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1. 发明专利

AU2020337938A1 KRas G12D inhibitors 未知
公开(公告)号：AU2020337938A1
公开(公告)日：2022-03-17
申请号：AU2020337938
申请日：2020-08-27
申请人： MIRATI THERAPEUTICS INC , ARRAY BIOPHARMA INC
发明人： WANG XIAOLUN , BURNS AARON CRAIG , CHRISTENSEN JAMES GAIL , KETCHAM JOHN MICHAEL , LAWSON JOHN DAVID , MARX MATTHEW ARNOLD , SMITH CHRISTOPHER RONALD , ALLEN SHELLEY , BLAKE JAMES FRANCIS , CHICARELLI MARK JOSEPH , DAHLKE JOSHUA RYAN , DAI DONGHUA , FELL JAY BRADFORD , FISCHER JOHN PETER , MEJIA MACEDONIO J , NEWHOUSE BRAD , NGUYEN PHONG , O'LEARY JACOB MATTHEW , PAJK SPENCER , RODRIGUEZ MARTHA E , SAVECHENKOV PAVEL , TANG TONY P , VIGERS GUY P A , ZHAO QIAN , KAHN DEAN RUSSELL , GAUDINO JOHN , HILTON MICHAEL CHRISTOPHER
IPC分类号： A61K31/435 , A61K31/4375 , A61K31/517 , C07D471/00 , C07D471/02 , C07D471/04
摘要： The present invention relates to compounds that inhibit KRas G12D. In particular, the present invention relates to compounds that inhibit the activity of KRas G12D, pharmaceutical compositions comprising the compounds and methods of use therefor.

2. 发明专利

CL2022000447A1 Inhibidores de kras g12d 未知
公开(公告)号：CL2022000447A1
公开(公告)日：2022-10-21
申请号：CL2022000447
申请日：2022-02-23
申请人： ARRAY BIOPHARMA INC , MIRATI THERAPEUTICS INC
发明人： SAVECHENKOV PAVEL , WANG XIAOLUN , BURNS AARON CRAIG , KETCHAM JOHN MICHAEL , LAWSON JOHN DAVID , MARX MATTHEW ARNOL , SMITH CHRISTOPHER RONALD , ALLEN SHELLEY , BLAKE JAMES FRANCIS , CHICARELLI MARK JOSEPH , DAHLKE JOSHUA RYAN , DAI DONGHUA , FELL JAY BRADFORD , FISCHER JOHN PETER , MEJIA MACEDONIO J , NEWHOUSE BRAD , NGUYEN PHONG , O'LEARY JACOB MATTHEW , PAJK SPENCER , RODRIGUEZ MARTHA E , TANG TONY P , VIGERS GUY P A , ZHAO QIAN , KAHN DEAN RUSSELL , GAUDINO JOHN , HILTON MICHAEL CHRISTOPHER , CHRISTENSEN JAMES GAIL
IPC分类号： A61K31/435 , A61K31/4375 , A61K31/517 , C07D471/00 , C07D471/02 , C07D471/04
摘要： La presente invención se refiere a compuestos que inhiben KRas G12D. En particular, la presente invención se refiere a compuestos que inhiben la actividad de KRas G12D, composiciones farmacéuticas que comprenden los compuestos y métodos de uso de las mismas.

3. 发明专利

ZA202202362B KRAS G12D INHIBITORS 未知
公开(公告)号：ZA202202362B
公开(公告)日：2022-09-28
申请号：ZA202202362
申请日：2022-02-24
申请人： MIRATI THERAPEUTICS INC , ARRAY BIOPHARMA INC
发明人： WANG XIAOLUN , BURNS AARON CRAIG , CHRISTENSEN JAMES GAIL , KETCHAM JOHN MICHAEL , LAWSON JOHN DAVID , MARX MATTHEW ARNOLD , SMITH CHRISTOPHER RONALD , ALLEN SHELLEY , BLAKE JAMES FRANCIS , CHICARELLI MARK JOSEPH , DAHLKE JOSHUA RYAN , DAI DONGHUA , FELL JAY BRADFORD , FISCHER JOHN PETER , MEJIA MACEDONIO J , NEWHOUSE BRAD , NGUYEN PHONG , O'LEARY JACOB MATTHEW , PAJK SPENCER , RODRIGUEZ MARTHA E , SAVECHENKOV PAVEL , TANG TONY P , VIGERS GUY P A , ZHAO QIAN , KAHN DEAN RUSSELL , GAUDINO JOHN , HILTON MICHAEL CHRISTOPHER
摘要： The present invention relates to compounds that inhibit KRas G12D. In particular, the present invention relates to compounds that inhibit the activity of KRas G12D, pharmaceutical compositions comprising the compounds and methods of use therefor.

