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公开(公告)号：EP1206436B1
公开(公告)日：2004-10-13
申请号：EP00951439.9
申请日：2000-07-25
IPC分类号： C07C63/64 , C07C57/26 , C07D213/80 , C07C61/24 , C07C69/757 , C07C233/63 , A61K31/167 , A61K31/215 , A61K31/4418 , A61P11/00 , A61P17/00
CPC分类号： C07D213/80 , C07C61/29 , C07C63/66 , C07C69/753 , C07C233/63 , C07C2602/08
摘要： This invention relates to new RAR selective retinoid agonists of formula (I) wherein the symbols are as defined in the specification to their pharmaceutically acceptable salts, individual isomers or to a racemic or non-racemic mixture; to pharmaceutical compositions containing them, and to methods for their use as therapeutic agents.
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公开(公告)号：EP1225878A1
公开(公告)日：2002-07-31
申请号：EP00972754.6
申请日：2000-10-13
IPC分类号： A61K31/00 , A61K31/192 , A61K31/353 , A61K31/44 , A61P11/00
CPC分类号： A61K31/44 , A61K31/00 , A61K31/192 , A61K31/195 , A61K31/24 , A61K31/352 , A61K31/355
摘要： This invention provides the use of RARη selective agonists for the manufacture of a medicament containing one or more such agonists for the treatment of emphysema and other diseases associated with alveolar damage. In another aspect, this invention provides the use of RAR agonists, preferably a RARη selective agonist for the manufacture of medicaments for promoting tropoelastin gene expression and alveolar matrix repair.
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公开(公告)号：EP1430024A1
公开(公告)日：2004-06-23
申请号：EP02764881.5
申请日：2002-09-11
IPC分类号： C07C275/42 , C07C335/22 , C07C279/18 , A61K31/192 , A61P11/00 , A61P17/00 , A61P35/00
CPC分类号： C07C275/42 , C07C2602/10
摘要： The current invention provide novel compounds, methods of treating or preventing emphysema, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders and methods for delivering formulations into the lung of a mammal suffering from emphysema, cancer and dermatological disorders.
摘要翻译： 本发明提供了新的化合物，治疗或预防肺气肿，癌症和皮肤病学的方法，适用于治疗或预防肺气肿，癌症和皮肤疾病的药物组合物和将制剂递送到患有肺气肿，癌症的哺乳动物的肺中的方法 和皮肤病。
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公开(公告)号：EP0775103A1
公开(公告)日：1997-05-28
申请号：EP95930430.0
申请日：1995-07-29
IPC分类号： A01N , A61K31 , A61P3 , A61P17 , A61P35 , A61P43 , C07C45 , C07C47 , C07C51 , C07C57 , C07C63 , C07C67 , C07C69 , C07D333 , C07F9
CPC分类号： C07F9/4056 , C07C45/29 , C07C45/298 , C07C45/63 , C07C47/24 , C07C47/277 , C07C57/50 , C07C2601/16 , C07D333/24 , C07C47/453 , C07C47/34 , C07C47/238 , C07C47/546 , C07C47/235
摘要： Compounds of formula (I) wherein R?1-R7, R10¿, X and the dotted bond have the meaning given in the specification, bind selectively to retinoid RXR receptors and are useful as antiproliferative agents for dermatological and oncological indications.
摘要翻译： PCT No.PCT / EP95 / 03021 Sec。 371日期1997年1月21日 102（e）日期1997年1月21日PCT提交1995年7月29日PCT公布。 出版物WO96 / 05165 日期：1996年2月22日其中R1-R7，R10，X和点键具有本说明书中给出的含义的式（I）化合物选择性地结合类视黄醇RXR受体，并且可用作皮肤病学和肿瘤学适应症的抗增生剂。
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公开(公告)号：EP1442032B1
公开(公告)日：2007-04-18
申请号：EP02802300.0
申请日：2002-10-21
IPC分类号： C07D311/58 , C07D335/06 , C07D215/12 , C07D409/04 , C07D409/12 , A61K31/38 , A61P17/00
CPC分类号： C07D335/06 , C07D215/12 , C07D311/58 , C07D409/04 , C07D409/12
摘要： The current invention provides novel heterocyclic retinoid compounds of formula (I), wherein R1 to R5, A,B,Z and n are as defined in the description and claims. The compounds of the present invention are useful for the treatment and/or prevention of diseases such as chronic obstructive pulmonary disease, cancer and dermatological disorders.
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公开(公告)号：EP1280757A2
公开(公告)日：2003-02-05
申请号：EP01947234.9
申请日：2001-04-23
IPC分类号： C07C69/82 , C07C63/64 , C07C65/26 , C07C65/28 , C07C69/94 , C07D311/00 , C07D263/00 , C07D215/12 , A61K31/19 , A61K31/235 , A61P11/00
CPC分类号： C07D213/30 , C07C63/64 , C07C65/26 , C07C65/28 , C07C69/76 , C07C69/80 , C07C69/90 , C07C255/33 , C07C271/58 , C07C2602/10 , C07D215/14 , C07D261/08 , C07D271/06 , C07D277/24 , C07D307/42 , C07D311/58 , C07D333/40 , C07D335/06
摘要： New RAR selective retinoid agonists of formula (I) wherein the symbols are as defined in the specification, and pharmaceutically active salts of carboxylic acids of formula (I), further the invention relates to the use of such retinoic acid receptor agonists, particularly retinoic acid receptor η(RARη) selective agonists for the treatment of emphysema and associated pulmonary diseases, as well as for the therapy and prophylaxis of dermatological disorders, for the therapy and prophylaxis of malignant and premalignant epithelial lesions, tumours and precancerous changes of the mucous membrane in the mouth, tongue, larynx, oesophagus, bladder, cervix and colon.
