AR069304A1 - Inhibidores del transportador equilibrativo de nucleosidos ent1 - Google Patents
Inhibidores del transportador equilibrativo de nucleosidos ent1Info
- Publication number
- AR069304A1 AR069304A1 ARP080104950A ARP080104950A AR069304A1 AR 069304 A1 AR069304 A1 AR 069304A1 AR P080104950 A ARP080104950 A AR P080104950A AR P080104950 A ARP080104950 A AR P080104950A AR 069304 A1 AR069304 A1 AR 069304A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- hydrogen
- halo
- alkylcarbonyl
- alkyloxy
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/10—Spiro-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- 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
- A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
- 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
-
- 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
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Dermatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Cardiology (AREA)
- Pain & Pain Management (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Anesthesiology (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La presente está relacionada con nuevos compuestos de formula (1) que tienen propiedades inhibitorias del transportador equilibrativo de nucleosidos ENT1, composiciones farmacéuticas que comprenden estos compuestos, procesos químicos para preparar estos compuestos y su utilizacion en el tratamiento de enfermedades vinculadas con la inhibicion de los receptores ENT1, como por ejemplo dolor agudo y cronico. Reivindicacion 1: El compuesto de formula (1) incluyendo cualquier forma estereoquímicamente isomérica del mismo, en donde -A-B- representa los grupos de formulas (2) a (7) en donde n es un entero 0 o 1; R13 representa hidroxi o halo; R14 representa hidrogeno o alquilo C1-6; en los radicales bivalentes (5), (6) y (7) cualquiera de los átomos de hidrogeno en el mismo átomo de carbono o en uno distinto, puede reemplazarse con halo; R1 y R2 se seleccionan cada uno independientemente de hidrogeno, halo o alquilo C1-6; R3, R4, R5 y R6 se seleccionan cada uno independientemente de hidrogeno, halo, alquilo C1-6, polihaloalquilo C1-6, cicloalquilo C3-6, NO2, Ciclo1, Ciclo2, o X-R8 en donde X representa O o NR9 en donde R9 es hidrogeno, alquilo C1-6 o alquiloxi C1-6-alquilo C1-6, y en donde R8 es hidrogeno, alquilo C1-6, alquenilo C2-6, cicloalquilo C3-6, polihaloalquilo C1-6, alquiloxi C1-6-carbonilo, alquilo C1-6-carbonilo, polihaloalquilo C1-6-carbonilo, Ciclo2, -(C=O)-(CH2)m-Ciclo2, -(C=O)-(CH2)m-CH2-OH, -(C=O)-(CH2)m-CH2-O-alquilo C1-4 o alquilo C1-6 sustituido con halo, hidroxi, ciano, cicloalquilo C3-6, alquiloxi C1-6, aminocarbonilo, fenilo, Ciclo1, o Ciclo2, o NR11R12 en donde R11 y R12 se seleccionan cada uno independientemente de hidrogeno, alquilo C1-6, alquilo C1-6-carbonilo, o alquiloxi C1-6-carbonilo; m es un entero 0, 1 o 2; Ciclo1 se selecciona del grupo de formulas (8) en donde R10 es hidrogeno, alquilo C1-6, alquilo C1-6-carbonilo, o alquiloxi C1-6-carbonilo; y Ciclo2 se selecciona del grupo de formulas (9), en donde R10 es hidrogeno, alquilo C1-6, alquilo C1-6-carbonilo, alquiloxi C1-6-carbonilo o alquiloxi C1-6-carbonilo sustituido con halo o hidroxi; o una sal de adicion de ácido de los mismos, o un solvato de los mismos, o una forma N-oxido de los mismos farmacéuticamente aceptables.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP07120630 | 2007-11-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR069304A1 true AR069304A1 (es) | 2010-01-13 |
Family
ID=39145373
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080104950A AR069304A1 (es) | 2007-11-14 | 2008-11-13 | Inhibidores del transportador equilibrativo de nucleosidos ent1 |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US8263592B2 (es) |
| EP (1) | EP2209790B1 (es) |
| JP (1) | JP5369108B2 (es) |
| KR (1) | KR101598136B1 (es) |
| CN (1) | CN101855224B (es) |
| AR (1) | AR069304A1 (es) |
| AU (1) | AU2008322960B2 (es) |
| BR (1) | BRPI0820642B1 (es) |
| CA (1) | CA2704423C (es) |
| CL (1) | CL2008003383A1 (es) |
| EA (1) | EA017215B1 (es) |
| ES (1) | ES2569511T3 (es) |
| HK (1) | HK1146722A1 (es) |
| IL (1) | IL205710A (es) |
| JO (1) | JO3126B1 (es) |
| PA (1) | PA8803401A1 (es) |
| TW (1) | TWI437000B (es) |
| WO (1) | WO2009062990A2 (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201101959D0 (en) | 2011-02-04 | 2011-03-23 | Univ Nottingham | Novel ether linked compoundsand improved treatments for cardiac and cardiovascular disease |
