公开(公告)号：US07960365B2

公开(公告)日：2011-06-14

申请号：US11641524

申请日：2006-12-19

申请人： Niall Morton Hamilton ,  Simon James Anthony Grove ,  Michael John Kiczun ,  John Richard Morphy ,  Brad Sherborne ,  Peter Thomas Albert Littlewood ,  Angus Richard Brown ,  Celia Kingsbury ,  Michael Ohhlmeyer ,  Koc-Kan Ho ,  Steven G. Kultgen

发明人： Niall Morton Hamilton ,  Simon James Anthony Grove ,  Michael John Kiczun ,  John Richard Morphy ,  Brad Sherborne ,  Peter Thomas Albert Littlewood ,  Angus Richard Brown ,  Celia Kingsbury ,  Michael Ohhlmeyer ,  Koc-Kan Ho ,  Steven G. Kultgen

IPC分类号： C07D401/00 ,  A01N57/00

CPC分类号： C07C311/17 ,  C07C311/29 ,  C07D213/61 ,  C07D261/10 ,  C07D307/64 ,  C07D333/34 ,  C07D401/12

摘要： The invention provides for compounds having the structure according to the formula I wherein: X is a carbon or nitrogen atom; Ar is phenyl or heteroaromatic ring; R1 is hydrogen, halogen, CN or (1C-4C)alkyl; R2 is hydrogen, halogen or optionally fluorinated (1C-3C)alkoxy; R3 and R5 are independently hydrogen, optionally halogenated (1C-4C)alkyl, optionally halogenated (1C-4C)alkoxy, optionally halogenated aryl(1C-4C)alkoxy, optionally halogenated (1C-4C)alkenyl or hydroxylmethyl; R4 is hydrogen, halogen, optionally halogenated (1C-4C)alkoxy or optionally halogenated aryl(1C-4C)alkoxy; R6 is hydrogen, benzyl, optionally substituted with one or more halogens or (1C-4C)alkyl, or R6 is optionally halogenated (1C-4C)alkyl; each R7 independently is hydrogen, halogen, optionally halogenated (1C-4C)alkyl or optionally halogenated (1C-4C)alkoxy and pharmaceutically suitable acid addition salts thereof for use as glucocorticoid receptor modulators, in particular for treatment of central nervous system disorders.

摘要翻译： 本发明提供具有式I结构的化合物，其中：X是碳原子或氮原子; Ar是苯基或杂芳环; R1是氢，卤素，CN或（1C-4C）烷基; R2是氢，卤素或任选氟化的（1C-3C）烷氧基; 任选卤代（1C-4C）烷氧基，任选卤代芳基（1C-4C）烷氧基，任选卤代（1C-4C）烯基或羟甲基; R4是氢，卤素，任选卤代（1C-4C）烷氧基或任选的卤代芳基（1C-4C）烷氧基; R6是氢，苄基，任选被一个或多个卤素或（1C-4C）烷基取代，或R6任选被卤代（1C-4C）烷基取代; 每个R 7独立地是氢，卤素，任选卤代（1C-4C）烷基或任选卤代（1C-4C）烷氧基及其药学上合适的酸加成盐，用作糖皮质激素受体调节剂，特别是用于治疗中枢神经系统疾病。

公开(公告)号：US07700638B2

公开(公告)日：2010-04-20

申请号：US10575380

申请日：2004-10-20

申请人： Niall Morton Hamilton ,  Susan Elizabeth Napier ,  Morag Ann MacCall Easson ,  Andrew John Cooke ,  Lene Teuber ,  Naheed Mirza ,  Frank Wätjen

发明人： Niall Morton Hamilton ,  Susan Elizabeth Napier ,  Morag Ann MacCall Easson ,  Andrew John Cooke ,  Lene Teuber ,  Naheed Mirza ,  Frank Wätjen

IPC分类号： A61K31/4184 ,  C07D235/04

CPC分类号： A61K31/4184 ,  C07D235/06 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D403/06 ,  C07D403/12 ,  C07D405/04

摘要： This invention relates to novel 1,5,7-trisubstituted benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith.The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex.

摘要翻译： 本发明涉及新的1,5,7-三取代苯并咪唑衍生物，含有这些化合物的药物组合物及其处理方法。 本发明的化合物可用于治疗对调节GABA A受体复合物有反应的中枢神经系统疾病和病症。

公开(公告)号：US07141560B2

公开(公告)日：2006-11-28

申请号：US10466805

申请日：2002-01-17

申请人： Niall Morton Hamilton ,  David Jonathan Bennett

发明人： Niall Morton Hamilton ,  David Jonathan Bennett

IPC分类号： A61K31/221 ,  A61K31/553 ,  A61K31/54 ,  C07C267/10 ,  C07C207/06

CPC分类号： C07D295/185 ,  C07C229/22 ,  C07C229/24 ,  C07D211/70 ,  C07D225/02 ,  C07D267/10 ,  C07D295/15

摘要： The present invention relates to alanine 2,6-dialkoxyphenyl ester derivatives having the general formula I The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these alanine 2,6-dialkoxyphenyl ester derivatives as hypnotics for the induction and maintenance of general anaesthesia.

摘要翻译： 本发明涉及具有通式I的丙氨酸2,6-二烷氧基苯基酯衍生物。本发明还涉及包含所述衍生物的药物组合物，以及这些丙氨酸2,6-二烷氧基苯基酯衍生物作为诱导和维持催眠剂的用途 的全身麻醉。

公开(公告)号：US06451854B1

公开(公告)日：2002-09-17

申请号：US09744004

申请日：2001-01-18

申请人： Niall Morton Hamilton

发明人： Niall Morton Hamilton

IPC分类号： A61K31325

CPC分类号： C07C229/12 ,  C07C229/16

摘要： The present invention relates to &agr;-amino acid phenyl ester derivatives having general formula (I) wherein R1 is (C1-3)alkyloxy; R2 is (C1-3)alkyl, (C1-3)alkyloxy or (C2-3)alkenyl; R3 is hydrogen, (C1-3)alkyl, (C1-3)alkyloxy or (C2-3)alkenyl; R4 is (C1-6)alkyl; R5 and R6 are independently (C1-6)alkyl, (C2-6)alkenyl, (C2-6)alkynyl or aralkyl, each of which may be optionally substituted with (C1-3)alkyloxy, (C1-3)alkyloxycarbonyl, cyano or NR7R8; R7 and R8 are independently (C1-6)alkyl; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these &agr;-amino acid phenyl ester derivatives as hypnotics for the induction and maintenance of general anaesthesia.

摘要翻译： 本发明涉及具有通式（I）的α-氨基酸苯酯衍生物，其中R 1为（C 1-3）烷氧基; R2是（C1-3）烷基，（C1-3）烷氧基或（C2-3）烯基; R3是氢，（C1-3）烷基，（C1-3）烷氧基或（C2-3）烯基; R4是（C1-6）烷基; R 5和R 6独立地为（C 1-6）烷基，（C 2-6）烯基，（C 2-6）炔基或芳烷基，它们各自可以被（C 1-3）烷氧基，（C 1-3）烷氧基羰基， 氰基或NR7R8; R 7和R 8独立地为（C 1-6）烷基; 或其药学上可接受的盐。 本发明还涉及包含所述衍生物的药物组合物以及这些α-氨基酸苯酯衍生物作催眠剂用于全身麻醉诱导和维持的用途。