利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

47 条记录 (耗时 0.037 秒)

    Hydroxylamine derivatives
    1.
    发明授权
    Hydroxylamine derivatives 失效
    羟胺衍生物

    公开(公告)号：US5334614A

    公开(公告)日：1994-08-02

    申请号：US59313

    申请日：1993-05-11

    申请人： Philip N. Edwards ,  Michael S. Large

    发明人： Philip N. Edwards ,  Michael S. Large

    IPC分类号： A61K31/135 ,  A61K31/27 ,  A61K31/275 ,  A61K31/35 ,  A61K31/496 ,  A61K31/505 ,  A61P37/08 ,  A61P43/00 ,  C07C239/20 ,  C07D213/63 ,  C07D263/36 ,  C07D277/22 ,  C07D307/42 ,  C07D309/10 ,  C07D405/12 ,  C07D417/04 ,  A61K31/34 ,  C07D307/20

    CPC分类号： C07D405/12 ,  C07D309/10

    摘要： The invention concerns hydroxylamine derivatives of the formula I ##STR1## wherein R.sup.4 is hydrogen, carbamoyl, (1-4C)alkyl, cyclopentyl, cyclohexyl, tetrahydrofuran-3-yl, tetrahydropyran-4-yl, piperidin-4-yl, N-(1-4C)alkylpiperidin-4-yl, (2-5C)alkanoyl, (1-4C)alkylsulphonyl, N-(1-4C)alkylcarbamoyl, N,N-di-(1-4C)alkylcarbamoyl, phenyl, phenyl-(1-4C)alkyl, di-phenyl-(1-4C)alkyl, benzoyl, phenylsulphonyl or a heteroarylmethyl group;R.sup.5 is hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, cyano-(1-4C)alkyl, phenyl or phenyl-(1-4C)alkyl;A.sup.4 is (1-4C)alkylene;Ar.sup.1 is phenylene, pyridinediyl or pyrimidinediyl;A.sup.1 is a direct link to X.sup.1, or A.sup.1 is (1-4C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is phenylene, pyridinediyl, pyrimidinediyl, thiophenediyl, furandiyl or thiazolediyl;R.sup.1 is hydrogen, (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula -A.sup.2 -X.sup.2 -A.sup.3 -wherein each of A.sup.2 and A.sup.3 is independently (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl, sulphonyl or imino;or a pharmaceutically-acceptable salt thereof; processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.

    摘要翻译： 本发明涉及式I的羟胺衍生物，其中R 4是氢，氨基甲酰基，（1-4C）烷基，环戊基，环己基，四氢呋喃-3-基，四氢吡喃-4-基，哌啶-4-基，N （1-4C）烷基哌啶-4-基，（2-5C）烷酰基，（1-4C）烷基磺酰基，N-（1-4C）烷基氨基甲酰基，N，N-二（1-4C）烷基氨基甲酰基，苯基， 苯基 - （1-4C）烷基，二 - 苯基 - （1-4C）烷基，苯甲酰基，苯基磺酰基或杂芳基甲基; R5是氢，（1-4C）烷基，（3-4C）烯基，（3-4C）炔基，氰基 - （1-4C）烷基，苯基或苯基 - （1-4C）烷基; A4是（1-4C）亚烷基; Ar1是亚苯基，吡啶二基或嘧啶二基; A1是直接连接到X1，或A1是（1-4C）亚烷基; X1是氧基，硫基，亚磺酰基或磺酰基; Ar 2是亚苯基，吡啶二基，嘧啶二基，噻吩二基，呋喃二基或噻唑二基; R1为氢，（1-4C）烷基，（3-4C）烯基或（3-4C）炔基; 并且R2和R3一起形成式-A2-X2-A3-的基团，其中A2和A3各自独立地为（1-3C）亚烷基，X2为氧基，硫基，亚磺酰基，磺酰基或亚氨基; 或其药学上可接受的盐; 制造过程; 含有它们的药物组合物及其作为5-脂肪氧合酶抑制剂的用途。

    Oxides of 1,2,5-thiadiazoles, their use in pharmaceutical compositions
    2.
    发明授权
    Oxides of 1,2,5-thiadiazoles, their use in pharmaceutical compositions 失效
    1,2,5-噻二唑的氧化物，它们在药物组合物中的用途

