HUP0401748A2 - 2-Amino-4,5-triszubsztituált tiazolilszármazékok, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények - Google Patents

2-Amino-4,5-triszubsztituált tiazolilszármazékok, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények

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Publication number
HUP0401748A2
HUP0401748A2 HU0401748A HUP0401748A HUP0401748A2 HU P0401748 A2 HUP0401748 A2 HU P0401748A2 HU 0401748 A HU0401748 A HU 0401748A HU P0401748 A HUP0401748 A HU P0401748A HU P0401748 A2 HUP0401748 A2 HU P0401748A2
Authority
HU
Hungary
Prior art keywords
alkyl
amino
group
carbonyl
mono
Prior art date
Application number
HU0401748A
Other languages
English (en)
Inventor
Christopher John Love
Guy Rosalia Eugeen Lommen
Julien Georges Pierre-Olivier Doyon
Jean-Pierre André Marc Bongartz
Marcel Jozef Maria AA
Robert Jozef Maria Hendrickx
Peter Jacobus Johannes Antonius Buijnsters
Ludwig Paul Cooymans
Nele Vandermaesen
Erwin Coesemans
Gustaaf Maria Boeckx
Original Assignee
Janssen Pharmaceutica N.V.
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 Janssen Pharmaceutica N.V. filed Critical Janssen Pharmaceutica N.V.
Publication of HUP0401748A2 publication Critical patent/HUP0401748A2/hu
Publication of HUP0401748A3 publication Critical patent/HUP0401748A3/hu

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Classifications

    • 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
    • A61K31/4261,3-Thiazoles
    • CCHEMISTRY; METALLURGY
    • 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
    • C07D417/02Heterocyclic 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
    • 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
    • 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
    • A61P33/00Antiparasitic 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/38Nitrogen atoms
    • C07D277/42Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • CCHEMISTRY; METALLURGY
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

A találmány tárgya (I') általános képletű vegyület, N-oxidja,gyógyászatilag elfogadható addíciós sója, kvaterner aminja éssztereokémiai izomer formájának alkalmazása gyulladásos és/vagyautoimmun betegségek kezelésére és gyógyítására, amelyeket TNF-aés/vagy IL-12 közvetít. Az (1) általános képletben Z jelentésehalogénatom, 1-6 szénatomos alkil-, (1-6 szénatomos alkil)-karbonil-,(1-6 szénatomos alkoxi)-karbonil-, amino-karbonit-csoport, vagyhidroxil-, karboxil-, ciano-, amino-, piperidinil-szubsztituáltamino-, 1-4 szénatomos alkilcsoporttal szubsztituáltpiperidinilcsoporttal szubsztituált amino-, mono- vagy di(1-6szénatomos alkil)-amino-, amino-karbonil-, mono- vagy di(1-6szénatomos alkil)-amino-karbonil-, (1-6 szénatomos alkoxi)-karbonil-,1-6 szénatomos alkoxi-, piperidinil-, piperazinil-, morfolinil-, tio-morfolinil-csoporttal szubsztituált 1-6 szénatomos alkilcsoport,továbbá polihalogén-(1-4 szénatomos alkil)-, ciano-, amino-, mono-vagy di(1-6 szénatomos alkil)-amino-karbonil-, (1-6 szénatomosalkoxi)-karbonil-, (1-6 szénatomos alkil)-karbonil-oxi-, amino-S(=O)2,mono- vagy di(1-6 szénatomos alkil)-amino-S(=O)2, -C(=N-Rx)NRyRzcsoport; Q jelentése adott esetben szubsztituált 3-6 szénatomoscikloalkil-, fenil-, piridil-, pirimidinil-, pirazinil-, piridazinil-,benztiazolil- benzoxazolil-, benzimidazolil-, indazolil- vagy imidazo-piridil-csoport, vagy Q jelentése (b-1), (b-2) vagy (b-3) képletűcsoport; L jelentése adott esetben szubsztituált fenil- vagy adottesetben szubsztituált monociklusos, 5- vagy 6-tagú, részben telítettvagy aromás heterociklus, vagy biciklusos, részben telített vagyaromás heterociklusos csoport; aril jelentése adott esetbenszubsztituált fenilcsoport. A vegyületeket gyógyszer előállításáralehet felhasználni gyulladásos betegségek és/vagy autoimmun betegségekkezelésére vagy megelőzésére, amelyeket TNF-a és/vagy IL-12 közvetít.A találmány kiterjed a vegyület előállítására és a vegyületekettartalmazó gyógyszerkészítményekre is. Ó
HU0401748A 2001-08-13 2002-08-09 2-amino-4,5-trisubstituted thiazolyl derivatives, process for their preparation and pharmaceutical compositions containing them HUP0401748A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP01203087 2001-08-13
PCT/EP2002/008955 WO2003015773A2 (en) 2001-08-13 2002-08-09 2-amino-4,5-trisubstituted thiazolyl derivatives and their use against autoimmune diseases

