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8 条记录 (耗时 0.025 秒)

    Substituted 1,4-benzodiazepines and uses thereof
    2.
    发明授权
    Substituted 1,4-benzodiazepines and uses thereof 失效
    取代的1,4-苯并二氮杂及其用途

    公开(公告)号：US07067512B2

    公开(公告)日：2006-06-27

    申请号：US10292876

    申请日：2002-11-13

    申请人： Tianbao Lu ,  Louis V Lafrance, III ,  Daniel J Parks ,  Karen L Milkiewicz ,  Raul R Calvo ,  Maxwell D Cummings ,  Alexander J Kim ,  Bruce L Grasberger ,  Theodore E Carver, Jr.

    发明人： Tianbao Lu ,  Louis V Lafrance, III ,  Daniel J Parks ,  Karen L Milkiewicz ,  Raul R Calvo ,  Maxwell D Cummings ,  Alexander J Kim ,  Bruce L Grasberger ,  Theodore E Carver, Jr.

    IPC分类号： C07D243/12 ,  C07D243/18 ,  C07D243/24 ,  A61K31/55

    CPC分类号： C07D401/04 ,  C07D243/14 ,  C07D403/10 ,  C07D405/04 ,  C07D409/04

    摘要： The present invention is directed to novel 1,4-benzodiazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions. Compounds have Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein: X and Y are independently —C(O)—, —CH2— or —C(S)—; R1, R2, R3, R4, R7, R8, Rb, Rc, Rd and M are defined herein; R5 is hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aralkyl, optionally substituted heteroaralkyl, carboxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, aminocarbonyl, aminocarbonylalkyl, alkylaminocarbonyl or alkylaminocarbonylalkyl; R6 is cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, aralkyl, heteroarylalkyl, or a saturated or partially unsaturated heterocycle, each of which is optionally substituted; R9 is cycloalkyl, aryl, heteroaryl, a saturated or partially unsaturated heterocycle, cycloalkyl(alkyl), aralkyl or heteroarylalkyl, each of which is optionally substituted; and R10 is —(CH2)n—CO2Rb, —(CH2)m—CO2M, —(CH2)i—OH or —(CH2)j—CONRcRd n is 0–8, m is 0–8, i is 1–8 and j is 0–8.

    摘要翻译： 本发明涉及新的1,4-苯二氮卓类药物，其药物组合物及其作为HDM2-p53相互作用抑制剂的用途。 化合物具有式I：或其溶剂合物，水合物或其药学上可接受的盐; 其中：X和Y独立地为-C（O） - ， - CH 2 - 或-C（S） - ; R 1，R 2，R 3，R 4，R 7， R 8，R b，R c，R d和M在本文中定义; R 5是氢，烷基，环烷基，任选取代的芳基，任选取代的杂芳基，任选取代的芳烷基，任选取代的杂芳烷基，羧基烷基，烷氧基羰基，烷氧基羰基烷基，氨基羰基，氨基羰基烷基，烷基氨基羰基或烷基氨基羰基烷基; R 6是环烷基，芳基，杂芳基，环烷基烷基，芳烷基，杂芳基烷基或饱和或部分不饱和的杂环，其各自任选被取代; R 9是环烷基，芳基，杂芳基，饱和或部分不饱和的杂环，环烷基（烷基），芳烷基或杂芳基烷基，其各自任选被取代; 和R 10是 - （CH 2）n - - - - - - （CH 2）n - ， - （CH 2）2 - ， - M 2 - ， - （CH 2） -OH或 - （CH 2 CH 2）n -CONR C n R n为0-8 ，m为0-8，i为1-8，j为0-8。

    Benzimidazole derivatives useful as TRP M8 receptor modulators
    3.
    发明授权
    Benzimidazole derivatives useful as TRP M8 receptor modulators 有权
    可用作TRP M8受体调节剂的苯并咪唑衍生物

    公开(公告)号：US08217060B2

    公开(公告)日：2012-07-10

    申请号：US12773083

    申请日：2010-05-04

    申请人： Raul R. Calvo ,  Sanath K. Meegalla ,  Mark R. Player

    发明人： Raul R. Calvo ,  Sanath K. Meegalla ,  Mark R. Player

    IPC分类号： A61K31/41 ,  A61K31/415

    CPC分类号： C07D235/08 ,  C07D235/10 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06

    摘要： The present invention is directed to benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8 (transient receptor potential M8 channel). More particularly, the compounds of the present invention are useful in the treatment of inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold, anxiety and depression.

