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1. 发明申请

WO2007056582A1 1 H-INDAZOLES, BENZOTHIAZOLES, 1,2-BENZOISOXAZOLES, 1,2-BENZOISOTHIAZOLES, AND CHROMONES AND PREPARATION AND USES THEREOF 审中-公开
标题翻译： 1 H-INDAZOLES，BENZOTHIAZOLES，1,2-BENZOISOXAZOLES，1,2-BENZOISOTHIAZOLES和CHROMONES及其制备及其用途
公开(公告)号：WO2007056582A1
公开(公告)日：2007-05-18
申请号：PCT/US2006/043818
申请日：2006-11-09
申请人： MEMORY PHARMACEUTICALS CORPORATION , SCHUMACHER, Richard A. , MA, Jianguo , HERBERT, Brian , DANCA, Mihaela Diana , XIE, Wenge , NGUYEN, Truc Minh , TEHIM, Ashok
发明人： SCHUMACHER, Richard A. , MA, Jianguo , HERBERT, Brian , DANCA, Mihaela Diana , XIE, Wenge , NGUYEN, Truc Minh , TEHIM, Ashok
IPC分类号： C07D487/08 , A61K31/551 , A61P25/28
CPC分类号： C07D471/08 , C07D487/08
摘要： The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of -disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the α7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
摘要翻译：本发明一般涉及烟碱乙酰胆碱受体（nAChR）的配体领域，nAChR的活化，以及治疗与缺陷或功能异常的烟碱乙酰胆碱受体（特别是脑）有关的疾病病症。此外，本发明涉及作为a7 nAChR亚型的配体的新化合物（吲唑和苯并噻唑），制备这种化合物的方法，含有这些化合物的组合物及其使用方法。

2. 发明申请

WO2010021797A1 CONDENSED HETEROCYCLIC COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY 审中-公开
标题翻译：具有5-HT6受体亲和性的稠合的杂环化合物
公开(公告)号：WO2010021797A1
公开(公告)日：2010-02-25
申请号：PCT/US2009/050799
申请日：2009-07-16
申请人： MEMORY PHARMACEUTICALS CORPORATION , DANCA, Mihaela, Diana , DUNN, Robert , TEHIM, Ashok , XIE, Wenge
发明人： DANCA, Mihaela, Diana , DUNN, Robert , TEHIM, Ashok , XIE, Wenge
IPC分类号： C07D519/00 , A61K31/4985 , A61P25/00 , A61P29/00 , A61P3/00
CPC分类号： C07D519/00
摘要： The present disclosure provides compounds having affinity for the 5-HT 6 receptor which are of the formula (I) wherein R 1 , A, B, D, E, G, Q, Ar, n, m, and p are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
摘要翻译：本公开内容提供了具有式（I）的5-HT 6受体的亲和力的化合物，其中R 1，A，B，D，E，G，Q，Ar，n，m和p如本文所定义。本公开还涉及制备这种化合物的方法，含有这些化合物的组合物及其使用方法。

3. 发明申请

WO2006076592A1 1,3 SUBSTITUTED DIARYL UREAS AS MODULATORS OF KINASE ACTIVITY 审中-公开
标题翻译： 1,3作为激素的调节剂的替代性尿崩症
公开(公告)号：WO2006076592A1
公开(公告)日：2006-07-20
申请号：PCT/US2006/001271
申请日：2006-01-13
申请人： CGI PHARMACEUTICALS, INC. , MITCHELL, Scott A. , DANCA, Mihaela Diana , BLOMGREN, Peter A. , DESIMONE, Robert W. , PIPPIN, Douglas A. I.
发明人： MITCHELL, Scott A. , DANCA, Mihaela Diana , BLOMGREN, Peter A. , DESIMONE, Robert W. , PIPPIN, Douglas A. I.
IPC分类号： C07D401/04 , A61K31/4164 , A61P35/00
CPC分类号： C07D401/04 , C07D401/06
摘要： Certain chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, crystal forms, chelates, non-covalent complexes, prodrugs, and mixtures thereof , are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are also provided herein. Use in treating patients suffering from certain diseases and disorders responsive to angiogenic kinase modulation, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma. A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with at least one chemical entity under conditions that permit detection of activity of the angiogenic kinase, detecting a level of the activity of the angiogenic kinase, and therefrom
摘要翻译：本文提供了选自式1化合物的某些化学实体及其药学上可接受的盐，溶剂合物，结晶形式，螯合物，非共价复合物，前药及其混合物。本文还提供了包含至少一种化学实体和一种或多种药学上可接受的载体的药物组合物，其选自载体，佐剂和赋形剂。用于治疗患有对血管生成激酶调节有反应的某些疾病和病症的患者，其包括向这些患者施用一定量的至少一种有效减少疾病或病症的体征或症状的化学实体。这些疾病包括癌症，包括乳腺肿瘤，子宫内膜癌，结肠癌和颈部鳞状细胞癌。一种用于确定样品中存在或不存在血管生成激酶的方法，包括在允许检测血管生成激酶活性，检测血管生成激酶活性水平的条件下将样品与至少一种化学实体接触

