公开(公告)号：US20100048547A1

公开(公告)日：2010-02-25

申请号：US12449286

申请日：2008-02-06

Applicant: Gordana Atallah ,  Sarah Bartulis ,  Matthew Burger ,  Hanne Merritt ,  Simon Ng ,  Zhi-Jie Ni ,  Sabina Pecchi ,  Keith B. Pfister ,  Aaron Smith ,  Charles Voliva ,  Allan Wagman ,  Yanchen Zhang

Inventor： Gordana Atallah ,  Sarah Bartulis ,  Matthew Burger ,  Hanne Merritt ,  Simon Ng ,  Zhi-Jie Ni ,  Sabina Pecchi ,  Keith B. Pfister ,  Aaron Smith ,  Charles Voliva ,  Allan Wagman ,  Yanchen Zhang

IPC: A61K31/5377 ,  C07D413/14 ,  A61K31/538 ,  A61P29/00 ,  A61P35/00 ,  A61P11/00 ,  A61P37/08 ,  A61P37/00 ,  A61P9/00

CPC classification number: C07D401/14 ,  C07D401/04 ,  C07D405/14 ,  C07D413/14

Abstract: Phosphatidylinositol (PI) 3-kinase inhibitor compounds, their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases, including proliferative diseases, inflammatory and obstructive airways diseases, allergic conditions, autoimmune and cardiovascular diseases.

Abstract translation: 磷脂酰肌醇（PI）3-激酶抑制剂化合物，其药学上可接受的盐和前药; 单独或与至少一种另外的治疗剂组合的新化合物与药学上可接受的载体的组合物; 以及单独或与至少一种另外的治疗剂组合的新化合物在预防或治疗特征在于生长因子异常活性，蛋白质丝氨酸/苏氨酸激酶和磷脂激酶（包括增殖性疾病）的疾病中的用途， 炎性和阻塞性气道疾病，过敏性疾病，自身免疫性疾病和心血管疾病。

公开(公告)号：US20060089369A1

公开(公告)日：2006-04-27

申请号：US11220400

申请日：2005-09-06

Applicant: John Nuss ,  Stephen Harrison ,  David Ring ,  Rustum Boyce ,  Kirk Johnson ,  Keith Pfister ,  Savithri Ramurthy ,  Lynn Seely ,  Allan Wagman ,  Manoj Desai ,  Barry Levine

Inventor： John Nuss ,  Stephen Harrison ,  David Ring ,  Rustum Boyce ,  Kirk Johnson ,  Keith Pfister ,  Savithri Ramurthy ,  Lynn Seely ,  Allan Wagman ,  Manoj Desai ,  Barry Levine

IPC: A61K31/52 ,  A61K31/497 ,  A61K31/4439 ,  A61K31/506 ,  C07D473/12 ,  C07D401/02 ,  C07D403/02 ,  C07D405/02 ,  C07D409/02

CPC classification number: C07D213/74 ,  C07D213/75 ,  C07D213/80 ,  C07D213/85 ,  C07D239/42 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

Abstract: New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.

公开(公告)号：US20050054663A1

公开(公告)日：2005-03-10

申请号：US10917707

申请日：2004-08-13

Applicant: Christina Bennett ,  Kurt Hankenson ,  Stephen Harrison ,  Kenneth Longo ,  Ormond MacDougald ,  Allan Wagman

Inventor： Christina Bennett ,  Kurt Hankenson ,  Stephen Harrison ,  Kenneth Longo ,  Ormond MacDougald ,  Allan Wagman

IPC: A61K31/506 ,  A61K33/06 ,  A61K38/29 ,  A61K45/06 ,  A61K31/513

CPC classification number: A61K31/535 ,  A61K31/505 ,  A61K31/506 ,  A61K33/06 ,  A61K38/29 ,  A61K45/06 ,  A61K2300/00

Abstract: This invention relates to methods of treating or preventing bone loss by administering to a human or animal subject pyrimidine and pyridine derivatives that inhibit the activity of glycogen synthase kinase 3 (GSK3), to pharmaceutical compositions containing the compounds, and to the use of the compounds and compositions alone or in combination with other pharmaceutically active agents.

