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    Allosteric adenosine receptor modulators
    13.
    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

    Applicant: Pier Giovanni Baraldi

    Inventor： Pier Giovanni Baraldi

    IPC: A61K31519

    CPC classification number: C07D333/36 ,  A61K31/381 ,  A61K31/382 ,  A61K31/4365 ,  A61K31/4436 ,  C07D333/66 ,  C07D333/78 ,  C07D495/04

    Abstract: 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.

    Abstract translation: 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
    14.
    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

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

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

    IPC: A61K3800

    CPC classification number: C07D403/14 ,  C07D405/14 ,  C07D409/14

    Abstract: 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.

    Abstract translation: 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。

    O-substituted-dibenzyl urea-derivatives as TRPV1 receptor antagonists
    17.
    发明授权
    O-substituted-dibenzyl urea-derivatives as TRPV1 receptor antagonists 有权
    O-取代二苄基脲衍生物作为TRPV1受体拮抗剂

    公开(公告)号：US07750049B2

    公开(公告)日：2010-07-06

    申请号：US12519753

    申请日：2007-12-06

    Applicant: Pier Giovanni Baraldi ,  Pier Andrea Borea ,  Pierangelo Geppetti ,  Francesca Fruttarolo ,  Maria Giovanna Pavani ,  Marcello Trevisani

    Inventor： Pier Giovanni Baraldi ,  Pier Andrea Borea ,  Pierangelo Geppetti ,  Francesca Fruttarolo ,  Maria Giovanna Pavani ,  Marcello Trevisani

    IPC: A61K31/535 ,  A61K31/497 ,  A61K31/44 ,  A61K31/335 ,  A61K31/195 ,  A61K31/17

    CPC classification number: C07C335/12 ,  C07C275/24

    Abstract: The invention relates to compounds of formula (I) in which R is selected from halogen, alkyl, alkoxy, aryl and heteroaryl; R1 is selected from 2-hydroxyethyl, 2,3-dihydroxypropyl, 3-hydroxypropyl, 2,2-dihydroxyethyl, 3,3-dihydroxypropyl, 1,3-dioxolane-ethyl, 1,3-dioxane-methyl, 1,3-dioxolane-methyl, 1,3-dioxane-ethyl, 3-fluoro-2-hydroxypropyl, 3-carboxy-2-hydroxy-propyl, 3-chloro-2-hydroxypropyl, 2-hydroxypropyl, 2-hydroxy-propen-2-yl, morpholinoethyl, piperazinoethyl, hydroxymethyl, benzyl, 4-(hydroxymethyl)benzyl, 4-chlorobenzyl, 4-fluorobenzyl, and 4-hydroxybenzyl. R2 is te/t-butyl or trifluoromethyl; R3 is independently selected from hydrogen, carboxy, cyano, alkyl or hydroxyalkyl, The compounds of formula (I) can be used for the preparation of pharmaceutical compositions for the therapy of inflammatory states, such as chronic neuropathic pain, over-active bladder syndrome, tumor pain, hemorrhoids, inflammatory hyperalgesia, post-intervention pain, dental extraction, airway and gastro-intestinal diseases.

    Abstract translation: 本发明涉及式（I）化合物，其中R选自卤素，烷基，烷氧基，芳基和杂芳基; R1选自2-羟基乙基，2,3-二羟丙基，3-羟丙基，2,2-二羟乙基，3,3-二羟基丙基，1,3-二氧戊环 - 乙基，1,3-二恶烷 - 甲基， 二氧杂环戊烷 - 甲基，1,3-二恶烷 - 乙基，3-氟-2-羟丙基，3-羧基-2-羟基丙基，3-氯-2-羟丙基，2-羟丙基，2-羟基 - 丙烯-2-酮， 吡啶基乙基，羟甲基，苄基，4-（羟甲基）苄基，4-氯苄基，4-氟苄基和4-羟基苄基。 R2是叔丁基或三氟甲基; R 3独立地选自氢，羧基，氰基，烷基或羟烷基。式（I）化合物可用于制备用于治疗炎性状态的药物组合物，例如慢性神经性疼痛，过度膀胱综合征， 肿瘤疼痛，痔疮，炎症痛觉过敏，干预后疼痛，牙齿拔除，气道和胃肠道疾病。

    ALLOSTERIC ENHANCERS OF THE A1 ADENOSINE RECEPTOR
    18.
    发明申请
    ALLOSTERIC ENHANCERS OF THE A1 ADENOSINE RECEPTOR 审中-公开
    A1腺苷受体的独立增强剂

    公开(公告)号：US20090281145A1

    公开(公告)日：2009-11-12

    申请号：US12437344

    申请日：2009-05-07

    Applicant: Pier Giovanni Baraldi ,  Allan R. Moorman ,  Romeo Romagnoli

    Inventor： Pier Giovanni Baraldi ,  Allan R. Moorman ,  Romeo Romagnoli

    IPC: A61K31/4436 ,  C07D333/36 ,  A61K31/381 ,  C07D409/04 ,  A61P25/00

    CPC classification number: C07D333/36 ,  C07D409/04

    Abstract: 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.

    Abstract translation: 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。

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