专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

US20100152206A1 Bicyclic Dihydropyrimidines and Uses Thereof 审中-公开
标题翻译：双环二嘧啶及其用途
公开(公告)号：US20100152206A1
公开(公告)日：2010-06-17
申请号：US11794586
申请日：2006-01-06
申请人： Ralph Mazitschek , John A. Tallarico , Zoltan Maliga , Timothy J. Mitchison
发明人： Ralph Mazitschek , John A. Tallarico , Zoltan Maliga , Timothy J. Mitchison
IPC分类号： A61K31/519 , C07D491/052 , C07D491/048 , C07D487/04 , C07D471/04 , A61P35/00 , C12N5/00
CPC分类号： C07D471/04 , C07D487/04 , C07D491/04
摘要： The present invention provides compounds having formula (I): (I) and pharmaceutically acceptable derivatives thereof; as described generally and in subclasses herein, which compounds are useful as kinesin inhibitors (e.g., Eg5 inhibitors), and thus are useful, for example, for the treatment of proliferative disorders e.g., cancer. The invention additionally provides methods for preparing compounds of the invention, compositions comprising them, and methods for the use thereof in the treatment of various disorders where Eg5 is involved. In certain embodiments, the present invention provides for compounds, compositions, methods and systems for inhibiting cell growth. More specifically, the present invention provides for methods, compounds and compositions which are capable of inhibiting mitosis in metabolically active cells. Compounds, compositions and methods of the present invention inhibit the activity of a protein involved in the assembly and maintenance of the mitotic spindle. One class of proteins which acts on the mitotic spindle is the family of mitotic kinesins, a subset of the kinesin superfamily.
摘要翻译：本发明提供具有式（I）的化合物：（I）及其药学上可接受的衍生物; 如本文中通常和在本文中所述的那样，哪些化合物可用作驱动蛋白抑制剂（例如Eg5抑制剂），因此可用于例如治疗增殖性疾病例如癌症。本发明另外提供了制备本发明化合物的方法，包含它们的组合物，以及用于治疗其中涉及Eg5的各种疾病的方法。在某些实施方案中，本发明提供了用于抑制细胞生长的化合物，组合物，方法和系统。更具体地，本发明提供能够抑制代谢活性细胞中有丝分裂的方法，化合物和组合物。本发明的化合物，组合物和方法抑制参与有丝分裂纺锤体的组装和维持的蛋白质的活性。作用于有丝分裂纺锤体的一类蛋白质是有丝分裂驱动蛋白家族，是驱动蛋白超家族的一个子集。

2. 发明申请

US20150038581A1 HISTONE DEACETYLASE INHIBITORS 有权
标题翻译： HISTONE脱乙酰酶抑制剂
公开(公告)号：US20150038581A1
公开(公告)日：2015-02-05
申请号：US14198764
申请日：2014-03-06
申请人： James Elliot Bradner , Ralph Mazitschek
发明人： James Elliot Bradner , Ralph Mazitschek
IPC分类号： C07C259/06
CPC分类号： A61K31/231 , A61K9/0014 , A61K31/165 , A61K31/337 , C07C235/78 , C07C259/06 , C07D319/06 , C07D413/12
摘要： In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are particularly useful in the treatment of skin disorders. When the compounds reaches the bloodstream, an esterase or an enzyme with esterase activity cleaves the compound into biologically inactive fragments or fragments with greatly reduced activity Ideally these degradation products exhibit a short serum and/or systemic half-life and are eliminated rapidly. These compounds and pharmaceutical compositions thereof are particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis, for example. The present invention also provides methods for preparing compounds of the invention and intermediates thereto.
摘要翻译：鉴于需要开发新的治疗剂，本发明提供了新的组蛋白脱乙酰酶抑制剂。这些化合物包括酯键，使它们对酯酶的失活敏感。因此，这些化合物特别可用于治疗皮肤病。当化合物达到血流时，酯酶或具有酯酶活性的酶将化合物切割成具有大大降低的活性的生物活性片段或片段。理想地，这些降解产物表现出短的血清和/或全身半衰期并被快速消除。这些化合物及其药物组合物例如特别可用于治疗皮肤T细胞淋巴瘤，神经纤维瘤病，牛皮癣，脱发，皮肤色素沉着和皮炎。本发明还提供了制备本发明化合物及其中间体的方法。

