BRPI0519085A2 - processos para a fabricaÇço de azd0530 e para a fabricaÇço de uma quinazolina, intermediÁrio, processo para a fabricaÇço de quinazolinona, forma cristalina substancialmente homogÊnea de 4-(6-cloro 2, 3-metileno-diàxi-anilino) - 7 - {2- (4-metil-piperazin -1- il) - etàxi} - 5 - tetraidropiran - 4-il- àxi - quinazolina, e, composiÇço farmacÊutica - Google Patents
processos para a fabricaÇço de azd0530 e para a fabricaÇço de uma quinazolina, intermediÁrio, processo para a fabricaÇço de quinazolinona, forma cristalina substancialmente homogÊnea de 4-(6-cloro 2, 3-metileno-diàxi-anilino) - 7 - {2- (4-metil-piperazin -1- il) - etàxi} - 5 - tetraidropiran - 4-il- àxi - quinazolina, e, composiÇço farmacÊuticaInfo
- Publication number
- BRPI0519085A2 BRPI0519085A2 BRPI0519085-1A BRPI0519085A BRPI0519085A2 BR PI0519085 A2 BRPI0519085 A2 BR PI0519085A2 BR PI0519085 A BRPI0519085 A BR PI0519085A BR PI0519085 A2 BRPI0519085 A2 BR PI0519085A2
- Authority
- BR
- Brazil
- Prior art keywords
- manufacture
- quinazoline
- processes
- piperazin
- chloro
- Prior art date
Links
- 238000004519 manufacturing process Methods 0.000 title abstract 9
- 238000000034 method Methods 0.000 title abstract 5
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 3
- AVRPFRMDMNDIDH-UHFFFAOYSA-N 1h-quinazolin-2-one Chemical compound C1=CC=CC2=NC(O)=NC=C21 AVRPFRMDMNDIDH-UHFFFAOYSA-N 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
- OUKYUETWWIPKQR-UHFFFAOYSA-N saracatinib Chemical compound C1CN(C)CCN1CCOC1=CC(OC2CCOCC2)=C(C(NC=2C(=CC=C3OCOC3=2)Cl)=NC=N2)C2=C1 OUKYUETWWIPKQR-UHFFFAOYSA-N 0.000 title 1
- 229950009919 saracatinib Drugs 0.000 title 1
- 239000000543 intermediate Substances 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004195 4-methylpiperazin-1-yl group Chemical group [H]C([H])([H])N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 abstract 1
- 238000001311 chemical methods and process Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 150000004684 trihydrates Chemical class 0.000 abstract 1
Classifications
-
- 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
- C07D405/14—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 three or more hetero rings
-
- 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
-
- 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
PROCESSOS PARA A FABRICAÇçO DE AZDO53O E PARA A FABRICAÇçO DE UMA QUINAZOLINA, INTERMEDIÁRIO, PROCESSO PARA A FABRICAÇçO DE QUINAZOLINONA, FORMA CRISTALINA SUBSTANCIALMENTE HOMOGÊNEA DE 4-(6- CLORO-2,3 -METILENO-DIàXI-ANILINO)-7- [2-(4-METIL-PIPERAZIN- 1 -IL)-ETàXI]-5-TETRAIDROPIRAN-4-IL-àXI-QUINAZOLINA, E, COMPOSIÇçO FARMACÊUTICA. A presente invenção refere-se aos processos químicos úteis na fabricação do composto 4-(6-cloro-2,3 -metileno-dióxi-anilino)-7- [2-(4-metil- piperazin- 1 -il)-etóxi]-5-tetraidropiran-4-il-óxi-quinazolina (a entidade ativa dentro de AZDO53O), aos intermediários úteis na fabricação daquele composto e aos processos para a fabricação daqueles intermediários. A invenção também se refere às formas cristalinas específicas daquele composto tal como um sal de difumarato e um tri-hidrato e às composições farmacêuticas contendo tais formas cristalinas.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0427697.8A GB0427697D0 (en) | 2004-12-17 | 2004-12-17 | Chemical process |
