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1. 发明授权

US08318935B2 Organic compounds 75074 有权
标题翻译：有机化合物75074
公开(公告)号：US08318935B2
公开(公告)日：2012-11-27
申请号：US12451152
申请日：2008-05-05
申请人： Robin Alec Fairhurst , Rebecca Butler , Paul Oakley , Stephen Paul Collingwood , Nichola Smith , Emily Stanley , Maria Ines Rodriguez Perez
发明人： Robin Alec Fairhurst , Rebecca Butler , Paul Oakley , Stephen Paul Collingwood , Nichola Smith , Emily Stanley , Maria Ines Rodriguez Perez
IPC分类号： C07D401/14 , A61K31/497 , A61P11/06
CPC分类号： C07D401/14
摘要： A compound of formula (I), or tautomers, or stereoisomers, or solvates, or pharmaceutically acceptable salts thereof, wherein M1, M2, L1, L2, W1, W2, X1, X2, Y1, Y2, A, R5 and R5a are as defined herein for the for treatment of conditions treatable by the blockade of an epithelial sodium channel, particularly conditions benefiting from mucosal hydration.
摘要翻译：其中M1，M2，L1，L2，W1，W2，X1，X2，Y1，Y2，A，R5和R5a为式（I）化合物或其互变异构体或立体异构体或溶剂合物或其药学上可接受的盐如本文所定义的用于治疗可通过阻断上皮钠通道治疗的病症，特别是有益于粘膜水合的病症。

2. 发明申请

US20100105660A1 ORGANIC COMPOUNDS75074 有权
标题翻译：有机化合物75074
公开(公告)号：US20100105660A1
公开(公告)日：2010-04-29
申请号：US12451152
申请日：2008-05-05
申请人： Robin Alec Fairhurst , Rebecca Fraser , Paul Oakley , Stephen Paul Collingwood , Nichola Smith , Emily Stanley , Maria Ines Rodriguez Perez
发明人： Robin Alec Fairhurst , Rebecca Fraser , Paul Oakley , Stephen Paul Collingwood , Nichola Smith , Emily Stanley , Maria Ines Rodriguez Perez
IPC分类号： A61K31/55 , C07D401/14 , C07D413/14 , A61K31/5377 , A61K31/53 , A61K31/497 , A61P37/08 , A61P11/00
CPC分类号： C07D401/14
摘要： A compound of formula (I), or tautomers, or stereoisomers, or solvates, or pharmaceutically acceptable salts thereof, wherein M1, M2, L1, L2, W1, W2, X1, X2, Y1, Y2, A, R5 and R5a are as defined herein for the for treatment of conditions treatable by the blockade of an epithelial sodium channel, particularly conditions benefiting from mucosal hydration.
摘要翻译：其中M1，M2，L1，L2，W1，W2，X1，X2，Y1，Y2，A，R5和R5a为式（I）化合物或其互变异构体或立体异构体或溶剂合物或其药学上可接受的盐如本文所定义的用于治疗可通过阻断上皮钠通道治疗的病症，特别是有益于粘膜水合的病症。

3. 发明申请

US20090264459A1 Organic Compounds 审中-公开
标题翻译：有机化合物
公开(公告)号：US20090264459A1
公开(公告)日：2009-10-22
申请号：US12308231
申请日：2007-06-28
申请人： Stephen Paul Collingwood , Robin Alec Fairhurst , Neil John Press
发明人： Stephen Paul Collingwood , Robin Alec Fairhurst , Neil John Press
IPC分类号： A61K31/4375 , C07D471/04 , C07D417/14 , C07D417/12 , A61K31/454 , A61K31/428 , A61P11/00
CPC分类号： C07D471/04 , C07D277/68 , C07D417/14
摘要： Compounds of formula (I) in free or a pharmaceutically acceptable salt form, wherein X1, L and Q have the meanings as indicated in the specification, are useful for treating obstructive or inflammatory airways diseases. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
摘要翻译：游离的或其药学上可接受的盐形式的式（I）化合物，其中X1，L和Q具有说明书中指出的含义，可用于治疗阻塞性或炎症性气道疾病。还描述了含有化合物的药物组合物和用于制备化合物的方法。

