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1. 发明公开

EP2862861A4 PIPERIDINYLPYRAZOLOPYRIDINE DERIVATIVE 失效
标题翻译： PIPERIDINYLPYRAZOLOPYRIDINDERIVAT
公开(公告)号：EP2862861A4
公开(公告)日：2015-04-22
申请号：EP13804804
申请日：2013-06-13
申请人： DAIICHI SANKYO CO LTD
发明人： KOBAYASHI HIDEKI , OHKAWA NOBUYUKI , TAKANO DAISUKE , KUBOTA HIDEKI , ONODA TOSHIO , KANEKO TOSHIO , ARAI MASAMI , TERASAKA NAOKI
IPC分类号： C07D471/04 , A61K31/4545 , A61K31/4709 , A61K31/497 , A61K31/501 , A61K31/506 , A61P3/06 , A61P9/10 , A61P13/12 , A61P43/00
CPC分类号： C07D471/04 , A61K9/0019 , A61K9/0095 , A61K9/2054 , A61K9/2059 , A61K9/4858 , A61K9/4875

2. 发明公开

EP3081566A4 5-HYDROXY-4-(TRIFLUOROMETHYL)PYRAZOLOPYRIDINE DERIVATIVE 有权
标题翻译： 5-羟基-4-（三氟甲基）PYRAZOLOPYRIDINDERIVAT
公开(公告)号：EP3081566A4
公开(公告)日：2017-05-10
申请号：EP14869320
申请日：2014-12-12
申请人： DAIICHI SANKYO CO LTD
发明人： KOBAYASHI HIDEKI , ARAI MASAMI , KANEKO TOSHIO , TERASAKA NAOKI
IPC分类号： C07D471/04 , A61K31/4545 , A61K31/497 , A61K31/501 , A61K31/506 , A61P3/06 , A61P9/04 , A61P9/10 , A61P13/12 , A61P43/00
CPC分类号： C07D471/04
摘要： A compound represented by the general formula (I) or a pharmacologically acceptable salt thereof has an excellent LCAT-activating effect and is useful as an active ingredient in a therapeutic or prophylactic agent for arteriosclerosis, arteriosclerotic heart disease, coronary heart disease (including heart failure, myocardial infarction, angina pectoris, cardiac ischemia, cardiovascular disturbance, and restenosis caused by angiogenesis), cerebrovascular disease (including stroke and cerebral infarction), peripheral vascular disease (including diabetic vascular complications), dyslipidemia, hypo-HDL-cholesterolemia, hyper-LDL-cholesterolemia, or renal disease, particularly, an anti-arteriosclerotic agent, wherein R is an optionally substituted aryl group or an optionally substituted heteroaryl group, and R 1 is a hydrogen atom or a hydroxy group.
摘要翻译：通式（I）表示的化合物或其药理学上可接受的盐具有优异的LCAT活化作用，可用作动脉硬化症，动脉硬化性心脏病，冠心病（包括心力衰竭）的治疗剂或预防剂中的有效成分，心肌梗塞，心绞痛，心脏缺血，心血管紊乱和由血管生成引起的再狭窄），脑血管疾病（包括中风和脑梗塞），外周血管疾病（包括糖尿病血管并发症），血脂异常，低HDL胆固醇血症， LDL胆固醇血症或肾脏疾病，特别是抗动脉硬化剂，其中R是任选取代的芳基或任选取代的杂芳基，并且R 1是氢原子或羟基。

