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    Interleukin-1 and tumor necrosis factor-α modulators, synthesis of said modulators and their enantiomers and methods of using said modulators
    87.
    发明授权
    Interleukin-1 and tumor necrosis factor-α modulators, synthesis of said modulators and their enantiomers and methods of using said modulators 失效

    公开(公告)号：US07119223B2

    公开(公告)日：2006-10-10

    申请号：US10112681

    申请日：2002-03-27

    Applicant: Michael Palladino ,  Emmanuel A. Theodorakis

    Inventor： Michael Palladino ,  Emmanuel A. Theodorakis

    IPC: C07C69/74

    CPC classification number: C07C33/14 ,  A61K31/12 ,  A61K31/16 ,  A61K31/215 ,  C07B2200/05 ,  C07B2200/07 ,  C07C57/26 ,  C07C61/29 ,  C07C61/35 ,  C07C62/30 ,  C07C62/32 ,  C07C69/753 ,  C07C69/757 ,  C07C233/58 ,  C07C2603/26 ,  C07D295/15 ,  C07D295/185 ,  C07D295/26 ,  Y02A50/463

    Abstract: Novel compounds are disclosed that have the following chemical structures, and prodrug esters and acid-addition salts thereof, that are useful as Interleukin-1 and Tumor Necrosis Factor-α modulators, and thus are useful in the treatment of various diseases. wherein the R groups are defined as follows: if any R3–R5, R7, R8, R11–R13 is not hydrogen, R2 or R6 or R9 is not methyl, or R10 is not CH2, then R1 is selected from the group consisting of hydrogen, a halogen, COOH, C1–C12 carboxylic acids, C1–C12 acyl halides, C1–C12 acyl residues, C1–C12 esters, C1–C12 secondary amides, (C1–C12)(C1–C12) tertiary amides, (C1–C12)(C1–C12) cyclic amides, (C1–C12) amines, C1–C12 alcohols, (C1–C12)(C1–C12) ethers, C1–C12 alkyls, C1–C12 substituted alkyls, C2–C12 alkenyls, C2–C12 substituted alkenyls, and C5–C12 aryls. If all R3–R5, R7, R8, R11–R13 are hydrogen, R2, R6, and R9 are each methyl, and R10 is CH2, then R1 is selected from hydrogen, a halogen, C1–C12 carboxylic acids, C1–C12 acyl halides, C1–C12 acyl residues, C2–C12 esters, C2–C12 secondary amides, (C1–C12)(C1–C12) tertiary amides, C2–C12 alcohols, (C1–C12)(C1–C12) ethers other than methyl-acetyl ether, C2–C12 alkyls, C1–C12 substituted alkyls, C2–C12 alkenyls, C2–C12 substituted alkenyls, and C2–C12 aryls. R2 and R9 are each separately selected from hydrogen, a halogen, C1–C12 alkyl, C1–C12 substituted alkyls, C2–C12 alkenyl, C2–C12 substituted alkenyl, C2–C12 alkynyl, C1–C12 acyl, C1–C12 alcohol, and C5–C12 aryl. R3–R5, R7, R8, and R11–R13 are each separately selected from hydrogen, a halogen, C1–C12 alkyl, C1–C12 substituted alkyls, C2–C12 alkenyl, C2–C12 substituted alkenyl, C2–C12 alkynyl, and C5–C12 aryl. R6 is selected from hydrogen, a halogen, C1–C12 alkyl, C1–C12 substituted alkyls, C2–C12 alkenyl, C2–C12 substituted alkenyl, and C2–C12 alkynyl. R10 is selected from hydrogen, a halogen, CH2, C1–C6 alkyl, C1–C6 substituted alkyl, C2–C6 alkenyl, C2–C6 substituted alkenyl, C1–C12 alcohol, and C5–C12 aryl. Pharmaceutical compositions comprising, and uses of, therapeutically effective amounts of the aove compounds and their prodrug esters, and a pharmaceutically acceptable carrier, are also disclosed, and are useful as, for example, anti-inflammatory analgesics, in treating immune disorders, as anti-cancer and anti-tumor agents, and in the treatment of cardiovascular disease, skin redness, and viral infection. Completely synthetic and semi-synthetic methods of making these compounds and their analogs, are also disclosed.

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