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    Alpha-methylbenzyl-containing thiourea inhibitors of herpes viruses containing a phenylenediamine group
    1.
    发明授权
    Alpha-methylbenzyl-containing thiourea inhibitors of herpes viruses containing a phenylenediamine group 失效
    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。

    Synthesis of inhibitors of calmodulin-mediated enzymes including KS-501, KS-502 and their enantiomers
    6.
    发明授权
    Synthesis of inhibitors of calmodulin-mediated enzymes including KS-501, KS-502 and their enantiomers 失效
    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。

    ENGINEERED POLYPEPTIDE CONJUGATES AND METHODS FOR MAKING THEREOF USING TRANSGLUTAMINASE
    7.
    发明申请
    ENGINEERED POLYPEPTIDE CONJUGATES AND METHODS FOR MAKING THEREOF USING TRANSGLUTAMINASE 审中-公开
    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。

    Heterocyclic carboxamide-containing thiourea inhibitors of herpes viruses containing a substituted phenylenediamine group
    8.
    发明授权
    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.

    Aminopyridine-containing thiourea inhibitors of herpes viruses
    10.
    发明授权
    Aminopyridine-containing thiourea inhibitors of herpes viruses 失效
    含有氨基吡啶的疱疹病毒的硫脲抑制剂

    公开(公告)号：US06262090B1

    公开(公告)日：2001-07-17

    申请号：US09444896

    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： A61K3144

    CPC分类号： C07D333/02 ,  C07D207/34 ,  C07D211/72 ,  C07D213/44 ,  C07D235/26 ,  C07D307/02

    摘要： Compounds of the formula wherein A is heteroaryl; 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; W is O, NR6, or is absent; G is aryl or heteroaryl; and X is a bond 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; and 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; or a pharmaceutical acceptable salt thereof, 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： 式Ⅳa的化合物是杂芳基; R 9 -R 12独立地是氢，1至4个碳原子的烷基，1至4个碳原子的全卤代烷基，卤素，1至4个碳原子的烷氧基或氰基，或R 9和R 10或R 11和 R 12可以一起形成5至7个碳原子的芳基; W是O，NR 6或不存在; G是芳基或杂芳基; X为键，X为碳原子数为1〜6的烷基，碳原子数为1〜6的烯基，碳原子数为1〜6的烷氧基，碳原子数为1〜6的硫代烷基，碳原子数为1〜6的烷基氨基 原子或（CH）J; 且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; 或其药学上可接受的盐，其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。