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20 条记录 (耗时 0.023 秒)

    Novel compounds
    4.
    发明授权
    Novel compounds 失效
    新型化合物

    公开(公告)号：US5075300A

    公开(公告)日：1991-12-24

    申请号：US398490

    申请日：1989-08-25

    申请人： Richard M. Hindley ,  David Haigh ,  Peter T. Duff

    发明人： Richard M. Hindley ,  David Haigh ,  Peter T. Duff

    IPC分类号： C07D277/20 ,  A61K31/425 ,  A61K31/426 ,  A61K31/44 ,  A61K31/496 ,  A61K31/505 ,  A61P3/06 ,  A61P3/08 ,  A61P9/00 ,  C07D263/58 ,  C07D277/34 ,  C07D417/12

    CPC分类号： C07D417/12

    摘要： A compound of formula (I): ##STR1## or a tautomeric form thereof and/or a pharamaceutically acceptable salt thereof, and/or a pharmaceutically acceptable solvate thereof, wherein:A.sup.1 represents a substituted or unsubstituted aromatic heterocyclyl group;A.sup.2 represents a benzene ring having in total up to five substituents;X represents O, S or NR.sup.1 l 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 providing that Y does not represent O when X represents NR.sup.1 ;R.sup.2 and R.sup.3 each represent hydrogen, or R.sup.2 and R.sup.3 together represent 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 a compound and a composition in medicine.

    Thiazolidinedione derivatives
    5.
    发明授权
    Thiazolidinedione derivatives 失效
    噻唑烷二酮衍生物

    公开(公告)号：US5478850A

    公开(公告)日：1995-12-26

    申请号：US50116

    申请日：1993-04-30

    申请人： Richard M. Hindley ,  David Haigh ,  Graham P. Cottam

    发明人： Richard M. Hindley ,  David Haigh ,  Graham P. Cottam

    IPC分类号： A61K31/425 ,  A61K31/426 ,  A61P3/06 ,  A61P3/08 ,  A61P3/10 ,  C07D277/20 ,  C07D277/34 ,  C07D417/12

    CPC分类号： C07D417/12 ,  C07D277/34

    摘要： ##STR1## A compound of formula (I) or a tautomeric form thereof and/or a pharmaceutically acceptable salt thereof, and/or a pharmaceutically acceptable solvate thereof, wherein R
    1 and R
    2 each independently represent an alkyl group, a substituted or unsubstituted aryl group or an aralkyl group being substituted or unsubstituted in the aryl or alkyl moiety; or R
    1 together with R
    2 represents a linking group, the linking group consisting of an optionally substituted methylene group and either a further optionally substituted methylene group or an O or S atom, optional substituents for the said methylene groups being selected from alkyl, aryl or aralkyl or substituents of adjacent methylene groups together with the carbon atoms to which they are attached form a substituted or unsubstituted phenylene group; R
    3 and R
    4 each represent hydrogen, or R
    3 and R
    4 together represent a bond; A
    1 represents a benzene ting having in total up to three optional substituents; X represents O or S; and n represents an integer in the range of from 2 to 6; a process for preparing such a compound, a pharmaceutical composition containing such a compound and the use of such a compound and composition in medicine.

    摘要翻译： PCT No.PCT / GB91 / 01835 Sec。 371日期：1993年04月30日 102（e）日期1993年4月30日PCT 1991年10月18日PCT公布。 出版物WO92 / 07839 （I）式（I）化合物或其互变异构形式和/或其药学上可接受的盐，和/或其药学上可接受的溶剂合物，其中R 1和R 2各自独立地表示 烷基，取代或未取代的芳基或在芳基或烷基部分被取代或未取代的芳烷基; 或R 1与R 2一起表示连接基团，连接基团由任选取代的亚甲基和进一步任选取代的亚甲基或O或S原子组成，所述亚甲基的任选取代基选自烷基，芳基或芳烷基 或相邻亚甲基的取代基与它们所连接的碳原子一起形成取代或未取代的亚苯基; R3和R4各自表示氢，或R3和R4一起表示键; A1代表总共具有三个任选的取代基的苯; X表示O或S; n表示2〜6的整数， 制备这种化合物的方法，含有这种化合物的药物组合物以及这种化合物和组合物在医药中的用途。

    Oxazolidine dione derivatives
    6.
    发明授权
    Oxazolidine dione derivatives 失效
    恶唑烷二酮衍生物

    公开(公告)号：US5391565A

    公开(公告)日：1995-02-21

    申请号：US978706

    申请日：1993-02-03

    申请人： Richard M. Hindley

    发明人： Richard M. Hindley

    IPC分类号： A61K31/42 ,  A61K31/421 ,  A61K31/425 ,  A61K31/44 ,  A61K31/496 ,  A61K31/505 ,  A61P3/06 ,  A61P3/08 ,  A61P9/00 ,  C07D263/44 ,  C07D263/58 ,  C07D413/12 ,  C07D417/12

