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1. 发明申请

US20050119261A1 Biaryl substituted triazoles as sodium channnel blockers 有权
标题翻译：二芳基取代三唑作为钠通道阻断剂
公开(公告)号：US20050119261A1
公开(公告)日：2005-06-02
申请号：US10799230
申请日：2004-03-12
申请人： Prasun Chakravarty , Michael Fisher , Jeffrey Fisher , Brenda Palucki , Min Park , William Parsons , Bishan Zhou , James Carey , Douglas Frantz , Michael Kress , Damian Weaver
发明人： Prasun Chakravarty , Michael Fisher , Jeffrey Fisher , Brenda Palucki , Min Park , William Parsons , Bishan Zhou , James Carey , Douglas Frantz , Michael Kress , Damian Weaver
IPC分类号： A61K31/4196 , A61P25/00 , C07D249/08 , C07D249/10 , C07D413/02 , A61K31/496 , A61K31/506 , A61K31/5377 , C07D417/02 , C07D43/02
CPC分类号： C07D249/08 , C07D249/10
摘要： Biaryl substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof, and a process for making such compounds and salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier.
摘要翻译：由式I，II或III表示的二芳基取代的三唑化合物或其药学上可接受的盐，以及其制备方法。药物组合物包含单独的或与一种或多种其它治疗活性化合物组合的有效量的本发明化合物和药学上可接受的载体。治疗与钠通道活性相关或由其引起的疾病的方法，包括例如急性疼痛，慢性疼痛，内脏痛，炎性疼痛，神经性疼痛，癫痫，肠易激综合征，抑郁症，焦虑症，多发性硬化症和双相包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物组合施用。施用局部麻醉的方法包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物和药学上可接受的载体组合施用。

2. 发明申请

US20060183897A1 Biaryl substituted triazoles as sodium channel blockers 审中-公开
公开(公告)号：US20060183897A1
公开(公告)日：2006-08-17
申请号：US10549790
申请日：2004-03-12
申请人： Prasun Chakravarty , Michael Fisher , Brenda Palucki , Min Park , William Parsons , Bishan Zhou , James Carey , Douglas Frantz , Michael Kress , Damian Weaver
发明人： Prasun Chakravarty , Michael Fisher , Brenda Palucki , Min Park , William Parsons , Bishan Zhou , James Carey , Douglas Frantz , Michael Kress , Damian Weaver
IPC分类号： C07D417/02 , C07D403/02 , C07D413/02
CPC分类号： C07D249/08 , C07D249/10
摘要： Biaryl substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof, and a process for making such compounds and salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier.

3. 发明申请

US20060020006A1 Substituted triazoles as sodium channel blockers 有权
标题翻译：取代的三唑作为钠通道阻断剂
公开(公告)号：US20060020006A1
公开(公告)日：2006-01-26
申请号：US10985592
申请日：2004-11-10
申请人： Min Park , Prasun Chakravarty , Bishan Zhou , Edward Gonzalez , Hyun Ok , Brenda Palucki , William Parsons , Rosemary Sisco , Michael Fisher , Louis Zuegner
发明人： Min Park , Prasun Chakravarty , Bishan Zhou , Edward Gonzalez , Hyun Ok , Brenda Palucki , William Parsons , Rosemary Sisco , Michael Fisher , Louis Zuegner
IPC分类号： A61K31/4196 , C07D403/02
CPC分类号： C07D249/10 , C07D403/10
摘要： Substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, migraine, headache pain, migraine headache, epilepsy, irritable bowel syndrome, diabetic neuropathy, multiple sclerosis, manic depression and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier.
摘要翻译：由式I，II或III表示的取代的三唑化合物或其药学上可接受的盐。药物组合物包含单独的或与一种或多种其它治疗活性化合物组合的有效量的本发明化合物和药学上可接受的载体。治疗与钠通道活性相关或由其引起的疾病的方法，包括例如急性疼痛，慢性疼痛，内脏痛，炎性疼痛，神经性疼痛，偏头痛，头痛，偏头痛，癫痫，肠易激综合征，糖尿病神经病，多发性硬化症，躁狂抑郁症和双相性精神障碍，包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物组合施用。施用局部麻醉的方法包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物和药学上可接受的载体组合施用。

