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1. 发明申请

US20100267755A1 PYRIMIDINE DERIVATIVES 审中-公开
公开(公告)号：US20100267755A1
公开(公告)日：2010-10-21
申请号：US10477546
申请日：2002-05-23
申请人： Gianpaolo Bravi , Malcolm Clive Carter , Richard Howard Green , Jennifer Margaret Doughty , Charles David Hartley , Alan Naylor , Martin Pass , Jeremy John Payne , Neil Anthony Pegg
发明人： Gianpaolo Bravi , Malcolm Clive Carter , Richard Howard Green , Jennifer Margaret Doughty , Charles David Hartley , Alan Naylor , Martin Pass , Jeremy John Payne , Neil Anthony Pegg
IPC分类号： A61K31/505 , A61P29/00 , C07D239/42 , C07D403/12 , C07D405/12 , C07D409/12 , A61K31/506
CPC分类号： C07D239/42 , C07D401/12 , C07D405/12 , C07D409/12
摘要： The invention provides the compounds of formula (I) and pharmaceutically acceptable salts thereof, in which: R1 and R2 are independently selected from the group consisting of H, C1-6alkyl, C1-2alkyl substituted by one to five fluorine atoms, C3-6alkenyl, C3-6alkynyl, C3-10cycloalkylC0-6alkyl, C4-12bridged cycloalkyl, A(CR7R8)n and B(CR7R8)n; R3 is selected from the group consisting of C1-6alkyl, NH2 and R10CONH; R4 is C1-2alkyl substituted by one to five fluorine atoms; R5 is selected from the group consisting of H, C1-4alkyl, C1-2alkyl substituted with one to five fluorine atoms, halogen and C3-10cycloalkylC0-6alkyl, with the proviso that when R6 is H R5 is not H. R6 is selected from the group consisting of H, C1-4alkyl, C1-2alkyl substituted with one to five fluorine atoms, halogen, C1-4alkoxy, CN, NO2, C1-6alkylOCO, NH2CO, C1-6alkylNHCO, NH2, C1-6alkylNH, (C1-6alkyl)2N, (C1-6alkyl)2NCO, C1-6alkylCONH, NH2SO2, C1-6alkylNHSO2, (C1-6alkyl)2NSO2, C1-6alkylSO2NH, ArSO2NH, C1-6alkylSO2, ArSO2, C3-10cycloalkylC0-6alkyl, C3-6alkenyl and C3-6alkynyl, with the proviso that when R5 is H R6 is not H. R7 and R8 are independently selected from H or C1-6alkyl; A is an unsubstituted 5- or 6-membered heteroaryl or an unsubstituted 6-membered aryl, or a 5- or 6-membered heteroaryl or a 6-membered aryl substituted by one or more R9; R9 is selected from the group consisting of hydroxy, halogen, C1-6alkyl, C1-6alkyl substituted by one more fluorine atoms, C1-6alkoxy, C1-6alkoxy substituted by one or more F, NH2SO2 and C1-6alkylSO2; R10 is selected from the group consisting of H, C1-6alkyl, C1-6alkoxy, C1-6alkylOC1-6alkyl, phenyl, HO2CC1-6alkyl, C1-6alkylOCOC1-6alkyl, C1-6alkylOCO, H2NC1-6alkyl, C1-6alkylOCONHC1-6alkyl and C1-6alkylCONHC1-6alkyl; B is selected from the group consisting of defines the point of attachment of the ring; and n is 0 to 4. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of pain, fever and inflammation of a variety of conditions and diseases.

