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1. 发明授权

EP3045206B1 POLYCYCLIC CARBAMOYLPYRIDONE DERIVATIVE HAVING HIV INTEGRASE INHIBITORY ACTIVITY 无效转让
标题翻译：具有HIV整合酶抑制活性的多环氨基甲酰基吡啶酮衍生物
公开(公告)号：EP3045206B1
公开(公告)日：2018-03-28
申请号：EP16154531.4
申请日：2006-04-28
申请人： VIIV Healthcare Company , Shionogi & Co., Ltd
发明人： JOHNS, Brian Alvin , KAWASUJI, Takashi , TAISHI, Teruhiko , TAODA, Yoshiyuki
IPC分类号： A61P31/18 , A61K31/4985 , C07D498/04
CPC分类号： C07D498/14 , A61K9/0053 , A61K31/4985 , A61K31/519 , A61K31/5365 , A61K31/551 , A61K45/06 , C07D471/04 , C07D471/14 , C07D471/22 , C07D498/04 , C07D498/20 , C07D498/22
摘要： The present invention is to provide a novel compound shown below, having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof.

2. 发明公开

EP3045206A1 POLYCYCLIC CARBAMOYLPYRIDONE DERIVATIVE HAVING HIV INTEGRASE INHIBITORY ACTIVITY 无效转让
标题翻译：多聚乙酰胆碱受体阻断剂HIV-INTEGRASE-HEMMUNGSAKTIVITÄT
公开(公告)号：EP3045206A1
公开(公告)日：2016-07-20
申请号：EP16154531.4
申请日：2006-04-28
申请人： VIIV Healthcare Company , Shionogi & Co., Ltd
发明人： JOHNS, Brian Alvin , KAWASUJI, Takashi , TAISHI, Teruhiko , TAODA, Yoshiyuki
IPC分类号： A61P31/18 , A61K31/4985 , C07D498/04
CPC分类号： C07D498/14 , A61K9/0053 , A61K31/4985 , A61K31/519 , A61K31/5365 , A61K31/551 , A61K45/06 , C07D471/04 , C07D471/14 , C07D471/22 , C07D498/04 , C07D498/20 , C07D498/22
摘要： The present invention is to provide a novel compound shown below, having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof.
摘要翻译：本发明提供具有抗病毒活性，特别是HIV整合酶抑制活性的药物，特别是抗HIV药物及其制备方法和中间体的下述新化合物。

3. 发明授权

EP1874117B1 POLYCYCLIC CARBAMOYLPYRIDONE DERIVATIVE HAVING HIV INTEGRASE INHIBITORY ACTIVITY 有权转让
标题翻译：与HIV整合LOCKING活动多环芳烃CARBAMOYLPYRIDON衍生物
公开(公告)号：EP1874117B1
公开(公告)日：2013-08-28
申请号：EP06758843.4
申请日：2006-04-28
申请人： VIIV Healthcare Company , Shionogi Co., Ltd.
发明人： JOHNS, Brian, Alvin , KAWASUJI, Takashi , TAISHI, Teruhiko , TAODA, Yoshiyuki
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D239/00 , C07D241/36 , C07D471/00 , C07D487/00 , C07D495/00 , C07D497/00
CPC分类号： C07D498/14 , A61K9/0053 , A61K31/4985 , A61K31/519 , A61K31/5365 , A61K31/551 , A61K45/06 , C07D471/04 , C07D471/14 , C07D471/22 , C07D498/04 , C07D498/20 , C07D498/22
摘要： The present invention is to provide a novel compound shown below, having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof.

4. 发明公开

EP3284519A8 POLYCYCLIC CARBAMOYLPYRIDONE DERIVATIVE HAVING HIV INTEGRASE INHIBITORY ACTIVITY 无效
公开(公告)号：EP3284519A8
公开(公告)日：2018-04-18
申请号：EP17195276.5
申请日：2006-04-28
申请人： VIIV Healthcare Company , Shionogi & Co., Ltd
发明人： JOHNS, Brian Alvin , KAWASUJI, Takashi , TAISHI, Teruhiko , TAODA, Yoshiyuki
IPC分类号： A61P31/18 , A61K31/4985 , C07D498/04
CPC分类号： C07D498/14 , A61K9/0053 , A61K31/4985 , A61K31/519 , A61K31/5365 , A61K31/551 , A61K45/06 , C07D471/04 , C07D471/14 , C07D471/22 , C07D498/04 , C07D498/20 , C07D498/22
摘要： The present invention is to provide a novel compound (I-1) shown below, having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof.

