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    Aromatic thioethers
    3.
    发明授权
    Aromatic thioethers 失效
    芳香硫醚

    公开(公告)号：US4785004A

    公开(公告)日：1988-11-15

    申请号：US941676

    申请日：1986-12-15

    Applicant: Andreas Von Sprecher ,  Werner Breitenstein ,  Andreas Beck ,  Robert W. Lang ,  Konrad Oertle

    Inventor： Andreas Von Sprecher ,  Werner Breitenstein ,  Andreas Beck ,  Robert W. Lang ,  Konrad Oertle

    IPC: C07D215/54 ,  C07D311/24 ,  C07C149/40 ,  A61K31/235

    CPC classification number: C07D311/24 ,  C07D215/54

    Abstract: Novel asymmetric thioethers of the formula ##STR1## in which the general symbols have the following meanings: R.sup.0 represents hydrogen or C.sub.1-7 -alkanoyl,R.sup.1 represents C.sub.1-3 -alkyl which may be substituted by one or more halogen atoms having an atomic number of at most 17,R.sup.2 represents an aliphatic radical having from 5 to 15 carbon atoms,A represents ethylene, a single bond or vinylene,B.sup.1 represents C.sub.1-7 -alkylene or phenylene,B.sup.2 represents a single bond, ethylene or phenylene, andM represents an aromatic radical of the partial formula ##STR2## in which the symbols have the following meanings: R.sup.3 represents hydrogen or C.sub.1-4 -alkyl,X represents NH, O, S or if R.sup.4 represents hydrogen, a single bond,one of the symbols R.sup.4 and R.sup.5 represents hydrogen and the other represents the group --CO--R.sup.6, orR.sup.4 and R.sup.5 together represent the radical --CO--C(R.sup.6).dbd.C(R.sup.7)--or--CO--C(R.sup.7).dbd.C(R.sup.6)--orR.sup.4 R.sup.5, together with X, represent the radical --N.dbd.C(R.sup.8)--C(R.sup.6).dbd.CH--,in whichR.sup.6 represents --(CH.sub.2).sub.b --COOR.sup.3 (in which b=0 to 2)R.sup.7 represents hydrogen or C.sub.1-4 -alkyl andR.sup.8 represents hydrogen, methyl, mythoxy or halogen,and their salts are active as leucotriene antagonists since they eliminate the contractions of smooth muscles brought about by leucotrienes, and are therefore suitable for the treatment of allergic, especially asthmatic, conditions.

    Abstract translation: 式（I）的新颖的不对称硫醚，其中通式符号具有以下含义：R 0表示氢或C 1-7 - 烷酰基，R 1表示可以被一个或多个具有 原子数最多为17，R 2表示具有5至15个碳原子的脂族基团，A表示乙烯，单键或亚乙烯基，B1表示C1-7 - 亚烷基或亚苯基，B2表示单键，乙烯或亚苯基 ，M表示部分结构式（M）的芳族基团，其中符号具有以下含义：R 3表示氢或C 1-4 - 烷基，X表示NH，O，S或如果R 4表示氢，则 单键，R4和R5之一表示氢，另一个表示-CO-R6基团，或R4和R5一起代表基团-CO-C（R6）= C（R7）-OR-CO-C（ R7）= C（R6） - 或R4R5与X一起代表基团-N = C（R8）-C（R6）= CH-，其中R6表示 - （CH2）b-COOR3（其中b = 0至2）R7表示氢或C1-4烷基，R8表示氢，甲基，乙氧基或卤素，并且它们的盐作为白三烯拮抗剂是有活性的，因为它们消除了由白三烯引起的平滑肌的收缩，因此适用于 治疗过敏，特别是哮喘，病情。

    Method for preparation of mercaptobenzoates
    6.
    发明授权
    Method for preparation of mercaptobenzoates 失效
    巯基苯甲酸酯的制备方法

    公开(公告)号：US4704467A

    公开(公告)日：1987-11-03

    申请号：US940995

    申请日：1986-12-12

    Applicant: Peter K. Wehrenberg

    Inventor： Peter K. Wehrenberg

    IPC: C07C20060101 ,  C07C317/44 ,  C07C149/40 ,  C07C147/14 ,  C07C147/107

    CPC classification number: C07C317/00 ,  C07C323/00

    Abstract: A method of preparing a compound of the formula ##STR1## wherein R is alkyl, R.sub.1 is alkyl or aryl and X is halogen or nitro comprising reacting ##STR2## wherein R and X are as defined above with a mercaptan having the formula R-SH in the presence of an inorganic base, a phase transfer catalyst and a non-polar aprotic solvent.

    Abstract translation: 一种制备下式化合物的方法，其中R是烷基，R 1是烷基或芳基，X是卤素或硝基，其中R和X如上所定义，与具有式R-SH的硫醇反应 在无机碱，相转移催化剂和非极性非质子溶剂的存在下进行。

    Process for producing phenolic thiocarboxylic esters
    7.
    发明授权
    Process for producing phenolic thiocarboxylic esters 失效
    酚类硫代羧酸酯的制备方法

    公开(公告)号：US4623745A

    公开(公告)日：1986-11-18

    申请号：US755383

    申请日：1985-07-16

    Applicant: Siegfried Rosenberger ,  Werner Stegmann

    Inventor： Siegfried Rosenberger ,  Werner Stegmann

    IPC: C09K15/14 ,  B01J31/02 ,  C07B61/00 ,  C07C67/00 ,  C07C313/00 ,  C07C319/00 ,  C07C319/14 ,  C07C323/52 ,  C10M135/26 ,  C10N30/08 ,  C10N30/10 ,  C07C149/40

    CPC classification number: C07C323/00

    Abstract: Compounds of the formula I ##STR1## wherein R.sup.1 and R.sup.2 independently of one another are each tert-butyl, R.sup.3 is C.sub.1 -C.sub.20 -alkyl, or C.sub.2 -C.sub.20 -alkyl interrupted by --O-- or --S--, and n is the number 1 or 2, can be obtained, with a very high degree of yield and purity, by reaction of a phenol of the formula II ##STR2## with formaldehyde and a mercaptan of the formula IIIR.sup.3 OOC--C.sub.n H.sub.2n --SH (III)in the presence of catalytic amounts of a primary or secondary amine. Such compounds are stabilizers for organic materials.

    Abstract translation: 其中R 1和R 2彼此独立的式I化合物（I）各自为叔丁基，R 3为C 1 -C 20 - 烷基或被-O-或-S-中断的C 2 -C 20 - 烷基，以及 通过将式II的苯酚（II）与甲醛和式III的三醇R 3 OOC-C n H 2n-n的硫醇反应，可以获得非常高的产率和纯度的n为1或2， SH（III）在催化量的伯胺或仲胺存在下反应。 这些化合物是有机材料的稳定剂。

    Substituted N-(.omega.-aroylpropionyl) derivatives of .alpha.-amino acids and esters thereof
    10.
    发明授权
    Substituted N-(.omega.-aroylpropionyl) derivatives of .alpha.-amino acids and esters thereof 失效
    α-氨基酸及其酯的取代的N-（ω-芳酰基丙酰基）衍生物

    公开(公告)号：US4435329A

    公开(公告)日：1984-03-06

    申请号：US312119

    申请日：1981-10-16

    Applicant: Francis J. McEvoy ,  Jay D. Albright

    Inventor： Francis J. McEvoy ,  Jay D. Albright

    IPC: C07D209/20 ,  C07C149/40 ,  C07C149/43 ,  C07C153/023

    CPC classification number: C07D209/20

    Abstract: Novel compounds are described having the formula ##STR1## wherein Z is ##STR2## R.sub.1 is hydrogen or a C.sub.1 -C.sub.4 lower alkyl; R.sub.2 is hydrogen, a C.sub.1 -C.sub.4 lower alkyl, hydroxy-R.sub.8 -, lower alkyl-R.sub.8 -, mercapto-R.sub.8 -, cyclohexyl, cyclopentyl, phenyl, phenyl-R.sub.8 -, indolyl-R.sub.8 -, carboxy-R.sub.8 -, amino-R.sub.8 - or carbamoyl-R.sub.8 -, wherein R.sub.8 - is a divalent C.sub.1 -C.sub.6 straight chain parafinic moiety; R.sub.3 is hydrogen or C.sub.1 -C.sub.4 lower alkyl; R.sub.4 is hydrogen, lower alkanoyl, benzoyl or phenyl-substituted-lower alkanoyl; R.sub.5 is hydrogen or a C.sub.1 -C.sub.4 lower alkyl; R.sub.1, R.sub.2 and R.sub.5 excluding tertiary butyl; ARYL is 1-naphthyl, 2-naphthyl, 4-chloro-1-naphthyl, 4-methoxy-1-naphthyl, 5,6,7,8-tetrahydro-1-naphthyl, 5,6,7,8-tetrahydro-2-naphthyl, 4-biphenylyl, 5-indanyl, 4-indanyl, phenyl, or substituted phenyl moieties having the formula ##STR3## wherein R.sub.6 is fluoro, chloro, bromo, trifluoromethyl, cyano, phenoxy, halophenoxy, phenylthio, halophenylthio, a C.sub.1 -C.sub.4 lower alkyl or a C.sub.1 -C.sub.4 lower alkoxy, and R.sub.7 is chloro, fluoro, bromo, a C.sub.1 -C.sub.4 lower alkyl or a C.sub.1 -C.sub.4 lower alkoxy; and where m is an integer of zero, one or two; including individual optically active isomers; racemic mixtures thereof; non-toxic pharmacologically-acceptable salts of the foregoing; and mixtures of the foregoing. Processes of preparing such compounds are also described. Such compounds are useful in ameliorating hypertension in mammals.

    Abstract translation: 描述了具有下式的新化合物：其中Z是R 1是氢或C 1 -C 4低级烷基; R2是氢，C1-C4低级烷基，羟基-R8-，低级烷基R8-，巯基-R8-，环己基，环戊基，苯基，苯基-R8-，吲哚基-R8-，羧基-R8-， R 8 - 或氨基甲酰基-R 8 - ，其中R 8为二价C 1 -C 6直链亚烷基部分; R3是氢或C1-C4低级烷基; R4是氢，低级烷酰基，苯甲酰基或苯基取代的低级烷酰基; R5是氢或C1-C4低级烷基; R1，R2和R5不包括叔丁基; ARYL是1-萘基，2-萘基，4-氯-1-萘基，4-甲氧基-1-萘基，5,6,7,8-四氢-1-萘基，5,6,7,8-四氢 - 2-萘基，4-联苯基，5-二氢化茚基，4-二氢化茚基，苯基或具有下式的取代的苯基部分：其中R6是氟，氯，溴，三氟甲基，氰基，苯氧基，卤代苯氧基，苯硫基，卤苯硫基， C1-C4低级烷基或C1-C4低级烷氧基，R7是氯，氟，溴，C1-C4低级烷基或C1-C4低级烷氧基; 并且其中m是零的整数，一个或两个; 包括单独的旋光异构体; 其外消旋混合物; 上述无毒的药理学上可接受的盐; 和上述的混合物。 还描述了制备这些化合物的方法。 这些化合物可用于改善哺乳动物的高血压。

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