WO2002070486A1 - Nitrogen-containing heteroaryl compounds having hiv integrase inhibitory activity - Google Patents

Nitrogen-containing heteroaryl compounds having hiv integrase inhibitory activity Download PDF

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Publication number
WO2002070486A1
WO2002070486A1 PCT/JP2002/001778 JP0201778W WO02070486A1 WO 2002070486 A1 WO2002070486 A1 WO 2002070486A1 JP 0201778 W JP0201778 W JP 0201778W WO 02070486 A1 WO02070486 A1 WO 02070486A1
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WO
WIPO (PCT)
Prior art keywords
nitrogen
inhibitory activity
containing heteroaryl
integrase inhibitory
hiv integrase
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/JP2002/001778
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English (en)
French (fr)
Japanese (ja)
Inventor
Masahiro Fuji
Hidenori Mikamiyama
Hitoshi Murai
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Shionogi and Co Ltd
Original Assignee
Shionogi and Co Ltd
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
Priority to BR0207809-0A priority Critical patent/BR0207809A/pt
Priority to IL15763802A priority patent/IL157638A0/xx
Priority to HU0400175A priority patent/HUP0400175A2/hu
Priority to MXPA03007765A priority patent/MXPA03007765A/es
Priority to US10/469,364 priority patent/US7148237B2/en
Priority to DE60229364T priority patent/DE60229364D1/de
Priority to JP2002569806A priority patent/JP3616628B2/ja
Priority to PL02365027A priority patent/PL365027A1/xx
Priority to CA002439666A priority patent/CA2439666A1/en
Priority to EP02701583A priority patent/EP1375486B1/en
Application filed by Shionogi and Co Ltd filed Critical Shionogi and Co Ltd
Priority to KR10-2003-7011406A priority patent/KR20030078958A/ko
Publication of WO2002070486A1 publication Critical patent/WO2002070486A1/ja
Priority to NO20033848A priority patent/NO20033848L/no
Anticipated expiration legal-status Critical
Priority to US11/500,387 priority patent/US7759372B2/en
Ceased legal-status Critical Current

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
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    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
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    • C07D215/20Oxygen atoms
    • C07D215/24Oxygen atoms attached in position 8
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    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
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    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • 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
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    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
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  • Animal Behavior & Ethology (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
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  • Engineering & Computer Science (AREA)
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  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
PCT/JP2002/001778 2001-03-01 2002-02-27 Nitrogen-containing heteroaryl compounds having hiv integrase inhibitory activity Ceased WO2002070486A1 (en)

Priority Applications (13)

Application Number Priority Date Filing Date Title
CA002439666A CA2439666A1 (en) 2001-03-01 2002-02-27 Nitrogen-containing heteroaryl compounds having hiv integrase inhibitory activity
HU0400175A HUP0400175A2 (en) 2001-03-01 2002-02-27 Nitrogen-containing heteroaryl compounds having hiv integrase inhibitory activity, their use and pharmaceutical compositions containing them
MXPA03007765A MXPA03007765A (es) 2001-03-01 2002-02-27 Compuestos heteroarilo que contienen nitrogeno, que tienen actividad inhibitoria contra virus de inmunodeficiencia humana integrasa.
US10/469,364 US7148237B2 (en) 2001-03-01 2002-02-27 Nitrogen-containing heteroaryl compounds having HIV integrase inhibitory activity
DE60229364T DE60229364D1 (de) 2001-03-01 2002-02-27 Stickstoffhaltige heteroarylverbindungen mit hiv-integrase inhibierender wirkung
JP2002569806A JP3616628B2 (ja) 2001-03-01 2002-02-27 Hivインテグラーゼ阻害活性を有する含窒素芳香族複素環化合物
PL02365027A PL365027A1 (en) 2001-03-01 2002-02-27 Nitrogen-containing heteroaryl compounds having hiv integrase inhibitory activity
BR0207809-0A BR0207809A (pt) 2001-03-01 2002-02-27 Compostos heteroarila contendo nitrogênio possuindo atividade inibidora contra integrase de hiv
IL15763802A IL157638A0 (en) 2001-03-01 2002-02-27 Nitrogen-containing heteroaryl compounds having hiv integrase inhibitory activity
EP02701583A EP1375486B1 (en) 2001-03-01 2002-02-27 Nitrogen-containing heteroaryl compounds having hiv integrase inhibitory activity
KR10-2003-7011406A KR20030078958A (ko) 2001-03-01 2002-02-27 Hiv 인테그라제 저해 활성을 갖는 질소 함유의헤테로아릴 화합물
NO20033848A NO20033848L (no) 2001-03-01 2003-08-29 Nitrogenholdige heteroarylforbindelser med en HIV integrase inhiberende aktivitet
US11/500,387 US7759372B2 (en) 2001-03-01 2006-08-08 Nitrogen-containing heteroaryl compounds having inhibitory activity against HIV integrase

