic compounds useful for antagonizing angiotensin II Type 2 (AT2) receptor. More particularly the invention relates to piperazine and diazepine compounds, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with AT2 receptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.
摘要翻译： 本发明涉及可用于拮抗血管紧张素II型2型（AT2）受体的杂环化合物。 更具体地，本发明涉及哌嗪和二氮杂化合物，其含有它们的组合物及其在治疗或预防与AT2受体功能相关的病症或疾病的方法中的用途，包括神经性疼痛，炎性疼痛，与神经元超敏反应相关的病症，神经传导速度受损，细胞 增生障碍，与骨吸收和骨形成之间的不平衡相关的疾病以及与异常神经再生有关的疾病。
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公开(公告)号：US08927575B2
公开(公告)日：2015-01-06
申请号：US14083391
申请日：2013-11-18
发明人： Thomas David McCarthy , Craig James Stewart Boyle , Alexander Redvers Eberlin , Peter Michael Kelly
IPC分类号： C07D217/26 , A61K31/47
CPC分类号： C07D217/26 , A61K31/47
摘要： (S)-2-(Diphenylacetyl)-1,2,3,4-tetrahydro-6-methoxy-5-(phenylmethoxy)-3-isoquinoline carboxylic acid in substantially pure form is described together with its sodium salt and solvates. Methods for preparing the compound, its sodium salt and its solvates and pharmaceutical compositions comprising them are also described.
摘要翻译： 与其钠盐和溶剂化物一起描述基本上纯的形式的（S）-2-（二苯基乙酰基）-1,2,3,4-四氢-6-甲氧基-5-（苯基甲氧基）-3-异喹啉羧酸。 还描述了制备化合物，其钠盐及其溶剂合物的方法和包含它们的药物组合物。
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公开(公告)号：US20140142116A1
公开(公告)日：2014-05-22
申请号：US14016900
申请日：2013-09-03
发明人： Maree Therese Smith
IPC分类号： C07D471/04 , C07D409/06 , C07D217/26 , C07D241/04 , C07D401/06
CPC分类号： C07D471/04 , A61K31/00 , A61K31/395 , A61K38/07 , A61K38/08 , C07D217/16 , C07D217/26 , C07D241/04 , C07D401/06 , C07D409/06 , C07D409/14 , C12N15/1138 , C12N2310/11 , C12N2310/12 , C12N2310/14 , C12N2320/30 , C12Q2600/136 , G01N33/74 , G01N2333/726 , G01N2410/02 , G01N2500/04 , G01N2500/10 , G01N2800/7095
摘要： A method of treatment, reversal and/or symptomatic relief of inflammatory pain, including hyperalgesia, thermal or mechanical allodynia, in vertebrate animals, particularly in human subjects, comprising administering angiotensin II receptor 2 (AT2 receptor) antagonists is disclosed. The AT2 receptor antagonist may be provided alone or in combination with other compounds such as those that are useful in the control of inflammatory pain.
摘要翻译： 公开了在脊椎动物，特别是人类受试者中治疗，逆转和/或症状缓解炎性疼痛的方法，包括痛觉过敏，热或机械异常性疼痛，包括给予血管紧张素II受体2（AT2受体）拮抗剂。 AT2受体拮抗剂可以单独提供或与其它化合物组合提供，例如可用于控制炎性疼痛的化合物。
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公开(公告)号：US08722675B2
公开(公告)日：2014-05-13
申请号：US13923085
申请日：2013-06-20
IPC分类号： A61K31/50 , A61K31/495 , A61K31/44 , A61K31/47 , A61K31/41
CPC分类号： C07D471/04 , A61K31/517 , A61K38/08 , C07D239/90 , C07D401/06 , C07D403/10 , C07D403/14 , C07D409/06 , C07D409/14 , C07D413/12 , G01N33/74 , G01N2500/00
摘要： The present invention is directed to methods and agents that are useful in the prevention and amelioration of signs and symptoms associated with neuropathic conditions. More particularly, the present invention discloses the use of angiotensin II receptor 2 (AT2 receptor) antagonists for the treatment, prophylaxis, reversal and/or symptomatic relief of neuropathic pain, including mechanical hyperalgesia, thermal or mechanical allodynia, diabetic pain and entrapment pain, in vertebrate animals and particularly in human subjects. The AT2 receptor antagonists may be provided alone or in combination with other compounds such as those that are useful in the control of neuropathic conditions.
