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1. 发明授权

US07411074B2 Process and intermediates for the preparation of the thienopyrrole derivatives 失效
标题翻译：制备噻吩并吡咯衍生物的方法和中间体
公开(公告)号：US07411074B2
公开(公告)日：2008-08-12
申请号：US10528974
申请日：2003-09-29
申请人： Paul Murray , Jeremy Stephen Parker , Paul Schofield , Andrew Stocker
发明人： Paul Murray , Jeremy Stephen Parker , Paul Schofield , Andrew Stocker
IPC分类号： C07D495/04
CPC分类号： C07D495/04 , C07D333/36 , Y02P20/55
摘要： A process for preparing a compound of formula (I) where R4 and R5 are as defined in the specification; and R6 is hydrogen or a protecting group, which process comprises cyclisation of a compound of formula (II) where R4, R5 and R6 are as defined in relation to formula (I), and R7 is nitrogen-protecting group, and removing the group R7—, and thereafter if desired or necessary, removing any protecting group R6 to obtain the corresponding carboxylic acid. Novel intermediates and the use of the products in the preparation of pharmaceutical compounds is also described and claimed.
摘要翻译：制备其中R 4和R 5的式（I）化合物的方法如说明书中所定义; 和R 6是氢或保护基，该方法包括使式（II）的化合物环化，其中R 4，R 5和 R 6如关于式（I）所定义，R 7为氮保护基，除去R 7 - ，然后如果需要或必要的话，除去任何保护基团R 6以获得相应的羧酸。还描述和要求保护新型中间体和制备药物化合物中产物的用途。

2. 发明申请

US20060035953A1 Process and intermediates for the preparation of the thienopyrrole derivatives 失效
标题翻译：制备噻吩并吡咯衍生物的方法和中间体
公开(公告)号：US20060035953A1
公开(公告)日：2006-02-16
申请号：US10528974
申请日：2003-09-29
申请人： Paul Murray , Jeremy Parker , Paul Schofield , Andrew Stocker
发明人： Paul Murray , Jeremy Parker , Paul Schofield , Andrew Stocker
IPC分类号： A61K31/407 , C07D498/02
CPC分类号： C07D495/04 , C07D333/36 , Y02P20/55
摘要： A process for preparing a compound of formula (I) where R4 and R5 are as defined in the specification; and R6 is hydrogen or a protecting group, which process comprises cyclisation of a compound of formula (II) where R4, R5 and R6 are as defined in relation to formula (I), and R7 is nitrogen-protecting group, and removing the group R7—, and thereafter if desired or necessary, removing any protecting group R6 to obtain the corresponding carboxylic acid. Novel intermediates and the use of the products in the preparation of pharmaceutical compounds is also described and claimed.
摘要翻译：制备其中R 4和R 5的式（I）化合物的方法如说明书中所定义; 和R 6是氢或保护基，该方法包括使式（II）的化合物环化，其中R 4，R 5和 R 6如关于式（I）所定义，R 7为氮保护基，除去R 7 - ，然后如果需要或必要的话，除去任何保护基团R 6以获得相应的羧酸。还描述和要求保护新型中间体和制备药物化合物中产物的用途。

3. 发明申请

US20050272938A1 Process and intermediates for the preparation of thienopyrrole derivatives 失效
标题翻译：制备噻吩并吡咯衍生物的方法和中间体
公开(公告)号：US20050272938A1
公开(公告)日：2005-12-08
申请号：US10528612
申请日：2003-09-29
申请人： Michael Butters , Paul Schofield , Andrew Stocker
发明人： Michael Butters , Paul Schofield , Andrew Stocker
IPC分类号： C07D333/36 , C07D495/04 , C07D497/02
CPC分类号： C07D495/04 , C07D333/36 , Y02P20/55
摘要： Novel Process and Intermediates. A process for preparing a compound of formula (I) where R4 and R5 are as defined in the specification; and R6 is hydrogen or a protecting group, which process comprises cyclisation of a compound of formula (II) where R4 and R5 and R6 are as defined in relation to formula (I), and R7 is nitrogen protecting group, and removing the group R7, and thereafter if desired, removing any protecting group R6. Novel intermediates and the use of these in the formation of pharmaceutical compounds is also described and claimed.
摘要翻译：新工艺和中间体。制备其中R 4和R 5的式（I）化合物的方法如说明书中所定义; 和R 6是氢或保护基，该方法包括式（II）化合物的环化，其中R 4和R 5和R 5和 R 6如关于式（I）所定义，R 7为氮保护基，除去基团R 7，和此后如果需要，除去任何保护基团R 6。还描述和要求保护新型中间体及其在药物化合物形成中的用途。

