Following is one of the Patent Families most requested by researchers using CAS electronic products.
|
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. | |
|
CAPLUS COPYRIGHT 2007 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
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 11/5/2007 2:01:37 PM
