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1. 发明申请

WO2009112839A1 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2009112839A1
公开(公告)日：2009-09-17
申请号：PCT/GB2009/000672
申请日：2009-03-11
申请人： AMURA THERAPEUTICS LIMITED , QUIBELL, Martin , WATTS, John, Paul , FLINN, Nicholas, Sean
发明人： QUIBELL, Martin , WATTS, John, Paul , FLINN, Nicholas, Sean
IPC分类号： C07D491/04 , A61K31/407 , A61P19/00
CPC分类号： C07D491/04 , C07D519/00
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: R 3 is selected from cyclopentyl and cyclohexyl; R 9 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 dual efficacies for human cathepsin S and K and are useful for the treatment of rheumatoid arthritis, osteoarthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, cardiovascular diseases which exhibit significant damage and remodeling of extracellular matrix (ECM) and chronic pain.
摘要翻译：本发明的第一方面涉及式（I）化合物或其药学上可接受的盐，水合物，络合物或前药，其中：R 3选自环戊基和环己基; R9是取代的5或6元芳基或杂芳基或6,5-或6,6-稠合的联芳基或杂二芳基。式（I）化合物对于人组织蛋白酶S和K具有令人惊奇的双重效力，并且可用于治疗类风湿性关节炎，骨关节炎，慢性阻塞性肺疾病（COPD），动脉粥样硬化，表现出显着损伤和重塑细胞外基质的心血管疾病（ECM）和慢性疼痛。

2. 发明申请

WO2008007114A1 TETRAHYDROFURO [3, 2 -B] PYRR0L-3-ONES AS CATHEPSIN K INHIBITORS 审中-公开
标题翻译：四氢呋喃[3，2 -B] PYRR0L-3-ONES作为CATHEPSIN K抑制剂
公开(公告)号：WO2008007114A1
公开(公告)日：2008-01-17
申请号：PCT/GB2007/002642
申请日：2007-07-13
申请人： AMURA THERAPEUTICS LIMITED , QUIBELL, Martin , WATTS, John, Paul
发明人： QUIBELL, Martin , WATTS, John, Paul
IPC分类号： C07D491/04 , A61K31/407 , A61P19/08 , A61P19/10 , A61P35/00
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; one of R 1 and R 2 is H, and the other is selected from from OR 6 , SR 6 , NR 6 R 7 , N 3 , Me, Et, CF 3 , SOR 8 and SO 2 R 8 ; R 3 is selected from tert -butylmethyl, iso -propylmethyl, sec -butyl, tert -butyl, cyclopentyl and cyclohexyl; R 4 is optionally substituted C 1-8 alkyl or optionally substituted C 3-8 cycloalkyl; R 6 and R 7 are each independently selected from H, C 1-8 -alkyl and C 3-8 -cycloalkyl, or R 6 and R 7 are linked to form a cyclic group together with the nitrogen to which they are attached; and R 8 is C 1-8 -alkyl or C 3-8 -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; R 1和R 2之一是H，另一个选自OR 6，SR 6，，N 6，R 6，N 3，Me，Et，CF 3，SOR 8， / SUP>和SO 2 R 8; R 3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; R 4是任选取代的C 1-8烷基或任选取代的C 3-8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连接形成环状基团以及它们所连接的氮原子; R 8是C 1-8 - 烷基或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。

