公开(公告)号：AU2002210474B2

公开(公告)日：2006-11-02

申请号：AU2002210474

申请日：2001-08-30

Applicant: HOFFMANN LA ROCHE

Inventor： PFLIEGER PHILIPPE ,  DAUTZENBERG FRANK ,  GUERRY PHILIPPE ,  BREU VOLKER ,  NETTEKOVEN MATTHIAS HEINRICH

IPC: C07D215/00 ,  C07D239/94 ,  A61K31/365 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/00 ,  A61P1/14 ,  A61P3/00 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P13/12 ,  A61P19/02 ,  A61P43/00 ,  C07D215/42 ,  C07D239/84 ,  C07D401/04 ,  C07D409/04

Abstract: Quinoline and quinazoline derivatives can be used in the form of pharmaceutical preparations as Neuropeptide Y antagonists for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.

公开(公告)号：ZA200302970B

公开(公告)日：2004-07-15

申请号：ZA200302970

申请日：2003-04-15

Applicant: HOFFMANN LA ROCHE

Inventor： BREU VOLKER ,  MATTEI PATRIZIO ,  PFLIEGER PHILIPPE ,  DAUTZENBERG FRANK ,  NEIDHART WERNER

IPC: A61K31/337 ,  A61K31/505 ,  A61K31/506 ,  A61P3/04 ,  A61P3/10 ,  A61P19/02 ,  A61P43/00 ,  C07D239/42 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D ,  A61K

Abstract: Pyrimidine derivatives have been found to be useful as neuropeptide Y receptor ligands and particularly as antagonists. These pyrimidine derivatives may be used in the form of pharmaceutical preparations for the treatment or prevention of arthritis, diabetes, eating disorders, and obesity.

公开(公告)号：AU1047402A

公开(公告)日：2002-03-22

申请号：AU1047402

申请日：2001-08-30

Applicant: HOFFMANN LA ROCHE

Inventor： BREU VOLKER ,  DAUTZENBERG FRANK ,  GUERRY PHILIPPE ,  NETTEKOVEN MATTHIAS HEINRICH ,  PFLIEGER PHILIPPE

IPC: C07D239/94 ,  A61K31/365 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/00 ,  A61P1/14 ,  A61P3/00 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P13/12 ,  A61P19/02 ,  A61P43/00 ,  C07D215/00 ,  C07D215/42 ,  C07D239/84 ,  C07D401/04 ,  C07D409/04

Abstract: Quinoline and quinazoline derivatives can be used in the form of pharmaceutical preparations as Neuropeptide Y antagonists for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.

公开(公告)号：PE20000549A1

公开(公告)日：2000-07-24

申请号：PE00048599

申请日：1999-06-08

Applicant: HOFFMANN LA ROCHE

Inventor： WICHMANN JURGEN ,  ADAM GEO ,  ROVER STEPHAN ,  DAUTZENBERG FRANK ,  KOLCZEWSKI SABINE

IPC: C07D401/14 ,  A01N43/42 ,  A61K31/00 ,  A61K31/395 ,  A61K31/435 ,  A61K31/438 ,  A61K31/44 ,  A61K31/445 ,  A61K31/505 ,  A61K31/535 ,  A61P3/04 ,  A61P3/12 ,  A61P9/12 ,  A61P25/04 ,  A61P25/08 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  C07D20060101 ,  C07D209/00 ,  C07D221/00 ,  C07D471/10 ,  C07D471/20 ,  C07D487/20 ,  C07D498/10 ,  C07D513/10

Abstract: SE REFIERE A ESPIRO[PIPERIDIN-4,1`-PIRROLO[3,4-c]PIRROL] DE FORMULA I, DONDE R1 ES CICLOALQUILO C5-C12 OPCIONALMENTE SUSTITUIDO CON ALQUILO, DECAHIDRO-NAFTALEN-1-ILO, INDAN-1-IL, DECAHIDRO-AZULEN-2-ILO, BICICLO[6.2.0]DEC-9-ILO, ACENAFTEN-1-ILO, BICICLO[3.3.1]NON-9-ILO, 2,3-DIHIDRO-1H-FENALEN-1-ILO, ENTRE OTROS; R2 Y R3 SON H, OH, ALQUILO, =O, FENILO OPCIONALMENTE SUSTITUIDO CON ALQUILO, HALOGENO, ALCOXILO; R4 ES H, ALQUILO, (CH2)nCHOHCF3, -(CH2)n-CICLOALQUILO C3-C6, FENILO, BENCILO, TETRAHIDROFURAN-3-ILO, -(CH2)nOCH2C6H5, -(CH2)nMORFOLINILO, 3-METIL-OXETAN-3-IL-METILO, -(CH2)nCH2OH, -SO2-ALQUILO, -CO-ALQUILO, -COCF3, ENTRE OTROS; R5 ES H, HALOGENO, ALQUILO, TRIFLUOROMETILO, ALCOXILO; n ES 0-3. SON COMPUESTOS PREFERIDOS (3'aRS,6'aSR)-1-CICLONONIL-5'-METIL-2'-FENIL-HEXAHIDRO-ESPIRO[PIPERIDIN-4,1'(2'H)-PIRROLO[3,4-c]PIRROL], (3'aRS,6'aSR)-1-CICLODECIL-5'-METIL-2'-FENIL-HEXAHIDRO-ESPIRO[PIPERIDIN-4,1'(2'H)-PIRROLO[3.4-c]PIRROL]-4',6'-DIONA, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. EL COMPUESTO I ES UN AGONISTA/ANTAGONISTA DEL RECEPTOR DE LA ORFANINA OFQ POR LO QUE PUEDE SER UTIL EN EL TRATAMIENTO DE TRASTORNOS PSIQUIATRICOS, NEUROLOGICOS Y FISIOLOGICOS COMO TRASTORNOS DE LA ANSIEDAD, ESTRES, DEPRESION, TRAUMAS, PERDIDA DE MEMORIA DEBIDA A LA ENFERMEDAD DE ALZHEIMER, EPILEPSIA, CONVULSIONES

