AR012340A1 - 3,4-dihidro-2(1h)-quinazolinonas 4,4-disustituidas utiles como inhibidores de la transcriptasa inversa del hiv, composicion y kitfarmaceuticos que las contienen - Google Patents
3,4-dihidro-2(1h)-quinazolinonas 4,4-disustituidas utiles como inhibidores de la transcriptasa inversa del hiv, composicion y kitfarmaceuticos que las contienenInfo
- Publication number
- AR012340A1 AR012340A1 ARP980101558A ARP980101558A AR012340A1 AR 012340 A1 AR012340 A1 AR 012340A1 AR P980101558 A ARP980101558 A AR P980101558A AR P980101558 A ARP980101558 A AR P980101558A AR 012340 A1 AR012340 A1 AR 012340A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- dihydro
- useful
- nr5r5a
- reverse transcriptase
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title abstract 2
- 102100034343 Integrase Human genes 0.000 title 1
- 108010092799 RNA-directed DNA polymerase Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 2
- 125000006555 (C3-C5) cycloalkyl group Chemical group 0.000 abstract 2
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 1
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 abstract 1
- 238000009007 Diagnostic Kit Methods 0.000 abstract 1
- 108010078851 HIV Reverse Transcriptase Proteins 0.000 abstract 1
- -1 NR5R5a Inorganic materials 0.000 abstract 1
- 229910052794 bromium Inorganic materials 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 229910052740 iodine Inorganic materials 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 239000003419 rna directed dna polymerase inhibitor Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
-
- 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
-
- 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
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
- C07D239/80—Oxygen atoms
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Virology (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La presente invencion hace conocer 3,4-dihidro-2(1H)-quinazolinonas 4,4- disustituidas de la formula (I), o las formas estereoisoméricas, mezclasestereoisoméricas o sales apras para uso farmacéutico de las mismas, que son de utilidad como inhibidores de la transcriptasa inversa del HIV y concomposiciones farmacéuticas y kits de diagnostico que contienen a las mismas, donde: R1 es alquilo-C1-3 sustituido con 1-7 halogenos; R2 se selecciona dealquilo-C1-5 sustituido con 1-2 R4, alquenilo-C2-5 sustituido con 1-2 R4 y alquinilo-C2-5 sustituido con 1 R4; R3, en cada aparicion, se seleccionaindependientemente de alquilo-C1-4, OH, alcoxi-C1-4, F, Cl, Br, I, NR5R5a, NO2, CN, C(O)R6, NHC(O)R7 y NHC(O)NR5R5a, como alternativa, si hay dosR3 yestán unidos a átomos de carbono adyacentes, entonces se pueden combinar para formar -OCH2O-; R4 se selecciona de cicloalquilo-C3-5 sustituido con 0-2 R3,fenilo sustituido con 0-5 R3 y un sistema heterocíclico de 5-6 miembros que contienede 1-3 heteroátomos seleccionados entre O, N y S, sustituido con 0-2R3; R5 y R5a se seleccionan independientemente de H y alquilo C1-3; R6 se selecciona de H, OH, alquilo C1-4, alcoxi-C1-4, y NR5R5a; R7 se selecciona dealquilo C1-3 y alcoxi-C1-3; R8 se selecciona de H, cicloalquilo-C3-5 y alquilo C1-3 y n se selecciona de 0, 1, 2, 3 y 4.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US83854097A | 1997-04-09 | 1997-04-09 | |
| US7132298P | 1998-01-14 | 1998-01-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR012340A1 true AR012340A1 (es) | 2000-10-18 |
Family
ID=26752095
