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1. 发明申请

WO2015143652A8 TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF 审中-公开
标题翻译： TrkA激酶抑制剂，其组合物及其方法
公开(公告)号：WO2015143652A8
公开(公告)日：2015-12-10
申请号：PCT/CN2014074143
申请日：2014-03-26
申请人： MERCK SHARP & DOHME , MITCHELL HELEN , FRALEY MARK E , COOKE ANDREW J , STUMP CRAIG A , BESHORE DOUGLAS C , MCCOMAS CASEY C , SCHIRRIPA KATHY , MCWHERTER MELODY , ZHANG XU-FANG , MERCER SWATI P , MOORE KEITH , LIU CHUNGSING , MAO QINGHAU
发明人： MITCHELL HELEN , FRALEY MARK E , COOKE ANDREW J , STUMP CRAIG A , BESHORE DOUGLAS C , MCCOMAS CASEY C , SCHIRRIPA KATHY , MCWHERTER MELODY , ZHANG XU-FANG , MERCER SWATI P , MOORE KEITH , LIU CHUNGSING , MAO QINGHAU
IPC分类号： C07D235/00 , A61K31/16 , A61P29/00 , C07D263/52 , C07D275/04 , C07D277/60 , C07D285/14 , C07D291/08
CPC分类号： C07D403/12 , C07D401/12 , C07D403/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention is directed to a bicyclic heteroaryl benzamide compounds of formula(I) which are tropomyosin-related kinase(Trk)family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF)receptor TrkA.
摘要翻译：本发明涉及式（I）的双环杂芳基苯甲酰胺化合物，其是原肌球蛋白相关激酶（Trk）家族蛋白激酶抑制剂，因此可用于治疗疼痛，炎症，癌症，再狭窄，动脉粥样硬化，牛皮癣，与神经生长因子（NGF）受体TrkA的异常活动相关的血栓形成，疾病，障碍，损伤或与脱髓鞘或脱髓鞘相关的疾病或障碍。

2. 发明申请

WO2015148373A3 TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF 审中-公开
公开(公告)号：WO2015148373A3
公开(公告)日：2015-11-26
申请号：PCT/US2015022004
申请日：2015-03-23
申请人： MERCK SHARP & DOHME , MITCHELL HELEN , FRALEY MARK E , COOKE ANDREW J , STUMP CRAIG A , CHEN YI HENG , BESHORE DOUGLAS C , ZHANG XU-FANG , MCCOMAS CASEY C , SCHIRRIPA KATHY , MCWHERTER MELODY , MERCER SWATI P , MOORE KEITH P , LIU PING , WOOD HAROLD B , LI CHUN SING , MAO QINGHUA
发明人： MITCHELL HELEN , FRALEY MARK E , COOKE ANDREW J , STUMP CRAIG A , CHEN YI HENG , BESHORE DOUGLAS C , ZHANG XU-FANG , MCCOMAS CASEY C , SCHIRRIPA KATHY , MCWHERTER MELODY , MERCER SWATI P , MOORE KEITH P , LIU PING , WOOD HAROLD B , LI CHUN SING , MAO QINGHUA
IPC分类号： A61K31/166
CPC分类号： C07D403/12 , C07D401/12 , C07D403/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention is directed to a bicyclic heteroaryl benzamide compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.

3. 发明申请

WO2015148344A2 TRKA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF 审中-公开
标题翻译： TRKA激酶抑制剂，其组合物及其方法
公开(公告)号：WO2015148344A2
公开(公告)日：2015-10-01
申请号：PCT/US2015021936
申请日：2015-03-23
申请人： MERCK SHARP & DOHME , MSD R & D CHINA CO LTD , MITCHELL HELEN , FRALEY MARK E , COOKE ANDREW J , CHEN YI-HENG , STUMP CRAIG A , ZHANG XU-FANG , MCCOMAS CASEY C , SCHIRRIPA KATHY , MCWHERTER MELODY , MERCER SWATI P , BABAOGLU KERIM , MENG DONGFANG , WU JANE , LIU PING , WOOD HAROLD B , BAO JIANMING , LI CHUN SING , MAO QINGHUA , QI ZHIQI
发明人： MITCHELL HELEN , FRALEY MARK E , COOKE ANDREW J , CHEN YI-HENG , STUMP CRAIG A , ZHANG XU-FANG , MCCOMAS CASEY C , SCHIRRIPA KATHY , MCWHERTER MELODY , MERCER SWATI P , BABAOGLU KERIM , MENG DONGFANG , WU JANE , LIU PING , WOOD HAROLD B , BAO JIANMING , LI CHUN SING , MAO QINGHUA , QI ZHIQI
IPC分类号： C07D471/04
CPC分类号： C07D491/107 , C07C233/66 , C07D213/75 , C07D231/12 , C07D239/42 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
摘要： The present invention is directed to six membered heteroaryl benzamide compounds of formula (I), which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
摘要翻译：本发明涉及式（I）的六元杂芳基苯甲酰胺化合物，其为原肌球蛋白相关激酶（Trk）家族蛋白激酶抑制剂，因此可用于治疗疼痛，炎症，癌症，再狭窄，动脉粥样硬化，牛皮癣，血栓形成，疾病，障碍，损伤或与神经生长因子（NGF）受体TrkA的异常活动相关的疾病或病症相关的异常髓鞘或脱髓鞘相关的功能障碍。