    公开(公告)号：US4746672A

    公开(公告)日：1988-05-24

    申请号：US376395

    申请日：1982-05-10

    申请人： Tobias O. Yellin ,  Philip N. Edwards ,  Michael S. Large

    发明人： Tobias O. Yellin ,  Philip N. Edwards ,  Michael S. Large

    IPC分类号： A61K31/425 ,  A61P1/04 ,  A61P43/00 ,  C07D417/12 ,  A61K31/41

    CPC分类号： C07D417/12

    摘要： Sulphur derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion of the formula I: ##STR1## in which R.sup.1 and R.sup.2 independently are hydrogen or 1-10C alkyl, 3-8C cycloalkyl or 4-14C cycloalkylalkyl, each alkyl, cycloalkyl or cycloalkylalkyl optionally carrying one or more F, Cl or Br atoms, provided that one of R.sup.1 and R.sup.2 is halogen substituted; ring X is a heterocyclic ring as defined in the specification; A is phenylene or 5-7C cycloalkylene or a 1-8C alkylene chain into which is optionally inserted one or two groups; p is 1 or 2; R.sup.3 is a variety of radicals described in the specification; and the pharmaceutically-acceptable acid-addition salts thereof. Manufacturing processes for the derivatives, intermediates and pharmaceutical compositions are also part of the invention.

    摘要翻译： 作为组胺H-2拮抗剂的硫衍生物，其抑制式I的胃酸分泌：其中R1和R2独立地为氢或1-10C烷基，3-8C环烷基或4-14C环烷基烷基，每个烷基 任选地携带一个或多个F，Cl或Br原子的环烷基或环烷基烷基，条件是R 1和R 2中的一个是卤素取代的; 环X是说明书中定义的杂环; A是亚苯基或5-7C亚环烷基或1-8C亚烷基链，其中任选地插入一个或两个基团; p为1或2; R3是说明书中描述的各种基团; 及其药学上可接受的酸加成盐。 衍生物，中间体和药物组合物的制备方法也是本发明的一部分。

    Pyrrolidine derivatives
    3.
    发明授权
    Pyrrolidine derivatives 失效
    吡咯烷衍生物

    公开(公告)号：US5420298A

    公开(公告)日：1995-05-30

    申请号：US114187

    申请日：1993-09-01

    申请人： Philip N. Edwards ,  Michael S. Large

    发明人： Philip N. Edwards ,  Michael S. Large

    IPC分类号： A61K31/40 ,  A61K31/4025 ,  A61K31/425 ,  A61K31/47 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D207/12 ,  C07D401/12 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D491/052 ,  C07D207/06 ,  C07D207/14

    CPC分类号： C07D401/12 ,  C07D207/12 ,  C07D409/12

    摘要： The invention concerns pyrrolidine derivatives of the formula ##STR1## wherein Ar.sup.1 is optionally-substituted phenyl, naphthyl or a 10-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur;A is a direct link to the group X or A is (1-4C)alkylene;X is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is phenylene, pyridinediyl, pyrimidinediyl, thiophendiyl, furandiyl or thiazolediyl;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl;R.sup.2 is (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, halogeno-(1-4C)alkyl, halogeno-(2-4C)alkenyl, halogeno-(2-4C)alkynyl, (1-4C)alkoxy-(2-4C)alkyl, hydroxy-(2-4C)alkyl, cyano-(1-4C)alkyl, carboxy-(1-4C)alkyl, carbamoyl-(1-4C)alkyl, (1-4C)alkoxycarbonyl-(1-4C)alkyl, N-(1-4C)alkylcarbamoyl-(1-4C)alkyl or N,N-di-(1-4C)alkylcarbamoyl-(1-4C)alkyl; andn is 1 or 2 and each R.sup.3 is independently hydrogen, hydroxy, (1-4C)alkyl or (1-4C)alkoxy;or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.

