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1. 发明申请

US20130225637A1 ISATIN DERIVATIVES, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USE THEREOF 有权
标题翻译： ISATIN衍生物，其药物组合物及其使用方法
公开(公告)号：US20130225637A1
公开(公告)日：2013-08-29
申请号：US13776374
申请日：2013-02-25
申请人： David A. Horne , Richard Jove , Christopher Lincoln , Sangkil Nam , Larry Overman , Jun Xie
发明人： David A. Horne , Richard Jove , Christopher Lincoln , Sangkil Nam , Larry Overman , Jun Xie
IPC分类号： C07D209/38 , C07D401/10
CPC分类号： C07D209/38 , C07D401/04 , C07D401/10
摘要： One aspect of the invention relates to novel isatin derivative compounds and the pharmaceutical composition thereof. Another aspect of the invention relates to methods of using the isatin derivative compounds disclosed herein and the pharmaceutical compositions thereof. In certain embodiments, the method is used to treat a cancer or a tumor in a subject including, without limitation, prostate cancer, melanoma, pancreatic cancer, ovarian cancer, and lymphoma. In certain embodiment, the method is used to treat a condition in a subject that can be regulated by the activation of one or more proteins such as EGFR, Erk1/2, Her2/Neu, Jak2, Src, Stat3, Akt, Cyclin B1, and Cdc25C. In certain embodiment, the method is used to treat a condition in a subject that can be regulated by the disruption of microtubule formations.
摘要翻译：本发明的一个方面涉及新颖的靛红衍生物化合物及其药物组合物。本发明的另一方面涉及使用本文公开的靛红衍生物化合物及其药物组合物的方法。在某些实施方案中，该方法用于治疗受试者中的癌症或肿瘤，包括但不限于前列腺癌，黑素瘤，胰腺癌，卵巢癌和淋巴瘤。在某些实施方案中，该方法用于治疗可以通过激活一种或多种蛋白质如EGFR，Erk1 / 2，Her2 / Neu，Jak2，Src，Stat3，Akt，细胞周期蛋白B1，和Cdc25C。在某些实施方案中，该方法用于治疗可受微管形成中断的受试者的状况。

2. 发明授权

US07615638B2 Synthesis of grossularines-1 and analogs thereof and method of use 有权
标题翻译：粗略-1及其类似物的合成及其使用方法
公开(公告)号：US07615638B2
公开(公告)日：2009-11-10
申请号：US11742383
申请日：2007-04-30
申请人： David A. Horne , Richard Jove , Sangkil Nam , Kenichi Yakushijin , Fumiko Y. Yakushijin
发明人： David A. Horne , Richard Jove , Sangkil Nam , Kenichi Yakushijin , Fumiko Y. Yakushijin
IPC分类号： C07D471/22 , C07D487/22
CPC分类号： C07D471/14
摘要： In one embodiment of the present invention, a synthesis of grossularine-1 and N,N-didesmethylgrossularine-1 2 and analogs thereof based on a novel oxidative dimerization-electrocyclization sequence of 2-amino-4-(3-indolyl)imidazoles derived from oxotryptamine 3 is described.
摘要翻译：在本发明的一个实施方案中，基于由2-氨基-4-（3-吲哚基）咪唑衍生的新的氧化二聚化 - 电循环序列，合成粗略1和N，N-二甲基十八烷基-1,2及其类似物描述了氧杂色胺3。

3. 发明授权

US08962804B2 Meditopes and meditope-binding antibodies and uses thereof 有权
标题翻译：凝胶和沉默结合抗体及其用途
公开(公告)号：US08962804B2
公开(公告)日：2015-02-24
申请号：US13443804
申请日：2012-04-10
申请人： John C. Williams , David A. Horne , Yuelong Ma , Heng Wei Chang , Joshua Michael Donaldson , Cindy Zer , Krzysztof Bzymek , Kendra Nicole Avery , Jun Xie
发明人： John C. Williams , David A. Horne , Yuelong Ma , Heng Wei Chang , Joshua Michael Donaldson , Cindy Zer , Krzysztof Bzymek , Kendra Nicole Avery , Jun Xie
IPC分类号： C07K16/00 , C12P21/08 , C07K1/00 , C07K17/00 , A61K47/48 , C07K16/28 , C07K16/32
CPC分类号： A61K47/6811 , A61K47/66 , A61K47/6813 , A61K47/6851 , A61K47/6877 , A61K47/6897 , A61K51/1087 , B82Y5/00 , C07K16/18 , C07K16/2863 , C07K16/32 , C07K2299/00 , C07K2317/34 , C07K2317/40 , C07K2317/55 , C07K2317/567 , C07K2317/622 , C07K2317/92
摘要： Antibodies and meditopes that bind to the antibodies are provided, as well as complexes, compositions and combinations containing the meditopes and antibodies, and methods of producing, using, testing, and screening the same, including therapeutic and diagnostic methods and uses.
摘要翻译：提供了与抗体结合的抗体和沉默剂，以及包含中间体和抗体的复合物，组合物和组合，以及生产，使用，测试和筛选其中的方法，包括治疗和诊断方法和用途。