    摘要翻译： 本发明涉及苯并咪唑衍生物，含有它们的药物组合物及其在治疗由TRP M8（瞬时受体电位M8通道）调节的病症和状况中的用途。 更具体地说，本发明的化合物可用于治疗炎症性疼痛，炎性痛觉过敏，炎性过敏症状，神经性疼痛，神经性寒冷异常性疼痛，炎症性体征痛觉过敏，炎性内脏痛觉过敏，由冷，焦虑和抑郁加重的心血管疾病。

    Substituted 1,4-diazepines and uses thereof
    8.
    发明授权
    Substituted 1,4-diazepines and uses thereof 有权
    取代的1,4-二氮杂及其用途

    公开(公告)号：US07115598B2

    公开(公告)日：2006-10-03

    申请号：US10829040

    申请日：2004-04-21

    申请人： Tianbao Lu ,  Karen L. Milkiewicz ,  Pierre Raboisson ,  Maxwell David Cummings ,  Raul R. Calvo ,  Daniel J. Parks ,  Louis V. Lafrance, III ,  Juan Jose Marugan Sanchez ,  Joan Gushue ,  Kristi Leonard

    发明人： Tianbao Lu ,  Karen L. Milkiewicz ,  Pierre Raboisson ,  Maxwell David Cummings ,  Raul R. Calvo ,  Daniel J. Parks ,  Louis V. Lafrance, III ,  Juan Jose Marugan Sanchez ,  Joan Gushue ,  Kristi Leonard

    IPC分类号： C07D243/14 ,  A61K31/55

    CPC分类号： C07D243/14

    摘要： The present invention is directed to novel 1,4-diazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions. Compounds have Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein: R1, R2, R9, R10, Ra, Rd and M are defined herein;X is a bivalent radical of: an alkane, a cycloalkane, an optionally-substituted arene, an optionally-substituted heteroarene, an optionally-substituted arylalkane or an optionally-substituted heteroarylalkane; andR3 is —CO2Rd, —CO2M, —OH, —NHRd, —SO2Rd, —NHCONHRd, optionally-substituted amidino or optionally-substituted guanidino;or R3—X— is hydrogen or an electron pair;R4 is oxygen or —NR9R10;R5 is cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, aralkyl, heteroarylalkyl, or a saturated or partially unsaturated heterocycle, each of which is optionally substituted; andR6, R7 and R8 are independently hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, a saturated or partially unsaturated heterocycle, cycloalkylalkyl, aralkyl or heteroarylalkyl, each of which is optionally substituted; or R6 and R7, together with the carbon atom to which they are attached form a 3- to 7-membered carbocyclic ring optionally substituted 1 to 3 times with Ra.

    摘要翻译： 本发明涉及新的1,4-二氮杂，其药物组合物及其作为HDM2-p53相互作用抑制剂的用途。 化合物具有式I：或其溶剂合物，水合物或其药学上可接受的盐; 其中：R 1，R 2，R 9，R 10，R a， >，R d和M在本文中定义; X是二价基团：烷烃，环烷烃，任选取代的芳烃，任选取代的杂芳烃，任选取代的芳基烷烃或任选取代的杂芳基烷烃; 和R 3是-CO 2 R 2，-CO 2 M，-OH，-NHR 0 任选取代的脒基或任选取代的胍基;其中R 1，R 2，R 3，R 4， 或R 3 -X-是氢或电子对; R 4是氧或-NR 9 R 10; R 5是环烷基，芳基，杂芳基，环烷基烷基，芳烷基，杂芳基烷基或饱和或部分不饱和的杂环，其各自任选被取代; R 6和R 8独立地是氢，烷基，环烷基，芳基，杂芳基，饱和或部分不饱和的杂环，环烷基烷基 ，芳烷基或杂芳基烷基，其各自任选被取代; 或R 6和R 7与它们所连接的碳原子一起形成3-至7-元碳环，任选地被R 1取代1至3倍， SUP> a 。