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1. 发明申请

US20190337934A1 RIP1 INHIBITORY COMPOUNDS AND METHODS FOR MAKING AND USING THE SAME 审中-公开
公开(公告)号：US20190337934A1
公开(公告)日：2019-11-07
申请号：US16402103
申请日：2019-05-02
申请人： Vanessa Taylor , Jiaxin Yu , Esteban Masuda , Ihab Darwish , Yan Chen
发明人： Vanessa Taylor , Jiaxin Yu , Esteban Masuda , Ihab Darwish , Yan Chen
IPC分类号： C07D413/14 , C07D491/107 , C07D471/10 , C07D487/08
摘要： Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to inhibit a RIP1 kinase in vivo or ex vivo, and also may treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.

2. 发明申请

US20210070743A1 RIP1 INHIBITORY COMPOUNDS AND METHODS FOR MAKING AND USING THE SAME 有权
公开(公告)号：US20210070743A1
公开(公告)日：2021-03-11
申请号：US17012779
申请日：2020-09-04
申请人： Yan Chen , Jiaxin Yu , Simon Shaw , Ihab Darwish , Vanessa Taylor , Somasekhar Bhamidipati , Zhushou Luo , Rao Kolluri
发明人： Yan Chen , Jiaxin Yu , Simon Shaw , Ihab Darwish , Vanessa Taylor , Somasekhar Bhamidipati , Zhushou Luo , Rao Kolluri
IPC分类号： C07D413/14 , C07D267/02 , C07D413/12 , C07D487/04 , C07D493/04 , C07D491/107 , A61K31/553
摘要： Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.

3. 发明申请

US20220288047A1 METHOD FOR TREATING A DISEASE OR CONDITION USING A PYRAZOLE COMPOUND OR FORMULATION THEREOF 有权
公开(公告)号：US20220288047A1
公开(公告)日：2022-09-15
申请号：US17684579
申请日：2022-03-02
申请人： Lu Chou , Matt Duan , Ihab Darwish , Simon Shaw , Somasekhar Bhamidipati , Vanessa Taylor , Yan Chen , Dazhong Fan , Zhushou Luo
发明人： Lu Chou , Matt Duan , Ihab Darwish , Simon Shaw , Somasekhar Bhamidipati , Vanessa Taylor , Yan Chen , Dazhong Fan , Zhushou Luo
IPC分类号： A61K31/4439 , A61K45/06 , A61K31/675 , A61K31/5377 , A61P17/00
摘要： Disclosed herein are embodiments of a method for treating a disease or condition in a subject, comprising administering to the subject, a pyrazole compound according to formula I. The compound may be administered as a composition, such as a spray-dried formulation. The disease or condition may be hidradenitis suppurativa, or a lymphoid neoplasm, and may be chronic myeloid leukemia or chronic myelomonocytic leukemia.

4. 发明申请

US20170369476A1 2,4-DIAMINO-PYRIMIDINE COMPOUNDS AND METHOD FOR MAKING AND USING THE COMPOUNDS 审中-公开
公开(公告)号：US20170369476A1
公开(公告)日：2017-12-28
申请号：US15633258
申请日：2017-06-26
申请人： Yan Chen , Rose Yen , Jiaxin Yu , Vanessa Taylor , Rajinder Singh
发明人： Yan Chen , Rose Yen , Jiaxin Yu , Vanessa Taylor , Rajinder Singh
IPC分类号： C07D403/12 , C07D405/14 , C07D401/14
摘要： Compounds within the scope of the present invention have a Formula 1 or a salt or prodrug thereof, where ring A is selected from cycloaliphatic; ring B is aryl; R1 is selected from (C1-C10)alkyl, (C3-C10)cycloalkyl, halo, aryl, and heteroaryl; and R2 and R3 are independently selected from hydrogen and (C1-C6)alkyl. Disclosed compounds may have an IRAK4 IC50 of from 0.003 μM to 3.7 μM; a TAK1 IC50 of from 0.008 μM to 132 μM; and/or an IRAK4/TAK1 selectivity of from 1 to 450. Particular compounds may have an IRAK4/TAK1 selectivity of from 100 to 500. Disclosed compositions may be formulated as pharmaceutical compositions. A method for using the compounds and/or compositions also are disclosed. The method may comprise administering to a subject an effective amount of a compound within the scope of the present invention, particularly to selectively inhibit IRAK 1 and/or IRAK4 over TAK1.

