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1. 发明授权

US06420438B1 1-amino-7-isoquinoline derivatives as serine protease inhibitors 失效
标题翻译： 1-氨基-7-异喹啉衍生物作为丝氨酸蛋白酶抑制剂
公开(公告)号：US06420438B1
公开(公告)日：2002-07-16
申请号：US09865418
申请日：2001-05-29
申请人： John Walter Liebeschuetz , William Alexander Wylie , Bohdan Waszkowycz , Christopher William Murray , Andrew David Rimmer , Pauline Mary Welsh , Stuart Donald Jones , Jonathan Michael Ernest Roscoe , Stephen Clinton Young , Phillip John Morgan , Nicholas Paul Camp , Andrew Philip Austin Crew
发明人： John Walter Liebeschuetz , William Alexander Wylie , Bohdan Waszkowycz , Christopher William Murray , Andrew David Rimmer , Pauline Mary Welsh , Stuart Donald Jones , Jonathan Michael Ernest Roscoe , Stephen Clinton Young , Phillip John Morgan , Nicholas Paul Camp , Andrew Philip Austin Crew
IPC分类号： A61K4360
CPC分类号： C07D401/12 , A61K38/00 , C07D217/22 , C07D217/24 , C07D401/14 , C07D405/12 , C07D409/14 , C07K5/0207
摘要： The invention relates to serine protease inhibitor compounds of formula (I) where R1 is hydrogen, halo, cyano, nitro or hydroxyl, amino, alkoxy, alkyl, aminoalkyl, hydroxyalkyl, thiol, alkylthio, aminosulphonyl, alkoxyalkyl, alkoxycarbonyl, acyloxymethoxycarbonyl or alkylamino optionally substituted by hydroxy, alkylamino, alkoxy, oxo, aryl, cycloalkyl, amino, halo, cyano, nitro, thiol, alkylthio, alkylsulphonyl, alkylsulphenyl, alkylsulphonamido, alkylaminosulphonyl, haloalkoxy and haloalkyl; R2 is hydrogen, halo, methyl, amino, hydroxy, or oxo; and R is X—X—Y(R7)—L—Lp(D)n; wherein each X independently is C, N, O or S atom or a CO, CR1, C(R1)2 or NR1 group, at least one X being C, CO, CR1 or a C(R1)2 group; Y (the &agr;-atom) is a nitrogen atom or a CR1 group or Y and L taken together form a cyclic group; R7 is a lipophilic group selected from alkyl, alkenyl, mono- or bi-cycloalkyl, aryl, heteroaryl, mono- or bicycloalkylalkyl, mono- or bicycloalkylalkenyl, aralkyl, heteroaryl-alkyl, arylalkenyl, heteroarylalkenyl all optionally substituted by a group R1; L is an organic linker group containing 1 to 5 backbone atoms selected from C, N, O and S, or a branched alkyl or cyclic group; Lp is a lipophilic organic group selected from alkyl, heterocyclic, alkenyl, alkaryl, cycloalkyl, polycycloalkyl, cycloalkenyl, aryl, aralkyl or haloalkyl group or a combination of two or more such groups optionally substituted by one or more of oxa, thia, aza or R1 groups; D is a hydrogen bond donor group; and n is 0, 1 or 2 and salts thereof.
摘要翻译：本发明涉及式（I）的丝氨酸蛋白酶抑制剂化合物，其中R1是氢，卤素，氰基，硝基或羟基，氨基，烷氧基，烷基，氨基烷基，羟基烷基，硫醇，烷硫基，氨基磺酰基，烷氧基烷基，烷氧基羰基，酰氧基甲氧基羰基或烷基氨基被羟基，烷基氨基，烷氧基，氧代，芳基，环烷基，氨基，卤素，氰基，硝基，硫醇，烷硫基，烷基磺酰基，烷基亚磺酰基，烷基磺酰氨基，烷基氨基磺酰基，卤代烷氧基和卤代烷基取代。 R2是氢，卤素，甲基，氨基，羟基或氧代; R为X-X-Y（R7）-L-Lp（D）n; 其中每个X独立地为C，N，O或S原子或CO，CR1，C（R1）2或NR1基团，至少一个X为C，CO，CR1或C（R1）2基团; Y（α原子）是氮原子或CR 1基，Y或L一起形成环状基团; R 7是选自烷基，烯基，单 - 或双 - 环烷基，芳基，杂芳基，单 - 或双环烷基烷基，单或双环烷基烯基，芳烷基，杂芳基 - 烷基，芳基烯基，杂芳基烯基的亲油基团，全部任选被基团R 1取代; L是含有1至5个选自C，N，O和S的骨架原子或支链烷基或环状基团的有机连接基团; Lp是选自烷基，杂环，烯基，烷芳基，环烷基，多环烷基，环烯基，芳基，芳烷基或卤代烷基中的亲脂性有机基团或两个或更多个这样的基团的组合，其任选被一个或多个氧杂，硫杂，氮杂或 R1组; D是氢键供体基团; 和n为0,1或2及其盐。