4. 发明申请

US20120301400A1 MEDITOPES AND MEDITOPE-BINDING ANTIBODIES AND USES THEREOF 有权
标题翻译： MED ES。。。。。。。。。。。。。。。。。。
公开(公告)号：US20120301400A1
公开(公告)日：2012-11-29
申请号：US13443804
申请日：2012-04-10
申请人： John C. Williams , David A. Horne , Yuelong Ma , Heng Wei Chang , Joshua Michael Donaldson , Cindy Zer , Krzysztof Bzymek , Kendra Nicole Avery , Jun Xie
发明人： John C. Williams , David A. Horne , Yuelong Ma , Heng Wei Chang , Joshua Michael Donaldson , Cindy Zer , Krzysztof Bzymek , Kendra Nicole Avery , Jun Xie
IPC分类号： C07K16/18 , C07K7/08 , C07K1/14 , A61K39/395 , A61K49/00 , C12N5/071 , C07K7/06 , C07K2/00
CPC分类号： A61K47/6811 , A61K47/66 , A61K47/6813 , A61K47/6851 , A61K47/6877 , A61K47/6897 , A61K51/1087 , B82Y5/00 , C07K16/18 , C07K16/2863 , C07K16/32 , C07K2299/00 , C07K2317/34 , C07K2317/40 , C07K2317/55 , C07K2317/567 , C07K2317/622 , C07K2317/92
摘要： Antibodies and meditopes that bind to the antibodies are provided, as well as complexes, compositions and combinations containing the meditopes and antibodies, and methods of producing, using, testing, and screening the same, including therapeutic and diagnostic methods and uses.
摘要翻译：提供了与抗体结合的抗体和沉默剂，以及包含中间体和抗体的复合物，组合物和组合，以及生产，使用，测试和筛选其中的方法，包括治疗和诊断方法和用途。

5. 发明申请

US20120177568A1 NOVEL MEDITOPES AND RELATED MEDITOPE-MONOCLONAL ANTIBODY DELIVERY SYSTEMS, SYNTHESIS AND THERAPEUTIC USES THEREOF 有权
标题翻译：新型药物和相关药物 - 单克隆抗体递送系统，其合成和治疗用途
公开(公告)号：US20120177568A1
公开(公告)日：2012-07-12
申请号：US13270207
申请日：2011-10-10
申请人： John C. WILLIAMS , David A. Horne , Yuelong Ma , Heng Wei Chen
发明人： John C. WILLIAMS , David A. Horne , Yuelong Ma , Heng Wei Chen
IPC分类号： A61K51/10 , C07K7/08 , C07K19/00 , C12N9/96 , C07K16/44 , A61K39/395 , A61K49/00 , C12N5/09 , C07K7/06 , A61P37/02 , A61P39/04 , C07K4/00 , C07K1/14 , B82Y5/00
CPC分类号： C07K16/2863 , A61K47/66 , A61K47/6851 , A61K47/6897 , B82Y5/00 , C07K7/64 , C07K16/32 , C07K16/44 , C07K2317/34 , C07K2317/55 , C07K2317/567 , C07K2317/622 , C07K2317/73 , C07K2317/92 , C07K2319/30
摘要： Meditope variants and methods for their use are provided herein. A meditope variant as described herein comprises a peptide having a sequence CQFDLSTRRLKC (SEQ ID NO:1) or CQYNLSSRALKC (SEQ ID NO:2) that has one or more modifications at of least one amino acid residue of the sequence. Multivalent meditope variant tethering entities are also provided. Such entities may include two or more meditopes coupled via a long linker, multivalent scaffold, biotin-streptavidin, or IgG Fc domain. Further, methods of treating, imaging or diagnosing a disease or condition are provided. Such methods may include administering a therapeutically effective amount of a pharmaceutical composition to a subject, the pharmaceutical compound comprising an antibody-meditope complex; a multivalent tethering agent in combination with a monoclonal antibody or functional fragment thereof; or a combination thereof.
摘要翻译：本文提供了Meditope变体及其使用方法。如本文所述的本发明变体包含在序列的至少一个氨基酸残基上具有一个或多个修饰的具有序列CQFDLSTRRLKC（SEQ ID NO：1）或CQYNLSSRALKC（SEQ ID NO：2）的肽。还提供了多重测井变体tethering实体。这样的实体可以包括通过长连接子，多价支架，生物素 - 链亲和素或IgG Fc结构域偶联的两个或更多个中枢。此外，提供了治疗，成像或诊断疾病或病症的方法。这样的方法可以包括向受试者施用治疗有效量的药物组合物，所述药物化合物包含抗体 - 中间体复合物; 多价连结剂与单克隆抗体或其功能片段组合; 或其组合。