5. 发明授权

US10710983B2 2,4-diamino-pyrimidine compounds and method for making and using the compounds 有权
公开(公告)号：US10710983B2
公开(公告)日：2020-07-14
申请号：US15633258
申请日：2017-06-26
申请人： Yan Chen , Rose Yen , Jiaxin Yu , Vanessa Taylor , Rajinder Singh
发明人： Yan Chen , Rose Yen , Jiaxin Yu , Vanessa Taylor , Rajinder Singh
IPC分类号： C07D401/14 , C07D403/12 , C07D239/48 , C07D405/14
摘要： Compounds within the scope of the present invention have a Formula 1 or a salt or prodrug thereof, where ring A is selected from cycloaliphatic; ring B is aryl; R1 is selected from (C1-C10)alkyl, (C3-C10)cycloalkyl, halo, aryl, and heteroaryl; and R2 and R3 are independently selected from hydrogen and (C1-C6)alkyl. Disclosed compounds may have an IRAK4 IC50 of from 0.003 μM to 3.7 μM; a TAK1 IC50 of from 0.008 μM to 132 μM; and/or an IRAK4/TAK1 selectivity of from 1 to 450. Particular compounds may have an IRAK4/TAK1 selectivity of from 100 to 500. Disclosed compositions may be formulated as pharmaceutical compositions. A method for using the compounds and/or compositions also are disclosed. The method may comprise administering to a subject an effective amount of a compound within the scope of the present invention, particularly to selectively inhibit IRAK 1 and/or IRAK4 over TAK1.

6. 发明申请

US20190337907A1 RIP1 INHIBITORY COMPOUNDS AND METHODS FOR MAKING AND USING THE SAME 审中-公开
公开(公告)号：US20190337907A1
公开(公告)日：2019-11-07
申请号：US16402111
申请日：2019-05-02
申请人： Esteban Masuda , Simon Shaw , Vanessa Taylor
发明人： Esteban Masuda , Simon Shaw , Vanessa Taylor
IPC分类号： C07D267/14 , C07D413/12 , C07D413/14 , C07D487/04 , A61P35/00
摘要： Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.

7. 发明申请

US20100152218A1 COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY 有权
公开(公告)号：US20100152218A1
公开(公告)日：2010-06-17
申请号：US12711534
申请日：2010-02-24
申请人： Ankush Argade , Arvinder Sran , David Carroll , Jeffrey Clough , Kin Tso , Somasekhar Bhamidipati , Sambaiah Thota , Rajinder Singh , Vanessa Taylor , Hui Li , Esteban Masuda
发明人： Ankush Argade , Arvinder Sran , David Carroll , Jeffrey Clough , Kin Tso , Somasekhar Bhamidipati , Sambaiah Thota , Rajinder Singh , Vanessa Taylor , Hui Li , Esteban Masuda
IPC分类号： A61K31/505 , C07D239/48 , A61P35/00 , A61P35/02
CPC分类号： C07D239/48 , A61K31/505 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D407/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D498/04
摘要： The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful.

8. 发明授权

US07601713B2 Kinase inhibitors and their uses 有权
标题翻译：激酶抑制剂及其用途
公开(公告)号：US07601713B2
公开(公告)日：2009-10-13
申请号：US11611568
申请日：2006-12-15
申请人： Pingyu Ding , Ankush Argade , Dane Goff , Rajinder Singh , Esteban Masuda , Vanessa Taylor , Sacha Holland
发明人： Pingyu Ding , Ankush Argade , Dane Goff , Rajinder Singh , Esteban Masuda , Vanessa Taylor , Sacha Holland
IPC分类号： A61K31/519 , A61K31/52 , A61K31/517 , C07D498/04 , C07D487/04 , C07D473/16 , A61K31/5355 , A61K31/497 , A61K31/551 , C07D265/36 , C07D413/12 , C07D403/12 , C07D243/08 , A61P19/02 , C07D239/84 , C07D471/04 , C07D401/12
CPC分类号： C07D519/00 , A61K31/517 , C07D239/94 , C07D239/95 , C07D471/04 , C07D473/16 , C07D487/04 , C07D495/04 , C07D495/12
摘要： The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropriate kinase activity. The compounds of the present invention are according to structural formula (I): or a salt or N-oxide thereof, wherein B is selected from
摘要翻译：本公开提供了抑制蛋白激酶（例如JAK，Ax1或Syk激酶）的化合物，包含该化合物的组合物和使用该化合物抑制蛋白激酶并治疗和/或预防与不适当激酶活性相关疾病的方法。本发明的化合物是根据结构式（I）：或其盐或N-氧化物，其中B选自

