AR043673A1 - Compuestos heterociclicos inhibidores no nucleosidos de la transcriptasa inversa i, preparacion de los mismos, composiciones farmaceuticas que los contienen y su uso en la preparacion de medicamentos para el tratamiento del sida - Google Patents
Compuestos heterociclicos inhibidores no nucleosidos de la transcriptasa inversa i, preparacion de los mismos, composiciones farmaceuticas que los contienen y su uso en la preparacion de medicamentos para el tratamiento del sidaInfo
- Publication number
- AR043673A1 AR043673A1 ARP040100937A ARP040100937A AR043673A1 AR 043673 A1 AR043673 A1 AR 043673A1 AR P040100937 A ARP040100937 A AR P040100937A AR P040100937 A ARP040100937 A AR P040100937A AR 043673 A1 AR043673 A1 AR 043673A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- alkyl
- preparation
- dialkylamino
- alkylthio
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
- C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
- C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
- C07D271/113—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the 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
- A61K31/41—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
- A61K31/4196—1,2,4-Triazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
- C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles 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 ring carbon atoms
- C07D249/12—Oxygen or sulfur atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
- C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
- C07D285/12—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
- C07D285/125—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
- C07D285/13—Oxygen atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Virology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Communicable Diseases (AREA)
- Epidemiology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Oncology (AREA)
- AIDS & HIV (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Pyridine Compounds (AREA)
Abstract
Métodos para inhibir o modular la transcriptasa inversa del virus de la inmunodeficiencia humana (HIV) con compuestos de la fórmula (1), a composiciones farmacéuticas que contienen un compuesto de la fórmula (1) mezclado por lo menos con un disolvente, vehículo o excipiente y a procesos para obtener compuestos de la fórmula (1). Estos compuestos son útiles para tratar trastornos en los que están implicados virus VIH o virus relacionados genéticamente. Reivindicación 1: Un compuesto de la fórmula (1) en la que: X1 se elige entre el grupo formado por R5O, R5S(O)n, R5CH2, R5CH2O, R5CH2S(O)n, R5OCH2, R5S(O)nCH2 y NR5R6; X2 se elige entre el grupo formado por o-fenileno, 1,2-ciclohexenileno; O, S y NR7; R1 y R2 (i) con independencia entre sí se eligen entre el grupo formado por H, alquilo C1-6, haloalquilo C1-6, cicloalquilo C3-8, alquiltio C1-6, alquilsulfinilo C1-6, alquilalquilsulfonilo C1-6, haloalcoxi C1-6, haloalquiltio C1-6, halógeno, amino, alquilamino, dialquilamino, aminoacilo, nitro y ciano; o (ii) juntos son -CH=CH-CH=CH-; o (iii) junto con los átomos de C a los que están unidos forman un anillo heteroaromático o heterocíclico de 5 o 6 eslabones con uno o dos heteroátomos elegidos con independencia entre sí entre el grupo formado por O, S y NH; R3 y R4 con independencia entre sí se eligen entre el grupo formado por