CA2488535C - Glucocorticoid receptor ligands for the treatment of metabolic disorders - Google Patents

Glucocorticoid receptor ligands for the treatment of metabolic disorders Download PDF

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Publication number
CA2488535C
CA2488535C CA2488535A CA2488535A CA2488535C CA 2488535 C CA2488535 C CA 2488535C CA 2488535 A CA2488535 A CA 2488535A CA 2488535 A CA2488535 A CA 2488535A CA 2488535 C CA2488535 C CA 2488535C
Authority
CA
Canada
Prior art keywords
beta
alpha
compound
hydroxy
group
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
CA2488535A
Other languages
English (en)
French (fr)
Other versions
CA2488535A1 (en
Inventor
Thomas W. Von Geldern
James T. Link
Noah Tu
Philip R. Kym
Chunqiu Lai
Steven J. Richards
Peer B. Jacobson
Richard D. Bishop
Bradley D. Gates
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Karo Healthcare AB
Original Assignee
Karo Bio AB
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from US10/460,491 external-priority patent/US7141559B2/en
Application filed by Karo Bio AB filed Critical Karo Bio AB
Publication of CA2488535A1 publication Critical patent/CA2488535A1/en
Application granted granted Critical
Publication of CA2488535C publication Critical patent/CA2488535C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0077—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom
    • C07J41/0083—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom substituted in position 11-beta by an optionally substituted phenyl group not further condensed with other rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/44—Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/46—Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of glucocorticosteroids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0055—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives
    • C07J41/0061—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives one of the carbon atoms being part of an amide group

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Diabetes (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CA2488535A 2002-06-19 2003-06-17 Glucocorticoid receptor ligands for the treatment of metabolic disorders Expired - Fee Related CA2488535C (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US17475002A 2002-06-19 2002-06-19
US10/174,750 2002-06-19
US10/460,491 2003-06-12
US10/460,491 US7141559B2 (en) 2002-06-19 2003-06-12 Glucocorticoid receptor ligands for the treatment of metabolic disorders
PCT/US2003/019157 WO2004000869A1 (en) 2002-06-19 2003-06-17 Glucocorticoid receptor ligands for the treatment of metabolic disorders

Publications (2)

Publication Number Publication Date
CA2488535A1 CA2488535A1 (en) 2003-12-31
CA2488535C true CA2488535C (en) 2012-02-07

Family

ID=30002639

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2488535A Expired - Fee Related CA2488535C (en) 2002-06-19 2003-06-17 Glucocorticoid receptor ligands for the treatment of metabolic disorders

Country Status (16)

