Diaryl-p-phenylenediamine disulfides
    1.
    发明公开
    Diaryl-p-phenylenediamine disulfides 有权
    二芳基对苯二胺二硫化物

    公开(公告)号:EP1186595A1

    公开(公告)日:2002-03-13

    申请号:EP01119793.6

    申请日:2001-08-28

    摘要: The present invention relates to mixed diaryl-p-phenylenediamine disulfides and its use in compounds. The mixed diaryl-p-phenylenediamine are of the formula


    and mixtures thereof wherein R 1 and R 2 are each independently selected from the group consisting of hydrogen and alkyls having from 1 to 8 carbon atoms.

    摘要翻译: 本发明涉及混合的二芳基 - 对苯二胺二硫化物及其在化合物中的用途。 混合的二芳基 - 对苯二胺具有下式和其混合物:其中R 1和R 2各自独立地选自氢和具有1至8个碳原子的烷基。

    PROCESSES FOR PRODUCING THIOARYL COMPOUND
    4.
    发明公开
    PROCESSES FOR PRODUCING THIOARYL COMPOUND 失效
    VERFAHRENFÜRDIE DARSTELLUNG VON THIOARYLVERBINDUNGEN

    公开(公告)号:EP0700901A1

    公开(公告)日:1996-03-13

    申请号:EP95912435.5

    申请日:1995-03-17

    摘要: A process for producing an alkali metal salt of an arylmercaptan compound represented by general formula (3), by the reaction of a disulfide compound represented by general formula (1) with a hydroxide of an alkali metal M¹ in the presence of a sulfur compound represented by the general formula (2): H(2-i)S(M¹)i, another process for producing an alkoxycarbonylalkylthioaryl compound represented by general formula (5) by the reaction of the alkali metal salt of an arylmercaptan compound obtained above with a halogenated fatty acid ester represented by the general formula (4): X¹-R²-COOR³ at a pH of 7 to 10; and still another process for producing the alkoxycarbonylalkylthioaryl compound by the reaction of the disulfide compound with the hydroxide of an alkali metal M¹ in the presence of the sulfur compound, followed by the reaction of the obtained alkali metal salt of an arylmercaptan compound, without being isolated, with the halogenated fatty acid ester under the same condition.

    摘要翻译: 一种由通式(3)表示的芳基硫醇化合物的碱金属盐的制备方法,通过通式(1)表示的二硫化物与碱金属M 1的氢氧化物在 由通式(2)表示的硫化合物:H(2-i)S(M 1)i,通过通式(5)所示的碱金属盐的反应制备由通式(5)表示的烷氧基羰基烷基硫代芳基化合物的另一种方法 在通式(4)表示的卤代脂肪酸酯:X 1 -R 2 -COOR 3,pH7〜10的条件下,得到上述得到的芳基硫醇化合物; 以及在硫化合物的存在下通过二硫化物与碱金属M 1的氢氧化物的反应制备烷氧基羰基烷基硫代芳基化合物的另一种方法,随后将所得的芳基硫醇化合物的碱金属盐, 在不同的条件下与卤代脂肪酸酯分离。

    Method for producing aminothiophenols and their derivatives
    7.
    发明公开
    Method for producing aminothiophenols and their derivatives 失效
    Verfahren zur Herstellung von Aminothio phenolen und deren Derivate。

    公开(公告)号:EP0269434A1

    公开(公告)日:1988-06-01

    申请号:EP87310404.6

    申请日:1987-11-25

    CPC分类号: C07C333/02

    摘要: A method is provided for preparing N-acyl-aminothiophenols, e.g., N-acetyl-para-aminothiophenol, or aminothiophenols, e.g., para-aminothiophenol, by reacting any of certain sulfur-containing ketones, viz., an S-(acylaryl) N,N-di(organo)thiocarbamate, e.g., S-(4'-acetophenyl)-N,N-dimethylthiocarbamate, an acylthiophenol acylate ester, e.g., 4-acetothiophenol acetate, or a free acylthiophenol, e.g., 4-acetothiophenol with hydroxylamine or a hydroxylamine salt, to form the oxime of the ketone, subjecting the oxime to a Beckmann rearrangement in the presence of a catalyst to form an S-(N-acyl-aminoaryl) N,N-di(organo)thiocarbamate, e.g., S-(N-acetyl-para-aminophenyl) N,N-dimethylthiocarbamate, an N,S-diacylaminothiophenol, e.g., N,S-diacetyl-para-aminothiophenol, or an N-acyl aminothiophenol, e.g., N-acetyl-para-amino- thiophenol, respectively. The S-(N-acyl-aminoaryl) N,N-di(organo)thiocarbamate may be hydrolyzed to the N-acyl amino- thiophenol or aminothiophenol. The S-(acylaryl) N,N-di(organo)thiocarbamate may be produced by reacting a hydroxy aromatic ketone, e.g., 4-hydroxyacetophenone (4-HAP) with an N,N-di(organo)thiocarbamoyl halide, e.g., N,N-dimethylthiocar- bamoyl chloride (DMTC) to form an O-(acylaryl) N,N-di(organo)thiocarbamate, e.g., O-(4'-acetophenyl) N,N-dimethylthiocarbamate, and pyrolytically rearranging the latter compound. The acylthiophenol may be produced by hydrolyzing the S-(acylaryl) N,N-di(organo)thiocarbamate.

