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1. 发明申请

US20120202756A1 USE OF PRODRUGS TO AVOID GI MEDIATED ADVERSE EVENTS 审中-公开
标题翻译：使用产品避免GI介入的不良事件
公开(公告)号：US20120202756A1
公开(公告)日：2012-08-09
申请号：US13253677
申请日：2011-10-05
申请人： Richard Franklin , Martin Quibell , Robert G. Tyson , Bernard T. Golding
发明人： Richard Franklin , Martin Quibell , Robert G. Tyson , Bernard T. Golding
IPC分类号： A61K31/7056 , C07H15/14 , C07C229/22 , C07C229/60 , C07D211/46 , C07D211/22 , C07D417/12 , C07D403/12 , A61K31/4164 , A61K31/225 , A61K31/24 , A61K31/445 , A61K31/554 , A61K31/506 , A61P31/04 , A61P9/06 , A61P25/28 , A61P19/02 , A61P25/24 , A61P35/00 , A61P19/10 , A61P31/12 , A61P3/10 , C07D233/94
CPC分类号： C07C279/26 , A61K31/4375 , C07C233/47 , C07C233/54 , C07C2601/14 , C07D211/32 , C07D211/46 , C07D233/94 , C07D285/135 , C07D307/20 , C07D403/12 , C07D405/12 , C07D417/12 , C07D471/04 , C07D501/60 , C07F9/3873 , C07H15/04
摘要： The present invention relates to prodrugs of a wide variety of drugs and pharmaceutical compositions containing such prodrugs. Methods for minimizing locally mediated (from within the gut lumen) adverse gastrointestinal events associated with the underivatised drug and increasing the sustainment of plasma drug levels with the aforementioned prodrugs are also provided. Thus, the present invention relates to the use of prodrugs of a wide diversity of drugs (other than opioids) to transiently inactivate them and so reduce directly, locally mediated adverse gastrointestinal (GI) side-effects normally evident after administration of the parent compound. Additionally, such prodrugs may confer improved pharmacokinetics.
摘要翻译：本发明涉及各种药物的前药和含有这些前药的药物组合物。还提供了用于使局部介导的（来自肠内腔）最小化与未发病药物相关的不良胃肠道事件和用上述前药增加血浆药物水平的维持的方法。因此，本发明涉及广泛多样的药物（阿片样物质除外）的前体药物使用以使其短暂失活，并因此降低在给予母体化合物后通常明显的局部介导的不良胃肠道（GI）副作用。此外，这样的前药可以赋予改善的药代动力学。

2. 发明授权

US07799791B2 Tetrahydrofuro(3,2-B) pyrrol-3-one derivatives as inhibitors of cysteine proteinases 有权
标题翻译：四氢呋喃（3,2-B）吡咯-3-酮衍生物作为半胱氨酸蛋白酶的抑制剂
公开(公告)号：US07799791B2
公开(公告)日：2010-09-21
申请号：US12319555
申请日：2009-01-08
申请人： Martin Quibell , John Paul Watts
发明人： Martin Quibell , John Paul Watts
IPC分类号： A61K31/427 , C07D491/04 , A61P19/10
CPC分类号： C07D491/04
摘要： A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: one of R1 and R2 is H, and the other is selected from OR6, SR6, NR6R7, N3, Me, Et, CF3, SOR8 and SO2R8; or R1 and R2 are both H; one of R3 and R4 is H, and the other is selected from tert-butylmethyl, iso-propylmethyl, sec-butyl, tert-butyl, cyclopentyl and cyclohexyl; or R3 and R4 are joined together with the adjacent backbone carbon atom to form a spiro-C5-C6 cycloalkyl group; R6 and R7 are each independently selected from H, C1-8-alkyl and C3-8-cycloalkyl; or R6 and R7 are linked to form a cyclic group together with the nitrogen to which they are attached; R8 is C1-8-alkyl or C3-8-cycloalkyl; R9 is a para-substituted 6-membered monocyclic aryl or heteroaryl ring which includes up to five heteroatoms. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.
摘要翻译：式（I）化合物或其药学上可接受的盐，水合物，复合物或前药，其中：R 1和R 2之一为H，另一个选自OR 6，SR 6，NR 6 R 7，N 3，Me，Et ，CF3，SOR8和SO2R8; 或R 1和R 2均为H; R3和R4之一是H，另一个选自叔丁基甲基，异丙基甲基，仲丁基，叔丁基，环戊基和环己基; 或者R 3和R 4与相邻的主链碳原子连接在一起形成螺C5-C6环烷基; R 6和R 7各自独立地选自H，C 1-8 - 烷基和C 3-8 - 环烷基; 或R 6和R 7与它们所连接的氮一起形成环状基团; R 8是C 1-8 - 烷基或C 3-8 - 环烷基; R9是包含至多5个杂原子的对位取代的6元单环芳基或杂芳基环。本发明还涉及包含式（I）化合物的药物组合物，以及这些化合物在治疗选自骨质疏松症，佩吉特氏病，恰加斯病，疟疾，牙龈疾病，高钙血症，代谢性骨病，涉及基质或软骨降解，以及骨癌症如骨转移和相关的疼痛。