Country Link
EP (1) EP1551860B1 (enExample)
JP (1) JP4611019B2 (enExample)
KR (1) KR101100826B1 (enExample)
CN (1) CN100348609C (enExample)
AR (1) AR040278A1 (enExample)
AT (1) ATE346082T1 (enExample)
AU (1) AU2003243622B9 (enExample)
CA (1) CA2488535C (enExample)
CY (1) CY1105982T1 (enExample)
DE (1) DE60309909T2 (enExample)
DK (1) DK1551860T3 (enExample)
ES (1) ES2278195T3 (enExample)
PT (1) PT1551860E (enExample)
TW (1) TWI285646B (enExample)
UY (1) UY27862A1 (enExample)
WO (1) WO2004000869A1 (enExample)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7253283B2 (en) 2004-01-16 2007-08-07 Bristol-Myers Squibb Company Tricyclic modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
US7605264B2 (en) 2004-01-16 2009-10-20 Bristol-Myers Squibb Company Heterocyclic modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
US7569689B2 (en) 2004-01-16 2009-08-04 Bristol-Myers Squibb Company Modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
US7326728B2 (en) 2004-01-16 2008-02-05 Bristol-Myers Squibb Company Modulators of glucocorticoid receptor, AP-1, and/or NF-κβ activity and use thereof
US7273881B2 (en) 2004-01-16 2007-09-25 Bristol-Myers Squibb Company Modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
US7625921B2 (en) 2004-01-16 2009-12-01 Bristol-Myers Squibb Company Modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
US7317024B2 (en) 2005-01-13 2008-01-08 Bristol-Myers Squibb Co. Heterocyclic modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
US7642273B2 (en) 2005-01-13 2010-01-05 Bristol-Myers Squibb Company Modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
US7361654B2 (en) 2005-01-13 2008-04-22 Bristol-Myers Squibb Co. Substituted heteroaryl amide modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
US7411071B2 (en) 2005-01-13 2008-08-12 Bristol-Myers Squibb Company Modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
GB0514302D0 (en) * 2005-07-12 2005-08-17 Karobio Ab Improved crystalline material
EP2348857B1 (en) 2008-10-22 2016-02-24 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
AU2009309037A1 (en) 2008-10-31 2010-05-06 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
CN102812011A (zh) 2009-11-16 2012-12-05 梅利科技公司 [1,5]-二氮杂环辛间四烯衍生物
US8895596B2 (en) 2010-02-25 2014-11-25 Merck Sharp & Dohme Corp Cyclic benzimidazole derivatives useful as anti-diabetic agents
MY159058A (en) 2011-02-25 2016-12-15 Merck Sharp & Dohme Novel cyclic azabenzimidazole derivatives useful as anti-diabetic agent
CN103957919B (zh) * 2011-09-19 2018-10-16 瑞士苏黎世联邦理工学院 RORγ调节剂
EP2880028B1 (en) 2012-08-02 2020-09-30 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
JP2016516004A (ja) 2013-02-22 2016-06-02 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． 抗糖尿病二環式化合物
WO2014139388A1 (en) 2013-03-14 2014-09-18 Merck Sharp & Dohme Corp. Novel indole derivatives useful as anti-diabetic agents
EP2781217A1 (en) * 2013-03-18 2014-09-24 ETH Zurich ROR gamma modulators
WO2015051496A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
CN105693808B (zh) * 2015-11-05 2018-03-16 华润紫竹药业有限公司 一种醋酸乌立妥原料药杂质及其制备方法和作为标准品的用途
FR3055627A1 (fr) * 2016-09-08 2018-03-09 Laboratoire Hra-Pharma Methode de preparation du compose cdb-3877
FR3055626B1 (fr) * 2016-09-08 2018-10-12 Hra Pharma Lab Procede de synthese d'un compose steroide comprenant un substituant n-methylaniline en position 11
US11072602B2 (en) 2016-12-06 2021-07-27 Merck Sharp & Dohme Corp. Antidiabetic heterocyclic compounds
US10968232B2 (en) 2016-12-20 2021-04-06 Merck Sharp & Dohme Corp. Antidiabetic spirochroman compounds
CN114230627B (zh) * 2021-12-31 2023-09-15 湖南新合新生物医药有限公司 一种倍他米松环氧水解物中间体的制备方法

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3930696A1 (de) * 1989-09-14 1991-03-28 Hoechst Ag Gallensaeurederivate, verfahren zu ihrer herstellung, verwendung als arzneimittel
DE4000397A1 (de) * 1990-01-09 1991-07-11 Hoechst Ag Lipidselektive antioxidantien sowie deren herstellung und verwendung
NZ240846A (en) * 1990-12-06 1994-04-27 Hoechst Ag Dimeric bile acid derivatives; preparatory processes and pharmaceutical compositions
GB9907048D0 (en) * 1999-03-27 1999-05-19 Karobio Ab Novel glucocorticoid receptor ligands for the treatment of meta bolic disorders

Also Published As

Publication number Publication date
WO2004000869A1 (en) 2003-12-31
CN1662549A (zh) 2005-08-31
AU2003243622A2 (en) 2004-01-06
EP1551860A1 (en) 2005-07-13
UY27862A1 (es) 2004-04-30
AU2003243622B9 (en) 2009-07-16
EP1551860B1 (en) 2006-11-22
ATE346082T1 (de) 2006-12-15
AU2003243622A1 (en) 2004-01-06
DK1551860T3 (da) 2007-04-02
DE60309909D1 (de) 2007-01-04
AU2003243622B2 (en) 2009-05-28
TW200410983A (en) 2004-07-01
JP4611019B2 (ja) 2011-01-12
JP2005533807A (ja) 2005-11-10
TWI285646B (en) 2007-08-21
AR040278A1 (es) 2005-03-23
ES2278195T3 (es) 2007-08-01
CN100348609C (zh) 2007-11-14
CA2488535A1 (en) 2003-12-31
DE60309909T2 (de) 2007-06-21
PT1551860E (pt) 2007-02-28
CY1105982T1 (el) 2011-04-06
KR101100826B1 (ko) 2012-01-02
KR20050016588A (ko) 2005-02-21

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MKLA Lapsed

Effective date: 20130618