BR9612043A - Derivado de quinazolina,processos para preparar o mesmo e para produzir um efeito anti-angiogênico e/ou redutor da permeabilidade vascular em um animal de sangue quente necessitado de um tratamento desse tipo, e, composição farmacêutica - Google Patents
Derivado de quinazolina,processos para preparar o mesmo e para produzir um efeito anti-angiogênico e/ou redutor da permeabilidade vascular em um animal de sangue quente necessitado de um tratamento desse tipo, e, composição farmacêuticaInfo
- Publication number
- BR9612043A BR9612043A BR9612043-6A BR9612043A BR9612043A BR 9612043 A BR9612043 A BR 9612043A BR 9612043 A BR9612043 A BR 9612043A BR 9612043 A BR9612043 A BR 9612043A
- Authority
- BR
- Brazil
- Prior art keywords
- alkyl
- processes
- quinazoline
- prepare
- trifluoromethyl
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- JWVCLYRUEFBMGU-UHFFFAOYSA-N quinazoline Chemical compound N1=CN=CC2=CC=CC=C21 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 title abstract 2
- 230000008728 vascular permeability Effects 0.000 title abstract 2
- 230000001772 anti-angiogenic effect Effects 0.000 title 1
- 230000001603 reducing effect Effects 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002431 hydrogen Chemical class 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- -1 hydroxy halogen Chemical class 0.000 abstract 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 3
- 150000003839 salts Chemical class 0.000 abstract 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 102000005789 Vascular Endothelial Growth Factors Human genes 0.000 abstract 1
- 108010019530 Vascular Endothelial Growth Factors Proteins 0.000 abstract 1
- 125000004423 acyloxy group Chemical group 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 125000004414 alkyl thio group Chemical group 0.000 abstract 1
- 125000006615 aromatic heterocyclic group Chemical class 0.000 abstract 1
- 239000008280 blood Substances 0.000 abstract 1
- 210000004369 blood Anatomy 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 239000003638 chemical reducing agent Substances 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 239000004615 ingredient Substances 0.000 abstract 1
- LVWZTYCIRDMTEY-UHFFFAOYSA-N metamizole Chemical class O=C1C(N(CS(O)(=O)=O)C)=C(C)N(C)N1C1=CC=CC=C1 LVWZTYCIRDMTEY-UHFFFAOYSA-N 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical class [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 150000003246 quinazolines Chemical class 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
-
- 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
-
- 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
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/88—Oxygen atoms
-
- 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
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/93—Sulfur atoms
-
- 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
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/94—Nitrogen atoms
-
- 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
-
- 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
- C07D405/12—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 chain containing hetero atoms as chain links
-
- 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
- C07D409/12—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 chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Furan Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
