公开(公告)号：US07514225B2

公开(公告)日：2009-04-07

申请号：US11182360

申请日：2005-07-15

Applicant: Federico C. A. Gaeta ,  Andrew Baird ,  Jerry Anchin ,  Wenbin Ying ,  Robert Florkiewicz ,  Jagadish Sircar ,  Sunil Kumar K. C.

Inventor： Federico C. A. Gaeta ,  Andrew Baird ,  Jerry Anchin ,  Wenbin Ying ,  Robert Florkiewicz ,  Jagadish Sircar ,  Sunil Kumar K. C.

IPC: G01N33/53 ,  C12N5/00 ,  C07K16/24 ,  C07K14/52

CPC classification number: C07D401/12 ,  C07D215/42 ,  C07D215/54 ,  C07D405/12 ,  C07D409/12

Abstract: Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R3, R4, X, Y and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.

Abstract translation: 提供了MIF的抑制剂，其可用于治疗各种疾病，包括治疗与MIF活性相关的病理状况。 MIF的抑制剂具有以下结构：包括其立体异构体，前药和药学上可接受的盐，其中n，R 1，R 2，R 3，R 4，X，Y和Z如本文所定义。 还提供了含有与药学上可接受的载体组合的MIF抑制剂的组合物，以及使用该组合物的方法。

公开(公告)号：US07432374B2

公开(公告)日：2008-10-07

申请号：US11687611

申请日：2007-03-16

Applicant: Federico C. A. Gaeta ,  Andrew Baird ,  Jerry Anchin ,  Wenbin Ying ,  Robert Florkiewicz ,  Jagadish Sircar ,  Sunil Kumar K. C.

Inventor： Federico C. A. Gaeta ,  Andrew Baird ,  Jerry Anchin ,  Wenbin Ying ,  Robert Florkiewicz ,  Jagadish Sircar ,  Sunil Kumar K. C.

IPC: C07D215/42 ,  C07D215/54 ,  C07D401/06 ,  C07D403/06

CPC classification number: C07D401/12 ,  C07D215/42 ,  C07D215/54 ,  C07D405/12 ,  C07D409/12

Abstract: Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R3, R4, X, Y and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.

Abstract translation: 提供了MIF的抑制剂，其可用于治疗各种疾病，包括治疗与MIF活性相关的病理状况。 MIF的抑制剂具有以下结构：包括其立体异构体，前药和药学上可接受的盐，其中n，R 1，R 2，R 3， >，R 4，X，Y和Z如本文所定义。 还提供了含有与药学上可接受的载体组合的MIF抑制剂的组合物，以及使用该组合物的方法。

公开(公告)号：US07365200B2

公开(公告)日：2008-04-29

申请号：US11687598

申请日：2007-03-16

Applicant: Jagadish Sircar ,  Sunil Kumar K. C. ,  Timothy James Davis ,  Wenbin Ying

Inventor： Jagadish Sircar ,  Sunil Kumar K. C. ,  Timothy James Davis ,  Wenbin Ying

IPC: C07D495/04 ,  A61K31/496

CPC classification number: C07D495/04 ,  C07D498/02

Abstract: Inhibitors of macrophage migration inhibitory factor having a thienopyridinone backbone are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with macrophage migration inhibitory factor activity. The inhibitors of macrophage migration inhibitory factor have the following structures: including forms such as stereoisomers, free forms, pharmaceutically acceptable salts or esters thereof, solvates, or combinations of such forms, wherein n, R1, R2, R3, X, and Y are as defined herein. Compositions comprising an inhibitor of macrophage migration inhibitory factor in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.

Abstract translation: 提供具有噻吩并吡啶酮骨架的巨噬细胞迁移抑制因子的抑制剂，其可用于治疗各种疾病，包括治疗与巨噬细胞迁移抑制因子活性相关的病理状况。 巨噬细胞迁移抑制因子的抑制剂具有以下结构：包括形式如立体异构体，游离形式，药学上可接受的盐或酯，溶剂合物或这些形式的组合，其中n，R 1，R R 3，R 3，X和Y如本文所定义。 还提供了包含与药学上可接受的载体组合的巨噬细胞迁移抑制因子抑制剂的组合物，以及其用途的方法。

公开(公告)号：US20070232613A1

公开(公告)日：2007-10-04

申请号：US11635319

申请日：2006-12-07

Applicant: Federico Gaeta ,  Andrew Baird ,  Jerry Anchin ,  Wenbin Ying ,  Robert Florkiewicz ,  Jagadish Sircar ,  Sunil K.C.

