CAS: 74050-97-8; 4-(4-Chlorophenyl)-1-(4-(4-Fluorophenyl)-4-Oxobutyl)Piperidin-4-Yl Decanoate

上下游产品

1-decanoic acid haloperidol n-decanoyl chloride

📜正癸酸置于草酰氯,N,N-二异丙基乙胺体系中,用 二氯甲烷 作为反应溶剂,化学反应 24.0H,反应生成 4-(4-氯苯基)-1-[4-(4-氟苯基)-4-氧丁基]-4-哌啶癸酸盐
参考文献:Synthesis And Binding Profile Of Haloperidol-Based Bivalent Ligands Targeting Dopamine D2-Like Receptors
标题:Synthesis And Binding Profile Of Haloperidol-Based Bivalent Ligands Targeting Dopamine D2-Like Receptors
摘要:Homodimers Of Dopamine D2-Like Receptors Are Suggested To Be Of Particular Importance In The Pathophysiology Of Schizophrenia And,Thus,Serve As Promising Targets For The Discovery Of Atypical Antipsychotics. This Study Describes The Development Of A Series Of Novel Bivalent Molecules With A Pharmacophore Derived From The Dopamine Receptor Antagonist Haloperidol. These Dimers Were Investigated In Comparison To Their Monomeric Analogues For Their D2Long,D2Short,D3,And D4 Receptor Binding And The Ability To Bridge Two Neighboring Receptor Protomers. Radioligand Binding Studies Provided Diagnostic Insights When Hill Slopes Close To Two For The Bivalent Ligand 13 Incorporating 22 Spacer Atoms And A Comparative Analysis With Monovalent Control Ligands Indicated A Bivalent Binding Mode With A Simultaneous occupancy Of Two Neighboring Binding Sites.
DOI:10.1016/j.Bmcl.2014.06.079

专利信息

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

专利号:US-9012445-B2
优先权日:2012-01-12
标题 :Substituted 4-(1H-pyrazol-4-yl)benzyl analogues as positive allosteric modulators of mAChR M1 receptors
发明人：LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; MELANCON BRUCE J; POSLUSNEY MICHAEL S; TARR JAMES C
权利人:UNIV VANDERBILT
摘要:In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl 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-9637498-B2
优先权日:2013-08-23
标 题:Substituted thieno[2,3-C]pyridazine-6-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M4
发明人：LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; POSLUSNEY MICHAEL S; TARR JAMES C; MELANCON BRUCE J
权利人:UNIV VANDERBILT
摘要:In one aspect, the invention relates to substituted 5-aminothieno[2,3-c]pyridazine-6-carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4); 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-2004138238-A1
优先权日:2002-08-08
标题 :Substituted aminopyrimidine compounds as neurokinin antagonists
发明人：DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; KESAVAN VENKITASAMY; SHARADENDU ANURAG; MOHANTY PRADYUMNA; CHEN DONGLI; CHERUKU SRINIVASA RAO; HEIFETZ ALEXANDER; KALID ORI; MARANTZ YAEL; NUDELMAN RAPHAEL; SBACHAM SHARON; BAR-HAIM SHAY
摘要:The invention discloses tachykinin receptor antagonists. The tachykinin family of receptors comprising the neurokinins substance P (SP), neurokinin A, and neurokinin B and related neuropeptides that are widely distributed in the peripheral and central nervous system. The invention discloses novel aminopyrimidine derivatives, synthesis and uses thereof for the treatment of diseases mediated directly or indirectly by the tachykinin receptors. These diseases include central nervous system disorders such as anxiety, pain, depression, emesis, in particular cancer chemotherapy induced emesis, respiratory and inflammatory bowel disease and other gastric disorders, asthma, schizophrenia, ophthalmic diseases such as glaucoma, ocular hypotension, neural injury, stroke, cardiac disorders, psoriasis, and migraine. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

专利号:US-2008280886-A1
优先权日:2007-05-08
标题:Substituted ureas
发明人：GANT THOMAS G; SARSHAR SEPEHR
权利人:AUSPEX PHARMACEUTICALS INC
摘要:Disclosed herein are urea-based 5-HT receptor modulators, pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and medical use of such compounds for the treatment and/or management of 5-HT receptor-mediated disorders.