AR088728A1 - Moduladores de lxr como prodroga de imidazol - Google Patents
Moduladores de lxr como prodroga de imidazolInfo
- Publication number
- AR088728A1 AR088728A1 ARP120100996A ARP120100996A AR088728A1 AR 088728 A1 AR088728 A1 AR 088728A1 AR P120100996 A ARP120100996 A AR P120100996A AR P120100996 A ARP120100996 A AR P120100996A AR 088728 A1 AR088728 A1 AR 088728A1
- Authority
- AR
- Argentina
- Prior art keywords
- prodroga
- imidazol
- lxr modulators
- compounds
- pharmaceutically acceptable
- Prior art date
Links
- RAXXELZNTBOGNW-UHFFFAOYSA-N 1H-imidazole Chemical compound C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 150000003839 salts Chemical class 0.000 abstract 2
- 230000000694 effects Effects 0.000 abstract 1
- 230000002440 hepatic effect Effects 0.000 abstract 1
- 125000002883 imidazolyl group Chemical group 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
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
- A61K31/4164—1,3-Diazoles
- A61K31/4174—Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
- 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
- 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
- A61P37/02—Immunomodulators
-
- 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
-
- 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
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/06—Phosphorus compounds without P—C bonds
- C07F9/08—Esters of oxyacids of phosphorus
- C07F9/09—Esters of phosphoric acids
- C07F9/12—Esters of phosphoric acids with hydroxyaryl compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
- C07F9/6503—Five-membered rings
- C07F9/6506—Five-membered rings having the nitrogen atoms in positions 1 and 3
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Immunology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Endocrinology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Child & Adolescent Psychology (AREA)
- Ophthalmology & Optometry (AREA)
- Emergency Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161467404P | 2011-03-25 | 2011-03-25 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR088728A1 true AR088728A1 (es) | 2014-07-02 |
Family
ID=45926934
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120100996A AR088728A1 (es) | 2011-03-25 | 2012-03-23 | Moduladores de lxr como prodroga de imidazol |
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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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 |
| PE20170693A1 (es) | 2014-10-03 | 2017-06-13 | Ucb Biopharma Sprl | Derivados de imidazol pentaciclicos fusionados |
| EP3402477A4 (en) | 2016-01-11 | 2019-08-21 | The Rockefeller University | METHOD FOR THE TREATMENT OF DISEASES RELATED TO MYELOID-DERIVED SUPPRESSOR CELLS |
| JP6968092B2 (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 |
| EA201892144A1 (ru) | 2016-04-01 | 2019-04-30 | Юсб Байофарма Спрл | Конденсированные гексациклические производные имидазола в качестве модуляторов активности tnf |
| EP3436460B1 (en) | 2016-04-01 | 2021-08-18 | UCB Biopharma SRL | Fused pentacyclic imidazole derivatives as modulators of tnf activity |
| JP6968091B2 (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 |
| EP3439658B1 (en) * | 2016-04-04 | 2021-11-24 | ChemoCentryx, Inc. | Soluble c5ar antagonists |
| WO2018167176A1 (en) | 2017-03-15 | 2018-09-20 | Ucb Biopharma Sprl | Fused pentacyclic imidazole derivatives as modulators of tnf activity |
| CA3078981A1 (en) | 2017-11-21 | 2019-05-31 | Rgenix, Inc. | Polymorphs and uses thereof |
| TWI888447B (zh) | 2019-12-13 | 2025-07-01 | 美商因思博納公司 | 金屬鹽及其用途 |
Family Cites Families (27)
| 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 |
| DK149080C (da) | 1980-06-06 | 1986-07-28 | Sankyo Co | Fremgangsmaade til fremstilling af derivater af ml-236b-carboxylsyre |
| 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 |
| CA2115452A1 (en) | 1991-09-17 | 1993-04-01 | Ronald M. Evans | Receptor of the thyroid/steroid hormone receptor superfamily |
| CN1248916A (zh) | 1997-01-24 | 2000-03-29 | 加利福尼亚大学董事会 | FXR、PPARα和LXRα激活剂恢复屏障功能、促进表皮分化和抑制增生的用途 |
| 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 |
| JP2002532729A (ja) | 1998-12-23 | 2002-10-02 | グラクソ グループ リミテッド | 核内受容体のリガンドのアッセイ |
| 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 |
| EP1165135B1 (en) | 1999-03-26 | 2004-09-01 | City of Hope | Methods of screening for compounds modulating fxr receptors |
| CN100513570C (zh) | 1999-06-18 | 2009-07-15 | Cv治疗公司 | 结合框运输蛋白abc1的调节作用 |
| 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 |
| WO2001082917A2 (en) | 2000-05-03 | 2001-11-08 | 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 |
| EP1692127B1 (en) * | 2003-10-08 | 2008-07-02 | Smithkline Beecham Corporation | Triphenylethylene compounds as selective estrogen receptor modulators |
| 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 |
| BRPI0612287A8 (pt) | 2005-06-27 | 2019-01-22 | Exelixis Inc | composição para uso farmacêutico no tratamento de doenças através da medicina nuclear e métodos de uso e para modulação de atividade de receptor nuclear |
| 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 |
-
2012
- 2012-03-23 AR ARP120100996A patent/AR088728A1/es not_active Application Discontinuation
- 2012-03-23 TW TW101110267A patent/TW201242953A/zh unknown
- 2012-03-26 JP JP2014501296A patent/JP2014510110A/ja active Pending
- 2012-03-26 ES ES12711739.8T patent/ES2548050T3/es active Active
- 2012-03-26 CN CN201280014836.6A patent/CN103443082B/zh not_active Expired - Fee Related
- 2012-03-26 EP EP12711739.8A patent/EP2688871B1/en not_active Not-in-force
- 2012-03-26 US US14/006,980 patent/US8901106B2/en active Active
- 2012-03-26 WO PCT/US2012/030499 patent/WO2012135082A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| CN103443082B (zh) | 2015-11-25 |
| ES2548050T3 (es) | 2015-10-13 |
| WO2012135082A1 (en) | 2012-10-04 |
| TW201242953A (en) | 2012-11-01 |
| US8901106B2 (en) | 2014-12-02 |
| EP2688871A1 (en) | 2014-01-29 |
| EP2688871B1 (en) | 2015-08-26 |
| JP2014510110A (ja) | 2014-04-24 |
| CN103443082A (zh) | 2013-12-11 |
| US20140018321A1 (en) | 2014-01-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |