PE20121815A1 - Compuestos de pirrolo-pirimidina como inhibidores de cdk4/6 - Google Patents

Compuestos de pirrolo-pirimidina como inhibidores de cdk4/6

Info

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
Application number
PE2012001259A
Other languages
English (en)
Inventor
Christopher Thomas Brain
Young Shin Cho
Jhon William Giraldes
Bharat Lagu
Julian Levell
Michael LUZZIO
Lawrence Blas Perez
Yaping Wang
Fan Yang
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20121815A1 publication Critical patent/PE20121815A1/es

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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
    • 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

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  • 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)
  • Saccharide Compounds (AREA)
  • Plural Heterocyclic 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
PE2012001259A 2010-02-19 2011-02-17 Compuestos de pirrolo-pirimidina como inhibidores de cdk4/6 PE20121815A1 (es)

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

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PE2012001259A PE20121815A1 (es) 2010-02-19 2011-02-17 Compuestos de pirrolo-pirimidina como inhibidores de cdk4/6

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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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