WO2002074742A3 - Derives d'indirubine inhibiteurs de cdk ayant une solubilite elevee - Google Patents

Derives d'indirubine inhibiteurs de cdk ayant une solubilite elevee Download PDF

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Publication number
WO2002074742A3
WO2002074742A3 PCT/EP2002/002983 EP0202983W WO02074742A3 WO 2002074742 A3 WO2002074742 A3 WO 2002074742A3 EP 0202983 W EP0202983 W EP 0202983W WO 02074742 A3 WO02074742 A3 WO 02074742A3
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WIPO (PCT)
Prior art keywords
diseases
disease
indirubin derivatives
increased solubility
production
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.)
Ceased
Application number
PCT/EP2002/002983
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German (de)
English (en)
Other versions
WO2002074742A2 (fr
Inventor
Rolf Jautelat
Thomas Brumby
Olaf Prien
Martina Schaefer
Gerhard Siemeister
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Bayer Pharma AG
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Schering AG
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Publication date
Application filed by Schering AG filed Critical Schering AG
Priority to JP2002573751A priority Critical patent/JP2004519502A/ja
Publication of WO2002074742A2 publication Critical patent/WO2002074742A2/fr
Publication of WO2002074742A3 publication Critical patent/WO2002074742A3/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/32Oxygen atoms
    • C07D209/36Oxygen atoms in position 3, e.g. adrenochrome
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • A61P31/22Antivirals for DNA viruses for herpes viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • Engineering & Computer Science (AREA)
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  • Neurology (AREA)
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  • Tropical Medicine & Parasitology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • AIDS & HIV (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Toxicology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)

Abstract

La présente invention concerne des dérivés d'indirubine qui, grâce à l'établissement d'un centre quaternaire en position R1, ont une solubilité radicalement accrue tout en conservant une activité biologique. Cette invention concerne également la préparation desdits dérivés et les produits intermédiaires intervenant dans leur préparation, ainsi que leur utilisation en tant que médicament pour traiter le cancer tels que les tumeurs solides et la leucémie, les maladies auto-immunes telles que le psoriasis, l'alopécie et la sclérose en plaques, l'alopécie induite par la chimiothérapie et la mucosite, les maladies cardio-vasculaires telles que les sténoses, les artérioscléroses et les resténoses, les maladies infectieuses telles que celles causées par les parasites unicellulaires tels que, Trypanosoma, Toxoplasma ou Plasmodium, ou par des champignons, les maladies néphrologiques telles que Glomerulonephritis, des maladies de neurodégénérescence chroniques telles que la maladie de Huntington, la sclérose amyotropique latérale, la maladie de Parkinson, la démence du SIDA et la maladie d'Alzheimer, les maladies de neurodégénérescence aiguës telles que les ischémies cérébrales et Neurotraumata, et les infections virales telles que les infections cytomégaliques, l'herpès, l'hépatite B et C, les maladies dues aux VIH.
PCT/EP2002/002983 2001-03-16 2002-03-18 Derives d'indirubine inhibiteurs de cdk ayant une solubilite elevee Ceased WO2002074742A2 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2002573751A JP2004519502A (ja) 2001-03-16 2002-03-18 高められた溶解性を有するcdk−阻害インジルビン誘導体

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10114138.6 2001-03-16
DE10114138A DE10114138C2 (de) 2001-03-16 2001-03-16 Cdk-inhibitorische Indirubinderivate mit erhöhter Löslichkeit

Publications (2)

Publication Number Publication Date
WO2002074742A2 WO2002074742A2 (fr) 2002-09-26
WO2002074742A3 true WO2002074742A3 (fr) 2003-02-20

Family

ID=7678630

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2002/002983 Ceased WO2002074742A2 (fr) 2001-03-16 2002-03-18 Derives d'indirubine inhibiteurs de cdk ayant une solubilite elevee

Country Status (3)

