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    Heterocyclic compounds and pharmaceutical use
    2.
    发明授权
    Heterocyclic compounds and pharmaceutical use 失效
    杂环化合物和药物用途

    公开(公告)号：US4250173A

    公开(公告)日：1981-02-10

    申请号：US094100

    申请日：1979-11-14

    申请人： Barrie C. C. Cantello

    发明人： Barrie C. C. Cantello

    IPC分类号： C07D263/28 ,  C07D265/08 ,  C07D277/18 ,  C07D279/06 ,  A61K31/425 ,  A61K31/535 ,  A61K31/54

    CPC分类号： C07D265/08 ,  C07D263/28 ,  C07D277/18 ,  C07D279/06

    摘要： A compound, with hypolgycaemic activity, having formula (II) or a pharmaceutically acceptable quaternary ammonium or acid addition salt thereof: ##STR1## wherein X represents oxygen or sulphur; n.sub.7 represents zero or 1;R.sup.7 represents hydrogen or C.sub.1-6 alkyl;R.sup.1 and R.sup.2 are the same or different and represent hydrogen, C.sub.1-6 alkyl, phenyl, benzyl, or C.sub.3-6 cycloalkyl;R.sup.3 represents hydrogen, C.sub.1-6 alkyl, phenyl or benzyl;R.sup.4 represents hydrogen or C.sub.1-6 alkyl;R.sup.5 represents C.sub.1-6 alkyl, phenyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl, and C.sub.1-6 alkoxy; or benzyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl and C.sub.1-6 alkoxy; or R.sup.4 and R.sup.5 together represent the remaining members of a 5- or 6-membered ring optionally containing an oxygen, sulphur or additional nitrogen atom and being optionally substituted with C.sub.1-6 alkyl, carboxy or C.sub.1-6 alkoxycarbonyl; andR.sup.6 represents phenyl, optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkanoyl, C.sub.1-6 alkanoyloxy, nitro, hydroxy, amino, substituted amino, carboxy, and C.sub.1-6 alkoxycarbonyl.

    摘要翻译： 具有降血糖活性的化合物，具有式（II）或其药学上可接受的季铵或其酸加成盐：其中X表示氧或硫; n7表示零或1; R 7表示氢或C 1-6烷基; R 1和R 2相同或不同，表示氢，C 1-6烷基，苯基，苄基或C 3-6环烷基; R3代表氢，C1-6烷基，苯基或苄基; R4表示氢或C1-6烷基; R5表示C1-6烷基，任选被至多3个选自卤素，C 1-6烷基和C 1-6烷氧基的基团取代的苯基; 或任选被至多3个选自卤素，C 1-6烷基和C 1-6烷氧基的基团取代的苄基; 或R 4和R 5一起代表任选地含有氧，硫或另外的氮原子并任选被C 1-6烷基，羧基或C 1-6烷氧基羰基取代的5-或6-元环的剩余成员; 并且R 6表示任选被至多3个选自卤素，C 1-6烷基，C 1-6烷氧基，C 1-6烷酰基，C 1-6烷酰氧基，硝基，羟基，氨基，取代的氨基，羧基和C1- 6烷氧基羰基。

    Method of treating diabetes using oxazoline or thiazoline compounds
    3.
    发明授权
    Method of treating diabetes using oxazoline or thiazoline compounds 失效
    使用恶唑啉或噻唑啉化合物治疗糖尿病的方法

    公开(公告)号：US4409216A

    公开(公告)日：1983-10-11

    申请号：US139284

    申请日：1980-04-11

    申请人： Barrie C. C. Cantello

    发明人： Barrie C. C. Cantello

    IPC分类号： C07D277/20 ,  A61K31/42 ,  A61K31/421 ,  A61P3/08 ,  A61P3/10 ,  C07D263/48 ,  C07D277/48 ,  C07D277/82 ,  A61K31/425 ,  A61K31/535 ,  A61K31/54

