Tricyclic compounds and intermediates thereof
    1.
    发明公开
    Tricyclic compounds and intermediates thereof 失效
    Tricyclische Verbindungen und ihre Zwischenprodukte。

    公开(公告)号:EP0497201A1

    公开(公告)日:1992-08-05

    申请号:EP92101012.0

    申请日:1992-01-22

    摘要: Disclosed is a tricyclic compound represented by the formula (I):

    wherein each of R¹, R², R³ and R⁴ independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR⁹R¹⁰CO₂R¹¹ (wherein each of R⁹, R¹⁰ and R¹¹ independently represents hydrogen or C1-6 alkyl) or CONR¹²R¹³ (wherein each of R¹² and R¹³ independently represents hydrogen or C1-6 alkyl); R⁵ represents hydrogen or C1-6 alkyl; each of R⁶, R⁷ and R⁸ independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y¹-Y² represents CH₂-O, CH₂-S(O) n , (wherein n represents 0, 1, or 2), CH₂CH₂, CH=CH or CON(R¹⁴) (wherein R¹⁴ represents hydrogen or C1-6 alkyl) and Z represents oxygen or sulfur, or a pharmaceutically acceptable salt thereof. The compound possesses an acyl coenzyme A: cholesterol acyltransferase-inhibiting activity, and thus are expected to have preventive and therapeutic effects on hyperlipemia and arteriosclerosis.

    摘要翻译: 公开了由式(I)表示的三环化合物:其中R 1,R 2,R 3和R 4各自独立地表示氢,C 1-6烷基,C 1-6 烷氧基,C 1-6烷硫基,氨基,C 1-6烷基氨基,卤代C 1-6烷基,卤代C 1-6烷氧基,卤素,硝基,氰基,羧基,C 1-6烷氧基羰基,羟甲基,CR 9 R 1, (其中R 9,R 1,O和R 1各自独立地表示氢或C 1-6烷基)或CONR 1 2 R 1(3)其中R 1和R 2各自独立地表示氢或C 1-6烷基)。 R 5表示氢或C 1-6烷基; R 6,R 7和R 8各自独立地表示氢,C 1-6烷基,羟基,C 1-6烷氧基,C 1-6烷酰氧基,C 1-6烷硫基,氰硫基或卤素; X表示CH或N; Y 1 -Y 2表示CH 2 -O,CH 2 -S(O)n,(其中n表示0,1或2),CH 2 CH 2,CH = CH或CON(R 1 4) (其中R 1 4代表氢或C 1-6烷基),Z代表氧或硫,或其药学上可接受的盐。 该化合物具有酰基辅酶A:胆固醇酰基转移酶抑制活性,因此预期对高脂血症和动脉硬化具有预防和治疗作用。

    Hexitol derivatives
    2.
    发明公开
    Hexitol derivatives 失效
    Hexitolderivate。

    公开(公告)号:EP0393574A2

    公开(公告)日:1990-10-24

    申请号:EP90107245.4

    申请日:1990-04-17

    CPC分类号: C07D493/04

    摘要: Disclosed are hexitol derivatives represented by the general formula (I):
    wherein
    Q represents a formula
    wherein a represents NH, O or S,
    each of b , c and d independently represents CH or N,
    each of R¹, R², R³ and R⁴ independently represents hydrogen, lower alkyl, trifluoromethyl, aryl, lower alkanoyloxy, amino, lower alkylamino, lower alkanoylamino, lower alkanoyl, aroyl, halogen, nitro, (CH₂) m OR⁷, (CH₂) m SR⁷, (CH₂) m CO₂R⁷ where R⁷ represents hydrogen or lower alkyl and m represents an integer of 0 to 3,
    each of R⁵ and R⁶ independently represents hydrogen or lower alkyl,
    wherein each of Y¹ and Y² independently represents hydrogen, lower alkyl, hydroxyl, lower alkanoyloxy, nitrile or phenyl; or Y¹ and Y² are combined together to form oxygen,
    each of Y³ and Y⁴ independently represents hydrogen or lower alkyl, and ℓ is an integer of 0 to 6, and where ℓ is an integer of 2 to 6, each
    may be the same or different,
    Z represents hydrogen or nitro, and, n is 2 or 3 or a pharmaceutically acceptable salt thereof. The compounds show prominent coronary vasodilative activities, and are useful in treating angina pectoris and myocardial infarction.

