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1. 发明授权

US06486153B1 Phenylindole derivatives as 5-HT2A receptor ligands 失效
标题翻译：苯基吲哚衍生物作为5-HT2A受体配体
公开(公告)号：US06486153B1
公开(公告)日：2002-11-26
申请号：US09508046
申请日：2000-03-03
申请人： Jose Luis Castro Pineiro , Steven Michael Hutchins , Stephen John Lewis , Michael Rowley , Adrian Leonard Smith , Graeme Irvine Stevenson
发明人： Jose Luis Castro Pineiro , Steven Michael Hutchins , Stephen John Lewis , Michael Rowley , Adrian Leonard Smith , Graeme Irvine Stevenson
IPC分类号： C07D20914
CPC分类号： C07D401/06 , C07D209/16 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D491/04
摘要： A class of tryptamine analogues bearing an optionally substituted phenyl nucleus at the 2-position are selective antagonists of the human 5-HT2A receptor and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse neurological conditions, including psychotic disorders such as schizophrenia.
摘要翻译：在2-位上带有任选取代的苯基核的一类色胺类似物是人5-HT 2A受体的选择性拮抗剂，因此可用作药物，特别是用于治疗和/或预防不良神经病症，包括精神病性疾病如精神分裂症。

2. 发明授权

US07049296B2 Gamma-secretase inhibitors 失效
标题翻译： γ-分泌酶抑制剂
公开(公告)号：US07049296B2
公开(公告)日：2006-05-23
申请号：US10204962
申请日：2001-02-28
申请人： Jose Luis Castro Pineiro , Adrian Leonard Smith , Graeme Irvine Stevenson
发明人： Jose Luis Castro Pineiro , Adrian Leonard Smith , Graeme Irvine Stevenson
IPC分类号： A61K38/05 , C07C271/00 , C07K5/06
CPC分类号： C07K5/06034 , A61K38/00 , C07K5/06026 , C07K5/06078
摘要： Urea derivatives of formula I are disclosed: The compounds are inhibitors of γ-secretase, and hence useful in the treatment or prevention of Alzheimer's Disease
摘要翻译：公开了式I的脲衍生物：该化合物是γ-分泌酶的抑制剂，因此可用于治疗或预防阿尔茨海默病

3. 发明授权

US07365196B2 Sulphonamido-substituted bridged bicycloalkyl derivatives 有权
标题翻译：磺酰氨基取代的桥连双环烷基衍生物
公开(公告)号：US07365196B2
公开(公告)日：2008-04-29
申请号：US10239233
申请日：2001-03-15
申请人： Patrice Charles Belanger , Ian James Collins , Joanne Claire Hannam , Timothy Harrison , Stephen John Lewis , Andrew Madin , Edward Giles McIver , Alan John Nadin , Joseph George Neduvelil , Mark Steven Shearman , Adrian Leonard Smith , Timothy Jason Sparey , Graeme Irvine Stevenson , Martin Richard Teall
发明人： Patrice Charles Belanger , Ian James Collins , Joanne Claire Hannam , Timothy Harrison , Stephen John Lewis , Andrew Madin , Edward Giles McIver , Alan John Nadin , Joseph George Neduvelil , Mark Steven Shearman , Adrian Leonard Smith , Timothy Jason Sparey , Graeme Irvine Stevenson , Martin Richard Teall
IPC分类号： C07D413/14 , C07D413/12 , C07D213/71 , C07D213/52 , C07D333/34 , C07D409/14 , C07D409/12 , C07D249/12 , C07D233/84 , C07D207/48 , C07D277/16 , C07D307/64 , A61P25/28
CPC分类号： C07D213/30 , A61K31/18 , A61K31/40 , C07C311/07 , C07C311/09 , C07C311/11 , C07C311/14 , C07C311/20 , C07C311/24 , C07C323/67 , C07C2601/08 , C07C2601/14 , C07C2602/44 , C07C2602/46 , C07C2603/72 , C07C2603/78 , C07D207/36 , C07D211/14 , C07D211/18 , C07D213/71 , C07D213/81 , C07D215/12 , C07D223/32 , C07D231/12 , C07D233/56 , C07D249/08 , C07D271/107 , C07D277/36 , C07D285/14 , C07D285/16 , C07D295/088 , C07D295/135 , C07D295/26 , C07D307/64 , C07D307/81 , C07D319/18 , C07D333/34 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D487/04 , C07D487/08 , C07D491/08 , C07D491/10 , C07D513/10
摘要： A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.
摘要翻译：公开了一类化合物，其包含磺酰氨基取代的桥连双环烷基结构。这些化合物是γ-分泌酶的抑制剂，因此可用于治疗和/或预防阿尔茨海默氏病。

