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    • 4. 发明授权
    • Condensed as-triazine derivatives and method of using the same
    • 缩合三嗪衍生物及其使用方法
    • US4419355A
    • 1983-12-06
    • US283971
    • 1981-07-16
    • Ibolya KosoczkyEva Toncsev, nee RavaszPal BenkoLaszlo PallosLujza PetoczSandor BatoriGyorgy HajosAndras MessmerKatalin Grasser
    • Ibolya KosoczkyEva Toncsev, nee RavaszPal BenkoLaszlo PallosLujza PetoczSandor BatoriGyorgy HajosAndras MessmerKatalin Grasser
    • C07D471/04A61K31/53A61P25/24A61P25/26C07D253/10C07D487/04C07D253/08
    • C07D487/04
    • The invention relates to new condensed as-triazine derivatives of the general formula (I) ##STR1## wherein Z represents a buta-1,3-dienyl group or a group of the formula (a), (b), (c) or (d) ##STR2## R.sub.1 denotes a C.sub.1-10 alkyl group, an oxo group or a C.sub.6-10 aryl or C.sub.6-10 aryl-(C.sub.1-3 alkyl) group optionally substituted by one or more identical or different substituents selected from the group consisting of amino, nitro, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy and halogen,R.sub.2 stands for hydrogen, C.sub.1-10 alkyl or amino,R.sub.3 represents hydrogen, C.sub.1-10 alkyl or C.sub.6-10 aryl or C.sub.6-10 aryl-(C.sub.1-3 alkyl) optionally substituted by one or more identical or different substituents selected from the group consisting of nitro, amino, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy and halogen,X.sup.- denotes an anion, andn is 0 or 1,with the proviso that if n is O, R.sub.1 is other than an oxo group and R.sub.1 ' and R.sub.2 ' form together a double bond, and with the further provisos that if n is 1, R.sub.1 represents an oxo group and the symbols R.sub.1 ' and R.sub.2 ' are not present, and if Z is a buta-1,3-dienyl group and R.sub.1 denotes an oxo group, R.sub.3 is other than unsubstituted phenyl.The new compounds of the general formula (I) can be prepared by cyclizing the compounds of the general formula (II) or (V), wherein R.sub.1, Z, R.sub.3 and X.sup.- have the above defined meanings, R.sub.4 is a leaving group and R.sub.7 represents hydrogen or C.sub.1-10 alkyl.The new compounds of the general formula (I) possess a valuable antidepressant effect and can advantageously be used in the therapy.
    • 本发明涉及通式(I)的新的缩合的三嗪衍生物,其中Z代表丁-1,3-二烯基或式(a),(b),( c)或(d)R1表示任选被一个或多个相同的C 1-6烷基,氧代基或C 6-10芳基或C 6-10芳基 - (C 1-3烷基) 或选自氨基,硝基,C 1-6烷基,C 1-6烷氧基,羟基和卤素的不同取代基,R 2代表氢,C 1-10烷基或氨基,R 3表示氢,C 1-10烷基或C 6- 芳基或任选被一个或多个相同或不同的选自硝基,氨基,C 1-6烷基,C 1-6烷氧基,羟基和卤素的取代基取代的芳基或C 6-10芳基 - (C 1-3烷基) 表示阴离子,n为0或1,条件是如果n为O,则R1不是氧代基,R1'和R2'一起形成双键,另外条件是,如果n为1, R1代表氧代基团, mbols R1'和R2'不存在,并且如果Z是丁-1,3-二烯基并且R 1表示氧代基,则R 3不是未取代的苯基。 通式(I)的新化合物可以通过使通式(II)或(V)的化合物环化来制备,其中R1,Z,R3和X具有上述定义,R4是离去基团, R 7表示氢或C 1-10烷基。 通式(I)的新化合物具有有价值的抗抑郁作用,可有利地用于治疗。
    • 10. 发明授权
    • 2-Hydroxymethyl-quinoxaline-1,4-dioxide derivatives, a process for
preparing same and compositions containing same
    • 2-羟甲基 - 喹喔啉-1,4-二氧化物衍生物,其制备方法和含有它们的组合物
    • US4511717A
    • 1985-04-16
    • US593204
    • 1984-03-27
    • Pal BenkoIldiko Ratz nee SimonekLaszlo PallosKaroly MagyarJeno KovacsErzsebet MatraiJanos GundelAlbert Balogh
    • Pal BenkoIldiko Ratz nee SimonekLaszlo PallosKaroly MagyarJeno KovacsErzsebet MatraiJanos GundelAlbert Balogh
    • A23K1/16A61K31/498A61P31/00C07D241/00C07D241/52C07D307/00C07D401/00C07D405/00A61K31/495C07D401/12C07D403/12
    • C07D241/52
    • The invention relates to new 2-hydroxymethyl-quinoxaline-1,4-dioxide derivatives of the general formula (I) ##STR1## wherein A represents an amino group, or a group of the general formula --NH--COOR.sub.1, wherein R.sub.1 stands for a C.sub.2-4 alkyl group, or a group of the general formula --NH--CX--NH.sub.2, whereinX denotes an oxygen or sulfur atom, or a group of the formula --NH--C(NH)--NH.sub.2, or a group of the general formula --NH--R.sub.2, wherein R.sub.2 represents a C.sub.1-6 alkyl, a phenyl, a benzyl, a hydroxyl or a hydroxy-(C.sub.2-4 alkyl) group, or a group of the general formula --NH--CO--R.sub.3, wherein R.sub.3 stands for a C.sub.1-20 alkyl group or a phenyl group optionally substituted by one, two or three identical or different substituent(s) selected from the group consisting of nitro, hydroxyl, amino, C.sub.1-3 alkoxy and halogen; a naphtyl group optionally substituted by a hydroxyl group, a phenyl-(C.sub.1-3 alkyl) group, a pyridyl, a piperidyl, a pyrazinyl, a pyrimidyl, a 1,2,4-triazinyl, a furyl, a nitrofuryl or an .alpha.,.alpha.-diphenyl-.alpha.-hydroxymethyl group.Due to their antimicrobial and weight-gain increasing effects, the new compounds of the general formula (I) can serve as active ingredients of pharmaceutical or veterinary compositions, particularly fodder concentrates, fodder additives and fodders.The invention relates also to the preparation of the new compounds of the general formula (I) and the compositions containing same.
    • PCT No.PCT / HU81 / 00038 Sec。 371日期1982年5月7日 102(e)日期1982年5月7日PCT提交1981年9月11日PCT公布。 出版物WO82 / 01001 日本1982年4月1日。本发明涉及通式(I)的新的2-羟甲基 - 喹喔啉-1,2-二氧化物衍生物,其中A表示氨基,或一般为 式-NH-COOR1,其中R1表示C2-4烷基,或通式为-NH-CX-NH2的基团,其中X表示氧或硫原子,或式-NH-C (NH)-NH 2或通式为-NH-R 2的基团,其中R 2表示C 1-6烷基,苯基,苄基,羟基或羟基 - (C 2-4烷基)基团,或一组 通式为-NH-CO-R3,其中R3代表C1-20烷基或任选被一个,两个或三个相同或不同的取代基取代的苯基,所述取代基选自硝基,羟基,氨基 ,C 1-3烷氧基和卤素; 任选被羟基取代的萘基,苯基 - (C 1-3烷基)基,吡啶基,哌啶基,吡嗪基,嘧啶基,1,2,4-三嗪基,呋喃基,硝基呋喃基或α ,α-二苯基-α-羟甲基。 由于其抗微生物和增重增加的作用,通式(I)的新化合物可用作药物或兽药组合物,特别是饲料浓缩物,饲料添加剂和饲料的有效成分。 本发明还涉及通式(I)的新化合物和含有其的组合物的制备。