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1. 发明专利

SG11201707638UA QUINOLINE DERIVATIVES AS TAM RTK INHIBITORS 未知
公开(公告)号：SG11201707638UA
公开(公告)日：2017-10-30
申请号：SG11201707638U
申请日：2016-04-14
申请人： QURIENT CO LTD , LEAD DISCOVERY CENTER GMBH
发明人： NAM KIYEAN , KIM JAESEUNG , AHN SEOHYUN , JEON YEEJIN , LEE DOOHYUNG , PARK DONGSIK , YANG YOUNG-IN , LEE SAEYEON , KIM JEONGJUN , AHN JIYE , KIM HANA , JUNG CHUN-WON , SCHULTZ-FADEMRECHT CARSTEN
IPC分类号： C07D401/14 , A61K31/4709 , A61P35/00 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to novel compounds which are inhibitors of TAM (Axl, Mer and Tyro 3) and/or Met family receptor tyrosine kinases (RTKs). These compounds are suitable for the treatment of disorders associated with, accompanied by, caused by or induced by a receptor of the TAM family, in particular a hyperfunction thereof. The compounds are suitable for the treatment of hyperproliferative disorders, such as cancer, particularly immune-suppressive cancer, refractory cancer and cancer metastases.

2. 发明专利

PH12017501822A1 QUINOLINE DERIVATIVES AS TAM RTK INHIBITORS 未知
公开(公告)号：PH12017501822A1
公开(公告)日：2018-04-23
申请号：PH12017501822
申请日：2017-10-04
申请人： LEAD DISCOVERY CENTER GMBH , QURIENT CO LTD
发明人： NAM KIYEAN , KIM JAESEUNG , AHN SEOHYUN , JEON YEEJIN , LEE DOOHYUNG , PARK DONGSIK , YANG YOUNG-IN , LEE SAEYEON , KIM JEONGJUN , AHN JIYE , KIM HANA , JUNG CHUN-WON , SCHULTZ-FADEMRECHT CARSTEN
IPC分类号： A61K31/4709 , A61P35/00 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to novel compounds which are inhibitors of TAM (Axl, Mer and Tyro 3) and/or Met family receptor tyrosine kinases (RTKs). These compounds are suitable for the treatment of disorders associated with, accompanied by, caused by or induced by a receptor of the TAM family, in particular a hyperfunction thereof. The compounds are suitable for the treatment of hyperproliferative disorders, such as cancer, particularly immune-suppressive cancer, refractory cancer and cancer metastases.

3. 发明专利

AU2016249860B2 Quinoline derivatives as TAM RTK inhibitors 未知
公开(公告)号：AU2016249860B2
公开(公告)日：2019-10-10
申请号：AU2016249860
申请日：2016-04-14
申请人： LEAD DISCOVERY CENTER GMBH , QURIENT CO LTD
发明人： NAM KIYEAN , KIM JAESEUNG , AHN SEOHYUN , JEON YEEJIN , LEE DOOHYUNG , PARK DONGSIK , YANG YOUNG-IN , LEE SAEYEON , KIM JEONGJUN , AHN JIYE , KIM HANA , JUNG CHUN-WON , SCHULTZ-FADEMRECHT CARSTEN
IPC分类号： C07D401/14 , A61K31/4709 , A61P35/00 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to novel compounds which are inhibitors of TAM (Axl, Mer and Tyro 3) and/or Met family receptor tyrosine kinases (RTKs). These compounds are suitable for the treatment of disorders associated with, accompanied by, caused by or induced by a receptor of the TAM family, in particular a hyperfunction thereof. The compounds are suitable for the treatment of hyperproliferative disorders, such as cancer, particularly immune-suppressive cancer, refractory cancer and cancer metastases.

4. 发明专利

ZA201706380B QUINOLINE DERIVATIVES AS TAM RTK INHIBITORS 未知
公开(公告)号：ZA201706380B
公开(公告)日：2022-03-30
申请号：ZA201706380
申请日：2017-09-21
申请人： QURIENT CO LTD , LEAD DISCOVERY CENTER GMBH
发明人： NAM KIYEAN , KIM JAESEUNG , AHN SEOHYUN , JEON YEEJIN , LEE DOOHYUNG , PARK DONGSIK , YANG YOUNG-IN , LEE SAEYEON , KIM JEONGJUN , AHN JIYE , KIM HANA , JUNG CHUN-WON , SCHULTZ-FADEMRECHT CARSTEN
摘要： The present invention relates to novel compounds which are inhibitors of TAM (Axl, Mer and Tyro 3) and/or Met family receptor tyrosine kinases (RTKs). These compounds are suitable for the treatment of disorders associated with, accompanied by, caused by or induced by a receptor of the TAM family, in particular a hyperfunction thereof. The compounds are suitable for the treatment of hyperproliferative disorders, such as cancer, particularly immune-suppressive cancer, refractory cancer and cancer metastases.