4. 发明授权

US06919337B2 8-Quinolinxanthine and 8-isoquinolinxanthine derivatives as PDE 5 inhibitors 失效
标题翻译： 8-喹啉黄嘌呤和8-异喹啉黄嘌呤衍生物作为PDE 5抑制剂
公开(公告)号：US06919337B2
公开(公告)日：2005-07-19
申请号：US10644328
申请日：2003-08-20
申请人： Gurdip Bhalay , Stephen Paul Collingwood , Robin Alec Fairhurst , Sylvie Felicite Gomez , Ret Naef , David Andrew Sandham
发明人： Gurdip Bhalay , Stephen Paul Collingwood , Robin Alec Fairhurst , Sylvie Felicite Gomez , Ret Naef , David Andrew Sandham
IPC分类号： C07D473/04 , C07D473/06 , A61K31/5355 , A61P15/10 , C07D473/02
CPC分类号： C07D473/04 , C07D473/06
摘要： A compound of formula (I) R1 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R2 is hydrogen, alkyl, hydroxyalkyl, alkylcarbonyloxyalkyl, alkoxyalkyl, alkylthioalkyl, alkenyl, cycloalkylalkyl, heterocyclylalkyl, aralkyl in which the aryl ring thereof is optionally fused to a 5-membered heterocyclic group or is optionally substituted by one or more substituents selected from alkoxy, amino, alkylamino, dialkylamino, acylamino, halogen, hydroxy, aminosulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl, alkylsulfonylamino or dialkylaminosulfonylamino, R3 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R4 is hydrogen or alkyl, R5 is a quinolinyl, isoquinolinyl or oxodihydroisoquinolinyl group optionally fused to a 5-membered heterocyclic group and optionally substituted by one or more substituents selected from halogen, cyano, hydroxy, alkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxy, alkylthio, alkenyl, alkoxycarbonyl, alkynyl, carboxyl, acyl, a group of formula —N(R6)R7, aryl optionally substituted by one or more substituents selected from halogen or alkoxy, or heteroaryl having 5 or 6 ring atoms attached through a ring carbon atom to the indicated carbon atom, and R6 and R7 are each independently hydrogen or alkyl optionally substituted by hydroxy or alkoxy or one of R6 and R7 is hydrogen and the other is acyl, or R6 and R7 together with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclyl group.
摘要翻译：式（I）R 1的化合物是氢或任选被羟基，烷氧基或烷硫基取代的烷基，R 2是氢，烷基，羟基烷基，烷基羰氧基烷基，烷氧基烷基，烷基硫代烷基，烯基，环烷基烷基，杂环基烷基，芳烷基，其中其芳基环任选地与5元杂环基稠合，或任选被一个或多个选自烷氧基，氨基，烷基氨基，二烷基氨基，酰氨基，卤素，羟基，氨基磺酰基，烷基氨基磺酰基，二烷基氨基磺酰基，烷基磺酰基氨基或二烷基氨基磺酰基氨基，R 3是氢或任选被羟基，烷氧基或烷硫基取代的烷基，R 4是氢或烷基，R 0 任选地与5元杂环基稠合并且任选地被一个或多个选自卤素，氰基，羟基，烷基，羟基烷基，烷氧基烷基，烷硫基的取代基取代的喹啉基，异喹啉基或氧代二氢异喹啉基烷基，烷氧基，烷硫基，烯基，烷氧基羰基，炔基，羧基，酰基，式-N（R 6）R 7的基团，任选地被一个或多个选自卤素或烷氧基的取代基或具有5或6个环原子通过环碳原子连接到指定碳原子的杂芳基，R 6和R 7各自独立地任选被羟基或烷氧基取代的氢或烷基或R 6和R 7中的一个是氢，另一个是酰基或R 6和 R 7与它们所连接的氮原子一起表示5-或6-元杂环基。

