AR045721A1 - Derivados de pirrol 2,5 diona como moduladores de receptores hormonales de higado - Google Patents
Derivados de pirrol 2,5 diona como moduladores de receptores hormonales de higadoInfo
- Publication number
- AR045721A1 AR045721A1 ARP040102419A ARP040102419A AR045721A1 AR 045721 A1 AR045721 A1 AR 045721A1 AR P040102419 A ARP040102419 A AR P040102419A AR P040102419 A ARP040102419 A AR P040102419A AR 045721 A1 AR045721 A1 AR 045721A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- phenyl
- optionally substituted
- group
- fluoro
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- 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
- 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
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/44—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/44—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members
- C07D207/444—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5
- C07D207/456—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5 with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurology (AREA)
- Hospice & Palliative Care (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Vascular Medicine (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole Compounds (AREA)
Abstract
Reivindicación 1: Un compuesto caracterizado porque responde a la fórmula 1 donde R1 se selecciona entre fenil (C1-4)alquilo donde el fenilo se sustituye por (C1-4)alcoxicarbonilo o un grupo de fórmula NRaRb donde Ra y Rb independientemente representan H o ( C1-4)alquilo; hereoaril (C1-4) alquilo donde el heteroarilom opcionalmente se sustituye por (C1-4alquilo o un grupo de fórmula NRaRb donde Ra y Rb independientemente representan H o (C1-4)alquilo; o un grupo (C1-4)alquilo el cual se sustituye por uno o más de los siguientes: Fluoro, (C1-4) alcoxicarbonilo, (C1-3)alquiltio o (C1-3)alcoxi opcionalmetne sustituido por uno o más fluoro; R2 es fenilo, R3 se selecciona entre fenilo, indolilo o benzofuranilo, cada uno opcionalmente sustituido por uno o más de los siguientes: (C1-3) alcanoilo, (C1-3)alcoxi opcionalmente sustituido por uno o más fluoro; (C1-3)alquiltio; o un grupo de fórmula NRaRb donde Ra y Rb independientemente representan H, (C1-3) alquilo o (C1-3)alcanoilo o Ra y Rb junto con el átomo de nitrógneo al cual se encuentran unidos representan morfolino, o una sal o solvato aceptable para uso farmacéutico de los mismos, o un solvato de dicha sal. Procesos para preparar tales compuestos, su utilidad en la modulación de receptores de hormonas nucleares de hígado (LXR) (NR1H3) y/o (NR1H2) y para el tratamiento o prevención de estados clínicos que incluyen enfermedades cardiovasculares tales como aterosclerosis, enfermedades inflamatorias, enfermedad de alzheimer, trastornos lipídicos ( dislipidemias) asociados o no con la resistencia a la insulina. diabetes de tipo 2 y otras manifestaciones del síndrome metabólico, métodos para su utilización terapéutica y composiciones farmacéuticas que los contienen.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0316232.8A GB0316232D0 (en) | 2003-07-11 | 2003-07-11 | Therapeutic agents |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR045721A1 true AR045721A1 (es) | 2005-11-09 |
Family
ID=27741983