3. 发明专利

CO2021004032A2 Derivado de dinucleótido cíclico novedoso y su conjugado anticuerpo-fármaco 未知
公开(公告)号：CO2021004032A2
公开(公告)日：2021-04-30
申请号：CO2021004032
申请日：2021-03-30
申请人： DAIICHI SANKYO CO LTD
发明人： TSUDA TOSHIFUMI , TABUCHI TOSHIKI , WATANABE HIDEAKI , KOBAYASHI HIROYUKI , ISHIZAKI MASAYUKI , HARA KYOKO , WADA TEIJI , ARAI MASAMI
IPC分类号： A61K31/7084 , A61P35/00 , A61P35/02 , A61P43/00 , C07H21/02 , C07K16/00
摘要： Resumen Se desea el desarrollo de derivados de CDN novedosos que tengan actividad agonista de STING; y agentes terapéuticos y/o métodos terapéuticos que utilicen los derivados de CDN novedosos para enfermedades asociadas con la actividad agonista de STING. Se desea además el desarrollo de agentes terapéuticos y/o métodos terapéuticos capaces de administrar los derivados de CDN novedosos específicamente a células y órganos objetivo para enfermedades asociadas con la actividad agonista de STING. La presente invención proporciona derivados de CDN novedosos que tienen una potente actividad agonista de STING y conjugados de derivados de anticuerpo-CDN que incluyen los derivados de CDN novedosos. [Dibujo seleccionado] Ninguno

4. 发明专利

AU2014362144B2 5-hydroxy-4-(trifluoromethyl)pyrazolopyridine derivative 未知
公开(公告)号：AU2014362144B2
公开(公告)日：2018-05-10
申请号：AU2014362144
申请日：2014-12-12
申请人： DAIICHI SANKYO CO LTD
发明人： KOBAYASHI HIDEKI , ARAI MASAMI , KANEKO TOSHIO , TERASAKA NAOKI
IPC分类号： C07D471/04 , A61K31/4545 , A61K31/497 , A61K31/501 , A61K31/506 , A61P3/06 , A61P9/04 , A61P9/10 , A61P13/12 , A61P43/00
摘要： A compound which has excellent LCAT activation effects, is useful as an active ingredient of a therapeutic or preventive agent for arteriosclerosis, arteriosclerotic cardiovascular disease, coronary heart disease (including heart failure, myocardial infarction, angina, cardiac ischemia, cardiovascular disorder, and angioplastic restenosis), cerebrovascular disease (including cerebral stroke and cerebral infarction), peripheral vascular disease (including diabetic vascular complication), dyslipidemia, low HDL cholesterol, high HDL cholesterol, or kidney disease, in particular, of an anti-arteriosclerosis agent, and is represented by general formula (I) (I) [In the formula, R is an aryl group which may be substituted or a heteroaryl group which may be substituted, and R

5. 发明专利

PH12016501129B1 5-HYDROXY-4-(TRIFLUOROMETHYL)PYRAZOLOPYRIDINE DERIVATIVE 未知
公开(公告)号：PH12016501129B1
公开(公告)日：2016-07-18
申请号：PH12016501129
申请日：2016-06-10
申请人： DAIICHI SANKYO CO LTD
发明人： KOBAYASHI HIDEKI , ARAI MASAMI , KANEKO TOSHIO , TERASAKA NAOKI
IPC分类号： A61K31/501 , A61K31/4545 , A61K31/497 , A61K31/506 , A61P3/06 , A61P9/04 , A61P9/10 , A61P13/12 , A61P43/00 , C07D471/04
摘要： A compound which has excellent LCAT activation effects, is useful as an active ingredient of a therapeutic or preventive agent for arteriosclerosis, arteriosclerotic cardiovascular disease, coronary heart disease (including heart failure, myocardial infarction, angina, cardiac ischemia, cardiovascular disorder, and angioplastic restenosis), cerebrovascular disease (including cerebral stroke and cerebral infarction), peripheral vascular disease (including diabetic vascular complication), dyslipidemia, low HDL cholesterol, high HDL cholesterol, or kidney disease, in particular, of an anti-arteriosclerosis agent, and is represented by general formula (I) (I) [In the formula, R is an aryl group which may be substituted or a heteroaryl group which may be substituted, and R1 is a hydrogen atom or a hydroxyl group.] or a pharmacologically acceptable salt thereof.