4. 发明专利

CA3148745A1 KRAS G12D INHIBITORS 未知
公开(公告)号：CA3148745A1
公开(公告)日：2021-03-04
申请号：CA3148745
申请日：2020-08-27
申请人： MIRATI THERAPEUTICS INC , ARRAY BIOPHARMA INC
发明人： WANG XIAOLUN , CHRISTENSEN JAMES GAIL , KETCHAM JOHN MICHAEL , MARX MATTHEW ARNOLD , SMITH CHRISTOPHER RONALD , ALLEN SHELLEY , DAI DONGHUA , FISCHER JOHN PETER , NEWHOUSE BRAD , O'LEARY JACOB MATTHEW , RODRIGUEZ MARTHA E , VIGERS GUY P A , ZHAO QIAN , GAUDINO JOHN , BURNS AARON CRAIG , LAWSON JOHN DAVID , BLAKE JAMES FRANCIS , CHICARELLI MARK JOSEPH , DAHLKE JOSHUA RYAN , FELL JAY BRADFORD , MEJIA MACEDONIO J , NGUYEN PHONG , PAJK SPENCER , SAVECHENKOV PAVEL , TANG TONY P , KAHN DEAN RUSSELL , GAUDINO JOHN , HILTON MICHAEL CHRISTOPHER
IPC分类号： A61K31/435 , A61K31/4375 , A61K31/517 , C07D471/00 , C07D471/02 , C07D471/04
摘要： The present invention relates to compounds that inhibit KRas G12D. In particular, the present invention relates to compounds that inhibit the activity of KRas G12D, pharmaceutical compositions comprising the compounds and methods of use therefor.

5. 发明专利

CO2022003782A2 Inhibidores de kras g12d 未知
公开(公告)号：CO2022003782A2
公开(公告)日：2022-07-08
申请号：CO2022003782
申请日：2022-03-29
申请人： ARRAY BIOPHARMA INC , MIRATI THERAPEUTICS INC
发明人： WANG XIAOLUN , BURNS AARON CRAIG , CHRISTENSEN JAMES GAIL , KETCHAM JOHN MICHAEL , LAWSON JOHN DAVID , MARX MATTHEW ARNOLD , SMITH CHRISTOPHER RONALD , ALLEN SHELLEY , BLAKE JAMES FRANCIS , CHICARELLI MARK JOSEPH , DAHLKE JOSHUA RYAN , DAI DONGHUA , FELL JAY BRADFORD , FISCHER JOHN PETER , MEJIA MACEDONIO J , NEWHOUSE BRAD , NGUYEN PHONG , O'LEARY JACOB MATTHEW , PAJK SPENCER , RODRIGUEZ MARTHA E , SAVECHENKOV PAVEL , TANG TONY P , VIGERS GUY P A , ZHAO QIAN , KAHN DEAN RUSSELL , GAUDINO JOHN , HILTON MICHAEL CHRISTOPHER
IPC分类号： A61K31/435 , A61K31/4375 , A61K31/517 , C07D471/00 , C07D471/02 , C07D471/04
摘要： La presente invención se refiere a compuestos que inhiben KRas G12D. En particular, la presente invención se refiere a compuestos que inhiben la actividad de KRas G12D, composiciones farmacéuticas que comprenden los compuestos y métodos de uso de las mismas.

6. 发明专利

BR112022003543A2 Inibidores de kras g12 未知
公开(公告)号：BR112022003543A2
公开(公告)日：2022-05-24
申请号：BR112022003543
申请日：2020-08-27
申请人： ARRAY BIOPHARMA INC , MIRATI THERAPEUTICS INC
发明人： AARON CRAIG BURNS , NEWHOUSE BRAD , CHRISTOPHER RONALD SMITH , DEAN RUSSELL KAHN , DAI DONGHUA , GUY P A VIGERS , JACOB MATTHEW O'LEARY , JAMES FRANCIS BLAKE , JAMES GAIL CHRISTENSEN , JAY BRADFORD FELL , JOHN DAVID LAWSON , GAUDINO JOHN , JOHN MICHAEL KETCHAM , JOHN PETER FISCHER , JOSHUA RYAN DAHLKE , MACEDONIO J MEJIA , MARK JOSEPH CHICARELLI , MARTHA E RODRIGUEZ , MATTHEW ARNOLD MARX , MICHAEL CHRISTOPHER HILTON , SAVECHENKOV PAVEL , NGUYEN PHONG , ZHAO QIAN , ALLEN SHELLEY , PAJK SPENCER , TONY P TANG , WANG XIAOLUN
IPC分类号： A61K31/435 , A61K31/4375 , A61K31/517 , C07D471/00 , C07D471/02 , C07D471/04
摘要： inibidores de kras g12. a presente invenção se refere a compostos que inibem kras g12d. em particular, a presente invenção se refere a compostos que inibem a atividade de kras g12d, composições farmacêuticas compreendendo os compostos e métodos de uso para os mesmos.

