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1. 发明授权

US07947712B2 8-hydroxyquinoline compounds and methods thereof 失效
标题翻译： 8-羟基喹啉化合物及其方法
公开(公告)号：US07947712B2
公开(公告)日：2011-05-24
申请号：US11895222
申请日：2007-08-23
申请人： Matthew G. Bursavich , Sabrina Lombardi , Adam M. Gilbert , Leif Mark Laakso , Gulnaz Khafizova , David Brian How , Joshua James Sabatini , Phaik-Eng Sum , Jeremy Clemens
发明人： Matthew G. Bursavich , Sabrina Lombardi , Adam M. Gilbert , Leif Mark Laakso , Gulnaz Khafizova , David Brian How , Joshua James Sabatini , Phaik-Eng Sum , Jeremy Clemens
IPC分类号： C07D215/04 , A61K31/04
CPC分类号： C07D215/28 , C07D215/26 , C07D401/06 , C07D401/12 , C07D405/06 , C07D409/10 , C07D417/10
摘要： The present invention relates to 8-Hydroxyquinoline Compounds; compositions comprising an 8-Hydroxyquinoline Compound; and methods for treating or preventing a metalloproteinase-related disorder, such as, an arthritic disorder, osteoarthritis, malignant neoplasm, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, atherosclerosis, age-related macular degeneration, myocardial infarction, a corneal ulceration, an ocular surface disease, hepatitis, an aortic aneurysm, tendonitis, a central nervous system disorder, abnormal wound healing, angiogenesis, restenosis, cirrhosis, multiple sclerosis, glomerulonephritis, graft versus host disease, diabetes, an inflammatory bowel disease, shock, invertebral disc degeneration, stroke, osteopenia or a periodontal disease or comprising administering an effective dose of an 8-Hydroxyquinoline Compound to a mammal in need thereof.
摘要翻译：本发明涉及8-羟基喹啉化合物; 包含8-羟基喹啉化合物的组合物; 以及用于治疗或预防金属蛋白酶相关疾病如关节炎疾病，骨关节炎，恶性肿瘤，类风湿性关节炎，哮喘，慢性阻塞性肺病，动脉粥样硬化，年龄相关性黄斑变性，心肌梗塞，角膜溃疡，眼表疾病，肝炎，主动脉瘤，腱炎，中枢神经系统疾病，伤口愈合异常，血管生成，再狭窄，肝硬化，多发性硬化，肾小球性肾炎，移植物抗宿主病，糖尿病，炎性肠病，休克，椎间盘退变，中风，骨质减少或牙周病，或包括向有需要的哺乳动物施用有效剂量的8-羟基喹啉化合物。

2. 发明申请

US20090298820A1 3-SUBSTITUTED-1H-PYRROLO[2,3-B]PYRIDINE AND 3-SUBSTITUTED-1H-PYRROLO[3,2-B]PYRIDINE COMPOUNDS, THEIR USE AS MTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES 审中-公开
标题翻译： 3-取代的1H-吡咯并[2,3-b]吡啶和3-取代的1H-吡咯[3,2-B]吡啶化合物，它们作为MTOR激酶和PI3激酶抑制剂使用，以及它们的合成
公开(公告)号：US20090298820A1
公开(公告)日：2009-12-03
申请号：US12473658
申请日：2009-05-28
申请人： Hwei-Ru Tsou , Gary Harold Birnberg , Gloria Jean MacEwan , Semiramis Ayral-Kaloustian , Matthew Gregory Bursavich , Sabrina Lombardi , Nan Zhang , Adam Matthew Gilbert , George Theordore Grosu , Natasja Brooijmans , Thai Hiep Nguyen
发明人： Hwei-Ru Tsou , Gary Harold Birnberg , Gloria Jean MacEwan , Semiramis Ayral-Kaloustian , Matthew Gregory Bursavich , Sabrina Lombardi , Nan Zhang , Adam Matthew Gilbert , George Theordore Grosu , Natasja Brooijmans , Thai Hiep Nguyen
IPC分类号： A61K31/437 , A61K31/5375 , A61K31/5377 , A61K31/496 , C07D471/04 , A61P35/00 , C07D498/08 , A61P29/00 , A61P17/00 , A61P19/00
CPC分类号： C07D471/04 , C07D498/08
摘要： The invention relates to 3-substituted-1H-pyrrolo[2,3-b]pyridine, and 3-substituted-1H-pyrrolo[3,2-b]pyridine compounds of the Formula 1: or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds.
摘要翻译：本发明涉及式1的3-取代-1H-吡咯并[2,3-b]吡啶和3-取代-1H-吡咯并[3,2-b]吡啶化合物或其药学上可接受的盐，其中组成变量如本文所定义，包含该化合物的组合物，以及制备和使用该化合物的方法。

3. 发明申请

US20080233127A1 IMIDAZOLOPYRIMIDINE ANALOGS AND THEIR USE AS PI3 KINASE AND MTOR INHIBITORS 审中-公开
标题翻译：咪唑吡嗪类似物及其作为PI3激酶和MT抑制剂的用途
公开(公告)号：US20080233127A1
公开(公告)日：2008-09-25
申请号：US12044500
申请日：2008-03-07
申请人： Matthew Gregory Bursavich , Aranapakam Mudumbai Venkatesan , Pawel Wojciech Nowak , Sabrina Lombardi , Adam Matthew Gilbert , Christoph Martin Denhardt , Osvaldo Dos Santos , Efren Guillermo Delos Santos , Natasja Brooijmans , Semiramis Ayral-Kaloustian , Zecheng Chen , Jeroen Cunera Verheijen , Joshua Kaplan , Arie Zask
发明人： Matthew Gregory Bursavich , Aranapakam Mudumbai Venkatesan , Pawel Wojciech Nowak , Sabrina Lombardi , Adam Matthew Gilbert , Christoph Martin Denhardt , Osvaldo Dos Santos , Efren Guillermo Delos Santos , Natasja Brooijmans , Semiramis Ayral-Kaloustian , Zecheng Chen , Jeroen Cunera Verheijen , Joshua Kaplan , Arie Zask
IPC分类号： A61K39/395 , C07D473/00 , A61K31/5377 , A61P35/04 , A61P3/00 , A61P1/00 , A61P29/00 , A61P19/00 , A61K31/52
CPC分类号： C07D473/34
摘要： The present invention relates to Imidazolopyrimidine Analogs, methods of making Imidazolopyrimidine Analogs, compositions comprising an Imidazolopyrimidine Analog, and methods for treating or preventing a PI3K-related disorder comprising administering to a subject in need thereof an effective amount of an Imidazolopyrimidine Analog. The invention also relates to methods for treating or preventing mTOR-related disorders comprising administering to a subject in need thereof an effective amount of an Imidazolopyrimidine Analog.
摘要翻译：本发明涉及咪唑并嘧啶类似物，制备咪唑并嘧啶类似物的方法，包含咪唑并嘧啶类似物的组合物，以及用于治疗或预防PI3K相关病症的方法，其包括向有需要的受试者施用有效量的咪唑并嘧啶类似物。本发明还涉及治疗或预防mTOR相关病症的方法，包括向有需要的受试者施用有效量的咪唑并嘧啶类似物。

