11-12-2014 дата публикации
Номер: US20140364409A1
In one aspect, the invention relates to substituted pyrazolo[3′,4′:4,5]thieno[2,3-c]pyridazine-3-amine analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M(mAChR M); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. 2. The compound of claim 1 , wherein each of Rand Ris independently selected from hydrogen claim 1 , C1-C8 alkyl claim 1 , C1-C8 monohaloalkyl claim 1 , C1-C8 polyhaloalkyl claim 1 , Cy claim 1 , Cy-(C1-C6 alkyl)- claim 1 , Ar claim 1 , and Ar—(C1-C6 alkyl)-;{'sup': 1', '1', '5', '5', '5', '5', '5', '5', '6', '2, 'sub': 2', '5', 'm', 'm, 'claim-text': wherein each m is an integer independently selected from 0, 1 and 2;', {'sup': 2', '2', '5, 'sub': 2', 'm, 'wherein each Ar, when present, is independently selected from phenyl and heteroaryl, and wherein each Aris independently substituted with 0, 1, 2, or 3 groups independently selected from halogen, —NH, —OH, —CN, C1-C8 alkyl, C1-C8 monohaloalkyl, C1-C8 polyhaloalkyl, C1-C8 alkoxy, C1-C8 alkylamino, C1-C8 dialkylamino, and —S(O)R;'}, {'sup': 5', '2', '2, 'wherein each R, when present, is independently selected from hydrogen, C1-C8 alkyl, C3-C8 cycloalkyl, C1-C8 monohaloalkyl, C1-C8 polyhaloalkyl, —(C1-C3)-Ar, and Ar; and'}, {'sup': '6', 'sub': '2', 'wherein each R, when present, is selected from C1-C4 alkyl, C1-C4 alkoxy, C1-C4 monoalkylamino, or C1-C4 dialkylamino substituted with 1 or 2 groups selected from fluoro, trifluoromethyl, methyl, —OH, —NH, and —CN;'}], 'wherein each Ar, when present, is independently selected from phenyl and heteroaryl, and ...
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