Rapid access to 1-benzyl 2-substituted piperazines: Application to the synthesis of 1-benzyl-2-difluoromethyl-piperazine
A rapid and efficient synthesis of 1-benzyl-2-difluoromethyl-piperazine is herein described. The new pathway has the advantage of avoiding orthogonal protection at the two piperazine nitrogen atoms; therefore it is suitable for access to several 1-benzyl
Disclosed are quinoline derivatives as hedgehog pathway inhibitors, especially as SMO inhibitors. Compounds of the present invention can be used in treating diseases relating to hedgehog pathway including cancer.
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Paragraph 0110; 0112
(2017/02/28)
Composition Comprising An NK-1 Receptor Antagonist And An SSRI For The Treatment Of Tinnitus And Hearing Loss
The present invention relates to methods for treating a subject suffering from tinnitus, hearing loss, or tinnitus and hearing loss comprising administering to the subject an effective amount of an NK1 receptor antagonist alone, or in combination with an
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(2010/12/29)
Design, synthesis, and biological activity of non-basic compounds as factor Xa inhibitors: SAR study of S1 and aryl binding sites
Compound 7 was identified as the active metabolite of 6 by HPLC and mass spectral analysis. Modification of lead compound 7 by transformation of its N-oxide 6-6 biaryl ring system and fused aromatics produced a series of non-basic fXa inhibitors with excellent potency in anti-fXa and anticoagulant assays. The optimized compounds 73b and 75b showed sub to one digit micromolar anticoagulant activity (PTCT2). Particularly, anti-fXa activity was detected in plasma of rats orally administered with 1 mg/kg of compound 75b.
Novel aminoglycoside derivatives and their salts containing 2-deoxystreptamine moiety, of which the 1-amino group is acylated by a group represented by the formula: STR1 (wherein R is 4 to 6 membered heterocyclic group containing 1 to 2 nitrogen atoms whi
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(2008/06/13)
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