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30 条记录 (耗时 0.037 秒)

    Aromatic ring derivatives
    22.
    发明授权
    Aromatic ring derivatives 失效
    芳香环衍生物

    公开(公告)号：US06242474B1

    公开(公告)日：2001-06-05

    申请号：US09446619

    申请日：2000-03-21

    申请人： Noritsugu Yamasaki ,  Takafumi Imoto ,  Takahiro Hiramura ,  Osamu Onomura ,  Masahiro Nishikawa ,  Hiroshi Kayakiri ,  Yoshito Abe ,  Hitoshi Hamashima ,  Hitoshi Sawada

    发明人： Noritsugu Yamasaki ,  Takafumi Imoto ,  Takahiro Hiramura ,  Osamu Onomura ,  Masahiro Nishikawa ,  Hiroshi Kayakiri ,  Yoshito Abe ,  Hitoshi Hamashima ,  Hitoshi Sawada

    IPC分类号： A61K314164

    CPC分类号： C07D213/78 ,  C07C311/51 ,  C07D213/81 ,  C07D233/64 ,  C07D233/68 ,  C07D409/06

    摘要： Novel aromatic ring derivatives represented by formula (I) or their pharmaceutical acceptable salts are provided. wherein Nu represents a 5- or 6-membered aromatic ring; ch1 and ch2 each represents a cross-linking group; and A represents an aromatic ring. These compounds have blood sugar-depressing activity or PDE 5 inhibitory activity and are useful as medicines for treating impaired glucose tolerance, diabetes, diabetic complications, syndrome of insulin-resistance, polycystic ovary syndrome, hyperlipidemia, atherosclerosis, cardiovascular disorders, hyperglycemia, hypertension, stenocardia, pulmonary hypertension, congestive heart failure, glomerulopathy, tubulointerstitial disorders, renal failure, angiostenosis, distal angiopathy, cerebral apoplexy, chronic reversible obstructions, autoimmune diseases, allergic rhinitis, urticaria, glaucoma, diseases characterized by enteromotility disorders, impotence, nephritis, cachexia, pancreatitis, restenosis after PTCA, etc.

    摘要翻译： 提供由式（I）表示的新颖芳环衍生物或其药学上可接受的盐。其中Nu表示5-或6-元芳环; ch1和ch2各自表示交联基团; 并且A代表芳香环。这些化合物具有抑制血糖的活性或PDE 5抑制活性，可用作治疗糖耐量异常，糖尿病，糖尿病并发症，胰岛素抵抗综合征，多囊卵巢综合症，高脂血症，动脉粥样硬化， 心血管疾病，高血糖症，高血压，心律失常，肺动脉高压，充血性心力衰竭，肾小球病，肾小管间质性疾病，肾衰竭，血管狭窄，远端血管病，脑中风，慢性可逆障碍，自身免疫性疾病，过敏性鼻炎，荨麻疹，青光眼，以肠蠕动为特征的疾病 疾病，阳ence，肾炎，恶病质，胰腺炎，PTCA后再狭窄等。

    Compounds capable of cleaving double-stranded DNA and method of utilization of the same
    23.
    发明授权
    Compounds capable of cleaving double-stranded DNA and method of utilization of the same 失效
    能切割双链DNA的化合物及其利用方法

    公开(公告)号：US06713633B1

    公开(公告)日：2004-03-30

    申请号：US09701264

    申请日：2001-08-08

    申请人： Hiroshi Sugiyama ,  Zhi-Fu Tao ,  Isao Saito

    发明人： Hiroshi Sugiyama ,  Zhi-Fu Tao ,  Isao Saito

    IPC分类号： A61K314164

    CPC分类号： A61K31/407 ,  C07D487/04

    摘要： Novel chemical species capable of simultaneously alkylating double-stranded DNA and cleaving the same; methods for alkylating and cleaving DNA by using these species; and anticancer agents with the use of these compounds. Compounds represented by the following general formula (I) which are capable of simultaneously alkylating double-stranded DNA and cleaving the same; a method for alkylating DNA and a method for cleaving double stranded DNA by using these compounds; and medicinal compositions with the use of these compounds: B—L—A(I) wherein B represents a chemical structure capable of recognizing the base sequence of DNA, for example, optionally substituted pyrrole-imidazole polyamide; A represents a chemical structure capable of binding to one base of DNA, for example, the alkylation moiety of duocarmycin A; and L represents a linker capable of binding the chemical structures A and B, for example, vinyl.

