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1. 发明申请

US20110318226A1 Calibration slide for fluorescence detection instruments and process of preparation 有权
标题翻译：用于荧光检测仪器的校准载玻片和制备过程
公开(公告)号：US20110318226A1
公开(公告)日：2011-12-29
申请号：US11660469
申请日：2004-11-22
申请人： Yu Ge , Wenjun Yang , Shuying Zhao , Lianghong Guo , Jing Cheng
发明人： Yu Ge , Wenjun Yang , Shuying Zhao , Lianghong Guo , Jing Cheng
IPC分类号： G01N33/00
CPC分类号： G01N21/6452 , G01N21/278 , Y10T436/255
摘要： The present invention relates to calibration slides for fluorescence detection instruments and processing method of making them. The aim of this invention is to disclose calibration slides with high photostability and long lifetime for fluorescence detection instruments. The calibration slides are fabricated by patterning calibration spot arrays of modified inorganic phosphors on the glass slide. The process for producing a calibration slide comprises the following procedure: 1) Dispersing the inorganic phosphors of rare-earth doped complex in water; 2) Patterning the affay of the above suspension on the glass slide. The calibration slides in the present invention employ a very stable fluorescing material that is insensitive to photobleaching, has long lifetime and stability under mild storage condition. The calibration slides in the present invention can be used to calibrate and test for some fluorescence instruments, i.e. microarray scanner, fluorescent microscopy, fluorescence spectrometer, fluorescent multiwell-plate reader
摘要翻译：本发明涉及用于荧光检测仪器的校准载片及其制作方法。本发明的目的是公开具有高荧光检测仪器的高光稳定性和长寿命的校准载玻片。通过在玻璃载片上图案化修饰的无机磷光体的校准点阵列来制造校准载玻片。制备校准载玻片的方法包括以下步骤：1）将稀土掺杂络合物的无机磷光体分散在水中; 2）将上述悬浮液的印刷图案化在玻璃载玻片上。本发明中的校准载玻片使用对光漂白不敏感的非常稳定的荧光材料，在温和储存条件下具有长寿命和稳定性。本发明中的校准载玻片可用于校准和测试一些荧光仪器，即微阵列扫描仪，荧光显微镜，荧光光谱仪，荧光多孔板读数器

2. 发明申请

US20090326251A1 METHODS FOR PREPARING 17-ALKYNYL-7-HYDROXY STEROIDS AND RELATED COMPOUNDS 有权
标题翻译：制备17-烷基-7-羟基甾体和相关化合物的方法
公开(公告)号：US20090326251A1
公开(公告)日：2009-12-31
申请号：US12479626
申请日：2009-06-05
申请人： Steven K. White , Yu Ge , Yujin Huang
发明人： Steven K. White , Yu Ge , Yujin Huang
IPC分类号： C07J1/00
CPC分类号： C07J1/0048 , C07J71/00 , C07J75/00
摘要： The invention relates to processes for preparing 17-alkynyl-7-hydroxy-steroids, such as 17-Ethynyl-10R,13S-dimethyl 2,3,4,7,8R,9S, 10,11,12,13,14S,15,16,17-hexadecahydro-1H-cyclopenta[a]phenanthrene-3R,7R,17S-triol (also referred to as 17α-ethynyl-androst-5-ene-3β,7β,17β-triol), that are essentially free of process impurities having binding activity at nuclear estrogen receptors.
摘要翻译：本发明涉及制备17-炔基-7-羟基甾族化合物的方法，例如17-乙炔基-10R，13S-二甲基2,3,4,7,8R，9S，10,11,12,13,14S， 15,16,17-十六氢-1H-环戊二烯并[a]菲-3R，7R，17S-三醇（也称为17α-乙炔基 - 雄甾-5-烯-3β，7beta，17β-三醇）没有在核雌激素受体上具有结合活性的工艺杂质。

