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    • 6. 发明授权
    • Process for producing xanthine derivatives with bacteria and fungi
    • 用细菌和真菌生产黄嘌呤衍生物的方法
    • US6107064A
    • 2000-08-22
    • US581533
    • 1996-01-17
    • Junichi ShimadaTamotsu EguchiKenichi MochidaAkira HoriguchiTohru YasuzawaHideaki KusakaHiromi NonakaFumio Suzuki
    • Junichi ShimadaTamotsu EguchiKenichi MochidaAkira HoriguchiTohru YasuzawaHideaki KusakaHiromi NonakaFumio Suzuki
    • C07D473/04C07D473/06C12P17/18C12P17/16
    • C07D473/04C07D473/06C12P17/18
    • The present invention relates to a process for producing a xanthine derivative represented by formula (II), comprising converting a xanthine derivative represented by formula (I) {hereinafter, referred to as Compound (I)}: ##STR1## (wherein R.sup.1 and R.sup.2 independently represent hydrogen, or hydroxy-substituted, oxo-substituted, or unsubstituted lower alkyl) into a xanthine derivative represented by formula (II) {hereinafter, referred to as Compound (II)}: ##STR2## (wherein R.sup.3 and R.sup.4 independently represent hydrogen, or hydroxy-substituted, oxo-substituted, or unsubstituted lower alkyl; R.sup.5 and R.sup.6 independently represent hydrogen, hydroxy, or oxo; with the proviso that R.sup.5 and R.sup.6 are both hydrogen, at least one of R.sup.3 and R.sup.4 is hydroxy-substituted or oxo-substituted lower alkyl; and X and Y both represent hydrogen or are combined with each other to form a single bond) in the presence of an enzyme source for catalyzing hydroxylation or carbonylation of Compound (I) into Compound (II), and collecting the produced Compound (II).
    • PCT No.PCT / JP95 / 00929 Sec。 371日期1996年1月17日 102(e)日期1996年1月17日PCT提交1995年5月16日PCT公布。 公开号WO95 / 31460 日本特开平9-1252号公报发明内容本发明涉及由式(II)表示的黄嘌呤衍生物的制造方法,其特征在于,将由式(I)表示的黄嘌呤衍生物{以下称为化合物(I)} 和R2独立地表示氢或羟基取代的,取代或未取代的低级烷基)转化为由式(II)表示的黄嘌呤衍生物(以下称为化合物(II)}:(其中R 3和R 4独立地表示氢 或羟基取代的,取代或未取代的低级烷基; R 5和R 6独立地表示氢,羟基或氧代;条件是R 5和R 6都是氢,R 3和R 4中的至少一个是羟基取代的或 氧代取代的低级烷基; X和Y均表示氢或彼此结合形成单键)在用于催化化合物(I)羟化或羰基化成化合物(II)的酶源的存在下,以及大学 将所制备的化合物(II)。
    • 7. 发明申请
    • Antidepressants or foods and beverage for antidepression
    • 抗抑郁药或抗抑郁食品和饮料
    • US20070021355A1
    • 2007-01-25
    • US10558706
    • 2004-05-28
    • Hiroaki KohnoHideaki Kusaka
    • Hiroaki KohnoHideaki Kusaka
    • A61K31/7056
    • C07D405/04A23L2/52A23L33/10A61K31/404A61K31/7056C07H7/06
    • An object of the present invention is to provide antidepressants or foods and drinks for antidepression. To solve the present problem, the present invention provides antidepressants or foods and drinks for antidepression comprising, as an active ingredient, a compound represented by formula (I): (wherein R1, R2, R3 and R4, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, or the like; R5 represents a hydrogen atom, hydroxy, or the like; R6 represents a hydrogen atom, or the like; R7 represents a hydrogen atom or substituted or unsubstituted lower alkyl; and R8, R9, R10 and R11, which may be the same or different, each represent a hydrogen atom or substituted or unsubstituted lower alkyl) or a salt thereof.
    • 本发明的目的是提供抗抑郁药或食品和饮料用于抗抑郁。 为了解决本发明的问题,本发明提供了抗抑郁药或抗抑郁药的食品和饮料,其含有作为活性成分的式(I)表示的化合物:(其中R 1,R 2,R 2, R 3,R 3和R 4可以相同或不同,各自表示氢原子,取代或未取代的低级烷基等; R 5是氢原子,羟基等; R 6表示氢原子等; R 7表示氢原子, 或取代或未取代的低级烷基;和R 8,R 9,R 10和R 11,其可以 相同或不同,各自表示氢原子或取代或未取代的低级烷基)或其盐。
    • 8. 发明授权
    • Quinazolines and phthalazines having adenosine uptake inhibitor activity
    • 喹唑啉和具有腺苷摄取抑制剂活性的酞嗪酮
    • US5648353A
    • 1997-07-15
    • US446235
    • 1995-05-22
    • Shigeki FujiwaraDaisuke MachiiHaruki TakaiHiromi NonakaHiroshi KaseKozo YaoMichiyo KawakageHideaki KusakaAkira Karasawa
    • Shigeki FujiwaraDaisuke MachiiHaruki TakaiHiromi NonakaHiroshi KaseKozo YaoMichiyo KawakageHideaki KusakaAkira Karasawa
    • C07D401/14C07D491/04C07D401/04A61K31/445A61K31/50A61K31/505
    • C07D401/14C07D491/04
    • The present invention relates to an adenosine uptake inhibitor and an agent for the myocardium protection or the prevention or treatment of inflammatory edema, comprising a 1,2,3,4-tetrahydro-2,4-dioxoquinazoline derivative represented by formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, alkenyl, or substituted or unsubstituted aralkyl; R.sup.2, R.sup.3, R.sup.4, and R.sup.5 independently represent hydrogen, halogen, amino, mono- or di(lower alkyl)amino, lower alkanoylamino, nitro, cyano, substituted or unsubstituted lower alkyl, hydroxy, lower alkoxy, lower alkylthio, carboxy, lower alkoxycarbonyl, lower alkanoyl, aralkyloxy, or lower alkanoyloxy; R.sup.6, R.sup.7, R.sup.8, and R.sup.9 independently represent hydrogen, hydroxy, substituted or unsubstituted lower alkoxy, or aralkyloxy, or any adjoining two of them are combined to form methylenedioxy; R.sup.10 represents hydrogen or lower alkyl; and Y and Z independently represent N or C--R.sup.11 (wherein R.sup.11 represents hydrogen, substituted or unsubstituted lower alkyl, or halogen),or a pharmaceutically acceptable salt thereof as an active ingredient.
    • 本发明涉及腺苷摄取抑制剂和用于心肌保护或预防或治疗炎性水肿的药剂,其包含由式(I)表示的1,2,3,4-四氢-2,4-二氧代喹唑啉衍生物: (I)其中R 1表示氢,取代或未取代的低级烷基,烯基或取代或未取代的芳烷基; R2,R3,R4和R5独立地表示氢,卤素,氨基,一或二(低级烷基)氨基,低级烷酰基氨基,硝基,氰基,取代或未取代的低级烷基,羟基,低级烷氧基,低级烷硫基,羧基,低级 烷氧基羰基,低级烷酰基,芳烷氧基或低级烷酰氧基; R 6,R 7,R 8和R 9独立地表示氢,羟基,取代或未取代的低级烷氧基或芳烷氧基,或者它们中的任何相邻的两个被结合形成亚甲二氧基; R 10表示氢或低级烷基; 并且Y和Z独立地表示作为活性成分的N或C-R11(其中R11表示氢,取代或未取代的低级烷基或卤素)或其药学上可接受的盐。