公开(公告)号：MY176608A

公开(公告)日：2020-08-18

申请号：MYPI20030378

申请日：2003-02-05

Applicant: HOFFMANN LA ROCHE

Inventor： GEO ADAM ,  THOMAS JOHANNES WOLTERING ,  ERWIN GOETSCHI ,  JUERGEN WICHMANN

IPC: A61K31/5513 ,  A61P25/00 ,  A61P25/18 ,  A61P25/28 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10

Abstract: This invention relates to dihydro-benzo[b][l,4]diazepin-2-one derivatives of the general formula wherein R1, R2, X and Y are as defined in the specification and R3 is a six-membered aromatic heterocyde containing l to 3 nitrogen atoms or a pyridine-N-oxide as further defined in the specification. The invention further relates to medicaments containing these compounds, a process for their preparation as well as their use for preparation of medicaments for the treatment or prevention of acute and/or chronic neurological disorders.

公开(公告)号：MA26520A1

公开(公告)日：2004-12-20

申请号：MA25167

申请日：1998-07-14

Applicant: HOFFMANN LA ROCHE

Inventor： GEO ADAM ,  SABINE KOLCZEWSKI ,  VINCENT MUTEL ,  JURGEN WICHMANN ,  THOMAS JOHANNES WOLTERING

IPC: A61K31/00 ,  A61K31/505 ,  A61K31/519 ,  A61P1/08 ,  C07D239/22 ,  A61P9/00 ,  A61P13/02 ,  A61P15/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P25/30 ,  A61P27/02 ,  A61P43/00 ,  C07D239/00 ,  C07D239/40 ,  C07D277/00 ,  C07D513/04 ,  C07D239/70 ,  C07D277/60 ,  A61K31/425

公开(公告)号：HRP990189A2

公开(公告)日：2000-02-29

申请号：HRP990189

申请日：1999-06-11

Applicant: HOFFMANN LA ROCHE

Inventor： GEO ADAM ,  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：JO2285B1

公开(公告)日：2005-09-12

申请号：JOP20020032

申请日：2002-04-10

Applicant: HOFFMANN LA ROCHE

Inventor： MUTEL VINCENT ,  WICHMANN JUERGEN ,  GEO ADAM ,  ERWIN GOETSCHI ,  THOMAS JOHANNES WOLTERING

IPC: C07D243/12 ,  A61K31/551 ,  A61K31/5513 ,  A61P25/00 ,  A61P25/18 ,  A61P25/28 ,  A61P43/00 ,  C07D401/04 ,  C07D403/04 ,  C07D403/10 ,  C07D403/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14

Abstract: This invention is concerned with dihydro-benzo [b] [1,4] diazepin-2-one derivatives of the general formula: Wherein RI, R2, R3, X and Y are as defined in the specification. The invention further relates to med medicaments containing there compounds, a process for their preparations as well as their use for preparation of medicaments for the treatment for the treatment or prevention of acute and/or chronic neurological disorders

公开(公告)号：JO2273B1

公开(公告)日：2005-04-07

申请号：JOP20020033

申请日：2002-04-10

Applicant: HOFFMANN LA ROCHE

Inventor： MUTEL VINCENT ,  WICHMANN JUERGEN ,  GEO ADAM ,  ERWIN GOETSCHI ,  THOMAS JOHANNES WOLTERING

IPC: C07D243/28 ,  A61K31/5513 ,  A61P1/06 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/34 ,  A61P25/36 ,  A61P43/00 ,  C07D401/04 ,  C07D403/10 ,  C07D403/14 ,  C07D413/10 ,  C07D417/10

Abstract: This invention Is concerned with dihydro-benzo [b][1 .4] diazepin-2-one derivatives of the general formula . Wherein RI, R2, R3 and Y are as defined in the specification. The invention further relates to rnedlcaments containing these compounds, a process for their preparation as well as their use for preparation of medicaments for the treatment or prevention of acute and/or chronic neurological disorders

