- NOVEL ROCK INHIBITORS
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The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceutic-als, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the ap-plication to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic dis-eases and Respiratory diseases. Compounds of the invention display soft drug characteristics, i.e. they are rapidly inactivated upon entry in the systemic circulation. Therefore, they allow for reduced systemic exposure to functionally active ROCK inhibitors
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(2014/05/24)
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- A potent, long-acting, orally active (2R)-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxy-2-phenylacetamide: A novel muscarinic M3 receptor antagonist with high selectivity for M3 over M2 receptors
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A novel series of (2R)-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxy-2-phenylacetamides was designed and synthesized based on the structure and biological profiles of an active metabolite 2 of our prototype muscarinic M3 receptor selective antagon
- Mitsuya,Kobayashi,Kawakami,Satoh,Ogino,Kakikawa,Ohtake,Kimura,Hirose,Sato,Numazawa,Hasegawa,Noguchi,Mase
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p. 5017 - 5029
(2007/10/03)
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