HUP0401740A2 - N-szubsztituált hidroxipirimidinon-karboxamid HIV-integráz inhibitorok és ezeket tartalmazó gyógyszerkészítmények - Google Patents

N-szubsztituált hidroxipirimidinon-karboxamid HIV-integráz inhibitorok és ezeket tartalmazó gyógyszerkészítmények

Info

Publication number
HUP0401740A2
HUP0401740A2 HU0401740A HUP0401740A HUP0401740A2 HU P0401740 A2 HUP0401740 A2 HU P0401740A2 HU 0401740 A HU0401740 A HU 0401740A HU P0401740 A HUP0401740 A HU P0401740A HU P0401740 A2 HUP0401740 A2 HU P0401740A2
Authority
HU
Hungary
Prior art keywords
hiv integrase
pharmaceutical compositions
compositions containing
carboxamide inhibitors
prevention
Prior art date
Application number
HU0401740A
Other languages
English (en)
Inventor
Benedetta Crescenzi
Cristina Gardelli
Ester Muraglia
Emanuela Nizi
Federica Orvieto
Paola Pace
Giovanna Pescatore
Alessia Petrocchi
Marco Poma
Michael Rowley
Rita Scarpelli
Vincenzo Summa
Original Assignee
Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A.
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=26991691&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HUP0401740(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. filed Critical Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A.
Publication of HUP0401740A2 publication Critical patent/HUP0401740A2/hu
Publication of HUP0401740A3 publication Critical patent/HUP0401740A3/hu
Publication of HU230248B1 publication Critical patent/HU230248B1/hu
Priority to HUS1600016C priority Critical patent/HUS1600016I1/hu

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/557—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms, e.g. orotic acid
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/04—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/06—Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/10—Heterocyclic 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 carbon chain containing aromatic rings
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    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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 three or more hetero rings
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    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
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    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07—ORGANIC CHEMISTRY
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    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic 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
    • C07D513/02—Heterocyclic 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
    • C07D513/04—Ortho-condensed systems

Abstract

A találmány (I) általános képletű N-szubsztituált 5-hidroxipirimidin-6-on-4-karboxamid-származékokra vonatkozik, amelyek HIV-integrázinhibitorok, így alkalmazhatók HIV-fertőzés kezelésére vagymegelőzésére, AIDS megelőzésére, kezelésére és kialakulásánakkésleltetésére szolgáló gyógyszerkészítmények hatóanyagaként. Aképletben R1, R2, R3 és R4 jelentése hidrogénatom vagy adott esetbenszubsztituált alkilcsoport, monociklusos vagy biciklusos, telítettvagy aromás széngyűrűs vagy heterogyűrűs, adott esetben szubsztituáltcsoportok, vagy pedig más szerves csoportok. Ó
HU0401740A 2001-10-26 2002-10-21 N-szubsztituált hidroxipirimidinon-karboxamid HIV-integráz inhibitorok HU230248B1 (hu)

Priority Applications (1)

Application Number Priority Date Filing Date Title
HUS1600016C HUS1600016I1 (hu) 2001-10-26 2016-04-07 N-szubsztituált hidroxipirimidinon-karboxamid HIV-integráz inhibitorok

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US33956801P 2001-10-26 2001-10-26
US60/339,568 2001-10-26
US36219102P 2002-03-06 2002-03-06
US60/362,191 2002-03-06
PCT/GB2002/004753 WO2003035077A1 (en) 2001-10-26 2002-10-21 N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase

Publications (3)

Publication Number Publication Date
HUP0401740A2 true HUP0401740A2 (hu) 2004-12-28
HUP0401740A3 HUP0401740A3 (en) 2009-06-29
HU230248B1 HU230248B1 (hu) 2015-11-30

Family

ID=26991691

Family Applications (2)

Application Number Title Priority Date Filing Date
HU0401740A HU230248B1 (hu) 2001-10-26 2002-10-21 N-szubsztituált hidroxipirimidinon-karboxamid HIV-integráz inhibitorok
HUS1600016C HUS1600016I1 (hu) 2001-10-26 2016-04-07 N-szubsztituált hidroxipirimidinon-karboxamid HIV-integráz inhibitorok

Family Applications After (1)

Application Number Title Priority Date Filing Date
HUS1600016C HUS1600016I1 (hu) 2001-10-26 2016-04-07 N-szubsztituált hidroxipirimidinon-karboxamid HIV-integráz inhibitorok

Country Status (35)

Country Link
US (5) US7169780B2 (hu)
EP (1) EP1441735B1 (hu)
JP (1) JP3927175B2 (hu)
KR (1) KR100862879B1 (hu)
CN (3) CN102229605B (hu)
AT (1) ATE318140T1 (hu)
BR (1) BRPI0213522C1 (hu)
CA (1) CA2463976C (hu)
CO (1) CO5580777A2 (hu)
CY (1) CY2008008I1 (hu)
DE (3) DE60209381T2 (hu)
DK (1) DK1441735T3 (hu)
EA (1) EA007060B1 (hu)
ES (1) ES2258668T3 (hu)
FR (1) FR08C0026I2 (hu)
GE (1) GEP20063848B (hu)
HK (1) HK1085665A1 (hu)
HR (1) HRP20040373B1 (hu)
HU (2) HU230248B1 (hu)
IL (2) IL161337A0 (hu)
IS (1) IS2436B (hu)
LT (1) LTC1441735I2 (hu)
LU (1) LU91428I2 (hu)
ME (1) ME00427B (hu)
MX (1) MXPA04003932A (hu)
NL (1) NL300340I2 (hu)
NO (3) NO325206B1 (hu)
NZ (1) NZ533057A (hu)
PL (1) PL212914B1 (hu)
PT (1) PT1441735E (hu)
RS (1) RS51542B (hu)
SI (1) SI1441735T1 (hu)
UA (1) UA77454C2 (hu)
WO (1) WO2003035077A1 (hu)
ZA (1) ZA200402796B (hu)

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