CAS: 982-24-1; Clopenthixol

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      专利号:US-2012177593-A1
      优先权日:2009-07-20
      标 题 :Synthesis of dendrimer conjugates
      发明人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
      权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
      摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

      专利号:US-2012232225-A1
      优先权日:2009-08-26
      标 题:Synthesis and isolation of dendrimer systems
      发明人:BAKER JR JAMES R; BANASZAK HOLL MARK M; MULLEN DOUGLAS GURNETT; ORR BRADFORD G; DESAI ANKUR; SANDER LEONARD M; WADDELL JACK NEEL
      权利人:BAKER JR JAMES R; BANASZAK HOLL MARK M; MULLEN DOUGLAS GURNETT; ORR BRADFORD G; DESAI ANKUR; SANDER LEONARD M; WADDELL JACK NEEL; UNIV MICHIGAN
      摘要:The present invention relates to novel methods of synthesis and isolation of dendrimer systems. In particular, the present invention is directed to novel dendrimer conjugates with defined and limited numbers of ligand conjugates and high levels of structural uniformity, methods of synthesizing the same, compositions comprising the conjugates, as well systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, pain therapy, etc.)).

      专利号:US-2023271983-A1
      优先权日:2020-07-29
      标题 :Functionalized isonitriles and products, preparation and uses thereof
      发明人:SOTELO PÉREZ EDDY; AZUAJE GUERRERO JHONNY ALBERTO; MAJELLARO MARIA
      权利人:UNIV SANTIAGO COMPOSTELA
      摘要:The present invention relates to functionalized isonitrile compounds, formed by means of multicomponent environmentally friendly reactions, suitable for coupling to functional molecules such as biomolecules, APIs, chromophore and fluorophore molecules. The invention also relates to conjugates between said isonitrile compounds and functional molecules, which are useful in the synthesis of pharmaceutic drugs or tools, fluorescent molecules and labels, polymeric smart materials. The invention furthermore provides a kit for the in-vitro preparation of the functionalized isontrile compounds and conjugates. The invention also contemplates the medical use of said compounds and conjugates.

      专利号:US-9580409-B2
      优先权日:2011-11-07
      标 题:Modulators of opioid receptors and methods of use thereof
      发明人:MALCOLM SCOTT; BOWEN CARRIE; MELNICK LAURENCE; XIE LINGHONG
      权利人:SUNOVION PHARMACEUTICALS INC; SUNOVION PHARMACEUTICALS INC
      摘要:Provided herein are compounds and methods of synthesis thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as pain, neurological disorders, psychiatric disorders, and neuromuscular disorders. Compounds provided herein modulate the activity of opioid receptor (e.g., μ-opioid receptor) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.

      专利号:WO-2011011384-A2
      优先权日:2009-07-20
      标 题 :Synthesis of dendrimer conjugates

      专利号:WO-2025118034-A1
      优先权日:2023-12-06
      标题 :Compounds active at the serotonergic 5-ht2a receptor
      发明人:JORGENSON WILLIAM; TAN JINLONG; WHISH LACHLAN; BANISTER SAMUEL
      权利人:Psylo Pty Ltd
      摘要:The present disclosure relates to compounds of formula (I), their methods of synthesis, and their use in the treatment of mental illness or central nervous system disorders.

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      主要参考文献

      1. Comparative efficacy and tolerability of 32 oral antipsychotics for the acute treatment of adults with multi-episode schizophrenia: a systematic review and network meta-analysis. 2. The pharmacokinetics of long-acting antipsychotic medications. Spanarello S, La Ferla T. 3. Serum concentrations of cis(Z)- and trans(E)-clopenthixol after administration of cis(Z)-clopenthixol and clopenthixol to human volunteers. 4. Cis(Z)-clopenthixol and clopenthixol (Sordinol) in chronic psychotic patients. A double-blind clinical investigation. 5. Pharmacokinetic studies on clopenthixol decanoate; a comparison with clopenthixol in dogs and rats. 6. Zuclopenthixol dihydrochloride for schizophrenia. 7. Clopenthixol decanoate in schizophrenia. 8. Effect of trans(E)-clopenthixol on Plasmodium berghei in vivo. 9. Serum levels of the isomers of clopenthixol in patients given cis(Z)-clopenthixol or cis(Z)/trans(E)-clopenthixol. 10. A specific method for assay of drug levels in serum of patients treated with clopenthixol decanoate injections.

      合成参考文献


      摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664
      摘要:Litvintsev SV, Reznik AM, Arbuzov AL, Barkov DA. [Clopixol: new possibilities in therapy of mental disorders (a review of clinical studies)]. Voen Med Zh. 2002 Mar;323(3):42–7.
      摘要:Mannaioni G, Baronti R, Moroni F. Gastrointestinal bleeding and massive liver damage in neuroleptic malignant syndrome. Ther Clin Risk Manag. 2005 Sep;1(3):225–30.
      参考文献:10.1515/cclm.2003.240
      摘要:Gutteck U, Rentsch KM. Therapeutic drug monitoring of 13 antidepressant and five neuroleptic drugs in serum with liquid chromatography-electrospray ionization mass spectrometry. Clin Chem Lab Med. 2003 Dec;41(12):1571–9. doi: 10.1515/cclm.2003.240.
      摘要:Romain JL, Dermain P, Greslé P, Grignon S, Moisan P, Nore D, Pech G, Benyaya J, Perret I. [Efficacy of zuclopenthixol acetate on psychotic anxiety evaluated in an open study]. Encephale. 1996 Jul;22(4):280–6.
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