AR074493A1 - Derivados de quinazolinamida - Google Patents
Derivados de quinazolinamidaInfo
- Publication number
- AR074493A1 AR074493A1 ARP090104724A ARP090104724A AR074493A1 AR 074493 A1 AR074493 A1 AR 074493A1 AR P090104724 A ARP090104724 A AR P090104724A AR P090104724 A ARP090104724 A AR P090104724A AR 074493 A1 AR074493 A1 AR 074493A1
- Authority
- AR
- Argentina
- Prior art keywords
- conh
- hal
- mono
- ncooa
- ncooh
- Prior art date
Links
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 abstract 6
- 125000004429 atom Chemical group 0.000 abstract 3
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 3
- 101710113864 Heat shock protein 90 Proteins 0.000 abstract 2
- 102100034051 Heat shock protein HSP 90-alpha Human genes 0.000 abstract 2
- 229910006074 SO2NH2 Inorganic materials 0.000 abstract 2
- 125000002618 bicyclic heterocycle group Chemical group 0.000 abstract 2
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 229920006395 saturated elastomer Polymers 0.000 abstract 2
- 125000000565 sulfonamide group Chemical group 0.000 abstract 2
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 abstract 1
- 240000000543 Pentas lanceolata Species 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 230000033228 biological regulation Effects 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- -1 mono-substituted biphenyl Chemical group 0.000 abstract 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 abstract 1
- 125000002911 monocyclic heterocycle group Chemical group 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- ABVYZAMNSCVWJA-UHFFFAOYSA-N quinazoline-2-carboxamide Chemical class C1=CC=CC2=NC(C(=O)N)=NC=C21 ABVYZAMNSCVWJA-UHFFFAOYSA-N 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
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- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- Urology & Nephrology (AREA)
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- Heart & Thoracic Surgery (AREA)
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- Hematology (AREA)
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- Emergency Medicine (AREA)
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Abstract
Los nuevos derivados de quinazolinamida de la fórmula (1) en donde R1 es H, (CH2)nHet, (CH2)nAr, Hal o A, R2, R3 son en cada caso, de modo independiente entre sí, H, (CH2)nHet, (CH2)nAr, Hal OH u OA, R4, R5 son en cada caso, de modo independiente entre sí, H, A, (CH2)nHet, (CH2)nAr, o (CH2)pOC(=O)(CH2)pNH2, R4 y R5 junto con el átomo de N al que están unidos también son un heterociclo mono- o bicíclico saturado, insaturado o aromático no sustituido o mono-, di- o trisustituido con Hal, A, (CH2)nOH, (CH2)nOA, (CH2)nNH2, (CH2)nCOOH, (CH2)nCOOA, NHCOA, NA'COA, CONH2, CONHA CONAA', OC(=O)(CH2)pNH2 y/u =O (oxigeno del carbonilo), que puede contener otros 1 a 3 átomos de N, O y/o S y en donde también un átomo de N puede estar oxidado, X es CO o SO2, Ar es fenilo, naftilo, tetrahidronaftilo o bifenilo no sustituido o mono-, di-, tri-, tetra- o pentasustituido con A, Hal, (CH2)nOA, (CH2)nOH, (CH2)nCN, SA, SOA, SO2A, NO2, C:::CH, (CH2)nCOOH, CHO, (CH2)nCOOA, CONH2, CONHA, CONAA', NHCOA, CH(OH)A, (CH2)nNH2, (CH2)nNHA, (CH2)nNAA', (CH2)nNHSO2A, SO2NH(CH2)nNH2, SO2NH2, SO2NHA, SO2NAA', CONH(CH2)nCOOA, CONH(CH2)nCOOH, NHCO(CH2)nCOOA, NHCO(CH2)nCOOH, CONH(CH2)nNH2, CONH(CH2)nNHA, CONH(CH2)nNAA', CONH(CH2)nCN y/o (CH2)nCH(NH2)COOH, Het es un heterociclo saturado, insaturado o aromático mono- o bicíclico con 1 a 4 átomos de N, O y/o S, que puede no estar sustituido o que puede estar mono-, di- o trisustituido con A, OA, OH, fenilo, SH, S(O)mA, Hal, NO2, CN, COA, COOA, COObencilo, CONH2, CONHA, CONAA', SO2NH2, NH2, NHA, NAA', NHCOA, NHSO2A y/u =O (oxigeno del carbonilo), A, A' son en cada caso, de modo independiente entre sí, alquilo no ramificado o ramificado C1-10, en donde 1-3 grupos CH2 no adyacentes pueden estar reemplazados por O, S, SO, SO2, NH, NMe o NEt y/o también 1-5 átomos de H pueden estar reemplazados por F y/o CI, o alquilo cíclico C3-8, n es 0, 1, 2, 3 o 4, p es 1, 2, 3 o 4, así como sus sales y estereoisómeros farmacéuticamente aceptables, incluyendo sus mezclas en todas las proporciones. Son inhibidores de la HSP90 y pueden ser utilizados para preparar un medicamento para el tratamiento de enfermedades en las que la inhibición, la regulación y/o la modulación de la HSP90 desempena, un papel importante.