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1. 发明授权

US07005538B1 Thyroid receptor antagonists for the treatment of cardiac and metabolic disorders 失效
标题翻译：甲状腺受体拮抗剂用于治疗心脏和代谢紊乱
公开(公告)号：US07005538B1
公开(公告)日：2006-02-28
申请号：US10130434
申请日：2000-11-16
申请人： Johan Malm , Chris Litten , Theresa Apelqvist , Asa Hedfors , Peter Brandt , Karin Edvinsson , Sandra Gordon
发明人： Johan Malm , Chris Litten , Theresa Apelqvist , Asa Hedfors , Peter Brandt , Karin Edvinsson , Sandra Gordon
IPC分类号： C07C61/00
CPC分类号： C07D213/30 , A61K31/192 , A61K31/42 , A61K31/4402 , A61K31/47 , A61K31/59 , C07C59/64 , C07C59/72 , C07C59/90 , C07C205/37 , C07C217/76 , C07C233/56 , C07C255/54 , C07C311/51 , C07C2601/02 , C07D215/14 , C07D261/08 , C07D277/24 , C07D309/06 , C07D333/56 , A61K31/44 , A61K31/19 , A61K2300/00
摘要： This invention relates to novel compounds which are thyroid receptor ligands, preferably antagonists, and to methods for using such compounds in the treatment of cardiac arrhythmias, thyrotoxicosis and subclinical hyperthyrodism.
摘要翻译：本发明涉及作为甲状腺受体配体，优选拮抗剂的新化合物，以及使用这些化合物治疗心律失常，甲状腺毒症和亚临床甲状腺功能亢进的方法。

2. 发明授权

US07319163B2 Thyroid receptor antagonists for the treatment of cardiac and metabolic disorders 失效
标题翻译：甲状腺受体拮抗剂用于治疗心脏和代谢紊乱
公开(公告)号：US07319163B2
公开(公告)日：2008-01-15
申请号：US11166821
申请日：2005-06-24
申请人： Johan Malm , Chris Litten , Theresa Apelqvist , Asa Hedfors , Peter Brandt , Karin Edvinsson , Sandra Gordon
发明人： Johan Malm , Chris Litten , Theresa Apelqvist , Asa Hedfors , Peter Brandt , Karin Edvinsson , Sandra Gordon
IPC分类号： C07C9/22 , C07C9/28 , C07C309/00 , C07C259/00
CPC分类号： C07D213/30 , A61K31/192 , A61K31/42 , A61K31/4402 , A61K31/47 , A61K31/59 , C07C59/64 , C07C59/72 , C07C59/90 , C07C205/37 , C07C217/76 , C07C233/56 , C07C255/54 , C07C311/51 , C07C2601/02 , C07D215/14 , C07D261/08 , C07D277/24 , C07D309/06 , C07D333/56 , A61K31/44 , A61K31/19 , A61K2300/00
摘要： This invention relates to novel compounds which are thyroid receptor ligands, preferably antagonists, and to methods for using such compounds in the treatment of cardiac arrhythmias, thyrotoxicosis and subclinical hyperthyrodism.
摘要翻译：本发明涉及作为甲状腺受体配体，优选拮抗剂的新化合物以及用于治疗心律失常，甲状腺毒症和亚临床甲状腺功能亢进的方法。

3. 发明申请

US20050267206A1 Thyroid receptor antagonists for the treatment of cardiac and metabolic disorders 失效
标题翻译：甲状腺受体拮抗剂用于治疗心脏和代谢紊乱
公开(公告)号：US20050267206A1
公开(公告)日：2005-12-01
申请号：US11166821
申请日：2005-06-24
申请人： Johan Malm , Chris Litten , Theresa Apelqvist , Asa Hedfors , Peter Brandt , Karin Edvinsson , Sandra Gordon
发明人： Johan Malm , Chris Litten , Theresa Apelqvist , Asa Hedfors , Peter Brandt , Karin Edvinsson , Sandra Gordon
IPC分类号： A61K31/192 , A61K31/42 , A61K31/4402 , A61K31/47 , A61K31/59 , A61P5/14 , A61P9/06 , C07C59/64 , C07C59/72 , C07C59/90 , C07C205/37 , C07C217/76 , C07C233/56 , C07C255/54 , C07C311/51 , C07D213/30 , C07D215/14 , C07D261/08 , C07D277/24 , C07D309/06 , C07D333/56 , A61K31/277
CPC分类号： C07D213/30 , A61K31/192 , A61K31/42 , A61K31/4402 , A61K31/47 , A61K31/59 , C07C59/64 , C07C59/72 , C07C59/90 , C07C205/37 , C07C217/76 , C07C233/56 , C07C255/54 , C07C311/51 , C07C2601/02 , C07D215/14 , C07D261/08 , C07D277/24 , C07D309/06 , C07D333/56 , A61K31/44 , A61K31/19 , A61K2300/00
摘要： This invention relates to novel compounds which are thyroid receptor ligands, preferably antagonists, and to methods for using such compounds in the treatment of cardiac arrhythmias, thyrotoxicosis and subclinical hyperthyrodism.
摘要翻译：本发明涉及作为甲状腺受体配体，优选拮抗剂的新化合物以及用于治疗心律失常，甲状腺毒症和亚临床甲状腺功能亢进的方法。

4. 发明授权

US06465687B1 Thyroid receptor ligands and method 失效
标题翻译：甲状腺受体配体及方法
公开(公告)号：US06465687B1
公开(公告)日：2002-10-15
申请号：US09445888
申请日：2000-03-20
申请人： Yi-Lin Li , Ye Liu , Asa Hedfors , Johan Malm , Charlotta Mellin , Minsheng Zhang
发明人： Yi-Lin Li , Ye Liu , Asa Hedfors , Johan Malm , Charlotta Mellin , Minsheng Zhang
IPC分类号： C07C5900
CPC分类号： C07F9/3882 , C07C43/295 , C07C59/68 , C07C65/24 , C07C255/37 , C07F9/4056
摘要： Novel thyroid receptor ligands are provided which have the general formula (I) where R1 is alkyl of 1 to 4 carbons or cycloalkyl of 3 to 7 carbons; R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 3 carbons or cycloalkyl of 3 to 5 carbons, at least one of R2 and R3 being other than hydrogen; n is an integer from 0 to 4; R4 is an aliphatic hydrocarbon, an aromatic hydrocarbon, carboxylic acid ester thereof, alkenyl carboxylic acid or ester thereof, hydroxy, halogen, cyano, or a phosphonic acid or an ester thereof, or a pharmaceutically acceptible salt thereof. A method for treating diseases associated with metabolism dysfunction or which are dependent on the expression of a T3 regulated gene, such as obesity, hypercholesterolemia, osteoporosis, hypothyroidism, and goiter, is also provided.
摘要翻译：提供了具有通式（I）的新型甲状腺受体配体，其中R 1是1至4个碳的烷基或3至7个碳的环烷基; R2和R3相同或不同，为氢，卤素，1〜3个碳的烷基或3〜5个碳的环烷基，R2和R3中的至少一个不是氢; n为0〜4的整数; R4是脂族烃，芳烃，其羧酸酯，烯基羧酸或其酯，羟基，卤素，氰基或膦酸或其酯，或其药学上可接受的盐。还提供了用于治疗与代谢功能障碍相关的疾病或依赖于T3调节基因如肥胖，高胆固醇血症，骨质疏松症，甲状腺机能减退和甲状腺肿的表达的方法。

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