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1. 发明申请

US20080004336A1 CRYSTAL STRUCTURES OF SGLT2 INHIBITORS AND PROCESSES FOR PREPARING SAME 有权
标题翻译： SGLT2抑制剂的晶体结构及其制备方法
公开(公告)号：US20080004336A1
公开(公告)日：2008-01-03
申请号：US11765481
申请日：2007-06-20
申请人： Jack Gougoutas , Hildegard Lobinger , Srividya Ramakrishnan , Prashant Deshpande , Jeffrey Bien , Chiajen Lai , Chenchi Wang , Peter Riebel , John Grosso , Alexandra Nirschl , Janak Singh , John DiMarco
发明人： Jack Gougoutas , Hildegard Lobinger , Srividya Ramakrishnan , Prashant Deshpande , Jeffrey Bien , Chiajen Lai , Chenchi Wang , Peter Riebel , John Grosso , Alexandra Nirschl , Janak Singh , John DiMarco
IPC分类号： C07D309/10 , A61K31/351 , A61P3/00 , A61P3/10
CPC分类号： C07H15/207 , A61K31/7034 , A61K45/06 , A61P3/10 , C07H7/04
摘要： The present invention relates to physical crystal structures of a compound of the formula I: wherein R1, R2, R2a, R3 and R4 are as defined herein, especially pharmaceutical compositions containing structures of compound I or II, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.
摘要翻译：本发明涉及式I化合物的物理结晶结构：其中R 1，R 2，R 2a，R SUP， > 3和R 4如本文所定义的，特别是含有化合物I或II结构的药物组合物，其制备方法，用于制备其的中间体，以及治疗疾病如使用这种结构的糖尿病。

2. 发明申请

US20070003539A1 Phenylglycinamide and pyridylglycinamide derivatives useful as anticoagulants 有权
标题翻译：苯基甘氨酰胺和吡啶基甘氨酰胺衍生物可用作抗凝剂
公开(公告)号：US20070003539A1
公开(公告)日：2007-01-04
申请号：US11472845
申请日：2006-06-22
申请人： Xiaojun Zhang , Alexandra Nirschl , Yan Zou , Eldon Priestley
发明人： Xiaojun Zhang , Alexandra Nirschl , Yan Zou , Eldon Priestley
IPC分类号： A61K38/48
CPC分类号： C07K5/06078 , A61K38/00 , C07D217/22 , C07D237/34 , C07D401/12 , C07K5/06191
摘要： The present invention provides novel phenylglycinamide derivatives of Formula (I) or (IV): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables W, W1, Y, Z, R7, R8, R9, and R11 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.
摘要翻译：本发明提供式（I）或（IV）的新型苯基甘氨酰胺衍生物：或其立体异构体，互变异构体，药学上可接受的盐，溶剂合物或前药，其中变量W，W 1，Y， Z，R 7，R 8，R 9和R 11如本文所定义。这些化合物是可用作药物的因子VIIa的选择性抑制剂。