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040102419A AR045721A1 (es) | 2003-07-11 | 2004-07-08 | Derivados de pirrol 2,5 diona como moduladores de receptores hormonales de higado |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US7432288B2 (es) |
| EP (1) | EP1646626B1 (es) |
| JP (1) | JP2007521312A (es) |
| KR (1) | KR20060035748A (es) |
| CN (1) | CN1823061A (es) |
| AR (1) | AR045721A1 (es) |
| AT (1) | ATE399777T1 (es) |
| AU (1) | AU2004255999B2 (es) |
| BR (1) | BRPI0412472A (es) |
| CA (1) | CA2532056A1 (es) |
| DE (1) | DE602004014773D1 (es) |
| ES (1) | ES2308204T3 (es) |
| GB (1) | GB0316232D0 (es) |
| HK (1) | HK1088320A1 (es) |
| IL (1) | IL172760A0 (es) |
| IS (1) | IS8293A (es) |
| MX (1) | MXPA06000414A (es) |
| MY (1) | MY135821A (es) |
| NO (1) | NO20060081L (es) |
| RU (1) | RU2006102130A (es) |
| SA (1) | SA04250204B1 (es) |
| TW (1) | TW200503691A (es) |
| UA (1) | UA82109C2 (es) |
| UY (1) | UY28408A1 (es) |
| WO (1) | WO2005005417A1 (es) |
| ZA (1) | ZA200600222B (es) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE513823T1 (de) * | 2004-08-17 | 2011-07-15 | Simpson Biotech Co Ltd | Mischung und verbindungen von mycelien von antrodia camphorata und deren verwendung |
| US7505238B2 (en) * | 2005-01-07 | 2009-03-17 | Agnes Neves Woo | ESD configuration for low parasitic capacitance I/O |
| US7582629B2 (en) | 2005-01-10 | 2009-09-01 | Astrazeneca Ab | Derivatives of isothiazol-3(2H)-one 1,1-dioxides as liver X receptor modulators |
| SE0500055D0 (sv) | 2005-01-10 | 2005-01-10 | Astrazeneca Ab | Therapeutic agents 3 |
| MX2008013477A (es) * | 2006-04-28 | 2008-10-29 | Esteve Labor Dr | Compuestos biciclicos de tetrahidropirrol. |
| AU2007286807B2 (en) | 2006-08-21 | 2013-03-21 | Genentech, Inc. | Aza-benzothiophenyl compounds and methods of use |
| CN101456863B (zh) * | 2007-12-14 | 2012-04-25 | 华北制药集团新药研究开发有限责任公司 | Lxr激动剂及其制备方法和用途 |
| EP2307364B1 (en) | 2008-07-01 | 2013-06-19 | Genentech, Inc. | Isoindolone derivatives as mek kinase inhibitors and methods of use |
| BRPI0910175A2 (pt) | 2008-07-01 | 2017-03-21 | Genentech Inc | composto de fórmula i e ii, composição farmacêutica, método de inibição do crescimento de células anormais ou de tratamento de um distúrbio hiperproliferativo em um mamífero e método de tratamento de uma doença inflamatória em um mamífero |
| KR101901741B1 (ko) | 2010-09-07 | 2018-10-01 | 서울대학교산학협력단 | 세스터터핀 화합물 및 이들 물질의 용도 |
| JP2014500264A (ja) | 2010-12-03 | 2014-01-09 | アラーガン インコーポレイテッド | スフィンゴシン−１−リン酸（ｓ１ｐ）受容体モジュレーターとしての新規オキシム誘導体 |
| JP2013544837A (ja) | 2010-12-03 | 2013-12-19 | アラーガン インコーポレイテッド | スフィンゴシン−１−リン酸（ｓ１ｐ）受容体モジュレーターとしての新規オキシムアゼチジン誘導体 |
| CA2939120A1 (en) | 2014-01-10 | 2015-07-16 | Rgenix, Inc. | Lxr agonists and uses thereof |
| WO2017123568A2 (en) | 2016-01-11 | 2017-07-20 | The Rockefeller University | Methods for the treatment of myeloid derived suppressor cells related disorders |
| WO2019104062A1 (en) | 2017-11-21 | 2019-05-31 | Rgenix, Inc. | Polymorphs and uses thereof |
| AU2020401286A1 (en) | 2019-12-13 | 2022-06-23 | Inspirna, Inc. | Metal salts and uses thereof |
| US11753374B2 (en) * | 2020-11-18 | 2023-09-12 | Southern Reserach Institute | Compounds for the treatment of acute and chronic kidney disease |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1120414A1 (en) | 1998-07-30 | 2001-08-01 | Japan Tobacco Inc. | Disubstituted maleimide compounds and medicinal utilization thereof |
