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1. 发明申请

WO2007063418A2 SUBSTITUTED INDOLE COMPOUNDS HAVING NOS INHIBITORY ACTIVITY 审中-公开
标题翻译：具有NOS抑制活性的取代吲哚化合物
公开(公告)号：WO2007063418A2
公开(公告)日：2007-06-07
申请号：PCT/IB2006/003873
申请日：2006-04-13
申请人： NEURAXON, INC. , MADDAFORD, Shawn , RAMNAUTH, Jailall , RAKHIT, Suman , PATMAN, Joanne , RENTON, Paul , ANNEDI, Subhash, C.
发明人： MADDAFORD, Shawn , RAMNAUTH, Jailall , RAKHIT, Suman , PATMAN, Joanne , RENTON, Paul , ANNEDI, Subhash, C.
IPC分类号： A61P25/28 , A61K31/00 , C07D401/04 , C07D405/12
CPC分类号： C07D453/02 , C07D209/08 , C07D401/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D451/02 , C07D471/04 , C07D471/08
摘要： The present invention features inhibitors of nitric oxide synthase (NOS)5 particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.
摘要翻译：本发明表征了一氧化氮合酶（NOS）5的抑制剂，特别是优先于其他NOS同种型选择性抑制神经元一氧化氮合酶（nNOS）的那些抑制剂。本发明的NOS抑制剂单独或与其它药物活性剂组合可以用于治疗或预防诸如例如中风，再灌注损伤，神经变性，头部创伤，CABG，具有和不具有先兆的偏头痛头痛，具有异常性疼痛的偏头痛，中枢性中风后疼痛（CPSP），神经性疼痛，吗啡/阿片样物质诱导的耐受性和痛觉过敏。

2. 发明申请

WO2007118314A1 1,5 AND 3,6- SUBSTITUTED INDOLE COMPOUNDS HAVING NOS INHIBITORY ACTIVITY 审中-公开
标题翻译：具有NOS抑制活性的1,5和3,6-取代的吲哚化合物
公开(公告)号：WO2007118314A1
公开(公告)日：2007-10-25
申请号：PCT/CA2007/000617
申请日：2007-04-13
申请人： NEURAXON, INC. , MADDAFORD, Shawn , RAMNAUTH, Jailall , RAKHIT, Suman , PATMAN, Joanne , RENTON, Paul , ANNEDI, Subhash, C.
发明人： MADDAFORD, Shawn , RAMNAUTH, Jailall , RAKHIT, Suman , PATMAN, Joanne , RENTON, Paul , ANNEDI, Subhash, C.
IPC分类号： C07D409/14 , A61K31/4025 , A61K31/439 , A61K31/4436 , A61K31/454 , A61K31/5377 , A61K31/55 , C07D405/14 , C07D409/12 , C07D413/14 , C07D471/08
CPC分类号： C07D409/14 , C07D403/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D471/08
摘要： The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, or chronic pain.
摘要翻译：本发明特征在于一氧化氮合酶（NOS）的抑制剂，特别是那些优先选择性抑制神经元一氧化氮合酶（nNOS）的那些，优于其它NOS同种型。本发明的NOS抑制剂单独或与其它药物活性剂组合可用于治疗或预防诸如卒中，再灌注损伤，神经变性，头部创伤，CABG，伴有和不伴有光环的偏头痛头痛等病症，偏头痛与异常性疼痛，中风后疼痛（CPSP），神经性疼痛或慢性疼痛。

3. 发明申请

WO2007017764A2 SUBSTITUTED BENZIMIDAZOLE COMPOUNDS WITH DUAL NOS INHIBITORY ACTIVITY AND MUOPIOID AGONIST ACTIVITY 审中-公开
标题翻译：具有双NOS抑制活性和多种激动剂活性的替代苯扎咪唑化合物
公开(公告)号：WO2007017764A2
公开(公告)日：2007-02-15
申请号：PCT/IB2006/003075
申请日：2006-05-18
申请人： NEURAXON, INC. , RENTON, Paul , MADDAFORD, Shawn , RAKHIT, Suman , ANDREWS, John
发明人： RENTON, Paul , MADDAFORD, Shawn , RAKHIT, Suman , ANDREWS, John
CPC分类号： C07D409/12 , C07D235/12 , C07D405/12
摘要： The present invention relates to benzimidazole compounds having dual nitric oxide synthase (NOS) inhibitory activity and agonist activity at the mu- opioid receptor, to pharmaceutical and diagnostic compositions containing them, and to their medical use, particularly as compounds for the treatment or prevention of chronic pain, acute pain, migraine, and neuropathic pain.
摘要翻译：本发明涉及具有双重一氧化氮合酶（NOS）抑制活性和在阿片受体受体的激动剂活性的苯并咪唑化合物，含有它们的药物和诊断组合物及其医疗用途，特别是作为治疗或预防慢性疼痛，急性疼痛，偏头痛和神经性疼痛。

