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公开(公告)号:NO20055150L
公开(公告)日:2005-11-04
申请号:NO20055150
申请日:2005-11-03
Applicant: HOFFMANN LA ROCHE
Inventor: JAKOB-ROETNE ROLAND , RIEMER CLAUS , FLOHR ALEXANDER , NORCROSS ROGER DAVID
IPC: A61K31/428 , A61P25/28 , C07D277/82 , C07D417/02 , C07D417/04 , C07D417/14 , C07D491/10
Abstract: This invention relates to compounds of formula I wherein R 1 and R 2 are defined herein, or a pharmaceutically acceptable salt thereof. It has been found that the compounds of formula I are adenosine receptor ligands with good affinity to the A 2A -receptor and a high selectivity to the A 1 - and A 3 receptors. These compounds are useful, inter alia, in treatment of Alzheimer's disease, depression, Parkinson's disease and ADHD.
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公开(公告)号:AR044362A1
公开(公告)日:2005-09-07
申请号:ARP040101684
申请日:2004-05-17
Applicant: HOFFMANN LA ROCHE
Inventor: FLOHR ALEXANDER , JAKOB-ROETNE ROLAND , NORCROSS ROGER DAVID , RIEMER CLAUS
IPC: A61K31/428 , A61P25/28 , C07D277/82 , C07D417/02 , C07D417/04 , C07D417/14 , C07D491/10 , C07D417/12 , C07D491/113 , A61K31/423 , A61K31/438 , A61P25/08 , A61P25/16 , A61P25/20
Abstract: Se refiere a compuestos de la fórmula general (1), en la que: R1 es 1,4-dioxepanilo o tetrahidropiran-4-ilo; R2 es -N(R)-(CH2)n-heterociclo no aromático de 5 ó 6 eslabones, opcionalmente sustituido por uno o varios sustituyentes elegidos entre alquilo inferior y -NR2 o es -(CH2)n-heterociclo no aromático de 5 ó 6 eslabones, opcionalmente sustituido por -(CH2)n-OH, alquilo inferior, alcoxi inferior o es -(CH2)n-heterociclo aromático de 5 ó 6 eslabones, opcionalmente sustituido por alquilo inferior, alcoxi inferior, halógeno, halógeno-alquilo inferior, -CH2N(R)-(CH2)2OCH3, -N(R)(CH2)2OCH3, -CH2-morfolinilo o -CH2-pirrolidinilo o es (CH2)n-cicloalquilo, opcionalmente sustituido por hidroxi o es -N(R)-cicloalquilo, opcionalmente sustituido por hidroxi o alquilo inferior o es fenilo, opcionalmente sustituido por alcoxi inferior, halógeno, halógeno-alquilo inferior, alquilo inferior, -CH2-pirrolidin-1-ilo, -CH2-morfolinilo, -CH2N(R)(CH2)2OCH3 o -CH2-N(R)C(O)-alquilo inferior o es 1,4-dioxa-8-aza-espiro[4,5]decano o es 2-oxa-5-aza-biciclo[2.2.1]heptano o es 1-oxa-8-aza-espiro[4,5]decano o es -N(R)-7-oxa-biciclo[2.2.1]hept-2-ilo o es 2-aza-biciclo[2.2.2]decano; R es hidrógeno o alquilo inferior; n es el número 0 ó 1; y a sales de adición de ácido farmacéuticamente aceptables de los mismos para el tratamiento de enfermedades en las que interviene el receptor A2A.
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公开(公告)号:PL371064A1
公开(公告)日:2005-06-13
申请号:PL37106402
申请日:2002-12-05
Applicant: HOFFMANN LA ROCHE
Inventor: FLOHR ALEXANDER , JAKOB-ROETNE ROLAND , NORCROSS ROGER DAVID , RIEMER CLAUS
IPC: C07D277/82 , A61K31/428 , A61K31/4439 , A61K31/454 , A61K31/5377 , A61P9/10 , A61P11/00 , A61P21/02 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P29/00 , A61P43/00 , C07D277/84 , C07D417/04 , C07D417/12 , C07D417/14
Abstract: The present invention relates to compounds of the formula wherein R1 and R2 are as described within. The compounds of formula I have been found to be adenosine receptor ligands. Specifically, the compounds of the present invention have a good affinity to the A2A-receptor and they may be used in the treatment of diseases, related to this receptor.