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP980101558A AR012340A1 (es) | 1997-04-09 | 1998-04-06 | 3,4-dihidro-2(1h)-quinazolinonas 4,4-disustituidas utiles como inhibidores de la transcriptasa inversa del hiv, composicion y kitfarmaceuticos que las contienen |
Country Status (19)
| Country | Link |
|---|---|
| EP (1) | EP0973753A2 (es) |
| JP (1) | JP2002504095A (es) |
| KR (1) | KR20010006146A (es) |
| CN (1) | CN1252063A (es) |
| AR (1) | AR012340A1 (es) |
| AU (1) | AU734928B2 (es) |
| BR (1) | BR9808513A (es) |
| CA (1) | CA2284996A1 (es) |
| EA (1) | EA001991B1 (es) |
| EE (1) | EE9900452A (es) |
| HR (1) | HRP980143A2 (es) |
| HU (1) | HUP0001446A3 (es) |
| IL (1) | IL132188A0 (es) |
| NO (1) | NO314936B1 (es) |
| NZ (1) | NZ500592A (es) |
| PL (1) | PL336305A1 (es) |
| SK (1) | SK137899A3 (es) |
| TW (1) | TW587078B (es) |
| WO (1) | WO1998045276A2 (es) |
Families Citing this family (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2002509922A (ja) * | 1998-03-27 | 2002-04-02 | デュポン ファーマシューティカルズ カンパニー | ４，４−二置換−３，４−ジヒドロ−２（１ｈ）−キナゾリンチオン誘導体、それらの調製法、およびｈｉｖ逆転写酵素阻害剤としてのそれらの使用 |
| AU6508899A (en) | 1998-10-13 | 2000-05-01 | Du Pont Pharmaceuticals Company | Selective eradication of virally-infected cells by combined use of a cytotoxic agent and an antiviral agent |
| US6225317B1 (en) * | 1998-11-19 | 2001-05-01 | Dupont Pharmaceuticals Company | Crystalline (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-3,4-dihydro-2(1H)-quinazolinone |
| HRP990359A2 (en) * | 1998-11-19 | 2000-08-31 | Du Pont Pharm Co | A process for the preparation of quinazolinones |
| US6175009B1 (en) | 1999-11-18 | 2001-01-16 | Dupont Pharmaceuticals Company | Process for the preparation of quinazolinones |
| EP1233950B1 (en) * | 1999-11-23 | 2005-10-05 | Smithkline Beecham Corporation | 3,4-DIHYDRO-(1H)QUINAZOLIN-2-ONE COMPOUNDS AS CSBP/P39 kINASE INHIBITORS |
| US6759410B1 (en) | 1999-11-23 | 2004-07-06 | Smithline Beecham Corporation | 3,4-dihydro-(1H)-quinazolin-2-ones and their use as CSBP/p38 kinase inhibitors |
| US6555686B2 (en) | 2000-03-23 | 2003-04-29 | Bristol-Myers Squibb Pharma | Asymmetric synthesis of quinazolin-2-ones useful as HIV reverse transcriptase inhibitors |
| CA2403230A1 (en) * | 2000-03-23 | 2001-09-27 | Lilian A. Radesca | Asymmetric synthesis of quinazolin-2-ones useful as hiv reverse transcriptase inhibitors |
| US6596729B2 (en) | 2000-07-20 | 2003-07-22 | Bristol-Myers Squibb Company | Tricyclic-2-pyridone compounds useful as HIV reverse transcriptase inhibitors |
| ZA200300255B (en) | 2000-07-20 | 2004-09-28 | Bristol Myers Squibb Pharma Co | Tricyclic 2-pyridone compounds useful as HIV reverse transcriptase inhibitors. |
| US8641644B2 (en) | 2000-11-21 | 2014-02-04 | Sanofi-Aventis Deutschland Gmbh | Blood testing apparatus having a rotatable cartridge with multiple lancing elements and testing means |
| US9226699B2 (en) | 2002-04-19 | 2016-01-05 | Sanofi-Aventis Deutschland Gmbh | Body fluid sampling module with a continuous compression tissue interface surface |
| US9427532B2 (en) | 2001-06-12 | 2016-08-30 | Sanofi-Aventis Deutschland Gmbh | Tissue penetration device |
| US9795747B2 (en) | 2010-06-02 | 2017-10-24 | Sanofi-Aventis Deutschland Gmbh | Methods and apparatus for lancet actuation |
| US7041068B2 (en) | 2001-06-12 | 2006-05-09 | Pelikan Technologies, Inc. | Sampling module device and method |
| US9314194B2 (en) | 2002-04-19 | 2016-04-19 | Sanofi-Aventis Deutschland Gmbh | Tissue penetration device |
| US8784335B2 (en) | 2002-04-19 | 2014-07-22 | Sanofi-Aventis Deutschland Gmbh | Body fluid sampling device with a capacitive sensor |
| US8579831B2 (en) | 2002-04-19 | 2013-11-12 | Sanofi-Aventis Deutschland Gmbh | Method and apparatus for penetrating tissue |
