CL2016002942A1 - Nuevos derivados de pirazolina pirimidina y su uso como inhibidores de malt1 - Google Patents

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

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Publication number
CL2016002942A1
CL2016002942A1 CL2016002942A CL2016002942A CL2016002942A1 CL 2016002942 A1 CL2016002942 A1 CL 2016002942A1 CL 2016002942 A CL2016002942 A CL 2016002942A CL 2016002942 A CL2016002942 A CL 2016002942A CL 2016002942 A1 CL2016002942 A1 CL 2016002942A1
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CL
Chile
Prior art keywords
rent
replaced
optionally replaced
alcoxyl
independently
Prior art date
Application number
CL2016002942A
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English (en)
Inventor
Tintelnot-Blomley Marina
Pissot Soldermann Carole
Quancard Jean
Schlapbach Achim
Zoller Thomas
Simic Oliver
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Novartis Ag
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Publication of CL2016002942A1 publication Critical patent/CL2016002942A1/es

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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
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hematology (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

<p>LA PRESENTE INVENCIÓN DESCRIBE NUEVOS DERIVADOS DE LA PIRAZOLO-PIRIMIDINA DE IA FORMULA (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, ALQUENILO C2-C 6, HIDROXILO, N,N-DI-AIQUILAMINO C1 -C6, N-MONO-ALQUILAMINO C1-C6, O-RG, RG, FENILO , O POR ALCOXILO C1-C6 EN DONDE DICHO ALCOXILO DE NUEVO PUEDE SER OPCIONALMENTE SUSTITUIDO POR ALCOXILO C1-C6, N, N-DI-ALQUILAMINO C1-C6, RG O ALQUILO; 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 - 20 ÁTOMOS; FENILO OPCIONALMENTE SUSTITUIDO POR ALCOXILO C1-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 PROTEOLÍTICA Y/O AUTOPROTEOLÍTICA DE MALT1.</p>
CL2016002942A 2014-05-28 2016-11-18 Nuevos derivados de pirazolina pirimidina y su uso como inhibidores de malt1 CL2016002942A1 (es)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
CL2016002942A1 true CL2016002942A1 (es) 2017-07-14

Family

ID=50828759

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CL2016002942A CL2016002942A1 (es) 2014-05-28 2016-11-18 Nuevos derivados de pirazolina pirimidina y su uso como inhibidores de malt1

Country Status (36)

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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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