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    Allosteric Enhancers of th A1 Adenosine Receptor
    1.
    发明申请
    Allosteric Enhancers of th A1 Adenosine Receptor 审中-公开
    A1腺苷受体的变构增强子

    公开(公告)号：US20120108636A1

    公开(公告)日：2012-05-03

    申请号：US13347999

    申请日：2012-01-11

    申请人： Pier Giovanni Baraldi ,  Allan R. Moorman ,  Romeo Romagnoli

    发明人： Pier Giovanni Baraldi ,  Allan R. Moorman ,  Romeo Romagnoli

    IPC分类号： A61K31/4436 ,  C07D409/04 ,  A61K31/381 ,  A61P29/00 ,  A61P9/10 ,  A61P25/08 ,  A61P25/24 ,  A61P9/00 ,  A61P9/06 ,  C07D333/36 ,  A61P25/00

    CPC分类号： C07D333/36 ,  C07D409/04

    摘要： The present invention provides compounds of formula (I) wherein W, R1, R5 and R6 have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric enhancers of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain, and inflammatory pain, cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke, neurological disease or injury, sleep disorders, epilepsy and depression.

    摘要翻译： 本发明提供式（I）化合物，其中W，R 1，R 5和R 6具有本说明书中定义的含义。 式（I）化合物是A1腺苷受体的变构增强子，因此可用于治疗由A1腺苷受体介导的病症。 因此，式（I）化合物可用于治疗疼痛，特别是慢性疼痛如神经性疼痛，炎症性疼痛，心脏病或病症如心脏性心律失常，例如过氧化物室上性心动过速，心绞痛，心肌梗死 和中风，神经系统疾病或损伤，睡眠障碍，癫痫和抑郁症。

    Allosteric adenosine receptor modulators
    7.
    发明授权
    Allosteric adenosine receptor modulators 失效
    变构腺苷受体调节剂

    公开(公告)号：US06727258B2

    公开(公告)日：2004-04-27

    申请号：US09811679

    申请日：2001-03-19

    申请人： Pier Giovanni Baraldi

    发明人： Pier Giovanni Baraldi

    IPC分类号： A61K31519

    CPC分类号： C07D333/36 ,  A61K31/381 ,  A61K31/382 ,  A61K31/4365 ,  A61K31/4436 ,  C07D333/66 ,  C07D333/78 ,  C07D495/04

    摘要： The present invention relates to compounds of formula (IA): the preparation thereof, pharmaceutical formulations thereof, and their use in medicine as allosteric adenosine receptor modulators for uses including protection against hypoxia and ischemia induced injury and treatment of adenosine-sensitive cardiac arrhythmias.

    摘要翻译： 本发明涉及式（IA）化合物：其制备方法，其药物组合物及其在医学中的用途，其用于包括防止缺氧和局部缺血诱导的损伤和治疗腺苷敏感性心律失常的用途的变构腺苷受体调节剂。

    Benzoheterocyclic distamycin derivatives, process for preparing them, and their use as antitumor agents
    8.
    发明授权
    Benzoheterocyclic distamycin derivatives, process for preparing them, and their use as antitumor agents 失效
    苯并杂环类霉素衍生物，其制备方法及其作为抗肿瘤剂

    公开(公告)号：US06458768B1

    公开(公告)日：2002-10-01

    申请号：US09623505

    申请日：2000-09-19

    申请人： Paolo Cozzi ,  Pier Giovanni Baraldi ,  Italo Beria ,  Marina Caldarelli ,  Laura Capolongo ,  Romeo Romagnoli

    发明人： Paolo Cozzi ,  Pier Giovanni Baraldi ,  Italo Beria ,  Marina Caldarelli ,  Laura Capolongo ,  Romeo Romagnoli

    IPC分类号： A61K3800

    CPC分类号： C07D403/14 ,  C07D405/14 ,  C07D409/14

    摘要： Compounds which are benzoheterocyclic distamycin derivatives of formula (I), wherein n is 2, 3 or 4; A is a heteroatom selected from O and S or is a group NR, wherein R is hydrogen or C1-C4 alkyl; B is CH or N; R1 is hydrogen or C1-C4 alkyl; G is selected from the group consisting of (a, b, c, d, e, f, g, h, i, j), and —C≡N; wherein R5, R6, R7, R8, R9, R10, R11 and R12 are, independently from each other, hydrogen or C1-C4 alkyl; T is a group of formula (II) or (III) as defined above, wherein p is 0 or 1; R2 and R3 are, independently from each other, hydrogen, C1-C4 alkyl optionally substituted by one or more fluorine atoms, or C1-C4 alkoxy; R4 is C1-C4 alkyl or C1-C3 haloalkyl; X1 and X2 are halogen atoms or pharmaceutically acceptable salts thereof; provided that at least one of R5, R6 and R7 is alkyl; are useful as antitumor agents.

    摘要翻译： 作为式（I）的苯并杂环类霉素衍生物的化合物，其中n为2,3或4; A是选自O和S的杂原子，或是基团NR，其中R是氢或C 1 -C 4烷基; B是CH或N; R1是氢或C1-C4烷基; G选自（a，b，c，d，e，f，g，h，i，j）和-C = N; 其中R 5，R 6，R 7，R 8，R 9，R 10，R 11和R 12彼此独立地为氢或C 1 -C 4烷基; T是如上定义的式（II）或（III）的基团，其中p是0或1; R2和R3彼此独立地为氢，任选被一个或多个氟原子取代的C 1 -C 4烷基或C 1 -C 4烷氧基; R4是C1-C4烷基或C1-C3卤代烷基; X1和X2是卤素原子或其药学上可接受的盐; 条件是R 5，R 6和R 7中的至少一个是烷基; 作为抗肿瘤剂有用。

    Allosteric modulators of the A1 adenosine receptor
    10.
    发明授权
    Allosteric modulators of the A1 adenosine receptor 失效
    A1腺苷受体的变构调节剂

    公开(公告)号：US07855209B2

    公开(公告)日：2010-12-21

    申请号：US11938465

    申请日：2007-11-12

    申请人： Pier Giovanni Baraldi ,  Allan R. Moorman ,  Romeo Romagnoli

    发明人： Pier Giovanni Baraldi ,  Allan R. Moorman ,  Romeo Romagnoli

    IPC分类号： A61K31/497 ,  C07D403/06

    CPC分类号： C07D333/36 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D487/08 ,  C07D487/10 ,  C07D491/10

    摘要： The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and Q have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric modulators of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain; cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke; neurological disease or injury; sleep disorder; epilepsy; and depression.

    摘要翻译： 本发明提供式（I）化合物，其中R 1，R 2，R 3，R 4和Q具有本说明书中定义的含义。 式（I）化合物是A1腺苷受体的变构调节剂，因此可用于治疗由A1腺苷受体介导的病症。 因此，式（I）化合物可用于治疗疼痛，特别是慢性疼痛如神经性疼痛; 心脏疾病或障碍，例如心脏性心律失常，例如过氧化物室上性心动过速，心绞痛，心肌梗死和中风; 神经系统疾病或损伤; 睡眠障碍; 癫痫; 和抑郁症。