3. 发明申请

US20100216811A1 FURO[3. 2-B] PYRROL DERIVATIVES 有权
标题翻译： FURO [3。 2-B]吡咯烷衍生物
公开(公告)号：US20100216811A1
公开(公告)日：2010-08-26
申请号：US12773524
申请日：2010-05-04
申请人： Martin Quibell , John Paul Watts
发明人： Martin Quibell , John Paul Watts
IPC分类号： A61K31/497 , C12N5/02 , A61K31/454 , A61P35/00 , A61P19/08 , A61P19/10
CPC分类号： C07D491/02
摘要： The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: R3 is tert-butylmethyl, sec-butyl or tert-butyl; X is CH or N; and R4 is optionally substituted C1-8 alkyl or optionally substituted C3-8 cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐，其中：R3是叔丁基甲基，仲丁基或叔丁基; X是CH或N; 且R 4为任选取代的C 1-8烷基或任选取代的C 3-8环烷基。本发明还涉及包含式（I）化合物的药物组合物，以及这些化合物在治疗选自骨质疏松症，佩吉特氏病，恰加斯病，疟疾，牙龈疾病，高钙血症，代谢性骨病，涉及基质或软骨降解，以及骨癌症如骨转移和相关的疼痛。

4. 发明申请

US20090186831A1 Tetrahydrofuro(3,2-B) pyrrol-3-one derivatives as inhibitors of cysteine proteinases 有权
标题翻译：四氢呋喃（3,2-B）吡咯-3-酮衍生物作为半胱氨酸蛋白酶的抑制剂
公开(公告)号：US20090186831A1
公开(公告)日：2009-07-23
申请号：US12319555
申请日：2009-01-08
申请人： Martin Quibell , John Paul Watts
发明人： Martin Quibell , John Paul Watts
IPC分类号： A61K38/05 , C07D493/04 , C12N9/99 , C12Q1/37 , G01N33/573 , A61P19/02
CPC分类号： C07D491/04
摘要： A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: one of R1 and R2 is H, and the other is selected from OR6, SR6, NR6R7, N3, Me, Et, CF3, SOR8 and SO2R8; or R1 and R2 are both H; one of R3 and R4 is H, and the other is selected from tert-butylmethyl, iso-propylmethyl, sec-butyl, tert-butyl, cyclopentyl and cyclohexyl; or R3 and R4 are joined together with the adjacent backbone carbon atom to form a spiro-C5-C6 cycloalkyl group; R6 and R7 are each independently selected from H, C1-8-alkyl and C3-8-cycloalkyl; or R6 and R7 are linked to form a cyclic group together with the nitrogen to which they are attached; R8 is C1-8-alkyl or C3-8-cycloalkyl; R9 is a para-substituted 6-membered monocyclic aryl or heteroaryl ring which includes up to five heteroatoms. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.
摘要翻译：式（I）化合物或其药学上可接受的盐，水合物，复合物或前药，其中：R 1和R 2之一为H，另一个选自OR 6，SR 6，NR 6 R 7，N 3，Me，Et ，CF3，SOR8和SO2R8; 或R 1和R 2均为H; R3和R4之一是H，另一个选自叔丁基甲基，异丙基甲基，仲丁基，叔丁基，环戊基和环己基; 或者R 3和R 4与相邻的主链碳原子连接在一起形成螺C5-C6环烷基; R 6和R 7各自独立地选自H，C 1-8 - 烷基和C 3-8 - 环烷基; 或R 6和R 7与它们所连接的氮一起形成环状基团; R 8是C 1-8 - 烷基或C 3-8 - 环烷基; R9是包含至多5个杂原子的对位取代的6元单环芳基或杂芳基环。本发明还涉及包含式（I）化合物的药物组合物，以及这些化合物在治疗选自骨质疏松症，佩吉特氏病，恰加斯病，疟疾，牙龈疾病，高钙血症，代谢性骨病，涉及基质或软骨降解，以及骨癌症如骨转移和相关的疼痛。

