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    INHIBITORS OF GAP JUNCTION COMMUNICATION
    4.
    发明申请
    INHIBITORS OF GAP JUNCTION COMMUNICATION 审中-公开
    间隙连通通讯抑制剂

    公开(公告)号：WO9926584A3

    公开(公告)日：1999-07-15

    申请号：PCT/US9824913

    申请日：1998-11-24

    Applicant: SCRIPPS RESEARCH INST ,  BOGER DALE L ,  GILULA NORTON B ,  LERNER RICHARD A ,  CRAVATT BENJAMIN F

    Inventor： BOGER DALE L ,  GILULA NORTON B ,  LERNER RICHARD A ,  CRAVATT BENJAMIN F

    IPC: C07D295/18 ,  A61K31/16 ,  A61K31/201 ,  A61K31/231 ,  A61K31/27 ,  A61K31/40 ,  C07C47/21 ,  C07C49/227 ,  C07C57/12 ,  C07C69/58 ,  C07C233/09 ,  C07C233/10 ,  C07C233/11 ,  C07C233/20 ,  C07C233/49 ,  C07C235/06 ,  C07C235/28 ,  C07C235/76 ,  C07C237/22 ,  C07C243/30 ,  C07C245/14 ,  C07C259/06 ,  C07C271/10 ,  C07C275/20 ,  C07C323/60 ,  C07C327/32 ,  C07D207/00 ,  A01N43/36 ,  C07C59/00 ,  C07C233/00 ,  C07D295/00

    CPC classification number: C07C233/09

    Abstract: Oleamide is an endogenous fatty acid primary amide that possesses sleep-inducing properties in animals and has been shown to effect seratonergic systems and block gap junction communication in a structurally specific manner. Certain agents can serve both as an oleamide agonist and as an inhibitor of fatty acid amide hydrolase. Fatty acid amide hydrolase is responsible for the rapid inactivation of oleamide in vivo. The structural features of oleamide required for inhibition of gap junction-mediated chemical and electrical transmission in rat glial cells are defined. Effective inhibitors fall into two classes of fatty acid primary amides of which oleamide and arachidonamide are the prototypical members. Of these two, oleamide constitutes the most effective and its structural requirements for inhibition of the gap junction are well defined. It requires a chain length of 16-24 carbons of which 16-18 carbons appears optimal, a polarized terminal carbonyl group capable of accepting but not necessarily donating a hydrogen bond, a DELTA 9 cis double bond, and a hydrophobic methyl terminus. Within these constraints, a range of modifications are possible, many of which may with enhanced in vivo properties.

    Abstract translation: 油酰胺是一种内源性脂肪酸伯酰胺，在动物中具有诱导睡眠的特性，并且已被证明能以结构特异性的方式影响seratonergic系统并阻断间隙连接通讯。 某些药剂既可以用作油酰胺激动剂又可以用作脂肪酸酰胺水解酶的抑制剂。 脂肪酸酰胺水解酶负责体内油酸酰胺的快速失活。 定义了抑制大鼠神经胶质细胞中间隙连接介导的化学和电传递所需的油酰胺的结构特征。 有效的抑制剂分为两类脂肪酸伯酰胺，其中油酰胺和花生四烯酰胺是原型成员。 在这两个中，油酰胺构成最有效的并且其对于间隙连接的抑制的结构要求已被很好地定义。 它需要16-24个碳原子的链长，其中16-18个碳原子看起来最适合，极性端羰基能够接受但不一定提供氢键，DELTA 9顺式双键和疏水甲基末端。 在这些限制范围内，可能有一系列修改，其中许多可能具有增强的体内性质。

    METHOD FOR PRODUCING 1-SUBSTITUTED 5-HYDROXYPYRAZOLES
    6.
    发明申请
    METHOD FOR PRODUCING 1-SUBSTITUTED 5-HYDROXYPYRAZOLES 审中-公开
    用于生产1-取代-5-羟基吡

    公开(公告)号：WO00027821A1

    公开(公告)日：2000-05-18

    申请号：PCT/EP1999/008275

    申请日：1999-10-30

    IPC: C07B61/00 ,  C07C243/30 ,  C07D231/20 ,  C07D231/18 ,  C07C241/04

    CPC classification number: C07C243/30 ,  C07D231/20

    Abstract: The invention relates to a method for producing substituted hydroxypyrazoles and new intermediate products. It relates in particular to a method for producing compounds of formula (I) in which R is hydrogen, an aliphatic group with between 1 and 8 carbon atoms, C1-C6-alkoxycarbonyl, C1-C6-alkyl thiocarbonyl or a cyclic ring system with between 3 and 14 ring atoms; R is hydrogen, an aliphatic group with between 1 and 8 carbon atoms; or R and R together with the carbon atom to which they are bound are a cyclic or bicyclic ring system with between 3 and 14 ring atoms. Said method comprises the production, as starting or intermediate products, of compounds of formula (II) in which R and R are readily cleavable groups and R and R have the meanings given above. Said compounds are cyclized under suitable reaction conditions to yield compounds of formula (I).

