AU2010254082B2 - LXR modulators - Google Patents

LXR modulators Download PDF

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Publication number
AU2010254082B2
AU2010254082B2 AU2010254082A AU2010254082A AU2010254082B2 AU 2010254082 B2 AU2010254082 B2 AU 2010254082B2 AU 2010254082 A AU2010254082 A AU 2010254082A AU 2010254082 A AU2010254082 A AU 2010254082A AU 2010254082 B2 AU2010254082 B2 AU 2010254082B2
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AU
Australia
Prior art keywords
propan
imidazol
biphenyl
hydroxymethyl
methylsulfonyl
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
AU2010254082A
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English (en)
Other versions
AU2010254082A1 (en
Inventor
Venkataiah Bollu
Brett B. Busch
Ellen K. Kick
Richard Martin
Raju Mohan
William C. Stevens Jr.
Haiying Zhang
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Exelixis Inc
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Exelixis Inc
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.)
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Publication date
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43223342&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AU2010254082(B2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Exelixis Inc filed Critical Exelixis Inc
Publication of AU2010254082A1 publication Critical patent/AU2010254082A1/en
Application granted granted Critical
Publication of AU2010254082B2 publication Critical patent/AU2010254082B2/en
Assigned to EXELIXIS PATENT COMPANY LLC reassignment EXELIXIS PATENT COMPANY LLC Request for Assignment Assignors: BRISTOL-MYERS SQUIBB COMPANY, EXELIXIS PATENT COMPANY LLC
Assigned to EXELIXIS, INC. reassignment EXELIXIS, INC. Request for Assignment Assignors: EXELIXIS PATENT COMPANY LLC
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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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
    • A61K31/4151,2-Diazoles
    • 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
    • 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
    • A61P17/00Drugs for dermatological disorders
    • A61P17/16Emollients or protectives, e.g. against radiation
    • 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
    • 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
    • A61P27/00Drugs for disorders of the senses
    • 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
    • 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
    • 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
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • 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
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/12Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14The ring being saturated

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Toxicology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
AU2010254082A 2009-05-28 2010-05-26 LXR modulators Ceased AU2010254082B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US18173609P 2009-05-28 2009-05-28
US61/181,736 2009-05-28
PCT/US2010/036211 WO2010138598A2 (en) 2009-05-28 2010-05-26 Lxr modulators

Publications (2)

Publication Number Publication Date
AU2010254082A1 AU2010254082A1 (en) 2011-12-08
AU2010254082B2 true AU2010254082B2 (en) 2015-01-29

Family

ID=43223342

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2010254082A Ceased AU2010254082B2 (en) 2009-05-28 2010-05-26 LXR modulators

Country Status (31)

Country Link
US (4) US8618154B2 (enExample)
EP (1) EP2435410B1 (enExample)
JP (1) JP5625050B2 (enExample)
KR (1) KR101676704B1 (enExample)
CN (1) CN102648184B (enExample)
AR (1) AR078049A1 (enExample)
AU (1) AU2010254082B2 (enExample)
BR (1) BRPI1013259B8 (enExample)
CA (1) CA2761934C (enExample)
CL (1) CL2011002972A1 (enExample)
CO (1) CO6470826A2 (enExample)
CY (1) CY1119407T1 (enExample)
DK (1) DK2435410T3 (enExample)
EA (1) EA019960B1 (enExample)
ES (1) ES2620451T3 (enExample)
HR (1) HRP20170194T1 (enExample)
IL (1) IL216176A (enExample)
LT (1) LT2435410T (enExample)
MX (1) MX2011012559A (enExample)
MY (1) MY153958A (enExample)
NZ (1) NZ596330A (enExample)
PE (1) PE20120797A1 (enExample)
PL (1) PL2435410T3 (enExample)
PT (1) PT2435410T (enExample)
SG (1) SG176247A1 (enExample)
SI (1) SI2435410T1 (enExample)
SM (1) SMT201700253T1 (enExample)
TN (1) TN2011000585A1 (enExample)
TW (1) TWI488844B (enExample)
WO (1) WO2010138598A2 (enExample)
ZA (1) ZA201108181B (enExample)

