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

    公开(公告)号：KR810000807B1

    公开(公告)日：1981-07-08

    申请号：KR780001679

    申请日：1978-06-02

    Applicant: HOFFMANN LA ROCHE

    Inventor： REINER R ,  MONTAVON M

    IPC: C07D501/36

    Abstract: Title compds. (I; R = furyl, thienyl, Ph; R' = lower alkyl, aminocarbonylmethyl; X = (a), (b), (c); R2, R3, R4 and R5 are H, lower alkyl, carboxymethyl or sulfomethyl), useful as bactericides, were prepd. by the reaction of II and III, or IV(Y = leaving group) and V. Thus, 5.06 g 2-methoxyimino-2-furyl-acetic acid reacted with oxalic chloride in the presence of DMF and Et3N, followed by the addn. of (7R)-7-amino-3-desacetoxy-3-[(1,2,5,6-tetrahydro-2-methyl-5,6-dioxo-as-triazin-3-yl)thio cephalosporanic acid in NaOH soln. to give I.

    PROCESS FOR PREPARING NORBORNANE DERIVATIVES
    2.
    发明授权
    PROCESS FOR PREPARING NORBORNANE DERIVATIVES 失效

    公开(公告)号：KR790001896B1

    公开(公告)日：1979-12-27

    申请号：KR750000597

    申请日：1975-03-20

    Applicant: HOFFMANN LA ROCHE

    Inventor： BRETSCHNEIDER H ,  BORGULYA J ,  BERMAUER K ,  MONTAVON M

    IPC: C07C87/40

    Abstract: Norbornane derivs. (I; R1,R2 = H, lower alkyl, lower alkenyl ; R3 = H, Me) and their acid addition salts were prepd., used as anticataleptics, e.g. in the treatment of parkinsonism, and useful as antidepressants and virucides. Thus, the protecting groups of compds. II or their salts, were isolated by solvolysis or reduction, and followed by loweralkylation or alkenylation to give I.

    ACYL DERIVATIVES AND THEIR PREPARATION
    3.
    发明授权
    ACYL DERIVATIVES AND THEIR PREPARATION 失效

    公开(公告)号：KR790001023B1

    公开(公告)日：1979-08-20

    申请号：KR750001368

    申请日：1975-06-20

    Applicant: HOFFMANN LA ROCHE

    Inventor： MONTAVON M ,  REINER R

    Abstract: Acyl cephalosporin derivs. (I, X = acetoxycephalosporinyl; Y = N-substituted 6-membered heterocyclic group) were manufd. by reacting II (X' = deactoxy-cephalosporinyl group contg. protected 4-carboxyl group; W' = free atom or group) with III, or by reacting IV (X'' = deacetoxy-cephalosporinyl group contg. protected 4-carboxyl group) with acids or their reactive derivs. of V (Z = acyl group being thought as substituent of amino acid in cephalosporin), and followed by isolating the protecting group to give I.

    ACRIDANONE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS
    5.
    发明专利
    ACRIDANONE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS 未知

    公开(公告)号：NZ206317A

    公开(公告)日：1987-06-30

    申请号：NZ20631783

    申请日：1983-11-18

    Applicant: HOFFMANN LA ROCHE

    Inventor： BROMBACHER U ,  LINK H ,  MONTAVON M

    IPC: A61K31/00 ,  A61K31/435 ,  A61P33/10 ,  C07D219/06 ,  C07D219/10 ,  C07D417/12 ,  C07D417/14 ,  C07D219/00 ,  C07D277/00 ,  C07D417/00 ,  A61K31/645