"DERIVADO DE QUINAZOLINA, PROCESSOS PARA PREPARAR O MESMO E PARA PRODUZIR UM EFEITO ANTI-ANTIGIOGêNIO E/OU REDUTOR DA PERMEABILIDADE VASCULAR EM UM ANIMAL DE SANGUE QUENTE NECESSITADO DE UM TRATAMENTO DESSE TIPO, E, COMPOSIçãO FARMACêUTICA". A invenção refere-se a derivados de quinazolina de fórmula (I) [em que: Y' representa -O-, -S-, -CH~ 2~, -SO-, -SO~ 2~, -NR^ 5^CO-, -CONR^ 6^, SO~ 2~NR^ 7^, -NR^ 8^SO~ 2~- OU -NR^ 9^- (em que R^ 5^, R^ 6^, R^ 7^, R^ 8^ e R^ 9^ cada um, independentemente, representa hidrogênio, alquila ou alcoxialquila0; R^ 1^ representa hidrogênio, hidróxi halogênio, nitro, trifluorometila, ciano, alquila, alcóxi, alquiltio, amino ou alquilamino, R6 2^ representa hidrogênio, hidróxi, halogênio, alquila, alcóxi, trifluorometila, ciano, amino ou nitro; m é um número inteiro de 1 a 5 representa hidróxi, halogênio, alquila, alcóxi, alcanoilóxi, trifluorometila, ciano, amino ou nitro; R^ 4^ representa um grupo que é ou que contém um piridona opcionalmente substituída, fenila ou um grupo heterocíclico aromático] e seus sais; processos para sua preparação e composições farmacêuticas que contêm um composto de fórmula (I) ou um seu sal farmaceuticamente aceitável como ingrediente ativo. Os compostos de fórmula (I): e seus sais farmaceuticamente aceitáveis inibem os efeitos de VEGF, uma propriedade valiosa no tratamento de uma variedade de quadros clínicos que incluem o câncer e a artrite reumatóide.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP95402846 | 1995-12-18 | ||
| EP96402190 | 1996-10-15 | ||
| PCT/GB1996/003075 WO1997022596A1 (en) | 1995-12-18 | 1996-12-13 | Quinazoline derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR9612043A true BR9612043A (pt) | 1999-12-28 |
Family
ID=26140602
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR9612043-6A BR9612043A (pt) | 1995-12-18 | 1996-12-13 | Derivado de quinazolina,processos para preparar o mesmo e para produzir um efeito anti-angiogênico e/ou redutor da permeabilidade vascular em um animal de sangue quente necessitado de um tratamento desse tipo, e, composição farmacêutica |
Country Status (29)
| Country | Link |
|---|---|
| US (4) | US5962458A (pt) |
| EP (1) | EP0873319B1 (pt) |
| JP (1) | JP4291413B2 (pt) |
| KR (1) | KR100530311B1 (pt) |
| CN (1) | CN1133625C (pt) |
| AT (1) | ATE203524T1 (pt) |
| AU (1) | AU712370B2 (pt) |
| BR (1) | BR9612043A (pt) |
| CA (1) | CA2237005C (pt) |
| CZ (1) | CZ291100B6 (pt) |
| DE (1) | DE69614147T2 (pt) |
| DK (1) | DK0873319T3 (pt) |
| ES (1) | ES2162656T3 (pt) |
| GB (1) | GB9624482D0 (pt) |
| GR (1) | GR3036954T3 (pt) |
| HU (1) | HUP9901243A3 (pt) |
| IL (1) | IL124925A0 (pt) |
| MX (1) | MX9804247A (pt) |
| MY (1) | MY132405A (pt) |
| NO (1) | NO311358B1 (pt) |
| NZ (1) | NZ324007A (pt) |
| PL (1) | PL192309B1 (pt) |
| PT (1) | PT873319E (pt) |
| RU (1) | RU2194701C2 (pt) |
| SI (1) | SI0873319T1 (pt) |
| SK (1) | SK282443B6 (pt) |
| TR (1) | TR199801115T2 (pt) |
| TW (1) | TW411274B (pt) |
| WO (1) | WO1997022596A1 (pt) |
Families Citing this family (545)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6228871B1 (en) | 1995-07-10 | 2001-05-08 | Merck & Co., Inc. | Angiogenesis inhibitors |
| GB9624482D0 (en) | 1995-12-18 | 1997-01-15 | Zeneca Phaema S A | Chemical compounds |
| EP0880508B1 (en) | 1996-02-13 | 2003-04-16 | AstraZeneca AB | Quinazoline derivatives as vegf inhibitors |
| IL125954A (en) | 1996-03-05 | 2003-06-24 | Zeneca Ltd | Quinazoline derivatives, processes for their preparation, pharmaceutical compositions containing them and use thereof in the manufacture of medicaments having an antiangiogenic and/or vascular permeability reducing effect |
| NZ332119A (en) | 1996-04-12 | 2001-08-31 | Warner Lambert Co | Quinazoline compounds which are irreversible inhibitors of tyrosine kinases |
| GB9707800D0 (en) | 1996-05-06 | 1997-06-04 | Zeneca Ltd | Chemical compounds |
| CN1102593C (zh) | 1996-06-27 | 2003-03-05 | 詹森药业有限公司 | N－[4－(杂芳基甲基)苯基]－杂芳基胺类化合物 |
