HUP0104177A2 - HIV-vírus szaporodását gátló pirimidin-származékok, eljárás az előállításukra, illetve ezeket tartalmazó gyógyászati készítmények - Google Patents

HIV-vírus szaporodását gátló pirimidin-származékok, eljárás az előállításukra, illetve ezeket tartalmazó gyógyászati készítmények

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Publication number
HUP0104177A2
HUP0104177A2 HU0104177A HUP0104177A HUP0104177A2 HU P0104177 A2 HUP0104177 A2 HU P0104177A2 HU 0104177 A HU0104177 A HU 0104177A HU P0104177 A HUP0104177 A HU P0104177A HU P0104177 A2 HUP0104177 A2 HU P0104177A2
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HU
Hungary
Prior art keywords
group
mono
general formula
alkyl
alkoxycarbonyl
Prior art date
Application number
HU0104177A
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English (en)
Inventor
Koen Jeanne Alfons Aken
Bart De Corte
Jan Heeres
Chih Yung Ho
Paul Adriaan Jan Janssen
Robert W. Kavash
Lucien Maria Henricus Koymans
Michael Joseph Kukla
Donald William Ludovici
Marc René de Jonge
Original Assignee
Janssen Pharmaceutica N.V.
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=26805159&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HUP0104177(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Janssen Pharmaceutica N.V. filed Critical Janssen Pharmaceutica N.V.
Publication of HUP0104177A2 publication Critical patent/HUP0104177A2/hu
Publication of HUP0104177A3 publication Critical patent/HUP0104177A3/hu
Publication of HU227453B1 publication Critical patent/HU227453B1/hu

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D403/12—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • 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
    • 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
    • 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
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/80—Oxygen atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

A találmány pirimidinszármazékoknak a humán immunhiányos vírus (HIV)szaporodását gátló hatású gyógyászati készítmények előállítására valóalkalmazására, továbbá új pirimidinszármazékokra, ezek gyógyászatihasznosítására és előállítására, illetve az új vegyületeket tartalmazógyógyászati készítményekre vonatkozik. A találmány szerinti, részbenúj vegyületek (I) általános képletében -a1=a2-a3=a4- jelentése akövetkezőkben felsorolt kétvegyértékű csoportok valamelyike: -CH=CH-CH=CH- (a-1); -N=CH-CH=CH- (a-2); -N=CH-N=CH- (a-3); -N=CH-CH=N- (a-4); vagy -N=N-CH=CH- (a-5); n értéke0, 1, 2, 3 vagy 4; és ha -a1=a2-a3=a4- jelentése (a-1) képletűcsoport, akkor n értéke 5 is lehet; R1 jelentése hidrogénatom vagyaril-, formil-, alkil-karbonil-, alkil-, alkoxi-karbonil-,szubsztituált alkilcsoport; vagy pedig alkoxi-karbonil-csoporttalszubsztituált alkoxi-alkil-karbonil-csoport; és mindegyik R2 egymástólfüggetlenül halogénatomot vagy hidroxil-, szubsztituált cikloalkil-,adott esetben szubsztituált alkenil-, alkinil-, alkoxi-, alkoxi-karbonil-, karboxil-, ciano-, nitro-, amino-, mono- vagy dialkil-amino-, polihalogén-metil-, polihalogén-metoxi-, polihalogén-metil-tio- vagy -S(=O)pR6-; -NH-S(=O)pR6-; -C(=O)R6-; -NHC(=O)H; -C(=O)NHNH2-; -NHC(=O)R6-; -C(=NH)R6 vagy (c) általános képletűcsoportot jelent; és az utóbbi képletben mindegyik A egymástólfüggetlenül nitrogénatomot vagy metincsoportot, vagy CR6 általánosképletű csoportot, és B iminocsoportot, vagy oxigén- vagy kénatomot,vagy -NR6 általános képletű csoportot jelent; p értéke 1 vagy 2; és R6jelentése metil-, amino-, mono- vagy dimetil-amino- vagy polihalogén-metil-csoport; L jelentése alkil-, alkenil-, alkinil- vagycikloalkilcsoport, mimellett mindegyik említett alifás csoport adottesetben szubsztituálva lehet, vagy L jelentése -X-R3 általános képletűcsoport, ahol R3 jelentése fenil-, piridinil-, pirimidinil-,pirazinil- vagy piridazinilcsoport, mely aromás gyűrűk mindegyikeadott esetben szubsztituálva lehet, és X jelentése -NR1-, -NH-NH-, -N=N-, -O-, -C(=O)-, -CHOH-, -S-, -S(=O)- vagy -S(=O)2- csoport; Qjelentése hidrogén- vagy halogénatom, vagy alkil-, polihalogén-alkil-vagy -NR4R5 általános képletű csoport; és R4 és R5egymástólfüggetlenül hidrogénatomot vagy hidroxi-, adott esetben szubsztituáltalkil-, alkoxi-, alkil-karbonil-, alkil-oxi-karbonil-, aril-, amino-,mono- vagy dialkil-amino-, vagy mono- vagy dialkil-amino-karbonil-csoportot jelent, vagy R4 és R5együtt pirrolidinil-, piperidinil-,morfolinil-, azido- vagy mono- vagy dialkil-amino-alkilidén-csoportotalkotnak; Y jelentése halogénatom; hidroxil-, cikloalkil-, adottesetben szubsztituált alkenil-, alkinil-; ciano- vagy -C(=O)R6-általános képletű csoporttal szubsztituált alkil-, alkoxi-, alkoxi-karbonil-, karboxil-, ciano-, nitro-, amino-, mono- va
HU0104177A 1998-11-10 1999-09-24 Hiv replication inhibiting pyrimidines, and pharmaceutical compositions containing them HU227453B1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US10779298P 1998-11-10 1998-11-10
US14396299P 1999-07-15 1999-07-15
PCT/EP1999/007417 WO2000027825A1 (en) 1998-11-10 1999-09-24 Hiv replication inhibiting pyrimidines

