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CAS indexed 3335 chemical substances from this document.
CAS subject entries for this document include: Antiarteriosclerotics; Anti-inflammatory agents; Antirheumatic agents; and 7 additional concepts. | |
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CAPLUS COPYRIGHT 2008 ACS on STN
| TITLE:
| Preparation of amide containing heterobicyclic metalloprotease inhibitors |
| INVENTOR(S):
| Steeneck, Christoph; Gege, Christian; Richter, Frank; Kroth, Heiko; Hochguertel, Matthias; Essers, Michael; Van Veldhuizen, Joshua; Nolte, Bert; Gallagher, Brian; Feuerstein, Tim; Schneider, Matthias; Arndt, Torsten; Deng, Hongbo; Biesinger, Ralf; Wu, Xinyuan; Bluhm, Harald; Sucholeiki, Irving; Taveras, Arthur G. |
| PATENT ASSIGNEE(S):
| Alantos Pharmaceuticals, Inc., USA |
| SOURCE:
| U.S. Pat. Appl. Publ., 1030pp., Cont.-in-part of U.S. Ser. No. 440,087. CODEN: USXXCO |
| LANGUAGE:
| English |
PATENT INFORMATION: PATENT NO. KIND DATE APPLICATION NO. DATE
--------------- ---- -------- -------------------- --------
US 2007155738 A1 20070705 US 2006-602140 20061120
US 2006293345 A1 20061228 US 2006-440087 20060522
WO 2007139856 A2 20071206 WO 2007-US12337 20070522
W: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BH, 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, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM,
KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG,
MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT,
RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, SV, SY, TJ, TM, TN, TR,
TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
RW: AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE,
IS, IT, LT, LU, LV, MC, MT, NL, PL, PT, RO, SE, SI, SK, TR, BF,
BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG, BW,
GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW, AM, AZ,
BY, KG, KZ, MD, RU, TJ, TM
ABSTRACT:
The present invention relates generally to amide group contg. pharmaceutical agents, and in particular, to amide contg. heterobicyclic metalloprotease inhibitor compds. More particularly, the present invention provides a new class of heterobicyclic MMP-13 inhibiting and MMP-3 inhibiting compds. I [R1 = H, alkyl, cycloalkyl, etc.; R2 = H, alkyl; or NR1R2 = 3-8 membered ring contg. carbon atoms and optionally a heteroatom selected from O, S(O)x or (un)substituted NH (wherein x = 0-2); R3 = NR20R21; R20 = H, alkyl; R21 = (un)substituted bicyclic or tricyclic fused ring system wherein at least one ring is partially satd.; Q = 5-6 membered ring selected from (un)substituted aryl or heteroaryl; D = CR22, N; R22 = H, OH, halo, etc.] that exhibit an increased potency in relation to currently known MMP-13 and MMP-3 inhibitors. Synthesis of compds. I is described in many examples. Thus, reacting the acid II with the corresponding amine (prepn. of both intermediates is provided) afforded 40% III. Compds. I have a MMP-13 inhibition activity (IC50) ranging from below 0.1 nM to about 20 .mu.M, and typically, from about 0.2 nM to about 2 .mu.M. Pharmaceutical compns. comprising compd. I alone or in combination with therapeutic other agents are disclosed.
Updated 1/25/2008 1:28:11 PM
