公开(公告)号：EP0685234B1

公开(公告)日：2000-05-10

申请号：EP94907061.9

申请日：1994-02-17

申请人： NIPPON SHINYAKU COMPANY, LIMITED

发明人： YANO, Junichi ,  OHGI, Tadaaki

IPC分类号： A61K47/10 ,  A61K47/44 ,  A61K9/127

CPC分类号： A61K31/70 ,  A61K9/1272 ,  C07C229/12 ,  C07C237/08 ,  C07C271/16 ,  C07C271/20 ,  C07C279/20 ,  C07C333/04 ,  C07D295/13 ,  C07F9/4075

公开(公告)号：EP0865446A1

公开(公告)日：1998-09-23

申请号：EP96942315.0

申请日：1996-12-06

申请人： HOECHST MARION ROUSSEL

发明人： KITAMURA, Kazuyuki ,  KOMIYAMA, Osamu ,  INAZU, Mizuho ,  BARON, Roland ,  GADEK, Thomas ,  KNOLLE, Jochen ,  STILZ, Han-Ulrich ,  WEHNER, Volkmar ,  MCDOWELL, Robert, S.

IPC分类号： C07D233 ,  A61K31 ,  A61K38 ,  A61P19 ,  A61P43 ,  C07C271 ,  C07C279 ,  C07K5 ,  C07K7 ,  C07K14

CPC分类号： C07K5/0821 ,  A61K38/04 ,  A61K38/05 ,  A61K38/07 ,  A61K38/12 ,  A61K38/1703 ,  A61K38/39 ,  C07C271/22 ,  C07C279/08 ,  C07C279/20 ,  C07K5/0202 ,  C07K5/0817 ,  C07K5/1019 ,  C07K5/1024 ,  C07K14/46 ,  C07K14/745 ,  C07K14/78

摘要： The object is to provide a promoting agent for bone formation, a therapeutic method for bone formation and a process for preparing a promoting agent for bone formation. A promoting agent for bone formation which comprises at least one of kistrin, echstatin, a peptide or polypeptide containing the amino acid sequence ArgGlyAsp in the molecule such as a peptide represented by Gly-Arg-Gly-Asp-Ser or a compound represented by general formula (IX) and so on, as well as a biologically acceptable salt thereof, wherein R16 represents -N(R20)2 (R20 represents a hydrogen atom or a C1-C4 alkyl group), R17 represents a hydrogen atom or a C1-C4 alkyl group, R18 represents a hydrogen atom, a C1-C4 alkyl group and so on, R19 represents OH, NH2 and so on, Y represents -NH-, -O- or a direct bond, a represents 1-3, b represents 1 or 2, c represents 0 or 1 and d represents 0 or 1.

公开(公告)号：EP0685457A4

公开(公告)日：1996-09-18

申请号：EP94907060

申请日：1994-02-17

申请人： NIPPON SHINYAKU CO LTD

发明人： YANO JUNICHI ,  OHGI TADAAKI

IPC分类号： A61K31/70 ,  A61K9/127 ,  A61K9/52 ,  A61K9/66 ,  A61K47/10 ,  A61K47/24 ,  A61K47/44 ,  C07C229/06 ,  C07C229/12 ,  C07C237/08 ,  C07C271/16 ,  C07C271/20 ,  C07C279/04 ,  C07C279/20 ,  C07C307/02 ,  C07C333/04 ,  C07D207/08 ,  C07D211/08 ,  C07D241/04 ,  C07D265/30 ,  C07D295/13 ,  C07F9/40

CPC分类号： A61K31/70 ,  A61K9/1272 ,  C07C229/12 ,  C07C237/08 ,  C07C271/16 ,  C07C271/20 ,  C07C279/20 ,  C07C333/04 ,  C07D295/13 ,  C07F9/4075

摘要： The invention aims at providing a device comprising lipids that act like the so-called cationic liposome and are reduced in toxicity and the lipids as the constituent of the device. The invention compounds are exemplified by 3-0-(4-dimethylaminobutanoyl)-1,2-0-dioleylglycerol, 3-0-(2-dimethylaminoethyl)carbamoyl-1,2-0-dioleylglycerol, 3-0-(2-diethylaminoethyl)carbamoyl-1,2-0-dioleylglycerol, and 2-0-(2-diethylaminoethyl)-carbamoyl-1,3-0-dioleylglycerol. The device comprises these lipids and phospholipids. The device enables, when administered together with, for example, a double-stranded RNA, the RNA to migrate to the action site safely.