    CPC分类号： C07D263/48 ,  C07D277/48 ,  C07D277/82

    摘要： A compound, with hypoglycaemic activity, having formula (II) or a pharmaceutically acceptable acid addition salt thereof: ##STR1## wherein X represents oxygen or sulphur;R.sup.1 R.sup.2 are the same or different and represent hydrogen, halogen, C.sub.1-6 alkyl, phenyl, benzyl,C.sub.3-6 cycloalkyl, carbo-C.sub.1-6 alkoxy or C.sub.1-6 carboxy or R.sup.1 and R.sup.2 represent the remaining members of a benzene ring;R.sup.3 represents hydrogen, C.sub.1-6 alkyl, phenyl or benzyl;R.sup.4 represents hydrogen or C.sub.1-6 alkyl;R.sup.5 represents C.sub.1-6 alkyl, phenyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl, and C.sub.1-6 alkoxy; or benzyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl and C.sub.1-6 alkoxy; or R.sup.4 and R.sup.5 together represent the remaining members of a 5- or 6- membered ring optionally containing an oxygen, sulphur or additional nitrogen atom and being optionally substituted with C.sub.1-6 alkyl; andR.sup.6 represents C.sub.1-6 alkyl, phenyl, optionally substituted with up to 3 groups selected from halogen, nitro-, amino-, trifluoromethyl, C.sub.1-6 alkyl and C.sub.1-6 alkoxy; or benzyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl and C.sub.1-6 al

    摘要翻译： 具有低血糖活性的化合物，具有式（II）或其药学上可接受的酸加成盐：其中X表示氧或硫; R1 R2相同或不同，代表氢，卤素，C 1-6烷基，苯基，苄基，C 3-6环烷基，碳-C 1-6烷氧基或C 1-6羧基或R 1和R 2表示苯环的剩余成员 ; R3代表氢，C1-6烷基，苯基或苄基; R4表示氢或C1-6烷基; R5表示C1-6烷基，任选被至多3个选自卤素，C 1-6烷基和C 1-6烷氧基的基团取代的苯基; 或任选被至多3个选自卤素，C 1-6烷基和C 1-6烷氧基的基团取代的苄基; 或R 4和R 5一起代表5-或6-元环的任选含有氧，硫或另外的氮原子并且任选地被C 1-6烷基取代的剩余成员; R 6表示C 1-6烷基，苯基，任选被至多3个选自卤素，硝基，氨基 - ，三氟甲基，C 1-6烷基和C 1-6烷氧基的基团取代; 或任选被至多3个选自卤素，C 1-6烷基和C 1-6的基团取代的苄基

    Secondary amines and use in pharmaceutical compositions
    4.
    发明授权
    Secondary amines and use in pharmaceutical compositions 失效
    仲胺并用于药物组合物

    公开(公告)号：US4629737A

    公开(公告)日：1986-12-16

    申请号：US513869

    申请日：1983-07-14

    申请人： Barrie C. C. Cantello

    发明人： Barrie C. C. Cantello

    IPC分类号： A61K31/135 ,  A61K31/19 ,  C07C43/225 ,  C07C43/303 ,  C07C43/313 ,  C07C229/38 ,  C07D307/81 ,  C07C101/16 ,  A61K31/195 ,  A61K31/215 ,  C07C101/447

    CPC分类号： C07C255/00 ,  C07C229/38 ,  C07C43/225 ,  C07C43/303 ,  C07C43/313 ,  C07D307/81

    摘要： A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt, ester or amide thereof, in which: W is an optionally substituted phenyl group of the formula ##STR2## wherein R.sup.1 is hydrogen or fluorine, R.sup.2 is hydrogen, C.sub.1-6 alkyl, halogen or trifluoromethyl; or W is a phenoxymethyl or benzofuran-2-yl group;R.sup.3 is C.sub.1-12 alkyl or phenyl C.sub.1-6 alkyl;A is hydrogen or methyl,X is carboxy, --Z--CO.sub.2 H, --Z--OH, T--Z--CO.sub.2 H,--Z--NR.sup.4 R.sup.5, --T--Y--OM, --T--Y--NR.sup.4 R.sup.5, or --T--R.sup.6, in the para- or meta-position with respect to the --(CH.sub.2).sub.n group, whereinR.sup.4 and R.sup.5 are each hydrogen or C.sub.1-6 alkyl,R.sup.6 is C.sub.1-6 alkyl,T is 0, S, --NH or --N--R.sup.7, in which R.sup.7 is C.sub.1-6 alkylZ is C.sub.1-10 straight or branched alkylene optionally containing a carbon-carbon double bond;Y is C.sub.2-10 straight or branched alkylene, provided that the hetero atoms in --T--Y--OM and --T--Y--NR.sup.4 R.sup.5 are separated by at least two carbon atoms, M is hydrogen, C.sub.1-6 alkyl or phenyl, and n is 1 or 2, is useful for obesity or hyperglycaemia.