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102008061214A DE102008061214A1 (de) | 2008-12-09 | 2008-12-09 | Chinazolinamidderivate |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR074493A1 true AR074493A1 (es) | 2011-01-19 |
Family
ID=41478685
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090104724A AR074493A1 (es) | 2008-12-09 | 2009-12-07 | Derivados de quinazolinamida |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US8546565B2 (es) |
| EP (1) | EP2356110B1 (es) |
| JP (1) | JP5749653B2 (es) |
| KR (1) | KR20110098772A (es) |
| CN (1) | CN102245596A (es) |
| AR (1) | AR074493A1 (es) |
| AU (1) | AU2009326602B2 (es) |
| BR (1) | BRPI0922652A2 (es) |
| CA (1) | CA2745988C (es) |
| DE (1) | DE102008061214A1 (es) |
| EA (1) | EA201100872A1 (es) |
| ES (1) | ES2564815T3 (es) |
| IL (1) | IL213424A (es) |
| MX (1) | MX2011005986A (es) |
| SG (1) | SG171902A1 (es) |
| WO (1) | WO2010066324A1 (es) |
| ZA (1) | ZA201105050B (es) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102009054302A1 (de) * | 2009-11-23 | 2011-05-26 | Merck Patent Gmbh | Chinazolinderivate |
| DE102010046837A1 (de) | 2010-09-29 | 2012-03-29 | Merck Patent Gmbh | Phenylchinazolinderivate |
| US9926309B2 (en) | 2011-10-05 | 2018-03-27 | The Board Of Trustees Of The Leland Stanford Junior University | Pi-kinase inhibitors with anti-infective activity |
| EP2763532B1 (en) | 2011-10-05 | 2018-09-19 | The Board of Trustees of the Leland Stanford Junior University | Pi-kinase inhibitors with broad spectrum anti-infective activity |
| AU2013226013B2 (en) * | 2012-02-29 | 2016-08-11 | Baruch S. Blumberg Institute | Inhibitors of Hepatitis B Virus Covalently Closed Circular DNA Formation and Their Method of Use |
| US10138212B2 (en) | 2015-02-06 | 2018-11-27 | Merck Sharp & Dohme Corp. | Aminoquinazoline compounds as A2A antagonist |
| EP3419980B1 (en) | 2016-02-26 | 2025-01-01 | The Board of Trustees of the Leland Stanford Junior University | Pi-kinase inhibitors with anti-infective activity |
| JP7701051B2 (ja) | 2019-03-21 | 2025-07-01 | ザ ボード オブ トラスティス オブ ザ リーランド スタンフォード ジュニア ユニヴァーシティー | Ｐｉ４－キナーゼ阻害剤及びその使用方法 |
| AU2020382723A1 (en) * | 2019-11-15 | 2022-06-02 | Georgia State University Research Foundation, Inc. | Small molecules polymerase inhibitors |
| MX2023009682A (es) | 2021-02-19 | 2023-10-30 | Sudo Biosciences Ltd | Inhibidores de tyk2 y sus usos. |
| IL305165A (en) | 2021-02-19 | 2023-10-01 | Sudo Biosciences Ltd | Tyk2 inhibitors and uses thereof |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5968921A (en) | 1997-10-24 | 1999-10-19 | Orgegon Health Sciences University | Compositions and methods for promoting nerve regeneration |
| AU3378599A (en) | 1998-04-03 | 1999-10-25 | University Of Pittsburgh | Benzoquinoid ansamycins for the treatment of cardiac arrest and stroke |
| CA2367108A1 (en) | 1999-03-12 | 2000-09-14 | The United States Of America, Represented By The Secretary, Department O F Health And Human Services | Method of inhibiting a chaperone protein |
| EP1265913A4 (en) | 2000-03-24 | 2004-07-14 | Univ Duke | CHARACTERIZATION OF THE INTERACTION BETWEEN GRP94 AND A LIGAND, AND CLEANING, SCREENING AND THERAPEUTIC PROCEDURES RELATING TO IT |
| WO2002002123A1 (en) | 2000-06-29 | 2002-01-10 | Trustees Of Boston University | Use of geldanamycin and related compounds for prophylaxis or treatment of fibrogenic disorders |