公开(公告)号：PL333694A1

公开(公告)日：1999-12-20

申请号：PL33369499

申请日：1999-06-11

Applicant: HOFFMANN LA ROCHE

Inventor： ADAM GEO ,  DAUTZENBERG FRANK ,  KOLCZEWSKI SABINE ,  ROEVER STEPHAN ,  WICHMANN JUERGEN

IPC: C07D401/14 ,  A01N43/42 ,  A61K31/00 ,  A61K31/395 ,  A61K31/435 ,  A61K31/438 ,  A61K31/44 ,  A61K31/445 ,  A61K31/505 ,  A61K31/535 ,  A61P3/04 ,  A61P3/12 ,  A61P9/12 ,  A61P25/04 ,  A61P25/08 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  C07D20060101 ,  C07D209/00 ,  C07D221/00 ,  C07D471/10 ,  C07D471/20 ,  C07D487/20 ,  C07D498/10 ,  C07D513/10

Abstract: The present invention relates to compounds of the general formula wherein the substituents are described in the application and to pharmaceutically acceptable acid addition salts thereof. The compound of the invention are useful in the treatment of diseases related to the orphanin FQ (OFQ) receptor, which include psychiatric, neurological and physiological disorders, such as anxiety and stress disorders, depression, trauma, memory loss due to Alzheimer's disease or other dementias, deficits in cognition and leaning, epilepsy and convulsions, acute and/or chronic pain conditions, and symptoms of addictive drug withdrawal, control of water balance, Na excretion, arterial blood pressure disorders and metabolic disorders such as obesity.

公开(公告)号：ZA200301719B

公开(公告)日：2004-06-22

申请号：ZA200301719

申请日：2003-02-28

Applicant: HOFFMANN LA ROCHE

Inventor： BREU VOLKER ,  DAUTZENBERG FRANK ,  GUERRY PHILIPPE ,  NETTEKOVEN MATTHIAS-HEINRICH ,  PFLIEGER PHILIPPE

IPC: C07D239/94 ,  A61K31/365 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/00 ,  A61P1/14 ,  A61P3/00 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P13/12 ,  A61P19/02 ,  A61P43/00 ,  C07D215/00 ,  C07D215/42 ,  C07D239/84 ,  C07D401/04 ,  C07D409/04 ,  C07D ,  A61P ,  A61K

Abstract: Quinoline and quinazoline derivatives can be used in the form of pharmaceutical preparations as Neuropeptide Y antagonists for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.

公开(公告)号：PA8531701A1

公开(公告)日：2003-06-30

申请号：PA8531701

申请日：2001-11-07

Applicant: HOFFMANN LA ROCHE

Inventor： MATTEI PATRIZIO ,  BREU VOLKER ,  NEIDHART WENER ,  PFLIEGER PHILIPPE ,  DAUTZENBERG FRANK

IPC: A61K31/337 ,  A61K31/505 ,  A61K31/506 ,  A61P3/04 ,  A61P3/10 ,  A61P19/02 ,  A61P43/00 ,  C07D239/42 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06

Abstract: COMPUESTOS DE LA FORMULA I ASI COMO LOS ESTRES Y LAS SALES FARMACEUTICAMENTE UTILIZABLES DE LOS MISMOS, EN DONDE R1, R2, R3, R4, A1 Y A2 TIENEN EL SIGNIFICADO DADO EN LA REIVINDICACION 1, QUE SE PUEDEN USAR EN FORMA DE PREPARACION FARMACEUTICAS PARA EL TRATAMIENTO O PREVENCION DE ARTRITIS, DIABETES, TRASTORNOS ALIMENTARIOS Y OBESIDAD.