9. 发明授权

US08637038B2 Methods for inhibiting allograft rejection 有权
标题翻译：抑制同种异体移植排斥的方法
公开(公告)号：US08637038B2
公开(公告)日：2014-01-28
申请号：US13444684
申请日：2012-04-11
申请人： Vanessa Taylor , Esteban Masuda
发明人： Vanessa Taylor , Esteban Masuda
IPC分类号： A61K39/00 , A01N43/54 , A01N43/00
CPC分类号： A61K31/506 , A61K31/436 , A61K31/4545 , A61K38/13 , A61K45/06 , A61K2300/00
摘要： Disclosed herein are methods for treating or inhibiting allograft rejection in a transplant recipient. In some embodiments, the methods include administering to the transplant recipient a first amount of a JAK1/3 inhibitor comprising 5-(2-(4-fluoro-3-methoxy-5-methylphenylamino)-5-methylpyrimidin-4-ylamino)benzo[d]oxazol-2(3H)-one (Compound I) or a prodrug thereof and administering to the transplant recipient a second amount of a non-JAK1/3 inhibitor immunosuppressant, wherein the combined effect of the first amount and the second amount is greater than the effect of the first amount or the second amount individually, wherein the JAK1/3 inhibitor acts in combination with the non-JAK1/3 inhibitor immunosuppressant to inhibit or treat allograft rejection. In some embodiments at least one of the first amount or the second amount is individually a suboptimal dose for inhibiting or treating allograft rejection. In some examples, the combined effect of the first amount and the second amount to inhibit or treat allograft rejection in the transplant recipient is synergistic.
摘要翻译：本文公开了用于在移植受体中治疗或抑制同种异体移植排斥的方法。在一些实施方案中，所述方法包括向移植受体施用第一量的包含5-（2-（4-氟-3-甲氧基-5-甲基苯基氨基）-5-甲基嘧啶-4-基氨基）苯并[ [d]恶唑-2（3H） - 酮（化合物I）或其前药，向移植受体施用第二量的非JAK1 / 3抑制剂免疫抑制剂，其中第一量和第二量的组合效应大于第一量或第二量的作用，其中JAK1 / 3抑制剂与非JAK1 / 3抑制剂免疫抑制剂联合用于抑制或治疗同种异体移植排斥反应。在一些实施方案中，第一量或第二量中的至少一种量单独为抑制或治疗同种异体移植物排斥反应的次优剂量。在一些实例中，第一量和第二量在移植受体中抑制或治疗同种异体移植排斥的组合作用是协同的。

10. 发明申请

US20120263737A1 METHODS FOR INHIBITING ALLOGRAFT REJECTION 有权
标题翻译：抑制ALLOGRAFT抑制剂的方法
公开(公告)号：US20120263737A1
公开(公告)日：2012-10-18
申请号：US13444684
申请日：2012-04-11
申请人： Vanessa Taylor , Esteban Masuda
发明人： Vanessa Taylor , Esteban Masuda
IPC分类号： A61K31/506 , A61K39/00 , A61P37/06 , A61K39/395
CPC分类号： A61K31/506 , A61K31/436 , A61K31/4545 , A61K38/13 , A61K45/06 , A61K2300/00
摘要： Disclosed herein are methods for treating or inhibiting allograft rejection in a transplant recipient. In some embodiments, the methods include administering to the transplant recipient a first amount of a JAK1/3 inhibitor comprising 5-(2-(4-fluoro-3-methoxy-5-methylphenylamino)-5-methylpyrimidin-4-ylamino)benzo[d]oxazol-2(3H)-one (Compound I) or a prodrug thereof and administering to the transplant recipient a second amount of a non-JAK1/3 inhibitor immunosuppressant, wherein the combined effect of the first amount and the second amount is greater than the effect of the first amount or the second amount individually, wherein the JAK1/3 inhibitor acts in combination with the non-JAK1/3 inhibitor immunosuppressant to inhibit or treat allograft rejection. In some embodiments at least one of the first amount or the second amount is individually a suboptimal dose for inhibiting or treating allograft rejection. In some examples, the combined effect of the first amount and the second amount to inhibit or treat allograft rejection in the transplant recipient is synergistic.
摘要翻译：本文公开了用于在移植受体中治疗或抑制同种异体移植排斥的方法。在一些实施方案中，所述方法包括向移植受体施用第一量的包含5-（2-（4-氟-3-甲氧基-5-甲基苯基氨基）-5-甲基嘧啶-4-基氨基）苯并[ [d]恶唑-2（3H） - 酮（化合物I）或其前药，向移植受体施用第二量的非JAK1 / 3抑制剂免疫抑制剂，其中第一量和第二量的组合效应大于第一量或第二量的作用，其中JAK1 / 3抑制剂与非JAK1 / 3抑制剂免疫抑制剂联合用于抑制或治疗同种异体移植排斥反应。在一些实施方案中，第一量或第二量中的至少一种量单独为抑制或治疗同种异体移植物排斥反应的次优剂量。在一些实例中，第一量和第二量在移植受体中抑制或治疗同种异体移植排斥的组合作用是协同的。

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