2. 发明授权

US07084148B2 Substituted pyrimidines as selective cyclooxygenase-2 inhibitors 失效
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：US07084148B2
公开(公告)日：2006-08-01
申请号：US10362745
申请日：2001-08-31
申请人： Malcolm Clive Carter , Alan Naylor , Martin Pass , Jeremy John Payne , Neil Anthony Pegg
发明人： Malcolm Clive Carter , Alan Naylor , Martin Pass , Jeremy John Payne , Neil Anthony Pegg
IPC分类号： C07D405/12 , A61K31/505
CPC分类号： C07D405/12
摘要： A compound of formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1 is H or C1-6alkyl; R2 is wherein defines the point of attachment of the ring; and R3 is C1-6alkyl or NH2. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of pain, fever, inflammation of a variety of conditions and diseases.
摘要翻译：式（I）化合物及其药学上可接受的衍生物，其中R 1是H或C 1-6烷基; R 2是其中限定环的连接点; R 3是C 1-6烷基或NH 2。式（I）化合物是COX-2的有效和选择性抑制剂，可用于治疗疼痛，发热，各种病症和疾病的炎症。

3. 发明授权

US06780870B2 Pyrimidine derivatives as selective inhibitors of COX-2 失效
标题翻译：嘧啶衍生物作为COX-2的选择性抑制剂
公开(公告)号：US06780870B2
公开(公告)日：2004-08-24
申请号：US10182788
申请日：2002-07-31
申请人： Malcolm Clive Carter , Alan Naylor , Jeremy John Payne , Neil Anthony Pegg
发明人： Malcolm Clive Carter , Alan Naylor , Jeremy John Payne , Neil Anthony Pegg
IPC分类号： C07D23942
CPC分类号： C07D239/42 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The invention provides the compounds of formula (I) and pharmaceutically acceptable derivatives thereof, in which: R1 and R2 are independently selected from H, or C1-6alkyl; R3 is C1-6alkyl or NH2; R4 is H or C1-6alkyl; A is a 5- or 6-membered aryl, or a 5- or 6-membered aryl substituted by one or more R5; R5 is halogen, C1-6alkyl, C1-6alkyl substituted by one ore more F, C1-6alkoxy, C1-6alkoxy substituted by one or more F, SO2NH2 or SO2C1-6alkyl; and n is 1 to 4.
摘要翻译：本发明提供式（I）化合物及其药学上可接受的衍生物，其中：R 1和R 2独立地选自H或C 1-6烷基; R 3是C 1-6烷基或NH 2; R 4是H或C 1-6烷基; A是5或6元芳基或被一个或多个R 5取代的5或6元芳基; R 5是卤素，C 1 -C 6烷基，被一个或多个F，C 1-6烷氧基，被一个或多个F，SO 2 NH 2或SO 2 C 1-6烷基取代的C 1-6烷氧基取代的C 1-6烷基; andn是1到4。

4. 发明授权

US07109333B2 Heterocyclic compounds 有权
标题翻译：杂环化合物
公开(公告)号：US07109333B2
公开(公告)日：2006-09-19
申请号：US11050033
申请日：2005-02-03
申请人： Malcolm Clive Carter , George Stuart Cockerill , Stephen Barry Guntrip , Karen Elizabeth Lackey , Kathryn Jane Smith
发明人： Malcolm Clive Carter , George Stuart Cockerill , Stephen Barry Guntrip , Karen Elizabeth Lackey , Kathryn Jane Smith
IPC分类号： C07D239/72 , A61K31/517 , A01N43/54
CPC分类号： A61K31/517 , C07D239/94 , C07D405/04 , C07D405/14 , C07D411/04 , C07D417/04 , C07D417/14 , C07D471/04
摘要： A process for the preparation of a compound of formula (I) comprising the steps: (a) reacting a compound of formula (II) wherein L and L′ are suitable leaving groups, with a compound of formula (III) UNH2 (III) to prepare a compound of formula (IV) and subsequently (b) substituting the group R1 by replacement of the leaving group L′.
摘要翻译：一种制备式（I）化合物的方法，包括步骤：（a）使其中L和L'是合适的离去基团的式（II）化合物与式（III）化合物反应， line-formula description =“In-line Formulas”end =“lead”？> UNH （III）<？in-line-formula description =“In-line Formulas”end =“tail” 制备式（IV）的化合物，随后（b）用R'取代基取代离去基团L'。