3. 发明授权

US08304451B2 Histone deacetylase and tubulin deacetylase inhibitors 有权
标题翻译：组蛋白脱乙酰酶和微管蛋白脱乙酰酶抑制剂
公开(公告)号：US08304451B2
公开(公告)日：2012-11-06
申请号：US12299430
申请日：2007-05-02
申请人： Ralph Mazitschek , Nicholas Paul Kwiatkowski , James Elliot Bradner
发明人： Ralph Mazitschek , Nicholas Paul Kwiatkowski , James Elliot Bradner
IPC分类号： A61K31/357 , C07D407/12
CPC分类号： C07D413/12 , C07D319/06 , C07D405/12 , C07D417/12
摘要： In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel inhibitors of histone deacetylases, tubulin deacetylases, and/or aggresome inhibitors, and pharmaceutically acceptable salts and derivatives thereof. The inventive compounds fall into two classes—“isotubacin” class and “isoisotubacin” class—all of which include a 1,3-dioxane core. The present invention further provides methods for treating disorders regulated by histone deacetylase activity, tubulin deacetylase activity, and/or the aggresome (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, protein degradation disorders, protein deposition disorders, etc.) comprising administering a therapeutically effective amount of an inventive compound to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.
摘要翻译：鉴于需要开发新的治疗剂及其有效的合成方法，本发明提供组蛋白脱乙酰酶，微管蛋白脱乙酰酶和/或聚集抑制剂的新型抑制剂及其药学上可接受的盐和衍生物。本发明的化合物分为两类：异豆豆素类和异倍他宁类，其中全部包括1,3-二恶烷核。本发明还提供了用于治疗由组蛋白脱乙酰酶活性，微管蛋白脱乙酰酶活性和/或聚集体（例如增殖性疾病，癌症，炎性疾病，原生动物感染，蛋白质降解紊乱，蛋白质沉积病症等）调节的病症的方法，其包括向有需要的受试者施用治疗有效量的本发明化合物。本发明还提供了制备本发明化合物的方法。

4. 发明申请

US20120190693A1 Reverse Amide Compounds As Protein Deacetylase Inhibitors And Methods Of Use Thereof 有权
公开(公告)号：US20120190693A1
公开(公告)日：2012-07-26
申请号：US13437672
申请日：2012-04-02
申请人： John H. van Duzer , Ralph Mazitschek , Walter Ogier , James E. Bradner , Guoxiang Huang , Dejian Xie , Nan Yu
发明人： John H. van Duzer , Ralph Mazitschek , Walter Ogier , James E. Bradner , Guoxiang Huang , Dejian Xie , Nan Yu
IPC分类号： A61K31/4965 , C07D403/12 , C07D239/42 , C07D213/74 , A61P35/02 , A61K31/166 , A61K31/506 , A61K31/505 , A61K31/4402 , A61P35/00 , C07C259/06 , C07D241/20
CPC分类号： A61K31/505 , A61K31/164 , A61K31/337 , A61K45/06 , C07C237/36 , C07C259/06 , C07D209/46 , C07D209/48 , C07D213/30 , C07D213/74 , C07D213/81 , C07D235/30 , C07D239/42 , C07D241/20 , C07D263/58 , C07D277/24 , C07D277/82 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D413/04 , C07D417/06
摘要： The present invention relates to novel “reverse amide” compounds comprising a zinc chelator group, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6.

