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1. 发明申请

WO2011093684A2 THIENO[3,2-d]PYRIMIDINE DERIVATIVES HAVING INHIBITORY ACTIVITY ON PROTEIN KINASES 审中-公开
标题翻译：具有蛋白激酶抑制活性的THIENO [3,2-d]吡嗪衍生物
公开(公告)号：WO2011093684A2
公开(公告)日：2011-08-04
申请号：PCT/KR2011000664
申请日：2011-01-31
申请人： HANMI HOLDINGS CO LTD , KOREA INST SCI & TECH , CATHOLIC UNIV IND ACAD COOP , SON JUNG BEOM , JUNG SEUNG HYUN , CHOI WHA IL , JUNG YOUNG HEE , CHOI JAE YUL , SONG JI YEON , LEE KYU HANG , LEE JAE CHUL , KIM EUN YOUNG , AHN YOUNG GIL , KIM MAENG SUP , CHOI HWAN GEUN , SIM TAE BO , HAM YOUNG JIN , PARK DONG-SIK , KIM HWAN , KIM DONG-WOOK
发明人： SON JUNG BEOM , JUNG SEUNG HYUN , CHOI WHA IL , JUNG YOUNG HEE , CHOI JAE YUL , SONG JI YEON , LEE KYU HANG , LEE JAE CHUL , KIM EUN YOUNG , AHN YOUNG GIL , KIM MAENG SUP , CHOI HWAN GEUN , SIM TAE BO , HAM YOUNG JIN , PARK DONG-SIK , KIM HWAN , KIM DONG-WOOK
IPC分类号： C07D495/04 , A61P35/00 , C07D409/14 , C07D495/14
CPC分类号： C07D495/04
摘要： The present invention relates to a thieno[3,2-d]pyrimidine derivative of formula (I), or a pharmaceutically acceptable salt, hydrate or solvate thereof, which has an excellent inhibitory activity on protein kinases, and a pharmaceutical composition comprising the same is effective in preventing or treating abnormal cell growth diseases.
摘要翻译：本发明涉及对蛋白激酶具有优异抑制活性的式（I）的噻吩并[3,2-d]嘧啶衍生物或其药学上可接受的盐，水合物或溶剂合物，以及含有该噻吩并[3,2-d] 有效预防或治疗异常细胞生长疾病。

2. 发明申请

WO2011093672A3 BICYCLIC HETEROARYL DERIVATIVES HAVING INHIBITORY ACTIVITY FOR PROTEIN KINASE 审中-公开
标题翻译：具有蛋白激酶抑制活性的双相异构体衍生物
公开(公告)号：WO2011093672A3
公开(公告)日：2012-01-05
申请号：PCT/KR2011000615
申请日：2011-01-28
申请人： HANMI PHARM IND CO LTD , KOREA INST SCI & TECH , JUNG SEUNG HYUN , JUNG YOUNG HEE , CHOI WHA IL , SON JUNG BEOM , JEON EUN JU , YANG IN HO , SONG TAE HUN , LEE MI KYOUNG , KO MYOUNG SIL , AHN YOUNG GIL , KIM MAENG SUP , HAM YOUNG JIN , SIM TAE BO , CHOI HWAN GEUN , HAH JUNG MI , PARK DONG-SIK , KIM HWAN
发明人： JUNG SEUNG HYUN , JUNG YOUNG HEE , CHOI WHA IL , SON JUNG BEOM , JEON EUN JU , YANG IN HO , SONG TAE HUN , LEE MI KYOUNG , KO MYOUNG SIL , AHN YOUNG GIL , KIM MAENG SUP , HAM YOUNG JIN , SIM TAE BO , CHOI HWAN GEUN , HAH JUNG MI , PARK DONG-SIK , KIM HWAN
IPC分类号： C07D487/04 , A61K31/519 , A61P43/00 , C07D495/04
CPC分类号： C07D495/04
摘要： The present invention relates to a novel bicyclic heteroaryl derivative, a pharmaceutically acceptable salt thereof, a hydrate thereof, and a solvate thereof having an improved inhibitory activity for protein kinases, and a pharmaceutical composition for preventing or treating an abnormal cell growth disorder comprising same as an active ingredient.
摘要翻译：本发明涉及对蛋白激酶具有改善的抑制活性的新型双环杂芳基衍生物，其药学上可接受的盐，其水合物及其溶剂合物，以及用于预防或治疗异常细胞生长障碍的药物组合物，活性成分。

