| PATENT NUMBER | This data is not available for free |
| PATENT GRANT DATE | 02.04.2002 |
| PATENT TITLE |
Interleukin-1 and tumor necrosis factors-.alpha. modulators, syntheses of said modulators and methods of using modulators |
| PATENT ABSTRACT |
Novel compounds are disclosed that have the chemical structure of Formula (IIB), and its prodrug esters and acid-addition salts, and that are useful as Interleukin-1 and Tumor Necrosis Factor-.alpha. modulators, and thus are useful in the treatment of various diseases. ##STR1## wherein the R groups include the following: R.sub.1 is selected from the group consisting of hydrogen, a halogen, COOH, C.sub.1 -C.sub.12 carboxylic acids, C.sub.1 -C.sub.12 acyl halides, C.sub.1 -C.sub.12 acyl residues, C.sub.1 -C.sub.12 esters, C.sub.1 -C.sub.12 secondary amides, (C.sub.1 -C.sub.12)(C.sub.1 -C.sub.12) tertiary amides, C.sub.1 -C.sub.12 alcohols, (C.sub.1 -C.sub.12)( C.sub.1 -C.sub.12) ethers, C.sub.1 -C.sub.12 alkyls, C.sub.1 -C.sub.12 substituted alkyls, C.sub.2 -C.sub.12 alkenyls, C.sub.2 -C.sub.12 substituted alkenyls; R.sub.2 is selected from hydrogen, a halogen, C.sub.1 -C.sub.12 alkyl, C.sub.1 -C.sub.12 substituted alkyls, C.sub.2 -C.sub.12 alkenyl, C.sub.2 -C.sub.12 substituted alkenyl, C.sub.2 -C.sub.12 alkynyl, and C.sub.1 -C.sub.12 acyl, and C.sub.5 -C.sub.12 aryl. R.sub.3, R.sub.4, R.sub.5, R.sub.7, R.sub.8, and R.sub.11 -R.sub.13 are each separately selected from hydrogen, a halogen, C.sub.1 -C.sub.12 alkyl, C.sub.1 -C.sub.12 substituted alkyls, C.sub.2 -C.sub.12 alkenyl, C.sub.2 -C.sub.12 substituted alkenyl, C.sub.2 -C.sub.12 alkynyl, and C.sub.5 -C.sub.12 aryl. R.sub.6 is selected from hydrogen, a halogen, C.sub.1 -C.sub.12 alkyls, C.sub.1 -C.sub.12 substituted alkyls, C.sub.2 -C.sub.12 alkenyls, C.sub.2 -C.sub.12 substituted alkenyl and C.sub.2 -C.sub.12 alkynyl. R.sub.10 is selected from hydrogen, a halogen, CH.sub.2, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 substituted alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 substituted alkenyl, C.sub.1 -C.sub.12 alcohol, and C.sub.5 -C.sub.12 aryl. -------------------------------------------------------------------------------- |
| PATENT INVENTORS | This data is not available for free |
| PATENT ASSIGNEE | This data is not available for free |
| PATENT FILE DATE | May 12, 2000 |
| PATENT REFERENCES CITED |
Kaufman et al. (1987). Synthesis and 13C nuclear magnetic resonance spectral analysis of some diterpenoids related to the cleisanthane type hydrocarbon isolated from Amphibolis antarctica. Canadian Journal of Chemistry 65(9):pp 2024-2026.* Ohtsuka et al. (1973). Diterpenoids. Chemical and Pharmaceutical Bulletin 21(3): pp 643-652.* Chemical abstracts., vol. 127, No. 1 Jul. 7, 1997 (Columbus Ohio) pp. 594, abstract No. 5280z F.G. Cruz et al. Relative stereochemistry determination of primaradienes through oxidation productions. Chemical abstracts, vol. 116, No. 11, Mar. 16, 1992 (Columbus Ohio), paget 411, abstract No. 102659c, C.M. Chamy et al. "Diterpenoids from Calceolaria species, Part 10. Diterpenes from Calceolaria polifolia" Phytochemistry 1991, 30(10), 3365-8. Chemical Abstracts, vol. 114, No. 3, Jan. 21, 1991 (Columbus Ohio), p. 408, abstract No 20960p, C.M. Chamy et al. "Diterpenoids from Calceolaria species Part 5. Diterpenes from Calceolaria lepida" Phytochemistry 1990, 29(9), 2943-6. Chemical abstracts, vol. 77, No. 15, Oct. 9, 1972 (Columbus Ohio), p. 193, abstract no. 98751h, V.K. Morozkov et al. "Neutral fraction of the oleoresim of Pinus sylvestri 3. Norditerpene compounds". Izv. Sib. Otd. Akad Nauk SSSR, Ser, Khim. Nauk 1972, (1), 128-34. Kim, Y.H. Chung B.S. Pimaradiene Diterpenes from Acanthopanax Koreanum, Journal of Natural Products, 1998, vol. 51, No. 6, pp. 1080-1083; p. 1080, paragraphs 1-3, compound No. 2, p. 1082, pa ragraph Extraction and Isolation (cited in the application). Kaufman et al. (1995). Synthesis and mass spectral data of four potential biomarkers related to the C19 tricyclanes found in Australian oils and Puget sound sediments. Synth. Commun., 25(8), pp 1205-1221. |
| PATENT PARENT CASE TEXT | This data is not available for free |
| PATENT PHOTOCOPY | Available on request |
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