4. 发明申请

WO2010002802A1 PYRROLIDINE-SUBSTITUTED AZAINDOLE COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY 审中-公开
标题翻译：具有5-HT6受体亲和性的吡咯烷 - 取代的唑烷化合物
公开(公告)号：WO2010002802A1
公开(公告)日：2010-01-07
申请号：PCT/US2009/049083
申请日：2009-06-29
申请人： MEMORY PHARMACEUTICALS CORPORATION , DANCA, Mihaela, Diana , DUNN, Robert , TEHIM, Ashok , XIE, Wenge
发明人： DANCA, Mihaela, Diana , DUNN, Robert , TEHIM, Ashok , XIE, Wenge
IPC分类号： C07D401/04 , A61P25/00 , A61K31/437
CPC分类号： C07D401/04
摘要： The present disclosure provides compounds having affinity for the 5-HTg receptor which are of the formula (I): wherein R 1 , R 2 , A, B, D, E, G, Ar, and n are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
摘要翻译：本公开内容提供对式（I）的5-HTg受体具有亲和性的化合物：其中R 1，R 2，A，B，D，E，G，Ar和n如本文所定义。本公开还涉及制备这种化合物的方法，含有这些化合物的组合物及其使用方法。

5. 发明申请

WO2007024294A3 CERTAIN SUBSTITUTED UREAS, AS MODULATORS OF KINASE ACTIVITY 审中-公开
标题翻译：某些替代的UREAS，作为激酶的调节剂
公开(公告)号：WO2007024294A3
公开(公告)日：2007-05-31
申请号：PCT/US2006016916
申请日：2006-05-02
申请人： CGI PHARMACEUTICALS INC , MITCHELL SCOTT A , DANCA MIHAELA DIANA , BLOMGREN PETER , BRITTELLI DAVID , ZHICHKIN PAVEL , VOSS MATTHEW E
发明人： MITCHELL SCOTT A , DANCA MIHAELA DIANA , BLOMGREN PETER , BRITTELLI DAVID , ZHICHKIN PAVEL , VOSS MATTHEW E
IPC分类号： C07D401/06 , A61K31/437 , A61P35/00 , C07D471/04
CPC分类号： C07D471/04 , C07D401/06
摘要： Certain chemical entities chosen from compounds of Formula (1) and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, and prodrugs thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicles chosen from carriers, adjuvants, and excipients, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to angiogenic kinase modulation, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma. Methods of treatment include administering at least one chemical entity as a single active agent or administering such at least one chemical entity in combination with one or more other therapeutic agents. A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with at least one chemical entity under conditions that permit detection of activity of the angiogenic kinase, detecting a level of the activity of the angiogenic kinase, and therefrom determining the presence or absence of the angiogenic kinase in the sample.
摘要翻译：在本文中提供了选自式（1）的化合物的某些化学实体及其药学上可接受的盐，溶剂合物，螯合物，非共价复合物和前药。还提供了包含至少一种化学实体和一种或多种选自载体，佐剂和赋形剂的药学上可接受的载体的药物组合物。公开了治疗患有对血管生成激酶调节反应的某些疾病和病症的患者的方法，其包括向这些患者施用一定量的至少一种有效减少疾病或病症体征或症状的化学实体。这些疾病包括癌症，包括乳腺肿瘤，子宫内膜癌，结肠癌和颈部鳞状细胞癌。治疗方法包括给予至少一种化学实体作为单一活性剂或者与一种或多种其它治疗剂组合施用这样的至少一种化学实体。一种用于确定样品中存在或不存在血管生成激酶的方法，包括在允许检测血管生成激酶活性，检测血管生成激酶活性水平的条件下将样品与至少一种化学实体接触确定样品中存在或不存在血管生成激酶。

6. 发明申请

WO2007038367A1 INDAZOLES, BENZOTHIAZOLES, BENZOISOTHIAZOLES, BENZISOXAZOLES, PYRAZOLOPYRIDINES, ISOTHIAZOLOPYRIDINES, AND PREPARATION AND USES THEREOF 审中-公开
标题翻译：辛唑，苯并噻唑，苯并三唑，苯并咪唑，吡唑并吡啶，异亮氨酸，其制备及用途
公开(公告)号：WO2007038367A1
公开(公告)日：2007-04-05
申请号：PCT/US2006/037142
申请日：2006-09-22
申请人： MEMORY PHARMACEUTICALS CORPORATION , SCHUMACHER, Richard , DANCA, Mihaela Diana , MA, Jianguo , HERBERT, Brian , NGUYEN, Truc Minh , XIE, Wenge , TEHIM, Ashok
发明人： SCHUMACHER, Richard , DANCA, Mihaela Diana , MA, Jianguo , HERBERT, Brian , NGUYEN, Truc Minh , XIE, Wenge , TEHIM, Ashok
IPC分类号： C07D453/02 , A61K31/435 , A61P25/00
CPC分类号： C07D453/02
摘要： The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the α7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
摘要翻译：本发明一般涉及烟碱乙酰胆碱受体（nACh受体）的配体领域，nACh受体的活化以及与缺陷或功能异常的烟碱乙酰胆碱受体，特别是脑的疾病相关的疾病状态的治疗。此外，本发明涉及作为a7 nACh受体亚型的配体的新化合物（例如吲唑和苯并噻唑），制备这些化合物的方法，含有这些化合物的组合物及其使用方法。

