公开(公告)号：YU108788A

公开(公告)日：1990-04-30

申请号：YU108788

申请日：1988-06-06

Applicant: HOFFMANN LA ROCHE

Inventor： WIDMER U

IPC: A61K31/495 ,  A61K31/50 ,  A61K31/5025 ,  A61P21/02 ,  A61P25/20 ,  A61P25/22 ,  C07D471/04 ,  C07D495/04 ,  C07D495/14

Abstract: The compounds of the formula A wherein Ra, Rb, Rc, Rd, Re and Rf are as hereinafter described, compounds of formula A which have one or more basic substituents are described and have valuable pharmacological properties. In particular, they have muscle relaxant, sedative-hypnotic, anxiolytic and/or anticonvulsive activity and can be used for the control or prevention of muscle tensions, stress conditions, insomnia, anxiety states and/or convulsions.

公开(公告)号：YU6792A

公开(公告)日：1994-11-15

申请号：YU6792

申请日：1992-01-23

Applicant: HOFFMANN LA ROCHE

Inventor： SCHERSCHLICHT R R ,  WIDMER U

IPC: A61K31/47 ,  A61K31/4025 ,  A61K31/435 ,  A61K31/4375 ,  A61P25/20 ,  C07D207/12 ,  C07D401/14 ,  C07D455/04 ,  C07D455/06 ,  C07D471/04

Abstract: TRICIKLIČNI DERIVAT PIRIDONA, jedinjenje (S)-1-((10-hlor-6,7-dihidro-4-okso-3-fenil-4H-benzo(a)hinolizin-1-il)karbonil) -3-etoksipirolidin formule I ima dragocene farmakološke osobine i može se primentiti za lečenje ili sprečavanje oboljenja. Ono ima naročito nesedativno, hipnotičko dejstvo, što znači dejstvo uredjivanja spavanja i prema tome se može primeniti za lečenje smetnji pri spavanju.

公开(公告)号：NZ214567A

公开(公告)日：1990-01-29

申请号：NZ21456785

申请日：1985-12-16

Applicant: HOFFMANN LA ROCHE

Inventor： BARBIER P ,  SCHNEIDER F ,  WIDMER U

IPC: C07D305/12 ,  C07D309/12 ,  C07D309/30 ,  C07F7/18

公开(公告)号：YU48221B

公开(公告)日：1997-08-22

申请号：YU6792

申请日：1992-01-23

Applicant: HOFFMANN LA ROCHE

Inventor： SCHERSCHLICHT R R ,  WIDMER U

IPC: A61K31/47 ,  A61K31/4025 ,  A61K31/435 ,  A61K31/4375 ,  A61P25/20 ,  C07D207/12 ,  C07D401/14 ,  C07D455/04 ,  C07D455/06 ,  C07D471/04

Abstract: Jedinjenje (S)-1-/(10-hlor-6,7-dihidro-4-okso-3-fenil-4H-benzo/a/hinolizin-1-il)karbonil/-3-etoksipirolidin ima drogocene farmakološke osobine i može se primeniti za lečenje ili sprečavanje oboljenja. Ono ima naročito nesedativno, hipnotičko dejstvo, što žnači dejstvo uređivanja spavanja i prema tome se može primeniti za lečenje smetnji pri spavanju.

公开(公告)号：NZ214565A

公开(公告)日：1989-06-28

申请号：NZ21456585

申请日：1985-12-16

Applicant: HOFFMANN LA ROCHE

Inventor： BARBIER P ,  SCHNEIDER F ,  WIDMER U

IPC: A61K31/335 ,  C07D305/12 ,  C07D309/12 ,  C07D309/30 ,  C07D407/12 ,  C07F7/18 ,  A61K31/40 ,  C07D207/08

Abstract: Oxetanones of formula (I) and their salts with weak acids are new: R1 and R2 = 1-17C alkyl (opt. having up to 8 double or triple bonds and opt. interrupted by an O or S atom which is not alpha to an unsatd. C atom), phenyl, benzyl or -C6H4-X-C6H5, all opt. ring-substd. by 1-3 1-6C alkyl, alkoxy or alkylthio; X = O, S or (CH2)m; m = 0-3; R3 = H or 1-3C alkyl or alkanoyl; R4 = H or 1-3C alkyl; R5 = H, Ar or Ar-(1-3C) alkyl or is 1-7C alkyl, opt. interrupted by Y and/or substd. by Z; or R4 and R5 together make a 4-6 membered satd. ring; Y = O, S, NR6, CONR6 or NR6.CO; Z = OR7, SR7, NR7R8, CONR7R8 or NR7.COR8; n = 0 or 1, and if 1 then R5 = H; Ar = phenyl, opt. substd. by up to 3 R9 or ORa; R6, R7, R8 and R9 = H or 1-3C alkyl. Where R3 = HCO and R5 = isobutyl, or R3 = MeCO and R5 = carbamoylethyl and also R2 = undecyl or 2,5-undecadienyl and R1 = n-hexyl, then R4 is not H. Also new are ethanol derivs. (III): when R1 = n -hexyl and R2 = undecyl or 2Z,5Z-undecadienyl, at least one asymmetric C atom in the ring or in beta-position to the ring has the R configuration. -

