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1. 发明授权

US07342127B2 Substituted anilide ligands for the thyroid receptor 有权
标题翻译：用于甲状腺受体的取代苯胺配体
公开(公告)号：US07342127B2
公开(公告)日：2008-03-11
申请号：US10763878
申请日：2004-01-23
申请人： William N. Washburn , Wei Meng , Denis E. Ryono , Bruce A. Ellsworth , Thomas Ericsson , Mahmoud Rahimi-Ghadim , Neeraj Garg , Johan Malm
发明人： William N. Washburn , Wei Meng , Denis E. Ryono , Bruce A. Ellsworth , Thomas Ericsson , Mahmoud Rahimi-Ghadim , Neeraj Garg , Johan Malm
IPC分类号： C07C54/00 , C07C315/00 , C07C229/00 , A01N37/12
CPC分类号： A61K45/06 , A61K31/195 , A61K31/277 , A61K31/44 , C07C233/25 , A61K2300/00
摘要： Novel thyroid receptor ligands are provided having the general formula I wherein X, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined herein. In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolic dysfunction or which are dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.
摘要翻译：提供了具有通式I的新型甲状腺受体配体，其中X，R 1，R 2，R 3，R 4， R 5，R 6，R 7，R 8，R 9， R 11，R 11，R 12和R 13如本文所定义。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病症或依赖于T 3 N调节基因的表达的方法，其中将如上所述的化合物施用于治疗有效量。

2. 发明申请

US20050171104A1 Novel thyroid receptor ligands 审中-公开
标题翻译：新型甲状腺受体配体
公开(公告)号：US20050171104A1
公开(公告)日：2005-08-04
申请号：US10510645
申请日：2003-02-10
申请人： Mahmoud Rahimi-Ghadim , Neeraj Garg , Johan Malm
发明人： Mahmoud Rahimi-Ghadim , Neeraj Garg , Johan Malm
IPC分类号： A61K31/192 , A61K31/42 , A61K31/421 , A61K31/4245 , A61K31/4402 , A61K31/53 , A61K31/59 , A61P1/16 , A61P3/00 , A61P5/14 , A61P5/16 , A61P9/00 , A61P9/04 , A61P9/06 , A61P17/00 , A61P17/02 , A61P17/06 , A61P17/14 , A61P25/32 , A61P31/14 , A61P43/00 , C07C59/72 , C07C65/26 , C07D209/12 , C07D213/30 , C07D251/18 , C07D261/08 , C07D263/32 , C07D271/06 , C07D413/04 , A61K31/194 , A61K31/44
CPC分类号： C07D213/30 , C07D209/12 , C07D251/18 , C07D261/08 , C07D263/32 , C07D271/06 , C07D413/04
摘要： This invention relates to novel compounds according to the general formula: which are thyroid receptor ligands, preferably antagonists, partial antagonists or partial agonists and to methods for using such compounds in the treatment of cardiac and metabolic disorders, such as cardiac arrhythmias, thyro-toxicosis, subclinical hyperthyrodism and liver diseases.
摘要翻译：本发明涉及根据通式的新化合物：其为甲状腺受体配体，优选拮抗剂，部分拮抗剂或部分激动剂，以及使用这些化合物治疗心脏和代谢紊乱如心律失常，甲状腺中毒的方法，亚临床甲状腺功能亢进和肝脏疾病。

3. 发明申请

US20090220598A1 Stable Oral Pharmaceutical Composition Containing Thyroid Hormone Receptor Agonists 审中-公开
标题翻译：含有甲状腺激素受体激动剂的稳定的口服药物组合物
公开(公告)号：US20090220598A1
公开(公告)日：2009-09-03
申请号：US12225631
申请日：2007-03-27
申请人： Neeraj Garg , Venkatramana M. Rao , Rajesh B. Gandhi , William N. Washburn , Konrad Koehler , Johan Malm
发明人： Neeraj Garg , Venkatramana M. Rao , Rajesh B. Gandhi , William N. Washburn , Konrad Koehler , Johan Malm
IPC分类号： A61K9/30 , A61K31/235 , A61K31/192
CPC分类号： A61K9/2077 , A61K9/1676 , A61K9/2846 , A61K31/185 , A61K31/215 , A61K45/06 , A61K2300/00
摘要： Compositions are described in which certain thyroid hormone receptor-binding compounds are formulated together with either an enteric coating, an antioxidant, or both an enteric coating and an antioxidant. Such formulation acts to prevent the formation of undesired reaction products in vivo.
摘要翻译：描述了其中某些甲状腺激素受体结合化合物与肠溶衣，抗氧化剂或肠溶衣和抗氧化剂一起配制的组合物。这种制剂用于防止在体内形成不期望的反应产物。

4. 发明授权

US08263659B2 Thyroid receptor ligands 失效
标题翻译：甲状腺受体配体
公开(公告)号：US08263659B2
公开(公告)日：2012-09-11
申请号：US12469791
申请日：2009-05-21
申请人： Denis E. Ryono , Jon J. Hangeland , Todd J. Friends , Tamara Dejneka , Pratik Devasthale , Yolanda V. Caringal , Minsheng Zhang , Arthur M. P. Doweyko , Johan Malm , Andrei Sanin
发明人： Denis E. Ryono , Jon J. Hangeland , Todd J. Friends , Tamara Dejneka , Pratik Devasthale , Yolanda V. Caringal , Minsheng Zhang , Arthur M. P. Doweyko , Johan Malm , Andrei Sanin
IPC分类号： A61K31/19 , A61K31/165 , C07C321/00 , C07C229/00 , C07C59/00
CPC分类号： C07C311/46 , A61K31/4439 , A61K31/662 , A61K45/06 , C07C43/29 , C07C43/295 , C07C59/68 , C07C59/72 , C07C65/24 , C07C65/26 , C07C69/16 , C07C69/736 , C07C69/94 , C07C205/38 , C07C217/58 , C07C233/29 , C07C235/34 , C07C235/42 , C07C235/46 , C07C235/52 , C07C235/60 , C07C235/62 , C07C235/64 , C07C311/37 , C07C2601/02 , C07C2601/14 , C07C2602/08 , C07C2603/18 , C07D213/30 , C07D239/26 , C07D257/04 , C07D263/14 , C07D263/32 , C07D277/24 , C07D285/06 , C07D307/42 , C07D307/52 , C07D307/87 , C07D317/58 , C07D317/60 , C07D333/32 , C07F9/306 , C07F9/3241 , C07F9/4056 , A61K2300/00
摘要： A method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolism dysfunction or which are dependent upon the expression of a T3 regulated gene, wherein a compound as described in the general formula I below is administered in a therapeutically effective amount:
摘要翻译：提供了一种用于预防，抑制或治疗与代谢功能障碍相关或与T3调节基因的表达有关的疾病或病症的方法，其中以治疗有效量施用下述通式I中所述的化合物：

5. 发明申请

US20100298276A1 THYROID RECEPTOR LIGANDS 失效
公开(公告)号：US20100298276A1
公开(公告)日：2010-11-25
申请号：US12469791
申请日：2009-05-21
申请人： Denis E. Ryono , Jon J. Hangeland , Todd J. Friends , Tamara Dejneka , Pratik Devasthale , Yolanda V. Caringal , Minsheng Zhang , Arthur M.P. Doweyko , Johan Malm , Andrei Sanin
发明人： Denis E. Ryono , Jon J. Hangeland , Todd J. Friends , Tamara Dejneka , Pratik Devasthale , Yolanda V. Caringal , Minsheng Zhang , Arthur M.P. Doweyko , Johan Malm , Andrei Sanin
IPC分类号： A61K31/662 , C07F9/02 , A61P3/10
CPC分类号： C07C311/46 , A61K31/4439 , A61K31/662 , A61K45/06 , C07C43/29 , C07C43/295 , C07C59/68 , C07C59/72 , C07C65/24 , C07C65/26 , C07C69/16 , C07C69/736 , C07C69/94 , C07C205/38 , C07C217/58 , C07C233/29 , C07C235/34 , C07C235/42 , C07C235/46 , C07C235/52 , C07C235/60 , C07C235/62 , C07C235/64 , C07C311/37 , C07C2601/02 , C07C2601/14 , C07C2602/08 , C07C2603/18 , C07D213/30 , C07D239/26 , C07D257/04 , C07D263/14 , C07D263/32 , C07D277/24 , C07D285/06 , C07D307/42 , C07D307/52 , C07D307/87 , C07D317/58 , C07D317/60 , C07D333/32 , C07F9/306 , C07F9/3241 , C07F9/4056 , A61K2300/00
摘要： Thyroid receptor ligands are provided which have the general formula I wherein: R1 is 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, provided that at least one of R2 and R3 is other than hydrogen; R4 is R5 and R6 are the same or different and are selected from hydrogen, aryl, heteroaryl, alkyl, cycloalkyl, aralkyl or heteroaralkyl. R7 is aryl, heteroaryl, alkyl, aralkyl, or heteroaralkyl; R8 is aryl, heteroaryl, or cycloalkyl; R9 is R7 or hydrogen; R10 is hydrogen, halogen, cyano or alkyl; R11 and R12 are each independently selected from the group consisting of hydrogen, halogen, alkoxy, hydroxy (—OH) cyano, and alkyl; R13 is carboxylic acid (COOH) or esters thereof, phosphonic and phosphinic acid or esters thereof, sulfonic acid, tetrazole, hydroxamic acid, thiazolidinedione, acylsulfonamide, or other carboxylic acid surrogates known in the art; R14 and R15 may be the same or different and are selected from hydrogen and alkyl, or R14 and R15 may be joined together forming a chain of 2 to 5 methylene groups [—(CH2)m-, m=2, 3, 4 or 5], thus forming 3- to 6-membered cycloalkyl rings; R16 is hydrogen or alkyl of 1 to 4 carbons; R17 and R18 are the same or different and selected from hydrogen, halogen and alkyl; n is 0 or an integer from 1 to 4; X is oxygen (—O—), sulfur (—S—), sulfonyl (—SO2—), sulfenyl (—SO—) selenium (—Se—), carbonyl (—CO—), amino (—NH—) or methylene (—CH2-); wherein the substituents are as described herein. In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolism dysfunction or which are dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.

