Following is one of the patent documents most requested by researchers using CAS electronic products.
|
CAS indexed 803 chemical substances from this document.
CAS subject entries for this document include: AIDS (disease); Mental disorder; Lymph node, disease; and 154 additional concepts. | |
CAPLUS COPYRIGHT 2005 ACS on STN
| TITLE:
| Preparation of amides of pyrazolamines and anilines as well as analogs as cytokine inhibitors for the treatment of inflammatory diseases |
| INVENTOR(S):
| Boman, Erik; Ceide, Susana C.; Dahl, Russell; Delaet, Nancy G. J.; Ernst, Justin; Montalban, Antonio G.; Kahl, Jeffrey D.; Larson, Christopher; Miller, Stephen; Nakanishi, Hiroshi; Roberts, Edward; Saiah, Eddine; Sullivan, Robert; Wang, Zhijun |
| PATENT ASSIGNEE(S):
| Kemia, Inc., USA |
| SOURCE:
| PCT Int. Appl., 316 pp. CODEN: PIXXD2 |
| LANGUAGE:
| English |
PATENT INFORMATION: PATENT NO. KIND DATE APPLICATION NO. DATE
--------------- ---- -------- -------------------- --------
WO 2005023761 A2 20050317 WO 2004-US29372 20040910
W: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH,
CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD,
GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC,
LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NI,
NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SY,
TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW
RW: BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW, AM,
AZ, BY, KG, KZ, MD, RU, TJ, TM, AT, BE, BG, CH, CY, CZ, DE, DK,
EE, ES, FI, FR, GB, GR, HU, IE, IT, LU, MC, NL, PL, PT, RO, SE,
SI, SK, TR, BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE,
SN, TD, TG
US 2005107399 A1 20050519 US 2004-939324 20040910
ABSTRACT:
Title compds., such as I and II (four Markush structures are claimed), wherein X = C(O), C(S) or CH2; G = (un)substituted carbocyclyl or heterocyclyl; Ar = indazolyl, indolyl, pyrazolyl, alkyl, etc.; L = covalent bond or (un)substituted carbon chain; Q = H, (un)substituted amino, cycloalkyl, heterocyclyl, alkoxy or sulfonyl; with some limitations and exclusions, and stereoisomers, tautomers, solvates, prodrugs and pharmaceutically acceptable salts thereof, were prepd. as cytokine inhibitors. For instance, cyclization of p-tolylhydrazine hydrochloride with 4,4-dimethyl-3-oxopentanenitrile to the corresponding pyrazolamine (92% yield) followed by EDC-mediated coupling with indazole-3-carboxylic acid gave indazolopyrazole III (40% yield). I were found to have activity in the TNFa ELISA assay, with some compds. having IC50 < 10 .mu.M. Therefore, I and their pharmaceutical compns. are useful in preventing or treating conditions mediated by cytokines, such as arthritis and inflammatory diseases.
Updated 5/8/2007 12:25:41 PM
