公开(公告)号：EP1867726A1

公开(公告)日：2007-12-19

申请号：EP06729942.0

申请日：2006-03-24

申请人： National University Corporation Hokkaido University ,  Kyoto University ,  SHIONOGI & CO., LTD.

发明人： KOGURE, Kentaro ,  NAKAMURA, Takashi ,  AKITA, Hidetaka ,  HARASHIMA, Hideyoshi ,  FUTAKI, Shiroh

IPC分类号： C12N15/88

CPC分类号： C12N15/88 ,  A61K48/00

摘要： Disclosed is a non-viral vector capable of delivering a given substance into the nucleus of a target cell effectively even when the target cells is a undividable cell such as a dendritic cell. A bilamellar liposome having a first lipid membrane and a second lipid membrane successively from the outside, the first lipid membrane having a membrane-fusing ability and the second lipid membrane having on its surface a nuclear transport peptide.

摘要翻译： 公开了即使当靶细胞是不可分割的细胞例如树突状细胞时，能够有效地将给定物质有效地递送到靶细胞的细胞核中的非病毒载体。 从外部依次具有第一脂质膜和第二脂质膜的第二脂质体膜，所述第一脂质膜具有膜融合能力，所述第二脂质膜在其表面上具有核转运肽。

公开(公告)号：EP1852436A1

公开(公告)日：2007-11-07

申请号：EP06713624.2

申请日：2006-02-14

申请人： Shionogi Co., Ltd.

发明人： UENAKA, Masaaki ,  HOZUMI, Yasuyuki ,  NOGUCHI, Kouichi ,  KOMURASAKI, Tadafumi

IPC分类号： C07D477/00

CPC分类号： C07D207/12 ,  C07D477/00

摘要： An object of the present invention is to provide a carbapenem synthetic intermediate which is advantageous in an industrial process. There are provided a process for producing Compound (I), or a pharmaceutically acceptable salt, or a solvate, or a crystal thereof, comprising reacting Compound (III) and Compound (IV) in the presence of the secondary amine, and a benzyl alcoholated crystal of Compound (I). There are further provided a method of deprotecting Compound (I) with a Pd catalyst, and a crystal of Compound (IV).

摘要翻译： 本发明的目的是提供一种在工业过程中有利的碳青霉烯合成中间体。 提供了一种制备化合物（I）或其药学上可接受的盐或其溶剂合物或其结晶的方法，其包括在仲胺存在下使化合物（III）和化合物（IV）与苄醇化的 化合物（I）的晶体。 还提供了使用Pd催化剂和化合物（IV）的结晶使化合物（I）脱保护的方法。

公开(公告)号：EP1844792A1

公开(公告)日：2007-10-17

申请号：EP05816775.0

申请日：2005-12-13

申请人： Shionogi Co., Ltd.

发明人： SUZUKI, Tsutomu ,  SAWADA, Takuko, c/o Shionogi & Co., Ltd. ,  ISHIHARA, Yasunobu, c/o Shionogi & Co., Ltd.

IPC分类号： A61K45/00 ,  A61K31/485 ,  A61P1/10

CPC分类号： A61K31/485 ,  A61K45/06

摘要： A therapeutic and/or prophylactic agent for constipation induced by a compound having an opioid µ receptor agonist activity, which agent comprises as an effective ingredient a compound having an opioid δ receptor antagonist activity, e.g., a compound of Formula (I):




(wherein R 1 represents hydrogen, lower alkyl, cycloalkyl lower alkyl or the like; R 2 and R 3 independently represent hydrogen, hydroxy or the like; R 4 is hydrogen, hydroxy or the like; R 5 is hydrogen; R 4 and R 5 may optionally form -O- or the like; R 6 represents hydrogen, lower alkyl or the like (wherein X represents -O- or -N(R 10 )-or the like; R 7 , R 8 , R 9a and R 9b independently represent hydrogen, lower alkyl, lower alkoxycarbonyl or the like; r represents an integer of 0 to 5; Y represents -CH- or the like; Z represents a crosslinkage composed of 2 to 5 atoms)
or a pharmaceutically acceptable salt thereof or a solvate of either.

摘要翻译： 一种由具有阿片样物质μ受体激动剂活性的化合物引起的便秘的治疗和/或预防剂，该药物包含作为有效成分的具有阿片受体拮抗剂活性的化合物，例如式（I）的化合物：（其中 R 1代表氢，低级烷基，环烷基低级烷基等; R 2和R 3独立地代表氢，羟基等; R 4是氢，羟基等; R 5是氢; R 4和R 5可以是 任选形成-O-等; R 6表示氢，低级烷基等（其中X表示-O-或-N（R 10） - 等; R 7，R 8，R 9a和R 9b独立地 表示氢，低级烷基，低级烷氧基羰基等; r表示0〜5的整数，Y表示-CH-等; Z表示2〜5个原子的交联键）或其药学上可接受的盐或溶剂合物 的任何一个。

公开(公告)号：EP1839655A1

公开(公告)日：2007-10-03

申请号：EP06711930.5

申请日：2006-01-19

申请人： Shionogi Co., Ltd.

