BRPI0414059B8 - síntese seletiva de pirimidinas substituídas em cf3 - Google Patents
síntese seletiva de pirimidinas substituídas em cf3Info
- Publication number
- BRPI0414059B8 BRPI0414059B8 BRPI0414059A BRPI0414059A BRPI0414059B8 BR PI0414059 B8 BRPI0414059 B8 BR PI0414059B8 BR PI0414059 A BRPI0414059 A BR PI0414059A BR PI0414059 A BRPI0414059 A BR PI0414059A BR PI0414059 B8 BRPI0414059 B8 BR PI0414059B8
- Authority
- BR
- Brazil
- Prior art keywords
- formula
- substituted pyrimidines
- selective synthesis
- compound
- hnr3r4
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Catalysts (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
síntese seletiva de pirimidinas substituídas em cf3. a presente invenção refere-se com um método de preparar um composto de fórmula (i) em que x1, x2 e r3-r4 são como aqui definido. o método inclui reagir um composto de fórmula (ii) com uma amina de fórmula (iii) (hnr3r4) na presença de um ácido de lewis e uma base não-nucleófila. a porção 2,4-diaminopirimidina é um componente comum em várias moléculas semelhantes a fármaco biologicamente ativas e verificou-se que derivados de pirimidina são úteis no tratamento de crescimento celular anormal, tal como câncer, em mamíferos.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US50073303P | 2003-09-05 | 2003-09-05 | |
| US60/500,733 | 2003-09-05 | ||
| PCT/IB2004/002744 WO2005023780A1 (en) | 2003-09-05 | 2004-08-24 | Selective synthesis of cf3-substituted pyrimidines |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| BRPI0414059A BRPI0414059A (pt) | 2006-10-24 |
| BRPI0414059B1 BRPI0414059B1 (pt) | 2018-11-06 |
| BRPI0414059B8 true BRPI0414059B8 (pt) | 2021-05-25 |
Family
ID=34272990
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0414059A BRPI0414059B8 (pt) | 2003-09-05 | 2004-08-24 | síntese seletiva de pirimidinas substituídas em cf3 |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US7122670B2 (pt) |
| EP (1) | EP1663991B1 (pt) |
| JP (1) | JP4842816B2 (pt) |
| KR (1) | KR100694732B1 (pt) |
| CN (1) | CN100465164C (pt) |
| AR (1) | AR045557A1 (pt) |
| BR (1) | BRPI0414059B8 (pt) |
| CA (1) | CA2537373C (pt) |
| CO (1) | CO5650237A2 (pt) |
| CY (1) | CY1106370T1 (pt) |
| DE (1) | DE602004004287T2 (pt) |
| DK (1) | DK1663991T3 (pt) |
| ES (1) | ES2276344T3 (pt) |
| IL (1) | IL173363A (pt) |
| MX (1) | MXPA06002552A (pt) |
| NO (1) | NO334383B1 (pt) |
| NZ (1) | NZ544969A (pt) |
| PL (1) | PL1663991T3 (pt) |
| PT (1) | PT1663991E (pt) |
| RU (1) | RU2315759C2 (pt) |
| TW (1) | TWI283667B (pt) |
| WO (1) | WO2005023780A1 (pt) |
| ZA (1) | ZA200600747B (pt) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH072586Y2 (ja) | 1988-11-25 | 1995-01-25 | 日東紡績株式会社 | ガラス繊維紡糸用冷却フィン装置 |
| PT1625121E (pt) * | 2002-12-20 | 2010-03-11 | Pfizer Prod Inc | Derivados de piridina para o tratamento de crescimento celular anormal |
| US20060205945A1 (en) * | 2004-05-14 | 2006-09-14 | Pfizer Inc | Pyrimidine derivatives for the treatment of abnormal cell growth |
| JP4778717B2 (ja) * | 2005-03-25 | 2011-09-21 | 富士フイルム株式会社 | 複素環式化合物の製造方法 |
