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    Pyridine derivatives and intermediates thereof
    5.
    发明公开
    Pyridine derivatives and intermediates thereof 失效
    Pyridinderivate和Zwischenprodukte。

    公开(公告)号：EP0347831A2

    公开(公告)日：1989-12-27

    申请号：EP89111177.5

    申请日：1989-06-20

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： Suzuki, Koji ,  Obase, Hiroyuki ,  Karasawa, Akira ,  Shirakura, Shiro ,  Kubo, Kazuhiro ,  Miki, Ichiro ,  Ishii, Akio

    IPC分类号： C07D471/04 ,  C07D491/107 ,  C07D221/16 ,  A61K31/55 ,  A61K31/435

    CPC分类号： C07D471/04 ,  C07D221/16 ,  C07D491/10

    摘要： A pyridine derivative of formula

    wherein X¹-X² represents
    wherein
    wherein R⁴ represents hydrogen alkyl or a substituted or unsubstituted aralkyl; R⁵ reoresents a hydrogen, alkoxy or alkylthio and R⁶ and R⁸, which may be the same or different, each represent hydrogen, alkyl or alkenyl, R⁷ represents hydrogen or R⁶ and R⁷ are taken together to form
    wherein R⁹ represents alkyl; and m represents an integer of from 1 to 3; and any one of a, b, and c represents a nitrogen or an N-oxide (N→O), with the other two representing a carbon atom, which exhibits selective, potential, and long-lasting inhibitory activity on biosynthesis of thromboxane A₂ and is useful in the treatment and prevention of a broad range of diseases.

    摘要翻译： 式的吡啶衍生物，其中X 1 -X 2表示CHEM> CHEM，其中R 4表示氢烷基或取代或未取代的芳烷基; R 5表示氢，烷氧基或烷硫基，R 6和R 8可以相同或不同，各自表示氢，烷基或烯基，R 7表示氢或R 6，和 R 7一起形成，其中R 9表示烷基; m表示1〜3的整数， a，b和c中的任一个表示氮或N-氧化物（N-> O），另外两个表示碳原子，其表现出对凝血恶烷生物合成的选择性，潜在和持久的抑制活性 A2，可用于治疗和预防广泛的疾病。

    Novel piperidine derivatives and pharmaceutical compositions containing same
    6.
    发明公开
    Novel piperidine derivatives and pharmaceutical compositions containing same 失效
    新型哌啶衍生物和含有其的药物组合物

    公开(公告)号：EP0092391A3

    公开(公告)日：1984-09-26

    申请号：EP83302123

    申请日：1983-04-14

    申请人： KYOWA HAKKO KOGYO CO., LTD

    发明人： Teranishi, Masayuki ,  Obase, Hiroyuki ,  Nomoto, Yuji ,  Shuto, Katsuichi ,  Karasawa, Akira ,  Kasuya, Yutaka

    IPC分类号： C07D401/06 ,  C07D401/04 ,  A61K31/445 ,  C07D211/58 ,  C07D211/26

    CPC分类号： C07D401/04 ,  C07D211/26 ,  C07D211/58 ,  C07D401/06

    摘要： Novel piperidine derivatives are disclosed having hypotensive activity, as well as pharmaceutical preparations containing them. The novel compounds are of the formula
    wherein A is a hydroxyl group, a halogen atom, a C,-C 5 alkyl group, a C 1 -C 5 alkoxy group, a C 2 -C 5 alkenyloxy group, a C 1 -C 5 alkinyloxy group, a C 1 -C 5 alkylthio group, a carboxyl group, a C 1 -C 5 alkoxycarbonyl group, a nitro group, an amino group, a C 1 -C 5 alkylamino group, a C,-C 5 alkanoylamino group, a sulfamoyl group, a mono- or di- (C 1 -C 5 alkyl) aminosulfonyl group, a C 1 -C 5 alkylsulfonyl group, a carbamoyl group, a cyano group or a trifluoromethyl group; when m is 2 or more, A may be the same or different groups, or two A groups may combine to form a C,-C 5 alkylenedioxy group; m is 0 or an integer of 1-5; Q is a carbonyl group or a hydroxymethylene group; R is a hydrogen atom or an alkyl group having 1-4 carbon atoms; X and Y are defined as follows: i) when Y = H, X represents
    ii) when Y = CH 3 , X represents
    and when
    X represents a hydrogen atom and their pharmacologically acceptable acid addition salts.

    摘要翻译： 公开了具有降血压活性的新型哌啶衍生物，以及含有它们的药物制剂。 该新化合物具有式CHEM，其中A为羟基，卤原子，C1-C5烷基，C1-C5烷氧基，C7-C5链烯氧基，C1-C5烷氧基， C1-C5烷硫基，羧基，C1-C5烷氧基羰基，硝基，氨基，C1-C5烷基氨基，C1-C5烷酰基氨基，氨磺酰基，一或二（ C1-C5烷基）氨基磺酰基，C1-C5烷基磺酰基，氨基甲酰基，氰基或三氟甲基; 当m为2以上时，A可以相同或不同，或两个A基团可以结合形成C1-C5亚烷基二氧基; m为0或1-5的整数; Q是羰基或羟基亚甲基; R是氢原子或具有1-4个碳原子的醇酸基; X和Y定义如下：i）当Y = H时，X表示 ii）当Y = CH 3时，X表示，当Y = CHEM时，X表示氢原子及其药理学上可接受的酸加成盐 。

    Tricyclic compounds
    10.
    发明公开
    Tricyclic compounds 失效
    Tricyclische Verbindungen。

    公开(公告)号：EP0325755A1

    公开(公告)日：1989-08-02

    申请号：EP88120889.6

    申请日：1988-12-14

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： Oshima, Etsuo ,  Obase, Hiroyuki ,  Karasawa, Akira ,  Kubo, Kazuhiro ,  Miki, Ichiro ,  Ishii, Akio ,  Ishii, Hidee ,  Ohmori, Kenji

    IPC分类号： C07D313/12 ,  C07D337/12 ,  C07D211/10 ,  C07D333/34 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D409/14 ,  C07D409/12 ,  C07D471/10 ,  A61K31/445

    CPC分类号： C07D405/06 ,  C07D211/14 ,  C07D313/12 ,  C07D333/34 ,  C07D405/12 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D471/10

    摘要： Tricyclic compounds represented by formula (I):
    wherein

    represents single bond or double bond; X 1 -X 2 represents -CH 2 O-,
    wherein t represents 0, 1 or 2, -CH 2 -CH 2 -, or -CH=CH-; W represents -S-or = CH-; n is 1, 2, 3, or 4; one of R A and R B represents hydrogen and the other represents -Y-M wherein Y represents single bond, -CR 1 R 2 -(CH 2 ) m -, or -CR 1 =CR 2 -(CH 2 ) m wherein each of R 1 and R 2 independently represents hydrogen or lower alkyl and m is 0, 1, 2, 3 or 4, in which the left side of each formula is bound to the mother nucleus; and M represents -COOR 3 wherein R 3 represents hydrogen or lower alkyl, -CONR 3a R 3b wherein each of R 3a and R 3b independently has the same significances for R 3 as described above, or tetrazolyl; each of G A and G B independently represents lower alkyl, halogen, hydroxyl, or lower alkoxyl; each of g A and g B independently represents 0, 1, 2 or 3; Z represents N-E 1 -Q wherein E 1 represents single bond, -CO-, -COO- wherein the left side of the formula is bound to the nitrogen atom, or -S0 2 -; and Q represents optionally substituted aryl, optionally substituted aralkyl, optionally substituted aralkenyl, aromatic heterocyclic group, or

    wherein L represents hydrogen, hydroxyl, or lower alkoxy; E 2 represents single bond, -CO-, or - wherein R 4 represents hydrogen or lower alkyl; and Q has the same significance as described above; C = CH-Q wherein Q has the same significance as described above; or
    p is 1, 2 or 3; possess a potent antagonizing action against thromboxane A 2 and also an antiallergic and/or antihistaminic activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.

    摘要翻译： 由式（I）表示的三环化合物：其中----表示单键或双键; X1-X2表示-CH2O-，，其中l代表0,1或2，-CH2-CH2-或-CH = CH-; W表示-S-或= CH-; n为1,2,3或4; R A和R B之一表示氢，另一个表示-YM，其中Y表示单键，-CR 1 R 2 - （CH 2）m - 或-CR 1 = CR < 2 - （CH 2）m，其中R 1和R 2各自独立地表示氢或低级烷基，m是0,1,2,3或4，其中每个式的左侧与 母核; 并且M表示-COOR 3，其中R 3表示氢或低级烷基-CONR 3a R 3b，其中R 3a和R 3b各自独立地对R 3表示相同的含义， 如上所述，或四唑基; G A和G B各自独立地表示低级烷基，卤素，羟基或低级烷氧基; g 和g p为1,2或3; 对血栓素A2具有有效的拮抗作用，还具有抗过敏和/或抗组胺活性，预期对缺血性疾病，脑血管疾病等具有预防和治疗作用。