BRPI0408704A - benzil-piridazinonas como inibidores de transcriptase reversa - Google Patents
benzil-piridazinonas como inibidores de transcriptase reversaInfo
- Publication number
- BRPI0408704A BRPI0408704A BRPI0408704-6A BRPI0408704A BRPI0408704A BR PI0408704 A BRPI0408704 A BR PI0408704A BR PI0408704 A BRPI0408704 A BR PI0408704A BR PI0408704 A BRPI0408704 A BR PI0408704A
- Authority
- BR
- Brazil
- Prior art keywords
- reverse transcriptase
- formula
- compounds
- transcriptase inhibitors
- pyridazinones
- Prior art date
Links
- 239000003419 rna directed dna polymerase inhibitor Substances 0.000 title abstract 2
- GZVJKNAPQDHVHH-UHFFFAOYSA-N 5-benzyl-1h-pyridazin-6-one Chemical class O=C1NN=CC=C1CC1=CC=CC=C1 GZVJKNAPQDHVHH-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 241000725303 Human immunodeficiency virus Species 0.000 abstract 3
- AAILEWXSEQLMNI-UHFFFAOYSA-N 1h-pyridazin-6-one Chemical class OC1=CC=CN=N1 AAILEWXSEQLMNI-UHFFFAOYSA-N 0.000 abstract 1
- 102100034343 Integrase Human genes 0.000 abstract 1
- 108010092799 RNA-directed DNA polymerase Proteins 0.000 abstract 1
- 241000700605 Viruses Species 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 239000002904 solvent Substances 0.000 abstract 1
- 239000003981 vehicle Substances 0.000 abstract 1
Classifications
-
- 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
- C07D401/12—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 chain containing hetero atoms as chain links
-
- 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
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members 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
- C07D237/14—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members 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
- C07D237/22—Nitrogen and oxygen 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
- C07D405/06—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Virology (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- AIDS & HIV (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Abstract
"BENZIL-PIRIDAZINONAS COMO INIBIDORES DE TRANSCRIPTASE REVERSA". Esta invenção refere-se a derivados de piridazinonas inusitados, da fórmula I, onde R¬ 1¬-R¬ 4¬, R¬ 7¬, R¬ 8¬ e X¬ 1¬ são como definidos no sumário, e seus sais e solvatos farmaceuticamente aceitáveis, e métodos para inibir ou modular a trasncriptase reversa do Vírus da Imunodeficiência Humana (HIV) com compostos da fórmula I, composições farmacêuticas que contêm os compostos da fórmula I misturados com pelo menos um solvente, veículo ou excipiente, e processos para preparar compostos da fórmula I. Os compostos são úteis para tratar distúrbios nos quais HIV e vírus geneticamente relacionados estão implicados.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US45714403P | 2003-03-24 | 2003-03-24 | |
| PCT/EP2004/002736 WO2004085406A1 (en) | 2003-03-24 | 2004-03-17 | Benzyl-pyridazinons as reverse transcriptase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0408704A true BRPI0408704A (pt) | 2006-03-07 |
Family
ID=33098202
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0408704-6A BRPI0408704A (pt) | 2003-03-24 | 2004-03-17 | benzil-piridazinonas como inibidores de transcriptase reversa |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US7189718B2 (pt) |
| EP (1) | EP1608629A1 (pt) |
| JP (1) | JP4485520B2 (pt) |
| KR (1) | KR20050119652A (pt) |
| CN (1) | CN100469769C (pt) |
| AR (1) | AR043674A1 (pt) |
| AU (1) | AU2004224191A1 (pt) |
| BR (1) | BRPI0408704A (pt) |
| CA (1) | CA2518823A1 (pt) |
| MX (1) | MXPA05010081A (pt) |
| RU (1) | RU2344128C2 (pt) |
| TW (1) | TW200505453A (pt) |
| WO (1) | WO2004085406A1 (pt) |
Families Citing this family (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE0102299D0 (sv) | 2001-06-26 | 2001-06-26 | Astrazeneca Ab | Compounds |