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
JP2001057037 2001-03-01
JP2001-057037 2001-03-01
JP2001-243530 2001-08-10
JP2001243530 2001-08-10
JP2001395022 2001-12-26
JP2001-395022 2001-12-26

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US10/469,364 A-371-Of-International US7148237B2 (en) 2001-03-01 2002-02-27 Nitrogen-containing heteroaryl compounds having HIV integrase inhibitory activity
US11/500,387 Division US7759372B2 (en) 2001-03-01 2006-08-08 Nitrogen-containing heteroaryl compounds having inhibitory activity against HIV integrase

Publications (1)

Publication Number Publication Date
WO2002070486A1 true WO2002070486A1 (en) 2002-09-12

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2002/001778 Ceased WO2002070486A1 (en) 2001-03-01 2002-02-27 Nitrogen-containing heteroaryl compounds having hiv integrase inhibitory activity

Country Status (16)

Country Link
US (2) US7148237B2 (https=)
EP (2) EP2033952B1 (https=)
JP (2) JP3616628B2 (https=)
KR (1) KR20030078958A (https=)
CN (1) CN1659143A (https=)
AT (1) ATE411292T1 (https=)
BR (1) BR0207809A (https=)
CA (1) CA2439666A1 (https=)
CZ (1) CZ20032332A3 (https=)
DE (1) DE60229364D1 (https=)
HU (1) HUP0400175A2 (https=)
IL (1) IL157638A0 (https=)
MX (1) MXPA03007765A (https=)
NO (1) NO20033848L (https=)
PL (1) PL365027A1 (https=)
WO (1) WO2002070486A1 (https=)

Cited By (25)

* Cited by examiner, † Cited by third party
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WO2003024963A3 (de) * 2001-09-14 2003-09-12 Basf Ag Substituierte imidazo [1, 2-a]-5, 6, 7, 8- tetrahydropyridin-8-one, verfahren zu ihrer herstellung, sowie deren verwendung zur herstellung von imidazo [1, 2-a] pyridinen
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US7759372B2 (en) 2010-07-20
JP2004175807A (ja) 2004-06-24
DE60229364D1 (de) 2008-11-27
EP2033952A1 (en) 2009-03-11
JP3616628B2 (ja) 2005-02-02
PL365027A1 (en) 2004-12-27
ATE411292T1 (de) 2008-10-15
KR20030078958A (ko) 2003-10-08
BR0207809A (pt) 2004-03-09
US20060293334A1 (en) 2006-12-28
JPWO2002070486A1 (ja) 2004-07-02
NO20033848L (no) 2003-10-30
CZ20032332A3 (cs) 2003-11-12
CA2439666A1 (en) 2002-09-12
EP1375486A4 (en) 2005-08-31
JP4367762B2 (ja) 2009-11-18
CN1659143A (zh) 2005-08-24
IL157638A0 (en) 2004-03-28

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