PE20070114A1 - Inhibidor de tubulina y proceso para su preparacion - Google Patents
Inhibidor de tubulina y proceso para su preparacionInfo
- Publication number
- PE20070114A1 PE20070114A1 PE2006000657A PE2006000657A PE20070114A1 PE 20070114 A1 PE20070114 A1 PE 20070114A1 PE 2006000657 A PE2006000657 A PE 2006000657A PE 2006000657 A PE2006000657 A PE 2006000657A PE 20070114 A1 PE20070114 A1 PE 20070114A1
- Authority
- PE
- Peru
- Prior art keywords
- trifluoro
- pirazin
- react
- phenyl
- give
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 2
- 229940122429 Tubulin inhibitor Drugs 0.000 title 1
- 239000002904 solvent Substances 0.000 abstract 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 abstract 2
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 abstract 2
- OFOBLEOULBTSOW-UHFFFAOYSA-N Malonic acid Chemical compound OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 abstract 2
- BAVYZALUXZFZLV-UHFFFAOYSA-N Methylamine Chemical compound NC BAVYZALUXZFZLV-UHFFFAOYSA-N 0.000 abstract 2
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical compound [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 2
- 239000000010 aprotic solvent Substances 0.000 abstract 2
- XHXFXVLFKHQFAL-UHFFFAOYSA-N phosphoryl trichloride Chemical compound ClP(Cl)(Cl)=O XHXFXVLFKHQFAL-UHFFFAOYSA-N 0.000 abstract 2
- SNMLKBMPULDPTA-REOHCLBHSA-N (2s)-1,1,1-trifluoropropan-2-amine Chemical compound C[C@H](N)C(F)(F)F SNMLKBMPULDPTA-REOHCLBHSA-N 0.000 abstract 1
- -1 METHYLAMINO Chemical class 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 102000004243 Tubulin Human genes 0.000 abstract 1
- 108090000704 Tubulin Proteins 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 150000003863 ammonium salts Chemical class 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 239000012320 chlorinating reagent Substances 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000001530 fumaric acid Substances 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 150000007522 mineralic acids Chemical class 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
SE REFIERE AL COMPUESTO HEMIFUMARATO DE 6-CLORO-5-{2,6-DIFLUORO-4-[3-(METILAMINO)PROPOXI]FENIL}-2-PIRAZIN-2-IL-N-[(1S)-2,2,2-TRIFLUORO-1-METILETIL]PIRIMIDIN-4-AMINA Y SU PROCEDIMIENTO DE PREPARACION QUE CONSISTE EN: A) HACER REACCIONAR UN PIRAZINO-2-CARBONITRILOEN UNA BASE A EN UN ALCOHOL Y TRATAR CON UNA SAL DE AMONIO DE UN ACIDO INORGANICO PARA DAR UNA SAL DE ACIDO PIRAZINO-2-CARBOXIAMIDINA INORGANICA (A); B) HACER REACCIONAR (A) CON UN ESTER DE ACIDO MALONICO DE FORMULA I, DONDE R1 Y R2 SON CADA UNO ALQUILO C1-C3 EN UN SOLVENTE APROTICO EN PRESENCIA DE UNA BASE Y ACIDIFICAR PARA OBTENER 2-PIRAZIN-2-IL-5-(2,4,6-TRIFLUORO-FENIL)-PIRIMIDINO-4,6-DIOL (B); C) CLORINAR (B) CON OXICLORURO FOSFOROSO COMO REACTIVO DE CLORINACION EN PRESENCIA DE UNA AMINA BASE EN UN SOLVENTE APROTICO PARA DAR 4,6-DICLORO-2-PIRAZIN-2-IL-5-(2,4,6-TRIFLUORO-FENIL)-PIRIMIDINA (C); D) HACER REACCIONAR (C) CON (S)-2,2,2-TRIFLUORO-1-METIL-ETILAMINA EN UN SOLVENTE APROTICO PARA DAR 6-CLORO-2-PIRAZIN-2-IL-N-[(1S)-2,2,2-TRIFLUORO-1-METILETIL]-5-(2,4,6-TRIFLUOROFENIL)PIRIMIDIN-4-AMINA (D); E) HACER REACCIONAR 3-METILAMINO-PROPAN-1-OL CONBASE BEN UN SOLVENTE APROTICO Y ADICIONAR (D) PARA DAR 6-CLORO-5-{2,6-DIFLUORO-4-[3-(METILAMINO)PROPOXI]FENIL}-2-IL-N-[(1S)-2,2,2-TRIFLUORO-1-METILETIL]PIRIMIDIN-4-AMINA (E); F) HACER REACCIONAR (E) EN UN SOLVENTE APROTICO CON ACIDO FUMARICO EN UN ALCOHOL PARA OBTENER DICHO HEMIFUMARATO, EL CUAL ES UN INHIBIDOR DE TUBULINA UTIL EN EL TRATAMIENTO DE CANCER