| SE0102764D0 (sv) | 2001-08-17 | 2001-08-17 | Astrazeneca Ab | Compounds |
| ES2232306B1 (es) * | 2003-11-10 | 2006-08-01 | Almirall Prodesfarma, S.A. | Nuevos derivados de piridazin-3(2h)-ona. |
| JP4627315B2 (ja) * | 2004-03-23 | 2011-02-09 | エフ.ホフマン−ラ ロシュ アーゲー | 非ヌクレオシド逆転写酵素阻害剤としてのベンジルピリダジノン誘導体 |
| WO2005100323A1 (en) * | 2004-04-15 | 2005-10-27 | F. Hoffmann-La Roche Ag | Process for preparing pyridazinone compounds |
| KR20070085371A (ko) * | 2004-10-16 | 2007-08-27 | 아스트라제네카 아베 | 페녹시 벤즈아미드 화합물의 제조 방법 |
| GB0423042D0 (en) * | 2004-10-16 | 2004-11-17 | Astrazeneca Ab | Chemical process |
| CN101180280A (zh) * | 2005-03-24 | 2008-05-14 | 弗·哈夫曼-拉罗切有限公司 | 作为杂环逆转录酶抑制剂的1,2,4-三唑-5-酮化合物 |
| KR101346902B1 (ko) | 2005-07-09 | 2014-01-02 | 아스트라제네카 아베 | 당뇨병 치료에 있어 glk 활성화제로서 사용하기 위한헤테로아릴 벤즈아미드 유도체 |
| DK1919878T3 (da) * | 2005-07-21 | 2010-10-25 | Hoffmann La Roche | Pyridazinonderivater som thyroidhormonreceptoragonister |
| AR057455A1 (es) | 2005-07-22 | 2007-12-05 | Merck & Co Inc | Inhibidores de la transcriptasa reversa de vih y composicion farmaceutica |
| CA2623728A1 (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 |
| JO2769B1 (en) | 2005-10-26 | 2014-03-15 | جانسين فارماسوتيكا ان. في | Rapid decomposition of physiologically antagonistic agents of the 2-dopamine receptor |
| GB0610680D0 (en) * | 2006-05-31 | 2006-07-12 | Istituto Di Ricerche D Biolog | Therapeutic compounds |
| 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 |
| RU2451676C2 (ru) | 2006-08-16 | 2012-05-27 | Ф.Хоффманн-Ля Рош Аг | Ненуклеозидные ингибиторы обратной транскриптазы |
| JO2849B1 (en) | 2007-02-13 | 2015-03-15 | جانسين فارماسوتيكا ان. في | Dopamine 2 receptor antagonists are rapidly hydrolyzed |
| WO2008119662A1 (en) | 2007-03-29 | 2008-10-09 | F. Hoffmann-La Roche Ag | Non-nucleoside reverse transcriptase inhibitors |
| CN101679414A (zh) * | 2007-04-09 | 2010-03-24 | 弗·哈夫曼-拉罗切有限公司 | 非核苷逆转录酶抑制剂 |
| RS52518B (sr) | 2007-04-23 | 2013-04-30 | Janssen Pharmaceutica N.V. | Derivati 4-alkoksipiridazina kao brzo disocirajući dopamin 2 receptorski antagonisti |
| MX2009011416A (es) | 2007-04-23 | 2009-11-05 | Janssen Pharmaceutica Nv | Tia(di)azoles como antagonistas del receptor de dopamina 2 de disociacion rapida. |
| JP5167350B2 (ja) | 2007-05-30 | 2013-03-21 | エフ.ホフマン−ラ ロシュ アーゲー | 非ヌクレオシド系逆転写酵素阻害剤 |
| JP2010530863A (ja) * | 2007-06-22 | 2010-09-16 | エフ.ホフマン−ラ ロシュ アーゲー | 非ヌクレオシド逆転写酵素阻害剤としての尿素及びカルバマート誘導体 |
| EP2220073B1 (en) | 2007-11-15 | 2014-09-03 | MSD Italia S.r.l. | Pyridazinone derivatives as parp inhibitors |
| KR20100088142A (ko) | 2007-11-20 | 2010-08-06 | 머크 샤프 앤드 돔 코포레이션 | 비-뉴클레오사이드 역전사효소 억제제 |
| US8877816B2 (en) * | 2007-11-21 | 2014-11-04 | Decode Genetics Ehf | 4-(or 5-) substituted catechol derivatives |
| WO2009080534A1 (en) * | 2007-12-21 | 2009-07-02 | F. Hoffmann-La Roche Ag | Heterocyclic antiviral compounds |
| ES2622161T3 (es) | 2008-07-31 | 2017-07-05 | Janssen Pharmaceutica, N.V. | Piridinas sustituidas con piperazin-1-il-trifluorometilo como antagonistas del receptor de la dopamina 2 de disociación rápida |
| EP2366699B1 (en) | 2008-10-02 | 2013-08-07 | Asahi Kasei Pharma Corporation | 8-substituted isoquinoline derivative and use thereof |
| HUE025336T2 (en) | 2010-03-30 | 2016-03-29 | Merck Canada Inc | Non-nucleoside reverse transcriptase inhibitors |
| CN102731410B (zh) * | 2012-07-06 | 2014-07-30 | 山东大学 | 一种哒嗪类hiv-1逆转录酶抑制剂的制备与应用 |
| AR092872A1 (es) | 2012-09-17 | 2015-05-06 | Madrigal Pharmaceuticals Inc | Metodo para sintetizar analogos de la hormona tiroidea y polimorfos de los mismos |
| JO3470B1 (ar) | 2012-10-08 | 2020-07-05 | Merck Sharp & Dohme | مشتقات 5- فينوكسي-3h-بيريميدين-4-أون واستخدامها كمثبطات ناسخ عكسي ل hiv |
| PL3125894T3 (pl) | 2014-04-01 | 2021-02-08 | Merck Sharp & Dohme Corp. | Proleki inhibitorów odwrotnej transkryptazy hiv |