公开(公告)号：EP0685457A1

公开(公告)日：1995-12-06

申请号：EP94907060.1

申请日：1994-02-17

申请人： NIPPON SHINYAKU COMPANY, LIMITED

发明人： YANO, Junichi ,  OHGI, Tadaaki

IPC分类号： C07C229/06 ,  C07C237/08 ,  C07C271/16 ,  C07C279/04 ,  C07C307/02 ,  C07D207/08 ,  C07D211/08 ,  C07D241/04 ,  C07D265/30 ,  C07F9/40

CPC分类号： A61K31/70 ,  A61K9/1272 ,  C07C229/12 ,  C07C237/08 ,  C07C271/16 ,  C07C271/20 ,  C07C279/20 ,  C07C333/04 ,  C07D295/13 ,  C07F9/4075

摘要： The invention aims at providing a device comprising lipids that act like the so-called cationic liposome and are reduced in toxicity and the lipids as the constituent of the device. The invention compounds are exemplified by 3-0-(4-dimethylaminobutanoyl)-1,2-0-dioleylglycerol, 3-0-(2-dimethylaminoethyl)carbamoyl-1,2-0-dioleylglycerol, 3-0-(2-diethylaminoethyl)carbamoyl-1,2-0-dioleylglycerol, and 2-0-(2-diethylaminoethyl)-carbamoyl-1,3-0-dioleylglycerol. The device comprises these lipids and phospholipids. The device enables, when administered together with, for example, a double-stranded RNA, the RNA to migrate to the action site safely.

摘要翻译： 本发明的目的在于提供一种装置，其包含像所谓的阳离子脂质体那样起作用并且毒性降低的脂质和作为装置成分的脂质。 本发明化合物的实例是3-0-（4-二甲基氨基丁酰基）-1,2-二油基甘油，3-0-（2-二甲基氨基乙基）氨基甲酰基-1,2-二油基甘油，3-0-（2- 二乙基氨基乙基）氨基甲酰基-1,2-二油基甘油和2-0-（2-二乙基氨基乙基） - 氨基甲酰基-1,3-0-二油基甘油。 该装置包括这些脂质和磷脂。 当与例如双链RNA一起施用时，该装置能够安全地迁移到作用部位的RNA。

公开(公告)号：EP2121639B1

公开(公告)日：2013-10-16

申请号：EP07856396.2

申请日：2007-12-06

申请人： Bayer CropScience AG

发明人： AHRENS, Hartmut ,  DIETRICH, Hansjörg ,  AULER, Thomas ,  HILLS, Martin ,  KEHNE, Heinz ,  FEUCHT, Dieter ,  HERRMANN, Stefan ,  KATHER, Kristian ,  LEHR, Stefan

IPC分类号： C07D251/18 ,  A01N43/68 ,  C07C279/26

CPC分类号： C07D251/18 ,  A01N43/68 ,  C07C279/20 ,  C07C279/26

公开(公告)号：EP2276727A1

公开(公告)日：2011-01-26

申请号：EP09751121.6

申请日：2009-05-01

申请人： The University of North Carolina At Chapel Hill

发明人： HUANG, Leaf ,  CHEN, Yunching ,  SEN, Joyeeta ,  BATHULA, Surendar, Reddy ,  CHONO, Sumio ,  LI, Shyh-Dar ,  HACKETT, Michael