    摘要翻译： 能够同时烷化双链DNA并切割相同的新型化学物质; 通过使用这些物质烷基化和切割DNA的方法; 和使用这些化合物的抗癌剂。 由以下通式（I）表示的化合物，其能够同时烷基化双链DNA并将其切割; 用于烷基化DNA的方法和通过使用这些化合物切割双链DNA的方法; 和使用这些化合物的药物组合物：B-L-A（I）其中B表示能够识别DNA碱基序列的化学结构，例如任选取代的吡咯 - 咪唑聚酰胺; A表示能够结合DNA的一个碱基的化学结构，例如二焦耳霉素A的烷基化部分; L表示能够结合化学结构A和B的接头，例如乙烯基。

    &bgr;3 adrenergic receptor agonists and uses thereof
    24.
    发明授权
    &bgr;3 adrenergic receptor agonists and uses thereof 失效
    β3肾上腺素能受体激动剂及其用途

    公开(公告)号：US06706743B2

    公开(公告)日：2004-03-16

    申请号：US10379976

    申请日：2003-03-05

    申请人： Robert F. Day ,  Jennifer A. Lafontaine

    发明人： Robert F. Day ,  Jennifer A. Lafontaine

    IPC分类号： A61K314164

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D249/08 ,  C07D263/32 ,  C07D271/06 ,  C07D271/10 ,  C07D277/24 ,  C07D285/06 ,  C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

    摘要： The instant invention provides &bgr;3 adrenergic receptor agonists of structural Formula (I), the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers and prodrugs, wherein Ar, R, R1, R2, R3, R4, R5, R6, R7, R8, X, and Y, are as defined herein. The invention further provides intermediates useful in the preparation of the compounds of Formula (I), to combinations of the compounds of Formula (I), the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers and prodrugs, with anti-obesity agents; to pharmaceutical compositions comprising the compounds of Formula (I), the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers and prodrugs, or pharmaceutical compositions comprising the compounds of Formula (I), the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers and prodrugs, and anti-obesity agents; and methods of treating &bgr;3 adrenergic receptor-mediated diseases, conditions, or disorders in a mammal which methods comprise administering to the mammal an effective amount of a compound of Formula (I), a stereoisomer or prodrug thereof, or a pharmaceutical composition thereof; or a combination of a compound of Formula (I), a pharmaceutically acceptable salt of the compound, stereoisomer, or prodrug, and an anti-obesity agent, or a pharmaceutical composition thereof.

    摘要翻译： 本发明提供结构式（I）的β3肾上腺素能受体激动剂，其立体异构体和前药以及化合物，立体异构体和前药的药学上可接受的盐，其中Ar，R，R 1，R 2，R 3，R 4，R 5，R 6 ，R7，R8，X和Y如本文所定义。本发明还提供可用于制备式（I）化合物的中间体，式（I）化合物，其立体异构体和前药的组合， 和化合物，立体异构体和前药的药学上可接受的盐与抗肥胖剂; 包括式（I）化合物，其立体异构体和前药以及化合物，立体异构体和前药的药学上可接受的盐或包含式（I）化合物的药物组合物，其立体异构体和前药以及 化合物的药学上可接受的盐，立体异构体和前药以及抗肥胖剂; 以及治疗哺乳动物中β3肾上腺素能受体介导的疾病，病症或病症的方法，所述方法包括向哺乳动物施用有效量的式（I）化合物，其立体异构体或前药或其药物组合物; 或式（I）的化合物，化合物的药学上可接受的盐，立体异构体或前药，和抗肥胖剂或其药物组合物的组合。

