PE20120797A1 - Derivados de 1-[(3'-fluoro-4'-hidroximetil-5'-metilsulfonil)bifenil-4-il]-2-bencil-4-[(1-hidroxi-1-metil)etil]-1h-imidazol como moduladores de lxr - Google Patents
Derivados de 1-[(3'-fluoro-4'-hidroximetil-5'-metilsulfonil)bifenil-4-il]-2-bencil-4-[(1-hidroxi-1-metil)etil]-1h-imidazol como moduladores de lxrInfo
- Publication number
- PE20120797A1 PE20120797A1 PE2011002005A PE2011002005A PE20120797A1 PE 20120797 A1 PE20120797 A1 PE 20120797A1 PE 2011002005 A PE2011002005 A PE 2011002005A PE 2011002005 A PE2011002005 A PE 2011002005A PE 20120797 A1 PE20120797 A1 PE 20120797A1
- Authority
- PE
- Peru
- Prior art keywords
- hydroximethyl
- biphenyl
- propan
- methylsulfonyl
- fluoro
- Prior art date
Links
- QUPDWYMUPZLYJZ-UHFFFAOYSA-N ethyl Chemical compound C[CH2] QUPDWYMUPZLYJZ-UHFFFAOYSA-N 0.000 title abstract 2
- -1 METHYLSULFONYL Chemical class 0.000 abstract 9
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 2
- 102000004311 liver X receptors Human genes 0.000 abstract 2
- 108090000865 liver X receptors Proteins 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 201000001320 Atherosclerosis Diseases 0.000 abstract 1
- 208000032928 Dyslipidaemia Diseases 0.000 abstract 1
- 208000017170 Lipid metabolism disease Diseases 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
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- 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
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- 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
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- A—HUMAN NECESSITIES
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- A61P17/16—Emollients or protectives, e.g. against radiation
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- 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
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- 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
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- 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)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Biomedical Technology (AREA)
- Dermatology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Immunology (AREA)
- Heart & Thoracic Surgery (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Emergency Medicine (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Child & Adolescent Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Ophthalmology & Optometry (AREA)
- Toxicology (AREA)
- Vascular Medicine (AREA)
- Physical Education & Sports Medicine (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
SE REFIERE A COMPUESTOS MODULADORES DE LA ACTIVIDAD DE RECEPTORES X DEL HIGADO (LXR) TALES COMO: 2-(1-(3-CLORO-3'-FLUORO-4'-(HIDROXIMETIL)-5'-(METILSULFONIL)BIFENIL-4-IL)-2-(2-(2,6-DICLOROFENIL)PROPAN-2-IL)-1H-IMIDAZOL-4-IL)PROPAN-2-OL; 2-(2-(2-(2-CLORO-3-FLUOROFENIL)PROPAN-2-IL)-1-(3'-FLUORO-4'-(HIDROXIMETIL)-5'-(METILSULFONIL)BIFENIL-4-IL)-1H-IMIDAZOL-4-IL)PROPAN-2-OL; 2-(2-(2-(2,6-DICLOROFENIL)PROPAN-2-IL)-1-(3'-FLUORO-4'-(HIDROXIMETIL)-5'-(METILSULFONIL)BIFENIL-4-IL)-1H-IMIDAZOL-4-IL)PROPAN-2-OL; 2-(2-(2-(2,6-DICLOROFENIL)PROPAN-2-IL)-1-(3,3'-DIFLUORO-4'-(HIDROXIMETIL)-5'-(METILSULFONIL)BIFENIL-4-IL)-1H-IMIDAZOL-4-IL)PROPAN-2-OL; 2-{2-[1-(2,6-DICLOROFENIL)ETIL]-1-[3,3'-DIFLUORO-4'-(HIDROXIMETIL)-5'-(METILSULFONIL)BIFENIL-4-IL]-1H-IMIDAZOL-4-IL}PROPAN-2-OL; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON UTILES EN EL TRATAMIENTO DE ATEROSCLEROSIS, DIABETES, DISLIPIDEMIA, ENFERMEDAD DE ALZHEIMER
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US18173609P | 2009-05-28 | 2009-05-28 |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20120797A1 true PE20120797A1 (es) | 2012-07-08 |
