CO6190626A2 - Compuestos y composiciones como inhibidores de proteasa activadora de canal - Google Patents

Compuestos y composiciones como inhibidores de proteasa activadora de canal

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Publication number
CO6190626A2
CO6190626A2 CO09072488A CO09072488A CO6190626A2 CO 6190626 A2 CO6190626 A2 CO 6190626A2 CO 09072488 A CO09072488 A CO 09072488A CO 09072488 A CO09072488 A CO 09072488A CO 6190626 A2 CO6190626 A2 CO 6190626A2
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CO
Colombia
Prior art keywords
carbon atoms
ring
alkynyl
alkenyl
alkyl
Prior art date
Application number
CO09072488A
Other languages
English (en)
Inventor
David C Tully
Arnab K Chatterjee
Agnes Vidal
Badry Bursulaya
Glen Spraggon
Original Assignee
Irm Llc
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 Irm Llc filed Critical Irm Llc
Publication of CO6190626A2 publication Critical patent/CO6190626A2/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06191Dipeptides containing heteroatoms different from O, S, or N
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/401Proline; Derivatives thereof, e.g. captopril
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/10Expectorants
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06078Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06086Dipeptides with the first amino acid being basic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrrole Compounds (AREA)

Abstract

1.- Un compuesto de la fórmula (1):o sales farmacéuticamente aceptables del mismo, en donde: O-(CR2)p-R2- es un sustituyente en cualquier posición del anillo A; J es un anillo carbocíclico monocíclico o fusionado de 5 a 12 miembros, un anillo heterocíclico que comprende N, O y/o S; un anillo de arilo o hetero-arilo, en el entendido de que J no es triazolilo; B es o (CR2)k-R5;Y es un enlace, -SO2-, -NHCO- u -O-(CO)-; R1 es halógeno, -(CR2)I-NR6R7, -(CR2)I-NRC(=NR)-NR6R7, -(CR2)I-C(=NR)-NR6R7, -C(O)-(CR2)I-NR6R7, -(CR2)I-NR- SO2R6, -(CR2)I-NR-C(O)-R6, -(CR2)I-SO2NR6R7, o -(CR2)I-OR6, o un alcoxilo de 1 a 6 átomos de carbono opcionalmente sustituido, alquilo de 1 a 6 átomos de carbono, alquenilo de 2 a 6 átomos de carbono, o alquinilo de 2 a 6 átomos de carbono; o un anillo carbocíclico opcionalmente sustituido, un anillo heterocíclico, arilo o heteroarilo; R3 es alquilo de 1 a 6 átomos de carbono, alquenilo de 2 a 6 átomos de carbono, alquinilo de 2 a 6 átomos de carbono, o -(CR2)I-R5; de una manera alternativa, NH-Y-R3 forman juntos NH2; R2, R4 y R5 son independientemente un anillo carbocíclico de 5 a 12 miembros opcionalmente sustituido, un anillo heterocíclico, arilo o heteroarilo; o R4 es H, alquilo de 1 a 6 átomos de carbono, alquenilo de 2 a 6 átomos de carbono, alquinilo de 2 a 6 átomos de carbono, o en donde P es C o N, y el anillo E junto con P forman un anillo monocíclico o fusionado de 5 a 12 miembros opcionalmente sustituido;R6 y R7 son independientemente H, alquilo de 1 a 6 átomos de carbono, alquenilo de 2 a 6 átomos de carbono, alquinilo de 2 a 6 átomos de carbono, o -(CR2)I-R5; cada R es H, o alquilo de 1 a 6 átomos de carbono, alquenilo de 2 a 6 átomos de carbono, o alquinilo de 2 a 6 átomos de carbono; l es desde 0 a 6; k, m, n, y p son independientemente de 1 a 6; x es de 0 a 4; en el entendido de que R4 es piperidinilo cuando NH-Y-R3 forman juntos NH2; y además en el entendido de que R5 es piperidinilo cuando B es (CR2)k-R5.
CO09072488A 2007-01-10 2009-07-13 Compuestos y composiciones como inhibidores de proteasa activadora de canal CO6190626A2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US88433407P 2007-01-10 2007-01-10
US89147407P 2007-02-23 2007-02-23

Publications (1)

Publication Number Publication Date
CO6190626A2 true CO6190626A2 (es) 2010-08-19

Family

ID=39148650

Family Applications (1)

Application Number Title Priority Date Filing Date
CO09072488A CO6190626A2 (es) 2007-01-10 2009-07-13 Compuestos y composiciones como inhibidores de proteasa activadora de canal

Country Status (33)

Country Link
US (1) US20080176901A1 (es)
EP (2) EP2279777A2 (es)
JP (1) JP2010515729A (es)
KR (1) KR101084787B1 (es)
AR (1) AR064841A1 (es)
AT (1) ATE493174T1 (es)
AU (1) AU2007342223B2 (es)
BR (1) BRPI0720799A2 (es)
CA (1) CA2673803A1 (es)
CL (1) CL2008000060A1 (es)
CO (1) CO6190626A2 (es)
CU (1) CU23762B7 (es)
CY (1) CY1111340T1 (es)
DE (1) DE602007011670D1 (es)
DK (1) DK2104535T3 (es)
EA (1) EA016199B1 (es)
EC (1) ECSP099517A (es)
GT (1) GT200900196A (es)
HK (1) HK1129860A1 (es)
HN (1) HN2009001282A (es)
HR (1) HRP20110201T1 (es)
MA (1) MA31037B1 (es)
MX (1) MX2009007476A (es)
NO (1) NO20092817L (es)
NZ (1) NZ577939A (es)
PE (1) PE20081566A1 (es)
PL (1) PL2104535T3 (es)
PT (1) PT2104535E (es)
RS (1) RS51644B (es)
SV (1) SV2009003330A (es)
TN (1) TN2009000294A1 (es)
TW (1) TW200845981A (es)
WO (1) WO2008085608A1 (es)

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EP2117537A1 (en) * 2007-02-09 2009-11-18 Irm Llc Compounds and compositions as channel activating protease inhibitors
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US20080176901A1 (en) 2008-07-24
GT200900196A (es) 2010-03-15
HRP20110201T1 (hr) 2011-08-31
JP2010515729A (ja) 2010-05-13
CU20090122A7 (es) 2011-07-11
EA200900920A1 (ru) 2010-02-26
RS51644B (en) 2011-10-31
AU2007342223A1 (en) 2008-07-17
PL2104535T3 (pl) 2011-05-31
EP2279777A2 (en) 2011-02-02
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NZ577939A (en) 2011-03-31
MX2009007476A (es) 2009-07-22
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BRPI0720799A2 (pt) 2014-03-11
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