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15 条记录 (耗时 0.03 秒)

    Polyprolyl inhibitors of cyclophilin
    1.
    发明申请
    Polyprolyl inhibitors of cyclophilin 审中-公开
    亲环蛋白的多脯氨酰抑制剂

    公开(公告)号：US20040204340A1

    公开(公告)日：2004-10-14

    申请号：US10411333

    申请日：2003-04-11

    申请人： Guilford Pharmaceuticals, Inc.

    发明人： Gregory S. Hamilton ,  Ling Wei ,  Joseph P. Steiner

    IPC分类号： A61K038/17

    CPC分类号： A61K38/08 ,  A61K38/005 ,  A61K38/07

    摘要： This invention relates to neurotrophic low molecular weight, small molecule peptidic cyclophilin inhibitor compounds having an affinity for cyclophilin-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.

    摘要翻译： 本发明涉及具有亲环蛋白型免疫亲和素亲和力的神经营养性低分子量小分子肽亲环蛋白抑制剂化合物，以及它们作为与免疫亲和素蛋白特别是肽基 - 脯氨酰异构酶或旋转异构酶酶活性相关的酶活性的抑制剂的用途。

    Oxo-substituted compounds, process of making, and compositions and methods for inhibiting PARP activity
    4.
    发明申请
    Oxo-substituted compounds, process of making, and compositions and methods for inhibiting PARP activity 审中-公开
    氧化取代的化合物，制备方法以及抑制PARP活性的组合物和方法

    公开(公告)号：US20030105102A1

    公开(公告)日：2003-06-05

    申请号：US10109730

    申请日：2002-04-01

    申请人： Guilford Pharmaceuticals Inc.

    发明人： Jia-He Li ,  Kevin Leonard Tays ,  Jie Zhang

    IPC分类号： A61K031/502 ,  A61K031/517 ,  A61K031/519 ,  A61K031/496 ,  C07D43/02

    CPC分类号： C07D471/06 ,  C07D217/22 ,  C07D217/24 ,  C07D221/12 ,  C07D221/18 ,  C07D237/30 ,  C07D237/32 ,  C07D237/34 ,  C07D239/88 ,  C07D239/93 ,  C07D239/94 ,  C07D475/02 ,  C07D491/04 ,  C07F9/6561

    摘要： Compounds, compositions containing compounds, methods of sing compounds, and processes of making compounds, of formula I containing at least one ring nitrogen: 1 or a pharmaceutically acceptable base or acid addition salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof, wherein: X is double-bonded oxygen or nullOH; when R7 is present, it is hydrogen or lower alkyl; Y represents the atoms necessary to form a fused mono-, bi- or tricyclic, carbocyclic or heterocyclic ring, wherein each individual ring has 5-6 ring member atoms; and Z is (i) nullCHR2CHR3null wherein R2 and R3 are independently hydrogen, alkyl, aryl, or aralkyl; (ii) nullR6CnullCR3null wherein R3 and R6 are independently hydrogen, lower alkyl, aryl, aralkyl, halo, nullNO2, nullCOOR7, or nullNR7R8 where R8 is independently hydrogen or C1-C9 alkyl, or R6 and R3, taken together, form a fused aromatic ring, wherein each individual ring has 5-6 ring members; (iii) nullR2CnullNnull; (iv) nullCR2(OH)nullNR7null; or (v) nullC(O)nullNR7null.

    摘要翻译： 含有化合物的化合物，含有化合物的方法，化合物的制备方法，以及含有至少一个环氮的式I化合物或其药学上可接受的碱或酸加成盐，水合物，酯，溶剂合物，前药，代谢物，立体异构体或 其中：X是双键氧或-OH; 当R7存在时，它是氢或低级烷基; Y表示形成稠合的单，双或三环，碳环或杂环所必需的原子，其中每个单独的环具有5-6个环成员原子; 并且Z是（i）-CHR2CHR3-，其中R2和R3独立地是氢，烷基，芳基或芳烷基; （ⅱ）-R6C = CR3-，其中R3和R6独立地是氢，低级烷基，芳基，芳烷基，卤素，-NO2，-COOR7或-NR7R8，其中R8独立地是氢或C1-C9烷基，或R6和R3， 一起形成稠合芳香环，其中每个单独的环具有5-6个环成员; （iii）-R2C = N- （iv）-CR2（OH）-NR7-; 或（ⅴ）-C（O）-NR7-。

    Fused tricyclic compounds, methods and compositions for inhibiting parp activity
    6.
    发明申请
    Fused tricyclic compounds, methods and compositions for inhibiting parp activity 审中-公开
    稠合三环化合物，抑制parp活性的方法和组合物

    公开(公告)号：US20020160984A1

    公开(公告)日：2002-10-31

    申请号：US10109645

    申请日：2002-04-01

    申请人： Guilford Pharmaceuticals Inc.

