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11. 发明申请

US20080280873A1 Biaryl Substituted Pyrazinones as Sodium Channel Blockers 审中-公开
标题翻译：二芳基取代的吡嗪酮作为钠通道阻断剂
公开(公告)号：US20080280873A1
公开(公告)日：2008-11-13
申请号：US10594367
申请日：2005-03-25
申请人： Jun Liang , Prasun K. Chakravarty , Deborah E. Pan , William H. Parsons , Pengcheng P. Shao , Feng Yee , Bishan Zhou
发明人： Jun Liang , Prasun K. Chakravarty , Deborah E. Pan , William H. Parsons , Pengcheng P. Shao , Feng Yee , Bishan Zhou
IPC分类号： A61K31/4965 , C07D241/24
CPC分类号： C07D241/24 , B05B1/02 , B05B1/14 , B05B1/34 , B65D83/20 , C07D241/18 , C07D403/06 , C07D405/04 , C07D413/06
摘要： Biaryl substituted pyrazinone compounds 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, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, 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表示的二芳基取代的吡嗪酮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，尿失禁，瘙痒，过敏性皮炎，癫痫，肠易激综合征，抑郁症，焦虑，多发性硬化和双相性精神障碍，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。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。

12. 发明授权

US07589116B2 Biaryl substituted pyrazoles as sodium channel blockers 失效
标题翻译：二芳基取代的吡唑作为钠通道阻断剂
公开(公告)号：US07589116B2
公开(公告)日：2009-09-15
申请号：US10552024
申请日：2004-03-30
申请人： Prasun K. Chakravarty , Michael H. Fisher , Jeffrey M. Fisher, legal representative , William H. Parsons , Sriram Tyagarajan , Bishan Zhou
发明人： Prasun K. Chakravarty , Michael H. Fisher , William H. Parsons , Sriram Tyagarajan , Bishan Zhou
IPC分类号： A61K31/415 , C07D231/00
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.
摘要翻译：双芳基取代的吡唑化合物是可用于治疗疼痛和其它病症的钠通道阻断剂。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。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治疗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。

13. 发明授权

US06686470B2 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：US06686470B2
公开(公告)日：2004-02-03
申请号：US09765515
申请日：2001-01-19
申请人： Samuel J. Danishefsky , Bishan Zhou
发明人： Samuel J. Danishefsky , Bishan Zhou
IPC分类号： C07D49122
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 - 海e素类化合物的化合物：其中R 1和R 4是H，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R5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R8和R9独立地为H，CH3，OCH3，OC2H5，CF3，卤素如Br和F，或R8和R9作为亚甲二氧基或其他五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 H 5，SCH 3或SC 2 H 5; 其中R 12为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。

14. 发明授权

US06172205B2 Synthetic process toward total synthesis of eleutherobin and its analogues and uses thereof 失效
标题翻译：合成方法，全面合成eleutherobin及其类似物及其用途
公开(公告)号：US06172205B2
公开(公告)日：2001-01-09
申请号：US09210290
申请日：1998-12-11
申请人： Samuel J. Danishefsky , Xiao-Tao Chen , Clare E. Gutteridge , Samit K. Bhattacharya , Bishan Zhou
发明人： Samuel J. Danishefsky , Xiao-Tao Chen , Clare E. Gutteridge , Samit K. Bhattacharya , Bishan Zhou
IPC分类号： C07G1100
CPC分类号： C07H15/04 , C07H15/26 , C07H17/04
摘要： This invention provides a process for the preparation of a Eleutherobin derivative of the formula: wherein R1 is a hydrogen, ester, nitrile or C2H4—R wherein R4 is a carbohydrate, an alcohol an amine, an amide, an alkyne, or, R2 is a linear or branched alkyl moiety, R3 is an ester, an amide, a carbamate, an acetal compound,an ether or a urethane, R4 is a hydrogen or CH2,position C2 and C3 is cis or trans,position C8 is &agr; or &bgr; and a compound is produced having the structures: Additionally, this experiment provides a method for inhibiting growth of cancerous cells comprising contracting an amount of Eleutherobin derivative effective to inhibit the growth of said cells. Further provided is a method for treating cancer in a subject which comprises administering to the subject a therapeutically effective amount of the Eleutherobin derivative.
摘要翻译：本发明提供了制备下式的十六烯炔酯衍生物的方法：其中R1是氢，酯，腈或C2H4-R，其中R4是碳水化合物，醇和胺，酰胺，炔烃，或者R2是直链或支链烷基部分，R3为酯，酰胺，氨基甲酸酯，缩醛化合物，醚或氨基甲酸酯，R4为氢或CH2，C2和C3为顺式或反式，C8为α或β 并且产生具有以下结构的化合物：另外，该实验提供了抑制癌细胞生长的方法，包括收缩一定量的有效抑制所述细胞生长的埃叶塞类衍生物。还提供了一种用于治疗受试者的癌症的方法，其包括向所述受试者施用治疗有效量的埃柳塞星衍生物。

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