| US8702624B2 (en) | 2006-09-29 | 2014-04-22 | Sanofi-Aventis Deutschland Gmbh | Analyte measurement device with a single shot actuator |
| US9795334B2 (en) | 2002-04-19 | 2017-10-24 | Sanofi-Aventis Deutschland Gmbh | Method and apparatus for penetrating tissue |
| US9248267B2 (en) | 2002-04-19 | 2016-02-02 | Sanofi-Aventis Deustchland Gmbh | Tissue penetration device |
| US7708701B2 (en) | 2002-04-19 | 2010-05-04 | Pelikan Technologies, Inc. | Method and apparatus for a multi-use body fluid sampling device |
| US7547287B2 (en) | 2002-04-19 | 2009-06-16 | Pelikan Technologies, Inc. | Method and apparatus for penetrating tissue |
| EP1575583A1 (en) * | 2002-12-16 | 2005-09-21 | Boehringer Ingelheim Pharmaceuticals Inc. | Treatment of hiv infection through combined administration of tipranavir and capravirine |
| US8574895B2 (en) | 2002-12-30 | 2013-11-05 | Sanofi-Aventis Deutschland Gmbh | Method and apparatus using optical techniques to measure analyte levels |
| WO2006001797A1 (en) | 2004-06-14 | 2006-01-05 | Pelikan Technologies, Inc. | Low pain penetrating |
| EP1671096A4 (en) | 2003-09-29 | 2009-09-16 | Pelikan Technologies Inc | METHOD AND APPARATUS FOR PROVIDING IMPROVED SAMPLE CAPTURING DEVICE |
| WO2005037095A1 (en) | 2003-10-14 | 2005-04-28 | Pelikan Technologies, Inc. | Method and apparatus for a variable user interface |
| EP1706026B1 (en) | 2003-12-31 | 2017-03-01 | Sanofi-Aventis Deutschland GmbH | Method and apparatus for improving fluidic flow and sample capture |
| EP1751546A2 (en) | 2004-05-20 | 2007-02-14 | Albatros Technologies GmbH & Co. KG | Printable hydrogel for biosensors |
| EP1765194A4 (en) | 2004-06-03 | 2010-09-29 | Pelikan Technologies Inc | METHOD AND DEVICE FOR A LIQUID DETECTION DEVICE |
| US9775553B2 (en) | 2004-06-03 | 2017-10-03 | Sanofi-Aventis Deutschland Gmbh | Method and apparatus for a fluid sampling device |
| WO2009126900A1 (en) | 2008-04-11 | 2009-10-15 | Pelikan Technologies, Inc. | Method and apparatus for analyte detecting device |
| US9375169B2 (en) | 2009-01-30 | 2016-06-28 | Sanofi-Aventis Deutschland Gmbh | Cam drive for managing disposable penetrating member actions with a single motor and motor and control system |
| US8440693B2 (en) | 2009-12-22 | 2013-05-14 | Novartis Ag | Substituted isoquinolinones and quinazolinones |
| US8965476B2 (en) | 2010-04-16 | 2015-02-24 | Sanofi-Aventis Deutschland Gmbh | Tissue penetration device |
| CN102060786A (zh) * | 2011-01-20 | 2011-05-18 | 天津大学 | 4-(取代-1,3-二炔基)-4-(三氟甲基)-3,4-二氢取代喹唑啉-2-酮类化合物及其制备方法和应用 |
| MX343037B (es) * | 2011-04-06 | 2016-10-20 | Biovaxim Ltd | Composiciones farmaceuticas para evitar y/o tratar una enfermedad de vih en humanos. |
| CN104321325B (zh) | 2012-05-24 | 2016-11-16 | 诺华股份有限公司 | 吡咯并吡咯烷酮化合物 |
| US9403827B2 (en) | 2013-01-22 | 2016-08-02 | Novartis Ag | Substituted purinone compounds |
| US9556180B2 (en) | 2013-01-22 | 2017-01-31 | Novartis Ag | Pyrazolo[3,4-d]pyrimidinone compounds as inhibitors of the P53/MDM2 interaction |
| EA029312B1 (ru) | 2013-05-27 | 2018-03-30 | Новартис Аг | Производные имидазопирролидинона и их применение при лечении заболеваний |
| KR20160012197A (ko) | 2013-05-28 | 2016-02-02 | 노파르티스 아게 | 피라졸로-피롤리딘-4-온 유도체 및 질환의 치료에서의 그의 용도 |
| MX2015016421A (es) | 2013-05-28 | 2016-03-03 | Novartis Ag | Derivados de pirazolo-pirrolidin-4-ona como inhibidores de bet y su uso en el tratamiento de enfermedades. |
| AU2014351413B2 (en) | 2013-11-21 | 2017-06-01 | Novartis Ag | Pyrrolopyrrolone derivatives and their use as BET inhibitors |
