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1. 发明申请

US20110223134A1 FUSED TRICYCLIC SILYL COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES 有权
标题翻译：熔融的三聚硅氧烷化合物及其用于治疗病毒性疾病的方法
公开(公告)号：US20110223134A1
公开(公告)日：2011-09-15
申请号：US13041082
申请日：2011-03-04
申请人： Anilkumar Gopinadhan Nair , Kerry M. Keertikar , Seong Heon Kim , Joseph A. Kozlowski , Stuart Rosenblum , Oleg B. Selyutin , Michael Wong , Wensheng Yu , Qingbei Zeng
发明人： Anilkumar Gopinadhan Nair , Kerry M. Keertikar , Seong Heon Kim , Joseph A. Kozlowski , Stuart Rosenblum , Oleg B. Selyutin , Michael Wong , Wensheng Yu , Qingbei Zeng
IPC分类号： A61K38/21 , C07F7/02 , A61P31/12 , A61K31/695 , A61K31/7056
CPC分类号： C07F7/0816
摘要： The present invention relates to novel Fused Tricyclic Silyl Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, C, D, M1, X1 and X2 are as defined herein. The present invention also relates to compositions comprising at least one Fused Tricyclic Silyl Compound, and methods of using the Fused Tricyclic Silyl Compounds for treating or preventing HCV infection in a patient.
摘要翻译：本发明涉及式（I）的新型稠合三环甲硅烷基化合物及其药学上可接受的盐，其中A，B，C，D，M1，X1和X2如本文所定义。本发明还涉及包含至少一种熔融三环甲硅烷基化合物的组合物，以及使用融合的三环甲硅烷基化合物治疗或预防患者HCV感染的方法。

2. 发明授权

US08609635B2 Fused tricyclic silyl compounds and methods of use thereof for the treatment of viral diseases 有权
标题翻译：稠合的三环甲硅烷基化合物及其用于治疗病毒性疾病的方法
公开(公告)号：US08609635B2
公开(公告)日：2013-12-17
申请号：US13041082
申请日：2011-03-04
申请人： Anilkumar Gopinadhan Nair , Kartik M. Keertikar , Seong Heon Kim , Joseph A. Kozlowski , Stuart Rosenblum , Oleg B. Selyutin , Michael Wong , Wensheng Yu , Qingbei Zeng
发明人： Anilkumar Gopinadhan Nair , Kartik M. Keertikar , Seong Heon Kim , Joseph A. Kozlowski , Stuart Rosenblum , Oleg B. Selyutin , Michael Wong , Wensheng Yu , Qingbei Zeng
IPC分类号： A61K31/695 , C07F7/10
CPC分类号： C07F7/0816
摘要： The present invention relates to novel Fused Tricyclic Silyl Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, C, D, M1, X1 and X2 are as defined herein. The present invention also relates to compositions comprising at least one Fused Tricyclic Silyl Compound, and methods of using the Fused Tricyclic Silyl Compounds for treating or preventing HCV infection in a patient.
摘要翻译：本发明涉及式（I）的新型稠合三环甲硅烷基化合物及其药学上可接受的盐，其中A，B，C，D，M1，X1和X2如本文所定义。本发明还涉及包含至少一种熔融三环甲硅烷基化合物的组合物，以及使用融合的三环甲硅烷基化合物治疗或预防患者HCV感染的方法。

3. 发明申请

US20070054919A1 Pyrazinyl substituted piperazine-piperidines with CXCR3 antagonist activity 有权
标题翻译：吡嗪基取代的哌嗪 - 哌啶与CXCR3拮抗剂活性
公开(公告)号：US20070054919A1
公开(公告)日：2007-03-08
申请号：US11354138
申请日：2006-02-14
申请人： Stuart Rosenblum , Seong Kim , Qingbei Zeng , Michael Wong , Gopinadhan Anilkumar , Yueheng Jiang , Wensheng Yu , Joseph Kozlowski , Neng-Yang Shih , Bandarpalle Shankar , Brian McGuinness , Guizhen Dong , Lisa Zawacki , Douglas Hobbs , John Baldwin , Yuefei Shao
发明人： Stuart Rosenblum , Seong Kim , Qingbei Zeng , Michael Wong , Gopinadhan Anilkumar , Yueheng Jiang , Wensheng Yu , Joseph Kozlowski , Neng-Yang Shih , Bandarpalle Shankar , Brian McGuinness , Guizhen Dong , Lisa Zawacki , Douglas Hobbs , John Baldwin , Yuefei Shao
IPC分类号： A61K31/497 , C07D403/14
CPC分类号： C07D405/14 , C07D401/12 , C07D401/14 , C07D413/14 , C07D417/14
摘要： The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: and the pharmaceutically acceptable salts, solvates and esters thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.
摘要翻译：本申请公开了所述化合物或所述前体药物的所述化合物或其药学上可接受的盐，溶剂合物或酯的化合物或对映异构体，立体异构体，旋转异构体，互变异构体或前药，所述化合物具有式1所示的一般结构：及其药学上可接受的盐，溶剂化物和酯。还公开了治疗趋化因子介导的疾病的方法，例如姑息治疗，疗效治疗，某些疾病和疾病如炎性疾病的预防性治疗（非限制性实例，牛皮癣），自身免疫性疾病（非限制性的例如，类风湿性关节炎，多发性硬化症），移植排斥反应（非限制性实例包括，同种异体移植排斥反应，异种移植物排斥），感染性疾病（例如结核性麻风病），固定药物爆发，皮肤迟发型超敏反应应答，眼部炎症，I型糖尿病，病毒性脑膜炎和使用式1的化合物的肿瘤。