4. 发明申请

WO2015143654A1 TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF 审中-公开
标题翻译： TrkA激酶抑制剂，组合物及其方法
公开(公告)号：WO2015143654A1
公开(公告)日：2015-10-01
申请号：PCT/CN2014074145
申请日：2014-03-26
申请人： MERCK SHARP & DOHME , MITCHELL HELEN , FRALEY MARK E , COOKE ANDREW J , STUMP CRAIG A , SCHIRRIPA KATHY , ZHANG XU-FANG , MCWHERTER MELODY , LIU CHUNGSING , MAO QINGHAU
发明人： MITCHELL HELEN , FRALEY MARK E , COOKE ANDREW J , STUMP CRAIG A , SCHIRRIPA KATHY , ZHANG XU-FANG , MCWHERTER MELODY , LIU CHUNGSING , MAO QINGHAU
IPC分类号： C07D213/00 , A61K31/16 , A61P29/00 , C07D221/00 , C07D239/02 , C07D241/02 , C07D251/02 , C07D265/00 , C07D279/00
CPC分类号： C07D491/107 , C07C233/66 , C07D213/75 , C07D231/12 , C07D239/42 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
摘要： The present invention is directed to six membered heteroaryl benzamide compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
摘要翻译：本发明涉及式（I）的六元杂芳基苯甲酰胺化合物，它们是原肌球蛋白相关激酶（Trk）家族蛋白激酶抑制剂，因此可用于治疗疼痛，炎症，癌症，再狭窄，动脉粥样硬化，牛皮癣，血栓形成，与髓鞘形成障碍或脱髓鞘有关的疾病，病症，损伤或功能障碍或与神经生长因子（NGF）受体TrkA的异常活性有关的疾病或病症。

5. 发明申请

WO2015148350A3 TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF 审中-公开
标题翻译： TrkA激酶抑制剂，其组合物及其方法
公开(公告)号：WO2015148350A3
公开(公告)日：2015-11-26
申请号：PCT/US2015021944
申请日：2015-03-23
申请人： MERCK SHARP & DOHME , MITCHELL HELEN , FRALEY MARK E , COOKE ANDREW J , STUMP CRAIG A , ZHANG XU-FANG , MCCOMAS CASEY C , SCHIRRIPA KATHY , MCWHERTER MELODY , LIU PING , PARKER DANN , LI CHUN SING , MAO QINGHUA
发明人： MITCHELL HELEN , FRALEY MARK E , COOKE ANDREW J , STUMP CRAIG A , ZHANG XU-FANG , MCCOMAS CASEY C , SCHIRRIPA KATHY , MCWHERTER MELODY , LIU PING , PARKER DANN , LI CHUN SING , MAO QINGHUA
IPC分类号： A61K31/166
CPC分类号： C07D487/04 , C07D231/40 , C07D277/46 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
摘要： The present invention is directed to substituted five membered heteroaryl benzamide compounds of formula (I) (Formula (I)) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
摘要翻译：本发明涉及作为原肌球蛋白相关激酶（Trk）家族蛋白激酶抑制剂的式（I）（式（I））的取代的五元杂芳基苯甲酰胺化合物，因此可用于治疗疼痛，炎症，癌症，再狭窄，动脉粥样硬化，牛皮癣，血栓形成，疾病，障碍，损伤或与神经生长因子（NGF）受体TrkA的异常活动相关的疾病或病症相关的异常髓鞘或脱髓鞘的功能障碍。

