HUP0401301A2 - Pirrolopirimidinek, eljárás előállításukra, alkalmazásuk és a vegyületeket tartalmazó gyógyszerkészítmények - Google Patents

Pirrolopirimidinek, eljárás előállításukra, alkalmazásuk és a vegyületeket tartalmazó gyógyszerkészítmények

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Publication number
HUP0401301A2
HUP0401301A2 HU0401301A HUP0401301A HUP0401301A2 HU P0401301 A2 HUP0401301 A2 HU P0401301A2 HU 0401301 A HU0401301 A HU 0401301A HU P0401301 A HUP0401301 A HU P0401301A HU P0401301 A2 HUP0401301 A2 HU P0401301A2
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Hungary
Prior art keywords
group
aryl
alkyl
heterocyclyl
cycloalkyl
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HU0401301A
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English (en)
Inventor
Claudia Betschart
Kenji Hayakawa
Osamu Irie
Junichi Sakaki
Genji Iwasaki
René Lattmann
Martin Missbach
Naoki Teno
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Novartis Ag.
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Application filed by Novartis Ag. filed Critical Novartis Ag.
Publication of HUP0401301A2 publication Critical patent/HUP0401301A2/hu
Publication of HUP0401301A3 publication Critical patent/HUP0401301A3/hu

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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
    • 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
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • 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
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • AHUMAN NECESSITIES
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • 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
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

A jelen találmány az (I) általános képletű katepszin K inhibitorokra -amelyek képletében R hidrogénatom, -R2, -OR2 vagy -NR1R2 csoport, aholRl hidrogénatom, alkil- vagy cikloalkilcsoport, és R2 alkil- vagycikloalkilcsoport, és ahol R1 és R2 egymástól függetlenül adottesetben szubsztituált; X nitrogénatom vagy =C(Z)- csoport, ahol Zhidrogénatom, -C(O)-NR3R4, -NH-C(O)-R3, -CH2-NH-C(O)-R3, -(O)-R3, -S(O)-R3, -S(O)2-R3, -CH2-C(O)-R3, -CH2-NR3R4, -R4, -C<C-CH2-R5, N-heterociklil-, (N-heterociklil)-karbonil- vagy -C(P)=C(Q)-R4 csoport,ahol P és Q hidrogénatom, alkil- vagy arilcsoport, R3 aril-, aril-alkil-, cikloalkil-, cikloalkil-alkil-, heterociklil- vagyheterociklil-alkil-csoport, R4 hidrogénatom vagy R3; vagy R3 és R4 anitrogénatommal együtt N-heterociklilcsoportot képez; és R3 és R4adott esetben szubsztituált; R5 aril-, aril-alkil-, aril-oxi-, aroil-vagy N-heterociklilcsoport, és ahol R5 adott esetben szubsztituált,ahol R13 adott esetben szubsztituált alkil-, cikloalkil- vagycikloalkil-alkil-csoport; és R14 hidrogénatom vagy adott esetbenszubsztituált[aril-, aril-W-, aril-(alkil)-W-, cikloalkil-,cikloalkil-W-, N-heterociklil- vagy N-heterociklil-W-, ftálimidil-,hidantoinil-, oxazolidinonil- vagy 2,6-dioxo-piperazinil-csoport],ahol W oxi-, karbonil-, -NH(R6)-, -NH(R6)-C(O)-, -NH(R6)-C(O)-O-,szulfinil-, szulfonil- vagy tiocsoport; R6 hidrogénatom vagy adottesetben szubsztituált alkil-, karboxi-, acil-, karbamoil-, aril-,szulfinil- vagy szulfonilcsoport; és ahol R14 adott esetbenszubsztituált vagy gyógyászatilag elfogadható sóikra vagy észtereikre,a vegyületek előállítására, valamint a találmány szerintiinhibitoroknak olyan betegségek, illetve egészségi állapotokkezelésére vagy megelőzésére történő gyógyszerészeti felhasználásáravonatkozik, amelyekben szerepet játszik a katepszin K. Ó
HU0401301A 2001-08-30 2002-08-29 Pyrrolo pyrimidines, process for their preparation, their use and pharmaceutical compositions containing them HUP0401301A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0121033.5A GB0121033D0 (en) 2001-08-30 2001-08-30 Organic compounds
PCT/EP2002/009663 WO2003020721A1 (en) 2001-08-30 2002-08-29 Pyrrolo pyrimidines as agents for the inhibition of cystein proteases

Publications (2)

Publication Number Publication Date
HUP0401301A2 true HUP0401301A2 (hu) 2004-10-28
HUP0401301A3 HUP0401301A3 (en) 2008-03-28

Family

ID=9921234

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0401301A HUP0401301A3 (en) 2001-08-30 2002-08-29 Pyrrolo pyrimidines, process for their preparation, their use and pharmaceutical compositions containing them

Country Status (30)

Country Link
US (2) US7452886B2 (hu)
EP (1) EP1423391B8 (hu)
JP (1) JP4629334B2 (hu)
KR (1) KR100695845B1 (hu)
CN (1) CN100372849C (hu)
AR (1) AR036374A1 (hu)
AT (1) ATE326469T1 (hu)
AU (1) AU2002333760B2 (hu)
BR (1) BR0212226A (hu)
CA (1) CA2458684C (hu)
CY (1) CY1105573T1 (hu)
DE (1) DE60211530T2 (hu)
DK (1) DK1423391T3 (hu)
EC (1) ECSP044998A (hu)
ES (1) ES2262888T3 (hu)
GB (1) GB0121033D0 (hu)
HK (1) HK1072254A1 (hu)
HU (1) HUP0401301A3 (hu)
IL (3) IL160367A0 (hu)
MX (1) MXPA04001935A (hu)
MY (1) MY157368A (hu)
NO (1) NO328890B1 (hu)
NZ (1) NZ531343A (hu)
PE (1) PE20030418A1 (hu)
PL (1) PL368280A1 (hu)
PT (1) PT1423391E (hu)
RU (1) RU2331644C2 (hu)
TW (1) TWI297690B (hu)
WO (1) WO2003020721A1 (hu)
ZA (1) ZA200401042B (hu)

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EP1423391B1 (en) 2006-05-17
IL160367A (en) 2009-12-24
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IL160367A0 (en) 2004-07-25
EP1423391B8 (en) 2007-12-12
AU2002333760B2 (en) 2007-01-04
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