ME00757B - Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze - Google Patents

Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze

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Publication number
ME00757B
ME00757B MEP-2000-448A MEP2000448A ME00757B ME 00757 B ME00757 B ME 00757B ME P2000448 A MEP2000448 A ME P2000448A ME 00757 B ME00757 B ME 00757B
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ME
Montenegro
Prior art keywords
halo
eqn
prod
sum
alkoxy
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MEP-2000-448A
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English (en)
Inventor
Malcolm Clive Carter
George Stuart Cockerill
Stephen Barry Guntrip
Karen Elizabeth Lackey
Kathryn Jane Smith
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Novartis Ag
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=10825153&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ME00757(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of ME00757B publication Critical patent/ME00757B/me

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    • 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
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
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    • 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]
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    • 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
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • 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
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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    • C07DHETEROCYCLIC COMPOUNDS
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    • C07D411/02Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D411/04Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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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
    • C07D471/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Indole Compounds (AREA)
  • Steroid Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Opisana suheteroaromatična jedinjenja formule (I): Opisana suheteroaromatična jedinjenja formule (I):     <!--[if gte vml 1]><v:shapetype id="_x0000_t75" coordsize="21600,21600" o:spt="75" o:preferrelative="t" path="m@4@5l@4@11@9@11@9@5xe" filled="f" stroked="f"> <v:stroke joinstyle="miter"/> <v:formulas> <v:f eqn="if lineDrawn pixelLineWidth 0"/> <v:f eqn="sum @0 1 0"/> <v:f eqn="sum 0 0 @1"/> <v:f eqn="prod @2 1 2"/> <v:f eqn="prod @3 21600 pixelWidth"/> <v:f eqn="prod @3 21600 pixelHeight"/> <v:f eqn="sum @0 0 1"/> <v:f eqn="prod @6 1 2"/> <v:f eqn="prod @7 21600 pixelWidth"/> <v:f eqn="sum @8 21600 0"/> <v:f eqn="prod @7 21600 pixelHeight"/> <v:f eqn="sum @10 21600 0"/> </v:formulas> <v:path o:extrusionok="f" gradientshapeok="t" o:connecttype="rect"/> <o:lock v:ext="edit" aspectratio="t"/></v:shapetype><v:shape id="_x0000_i1025" type="#_x0000_t75" style='width:155.5pt; height:112.5pt'> <v:imagedata src="file:///C:\Users\Igor\AppData\Local\Temp\msohtmlclip1\01\clip_image001.jpg" o:title="sI"/></v:shape><![endif]--><!--[if !vml]-->     ili njegova so ili solvat; gde Y je CR1 i V je N; ili Y je CR1i V je CR2; R1 predstavlja grupu CH3SO2CH2CH2NHCH2-Ar-,gde Ar se bira između furana i tiazola, od kojih svaki može biti opcionosupstituisan sa jednim ili dva halo, C1-4 alkil ili C1-4aloksigrupama; R2 je vodonik ili C1-4 alkoksi; ili R2je halo; R3 se bira iz grupe koju čine benzil-, halo-, dihalo- itrihalobenzil, benzoil, piridilmetil, piridilmetoksi, fenoksi, benziloksi,halo-, dihalo- i trihalobenziloksi i benzensulfonil; R4 je halo iliC1-4 alkoksi ili nije prisutan; gde ili (a) R3predstavlja 3-fluorobenziloksi; ili njegova so ili solvat; gde Y je CR 1 i V je N; ili Y je CR 1 i V je CR 2 ; R 1 predstavlja grupu CH 3 SO 2 CH 2 CH 2 NHCH 2 -Ar-,gde Ar se bira između furana i tiazola, od kojih svaki može biti opcionosupstituisan sa jednim ili dva halo, C 1-4 alkil ili C 1-4 aloksigrupama; R 2 je vodonik ili C 1-4 alkoksi; ili R 2 je halo; R 3 se bira iz grupe koju čine benzil-, halo-, dihalo- itrihalobenzil, benzoil, piridilmetil, piridilmetoksi, fenoksi, benziloksi,halo-, dihalo- i trihalobenziloksi i benzensulfonil; R 4 je halo iliC 1-4 alkoksi ili nije prisutan; gde ili (a) R 3 predstavlja 3-fluorobenziloksi; i/ili (b) R4 se bira od halo i supstituent je u položaju 3fenil prstena; i halo predstavlja fluoro, hloro ili bromo, kao i njihovodobijanje, farmaceutski preparati koji ih sadrže i njihova upotreba u medicini. i/ili (b) R 4 se bira od halo i supstituent je u položaju 3fenil prstena; i halo predstavlja fluoro, hloro ili bromo, kao i njihovodobijanje, farmaceutski preparati koji ih sadrže i njihova upotreba u medicini.
MEP-2000-448A 1998-01-12 1999-01-08 Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze ME00757B (me)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB9800569.7A GB9800569D0 (en) 1998-01-12 1998-01-12 Heterocyclic compounds
PCT/EP1999/000048 WO1999035146A1 (en) 1998-01-12 1999-01-08 Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors

Publications (1)

Publication Number Publication Date
ME00757B true ME00757B (me) 2008-06-05

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US (11) US6727256B1 (me)
EP (3) EP1047694B1 (me)
JP (2) JP3390741B2 (me)
KR (1) KR100569776B1 (me)
CN (1) CN1134438C (me)
AP (1) AP1446A (me)
AR (2) AR015507A1 (me)
AT (3) ATE417847T1 (me)
AU (2) AU749549C (me)
BG (1) BG64825B1 (me)
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ES (3) ES2262087T3 (me)
FR (1) FR08C0038I2 (me)
GB (1) GB9800569D0 (me)
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IL (2) IL137041A0 (me)
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