CN100348609C - 治疗代谢紊乱的糖皮质激素受体配基 - Google Patents

治疗代谢紊乱的糖皮质激素受体配基 Download PDF

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Publication number
CN100348609C
CN100348609C CNB03814137XA CN03814137A CN100348609C CN 100348609 C CN100348609 C CN 100348609C CN B03814137X A CNB03814137X A CN B03814137XA CN 03814137 A CN03814137 A CN 03814137A CN 100348609 C CN100348609 C CN 100348609C
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China
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hydroxy
hydrogen
methyl
compound
alkyl
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Expired - Fee Related
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CNB03814137XA
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English (en)
Chinese (zh)
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CN1662549A (zh
Inventor
托马斯·W·范格尔顿
詹姆士·T·林克
诺亚·子
菲利普·R·许姆
赖春秋
史蒂文·J·理查兹
皮尔·B·雅各布森
理查德·D·毕晓普
布雷德利·D·盖茨
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Karo Healthcare AB
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Karo Bio AB
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Priority claimed from US10/460,491 external-priority patent/US7141559B2/en
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Publication of CN1662549A publication Critical patent/CN1662549A/zh
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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Diabetes (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (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)
CNB03814137XA 2002-06-19 2003-06-17 治疗代谢紊乱的糖皮质激素受体配基 Expired - Fee Related CN100348609C (zh)

Applications Claiming Priority (4)

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

Publications (2)

Publication Number Publication Date
CN1662549A CN1662549A (zh) 2005-08-31
CN100348609C true CN100348609C (zh) 2007-11-14

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ID=30002639

Family Applications (1)

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CNB03814137XA Expired - Fee Related CN100348609C (zh) 2002-06-19 2003-06-17 治疗代谢紊乱的糖皮质激素受体配基

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
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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
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
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
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
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
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
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
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
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
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
GB0514302D0 (en) * 2005-07-12 2005-08-17 Karobio Ab Improved crystalline material
US8410284B2 (en) 2008-10-22 2013-04-02 Merck Sharp & Dohme Corp Cyclic benzimidazole derivatives useful as anti-diabetic agents
WO2010051206A1 (en) 2008-10-31 2010-05-06 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
WO2011058193A1 (en) 2009-11-16 2011-05-19 Mellitech [1,5]-diazocin derivatives
JP2013520502A (ja) 2010-02-25 2013-06-06 メルク・シャープ・エンド・ドーム・コーポレイション 有用な抗糖尿病薬である新規な環状ベンズイミダゾール誘導体
CA2826649C (en) 2011-02-25 2016-07-26 Merck Sharp & Dohme Corp. Novel cyclic azabenzimidazole derivatives useful as anti-diabetic agents
PT2758060T (pt) * 2011-09-19 2018-01-24 ETH Zürich Moduladores de ror gama para o tratamento de complicações de diabetes ii
US20140045746A1 (en) 2012-08-02 2014-02-13 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
WO2018106518A1 (en) 2016-12-06 2018-06-14 Merck Sharp & Dohme Corp. Antidiabetic heterocyclic compounds
WO2018118670A1 (en) 2016-12-20 2018-06-28 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

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0489423A1 (de) * 1990-12-06 1992-06-10 Hoechst Aktiengesellschaft Gallensäurederivate, Verfahren zu ihrer Herstellung und Verwendung dieser Verbindung als Arzneimittel
US5462933A (en) * 1989-09-14 1995-10-31 Hoechst Aktiengesellschaft Modified bile acid conjugates, and their use as pharmaceuticals
WO2000058337A1 (en) * 1999-03-27 2000-10-05 Karo Bio Ab Liver specific bile acid derivatives of the glucocorticoid antagonist ru486

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4000397A1 (de) * 1990-01-09 1991-07-11 Hoechst Ag Lipidselektive antioxidantien sowie deren herstellung und verwendung

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5462933A (en) * 1989-09-14 1995-10-31 Hoechst Aktiengesellschaft Modified bile acid conjugates, and their use as pharmaceuticals
EP0489423A1 (de) * 1990-12-06 1992-06-10 Hoechst Aktiengesellschaft Gallensäurederivate, Verfahren zu ihrer Herstellung und Verwendung dieser Verbindung als Arzneimittel
WO2000058337A1 (en) * 1999-03-27 2000-10-05 Karo Bio Ab Liver specific bile acid derivatives of the glucocorticoid antagonist ru486

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
LIVER-SPECIFIC DRUG TARGETING BY COUPLING TOBILE ACIDS. KRAMER W ET AL.J.BIO.CHEM,Vol.267 No.26. 1992 *

Also Published As

Publication number Publication date
UY27862A1 (es) 2004-04-30
AU2003243622A2 (en) 2004-01-06
CA2488535C (en) 2012-02-07
AU2003243622A1 (en) 2004-01-06
DE60309909D1 (de) 2007-01-04
DK1551860T3 (da) 2007-04-02
DE60309909T2 (de) 2007-06-21
ATE346082T1 (de) 2006-12-15
EP1551860A1 (en) 2005-07-13
CY1105982T1 (el) 2011-04-06
WO2004000869A1 (en) 2003-12-31
CN1662549A (zh) 2005-08-31
AU2003243622B2 (en) 2009-05-28
KR101100826B1 (ko) 2012-01-02
KR20050016588A (ko) 2005-02-21
EP1551860B1 (en) 2006-11-22
AR040278A1 (es) 2005-03-23
JP2005533807A (ja) 2005-11-10
TW200410983A (en) 2004-07-01
JP4611019B2 (ja) 2011-01-12
TWI285646B (en) 2007-08-21
PT1551860E (pt) 2007-02-28
ES2278195T3 (es) 2007-08-01
AU2003243622B9 (en) 2009-07-16
CA2488535A1 (en) 2003-12-31

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Termination date: 20120617