PE20121815A1 - Compuestos de pirrolo-pirimidina como inhibidores de cdk4/6 - Google Patents
Compuestos de pirrolo-pirimidina como inhibidores de cdk4/6Info
- Publication number
- PE20121815A1 PE20121815A1 PE2012001259A PE2012001259A PE20121815A1 PE 20121815 A1 PE20121815 A1 PE 20121815A1 PE 2012001259 A PE2012001259 A PE 2012001259A PE 2012001259 A PE2012001259 A PE 2012001259A PE 20121815 A1 PE20121815 A1 PE 20121815A1
- Authority
- PE
- Peru
- Prior art keywords
- pirrolo
- alkyl
- cyclopentil
- pyrimidin
- pyridin
- Prior art date
Links
- 229940124297 CDK 4/6 inhibitor Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 abstract 2
- 229910052805 deuterium Inorganic materials 0.000 abstract 2
- -1 9-HYDROXY-1,5,7-TRIMETHYL-3,7-DIAZABICYCLO- [3.3.1] -NONAN-3-CARBONYL Chemical class 0.000 abstract 1
- 102000013701 Cyclin-Dependent Kinase 4 Human genes 0.000 abstract 1
- 108010025464 Cyclin-Dependent Kinase 4 Proteins 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical group [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 230000001419 dependent effect Effects 0.000 abstract 1
- QKIUAMUSENSFQQ-UHFFFAOYSA-N dimethylazanide Chemical compound C[N-]C QKIUAMUSENSFQQ-UHFFFAOYSA-N 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- JTJMJGYZQZDUJJ-UHFFFAOYSA-N phencyclidine Chemical compound C1CCCCN1C1(C=2C=CC=CC=2)CCCCC1 JTJMJGYZQZDUJJ-UHFFFAOYSA-N 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61P35/02—Antineoplastic agents specific for leukemia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/002—Heterocyclic compounds
-
- 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
-
- 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
- C07D471/08—Bridged systems
-
- 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
- C07D471/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/20—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
- Saccharide Compounds (AREA)
Abstract
SE REFIERE A COMPUESTOS DERIVADOS DE PIRROLO-PIRIMIDINA DE FORMULA (I) DONDE A ES CH O N; L ES UN ENLACE, C(O) O S(O)2; R1 ES ALQUILO(C3-C7), CICLOALQUILO(C3-C7) OPCIONALMENTE SUSTITUIDO CON ALQUILO(C1-C6) O OH, FENILO OPCIONALMENTE SUSTITUIDO CON ALQUILO(C1-C6), C(CH3)2CN U OH, ENTRE OTROS; R11 ES H O ALQUILO(C1-C4); R2Y ES UN COMPUESTO DE FORMULA (a), (b), ENTRE OTROS, EN DONDE V ES NH O CH2; R4 ES H, DEUTERIO, C(R5)-(R6)-(R7), EN DONDE R5, R6, R7, R8, R9 Y R10 SON CADA UNO H O DEUTERIO. SON COMPUESTOS PREFERIDOS: CICLOPENTIL-2-(5-(9-HIDROXI-1,5,7-TRIMETIL-3,7-DIAZABICICLO-[3.3.1]-NONAN-3-CARBONIL)-PIRIDIN-2-IL-AMINO)-N,N-DIMETIL-7H-PIRROLO-[2,3-d]-PIRIMIDIN-6-CARBOXAMIDA; DIMETIL-AMIDA DEL ACIDO 7-CICLOPENTIL-2-[5-(8-METIL-3,8-DIAZA-BICICLO-[3.2.1]-OCTAN-3-CARBONIL)-PIRIDIN-2-IL-AMINO]-7H-PIRROLO-[2,3-d]-PIRIMIDIN-6-CARBOXILICO; 7-CICLOPENTIL-N,N-DIMETIL-2-(5-((3aS,6aR)-1-OXOHEXAHIDRO-PIRROLO-[3,4-c]-PIRROL-2(1H)-IL)-PIRIDIN-2-IL-AMINO)-7H-PIRROLO-[2,3-d]-PIRIMIDIN-6-CARBOXAMIDA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE QUINASAS DEPENDIENTES DE CICLINA 4 Y 6 (CDK4/6) SIENDO UTILES EN EL TRATAMIENTO DEL CANCER
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30624810P | 2010-02-19 | 2010-02-19 | |
| US201161429372P | 2011-01-03 | 2011-01-03 | |
| US201161429997P | 2011-01-05 | 2011-01-05 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20121815A1 true PE20121815A1 (es) | 2013-02-03 |
Family
ID=44201966
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2012001259A PE20121815A1 (es) | 2010-02-19 | 2011-02-17 | Compuestos de pirrolo-pirimidina como inhibidores de cdk4/6 |
Country Status (38)
| Country | Link |
|---|---|
| US (2) | US8957074B2 (es) |
| EP (1) | EP2536730B1 (es) |
| JP (1) | JP5788415B2 (es) |
| KR (1) | KR101812357B1 (es) |
| CN (1) | CN102918043B (es) |
| AR (1) | AR080198A1 (es) |
| AU (1) | AU2011217286B2 (es) |
| BR (1) | BR112012020922B1 (es) |
| CA (1) | CA2790637C (es) |
| CL (1) | CL2012002270A1 (es) |
| DK (1) | DK2536730T3 (es) |
| DO (1) | DOP2012000225A (es) |
| EA (1) | EA022355B1 (es) |
| EC (1) | ECSP12012111A (es) |
| ES (1) | ES2548532T3 (es) |
| GE (1) | GEP20146146B (es) |
| HN (1) | HN2012001744A (es) |
| HR (1) | HRP20151071T1 (es) |
| IL (1) | IL221520A (es) |
| MA (1) | MA34066B1 (es) |
| ME (1) | ME02202B (es) |
| MX (1) | MX2012009613A (es) |
| NI (1) | NI201200135A (es) |
| NZ (1) | NZ601754A (es) |
| PE (1) | PE20121815A1 (es) |
| PH (1) | PH12012501649A1 (es) |
| PL (1) | PL2536730T3 (es) |
| PT (1) | PT2536730E (es) |
| RS (1) | RS54263B1 (es) |
| SG (1) | SG183218A1 (es) |
| SI (1) | SI2536730T1 (es) |
| SM (1) | SMT201500265B (es) |
| TN (1) | TN2012000413A1 (es) |
| TW (1) | TWI503322B (es) |
| UA (1) | UA108369C2 (es) |
| UY (1) | UY33227A (es) |
| WO (1) | WO2011101409A1 (es) |
| ZA (1) | ZA201206079B (es) |
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