| PE20161476A1 (es) | 2014-06-26 | 2017-01-07 | Hoffmann La Roche | Derivados de indolin-2-ona o pirrolo-piridin-2-ona |
| CN108349942B (zh) | 2015-11-06 | 2021-03-30 | 豪夫迈·罗氏有限公司 | 用于治疗cns和相关疾病的二氢吲哚-2-酮衍生物 |
| JP6857662B2 (ja) | 2015-11-06 | 2021-04-14 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | インドリン−２−オン誘導体 |
| EP3371174B1 (en) * | 2015-11-06 | 2021-03-17 | H. Hoffnabb-La Roche Ag | Indolin-2-one derivatives |
| CN105802999B (zh) * | 2016-04-01 | 2019-05-03 | 中南大学湘雅医院 | 一种膜蛋白ENTs跨膜转运ODNs的试剂盒及方法 |
| JP6879677B2 (ja) | 2016-05-26 | 2021-06-02 | 株式会社クボタ | 作業車 |
| TW201817726A (zh) | 2016-11-14 | 2018-05-16 | 大陸商江蘇恆瑞醫藥股份有限公司 | ３，４－二吡啶基吡唑類衍生物、其製備方法及其在醫藥上的應用 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE9701396D0 (sv) * | 1997-04-15 | 1997-04-15 | Astra Pharma Prod | Compounds |
| GB0003397D0 (en) * | 2000-02-14 | 2000-04-05 | Merck Sharp & Dohme | Therapeutic agents |
| WO2004060902A2 (en) | 2002-12-31 | 2004-07-22 | John K Buolamwini | Novel nucleoside transport inhibitors |
| JPWO2004101593A1 (ja) * | 2003-05-16 | 2006-07-13 | キッセイ薬品工業株式会社 | ５’−修飾ヌクレオシド誘導体及びその医薬用途 |
| EP1698635B1 (en) * | 2003-12-26 | 2011-12-14 | Kissei Pharmaceutical Co., Ltd. | Benzimidazole derivatives and medical uses thereof |
| US8083773B2 (en) * | 2005-07-15 | 2011-12-27 | Muhammad Abubakar Atiq Durrani | Apparatus for minimally invasive posterior correction of spinal deformity |
| AR057570A1 (es) * | 2005-11-14 | 2007-12-05 | Solvay Pharm Gmbh | Derivados de n-sulfamoil-n'-benzopiranopiperidinas espirocondensadas, composiciones farmaceuticas que los comprenden, un procedimiento para su preparacion y su uso en la preparacion de medicamentos para el tratamiento de enfermedades mediadas por las isoenzimas anhidrasas carbonicas subtipos ii y/o |
| US7576207B2 (en) * | 2006-04-06 | 2009-08-18 | Adolor Corporation | Spirocyclic heterocyclic derivatives and methods of their use |
-
2008
- 2008-10-07 JO JOP/2008/0435A patent/JO3126B1/ar active
- 2008-11-07 PA PA20088803401A patent/PA8803401A1/es unknown
- 2008-11-13 KR KR1020107011152A patent/KR101598136B1/ko active IP Right Grant
- 2008-11-13 WO PCT/EP2008/065438 patent/WO2009062990A2/en active Application Filing
- 2008-11-13 AU AU2008322960A patent/AU2008322960B2/en not_active Ceased
- 2008-11-13 CA CA2704423A patent/CA2704423C/en active Active
- 2008-11-13 EP EP08849500.7A patent/EP2209790B1/en active Active
- 2008-11-13 CL CL2008003383A patent/CL2008003383A1/es unknown
- 2008-11-13 AR ARP080104950A patent/AR069304A1/es active IP Right Grant
- 2008-11-13 CN CN2008801159592A patent/CN101855224B/zh not_active Expired - Fee Related
- 2008-11-13 BR BRPI0820642-2A patent/BRPI0820642B1/pt not_active IP Right Cessation
- 2008-11-13 ES ES08849500.7T patent/ES2569511T3/es active Active
- 2008-11-13 EA EA201070599A patent/EA017215B1/ru not_active IP Right Cessation
- 2008-11-13 US US12/742,807 patent/US8263592B2/en active Active
- 2008-11-13 TW TW097143772A patent/TWI437000B/zh not_active IP Right Cessation
- 2008-11-13 JP JP2010533574A patent/JP5369108B2/ja not_active Expired - Fee Related
-
2010
- 2010-05-12 IL IL205710A patent/IL205710A/en active IP Right Grant
-
2011
- 2011-01-26 HK HK11100813.2A patent/HK1146722A1/xx not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| TWI437000B (zh) | 2014-05-11 |
| CL2008003383A1 (es) | 2010-02-05 |
| US8263592B2 (en) | 2012-09-11 |
| EP2209790A2 (en) | 2010-07-28 |
| JP5369108B2 (ja) | 2013-12-18 |
| PA8803401A1 (es) | 2009-06-23 |
| US20100280025A1 (en) | 2010-11-04 |
| AU2008322960B2 (en) | 2013-02-07 |
| EA201070599A1 (ru) | 2010-12-30 |
| KR20100089088A (ko) | 2010-08-11 |
| EA017215B1 (ru) | 2012-10-30 |
| BRPI0820642A2 (pt) | 2020-08-11 |
| AU2008322960A1 (en) | 2009-05-22 |
| CA2704423C (en) | 2017-01-10 |
| WO2009062990A2 (en) | 2009-05-22 |
| EP2209790B1 (en) | 2016-02-17 |
| KR101598136B1 (ko) | 2016-02-29 |
| JO3126B1 (ar) | 2017-09-20 |
| JP2011503147A (ja) | 2011-01-27 |
| ES2569511T3 (es) | 2016-05-11 |
| HK1146722A1 (en) | 2011-07-08 |
| CA2704423A1 (en) | 2009-05-22 |
| CN101855224A (zh) | 2010-10-06 |
| TW200936593A (en) | 2009-09-01 |
| WO2009062990A3 (en) | 2009-09-24 |
| BRPI0820642B1 (pt) | 2021-05-25 |
| CN101855224B (zh) | 2012-11-28 |
| IL205710A (en) | 2013-07-31 |
| IL205710A0 (en) | 2010-11-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration |