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。

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。

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。

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。

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。

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。

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。