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    Condensed azepines as vasopressin agonists
    1.
    发明授权
    Condensed azepines as vasopressin agonists 有权
    浓缩吖庚因作为血管加压素激动剂

    公开(公告)号：US07560454B2

    公开(公告)日：2009-07-14

    申请号：US11370861

    申请日：2006-03-09

    申请人： Doreen Mary Ashworth ,  Gary Robert William Pitt ,  Peter Hudson ,  Christopher Martyn Yea ,  Richard Jeremy Franklin

    发明人： Doreen Mary Ashworth ,  Gary Robert William Pitt ,  Peter Hudson ,  Christopher Martyn Yea ,  Richard Jeremy Franklin

    IPC分类号： A61P13/00 ,  A61K31/55 ,  C07D403/12 ,  C07D495/04 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

    CPC分类号： C07D403/12 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

    摘要： This invention provides novel compounds according to general formula (1) wherein A is a bicyclic or tricyclic azepine derivative, V1 and V2 are both H, OMe or F, or one of V1 and V2 is Br, Cl, F, OH, OMe, OBn, OPh, O-acyl, N3, NH2, NHBn or NH-acyl and the other is H, or V1 and V2 together are ═O, —O(CH2)pO— or —S(CH2)pS—; W1 is either O or S; X1 and X2 are both H, or together are ═O or ═S; Y is OR5 or NR6R7; R1, R2, R3 and R4 are independently selected from H, lower alkyl, lower alkyloxy, F, Cl and Br; R5 is selected from H and lower alkyl; R6 and R7 are independently selected from H and lower alkyl, or together are —(CH2)n—; n=3, 4, 5, 6; and p is 2 or 3. The compounds are agonists at the vasopressin V2 receptor and are useful as antidiuretics and procoagulants. The invention further comprises pharmaceutical compositions incorporating these vasopressin agonists, which compositions are particularly useful in the treatment of central diabetes insipidus, nocturnal enuresis and nocturia.

    摘要翻译： 本发明提供根据通式（1）的新化合物，其中A为双环或三环吖庚因衍生物，V1和V2均为H，OMe或F，或V1和V2中的一个为Br，Cl，F，OH，OMe， OBn，OPh，O-酰基，N3，NH2，NHBn或NH-酰基，另一个为H，或V 1和V 2一起为-O，-O（CH 2）p O-或-S（CH 2）p -S-; W1是O或S; X1和X2均为H，或一起为-O或-S; Y为OR5或NR6R7; R 1，R 2，R 3和R 4独立地选自H，低级烷基，低级烷氧基，F，Cl和Br; R5选自H和低级烷基; R6和R7独立地选自H和低级烷基，或一起是 - （CH 2）n - ; n = 3,4,5,6; p是2或3.化合物是加压素V2受体的激动剂，可用作抗利尿剂和促凝剂。 本发明还包括掺入这些加压素激动剂的药物组合物，该组合物特别可用于治疗中枢性尿崩症，夜间遗尿和夜尿症。

    Condensed azepines as vasopressin agonists
    2.
    发明授权
    Condensed azepines as vasopressin agonists 有权
    浓缩吖庚因作为血管加压素激动剂

    公开(公告)号：US07074781B2

    公开(公告)日：2006-07-11

    申请号：US10130749

    申请日：2001-01-04

    申请人： Doreen Mary Ashworth ,  Gary Robert William Pitt ,  Peter Hudson ,  Christopher Martyn Yea ,  Richard Jeremy Franklin

    发明人： Doreen Mary Ashworth ,  Gary Robert William Pitt ,  Peter Hudson ,  Christopher Martyn Yea ,  Richard Jeremy Franklin

    IPC分类号： A61P13/00 ,  A61K31/55 ,  C07D403/12 ,  C07D471/04 ,  C07D495/04

    CPC分类号： C07D403/12 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

    摘要： This invention provides novel compounds according to general formula (1) wherein A is a bicyclic or tricyclic azepine derivative, V1 and V2 are both H, OMe or F, or one of V1 and V2 is Br, Cl, F, OH, OMe, OBn, OPh, O-acyl, N3, NH2, NHBn or NH-acyl and the other is H, or V1 and V2 together are ═O, —O(CH2)pO— or —S(CH2)pS—; W1 is either O or S; X1 and X2 are both H, or together are ═O or ═S; Y is OR5 or NR6R7; R1, R2, R3 and R4 are independently selected from H, lower alkyl, lower alkyloxy, F, Cl and Br; R5 is selected from H and lower alkyl; R6 and R7 are independently selected from H and lower alkyl, or together are —(CH2)n—; n=3, 4, 5, 6; and p is 2 or 3. The compounds are agonists at the vasopressin V2 receptor and are useful as antidiuretics and procoagulants. The invention further comprises pharmaceutical compositions incorporating these vasopressin agonists, which compositions are particularly useful in the treatment of central diabetes insipidus, nocturnal enuresis and nocturia.