4. 发明申请

US20100015141A1 4-PHENOXY-6-ARYL-1H-PYRAZOLO[3,4-D]PYRIMIDINE AND N-ARYL-6-ARYL-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-AMINE COMPOUNDS, THEIR USE AS MTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES 审中-公开
标题翻译： 4-苯基-6-芳基-1H-吡唑并[3,4-D]吡嗪和N-芳基-6-芳基-1H-吡唑并[3,4-D]嘧啶-4-胺化合物，它们作为MTOR KINASE 和PI3激酶抑制剂及其合成
公开(公告)号：US20100015141A1
公开(公告)日：2010-01-21
申请号：US12506291
申请日：2009-07-21
申请人： Matthew Gregory Bursavich , Pawel Wojciech Nowak , David Malwitz , Sabrina Lombardi , Adam Matthew Gilbert , Nan Zhang , Semiramis Ayral-Kaloustian , James Thomas Anderson , Natasja Brooijmans
发明人： Matthew Gregory Bursavich , Pawel Wojciech Nowak , David Malwitz , Sabrina Lombardi , Adam Matthew Gilbert , Nan Zhang , Semiramis Ayral-Kaloustian , James Thomas Anderson , Natasja Brooijmans
IPC分类号： A61K31/519 , C07D487/04 , A61K39/395 , A61P35/00
CPC分类号： C07D487/04
摘要： The invention relates to 4,6-disubstituted-1H-pyrazolo[3,4-d]pyrimidin-4-amine compounds, including 4-phenoxy-6-aryl-1H-pyrazolo[3,4-d]pyrimidine and N-aryl-6-aryl-1H-pyrazolo[3,4-d]pyrimidin-4-amine compounds of the Formula I: or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds.
摘要翻译：本发明涉及4,6-二取代-1H-吡唑并[3,4-d]嘧啶-4-胺化合物，包括4-苯氧基-6-芳基-1H-吡唑并[3,4-d]嘧啶和N- 芳基-6-芳基-1H-吡唑并[3,4-d]嘧啶-4-胺化合物或其药学上可接受的盐，其中组成变量如本文所定义，包含该化合物的组合物和方法用于制造和使用这些化合物。

5. 发明申请

US20090311217A1 3-SUBSTITUTED-1H-INDOLE COMPOUNDS, THEIR USE AS MTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES 审中-公开
标题翻译： 3-取代的1H-吲哚化合物，它们作为MTOR激酶和PI3激酶抑制剂使用，以及它们的合成
公开(公告)号：US20090311217A1
公开(公告)日：2009-12-17
申请号：US12473605
申请日：2009-05-28
申请人： Matthew Gregory Bursavich , Nan Zhang , Semiramis Ayral-Kaloustian , James Thomas Anderson , Thai Hiep Nguyen , Sabrina Lombardi , David Malwitz , Natasja Brooijmans , Derek Cecil Cole , Adam Matthew Gilbert , Pawel Wojciech Nowak , Kaapjoo Park , Sasmita Das , Hwei-Ru Tsou , Aranapakam Mudumbai Venkatesan , Mercy Adufa Otteng , Gary Harold Birnberg , Gloria Jean MacEwan
发明人： Matthew Gregory Bursavich , Nan Zhang , Semiramis Ayral-Kaloustian , James Thomas Anderson , Thai Hiep Nguyen , Sabrina Lombardi , David Malwitz , Natasja Brooijmans , Derek Cecil Cole , Adam Matthew Gilbert , Pawel Wojciech Nowak , Kaapjoo Park , Sasmita Das , Hwei-Ru Tsou , Aranapakam Mudumbai Venkatesan , Mercy Adufa Otteng , Gary Harold Birnberg , Gloria Jean MacEwan
IPC分类号： A61K31/404 , C07D405/02 , C07D403/14 , C07D413/02 , A61K31/496 , A61K31/5377 , A61K38/21 , A61K39/395 , A61P35/00
CPC分类号： C07D405/14 , C07D405/06
摘要： The invention relates to 3-substituted-1H-indole compounds of the Formula I: or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds.
摘要翻译：本发明涉及式I的3-取代-1H-吲哚化合物或其药学上可接受的盐，其中组分变量如本文所定义，包含该化合物的组合物，以及制备和使用该化合物的方法。