4. 发明申请

US20100010014A1 AMINOPYRIMIDINE COMPOUNDS AND METHODS OF USE 有权
标题翻译：氨基嘧啶化合物和使用方法
公开(公告)号：US20100010014A1
公开(公告)日：2010-01-14
申请号：US12562853
申请日：2009-09-18
申请人： Adrian Leonard Smith , Paul Edward Brennan , Frenel Fils DeMorin , Gang Lin , Nick A. Paras , Daniel Martin Retz , Elizabeth Rainbeau
发明人： Adrian Leonard Smith , Paul Edward Brennan , Frenel Fils DeMorin , Gang Lin , Nick A. Paras , Daniel Martin Retz , Elizabeth Rainbeau
IPC分类号： A61K31/506 , C07D417/04 , C07D417/14 , A61P19/02 , A61P35/00
CPC分类号： C07D417/14 , C07D409/14
摘要： The invention relates to aminopyrimidine compounds useful for treating diseases mediated by polo-like kinase 1 (Plk1). The invention also relates to the therapeutic use of such aminopyrimidine compounds and compositions thereof in treating disease states associated with abnormal cell growth and unwanted cell proliferation.
摘要翻译：本发明涉及用于治疗由polo样激酶1（Plk1）介导的疾病的氨基嘧啶化合物。本发明还涉及这种氨基嘧啶化合物及其组合物在治疗与异常细胞生长和不想要的细胞增殖相关的疾病状态中的治疗用途。

5. 发明授权

US5919947A Traceless solid phase synthesis of indole derivatives 失效
标题翻译：无痕固相合成吲哚衍生物
公开(公告)号：US5919947A
公开(公告)日：1999-07-06
申请号：US145692
申请日：1998-09-02
申请人： Adrian Leonard Smith
发明人： Adrian Leonard Smith
IPC分类号： C07D209/08 , C07D209/12 , C07D209/14
CPC分类号： C07D209/08 , C07D209/12 , C07D209/14
摘要： The present invention relates to a traceless solid phase process for the preparation of an indole derivative, which comprises the following steps:(1) reaction of an optionally substituted 2-iodoaniline derivative via the nitrogen atom of the NH.sub.2 moiety thereof with a dihydropyran-functionalized polymeric resin under conditions effective to form an aminal linkage;(2) reaction of the tetrahydropyran aminal derivative thereby obtained with an acetylene derivative in the presence of a transition metal catalyst under conditions effective to promote indole formation;(3) treatment of the product thereby obtained with acid, whereby the aminal linkage is cleaved and the desired indole derivative is liberated from the resin; and(4) isolation of the desired indole derivative thereby obtained.
摘要翻译：本发明涉及一种用于制备吲哚衍生物的无痕固相法，其包括以下步骤：（1）通过其NH 2部分的氮原子将任选取代的2-碘苯胺衍生物与二氢吡喃官能化的聚合物树脂在有效形成氨基键的条件下; （2）由此得到的四氢吡喃二胺衍生物与乙炔衍生物在过渡金属催化剂存在下在有效促进吲哚形成的条件下反应; （3）用酸处理由此得到的产物，由此使所述的二胺键断裂并从所述树脂中释出所需的吲哚衍生物; 和（4）所得吲哚衍生物的分离。

6. 发明授权

US08440674B2 Substituted pyrimidine compounds as RAF inhibitors and methods of use 失效
标题翻译：取代的嘧啶化合物作为RAF抑制剂和使用方法
公开(公告)号：US08440674B2
公开(公告)日：2013-05-14
申请号：US13163666
申请日：2011-06-17
申请人： Frenel F. De Morin , Jian J. Chen , Elizabeth M. Doherty , Stephen A. Hitchcock , Qi Huang , Joseph L. Kim , Gang Liu , Thomas Nixey , Nick A. Paras , Jeffrey Petkus , Daniel Martin Retz , Adrian Leonard Smith , Jiawang Zhu
发明人： Frenel F. De Morin , Jian J. Chen , Elizabeth M. Doherty , Stephen A. Hitchcock , Qi Huang , Joseph L. Kim , Gang Liu , Thomas Nixey , Nick A. Paras , Jeffrey Petkus , Daniel Martin Retz , Adrian Leonard Smith , Jiawang Zhu
IPC分类号： A01N43/54
CPC分类号： C07D401/14 , C07D239/84 , C07D239/95 , C07D401/04 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04
摘要： The present invention comprises a new class of compounds capable of modulating Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula I wherein R1 is and A1, A2, A3, A4, X, Z, Z′, R1, R2, R3, R4, R5 and R6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
摘要翻译：本发明包括能够调节Raf激酶的新一类化合物，因此可用于治疗Raf激酶介导的疾病，包括黑素瘤，肿瘤和其它癌症相关病症。该化合物具有通式I，其中R1为和A1，A2，A3，A4，X，Z，Z'，R1，R2，R3，R4，R5和R6如本文所定义。本发明还包括药物组合物，用于治疗Raf激酶介导的疾病的方法，以及可用于制备本发明化合物的中间体和方法。

