EA201171488A1 - Lxr модуляторы - Google Patents

Lxr модуляторы

Info

Publication number
EA201171488A1
EA201171488A1 EA201171488A EA201171488A EA201171488A1 EA 201171488 A1 EA201171488 A1 EA 201171488A1 EA 201171488 A EA201171488 A EA 201171488A EA 201171488 A EA201171488 A EA 201171488A EA 201171488 A1 EA201171488 A1 EA 201171488A1
Authority
EA
Eurasian Patent Office
Prior art keywords
compounds
lxr modulators
lxr
modulators
prodrugs
Prior art date
Application number
EA201171488A
Other languages
English (en)
Other versions
EA019960B1 (ru
Inventor
Бретт Б. Буш
Уилльям К. мл. Стивенс
Эллен К. Кик
Хайин Чжан
Венкатаях Боллу
Ричард Мартин
Раджу Мохан
Original Assignee
ЭКСЕЛИКСИС ПАТЕНТ КОМПАНИ ЭлЭлСи
Бристоль-Мейерз Сквибб Компани
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
Family has litigation
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=EA201171488(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by ЭКСЕЛИКСИС ПАТЕНТ КОМПАНИ ЭлЭлСи, Бристоль-Мейерз Сквибб Компани filed Critical ЭКСЕЛИКСИС ПАТЕНТ КОМПАНИ ЭлЭлСи
Publication of EA201171488A1 publication Critical patent/EA201171488A1/ru
Publication of EA019960B1 publication Critical patent/EA019960B1/ru

Links

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

Abstract

Представлены соединения, их фармацевтически приемлемые соли, изомеры или пролекарства изобретения, которые полезны в качестве модуляторов активности Х рецепторов (LXR) печени. Также предоставлены фармацевтические композиции, содержащие соединения и способы использования соединений.
EA201171488A 2009-05-28 2010-05-26 Lxr модуляторы EA019960B1 (ru)

Applications Claiming Priority (2)

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

Publications (2)

Publication Number Publication Date
EA201171488A1 true EA201171488A1 (ru) 2012-07-30
EA019960B1 EA019960B1 (ru) 2014-07-30

Family

ID=43223342

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201171488A EA019960B1 (ru) 2009-05-28 2010-05-26 Lxr модуляторы

Country Status (30)

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

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LT2435410T (lt) * 2009-05-28 2017-04-10 Exelixis Patent Company Llc Lxr moduliatoriai
AR088728A1 (es) 2011-03-25 2014-07-02 Bristol Myers Squibb Co Moduladores de lxr como prodroga de imidazol
CA2866113C (en) 2012-03-02 2020-05-12 Alexar Therapeutics, Inc. Pyrazolyl derivatives as liver x receptor (lxr) modulators for the treatment of dermal diseases, disorders and conditions
EP2882496B1 (en) 2012-08-13 2019-10-09 The Rockefeller University Treatment and diagnosis of melanoma
WO2014144037A1 (en) * 2013-03-15 2014-09-18 Bristol-Myers Squibb Company Lxr modulators
WO2014152738A1 (en) 2013-03-15 2014-09-25 Bristol-Myers Squibb Company Lxr modulators
US9981913B2 (en) 2013-09-04 2018-05-29 Ralexar Therapeutics, Inc. Liver X receptor (LXR) modulators
BR112016004904B1 (pt) 2013-09-04 2023-01-24 Ellora Therapeutics, Inc. Compostos moduladores de receptor x do fígado (lxr), seu uso e composição farmaceutica compreendendo os mesmos
AU2015204572B2 (en) 2014-01-10 2020-07-30 Inspirna, 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
JP7025022B2 (ja) 2016-01-11 2022-02-24 ザ ロックフェラー ユニバーシティー 骨髄系由来抑制細胞関連障害の治療のための方法
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CN114126618A (zh) 2019-07-15 2022-03-01 诺华股份有限公司 用肝脏x受体激动剂治疗睑板腺功能障碍的方法
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

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LT2435410T (lt) * 2009-05-28 2017-04-10 Exelixis Patent Company Llc Lxr moduliatoriai

Also Published As

Publication number Publication date
EP2435410B1 (en) 2017-01-18
CO6470826A2 (es) 2012-06-29
US8618154B2 (en) 2013-12-31
US20140163081A1 (en) 2014-06-12
JP2012528180A (ja) 2012-11-12
DK2435410T3 (da) 2017-04-10
CA2761934A1 (en) 2010-12-02
HRP20170194T1 (hr) 2017-05-19
SG176247A1 (en) 2012-01-30
BRPI1013259B1 (pt) 2021-04-13
MY153958A (en) 2015-04-30
AR078049A1 (es) 2011-10-12
US20160280661A1 (en) 2016-09-29
CN102648184A (zh) 2012-08-22
WO2010138598A3 (en) 2011-07-28
SI2435410T1 (sl) 2017-06-30
PT2435410T (pt) 2017-05-03
JP5625050B2 (ja) 2014-11-12
KR20120047868A (ko) 2012-05-14
ZA201108181B (en) 2013-01-30
PL2435410T3 (pl) 2017-07-31
BRPI1013259A2 (pt) 2016-04-05
EP2435410A2 (en) 2012-04-04
IL216176A (en) 2015-10-29
LT2435410T (lt) 2017-04-10
TWI488844B (zh) 2015-06-21
CN102648184B (zh) 2015-09-30
NZ596330A (en) 2013-07-26
KR101676704B1 (ko) 2016-11-16
IL216176A0 (en) 2012-01-31
CY1119407T1 (el) 2018-03-07
TN2011000585A1 (en) 2013-05-24
US20120071534A1 (en) 2012-03-22
AU2010254082B2 (en) 2015-01-29
US20150299136A1 (en) 2015-10-22
CA2761934C (en) 2018-01-09
ES2620451T3 (es) 2017-06-28
EA019960B1 (ru) 2014-07-30
BRPI1013259B8 (pt) 2021-05-25
CL2011002972A1 (es) 2012-08-17
TW201109308A (en) 2011-03-16
WO2010138598A2 (en) 2010-12-02
AU2010254082A1 (en) 2011-12-08
PE20120797A1 (es) 2012-07-08
MX2011012559A (es) 2012-06-08

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