3. 发明申请

US20050182105A1 Method of using 3-cyano-4-arylpyridine derivatives as modulators of androgen receptor function 审中-公开
标题翻译：使用3-氰基-4-芳基吡啶衍生物作为雄激素受体功能的调节剂的方法
公开(公告)号：US20050182105A1
公开(公告)日：2005-08-18
申请号：US11048437
申请日：2005-02-01
申请人： Alexandra Nirschl , Lawrence Hamann
发明人： Alexandra Nirschl , Lawrence Hamann
IPC分类号： A61K31/44 , A61K31/4439 , A61K45/06
CPC分类号： A61K45/06 , A61K31/44 , A61K31/4439 , A61K2300/00
摘要： A method is provided for treating androgen receptor-associated conditions such as age-related diseases, for example sarcopenia, employing a compound of the structure wherein R1 is CN or H; X is O or S; R2 is alkyl or substituted alkyl, cycloalkyl or substituted cycloalkyl, arylalkyl or substituted arylalkyl, aryl or substituted aryl, or heteroaryl or substituted heteroaryl; R3 and R4 are the same or different and are independently selected from H, C(O)R2a, alkyl or substituted alkyl, cycloalkyl or substituted cycloalkyl, arylalkyl or substituted arylalkyl, aryl or substituted aryl, or heteroaryl or substituted heteroaryl; R2a is alkyl or substituted alkyl, cycloalkyl or substituted cycloalkyl, arylalkyl or substituted arylalkyl, aryl or substituted aryl, or heteroaryl or substituted heteroaryl; G is aryl or heteroaryl, or aryl or heteroaryl substituted with one, two, three, four or five, where possible, of the substituents selected from the group consisting of hydrogen (H), halo, NO2, CN, OR2b, OH, CF3, NR3aR4a; wherein R3a and R4a, and R2b are the same or different and are independently selected from alkyl or substituted alkyl, cycloalkyl or substituted cycloalkyl, arylalkyl or substituted arylalkyl, aryl or substituted aryl, or heteroaryl and substituted heteroaryl; or a pharmaceutically acceptable salt thereof and a prodrug ester thereof.
摘要翻译：提供了一种用于治疗雄激素受体相关病症例如年龄相关疾病，例如肌钙蛋白减少症的方法，使用其中R 1为CN或H的结构的化合物; X是O或S; R 2是烷基或取代的烷基，环烷基或取代的环烷基，芳基烷基或取代的芳基烷基，芳基或取代的芳基或杂芳基或取代的杂芳基; R 3和R 4相同或不同，独立地选自H，C（O）R 2a，烷基或取代的烷基，环烷基或取代的环烷基，芳基烷基或取代的芳基烷基，芳基或取代的芳基，或杂芳基或取代的杂芳基; R 2a是烷基或取代的烷基，环烷基或取代的环烷基，芳烷基或取代的芳基烷基，芳基或取代的芳基或杂芳基或取代的杂芳基; G是芳基或杂芳基，或在可能的情况下用一个，两个，三个，四个或五个取代基取代的芳基或杂芳基，所述取代基选自氢（H），卤素，，CN，OR 2b，OH，CF 3，NR 3a，R 4a，其中R 3a和R 4a和R 2b相同或不同，并且独立地选自烷基或取代的烷基，环烷基或取代的环烷基，芳基烷基或取代的芳基烷基，芳基或取代的芳基，或杂芳基和取代的杂芳基; 或其药学上可接受的盐和其前药酯。

4. 发明申请

US20060166997A1 Phenylglycinamide derivatives useful as anticoagulants 有权
公开(公告)号：US20060166997A1
公开(公告)日：2006-07-27
申请号：US11328479
申请日：2006-01-09
申请人： Xiaojun Zhang , Eldon Priestley , Alexandra Nirschl , Yan Zou
发明人： Xiaojun Zhang , Eldon Priestley , Alexandra Nirschl , Yan Zou
IPC分类号： A61K31/517 , A61K31/502 , A61K31/4745 , A61K31/4709
CPC分类号： C07D401/12 , C07D207/14
摘要： The present invention relates generally to phenylglycinamide derivatives that inhibit serine proteases. In particular it is directed to novel phenylglycinamide derivatives, and analogues thereof, which are useful as selective inhibitors of serine protease enzymes of the coagulation cascade; for example thrombin, factor VIIa, factor Xa, factor XIa, factor IXa, and/or plasma kallikrein. In particular, it relates to compounds that are factor VIIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.

5. 发明授权

US07625923B2 Bicyclic modulators of androgen receptor function 有权
标题翻译：雄激素受体功能的双环调节剂
公开(公告)号：US07625923B2
公开(公告)日：2009-12-01
申请号：US11070808
申请日：2005-03-02
申请人： Alexandra Nirschl , James C. Sutton , Lawrence Hamann , Tammy Wang , Yan Zou , Chongqing Sun
发明人： Alexandra Nirschl , James C. Sutton , Lawrence Hamann , Tammy Wang , Yan Zou , Chongqing Sun
IPC分类号： A61K31/4745 , C07D491/02
CPC分类号： C07D487/04 , C07D498/04 , C07D513/04
摘要： The present invention relates to bicyclic compounds according to formula I, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of androgen receptor-associated conditions, such as age-related diseases, for example sarcopenia, wherein R1, R2, R5, X, Y and n are defined herein.
摘要翻译：本发明涉及式I的双环化合物，含有这些化合物的药物组合物和使用这些化合物治疗雄激素受体相关病症如年龄相关疾病，例如肌肉减少症的方法，其中R1，R2，R5 ，X，Y和n如本文所定义。