3. 发明申请

WO2008007112A1 TETRAHYDROFURO [3, 2-B] PYRR0L-3-ONES AS CATHEPSIN K INHIBITORS 审中-公开
标题翻译：四氢呋喃[3，2-B] PYRR0L-3-ONES作为CATHEPSIN K抑制剂
公开(公告)号：WO2008007112A1
公开(公告)日：2008-01-17
申请号：PCT/GB2007/002639
申请日：2007-07-13
申请人： AMURA THERAPEUTICS LIMITED , QUIBELL, Martin , WATTS, John, Paul
发明人： QUIBELL, Martin , WATTS, John, Paul
IPC分类号： C07D491/04 , A61K31/407 , A61P19/08 , A61P19/10 , A61P35/00
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; one of R 1 and R 2 is H, and the other is selected from H, OR 6 , SR 6 , NR 6 R 7 , N 3 , Me, Et, CF 3 , SOR 8 and SO 2 R 8 ; R 4 is optionally substituted C i-8 alkyl or optionally substituted C 3-8 cycloalkyl; R 6 and R 7 are each independently selected from H, C 1-8 -alkyl and C 3-8 -cycloalkyl, or R 6' and R 7 are linked to form a cyclic group together with the nitrogen to which they are attached; R 8 is C 1-8 -alkyl or C 3-g -cycloalkyl; and k is an integar chosen from 1 or 2. 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; R 1和R 2之一是H，另一个选自H，OR 6，SR 6 >，NR 6，R 7，N 3，Me，Et，CF 3，SOR 8 ＆lt; 2＆gt;和＆lt; S＆gt; 2＆lt; 8＆gt; R 4是任选取代的C 1-8烷基或任选取代的C 3-8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连接形成环状基团以及它们所连接的氮原子; R 8是C 1-8 - 烷基或C 3-g-环烷基; 并且k是选自1或2的整数。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，恰加斯氏病，疟疾，牙龈疾病，高钙血症，代谢性骨病，涉及基质或软骨退化的疾病，以及诸如骨转移和相关疼痛的骨癌症。

4. 发明申请

WO2008007130A1 FURO [3,2-B] PYRROL-3-ONE DERIVATIVES AND THEIR USE AS CYSTEINYL PROTEINASE INHIBITORS 审中-公开
标题翻译： FURO [3,2-B]吡咯-3-酮衍生物及其作为CYSTEINYL蛋白酶抑制剂的用途
公开(公告)号：WO2008007130A1
公开(公告)日：2008-01-17
申请号：PCT/GB2007/002664
申请日：2007-07-13
申请人： AMURA THERAPEUTICS LIMITED , QUIBELL, Martin , WATTS, John, Paul
发明人： QUIBELL, Martin , WATTS, John, Paul
IPC分类号： C07D491/04 , A61K31/407 , A61P19/00
CPC分类号： C07D491/04
摘要： The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof (I), wherein: R 3 is cyclopentyl or cyclohexyl; X is CH or N; and R 4 is optionally substituted C 1-8 alkyl or optionally substituted C 3-8 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（I），其中：R 3是环戊基或环己基; X是CH或N; R 4是任选取代的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，涉及基质或软骨退化的疾病，以及骨癌症如骨转移和相关的疼痛。

5. 发明申请

WO2009112826A1 FURO [3, 2-B] PYRR0L-3-0NES AS CATHEPSIN S INHIBITORS 审中-公开
标题翻译： FURO [3，2-B] PYRR0L-3-0作为CATHEPSIN S抑制剂
公开(公告)号：WO2009112826A1
公开(公告)日：2009-09-17
申请号：PCT/GB2009/000653
申请日：2009-03-11
申请人： AMURA THERAPEUTICS LIMITED , QUIBELL, Martin , WATTS, John, Paul , FLINN, Nicholas, Sean
发明人： QUIBELL, Martin , WATTS, John, Paul , FLINN, Nicholas, Sean
IPC分类号： C07D491/04 , A61K31/407 , A61P3/04 , A61P7/12 , A61P9/00 , A61P11/06 , A61P17/06 , A61P19/02 , A61P25/00 , A61P29/00
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 R 3 and R 4 is H, and the other is selected from C 1-6 -alkyl, C1-6-haloalkyl, C 1-6 - alkoxy, and C 6-12 -aralkyl; or R 3 and R 4 are each independently selected from C 1-6 -aIkyl and halo; R 9 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.
摘要翻译：本发明的第一方面涉及式（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 3和R 4中的一个为H，另一个选自C 1-6 - 烷基，C 1-6 - 卤代烷基，C 1-6 - 烷氧基和C 6-12 - 芳烷基; 或R 3和R 4各自独立地选自C 1-6 - 烷基和卤素; R9是取代的5或6元芳基或杂芳基或6,5-或6,6-稠合的联芳基或杂二芳基。式（I）化合物对人组织蛋白酶S具有惊人的高效力，优于其它哺乳动物组织蛋白酶的选择性，并且可用于治疗诸如类风湿性关节炎，多发性硬化症，重症肌无力，移植排斥，糖尿病，干燥综合症，格雷夫斯病，系统性红斑狼疮，骨关节炎，牛皮癣，特发性血小板减少性紫癜，过敏性鼻炎，哮喘，动脉粥样硬化，肥胖症，慢性阻塞性肺病和慢性疼痛。

