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1. 发明申请

US20080058332A1 2,4,6-Trisubstituted Pyrimidines as Phosphotidylinositol (Pi) 3-Kinase Inhibitors and Their Use in the Treatment of Cancer 审中-公开
公开(公告)号：US20080058332A1
公开(公告)日：2008-03-06
申请号：US11630677
申请日：2005-07-07
申请人： John Bailey , Michael Giles , Martin Pass
发明人： John Bailey , Michael Giles , Martin Pass
IPC分类号： A61K31/5377 , A61P35/00 , A61P35/02 , C07D413/04
CPC分类号： C07D239/42 , C07D401/12 , C07D403/12 , C07D409/12 , C07D417/12
摘要： The invention concerns pyrimidine derivatives of Formula (I) wherein each of p, R1, R2, q, R3, r, R4, X1 and Q1 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the production of an anti-proliferative effect in a warm-blooded animal such as man.

2. 发明申请

US20070149560A1 Novel fused triazolones and the uses thereof 审中-公开
标题翻译：新型稠合三唑酮及其用途
公开(公告)号：US20070149560A1
公开(公告)日：2007-06-28
申请号：US10549053
申请日：2004-03-10
申请人： Susan Ashwell , Jayachandran Ezhuthachan , Paul Lyne , Nicholas Newcombe , Martin Pass , Vibha Oza , Mei Su , Dorin Toader , Dingwei Yu , Yan Yu
发明人： Susan Ashwell , Jayachandran Ezhuthachan , Paul Lyne , Nicholas Newcombe , Martin Pass , Vibha Oza , Mei Su , Dorin Toader , Dingwei Yu , Yan Yu
IPC分类号： A61K31/4745 , C07D487/02
CPC分类号： C07D471/04 , A61K31/4196
摘要： This invention relates to novel compounds having the structural diagram (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment or prophylaxis of cancer.
摘要翻译：本发明涉及具有结构图（I）及其药物组合物及其使用方法的新型化合物。这些新化合物提供癌症的治疗或预防。

3. 发明申请

US20070088044A1 Quinazoline derivatives as antitumor agents 审中-公开
标题翻译：喹唑啉衍生物作为抗肿瘤剂
公开(公告)号：US20070088044A1
公开(公告)日：2007-04-19
申请号：US11443395
申请日：2006-05-31
申请人： Laurent Hennequin , Jason Kettle , Martin Pass , Robert Bradbury
发明人： Laurent Hennequin , Jason Kettle , Martin Pass , Robert Bradbury
IPC分类号： A61K31/517 , C07D403/02 , C07D239/94
CPC分类号： C04B35/632 , C07D239/94 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The invention concerns quinazoline derivatives of Formula (I); wherein each of Q , Q , Z, R , R , R , and m have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the prevention or treatment of tumours which are sensitive to inhibition of erbB receptor tyrosin kinases.
摘要翻译：本发明涉及式（I）的喹唑啉衍生物; 其中Q 1，Q 2，Z，R 1，R 2，R 3和m各自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预防或治疗对抑制erbB受体酪氨酸激酶敏感的肿瘤的药物中的用途。

4. 发明授权

US06670381B2 Benzamide derivatives as thrombin inhibitors 失效
标题翻译：苯甲酰胺衍生物作为凝血酶抑制剂
公开(公告)号：US06670381B2
公开(公告)日：2003-12-30
申请号：US10044769
申请日：2002-01-10
申请人： Henry Anderson Kelly , Martin Pass , David Neil Smith
发明人： Henry Anderson Kelly , Martin Pass , David Neil Smith
IPC分类号： C07D21374
CPC分类号： C07D213/74
摘要： There are provided according to the invention novel compounds of formula (I) wherein R1 represents C1-4alkyl or C3-8cycloalkyl, R2 represents C1-4alkyl or C3-4alkenyl, R3 represents hydrogen, C1-3alkyl or halogen, and R4 represents C1-6alkyl, processes for preparing them, pharmaceutical formulations containing them and their use in therapy particularly as thrombin inhibitors.
摘要翻译：根据本发明提供新的式（I）化合物，其中R 1表示C 1-4烷基或C 3-8环烷基，R 2表示C 1-4烷基或C 3-4烯基，R 3表示氢，C1- 3烷基或卤素，R 4表示C 1-6烷基，其制备方法，含有它们的药物制剂及其在治疗中的用途，特别是作为凝血酶抑制剂。