4. 发明申请

WO2009062318A1 3,5-SUBSTITUTED INDOLE COMPOUNDS HAVING NOS AND NOREPINEPHRINE REUPTAKE INHIBITORY ACTIVITY 审中-公开
标题翻译：具有NOS和NOREPINEPHRINE REUPTAKE抑制活性的3,5取代的吲哚化合物
公开(公告)号：WO2009062318A1
公开(公告)日：2009-05-22
申请号：PCT/CA2008/002033
申请日：2008-11-17
申请人： NEURAXON, INC. , ANNEDI, Subhash, C. , MADDAFORD, Shawn , RAMNAUTH, Jailall , RENTON, Paul , RAKHIT, Suman , ANDREWS, John, S , MLADENOVA, Gabriela
发明人： ANNEDI, Subhash, C. , MADDAFORD, Shawn , RAMNAUTH, Jailall , RENTON, Paul , RAKHIT, Suman , ANDREWS, John, S , MLADENOVA, Gabriela
IPC分类号： C07D409/12 , A61K31/4045 , A61P25/04 , A61P25/18
CPC分类号： C07D409/12
摘要： The present invention relates to novel 3,5-substituted indole compounds of Formula (I) having nitric oxide synthase (NOS) inhibitory activity, particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other eNOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing condition such as chronic pain and psychiatric disorders.
摘要翻译：本发明涉及具有一氧化氮合酶（NOS）抑制活性的新颖的式（I）的3,5-取代吲哚化合物，特别是选择性地抑制神经元一氧化氮合酶（nNOS）优先于其它eNOS同种型的那些。本发明的NOS抑制剂单独或与其它药物活性剂组合可用于治疗或预防诸如慢性疼痛和精神障碍的病症。

5. 发明申请

WO2007017764A3 SUBSTITUTED BENZIMIDAZOLE COMPOUNDS WITH DUAL NOS INHIBITORY ACTIVITY AND MUOPIOID AGONIST ACTIVITY 审中-公开
标题翻译：具有双重NOS抑制活性和多功能激动剂活性的取代苯并咪唑化合物
公开(公告)号：WO2007017764A3
公开(公告)日：2007-07-05
申请号：PCT/IB2006003075
申请日：2006-05-18
申请人： NEURAXON INC , RENTON PAUL , MADDAFORD SHAWN , RAKHIT SUMAN , ANDREWS JOHN
发明人： RENTON PAUL , MADDAFORD SHAWN , RAKHIT SUMAN , ANDREWS JOHN
IPC分类号： C07D409/12 , A61K31/4184 , A61K31/454 , A61K31/5377 , A61K45/06 , C07D235/12
CPC分类号： C07D409/12 , C07D235/12 , C07D405/12
摘要： The present invention relates to benzimidazole compounds having dual nitric oxide synthase (NOS) inhibitory activity and agonist activity at the mu- opioid receptor, to pharmaceutical and diagnostic compositions containing them, and to their medical use, particularly as compounds for the treatment or prevention of chronic pain, acute pain, migraine, and neuropathic pain.
摘要翻译：本发明涉及对μ阿片受体具有双重一氧化氮合酶（NOS）抑制活性和激动剂活性的苯并咪唑化合物，含有它们的药物和诊断组合物，及其医学用途，特别是作为用于治疗或预防慢性疼痛，急性疼痛，偏头痛和神经性疼痛。

