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21. 发明申请

WO2002096885A1 PYRIMIDINE DERIVATIVES USEFUL AS SELECTIVE COX-2 INHIBITORS 审中-公开
标题翻译：有用的选择性COX-2抑制剂的吡嗪衍生物
公开(公告)号：WO2002096885A1
公开(公告)日：2002-12-05
申请号：PCT/GB2002/002415
申请日：2002-05-23
申请人： GLAXO GROUP LIMITED , NAYLOR, Alan , PAYNE, Jeremy, John , PEGG, Neil, Anthony
发明人： NAYLOR, Alan , PAYNE, Jeremy, John , PEGG, Neil, Anthony
IPC分类号： C07D239/34
CPC分类号： C07D239/34 , A61K31/505 , C07D401/12
摘要： The invention provides the compounds of formula (I) in which: R 1 is selected from the group consisting of H, C 1-6 alkyl, C 1-2 alkyl substituted by one to five fluorine atoms, C 3-6 alkenyl, C 3-10 cycloalkylC 0-6 alkyl, C 4-12 bridged cycloalkyl, A(CR 4 R 5 ) n and b(CR 4 R 5 ) n ; R 2 is C 1-2 alkyl substituted by one to five fluorine atoms; R 3 is selected from the group consisting of C 1-6 alkyl, NH 2 and R 7 CONH; R 4 and R 5 are independently selected from H or C 1-6 alkyl; A is an unsubstituted 5- or 6-membered heteroaryl or an unsubstituted 6-membered aryl, or a 5- or 6-membered heteroaryl or a 6-membered aryl substituted by one or more R 6 ; R 6 is selected from the group consisting of halogen, C 1-6 alkyl, C 1-6 alkyl substituted by one or more fluorine atoms, C 1-6 alkoxy, C 1-6 alkoxy substituted by one or more F, NH 2 SO 2 and C 1-6 alkylSO 2 ; B is selected from the group consisting of Formula (i) and (ii) and where (iv) defines the point of attachment of the ring; R 7 is selected from the group consisting of H, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkylOC 1-6 alkyl, phenyl, HO 2 CC 1-6 alkyl, C 1-6 alkylOCOC 1-6 alkyl, C 1-6 alkylOCO, H 2 NC 1-6 alkyl, C 1-6 alkylOCONHC 1-6 alkyl and C 1-6 alkylCONHC 1-6 alkyl; and n is 0 to 4. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in treatment of the pain, fever and inflammation of variety of conditions and diseases.
摘要翻译：本发明提供式（I）化合物，其中：R 1选自H，C 1-6烷基，被1至5个氟原子取代的C 1-2烷基，C 3-6烯基，C 3-10环烷基C 1-6烷基，C 4-12桥环烷基，A（CR 4 R 5）n和b（CR 4 R 5）n; R 2是被1至5个氟原子取代的C 1-2烷基; R 3选自C 1-6烷基，NH 2和R 7 CONH; R 4和R 5独立地选自H或C 1-6烷基; A是未取代的5-或6-元杂芳基或未取代的6-元芳基，或被一个或多个R 6取代的5-或6-元杂芳基或6-元芳基; R 6选自卤素，C 1-6烷基，被一个或多个氟原子取代的C 1-6烷基，C 1-6烷氧基，被一个或多个F，NH 2 SO 2和C 1-6烷基SO 2取代的C 1-6烷氧基; B选自式（i）和（ii），其中（iv）定义环的连接点; R 7选自H，C 1-6烷基，C 1-6烷氧基，C 1-6烷基C 1-6烷基，苯基，HO 2 CCl 1-6烷基，C 1-6烷基COC 1-6烷基，C 1-6烷基COO，H 2 NC 1-6烷基，C 1-6烷基OCONHC 1 -6-烷基和C 1-6烷基CONHC 1-6烷基; 并且n为0至4.式（I）化合物是COX-2的有效和选择性抑制剂，并且可用于治疗各种病症和疾病的疼痛，发热和炎症。

22. 发明申请

WO2002096427A1 PYRIMIDINE DERIVATIVES AS SELECTIVE INHIBITORS OF COX-2 审中-公开
标题翻译：作为COX-2的选择性抑制剂的吡嗪衍生物
公开(公告)号：WO2002096427A1
公开(公告)日：2002-12-05
申请号：PCT/GB2002/002414
申请日：2002-05-23
申请人： GLAXO GROUP LIMITED , HARTLEY, Charles, David , NAYLOR, Alan , PAYNE, Jeremy, John , PEGG, Neil, Anthony
发明人： HARTLEY, Charles, David , NAYLOR, Alan , PAYNE, Jeremy, John , PEGG, Neil, Anthony
IPC分类号： A61K31/505
CPC分类号： C07D239/42
摘要： The invention thus provides the compounds of formula (I) and pharmaceutically acceptable salts thereof, in which: R 1 and R 2 are independently selected from the group consisting of H, C 1-6 alkyl, C 2-6 alkenyl, C 3-6 alkynyl, C 3-10 cycloalkylC 0-6 alkyl and C 4-12 bridged cycloalkyl; R 3 is selected from the group consisting of C 1-6 alkyl, NH 2 and R 5 CONH; R 4 is selected from the group consisting of CH 2 F, CHF 2 , CF 3 CH 2 , CF 3 CHF and CF 3 CF 2 ; and R 5 is selected from the group consisting of H, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkylOC 1-6 alkyl, phenyl, HO¿ 2 CC 1-6?alkyl, C 1-6 alkylOCOC 1-6 alkyl, C 1-6 alkylOCO, H 2 NC 1-6 alkyl, C 1-6 alkylOCONHC 1-6 alkyl and C 1-6 alkylCONHC 1-6 alkyl. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever, inflammation of a variety of conditions and diseases.
摘要翻译：因此，本发明提供式（I）化合物及其药学上可接受的盐，其中：R 1和R 2独立地选自H，C 1-6烷基，C 2-6烯基，C 3-6炔基，C 3-10环烷基C 1-6烷基和C 4-12桥环烷基; R 3选自C 1-6烷基，NH 2和R 5 CONH; R 4选自CH 2 F，CHF 2，CF 3 CH 2，CF 3 CHF和CF 3 CF 2; 和R 5选自H，C 1-6烷基，C 1-6烷氧基，C 1-6烷基C 1-6烷基，苯基，HO 2 CCl 1-6烷基，C 1-6烷基COOC 1-6烷基，C 1-6烷基COO，H 2 NC 1-6烷基，C 1 1-6烷基OCONHC 1-6烷基和C 1-6烷基CONHC 1-6烷基。式（I）化合物是COX-2的有效和选择性抑制剂，可用于治疗疼痛，发热，各种病症和疾病的炎症。

