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    DERIVADOS DE BENZOTIAZOL
    91.
    发明专利
    DERIVADOS DE BENZOTIAZOL 未知

    公开(公告)号：PA8558201A1

    公开(公告)日：2003-09-05

    申请号：PA8558201

    申请日：2002-11-22

    Applicant: HOFFMANN LA ROCHE

    Inventor： FLOHR ALEXANDER ,  RIEMER CLAUS ,  JAKOB-ROETNE ROLAND ,  NORCROSS ROGER DAVID

    IPC: A61K31/428 ,  A61K31/429 ,  A61K31/44 ,  A61K31/5377 ,  A61P9/04 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P21/02 ,  A61P25/04 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P37/08 ,  A61P39/02 ,  C07D277/68 ,  C07D277/82 ,  C07D409/12 ,  C07D417/12 ,  C07D477/12 ,  C07D417/09

    Abstract: LA INVENCION SE REFIERE A COMPUESTOS DE FORMULA GENERAL EN DONDE R ES HIDROGENO, - (CH2)N-FENILO, OPCIONALMENTE SUSTITUIDO POR HALOGENO, ALQUILO INFERIOR, ALCOXILO INFERIOR, TRIFLUOROMETILO O -N(R´)-C(O)-ALQUILO INFERIOR,-(CH2)N-PIRIDINILO, OPCIONALMENTE SUSTITUIDO POR ALQUILO INFERIOR,-(CH2)N-C3-6-CICLOALQUILO, OPCIONALMENTE SUSTITUIDO POR HIDROXILO,-(CH2)N-N(R´) -C3-6-CICLOALQUILO,-(CH2)N-BENZO [1,3]-DIOXILO,-(CR´2)-TIOFENILO, OPCIONALMENTE SUSTITUIDO POR ALQUILO INFERIOR,-(CR´2)N-TIAZOLILO, OPCIONALMENTE SUSTITUIDO POR ALQUILO INFERIOR,-(CH2)N-C(O)-TIOFENILO, OPCIONALMENTE SUSTITUIDO POR HALOGENO,-(CH2)N-FURANILO, OPCIONALMENTE SUSTITUIDO POR ALQUILO INFERIOR,-(CH2)N-C(O)-(CH2)N-TIOFENILO,-(CHR´)N-BENZOFURAN-2-ILO,-(CH2)N-BENZO[B]TIOFENILO,OPCIONALMENTE SUSTITUIDO POR ALQUILO INFERIOR, -(CH2)N-N(R´)-C(O)-FENILO, OPCIONALMENTE SUSTITUIDO POR HALOGENO O ALCOXILO INFERIOR, -(CH2)N-C(O)-FENILO, OPCIONALMENTE SUSTITUIDO POR ALCOXILO INFERIOR, -(CH2)N-C(O)-2, 3-DIHIDRO-BENZO[1,4]DIOXIN-6-ILO, -(CH2)N-N(R´)-C(O)-PIRIDINILO,-(CH2)N-TETRAHIDROFURANILO,-CH-BI-FENILO,-CH(FENIL)-PIRIDINILO, -(CH2)N-1-OXO-1-OXO-1, 3-DIHIDRO-ISOINDOL-2-ILO, -(CH2)N-1, 3-DIOXO-1,3-DIHIDRO-ISOINDOL -2-ILO, -(CH2)N-CH(FENIL)-TETRAHIDROPIRANILO, -(CH2)N-1-OXO-1,2,3,4-TETRAHIDRO-ISOQUINOLIN-3-IL O -(CH2)N-S-[1,3,4]TIAZOL-2-ILO, OPCIONALMENTE SUSTITUIDO POR AMINO; ES HIDROGENO O ALQUILO INFERIOR, INDEPENDIENTEMENTE UNO DEL OTRO EN EL CASO DE R´2; Y N ES 0,1,2,3 O 4; Y LAS SALES DE ADICION ACIDA FARMACEUTICAMENTE ACEPTABLES DE LOS MISMOS. LOS COMPUESTOS DE FORMULA I TIENEN UNA BUENA AFINIDAD POR EL RECEPTOR A2A Y ESTOS SON POR LO TANTO UTILES EN EL TRATAMIENTO DE ENFERMEDADES, RELACIONADAS CON ESTE RECEPTOR.

