METHOD FOR NITRATING ANILINE DERIVATIVES
    21.
    发明申请
    METHOD FOR NITRATING ANILINE DERIVATIVES 审中-公开
    氮化苯胺衍生物的方法

    公开(公告)号:WO00063158A1

    公开(公告)日:2000-10-26

    申请号:PCT/EP2000/003247

    申请日:2000-04-12

    摘要: The invention relates to a method for carrying out the highly regioselective aromatic nitration of 4-alkanoylamino-3-alkyl-benzoic acid alkyl esters at the 5-position in a mixture containing nitric acid. The invention also relates to the use of the products obtained using said method and to the production of benzimidazole derivatives which are, in particular, pharmaceutically active.

    摘要翻译: 本发明涉及一种用于在5-位的4 - 烷酰基-3-烷基苯甲酸丙酯高度选择性芳烃硝化的方法为含有硝酸的混合物中,并使用所得到的产品的生产,特别是药物活性的苯并咪唑衍生物。

    NOVEL GLUTAMATE RECEPTOR ANTAGONISTS: FUSED CYCLOALKYLQUINOXALINEDIONES
    26.
    发明申请
    NOVEL GLUTAMATE RECEPTOR ANTAGONISTS: FUSED CYCLOALKYLQUINOXALINEDIONES 审中-公开
    新型谷氨酸受体拮抗剂:融合的环丙基胆碱酯

    公开(公告)号:WO1996017832A1

    公开(公告)日:1996-06-13

    申请号:PCT/US1995014571

    申请日:1995-11-07

    IPC分类号: C07D241/38

    摘要: Novel substituted alicyclic fused ring 2,3-quinoxalinediones, pharmaceutical compositions containing the same and the method of using the same, for the blockade of glutamate receptors, including either or both N-methyl-D-aspartate (NMDA) receptors and non-NMDA receptors such as the alpha -amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptor and the kainate receptor, are described. Methods of preparing the substituted alicyclic fused ring 2,3-quinoxalinediones are also described. Novel intermediates of the inventive quinoxalinediones are disclosed. The novel substituted alicyclic fused ring 2,3-quinoxalinediones may be used, for example, as neuroprotective agents, for treatment of chronic neurodegenerative disorders, as anticonvulsants and in the treatment of schizophrenia, epilepsy, anxiety, pain and drug addiction.

    摘要翻译: 新型取代的脂环稠合环2,3-喹喔啉二酸盐,含有它们的药物组合物及其使用方法,用于封闭谷氨酸受体,包括N-甲基-D-天冬氨酸(NMDA)受体和非NMDA 描述了α-氨基-3-羟基-5-甲基-4-异恶唑丙酸(AMPA)受体和红藻氨酸受体等受体。 还描述了制备取代的脂环稠合环2,3-喹喔啉的方法。 公开了本发明喹喔啉的新型中间体。 新型取代的脂环稠合环2,3-喹喔啉二醇可用作例如神经保护剂,用于治疗慢性神经变性疾病,抗惊厥药和治疗精神分裂症,癫痫,焦虑,疼痛和药物成瘾。

    2,4,6-TRIIODO-5-SUBSTITUTED-AMINO-ISOPHTHALATE ESTERS USEFUL AS X-RAY CONTRAST AGENTS FOR MEDICAL DIAGNOSTIC IMAGING
    27.
    发明申请
    2,4,6-TRIIODO-5-SUBSTITUTED-AMINO-ISOPHTHALATE ESTERS USEFUL AS X-RAY CONTRAST AGENTS FOR MEDICAL DIAGNOSTIC IMAGING 审中-公开
    2,4,6-TRIIODO-5-取代的氨基异癸酸酯作为用于医学诊断成像的X射线对比剂

    公开(公告)号:WO1996000210A1

    公开(公告)日:1996-01-04

    申请号:PCT/US1995007400

    申请日:1995-06-09

    IPC分类号: C07C233/54

    CPC分类号: C07C233/54 A61K49/0433

    摘要: Compounds having structure (I) wherein Q is (II); n is an integer from 0 to 20; R is H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxyalkyl or acetamidoalkyl; R , R , R and R are independently H, alkyl, fluoroalkyl, halogen, hydroxy, acylamino, acetamidoalkyl, cyano, sulfonyl, carboxamido or sulfonamido; R is alkyl, cycloalkyl, aryl or aralkyl; and R is H or -COR are useful as contrast agents in medical diagnostic x-ray imaging compositions and methods.