6. 发明申请

WO2015148354A2 TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF 审中-公开
标题翻译： TrkA激酶抑制剂，组合物及其方法
公开(公告)号：WO2015148354A2
公开(公告)日：2015-10-01
申请号：PCT/US2015021952
申请日：2015-03-23
申请人： MERCK SHARP & DOHME , MITCHELL HELEN , WOOD HAROLD B , LI CHUN SING , MAO QINGHUA , QI ZHIQI
发明人： MITCHELL HELEN , WOOD HAROLD B , LI CHUN SING , MAO QINGHUA , QI ZHIQI
IPC分类号： A61K31/506 , C07D471/04
CPC分类号： C07D403/12 , C07D401/12 , C07D403/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention is directed to a bicyclic heteroaryl benzamide compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
摘要翻译：本发明涉及式（I）的双环杂芳基苯甲酰胺化合物，其为原肌球蛋白相关激酶（Trk）家族蛋白激酶抑制剂，因此可用于治疗疼痛，炎症，癌症，再狭窄，动脉粥样硬化，牛皮癣，血栓形成，与髓鞘形成障碍或脱髓鞘有关的疾病，病症，损伤或功能障碍或与神经生长因子（NGF）受体TrkA的异常活性有关的疾病或病症。

7. 发明申请

WO2013169574A2 ALIPHATIC SPIROLACTAM CGRP RECEPTOR ANTAGONISTS 审中-公开
标题翻译： ALIPHATIC SPIROLACTAM CGRP受体拮抗剂
公开(公告)号：WO2013169574A2
公开(公告)日：2013-11-14
申请号：PCT/US2013039373
申请日：2013-05-03
申请人： MERCK SHARP & DOHME , BELL IAN M , FRALEY MARK , BIFTU TESFAYE , ZHU CHENG , NAIR ANILKUMAR , MITCHELL HELEN
发明人： BELL IAN M , FRALEY MARK , BIFTU TESFAYE , ZHU CHENG , NAIR ANILKUMAR , MITCHELL HELEN
IPC分类号： A61K31/55
CPC分类号： C07D471/20 , A61K9/4858 , A61K31/45 , A61K31/451 , A61K31/4523
摘要： The present invention is directed to aliphatic spirolactam derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical\compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
摘要翻译：本发明涉及作为CGRP受体的拮抗剂的脂族螺内酰胺衍生物，其可用于治疗或预防涉及CGRP的疾病，例如偏头痛。本发明还涉及包含这些化合物的药物\组合物以及这些化合物和组合物在预防或治疗涉及CGRP的疾病中的用途。

8. 发明专利

ES2525021T3 Antagonistas del receptor de piperidinona carboxamida azaindano CGRP 未知
公开(公告)号：ES2525021T3
公开(公告)日：2014-12-16
申请号：ES11787987
申请日：2011-11-10
申请人： MERCK SHARP & DOHME
发明人： BELL IAN , FRALEY MARK , GALLICCHIO STEVEN , GINNETTI ANTHONY , MITCHELL HELEN , PAONE DANIEL , STAAS DONNETTE , WANG CHENG , ZARTMAN C BLAIR , STEVENSON HEATHER
IPC分类号： C07D471/10 , A61K31/437 , A61K31/519 , A61P9/08
摘要： compuesto de Fórmula I:**Fórmula** o una sal farmacéuticamente aceptable del 5 mismo, en la que: X se selecciona entre -C(R8)>= o -N>=, en la que R8 es hidrógeno, F o CN; R1 se selecciona entre el grupo que consiste en: alquilo C1-4, ciclopropilmetilo, ciclobutilmetilo y [1-(trifluorometil)ciclopropil]metilo, cada uno de los cuales está opcionalmente sustituido con uno o más sustituyentes según lo permitido por la valencia, seleccionado independientemente entre el grupo que consiste en: F e hidroxilo; R2 se selecciona entre hidrógeno y metilo; cuando R2 es hidrógeno entonces R3 se selecciona entre hidrógeno, F o Cl; R4 se selecciona entre hidrógeno, F o Cl; R5 es hidrógeno; R6 se selecciona entre hidrógeno o F; y R7 se selecciona entre hidrógeno, F o Cl; excepto que al menos dos de R3, R4, R6 y R7 deben ser F o Cl, a menos que R3 sea F en cuyo caso R4, R6 y R7 pueden ser todos hidrógeno; y si R4 es Cl entonces R7 no puede ser Cl; cuando R2 es metilo entonces R3 se selecciona entre hidrógeno, metilo, F, Cl o Br; R4 se selecciona entre hidrógeno, metilo, F o Cl; R5 se selecciona entre hidrógeno o F; R6 se selecciona entre hidrógeno o F; y R2 se selecciona entre hidrógeno, metilo, F o Cl; excepto que si R5 es F entonces al menos tres de R3, R4, R6 y R7 deben ser F; y si R4 es metilo o Cl entonces R7 no puede ser metilo o Cl.