Inventor： Federico Gaeta ,  Andrew Baird ,  Jerry Anchin ,  Wenbin Ying ,  Robert Florkiewicz ,  Jagadish Sircar ,  Sunil K.C.

IPC: A61K31/497 ,  A61K31/496 ,  C07D417/14 ,  C07D413/14 ,  C07D409/14 ,  C07D403/14

CPC classification number: C07D401/12 ,  C07D215/42 ,  C07D215/54 ,  C07D405/12 ,  C07D409/12

Abstract: Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R3, R4, X, Y and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.

Abstract translation: 提供了MIF的抑制剂，其可用于治疗各种疾病，包括治疗与MIF活性相关的病理状况。 MIF的抑制剂具有以下结构：包括其立体异构体，前药和药学上可接受的盐，其中n，R 1，R 2，R 3， >，R 4，X，Y和Z如本文所定义。 还提供了含有与药学上可接受的载体组合的MIF抑制剂的组合物，以及使用该组合物的方法。

公开(公告)号：US07202248B2

公开(公告)日：2007-04-10

申请号：US11344938

申请日：2006-01-31

Applicant: Federico C. A. Gaeta ,  Andrew Baird ,  Jerry Anchin ,  Wenbin Ying ,  Robert Florkiewicz ,  Jagadish Sircar ,  Sunil Kumar K. C.

Inventor： Federico C. A. Gaeta ,  Andrew Baird ,  Jerry Anchin ,  Wenbin Ying ,  Robert Florkiewicz ,  Jagadish Sircar ,  Sunil Kumar K. C.

IPC: A61K31/496

CPC classification number: C07D401/12 ,  C07D215/42 ,  C07D215/54 ,  C07D405/12 ,  C07D409/12

Abstract: Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R3, R4, X, Y and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.

Abstract translation: 提供了MIF的抑制剂，其可用于治疗各种疾病，包括治疗与MIF活性相关的病理状况。 MIF的抑制剂具有以下结构：

公开(公告)号：US20060194792A1

公开(公告)日：2006-08-31

申请号：US11415785

申请日：2006-05-02

Applicant: Federico Gaeta ,  Andrew Baird ,  Jerry Anchin ,  Wenbin Ying ,  Robert Florkiewicz ,  Jagadish Sircar ,  Sunil K.C.

Inventor： Federico Gaeta ,  Andrew Baird ,  Jerry Anchin ,  Wenbin Ying ,  Robert Florkiewicz ,  Jagadish Sircar ,  Sunil K.C.

IPC: A61K31/551

CPC classification number: C07D401/12 ,  C07D215/42 ,  C07D215/54 ,  C07D405/12 ,  C07D409/12

Abstract: Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R3, R4, X, Y and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.

公开(公告)号：US20060094727A1

公开(公告)日：2006-05-04

申请号：US11268375

申请日：2005-11-07

Applicant: Federico Gaeta ,  Andrew Baird ,  Jerry Anchin ,  Wenbin Ying ,  Robert Florkiewicz ,  Jagadish Sircar ,  Sunil K.C.

Inventor： Federico Gaeta ,  Andrew Baird ,  Jerry Anchin ,  Wenbin Ying ,  Robert Florkiewicz ,  Jagadish Sircar ,  Sunil K.C.

IPC: A61K31/497 ,  A61K31/496

CPC classification number: C07D401/12 ,  C07D215/42 ,  C07D215/54 ,  C07D405/12 ,  C07D409/12

Abstract: Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R3, R4, X, Y and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.

Abstract translation: 提供了MIF的抑制剂，其可用于治疗各种疾病，包括治疗与MIF活性相关的病理状况。 MIF的抑制剂具有以下结构：包括其立体异构体，前药和药学上可接受的盐，其中n，R 1，R 2，R 3， >，R 4，X，Y和Z如本文所定义。 还提供了含有与药学上可接受的载体组合的MIF抑制剂的组合物，以及使用该组合物的方法。

公开(公告)号：US20050287617A1

公开(公告)日：2005-12-29

申请号：US11182360

申请日：2005-07-15

Applicant: Federico Gaeta ,  Andrew Baird ,  Jerry Anchin ,  Wenbin Ying ,  Robert Florkiewicz ,  Jagadish Sircar ,  Sunil K.C.

Inventor： Federico Gaeta ,  Andrew Baird ,  Jerry Anchin ,  Wenbin Ying ,  Robert Florkiewicz ,  Jagadish Sircar ,  Sunil K.C.