6. 发明申请

US20080269213A1 8-Hydroxyquinoline compounds and methods thereof 失效
标题翻译： 8-羟基喹啉化合物及其方法
公开(公告)号：US20080269213A1
公开(公告)日：2008-10-30
申请号：US11895222
申请日：2007-08-23
申请人： Matthew G. Bursavich , Sabrina Lombardi , Adam M. Gilbert , Leif Mark Laakso , Gulnaz Khafizova , David Brian How , Joshua James Sabatini , Phaik-Eng Sum , Jeremy Clemens
发明人： Matthew G. Bursavich , Sabrina Lombardi , Adam M. Gilbert , Leif Mark Laakso , Gulnaz Khafizova , David Brian How , Joshua James Sabatini , Phaik-Eng Sum , Jeremy Clemens
IPC分类号： A61K31/5377 , C07D401/12 , A61K31/4709 , A61K31/47 , A61P9/10 , C07D215/14 , C07D413/02
CPC分类号： C07D215/28 , C07D215/26 , C07D401/06 , C07D401/12 , C07D405/06 , C07D409/10 , C07D417/10
摘要： The present invention relates to 8-Hydroxyquinoline Compounds; compositions comprising an 8-Hydroxyquinoline Compound; and methods for treating or preventing a metalloproteinase-related disorder, such as, an arthritic disorder, osteoarthritis, malignant neoplasm, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, atherosclerosis, age-related macular degeneration, myocardial infarction, a corneal ulceration, an ocular surface disease, hepatitis, an aortic aneurysm, tendonitis, a central nervous system disorder, abnormal wound healing, angiogenesis, restenosis, cirrhosis, multiple sclerosis, glomerulonephritis, graft versus host disease, diabetes, an inflammatory bowel disease, shock, invertebral disc degeneration, stroke, osteopenia or a periodontal disease or comprising administering an effective dose of an 8-Hydroxyquinoline Compound to a mammal in need thereof.
摘要翻译：本发明涉及8-羟基喹啉化合物; 包含8-羟基喹啉化合物的组合物; 以及用于治疗或预防金属蛋白酶相关疾病如关节炎疾病，骨关节炎，恶性肿瘤，类风湿性关节炎，哮喘，慢性阻塞性肺病，动脉粥样硬化，年龄相关性黄斑变性，心肌梗塞，角膜溃疡，眼表疾病，肝炎，主动脉瘤，腱炎，中枢神经系统疾病，伤口愈合异常，血管生成，再狭窄，肝硬化，多发性硬化，肾小球性肾炎，移植物抗宿主病，糖尿病，炎性肠病，休克，椎间盘退变，中风，骨质减少或牙周病，或包括向有需要的哺乳动物施用有效剂量的8-羟基喹啉化合物。

7. 发明申请

US20080125469A1 Thiadiazole compounds and methods of use thereof 审中-公开
标题翻译：噻二唑化合物及其使用方法
公开(公告)号：US20080125469A1
公开(公告)日：2008-05-29
申请号：US11810911
申请日：2007-06-07
申请人： Matthew G. Bursavich , Sabrina Lombardi , Adam M. Gilbert
发明人： Matthew G. Bursavich , Sabrina Lombardi , Adam M. Gilbert
IPC分类号： A61K31/433 , C07D285/14 , A61P35/00 , A61P19/02
CPC分类号： C07D513/10
摘要： The present invention relates to Thiadiazole Compounds; compositions comprising an effective dose of a Thiadiazole Compound; and methods treating or preventing a metalloproteinase-related disorder, such as, an arthritic disorder, osteoarthritis, cancer, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, atherosclerosis, age-related macular degeneration, myocardial infarction, a corneal ulceration, an ocular surface disease, hepatitis, an aortic aneurysm, tendonitis, a central nervous system disorder, abnormal wound healing, angiogenesis, restenosis, cirrhosis, multiple sclerosis, glomerulonephritis, graft versus host disease, diabetes, an inflammatory bowel disease, shock, invertebral disc degeneration, stroke, osteopenia or a periodontal disease or comprising administering an effective dose of a Thiadiazole Compound to a mammal in need thereof.
摘要翻译：本发明涉及噻二唑化合物; 包含有效剂量的噻二唑化合物的组合物; 以及治疗或预防金属蛋白酶相关疾病如关节炎疾病，骨关节炎，癌症，类风湿性关节炎，哮喘，慢性阻塞性肺病，动脉粥样硬化，年龄相关性黄斑变性，心肌梗塞，角膜溃疡，眼表面疾病，肝炎，主动脉瘤，腱炎，中枢神经系统疾病，异常伤口愈合，血管生成，再狭窄，肝硬化，多发性硬化，肾小球性肾炎，移植物抗宿主病，糖尿病，炎性肠病，休克，椎间盘退变，中风，骨质减少或牙周病，或包括向有需要的哺乳动物施用有效剂量的噻二唑化合物。

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