    摘要翻译： 本发明涉及式Ia的吡咯烷衍生物，其中Ar1是任选取代的苯基，萘基或含有一个或两个氮杂原子并且任选地含有另外选自氮，氧和硫的杂原子的10元双环杂环部分; A是直接连接到基团X或A是（1-4C）亚烷基; X是氧基，硫基，亚磺酰基或磺酰基; Ar 2是亚苯基，吡啶二基，嘧啶二基，噻吩二基，呋喃二基或噻唑二基; R1是（1-4C）烷基，（3-4C）烯基或（3-4C）炔基; R2是（1-4C）烷基，（2-4C）烯基，（2-4C）炔基，卤代 - （1-4C）烷基，卤代 - （2-4C）烯基，卤代 - （2-4C） （1-4C）烷基，（2-4C）烷基，氰基 - （1-4C）烷基，羧基 - （1-4C）烷基，氨基甲酰基 - （1-4C） （1-4C）烷氧基羰基 - （1-4C）烷基，N-（1-4C）烷基氨基甲酰基 - （1-4C）烷基或N，N-二（1-4C）烷基氨基甲酰基 - （1-4C）烷基; 并且n为1或2，并且每个R 3独立地为氢，羟基，（1-4C）烷基或（1-4C）烷氧基; 或其药学上可接受的盐; 制造过程; 含有它们的药物组合物及其作为5-脂肪氧合酶抑制剂的用途。

    (Substituted aralkyl) heterocyclic compounds
    6.
    再颁专利
    (Substituted aralkyl) heterocyclic compounds 失效

    公开(公告)号：USRE36617E

    公开(公告)日：2000-03-14

    申请号：US627311

    申请日：1996-04-03

    申请人： Philip N. Edwards ,  Michael S. Large

    发明人： Philip N. Edwards ,  Michael S. Large

    IPC分类号： A61K31/395 ,  A61K31/40 ,  A61K31/41 ,  A61K31/415 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/4418 ,  A61K31/445 ,  A61K31/505 ,  A61K31/535 ,  A61K31/5375 ,  A61P3/00 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  C07D213/46 ,  C07D213/57 ,  C07D233/60 ,  C07D233/61 ,  C07D233/64 ,  C07D233/90 ,  C07D239/26 ,  C07D249/08 ,  C07D295/18 ,  C07D521/00

    CPC分类号： C07D239/26 ,  C07D213/57 ,  C07D231/12 ,  C07D233/56 ,  C07D233/90 ,  C07D249/08

    摘要： A (substituted-aralkyl)heterocyclic compound of the formula I ##STR1## wherein R.sup.1 is an azido, carbamoyl, cyano, formyl, hydroxy or nitro radical, a 1-6C 1-hydroxyalkyl, alkoxy, alkylcarbamoyl, alkylthio, alkylsulphinyl or alkylsulphonyl radical, a 2-cyanoethyl radical, optionally bearing one to four 1-6C alkyl substituents, or a 2-6C alkanoyl, halogenoalkanoyl, alkanoyloxy, alkanoylamino, dialkylcarbamoyl or alkoxycarbonyl radical; R.sup.2 and R.sup.3, which may be the same or different, are each a hydrogen atom, a 1-6C alkyl, dueterioalkyl or halogenoalkyl radical, or a phenyl or phenyl(1-6C alkyl) radical, in each of which the phenyl may optionally bear one or more substituents; or R.sup.2 and R.sup.3, together with the carbon atom to which they are attached, may form a 3- to 6-membered ring; or R.sup.1 R.sup.2 R.sup.3 C- is a 1,1-dicyanoethyl or trifluoromethylsulphonyl radical; R.sup.4 is a hydrogen or halogen atom, a cyano or nitro radical or a 1-6C alkyl or halogenoalkyl radical; R.sup.5 has any of the values defined above for the group R.sup.1 R.sup.2 R.sup.3 C but is not necessarily the same as R.sup.1 R.sup.2 R.sup.3 C, or has any of the values defined above for R.sup.4 but is not necesarily the same as R.sup.4, or is a carbamoyl, 1-pyrrolidinyl-carbonyl, piperidinocarbonyl, morpholinocarbonyl or nitro radical, a 1-6C alkoxy or halogenoalkoxy radical or a 2-6C alkanoyl or alkoxy-carbonyl radical; A is a methylene or ethylene radical optionally bearing one or more substituents selected from deuterium and halogen atoms, carbamoyl, cyano and hydroxy radicals, 1-6C alkyl and alkoxy radicals, and 2-6C alkanoyloxy radicals provided that when A is linked to R.sup.6 through a nitrogen atom thereof, it may not bear a hydroxy, alkoxy or alkanoyloxy substituent on the carbon atom adjacent to such nitrogen atoms; and R.sup.6 is a 1H-1,2,4-triazol-1-yl, 4H-1,2,4-triazol-4-yl, 1H-imidazol-1-yl, 5-cyano-1H-imidazol-1-yl, 3-pyridyl or 5-pyrimidinyl radical, or a 1H-imidazol-1-yl radical, bearing at the 5-position thereof a 1-6C alkyl substituent which is itself optionally substituted by one or more carbamoyl, cyano, hydroxy or 2-6C alkoxycarbonyl radicals; and provided that when R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are hydrogen, A is a methylene radical and R.sup.6 is a 3-pyridyl radical, R.sup.1 is not a cyano, hydroxy or hydroxymethyl radical, and when R.sup.1 is a hydroxy radical, R.sup.3, R.sup.4 and R.sup.5 are hydrogen, A is a methylene radical and R.sup.6 is 3-pyridyl, R.sup.2 is not a methyl or a 2-chloro-1-methylethyl radical, and provided that when R.sup.1 is a methoxycarbonyl radical, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are hydrogen and A is a methylene radical, R.sub.1 is not a 1H-imidazol-1-yl radical; and the pharmaceutically acceptable acid addition salts thereof.

