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1. 发明授权

US08183252B2 Heterocyclic aspartyl protease inhibitors 有权
公开(公告)号：US08183252B2
公开(公告)日：2012-05-22
申请号：US12693874
申请日：2010-01-26
申请人： Zhaoning Zhu , Zhong-Yue Sun , Andrew Stamford , William J. Greenlee , Jared N. Cumming , Lingyan Wang , Ulrich Iserloh , Xiaoxiang Liu , Ying Huang , Guoqing Li , Jianping Pan
发明人： Zhaoning Zhu , Zhong-Yue Sun , Andrew Stamford , William J. Greenlee , Jared N. Cumming , Lingyan Wang , Ulrich Iserloh , Xiaoxiang Liu , Ying Huang , Guoqing Li , Jianping Pan
IPC分类号： A01N43/54 , A61K31/505 , C07D239/02
CPC分类号： C07D233/88 , A61K31/4168 , A61K31/4178 , C07D239/22 , C07D401/06 , C07D401/10 , C07D403/06 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/10 , C07D417/14 , C07D495/10
摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(═S)—, —S(O)—, —S(O)2—, —C(═O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(═N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(═O)— or —C(═NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(═NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes.Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.

2. 发明授权

US08017616B2 Heterocyclic substituted pyridine compounds with CXCR3 antagonist activity 有权
标题翻译：具有CXCR3拮抗活性的杂环取代的吡啶化合物
公开(公告)号：US08017616B2
公开(公告)日：2011-09-13
申请号：US12642931
申请日：2009-12-21
申请人： Stuart B. Rosenblum , Joseph A. Kozlowski , Neng-Yang Shih , Brian F. McGuinness , Douglas W. Hobbs
发明人： Stuart B. Rosenblum , Joseph A. Kozlowski , Neng-Yang Shih , Brian F. McGuinness , Douglas W. Hobbs
IPC分类号： A61K31/496 , C07D413/14
CPC分类号： C07D401/14 , 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. 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。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。

3. 发明申请

US20080058343A1 HETEROCYCLIC SUBSTITUTED PIPERAZINE COMPOUNDS WITH CXCR3 ANTAGONIST ACTIVITY 有权
标题翻译：具有CXCR3拮抗剂活性的杂环取代的哌嗪化合物
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。

4. 发明申请

US20070054925A1 Novel pyrazolopyrimidines as cyclin dependent kinase inhibitors 审中-公开
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.

5. 发明申请

US20070054906A1 Novel pyrazolopyrimidines as cyclin dependent kinase inhibitors 有权
标题翻译：新型吡唑并嘧啶作为细胞周期蛋白依赖性激酶抑制剂
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。

6. 发明申请

US20040209878A1 Novel pyrazolopyrimidines as cyclin dependent kinase inhibitors 有权
公开(公告)号：US20040209878A1
公开(公告)日：2004-10-21
申请号：US10776988
申请日：2004-02-11
申请人： Schering Corporation and Pharmacopeia, Inc.
发明人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Alan Mallams , Carmen S. Alvarez , Kartik M. Keertikar , Jocelyn Rivera , Tin-Yau Chan , Vincent Madison , Thierry O. Fischmann , Lawrence W. Dillard , Vinh D. Tran , Zhen Min He , Ray Anthony James , Haengsoon Park , Vidyadhar M. Paradkar , Douglas Walsh Hobbs
IPC分类号： A61K031/5377 , A61K031/519 , C07D487/04
CPC分类号： C07D487/04 , A61K31/495
摘要： In its many embodiments, the present invention provides a novel class of pyrazolonull1,5-anullpyrimidine 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.

7. 发明申请

US20040186142A1 Thiadiazoledioxides and thiadiazoleoxides as CXC- and CC- chemokine receptor ligands 审中-公开
标题翻译：噻二唑二氧化物和噻二唑氧化物作为CXC-和CC-趋化因子受体配体
公开(公告)号：US20040186142A1
公开(公告)日：2004-09-23
申请号：US10680393
申请日：2003-10-07
申请人： Schering Corporation Pharmacopeia, Inc.
发明人： Arthur G. Taveras , Jianhua Chao , Purakkattle J. Biju , Younong Yu , Jay S. Fine , William Hipkin , Cynthia J. Aki , J. Robert Merritt , Ge Li , John J. Baldwin , Gaifa Lai , Minglang Wu , Evan A. Hecker
IPC分类号： A61K031/4439 , A61K031/433 , C07D417/02
CPC分类号： C07D285/10 , C07D417/02 , C07D417/12 , C07D417/14
摘要： Disclosed are novel compounds of the formula: 1 and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, acute pain, acute and chronic inflammatory pain, and neuropathic pain using a compound of formula IA.
摘要翻译：公开了下式的新化合物及其药学上可接受的盐和溶剂合物。包含取代基A的基团的实例包括杂芳基，芳基，杂环烷基，环烷基，芳基，炔基，烯基，氨基烷基，烷基或氨基。包含取代基B的基团的实例包括芳基和杂芳基。还公开了治疗趋化因子介导的疾病如癌症，血管生成，血管生成性眼病，肺部疾病，多发性硬化，类风湿性关节炎，骨关节炎，中风和心脏再灌注损伤，急性疼痛，急性和慢性炎症性疼痛的方法使用式IA化合物的神经性疼痛。

