Title:
NOVEL COMPOUNDS AND THEIR USES AS THYROID HORMONE RECEPTOR AGONISTS
Document Type and Number:
WIPO Patent Application WO/2020/169069
Kind Code:
A1
Abstract:
A compound of formula (I) or (Ia), or a tautomer or a pharmaceutically acceptable salt thereof is provided. Compounds of formula (II) to (V), or a tautomer or a pharmaceutically acceptable salt thereof are also provided. These compounds and the pharmaceutical compositions containing them are useful for the treatment of diseases such as obesity, hyperlipidemia, hypercholesterolemia and diabetes and other related disorders and diseases, and may be useful for other diseases such as NASH, atherosclerosis, cardiovascular diseases, hypothyroidism, thyroid cancer and other disorders and diseases related thereto． (I), (Ia)
More Like This:
Inventors:
ZHANG JUNBO (CN)
QI XIAOXIN (CN)
QI XIAOXIN (CN)
Application Number:
PCT/CN2020/076038
Publication Date:
August 27, 2020
Filing Date:
February 20, 2020
Export Citation:
Assignee:
NANJING RUIJIE PHARMA CO LTD (CN)
International Classes:
C07D253/075; A61K31/53; A61P5/16; C07D403/10
Domestic Patent References:
| WO2020010068A1 | 2020-01-09 | |||
| WO2019242766A1 | 2019-12-26 | |||
| WO2019144835A1 | 2019-08-01 | |||
| WO2019240938A1 | 2019-12-19 | |||
| WO2018075650A1 | 2018-04-26 | |||
| WO2008046657A1 | 2008-04-24 | |||
| WO2009037172A1 | 2009-03-26 | |||
| WO2007009913A1 | 2007-01-25 | |||
| WO2014043706A1 | 2014-03-20 | |||
| WO2005086661A2 | 2005-09-22 | |||
| WO2007003419A1 | 2007-01-11 | |||
| WO2008030618A1 | 2008-03-13 | |||
| WO2007128492A1 | 2007-11-15 | |||
| WO2007134864A1 | 2007-11-29 | |||
| WO2002030863A2 | 2002-04-18 | |||
| WO2001060784A1 | 2001-08-23 | |||
| WO2007009913A1 | 2007-01-25 | |||
| WO2009037172A1 | 2009-03-26 | |||
| WO2010122980A1 | 2010-10-28 | |||
| WO2020010068A1 | 2020-01-09 | |||
| WO2019242766A1 | 2019-12-26 | |||
| WO2019144835A1 | 2019-08-01 | |||
| WO2019240938A1 | 2019-12-19 | |||
| WO2018075650A1 | 2018-04-26 | |||
| WO2008046657A1 | 2008-04-24 | |||
| WO2009037172A1 | 2009-03-26 | |||
| WO2007009913A1 | 2007-01-25 | |||
| WO2007003419A1 | 2007-01-11 | |||
| WO2014043706A1 | 2014-03-20 | |||
| WO2005086661A2 | 2005-09-22 | |||
| WO2008030618A1 | 2008-03-13 | |||
| WO2007128492A1 | 2007-11-15 | |||
| WO2007134864A1 | 2007-11-29 | |||
| WO2002030863A2 | 2002-04-18 |
Foreign References:
| JPH03261783A | 1991-11-21 | |||
| US5141938A | 1992-08-25 | |||
| JP2012106996A | 2012-06-07 | |||
| US20120129812A1 | 2012-05-24 | |||
| US6787652B1 | 2004-09-07 | |||
| US5141938A | 1992-08-25 | |||
| JP2012010699A | 2012-01-19 | |||
| US20120129812A1 | 2012-05-24 | |||
| US6787652B1 | 2004-09-07 |
Other References:
DANZI S , KLEIN I : "Cardiac specific effects of thyroid hormone analogues", HORMONE AND METABOLIC RESEARCH, vol. 43, no. 11, 31 December 2011 (2011-12-31), pages 737 - 742, XP009524228, ISSN: 0018-5043, DOI: 10.1055/s-0031-1291177
CHEMICAL ABSTRACTS, 15 July 2001, Columbus, Ohio, US; CHEMICAL ABSTRACTS SERVICE，COLUMBUS，OHIO: "345935-02-6: 1，2，4-Triazine-6-carbonitrile， 2，3，4，5-tetrahydro-3，5-dioxo-2-[4-(2-thienylcarbonyl)phenyl]-"
MILLER，M. W. ET AL.: "Anticoccidial derivatives of 6-azauracil. 3. Synthesis，high activity，and short plasma half-life of 1-phenyl-6-azauracils containing sulfonamide substituents", JOURNAL OF MEDICINAL CHEMISTRY, vol. 23, no. 10, 1 October 1980 (1980-10-01), XP055170315, ISSN: 0022-2623
