WO2004072041A8 - Tetrahydroquinolines as agonists of liver- x receptors - Google Patents

Tetrahydroquinolines as agonists of liver- x receptors

Info

Publication number
WO2004072041A8
WO2004072041A8 PCT/EP2004/001277 EP2004001277W WO2004072041A8 WO 2004072041 A8 WO2004072041 A8 WO 2004072041A8 EP 2004001277 W EP2004001277 W EP 2004001277W WO 2004072041 A8 WO2004072041 A8 WO 2004072041A8
Authority
WO
WIPO (PCT)
Prior art keywords
disorders
diseases
disease
pharmaceutically acceptable
liver
Prior art date
Application number
PCT/EP2004/001277
Other languages
French (fr)
Other versions
WO2004072041A1 (en
Inventor
Hana Koutnikova
Claire Marsol
Michael Sierra
Evelyne Klotz
Anne Braun-Egles
Juergen Lehmann
Original Assignee
Care X S A
Hana Koutnikova
Claire Marsol
Michael Sierra
Evelyne Klotz
Anne Braun-Egles
Juergen Lehmann
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 Care X S A, Hana Koutnikova, Claire Marsol, Michael Sierra, Evelyne Klotz, Anne Braun-Egles, Juergen Lehmann filed Critical Care X S A
Publication of WO2004072041A1 publication Critical patent/WO2004072041A1/en
Publication of WO2004072041A8 publication Critical patent/WO2004072041A8/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/20Oxygen atoms
    • C07D215/22Oxygen atoms attached in position 2 or 4
    • C07D215/233Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/20Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/38Nitrogen atoms
    • C07D215/42Nitrogen atoms attached in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/38Nitrogen atoms
    • C07D215/42Nitrogen atoms attached in position 4
    • C07D215/44Nitrogen atoms attached in position 4 with aryl radicals attached to said nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/48Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond

Abstract

The present invention relates to specific compounds and pharmaceutically acceptable salts thereof; methods for synthesizing these compounds; compositions comprising at least one of these compounds or a pharmaceutically acceptable salt thereof; and methods for modulating liver-X receptors (LXRs) activity. The present invention further concerns methods for treating and/or preventing a disease or disorder selected from the group consisting of dyslipidemia, including hyperlipidemia, dyslipoproteinemia, including hyperlipoproteinemia, disorders related to cholesterol or bile acid metabolisms, including hypercholesterolemia, gall stone or gall bladder disorders, cardiovascular disease, including atherosclerotic cardiovascular diseases, coronary artery diseases, peripheral vascular diseases, cerebrovascular diseases, thrombotic disorders, restenosis or septic shock, CNS diseases including those affecting cognitive function or age related disorders such as Alzheimer's disease, Syndrome X, a liver-X receptor-associated disorder, obesity, pancreatitis, hypertension, renal disease, cancer, rheumatoid arthritis, inflammation, skin proliferative disorders, including psoriasis, atopic dermatitis or acne, and sexual impotence, comprising administering a therapeutically effective amount of a composition comprising at least one compound or a pharmaceutically acceptable salt thereof of the invention.
PCT/EP2004/001277 2003-02-12 2004-02-11 Tetrahydroquinolines as agonists of liver- x receptors WO2004072041A1 (en)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
EP03360028 2003-02-12
EP03360027.1 2003-02-12
EP03360026.3 2003-02-12
EP03360028.9 2003-02-12
EP03360026 2003-02-12
EP03360027 2003-02-12

Publications (2)

Publication Number Publication Date
WO2004072041A1 WO2004072041A1 (en) 2004-08-26
WO2004072041A8 true WO2004072041A8 (en) 2004-12-09

Family

ID=32872413

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2004/001277 WO2004072041A1 (en) 2003-02-12 2004-02-11 Tetrahydroquinolines as agonists of liver- x receptors

Country Status (1)

Country Link
WO (1) WO2004072041A1 (en)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2881137B1 (en) * 2005-01-27 2007-03-02 Servier Lab NOVEL HETEROCYCLIC OXIMIC DERIVATIVES, PROCESS FOR PREPARING THEM AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
DE102005027168A1 (en) * 2005-06-13 2006-12-14 Merck Patent Gmbh Tetrahydroquinolines
UY30244A1 (en) 2006-03-30 2007-11-30 Tanabe Seiyaku Co A PROCESS TO PREPARE DERIVATIVES OF TETRAHYDROQUINOLINE
JP2009536954A (en) 2006-05-11 2009-10-22 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 3,4-Dihydro-2H-benzo [1,4] oxazine and thiazine derivatives as CETP inhibitors
JP2009536953A (en) 2006-05-11 2009-10-22 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 1,2,3,4-Tetrahydro-quinoline derivatives as CETP inhibitors
WO2010047982A1 (en) 2008-10-22 2010-04-29 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
WO2010051206A1 (en) 2008-10-31 2010-05-06 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
AU2011218830B2 (en) 2010-02-25 2014-07-24 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
CA2811145A1 (en) 2010-09-07 2012-03-15 Snu R&Db Foundation Sesterterpene compound and use thereof
US8546427B2 (en) * 2010-10-20 2013-10-01 Hoffmann-La Roche Inc. Tetrahydroquinoline derivatives
CN103476258B (en) 2011-02-25 2017-04-26 默沙东公司 Novel cyclic azabenzimidazole derivatives useful as anti-diabetic agents
EP2880028B1 (en) 2012-08-02 2020-09-30 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
CA2898482A1 (en) 2013-02-22 2014-08-28 Linda L. Brockunier Antidiabetic bicyclic compounds
EP2970119B1 (en) 2013-03-14 2021-11-03 Merck Sharp & Dohme Corp. Novel indole derivatives useful as anti-diabetic agents
WO2015051496A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
WO2015074081A1 (en) 2013-11-18 2015-05-21 Bair Kenneth W Benzopiperazine compositions as bet bromodomain inhibitors
CN110627770A (en) 2013-11-18 2019-12-31 福马疗法公司 Tetrahydroquinoline compositions as BET bromodomain inhibitors
EP3091970B1 (en) 2014-01-10 2020-10-28 Rgenix, Inc. Lxr agonists and uses thereof
CA3010883A1 (en) 2016-01-11 2017-07-20 The Rockefeller University Methods for the treatment of myeloid derived suppressor cells related disorders
EP3551176A4 (en) 2016-12-06 2020-06-24 Merck Sharp & Dohme Corp. Antidiabetic heterocyclic compounds
EP3558298A4 (en) 2016-12-20 2020-08-05 Merck Sharp & Dohme Corp. Antidiabetic spirochroman compounds
CA3078981A1 (en) 2017-11-21 2019-05-31 Rgenix, Inc. Polymorphs and uses thereof
JP2023509845A (en) 2019-12-13 2023-03-10 インスピルナ,インコーポレーテッド Metal salt and its use