| GB9718972D0 (en) * | 1996-09-25 | 1997-11-12 | Zeneca Ltd | Chemical compounds |
| US6809097B1 (en) | 1996-09-25 | 2004-10-26 | Zeneca Limited | Quinoline derivatives inhibiting the effect of growth factors such as VEGF |
| JP2009007364A (ja) * | 1996-10-15 | 2009-01-15 | Astrazeneca Uk Ltd | キナゾリン誘導体 |
| US6225318B1 (en) | 1996-10-17 | 2001-05-01 | Pfizer Inc | 4-aminoquinazolone derivatives |
| ZA986729B (en) * | 1997-07-29 | 1999-02-02 | Warner Lambert Co | Irreversible inhibitors of tyrosine kinases |
| DE69838172T2 (de) | 1997-08-22 | 2008-04-10 | Astrazeneca Ab | Oxindolylchinazolinderivate als angiogenesehemmer |
| US6162804A (en) * | 1997-09-26 | 2000-12-19 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| US6465484B1 (en) | 1997-09-26 | 2002-10-15 | Merck & Co., Inc. | Angiogenesis inhibitors |
| FR2772763B1 (fr) * | 1997-12-24 | 2004-01-23 | Sod Conseils Rech Applic | Nouveaux analogues tetracycliques de camptothecines, leurs procedes de preparation, leur application comme medicaments et les compositions pharmaceutiques les contenant |
| US6686366B1 (en) | 1998-06-02 | 2004-02-03 | Osi Pharmaceuticals, Inc. | Compounds specific to adenosine A3 receptor and uses thereof |
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| SE9903544D0 (sv) | 1999-10-01 | 1999-10-01 | Astra Pharma Prod | Novel compounds |
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| UA74803C2 (uk) | 1999-11-11 | 2006-02-15 | Осі Фармасьютікалз, Інк. | Стійкий поліморф гідрохлориду n-(3-етинілфеніл)-6,7-біс(2-метоксіетокси)-4-хіназолінаміну, спосіб його одержання (варіанти) та фармацевтичне застосування |
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1996
- 1996-11-25 GB GBGB9624482.7A patent/GB9624482D0/en active Pending
- 1996-12-13 TR TR1998/01115T patent/TR199801115T2/xx unknown
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- 1996-12-13 PL PL327310A patent/PL192309B1/pl not_active IP Right Cessation
- 1996-12-13 JP JP52256897A patent/JP4291413B2/ja not_active Expired - Fee Related
- 1996-12-13 CZ CZ19981882A patent/CZ291100B6/cs not_active IP Right Cessation
- 1996-12-13 SI SI9630354T patent/SI0873319T1/xx unknown
- 1996-12-13 NZ NZ324007A patent/NZ324007A/xx not_active IP Right Cessation
- 1996-12-13 WO PCT/GB1996/003075 patent/WO1997022596A1/en not_active Application Discontinuation
- 1996-12-13 ES ES96941787T patent/ES2162656T3/es not_active Expired - Lifetime
- 1996-12-13 KR KR1019980704613A patent/KR100530311B1/ko not_active IP Right Cessation
- 1996-12-13 CN CNB961991100A patent/CN1133625C/zh not_active Expired - Fee Related
- 1996-12-13 CA CA002237005A patent/CA2237005C/en not_active Expired - Fee Related
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- 1996-12-13 RU RU98113300/04A patent/RU2194701C2/ru not_active IP Right Cessation
- 1996-12-13 AT AT96941787T patent/ATE203524T1/de active
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- 1996-12-13 BR BR9612043-6A patent/BR9612043A/pt not_active IP Right Cessation
- 1996-12-13 AU AU11061/97A patent/AU712370B2/en not_active Ceased
- 1996-12-13 IL IL12492596A patent/IL124925A0/xx not_active IP Right Cessation
- 1996-12-13 SK SK828-98A patent/SK282443B6/sk not_active IP Right Cessation
- 1996-12-17 TW TW085115569A patent/TW411274B/zh not_active IP Right Cessation
- 1996-12-17 MY MYPI96005309A patent/MY132405A/en unknown
- 1996-12-17 US US08/768,887 patent/US5962458A/en not_active Expired - Lifetime
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- 1998-05-28 MX MX9804247A patent/MX9804247A/es unknown
- 1998-06-17 NO NO19982784A patent/NO311358B1/no not_active IP Right Cessation
- 1998-12-02 US US09/203,764 patent/US6071921A/en not_active Expired - Lifetime
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