3. 发明申请

US20120214987A1 METHODS AND COMPOUNDS FOR PREPARING 3ALPHA-OXYGEN SUBSTITUTED STEROIDS 审中-公开
标题翻译：制备3ALPHA-氧气取代的甾体的方法和化合物
公开(公告)号：US20120214987A1
公开(公告)日：2012-08-23
申请号：US13327701
申请日：2011-12-15
申请人： Yu Ge , Steven K. White , Yujin Huang
发明人： Yu Ge , Steven K. White , Yujin Huang
IPC分类号： C07J71/00 , C07J3/00
CPC分类号： C07J11/00 , C07J1/0011 , C07J1/0022 , C07J1/0025 , C07J1/0048 , C07J21/003 , C07J41/0038 , C07J51/00 , C07J71/001
摘要： The invention relates to processes for preparing 3α-O-linked steroids including 3α-O-linked-androst-5-ene steroids and 3α-O-linked-5a-androstane steroids. In one process a 3α,4α-epoxy androst-5-en-17-one is predominately reduced at the epoxy moiety wherein reduction of the 3α,4α epoxy functional group occurs preferentially at position C4 with retention of configuration at position C3 to provide a 3α-O-linked-androst-5-ene steroid. In another process, conditions are provided for inversion of configuration of a 3β-hydroxy-androst-5-ene steroid by the Mitsunobu reaction to provide a 3α-O-linked-androst-5-ene steroid with reduced amounts of 3α,5α-cycloandrostane side-product impurities.
摘要翻译：本发明涉及制备包括3α-O-连接的雄甾-5-烯类固醇和3α-O-连接的-5α-雄甾烷类固醇的3α-O-连接的类固醇的方法。在一个方法中，3α，4α-环氧雄甾-5-烯-17-酮在环氧部分主要降低，其中3α，4α环氧官能团的还原优先在位置C4处发生，并保留C3位置上的构型，以提供 3α-O-连接 - 雄甾-5-烯类固醇。在另一种方法中，通过Mitsunobu反应提供3β-羟基 - 雄甾-5-烯类固醇的构型的反转条件，以提供3α-5连接的雄甾-5-烯类固醇，减少量的3α，5α - 环二雄甾烷副产物杂质。

4. 发明申请

US20090258850A1 STABILIZED THERAPEUTIC COMPOSITIONS AND FORMULATIONS 审中-公开
标题翻译：稳定的治疗组合物和制剂
公开(公告)号：US20090258850A1
公开(公告)日：2009-10-15
申请号：US12196271
申请日：2008-08-21
申请人： James M. Frincke , Steven K. White , Yu Ge , Weicheng Liaw , Tao Hu
发明人： James M. Frincke , Steven K. White , Yu Ge , Weicheng Liaw , Tao Hu
IPC分类号： A61K31/5685
CPC分类号： A61K9/10 , A61K9/0019
摘要： The invention relates to pharmaceutically acceptable formulations comprising an active pharmaceutical ingredient such as androst-5-ene-3β,17β-diol, androst-5-ene-3β,7β,17β-triol or derivatives of either of these compounds and an air oxidizable excipient that have been stabilized with respect to efficacy. Use of the efficacy-stabilized formulations to treat a number of conditions or symptoms thereof, such as a symptom associated with exposure to radiation is described.
摘要翻译：本发明涉及包含活性药物成分如雄甾-5-烯-3β，17β-二醇，雄甾-5-烯-3β，7beta，17β-三醇或这些化合物的衍生物的药学上可接受的制剂和可氧化的相关功效已被稳定的赋形剂。描述了使用功效稳定的制剂来治疗许多病症或症状，例如与暴露于辐射相关的症状。