Family
ID=43223342
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2011002005A PE20120797A1 (es) | 2009-05-28 | 2010-05-26 | Derivados de 1-[(3'-fluoro-4'-hidroximetil-5'-metilsulfonil)bifenil-4-il]-2-bencil-4-[(1-hidroxi-1-metil)etil]-1h-imidazol como moduladores de lxr |
Country Status (31)
Country | Link |
---|---|
US (4) | US8618154B2 (es) |
EP (1) | EP2435410B1 (es) |
JP (1) | JP5625050B2 (es) |
KR (1) | KR101676704B1 (es) |
CN (1) | CN102648184B (es) |
AR (1) | AR078049A1 (es) |
AU (1) | AU2010254082B2 (es) |
BR (1) | BRPI1013259B8 (es) |
CA (1) | CA2761934C (es) |
CL (1) | CL2011002972A1 (es) |
CO (1) | CO6470826A2 (es) |
CY (1) | CY1119407T1 (es) |
DK (1) | DK2435410T3 (es) |
EA (1) | EA019960B1 (es) |
ES (1) | ES2620451T3 (es) |
HR (1) | HRP20170194T1 (es) |
IL (1) | IL216176A (es) |
LT (1) | LT2435410T (es) |
MX (1) | MX2011012559A (es) |
MY (1) | MY153958A (es) |
NZ (1) | NZ596330A (es) |
PE (1) | PE20120797A1 (es) |
PL (1) | PL2435410T3 (es) |
PT (1) | PT2435410T (es) |
SG (1) | SG176247A1 (es) |
SI (1) | SI2435410T1 (es) |
SM (1) | SMT201700253T1 (es) |
TN (1) | TN2011000585A1 (es) |
TW (1) | TWI488844B (es) |
WO (1) | WO2010138598A2 (es) |
ZA (1) | ZA201108181B (es) |
Families Citing this family (16)
Publication number | Priority date | Publication date | Assignee | Title |
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LT2435410T (lt) * | 2009-05-28 | 2017-04-10 | Exelixis Patent Company Llc | Lxr moduliatoriai |
TW201242953A (en) | 2011-03-25 | 2012-11-01 | Bristol Myers Squibb Co | Imidazole prodrug LXR modulators |
HRP20181623T1 (hr) | 2012-03-02 | 2018-12-14 | Ralexar Therapeutics, Inc. | Modulatori x receptora jetre (lxr) za liječenje bolesti, poremećaja i stanja kože |
EP4218935A1 (en) | 2012-08-13 | 2023-08-02 | The Rockefeller University | Lxrbeta agonist for the treatment of cancer |
WO2014144037A1 (en) * | 2013-03-15 | 2014-09-18 | Bristol-Myers Squibb Company | Lxr modulators |
CN105188380B (zh) | 2013-03-15 | 2017-08-15 | 百时美施贵宝公司 | Lxr调节剂 |
SG11201601644RA (en) | 2013-09-04 | 2016-04-28 | Alexar Therapeutics Inc | Liver x receptor (lxr) modulators |
HUE051094T2 (hu) | 2013-09-04 | 2021-03-01 | Ellora Therapeutics Inc | Liver X receptor (LXR) módosítók |
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 |
AU2017207291B2 (en) | 2016-01-11 | 2023-06-15 | The Rockefeller University | Methods for the treatment of myeloid derived suppressor cells related disorders |
EP3713575A4 (en) | 2017-11-21 | 2021-08-25 | Rgenix, Inc. | POLYMORPHS AND THEIR USES |
WO2021009664A1 (en) | 2019-07-15 | 2021-01-21 | 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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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 |
DK149080C (da) | 1980-06-06 | 1986-07-28 | Sankyo Co | Fremgangsmaade til fremstilling af derivater af ml-236b-carboxylsyre |
WO1984002131A1 (en) | 1982-11-22 | 1984-06-07 | Sandoz Ag | Analogs of mevalolactone and derivatives thereof, processes for their production, pharmaceutical compositions containing them and their use as pharmaceuticals |
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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 |
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BR9806989A (pt) | 1997-01-24 | 2000-03-14 | Univ California | Processo para tratar a epiderme ou membrana da mucosa de um indivìduo mamìfero. |
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US7482366B2 (en) * | 2001-12-21 | 2009-01-27 | X-Ceptor Therapeutics, Inc. | Modulators of LXR |