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JP (1) JP2004519502A (fr)
DE (1) DE10114138C2 (fr)
WO (1) WO2002074742A2 (fr)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10129028A1 (de) * 2001-06-11 2003-01-02 Schering Ag Lösliche Cdk-inhibitorische Indirubinderivate
US20050154046A1 (en) 2004-01-12 2005-07-14 Longgui Wang Methods of treating an inflammatory-related disease
US8563525B2 (en) 2004-01-12 2013-10-22 Natrogen Therapeutics International, Inc. Methods of treating an inflammatory-related disease
US7582670B2 (en) 2001-12-13 2009-09-01 Natrogen Therapeutics, Inc. Methods of treating an inflammatory-related disease
DE102004028899B4 (de) * 2004-06-09 2009-09-03 Technische Universität Dresden Verwendung einer Kombination zur präventiven und/oder therapeutischen Behandlung von bakteriell bedingten Infektionserkrankungen oder der Sepsis
US7781478B2 (en) 2004-07-14 2010-08-24 Ptc Therapeutics, Inc. Methods for treating hepatitis C
US20080207594A1 (en) 2005-05-04 2008-08-28 Davelogen Aktiengesellschaft Use of Gsk-3 Inhibitors for Preventing and Treating Pancreatic Autoimmune Disorders
AR059066A1 (es) 2006-01-27 2008-03-12 Amgen Inc Combinaciones del inhibidor de la angiopoyetina -2 (ang2) y el inhibidor del factor de crecimiento endotelial vascular (vegf)
WO2008152014A2 (fr) * 2007-06-12 2008-12-18 Boehringer Ingelheim International Gmbh Nouveaux composés
AU2008309517B2 (en) 2007-10-12 2013-03-14 Astrazeneca Ab Inhibitors of protein kinases
CA2789189A1 (fr) 2010-03-10 2011-09-15 Ingenium Pharmaceuticals Gmbh Inhibiteurs de proteine kinases
EP2621483A1 (fr) 2010-09-27 2013-08-07 Exelixis, Inc. Doubles inhibiteurs de met et vegf pour le traitement du cancer de la prostate résistant à la castration et des métastases osseuses ostéoblastiques
US11083755B2 (en) 2015-01-08 2021-08-10 The Board Of Trustees Of The Leland Stanford Junior University Factors and cells that provide for induction of bone, bone marrow, and cartilage
WO2024181799A1 (fr) * 2023-02-28 2024-09-06 주식회사 씨케이리제온 Nouveau dérivé d'indoline et son utilisation

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998007695A1 (fr) * 1996-08-23 1998-02-26 Sugen, Inc. Banques combinatoires d'indolinone, produits et procedes associes pour traiter des maladies
WO1999062503A2 (fr) * 1998-05-29 1999-12-09 Cnrs (Centre National De Recherche Scientifique) France Innovation Scientifique Et Transfert Utilisation de derives bisindoliques d'indigoides pour la preparation d'un medicament servant a inhiber des kinases dependantes de cycline
WO2000061555A1 (fr) * 1999-04-12 2000-10-19 Gerhard Eisenbrand Derives bisindoliques d'indigoides
WO2001037819A2 (fr) * 1999-11-23 2001-05-31 Centre National De La Recherche Scientifique (C.N.R.S.) Utilisation de derives d'indirubine pour la fabrication de medicaments
WO2002034717A1 (fr) * 2000-10-24 2002-05-02 Schering Aktiengesellschaft Derives d'indirubine soufres, leur preparation et leur utilisation

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0966963A1 (fr) * 1998-05-29 1999-12-29 Gerhard Prof. Dr. Eisenbrand Utilisation des bisindole indigoides comme inhibiteurs de CDK1

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998007695A1 (fr) * 1996-08-23 1998-02-26 Sugen, Inc. Banques combinatoires d'indolinone, produits et procedes associes pour traiter des maladies
WO1999062503A2 (fr) * 1998-05-29 1999-12-09 Cnrs (Centre National De Recherche Scientifique) France Innovation Scientifique Et Transfert Utilisation de derives bisindoliques d'indigoides pour la preparation d'un medicament servant a inhiber des kinases dependantes de cycline
WO2000061555A1 (fr) * 1999-04-12 2000-10-19 Gerhard Eisenbrand Derives bisindoliques d'indigoides
WO2001037819A2 (fr) * 1999-11-23 2001-05-31 Centre National De La Recherche Scientifique (C.N.R.S.) Utilisation de derives d'indirubine pour la fabrication de medicaments
WO2002034717A1 (fr) * 2000-10-24 2002-05-02 Schering Aktiengesellschaft Derives d'indirubine soufres, leur preparation et leur utilisation

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
HOESSEL R ET AL: "INDIRUBIN, THE ACTIVE CONSTITUENT OF A CHINESE ANTILEUKAEMIA MEDICINE, INHIBITS CYCLIN-DEPENDENT KINASES", NATURE CELL BIOLOGY, MACMILLAN PUBLISHERS, GB, vol. 1, no. 1, 1 May 1999 (1999-05-01), pages 60 - 67, XP000856197, ISSN: 1465-7392 *

Also Published As

Publication number Publication date
DE10114138A1 (de) 2002-10-02
DE10114138C2 (de) 2003-03-27
WO2002074742A2 (fr) 2002-09-26
JP2004519502A (ja) 2004-07-02

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