7. 发明专利

AR119847A1 INHIBIDORES DE KRAS G12D 未知
公开(公告)号：AR119847A1
公开(公告)日：2022-01-12
申请号：ARP200102418
申请日：2020-08-27
申请人： MIRATI THERAPEUTICS INC , ARRAY BIOPHARMA INC
发明人： WANG XIAOLUN , BURNS AARON CRAIG , CHRISTENSEN JAMES GAIL , KETCHAM JOHN MICHAEL , LAWSON JOHN DAVID , MARX MATTHEW ARNOLD , SMITH CHRISTOPHER RONALD , ALLEN SHELLEY , BLAKE JAMES F , CHICARELLI MARK JOSEPH , DAHLKE JOSHUA , DAI DONGHUA , FELL JAY BRADFORD , FISCHER JOHN PETER , MEJIA MACEDONIO J , NEWHOUSE BRAD , NGUYEN PHONG , OLEARY JACOB M , PAJK SPENCER , RODRIGUEZ MARTHA E , SAVECHENKOV PAVEL , TANG TONY P , VIGERS GUY P A , ZHAO QIAN
IPC分类号： C07D487/08 , A61K31/529 , A61P35/00 , A61P35/02
摘要： Compuestos derivados de 3,8-diazabiciclo[3.2.1]octan-3-ilo como inhibidores de la actividad de KRas G12D, composiciones farmacéuticas que los comprenden y el uso de los mismos en el tratamiento de diversos tipos de cáncer, incluyendo leucemia. Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1) o una sal farmacéuticamente aceptable del mismo, donde: R¹ es hidrógeno, hidroxi, halógeno, C₁₋₃ alquilo, C₁₋₃ cianoalquilo, C₁₋₃ hidroxialquilo, HC(=O)-, -CO₂R⁵, -CO₂N(R⁵)₂ o un heteroarilo de 5 - 6 miembros; Y es una unión, O ó NR⁵; R² es hidrógeno, -N(R⁵)₂, heterociclilo, C₁₋₆ alquilo, -L-heterociclilo, -L-arilo, -L-heteroarilo, -L-cicloalquilo, -L-N(R⁵)₂, -L-NHC(=NH)NH₂, -L-C(O)N(R⁵)₂, -L-C₁₋₆ haloalquilo, -L-OR⁵, -L-(CH₂OR⁵)(CH₂)ₙOR⁵, -L-NR⁵C(O)-arilo, -L-COOH, o -LC(=O)OC₁₋₆ alquilo, donde las unidades heterociclilo y arilo de -L-NR⁵C(O)-arilo y la unidad heterociclilo de -L-heterociclilo y la unidad cicloalquilo de -L-cicloalquilo pueden estar opcionalmente sustituidas con uno o más R⁶, y donde el arilo o heteroarilo de -L-arilo y -L-heteroarilo puede estar opcionalmente sustituido con uno o más R⁷; cada L es en forma independiente un C₁₋₄ alquileno opcionalmente