5. 发明授权

US06713485B2 Heterocyclic compounds 有权
标题翻译：杂环化合物
公开(公告)号：US06713485B2
公开(公告)日：2004-03-30
申请号：US10071358
申请日：2002-02-08
申请人： Malcolm Clive Carter , George Stuart Cockerill , Stephen Barry Guntrip , Karen Elizabeth Lackey , Kathryn Jane Smith
发明人： Malcolm Clive Carter , George Stuart Cockerill , Stephen Barry Guntrip , Karen Elizabeth Lackey , Kathryn Jane Smith
IPC分类号： A61K31517
CPC分类号： A61K31/517 , C07D239/94 , C07D405/04 , C07D405/14 , C07D411/04 , C07D417/04 , C07D417/14 , C07D471/04
摘要： The present invention relates to substituted heteroaromatic compounds, methods for their preparation, pharmaceutical compositions containing them and their use in medicine. Specifically, the invention relates to quinazoline derivatives useful in treating disorders mediated by protein tyrosine kinase activity, in particular erbB-2 and/or EGFR activity.
摘要翻译：本发明涉及取代的杂芳族化合物，其制备方法，含有它们的药物组合物及其在药物中的用途。具体地，本发明涉及可用于治疗由蛋白酪氨酸激酶活性介导的病症的喹唑啉衍生物，特别是erbB-2和/或EGFR活性。

6. 发明授权

US06727256B1 Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors 有权
公开(公告)号：US06727256B1
公开(公告)日：2004-04-27
申请号：US09582746
申请日：2000-06-30
申请人： Malcolm Clive Carter , George Stuart Cockerill , Stephen Barry Guntrip , Karen Elizabeth Lackey , Kathryn Jane Smith
发明人： Malcolm Clive Carter , George Stuart Cockerill , Stephen Barry Guntrip , Karen Elizabeth Lackey , Kathryn Jane Smith
IPC分类号： A61K31505
CPC分类号： A61K31/517 , C07D239/94 , C07D405/04 , C07D405/14 , C07D411/04 , C07D417/04 , C07D417/14 , C07D471/04
摘要： Substituted heteroaromatic compounds of formula (I), wherein X is N or CH; Y is CR1 and V is N; or Y is N and V is CR1; or Y is CR1 and V is CR2; or Y is CR2 and V is CR1; R1 represents a group CH3SO2CH2CH2NHCH2—Ar—, wherein Ar is selected from phenyl, furan, thiophene, pyrrole and thiazole, each of which may optionally be substituted by one or two halo, C1-4alkyl or C1-4alkoxy groups; R2 is selected from the group comprising hydrogen, halo, hydroxy, C1-4alkyl, C1-4alkoxy, C1-4alkylamino and di[C1-4alkyl]amino; U represents a phenyl, pyridyl, 3H-imidazolyl, indolyl, isoindolyl, indolinyl, isoindolinyl, 1H-indazolyl, 2,3-dihydro-1H-indazolyl, 1H-benzimidazolyl, 2,3-dihydro-1H-benzimidazolyl or 1H-benzotriazolyl group, substituted by an R3 group and optionally substituted by at least one independently selected R4 group; R3 is selected from a group comprising benzyl, halo-, dihalo- and trihalobenzyl, benzoyl, pyridylmethyl, pyridylmethoxy, phenoxy, benzyloxy, halo-, dihalo- and trihalobenzyloxy and benzenesulphonyl, or R3 represents trihalomethylbenzyl or trihalomethylbenzyloxy; or R3 represents a group of formula (a) wherein each R5 is independently selected from halogen, C1-4alkyl, C1-4alkoxy; and n is 0 to 3; each R4 is independently hydroxy, halogen, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4alkoxy, amino, C1-4alkylamino, di[C1-4alkyl]amino, C1-4alkylthio, C1-4alkylsulphinyl, C1-4alkylsulphonyl, C1-4alkylcarbonyl, carboxy, carbamoyl, C1-4alkoxycarbonyl, C1-4alkanoylamino, N-(C1-4alkyl)carbamoyl, N,N-di(C1-4alkyl)carbamoyl, cyano, nitro and trifluoromethyl; and salts and solvates thereof, are disclosed, as are methods for their preparation, pharmaceutical compositions containing them and their use in medicine.

