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    • 3. 发明申请
    • ANTI-HELICOBACTER ACYL DERIVATIVES OF AZOLONES
    • 丙二醇的抗真菌ACYL衍生物
    • WO1996001822A1
    • 1996-01-25
    • PCT/EP1995002618
    • 1995-07-05
    • JANSSEN PHARMACEUTICA N.V.HEERES, JanSTOKBROEKX, Raymond, AntoineMOSTMANS, Joseph, HectorVAN DER VEKEN, Louis, Jozef, Elisabeth
    • JANSSEN PHARMACEUTICA N.V.
    • C07D403/12
    • C07D401/04C07D233/70C07D249/12C07D401/12C07D401/14C07D403/12C07D405/12C07D409/12
    • The invention is concerned with the compounds having formula (I), the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Y is CH or N; R , R and R each independently are hydrogen or C1-4alkyl; R and R each independently are hydrogen, halo, C1-4alkyl, C1-4alkyloxy, hydroxy, trifluoromethyl, trifluoromethyloxy or difluoromethyloxy; R is hydrogen; or R is phenyl optionally substituted with halo; pyridinyl; furanyl; thienyl; 3-chlorobenzo[b]thien-2-yl; trifluoromethyl; C1-4alkyloxycarbonyl; dihalophenylcyclopropanyl; C3-6cycloalkyl; adamantyl; C2-6alkenyl optionally substituted with halophenyl; or C1-4alkyl optionally substituted with halo, phenyl, halophenyl, dihalophenyl, phenyloxy, piperidinyl, pyrrolidinyl, piperazinyl, C1-4alkylpiperazinyl, C1-4alkyl-carbonylpiperazinyl, C1-4alkyloxycarbonylpiperazinyl, phthalimino, amino, mono- or di(C1-20)alkylamino or C3-6cycloalkylamino; Z is C=O or CHOH; and (1) is a radical of formula (a-1), (a-2), (a-3), (a-4), (a-5), (a-6), or (a-7). Compositions comprising said compounds, processes for preparing the same and the use of these compounds as a medicine.
    • 本发明涉及具有式(I)的化合物,其药学上可接受的加成盐和立体化学异构形式,其中Y是CH或N; R 1,R 2和R 3各自独立地是氢或C 1-4烷基; R 4和R 5各自独立地为氢,卤素,C 1-4烷基,C 1-4烷氧基,羟基,三氟甲基,三氟甲氧基或二氟甲氧基; R 6是氢; 或R 6为任选被卤素取代的苯基; 吡啶基; 呋喃基; 噻吩; 3-氯苯并[b]噻吩-2-基; 三氟甲基; C1-4alkyloxycarbonyl; dihalophenylcyclopropanyl; 3-6环; 金刚; 任选被卤代苯基取代的C 2-6烯基; 哌啶基,吡咯烷基,哌嗪基,C 1-4烷基哌嗪基,C 1-4烷基 - 羰基哌嗪基,C 1-4烷氧基羰基哌嗪基,邻苯二甲酰亚氨基,氨基,单或二(C1-20) 烷基氨基或C 3-6环烷基氨基; Z是C = O或CHOH; (a-3),(a-4),(a-5),(a-6)或(a-7)中的基团,式(a-1),(a-2),(a-3) )。 包含所述化合物的组合物,其制备方法以及这些化合物作为药物的用途。
    • 5. 发明申请
    • ANTI-HELICOBACTER HETEROCYCLIC DERIVATIVES OF AZOLONES
    • 丙二醇的抗真菌剂杂环衍生物
    • WO1996001821A1
    • 1996-01-25
    • PCT/EP1995002616
    • 1995-07-05
    • JANSSEN PHARMACEUTICA N.V.HEERES, JanSTOKBROEKX, Raymond, AntoineWILLEMS, MarcHENDRICKX, Robert, Jozef, Maria
    • JANSSEN PHARMACEUTICA N.V.
    • C07D403/12
    • C07D401/14C07D403/12C07D413/12C07D417/14
    • The invention is concerned with the compounds having formula (I), the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Y is CH or N; R , R and R each independently are hydrogen or C1-4alkyl; R and R each independently are hydrogen, halo, C1-4alkyl, C1-4alkyloxy, hydroxy, trifluoromethyl, trifluoromethyloxy or difluoromethyloxy; R is pyridinyl optionally substituted with up to two C1-4alkyl groups; di(C1-4alkyl)hydroxypyridinyl; di(C1-4alkyl)C1-4alkyloxypyridinyl; pyridazinyl optionally substituted with C1-4alkyloxy; pyrimidinyl optionally substituted with hydroxy or C1-4alkyloxy; thiazolyl optionally substituted with C1-4alkyl; thiadiazolyl optionally substituted with C1-4alkyl; benzoxazolyl or benzothiazolyl; or R is pyrazinyl or pyridazinyl substituted with C1-4alkyl; Z is C=O or CHOH; and (a) is a radical of formula (a-1), (a-2), (a-3), (a-4), (a-5), (a-6), or (a-7). Compositions comprising said compounds, processes for preparing the same and the use of these compounds as a medicine.