WIEDERMANNOVA，I. ET AL.: "The synthesis of some polycyclic N-H acids with quinoxaline and [1，2，4]triazines", ARKIVOC, no. 15, 31 December 2003 (2003-12-31), XP055533780, ISSN: 1551-7012, DOI: 20200430162441X
WIEDERMANNOVA，I. ET AL.: "Synthesis of some isomeric quinoxaline derivatives with 6-azauracil cycle", JOURNAL OF HETEROCYCLIC CHEMISTRY, vol. 38, no. 6, 31 December 2001 (2001-12-31), XP055065586, ISSN: 0022-152X, DOI: 20200430162653X
SLOUKA，J.: "5-Substituted 6-azauracils. Part 7: Synthesis of some derivatives of 5-[4-(6-azauracil-1-yl)benzyl] -6-azauracil", PHARMAZIE, vol. 35, no. 12, 31 December 1980 (1980-12-31), DE, pages 744 - 745, XP009530659, ISSN: 0031-7144
ABEL, J. CLIN. INVEST., vol. 104, 1999, pages 291 - 300
DANZI ET AL., HORMONE AND METABOLIC RESEARCH, vol. 43, no. 11
MILLER ET AL., JOURNAL OF MEDICINAL CHEMISTRY, vol. 23, no. 10
WIEDERMANNOVA ET AL., ARKIVOC, no. 15
SLOUKA, PHARMAZIE, DE, vol. 35, no. 12, pages 744 - 745
"Handbook of Chemistry and Physics", article "Periodic Table of the Elements, CAS version"
"Thomas Sorrell", 1999, UNIVERSITY SCIENCE BOOKS, article "Organic Chemistry"
SMITH, M. B.MARCH, J.: "March's Advanced Organic Chemistry", 2001, JOHN WILEY &SONS
H. ANSEL: "Pharmaceutical Dosage Forms and Drug Delivery Systems", 1995, pages: 196,1456 - 1457
See also references of EP 3927693A4
CHEMICAL ABSTRACTS, 15 July 2001, Columbus, Ohio, US; CHEMICAL ABSTRACTS SERVICE，COLUMBUS，OHIO: "345935-02-6: 1，2，4-Triazine-6-carbonitrile， 2，3，4，5-tetrahydro-3，5-dioxo-2-[4-(2-thienylcarbonyl)phenyl]-"
MILLER，M. W. ET AL.: "Anticoccidial derivatives of 6-azauracil. 3. Synthesis，high activity，and short plasma half-life of 1-phenyl-6-azauracils containing sulfonamide substituents", JOURNAL OF MEDICINAL CHEMISTRY, vol. 23, no. 10, 1 October 1980 (1980-10-01), XP055170315, ISSN: 0022-2623
WIEDERMANNOVA，I. ET AL.: "The synthesis of some polycyclic N-H acids with quinoxaline and [1，2，4]triazines", ARKIVOC, no. 15, 31 December 2003 (2003-12-31), XP055533780, ISSN: 1551-7012, DOI: 20200430162441X
WIEDERMANNOVA，I. ET AL.: "Synthesis of some isomeric quinoxaline derivatives with 6-azauracil cycle", JOURNAL OF HETEROCYCLIC CHEMISTRY, vol. 38, no. 6, 31 December 2001 (2001-12-31), XP055065586, ISSN: 0022-152X, DOI: 20200430162653X
SLOUKA，J.: "5-Substituted 6-azauracils. Part 7: Synthesis of some derivatives of 5-[4-(6-azauracil-1-yl)benzyl] -6-azauracil", PHARMAZIE, vol. 35, no. 12, 31 December 1980 (1980-12-31), DE, pages 744 - 745, XP009530659, ISSN: 0031-7144
ABEL, J. CLIN. INVEST., vol. 104, 1999, pages 291 - 300
DANZI ET AL., HORMONE AND METABOLIC RESEARCH, vol. 43, no. 11
MILLER ET AL., JOURNAL OF MEDICINAL CHEMISTRY, vol. 23, no. 10
WIEDERMANNOVA ET AL., ARKIVOC, no. 15
SLOUKA, PHARMAZIE, DE, vol. 35, no. 12, pages 744 - 745
"Handbook of Chemistry and Physics", article "Periodic Table of the Elements, CAS version"
"Thomas Sorrell", 1999, UNIVERSITY SCIENCE BOOKS, article "Organic Chemistry"
SMITH, M. B.MARCH, J.: "March's Advanced Organic Chemistry", 2001, JOHN WILEY &SONS
H. ANSEL: "Pharmaceutical Dosage Forms and Drug Delivery Systems", 1995, pages: 196,1456 - 1457
See also references of EP 3927693A4
Attorney, Agent or Firm:
NANJING CIPIC INTELLECTUAL PROPERTY FIRM (GENERAL PARTNERSHIP) (CN)
Download PDF:
Previous Patent: DATA TRANSMISSION METHOD AND APPARATUS, AND COMPUTER STORAGE MEDIUM
Next Patent: DEVICE FOR ARRANGEMENT OF DRINKS
Next Patent: DEVICE FOR ARRANGEMENT OF DRINKS