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1. 发明专利

MA55516A AGENTS DE DÉGRADATION, À PETITES MOLÉCULES, DE STAT3 未知
公开(公告)号：MA55516A
公开(公告)日：2022-02-09
申请号：MA55516
申请日：2020-03-26
申请人： UNIV MICHIGAN REGENTS
发明人： BAI LONGCHUAN , MCEACHERN DONNA , STUCKEY JEANNE , WANG SHAOMENG , XU RENQI , YANG CHAO-YIE , ZHOU HAIBIN
IPC分类号： A61K31/675 , A61P35/00 , C07F9/6561

2. 发明专利

AU2018251687B2 Covalent small molecule DCN1 inhibitors and therapeutic methods using the same 未知
公开(公告)号：AU2018251687B2
公开(公告)日：2021-07-29
申请号：AU2018251687
申请日：2018-04-10
申请人： UNIV MICHIGAN REGENTS
发明人： WANG SHAOMENG , STUCKEY JEANNE , LIU LIU , LU JIANFENG , ZHOU HAIBIN , RUI LIANGYOU , SUN YI
IPC分类号： C07D277/64 , A61K31/428 , A61P1/16 , C07D405/12
摘要： Small molecule covalent inhibitors of DCNl and compositions containing the same are disclosed. Methods of using the DCNl covalent inhibitors in the treatment of diseases and conditions wherein inhibition of DCNl provides a benefit, like oxidative stress- related diseases and conditions, neurodegenerative diseases and conditions, metabolic disorders, and muscular nerve degeneration, also are disclosed.

3. 发明专利

CA3112340A1 SMALL MOLECULE MENIN INHIBITORS 未知
公开(公告)号：CA3112340A1
公开(公告)日：2020-04-09
申请号：CA3112340
申请日：2019-09-30
申请人： UNIV MICHIGAN REGENTS , AGIOS PHARMACEUTICALS INC
发明人： WANG SHAOMENG , XU SHILIN , AGUILAR ANGELO , HUANG LIYUE , XU TIANFENG , ZHANG MENG , XU RENQI , XU FUMING , ZHOU HAIBIN , LIU TAO
IPC分类号： C07D211/34 , A61K31/445 , A61K31/4523 , A61P35/00 , C07D401/06 , C07D401/14
摘要： The present disclosure provides compounds represented by Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein R1a, R1b, R1c, E, G, and Q are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat cancer or any other disease, condition, or disorder that is responsive to inhibition of menin.

4. 发明专利

AU2020248002A1 Small molecule degraders of STAT3 未知
公开(公告)号：AU2020248002A1
公开(公告)日：2021-10-21
申请号：AU2020248002
申请日：2020-03-26
申请人： UNIV MICHIGAN REGENTS
发明人： WANG SHAOMENG , ZHOU HAIBIN , XU RENQI , BAI LONGCHUAN , MCEACHERN DONNA , STUCKEY JEANNE , YANG CHAO-YIE
IPC分类号： A61P35/00 , A61K31/675 , C07F9/6561
摘要： The present disclosure provides compounds represented by Formula I or Formula VIII: wherein R

5. 发明专利

SG11202101733TA SMALL MOLECULE MENIN INHIBITORS 未知
公开(公告)号：SG11202101733TA
公开(公告)日：2021-03-30
申请号：SG11202101733T
申请日：2019-09-30
申请人： UNIV MICHIGAN REGENTS , AGIOS PHARMACEUTICALS INC
发明人： WANG SHAOMENG , XU SHILIN , AGUILAR ANGELO , HUANG LIYUE , XU TIANFENG , ZHANG MENG , XU RENQI , XU FUMING , ZHOU HAIBIN , LIU TAO
IPC分类号： A61K31/445 , C07D211/34 , A61K31/4523 , A61P35/00 , C07D401/06 , C07D401/14
摘要： The present disclosure provides compounds represented by Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein R1a, R1b, R1c, E, G, and Q are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat cancer or any other disease, condition, or disorder that is responsive to inhibition of menin.

