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    Ergoline derivatives and a process for their preparation
    2.
    发明授权
    Ergoline derivatives and a process for their preparation 失效
    艾尔莫林衍生物及其制备方法

    公开(公告)号：US4196288A

    公开(公告)日：1980-04-01

    申请号：US856536

    申请日：1977-12-01

    Applicant: Enzo Beacco ,  Luigi Bernardi ,  Enrico Di Salle ,  Giovanni Falconi ,  Bianca Patelli

    Inventor： Enzo Beacco ,  Luigi Bernardi ,  Enrico Di Salle ,  Giovanni Falconi ,  Bianca Patelli

    IPC: A61K31/48 ,  A61K31/495 ,  A61K31/505 ,  C07D457/02

    CPC classification number: C07D457/02

    Abstract: New ergoline derivatives are disclosed which are compounds of formula (I) having the structure: ##STR1## wherein R.sub.1 is hydrogen or methoxy; R.sub.2 is hydrogen or methyl; andX is hydroxy, R.sub.3 COO, S--R.sub.4 or NR.sub.5 R.sub.6 in which R.sub.3 is a straight or branched alkyl having from 1 to 6 carbon atoms, unsubstituted- or substituted-phenyl, the substituents being selected from the class consisting of chlorine, bromine, alkyl or alkoxy having from 1 to 4 carbon atoms, cycloalkyl containing from 3 to 6 carbon atoms, or a heterocycle;R.sub.4 is phenyl or a heterocycle, andR.sub.5 and R.sub.6 are alkyl having from 1 to 4 carbon atoms, or together with the N atom to which they are attached, forming a heterocycle. The heterocycle may be a 5- or 6-membered ring which contains from 1 to 3 hetero atoms selected from the class consisting of nitrogen, oxygen and sulphur, and may be saturated or unsaturated, and unsubstituted or substituted by halogen, alkyl having from 1 to 3 carbon atoms, hydroxy, nitro, amino, CONHNH.sub.2 and COOH.

    Abstract translation: 公开了新的麦角灵衍生物，其是具有以下结构的式（I）的化合物：其中R 1是氢或甲氧基; R2是氢或甲基; 并且X是羟基，R 3 COO，S-R 4或NR 5 R 6，其中R 3是具有1至6个碳原子的直链或支链烷基，未取代或取代的苯基，所述取代基选自氯，溴，烷基 或具有1至4个碳原子的烷氧基，含3至6个碳原子的环烷基或杂环; R 4是苯基或杂环，R 5和R 6是具有1至4个碳原子的烷基，或与它们相连的N原子一起形成杂环。 杂环可以是含有1至3个选自氮，氧和硫的杂原子的5或6元环，并且可以是饱和或不饱和的，未取代的或被卤素取代的烷基，具有1个 至3个碳原子，羟基，硝基，氨基，CONHNH 2和COOH。

    Process for preparing azetidinone thiazolidine derivatives
    4.
    发明授权
    Process for preparing azetidinone thiazolidine derivatives 失效
    制备氮杂环丁酮噻唑烷衍生物的方法

    公开(公告)号：US4077969A

    公开(公告)日：1978-03-07

    申请号：US587090

    申请日：1975-06-16

    Applicant: Luigi Bernardi ,  Maurizio Foglio ,  Giovanni Francheschi

    Inventor： Luigi Bernardi ,  Maurizio Foglio ,  Giovanni Francheschi

    IPC: C07D513/04

    CPC classification number: C07D513/04

    Abstract: A process is disclosed for preparing azetidonethiazolidines of the formula ##STR1## where R and V are defined herein below, wherein a compound of the structure ##STR2## dissolved in a suitable solvent, is treated at about 0.degree. C with a solution of preferably anhydrous hydrochloric acid in a lower aliphatic alcohol with a slight excess of sodium cyanoborohydride.