7. 发明申请

WO2007024294A2 CERTAIN SUBSTITUTED UREAS, AS MODULATORS OF KINASE ACTIVITY 审中-公开
标题翻译：某些取代的尿素作为激酶活性的调节剂
公开(公告)号：WO2007024294A2
公开(公告)日：2007-03-01
申请号：PCT/US2006/016916
申请日：2006-05-02
申请人： CGI PHARMACEUTICALS, INC. , MITCHELL, Scott, A. , DANCA, Mihaela, Diana , BLOMGREN, Peter , BRITTELLI, David , ZHICHKIN, Pavel , VOSS, Matthew, E.
发明人： MITCHELL, Scott, A. , DANCA, Mihaela, Diana , BLOMGREN, Peter , BRITTELLI, David , ZHICHKIN, Pavel , VOSS, Matthew, E.
CPC分类号： C07D471/04 , C07D401/06
摘要： Certain chemical entities chosen from compounds of Formula (1) and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, and prodrugs thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicles chosen from carriers, adjuvants, and excipients, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to angiogenic kinase modulation, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma. Methods of treatment include administering at least one chemical entity as a single active agent or administering such at least one chemical entity in combination with one or more other therapeutic agents. A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with at least one chemical entity under conditions that permit detection of activity of the angiogenic kinase, detecting a level of the activity of the angiogenic kinase, and therefrom determining the presence or absence of the angiogenic kinase in the sample.
摘要翻译：本文提供了选自式（1）化合物及其药学上可接受的盐，溶剂合物，螯合物，非共价复合物和前药的某些化学实体。本文还提供了包含至少一种化学实体和一种或多种选自载体，佐剂和赋形剂的药学上可接受的载体的药物组合物。公开了治疗患有对血管生成激酶调节有响应的某些疾病和病症的患者的方法，其包括向所述患者施用有效量的至少一种化学实体以减少疾病或病症的体征或症状。这些疾病包括癌症，包括乳腺瘤，子宫内膜癌，结肠癌和颈部鳞状细胞癌。治疗方法包括施用至少一种化学实体作为单一活性剂或施用这种至少一种化学实体与一种或多种其他治疗剂的组合。用于确定样品中血管生成激酶的存在或不存在的方法，包括在允许检测血管生成激酶活性，检测血管生成激酶活性水平的条件下使样品与至少一种化学实体接触，并由此确定样品中血管生成激酶的存在或不存在。

8. 发明申请

WO2006076593A1 1,3-DIARYL SUBSTITUTED UREAS AS MODULATORS OF KINASE ACTIVITY 审中-公开
标题翻译：作为激酶活性调节剂的1,3-DIARYL替代尿素
公开(公告)号：WO2006076593A1
公开(公告)日：2006-07-20
申请号：PCT/US2006/001272
申请日：2006-01-13
申请人： CGI PHARMACEUTICALS, INC. , MITCHELL, Scott A. , DANCA, Mihaela Diana , BLOMGREN, Peter A. , DESIMONE, Robert W. , PIPPIN, Douglas A. I. , BRITTELLI, David R.
发明人： MITCHELL, Scott A. , DANCA, Mihaela Diana , BLOMGREN, Peter A. , DESIMONE, Robert W. , PIPPIN, Douglas A. I. , BRITTELLI, David R.
IPC分类号： C07D401/06 , A61K31/404 , A61P35/04
CPC分类号： C07D401/14 , C07D401/06
摘要： Certain chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, crystal forms, chelates, non-covalent complexes, prodrugs, and mixtures thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are also provided herein. Use in treating patients suffering from certain diseases and disorders responsive to angiogenic kinase modulation, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck sguamous cell carcinoma. A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with at least one chemical entity under conditions that permit detection of activity of the angiogenic kinase, detecting a level of the activity of the angiogenic kinase, and therefrom
摘要翻译：本文提供了选自式1化合物的某些化学实体及其药学上可接受的盐，溶剂合物，结晶形式，螯合物，非共价复合物，前药及其混合物。本文还提供了包含至少一种化学实体和一种或多种药学上可接受的载体的药物组合物，其选自载体，佐剂和赋形剂。用于治疗患有对血管生成激酶调节有反应的某些疾病和病症的患者，其包括向这些患者施用一定量的至少一种有效减少疾病或病症的体征或症状的化学实体。这些疾病包括癌症，包括乳腺肿瘤，子宫内膜癌，结肠癌和颈部鳞状细胞癌。一种用于确定样品中存在或不存在血管生成激酶的方法，包括在允许检测血管生成激酶活性，检测血管生成激酶活性水平的条件下将样品与至少一种化学实体接触

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