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公开(公告)号：EP2308880A1
公开(公告)日：2011-04-13
申请号：EP09773568.2
申请日：2009-07-03
IPC分类号： C07D491/044 , A61K31/4162 , A61P1/02 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/10 , A61P5/14 , A61P5/38 , A61P7/06 , A61P7/10 , A61P9/10 , A61P9/14 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/02 , A61P17/04 , A61P17/06 , A61P17/08
CPC分类号： C07D491/044 , C07D491/14
摘要： Provided are a tetracyclic compound represented by the formula (I):
[in the formula(I),the formula (A) represents a benzene ring or the like,
X represents CH or a nitrogen atom,
Q represents -O- or the like,
R 1 , R 2 , and R 3 may be the same or different and each represent a hydrogen atom or the like,
1, m, and n each represent an integer from one to the maximum substitutable number of substituents, and
R 4 and R 5 may be the same or different and each represent a hydrogen atom or the like], or a pharmaceutically acceptable salt thereof, and the like.摘要翻译： 提供由式（I）表示的四环化合物：[式（I）中，式（A）表示苯环等，X表示CH或氮原子，Q表示-O-等 中，R 1，R 2和R 3可以相同或不同，各自表示氢原子等，1，m，n分别表示1个至最大可取代数的取代基的整数，R 4和 R 5可以相同或不同，各自表示氢原子等]或其药学上可接受的盐等。
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公开(公告)号：EP2108642A1
公开(公告)日：2009-10-14
申请号：EP07829979.9
申请日：2007-10-17
发明人： AMISHIRO, Nobuyoshi , ATSUMI,Toshiyuki , NAKAZATO, Tomoyuki , UMEHARA, Hiroshi , FUJIHARA, Hiroaki , SHINOHARA, Fumikazu , FUNAHASHI, Jun , YAMAMOTO, Junichiro , YAGI, Kaori
IPC分类号： C07D209/46 , A61K31/404 , A61K31/4178 , A61K31/4184 , A61K31/423 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/536 , A61K31/5377 , A61K31/541 , A61K31/55 , A61P35/00 , A61P37/02 , A61P43/00 , C07D209/48 , C07D401/14 , C07D403/14 , C07D413/04
CPC分类号： C07D209/46 , A61K31/404 , A61K31/4178 , A61K31/4184 , A61K31/423 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/536 , A61K31/5377 , A61K31/541 , A61K31/55 , C07D209/48 , C07D401/14 , C07D403/14 , C07D413/04 , C07D471/04
摘要： A JAK inhibitor comprising, as an active ingredient, a nitrogen-containing heterocyclic compound represented by formula (I)
{wherein W represents a nitrogen atom or -CH-;
X represents -C (=O) - or -CHR 4 - (wherein R 4 represents a hydrogen atom, or the like);
R 1 represents the formula described below [wherein Q 1 represents-CR 8 -(wherein R 8 represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like);
Q 2 represents -NR 15 - (wherein R 15 represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like); and R 5 and R 6 may be the same or different and each represents a hydrogen atom, halogen, carboxy, substituted or unsubstituted lower alkyl, or the like], or the like; and
R 2 and R 3 may be the same or different and each represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, or the like} or a pharmaceutically acceptable salt thereof.摘要翻译： 作为活性成分的JAK抑制剂含有式（I）表示的含氮杂环化合物{其中W表示氮原子或-CH-; X表示-C（= O） - 或-CHR 4 - （其中R 4表示氢原子等）; R 1表示下述式[其中Q 1表示-CR 8 - （其中R 8表示氢原子，取代或未取代的低级烷基等）; Q 2表示-NR 15 - （其中R 15表示氢原子，取代或未取代的低级烷基等）; R 5和R 6可以相同或不同，各自表示氢原子，卤素，羧基，取代或未取代的低级烷基等〕等。 R 2和R 3可以相同或不同，各自表示氢原子，卤素，取代或未取代的低级烷基等}或其药学上可接受的盐。
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公开(公告)号：EP2891717A1
公开(公告)日：2015-07-08
申请号：EP13833206.9
申请日：2013-09-02
发明人： SHINOHARA, Fumikazu , MAKINO, Asana , YAMAMOTO, Junichiro , OASHI, Taiji , SUZUKI, Michihiko , SAITO, Jun-ichi , NAKAJIMA, Takahiro , NISHIKAWA, Tomoyuki , NAKOJI, Masayoshi , TAKAHASHI, Yuichi
IPC分类号： C12N15/113 , A61K31/713 , A61K48/00 , A61P43/00 , C07H21/02 , C12N15/09
CPC分类号： C12N15/113 , A61K31/713 , C07H21/02 , C12N15/111 , C12N2310/14 , C12N2310/32 , C12N2310/33 , C12N2320/50 , C12N2320/51 , C12N2330/30
摘要： The present invention provides an oligonucleotide having improved affinity for AG02, and the like. The oligonucleotide has a nucleotide residue or a nucleoside residue represented by formula (I) {wherein X 1 is an oxygen atom or the like, R 1 is formula (IIA) (wherein R 5A is halogen or the like, and R 6A is a hydrogen atom or the like) or formula (IVA) (wherein Y 3A is a nitrogen atom or the like, and Y 4A is CH or the like), or the like, R 2 is a hydrogen atom, hydroxy, halogen, or optionally substituted lower alkoxy, and R 3 is a hydrogen atom or the like} at the 5' end thereof, and the nucleotide residue or the nucleoside residue binds to an adjacent nucleotide residue through the oxygen atom at position 3.
摘要翻译： 本发明提供了对AG02具有改善的亲和性的寡核苷酸等。 寡核苷酸具有由式（I）表示的核苷酸残基或核苷残基{其中X 1为氧原子等，R 1为式（IIA）（其中R 5A为卤素等，R 6A为 氢原子等）或式（IVA）（其中Y 3A为氮原子等，Y 4A为CH等）等，R 2为氢原子，羟基，卤素或任选地 取代的低级烷氧基，R 3为氢原子等），核苷酸残基或核苷残基通过第3位的氧原子与相邻的核苷酸残基结合。
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公开(公告)号：EP3315507A1
公开(公告)日：2018-05-02
申请号：EP16814541.5
申请日：2016-06-27
发明人： YAMAMOTO, Junichiro , SAWADA, Takashi , HAGIWARA, Kenji , ATSUMI, Toshiyuki , SHINOHARA, Fumikazu
IPC分类号： C07H21/00 , C12N15/113
CPC分类号： A61K31/7125 , A61K31/712 , C07H21/00 , C12N15/113 , C12N2310/14
摘要： The present invention provides an oligonucleotide derivative having, at an oxygen atom of at least one phosphate group of an oligonucleotide, a group represented by formula (I):
(wherein R 1 represents lower alkyl or the like; and R 2 and R 3 are the same or different and respectively represent an electron-withdrawing group or the like), or a salt thereof.摘要翻译： 本发明提供了具有寡核苷酸衍生物，在至少一个磷酸基团的寡核苷酸的，通过使式（I）表示的基团的氧原子：（其中R1代表低级烷基等; R 2和R 3相同或 不同且分别表示吸电子基团等）或其盐。
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5.发明公开OLIGONUCLEOTIDE HAVING NON-NATURAL NUCLEOTIDE AT 5'-TERMINAL THEREOF 审中-公开OLIGONUKLEOTID MIT NICHT-NATÜRLICHENNUKLEOTID AM 5-ENDE
公开(公告)号：EP3130597A1
公开(公告)日：2017-02-15
申请号：EP15758130.7
申请日：2015-03-03
发明人： SHINOHARA, Fumikazu , MAKINO, Asana , YAMAMOTO, Junichiro , NAKAJIMA, Takahiro , OASHI, Taiji , SUZUKI, Michihiko , SAITO, Jun-ichi , NISHIKAWA, Tomoyuki , NAKOJI, Masayoshi , TAKAHASHI, Yuichi , KOUDA, Yasuo
IPC分类号： C07H19/16 , A61K31/7076 , A61K31/713 , A61K48/00 , A61P43/00 , C07H19/167 , C07H19/173 , C07H19/20 , C12N15/113
CPC分类号： A61K31/7115 , A61K31/5377 , A61K31/7076 , A61K31/713 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/167 , C07H19/173 , C07H19/20 , C07H21/00 , C07H23/00 , C12N15/111 , C12N15/113 , C12N2310/14 , C12N2310/32 , C12N2310/33 , C12N2320/31
摘要： An oligonucleotide having a nucleotide residue or a nucleoside residue represented by formula (I) {wherein X 1 is an oxygen atom or the like, R 1 is formula (IIA) (wherein R 5A is halogen or the like, and R 6A is a hydrogen atom or the like) , formula (IVA) (wherein Y 3A is a nitrogen atom or the like, and Y 4A is CH or the like), or the like, R 2 is a hydrogen atom, hydroxy, halogen, or optionally substituted lower alkoxy, and R 3 is a hydrogen atom or the like, or formula (VI)(wherein n2 is 1, 2 or 3)} at the 5' end thereof, wherein the nucleotide residue or the nucleoside residue binds to an adjacent nucleotide residue through the oxygen atom at position 3, is provided.
摘要翻译： 具有式（I）表示的核苷酸残基或核苷残基的寡核苷酸{其中，X 1为氧原子等，R 1为式（IIA）（式中，R 5A为卤素等，R 6A为 氢原子等），式（IVA）（其中Y 3A为氮原子等，Y 4A为CH等）等，R 2为氢原子，羟基，卤素或任选地 取代的低级烷氧基，R 3为氢原子等，或式（VI）（其中n2为1,2或3）}，其中核苷酸残基或核苷残基与相邻的 提供了通过位置3的氧原子的核苷酸残基。
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