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1. 发明申请

WO1996006097A1 NEW MULTIMERIZING AGENTS 审中-公开
标题翻译：新型多功能药剂
公开(公告)号：WO1996006097A1
公开(公告)日：1996-02-29
申请号：PCT/US1995010559
申请日：1995-08-18
申请人： ARIAD GENE THERAPEUTICS, INC. , HOLT, Dennis, A. , SCHREIBER, Stuart , KEENAN, Terence , GUO, Tao , LABORDE, Edgardo
发明人： ARIAD GENE THERAPEUTICS, INC.
IPC分类号： C07D471/04
CPC分类号： C07D401/14 , C07D207/16 , C07D211/60 , C07D401/12 , C07D405/12
摘要： New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains. The compounds are of the formula: M -L-M where M and M are independently moieties of formula (II), in which R , R , n, X and Y are as defined.
摘要翻译：公开了用于多聚化免疫亲和素和含有免疫亲和素相关结构域的蛋白质的新化合物。化合物具有下式：M 1 -LM 2其中M 1和M 2独立地是式（II）的部分，其中R 1，R 2，n，X 和Y如所定义。

2. 发明申请

WO1997031898A1 SYNTHETIC DERIVATIVES OF RAPAMYCIN AS MULTIMERIZING AGENTS FOR CHIMERIC PROTEINS WITH IMMUNOPHILIN-DERIVED DOMAINS 审中-公开
标题翻译： RAPAMYCIN作为多发性蛋白质与免疫球蛋白衍生域的多重化合物的合成衍生物
公开(公告)号：WO1997031898A1
公开(公告)日：1997-09-04
申请号：PCT/US1997003137
申请日：1997-02-28
申请人： ARIAD GENE THERAPEUTICS, INC. , HOLT, Dennis, A. , KEENAN, Terence, P. , GUO, Tao , LABORDE, Edgardo , YANG, Wu
发明人： ARIAD GENE THERAPEUTICS, INC.
IPC分类号： C07D211/60
CPC分类号： C07D401/14 , C07D207/16 , C07D211/60 , C07D401/12 , C07D405/12
摘要： New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains. The compounds are of the formula (I): M-L-Q, a resolved stereoisomer thereof or mixture of one or more such stereoisomers, and pharmaceutically acceptable salts thereof, wherein M is an immunophilin-binding group comprising a moiety of formula (II); G is independently selected from the group consisting of (a), (b), and (c); Q comprises a moiety of formula (II), a naturally occurring macrocyclic FKBP ligand or derivative thereof, or is a synthetic FKBP ligand of formula (III); n = 1 or 2; X = O, NH or CH2; B and B are independently H or aliphatic, heteroaliphatic, aryl or heteroaryl; Y = O, S, NH, -NH(C=O)-, -NH(C=O)-O-, -NH(SO2)- or NR , or represents a covalent bond from R to carbon 9; R , R , and R are the same or different and are independently aliphatic, heteroaliphatic, aryl or heteroaryl; and, L is a linker moiety covalently linking monomers M to Q or covalently linking M to M through covalent bonds to either R , R , not necessarily the same in each of M and M .
摘要翻译：公开了用于多聚化免疫亲和素和含有免疫亲和素相关结构域的蛋白质的新化合物。所述化合物具有式（I）：M-L-Q，其拆分立体异构体或一种或多种此类立体异构体的混合物及其药学上可接受的盐，其中M为包含式（II）部分的免疫亲和力结合基团。 G独立地选自（a），（b）和（c）组成的组。 Q包括式（II）的部分，天然存在的大环FKBP配体或其衍生物，或者是式（III）的合成FKBP配体; n = 1或2; X = O，NH或CH 2; B 1和B 2独立地是H或脂族，杂脂族，芳基或杂芳基; Y = O，S，NH，-NH（C = O） - ， - NH（C = O）-O-，-NH（SO 2） - 或NR 3，或表示来自R 2的共价键到碳9; R 1，R 2和R 3相同或不同，独立地为脂族，杂脂族，芳基或杂芳基; 并且L是将单体M与Q共价连接或通过共价键通过共价键与M 2共价连接至R 1，R 2的连接部分，在M <1中不一定相同 >和M <2>。