23. 发明申请

WO2013110135A1 HETEROCYCLIC COMPOUNDS AND METHODS FOR THEIR USE 审中-公开
标题翻译：杂环化合物及其使用方法
公开(公告)号：WO2013110135A1
公开(公告)日：2013-08-01
申请号：PCT/AU2013/000062
申请日：2013-01-25
申请人： SPINIFEX PHARMACEUTICALS PTY LTD , MCCARTHY, Thomas David , NAYLOR, Alan
发明人： MCCARTHY, Thomas David , NAYLOR, Alan
IPC分类号： C07D495/04 , C07D211/60 , C07D211/66 , C07D471/04 , C07D491/048 , C07D491/056 , A61K31/4355 , A61K31/436 , A61K31/4365 , A61K31/437 , A61K31/4375 , A61K31/519 , A61P25/02 , A61P25/04 , A61P35/00
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 (AT 2 ) 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 AT 2 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。

24. 发明申请

WO2013110134A1 HETEROCYCLIC COMPOUNDS AND METHODS FOR THEIR USE 审中-公开
标题翻译：杂环化合物及其使用方法
公开(公告)号：WO2013110134A1
公开(公告)日：2013-08-01
申请号：PCT/AU2013/000061
申请日：2013-01-25
申请人： SPINIFEX PHARMACEUTICALS PTY LTD , MCCARTHY, Thomas David , NAYLOR, Alan
发明人： MCCARTHY, Thomas David , NAYLOR, Alan
IPC分类号： C07D241/04 , C07D403/04 , C07D487/04 , C07D413/04 , C07D413/06 , C07D243/08 , A61P25/02 , A61P25/04 , A61P35/00 , A61K31/551 , A61K31/4985 , A61K31/496
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 antagonising angiotensin II Type 2 (AT 2 ) 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 AT 2 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受体功能相关的疾病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。

25. 发明申请

WO2016113668A1 PYRROLIDINE DERIVATIVES AS ANGIOTENSIN II TYPE 2 ANTAGONISTS 审中-公开
标题翻译：吡咯啉衍生物作为ANGIOTENSIN II型2型拮抗剂
公开(公告)号：WO2016113668A1
公开(公告)日：2016-07-21
申请号：PCT/IB2016/050122
申请日：2016-01-12
申请人： NOVARTIS AG , BROWN, Jane , MCCARTHY, Thomas David , NAYLOR, Alan , WATTS, John Paul
发明人： BROWN, Jane , MCCARTHY, Thomas David , NAYLOR, Alan , WATTS, John Paul
IPC分类号： C07D403/04 , C07D413/04 , C07D417/04 , C07D471/04 , C07D495/04 , A61K31/40 , A61P25/00 , A61P29/00 , A61P35/00
CPC分类号： C07D403/04 , C07D401/04 , C07D413/04 , C07D417/04 , C07D471/04 , C07D495/04
摘要： The invention relates to heterocyclic angiotensin II type 2 (AT 2 ) receptor antagonists of formula (I), and pharmaceutically acceptable salts thereof, ((I) in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of neuropathic or inflammatory pain.
摘要翻译：本发明涉及式（I）的杂环血管紧张素II 2型（AT2）受体拮抗剂及其药学上可接受的盐，（（I）其中所有变量如说明书中所定义，其药物组合物，其组合，并将其用作药物，特别是用于治疗神经性或炎性疼痛。

26. 发明申请

WO2013102242A1 HETEROCYCLIC COMPOUNDS AND METHODS FOR THEIR USE 审中-公开
标题翻译：杂环化合物及其使用方法
公开(公告)号：WO2013102242A1
公开(公告)日：2013-07-11
申请号：PCT/AU2013/000003
申请日：2013-01-04
申请人： SPINIFEX PHARMACEUTICALS PTY LTD , MCCARTHY, Thomas David , NAYLOR, Alan
发明人： MCCARTHY, Thomas David , NAYLOR, Alan
IPC分类号： C07D207/16 , C07D205/04 , C07D207/22 , C07D209/18 , C07D209/42 , C07D209/94 , C07D403/04 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10 , C07D498/10 , A61K31/40 , A61K31/397 , A61K31/4025 , A61K31/404 , A61P25/00 , A61P29/00 , A61P35/00
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 (AT 2 ) 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 AT 2 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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