| DE102015011861B4 (de) | 2015-09-10 | 2018-03-01 | Rudolf Schindler | Neue cyclische Carboxamide als NMDA NR2B Rezeptor Inhibitoren |
| WO2018075650A1 (en) | 2016-10-18 | 2018-04-26 | Madrigal Pharmaceuticals, Inc. | Methods of treating liver disorders or lipid disorders with a thr-beta agonist |
| CN109053693B (zh) * | 2018-09-20 | 2021-02-05 | 顺毅股份有限公司 | 哒嗪胺类化合物的制备及其应用 |
| PE20211704A1 (es) | 2018-12-18 | 2021-09-01 | Merck Sharp & Dohme | Derivados de pirimidona como agentes citotoxicos selectivos contra celulas infectadas por vih |
| KR20220030256A (ko) * | 2019-07-01 | 2022-03-10 | 아센타위츠 파마슈티컬즈 리미티드 | Akr1c3 저해제 및 이의 의학적 용도 |
| CN116003253A (zh) * | 2022-12-31 | 2023-04-25 | 上海试四化学品有限公司 | 一种三氟苯嘧啶中间体2-[3-(三氟甲基)苯基]丙二酸二甲酯的制备方法 |
| US12377104B1 (en) | 2024-02-06 | 2025-08-05 | Madrigal Pharmaceuticals, Inc. | Methods for treating a fatty liver disease |
| WO2026042788A1 (ja) * | 2024-08-20 | 2026-02-26 | 塩野義製薬株式会社 | 複素環誘導体 |
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| US4949314A (en) | 1966-08-16 | 1990-08-14 | The United States Of America As Represented By The Secretary Of The Navy | Method and means for increasing echo-ranging-search rate |
| US4211771A (en) | 1971-06-01 | 1980-07-08 | Robins Ronald K | Treatment of human viral diseases with 1-B-D-ribofuranosyl-1,2,4-triazole-3-carboxamide |
| US4518584A (en) | 1983-04-15 | 1985-05-21 | Cetus Corporation | Human recombinant interleukin-2 muteins |
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| GB8327880D0 (en) | 1983-10-18 | 1983-11-16 | Ajinomoto Kk | Saccharomyces cerevisiae |
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| CA2225666A1 (en) | 1995-06-30 | 1997-01-23 | Smithkline Beecham Corporation | Use of stat 5 sh2 domain specific compounds to enhance erythropoiesis |
| WO1997002023A1 (en) | 1995-06-30 | 1997-01-23 | Smithkline Beecham Corporation | USE OF Stat 6 SH2 DOMAIN SPECIFIC COMPOUNDS TO TREAT ALLERGIC REACTIONS |
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| RU2000129671A (ru) * | 1998-04-27 | 2004-02-20 | Сантр Насьональ Де Ля Решерш Сьентифик (Fr) | Производные 3-(амино- или аминоалкил) пиридинона и их применение для лечения болезней, связанных с ВИЧ |
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-
2004
- 2004-03-17 CN CNB2004800081215A patent/CN100469769C/zh not_active Expired - Fee Related
- 2004-03-17 EP EP04721167A patent/EP1608629A1/en not_active Withdrawn
- 2004-03-17 AU AU2004224191A patent/AU2004224191A1/en not_active Abandoned
- 2004-03-17 CA CA002518823A patent/CA2518823A1/en not_active Abandoned
- 2004-03-17 KR KR1020057017745A patent/KR20050119652A/ko not_active Withdrawn
- 2004-03-17 RU RU2005132630/04A patent/RU2344128C2/ru active
- 2004-03-17 MX MXPA05010081A patent/MXPA05010081A/es active IP Right Grant
- 2004-03-17 JP JP2006504704A patent/JP4485520B2/ja not_active Expired - Fee Related
- 2004-03-17 BR BRPI0408704-6A patent/BRPI0408704A/pt not_active IP Right Cessation
- 2004-03-17 WO PCT/EP2004/002736 patent/WO2004085406A1/en not_active Ceased
- 2004-03-18 TW TW093107263A patent/TW200505453A/zh unknown
- 2004-03-22 AR ARP040100938A patent/AR043674A1/es unknown
- 2004-03-23 US US10/807,993 patent/US7189718B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| CN100469769C (zh) | 2009-03-18 |
| WO2004085406A1 (en) | 2004-10-07 |
| US20040198736A1 (en) | 2004-10-07 |
| AR043674A1 (es) | 2005-08-03 |
| JP4485520B2 (ja) | 2010-06-23 |
| CN1764649A (zh) | 2006-04-26 |
| TW200505453A (en) | 2005-02-16 |
| CA2518823A1 (en) | 2004-10-07 |
| AU2004224191A1 (en) | 2004-10-07 |
| RU2005132630A (ru) | 2006-07-27 |
| RU2344128C2 (ru) | 2009-01-20 |
| US7189718B2 (en) | 2007-03-13 |
| EP1608629A1 (en) | 2005-12-28 |
| MXPA05010081A (es) | 2005-11-23 |
| JP2006521310A (ja) | 2006-09-21 |
| KR20050119652A (ko) | 2005-12-21 |
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