CL2011002956A1 - Compuestos derivados de pirrolo[2,3-d]pirimidina, inhibidores de la quinasa janus (jak1); composicion farmaceutica; y uso para el tratamiento de una enfermedad autoinmune, cancer, trastorno mieloproliferativo, una enfermedad inflamatoria o rechazo de trasplante de organos. - Google Patents

Compuestos derivados de pirrolo[2,3-d]pirimidina, inhibidores de la quinasa janus (jak1); composicion farmaceutica; y uso para el tratamiento de una enfermedad autoinmune, cancer, trastorno mieloproliferativo, una enfermedad inflamatoria o rechazo de trasplante de organos.

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Publication number
CL2011002956A1
CL2011002956A1 CL2011002956A CL2011002956A CL2011002956A1 CL 2011002956 A1 CL2011002956 A1 CL 2011002956A1 CL 2011002956 A CL2011002956 A CL 2011002956A CL 2011002956 A CL2011002956 A CL 2011002956A CL 2011002956 A1 CL2011002956 A1 CL 2011002956A1
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CL
Chile
Prior art keywords
pyrrolo
pyrimidine
inhibitors
cancer
treatment
Prior art date
Application number
CL2011002956A
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English (en)
Inventor
James D Rodgers
Stacey Shepard
Argyrios G Arvanitis
Haisheng Wang
Louis Storage
Beverly Folmer
Lixin Shao
Wenyu Zhu
Joseph P Glenn
Original Assignee
Incyte Holdings Corp
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42543342&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CL2011002956(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Incyte Holdings Corp filed Critical Incyte Holdings Corp
Publication of CL2011002956A1 publication Critical patent/CL2011002956A1/es

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    • 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
    • A61K31/495Heterocyclic 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
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    • A61P19/00Drugs for skeletal disorders
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61P35/00Antineoplastic agents
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    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
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    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
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    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
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Abstract

Compuestos derivados de pirrolo[2,3-d]pirimidina, inhibidores de la quinasa janus; composición farmacéutica; y uso para el tratamiento de una enfermedad autoinmune, cáncer, trastorno mieloproliferativo, una enfermedad inflamatoria o rechazo de trasplante de órganos.
CL2011002956A 2009-05-22 2011-11-22 Compuestos derivados de pirrolo[2,3-d]pirimidina, inhibidores de la quinasa janus (jak1); composicion farmaceutica; y uso para el tratamiento de una enfermedad autoinmune, cancer, trastorno mieloproliferativo, una enfermedad inflamatoria o rechazo de trasplante de organos. CL2011002956A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US18062209P 2009-05-22 2009-05-22
US22509209P 2009-07-13 2009-07-13

Publications (1)

Publication Number Publication Date
CL2011002956A1 true CL2011002956A1 (es) 2012-05-25

Family

ID=42543342

Family Applications (1)

Application Number Title Priority Date Filing Date
CL2011002956A CL2011002956A1 (es) 2009-05-22 2011-11-22 Compuestos derivados de pirrolo[2,3-d]pirimidina, inhibidores de la quinasa janus (jak1); composicion farmaceutica; y uso para el tratamiento de una enfermedad autoinmune, cancer, trastorno mieloproliferativo, una enfermedad inflamatoria o rechazo de trasplante de organos.

Country Status (22)

Country Link
US (2) US8716303B2 (es)
EP (1) EP2432555B1 (es)
JP (1) JP5775070B2 (es)
KR (1) KR101771401B1 (es)
CN (1) CN102458581B (es)
AR (1) AR076794A1 (es)
AU (1) AU2010249380B2 (es)
BR (1) BRPI1012159B1 (es)
CA (1) CA2762174C (es)
CL (1) CL2011002956A1 (es)
CO (1) CO6440524A2 (es)
CR (1) CR20110620A (es)
EA (1) EA025520B1 (es)
ES (1) ES2487542T3 (es)
IL (1) IL216463A (es)
MX (1) MX2011012353A (es)
MY (1) MY156727A (es)
NZ (1) NZ596479A (es)
SG (1) SG176130A1 (es)
TW (1) TW201100429A (es)
WO (1) WO2010135650A1 (es)
ZA (1) ZA201108544B (es)

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