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1. 发明授权

US07288571B2 Thyroid receptor ligands and method II 失效
标题翻译：甲状腺受体配体及方法二
公开(公告)号：US07288571B2
公开(公告)日：2007-10-30
申请号：US11189654
申请日：2005-07-26
申请人： Jon Hangeland , Minsheng Zhang , Yolanda Caringal , Denis Ryono , Yi-Lin Li , Johan Malm , Ye Liu , Neeraj Garg , Chris Litten , Ana Maria Garcia Collazo , Konrad Koehler
发明人： Jon Hangeland , Minsheng Zhang , Yolanda Caringal , Denis Ryono , Yi-Lin Li , Johan Malm , Ye Liu , Neeraj Garg , Chris Litten , Ana Maria Garcia Collazo , Konrad Koehler
IPC分类号： A61K31/18 , C07C311/50
CPC分类号： C07D207/27 , C07C235/32 , C07C235/52 , C07C307/06 , C07C311/51 , C07C323/41 , C07C323/60 , C07D207/09 , C07D211/24 , C07D211/34 , C07D211/58 , C07D211/96 , C07D213/40 , C07D223/12 , C07D231/38 , C07D233/64 , C07D257/04 , C07D285/06 , C07D285/135 , C07D295/13 , C07D295/185 , C07D333/20
摘要： New thyroid receptor ligands are provided which have general formula (I) in which: n is an integer from 0 to 4; R1 is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, at least one of R2 and R3 being other than hydrogen; R4 is a carboxylic acid amide (CONR′R″) or an acylsulphonamide (CONHSO2R′) derivative, or a pharmaceutically acceptable salt thereof, and all stereolsom thereof; or when n is equal to or greater than one, R4 may be heteroaromatic moiety which may be substituted or unsubstituted, or an amine (NR′R″). R5 is hydrogen or an acyl (such as acetyl or benzoyl) or other group capable of bioconversion to generate the free phenol structure (wherein R5—H). In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependant upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount. Examples of such diseases associated with metabolism dysfunction or are dependent upon the expression of a T3 regulated gene include obesity, hypercholesterolemia, atherosclerosis, cardiac arrhythmias, depression, osteoporosis, hypothyroidism, goiter, thyroid cancer as well as glaucoma, congestive heart failure and skin disorders.
摘要翻译：提供了具有通式（I）的新甲状腺受体配体，其中：n为0至4的整数; R 1是卤素，三氟甲基或1至6个碳的烷基或3至7个碳的环烷基; R 2和R 3相同或不同，为氢，卤素，1至4个碳的烷基或3至5个碳的环烷基，R 1， SUB 2和R 3不是氢; R 4是羧酸酰胺（CONR'R“）或酰基磺酰胺（CONHSO 2 R'）衍生物或其药学上可接受的盐及其所有立体异构体; 或当n等于或大于1时，R 4可以是可被取代或未取代的杂芳族部分，或胺（NR'R“）。 R 5是氢或酰基（如乙酰基或苯甲酰基）或能够生物转化以产生游离酚结构的其它基团（其中R 5 -H）。此外，提供了一种用于预防，抑制或治疗与代谢功能障碍相关的疾病或依赖于T 3 N调节基因的表达的方法，其中如上所述的化合物以治疗有效量。与代谢功能障碍相关或依赖于T 3受体基因表达的这种疾病的实例包括肥胖症，高胆固醇血症，动脉粥样硬化，心律失常，抑郁症，骨质疏松症，甲状腺机能减退，甲状腺肿，甲状腺癌以及青光眼，充血性心力衰竭和皮肤疾病。