Abstract translation: 本发明涉及通过向人或动物施用抑制糖原合酶激酶3（GSK3）的活性的嘧啶和吡啶衍生物，含有该化合物的药物组合物以及使用该化合物来治疗或预防骨丢失的方法 单独或与其它药物活性剂组合的组合物。

公开(公告)号：US08173647B2

公开(公告)日：2012-05-08

申请号：US12449286

申请日：2008-02-06

Applicant: Gordana Atallah ,  Sarah Bartulis ,  Matthew Burger ,  Hanne Merritt ,  Simon Ng ,  Zhi-Jie Ni ,  Sabina Pecchi ,  Keith B. Pfister ,  Aaron Smith ,  Charles Voliva ,  Allan Wagman ,  Yanchen Zhang

Inventor： Gordana Atallah ,  Sarah Bartulis ,  Matthew Burger ,  Hanne Merritt ,  Simon Ng ,  Zhi-Jie Ni ,  Sabina Pecchi ,  Keith B. Pfister ,  Aaron Smith ,  Charles Voliva ,  Allan Wagman ,  Yanchen Zhang

IPC: A61K31/5377 ,  C07D413/14

CPC classification number: C07D401/14 ,  C07D401/04 ,  C07D405/14 ,  C07D413/14

Abstract: Phosphatidylinositol (PI) 3-kinase inhibitor compounds, their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases, including proliferative diseases, inflammatory and obstructive airways diseases, allergic conditions, autoimmune and cardiovascular diseases.

Abstract translation: 磷脂酰肌醇（PI）3-激酶抑制剂化合物，其药学上可接受的盐和前药; 单独或与至少一种另外的治疗剂组合的新化合物与药学上可接受的载体的组合物; 以及单独或与至少一种另外的治疗剂组合的新化合物在预防或治疗特征在于生长因子异常活性，蛋白质丝氨酸/苏氨酸激酶和磷脂激酶（包括增殖性疾病）的疾病中的用途， 炎性和阻塞性气道疾病，过敏性疾病，自身免疫性疾病和心血管疾病。

公开(公告)号：US20080045528A1

公开(公告)日：2008-02-21

申请号：US11737069

申请日：2007-04-18

Applicant: James Sutton ,  Marion Wiesmann ,  Weibo Wang ,  Mika Lindvall ,  Jiong Lan ,  Savithri Ramurthy ,  Anu Sharma ,  Elizabeth Mieuli ,  Liana Klivansky ,  William Lenahan ,  Susan Kaufman ,  Hong Yang ,  Simon Ng ,  Keith Pfister ,  Allan Wagman ,  Victoria Sung ,  Martin Sendzik

Inventor： James Sutton ,  Marion Wiesmann ,  Weibo Wang ,  Mika Lindvall ,  Jiong Lan ,  Savithri Ramurthy ,  Anu Sharma ,  Elizabeth Mieuli ,  Liana Klivansky ,  William Lenahan ,  Susan Kaufman ,  Hong Yang ,  Simon Ng ,  Keith Pfister ,  Allan Wagman ,  Victoria Sung ,  Martin Sendzik

IPC: A61K31/535 ,  A61K31/44 ,  A61K31/445 ,  C07D211/00 ,  C07D413/00 ,  C07D417/00 ,  C07D401/00 ,  A61P43/00 ,  A61K31/497

CPC classification number: C07D413/12 ,  C07D417/12

Abstract: Benzoxazole and benzothiazole compounds and the stereoisomers, tautomers, solvates, oxides, esters, and prodrugs thereof and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF-1R.

Abstract translation: 公开了苯并恶唑和苯并噻唑化合物及其立体异构体，互变异构体，溶剂合物，氧化物，酯和前药及其药学上可接受的盐。 还公开了单独或与至少一种另外的治疗剂组合的化合物与药学上可接受的载体的组合，以及化合物单独或与至少一种另外的治疗剂组合的用途。 这些实施方案可用于抑制细胞增殖，抑制肿瘤的生长和/或复分解，治疗或预防癌症，治疗或预防退行性骨疾病如类风湿性关节炎和/或抑制分子如CSF-1R。

公开(公告)号：US08563549B2

公开(公告)日：2013-10-22

申请号：US13471111

申请日：2012-05-14

Applicant: Matthew Burger ,  Zhi-Jie Ni ,  Sabina Pecchi ,  Gordana Ataliah ,  Sarah Bartulis ,  Kelly Frazier ,  Aaron Smith ,  Joelle Verhagen ,  Yanchen Zhang ,  Allan Wagman ,  Simon Ng ,  Keith Pfister ,  Daniel J. Poon ,  Alicia Louie ,  Teresa Pick ,  Paul Barsanti ,  Edwin Iwanowicz ,  Wendy Fantl ,  Thomas Hendrickson ,  Mark Knapp ,  Hanne Meritt ,  Charles Voliva ,  Marion Wiesmann ,  Xiahua Xin

Inventor： Matthew Burger ,  Zhi-Jie Ni ,  Sabina Pecchi ,  Gordana Ataliah ,  Sarah Bartulis ,  Kelly Frazier ,  Aaron Smith ,  Joelle Verhagen ,  Yanchen Zhang ,  Allan Wagman ,  Simon Ng ,  Keith Pfister ,  Daniel J. Poon ,  Alicia Louie ,  Teresa Pick ,  Paul Barsanti ,  Edwin Iwanowicz ,  Wendy Fantl ,  Thomas Hendrickson ,  Mark Knapp ,  Hanne Meritt ,  Charles Voliva ,  Marion Wiesmann ,  Xiahua Xin

IPC: A61K31/535 ,  C07D413/14

CPC classification number: C07D401/04 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D417/12

Abstract: Phosphatidylinositol (PI) 3-kinase inhibitor compounds (I), their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases.