IPC分类号： C07C279/10 ,  C07C279/20 ,  A61K31/155 ,  A61P35/00

CPC分类号： C07C279/10 ,  A61K9/1271 ,  A61K9/1272 ,  A61K47/6911 ,  C07C279/20 ,  C12N15/88

摘要： Provided herein are novel cationic lipids, compositions comprising the cationic lipids, and methods of using the cationic lipids. In some claims, the cationic lipids have cytotoxic activity and can be used alone or in combination with a cytotoxic bioactive compound to kill a cell. In some of these claims, the cationic lipid enhances the cytotoxic activity of the cytotoxic bioactive compound. Methods for treating a subject afflicted with a disease or unwanted condition are provided, wherein the method comprises administering a delivery system comprising a novel cationic lipid to the subject. The invention further provides methods for making delivery systems comprising the novel cationic lipids of the invention.

公开(公告)号：EP0820991B1

公开(公告)日：2007-08-29

申请号：EP97112198.3

申请日：1997-07-17

申请人： HOECHST AKTIENGESELLSCHAFT ,  GENENTECH, INC.

发明人： Wehner, Volkmar, Dr. ,  Knolle, Jochen, Dr. ,  Stilz, Hans Ulrich, Dr. ,  Gourvest, Jean-Francois, Dr. ,  Carniato, Denis, Dr. ,  Gadek, Thomas, Richard, Dr. ,  Mcdowell, Robert, Dr. ,  Pitti, Robert Maurice ,  Bodary, Sarah Carherine, Dr.

IPC分类号： C07D239/16 ,  C07D233/48 ,  C07C279/22 ,  C07C279/20 ,  A61K31/415 ,  A61K31/505

CPC分类号： C07C277/08 ,  C07C279/20 ,  C07C2603/74 ,  C07D233/48 ,  C07D239/16 ,  C07C279/22

公开(公告)号：EP1042301B1

公开(公告)日：2002-11-20

申请号：EP98966287.9

申请日：1998-12-10

申请人： Aventis Pharma Deutschland GmbH ,  Genentech, Inc.

发明人： PEYMAN, Anuschirwan ,  KNOLLE, Jochen ,  BREIPOHL, Gerhard ,  SCHEUNEMANN, Karl-Heinz ,  CARNIATO, Denis ,  GOURVEST, Jean-François ,  GADEK, Thomas ,  MCDOWELL, Robert ,  BODARY, Sarah, Catherine ,  CUTHBERTSON, Robert, Andrew ,  FERRARA, Napoleane

IPC分类号： C07D239/16 ,  C07C279/20 ,  A61K31/505

CPC分类号： C07C279/20 ,  C07D239/16

摘要： The present invention relates to acylguanidine derivatives of formula (I) in which R?1, R2, R4, R5, R6¿, A, m and n have the meanings indicated in the patent claims, their physiologically tolerable salts and their prodrugs. The compounds of formula (I) are valuable pharmaceutical active ingredients. They are vitronectin receptor antagonists and inhibitors of bone resorption by osteoclasts and are suitable, for example, for the therapy or prophylaxis of diseases which are caused at least partially by an undesired extend of bone resorption, for example of osteoporosis. The invention furthermore relates to processes for the preparation of compounds of formula (I), their use, in particular as pharmaceutical active ingredients, and pharmaceutical preparations comprising them.

公开(公告)号：EP0685234A4

公开(公告)日：1997-10-22

申请号：EP94907061

申请日：1994-02-17

申请人： NIPPON SHINYAKU CO LTD

发明人： YANO JUNICHI ,  OHGI TADAAKI

IPC分类号： A61K31/70 ,  A61K9/127 ,  A61K9/52 ,  A61K9/66 ,  A61K47/10 ,  A61K47/24 ,  A61K47/44 ,  C07C229/06 ,  C07C229/12 ,  C07C237/08 ,  C07C271/16 ,  C07C271/20 ,  C07C279/04 ,  C07C279/20 ,  C07C307/02 ,  C07C333/04 ,  C07D207/08 ,  C07D211/08 ,  C07D241/04 ,  C07D265/30 ,  C07D295/13 ,  C07F9/40