6. 发明申请

WO2004014885B1 AMINO BENZOTHIAZOLE COMPOUNDS WITH NOS INHIBITORY ACTIVITY 审中-公开
标题翻译：具有NOS抑制活性的氨基苯并噻唑化合物
公开(公告)号：WO2004014885B1
公开(公告)日：2004-05-13
申请号：PCT/CA0301185
申请日：2003-08-07
申请人： MCR RES INC , RAMNAUTH JAILALL , BHARDWAJ NAMRTA , RAKHIT SUMAN , MADDAFORD SHAWN
发明人： RAMNAUTH JAILALL , BHARDWAJ NAMRTA , RAKHIT SUMAN , MADDAFORD SHAWN
IPC分类号： C07D277/82 , C07D417/12 , C07D417/14 , C07D521/00 , A61K31/428
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D277/82 , C07D417/12 , C07D417/14
摘要： The present invention provides novel amino benzothiazole compounds, compositions comprising these compounds and methods of using these compounds as neuroprotectants. In particular, the compounds described in the present invention are useful for treating stroke.
摘要翻译：本发明提供新的氨基苯并噻唑化合物，包含这些化合物的组合物和使用这些化合物作为神经保护剂的方法。特别地，本发明中描述的化合物可用于治疗中风。

7. 发明申请

WO2010000073A1 BENZOXAZINES, BENZOTHIAZINES, AND RELATED COMPOUNDS HAVING NOS INHIBITORY ACTIVITY 审中-公开
标题翻译：苯并噻嗪类，苯并嗪类，以及具有NOS抑制活性的相关化合物
公开(公告)号：WO2010000073A1
公开(公告)日：2010-01-07
申请号：PCT/CA2009/000923
申请日：2009-07-03
申请人： NEURAXON, INC. , RAMNAUTH, Jailall , ANNEDI, Subhash, C. , SILVERMAN, Sarah , DOVE, Peter , MADDAFORD, Shawn , RAKHIT, Suman
发明人： RAMNAUTH, Jailall , ANNEDI, Subhash, C. , SILVERMAN, Sarah , DOVE, Peter , MADDAFORD, Shawn , RAKHIT, Suman
IPC分类号： C07D417/12 , A61K31/538 , A61K31/5415 , A61P25/00 , A61P25/02 , C07D413/12 , C07D413/14 , C07D417/14
CPC分类号： C07D417/14 , A61K31/538 , A61K31/5415 , C07D413/12 , C07D413/14 , C07D417/12 , Y02A50/475
摘要： Disclosed are benzoxazines and benzothiazines of formula (I) wherein Q is O-(CHR 6 ) 1-3 or S-(CHR 6 ) 1-3 ; R 1 and each R 6 is H, optionally substituted [C 1-6 alkyl, C 1-4 alkaryl, C 1-4 alkheterocyclyl, C 2-9 heterocyclyl, C 3-8 cycloalkyl, C 1-4 alkcycloalkyl] or - (CR 1A R 1B )nNR 1c R 1D wherein R 1A , R 1B , R 1C , R 1D are independently hydrogen, optionally substituted [C 1-6 alkyl, C 1-4 alkaryl, C 1-4 alkheterocyclyl, C 2-9 heterocyclyl, C 3-8 cycloalkyl, etc.] or wherein R 1A and R 1B combine to form =O, or wherein R 1C and R 1D combine to form an optionally substituted C 2-9 heterocyclyl, and n is an integer between 1-6; each of R 2 and R 3 is H, hal, optionally substituted [C 1-6 alkyl, C 6-10 aryl, C 1-6 alkaiyl, C 2-9 heterocyclyl, C 1-6 alkoxy, C 1-6 thioalkoxy, (CH 2 ) r2 NHC(NH)R 2A , CH 2 ) r2 NHC(S)NHR 2A , C 1-4 alkheterocyclyl] or hydroxy, wherein r2 is an integer from 0 to 2, R 2A is optionally substituted [C 1-6 alkyl, C 6-10 aryl, C^alkaryl, C 2-9 heterocyclyl, C 1-4 alkheterocyclyl,C 1-6 thioalkoxy, C 1-4 thioalkaryl, aryloyl, C 1- 4 thioalkheterocylyl, or amino]; each R 4 and R 5 is H, hal, (CH 2 ) r2 NHC(NH)R 2A or CH 2 ) r2 NHC(S)NH R 2A ; Y 1 and Y 2 are together =O or Y 1 and Y 2 are independently H, optionally substituted [C 1-6 alkyl, C 6-10 aryl, C 1-6 alkaryl, C 2-9 heterocyclyl, C 1-6 alkoxy, C 1-6 thioalkoxy, C 1-4 alkheterocyclyl] or hydroxy; wherein only one of R 2 , R 3 , R 4 and R 5 is (CH 2 ) r2 NHC(NH)R 2A or CH 2 ) r2 NHC(S)NH R 2A ; or a pharmaceutically acceptable salt or prodrug thereof. Said benzoxazines and benzothiazines of formula (I) inhibit nitric oxide synthase (NOS), particularly selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of formula (I), alone or in combinatioon with other pharmaceutically active agents, can be used for treating or preventing various medical conditions.
摘要翻译：公开了式（I）的苯并恶嗪和苯并噻嗪，其中Q是O-（CHR 6）1-3或S-（CHR 6）1-3; R 1和R 6各自为H，任选取代的[C 1-6烷基，C 1-4烷芳基，C 1-4烷基杂环基，C 2-9杂环基，C 3-8环烷基，C 1-4烷环烷基]或 - （CR 1 AR 1 B）n N R c R D，其中R 1A， R1C，R1D独立地为氢，任选取代的[C 1-6烷基，C 1-4烷芳基，C 1-4烷基杂环基，C 2-9杂环基，C 3-8环烷基等]或其中R 1A和R 1B结合形成= O，或其中 R1C和R1D结合形成任选取代的C2-9杂环基，n为1-6之间的整数; R2和R3各自为H，Hal，任选取代的[C 1-6烷基，C 6-10芳基，C 1-6烷酰基，C 2-9杂环基，C 1-6烷氧基，C 1-6硫烷氧基，（CH 2）r R 2 NHC（NH） CH2）r2NHC（S）NHR2A，C1-4烷基杂环基]或羟基，其中R2是0-2的整数，R2A是任选取代的[C 1-6烷基，C 6-10芳基，C 1-4烷芳基，C 2-9杂环基，C 1 -4烷基杂环基，C1-6硫代烷氧基，C1-4硫代烷基芳基，芳基，C1-4硫代炔基或氨基]。每个R 4和R 5是H，Hal，（CH 2）r R 2 NHC（NH）R 2 A或CH 2）r R 2 NHC（S）NHR 2 A; Y1和Y2一起= O或Y1，Y2独立地为H，任选取代的[C 1-6烷基，C 6-10芳基，C 1-6烷芳基，C 2-9杂环基，C 1-6烷氧基，C 1-6硫烷氧基，C 1-4杂环基] 或羟基; 其中R2，R3，R4和R5中只有一个是（CH2）r2NHC（NH）R2A或CH2）r2NHC（S）NHR2A; 或其药学上可接受的盐或前药。式（I）的所述苯并恶嗪和苯并噻嗪抑制一氧化氮合酶（NOS），特别是选择性地抑制神经元一氧化氮合酶（nNOS）优于其它NOS同种型。式（I）的NOS抑制剂单独或与其它药物活性剂组合可用于治疗或预防各种医学病症。

