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)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (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)
- Epidemiology (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Neurosurgery (AREA)
- Immunology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Dermatology (AREA)
- Cardiology (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Ophthalmology & Optometry (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Child & Adolescent Psychology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (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 (enExample) |
| EP (1) | EP2688871B1 (enExample) |
| JP (1) | JP2014510110A (enExample) |
| CN (1) | CN103443082B (enExample) |
| AR (1) | AR088728A1 (enExample) |
| ES (1) | ES2548050T3 (enExample) |
| TW (1) | TW201242953A (enExample) |
| WO (1) | WO2012135082A1 (enExample) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG11201405378VA (en) | 2012-03-02 | 2014-09-26 | Anayaderm Inc | Liver x receptor (lxr) modulators for the treatment of dermal diseases, disorders and conditions |
| WO2014028461A2 (en) | 2012-08-13 | 2014-02-20 | The Rockefeller University | Treatment and diagnosis of melanoma |
| JP6442475B2 (ja) * | 2013-03-15 | 2018-12-19 | 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 |
| EP3041835B1 (en) | 2013-09-04 | 2020-04-08 | Ellora Therapeutics, Inc. | Liver x receptor (lxr) modulators |
| KR20160048997A (ko) | 2013-09-04 | 2016-05-04 | 알렉사르 테라퓨틱스 인코퍼레이티드 | 간 x 수용체 (lxr) 조절인자 |
| AU2015204572B2 (en) | 2014-01-10 | 2020-07-30 | Inspirna, Inc. | LXR agonists and uses thereof |
| ES2885432T3 (es) | 2014-10-03 | 2021-12-13 | Ucb Biopharma Sprl | Derivados de imidazol pentacíclicos condensados |
| AU2017207291B2 (en) | 2016-01-11 | 2023-06-15 | The Rockefeller University | Methods for the treatment of myeloid derived suppressor cells related disorders |
| CA3019245A1 (en) | 2016-04-01 | 2017-10-05 | Ucb Biopharma Sprl | Fused pentacyclic imidazole derivatives as modulators of tnf activity |
| WO2017167993A1 (en) | 2016-04-01 | 2017-10-05 | Ucb Biopharma Sprl | Fused pentacyclic imidazole derivatives as modulators of tnf activity |
| CN109219609B (zh) | 2016-04-01 | 2022-02-01 | Ucb生物制药私人有限公司 | 作为tnf活性调节剂的稠合六环咪唑衍生物 |
| WO2017167996A1 (en) | 2016-04-01 | 2017-10-05 | Ucb Biopharma Sprl | Fused pentacyclic imidazole derivatives as modulators of tnf activity |
| SG11201808625QA (en) | 2016-04-04 | 2018-10-30 | 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 |
| EP3713575A4 (en) | 2017-11-21 | 2021-08-25 | Rgenix, Inc. | POLYMORPHS AND THEIR USES |
| JP7689964B2 (ja) | 2019-12-13 | 2025-06-09 | インスピルナ，インコーポレーテッド | 金属塩及びその使用 |
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 |
| MX7065E (es) | 1980-06-06 | 1987-04-10 | Sankyo Co | Un procedimiento microbiologico para preparar derivados de ml-236b |
| US5354772A (en) | 1982-11-22 | 1994-10-11 | Sandoz Pharm. Corp. | Indole analogs of mevalonolactone and derivatives thereof |
| HU204253B (en) | 1982-11-22 | 1991-12-30 | Sandoz Ag | Process for producing mevalonolactone analogues and derivatives and pharmaceutical compositions containing them |
| 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 |
| ATE215601T1 (de) | 1991-09-17 | 2002-04-15 | Salk Inst For Biological Studi | Rezeptoren der steroid/thyroid superfamilie von rezeptoren |
| EP1019059A4 (en) | 1997-01-24 | 2004-01-14 | Univ California | USE OF FXR, PPAR-ALPHA AND LXR-ALPHA ACTIVATORS TO RESTORE THE BARRIER FUNCTION, TO PROMOTE EPIDERMIS DIFFERENTIATION, AND TO PROLIFERATE |
| US5767134A (en) * | 1997-05-15 | 1998-06-16 | Vion Pharmaceuticals, Inc. | Prodrug forms of ribonucleotide reductase inhibitors 3-AP and 3-AMP |
| AU5994199A (en) | 1998-09-23 | 2000-04-10 | Alexander Mata De Urquiza | Analysis of ligand activated nuclear receptors (in vivo) |
| ES2326850T3 (es) | 1998-12-23 | 2009-10-20 | Glaxo Group Limited | Ensayos para ligandos de receptores nucleares. |
| 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 |
| ATE274921T1 (de) | 1999-03-26 | 2004-09-15 | Hope City | Verfahren zur selektion von fxr- rezeptormodulatoren |
| EP1190065A2 (en) | 1999-06-18 | 2002-03-27 | Cv Therapeutics, Inc. | Atp binding cassette transporter protein abc1 polypeptides |
| EP1212065A4 (en) | 1999-07-08 | 2004-02-11 | Tularik Inc | COMPILATIONS AND METHODS FOR INCREASING THE HDL CHOLESTEROL LEVEL |
| AU2000235960A1 (en) | 2000-02-14 | 2001-08-27 | Tularik, Inc. | Lxr modulators |
| AU2001262984A1 (en) | 2000-05-03 | 2001-11-12 | 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 |
| KR101363278B1 (ko) * | 2005-06-27 | 2014-02-21 | 엑셀리시스 페이턴트 컴퍼니 엘엘씨 | 이미다졸계 ｌｘｒ 변조제 |
| SG162803A1 (en) * | 2005-06-27 | 2010-07-29 | Exelixis Inc | Imidazole based lxr modulators |
| EP2121621B1 (en) * | 2006-12-08 | 2014-05-07 | Exelixis Patent Company LLC | Lxr and fxr modulators |
| WO2008107878A1 (en) * | 2007-03-05 | 2008-09-12 | Yissum Research Development Company Of The Hebrew University Of Jerusalem | Novel quinonoid derivatives of cannabinoids and their use in the treatment of malignancies |
| MY153958A (en) | 2009-05-28 | 2015-04-30 | Exelixis Patent Co Llc | Lxr modulators |
-
2012
- 2012-03-23 TW TW101110267A patent/TW201242953A/zh unknown
- 2012-03-23 AR ARP120100996A patent/AR088728A1/es not_active Application Discontinuation
- 2012-03-26 CN CN201280014836.6A patent/CN103443082B/zh not_active Expired - Fee Related
- 2012-03-26 ES ES12711739.8T patent/ES2548050T3/es active Active
- 2012-03-26 JP JP2014501296A patent/JP2014510110A/ja active Pending
- 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 |
|---|---|
| EP2688871B1 (en) | 2015-08-26 |
| US8901106B2 (en) | 2014-12-02 |
| CN103443082A (zh) | 2013-12-11 |
| WO2012135082A1 (en) | 2012-10-04 |
| CN103443082B (zh) | 2015-11-25 |
| ES2548050T3 (es) | 2015-10-13 |
| JP2014510110A (ja) | 2014-04-24 |
| US20140018321A1 (en) | 2014-01-16 |
| TW201242953A (en) | 2012-11-01 |
| EP2688871A1 (en) | 2014-01-29 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |