Novel 2-aminooctahydrocyclopentalene-3a-carboxamides as potent CCR2 antagonists |
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| Authors: | Chaozhong Cai Fu-An Kang Cuifen Hou John C O’Neill Evan Opas Sandra McKenney Dana Johnson Zhihua Sui |
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| Institution: | Janssen Research and Development, L.L.C. Welsh & McKean Roads, Spring House, Box 776, PA 19477, USA |
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| Abstract: | Novel CCR2 antagonists with a novel 2-aminooctahydrocyclopentalene-3a-carboxamide scaffold were designed. SAR studies led to a series of potent compounds. For example, compound 51 had a good PK profile in both dog and monkey, and exhibited excellent efficacy when dosed orally in an inflammation model in hCCR2 KI mice. In addition, an asymmetric synthesis to the core structures was developed. |
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