3. 发明申请

WO2010064875A3 NOVEL INDAZOLE DERIVATIVES OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF AS PROTEIN KINASE INHIBITORS FOR PROLIFERATIVE DISEASES TREATMENT, AND A PHARMACEUTICAL COMPOSITION CONTAINING THE SAME AS AN ACTIVE INGREDIENT 审中-公开
标题翻译：新颖的吲哚衍生物或其药学上可接受的盐作为蛋白激酶抑制剂用于增殖性疾病治疗，以及含有作为活性成分的药物组合物
公开(公告)号：WO2010064875A3
公开(公告)日：2010-09-10
申请号：PCT/KR2009007247
申请日：2009-12-04
申请人： KOREA INST SCI & TECH , KOREA RES INST CHEM TECH , KOREA RES INST OF BIOSCIENCE , SIM TAE BO , SON JUNG BEOM , KIM HWAN , PARK DONG SIK , CHOI HWAN GEUN , HAM YOUNG JIN , HAH JUNG MI , YOO KYUNG HO , OH CHANG HYUN , LEE SO HA , HA JAE DU , CHO SUNG YUN , KWON BYOUNG-MOG , HAN DONG CHO
发明人： SIM TAE BO , SON JUNG BEOM , KIM HWAN , PARK DONG SIK , CHOI HWAN GEUN , HAM YOUNG JIN , HAH JUNG MI , YOO KYUNG HO , OH CHANG HYUN , LEE SO HA , HA JAE DU , CHO SUNG YUN , KWON BYOUNG-MOG , HAN DONG CHO
IPC分类号： C07D231/56
CPC分类号： C07D413/14 , C07D231/56 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/04 , C07D409/04 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14
摘要： Disclosed are novel indazole derivatives represented by the following Chemical Formula 1 or pharmaceutically acceptable salts, hydrates or solvates thereof, and pharmaceutical compositions for the prevention or treatment of proliferative diseases, containing the same as an active ingredient. Having potent inhibitory effect against protein kinase, such as b-raf, KDR, Fms, Tie2, SAPK2a and Ret, inducing diseases caused by abnormal cell proliferation, the novel indazole derivatives can be used for the prevention or treatment of diseases caused by abnormal cell proliferation.
摘要翻译：公开了由以下化学式1表示的新型吲唑衍生物或其药学上可接受的盐，水合物或溶剂合物，以及用于预防或治疗增殖性疾病的药物组合物，其含有活性成分。具有对蛋白激酶（如b-raf，KDR，Fms，Tie2，SAPK2a和Ret）的有效抑制作用，诱导由异常细胞增殖引起的疾病，该新型吲唑衍生物可用于预防或治疗由异常细胞引起的疾病增殖。

4. 发明申请

WO2011062372A3 2, 4, 7 -SUBSTITUTED THIENO [3, 2 -D] PYRIMIDINE COMPOUNDS AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译： 2,4 - 7 - 作为蛋白激酶抑制剂的三羟基[3，2 -D]吡啶化合物
公开(公告)号：WO2011062372A3
公开(公告)日：2011-11-03
申请号：PCT/KR2010007275
申请日：2010-10-22
申请人： KOREA INST SCI & TECH , SIM TAE BO , HAH JUNG MI , CHOI HWAN GEUN , HAM YOUNG JIN , LEE JUNG HUN , PARK DONG SIK , KIM HWAN
发明人： SIM TAE BO , HAH JUNG MI , CHOI HWAN GEUN , HAM YOUNG JIN , LEE JUNG HUN , PARK DONG SIK , KIM HWAN
IPC分类号： C07D495/04 , A61K31/4365 , A61P35/00 , C07D495/02
CPC分类号： C07D495/04
摘要： Disclosed are a 2,4,7-substituted thieno[3,2-d]pyrimidine compound having a protein kinase inhibition activity, a pharmaceutically acceptable salt, and a pharmaceutical composition for prevention and treatment of diseases caused by abnormal cell growth comprising the compound as an effective ingredient. Since the novel 2,4,7-substituted thieno[3,2-d]pyrimidine compound exhibits superior inhibition activity against various protein kinases involved in growth factor signal transduction, it is useful as an agent for preventing or treating diseases caused by abnormal cell growth.
摘要翻译：公开了具有蛋白激酶抑制活性的2,4,7-取代噻吩并[3,2-d]嘧啶化合物，药学上可接受的盐和用于预防和治疗由异常细胞生长引起的疾病的药物组合物，其包含化合物作为有效成分。由于新的2,4,7-取代噻吩并[3,2-d]嘧啶化合物对参与生长因子信号转导的各种蛋白激酶具有优异的抑制活性，因此可用作预防或治疗由异常细胞引起的疾病生长。

5. 发明申请

WO2011052923A3 NOVEL 1,6-DISUBSTITUTED INDOLE COMPOUNDS AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：新的1,6-二取代吲哚化合物作为蛋白激酶抑制剂
公开(公告)号：WO2011052923A3
公开(公告)日：2011-10-20
申请号：PCT/KR2010007205
申请日：2010-10-20
申请人： KOREA INST SCI & TECH , SIM TAE BO , HAM YOUNG JIN , YOO KYUNG HO , OH CHANG HYUN , HAH JUNG MI , CHOI HWAN GEUN , KIM HWAN , JUN EUN JIN
发明人： SIM TAE BO , HAM YOUNG JIN , YOO KYUNG HO , OH CHANG HYUN , HAH JUNG MI , CHOI HWAN GEUN , KIM HWAN , JUN EUN JIN
IPC分类号： C07D403/04 , A61K31/40 , A61P35/00 , C07D209/04
CPC分类号： C07D403/04 , A61K31/404 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D487/04
摘要： Disclosed are a 1,6-substituted indole compound having a protein kinase inhibition activity, a pharmaceutically acceptable salt, and a pharmaceutical composition for prevention and treatment of cancers caused by abnormal cell growth comprising the compound as an effective ingredient. Since the novel indole compound exhibits superior inhibition activity against various protein kinases involved in growth factor signal transduction, it is useful as an agent for preventing or treating cancers caused by abnormal cell growth.
摘要翻译：本发明公开了一种具有蛋白激酶抑制活性的1,6-取代的吲哚化合物，其药学上可接受的盐以及用于预防和治疗由异常细胞生长引起的癌症的药物组合物，其包含该化合物作为有效成分。由于该新型吲哚化合物对参与生长因子信号转导的各种蛋白激酶具有优良的抑制活性，因此它可用作预防或治疗由异常细胞生长引起的癌症的药物。

6. 发明申请

WO2011049332A2 2,7-SUBSTITUTED THIENO[3,2-D]PYRIMIDINE COMPOUNDS AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译： 2,7-取代的噻吩并[3,2-D]吡啶化合物作为蛋白激酶抑制剂
公开(公告)号：WO2011049332A2
公开(公告)日：2011-04-28
申请号：PCT/KR2010007093
申请日：2010-10-15
申请人： KOREA INST SCI & TECH , SIM TAE BO , CHOI HWAN GEUN , HAH JUNG MI , HAM YOUNG JIN , JUN EUN JIN , LEE JUNG HUN , KIM HWAN
发明人： SIM TAE BO , CHOI HWAN GEUN , HAH JUNG MI , HAM YOUNG JIN , JUN EUN JIN , LEE JUNG HUN , KIM HWAN
IPC分类号： C07D495/04 , A61K31/505 , A61P35/00 , C07D495/02
CPC分类号： C07D495/04 , C07D519/00
摘要： Disclosed are a 2,7-substituted thieno[3,2-d]pyrimidine compound having a protein kinase inhibition activity, a pharmaceutically acceptable salt, and a pharmaceutical composition for prevention and treatment of diseases caused by abnormal cell growth comprising the compound as an effective ingredient. Since the novel 2,7-substituted thieno[3,2-d]pyrimidine compound exhibits superior inhibition activity against various protein kinases involved in growth factor signal transduction, it is useful as an agent for preventing or treating diseases caused by abnormal cell growth.
摘要翻译：公开了具有蛋白激酶抑制活性的2,7-取代的噻吩并[3,2-d]嘧啶化合物，药学上可接受的盐和用于预防和治疗由异常细胞生长引起的疾病的药物组合物，其包含作为有效成分。由于新的2,7-取代的噻吩并[3,2-d]嘧啶化合物对参与生长因子信号转导的各种蛋白激酶具有优异的抑制活性，因此可用作预防或治疗异常细胞生长引起的疾病的药剂。

7. 发明公开

EP2528925A4 THIENO[3,2-d]PYRIMIDINE DERIVATIVES HAVING INHIBITORY ACTIVITY ON PROTEIN KINASES 有权
标题翻译： THIENO- [3,2-D-] PYRIMIDIN-DERIVATE MIT HEMMENDER WIRKUNG AUF PROTEINKINASEN
公开(公告)号：EP2528925A4
公开(公告)日：2013-07-31
申请号：EP11737323
申请日：2011-01-31
申请人： HANMI SCIENCE CO LTD , KOREA INST SCI & TECH , CATHOLIC UNIV IND ACAD COOP
发明人： SON JUNG BEOM , JUNG SEUNG HYUN , CHOI WHA IL , JUNG YOUNG HEE , CHOI JAE YUL , SONG JI YEON , LEE KYU HANG , LEE JAE CHUL , KIM EUN YOUNG , AHN YOUNG GIL , KIM MAENG SUP , CHOI HWAN GEUN , SIM TAE BO , HAM YOUNG JIN , PARK DONG-SIK , KIM HWAN , KIM DONG-WOOK
IPC分类号： C07D495/04 , A61P35/00 , C07D409/14 , C07D495/14
CPC分类号： C07D495/04