5. 发明授权

US6087490A Dinucleotide and oligonucleotide analogues 失效
标题翻译：二核苷酸和寡核苷酸类似物
公开(公告)号：US6087490A
公开(公告)日：2000-07-11
申请号：US155198
申请日：1998-10-08
申请人： Anthony David Baxter , Eric Keith Baylis , Stephen Paul Collingwood , Robin Alec Fairhurst , Roger John Taylor
发明人： Anthony David Baxter , Eric Keith Baylis , Stephen Paul Collingwood , Robin Alec Fairhurst , Roger John Taylor
IPC分类号： C07H19/06 , C07H21/00 , C07H19/00 , C07H21/02 , C07H21/04
CPC分类号： C07H19/06 , C07H21/00 , Y02P20/55
摘要： A compound which is a dinucleotide analogue of formula ##STR1## or a salt thereof, where B.sup.1 and B.sup.2 are each independently a monovalent nucleoside base radical,R.sup.1 is hydrogen or Y.sup.1,R.sup.2 and R.sup.3 are each independently hydrogen, halogen, hydroxy or --OY.sup.2,R.sup.4 is hydrogen, halogen, hydroxy, --OY.sup.3 or R.sup.7,R.sup.5 is hydrogen, halogen or R.sup.8,R.sup.6 is hydrogen, Y.sup.4 or a phosphoramidyl group,Z is a group of formula II, III or IV ##STR2## where R.sup.9 is hydrogen, halogen, hydroxy, --OY.sup.5 or R.sup.13, R.sup.10 is hydrogen, halogen or R.sup.14, R.sup.11 is hydroxy, R.sup.15 or --OR.sup.15 where R.sup.15 is a C.sub.1 to C.sub.10 aliphatic group, a C.sub.3 to C.sub.8 cycloaliphatic group, a C.sub.6 to C.sub.10 aromatic group or a C.sub.7 to C.sub.13 araliphatic group, and R.sup.12 is hydrogen, R.sup.12.sub.a or --OCOR.sup.12.sub.a where R.sup.12.sub.a is a C.sub.1 to C.sub.10 aliphatic group, a C.sub.3 to C.sub.8 cycloaliphatic group, a C.sub.6 to C.sub.10 aromatic group or a C.sub.7 to C.sub.13 araliphatic group, Y.sup.1, Y.sup.2, Y.sup.3, Y.sup.4 and Y.sup.5 are each indpendently a hydroxy-protecting group, and R.sup.7, R.sup.8, R.sup.13 and R.sup.14 are each independently a C.sub.1 to C.sub.10 aliphatic group, a C.sub.3 to C.sub.8 cycloaliphatic group, a C.sub.6 to C.sub.10 aromatic group or a C.sub.7 to C.sub.13 araliphatic group.
摘要翻译： PCT No.PCT / GB97 / 00651 Sec。 371日期：1998年10月8日 102（e）日期1998年10月8日PCT 1997年11月3日PCT PCT。公开号WO97 / 35869 日期1997年10月2日为式或二价核苷酸类似物的化合物或其盐，其中B1和B2各自独立地为一价核苷碱基，R1为氢或Y1，R2和R3各自独立地为氢，卤素，羟基或 -OY2，R4是氢，卤素，羟基，-OY3或R7，R5是氢，卤素或R8，R6是氢，Y4或磷酰胺基，Z是式II，III或IV的基团，其中R9是氢，卤素，羟基，-OY5或R13，R10为氢，卤素或R14，R11为羟基，R15或-OR15，其中R15为C1至C10脂族基团，C3至C8脂环族基团，C6至C10芳族基团或 C7至C13芳脂族基团，R12为氢，R12a或-OCOR12a，其中R12a为C1至C10脂族基团，C3至C8脂环族基团，C6至C10芳族基团或C7至C13芳脂族基团，Y1，Y2， Y3，Y4和Y5各自独立地为羟基保护基，R7，R8，R13和R14各自独立地为C1至C10脂族基团，C3t C 8脂环族基团，C 6至C 10芳族基团或C 7至C 13芳脂基基团。

