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

发明人： RAHIMI-GHADIM, Mahmoud ,  GARG, Neeraj ,  MALM, Johan

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.

公开(公告)号：EP1537073A2

公开(公告)日：2005-06-08

申请号：EP03763744.4

申请日：2003-07-08

申请人： KARO BIO AB ,  BRISTOL-MYERS SQUIBB COMPANY

发明人： GARG, Neeraj ,  GADIM, Mahmoud, Rahimi ,  ERICSSON, Thomas, Anders, Wilson ,  MALM, Lars, Johan ,  RYONO, Denis, Evan

IPC分类号： C07C235/52 ,  C07C235/34 ,  A61K31/195 ,  A61P5/16

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.

公开(公告)号：EP2004593B1

公开(公告)日：2012-03-21

申请号：EP07723633.9

申请日：2007-03-27

申请人： KARO BIO AB ,  Bristol-Myers Squibb Company

发明人： CHIDAMBARAM, Ramakrishnan ,  GARG, Neeraj ,  RASMUSON, Ake ,  GRACIN, Sandra

IPC分类号： C07C233/25 ,  A61K31/167 ,  A61P3/04

CPC分类号： C07C233/25 ,  C07B2200/13

摘要： The invention relates to novel crystalline forms of 3-[ [3, 5-dibromo-4-[4-hydroxy-3-(1-methylethyl)-phenoxy] -phenyl]-amino]-3-oxopropanoic acid, said crystalline forms being characterised by a powder X-ray diffraction pattern having major peaks at either 2ϑ = 16.1±0.2, 20.1±0.2, 20.7±0.2, and 24.2+0.2; or 2ϑ = 9.0±0.2, 14.7±0.2, 19.6±0.2, 21.6±0.2, and 24.3+0.2.

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

申请人： Bristol-Myers Squibb Company ,  KARO BIO AB

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.

公开(公告)号：EP1296936A1

公开(公告)日：2003-04-02

申请号：EP01951600.4

申请日：2001-06-15

申请人： KARO BIO AB

发明人： YI-LIN, Li ,  MALM, Johan ,  LITTEN, Chris ,  GARCIA COLLAZO, Ana, Maria ,  GARG, Neeraj

IPC分类号： C07C233/25 ,  C07C233/27 ,  C07D209/34 ,  C07C235/34 ,  C07C233/75 ,  C07D235/26 ,  A61K31/195 ,  A61K31/40 ,  A61K31/41

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： 本发明涉及是甲状腺受体配体，并且优选是选择性的甲状腺激素受体β，制备测试化合物的方法以及使用检测化合物的方法式（I）的化合物：如在代谢的调控。

公开(公告)号：EP2739609A1

公开(公告)日：2014-06-11

申请号：EP12745463.5

申请日：2012-08-02

申请人： KARO BIO AB

发明人： CHENG, Aiping ,  GARG, Neeraj ,  KRÜGER, Lars ,  LÖFSTEDT, Joakim ,  KOCH, Eva ,  KOEHLER, Konrad ,  HAGBERG, Lars ,  NÖTEBERG, Daniel

IPC分类号： C07D213/58 ,  C07D215/12 ,  C07D217/14 ,  C07D231/12 ,  C07D233/64 ,  C07D235/16 ,  C07D261/08 ,  C07D277/30 ,  C07D277/34 ,  C07D307/54 ,  C07D307/68 ,  C07D307/87 ,  C07D317/60 ,  C07D333/20 ,  C07D409/10

CPC分类号： A61K31/472 ,  A61K31/155 ,  A61K31/165 ,  A61K31/277 ,  A61K31/341 ,  A61K31/343 ,  A61K31/365 ,  A61K31/381 ,  A61K31/402 ,  A61K31/404 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/47 ,  C07C209/68 ,  C07C251/48 ,  C07D207/327 ,  C07D213/58 ,  C07D215/12 ,  C07D215/14 ,  C07D217/14 ,  C07D217/16 ,  C07D231/12 ,  C07D233/64 ,  C07D235/16 ,  C07D261/08 ,  C07D277/30 ,  C07D277/34 ,  C07D295/155 ,  C07D307/54 ,  C07D307/68 ,  C07D307/87 ,  C07D317/60 ,  C07D333/20 ,  C07D333/24 ,  C07D409/10 ,  C07D413/10 ,  C07C211/65

摘要： Compounds of formula (I) or a pharmaceutically acceptable ester, amide, carbamate or salt thereof, including a salt of such an ester, amide or carbamate in which R1 to R9 have meanings as defined in the Specification, are useful as estrogen receptor ligands.

摘要翻译： 式（I）化合物或其药学上可接受的酯，酰胺，氨基甲酸酯或其盐，包括其中R 1至R 9具有如本说明书中所定义的含义的酯，酰胺或氨基甲酸酯的盐，可用作雌激素受体配体。

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

申请人： KARO BIO AB ,  Bristol-Myers Squibb Company

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.

公开(公告)号：EP2004593A1

公开(公告)日：2008-12-24

申请号：EP07723633.9

申请日：2007-03-27

申请人： KARO BIO AB ,  Bristol-Myers Squibb Company

发明人： CHIDAMBARAM, Ramakrishnan ,  GARG, Neeraj ,  RASMUSON, Ake ,  GRACIN, Sandra

IPC分类号： C07C233/25 ,  A61K31/167 ,  A61P3/04

CPC分类号： C07C233/25 ,  C07B2200/13

摘要： The invention relates to novel crystalline forms of 3-[ [3, 5-dibromo-4-[4-hydroxy-3-(1-methylethyl)-phenoxy] -phenyl]-amino]-3-oxopropanoic acid, said crystalline forms being characterised by a powder X-ray diffraction pattern having major peaks at either 2ϑ = 16.1±0.2, 20.1±0.2, 20.7±0.2, and 24.2+0.2; or 2ϑ = 9.0±0.2, 14.7±0.2, 19.6±0.2, 21.6±0.2, and 24.3+0.2.

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

申请人： KARO BIO AB ,  Bristol-Myers Squibb Company

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.

公开(公告)号：EP1537073B1

公开(公告)日：2007-09-12

申请号：EP03763744.4

申请日：2003-07-08

申请人： KARO BIO AB ,  Bristol-Myers Squibb Company

发明人： GARG, Neeraj ,  GADIM, Mahmoud, Rahimi ,  NORIN, Thomas, Anders, Wilson ,  MALM, Lars, Johan ,  RYONO, Denis, Evan

IPC分类号： C07C235/52 ,  C07C235/34 ,  A61K31/195 ,  A61P5/16

CPC分类号： C07C235/52 ,  C07C235/34