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1. 发明申请

US20130317045A1 THIENOPYRIDINE AND THIENOPYRIMIDINE COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
标题翻译：三硝基吡啶和三烯炔基化合物及其使用方法
公开(公告)号：US20130317045A1
公开(公告)日：2013-11-28
申请号：US13819274
申请日：2011-08-31
申请人： Michael J. Hadd , Mark W. Holladay , Eduardo Setti
发明人： Michael J. Hadd , Mark W. Holladay , Eduardo Setti
IPC分类号： C07D495/04 , A61K31/519
CPC分类号： A61K31/519 , A61K31/4743 , A61K45/06 , C07D495/02 , C07D495/04 , A61K2300/00
摘要： Provided herein are thienopyridine and thienopyrimidine compounds of formula (I) for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
摘要翻译：本文提供式（I）的噻吩并吡啶和噻吩并嘧啶化合物，用于治疗JAK激酶介导的疾病，包括JAK2激酶，JAK3激酶或TYK2激酶介导的疾病。还提供了包含该化合物的药物组合物和使用该化合物和组合物的方法。

2. 发明授权

US08349851B2 JAK kinase modulating compounds and methods of use thereof 有权
公开(公告)号：US08349851B2
公开(公告)日：2013-01-08
申请号：US12714323
申请日：2010-02-26
申请人： Sunny Abraham , Qi Chao , Michael J. Hadd , Mark W. Holladay , Gang Liu , Eduardo Setti
发明人： Sunny Abraham , Qi Chao , Michael J. Hadd , Mark W. Holladay , Gang Liu , Eduardo Setti
IPC分类号： A61K31/517
CPC分类号： A61K31/517 , A61K31/5377 , A61K45/06 , C07D401/14 , C07D403/12 , C07D405/14
摘要： Provided herein are quinazoline compounds of formula (I): The compounds are useful for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.

3. 发明申请

US20100317659A1 JAK KINASE MODULATING COMPOUNDS AND METHODS OF USE THEREOF 有权
标题翻译： JAK激酶调节化合物及其使用方法
公开(公告)号：US20100317659A1
公开(公告)日：2010-12-16
申请号：US12714323
申请日：2010-02-26
申请人： Sunny Abraham , Qi Chao , Michael J. Hadd , Mark W. Holladay , Gang Liu , Eduardo Setti
发明人： Sunny Abraham , Qi Chao , Michael J. Hadd , Mark W. Holladay , Gang Liu , Eduardo Setti
IPC分类号： A61K31/5377 , C07D403/12 , C07D413/14 , C07D407/14 , A61K31/517 , A61P35/00 , A61P37/00 , A61P29/00 , A61P37/06 , A61P37/02
CPC分类号： A61K31/517 , A61K31/5377 , A61K45/06 , C07D401/14 , C07D403/12 , C07D405/14
摘要： Provided herein are quinazoline compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
摘要翻译：本文提供了用于治疗JAK激酶介导的疾病的喹唑啉化合物，包括JAK2激酶，JAK3激酶或TYK2激酶介导的疾病。还提供了包含该化合物的药物组合物和使用该化合物和组合物的方法。

4. 发明申请

US20080182802A1 SPIROHETEROCYCLIC GLYCOSIDES AND MEHTODS OF USE 有权
标题翻译：螺旋藻糖苷和使用的MEHTODS
公开(公告)号：US20080182802A1
公开(公告)日：2008-07-31
申请号：US11964493
申请日：2007-12-26
申请人： Michael J. Hadd , Yuanwei Chen , Yan Feng , Sengen Sen , Brian Seed
发明人： Michael J. Hadd , Yuanwei Chen , Yan Feng , Sengen Sen , Brian Seed
IPC分类号： A61K31/7048 , C07H17/04 , A61P3/10 , A61P3/04
CPC分类号： C07H17/04
摘要： Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.
摘要翻译：提供对钠依赖性葡萄糖转运蛋白SGLT具有抑制作用的化合物。本发明还提供药物组合物，制备化合物的方法，合成中间体，以及独立地或与其它治疗剂组合使用化合物治疗受SGLT抑制影响的疾病和病症的方法。

5. 发明授权

US06812365B2 Disulfone reagents and methods of preparing and using same 失效
标题翻译：二砜试剂及其制备及使用方法
公开(公告)号：US06812365B2
公开(公告)日：2004-11-02
申请号：US10287760
申请日：2002-11-05
申请人： Jacqueline Gervay-Hague , Michael J. Hadd
发明人： Jacqueline Gervay-Hague , Michael J. Hadd
IPC分类号： C07F902
CPC分类号： C07F9/65502 , C07F9/4006
摘要： The present invention provides novel disulfone compounds and methods of preparing and using those compounds to further prepare biologically relevant gem-disulfone analogs of natural enzyme substrates. Methods of using a variety of disulfone compounds as reagents capable of forming symmetrical and non-symmetrical &agr;, &bgr; unsaturated gem-disulfones are also provided. There is also provided a disulfone reagent which reacts with both aromatic and aliphatic aldehydes in good to moderate yield to give exclusively the trans isomer. In accordance with further aspects of the present invention, a methodology for stereospecifically preparing potential gem-disulfone enzyme inhibitors is provided. A synthetic design which allows easy substitution of functional groups so that a number of substrate analogs can be synthesized readily is also provided. In addition, there is provided a new class of compounds which are potential glycosyl transferase inhibitors having characteristics which can inhibit the incorporation of sialic acid and/or fucose into glycoconjugates present at the surface of certain cancer cells. Additionally, a class of potent disulfone-linked catechol-based enzyme inhibitors, such as HIV-1 integrase inhibitors, is provided.
摘要翻译：本发明提供了新的二砜化合物以及制备和使用这些化合物以进一步制备天然酶底物的生物学相关的宝石 - 二砜类似物的方法。还提供了使用各种二砜化合物作为能够形成对称和非对称的α，β不饱和Gem-disulfones的试剂的方法。还提供了一种二砜试剂，其以良好至中等的产率与芳族和脂族醛反应，仅产生反式异构体。根据本发明的另外的方面，提供了立体选择性制备潜在的宝石 - 二砜酶抑制剂的方法。还提供了容易地代替官能团以便容易地合成许多底物类似物的合成设计。此外，提供了一类新的具有潜在的糖基转移酶抑制剂的化合物，其具有可抑制唾液酸和/或岩藻糖掺入存在于某些癌细胞表面的糖缀合物的特征。另外，提供一类有效的基于二硫键的儿茶酚基酶抑制剂，如HIV-1整合酶抑制剂。

6. 发明申请

US20130303533A1 AZOLOPYRIDINE AND AZOLOPYRIMIDINE COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
标题翻译：吡咯并吡嗪和亚氨基吡啶化合物及其使用方法
公开(公告)号：US20130303533A1
公开(公告)日：2013-11-14
申请号：US13820119
申请日：2011-08-31
申请人： Qi Chao , Michael J. Hadd , Mark W. Holladay , Martin Rowbottom
发明人： Qi Chao , Michael J. Hadd , Mark W. Holladay , Martin Rowbottom
IPC分类号： C07D487/04 , C07D513/04 , A61K31/5377 , A61K31/519 , A61K45/06
CPC分类号： C07D487/04 , A61K31/519 , A61K31/5377 , A61K45/06 , C07D513/04
摘要： Provided herein are azolopyridine and azolopyrimidine compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
摘要翻译：本文提供了用于治疗JAK激酶介导的疾病的包括JAK2激酶，JAK3激酶或TYK2激酶介导的疾病的偶氮吡啶和偶氮嘧啶化合物。还提供了包含该化合物的药物组合物和使用该化合物和组合物的方法。

7. 发明申请

US20130296363A1 QUINOLINE AND ISOQUINOLINE DERIVATIVES FOR USE AS JAK MODULATORS 审中-公开
标题翻译：用作JAK调节剂的喹啉和异喹啉衍生物
公开(公告)号：US20130296363A1
公开(公告)日：2013-11-07
申请号：US13819283
申请日：2011-08-31
申请人： Raffaella Faraoni , Michael J. Hadd , Mark W. Holladay , Martin W. Rowbottom , Eduardo Setti
发明人： Raffaella Faraoni , Michael J. Hadd , Mark W. Holladay , Martin W. Rowbottom , Eduardo Setti
IPC分类号： C07D401/12 , A61K31/4709 , A61K45/06 , C07D417/12 , C07D413/12 , A61K31/4725 , C07D405/14
CPC分类号： C07D401/12 , A61K31/4709 , A61K31/4725 , A61K45/06 , C07D401/14 , C07D405/14 , C07D413/12 , C07D417/12 , A61K2300/00
摘要： Provided herein are compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
摘要翻译：本文提供了用于治疗JAK激酶介导的疾病的化合物，包括JAK2激酶，JAK3激酶或TYK2激酶介导的疾病。还提供了包含该化合物的药物组合物和使用该化合物和组合物的方法。