| DE102007010801A1 (de) | 2007-03-02 | 2008-09-04 | Bayer Cropscience Ag | Diaminopyrimidine als Fungizide |
| AU2008240359B2 (en) * | 2007-04-18 | 2014-06-26 | Pfizer Products Inc. | Sulfonyl amide derivatives for the treatment of abnormal cell growth |
| KR101294731B1 (ko) * | 2007-06-04 | 2013-08-16 | 삼성디스플레이 주식회사 | 어레이 기판, 이를 갖는 표시패널 및 이의 제조방법 |
| WO2009115583A1 (en) * | 2008-03-20 | 2009-09-24 | Boehringer Ingelheim International Gmbh | Regioselective preparation of substituted pyrimidines |
| UY31714A (es) * | 2008-03-20 | 2009-11-10 | Boehringer Ingelheim Int | Preparación selectiva de pirimidinas sustituidas |
| DE102009006643A1 (de) | 2009-01-29 | 2010-08-05 | Saltigo Gmbh | Herstellung von halogenierten N-heteroaromatischen Polyhalogenderivaten |
| TW201100441A (en) | 2009-06-01 | 2011-01-01 | Osi Pharm Inc | Amino pyrimidine anticancer compounds |
| US8933227B2 (en) | 2009-08-14 | 2015-01-13 | Boehringer Ingelheim International Gmbh | Selective synthesis of functionalized pyrimidines |
| WO2011018517A1 (en) | 2009-08-14 | 2011-02-17 | Boehringer Ingelheim International Gmbh | Regioselective preparation of 2-amino-5-trifluoromethylpyrimidine derivatives |
| PL2646448T3 (pl) | 2010-11-29 | 2017-12-29 | OSI Pharmaceuticals, LLC | Makrocykliczne inhibitory kinazy |
| US8546443B2 (en) | 2010-12-21 | 2013-10-01 | Boehringer Ingelheim International Gmbh | Benzylic oxindole pyrimidines |
| US9174946B2 (en) | 2011-02-17 | 2015-11-03 | Cancer Therapeutics Crc Pty Ltd | Selective FAK inhibitors |
| ES2691673T3 (es) | 2011-02-17 | 2018-11-28 | Cancer Therapeutics Crc Pty Limited | Inhibidores de Fak |
| WO2014126954A1 (en) | 2013-02-13 | 2014-08-21 | OSI Pharmaceuticals, LLC | Regioselective synthesis of substituted pyrimidines |
| WO2015170600A1 (ja) * | 2014-05-08 | 2015-11-12 | 東ソー・エフテック株式会社 | ５－（トリフルオロメチル）ピリミジン誘導体及びその製造方法 |
| JP6391985B2 (ja) * | 2014-05-16 | 2018-09-19 | 東ソー・ファインケム株式会社 | ２−置換−４−（２，２，２−トリフルオロエトキシ）−５−（トリフルオロメチル）ピリミジン誘導体及びその製造方法 |
| JP6391988B2 (ja) * | 2014-05-21 | 2018-09-19 | 東ソー・ファインケム株式会社 | ５−（トリフルオロメチル）ピリミジン誘導体の製造方法及び新規５−（トリフルオロメチル）ピリミジン誘導体 |
| CN108440499A (zh) * | 2018-03-22 | 2018-08-24 | 盐城师范学院 | 一种色瑞替尼及其关键中间体的制备方法 |
| CN114213339B (zh) * | 2021-12-20 | 2023-10-31 | 苏州康纯医药科技有限公司 | 一种表皮细胞生长因子受体突变抑制剂的制备方法 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2896532B2 (ja) * | 1994-08-13 | 1999-05-31 | ユーハン コーポレーション | 新規なピリミジン誘導体およびその製造方法 |
| WO2003030909A1 (en) * | 2001-09-25 | 2003-04-17 | Bayer Pharmaceuticals Corporation | 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer |
| JP4460292B2 (ja) * | 2001-10-17 | 2010-05-12 | ベーリンガー インゲルハイム ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト | ピリミジン誘導体、これらの化合物を含む医薬組成物、その使用及びその調製方法 |
-
2004
- 2004-08-24 EP EP04769170A patent/EP1663991B1/en not_active Expired - Lifetime
- 2004-08-24 RU RU2006106727/04A patent/RU2315759C2/ru not_active IP Right Cessation
- 2004-08-24 CN CNB2004800254318A patent/CN100465164C/zh not_active Expired - Lifetime
- 2004-08-24 JP JP2006525198A patent/JP4842816B2/ja not_active Expired - Lifetime
