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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
    2.
    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

    申请人： Michael Palladino ,  Emmanuel A. Theodorakis

    发明人： Michael Palladino ,  Emmanuel A. Theodorakis

    IPC分类号： C07C69/74

    CPC分类号： 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

    摘要： 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.

    Novel interleukin-1 and tumor necrosis factor-alpha modulators, synthesis of said and their enantimoners and methods of using said modulators
    3.
    发明申请
    Novel interleukin-1 and tumor necrosis factor-alpha modulators, synthesis of said and their enantimoners and methods of using said modulators 失效
    新型白细胞介素-1和肿瘤坏死因子-α调节剂，所述及其配子的合成以及使用所述调节剂的方法

    公开(公告)号：US20030050338A1

    公开(公告)日：2003-03-13

    申请号：US10112681

    申请日：2002-03-27

    发明人： Michael Palladino ,  Emmanuel A. Theodorakis

    IPC分类号： A61K031/21 ,  A61K031/195 ,  A61K031/19 ,  A61K031/16 ,  A61K031/13 ,  A61K031/12

    CPC分类号： 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

    摘要： 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-null modulators, and thus are useful in the treatment of various diseases. 1 wherein the R groups are defined as follows: if any R3nullR5, R7, R8, R11nullR13 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 R3nullR5, R7, R8, R11nullR13 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. R3nullR5, R7, R8, and R11nullR13 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.

    摘要翻译： 公开了具有以下化学结构的新型化合物，以及可用作白细胞介素-1和肿瘤坏死因子-α调节剂的前药酯及其酸加成盐，因此可用于治疗各种疾病。 其中R基定义如下：如果任何R 3 -R 5，R 7，R 8，R 11 -R 13不是氢，则R 2或R 6或R 9不是甲基，或R 10不是CH 2，则R 1选自 氢，卤素，COOH，C1-C12羧酸，C1-C12酰基卤，C1-C12酰基残基，C1-C12酯，C1-C12仲酰胺，（C1-C12）（C1-C12）叔酰胺（ C1-C12）（C1-C12）环状酰胺，（C1-C12）胺，C1-C12醇，（C1-C12）（C1-C12）醚，C1-C12烷基，C1-C12取代烷基，C2-C12 烯基，C 2 -C 12取代的烯基和C 5 -C 12芳基。 如果所有的R 3 -R 5，R 7，R 8，R 11 -R 13均为氢，则R 2，R 6和R 9各自为甲基，R 10为CH 2，则R 1选自氢，卤素，C 1 -C 12羧酸，C 1 -C 12 酰基卤，C 1 -C 12酰基残基，C

    Novel Interleukin-1 and Tumor Necrosis Factor-Alpha Modulators, Syntheses of Said Modulators and Their Enantiomers and Methods of Using Said Modulators
    7.
    发明申请
    Novel Interleukin-1 and Tumor Necrosis Factor-Alpha Modulators, Syntheses of Said Modulators and Their Enantiomers and Methods of Using Said Modulators 审中-公开

    公开(公告)号：US20080103328A1

    公开(公告)日：2008-05-01

    申请号：US11926695

    申请日：2007-10-29

    申请人： Michael Palladino ,  Emmanuel Theodorakis

    发明人： Michael Palladino ,  Emmanuel Theodorakis

    IPC分类号： C07C61/135 ,  C07C69/75

    CPC分类号： 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

    摘要： 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 above 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.

    Interleukin-1 and tumor necrosis factor-α modulators, synthesis of said modulators and their enantiomers and methods of using said modulators
    8.
    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 有权

    公开(公告)号：US07288671B2

    公开(公告)日：2007-10-30

    申请号：US11417906

    申请日：2006-05-03

    申请人： Michael Palladino ,  Emmanuel A. Theodorakis

    发明人： Michael Palladino ,  Emmanuel A. Theodorakis

    IPC分类号： C07C61/29 ,  C07C69/74

    CPC分类号： 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

    摘要： 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.