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    • 10. 发明申请
    • Pancreatic lipase inhibitor compounds, their synthesis and use
    • US20030195199A1
    • 2003-10-16
    • US10326302
    • 2002-12-20
    • David WitterArlindo Castelhano
    • A61K031/542A61K031/538C07D513/02C07D498/02
    • C07D513/04A61K31/5365A61K31/542C07D333/38C07D409/12C07D498/02C07D513/02
    • The subject invention features compounds having the structure: 1 wherein X is O, S, CH2 or NR5; Y is O or S; R1 is H, substituted or unsubstituted C1-C15 alkyl, C1-C8 alkylaryl, nullC(O)OR4, nullC(O)NR4R5, nullCR6R6nullOR4, nullCR6R6nullOC(O)R4, nullCR6R6nullOC(O)NHR7, nullC(O)NR10R11, nullC(O)NR8R9 NR8R9, nullN(R5)C(O)NHR5, or CH2R4; R2 is a substituted or unsubstituted, straight chain C1nullC30 alkyl or branched C3-C30 alkyl, aryl, alkylaryl, arylalkyl, heteroarylalkyl or cycloalkyl; R3 is H or substituted or unsubstituted C1-C6 alkyl or C3-C10 cycloalkyl; R4 is H or a substituted or unsubstituted, straight chain or branched, C6-C30 alkyl, aryl, nullCH2-aryl, aryl nullC1-C15 alkyl, heteroaryl-C1-C15alkyl or C3-C10 cycloalkyl; R5 is H or a substituted or unsubstituted, straight chain or branched, C6-C30 alkyl, aryl C1-C30alkyl, heteroarylalkyl or cycloalkyl; R6 and R6null are each independently H, substituted or unsubstituted C1-C6 alkyl, dialkyl or C3-C10 cycloalkyl or together form a 3-7 membered ring system; R7 is H or substituted or unsubstituted C1-C12 alkyl or C3-C10 cycloalkyl; R8 and R9 are each independently H, substituted or unsubstituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylaryl, or NR8R9 together form a substituted piperazine or piperidine ring or a dihydro-1H-isoquinoline ring system, or a specific enantiomer thereof, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating diabetes or obesity by administering a therapeutically effective amount of the compounds of the invention.