SCHUDOK, MANFRED,WAGNER, MICHAEL,BAUER, ARMIN,KOHLMANN, ANNA
申请号：
EP12178418.5
公开号：
EP2520568A1
申请日:
2007.05.23
申请国别(地区):
EP
年份:
2012
代理人:
摘要：
Die Erfindung betrifft substituierte heterocyclische Spiro-Verbindungen der Formel I,die Cathepsine inhibieren, Verfahren zu ihrer Herstellung und Verwendung derselben als Arzneimittel.Substituted heterocyclic spiro compound (I), is new. Substituted heterocyclic spiro compound of formula (I), is new. Either Ring A, Ring B : saturated or partially saturated 3-11C cycloalkyl (optionally substituted), 3-11 membered heterocycle containing 1-4 heteroatoms of O, S or N (where the heterocycle is unbridged, bridged or annealed, and according to ring size, the cycloalkyl is optionally substituted)； or Ring A-B : spiro compound； X : e.g. covalent bond, -O- or -S-； Y1 : e.g. covalent bond, -C(O)-, -S(O)-, -S(O 2)-, -C(NR1)-, -C(S)-, -C(=N-CN)-, -C(=CHNO 2)- or -CH(CF 3)-； R1 : H, -(1-4C)-alkyl or -(0-4C)-alkylen-(3-6C)-cycloalkyl； either R2, R3 : e.g. H, -(1-10C)-alkyl, -(1-6C)-fluoroalkyl, -(0-4C)-alkylen-(3-8C)-cycloalkyl or -(0-4C)-alkylen-aryl (optionally substituted), -(0-4C)-alkylen-Het (where Het is optionally substituted)； or CR2R3 : 3-6 membered cycloalkyl ring (optionally substituted) or 3-6 membered heterocycloalkyl ring (optionally substituted)； Z : -N(R26)-(C(R24)(R25)) m-CN； R26 : H, -(1-4C)-alkyl or -(0-4C)-alkylene-(3-6C)-cycloalkyl； either R24, R25 : e.g. H, -(1-6C)-alkyl, -(0-4C)-alkylene-(3-6C)-cycloalkyl, -(1-3C)-fluoroalkyl, -(0-4C)-alkylene-aryl (where aryl is optionally substituted) or -(0-4C)-alkylen-Het (where Het is optionally substituted)； or CR24R25 : 3-6 membered cycloalkyl ring (optionally substituted) or 3-6 membered cycloalkyl ring (optionally substituted)； and m : 1-3. Full Definitions are given in the DEFINITIONS (Full Definitions) Field. An independent claim is included for the preparation of (I). [Image] ACTIVITY : Osteopathic； Antiallergic； Neuroprotective； Nootropic； Anticoagulant； Thrombolytic； Antiasthmatic； Antiarteriosclerotic； Immunosuppressive； Virucide； Antibacterial； Hemostatic； Vasotropic； Anticonvulsant； Antiinflammatory； Gas