    Abstract: For the Contracting States BE CH DE FR GB IT LI LU NL SE 1. Acridanone derivatives of the general formula see diagramm : EP0110298,P20,F1 wherein the dotted line signifies an optional bond, R**1 signifies hydrogen, halogen or nitro, R**2 signifies hydrogen or lower alkyl, one of the symbols R**3 and R**4 signifies hydrogen or lower alkyl and the other together with R signifies an additional bond, A signifies lower alkylene, R**5 signifies a 5-membered, nitrogen-containig, optionally lower alkyl-substituted aromatic heterocycle, amino or a group see diagramm : EP0110298,P20,F2 or see diagramm : EP0110298,P20,F3 the symbol see diagramm : EP0110298,P20,F4 signifies a 5- or 6-membered, optionally lower-alkyl substituted saturated heterocycle which can contain as a ring member an oxygen or sulphur atom or the group >NH ou >N(B)n -A**1-R**6, B signifies the group -CO-, -COO- or -SO2 -, n signifies the number 0 or 1, A**1 signifies lower alkylene, R**6 signifies hydrogen, amino, lower alkylamino or di(lower alkyl)amino and R**7 signifies hydrogen or lower alkyl, and the residues denoted as lower contain 1 to 7 carbon atoms, and pharmaceutically acceptable acid addition salts thereof. For the Contracting State AT 1. A process for the manufacture of acridanone derivatives of the general formula see diagramm : EP0110298,P22,F1 wherein the dotted line signifies an optional bond, R**1 signifies hydrogen, halogen or nitro, R**2 signifies hydrogen or lower alkyl, one of the symbols R**3 and R**4 signifies hydrogen or lower alkyl and the other together with R signifies an additional bond, A signifies lower alkylene, R**5 signifies a 5-membered, nitrogen-containing, optionally lower alkyl-substituted aromatic heterocycle, amino or a group see diagramm : EP0110298,P23,F2 or see diagramm : EP0110298,P23,F3 the symbol see diagramm : EP0110298,P23,F4 signifies a 5- or 6-membered, optionally lower-alkyl substituted saturated heterocycle which can contain as a ring member an oxygen or sulphur atom or the group >NH ou >N(B)n -A**1-R**6, B signifies the group -CO-, -COO- or -SO2 -, n signifies the number 0 or 1, A**1 signifies lower alkylene, R**6 signifies hydrogen, amino, lower alkylamino or di(lower alkyl)amino and R**7 signifies hydrogen or lower alkyl, and the residues denoted as lower contains 1 to 7 carbon atoms, and pharmaceutically acceptable acid addition salts thereof, characterized by a) cyclizing a compound of the general formula see diagramm : EP0110298,P23,F5 wherein one of the symbols R**31 and R**41 signifies hydrogen or lower alkyl and the other signifies hydrogen, R**42 signifies hydrogen or lower alkyl, R**51 signifies a residue R**5, but does not contain a primary or secondary basic amino group, and X' signifies a leaving group, and R**1, R**2 and R**5 have the above significance, b) reacting a compound of the general formula see diagramm : EP0110298,P23,F6 wherein A, R**1, R**42 and R**51 have the above significance, with a compound of the general formula see diagramm : EP0110298,P23,F7 wherein X" signifies a leaving group and the dotted line and R**2 have the above significance, or c) reacting a compound of the general formula see diagramm : EP0110298,P23,F8 wherein Y(anion) signifies an anion and X signifies a leaving group, and A, R**1 and R**51 have the above significance, with a compound of the general formula see diagramm : EP0110298,P23,F9 wherein the dotted line, R, R**2, R**3 and R**4 have the above significance, or d) cleaving off the N-protecting group in a compound of the general formula see diagramm : EP0110298,P24,F10 wherein R**8 signifies a residue R**5 which contains a primary or secondary basic amino group blocked by a N-protecting group and the dotted line, R, R**1, R**2, R**3 and R**4 have the above significance, and e) if desired, converting a compound of formula I obtained into a pharmaceutically acceptable acid addition salt.

    MANUFACTURE OF CEPHALOSPORINS INTERMEDIATES
    9.
    发明专利
    MANUFACTURE OF CEPHALOSPORINS INTERMEDIATES 未知

    公开(公告)号：NZ195547A

    公开(公告)日：1983-05-10

    申请号：NZ19554780

    申请日：1980-11-14

    Applicant: HOFFMANN LA ROCHE

    Inventor： MONTAVON M ,  REINER R

    IPC: C07D501/00 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07C20060101 ,  C07D20060101 ,  C07D501/04 ,  C07D501/16 ,  C07D501/36 ,  C07D501/46

    Abstract: For the Contracting States : BE, CH, DE, FR, GB, IT, LI, LU, NL, SE 1. A process for the manufacture of acyl derivatives of general formula I see diagramm : EP0030294,P12,F1 in which R represents hydrogen or a readily hydrolyzable ester group, as well as of salts of these compounds and hydrates of these compounds or of their salts by reating a halide of general formula II see diagramm : EP0030294,P12,F2 in which R has the significance given above and Y represents a halogen atom, or a salt of this compound with thiourea and, if desired, converting a compound of formula I obtained into a salt or hydrate or into a hydrate of this salt, characterized in that X signifies one of the groups see diagramm : EP0030294,P13,F3 in which R' represents hydrogen or a readily hydrolysable ether group.

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