4. 发明申请

US20060183785A1 Biaryl substituted pyrazoles as sodium channel blockers 失效
公开(公告)号：US20060183785A1
公开(公告)日：2006-08-17
申请号：US10552024
申请日：2004-03-30
申请人： Prasun Chakravarty , Michael Fisher , William Parsons , Sriram Tyagarajan , Bishan Zhou , Jeffrey Fisher
发明人： Prasun Chakravarty , Michael Fisher , William Parsons , Sriram Tyagarajan , Bishan Zhou , Jeffrey Fisher
IPC分类号： A61K31/416 , C07D231/02 , C07D231/12 , C07D403/04
CPC分类号： C07D401/04 , C07D231/14 , C07D401/10 , C07D403/04 , C07D403/10 , C07D403/12 , C07D409/10 , C07D409/14 , C07D413/12 , C07D417/12
摘要： Biaryl substituted pyrazole compounds are sodium channel blockers useful for the treatment of pain and other conditions. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treatment of conditions, including acute pain, chronic pain, visceral pain, inflammatory pain, and neuropathic pain, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more therapeutically active compounds.

5. 发明申请

US20070060584A1 Biaryl substituted thiazoles, oxazoles and imidazoles as sodium channel blockers 审中-公开
标题翻译：二芳基取代的噻唑，恶唑和咪唑作为钠通道阻断剂
公开(公告)号：US20070060584A1
公开(公告)日：2007-03-15
申请号：US10553554
申请日：2004-04-14
申请人： Prasun Chakravarty , Michael Fisher , William Parsons , Sriram Tyagarajan , Bishan Zhou , Jeffrey Fisher
发明人： Prasun Chakravarty , Michael Fisher , William Parsons , Sriram Tyagarajan , Bishan Zhou , Jeffrey Fisher
IPC分类号： A61K31/5377 , A61K31/497 , A61K31/496 , A61K31/454 , A61K31/427 , A61K31/422 , A61K31/4178 , C07D413/02 , C07D417/02 , C07D403/02
CPC分类号： C07D233/64 , C07D233/68 , C07D233/90 , C07D233/96 , C07D263/32 , C07D263/34 , C07D263/48 , C07D277/22 , C07D277/24 , C07D277/30 , C07D277/40 , C07D277/46 , C07D277/48 , C07D277/52 , C07D277/56 , C07D403/04 , C07D417/04 , C07D417/12 , C07D417/14
摘要： Biaryl substituted thiazole, oxazole and imidazole compounds are sodium channel blockers useful for the treatment of pain. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treatment or prevention of conditions, including acute pain, chronic pain, visceral pain, inflammatory pain, and neuropathic pain comprise administering an effective amount of the present compounds, either alone, or in combination with one or more therapeutically active compounds.
摘要翻译：双芳基取代的噻唑，恶唑和咪唑化合物是可用于治疗疼痛的钠通道阻滞剂。药物组合物包含单独的或与一种或多种治疗活性化合物组合的有效量的本发明化合物和药学上可接受的载体。治疗或预防包括急性疼痛，慢性疼痛，内脏痛，炎性疼痛和神经性疼痛的病症的方法包括单独施用有效量的本发明化合物或与一种或多种治疗活性化合物组合施用。