公开(公告)号：DK600385A

公开(公告)日：1986-06-22

申请号：DK600385

申请日：1985-12-20

Applicant: HOFFMANN LA ROCHE

Inventor： BARBIER P ,  SCHNEIDER F ,  WIDMER U

IPC: A61K31/335 ,  C07D305/12 ,  C07D309/12 ,  C07D309/30 ,  C07D407/12 ,  C07F7/18 ,  C07D

Abstract: Oxetanones of formula (I) and their salts with weak acids are new: R1 and R2 = 1-17C alkyl (opt. having up to 8 double or triple bonds and opt. interrupted by an O or S atom which is not alpha to an unsatd. C atom), phenyl, benzyl or -C6H4-X-C6H5, all opt. ring-substd. by 1-3 1-6C alkyl, alkoxy or alkylthio; X = O, S or (CH2)m; m = 0-3; R3 = H or 1-3C alkyl or alkanoyl; R4 = H or 1-3C alkyl; R5 = H, Ar or Ar-(1-3C) alkyl or is 1-7C alkyl, opt. interrupted by Y and/or substd. by Z; or R4 and R5 together make a 4-6 membered satd. ring; Y = O, S, NR6, CONR6 or NR6.CO; Z = OR7, SR7, NR7R8, CONR7R8 or NR7.COR8; n = 0 or 1, and if 1 then R5 = H; Ar = phenyl, opt. substd. by up to 3 R9 or ORa; R6, R7, R8 and R9 = H or 1-3C alkyl. Where R3 = HCO and R5 = isobutyl, or R3 = MeCO and R5 = carbamoylethyl and also R2 = undecyl or 2,5-undecadienyl and R1 = n-hexyl, then R4 is not H. Also new are ethanol derivs. (III): when R1 = n -hexyl and R2 = undecyl or 2Z,5Z-undecadienyl, at least one asymmetric C atom in the ring or in beta-position to the ring has the R configuration. -

公开(公告)号：DK600385D0

公开(公告)日：1985-12-20

申请号：DK600385

申请日：1985-12-20

Applicant: HOFFMANN LA ROCHE

Inventor： BARBIER P ,  SCHNEIDER F ,  WIDMER U

IPC: A61K31/335 ,  C07D305/12 ,  C07D309/12 ,  C07D309/30 ,  C07D407/12 ,  C07F7/18 ,  C07D

Abstract: Oxetanones of formula (I) and their salts with weak acids are new: R1 and R2 = 1-17C alkyl (opt. having up to 8 double or triple bonds and opt. interrupted by an O or S atom which is not alpha to an unsatd. C atom), phenyl, benzyl or -C6H4-X-C6H5, all opt. ring-substd. by 1-3 1-6C alkyl, alkoxy or alkylthio; X = O, S or (CH2)m; m = 0-3; R3 = H or 1-3C alkyl or alkanoyl; R4 = H or 1-3C alkyl; R5 = H, Ar or Ar-(1-3C) alkyl or is 1-7C alkyl, opt. interrupted by Y and/or substd. by Z; or R4 and R5 together make a 4-6 membered satd. ring; Y = O, S, NR6, CONR6 or NR6.CO; Z = OR7, SR7, NR7R8, CONR7R8 or NR7.COR8; n = 0 or 1, and if 1 then R5 = H; Ar = phenyl, opt. substd. by up to 3 R9 or ORa; R6, R7, R8 and R9 = H or 1-3C alkyl. Where R3 = HCO and R5 = isobutyl, or R3 = MeCO and R5 = carbamoylethyl and also R2 = undecyl or 2,5-undecadienyl and R1 = n-hexyl, then R4 is not H. Also new are ethanol derivs. (III): when R1 = n -hexyl and R2 = undecyl or 2Z,5Z-undecadienyl, at least one asymmetric C atom in the ring or in beta-position to the ring has the R configuration. -