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1. 发明公开

EP3603648A1 COMPLEX OF NUCLEIC ACID MEDICINE AND MULTIBRANCHED LIPID 审中-实审
公开(公告)号：EP3603648A1
公开(公告)日：2020-02-05
申请号：EP18775491.6
申请日：2018-03-28
申请人： Shionogi & Co., Ltd
发明人： KUGIMIYA, Akira , SEKIGUCHI, Mitsuaki , KURODA, Norikazu , NAKAMURA, Jun , TANINO, Tetsuya , MITSUOKA, Yasunori , KASUYA, Takeshi , KATO Yasuharu
IPC分类号： A61K31/7088 , A61K47/50 , C12N15/00
摘要： The purpose of the present invention is to provide novel complexes that improve the effect of nucleic acid medicines.
Provided is a complex in which a multibranched lipid(s) binds through a linker to a strand of an oligonucleotide comprising a nucleic acid medicine having suppressing activity of the target gene expression.

2. 发明公开

EP3357507A1 NUCLEIC ACID DERIVATIVE HAVING IMMUNOSTIMULATORY ACTIVITY 审中-公开
公开(公告)号：EP3357507A1
公开(公告)日：2018-08-08
申请号：EP16851711.8
申请日：2016-09-29
申请人： Shionogi & Co., Ltd
发明人： KUGIMIYA, Akira , TANINO, Tetsuya , SEKIGUCHI, Mitsuaki , MITSUOKA, Yasunori , KURODA, Norikazu , NAKAMURA, Jun
IPC分类号： A61K39/39 , A61K39/00 , A61P35/00 , A61P37/04 , C07K14/47 , C12N15/09 , C12N15/117
CPC分类号： A61K39/00 , A61K39/39 , C07K14/47 , C12N15/09 , C12N15/117
摘要： The purpose of the present invention is to provide double-stranded oligonucleotides comprising the CpG oligonucleotide mentioned below, as a nucleic acid derivative having an immunostimulatory activity.
An adjuvant comprising a double-stranded oligonucleotide, wherein
a first strand is a CpG oligonucleotide consisting of 8 to 50 nucleotides,
a second strand is an oligonucleotide consisting of 8 to 60 nucleotides and comprising a sequence capable of hybridizing with the first strand, and a lipid binds to the second strand through a linker or without a linker.

3. 发明公开

EP1939175A1 SULFONAMIDE DERIVATIVE HAVING PGD2 RECEPTOR ANTAGONISTIC ACTIVITY 有权
标题翻译：磺胺类药物与PGD2受体拮抗作用
公开(公告)号：EP1939175A1
公开(公告)日：2008-07-02
申请号：EP06810485.0
申请日：2006-09-25
申请人： Shionogi&Co., Ltd.
发明人： KUGIMIYA, Akira , FUJIOKA, Masahiko , TACHIBANA, Yuki , MURASHI, Takami , ONODERA, Naohiro
IPC分类号： C07D207/48 , A61K31/40 , A61K31/445 , A61K31/451 , A61K31/4545 , A61K31/495 , A61K31/496 , A61P11/06 , A61P37/08 , A61P43/00 , C07D207/14 , C07D211/58 , C07D211/70 , C07D211/96 , C07D213/38 , C07D213/71 , C07D213/74 , C07D231/12 , C07D235/08 , C07D235/32
CPC分类号： C07D295/26 , C07D207/14 , C07D207/48 , C07D211/58 , C07D211/70 , C07D211/96 , C07D213/38 , C07D213/40 , C07D213/64 , C07D213/71 , C07D213/74 , C07D231/12 , C07D231/40 , C07D235/08 , C07D235/30 , C07D235/32 , C07D243/08 , C07D261/08 , C07D261/18 , C07D263/32 , C07D263/58 , C07D265/36 , C07D271/10 , C07D277/24 , C07D277/28 , C07D285/12 , C07D285/135 , C07D295/096 , C07D295/155 , C07D307/42 , C07D307/52 , C07D307/56 , C07D307/68 , C07D333/36 , C07D401/12 , C07D413/12
摘要： The present invention provides an sulfonamide derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases.
A compound of the general formula (II):

wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the ring C is an aromatic carbocyclic ring etc.; R1 is carboxy etc.; R2 is independently a halogen atom etc.; R3 is optionally substituted alkyloxy etc.; R4 is independently a halogen atom etc.; R5 is independently optionally substituted alkyl etc.; M is sulfonyl etc.; Y is a single bond etc.; L1 is a single bond etc.; L2 is a single bond etc.; k is 0, 1, 2, 3 or 4; n is 0, 1 or 2; and q is 0, 1, 2 or 3; provided that a) k is not 0 when the ring B is a 6-membered nitrogen-containing heterocyclic ring containing one or two nitrogen atom(s) and the ring C is a benzene ring, etc.;
a pharmaceutically acceptable salt or a hydrate thereof.

