公开(公告)号：US08217035B2

公开(公告)日：2012-07-10

申请号：US12161537

申请日：2007-01-22

申请人： 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

发明人： 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分类号： A61K31/535 ,  C07D413/14

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D417/12

摘要： 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.

摘要翻译： 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：US20120225859A1

公开(公告)日：2012-09-06

申请号：US13471111

申请日：2012-05-14

申请人： 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

发明人： 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分类号： A61K31/5377 ,  C07D413/14 ,  C12N5/07 ,  A61K31/553 ,  A61K31/541 ,  C07D471/08 ,  A61P35/00 ,  A61K31/538

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D417/12

摘要： 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.

摘要翻译： 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

申请人： 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

发明人： 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分类号： A61K31/5377 ,  C07D413/14 ,  A61P35/00

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D417/12

摘要： 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.

摘要翻译： 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：US20050004153A1

公开(公告)日：2005-01-06

申请号：US10869292

申请日：2004-06-16

申请人： T.G. Dhar ,  Dominique Potin ,  Magali Blandine Maillet ,  Michele Launay ,  Eric Nicolai ,  Edwin Iwanowicz

发明人： T.G. Dhar ,  Dominique Potin ,  Magali Blandine Maillet ,  Michele Launay ,  Eric Nicolai ,  Edwin Iwanowicz

IPC分类号： C07D233/76 ,  A61K31/4166 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/42 ,  A61K31/427 ,  A61K31/428 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/498 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61P1/00 ,  A61P1/04 ,  A61P1/16 ,  A61P1/18 ,  A61P3/10 ,  A61P7/00 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P11/08 ,  A61P13/12 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P19/10 ,  A61P25/00 ,  A61P25/28 ,  A61P27/02 ,  A61P27/16 ,  A61P29/00 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  A61P39/02 ,  C07D233/96 ,  C07D235/02 ,  C07D401/04 ,  C07D401/14 ,  C07D487/10 ,  C07D487/20 ,  C07D519/00 ,  A61K31/4747

CPC分类号： C07D235/02 ,  C07D233/96 ,  C07D487/10

摘要： Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates, enantiomers, and diastereomers, and prodrugs thereof, are useful as inhibitors of LFA-1/ICAM and as anti-inflammatory agents, wherein L and K are O or S; Z is N or CR4b; Ar is an optionally-substituted aryl or heteroaryl; G is a linker attached to T or M or is absent; J, M and T are selected to define a three to six membered saturated or partially unsaturated non-aromatic ring; and R2, R4a, R4b, and R4c are as defined in the specification.

摘要翻译： 具有式（I）的化合物及其药学上可接受的盐，水合物，对映异构体和非对映异构体及其前药可用作LFA-1 / ICAM的抑制剂和作为抗炎剂的其中L和K为O或S ; Z是N或CR4b; Ar是任选取代的芳基或杂芳基; G是连接于T或M或不存在的接头; 选择J，M和T来定义三至六元饱和或部分不饱和的非芳香环; R2，R4a，R4b和R4c如说明书中所定义。

公开(公告)号：US08563549B2

公开(公告)日：2013-10-22

申请号：US13471111

申请日：2012-05-14

申请人： 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

发明人： 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分类号： A61K31/535 ,  C07D413/14

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D417/12

摘要： 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.

摘要翻译： 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：US07199125B2

公开(公告)日：2007-04-03

申请号：US10957255

申请日：2004-10-01

申请人： T. G. Murali Dhar ,  Edwin Iwanowicz ,  Michele Launay ,  Dominique Potin ,  Magali Jeannine Blandine Maillet ,  Eric Nicolai

发明人： T. G. Murali Dhar ,  Edwin Iwanowicz ,  Michele Launay ,  Dominique Potin ,  Magali Jeannine Blandine Maillet ,  Eric Nicolai

IPC分类号： C07D497/20 ,  C07D498/20 ,  A61K31/424 ,  A61K31/429 ,  A61K31/506

CPC分类号： C07D498/20 ,  C07D513/20

摘要： The present invention is directed to compounds having the formula (I): useful in treating inflammatory and immune diseases, in which K and L are independently, O or S; Q is —C(═O)— or optionally substituted C1-6alkylene; Ar is optionally-substituted aryl or heteroaryl; J1, J2, J3 and Y are selected so that ring A is a five-to-six membered optionally-substituted cycloalkenyl or heterocyclo ring having 0 to 2 nitrogen heteroatoms; R1 is N or C(R9); and R2, and R3, are as defined in the specification.

摘要翻译： 本发明涉及具有式（I）的化合物：

公开(公告)号：US20050119279A1

公开(公告)日：2005-06-02

申请号：US10957255

申请日：2004-10-01

申请人： T. G. Dhar ,  Edwin Iwanowicz ,  Michele Launay ,  Dominique Potin ,  Magali Blandine Maillet ,  Eric Nicolai

发明人： T. G. Dhar ,  Edwin Iwanowicz ,  Michele Launay ,  Dominique Potin ,  Magali Blandine Maillet ,  Eric Nicolai

IPC分类号： C07D498/20 ,  C07D513/20 ,  A61K31/519 ,  A61K31/4188 ,  A61K31/4747 ,  C07D487/12

CPC分类号： C07D498/20 ,  C07D513/20

摘要： The present invention is directed to compounds having the formula (I): useful in treating inflammatory and immune diseases, in which K and L are independently, O or S; Q is —C(═O)— or optionally substituted C1-6alkylene; Ar is optionally-substituted aryl or heteroaryl; J1, J2, J3 and Y are selected so that ring A is a five-to-six membered optionally-substituted cycloalkenyl or heterocyclo ring having 0 to 2 nitrogen heteroatoms; R1 is N or C(R9); and R2, and R3, are as defined in the specification.

摘要翻译： 本发明涉及具有式（I）的化合物：可用于治疗其中K和L独立地为O或S的炎症和免疫疾病; Q是-C（-O） - 或任选取代的C 1-6 - 亚烷基; Ar是任选取代的芳基或杂芳基; 选择J 1，J 2，J 3和Y，使得环A为5至6元任选取代的环烯基或 具有0至2个氮杂原子的杂环; R 1是N或C（R 9）; 和R 2 R 3和R 3'如说明书中所定义。

公开(公告)号：US20060122245A1

公开(公告)日：2006-06-08

申请号：US10465427

申请日：2003-06-19

申请人： Henry Gu ,  T.G. Dhar ,  Edwin Iwanowicz

发明人： Henry Gu ,  T.G. Dhar ,  Edwin Iwanowicz

IPC分类号： C07D263/18 ,  C07D263/48 ,  A61K31/421

CPC分类号： C07D413/12 ,  C07D263/32 ,  C07D307/20 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04

摘要： The present invention discloses the identification of the novel inhibitors of IMPDH (inosine-5′-monophosphate dehydrogenase). The compounds and pharmaceutical compositions disclosed herein are useful in treating or preventing IMPDH associated disorders, such as transplant rejection and autoimmune diseases.

摘要翻译： 本发明公开了IMPDH（肌苷-5'-单磷酸脱氢酶）的新型抑制剂的鉴定。 本文公开的化合物和药物组合物可用于治疗或预防IMPDH相关疾病，例如移植排斥反应和自身免疫性疾病。