Process for the preparation of carbacyclic nucleosides, and intermediates
    2.
    发明授权
    Process for the preparation of carbacyclic nucleosides, and intermediates 失效
    制备碳环核苷的方法和中间体

    公开(公告)号:US5332814A

    公开(公告)日:1994-07-26

    申请号:US969631

    申请日:1992-10-30

    Applicant: Heinz Moser

    Inventor: Heinz Moser

    Abstract: Process for the preparation of racemic compounds of the formula I ##STR1## or enantiomers thereof, in which B is the radical of a nucleic base from the series comprising purine, a purine analogue or a pyridine analogue, and R is H or a protective group R.sub.1, by reactinga) a compound of the formula II or enantiomer thereof ##STR2## with a compound of the formulae X--CO--X, X--CS--X, X--SO--X, X--SO.sub.2 --X, R.sub.2 --NCO, R.sub.3 R.sub.4 N--C(O)--R.sub.5, X.sub.2 P--R.sub.6 or X.sub.2 P(O)--R.sub.6, in which X is a leaving group, R.sub.2 is, for example, C.sub.1 -C.sub.18 alkyl, R.sub.3 and R.sub.4 are, for example, H or C.sub.1 -C.sub.18 alkyl, R.sub.5 is, for example, H or C.sub.1 -C.sub.12 alkyl, and R.sub.6 is, for example, C.sub.1 -C.sub.12 alkyl or C.sub.1 -C.sub.12 alkoxy, to give a compound of the formula III or enantiomers thereof ##STR3## in which Y is the groups --C(O)--, --C(S)--, --SO--, --SO.sub.2 --, R.sub.2 NH--CH.dbd., R.sub.3 R.sub.4 N--CR.sub.5 .dbd., R.sub.6 P.dbd. and R.sub.6 (O)P.dbd.;b) the further reaction of the compounds of the formulae III or enantiomers thereof with a nucleic base B on its own or together with a non-nucleophilic base, or with an alkali metal salt of the nucleic base B, to give compounds of the formula IV or enantiomers thereof ##STR4## in which M is H, an alkali metal or a non-nucleophilic base, and c) the conversion of the compounds of the formulae IV into the compounds of the formulae I by elimination of the protective group R.sub.1 and of the group YOM. The reactionb) is regioselective and diastereoselective, and the compounds of the formula I are obtained in high yields and purities.

    Abstract translation: 制备式I的外消旋化合物(I)或其对映体的方法,其中B是包含嘌呤,嘌呤类似物或吡啶类似物的系列的核酸基团,R是H或 保护基团R1,通过使a)式II化合物或其对映异构体(II)与式X-CO-X,X-CS-X,X-SO-X,X- SO2-X,R2-NCO,R3R4N-C(O)-R5,X2P-R6或X2P(O)-R6,其中X为离去基团,R2为例如C1-C18烷基,R3和R4为 例如H或C1-C18烷基,R5为例如H或C1-C12烷基,R6为例如C1-C12烷基或C1-C12烷氧基,得到式III化合物或其对映体

    Transfer station for foundry ladles
    4.
    发明授权
    Transfer station for foundry ladles 失效
    转运站为铸造水饺

    公开(公告)号:US5340092A

    公开(公告)日:1994-08-23

    申请号:US112388

    申请日:1993-08-27

    CPC classification number: B22D41/13 B22D41/12

    Abstract: A transfer station for transferring foundry ladles from a delivery station situated on the shop floor level to a higher pouting position of a curved continuous-casting installation, and includes a revolving turret with a foundation and supporting arms for receiving the foundry ladle. The arms are guided by paths and are arranged at a column which is rotatably supported on the foundation. A lifting device in the form of a hydraulic cylinder is provided for vertically moving the supporting arms. The lifting device is arranged below the plane of the rotating ring of the column only on the side of the take-over position regardless of the position of the column. The take-over position for the foundry ladle is likewise arranged below the plane of the rotating ting. The paths provided at the column extend below the plane of the rotating ring on the side of the delivery station and are severed in the plane of the rotating ting. A supporting member which can be moved out laterally and serves to support the supporting arms receiving the foundry ladle is arranged above the plane of the rotating ring at the column inside two paths guiding the supporting arms.

