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1. 发明授权

US5990133A Indole derivatives as 5-HT receptor antagonist 失效
标题翻译：吲哚衍生物作为5-HT受体拮抗剂
公开(公告)号：US5990133A
公开(公告)日：1999-11-23
申请号：US875506
申请日：1997-10-16
申请人： Laramie Mary Gaster , Paul Adrian Wyman , Keith Raymond Mulholland , David Thomas Davies , David Malcolm Duckworth , Ian Thomson Forbes , Graham Elgin Jones
发明人： Laramie Mary Gaster , Paul Adrian Wyman , Keith Raymond Mulholland , David Thomas Davies , David Malcolm Duckworth , Ian Thomson Forbes , Graham Elgin Jones
IPC分类号： A61K31/40 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/475 , A61K31/495 , A61K31/50 , A61K31/505 , A61P25/00 , A61P25/30 , A61P43/00 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/14 , C07D401/10 , C07D403/10
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/14
摘要： A compound of formula (I) or a salt thereof: ##STR1## wherein: P.sup.1 is pyridyl;P.sup.2 is phenyl;A is a bond or a chain of 1 to 5 atoms optionally substituted by C.sub.1-6 alkyl;R.sup.1 and R.sup.2 groups are each independently hydrogen, C.sub.1-6 alkyl optionally substituted by NR.sup.12 R.sup.13, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, cyano, halogen, CF.sub.3, NR.sup.12 R.sup.13, CHO, OCF.sub.3, COR.sup.14, CH.sub.2 OR.sup.14 or OR.sup.14 where R.sup.12, R.sup.13 and R.sup.14 are independently hydrogen or C.sub.1-6 alkyl;n and m are independently 0, 1 or 2;R.sup.3 is hydrogen or C.sub.1-6 alkyl;R.sup.4 is a group of formula (i): ##STR2## in which: R.sup.6 and R.sup.7 are independently hydrogen, C.sub.1-6 alkyl optionally substituted by one or more fluorine atoms, C.sub.1-6 alkylthio, C.sub.1-6 alkoxy or halogen.
摘要翻译： PCT No.PCT / EP96 / 00368 Sec。 371日期：1997年10月16日 102（e）1997年10月16日PCT PCT 1996年1月26日PCT公布。公开号WO96 / 23783 日期：1996年8月8日A式（I）化合物或其盐：其中：P1为吡啶基; P2是苯基; A是任选被C 1-6烷基取代的1至5个原子的键或链; R1和R2各自独立地为氢，任选被NR 12 R 13，C 2-6烯基，C 2-6炔基，氰基，卤素，CF 3，NR 12 R 13，CHO，OCF 3，COR 14，CH 2 OR 14或OR 14取代的C 1-6烷基，其中R 12，R 13和R 14独立地为氢或C 1-6烷基; n和m独立地为0,1或2; R3是氢或C1-6烷基; R4是式（ⅰ）的基团：其中：R6和R7独立地是氢，任意被一个或多个氟原子取代的C 1-6烷基，C 1-6烷硫基，C 1-6烷氧基或卤素。

2. 发明授权

US06235758B1 Indole derivatives as 5-HT receptor antagonist 失效
标题翻译：吲哚衍生物作为5-HT受体拮抗剂
公开(公告)号：US06235758B1
公开(公告)日：2001-05-22
申请号：US09359606
申请日：1999-07-23
申请人： Laramie Mary Gaster , Paul Adrian Wyman , Keith Raymond Mulholland , David Thomas Davies , David Malcolm Duckworth , Ian Thomson Forbes , Graham Elgin Jones
发明人： Laramie Mary Gaster , Paul Adrian Wyman , Keith Raymond Mulholland , David Thomas Davies , David Malcolm Duckworth , Ian Thomson Forbes , Graham Elgin Jones
IPC分类号： C07D40104
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/14
摘要： A compound of formula (I) or a salt thereof: wherein: P1 is pyridiyl; P2 is phenyl; A is a bond or a chain of 1 to 5 atoms optionally substituted by C1-6 alkyl; R1 and R2 groups are each independently hydrogen, C1-6alkyl optionally substituted by NR12R13, C2-6alkenyl, C2-6alkynyl, cyano, halogen, CF3, NR12R13, CHO, OCF3, COR14, CH2OR14 or OR14 where R12, R13 and R14 are independently hydrogen or C1-6alkyl; n and m are independently 0, 1 or 2; R3 is hydrogen or C1-6 alkyl; R4 is a group of formula (i): in which: R6 and R7 are independently hydrogen, C1-6 alkyl optionally substituted by one or more fluorine atoms, C1-6alkylthio, C1-6alkoxy or halogen.
摘要翻译：式（I）化合物或其盐：其中：P1为吡啶基; P2为苯基; A为任选被C 1-6烷基取代的1至5个原子的键或链; R 1和R 2基团各自独立地为氢任选被NR 12 R 13，C 2-6烯基，C 2-6炔基，氰基，卤素，CF 3，NR 12 R 13，CHO，OCF 3，COR 14，CH 2 OR 14或OR 14取代的C 1-6烷基，其中R 12，R 13和R 14独立地为氢或C 1-6烷基; n和 m独立地是0,1或2; R 3是氢或C 1-6烷基; R 4是式（ⅰ）的基团：其中：R 6和R 7独立地是氢，被一个或多个氟原子任意取代的C 1-6烷基，C 1-6烷硫基，C 1-6烷氧基或卤素。