| EP1322325A4 (en) | 2000-07-20 | 2004-09-15 | Merck & Co Inc | INHIBITION OF PROCESSING AND REPLICATION OF HEPATITIS C VIRUS |
| WO2002009696A1 (en) | 2000-07-28 | 2002-02-07 | Sloan-Kettering Institute For Cancer Research | Methods for treating cell proliferative disorders and viral infections |
| CA2440842A1 (en) | 2001-04-16 | 2002-10-24 | Eisai Co., Ltd. | Novel 1h-indazole compounds |
| AU2002356922A1 (en) | 2001-11-09 | 2003-05-26 | Conforma Therapeutics Corporation | Hsp90-inhibiting zearalanol compounds and methods of producing and using same |
| BRPI0513819A (pt) | 2004-07-27 | 2008-05-20 | Novartis Ag | inibidores de hsp90 |
| AU2005302000A1 (en) | 2004-11-02 | 2006-05-11 | Conforma Therapeutics Corporation | Methods and compositions for treating chronic lymphocytic leukemia |
| AU2006236557A1 (en) | 2005-04-14 | 2006-10-26 | Novartis Vaccines And Diagnostics Inc. | 2-amino-quinazolin-5-ones as HSP90 inhibitors useful in treating proliferation diseases |
| DE102005022977A1 (de) * | 2005-05-19 | 2006-12-07 | Merck Patent Gmbh | Phenylchinazolinderivate |
| DE102005037733A1 (de) * | 2005-08-10 | 2007-02-15 | Merck Patent Gmbh | Adeninderivate |
| CL2007002994A1 (es) * | 2006-10-19 | 2008-02-08 | Wyeth Corp | Compuestos derivados heterociclicos que contienen sulfamoilo, inhibidores de hsp90; composicion farmaceutica; y uso para el tratamiento del cancer, tal como cancer de mama, de colon y prostata, entre otros. |
| DE602008003404D1 (de) * | 2007-02-01 | 2010-12-23 | Astrazeneca Ab | 5,6,7,8-tetrahydropteridin-derivate als hsp90-hemmer |
| GB2449293A (en) * | 2007-05-17 | 2008-11-19 | Evotec | Compounds having Hsp90 inhibitory activity |
| DE102007032739A1 (de) | 2007-07-13 | 2009-01-15 | Merck Patent Gmbh | Chinazolinamidderivate |
-
2008
- 2008-12-09 DE DE102008061214A patent/DE102008061214A1/de not_active Withdrawn
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2009
- 2009-11-12 ES ES09751824.5T patent/ES2564815T3/es active Active
- 2009-11-12 BR BRPI0922652-4A patent/BRPI0922652A2/pt not_active IP Right Cessation
- 2009-11-12 US US13/133,495 patent/US8546565B2/en not_active Expired - Fee Related
- 2009-11-12 WO PCT/EP2009/008061 patent/WO2010066324A1/de not_active Ceased
- 2009-11-12 AU AU2009326602A patent/AU2009326602B2/en not_active Ceased
- 2009-11-12 EP EP09751824.5A patent/EP2356110B1/de not_active Not-in-force
- 2009-11-12 JP JP2011539912A patent/JP5749653B2/ja not_active Expired - Fee Related
- 2009-11-12 CN CN2009801492388A patent/CN102245596A/zh active Pending
- 2009-11-12 EA EA201100872A patent/EA201100872A1/ru unknown
- 2009-11-12 KR KR1020117015247A patent/KR20110098772A/ko not_active Withdrawn
- 2009-11-12 SG SG2011039997A patent/SG171902A1/en unknown
- 2009-11-12 MX MX2011005986A patent/MX2011005986A/es active IP Right Grant
- 2009-11-12 CA CA2745988A patent/CA2745988C/en not_active Expired - Fee Related
- 2009-12-07 AR ARP090104724A patent/AR074493A1/es unknown
-
2011
- 2011-06-06 IL IL213424A patent/IL213424A/en active IP Right Grant
- 2011-07-08 ZA ZA2011/05050A patent/ZA201105050B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA2745988A1 (en) | 2010-06-17 |
| BRPI0922652A2 (pt) | 2015-08-11 |
| ES2564815T3 (es) | 2016-03-29 |
| SG171902A1 (en) | 2011-07-28 |
| EP2356110B1 (de) | 2016-01-06 |
| KR20110098772A (ko) | 2011-09-01 |
| JP5749653B2 (ja) | 2015-07-15 |
| AU2009326602B2 (en) | 2015-12-17 |
| WO2010066324A1 (de) | 2010-06-17 |
| DE102008061214A1 (de) | 2010-06-10 |
| US20110245225A1 (en) | 2011-10-06 |
| US8546565B2 (en) | 2013-10-01 |
| JP2012511520A (ja) | 2012-05-24 |
| MX2011005986A (es) | 2011-06-27 |
| EP2356110A1 (de) | 2011-08-17 |
| AU2009326602A1 (en) | 2011-07-28 |
| IL213424A (en) | 2014-03-31 |
| ZA201105050B (en) | 2012-03-28 |
| EA201100872A1 (ru) | 2012-01-30 |
| IL213424A0 (en) | 2011-07-31 |
| CN102245596A (zh) | 2011-11-16 |
| CA2745988C (en) | 2017-02-28 |
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