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1. 发明授权

US07253184B2 4-Substituted quinolines as antitumor agents 失效
标题翻译： 4-取代的喹啉作为抗肿瘤剂
公开(公告)号：US07253184B2
公开(公告)日：2007-08-07
申请号：US10415813
申请日：2001-10-25
申请人： Francis Thomas Boyle , Keith Hopkinson Gibson
发明人： Francis Thomas Boyle , Keith Hopkinson Gibson
IPC分类号： A61K31/4706 , C07D215/42
CPC分类号： C07D215/56 , C07D215/54 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The invention concerns compounds of formula (I), wherein each of R1, R2, R3, R4, R5, R6, R8, R9, R10 m, n, p, X, Y and Z have any meanings defined in the description, processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-proliferative agent in the treatment of solid tumour disease.
摘要翻译：本发明涉及式（I）化合物，其中R 1，R 2，R 3，R 4， R 5，R 5，R 6，R 8，R 9，R 10， SUP，m，n，p，X，Y和Z具有本说明书中定义的任何含义，其制备方法，含有它们的药物组合物及其在制备用于治疗中的抗增殖剂的药物中的用途的实体瘤病。

2. 发明授权

US07101897B2 Farnesyl transferase inhibitors 失效
标题翻译：法呢基转移酶抑制剂
公开(公告)号：US07101897B2
公开(公告)日：2006-09-05
申请号：US10110690
申请日：2000-12-18
申请人： James Michael Wardleworth , Francis Thomas Boyle , Zbigniew Matusiak
发明人： James Michael Wardleworth , Francis Thomas Boyle , Zbigniew Matusiak
IPC分类号： A61K31/40 , A61K31/44 , A61K31/445 , C07D260/02 , C07D207/12
CPC分类号： C07D401/12 , C07D207/12
摘要： This invention relates to compounds of formula (I) that inhibit farnesylation of gene products through inhibition of the enzyme farnesyl-protein transferase (FPTase). The invention also relates to methods of manufacturing the compounds, pharmaceutical compositions and methods of treating diseases, especially cancer, which are mediated through farnesylation.
摘要翻译：本发明涉及通过抑制法呢基蛋白转移酶（FPTase）抑制基因产物法尼基化的式（I）化合物。本发明还涉及制备化合物的方法，药物组合物和治疗由法呢基化介导的疾病，特别是癌症的方法。

3. 发明授权

US07067532B2 Substituted quinolines as antitumor agents 失效
标题翻译：取代的喹啉作为抗肿瘤剂
公开(公告)号：US07067532B2
公开(公告)日：2006-06-27
申请号：US10415812
申请日：2001-10-26
申请人： Francis Thomas Boyle , Keith Hopkinson Gibson , Kevin Michael Foote
发明人： Francis Thomas Boyle , Keith Hopkinson Gibson , Kevin Michael Foote
IPC分类号： A61K31/47 , C07D215/38 , C07D413/00 , C07D417/00 , C07D205/08 , C07D401/00 , C07D279/10
CPC分类号： C07D215/56 , C07D215/54 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The invention provides a compound of Formula (Ia), or a pharmaceutically acceptable salt pro-drug or solvate thereof. The invention also provides a process for the preparation of a compound of Formula (Ia), pharmaceutical compositions of a compound of Formula (Ia) and methods for the treatment or prevention of cancer comprising administering an effective amount of a compound of Formula (Ia).
摘要翻译：本发明提供式（Ia）化合物或其药学上可接受的盐前体药物或其溶剂合物。本发明还提供了制备式（Ia）化合物，式（Ia）化合物的药物组合物和治疗或预防癌症的方法的方法，包括给予有效量的式（Ia）化合物，。

4. 发明授权

US06777438B2 Inhibitors of farnesyl protein transferase 失效
标题翻译：法呢基蛋白转移酶抑制剂
公开(公告)号：US06777438B2
公开(公告)日：2004-08-17
申请号：US10168379
申请日：2002-06-20
申请人： James Michael Wardleworth , Francis Thomas Boyle , Zbigniew Matusiak
发明人： James Michael Wardleworth , Francis Thomas Boyle , Zbigniew Matusiak
IPC分类号： A61K3140
CPC分类号： C07D401/12 , C07D207/12 , C07D401/14
摘要： This invention relates to compounds of formula (I) that inhibit farnesylation of gene products through inhibition of the enzyme farnesyl-protein transferase (FPTase). The invention also relates to methods of manufacturing the compounds, pharmaceutical compositions and methods of treating diseases, especially cancer, which are mediated through farnesylation.
摘要翻译：本发明涉及通过抑制法呢基蛋白转移酶（FPTase）抑制基因产物法尼基化的式（I）化合物。本发明还涉及制备化合物的方法，药物组合物和治疗由法呢基化介导的疾病，特别是癌症的方法。