    CPC分类号： C07D263/44 ,  C07D263/58 ,  C07D413/10

    摘要： Compounds of the formula: ##STR1## or tautomeric forms and a pharmaceutically acceptable salt, and pharmaceutically acceptable solvates thereof, wherein:A.sup.1 is a substituted or unsubstituted oxazole substituted by up to 4 substituents selected from the group consisting of C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, phenyl, and halogen or any two substituents on adjacent carbon atoms, together with the carbon atoms to which they are attached, form a benzene ring, and wherein the carbon atoms of the benzene ring represented by the said two substituents are unsubstituted or substituted with up to three groups selected from halogen, C.sub.1-6 -alkyl, phenyl, C.sub.1-6 -alkoxy, halo-C.sub.1-6 -alkyl, hydroxy, amino, nitro, carboxy, C.sub.1-6 -alkoxycarbonyl, C.sub.1-6 -alkoxycarbonyl-C.sub.1-6 -alkyl, C.sub.1-6 -alkylcarbonyloxy, and C.sub.1-5 -alkylcarbonyl;R.sup.l is a hydrogen atom, a C.sub.1-6 -alkyl group, a C.sub.1-6 -alkylcarbonyloxy group, a phenyl-C.sub.1-6 -alkyl group, wherein the phenyl moiety may be substituted or unsubstituted, or a substituted or unsubstituted phenyl group, wherein the said phenyl groups may be substituted with up to three groups selected from halogen, C.sub.1-6 -alkyl, phenyl, C.sub.1-6 -alkoxy, halo-C.sub.1-6 -alkyl, hydroxy, amino, nitro, carboxy, C.sub.1-6 -alkoxycarbonyl, C.sub.1-6 -alkoxycarbonyl-C.sub.1-6 -alkyl, C.sub.1-6 -alkylcarbonyloxy, and C.sub.1-6 -alkylcarbonyl;A.sup.2 is a benzene ring having in total up to five substituents wherein three optional substituents are selected from halogen, C.sub.1-6 -alkyl, phenyl, C.sub.1-6 -alkoxy, halo-C.sub.1-6 -alkyl, hydroxy, amino, nitro, carboxy, C.sub.1-6 -alkoxycarbonyl. C.sub.1-6 -alkoxycarbonyl-C.sub.1-6 -alkyl, C.sub.1-6 -alkylcarbonyloxy, and C.sub.1-6 -alkylcarbonyl; and n is an integer from 2 to 6, are disclosed as hypoglycemics, hypolipidemics and antihypertensives.

    摘要翻译： PCT No.PCT / GB91 / 01337 Sec。 371日期：1993年2月3日 102（e）日期1993年2月3日PCT 1991年8月5日PCT PCT。 出版物WO92 / 02520 日期：1992年2月20日，下列化合物：或互变异构形式及其药学上可接受的盐及其药学上可接受的溶剂化物，其中：A1是被至多4个取代基取代的取代或未取代的恶唑， C 1-6 - 烷基，C 1-6 - 烷氧基，苯基和卤素或相邻碳原子上的任何两个取代基与它们所连接的碳原子一起形成苯环，并且其中苯的碳原子 由所述两个取代基表示的环是未取代的或被至多三个选自卤素，C 1-6 - 烷基，苯基，C 1-6 - 烷氧基，卤代-C 1-6 - 烷基，羟基，氨基，硝基，羧基， C 1-6 - 烷氧基羰基，C 1-6 - 烷氧基羰基-C 1-6 - 烷基，C 1-6 - 烷基羰基氧基和C 1-5 - 烷基羰基; R1是氢原子，C1-6烷基，C1-6烷基羰基氧基，苯基-C1-6烷基，其中苯基部分可以是取代或未取代的，或取代或未取代的苯基， 其中所述苯基可以被最多三个选自卤素，C 1-6 - 烷基，苯基，C 1-6 - 烷氧基，卤代-C 1-6 - 烷基，羟基，氨基，硝基，羧基，C 1-6 - 烷氧基羰基-C 1-6 - 烷基，C 1-6 - 烷基羰基氧基和C 1-6 - 烷基羰基; A2是总共具有五个取代基的苯环，其中三个任选的取代基选自卤素，C 1-6 - 烷基，苯基，C 1-6 - 烷氧基，卤代-C 1-6 - 烷基，羟基，氨基，硝基，羧基 ，C 1-6 - 烷氧基羰基。 C 1-6 - 烷氧基羰基-C 1-6 - 烷基，C 1-6 - 烷基羰基氧基和C 1-6 - 烷基羰基; 并且n是2至6的整数，被公开为低血糖症，降血脂药和抗高血压药。

