Abstract:
Charged compounds are provided that comprise one or more regions of localized positive charge, compositions comprising such compounds, methods of synthesizing such compounds, methods of screening such compounds to identify those having anti-infective activity, and methods of using such compounds to prevent or inhibit infections. These compounds, and compositions containing them, have multiple applications, including use in human and animal medicine and in agriculture.
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:
The present invention relates to cyclic terpyridine-lanthanide complexes having 8 nitrogen atoms and 10 carbon atoms in the macrocycle and containing a functional group in the terpyridine moiety. The invention also relates to a process for the preparation of cyclic terpyridine-lanthanide complexes through the condensation of terpyridine hydrazines with pyridine-2,6-dialdehydes or -ketones. The compounds can be complexed with oligonculeotides and are useful in the sequence-specific cleavage of RNA.
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:
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:
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:
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:
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:
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:
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.