2. 发明授权

US07220781B2 Meta-benzamidine derivatives as serine protease inhibitors 失效
公开(公告)号：US07220781B2
公开(公告)日：2007-05-22
申请号：US10752568
申请日：2004-01-08
申请人： John Walter Liebeschuetz , William Alexander Wylie , Bohdan Waszkowycz , Christopher William Murray , Andrew David Rimmer , Pauline Mary Welsh , Stuart Donald Jones , Jonathan Michael Ernest Roscoe , Stephen Clinton Young , Phillip John Morgan
发明人： John Walter Liebeschuetz , William Alexander Wylie , Bohdan Waszkowycz , Christopher William Murray , Andrew David Rimmer , Pauline Mary Welsh , Stuart Donald Jones , Jonathan Michael Ernest Roscoe , Stephen Clinton Young , Phillip John Morgan
IPC分类号： A01N37/52
CPC分类号： C07K5/0207 , A61K38/00 , C07C237/36 , C07C255/60 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/42 , C07D209/08 , C07D209/30 , C07D209/34 , C07D209/42 , C07D211/26 , C07D211/34 , C07D211/46 , C07D211/60 , C07D213/53 , C07D213/74 , C07D213/82 , C07D215/38 , C07D217/04 , C07D217/06 , C07D217/22 , C07D217/24 , C07D231/56 , C07D235/06 , C07D241/24 , C07D277/28 , C07D277/46 , C07D277/64 , C07D277/82 , C07D295/135 , C07D295/185 , C07D317/68 , C07D333/38 , C07D333/68 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/06 , C07D487/04
摘要： Compounds of formula I in which R1, R2, R3, each X, L, Y, Cy, Lp, D and n have the meanings as set out in the specification, and corresponding compounds in which the unsubstituted or substituted amidine group is replaced with an unsubstituted or substituted aminomethyl group, are useful as serine protease inhibitors.

3. 发明授权

US07928137B2 Meta-benzamidine derivatives as serine protease inhibitors 失效
标题翻译：元 - 苯甲脒衍生物作为丝氨酸蛋白酶抑制剂
公开(公告)号：US07928137B2
公开(公告)日：2011-04-19
申请号：US11712906
申请日：2007-03-02
申请人： John Walter Liebeschuetz , William Alexander Wylie , Bohdan Waszkowycz , Christopher William Murray , Andrew David Rimmer , Pauline Mary Welsh , Stuart Donald Jones , Jonathan Michael Ernest Roscoe , Stephen Clinton Young , Phillip John Morgan
发明人： John Walter Liebeschuetz , William Alexander Wylie , Bohdan Waszkowycz , Christopher William Murray , Andrew David Rimmer , Pauline Mary Welsh , Stuart Donald Jones , Jonathan Michael Ernest Roscoe , Stephen Clinton Young , Phillip John Morgan
IPC分类号： A61K31/404 , C07D333/10
CPC分类号： C07K5/0207 , A61K38/00 , C07C237/36 , C07C255/60 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/42 , C07D209/08 , C07D209/30 , C07D209/34 , C07D209/42 , C07D211/26 , C07D211/34 , C07D211/46 , C07D211/60 , C07D213/53 , C07D213/74 , C07D213/82 , C07D215/38 , C07D217/04 , C07D217/06 , C07D217/22 , C07D217/24 , C07D231/56 , C07D235/06 , C07D241/24 , C07D277/28 , C07D277/46 , C07D277/64 , C07D277/82 , C07D295/135 , C07D295/185 , C07D317/68 , C07D333/38 , C07D333/68 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/06 , C07D487/04
摘要： Compounds of formula I in which R1, R2, R3, each X, L, Y, Cy, Lp, D and n have the meanings as set out in the specification, and corresponding compounds in which the unsubstituted or substituted amidine group is replaced with an unsubstituted or substituted aminomethyl group, are useful as serine protease inhibitors.
摘要翻译：其中R 1，R 2，R 3，各X，L，Y，Cy，Lp，D和n具有本说明书中所述的含义的式Ⅰ化合物，其中未取代或取代的脒基被替换为未取代或取代的氨基甲基可用作丝氨酸蛋白酶抑制剂。

