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WO2003031408A3 - Tricyclic compounds useful for modulating lxr - Google Patents

Tricyclic compounds useful for modulating lxr Download PDF

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Publication number
WO2003031408A3
WO2003031408A3 PCT/US2002/028147 US0228147W WO03031408A3 WO 2003031408 A3 WO2003031408 A3 WO 2003031408A3 US 0228147 W US0228147 W US 0228147W WO 03031408 A3 WO03031408 A3 WO 03031408A3
Authority
WO
WIPO (PCT)
Prior art keywords
compounds useful
tricyclic compounds
modulating lxr
modulating
lxr
Prior art date
Application number
PCT/US2002/028147
Other languages
French (fr)
Other versions
WO2003031408A2 (en
Inventor
Thomas Patrick Burris
Guoqing Cao
George Joseph Cullinan
Patrick Irving Eacho
Jefferson Ray Mccowan
Kuo-Long Yu
Original Assignee
Lilly Co Eli
Thomas Patrick Burris
Guoqing Cao
George Joseph Cullinan
Patrick Irving Eacho
Jefferson Ray Mccowan
Kuo-Long Yu
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 Lilly Co Eli, Thomas Patrick Burris, Guoqing Cao, George Joseph Cullinan, Patrick Irving Eacho, Jefferson Ray Mccowan, Kuo-Long Yu filed Critical Lilly Co Eli
Priority to AU2002336433A priority Critical patent/AU2002336433A1/en
Publication of WO2003031408A2 publication Critical patent/WO2003031408A2/en
Publication of WO2003031408A3 publication Critical patent/WO2003031408A3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/096—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Compounds of formula (I) useful for treating artherosclerosis and its sequelae, useful for modulating LXR activity, their compositions and processes for their preparing are provided.
PCT/US2002/028147 2001-10-08 2002-09-30 Tricyclic compounds useful for modulating lxr WO2003031408A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2002336433A AU2002336433A1 (en) 2001-10-08 2002-09-30 Tricyclic compounds useful for modulating lxr

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US32764401P 2001-10-08 2001-10-08
US60/327,644 2001-10-08

Publications (2)

Publication Number Publication Date
WO2003031408A2 WO2003031408A2 (en) 2003-04-17
WO2003031408A3 true WO2003031408A3 (en) 2003-08-14

Family

ID=23277404

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2002/028147 WO2003031408A2 (en) 2001-10-08 2002-09-30 Tricyclic compounds useful for modulating lxr

Country Status (2)

Country Link
AU (1) AU2002336433A1 (en)
WO (1) WO2003031408A2 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7576215B2 (en) 2003-12-12 2009-08-18 Wyeth Quinolines and pharmaceutical compositions thereof

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004072046A2 (en) * 2003-02-12 2004-08-26 Carex S.A. Quinoline derivatives and their use for modulation of lxr activity
TW200619191A (en) 2004-10-27 2006-06-16 Sankyo Co Phenyl compounds with more than 2 substitutes
AU2009307884B2 (en) 2008-10-22 2014-07-31 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
US8329914B2 (en) 2008-10-31 2012-12-11 Merck Sharp & Dohme Corp Cyclic benzimidazole derivatives useful as anti-diabetic agents
US8895596B2 (en) 2010-02-25 2014-11-25 Merck Sharp & Dohme Corp Cyclic benzimidazole derivatives useful as anti-diabetic agents
EP2615094A4 (en) 2010-09-07 2013-09-18 Snu R&Db Foundation Sesterterpene compounds and use thereof
BR122021002201A8 (en) 2011-02-25 2023-04-11 Merck Sharp & Dohme COMPOUND, COMPOSITION, USE OF A COMPOUND, AND METHOD OF TREATMENT OF A DISORDER, CONDITION OR DISEASE
EP2880028B1 (en) 2012-08-02 2020-09-30 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
MX2015010935A (en) 2013-02-22 2015-10-29 Merck Sharp & Dohme Antidiabetic bicyclic compounds.
WO2014139388A1 (en) 2013-03-14 2014-09-18 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
EP3091970B1 (en) 2014-01-10 2020-10-28 Rgenix, Inc. Lxr agonists and uses thereof
US11648220B2 (en) 2016-01-11 2023-05-16 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
WO2018118670A1 (en) 2016-12-20 2018-06-28 Merck Sharp & Dohme Corp. Antidiabetic spirochroman compounds
EP3713575A4 (en) 2017-11-21 2021-08-25 Rgenix, Inc. Polymorphs and uses thereof
CN111303017B (en) * 2019-08-28 2022-11-11 上海中医药大学 A class of compounds containing 9,10-dihydrophenanthrene skeleton and preparation method and use 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