    摘要翻译： 本发明提供了根据通式（1）的新化合物，其中A是双环或三环吖庚因衍生物，V 1和V 2均为H，OMe或F，或 V 1和V 2之一是Br，Cl，F，OH，OMe，OBn，OPh，O-酰基，N 3， NH 2，NHBn或NH-酰基，另一个是H，或V 1和V 2一起是-O，-O（CH O - 或-S（CH 2）n -S-; -S-（CH 2）n - O 1或O 2是O或S; X 1和X 2均为H或一起为-O或-S; Y是OR 5或NR 6 R 7; R 1，R 2，R 3和R 4独立地选自H，低级烷基，低级烷氧基 ，F，Cl和Br; R 5选自H和低级烷基; R 6和R 7独立地选自H和低级烷基，或者一起是 - （CH 2）n - ; n = 3,4,5,6; 并且p是2或3.化合物是加压素V2受体的激动剂，并且可用作抗利尿剂和促凝剂。 本发明还包括掺入这些加压素激动剂的药物组合物，该组合物特别可用于治疗中枢性尿崩症，夜间遗尿和夜尿症。

    Bicyclic vasopressin agonists
    3.
    发明授权
    Bicyclic vasopressin agonists 失效
    双环血管加压素激动剂

    公开(公告)号：US06664249B1

    公开(公告)日：2003-12-16

    申请号：US10111007

    申请日：2002-06-10

    申请人： Doreen Mary Ashworth ,  Gary Robert William Pitt ,  Peter Hudson ,  Christopher Martyn Yea ,  Richard Jeremy Franklin

    发明人： Doreen Mary Ashworth ,  Gary Robert William Pitt ,  Peter Hudson ,  Christopher Martyn Yea ,  Richard Jeremy Franklin

    IPC分类号： A01N4300

    CPC分类号： C07D223/16 ,  C07D495/04

    摘要： Compounds according to general formula (1), and pharmaceutically acceptable salts thereof, wherein V is a covalent bond or NH, X is selected from CH2, O and N-alkyl, Z is either S or —CH═CH—, R1 and R2 are independently selected from H, F, Cl, Br and alkyl, R3 is selected from OH, O-alkyl and NR4R5, R4 and R5 are each independently H or alkyl, or together are —(CH2)q—, p is 0, 1, 2, 3 or 4, and q is 4 or 5, are new. They are agonists at the asopressin V2 receptor and are useful as antidiuretics and pro-coagulants.

    摘要翻译： 根据通式（1）的化合物及其药学上可接受的盐，其中V是共价键或NH，X选自CH 2，O和N-烷基，Z是S或-CH = CH-，R 1 且R 2独立地选自H，F，Cl，Br和烷基，R 3选自OH，O-烷基和NR 4 R 5，R 4和R 5 各自独立地为H或烷基，或一起为 - （CH 2）q - ，p为0,1,2,3或4，q为4或5，为新的。 它们是加压素V2受体的激动剂，可用作抗利尿剂和促凝血剂。

    Condensed azepines as vasopressin agonists
    4.
    发明申请
    Condensed azepines as vasopressin agonists 审中-公开
    浓缩吖庚因作为血管加压素激动剂

    公开(公告)号：US20080261951A1

    公开(公告)日：2008-10-23

    申请号：US12213651

    申请日：2008-06-23

    申请人： Doreen Mary Ashworth ,  Gary Robert William Pitt ,  Peter Hudson ,  Christopher Martyn Yea ,  Richard Jeremy Franklin

    发明人： Doreen Mary Ashworth ,  Gary Robert William Pitt ,  Peter Hudson ,  Christopher Martyn Yea ,  Richard Jeremy Franklin

    IPC分类号： C07D403/12 ,  C07D495/04 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  A61P13/00

    CPC分类号： C07D403/12 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

    摘要： This invention provides novel compounds according to general formula (1) wherein A is a bicyclic or tricyclic azepine derivative, V1 and V2 are both H, OMe or F, or one of V1 and V2 is Br, Cl, F, OH, OMe, OBn, OPh, O-acyl, N3, NH2, NHBn or NH-acyl and the other is H, or V1 and V2 together are ═O, —O(CH2)pO— or —S(CH2)S—; W1 is either O or S; X1 and X2 are both H, or together are ═O or ═S; Y is OR5 or NR6R7; R1, R2, R3 and R4 are independently selected from H, lower alkyl, lower alkyloxy, F, Cl and Br; R5 is selected from H and lower alkyl; R6 and R7 are independently selected from H and lower alkyl, or together are —(CH2)n—; n=3, 4, 5, 6; and p is 2 or 3. The compounds are agonists at the vasopressin V2 receptor and are useful as antidiuretics and procoagulants. The invention further comprises pharmaceutical compositions incorporating these vasopressin agonists, which compositions are particularly useful in the treatment of central diabetes insipidus, nocturnal enuresis and nocturia.

