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1. 发明授权

US06462055B2 Alpha-methylbenzyl-containing thiourea inhibitors of herpes viruses containing a phenylenediamine group 失效
标题翻译：含α-甲基苄基的含有苯二胺基团的疱疹病毒的硫脲抑制剂
公开(公告)号：US06462055B2
公开(公告)日：2002-10-08
申请号：US09845428
申请日：2001-04-30
申请人： Jonathan Bloom , Kevin Curran , Martin DiGrandi , Russell Dushin , Stanley Lang , Emily Norton , Adma Ross , Bryan O'Hara
发明人： Jonathan Bloom , Kevin Curran , Martin DiGrandi , Russell Dushin , Stanley Lang , Emily Norton , Adma Ross , Bryan O'Hara
IPC分类号： A61K3147
CPC分类号： C07D211/96 , C07C335/20
摘要： Compounds having the formula: wherein R1-R5 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon members, aryl, heteroaryl, halogen, —CN, —NO2, —CO2R6, —COR6, —OR6, —SR6, —SOR6, —SO2R6, —CONR7R8, —NR6N(R7R8), —N(R7R8) or W-Y-(CH2)n-Z provided that at least one of R1-R5 is not hydrogen; or R1 and R2 or R3 and R4, taken together form a 3 to 7 membered heterocycloalkyl or 3 to 7 membered heteroaryl; R6 and R7 are independently hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, or aryl; R8 is hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 members, aryl or heteroaryl, or R7 and R8, taken together may form a 3 to 7 membered heterocycloalkyl; W is O, NR6, or is absent; Y is —(CO)— or —(CO2)—, or is absent; Z is alkyl of 1 to 4 carbon atoms, —CN, —CO2R6, COR6, —CONR7R8, —OCOR6, —NR6COR7, —OCONR6, —OR6, —SR6, —SOR6, —SO2R6, SR6N(R7R8), —N(R7R8) or phenyl; G is aryl or fused bicyclic heteroaryl; X is a bond, —NH, alkyl of 1 to 6 carbon atoms, alkenyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, thioalkyl of 1 to 6 carbon atoms, alkylamino of 1 to 6 carbon atoms, or (CH)J; J is alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, phenyl or benzyl; and n is an integer from 1 to 6; useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpesvirus.
摘要翻译：具有下式的化合物：其中R 1 -R 5独立地选自氢，1至6个碳原子的烷基，2至6个碳原子的烯基，2至6个碳原子的炔基，1至6个碳原子的全卤代烷基，3至 3至10个碳原子的杂环烷基，芳基，杂芳基，卤素，-CN，-NO 2，-CO 2 R 6，-COR 6，-OR 6，-SR 6，-SOR 6，-SO 2 R 6，-CONR 7 R 8，-NR 6 N（R 7 R 8），-N（R 7 R 8）或WY-（CH 2）n Z，条件是R 1 -R 5中的至少一个不是氢; 或R 1和R 2或R 3和R 4一起形成3至7元杂环烷基或3至7元杂芳基; R 6和R 7独立地为氢，1至6个碳原子的烷基，1至6个碳原子的全卤代烷基或芳基 ; R 8为氢，1至6个碳原子的烷基，1至6个碳原子的全卤烷基，3至10个碳原子的环烷基，3至10个成员的杂环烷基，芳基或杂芳基，或R 7和R 8一起可以形成3 至7元杂环烷基; W为O，NR 6或不存在; Y为 - （CO） - 或 - （CO 2） - 或不存在; Z为1至4个碳原子的烷基，-CN，-CO 2 R 6，COR 6 ，-CONR7R8，-OCOR6，-NR6COR7，-OCONR6，-OR6，-SR6，-SOR6，-SO2R6，SR6N（R7R8），-N（R7R8）或苯基; G是芳基或稠合双环杂芳基; X是键，-NH，1至6个碳原子的烷基，1至6个碳原子的烯基，1至6个碳原子的烷氧基，1至6个碳原子的硫代烷基，1至6个碳原子的烷基氨基或（CH） J为1至6个碳原子的烷基，3至7个碳原子的环烷基，苯基或苄基; andn是1〜6的整数; 可用于治疗与疱疹病毒相关的疾病，包括人巨细胞病毒，单纯疱疹病毒，爱泼斯坦 - 巴尔病毒，水痘带状疱疹病毒，人疱疹病毒-6和-7以及卡波西疱疹病毒。

