TW201242953A - Imidazole prodrug LXR modulators - Google Patents

Imidazole prodrug LXR modulators Download PDF

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Publication number
TW201242953A
TW201242953A TW101110267A TW101110267A TW201242953A TW 201242953 A TW201242953 A TW 201242953A TW 101110267 A TW101110267 A TW 101110267A TW 101110267 A TW101110267 A TW 101110267A TW 201242953 A TW201242953 A TW 201242953A
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TW
Taiwan
Prior art keywords
compound
doc
pharmaceutically acceptable
acid
solvent
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Application number
TW101110267A
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English (en)
Chinese (zh)
Inventor
Ellen K Kick
Michael J Hageman
Victor R Guarino
Ching-Chiang Su
Chenkou Wei
Jayakumar Sankara Warrier
Satheesh Kesavan Nair
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Bristol Myers Squibb Co
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Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of TW201242953A publication Critical patent/TW201242953A/zh

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/4174Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/675Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
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    • 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
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • 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
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/06Phosphorus compounds without P—C bonds
    • C07F9/08Esters of oxyacids of phosphorus
    • C07F9/09Esters of phosphoric acids
    • C07F9/12Esters of phosphoric acids with hydroxyaryl compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6503Five-membered rings
    • C07F9/6506Five-membered rings having the nitrogen atoms in positions 1 and 3

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
TW101110267A 2011-03-25 2012-03-23 Imidazole prodrug LXR modulators TW201242953A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201161467404P 2011-03-25 2011-03-25

Publications (1)

Publication Number Publication Date
TW201242953A true TW201242953A (en) 2012-11-01

Family

ID=45926934

Family Applications (1)

Application Number Title Priority Date Filing Date
TW101110267A TW201242953A (en) 2011-03-25 2012-03-23 Imidazole prodrug LXR modulators

Country Status (8)

Country Link
US (1) US8901106B2 (https=)
EP (1) EP2688871B1 (https=)
JP (1) JP2014510110A (https=)
CN (1) CN103443082B (https=)
AR (1) AR088728A1 (https=)
ES (1) ES2548050T3 (https=)
TW (1) TW201242953A (https=)
WO (1) WO2012135082A1 (https=)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2820013T3 (en) 2012-03-02 2018-10-29 Ralexar Therapeutics Inc Liver X Receptor (LXR) modulators for the treatment of dermal diseases, disorders and conditions
EP3626309B1 (en) 2012-08-13 2023-03-08 The Rockefeller University Lxrbeta agonist for the treatment of cancer
JP6442475B2 (ja) * 2013-03-15 2018-12-19 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company Lxr調節因子
JP2016532713A (ja) 2013-09-04 2016-10-20 アレクサー セラピューティクス, インク. 肝臓x受容体(lxr)調節因子
PT3041835T (pt) 2013-09-04 2020-07-13 Ellora Therapeutics Inc Moduladores de recetor de fígado x (lxr)
US10669296B2 (en) 2014-01-10 2020-06-02 Rgenix, Inc. LXR agonists and uses thereof
MX380578B (es) 2014-10-03 2025-03-12 Ucb Biopharma Sprl Derivados de imidazol pentaciclicos fusionados.
CA3010883A1 (en) 2016-01-11 2017-07-20 The Rockefeller University Methods for the treatment of myeloid derived suppressor cells related disorders
EA201892153A1 (ru) 2016-04-01 2019-04-30 Юсб Байофарма Спрл Конденсированные пентациклические производные имидазола в качестве модуляторов активности tnf
JP6968090B2 (ja) 2016-04-01 2021-11-17 ユーシービー バイオファルマ エスアールエル Tnf活性のモジュレーターとしての縮合五環式イミダゾール誘導体
US10766906B2 (en) 2016-04-01 2020-09-08 UCB Biopharma SRL Fused hexacyclic imidazole derivatives as modulators of TNF activity
EP3436458B1 (en) 2016-04-01 2021-06-02 UCB Biopharma SRL Fused pentacyclic imidazole derivatives as modulators of tnf activity
AU2017246228B2 (en) * 2016-04-04 2021-04-15 Chemocentryx, Inc. Soluble C5aR antagonists
CN110461842A (zh) 2017-03-15 2019-11-15 Ucb生物制药私人有限公司 作为tnf活性调节剂的稠合五环咪唑衍生物
EP3713575A4 (en) 2017-11-21 2021-08-25 Rgenix, Inc. POLYMORPHS AND THEIR USES
HUE067466T2 (hu) 2019-12-13 2024-10-28 Inspirna Inc Fémsók és alkalmazásuk

