PE20061426A1 - Derivados de indol como inhibidores de la fosfolipasa a2 citosolica - Google Patents
Derivados de indol como inhibidores de la fosfolipasa a2 citosolicaInfo
- Publication number
- PE20061426A1 PE20061426A1 PE2006000559A PE2006000559A PE20061426A1 PE 20061426 A1 PE20061426 A1 PE 20061426A1 PE 2006000559 A PE2006000559 A PE 2006000559A PE 2006000559 A PE2006000559 A PE 2006000559A PE 20061426 A1 PE20061426 A1 PE 20061426A1
- Authority
- PE
- Peru
- Prior art keywords
- inhibitors
- indol
- chloro
- ethyl
- amino
- Prior art date
Links
- 102100037611 Lysophospholipase Human genes 0.000 title abstract 3
- 108020002496 Lysophospholipase Proteins 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title abstract 3
- -1 BENZYLOXY Chemical class 0.000 abstract 5
- 150000001875 compounds Chemical class 0.000 abstract 3
- CZZYITDELCSZES-UHFFFAOYSA-N diphenylmethane Chemical class C=1C=CC=CC=1CC1=CC=CC=C1 CZZYITDELCSZES-UHFFFAOYSA-N 0.000 abstract 3
- 239000005711 Benzoic acid Substances 0.000 abstract 2
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 abstract 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N Benzoic acid Natural products OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 abstract 1
- 102000003658 Group IV Phospholipases A2 Human genes 0.000 abstract 1
- 108010082107 Group IV Phospholipases A2 Proteins 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 108010064785 Phospholipases Proteins 0.000 abstract 1
- 102000015439 Phospholipases Human genes 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 235000010233 benzoic acid Nutrition 0.000 abstract 1
- 230000001086 cytosolic effect Effects 0.000 abstract 1
- QUPDWYMUPZLYJZ-UHFFFAOYSA-N ethyl Chemical compound C[CH2] QUPDWYMUPZLYJZ-UHFFFAOYSA-N 0.000 abstract 1
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 abstract 1
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
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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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pulmonology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Vascular Medicine (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Cardiology (AREA)
- Obesity (AREA)
- Heart & Thoracic Surgery (AREA)
- Immunology (AREA)
- Psychology (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Enzymes And Modification Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Indole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
REFERIDA A UN COMPUESTO DERIVADO DE INDOL DE FORMULA (I), DONDE n1 ES 1 O 2; n2 ES 1 O 2; n3 ES 1 O 2; n5 ES 0, 1 O 2; X2 ES UN ENLACE, O, CH2, SO2; R5 ES H O ALQUILO C1-C3; R6 ES H O ALQUILO C1-C6; R7 ES OH, BENCILOXI, CH3, CF3, ENTRE OTROS; R8 ES H, OH, NO2, CF3, OCF3, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: ACIDO 4-{2-[2-[2-({[2-(BENCILOXI)BENCIL]-SULFONIL}AMINO)ETIL]-5-CLORO-1-(DIFENIL-METIL)-1H-INDOL-3-IL]-ETOXI}BENZOICO, ACIDO 4-{2-[5-CLORO-1-(DIFENILMETIL)-2-(2-{[(2-HIDROXIBENCIL)SULFONIL]AMINO}ETIL)-1H-INDOL-3-IL]ETOXI}-BENZOICO, ACIDO 4-{2-[5--CLORO-2-(2-{[(2,6-DIBROMO-BENCIL)SULFONIL]AMINO}ETIL)-1-(DIFENILMETIL)-1H-INDOL-3-IL]-ETOXI}BENZOICO, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LAS FOSFOLIPASAS, PARTICULARMENTE, FOSFOLIPASA A2 CITOSOLICA (cPLA2), Y MAS PARTICULARMENTE DE LA ENZIMA FOSFOLIPASA A2 ALFA CITOSOLICA Y SON UTILES EN EL TRATAMIENTO DE LA INFLAMACION, DOLOR, ASMA, INFARTO, ENTRE OTROS
