WO2007041076A3 - Derives de 1,2,3,5-tetrahydro-cyclopental[c]quinolin-4-one utilises en tant qu'agonistes du recepteur rxr pour le traitement de la dyslipidemie, de l'hypercholesterolemie et du diabete - Google Patents

Derives de 1,2,3,5-tetrahydro-cyclopental[c]quinolin-4-one utilises en tant qu'agonistes du recepteur rxr pour le traitement de la dyslipidemie, de l'hypercholesterolemie et du diabete Download PDF

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Publication number
WO2007041076A3
WO2007041076A3 PCT/US2006/037321 US2006037321W WO2007041076A3 WO 2007041076 A3 WO2007041076 A3 WO 2007041076A3 US 2006037321 W US2006037321 W US 2006037321W WO 2007041076 A3 WO2007041076 A3 WO 2007041076A3
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WIPO (PCT)
Prior art keywords
derivatives
cyclopental
dyslipidemia
hypercholesterolemia
quinolin
Prior art date
Application number
PCT/US2006/037321
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English (en)
Other versions
WO2007041076A2 (fr
Inventor
Lagu Bharat
Barbara Pio
Original Assignee
Janssen Pharmaceutica Nv
Lagu Bharat
Barbara Pio
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
Application filed by Janssen Pharmaceutica Nv, Lagu Bharat, Barbara Pio filed Critical Janssen Pharmaceutica Nv
Priority to JP2008533489A priority Critical patent/JP2009510071A/ja
Priority to EP06815371A priority patent/EP1937640A2/fr
Priority to CA002624345A priority patent/CA2624345A1/fr
Publication of WO2007041076A2 publication Critical patent/WO2007041076A2/fr
Publication of WO2007041076A3 publication Critical patent/WO2007041076A3/fr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/233—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/12—Ophthalmic agents for cataracts
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P3/02—Nutrients, e.g. vitamins, minerals
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • 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
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Nutrition Science (AREA)
  • Biomedical Technology (AREA)
  • Vascular Medicine (AREA)
  • Neurosurgery (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)

Abstract

L'invention concerne des composés de formule (I), des méthodes de préparation desdits composés, de compositions, d'intermédiaires et de dérivés de ceux-ci ; et des méthodes de traitement de troubles à médiation assurée par le récepteur RXR. Plus particulièrement, les composés de l'invention sont des agonistes du récepteur RXR utilisés pour le traitement de troubles à médiation assurée par le récepteur RXR.
PCT/US2006/037321 2005-09-30 2006-09-25 Derives de 1,2,3,5-tetrahydro-cyclopental[c]quinolin-4-one utilises en tant qu'agonistes du recepteur rxr pour le traitement de la dyslipidemie, de l'hypercholesterolemie et du diabete WO2007041076A2 (fr)

Priority Applications (3)

Application Number Priority Date Filing Date Title
JP2008533489A JP2009510071A (ja) 2005-09-30 2006-09-25 異常脂血症、高コレステロール血症及び糖尿病の処置のためのｒｘｒアゴニストとしての１，２，３，５−テトラヒドロ−シクロペンタ［ｃ］キノリン−４−オン誘導体
EP06815371A EP1937640A2 (fr) 2005-09-30 2006-09-25 Derives de 1,2,3,5-tetrahydro-cyclopental[c]quinolin-4-one utilises en tant qu'agonistes du recepteur rxr pour le traitement de la dyslipidemie, de l'hypercholesterolemie et du diabete
CA002624345A CA2624345A1 (fr) 2005-09-30 2006-09-25 Derives de 1,2,3,5-tetrahydro-cyclopental[c]quinolin-4-one utilises en tant qu'agonistes du recepteur rxr pour le traitement de la dyslipidemie, de l'hypercholesterolemie et du diabete

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US72250705P 2005-09-30 2005-09-30
US60/722,507 2005-09-30

Publications (2)

Publication Number Publication Date
WO2007041076A2 WO2007041076A2 (fr) 2007-04-12
WO2007041076A3 true WO2007041076A3 (fr) 2007-06-07

