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21. 发明授权

US07919510B2 Substituted benzimidazole compounds with dual NOS inhibitory activity and mu opioid agonist activity 失效
标题翻译：具有双重NOS抑制活性和μ阿片样物质激动剂活性的取代的苯并咪唑化合物
公开(公告)号：US07919510B2
公开(公告)日：2011-04-05
申请号：US11436393
申请日：2006-05-18
申请人： Paul Renton , Shawn Maddaford , Suman Rakhit , John Andrews
发明人： Paul Renton , Shawn Maddaford , Suman Rakhit , John Andrews
IPC分类号： A01N43/40
CPC分类号： C07D409/12 , C07D235/12 , C07D405/12
摘要： The present invention relates to benzimidazole compounds having dual nitric oxide synthase (NOS) inhibitory activity and agonist activity at the mu-opioid receptor, to pharmaceutical and diagnostic compositions containing them, and to their medical use, particularly as compounds for the treatment or prevention of chronic pain, acute pain, migraine, and neuropathic pain.
摘要翻译：本发明涉及具有双重一氧化氮合酶（NOS）抑制活性和在μ-阿片受体上的激动剂活性的苯并咪唑化合物，含有它们的药物和诊断组合物及其医疗用途，特别是作为治疗或预防慢性疼痛，急性疼痛，偏头痛和神经性疼痛。

22. 发明授权

US06251893B1 Bicyclic piperidine and piperazine compounds having 5-HT6 receptor affinity 有权
标题翻译：具有5-HT 6受体亲和力的双环哌啶和哌嗪化合物
公开(公告)号：US06251893B1
公开(公告)日：2001-06-26
申请号：US09156495
申请日：1998-09-18
申请人： Shawn Maddaford , Tao Xin , Abdelmalik Slassi , Ashok Tehim , Qi Qiao
发明人： Shawn Maddaford , Tao Xin , Abdelmalik Slassi , Ashok Tehim , Qi Qiao
IPC分类号： A61K3155
CPC分类号： C07D471/04 , C07D487/04
摘要： Described herein are compounds with affinity for the 5-HT6 receptor, which have the general formula: wherein R1, R2, R3 and R4 are independently selected from the group consisting of H, halo, OH, C1-6alkyl, C1-6alkoxy, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl and others; R5 is selected from the group consisting of SO2Ar, C(O)Ar, Ar and CH2Ar; R6 and R7 are independently selected from the group consisting of H, C1-6alkyl, optionally substituted phenyl and optionally substituted benzyl; ————— represents a single or double bond; n is selected from an integer of from 1-3; X is selected from the group consisting of CR17 and N; Z is selected from the group consisting of C, CH and N, provided that when ————— is a double bond, Z is C and when ————— is a single bond, Z is selected from CH and N; Ar is an optionally substituted aromatic group selected from the group consisting of phenyl, pyridyl, thienyl, furanyl, naphthyl, quinolyl and isoquinolyl; R16 is selected from the group consisting of H, C1-6alkyl and benzyl. Also described is the use of these compounds as pharmaceuticals to treat indications where inhibition of the 5-HT6 receptor is implicated, such as schizophrenia.
摘要翻译：本文描述的是对5-HT 6受体具有亲和力的化合物，其具有以下通式：其中R 1，R 2，R 3和R 4独立地选自H，卤素，OH，C 1-6烷基，C 1-6烷氧基，C 2 C 1-6烷基，C 2-6炔基，C 3-7环烷基等; R 5选自SO 2 Ar，C（O）Ar，Ar和CH 2 Ar; R 6和R 7独立地选自H，C 1-6烷基，任选取代的苯基和任选取代的苄基; -----表示单键或双键; n选自1-3的整数; X选自CR 17和N; Z选自由C，CH和N组成，条件是当-----是双键时，Z是C，当-----是单键时，Z选自CH和N; Ar是任选取代的芳族基团，其选自苯基，吡啶基，噻吩基，呋喃基，萘基，喹啉基和异喹啉基; R16选自H，C1-6烷基 1和苄基。还描述了这些化合物作为药物用于治疗其中涉及5-HT 6受体的抑制的指征的用途，例如精神分裂症。

23. 发明授权

US06716837B1 Heterocyclic compounds for the treatment of migraine 失效
标题翻译：用于治疗偏头痛的杂环化合物
公开(公告)号：US06716837B1
公开(公告)日：2004-04-06
申请号：US09709579
申请日：2000-11-13
申请人： Louise Edwards , Methvin Isaac , Shawn Maddaford , Abdelmalik Slassi , Tao Xin
发明人： Louise Edwards , Methvin Isaac , Shawn Maddaford , Abdelmalik Slassi , Tao Xin
IPC分类号： C07D40112
CPC分类号： C07F7/0814 , C07D209/08 , C07D231/56 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D417/04 , C07D417/14 , C07D471/04
摘要： Described herein are compounds useful in the treatment of migraine, which have the general formula: wherein: W is a CH group or a N atom; Z is N or C—R4; B and D are selected independently from CH and N, with the proviso that at least one of B and D is CH and with the further proviso that one of B and D can represent N only when W and Z are both other than N; A is a group of Formula II, III or IV, such that group A contains at least 1 N atom; NR7 is either —NH— or —N═; is a single or double bond; X is a N atom, a CH group or a C(OH) group when is a single bond; or, when is a double bond, a C atom; Y is an NH, N-alkyl, N-benzyl or CH2 group; U and V each represent a N atom or a CH group, with the proviso that both cannot be N; a and b are, independently, 0 or 1; c is an integer from 0 to 3; d is an integer from 1 to 3; e is an integer from 1 to 2; f is an integer from 0 to 3; g is an integer from 3 to 6 and h is an integer from 2 to 3; such that the sum of c and d is at least 2 and the sum of e and f is at least 2; and salts and solvates thereof.
摘要翻译：本文描述了可用于治疗偏头痛的化合物，其具有以下通式：其中：W是CH基团或N原子; Z是N或C-R4; B和D独立地选自CH和N，条件是B和D中的至少一个是CH，进一步的条件是仅当W和Z都不是N时，B和D中的一个可以表示N; A是式II，III或IV的基团，使得A组含有至少1个N原子; NR 7是-NH-或-N =; 是单键或双键; 当是单键; 或者，当是双键时，一个C原子; Y是NH，N-烷基，N-苄基或CH2基团; U和V各自表示N原子或CH基团，条件是两者不能为N; a和b独立地为0或1; c是0至3的整数; d为1〜3的整数; e为1〜2的整数; f为0〜3的整数; g为3〜6的整数，h为2〜3的整数，使得c和d的和为至少2，e和f的和为至少2; 及其盐和溶剂合物。

24. 发明授权

US06667336B2 GlyT-1 inhibitors 失效
标题翻译： GlyT-1抑制剂
公开(公告)号：US06667336B2
公开(公告)日：2003-12-23
申请号：US10077579
申请日：2002-02-15
申请人： Zhaoqing Wang , William Delaney , Ashok Tehim , Shawn Maddaford , Ian Egle , Richard Schumacher , Allen T. Hopper
发明人： Zhaoqing Wang , William Delaney , Ashok Tehim , Shawn Maddaford , Ian Egle , Richard Schumacher , Allen T. Hopper
IPC分类号： A61K3138
CPC分类号： C07D409/10 , C07D333/20
摘要： The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了治疗神经和神经精神障碍的药物，其包含下式化合物或其药学上可接受的盐。

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