6. 发明授权

US07019136B2 8-quinolinxanthine and 8-isoquinolinxanthine derivatives as PDE 5 inhibitors 失效
标题翻译： 8-喹啉黄嘌呤和8-异喹啉黄嘌呤衍生物作为PDE 5抑制剂
公开(公告)号：US07019136B2
公开(公告)日：2006-03-28
申请号：US10937639
申请日：2004-09-09
申请人： Gurdip Bhalay , Stephen Paul Collingwood , Robin Alec Fairhurst , Sylvie Felicite Gomez , Reto Naef , David Andrew Sandham
发明人： Gurdip Bhalay , Stephen Paul Collingwood , Robin Alec Fairhurst , Sylvie Felicite Gomez , Reto Naef , David Andrew Sandham
IPC分类号： C07D239/02
CPC分类号： C07D239/545 , A61K31/522 , C07D473/04 , C07D473/06
摘要： A compound of formula (I): R1 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R2 is hydrogen, alkyl, hydroxyalkyl, alkylcarbonyloxyalkyl, alkoxyalkyl, alkylthioalkyl, alkenyl, cycloalkylalkyl, heterocyclylalkyl, aralkyl in which the aryl ring thereof is optionally fused to a 5-membered heterocyclic group or is optionally substituted by one or more substituents selected from alkoxy, amino, alkylamino, dialkylamino, acylamino, halogen, hydroxy, aminosulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl, alkylsulfonylamino or dialkylaminosulfonylamino, R3 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R4 is hydrogen or alkyl, R5 is a quinolinyl, isoquinolinyl or oxodihydroisoquinolinyl group optionally fused to a 5-membered heterocyclic group and optionally substituted by one or more substituents selected from halogen, cyano, hydroxy, alkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxy, alkylthio, alkenyl, alkoxycarbonyl, alkynyl, carboxyl, acyl, a group of formula —N(R6)R7, aryl optionally substituted by one or more substituents selected from halogen or alkoxy, or heteroaryl having 5 or 6 ring atoms attached through a ring carbon atom to the indicated carbon atom, and R6 and R7 are each independently hydrogen or alkyl optionally substituted by hydroxy or alkoxy or one of R6 and R7 is hydrogen and the other is acyl, or R6 and R7 together with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclyl group.
摘要翻译：式（I）化合物：R 1是氢或任选被羟基，烷氧基或烷硫基取代的烷基，R 2是氢，烷基，羟基烷基，烷基羰氧基烷基，烷氧基烷基，烷基硫代烷基，烯基，环烷基烷基，杂环基烷基，芳烷基，其中其芳基环任选地与5元杂环基稠合，或任选地被一个或多个选自烷氧基，氨基，烷基氨基，二烷基氨基，酰氨基，卤素，羟基，氨基磺酰基，烷基氨基磺酰基，二烷基氨基磺酰基，烷基磺酰基氨基或二烷基氨基磺酰基氨基，R 3是氢或任选被羟基，烷氧基或烷硫基取代的烷基，R 4是氢或烷基，任选地与5元杂环基稠合的喹啉基，异喹啉基或氧代二氢异喹啉基，任选地被一个或多个选自卤素，氰基，羟基，烷基，羟烷基，烷氧基烷基，烷硫基烷基，烷氧基，烷硫基，烯基，烷氧基羰基，炔基，羧基，酰基，式-N（R 6）R 7的基团，任选地被一个或多个选自卤素或烷氧基的取代基或具有5或6个环原子通过环碳原子连接到指定碳原子的杂芳基，R 6和R 7各自独立地任选被羟基或烷氧基取代的氢或烷基或R 6和R 7中的一个是氢，另一个是酰基或R 6和 R 7与它们所连接的氮原子一起表示5-或6-元杂环基。

7. 发明授权

US10189813B2 Formylated N-heterocyclic derivatives as FGFR4 inhibitors 有权
公开(公告)号：US10189813B2
公开(公告)日：2019-01-29
申请号：US15561189
申请日：2016-03-23
申请人： Nicole Buschmann , Robin Alec Fairhurst , Pascal Furet , Thomas Knoepfel , Catherine Leblanc , Robert Mah
发明人： Nicole Buschmann , Robin Alec Fairhurst , Pascal Furet , Thomas Knoepfel , Catherine Leblanc , Robert Mah
IPC分类号： C07D401/12 , C07D401/14 , A61K31/4427 , C07D213/75 , C07D405/14
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.