    Abstract translation: 一个转运站,用于将代工钢包从位于车间一级的配送站转移到弯曲的连续铸造设备的较高的踩踏位置,并且包括具有基座的旋转转台和用于接收铸造钢包的支撑臂。 臂由路径引导并且布置在可旋转地支撑在基座上的列上。 提供液压缸形式的提升装置用于垂直移动支撑臂。 提升装置仅在列的旋转环的平面下方布置在接收位置的一侧,而与柱的位置无关。 铸造钢包的接收位置同样布置在旋转平面下方。 设置在该列处的路径延伸到在输送站一侧的旋转环的平面之下,并且在转动平面中被切断。 可以横向移出并用于支撑接收铸造浇包的支撑臂的支撑构件设置在引导支撑臂的两个路径内的列处的旋转环的平面上方。

    Protected formylpentanediols, hydroxymethylpentanediols, process for
their preparation and intermediates
    5.
    发明授权
    Protected formylpentanediols, hydroxymethylpentanediols, process for their preparation and intermediates 失效
    受保护的甲酰戊二醇,羟甲基戊二醇,其制备方法和中间体

    公开(公告)号:US5274157A

    公开(公告)日:1993-12-28

    申请号:US969632

    申请日:1992-10-30

    Applicant: Heinz Moser

    Inventor: Heinz Moser

    Abstract: Compounds of the formula Ib ##STR1## in which R.sub.1 and R.sub.2 independently of one another are linear or branched C.sub.1 -C.sub.12 alkyl, cycloalkyl having 5 to 8 ring carbon atoms, phenylalkyl having 1 to 4 C atoms in the alkylene group, the cyclic radicals being unsubstituted or substituted by C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, or R.sub.1 and R.sub.2 independently of one another are --SiR.sub.4 R.sub.5 R.sub.6 in which R.sub.4, R.sub.5 and R.sub.6 independently of one another are C.sub.1 -C.sub.12 alkyl, phenyl, benzyl, or phenyl or benzyl, each of which is substituted by C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, and R.sub.3 is a bridging member which, together with the radical --OCH--CH.sub.2 --CHO-- to which it is bonded, forms a 6- to 8-membered ring. These compounds are valuable intermediates for the preparation of carbacyclic nucleosides of the natural and unnatural series and of the racemates.

    Abstract translation: 其中R 1和R 2彼此独立地为直链或支链C 1 -C 12烷基,具有5至8个环碳原子的环烷基,亚烷基中具有1至4个C原子的苯基烷基的式Ib化合物 未取代或被C1-C4烷基或C1-C4烷氧基或R1和R2彼此独立取代的环基是-SiR4R5R6,其中R4,R5和R6彼此独立地是C1-C12烷基,苯基,苄基或苯基或苄基 ,其各自被C 1 -C 4烷基或C 1 -C 4烷氧基取代,并且R 3是与其键合的基团-OCH-CH 2 -CH 2 - 一起形成6-至8-元环的桥连构件。 这些化合物是制备天然和非天然系列和外消旋体的碳环核苷的有价值的中间体。

    Bone substitute and a method of production thereof
    6.
    发明授权
    Bone substitute and a method of production thereof 失效
    骨代用品及其生产方法

    公开(公告)号:US4516276A

    公开(公告)日:1985-05-14

    申请号:US593174

    申请日:1984-03-26

    Abstract: A bone substitute comprised of collagen material in the form of fleece or a spatial meshwork having apatite, the mineral component of bone material, admixed therewith. The structure of the collagen material may be strengthened by carbohydrate or starch or may be applied, in the form of a coating, to a honeycomb-like basic structure made from a variety of materials.Such a bone substitute has a good support quality, promotes bone growth and also has a good styptic or haemostatic effect.

    Abstract translation: 由羊毛形式的胶原材料或具有磷灰石的空间网状物(骨材料的矿物成分)混合的骨替代物。 胶原材料的结构可以通过碳水化合物或淀粉加强,或者以涂层的形式施用到由各种材料制成的蜂窝状基本结构上。 这种骨替代物具有良好的支持质量,促进骨生长,并且具有良好的止血或止血作用。

    Slide prosthesis for the knee joint
    7.
    发明授权
    Slide prosthesis for the knee joint 失效
    滑动假体用于膝关节

    公开(公告)号:US4355429A

    公开(公告)日:1982-10-26

    申请号:US114335

    申请日:1980-01-23

    CPC classification number: A61F2/38 A61F2002/3895

    Abstract: A slide prosthesis for the knee joint is provided to be secured free of cement, the tibia members, the femur members and the surface replacement for the knee cap having anchoring pins which are provided with a saw tooth-like or bone screw-shaped profile. The tibia and knee cap members are preferably made of carbon fibre-reinforced plastics material and the femur members of aluminium oxide ceramic material. In order to assist growth of the bone to the prosthesis members, the members are coated at the corresponding points with bio-active particles, such as apatite-containing glasses, apatite particles or dealbumined bone material.

