公开(公告)号：US20070282101A1

公开(公告)日：2007-12-06

申请号：US11731950

申请日：2007-04-02

Applicant: Anna Ericsson ,  Andrew Burchat ,  Kristine Frank ,  David Calderwood ,  Lily Abbott ,  Maria Argiriadi ,  David Borhani ,  Kevin Cusack ,  Richard Dixon ,  Thomas Gordon ,  Kelly Mullen ,  Robert Talanian ,  Xiaoyun Wu ,  Xiaolei Zhang ,  Lu Wang ,  Biqin Li ,  Claude Barberis ,  Neil Wishart

Inventor： Anna Ericsson ,  Andrew Burchat ,  Kristine Frank ,  David Calderwood ,  Lily Abbott ,  Maria Argiriadi ,  David Borhani ,  Kevin Cusack ,  Richard Dixon ,  Thomas Gordon ,  Kelly Mullen ,  Robert Talanian ,  Xiaoyun Wu ,  Xiaolei Zhang ,  Lu Wang ,  Biqin Li ,  Claude Barberis ,  Neil Wishart

IPC: C07D409/14 ,  C07D409/04 ,  C07D413/14

CPC classification number: C07D487/04 ,  C07D403/12 ,  C07D403/14 ,  C07D409/04 ,  C07D409/14

Abstract: Novel compounds of Formula (I) or pharmaceutically acceptable salts, prodrugs and biologically active metabolites thereof of Formula (I) wherein the substituents are as defined herein, which are useful as therapeutic agents.

Abstract translation: 式（I）的新型化合物或其药学上可接受的盐，前体药物和式（I）的生物活性代谢物，其中取代基如本文所定义，其可用作治疗剂。

公开(公告)号：US20090118298A1

公开(公告)日：2009-05-07

申请号：US12284758

申请日：2008-09-25

Applicant: Dawn M. George ,  Lu Wang ,  Biqin Li ,  Anna M. Ericsson ,  Graham K. Ansell

Inventor： Dawn M. George ,  Lu Wang ,  Biqin Li ,  Anna M. Ericsson ,  Graham K. Ansell

IPC: A61K31/496 ,  C07D405/14 ,  A61K31/4375 ,  A61K31/4025 ,  A61K31/495 ,  A61K31/497 ,  A61P11/06 ,  A61P11/00 ,  A61P17/06 ,  A61P31/10 ,  A61P31/12 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P17/00 ,  A61P31/04 ,  A61P35/02 ,  A61P35/00 ,  A61P25/16 ,  A61P3/00 ,  A61P29/00 ,  A61P17/02 ,  A61P17/14 ,  A61P3/10 ,  A61P33/02 ,  A61P27/06 ,  A61P37/06 ,  A61P1/00 ,  A61P25/00 ,  A61P19/10 ,  C07D401/14 ,  C07D241/04 ,  C07D401/08 ,  C07D405/12

CPC classification number: C07D471/04 ,  C07D211/14 ,  C07D295/185 ,  C07D309/14 ,  C07D405/12

Abstract: The present invention is directed to novel compounds of Formula (I) pharmaceutically acceptable salts thereof, pro-drugs thereof, biologically active metabolites thereof, isomers thereof or stereoisomers thereof wherein the variables are as defined herein. The compounds of Formula (I) are useful as chemokine receptor antagonists and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, rheumatoid arthritis, osteoarthritis, multiple sclerosis and asthma.

Abstract translation: 本发明涉及新的式（I）化合物，其药学上可接受的盐，其前药，其生物活性代谢物，其异构体或其立体异构体，其中变量如本文所定义。 式（I）的化合物可用作趋化因子受体拮抗剂，因此可用于治疗某些病症和疾病，特别是炎性病症和疾病以及增殖性疾病和病症，例如类风湿性关节炎，骨关节炎，多发性硬化和哮喘。

公开(公告)号：US20120053345A1

公开(公告)日：2012-03-01

申请号：US13198363

申请日：2011-08-04

Applicant: Anna M. Ericson ,  Andrew Burchat ,  Kristine E. Frank ,  David J. Calderwood ,  Lily K. Abbott ,  Maria A. Argiriadi ,  David W. Borhani ,  Kevin P. Cusack ,  Richard W. Dixon ,  Thomas D. Gordon ,  Kelly D. Mullen ,  Robert V. Talanian ,  Xiaoyun Wu ,  Xiaolei Zhang ,  Lu Wang ,  Biqin Li ,  Claude E. Barberis ,  Neil Wishart

