PE20120575A1 - Derivados de pirazolopirimidina como inhibidores de jak quinasas - Google Patents

Derivados de pirazolopirimidina como inhibidores de jak quinasas

Info

Publication number
PE20120575A1
PE20120575A1 PE2012000003A PE2012000003A PE20120575A1 PE 20120575 A1 PE20120575 A1 PE 20120575A1 PE 2012000003 A PE2012000003 A PE 2012000003A PE 2012000003 A PE2012000003 A PE 2012000003A PE 20120575 A1 PE20120575 A1 PE 20120575A1
Authority
PE
Peru
Prior art keywords
alkyl
carboxamide
pyrazole
pyrimidine
inhibitors
Prior art date
Application number
PE2012000003A
Other languages
English (en)
Inventor
Paul Gibbons
Emily Hanan
Wendy Liu
Joseph P Lyssikatos
Steven R Magnuson
Rohan Mendonca
Richard Pastor
Thomas E Rawson
Michael Siu
Mark E Zak
Aihe Zhou
Bing-Yan Zhu
Original Assignee
Genentech Inc
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 Genentech Inc filed Critical Genentech Inc
Publication of PE20120575A1 publication Critical patent/PE20120575A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

REFERIDA A UN COMPUESTO DERIVADO DE PIRAZOLOPIRIMIDINA DE FORMULA (I), DONDE R1 ES H, ALQUILO C1-C6, OR6, NR6R7 O HALOGENO; R2 ES UN HETEROARILO DE 5 O 6 MIEMBROS OPCIONALMENTE SUSTITUIDO CON R4; R3 ES FENILO, CICLOALQUILO C3-C6, HETEROCICLILO DE 3 A 10 MIEMBROS, ENTRE OTROS; R4 ES ALQUILO C1-C6, ALQUENILO C2-C6, ALQUINILO C2-C6, ENTRE OTROS; R6 Y R7 SON H, ALQUILO C1-C6, ALQUINILO C2-C6, CN, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N-(3-(5-CLORO-2-METOXIFENIL)-1-METIL-1H-PIRAZOL-4-IL)PIRAZOLO[1,5-a]PIRIMIDINA-3-CARBOXAMIDA, N-(5-(5-CLORO-2-METOXIFENIL)-1-METIL-1H-PIRAZOL-4-IL)PIRAZOLO[1,5-a]PIRIMIDINA-3-CARBOXAMIDA, N-(3-(2,5-DIMETILOFENIL)-1-METIL-1H-PIRAZOL-4-IL)PIRAZOLO[1,5-a]PIRIMIDINA-3-CARBOXAMIDA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS INHIBEN UNA O MAS JANUS QUINASAS Y SON UTILES EN EL TRATAMIENTO DE CANCER, POLICITEMIA VERA, MIELOFIBROSIS, ENFERMEDAD DE CHRON, ARTRITIS REUMATOIDE, TROMBOCITOSIS PRIMARIA, ENTRE OTROS
PE2012000003A 2009-07-02 2010-07-02 Derivados de pirazolopirimidina como inhibidores de jak quinasas PE20120575A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US22291809P 2009-07-02 2009-07-02

Publications (1)

Publication Number Publication Date
PE20120575A1 true PE20120575A1 (es) 2012-05-25

Family

ID=43411778

Family Applications (2)

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PE2015000692A PE20151249A1 (es) 2009-07-02 2010-07-02 Derivados de pirazolopirimidina como inhibidores de jak quinasas
PE2012000003A PE20120575A1 (es) 2009-07-02 2010-07-02 Derivados de pirazolopirimidina como inhibidores de jak quinasas

Family Applications Before (1)

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Country Status (35)

Country Link
US (6) US8999998B2 (es)
EP (3) EP2448941B1 (es)
JP (4) JP5769261B2 (es)
KR (3) KR20180108858A (es)
CN (2) CN102482284B (es)
AU (1) AU2010266188B2 (es)
BR (1) BRPI1010197A2 (es)
CA (1) CA2767097A1 (es)
CL (1) CL2012000001A1 (es)
CO (1) CO6491081A2 (es)
CR (2) CR20170115A (es)
DK (1) DK2448941T3 (es)
EC (1) ECSP12011645A (es)
ES (1) ES2657839T3 (es)
HR (1) HRP20180157T1 (es)
HU (1) HUE035537T2 (es)
IL (3) IL217224B (es)
IN (1) IN2012DN00755A (es)
LT (1) LT2448941T (es)
MA (1) MA33502B1 (es)
MX (1) MX2012000169A (es)
MY (1) MY160156A (es)
NO (1) NO2448941T3 (es)
NZ (4) NZ706218A (es)
PE (2) PE20151249A1 (es)
PH (1) PH12015500666A1 (es)
PL (1) PL2448941T3 (es)
PT (1) PT2448941T (es)
RS (1) RS56671B1 (es)
RU (2) RU2567238C2 (es)
SG (2) SG10201509607XA (es)
SI (1) SI2448941T1 (es)
UA (1) UA110324C2 (es)
WO (1) WO2011003065A2 (es)
ZA (2) ZA201200490B (es)

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