-
1.
公开(公告)号:US20120093891A1
公开(公告)日:2012-04-19
申请号:US13333526
申请日:2011-12-21
申请人: John Yan , Xiaoxia Zheng , Vinayak D. Bhat
发明人: John Yan , Xiaoxia Zheng , Vinayak D. Bhat
IPC分类号: A61K31/436 , A61K9/00 , A61F2/82 , A61M25/00 , A61P7/02 , A61P29/00 , A61P35/00 , A61P37/06 , A61M25/10 , C07D498/16 , A61F2/02 , B82Y5/00
CPC分类号: A61K31/787 , A61L27/34 , A61L27/54 , A61L29/085 , A61L29/16 , A61L31/10 , A61L31/16 , A61L2300/416 , A61K2300/00
摘要: The present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of the formula: wherein R1, R2, R3, R5, R6 and R8 are each independently a member selected from the group consisting of H, C1-6 alkyl and OH; R4, R7 and R9 are each independently selected from the group consisting of C1-6 alkoxy and OH; R10 is a member selected from the group consisting of H, —OH, —OP(O)Me2, —O—(CH2)n—OH and —O—(CH2)m—O—(CH2)o—CH3, wherein subscripts n and m are each independently from 2 to 8 and subscript o is from 1 to 6; each of L1 and L4 are independently selected from the group consisting of: each of L2 and L3 are independently selected from the group consisting of: and salts, hydrates, isomers, metabolites and prodrugs thereof.
摘要翻译: 本发明提供包含药学上可接受的赋形剂和下式化合物的药物组合物:其中R 1,R 2,R 3,R 5,R 6和R 8各自独立地选自H,C 1-6烷基和OH ; R 4,R 7和R 9各自独立地选自C 1-6烷氧基和OH; R 10是选自H,-OH,-OP(O)Me 2,-O-(CH 2)n -OH和-O-(CH 2)m -O-(CH 2)o -CH 3的成员,其中 下标n和m各自独立地为2至8,下标o为1至6; L1和L4中的每一个独立地选自以下各项:L2和L3各自独立地选自:和其盐,水合物,异构体,代谢物和前药。
-
公开(公告)号:US08088789B2
公开(公告)日:2012-01-03
申请号:US12046024
申请日:2008-03-11
申请人: John Yan , Xiaoxia Zheng , Vinayak D. Bhat
发明人: John Yan , Xiaoxia Zheng , Vinayak D. Bhat
IPC分类号: A61K31/427 , A61K31/4525 , A61K31/365 , A61K31/4353 , A61K31/436
CPC分类号: A61K31/436 , A61K9/0004 , A61K31/439 , A61K31/4525 , A61K45/06
摘要: A method of treating an ophthalmic condition or disease by administering a compound disclosed herein is provided. The compound can be administered systemically or locally and in a variety of ways, such as via a temporary device, an implant, an injection or an eye drop. The compound can also be administered with an additional therapeutic agent.
摘要翻译: 提供了通过施用本文公开的化合物治疗眼部疾病或疾病的方法。 化合物可以全身或局部地以各种方式施用,例如经由临时装置,植入物,注射剂或滴眼剂。 化合物也可以与另外的治疗剂一起施用。
-
3.
公开(公告)号:US20080138375A1
公开(公告)日:2008-06-12
申请号:US11854312
申请日:2007-09-12
申请人: John Yan , Xiaoxia Zheng , Vinayak D. Bhat
发明人: John Yan , Xiaoxia Zheng , Vinayak D. Bhat
IPC分类号: A61F2/02 , A61K31/4353 , C07D221/06 , A61P43/00
CPC分类号: A61K31/787 , A61L27/34 , A61L27/54 , A61L29/085 , A61L29/16 , A61L31/10 , A61L31/16 , A61L2300/416 , A61K2300/00
摘要: The present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of the formula: wherein R1, R2, R3, R5, R6 and R8 are each independently a member selected from the group consisting of H, C1-6 alkyl and OH; R4, R7 and R9 are each independently selected from the group consisting of C1-6 alkoxy and OH; R10 is a member selected from the group consisting of H, —OH, —OP(O)Me2, —O—(CH2)n—OH and —O—(CH2)m—O—(CH2)o— CH3, wherein subscripts n and m are each independently from 2 to 8 and subscript o is from 1 to 6; each of L1 and L4 are independently selected from the group consisting of: each of L2 and L3 are independently selected from the group consisting of: salts, hydrates, isomers, metabolites and prodrugs thereof.