2. 发明授权

US06989402B1 Thyroid receptor ligands and method II 失效
标题翻译：甲状腺受体配体及方法二
公开(公告)号：US06989402B1
公开(公告)日：2006-01-24
申请号：US09868889
申请日：1999-12-23
申请人： Jon Hangeland , Minsheng Zhang , Yolanda Caringal , Denis Ryono , Yi-Lin Li , Johan Malm , Ye Liu , Neeraj Garg , Chris Litten , Ana Maria Garcia Collazo , Konrad Koehler
发明人： Jon Hangeland , Minsheng Zhang , Yolanda Caringal , Denis Ryono , Yi-Lin Li , Johan Malm , Ye Liu , Neeraj Garg , Chris Litten , Ana Maria Garcia Collazo , Konrad Koehler
IPC分类号： A61K31/44 , A61K31/192 , A61K31/40 , A61K31/4174 , C07D211/56 , C07D213/72 , C07D229/38 , C07D265/30 , C07D241/04 , C07D207/14
CPC分类号： C07D207/27 , C07C235/32 , C07C235/52 , C07C307/06 , C07C311/51 , C07C323/41 , C07C323/60 , C07D207/09 , C07D211/24 , C07D211/34 , C07D211/58 , C07D211/96 , C07D213/40 , C07D223/12 , C07D231/38 , C07D233/64 , C07D257/04 , C07D285/06 , C07D285/135 , C07D295/13 , C07D295/185 , C07D333/20
摘要： New thyroid receptor ligands are provided which have general formula (I) in which: n is an integer from 0 to 4; R1 is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, at least one of R2 and R3 being other than hydrogen; R4 is a carboxylic acid amide (CONR′R″) or an acylsulphonamide (CONHSO2R′) derivative, or a pharmaceutically acceptable salt thereof, and all stereoisomers thereof; or when n is equal to or greater than one, R4 may be a heteroaromatic moiety which may be substituted or unsubstituted, or an amine (NR′R″). R5 is hydrogen or an acyl (such as acetyl or benzoyl) or other group capable of bioconversion to generate the free phenol structure (wherein R5=H). In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount. Examples of such diseases associated with metabolism dysfunction or are dependent upon the expression of a T3 regulated gene include obesity, hypercholesterolemia, atherosclerosis, cardiac arrhythmias, depression, osteoporosis, hypothyroidism, goiter, thyroid cancer as well as glaucoma, congestive heart failure and skin disorders.
摘要翻译：提供了具有通式（I）的新甲状腺受体配体，其中：n为0至4的整数; R 1是卤素，三氟甲基或1至6个碳的烷基或3至7个碳的环烷基; R 2和R 3相同或不同，为氢，卤素，1至4个碳的烷基或3至5个碳的环烷基，R 1， SUB 2和R 3不是氢; R 4是羧酸酰胺（CONR'R“）或酰基磺酰胺（CONHSO 2 R'）衍生物或其药学上可接受的盐及其所有立体异构体; 或当n等于或大于1时，R 4可以是可被取代或未取代的杂芳族部分，或胺（NR'R“）。 R 5是氢或酰基（例如乙酰基或苯甲酰基）或能够生物转化以产生游离酚结构（其中R 5 = H）的其它基团。此外，提供了一种用于预防，抑制或治疗与代谢功能障碍相关的疾病或依赖于T 3 N调节基因的表达的方法，其中如上所述的化合物以治疗有效量。与代谢功能障碍相关或依赖于T 3受体基因表达的这种疾病的实例包括肥胖症，高胆固醇血症，动脉粥样硬化，心律失常，抑郁症，骨质疏松症，甲状腺机能减退，甲状腺肿，甲状腺癌以及青光眼，充血性心力衰竭和皮肤疾病。