Inventor： Anna M. Ericson ,  Andrew Burchat ,  Kristine E. Frank ,  David J. Calderwood ,  Lily K. Abbott ,  Maria A. Argiriadi ,  David W. Borhani ,  Kevin P. Cusack ,  Richard W. Dixon ,  Thomas D. Gordon ,  Kelly D. Mullen ,  Robert V. Talanian ,  Xiaoyun Wu ,  Xiaolei Zhang ,  Lu Wang ,  Biqin Li ,  Claude E. Barberis ,  Neil Wishart

IPC: C07D495/04 ,  C07D401/14 ,  C07D403/14 ,  C07D231/54 ,  C07D487/04

CPC classification number: C07D487/04 ,  C07D403/12 ,  C07D403/14 ,  C07D409/04 ,  C07D409/14

Abstract: Novel compounds of Formula (I) or pharmaceutically acceptable salts, prodrugs and biologically active metabolites thereof of Formula (I) wherein the substituents are as defined herein, which are useful as therapeutic agents.

Abstract translation: 式（I）的新型化合物或其药学上可接受的盐，前体药物和式（I）的生物活性代谢物，其中取代基如本文所定义，其可用作治疗剂。

公开(公告)号：US08008481B2

公开(公告)日：2011-08-30

申请号：US11731950

申请日：2007-04-02

Applicant: Anna M. Ericsson ,  Andrew Burchat ,  Kristine E. Frank ,  David J. Calderwood ,  Lily K. Abbott ,  Maria A. Argiriadi ,  David W. Borhani ,  Kevin P. Cusack ,  Richard W. Dixon ,  Thomas D. Gordon ,  Kelly D. Mullen ,  Robert V. Talanian ,  Xiaoyun Wu ,  Xiaolei Zhang ,  Lu Wang ,  Biqin Li ,  Claude E. Barberis ,  Neil Wishart

Inventor： Anna M. Ericsson ,  Andrew Burchat ,  Kristine E. Frank ,  David J. Calderwood ,  Lily K. Abbott ,  Maria A. Argiriadi ,  David W. Borhani ,  Kevin P. Cusack ,  Richard W. Dixon ,  Thomas D. Gordon ,  Kelly D. Mullen ,  Robert V. Talanian ,  Xiaoyun Wu ,  Xiaolei Zhang ,  Lu Wang ,  Biqin Li ,  Claude E. Barberis ,  Neil Wishart

IPC: C07D409/14 ,  C07D413/14

CPC classification number: C07D487/04 ,  C07D403/12 ,  C07D403/14 ,  C07D409/04 ,  C07D409/14

Abstract: Novel compounds of Formula (I) or pharmaceutically acceptable salts, prodrugs and biologically active metabolites thereof of Formula (I) wherein the substituents are as defined herein, which are useful as therapeutic agents.

Abstract translation: 式（I）的新型化合物或其药学上可接受的盐，前体药物和式（I）的生物活性代谢物，其中取代基如本文所定义，其可用作治疗剂。

公开(公告)号：US20080176883A1

公开(公告)日：2008-07-24

申请号：US11985724

申请日：2007-11-16

Applicant: Dawn M. George ,  Richard W. Dixon ,  Michael Friedman ,  Adrian D. Hobson ,  Biqin Li ,  Lu Wang ,  Xiaoyun Wu ,  Neil Wishart

Inventor： Dawn M. George ,  Richard W. Dixon ,  Michael Friedman ,  Adrian D. Hobson ,  Biqin Li ,  Lu Wang ,  Xiaoyun Wu ,  Neil Wishart

IPC: A61K31/438 ,  C07D471/04 ,  A61K31/4375 ,  C07D401/04 ,  A61K31/454

CPC classification number: A61K31/454 ,  A61K31/437 ,  A61K31/438 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4747 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/553 ,  C07D207/14 ,  C07D401/04 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D487/14

Abstract: The present invention is directed to novel aminopyrrolidines of formula I pharmaceutically acceptable salts thereof, metabolites thereof, isomers thereof, stereoisomers thereof or pro-drugs thereof, wherein the variables are as defined herein. The compounds of formula (I) are useful as chemokine receptor antagonists and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.