    发明人： Jia-He Li ,  Jie Zhang

    IPC分类号： A61K031/675 ,  C07D221/04 ,  A61K031/473

    CPC分类号： C07D221/14 ,  A61K41/0038

    摘要： A compound of formula I: 1 or a pharmaceutically acceptable salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof, wherein the compound of formula I is present in an amount that is effective for treating diabetes; and wherein: Y represents the atoms necessary to form a fused 5- to 6-membered, aromatic or non-aromatic, carbocyclic or heterocyclic ring, wherein Y and any heteroatom(s) therein is unsubstituted or independently substituted with at least one non-interfering hydroxy, amino, nitro, dimethylamino, alkylamino, alkyl, alkenyl, cycloalkyl, cycloalkenyl, aralkyl or aryl substituent; R1 and R3 are independently hydrogen, alkyl, halo, alkenyl, cycloalkyl, cycloalkenyl, aralkyl, aryl, double bonded oxygen, nullCOOR5, or a moiety selected from the group consisting of: 2 wherein R7 is alkyl, alkenyl, cycloalkyl, cycloalkenyl, aralkyl or aryl; R2, when present, is hydrogen, alkyl, alkenyl, amino, cycloalkyl, cycloalkenyl, aralkyl or aryl; R4, R5 and R6 are independently hydrogen, hydroxy, amino, dimethylamino, alkylamino, nitro, alkyl, alkenyl, cycloalkyl, cycloalkenyl, aralkyl or aryl; wherein R2, R4, R5 and R6 are unsubstituted or independently substituted with a moiety selected from the group consisting of alkyl, alkenyl, alkoxy, phenoxy, benzyloxy, cycloalkyl, cycloalkenyl, hydroxy, carboxy, carbonyl, amino, dimethylamino, alkylamino, amido, cyano, isocyano, nitro, nitroso, nitrilo, isonitrilo, imino, azo, diazo, sulfonyl, sulfoxy, thio, thiocarbonyl, alkylthio, sulfhydryl, halo, haloalkyl, trifluoromethyl and aryl.

    摘要翻译： 式I化合物或其药学上可接受的盐，水合物，酯，溶剂化物，前药，代谢物，立体异构体或其混合物，其中式I化合物以有效治疗糖尿病的量存在; 并且其中：Y表示形成稠合的5-至6-元芳族或非芳族，碳环或杂环所必需的原子，其中Y及其中的任何杂原子未被取代或独立地被至少一个非 - 干扰羟基，氨基，硝基，二甲基氨基，烷基氨基，烷基，烯基，环烷基，环烯基，芳烷基或芳基取代基; R 1和R 3独立地是氢，烷基，卤素，烯基，环烷基，环烯基，芳烷基，芳基，双键氧，-COOR 5或选自以下的部分：其中R 7是烷基，烯基，环烷基，环烯基， 或芳基; 当存在时，R2是氢，烷基，烯基，氨基，环烷基，环烯基，芳烷基或芳基; R4，R5和R6独立地是氢，羟基，氨基，二甲基氨基，烷基氨基，硝基，烷基，烯基，环烷基，环烯基，芳烷基或芳基。 其中R2，R4，R5和R6是未取代的或独立地被选自烷基，烯基，烷氧基，苯氧基，苄氧基，环烷基，环烯基，羟基，羧基，羰基，氨基，二甲基氨基，烷基氨基，酰胺基， 氰基，异氰基，硝基，亚硝基，次氮基，异亚硝基，亚氨基，偶氮，重氮，磺酰基，亚砜，硫代，硫代羰基，烷硫基，巯基，卤素，卤代烷基，三氟甲基和芳基。

    Carboxamine compounds, methods and compositions for inhibiting PARP activity
    8.
    发明申请
    Carboxamine compounds, methods and compositions for inhibiting PARP activity 审中-公开
    羧甲基胺化合物，抑制PARP活性的方法和组合物

    公开(公告)号：US20020156050A1

    公开(公告)日：2002-10-24

    申请号：US10109646

    申请日：2002-04-01

    申请人： Guilford Pharmaceuticals Inc.