摘要翻译: 本发明提供一种药物组合物,其包含药学上可接受的赋形剂和下式化合物:其中R 1,R 2,R 3, R 5,R 6和R 8各自独立地是选自H,C 1-6, 烷基和OH; R 4,R 7和R 9各自独立地选自C 1-6 - 烷氧基 和OH; R 10是选自H,-OH,-OP(O)Me 2,-O - (CH 2/2), OH)和-O-(CH 2 CH 2)m -O - (CH 2 CH 2) 其中下标n和m各自独立地为2至8,下标o为1至6; L 1和L 4中的每一个独立地选自:L 2和L 3中的每一个, 独立地选自:其盐,水合物,异构体,代谢物和前药。
-
公开(公告)号:US09149470B2
公开(公告)日:2015-10-06
申请号:US13302588
申请日:2011-11-22
申请人: John Yan , Xiaoxia Zheng , Vinayak D. Bhat
发明人: John Yan , Xiaoxia Zheng , Vinayak D. Bhat
IPC分类号: A61K31/4741 , A61K31/4525 , A61K31/365 , A61K31/436 , A61K31/427
CPC分类号: A61K31/436 , A61K9/0004 , A61K31/439 , A61K31/4525 , A61K45/06
摘要: The present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of the general formula:
摘要翻译: 本发明提供药物组合物,其包含药学上可接受的赋形剂和通式如下的化合物:
-
5.
公开(公告)号:US20120071500A1
公开(公告)日:2012-03-22
申请号:US13302588
申请日:2011-11-22
申请人: John Yan , Xiaoxia Zheng , Vinayak D. Bhat
发明人: John Yan , Xiaoxia Zheng , Vinayak D. Bhat
IPC分类号: A61K31/4741
CPC分类号: A61K31/436 , A61K9/0004 , A61K31/439 , A61K31/4525 , A61K45/06
摘要: The present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of the formula: wherein R1, R2, R3, R5, R6, R8, M1, M2, M3, M4, M5, M6 and M7 are each independently a member selected from the group consisting of H, C1-6 alkyl, OH and C1-6 hydroxyalkyl; R4, R7 and R9 are each independently selected from the group consisting of C1-6 alkoxy and OH; R10 is a member selected from the group consisting of H, —OH, —OP(O)Me2, —O—(CH2)n—OH and —O—(CH2)m—O—(CH2)o—CH3, wherein subscripts n and m are each independently from 2 to 8 and subscript o is from 1 to 6; each of L1 and L4 are independently selected from the group consisting of: wherein each M8 is independently a member selected from the group consisting of C1-6 alkyl, OH and C1-6 hydroxyalkyl; each of L2 and L3 are independently selected from the group consisting of: and salts, hydrates, isomers, metabolites, N-oxides and prodrugs thereof.
摘要翻译: 本发明提供包含药学上可接受的赋形剂和下式化合物的药物组合物:其中R1,R2,R3,R5,R6,R8,M1,M2,M3,M4,M5,M6和M7各自独立地为成员 选自H,C 1-6烷基,OH和C 1-6羟基烷基; R 4,R 7和R 9各自独立地选自C 1-6烷氧基和OH; R 10是选自H,-OH,-OP(O)Me 2,-O-(CH 2)n -OH和-O-(CH 2)m -O-(CH 2)o -CH 3的成员,其中 下标n和m各自独立地为2至8,下标o为1至6; L1和L4各自独立地选自:其中每个M8独立地是选自C 1-6烷基,OH和C 1-6羟基烷基的成员; L2和L3中的每一个独立地选自:其盐,水合物,异构体,代谢物,N-氧化物和前药。
-
6.
