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1. 发明公开

US20240252899A1 TRAINING DEVICE 审中-公开
公开(公告)号：US20240252899A1
公开(公告)日：2024-08-01
申请号：US18465064
申请日：2023-09-11
申请人： Michael Pack , Charles Pack
发明人： Michael Pack , Charles Pack
IPC分类号： A63B69/00 , A63B17/04 , A63B63/08
CPC分类号： A63B69/0071 , A63B17/04 , A63B63/083 , A63B2210/50 , A63B2225/055 , A63B2225/09
摘要： A training device for teaching and practicing ball handling skills for basketball players or persons training for sports, the training device including stanchions positionable on a floor using attachment members, such as suction cups, or a flexible resilient layer. A crossbar extends between the stanchions. Flexible elements can be used to connect the stanchions to the suction cups. The lengths of the stanchions and crossbar can be adjustable to set the height of the crossbar above the floor and the separation of the crossbars. Detents can allow for adjustably fixing the lengths.

2. 发明授权

US08440663B2 4-aryl-2-amino-pyrimidines or 4-aryl-2-aminoalkyl-pyrimidines as JAK-2 modulators and methods of use 失效
标题翻译： 4-芳基-2-氨基 - 嘧啶或4-芳基-2-氨基烷基 - 嘧啶作为JAK-2调节剂和使用方法
公开(公告)号：US08440663B2
公开(公告)日：2013-05-14
申请号：US11992224
申请日：2007-01-30
申请人： Grace Mann , Naing Aay , Arlyn Arcalas , S. David Brown , Wai Ki Vicky Chan , Jeff Chen , Hongwang Du , Sergey Epshteyn , Timothy Patrick Forsyth , Adam A. Galan , Tai Phat Huynh , Mohamed Abdulkader Ibrahim , Henry William Beecroft Johnson , Brian Kane , Patrick Kearney , Byung Gyu Kim , Elena S. Koltun , James W. Leahy , Matthew Sangyup Lee , Gary L. Lewis , Lisa E. Meyr , Robin Tammie Noguchi , Michael Pack , Brian Hugh Ridgway , Xian Shi , John Woolfrey , Peiwen Zhou
发明人： Grace Mann , Naing Aay , Arlyn Arcalas , S. David Brown , Wai Ki Vicky Chan , Jeff Chen , Hongwang Du , Sergey Epshteyn , Timothy Patrick Forsyth , Adam A. Galan , Tai Phat Huynh , Mohamed Abdulkader Ibrahim , Henry William Beecroft Johnson , Brian Kane , Patrick Kearney , Byung Gyu Kim , Elena S. Koltun , James W. Leahy , Matthew Sangyup Lee , Gary L. Lewis , Lisa E. Meyr , Robin Tammie Noguchi , Michael Pack , Brian Hugh Ridgway , Xian Shi , John Woolfrey , Peiwen Zhou
IPC分类号： A61K31/535 , C07D239/24 , C07D401/10 , C07D413/10
CPC分类号： C07D239/42 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D417/12 , C07D453/02 , C07D487/04
摘要： This invention relates to certain pyrimidine derivative inhibitors of JAK-2, having Formula (I): wherein D, E, L, Z, R1, R2, R25, and n1 are as defined in the specification, pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof.
摘要翻译：本发明涉及具有式（I）的JAK-2的某些嘧啶衍生物抑制剂：其中D，E，L，Z，R 1，R 2，R 25和n 1如说明书中所定义，其药学上可接受的盐，药物组合物及其使用方法。

3. 发明申请

US20090136428A1 High Throughput Genetic Screening Of Lipid And Cholesterol Processing Using Fluorescent Compounds 有权
标题翻译：使用荧光化合物进行脂质和胆固醇处理的高通量遗传筛选
公开(公告)号：US20090136428A1
公开(公告)日：2009-05-28
申请号：US12362698
申请日：2009-01-30
申请人： Steven Farber , Michael Pack , Marnie Halpern
发明人： Steven Farber , Michael Pack , Marnie Halpern
IPC分类号： A61B10/00
CPC分类号： C12N15/8509 , A01K2217/05 , A01K2217/075 , A01K2227/105 , A01K2227/40 , A01K2267/03 , A01K2267/0362 , A61K49/0004 , G01N21/6428 , G01N2021/6432 , G01N2021/6439
摘要： The present invention utilizes fluorescent lipids, particularly quenched phospholipid or cholesterol analogues, to facilitate screening for phenotypes representing perturbations of lipid and/or cholesterol processing in a vertebrate; screening for genetic mutations that lead to disorders of phospholipid and/or cholesterol metabolism; and screening of compounds designed to treat disorders of phospholipid and/or cholesterol metabolism in the vertebrate.
摘要翻译：本发明利用荧光脂质，特别是淬灭的磷脂或胆固醇类似物，以便于筛选代表脊椎动物脂质和/或胆固醇加工紊乱的表型; 筛选导致磷脂和/或胆固醇代谢紊乱的遗传突变; 以及筛选旨在治疗脊椎动物中磷脂和/或胆固醇代谢紊乱的化合物。

