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    ACRIDANONE DERIVATIVES
    2.
    发明专利
    ACRIDANONE DERIVATIVES 未知

    公开(公告)号：ZW23783A1

    公开(公告)日：1985-05-22

    申请号：ZW23783

    申请日：1983-11-02

    Applicant: HOFFMANN LA ROCHE

    Inventor： URS BROMBACHER ,  HELMUT LINK ,  MARC MONTAVON

    IPC: A61K31/00 ,  A61K31/435 ,  A61P33/10 ,  C07D219/06 ,  C07D219/10 ,  C07D417/12 ,  C07D417/14 ,  A61K ,  C07D

    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.

    CEPHALOSPORIN DERIVATIVES
    4.
    发明专利
    CEPHALOSPORIN DERIVATIVES 未知

    公开(公告)号：AU2856692A

    公开(公告)日：1993-05-27

    申请号：AU2856692

    申请日：1992-11-20

    Applicant: HOFFMANN LA ROCHE

    Inventor： PETER ANGEHRN ,  ANDRE FURLENMEIER ,  PAUL HEBEISEN ,  WERNER HOFHEINZ ,  HELMUT LINK

    IPC: A61K31/545 ,  A61K20060101 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D501/00 ,  C07D501/18 ,  C07D501/20 ,  C07D501/34 ,  C07D501/36 ,  C07D519/00 ,  C07D519/06

    Abstract: Cephalosporin derivatives of the general formula in which Z and Z each individually denotes a 6-membered aromatic ring substituted by two vicinal groups -OR (in which R represents hydrogen or lower alkanoyl), which additionally contain 1 or 2 O or N atoms and/or can be substituted by halogen, carboxyl or carboxy-lower alkyl, or -X-Z and -(Q)p-Z each individually denotes a group -X -CONR OH or -(Q )p-CONR OH, in which R represents hydrogen, lower alkyl or phenyl; and in which additionally A represents a nitrogen atom or a methine group (-CH=), X represents lower alkylenephenylene, phenylene or lower alkylene which is optionally substituted by carboxyl and optionally linked to one of the groups -S-, -SO-, -SO2-, -CO-, -OCO-, -NHCO-, -NHSO2- and -CONHNHCO-, X represents lower alkylene, phenylene or lower alkylenephenylene, Y represents one of the groups -O-, -OCO-, -OCH2-, -S-, -SCO-, -SO- and -SO2-, P represents a 5- or 6- membered N-monoheterocycle which is optionally substituted by lower alkyl, phenyl, hydroxyl or oxo, or an 8- to 10-membered N-biheterocycle which is optionally substituted by lower alkyl, carboxyl, lower alkoxycarbonyl, carbamoyl, hydroxymethyl or lower alkanoyloxymethyl, Q represents lower alkylenephenylene, phenylene or lower alkylene which is optionally linked to one of the groups -CO-, -OCO-, -SO2-, -NHCO- and -NHSO2-, or one of the groups -S-, -SO-, -SO2-, -CO-, -OCO-, -NHCO-, -NHSO2- and -CONHNHCO-, Q represents lower alkylene, phenylene or lower alkylenephenylene and m, n and p in each case represent the number 0 or 1; and also easily hydrolysable esters and pharmaceutically tolerable salts of these compounds and hydrates of compounds of the formula I or of their esters and salts as well as a process for their preparation and pharmaceutical preparations which contain these compounds, and also intermediates for the preparation of these compounds, and further the use of the compounds in the control of diseases and in the production of the preparations mentioned.