3. 发明授权

US06638953B2 Indole derivatives as 5-HT receptor antagonist 失效
公开(公告)号：US06638953B2
公开(公告)日：2003-10-28
申请号：US09767245
申请日：2001-01-22
申请人： Laramie Mary Gaster , Paul Adrian Wyman , Keith Raymond Mulholland , David Thomas Davies , David Malcolm Duckworth , Ian Thomson Forbes , Graham Elgin Jones
发明人： Laramie Mary Gaster , Paul Adrian Wyman , Keith Raymond Mulholland , David Thomas Davies , David Malcolm Duckworth , Ian Thomson Forbes , Graham Elgin Jones
IPC分类号： A61K3144
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/14
摘要： The invention relates to heterocyclic compounds having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders such as anxiety.

4. 发明授权

US5922733A Pyridil carboxamides as 5HT2B/2C receptor antagonists 失效
标题翻译：吡啶甲酰胺作为5HT2B / 2C受体拮抗剂
公开(公告)号：US5922733A
公开(公告)日：1999-07-13
申请号：US765933
申请日：1997-06-30
申请人： Ian Thomson Forbes , Graham Elgin Jones , Francis David King , Peter Ham , David Thomas Davies , Angela Moghe
发明人： Ian Thomson Forbes , Graham Elgin Jones , Francis David King , Peter Ham , David Thomas Davies , Angela Moghe
IPC分类号： A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/47 , A61P25/00 , A61P43/00 , C07D401/12 , C07D405/12 , C07D409/12 , A01N43/42 , C07D401/00
CPC分类号： C07D401/12 , C07D409/12 , Y02E20/16
摘要： Novel heterocyclic compounds having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders are disclosed.
摘要翻译： PCT No.PCT / EP95 / 02637 371日期：1997年6月30日 102（e）日期1997年6月30日PCT提交1995年7月6日PCT公布。公开号WO96 / 02537 日期1996年2月1日公开了具有药理活性的新型杂环化合物，其制备方法，含有它们的组合物及其在治疗CNS紊乱中的用途。

5. 发明授权

US5866586A CNS-active pyridinylurea derivatives 失效
标题翻译： CNS-活性吡啶基脲衍生物
公开(公告)号：US5866586A
公开(公告)日：1999-02-02
申请号：US817580
申请日：1997-04-17
申请人： Ian Thomson Forbes , Graham Elgin Jones
发明人： Ian Thomson Forbes , Graham Elgin Jones
IPC分类号： C07D241/20 , A61K31/44 , A61K31/4406 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/20 , A61P25/26 , A61P25/28 , C07D213/75 , C07D471/04
CPC分类号： C07D213/75 , C07D471/04
摘要： The invention relates to heterocyclic compounds of formula (I) having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders, wherein P represents phenyl, a quinoline or isoquinoline residue, or a 5 -membered or 6 -membered aromatic heterocyclic ring containing up to three heteroatoms selected from nitrogen, oxygen or sulphur; R.sup.3 is a group of formula (i) or (ii).
摘要翻译： PCT No.PCT / EP95 / 03944 Sec。 371日期1997年04月17日 102（e）日期1997年4月17日PCT 1997年10月5日PCT公布。出版物WO96 / 11930 日期1996年04月25日本发明涉及具有药理活性的式（I）的杂环化合物，其制备方法，含有它们的组合物及其在治疗CNS病症中的用途，其中P表示苯基，喹啉或异喹啉残基或含有至多三个选自氮，氧或硫的杂原子的5元素或6元芳族杂环; R3是式（i）或（ii）的基团。