    摘要翻译： 本发明提供了根据通式（1）的新化合物，其中A是双环或三环吖庚因衍生物，V 1和V 2均为H，OMe或F，或 V 1和V 2之一是Br，Cl，F，OH，OMe，OBn，OPh，O-酰基，N 3， NH 2，NHBn或NH-酰基，另一个是H，或V 1和V 2一起是-O，-O（CH O-或-S（CH 2 CH 2）S - ; O 1或O 2是O或S; X 1和X 2均为H或一起为-O或-S; Y是OR 5或NR 6 R 7; R 1，R 2，R 3和R 4独立地选自H，低级烷基，低级烷氧基 ，F，Cl和Br; R 5选自H和低级烷基; R 6和R 7独立地选自H和低级烷基，或者一起是 - （CH 2）n - ; n = 3,4,5,6; p是2或3.化合物是加压素V2受体的激动剂，可用作抗利尿剂和促凝剂。 本发明还包括掺入这些加压素激动剂的药物组合物，该组合物特别可用于治疗中枢性尿崩症，夜间遗尿和夜尿症。

    Pyridine and pyrimidine derivatives
    6.
    发明授权
    Pyridine and pyrimidine derivatives 失效
    吡啶和嘧啶衍生物

    公开(公告)号：US07323464B2

    公开(公告)日：2008-01-29

    申请号：US10495885

    申请日：2002-11-20

    申请人： Jeremy Martin Davis ,  Barry John Langham ,  Manisha Naik ,  Daniel Christopher Brookings ,  Rachel Jane Cubbon ,  Richard Jeremy Franklin

    发明人： Jeremy Martin Davis ,  Barry John Langham ,  Manisha Naik ,  Daniel Christopher Brookings ,  Rachel Jane Cubbon ,  Richard Jeremy Franklin

    IPC分类号： C07D403/04 ,  A61K31/506

    CPC分类号： C07D401/04 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14

    摘要： Compounds of formula (1) are described in which Ra and Rb is each independently a hydrogen atom or a group Rc, or Ra and Rb together form an oxo (═O) or thio (═S) group; X is a N atom or an optionally substituted CH group: Y is a —O— or —S— atom or —SO— or —SO2— group or an optionally substituted —CH2— or —NH— group with the proviso that when Ra and Rb together form an oxo (═O) or thio (═S) group Y is an optionally substituted —CH2— or —NH-group; L1 is a covalent bond or a linker atom or group; p is zero or the integer 1; Alk1 is an optionally substituted C1-10aliphatic or C1-10heteroaliphatic chain; n is zero the integer 1, 2 or 3 with the proviso that when n is zero Y is an optionally substituted —CH2— group; Ar is an optionally substituted C6-12aromatic or C1-9heteroaromatic group; m is zero or the integer 1, 2 or 3; q is zero or the integer 1 or 2; R1, Rc and Rd are hydrogen atoms or the substituents described in the patent specification; and the salts, solvates, hydrates and N-oxides thereof. The compounds are potent and selective inhibitors of p38 kinase and are useful in the treatment of immune or inflammatory disorders.

    摘要翻译： 描述式（1）的化合物，其中R a和R b各自独立地为氢原子或基团R c，或R （-O）或硫代（-S）基团一起形成一个或多个， X是N原子或任选取代的CH基团：Y是-O-或-S-原子或-SO-或-SO 2 - 基团或任选取代的-CH 2 或-NH-基团，条件是当R a a和R b一起形成氧代（-O）或硫代（-S）基团Y 是任选取代的-CH 2 - 或-NH-基团; L 1是共价键或连接子原子或基团; p为零或整数1; Alk 1是任选取代的C 1-10 1-10脂族或C 1-10 1-10杂脂肪族链; n为整数1,2或3，条件是当n为零时，Y为任选取代的-CH 2 - 基团; Ar是任选取代的C 6-12芳族或C 1-19杂芳族基团; m为零或整数1,2或3; q为零或整数1或2; R 1，R 2和R d是氢原子或专利说明书中所述的取代基; 及其盐，溶剂合物，水合物和N-氧化物。 这些化合物是p38激酶的有效和选择性抑制剂，可用于治疗免疫或炎症性疾病。