5. 发明授权

US07893063B2 2,4,6-trisubstituted pyrimidines as phosphotidylinositol (PI) 3-kinase inhibitors and their use in the treatment of cancer 失效
标题翻译： 2,4,6-三取代嘧啶作为磷脂酰肌醇（PI）3-激酶抑制剂及其在治疗癌症中的应用
公开(公告)号：US07893063B2
公开(公告)日：2011-02-22
申请号：US11630881
申请日：2005-07-07
申请人： Martin Pass
发明人： Martin Pass
IPC分类号： C07D413/14 , A61K31/5377
CPC分类号： C07D239/42 , C07D403/04 , C07D405/04 , C07D409/04
摘要： The invention concerns pyrimidine derivatives of Formula (I) wherein each of Qa, G1, G2, q, R3, r, R4, X1 and Qb have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the production of an anti-proliferative effect in a warm-blooded animal such as man.
摘要翻译：本发明涉及式（I）的嘧啶衍生物，其中Qa，G1，G2，q，R3，r，R4，X1和Qb中的每一个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在温血动物如人中产生抗增殖作用的药物中的用途。

6. 发明授权

US06677316B2 Adenosine derivatives and methods of administration 有权
标题翻译：腺苷衍生物和给药方法
公开(公告)号：US06677316B2
公开(公告)日：2004-01-13
申请号：US10217107
申请日：2002-08-13
申请人： David Edmund Bays , Richard Peter Charles Cousins , Hazel Joan Dyke , Colin David Eldred , Brian David Judkins , Martin Pass , Andrew Michael Kenneth Pennell
发明人： David Edmund Bays , Richard Peter Charles Cousins , Hazel Joan Dyke , Colin David Eldred , Brian David Judkins , Martin Pass , Andrew Michael Kenneth Pennell
IPC分类号： A61K3170
CPC分类号： C07D473/00 , C07H19/16
摘要： A method of treating a patient suffering from or susceptible to ischemic heart disease, peripheral vascular disease or stroke or which subject is suffering pain, a CNS disorder or sleep apnea which comprises administering a therapeutically effective amount of an adenosine derivative which is an agonist at the adenosine A1 receptor and which exhibits little or no agonist activity of the A3 receptor. The adenosine derivative has a general formula (I) as follows:
摘要翻译：治疗患有或易患缺血性心脏病，外周血管疾病或中风或受试者患有疼痛，CNS病症或睡眠呼吸暂停症的患者的方法，其包括给予治疗有效量的作为激动剂的腺苷衍生物腺苷A1受体并且其表现出很少或没有A3受体的激动剂活性。腺苷衍生物具有如下通式（I）：

7. 发明申请

US20080051401A1 2,4,6-Trisubstituted Pyrimidines as Phosphotidylinositol (Pi) 3-Kinase Inhibitors and Their Use in the Treatment of Cancer 审中-公开
标题翻译： 2,4,6-三取代嘧啶作为磷酸肌醇（Pi）3-激酶抑制剂及其在治疗癌症中的应用
公开(公告)号：US20080051401A1
公开(公告)日：2008-02-28
申请号：US11630676
申请日：2005-07-07
申请人： Martin Pass
发明人： Martin Pass
IPC分类号： A61K31/5377 , A61K31/445 , A61P35/00 , C07D211/00 , C07D413/00 , C07D413/04 , C07D413/14
CPC分类号： C07D401/12 , C07D239/42 , C07D403/12 , C07D413/12
摘要： The invention concerns pyrimidine derivatives of Formula (I) wherein each of p, R1, R2, q, R3, r, R4, X1 and Q1 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the production of an anti-proliferative effect in a warm-blooded animal such as man.
摘要翻译：本发明涉及式（I）的嘧啶衍生物，其中p，R 1，R 2，q，R 3，r，R “1”和“1”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在温血动物如人中产生抗增殖作用的药物中的用途。

8. 发明申请

US20070082921A1 Quinazoline derivatives as antitumor agents 审中-公开
公开(公告)号：US20070082921A1
公开(公告)日：2007-04-12
申请号：US11443208
申请日：2006-05-31
申请人： Laurent Hennequin , Jason Kettle , Martin Pass , Robert Bradbury
发明人： Laurent Hennequin , Jason Kettle , Martin Pass , Robert Bradbury
IPC分类号： A61K31/517 , C07D403/02
CPC分类号： C07D401/12 , C07D239/94 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The invention concerns quinazoline derivatives of Formula (I); wherein each of Q , Q , Z, R , R , R , and m have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the prevention or treatment of tumours which are sensitive to inhibition of erbB receptor tyrosin kinases.

