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    Midazopyrazinones and imidazotriazinones derivates as gaba-a receptor anxiolytic
    3.
    发明申请
    Midazopyrazinones and imidazotriazinones derivates as gaba-a receptor anxiolytic 失效
    咪唑并吡嗪酮和咪唑并三嗪酮衍生为gaba-a受体抗焦虑药

    公开(公告)号：US20060014744A1

    公开(公告)日：2006-01-19

    申请号：US10533152

    申请日：2003-10-29

    申请人： William Carling ,  Jose Castro Pineiro ,  Simon Goodacre ,  David Hallett ,  Leslie Street

    发明人： William Carling ,  Jose Castro Pineiro ,  Simon Goodacre ,  David Hallett ,  Leslie Street

    IPC分类号： A61K31/53 ,  A61K31/519 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： The present invention discloses a compound of formula I, or a pharmaceutically acceptable salt thereof: (I) wherein —U—V— represents —CH═CH—, or —CH2—CH2—, —N═CH— or —CH═N—; X1 represents hydrogen, halogen, C1-6 alkyl, trifluoromethyl or C1-6 alkoxy; X2 represents hydrogen or halogen; Y represents a chemical bond, an oxygen atom, or a —NH— or —OCH2— linkage; Z represents an optionally substituted aryl or heteroaryl group; R1 represents hydrocarbon, a heterocyclic group, trifluoromethyl, —SO2Ra, —SO2NRaRb, —CORa, —CO2Ra or —CONRaRb; and Ra and Rb independently represent hydrogen, hydrocarbon or a heterocyclic group; pharmaceutical compositions comprising it; its use in methods of treatment; use of it in the manufacture of a medicament for treating and/or preventing anxiety; convulsions or a cognitive disorder; and methods of treatment using it.

    摘要翻译： 本发明公开了式I化合物或其药学上可接受的盐：（I）其中-UV-表示-CH-CH-或-CH 2 -CH 2， -N - ， - CH-或-CH-N-; X 1表示氢，卤素，C 1-6烷基，三氟甲基或C 1-6烷氧基; X 2表示氢或卤素; Y表示化学键，氧原子或-NH-或-OCH 2 - 键; Z表示任选取代的芳基或杂芳基; R 1表示烃，杂环基，三氟甲基，-SO 2 R 2，-SO 2 NR 2， - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - a B ; R a和R b各自独立地表示氢，烃或杂环基; 包含它的药物组合物; 其用于治疗方法; 在制备用于治疗和/或预防焦虑的药物中的用途; 惊厥或认知障碍; 和使用它的治疗方法。

    BICYCLIC AMIDES FOR ENHANCING GLUTAMATERGIC SYNAPTIC RESPONSES
    5.
    发明申请
    BICYCLIC AMIDES FOR ENHANCING GLUTAMATERGIC SYNAPTIC RESPONSES 有权
    用于增强谷氨酸反应性的双酚A

    公开(公告)号：US20130190351A1

    公开(公告)日：2013-07-25

    申请号：US13557681

    申请日：2012-07-25

    申请人： Rudolf Mueller ,  Leslie Street

    发明人： Rudolf Mueller ,  Leslie Street

    IPC分类号： A61K31/46 ,  C07D451/06 ,  C07D451/04 ,  A61K45/06 ,  C07D471/08 ,  A61K31/4245 ,  A61K31/439 ,  C07D451/02 ,  C07D487/08

    CPC分类号： A61K31/46 ,  A61K31/4245 ,  A61K31/439 ,  A61K31/519 ,  A61K31/53 ,  A61K45/06 ,  C07D209/52 ,  C07D451/02 ,  C07D451/04 ,  C07D451/06 ,  C07D453/06 ,  C07D471/08 ,  C07D487/08 ,  C07D491/08

    摘要： This invention relates to bicyclic amide compounds, pharmaceutical compositions and methods for use in the prevention and treatment of a variety of conditions and/or disease states including cerebral insufficiency, through the enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors as defined herein. These brain networks, which are involved in regulation of breathing, and cognitive abilities related to memory impairment, such as is observed in a variety of dementias, in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia, respiratory depression, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, and in other disorders wherein a deficiency in neurotrophic factors is implicated, as well as other disorders as described herein.

    摘要翻译： 本发明涉及双环酰胺化合物，药物组合物和用于预防和治疗各种病症和/或疾病状态（包括脑功能不全）的方法，其通过增强负责基本和高等级的脑网络中的突触中的受体功能 行为如本文所定义。 涉及呼吸调节的这些脑网络，以及与记忆障碍有关的认知能力，例如在各种痴呆中观察到的，在不同脑区域之间的神经元活动不平衡中，如在帕金森病， 精神分裂症，呼吸抑制，睡眠呼吸暂停，注意缺陷多动障碍和情感或情绪障碍，以及涉及神经营养因子缺乏的其它疾病以及本文所述的其它病症。

    Di-substituted amides for enhancing glutamatergic synaptic responses
    6.
    发明授权
    Di-substituted amides for enhancing glutamatergic synaptic responses 有权
    用于增强谷氨酸能突触反应的二取代酰胺

