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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. 发明申请

US20060135614A1 Novel compounds 失效
标题翻译：新型化合物
公开(公告)号：US20060135614A1
公开(公告)日：2006-06-22
申请号：US10520902
申请日：2003-07-08
申请人： Neeraj Garg , Mahmoud Ghadim , Thomas Ericsson , Lars Malm , Denis Ryono
发明人： Neeraj Garg , Mahmoud Ghadim , Thomas Ericsson , Lars Malm , Denis Ryono
IPC分类号： A61K31/198 , C07C237/28
CPC分类号： C07C235/52 , C07C235/34
摘要： This invention relates to novel compounds, which are thyroid receptor ligands, and to methods of preparing such compounds. 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 herein is administered in a therapeutically effective amount.
摘要翻译：本发明涉及作为甲状腺受体配体的新化合物及其制备方法。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与T3调节基因的表达相关的疾病或病症的方法，其中本文所述的化合物以治疗有效量施用。

3. 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。

4. 发明申请

US20050004184A1 Thyroid receptor ligands 失效
标题翻译：甲状腺受体配体
公开(公告)号：US20050004184A1
公开(公告)日：2005-01-06
申请号：US10826100
申请日：2004-04-15
申请人： Denis Ryono , Jon Hangeland , Todd Friends , Tamara Dejneka , Pratik Devasthale , Yolanda Caringal , Minsheng Zhang , Arthur Doweyko , Johan Malm , Andrei Sanin
发明人： Denis Ryono , Jon Hangeland , Todd Friends , Tamara Dejneka , Pratik Devasthale , Yolanda Caringal , Minsheng Zhang , Arthur Doweyko , Johan Malm , Andrei Sanin
IPC分类号： A61K20060101 , A61K31/16 , A61K31/165 , A61K31/19 , A61K31/277 , A61K31/421 , A61K31/44 , A61K47/00 , C07C205/00 , C07C235/20 , C07C255/49 , C07C381/00
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（-CH 2 - ）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。

5. 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。

6. 发明申请

US20050032890A1 Aniline-derived ligands for the thyroid receptor 有权
标题翻译：苯胺衍生的甲状腺受体配体
公开(公告)号：US20050032890A1
公开(公告)日：2005-02-10
申请号：US10930360
申请日：2004-08-30
申请人： Todd Friends , Denis Ryono , Minsheng Zhang
发明人： Todd Friends , Denis Ryono , Minsheng Zhang
IPC分类号： A61K45/00 , A61K31/155 , A61K31/167 , A61K31/192 , A61K31/22 , A61K31/351 , A61K31/40 , A61K31/404 , A61K31/425 , A61K31/4418 , A61K31/59 , A61K31/64 , A61K38/26 , A61K38/28 , A61K45/06 , A61P3/00 , A61P3/04 , A61P3/06 , A61P5/14 , A61P9/04 , A61P9/06 , A61P9/10 , A61P17/00 , A61P17/02 , A61P17/06 , A61P17/10 , A61P17/16 , A61P19/10 , A61P25/24 , A61P27/06 , A61P35/00 , A61P43/00 , C07C233/25 , C07C233/27 , C07C235/74 , C07C235/76 , A61K31/195 , A61K31/24
CPC分类号： C07C233/27 , A61K31/167 , A61K45/06 , C07C233/25 , A61K2300/00
摘要： New thyroid receptor ligands are provided which have the general formula in which: X is —O—, —S—, —CH2—, —CO—, or —NH—; Y is —(CH2)n— where n is an integer from 1 to 5, or cis- or trans-ethylene; 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 6 carbons, at least one of R2 and R3 being other than hydrogen; R4 is hydrogen or lower alkyl; R5 is hydrogen or lower alkyl; R6 is carboxylic acid, or esters or prodrugs; R7 is hydrogen or an alkanoyl or an aroyl. 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：提供了新的甲状腺受体配体，其具有以下通式：其中：X是-O - ， - S - ， - CH 2 - ， - CO-或-NH-; Y是 - （CH 2）n - ，其中n是1至5的整数，或顺式或反式 - 亚乙基; R1是卤素，三氟甲基或1-6个碳的烷基或3-7个碳的环烷基; R2和R3相同或不同，为氢，卤素，1至4个碳的烷基或3至6个碳的环烷基，R2和R3中的至少一个不是氢; R4是氢或低级烷基; R5是氢或低级烷基; R6是羧酸，或酯或前药; R7是氢或烷酰基或芳酰基。此外，提供了用于预防，抑制或治疗与代谢功能障碍相关的疾病或依赖于T3调节基因的表达的方法，其中以治疗有效量施用如上所述的化合物。与代谢功能障碍相关或依赖于T3调节基因的表达的这些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，甲状腺功能减退，甲状腺癌以及青光眼，充血性心力衰竭和皮肤病。

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