| CN116745269A (zh) * | 2020-08-27 | 2023-09-12 | 默沙东有限责任公司 | 用于治疗hiv的作为选择性细胞毒性剂的二氢喹唑啉-2-酮衍生物 |
| AR133187A1 (es) * | 2023-07-07 | 2025-09-03 | Merck Sharp & Dohme Llc | Derivados de tetrahidroquinazolina como agentes citotóxicos selectivos |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL102764A0 (en) * | 1991-08-16 | 1993-01-31 | Merck & Co Inc | Quinazoline derivatives,and pharmaceutical compositions containing them |
| AU2436792A (en) * | 1991-08-16 | 1993-03-16 | Merck & Co., Inc. | Quinazoline derivatives as inhibitors of hiv reverse transcriptase |
| KR950701322A (ko) * | 1992-05-07 | 1995-03-23 | 조셉 에프. 디프리마 | 사람면역결핍바이러스 역전사효소의 억제제로서의 신규한 퀴나졸린(New quinazolines as inhibitors of HIV reversetranscriptase) |
| US5665720A (en) * | 1992-08-07 | 1997-09-09 | Merck & Co., Inc. | Benzoxazinones as inhibitors of HIV reverse transcriptase |
| DE4320347A1 (de) * | 1993-06-19 | 1994-12-22 | Boehringer Mannheim Gmbh | Quinazolin-Derivate und diese enthaltende Arzneimittel |
| GB2281297A (en) * | 1993-08-27 | 1995-03-01 | Merck & Co Inc | Quinazoline compounds |
| WO1995012583A1 (en) * | 1993-11-05 | 1995-05-11 | Merck & Co., Inc. | New quinazolines as inhibitors of hiv reverse transcriptase |
| US5434152A (en) * | 1993-11-08 | 1995-07-18 | Merck & Co., Inc. | Asymmetric synthesis of (S)-(-)-6-chloro-4- cyclopropyl-3,4-dihydro-4-[(2-pyridyl)ethynyl]-2(1H)-quinazolinone |
-
1998
- 1998-03-19 HR HR60/071,322A patent/HRP980143A2/hr not_active Application Discontinuation
- 1998-04-06 AR ARP980101558A patent/AR012340A1/es not_active Application Discontinuation
- 1998-04-07 PL PL98336305A patent/PL336305A1/xx unknown
- 1998-04-07 JP JP54297198A patent/JP2002504095A/ja active Pending
- 1998-04-07 CA CA002284996A patent/CA2284996A1/en not_active Abandoned
- 1998-04-07 EP EP98913401A patent/EP0973753A2/en not_active Withdrawn
- 1998-04-07 KR KR1019997009225A patent/KR20010006146A/ko not_active Ceased
- 1998-04-07 WO PCT/US1998/006733 patent/WO1998045276A2/en not_active Ceased
- 1998-04-07 CN CN98803974A patent/CN1252063A/zh active Pending
- 1998-04-07 IL IL13218898A patent/IL132188A0/xx unknown
- 1998-04-07 AU AU67960/98A patent/AU734928B2/en not_active Ceased
- 1998-04-07 SK SK1378-99A patent/SK137899A3/sk unknown
- 1998-04-07 EA EA199900907A patent/EA001991B1/ru not_active IP Right Cessation
- 1998-04-07 EE EEP199900452A patent/EE9900452A/xx unknown
- 1998-04-07 NZ NZ500592A patent/NZ500592A/en unknown
- 1998-04-07 BR BR9808513-1A patent/BR9808513A/pt not_active IP Right Cessation
- 1998-04-07 HU HU0001446A patent/HUP0001446A3/hu unknown
- 1998-04-15 TW TW087105365A patent/TW587078B/zh active
-
1999
- 1999-10-08 NO NO19994904A patent/NO314936B1/no not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| AU6796098A (en) | 1998-10-30 |
| NZ500592A (en) | 2001-09-28 |
| EE9900452A (et) | 2000-04-17 |
| HUP0001446A3 (en) | 2001-11-28 |
| PL336305A1 (en) | 2000-06-19 |
| BR9808513A (pt) | 2000-05-23 |
| CN1252063A (zh) | 2000-05-03 |
| KR20010006146A (ko) | 2001-01-26 |
| HUP0001446A2 (hu) | 2001-05-28 |
| NO994904L (no) | 1999-12-01 |
| NO314936B1 (no) | 2003-06-16 |
| EA001991B1 (ru) | 2001-10-22 |
| WO1998045276A2 (en) | 1998-10-15 |
| CA2284996A1 (en) | 1998-10-15 |
| NO994904D0 (no) | 1999-10-08 |
| SK137899A3 (en) | 2000-05-16 |
| EP0973753A2 (en) | 2000-01-26 |
| JP2002504095A (ja) | 2002-02-05 |
| IL132188A0 (en) | 2001-03-19 |
| AU734928B2 (en) | 2001-06-28 |
| EA199900907A1 (ru) | 2000-04-24 |
| TW587078B (en) | 2004-05-11 |
| WO1998045276A3 (en) | 1999-01-14 |
| HRP980143A2 (en) | 1999-02-28 |
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