公开(公告)号：JPH10212290A

公开(公告)日：1998-08-11

申请号：JP1371198

申请日：1998-01-27

Applicant: HOFFMANN LA ROCHE

Inventor： ADAM GEO ,  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

Abstract: PROBLEM TO BE SOLVED: To obtain the subject new compound which is an agonist for OFQ receptor and/or an antagonist useful for treating mental disturbance, nervous disturbance and physiological disorder. SOLUTION: This compound is shown by formula I (R and R are each H, a lower alkyl, etc.; R is phenyl; R is H, a lower alkyl, an acyl, etc.; R and R are each H, a lower alkyl, etc., or bonded together to form a phenyl ring; R and one of R and R can be bonded to form a 6-memered ring; A is a saturated 4- to 7-membered ring containing a hetero atom such as O or S) or its acid addition salt such as 8-(8-chloro-1,2,3,4,-tetrahydro-naphthyl-2)-1- phenyl-1,3,8-triaza-spiro[4,5]decan-4-one. The compound of formula I is obtained by hydrogenating a double bond in a compound of formula II (A' is a 5 to 7-membered ring containing a hetero atom such as O or S). The compound is useful for treating anxiety, stress disorder, depression, traumatic disorder, amnesia caused by Alzheimer's disease or other dementia, epilepsy and convulsion.

公开(公告)号：JPH1068724A

公开(公告)日：1998-03-10

申请号：JP15117397

申请日：1997-06-09

Applicant: HOFFMANN LA ROCHE

Inventor： CIVELLI OLIVIER ,  MARTIN JAMES RICHARD ,  MONSMA FREDERICK ,  MOREAU JEAN-LUC ,  NOTHACKER HANS-PETER ,  REINSCHEID RAINER

IPC: G01N33/53 ,  A61K38/00 ,  A61K38/10 ,  A61P25/08 ,  A61P25/20 ,  A61P25/26 ,  G01N33/15 ,  G01N33/566 ,  G01N33/94

Abstract: PROBLEM TO BE SOLVED: To verify activity related to treatment by bringing LC 132 receptor in contact with a compound supposed to be agonist of the receptor and detecting the bonding of the compound with LC 132 receptor and/or agonist activity. SOLUTION: An LC 132 receptor is brought in contact and react with a compound which bonds with an LC 132 (opioid like) orphan receptor and is supposed to have the LC 132 receptor agonist function thereby adjusting the function of the LC 132 receptor. Then, it is labeled and laid on the compound so that the bonding of the LC 132 receptor is detected. The agonist activity is measured by an inhibition degree of cAMP cumulation caused by false choline stimulus in a host cell which is transfected by a vector expressing the LC 132 receptor. Next, the agonist activity is tested by a screening assay of psychiatric and/or neurological disorder.

公开(公告)号：EP0813065A3

公开(公告)日：1998-07-22

申请号：EP97109078

申请日：1997-06-05

Applicant: HOFFMANN LA ROCHE

Inventor： CIVELLI OLIVIER ,  MARTIN JAMES RICHARD ,  MONSMA FREDERICK ,  MOREAU JEAN-LUC ,  NOTHACKER HANS-PETER ,  REINSCHEID RAINER

IPC: G01N33/94 ,  G01N33/566 ,  A61K38/10

CPC classification number: G01N33/9486 ,  G01N2500/00

Abstract: The present invention relates to a method of screening for a therapeutically useful compound which comprises testing an LC132 receptor agonist in a screening assay for psychiatric and/or neurological disorders. More particularly, the screening method is based on contacting an LC132 receptor with an agent suspected of being an agonist of the LC132 receptor function, followed by the detection of the binding and/or the agonist activity of the compound and then testing of an agent with LC132 agonist activity in an antiepileptic, anticonvulsant or anxiolytic screening assay.

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：GR3036523T3

公开(公告)日：2001-12-31

申请号：GR20010401383

申请日：2001-09-05

Applicant: HOFFMANN LA ROCHE

Inventor： ADAM GEO ,  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：DE69800896D1

公开(公告)日：2001-07-19

申请号：DE69800896

申请日：1998-01-21

Applicant: HOFFMANN LA ROCHE

Inventor： ADAM GEO ,  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：AU5280998A

公开(公告)日：1998-08-06

申请号：AU5280998

申请日：1998-01-29

Applicant: HOFFMANN LA ROCHE

Inventor： ADAM GEO ,  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 ,  A61K31/395

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：NO980332A

公开(公告)日：1998-07-31

申请号：NO980332

申请日：1998-01-26

Applicant: HOFFMANN LA ROCHE

Inventor： ADAM GEO ,  CESURA ANDREA ,  GALLEY GUIDO ,  JENCK FRANÇOIS ,  MONSMA FREDERICK ,  ROEVER STEPHAN ,  WICKMANN 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 ,  C07D471/20 ,  A61K31/395

CPC classification number: C07D471/10

公开(公告)号：PL320527A1

公开(公告)日：1997-12-22

申请号：PL32052797

申请日：1997-06-12

Applicant: HOFFMANN LA ROCHE

Inventor： CIVELLI OLIVIER ,  MARTIN JAMES RICHARD ,  MONSMA FREDERICK ,  MOREAU JEAN-LUC ,  NOTHACKER HANS-PETER ,  REINSCHEID RAINER

IPC: G01N33/53 ,  A61K38/00 ,  A61K38/10 ,  A61P25/08 ,  A61P25/20 ,  A61P25/26 ,  G01N33/15 ,  G01N33/566 ,  G01N33/94

Abstract: The present invention relates to a method of screening for a therapeutically useful compound which comprises testing an LC132 receptor agonist in a screening assay for psychiatric and/or neurological disorders. More particularly, the screening method is based on contacting an LC132 receptor with an agent suspected of being an agonist of the LC132 receptor function, followed by the detection of the binding and/or the agonist activity of the compound and then testing of an agent with LC132 agonist activity in an antiepileptic, anticonvulsant or anxiolytic screening assay.

公开(公告)号：NO972707L

公开(公告)日：1997-12-15

申请号：NO972707

申请日：1997-06-12

Applicant: HOFFMANN LA ROCHE

Inventor： CIVELLI OLIVIER ,  MARTIN JAMES RICHARD ,  MONSMA FREDERICK ,  MOREAU JEAN-LUC ,  NOTHACKER HANS-PETER ,  REINSCHEID RAINER

IPC: G01N33/53 ,  A61K38/00 ,  A61K38/10 ,  A61P25/08 ,  A61P25/20 ,  A61P25/26 ,  G01N33/15 ,  G01N33/566 ,  G01N33/94 ,  G01N33/68

Abstract: The present invention relates to a method of screening for a therapeutically useful compound which comprises testing an LC132 receptor agonist in a screening assay for psychiatric and/or neurological disorders. More particularly, the screening method is based on contacting an LC132 receptor with an agent suspected of being an agonist of the LC132 receptor function, followed by the detection of the binding and/or the agonist activity of the compound and then testing of an agent with LC132 agonist activity in an antiepileptic, anticonvulsant or anxiolytic screening assay.