公开(公告)号：US20070037824A1

公开(公告)日：2007-02-15

申请号：US10654546

申请日：2003-09-03

申请人： Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  Ronald Doll ,  Viyyoor Girijavallabhan ,  Alan Mallams ,  Carmen Alvarez ,  Kartik Keertikar ,  Jocelyn Rivera ,  Tin-Yau Chan ,  Vincent Madison ,  Thierry Fischmann ,  Lawrence Dillard ,  Vinh Tran ,  Zhen He ,  Ray James ,  Haengsoon Park ,  Vidyadhar Paradkar ,  Douglas Hobbs

发明人： Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  Ronald Doll ,  Viyyoor Girijavallabhan ,  Alan Mallams ,  Carmen Alvarez ,  Kartik Keertikar ,  Jocelyn Rivera ,  Tin-Yau Chan ,  Vincent Madison ,  Thierry Fischmann ,  Lawrence Dillard ,  Vinh Tran ,  Zhen He ,  Ray James ,  Haengsoon Park ,  Vidyadhar Paradkar ,  Douglas Hobbs

IPC分类号： A61K31/519 ,  C07D487/02

CPC分类号： C07D487/04

摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

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。

公开(公告)号：US20060121187A1

公开(公告)日：2006-06-08

申请号：US11003137

申请日：2004-12-03

申请人： Jeffrey Haynes ,  Douglas Hobbs

发明人： Jeffrey Haynes ,  Douglas Hobbs

IPC分类号： B05D1/12 ,  B05C5/00 ,  B05D1/08

CPC分类号： C23C24/04

摘要： A method for depositing a metallic material onto a substrate comprises the steps of placing the substrate in a vacuum chamber, inserting a spray gun nozzle into a port of the vacuum chamber, and depositing a powdered metallic material onto a surface of the substrate without melting the powdered metal material. The depositing step comprises accelerating particles of the powdered metal materials within the vacuum chamber to a velocity so that upon impact the particles plastically deform and bond to a surface of the substrate.

摘要翻译： 用于将金属材料沉积到基底上的方法包括以下步骤：将基底放置在真空室中，将喷枪喷嘴插入真空室的端口中，并将粉末状金属材料沉积在基底表面上，而不熔化 金属粉末材料。 沉积步骤包括将真空室内的粉末金属材料的颗粒加速到一定的速度，使得在冲击时，颗粒塑性地变形并结合到衬底的表面。

公开(公告)号：US20050043290A1

公开(公告)日：2005-02-24

申请号：US10911030

申请日：2004-08-04

申请人： Jared Cumming ,  Ying Huang ,  Guoqing Li ,  Ulrich Iserloh ,  Andrew Stamford ,  Corey Strickland ,  Johannes Voigt ,  Yusheng Wu ,  Jianping Pan ,  Tao Guo ,  Douglas Hobbs ,  Thuy Le ,  Jeffrey Lowrie

发明人： Jared Cumming ,  Ying Huang ,  Guoqing Li ,  Ulrich Iserloh ,  Andrew Stamford ,  Corey Strickland ,  Johannes Voigt ,  Yusheng Wu ,  Jianping Pan ,  Tao Guo ,  Douglas Hobbs ,  Thuy Le ,  Jeffrey Lowrie

IPC分类号： C07D207/26 ,  C07D207/277 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  A61K31/55 ,  C07D43/02

CPC分类号： C04B35/632 ,  C07D207/277 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14

摘要： Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is X is —O—, —C(R14)2— or —N(R)—; Z is —C(R14)2— or —N(R)—; t is 0, 1, 2 or 3; each R and R2 is independently H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, alkenyl or alkynyl; each R14 is H, alkyl, alkenyl, alkynyl, halo, —CN, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, —OR35, —N(R24)(R25) or —SR35; R41 is alkyl, cycloalkyl, —SO2(alkyl), —C(O)-alkyl, —C(O)-cycloalkyl or -alkyl-NH—C(O)CH3; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating cognitive or neurodegenerative diseases with compounds of formula I. Also disclosed are pharmaceutical compositions and methods of treatment comprising compounds of formula I in combination with other agents useful in treating cognitive or neurodegenerative diseases.