    DERIVADOS DE ISONICOTIN Y NICOTINAMIDA DE BENZOTIAZOLES
    93.
    发明专利
    DERIVADOS DE ISONICOTIN Y NICOTINAMIDA DE BENZOTIAZOLES 未知

    公开(公告)号：PA8558001A1

    公开(公告)日：2003-07-28

    申请号：PA8558001

    申请日：2002-11-14

    Applicant: HOFFMANN LA ROCHE

    Inventor： FLOHR ALEXANDER ,  JAKOB-ROETNE ROLAND ,  NORCROSS ROGER DAVID ,  RIEMER CLAUS

    IPC: A61K31/4439 ,  A61K31/5377 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/32 ,  A61P25/34 ,  A61P25/36 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D417/12 ,  C07D417/14

    Abstract: LA PRESENTE INVENCION SE REFIERE A LOS COMPUESTOS DE FORMULA GENERAL EN DONDE R1 ES FENILO, PIPERIDIN-1-ILO O MORFOLINILO; A ES -O- Y R ES - (CH2) N-N(R' ') -C(O) -ALQUILO INFERIOR, -(C2)N-O-ALQUILO INFERIOR, -(CH2), N-O-(CH2)N-O-ALQUILO INFERIOR. ALQUILO INFERIOR, -(CH2)n-MORFOLINILO, -(CH2)n-FENILO, -(CH2)n- N (R' ') 2, -(CH2) N-PIRIDINILO, -(CH2)N-CF3, -(CH2)n-2-OXO-PIRROLIDINILO O C4-6-CICLOALQUILO; R' ' ES INDEPENDIENTEMENTE UNO DEL OTRO HIDROGENO O ALQUILO INFERIOR Y N ES 1 O 2; O A ES -N(R')-Y R ES ALQUILO INFERIOR, C4-6-CICLOALQUILO, -(CH2)N-O-ALQUILO INFERIOR, -(CH2)N-PIRIDINILO, -(CH2)N-PIPERIDINILO, -(CH2)N N-FENILO, -(CH2)N -N(R' ')-C(O)-ALQUILO INFERIOR, -(CH2)N-MORFOLINILO, 0-(CH2)N-N(R' ')2; R' Y R' ' SON INDEPENDIENTEMENTE UNO DEL OTRO HIDROGENO O ALQUILO INFERIOR Y N ES 1 O 2; O A ES -CH2- Y R ES -N(R' ')-(CH2)M-O-ALQUILO INFERIOR, -N(R' ')2, S-ALQUILO INFERIOR, O ES ACETIDINILO, PIRROLIDINILO O PIPERIDINILO, QUE ESTAN OPCIONALMENTE SUSTITUIDOS POR HIDROXILO O ALCOXILO INFERIOR O ES MORFOLINILO,- N(R'') -(CH2)M-C4-6-CICLOALQUILO, -N(R'')-(CH2)M-C(O)O-ALQUILO INFERIOR, -N(R'')-(CH2)M-C(O) OH, -2-OXO-PIRROLIDINILO, -N(R'')-C(O)O-ALQUILO INFERIOR, -O(CH2)M-O-ALQUILO INFERIOR O ALCOXILO; R'' ES INDEPENDIENTEMENTE UNO DEL OTRO HIDROGENO O ALQUILO INFERIOR Y M ES 1,2 Ó 3; O A ES-S-Y R ES ALQUILO INFERIOR; O A-R SON JUNTOS-PIPERAZINILO, SUSTITUIDO POR ALQUILO INFERIOR, -C(O)-ALQUILO INFERIOR O UN GRUPO OXO, O ES PIPERIDINILO, SUSTITUIDO POR ALCOXILO INFERIOR O HIDROXILO, O ES MORFOLINILO, SUSTITUIDO POR ALQUILO INFERIOR, O ES-C4-6-CICLOALQUILO, - AZETIDIN-1-ILO, OPCIONALMENTE SUSTITUIDO POR HIDROXILO O ALCOXILO INFERIOR, TIOMORFOLIN-1,1- POR DIOXO,- TETRAHIDOPIRANO O 2-OXA-5-AZA-BICICLO[2.2.1]HEPT-5-ILO; Y LAS SALES FARMACEUTICAMENTE ACEPTABLES DE LOS MISMOS. SE HA ENCONTRADO QUE LOS COMPUESTOS DE FORMULA GENERAL I SON LIGANDOS DEL RECEPTOR DE ADENOSINA. ESPECIFICAMENTE, LOS COMPUESTOS DE LA PRESENTE INVENCION TIENEN UNA BUENA AFINIDAD POR EL RECEPTOR A2A Y ESTOS SON POR LO TANTO UTILES EN EL TRATAMIENTO DE ENFERMEDADES RELACIONADAS CON ESTE RECEPTOR.

