专利号:US-8350031-B2 优先权日:2008-06-02 标 题:Processes for the synthesis of levocetirizine and intermediates for use therein 发明人:RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI; CHIKHALIKAR SANDIP VASANT 权利人:CIPLA LTD; RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI; CHIKHALIKAR SANDIP VASANT 摘要:The present invention provides a compound of formula (IV) n nwherein R is Cl, Br, NO 2 , OH or OR′, and R′ is alkyl, and its use in the synthesis of levocetirizine, including its use in the synthesis of (−)-1-[(4-chlorophenyl)-phenylmethyl]piperazine, an intermediate useful in the synthesis of levocetirizine. The present invention also provides compounds (II) and (III) which are useful in the synthesis of compound (IV).
专利号:US-12221452-B2 优先权日:2017-10-04 标题:Synthesis of cantharidin 发明人:DAVIDSON MATTHEW GENE; EKLOV BRIAN MATTHEW; WUTS PETER; LOERTSCHER BRAD MELVIN; SCHOW STEVEN R 权利人:VERRICA PHARMACEUTICALS INC 摘要:The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).
专利号:US-2014275582-A1 优先权日:2013-03-14 标 题 :Chiral 2-arylpropyl-2-sulfinamide and chiral n-2-arylpropyl-2-sulfinylimines and synthesis thereof 发明人:LI GUIGEN 权利人:LI GUIGEN; UNIV TEXAS TECH; NANJING UNIVERSITY INST OF CHEMISTRY AND BIOMEDICAL SCIENCES 摘要:Provided herein are novel chiral sulfinamide and imine compounds. Also provided herein are methods of synthesizing novel chiral sulfinamide and imine compounds comprising simplified purification methods when compared to prior methods. The novel chiral sulfinamide and imine compounds are useful, for example, in the synthesis of complex natural products and pharmaceutical important compounds.
专利号:US-9216953-B2 优先权日:2012-11-02 标题 :Chiral 2-arylpropyl-2-sulfinamide and chiral N-2-arylpropyl-2-sulfinylimines and synthesis thereof 发明人:LI GUIGEN; PINDI SURESH 权利人:LI GUIGEN; PINDI SURESH 摘要:Provided herein are novel chiral sulfinamide and imine compounds. Also provided herein are methods of synthesizing novel chiral sulfinamide and imine compounds comprising simplified purification methods when compared to prior methods. The novel chiral sulfinamide and imine compounds are useful, for example, in the synthesis of complex natural products and pharmaceutical important compounds.
专利号:US-2024109911-A1 优先权日:2017-10-04 标 题 :Synthesis of cantharidin
专利号:US-10391166-B2 优先权日:2013-02-18 标 题:Short oligonucleotides as vaccine adjuvants and therapeutic agents 发明人:IYER RADHAKRISHNAN P 权利人:SPRING BANK PHARMACEUTICALS INC; SPRING BREAK PHARMACEUTICALS INC 摘要:The invention provides a method of treating a microbial infection in a subject and a method of improving an immune system response in a subject against a disease, condition, infection, or virus thereof, by administering an effective amount of a nucleoside, short oligonucleotide compound or an analog thereof, or a pharmaceutically acceptable salt, racemate, enantiomer, diastereomer, geometric isomer, or tautomer thereof. In addition, the invention provides methods for treating or preventing a viral infection, bacterial infection, parasitic infection, or fungal infection in a subject (such as, a human). The compounds of the invention include, for example, di-, and trinucleotide compounds as provided herein. The compounds of the invention are useful for different therapeutic applications including, such as, prophylactics and therapeutics. The invention also provides design and synthesis of a compound that is useful for various therapeutic applications as mentioned herein.
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