4. 发明授权

US07488467B2 High throughput genetic screening of lipid and cholesterol processing using fluorescent compounds 有权
公开(公告)号：US07488467B2
公开(公告)日：2009-02-10
申请号：US10341538
申请日：2003-01-13
申请人： Steven Farber , Michael Pack , Marnie Halpern
发明人： Steven Farber , Michael Pack , Marnie Halpern
IPC分类号： A61K49/00
CPC分类号： C12N15/8509 , A01K2217/05 , A01K2217/075 , A01K2227/105 , A01K2227/40 , A01K2267/03 , A01K2267/0362 , A61K49/0004 , G01N21/6428 , G01N2021/6432 , G01N2021/6439
摘要： The present invention utilizes fluorescent lipids, particularly quenched phospholipid or cholesterol analogues, to facilitate screening for phenotypes representing perturbations of lipid processing; screening for genetic mutations that lead to disorders of phospholipid and/or cholesterol metabolism; and screening of compounds designed to treat disorders of phospholipid and/or cholesterol metabolism.

5. 发明授权

US11752411B2 Training device 有权
公开(公告)号：US11752411B2
公开(公告)日：2023-09-12
申请号：US17156890
申请日：2021-01-25
申请人： Michael Pack , Charles Pack
发明人： Michael Pack , Charles Pack
IPC分类号： A63B69/00 , A63B63/08 , A63B17/04
CPC分类号： A63B69/0071 , A63B17/04 , A63B63/083 , A63B2210/50 , A63B2225/055 , A63B2225/09
摘要： A training device for teaching and practicing ball handling skills for basketball players or persons training for sports, the training device including stanchions positionable on a floor using attachment members, such as suction cups, or a flexible resilient layer. A crossbar extends between the stanchions. Flexible elements can be used to connect the stanchions to the suction cups. The lengths of the stanchions and crossbar can be adjustable to set the height of the crossbar above the floor and the separation of the crossbars. Detents can allow for adjustably fixing the lengths.

6. 发明授权

US08637499B2 Benzoxazepines as inhibitors of PI3K/mTOR and methods of their use and manufacture 失效
标题翻译：苯并西泮作为PI3K / mTOR的抑制剂及其使用和制造方法
公开(公告)号：US08637499B2
公开(公告)日：2014-01-28
申请号：US13322160
申请日：2010-05-25
申请人： Naing Aay , Arlyn Arcalas , Joerg Bussenius , Steven Charles DeFina , Larisa Dubenko , Jason R. Harris , Eileen E. Jackson-Ugueto , Angie Inyoung Kim , Jean-Claire Limun Manalo , Michael Pack , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang , Owen Joseph Bowles , Jeffry Kimo Curtis
发明人： Naing Aay , Arlyn Arcalas , Joerg Bussenius , Steven Charles DeFina , Larisa Dubenko , Jason R. Harris , Eileen E. Jackson-Ugueto , Angie Inyoung Kim , Jean-Claire Limun Manalo , Michael Pack , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang , Owen Joseph Bowles , Jeffry Kimo Curtis
IPC分类号： A61P35/00 , A61K31/553 , C07D267/14
CPC分类号： C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04
摘要： The invention is directed to Compounds of Formula (I): the invention provides compounds that inhibit, regulate, and/or modulate P13K and/or mTOR that are useful in the treatment of hyperproliferative diseases, such as cancer, in mammals. This invention also provides methods of making the compound methods of using such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and to pharmaceutical compositions containing such compounds. For example, cancer in which activity against PI3fC-alph mTOR, or both contributes to its pathology and/or symptomatology include breast cancer mantle cell lymphoma, renal cell carcinoma, acute myelogenous leukemia, chronic myelogenous leukemia, NPM/ALK-transformed anaplastic large cell lymphoma, diffu large B cell lymphoma, rhabdomyosarcoma, ovarian cancer, endometrial cancer, cervic cancer, non small cell lung carcinoma, small cell lung carcinoma, adenocarcinoma, col cancer, rectal cancer, gastric carcinoma, hepatocellular carcinoma, melanoma, pancreat cancer, prostate carcinoma, thyroid carcinoma, anaplastic large cell lymphoma, hemangiom glioblastoma, or head and neck cancer.
摘要翻译：本发明涉及式（I）的化合物：本发明提供抑制，调节和/或调节P13K和/或mTOR的化合物，其可用于治疗哺乳动物中过度增殖性疾病如癌症。本发明还提供了使用这些化合物在哺乳动物，特别是人类中过度增殖性疾病的治疗方法和含有这些化合物的药物组合物的方法。例如，其中针对PI3fC-alph mTOR或其两者都有助于其病理学和/或症状学的活性的癌症包括乳腺癌套细胞淋巴瘤，肾细胞癌，急性骨髓性白血病，慢性骨髓性白血病，NPM / ALK转化的间变型大细胞淋巴瘤，弥漫性大B细胞淋巴瘤，横纹肌肉瘤，卵巢癌，子宫内膜癌，宫颈癌，非小细胞肺癌，小细胞肺癌，腺癌，胆囊癌，直肠癌，胃癌，肝细胞癌，黑素瘤，胰腺癌，前列腺癌，甲状腺癌，间变性大细胞淋巴瘤，血管瘤胶质母细胞瘤或头颈癌。