Abstract translation: 磷脂酰肌醇（PI）3-激酶抑制剂化合物（I），其药学上可接受的盐和前药; 单独或与至少一种另外的治疗剂组合的新化合物与药学上可接受的载体的组合物; 以及单独或与至少一种另外的治疗剂组合的新化合物在预防或治疗以生长因子，蛋白质丝氨酸/苏氨酸激酶和磷脂激酶异常活性为特征的增殖性疾病中的用途。

公开(公告)号：US20070244197A1

公开(公告)日：2007-10-18

申请号：US11417346

申请日：2006-05-03

Applicant: Niels Andersen ,  Jason Bowman ,  Alice Erwin ,  Eric Harwood ,  Toni Kline ,  Khisimuzi Mdluli ,  Simon Ng ,  Keith Pfister ,  Ribhi Shawar ,  Allan Wagman ,  Asha Yabannavar

Inventor： Niels Andersen ,  Jason Bowman ,  Alice Erwin ,  Eric Harwood ,  Toni Kline ,  Khisimuzi Mdluli ,  Simon Ng ,  Keith Pfister ,  Ribhi Shawar ,  Allan Wagman ,  Asha Yabannavar

IPC: A61K31/19 ,  C07C259/04

CPC classification number: C07D453/00 ,  C07C233/83 ,  C07C239/16 ,  C07C251/40 ,  C07C255/24 ,  C07C255/25 ,  C07C255/44 ,  C07C255/57 ,  C07C259/06 ,  C07C275/14 ,  C07C275/16 ,  C07C275/26 ,  C07C279/14 ,  C07C311/06 ,  C07C311/08 ,  C07C311/19 ,  C07C311/21 ,  C07C317/32 ,  C07C323/25 ,  C07C323/41 ,  C07C323/60 ,  C07C323/62 ,  C07C335/08 ,  C07C337/08 ,  C07C381/00 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/42 ,  C07C2603/74 ,  C07D207/08 ,  C07D207/09 ,  C07D207/14 ,  C07D207/16 ,  C07D207/27 ,  C07D207/327 ,  C07D211/26 ,  C07D211/42 ,  C07D211/56 ,  C07D211/58 ,  C07D211/62 ,  C07D213/38 ,  C07D213/40 ,  C07D213/54 ,  C07D213/56 ,  C07D213/61 ,  C07D213/74 ,  C07D213/80 ,  C07D213/81 ,  C07D213/82 ,  C07D215/48 ,  C07D217/26 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D235/14 ,  C07D239/26 ,  C07D239/42 ,  C07D241/04 ,  C07D241/12 ,  C07D241/18 ,  C07D263/34 ,  C07D285/01 ,  C07D295/13 ,  C07D295/135 ,  C07D295/155 ,  C07D295/192 ,  C07D295/215 ,  C07D307/68 ,  C07D311/24 ,  C07D317/60 ,  C07D317/68 ,  C07D333/20 ,  C07D333/24 ,  C07D333/32 ,  C07D333/36 ,  C07D333/58

Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.

Abstract translation: 提供式I的抗菌化合物：以及立体异构体，其药学上可接受的盐，酯和前药; 包含这些化合物的药物组合物; 通过施用这些化合物治疗细菌感染的方法; 和化合物的制备方法。

公开(公告)号：US20120225859A1

公开(公告)日：2012-09-06

申请号：US13471111

申请日：2012-05-14

Applicant: Matthew BURGER ,  Zhi-Jie NI ,  Sabina PECCHI ,  Gordana ATALLAH ,  Sarah BARTULIS ,  Kelly FRAZIER ,  Aaron SMITH ,  Joelle VERHAGEN ,  Yanchen ZHANG ,  Allan WAGMAN ,  Simon NG ,  Keith PFISTER ,  Daniel POON ,  Alicia LOUIE ,  Teresa PICK ,  Paul BARSANTI ,  Edwin IWANOWICZ ,  Wendy FANTL ,  Thomas HENDRICKSON ,  Mark KNAPP ,  Hanne MERRITT ,  Charles VOLIVA ,  Marion WIESMANN ,  Xiaohua XIN