4. 发明申请

US20060276448A1 Heteroaryl substituted pyrazinyl-piperazine-piperidines with CXCR3 antagonist activity 有权
标题翻译：具有CXCR3拮抗活性的杂芳基取代的吡嗪基 - 哌嗪 - 哌啶
公开(公告)号：US20060276448A1
公开(公告)日：2006-12-07
申请号：US11353474
申请日：2006-02-14
申请人： Qingbei Zeng , De-Yi Yang , Stuart Rosenblum , Michael Wong , Gopinadhan Anilkumar , Seong Kim , Wensheng Yu , Joseph Kozlowski , Neng-Yang Shih , Brian McGuinness , Lisa Guise-Zawacki , Doublas Hobbs
发明人： Qingbei Zeng , De-Yi Yang , Stuart Rosenblum , Michael Wong , Gopinadhan Anilkumar , Seong Kim , Wensheng Yu , Joseph Kozlowski , Neng-Yang Shih , Brian McGuinness , Lisa Guise-Zawacki , Doublas Hobbs
IPC分类号： A61K31/5377 , A61K31/506 , A61K31/497 , C07D413/14 , C07D403/14
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D487/04
摘要： The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts or solvates of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: and the pharmaceutically acceptable salts, solvates or esters thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.
摘要翻译：本申请公开了所述化合物或所述前药的所述化合物或其对映异构体，立体异构体，旋转异构体，互变异构体，外消旋体或前药，或所述前药的所述化合物，所述化合物具有式1所示的一般结构：和其药学上可接受的盐，溶剂合物或酯。还公开了治疗趋化因子介导的疾病的方法，例如姑息治疗，疗效治疗，某些疾病和疾病如炎性疾病的预防性治疗（非限制性实例，牛皮癣），自身免疫性疾病（非限制性的例如，类风湿性关节炎，多发性硬化症），移植排斥反应（非限制性实例包括同种异体移植排斥反应，异种移植排斥），感染性疾病（例如结核性麻风病），固定药物喷发，皮肤迟发型超敏反应应答，眼部炎症，I型糖尿病，病毒性脑膜炎和使用式1的化合物的肿瘤。

5. 发明申请

US20060276479A1 Heterocyclic substituted piperazines with CXCR3 antagonist activity 有权
标题翻译：具有CXCR3拮抗剂活性的杂环取代哌嗪
公开(公告)号：US20060276479A1
公开(公告)日：2006-12-07
申请号：US11353641
申请日：2006-02-14
申请人： Seong Kim , Gopinadhan Anilkumar , Michael Wong , Qingbei Zeng , Stuart Rosenblum , Joseph Kozlowski , Yuefei Shao , Brian McGuinness , Douglas Hobbs
发明人： Seong Kim , Gopinadhan Anilkumar , Michael Wong , Qingbei Zeng , Stuart Rosenblum , Joseph Kozlowski , Yuefei Shao , Brian McGuinness , Douglas Hobbs
IPC分类号： A61K31/497 , C07D413/14 , C07D403/14
CPC分类号： C07D401/12 , C07D401/14 , C07D413/14 , C07D417/14
摘要： The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof, wherein the various moieties are defined herein. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.
摘要翻译：本申请公开了所述化合物或所述前体药物的所述化合物或其药学上可接受的盐，溶剂合物或酯的化合物或对映异构体，立体异构体，旋转异构体，互变异构体或前药，所述化合物具有式1所示的一般结构：或其药学上可接受的盐，溶剂合物或酯，其中各种部分在本文中定义。还公开了治疗趋化因子介导的疾病的方法，例如姑息治疗，疗效治疗，某些疾病和疾病如炎性疾病的预防性治疗（非限制性实例，牛皮癣），自身免疫性疾病（非限制性的例如，类风湿性关节炎，多发性硬化症），移植排斥反应（非限制性实例包括，同种异体移植排斥反应，异种移植物排斥），感染性疾病（例如结核性麻风病），固定药物爆发，皮肤迟发型超敏反应应答，眼部炎症，I型糖尿病，病毒性脑膜炎和使用式1的化合物的肿瘤。