    摘要翻译: 公开了由通式(I)表示的己糖醇衍生物:其中Q表示式CHEM,其中a表示NH,O或S,b,c和d各自独立地表示CH或N, 1,R 2,R 3和R 4独立地表示氢,低级烷基,三氟甲基,芳基,低级烷酰氧基,氨基,低级烷基氨基,低级烷酰基氨基,低级烷酰基,芳酰基,卤素,硝基, )mOR 7,(CH 2)m SR 7,(CH 2)m CO 2 R 7,其中R 7表示氢或低级烷基,m表示0〜3的整数,R 5和R 5, 6>独立地表示氢或低级烷基,CHEM,其中Y 1和Y 2各自独立地表示氢,低级烷基,羟基,低级烷酰氧基,腈或苯基; 或Y 1和Y 2组合在一起形成氧,Y 3和Y 4各自独立地表示氢或低级烷基,l是0-6的整数,其中l是 2〜6的整数,每个可以相同或不同,Z表示氢或硝基,n为2或3或其药学上可接受的盐。 该化合物显示出显着的冠状动脉血管扩张活性,可用于治疗心绞痛和心肌梗死。

    Phosphorus-containing peptide derivative
    4.
    发明公开
    Phosphorus-containing peptide derivative 失效
    磷光体吸附剂Peptidderivat。

    公开(公告)号:EP0103867A1

    公开(公告)日:1984-03-28

    申请号:EP83109190.5

    申请日:1983-09-16

    摘要: A phosphorus-containing peptide derivative represented by the general formula [I]:
    {wherein R, is hydrogen, lower alkyl, lower alkoxycarbonyl, aralkyloxycarbonyl or
    [wherein R e is hydrogen, alkyl having 1 to 17 carbon atoms, unsubstituted or substituted aryl (wherein the substituent is selected from lower alkyl, lower alkoxy and halogen), unsubstituted or substituted aralkyl (wherein the substituent is selected from lower alkyl, lower alkoxy and halogen), or cycloalkyl having 5 or 6 carbon atoms]; R 2 is hydrogen, unsubstituted or substituted lower alkyl (wherein the substituent is selected from amino, mercapto, lower alkylthio, carboxyl, hydroxyl, guanidino and imidazolyl), unsubstituted or substituted aryl (wherein the substituent is selected from amino, hydroxyl, lower alkoxy, aralkyloxy, lower alkyl, halogen and nitro), unsubstituted or substituted aralkyl (wherein the substituent is seiected from amino, lower alkyl halogen and nitro) or

    (wherein R 7 has the same meaning as R 3 ); R 3 is hydrogen, lower alkyl, unsubstituted or substituted aralkyl (wherein the substituent has the same meaning as in R e ), R 8 -CO-(wherein R 8 has the same meaning as R e ), R 9 -O-CO-[wherein R 9 is lower alkyl, unsubstituted or substituted aryl (wherein the substituent has the same meaning as in R e ), unsubstituted or substituted aralkyl (wherein the substituent has the same meaning as in R 8 )], or R 9 NHCO- (wherein R 9 has the same meaning as defined above); and R 4 and R 5 are the same or different, and are hydrogens, alkyls having 1 to 18 carbon atoms, unsubstituted or substituted aryl (wherein the substituent has the same meaning as in R e ), unsubstituted or substituted aralkyl (wherein the substituent has the same meaning as in R 6 ), -(CH 2 CH 2 O) m CH 3 (wherein m is an integer of 1 - 4), or -CH[CH 2 OCO(CH 2 ) n CH 3 ] 2 (wherein n is 0 or an integer of 1 - 10) }, and pharmacologically acceptable salts thereof is prepared. Said compounds have an angiotensin converting enzyme-inhibiting action and as the result an anti-hypertensive action.