发明人： SENO, Kaoru ,  SHINOSAKI, Toshihiro ,  HATA, Satoshi ,  YAMADA, Isamu ,  SATO, Hiroki ,  KATAOKA, Mikayo

IPC分类号： A61K31/167 ,  A61K31/17 ,  A61K31/18 ,  A61K31/27 ,  A61K31/277 ,  A61K31/341 ,  A61K31/343 ,  A61K31/36 ,  A61K31/381 ,  A61K31/382 ,  A61K31/395 ,  A61K31/40

CPC分类号： C07C305/24 ,  C07C235/64 ,  C07C255/57 ,  C07C271/28 ,  C07C309/76 ,  C07C311/04 ,  C07C311/08 ,  C07C311/21 ,  C07C311/29 ,  C07C317/40 ,  C07C323/12 ,  C07C323/62 ,  C07D211/96 ,  C07D213/40 ,  C07D213/74 ,  C07D239/47 ,  C07D243/08 ,  C07D295/135 ,  C07D317/54 ,  C07D319/18 ,  C07D333/20 ,  C07D333/58

摘要： A CTGF expression inhibitor comprising a compound of the formula I:

a pharmaceutically acceptable salt or solvate thereof as an active ingredient,
(wherein Y is hydroxy or a group of the formula: -NH-SO 2 -Y' (wherein Y' is optionally substituted aryl or optionally substituted alkyl), and
R 1 to R 9 are each independently hydrogen, halogen, optionally substituted alkyl, optionally substituted alkoxy or the like).

摘要翻译： 一种CTGF表达抑制剂，其包含式I化合物：其药学上可接受的盐或溶剂化物作为活性成分（其中Y是羟基或式-NH-SO 2 -Y'的基团（其中Y'任选地 取代的芳基或任选取代的烷基），R 1至R 9各自独立地为氢，卤素，任选取代的烷基，任选取代的烷氧基等。

公开(公告)号：EP1808427A2

公开(公告)日：2007-07-18

申请号：EP07008812.5

申请日：2000-06-26

申请人： SHIONOGI & CO., LTD.

发明人： Honma, Tsunetoshi ,  Hiramatsu, Yoshiharu ,  Mitsumori, Susumu

IPC分类号： C07C67/343

CPC分类号： C07F7/1836 ,  C07B2200/07 ,  C07C67/343 ,  C07C213/00 ,  C07C213/02 ,  C07C215/42 ,  C07C249/08 ,  C07C2602/42 ,  C07D333/68 ,  C07D333/70 ,  C07F7/188 ,  C07C69/716 ,  C07C251/44 ,  C07C251/50

摘要： The present invention provides a process for the preparation of a bicyclic aminoalcohol which comprises reacting a starting compound, nopinone (I), with XCH 2 COOR 1 wherein X is halogen, and R 1 is alkyl, in the presence of an additive and a base to produce a compound (II), converting it to oxime derivative (III), and reducing it with an aluminum hydride.

摘要翻译： 本发明提供了制备双环氨基醇的方法，该方法包括在添加剂和碱的存在下，使起始化合物，诺酮酮（I）与X为卤素的XCH 2 COOR 1和R 1为烷基反应 制备化合物（II），将其转化为肟衍生物（III），并用氢化铝还原。

公开(公告)号：EP1806342A1

公开(公告)日：2007-07-11

申请号：EP05800158.7

申请日：2005-10-28

申请人： SHIONOGI & CO., LTD.

发明人： ISHIZUKA, Natsuki, Shionogi & Co., Ltd. ,  SASATANI, Takashi, Shionogi & Co., Ltd. ,  HIRAMATSU, Yoshiharu, Shionogi & Co., Ltd. ,  INAGAKI, Masanao, Shionogi & Co., Ltd. ,  ODAN, Masahide, Shionogi & Co., Ltd. ,  HASHIZUME, Hiroshi, Shionogi & Co., Ltd. ,  MITSUMORI, Susumu, Shionogi & Co., Ltd. ,  FUJII, Yasuhiko, Shionogi & Co., Ltd. ,  FUKUI, Yoshikazu, Shionogi & Co., Ltd. ,  WATANABE, Hideaki, Shionogi & Co., Ltd. ,  SATO, Jun, Shionogi & Co., Ltd.

IPC分类号： C07D213/82

CPC分类号： C07D213/82

摘要： The present invention provides compounds having an agonistic activity to the cannabinoid receptor, which is represented by the formula (I):

wherein R 1 is optionally substituted C1-C8 alkyl and the like; R 2 is C1-C6 alkyl; R 3 is C1-C6 alkyl and the like; or R 2 and R 3 taken together with may form an optionally substituted 5 to 10 membered non-aromatic carbon ring; R 4 is hydrogen and the like; G is a group selected from the groups shown by the formula an the like:

wherein R 5 is hydrogen and the like; X 1 is a single bond and the like; X 2 is optionally substituted C1-C8 alkylene that may be replaced by one or two groups of -O-, or -N(R 6 )-, wherein R 6 is hydrogen and the like, and the like; X 3 is a single bond and the like;
a pharmaceutically acceptable salt or a solvate thereof, and pharmaceutical compositions, atopic dermatitis treating agents, and anti-pruritus agents, especially anti-pruritus agents for oral used and for external application, which each contains the said compound as an active ingredient.

摘要翻译： 本发明提供对大麻素受体具有激动作用的化合物，其由式（I）表示：其中R 1为任选取代的C 1 -C 8烷基等; R 2是C 1 -C 6烷基; R 3是C 1 -C 6烷基等; 或R 2和R 3可以一起形成任选取代的5至10元非芳族碳环; R 4是氢等; G为选自下式的基团：其中R 5为氢等; X 1是单键等; X 2是可以被一个或两个-O-或-N（R 6） - 基团取代的任选取代的C 1 -C 8亚烷基，其中R 6是氢等; X 3是单键等; 其药学上可接受的盐或溶剂合物，以及药物组合物，特应性皮炎治疗剂和抗瘙痒剂，特别是用于口服使用和外用的抗瘙痒剂，其各自含有所述化合物作为活性成分。

公开(公告)号：EP1806118A1

公开(公告)日：2007-07-11

申请号：EP05786004.1

申请日：2005-09-26

申请人： NIPRO CORPORATION ,  FUJIMORI KOGYO CO., LTD. ,  Shionogi Co., Ltd.

发明人： OMORI, Kenji, c/o NIPRO CORPORATION, ,  NIZUKA, Takeshi, c/o NIPRO CORPORATION, ,  SUDO, Dai, c/o NIPRO CORPORATION, 9-3, ,  FUJIMOTO, Manabu, c/o NIPRO CORPORATION, ,  MOTEKI, Masashi, c/o NIPRO CORPORATION, ,  SUZUKI, Toyoaki, c/o Fujimori Kogyo Co., Ltd., ,  MIURA, Koichi, c/o Fujimori Kogyo Co., Ltd., ,  IKEDA, Kaori, c/o Shionogi & Co., Ltd., ,  KASHIWAGI, Hideji, c/o Shionogi & Co., Ltd., ,  MYOJYO, Hidetoshi, c/o Shionogi & Co., Ltd.,

IPC分类号： A61J1/10 ,  A61J1/05 ,  B32B27/32

CPC分类号： A61J1/2093 ,  A61J1/10 ,  A61J1/2024 ,  A61M2207/00 ,  B32B3/02 ,  B32B15/08 ,  B32B15/20 ,  B32B27/08 ,  B32B27/32 ,  B32B27/325 ,  B32B27/36 ,  B32B2255/10 ,  B32B2255/205 ,  B32B2307/7242 ,  B32B2307/7246 ,  B32B2307/75 ,  B32B2439/46 ,  B32B2439/80 ,  Y10T428/13 ,  Y10T428/1303 ,  Y10T428/1352 ,  Y10T428/1359 ,  Y10T428/139

摘要： A medical container comprising a body for containing a medicament, the body of the medical container being formed of a multilayered film comprising (i) a layer formed of a linear polyolefin and (ii) a layer formed of a cyclic polyolefin adjacent to the layer (i), and the layer (i) formed of the linear polyolefin satisfying the following conditions (a) and/or (b):
Condition (a): an amount of a liquid component, which remains after Soxhlet's extraction with organic solvents followed by evaporation of the solvenst, is 0.2% by weight or less, and
Condition (b): a branching degree of a component, which remains after Soxhlet's extraction with n-hexane followed by evaporation of n-hexane, is 50 or less per 1,000 carbon atoms.