6. 发明申请

US20060276480A1 Amine-linked pyridyl and phenyl substituted piperazine-piperidines with CXCR3 antagonist activity 有权
公开(公告)号：US20060276480A1
公开(公告)日：2006-12-07
申请号：US11354328
申请日：2006-02-14
申请人： Michael Wong , Youheng Shu , Wensheng Yu , Stuart Rosenblum , Joseph Kozlowski , Brian McGuinness , Yuefei Shao , Douglas Hobbs
发明人： Michael Wong , Youheng Shu , Wensheng Yu , Stuart Rosenblum , Joseph Kozlowski , Brian McGuinness , Yuefei Shao , Douglas Hobbs
IPC分类号： A61K31/496 , C07D403/14
CPC分类号： C07D401/14 , C07D211/58 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: and the pharmaceutically acceptable salts, solvates and esters thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.

7. 发明申请

US20060217392A1 Novel heterocyclic substituted pyridine or phenyl compounds with CXCR3 antagonist activity 有权
标题翻译：新型杂环取代吡啶或具有CXCR3拮抗活性的苯基化合物
公开(公告)号：US20060217392A1
公开(公告)日：2006-09-28
申请号：US11353609
申请日：2006-02-14
申请人： Gopinadhan Anilkumar , Qingbei Zeng , Stuart Rosenblum , Joseph Kozlowski , Brian McGuinness , Douglas Hobbs
发明人： Gopinadhan Anilkumar , Qingbei Zeng , Stuart Rosenblum , Joseph Kozlowski , Brian McGuinness , Douglas Hobbs
IPC分类号： C07D403/14 , A61K31/496
CPC分类号： C07D417/14 , C07D401/04 , C07D401/14 , C07D413/14
摘要： The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prod rug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, zenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.
摘要翻译：本申请公开了所述化合物或所述前药的所述化合物或其药学上可接受的盐，溶剂合物或酯的化合物或对映异构体，立体异构体，旋转异构体，互变异构体，产物，所述化合物具有式 1：或其药学上可接受的盐，溶剂化物或酯。还公开了治疗趋化因子介导的疾病的方法，例如姑息治疗，疗效治疗，某些疾病和疾病如炎性疾病的预防性治疗（非限制性实例，牛皮癣），自身免疫性疾病（非限制性的例如，类风湿性关节炎，多发性硬化），移植物排斥（非限制性实例，包括同种异体移植排斥，移植排斥），感染性疾病（例如结核性麻风病），固定药物喷发，皮肤迟发型超敏反应应答，眼部炎症，I型糖尿病，病毒性脑膜炎和使用式1的化合物的肿瘤。

8. 发明申请

US20050113383A1 Novel non-imidazole compounds 失效
标题翻译：新型非咪唑化合物
公开(公告)号：US20050113383A1
公开(公告)日：2005-05-26
申请号：US10974329
申请日：2004-10-27
申请人： Stuart Rosenblum , Qingbei Zeng , Mwangi Mutahi , Robert Aslanian , Pauline Ting , Neng-Yang Shih , Daniel Solomon , Jianhua Cao , Henry Vaccaro , Kevin McCormick , John Baldwin , Ge Li
发明人： Stuart Rosenblum , Qingbei Zeng , Mwangi Mutahi , Robert Aslanian , Pauline Ting , Neng-Yang Shih , Daniel Solomon , Jianhua Cao , Henry Vaccaro , Kevin McCormick , John Baldwin , Ge Li
IPC分类号： C07D211/34 , A61K31/496 , A61P1/00 , A61P1/04 , A61P3/04 , A61P9/00 , A61P9/04 , A61P11/00 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/20 , A61P25/28 , A61P37/08 , A61P43/00 , C07D211/26 , C07D211/38 , C07D211/62 , C07D211/96 , C07D243/08 , C07D401/06 , C07D401/14 , C07D405/14 , C07D407/12 , C07D407/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14 , C07D451/02 , C07D487/06 , A61K31/4545 , C07D43/14 , C07D45/14
CPC分类号： C07D401/14 , C07D211/26 , C07D211/38 , C07D211/62 , C07D211/96 , C07D243/08 , C07D401/06 , C07D407/12 , C07D407/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14 , C07D451/02 , C07D487/06
摘要： Disclosed are novel compounds of the formula Also disclosed are pharmaceutical compositions comprising the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I in combination with a H1 receptor antagonist.
摘要翻译：公开的是式的新化合物还公开了包含式I化合物的药物组合物。还公开了治疗各种疾病或病症的方法，例如过敏，过敏诱发的气道反应和充血（例如，鼻拥塞）。还公开了使用组合式I化合物来治疗各种疾病或病症的方法，例如过敏，过敏诱发的气道反应和充血（例如，鼻塞）具有H 1受体拮抗剂。