H, alquilo C1-6, haloalquilo C1-6, cicloalquilo C3-8, alcoxi C1-6, alquiltio C1-6, haloalcoxi C1-6, haloalquiltio C1-6, halógeno, amino, alquilamino, dialquilamino, aminoacilo, nitro y ciano; R5 se elige entre el grupo formado por fenilo, naftilo, piridinilo, pirimidinilo, pirazinilo y pirrolilo; en el que dicho grupo fenilo, dicho naftilo, dicho piridinilo, dicho pirimidinilo, dicho pirazinilo y dicho pirrolilo están eventualmente sustituidos de una a tres veces por sustituyentes elegidos con independencia entre si entre el grupo formado por H, alquilo C1-6, haloalquilo C1-6, cicloalquilo C3-8, alcoxi C1-6, alquiltio C1-6, alquilsulfinilo C1-6, alquilalquilsulfonilo C1-6, haloalcoxi C1-6, haloalquiltio C1-6, halógeno, amino, alquilamino, dialquilamino, aminoacilo, acilo, alcoxicarbonilo, carbamoilo, N-alquilcarbonilo, N,N-dialquilcarbamoilo, nitro, y ciano; R6 es H, alquilo C1-6 o acilo; R7 es H, o alquilo C1-6 eventualmente sustituido por uno o dos sustituyentes elegidos con independencia entre si entre el grupo formado por hidroxi, alcoxi, tiol, alquiltio, alquilsulfinilo C1-6, alquilsulfonilo C1-6, halógeno, amino, alquilamino, dialquilamino, aminoalquilo, alquilaminoalquilo y dialquilaminoalquilo; n es un número entero de 0 a 2; e hidratos, solvatos, clatratos y sales de adición de ácido del mismo, con la condición de que si X2 es orto-fenileno, R5 no puede ser fenilo sin sustituir.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US45713003P | 2003-03-24 | 2003-03-24 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR043673A1 true AR043673A1 (es) | 2005-08-03 |
Family
ID=33098199
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040100937A AR043673A1 (es) | 2003-03-24 | 2004-03-22 | Compuestos heterociclicos inhibidores no nucleosidos de la transcriptasa inversa i, preparacion de los mismos, composiciones farmaceuticas que los contienen y su uso en la preparacion de medicamentos para el tratamiento del sida |
Country Status (20)
| Country | Link |
|---|---|
| US (2) | US7208509B2 (es) |
| EP (1) | EP1608633B1 (es) |
| JP (1) | JP4708329B2 (es) |
| KR (1) | KR101122456B1 (es) |
| CN (1) | CN100588650C (es) |
| AR (1) | AR043673A1 (es) |
| AU (1) | AU2004224153B2 (es) |
| BR (2) | BRPI0408767B8 (es) |
| CA (1) | CA2518437C (es) |
| CL (1) | CL2004000590A1 (es) |
| CO (1) | CO5601029A2 (es) |
| ES (1) | ES2574580T3 (es) |
| HR (1) | HRP20050830A2 (es) |
| IL (1) | IL170343A (es) |
| MX (1) | MXPA05010210A (es) |
| NO (1) | NO334095B1 (es) |
| NZ (1) | NZ541829A (es) |
| RU (1) | RU2342367C2 (es) |
| TW (1) | TW200505441A (es) |
| WO (1) | WO2004085411A1 (es) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005097762A2 (en) * | 2004-04-01 | 2005-10-20 | Aventis Pharmaceuticals Inc. | 1,3,4-oxadiazol-2-ones as ppar delta modulators |
| EP1773790B1 (en) | 2004-07-27 | 2012-08-15 | F.Hoffmann-La Roche Ag | Benzyltriazolone compounds as non-nucleoside reverse transcriptase inhibitors |
| US8293778B2 (en) | 2004-07-27 | 2012-10-23 | Roche Palo Alto Llc | Heterocyclic antiviral compounds |
| EP1863777A1 (en) * | 2005-03-24 | 2007-12-12 | F.Hoffmann-La Roche Ag | 1,2,4 -triazole-5-one compounds as heterocyclic reverse transcriptase inhibitors |
| AR057455A1 (es) | 2005-07-22 | 2007-12-05 | Merck & Co Inc | Inhibidores de la transcriptasa reversa de vih y composicion farmaceutica |
