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Biphenylsulfonyl-thiophene-carboxamidine inhibitors of the complement component C1s
Authors:Travins Jeremy M  Ali Farah  Huang Hui  Ballentine Shelley K  Khalil Ehab  Hufnagel Heather R  Pan Wenxi  Gushue Joan  Leonard Kristi  Bone Roger F  Soll Richard M  DesJarlais Renee L  Crysler Carl S  Ninan Nisha  Kirkpatrick Jennifer  Cummings Maxwell D  Huebert Norman  Molloy Christopher J  Gaul Michael  Tomczuk Bruce E  Subasinghe Nalin L
Institution:Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 665 Stockton Drive, Exton, PA 19341, USA.
Abstract:Complement activation has been implicated in disease states such as hereditary angioedema, ischemia-reperfusion injury, acute respiratory distress syndrome, and acute transplant rejection. Even though the complement cascade provides several protein targets for potential therapeutic intervention only two complement inhibitors have been approved so far for clinical use including anti-C5 antibodies for the treatment of paroxysmal nocturnal hemoglobinuria and purified C1-esterase inhibitor replacement therapy for the control of hereditary angioedema flares. In the present study, optimization of potency and physicochemical properties of a series of thiophene amidine-based C1s inhibitors with potential utility as intravenous agents for the inhibition of the classical pathway of complement is described.
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