| WO2000021927A2 (en) | 1998-10-08 | 2000-04-20 | Smithkline Beecham Plc | Pyrrole-2,5-diones as gsk-3 inhibitors |
| WO2001003705A1 (en) | 1999-07-08 | 2001-01-18 | Tularik Inc. | Compositions and methods for raising hdl cholesterol levels |
| AU6593600A (en) | 1999-08-20 | 2001-03-19 | Rei Asakai | Drugs inhibiting cell death |
| GB0008264D0 (en) | 2000-04-04 | 2000-05-24 | Smithkline Beecham Plc | Novel method and compounds |
-
2003
- 2003-07-11 GB GBGB0316232.8A patent/GB0316232D0/en not_active Ceased
-
2004
- 2004-06-29 TW TW093119064A patent/TW200503691A/zh unknown
- 2004-07-05 SA SA4250204A patent/SA04250204B1/ar unknown
- 2004-07-08 AU AU2004255999A patent/AU2004255999B2/en not_active Ceased
- 2004-07-08 JP JP2006520138A patent/JP2007521312A/ja not_active Withdrawn
- 2004-07-08 AT AT04749150T patent/ATE399777T1/de not_active IP Right Cessation
- 2004-07-08 RU RU2006102130/04A patent/RU2006102130A/ru not_active Application Discontinuation
- 2004-07-08 ES ES04749150T patent/ES2308204T3/es active Active
- 2004-07-08 EP EP04749150A patent/EP1646626B1/en active Active
- 2004-07-08 CA CA002532056A patent/CA2532056A1/en not_active Abandoned
- 2004-07-08 WO PCT/SE2004/001114 patent/WO2005005417A1/en active IP Right Grant
- 2004-07-08 DE DE602004014773T patent/DE602004014773D1/de not_active Expired - Fee Related
- 2004-07-08 AR ARP040102419A patent/AR045721A1/es not_active Application Discontinuation
- 2004-07-08 MX MXPA06000414A patent/MXPA06000414A/es not_active Application Discontinuation
- 2004-07-08 US US10/564,235 patent/US7432288B2/en not_active Expired - Fee Related
- 2004-07-08 BR BRPI0412472-3A patent/BRPI0412472A/pt not_active IP Right Cessation
- 2004-07-08 CN CNA2004800198411A patent/CN1823061A/zh active Pending
- 2004-07-08 KR KR1020067000712A patent/KR20060035748A/ko not_active Application Discontinuation
- 2004-07-09 MY MYPI20042745A patent/MY135821A/en unknown
- 2004-07-09 UY UY28408A patent/UY28408A1/es unknown
- 2004-08-07 UA UAA200600272A patent/UA82109C2/uk unknown
-
2005
- 2005-12-22 IL IL172760A patent/IL172760A0/en unknown
-
2006
- 2006-01-05 NO NO20060081A patent/NO20060081L/no not_active Application Discontinuation
- 2006-01-10 ZA ZA200600222A patent/ZA200600222B/en unknown
- 2006-02-09 IS IS8293A patent/IS8293A/is unknown
- 2006-08-08 HK HK06108803.4A patent/HK1088320A1/xx not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| ZA200600222B (en) | 2007-04-25 |
| EP1646626A1 (en) | 2006-04-19 |
| IS8293A (is) | 2006-02-09 |
| HK1088320A1 (en) | 2006-11-03 |
| NO20060081L (no) | 2006-02-08 |
| UA82109C2 (uk) | 2008-03-11 |
| BRPI0412472A (pt) | 2006-09-19 |
| WO2005005417A1 (en) | 2005-01-20 |
| UY28408A1 (es) | 2005-02-28 |
| ATE399777T1 (de) | 2008-07-15 |
| EP1646626B1 (en) | 2008-07-02 |
| GB0316232D0 (en) | 2003-08-13 |
| JP2007521312A (ja) | 2007-08-02 |
| DE602004014773D1 (de) | 2008-08-14 |
| SA04250204B1 (ar) | 2008-03-23 |
| CN1823061A (zh) | 2006-08-23 |
| MY135821A (en) | 2008-07-31 |
| US20060235015A1 (en) | 2006-10-19 |
| AU2004255999B2 (en) | 2007-08-02 |
| RU2006102130A (ru) | 2007-08-20 |
| US7432288B2 (en) | 2008-10-07 |
| ES2308204T3 (es) | 2008-12-01 |
| MXPA06000414A (es) | 2006-03-17 |
| IL172760A0 (en) | 2006-04-10 |
| CA2532056A1 (en) | 2005-01-20 |
| KR20060035748A (ko) | 2006-04-26 |
| TW200503691A (en) | 2005-02-01 |
| AU2004255999A1 (en) | 2005-01-20 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |