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1. 发明公开

EP3010915A4 SUBSTITUTED (E)-N'-(1-PHENYLETHYLIDENE) BENZOHYDRAZIDE ANALOGS AS HISTONE DEMETHYLASE INHIBITORS 有权
标题翻译：替代物（E）-N' - （1-苯基乙基） - 苯甲酰基 - 阿诺考酸二甲基乙酰化酶
公开(公告)号：EP3010915A4
公开(公告)日：2016-12-28
申请号：EP14813387
申请日：2014-06-19
申请人： UNIV UTAH RES FOUND
发明人： VANKAYALAPATI HARIPRASAD , SORNA VENKATASWAMY , WARNER STEVE L , BEARSS DAVID J , SHARMA SUNIL , STEPHENS BRET
IPC分类号： A61K31/506 , A61P35/00 , C07D211/96 , C07D213/87 , C07D231/50 , C07D295/26
CPC分类号： C07D295/26 , C07D211/96 , C07D213/87 , C07D231/12
摘要： Substituted (E)-N'-(1-phenylethylidene)benzohydrazide analogs or (3-(5-chloro-2-hydroxyphenyl)-4-METHYL-1 H-pyrazol-1-YL)(3- (morpholinosulfonyl)phenyl)methanone, derivatives thereof, and related compounds are useful as inhibitors of lysine-specific histone demethylase, including LSD1. Synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1 (lysine-specific demethylase). A pharmaceutically acceptable salt, hydrate, solvate, or polymorph thereof, and one or more of: (a) at least one agent known to increase histone demethylase activity; (b) at least one agent known to decrease histone demethylase activity; (c) at least one agent known to treat a disorder of uncontrolled cellular proliferation; (d) at least one agent known to treat a neurodegenerative disorder; (e) instructions for treating a neurodegenerative disorder; or (f) instructions for treating a disorder associated with uncontrolled cellular proliferation.
摘要翻译：取代的（E）-N' - （1-苯基亚乙基）苯甲酰肼类似物或（3-（5-氯-2-羟基苯基）-4-甲基-1H-吡唑-1-基）（3-（吗啉代磺酰基）苯基）甲酮，其衍生物和相关化合物可用作赖氨酸特异性组蛋白脱甲基酶（包括LSD1）的抑制剂。制备化合物的合成方法; 包含该化合物的药物组合物; 以及使用该化合物和组合物来治疗与LSD1（赖氨酸特异性脱甲基酶）的功能障碍相关的疾病的方法。其药学上可接受的盐，水合物，溶剂化物或多晶型物，以及一种或多种：（a）已知增加组蛋白脱甲基酶活性的至少一种试剂; （b）至少一种已知降低组蛋白脱甲基酶活性的药剂; （c）至少一种已知治疗不受控制的细胞增殖病症的药剂; （d）至少一种已知治疗神经变性疾病的药物; （e）治疗神经变性疾病的说明书; 或（f）治疗与不受控制的细胞增殖相关的病症的说明书。

2. 发明公开

EP2694486A4 SUBSTITUTED N-(3-(PYRIMIDIN-4-YL)PHENYL)ACRYLAMIDE ANALOGS AS TYROSINE RECEPTOR KINASE BTK INHIBITORS 失效
标题翻译：替代N-（3-（吡啶基-4-YL-）苯基） - 丙烯酰胺 - 阿那膦酸酯类抗坏血酸酶 - BTK-HEMMER
公开(公告)号：EP2694486A4
公开(公告)日：2014-08-27
申请号：EP12765879
申请日：2012-04-01
申请人： UNIV UTAH RES FOUND
发明人： BEARSS DAVID J , VANKAYALAPATI HARIPRASAD , SORNA VENKATASWAMY , WARNER STEVEN L , SHARMA SUNIL
IPC分类号： C07D239/72 , A01N43/00 , A61K31/55
CPC分类号： C07D239/48 , C07D239/30 , C07D239/42 , C07D471/04 , C07D487/04
摘要： In one aspect, the invention relates to substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
摘要翻译：一方面，本发明涉及可用作BTK激酶抑制剂的取代的N-（3-（嘧啶-4-基）苯基）丙烯酰胺类似物，其衍生物和相关化合物。制备化合物的合成方法; 包含该化合物的药物组合物; 以及使用该化合物和组合物来治疗与BTK激酶功能障碍相关的疾病的方法。该摘要旨在作为用于在特定技术中进行搜索的扫描工具，而不意在限制本发明。

