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)
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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
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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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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic 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
    • C07D233/64—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic 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
    • A61K31/415—1,2-Diazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic 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
    • A61K31/4164—1,3-Diazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/16—Emollients or protectives, e.g. against radiation
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Urology & Nephrology (AREA)
  • Toxicology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Vascular Medicine (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 (https=)
EP (1) EP2435410B1 (https=)
JP (1) JP5625050B2 (https=)
KR (1) KR101676704B1 (https=)
CN (1) CN102648184B (https=)
AR (1) AR078049A1 (https=)
AU (1) AU2010254082B2 (https=)
BR (1) BRPI1013259B8 (https=)
CA (1) CA2761934C (https=)
CL (1) CL2011002972A1 (https=)
CO (1) CO6470826A2 (https=)
CY (1) CY1119407T1 (https=)
DK (1) DK2435410T3 (https=)
EA (1) EA019960B1 (https=)
ES (1) ES2620451T3 (https=)
HR (1) HRP20170194T1 (https=)
IL (1) IL216176A (https=)
LT (1) LT2435410T (https=)
MX (1) MX2011012559A (https=)
MY (1) MY153958A (https=)
NZ (1) NZ596330A (https=)
PE (1) PE20120797A1 (https=)
PL (1) PL2435410T3 (https=)
PT (1) PT2435410T (https=)
SG (1) SG176247A1 (https=)
SI (1) SI2435410T1 (https=)
SM (1) SMT201700253T1 (https=)
TN (1) TN2011000585A1 (https=)
TW (1) TWI488844B (https=)
WO (1) WO2010138598A2 (https=)
ZA (1) ZA201108181B (https=)

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KR101676704B1 (ko) * 2009-05-28 2016-11-16 엑셀리시스 페이턴트 컴퍼니 엘엘씨 Ｌｘｒ 조절자
AR088728A1 (es) * 2011-03-25 2014-07-02 Bristol Myers Squibb Co Moduladores de lxr como prodroga de imidazol
SG10201607345YA (en) 2012-03-02 2016-11-29 Ralexar Therapeutics Inc Liver x receptor (lxr) modulators for the treatment of dermal diseases, disorders and conditions
AU2013302861A1 (en) 2012-08-13 2015-03-05 The Rockefeller University Treatment and diagnosis of melanoma
JP6456909B2 (ja) 2013-03-15 2019-01-23 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
CN105209039B (zh) * 2013-03-15 2018-06-22 百时美施贵宝公司 Lxr调节剂
RS60479B1 (sr) 2013-09-04 2020-08-31 Ellora Therapeutics Inc Modulatori receptora x jetre (lxr)
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
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
EP3402477A4 (en) 2016-01-11 2019-08-21 The Rockefeller University METHOD FOR THE TREATMENT OF DISEASES RELATED TO MYELOID-DERIVED SUPPRESSOR CELLS
CA3078981A1 (en) 2017-11-21 2019-05-31 Rgenix, 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
TWI888447B (zh) 2019-12-13 2025-07-01 美商因思博納公司 金屬鹽及其用途
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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KR101676704B1 (ko) * 2009-05-28 2016-11-16 엑셀리시스 페이턴트 컴퍼니 엘엘씨 Ｌｘｒ 조절자

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Also Published As

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

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