7. 发明授权

US06174889B1 Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors 失效
标题翻译：双环杂芳族化合物作为蛋白酪氨酸激酶抑制剂
公开(公告)号：US06174889B1
公开(公告)日：2001-01-16
申请号：US09214270
申请日：1998-12-31
申请人： George Stuart Cockerill , Malcolm Clive Carter , Stephen Barry Guntrip , Kathryn Jane Smith
发明人： George Stuart Cockerill , Malcolm Clive Carter , Stephen Barry Guntrip , Kathryn Jane Smith
IPC分类号： A61K31519
CPC分类号： C07D493/08 , C07D209/08 , C07D231/56 , C07D235/08 , C07D401/06 , C07D407/12 , C07D471/04
摘要： Substituted heteroaromatic compounds, and in particular substituted bicyclic heteroaromatic compounds of formula (I), wherein X is N or CH; A represents a fused 5, 6 or 7-membered heterocyclic ring containing 1 to 5 heteroatoms which may be the same or different and which are selected from N, O or S(O)m, wherein m is as defined above, the heterocyclic ring containing a total of 1, 2 or 3 double bonds inclusive of the bond in the pyridine or pyrimidine ring to which it is fused, with the provisos that the heterocyclic ring does not form part of a purine and that the fused heterocyclic ring does not contain two adjacent O or S(O)m atoms. U represents a 5 to 10-membered mono or bicyclic ring system in which one or more of the carbon atoms is optionally replaced by a heteroatom independently selected from N, O and S(O)m, wherein m is 0, 1 or 2 and wherein the ring system is substituted by at least one independently selected R6 group and is optionally substituted by at least one independently selected R4 group, with the proviso that U does not represent phenyl; are protein tyrosine kinase inhibitors. The compounds are described as are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of cancer and psoriasis.
摘要翻译：取代的杂芳族化合物，特别是式（I）的取代的双环杂芳族化合物，其中X是N或CH; A表示稠合的5,6或7元杂环，其含有1至5个可以相同或不同的杂原子，并且其选自N，O或S（O）m，其中m如上定义，杂环包含总共1,2或3个双键，包括其所融合的吡啶或嘧啶环中的键，条件是杂环不形成嘌呤的一部分，并且稠合杂环不包含两个相邻的O或S（O）m原子。 U表示5至10元单或双环体系，其中一个或多个碳原子任选被独立地选自N，O和S（O）m的杂原子取代，其中m为0,1或2，以及其中所述环系被至少一个独立选择的R 6基团取代，并且任选地被至少一个独立选择的R 4基团取代，条件是U不表示苯基; 是蛋白酪氨酸激酶抑制剂。这些化合物被描述为它们的制备方法，包括这些化合物的药物组合物及其在药物中的用途，例如治疗癌症和牛皮癣。

8. 发明授权

US08513262B2 Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors 有权
标题翻译：双环杂芳族化合物作为蛋白酪氨酸激酶抑制剂
公开(公告)号：US08513262B2
公开(公告)日：2013-08-20
申请号：US12691784
申请日：2010-01-22
申请人： Malcolm Clive Carter , George Stuart Cockerill , Karen Elizabeth Lackey
发明人： Malcolm Clive Carter , George Stuart Cockerill , Karen Elizabeth Lackey
IPC分类号： A01N43/90 , A61K31/519 , C07D239/72
CPC分类号： A61K31/517 , C07D239/94 , C07D405/04 , C07D405/14 , C07D411/04 , C07D417/04 , C07D417/14 , C07D471/04
摘要： A process for the preparation of a compound of formula (I) comprising the steps: (a) reacting a compound of formula (II) wherein L and L′ are suitable leaving groups, with a compound of formula (III) UNH2 (III) to prepare a compound of formula (IV) and subsequently (b) substituting the group R1 by replacement of the leaving group L′.
摘要翻译：一种制备式（I）化合物的方法，包括以下步骤：（a）将其中L和L'是合适的离去基团的式（II）化合物与式（III）化合物UNH2（III）制备式（Ⅳ）化合物，随后（b）用置换基团L'代替基团R 1。