3. 发明申请

WO2005014600A1 ANTAGONISTS OF MCP-1 FUNCTION AND METHODS OF USE THEREOF 审中-公开
标题翻译： MCP-1功能的拮抗剂及其使用方法
公开(公告)号：WO2005014600A1
公开(公告)日：2005-02-17
申请号：PCT/US2004/025400
申请日：2004-08-06
申请人： TELIK, INC. , SANWA KAGAKU KENKYUSHO CO., LTD , LABORDE, Edgardo , ROBINSON, Louise , MENG, Fanying , PETERSON, Brian, T. , VILLAR, Hugo, O. , ANUSKIEWICZ, Steven, E. , MA, Wenli , MATSUMOTO, Yukiharu , BABA, Kunihisa , INAGAKI, Hideaki , TANAKA, Katsumasa , ISHIWATA, Yoshiro , YOKOCHI, Shoji , OKAMOTO, Masayuki , NAKAMURA, Takashi , MIYACHI, Atsushi , TAKEUCHI, Mitsuaki , MATSUSHIMA, Kouji
发明人： LABORDE, Edgardo , ROBINSON, Louise , MENG, Fanying , PETERSON, Brian, T. , VILLAR, Hugo, O. , ANUSKIEWICZ, Steven, E. , MA, Wenli , MATSUMOTO, Yukiharu , BABA, Kunihisa , INAGAKI, Hideaki , TANAKA, Katsumasa , ISHIWATA, Yoshiro , YOKOCHI, Shoji , OKAMOTO, Masayuki , NAKAMURA, Takashi , MIYACHI, Atsushi , TAKEUCHI, Mitsuaki , MATSUSHIMA, Kouji
IPC分类号： C07D498/04
CPC分类号： A61K31/437 , A61K9/0019 , A61K9/2054 , A61K9/4866 , A61K31/496 , A61K31/5377 , A61K31/5513 , A61K45/06 , C07D231/56 , C07D471/04 , A61K2300/00
摘要： Compounds of formula (A) and formula (B): and their pharmaceutically acceptable salts, compositions comprising them, methods for their use, and their use in the preparation of medicaments. The compounds are antagonists of MCP-1 function, and are useful in the prevention and treatment of chronic or acute inflammatory or autoimmune diseases, such as multiple sclerosis, and in the prevention and treatment of allergic hypersensitivity diseases.
摘要翻译：式（A）和式（B）的化合物及其药学上可接受的盐，包含它们的组合物，其使用方法及其在制备药物中的用途。这些化合物是MCP-1功能的拮抗剂，可用于预防和治疗慢性或急性炎症或自身免疫性疾病如多发性硬化，以及预防和治疗过敏性超敏反应性疾病。

4. 发明申请

WO1997031899A1 SYNTHETIC DERIVATIVES OF RAPAMYCIN AS MULTIMERISING AGENTS FOR CHIMERIC PROTEINS WITH IMMUNOPHILIN DERIVED DOMAINS 审中-公开
标题翻译： RAPAMYCIN作为多发性蛋白质与免疫球蛋白衍生系统的多态性代谢物的合成衍生物
公开(公告)号：WO1997031899A1
公开(公告)日：1997-09-04
申请号：PCT/US1997003157
申请日：1997-02-28
申请人： ARIAD GENE THERAPEUTICS, INC. , HOLT, Dennis, A. , KEENAN, Terence, P. , GUO, Tao , LABORDE, Edgardo , YANG, Wu
发明人： ARIAD GENE THERAPEUTICS, INC.
IPC分类号： C07D211/60
CPC分类号： C07D401/14 , C07D207/16 , C07D211/60 , C07D401/12 , C07D405/12
摘要： New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains. The compounds are of the formula M -L-M where M and M are independently moieties of formula (II), (a) or (b), in which B , B , B , R , R , n, W, X and Y are as defined.
摘要翻译：公开了用于多聚化免疫亲和素和含有免疫亲和素相关结构域的蛋白质的新化合物。化合物具有式M 1 -LM 2，其中M 1和M 2独立地是式（II），（a）或（b）的部分，其中B 1，B 2 2，B 3，R 1，R 2，n，W，X和Y如上所定义。

5. 发明申请

WO2009076473A1 2-{[2-(SUBSTITUTED AMINO)ETHYL]SULFONYL}ETHYL N,N-BIS(2- CHLOROETHYL)PHOSPHORODIAMIDATES 审中-公开
标题翻译： 2 - {[2-（取代的氨基）乙基]磺酰基}乙基N，N-双（2-氯代乙基）磷酰二胺
公开(公告)号：WO2009076473A1
公开(公告)日：2009-06-18
申请号：PCT/US2008/086286
申请日：2008-12-10
申请人： TELIK, INC. , LABORDE, Edgardo , KELSON, Andrew B. , MA, Wenli , WEBER, Kevin T.
发明人： LABORDE, Edgardo , KELSON, Andrew B. , MA, Wenli , WEBER, Kevin T.
IPC分类号： C07F9/24 , A61K31/664 , A61P35/04
CPC分类号： C07F9/2458 , C07F9/2408
摘要： 2- {[2 (Substituted amino)ethyl]sulfonyl}ethyl N,N bis(2 chloroethyl)phosphorodiamidates and their salts, their preparation and intermediates in their preparation, pharmaceutical compositions containing them, and methods of treatment using them. The compounds are useful for treating cancer and autoimmune diseases, alone and in combination with other therapies.
摘要翻译： 2 - {[2（取代氨基）乙基]磺酰基}乙基N，N-双（2-氯乙基）磷酰胺及其盐，其制备方法和中间体，含有它们的药物组合物，以及使用它们的治疗方法。这些化合物可用于单独治疗癌症和自身免疫性疾病，并与其他疗法结合使用。

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