Family

ID=37625109

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2006/037321 WO2007041076A2 (fr) 2005-09-30 2006-09-25 Derives de 1,2,3,5-tetrahydro-cyclopental[c]quinolin-4-one utilises en tant qu'agonistes du recepteur rxr pour le traitement de la dyslipidemie, de l'hypercholesterolemie et du diabete

Country Status (5)

Country Link
EP (1) EP1937640A2 (fr)
JP (1) JP2009510071A (fr)
CN (1) CN101316822A (fr)
CA (1) CA2624345A1 (fr)
WO (1) WO2007041076A2 (fr)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009510114A (ja) 2005-09-30 2009-03-12 ビテ ファーマシューティカルズ， インコーポレイテッド 特定のｒｘｒアゴニストによる癌治療
CA2716726C (fr) * 2008-03-27 2017-01-24 Janssen Pharmaceutica Nv Tetrahydrophenanthridinones et tetrahydrocyclopentaquinolinones comme inhibiteurs de la polymerisation de la tubuline et de parp
CN104114171A (zh) 2011-12-13 2014-10-22 Io治疗公司 使用rxr激动剂的自身免疫紊乱的治疗
US10653650B2 (en) 2011-12-13 2020-05-19 Io Therapeutics, Inc. Treatment of diseases by concurrently eliciting remyelination effects and immunomodulatory effects using selective RXR agonists
MY192609A (en) * 2014-01-14 2022-08-29 Connexios Life Sciences Pvt Ltd Substituted bicyclic heteroaryl compounds as rxr agonists
GB201406486D0 (en) 2014-04-10 2014-05-28 Redx Pharma Ltd Antibacterial compounds
CA3003734A1 (fr) 2015-10-31 2017-05-04 Io Therapeutics, Inc. Traitement des troubles du systeme nerveux au moyen de combinaisons d'agonistes de rxr et d'hormones thyroidiennes
CA3016878C (fr) 2016-03-10 2024-02-27 Io Therapeutics, Inc. Traitement de troubles musculaires avec des combinaisons d'agonistes de rxr et d'hormones thyroidiennes
ES2940239T3 (es) 2016-03-10 2023-05-04 Io Therapeutics Inc Tratamiento de enfermedades autoinmunitarias con combinaciones de agonistas de RXR y hormonas tiroideas
CA3076373A1 (fr) 2017-09-20 2019-03-28 Io Therapeutics, Inc. Traitement de maladie avec des esters d'agonistes de rxr selectifs
US10966950B2 (en) 2019-06-11 2021-04-06 Io Therapeutics, Inc. Use of an RXR agonist in treating HER2+ cancers
US11896558B2 (en) 2021-12-07 2024-02-13 Io Therapeutics, Inc. Use of an RXR agonist and taxanes in treating Her2+ cancers

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1117648B1 (fr) * 1998-10-01 2003-08-06 Allergan, Inc. Derives de tetrahydroquinoline dotes d'une activite selective pour les recepteurs de retinoide x

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1117648B1 (fr) * 1998-10-01 2003-08-06 Allergan, Inc. Derives de tetrahydroquinoline dotes d'une activite selective pour les recepteurs de retinoide x

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
HAFFNER, CURT D. ET AL: "Structure-Based Design of Potent Retinoid X Receptor alpha Agonists", JOURNAL OF MEDICINAL CHEMISTRY, vol. 47, 2004, pages 2010 - 2029, XP002415204 *
POGENBERG, VIVIAN ET AL: "Characterization of the Interaction between Retinoic Acid Receptor/Retinoid X Receptor (RAR/RXR) Heterodimers and Transcriptional Coactivators through Structural and Fluorescence Anisotropy Studies", JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 280, no. 2, January 2005 (2005-01-01), pages 1625 - 1633, XP002415142 *

Also Published As

Publication number Publication date
JP2009510071A (ja) 2009-03-12
CA2624345A1 (fr) 2007-04-12
WO2007041076A2 (fr) 2007-04-12
CN101316822A (zh) 2008-12-03
EP1937640A2 (fr) 2008-07-02

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