6. 发明申请

US20060111413A1 2-Amino-3-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors 有权
标题翻译： 2-氨基-3-官能化的四氢化萘衍生物和相关的糖原磷酸化酶抑制剂
公开(公告)号：US20060111413A1
公开(公告)日：2006-05-25
申请号：US11273167
申请日：2005-11-14
申请人： Philip Sher , Gang Wu , Wei Meng , Alexandra Nirschl , William Washburn , Terry Stouch
发明人： Philip Sher , Gang Wu , Wei Meng , Alexandra Nirschl , William Washburn , Terry Stouch
IPC分类号： A61K31/4184 , A61K31/407 , C07D498/02 , C07D407/02
CPC分类号： C07D209/42 , C07D235/24 , C07D401/12 , C07D403/12 , C07D405/12 , C07D491/04 , C07D493/08 , C07D495/04
摘要： Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hyperglycemia, impaired glucose tolerance, insulin resistance and hyperinsulinemia), the microvascular complications associated with diabetes (such as retinopathy, neuropathy, nephropathy and delayed wound healing), the macrovascular complications associated with diabetes (cardiovascular diseases such as atherosclerosis, abnormal heart function, myocardial ischemia and stroke), as well as Metabolic Syndrome and its component conditions including hypertension, obesity and dislipidemia (including hypertriglyceridemia, hypercholesterolemia and low HDL), and other maladies such as non-cardiac ischemia, infection and cancer. These novel compounds have the structure or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W, R1, R2, X, Y and Z are defined herein.
摘要翻译：提供了新型化合物，其是可用于治疗，预防或减缓需要糖原磷酸化酶抑制剂治疗（如糖尿病和相关病症（如高血糖，葡萄糖耐量异常，胰岛素抵抗和高胰岛素血症））的疾病进展的糖原磷酸化酶抑制剂，微血管与糖尿病相关的并发症（如视网膜病变，神经病变，肾病和延迟伤口愈合），与糖尿病相关的大血管并发症（心血管疾病如动脉粥样硬化，心脏功能异常，心肌缺血和中风）以及代谢综合征及其组成条件包括高血压，肥胖和血脂异常（包括高甘油三酯血症，高胆固醇血症和低HDL）以及其他疾病如非心脏缺血，感染和癌症。这些新化合物具有其结构或立体异构体或前药或其药学上可接受的盐，其中W，R 1，R 2，X，Y和Z在本文中定义。

7. 发明申请

US20060111338A1 2-Amino-4-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors 有权
标题翻译： 2-氨基-4-官能化的四氢化萘衍生物和相关的糖原磷酸化酶抑制剂
公开(公告)号：US20060111338A1
公开(公告)日：2006-05-25
申请号：US11272845
申请日：2005-11-14
申请人： Philip Sher , Alexandra Nirschl , Wei Meng , William Washburn
发明人： Philip Sher , Alexandra Nirschl , Wei Meng , William Washburn
IPC分类号： A61K31/4709 , A61K31/4184 , A61K31/407 , C07D403/14
CPC分类号： C07D401/12 , C07D209/42 , C07D403/12
摘要： Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hyperglycemia, impaired glucose tolerance, insulin resistance and hyperinsulinemia), the microvascular complications associated with diabetes (such as retinopathy, neuropathy, nephropathy and delayed wound healing), the macrovascular complications associated with diabetes (cardiovascular diseases such as atherosclerosis, abnormal heart function, myocardial ischemia and stroke), as well as Metabolic Syndrome and its component conditions including hypertension, obesity and dislipidemia (including hypertriglyceridemia, hypercholesterolemia and low HDL), and other maladies such as non-cardiac ischemia, infection and cancer. These novel compounds have the structure or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W, R1, R2, X and Z are defined herein.
摘要翻译：提供了新型化合物，其是可用于治疗，预防或减缓需要糖原磷酸化酶抑制剂治疗（如糖尿病和相关病症（如高血糖，葡萄糖耐量异常，胰岛素抵抗和高胰岛素血症））的疾病进展的糖原磷酸化酶抑制剂，微血管与糖尿病相关的并发症（如视网膜病变，神经病变，肾病和延迟伤口愈合），与糖尿病相关的大血管并发症（心血管疾病如动脉粥样硬化，心脏功能异常，心肌缺血和中风）以及代谢综合征及其组成条件包括高血压，肥胖和血脂异常（包括高甘油三酯血症，高胆固醇血症和低HDL）以及其他疾病如非心脏缺血，感染和癌症。这些新化合物具有其结构或立体异构体或前药或其药学上可接受的盐，其中W，R 1，R 2，X和Z在本文中定义。