4. 发明授权

US06262069B1 1-amino-7-isoquinoline derivatives as serine protease inhibitors 失效
标题翻译： 1-氨基-7-异喹啉衍生物作为丝氨酸蛋白酶抑制剂
公开(公告)号：US06262069B1
公开(公告)日：2001-07-17
申请号：US09485677
申请日：2000-02-25
申请人： John Walter Liebeschuetz , William Alexander Wylie , Bohdan Waszkowycz , Christopher William Murray , Andrew David Rimmer , Pauline Mary Welsh , Stuart Donald Jones , Jonathan Michael Ernest Roscoe , Stephan Clinton Young , Phillip John Morgan , Nicholas Paul Camp , Andrew Philip Austin Crew
发明人： John Walter Liebeschuetz , William Alexander Wylie , Bohdan Waszkowycz , Christopher William Murray , Andrew David Rimmer , Pauline Mary Welsh , Stuart Donald Jones , Jonathan Michael Ernest Roscoe , Stephan Clinton Young , Phillip John Morgan , Nicholas Paul Camp , Andrew Philip Austin Crew
IPC分类号： A61K3147
CPC分类号： C07D401/12 , A61K38/00 , C07D217/22 , C07D217/24 , C07D401/14 , C07D405/12 , C07D409/14 , C07K5/0207
摘要： The invention relates to serine protease inhibitor compounds of fornula (I) where R1 is hydrogen, halo, cyano, nitro or hydroxyl, amino, alkoxy, alkyl amminoalkyl, hydroxyalkyl, thiol, alkylthio, aminosulphonyl alkoxyalkyl, alkoxycarbonyl, acyloxymethoxycabonyl or alkylamino optionally substituted by hydroxy, alkylamino, alkoxy, oxo, aryl, cycloalkyl, amino, halo, cyano, nitro, thiol, alkylthio, alkylsulphonyl, alkylsulphenyl, alkylsulphonamido, alkylaminosulphonyl, haloalkoxy and haloalkyl; R2 is hydrogen, halo, methyl amino, hydroxy, or oxo; and R is X—X—Y(R7)—L—Lp(D)n; wheren each X independently is a C, N, O or S atom or a CO, CR1, C(R1)2 or NR1 group, at least one X being C, CO, CR1 or a C(R1)2 group; Y (the &agr;-atom) is a nitrogen atom or a CR1 group or Y and L taken together form a cyclic group; R7 is a lipophilic group selected from alkyl, alkenyl, mono- or bi-cycloalkyl, aryl, heteroaryl, mono- or bicycloalkylalkyl, mono- or bicycloalkylakenyl, aralkyl, heteroaryl-alkyl, arylalkenyl, heteroarylalkenyl all optionally substituted by a group R1; L is an organic linker group containing 1 to 5 backbone atoms selected from C, N, O and S, or a branched alkyl or cyclic group; Lp is a lipophilic organic group selected from alkyl, heterocyclic, alkenyl, alkaryl cycloalkyl, polycycloalkyl, cycloalkenyl, aryl, aralkyl or haloalkyl group or a combination of two or more such groups optionally substituted by one or more of oxa, thia, aza or R1 groups; D is a hydrogen bond donor group; and n is 0, 1 or 2 and salts thereof.

5. 发明授权

US08653089B2 Heterocyclic compounds and methods of use 失效
标题翻译：杂环化合物和使用方法
公开(公告)号：US08653089B2
公开(公告)日：2014-02-18
申请号：US13369016
申请日：2012-02-08
申请人： Robert Heald , Stephen Price , Brian Safina , Pascal Pierre Alexandre Savy , Eileen Mary Seward , Daniel P. Sutherlin , Bohdan Waszkowycz
发明人： Robert Heald , Stephen Price , Brian Safina , Pascal Pierre Alexandre Savy , Eileen Mary Seward , Daniel P. Sutherlin , Bohdan Waszkowycz
IPC分类号： A61K31/52 , C07D473/00
CPC分类号： C07D473/34 , A61K31/519 , A61K31/52 , A61K31/5377 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D471/04 , C07D473/16 , C07D473/32 , C07D473/40 , C07D487/04 , C07D495/04 , C07D498/06 , C07D513/04 , C07D519/00
摘要： Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译：式I化合物，包括立体异构体，几何异构体，互变异构体，代谢物及其药学上可接受的盐，可用于抑制PI3K的δ同种型，以及用于治疗由脂质激酶如炎症，免疫学障碍和癌症介导的病症。公开了使用式I化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

