27-06-2013 дата публикации
Номер: US20130165390A1
Автор:
Elliott Eric L.,
Ferdous Abu J.,
Kaufman Michael J.,
Komar Sonja A.,
Mazaik Debra L.,
Mccubbin Quentin J.,
Nguyen Phuong M.,
Palaniappan Vaithianathan,
Skwierczynski Raymond D.,
Truong Nobel T.,
Varga Csanad M.,
Zawaneh Peter N.
The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. 3. The compound of claim 2 , wherein each of Rand Rindependently is hydrogen claim 2 , Caliphatic claim 2 , or —(CH)—COH;and p is 0, 1, or 2.4. The compound of wherein P is R—C(O)— claim 3 , R—O—C(O)— claim 3 , R—N(R)—C(O)— claim 3 , R—S(O)— claim 3 , or R—N(R)—S(O)—;{'sup': c', 'D', '1', 'D', '1', '2c, 'sub': 1-6', '1-6, 'claim-text': [{'sup': 1', '3a', '3b', '5', '5, 'sub': '1-6', 'Tis a Calkylene chain substituted with 0-2 independently selected Ror R, wherein the alkylene chain optionally is interrupted by —C(R)═C(R)—, —C≡C—, or —O—;'}, {'sup': 'D', 'Ris a substituted or unsubstituted mono- or bicyclic ring system;'}, {'sup': 2c', '5', '6', '6', '6', '4', '4', '4', '5', '4', '4', '4', '6', '4', '6', '4', '4', '5', '4', '5', '5', '4, 'sub': 2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2, 'Ris halo, —ORe, —SR, —S(O)R, —SOR, —SON(R), —N(R), —NRC(O)R, —NRC(O)—N(R), —NRCOR, —N(R)SOR, —N(R)SON(R), —O—C(O)R, —OC(O)N(R), —C(O)—R, —COR, or —C(O)N(R);'}, {'sup': 3a', '4, 'sub': 1-4', '2', '1-4', '2', '2', '1-4', '2', '1-4, 'each Rindependently is selected from the group consisting of —F, —OH, —O(Calkyl), —CN, —N(R), —C(O)(Calkyl), —COH, —CO(Calkyl), —C(O)NH, and —C(O)—NH(Calkyl);'}, {'sup': 3b', '3a', '7', '3b, 'sub': '1-3', 'each Rindependently is a Caliphatic substituted or unsubstituted with Ror R; or two substituents Ron the same carbon atom, taken together with the carbon atom to which they are attached, form a 3- to 6-membered cycloaliphatic ring;'}, {'sup': '7', 'each Ris a substituted or unsubstituted aromatic group; and'}], 'Ris selected from the group consisting of Caliphatic, Cfluoroaliphatic, —R, -T-R, and -T-R;'}{'sup': '4c', 'sub': 1-4', '1-4', '6-10', '1-4, 'Ris hydrogen, Calkyl, Cfluoroalkyl, or ...
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