6. 发明授权

US5834494A Pyridylcarbamoyl Indolines 失效
标题翻译：吡啶基氨基甲酰基吲哚啉
公开(公告)号：US5834494A
公开(公告)日：1998-11-10
申请号：US717957
申请日：1996-09-23
申请人： Peter Ham , Graham Elgin Jones , Ian Thomson Forbes
发明人： Peter Ham , Graham Elgin Jones , Ian Thomson Forbes
IPC分类号： A61K31/42 , A61K31/44 , A61K31/4427 , A61K31/475 , A61P1/14 , A61P25/00 , A61P25/26 , A61P25/28 , A61P43/00 , C07D401/12 , C07D413/12
CPC分类号： C07D401/12 , C07D413/12
摘要： Compounds of formula (I), processes for their preparation and their use in medicine are disclosed: ##STR1## wherein: P represents phenyl, a quinoline or isoquinoline residue, or a 5-membered or 6-membered aromatic heterocyclic ring containing up to three heteroatoms selected from nitrogen, oxygen or sulphur; R.sup.1 is hydrogen, C.sub.1-6 alkyl, halogen, CF.sub.3, NR.sup.7 R.sup.8 or OR.sup.9 where R.sup.7, R.sup.8 and R.sup.9 are independently hydrogen, C.sub.1-6 alkyl or arylC.sub.1-6 alkyl; R.sup.2 is hydrogen or C.sub.1-6 alkyl; R.sup.3 is C.sub.1-6 alkyl; n is 0 to 3; m is 0 to 4; and R.sup.4 groups are independently C.sub.1-6 alkyl optionally substituted by one or more halogen atoms, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkyl-C.sub.1-6 alkyl, C.sub.1-6 alkylthio, C.sub.3-6 cycloalkylthio, C.sub.3-6 cycloalkylC.sub.1 C.sub.6 alkylthio, halogen, nitro, CF.sub.3, OCF.sub.3, SCF.sub.3, SO.sub.2 CF.sub.3, SO.sub.2 F, formyl, C.sub.2-6 alkanoyl, cyano, optionally substituted phenyl or thienyl, NR.sup.7 R.sup.8, CONR.sup.7 R.sup.8, or OR.sup.9 where R.sup.7, R.sup.8 and R.sup.9 are as defined for R.sup.1, CO.sub.2 R.sup.10 where R.sup.10 is hydrogen or C.sub.1-6 alkyl.
摘要翻译：公开了式（I）化合物，其制备方法及其在药物中的用途：吲哚或异喹啉残基或含有至多三个选自氮，氧或硫的杂原子的5元或6元芳族杂环; R 1是氢，C 1-6烷基，卤素，CF 3，NR 7 R 8或OR 9，其中R 7，R 8和R 9独立地是氢，C 1-6烷基或芳基C 1-6烷基; R2是氢或C1-6烷基; R3是C1-6烷基; n为0〜3; m为0〜4; 并且R 4基团独立地是任选地被一个或多个卤素原子取代的C 1-6烷基，C 2-6烯基，C 2-6炔基，C 3-6环烷基，C 3-6环烷基-C 1-6烷基，C 1-6烷硫基， C 3-6环烷基C 1 -C 6烷硫基，卤素，硝基，CF 3，OCF 3，SCF 3，SO 2 CF 3，SO 2 F，甲酰基，C 2-6烷酰基，氰基，任选取代的苯基或噻吩基，NR 7 R 8，CONR 7 R 8或OR 9，其中R 7，如R1所定义，CO 2 R 10，其中R 10是氢或C 1-6烷基。

7. 发明申请

US20100190825A1 BENZIMIDAZOLES WHICH HAVE ACTIVITY AT M1 RECEPTOR AND THEIR USES IN MEDICINE 审中-公开
标题翻译：在M1受体上具有活性的BENZIMIDAZOLES及其在医学中的用途
公开(公告)号：US20100190825A1
公开(公告)日：2010-07-29
申请号：US12293572
申请日：2007-03-20
申请人： David Gwyn Cooper , Ian Thomson Forbes , Vincenzo Garzya , Jian Jin , Yann Louchart , Graham Walker , Paul Adrian Wyman
发明人： David Gwyn Cooper , Ian Thomson Forbes , Vincenzo Garzya , Jian Jin , Yann Louchart , Graham Walker , Paul Adrian Wyman
IPC分类号： A61K31/454 , C07D401/04 , A61P25/18 , A61P25/00
CPC分类号： C07D235/26
摘要： Compounds of formula (I) and salts and solvates are provided: whereinUses of the compounds for the treatment of psychotic disorders and cognitive mpairment, are also disclosed.
摘要翻译：提供式（I）化合物和盐和溶剂合物：其中还公开了用于治疗精神病和认知功能的化合物的用途。