5. 发明授权

US07425562B2 Inhibitors of cruzipain and other cysteine proteases 有权
标题翻译：克鲁替班和其他半胱氨酸蛋白酶抑制剂
公开(公告)号：US07425562B2
公开(公告)日：2008-09-16
申请号：US10466384
申请日：2002-01-17
申请人： Martin Quibell
发明人： Martin Quibell
IPC分类号： A61K31/44 , A61K31/40 , C07D471/02 , C07D487/04
CPC分类号： C07D491/04
摘要： Compounds of general formula (I) or general formula (II) wherein R1, P1, P2, Q, Y, (X)o, (W)n, (V)m, Z and U are as defined in the specification, are inhibitors of cruzipain and other cysteine protease inhibitors and are useful as therapeutic agents, for example in Chagas' disease, or for validating therapeutic target compounds.
摘要翻译：通式（I）或通式（II）的化合物，其中R 1，P 1，P 2，Q，Y，（X ）（W）N，Z（Z），Z和U如说明书中所定义，是克鲁替班和其他的抑制剂半胱氨酸蛋白酶抑制剂，并且可用作治疗剂，例如在恰加斯病中或用于验证治疗性靶化合物。

6. 发明申请

US20050070598A1 Cysteine protease inhibitors 审中-公开
标题翻译：半胱氨酸蛋白酶抑制剂
公开(公告)号：US20050070598A1
公开(公告)日：2005-03-31
申请号：US10678947
申请日：2003-10-03
申请人： Martin Quibell , Steven Taylor , Urszula Grabowska , Magnus Nilsson , Veronique Morrison
发明人： Martin Quibell , Steven Taylor , Urszula Grabowska , Magnus Nilsson , Veronique Morrison
IPC分类号： C07D307/22 , C07D307/32 , C07D307/68 , C07D307/85 , C07D309/14 , C07D309/30 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , A61K31/541 , A61K31/366 , A61K31/496 , A61K31/5377 , C07D413/02 , C07D417/02 , C07D45/02
CPC分类号： C07D405/12 , C07D307/22 , C07D307/32 , C07D307/68 , C07D307/85 , C07D309/14 , C07D309/30 , C07D405/14 , C07D409/12 , C07D409/14
摘要： of the formula (IV): where: R1=R′C(O), R′SO2, R′=a bicyclic, saturated or unsaturated, 8-12 membered ring system containing 0-4 hetero atoms selected from S, O and N, which is optionally substituted with up to four substituents independently selected from groups a), b) and c) below; or R′=a monocyclic, saturated or unsaturated, 5-7 membered ring containing 0-3 hetero atoms selected from S, O and N, which monocyclic ring bears at least one substituent selected from group a) and/or c) and which may optionally bear one or two further substituents selected from group b); R4=H, C1-7-alkyl, Ar—C1-7-alkyl, Ar, C3-7-cycloalkyl; C2-7alkenyl; R3=C1-7-alkyl, C2-C7 alkenyl, C2-C7 alkenyl, C3-7-cycloalkyl, Ar—C1-7-alkyl, Ar; R5=C1-7-alkyl, halogen, Ar—C1-7-alkyl, CO-3-alkyl-CONR3R4 or a bulky amine R6 is H, C1-7-alkyl, Ar—C1-7-alkyl, C1-3-alkyl-SO2-Rix, C1-3-alkyl-C(O)—NHRix or CH2XAr q is 0 or 1 have utility as inhibitors of cysteine proteases such as cathepsin K and falcipain.
摘要翻译：式（Ⅳ）：其中：R1 = R'C（O），R'SO2，R'=含有0-4个杂原子的双环饱和或不饱和的8-12元环系，其选自S，O和 N，其任选被至多四个独立地选自以下的基团a），b）和c）中的取代基取代; 或R'=含有0-3个选自S，O和N的杂原子的单环，饱和或不饱和的5-7元环，该单环具有至少一个选自a）和/或c）的取代基，并且其中可以任选地带有一个或两个其它选自组b）的取代基; R 4 = H，C 1-7 - 烷基，Ar-C 1-7 - 烷基，Ar，C 3-7 - 环烷基; C2-7烯基; R 3 = C 1-7 - 烷基，C 2 -C 7烯基，C 2 -C 7链烯基，C 3-7 - 环烷基，Ar-C 1-7 - 烷基，Ar; R 5 = C 1-7 - 烷基，卤素，Ar-C 1-7 - 烷基，CO-3-烷基-CONR 3 R 4或大体积的胺R 6是H，C 1-7 - 烷基，Ar-C 1-7 - 烷基，C 1-3 - 烷基-SO 2 -R 5，C 1-3 - 烷基-C（O）-NHR x或CH 2 XAr q为0或1可用作半胱氨酸蛋白酶如组织蛋白酶K和恶性蛋白酶的抑制剂。