5. 发明申请

US20100056588A1 HISTONE DEACETYLASE INHIBITORS 有权
标题翻译： HISTONE脱乙酰酶抑制剂
公开(公告)号：US20100056588A1
公开(公告)日：2010-03-04
申请号：US12279398
申请日：2007-02-14
申请人： James Elliot Bradner , Ralph Mazitschek
发明人： James Elliot Bradner , Ralph Mazitschek
IPC分类号： A61K31/422 , C07D413/12 , A61K31/22 , C07C229/00 , C12N5/02 , C07D319/06
CPC分类号： A61K31/231 , A61K9/0014 , A61K31/165 , A61K31/337 , C07C235/78 , C07C259/06 , C07D319/06 , C07D413/12
摘要： In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are particularly useful in the treatment of skin disorders. When the compounds reaches the bloodstream, an esterase or an enzyme with esterase activity cleaves the compound into biologically inactive fragments or fragments with greatly reduced activity Ideally these degradation products exhibit a short serum and/or systemic half-life and are eliminated rapidly. These compounds and pharmaceutical compositions thereof are particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis, for example. The present invention also provides methods for preparing compounds of the invention and intermediates thereto.
摘要翻译：鉴于需要开发新的治疗剂，本发明提供了新的组蛋白脱乙酰酶抑制剂。这些化合物包括酯键，使它们对酯酶的失活敏感。因此，这些化合物特别可用于治疗皮肤病。当化合物达到血流时，酯酶或具有酯酶活性的酶将化合物切割成具有大大降低的活性的生物活性片段或片段。理想地，这些降解产物表现出短的血清和/或全身半衰期并被快速消除。这些化合物及其药物组合物例如特别可用于治疗皮肤T细胞淋巴瘤，神经纤维瘤病，牛皮癣，脱发，皮肤色素沉着和皮炎。本发明还提供了制备本发明化合物及其中间体的方法。

6. 发明授权

US09284297B2 Halofuginone analogs for inhibition of tRNA synthetases and uses thereof 有权
标题翻译：卤夫酮类似物用于抑制tRNA合成酶及其用途
公开(公告)号：US09284297B2
公开(公告)日：2016-03-15
申请号：US13058486
申请日：2009-08-11
申请人： Tracy Keller , Ralph Mazitschek , Malcolm Whitman , Jinbo Lee , Mark S. Sundrud , Anjana Rao
发明人： Tracy Keller , Ralph Mazitschek , Malcolm Whitman , Jinbo Lee , Mark S. Sundrud , Anjana Rao
IPC分类号： A61K31/4184 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/14 , C07D491/04 , C07D495/04 , C07F9/6558
CPC分类号： A61K31/4184 , A61K31/685 , A61K31/695 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/14 , C07D491/04 , C07D495/04 , C07F9/65583
摘要： The present invention provides novel analogs and derivatives of halofuginone. The invention also provides pharmaceutical and cosmetic compositions thereof and methods for using halofuginone analogs in treating chronic inflammatory diseases, autoimmune diseases, dry eye syndrome, fibrosis, scar formation, angiogenesis, viral infections, ischemic damage, transplant and implant rejection, neurodegenerative diseases, and cosmetic applications.
摘要翻译：本发明提供卤代酮的新型类似物和衍生物。本发明还提供了其药物和化妆品组合物以及使用卤夫酮类似物治疗慢性炎性疾病，自身免疫性疾病，干眼症，纤维化，瘢痕形成，血管生成，病毒感染，缺血性损伤，移植和植入物排斥，神经变性疾病和化妆品应用。

7. 发明授权

US08716344B2 Class- and isoform-specific HDAC inhibitors and uses thereof 有权
标题翻译：类别和异构体特异性HDAC抑制剂及其用途
公开(公告)号：US08716344B2
公开(公告)日：2014-05-06
申请号：US13389814
申请日：2010-08-11
申请人： Ralph Mazitschek , James Elliot Bradner
发明人： Ralph Mazitschek , James Elliot Bradner
IPC分类号： A61K38/05 , A61K31/495 , C12Q1/48 , A61K45/06 , C07D239/42 , C07D401/04
CPC分类号： C07C243/38 , A61K31/175 , A61K31/495 , A61K38/05 , A61K45/06 , C07D239/42 , C07D401/04 , C12Q1/48
摘要： The present invention relates to compounds of the following formula wherein R3 is a fluorescent tag. Another aspect of the invention provides an assay for determining the inhibitory effect of a test compound on an HDAC protein comprising: incubating the HDAC protein with a substrate of the above formula in the presence of a test compound; and determining the activity of the HDAC protein.
摘要翻译：本发明涉及下式的化合物，其中R3是荧光标记。本发明的另一方面提供了一种用于测定测试化合物对HDAC蛋白质的抑制作用的测定法，包括：在测试化合物存在下，将HDAC蛋白质与上式的底物一起孵育; 并测定HDAC蛋白的活性。