4. 发明授权

EP2957567B1 NUCLEOSIDE AND NUCLEOTIDE, HAVING NITROGEN-CONTAINING HETERCYCLE STRUCTURE 有权
公开(公告)号：EP2957567B1
公开(公告)日：2019-06-05
申请号：EP14751080.4
申请日：2014-02-17
申请人： Shionogi & Co., Ltd.
发明人： MITSUOKA, Yasunori , KUGIMIYA, Akira , YAMASHITA, Aiko
IPC分类号： C07H19/06 , C07H19/16 , C07H21/00

6. 发明公开

EP1932839A1 INDOLECARBOXYLIC ACID DERIVATIVE HAVING PGD2 RECEPTOR ANTAGONISTIC ACTIVITY 审中-公开
标题翻译：印度尼西亚麻醉师麻醉师WIRKUNG AM PGD2-REZEPTOR
公开(公告)号：EP1932839A1
公开(公告)日：2008-06-18
申请号：EP06797344.6
申请日：2006-09-04
申请人： Shionogi Co., Ltd.
发明人： KUGIMIYA, Akira , TACHIBANA, Yuki
IPC分类号： C07D401/04 , A61K31/405 , A61K31/437 , A61K31/454 , A61K31/4545 , A61P9/10 , A61P11/00 , A61P17/00 , A61P35/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07D401/14 , C07D403/04 , C07D471/04
CPC分类号： C07D401/04 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D413/14 , C07D419/14 , C07D471/04
摘要： The present invention provides an indolecarboxylic acid derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases.
A compound of the general formula (I):

wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the formula of -X 1 =X 2 -X 3 =X 4 - is a formula of -C(R 1 )=C(R 2 )-C(R 3 )=C(R 4 )- etc.; X 5 is C(R 5 ) or N; R 1 , R 2 , R 3 , R 4 and R 5 is independently a hydrogen atom, a halogen atom etc; R 6 is a formula of -Z-R 10 etc. wherein Z is alkylene etc., and R 10 is carboxy etc.; R 7 is optionally substituted alkyloxy etc.; R 8 is independently a halogen atom etc.; R 9 is independently optionally substituted alkyl etc.; Y is a single bond etc.; n is 0 etc.; q is 0 etc.;
a pharmaceutically acceptable salt or a solvate thereof.
摘要翻译：本发明提供了具有DP受体拮抗作用的吲哚羧酸衍生物和包含所述化合物作为活性成分的药物组合物，还有用于治疗过敏性疾病的治疗剂。通式（I）的化合物：其中环A为芳族碳环等; 环B为含氮非芳族杂环等; -X 1 = X 2 -X 3 = X 4 - 的式为-C（R 1）= C（R 2）-C（R 3）= C（R 4）等的式; X 5为C（R 5）或N; R 1，R 2，R 3，R 4和R 5独立地为氢原子，卤素原子等; R 6是-Z-R 10等的化合物，其中Z是亚烷基等，R 10是羧基等; R 7是任选取代的烷氧基等; R 8独立地为卤素原子等; R 9独立地是任选取代的烷基等; Y是单键等; n为0等 q是0等其药学上可接受的盐或溶剂合物。

8. 发明公开

EP2957567A1 NUCLEOSIDE AND NUCLEOTIDE, HAVING NITROGEN-CONTAINING HETERCYCLE STRUCTURE 有权
标题翻译： NUKLEOSID UND NUKLEOTID MIT EINER STICKSTOFFHALTIGEN HETEROCYCLISCHEN STRUKTUR
公开(公告)号：EP2957567A1
公开(公告)日：2015-12-23
申请号：EP14751080.4
申请日：2014-02-17
申请人： Shionogi & Co., Ltd.
发明人： MITSUOKA, Yasunori , KUGIMIYA, Akira , YAMASHITA, Aiko
IPC分类号： C07H19/06 , C07H21/00
CPC分类号： C07H19/10 , C07H19/06 , C07H19/16 , C07H21/00 , Y02P20/55
摘要： The present invention provides compounds shown by the formula:

wherein
Y 1 is CR 6 or N,
Y 2 is CR 7 or N,
Y 3 is CR 8 or N,
R 6 , R 7 and R 8 are each independently, a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl or the like,
Bx is a nucleic acid base moiety,
Z 1 and Z 2 are each independently, a hydrogen atom, a hydroxyl protecting group or a reactive phosphorus group,
R 1 to R 5 are each independently, a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl or the like, and
n is an integer of 0 to 3,
or salts thereof, that are novel nucleosides or nucleotides that can be useful as materials for synthesizing nucleic acid pharmaceuticals.
摘要翻译：本发明提供下列化合物：其中Y 1为CR 6或N，Y 2为CR 7或N，Y 3为CR 8或N，R 6，R 7和R 8各自独立地为氢原子，卤素，氰基，取代或未取代的烷基等，Bx是核酸碱基部分，Z 1和Z 2各自独立地为氢原子，羟基保护基或反应性磷基，R 1〜R 5为各自独立地为氢原子，卤素，氰基，取代或未取代的烷基等，n为0〜3的整数，或其盐，可用作合成核酸药物的材料的新型核苷或核苷酸。