    发明人： Jia-He Li ,  Jie Zhang

    IPC分类号： A61K031/675 ,  A61K031/5415 ,  A61K031/538 ,  A61K031/517 ,  A61K031/4709

    CPC分类号： C07D257/04 ,  A61K31/16 ,  A61K31/47 ,  C07C233/65 ,  C07C235/84 ,  C07D209/42 ,  C07D215/50 ,  C07D217/24 ,  C07D217/26 ,  C07D221/12 ,  C07D221/18 ,  C07D239/72 ,  C07D307/84 ,  C07D333/68 ,  C07D495/04

    摘要： A compound of formula I: 1 or a pharmaceutically acceptable salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof; wherein: Y represents the atoms necessary to form a fused 5- to 6-membered, aromatic or non-aromatic, carbocyclic or N-containing heterocyclic ring, wherein Y and any heteroatom(s) therein are unsubstituted or independently substituted by at least one non-interfering alkyl, alkenyl, cycloalkyl, cycloalkenyl, aralkyl, aryl, carboxy or halo substituent; X is at the 1-position of ring Y and is nullCOOR5 or a substituted or unsubstituted moiety selected from the group consisting of 2 wherein R7 is hydrogen, alkyl, alkenyl, cycloalkyl or cycloalkenyl, and is itself either unsubstituted or substituted with an alkyl, alkenyl, cycloalkyl or cycloalkenyl group; R1 is hydrogen, alkyl, alkenyl, cycloalkyl or cycloalkenyl, and is itself either unsubstituted or substituted with an alkyl, alkenyl, cycloalkyl or cycloalkenyl group; R2, R3, R4 and R5 are independently hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkenyl, aralkyl, or aryl, and are either unsubstituted or substituted with a moiety selected from the group consisting of alkyl, alkenyl, alkoxy, phenoxy, benzyloxy, cycloalkyl, cycloalkenyl, hydroxy, carboxy, carbonyl, amino, amido, cyano, isocyano, nitro, nitroso, nitrilo, isonitrilo, imino, azo, diazo, sulfonyl, sulfoxy, thio, thiocarbonyl, sulfhydryl, halo, haloalkyl, trifluoromethyl and aryl.

    摘要翻译： 式I化合物或其药学上可接受的盐，水合物，酯，溶剂化物，前药，代谢物，立体异构体或其混合物; 其中：Y表示形成稠合的5-至6-元芳族或非芳族，碳环或含氮杂环所必需的原子，其中Y及其中的任何杂原子是未取代的或独立地被至少一个 非干扰性烷基，烯基，环烷基，环烯基，芳烷基，芳基，羧基或卤素取代基; X为环Y的1-位，为-COOR 5或取代或未取代的部分，其选自由以下组成的组：其中R 7为氢，烷基，烯基，环烷基或环烯基，并且本身未被取代或被烷基取代， 烯基，环烷基或环烯基; R1是氢，烷基，烯基，环烷基或环烯基，并且本身是未取代的或被烷基，烯基，环烷基或环烯基取代; R2，R3，R4和R5独立地是氢，烷基，烯基，环烷基，环烯基，芳烷基或芳基，并且是未取代的或被选自烷基，烯基，烷氧基，苯氧基，苄氧基，环烷基 ，环烯基，羟基，羧基，羰基，氨基，酰胺基，氰基，异氰基，硝基，亚硝基，次氮基，异噻唑基，亚氨基，偶氮，重氮，磺酰基，亚磺酰基，硫代，硫代羰基，巯基，卤素，卤代烷基，三氟甲基和芳基。

    Thioalkyl benzoic acid derivatives
    9.
    发明申请
    Thioalkyl benzoic acid derivatives 有权
    硫代烷基苯甲酸衍生物

    公开(公告)号：US20040198824A1

    公开(公告)日：2004-10-07

    申请号：US10819146

    申请日：2004-04-07

    申请人： Guilford Pharmaceuticals Inc.

    发明人： Takashi Tsukamoto ,  Doris Stoermer ,  Dilrukshi Vitharana

    IPC分类号： C07D321/02 ,  A61K031/19

    CPC分类号： C07C323/62 ,  C07C323/56 ,  C07C323/58

    摘要： The present invention relates to new thiolalkyl benzoic acids, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-null activity, inhibiting angiogenesis, and treating glutamate abnormalities, neuropathy, pain, compulsive disorders, prostate diseases, cancers, glaucoma, retinal disorders, and cancer.

    摘要翻译： 本发明涉及新的硫醇烷基苯甲酸，包含这些化合物的药物组合物和诊断试剂，以及使用这些化合物抑制NAALADase酶活性的方法，检测其中NAALADase水平被改变，影响神经元活性，影响TGF-β活性，抑制 血管生成和治疗谷氨酸异常，神经病，疼痛，强迫症，前列腺疾病，癌症，青光眼，视网膜疾病和癌症。