3. 发明公开

EP2903971A4 SUBSTITUTED N-(3-(PYRIMIDIN-4-YL)PHENYL)ACRYLAMIDE ANALOGS AS TYROSINE RECEPTOR KINASE BTK INHIBITORS 审中-公开
标题翻译：取代的N-（3-（嘧啶-4-基）苯基）丙烯酰胺类似物如TYROSINREZEPTORKINASE-BTK-缝边
公开(公告)号：EP2903971A4
公开(公告)日：2016-05-25
申请号：EP13844062
申请日：2013-10-04
申请人： UNIV UTAH RES FOUND
发明人： VANKAYALAPATI HARIPRASAD , SORNA VENKATASWAMY , WARNER STEVEN L , BEARSS DAVID J , SHARMA SUNIL
IPC分类号： C07D239/24 , A61K31/505 , A61K31/506 , A61K31/661 , A61K31/6615 , C07D239/42 , C07D487/04 , C07F9/06 , C07F9/6558 , C07F9/6561
CPC分类号： C07D239/42 , A61K31/505 , A61K31/506 , A61K31/661 , A61K31/6615 , C07D487/04 , C07F9/06 , C07F9/65583 , C07F9/6561
摘要： In one aspect, the invention relates to substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

4. 发明公开

EP2693881A4 SUBSTITUTED N-PHENYLPYRIMIDIN-2-AMINE ANALOGS AS INHIBITORS OF THE AXL KINASE 有权
标题翻译：替代N-苯基嘧啶-2-氨基-ANALOGA ALS AXL-激酶-HEMMER
公开(公告)号：EP2693881A4
公开(公告)日：2014-11-19
申请号：EP12763555
申请日：2012-03-31
申请人： UNIV UTAH RES FOUND
发明人： BEARSS DAVID J , VANKAYALAPATI HARIPRASAD , MOLLARD ALEXIS , WARNER STEVEN L , SHARMA SUNIL
IPC分类号： C07D239/02 , A61K31/506
CPC分类号： C07D239/42 , A61K31/506 , C07D239/48 , C07D401/12 , C07D403/12
摘要： In one aspect, the invention relates to substituted N-phenylpyrimidin-2-amine analogs, derivatives thereof, and related compounds, which are useful as inhibitors of Axl kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions for treating disorders associated with dysfunction of the Axl kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
摘要翻译：一方面，本发明涉及可用作Ax1激酶抑制剂的取代的N-苯基嘧啶-2-胺类似物，其衍生物和相关化合物。制备化合物的合成方法; 包含该化合物的药物组合物; 以及使用化合物和组合物治疗与Axl激酶功能障碍相关的疾病的方法。该摘要旨在作为用于在特定技术中进行搜索的扫描工具，而不意在限制本发明。

5. 发明公开

EP2903972A4 SUBSTITUTED N-(3-(PYRIMIDIN-4-YL)PHENYL)ACRYLAMIDE ANALOGS AS TYROSINE RECEPTOR KINASE BTK INHIBITORS 审中-公开
标题翻译：取代的N-（3-（嘧啶-4-基） - 苯基）
公开(公告)号：EP2903972A4
公开(公告)日：2016-04-06
申请号：EP13844466
申请日：2013-10-04
申请人： UNIV UTAH RES FOUND
发明人： VANKAYALAPATI HARIPRASAD , SORNA VENKATASWAMY , WARNER STEVEN L , BEARSS DAVID J , SHARMA SUNIL
IPC分类号： C07D239/24 , A61K31/33 , A61P35/00
CPC分类号： C07D487/04 , C07D239/42 , C07D239/48 , C07D401/12
摘要： In one aspect, the invention relates to substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

6. 发明公开

EP2694060A4 SUBSTITUTED 3-(1H-BENZO{D}IMIDAZOL-2-YL)-1H-INDAZOLE-ANALOGS AS INHIBITORS OF THE PDK1 KINASE 审中-公开
标题翻译：取代的3-（1H-苯并{D} - 咪唑-2-基）-1H-吲唑类似物作为PDK1激酶抑制剂
公开(公告)号：EP2694060A4
公开(公告)日：2014-09-10
申请号：EP12763840
申请日：2012-03-31
申请人： UNIV UTAH RES FOUND
发明人： BEARSS DAVID J , VANKAYALAPATI HARIPRASAD , SORNA VENKATASWAMY , WARNER STEVEN L , SHARMA SUNIL
IPC分类号： C07D403/04 , A61K31/416 , A61P35/00
CPC分类号： C07D403/04