9. 发明申请

US20060276457A1 Piperazine-piperidines with CXCR3 antagonist activity 有权
标题翻译：哌嗪 - 哌啶与CXCR3拮抗剂活性
公开(公告)号：US20060276457A1
公开(公告)日：2006-12-07
申请号：US11353806
申请日：2006-02-14
申请人： Wensheng Yu , Seong Kim , Gopinadhan Anilkumar , Stuart Rosenblum , Bandarpalle Shankar , Brian McGuinness , Douglas Hobbs , Yuefei Shao
发明人： Wensheng Yu , Seong Kim , Gopinadhan Anilkumar , Stuart Rosenblum , Bandarpalle Shankar , Brian McGuinness , Douglas Hobbs , Yuefei Shao
IPC分类号： A61K31/551 , A61K31/498 , A61K31/496 , A61K31/525 , C07D487/02 , C07D475/02
CPC分类号： C07D487/04 , C07D401/12
摘要： The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof, wherein the various moieties are defined herein. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.
摘要翻译：本申请公开了所述化合物或所述前体药物的所述化合物或其药学上可接受的盐，溶剂合物或酯的化合物或对映异构体，立体异构体，旋转异构体，互变异构体或前药，所述化合物具有式1所示的一般结构：或其药学上可接受的盐，溶剂合物或酯，其中各种部分在本文中定义。还公开了治疗趋化因子介导的疾病的方法，例如姑息治疗，疗效治疗，某些疾病和疾病如炎性疾病的预防性治疗（非限制性实例，牛皮癣），自身免疫性疾病（非限制性的例如，类风湿性关节炎，多发性硬化症），移植排斥反应（非限制性实例包括，同种异体移植排斥反应，异种移植物排斥），感染性疾病（例如结核性麻风病），固定药物爆发，皮肤迟发型超敏反应应答，眼部炎症，I型糖尿病，病毒性脑膜炎和使用式1的化合物的肿瘤。

10. 发明申请

US20070082913A1 Substituted heterocyclic compounds with CXCR3 antagonist activity 有权
标题翻译：取代的具有CXCR3拮抗剂活性的杂环化合物
公开(公告)号：US20070082913A1
公开(公告)日：2007-04-12
申请号：US11545201
申请日：2006-10-10
申请人： Seong Kim , Bandarpalle Shankar , Joseph Kozlowski , Stuart Rosenblum , Neng-Yang Shih
发明人： Seong Kim , Bandarpalle Shankar , Joseph Kozlowski , Stuart Rosenblum , Neng-Yang Shih
IPC分类号： A61K31/497 , A61K31/496 , C07D403/14
CPC分类号： C07D401/14 , C07D401/08 , C07D413/14
摘要： The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof, wherein the various moieties are defined herein. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, type I diabetes, viral meningitis and tumors using a compound of Formula 1.
摘要翻译：本申请公开了所述化合物或所述前体药物的所述化合物或其药学上可接受的盐，溶剂合物或酯的化合物或对映异构体，立体异构体，旋转异构体，互变异构体或前药，所述化合物具有式1所示的一般结构：或其药学上可接受的盐，溶剂合物或酯，其中各种部分在本文中定义。还公开了治疗趋化因子介导的疾病的方法，例如姑息治疗，疗效治疗，某些疾病和疾病如炎性疾病的预防性治疗（非限制性实例，牛皮癣），自身免疫性疾病（非限制性的例如，类风湿性关节炎，多发性硬化症），移植排斥反应（非限制性实例包括，同种异体移植排斥反应，异种移植物排斥），感染性疾病（例如结核性麻风病），固定药物爆发，皮肤迟发型超敏反应应答，I型糖尿病，病毒性脑膜炎和使用式1的化合物的肿瘤。

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