公开(公告)号:US20100086579A1
公开(公告)日:2010-04-08
申请号:US12572529
申请日:2009-10-02
申请人: John Yan , Xiaoxia Zheng , Vinayak D. Bhat
发明人: John Yan , Xiaoxia Zheng , Vinayak D. Bhat
IPC分类号: A61K9/00 , A61K31/4353 , A61K39/395 , A61P31/00
CPC分类号: A61K31/436 , A61K45/06 , A61L29/041 , A61L29/148 , A61L29/16 , A61L31/048 , A61L31/148 , A61L31/16 , A61L2300/41 , A61L2300/416 , A61L2300/42 , A61L2300/426
摘要: The present invention provides a device for intracorporeal use including an implant or a temporary device and at least one source of a compound myolimus, or a derivative thereof. The present invention also provides a method of inhibiting cell proliferation by local administration of a therapeutically effective amount of a compound myolimus, or a derivative thereof. Further included in the present invention is a method of treating an ophthalmic condition or disease by administering a therapeutically effective amount of a compound myolimus, or a derivative thereof.
摘要翻译: 本发明提供了一种用于体内使用的装置,包括植入物或临时装置和至少一种化合物myolimus的源或其衍生物。 本发明还提供了通过局部施用治疗有效量的化合物肌醇酰胺或其衍生物来抑制细胞增殖的方法。 本发明还包括通过施用治疗有效量的化合物myolimus或其衍生物来治疗眼科疾病或疾病的方法。
-
7.
公开(公告)号:US20080234309A1
公开(公告)日:2008-09-25
申请号:US12046024
申请日:2008-03-11
申请人: John Yan , Xiaoxia Zheng , Vinayak D. Bhat
发明人: John Yan , Xiaoxia Zheng , Vinayak D. Bhat
IPC分类号: A61K31/4525 , A61P27/02 , C07D491/052
CPC分类号: A61K31/436 , A61K9/0004 , A61K31/439 , A61K31/4525 , A61K45/06
摘要: The present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of the formula: wherein R1, R2, R3, R5, R6, R8, M1, M2, M3, M4, M5, M6 and M7 are each independently a member selected from the group consisting of H, C1-6 alkyl, OH and C1-6 hydroxyalkyl; R4, R7 and R9 are each independently selected from the group consisting of C1-6 alkoxy and OH; R10 is a member selected from the group consisting of H, —OH, —OP(O)Me2, —O—(CH2)n—OH and —O—(CH2)m—O—(CH2)o—CH3, wherein subscripts n and m are each independently from 2 to 8 and subscript o is from 1 to 6; each of L1 and L4 are independently selected from the group consisting of: wherein each M8 is independently a member selected from the group consisting of C1-6 alkyl, OH and C1-6 hydroxyalkyl; each of L2 and L3 are independently selected from the group consisting of: and salts, hydrates, isomers, metabolites, N-oxides and prodrugs thereof.
