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1. 发明授权

EP2862861B1 PIPERIDINYLPYRAZOLOPYRIDINE DERIVATIVE 失效
标题翻译：哌啶基吡唑并吡啶衍生物
公开(公告)号：EP2862861B1
公开(公告)日：2016-01-06
申请号：EP13804804.6
申请日：2013-06-13
申请人： Daiichi Sankyo Company, Limited
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

EP2862861A1 PIPERIDINYLPYRAZOLOPYRIDINE DERIVATIVE 失效
标题翻译：哌啶基吡唑并吡啶衍生物
公开(公告)号：EP2862861A1
公开(公告)日：2015-04-22
申请号：EP13804804.6
申请日：2013-06-13
申请人： Daiichi Sankyo Company, Limited
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
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.
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胆固醇血症或肾疾病，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。

3. 发明公开

EP3915558A1 SUBSTITUENT-INCLUDING UREA COMPOUND 审中-实审
公开(公告)号：EP3915558A1
公开(公告)日：2021-12-01
申请号：EP20744530.5
申请日：2020-01-23
申请人： Daiichi Sankyo Company, Limited
发明人： KAWAI, Junya , IWAMOTO, Osamu , UMEZAKI, Yuma , NAKAJIMA, Katsuyoshi , TSURUOKA, Hiroyuki , SAITO, Keiji , KURIKAWA, Nobuya , NISHIHAMA, Natsumi , TANAKA, Shinji , OGITANI, Momoko , HONDA, Tomohiro , SAITOH, Wataru , SONEDA, Tsuyoshi , OHKAWA, Nobuyuki
IPC分类号： A61K31/437
摘要： An object of the present invention is to provide a compound that has a specific chemical structure having an activation effect on SIRT6 and is useful as an active component for preventing and treating inflammatory diseases. The present invention relates to a compound represented by Formula (1) or a pharmaceutically acceptable salt thereof.

(Each symbol in Formula (1) has the same definition as that described in the specification.)

4. 发明授权

EP1935879B1 SUBSTITUTED CYCLOALKENE DERIVATIVE 有权
标题翻译：取代的环烯烃衍生物
公开(公告)号：EP1935879B1
公开(公告)日：2016-05-11
申请号：EP06810068.4
申请日：2006-09-13
申请人： Daiichi Sankyo Company, Limited
发明人： KIMURA, Tomio , OHKAWA, Nobuyuki , NAGASAKI, Takayoshi , SUGIDACHI, Atsuhiro , ANDO, Osamu
IPC分类号： A61K31/357 , A61P43/00 , C07D317/72
CPC分类号： C07C311/14 , C07C2601/16 , C07C2602/50 , C07D303/38 , C07D307/94 , C07D317/72 , C07D319/08 , C07D321/10 , C07D327/04 , C07D339/06 , C07D339/08 , C07D493/04 , C07D493/10

5. 发明公开

EP1935879A1 SUBSTITUTED CYCLOALKENE DERIVATIVE 有权
标题翻译：取代的环烯烃衍生物
公开(公告)号：EP1935879A1
公开(公告)日：2008-06-25
申请号：EP06810068.4
申请日：2006-09-13
申请人： Daiichi Sankyo Company, Limited
发明人： KIMURA, Tomio , OHKAWA, Nobuyuki , NAGASAKI, Takayoshi , SUGIDACHI, Atsuhiro , ANDO, Osamu
IPC分类号： C07C311/14 , A61K31/215 , A61K31/336 , A61K31/343 , A61K31/357 , A61K31/385 , A61K31/39 , A61K31/40 , A61K31/4025 , A61K31/443 , A61K31/5375 , A61P43/00 , C07D207/50 , C07D303/36 , C07D307/94 , C07D311/96 , C07D317/72 , C07D319/08 , C07D327/04 , C07D339/06 , C07D405/12
CPC分类号： C07C311/14 , C07C2601/16 , C07C2602/50 , C07D303/38 , C07D307/94 , C07D317/72 , C07D319/08 , C07D321/10 , C07D327/04 , C07D339/06 , C07D339/08 , C07D493/04 , C07D493/10
摘要： [Object]
To provide a substituted cycloalkene derivative having an action to supress intracellular signal transduction or cell activation induced by endotoxin and to suppress cell responses due to the intracellular signal transduction and cell activation such as an excess generation of inflammatory mediators such as TNF-α, pharmacologically acceptable salts therefor, a medicament containing them as an active ingredient, a preparation method therefor, and a medicament containing the aforementioned substituted cycloalkene derivative as an active ingredient which is superior in prophylaxis and/or treatment of diseases such as sepsis (septic shock, disseminated intravascular coagulation, multiple organ failure and the like), that are associated with intracellular signal transduction or cell activation induced by endotoxin and to cell responses to the intracellular signal transduction and cell activation.
[Solution]
A compound represented by the general formula (I):