    (Substituted aralkyl) heterocyclic compounds
    7.
    发明授权
    (Substituted aralkyl) heterocyclic compounds 失效
    （取代的芳烷基）杂环化合物

    公开(公告)号：US4935437A

    公开(公告)日：1990-06-19

    申请号：US204743

    申请日：1988-06-10

    申请人： Philip N. Edwards ,  Michael S. Large

    发明人： Philip N. Edwards ,  Michael S. Large

    IPC分类号： A61K31/395 ,  A61K31/40 ,  A61K31/41 ,  A61K31/415 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/4418 ,  A61K31/445 ,  A61K31/505 ,  A61K31/535 ,  A61K31/5375 ,  A61P3/00 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  C07D213/46 ,  C07D213/57 ,  C07D233/60 ,  C07D233/61 ,  C07D233/64 ,  C07D233/90 ,  C07D239/26 ,  C07D249/08 ,  C07D295/18 ,  C07D521/00

    CPC分类号： C07D239/26 ,  C07D213/57 ,  C07D231/12 ,  C07D233/56 ,  C07D233/90 ,  C07D249/08

    摘要： A (substituted-aralkyl)heterocyclic compound of the formula I ##STR1## wherein R.sup.1 is an azido, carbamoyl, cyano, formyl, hydroxy or nitro radical, a 1-6C 1-hydroxyalkyl, alkoxy, alkylcarbamoyl, alkylthio, alkylsulphinyl or alkylsulphonyl radical, a 2-cyanoethyl radical, optionally bearing one to four 1-6C alkyl substituents, or a 2-6C alkanoyl, halogenoalkanoyl, alkanoyloxy, alkanoylamino, dialkylcarbamoyl or alkoxycarbonyl radical; R.sup.2 and R.sup.3, which may be the same or different, are each a hydrogen atom, a 1-6C alkyl, dueterioalkyl or halogenoalkyl radical, or a phenyl or phenyl(1-6C alkyl) radical, in each of which the phenyl may optionally bear one or more substituents; or R.sup.2 and R.sup.3, together with the carbon atom to which they are attached, may form a 3- to 6-membered ring; or R.sup.1 R.sup.2 R.sup.3 C- is a 1,1-dicyanoethyl or trifluoromethylsulphonyl radical; R.sup.4 is a hydrogen or halogen atom, a cyano or nitro radical or a 1-6C alkyl or halogenoalkyl radical; R.sup.5 has any of the values defined above for the group R.sup.1 R.sup.2 R.sup.3 C but is not necessarily the same as R.sup.1 R.sup.2 R.sup.3 C, or has any of the values defined above for R.sup.4 but is not necesarily the same as R.sup.4, or is a carbamoyl, 1-pyrrolidinyl-carbonyl, piperidinocarbonyl, morpholinocarbonyl or nitro radical, a 1-6C alkoxy or halogenoalkoxy radical or a 2-6C alkanoyl or alkoxy-carbonyl radical; A is a methylene or ethylene radical optionally bearing one or more substituents selected from deuterium and halogen atoms, carbamoyl, cyano and hydroxy radicals, 1-6C alkyl and alkoxy radicals, and 2-6C alkanoyloxy radicals provided that when A is linked to R.sup.6 through a nitrogen atom thereof, it may not bear a hydroxy, alkoxy or alkanoyloxy substituent on the carbon atom adjacent to such nitrogen atoms; and R.sup.6 is a 1H-1,2,4-triazol-1-yl, 4H-1,2,4-triazol-4-yl, 1H-imidazol-1-yl, 5-cyano-1H-imidazol-1-yl, 3-pyridyl or 5-pyrimidinyl radical, or a 1H-imidazol-1-yl radical, bearing at the 5-position thereof a 1-6C alkyl substituent which is itself optionally substituted by one or more carbamoyl, cyano, hydroxy or 2-6C alkoxycarbonyl radicals; and provided that when R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are hydrogen, A is a methylene radical and R.sup.6 is a 3-pyridyl radical, R.sup.1 is not a cyano, hydroxy or hydroxymethyl radical, and when R.sup.1 is a hydroxy radical, R.sup.3, R.sup.4 and R.sup.5 are hydrogen, A is a methylene radical and R.sup.6 is 3-pyridyl, R.sup.2 is not a methyl or a 2-chloro-1-methylethyl radical, and provided that when R.sup.1 is a methoxycarbonyl radical, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are hydrogen and A is a methylene radical, R.sub.1 is not a 1H-imidazol-1-yl radical; and the pharmaceutically acceptable acid addition salts thereof.

