摘要:
The present invention relates to the design of trimeric polypeptides using polypeptide structural elements derived from the tetranectin protein family, and their use in rational de novo design and production of multi-functional molecules including the application of the multi-functional molecules in protein library technology, such as phage display technology, diagnostic and therapeutic systems, such as human gene therapy and imaging. The trimeric polypeptides being constructed as a monomer polypeptide construct comprising at least one tetranectin trimerising structural element (TTSE) which is covalently linked to at least one heterologous moiety, said TTSE being capable of forming a stable complex with two other TTSEs; or as an oligomer which is comprised of two monomer polypeptide constructs as mentioned above, and which comprises three TTSEs or a multiplum of three TTSEs, or which is comprised of three monomer polypeptide constructs.
摘要:
The invention is directed to a method in the treatment of hypercalcitriolemic disease states which comprises administering an effective amount of 25S,26-dihydroxycholecalciferol to a host in need of such treatment.
摘要:
The present invention relates to novel p75 heterodimer specific anti-human IL-12 antibodies that are characterized by a higher potency and greater efficacy in neutralizing human IL-12 bioactivity than known heterodimer specific IL-12 monoclonal antibodies. The heterodimer specific antibodies recognize one or more epitopes of the human IL-12 p75 heterodimer, but do not bind to the p40 subunit alone. The heterodimer specific IL-12 antibodies neutralize rhesus monkey IL-12 bioactivity with a potency similar to their potency for neutralizing human IL-12 bioactivity making them useful IL-12 antagonists for in vivo studies in the rhesus monkey.
摘要:
The present invention relates to the use of pyrrolidine and piperidine derivatives of the general formula ##STR1## wherein R.sup.1 and R.sup.2 are, independently from each other, hydrogen, lower alkoxy, hydroxy, halogen, --CONH.sub.2 or --C(O)O-lower alkyl; or taken together are --O--CH.sub.2 O;R.sup.3 and R.sup.4 are, independently from each other, hydrogen, lower alkoxy, benzyloxy, halogen, hydroxy, --CONH.sub.2 or --SCH3; or taken together are --O--CH.sub.2 --O--;R.sup.5 is hydrogen or lower alkyl;X and Y are, independently from each other --CH(OH)--, --(CH.sub.2).sub.n --, --C(O)-- or --CH(lower alkoxy)-; andin, n and p are 1 or 2;and to their pharmaceutically acceptable addition salts for the treatment of diseases caused by over activation of NMDA receptor subtypes.
摘要:
Ethylenediamine monoamides of the formulaR--CO--NH--CH.sub.2 --CH.sub.2 --NH.sub.2 Iwherein R is one of groups ##STR1## in which R.sup.1 is phenyl, monohalophenyl, monolower-alkylphenyl, monolower-alkoxyphenyl, monotrifluoromethylphenyl, monocyanophenyl or monaryl-lower-alkoxyphenyl, dihalophenyl, furyl, thienyl or monohalothienyl, R.sup.2 is hydrogen, halogen or amino, R.sup.3, R.sup.5 and R.sup.7 each are phenyl, monohalophenyl, dihalophenyl, thienyl, furyl or monohalofuryl, R.sup.4 and R.sup.6 each are hydrogen or amino and R.sup.8 is hydrogen or lower-alkyl,as well as their pharmaceutically usable acid addition salts are disclosed. The compounds have monoamine oxidase inhibiting properties with low toxicity and are useful for the treatment of depressive states and cognitive disorders.
摘要:
The present invention relates to novel p75 heterodimer specific anti-human IL-12 antibodies that are characterized by a higher potency and greater efficacy in neutralizing human IL-12 bioactivity than known heterodimer specific IL-12 monoclonal antibodies. The heterodimer specific antibodies recognize one or more epitopes of the human IL-12 p75 heterodimer, but do not bind to the p40 subunit alone. The heterodimer specific IL-12 antibodies neutralize rhesus monkey IL-12 bioactivity with a potency similar to their potency for neutralizing human IL-12 bioactivity making them useful IL-12 antagonists for in vivo studies in the rhesus monkey.
摘要:
The present invention relates to novel p75 heterodimer specific anti-human IL-12 antibodies that are characterized by a higher potency and greater efficacy in neutralizing human IL-12 bioactivity than known heterodimer specific IL-12 monoclonal antibodies. The heterodimer specific antibodies recognize one or more epitopes of the human IL-12 p75 heterodimer, but do not bind to the p40 subunit alone. The heterodimer specific IL-12 antibodies neutralize rhesus monkey IL-12 bioactivity with a potency similar to their potency for neutralizing human IL-12 bioactivity making them useful IL-12 antagonists for in vivo studies in the rhesus monkey.
摘要:
The present invention relates to the design of trimeric polypeptides using polypeptide structural elements derived from the tetranectin protein family, and their use in rational de novo design and production of multi-functional molecules including the application of the multi-functional molecules in protein library technology, such as phage display technology, diagnostic and therapeutic systems, such as human gene therapy and imaging. The trimeric polypeptides being constructed as a monomer polypeptide construct comprising at least one tetranectin trimerising structural element (TTSE) which is covalently linked to at least one heterologous moiety, said TTSE being capable of forming a stable complex with two other TTSEs; or as an oligomer which is comprised of two monomer polypeptide constructs as mentioned above, and which comprises three TTSEs or a multiplum of three TTSEs, or which is comprised of three monomer polypeptide constructs.
摘要:
The compounds of the formula ##STR1## wherein A, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as set forth above, are described.The compounds of formula I have an inhibitory activity on the natural enzyme renin and can accordingly be used in the form of pharmaceutical preparations for the control or prevention of high blood pressure and cardiac insufficiency.