Heterocyclic compounds, their production and use as tachykinin reactor
antagonists
    4.
    发明授权
    Heterocyclic compounds, their production and use as tachykinin reactor antagonists 失效
    杂环化合物,它们的生产和用作速激肽反应器拮抗剂

    公开(公告)号:US5585385A

    公开(公告)日:1996-12-17

    申请号:US338762

    申请日:1994-11-10

    摘要: A novel compound represented by the formula: ##STR1## wherein Ring A and Ring B respectively stands for an optionally substituted homo- or hetero-cyclic ring, and at least one of them stands for an optionally substituted heterocyclic ring stand; Ring C stands for an optionally substituted benzene ring; R stands for a hydrogen atom or an optionally substituted hydrocarbon residue; one of X and Y stands for --NR.sup.1 -- (R.sup.1 stands for a hydrogen atom or an optionally substituted hydrocarbon residue) or --O--, and the other stands for--CO-- or --CS--, or one of them stands for --N.dbd. and the other stands for .dbd.CR.sup.2 -- (R.sup.2 stands for a hydrogen atom, a halogen atom, an optionally substituted hydrocarbon residue, an optionally substituted amino group or an optionally substituted hydroxyl group); n denotes 1 or 2 or salts thereof which have an excellent tachykinin receptor antagonistic action and inhibitory action on plasma extravasation.

    摘要翻译: 由下式表示的新化合物:其中环A和环B分别代表任选取代的同 - 或杂环环,并且其中至少一个代表任选取代的杂环环; 环C代表任选取代的苯环; R代表氢原子或任选取代的烃残基; X和Y之一代表-NR1-(R1代表氢原子或任选取代的烃残基)或-O-,另一个代表-CO-或-CS-,或其中一个代表-N =和另一个代表= CR2-(R2代表氢原子,卤原子,任选取代的烃残基,任选取代的氨基或任选取代的羟基); n表示1或2或其盐,其具有优异的速激肽受体拮抗作用和对血浆外渗的抑制作用。

    Antibiotic tan-749, its derivatives, production and use thereof
    5.
    发明授权
    Antibiotic tan-749, its derivatives, production and use thereof 失效
    抗生素tan-749,其衍生物,生产和使用

    公开(公告)号:US4906659A

    公开(公告)日:1990-03-06

    申请号:US129737

    申请日:1987-12-07

    摘要: A compound of the formula ##STR1## wherein R.sup.1 and R.sup.4 are independently amino or an organic residue bonded through nitrogen, R.sup.2 is hydrogen or alkyl which may be substituted, R.sup.3 is hydrogen or a protecting group and R5 is hydroxyl which may be substituted or amino which may be substituted or salts thereof; with the proviso that when R.sup.1 is amino, leucylamino, acetylamino or benzyloxycarbonylamino, R.sup.3 is hydrogen, methyl or 2-tettrahydropyranyl, R.sup.4 is amino, acetylamino or benzyloxycarbonylamino and R.sup.5 is hydroxyl which may be substituted or amino which may be substituted, R.sup.2 is alkyl which may be substituted, has antibacterial activities against drug-resistant bacteria and therefore can be useful as a chemotherapeutic drug for bacterial infections in mammals.

    摘要翻译: 式IMA的化合物,其中R 1和R 4独立地为氨基或通过氮键合的有机残基,R 2为氢或可被取代的烷基,R 3为氢或保护基,R 5为可被取代的羟基或氨基 其可以被取代或其盐; 条件是当R1为氨基,亮氨酰氨基,乙酰氨基或苄氧羰基氨基时,R3为氢,甲基或2-四氢吡喃基,R4为氨基,乙酰氨基或苄氧羰基氨基,R5为可被取代的羟基或可被取代的氨基,R2为烷基 其可以被取代,对耐药细菌具有抗菌活性,因此可用作哺乳动物细菌感染的化学治疗药物。

    Carbapenems, their production and use
    7.
    发明授权
    Carbapenems, their production and use 失效
    碳水化合物,其生产和使用