8. 发明申请

US20140107166A1 HISTONE DEACETYLASE INHIBITORS AND METHODS OF USE THEREOF 审中-公开
标题翻译：组胺脱乙酰酶抑制剂及其使用方法
公开(公告)号：US20140107166A1
公开(公告)日：2014-04-17
申请号：US13985149
申请日：2012-02-13
申请人： Ralph Mazitschek , James E. Bradner , Melissa Grachan Harman
发明人： Ralph Mazitschek , James E. Bradner , Melissa Grachan Harman
IPC分类号： C07C259/10 , A61K31/165 , C07D213/81 , C07D333/38 , C07C69/734 , C07C259/06
CPC分类号： C07C259/10 , A61K31/165 , C07C69/732 , C07C69/734 , C07C259/06 , C07D213/81 , C07D333/38
摘要： The present invention provides novel compounds for inhibiting histone deacetylases, and pharmaceutically acceptable salts and derivatives thereof. The present invention further provides methods for treating disorders regulated by histone deacetylase activity (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, hair loss, etc.) comprising administering a therapeutically effective amount of a compound of the invention to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.
摘要翻译：本发明提供抑制组蛋白脱乙酰酶的新化合物及其药学上可接受的盐和衍生物。本发明还提供了治疗由组蛋白脱乙酰酶活性（例如增殖性疾病，癌症，炎性疾病，原生动物感染，脱发等）调节的病症的方法，其包括向受试者施用治疗有效量的本发明化合物需要。本发明还提供了制备本发明化合物的方法。

9. 发明申请

US20130040998A1 FLUORINATED HDAC INHIBITORS AND USES THEREOF 审中-公开
标题翻译：氟化HDAC抑制剂及其用途
公开(公告)号：US20130040998A1
公开(公告)日：2013-02-14
申请号：US13520650
申请日：2011-01-05
申请人： James Elliot Bradner , Ralph Mazitschek
发明人： James Elliot Bradner , Ralph Mazitschek
IPC分类号： A61K31/165 , A61K31/4045 , C07C239/14 , A61P35/00 , A61K31/40 , C07D213/56 , A61K31/44 , C07D209/14 , C07D207/333
CPC分类号： C07C259/06 , C07C259/10 , C07C271/28 , C07D207/323 , C07D209/14 , C07D213/75 , C07D221/14 , C07D413/12
摘要： Fluorinated deacetylase inhibitors of the general formulae (I), (II), and (III): and pharmaceutically acceptable salts thereof, as described herein, are useful as inhibitors of histone deacetylases or other deacetylases, and thus are useful for the treatment of various diseases and disorders associated with acetylase activity as described herein (e.g., cancer, neurodegenerative diseases, inflammatory diseases).
摘要翻译：如本文所述的通式（I），（II）和（III）的氟化脱乙酰酶抑制剂及其药学上可接受的盐可用作组蛋白脱乙酰酶或其它脱乙酰酶的抑制剂，因此可用于治疗各种与本文所述的乙酰酶活性相关的疾病和病症（例如，癌症，神经变性疾病，炎性疾病）。

10. 发明授权

US08324267B2 Kinase inhibitors and the use thereof 有权
标题翻译：激酶抑制剂及其用途
公开(公告)号：US08324267B2
公开(公告)日：2012-12-04
申请号：US10483687
申请日：2002-07-12
申请人： Vladimir Chirchin , Giannis Athanassios , Ralph Mazitschek , Jonathan Sleemann
发明人： Vladimir Chirchin , Giannis Athanassios , Ralph Mazitschek , Jonathan Sleemann
IPC分类号： A61K31/405 , C07D209/00
CPC分类号： A61K31/404 , C07D209/34
摘要： The present invention relates to protein kinase inhibitors and to the use thereof for the treatment of diseases induced by pathological signal transduction cascades.
摘要翻译：本发明涉及蛋白激酶抑制剂及其用于治疗由病理信号转导级联诱导的疾病的用途。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式