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公开(公告)号：WO2009143178A3
公开(公告)日：2010-11-11
申请号：PCT/US2009044556
申请日：2009-05-19
申请人： OMEROS CORP , CUTSHALL NEIL S , GAGE JENNIFER LYNN
IPC分类号： C07D209/42 , C07D213/70 , C07D213/78 , C07D215/36 , C07D235/02 , C07D235/16 , C07D235/28 , C07D239/10 , C07D239/93 , C07D241/24 , C07D249/12 , C07D263/58 , C07D307/68 , C07D319/20 , C07D495/04
CPC分类号： C07D279/16 , C07D209/18 , C07D209/42 , C07D209/86 , C07D213/70 , C07D213/78 , C07D215/22 , C07D215/36 , C07D215/42 , C07D217/02 , C07D235/02 , C07D235/16 , C07D235/28 , C07D239/10 , C07D239/38 , C07D239/93 , C07D239/95 , C07D241/18 , C07D241/24 , C07D249/12 , C07D249/18 , C07D263/58 , C07D277/74 , C07D295/03 , C07D295/14 , C07D307/68 , C07D319/20 , C07D333/24 , C07D495/04
摘要： Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's diseases, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. The compounds have one of the following general structures: wherein m, n, p, x, y, R, R1, R2, R3, R4, R5, R10, A, B and D, are as defined herein, including pharmaceutically acceptable salts, stereoisomers, solvates or prodrugs thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.
摘要翻译： 公开了抑制PDE10的化合物，其可用于治疗各种病症，包括（但不限于）精神病性，焦虑症，运动障碍和/或神经障碍，例如帕金森病，亨廷顿氏病，阿尔茨海默病，脑炎，恐惧症 癫痫，失语症，贝尔麻痹，脑性麻痹，睡眠障碍，疼痛，图雷特综合征，精神分裂症，妄想症，药物诱发的精神病，恐慌和强迫症。 这些化合物具有以下一般结构之一：其中m，n，p，x，y，R，R 1，R 2，R 3，R 4，R 5，R 10，A，B和D如本文所定义，包括药学上可接受的盐 ，立体异构体，溶剂合物或前药。 还公开了含有本发明化合物与药学上可接受的载体的组合物的组合物，以及涉及其在需要其的温血动物中用于抑制PDE10的方法。
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公开(公告)号：WO2010017236A1
公开(公告)日：2010-02-11
申请号：PCT/US2009/052754
申请日：2009-08-04
IPC分类号： A61K31/54
CPC分类号： C07D401/04 , A61K31/15 , A61K31/357 , A61K31/36 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/4184 , A61K31/4196 , A61K31/425 , A61K31/47 , A61K31/5375 , A61K31/54 , C07C243/32 , C07C251/80 , C07C251/86 , C07C251/88 , C07C255/66 , C07C2601/08 , C07D213/56 , C07D213/74 , C07D215/14 , C07D231/12 , C07D235/16 , C07D249/04 , C07D249/08 , C07D257/06 , C07D265/36 , C07D275/02 , C07D295/135 , C07D295/155 , C07D317/62 , C07D319/18 , C07D333/60
摘要： Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.
摘要翻译： 公开了抑制PDE10的化合物，其可用于治疗各种病症，包括（但不限于）精神病性，焦虑症，运动障碍和/或神经障碍，例如帕金森病，亨廷顿氏病，阿尔茨海默病，脑炎，恐惧症 ，癫痫，失语症，贝尔麻痹，脑性麻痹，睡眠障碍，疼痛，图雷特综合征，精神分裂症，妄想症，药物诱发的精神病，恐慌和强迫症。 还提供了化合物的药学上可接受的盐，立体异构体，溶剂合物和前药。 还公开了含有与药学上可接受的载体组合的化合物的组合物，以及涉及其在需要其的温血动物中用于抑制PDE10的方法。
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公开(公告)号：WO2006055525A3
公开(公告)日：2006-05-26
申请号：PCT/US2005/041269
申请日：2005-11-15
申请人： CEPTYR, INC. , BLASKOVICH, Mark A. , BAUGHMAN, Ted , LITTLE, Thomas , PATT, William , QABAR, Maher , SCHULTZ, Lauri , HONG, Feng , NAGULA, Gangadhar , GAGE, Jennifer Lynn , HOWBERT, James Jeffry
发明人： BLASKOVICH, Mark A. , BAUGHMAN, Ted , LITTLE, Thomas , PATT, William , QABAR, Maher , SCHULTZ, Lauri , HONG, Feng , NAGULA, Gangadhar , GAGE, Jennifer Lynn , HOWBERT, James Jeffry
摘要： The present invention provides compounds of Formula (I) and Formula (II) that are useful for modulating the biological activity of the protein tyrosine phosphatase-1b (PTP1B) enzyme. Compounds of this invention can be used to treat diseases and/or conditions in which the PTP1B enzyme is a factor. Such diseases and/or conditions include, but are not limited to, Type 1 diabetes, Type 2 diabetes, inadequate glucose tolerance, insulin resistance, obesity, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, low HDL levels, atherosclerosis, vascular restenosis, inflammatory bowel disease, pancreatitis, adipose cell tumors, adipose cell carcinoma, liposarcoma, dyslipidemia, cancer, and neurodegenerative diseases.