2. 发明授权

US06426355B1 Heterocyclic carboxamide-containing thiourea inhibitors of herpes viruses containing phenylenediamine group 失效
标题翻译：含有苯二胺的疱疹病毒含杂环酰胺的硫脲抑制剂
公开(公告)号：US06426355B1
公开(公告)日：2002-07-30
申请号：US09671486
申请日：2000-09-27
申请人： Jonathan Bloom , Kevin Curran , Martin DiGrandi , Russell Dushin , Thomas Jones , Stanley Lang , Adma Ross , Eugene A. Terefenko , Bryan O'Hara
发明人： Jonathan Bloom , Kevin Curran , Martin DiGrandi , Russell Dushin , Thomas Jones , Stanley Lang , Adma Ross , Eugene A. Terefenko , Bryan O'Hara
IPC分类号： A61K31433
CPC分类号： C07D277/56 , C07D285/06 , C07D417/12
摘要： Compounds having the formula: wherein R1-R5, X and G are described herein and which are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpesvirus.
摘要翻译：具有下式的化合物：其中R1-R5，X和G在本文中描述并且可用于治疗与疱疹病毒相关的疾病，包括人巨细胞病毒，单纯疱疹病毒，爱泼斯坦 - 巴尔病毒，水痘带状疱疹病毒，人疱疹病毒 - 6和-7，以及卡波西疱疹病毒。

3. 发明授权

US06403617B1 Diaminopyridine-containing thiourea inhibitors of herpes viruses 失效
标题翻译：含二氨基吡啶的疱疹病毒的硫脲抑制剂
公开(公告)号：US06403617B1
公开(公告)日：2002-06-11
申请号：US09669535
申请日：2000-09-26
申请人： Jonathan Bloom , Martin DiGrandi , Russell Dushin , Stanley Lang , Bryan O'Hara
发明人： Jonathan Bloom , Martin DiGrandi , Russell Dushin , Stanley Lang , Bryan O'Hara
IPC分类号： A61K3144
CPC分类号： C07D213/75 , C07D213/81 , C07D405/12 , C07D417/12
摘要： Compounds of the formula Useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, humanherpesviruses-6 and -7, and Kaposi herpesvirus.
摘要翻译：用于治疗与疱疹病毒相关疾病（包括人巨细胞病毒，单纯疱疹病毒，爱泼斯坦 - 巴尔病毒，水痘带状疱疹病毒，人类疱疹病毒-6和-7）以及卡波西疱疹病毒的化合物。

4. 发明专利

IL268245D0 Calicheamicin derivatives and antibody drug conjugates thereof 未知
公开(公告)号：IL268245D0
公开(公告)日：2019-09-26
申请号：IL26824519
申请日：2019-07-24
申请人： PFIZER , OMAR KHALED AHMAD , STEPHEN PAUL BROWN , KENNETH JOHN DIRICO , RUSSELL DUSHIN , GARY FREDERICK FILZEN , SUJIET PUTHENVEETIL , PAVEL STROP , CHAKRAPANI SUBRAMANYAM , LAWRENCE N TUMEY
发明人： OMAR KHALED AHMAD , STEPHEN PAUL BROWN , KENNETH JOHN DIRICO , RUSSELL DUSHIN , GARY FREDERICK FILZEN , SUJIET PUTHENVEETIL , PAVEL STROP , CHAKRAPANI SUBRAMANYAM , LAWRENCE N TUMEY
IPC分类号： A61K20060101
摘要： The present invention is directed to novel calicheamicin derivatives useful as payloads in antibody-drug-conjugates (ADC's), and to payload-linker compounds and ADC compounds comprising the same; to pharmaceutical compositions comprising the same and to methods for using the same to treat pathological conditions such as cancer.