6. 发明申请

WO2008007109A1 FURO[3,2-B]PYRROL-3-ONE DERIVATIVES AND THEIR USE AS CYSTEINYL PROTEINASE INHIBITORS 审中-公开
标题翻译： FURO [3,2-B]吡咯-3-酮衍生物及其作为CYSTEINYL蛋白酶抑制剂的用途
公开(公告)号：WO2008007109A1
公开(公告)日：2008-01-17
申请号：PCT/GB2007/002630
申请日：2007-07-13
申请人： AMURA THERAPEUTICS LIMITED , QUIBELL, Martin , WATTS, John Paul
发明人： QUIBELL, Martin , WATTS, John Paul
IPC分类号： C07D491/04 , A61K31/407 , A61P19/00
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 R 4 is optionally substituted C 3-8 alkyl or optionally substituted C 3-8 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为CH或N; 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。

7. 发明申请

WO2007023281A2 BIOLOGICALLY ACTIVE COMPOUNDS 审中-公开
标题翻译：生物活性化合物
公开(公告)号：WO2007023281A2
公开(公告)日：2007-03-01
申请号：PCT/GB2006/003155
申请日：2006-08-23
申请人： AMURA THERAPEUTICS LIMITED , QUIBELL, Martin , WATTS, John, Paul , WANG, Yikang , PATIENT, Lee , HEAL, Jonathan, Richard
发明人： QUIBELL, Martin , WATTS, John, Paul , WANG, Yikang , PATIENT, Lee , HEAL, Jonathan, Richard
CPC分类号： C07D491/048 , C07D487/04 , C07D498/04
摘要： The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. 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 and diseases involving matrix or cartilage degradation.
摘要翻译：本发明涉及式（I）的化合物及其药学上可接受的盐。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，佩吉特病，查加斯病，疟疾，牙龈病，高血钙症，代谢性骨病和涉及基质或软骨降解。

8. 发明申请

WO2007017698A1 PREPARATION OF DIAZAPENTALENE DERIVATIVES VIA EPOXYDATION OF DIHYDROPYRROLES 审中-公开
标题翻译：通过二氢吲哚的环氧化合物制备二氮杂萘衍生物
公开(公告)号：WO2007017698A1
公开(公告)日：2007-02-15
申请号：PCT/GB2006/003061
申请日：2006-08-10
申请人： AMURA THERAPEUTICS LIMITED , QUIBELL, Martin , WANG, Yikang , NALLY, James , WATTS, John, Paul , AGGARWAL, Virendar, Kumar , STANDEN, Michael
发明人： QUIBELL, Martin , WANG, Yikang , NALLY, James , WATTS, John, Paul , AGGARWAL, Virendar, Kumar , STANDEN, Michael
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , Y02P20/55
摘要： The present invention relates to a process for preparing a compound of formula (I), wherein R 1 Is Pg 1 Or P 1 ’; P 1 ' is CO-hydrocarbyl; P 2 is CH 2 , O or N-Pg 2 ; and Pg 1 and Pg 2 are each independently nitrogen protecting groups; (i) reacting a compound of formula (II) with a dioxirane to form an epoxide of formula (III); where X is selected from CN, CH 2 N 3 , CH 2 NH-Pg 2 , ONH-Pg 2 , NHNH-Pg 2 , N(Pg 2 )NH-Pg 2 ; (ii) converting a compound of formula (III) to a compound of formula (I).
摘要翻译：本发明涉及一种制备式（I）化合物的方法，其中R 1是Pg 1或P 1'; P 1是CO-烃基; P 2是CH 2，O或N-Pg 2; 和Pg <！ - SIPO - > 1和Pg 2 2各自独立地为氮保护基; （i）使式（II）的化合物与二环氧环酮反应以形成式（III）的环氧化物; 其中X选自CN，CH 2，N 3，CH 2，NH-Pg 2，ONH-Pg N，P（NH 2）NH 2 P 2 O 2，NHNH-Pg 2，N（Pg 2）NH-Pg 2 （ii）将式（III）化合物转化为式（I）化合物。