    摘要翻译： 式（I）的化合物：其中：W是任选取代的下式的苯基，其中R 1是氢或氟，R 2是 氢，C 1-6烷基，卤素或三氟甲基; 或W是苯氧基甲基或苯并呋喃-2-基; R3是C1-12烷基或苯基C1-6烷基; A是氢或甲基，X是羧基，-Z-CO 2 H，-Z-OH，TZ-CO 2 H，-Z-NR 4 R 5，-TY-OM，-TY-NR 4 R 5或-T- 相对于 - （CH 2）n基的间位，其中R 4和R 5各自为氢或C 1-6烷基，R 6为C 1-6烷基，T为0，S，-NH或-N-R 7，其中 R 7是C 1-6烷基Z是任选含有碳 - 碳双键的C 1-10直链或支链亚烷基; Y是C2-10直链或支链亚烷基，条件是-TY-OM和-TY-NR4R5中的杂原子被至少两个碳原子分开，M是氢，C 1-6烷基或苯基，n是1或 2，可用于肥胖或高血糖。

    Intermediates for heterocyclic imines having hypolipidaemic activity
    5.
    发明授权
    Intermediates for heterocyclic imines having hypolipidaemic activity 失效
    具有降血脂活性的杂环亚胺的中间体

    公开(公告)号：US4282356A

    公开(公告)日：1981-08-04

    申请号：US158212

    申请日：1980-06-10

    申请人： Barrie C. C. Cantello

    发明人： Barrie C. C. Cantello

    IPC分类号： C07D263/28 ,  C07D265/08 ,  C07D277/18 ,  C07D279/06 ,  C07D263/06 ,  C07D265/06 ,  C07D277/04

    CPC分类号： C07D265/08 ,  C07D263/28 ,  C07D277/18 ,  C07D279/06

    摘要： A compound, with hypoglycaemic activity, having formula (II) or a pharmaceutically acceptable quaternary ammonium or acid addition salt thereof: ##STR1## wherein X represents oxygen or sulphur;n represents zero or 1;R.sup.7 represents hydrogen or C.sub.1-6 alkyl;R.sup.1 and R.sup.2 are the same or different and represent hydrogen, C.sub.1-6 alkyl, phenyl, benzyl, or C.sub.3-6 cycloalkyl;R.sup.3 represents hydrogen, C.sub.1-6 alkyl, phenyl or benzyl;R.sup.4 represents hydrogen or C.sub.1-6 alkyl;R.sup.5 represents C.sub.1-6 alkyl, phenyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl, and C.sub.1-6 alkoxy; or benzyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl and C.sub.1-6 alkoxy; or R.sup.4 and R.sup.5 together represent the remaining members of a 5- or 6-membered ring optionally containing an oxygen, sulphur or additional nitrogen atom and being optionally substituted with C.sub.1-6 alkyl, carboxy or C.sub.1-6 alkoxycarbonyl; andR.sup.6 represents phenyl, optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkanoyl, C.sub.1-6 alkanoyloxy, nitro, hydroxy, amino, substituted amino, carboxy, and C.sub.1-6 alkoxycarbonyl.

    Morpholine derivatives, compositions and medicinal use
    7.
    发明授权
    Morpholine derivatives, compositions and medicinal use 失效
    吗啉衍生物，组合物和医药用途

    公开(公告)号：US4607033A

    公开(公告)日：1986-08-19

    申请号：US666818

    申请日：1984-10-31

    申请人： Barrie C. C. Cantello

    发明人： Barrie C. C. Cantello

    IPC分类号： A61K31/535 ,  A61K31/5375 ,  A61K31/55 ,  A61P3/04 ,  A61P3/08 ,  C07D265/30 ,  C07D267/08 ,  C07D267/10 ,  C07D413/04

    CPC分类号： C07D265/30 ,  C07D267/10 ,  C07D413/04

    摘要： Compounds of formula (I): ##STR1## or a salt thereof, in which W is phenyl optionally substituted by halogen or trifluoromethyl, or a benzofuran-2-yl group,R.sup.1 is hydrogen or methyl,R.sup.2 is carboxyl or a group O--Z--CO.sub.2 H or an ester or amide thereof; a groupO--E--NR.sup.3 R.sup.4 or a group O--E--OR.sup.5,wherein R.sup.3, R.sup.4 and R.sup.5 each represents hydrogen or C.sub.1-6 alkyl, Z is a C.sub.1-6 straight or branched alkylene chain, n is 1 or 2, a is 2 or 3, and E is a C.sub.2-7 straight or branched alkylene chain with at least two carbon atoms separating the two heteroatoms in the group R.sup.2 ; a process for the production of such compounds and their use in treating hyperglycaemia and/or obesity.