    Novel compounds
    7.
    发明授权
    Novel compounds 失效

    公开(公告)号：US5063240A

    公开(公告)日：1991-11-05

    申请号：US521157

    申请日：1990-05-07

    申请人： Richard M. Hindley

    发明人： Richard M. Hindley

    IPC分类号： C07D277/20 ,  A61K31/425 ,  A61K31/426 ,  A61P3/06 ,  A61P3/08 ,  A61P9/12 ,  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, characterized in that:R.sup.1 represents hydrogen, alkyl, aralkyl or aryl and R.sup.2 represents hydrogen or R.sup.1 and R.sup.2 together represent a bond;R.sup.3 represents hydrogen and R.sup.4 represents hydrogen, akyl, aralkyl or aryl or R.sup.3 and R.sup.4 together represent a bond;X represents a bond, >C.dbd.O, >CHOH, O, S or NR wherein R is an alkyl group;n represents an integer 1, 2 or 3;m represents an integer 1, 2 or 3 andA.sup.1 and A.sup.2 each independently represent a benzene ring having a total up to 5 substituents comprising up to 3 optional substituents; a process for preparing such a compound, a pharmaceutical composition comprising such a compound and the use of such compounds and compositions in medicine.

    Compounds
    8.
    发明授权
    Compounds 失效
    化合物

    公开(公告)号：US5194443A

    公开(公告)日：1993-03-16

    申请号：US645092

    申请日：1991-01-24

    申请人： Richard M. Hindley

    发明人： Richard M. Hindley

    IPC分类号： C07D277/20 ,  C07D277/42 ,  C07D277/82 ,  C07D417/12

    CPC分类号： C07D277/20 ,  C07D277/42 ,  C07D277/82 ,  C07D417/12

    摘要： Compounds of formula (I): ##STR1## or a tautomeric form thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, wherein:A.sup.1 represents a substituted or unsubstituted aromatic heterocyclyl group;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;R.sup.2 and R.sup.3 each represent hydrogen, or R.sup.2 and R.sup.3 together represent a bond;A.sup.2 represents a benzene ring having in total up to five substituents; andn represents an integer in the range of from 2 to 6; pharmaceutical compositions containing such compounds and the use of such compounds and compositions in medicine.

    摘要翻译： 式（I）的化合物：其中：A1表示取代或未取代的芳族杂环基;或其药学上可接受的盐， R1表示氢原子，烷基，酰基，芳烷基，其中芳基部分可以是取代或未取代的，或取代或未取代的芳基; R2和R3各自表示氢，或R2和R3一起表示键; A2代表总共有五个取代基的苯环; n表示2〜6的整数， 含有这些化合物的药物组合物以及这些化合物和组合物在医药中的用途。

    6-oxomorpholines
    9.
    发明授权
    6-oxomorpholines 失效
    6-氧代吗啉

    公开(公告)号：US4593023A

    公开(公告)日：1986-06-03

    申请号：US735357

    申请日：1985-05-17

    申请人： Richard M. Hindley

    发明人： Richard M. Hindley

    IPC分类号： A61K31/535 ,  A61K31/5375 ,  A61P1/00 ,  A61P3/00 ,  A61P3/08 ,  C07C67/00 ,  C07C227/00 ,  C07C229/14 ,  C07C229/16 ,  C07D265/32

    CPC分类号： C07D265/32

    摘要： A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt, thereof, in which R.sup.1 is hydrogen, halogen, or trifluoromethyl,R.sup.2 is hydrogen or halogen,R.sup.3 is hydrogen or methyl.R.sup.4 is --O(CH.sub.2).sub.a CO.sub.2 H, --O(CH.sub.2).sub.b M, --CO.sub.2 H or an esteror amide derivative thereof in whicha is an integer from 1 to 6,b is an integer from 2 to 7, andM is hydroxy, C.sub.1-6 alkoxy or ##STR2## in which R.sup.5 and R.sup.6 are each hydrogen or C.sub.1-6 alkyl or ##STR3## together form a five or six membered ring, and n is 1 or 2; a process for preparing such a compound and its use in medicine and agriculture.

    摘要翻译： 式（I）化合物：其中R 1是氢，卤素或三氟甲基，R 2是氢或卤素，R 3是氢或甲基。 R 4是-O（CH 2）a CO 2 H，-O（CH 2）b M，-CO 2 H或其中a为1至6的整数的酯或酰胺衍生物，b为2至7的整数，M为羟基 ，C 1-6烷氧基或者其中R 5和R 6各自为氢或C 1-6烷基或“IMAGE”一起形成五或六元环，且n为1或2; 这种化合物的制备方法及其在医药和农业中的应用。