5. 发明申请

US20110003831A1 N-(-3-METHOXY-5-METHYLPYRAZIN-2-YL)-2-(4-'1,3,4-OXADIAZOL-2-YL!PHENYL)PYRIDINE-3 SULPHONAMIDE AS AN ANTICANCER AGENT 审中-公开
标题翻译： N - （ - 3-甲氧基-5-甲基吡嗪-2-基）-2-（4'，3,3,4-氧杂双环-2-基）苯基）吡啶-3-磺酰胺作为反应剂
公开(公告)号：US20110003831A1
公开(公告)日：2011-01-06
申请号：US12880347
申请日：2010-09-13
申请人： David Williams Tonge , Sian Tomiko Taylor , Francis Thomas Boyle , Andrew Mark Hughes , Donna Johnson , Marianne Bernice Ashford , Nigel Charles Barrass
发明人： David Williams Tonge , Sian Tomiko Taylor , Francis Thomas Boyle , Andrew Mark Hughes , Donna Johnson , Marianne Bernice Ashford , Nigel Charles Barrass
IPC分类号： A61K31/497 , A61P35/00 , A61P35/02 , A61P35/04
CPC分类号： A61K31/497
摘要： The use of N-(3-methoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl]phenyl)pyridine-3-sulphonamide, or a pharmaceutically acceptable salt thereof, in the treatment of cancer and/or pain in a warm blooded animal such as man is described.
摘要翻译：使用N-（3-甲氧基-5-甲基吡嗪-2-基）-2-（4- [1,3,4-恶二唑-2-基]苯基）吡啶-3-磺酰胺或其药学上可接受的盐描述了在诸如人类的温血动物中治疗癌症和/或疼痛。

6. 发明授权

US07449489B2 Indolylalkylamino-methylidenecarbamate derivatives useful as GnRH antagonists 失效
标题翻译：用作GnRH拮抗剂的吲哚基烷基氨基 - 亚甲基氨基甲酸酯衍生物
公开(公告)号：US07449489B2
公开(公告)日：2008-11-11
申请号：US10524986
申请日：2003-08-18
申请人： Francis Thomas Boyle , Robert Davies , Zbigniew Matusiak , Michael Wardleworth
发明人： Francis Thomas Boyle , Robert Davies , Zbigniew Matusiak , Michael Wardleworth
IPC分类号： A61K31/404 , C07D209/04
CPC分类号： C07D405/14 , C07D209/16 , C07D401/14 , C07D453/06 , C07D487/08
摘要： The invention relates to a group of novel indole compounds of Formula (I): wherein: R1, R2, R4, R6, R6a, R7, R8, R9, R10, and A are as defined in the specification, which are useful as gonadotrophin releasing hormone antagonists. The invention also relates to pharmaceutical formulations of said compounds, methods of treatment using said compounds and to processes for the preparation of said compounds.
摘要翻译：本发明涉及一组式（I）的新型吲哚化合物：其中：R 1，R 2，R 4，R 4， R 6，R 6a，R 7，R 8，R 9，R 9， SUP> 10和A如说明书中所定义，其可用作促性腺激素释放激素拮抗剂。本发明还涉及所述化合物的药物制剂，使用所述化合物的治疗方法和所述化合物的制备方法。