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公开(公告)号：WO2009143178A2
公开(公告)日：2009-11-26
申请号：PCT/US2009/044556
申请日：2009-05-19
IPC分类号： C07D209/42 , C07D213/70 , C07D213/78 , C07D215/36
CPC分类号： C07D279/16 , C07D209/18 , C07D209/42 , C07D209/86 , C07D213/70 , C07D213/78 , C07D215/22 , C07D215/36 , C07D215/42 , C07D217/02 , C07D235/02 , C07D235/16 , C07D235/28 , C07D239/10 , C07D239/38 , C07D239/93 , C07D239/95 , C07D241/18 , C07D241/24 , C07D249/12 , C07D249/18 , C07D263/58 , C07D277/74 , C07D295/03 , C07D295/14 , C07D307/68 , C07D319/20 , C07D333/24 , C07D495/04
摘要： Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's diseases, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. The compounds have one of the following general structures: wherein m, n, p, x, y, R, R 1 , R 2 , R 3 , R 4 , R 5 , R 10 , A, B and D, are as defined herein, including pharmaceutically acceptable salts, stereoisomers, solvates or prodrugs thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.
摘要翻译： 公开了抑制PDE10的化合物，其可用于治疗各种病症，包括（但不限于）精神病性，焦虑症，运动障碍和/或神经障碍，例如帕金森病，亨廷顿氏病，阿尔茨海默病，脑炎，恐惧症 癫痫，失语症，贝尔麻痹，脑性麻痹，睡眠障碍，疼痛，图雷特综合征，精神分裂症，妄想症，药物诱发的精神病，恐慌和强迫症。 这些化合物具有以下一般结构之一：其中m，n，p，x，y，R，R 1，R 2，R 3，R 4，R 5，R 10，A，B和D如本文所定义，包括药学上可接受的盐 ，立体异构体，溶剂合物或前药。 还公开了含有本发明化合物与药学上可接受的载体的组合物的组合物，以及涉及其在需要其的温血动物中用于抑制PDE10的方法。
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公开(公告)号：WO2019231935A1
公开(公告)日：2019-12-05
申请号：PCT/US2019/034225
申请日：2019-05-28
申请人： OMEROS CORPORATION , CUTSHALL, Neil S. , GAGE, Jennifer Lynn , GRUSWITZ, Franz A. , KHALAF, Juhienah , LITTLE, Thomas L. , METZ, Markus , NGUYEN, Jeremiah H. , NOLLERT VON SPECHT, Peter Kurt , TSOUNG, Jennifer , CICIRELLI, Michael , GOLDSTEIN, Sara Rebecca , KESHIPEDDY, Santosh Kumar , KWON, Do Yeon , LEMUS, Robert Huerta , VADDELA, Sudheer Babu
发明人： CUTSHALL, Neil S. , GAGE, Jennifer Lynn , GRUSWITZ, Franz A. , KHALAF, Juhienah , LITTLE, Thomas L. , METZ, Markus , NGUYEN, Jeremiah H. , NOLLERT VON SPECHT, Peter Kurt , TSOUNG, Jennifer , CICIRELLI, Michael , GOLDSTEIN, Sara Rebecca , KESHIPEDDY, Santosh Kumar , KWON, Do Yeon , LEMUS, Robert Huerta , VADDELA, Sudheer Babu
摘要： The present disclosure provides, inter alia , compounds with MASP-2 inhibitory activity, compositions of such compounds and methods of making and using such compounds.
