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    20-hydrocarbyl-6-keto-steroids
    1.
    发明授权
    20-hydrocarbyl-6-keto-steroids 失效
    20-油酰六-KETO-STEROIDS

    公开(公告)号：US3835127A

    公开(公告)日：1974-09-10

    申请号：US70923968

    申请日：1968-02-29

    Applicant: HOFFMANN LA ROCHE

    Inventor： FURST A ,  FURLENMEIER A ,  WIECHERT R ,  HOCKS P ,  KERB U ,  LANGEMANN A ,  WALDVOGEL G

    IPC: C07J9/00 ,  C07C173/00

    CPC classification number: C07J9/00

    Abstract: This invention is directed to 2,3-substituted-20-hydrocarbyl 6keto-steroids which are useful as metamorphosis hormones and are additionally useful as intermediates for the production of other insect hormones. Accordingly, the compounds may be employed in the control of insect population.

    Abstract translation: 本发明涉及可用作变态激素的2,3-取代的20-烃基6-酮类固醇，并且还可用作生产其它昆虫激素的中间体。 因此，这些化合物可用于防治昆虫群体。

    ACYL DERIVATIVES
    4.
    发明专利
    ACYL DERIVATIVES 未知

    公开(公告)号：ZA728924B

    公开(公告)日：1973-09-26

    申请号：ZA728924

    申请日：1972-12-18

    Applicant: HOFFMANN LA ROCHE

    Inventor： FURLENMEIER A ,  VOGLER K ,  LANZ P ,  QUITT P

    IPC: C07D207/32 ,  C07D207/327 ,  C07D209/18 ,  C07D213/55 ,  C07D257/04 ,  C07D307/54 ,  C07D333/24 ,  C07D499/00 ,  C07D499/60 ,  C07D

    Abstract: 1353578 Penicillins F HOFFMANN-LA ROCHE & CO AG 11 Jan 1973 [12 Jan 1972] 1605/73 Headings C2A and C2C Novel penicillins having the general Formula (I) and salts thereof, wherein T is a C 2-5 alkyl group and R is a furyl, pyrrolyl, thienyl, oxazolyl, isoxazolyl, thiazolyl, pyridyl, pyrimidinyl, tetrazolyl or indolyl group, which groups R can be substituted by halogen, C 1-3 alkyl, C 1-3 alkoxy or C 1-3 alkylthio, are prepared by N-acylating 6- aminopenicillanic acid (having the carboxyl group protected) with an acid of Formula (II) wherein T and R have the aforesaid meanings, or with an N-acylating functional derivative thereof, and cleaving off the carboxyl-protecting group. The carboxyl group may be protected by saltformation or esterification. Functional derivatives of the acid (II) are, e.g. halides, azides, anhydrides, reactive esters and active amides. When the acid itself is used, a condensing agent such as dicyclohexylcarbodiimide is preferably present. The reaction is usually performed in an inert solvent. The acids of Formula (II) above, which are said to be novel, are prepared by reacting an acid of Formula (V) with the benzyl or tert. butyl ester of a compound of Formula IV in the presence of benzenesulphonyl chloride or phosgene, R and T having the aforesaid meanings, to give an ester of Formula (III) wherein B is a benzyl- or tert.butyl-protected carboxyl group and then cleaving off the protecting group, e.g. by hydrogenation or treatment with a strong acid respectively, to give the desired acid (II). The latter may be converted to the corresponding acid chloride with thionyl chloride. Examples are given for preparing the following acids (II): (R)-2-[(2-isopropyl-2H- tetrazol - 5 - yl)acetoxy] - isocaproic acid; (R)-2- [(2-thienyl)acetoxy]isocaproic acid; and (R)-2-[(3- indolyl)acetoxy]isocaproic acid. Pharmaceutical compositions having antibiotic activity against Gram-positive and -negative bacteria comprise a penicillin of Formula (I) hereinbefore or a salt or hydrate thereof, in association with a compatible pharmaceutical carrier.

    5.
    发明专利
    未知

    公开(公告)号：SE349290B

    公开(公告)日：1972-09-25

    申请号：SE1335867

    申请日：1967-09-28

    Applicant: HOFFMANN LA ROCHE

    Inventor： SCHAEREN S ,  FURLENMEIER A

    IPC: C07C45/40 ,  C07C45/81 ,  C07C49/757 ,  C07C45/00 ,  C07C169/22 ,  C07C169/34

    Abstract: Method for prepn. of carbonyl cpds. (R1, R2 & R3 = sec. amine residues, pref. from di-(1-7C)-alkylamines or heterocyclic amines). (a) The redn. proceeds at low temp., (b) high yield and the carbonyl group does not reduce further, (c) excess phosphine is readily removed by acid washing and (d) no additional solvent is required.

    PROCESS FOR OBTAINING ACYL DERIVATIVE
    7.
    发明专利
    PROCESS FOR OBTAINING ACYL DERIVATIVE 未知

    公开(公告)号：YU70888A

    公开(公告)日：1989-12-31

    申请号：YU70888

    申请日：1988-04-08

    Applicant: HOFFMANN LA ROCHE

    Inventor： FURLENMEIER A ,  GOETSCHI E ,  HEBEISEN P ,  HOFHEIZ W ,  LINK H

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

    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.

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