    Abstract translation: 公开了一种制备下式定义的式“IMAGE”的氮杂环丁烷的方法，其中R和V如下文定义，其中溶解在合适溶剂中的结构式“IMAGE”的化合物在约0℃下用优选无水溶液 在低级脂族醇中加入盐酸，稍加过量氰基硼氢化钠。

    L-lyxohex-1-enopyranose derivative
    6.
    发明授权
    L-lyxohex-1-enopyranose derivative 失效
    L-赖索昔-1-吡喃葡萄糖衍生物

    公开(公告)号：US4020270A

    公开(公告)日：1977-04-26

    申请号：US650519

    申请日：1976-01-19

    Applicant: Federico Arcamone ,  Giuseppe Cassinelli

    Inventor： Federico Arcamone ,  Giuseppe Cassinelli

    IPC: C07D309/30 ,  C07H15/252 ,  C07H5/06

    CPC classification number: C07H15/252 ,  C07D309/30 ,  Y02P20/55

    Abstract: Anthracyclinone glycoside antibiotics including the known antibiotics daunomycin and adriamycin, as well as other, novel glycoside antibiotics of the formula (VIII): ##STR1## wherein WHEN R.sub.1 is hydrogen, R.sub.2 and R.sub.3 are each independently hydrogen, methyl, methoxy, chloro, or bromo; and when R.sub.2 and R.sub.3 are hydrogen, R.sub.1 is methyl, chloro, or bromo and R.sub.4 and R.sub.5 are each independently hydrogen or hydroxy are prepared by an acid catalyzed addition reaction between (a) an anthracyclinone compound of the formula ##STR2## or a dioxolanyl protected derivative thereof (VI) having the formula: ##STR3## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined above, and R.sub.6, R.sub.7 and R.sub.8 are independently selected from the group consisting of hydrogen and C.sub.1 -C.sub.4 alkyl; or R.sub.7 and R.sub.8, together with the carbon atom to which they are bound may form a saturated or unsaturated ring of 3-8 carbon atoms and (b) a novel reactive, protected 1,2-unsaturated pyranoid sugar, preferably, 1,2,3,6-tetradeoxy-3-trifluoroacetamido-4-trifluoroacetoxy-L-lyxo-hex-1-enopyranose which forms protected derivatives of said glycoside antibiotics and then removing the protecting groups from said glycoside antibiotics. These antibiotics are useful in the treatment of various human cancers and leukemia such as sarcomas, breast cancer, bronchogenic carcinoma, malignant lymphomas, neuroblastomas, acute leukemia and bladder cancer.

    Abstract translation: 蒽环类抗生素包括已知的抗生素道诺霉素和阿霉素，以及其它式（VIII）的新型糖苷抗生素：其中当R1是氢时，R2和R3各自独立地是氢，甲基，甲氧基， 氯或溴; 并且当R 2和R 3为氢时，R 1为甲基，氯或溴，并且R 4和R 5各自独立地为氢或羟基，是通过（a）式（III）的蒽环类化合物之间的酸催化加成反应制备的， 或其具有下式的二氧杂环戊烷基保护的衍生物（VI）：其中R 1，R 2，R 3，R 4和R 5如上所定义，并且R 6，R 7和R 8独立地选自氢 和C 1 -C 4烷基; 或R 7和R 8与它们所连接的碳原子一起可以形成3-8个碳原子的饱和或不饱和的环，和（b）新的反应性保护的1,2-不饱和吡喃糖，优选1,2 ，3,6-四脱氧-3-三氟乙酰氨基-4-三氟乙酰氧基-L-赖摩尔 - 己-1-吡喃糖，其形成所述糖苷抗生素的受保护的衍生物，然后从所述糖苷抗生素中除去保护基团。 这些抗生素可用于治疗各种人类癌症和白血病如肉瘤，乳腺癌，支气管癌，恶性淋巴瘤，神经母细胞瘤，急性白血病和膀胱癌。

    Thiohydrazoazetidinones
    7.
    发明授权
    Thiohydrazoazetidinones 失效
    THIOHYDRAZOAZETIDINONES

    公开(公告)号：US4143037A

    公开(公告)日：1979-03-06

    申请号：US797608

    申请日：1977-05-16

    Applicant: Maurizio Foglio ,  Giovanni Franceschi ,  Paolo Masi ,  Antonino Suarato