    • 本发明涉及具有式(I)的化合物,其药学上可接受的加成盐和立体化学异构形式,其中Y是CH或N; R 1,R 2和R 3各自独立地是氢或C 1-4烷基; R 4和R 5各自独立地为氢,卤素,C 1-4烷基,C 1-4烷氧基,羟基,三氟甲基,三氟甲氧基或二氟甲氧基; R 6是任选被至多两个C 1-4烷基取代的吡啶基; 二(C 1-4烷基)羟基吡啶基; 二(C 1-4烷基)C1-4alkyloxypyridinyl; 任选被C 1-4烷氧基取代的哒嗪基; 任选被羟基或C 1-4烷氧基取代的嘧啶基; 任选被C 1-4烷基取代的噻唑基; 任选被C 1-4烷基取代的噻二唑基; 苯并恶唑基或苯并噻唑基; 或R 6是被C 1-4烷基取代的吡嗪基或哒嗪基; Z是C = O或CHOH; 和(a)是式(a-1),(a-2),(a-3),(a-4),(a-5),(a-6)或(a-7) )。 包含所述化合物的组合物,其制备方法以及这些化合物作为药物的用途。
    • 8. 发明申请
    • ANGIOGENESIS INHIBITING PYRIDAZINAMINES
    • 血管生成抑制吡咯烷胺
    • WO1997026258A1
    • 1997-07-24
    • PCT/EP1997000201
    • 1997-01-14
    • JANSSEN PHARMACEUTICA N.V.STOKBROEKX, Raymond, AntoineVAN DER AA, Marcel, Jozef, MariaWILLEMS, MarcMEERPOEL, LievenLUYCKX, Marcel, Gerebernus, MariaTUMAN, Robert, W.
    • JANSSEN PHARMACEUTICA N.V.
    • C07D417/04
    • C07D417/04C07D417/14
    • This invention concerns compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is CH or N; m is 2 or 3 and n is 1, 2 or 3; wherein 1 or 2 C-atoms of the CH2 groups of the (a) moiety, which may also contain one double bond, may be substituted with C1-6alkyl, amino, aminocarbonyl, mono- or di(C1-6alkyl)amino, C1-6alkyloxycarbonyl, C1-6alkylcarbonylamino, hydroxy or C1-6alkyloxy; and/or 2 C-atoms of said CH2 groups may be bridged with C2-4alkanediyl; R is hydrogen, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, mono- or di(C1-6alkyl)amino, Ar, ArNH-, C3-6cycloalkyl, hydroxymethyl or benzyloxymethyl; R and R are hydrogen, or taken together may form a bivalent radical of the formula -CH=CH-CH=CH-; in case X represents CH then L is a radical L , L or L ; or in case X represents N then L is a radical L or L ; L is Ar-C1-6alkyloxy, Ar-oxy, Ar-thio, Ar-carbonylamino, di-Ar-methyloxy-, N-Ar-piperazinyl, N-Ar-homopiperazinyl, 2-benzimidazolinonyl, Ar-NR -, Ar-Alk-NR -, Ar-NR -Alk-NR - or Het-NR -; L is Ar, Ar-carbonyl, Ar-CH=CH-CH2-, naphtalenyl or Het; L is C1-6alkyl substituted with one or two radicals selected from Ar, Ar-oxy, or Ar-thio, further optionally substituted with cyano or hydroxy; 2,2-dimethyl-1,2,3,4-tetrahydro-naphtalenyl; 2,2-dimethyl-1H-2,3-dihydroindenyl; Ar-piperidinyl or Ar-NR -Alk-; R and R are each independently selected from hydrogen or C1-6alkyl; Alk is C1-6alkanediyl; their preparation, compositions containing them and their use as a medicine.
    • 本发明涉及式(I)的化合物,N-氧化物形式,其药学上可接受的酸加成盐和立体化学异构形式,其中X是CH或N; m为2或3,n为1,2或3; 其中也可以含有一个双键的(a)部分的CH 2基团的1或2个C原子可以被C 1-6烷基,氨基,氨基羰基,一或二(C 1-6烷基)氨基,C 1 1-6烷氧基羰基,C 1-6烷基羰基氨基,羟基或C 1-6烷氧基; 和/或所述CH 2基团的2个C原子可以与C 2-4烷二基桥接; R 1是氢,C 1-6烷基,C 1-6烷氧基,C 1-6烷硫基,氨基,单或二(C 1-6烷基)氨基,Ar,ArNH-,C 3-6环烷基,羟甲基或苄氧基甲基; R 2和R 3是氢或一起可以形成式-CH = CH-CH = CH-的二价基团; 在X表示CH的情况下,L是基团L 1,L 2或L 3; 或者在X表示N的情况下,L是基团L 2或L 3; L 1是Ar-C 1-6烷氧基,Ar-氧基,Ar-硫基,Ar-羰基氨基,二-Ar-甲氧基 - ,N-Ar-哌嗪基,N-Ar-高哌嗪基,2-苯并咪唑啉酮基,Ar- Ar-Alk-NR 4 - ,Ar-NR 4 -Alk-NR 5 - 或Het-NR 4 - ; L 2是Ar,Ar-羰基,Ar-CH = CH-CH 2 - ,萘基或Het; L 3是被一个或两个选自Ar,Ar-氧基或Ar-硫基的基团取代的C 1-6烷基,进一步任选被氰基或羟基取代; 2,2-二甲基-1,2,3,4-四氢naphtalenyl; 2,2-二甲基-1H-2,3-二氢; Ar-哌啶基或Ar-NR 4 -Alk-; R 4和R 5各自独立地选自氢或C 1-6烷基; Alk是C1-6烷二基; 其制剂,含有它们的组合物及其作为药物的用途。