6. 发明专利

AU2018251687A1 Covalent small molecule DCN1 inhibitors and therapeutic methods using the same 未知
公开(公告)号：AU2018251687A1
公开(公告)日：2019-10-24
申请号：AU2018251687
申请日：2018-04-10
申请人： UNIV MICHIGAN REGENTS
发明人： WANG SHAOMENG , STUCKEY JEANNE , LIU LIU , LU JIANFENG , ZHOU HAIBIN , RUI LIANGYOU , SUN YI
IPC分类号： C07D277/64 , A61K31/428 , A61P1/16 , C07D405/12
摘要： Small molecule covalent inhibitors of DCNl and compositions containing the same are disclosed. Methods of using the DCNl covalent inhibitors in the treatment of diseases and conditions wherein inhibition of DCNl provides a benefit, like oxidative stress- related diseases and conditions, neurodegenerative diseases and conditions, metabolic disorders, and muscular nerve degeneration, also are disclosed.

7. 发明专利

AU2012209295B2 Bcl-2/Bcl-xL inhibitors and therapeutic methods using the same 未知
公开(公告)号：AU2012209295B2
公开(公告)日：2016-06-30
申请号：AU2012209295
申请日：2012-01-24
申请人： UNIV MICHIGAN REGENTS
发明人： WANG SHAOMENG , ZHOU HAIBIN , CHEN JIANFANG , AGUILAR ANGELO , MEAGHER JENNIFER LYNN , SUN DUXIN , YANG CHAO-YIE , LIU LIU , BAI LONGCHUAN , MCEACHERM DONNA , STUCKEY JEANNE , LI XIAOQIN
IPC分类号： C07D403/10 , A61K31/496 , A61P35/00 , C07D403/14
摘要： Inhibitors of Bcl-2/Bcl-xL and compositions containing the same are disclosed. Methods of using the Bcl-2/Bcl-xL inhibitors in the treatment of diseases and conditions wherein inhibition of Bcl-2/Bcl-xL provides a benefit, like cancers, also are disclosed.

8. 发明专利

ES2916449T3 Inhibidores de DCN1 de molécula pequeña covalentes y métodos terapéuticos de uso de los mismos 未知
公开(公告)号：ES2916449T3
公开(公告)日：2022-07-01
申请号：ES18720910
申请日：2018-04-10
申请人： UNIV MICHIGAN REGENTS
发明人： WANG SHAOMENG , STUCKEY JEANNE , LIU LIU , LU JIANFENG , ZHOU HAIBIN , RUI LIANGYOU , SUN YI
IPC分类号： C07D277/64 , A61K31/428 , A61P1/16 , C07D405/12
摘要： Un compuesto que tiene una fórmula estructural (III) **(Ver fórmula)** en donde: Ar1 es un anillo aromático o heteroaromático de cinco o seis miembros o un anillo bicíclico aromático o heteroaromático que tiene de 8 a 12 átomos, que incluye hasta cuatro heteroátomos elegidos de N, O y S, en una disposición químicamente estable, opcionalmente sustituido con hasta cuatro sustituyentes R2; R1 se selecciona del grupo que consiste de H, alquilo C1-6, cicloalquilo C3-6, cicloalquilmetileno C3-6, NHMe, N(Me)2, NHEt, NH-ciclopropilo, OMe, OEt, O-ciclopropilo; R2 se seleccionan independientemente del grupo que consiste de halo, CN, N3, CF3, NO2, H, alquilo C1-6, alquilo C1-6 sustituido, alquenilo C2-6, alquenilo C2-6 sustituido, alquinilo C2-6, alquinilo C2-6 sustituido, cicloalquilo C3-6, cicloalquilo C3-6 sustituido, cicloalquenilo C4-6, cicloalquenilo C4-6 sustituido, heterocicloalquilo C4-7, fenilo, fenilo sustituido, heteroarilo monocíclico, heteroarilo monocíclico sustituido, OR5, NR3R4, COOR5, CONR3R4; R3 y R4 se seleccionan independientemente del grupo que consiste de hidrógeno, alquilo C1-6, alilo, cicloalquilo C3-6, heterociclilo C4-7, arilo, heteroarilo, alquilo C1-6-cicloalquilo C3-6, alquilo C1-6-cicloalquenilo C4-6, alquilo C1-6- heterocicloalquilo C4-6, alcarilo C1-6, alquilo C1-6-heteroarilo, acilo C1-6 cicloalquilcarbonilo C3-6, heterocicloalquilcarbonilo C4-7, aroílo, heteroaroílo, o se toman junto con el átomo de nitrógeno al que están unidos para formar un anillo de cuatro a siete miembros, incluyendo opcionalmente cualquier combinación químicamente estable de uno a tres O, C=O, NR5 y S; R5 se selecciona del grupo que consiste de hidrógeno, CF3, CHF2, alquilo C1-6, alilo, propargilo, cicloalquilo C3-6, alquilo C1-6-cicloalquenilo C4-6, heterocicloalquilo C4-7, arilo, heteroarilo, alquilo C1-6-cicloalquilo C3-6, alquilo C1-6- heterocicloalquilo C4-7, alcarilo C1-6, alquilo C1-6-heteroarilo, acilo C1-6, cicloalquilcarbonilo C3-6, heterocicloalquilcarbonilo C4-7, aroílo, heteroaroílo, cada uno opcionalmente sustituido con hasta tres sustituyentes seleccionados independientemente de halo, hidroxi, oxo, tio, tiono, amino, ciano, alcoxi C1-6, alquiltio C1-6, alquilamino C1-6, dialquilamino C1-6, heterocicloalquilo C4-7, arilo y heteroarilo; R6 se selecciona del grupo que consiste de alquilo C1-6, cicloalquilo C3-6, alquenilo C2-6, cicloalquenilo C4-6, heterocicloalquilo C4-7, alquinilo C2-6, alquilo C1-6-cicloalquilo C3-6, alquilo C1-6-cicloalquenilo C4-6, alquilo C1-6- heterocicloalquilo C4-7, arilo, alquilarilo C1-6, heteroarilo, alquilo C1-6-heteroarilo, bicicloalquilo C5-10 y alquilo C1-6- bicicloalquilo C5-10; R9 se selecciona del grupo que consiste de H, alquilo C1-6, alquilo C1-6 sustituido, alquenilo C3-6, alquenilo C3-6 sustituido, alquinilo C3-6, alquinilo C3-6 sustituido, cicloalquilo C3-6, cicloalquilo C3-6 sustituido, cicloalquenilo C4-6 cicloalquenilo C4-6 sustituido, fenilo, fenilo sustituido, heteroarilo monocíclico, heteroarilo monocíclico sustituido o heterocicloalquilo C4-7; o una sal, hidrato o solvato farmacéuticamente aceptable del mismo.