8. 发明申请

US20180064709A1 PHARMACEUTICAL COMBINATIONS 审中-公开
公开(公告)号：US20180064709A1
公开(公告)日：2018-03-08
申请号：US15561209
申请日：2016-03-23
申请人： Nicole Buschmann , Robin Alec Fairhurst , Jorge Garcia Fortanet , Pascal Furet , Diana Graus Porta , Nafeeza Hafeez , Bo Han , Thomas Knoepfel , Matthew J. LaMarche , Catherine Leblanc
发明人： Nicole Buschmann , Robin Alec Fairhurst , Jorge Garcia Fortanet , Pascal Furet , Diana Graus Porta , Nafeeza Hafeez , Bo Han , Thomas Knoepfel , Matthew J. LaMarche , Catherine Leblanc
IPC分类号： A61K31/496 , A61K31/497
CPC分类号： A61K31/496 , A61K31/4439 , A61K31/497 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K2300/00
摘要： A pharmaceutical combination comprising N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide, or a pharmaceutically acceptable salt thereof, and at least one active ingredient, as defined herein, or a pharmaceutically acceptable salt thereof, and optionally a pharmaceutically acceptable carrier, for simultaneous or sequential administration; the uses of such combination in the treatment of proliferative diseases; and methods of treating a subject suffering from a proliferative disease comprising administering a therapeutically effective amount of such combination.

9. 发明授权

US09802917B2 Particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide 有权
公开(公告)号：US09802917B2
公开(公告)日：2017-10-31
申请号：US15073766
申请日：2016-03-18
申请人： Nicole Buschmann , Robin Alec Fairhurst , Pascal Furet , Bo Han , Thomas Knöpfel , Catherine Leblanc , Lv Liao , Robert Mah , Franck Mallet , Julie Martz , Can Wang , Jing Xiong , Xianglin Zhao
发明人： Nicole Buschmann , Robin Alec Fairhurst , Pascal Furet , Bo Han , Thomas Knöpfel , Catherine Leblanc , Lv Liao , Robert Mah , Franck Mallet , Julie Martz , Can Wang , Jing Xiong , Xianglin Zhao
IPC分类号： A61K31/496 , C07D471/04 , C07D401/14 , C07C51/41 , C07C59/265
CPC分类号： C07D401/14 , C07B2200/13 , C07C51/412 , C07C59/265 , C07D471/04
摘要： The present invention relates to particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide, to a process of making said particles, to pharmaceutical compositions comprising said particles and to method of treating cancers using said pharmaceutical compositions.

10. 发明授权

US08940771B2 Organic compounds 有权
标题翻译：有机化合物
公开(公告)号：US08940771B2
公开(公告)日：2015-01-27
申请号：US12338432
申请日：2008-12-18
申请人： Giorgio Caravatti , Robin Alec Fairhurst , Pascal Furet , Vito Guagnano , Patricia Imbach
发明人： Giorgio Caravatti , Robin Alec Fairhurst , Pascal Furet , Vito Guagnano , Patricia Imbach
IPC分类号： A61K31/4439 , A61K31/427 , C07D417/14 , C07D417/12
CPC分类号： C07D417/14 , A61K31/427 , A61K31/4439 , C07D417/12
摘要： The present invention relates to compounds of formula I and its salts, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.
摘要翻译：本发明涉及式I化合物及其盐，其中取代基如说明书中所定义，化合物在治疗通过抑制磷脂酰肌醇3-激酶而变性的疾病中的组合物和用途。

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