NITROSO DERIVATIVES OF DIPHENYLAMINE
    81.
    发明申请
    NITROSO DERIVATIVES OF DIPHENYLAMINE 审中-公开
    二苯胺的硝基衍生物

    公开(公告)号:WO2005051896A1

    公开(公告)日:2005-06-09

    申请号:PCT/EP2004/014892

    申请日:2004-11-17

    IPC分类号: C07C243/06

    摘要: The invention relates to a compound of the formula (I) in which: - R 1 represents, independently of each other, a halogen atom; an aliphatic hydrocarbon-based group optionally substituted and/or optionally interrupted by one or more oxygen or sulfur atoms; a nitro group; a cyano group; an amino group; a mono- or dialkylamino group; an alkylcarbonyl group; a carboxyl group; an alkylcarbonylamino group; an alkylsulfonyl group; - R 2 represents, independently of each other, a cyano group; a hydroxyl group, an alkylcarbonyl group; a carboxyl group; an alkoxycarbonyl group; an unsubstituted amide group; or a linear or branched alkyl group substituted by a cyano, hydroxyl, carboxyl, alkoxycarbonyl or unsubstituted amide group; - i and j independently being 1 to 5, with the exclusion of the compound for which i and j = 1 and R 1 = carboxyl and R 2 = alkoxycarbonyl or R 1 = CF 3 and R 2 = carboxyl, and also the pharmaceutically acceptable derivatives, salts, solvates and stereoisomers thereof, including mixtures thereof in all proportions.

    摘要翻译: 本发明涉及式(I)的化合物,其中:-R 1彼此独立地表示卤素原子; 任选被一个或多个氧或硫原子取代和/或任选地中断的脂族烃基; 硝基; 氰基; 氨基; 单或二烷基氨基; 烷基羰基; 羧基; 烷基羰基氨基; 烷基磺酰基; -R 2彼此独立地表示氰基; 羟基,烷基羰基; 羧基; 烷氧基羰基; 未取代的酰胺基; 或被氰基,羟基,羧基,烷氧基羰基或未取代的酰胺基取代的直链或支链烷基; - i和j独立地为1至5,排除i和j = 1且R1 =羧基和R2 =烷氧基羰基或R1 = CF3和R2 =羧基的化合物,以及其药学上可接受的衍生物,盐,溶剂合物 其立体异构体,包括其各种比例的混合物。

    PROCESS FOR THE PREPARATION OF 2-[ALKYL(ARYL)]SULFONYLBENZENE-SULFONYL CHLORIDES AND THEIR INTERMEDIATES
    86.
    发明申请
    PROCESS FOR THE PREPARATION OF 2-[ALKYL(ARYL)]SULFONYLBENZENE-SULFONYL CHLORIDES AND THEIR INTERMEDIATES 审中-公开
    制备2- [烷基(芳基)]磺酰苯磺酰氯及其中间体的方法

    公开(公告)号:WO2003040087A1

    公开(公告)日:2003-05-15

    申请号:PCT/US2002/034900

    申请日:2002-10-31

    申请人: WYETH

    IPC分类号: C07C315/00

    摘要: A process for the preparation of 2-[alkyl(aryl)]sulfonylbenzene sulfonyl chlorides of the formula (I), in which R is alkyl or aryl substituted at the ortho or meta positions with alkyl, aryl, NHAc or alkoxy, comprising the steps of: a) reacting 2-chloronitrobenzene, 2-fluoronitrobenzene or 2-bromonitrobenzene with a compound of the following formula: RSO 2 - M + wherein R is defined above; and M is sodium, potassium, lithium, ammonium or quaternary ammonium, in a polar aprotic solvent at a temperature of about 50 to 190°C; b) reacting the material prepared in step (a) with hydrogen at a pressure of about 20 to about 60 psi in a polar aprotic solvent at a temperature of about 20 to about 60°C; and c) diazotizing the material prepared in step (b) with sodium nitrite in the presence of hydrochloric acid and reacting the resulting diazonium salt with sulfur dioxide in the presence of copper (I) or copper (II) compounds or a mixture thereof, in water.

    摘要翻译: 一种制备式(I)的2- [烷基(芳基)]磺酰基磺酰氯的方法,其中R是在邻位或间位被烷基,芳基,NHAc或烷氧基取代的烷基或芳基,包括步骤 :a)使2-氯硝基苯,2-氟硝基苯或2-溴硝基苯与下式化合物反应:其中R定义如上: 和M是钠,钾,锂,铵或季铵,在极性非质子溶剂中在约50至190℃的温度下进行; b)使步骤(a)中制备的材料在约20至约60psi的压力下在约20至约60℃的温度下在极性非质子溶剂中反应; 和c)在盐酸存在下,用亚硝酸钠在步骤(b)中制备的材料重氮化,并在铜(I)或铜(II)化合物或其混合物的存在下,使得到的重氮盐与二氧化硫反应, 水。

    ARYLHYDRAZONE DERIVATIVES USEFUL AS ANTIBACTERIAL AGENTS
    89.
    发明申请
    ARYLHYDRAZONE DERIVATIVES USEFUL AS ANTIBACTERIAL AGENTS 审中-公开
    ARYLHYDRAZONE衍生物可用作抗菌剂

    公开(公告)号:WO1997009878A1

    公开(公告)日:1997-03-20

    申请号:PCT/US1996015311

    申请日:1996-09-13

    IPC分类号: A01N37/34

    摘要: The subject invention provides arylhydrazone compounds having formula (I), wherein A and B are independently aryl or heteroaryl and A and B independently are substituted with at least one group selected from alkyl, halogen, CN, COOR , NR R , CONR R , NO2, SR , SOR , SO2R , NHCOR , NHSO2R , OR , hydroxyalkyl, and aminoalkyl. The compounds of this invention are useful for treating a wide variety of bacterial infections, including diseases of the skin, e.g., acne and skin ulcers, gastroenteritis, colitis, meningitis, keratinitis, conjunctivitis, diseases of the urinary and genital tracts, etc.

    摘要翻译: 本发明提供具有式(I)的芳基腙化合物,其中A和B独立地为芳基或杂芳基,A和B各自独立地被至少一个选自烷基,卤素,CN,COOR 7,NR 7, R 8,CONR 7 R 8,NO 2,SR 7,SOR 7,SO 2 R 7,NHCOR 7,NHSO 2 R 7,OR 7,羟烷基和氨基烷基 。 本发明的化合物可用于治疗各种细菌感染,包括皮肤疾病,例如痤疮和皮肤溃疡,胃肠炎,结肠炎,脑膜炎,角化炎,结膜炎,泌尿系和生殖道疾病等。

    AROMATIC SULPHONYL COMPOUNDS HAVING AN ADDITIONAL THIOETHER, SULPHOXIDE OR SULPHONYL GROUP
    90.
    发明申请
    AROMATIC SULPHONYL COMPOUNDS HAVING AN ADDITIONAL THIOETHER, SULPHOXIDE OR SULPHONYL GROUP 审中-公开
    芳香族磺酰一个附加硫醚,亚砜或磺酰HAVING

    公开(公告)号:WO1997003955A1

    公开(公告)日:1997-02-06

    申请号:PCT/EP1996002929

    申请日:1996-07-04

    IPC分类号: C07C323/65

    摘要: Sulfonyl compounds of formula (I) in which n is 0, 1 or 2; Y is vinyl or a radical of the formula C2H4Q, where Q is hydroxy or a group separable in alkaline reaction conditions; E is C3-C6 alkylene which may be interrupted by 1 or 2 oxygen atoms in the ether function; Ar is the radical of benzole or naphthalene; and R , R and R are hydrogen, possibly substituted C1-C6 alkyl, C1-C6 alkoxy, hydroxy, halogen, nitro, possibly substituted amino, hydroxysulphonyl, carboxyl, possibly substituted carbamoyl, possibly substituted sulphamoyl, cyano or a radical of the formula (NH-)m(CH2)qSO2-Y, where m is 0 or 1 and q is 0, 2 or 3 and Y has the meaning given above.

    摘要翻译: 式(I),其中n为0,1或2的磺酰基化合物中,Y为乙烯基或下式基团C2H4Q的,其中Q是羟基或者在碱性反应条件下基团E C3-C6亚烷基的可拆卸,其被1或2 氧原子的醚功能中,Ar基团的苯或萘,和R <1>,R <2>和R <3>为氢,任选取代的C1-C6-烷基,C1-C6烷氧基,羟基,卤素,硝基的 ,任选取代的氨基,羟基磺酰基,羧基,任选取代的氨基甲酰基,任选取代的氨磺酰基,氰基或下式基团的(NH - )M(CH 2)qSO2-Y,其中m是0或1,q为0,2或3 和Y具有上述含义,意思。