| WO2007039463A1 (en) * | 2005-09-30 | 2007-04-12 | F. Hoffmann-La Roche Ag | Nnrt inhibitors |
| CN101291905A (zh) | 2005-10-19 | 2008-10-22 | 弗·哈夫曼-拉罗切有限公司 | 苯乙酰胺nnrt抑制剂 |
| US20080293775A1 (en) * | 2005-12-15 | 2008-11-27 | Astrazeneca Ab | Substituted Diphenylethers, -Amines, -Sulfides and -Methanes for the Treatment of Respiratory Disease |
| AP2985A (en) | 2006-07-07 | 2014-09-30 | Gilead Sciences Inc | Modulators of pharmacokinetic properties of therapeutics |
| CL2007002105A1 (es) * | 2006-07-21 | 2008-02-22 | Hoffmann La Roche | Compuestos derivados de 2-[3-(3-cianofenoxi)(fenoxi o fenilsulfanil)]-n-fenil acetamida, inhibidores de la transcriptasa inversa del vih; procedimiento de preparacion; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar u |
| KR101401811B1 (ko) | 2006-08-16 | 2014-05-29 | 에프. 호프만-라 로슈 아게 | 비-뉴클레오사이드 역전사효소 저해제 |
| TW200831085A (en) * | 2006-12-13 | 2008-08-01 | Merck & Co Inc | Non-nucleoside reverse transcriptase inhibitors |
| ES2602784T3 (es) * | 2007-02-23 | 2017-02-22 | Gilead Sciences, Inc. | Moduladores de las propiedades farmacocinéticas de los agentes terapéuticos |
| KR20100015435A (ko) * | 2007-04-09 | 2010-02-12 | 에프. 호프만-라 로슈 아게 | 비뉴클레오시드 역전사효소 저해제 |
| CA2687770C (en) * | 2007-05-30 | 2016-03-08 | F. Hoffmann-La Roche Ag | Process for preparing triazolones |
| KR101542629B1 (ko) | 2007-05-30 | 2015-08-06 | 에프. 호프만-라 로슈 아게 | 비-뉴클레오사이드 역전사효소 억제제 |
| WO2008157273A1 (en) * | 2007-06-14 | 2008-12-24 | Smithkline Beecham Corporation | Chemical compounds |
| WO2008157330A1 (en) * | 2007-06-14 | 2008-12-24 | Smithkline Beecham Corporation | Chemical compounds |
| KR20100039348A (ko) * | 2007-06-22 | 2010-04-15 | 에프. 호프만-라 로슈 아게 | 비-뉴클레오사이드 역 전사효소 억제제로서 우레아 및 카바메이트 유도체 |
| WO2009005811A1 (en) * | 2007-07-03 | 2009-01-08 | Yale University | Novel azoles and related derivatives as non-nucleoside reverse transcriptase inhibitors (nnrtis) in antiviral therapy (hiv) |
| BRPI0821349A2 (pt) * | 2007-12-21 | 2019-09-24 | Hoffmann La Roche | compostos antivirais heterocíclicos |
| ME02181B (me) * | 2010-03-30 | 2015-10-20 | Merck Canada Inc | Ne-nukleozidni inhibitori reverzne transkriptaze |
| CU23896B1 (es) * | 2010-04-01 | 2013-05-31 | Ct De Ingeniería Genética Y Biotecnología | Método para inhibir la replicación del vih en células de mamíferos |
| JO3470B1 (ar) | 2012-10-08 | 2020-07-05 | Merck Sharp & Dohme | مشتقات 5- فينوكسي-3h-بيريميدين-4-أون واستخدامها كمثبطات ناسخ عكسي ل hiv |
| CN104230929B (zh) * | 2013-06-19 | 2015-11-18 | 华东师范大学 | 一种非核苷类hiv-1反转录酶抑制剂 |
| DK3125894T3 (da) | 2014-04-01 | 2020-11-16 | Merck Sharp & Dohme | Prodrugs af hiv-reverstranscriptasehæmmere |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3274185A (en) | 1963-10-08 | 1966-09-20 | S E Massengill Company | Phthalazine derivatives |
| US3813384A (en) | 1972-01-17 | 1974-05-28 | Asta Werke Ag Chem Fab | Basically substituted benzyl phthalazone derivatives,acid salts thereof and process for the production thereof |
| JP2542880B2 (ja) | 1986-12-19 | 1996-10-09 | メレルダウファーマスーティカルズ インコーポレーテッド | ５−アリ―ル−３ｈ−１，２，４，−トリアゾ―ル−３−オン類の抗痙攣剤としての用途 |
| US5436252A (en) | 1986-12-19 | 1995-07-25 | Merrell Dow Pharmaceuticals Inc. | 5-aryl-3H-1,2,4-triazol-3-ones and their use in the treatment of neurodegenerative disorders |
| JP2593084B2 (ja) | 1986-12-19 | 1997-03-19 | メレルダウファーマスーティカルズ インコーポレーテッド | ５−アリールー３ｈ−１，２，４−トリアゾールー３−オン類の神経変性障害の処置への用途 |