Abstract translation: 本发明涉及式I的药学上可接受的盐的新型氨基吡咯烷，其代谢物，其异构体，其立体异构体或其前体药物，其中变量如本文所定义。 式（I）化合物可用作趋化因子受体拮抗剂，因此可用于治疗某些病症和疾病，特别是炎性病症和疾病以及增殖性疾病和病症，例如癌症。

公开(公告)号：US20080076924A1

公开(公告)日：2008-03-27

申请号：US11824441

申请日：2007-06-29

Applicant: Patrick Betschmann ,  William Carroll ,  Anna Ericsson ,  Shannon Fix-Stenzel ,  Michael Friedman ,  Gavin Hirst ,  Nathan Josephsohn ,  Biqin Li ,  Arturo Perez-Medrano ,  Michael Morytko ,  Paul Rafferty ,  Haipeng Chen

Inventor： Patrick Betschmann ,  William Carroll ,  Anna Ericsson ,  Shannon Fix-Stenzel ,  Michael Friedman ,  Gavin Hirst ,  Nathan Josephsohn ,  Biqin Li ,  Arturo Perez-Medrano ,  Michael Morytko ,  Paul Rafferty ,  Haipeng Chen

IPC: C07D471/04 ,  C07D401/00

CPC classification number: C07D241/04 ,  C07D241/36 ,  C07D295/215 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

Abstract: Novel compounds of Formula (I) or pharmaceutically acceptable salts thereof, metabolites thereof, isomers thereof, enantiomers thereof or prodrugs thereof of Formula (I) wherein the substituents are as defined herein, which are useful as therapeutic agents.

Abstract translation: 式（I）的新型化合物或其药学上可接受的盐，其代谢物，其异构体，其对映体或式（I）的前药，其中取代基如本文所定义，其可用作治疗剂。

公开(公告)号：US08648069B2

公开(公告)日：2014-02-11

申请号：US12327991

申请日：2008-12-04

Applicant: Irini Akritopoulou-Zanze ,  Brian D. Wakefield ,  Helmut Mack ,  Sean C. Turner ,  Alan F. Gasiecki ,  Vijaya J. Gracias ,  Kathy A. Sarris ,  Douglas M. Kalvin ,  Melissa J. Michmerhuizen ,  Qi Shuai ,  Jyoti R. Patel ,  Margaretha Bakker ,  Nicole Teusch ,  Eric F. Johnson ,  Peter J. Kovar ,  Stevan W. Djuric ,  Andrew J. Long ,  Anil Vasudevan ,  Dawn George ,  Lu Wang ,  Biqin Li ,  N. St. John Moore ,  Adrian D. Hobson ,  Keith W. Woods ,  Julie M. Miyashiro ,  Steven L. Swann, Jr. ,  Thomas D. Penning

Inventor： Irini Akritopoulou-Zanze ,  Brian D. Wakefield ,  Helmut Mack ,  Sean C. Turner ,  Alan F. Gasiecki ,  Vijaya J. Gracias ,  Kathy A. Sarris ,  Douglas M. Kalvin ,  Melissa J. Michmerhuizen ,  Qi Shuai ,  Jyoti R. Patel ,  Margaretha Bakker ,  Nicole Teusch ,  Eric F. Johnson ,  Peter J. Kovar ,  Stevan W. Djuric ,  Andrew J. Long ,  Anil Vasudevan ,  Dawn George ,  Lu Wang ,  Biqin Li ,  N. St. John Moore ,  Adrian D. Hobson ,  Keith W. Woods ,  Julie M. Miyashiro ,  Steven L. Swann, Jr. ,  Thomas D. Penning

IPC: A61K31/541 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/454 ,  A61K31/4192 ,  C07D417/14 ,  C07D405/14 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14

CPC classification number: C07D413/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, R1, R2, R3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), Cdc7, AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.

Abstract translation: 本发明涉及式（I）化合物或其药学上可接受的盐，其中A，R 1，R 2，R 3和m在说明书中定义。 本发明还涉及制备所述化合物的方法和含有所述化合物的组合物，其可用于抑制激酶例如糖原合成酶激酶3（GSK-3），Rho激酶（ROCK），Janus激酶（JAK），Cdc7，AKT ，PAK4，PLK，CK2，KDR，MK2，JNK1，极光，pim1和nek2。

公开(公告)号：US20110178096A1

公开(公告)日：2011-07-21

申请号：US13074676

申请日：2011-03-29

Applicant: Dawn M. George ,  Lu X. Wang ,  Biqin Li ,  Anna M. Ericsson ,  Graham K. Ansell

Inventor： Dawn M. George ,  Lu X. Wang ,  Biqin Li ,  Anna M. Ericsson ,  Graham K. Ansell

IPC: A61K31/4375 ,  C07D211/34 ,  C07D471/04 ,  C07D405/12 ,  C07D401/08 ,  C07D295/192 ,  A61K31/496 ,  A61K31/4025 ,  A61K31/495 ,  A61K31/497 ,  A61K31/451 ,  A61P19/02 ,  A61P29/00 ,  A61P11/00 ,  A61P11/06 ,  A61P17/06 ,  A61P1/00 ,  A61P35/00 ,  A61P35/02 ,  A61P31/04 ,  A61P9/12 ,  A61P9/10 ,  A61P1/04 ,  A61P21/04 ,  A61P3/10 ,  A61P25/00

CPC classification number: C07D471/04 ,  C07D211/14 ,  C07D295/185 ,  C07D309/14 ,  C07D405/12

Abstract: The present invention is directed to novel compounds of Formula (I) pharmaceutically acceptable salts thereof, pro-drugs thereof, biologically active metabolites thereof, isomers thereof or stereoisomers thereof wherein the variables are as defined herein. The compounds of Formula (I) are useful as chemokine receptor antagonists and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, rheumatoid arthritis, osteoarthritis, multiple sclerosis and asthma.

Abstract translation: 本发明涉及新的式（I）化合物，其药学上可接受的盐，其前药，其生物活性代谢物，其异构体或其立体异构体，其中变量如本文所定义。 式（I）的化合物可用作趋化因子受体拮抗剂，因此可用于治疗某些病症和疾病，特别是炎性病症和疾病以及增殖性疾病和病症，例如类风湿性关节炎，骨关节炎，多发性硬化和哮喘。

公开(公告)号：US07939544B2

公开(公告)日：2011-05-10

申请号：US12284758

申请日：2008-09-25

Applicant: Dawn M. George ,  Lu Wang ,  Biqin Li ,  Anna M. Ericsson ,  Graham K. Ansell

Inventor： Dawn M. George ,  Lu Wang ,  Biqin Li ,  Anna M. Ericsson ,  Graham K. Ansell

IPC: A01N43/42 ,  A61K31/44 ,  C07D221/02

CPC classification number: C07D471/04 ,  C07D211/14 ,  C07D295/185 ,  C07D309/14 ,  C07D405/12

Abstract: The present invention is directed to novel compounds of Formula (I) pharmaceutically acceptable salts thereof, pro-drugs thereof, biologically active metabolites thereof, isomers thereof or stereoisomers thereof wherein the variables are as defined herein. The compounds of Formula (I) are useful as chemokine receptor antagonists and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, rheumatoid arthritis, osteoarthritis, multiple sclerosis and asthma.

Abstract translation: 本发明涉及新的式（I）化合物，其药学上可接受的盐，其前药，其生物活性代谢物，其异构体或其立体异构体，其中变量如本文所定义。 式（I）的化合物可用作趋化因子受体拮抗剂，因此可用于治疗某些病症和疾病，特别是炎性病症和疾病以及增殖性疾病和病症，例如类风湿性关节炎，骨关节炎，多发性硬化和哮喘。

公开(公告)号：US5912269A

公开(公告)日：1999-06-15

申请号：US640260

申请日：1996-04-30

Applicant: Roger D. Tung ,  Biqin Li

Inventor： Roger D. Tung ,  Biqin Li

IPC: C07C69/68 ,  A01N37/02

CPC classification number: C07C69/68

Abstract: This invention relates to butyrate prodrugs derived from lactic acid and pharmaceutical compositions and methods employing them, either alone or in combination with other agents, for increasing gamma globin and fetal hemoglobin in a patient. These compounds, compositions and methods are particularly effective in treating .beta.-hemoglobinopathies, including sickle cell syndromes and .beta.-thalassemia syndromes. In addition, this invention relates to the use of these prodrugs, alone or in combination with other agents, to stimulate cell differentiation which prevents proliferation of malignant cells. These methods are particularly useful in treating cancer, especially malignant hematological disorders.

Abstract translation: 本发明涉及由乳酸衍生的丁酸酯前药以及使用它们的单独或与其它试剂组合的药物组合物和方法，用于增加患者中的γ珠蛋白和胎儿血红蛋白。 这些化合物，组合物和方法在治疗β-血红蛋白病，包括镰状细胞综合征和β-地贫综合征中特别有效。 此外，本发明涉及这些前药单独或与其它试剂组合来刺激细胞分化的用途，其阻止恶性细胞的增殖。 这些方法特别适用于治疗癌症，特别是恶性血液病。