摘要翻译： 本发明涉及可用于预防和改善与神经病变相关的体征和症状的方法和试剂。 更具体地，本发明公开了血管紧张素II受体2（AT2受体）拮抗剂用于治疗，预防，逆转和/或症状缓解神经性疼痛，包括机械性痛觉过敏，热或机械异常性疼痛，糖尿病性疼痛和包埋性疼痛， 在脊椎动物，特别是在人类受试者。 AT2受体拮抗剂可以单独提供或与其它化合物组合提供，例如可用于控制神经病症的化合物。
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公开(公告)号：US20150218180A1
公开(公告)日：2015-08-06
申请号：US14373357
申请日：2013-01-25
发明人： Thomas David McCarthy , Alan Naylor
IPC分类号： C07D491/056 , C07D211/60 , C07D401/04 , C07D471/04
CPC分类号： C07D491/056 , C07D211/60 , C07D401/04 , C07D471/04 , C07D491/048 , C07D495/04
摘要： The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT2) receptor. More particularly the invention relates to piperidine compounds, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with AT2 receptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.
摘要翻译： 本发明涉及可用于拮抗血管紧张素II型2型（AT2）受体的杂环化合物。 更具体地，本发明涉及哌啶化合物，含有它们的组合物及其在治疗或预防与AT2受体功能相关的病症或疾病的方法中的用途，包括神经性疼痛，炎性疼痛，与神经元超敏反应相关的病症，神经传导速度受损，细胞增殖紊乱 ，与骨吸收和骨形成之间的不平衡相关的疾病以及与异常神经再生相关的疾病。
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公开(公告)号：US20140378430A1
公开(公告)日：2014-12-25
申请号：US14370737
申请日：2013-01-04
发明人： Thomas David McCarthy , Alan Naylor
IPC分类号： C07D498/10 , C07D209/42 , C07D413/04 , C07D401/04 , C07D403/04 , C07D401/12 , C07D409/04 , C07D205/04 , C07D207/14 , C07D207/16 , C07D471/10
CPC分类号： C07D498/10 , C07D205/04 , C07D207/14 , C07D207/16 , C07D207/22 , C07D209/18 , C07D209/42 , C07D209/94 , C07D401/04 , C07D401/12 , C07D403/04 , C07D409/04 , C07D413/04 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10 , C07D498/04
摘要： The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT2) receptor. More particularly the invention relates to pyrrolidine and azetidine compounds, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with AT2 receptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.
摘要翻译： 本发明涉及可用于拮抗血管紧张素II型2型（AT2）受体的杂环化合物。 更具体地说，本发明涉及吡咯烷和氮杂环丁烷化合物，含有它们的组合物及其在治疗或预防与AT2受体功能相关的病症或疾病的方法中的用途，包括神经性疼痛，炎性疼痛，与神经元超敏反应相关的病症，神经传导速度受损，细胞 增生障碍，与骨吸收和骨形成之间的不平衡相关的疾病以及与异常神经再生有关的疾病。
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公开(公告)号：US20140228362A1
公开(公告)日：2014-08-14
申请号：US14229746
申请日：2014-03-28
IPC分类号： C07D471/04 , C07D409/06 , C07D403/14 , C07D239/90 , C07D413/12 , C07D403/10 , C07D401/06
CPC分类号： C07D471/04 , A61K31/517 , A61K38/08 , C07D239/90 , C07D401/06 , C07D403/10 , C07D403/14 , C07D409/06 , C07D409/14 , C07D413/12 , G01N33/74 , G01N2500/00
摘要： The present invention is directed to methods and agents that are useful in the prevention and amelioration of signs and symptoms associated with neuropathic conditions. More particularly, the present invention discloses the use of angiotensin II receptor 2 (AT2 receptor) antagonists for the treatment, prophylaxis, reversal and/or symptomatic relief of neuropathic pain, including mechanical hyperalgesia, thermal or mechanical allodynia, diabetic pain and entrapment pain, in vertebrate animals and particularly in human subjects. The AT2 receptor antagonists may be provided alone or in combination with other compounds such as those that are useful in the control of neuropathic conditions.
摘要翻译： 本发明涉及可用于预防和改善与神经病变相关的体征和症状的方法和试剂。 更具体地，本发明公开了血管紧张素II受体2（AT2受体）拮抗剂用于治疗，预防，逆转和/或症状缓解神经性疼痛，包括机械性痛觉过敏，热或机械异常性疼痛，糖尿病性疼痛和包埋性疼痛， 在脊椎动物，特别是在人类受试者。 AT2受体拮抗剂可以单独提供或与其它化合物组合提供，例如可用于控制神经病症的化合物。
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