    摘要翻译: 具有结构(I)的化合物,其中Q是(II); n为0〜20的整数, R 1是H,烷基,氟代烷基,环烷基,芳基,芳烷基,烷氧基烷基或乙酰氨基烷基; R 2,R 3,R 4和R 5独立地是H,烷基,氟烷基,卤素,羟基,酰氨基,乙酰氨基烷基,氰基,磺酰基,甲酰氨基或亚磺酰氨基; R 6是烷基,环烷基,芳基或芳烷基; 和R 7是H或-COR 6可用作医学诊断x射线成像组合物和方法中的造影剂。

    SUBSTITUTED N-PHENYLGLUTARIMIDES AND N-PHENYLGLUTARIC ACID AMIDES, THEIR PREPARATION AND USE IN AGRICULTURE
    28.
    发明申请
    SUBSTITUTED N-PHENYLGLUTARIMIDES AND N-PHENYLGLUTARIC ACID AMIDES, THEIR PREPARATION AND USE IN AGRICULTURE 审中-公开
    取代的N- phenylglutarimide和正PHENYLGLUTARSÄUREAMIDE,生产和使用农业

    公开(公告)号:WO1994010147A1

    公开(公告)日:1994-05-11

    申请号:PCT/EP1993002879

    申请日:1993-10-19

    IPC分类号: C07D211/88

    摘要: Substituted N-phenylglutarimides (I), wherein X , X = O, S; R = halogen, NO2, CN, CF3; R = H, halogen; R , R , R = H, halogen, CN, alkyl, cycloalkyl, alkenyl, alkinyl, alkyl halide, alkoxy, alkoxy halide, alkyl thio, alkyl thio halide, cyanoalkyl, alkoxy carbonyl, possibly substituted phenyl or benzyl, or 2 substituents of a C atom of the glutarimide ring are linked via a possibly substituted chain, or 2 substituents of adjacent C atoms of the glutarimide ring are linked via a possibly substituted chain; A = CHR -CHR -CO-B or CR =CR -CO-B; R = H, C1-C6-alkyl or C1-C6-alkyl halide; R = halogen, alkyl halide, OH, alkoxy or alkyl carbonyl alkoxy; R = H, halogen, CN, alkyl, alkyl halide, OH, alkoxy, alkyl carbonyl, alkoxy carbonyl or alkyl carbonyloxy; B = H, alkyl, alkenyl, alkinyl, alkyl halide, cycloalkyl, alkoxy alkyl, dialkoxy alkyl, alkyl thioalkyl, OR , SR , NR , R ; R = H, alkyl, alkenyl, alkinyl, cycloalkyl, alkyl halide, cyanoalkyl, alkenyl halide, alkoxy carbonyl alkyl, alkoxyalkyl, alkyl thioalkyl, alkylimino, alkylimino alkyl, possibly substituted phenyl or benzyl; R , R = H, alkyl, alkenyl, alkinyl, cycloalkyl, alkyl halide, alkyl carbonyl, alkoxy carbonyl, alkoxy alkyl, possibly substituted phenyl, or R und R together with the common N atom = saturated or unsaturated 4- to 7- membered heterocycle with 1-2 other heteroatoms, as well as salts of (I) that are tolerable to plants; their preparation and use as herbicides and desiccants/defoliants, as well as preproducts for preparing the N-phenylglutarimides (I).

    COMPOSITIONS FOR TREATMENT OF INFLAMMATION-RELATED DISORDERS, PAIN AND FEVER, SKIN DISORDERS, CANCER AND PRECANCEROUS CONDITIONS THEREOF
    30.
    发明申请
    COMPOSITIONS FOR TREATMENT OF INFLAMMATION-RELATED DISORDERS, PAIN AND FEVER, SKIN DISORDERS, CANCER AND PRECANCEROUS CONDITIONS THEREOF 审中-公开
    用于治疗与感染相关的疾病,疼痛和感冒,皮肤疾病,癌症和预防性疾病的组合物

    公开(公告)号:WO2014047592A3

    公开(公告)日:2015-07-23

    申请号:PCT/US2013061247

    申请日:2013-09-23

    申请人: RIGAS BASIL

    发明人: RIGAS BASIL

    摘要: The present invention provides novel compounds and pharmaceutical compositions suitable for administration to mammals, for the prevention and/or treatment of cancer, precancerous conditions, pain, fever, skin disorders, inflammation-related diseases and/or cardiovascular diseases. The compounds of the invention have improved efficacy and safety, including higher potency and/or fewer or less severe side effects, than conventional therapies. These comprise a biologically active moiety or portion (A) preferably derived from a non-steroidal anti-inflammatory drug or NSAID (A), bound via a linker moiety (B) to functional moiety Z, which facilitates access of the compound into cells. The moiety Z can comprise, for example, a phosphorous-containing group, a nitrogen-containing group, or a folic acid residue.

    摘要翻译: 本发明提供适用于哺乳动物施用,用于预防和/或治疗癌症,癌前病症,疼痛,发热,皮肤病症,炎症相关疾病和/或心血管疾病的新型化合物和药物组合物。 本发明的化合物具有改善的功效和安全性,包括比常规疗法更高的效力和/或更少或更少的副作用。 它们包括生物活性部分或部分(A),优选衍生自通过接头部分(B)与功能部分Z结合的非甾体抗炎药或NSAID(A),其有助于化合物进入细胞。 部分Z可以包括例如含磷基团,含氮基团或叶酸残基。