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    • 27. 发明授权
    • 2,4-disubstituted triazine derivatives
    • 2,4-二取代的三嗪衍生物
    • US06638932B1
    • 2003-10-28
    • US09831808
    • 2001-08-02
    • Bart De CorteMarc René de JongeJan HeeresPaul Adriaan Jan JanssenRobert W. KavashLucien Maria Henricus KoymansMichael Joseph KuklaDonald William LudoviciKoen Jeanne Alfons Van Aken
    • Bart De CorteMarc René de JongeJan HeeresPaul Adriaan Jan JanssenRobert W. KavashLucien Maria Henricus KoymansMichael Joseph KuklaDonald William LudoviciKoen Jeanne Alfons Van Aken
    • C07D25116
    • A61K9/146Y10S977/775Y10S977/915
    • This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein —a1═a2—a3═a4— forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl or substituted C1-6alkyl; each R2 independently is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR4, —NH—S(═O)pR4, —C(═O)R4, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R4, —C(═NH)R4 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is —X—R3 wherein R3 is optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl, or pyridazinyl; X is —NR1—, —NH—NH—, —N═N—, —O—, —C(═O)—, —CHOH—, —S—, —S(═O)— or —S(═O)2—; aryl is optionally substituted phenyl; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection.
    • 本发明涉及配制N-氧化物的化合物,药学上可接受的加成盐,季胺及其立体化学异构形式的用途,其中-a 1 = a 2 -a 3 = a 4 - 与连接的乙烯基形成苯基,吡啶基,嘧啶基,哒嗪基或吡嗪基; n为0〜4; 并在可能的情况下5; R 1是氢,芳基,甲酰基,C 1-6烷基羰基,C 1-6烷基,C 1-6烷氧基羰基或取代的C 1-6烷基; 每个R 2独立地是羟基,卤素,任选取代的C 1-6烷基,C 2-6烯基或C 2-6炔基,C 3-7环烷基,C 1-6烷氧基,C 1-6烷氧基羰基,羧基,氰基,硝基,氨基,单或二( C 1-6烷基)氨基,多卤代甲基,多卤甲氧基,多卤甲硫基,-S(= O)p R 4,-NH-S(= O)p R 4,-C(= O)R 4, = O)H,-C(= O)NHNH 2,-NHC(= O)R 4,-C(= NH)R 4或5元杂环; p为1或2; L是任选取代的C 1-10烷基,C 2-10烯基,C 2-10炔基或C 3-7环烷基; 或L是-X-R 3,其中R 3是任选取代的苯基,吡啶基,嘧啶基,吡嗪基或哒嗪基; X是-NR 1 - , - NH-NH-,-N = N-,-O-,-C(= O) - , - CHOH-,-S-,-S(= O) - 或 - S(= O)2-; 芳基是任选取代的苯基; 用于制造用于治疗患有HIV(人类免疫缺陷病毒)感染的受试者的药物。
    • 28. 发明授权
    • HIV inhibiting pyrimidine derivative
    • HIV抑制嘧啶衍生物
    • US06197779B1
    • 2001-03-06
    • US09276360
    • 1999-03-25
    • Koenraad Jozef Lodewijk Marcel AndriesBart De CorteMarc René De JongeJan HeeresChih Yung HoMarcel August Constant JanssenPaul Adriaan Jan JanssenLucien Maria Henricus KoymansMichael Joseph KuklaDonald William LudoviciKoen Jeanne Alfons Van Aken
    • Koenraad Jozef Lodewijk Marcel AndriesBart De CorteMarc René De JongeJan HeeresChih Yung HoMarcel August Constant JanssenPaul Adriaan Jan JanssenLucien Maria Henricus KoymansMichael Joseph KuklaDonald William LudoviciKoen Jeanne Alfons Van Aken
    • A61K31506
    • C07D239/42C07D239/47C07D239/48C07D239/49C07D239/50C07D401/12
    • This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0 to 4; Q is hydrogen or —NR1R2; R1 and R2 are selected from hydrogen, hydroxy, C1-12alkyl, C1-12alkyloxy, C1-12alkylcarbonyl, C1-12alkyloxycarbonyl, aryl, amino, mono- or di(C1-12alkyl)amino, mono- or di(C1-12alkyl)aminocarbonyl wherein each C1-12alkyl may optionally be substituted; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-12alkyl)aminoC1-4alkylidene; R3 is hydrogen, aryl, C1-6alkylcarbonyl, optionally substituted C1-6alkyl, C1-6alkyloxycarbonyl,; and R4 is hydroxy, halo, optionally substituted C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R5 is hydrogen or C1-4alkyl; L is optionally substituted C1-10alkyl, C3-10alkenyl, C3-10alkynyl, C3-7cycloalkyl; or L is —X1—R6 or —X2-Alk-R7 wherein R6 and R7 are optionally substituted phenyl; X1 and X2 are —NR3—, —NH—NH—, —N═N—, —O—, —S—, —S(═O)— or —S(═O)2—; Alk is C1-4alkanediyl; aryl is potionally substituted phenyl; Het is an optionally substituted aliphatic or aromatic heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and compositions comprising them.
    • 本发明涉及N-氧化物,其药学上可接受的加成盐和立体化学异构形式的化合物的用途,其中A是CH,CR 4或N; n为0〜4; Q是氢或-NR1R2; R1和R2选自氢,羟基,C1-12烷基,C1-12烷氧基,C1-12烷基羰基,C1-12烷氧基羰基,芳基,氨基,一或二(C1-12烷基)氨基,单或二(C1-12烷基) 其中每个C 1-12烷基可以任选被取代; 或R 1和R 2可以一起形成吡咯烷基,哌啶基,吗啉基,叠氮基或单或二(C 1-12烷基)氨基C 1-4亚烷基; R 3是氢,芳基,C 1-6烷基羰基,任选取代的C 1-6烷基,C 1-6烷氧基羰基。 R4为羟基,卤素,任选取代的C 1-6烷基,C 1-6烷氧基,氰基,氨基羰基,硝基,氨基,三卤代甲基,三卤代甲氧基; R5是氢或C1-4烷基; L是任选取代的C 1-10烷基,C 3-10烯基,C 3-10炔基,C 3-7环烷基; 或L是-X1-R6或-X2-Alk-R7,其中R6和R7是任选取代的苯基; X1和X2是-NR3-,-NH-NH-,-N = N-,-O - , - S - , - S(= O) - 或-S(= O) Alk是C1-4烷二基; 芳基是取代的苯基; Het是任选取代的脂族或芳族杂环基; 用于制造用于治疗患有HIV(人类免疫缺陷病毒)感染的受试者的药物。 它还涉及作为式(I)化合物的亚组的新化合物,其制备方法和包含它们的组合物。