公开(公告)号：PA8528401A1

公开(公告)日：2002-09-30

申请号：PA8528401

申请日：2001-09-04

Applicant: HOFFMANN LA ROCHE

Inventor： BREU VOLKER ,  DAUTZENBERG FRANK ,  GUERRY PHILIPPE ,  NETTEKOVEN MATTHIAS HEINRICH ,  PFLIEGER PHILIPPE

IPC: C07D239/94 ,  A61K31/365 ,  A61K31/4706 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/00 ,  A61P1/14 ,  A61P3/00 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P13/12 ,  A61P19/02 ,  A61P43/00 ,  C07D215/00 ,  C07D215/42 ,  C07D239/84 ,  C07D401/04 ,  C07D409/04 ,  C07D329/84

Abstract: LOS COMPUESTOS DE FORMULA 1 ASI COMO LAS SALES UTILIZABLES FARMACEUTICAMENTE, SOLVATOS Y ESTERES DEL MISMO EN DONDE R1, R2, R3, R4, A1 Y A2 TIENEN EL SIGNIFICADO DADO EN LA REIVINDICACION 1, SE PUEDEN USAR EN FORMA DE PREPARACIONES FARMACEUTICAS PARA EL TRATAMIENTO O PREVENCION DE ARTRITIS, ENFERMEDADES CARDIOVASCULARES, DIABETES, INSUFICIENCIA RENAL, TRASTORNOS ALIMENTARIOS Y OBESIDAD.

公开(公告)号：ZA993853B

公开(公告)日：1999-12-13

申请号：ZA993853

申请日：1999-06-08

Applicant: HOFFMANN LA ROCHE

Inventor： ADAM GEO ,  DAUTZENBERG FRANK ,  ROEVER STEPHAN ,  WICHMANN JUERGEN ,  KOLCZEWSKI SABINE

IPC: A61K20060101 ,  A61K31/00 ,  C07D401/04 ,  A61K31/395 ,  A61K31/40 ,  A61K31/435 ,  A61K31/438 ,  A61K31/44 ,  A61K31/445 ,  A61P3/04 ,  A61P3/12 ,  A61P9/00 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/08 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/36 ,  A61P43/00 ,  C07D20060101 ,  C07D207/00 ,  C07D209/00 ,  C07D211/00 ,  C07D221/00 ,  C07D271/00 ,  C07D277/00 ,  C07D401/00 ,  C07D401/14 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/10 ,  C07D471/20 ,  C07D487/12 ,  C07D498/10 ,  C07D513/10 ,  C07D ,  A61K

Abstract: The present invention relates to compounds of the general formula wherein R is C6-10-cycloalkyl, optionally substituted by lower alkyl or -C(O)O-lower alkyl; decahydro-naphthalen-1-yl; decahydro-naphthalen-2-yl; indan-1-yl or indan-2-yl, optionally substituted by lower alkyl; decahydro-azulen-2-yl; bicycloÄ6.2.0Üdec-9-yl; acenaphthen-1-yl; 2,3-dihydro-1H-phenalen-1-yl; 2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl or octahydro-inden-2-yl; R is hydrogen; lower alkyl; =O or phenyl, optionally substituted by lower alkyl, halogen or alkoxy; A &cir& is cyclohexyl or phenyl, optionally substituted by lower alkyl, halogen or alkoxy; X is -CH(OH)-; -C(O)-; -CHR -; -CR =; -O-; -S-; -CH(COOR )- or - C(COOR )=; Y is -CH2-; -CH=; -CH(COOR )-, -C(COOR )=; or -C(CN)-; R is hydrogen or lower alkoxy; R is lower alkyl, cycloalkyl, phenyl, or benzyl and either a or b is optionally an additional bond, and to pharmaceutically acceptable acid addition salts thereof. The compounds are agonists and/or antagonists of the orphanin FQ (QFQ) receptor and therefore useful in the treatment of diseases, related to this receptor.

公开(公告)号：NO992872L

公开(公告)日：1999-12-13

申请号：NO992872

申请日：1999-06-11

Applicant: HOFFMANN LA ROCHE

Inventor： ADAM GEO ,  DAUTZENBERG FRANK ,  KOLCZEWSKI SABINE ,  ROEVER STEPHAN ,  WICHMANN JUERGEN

IPC: C07D401/14 ,  A01N43/42 ,  A61K31/00 ,  A61K31/395 ,  A61K31/435 ,  A61K31/438 ,  A61K31/44 ,  A61K31/445 ,  A61K31/505 ,  A61K31/535 ,  A61P3/04 ,  A61P3/12 ,  A61P9/12 ,  A61P25/04 ,  A61P25/08 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  C07D20060101 ,  C07D209/00 ,  C07D221/00 ,  C07D471/10 ,  C07D471/20 ,  C07D487/20 ,  C07D498/10 ,  C07D513/10

Abstract: The present invention relates to compounds of the general formula wherein the substituents are described in the application and to pharmaceutically acceptable acid addition salts thereof. The compound of the invention are useful in the treatment of diseases related to the orphanin FQ (OFQ) receptor, which include psychiatric, neurological and physiological disorders, such as anxiety and stress disorders, depression, trauma, memory loss due to Alzheimer's disease or other dementias, deficits in cognition and leaning, epilepsy and convulsions, acute and/or chronic pain conditions, and symptoms of addictive drug withdrawal, control of water balance, Na excretion, arterial blood pressure disorders and metabolic disorders such as obesity.