8. 发明申请

WO2009062319A1 INDOLE COMPOUNDS AND METHODS FOR TREATING VISCERAL PAIN 审中-公开
标题翻译：吲哚化合物和治疗粘膜疼痛的方法
公开(公告)号：WO2009062319A1
公开(公告)日：2009-05-22
申请号：PCT/CA2008/002047
申请日：2008-11-17
申请人： NEURAXON, INC. , MADDAFORD, Shawn , RAMNAUTH, Jailall , RAKHIT, Suman , PATMAN, Joanne , RENTON, Paul , ANNEDI, Subhash, C. , ANDREWS, John, S. , MLADENOVA, Gabriela
发明人： MADDAFORD, Shawn , RAMNAUTH, Jailall , RAKHIT, Suman , PATMAN, Joanne , RENTON, Paul , ANNEDI, Subhash, C. , ANDREWS, John, S. , MLADENOVA, Gabriela
IPC分类号： C07D409/14 , A61K31/404 , A61K31/437 , A61K31/439 , A61K31/454 , A61K31/5377 , A61P25/04 , A61P29/00 , C07D403/04
CPC分类号： A61K31/404 , A61K31/437 , A61K31/439 , A61K31/454 , A61K31/5377 , C07D403/04 , C07D409/14
摘要： The invention features methods of treating visceral pain or a condition in a mammal caused by the action of nitric oxide synthase (NOS) or by the action of serotonin 5HT1D/1B receptors, by administering to a patient in need thereof a therapeutically effective amount of an indole compound of Formula (I), or a pharmaceutically acceptable salt or prodrug thereof. The methods of the invention may further comprise the administration of additional therapeutic agent. The invention also features new compounds of Formula (I), pharmaceutical compositions thereof, and methods of resolving enantiomeric mixtures.
摘要翻译：本发明的特征在于，通过向有需要的患者施用治疗有效量的治疗有效量的治疗由一氧化氮合酶（NOS）的作用或通过5-羟色胺5HT1D / 1B受体的作用而引起的哺乳动物的内脏疼痛或病症的方法式（I）的吲哚化合物或其药学上可接受的盐或前药。本发明的方法还可以包括施用另外的治疗剂。本发明还具有式（I）的新化合物，其药物组合物和拆分对映体混合物的方法。

