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1. 发明授权

EP2330902B1 CHEMICAL COMPOUNDS 有权转让
标题翻译：化合物
公开(公告)号：EP2330902B1
公开(公告)日：2012-11-14
申请号：EP09800993.9
申请日：2009-07-23
申请人： GlaxoSmithKline LLC , Shionogi & Co., Ltd.
发明人： JOHNS, Brian, Alvin , WEATHERHEAD, Jason, Gordon , AOYAMA, Yasunori , YOSHIDA, Hiroshi , TAODA, Yoshiyuki
IPC分类号： A01N43/42 , A61K31/44 , C07D471/14
CPC分类号： C07D471/14

2. 发明公开

EP2376080A1 SYNTHESIS OF CARBAMOYLPYRIDONE HIV INTEGRASE INHIBITORS AND INTERMEDIATES 有权转让
标题翻译： ZWISCHENPRODUKTE的合成维生素B-HIV-INTEGRASE-HEMMERN
公开(公告)号：EP2376080A1
公开(公告)日：2011-10-19
申请号：EP09832226.6
申请日：2009-12-08
申请人： Shionogi & Co., Ltd. , GlaxoSmithKline LLC
发明人： YOSHIDA, Hiroshi , TAODA, Yoshiyuki , JOHNS, Brian, Alvin , KAWASUJI, Takashi , NAGAMATSU, Daiki
IPC分类号： A61K31/4412 , A61K31/351
CPC分类号： C07D498/14 , A61K31/351 , A61K31/4412 , C07D213/803 , C07D213/81 , C07D471/22 , C07D487/22 , Y02P20/55
摘要： A synthesis approach providing an early ring attachment via a bromination to compound l-l yielding compound II-Il, whereby a final product such as AA can be synthesized. In particular, the 2,4-difluorophenyl-containing sidechain is attached before creation of the additional ring Q.
摘要翻译：通过溴化将早期的环连接提供给化合物I-1的合成方法，得到化合物II-II：由此可以合成最终产物如AA。特别地，在产生附加环Q之前附着了含2,4-二氟苯基的侧链。

3. 发明公开

EP2330902A1 CHEMICAL COMPOUNDS 有权转让
标题翻译：化学化合物
公开(公告)号：EP2330902A1
公开(公告)日：2011-06-15
申请号：EP09800993.9
申请日：2009-07-23
申请人： GlaxoSmithKline LLC , Shionogi&Co., Ltd.
发明人： JOHNS, Brian, Alvin , WEATHERHEAD, Jason, Gordon , AOYAMA, Yasunori , YOSHIDA, Hiroshi , TAODA, Yoshiyuki
IPC分类号： A01N43/42 , A61K31/44
CPC分类号： C07D471/14
摘要： The present invention features compounds that are prodrugs of HIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.
摘要翻译：本发明的特征是作为HIV整合酶抑制剂的前药的化合物，因此可用于抑制HIV复制，预防和/或治疗HIV感染，以及治疗AIDS和/或ARC。

4. 发明授权

EP1950212B1 POLYCYCLIC CARBAMOYLPYRIDONE DERIVATIVE HAVING INHIBITORY ACTIVITY ON HIV INTEGRASE 有权
标题翻译：有锁定效应对HIV整合多环芳烃CARBAMOYLPYRIDONDERIVAT
公开(公告)号：EP1950212B1
公开(公告)日：2016-02-24
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： A61K31/403 , A61K31/519 , A61K31/50 , A61K31/495 , C07D239/00 , C07D241/36 , C07D471/00 , C07D487/00 , C07D495/00 , C07D497/00
CPC分类号： C07F9/6561 , C07D471/04 , C07D471/14 , C07D471/20 , C07D498/14

5. 发明公开

EP2404896A1 CYCLOHEXANE DERIVATIVE HAVING NPY Y5 RECEPTOR ANTAGONISM 审中-公开
标题翻译： CYCLOHEXANDERIVAT MIT NPY-Y5-REZEPTORANTAGONISMUS
公开(公告)号：EP2404896A1
公开(公告)日：2012-01-11
申请号：EP10748840.5
申请日：2010-03-05
申请人： Shionogi & Co., Ltd.
发明人： YOSHIDA, Hiroshi , TONOGAKI, Keisuke , SAKAGAMI, Masahiro , TAKAYA, Kenji
IPC分类号： C07C237/24 , A61K31/167 , A61K31/275 , A61K31/415 , A61K31/4184 , A61K31/4192 , A61K31/42 , A61K31/421 , A61K31/422 , A61K31/423 , A61K31/427 , A61K31/4375 , A61K31/44 , A61K31/4439 , A61K31/4709 , A61K31/4965 , A61K31/497 , A61K31/5375 , A61K31/5377 , A61P3/04 , A61P43/00
CPC分类号： C07D213/64 , C07C237/24 , C07C255/54 , C07C2601/14 , C07D213/74 , C07D213/81 , C07D213/84 , C07D231/38 , C07D241/18 , C07D249/06 , C07D261/18 , C07D263/34 , C07D263/58 , C07D265/30 , C07D401/12 , C07D413/12 , C07D417/12 , C07D471/04
摘要： The present invention discloses novel cyclohexane derivatives having NPY Y5 receptor antagonistic activity. Specifically, the present invention discloses a compound represented by the formula (I), or a pharmaceutically acceptable salt or a solvate thereof:

wherein A is substituted or unsubstituted aryl or heterocyclyl; a combination of X and Y is a combination selected from (X, Y)=(C(=O)N(R 1 ), C(=O)N(R 2 )), (C(=O)N(R 1 ), imidazole-1,3-diyl), (N(R 1 ), C(=O)N(R 2 )), (O, C(=O)N(R 2 )), (C(R 3 )(R 4 ), N(R 2 )) or (a single bond, C(=O)N(R 2 )); R 1 , R 2 and R 3 are independently hydrogen or substituted or unsubstituted alkyl; R 5 is substituted or unsubstituted aryl or heterocyclyl; R 6 is halogen, oxo, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryloxy; m is 0 or 1; and n is an integer of 0 to 5; and B is aromatic carbocycle, monocyclic heterocycle or fused bicyclic heterocycle.
摘要翻译：本发明公开了具有NPY Y5受体拮抗活性的新型环己烷衍生物。具体而言，本发明公开了式（I）表示的化合物或其药学上可接受的盐或溶剂化物：其中A为取代或未取代的芳基或杂环基; X和Y的组合是选自（X，Y）=（C（= O）N（R 1），C（= O）N（R 2）），（C（= O） 1，咪唑-1,3-二基），（N（R 1），C（= O）N（R 2）），（O，C（= O）N（R 2）），（C 3）（R 4），N（R 2））或（单键，C（= O）N（R 2））; R 1，R 2和R 3独立地为氢或取代或未取代的烷基; R 5是取代或未取代的芳基或杂环基; R 6是卤素，氧代，取代或未取代的烷基，取代或未取代的烷氧基，取代或未取代的芳氧基; m为0或1; n为0〜5的整数，和B是芳族碳环，单环杂环或稠合双环杂环。

6. 发明公开

EP1852434A1 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：EP1852434A1
公开(公告)日：2007-11-07
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： C07D471/04 , A61K31/4985 , A61P31/12 , A61P31/18 , A61P37/04 , A61P43/00
CPC分类号： C07D471/04 , C07F9/6561
摘要： [Object] Is to provide a novel compound having an anti-viral activity, particularly a HIV integrase inhibitory activity, and an agent, particularly an anti-HIV agent.
[Solving means] A compound represented by the formula:

(wherein
Z 1 is NR 4 (R 4 is hydrogen, optionally substituted lower alkyl etc.), O or CH 2 ;
Z 2 is optionally substituted lower alkylene or optionally substituted lower alkenylene, each may be intervened by a heteroatom group selected from group consisting O, S, SO, SO 2 , NR 5 (R 5 is selected independently from the same substituent group of R 4 ) -N= and =N-;
R 1 is hydrogen or lower alkyl;
X is a single bond, a heteroatom group selected from O, S, SO, SO 2 and NH, or lower alkylene or lower alkenylene each may be intervened by the heteroatom group;
R 2 is optionally substituted aryl;
R 3 is hydrogen, halogen, hydroxy, optionally substituted alkyl group etc.)

7. 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）

8. 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.

9. 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

10. 发明公开

EP3210603A1 SYNTHESIS OF CARBAMOYLPYRIDONE HIV INTEGRASE INHIBITORS AND INTERMEDIATES 无效转让
公开(公告)号：EP3210603A1
公开(公告)日：2017-08-30
申请号：EP17157972.5
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 , KAWASJUI, Takashi , NAGAMATSU, Daiki
IPC分类号： A61K31/351 , A61K31/4412 , C07D213/803 , C07D213/81 , C07D487/22 , C07D471/22 , C07D498/14
CPC分类号： C07D498/14 , A61K31/351 , A61K31/4412 , C07D213/803 , C07D213/81 , C07D471/22 , C07D487/22 , Y02P20/55
摘要： A synthesis approach providing an early ring attachment via a bromination to compound I-I yielding compound II-II:

whereby a final product such as AA:

can be synthesized. In particular, the 2,4-difluorophenyl-containing sidechain is attached before creation of the additional ring Q.

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