4. 发明授权

US07307174B2 Process and intermediates for the preparation of thienopyrrole derivatives 失效
标题翻译：制备噻吩并吡咯衍生物的方法和中间体
公开(公告)号：US07307174B2
公开(公告)日：2007-12-11
申请号：US10528612
申请日：2003-09-29
申请人： Michael Butters , Paul Schofield , Andrew Stocker
发明人： Michael Butters , Paul Schofield , Andrew Stocker
IPC分类号： C07D495/04
CPC分类号： C07D495/04 , C07D333/36 , Y02P20/55
摘要： Novel Process and Intermediates. A process for preparing a compound of formula (I) where R4 and R5 are as defined in the specification; and R6 is hydrogen or a protecting group, which process comprises cyclisation of a compound of formula (II) where R4 and R5 and R6 are as defined in relation to formula (I), and R7 is nitrogen protecting group, and removing the group R7, and thereafter if desired, removing any protecting group R6. Novel intermediates and the use of these in the formation of pharmaceutical compounds is also described and claimed
摘要翻译：新工艺和中间体。制备其中R 4和R 5的式（I）化合物的方法如说明书中所定义; 和R 6是氢或保护基，该方法包括式（II）化合物的环化，其中R 4和R 5和R 5和 R 6如关于式（I）所定义，R 7为氮保护基，除去基团R 7，和此后如果需要，除去任何保护基团R 6。还描述和要求保护新型中间体及其在药物化合物形成中的用途

5. 发明申请

US20090221663A1 PYRAZOLE DERIVATIVES AS 11-BETA-HSD1 INHIBITORS 失效
标题翻译：作为11-BETA-HSD1抑制剂的吡唑衍生物
公开(公告)号：US20090221663A1
公开(公告)日：2009-09-03
申请号：US12259562
申请日：2008-10-28
申请人： Martin John Packer , James Stewart Scott , Andrew Stocker , Paul Robert Owen Whittamore
发明人： Martin John Packer , James Stewart Scott , Andrew Stocker , Paul Robert Owen Whittamore
IPC分类号： A61K31/4155 , C07D405/12
CPC分类号： C07D231/18 , C07D231/14 , C07D403/06 , C07D405/12
摘要： A compound of Formula (I): and pharmaceutically-acceptable salts thereof wherein the variable groups are defined within; their use in the inhibition of 11βHSD1, processes for making them and pharmaceutical compositions comprising them are also described.
摘要翻译：式（I）的化合物及其药学上可接受的盐，其中定义可变基团; 还描述了其用于抑制11betaHSD1的用途，其制备方法和包含它们的药物组合物。

6. 发明授权

US06730672B2 Aminoheterocyclic derivatives as antithrombotic or anticoagulant agents 失效
标题翻译：氨基杂环衍生物作为抗血栓形成或抗凝血剂
公开(公告)号：US06730672B2
公开(公告)日：2004-05-04
申请号：US09800745
申请日：2001-03-08
申请人： Alan Wellington Faull , Andrew Stocker , Colette Marie Mayo , John Preston
发明人： Alan Wellington Faull , Andrew Stocker , Colette Marie Mayo , John Preston
IPC分类号： C07D40114
CPC分类号： C07D213/74 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14
摘要： The invention concerns compounds of formula (I) wherein each of G1, G2 and G3 is CH or N; m is 1 or 2; R1 includes hydrogen, halogeno and (1-4C)alkyl; M1 is a group of the formula: NR2—L1—T1R3 in which R2 and R3 together form a (1-4C)alkylene group, L1 includes (1-4C)alkylene, and T1 is CH or N; A may be a direct link; M2 is a group of the formula: (T2R4)r—L2—T3R5 in which r is 0 or 1, each of T2 and T3 is CH or N, each of R4 and R5 is hydrogen or (1-4C)alkyl, or R4 and R5 together form a (1-4C)alkylene group, and L2 includes (1-4C)alkylene; M3 may be a direct link to X; X includes sulphonyl; and Q includes naphthyl and a heterocyclic moiety; or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use as antithrombotic or anticoagulant agents.
摘要翻译：本发明涉及式（I）化合物，其中G 1，G 2和G 3各自为CH或N; m为1或2; R 1包括氢，卤素和（1-4C）烷基; M 1是下式的基团：其中R 2和R 3一起形成（1-4C）亚烷基，其中R 2，R 2，R 3，R 3，，L 1包括（1-4C）亚烷基，T 1是CH或N; A可能是直接链接; M 2是下式的基团：（T 2 R 4）r L 2 -T 3 R 5，其中r是0或1，每个T 2和T R 3和R 5分别是氢或（1-4C）烷基，或者R 4和R 5一起形成（1-4C）亚烷基，和L 2包括（1-4C）亚烷基; M 3可以直接连接到X; X包括磺酰基; 且Q包括萘基和杂环部分; 或其药学上可接受的盐; 其制备方法，含有它们的药物组合物及其作为抗血栓形成或抗凝血剂的用途。