wherein
A ring is substituted ring of (a), (b) or (c)

wherein Z is O or NR 19 ,
R 19 is hydrogen, C 1-10 alkyl, C 2-8 alkenyl, C 1-10 alkylcarbonyl or C 1-10 alkylsulfonyl, and the other substituents on the A ring form a ring;
R 14 and R X are hydrogen;
a broken line represents the presence or absence of a bond, provided that when the broken line represents the presence of a bond, R X is not present;
R 1 is hydrogen or C 1-10 alkyl;
X is C 1-6 alkylene;
R 2 is phenyl or phenyl substituted with at least halogen;
R 3 is hydrogen, halogen, hydroxy, C 1-10 alkyl, C 2-8 alkenyl, C 1-10 alkoxy, C 2-8 alkenyloxy or amino;
or a pharmaceutically acceptable salt, or solvate thereof.

5. 发明授权

EP2376080B1 SYNTHESIS OF CARBAMOYLPYRIDONE HIV INTEGRASE INHIBITORS AND INTERMEDIATES 有权转让
标题翻译：氨甲酰基吡啶酮HIV整合酶抑制剂和中间体的合成
公开(公告)号：EP2376080B1
公开(公告)日：2017-09-13
申请号：EP09832226.6
申请日：2009-12-08
申请人： Shionogi & Co., Ltd. , VIIV Healthcare Company
发明人： YOSHIDA, Hiroshi , TAODA, Yoshiyuki , JOHNS, Brian, Alvin , KAWASUJI, Takashi , NAGAMATSU, Daiki
IPC分类号： C07D213/803 , C07D213/81 , C07D471/22 , C07D487/22 , C07D498/14 , A61K31/351 , A61K31/4412
CPC分类号： C07D498/14 , A61K31/351 , A61K31/4412 , C07D213/803 , C07D213/81 , C07D471/22 , C07D487/22 , Y02P20/55

6. 发明授权

EP1874117B8 POLYCYCLIC CARBAMOYLPYRIDONE DERIVATIVE HAVING HIV INTEGRASE INHIBITORY ACTIVITY 有权转让
标题翻译：与HIV整合LOCKING活动多环芳烃CARBAMOYLPYRIDON衍生物
公开(公告)号：EP1874117B8
公开(公告)日：2014-03-12
申请号：EP06758843.4
申请日：2006-04-28
申请人： VIIV Healthcare Company , Shionogi & Co., Ltd
发明人： JOHNS, Brian, Alvin , KAWASUJI, Takashi , TAISHI, Teruhiko , TAODA, Yoshiyuki
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D239/00 , C07D241/36 , C07D471/00 , C07D487/00 , C07D495/00 , C07D497/00
CPC分类号： C07D498/14 , A61K9/0053 , A61K31/4985 , A61K31/519 , A61K31/5365 , A61K31/551 , A61K45/06 , C07D471/04 , C07D471/14 , C07D471/22 , C07D498/04 , C07D498/20 , C07D498/22
摘要： The present invention is to provide a novel compound shown below, having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof.

7. 发明授权

EP1852434B1 BICYCLIC CARBAMOYLPYRIDONE DERIVATIVE HAVING HIV INTEGRASE INHIBITING ACTIVITY 失效
标题翻译：与HIV整合酶的锁定效果双环CARBAMOYLPYRIDONDERIVAT
公开(公告)号：EP1852434B1
公开(公告)日：2011-07-13
申请号：EP06714066.5
申请日：2006-02-20
申请人： Shionogi Co., Ltd.
发明人： YOSHIDA, Hiroshi , KAWASUJI, Takashi , TAODA, Yoshiyuki
IPC分类号： A61K31/403 , A61K31/519 , A61K31/50 , A61K31/495 , C07D239/00 , C07D241/36 , C07D471/00 , C07D487/00 , C07D495/00 , C07D497/00
CPC分类号： C07D471/04 , C07F9/6561
摘要： [PROBLEMS] To provide a novel compound having an antiviral activity, especially HIV integrase inhibiting activity, and a pharmaceutical, especially anti-HIV drug, containing the same. [MEANS FOR SOLVING PROBLEMS] A compound of the formula: (I) wherein Z1 is NR4 (R4 is hydrogen, an optionally substituted lower alkyl, etc.), O or CH2; Z2 is an optionally substituted lower alkenylene or optionally substituted lower alkylene wherein there may be interposed a heteroatom group selected from the group consisting of =N- and -N=, O, S, SO, SO2 or NR5 (R5 is independent from R4 and selected from among the same substituent group as that of R4); R1 is hydrogen or a lower alkyl; X is a single bond, a heteroatom group selected from among O, S, SO, SO2 and NH, or a lower alkenylene or lower alkylene wherein there may be interposed the heteroatom group; R2 is an optionally substituted aryl; and R3 is hydrogen, a halogen, hydroxyl, an optionally substituted lower alkyl, etc.