    PRODRUGS TO D-PROLINES
    94.
    发明专利
    PRODRUGS TO D-PROLINES 未知

    公开(公告)号：CA2470037A1

    公开(公告)日：2003-06-26

    申请号：CA2470037

    申请日：2002-12-06

    Applicant: HOFFMANN LA ROCHE

    Inventor： POLI SONIA MARIA ,  JAKOB-ROETNE ROLAND ,  HUWYLER JOERG

    IPC: A61K31/401 ,  A61K31/407 ,  A61P3/10 ,  A61P25/28 ,  A61P43/00 ,  C07D207/16 ,  C07D498/14

    Abstract: The invention relates to compounds of formulae (I) or (IA), wherein R1 and R 2 are independently from each other and signify lower alkoxy, lower alkenyloxy , benzyloxy, hydroxy, -OCH(CH3)OC(O)-lower alkyl or OCH2C(O)N(R3)(R4), with th e proviso that only one of R1 or R2 may be hydroxy; R3 and R4 are independentl y from each other and signify hydrogen, lower alkyl, lower alkenyl or cycloalkyl; or R1 and R2 form together with the carbon atom, to which they a re attached the linking group X, wherein X is -O(CH2)nCH=CH(CH2)n0- or -O(CH2)m O- ; n is l, 2 or 3; and m is 4-8. as well as pharmaceutically acceptable salts of said compounds. Compounds of the present invention can be used for the treatment of diseases where Serum Amyloid P Component depletion has a beneficial effect, in particular in the treatment or prevention of all forms of central and systemic amyloidosis.

    99.
    发明专利
    未知

    公开(公告)号：NO20021077D0

    公开(公告)日：2002-03-05

    申请号：NO20021077

    申请日：2002-03-05

    Applicant: HOFFMANN LA ROCHE

    Inventor： TROTTMANN GERDA HUBER ,  HUNKELER WALTER ,  JAKOB-ROETNE ROLAND ,  KILPATRICK GAVIN JOHN ,  NETTEKOVEN MATTHIAS HEINRICH ,  RIEMER CLAUS

    IPC: C07D213/73 ,  A61K31/437 ,  A61K31/4418 ,  A61K31/444 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/551 ,  A61K31/635 ,  A61P9/10 ,  A61P11/06 ,  A61P11/16 ,  A61P25/00 ,  A61P25/04 ,  A61P25/08 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P37/08 ,  A61P43/00 ,  C07D409/04 ,  C07D471/04 ,  C07D519/00 ,  C07D