7. 发明申请

US20120258953A1 Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their Use and Manufacture 失效
标题翻译：苯并西泮作为PI3K / mTOR的抑制剂及其使用和制造方法
公开(公告)号：US20120258953A1
公开(公告)日：2012-10-11
申请号：US13322160
申请日：2010-05-25
申请人： Naing Aay , Arlyn Arcalas , Joerg Bussenius , Charles Steven Defina , Larisa Dubenko , Jason R. Harris , Eileen E. Jackson-Ugueto , Angie Inyoung Kim , Jean-Claire Limun Manalo , Michael Pack , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang , Owen Joseph Bowles , Jeffry Kimo Curtis
发明人： Naing Aay , Arlyn Arcalas , Joerg Bussenius , Charles Steven Defina , Larisa Dubenko , Jason R. Harris , Eileen E. Jackson-Ugueto , Angie Inyoung Kim , Jean-Claire Limun Manalo , Michael Pack , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang , Owen Joseph Bowles , Jeffry Kimo Curtis
IPC分类号： A61K31/553 , A61P35/02 , A61P35/00 , C07D267/14 , C07D225/02
CPC分类号： C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04
摘要： The invention is directed to Compounds of Formula (I): the invention provides compounds that inhibit, regulate, and/or modulate P13K and/or mTOR that are useful in the treatment of hyperproliferative diseases, such as cancer, in mammals. This invention also provides methods of making the compound methods of using such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and to pharmaceutical compositions containing such compounds. For example, cancer in which activity against PI3fC-alph mTOR, or both contributes to its pathology and/or symptomatology include breast cancer mantle cell lymphoma, renal cell carcinoma, acute myelogenous leukemia, chronic myelogenous leukemia, NPM/ALK-transformed anaplastic large cell lymphoma, diffu large B cell lymphoma, rhabdomyosarcoma, ovarian cancer, endometrial cancer, cervic cancer, non small cell lung carcinoma, small cell lung carcinoma, adenocarcinoma, col cancer, rectal cancer, gastric carcinoma, hepatocellular carcinoma, melanoma, pancreat cancer, prostate carcinoma, thyroid carcinoma, anaplastic large cell lymphoma, hemangiom glioblastoma, or head and neck cancer.
摘要翻译：本发明涉及式（I）的化合物：本发明提供抑制，调节和/或调节P13K和/或mTOR的化合物，其可用于治疗哺乳动物中过度增殖性疾病如癌症。本发明还提供了使用这些化合物在哺乳动物，特别是人类中过度增殖性疾病的治疗方法和含有这些化合物的药物组合物的方法。例如，其中针对PI3fC-alph mTOR或其两者都有助于其病理学和/或症状学的活性的癌症包括乳腺癌套细胞淋巴瘤，肾细胞癌，急性骨髓性白血病，慢性骨髓性白血病，NPM / ALK转化的间变型大细胞淋巴瘤，弥漫性大B细胞淋巴瘤，横纹肌肉瘤，卵巢癌，子宫内膜癌，宫颈癌，非小细胞肺癌，小细胞肺癌，腺癌，胆囊癌，直肠癌，胃癌，肝细胞癌，黑素瘤，胰腺癌，前列腺癌，甲状腺癌，间变性大细胞淋巴瘤，血管瘤胶质母细胞瘤或头颈癌。