5. 发明专利

CA2980652C QUINOLINE DERIVATIVES AS TAM RTK INHIBITORS 未知
公开(公告)号：CA2980652C
公开(公告)日：2021-04-27
申请号：CA2980652
申请日：2016-04-14
申请人： QURIENT CO LTD , LEAD DISCOVERY CENTER GMBH
发明人： NAM KIYEAN , KIM JAESEUNG , AHN SEOHYUN , JEON YEEJIN , LEE DOOHYUNG , PARK DONGSIK , YANG YOUNG-IN , LEE SAEYEON , KIM JEONGJUN , AHN JIYE , KIM HANA , JUNG CHUN-WON , SCHULTZ-FADEMRECHT CARSTEN
IPC分类号： C07D401/14 , A61K31/4709 , A61P35/00 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to novel compounds having TAM family and Met receptor tyrosine kinase-inhibiting activity and having the general formula l: (see formula I). The compounds are suitable for the treatment of infectious, diseases and hyperproliferative disorders, such as cancer, particularly immune-suppressive cancer, refractory cancer and cancer metastases.

6. 发明专利

BR112017021929A2 derivados de quinolina como inibidores tam rtk, composição farmacêutica compreendendo os referidos derivados e uso destes 未知
公开(公告)号：BR112017021929A2
公开(公告)日：2018-07-03
申请号：BR112017021929
申请日：2016-04-14
申请人： LEAD DISCOVERY CENTER GMBH , QURIENT CO LTD
发明人： AHN JIYE , AHN SEOHYUN , CARSTEN SCHULTZ-FADEMRECHT , JEON YEEJIN , JUNG CHUN-WON , KIM HANA , KIM JAESEUNG , KIM JEONGJUN , LEE DOOHYUNG , LEE SAEYEON , NAM KIYEAN , PARK DONGSIK , YANG YOUNG-IN
IPC分类号： C07D401/12 , A61K31/4709 , A61P35/00 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： a presente invenção refere-se aos novos compostos que são inibidores de tam (axl, mer e tyro3) e/ou receptor de família de tirosina quinases (rtks). estes compostos são adequados para o tratamento de distúrbios associados, acompanhados de, causados por ou induzidos por um receptor da família tam, em particular a sua hiperfunção. os compostos são adequados para o tratamento de distúrbios hiperproliferativos, tais como câncer, particularmente câncer imunossurpresivo, câncer refratário e metástases de câncer.

7. 发明公开

EP3286177A1 QUINOLINE DERIVATIVES AS TAM RTK INHIBITORS 有权
公开(公告)号：EP3286177A1
公开(公告)日：2018-02-28
申请号：EP16716247
申请日：2016-04-14
申请人： QURIENT CO LTD , LEAD DISCOVERY CENTER GMBH
发明人： NAM KIYEAN , KIM JAESEUNG , AHN SEOHYUN , JEON YEEJIN , LEE DOOHYUNG , PARK DONGSIK , YANG YOUNG-IN , LEE SAEYEON , KIM JEONGJUN , AHN JIYE , KIM HANA , JUNG CHUNG-WON , SCHULTZ-FADEMRECHT CARSTEN
IPC分类号： C07D401/14 , A61K31/4709 , A61P35/00 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
CPC分类号： C07D401/14 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to novel compounds which are inhibitors of TAM (Axl, Mer and Tyro 3) and/or Met family receptor tyrosine kinases (RTKs). These compounds are suitable for the treatment of disorders associated with, accompanied by, caused by or induced by a receptor of the TAM family, in particular a hyperfunction thereof. The compounds are suitable for the treatment of hyperproliferative disorders, such as cancer, particularly immune-suppressive cancer, refractory cancer and cancer metastases.

