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    METHOD OF PREPARING 21-ALKYLATED PREGNA-1,4,16-TRIEN-3,20-DIONES
    31.
    发明申请
    METHOD OF PREPARING 21-ALKYLATED PREGNA-1,4,16-TRIEN-3,20-DIONES 审中-公开
    制备21-烷基丙酰-1,4,16-三烯-3,20-二酮的方法

    公开(公告)号：WO1998018813A1

    公开(公告)日：1998-05-07

    申请号：PCT/US1997019276

    申请日：1997-10-22

    Applicant: ALCON LABORATORIES, INC. ,  CONROW, Raymond, E.

    Inventor： ALCON LABORATORIES, INC.

    IPC: C07J13/00

    CPC classification number: C07J51/00 ,  C07J13/005 ,  C07J71/0015

    Abstract: Methods for preparing intermediates for 21-alkylated corticosteroids are discloded. Pregna-1,4,16-trien-3,20-diones are contacted with a base and an alkylating agent to produce corresponding 21-alkylated pregna-1,4,16-trien-3,20-diones.

    Abstract translation: 制备21烷基化皮质类固醇中间体的方法已被剥离。 将前草-1,4,16-三烯-3,20-二酮与碱和烷基化剂接触以产生相应的21-烷基化的前 - 1,4,16-三烯-3,20-二酮。

    PRESERVATIVE SYSTEMS FOR PHARMACEUTICAL COMPOSITIONS CONTAINING CYCLODEXTRINS
    32.
    发明申请
    PRESERVATIVE SYSTEMS FOR PHARMACEUTICAL COMPOSITIONS CONTAINING CYCLODEXTRINS 审中-公开
    含有CYCLODEXTRINS的药物组合物的防腐剂系统

    公开(公告)号：WO1998006381A1

    公开(公告)日：1998-02-19

    申请号：PCT/US1997014119

    申请日：1997-08-08

    Applicant: ALCON LABORATORIES, INC. ,  CASTILLO, Ernesto, J. ,  ESPINO, Ramon, L.

    Inventor： ALCON LABORATORIES, INC.

    IPC: A61K09/00

    CPC classification number: A61K47/186 ,  A61K9/0048 ,  A61K47/02 ,  A61K47/12 ,  A61K47/183 ,  A61K47/24

    Abstract: Disclosed are preservative systems useful in aqueous pharmaceutical compositions containing an active agent and a cyclodextrin. The preservative systems comprise boric acid and one or more compounds selected from the group consisting of C16 benzalkonium halide compounds, polymeric quaternary ammonium compounds, and quaternary ammonium alkylene glycol phospholipid derivatives of structure (I), where a + b = 3; R is C8-C22 alkyl or alkene; X is NH, O or CH2; R is C2-C6 alkyl; each R is independently C1-C12 alkyl or alkene; and Y is nothing or C1-C6 alkyl or alkene; and pharmaceutically acceptable salts thereof.

    Abstract translation: 公开了可用于含有活性剂和环糊精的水性药物组合物中的防腐剂体系。 防腐体系包括硼酸和一种或多种选自C16苯扎氯铵化合物，聚合季铵化合物和结构（I）的季铵亚烷基二醇磷脂衍生物的化合物，其中a + b = 3; R 1是C 8 -C 22烷基或烯烃; X是NH，O或CH 2; R 2是C 2 -C 6烷基; 每个R 3独立地为C 1 -C 12烷基或烯烃; 且Y不为或C 1 -C 6烷基或烯烃; 及其药学上可接受的盐。

    THIAZOLIDINE-4-CARBOXYLIC ACID DERIVATIVES AS CYTOPROTECTIVE AGENTS
    34.
    发明申请
    THIAZOLIDINE-4-CARBOXYLIC ACID DERIVATIVES AS CYTOPROTECTIVE AGENTS 审中-公开
    作为杀菌剂的噻唑烷-4-羧酸衍生物

    公开(公告)号：WO1997035852A1

    公开(公告)日：1997-10-02

    申请号：PCT/US1997004387

    申请日：1997-03-19

    Applicant: ALCON LABORATORIES, INC. ,  HELLBERG, Mark, R.

