HUP0101204A2 - HIV-gátló pirimidinszármazékok és a vegyületeket tartalmazó gyógyászati készítmények - Google Patents

HIV-gátló pirimidinszármazékok és a vegyületeket tartalmazó gyógyászati készítmények

Info

Publication number
HUP0101204A2
HUP0101204A2 HU0101204A HUP0101204A HUP0101204A2 HU P0101204 A2 HUP0101204 A2 HU P0101204A2 HU 0101204 A HU0101204 A HU 0101204A HU P0101204 A HUP0101204 A HU P0101204A HU P0101204 A2 HUP0101204 A2 HU P0101204A2
Authority
HU
Hungary
Prior art keywords
alkyl
group
optionally substituted
amino
atom
Prior art date
Application number
HU0101204A
Other languages
English (en)
Inventor
Koenraad Jozef Lodewijk Marcel Andries
Jan Heeres
Chih Yung Ho
Marcel August Constant Janssen
Paul Adriaan Jan Janssen
Lucien Maria Henricus Koymans
Michael Joseph Kukla
Donald William Ludovici
Bart De Corte
Marc René de Jonge
Koen Jeanne Alfons Van Aken
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=27239326&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HUP0101204(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from EP98201587A external-priority patent/EP0945442A1/en
Application filed by Janssen Pharmaceutica N.V. filed Critical Janssen Pharmaceutica N.V.
Publication of HUP0101204A2 publication Critical patent/HUP0101204A2/hu
Publication of HUP0101204A3 publication Critical patent/HUP0101204A3/hu
Publication of HU230522B1 publication Critical patent/HU230522B1/hu

Links

Classifications

    • 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
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • 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
    • 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
    • C07D239/02—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
    • C07D239/48—Two nitrogen atoms
    • 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
    • C07D239/48—Two nitrogen atoms
    • C07D239/49—Two nitrogen atoms with an aralkyl radical, or substituted aralkyl radical, attached in position 5, e.g. trimethoprim
    • 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
    • C07D239/50—Three nitrogen 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
    • C07D401/12—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

Abstract

A találmány tárgya (I) általános képletű vegyületek N-oxidjai,gyógyászatilag elfogadható addíciós sói és sztereokémiai izomer formáialkalmazása, ahol A jelentése HC, CR4 vagy N; n értéke 0-4; Qjelentése hidrogénatom vagy -NR1R2; R1 és R2 egymástól függetlenülhidrogénatom, hidroxil-, 1-12 szénatomos alkil-, 1-12 szénatomosalkoxi-, 1-12 szénatomos alkilkarbonil-, 1-12 szénatomosalkoxikarbonil-, aril-, amino-, mono- vagy di(1-12 szénatomos alkil)-amino-, mono- vagy di(1-12 szénatomos alkil)-aminokarbonil-csoport,ahol az 1-12 szénatomos alkilcsoportok adott esetben szubsztituálvalehetnek, vagy R1 és R2 együtt képezhet pirrolidinil-, piperidinil-,morfolinil-, azido- vagy mono- vagy di(1-12 szénatomos alkil)-amino-(1-4 szénatomos alkilidén)-csoportot, R3 jelentése hidrogénatom,aril-, 1-6 szénatomos alkilkarbonil-, adott esetben szubsztituált 1-6szénatomos alkil-, 1-6 szénatomos alkoxikarbonilcsoport, és R4jelentése hidroxil-, halogénatom, adott esetben szubsztituált 1-6szénatomos alkil- vagy alkoxicsoport, cianocsoport, aminokarbonil-,nitro-, amino-, trihalometil-, trihalometoxicsoport; R5 jelentésehidrogénatom vagy 1-4 szénatomos alkilcsoport, L jelentése adottesetben szubsztituált 1-10 szénatomos alkil-, 3-10 szénatomosalkenil-, 3-10 szénatomos alkinil-, 3-7 szénatomos cikloalkilcsoport,vagy L jelentése -X1-R6 vagy -X2-Alk-R7, ahol R6 és R7 adott esetbenszubsztituált fenilcsoport, X1 és X2 jelentése -NR3, -NH-NH-, -N=N-, -O-, -S-, -S(=O)- vagy -S(=O)2-csoport; Alk jelentése 1-4 szénatomosalkándiilcsoport; aril jelentése adott esetben szubsztituáltfenilcsoport, Het jelentése adott esetben szubsztituált alifás vagyaromás heterociklusos csoport, gyógyszer előállítására, amellyel HIV,azaz humán immunhiány vírusfertőzésben szenvedő paciensek kezelhetők.Kiterjed a találmány továbbá az (I) általános képletű vegyületek egycsoportját képező új vegyületekre, előállításukra és a vegyületekettartalmazó készítményekre. Ó
HU0101204A 1998-03-27 1999-03-24 HIV-gátló pirimidinszármazékok HU230522B1 (hu)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US7963298P 1998-03-27 1998-03-27
US60/079,632 1998-03-27
EP98201587A EP0945442A1 (en) 1998-03-27 1998-05-14 Trisubstituted pyrimidine derivatives
EP98201587.7 1998-05-14
EP98203948 1998-11-25
EP98203948.9 1998-11-25
PCT/EP1999/002043 WO1999050250A1 (en) 1998-03-27 1999-03-24 Hiv inhibiting pyrimidine derivatives

Publications (3)

Publication Number Publication Date
HUP0101204A2 true HUP0101204A2 (hu) 2001-10-28
HUP0101204A3 HUP0101204A3 (en) 2002-08-28
HU230522B1 HU230522B1 (hu) 2016-10-28

Family

ID=27239326

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0101204A HU230522B1 (hu) 1998-03-27 1999-03-24 HIV-gátló pirimidinszármazékok

Country Status (32)

Country Link
EP (2) EP0945443B9 (hu)
JP (1) JP3507917B2 (hu)
KR (1) KR100699514B1 (hu)
CN (1) CN1214014C (hu)
AP (1) AP1468A (hu)
AT (1) ATE232521T1 (hu)
AU (1) AU751573C (hu)
BG (1) BG64702B1 (hu)
CA (1) CA2324919C (hu)
CZ (1) CZ299380B6 (hu)
DE (1) DE69905306T2 (hu)
DK (1) DK0945443T3 (hu)
EA (1) EA002973B1 (hu)
EE (1) EE04850B1 (hu)
ES (1) ES2193660T3 (hu)
HK (1) HK1035901A1 (hu)
HR (1) HRP20000620B1 (hu)
HU (1) HU230522B1 (hu)
ID (1) ID26291A (hu)
IL (1) IL138669A0 (hu)
MY (1) MY126493A (hu)
NO (1) NO317424B1 (hu)
NZ (1) NZ506679A (hu)
OA (1) OA11492A (hu)
PL (1) PL202675B1 (hu)
PT (1) PT945443E (hu)
SI (1) SI0945443T1 (hu)
SK (1) SK287996B6 (hu)
TR (1) TR200002760T2 (hu)
TW (1) TW531534B (hu)
UA (1) UA72458C2 (hu)
WO (1) WO1999050250A1 (hu)

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