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公开(公告)号：WO2011112828A1
公开(公告)日：2011-09-15
申请号：PCT/US2011/027927
申请日：2011-03-10
申请人： OMEROS CORPORATION , CUTSHALL, Neil, S. , GAGE, Jennifer, Lynn, , WHEELER, Thomas, Neil, , LITTLE, Thomas, L.
IPC分类号： A61K31/33
CPC分类号： C07D307/46 , A61K31/341 , A61K31/415 , A61K31/4155 , A61K31/4192 , A61K31/4196 , A61K31/421 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/433 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/497 , A61K31/5377 , C07D231/12 , C07D285/08 , C07D285/12 , C07D307/34 , C07D307/40 , C07D401/04 , C07D405/10 , C07D407/10 , C07D413/10 , C07D417/10 , Y02A50/465
摘要： Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive- compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.
摘要翻译： 公开了抑制PDE10的化合物，其可用于治疗各种病症，包括（但不限于）精神病性，焦虑症，运动障碍和/或神经障碍，例如帕金森病，亨廷顿氏病，阿尔茨海默病，脑炎，恐惧症 ，癫痫，失语症，贝尔麻痹，脑瘫，睡眠障碍，疼痛，图雷特综合征，精神分裂症，妄想症，药物诱发的精神病，恐慌和强迫症。 还提供了化合物的药学上可接受的盐，立体异构体，溶剂合物和前药。 还公开了含有与药学上可接受的载体组合的化合物的组合物，以及涉及其在需要其的温血动物中用于抑制PDE10的方法。
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公开(公告)号：WO2006055525A2
公开(公告)日：2006-05-26
申请号：PCT/US2005041269
申请日：2005-11-15
申请人： CEPTYR INC , BLASKOVICH MARK A , BAUGHMAN TED , LITTLE THOMAS , PATT WILLIAM , QABAR MAHER , SCHULTZ LAURI , HONG FENG , NAGULA GANGADHAR , GAGE JENNIFER LYNN , HOWBERT JAMES JEFFRY
发明人： BLASKOVICH MARK A , BAUGHMAN TED , LITTLE THOMAS , PATT WILLIAM , QABAR MAHER , SCHULTZ LAURI , HONG FENG , NAGULA GANGADHAR , GAGE JENNIFER LYNN , HOWBERT JAMES JEFFRY
IPC分类号： A61K31/675 , A61K31/66
CPC分类号： C07F9/6541 , C07F9/3808 , C07F9/4006 , C07F9/5721 , C07F9/5728 , C07F9/591 , C07F9/65517
摘要： The present invention provides compounds of Formula (I) and Formula (II) that are useful for modulating the biological activity of the protein tyrosine phosphatase-1b (PTP1B) enzyme. Compounds of this invention can be used to treat diseases and/or conditions in which the PTP1B enzyme is a factor. Such diseases and/or conditions include, but are not limited to, Type 1 diabetes, Type 2 diabetes, inadequate glucose tolerance, insulin resistance, obesity, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, low HDL levels, atherosclerosis, vascular restenosis, inflammatory bowel disease, pancreatitis, adipose cell tumors, adipose cell carcinoma, liposarcoma, dyslipidemia, cancer, and neurodegenerative diseases.
摘要翻译： 本发明提供了可用于调节蛋白酪氨酸磷酸酶-1b（PTP1B）酶的生物学活性的式（I）和式（II）的化合物。 本发明的化合物可用于治疗其中PTP1B酶是因子的疾病和/或病症。 这些疾病和/或病症包括但不限于1型糖尿病，2型糖尿病，葡萄糖耐量不足，胰岛素抵抗，肥胖症，高脂血症，高甘油三酯血症，高胆固醇血症，低HDL水平，动脉粥样硬化，血管再狭窄，炎性肠病， 胰腺炎，脂肪细胞瘤，脂肪细胞癌，脂肪肉瘤，血脂异常，癌症和神经变性疾病。
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