7. 发明申请

US20050020588A1 Cysteine protease inhibitors 审中-公开
标题翻译：半胱氨酸蛋白酶抑制剂
公开(公告)号：US20050020588A1
公开(公告)日：2005-01-27
申请号：US10929133
申请日：2004-08-27
申请人： Martin Quibell , Steven Taylor , Urszula Grabowska , Magnus Nilsson , Veronique Morisson
发明人： Martin Quibell , Steven Taylor , Urszula Grabowska , Magnus Nilsson , Veronique Morisson
IPC分类号： C07D307/22 , C07D307/32 , C07D307/68 , C07D307/85 , C07D309/14 , C07D309/30 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , A61K31/541 , A61K31/496 , A61K31/5377 , C07D413/02 , C07D417/02 , C07
CPC分类号： C07D307/32 , C07D307/22 , C07D307/68 , C07D307/85 , C07D309/14 , C07D309/30 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14
摘要： Cathepsin S is a highly active cysteine protease belonging to the papain superfamily. It is found mainly in lymph nodes, spleen, and macrophages and this limited occurrence suggests the potential involvement of this enzyme in the pathogenesis of degenerative disease. The invention relates to novel protease inhibitors, particularly inhibitors of the cysteine proteases of the papain superfamily and more particularly to Cathepsin S. The inhibitors are Furanone derivatives of Formula (II) which have a characteristic non-hydrogen substituent R5. They are selective over other members of the family and in particular show selectivity over other members of the Cathepsin family such as L and K.
摘要翻译：组织蛋白酶S是属于木瓜蛋白酶超家族的高活性半胱氨酸蛋白酶。主要发现在淋巴结，脾脏和巨噬细胞中，这种有限的发生表明该酶潜在地参与退行性疾病的发病机制。本发明涉及新型蛋白酶抑制剂，特别是木瓜蛋白酶超家族的半胱氨酸蛋白酶的抑制剂，更具体地涉及组织蛋白酶S.抑制剂是具有特征非氢取代基R5的式（II）的呋喃酮衍生物。它们对家族的其他成员具有选择性，并且特别地显示出组织蛋白酶家族的其它成员如L和K的选择性。