| PCT/GB2005/004807 WO2006064217A2 (en) | 2004-12-17 | 2005-12-14 | PROCESS FOR THE PREPARATION OF 4-(6-CHLORO-2, 3-METHYLENEDIOXYANILINO)-7-[2-(4-METHYLPIPERAZIN-l-YL) ETHOXY]-5-TETRAHYDROPYRAN-4-YLOXYQUINAZOLINE , THEIR INTERMEDIATES AND CRYSTALLINE SALTS THEREOF |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0519085A2 true BRPI0519085A2 (pt) | 2008-12-23 |
Family
ID=34090249
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0519085-1A BRPI0519085A2 (pt) | 2004-12-17 | 2005-12-14 | processos para a fabricaÇço de azd0530 e para a fabricaÇço de uma quinazolina, intermediÁrio, processo para a fabricaÇço de quinazolinona, forma cristalina substancialmente homogÊnea de 4-(6-cloro 2, 3-metileno-diàxi-anilino) - 7 - {2- (4-metil-piperazin -1- il) - etàxi} - 5 - tetraidropiran - 4-il- àxi - quinazolina, e, composiÇço farmacÊutica |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US8304417B2 (pt) |
| EP (1) | EP1871769B1 (pt) |
| JP (2) | JP5161584B2 (pt) |
| KR (6) | KR20070090004A (pt) |
| CN (1) | CN101115744B (pt) |
| AU (2) | AU2005315458B2 (pt) |
| BR (1) | BRPI0519085A2 (pt) |
| CA (2) | CA2590735C (pt) |
| ES (1) | ES2622480T3 (pt) |
| GB (1) | GB0427697D0 (pt) |
| IL (1) | IL183525A0 (pt) |
| MX (1) | MX2007007210A (pt) |
| NO (1) | NO20072755L (pt) |
| NZ (1) | NZ555468A (pt) |
| WO (1) | WO2006064217A2 (pt) |
| ZA (1) | ZA200704532B (pt) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0412074D0 (en) * | 2004-05-29 | 2004-06-30 | Astrazeneca Ab | Combination product |
| WO2009068906A2 (en) * | 2007-11-26 | 2009-06-04 | Astrazeneca Ab | Combinations comprising zd4054 and a src family kinase inhibitor 172 |
| CN103275072B (zh) * | 2013-05-22 | 2016-01-20 | 苏州明锐医药科技有限公司 | 塞卡替尼的制备方法 |
| US10660957B2 (en) * | 2013-06-13 | 2020-05-26 | Yale University | Compositions and methods for treating an Aβ-modulated disease or disorder or improving cognition in a subject |
| US11241434B2 (en) | 2013-06-13 | 2022-02-08 | Yale Uninversity | Compositions and methods for improving cognition in a subject |
| WO2016130897A1 (en) | 2015-02-13 | 2016-08-18 | Yu Paul B | Methods and compositions for the treatment or prevention of abnormal bone formation in a soft tissue |
| FI3930715T3 (fi) | 2019-02-27 | 2024-08-05 | Astrazeneca Ab | Sarakatinibi käytettäväksi idiopaattisen keuhkofibroosin hoidossa |
| CN116332789A (zh) * | 2023-03-10 | 2023-06-27 | 上海康鹏科技股份有限公司 | 一种4-氨基-2-氟苯甲酰胺的制备方法 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA73993C2 (uk) * | 2000-06-06 | 2005-10-17 | Астразенека Аб | Хіназолінові похідні для лікування пухлин та фармацевтична композиція |
| AU2001278609B2 (en) | 2000-08-21 | 2005-04-14 | Astrazeneca Ab | Quinazoline derivatives |
| ATE409185T1 (de) | 2001-04-19 | 2008-10-15 | Astrazeneca Ab | Chinazolin derivate |
| RU2350618C2 (ru) * | 2002-11-04 | 2009-03-27 | Астразенека Аб | ПРОИЗВОДНЫЕ ХИНАЗОЛИНА В КАЧЕСТВЕ ИНГИБИТОРОВ Src ТИРОЗИНКИНАЗЫ |
| GB0226434D0 (en) | 2002-11-13 | 2002-12-18 | Astrazeneca Ab | Combination product |
| GB0307333D0 (en) | 2003-03-29 | 2003-05-07 | Astrazeneca Ab | Therapeutic agent |
| GB0309850D0 (en) * | 2003-04-30 | 2003-06-04 | Astrazeneca Ab | Quinazoline derivatives |
