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30 条记录 (耗时 0.033 秒)

    Small molecules useful in the treatment of inflammatory disease
    4.
    发明授权
    Small molecules useful in the treatment of inflammatory disease 有权
    用于治疗炎性疾病的小分子

    公开(公告)号：US06353013B1

    公开(公告)日：2002-03-05

    申请号：US09605574

    申请日：2000-06-28

    申请人： Terence Alfred Kelly ,  Ronald John Sorcek

    发明人： Terence Alfred Kelly ,  Ronald John Sorcek

    IPC分类号： A61K314164

    CPC分类号： C07D233/76

    摘要： Novel compounds of the formula I which are useful for treating or preventing inflammatory and immune cell-mediated diseases. Exemplary compounds are: 5-(R)-(4-bromobenzyl)-3-(3-chloro-5-nitrophenyl)-5-methylimidazoline-2,4-dione; and, 5-(R)-(4-bromobenzyl)-3-(3-chloro-5-cyanophenyl)-5-methylimidazoline-2,4-dione.

    摘要翻译： 新颖的式I化合物，其可用于治疗或预防炎性和免疫细胞介导的疾病。 示例性化合物是：5-（R） - （4-溴苄基）-3-（3-氯-5-硝基苯基）-5-甲基咪唑啉-2,4-二酮; 和5-（R） - （4-溴苄基）-3-（3-氯-5-氰基苯基）-5-甲基咪唑啉-2,4-二酮。

    Alicyclic imidazoles as H3 agents
    6.
    发明授权
    Alicyclic imidazoles as H3 agents 失效
    脂环族咪唑作为H3剂

    公开(公告)号：US06794405B2

    公开(公告)日：2004-09-21

    申请号：US10344787

    申请日：2003-08-04

    申请人： Yajing Rong ,  Jack B. Jiang ,  Syed M. Ali

    发明人： Yajing Rong ,  Jack B. Jiang ,  Syed M. Ali

    IPC分类号： A61K314164

    CPC分类号： C07D233/64

    摘要： Alicyclic imidazole compounds; pharmaceutically active compositions containing such compounds; and the use of such compounds in formulations for the control or prevention of disease states in which histamine H3 receptors are involved, such as allergy, inflammation, hypotension, glaucoma, sleeping disorders, states of hyper- and hypo-motility of the gastro-intestinal tract, cardiovascular disease, hypo- and hyper-activity of the central nervous system, Alzheimer's, schizophrenia, obesity and migraines are disclosed.

    摘要翻译： 脂环咪唑化合物; 含有这些化合物的药物活性组合物; 以及这些化合物在制剂中的用途，用于控制或预防其中涉及组胺H3受体的疾病状态，例如过敏，炎症，低血压，青光眼，睡眠障碍，胃肠超和运动不足的状态 公开了中枢神经系统，阿尔茨海默病，精神分裂症，肥胖症和偏头痛的低血压，高血压，心脑血管疾病，低血压和高活性。

    Cationic lipids
    7.
    发明授权
    Cationic lipids 有权

    公开(公告)号：US06610664B2

    公开(公告)日：2003-08-26

    申请号：US10162963

    申请日：2002-06-04

    申请人： Kuei-Ying Lin ,  Mark D. Mattuecci

    发明人： Kuei-Ying Lin ,  Mark D. Mattuecci

    IPC分类号： A61K314164

    CPC分类号： C07D233/64 ,  A61K38/00 ,  C07K5/06026 ,  C07K5/06147 ,  C07K5/0806 ,  Y10T436/207497

    摘要： The present invention is directed to new cationic lipids and intermediates in their synthesis that are useful for transfecting nucleic acids or peptides into prokaryotic or eukaryotic cells. The lipids comprise one or two substituted histidine residues, or similar compounds, linked to a lipophilic moiety. The lipids form a complex when mixed with polyanions such as nucleic acids or peptides. The complexes permit efficient transfer of polyanions into cells, usually without significant toxicity to the cells.

    Heterocyclic compound, composition and method for inhibiting adenosine deaminase
    8.
    发明授权
    Heterocyclic compound, composition and method for inhibiting adenosine deaminase 失效
    杂环化合物，抑制腺苷脱氨酶的组合物和方法

    公开(公告)号：US06596738B1

    公开(公告)日：2003-07-22

    申请号：US09926134

    申请日：2001-09-07

    申请人： Tadashi Terasaka ,  Nobuo Seki ,  Kiyoshi Tsuji ,  Isao Nakanishi ,  Takayoshi Kinoshita ,  Katsuya Nakamura

    发明人： Tadashi Terasaka ,  Nobuo Seki ,  Kiyoshi Tsuji ,  Isao Nakanishi ,  Takayoshi Kinoshita ,  Katsuya Nakamura

    IPC分类号： A61K314164

    CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56 ,  C07D233/90 ,  C07D249/10 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04 ,  C07F7/1804 ,  Y02P20/55

    摘要： Heterocyclic compounds of the following formula: wherein B is  [wherein R1 is hydrogen or lower alkyl; R2 is hydrogen or lower alkyl; and X is hydrogen or hydroxy protective group], lower alkanoyl or hydroxyimino(lower)alkyl A is lower alkylene; W is heterocyclic or carbocyclic group, each of which may have one or more substituent(s); Z is heterocyclic group selected from the group consisting of imidazolyl, triazolyl,imidazopyridyl and adenyl, each of which may have one or more substituent(s); or a salt thereof, provided that when W is aryl which may have one or more substituent(s), then (i) Z is triazolyl, imidazopyridyl or adenyl, each of which may have one or more substituent(s); (ii) Z is imidazolyl which may have one or more substituent(s) and B is lower alkanoyl or hydroxyimino(lower)alkyl; or (iii) Z is imidazolyl which may have one or more substituent(s) and R1 and R2 are both lower alkyl. or pharmaceutically acceptable salts thereof, which are useful as a medicament.

