- Cyclopentane-based human NK1 antagonists. Part 1: Discovery and initial SAR
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An initial investigation of the novel cyclopentane scaffold 6 afforded low nanomolar human NK1 antagonists having enhanced water solubility properties compared to morpholine 1. A synthesis of this cyclopentane scaffold, having three contiguous chiral cent
- Finke, Paul E.,Meurer, Laura C.,Levorse, Dorothy A.,Mills, Sander G.,MacCoss, Malcolm,Sadowski, Sharon,Cascieri, Margaret A.,Tsao, Kwei-Lan,Chicchi, Gary G.,Metzger, Joseph M.,MacIntyre, D. Euan
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p. 4497 - 4503
(2007/10/03)
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- Zwitterionic tachykinin receptor antagonists
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The present invention is directed to certain novel compounds represented by structural formula I: or a pharmaceutically acceptable salt thereof, wherein R3, R5, R6, R7, R8, R11, R12 R13, Q, W, X, Y and Z are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of psychiatric disorders including depression and anxiety.
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- Phenyl spiroethercycloalkyl tachykinin receptor antagonists
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The present invention is directed to certain novel compounds represented by structural formula I: STR1 or a pharmaceutically acceptable salt thereof, wherein R 3, R 6, R 7, R 8, R 11, R 12, R 13, m, n and the dashed lines are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis.
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- Heteroaryl spiroethercycloalkyl tachykinin receptor antagonists
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The present invention is directed to certain novel compounds represented by structural formula I: STR1 or a pharmaceutically acceptable salt thereof, wherein R 3, R 6, R 7, R 8, R 11, R 12, R 13, A, m, n and the dashed lines are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis.
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