摘要翻译: 本发明提供一种药物组合物,其包含药学上可接受的赋形剂和下式化合物:其中R 1,R 2,R 3, R 5,R 6,R 8,M 1,M 2, M 3,M 4,M 5,M 6和M 7均为 各自独立地是选自H,C 1-6烷基,OH和C 1-6 1-6羟基烷基的成员; R 4,R 7和R 9各自独立地选自C 1-6 - 烷氧基 和OH; R 10是选自H,-OH,-OP(O)Me 2,-O - (CH 2/2), OH)和-O-(CH 2 CH 2)m -O - (CH 2 CH 2) 其中下标n和m各自独立地为2至8,下标o为1至6; L 1和L 4中的每一个独立地选自:其中每个M 8独立地是选自以下的成员: 的C 1-6烷基,OH和C 1-6烷基羟基烷基; L 2和L 3中的每一个独立地选自:其盐,水合物,异构体,代谢物,N-氧化物和前药。
-
公开(公告)号:US08404641B2
公开(公告)日:2013-03-26
申请号:US13333573
申请日:2011-12-21
申请人: John Yan , Xiaoxia Zheng , Vinayak D. Bhat
发明人: John Yan , Xiaoxia Zheng , Vinayak D. Bhat
IPC分类号: A61K31/365 , A61K31/436 , A61L27/00 , A61L29/00
CPC分类号: A61K31/787 , A61L27/34 , A61L27/54 , A61L29/085 , A61L29/16 , A61L31/10 , A61L31/16 , A61L2300/416 , A61K2300/00
摘要: A method of inhibiting cell migration or treating an inflammatory condition, comprising administering a compound disclosed herein to the subject, is provided. The compound can be administered systemically, locally, or a combination thereof. For example, the compound can be locally delivered from a temporary device or an implant, such as a vascular prosthesis.
摘要翻译: 提供了抑制细胞迁移或治疗炎性病症的方法,其包括将本文公开的化合物施用于受试者。 化合物可以全身,局部施用或其组合施用。 例如,化合物可以从临时装置或植入物如血管假体局部递送。
-
公开(公告)号:US08367081B2
公开(公告)日:2013-02-05
申请号:US13333526
申请日:2011-12-21
申请人: John Yan , Xiaoxia Zheng , Vinayak D. Bhat
发明人: John Yan , Xiaoxia Zheng , Vinayak D. Bhat
IPC分类号: A61K31/436 , A61F9/00 , A61F2/02 , A61F2/82
CPC分类号: A61K31/787 , A61L27/34 , A61L27/54 , A61L29/085 , A61L29/16 , A61L31/10 , A61L31/16 , A61L2300/416 , A61K2300/00
摘要: A method of inhibiting smooth muscle cell proliferation or cytokine production in a subject, comprising administering a compound disclosed herein to the subject, is provided. The compound can be administered systemically, locally, or a combination thereof. For example, the compound can be locally delivered from a temporary device or an implant, such as a vascular prosthesis.
摘要翻译: 提供一种抑制受试者平滑肌细胞增殖或细胞因子产生的方法,包括将本文公开的化合物施用于受试者。 化合物可以全身,局部施用或其组合施用。 例如,化合物可以从临时装置或植入物如血管假体局部递送。
-
公开(公告)号:US20120094932A1
公开(公告)日:2012-04-19
申请号:US13333573
申请日:2011-12-21
申请人: John Yan , Xiaoxia Zheng , Vinayak D. Bhat
发明人: John Yan , Xiaoxia Zheng , Vinayak D. Bhat
IPC分类号: A61K31/436 , A61K31/616 , A61K31/5415 , A61K31/542 , A61P7/02 , A61K38/13 , A61P35/00 , A61P37/00 , A61P29/00 , A61P37/06 , A61K31/727 , A61K31/573
CPC分类号: A61K31/787 , A61L27/34 , A61L27/54 , A61L29/085 , A61L29/16 , A61L31/10 , A61L31/16 , A61L2300/416 , A61K2300/00
摘要: The present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of the formula: wherein R1, R2, R3, R5, R6 and R8 are each independently a member selected from the group consisting of H, C1-6 alkyl and OH; R4, R7 and R9 are each independently selected from the group consisting of C1-6 alkoxy and OH; R10 is a member selected from the group consisting of H, —OH, —OP(O)Me2, —O—(CH2)n—OH and —O—(CH2)m—O—(CH2)o—CH3, wherein subscripts n and m are each independently from 2 to 8 and subscript o is from 1 to 6; each of L1 and L4 are independently selected from the group consisting of: each of L2 and L3 are independently selected from the group consisting of: and salts, hydrates, isomers, metabolites and prodrugs thereof.
-
-
-
-
-
-
-
-
-