7. 发明授权

US06946468B1 3-mercaptopyrrolidines as farnesyl protein transferase inhibitors 失效
标题翻译： 3-巯基吡咯烷作为法呢基蛋白转移酶抑制剂
公开(公告)号：US06946468B1
公开(公告)日：2005-09-20
申请号：US09242461
申请日：1997-08-13
申请人： Francis Thomas Boyle , James Michael Wardleworth
发明人： Francis Thomas Boyle , James Michael Wardleworth
IPC分类号： A61K31/40 , A61K31/427 , A61K31/4439 , A61K31/496 , A61P25/00 , A61P35/00 , A61P43/00 , C07D207/12 , C07D401/12 , C07D403/06 , C07D403/12 , C07D417/12 , A16K31/495 , C07D403/00 , A16K31/50
CPC分类号： C07D401/12 , C07D207/12 , C07D403/06 , C07D417/12
摘要： The present invention relates to inhibitors of ras farnesylation of the Formula I wherein: R1 is for example H and further values as defined in the specification; R2 is for example H and further values as defined in the specification; R3 is for example H or a substituent having values as defined in the specification; p is 0-3 in which R3 values can be the same or different; L is a linking moiety for example —CH2—NH— and further values as defined in the specification; A is selected from phenyl; naphthyl; a 5-10 membered monocyclic or bicyclic heteroaryl ring containing upto 5 heteroatoms where the heteroatoms are independently selected from O, N & S; or a —S—S— dimer thereof when R2═H; or a N-oxide or a pharmaceutically-acceptable salt, prodrug or solvate thereof. Processes for their preparation their use as therapeutic agents and pharmaceutical compositions containing them.
摘要翻译：本发明涉及式I的Ras法呢基化抑制剂，其中：R 1是例如H和如说明书中定义的其它值; R 2是例如H和说明书中定义的其它值; R 3是例如H或具有本说明书中定义的值的取代基; p为0-3，其中R 3 3可以相同或不同; L是例如-CH 2 - NH-的连接部分和如说明书中定义的进一步的值; A选自苯基; 萘基; 含有至多5个杂原子的5-10元单环或双环杂芳基环，其中杂原子独立地选自O，N和S; 或其-S-S-二聚体;当R 2〜或N-氧化物或其药学上可接受的盐，前药或溶剂化物。其制备方法用作治疗剂和含有它们的药物组合物。

8. 发明授权

US06232338B1 4-Mercaptopyrrolidine derivatives as farnesyl transferase inhibitors 失效
标题翻译： 4-巯基吡咯烷衍生物作为法呢基转移酶抑制剂
公开(公告)号：US06232338B1
公开(公告)日：2001-05-15
申请号：US09011135
申请日：1998-02-03
申请人： David Huw Davies , Francis Thomas Boyle , James Michael Wardleworth , Peter Wedderburn Kenny , Peter Beverley Scholes , Zbigniew Stanely Matusiak
发明人： David Huw Davies , Francis Thomas Boyle , James Michael Wardleworth , Peter Wedderburn Kenny , Peter Beverley Scholes , Zbigniew Stanely Matusiak
IPC分类号： A61K3140
CPC分类号： C07D401/12 , C07D207/12 , C07D409/12
摘要： Pharmaceutical compositions comprising an inhibitor of ras farnesylation of formula (I) wherein, R1 is for example H and further values as defined in the specification; R2 is for example H and further values as defined in the specification; R3 is for example H or a substituent having values as defined in the specification; p is 0-3 in which R3 values can be the same or different; L is a linking moiety for example —CO—NH2— and further values as defined in the specification; A is selected from phenyl; naphthyl; a 5-10 membered monocyclic or bicyclic heteroaryl ring containing up to 5 heteroatoms where the heteroatoms are independently selected from O, N and S; or a —S—S— dimer thereof when R2=H; or an enantiomer, diastereoisomer, pharmaceutically acceptable salt, prodrug or solvate thereof together with a pharmaceutically acceptable diluent or carrier. A particular use is cancer therapy.
摘要翻译：包含式（I）的ras法呢基酯化抑制剂的药物组合物，其中R1为例如本说明书中定义的其它值; R2是例如H和说明书中定义的其它值; R3是例如H或具有本说明书中定义的值的取代基; p为0-3，其中R3值可以相同或不同; L是例如-CO-NH 2的连接部分和如说明书中定义的进一步的值; A选自苯基; 萘基; 含有多达5个杂原子的5-10元单环或双环杂芳基环，其中杂原子独立地选自O，N和S; 或其-S-S-二聚体时，R 2 = H; 或其对映体，非对映异构体，药学上可接受的盐，前药或溶剂合物以及药学上可接受的稀释剂或载体。一个特别的用途是癌症治疗。