6. 发明申请

US20060293339A1 Biaryl substituted 6-membered heterocycles as sodium channel blockers 审中-公开
标题翻译：二芳基取代的6元杂环作为钠通道阻断剂
公开(公告)号：US20060293339A1
公开(公告)日：2006-12-28
申请号：US10550641
申请日：2004-03-19
申请人： Prasun Chakravarty , Michael Fisher , William Parsons , Jun Liang , Bishan Zhou
发明人： Prasun Chakravarty , Michael Fisher , William Parsons , Jun Liang , Bishan Zhou
IPC分类号： A61K31/506 , A61K31/4965 , A61K31/497 , A61K31/455 , A61K31/4439 , C07D403/02 , A61K31/5377 , C07D413/02
CPC分类号： C07D213/26 , C07D213/55 , C07D213/56 , C07D239/26 , C07D401/04 , C07D403/04
摘要： Biaryl substituted pyridine, pyrimidine and pyrazine compounds are sodium channel blockers useful for the treatment of pain. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
摘要翻译：双芳基取代的吡啶，嘧啶和吡嗪化合物是可用于治疗疼痛的钠通道阻滞剂。药物组合物包含单独的或与一种或多种治疗活性化合物组合的有效量的本发明化合物和药学上可接受的载体。治疗与钠通道活性相关或由其引起的疾病的方法，包括例如急性疼痛，慢性疼痛，内脏痛，炎性疼痛，神经性疼痛，癫痫，肠易激综合征，抑郁症，焦虑症，多发性硬化症和双相包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物组合施用。

7. 发明申请

US20090074890A1 Substituted Triazoles as Sodium Channel Blockers 审中-公开
标题翻译：取代三唑作为钠通道阻断剂
公开(公告)号：US20090074890A1
公开(公告)日：2009-03-19
申请号：US10578950
申请日：2004-11-05
申请人： Min K. Park , Prasun K. Chakravarty , Bishan Zhou , Edward Gonzalez , Hyun Ok , Brenda Palucki , William H. Parsons , Rosemary Sisco , Michael H. Fisher , Louis L. Zuegner, III
发明人： Min K. Park , Prasun K. Chakravarty , Bishan Zhou , Edward Gonzalez , Hyun Ok , Brenda Palucki , William H. Parsons , Rosemary Sisco , Michael H. Fisher , Louis L. Zuegner, III
IPC分类号： C07D249/08 , A61P29/00 , A61P9/00 , A61P25/00 , A61K33/00 , A61K31/4196 , A61P1/00 , A61P31/12 , A61P37/00
CPC分类号： C07D249/10 , C07D403/10
摘要： Substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, migraine, headache pain, migraine headache, epilepsy, irritable bowel syndrome, diabetic neuropathy, multiple sclerosis, manic depression and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier (I), (II), (III).
摘要翻译：由式I，II或III表示的取代的三唑化合物或其药学上可接受的盐。药物组合物包含单独的或与一种或多种其它治疗活性化合物组合的有效量的本发明化合物和药学上可接受的载体。治疗与钠通道活性相关或由其引起的疾病的方法，包括例如急性疼痛，慢性疼痛，内脏痛，炎性疼痛，神经性疼痛，偏头痛，头痛，偏头痛，癫痫，肠易激综合征，糖尿病神经病，多发性硬化症，躁狂抑郁症和双相性精神障碍，包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物组合施用。施用局部麻醉的方法包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物和药学上可接受的载体（I），（II），（III）。

8. 发明申请

US20080171777A1 Biaryl substituted triazoles as sodium channel blockers 有权
公开(公告)号：US20080171777A1
公开(公告)日：2008-07-17
申请号：US12011967
申请日：2008-01-30
申请人： Prasun K. Chakravarty , Michael H. Fisher , Louis L. Zuegner , William H. Parsons , Brenda Palucki , Bishan Zhou , Min K. Park
发明人： Prasun K. Chakravarty , Michael H. Fisher , Louis L. Zuegner , William H. Parsons , Brenda Palucki , Bishan Zhou , Min K. Park
IPC分类号： A61K31/4196 , C07D249/08 , A61P23/02 , A61P25/04
CPC分类号： C07D249/08 , C07D249/10
摘要： Biaryl substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof, and a process for making such compounds and salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier.