    摘要翻译： 式（I）化合物：其中W为任选被卤素或三氟甲基取代的苯基或苯并呋喃-2-基，R1为氢或甲基，R2为羧基或 基团OZ-CO 2 H或其酯或酰胺; 基团OE-NR3R4或OE-OR5基团，其中R3，R4和R5各自表示氢或C1-6烷基，Z是C1-6直链或支链亚烷基链，n是1或2，a是2或3 并且E是具有至少两个碳原子的C2-7直链或支链亚烷基链，其分离基团R2中的两个杂原子; 这种化合物的制备方法及其在治疗高血糖症和/或肥胖症中的用途。

    Carboxamidine derivatives and hypoglycemical use
    8.
    发明授权
    Carboxamidine derivatives and hypoglycemical use 失效
    卡巴胺衍生物和低血糖用途

    公开(公告)号：US4333929A

    公开(公告)日：1982-06-08

    申请号：US226180

    申请日：1981-01-19

    申请人： Barrie C. C. Cantello

    发明人： Barrie C. C. Cantello

    IPC分类号： A61K31/155 ,  A61P3/08 ,  A61P3/10 ,  C07C67/00 ,  C07C239/00 ,  C07C279/26 ,  C07C281/16 ,  C07D295/215 ,  A61K31/54 ,  C07C129/00 ,  C07D279/10

    CPC分类号： C07D295/215 ,  C07C279/26 ,  Y10S514/866

    摘要： A compound of formula (II) or a pharmaceutically acceptable acid addition salt thereof ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and each represents C.sub.1-6 alkyl; R.sup.5 represents hydrogen or C.sub.1-6 alkyl; R.sup.6 represents C.sub.1-6 alkyl, phenyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl, and C.sub.1-6 alkoxy; or benzyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl and C.sub.1-6 alkoxy; or R.sup.5 and R.sup.6 together represent the remaining members of a 5- or 6-membered ring optionally containing an oxygen, sulphur or additional nitrogen atom and being optionally substituted with C.sub.1-6 alkyl, carboxy or C.sub.1-6 alkoxycarbonyl; and R.sup.7 represents C.sub.1-6 alkyl, phenyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl and C.sub.1-6 alkoxy; or benzyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl and C.sub.1-6 alkoxy, has useful hypoglycaemic activity.

    摘要翻译： 式（II）化合物或其药学上可接受的酸加成盐其中R 1，R 2，R 3和R 4相同或不同，各自表示C 1-6烷基; R5表示氢或C1-6烷基; R 6表示C 1-6烷基，任选被至多3个选自卤素，C 1-6烷基和C 1-6烷氧基的基团取代的苯基; 或任选被至多3个选自卤素，C 1-6烷基和C 1-6烷氧基的基团取代的苄基; 或R 5和R 6一起表示任选地含有氧，硫或另外的氮原子并且任选被C 1-6烷基，羧基或C 1-6烷氧基羰基取代的5-或6-元环的剩余成员; 并且R 7表示C 1-6烷基，任选被至多3个选自卤素，C 1-6烷基和C 1-6烷氧基的基团取代的苯基; 或任选被至多3个选自卤素，C 1-6烷基和C 1-6烷氧基的基团取代的苄基具有有效的低血糖活性。

    Compounds
    10.
    发明授权
    Compounds 失效

    公开(公告)号：US5132317A

    公开(公告)日：1992-07-21

    申请号：US571734

    申请日：1990-08-23

    申请人： Barrie C. C. Cantello ,  Peter T. Duff

    发明人： Barrie C. C. Cantello ,  Peter T. Duff

    IPC分类号： C07D277/20 ,  A61K31/425 ,  A61K31/426 ,  A61P3/06 ,  A61P3/08 ,  A61P3/10 ,  C07D277/34

    CPC分类号： C07D277/34

    摘要： A compound of formula (I): ##STR1## or a tautomeric form thereof and/or a pharmaceutically acceptable salt thereof, and/or a pharmaceutically acceptable solvate thereof, wherein:A.sup.1 represents a substituted or unsubstituted aryl group;A.sup.2 represents a benzene ring having in total up to five substituents;X represents O, S or NR.sup.1 wherein R.sup.1 represents a hydrogen atom, an alkyl group, an acyl group, an aralkyl group, wherein the aryl moiety may be substituted or unsubstituted, or a substituted or unsubstituted aryl group;Y represents O or S;R.sup.2 represents hydrogen;R.sup.3 represents hydrogen or an alkyl, aralkyl or aryl group or R.sup.2 together with R.sup.3 represents a bond; andn represents an integer in the range of from 2 to 6; a process for preparing such a compound, a pharmaceutical composition comprising such a compound and the use of such compound and composition in medicine.