8. 发明申请

US20040102452A1 Novel pyrazolopyrimidines as cyclin dependent kinase inhibitors 失效
公开(公告)号：US20040102452A1
公开(公告)日：2004-05-27
申请号：US10654163
申请日：2003-09-03
申请人： Schering Corporation and Pharmacopeia, Inc.
发明人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Chad Knutson , Brian McKittrick , Lawrence W. Dillard , Vinh D. Tran , Zhen Min He , Ray Anthony James , Haengsoon Park
IPC分类号： A61K031/519 , C07D487/02
CPC分类号： C07D487/04
摘要： In its many embodiments, the present invention provides a novel class of pyrazolonull1,5-anullpyrimidine 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.

9. 发明授权

US5976807A Eukaryotic cells stably expressing genes from multiple transfected episomes 失效
标题翻译：真核细胞稳定地表达来自多个转染的附加体的基因
公开(公告)号：US5976807A
公开(公告)日：1999-11-02
申请号：US130114
申请日：1998-08-06
申请人： Robert A. Horlick , Bassam B. Damaj , Alan K. Robbins
发明人： Robert A. Horlick , Bassam B. Damaj , Alan K. Robbins
IPC分类号： G01N33/50 , C07K14/705 , C12N5/10 , C12N15/09 , C12N15/10 , C12Q1/02 , G01N33/15 , C12Q1/68
CPC分类号： C12N15/10
摘要： A method is described for producing recombinant eukaryotic cell lines expressing multiple proteins of interest. Eukaryotic host cells are transfected with (a) a first episome which contains an EBV origin of replication and a first gene encoding a protein of interest; and (b) a second episome containing an EBV origin of replication and a second gene encoding a protein of interest. Transfected cells are obtained expressing an EBNA 1 protein. The cells are grown under conditions wherein the episomes express the first and second genes.
摘要翻译：描述了用于产生表达多种目的蛋白质的重组真核细胞系的方法。用（a）含有EBV复制起点的第一个附加物和编码目的蛋白质的第一个基因转染真核宿主细胞; 和（b）含有EBV复制起点的第二次附加组合和编码目的蛋白质的第二个基因。获得表达EBNA1蛋白的转染细胞。细胞在其中附加体表达第一和第二基因的条件下生长。

10. 发明授权

US5962506A Glycol and hydroxyphosphonate peptidomimetics as inhibitors of aspartyl proteases 失效
标题翻译：乙二醇和羟基膦酸酯肽模拟物作为天冬氨酰蛋白酶的抑制剂
公开(公告)号：US5962506A
公开(公告)日：1999-10-05
申请号：US888957
申请日：1997-07-07
申请人： Carolyn DiIanni Carroll , Roland Ellwood Dolle, III , Yvonne Class Shimshock , Timothee Felix Herpin
发明人： Carolyn DiIanni Carroll , Roland Ellwood Dolle, III , Yvonne Class Shimshock , Timothee Felix Herpin
IPC分类号： A61K38/00 , C07C237/22 , C07C271/22 , C07C271/28 , C07C311/18 , C07D207/14 , C07D217/06 , C07F9/40 , C07F9/60 , C07K5/02 , C08F8/30 , C08F8/40 , C07D207/10 , A61K31/40
CPC分类号： C07C237/22 , C07C271/22 , C07C271/28 , C07C311/18 , C07D207/14 , C07D217/06 , C07F9/4006 , C07F9/4056 , C07F9/60 , C07K5/0205 , A61K38/00 , C07B2200/07
摘要： Compounds of Formula I ##STR1## are disclosed as inhibitors having activity against the aspartyl proteases, plasmepsin and cathepsin D. The compounds are therefore useful for treatment of diseases such as malaria and Alzheimer's disease. In preferred compounds of Formula I, Y is an dialkoxyphosphonate, or .alpha.-hydroxyamide group and Z is an acyl or .alpha.-ketocarbamate functionality. Intermediates in the solid phase synthesis of compounds of Formula I, in which compounds are attached to a solid support, are also disclosed.
摘要翻译：公开了式I化合物作为具有针对天冬氨酰蛋白酶，质膜蛋白酶和组织蛋白酶D的活性的抑制剂。因此，该化合物可用于治疗疾病如疟疾和阿尔茨海默氏病。在优选的式I化合物中，Y是二烷氧基膦酸酯或α-羟基酰胺基团，Z是酰基或α-酮酸氨基甲酸酯官能团。还公开了其中化合物连接到固体支持物的式I化合物的固相合成中的中间体。

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