摘要翻译： 公开了下式的新化合物或其药学上可接受的盐或溶剂化物，其中R 1是X是-O - ， - C（R 14）2 - 或-N（R） - ; Z是-C（R 14）2 - 或-N（R） - ; t为0,1,2或3; 每个R和R 2独立地是H，烷基，环烷基，环烷基烷基，芳基，杂芳基，杂环烷基，芳基烷基，杂芳基烷基，杂环烷基烷基，烯基或炔基; 每个R 14是H，烷基，烯基，炔基，卤素，-CN，卤代烷基，环烷基，环烷基烷基，芳基，杂芳基，杂环烷基，芳基烷基，杂芳基烷基，杂环烷基烷基，-OR 35，-N（R 24） ）（R 25）或-SR 35; R 41是烷基，环烷基，-SO 2（烷基），-C（O） - 烷基，-C（O） - 环烷基或 - 烷基-NH-C（O）CH 3; 其余变量如本说明书中所定义。 还公开了包含式I化合物的药物组合物和用式I化合物治疗认知障碍或神经变性疾病的方法。还公开了药物组合物和治疗方法，其包含式I化合物与用于治疗认知或神经变性的其它药剂 疾病

公开(公告)号：US20080058343A1

公开(公告)日：2008-03-06

申请号：US11776901

申请日：2007-07-12

申请人： Stuart Rosenblum ,  Joseph Kozlowski ,  Neng-Yang Shih ,  Brian McGuinness ,  Douglas Hobbs

发明人： Stuart Rosenblum ,  Joseph Kozlowski ,  Neng-Yang Shih ,  Brian McGuinness ,  Douglas Hobbs

IPC分类号： A61K31/497 ,  A61P25/00 ,  C07D401/02

CPC分类号： C07D401/14

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 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，溶剂合物或酯还公开了治疗趋化因子介导的疾病的方法，例如姑息治疗，治疗性治疗，某些疾病和疾病如炎性疾病的预防性治疗（非限制性实例） 包括牛皮癣），自身免疫疾病（非限制性实例包括类风湿性关节炎，多发性硬化症），移植物排斥（非限制性实例，包括同种异体移植物排斥，移植排斥），感染性疾病（例如，结节性麻风病 ），固定药物喷发，皮肤迟发型超敏反应，眼部炎症，I型糖尿病，病毒性脑膜炎和使用组合物的肿瘤 和式1。

公开(公告)号：US20070054925A1

公开(公告)日：2007-03-08

申请号：US11396079

申请日：2006-03-31

申请人： Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  Ronald Doll ,  Viyyoor Girijavallabhan ,  Alan Mallams ,  Carmen Alvarez ,  Kartik Keertikar ,  Jocelyn Rivera ,  Tin-Yau Chan ,  Vincent Madison ,  Thierry Fischmann ,  Lawrence Dillard ,  Vinh Tran ,  Zhen He ,  Ray James ,  Haengsoon Park ,  Vidyadhar Paradkar ,  Douglas Hobbs

发明人： Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  Ronald Doll ,  Viyyoor Girijavallabhan ,  Alan Mallams ,  Carmen Alvarez ,  Kartik Keertikar ,  Jocelyn Rivera ,  Tin-Yau Chan ,  Vincent Madison ,  Thierry Fischmann ,  Lawrence Dillard ,  Vinh Tran ,  Zhen He ,  Ray James ,  Haengsoon Park ,  Vidyadhar Paradkar ,  Douglas Hobbs

IPC分类号： A61K31/519 ,  C07D487/04

CPC分类号： C07D487/04 ,  A61K31/495

摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

公开(公告)号：US20070054906A1

公开(公告)日：2007-03-08

申请号：US11396001

申请日：2006-03-31

申请人： Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  Ronald Doll ,  Viyyoor Girijavallabhan ,  Alan Mallams ,  Carmen Alvarez ,  Kartik Keertikar ,  Jocelyn Rivera ,  Tin-Yau Chan ,  Vincent Madison ,  Thierry Fischmann ,  Lawrence Dillard ,  Vinh Tran ,  Zhen He ,  Ray James ,  Haengsoon Park ,  Vidyadhar Paradkar ,  Douglas Hobbs