9. 发明申请

WO2008116308A1 QUINOLONE AND TETRAHYDROQUINOLINE AND RELATED COMPOUNDS HAVING NOS INHIBITORY ACTIVITY 审中-公开
标题翻译：喹诺酮和四氢喹啉以及具有NOS抑制活性的相关化合物
公开(公告)号：WO2008116308A1
公开(公告)日：2008-10-02
申请号：PCT/CA2008/000569
申请日：2008-03-25
申请人： NEURAXON, INC. , MADDAFORD, Shawn , RAMNAUTH, Jailall , RAKHIT, Suman , PATMAN, Joanne , ANNEDI, Subhash, C. , ANDREWS, John , DOVE, Peter , SILVERMAN, Sarah , RENTON, Paul
发明人： MADDAFORD, Shawn , RAMNAUTH, Jailall , RAKHIT, Suman , PATMAN, Joanne , ANNEDI, Subhash, C. , ANDREWS, John , DOVE, Peter , SILVERMAN, Sarah , RENTON, Paul
IPC分类号： C07D409/14 , A61K31/4709 , A61K31/55 , C07D209/04 , C07D215/02 , C07D223/16 , C07D409/12 , C07D413/14
CPC分类号： C07D409/14 , C07D409/12 , C07D413/14
摘要： The present invention features quinolones, tetrahydroquinolines, and related compounds that inhibit nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions.
摘要翻译：本发明的特征在于抑制一氧化氮合酶（NOS）的喹诺酮类，四氢喹啉类和相关化合物，特别是选择性抑制神经元一氧化氮合成酶（nNOS）优先于其它NOS同种型的化合物。本发明的NOS抑制剂单独或与其它药物活性剂组合可用于治疗或预防各种医学病症。

10. 发明申请

WO2007063418A3 SUBSTITUTED INDOLE COMPOUNDS HAVING NOS INHIBITORY ACTIVITY 审中-公开
标题翻译：具有NOS抑制活性的取代的吲哚化合物
公开(公告)号：WO2007063418A3
公开(公告)日：2007-12-21
申请号：PCT/IB2006003873
申请日：2006-04-13
申请人： NEURAXON INC , MADDAFORD SHAWN , RAMNAUTH JAILALL , RAKHIT SUMAN , PATMAN JOANNE , RENTON PAUL , ANNEDI SUBHASH C
发明人： MADDAFORD SHAWN , RAMNAUTH JAILALL , RAKHIT SUMAN , PATMAN JOANNE , RENTON PAUL , ANNEDI SUBHASH C
IPC分类号： A61P25/28 , A61K31/404 , C07D401/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D453/02 , C07D471/04 , C07D471/08
CPC分类号： C07D453/02 , C07D209/08 , C07D401/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D451/02 , C07D471/04 , C07D471/08
摘要： The present invention features inhibitors of nitric oxide synthase (NOS)5 particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.
摘要翻译：本发明的特征在于一氧化氮合酶（NOS）5的抑制剂，特别是选择性抑制神经元一氧化氮合酶（nNOS）优先于其它NOS同种型的抑制剂。本发明的NOS抑制剂单独或与其它药物活性剂组合可用于治疗或预防诸如中风，再灌注损伤，神经变性，头部创伤，CABG，伴有和不伴有光环的偏头痛头痛等病症，偏头痛与异常性疼痛，中风后疼痛（CPSP），神经性疼痛，吗啡/阿片样物质诱导的耐受性和痛觉过敏。

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