8. 发明申请

US20050197359A1 Bicyclic modulators of androgen receptor function 有权
标题翻译：雄激素受体功能的双环调节剂
公开(公告)号：US20050197359A1
公开(公告)日：2005-09-08
申请号：US11070808
申请日：2005-03-02
申请人： Alexandra Nirschl , James Sutton , Lawrence Hamann , Tammy Wang , Yan Zou , Chongqing Sun
发明人： Alexandra Nirschl , James Sutton , Lawrence Hamann , Tammy Wang , Yan Zou , Chongqing Sun
IPC分类号： A61K31/424 , A61K31/425 , A61K31/428 , A61K31/44 , A61K31/4745 , C07D263/60 , C07D471/02 , C07D491/02 , C07D498/02
CPC分类号： C07D487/04 , C07D498/04 , C07D513/04
摘要： The present invention relates to bicyclic compounds according to formula I, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of androgen receptor-associated conditions, such as age-related diseases, for example sarcopenia, wherein R1, R2, R5, X, Y and n are defined herein.
摘要翻译：本发明涉及式I的双环化合物，含有这些化合物的药物组合物和使用这些化合物治疗雄激素受体相关病症例如年龄相关疾病，例如肌肉减少症的方法，其中R 1 R 2，R 5，X，Y和n在本文中定义。

9. 发明申请

US20050187267A1 Sulfonylpyrrolidine modulators of androgen receptor function and method 有权
公开(公告)号：US20050187267A1
公开(公告)日：2005-08-25
申请号：US11048439
申请日：2005-02-01
申请人： Lawrence Hamann , Yingzhi Bi , Mark Manfredi , Alexandra Nirschl , James Sutton
发明人： Lawrence Hamann , Yingzhi Bi , Mark Manfredi , Alexandra Nirschl , James Sutton
IPC分类号： A61K31/4015 , A61K31/433 , C07D207/48 , C07D285/06 , C07D285/14 , C07D498/04
CPC分类号： C07D285/14 , C07D207/48
摘要： Compounds are provided which are useful in the treatment of androgen receptor-associated conditions, such as age-related diseases, which compounds have the structure wherein R1 is hydrogen (H), alkyl or substituted alkyl, alkenyl or substituted alkenyl, arylalkyl or substituted arylalkyl, CO2R4a, CONR4aR4b, and CH2OR4a; R2 is hydrogen (H), OR3, SR3, halo, NHR3, NHCOR4c1, NHCO2R4c1, NHCONR4cR4d and NHSO2R4c; R3 in each functional group is hydrogen (H), alkyl or substituted alkyl, CHF2, CF3 and CON4e; R4, R4a, R4b, R4c, R4c1, R4d, R4e, R4f, R4g, or R4h in each functional group are the same or different and are hydrogen(H), alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, arylalkyl or substituted arylalkyl, aryl or substituted aryl, or heteroaryl or substituted heteroaryl; R5 and R5′ are the same or different and are hydrogen(H), alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, arylalkyl or substituted arylalkyl, aryl or substituted aryl, or heteroaryl or substituted heteroaryl, wherein at least one of R5 and R5′ is hydrogen, or R5 and R5′ taken together form a double bond with oxygen (O), sulfur (S), NR7 or CR7R7′; where R7 and R7′ are as defined herein; G is an aryl, heterocyclo or heteroaryl group, wherein said group is mono- or polycyclic, and which is optionally substituted; and n is an integer of 1 or 2, m is an integer of 1 or 2, Z is oxygen (—O—) or NR4h, a prodrug ester, all stereoisomers thereof and a pharmaceutically acceptable salt. A method for treating androgen receptor-associated conditions such as age-related diseases is also provided.

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