Substituted imidazolidine derivatives, their preparation, their use and pharmaceutical preparations including them
    33.
    发明授权
    Substituted imidazolidine derivatives, their preparation, their use and pharmaceutical preparations including them 有权
    取代的咪唑烷衍生物,其制备方法,用途及包括它们在内的药物制剂

    公开(公告)号:US06331552B1

    公开(公告)日:2001-12-18

    申请号:US09516587

    申请日:2000-03-01

    IPC分类号: A61K31415

    CPC分类号: C07K5/0202 C07K5/1016

    摘要: Substituted imidazolidine derivatives of the formula I, in which B, E, W, Y, R, R2, R3, R30, e and h have the meanings indicated in the claims. The compounds of the formula I are valuable pharmaceutical active compounds, which are suitable, for example, for the therapy of inflammatory disorders, for example of rheumatoid arthritis, or of allergic disorders. The compounds of the formula I are inhibitors of the adhesion and migration of leucocytes and/or antagonists of the adhesion receptor VLA-4 belonging to the integrins group. They are generally suitable for the therapy or prophylaxis of illnesses which are caused by an undesired extent of leucocyte adhesion and/or leucocyte migration or are associated therewith, or in which cell-cell or cell-matrix interactions which are based on interactions of VLA-4 receptors with their ligands play a part. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use, in particular as pharmaceutical active compounds, and pharmaceutical preparations which contain compounds of the formula I.

    摘要翻译: 取代的式I的咪唑烷衍生物,其中B,E,W,Y,R,R 2,R 3,R 30,e和h具有权利要求中所示的含义。 式I的化合物是有价值的药物活性化合物,其适用于例如治疗炎症性疾病,例如类风湿性关节炎或过敏性疾病。 式I的化合物是属于整联蛋白组的粘附受体VLA-4的白细胞和/或拮抗剂的粘附和迁移的抑制剂。 它们通常适用于治疗或预防由不良程度的白细胞粘附和/或白细胞迁移或与之相关的疾病或其中基于VLA- 4受体与其配体发挥作用。 本发明还涉及制备式I化合物,其用途,特别是作为药物活性化合物的方法和含有式I化合物的药物制剂。

    Filter arrangement and a method for its manufacture
    35.
    发明授权
    Filter arrangement and a method for its manufacture 失效
    过滤装置及其制造方法

    公开(公告)号:US06179891B2

    公开(公告)日:2001-01-30

    申请号:US09130035

    申请日:1998-08-04

    IPC分类号: B01D2907

    摘要: A filter arrangement made up of an accordion fold pack which is sealingly arranged in a housing. The housing is deep drawn in one piece from a polymeric material sheet. A limit stop is punched out of the base of the housing. A seal surrounds the accordion fold pack and seals against the housing.

    摘要翻译: 一种过滤器装置,其由密封地布置在壳体中的手风琴折叠组件构成。 外壳从聚合物材料片中深度拉成一体。 极限挡块从外壳的底部冲出。 密封圈围绕手风琴折叠包装并密封住外壳。

    Polymer-conjugated malonic acid derivatives and their use as medicaments
and diagnostic agents
    36.
    发明授权
    Polymer-conjugated malonic acid derivatives and their use as medicaments and diagnostic agents 失效
    聚合物共轭丙二酸衍生物及其作为药物和诊断剂的用途