6. 发明授权

US06211361B1 Method for making debromohymenialdisine and analogs thereof 失效
标题翻译：制备脱血管麻黄碱及其类似物的方法
公开(公告)号：US06211361B1
公开(公告)日：2001-04-03
申请号：US09357687
申请日：1999-07-20
申请人： David A. Horne , Kenichi Yakushijin
发明人： David A. Horne , Kenichi Yakushijin
IPC分类号： C07D48704
CPC分类号： C07D487/04
摘要： A method for making debromohymenialdisine (DBH) 2 and analogs thereof is described. One embodiment of the present method first comprises forming hymenin 4, and then converting hymenin into DBH 2 as described herein. One such embodiment first comprises providing a compound having Formula 3 where R is independently selected from the group consisting of hydrogen and lower aliphatic, and X is independently selected from the group consisting of hydrogen and halogen. A compound having Formula 3, such as Compound 10 with R and X as hydrogen, is then converted to DBH 2 or an analog thereof. An alternative embodiment of the method comprises forming Compound 30 or Compound 32, which are then directly converted to DBH 2. Alternatively, Compound 30 can be converted to Compound 10, which is then subsequently converted to DBH 2 by reaction with a halogen in the presence of an acid. The method of the present invention can be used to make analogs of DBH 2, including alkoxy derivatives, such as Compound 12, and conjugated diene derivatives, such as Compound 14.
摘要翻译：描述了制备脱血管麻黄碱（DBH）2及其类似物的方法。本方法的一个实施方案首先包括形成hymenin 4，然后如本文所述将hymenin转化为DBH 2。一个这样的实施方案首先包括提供具有式3的化合物，其中R独立地选自氢和低级脂族，并且X独立地选自氢和卤素。然后将具有式3的化合物，例如具有R和X作为氢的化合物10转化为DBH 2或其类似物。该方法的替代实施方案包括形成化合物30或化合物32，然后将其直接转化为DBH 2.或者，化合物30可以转化为化合物10，然后将其转化为DBH 2，通过在存在下与卤素反应的酸。本发明的方法可用于制备包括烷氧基衍生物如化合物12和共轭二烯衍生物如化合物14的DBH 2的类似物。

7. 发明授权

US6103899A Bicyclic aminoimidazoles 失效
标题翻译：双环氨基咪唑
公开(公告)号：US6103899A
公开(公告)日：2000-08-15
申请号：US185831
申请日：1998-11-04
申请人： David A. Horne , Kenichi Yakushijin
发明人： David A. Horne , Kenichi Yakushijin
IPC分类号： C07D207/00 , C07D207/337 , C07D233/88 , C07D403/04 , C07D405/00 , C07D405/12 , C07D487/04 , C07D487/14 , C07D498/14
CPC分类号： C07D403/04 , C07D233/88 , C07D487/04 , C07D487/14
摘要： The subject invention provides a bicyclic aminoimidazole compound, a hydroxyalkyl aminoimidazole compound, a bicyclic pyrrole compound, a hymenin compound, an aldehyde aminoimidazole compound, a ketal aminoimidazole compound, a tricyclic compound, and a tetrahydropurine compound. The subject invention also provides for processes for preparing the compounds.
摘要翻译：本发明提供双环氨基咪唑化合物，羟烷基氨基咪唑化合物，双环吡咯化合物，hymenin化合物，醛氨基咪唑化合物，缩酮氨基咪唑化合物，三环化合物和四氢嘌呤化合物。本发明还提供了制备化合物的方法。