9. 发明申请

WO2009144450A1 TETRAHYDROFURO [3, 2-B] PYRROL-3-ONE DERIVATIVES AS INHIBITORS OF CYSTEINE PROTEASES 审中-公开
标题翻译：作为CYSTEINE PROTEASES的抑制剂的四氢呋喃[3,2-B]吡咯-3-酮衍生物
公开(公告)号：WO2009144450A1
公开(公告)日：2009-12-03
申请号：PCT/GB2009/001319
申请日：2009-05-28
申请人： AMURA THERAPEUTICS LIMITED , QUIBELL, Martin , WATTS, John, Paul
发明人： QUIBELL, Martin , WATTS, John, Paul
IPC分类号： C07D491/04 , A61K31/407 , 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 R 1 and R 2 is H, and the other is selected fromC 1-8 -alkyl, C 3-6 -cycloalkyl and C 1-8 -alkyl-C 5-10 -aryl; R 3 is selected from ter t-butyl, cyclopentyl and 1-methylcyclopentyl; R 9 is selected from the following: (F). The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of various diseases.
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C 1-8 - 烷基，C 3-6 - 环烷基和C 1 -C 8 -8烷基C 5-10 - 芳基; R3选自叔丁基，环戊基和1-甲基环戊基; R9选自以下：（F）。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各种疾病中的用途。

10. 发明申请

WO2009087379A2 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2009087379A2
公开(公告)日：2009-07-16
申请号：PCT/GB2009/000039
申请日：2009-01-07
申请人： AMURA THERAPEUTICS LIMITED , QUIBELL, Martin , WATTS, John, Paul
发明人： QUIBELL, Martin , WATTS, John, Paul
IPC分类号： C07D491/04 , A61K31/407 , A61P19/00
CPC分类号： A61K31/496 , C07D491/048 , Y02A50/411
摘要： A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein one of R 1 and R 2 is H, and the other is selected from C 1-8 -alkyl, C 3-6 -cycloalkyl and C 1-8 -alkyl-C 5-10 -aryl; R 3 is selected from tert -butylmethyl, zso-propylmethyl, sec- butyl, tert-butyl, cyclopentyl, cyclohexyl and 1-methylcyclopentyl; R 9 is selected from the following: wherein: R 4 is selected from C 1-8 -alkyl and C 3-8 -cycloalkyl; G is selected from: ) CH, ) CMe and N; E is selected from: O, S, ) SO 2 , )NH, )NMe and N-oxide ()N->O); J and R are independently selected from: )CH, N and N-oxide ()N-^O); and R 41 is selected from amino, methylamino, dimethylamino, isopropylamino, isopropyl(methyl)amino, cyclopropylamino, cyclopropyl(methyl)amino, cyclopentylamino, morpholino, piperidin-1-yl, piperidin-1-ylmethyl, morpholinomethyl, 4-methylpiperazin-l-yl, 4-(2-methoxyethyl)piperazin-l-yl, 1- moφholinoethyl, l-(dimethylamino)ethyl, l-(methylamino)ethyl, 4-fluoro-l- methylpyrrolidin-2-yl, 4,4-difluoropiperidin-l-yl, piperidin-4-yl, l-methylpiperidin-4- yl, pyridin-3-ylamino, pyridin-2-ylamino, l-methylpyrrolidin-3-yl, methyl, isopropyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of various diseases.
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C 1-8 - 烷基，C 3-6 - 环烷基和 C 1-8 - 烷基 - C 5-10 - 芳基; R 3选自叔丁基甲基，异丙基甲基，仲丁基，叔丁基，环戊基，环己基和1-甲基环戊基; R 9选自如下：其中：R 4选自C 1-8 - 烷基和C 3-8 - 环烷基; G选自：）CH，）CMe和N; E选自：O，S，）SO 2，）NH，）NMe和N-氧化物（）N-> O）; J和R独立地选自：CH，N和N-氧化物（）N - O）; （甲基）氨基，环丙基氨基，环丙基（甲基）氨基，环戊基氨基，吗啉代，哌啶-1-基，哌啶-1-基甲基，吗啉代甲基，4-甲基哌嗪-1-基（2-甲氧基乙基）哌嗪-1-基，1-吗啉基乙基，1-（二甲基氨基）乙基，1-（甲基氨基）乙基，4-氟-1-甲基吡咯烷-2-基，二氟哌啶-1-基，哌啶-4-基，1-甲基哌啶-4-基，吡啶-3-基氨基，吡啶-2-基氨基，1-甲基吡咯烷-3-基，甲基，异丙基。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各种疾病中的用途。

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