公开(公告)号：YU26202A

公开(公告)日：2004-12-31

申请号：YUP26202

申请日：2000-09-29

Applicant: HOFFMANN LA ROCHE

Inventor： GEO ADAM ,  ALANINE ALEXANDER ,  GOETSCHI ERWIN ,  MUTEL VINCENT ,  WOLTERING THOMAS JOHANNES

IPC: A61K31/55 ,  A61K31/551 ,  A61K31/5513 ,  A61P1/08 ,  A61P3/08 ,  A61P9/00 ,  A61P9/10 ,  A61P13/00 ,  A61P21/02 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/34 ,  A61P25/36 ,  A61P27/02 ,  A61P43/00 ,  C07D243/12 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D417/10 ,  C07D417/14 ,  C07D491/056 ,  C07D491/113 ,  C07F7/10

Abstract: Ovaj pronalazak se odnosi na jedinjenja opšte formule (I) gde je X jednostruka veza ili etinedil grupa, gde je, u slučaju da je X jednostruka veza, R1 je halogen ili fenil koji je proizvoljno supstituisan sa halogenom, nižim alkilom, halogen-nižim alkilom, nižim alkoksi, halogen-nižim alkoksi, ili sa cijano; u slučaju da je X etinedil grupa, R1 je fenil, proizvoljno supstituisan sa halogenom, nižim alkilom, halogen-nižim alkilom, nižim cikloalkilom, nižim alkoksi ili halogen-nižim alkoksi; R3 je 5 ili 6 člani aril ili heteroaril aril ili heteroaril koji su proizvoljno supstituisani. Jedinjenja prema ovom pronalasku se mogu koristiti za tretiranje ili prevenciju akutnih i/ili hroničnih neuroloških poremećaja kao što su psihoza, šizofrenija, Alchajmerova bolest, spoznajni poremećaji i gubici pamćenja.[The present invention relates to compounds of general formula (I) wherein X is a single bond or an ethynediyl group, wherein, in case X is a single bond, R1 is halogen or phenyl which is optionally substituted with halogen, lower alkyl, halo-lower alkyl, lower alkoxy, halo-lower alkoxy, or cyano; In case X is an ethynediyl group, R1 is phenyl, optionally substituted with halogen, lower alkyl, halo- lower alkyl, lower cycloalkyl, lower alkoxy or halo-lower alkoxy; R3 is a 5 or 6 membered aryl or heteroaryl which are optionally substituted. The compounds according to the present invention can be used for treating or preventing acute and/or chronic neurological disorders such as psychosis, schizophrenia, Alzheimer's disease, cognitive disorders and memory deficits.

公开(公告)号：YU26499A

公开(公告)日：2002-09-19

申请号：YU26499

申请日：1999-06-10

Applicant: HOFFMANN LA ROCHE

Inventor： GEO ADAM ,  ANDREA CESURA ,  FRANCOIS JENCK ,  SABINE KOLCZEWSKI ,  STEPHAN ROVER ,  JURGEN WICHMANN

IPC: C07D401/00 ,  A61K31/00 ,  A61K31/438 ,  A61P3/04 ,  A61P9/10 ,  A61P25/04 ,  A61P25/08 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  C07D471/10