8. 发明授权

US08877927B2 Furo[3,2-B] pyrrol -3-one derivatives and their use as cysteinyl proteinase inhibitors 有权
标题翻译：呋喃并[3,2-B]吡咯-3-酮衍生物及其作为半胱氨酰蛋白酶抑制剂的用途
公开(公告)号：US08877927B2
公开(公告)日：2014-11-04
申请号：US12319549
申请日：2009-01-08
申请人： Martin Quibell , John Paul Watts
发明人： Martin Quibell , John Paul Watts
IPC分类号： A61K31/496 , C07D491/044 , A61K31/454 , A61P19/00 , G01N33/53 , A61P29/00 , C07D491/04
CPC分类号： C07D491/04
摘要： The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof (I), wherein: one of R1 and R2 is H, and the other is selected from F and Cl, or R1 and R2 are both F; R3 is selected from cyclopentyl and cyclohexyl; R4 is an optionally substituted 5- or 6-membered monocyclic or an 8- to 10-membered bicyclic aryl or heteroaryl ring which includes up to four heteroatoms. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐，式（I）化合物或其药学上可接受的盐，水合物，复合物或前体药物（I），其中：R1和 R2为H，另一个选自F和Cl，或R1和R2均为F; R3选自环戊基和环己基; R 4是任选取代的5或6元单环或8至10元双环芳基或杂芳环，其包含至多四个杂原子。本发明还涉及包含式（I）化合物的药物组合物，以及这些化合物在治疗选自骨质疏松症，佩吉特氏病，恰加斯病，疟疾，牙龈疾病，高钙血症，代谢性骨病，涉及基质或软骨降解，以及骨癌症如骨转移和相关的疼痛。

9. 发明授权

US08389737B2 Furo[3, 2-B] pyrrol-3-ones as cathespin S inhibitors 失效
公开(公告)号：US08389737B2
公开(公告)日：2013-03-05
申请号：US12853005
申请日：2010-08-09
申请人： Martin Quibell , John P. Watts , Nicholas S. Flinn
发明人： Martin Quibell , John P. Watts , Nicholas S. Flinn
IPC分类号： C07D417/14 , A61K31/428
CPC分类号： A61K31/407 , A61K31/41 , A61K31/4155 , A61K31/4178 , A61K31/4192 , A61K31/4196 , A61K31/4245 , A61K31/428 , A61K31/4439 , A61K31/4709 , A61K31/498 , A61K31/538 , A61K31/55 , C07D417/12 , C07D491/04 , C07D491/048 , G01N33/573 , G01N2333/96466 , G01N2500/04
摘要： A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: one of R3 and R4 is H, and the other is selected from C1-6-alkyl, C1-6-haloalkyl, C1-6-alkoxy, and C6-12-aralkyl; or R3 and R4 are each independently selected from C1-6-alkyl and halo; R9 is a substituted 5 or 6-membered aryl or heteroaryl group or a 6,5- or 6,6-fused biaryl or heterobiaryl group. Compounds of formula (I) exhibit surprisingly high efficacies for human cathepsin S, excellent selectivity verses other mammalian cathepsins and are useful for treatment of diseases such as rheumatoid arthritis, multiple sclerosis, myasthenia gravis, transplant rejection, diabetes, Sjogrens syndrome, Grave's disease, systemic lupus erythematosis, osteoarthritis, psoriasis, idiopathic thrombocytopenic purpura, allergic rhinitis, asthma, atherosclerosis, obesity, chronic obstructive pulmonary disease and chronic pain.

10. 发明授权

US07846935B2 Furo[3,2-B]pyrrol-3-one derivatives and their use as cysteinyl proteinase inhibitors 失效
标题翻译：呋喃并[3,2-B]吡咯-3-酮衍生物及其作为半胱氨酰蛋白酶抑制剂的用途
公开(公告)号：US07846935B2
公开(公告)日：2010-12-07
申请号：US12319556
申请日：2009-01-08
申请人： Martin Quibell , John Paul Watts
发明人： Martin Quibell , John Paul Watts
IPC分类号： A61K31/496 , A61K31/454 , C07D491/08 , C12Q1/37
CPC分类号： C07D491/04
摘要： The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: X is CH or N; and R4 is optionally substituted C3-8 alkyl or optionally substituted C3-8 cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐，其中：X是CH或N; 并且R 4是任选取代的C 3-8烷基或任选取代的C 3-8环烷基。本发明还涉及包含式（I）化合物的药物组合物，以及这些化合物在治疗选自骨质疏松症，佩吉特氏病，恰加斯病，疟疾，牙龈疾病，高钙血症，代谢性骨病，涉及基质或软骨降解，以及骨癌症如骨转移和相关的疼痛。

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