9. 发明公开

EP3444345A1 microRNA-143 DERIVATIVE 有权转让
公开(公告)号：EP3444345A1
公开(公告)日：2019-02-20
申请号：EP17782473.7
申请日：2017-04-13
申请人： Shionogi & Co., Ltd.
发明人： AKAO, Yukihiro , KITADE, Yukio , SEKIGUCHI, Mitsuaki , MITSUOKA, Yasunori , KUGIMIYA, Akira , SASAKI, Yasuo
IPC分类号： C12N15/09 , A61K31/713 , A61K48/00 , A61P35/00 , C12N15/113
摘要： The purpose of the present invention is to provide novel miR-143 derivatives described herein that can be used as oligonucleotide therapeutics.
A microRNA-143 derivative wherein
the first strand is an oligonucleotide consisting of
a sequence of SEQ ID NO: 3; or
a sequence in which one or two bases are substituted, deleted, inserted or added to the sequence of SEQ ID NO: 3 and
does not include a 3'-end modification, but may include a 5'-end modification; and
the second strand is an oligonucleotide consisting of
a sequence of SEQ ID NO: 4 or
a sequence in which one or two bases are substituted, deleted or inserted to the sequence of SEQ ID NO: 4 and
includes a 3'-end modification, and may include a 5'-end modification;
or
a sequence of SEQ ID NO: 5 or
a sequence in which one or two bases are substituted or inserted to the sequence of SEQ ID NO: 5 and
does not include a 3'-end modification, and may include a 5'-end modification;
wherein
the 3'-end modification is a 1 to 5-mer oligonucleotide derivative which may include a nucleoside derivative(s) and/or modified internucleoside linkage(s) or a benzene-pyridine derivative and
the 5'-end modification is a phosphate ester moiety or a group of the formula: =CQ 1 - P(=O)(OH) 2 , wherein Q 1 is hydrogen, halogen, substituted or unsubstituted alkyl,
substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or
substituted or unsubstituted alkyloxy.

10. 发明公开

EP2351744A1 ACETIC ACID AMIDE DERIVATIVE HAVING INHIBITORY ACTIVITY ON VASCULAR ENDOTHELIAL LIPASE 有权
标题翻译：醋酸酰胺衍生物对血管内皮细胞脂肪酶具有抑制作用
公开(公告)号：EP2351744A1
公开(公告)日：2011-08-03
申请号：EP09820619.6
申请日：2009-10-15
申请人： Shionogi & Co., Ltd.
发明人： MASUDA, Kouji , KIDA, Shiro , HAYASHI, Kyohei , KATOU, Manabu , YOSHIKAWA, Naoki , KUGIMIYA, Akira , NAKAJIMA, Mado , TANAKA, Nobuyuki
IPC分类号： C07D235/16 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/429 , A61K31/437 , A61K31/4439 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/5377 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , A61P43/00 , C07D263/56 , C07D277/64 , C07D417/04 , C07D417/12 , C07D513/04
CPC分类号： C07D235/16 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/429 , A61K31/437 , A61K31/4439 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/5377 , C07D263/56 , C07D263/57 , C07D277/30 , C07D277/64 , C07D417/04 , C07D417/06 , C07D417/12 , C07D513/04
摘要： Disclosed is a compound which is useful as an endothelial lipase inhibitor. A pharmaceutical composition having inhibitory activity on endothelial lipase comprising a compound represented by the formula:

, its pharmaceutically acceptable salt, or a solvate thereof,
wherein
Ring A is nitrogen-containing hetero ring,
Ring A may be substituted with a substituent other than a group represented by the formula: -C(R 1 R 2 )-C(=O)-NR 3 R 4 and a group represented by the formula: -R 5 ,
a broken line represents the presence or the absence of a bond,
Z is -NR 6 -, =N-, -O-, or -S-,
R 6 is halogen, substituted or unsubstituted alkyl or the like,
R 1 and R 2 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy or substituted or unsubstituted alkyl,
R 3 is hydrogen or substituted or unsubstituted alkyl,
R 4 is hydrogen, substituted or unsubstituted alkyl or the like,
R 3 and R 4 taken together with the adjacent nitrogen atom to which they are attached may form a substituted or unsubstituted ring,
R 5 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl or the like.
摘要翻译：公开了可用作内皮脂肪酶抑制剂的化合物。一种对内皮脂肪酶具有抑制活性的药物组合物，其含有下式所示化合物，其药学上可接受的盐或其溶剂化物，其中环A为含氮杂环，环A可以被除基团以外的取代基由式-C（R 1 R 2）-C（= O）-NR 3 R 4表示的基团和由式-R 5表示的基团表示，虚线表示键的存在或不存在，Z是-NR 6 - ，= N -O-或-S-，R 6为卤素，取代或未取代的烷基等，R 1和R 2各自独立地为氢，卤素，羟基，氰基，硝基，羧基或取代或未取代的烷基，R 3为氢或取代或未取代的烷基，R 4为氢，取代或未取代的烷基等，R 3和R 4与它们所连接的相邻氮原子一起可形成取代或未取代的环，R 5为氢，卤素，羟基，氰基，硝基，羧基，取代的或未取代的取代或未取代的烷基，取代或未取代的烯基，取代或未取代的炔基等。

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