- SUBSTITUTED AZASPIRO DERIVATIVES
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Substituted azaspiro derivatives of the Formula:are provided, in which variables are as described herein. Such compounds may be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) and other disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).
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Page/Page column 35
(2008/12/08)
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- SPIROCYCLIC SULFONAMIDES AND RELATED COMPOUNDS
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Spirocyclic sulfonamides and related compounds of Formula 1 are provided : (Formula (I)): in which the variables are as described herein. Such compounds may be used to modulate bradykinin receptor activity in vivo or in vitro, and are particularly useful
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Page/Page column 55
(2010/11/29)
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- 2-CYANOPYRROLOPYRIMIDINES AND PHARMACEUTICAL USES THEREOF
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The invention relates to pyrrolo pyrimidines of formula (I), wherein Y represents -(CH2)t-O- or -(CH2)r-S-, p is 1 or 2, r is 1, 2 or 3, t is 1, 2 or 3, or Y is -(CH2)j- or -CH=CH-, j is 1 or 2; p is 1 or 2, or Y is -(CH2)f-, f is 1 or 2, p is 1, and the further radicals and symbols have the meaning as defined herein; their preparation, their use as pharmaceuticals, pharmaceutical compositions containing them, the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment of neuropathic pain and to a method for the treatment of such a disease in animals, especially in humans.
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Page/Page column 42
(2010/02/08)
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- Pyridyl-containing spirocyclic compounds as inhibitors of fibrinogen-dependent platelet aggregation
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Disclosed are certain substituted or unsubstituted pyridyl-containing spirocyclic compounds substituted with both basic and acidic functionality, which are useful in inhibiting platelet aggregation, inhibiting the binding of fibrinogen to blood platelets, and preventing or treating thrombosis
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- Spirocyclic nonpeptide glycoprotein IIb-IIIa antagonists. Part 3: Synthesis and SAR of potent and specific 2,8-diazaspiro[4.5]decanes
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The synthesis and biological activity of analogues containing spiro piperidinylpyridine and pyrrolidinylpyridine templates are described. The potent activity of these compounds as platelet aggregation inhibitors demonstrates the utility of the spiro structures as central template for nonpeptide RGD mimics.
- Mehrotra, Mukund M.,Heath, Julie A.,Rose, Jack W.,Smyth, Mark S.,Seroogy, Joseph,Volkots, Deborah L.,Ruhter, Gerd,Schotten, Theo,Alaimo, Lisa,Park, Gary,Pandey, Anjali,Scarborough, Robert M.
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p. 1103 - 1107
(2007/10/03)
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