8. 发明授权

US07838498B2 Benzylic glycoside derivatives and methods of use 有权
标题翻译：苄基苷衍生物及其使用方法
公开(公告)号：US07838498B2
公开(公告)日：2010-11-23
申请号：US12060767
申请日：2008-04-01
申请人： Yuanwei Chen , Yan Feng , Baihua Xu , Binhua Lv , Brian Seed , Michael J. Hadd , Huawei Cheng , Zelin Sheng , Min Xu , Congna Wang , Jiyan Du , Lili Zhang , Ge Xu , Yuelin Wu
发明人： Yuanwei Chen , Yan Feng , Baihua Xu , Binhua Lv , Brian Seed , Michael J. Hadd , Huawei Cheng , Zelin Sheng , Min Xu , Congna Wang , Jiyan Du , Lili Zhang , Ge Xu , Yuelin Wu
IPC分类号： A01N43/04 , A61K31/70 , C07H1/00
CPC分类号： C07H7/04 , A61K38/00 , C07D309/10
摘要： Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.
摘要翻译：提供对钠依赖性葡萄糖转运蛋白SGLT具有抑制作用的化合物。本发明还提供药物组合物，制备化合物的方法，合成中间体，以及独立地或与其它治疗剂组合使用化合物治疗受SGLT抑制影响的疾病和病症的方法。

9. 发明申请

US20090118201A1 BENZYLBENZENE DERIVATIVES AND METHODS OF USE 有权
标题翻译：苯并噻吩衍生物及其使用方法
公开(公告)号：US20090118201A1
公开(公告)日：2009-05-07
申请号：US12197095
申请日：2008-08-22
申请人： Yuanwei Chen , Huawei Cheng , Shengbin Li , Yuelin Wu , Yan Feng , Binhua Lv , Baihua Xu , Brian Seed , Michael J. Hadd , Yanli Song , Jiyan Du , Congna Wang , Jacques Y. Roberge
发明人： Yuanwei Chen , Huawei Cheng , Shengbin Li , Yuelin Wu , Yan Feng , Binhua Lv , Baihua Xu , Brian Seed , Michael J. Hadd , Yanli Song , Jiyan Du , Congna Wang , Jacques Y. Roberge
IPC分类号： A61K31/7028 , C07H7/04 , C07H7/06 , A61P3/10
CPC分类号： C07H7/04 , C07D309/10 , C07D407/12
摘要： Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.
摘要翻译：提供对钠依赖性葡萄糖转运蛋白SGLT具有抑制作用的化合物。本发明还提供药物组合物，制备化合物的方法，合成中间体，以及独立地或与其它治疗剂组合使用化合物治疗受SGLT抑制影响的疾病和病症的方法。

10. 发明申请

US20130225614A1 4-AZOLYLAMINOQUINAZOLINE DERIVATIVES AND METHODS OF USE THEREOF 审中-公开
标题翻译： 4-氨基亚氨基喹啉衍生物及其使用方法
公开(公告)号：US20130225614A1
公开(公告)日：2013-08-29
申请号：US13819290
申请日：2011-08-31
申请人： Michael J. Hadd
发明人： Michael J. Hadd
IPC分类号： A61K31/517 , C07D417/12 , A61K45/06 , C07D403/12
CPC分类号： A61K31/517 , A61K45/06 , C07D403/12 , C07D417/12
摘要： Provided herein are 4-azolylaminoquinazoline compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
摘要翻译：本文提供了用于治疗JAK激酶介导的疾病的4-唑基氨基喹唑啉化合物，包括JAK2激酶，JAK3激酶或TYK2激酶介导的疾病。还提供了包含该化合物的药物组合物和使用该化合物和组合物的方法。

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