9. 发明授权

US06828320B2 Heterocyclic compounds 有权
标题翻译：杂环化合物
公开(公告)号：US06828320B2
公开(公告)日：2004-12-07
申请号：US10062647
申请日：2002-01-31
申请人： George Stuart Cockerill , Malcolm Clive Carter , Stephen Barry Guntrip , Kathryn Jane Smith
发明人： George Stuart Cockerill , Malcolm Clive Carter , Stephen Barry Guntrip , Kathryn Jane Smith
IPC分类号： A61K31535
CPC分类号： C07D401/04 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D413/14
摘要： Substituted heteroaromatic compounds, and in particular substituted quinolines and quinazolines, are protein tyrosine kinase inhibitors. The compounds are described as are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of cancer and psoriasis.
摘要翻译：取代的杂芳族化合物，特别是取代的喹啉和喹唑啉是蛋白质酪氨酸激酶抑制剂。这些化合物被描述为它们的制备方法，包括这些化合物的药物组合物及其在药物中的用途，例如治疗癌症和牛皮癣。

10. 发明授权

US06723726B1 Protein tyrosine kinase inhibitors 失效
标题翻译：蛋白酪氨酸激酶抑制剂
公开(公告)号：US06723726B1
公开(公告)日：2004-04-20
申请号：US09608971
申请日：2000-06-30
申请人： George Stuart Cockerill , Malcolm Clive Carter , Stephen Barry Guntrip , Kathryn Jane Smith
发明人： George Stuart Cockerill , Malcolm Clive Carter , Stephen Barry Guntrip , Kathryn Jane Smith
IPC分类号： A61K31519
CPC分类号： C07D493/08 , C07D209/08 , C07D231/56 , C07D235/08 , C07D401/06 , C07D407/12 , C07D471/04
摘要： Substituted heteroaromatic compounds, and in particular substituted bicyclic heteroaromatic compounds of formula (I), wherein X is N or CH; A represents a fused 5, 6 or 7-membered heterocyclic ring containing 1 to 5 heteroatoms which may be the same or different and which are selected from N, O or S(O)m, wherein m is as defined above, the heterocyclic ring containing a total of 1, 2 or 3 double bonds inclusive of the bond in the pyridine or pyrimidine ring to which it is fused, with the provisos that the heterocyclic ring does not form part of a purine and that the fused heterocyclic ring does not contain two adjacent O or S(O)m atoms. U represents a 5 to 10-membered mono or bicyclic ring system in which one or more of the carbon atoms is optionally replaced by a heteroatom independently selected from N, O and S(O)m, wherein m is 0,1 or 2 and wherein the ring system is substituted by at least one independently selected R6 group and is optionally substituted by at least one independently selected R4 group, with the proviso that U does not represent phenyl; are protein tyrosine kinase inhibitors. The compounds are described as are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of cancer and psoriasis.
摘要翻译：取代的杂芳族化合物，特别是式（I）的取代的双环杂芳族化合物，其中X是N或CH; A表示稠合的5,6或7元杂环，其含有1至5个可以相同或不同的杂原子，并且其选自N，O或S（O）m，其中m如上定义，杂环包含总共1,2或3个双键，包括其所融合的吡啶或嘧啶环中的键，条件是杂环不形成嘌呤的一部分，并且稠合杂环不包含两个相邻的O或S（O）m原子。 U表示5至10元单环或双环系，其中一个或多个碳原子任选被独立地选自N，O和S（O）m的杂原子取代，其中m为0,1或2，以及其中所述环系被至少一个独立选择的R 6基团取代，并且任选地被至少一个独立选择的R 4基团取代，条件是U不表示苯基; 是蛋白酪氨酸激酶抑制剂。这些化合物被描述为它们的制备方法，包括这些化合物的药物组合物及其在药物中的用途，例如治疗癌症和牛皮癣。

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