5. 发明申请

US20070299092A1 Quinone Substituted Quinazoline and Quinoline Kinase Inhibitors 审中-公开
标题翻译：喹诺酮取代喹唑啉和喹啉激酶抑制剂
公开(公告)号：US20070299092A1
公开(公告)日：2007-12-27
申请号：US11569306
申请日：2005-05-11
申请人： Middleton Floyd Jr , Thomas Nittoli , Allan Wissner , Russell Dushin , Ramaswamy Nilakantan , Charles Ingalls , Heidi Fraser , Bernard Johnson
发明人： Middleton Floyd Jr , Thomas Nittoli , Allan Wissner , Russell Dushin , Ramaswamy Nilakantan , Charles Ingalls , Heidi Fraser , Bernard Johnson
IPC分类号： C07D239/72 , A61K31/517 , A61P19/02 , A61P27/00 , C12N9/99 , A61P3/00 , A61P35/00 , A61P9/00
CPC分类号： C07D239/94 , C07D215/42 , C07D215/54 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D487/08
摘要： The present invention provides for compounds with the general formula: A compound of formula (1) having the structure (1) wherein Z is a radical selected from the group (a), (b), or (c) as well as methods and compositions containing these compounds useful for treatment of diseases that are characterized, at least in part, by excessive, abnormal, or inappropriate angiogenesis. These disease states, include but are not limited to, cancer, diabetic retinopathy, macular degeneration and rheumatoid arthritis. These compounds inhibit angiogenesis by inhibiting a tyrosine kinase receptor enzyme, specifically KDR, and binding to the KDR in an irreversible manner.
摘要翻译：本发明提供具有以下通式的化合物：具有结构（1）的式（1）化合物，其中Z是选自（a），（b）或（c）的基团，以及方法和含有这些化合物的组合物可用于治疗至少部分由过度，异常或不合适的血管生成表征的疾病。这些疾病状态包括但不限于癌症，糖尿病性视网膜病变，黄斑变性和类风湿性关节炎。这些化合物通过抑制酪氨酸激酶受体酶，特别是KDR，并以不可逆的方式结合KDR来抑制血管生成。

6. 发明授权

US06410571B1 Heterocyclic carboxamide-containing thiourea inhibitors of herpes viruses containing a substituted phenylenediamine group 失效
标题翻译：含有取代苯二胺基团的含有杂环羧酰胺的疱疹病毒的硫脲抑制剂
公开(公告)号：US06410571B1
公开(公告)日：2002-06-25
申请号：US09684773
申请日：2000-12-29
申请人： Jonathan Bloom , Kevin Curran , Martin DiGrandi , Russell Dushin , Thomas Jones , Stanley Lang , Adma Ross , Eugene A. Terefenko , Bryan O'Hara
发明人： Jonathan Bloom , Kevin Curran , Martin DiGrandi , Russell Dushin , Thomas Jones , Stanley Lang , Adma Ross , Eugene A. Terefenko , Bryan O'Hara
IPC分类号： A61K3144
CPC分类号： C07D213/75 , C07D213/81 , C07D405/12 , C07D417/12
摘要： Compounds of the formula: wherein the substituents are defined herein which are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpesvirus.
摘要翻译：下式的化合物：其中本文定义的取代基可用于治疗与疱疹病毒有关的疾病，包括人巨细胞病毒，单纯疱疹病毒，爱泼斯坦 - 巴尔病毒，水痘带状疱疹病毒，人疱疹病毒-6和-7，以及卡波西疱疹病毒