    Inventor： Maurizio Foglio ,  Giovanni Franceschi ,  Paolo Masi ,  Antonino Suarato

    IPC: C07D205/095 ,  C07D205/08

    CPC classification number: C07D205/095

    Abstract: A process is disclosed for preparing compounds of structure: ##STR1## where R.sup.1 is hydroxyl, alkoxy with 1 to 4 carbon atoms, trichloroethoxy, benzyloxy, p-methoxybenzyloxy, p-nitrobenzyloxy, benzhydryloxy, triphenylmethoxy, phenacyloxy, or p-halophenacyloxy;Z is hydrogen, hydroxyl, --O-alkyl, --O--CO-alkyl, --Br, --I, --N.sub.3, --O--CO--CH.sub.3, O--CO--NH.sub.2, or an S-mononuclear heterocyclic ring,Starting from ##STR2## where R is hydrogen, alkyl having from 1 to 4 carbon atoms, cyano-methyl, thienyl-methyl, furyl-methyl, naphthyl-methyl, phenyl-methyl, phenoxy-methyl, phenyl-isopropyl, phenoxy-isopropyl, pyridyl-4-thiomethyl, or tetrazolyl-1-methyl;R.sup.2 and R.sup.3 are lower alkyl, a mononuclear aryl ring, CN, a mononuclear heterocyclic ring or the radicals --COR.sup.4, --COOR.sup.4, ##STR3## --CONHR.sup.4, or R.sub.2 and R.sub.3 together represent ##STR4## where T represents ##STR5## and R.sup.4 is a lower alkyl, a mononuclear aryl or heterocyclic ring, WHEREIN THE COMPOUND (II') is reacted with a phosphorous halide in the presence of a tertiary amine, the corresponding imino chloride is reacted with a lower aliphatic alcohol, the iminoether so formed is hydrolyzed in an acid medium, and the resultant 3-amino-2-.beta.-thiohydrazoazetidinone: ##STR6## in which R.sup.1, R.sup.2, R.sup.3 and Z have the meanings given heretofore,Is reacted between -100.degree. and +120.degree. C. with inorganic basic or weakly acid oxides or inorganic and organic bases, to give (V).

    Daunomycin analogues, their preparation and use
    10.
    发明授权
    Daunomycin analogues, their preparation and use 失效
    道诺霉素类似物，其制备和用途

    公开(公告)号：US4046878A

    公开(公告)日：1977-09-06

    申请号：US579901

    申请日：1975-05-22

    Applicant: Bianca Patelli ,  Luigi Bernardi ,  Federico Arcamone ,  Aurelio Di Marco

    Inventor： Bianca Patelli ,  Luigi Bernardi ,  Federico Arcamone ,  Aurelio Di Marco

    IPC: A61K31/704 ,  C07H15/252 ,  A61K31/71 ,  C07H11/00

    CPC classification number: C07H15/252 ,  Y10S514/908

    Abstract: Daunomycin analogues of the formula: ##STR1## wherein when each R.sub.1 is hydrogen, each R is hydrogen, chlorine, bromine, methyl or methoxy and when each R.sub.1 is chlorine, bromine or methyl, each R is hydrogen, are useful in treating various mammalian tumors and are prepared by reacting a daunomycinone derivative of the formula: ##STR2## wherein R and R.sub.1 are as defined above with 1-chloro-2,3,6-trideoxy-3-trifluoroacetamido-4-trifluoroacetoxy-.alpha.-L-lyxopyranose in an inert anhydrous organic solvent in the presence of a catalyst and a hydrogen chloride acceptor.

    Abstract translation: 道诺霉素类似物，具有下式：其中当每个R 1是氢时，每个R是氢，氯，溴，甲基或甲氧基，并且当每个R 1是氯，溴或甲基时，每个R是氢，可用于 治疗各种哺乳动物肿瘤，并且通过使下式的道诺霉素酮衍生物：其中R和R 1如上所定义的道诺霉素酮衍生物与1-氯-2,3,6-三脱氧-3-三氟乙酰氨基-4-三氟乙酰氧基 α-L-吡喃葡萄糖在惰性无水有机溶剂中，在催化剂和氯化氢受体存在下。

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