8. 发明专利

ES2636262T3 Derivados de tieno[3,2-d]pirimidina que tienen actividad inhibidora en las proteínas cinasas 未知
公开(公告)号：ES2636262T3
公开(公告)日：2017-10-05
申请号：ES11737323
申请日：2011-01-31
申请人： HANMI SCIENCE CO LTD , KOREA INST SCI & TECH , CATHOLIC UNIV IND ACAD COOP FOUND
发明人： SON JUNG BEOM , JUNG SEUNG HYUN , CHOI WHA IL , JUNG YOUNG HEE , CHOI JAE YUL , SONG JI YEON , LEE KYU HANG , LEE JAE CHUL , KIM EUN YOUNG , AHN YOUNG GIL , KIM MAENG SUP , CHOI HWAN GEUN , SIM TAE BO , HAM YOUNG JIN , PARK DONG-SIK , KIM HWAN , KIM DONG-WOOK
IPC分类号： C07D495/04 , A61P35/00 , C07D409/14 , C07D495/14
摘要： Un compuesto seleccionado del grupo que consiste en un derivado de tieno[3,2-d] pirimidina de fórmula (I), y una sal farmacéuticamente aceptable, hidrato y solvato del mismo: en la que, Y es -CH>=CR1-, -CC-, o -C(>=O)NR1-; L es -C(>=O)NR2-, -NR2C(>=O)-, o -NR2C(>=O)NR2-; cada uno de R1 y R2 es independientemente H, alquilo C1-6, o cicloalquilo C3-8; R es H, halógeno, metilo, o metoxi; E es arilo de hasta 14 átomos de C, que está sin sustituir o sustituido por 1 a 3 sustituyentes seleccionados entre el grupo que consiste en halógeno, -NO2, -CN, -NH2, -OH, -CF3, alquilo C1-6, hidroxi-alquilo C1-6, cicloalquilo C3-8, -(CH2)n-alquilamino C1-6, -(CH2)n-dialquilamino C1-6, -(CH2)nalcoxi C1-6,-(CH2)n-OS(>=O)2-alquilo C1-6, -(CH2)n-Q, donde Q es arilo de hasta 14 átomos de C y -(CH2)n-heterocicloalquilo C2-13, en la que n es un número entero de 0 a 3, y el arilo y heterocicloalquilo están cada uno independientemente sin sustituir o sustituido con un sustituyente seleccionado entre el grupo que consiste en alquilo C1-6, hidroxi-alquilo C1-6, halógeno, dialquilamino C1-6, y alcoxi C1-6; o E es fenilo, piridinilo, quinolinilo, isoquinolinilo, indolilo, isoxazlilo, o pirazolilo, que está sin sustituir o sustituido por 1 a 3 sustituyentes seleccionados entre el grupo que consiste en halógeno, -NO2, -CN, -NH2, -OH, -CF3, alquilo C1-6, cicloalquilo C3-8, -(CH2)n-alquilamino C1-6, -(CH2)n-dialquilamino C1-6, -(CH2)nalcoxi C1-6, -(CH2)n- OS(>=O)2-alquilo C1-6, -(CH2)n-Q, donde Q es arilo de hasta 14 átomos de C y -(CH2)n-heterocicloalquilo C2-13, en la que n es un número entero de 0 a 3; y Z es H, -C(>=O)R3, alquilo C1-6, hidroxialquilo C1-6, cicloalquilo C3-8, heterocicloalquilo C2-7, arilo de hasta 14 átomos de C, en la que el arilo y heterocicloalquilo están cada uno independientemente sin sustituir o sustituido por alquilo C1-6, alcoxi C1-6, cicloalquilo C3-8, R3-heterocicloalquilo C2-7 o heterocicloalquilo C2-7, y R es alquilo C1-6, cicloalquilo C3-6, o fenilo.