6. 发明授权

US08461328B2 Tricyclic heterocyclic compounds, compositions and methods of use thereof 失效
标题翻译：三环杂环化合物，其组合物及其使用方法
公开(公告)号：US08461328B2
公开(公告)日：2013-06-11
申请号：US13004808
申请日：2011-01-11
申请人： Srinivasan Babu , Phillippe Bergeron , Peter Dragovich , Hazel Joan Dyke , Paul Gibbons , Stefan Gradl , Emily Hanan , Christopher Hurley , Tony Johnson , Michael Koehler , Janusz Kulagowski , Sharada Labadie , Joseph Lyssikatos , Rohan Mendonca , Rebecca Pulk , Stuart Ward , Bohdan Waszkowycz , Mark Zak
发明人： Srinivasan Babu , Phillippe Bergeron , Peter Dragovich , Hazel Joan Dyke , Paul Gibbons , Stefan Gradl , Emily Hanan , Christopher Hurley , Tony Johnson , Michael Koehler , Janusz Kulagowski , Sharada Labadie , Joseph Lyssikatos , Rohan Mendonca , Rebecca Pulk , Stuart Ward , Bohdan Waszkowycz , Mark Zak
IPC分类号： A61P11/06 , A61P17/06 , A61P19/02 , A61P37/06 , C07D413/14 , C07D471/14
CPC分类号： C07D471/14 , C07D487/10
摘要： The invention provides novel compounds of formula I having the general formula: wherein R1, R2, R3, X and Y are as described herein. Accordingly, the compounds may be provided in pharmaceutically acceptable compositions and used for the treatment of immunological or hyperproliferative disorders.
摘要翻译：本发明提供具有以下通式的新颖的式I化合物：其中R1，R2，R3，X和Y如本文所述。因此，化合物可以以药学上可接受的组合物提供，并用于治疗免疫学或过度增殖性疾病。

7. 发明申请

US20120088763A1 TRIAZOLOPYRIDINE DERIVATIVES AND THEIR THERAPEUTIC USE 失效
标题翻译：三唑吡啶衍生物及其治疗用途
公开(公告)号：US20120088763A1
公开(公告)日：2012-04-12
申请号：US13201716
申请日：2010-02-16
申请人： Harry Finch , John Montana , Monique Bodil Van Niel , Chi-Kit Woo , Jamie Knight , Bohdan Waszkowycz
发明人： Harry Finch , John Montana , Monique Bodil Van Niel , Chi-Kit Woo , Jamie Knight , Bohdan Waszkowycz
IPC分类号： A61K31/5377 , A61P11/00 , A61P11/06 , C07D471/04 , A61K31/437
CPC分类号： C07D471/04
摘要： Compounds of formula (I) are inhibitors of p38 MAP kinase, useful as anti-inflammatory agents in the treatment of inter alia, diseases of the respiratory tract wherein; R1 is C1-C6 alkyl, C3-C6 cycloalkyl, phenyl which is optionally substituted, 5- or 6 membered monocyclic heteroaryl which is optionally substituted, or a radical of formula (II) wherein n is 1 or 2, and R3 and R4 are independently H or C1-C6 alkyl, or R3 and R4 taken together with the nitrogen to which they are attached form a 6-membered heterocyclic ring optionally containing a further heteroatom selected from N and O; Y is —O— or —S(O)p— wherein p is 0, 1 or 2; A is an optionally substituted divalent arylene radical, or a mono- or bicyclic heteroarylene radical, or a C3-C6 divalent cycloalkylene radical having 5 or 6 ring atoms, or a piperidinylene radical wherein the ring nitrogen is linked to R2NHC(═O)W—; W is a bond, —NH— or —C(RA)(RB), wherein RA and RB are independently H, methyl, ethyl, amino, hydroxyl or halo; and R2 is a radical as defined in the claims.
摘要翻译：式（I）化合物是p38MAP激酶的抑制剂，其可用作治疗特别是呼吸道疾病的抗炎剂，其中： R 1是C 1 -C 6烷基，C 3 -C 6环烷基，任选取代的苯基，任选被取代的5-或6-元单环杂芳基，或其中n是1或2的式（II）基团，R 3和R 4是独立地是H或C 1 -C 6烷基，或者R 3和R 4与它们所连接的氮一起形成任选含有另外选自N和O的杂原子的6元杂环; Y是-O-或-S（O）p - ，其中p是0,1或2; A是任选取代的二价亚芳基，或单环或双环亚杂芳基或具有5或6个环原子的C 3 -C 6二价亚环烷基或哌啶子基，其中环氮连接至R 2 NHC（= O）W - ; W是键，-NH-或-C（RA）（RB），其中RA和RB独立地是H，甲基，乙基，氨基，羟基或卤素; 并且R 2是如权利要求中所定义的基团。

