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    PROCESS PREPARING FOR PYROLIDINE DERIVATIVES
    1.
    发明授权
    PROCESS PREPARING FOR PYROLIDINE DERIVATIVES 失效

    公开(公告)号：KR800001279B1

    公开(公告)日：1980-10-26

    申请号：KR760000422

    申请日：1976-02-20

    Applicant: HOFFMANN LA ROCHE

    Inventor： BERNAUER K ,  SCHNEIDER F ,  PFOERTNER K

    IPC: C07D207/10

    Abstract: Analgesic pyrrolidine derivs. (I; R1 = pyridy1; R2 = H, lower alky1; R3 = H, lower alky1, benzy1; R4 = halogen, lower alcohol, lower alkoxy, nitro, and amino-substituted pheny1) were prepd. by the redn. of pyrrolines II. Thus, 4-methy1-4-nitro-3-(4-pytidy1)-valerophenon was reduced by Zn in CH3COOH followed by treating with 1n-HC1 and crystallizing with EtOH/(CH3)2CO gave trans-4-(2,2-dimethy1-5-pheny1-pyrolidy1)-pyridine dihydrochloride. I are useful as non-addictive analgesic agent, 3.0g., racemic 4-(cis-2,2-dimethy1-5-pheny1-3-pyrrolidiny1)-pyridine dihydrochloride had ED50 47mg/kg.

    PRCESS FOR PYROLIDINES
    2.
    发明授权
    PRCESS FOR PYROLIDINES 失效

    公开(公告)号：KR800001143B1

    公开(公告)日：1980-10-14

    申请号：KR770001711

    申请日：1977-07-25

    Applicant: HOFFMANN LA ROCHE

    Inventor： BERNAUER K ,  SCHNEIDER F ,  WERTNER K ,  SCHMITT H

    IPC: C07D207/09

    Abstract: Title compds. (I; R1 = 2-thienyl or phenyl substuted with lower t-amino group, R2 and R3 are independently, H or lower alkyl; R4 = halogen, lower alkyl, lower alkoxy, nitro, phenyl), useful as anaesthetics, were prepd. by reduction of compd. II in the presence of catalyst. Thus, 17 g 2-(P-methoxy-phenyl)-5, 5-dimethyl-4-(2-thienyl)-1-pyrroline and 10 g sodium borohydride were reacted in 250 ml anhydrous ethanol gor 6 hr with N2 gas to give cis-5-(p-methoxyphenyl)-2, 2-dimethyl-3-(2-thienyl)-pyrrolidine hydrochloric acid salt (m.p. 180oC).

    OXETANONE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS
    3.
    发明专利
    OXETANONE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS 未知

    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. -

    4.
    发明专利
    未知

    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. -

    5.
    发明专利
    未知

    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. -

    7.
    发明专利
    未知

    公开(公告)号：SE421694B

    公开(公告)日：1982-01-25

    申请号：SE7602069

    申请日：1976-02-20

    Applicant: HOFFMANN LA ROCHE

    Inventor： BERNAUER K ,  PFOERTNER K ,  SCHNEIDER F ,  SCHMID H

    IPC: C07D213/50 ,  C07D401/04

    Abstract: Compounds represented by the formula +q,10 WHEREIN R1 is a pyridyl, R2 is hydrogen or lower alkyl, R3 is hydrogen, lower alkyl or benzyl and R4 is phenyl or phenyl substituted at one or more carbon atoms with one or more of halogen, lower alkyl, lower alkoxy, nitro or amino AND PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF, HAVING ANALGESIC ACTIVITY ARE DISCLOSED.

    9.
    发明专利
    未知

    公开(公告)号：NO760561L

    公开(公告)日：1976-08-24

    申请号：NO760561

    申请日：1976-02-20

    Applicant: HOFFMANN LA ROCHE

    Inventor： BERNAUER K ,  PFOERTNER K ,  SCHNEIDER F ,  SCHMID H

    IPC: C07D213/50 ,  C07D401/04 ,  C07D

    Abstract: Compounds represented by the formula +q,10 WHEREIN R1 is a pyridyl, R2 is hydrogen or lower alkyl, R3 is hydrogen, lower alkyl or benzyl and R4 is phenyl or phenyl substituted at one or more carbon atoms with one or more of halogen, lower alkyl, lower alkoxy, nitro or amino AND PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF, HAVING ANALGESIC ACTIVITY ARE DISCLOSED.

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