7. 发明授权

US5386019A Synthesis of inhibitors of calmodulin-mediated enzymes including KS-501, KS-502 and their enantiomers 失效
标题翻译：钙调蛋白介导的酶抑制剂的合成，包括KS-501，KS-502及其对映异构体
公开(公告)号：US5386019A
公开(公告)日：1995-01-31
申请号：US821719
申请日：1992-01-15
申请人： Samuel J. Danishefsky , Russell Dushin , William N. Hait
发明人： Samuel J. Danishefsky , Russell Dushin , William N. Hait
IPC分类号： C07H15/203 , C07H1/00 , C07H13/02
CPC分类号： C07H15/203
摘要： The total synthesis of a group of compounds with inhibitory effects on calmodulin-mediated enzyme activities has been accomplished. Among these synthesized compounds are KS-501 and KS-502. Other compounds that have been synthesized by the described scheme are ent-KS-501 and ent-KS-502 which are enantiomers of KS-501 and KS-502 and which also have inhibitory effects on calmodulin-mediated enzyme activities.
摘要翻译：已经完成了对钙调蛋白介导的酶活性具有抑制作用的一组化合物的总合成。其中合成的化合物有KS-501和KS-502。通过所述方案合成的其它化合物是KS-501和KS-502的对映体的ent-KS-501和ent-KS-502，其也对钙调蛋白介导的酶活性具有抑制作用。

8. 发明申请

US20130230543A1 ENGINEERED POLYPEPTIDE CONJUGATES AND METHODS FOR MAKING THEREOF USING TRANSGLUTAMINASE 审中-公开
标题翻译：工程聚氨酯共聚物及其制备方法使用转氨酶
公开(公告)号：US20130230543A1
公开(公告)日：2013-09-05
申请号：US13883535
申请日：2011-11-03
申请人： Jaume Pons , Arvind Rajpal , Pavel Strop , Magdalena Grazyna Dorywalska , David Shelton , Shu-Hui Liu , Russell Dushin
发明人： Jaume Pons , Arvind Rajpal , Pavel Strop , Magdalena Grazyna Dorywalska , David Shelton , Shu-Hui Liu , Russell Dushin
IPC分类号： C07K17/02
CPC分类号： C07K17/02 , A61K47/48369 , A61K47/48384 , A61K47/48569 , A61K47/48715 , A61K47/68 , A61K47/6803 , A61K47/6851 , A61K47/6889 , C07K16/30 , C07K2317/31 , C07K2317/73
摘要： The present invention provides engineered polypeptide conjugates (e.g., antibody-drug-conjugates, toxin-(biocompatible polymer) conjugates, antibody-(biocompatible polymer) conjugates, and bispecific antibodies) comprising acyl donor glutamine-containing tags and amine donor agents. In one aspect, the invention provides an engineered Fc-containing polypeptide conjugate comprising the formula (Fc-containing polypeptide)-T-A, wherein T is an acyl donor glutamine-containing tag engineered at a specific site or comprises an endogenous glutamine made reactive by the Fc-containing polypeptide engineering, wherein A is an amine donor agent, and wherein the amine donor agent is site-specifically conjugated to the acyl donor glutamine-containing tag or the endogenous glutamine. The invention also provides methods of making engineered polypeptide conjugates using transglutaminase.
摘要翻译：本发明提供包含酰基供体谷氨酰胺标签和胺供体试剂的工程改造的多肽缀合物（例如，抗体 - 药物偶联物，毒素 - （生物相容性聚合物）缀合物，抗体 - （生物相容性聚合物）缀合物和双特异性抗体）。一方面，本发明提供了包含式（Fc-含多肽）-TA的工程改造的含Fc多肽缀合物，其中T是在特定位点工程化的含酰基供体谷氨酰胺标签，或包含由 Fc多肽工程，其中A是胺供体试剂，其中胺供体试剂与含酰基供体谷氨酰胺的标签或内源性谷氨酰胺位点特异性结合。本发明还提供了使用转谷氨酰胺酶制备工程化多肽缀合物的方法。