8. 发明授权

US06399767B1 Intermediates for the synthesis of vitamin D and steroid derivatives and process for preparation thereof 失效
标题翻译：用于合成维生素D和类固醇衍生物的中间体及其制备方法
公开(公告)号：US06399767B1
公开(公告)日：2002-06-04
申请号：US09576543
申请日：2000-05-22
申请人： David A. Horne , Noboru Kubodera , Hiroshi Suzuki , Hitoshi Shimizu
发明人： David A. Horne , Noboru Kubodera , Hiroshi Suzuki , Hitoshi Shimizu
IPC分类号： C07C40300
CPC分类号： C07D303/24 , C07C319/14 , C07C401/00 , C07C2601/14 , C07C2602/24 , C07J7/0065 , C07J17/00 , C07J51/00 , Y02P20/55 , C07C321/16
摘要： A process for preparing a compound having structure (I) wherein n is an integer from 1-5; each of R1 and R2 independently is optionally substituted C1-C6 alkyl; each of W and X is independently hydrogen or C1-C6 alkyl; Y is O, S or NR3 where R3 is hydrogen, C1-C6 alkyl or a protective group; and Z is a CD ring structure, a steroid structure, or a vitamin D structure, each of which optionally having structure (IV) wherein W, X, Y and Z are defined above, in the presence of a base, with a compound having structure (V) or (v′) wherein n, R1 and R2 are as defined above, and E is an eliminating group.
摘要翻译：一种制备具有结构（I）的化合物的方法，其中n为1-5的整数; R 1和R 2各自独立地是任选取代的C 1 -C 6烷基; W和X各自独立地为氢或C 1 -C 6烷基; Y是O，S或NR 3，其中R 3是氢，C 1 -C 6烷基或保护基; Z是CD环结构，类固醇结构或维生素D结构，其中任一种具有结构（Ⅳ），其中W，X，Y和Z如上定义，在碱的存在下，结构（V）或（v'），其中n，R 1和R 2如上所定义，E是除去基团。

9. 发明授权

US06197954B1 Intermediates for the synthesis of debromohymenialdisine and processes thereof 失效
标题翻译：用于合成脱溴尿路胰岛素的中间体及其过程
公开(公告)号：US06197954B1
公开(公告)日：2001-03-06
申请号：US09016748
申请日：1998-01-30
申请人： David A. Horne , Kenichi Yakushijin
发明人： David A. Horne , Kenichi Yakushijin
IPC分类号： C07D48704
CPC分类号： C07D487/04
摘要： The synthesis of C11N5 marine sponge alkaloids (±)-hymenin (1), stevensine (2), hymenialdisine (3), and debromohymenialdisine (4) is described. These natural products are the primary family members of the sponge metabolites that contain a fused pyrrolo[2,3-c]azepin-8-one ring system with either a 2-aminoimidazole (AI) or glycocyamidine appendage. The key steps in the synthesis centered around the generation of novel azafulvenium ions and their regioselective heterodimerization with AI in order to create the tricyclic core. A rarely used protodebromination/oxidation strategy was employed to selectively generate the desired a-bromo substitution pattern seen in hymenialdisine (3). In addition, the AI moiety was shown to be a useful precursor to the glycocyamidine unit found in 3 and 4, which suggests that AI derived natural products may be the biogenic forerunners to glycocyamidine metabolites.
摘要翻译：描述了C11N5海绵状海藻生物碱（） - 香豆素（1），stevensine（2），hymenialdisine（3）和脱海马氏体（4）的合成。这些天然产物是海绵代谢物的主要成员，其含有具有2-氨基咪唑（AI）或糖基脒附属物的稠合吡咯并[2,3-c]吖庚因-8-酮环系。合成中的关键步骤围绕新生的氮杂多氟离子的产生以及其与AI的区域选择性异二聚化以产生三环核心。使用很少使用的原溴化/氧化策略来选择性地产生在hymenialdisine中看到的所需的α-溴取代模式（3）。此外，AI部分被证明是在3和4中发现的糖胞苷单位的有用前体，这表明AI衍生的天然产物可能是糖基代谢物的生物来源先驱

10. 发明授权

US06841685B2 Methods for making bis-heterocyclic alkaloids 失效
标题翻译：制备双杂环生物碱的方法
公开(公告)号：US06841685B2
公开(公告)日：2005-01-11
申请号：US10297688
申请日：2001-06-07
申请人： David A. Horne , Kenichi Yakushijin
发明人： David A. Horne , Kenichi Yakushijin
IPC分类号： C07D209/16 , C07D209/18 , C07D209/42 , C07D403/14 , C07D413/14 , C07D209/12 , A61K31/405
CPC分类号： C07D403/14 , C07D209/16 , C07D209/18 , C07D209/42 , C07D413/14
摘要： Methods for making bis-heterocyclic compounds, especially bis-heterocyclic compounds having five and six-membered heterocyclic linkers are described. Also described are methods for making an alpha amino ketone synthon that enables facile syntheses of bisindole compounds, including topsentins and dragmacidins
摘要翻译：描述了制备双杂环化合物，特别是具有五和六元杂环连接体的双杂环化合物的方法。还描述了制备能够容易地合成双吲哚化合物的α-氨基酮合成酶的方法，所述双吲哚化合物包括外源和拖曳剂

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