N,N-substituted cyclic amine derivatives
    27.
    发明授权
    N,N-substituted cyclic amine derivatives 失效
    N,N-取代的环胺衍生物

    公开(公告)号:US06737425B1

    公开(公告)日:2004-05-18

    申请号:US09743358

    申请日:2001-01-29

    IPC分类号: A61K31497

    摘要: The invention provides an N,N-substituted cyclic amine compound represented by the following formula (VIII): wherein A represents an aryl group etc.; E represents a group represented by the formula —CO— or a group represented by the formula —CHOH—; G represents an oxygen atom etc.; J represents an aryl group which may be substituted; R1 represents a lower alkyl group etc.; Alk represents a linear or branched lower alkylene group; n, v, w, x and y are independent of each other and each represents 0 or 1; and p represents 2 or 3, or a pharmacologically acceptable salt thereof. The compound of the present invention or a salt thereof is effective to treat a disease against which calcium antagonism is effective. The disease may include acute ischemic stroke, cerebral apoplexy, cerebral infarction, head trauma, cerebral nerve cell death, Alzheimer disease, Parkinson disease, amyotrophic lateral sclerosis, Huntington disease, cerebral circulatory metabolism disturbance, cerebral function disturbance, pain, spasm, schizophrenia, migraine, epilepsy, maniac-depressive psychosis, nerve degenerative diseases, cerebral ischemia, AIDS dementia complications, edema, anxiety disorder (generalized anxiety disorder) and diabetic neuropathy.

    摘要翻译: 本发明提供由下式(VIII)表示的N,N-取代的环胺化合物:其中A表示芳基等; E表示由式-CO-表示的基团或由式-CHOH-表示的基团; G表示氧原子等。 J表示可被取代的芳基; R 1表示低级烷基等。 Alk表示直链或支链低级亚烷基; n,v,w,x和y彼此独立,各自表示0或1; 和p表示2或3,或其药理学上可接受的盐。 本发明的化合物或其盐可有效治疗钙拮抗作用有效的疾病。 该疾病可能包括急性缺血性脑卒中,脑中风,脑梗塞,头部创伤,脑神经细胞死亡,阿尔茨海默病,帕金森病,肌萎缩性侧索硬化,亨廷顿病,脑循环代谢障碍,脑功能障碍,疼痛,痉挛,精神分裂症, 偏头痛,癫痫,疯子抑郁精神病,神经退行性疾病,脑缺血,艾滋病痴呆并发症,水肿,焦虑症(广泛性焦虑症)和糖尿病性神经病变。

    Nitrile compound
    28.
    发明授权
    Nitrile compound 失效
    腈化合物

    公开(公告)号:US06667412B1

    公开(公告)日:2003-12-23

    申请号:US09914349

    申请日:2001-08-27

    IPC分类号: C07C25536

    摘要: The present invention provides a novel nitrile compound useful as an intermediate for the production of, for example, N,N-substituted cyclic amine derivatives or phenylacetonitrile derivatives that are useful as a medicine. Specifically it provides a nitrile carboxylic acid compound, nitrile ester compound and nitrile alcohol compound. That is, it provides a nitrile compound represented by the following formula (I): wherein R1 and R2 means substituents; m means 0 or an integer of from 1 to 6; n means 0 or an integer of from 1 to 5; and R3 means carboxyl group, a lower alkoxycarbonyl group or hydroxymethyl group.

    摘要翻译: 本发明提供了可用作制备例如可用作药物的N,N-取代的环胺衍生物或苯乙腈衍生物的中间体的新型腈化合物。 具体地说,它提供了一种腈羧酸化合物,腈酯化合物和腈醇化合物。 也就是说,它提供由下式(I)表示的腈化合物:其中R 1和R 2表示取代基; m表示0或1〜6的整数; n表示0或1至5的整数; R 3表示羧基,低级烷氧基羰基或羟甲基。

    Transglycosylation reactions employing .beta.-galactosidase
    30.
    发明授权
    Transglycosylation reactions employing .beta.-galactosidase 失效
    使用β-半乳糖苷酶的转糖基化反应

    公开(公告)号:US5876981A

    公开(公告)日:1999-03-02

    申请号:US733232

    申请日:1996-10-17

    CPC分类号: C12P19/26 C12P19/14

    摘要: .beta.-Galactosides are synthesized using a transglycosylation reaction catalyzed by .beta.-galactosidase. The reaction employs a carbohydrate donor having a glycosidic leaving group attached to its anomeric carbon and an oxo group attached to the C-6 carbon. Strong leaving groups are preferred over weak leaving groups. The method can be carried out in aqueous solution without organic solvents to give the transglycosylation product in high yields and high regioselectivity. The synthesis of lactosamine using this methodology with galactose oxidase (GO) and .beta.-galactosidase has been accomplished. (FIG. 3). The methodology affords simple reaction conditions and minimal purification steps. In addition, the intermediate substrates maintain high stability, the process affords high yields and the enzymes and reagents employed are commercially available with high stability and low costs.

    摘要翻译: β-半乳糖苷是使用由β-半乳糖苷酶催化的转糖基化反应合成的。 该反应采用具有与其端基异构碳连接的糖苷离去基团和与C-6碳连接的氧代基团的碳水化合物供体。 强离去基团优于弱离去基团。 该方法可以在没有有机溶剂的水溶液中进行,以高收率和高区域选择性得到转糖基化产物。 已经完成了使用该方法与半乳糖氧化酶(GO)和β-半乳糖苷酶合成乳糖胺。 (图3)。 该方法提供简单的反应条件和最小的纯化步骤。 此外,中间基材保持高稳定性,该方法提供高产率,所用的酶和试剂可以高稳定性和低成本商购。