    Imidazole derivatives having affinity for &agr;2 receptors
    29.
    发明授权
    Imidazole derivatives having affinity for &agr;2 receptors 有权
    对α2受体具有亲和力的咪唑衍生物

    公开(公告)号：US06479530B2

    公开(公告)日：2002-11-12

    申请号：US09904836

    申请日：2001-07-16

    申请人： Arto Karjalainen ,  Paavo Huhtala ,  Juha-Matti Savola ,  Siegfried Wurster ,  Maire Eloranta ,  Maarit Hillilä ,  Raimo Saxlund ,  Victor Cockcroft ,  Arja Karjalainen

    发明人： Arto Karjalainen ,  Paavo Huhtala ,  Juha-Matti Savola ,  Siegfried Wurster ,  Maire Eloranta ,  Maarit Hillilä ,  Raimo Saxlund ,  Victor Cockcroft ,  Arja Karjalainen

    IPC分类号： A61K314164

    CPC分类号： C07D233/56 ,  C07D233/64

    摘要： Imidazole derivatives of formula I wherein n is 0 or 1, R1 is hydrogen or C1-C4-alkyl, R2 is hydrogen or R2 and R3 together form a double bond, R3 is hydrogen or C1-C4-alkyl or R2 and R3 together form a double bond, R4 is hydrogen, C1-C4-alkyl, hydroxy or C1-C4-alkoxy, R5 is hydrogen or C1-C4-alkyl or R4 and R5 together with the carbon atom to which they are attached form a carbonyl group, R6, R7 and R8 are each the same or different and are independently hydrogen, C1-C4-alkyl or C2-C4-alkenyl, C3-C7-cycloalkyl, hydroxy, C1-C4-alkoxy, C1-C4-hydroxyalkyl, thiol, C1-4-alkylthio, C1-4-alkylthiol, halogen, trifluoromethyl, nitro or optionally substituted amino, X is —CHR9—(CHR10)m—, m is 0 or 1, and R9 and R10 are each the same or different and are independently hydrogen or C1-C4-alkyl; or a pharmaceutically acceptable ester or salt thereof, their preparation, use and pharmaceutical compositions comprising them are described. The compounds have affinity for alpha2 receptors and are useful e.g. in the treatment of hypertension, glaucoma, chronic or acute pain, migraine, diarrhea, common cold, ischemia, addiction to chemical substances, anxiety, especially preoperative anxiety and different neurological, musculoskeletal, psychiatric and cognition disorders or as adjuncts to anesthesia.

    摘要翻译： 式I的咪唑衍生物，其中n为0或1，R 1为氢或C 1 -C 4 - 烷基，R 2为氢或R 2和R 3一起形成双键，R 3为氢或C 1 -C 4烷基或R 2和R 3一起形成 R 2是氢，C 1 -C 4 - 烷基，羟基或C 1 -C 4 - 烷氧基，R 5是氢或C 1 -C 4 - 烷基或R 4和R 5与它们所连接的碳原子一起形成羰基，R 6 ，R 7和R 8各自相同或不同，独立地为氢，C 1 -C 4 - 烷基或C 2 -C 4 - 烯基，C 3 -C 7 - 环烷基，羟基，C 1 -C 4 - 烷氧基，C 1 -C 4 - 羟基烷基，硫醇，C 1 4-烷硫基，C 1-4 - 烷基硫醇，卤素，三氟甲基，硝基或任选取代的氨基，X是-CHR 9 - （CHR 10）m - ，m是0或1，并且R 9和R 10各自相同或不同， 独立地是氢或C 1 -C 4 - 烷基; 或其药学上可接受的酯或其盐，描述了它们的制备，用途和包含它们的药物组合物。 该化合物对α2受体具有亲和性，并且可用于例如 在治疗高血压，青光眼，慢性或急性疼痛，偏头痛，腹泻，感冒，局部缺血，化学物质成瘾，焦虑症，特别是术前焦虑和不同的神经系统，肌肉骨骼，精神和认知障碍或麻醉的辅助治疗。