sustituido con hidroxi, C₁₋₄ hidroxialquilo o heteroarilo; R³ es arilo o heteroarilo, donde el arilo o el heteroarilo está opcionalmente sustituido con uno o más R⁸; R⁴ es hidrógeno, halógeno o C₁₋₃ alquilo; cada R⁵ es en forma independiente hidrógeno o C₁₋₃ alquilo; cada R⁶ es en forma independiente halógeno, hidroxi, C₁₋₃ hidroxialquilo, C₁₋₃ alquilo, C₁₋₃ haloalquilo, C₁₋₃ alcoxi, ciano, -Q-fenilo, -Q-fenilSO₂F, -NHC(O)fenilo, -NHC(O)fenilSO₂F, pirazolilo sustituido con C₁₋₃ alquilo, araC₁₋₃ alquilo-, tert-butildimetilsililoxiCH₂-, -N(R⁵)₂, (C₁₋₃ alcoxi)C₁₋₃ alquilo-, (C₁₋₃ alquil)C(=O), oxo, (C₁₋₃ haloalquil)C(=O)-, -SO₂F, (C₁₋₃ alcoxi)C₁₋₃ alcoxi, -CH₂OC(O)N(R⁵)₂, -CH₂NHC(O)OC₁₋₆ alquilo, -CH₂NHC(O)N(R⁵)₂, -CH₂NHC(O)C₁₋₆ alquilo, -CH₂(pirazolilo), -CH₂NHSO₂C₁₋₆ alquilo, -CH₂OC(O)heterociclilo, -OC(O)N(R⁵)₂, -OC(O)NH(C₁₋₃ alquil)O(C₁₋₃ alquilo), -OC(O)NH(C₁₋₃ alquil)O(C₁₋₃ alquil)fenil(C₁₋₃ alquil)N(CH₃)₂, -OC(O)NH(C₁₋₃ alquil)O(C₁₋₃ alquil)fenilo o -OC(O)heterociclilo, -CH₂-heterociclilo, donde el fenilo de -NHC(O)fenilo o -OC(O)NH(C₁₋₃ alquil)O(C₁₋₃ alquil)fenilo está opcionalmente sustituido con -C(O)H u OH y donde el heterociclilo de -CH₂-heterociclilo está opcionalmente sustituido con oxo; Q es una unión ó O; cada R⁷ es en forma independiente halógeno, hidroxi, HC(=O)-, C₁₋₄ alquilo, C₁₋₄ alcoxi, C₁₋₄ haloalquilo, C₁₋₄ hidroxialquilo, o -N(R⁵)₂; y cada R⁸ es en forma independiente halógeno, ciano, hidroxi, C₁₋₄ alquilo, -S-C₁₋₃ alquilo, C₂₋₄ alquenilo, C₂₋₄ alquinilo, C₂₋₄ hidroxialquinilo, C₁₋₃ cianoalquilo, triazolilo, C₁₋₃ haloalquilo, -O-C₁₋₃ haloalquilo, -S-C₁₋₃ haloalquilo, C₁₋₃ alcoxi, hidroxiC₁₋₃ alquilo, -CH₂C(=O)N(R⁵)₂, -C₃₋₄ alquinil(NR⁵)₂, -N(R⁵)₂, deuteroC₂₋₄ alquinilo, (C₁₋₃ alcoxi)haloC₁₋₃ alquilo-, o C₃₋₆ cicloalquilo donde dicho C₃₋₆ cicloalquilo está opcionalmente sustituido con halógeno o C₁₋₃ alquilo.