| GB0310401D0 (en) * | 2003-05-07 | 2003-06-11 | Astrazeneca Ab | Therapeutic agent |
-
2004
- 2004-12-17 GB GBGB0427697.8A patent/GB0427697D0/en not_active Ceased
-
2005
- 2005-12-14 KR KR1020077015972A patent/KR20070090004A/ko not_active Ceased
- 2005-12-14 WO PCT/GB2005/004807 patent/WO2006064217A2/en not_active Ceased
- 2005-12-14 CA CA002590735A patent/CA2590735C/en not_active Expired - Lifetime
- 2005-12-14 NZ NZ555468A patent/NZ555468A/en not_active IP Right Cessation
- 2005-12-14 ES ES05818127.2T patent/ES2622480T3/es not_active Expired - Lifetime
- 2005-12-14 MX MX2007007210A patent/MX2007007210A/es not_active Application Discontinuation
- 2005-12-14 CA CA002675642A patent/CA2675642A1/en not_active Abandoned
- 2005-12-14 AU AU2005315458A patent/AU2005315458B2/en not_active Expired
- 2005-12-14 US US11/793,064 patent/US8304417B2/en active Active
- 2005-12-14 KR KR1020087023973A patent/KR20080094849A/ko not_active Withdrawn
- 2005-12-14 BR BRPI0519085-1A patent/BRPI0519085A2/pt not_active IP Right Cessation
- 2005-12-14 EP EP05818127.2A patent/EP1871769B1/en not_active Expired - Lifetime
- 2005-12-14 JP JP2007546172A patent/JP5161584B2/ja not_active Expired - Lifetime
- 2005-12-14 CN CN2005800476248A patent/CN101115744B/zh not_active Expired - Lifetime
- 2005-12-14 KR KR1020087023969A patent/KR20080094846A/ko not_active Withdrawn
- 2005-12-14 KR KR1020087023972A patent/KR20080094848A/ko not_active Withdrawn
- 2005-12-14 KR KR1020087023971A patent/KR20080094847A/ko not_active Withdrawn
- 2005-12-14 KR KR1020117022793A patent/KR20110114727A/ko not_active Ceased
-
2007
- 2007-05-29 IL IL183525A patent/IL183525A0/en unknown
- 2007-05-30 NO NO20072755A patent/NO20072755L/no not_active Application Discontinuation
- 2007-05-31 ZA ZA200704532A patent/ZA200704532B/en unknown
-
2008
- 2008-12-15 JP JP2008318186A patent/JP2009143920A/ja active Pending
-
2009
- 2009-02-18 AU AU2009200622A patent/AU2009200622A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| AU2009200622A1 (en) | 2009-03-12 |
| US8304417B2 (en) | 2012-11-06 |
| US20090099196A1 (en) | 2009-04-16 |
| KR20080094847A (ko) | 2008-10-24 |
| JP2008524183A (ja) | 2008-07-10 |
| ZA200704532B (en) | 2008-07-30 |
| KR20070090004A (ko) | 2007-09-04 |
| MX2007007210A (es) | 2007-11-07 |
| EP1871769B1 (en) | 2017-02-22 |
| NZ555468A (en) | 2010-12-24 |
| NO20072755L (no) | 2007-07-02 |
| JP5161584B2 (ja) | 2013-03-13 |
| EP1871769A2 (en) | 2008-01-02 |
| KR20110114727A (ko) | 2011-10-19 |
| CN101115744A (zh) | 2008-01-30 |
| AU2005315458B2 (en) | 2009-03-12 |
| KR20080094846A (ko) | 2008-10-24 |
| KR20080094849A (ko) | 2008-10-24 |
| WO2006064217A3 (en) | 2006-12-21 |
| WO2006064217A8 (en) | 2007-07-05 |
| CN101115744B (zh) | 2012-02-01 |
| IL183525A0 (en) | 2007-09-20 |
| WO2006064217A2 (en) | 2006-06-22 |
| ES2622480T3 (es) | 2017-07-06 |
| CA2590735A1 (en) | 2006-06-22 |
| KR20080094848A (ko) | 2008-10-24 |
| GB0427697D0 (en) | 2005-01-19 |
| JP2009143920A (ja) | 2009-07-02 |
| CA2590735C (en) | 2009-11-10 |
| CA2675642A1 (en) | 2006-06-22 |
| AU2005315458A1 (en) | 2006-06-22 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE A 8A ANUIDADE. |
|
| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2260 DE 29/04/2014. |