220022-94-6Relevant articles and documents
A CONJUGATE OF A TUBULYSIN ANALOG WITH BRANCHED LINKERS
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Paragraph 000253; 000254, (2021/03/02)
The present invention relates to the conjugation of a tubulysin analog compound to a cell-binding molecule with branched/side-chain linkers for having better delivery of the conjugate compound and targeted treatment of abnormal cells. It also relates to a branched-linkage method of conjugation of a tubulysin analog molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and autoimmune disease.
New active series of growth hormone secretagogues
Guerlavais, Vincent,Boeglin, Damien,Mousseaux, Delphine,Oiry, Catherine,Heitz, Annie,Deghenghi, Romano,Locatelli, Vittorio,Torsello, Antonio,Ghé, Corrado,Catapano, Filomena,Muccioli, Giampiero,Galleyrand, Jean-Claude,Fehrentz, Jean-Alain,Martinez, Jean
, p. 1191 - 1203 (2007/10/03)
New growth hormone secretagogue (GHS) analogues were synthesized and evaluated for growth hormone releasing activity. This series derived from EP-51389 is based on a gem-diamino structure. Compounds that exhibited higher in vivo GH-releasing potency than hexarelin in rat (subcutaneous administration) were then tested per os in beagle dogs and for their binding affinity to human pituitary GHS receptors and to hGHS-R 1a. Compound 7 (JMV 1843, H-Aib-(D)-Trp-(D)-gTrp-formyl) showed high potency in these tests and was selected for clinical studies.