9. 发明授权

US08450314B2 Pyrimidopyridazine derivatives useful as P38 MAPK inhibitors 失效
标题翻译：可用作P38 MAPK抑制剂的嘧啶并哒嗪衍生物
公开(公告)号：US08450314B2
公开(公告)日：2013-05-28
申请号：US13201534
申请日：2010-02-16
申请人： Amanda Beswick , Bohdan Waszkowycz
发明人： Amanda Beswick , Bohdan Waszkowycz
IPC分类号： A61K31/535 , C07D413/12 , C07D413/14
CPC分类号： C07D487/04 , C07D237/14 , C07D237/18 , C07D403/12
摘要： A compound formula (IA) or (IB), or a pharmaceutically acceptable thereof; wherein the substituents are defined as in the claims, and their use as P38 MAP kinase.
摘要翻译：化合物式（IA）或（IB），或其药学上可接受的; 其中取代基如权利要求中所定义，及其用作P38 MAP激酶。

10. 发明申请

US20130012485A1 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：US20130012485A1
公开(公告)日：2013-01-10
申请号：US12520323
申请日：2007-12-20
申请人： Daniel Kaspar Bäschlin , Richard Sedrani , Stefanie Flohr , Kenji Namoto , Nils Ostermann , Finton Sirockin , François Gessier , Garry Fenton , Mandy Christine Beswick , David Edward Clark , Bohdan Waszkowycz
发明人： Daniel Kaspar Bäschlin , Richard Sedrani , Stefanie Flohr , Kenji Namoto , Nils Ostermann , Finton Sirockin , François Gessier , Garry Fenton , Mandy Christine Beswick , David Edward Clark , Bohdan Waszkowycz
IPC分类号： A61K31/135 , A61K31/568 , A61K31/565 , C07C217/52 , C07D487/04 , A61K31/4985 , C07D211/08 , A61K31/451 , C07D295/135 , A61K31/495 , C07D401/04 , A61K31/4545 , A61K31/454 , C07D243/08 , A61K31/551 , C07D223/04 , A61K31/55 , A61K31/501 , C07D237/14 , A61K31/50 , A61P3/10 , A61P19/02 , A61P3/04 , A61P19/10 , A61P9/04 , A61P25/28 , A61P13/12 , A61P3/06 , A61P9/10 , A61P29/00 , A61P25/00 , A61P35/04 , A61P9/12 , A61P25/22 , A61P5/00 , C07C215/42
CPC分类号： C07C215/42 , C07C211/29 , C07C211/31 , C07C211/40 , C07C215/14 , C07C217/16 , C07C217/52 , C07C229/16 , C07C233/41 , C07C237/10 , C07C237/24 , C07C237/36 , C07C255/24 , C07C271/20 , C07C311/07 , C07C311/08 , C07C311/20 , C07C311/29 , C07C317/32 , C07C317/44 , C07C2601/02 , C07C2601/14 , C07D207/404 , C07D211/14 , C07D211/60 , C07D213/64 , C07D213/81 , C07D213/82 , C07D233/36 , C07D237/14 , C07D237/24 , C07D239/10 , C07D239/90 , C07D263/20 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/14 , C07D409/04 , C07D471/04 , C07D487/04
摘要： Compounds of the formula (I) are provided: wherein V, W, X, Y, Z, R3, R4, R5, R6, R7 and m are as defined in the specification; and pharmaceutically acceptable salts and prodrugs thereof. The compounds may be useful in the treatment or prevention of various diseases and conditions in which dipeptidylpeptidase-IV (DPP-IV) is implicated.
摘要翻译：提供式（I）化合物：其中V，W，X，Y，Z，R 3，R 4，R 5，R 6，R 7和m如说明书中所定义; 及其药学上可接受的盐和前药。该化合物可用于治疗或预防涉及二肽基肽酶-IV（DPP-IV）的各种疾病和病症。

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