5. 发明授权

US07115624B1 Method of inhibiting protein tyrosine phosphatase 1B and/or T-cell protein tyrosine phosphatase 4 and/or other PTPases with an Asp residue at position 48 失效
标题翻译：抑制第48位Asp蛋白酪氨酸磷酸酶1B和/或T细胞蛋白酪氨酸磷酸酶4和/或其他PTPase的方法
公开(公告)号：US07115624B1
公开(公告)日：2006-10-03
申请号：US09659622
申请日：2000-09-11
申请人： Henrik Sune Andersen , Thomas Kruse Hansen , Lars Fogh Iversen , Jesper Lau , Niels Peter Hundahl Møller , Ole Hvilsted Olsen , Frank Urban Axe , Yu Ge , Daniel Dale Holsworth , Todd Kevin Jones , Luke Milburn Judge , Wiliam Charles Ripka , Barry Zvi Shapira , Roy Teruyuki Uyeda
发明人： Henrik Sune Andersen , Thomas Kruse Hansen , Lars Fogh Iversen , Jesper Lau , Niels Peter Hundahl Møller , Ole Hvilsted Olsen , Frank Urban Axe , Yu Ge , Daniel Dale Holsworth , Todd Kevin Jones , Luke Milburn Judge , Wiliam Charles Ripka , Barry Zvi Shapira , Roy Teruyuki Uyeda
IPC分类号： A01N43/42 , A61K31/44
CPC分类号： A61K31/44
摘要： The present invention provides a method of inhibiting a member of a family of Protein Tyrosine Phosphatases (PTPases, PTPs) such as PTP1B, TC-PTP, CD45, SHP-1, SHP-2, PTPα, PTPε, PTPμ, PTPδ, PTPσ, PTPζ, PTPβ, PTPD1, PTPD2, PTPH1, PTP-MEG1, PTP-LAR, and HePTP by exposing said Ptpase member by administration to a host or otherwise to at least one compound with certain structural, physical and spatial characteristics that allow for the interaction of said compound with specific residues of the active site of PTP1B and/or TC-PTP. These compounds are indicated in the management or treatment of a broad range of diseases such as autoimmune diseases, acute and chronic inflammation, osteoporosis, various forms of cancer and malignant diseases, and type I diabetes and type II diabetes, as well as in the isolation of PTPases and in elucidation or further elucidation of their biological function.
摘要翻译：本发明提供了抑制蛋白酪氨酸磷酸酶（PTPase，PTP）家族成员如PTP1B，TC-PTP，CD45，SHP-1，SHP-2，PTPalpha，PTPepsilon，PTPmu，PTPdelta，PTPsigma， PTPzeta，PTPbeta，PTPD1，PTPD2，PTPH1，PTP-MEG1，PTP-LAR和HePTP，通过将所述Ptpase成员通过给予宿主或以其他方式暴露于至少一种具有允许相互作用的结构，物理和空间特征的化合物的所述化合物与PTP1B和/或TC-PTP的活性位点的特异性残基。这些化合物在管理或治疗广泛的疾病如自身免疫性疾病，急性和慢性炎症，骨质疏松症，各种形式的癌症和恶性疾病以及I型糖尿病和II型糖尿病以及在隔离中被指示的PTPases，并阐明或进一步阐明其生物学功能。

6. 发明授权

US07019026B1 Modulators of Protein Tyrosine Phosphatases (PTPases) 失效
标题翻译：蛋白酪氨酸磷酸酶（PTPases）的调节剂
公开(公告)号：US07019026B1
公开(公告)日：2006-03-28
申请号：US09662457
申请日：2000-09-11
申请人： Henrik Sune Andersen , Thomas Kruse Hansen , Jesper Lau , Niels Peter Hundahl Møller , Ole Hvilsted Olsen , Frank Urban Axe , Yu Ge , Daniel Dale Holsworth , Todd Kevin Jones , Luke Milburn Judge , Wiliam Charles Ripka , Barry Zvi Shapira , Roy Teruyuki Uyeda
发明人： Henrik Sune Andersen , Thomas Kruse Hansen , Jesper Lau , Niels Peter Hundahl Møller , Ole Hvilsted Olsen , Frank Urban Axe , Yu Ge , Daniel Dale Holsworth , Todd Kevin Jones , Luke Milburn Judge , Wiliam Charles Ripka , Barry Zvi Shapira , Roy Teruyuki Uyeda
IPC分类号： A61K31/381 , C07D409/04
CPC分类号： C07D495/04
摘要： Disclosed are novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds of Formula 1 are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPases) such as PTP1B, CD45, SHP-1, SHP-2, PTPα, LAR and HePTP or the like, wherein n, m, X, Y, R1, R2, R3, R4, R5 and R6 are defined more fully in the description. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, and other diseases.
摘要翻译：公开了新的化合物，新组合物，其使用方法及其制备方法，其中式1的这种化合物是蛋白质酪氨酸磷酸酶（PTPase）如PTP1B，CD45，SHP-1，SHP-2， PTPalpha，LAR和HePTP等，其中n，m，X，Y，R 1，R 2，R 3，R 3，在说明书中更完整地定义了SUB 4，R 5和R 6。该化合物可用于治疗I型糖尿病，II型糖尿病，葡萄糖耐量降低，胰岛素抵抗，肥胖症等疾病。