    摘要翻译: 提供了通过使任何某些含硫酮,即S-(酰基芳基)酮与任何含硫的酮反应来制备N-酰基 - 氨基噻吩酚的方法,例如N-乙酰基 - 对氨基苯硫酚或氨基硫酚,例如对氨基苯硫酚, N,N-二(有机)硫代氨基甲酸酯,例如S-(4'-乙酰苯基)-N,N-二甲基硫代氨基甲酸酯,酰基硫酚
    酯酰化酯,例如4-乙酰硫苯硫酚乙酸酯或游离酰基苯硫酚,例如4-乙酰硫酚 羟胺或羟胺盐,形成酮的肟,在催化剂存在下使肟进行贝克曼重排,形成S-(N-酰基 - 氨基芳基)N,N-二(有机)硫代氨基甲酸酯,例如 ,N-(N-乙酰基对氨基苯基)N,N-二甲基硫代氨基甲酸酯,N,S-二酰基氨基苯硫酚,例如N,S-二乙酰基对氨基苯硫酚或N-酰基氨基苯硫酚, 对氨基苯硫酚。 可以将N-(N-酰基 - 氨基芳基)N,N-二(有机))硫代氨基甲酸酯水解成N-酰基氨基苯硫酚或氨基苯硫酚。 S-(酰基芳基)N,N-二(有机))硫代氨基甲酸酯可以通过使羟基芳族酮例如4-羟基苯乙酮(4-HAP)与N,N-二(有机)硫代氨基甲酰卤反应来制备, N,N-二甲基硫代氨基甲酰氯(DMTC)以形成O-(酰基芳基)N,N-二(有机))硫代氨基甲酸酯,例如O-(4'-乙酰苯基)N,N-二甲基硫代氨基甲酸酯,并热解重新排列后一种化合物。 酰基苯硫酚可以通过水解S-(酰基芳基)N,N-二(有机))硫代氨基甲酸酯来制备。

    MATRIX METALLOPROTEINASE INHIBITORS
    9.
    发明公开
    MATRIX METALLOPROTEINASE INHIBITORS 有权
    MATRIX METALLOPROTEASE INHIBITOREN

    公开(公告)号:EP1654213A1

    公开(公告)日:2006-05-10

    申请号:EP04739544.7

    申请日:2004-06-01

    摘要: Compounds of formula (1): Wherein: Q represents an optionally substituted 5- or 6-membered aryl or heteroaryl ring; X represents 0, S, NR5 or CR6 R7; Y represents CHOH, CHSH, NOR8, CNR8 or CNOR8; Z represents a bond, CR10 R11, 0,S,S0,S02, NR10, OCR10R11, CR10R11O or Z, R4 and Q together form an optionally substituted fused tricyclic group; R1, R1’, R3 and R3 each independently represents H, C1-6 alkyl or C1-4 alkylaryl; R2 represents C02 R8, CONR5OR9 or NR5 COR9; R4 represents optionally substituted 5- or 6-membered aryl or heteroaryl; R5 represents H or C1-3 alkyl; R6 and R7 each independently represents H, C1-3 alkyl or halo; R8 represents H or C1-2 alkyl; R9 represents H or C1-3 alkyl; R10 and R11 each independently represents H, C1-6 alkyl or C1-4 alkylaryl; and physiologically functional derivatives thereof, processes for their preparation, pharmaceutical formulations containing them and their use as inhibitors of matrix metal loproteinase enzymes (MMPs) are described.

    摘要翻译: 式(I)化合物:其中:Q表示任选取代的5或6元芳基或杂芳基环; X表示O,S,NR 5或CR 6 R 7; Y代表CHOH,CHSH,NOR 8,CNR 8或CNOR 8; Z表示键,CR 10,O,S,SO,SO 2,NR 10, OCR 10,10,11,10,10,10或10,其中R 4,R 4, 和Q一起形成任选取代的稠合三环基团; R 1,R 1,R 3,R 3和R 3'各自独立地表示H,C 1, 1-6烷基或C 1-4烷基芳基; R 2表示CO 2 R 8,CONR 5或9或NR 9, SUP> 5 COR 9 ; R 4表示任选取代的5或6元芳基或杂芳基; R 5表示H或C 1-3烷基; R 6和R 7各自独立地表示H,C 1-3烷基或卤素; R 8表示H或C 1-12烷基; R 9表示H或C 1-3烷基; R 10和R 11各自独立地表示H,C 1-6烷基或C 1-4烷基芳基; 和其生理功能衍生物,其制备方法,含有它们的药物制剂及其作为基质金属蛋白酶(MMP)抑制剂的用途。