Abstract: Ovaj pronalazak se odnosi na jedinjenja opste formule (I) u kojoj R1 je C6-C12-cikloalkil, proizvoljno supstituisan nizim alkilom ili C(O)O nizim alkilom, indan-1-il ili indan-2-il, proizvoljno supstituisan nizim alkilom; acenaften-1-il; biciklo[3.3.1] non-9-il, oktahidro-inden-2-il; 2,3-dihidro-1H-fenalen-1-il; 2,3,3a,4,5,6-heksahidro-1H-fenalen-1-il, dekahidro-azulen-2-il; biciklo[6.2.0] dek-9-il; dekahidronaftalen-1-il; dekahidro-naftalen-2-il; tetrahidro-naftalen-2-il, tetrahidro-naftalen-2-il ili 2-okso-1,2-difenil-etil; R2 je =O ili vodonik, R3 je vodonik, izoindolil-1,3-dion, nizi alkoksi, nizi alkil, amino, benziloksi, -CH2OR5 ili -CH2N(R5)2; R4 je vodonik ili -CH2OR5; R5 je vodonik ili nizi alkil; A je cikloheksil ili fenil, proizvoljno supstituisan nizim alkilom, halogenom ili alkoksijem, i na njihove farmaceutski prihvatljive kisele adicione soli. Jedinjenja ovog pronalaska su agonisti i/ili antagonisti orfamin FQ (OFQ) receptora i zato korisni u tretiranju bolesti, vezanih za ovaj receptor.

公开(公告)号：HRP980043B1

公开(公告)日：2001-12-31

申请号：HRP980043

申请日：1998-01-27

Applicant: HOFFMANN LA ROCHE

Inventor： GEO ADAM ,  CESURA ANDREA ,  GALLEY GUIDO ,  JENCK FRANCOIS ,  MONSMA FREDERICK ,  ROEVER STEPHAN ,  WICHMANN JUERGEN

IPC: C07D233/04 ,  A61K31/00 ,  A61K31/41 ,  A61K31/435 ,  A61K31/438 ,  A61K31/445 ,  A61K31/55 ,  A61K51/02 ,  A61P3/04 ,  A61P3/12 ,  A61P9/00 ,  A61P9/12 ,  A61P25/00 ,  A61P25/04 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  C07D215/58 ,  C07D305/14 ,  C07D471/00 ,  C07D471/10 ,  C07D498/00 ,  A61K31/44

Abstract: The present invention relates to compounds of the formula wherein R and R are, independently from each other, hydrogen, lower alkyl, lower alkoxy or halogen; R is phenyl, optionally substituted by lower alkyl,CF3, lower alkoxy or halogen; and R is hydrogen, lower alkyl, lower alkenyl, -C(O)-lower alkyl, -C(O)-phenyl, lower alkyl-C(O)-phenyl, lower alkylen-C(O)O-lower alkyl, lower alkantriyl-di-C(O)O-lower alkyl, hydroxy-lower alkyl, lower alkyl-O-lower alkyl, lower alkyl-CH(OH)CF3, phenyl or benzyl, R and R are, independently from each other, hydrogen, phenyl, lower alkyl or di-lower alkyl or may form together a phenyl ring, and R and one of R or R may form together a saturated or unsaturated 6 membered ring, A is a 4 - 7 membered saturated ring which may contain a heteroatom such as O or S, and to pharmaceutically acceptable acid addition salts thereof which are agonists and/or antagonists of the OFQ receptor.

公开(公告)号：TR9901304A3

公开(公告)日：2000-01-21

申请号：TR9901304

申请日：1999-06-10

Applicant: F. HOFFMANN-LA ROCHE AG

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

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 ,  C07D

CPC classification number: C07D471/20

公开(公告)号：JO2495B1

公开(公告)日：2009-10-05

申请号：JOP20030009

申请日：2003-02-02

Applicant: HOFFMANN LA ROCHE

Inventor： GEO ADAM ,  ERWIN GOETSCHI ,  JUERGEN WICHMANN ,  THOMAS JOHANNES WOLTERING

Abstract: The invention relates to dihydro-‎benzo[b][1,4] diazepin-2-one derivatives of ‎the general formula ‎ wherein R1, R2, X and Y are as defined in ‎the specification and R3 is a six-membered ‎aromatic heterocycle containing 1 to 3 ‎nitrogen atoms or a pyridine-N-oxide as ‎further defined in the specification. The ‎invention further relates to medicaments ‎containing these compounds, a process for ‎their preparation as well as their use for ‎preparation of medicaments for the ‎treatment or prevention of acute and/or ‎chronic neurological disorders.