6. 发明专利

HK1207375A1 PIPERIDINYLPYRAZOLOPYRIDINE DERIVATIVE 未知
公开(公告)号：HK1207375A1
公开(公告)日：2016-01-29
申请号：HK15108048
申请日：2015-08-19
申请人： DAIICHI SANKYO CO LTD
发明人： KOBAYASHI HIDEKI , OHKAWA NOBUYUKI , TAKANO DAISUKE , KUBOTA HIDEKI , ONODA TOSHIO , KANEKO TOSHIO , ARAI MASAMI , TERASAKA NAOKI
IPC分类号： C07D20060101 , A61K20060101 , A61P20060101
摘要： A compound represented by the general formula (I) or a pharmacologically acceptable salt thereof has an excellent LCAT-activating effect and is useful as an active ingredient in a therapeutic or prophylactic agent for arteriosclerosis, arteriosclerotic heart disease, coronary heart disease (including heart failure, myocardial infarction, angina pectoris, cardiac ischemia, cardiovascular disturbance, and restenosis caused by angiogenesis), cerebrovascular disease (including stroke and cerebral infarction), peripheral vascular disease (including diabetic vascular complications), dyslipidemia, hypo-HDL-cholesterolemia, or renal disease, particularly, an anti-arteriosclerotic agent, wherein R is an optionally substituted aryl group or an optionally substituted heteroaryl group.

7. 发明专利

PH12021550442A1 NOVEL CYCLIC DINUCLEOTIDE DERIVATIVE AND ANTIBODY-DRUG CONJUGATE THEREOF 未知
公开(公告)号：PH12021550442A1
公开(公告)日：2021-11-22
申请号：PH12021550442
申请日：2021-03-02
申请人： DAIICHI SANKYO CO LTD
发明人： TSUDA TOSHIFUMI , TABUCHI TOSHIKI , WATANABE HIDEAKI , KOBAYASHI HIROYUKI , ISHIZAKI MASAYUKI , HARA KYOKO , WADA TEIJI , ARAI MASAMI
IPC分类号： A61K31/7084 , A61K47/65 , A61K47/68 , A61P35/00 , A61P35/02 , A61P43/00 , C07H21/02 , C07K16/00
摘要： [Problem] To develop a novel CDN derivative that has a STING agonist activity, and a therapeutic agent and/or method for treating a disease related to a STING agonist activity by using the novel CDN derivative. Additionally, to develop a therapeutic agent and/or method for treating a disease related to a STING agonist activity that is capable of delivering the novel CDN derivative to a target cell or a target organ. [Solution] According to the present invention, a novel CDN derivative that has a strong STING agonist activity, and an antibody-CDN derivative conjugate that comprises the novel CDN derivative are provided.

8. 发明专利

CA3111397A1 NOVEL CYCLIC DINUCLEOTIDE DERIVATIVE AND ANTIBODY-DRUG CONJUGATE THEREOF 未知
公开(公告)号：CA3111397A1
公开(公告)日：2020-03-12
申请号：CA3111397
申请日：2019-09-06
申请人： DAIICHI SANKYO CO LTD
发明人： TSUDA TOSHIFUMI , TABUCHI TOSHIKI , WATANABE HIDEAKI , KOBAYASHI HIROYUKI , ISHIZAKI MASAYUKI , HARA KYOKO , WADA TEIJI , ARAI MASAMI
IPC分类号： A61K47/68 , A61K31/7084 , A61K47/65 , A61P35/00 , A61P35/02 , A61P43/00 , C07H21/02 , C07K16/00
摘要： [Problem] To develop a novel CDN derivative that has a STING agonist activity, and a therapeutic agent and/or method for treating a disease related to a STING agonist activity by using the novel CDN derivative. Additionally, to develop a therapeutic agent and/or method for treating a disease related to a STING agonist activity that is capable of delivering the novel CDN derivative to a target cell or a target organ. [Solution] According to the present invention, a novel CDN derivative that has a strong STING agonist activity, and an antibody-CDN derivative conjugate that comprises the novel CDN derivative are provided.