8. 发明授权

US08242129B2 6-phenylpyrimidinones as PIM modulators 失效
标题翻译： 6-苯基嘧啶酮作为PIM调节剂
公开(公告)号：US08242129B2
公开(公告)日：2012-08-14
申请号：US12597275
申请日：2008-04-25
申请人： Amy L. Tsuhako , Naing Aay , S. David Brown , Wai Ki Vicky Chan , Hongwang Du , Ping Huang , Brian Kane , Patrick Kearney , Moon Hwan Kim , Elena S. Koltun , Michael Pack , Wei Xu , Peiwen Zhou
发明人： Amy L. Tsuhako , Naing Aay , S. David Brown , Wai Ki Vicky Chan , Hongwang Du , Ping Huang , Brian Kane , Patrick Kearney , Moon Hwan Kim , Elena S. Koltun , Michael Pack , Wei Xu , Peiwen Zhou
IPC分类号： A61K31/505
CPC分类号： C07D213/64 , C07D239/36 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/04 , C07D409/12 , C07D413/04
摘要： A compound having Formula I or II (Formula I) or (Formula II), or a pharmaceutically acceptable salt thereof, wherein X, Z, R1, R2, R11 and R12 are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof.
摘要翻译：具有式I或II（式I）或（式II）的化合物或其药学上可接受的盐，其中X，Z，R 1，R 2，R 11和R 12如说明书中所定义; 其药物组合物; 及其使用方法。

9. 发明授权

US08124056B2 High throughput genetic screening of lipid and cholesterol processing using fluorescent compounds 有权
标题翻译：使用荧光化合物的高通量遗传筛选脂质和胆固醇加工
公开(公告)号：US08124056B2
公开(公告)日：2012-02-28
申请号：US12362698
申请日：2009-01-30
申请人： Steven Farber , Michael Pack , Marnie Halpern
发明人： Steven Farber , Michael Pack , Marnie Halpern
IPC分类号： A61K49/00
CPC分类号： C12N15/8509 , A01K2217/05 , A01K2217/075 , A01K2227/105 , A01K2227/40 , A01K2267/03 , A01K2267/0362 , A61K49/0004 , G01N21/6428 , G01N2021/6432 , G01N2021/6439
摘要： The present invention utilizes fluorescent lipids, particularly quenched phospholipid or cholesterol analogues, to facilitate screening for phenotypes representing perturbations of lipid and/or cholesterol processing in a vertebrate; screening for genetic mutations that lead to disorders of phospholipid and/or cholesterol metabolism; and screening of compounds designed to treat disorders of phospholipid and/or cholesterol metabolism in the vertebrate.
摘要翻译：本发明利用荧光脂质，特别是淬灭的磷脂或胆固醇类似物，以便于筛选代表脊椎动物脂质和/或胆固醇加工紊乱的表型; 筛选导致磷脂和/或胆固醇代谢紊乱的遗传突变; 以及筛选旨在治疗脊椎动物中磷脂和/或胆固醇代谢紊乱的化合物。

10. 发明申请

US20110126300A1 High Through-Put Method of Screening Compounds for Pharmacological Activity 审中-公开
标题翻译：用于药物活性筛选化合物的高通量法
公开(公告)号：US20110126300A1
公开(公告)日：2011-05-26
申请号：US12086948
申请日：2006-12-19
申请人： Michael Pack
发明人： Michael Pack
IPC分类号： A01K67/00 , C40B30/06 , C40B40/02 , A61K31/55 , C07D487/04
CPC分类号： A61K49/0008 , A61K49/0021 , A61K49/0052 , A61K49/0089
摘要： Provided is a method for high through-put screening for physiologic alterations in an altered teleost displaying a phenotype that is characteristic of the alteration and different from a wild-type, unaltered, matched teleost, comprising the steps of contacting the teleost displaying a genetically-inherited or chemically-induced phenotype with at least one test compound for a sufficient time and under suitable conditions to induce a response in the teleost indicative of pharmacological activity of the compound, and detecting and comparing the response with that of a matched, untreated, control, wherein a change in the teleost signal that is different from that of the control, indicates an altered phenotype and pharmacological activity of the at least one test compound. Further provided are the compounds identified by this method, the zebrafish having an altered phenotype resulting from treatment in accordance with these methods, and kits for facilitating the high through-put screening methods.
摘要翻译：本发明提供了一种显示表现型变异和不同于野生型未改变的匹配硬骨转基因的表型的改变的硬骨鱼的生物学改变的高通量筛选方法，包括以下步骤：遗传的或化学诱导的表型与至少一种测试化合物足够的时间和在合适的条件下诱导指示化合物的药理学活性的硬骨中的反应，以及检测和比较匹配的未处理的对照的响应其中所述硬骨架信号与所述对照不同的改变指示所述至少一种测试化合物的改变的表型和药理学活性。进一步提供的是通过该方法鉴定的化合物，斑马鱼具有根据这些方法的治疗产生的改变的表型，以及用于促进高通量筛选方法的试剂盒。

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