8. 发明专利

AU2015295248B2 2-amino-benzimidazole derivatives and their use as 5-lipoxygenase and/or prostaglandin e synthase inhibitors 未知
公开(公告)号：AU2015295248B2
公开(公告)日：2019-05-16
申请号：AU2015295248
申请日：2015-07-31
申请人： PASTEUR INSTITUT KOREA , QURIENT CO LTD
发明人： KIM JAESEUNG , AHN SEOHYUN , JEON YEEJIN , PARK DONGSIK , YANG YOUNG-IN , LEE DOOHYUNG , LEE SAEYEON , AHN JIYE , KIM JEONGJUN , NAM KIYEAN , KANG SUNHEE , SEO MINJUNG , SEO MOOYOUNG , SEO JEONGJEA , HAN SUNG-JUN , KIM JUNG HWAN , LEE SANGCHUL , CHOI GAHEE , LEE YUNMI
IPC分类号： C07D235/20 , A61K31/4184 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04
摘要： The present invention relates to benzimidazole derivatives having the general formula I, wherein n is 0 or 1; X

9. 发明专利

ES2795748T3 Derivados de 2-amino-bencimidazol como inhibidores de 5-lipoxigenasa y/o prostaglandina E sintasa para tratar enfermedades inflamatorias 未知
公开(公告)号：ES2795748T3
公开(公告)日：2020-11-24
申请号：ES15748009
申请日：2015-07-31
申请人： PASTEUR INSTITUT KOREA , QURIENT CO LTD
发明人： KIM JAESEUNG , AHN SEOHYUN , JEON YEEJIN , PARK DONGSIK , YANG YOUNG-IN , LEE DOOHYUNG , LEE SAEYEON , AHN JIYE , KIM JEONGJUN , NAM KIYEAN , KANG SUNHEE , SEO MINJUNG , SEO MOOYOUNG , SEO JEONGJEA , HAN SUNG-JUN , KIM JUNG HWAN , LEE SANGCHUL , CHOI GAHEE , LEE YUNMI
IPC分类号： C07D235/20 , A61K31/4184 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04
摘要： Un compuesto que tiene la fórmula general II: **(Ver fórmula)** Fórmula II en la que n es 0 o 1; X1 es CR5 o N; Y es alquileno C1-C6, en el que el alquileno está opcionalmente sustituido con uno a dos grupos alquilo C1-C3; R5 se selecciona entre el grupo que consiste en hidrógeno, halógeno, alquilo C1-C6, haloalquilo C1-C6 y un grupo alcoxi C1-C6; R23 se selecciona entre el grupo que consiste en alquilo C1-C6, haloalquilo C1-C3, arilo, heteroarilo y un grupo heterociclilo, en el que cada uno de dichos arilo, heteroarilo y heterociclilo está opcional e independientemente sustituido con uno a cuatro grupos Ra; R24 se selecciona entre el grupo que consiste en hidrógeno, cicloalquilo C3-C10, arilo, heteroarilo y un grupo heterociclilo, en el que cada uno de dicho cicloalquilo, arilo, heteroarilo y heterociclilo está opcional e independientemente sustituido con uno a cuatro grupos Ra; R25 se selecciona entre el grupo que consiste en hidrógeno, -(V)pR26 y -(V)p-OR14; en las que, p es 0 o 1, V es alquileno C1-C6, en el que el alquileno está opcionalmente sustituido con uno a tres grupos alquilo C1-C3 o fenilo, o en el que un átomo de carbono de dicho alquileno forma parte de un grupo cicloalquilo C3-C6; R14 se selecciona entre el grupo que consiste en hidrógeno, alquilo C1-C6 y arilo, en el que cada uno de dichos alquilo y arilo está opcional e independientemente sustituido con uno a cuatro grupos halógenos o grupos haloalcoxi C1-C3; R26 se selecciona entre el grupo que consiste en hidrógeno, alquilo C1-C6, -CN y C1-C3 haloalquilo, y grupos de fórmula IIa mostrada a continuación, **(Ver fórmula)** en las que, A2 es -O- o NH-; A3 es -O-, -CH2O-, -OCH2- o -NH-; B se selecciona entre el grupo que consiste en arilo, por ejemplo fenilo o bencilo, heteroarilo y grupo heterociclilo en el que cada uno de dichos arilo, heteroarilo y heterociclilo está opcional e independientemente sustituido con uno a cuatro grupos Ra; R19 se selecciona entre el grupo que consiste en hidrógeno, -OR22 y -CH2OR22; R20 se selecciona entre el grupo que consiste en hidrógeno, halógeno, alquilo C1-C6, alcoxi C1-C6 y haloalcoxi C1- C6; R21 se selecciona entre el grupo que consiste en hidrógeno, halógeno y alquilo C1-C6; R22 se selecciona entre el grupo que consiste en arilo, por ejemplo, fenilo o bencilo, y heteroarilo, en el que cada uno de dichos arilo y heteroarilo está opcional e independientemente sustituido con uno a cuatro grupos Ra; Ra se selecciona independientemente, cada vez que aparece, entre el grupo que consiste en hidrógeno, halógeno, alquilo C1-C3, cicloalquilo C3-C10, alcoxi C1-C4, haloalquilo C1-C4, haloalcoxi C1-C6, hidroxilo, alquilhidroxilo C1-C3, -CH2ORc, -OCH2Rc, -ORc, -CN, NO2, -NRbRc, -C(O)NRbRc, -C(NH)NH2, -C(O)Rc, -C(O)ORc, sulfonilo, sulfóxido, heterociclilo, heteroarilo y arilo, por ejemplo fenilo, bencilo, en el que cada uno de dicho alquilo, haloalquilo, haloalcoxi, alcoxi, cicloalquilo, arilo, heteroarilo y heterociclilo está opcional e independientemente sustituido con uno a cuatro alquilo C1-C3, alcoxi C1-C4, halógeno, haloalquilo C1-C3, -CN, -C(O)NH2, -COOH, -CO2Et y heteroarilo; Rb y Rc se seleccionan independientemente, cada vez que aparece, entre el grupo que consiste en hidrógeno, alquilo C1-C10, cicloalquilo C3-C10, alquil C1-C6-O-alquilo, alquenilo C2-C10, alcoxi C1-C4, alquilhidroxilo C1-C3, cicloalquenilo C3-C10, alquinilo C2-C10, haloalquilo C1-C6, arilo, por ejemplo fenilo o bencilo, heteroarilo y heterociclilo, en el que cada uno de dichos alquilo, alquil-O-alquilo, alquenilo, alcoxi, cicloalquenilo, alquinilo, haloalquilo, cicloalquilo, arilo, heteroarilo y heterociclilo está opcional e independientemente sustituido con uno a cuatro alquilo C1-C3, alcoxi C1-C4, halógeno, haloalquilo C1-C6, haloalcoxi C1-C6, hidroxilo, -C(O)NH2, -COOH, - COOMe, -COOEt, -CN, -NO2, -NH2; o Rb y Rc se conectan entre sí para formar un anillo cíclico o heterocíclico, saturado o insaturado de cuatro, cinco o seis miembros; y sus sales farmacéuticamente aceptables.