Publications (3)

Publication Number Publication Date
HUP0104177A2 true HUP0104177A2 (hu) 2002-03-28
HUP0104177A3 HUP0104177A3 (en) 2003-01-28
HU227453B1 HU227453B1 (en) 2011-06-28

Family

ID=26805159

Family Applications (2)

Application Number Title Priority Date Filing Date
HU1100091A HU230394B1 (hu) 1998-11-10 1999-09-24 HIV-vírus szaporodását gátló pirimidin-származékok
HU0104177A HU227453B1 (en) 1998-11-10 1999-09-24 Hiv replication inhibiting pyrimidines, and pharmaceutical compositions containing them

Family Applications Before (1)

Application Number Title Priority Date Filing Date
HU1100091A HU230394B1 (hu) 1998-11-10 1999-09-24 HIV-vírus szaporodását gátló pirimidin-származékok

Country Status (41)

Country Link
US (5) US6878717B2 (hu)
EP (2) EP1002795B1 (hu)
JP (1) JP3635238B2 (hu)
KR (1) KR100658489B1 (hu)
CN (1) CN1214013C (hu)
AP (1) AP1683A (hu)
AR (1) AR024227A1 (hu)
AT (2) ATE455107T1 (hu)
AU (2) AU762523C (hu)
BG (1) BG65103B1 (hu)
BR (1) BRPI9915552B8 (hu)
CA (1) CA2350801C (hu)
CY (1) CY2008021I1 (hu)
CZ (1) CZ301367B6 (hu)
DE (3) DE69905683T2 (hu)
DK (1) DK1002795T3 (hu)
EA (1) EA004049B1 (hu)
EE (1) EE05086B1 (hu)
ES (2) ES2193664T3 (hu)
FR (1) FR09C0004I2 (hu)
HK (2) HK1025330A1 (hu)
HR (2) HRP20010161B9 (hu)
HU (2) HU230394B1 (hu)
ID (1) ID28376A (hu)
IL (2) IL143023A0 (hu)
LT (1) LTC1002795I2 (hu)
LU (1) LU91528I2 (hu)
MY (1) MY121108A (hu)
NL (1) NL300373I2 (hu)
NO (3) NO318801B1 (hu)
NZ (1) NZ511116A (hu)
OA (1) OA11674A (hu)
PL (1) PL204427B1 (hu)
PT (1) PT1002795E (hu)
SI (1) SI1002795T1 (hu)
SK (2) SK287269B6 (hu)
TR (1) TR200101306T2 (hu)
TW (1) TWI238161B (hu)
UA (1) UA70966C2 (hu)
WO (1) WO2000027825A1 (hu)
ZA (1) ZA200103769B (hu)

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