9. 发明申请

US20050282845A1 Substituted pyrimidines as selective cyclooxygenase-2 inhibitors 审中-公开
标题翻译：取代的嘧啶作为选择性环氧合酶-2抑制剂
公开(公告)号：US20050282845A1
公开(公告)日：2005-12-22
申请号：US11165073
申请日：2005-06-23
申请人： Malcolm Carter , Alan Naylor , Martin Pass , Jeremy Payne , Neil Pegg
发明人： Malcolm Carter , Alan Naylor , Martin Pass , Jeremy Payne , Neil Pegg
IPC分类号： A61K31/506 , A61P29/00 , A61P43/00 , C07D405/12
CPC分类号： C07D405/12
摘要： Methods for the treatment of pain, fever, inflammation of a variety of conditions and diseases.
摘要翻译：治疗疼痛，发烧，炎症的各种病症和疾病的方法。

10. 发明授权

US06326386B1 Benzamide derivatives as thrombin inhibitors 失效
标题翻译：苯甲酰胺衍生物作为凝血酶抑制剂
公开(公告)号：US06326386B1
公开(公告)日：2001-12-04
申请号：US09678610
申请日：2000-10-04
申请人： Nigel Stephen Watson , Martin Pass , Vipulkumar Patel
发明人： Nigel Stephen Watson , Martin Pass , Vipulkumar Patel
IPC分类号： C07D21302
CPC分类号： C07D213/74 , A61K31/4409 , A61K31/4439 , C07D401/12 , C07D405/12 , C07D417/12
摘要： The invention relates to a novel class of amide derivatives which act as thrombin inhibitors as described by formula (I), where R1 and R2, independently represent a group (a) or R1 and R2 together form a C3-7 heterocycloalkyl or heterocycloalkenyl group which may be optionally substituted by C1-6 alkyl, C1-4 alkoxy, halogen, carboxylic acid or a C1-4 carboxylic acid ester group; R3 represents hydrogen, C1-3 alkyl, halogen, or C1-2 alkoxy; R4, R5 and R6 independently represent hydrogen, or halogen; R7 represents hydrogen or C1-6 alkyl; R8 represents hydrogen, C3-7 cycloalkyl, C3-7 cycloalkenyl, C3-7 heterocycloalkyl, C3-7 heterocycloalkenyl, aryl or heteroaryl, which groups are optionally substituted by one or more groups selected from halogen, hydroxy, CN, C1-6 alkyl, C1-6 alkoxy, C1-6 acyloxy, NR9R10, NHCOR11, NHSO2R12, COR13, CO2R14, CONR15R16, and SO2NHR17; X represents a bond, a C1-6 alkyl chain, or a C3-6 alkenyl chain, where one or two nitrogen, oxygen, or sulfur atoms may be optionally contained within each chain, and the chains are optionally substituted by one or more groups selected from halogen, hydroxy, CN, C1-6 alkyl, C1-6 alkoxy, C1-6 acyloxy, NR9R10, NHCOR11, NHSO2R12, COR13, CO2R14, CONR15R16, and SO2NHR17; R9-R17 represent hydrogen, C1-6 alkyl, or R9 and R10 or R15 and R16 form a C3-7 heterocycloalkyl ring, or R12 additionally may represent trifluoromethyl; and pharmaceutically acceptable derivatives or solvates thereof, to processes for their preparation; and their use in the treatment of clinical conditions susceptible to amelioration by administration of a thrombin inhibitor.
摘要翻译：本发明涉及作为如式（I）所述的凝血酶抑制剂的新一类酰胺衍生物，其中R 1和R 2独立地表示基团（a）或R 1和R 2一起形成C 3-7杂环烷基或杂环烯基，其中可以任选地被C 1-6烷基，C 1-4烷氧基，卤素，羧酸或C 1-4羧酸酯基取代; R 3表示氢，C 1-3烷基，卤素或C 1-2烷氧基; R4，R5和R6独立地表示氢或卤素; R 7表示氢或C 1-6烷基; R8表示氢，C3-7环烷基，C3-7环烯基，C3-7杂环烷基，C3-7杂链烯基，芳基或杂芳基，这些基团任选被一个或多个选自卤素，羟基，CN，C 1-6烷基的基团取代，C 1-6烷氧基，C 1-6酰氧基，NR 9 R 10，NHCOR 11，NHSO 2 R 12，COR 13，CO 2 R 14，CONR 15 R 16和SO 2 NHR 17; X表示键，C 1-6烷基链或C 3-6烯基链，其中每个链中可任选地含有一个或两个氮，氧或硫原子，并且该链任选被一个或多个基团取代选自卤素，羟基，CN，C 1-6烷基，C 1-6烷氧基，C 1-6酰氧基，NR 9 R 10，NHCOR 11，NHSO 2 R 12，COR 13，CO 2 R 14，CONR 15 R 16和SO 2 NHR 17; R9-R17表示氢，C1-6烷基或R9，R10或R15和R16形成C

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