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US68556405P | 2005-05-27 | 2005-05-27 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20061426A1 true PE20061426A1 (es) | 2007-01-24 |
Family
ID=37188759
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2006000559A PE20061426A1 (es) | 2005-05-27 | 2006-05-26 | Derivados de indol como inhibidores de la fosfolipasa a2 citosolica |
Country Status (32)
| Country | Link |
|---|---|
| US (3) | US7557135B2 (es) |
| EP (2) | EP2248801A1 (es) |
| JP (1) | JP5116666B2 (es) |
| KR (1) | KR101353982B1 (es) |
| CN (2) | CN101184729B (es) |
| AR (1) | AR054195A1 (es) |
| AT (1) | ATE489364T1 (es) |
| AU (1) | AU2006251946B2 (es) |
| BR (1) | BRPI0610049A2 (es) |
| CA (1) | CA2607857C (es) |
| CR (1) | CR9520A (es) |
| CY (1) | CY1111151T1 (es) |
| DE (1) | DE602006018451D1 (es) |
| DK (1) | DK1891006T3 (es) |
| ES (1) | ES2354908T3 (es) |
| GT (1) | GT200600228A (es) |
| HN (1) | HN2006019513A (es) |
| IL (1) | IL186912A (es) |
| MX (1) | MX2007014589A (es) |
| MY (1) | MY144672A (es) |
| NI (1) | NI200700287A (es) |
| NO (1) | NO20075627L (es) |
| NZ (1) | NZ563736A (es) |
| PE (1) | PE20061426A1 (es) |
| PL (1) | PL1891006T3 (es) |
| PT (1) | PT1891006E (es) |
| RU (1) | RU2433997C2 (es) |
| SI (1) | SI1891006T1 (es) |
| SV (1) | SV2008002551A (es) |
| TW (1) | TW200718687A (es) |
| UA (1) | UA91053C2 (es) |
| WO (1) | WO2006128142A2 (es) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8283373B2 (en) | 2005-05-27 | 2012-10-09 | Pfizer Inc. | Inhibitors of cytosolic phospholipase A2 |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7605156B2 (en) | 2001-12-03 | 2009-10-20 | Wyeth | Methods for the use of inhibitors of cytosolic phospholipase A2 |
| US7713964B2 (en) | 2001-12-03 | 2010-05-11 | Wyeth Llc | Methods for treating asthmatic conditions |
| HN2004000536A (es) * | 2003-12-16 | 2009-02-18 | Wyeth Corp | Un procediemiento de sintesis para la alquilacion reductiva de la posicon c-3 de indoles |
| IL161579A0 (en) | 2004-04-22 | 2004-09-27 | Mor Research Applic Ltd | ANTISENSE OLIGONUCLEOTIDES AGAINST cPLA2, COMPOSITIONS AND USES THEREOF |
| US8029815B2 (en) | 2004-04-28 | 2011-10-04 | Elford Howard L | Methods for treating or preventing restenosis and other vascular proliferative disorders |
| US20080009485A1 (en) * | 2006-05-26 | 2008-01-10 | Wyeth | Methods for the use of inhibitors of cytosolic phospholipase A2 in the treatment of thrombosis |
| IL178401A (en) * | 2006-09-28 | 2012-04-30 | Univ Ben Gurion | Use of antisense oligonucleotides against 2 cPLA in the treatment of cancer |
| BRPI0717943A2 (pt) * | 2006-10-31 | 2013-10-29 | Wyeth Corp | Composição farmacêutica; forma de dosagem farmacêutica; processo para a preparação de uma composição farmacêutica; e produto preparado pelo processo |
| WO2008055148A2 (en) * | 2006-10-31 | 2008-05-08 | Wyeth | Semi-solid formulations of phospholipase enzyme inhibitors |
| EP2141148B1 (en) | 2007-03-29 | 2013-07-03 | Daiichi Sankyo Company, Limited | Indole derivative having cpla2 inhibitory activity, use of the same and method for producing the same |
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| KR101931628B1 (ko) * | 2010-06-18 | 2019-03-13 | 화이트헤드 인스티튜트 포 바이오메디칼 리서치 | 항바이러스 화합물에 대한 타켓인 pla2g16 |
| US20130209403A1 (en) | 2010-09-08 | 2013-08-15 | Ruprecht-Karls-Universitaet | Use of inhibitors of phospholipase a2 for the treatment or prevention of flavivirus infection |