CPC分类号： A61K31/70 ,  A61K9/1272 ,  C07C229/12 ,  C07C237/08 ,  C07C271/16 ,  C07C271/20 ,  C07C279/20 ,  C07C333/04 ,  C07D295/13 ,  C07F9/4075

摘要： The invention aims at effectively utilizing a single-stranded nucleic acid copolymer, in particular, poly(adenylic acid-uridylic acid) and providing a drug composition having an antitumor effect. An example of the drug composition of the invention is one containing a lipid device, such as Lipofecting®, 3-0-(4-dimethylaminobutanoyl)-1,2-0-dioleylglycerol, 3-0-(2-dimethylaminoethyl)carbamoyl-1,2-0-dioleylglycerol, 3-0-(2-diethylaminoethyl)-carbamoyl-1,2-0-dioleylglycerol or 2-0-(2-diethyl-aminoethyl)carbamoyl-1,3-0-dioleylglycerol, and poly(adenylic acid-uridylic acid).

摘要翻译： 本发明的目的在于提供一种装置，其包含像所谓的阳离子脂质体那样起作用并且毒性降低的脂质和作为装置成分的脂质。 本发明化合物的实例是3-0-（4-二甲基氨基丁酰基）-1,2-二油基甘油，3-0-（2-二甲基氨基乙基）氨基甲酰基-1,2-二油基甘油，3-0-（2- 二乙基氨基乙基）氨基甲酰基-1,2-二油基甘油和2-0-（2-二乙基氨基乙基） - 氨基甲酰基-1,3-0-二油基甘油。 该装置包括这些脂质和磷脂。 当与例如双链RNA一起施用时，该装置能够安全地迁移到作用部位的RNA。

公开(公告)号：EP0685234A1

公开(公告)日：1995-12-06

申请号：EP94907061.9

申请日：1994-02-17

申请人： NIPPON SHINYAKU COMPANY, LIMITED

发明人： YANO, Junichi ,  OHGI, Tadaaki

IPC分类号： A61K31/70 ,  A61K47/24 ,  A61K47/44

CPC分类号： A61K31/70 ,  A61K9/1272 ,  C07C229/12 ,  C07C237/08 ,  C07C271/16 ,  C07C271/20 ,  C07C279/20 ,  C07C333/04 ,  C07D295/13 ,  C07F9/4075

摘要： The invention aims at effectively utilizing a single-stranded nucleic acid copolymer, in particular, poly(adenylic acid-uridylic acid) and providing a drug composition having an antitumor effect. An example of the drug composition of the invention is one containing a lipid device, such as Lipofecting®, 3-O-(4-dimethylaminobutanoyl)-1,2-O-dioleylglycerol, 3-O-(2-dimethylaminoethyl)carbamoyl-1,2-O-dioleylglycerol, 3-O-(2-diethylaminoethyl)-carbamoyl-1,2-O-dioleylglycerol or 2-O-(2-diethyl-aminoethyl)carbamoyl-1,3-O-dioleylglycerol, and poly(adenylic acid-uridylic acid).

摘要翻译： 本发明旨在有效利用单链核酸共聚物，特别是聚（腺苷酸 - 尿苷酸）并提供具有抗肿瘤作用的药物组合物。 本发明的药物组合物的实例是含有脂质装置的脂肪装置，例如Lipofecting TM，3-O-（4-二甲基氨基丁酰）-1,2-O-二油基甘油，3-O-（2-二甲基氨基乙基） 3-O-（2-二乙基氨基乙基） - 氨基甲酰基-1,2-二油基甘油或2-O-（2-二乙基 - 氨基乙基）氨基甲酰基-1,3-O-二油基甘油，和 聚（腺苷酸 - 尿苷酸）。