    Abstract translation: 本发明涉及一种制备取代的羟基吡，以及新的中间体的方法。 本发明涉及一种用于具有1-8个碳原子，C1-C6烷氧基羰基，C1-C6-烷硫基羰基或环状环系统中的脂肪族基团的式（I）中R <1>是氢，的化合物的制备 具有3-14个环原子，且R <2>为氢，具有1-8个碳原子的脂族基团，或R <1>和R <2>一起的碳原子它们所连接形成环状或双环环系 3-14个环原子，其包括，作为起始原料或中间体，式I化合物的制备（II），<3>和R <4>容易地移除基团，其中R，和R <1>和R <2>中，上述 如所定义的，其合适的反应条件下，得到式（I）的化合物可以环化。

    INHIBITORS OF GAP JUNCTION COMMUNICATION
    7.
    发明申请
    INHIBITORS OF GAP JUNCTION COMMUNICATION 审中-公开
    GAP连接通信的抑制剂

    公开(公告)号：WO99026584A2

    公开(公告)日：1999-06-03

    申请号：PCT/US1998/024913

    申请日：1998-11-24

    IPC: C07D295/18 ,  A61K31/16 ,  A61K31/201 ,  A61K31/231 ,  A61K31/27 ,  A61K31/40 ,  C07C47/21 ,  C07C49/227 ,  C07C57/12 ,  C07C69/58 ,  C07C233/09 ,  C07C233/10 ,  C07C233/11 ,  C07C233/20 ,  C07C233/49 ,  C07C235/06 ,  C07C235/28 ,  C07C235/76 ,  C07C237/22 ,  C07C243/30 ,  C07C245/14 ,  C07C259/06 ,  C07C271/10 ,  C07C275/20 ,  C07C323/60 ,  C07C327/32 ,  C07D207/00 ,  A61K

    CPC classification number: C07C233/09

    Abstract: Oleamide is an endogenous fatty acid primary amide that possesses sleep-inducing properties in animals and has been shown to effect seratonergic systems and block gap junction communication in a structurally specific manner. Certain agents can serve both as an oleamide agonist and as an inhibitor of fatty acid amide hydrolase. Fatty acid amide hydrolase is responsible for the rapid inactivation of oleamide in vivo. The structural features of oleamide required for inhibition of gap junction-mediated chemical and electrical transmission in rat glial cells are defined. Effective inhibitors fall into two classes of fatty acid primary amides of which oleamide and arachidonamide are the prototypical members. Of these two, oleamide constitutes the most effective and its structural requirements for inhibition of the gap junction are well defined. It requires a chain length of 16-24 carbons of which 16-18 carbons appears optimal, a polarized terminal carbonyl group capable of accepting but not necessarily donating a hydrogen bond, a DELTA 9 cis double bond, and a hydrophobic methyl terminus. Within these constraints, a range of modifications are possible, many of which may with enhanced in vivo properties.

    Abstract translation: 油酰胺是在动物中具有睡眠诱导性质的内源性脂肪酸伯酰胺，并且已经显示出以结构特异性方式影响血清素能系统和阻断间隙连接通信。 某些试剂可用作油酰胺激动剂和作为脂肪酸酰胺水解酶的抑制剂。 脂肪酸酰胺水解酶负责体内油酰胺的快速失活。 定义了抑制大鼠神经胶质细胞中间隙连接介导的化学和电传递所需的油酰胺的结构特征。 有效的抑制剂分为两类脂肪酸伯酰胺，其中油酰胺和花生四烯酰胺是原型成员。 在这两个中，油酰胺是最有效的，其对间隙连接的抑制的结构要求是明确的。 它需要16-24个碳原子的链长，其中16-18个碳是最佳的，可以接受但不一定要赋予氢键的极化末端羰基，DELTA 9顺式双键和疏水性甲基末端。 在这些约束条件下，一系列修改是可能的，其中许多可能具有增强的体内特性。

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