摘要翻译： 一种医疗容器，包括用于容纳药物的本体，所述医疗容器的主体由多层膜形成，所述多层膜包括（i）由线性聚烯烃形成的层和（ii）由邻近所述层的环状聚烯烃形成的层 i）和由线性聚烯烃形成的满足以下条件（a）和/或（b）的层（i）：条件（a）：索格利特用有机溶剂萃取后留下的液体组分的量， 溶剂的蒸发为0.2重量％以下，条件（b）：在索氏提取后，用正己烷蒸发后残留的成分的支化度为每1000个碳原子数为50以下 原子。

公开(公告)号：EP1801118A1

公开(公告)日：2007-06-27

申请号：EP05783456.6

申请日：2005-09-14

申请人： SHIONOGI & CO., LTD. ,  National Institute of Advanced Industrial Science and Technology

发明人： NISHIMURA, Shinichiro ,  HINOU, Hiroshi ,  FUMOTO, Masataka, Room 403, Flat Sapporo

IPC分类号： C07K14/435 ,  C07K7/06 ,  C07K7/08 ,  C12P21/02

CPC分类号： C12P21/005 ,  C07K14/4727 ,  C12P21/06

摘要： The invention aims at providing novel compounds useful as primer in producing mucin-type glycopeptides which are useful in a wide field including materials for biochemical research, drugs, and food and the production of which was difficult in the prior art; and a process for the production of glycopeptides by using the primers. The aim is attained by providing novel glycopeptide derivatives (represented by the general formula (I)) which each bear an aldehyde or ketone group at the end and each contain an amino acid residue cleavable with a protease; and an easy and simple process for the production of glycopeptides by using the derivative as the primer.

公开(公告)号：EP1787979A1

公开(公告)日：2007-05-23

申请号：EP05781598.7

申请日：2005-09-05

申请人： Shionogi Co., Ltd.

发明人： WATANABE, Fumihiko c/o Shionogi & Co., Ltd. ,  TAMURA, Yoshinori c/o Shionogi & Co., Ltd. ,  YOSHIKAWA, Naoki c/o Shionogi & Co., Ltd.

IPC分类号： C07C311/00

CPC分类号： C07D333/34 ,  C07C311/19 ,  C07C311/29 ,  C07C311/42 ,  C07C311/46 ,  C07C323/58 ,  C07C2601/08 ,  C07C2601/14 ,  C07D209/18 ,  C07D215/12 ,  C07D307/84 ,  C07D309/08 ,  C07D333/62

摘要： It is considered that MMP-13 inhibitors contribute to the treatment or prevention against the diseases caused by or related to activity of MMP-13, especially osteoarthritis (OA). Therefore, the development of MMP-13 inhibitors has been desired.
A compound represented by the general formula (I):

wherein Z is 1,4-phenylene and the like; R 1 is hydroxy and the like; R 2 is hydrogen atom, optionally substituted lower alkyl, and the like; R 12 is hydrogen atom; or R 2 and R 12 taken together with the adjacent carbon atom may form a ring; R 3 is hydrogen atom, optionally substituted lower alkyl, and the like; R 4 is halogen, lower alkyl, and the like; m is 0, 1, or 2; X is a bond, -C≡C-, and the like; Y is optionally substituted phenyl, optionally substituted naphthyl, and the like, its optically active substance, their pharmaceutically acceptable salt, or a solvate thereof.

摘要翻译： 认为MMP-13抑制剂有助于治疗或预防由MMP-13，特别是骨关节炎（OA）引起的或与MMP-13的活性有关的疾病。 因此，期望MMP-13抑制剂的发展。 由通式（I）表示的化合物：其中Z是1,4-亚苯基等; R 1是羟基等; R 2是氢原子，任选取代的低级烷基等; R 12是氢原子; 或R 2和R 12与相邻碳原子一起可以形成环; R 3是氢原子，任选取代的低级烷基等; R 4是卤素，低级烷基等; m为0,1或2; X是一个债券，-C¡C等等; Y是任选取代的苯基，任选取代的萘基等，其光学活性物质，其药学上可接受的盐或其溶剂化物。

公开(公告)号：EP1749539A2

公开(公告)日：2007-02-07

申请号：EP06024179.1

申请日：2001-07-30

申请人： Shionogi Co., Ltd.

发明人： Shiomi, Teruo ,  Hara, Seijiro

IPC分类号： A61K45/00 ,  A61K31/235 ,  A61K31/704 ,  A61P1/16

CPC分类号： A61K31/704 ,  A61K31/235

摘要： The present invention provides a new use of an agent that inhibits bile acid reabsorption. An agent that inhibits bile acid reabsorption is useful for the prevention of fatty liver.

摘要翻译： 本发明提供抑制胆汁酸重吸收的药剂的新用途。 抑制胆汁酸重吸收的药物可用于预防脂肪肝。