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SV2016005328A - Nuevos derivados de pirazolo pirimidina y su uso como inhibidores de malt1 - Google Patents

Nuevos derivados de pirazolo pirimidina y su uso como inhibidores de malt1

Info

Publication number
SV2016005328A
SV2016005328A SV2016005328A SV2016005328A SV2016005328A SV 2016005328 A SV2016005328 A SV 2016005328A SV 2016005328 A SV2016005328 A SV 2016005328A SV 2016005328 A SV2016005328 A SV 2016005328A SV 2016005328 A SV2016005328 A SV 2016005328A
Authority
SV
El Salvador
Prior art keywords
rent
replaced
optionally replaced
independently
pirazolo
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Application number
SV2016005328A
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English (en)
Inventor
Soldermann Carole Pissot
Jean Quancard
Achim Schlapbach
Oliver Simic
Thomas Zoller
Marina Tintel-Not-Blomley
Original Assignee
Novartis Ag
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Publication of SV2016005328A publication Critical patent/SV2016005328A/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
    • A61K31/495Heterocyclic 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
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • 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
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
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    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Transplantation (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

LA PRESENTE INVENCIÓN DESCRIBE NUEVOS DERIVADOS DE LA PIRAZOLO-PIRIMIDINA DE LA FÓRMULA (I) O UNA SAL FARMACÉUTICAMENTE ACEPTABLE DEL MISMO; (I) EN LA QUE, R1 ES HALÓGENO, CIANO, O ALQUILO C1-C3 OPCIONALMENTE SUSTITUIDO POR HALÓGENO; R2 ES ALQUILO C1-C6 OPCIONALMENTE SUSTITUIDO UNA O MÁS VECES POR ALQUILO C1-C6, ALQUENILOC2-C 6, HIDROXILO, N,N-DI-ALQUILAMINO C1-C6, N-MONO-ALQUILAMINO C1-C6, O-RG, RG, FENILO , O POR ALCOXILOC1-C6 EN DONDE DICHO ALCOXILO DE NUEVO PUEDE SER OPCIONALMENTE SUSTITUIDO POR ALCOXILO C1-C6, N, N-DI-ALQUILAMINO C1-C6, RG O FENILO; CICLOALQUILO C3-C6 OPCIONALMENTE SUSTITUIDO POR ALQUILO C1-C6, N,N-DI-ALQUILAMINO C1-C6 O ALCOXILO C1-C6-ALQUILO C1-C6, Y/O DOS DE DICHOS SUSTITUYENTES OPCIONALES JUNTO CON LOS ÁTOMOS A LOS QUE ESTÁN UNIDOS PUEDEN FORMAR UN ANILLO HETEROCÍCLICO SATURADO ANULADO O ESPIROCÍCLICO DE 4-6 MIEMBROS QUE COMPRENDE 1 - 2 0 ÁTOMOS; FENILO OPCIONALMENTE SUSTITUIDO POR ALCOXILOC1-C6; UN ANILLO HETEROARILO DE 5 - 6 MIEMBROS QUE TIENE 1 A 3 HETEROÁTOMOS SELECCIONADOS DE N Y O, DICHO ANILLO ES OPCIONALMENTE SUSTITUIDO POR ALQUILO C1-C6 QUE PUEDE ESTAR OPCIONALMENTE SUSTITUIDO POR AMINO O HIDROXILO; RG; O N,N-DI-ALQUILAMINO CARBONILO C1-C6; Y R ES FENILO SUSTITUIDO INDEPENDIENTEMENTE DOS O MÁS VECES POR RA, 2-PIRIDILO SUSTITUIDO INDEPENDIENTEMENTE UNA O MÁS VECES POR RB, 3-PIRIDILO SUSTITUIDO INDEPENDIENTEMENTE UNA O MÁS VECES POR RC, O 4-PIRIDILO INDEPENDIENTEMENTE SUSTITUIDO UNA O MÁS VECES POR RD; QUE GENERALMENTE ESTÁN INTERACTUANDO CON ACTIVIDAD PROTEOLÍTICA Y/O AUTOPROTEOLÍTICA DE MALT1, Y EN PARTICULAR QUE PUEDEN INHIBIR DICHA ACTIVIDAD. LA PRESENTE INVENCIÓN DESCRIBE ADEMÁS LA SÍNTESIS DE ESTOS NUEVOS DERIVADOS DE LA PIRAZOLO-PIRIMIDINA, SU USO COMO UN MEDICAMENTO, ESPECIALMENTE MEDIANTE LA INTERACCIÓN CON ACTIVIDAD PROTEOLITÍCA Y/O AUTOPROTEOLÍTICA DE MALT1
SV2016005328A 2014-05-28 2016-11-28 Nuevos derivados de pirazolo pirimidina y su uso como inhibidores de malt1 SV2016005328A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP14170408 2014-05-28

Publications (1)

Publication Number Publication Date
SV2016005328A true SV2016005328A (es) 2018-06-12

Family

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SV2016005328A SV2016005328A (es) 2014-05-28 2016-11-28 Nuevos derivados de pirazolo pirimidina y su uso como inhibidores de malt1

Country Status (36)

Country Link
US (2) US9815842B2 (es)
EP (1) EP3149001B1 (es)
JP (1) JP6545197B2 (es)
KR (1) KR20170007311A (es)
CN (1) CN106170489B (es)
AP (1) AP2016009487A0 (es)
AR (1) AR100645A1 (es)
AU (1) AU2015265478B2 (es)
BR (1) BR112016024545A2 (es)
CA (1) CA2945077A1 (es)
CL (1) CL2016002942A1 (es)
CR (1) CR20160548A (es)
CU (1) CU24393B1 (es)
CY (1) CY1121946T1 (es)
DK (1) DK3149001T3 (es)
EA (1) EA032050B1 (es)
ES (1) ES2738695T3 (es)
GT (1) GT201600249A (es)
HR (1) HRP20191261T1 (es)
HU (1) HUE044351T2 (es)
IL (1) IL247949A0 (es)
LT (1) LT3149001T (es)
MX (1) MX373846B (es)
MY (1) MY182487A (es)
PE (1) PE20170189A1 (es)
PH (1) PH12016501862B1 (es)
PL (1) PL3149001T3 (es)
PT (1) PT3149001T (es)
RS (1) RS59039B1 (es)
SG (1) SG11201607895PA (es)
SI (1) SI3149001T1 (es)
SV (1) SV2016005328A (es)
TR (1) TR201910730T4 (es)
TW (1) TWI709561B (es)
UY (1) UY36143A (es)
WO (1) WO2015181747A1 (es)

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