AU2003263814A1 (en) * | 2002-07-26 | 2004-02-16 | Bayer Pharmaceuticals Corporation | Indane, dihydrobenzofuran, and tetrahydronaphthalene carboxylic acid derivatives and their use as antidiabetics |
US7109227B2 (en) * | 2002-08-26 | 2006-09-19 | National Health Research Institutes | Imidazolamino compounds |
EP1638943B1 (fr) * | 2003-05-27 | 2008-08-06 | Société de Conseils de Recherches et d'Applications Scientifiques ( S.C.R.A.S.) | NOUVEAUX DERIVES D’IMIDAZOLES, LEUR PREPARATION ET LEUR UTILISATION EN TANT QUE MEDICAMENT |
JP5095216B2 (ja) * | 2003-11-14 | 2012-12-12 | ローラス セラピューティクス インコーポレーテッド | アリールイミダゾールおよびその抗癌剤としての使用 |
CN1918155B (zh) * | 2004-02-11 | 2010-05-26 | Irm责任有限公司 | 作为lxr调节剂的化合物和组合物 |
EP1910307A1 (en) * | 2005-06-27 | 2008-04-16 | Exelixis, Inc. | Pyrazole based lxr modulators |
CN101248048B (zh) * | 2005-06-27 | 2013-08-28 | 埃克塞利希斯专利有限责任公司 | 吡唑基lxr调节剂 |
EP2121621B1 (en) * | 2006-12-08 | 2014-05-07 | Exelixis Patent Company LLC | Lxr and fxr modulators |
LT2435410T (lt) * | 2009-05-28 | 2017-04-10 | Exelixis Patent Company Llc | Lxr moduliatoriai |
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2010
- 2010-05-26 LT LTEP10721902.4T patent/LT2435410T/lt unknown
- 2010-05-26 CA CA2761934A patent/CA2761934C/en active Active
- 2010-05-26 NZ NZ596330A patent/NZ596330A/xx unknown
- 2010-05-26 SM SM20170253T patent/SMT201700253T1/it unknown
- 2010-05-26 PL PL10721902T patent/PL2435410T3/pl unknown
- 2010-05-26 SI SI201031427A patent/SI2435410T1/sl unknown
- 2010-05-26 EP EP10721902.4A patent/EP2435410B1/en active Active
- 2010-05-26 MX MX2011012559A patent/MX2011012559A/es active IP Right Grant
- 2010-05-26 HR HRP20170194TT patent/HRP20170194T1/hr unknown
- 2010-05-26 JP JP2012513215A patent/JP5625050B2/ja not_active Expired - Fee Related
- 2010-05-26 MY MYPI2011006278A patent/MY153958A/en unknown
- 2010-05-26 BR BRPI1013259A patent/BRPI1013259B8/pt not_active IP Right Cessation
- 2010-05-26 PT PT107219024T patent/PT2435410T/pt unknown
- 2010-05-26 PE PE2011002005A patent/PE20120797A1/es active IP Right Grant
- 2010-05-26 AU AU2010254082A patent/AU2010254082B2/en not_active Ceased
- 2010-05-26 DK DK10721902.4T patent/DK2435410T3/da active
- 2010-05-26 WO PCT/US2010/036211 patent/WO2010138598A2/en active Application Filing
- 2010-05-26 CN CN201080033601.2A patent/CN102648184B/zh not_active Expired - Fee Related
- 2010-05-26 SG SG2011087459A patent/SG176247A1/en unknown
- 2010-05-26 US US13/319,937 patent/US8618154B2/en active Active
- 2010-05-26 KR KR1020117031397A patent/KR101676704B1/ko active Active
- 2010-05-26 ES ES10721902.4T patent/ES2620451T3/es active Active
- 2010-05-26 EA EA201171488A patent/EA019960B1/ru not_active IP Right Cessation
- 2010-05-28 TW TW099117252A patent/TWI488844B/zh not_active IP Right Cessation
- 2010-05-28 AR ARP100101870A patent/AR078049A1/es not_active Application Discontinuation
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2011
- 2011-11-07 IL IL216176A patent/IL216176A/en active IP Right Grant
- 2011-11-08 ZA ZA2011/08181A patent/ZA201108181B/en unknown
- 2011-11-16 TN TNP2011000585A patent/TN2011000585A1/en unknown
- 2011-11-24 CL CL2011002972A patent/CL2011002972A1/es unknown
- 2011-11-25 CO CO11161736A patent/CO6470826A2/es active IP Right Grant
-
2013
- 2013-11-21 US US14/085,926 patent/US20140163081A1/en not_active Abandoned
-
2015
- 2015-05-04 US US14/703,247 patent/US20150299136A1/en not_active Abandoned
-
2016
- 2016-06-07 US US15/175,425 patent/US20160280661A1/en not_active Abandoned
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2017
- 2017-04-05 CY CY20171100403T patent/CY1119407T1/el unknown
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