- 2004-08-24 WO PCT/IB2004/002744 patent/WO2005023780A1/en not_active Ceased
- 2004-08-24 KR KR1020067004428A patent/KR100694732B1/ko not_active Expired - Lifetime
- 2004-08-24 PT PT04769170T patent/PT1663991E/pt unknown
- 2004-08-24 CA CA002537373A patent/CA2537373C/en not_active Expired - Lifetime
- 2004-08-24 DK DK04769170T patent/DK1663991T3/da active
- 2004-08-24 NZ NZ544969A patent/NZ544969A/en not_active IP Right Cessation
- 2004-08-24 PL PL04769170T patent/PL1663991T3/pl unknown
- 2004-08-24 BR BRPI0414059A patent/BRPI0414059B8/pt not_active IP Right Cessation
- 2004-08-24 ES ES04769170T patent/ES2276344T3/es not_active Expired - Lifetime
- 2004-08-24 DE DE602004004287T patent/DE602004004287T2/de not_active Expired - Lifetime
- 2004-08-24 MX MXPA06002552A patent/MXPA06002552A/es active IP Right Grant
- 2004-08-27 US US10/928,954 patent/US7122670B2/en not_active Expired - Lifetime
- 2004-09-02 AR ARP040103140A patent/AR045557A1/es not_active Application Discontinuation
- 2004-09-03 TW TW093126748A patent/TWI283667B/zh not_active IP Right Cessation
-
2006
- 2006-01-25 IL IL173363A patent/IL173363A/en active IP Right Grant
- 2006-01-26 ZA ZA200600747A patent/ZA200600747B/xx unknown
- 2006-02-23 CO CO06018320A patent/CO5650237A2/es not_active Application Discontinuation
- 2006-04-03 NO NO20061509A patent/NO334383B1/no unknown
-
2007
- 2007-03-12 CY CY20071100341T patent/CY1106370T1/el unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B06F | Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette] | ||
| B15K | Others concerning applications: alteration of classification |
Free format text: "PARA: INT. CL. C07D 239/42 Ipc: C07D 239/42 (2011.01), A61P 35/00 (2011.01) Free format text: PARA: INT. CL. C07D 239/42; A61P 35/00 Ipc: C07D 239/42 (2011.01), A61P 35/00 (2011.01) |
|
| B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] | ||
| B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] | ||
| B09A | Decision: intention to grant [chapter 9.1 patent gazette] | ||
| B16A | Patent or certificate of addition of invention granted [chapter 16.1 patent gazette] |
Free format text: PRAZO DE VALIDADE: 10 (DEZ) ANOS CONTADOS A PARTIR DE 06/11/2018, OBSERVADAS AS CONDICOES LEGAIS. |
|
| B16C | Correction of notification of the grant [chapter 16.3 patent gazette] |
Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 24/08/2004 OBSERVADAS AS CONDICOES LEGAIS. PATENTE CONCEDIDA CONFORME ADI 5.529/DF |
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| B21F | Lapse acc. art. 78, item iv - on non-payment of the annual fees in time |
Free format text: REFERENTE A 21A ANUIDADE. |
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| B24J | Lapse because of non-payment of annual fees (definitively: art 78 iv lpi, resolution 113/2013 art. 12) |
Free format text: EM VIRTUDE DA EXTINCAO PUBLICADA NA RPI 2844 DE 08-07-2025 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDA A EXTINCAO DA PATENTE E SEUS CERTIFICADOS, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013. |