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公开(公告)号:PL371063A1
公开(公告)日:2005-06-13
申请号:PL37106302
申请日:2002-12-05
Applicant: HOFFMANN LA ROCHE
Inventor: FLOHR ALEXANDER , JAKOB-ROETNE ROLAND , NORCROSS ROGER DAVID , RIEMER CLAUS
IPC: C07D277/82 , A61K31/428 , A61K31/454 , A61K31/4747 , A61K31/497 , A61K31/5377 , A61K31/5386 , A61K31/553 , A61P9/10 , A61P11/06 , A61P11/16 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/22 , A61P25/28 , A61P25/36 , A61P37/08 , A61P43/00 , C07D413/14 , C07D417/00 , C07D417/04 , C07D417/12 , C07D453/06 , C07D471/10 , C07D487/08 , C07D491/08 , C07D491/107 , C07D498/08
Abstract: A compound of formula I and a method of treatment of diseases, related to modulation of the adenosine A 2 receptor system comprising administering a compound of formula to a person in need of such treatment.
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公开(公告)号:ZA200403817B
公开(公告)日:2005-05-23
申请号:ZA200403817
申请日:2004-05-18
Applicant: HOFFMANN LA ROCHE
Inventor: FLOHR ALEXANDER , NORCROSS ROGER DAVID , JAKOB-ROETNE ROLAND , 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 , A61K , C07D
Abstract: The present invention relates to compounds of the formulawherein R1, A and R are as described within. The compounds of the present invention have been found to be adenosine receptor ligands. Specifically, the compounds of the present invention have an affinity to the A2A-receptor and are therefore useful in the treatment of diseases related to this receptor.
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公开(公告)号:HRP20020962A2
公开(公告)日:2005-02-28
申请号:HRP20020962
申请日:2002-12-05
Applicant: HOFFMANN LA ROCHE
Inventor: ALANINE ALEXANDER , FLOHR ALEXANDER , MILLER AUBRY KERN , NORCROSS ROGER DAVID , RIEMER CLAUS
IPC: A61K31/422 , A61K31/423 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/455 , A61K31/4725 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K31/5513 , A61P11/06 , A61P21/02 , A61P25/04 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/26 , A61P25/28 , C07D277/82 , C07D417/04 , C07D417/12 , C07D417/14
Abstract: The present invention relates to compounds of the general formula and to their pharmaceutically acceptable salts for the treatment of diseases related to the adenosine receptor.
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公开(公告)号:MA26599A1
公开(公告)日:2004-12-20
申请号:MA25434
申请日:1999-01-15
Applicant: HOFFMANN LA ROCHE
Inventor: BOES MICHAEL , HUNKELER WALTER , RIEMER CLAUS
IPC: C07C309/30 , A61K31/00 , A61K31/10 , A61K31/135 , A61K31/44 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/4433 , A61K31/4436 , A61K31/505 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P43/00 , C07C315/04 , C07C317/22 , C07C317/32 , C07C317/36 , C07D213/61 , C07D213/62 , C07D213/71 , C07D213/73 , C07D213/74 , C07D213/84 , C07D239/38 , C07D401/04 , C07D401/14 , C07D409/04 , C07C309/00 , A61K31/095
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公开(公告)号:YU13502A
公开(公告)日:2004-11-25
申请号:YUP13502
申请日:2000-08-28
Applicant: HOFFMANN LA ROCHE
Inventor: HUBER TROTTMANN GERDA , 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
Abstract: Pronalazak se odnosi na jedinjenja formule I, naznacena time sto R1 perdstavlja 5-to ili 6-toclanu heteroarilnu grupu, koja sadrzi 1 do 3 heteroatoma, izabrana izmedju N, O ili S, i cije su grupe opciono supstituisane jednim ili sa dva supstituenta, koji su nizi alkil, -(CH2)nOH, halogen ili nizi alkoksi, i naznacena time sto heteroarilne grupe mogu biti opciono vezane za pirazolski prsten preko nekog alkilena ili alkenil grupe ili je to fenil, opciono supstituisan jednim ili sa dva supstituenta, koji su nizi alkil, hidroksi-nizi alkil, halogen, hidroksi