发明人： Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  Ronald Doll ,  Viyyoor Girijavallabhan ,  Alan Mallams ,  Carmen Alvarez ,  Kartik Keertikar ,  Jocelyn Rivera ,  Tin-Yau Chan ,  Vincent Madison ,  Thierry Fischmann ,  Lawrence Dillard ,  Vinh Tran ,  Zhen He ,  Ray James ,  Haengsoon Park ,  Vidyadhar Paradkar ,  Douglas Hobbs

IPC分类号： A61K31/5377 ,  A61K31/519 ,  C07D487/04

CPC分类号： C07D487/04

摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

摘要翻译： 在其许多实施方案中，本发明提供了一类新颖的吡唑并[1,5-a]嘧啶化合物作为细胞周期蛋白依赖性激酶的抑制剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备药物制剂的方法 包括一种或多种这样的化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与CDK相关的一种或多种疾病的方法。

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。

公开(公告)号：US20080050384A1

公开(公告)日：2008-02-28

申请号：US11788847

申请日：2007-04-20

申请人： Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  Ronald Doll ,  Viyyoor Girijavallabhan ,  Alan Mallams ,  Carmen Alvarez ,  Kartik Keertikar ,  Jocelyn Rivera ,  Tin-Yau Chan ,  Vincent Madison ,  Thierry Fischmann ,  Lawrence Dillard ,  Vinh Tran ,  Zhenmin He ,  Ray James ,  Haengsoon Park ,  Vidyadhar Paradkar ,  Douglas Hobbs ,  Paul Kirschmeier ,  Rajat Bannerji

发明人： Timothy Guzi ,  Kamil Paruch ,  Michael Dwyer ,  Ronald Doll ,  Viyyoor Girijavallabhan ,  Alan Mallams ,  Carmen Alvarez ,  Kartik Keertikar ,  Jocelyn Rivera ,  Tin-Yau Chan ,  Vincent Madison ,  Thierry Fischmann ,  Lawrence Dillard ,  Vinh Tran ,  Zhenmin He ,  Ray James ,  Haengsoon Park ,  Vidyadhar Paradkar ,  Douglas Hobbs ,  Paul Kirschmeier ,  Rajat Bannerji

IPC分类号： A61K31/519 ,  A61K31/33 ,  A61K31/4965 ,  A61K31/56 ,  A61K31/675 ,  A61K33/24 ,  A61K38/46 ,  A61P19/02 ,  A61P35/00 ,  A61P43/00 ,  A61P29/00 ,  A61K39/395 ,  A61K33/36 ,  A61K31/7004 ,  A61K31/655 ,  A61K31/535 ,  A61K31/497

CPC分类号： A61K31/33 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/519 ,  A61K31/535 ,  A61K31/555 ,  A61K31/56 ,  A61K31/655 ,  A61K31/675 ,  A61K31/7004 ,  A61K33/24 ,  A61K45/06 ,  A61K2300/00

摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

摘要翻译： 在其许多实施方案中，本发明提供了一类新颖的吡唑并[1,5-a]嘧啶化合物作为细胞周期蛋白依赖性激酶的抑制剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备药物制剂的方法 包括一种或多种这样的化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与CDK相关的一种或多种疾病的方法。

公开(公告)号：US20070021611A1

公开(公告)日：2007-01-25

申请号：US11353697

申请日：2006-02-14

申请人： Brian McGuinness ,  Stuart Rosenblum ,  Joseph Kozlowski ,  Gopinadhan Anilkumar ,  Seong Kim ,  Neng-Yang Shih ,  Chung-Her Jenh ,  Paul Zavodny ,  Douglas Hobbs ,  Guizhen Dong ,  Yuefei Shao ,  Lisa Zawacki ,  Cangming Yang ,  Carolyn Carroll

发明人： Brian McGuinness ,  Stuart Rosenblum ,  Joseph Kozlowski ,  Gopinadhan Anilkumar ,  Seong Kim ,  Neng-Yang Shih ,  Chung-Her Jenh ,  Paul Zavodny ,  Douglas Hobbs ,  Guizhen Dong ,  Yuefei Shao ,  Lisa Zawacki ,  Cangming Yang ,  Carolyn Carroll

IPC分类号： C07D401/00

CPC分类号： C07D401/12 ,  C07D211/58 ,  C07D401/14 ,  C07D405/14 ,  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。