CAS: 131986-45-3; 3-(Hexyloxy)-4-(1-Methyl-1,2,5,6-Tetrahydropyridin-3-yl)-1,2,5-Thiadiazole

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CAS号131988-19-7 3-(4-HEXYLOXY-1... | CAS号111-27-3 正己醇

3-(3-Pentyloxy-1,2,5-Thiadiazol-4-yl)-1-Methylpyridinium Iodide置于甲醇,Sodium Tetrahydroborate体系中,用75%的收率获得占诺美林
参考文献:Tacrine-Xanomeline And Tacrine-Iperoxo Hybrid Ligands: Synthesis And Biological Evaluation At Acetylcholinesterase And M1 Muscarinic Acetylcholine Receptors
标题:Tacrine-Xanomeline And Tacrine-Iperoxo Hybrid Ligands: Synthesis And Biological Evaluation At Acetylcholinesterase And M1 Muscarinic Acetylcholine Receptors
摘要:We Synthesized A Set Of New Hybrid Derivatives (7-C8,7-C10,7-C12 And 8-C8,8-C10,8-C12),In Which A Polymethylene Spacer Chain Of Variable Length Connected The Pharmacophoric Moiety Of Xanomeline,An M-1/m-4 Preferring Orthosteric Muscarinic Agonist,With That Of Tacrine,A Well-Known Acetylcholinesterase (Ache) Inhibitor Able To Allosterically Modulate Muscarinic Acetylcholine Receptors (Machrs). When Tested In Vitro In A Colorimetric Assay For Their Ability To Inhibit Ache,The New Compounds Showed Higher Or Similar Potency Compared To That Of Tacrine. Docking Analyses Were Performed On The Most Potent Inhibitors In The Series (8-C8,8-C10,8-C12) To Rationalize Their Experimental Inhibitory Power Against Ache. Next,We Evaluated The Signaling Cascade At M-1 Machrs By Exploring The Interaction Of G Alpha(Q)-Plc-Beta 3 Proteins Through Split Luciferase Assays And The Myo-Inositol 1 Phosphate (Ip1) Accumulation In Cells. The Results Were Compared With Those Obtained On The Known Derivatives 6-C7 And 6-C10,Two Quite Potent Ache Inhibitors In Which Tacrine Is Linked To Iperoxo,An Exceptionally Potent Muscarinic Orthosteric Activator. Interestingly,We Found That 6-C7 And 6-C10 Behaved As Partial Agonists Of The M-1 Machr,At Variance With Hybrids 7-Cn And 8-Cn Containing Xanomeline As The Orthosteric Molecular Fragment,Which Were All Unable To Activate The Receptor Subtype Response.
Doi:10.1016/j.Bioorg.2020.103633

专利信息

专利号:US-7576211-B2
优先权日:2004-09-30
标题 :Synthesis of thienopyridinone compounds and related intermediates
发明人：DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; CHEN DONGLI; MARANTZ YAEL; SHACHAM SHARON; HEIFETZ ALEXANDER; INBAL BOAZ; BAR-HAIM SHAY; MOHANTY PRADYUMNA; LOBERA MERCEDES; WU LAURENCE
权利人:EPIX DELAWARE INC
摘要:The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

专利号:US-8697888-B2
优先权日:2012-01-06
标题 :Substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs as antagonists of muscarinic acetylcholine M1 receptors
发明人：LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; MELANCON BRUCE J; CHEUNG YIU-YIN
权利人:UNIV VANDERBILT
摘要:In one aspect, the invention relates to substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs, derivatives thereof, and related compounds, which are useful as antagonists of the muscarinic acetylcholine receptor M 1 (mAChR M 1 ); 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.

专利号:US-9056875-B2
优先权日:2012-08-31
标 题 :Substituted pyrazolo[3′,4′:4,5]thieno[2,3-C]pyridazin-3-amine analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M4
发明人：LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; SALOVICH JAMES M
权利人:UNIV VANDERBILT
摘要: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 4 (mAChR M 4 ); 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.

专利号:US-9073935-B2
优先权日:2011-11-11
标 题:Substituted benzylspiroindolin-2-one analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M1
发明人：LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; HOPKINS COREY R; MELANCON BRUCE J; POSLUSNEY MICHAEL S
权利人:UNIV VANDERBILT
摘要:In one aspect, the invention relates to substituted benzylspiroindolin-2-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 1 (mAChR M 1 ); 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.

专利号:US-2006205714-A1
优先权日:2004-04-01
标 题 :Method of synthesis and isolation of solid N-desmethylclozapine and crystalline forms thereof
发明人：TOLF BO-RAGNAR; THYGESEN MIKKEL B; BLATTER FRITZ; BERGHAUSEN JORG
权利人:TOLF BO-RAGNAR; THYGESEN MIKKEL B; BLATTER FRITZ; BERGHAUSEN JORG
摘要:Disclosed herein are crystalline Forms A, B, C, D, and E of N-desmethylclozapine, methods of preparing the same, pharmaceutical compositions comprising the same, and methods of therapeutic treatment involving N-desmethylclozapine polymorphic forms.

专利号:US-2006084805-A1
优先权日:2004-09-30
标题:Synthesis of thienopyridinone compounds and related intermediates