7. 发明申请

US20070123528A1 INDOLE-AMID DERIVATIVES WHICH POSSESS GLYCOGEN PHOSPHORYLASE INHIBITORY ACTIVITY 失效
标题翻译：含有胶原酶抑制活性的吲哚美辛衍生物
公开(公告)号：US20070123528A1
公开(公告)日：2007-05-31
申请号：US11565605
申请日：2006-11-30
申请人： Andrew Stocker , Paul Whittamore
发明人： Andrew Stocker , Paul Whittamore
IPC分类号： A61K31/5377 , A61K31/497 , A61K31/496 , A61K31/454 , A61K31/4439 , A61K31/433 , A61K31/4178 , A61K31/405 , C07D413/02 , C07D403/02
CPC分类号： C07D413/12 , C07D209/42
摘要： Heterocyclic amides of formula (1) and pharmaceutically acceptable salts or pro-drugs thereof wherein variable groups are as described herein; which possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity are described. Processes for the manufacture of said heterocyclic amide derivatives and pharmaceutical compositions containing them are also described.
摘要翻译：式（1）的杂环酰胺及其药学上可接受的盐或前药，其中可变基团如本文所述; 其具有糖原磷酸化酶抑制活性，因此具有与增加的糖原磷酸化酶活性相关的疾病状态的治疗价值。还描述了制备所述杂环酰胺衍生物和含有它们的药物组合物的方法。

8. 发明申请

US20050131015A1 Heterocyclic amide derivatives as inhibitors of glycogen phoshorylase 失效
标题翻译：杂环酰胺衍生物作为糖原磷酸化酶的抑制剂
公开(公告)号：US20050131015A1
公开(公告)日：2005-06-16
申请号：US10506741
申请日：2003-03-04
申请人： Alan Birch , Andrew Morley , Andrew Stocker , Paul Whittamore
发明人： Alan Birch , Andrew Morley , Andrew Stocker , Paul Whittamore
IPC分类号： A61K31/4375 , A61K31/4709 , A61K31/519 , A61P3/00 , A61P3/04 , A61P3/10 , A61P9/10 , A61P43/00 , C07D495/04 , C07D519/00 , C07D498/02
CPC分类号： C07D495/04
摘要： Heterocyclic amides of formula (1) wherein: X is N or CH; R4 and R5 together are either —S—C(R6)═C(R7)— or —C(R7)═C(R6)—S—; R6 and R7 are independently selected from, for example hydrogen, halo and Cl-4alkyl; A is phenylene or heteroarylene; n is 0, 1 or 2; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; R2 is hydrogen, hydroxy or carboxy; R3 is selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C1-4alkyl(optionally substituted by 1 or 2 R8 groups); R8 is selected from for example hydroxy, —COCOOR9, —C(O)N(R9)(R10), —NHC(O)R9, (R9)(R10)N— and —COOR9; R9 and R10 are selected from for example hydrogen, hydroxy, C1-4alkyl (optionally substituted by 1 or 2 R13); R13 is selected from hydroxy, halo, trihalomethyl and C1-4alkoxy; or a pharmaceutically acceptable salt or pro-drug thereof; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of said heterocyclic amide derivatives and pharmaceutical compositions containing them are described.
摘要翻译：式（1）的杂环酰胺其中：X是N或CH; R 4和R 5一起是-SC（R 6）-C（R 7） - 或 -C（R 7）C（R 6）-S-; R 6和R 7独立地选自，例如氢，卤素和C 1-4烷基; A是亚苯基或亚杂芳基; n为0,1或2; R 1选自例如卤素，硝基，氰基，羟基，羧基; R 2是氢，羟基或羧基; R 3选自例如氢，羟基，芳基，杂环基和C 1-4烷基（任选被1或2个R 8取代）组）; R 8选自例如羟基，-COCOOR 9，-C（O）N（R 9）（R 10）），-NHC（O）R 9，（R 9）（R 10）N - 和-COOR ^{9 ; R 9和R 10选自例如氢，羟基，C 1-4烷基（任选被1或2个R SUP取代 > 13 ）; R 13选自羟基，卤素，三卤代甲基和C 1-4烷氧基; 或其药学上可接受的盐或前体药物; 具有糖原磷酸化酶抑制活性，因此具有与增加的糖原磷酸化酶活性相关的疾病状态的治疗价值。描述了制备所述杂环酰胺衍生物和含有它们的药物组合物的方法。}