    公开(公告)号:US5817742A

    公开(公告)日:1998-10-06

    申请号:US718524

    申请日:1996-09-11

    摘要: Polymer-based polyvalent malonic acid derivatives having anti-adhesive properties are described. The compounds comprise a polyamino acid linked to a group of formula (I). In formula (I), R.sup.1 and R.sup.2 together form a six-membered carbocylic or heterocyclic ring, containing at least one substituent selected from R.sup.4, R.sup.5, and R.sup.6. R.sup.3 is H, (CH.sub.2) .sub.m X or CH.sub.2 O(CH.sub.2).sup.m X.sup.1. The polyamino acid and the group of formula II are linked via R.sup.4, R.sup.5, or R.sup.6, or optionally via a spacer of formula --�Q.sup.1 --(CH.sub.2).sub.p --Q.sup.2 --!.sub.r. A and B independently are O, S, NH, HN--CO, OC--NH, O--CO, OC--O, NH--CO--O, --O--CO--NH, S--CO, SC--O, O--CS--S, S--CS--OS, NH--CS--S, S--CS--NH, or CH.sub.2. Z is a pyranose, furanose, open-chain polyalcohol or Y--X.sup.6. Y is --O--(CX.sup.2,X.sup.3).sub.n, -(CX.sup.2,X.sup.3).sub.n, --CH.sub.2 --(CX.sup.2,X.sup.3).sub.n or a saturated or unsaturated six-membered carbo- or heterocyclic group having at least one substituent R.sup.9, or a combination of the chain --O--(CX.sup.2,X.sup.3).sub.n, or -(CX.sup.2,X.sup.3).sub.n, and the carbocyclic or heterocyclic group, in which R.sup.4, R.sup.5, and R.sup.6 independently are H, OH, --O--(CH.sub.2) .sub.q X.sup.4, --CH.sub.2 O(CH.sub.2) .sub.q X.sup.5, or HNC(O)CH.sub.3, and X, X.sup.1, X.sup.2, and X.sup.3 independently are H, NH.sub.2, COOH, OH, CH.sub.2 OH, CH.sub.2 NH.sub.2, C.sub.1 -C.sub.20 -alkyl, or C.sub.6 -C.sub.10 -aryl, X.sup.4 and X.sup.5 independently are --NH-- or --O--, and X.sup.6 is OH or --C(R.sup.3) (COOH).sub.2. m, n, and q independently can be 1-20. In the linker, Q.sup.1 is CH.sub.2 or --CO--, Q.sup.2 is --NH-- or --CO--NH--, p is 1-6, and r is 0 or 1. Methods of preparing the compounds, and their use as medicaments or diagnostic agents also are disclosed. ##STR1##

    摘要翻译: PCT No.PCT / EP95 / 00844 Sec。 371日期:1996年9月11日 102(e)1996年9月11日PCT PCT 1995年3月7日PCT公布。 公开号WO95 / 24437 日期1995年9月14日描述了具有防粘性的聚合物多价丙二酸衍生物。 化合物包含与式(I)的基团连接的聚氨基酸。 在式(I)中,R 1和R 2一起形成含有至少一个选自R4,R5和R6的取代基的六元碳环或杂环。 R3是H,(CH2)mX或CH2O(CH2)mX1。 聚氨基酸和式II基团通过R4,R5或R6连接,或任选地经由式[Q1-(CH2)p-Q2-] r的间隔基连接。 A和B分别是O,S,NH,HN-CO,OC-NH,O-CO,OC-O,NH-CO-O,-O-CO-NH,S-CO,SC-O, CS-S,S-CS-OS,NH-CS-S,S-CS-NH或CH 2。 Z是吡喃糖,呋喃糖,开链多元醇或Y-X6。 Y是-O-(CX2,X3)n, - (CX2,X3)n,-CH2-(CX2,X3)n或具有至少一个取代基R9的饱和或不饱和六元碳 - 或杂环基,或 链-O-(CX2,X3)n或 - (CX2,X3)n和碳环或杂环基团的组合,其中R4,R5和R6独立地为H,OH,-O-(CH2 )qX4,-CH2O(CH2)qX5或HNC(O)CH3,X,X1,X2和X3独立地为H,NH2,COOH,OH,CH2OH,CH2NH2,C1-C20-烷基或C6-C10 芳基,X 4和X 5独立地是-NH-或-O-,X 6是OH或-C(R 3)(COOH)2。 m,n和q独立地可以是1-20。 在接头中,Q1是CH2或-CO-,Q2是-NH-或-CO-NH-,p是1-6,r是0或1.制备化合物的方法及其用作药物或诊断 代理商也被披露。

    Titanium-containing catalyst and process for the production of polyester
    37.
    发明授权
    Titanium-containing catalyst and process for the production of polyester 失效
    含钛催化剂和生产聚酯的方法

    公开(公告)号:US5656716A

    公开(公告)日:1997-08-12

    申请号:US617562

    申请日:1996-03-19

    IPC分类号: C08G63/85 C08G64/00

    CPC分类号: C08G63/85

    摘要: The present invention comprises a new catalyst for the production of polyesters consisting essentially of a finely dispersed, large surface area titanium compound selected from hydrated TiO.sub.2 obtained by hydrolysis and having the composition yTiO.sub.2.zH.sub.2 O and from titanates having the composition (Me.sub.n O).sub.x.(TiO.sub.2).sub.y.(H.sub.2 O).sub.z, wherein Me is an alkaline earth metal or alkali metal. In addition, the present method comprises a process for the production of polyesters using this catalyst as an esterification or transesterification catalyst and as a polycondensation catalyst, whereby a phosphorous-oxygen-compound is added immediately before, during, or after the polycondensation.