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US69001605P | 2005-06-13 | 2005-06-13 | |
| US80278106P | 2006-05-24 | 2006-05-24 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20070114A1 true PE20070114A1 (es) | 2007-02-03 |
Family
ID=37074929
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2006000657A PE20070114A1 (es) | 2005-06-13 | 2006-06-13 | Inhibidor de tubulina y proceso para su preparacion |
Country Status (12)
| Country | Link |
|---|---|
| EP (1) | EP1891052A1 (es) |
| JP (1) | JP2008543838A (es) |
| AR (1) | AR054392A1 (es) |
| AU (1) | AU2006259663A1 (es) |
| BR (1) | BRPI0612145A2 (es) |
| CA (1) | CA2610416A1 (es) |
| GT (1) | GT200600257A (es) |
| MX (1) | MX2007015718A (es) |
| PE (1) | PE20070114A1 (es) |
| SV (1) | SV2007002573A (es) |
| TW (1) | TW200716613A (es) |
| WO (1) | WO2006138180A1 (es) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9163060B2 (en) | 2009-11-12 | 2015-10-20 | R&D Biopharmaceuticals Gmbh | Tubulin inhibitors |
| US9649317B2 (en) * | 2012-09-19 | 2017-05-16 | The Trustees Of The University Of Pennsylvania | Heterocyclic compounds and their use for the treatment of neurodegenerative tauopathies |
| WO2017181974A1 (zh) * | 2016-04-20 | 2017-10-26 | 苏州苏领生物医药有限公司 | 五元杂环类化合物及其制备方法、药物组合物和用途 |
| US11623927B2 (en) | 2018-03-02 | 2023-04-11 | The Trustees Of The University Of Pennsylvania | Substituted [1,2,4]triazolo[1,5-a]pyrimidines for stabilizing microtubules |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2007506746A (ja) * | 2003-09-24 | 2007-03-22 | ワイス・ホールディングズ・コーポレイション | 抗癌剤としての５−アリールピリミジン類 |
| WO2005030775A1 (en) * | 2003-09-24 | 2005-04-07 | Wyeth Holdings Corporation | 6-[(substituted)phenyl]triazolopyrimidines as anticancer agents |
-
2006
- 2006-06-08 CA CA002610416A patent/CA2610416A1/en not_active Abandoned
- 2006-06-08 MX MX2007015718A patent/MX2007015718A/es not_active Application Discontinuation
- 2006-06-08 WO PCT/US2006/022574 patent/WO2006138180A1/en not_active Ceased
- 2006-06-08 AU AU2006259663A patent/AU2006259663A1/en not_active Abandoned
- 2006-06-08 EP EP06784720A patent/EP1891052A1/en not_active Withdrawn
- 2006-06-08 JP JP2008516956A patent/JP2008543838A/ja not_active Withdrawn
- 2006-06-08 BR BRPI0612145-4A patent/BRPI0612145A2/pt not_active Application Discontinuation
- 2006-06-12 AR ARP060102470A patent/AR054392A1/es unknown
- 2006-06-12 TW TW095120855A patent/TW200716613A/zh unknown
- 2006-06-13 PE PE2006000657A patent/PE20070114A1/es not_active Application Discontinuation
- 2006-06-13 SV SV2006002573A patent/SV2007002573A/es not_active Application Discontinuation
- 2006-06-13 GT GT200600257A patent/GT200600257A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| MX2007015718A (es) | 2008-02-21 |
| TW200716613A (en) | 2007-05-01 |
| JP2008543838A (ja) | 2008-12-04 |
| SV2007002573A (es) | 2007-01-03 |
| AU2006259663A1 (en) | 2006-12-28 |
| WO2006138180A1 (en) | 2006-12-28 |
| CA2610416A1 (en) | 2006-12-28 |
| AR054392A1 (es) | 2007-06-20 |
| GT200600257A (es) | 2007-02-14 |
| BRPI0612145A2 (pt) | 2010-10-19 |
| EP1891052A1 (en) | 2008-02-27 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Refusal |