PROCESS FOR PREPARATION OF CHIRAL 3-AMINOPYRROLIDINE AND ANALOGOUS BICYCLIC COMPOUNDS
    11.
    发明申请
    PROCESS FOR PREPARATION OF CHIRAL 3-AMINOPYRROLIDINE AND ANALOGOUS BICYCLIC COMPOUNDS 审中-公开
    制备三氨基吡啶和类似物双环化合物的方法

    公开(公告)号:WO1998022437A1

    公开(公告)日:1998-05-28

    申请号:PCT/US1997021081

    申请日:1997-11-18

    CPC classification number: C07D207/14 C07D455/02 C07D471/04 Y02P20/55

    Abstract: A process for the preparation of chiral 3-aminopyrrolidine of formula (I) and analogous bicyclic derivatives of formula (II) from dihydroxy olefins such as for the formula: HO-CH2-CH=CH-CH2-OAr by treatment with titanium isopropoxide, an optically active tartrate ester and tert-butyl hydroperoxide, followed by subsequent alkylation of the intermediate with an alkyl or alkenyl magnesium halide, then pyrrolidine ring formation by condensation with an arylmethylamine, subsequent chiral replacement of a ring hydroxyl group with an amino group with further protection thereof, optional additional substitution closing of the second ring, and hydrogenolysis to remove a ring-nitrogen protecting group.

    Abstract translation: 通过用异丙醇钛处理从二羟基烯烃如式HO-CH2-CH = CH-CH2-OAr制备式(I)的手性3-氨基吡咯烷和式(Ⅱ)的类似双环衍生物的方法, 光学活性酒石酸酯和叔丁基过氧化氢,然后用烷基或烯基卤化镁随后烷基化中间体,然后通过与芳基甲胺缩合形成吡咯烷环,随后进一步用氨基取代环羟基 其保护,第二环的任选的另外的取代封闭,以及氢解以除去环 - 氮保护基。

    6-O-SUBSTITUTED KETOLIDES HAVING ANTIBACTERIAL ACTIVITY
    12.
    发明申请
    6-O-SUBSTITUTED KETOLIDES HAVING ANTIBACTERIAL ACTIVITY 审中-公开
    具有抗生素活性的6-O-取代的硬脂酸酯

    公开(公告)号:WO1998009978A1

    公开(公告)日:1998-03-12

    申请号:PCT/US1997015506

    申请日:1997-09-02

    CPC classification number: C07H17/08 Y02P20/55

    Abstract: Antimicrobial compounds having formula (II), (III), (IV), (IV-A) or (V) as well as pharmaceutically acceptable salts, esters or prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compunds.

    Abstract translation: 具有式(II),(III),(IV),(IV-A)或(V)的抗微生物化合物及其药学上可接受的盐,酯或前药; 包含这些化合物的药物组合物; 通过施用这些化合物治疗细菌感染的方法; 以及制备肥料的过程。

    6-O-SUBSTITUTED ERYTHROMYCINS AND METHOD FOR MAKING THEM
    13.
    发明申请
    6-O-SUBSTITUTED ERYTHROMYCINS AND METHOD FOR MAKING THEM 审中-公开
    6-O-取代的红霉素及其制备方法

    公开(公告)号:WO1997042204A1

    公开(公告)日:1997-11-13

    申请号:PCT/US1997004622

    申请日:1997-03-21

    CPC classification number: C07H17/08

    Abstract: Antimicrobial compounds having formula (II), (III), (IV), (V), (VI), (VII), (VIII) and (IX) as well as the pharmaceutically acceptable salts, esters and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.

    Abstract translation: 具有式(II),(III),(IV),(V),(VI),(VII),(VIII)和(IX)的抗微生物化合物及其药学上可接受的盐,酯和前药; 包含这些化合物的药物组合物; 通过施用这些化合物治疗细菌感染的方法; 和化合物的制备方法。

    QUINOLIZINONE TYPE COMPOUNDS
    14.
    发明申请
    QUINOLIZINONE TYPE COMPOUNDS 审中-公开
    喹诺酮类化合物

    公开(公告)号:WO1996039407A1

    公开(公告)日:1996-12-12

    申请号:PCT/US1996008991

    申请日:1996-06-05

    Abstract: Antibacterial compounds having formula (I) and the pharmaceutically acceptable salts, esters and amides thereof, selected preferred examples of which include those compounds wherein A is =CR -; R is cycloalkyl of from three to eight carbon atoms or substituted phenyl; R is selected from the group consisting of (a), (b), (c) and (d); R is halogen; R is hydrogen, loweralkyl, a pharmaceutically acceptable cation, or a prodrug ester group; R is hydrogen, loweralkyl, halo(loweralkyl), or -NR R ; and R is halogen, loeralkyl, halo(loweralkyl), hydroxy-substituted loweralkyl, loweralkoxy(loweralkyl), loweralkoxy, or amino(loweralkyl), as well as pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.

    Abstract translation: 具有式(I)的抗菌化合物及其药学上可接受的盐,酯和酰胺,其选择的优选实例包括其中A = CR 6 - 的那些化合物; R 1是3至8个碳原子的环烷基或取代的苯基; R 2选自(a),(b),(c)和(d); R 3是卤素; R 4是氢,低级烷基,药学上可接受的阳离子或前药酯基; R 5是氢,低级烷基,卤代(低级烷基)或-NR 13 R 14; 和R 6是卤素,低级烷基,卤代(低级烷基),羟基取代的低级烷基,低级烷氧基(低级烷基),低级烷氧基或氨基(低级烷基),以及含有这些化合物的药物组合物及其在治疗中的用途 的细菌感染。

    QUINOBENZOXAZINE, QUINOBENZOTHIAZINE, AND PYRIDO-ACRIDINE ANTINEOPLASTIC AGENTS
    20.
    发明公开
    QUINOBENZOXAZINE, QUINOBENZOTHIAZINE, AND PYRIDO-ACRIDINE ANTINEOPLASTIC AGENTS 失效
    基于CHINOBENZOXAZINEN,CHINOBENZOTHIAZINEN和吡啶并吖啶抗肿瘤物质。

    公开(公告)号:EP0608215A1

    公开(公告)日:1994-08-03

    申请号:EP91918185.0

    申请日:1991-08-23

    CPC classification number: C07D455/00 C07D513/06 Y02P20/55

    Abstract: L'invention se rapporte à de la quinobenzoxazine, des quinobenzothiazines et des dérivés de pyrido-acridine, représentés par la formule (I), ainsi qu'à leurs sels, esters, amides, et pro-médicaments pharmaceutiquement acceptables. Dans la formule (I), R1 représente hydrogène ou un groupe protecteur de carboxy, R2 et R3 représentent des substituants, A représente oxygène, soufre ou carbone, Z représente un halogène ou un groupe contenant de l'azote, X représente hydrogène, halogène ou alkyle, et W représente hydrogène, alkyle, amino ou halogène. Ces composés ont un pouvoir antinéoplastique puissant.

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