9. 发明授权

US5789417A Tricyclic compounds with pharmaceutical activity 失效
标题翻译：具有药物活性的三环化合物
公开(公告)号：US5789417A
公开(公告)日：1998-08-04
申请号：US432161
申请日：1995-06-28
申请人： Francis Thomas Boyle , James William Crook , Zbigniew Stanley Matusiak
发明人： Francis Thomas Boyle , James William Crook , Zbigniew Stanley Matusiak
IPC分类号： A61K31/505 , A61K31/517 , A61K31/519 , A61P35/00 , C07D239/70 , C07D401/12 , C07D403/12 , A61K31/495
CPC分类号： C07D401/12 , C07D239/70 , C07D403/12
摘要： The invention relates to tricyclic compounds of formula (I) ##STR1## wherein R.sup.1 is hydrogen, amino, (1-4C)alkyl, (1-4C)alkoxy, hydroxy-(1-4C)alkyl or fluoro-(1-4C)alkyl; R.sup.2 is hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, hydroxy-(2-4C)alkyl, halogeno-(2-4C)alkyl or cyano-(1-4C)alkyl; Ar is optionally-substituted phenylene, thiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediyl; and R.sup.3 includes a group of the formula --NHCH(CO.sub.2 H)--A.sup.1 --Y.sup.1 wherein A.sup.1 is (1-6C)alkylene and Y.sup.1 is carboxy, tetrazol-5-yl, N-�(1-4C)alkylsulphonyl!carbamoyl, N(phenylsulphonyl)carbamoyl, tetrazol-5-ylthio, tetrazol-5-ylsulphinyl or tetrazol-5-ylsulphonyl; or pharmaceutically-acceptable salts or esters thereof; to processes for their manufacture; to pharmaceutical compositions containing them; and to their use as anti-cancer agents.
摘要翻译： PCT No.PCT / GB93 / 02281 Sec。 371日期：1995年6月28日 102（e）日期1995年6月28日PCT提交1993年11月4日PCT公布。出版物WO94 / 11354 日期：1994年5月26日本发明涉及式（I）的三环化合物其中R 1为氢，氨基，（1-4C）烷基，（1-4C）烷氧基，羟基 - （1-4C）烷基或氟 - （1-4C）烷基; R2是氢，（1-4C）烷基，（3-4C）烯基，（3-4C）炔基，羟基 - （2-4C）烷基，卤代 - （2-4C）烷基或氰基 - （1-4C）烷基; Ar是任选取代的亚苯基，噻吩二基，噻唑二基，吡啶二基或嘧啶二基; 并且R 3包括式-NHCH（CO 2 H）-A1-Y1的基团，其中A 1为（1-6C）亚烷基且Y 1为羧基，四唑-5-基，N - [（1-4C）烷基磺酰基]氨基甲酰基，N （苯基磺酰基）氨基甲酰基，四唑-5-基硫代，四唑-5-基亚磺酰基或四唑-5-基磺酰基; 或其药学上可接受的盐或酯; 制造过程; 含有它们的药物组合物; 并将其用作抗癌剂。

10. 发明授权

US06414145B1 Imidazolyl compounds as inhibitors of farnesyl-protein tranferase 失效
标题翻译：咪唑基化合物作为法呢基蛋白转移酶抑制剂
公开(公告)号：US06414145B1
公开(公告)日：2002-07-02
申请号：US09355440
申请日：1999-07-28
申请人： Francis Thomas Boyle , Gareth Morse Davies , James Michael Wardleworth , Jean-Claude Arnould
发明人： Francis Thomas Boyle , Gareth Morse Davies , James Michael Wardleworth , Jean-Claude Arnould
IPC分类号： C07D23361
CPC分类号： C07D233/64 , C07D231/12 , C07D233/56 , C07D249/08
摘要： The present invention relates to inhibitors of ras farnesylation of Formula (I), wherein T is of Formula (1) or (2) or (3); A is aryl or heteroaryl; B is aryl or heteroaryl; X and Y represent hydrogen, or both X and Y can represent a single bond (so as to form a double bond); R1 represents a group of Formula (II) or (III), the group of Formula (II) or Formula (III) (having L or D configuration at the chiral alpha carbon in the corresponding free amino acid); R2 represents hydrogen, aryl or heteroaryl; Z represents a direct bond, methylene, ethylene, vinylene, oxy, —CH2—O— or —O—CH2—; and R3—R4, p and r are as defined in the specification or a pharmaceutically-acceptable salt, prodrug or solvate thereof. Processes for their preparation, their use as therapeutic agents and pharmaceutical compositions containing them. A particular use is in cancer therapy
摘要翻译：本发明涉及式（I）的ras法呢基化抑制剂，其中T为式（1）或（2）或（3）; A是芳基或杂芳基; B是芳基或杂芳基; X和Y表示氢，或者X和Y可以表示单键（从而形成双键）; R 1表示式（II）或（III）中的基团，式（II）或式（III）的基团（在相应的游离氨基酸中的手性α碳上具有L或D构型）; R2代表氢，芳基或杂芳基; Z表示直接键，亚甲基，亚乙基，亚乙烯基，氧基，-CH 2 -O-或-O-CH 2 - ; 和R3-R4，p和r如说明书中所定义或其药学上可接受的盐，前药或溶剂化物。其制备方法，用作治疗剂和含有它们的药物组合物。一个特别的用途是癌症治疗

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