Following is one of the patent documents most requested by researchers using CAS electronic products.
|
CAS indexed 932 chemical substances from this document.
CAS subject entries for this document include: Antiarteriosclerotics; Nervous system, disease; Lipids, biological studies; and 15 additional concepts. | |
CAPLUS COPYRIGHT 2005 ACS on STN
| TITLE:
| Pharmaceutical use of substituted 1,2,4-triazoles for modulating the activity of 11.beta.-hydroxysteroid dehydrogenase type 1 (11.beta.HSD1) |
| INVENTOR(S):
| Andersen, Henrik Sune; Kampen, Gita Camilla Tejlgaard; Christensen, Inge Thoger; Mogensen, John Patrick; Larsen, Annette Rosendal |
| PATENT ASSIGNEE(S):
| Novo Nordisk A/S, Den. |
| SOURCE:
| PCT Int. Appl., 155 pp. CODEN: PIXXD2 |
| LANGUAGE:
| English |
PATENT INFORMATION: PATENT NO. KIND DATE APPLICATION NO. DATE
--------------- ---- -------- -------------------- --------
WO 2004089367 A1 20041021 WO 2004-DK249 20040406
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, 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
ABSTRACT:
The use of substituted 1,2,4-triazoles I [X = S, O; R1 = H, alkyl, cycloalkyl, etc.; R2 = alkyl, arylalkyl, cycloalkyl, etc.; R3 = cycloalkyl, aryl, heteroaryl, etc.] for modulating the activity of 11.beta.-hydroxysteroid dehydrogenase type 1 (11.beta.HSD1) and the use of these compds. as pharmaceutical compns. has been described. There general methods of synthesis of compds. I are described (three exemplified compds. I were prepd.). Thus, reacting isonicotinic acid hydrazide with EtNCS in the presence of Et3N in EtOH followed by the addn. of N-(2-chloroethyl)morpholine.HCl in EtOH afforded 22% II which showed IC50 of 0.16 .mu.M against 11.beta.HSD1. Over 900 compds. I were claimed. The present compds. I are modulators and more specifically inhibitors of the activity of 11 .beta.HSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concn. of active glucocorticoid is desirable.
Updated 5/11/2007 12:21:08 PM