    Abstract translation: 提供了一种用于膝关节的滑动假体,其被固定而没有水泥,胫骨构件,股骨构件以及具有固定销的膝盖帽的表面替换物,其具有锯齿形或骨螺纹形状。 胫骨和膝盖构件优选地由碳纤维增强塑料材料和氧化铝陶瓷材料的股骨构件制成。 为了帮助骨对假体构件的生长,使用生物活性颗粒(例如含磷灰石的玻璃,磷灰石颗粒或经骨化的骨材料)在相对应的位置涂覆构件。

    Implant for the jaw
    8.
    发明授权
    Implant for the jaw 失效
    下颌植入

    公开(公告)号:US4324550A

    公开(公告)日:1982-04-13

    申请号:US209296

    申请日:1980-11-21

    CPC classification number: A61C8/0086 A61C8/0022 A61C8/005 A61C8/0069

    Abstract: An implant for the jaw includes an implant body, to be fixed without bone cement, a bed made of plastics material and an implant support for receiving the suprastructure. In order to reduce the specific load on the bone the implant body is provided with support ribs, which have the profile of a bone screw. The bed, providing a flexible layer between the implant body and support is frusto-conical towards its lower end and is spread by the implant support, when said support is screwed in.This construction provides for secure anchorage of the implant body into the bone as well as of the bed and the implant support into the implant body.

    Abstract translation: 用于钳口的植入物包括植入体,待固定而不含骨水泥,由塑料材料制成的床和用于接收超基面的植入物支架。 为了减少骨上的特定负荷,植入体具有支撑肋,支撑肋具有骨螺钉的轮廓。 当植入物主体和支撑件之间提供柔性层时,该床在其下端具有截头圆锥形,并且当所述支撑件被拧入时由植入物支撑件扩展。这种结构提供将植入体本体固定到骨骼中作为 以及床和种植体支撑体到植入体中。

    2'-Substituted nucleosides and oligonucleotide derivatives
    9.
    发明申请
    2'-Substituted nucleosides and oligonucleotide derivatives 审中-公开
    2'-取代的核苷和寡核苷酸衍生物

    公开(公告)号:US20050159374A1

    公开(公告)日:2005-07-21

    申请号:US10696488

    申请日:2003-10-29

    CPC classification number: C07H21/00

    Abstract: The invention relates to an oligonucleotide derivative which comprises at least one nucleoside building block of the formula (I) The invention furthermore relates to nucleoside building blocks, intermediates and processes for preparing the oligonucleotide derivatives and the nucleoside building blocks. The invention also relates to pharmaceutical compositions and to uses of the oligonucleotide derivatives and the nucleoside building blocks.

    Abstract translation: 本发明涉及包含至少一种式(I)核苷结构单元的寡核苷酸衍生物。本发明还涉及核苷结构单元,中间体和制备寡核苷酸衍生物和核苷结构单元的方法。 本发明还涉及药物组合物以及寡核苷酸衍生物和核苷结构单元的用途。

    Angularly adjustable offset spherical head endoprosthesis
    10.
    发明授权
    Angularly adjustable offset spherical head endoprosthesis 失效
    角度可调的偏心球头内置假体

    公开(公告)号:US5480451A

    公开(公告)日:1996-01-02

    申请号:US106152

    申请日:1993-08-12

    Abstract: A spherical head endoprosthesis has a spherical head and a base piece. Between the base piece and the spherical head is a conical interference fit connection, wherein the spherical head has a conical bore and the base piece has a conical pin. The axis of the conical bore and the center line of the spherical head form an angle in the range of 7.degree. to 15.degree.. The conical bore is decentralized in relation to the center line with an offset of 1 to 4 mm. On the inside of the bore are at least five grooves parallel to the axis of the bore, into which, after assembly of the conical interference fit connection, grips at least one locking projection provided on the peripheral surface of the conical pin. The grooves may be designated by markings around the periphery of the bore opening for easy identification of the proper groove for insertion of the locking projection during the replacement operation.

    Abstract translation: 球形头内假体具有球形头部和基部件。 在基部件和球形头之间是锥形过盈配合连接,其中球形头部具有锥形孔,并且基部件具有锥形销。 锥形孔的轴线和球头的中心线形成7°至15°的角度。 锥形孔相对于中心线分散,偏移为1至4毫米。 在孔的内侧是至少五个平行于孔的轴线的凹槽,在锥形过盈配合连接的组装之后,夹紧设置在锥形销的外周表面上的至少一个锁定突起。 凹槽可由围绕孔开口的周边的标记指定,以便于在更换操作期间识别用于插入锁定突起的适当凹槽。

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