Inventor： Matthew BURGER ,  Zhi-Jie NI ,  Sabina PECCHI ,  Gordana ATALLAH ,  Sarah BARTULIS ,  Kelly FRAZIER ,  Aaron SMITH ,  Joelle VERHAGEN ,  Yanchen ZHANG ,  Allan WAGMAN ,  Simon NG ,  Keith PFISTER ,  Daniel POON ,  Alicia LOUIE ,  Teresa PICK ,  Paul BARSANTI ,  Edwin IWANOWICZ ,  Wendy FANTL ,  Thomas HENDRICKSON ,  Mark KNAPP ,  Hanne MERRITT ,  Charles VOLIVA ,  Marion WIESMANN ,  Xiaohua XIN

IPC: A61K31/5377 ,  C07D413/14 ,  C12N5/07 ,  A61K31/553 ,  A61K31/541 ,  C07D471/08 ,  A61P35/00 ,  A61K31/538

CPC classification number: C07D401/04 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D417/12

Abstract: Phosphatidylinositol (PI) 3-kinase inhibitor compounds (I), their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases.

Abstract translation: 磷脂酰肌醇（PI）3-激酶抑制剂化合物（I），其药学上可接受的盐和前药; 单独或与至少一种另外的治疗剂组合的新化合物与药学上可接受的载体的组合物; 以及单独或与至少一种另外的治疗剂组合的新化合物在预防或治疗以生长因子，蛋白质丝氨酸/苏氨酸激酶和磷脂激酶异常活性为特征的增殖性疾病中的用途。

公开(公告)号：US20100249126A1

公开(公告)日：2010-09-30

申请号：US12161537

申请日：2007-01-22

Applicant: Matthew Burger ,  Zhi-Jie Ni ,  Sabina Pecchi ,  Gordana Atallah ,  Sarah Bartulis ,  Kelly Frazier ,  Aaron Smith ,  Joelle Verhagen ,  Yanchen Zhang ,  Allan Wagman ,  Simon Ng ,  Keith Pfister ,  Daniel J. Poon ,  Alicia Louie ,  Teresa Pick ,  Paul Barsanti ,  Edwin Iwanowicz ,  Wendy Fantl ,  Thomas Hendrickson ,  Mark Knapp ,  Hanne Meritt ,  Charles Voliva ,  Marion Wiesmann ,  Xiahua Xin

Inventor： Matthew Burger ,  Zhi-Jie Ni ,  Sabina Pecchi ,  Gordana Atallah ,  Sarah Bartulis ,  Kelly Frazier ,  Aaron Smith ,  Joelle Verhagen ,  Yanchen Zhang ,  Allan Wagman ,  Simon Ng ,  Keith Pfister ,  Daniel J. Poon ,  Alicia Louie ,  Teresa Pick ,  Paul Barsanti ,  Edwin Iwanowicz ,  Wendy Fantl ,  Thomas Hendrickson ,  Mark Knapp ,  Hanne Meritt ,  Charles Voliva ,  Marion Wiesmann ,  Xiahua Xin

IPC: A61K31/5377 ,  C07D413/14 ,  A61P35/00

CPC classification number: C07D401/04 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D417/12

Abstract: Phosphatidylinositol (PI) 3-kinase inhibitor compounds (I), their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases.

Abstract translation: 磷脂酰肌醇（PI）3-激酶抑制剂化合物（I），其药学上可接受的盐和前药; 单独或与至少一种另外的治疗剂组合的新化合物与药学上可接受的载体的组合物; 以及单独或与至少一种另外的治疗剂组合的新化合物在预防或治疗以生长因子，蛋白质丝氨酸/苏氨酸激酶和磷脂激酶异常活性为特征的增殖性疾病中的用途。

公开(公告)号：US20070244109A1

公开(公告)日：2007-10-18

申请号：US11761937

申请日：2007-06-12

Applicant: Manoj Desai ,  Simon Ng ,  Zhi-Jie Ni ,  Keith Pfister ,  Savithri Ramurthy ,  Sharadha Subramanian ,  Allan Wagman

Inventor： Manoj Desai ,  Simon Ng ,  Zhi-Jie Ni ,  Keith Pfister ,  Savithri Ramurthy ,  Sharadha Subramanian ,  Allan Wagman

IPC: A61K31/44 ,  A61K31/445 ,  A61K31/497 ,  A61K31/535 ,  A61P25/28 ,  A61P3/10

CPC classification number: C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D453/02 ,  C07D487/08

Abstract: New pyrrole based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.

Abstract translation: 提供了新的基于吡咯的化合物，组合物和抑制糖原合酶激酶（GSK3）活性并在体内治疗GSK3介导的病症的方法。 本发明的方法，化合物和组合物可以单独使用或与其它药理活性剂组合用于治疗由GSK3活性介导的病症，例如糖尿病，阿尔茨海默病和其他神经变性疾病，肥胖症，动脉粥样硬化性心血管疾病，必需的 高血压，多囊卵巢综合征，X综合征，缺血，创伤性脑损伤，双相情感障碍，免疫缺陷或癌症。