    摘要翻译： 下式的杂环化合物：其中B是[其中R 1是氢或低级烷基; R 2是氢或低级烷基; 和X是氢或羟基保护基]，低级烷酰基或羟基亚氨基（低级）烷基A是低级亚烷基; W是杂环或碳环基，每一个可以具有一个或多个取代基; Z是选自 咪唑基，三唑基，咪唑并吡啶基和腺嘌呤，其各自可以具有一个或多个取代基;或其盐，条件是当W是可以具有一个或多个取代基的芳基时，则（i）Z是 三唑基，咪唑并吡啶基或腺苷酸，其各自可以具有一个或多个取代基; （ii）Z是可以具有一个或多个取代基的咪唑基，B是低级烷酰基或羟基亚氨基（低级）烷基; 或（iii）Z是可具有一个或多个取代基的咪唑基，R 1和R 2均为低级烷基或其药学上可接受的盐，其可用作药物。

    Substituted imidazole derivatives and their use as histamine H3 receptor ligands
    9.
    发明授权
    Substituted imidazole derivatives and their use as histamine H3 receptor ligands 失效
    取代的咪唑衍生物及其作为组胺H3受体配体的用途

    公开(公告)号：US06407132B1

    公开(公告)日：2002-06-18

    申请号：US09463445

    申请日：2000-03-13

    申请人： Sarkis Barret Kalindjian ,  Ildiko Maria Buck

    发明人： Sarkis Barret Kalindjian ,  Ildiko Maria Buck

    IPC分类号： A61K314164

    CPC分类号： C07D233/64 ,  Y10S435/968 ,  Y10S435/975

    摘要： Compounds of formula (I) and their pharmaceutically acceptable salts are useful as histamine H3 receptor ligands. R1 and R3 are optional substituents such as C1 to C6 alkyl. R2 represents a bond or C1 to C5 (preferably C1 to C3) hydrocarbylene; R4 represents a bond or C1 to C5 (preferably C1 to C3) hydrocarbylene; R5 is hydrogen, C1 to C3 alkyl, R8—O—(C1 to C3)alkyl (wherein R8 is hydrogen or C1 to C3 alkyl), aryl, aryl(C1 to C3)alkyl; R6 represents a bond or —NR9—, wherein R9 is any of the groups mentioned above for R5; R7 is H or C1 to C15 hydrocarbyl (in which one or more hydrogen atoms may be replaced by halogen, and up to three carbon atoms may be replaced by oxygen, nitrogen or sulfur atoms); a is from 0 to 2; and b is from 0 to 3.

    摘要翻译： 式（I）化合物及其药学上可接受的盐可用作组胺H3受体配体。 R 1和R 3是任选的取代基，例如C 1至C 6烷基。 R2表示键或C1至C5（优选C1至C3）亚烃基; R4表示键或C1至C5（优选C1至C3）亚烃基; R 5为氢，C 1至C 3烷基，R 8 -O-（C 1至C 3）烷基（其中R 8为氢或C 1至C 3烷基），芳基，芳基（C 1至C 3） R 6表示键或-NR 9 - ，其中R 9是上述对R 5的任何基团; R 7是H或C 1至C 15烃基（其中一个或多个氢原子可以被卤素取代，并且最多三个碳原子可被氧，氮或硫原子替代）; a为0〜2; b为0〜3。

    1-N-phenylamino-1H-imidazole derivatives as aromatase inhibitors and pharmaceutical compositions containing them
    10.
    发明授权
    1-N-phenylamino-1H-imidazole derivatives as aromatase inhibitors and pharmaceutical compositions containing them 失效
    1-N-苯基氨基-1H-咪唑衍生物作为芳香酶抑制剂和含有它们的药物组合物

    公开(公告)号：US06737433B1

    公开(公告)日：2004-05-18

    申请号：US10319840

    申请日：2002-12-16

    申请人： Nathalie Adje ,  Paule Bonnet ,  Denis Carniato ,  Remi Delansorne ,  Jean Lafay ,  Jean-Claude Pascal

    发明人： Nathalie Adje ,  Paule Bonnet ,  Denis Carniato ,  Remi Delansorne ,  Jean Lafay ,  Jean-Claude Pascal

    IPC分类号： A61K314164

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： Imidazole derivatives of the formula: in which R1 and R2 are each independently hydrogen, (C1-C6)alkyl or (C3-C8)cycloalkyl; n is 0, 1 or 2; R3, R4, R5 and R6 are each independently hydrogen or a (C1-C6)alkyl, halogen, cyano, (C1-C6)alkoxy, trifluoromethyl, (C1-C6)alkylthio, (C1-C6)alkylsulfonyl, sulfonamido, acyl, (C1-C6)alkoxycarbonyl, or carboxamido group; R3 and R6 together with the phenyl ring bearing them can also form a benzofurane, or a N-methylbenzotriazole. The invention also relates to pharmaceutical compositions containing these derivatives, and to the uses thereof.

    摘要翻译： 下式的咪唑衍生物：其中R 1和R 2各自独立地为氢，（C 1 -C 6）烷基或（C 3 -C 8）环烷基; n为0,1或2; R 3，R 4，R 5和R 6各自独立地为氢或 （C1-C6）烷基，卤素，氰基，（C1-C6）烷氧基，三氟甲基，（C1-C6）烷硫基，（C1-C6）烷基磺酰基，亚磺酰氨基，酰基，（C1-C6）烷氧基羰基或甲酰氨基; R3 和R6与带有它们的苯环一起也可以形成苯并呋喃或N-甲基苯并三唑。 本发明还涉及含有这些衍生物的药物组合物及其用途。