7. 发明授权

US06613903B2 Modulators of protein tyrosine phosphatases (PTPases) 失效
标题翻译：蛋白酪氨酸磷酸酶（PTPases）的调节剂
公开(公告)号：US06613903B2
公开(公告)日：2003-09-02
申请号：US09901367
申请日：2001-07-09
申请人： Henrik Sune Andersen , Thomas Kruse Hansen , Jesper Lau , Niels Peter Hundahl Moller , Ole Hvilsted Olsen , Frank Urban Axe , Farid Bakir , Yu Ge , Daniel Dale Holsworth , Luke Milburn Judge , Michael James Newman , Roy Teruyuki Uyeda , Barry Zvi Shapira
发明人： Henrik Sune Andersen , Thomas Kruse Hansen , Jesper Lau , Niels Peter Hundahl Moller , Ole Hvilsted Olsen , Frank Urban Axe , Farid Bakir , Yu Ge , Daniel Dale Holsworth , Luke Milburn Judge , Michael James Newman , Roy Teruyuki Uyeda , Barry Zvi Shapira
IPC分类号： C07D47102
CPC分类号： C07D495/04 , A61K31/4365
摘要： The present invention provides novel thienopyridines, novel compositions, methods of their use, and methods of their manufacture, where such compounds of Formula 1 are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) including PTP1B, T cell PTP, wherein X, R1, R2, R3, and R4 are defined more fully in the description. The compounds are useful in the treatment of type 1 diabetes, type 2 diabetes, impaired glucose tolerance, insulin resistance, obesity, and other diseases.
摘要翻译：本发明提供新颖的噻吩并吡啶类，其新颖的组合物，使用方法及其制备方法，其中式1化合物是包括PTP1B，T细胞PTP在内的蛋白酪氨酸磷酸酶（PTPase）的药理学有用的抑制剂，其中X， R2，R3和R4在说明书中更全面地定义。该化合物可用于治疗1型糖尿病，2型糖尿病，葡萄糖耐量降低，胰岛素抵抗，肥胖症等疾病。

8. 发明授权

US09163059B2 Methods for preparing 17-alkynyl-7-hydroxy steroids and related compounds-2 有权
标题翻译：制备17-炔基-7-羟基类固醇及相关化合物的方法2
公开(公告)号：US09163059B2
公开(公告)日：2015-10-20
申请号：US13664304
申请日：2012-10-30
申请人： Steven K. White , Yu Ge , Yujin Huang
发明人： Steven K. White , Yu Ge , Yujin Huang
IPC分类号： C07J71/00
CPC分类号： C07J1/0048 , C07J71/00 , C07J75/00
摘要： The invention relates to processes for preparing 17-alkynyl-7-hydroxy-steroids, such as 17-Ethynyl-10R,13S-dimethyl 2,3,4,7,8R,9S,10,11,12,13,14S,15,16,17-hexadecahydro-1H-cyclopenta[a]phenanthrene-3R,7R,17S-triol (also referred to as 17α-ethynyl-androst-5-ene-3β,7β,17β-triol), that are essentially free of process impurities having binding activity at nuclear estrogen receptors.
摘要翻译：本发明涉及制备17-炔基-7-羟基甾族化合物的方法，例如17-乙炔基-10R，13S-二甲基2,3,4,7,8R，9S，10,11,12,13,14S， 15,16,17-十六氢-1H-环戊二烯并[a]菲-3R，7R，17S-三醇（也称为17α-乙炔基 - 雄甾-5-烯-3＆bgr，7＆bgr，17＆bgr三醇）其基本上不含在核雌激素受体上具有结合活性的工艺杂质。