9. 发明授权

US06486154B1 (Hetero) aryl-sulfonamide derivatives, their preparation and their use as factor XA inhibitors 失效
标题翻译：（杂芳基）磺酰胺衍生物，它们的制备及其作为因子XA抑制剂的用途
公开(公告)号：US06486154B1
公开(公告)日：2002-11-26
申请号：US09463446
申请日：2000-01-27
申请人： Andrew Stocker , John Preston
发明人： Andrew Stocker , John Preston
IPC分类号： A61K3154
CPC分类号： C07D401/04
摘要： A compound of formula (I), or a pharmaceutically-acceptable salt thereof, wherein A is an optionally substituted 5- or 6-membered monocyclic aromatic ring containing 1, 2 or 3 ring heteroatoms; B is optionally substituted phenylene or a 6-membered heterocyclic ring containing 1, 2 or 3 nitrogen heteroatoms; R and R1 are hydrogen or (1-4C)alkyl; n is 1 or 2; R2 and R3 are hydrogen, (1-6C)alkyl, (4-7C)cycloalkyl, or (2-6C)alkenyl, or R2 and R3 may form along with the nitrogen to which they are attached a 5-, 6- or 7-membered heterocyclic ring, wherein each R2 or R3 group or any heterocyclic ring formed from R2 and R3 may be optionally substituted with various substituent groups, and wherein Q may be optionally substituted by various substituent groups, which posseses antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention relates to processes for the preparation of the compounds represented by formula (I), to pharmaceutical compositions containing them, and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect.
摘要翻译：式（I）化合物或其药学上可接受的盐，其中A是含有1,2或3个环杂原子的任选取代的5元或6元单环芳环; B是任选取代的亚苯基或含有1,2或3个氮杂原子的6元杂环; R和R 1是氢或（1-4C）烷基; n为1或2; R2和R3是氢，（1-6C）烷基，（4-7C）环烷基或（2-6C）烯基，或R2和R3可以与它们所连接的氮一起形成5-，6-或 7元杂环，其中每个R 2或R 3基团或由R 2和R 3形成的任何杂环可以任选被各种取代基取代，并且其中Q可任选地被各种取代基取代，这些取代基具有抗血栓形成和抗凝血性质，因此在治疗人或动物的方法中有用。本发明涉及制备由式（I）表示的化合物的方法，含有它们的药物组合物及其在制备用于产生抗血栓形成或抗凝血作用的药物中的用途。

10. 发明授权

US06395731B1 Heterocyclic derivatives which inhibit Factor Xa 失效
标题翻译：抑制因子Xa的杂环衍生物
公开(公告)号：US06395731B1
公开(公告)日：2002-05-28
申请号：US09674563
申请日：2000-12-20
申请人： Nowak Thorsten , John Preston , John W Rayner , Michael J Smithers , Andrew Stocker
发明人： Nowak Thorsten , John Preston , John W Rayner , Michael J Smithers , Andrew Stocker
IPC分类号： A61K31541
CPC分类号： C07D233/64 , C07D213/56 , C07D233/88 , C07D237/12 , C07D237/14 , C07D237/20 , C07D239/26 , C07D239/34 , C07D239/36 , C07D239/42 , C07D295/26
摘要： The invention relates to heterocyclic derivatives of formula (I) and (Ia), or pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect.
摘要翻译：本发明涉及具有抗血栓形成和抗凝血性质的式（I）和（Ia）的杂环衍生物或其药学上可接受的盐，因此可用于治疗人或动物的方法。本发明还涉及制备杂环衍生物的方法，含有它们的药物组合物及其在制备用于产生抗血栓形成或抗凝血作用的药物中的用途。

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