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1.发明授权STABLE ORAL PHARMACEUTICAL COMPOSITION CONTAINING THYROID HORMONE RECEPTOR AGONISTS 有权与THYROIDHORMONREZEPTORAGONISTEN稳定的口服药物组合物
公开(公告)号：EP2004168B1
公开(公告)日：2011-08-03
申请号：EP07723634.7
申请日：2007-03-27
发明人： GARG, Neeraj , RAO, VENKATRAMANA M. , GANDHI, Rajesh, B. , WASHBURN, William N. , KOEHLER, Konrad , MALM, Johan
IPC分类号： A61K31/185 , A61K31/215 , A61K45/06 , A61K9/28 , A61P5/16
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.
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2.发明公开STABLE ORAL PHARMACEUTICAL COMPOSITION CONTAINING THYROID HORMONE RECEPTOR AGONISTS 有权与THYROIDHORMONREZEPTORAGONISTEN稳定的口服药物组合物
公开(公告)号：EP2004168A1
公开(公告)日：2008-12-24
申请号：EP07723634.7
申请日：2007-03-27
发明人： GARG, Neeraj , RAO, VENKATRAMANA M. , GANDHI, Rajesh, B. , WASHBURN, William N. , KOEHLER, Konrad , MALM, Johan
IPC分类号： A61K31/185 , A61K31/215 , A61K45/06 , A61K9/28 , A61P5/16
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.
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公开(公告)号：EP1144370A2
公开(公告)日：2001-10-17
申请号：EP99962486.9
申请日：1999-12-23
发明人： HANGELAND, Jon , ZHANG, Minsheng , CARINGAL, Yolanda , RYONO, Denis , LI, Yi-Lin , MALM, Johan , LIU, Ye , GARG, Neeraj , LITTEN, Chris , GARCIA COLLAZO, Ana Maria , KOEHLER, Konrad
IPC分类号： C07C311/00
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.
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公开(公告)号：EP1601641A2
公开(公告)日：2005-12-07
申请号：EP04704944.0
申请日：2004-01-23
发明人： WASHBURN, William, N. , MENG, Wei , RYONO, Denis, E. , ELLSWORTH, Bruce, A. , ERICSSON, Thomas , RAHIMI- GHADIM, Mahmoud , GARG, Neeraj , MALM, Johan
IPC分类号： C07C229/08 , C07C229/22 , A61K31/24 , A61K31/195
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.
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公开(公告)号：EP1492756A1
公开(公告)日：2005-01-05
申请号：EP03745755.3
申请日：2003-02-10
申请人： KARO BIO AB
IPC分类号： C07C59/215 , C07D261/06 , C07D213/04 , C07D209/04 , C07D271/06 , C07D251/12 , C07D413/02 , C07D263/30 , A61K31/085 , A61K31/33 , A61K51/00 , A61P5/14 , A61P9/06 , A61P17/00
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.
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公开(公告)号：EP1408958A1
公开(公告)日：2004-04-21
申请号：EP02764700.7
申请日：2002-07-15
申请人： KARO BIO AB
发明人： BRANDTS, Bodo , CARLSSON, Bo , MALM, Johan
IPC分类号： A61K31/343 , A61P9/06 , C07D307/80
CPC分类号： A61K31/343 , C07D307/80
摘要： This invention relates to new compounds and their pharmaceutical use, and to the pharmaceutical use of known compounds, which compounds inhibit certain transmembrane potassium currents in the atrium of the heart of a mammal without significantly affecting other ion channels, for the treatment of heart disease particularly atrial fibrillation. The invention also relates to pharmaceutical compositions comprising such compounds.
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7.发明公开
公开(公告)号：EP1358175A2
公开(公告)日：2003-11-05
申请号：EP02703589.8
申请日：2002-01-30
申请人： KARO BIO AB
发明人： MALM, Johan , FLÖISTRUP, Erik , GRIVAS, Spiros , LI, Yi-Lin
IPC分类号： C07D307/79 , C07D235/06 , A61K31/4184 , A61K31/343 , A61P5/14 , A61P17/00 , A61P9/06
CPC分类号： C07D235/06 , C07D307/79
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 and metabolic disorders, such as cardiac arrhythmias, thyrotoxicosis, subcllinical hyperthyrodism and liver diseases.
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公开(公告)号：EP1000008A1
公开(公告)日：2000-05-17
申请号：EP98935008.7
申请日：1998-06-26
申请人： KARO BIO AB
发明人： LI, Yi-Lin , LIU, Ye , HEDFORS, Asa , MALM, Johan , MELLIN, Charlotta , ZHANG, Minsheng
IPC分类号： C07C59/68 , A61K31/19 , C07C65/24 , C07C43/295 , C07C255/37 , A61K31/085 , A61K31/275 , A61K31/66
CPC分类号： C07F9/3882 , C07C43/295 , C07C59/68 , C07C65/24 , C07C255/37 , C07F9/4056
摘要： Novel thyroid receptor ligands as provided which have general formula (I) in which: 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 acceptable 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.
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9.发明公开PRIME RING SUBSTITUTED THYROID RECEPTOR ANTAGONISTS FOR THE TREATMENT OF CARDIAC AND METABOLIC DISORDERS 审中-公开在取代的THYROIDREZEPTORANTAGONISTEN心血管和代谢疾病的治疗主环
公开(公告)号：EP1499578A2
公开(公告)日：2005-01-26
申请号：EP02767384.7
申请日：2002-08-13
申请人： KARO BIO AB
发明人： MALM, Johan , BRANDT, Peter , EDVINSSON, Karin , KOEHLER, Konrad , SANIN, Andrei , GORDON, Sandra
IPC分类号： C07C59/68 , C07C65/24 , C07D213/04 , C07D241/10 , C07D277/20 , A61K31/192 , A61K31/435 , A61K31/4965 , A61K31/426 , A61K51/00 , A61P3/00 , A61P5/14 , A61P9/00
CPC分类号： C07D213/30 , A61K31/192 , A61K31/425 , A61K31/44 , A61K31/603 , C07C59/68 , C07C65/26 , C07D241/12
摘要： This invention relates to novel compounds according to the general formula (I) or a pharmaceutically acceptable salt thereof, which are thyroid receptor ligands, preferably antagonists and to methods for using such compounds in the treatment of cardiac and metabolic disorders, such as cardiac arrhythmias, thyrotoxicosis, subclinical hyperthyroidism and liver diseases.
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10.发明公开THYROID HORMONE RECEPTOR ANTAGONISTS FOR CARDIAC & METABOLIC DISORDERS II 审中-公开甲状腺激素受体拮抗剂心脏疾病和代谢疾病的治疗
公开(公告)号：EP1387825A1
公开(公告)日：2004-02-11
申请号：EP02735262.4
申请日：2002-04-15
申请人： KARO BIO AB
IPC分类号： C07C229/36 , C07C57/52 , C07C59/48 , C07D213/30 , C07D261/08 , C07D333/16 , A61K31/19 , A61K31/198 , A61K31/44 , A61K31/42 , A61K31/381 , A61P9/06
CPC分类号： C07D213/30 , C07C59/68 , C07C229/36 , C07D261/08 , C07D277/24
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 and metabolic disorders, such as cardiac arrhythmias, thyrotoxicosis, subclinical hyperthyrodism and liver diseases.
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