7. 发明授权

US5700809A Pyrrolo-pyridine derivatives 失效
标题翻译：吡咯并吡啶衍生物
公开(公告)号：US5700809A
公开(公告)日：1997-12-23
申请号：US513828
申请日：1995-08-29
申请人： Paul David Leeson , Adrian Leonard Smith , Mark Peter Ridgill , Raymond Baker , Neil Roy Curtis , Janusz Jozef Kulagowski
发明人： Paul David Leeson , Adrian Leonard Smith , Mark Peter Ridgill , Raymond Baker , Neil Roy Curtis , Janusz Jozef Kulagowski
IPC分类号： C07D471/04 , C07D410/14 , A61K31/54 , C07D217/24 , C07D109/14
CPC分类号： C07D471/04
摘要： Compounds of formula I are ligands for dopamine receptor subtypes within the body and are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia. ##STR1## wherein Q is ##STR2##
摘要翻译： PCT No.PCT / GB94 / 00384 Sec。 371日期1995年8月29日 102（e）日期1995年8月29日PCT 1994年2月25日PCT PCT。第WO94 / 20459号公报日期1994年9月15日式I化合物是体内多巴胺受体亚型的配体，因此可用于治疗和/或预防多巴胺系统疾病，特别是精神分裂症。（I）其中Q是（Qa）（Qb）（Qc）

8. 发明授权

US07858785B2 Aminopyrimidine compounds and methods of use 有权
公开(公告)号：US07858785B2
公开(公告)日：2010-12-28
申请号：US12562853
申请日：2009-09-18
申请人： Adrian Leonard Smith , Paul Edward Brennan , Fenel F. Fils , Gang Liu , Nick A. Paras , Daniel Martin Retz , Elizabeth Rainbeau
发明人： Adrian Leonard Smith , Paul Edward Brennan , Fenel F. Fils , Gang Liu , Nick A. Paras , Daniel Martin Retz , Elizabeth Rainbeau
IPC分类号： C07D417/14 , A61K31/506 , A61P19/02 , A61P35/00
CPC分类号： C07D417/14 , C07D409/14
摘要： The invention relates to aminopyrimidine compounds useful for treating diseases mediated by polo-like kinase 1 (Plk1). The invention also relates to the therapeutic use of such aminopyrimidine compounds and compositions thereof in treating disease states associated with abnormal cell growth and unwanted cell proliferation.

9. 发明授权

US07786132B2 Aminopyrimidine compounds and methods of use 有权
标题翻译：氨基嘧啶化合物及其使用方法
公开(公告)号：US07786132B2
公开(公告)日：2010-08-31
申请号：US11304901
申请日：2005-12-16
申请人： Adrian Leonard Smith , Paul Edward Brennan , Frenel Fils DeMorin , Gang Liu , Nick A. Paras , Daniel Martin Retz , Elizabeth Rainbeau
发明人： Adrian Leonard Smith , Paul Edward Brennan , Frenel Fils DeMorin , Gang Liu , Nick A. Paras , Daniel Martin Retz , Elizabeth Rainbeau
IPC分类号： C07D409/14 , C07D417/14 , A61K31/506 , A61P19/02 , A61P35/00
CPC分类号： C07D417/14 , C07D409/14
摘要： The invention relates to aminopyrimidine compounds useful for treating diseases mediated by polo-like kinase 1 (Plk1). The invention also relates to the therapeutic use of such aminopyrimidine compounds and compositions thereof in treating disease states associated with abnormal cell growth and unwanted cell proliferation.
摘要翻译：本发明涉及可用于治疗由polo样激酶1（Plk1）介导的疾病的氨基嘧啶化合物。本发明还涉及这种氨基嘧啶化合物及其组合物在治疗与异常细胞生长和不想要的细胞增殖相关的疾病状态中的治疗用途。

10. 发明授权

US5783698A Chemical synthesis of 1,3-disubstituted quinazolinediones 失效
标题翻译：化学合成1,3-二取代喹唑啉二酮
公开(公告)号：US5783698A
公开(公告)日：1998-07-21
申请号：US779498
申请日：1997-01-07
申请人： Adrian Leonard Smith
发明人： Adrian Leonard Smith
IPC分类号： C07D239/96 , C07D239/54
CPC分类号： C07D239/96
摘要： The present invention relates to a method for the synthesis of 1,3-disubstituted quinazolinedione derivatives which comprises: (a) reacting a haloformate functionalized polystyrene resin with a substituted anthranilic acid derivative under conditions effective to form a urethane-linkage; (b) reacting the product of step (a) with a primary amine under conditions effective to form an anthranilamide derivative; (c) heating the anthranilamide to effect intramolecular cyclization thereby liberating the 1,3-disubstituted quinazolinedione derivative from the resin into solution; and (d) isolating the 1,3-disubstituted quinazolinedione by filtration and solvent removal.
摘要翻译：本发明涉及1,3-二取代喹唑啉二酮衍生物的合成方法，其包括：（a）在有效形成氨基甲酸酯键的条件下，使卤代甲酸酯官能化聚苯乙烯树脂与取代的邻氨基苯甲酸衍生物反应; （b）在有效形成邻氨基苯甲酰胺衍生物的条件下使步骤（a）的产物与伯胺反应; （c）加热邻氨基苯甲酰胺进行分子内环化，从而将1,3-二取代的喹唑啉二酮衍生物从树脂释放到溶液中; 和（d）通过过滤和溶剂去除分离1,3-二取代的喹唑啉二酮。

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