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6316503B1 (en) * 1999-03-15 2001-11-13 Tularik Inc. LXR modulators

Also Published As

Publication number Publication date
WO2004072041A1 (en) 2004-08-26

Similar Documents

Publication Publication Date Title
WO2004072046A3 (en) Quinoline derivatives and their use for modulation of lxr activity
WO2004072041A8 (en) Tetrahydroquinolines as agonists of liver- x receptors
WO2004072042A3 (en) Quinoline derivative and their use for modulation of lxr activity
WO2007038209A3 (en) Fused tetracyclic mglur1 antagonists as therapeutic agents
TW200609231A (en) Mglur1 antagonists as therapeutic agents
ATE423769T1 (en) FLUORINE AND SULFONYLAMINO CONTAINING, 3,6-DISUBSTITUTED AZABICYCLO 3.1.0 HEXANE DERIVATIVES AS MUSCARINO RECEPTOR ANTAGONISTS
WO2003047577A3 (en) Pharmaceutical compositions comprising dihydropyridinone compounds and an immunoregulatory or an antiinflammatory agent and their uses
WO2004094384A3 (en) (hetero) arylamide 2-hydroxy-3-diaminoalkanes for use in the treatment of alzheimer’s disease
WO2003027068A3 (en) Substituted amines for the treatment of neurological disorders
WO1999065449A8 (en) INHIBITORS OF TRANSCRIPTION FACTOR NF-λB
WO1998020864A3 (en) Use of selected non-steroidal antiinflammatory compounds for the prevention and the treatment of neurodegenerative diseases
WO2007064932A3 (en) Pyrrolotriazine derivatives useful for treating cancer through inhibition of aurora kinase
CA2460939A1 (en) Substituted pyrazolyl compounds for the treatment of inflammation
WO2004110418A3 (en) Carbonyl compounds as inhibitors of histone deacetylase for the treatment of disease
WO2007067511A3 (en) Morpholine carboxamide prokineticin receptor antagonists
WO2004050609A8 (en) Substituted ureas and carbamates
WO2003024935A3 (en) Substituted pyrazolyl compounds for the treatment of inflammation
WO2007087151A3 (en) Combination of ache inhibitor and 5-ht6 antagonist for the treatment of cognitive dysfunction
EP1251126A3 (en) Fluoro-substituted benzenesulfonyl compounds for the treatment of inflammation
MY136718A (en) Sulfonamide compounds for the treatment of neurodegenerative disorders
WO2003027075A3 (en) Substituted pyrazolyl benzenesulfamide compounds for the treatment of inflammation
WO2001051044A3 (en) Substances for use in treating psoriasis
WO2004055201A3 (en) Cholesterol 24-hydroxylase (cyp46) as therapeutic target for the treatment of alzheimer's disease
WO2001079209A3 (en) Diazafluorenone il-8 antagonists
EP1958939A3 (en) Pyrazole-amine compounds for the treatment of neurodegenerative disorders

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A1

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BW BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE EG ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NA NI NO NZ OM PG PH PL PT RO RU SC SD SE SG SK SL SY TJ TM TN TR TT TZ UA UG US UZ VC VN YU ZA ZM ZW

AL Designated countries for regional patents

Kind code of ref document: A1

Designated state(s): BW GH GM KE LS MW MZ SD SL SZ TZ UG ZM ZW AM AZ BY KG KZ MD RU TJ TM AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IT LU MC NL PT RO SE SI SK TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
WR Later publication of a revised version of an international search report
CFP Corrected version of a pamphlet front page
CR1 Correction of entry in section i

Free format text: IN PCT GAZETTE 35/2004 UNDER (72, 75) REPLACE "LEHMANN, JÜRGER" BY "LEHMANN, JÜRGEN" AND UNDER (74)THE ADDRESS SHOULD READ "SIEBERTSTRASSE 4, 81675 MÜNICH (DE)."

122 Ep: pct application non-entry in european phase