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    Imidazolinyl-ethyl-dithiocarbamic acid esters
    2.
    发明授权
    Imidazolinyl-ethyl-dithiocarbamic acid esters 失效
    咪唑啉-2-乙酸二盐酸酯

    公开(公告)号：US3784633A

    公开(公告)日：1974-01-08

    申请号：US3784633D

    申请日：1972-05-16

    Applicant: HOECHST AG

    Inventor： SCHORR M ,  DUWEL D

    IPC: C07D233/26 ,  C07D49/34

    CPC classification number: C07D233/26

    Abstract: -2-IMIDAZOLINE

    IN WHICH X AND Y STANDS FOR HYDROGEN OR HALOGEN.

    IMIDAZOLINYL-ETHYL-DITHIOCARBAMIC ACID ESTERS AND THEIR PHYSIOLOGICALLY COMPATIBLE SALTS ARE DESCRIBED AS WELL AS THE PROCESS OF THEIR MANUFACTURE AND THEIR ANTHELMINTIC ACTION. THE NOVEL COMPOUNDS CORRESPOND TO FORMULA I

    2-(4-(NC-)PHENYL),1-((X,Y-PHENYL)-CH2-S-C(=S)-NH-CH2-CH2-)

    3-aminoacylamino thiophenes
    3.
    发明授权
    3-aminoacylamino thiophenes 失效
    3-氨基亚氨基硫醇

    公开(公告)号：US3855243A

    公开(公告)日：1974-12-17

    申请号：US40238273

    申请日：1973-10-01

    Applicant: HOECHST AG

    Inventor： RUSCHIG H ,  SCHORR M ,  MUSCHAWECK R ,  RIPPEL R

    IPC: C07D333/36 ,  A61K27/00 ,  C07D63/12 ,  C07D63/16

    CPC classification number: C07D333/42 ,  Y10S514/818

    Abstract: 3-Aminoacylamino-thiophenes of the formula

    AND THEIR PHYSIOLOGICALLY TOLERATED SALTS, USEFUL AS LOCAL ANESTHETICS. Methods of making these compounds. In the formula, R1 may be hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl, cycloalkenyl, or alkenyl; R2 is alkyl, hydroxyalkyl, alkoxyalkyl, cycloalkyl, or alkenyl; R1 and R2, taken together, may also form a saturated heterocyclic ring with the nitrogen atom to which they are attached, which ring may also contain an oxygen atom, a methylimino group, or a further nitrogen atom; R3, R4, and R5 are each hydrogen, alkyl, or carbalkoxy; and A is alkylene.

    Abstract translation: 3-氨基酰基氨基 - 噻吩类化合物及其生理学上可容忍的盐，有用的当地麻醉品。 制备这些化合物的方法。 在该式中，R 1可以是氢，烷基，羟基烷基，烷氧基烷基，环烯基或烯基; R2是烷基，羟基烷基，烷氧基烷基，环烷基或烯基; R 1和R 2一起也可以与它们所连接的氮原子形成饱和杂环，该环也可以含有氧原子，甲基亚氨基或另外的氮原子; R 3，R 4和R 5各自为氢，烷基或烷氧基; A是亚烷基。

    Acylaminopenicillanic acids and salts thereof
    5.
    发明授权
    Acylaminopenicillanic acids and salts thereof 失效
    ACYLAMINOPENICILLANIC酸及其盐

    公开(公告)号：US3749711A

    公开(公告)日：1973-07-31

    申请号：US3749711D

    申请日：1970-09-18

    Applicant: HOECHST AG

    Inventor： SCHORR M ,  SCHRINNER E ,  SCHUTZE E

    IPC: C07D233/22 ,  C07D499/00 ,  C07D499/44 ,  C07D499/48 ,  C07D99/16

    CPC classification number: C07D499/00 ,  C07D233/22

    Abstract: ANTIBIOTICALLY ACTIVE ACYLAMINOPENICILLANIC ACIDS OF THE GENERAL FORMULA I

    6-(R1-N=C(-N(-R2)(-R3))-A-B-CH2-CO-NH-),2-(HOOC-),3,3-

    DI(CH3-)PENAM

    IN WHICH R1, R2 AND R3 REPRESENT HYDROGEN OR LOWER ALKYL GROUPS, R1 AND R2 MAY FORM TOGETHER AN ALKYLENE GROUP WHICH MAY BE SUBSTITUTED, A REPRESENTS A PHENYLENE OR THIENYLENE GROUP WHICH MAY BE SUBSTITUTED AND B REPRESENTS OXYGEN OR A CHEMICAL BOND, AND THE PHYSIOLOGICALLY TOLERATED SALTS THEREOF, PHARMACEUTICAL PREPARATIONS CONTAINING THESE COMPOUNDS AND PROCESS FOR THE PREPARATION OF SUCH COMPOUNDS AND PREPARATIONS.

    9.
    发明专利
    未知

    公开(公告)号：SE375097B

    公开(公告)日：1975-04-07

    申请号：SE1307070

    申请日：1970-09-25

    Applicant: HOECHST AG

    Inventor： SCHORR M ,  SCHRINNER E ,  SCHUTZE E

    IPC: C07D233/22 ,  C07D499/00 ,  C07D499/44 ,  C07D499/48 ,  C07D99/16

    Abstract: 1285790 Acylaminopenicillins FARBWERKE HOECHST AG 28 Sept 1970 [27 Sept 1969 (2)] 46107/70 Headings C2A andC2C Novel acylaminopenicillanic acids of Formula I wherein R 1 and R 2 are the same or different and are hydrogen or C 1 to C 5 alkyl or together form an optionally substituted alkylene group linking the nitrogen atoms, R 3 is hydrogen or C 1 to C 5 alkyl, A is an optionally substituted phenylene or thienylene group and B is oxygen or a chemical bond, and salts thereof, are prepared by reacting 6-aminopenicillanic acid or a salt thereof with a carboxylic acid of Formula II wherein R 1 , R 2 , R 3 , A and B are as defined above or an N-acylating derivative or salt thereof. The groups R1, R 2 and R 3 preferably contain a total of not more than 6 carbon atoms. When R 1 and R 2 form an alkylene group, this may be substituted, e.g. by C 1 to C 5 alkyl groups which may be closed into a ring and this ring may include a hetero atom. A is preferably 1,4-phenylene or 2,5-thienylene and may be substituted, e.g. by alkyl, alkoxy and/or halogen. The reaction may be carried out in water, preferably together with a water-miscible solvent, at pH 6-9 and at ambient temperature or below; an acid-acceptor, e.g. NaHC0 3 or triethylamine, is preferably present in the medium. The product may be isolated by simply lyophilizing the reaction mixture to give the penicillin in the form of a crude mixture with salts (e.g. NaCl) formed as by-products, which may be used therapeutically without purification providing the salts are non-toxic. It is purified by re-crystallization from concentrated aqueous solution. The acid chlorides of 4-amidinophenylacetic acid, 4-amidmophenoxyacetic acid and 4-(2- imidazolinyl)-phenoxyacetic acid as their hydrochloride salts are prepared by reacting the acid with thionyl chloride. Pharmaceutical compositions having antibacterial activity against gram-positive and gramnegative bacteria comprise an acylaminopenicillanic acid of Formula I as defined above or a physiologically tolerable salt thereof together with a pharmaceutical carrier.

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