3. 发明申请

US20050282872A1 Novel thyroid receptor ligands and method II 失效
标题翻译：新型甲状腺受体配体及方法二
公开(公告)号：US20050282872A1
公开(公告)日：2005-12-22
申请号：US11189654
申请日：2005-07-26
申请人： Jon Hangeland , Minsheng Zhang , Yolanda Caringal , Denis Ryono , Yi-Lin Li , Johan Malm , Ye Liu , Neeraj Garg , Chris Litten , Ana Collazo , Konrad Koehler
发明人： Jon Hangeland , Minsheng Zhang , Yolanda Caringal , Denis Ryono , Yi-Lin Li , Johan Malm , Ye Liu , Neeraj Garg , Chris Litten , Ana Collazo , Konrad Koehler
IPC分类号： C07D233/88 , A61K31/381 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/4168 , A61K31/433 , A61K31/44 , A61K31/4409 , A61K31/495 , A61K31/55 , A61K45/00 , A61P3/04 , A61P3/06 , A61P5/14 , A61P9/06 , A61P9/10 , A61P17/00 , A61P17/02 , A61P17/04 , A61P17/06 , A61P19/10 , A61P25/24 , A61P27/06 , A61P35/00 , C07C235/32 , C07C235/34 , C07C235/52 , C07C307/06 , C07C311/00 , C07C311/51 , C07C323/41 , C07C323/59 , C07C323/60 , C07D207/09 , C07D207/26 , C07D207/27 , C07D211/24 , C07D211/34 , C07D211/58 , C07D211/60 , C07D211/96 , C07D213/38 , C07D213/40 , C07D213/74 , C07D223/12 , C07D231/38 , C07D233/54 , C07D241/04 , C07D257/04 , C07D285/06 , C07D285/12 , C07D285/125 , C07D285/135 , C07D295/13 , C07D295/185 , C07D333/20 , C07D333/34 , A61K31/426
CPC分类号： C07D207/27 , C07C235/32 , C07C235/52 , C07C307/06 , C07C311/51 , C07C323/41 , C07C323/60 , C07D207/09 , C07D211/24 , C07D211/34 , C07D211/58 , C07D211/96 , C07D213/40 , C07D223/12 , C07D231/38 , C07D233/64 , C07D257/04 , C07D285/06 , C07D285/135 , C07D295/13 , C07D295/185 , C07D333/20
摘要： New thyroid receptor ligands are provided which have general formula (I) in which: n is an integer from 0 to 4; R1 is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; R2 and R3 are the same or differential hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, at least one of R2 and R3 being other than hydrogen; R4 is a carboxylic acid thereof; or when n is equal to or greater than one, R4 may be heteroaromatic moiety which may be substituted or unsubstituted, or an amine (NR′R″). R5 is hydrogen or an acyl (such as acetyl or benzoyl) or other group capable of bioconversion to generate the free phenol structure (wherein R5—H). In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependant upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount. Examples of such diseases associated with metabolism dysfunction or are dependent upon the expression of a T3 regulated gene include obesity, hypercholesterolemia, atherosclerosis, cardiac arrhythmias, depression, osteoporosis, hypothyroidism, goiter, thyroid cancer as well as glaucoma, congestive heart failure and skin disorders.
摘要翻译：提供了具有通式（I）的新甲状腺受体配体，其中：n为0至4的整数; R 1是卤素，三氟甲基或1至6个碳的烷基或3至7个碳的环烷基; R 2和R 3是相同或不同的氢，卤素，1至4个碳的烷基或3至5个碳的环烷基，R 1， 2和R 3不是氢; R 4是其羧酸; 或当n等于或大于1时，R 4可以是可被取代或未取代的杂芳族部分，或胺（NR'R“）。 R 5是氢或酰基（如乙酰基或苯甲酰基）或能够生物转化以产生游离酚结构的其它基团（其中R 5 -H）。此外，提供了一种用于预防，抑制或治疗与代谢功能障碍相关的疾病或依赖于T 3 N调节基因的表达的方法，其中如上所述的化合物以治疗有效量。与代谢功能障碍相关或依赖于T 3受体基因表达的这种疾病的实例包括肥胖症，高胆固醇血症，动脉粥样硬化，心律失常，抑郁症，骨质疏松症，甲状腺机能减退，甲状腺肿，甲状腺癌以及青光眼，充血性心力衰竭和皮肤疾病。

4. 发明授权

US07199265B2 Thyroid receptor ligands, pharmaceutical compositions comprising them and their use in the treatment of disorders influenced by thyroid hormones 失效
标题翻译：甲状腺受体配体，包含它们的药物组合物及其用于治疗受甲状腺激素影响的疾病的用途
公开(公告)号：US07199265B2
公开(公告)日：2007-04-03
申请号：US10311524
申请日：2001-06-15
申请人： Li Yi-Lin , Johan Malm , Chris Litten , Ana Maria Garcia Collazo , Neeraj Garg
发明人： Li Yi-Lin , Johan Malm , Chris Litten , Ana Maria Garcia Collazo , Neeraj Garg
IPC分类号： C07C321/00 , C07C315/00 , C07C229/00 , C07D215/00 , C07D209/00
CPC分类号： C07D213/70 , A61K31/195 , A61K31/40 , A61K31/41 , C07C233/25 , C07C233/27 , C07C233/60 , C07C233/75 , C07C235/34 , C07C237/40 , C07C311/08 , C07C311/13 , C07C311/21 , C07C311/24 , C07C311/29 , C07C335/18 , C07C2601/04 , C07C2601/14 , C07C2601/18 , C07D209/34 , C07D209/42 , C07D215/48 , C07D217/26 , C07D265/36 , C07D295/15 , A61K2300/00
摘要： This invention relates to compounds of the formula (I) which are thyroid receptor ligands, and are preferably selective for the thyroid hormone receptor β, to methods of preparing such compounds and to methods for using such compounds such as in the regulation of metabolism.
摘要翻译：本发明涉及甲状腺受体配体的式（I）化合物，优选甲状腺激素受体β的选择性，制备这些化合物的方法以及使用这些化合物如调节代谢的方法。

5. 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。

6. 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。

7. 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。

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