7. 发明申请

WO2014055934A3 SUBSTITUTED N-(3-(PYRIMIDIN-4-YL)PHENYL)ACRYLAMIDE ANALOGS AS TYROSINE RECEPTOR KINASE BTK INHIBITORS 审中-公开
标题翻译：取代的N-（3-（嘧啶-4-基）苯基）丙烯酰胺类似物作为酪氨酸受体激酶BTK抑制剂
公开(公告)号：WO2014055934A3
公开(公告)日：2014-06-26
申请号：PCT/US2013063555
申请日：2013-10-04
申请人： UNIV UTAH RES FOUND
发明人： VANKAYALAPATI HARIPRASAD , SORNA VENKATASWAMY , WARNER STEVEN L , BEARSS DAVID J , SHARMA SUNIL
IPC分类号： C07D239/24
CPC分类号： C07D239/42 , A61K31/505 , A61K31/506 , A61K31/661 , A61K31/6615 , C07D487/04 , C07F9/06 , C07F9/65583 , C07F9/6561
摘要： In one aspect, the invention relates to substituted N-(3-(pyrimidin-4- yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
摘要翻译：在一个方面，本发明涉及取代的N-（3-（嘧啶-4-基）苯基）丙烯酰胺类似物，其衍生物和相关化合物，其可用作BTK激酶的抑制剂; 用于制备该化合物的合成方法; 包含该化合物的药物组合物以及使用该化合物和组合物治疗与BTK激酶功能障碍相关的病症的方法。该摘要旨在作为用于在特定领域中进行搜索的目的的扫描工具，并且不旨在限制本发明。

8. 发明申请

WO2014055928A3 SUBSTITUTED N-(3-(PYRIMIDIN-4-YL)PHENYL)ACRYLAMIDE ANALOGS AS TYROSINE RECEPTOR KINASE BTK INHIBITORS 审中-公开
公开(公告)号：WO2014055928A3
公开(公告)日：2014-06-26
申请号：PCT/US2013063549
申请日：2013-10-04
申请人： UNIV UTAH RES FOUND
发明人： VANKAYALAPATI HARIPRASAD , SORNA VENKATASWAMY , WARNER STEVEN L , BEARSS DAVID J , SHARMA SUNIL
IPC分类号： C07D239/24
CPC分类号： C07D487/04 , C07D239/42 , C07D239/48 , C07D401/12
摘要： In one aspect, the invention relates to substituted N-(3-(pyrimidin-4- yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

9. 发明公开

EP2744330A4 SUBSTITUTED (E)-N'-(1-PHENYLETHYLIDENE) BENZOHYDRAZIDE ANALOGS AS HISTONE DEMETHYLASE INHIITORS 有权
标题翻译：取代的（E）-N“ - （1-苯基亚乙基）苯甲酰肼类似物作为抑制剂HISTONDEMETHYLASE
公开(公告)号：EP2744330A4
公开(公告)日：2015-03-25
申请号：EP12823540
申请日：2012-08-15
申请人： UNIV UTAH RES FOUND
发明人： VANKAYALAPATI HARIPRASAD , SORNA VENKATASWAMY , WARNER STEVE L , BEARSS DAVID J , SHARMA SUNIL , STEPHENS BRET
IPC分类号： A01N37/36 , C07C241/00 , C07C243/00 , C07C311/46 , C07D205/04 , C07D295/155 , C07D295/26
CPC分类号： A61K31/4453 , A61K31/18 , A61K31/397 , A61K31/40 , A61K31/495 , A61K31/5375 , A61K31/5377 , C07C311/16 , C07C311/46 , C07D205/04 , C07D295/155 , C07D295/26
摘要： In one aspect, the invention relates to substituted (E)-N′-(1-phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

10. 发明专利

DK2744330T3 ERSTATTEDE (E)-N'-(1-PHENYLETHYLIDEN) BENZOHYDRAZID-ANALOGER SOM HISTONE-DEMETHYLASE-HÆMMERE 未知
公开(公告)号：DK2744330T3
公开(公告)日：2020-09-07
申请号：DK12823540
申请日：2012-08-15
申请人： UNIV UTAH RES FOUND
发明人： VANKAYALAPATI HARIPRASAD , SORNA VENKATASWAMY , WARNER STEVE L , BEARSS DAVID J , SHARMA SUNIL , STEPHENS BRET
IPC分类号： A01N37/36 , A61K31/18 , A61K31/40 , A61K31/495 , A61K31/5375 , C07C241/00 , C07C243/00 , C07C311/16 , C07D205/04 , C07D295/155 , C07D295/26

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