    公开(公告)号:US4698339A

    公开(公告)日:1987-10-06

    申请号:US655454

    申请日:1984-09-28

    摘要: A compound of the general formula: ##STR1## wherein X is a lower alkylene group which may optionally be substituted by a hydroxyl group, or a lower alkenylene group, Y is (1) a lower alkyl group, (2) a cycloalkyl group containing 3 to 8 carbon atoms, (3) a lower alkenyl group, (4) an aryl group, (5) an aralkyl group or (6) a 3- to 8-membered heterocyclic group, or the partial structural formula Y--SO.sub.2 --X--, with X and Y being combined with each other, represents a group of the formula: ##STR2## wherein l is an integer of 0 to 3, and m and n each is an integer of 0 to 6, provided that the sum of m and n is in the range of 2 to 6, and R is a hydrocarbon group which may optionally be substituted or a 3- to 8-membered heterocyclic group, or a pharmaceutically acceptable salt thereof a method of production thereof and use thereof. The compound (I) has antimicrobial and .beta.-lactamase inhibitory activities.

    摘要翻译: 下式的化合物:其中X是可以被羟基或低级亚烯基取代的低级亚烷基,Y是(1)低级烷基,(2)a 含有3〜8个碳原子的环烷基,(3)低级烯基,(4)芳基,(5)芳烷基或(6)3-8元杂环基,或部分结构式Y -SO 2 -X-,其中X和Y彼此结合,表示下式的基团:其中l为0〜3的整数,m和n各自为0〜 6,条件是m和n的总和在2至6的范围内,并且R是可任选取代的烃基或3至8元杂环基,或其药学上可接受的盐,其方法为 其生产和使用。 化合物(I)具有抗微生物和β-内酰胺酶抑制活性。

    Benzodiazepine carboxamides and pharmaceutical compositions with central
nervous system activity
    9.
    发明授权
    Benzodiazepine carboxamides and pharmaceutical compositions with central nervous system activity 失效
    苯二氮卓类甲酰胺和具有中枢神经系统活性的药物组合物

    公开(公告)号:US4049812A

    公开(公告)日:1977-09-20

    申请号:US572943

    申请日:1975-04-30

    CPC分类号: C07D487/14 C07D213/50

    摘要: There is disclosed a novel heterocyclic compound of the general formula: ##STR1## wherein each of R.sup.1 and R.sup.2 represents hydrogen atom, or an alkyl group which may be substituted by alkyl-substituted amino, hydroxy or alkoxy group, or R.sup.1 and R.sup.2 may form a heterocyclic ring together with the nitrogen atom adjacent thereto; R.sup.3 represents hydrogen atom or a lower alkyl group; P.sub.y represents a pyridyl group; B represents a lower alkylene group which may have lower alkyl group as a substituent; Y represents oxygen atom, sulfur atom or --NH-- group; and ring A is either unsubstituted or substituted by halogen atom, nitro, lower alkyl, lower alkoxy or polyhalo-lower alkyl group. This class of compounds is found to be useful as medicine in human and animal therapy, which act on the central nervous system, for example, muscle relaxants, anticonvulsants, sedatives, minor tranquilizers. There is also disclosed intermediates for the production of said compound.

    摘要翻译: 公开了以下通式的新型杂环化合物:其中R 1和R 2各自表示氢原子,或可被烷基取代的氨基,羟基或烷氧基取代的烷基,或R 1和R 2可形成 杂环与与其相邻的氮原子一起; R3表示氢原子或低级烷基; Py代表吡啶基; B表示可以具有低级烷基作为取代基的低级亚烷基; Y表示氧原子,硫原子或-NH-基团; 并且环A是未取代的或被卤素原子,硝基,低级烷基,低级烷氧基或多卤代低级烷基取代。 发现这类化合物可用作人和动物治疗中的药物,其作用于中枢神经系统,例如肌肉松弛剂,抗惊厥药,镇静剂,微量镇静剂。 还公开了用于生产所述化合物的中间体。