{wherein
X and Y represent a group in which X and Y together with a carbon atom to which they are bound form ring A (the ring is 3- to 7-membered heterocyclyl ring or 3- to 7-membered cycloalkyl ring), each represents a hydrogen atom, or X and Y together represent a substituent of ring B.
1 and m, independently from each other, represent an integer of 0 to 3, and 1 + m is 1 to 3.
R 1 is an aliphatic hydrocarbon group and the like which may be substituted with a group selected from Substituent group β and
Substituent group γ. n represents an integer of 0 to 3.
R 2 is a C 1 -C 6 alkyl group and the like which may be substituted with a group selected from a hydrogen atom and Substituent
group β.
R 3 is a phenyl group, 5- to 6-membered heteroaryl group and the like which may be substituted with a group selected from Substituent group ε.
R 5 is a C 1 -C 6 alkyl group and the like which may be substituted with a group selected from a hydrogen atom and Substituent group β.
Provided that in the case where R 3 is a phenyl group which may be substituted with a group selected from Substituent group ε, X and Y represent a group in which X and Y together with a carbon atom to which they are bound form ring A, or X and Y together represent a substituent of ring B.
摘要翻译：本发明提供一种取代的环烯烃衍生物，其具有抑制由内毒素诱导的细胞内信号传导或细胞活化的作用，并且抑制由细胞内信号转导和细胞活化引起的细胞应答，例如过量代炎症介质如TNF-α ，其药理学上可接受的盐，含有它们作为活性成分的药物，其制备方法和含有上述取代的环烯烃衍生物作为活性成分的药物，其在预防和/或治疗诸如败血症（败血性休克），弥散性血管内凝血，多器官功能衰竭等），其与内毒素诱导的细胞内信号转导或细胞激活以及细胞对细胞内信号转导和细胞活化的应答有关。由通式（I）表示的化合物：其中X和Y表示其中X和Y与它们所键合的碳原子一起形成环A的基团（该环是3-至7-元杂环基环或3至7元环烷基环）各自表示氢原子，或者X和Y一起表示环B的取代基。1和m彼此独立地表示0至3的整数，并且1 + m是1至3.R 1是可以被选自取代基组β和取代基组γ的基团取代的脂族烃基等。 n表示0至3的整数.R 2为可以被选自氢原子和取代基组β的基团取代的C 1 -C 6烷基等。 R3是可以被选自取代基组ε的基团取代的苯基，5至6元杂芳基等。 R5是可以被选自氢原子和取代基组β的基团取代的C1-C6烷基等。只要在R3是可以被选自取代基组ε的基团取代的苯基的情况下，X和Y表示其中X和Y与它们所键合的碳原子一起形成环A的基团，或 X和Y一起表示环B的取代基。

6. 发明授权

EP2620434B1 A METHOD OF PREPARING CRYSTALS OF A SUBSTITUTED CYCLOALKENE DERIVATIVE 有权
标题翻译： VERFAHREN ZUR HERSTELLUNG EINES KRISTALLINEN SUBSTITUIERTEN CYCLOALKENDERIVATES
公开(公告)号：EP2620434B1
公开(公告)日：2017-01-04
申请号：EP11826892.9
申请日：2011-09-22
申请人： Daiichi Sankyo Company, Limited
发明人： OHKAWA, Nobuyuki , IIDA, Kouki , NAGASAKI, Takayoshi
IPC分类号： C07D317/72 , A61K31/357 , A61P29/00 , A61P31/04 , A61P31/12 , A61P43/00
CPC分类号： C07D317/72 , A61K31/357

7. 发明公开

EP2620434A1 CRYSTALS OF SUBSTITUTED CYCLOALKENE DERIVATIVES 有权
标题翻译：用于生产结晶取代CYCLOALKENDERIVATES
公开(公告)号：EP2620434A1
公开(公告)日：2013-07-31
申请号：EP11826892.9
申请日：2011-09-22
申请人： Daiichi Sankyo Company, Limited
发明人： OHKAWA, Nobuyuki , IIDA, Kouki , NAGASAKI, Takayoshi
IPC分类号： C07D317/72 , A61K31/357 , A61P29/00 , A61P31/04 , A61P31/12 , A61P43/00
CPC分类号： C07D317/72 , A61K31/357
摘要： To provide potassium salts of substituted cycloalkene derivatives, which suppress the production of an inflammatory mediator caused by intracellular signal transduction or cell activation induced by endotoxin, and crystals thereof. The present invention provides potassium (2-chloro-4-fluorophenyl){[(2R,3R,8R)-7-(ethoxycarbonyl)-2,3-bis(hydroxymethyl)-1,4-dioxaspiro[4.5]deca-6-en-8-yl]sulfonyl}azanide and potassium (2-bromo-4-fluorophenyl){[(2R,3R,8R)-7-(ethoxycarbonyl)-2,3-bis(hydroxymethyl)-1,4-dioxaspiro[4.5]deca-6-en-8-yl]sulfonyl}azanide, each of which suppresses the production of an inflammatory mediator caused by intracellular signal transduction or cell activation induced by endotoxin, crystals thereof, and a pharmaceutical containing any of the same, and a prophylactic and/or therapeutic agent for sepsis containing any of the same.

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