8. 发明公开

EP3144311A1 TRICYCLIC HETEROCYCLIC DERIVATIVE HAVING HIV REPLICATION-INHIBITING EFFECT 审中-公开
标题翻译：干细胞移植治疗麻疹艾滋病毒感染病毒WIRKUNG
公开(公告)号：EP3144311A1
公开(公告)日：2017-03-22
申请号：EP15793640.2
申请日：2015-05-15
申请人： Shionogi & Co., Ltd.
发明人： KAWASUJI, Takashi , TANIYAMA, Daisuke , SUGIYAMA, Shuichi , TAMURA, Yoshinori
IPC分类号： C07D487/06 , A61K31/519 , A61K31/5513 , A61K31/554 , A61P31/12 , A61P31/18 , C07D513/06
CPC分类号： C07D513/06 , A61K31/519 , A61K31/5513 , A61K31/554 , C07D471/06 , C07D471/16 , C07D487/06 , Y02P20/55
摘要： The present invention provides the following compound having anti-HIV activity of formula:

wherein, A 1 is C, CR 1A or N;
A 2 is C, CR 2A , or N;
A 3 is CR 3A , CR 3A R 3B , N, NR 3c O, S, SO, or SO 2 ;
A 4 is CR 4A , CR 4A R 4B , N, NR 4C O, S, SO, or SO2;
A 5 is C, CR 5A , or N;
T 1 ring is substituted or unsubstituted monocyclic carbocycle or substituted or unsubstituted monocyclic heterocycle;
R 1 is halogen, cyano, nitro or -X 1 -R 11 ;
R 2 is substituted or unsubstituted alkyl and the like;
n is 1 or 2;
R 3 is hydrogen, substituted or unsubstituted aromatic varbocyclyl;
R 4 is hydrogen or a carboxy protecting group;
the other symbols are as specified in the description.
摘要翻译：本发明提供具有下式的抗HIV活性的下列化合物：其中A 1为C，CR 1A或N; A 2为C，CR 2A或N; A 3为CR 3A，CR 3A R 3B，N，NR 3c O，S，SO或SO 2; A 4是CR 4A，CR 4A R 4B，N，NR 4C O，S，SO或SO 2; A 5为C，CR 5A或N; T 1环是取代或未取代的单环碳环或取代或未取代的单环杂环; R 1是卤素，氰基，硝基或-X 1 -R 11; R 2是取代或未取代的烷基等; n为1或2; R 3是氢，取代或未取代的芳族杂环基; R 4是氢或羧基保护基; 其他符号在说明书中指定。

9. 发明公开

EP1950212A1 POLYCYCLIC CARBAMOYLPYRIDONE DERIVATIVE HAVING INHIBITORY ACTIVITY ON HIV INTEGRASE 有权
标题翻译：多聚乙二胺四乙基纤维素
公开(公告)号：EP1950212A1
公开(公告)日：2008-07-30
申请号：EP06822311.4
申请日：2006-10-26
申请人： Shionogi Co., Ltd.
发明人： YOSHIDA, Hiroshi , KAWASUJI, Takashi , TAISHI, Teruhiko , TAODA, Yoshiyuki
IPC分类号： C07D471/04 , A61K31/4985 , A61K31/53 , A61K31/5377 , A61K31/5383 , A61K31/55 , A61K31/553 , A61K31/683 , A61P31/18 , C07D471/14 , C07D471/20 , C07D498/14 , C07F9/6521
CPC分类号： C07F9/6561 , C07D471/04 , C07D471/14 , C07D471/20 , C07D498/14
摘要： Is to provide a novel compound having an anti-viral activity, particularly a HIV integrase inhibitory activity, and a pharmaceutical composition, particularly an anti-HIV agent.