    6.
    发明专利
    未知

    公开(公告)号：MC1920A1

    公开(公告)日：1989-04-06

    申请号：MC1967

    申请日：1988-04-07

    Applicant: HOFFMANN LA ROCHE

    Inventor： ANDRE FURLENMEIER ,  ERWIN GOETSCHI ,  PAUL HEBEISEN ,  WERNER HOFHEINZ ,  HELMUT LINK

    IPC: C07D519/06 ,  A61K31/545 ,  A61P31/04 ,  C07D501/36 ,  C07D501/46 ,  C07D519/00 ,  C07D ,  A61K

    Abstract: Acyl derivatives of the formula I in which R is an acyl group, excluding those acyl groups of the formula in which A is a group of the formulae -NHCO-, -NHCONHCO-, -NHCOCH=CH-, wherein R6 is hydrogen or lower alkyl; R1 and R2 are hydrogen or a protecting group, X is hydrogen, halogen, lower alkoxy, nitro or -OR2, n is 1 or 2, R4 and R5 are hydrogen or together represent an additional bond and Z is a direct bond or carbonyl (where R4 and R5 both represent hydrogen) or a group of the formula -O-B- (where R4 and R5 together represent an additional bond) in which B is a straight-chain, branched or cyclic lower alkylene; and wherein R3 is a substituted bicyclic group of the formulae 7 5 NR7NNN+RE wherein R7 and R8 are independently hydrogen, lower alkyl or trifluoromethyl or, in formulae (a), (b), (e) and (f) together represent alkylene with 3 or 4 carbon atoms, and R', R'' and R''' are independently hydrogen, lower alkyl or lower cycloalkyl; wherein compounds of formula I in which R4 and R5 together represent an additional bond are present in the syn-isomeric form or as a mixture with the anti-isomeric form in which the syn-isomeric form predominates, as well as readily hydrolyzable esters and salts of these compounds and hydrates of the compounds of formula I or of their esters and salts. These compounds are useful as antibiotics.

    1,3-DISUBSTITUTED IMIDAZOLIUM SALTS
    7.
    发明专利
    1,3-DISUBSTITUTED IMIDAZOLIUM SALTS 未知

    公开(公告)号：ZW18087A1

    公开(公告)日：1988-05-18

    申请号：ZW18087

    申请日：1987-09-23

    Applicant: HOFFMANN LA ROCHE

    Inventor： HELMUT LINK

    IPC: A61K31/415 ,  A61P31/04 ,  A61P31/10 ,  A61P33/02 ,  A61P33/10 ,  C07D233/20 ,  C07D233/22 ,  C07D233/38 ,  C07D233/42 ,  C07D233/56 ,  C07D233/60 ,  C07D233/61 ,  C07D233/64 ,  C07D233/70 ,  C07D233/84 ,  C07D233/88 ,  C07D521/00 ,  A61K

    Abstract: The pharmaceutically acceptable salts corresponding to the imidazolium hydrogen carbonates of the formula I wherein the symbol Q is arylene or heteroarylene, the group -NR1R2 is a basic amino group, R3 is hydrogen, lower alkyl, lower hydroxyalkyl, lower alkoxyalkyl, lower haloalkyl, lower alkylthio, lower alkoxy or the group -(A)n-Ra, R4 is a saturated or partially unsaturated lower hydrocarbon group, a basic amino group or the group -N=CRc-Rb, -CHRcRd, -NH-CHRcRd, -NH-CO-Re or -CHRc-CO-Re, R5 is hydrogen, lower alkyl, lower hydroxyalkyl, lower alkoxyalkyl, lower haloalkyl, aryl or a fused benzene ring, R6 is hydrogen or lower alkyl, Ra and Rb each is aryl, heteroaryl or a basic amino group, Rc is hydrogen or lower alkyl, Rd is aryl or heteroaryl, Re is hydrogen, a saturated or partially unsaturated lower hydrocarbon group optionally attached via an oxygen atom or an aryl, heteroaryl or basic amino group optionally attached via a lower alkyl group, A is vinylene or lower alkylene, n is the integer 0 or 1 and the dotted line is an additional double bond, possess valuable antibacterial, antimycotic, protozoocidal and/or anthelmintic properties. The imidazolium bicarbonates of formula I can be used to prepare such pharmaceutically acceptable, especially water-soluble, salts in a simple and inexpensive manner.

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