IPC: C12Q1/02 ,  A61K31/47 ,  A61K31/496 ,  A61K31/497 ,  A61K45/00 ,  A61P1/04 ,  A61P3/10 ,  A61P5/08 ,  A61P5/46 ,  A61P9/00 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P19/02 ,  A61P25/28 ,  A61P29/00 ,  A61P35/00 ,  A61P37/06 ,  A61P43/00 ,  C07D215/42 ,  C07D215/46 ,  C07D215/54 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  G01N33/53 ,  G01N33/537 ,  G01N33/543

CPC classification number: C07D401/12 ,  C07D215/42 ,  C07D215/54 ,  C07D405/12 ,  C07D409/12

Abstract: Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R3, R4, X, Y and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.

Abstract translation: 提供了MIF的抑制剂，其可用于治疗各种疾病，包括治疗与MIF活性相关的病理状况。 MIF的抑制剂具有以下结构：包括其立体异构体，前药和药学上可接受的盐，其中n，R 1，R 2，R 3， >，R 4，X，Y和Z如本文所定义。 还提供了含有与药学上可接受的载体组合的MIF抑制剂的组合物，以及使用该组合物的方法。

公开(公告)号：US20050124604A1

公开(公告)日：2005-06-09

申请号：US10920031

申请日：2004-08-17

Applicant: Jagadish Sircar ,  Sunil K.C. ,  Wenbin Ying ,  Timothy Davis

Inventor： Jagadish Sircar ,  Sunil K.C. ,  Wenbin Ying ,  Timothy Davis

IPC: A61P29/02 ,  A61P35/00 ,  A61P37/06 ,  C07D471/04 ,  A61K31/55 ,  A61K31/496 ,  C07D471/02

CPC classification number: C07D471/04

Abstract: Inhibitors of MIF having a naphthyridine backbone are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R, R1, R2, X, Y and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.

Abstract translation: 提供了具有萘啶主链的MIF抑制剂，其可用于治疗各种疾病，包括治疗与MIF活性相关的病理状况。 MIF的抑制剂具有以下结构：包括其立体异构体，前药和药学上可接受的盐，其中n，R 1，R 1，R 2，X，Y和Z是 如本文所定义。 还提供了含有与药学上可接受的载体组合的MIF抑制剂的组合物，以及使用该组合物的方法。

公开(公告)号：US20130071467A1

公开(公告)日：2013-03-21

申请号：US13492594

申请日：2012-06-08

Applicant: Yoshiro Niitsu ,  Victor Knopov ,  Joseph E. Payne ,  Richard P. Witte ,  Mohammad Ahmadian ,  Loren A. Perelman ,  Violetta Akopian ,  Yasunobu Tanaka ,  Elena Feinstein ,  Sharon Avkin-Nahum ,  Hagar Kalinski ,  Igor Mett ,  Kenjiro Minomi ,  Wenbin Ying ,  Yun Liu

Inventor： Yoshiro Niitsu ,  Victor Knopov ,  Joseph E. Payne ,  Richard P. Witte ,  Mohammad Ahmadian ,  Loren A. Perelman ,  Violetta Akopian ,  Yasunobu Tanaka ,  Elena Feinstein ,  Sharon Avkin-Nahum ,  Hagar Kalinski ,  Igor Mett ,  Kenjiro Minomi ,  Wenbin Ying ,  Yun Liu

IPC: A61K9/127 ,  A61K31/713

CPC classification number: A61K9/1271 ,  A61K9/127 ,  A61K31/713 ,  C07H21/02 ,  C12N15/111 ,  C12N15/113 ,  C12N2310/11 ,  C12N2310/14 ,  C12N2320/32 ,  C12N2320/52

Abstract: What is described are pharmaceutical compositions comprising a double-stranded nucleic acid molecule comprising a sense strand and an antisense strand wherein the sense and antisense strands are selected from the oligonucleotides described as SERPINH1_2 (SEQ ID NOS: 60 and 127), SERPINH1_45a (SEQ ID NOS: 98 and 165), and SERPINH1_51 (SEQ ID NOS: 101 and 168), and drug carrier comprising a mixture of a retinoid and a lipid vesicle, and methods of using these pharmaceutical compositions to treat a disease associated with hsp47 expression, including fibrosis.

Abstract translation: 描述的是包含包含有义链和反义链的双链核酸分子的药物组合物，其中有义链和反义链选自描述为SERPINH1_2的寡核苷酸（SEQ ID NO：60和127），SERPINH1_45a（SEQ ID NO： NOS：98和165）和SERPINH1_51（SEQ ID NO：101和168）和包含类视黄醇和脂质囊泡的混合物的药物载体，以及使用这些药物组合物治疗与hsp47表达相关的疾病的方法，包括 纤维化。