(wherein
R 1 is hydrogen or lower alkyl;
X is lower alkylene etc.;
R 2 is optionally substituted aryl;
R 3 is hydrogen, halogen, hydroxy, optionally substituted lower alkyl etc.;
R 4 is hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkyl lower alkyl, optionally substituted aryl, optionally substituted aryl lower alkyl, optionally substituted heterocyclic group, optionally substituted heterocyclic lower alkyl etc.;
A broken line indicates the presence or absence of a bond;
B 1 and B 2 are such that any one of them is CR 20 R 21 , and the other is NR 22 and, in this case, there is no broken line.
When B 2 is NR 22 , R 4 and R 22 may be connected together to form an optionally substituted heterocycle;
When B 2 is CHR 21 , R 4 and R 21 may be connected together to form an optionally substituted heterocycle.
Alternatively, B 1 and B 2 are independently C, CR 23 or N and, in this case, B 1 and B 2 may be taken together to form a heterocycle.
R 20 , R 21 , R 22 and R 23 are independently hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkyl lower alkyl etc.)
摘要翻译：提供具有抗病毒活性，特别是HIV整合酶抑制活性的新型化合物，以及药物组合物，特别是抗HIV剂。（其中R 1为氢或低级烷基; X为低级亚烷基等; R 2为任选取代的芳基; R 3为氢，卤素，羟基，任选取代的低级烷基等; R 4为氢，任选取代的低级烷基，任选取代的环烷基，任选取代的环烷基低级烷基，任选取代的芳基，任选取代的芳基低级烷基，任选取代的杂环基，任选取代的杂环低级烷基等;虚线表示存在或不存在键; B 1和B 2 其中任何一个是CR 20 R 21，另一个是NR 22，在这种情况下，没有虚线，当B 2是NR 22时，R 4和R 22可以连接在一起形成任选取代的杂环;当B 2是CHR 21时，R 4和R 21可以连接在一起形成任选取代的杂环;或者，B 1和B 2独立地是C，CR 23或N，在这种情况下，B 1 并且B 2可以一起形成a 杂环。 R 20，R 21，R 22和R 23独立地为氢，任选取代的低级烷基，任选取代的环烷基，任选取代的环烷基低级烷基等）

10. 发明公开

EP2952503A1 HIV REPLICATION INHIBITOR 审中-公开
标题翻译： HIV复制抑制剂
公开(公告)号：EP2952503A1
公开(公告)日：2015-12-09
申请号：EP14746481.2
申请日：2014-01-30
申请人： Shionogi & Co., Ltd.
发明人： TOMITA, Kenji , TAODA, Yoshiyuki , IWAKI, Tsutomu , KAWASUJI, Takashi , AKIYAMA, Toshiyuki , SUGIYAMA, Shuichi , TAMURA, Yoshinori , IWATSU, Masafumi
IPC分类号： C07D209/58 , A61K31/395 , A61K31/403 , A61K31/4184 , A61K31/4439 , A61K31/473 , A61K31/4741 , A61K31/4743 , A61K31/4745 , A61K31/538 , A61K31/5383 , A61K31/5415 , A61K31/55 , A61K31/554 , A61P31/18 , A61P43/00 , C07D221/12 , C07D223/18 , C07D225/08 , C07D279/02 , C07D281/02
CPC分类号： C07D498/06 , C07D209/80 , C07D221/12 , C07D221/18 , C07D223/18 , C07D225/08 , C07D237/36 , C07D241/44 , C07D243/04 , C07D243/12 , C07D243/38 , C07D265/34 , C07D267/20 , C07D273/01 , C07D275/06 , C07D279/02 , C07D281/02 , C07D285/36 , C07D291/08 , C07D311/80 , C07D335/10 , C07D401/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D471/04 , C07D471/06 , C07D471/10 , C07D487/04 , C07D491/056 , C07D491/06 , C07D495/04 , C07D495/14 , C07D498/04 , C07D513/04 , C07D513/06
摘要： The present invention provides a novel compound having an antiviral activity, in particular, an HIV replication inhibiting activity, as well as a pharmaceutical composition, in particular, an anti-HIV agent.

wherein ring A is substituted or unsubstituted carbocycle or substituted or unsubstituted heterocycle; R 1 is substituted or unsubstituted alkyl etc.; R 2 is substituted or unsubstituted alkyloxy etc.; n is 1 or 2; R 3 is substituted or unsubstituted carbocyclyl or substituted or unsubstituted heterocyclyl; R 4 is a hydrogen atom etc.; R 6 is substituted or unsubstituted alkyl etc.
摘要翻译：本发明提供具有抗病毒活性，特别是HIV复制抑制活性的新型化合物，以及药物组合物，特别是抗HIV剂。其中环A是取代或未取代的碳环或取代或未取代的杂环; R1是取代或未取代的烷基等; R2是取代或未取代的烷氧基等; n是1或2; R3是取代或未取代的碳环基或取代或未取代的杂环基; R4是氢原子等; R6是取代或未取代的烷基等

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