    公开(公告)号：US08404682B2

    公开(公告)日：2013-03-26

    申请号：US13226146

    申请日：2011-09-06

    申请人： Leslie Street ,  Rudolf Mueller ,  Steven Lee

    发明人： Leslie Street ,  Rudolf Mueller ,  Steven Lee

    IPC分类号： A61K31/5377 ,  A61K31/4245 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/433 ,  A61K31/498

    CPC分类号： A61K31/4245 ,  A61K45/06 ,  C07D271/12 ,  C07D285/14 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

    摘要： This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors. These brain networks, which are involved in regulation of breathing, and cognitive abilities related to memory impairment, such as is observed in a variety of dementias, in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia, respiratory depression, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, and in disorders wherein a deficiency in neurotrophic factors is implicated, as well as in disorders of respiration such as overdose of an alcohol, an opiate, an opioid, a barbiturate, an anesthetic, or a nerve toxin, or where the respiratory depression results form a medical condition such as central sleep apnea, stroke-induced central sleep apnea, obstructive sleep apnea, congenital hypoventilation syndrome, obesity hypoventilation syndrome, sudden infant death syndrome, Rett syndrome, spinal cord injury, traumatic brain injury, Cheney-Stokes respiration, Ondines curse, Prader-Willi's syndrome and drowning. In a particular aspect, the invention relates to compounds useful for treatment of such conditions, and methods of using these compounds for such treatment.

    摘要翻译： 本发明涉及用于预防和治疗脑功能不全的化合物，药物组合物和方法，包括在负责基本和高级行为的脑网络中的突触中增强受体功能。 涉及呼吸调节的这些脑网络，以及与记忆障碍有关的认知能力，例如在各种痴呆中观察到的，在不同脑区域之间的神经元活动不平衡中，如在帕金森病， 精神分裂症，呼吸抑制，睡眠呼吸暂停，注意缺陷多动障碍和情感或情绪障碍，以及涉及神经营养因子缺乏的疾病，以及呼吸障碍，例如过量的酒精，阿片剂，阿片样物质， 巴比妥酸盐，麻醉剂或神经毒素，或呼吸抑制结果形成中枢性睡眠呼吸暂停，中风引起的中枢性睡眠呼吸暂停，阻塞性睡眠呼吸暂停，先天性通气不足综合征，肥胖低通气综合征，婴儿猝死综合征 ，Rett综合征，脊髓损伤，创伤性脑损伤，Cheney-Stokes呼吸，Ondines诅咒 ，Prader-Willi综合征和溺水。 在一个特定方面，本发明涉及可用于治疗这些病症的化合物，以及使用这些化合物进行这种治疗的方法。

    Bicyclic amides for enhancing glutamatergic synaptic responses
    8.
    发明授权
    Bicyclic amides for enhancing glutamatergic synaptic responses 有权
    用于增强谷氨酸能突触反应的双环酰胺

    公开(公告)号：US08263591B2

    公开(公告)日：2012-09-11

    申请号：US12733073

    申请日：2008-08-08

    申请人： Rudolf Mueller ,  Leslie Street

    发明人： Rudolf Mueller ,  Leslie Street

    IPC分类号： A61K31/535 ,  C07D498/02 ,  C07D265/00

    CPC分类号： A61K31/46 ,  A61K31/4245 ,  A61K31/439 ,  A61K31/519 ,  A61K31/53 ,  A61K45/06 ,  C07D209/52 ,  C07D451/02 ,  C07D451/04 ,  C07D451/06 ,  C07D453/06 ,  C07D471/08 ,  C07D487/08 ,  C07D491/08

    摘要： This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors. These brain networks, which are involved in regulation of breathing, and cognitive abilities related to memory impairment, such as is observed in a variety of dementias, in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia, respiratory depression, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, and in disorders wherein a deficiency in neurotrophic factors is implicated, as well as in disorders of respiration such as overdose of an alcohol, an opiate, an opioid, a barbiturate, an anesthetic, or a nerve toxin, or where the respiratory depression results form a medical condition such as central sleep apnea, stroke-induced central sleep apnea, obstructive sleep apnea, congenital hypoventilation syndrome, obesity hypoventilation syndrome, sudden infant death syndrome, Rett syndrome, spinal cord injury, traumatic brain injury, Cheney-Stokes respiration, Ondines curse, Prader-Willi's syndrome and drowning, hi a particular aspect, the invention relates to bicyclic amide compounds useful for treatment of such conditions, and methods of using these compounds for such treatment.