9. 发明授权

US06407249B1 Heterocyclic carboxamide-containing thiourea inhibitors of herpes viruses containing a substituted phenylenediamine group 失效
公开(公告)号：US06407249B1
公开(公告)日：2002-06-18
申请号：US09684011
申请日：2000-12-29
申请人： Jonathan Bloom , Kevin Curran , Martin DiGrandi , Russell Dushin , Thomas Jones , Stanley Lang , Adma Ross , Eugene A. Terefenko , Bryan O'Hara
发明人： Jonathan Bloom , Kevin Curran , Martin DiGrandi , Russell Dushin , Thomas Jones , Stanley Lang , Adma Ross , Eugene A. Terefenko , Bryan O'Hara
IPC分类号： A61K31341
CPC分类号： C07D213/75 , C07D213/81 , C07D405/12 , C07D417/12
摘要： Compounds of the formula: wherein R1-R5 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon members, aryl, heteroaryl, halogen, —CN, —NO2, —CO2R6, —COR6, —OR6, —SR6, —SOR6, —SO2R6, —CONR7R8, —NR6N(R7R8), —N(R7R8) or W—Y—(CH2)n—Z provided that at least one of R1-R5 is not hydrogen; or R2 and R3 or R3 and R4, taken together form a 3 to 7 membered heterocycloalkyl or 3 to 7 membered heteroaryl; R6 and R7 are independently hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, or aryl; R8 is hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 members, aryl or heteroaryl, or R7 and R8, taken together may form a 3 to 7 membered heterocycloalkyl; R9-R12 are independently hydrogen, alkyl of 1 to 4 carbon atoms, perhaloalkyl of 1 to 4 carbon atoms, halogen, alkoxy of 1 to 4 carbon atoms, or cyano, or R9 and R10 or R11 and R12 may be taken together to form aryl of 5 to 7 carbon atoms; provided that at least one of R9-12 is not hydrogen; W is O, NR6, or is absent; Y is —(CO)— or —(CO2)—, or is absent; Z is alkyl of 1 to 4 carbon atoms, —CN, —CO2R6, COR6, —CONR7R8, —OCOR6, —NR6COR7, —OCONR6, —OR6, —SR6, —SOR6, —SO2R6, SR6N(R7R8), —N(R7R3R) or phenyl; G is a monocyclic heteroaryl; X is a bond, —NH, alkyl of 1 to 6 carbon atoms, alkenyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, or thioalkyl of 1 to 6 carbon atoms, alkylamino of 1 to 6 carbon atoms, or (CH)J; J is alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, phenyl or benzyl; and n is an integer from 1 to 6 useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpesvirus.

10. 发明授权

US06335350B1 Acetamide and substituted acetamide-containing thiourea inhibitors of herpes viruses 失效
标题翻译：乙酰胺和取代乙酰胺的硫脲抑制剂的疱疹病毒
公开(公告)号：US06335350B1
公开(公告)日：2002-01-01
申请号：US09447005
申请日：1999-11-22
申请人： Jonathan Bloom , Martin DiGrandi , Russell Dushin , Stanley Lang , Bryan O'Hara
发明人： Jonathan Bloom , Martin DiGrandi , Russell Dushin , Stanley Lang , Bryan O'Hara
IPC分类号： C07D21126
CPC分类号： C07D213/75 , C07C335/20 , C07D207/456 , C07D209/42 , C07D215/16 , C07D217/12 , C07D241/24 , C07D249/04 , C07D261/18 , C07D277/56 , C07D285/06 , C07D307/84 , C07D333/38
摘要： Compounds of the formula: are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpesvirus.
摘要翻译：下式的化合物可用于治疗与疱疹病毒相关的疾病，包括人巨细胞病毒，单纯疱疹病毒，爱泼斯坦 - 巴尔病毒，水痘带状疱疹病毒，人疱疹病毒-6和-7以及卡波西疱疹病毒。

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