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4444784A (en) * 1980-08-05 1984-04-24 Merck & Co., Inc. Antihypercholesterolemic compounds
WO1999066915A2 (en) * 1998-06-23 1999-12-29 Southern Illinois University At Carbondale Therapeutic applications of estrogenic carboxylic acids
WO2001041704A2 (en) * 1999-12-13 2001-06-14 Merck & Co., Inc. Method for the prevention and/or treatment of atherosclerosis

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4444784A (en) * 1980-08-05 1984-04-24 Merck & Co., Inc. Antihypercholesterolemic compounds
WO1999066915A2 (en) * 1998-06-23 1999-12-29 Southern Illinois University At Carbondale Therapeutic applications of estrogenic carboxylic acids
WO2001041704A2 (en) * 1999-12-13 2001-06-14 Merck & Co., Inc. Method for the prevention and/or treatment of atherosclerosis

Non-Patent Citations (7)

* Cited by examiner, † Cited by third party
Title
BIEN, SHLOMO ET AL: "Steric aspects of the intramolecular cyclization of 2-arylcyclohexylacetic acids. III", JOURNAL OF THE CHEMICAL SOCIETY [SECTION] C: ORGANIC (1967), (1), 115-19, XP009010266 *
CHINI, MARCO ET AL: "Effect of the 7-methyl substituent on the ring opening process of the diastereoisomeric benzylic epoxides derived from 1,2,3,9,10,10a-hexahydrophenanthrene. Differences and similarities between different 2-aryloxirane models", GAZZETTA CHIMICA ITALIANA (1990), 120(12), 733-9, XP009010270 *
CHINI, MARCO ET AL: "Synthesis and reactivity of benzylic epoxides derived from 1,2,3,9,10,10a-hexahydrophenanthrene. Search for a unified mechanism for the ring opening of 2-aryloxiranes", JOURNAL OF ORGANIC CHEMISTRY (1989), 54(16), 3930-6, XP002240152 *
DUTHALER, RUDOLF O. ET AL: "The relative stabilities of substituted cis- and trans-1,2,3,4,4a,9,10,10a-octahydrophenanthrenes, including configurational corrections in the Elad-Ginsburg morphine synthesis", HELVETICA CHIMICA ACTA (1986), 69(7), 1559-66, XP009010269 *
THOMPSON, HUGH W. ET AL: "Mechanism of the catalyzed Diels-Alder reaction", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (1970), 92(10), 3218-20, XP002240150 *
THOMPSON, HUGH W. ET AL: "Stereochemical equilibrium in benzoctalones", JOURNAL OF ORGANIC CHEMISTRY (1988), 53(18), 4201-9, XP002008448 *
ZEE, SHENG HSU ET AL: "The reduction and nitration of 1-keto and 4-keto-1,2,3,4- tetrahydrophenanthrene", JOURNAL OF THE CHINESE CHEMICAL SOCIETY (TAIPEI, TAIWAN) (1987), 34(1), 25-32, XP009010265 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7576215B2 (en) 2003-12-12 2009-08-18 Wyeth Quinolines and pharmaceutical compositions thereof

Also Published As

Publication number Publication date
AU2002336433A1 (en) 2003-04-22
WO2003031408A2 (en) 2003-04-17

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