WO2010125216A3 - Preparación de compuestos 5,6-dihidropirido[2,3-d]pirimidin-7(8h)-ona sustituidos - Google Patents
Preparación de compuestos 5,6-dihidropirido[2,3-d]pirimidin-7(8h)-ona sustituidos Download PDFInfo
- Publication number
- WO2010125216A3 WO2010125216A3 PCT/ES2010/070238 ES2010070238W WO2010125216A3 WO 2010125216 A3 WO2010125216 A3 WO 2010125216A3 ES 2010070238 W ES2010070238 W ES 2010070238W WO 2010125216 A3 WO2010125216 A3 WO 2010125216A3
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- general formula
- dihydropyrido
- pyrimidin
- substituted
- compounds
- Prior art date
Links
- IEPKYYKIHJSXQJ-UHFFFAOYSA-N 6,8-dihydro-5h-pyrido[2,3-d]pyrimidin-7-one Chemical class N1=CN=C2NC(=O)CCC2=C1 IEPKYYKIHJSXQJ-UHFFFAOYSA-N 0.000 title abstract 2
- 238000002360 preparation method Methods 0.000 title abstract 2
- 239000000543 intermediate Substances 0.000 abstract 2
- CHJJGSNFBQVOTG-UHFFFAOYSA-N N-methyl-guanidine Natural products CNC(N)=N CHJJGSNFBQVOTG-UHFFFAOYSA-N 0.000 abstract 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- ZRALSGWEFCBTJO-UHFFFAOYSA-N anhydrous guanidine Natural products NC(N)=N ZRALSGWEFCBTJO-UHFFFAOYSA-N 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- SWSQBOPZIKWTGO-UHFFFAOYSA-N dimethylaminoamidine Natural products CN(C)C(N)=N SWSQBOPZIKWTGO-UHFFFAOYSA-N 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- -1 guanidine compound Chemical class 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
- FVSKHRXBFJPNKK-UHFFFAOYSA-N propionitrile Chemical compound CCC#N FVSKHRXBFJPNKK-UHFFFAOYSA-N 0.000 abstract 1
- 229940121649 protein inhibitor Drugs 0.000 abstract 1
- 239000012268 protein inhibitor Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C253/00—Preparation of carboxylic acid nitriles
- C07C253/30—Preparation of carboxylic acid nitriles by reactions not involving the formation of cyano groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C255/00—Carboxylic acid nitriles
- C07C255/01—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms
- C07C255/19—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms containing cyano groups and carboxyl groups, other than cyano groups, bound to the same saturated acyclic carbon skeleton
- C07C255/20—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms containing cyano groups and carboxyl groups, other than cyano groups, bound to the same saturated acyclic carbon skeleton the carbon skeleton being further substituted by singly-bound oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C255/00—Carboxylic acid nitriles
- C07C255/01—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms
- C07C255/23—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms containing cyano groups and carboxyl groups, other than cyano groups, bound to the same unsaturated acyclic carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
La invención describe un procedimiento para la preparación de compuestos 5,6-dihidropirido[2,3-d]pirimidin-7(8H)-ona sustituidos de fórmula general (3) útiles como inhibidores selectivos de las Proteína Quinasas, que comprende condensar un éster α,β-insaturado de fórmula general (4) con un propionitrilo de fórmula general (5) en presencia de una base concreta y hacer reaccionar el intermedio resultante con un compuesto guanidina de fórmula general (6) o una sal del mismo en presencia de otra base. La invención describe asimismo nuevos intermedios de síntesis de fórmula general (1) y de fórmula general (2).
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
ESP200901191 | 2009-04-29 | ||
ES200901191A ES2347630B1 (es) | 2009-04-29 | 2009-04-29 | Sintesis y usos de 4-cianopentanoatos y 4-cianopentenoatos sustituidos. |
Publications (2)
Publication Number | Publication Date |
---|---|
WO2010125216A2 WO2010125216A2 (es) | 2010-11-04 |
WO2010125216A3 true WO2010125216A3 (es) | 2012-12-27 |
Family
ID=42978783
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/ES2010/070238 WO2010125216A2 (es) | 2009-04-29 | 2010-04-19 | Preparación de compuestos 5,6-dihidropirido[2,3-d]pirimidin-7(8h)-ona sustituidos |
Country Status (2)
Country | Link |
---|---|
ES (1) | ES2347630B1 (es) |
WO (1) | WO2010125216A2 (es) |
Families Citing this family (21)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
CN107383009B (zh) | 2012-06-13 | 2020-06-09 | 因塞特控股公司 | 作为fgfr抑制剂的取代的三环化合物 |
WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
SG11201508328PA (en) | 2013-04-19 | 2015-11-27 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
CN107438607B (zh) | 2015-02-20 | 2021-02-05 | 因赛特公司 | 作为fgfr抑制剂的双环杂环 |
AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
CA3099116A1 (en) | 2018-05-04 | 2019-11-07 | Incyte Corporation | Salts of an fgfr inhibitor |
AU2019262195B2 (en) | 2018-05-04 | 2024-09-12 | Incyte Corporation | Solid forms of an FGFR inhibitor and processes for preparing the same |
US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
JP2022552324A (ja) | 2019-10-14 | 2022-12-15 | インサイト・コーポレイション | Fgfr阻害剤としての二環式複素環 |
US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
KR20220131900A (ko) | 2019-12-04 | 2022-09-29 | 인사이트 코포레이션 | Fgfr 억제제의 유도체 |
CA3163875A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
WO2021146424A1 (en) | 2020-01-15 | 2021-07-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
US12065494B2 (en) | 2021-04-12 | 2024-08-20 | Incyte Corporation | Combination therapy comprising an FGFR inhibitor and a Nectin-4 targeting agent |
JP2024522189A (ja) | 2021-06-09 | 2024-06-11 | インサイト・コーポレイション | Fgfr阻害剤としての三環式ヘテロ環 |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1996015128A2 (en) * | 1994-11-14 | 1996-05-23 | Warner-Lambert Company | 6-ARYL PYRIDO[2,3-d]PYRIMIDINES AND NAPHTHYRIDINES FOR INHIBITING PROTEIN TYROSINE KINASE MEDIATED CELLULAR PROLIFERATION |
-
2009
- 2009-04-29 ES ES200901191A patent/ES2347630B1/es not_active Expired - Fee Related
-
2010
- 2010-04-19 WO PCT/ES2010/070238 patent/WO2010125216A2/es active Application Filing
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1996015128A2 (en) * | 1994-11-14 | 1996-05-23 | Warner-Lambert Company | 6-ARYL PYRIDO[2,3-d]PYRIMIDINES AND NAPHTHYRIDINES FOR INHIBITING PROTEIN TYROSINE KINASE MEDIATED CELLULAR PROLIFERATION |
Non-Patent Citations (2)
Title |
---|
J L FALCO ET AL.: "Solid-phase synthesis of 2- substituted 4-amino-7-exo-5,6,7,8- tetrahydropyrido[2,3-d]pyrimidines: An example of cyclization-assisted cleavage", MOLECULAR DIVERSITY, vol. 6, 2003, pages 3 - 11 * |
N MONT ET AL.: "A one-pot microwave- assisted synthesis of pyrido[2,3-d]pyrimidines", MOLECULAR DIVERSITY, vol. 7, 2003, pages 153 - 159 * |
Also Published As
Publication number | Publication date |
---|---|
ES2347630A1 (es) | 2010-11-02 |
WO2010125216A2 (es) | 2010-11-04 |
ES2347630B1 (es) | 2011-09-08 |
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