9. 发明授权

US06936714B2 Compounds of the saframycin-ecteinascidin series, uses, and synthesis thereof 失效
标题翻译：安全霉素类抗坏血病素系列化合物，用途及其合成
公开(公告)号：US06936714B2
公开(公告)日：2005-08-30
申请号：US10728580
申请日：2003-12-05
申请人： Samuel J. Danishefsky , Bishan Zhou
发明人： Samuel J. Danishefsky , Bishan Zhou
IPC分类号： A61K31/4995 , A61P35/00 , C07C271/22 , C07D217/24 , C07D471/18 , C07D491/04 , C07D491/056 , C07D491/22 , C07D471/14
CPC分类号： C07D491/04 , C07D217/24
摘要： Compounds of the saframycin-ecteinascidin series with cytotoxic properties having the following general formula, their uses and synthesis, are disclosed: wherein R1 and R4 is H, a C1 to C4 alkyl group, or an acyl group; wherein R2 is an ether, ester, amide, or a phthalimide group; wherein R3 is ═O, OH, an ether group, an acyl group such as OC(O)Me, OC(O)Bn and OC(O)Et, or a sulfide group; wherein R5 is H, halogen, OH, an ether group, an acyl group, or an amide group; wherein R6 is ═O, OH, OCH3, CN, or an acyloxy group; wherein R7, is ═O, OH, halogen, an ether group, or an acyl group; wherein R8 and R9 are independently H, CH3, OCH3, OC2H5, CF3, halogen such as Br and F, or R8 and R9 are joined together as a methylenedioxy group, or other five or six membered ring; wherein R10 and R11 are independently CH3, OCH3, OC2H5, SCH3, or SC2H5; wherein R12 is H, a C1 to C4 alkyl group, or an acyl group; and wherein the chiral center marked * has the R or the S configuration.
摘要翻译：公开了具有以下通式及其用途和合成的具有细胞毒性的安全霉素 - 白in素类化合物的化合物：其中R 1和R 4均为H，C < 或C 1至C 4烷基，或酰基; 其中R 2是醚，酯，酰胺或邻苯二甲酰亚胺基团; 其中R 3为-O，OH，醚基，酰基如OC（O）Me，OC（O）Bn和OC（O）Et）或硫醚基; 其中R 5是H，卤素，OH，醚基，酰基或酰胺基; 其中R 6为-O，OH，OCH 3，CN或酰氧基; 其中R 7为-O，OH，卤素，醚基或酰基; 其中R 8和R 9独立地为H，CH 3，OCH 3，OC 2， CH 3，CF 3，卤素如Br和F，或R 8和R 9，作为亚甲二氧基或其它五元或六元环连接在一起; 其中R 10和R 11独立地是CH 3，OCH 3，OC 2， 5 H 3，SCH 3，或SC 2 H 5; 其中R 12是H，C 1至C 4烷基或酰基; 并且其中标记为*的手性中心具有R或S构型。

10. 发明申请

US20100087446A1 2-SUBSTITUTED INDOLE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS 审中-公开
标题翻译： 2取代的吲哚衍生物作为钙通道阻断剂
公开(公告)号：US20100087446A1
公开(公告)日：2010-04-08
申请号：US12597081
申请日：2008-04-22
申请人： Prasun K. Chakravarty , Joseph L. Duffy , Min K. Park , Sriram Tyagarajan , Bishan Zhou
发明人： Prasun K. Chakravarty , Joseph L. Duffy , Min K. Park , Sriram Tyagarajan , Bishan Zhou
IPC分类号： A61K31/404 , C07D209/04 , C07D401/04 , C07D403/06 , A61K31/4439 , A61K31/496 , A61P25/00 , A61P25/08
CPC分类号： C07D209/08 , C07D209/10 , C07D209/12 , C07D209/14 , C07D209/18 , C07D209/30 , C07D209/42 , C07D401/04 , C07D403/04 , C07D403/06 , C07D413/04 , C07D413/14 , C07D417/04
摘要： 2-Substituted indole derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
摘要翻译：由式I表示的2-取代的吲哚衍生物或其药学上可接受的盐。药物组合物包含单独的或与一种或多种其它治疗活性化合物组合的有效量的本发明化合物和药学上可接受的载体。治疗与钙通道活性相关或由其引起的疾病的方法，包括例如急性疼痛，慢性疼痛，内脏痛，炎性疼痛，神经性疼痛，尿失禁，瘙痒，过敏性皮炎，癫痫，糖尿病性神经病，肠易激综合征综合征，抑郁症，焦虑症，多发性硬化症，双相性精神障碍和中风，包括单独或与一种或多种其它治疗活性化合物组合施用有效量的本发明化合物。

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