    摘要翻译： 本发明涉及用于预防和治疗脑功能不全的化合物，药物组合物和方法，包括在负责基本和高级行为的脑网络中的突触中增强受体功能。 涉及呼吸调节的这些脑网络，以及与记忆障碍有关的认知能力，例如在各种痴呆中观察到的，在不同脑区域之间的神经元活动不平衡中，如在帕金森病， 精神分裂症，呼吸抑制，睡眠呼吸暂停，注意缺陷多动障碍和情感或情绪障碍，以及涉及神经营养因子缺乏的疾病，以及呼吸障碍，例如过量的酒精，阿片剂，阿片样物质， 巴比妥酸盐，麻醉剂或神经毒素，或呼吸抑制结果形成中枢性睡眠呼吸暂停，中风引起的中枢性睡眠呼吸暂停，阻塞性睡眠呼吸暂停，先天性通气不足综合征，肥胖低通气综合征，婴儿猝死综合征 ，Rett综合征，脊髓损伤，创伤性脑损伤，Cheney-Stokes呼吸，Ondines诅咒 ，Prader-Willi综合征和溺水。在一个特定方面，本发明涉及可用于治疗这些病症的双环酰胺化合物，以及使用这些化合物进行这种治疗的方法。

    DI-SUBSTITUTED AMIDES FOR ENHANCING GLUTAMATERGIC SYNAPTIC RESPONSES
    9.
    发明申请
    DI-SUBSTITUTED AMIDES FOR ENHANCING GLUTAMATERGIC SYNAPTIC RESPONSES 有权
    用于增强GLUTAMATERGIC SYNAPTIC RESPONS的DI替代剂

    公开(公告)号：US20120035173A1

    公开(公告)日：2012-02-09

    申请号：US13226146

    申请日：2011-09-06

    申请人： Leslie Street ,  Rudolf Mueller ,  Steven Lee

    发明人： Leslie Street ,  Rudolf Mueller ,  Steven Lee

    IPC分类号： A61K31/4245 ,  C07D413/12 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/433 ,  A61P11/00 ,  A61K31/498 ,  A61K31/5377 ,  A61P25/28 ,  A61P25/16 ,  A61P25/00 ,  C07D271/12 ,  C07D405/12

    CPC分类号： A61K31/4245 ,  A61K45/06 ,  C07D271/12 ,  C07D285/14 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

    摘要： This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors. These brain networks, which are involved in regulation of breathing, and cognitive abilities related to memory impairment, such as is observed in a variety of dementias, in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia, respiratory depression, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, among numerous others. In a particular aspect, the invention relates to compounds useful for treatment of such conditions, and methods of using these compounds for such treatment.

    摘要翻译： 本发明涉及用于预防和治疗脑功能不全的化合物，药物组合物和方法，包括在负责基本和高级行为的脑网络中的突触中增强受体功能。 涉及呼吸调节的这些脑网络，以及与记忆障碍有关的认知能力，例如在各种痴呆中观察到的，在不同脑区域之间的神经元活动不平衡中，如在帕金森病， 精神分裂症，呼吸抑制，睡眠呼吸暂停，注意缺陷多动障碍和情感或情绪障碍等。 在一个特定方面，本发明涉及可用于治疗这些病症的化合物，以及使用这些化合物进行这种治疗的方法。

    Imidazole, triazole and tetrazole derivatives
    10.
    发明授权
    Imidazole, triazole and tetrazole derivatives 失效
    咪唑，三唑和四唑衍生物

    公开(公告)号：US5510362A

    公开(公告)日：1996-04-23

    申请号：US295884

    申请日：1994-09-08

    申请人： Victor G. Matassa ,  Austin J. Reeve ,  Francine Sternfeld ,  Helen Routledge ,  Leslie Street

    发明人： Victor G. Matassa ,  Austin J. Reeve ,  Francine Sternfeld ,  Helen Routledge ,  Leslie Street

    IPC分类号： A61K31/41 ,  A61K31/4178 ,  A61K31/4196 ,  A61P25/04 ,  A61P25/06 ,  C07D403/14 ,  C07D521/00

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D403/14

    摘要： A class of substituted imidazole, triazole and tetrazole derivatives of formula (I), wherein the broken circle represents two non-adjacent double bonds in any position in the five-membered ring; two, three or four of V,W,X,Y and Z represent nitrogen and the remainder represent carbon provided that, when two of V,W,X,Y and Z represent nitrogen and the remainder represent carbon, then the said nitrogen atoms are in non-adjacent positions within the five-membered ring; E represents a bond or a straight or branched alkylene chain containing from 1 to 4 carbon atoms; F represents a group of formula (lI); U represents nitrogen or C--R.sup.2 ; B represents oxygen, sulphur or N--R.sup.3 ; are selective agonists of 5--HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.

    摘要翻译： PCT No.PCT / GB93 / 00474 Sec。 371日期1994年9月8日 102（e）1994年9月8日PCT 1993年3月5日PCT公布。 公开号WO93 / 18029 （I）一类式（I）的取代的咪唑，三唑和四唑衍生物，其中，所述断圆代表在任何位置上的两个不相邻的双键 五元环; V，W，X，Y和Z中的两个，三个或四个表示氮，余数表示碳，条件是当V，W，X，Y和Z中的两个表示氮并且其余表示碳时，则所述氮原子 在五元环内的非相邻位置; E表示含有1至4个碳原子的键或直链或支链亚烷基链; F表示式（I）的基团; U表示氮或C-R2; B代表氧，硫或N-R3; 是5-HT1样受体的选择性激动剂，因此可用于治疗临床状况，特别是偏头痛和相关疾病，其中指出了这些受体的选择性激动剂。