6. 发明授权

US07557143B2 Thyroid receptor ligands 失效
标题翻译：甲状腺受体配体
公开(公告)号：US07557143B2
公开(公告)日：2009-07-07
申请号：US10826100
申请日：2004-04-15
申请人： Denis E. Ryono , Jon J. Hangeland , Todd J. Friends , Tamara Dejneka , Pratik Devasthale , Yolanda V. Caringal , Minsheng Zhang , Arthur M. P. Doweyko , Johan Malm , Andrei Sanin
发明人： Denis E. Ryono , Jon J. Hangeland , Todd J. Friends , Tamara Dejneka , Pratik Devasthale , Yolanda V. Caringal , Minsheng Zhang , Arthur M. P. Doweyko , Johan Malm , Andrei Sanin
IPC分类号： A61K31/165 , A61K31/19 , C07C239/00 , C07C325/00 , C07C229/00 , C07C59/00
CPC分类号： C07C311/46 , A61K31/4439 , A61K31/662 , A61K45/06 , C07C43/29 , C07C43/295 , C07C59/68 , C07C59/72 , C07C65/24 , C07C65/26 , C07C69/16 , C07C69/736 , C07C69/94 , C07C205/38 , C07C217/58 , C07C233/29 , C07C235/34 , C07C235/42 , C07C235/46 , C07C235/52 , C07C235/60 , C07C235/62 , C07C235/64 , C07C311/37 , C07C2601/02 , C07C2601/14 , C07C2602/08 , C07C2603/18 , C07D213/30 , C07D239/26 , C07D257/04 , C07D263/14 , C07D263/32 , C07D277/24 , C07D285/06 , C07D307/42 , C07D307/52 , C07D307/87 , C07D317/58 , C07D317/60 , C07D333/32 , C07F9/306 , C07F9/3241 , C07F9/4056 , A61K2300/00
摘要： Thyroid receptor ligands are provided which have the general formula I wherein: R1 is 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, provided that at least one of R2 and R3 is other than hydrogen; R4 is R5 and R6 are the same or different and are selected from hydrogen, aryl, heteroaryl, alkyl, cycloalkyl, aralkyl or heteroaralkyl. R7 is aryl, heteroaryl, alkyl, aralkyl, or heteroaralkyl; R8 is aryl, heteroaryl, or cycloalkyl; R9 is R7 or hydrogen; R10 is hydrogen, halogen, cyano or alkyl; R11 and R12 are each independently selected from the group consisting of hydrogen, halogen, alkoxy, hydroxy (—OH) cyano, and alkyl; R13 is carboxylic acid (COOH) or esters thereof, phosphonic and phosphinic acid or esters thereof, sulfonic acid, tetrazole, hydroxamic acid, thiazolidinedione, acylsulfonamide, or other carboxylic acid surrogates known in the art; R14 and R15 may be the same or different and are selected from hydrogen and alkyl, or R14 and R15 may be joined together forming a chain of 2 to 5 methylene groups [—(CH2)m-, m=2, 3, 4 or 5], thus forming 3- to 6-membered cycloalkyl rings; R16 is hydrogen or alkyl of 1 to 4 carbons; R17 and R18 are the same or different and selected from hydrogen, halogen and alkyl; n is 0 or an integer from 1 to 4; X is oxygen (—O—), sulfur (—S—), sulfonyl (—SO2—), sulfenyl (—SO—) selenium (—Se—), carbonyl (—CO—), amino (—NH—) or methylene (—CH2-); wherein the substituents are as described herein. In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolism dysfunction or which are dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.
摘要翻译：提供具有通式I的甲状腺受体配体，其中：R 1是R 2和R 3相同或不同，是氢，卤素，1至4个碳的烷基或3至5个碳原子的环烷基，条件是R2中的至少一个并且R 3不是氢; R 4是R 5和R 6相同或不同，并且选自氢，芳基，杂芳基，烷基，环烷基，芳烷基或杂芳烷基。 R7是芳基，杂芳基，烷基，芳烷基或杂芳烷基; R8是芳基，杂芳基或环烷基; R9为R7或氢; R 10是氢，卤素，氰基或烷基; R 11和R 12各自独立地选自氢，卤素，烷氧基，羟基（-OH）氰基和烷基; R13是羧酸（COOH）或其酯，膦酸和次膦酸或其酯，磺酸，四唑，异羟肟酸，噻唑烷二酮，酰基磺酰胺或本领域已知的其它羧酸替代物; R 14和R 15可以相同或不同，并且选自氢和烷基，或者R 14和R 15可以连接在一起形成2至5个亚甲基 - [ - （CH 2）m - ，m = 2,3,4或 5]，从而形成3-至6-元环烷基环; R16是氢或1至4个碳的烷基; R 17和R 18相同或不同，选自氢，卤素和烷基; n为0或1至4的整数; X是氧（-O-），硫（-S-），磺酰基（-SO 2 - ），亚磺酰基（-SO-），硒（-Se-），羰基（-CO-），氨基（-NH-）或亚甲基（-CH2-）; 其中取代基如本文所述。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或依赖于T3调节基因的表达的疾病或病症的方法，其中如上所述的化合物以治疗有效量施用。

7. 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。

8. 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。

9. 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。

10. 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。

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