Publications (2)

Publication Number Publication Date
HUP0401748A2 true HUP0401748A2 (hu) 2004-12-28
HUP0401748A3 HUP0401748A3 (en) 2011-03-28

Family

ID=8180790

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0401748A HUP0401748A3 (en) 2001-08-13 2002-08-09 2-amino-4,5-trisubstituted thiazolyl derivatives, process for their preparation and pharmaceutical compositions containing them

Country Status (21)

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US (2) US7232838B2 (hu)
EP (1) EP1418909B1 (hu)
JP (1) JP4388805B2 (hu)
KR (2) KR100979988B1 (hu)
CN (1) CN100496493C (hu)
AU (1) AU2002324045C1 (hu)
BR (1) BR0211887A (hu)
CA (1) CA2451980C (hu)
EA (1) EA007717B1 (hu)
ES (1) ES2407807T3 (hu)
HK (1) HK1069997A1 (hu)
HR (1) HRP20040097B1 (hu)
HU (1) HUP0401748A3 (hu)
IL (2) IL160329A0 (hu)
MX (1) MXPA04001399A (hu)
NO (1) NO327409B1 (hu)
NZ (1) NZ530950A (hu)
PL (1) PL368130A1 (hu)
UA (1) UA82176C2 (hu)
WO (1) WO2003015773A2 (hu)
ZA (1) ZA200401162B (hu)

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US8106209B2 (en) * 2008-06-06 2012-01-31 Achillion Pharmaceuticals, Inc. Substituted aminothiazole prodrugs of compounds with anti-HCV activity
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Also Published As

Publication number Publication date
CN100496493C (zh) 2009-06-10
HRP20040097B1 (hr) 2013-10-11
IL160329A0 (en) 2004-07-25
MXPA04001399A (es) 2004-05-27
AU2002324045B2 (en) 2007-10-04
PL368130A1 (en) 2005-03-21
US20070203189A1 (en) 2007-08-30
EA200400306A1 (ru) 2004-08-26
ES2407807T3 (es) 2013-06-14
KR20040031712A (ko) 2004-04-13
BR0211887A (pt) 2004-09-21
US7232838B2 (en) 2007-06-19
UA82176C2 (en) 2008-03-25
WO2003015773A2 (en) 2003-02-27
CA2451980C (en) 2012-12-11
CN1541097A (zh) 2004-10-27
NZ530950A (en) 2006-03-31
ZA200401162B (en) 2005-07-27
HRP20040097A2 (en) 2004-06-30
IL160329A (en) 2010-05-31
NO20040632L (no) 2004-03-11
JP4388805B2 (ja) 2009-12-24
NO327409B1 (no) 2009-06-22
WO2003015773A3 (en) 2003-12-18
KR100979988B1 (ko) 2010-09-03
HK1069997A1 (en) 2005-06-10
US20040254191A1 (en) 2004-12-16
EA007717B1 (ru) 2006-12-29
US7803823B2 (en) 2010-09-28
JP2005501099A (ja) 2005-01-13
CA2451980A1 (en) 2003-02-27
KR20100076043A (ko) 2010-07-05
EP1418909B1 (en) 2013-02-20
KR101034489B1 (ko) 2011-05-17
AU2002324045C1 (en) 2008-05-29
HUP0401748A3 (en) 2011-03-28
EP1418909A2 (en) 2004-05-19

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