9. 发明专利

PH12021550374A1 SMALL MOLECULE MENIN INHIBITORS 未知
公开(公告)号：PH12021550374A1
公开(公告)日：2021-11-08
申请号：PH12021550374
申请日：2021-02-22
申请人： UNIV MICHIGAN REGENTS , AGIOS PHARMACEUTICALS INC
发明人： WANG SHAOMENG , XU SHILIN , AGUILAR ANGELO , HUANG LIYUE , XU TIANFENG , ZHANG MENG , XU RENQI , XU FUMING , ZHOU HAIBIN , LIU TAO
IPC分类号： A61K31/445 , A61K31/4523 , A61P35/00 , C07D211/34 , C07D401/06 , C07D401/14
摘要： The present disclosure provides compounds represented by Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein R1a, R1b, R1c, E, G, and Q are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat cancer or any other disease, condition, or disorder that is responsive to inhibition of menin.

10. 发明专利

SG11202110449YA SMALL MOLECULE DEGRADERS OF STAT3 未知
公开(公告)号：SG11202110449YA
公开(公告)日：2021-10-28
申请号：SG11202110449Y
申请日：2020-03-26
申请人： UNIV MICHIGAN REGENTS
发明人： WANG SHAOMENG , ZHOU HAIBIN , XU RENQI , BAI LONGCHUAN , MCEACHERN DONNA , STUCKEY JEANNE , YANG CHAO-YIE
IPC分类号： A61K31/675 , A61P35/00 , C07F9/6561
摘要： The present disclosure provides compounds represented by Formula I or Formula VIII: wherein R1a, R1b, M, A, E, QA, and QB are as defined in the specification, and the salts and solvates thereof. Compounds of Formula I are degraders of STAT3 or dedraders of STAT3 and STAT1. Compounds of Formula VIII are inhibitors of STAT3. STAT3 degraders and inhibitors are useful for the treatment of cancer and other diseases.

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