    4,4'-Alkylenedipiperidine derivatives
    10.
    发明授权
    4,4'-Alkylenedipiperidine derivatives 失效
    4,4'-亚烷基二哌啶衍生物

    公开(公告)号：US4574123A

    公开(公告)日：1986-03-04

    申请号：US606688

    申请日：1984-05-03

    申请人： Philip N. Edwards ,  Michael S. Large

    发明人： Philip N. Edwards ,  Michael S. Large

    IPC分类号： A01N47/44 ,  A61K31/445 ,  A61P31/04 ,  C07C279/28 ,  C07D211/06 ,  C07D211/16 ,  C07D401/14 ,  A01N43/40

    CPC分类号： C07C279/28 ,  C07D211/06 ,  C07D211/16

    摘要： A 4,4'-alkylenebis[piperidine-1-(N-amidinoamidine)] derivative of the formula: ##STR1## or a tautomeric form thereof, wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, is hydrogen or an alkyl, alkenyl or alkoxyalkyl radical of up to 20 carbon atoms; or R.sup.1, R.sup.2 and the nitrogen atom to which they are attached, or R.sup.3 and R.sup.4 and the nitrogen atom to which they are attached, which may be the same or different, are each a 1-azetidinyl, 1-pyrrolidinyl, piperidino, hexamethyleneimino, heptamethyleneimino, morpholino or 4-(1-8C alkanoyl)-1-piperazinyl radical each of which may bear 1-3C alkyl substituents; a 3-20C cycloalkyl radical; or an optionally substituted phenyl or phenylalkyl radical; provided that at least one of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is other than hydrogen; X is a direct bond or a 1-6C straight- or branched-chain alkylene radical which is linked to the 3- or 4-positions of the piperidine rings; and R.sup.5 and R.sup.6, which may be the same or different, are each hydrogen or a 1-8C alkyl radical; and the acid addition salts thereof, processes for their manufacture, and antibacterial and antifungal compositions and methods using said compounds.

    摘要翻译： 具有下式的4,4'-亚烷基双[哌啶-1-（N-脒基脒））衍生物或其互变异构形式，其中R 1，R 2，R 3， R 2，R 3和R 4可以相同或不同，是氢或至多20个碳原子的烷基，烯基或烷氧基烷基; 或它们所连接的R 1，R 2和它们所连接的氮原子，或者R 3和R 4及它们所连接的氮原子可以相同或不同，分别为1-氮杂环丁烷基，1-吡咯烷基，哌啶子基，六亚甲基亚氨基 ，七亚甲基亚氨基，吗啉代或4-（1-8C烷酰基）-1-哌嗪基，其各自可以具有1-3C烷基取代基; 3-20C环烷基; 或任选取代的苯基或苯基烷基; 条件是R 1，R 2，R 3和R 4中的至少一个不是氢; X是与哌啶环的3-或4-位连接的直接键或1-6C直链或支链亚烷基; R 5和R 6可以相同或不同，分别为氢或1-8C烷基; 及其酸加成盐，其制备方法，以及使用所述化合物的抗菌和抗真菌组合物和方法。