9. 发明专利

ES2563861T3 Derivado de piperidinilpirazolopiridina 未知
公开(公告)号：ES2563861T3
公开(公告)日：2016-03-16
申请号：ES13804804
申请日：2013-06-13
申请人： DAIICHI SANKYO CO LTD
发明人： KOBAYASHI HIDEKI , OHKAWA NOBUYUKI , TAKANO DAISUKE , KUBOTA HIDEKI , ONODA TOSHIO , KANEKO TOSHIO , ARAI MASAMI , TERASAKA NAOKI
IPC分类号： C07D471/04 , A61K31/4545 , A61K31/4709 , A61K31/497 , A61K31/501 , A61K31/506 , A61P3/06 , A61P9/10 , A61P13/12 , A61P43/00
摘要： Un compuesto representado por la fórmula general (I) o una sal farmacológicamente aceptable del mismo:**Fórmula** en la que R representa un grupo arilo opcionalmente sustituido (el sustituyente o sustituyentes son de 1 a 3 grupos idénticos o diferentes seleccionados de entre el grupo que consiste en un átomo de halógeno, un grupo alquilo C1-6, un grupo cicloalquilo C3-7, un grupo trifluorometilo, un grupo difluorometoxi, un grupo trifluorometoxi, un grupo ciano, un grupo alcoxi C1-6, un grupo cicloalcoxi C3-7, un grupo fenilo, un grupo alcoxicarbonilo C2-7, un grupo benciloxicarbonilo, un grupo di(alquilo C1-6)aminocarbonilo y un grupo di(alquilo C1-6)amino) o un grupo heteroarilo opcionalmente sustituido (el heteroarilo es un anillo de 5 o de 6 miembros que opcionalmente está condensado adicionalmente con un anillo de benceno; el heteroátomo o heteroátomos en el anillo del grupo heteroarilo son 1 o 2 átomos de nitrógeno, y el anillo opcionalmente contiene adicionalmente un átomo de nitrógeno, átomo de oxígeno o átomo de azufre; el sustituyente o sustituyentes son 1 o 2 grupos idénticos o diferentes seleccionados de entre el grupo que consiste en un átomo de halógeno, un grupo alquilo C1-6, un grupo cicloalquilo C3-7, un grupo trifluorometilo, un grupo difluorometoxi, un grupo trifluorometoxi, un grupo ciano, un grupo alcoxi C1-6, un grupo cicloalcoxi C3-7, un grupo fenilo, un grupo alcoxicarbonilo C2-7, un grupo benciloxicarbonilo, un grupo di(alquilo C1-6)aminocarbonilo y un grupo di(alquilo C1-6)amino; y el grupo heteroarilo está opcionalmente sustituido adicionalmente con un grupo heteroarilo opcionalmente sustituido (el heteroarilo es un anillo de 5 o de 6 miembros que opcionalmente está condensado adicionalmente con un anillo de benceno; el heteroátomo o heteroátomos en el anillo del grupo heteroarilo son 1 o 2 átomos de nitrógeno, y el anillo opcionalmente contiene adicionalmente un de nitrógeno, átomo de oxígeno o átomo de azufre; y el sustituyente o sustituyentes son 1 o 2 grupos idénticos o diferentes seleccionados de entre el grupo que consiste en un átomo de halógeno, un grupo alquilo C1-6, un grupo trifluorometilo, un grupo ciano y un grupo alcoxi C1-6)).

10. 发明专利

AU2866297A Neuraminic acid derivatives, their preparation and their medical use 未知
公开(公告)号：AU2866297A
公开(公告)日：1998-07-02
申请号：AU2866297
申请日：1997-07-16
申请人： DAIICHI SANKYO CO LTD
发明人： HONDA TAKESHI , KOBAYASHI YOSHIYUKI , MASUDA TAKESHI , YAMASHITA MAKOTO , ARAI MASAMI
IPC分类号： C07D311/28 , A61K31/351 , A61P31/12 , A61P31/16 , C07D309/28 , A61K31/35
摘要： Compounds of formula (I): Äin which R is alkyl or haloalkyl; R and R each represents hydrogen or aliphatic acyl; X is hydroxy, halogen, alkoxy, or a group of formula R O-, where R is aliphatic acyl; Y is a group of formula R R N- or R R N-O-, where R and R each is hydrogen or alkyl; and Z is oxygen or sulphurÜ have excellent sialidase inhibitory activity and are therefore useful for the treatment and prevention of influenza and other viral diseases where the replication of the virus is susceptible to sialidase inhibitors.

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