CAS: 119290-87-8; 1-Phenanthrenecarboxylicacid, 7-Ethenyl-1,2,3,4,4A,6,7,8,8A,9,10,10A-Dodecahydro-1,4A,7-Trimethyl-,(1R,4Ar,7S,8As,10As)-

专利信息

专利号:US-7288671-B2
优先权日:1999-05-14
标题:Interleukin-1 and tumor necrosis factor-α modulators, synthesis of said modulators and their enantiomers and methods of using said modulators
发明人：PALLADINO MICHAEL; THEODORAKIS EMMANUEL A
权利人:UNIV CALIFORNIA
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. n nwherein the R groups are defined as follows: if any R 3 -R 5 , R 7 , R 8 , R 11 -R 13 is not hydrogen, R 2 or R 6 or R 9 is not methyl, or R 10 is not CH 2 , then R 1 is selected from the group consisting of hydrogen, a halogen, COOH, C 1 -C 12 carboxylic acids, C 1 -C 12 acyl halides, C 1 -C 12 acyl residues, C 1 -C 12 esters, C 1 -C 12 secondary amides, (C 1 -C 12 )(C 1 -C 12 ) tertiary amides, (C 1 -C 12 )(C 1 -C 12 ) cyclic amides, (C 1 -C 12 ) amines, C 1 -C 12 alcohols, (C 1 -C 12 )(C 1 -C 12 ) ethers, C 1 -C 12 alkyls, C 1 -C 12 substituted alkyls, C 2 -C 12 alkenyls, C 2 -C 12 substituted alkenyls, and C 5 -C 12 aryls. If all R 3 -R 5 , R 7 , R 8 , R 11 -R 13 are hydrogen, R 2 , R 6 , and R 9 are each methyl, and R 10 is CH 2 , then R 1 is selected from hydrogen, a halogen, C 1 -C 12 carboxylic acids, C 1 -C 12 acyl halides, C 1 -C 12 acyl residues, C 2 -C 12 esters, C 2 -C 12 secondary amides, (C 1 -C 12 )(C 1 -C 12 ) tertiary amides, C 2 -C 12 alcohols, (C 1 -C 12 )(C 1 -C 12 ) ethers other than methyl-acetyl ether, C 2 -C 12 alkyls, C 1 -C 12 substituted alkyls, C 2 -C 12 alkenyls, C 2 -C 12 substituted alkenyls, and C 2 -C 12 aryls. R 2 and R 9 are each separately selected from hydrogen, a halogen, C 1 -C 12 alkyl, C 1 -C 12 substituted alkyls, C 2 -C 12 alkenyl, C 2 -C 12 substituted alkenyl, C 2 -C 12 alkynyl, C 1 -C 12 acyl, C 1 -C 12 alcohol, and C 5 -C 12 aryl. R 3 -R 5 , R 7 , R 8 , and R 11 -R 13 are each separately selected from hydrogen, a halogen, C 1 -C 12 alkyl, C 1 -C 12 substituted alkyls, C 2 -C 12 alkenyl, C 2 -C 12 substituted alkenyl, C 2 -C 12 alkynyl, and C 5 -C 12 aryl. R 6 is selected from hydrogen, a halogen, C 1 -C 12 alkyl, C 1 -C 12 substituted alkyls, C 2 -C 12 alkenyl, C 2 -C 12 substituted alkenyl, and C 2 -C 12 alkynyl. R 10 is selected from hydrogen, a halogen, CH 2 , C 1 -C 6 alkyl, C 1 -C 6 substituted alkyl, C 2 -C 6 alkenyl, C 2 -C 6 substituted alkenyl, C 1 -C 12 alcohol, and C 5 -C 12 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.

专利号:US-7119223-B2
优先权日:1999-05-14
标题:Interleukin-1 and tumor necrosis factor-α modulators, synthesis of said modulators and their enantiomers and methods of using said modulators

专利号:JP-2012211162-A
优先权日:1999-05-14
标题 :Novel interleukin-1 and tumor necrosis factor-α modulator, synthesis of the modulator, and method of using the modulator

专利号:US-2006252832-A1
优先权日:1999-05-14
标题 :Novel interleukin-1 and tumor necrosis factor-alpha modulators, synthesis of said modulators and their enantiomers and methods of using said modulators

专利号:US-2003050338-A1
优先权日:1999-05-14
标 题:Novel interleukin-1 and tumor necrosis factor-alpha modulators, synthesis of said and their enantimoners and methods of using said modulators