9. 发明授权

US09090594B2 PIM kinase inhibitors and preparation methods and use in medicinal manufacture thereof 有权
标题翻译： PIM激酶抑制剂及其药物制备方法及用途
公开(公告)号：US09090594B2
公开(公告)日：2015-07-28
申请号：US14177156
申请日：2014-02-10
申请人： Yu Ge
发明人： Yu Ge
IPC分类号： C07D403/14 , C07D417/12 , C07D417/14 , A61K31/4439 , A61K31/4545 , C07D471/08 , C07D405/14 , C07D451/02 , C07D453/02 , C07D401/14 , C07D413/14 , C07D451/06 , C07D487/08 , A61K31/549 , A61K31/5395 , C07D403/02 , A61K31/541 , A61K31/5355 , C07D413/12
CPC分类号： C07D403/14 , A61K31/4439 , A61K31/4545 , A61K31/5355 , A61K31/5395 , A61K31/541 , A61K31/549 , C07D401/14 , C07D403/02 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D451/02 , C07D451/06 , C07D453/02 , C07D471/08 , C07D487/08
摘要： PIM kinase inhibitor compound having a structure as represented by Formula I, and isomers, diastereomers, enantiomers, tautomers, and pharmaceutically acceptable salts of the compounds as represented by Formula I. The compounds significantly inhibit the Pim kinase activity and are used to prepare drugs to treat PIM kinase mediated diseases, such as cancers, autoimmune diseases, allergic reactions, or organ transplant rejection. Also provided are methods for preparing the compounds represented by Formula I.
摘要翻译：具有由式I表示的结构的PIM激酶抑制剂化合物，以及由式I表示的化合物的异构体，非对映异构体，对映异构体，互变异构体和药学上可接受的盐。化合物显着抑制Pim激酶活性并用于制备药物治疗PIM激酶介导的疾病，如癌症，自身免疫疾病，过敏反应或器官移植排斥反应。还提供了制备由式I表示的化合物的方法。

10. 发明授权

US08969584B2 PIM kinase inhibitors and preparation methods and use in medicinal manufacture thereof 有权
标题翻译： PIM激酶抑制剂及其药物制备方法及用途
公开(公告)号：US08969584B2
公开(公告)日：2015-03-03
申请号：US14177131
申请日：2014-02-10
申请人： Yu Ge
发明人： Yu Ge
IPC分类号： C07D417/00 , C07D403/14 , C07D417/12 , C07D417/14 , A61K31/4439 , A61K31/4545 , C07D471/08 , C07D405/14 , C07D451/02 , C07D453/02
CPC分类号： C07D403/14 , A61K31/4439 , A61K31/4545 , A61K31/5355 , A61K31/5395 , A61K31/541 , A61K31/549 , C07D401/14 , C07D403/02 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D451/02 , C07D451/06 , C07D453/02 , C07D471/08 , C07D487/08
摘要： A Pim kinase inhibitor compound having the structure represented by Formula I, and isomers, diastereomers, enantiomers, tautomers, and pharmaceutically acceptable salts thereof. The compounds significantly inhibit Pim kinase activity and can be used to prepare drugs for treating Pim kinase mediated diseases, such as cancers, autoimmune diseases, allergic reactions, or organ transplant rejection. Also provided are methods for preparing the compounds represented by Formula I.
摘要翻译：具有由式I表示的结构的Pim激酶抑制剂化合物及其异构体，非对映异构体，对映异构体，互变异构体及其药学上可接受的盐。该化合物显着抑制Pim激酶活性，可用于制备治疗Pim激酶介导的疾病如癌症，自身免疫疾病，过敏反应或器官移植排斥的药物。还提供了制备由式I表示的化合物的方法。

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