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7.发明公开TREATMENT OF T-HELPER CELL TYPE 2 MEDIATED IMMUNE DISEASES WITH RETINOID ANTAGONISTS 有权T辅助ZEL类型的治疗2介导的以维A拮抗剂免疫疾病
公开(公告)号：EP1030662A2
公开(公告)日：2000-08-30
申请号：EP98959850.3
申请日：1998-11-05
IPC分类号： A61K31/38 , A61K31/44 , A61K31/20 , A61K31/195 , A61K31/35 , A61K31/55 , A61K31/415 , A61K31/19 , A61K31/385
CPC分类号： C07C57/42 , A61K31/192 , A61K31/195 , A61K31/352 , A61K31/353 , A61K31/382 , A61K31/385 , A61K31/4184 , A61K31/4188 , A61K31/4439 , A61K31/551 , C07C57/48
摘要： Retinoids with retinoid receptor antagonistic activity called retinoid antagonists, pharmaceutically acceptable salts and pharmaceutically acceptable hydrolyzable esters thereof, have been found to be efficacious in the treatment of T-helper cell type 2 (Th2)-mediated immune diseases, such as immunoglobulin E (IgE)-mediated allergic diseases.
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公开(公告)号：EP1430023B1
公开(公告)日：2009-04-08
申请号：EP02774599.1
申请日：2002-09-11
IPC分类号： C07C275/28 , C07C279/18 , C07C335/16 , A61K31/17 , A61P17/00 , A61P31/00
CPC分类号： C07C275/42 , C07C2602/10 , C07D261/08 , C07D333/20
摘要： The current invention provide novel compounds, methods of treating or preventing emphysema, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders and methods for delivering formulations into the lung of a mammal suffering from emphysema, cancer and dermatological disorders.
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公开(公告)号：EP1280757B1
公开(公告)日：2005-08-17
申请号：EP01947234.9
申请日：2001-04-23
IPC分类号： C07C69/82 , C07C63/64 , C07C65/26 , C07C65/28 , C07C69/94 , C07D311/00 , C07D263/00 , C07D215/12 , A61K31/19 , A61K31/235 , A61P11/00
CPC分类号： C07D213/30 , C07C63/64 , C07C65/26 , C07C65/28 , C07C69/76 , C07C69/80 , C07C69/90 , C07C255/33 , C07C271/58 , C07C2602/10 , C07D215/14 , C07D261/08 , C07D271/06 , C07D277/24 , C07D307/42 , C07D311/58 , C07D333/40 , C07D335/06
摘要： New RAR selective retinoid agonists of formula (I) wherein the symbols are as defined in the specification, and pharmaceutically active salts of carboxylic acids of formula (I), further the invention relates to the use of such retinoic acid receptor agonists, particularly retinoic acid receptor η(RARη) selective agonists for the treatment of emphysema and associated pulmonary diseases, as well as for the therapy and prophylaxis of dermatological disorders, for the therapy and prophylaxis of malignant and premalignant epithelial lesions, tumours and precancerous changes of the mucous membrane in the mouth, tongue, larynx, oesophagus, bladder, cervix and colon.
摘要翻译： 含有双环稠合环的新化合物，其中一个是通过脂族链连接到环烷基或芳基部分的苯基部分及其药学活性盐，可用作RAR选择性类维生素A激动剂。 此外，这种视黄酸受体激动剂，特别是视黄酸受体γ（RARγ）选择性激动剂可用于治疗肺气肿和相关的肺部疾病，以及用于治疗和预防皮肤病学障碍，用于治疗和预防恶性肿瘤 和恶变前上皮病变，口腔，舌头，喉，食道，膀胱，子宫颈和结肠中的粘膜的肿瘤和癌前变化。
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10.发明授权
公开(公告)号：EP0862554B1
公开(公告)日：2004-10-20
申请号：EP96934302.9
申请日：1996-11-05
发明人： KLAUS, Michael , MOHR, Peter
IPC分类号： C07D213/80 , A61K31/44
CPC分类号： C07D213/80 , A61K31/44 , A61K31/455
摘要： Disclosed are compounds of formula (I) in which R1 stands for hydrogen or C¿1-6?-alkyl, R?2¿ stands for C¿1-6?-alkyl or adamantyl, R?3¿ stands for C¿1-6?-alkyl or hydroxy or R?2 and R3¿ together represent -(CR6R7)n-, R4 stands for C¿2-8?-alkyl, C2-8-alkenyl, C2-8-alkinyl, -OCH2R?5¿ or C¿2-8?-alkanoyl and, if R?3¿ is hydroxy, hydrogen, R5 stands for C¿1-6?-alkyl, C2-6-alkenyl or C2-6-alkinyl, R?6 and R7¿ independently of one another represent hydrogen or C¿1-6?-alkyl, Y represents oxygen or sulphur, and n is 3, 4 or 5. These compounds and pharmaceutically usable salts of carboxylic acids of formula (I) act as selective ligands of the retinoic acid η receptor and can be used for treating of epithelial lesions.
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