    Abstract: The invention relates to compounds of formulawhereinR1 is a 5 or 6 membered heteroaryl group, containing 1 to 3 heteroatoms, selected from N, O or S, and which groups are optionally substituted by one or two substituents, which are lower alkyl, -(CH2)nOH, halogen or lower alkoxy, and wherein the heteroaryl groups may be optionally linked to the pyrazole ring via an alkylene or alkenyl group, or isphenyl, optionally substituted by one or two substituents being lower alkyl, hydroxy-lower alkyl, halogen, hydroxy or lower alkoxy or is-O(CH2)n,phenyl, benzofuryl, indolyl or benzothiophenyl, or is-S-lower alkyl;R2 and R4 are independently from each other hydrogen, cyano or -S(O)2-phenyl;R3 is hydrogen, halogen or isa 5 or 6 membered heteroaryl group, containing 1 to 3 heteroatoms, selected from N, O or S, and which groups are optionally substituted by one or two substituents, which are lower alkyl, -(CH2)n-aryl, hydroxy, halogen, lower alkoxy, morpholinyl, amino, lower alkylamino or -C(O)NR'2, and wherein R' is lower alkyl or hydrogen, or isphenyl, optionally substituted by one or two substituents being halogen, lower alkyl, lower alkoxy, amino, di-lower alkyl amino, CF3, -OCF3, -NHC(O)lower alkyl, cyano, -C(O)-lower alkyl, -C(O)O-lower alkyl, -S-lower alkyl, -S(O)2NH-phenyl, -S(O)2-methylpiperazinyl; or is-NR'R'', wherein R' and R'' are independently from each other hydrogen, -(CH2)nphenyl, which phenyl ring is optionally substituted by halogen or lower alkoxy, -CH(lower alkyl)-phenyl, indan-1-yl, 1,2,3,4-tetrahydro-naphthalen, or cycloalkyl; or is-O-phenyl, which phenyl ring is optionally substituted by halogen, lower alkyl or lower alkoxy, -O-tetrahydronaphthalenyl or -O-CH2-6-methyl-pyridin-2-yl; or is-benzo[1,3]dioxolyl, -1H-indol-5-yl, naphthyl, benzofuran-2-yl, 1,3,4,9-tetrahydro-b-carbolin-2-yl, piperidin-1-yl, pyrrolidin-1-yl, piperazin-4-yl-methyl or morpholinyl;R5 is -NR2, wherein R may be the same or different and is hydrogen, lower alkyl, phenyl, benzyl, -CO-lower alkyl, -CO-lower alkoxy, -lower alkenyl, -CO(CH2)n-phenyl or -COO(CH2)n-phenyl, wherein the phenyl ring is optionally substituted by CF3, lower alkoxy, halogen or lower alkyl, -CO(CH2)3-NHCO-lower alkoxy, -(CH2)n-phenyl, wherein the phenyl ring is optionally substituted by lower alkoxy, CF3 or halogen, or is 4,5-dihydro-1H-imidazol-2-yl-benzoic acid, 1,4,5,6-tetrahydro-pyrimidin-2-yl-benzoic acid or 4,5,6,7-tetrahydro-1H-[1,3]diazepin-2-yl-benzoic acid;n is 0-4and their pharmaceutically acceptable salts

    Oxazolidine-2-one derivatives.
    100.
    发明专利
    Oxazolidine-2-one derivatives. 未知

    公开(公告)号：GR3033815T3

    公开(公告)日：2000-10-31

    申请号：GR20000401515

    申请日：2000-06-29

    Applicant: HOFFMANN LA ROCHE

    Inventor： BORGULYA JANOS ,  BRUDERER HANS ,  JAKOB-ROETNE ROLAND ,  ROEVER STEPHAN

    IPC: A61K31/42 ,  A61K31/421 ,  A61K31/422 ,  A61K31/425 ,  A61K31/44 ,  A61K31/445 ,  A61P25/00 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  C07D263/24 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14

    Abstract: The invention relates to oxazolidin-2-one derivatives of the formula wherein R is hydrogen or lower alkyl; X is cycloalkenyl; bicyclo[2.2.1]hept-2-yl, opt. substituted by phenyl-2-oxo-5-methoxymethyloxazolidinyl; bicyclo[2.2.1]hept-5-en-2-yl; adamantyl; or cycloalkyl or piperidine, optionally mono- or polysubstituted by halogen, amino, lower alkyl, nitrile, an oxo group, hydroxyimino, ethylenedioxy or by -OR , wherein R is -CH(C6H5)2, -(CH2)nC6H5, lower alkyl, hydrogen, - (CH2)nNHCOCH3, -(CH2)nNH2, -(CH2)nSOCH3, -(CH2)nCN, -(CH2) nSCH3, -(CH2)nSO2CH3, -CO-lower alkyl, -COC6H5, opt. substituted by an oxazolidinyl group: or by =CR R , wherein R is hydrogen or lower alkyl; R is hydrogen, nitrile, lower alkyl, phenyl or COO-lower alkyl; or by -(CH2)nR , wherein R is nitrile, amino, -NHCOCH3, -COC6H5Hal, phenyl or hydroxyl; or by -COR , wherein R is lower alkyl, -CH=CH-C6H5, -C6H5CF3, -O-C(CH3)3 or -O-lower alkyl; or by -NR R , wherein R is hydrogen or -COCH3; R is -COCH3, benzyl or -(CH2)nNHCOC6H4Hal; n is 1-3; Y is -CH= or -N=; Y is -CH=, -C(OH)=, -C(NO2)=, -C(NH2)=, -C(Hal)= or -N= and pharmaceutically acceptable salts of basic compounds of the formula I with acids. These novel compounds and their pharmaceutically acceptable salts can be used for the prevention or control of depressive states, panic and anxiety states, cognitive disorders and neurodegenerative disorders such as Parkinson's disease and Alzheimer's disease.

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