    摘要翻译: 本发明包括用于生产聚酯的新催化剂,其基本上由细分散的大表面积钛化合物组成,所述钛化合物选自通过水解获得的并且具有组成yTiO 2·zH 2 O的水合TiO 2和具有组成(MenO)x。( TiO 2)y。(H 2 O)z,其中Me是碱土金属或碱金属。 此外,本方法包括使用该催化剂作为酯化或酯交换催化剂和缩聚催化剂生产聚酯的方法,由此在缩聚之前,之中或之后加入磷 - 氧化合物。

    Process for the production of light-colored .alpha.-sulfofatty acid
alkyl ester alkali metal salt pastes
    38.
    发明授权
    Process for the production of light-colored .alpha.-sulfofatty acid alkyl ester alkali metal salt pastes 失效
    制备浅色α-磺基脂肪酸烷基酯碱金属盐浆料的方法

    公开(公告)号:US5384422A

    公开(公告)日:1995-01-24

    申请号:US952714

    申请日:1992-11-25

    CPC分类号: C07C303/32 C07C303/22

    摘要: In the production of .alpha.-sulfofatty acid alkyl ester alkali metal salt pastes by reaction of fatty acid alkyl esters with gaseous SO.sub.3, subsequent after-reaction in liquid phase and neutralization with aqueous alkali metal hydroxide solutions, the crude sulfonation product is fed to an at least two-stage cascade of stirred tanks equipped with heating and cooling systems in which it is subjected with mechanical agitation to a temperature-controlled after-reaction until a degree of sulfonation of at least 90% is reached, after which the aged sulfonation product is further processed in known manner to .alpha.-sulfofatty acid alkyl ester alkali metal salt pastes.

    摘要翻译: PCT No.PCT / EP91 / 00951 Sec。 371日期:1992年11月25日 102(e)日期1992年11月25日PCT 1991年5月21日PCT PCT。 公开号WO91 / 18874 1991年12月12日。在通过脂肪酸烷基酯与气态SO 3反应制备α-磺基脂肪酸烷基酯碱金属盐浆料中,随后在液相中进行后反应并用碱金属氢氧化物水溶液中和, 将磺化产物加入到装有加热和冷却系统的搅拌釜的至少两级级联中,其中将其经机械搅拌进行温度控制的后反应直到达到至少90%的磺化程度, 之后将老化的磺化产物以已知方式进一步加工成α-磺基脂肪酸烷基酯碱金属盐浆料。

    Administration and dosage form for drug active agents, reagents or the
like and process for the preparation thereof
    40.
    发明授权
    Administration and dosage form for drug active agents, reagents or the like and process for the preparation thereof 失效
    用于药物活性剂,试剂等的给药和剂型及其制备方法

    公开(公告)号:US4925670A

    公开(公告)日:1990-05-15

    申请号:US344519

    申请日:1989-04-24

    申请人: Wolfgang Schmidt

    发明人: Wolfgang Schmidt

    IPC分类号: A61K9/20 A61K9/70

    CPC分类号: A61K9/70 A61K9/2086

    摘要: A novel dosage form for drug active agents, reagents or other active agents comprising a film-like carrier material having an active agent-containing coating one side thereof and wherein the carrier material is in the form of a release paper, film or foil, and the active agent-containing coating is removed in a dosewise manner from the carrier material after subdivision into dosage units. The removed active agent-containing portions are suitable as oral drugs, pharmaceuticals, reagents or foodstuff.

    摘要翻译: 用于药物活性剂,试剂或其它活性剂的新型剂型,其包含具有其一侧含活性剂的涂层的膜状载体材料,并且其中所述载体材料为剥离纸,膜或箔的形式,以及 在分解成剂量单位之后,以载体材料的方式从剂量方式除去含活性剂的涂层。 去除的含活性剂的部分适合作为口服药物,药物,试剂或食品。