| US4942236A (en) | 1987-09-30 | 1990-07-17 | American Home Products Corporation | 2-aryl substituted pyridyl-containing phenyl sulfonamido compounds as antiallergic and antiinflammatory agents |
| US4826990A (en) | 1987-09-30 | 1989-05-02 | American Home Products Corporation | 2-aryl substituted heterocyclic compounds as antiallergic and antiinflammatory agents |
| US5103014A (en) | 1987-09-30 | 1992-04-07 | American Home Products Corporation | Certain 3,3'-[[[(2-phenyl-4-thiazolyl)methoxy]phenyl]methylene]dithiobis-propanoic acid derivatives |
| US4966909A (en) | 1989-12-20 | 1990-10-30 | Merrell Dow Pharmaceuticals | 4-benzyl-5-phenyl-2,4-dihydro-3H-1,2,4-triazol-3-ones and their use as anticonvulsants |
| US5331002A (en) | 1990-04-19 | 1994-07-19 | Merrell Dow Pharmaceuticals Inc. | 5-aryl-4-alkyl-3H-1,2,4-triazole-3-thiones useful as memory enhancers |
| US5922751A (en) | 1994-06-24 | 1999-07-13 | Euro-Celtique, S.A. | Aryl pyrazole compound for inhibiting phosphodiesterase IV and methods of using same |
| US5641796A (en) | 1994-11-01 | 1997-06-24 | Eli Lilly And Company | Oral hypoglycemic agents |
| JP2000511883A (ja) | 1996-04-19 | 2000-09-12 | ノボ ノルディスク アクティーゼルスカブ | ホスホチロシン認識ユニットを有する分子のモジュレーター |
| TW467902B (en) | 1996-07-31 | 2001-12-11 | Bristol Myers Squibb Co | Diphenyl heterocycles as potassium channel modulators |
| MXPA03003218A (es) * | 2000-10-30 | 2004-12-03 | Kudos Pharm Ltd | Derivados de ftalazinona. |
| UA82048C2 (uk) | 2000-11-10 | 2008-03-11 | Эли Лилли Энд Компани | Агоністи альфа-рецепторів, активованих проліфератором пероксисом |
| JP2002275165A (ja) * | 2001-01-12 | 2002-09-25 | Sumitomo Pharmaceut Co Ltd | トリアゾール誘導体 |
-
2004
- 2004-03-18 TW TW093107292A patent/TW200505441A/zh unknown
- 2004-03-22 BR BRPI0408767A patent/BRPI0408767B8/pt active IP Right Grant
- 2004-03-22 WO PCT/EP2004/002995 patent/WO2004085411A1/en active Application Filing
- 2004-03-22 KR KR1020057017771A patent/KR101122456B1/ko active IP Right Grant
- 2004-03-22 MX MXPA05010210A patent/MXPA05010210A/es active IP Right Grant
- 2004-03-22 CA CA2518437A patent/CA2518437C/en not_active Expired - Lifetime
- 2004-03-22 JP JP2006504792A patent/JP4708329B2/ja not_active Expired - Lifetime
- 2004-03-22 EP EP04722259.1A patent/EP1608633B1/en not_active Expired - Lifetime
- 2004-03-22 CL CL200400590A patent/CL2004000590A1/es unknown
- 2004-03-22 BR BR122016023941-1A patent/BR122016023941B1/pt active IP Right Grant
- 2004-03-22 CN CN200480006480A patent/CN100588650C/zh not_active Expired - Lifetime
- 2004-03-22 RU RU2005132632/04A patent/RU2342367C2/ru active
- 2004-03-22 ES ES04722259.1T patent/ES2574580T3/es not_active Expired - Lifetime
- 2004-03-22 NZ NZ541829A patent/NZ541829A/en unknown
- 2004-03-22 AR ARP040100937A patent/AR043673A1/es not_active Application Discontinuation
- 2004-03-22 AU AU2004224153A patent/AU2004224153B2/en not_active Expired
- 2004-03-23 US US10/807,766 patent/US7208509B2/en active Active
-
2005
- 2005-08-18 IL IL170343A patent/IL170343A/en active IP Right Grant
- 2005-09-15 NO NO20054264A patent/NO334095B1/no unknown
- 2005-09-21 CO CO05095661A patent/CO5601029A2/es not_active Application Discontinuation
- 2005-09-21 HR HR20050830A patent/HRP20050830A2/xx not_active Application Discontinuation
-
2007
- 2007-02-02 US US11/701,881 patent/US7348345B2/en not_active Expired - Lifetime
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