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DK2435410T3 (da) * 2009-05-28 2017-04-10 Exelixis Patent Co Llc LXR-modulatorer
AR088728A1 (es) 2011-03-25 2014-07-02 Bristol Myers Squibb Co Moduladores de lxr como prodroga de imidazol
HUE040231T2 (hu) 2012-03-02 2019-02-28 Ralexar Therapeutics Inc Máj X receptor (LXR) modulátorok bõrbetegségek, rendellenességek és állapotok kezelésére
EP3626309B1 (en) 2012-08-13 2023-03-08 The Rockefeller University Lxrbeta agonist for the treatment of cancer
ES2694001T3 (es) 2013-03-15 2018-12-17 Bristol-Myers Squibb Company Moduladores de LXR
WO2014144037A1 (en) * 2013-03-15 2014-09-18 Bristol-Myers Squibb Company Lxr modulators
US9981913B2 (en) 2013-09-04 2018-05-29 Ralexar Therapeutics, Inc. Liver X receptor (LXR) modulators
CN110003108A (zh) 2013-09-04 2019-07-12 瑞雷克萨治疗公司 肝脏x受体(lxr)调节剂
WO2015106164A1 (en) 2014-01-10 2015-07-16 Rgenix, Inc. Lxr agonists and uses thereof
KR101815734B1 (ko) 2015-05-29 2018-01-05 가톨릭대학교 산학협력단 miR-7, miR-18a 또는 miR-18b를 유효성분으로 포함하는 대사성 질환의 예방 또는 치료용 약학적 조성물
CA3010883A1 (en) 2016-01-11 2017-07-20 The Rockefeller University Methods for the treatment of myeloid derived suppressor cells related disorders
AU2018373028A1 (en) 2017-11-21 2020-04-30 Inspirna, Inc. Polymorphs and uses thereof
EP3999055A1 (en) 2019-07-15 2022-05-25 Novartis AG Methods for treating meibomian gland dysfunction with liver x receptor agonists
CN110305141B (zh) * 2019-07-18 2022-01-11 深圳市三启药物开发有限公司 一种螺(3,3’-异丙基吡咯烷氧化吲哚)类肝x受体调节剂及其制备方法和应用
WO2021119397A1 (en) 2019-12-13 2021-06-17 Rgenix, Inc. Metal salts and uses thereof
CN115656401B (zh) * 2022-11-09 2025-03-28 武汉海特生物创新医药研究有限公司 一种咪唑-4-甲酸乙酯纯度的hplc检测方法

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Also Published As

Publication number Publication date
ES2620451T3 (es) 2017-06-28
TWI488844B (zh) 2015-06-21
LT2435410T (lt) 2017-04-10
WO2010138598A3 (en) 2011-07-28
DK2435410T3 (da) 2017-04-10
CO6470826A2 (es) 2012-06-29
JP2012528180A (ja) 2012-11-12
PE20120797A1 (es) 2012-07-08
EA019960B1 (ru) 2014-07-30
AU2010254082A1 (en) 2011-12-08
CA2761934C (en) 2018-01-09
CL2011002972A1 (es) 2012-08-17
PL2435410T3 (pl) 2017-07-31
WO2010138598A2 (en) 2010-12-02
CY1119407T1 (el) 2018-03-07
IL216176A (en) 2015-10-29
JP5625050B2 (ja) 2014-11-12
ZA201108181B (en) 2013-01-30
PT2435410T (pt) 2017-05-03
US20140163081A1 (en) 2014-06-12
MX2011012559A (es) 2012-06-08
KR20120047868A (ko) 2012-05-14
CA2761934A1 (en) 2010-12-02
US20120071534A1 (en) 2012-03-22
SG176247A1 (en) 2012-01-30
TW201109308A (en) 2011-03-16
NZ596330A (en) 2013-07-26
BRPI1013259B8 (pt) 2021-05-25
EA201171488A1 (ru) 2012-07-30
US20160280661A1 (en) 2016-09-29
BRPI1013259B1 (pt) 2021-04-13
SI2435410T1 (sl) 2017-06-30
EP2435410B1 (en) 2017-01-18
US8618154B2 (en) 2013-12-31
HRP20170194T1 (hr) 2017-05-19
EP2435410A2 (en) 2012-04-04
IL216176A0 (en) 2012-01-31
MY153958A (en) 2015-04-30
CN102648184A (zh) 2012-08-22
US20150299136A1 (en) 2015-10-22
TN2011000585A1 (en) 2013-05-24
KR101676704B1 (ko) 2016-11-16
CN102648184B (zh) 2015-09-30
AR078049A1 (es) 2011-10-12
SMT201700253T1 (it) 2017-07-18
BRPI1013259A2 (pt) 2016-04-05

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