| GB201401904D0 (en) | 2014-02-04 | 2014-03-19 | Ziarco Pharma Ltd | Pharmaceutical composition for topical administration |
| US9815768B2 (en) | 2014-02-28 | 2017-11-14 | Sumitomo Chemical Company, Limited | Method for producing 2-(halogenomethyl)-3-methylnitrobenzene |
| CN103804150A (zh) * | 2014-03-01 | 2014-05-21 | 江苏斯威森生物医药工程研究中心有限公司 | 一种3,4-二甲氧基苄基溴的制备方法 |
| CN108017522B (zh) * | 2017-11-16 | 2021-01-05 | 贵州大学 | 一种2,6-二溴苯甲磺酰氯的制备工艺 |
| WO2020236777A1 (en) * | 2019-05-20 | 2020-11-26 | Saint Louis University | Reprogramming of lipid metabolism to inhibit t cell senescence and enhance tumor immunotherapy |
| TWI770527B (zh) | 2019-06-14 | 2022-07-11 | 美商基利科學股份有限公司 | Cot 調節劑及其使用方法 |
| EP4126231A1 (en) | 2020-03-30 | 2023-02-08 | Gilead Sciences, Inc. | Solid forms of (s)-6-(((1-(bicyclo[1.1.1]pentan-1-yl)-1h-1,2,3-triazol-4-yl)2-methyl-1-oxo-1,2- dihydroisoquinolin-5-yl)methyl)))amino)8-chloro-(neopentylamino)quinoline-3-carb onitrile a cot inhibitor compound |
| CN115397824B (zh) | 2020-04-02 | 2024-10-22 | 吉利德科学公司 | 用于制备cot抑制剂化合物的方法 |
| WO2022031931A2 (en) * | 2020-08-06 | 2022-02-10 | The Children's Medical Center Corporation | Compositions for altering a microglial cell, and methods of use therefore |
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| TW200718687A (en) | 2005-05-27 | 2007-05-16 | Wyeth Corp | Inhibitors of cytosolic phospholipase A2 |
| US20080009485A1 (en) | 2006-05-26 | 2008-01-10 | Wyeth | Methods for the use of inhibitors of cytosolic phospholipase A2 in the treatment of thrombosis |
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2006
- 2006-05-25 TW TW095118534A patent/TW200718687A/zh unknown
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- 2006-05-26 PL PL06771540T patent/PL1891006T3/pl unknown
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- 2006-05-26 SI SI200630865T patent/SI1891006T1/sl unknown
- 2006-05-26 PE PE2006000559A patent/PE20061426A1/es not_active Application Discontinuation
- 2006-05-26 EP EP10172388A patent/EP2248801A1/en not_active Withdrawn
- 2006-05-26 DE DE602006018451T patent/DE602006018451D1/de active Active
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- 2006-05-26 CN CN2006800186466A patent/CN101184729B/zh not_active Expired - Fee Related
- 2006-05-26 CA CA2607857A patent/CA2607857C/en active Active
- 2006-05-26 US US11/442,199 patent/US7557135B2/en active Active
- 2006-05-26 WO PCT/US2006/020847 patent/WO2006128142A2/en not_active Ceased
- 2006-05-26 MY MYPI20062443A patent/MY144672A/en unknown
- 2006-05-26 NZ NZ563736A patent/NZ563736A/en not_active IP Right Cessation
- 2006-05-26 KR KR1020077027672A patent/KR101353982B1/ko not_active Expired - Fee Related
- 2006-05-26 JP JP2008513819A patent/JP5116666B2/ja not_active Expired - Fee Related
- 2006-05-26 UA UAA200713220A patent/UA91053C2/ru unknown
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- 2006-05-26 AU AU2006251946A patent/AU2006251946B2/en not_active Ceased
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- 2006-05-26 RU RU2007140910/04A patent/RU2433997C2/ru not_active IP Right Cessation
- 2006-05-26 CN CN2010105355308A patent/CN102040550B/zh not_active Expired - Fee Related
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2009
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8283373B2 (en) | 2005-05-27 | 2012-10-09 | Pfizer Inc. | Inhibitors of cytosolic phospholipase A2 |
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