    摘要翻译: 由通式[I]表示的含磷肽衍生物:... ... {其中R1是氢,低级烷基,低级烷氧基羰基,芳烷氧基羰基或...... R6- [... [其中R6是氢,具有1 至17个碳原子,未取代或取代的芳基(其中取代基选自低级烷基,低级烷氧基和卤素),未取代或取代的芳烷基(其中取代基选自低级烷基,低级烷氧基和卤素)或具有5或 6个碳原子]; R2是氢,未取代或取代的低级烷基(其中取代基选自氨基,巯基,低级烷硫基,羧基,羟基,胍基和咪唑基),未取代或取代的芳基(其中取代基选自氨基,羟基,低级烷氧基, 芳烷氧基,低级烷基,卤素和硝基),未取代或取代的芳烷基(其中取代基选自氨基,低级烷基,卤素和硝基)或...(其中R7具有与R3相同的含义)。 R3是氢,低级烷基,未取代或取代的芳烷基(其中取代基与R6相同),R8-CO-(其中R8与R6相同),R9-O-CO- [其中R9较低 烷基,未取代或取代的芳基(其中取代基具有与R6相同的含义),未取代或取代的芳烷基(其中取代基具有与R 6相同的含义)]或R9NHCO-(其中R9具有与上述相同的含义 ); 并且R 4和R 5相同或不同,并且是氢,具有1至18个碳原子的烷基,未取代或取代的芳基(其中取代基具有与R 6相同的含义),未取代或取代的芳烷基(其中取代基具有相同 意义如R6)中, - (CH2CH2O)m CH3(其中m为1-4的整数)或CH [CH 2 OCO(CH 2)n CH 3] 2(其中n为0或1-10的整数)}, 并制备其药理学上可接受的盐。 所述化合物具有血管紧张素转化酶抑制作用,结果是抗高血压作用。

    S-triazolo[3,4-i]purine derivatives
    8.
    发明公开
    S-triazolo[3,4-i]purine derivatives 失效
    5三唑并(3,4-i)的purinderivate。

    公开(公告)号:EP0417790A2

    公开(公告)日:1991-03-20

    申请号:EP90117662.8

    申请日:1990-09-13

    CPC分类号: C07D471/14

    摘要: There are disclosed s-triazolo[3,4-i]purine derivatives represented by formula:

    wherein Y-Z represents

    where R⁴ represents hydrogen, alkyl, substituted or unsubstituted aromatic heterocyclic group or substituted or unsubstituted aryl; and X² represents oxygen, sulfur or NH; each of R¹ and R² independently represents hydrogen, alkyl, cycloalkyl, aralkyl or substituted or unsubstituted aryl; R³ represents alkyl, cycloalkyl, aralkyl or substituted or unsubstituted aryl; X¹ represents oxygen or sulfur; and
    represents a single bond or a double bond or pharmaceutically acceptable salts thereof.

    摘要翻译: 公开了由式:表示的三唑并[3,4-i]嘌呤衍生物,其中Y-Z表示,其中R 4表示氢,烷基,取代或未取代的芳族杂环基或取代或未取代的芳基; X 2表示氧,硫或NH; R 1和R 2各自独立地表示氢,烷基,环烷基,芳烷基或取代或未取代的芳基; R 3表示烷基,环烷基,芳烷基或取代或未取代的芳基; X 1表示氧或硫; 和表示单键或双键或其药学上可接受的盐。

    Xanthine compounds
    9.
    发明公开
    Xanthine compounds 失效
    Xanthinverbindungen。

    公开(公告)号:EP0415456A2

    公开(公告)日:1991-03-06

    申请号:EP90116791.6

    申请日:1990-08-31

    摘要: Novel xanthine compounds represented by the following formula:
    wherein each of R¹, R² and R³ independently represents a hydrogen atom or a lower alkyl group;
    each of X¹ and X² independently represents an oxygen or sulfur atom;
    represents a single bond or a double bond;
    Y represents a single bond or an alkylene group, n represents 0 or 1, each of W¹ and W² independently represents a hydrogen atom, a lower alkyl or amino group, Z represents -CH₂-, -O-, -S- or -NH-residues; provided that when Q is
    then R¹, R² and R³ are not simultaneously methyl; and physiologically acceptable salts thereof have a diuretic effect, a renal-protecting effect and/or a bronchodilatory effect.
    The compounds are useful as a diuretic, a renal-­protecting agent and /or bronchodilator.

    摘要翻译: 由下式表示的新型黄嘌呤化合物:其中R 1,R 2和R 3各自独立地表示氢原子或低级烷基; X 1和X 2各自独立地表示氧或硫原子; 表示单键或双键; Y表示单键或亚烷基,n表示0或1,W 1和W 2各自独立地表示氢原子,低级烷基或氨基,Z表示-CH 2 - , - O-, -S-或-NH-残基; 条件是当Q为则R 1,R 2和R 3不同时为甲基; 和其生理上可接受的盐具有利尿作用,肾保护作用和/或支气管扩张作用。 该化合物可用作利尿剂,肾保护剂和/或支气管扩张剂。