8. 发明申请

US20120041027A1 BENZIMIDAZOLES WHICH HAVE ACTIVITY AT M1 RECEPTOR AND THEIR USES IN MEDICINE 审中-公开
标题翻译：在M1受体上具有活性的BENZIMIDAZOLES及其在医学中的用途
公开(公告)号：US20120041027A1
公开(公告)日：2012-02-16
申请号：US13282604
申请日：2011-10-27
申请人： David Gwyn COOPER , Ian Thomson Forbes , Vincenzo Garzya , Jian Jin , Yann Louchart , Graham Walker , Paul Adrian Wyman
发明人： David Gwyn COOPER , Ian Thomson Forbes , Vincenzo Garzya , Jian Jin , Yann Louchart , Graham Walker , Paul Adrian Wyman
IPC分类号： A61K31/454 , A61P25/18 , A61P25/28 , C07D401/04
CPC分类号： C07D235/26
摘要： Compounds of formula (I) and salts and solvates are provided: wherein Uses of the compounds for therapy, for example in the treatment of psychotic disorders and cognitive impairment, are also disclosed.
摘要翻译：提供式（I）化合物和盐和溶剂合物：其中还公开了化合物用于治疗的用途，例如治疗精神病和认知障碍。

9. 发明申请

US20110207777A1 BENZIMIDAZOLES WHICH HAVE ACTIVITY AT M1 RECEPTOR AND THEIR USES IN MEDICINE 审中-公开
标题翻译：在M1受体上具有活性的BENZIMIDAZOLES及其在医学中的用途
公开(公告)号：US20110207777A1
公开(公告)日：2011-08-25
申请号：US12293588
申请日：2007-03-20
申请人： David Gwyn Cooper , Ian Thomson Forbes , Vincenzo Garzya , Jian Jin , Yann Louchart , Graham Walker , Paul Adrian Wyman
发明人： David Gwyn Cooper , Ian Thomson Forbes , Vincenzo Garzya , Jian Jin , Yann Louchart , Graham Walker , Paul Adrian Wyman
IPC分类号： A61K31/454 , C07D401/04 , C07D211/58 , A61P25/18 , A61P25/30 , A61P25/32 , A61P25/34 , A61P25/36 , A61P25/24 , A61P25/22
CPC分类号： C07D235/26
摘要： Compounds of formula (I), salts and solvates are provided, Uses of the compounds for therapy, for example in the treatment of psychotic disorders and cognitive impairment, are also disclosed.
摘要翻译：提供式（I）化合物，盐和溶剂化物，还公开了用于治疗的化合物的用途，例如治疗精神病和认知障碍。

10. 发明授权

US08426443B2 Compounds which have activity at M1 receptor and their uses in medicine 失效
标题翻译：具有M1受体活性的化合物及其在药物中的用途
公开(公告)号：US08426443B2
公开(公告)日：2013-04-23
申请号：US13592785
申请日：2012-08-23
申请人： David Gwyn Cooper , Ian Thomson Forbes , Vincenzo Garzya , Dale James Johnson , Graeme Irvine Stevenson , Paul Adrian Wyman
发明人： David Gwyn Cooper , Ian Thomson Forbes , Vincenzo Garzya , Dale James Johnson , Graeme Irvine Stevenson , Paul Adrian Wyman
IPC分类号： A61K31/445 , A61K31/425 , A61K31/42
CPC分类号： C07D498/04 , C07D209/34 , C07D215/227
摘要： Compounds of formula (I) or a salt thereof are provided: wherein R4, R5, R6, Q, A, Y and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders, cognitive impairments and Alzheimer's Disease are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
摘要翻译：提供式（I）化合物或其盐：其中R 4，R 5，R 6，Q，A，Y和R如说明书中所定义。公开了化合物作为药物的用途和用于治疗精神病，认知障碍和阿尔茨海默氏病的药物的制备。本发明还公开了包含该化合物的药物组合物。

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