Family Cites Families (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4231938A (en) 1979-06-15 1980-11-04 Merck & Co., Inc. Hypocholesteremic fermentation products and process of preparation
US4444784A (en) 1980-08-05 1984-04-24 Merck & Co., Inc. Antihypercholesterolemic compounds
MX7065E (es) 1980-06-06 1987-04-10 Sankyo Co Un procedimiento microbiologico para preparar derivados de ml-236b
HU204253B (en) 1982-11-22 1991-12-30 Sandoz Ag Process for producing mevalonolactone analogues and derivatives and pharmaceutical compositions containing them
US5354772A (en) 1982-11-22 1994-10-11 Sandoz Pharm. Corp. Indole analogs of mevalonolactone and derivatives thereof
FI94339C (fi) 1989-07-21 1995-08-25 Warner Lambert Co Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi
US5177080A (en) 1990-12-14 1993-01-05 Bayer Aktiengesellschaft Substituted pyridyl-dihydroxy-heptenoic acid and its salts
WO1993006215A1 (en) 1991-09-17 1993-04-01 The Salk Institute For Biological Studies Receptor of the thyroid/steroid hormone receptor superfamily
WO1998032444A1 (en) 1997-01-24 1998-07-30 The Regents Of The University Of California USE OF FXR, PPARα AND LXRα ACTIVATORS TO RESTORE BARRIER FUNCTION, PROMOTE EPIDERMAL DIFFERENTIATION AND INHIBIT PROLIFERATION
US5767134A (en) * 1997-05-15 1998-06-16 Vion Pharmaceuticals, Inc. Prodrug forms of ribonucleotide reductase inhibitors 3-AP and 3-AMP
EP1115853A2 (en) 1998-09-23 2001-07-18 Ludmila Solomin Analysis of ligand activated nuclear receptors in vivo
DE69940958D1 (de) 1998-12-23 2009-07-16 Glaxo Group Ltd Bestimmungsmethode fur liganden der nuklearen rezeptoren
US6071955A (en) 1999-02-25 2000-06-06 The Regents Of The University Of California FXR, PPARA and LXRA activators to treat acne/acneiform conditions
US6316503B1 (en) 1999-03-15 2001-11-13 Tularik Inc. LXR modulators
AU780658B2 (en) 1999-03-26 2005-04-07 City Of Hope Method of affecting cholesterol catabolism using nuclear bile acid receptor
SG121853A1 (en) 1999-06-18 2006-05-26 Cv Therapeutics Inc Compositions and methods for increasing cholesterol efflux and raising hdl using atp binding cassette transporter protein abc1
JP2004500332A (ja) 1999-07-08 2004-01-08 テュラリク インコーポレイテッド Hdlコレステロール値を上昇させる組成物および方法
AU2000235960A1 (en) 2000-02-14 2001-08-27 Tularik, Inc. Lxr modulators
AU2001262984A1 (en) 2000-05-03 2001-11-12 Tularik, Inc. Treatment of hypertriglyceridemia and other conditions using lxr modulators
US6924311B2 (en) 2001-10-17 2005-08-02 X-Ceptor Therapeutics, Inc. Methods for affecting various diseases utilizing LXR compounds
DE602004014806D1 (de) * 2003-10-08 2008-08-14 Smithkline Beecham Corp Triphenylethyleneverbindungen als selektive modulatoren des östrogenrezeptors
WO2006066070A2 (en) * 2004-12-17 2006-06-22 Nps Pharmaceuticals, Inc. Prodrug constructs of pyrimidinone compounds as calcilytics
SG162803A1 (en) * 2005-06-27 2010-07-29 Exelixis Inc Imidazole based lxr modulators
US8703805B2 (en) 2005-06-27 2014-04-22 Exelixis Patent Company Llc Modulators of LXR
KR20090094125A (ko) * 2006-12-08 2009-09-03 엑셀리시스, 인코포레이티드 Lxr 및 fxr 조절자
US20100152238A1 (en) * 2007-03-05 2010-06-17 Yissum Research Development Company Of The Hebrew University Of Jerusalem Novel quinonoid derivatives of cannabinoids and their use in the treatment of malignancies
KR101676704B1 (ko) 2009-05-28 2016-11-16 엑셀리시스 페이턴트 컴퍼니 엘엘씨 Lxr 조절자

Also Published As

Publication number Publication date
EP2688871A1 (en) 2014-01-29
WO2012135082A1 (en) 2012-10-04
CN103443082A (zh) 2013-12-11
CN103443082B (zh) 2015-11-25
US20140018321A1 (en) 2014-01-16
EP2688871B1 (en) 2015-08-26
US8901106B2 (en) 2014-12-02
AR088728A1 (es) 2014-07-02
JP2014510110A (ja) 2014-04-24
ES2548050T3 (es) 2015-10-13

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