9. 发明专利

SG11202106310YA PYRIMIDONE DERIVATIVES AS SELECTIVE CYTOTOXIC AGENTS AGAINST HIV INFECTED CELLS 未知
公开(公告)号：SG11202106310YA
公开(公告)日：2021-07-29
申请号：SG11202106310Y
申请日：2019-12-13
申请人： MERCK SHARP & DOHME
发明人： CONVERSO ANTONELLA , EL MARROUNI ABDELLATIF , FORSTER ASHLEY , FRIE JESSICA , HUNTER DAVID , KUDUK SCOTT , MITCHELL HELEN , NANTERMET PHILIPPE , SHA DEYOU , SHIPE WILLIAM DANIEL , WANG CHENG , WANG DEPING
IPC分类号： A61K31/505 , C07D239/52 , A61P31/18
摘要： The present disclosure is directed to pyrimidone derivatives of Formula I and their use for selectively killing HIV infected GAG-POL expressing cells without concomitant cytotoxicity to HIV nave cells, and for the treatment or prophylaxis of infection by HIV, or for the treatment, prophylaxis or delay in the onset or progression of AIDS or AIDS Related Complex (ARC).

10. 发明专利

ES2604827T3 Antagonistas del receptor de piperidinona carboxamida azaindano CGRP 未知
公开(公告)号：ES2604827T3
公开(公告)日：2017-03-09
申请号：ES14185954
申请日：2011-11-10
申请人： MERCK SHARP & DOHME
发明人： BELL IAN , FRALEY MARK , GALLICCHIO STEVEN , GINNETTI ANTHONY , MITCHELL HELEN , PAONE DANIEL , STAAS DONNETTE , WANG CHENG , ZARTMAN C BLAIR , STEVENSON HEATHER
IPC分类号： A61K31/437 , C07D471/10 , A61K31/519 , A61P9/08
摘要： Un compuesto de Fórmula I:**Fórmula** o una sal farmacéuticamente aceptable del mismo, para su uso en el tratamiento agudo o profiláctico de cefalea migrañosa o cefalea en racimo junto con uno o más agentes seleccionados entre: un agente anti-migraña; un agonista de 5-HT1B/1D; un agonista de 5-HT1D; un agonista de 5-HT1F; un inhibidor de la ciclooxigenasa; un agente anti-inflamatorio no estereoideo o un agente anti-inflamatorio supresor de la citocina; un glucocorticoide y un analgésico; en la que: X se selecciona entre -C(R8)>= o -N>=, en donde R8 es hidrógeno, F o CN; R1 se selecciona entre el grupo que consiste en: alquilo C1-4, ciclopropilmetilo, ciclobutilmetilo y [1-(trifluorometil)ciclopropil]metilo, cada uno de los cuales está opcionalmente sustituido con uno o más sustituyentes según lo permitido por la valencia, seleccionado independientemente entre el grupo que consiste en: F e hidroxilo; R2 se selecciona entre hidrógeno y metilo; cuando R2 es hidrógeno entonces R3 se selecciona entre hidrógeno, F o Cl; R4 se selecciona entre hidrógeno, F o Cl; R5 es hidrógeno; R6 se selecciona entre hidrógeno o F; y R7 se selecciona entre hidrógeno, F o Cl; excepto que al menos dos de R3, R4, R6 y R7 deben ser F o Cl, a menos que R3 sea F en cuyo caso R4, R6 y R7 pueden ser todos hidrógeno; y si R4 es Cl entonces R7 no puede ser Cl; cuando R2 es metilo entonces R3 se selecciona entre hidrógeno, metilo, F, Cl o Br; R4 se selecciona entre hidrógeno, metilo, F o Cl; R5 se selecciona entre hidrógeno o F; R6 se selecciona entre hidrógeno o F; y R7 se selecciona entre hidrógeno, metilo, F o Cl; excepto que si R5 es F entonces al menos tres de R3, R4, R6 y R7 deben ser F; y si R4 es metilo o Cl entonces R7 no puede ser metilo o Cl.

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