10. 发明专利

SG11201700439VA 2-AMINO-BENZIMIDAZOLE DERIVATIVES AND THEIR USE AS 5-LIPOXYGENASE AND/OR PROSTAGLANDIN E SYNTHASE INHIBITORS 未知
公开(公告)号：SG11201700439VA
公开(公告)日：2017-02-27
申请号：SG11201700439V
申请日：2015-07-31
申请人： PASTEUR INSTITUT KOREA , QURIENT CO LTD
发明人： KIM JAESEUNG , AHN SEOHYUN , JEON YEEJIN , PARK DONGSIK , YANG YOUNG-IN , LEE DOOHYUNG , LEE SAEYEON , AHN JIYE , KIM JEONGJUN , NAM KIYEAN , KANG SUNHEE , SEO MINJUNG , SEO MOOYOUNG , SEO JEONGJEA , HAN SUNG-JUN , KIM JUNG HWAN , LEE SANGCHUL , CHOI GAHEE , LEE YUNMI
IPC分类号： C07D235/20 , A61K31/4184 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04
摘要： The present invention relates to benzimidazole derivatives having the general formula I, wherein n is 0 or 1; X1 and X2 are independently, at each occurrence, CR5 or N; Y is C1-C6 alkylene, wherein alkylene is optionally substituted with one to two C1-C3 alkyl groups; R1 is selected from the group consisting of hydrogen, halogen, C1-C6 alkoxy, -NH2, -NHR6, -NR7R8 and -NH-(R9)n-R10, n being 0 or 1; R2 is selected from the group consisting of hydrogen, halogen, C1-C6 alkyl, -NH2, -NHR6, - NR7R8 and -NH-(R9)n-R10; R3 is selected from the group consisting of hydrogen, hydroxyl, OR11, -NR7R8, C1-C6 alkoxy, C1-C6 alkyl, C3-C10 cycloalkyl, C1-C3 haloalkyl, -C(O)NHR11, aryl, heteroaryl and heterocyclyl, wherein each of said cycloalkyl, aryl, heteroaryl and heterocyclyl is optionally and independently substituted with one to four Ra groups; and R4 is selected from the group consisting of -NH2, -N(R12)(V)pR13, - NH(V)p-OR14, -NHC(O)R15, and groups of formula la shown below, and their use in the treatment of diseases, in particular inflammatory diseases, cancer, stroke and/or Alzheimer's disease.

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