9. 发明专利

RU2524210C2 ПРОИЗВОДНЫЕ ТИЕНО[3,2-d]ПИРИМИДИНА, ОБЛАДАЮЩИЕ ИНГИБИРУЮЩЕЙ АКТИВНОСТЬЮ В ОТНОШЕНИИ ПРОТЕИНКИНАЗЫ 未知
公开(公告)号：RU2524210C2
公开(公告)日：2014-07-27
申请号：RU2012132426
申请日：2011-01-31
申请人： HANMI SCIENCE CO LTD , KOREA INST SCI & TECH , CATHOLIC UNIV IND ACAD COOP
发明人： SON DZUNG BEOM , DZUNG SEUNG KHIUN , CHOJ VA IL , DZUNG JOUNG KHEE , CHOJ DZAE JUL , SONG DZI JEON , LI KIU KHANG , LI DZAE CHUL , KIM EUN JOUNG , AKHN JUNG GIL , KIM MAENG SUP , CHOJ KHVAN GEUN , SIM TAE BO , KHAM JOUNG DZIN , PARK DONG-SIK , KIM KHVAN , KIM DONG-VOOK
IPC分类号： C07D495/04 , A61K31/496 , A61K31/519 , A61K31/5377 , A61K31/551 , A61P35/00
摘要： Изобретениеотноситсяк производномутиено[3,2-d]пиримидинаформулы (I) илик егофармацевтическиприемлемойсоли:, где Y обозначает -CH=CR-, -C≡C- или -C(=O)NR-; L обозначает -C(=O)NR-, -NRC(=O)- или -NRC(=O)NR-;Rи R, каждыйнезависимо, обозначает H; R обозначает H, атомгалогена, метилилиметокси; E обозначаетфенилили Cгетероарил, которыйявляетсянезамещеннымилизамещенным 1-2 заместителями, состоящимиизгруппы, включающейатомгалогена, -CF, Cалкил, гидрокси-Cалкил, Cциклоалкил, -(CH)-Cалкиламино, -(CH)-диCалкиламино, -(CH)Cалкокси, -(CH)-OS(=O)-C-алкил, -(CH)-фенил, -(CH)-Cгетероарили -(CH)-Cгетероциклоалкил, где Cгетероарилпредставляетсобойпиридин, изохинолин, индолилиизоксазол, Cгетероарилрадикала -(CH)-Cгетероарилпредставляетсобойимидазолилипиррол, Cгетероциклоалкилрадикала -(CH)-Cгетероциклоалкилпредставляетсобойпиперазин, морфолин, диазепан, пирролидинилипиперидин, ифенил, гетероарили гетероциклоалкил, каждыйнезависимо, являетсянезамещеннымилизамещеннымзаместителем, выбраннымизгруппы, состоящейиз Cалкила, гидрокси-Cалкила, атомагалогенаи диCалкиламино, n равно 0 или 1; и Z обозначает H, -C(=O)R, Cалкил, гидроксиCалкил, Cциклоалкил, пиперидин, фенилилипиридин, гдепиперидин, фенили пиридин, каждыйнезависимо, являетсянезамещеннымилизамещенным Cалкилом, Cалкоксиили R-пиперазиниломи Rпредставляетсобой Cалкилилифенил. Изобретениетакжеотноситсяк промежуточномусоединениюдляполученияуказанногоконечногосоединенияформулы (I). Техническийрезультат: полученоновоесоединение, котороеможетнайтиприменениев медицинедляпредупрежденияилилечениязаболеваний, характеризующихсяаномальнымростомклетокв результатечрезмернойэкспр

10. 发明专利

AU2011210116A1 Thieno[3,2-d]pyrimidine derivatives having inhibitory activity on protein kinases 未知
公开(公告)号：AU2011210116A1
公开(公告)日：2012-07-19
申请号：AU2011210116
申请日：2011-01-31
申请人： HANMI SCIENCE CO LTD , KOREA INST SCI & TECH , CATHOLIC UNIV IND ACAD COOP
发明人： SON JUNG BEOM , JUNG SEUNG HYUN , CHOI WHA IL , JUNG YOUNG HEE , CHOI JAE YUL , SONG JI YEON , LEE KYU HANG , LEE JAE CHUL , KIM EUN YOUNG , AHN YOUNG GIL , KIM MAENG SUP , CHOI HWAN GEUN , SIM TAE BO , HAM YOUNG JIN , PARK DONG-SIK , KIM HWAN , KIM DONG-WOOK
IPC分类号： C07D495/04 , A61P35/00 , C07D409/14 , C07D495/14
摘要： The present invention relates to a thieno[3,2-d]pyrimidine derivative of formula (I), or a pharmaceutically acceptable salt, hydrate or solvate thereof, which has an excellent inhibitory activity on protein kinases, and a pharmaceutical composition comprising the same is effective in preventing or treating abnormal cell growth diseases.

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