ili nizi alkoksi ili je -O(CH2)nfenil, benzofuril, indolil ili benzotiofenil ili je -S-nizi alkil; R2 i R4 su nezavisno jedan od drugog, vodonik, cijano ili -S(O)2-fenil; R3 je vodonik, halogen ili 5-to ili 6-toclana heteroarilna grupa, koja sadrzi 1 do 3 heteroatoma, izabrana izmedju N, O ili S i gde su grupe opciono supstituisane jednim ili sa dva supstituenta, koji su nizi alkil, -(CH2)n-aril, hldroksi, halogen, nizi alkoksi, morfolinil, amino, nizi alkilamino ili -C(O)NR'2, naznaceno time sto je R* nizi alkil ili vodonik ili je fenil, opciono supstituisan jednim ili sa dva supstituenta koji su halogen, nizi alkoksi, amino, di-nizi alkil amino, CF3, -OCF3, -NHC(O)nizi alkil cijano, -C(O)-nizi alkil, -C(O)O-nizi alkil, -S-nizi alkil, -S(O)2NH-fenil, -S(O)2metilpiperazinil; ili je NR'R", naznacen time sto su R' i R", nezavisno jedan od drugog, vodonik, -(CH2)nfenil, koji je opciono supstituisan halogenom ili nizom alkoksi grupom, -CH(nizi alkil)-fenil, indan-1-il, 1,2,3,4-tetrahidro-naftalen ili cikloalkil; ili je O-fenil, ciji je fenilni prsten opciono supstituisan halogenom, nizom alkil ili nizom alkoksi grupom, -O-tetraidronaftalenil ili -O-CH2-6-metil-piridin-2-il; ili je -benzol[1,3]dioksolil, -1H-indol-5-il, naftil, benzofuran-2-il, 1,3,4,9-tetrahidro-b-karbolin-2-il, piperidin-1-il, pirolidin-1-il, piperazin-4-il-metil ili morfolinil; R5 je -NR2, pri cemu R moze ili ne mora biti vodonik, nizi alkil, fenil, benzil, -CO-nizi alkil, -CO-nizi alkoksi, -nizi alkenil, -CO(CH2)n-fenil ili -COO(CH2)n-fenil, naznacen time sto je fenilni prsten opciono supstituisan sa CF3 nizom alkoksi, halogen ili nizom alkil grupom, -CO(CH2)3-NHCO-nizi alkoksi, -(CH2)n-fenil, naznacen time, sto je fenilni prsten opciono supstituisan nizom alkoksi, CF3 ili halogenom ili je 4,5-dihidro-1H-imidazol-2-il-benzojeva kiselina, 1,4,5,6-tetrahidro-pirimidin-2-il-benzojeva kiselina ili 4,5,6,7-tetrahidro-1H-[1,3]diazepin-2-il-benzojeva kiselina; n je 0-4, i njihove farmaceutski prihvatljive soli.
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公开(公告)号:BR0214488A
公开(公告)日:2004-10-19
申请号:BR0214488
申请日:2002-11-21
Applicant: HOFFMANN LA ROCHE
Inventor: FLOUHR ALEXANDER , JAKOB-ROETNE ROLAND , NORCROSS ROGER DAVID , RIEMER CLAUS
IPC: A61K31/428 , A61K31/5377 , A61P9/00 , A61P9/04 , A61P9/10 , A61P11/00 , A61P11/06 , A61P21/02 , A61P25/00 , A61P25/02 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/36 , A61P29/00 , A61P37/08 , A61P43/00 , C07D277/82 , C07D417/12
Abstract: The present invention relates to compounds of the formulawherein R and R are as defined herewithin. The compounds of formula I have been found to be adenosine receptor ligands. Specifically, the compounds of the present invention have a good affinity to the A2A-receptor and they are therefore useful in the treatment of diseases, related to this receptor.
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公开(公告)号:HK1058148A1
公开(公告)日:2004-05-07
申请号:HK04100949
申请日:2004-02-12
Applicant: HOFFMANN LA ROCHE
Inventor: ALANINE ALEXANDER , FLOHR ALEXANDER , MILLER AUBRY KERN , NORCROSS ROGER DAVID , RIEMER CLAUS
IPC: A61K31/422 , A61K31/423 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/455 , A61K31/4725 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K31/5513 , A61P11/06 , A61P21/02 , A61P25/04 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/26 , A61P25/28 , C07D277/82 , C07D417/04 , C07D417/12 , C07D417/14 , A61K , C07D , A61P
Abstract: The present invention relates to compounds of the general formula and to their pharmaceutically acceptable salts for the treatment of diseases related to the adenosine receptor.
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