    Inventor： ALCON LABORATORIES, INC.

    IPC: C07D277/06

    CPC classification number: C07D417/04 ,  C07D277/06 ,  C07D417/12

    Abstract: Compounds useful as cytoprotective agents of formula (I), wherein z = (a) and (b); n = 0-12; m = 0-12; X = nothing, NR , O, or S(O)n'; provided that when X = NR , O, or S(O)n', then m>0 and n>0; n' = 0-2; R = H, C1-C6 alkyl; R = OH or a pharmaceutically acceptable salt thereof, C1-C6 alkoxyl, amino, mono- or dialkylamino where the alkyl has from 1 to 4 carbon atoms, or a radical of an amino acid of the formula: -NH-(CH2)n-CH(R )-CO-R ; R = H, C1-C4 alkyl, optionally substituted by hydroxy, SH, SCH3, or (un)substituted phenyl; and R = OH, C1-C6 alkoxyl, amino, or mono- or dialkyl amino where the alkyl has from 1 to 4 carbon atoms. The compounds possess dual activity, containing a phenolic portion selected to have antioxidant or free radical scavenging properties and a thiazolidine-4-carboxylate portion selected for its potential to act as a cysteine prodrug.

    Abstract translation: 可用作式（I）的细胞保护剂的化合物，其中z =（a）和（b）; n = 0-12; m = 0-12; X =无，NR 1，O或S（O）n'; 条件是当X = NR 1，O或S（O）n'时，则m> 0且n> 0; n'= 0-2; R 1 = H，C 1 -C 6烷基; R = OH或其药学上可接受的盐，其中烷基具有1至4个碳原子的C 1 -C 6烷氧基，氨基，一或二烷基氨基，或下式的氨基酸基团-NH-（CH 2）n -CH（R <2>） - CO-R <3>; R 2 = H，任选被羟基取代的C 1 -C 4烷基，SH，SCH 3或（未）取代的苯基; 和R 3 = OH，C 1 -C 6烷氧基，氨基或单或二烷基氨基，其中烷基具有1至4个碳原子。 该化合物具有双重活性，其含有被选择具有抗氧化剂或自由基清除性质的酚类部分和选择用作半胱氨酸前药的潜力的噻唑烷-4-羧酸酯部分。

    USE OF AMIDOAMINES IN OPHTHALMIC COMPOSITIONS
    40.
    发明申请
    USE OF AMIDOAMINES IN OPHTHALMIC COMPOSITIONS 审中-公开
    氨基甲酸酯在眼科组合物中的应用

    公开(公告)号：WO1996026747A2

    公开(公告)日：1996-09-06

    申请号：PCT/US1996002588

    申请日：1996-02-26

    Applicant: ALCON LABORATORIES, INC.

    Inventor： ALCON LABORATORIES, INC. ,  DASSANAYAKE, Nissanke, L. ,  SCHLITZER, Ronald, L. ,  PARK, Joonsup

    IPC: A61L02/18

    CPC classification number: A61K31/164 ,  A01N37/20 ,  A01N37/36 ,  A01N37/44 ,  A61L12/12 ,  Y10S514/84

    Abstract: The use of certain amidoamines to disinfect contact lenses and preserve ophthalmic compositions is described. Ophthalmic compositions containing these compounds as disinfecting agents or preservatives are also described. The amidoamines utilized in the present invention have potent antibacterial and antifungal activity, and are chemically compatible with inorganic ions and other materials utilized in ophthalmic compositions.

    Abstract translation: 描述使用某些酰氨基胺消毒隐形眼镜并保护眼用组合物。 还描述了含有这些化合物作为消毒剂或防腐剂的眼科组合物。 本发明中使用的酰氨基胺具有有效的抗细菌和抗真菌活性，并且与眼用组合物中所用的无机离子和其它材料化学相容。

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