8. 发明公开

KR20180043407A TRK 키나제 저해제로서의 매크로시클릭 화합물 审中-公开
公开(公告)号：KR20180043407A
公开(公告)日：2018-04-27
申请号：KR20187011138
申请日：2011-05-13
申请人： ARRAY BIOPHARMA INC
发明人： ANDREWS STEVEN WADE , CONDROSKI KEVIN RONALD , HAAS JULIA , JIANG YUTONG , KOLAKOWSKI GABRIELLE R , SEO JEONGBEOB , YANG HONG WOON , ZHAO QIAN
IPC分类号： C07D487/22 , A61K31/519 , A61P25/00 , A61P35/00 , C07D471/22 , C07D498/22
CPC分类号： C07D498/22 , A61K31/519 , C07D471/22 , C07D487/04 , C07D487/22 , C07D519/00
摘要： 식의화합물:및약제학적으로허용가능한그의염, 여기서링 A, 링 B, W, m, D, R, R, R, R, 및 Z은본 명세서에서정의된바와같음, 은 Trk 키나제의저해제이고통증, 암, 염증, 신경퇴행성질환및 특정의감염성질환의치료에서유용하다.

9. 发明专利

JP2014139249A Mitotic kinesin inhibitor and method for using the same 有权
标题翻译： MITOTIC KINESIN INHIBITOR及其使用方法
公开(公告)号：JP2014139249A
公开(公告)日：2014-07-31
申请号：JP2014094479
申请日：2014-05-01
申请人： Array Biopharma Inc , アレイバイオファーマ、インコーポレイテッド
发明人： HANS JEREMY , ELI M WALLACE , ZHAO QIAN , LYSSIKATOS JOSEPH P , AICHER TOM , LAIRD ELLEN , ROBINSON JOHN , ALLEN SHELLEY
IPC分类号： C07D271/10 , A61K31/4245 , A61K31/433 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , A61P1/00 , A61P19/02 , A61P31/00 , A61P35/00 , A61P37/02 , A61P37/06 , A61P43/00 , C07D285/12 , C07D413/04 , C07D413/06 , C07D417/06 , C07D417/12 , C07F9/6539
CPC分类号： C07D285/12 , C07D271/107 , C07D401/12 , C07D413/04 , C07D413/06 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/12 , C07F9/201 , C07F9/65392
摘要： PROBLEM TO BE SOLVED: To provide new inhibitors for mitotic kinesin, more concretely, for the mitotic kinesin KSP, pharmaceutical compositions comprising the inhibitors, and methods for preparing the inhibitors.SOLUTION: Provided are inhibitors for mitotic kinesin, concretely, for KSP, and a method for producing the inhibitors. Also provided are a pharmaceutical composition comprising the inhibitor, and a method of utilizing the inhibitors and the pharmaceutical composition in the treatment and prevention of various disorders. The compound has usefulness as therapeutic agents for disease treatable by the inhibition of the assembly and/or function of microtubule structures including a mitotic spindle.
摘要翻译：要解决的问题：为有丝分裂驱动蛋白提供新的抑制剂，更具体地，对于有丝分裂驱动蛋白KSP，包含抑制剂的药物组合物和制备抑制剂的方法。解决方案：提供有丝分裂驱动蛋白的抑制剂，具体地，用于KSP，和制备抑制剂的方法。还提供了包含抑制剂的药物组合物，以及利用抑制剂和药物组合物治疗和预防各种疾病的方法。该化合物作为用于通过抑制包含有丝分裂纺锤体的微管结构的组装和/或功能可治疗的疾病的治疗剂是有用的。

10. 发明专利

JP2014129409A Triazolopyridine compound as pim kinase inhibitor 审中-公开
标题翻译：三唑吡啶化合物作为PIM激酶抑制剂
公开(公告)号：JP2014129409A
公开(公告)日：2014-07-10
申请号：JP2014044674
申请日：2014-03-07
申请人： Array Biopharma Inc , アレイバイオファーマ、インコーポレイテッド
发明人： ALLEN SHELLEY , LAURA L CELESTE , T GREGG DAVIS , ROBERT KIRK DELISLE , JULIE MARIE GRESCHUK , STEFAN D GROSS , ERIK JAMES HICKEN , LEILA J JACKSON , LYSSIKATOS JOSEPH P , KALLEN NICHOLAS C , MARMSATER FREDRIK P , MUNSON MARK C , JED PHENEGER , RAST BRYSON , JOHN E ROBINSON , STEPHEN T SCHLACHTER , GEORGE T TOPALOV , A DALE WRIGHT , ZHAO QIAN
IPC分类号： C07D471/04 , A61K31/4709 , A61K31/55 , A61P1/04 , A61P17/00 , A61P25/00 , A61P29/00 , A61P35/00 , A61P37/06 , A61P43/00 , C07D519/00
CPC分类号： C07D471/04
摘要： PROBLEM TO BE SOLVED: To provide a novel triazolopyridine compound having a PIM kinase inhibition effect and useful for treatment of cancer, autoimmune disease, inflammatory disease and the like.SOLUTION: There is provided a compound represented by the formula I or pharmaceutically acceptable salt thereof. I, where A represents a C1 to 3 alkyloxy substituted by 4 to 7-membered heterocycle and the like, a C1 to 6 alkyloxy substituted by amino and the like, an amino substituted by 4 to 7-membered heterocycle and the like, and the like, B, Rto Rand Rare each independently H, F, Me and the like. cis-3-fluoropiperidine-4-yloxy, piperidine-3-ylmethoxy, 3-amino-2,2-dimethylpropane-1-yloxy, (piperidine-4-yl)amino and the like are preferable as the A.
摘要翻译：要解决的问题：提供具有PIM激酶抑制作用的新型三唑并吡啶化合物，可用于治疗癌症，自身免疫疾病，炎症性疾病等。溶液：提供由式I表示的化合物或其药学上可接受的盐。 I，其中A表示被4至7元杂环等取代的C1至3烷氧基，由氨基等取代的C1至6烷氧基，由4-至7-元杂环取代的氨基等，像B，Rto Rand Rare各自独立地是H，F，Me等。顺式-3-氟哌啶-4-基氧基，哌啶-3-基甲氧基，3-氨基-2,2-二甲基丙烷-1-基氧基，（哌啶-4-基）氨基等优选为A.

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