公开(公告)号：US20060252792A1

公开(公告)日：2006-11-09

申请号：US11459489

申请日：2006-07-24

Applicant: Joseph Dellaria ,  Kyle Lindstrom ,  Luke Dressel ,  Philip Heppner ,  John Jacobsen ,  Joan Moseman ,  William Moser ,  Matthew Radmer ,  Doris Stoermer

Inventor： Joseph Dellaria ,  Kyle Lindstrom ,  Luke Dressel ,  Philip Heppner ,  John Jacobsen ,  Joan Moseman ,  William Moser ,  Matthew Radmer ,  Doris Stoermer

IPC: C07D471/02 ,  A61K31/4745

CPC classification number: C07D471/04

Abstract: Imidazopyridine compounds that contain an ether or thioether functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases. Methods of preparing the compounds and intermediates useful in the preparation of the compounds are also disclosed.

Abstract translation: 在1位含有醚或硫醚官能团的咪唑并吡啶化合物可用作免疫应答调节剂。 本发明的化合物和组合物可以诱导各种细胞因子的生物合成，并且可用于治疗各种病症，包括病毒性疾病和肿瘤性疾病。 还公开了制备可用于制备化合物的化合物和中间体的方法。

公开(公告)号：US20050085503A1

公开(公告)日：2005-04-21

申请号：US10959199

申请日：2004-10-07

Applicant: Takashi Tsukamoto ,  Pavel Majer ,  Doris Stoermer ,  Barbara Slusher

Inventor： Takashi Tsukamoto ,  Pavel Majer ,  Doris Stoermer ,  Barbara Slusher

IPC: A61P9/00 ,  A61K31/192 ,  A61K31/194 ,  A61K31/277 ,  A61P13/08 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/28 ,  A61P25/32 ,  A61P25/34 ,  A61P25/36 ,  A61P27/06 ,  A61P35/00 ,  A61P43/00 ,  C07C323/52 ,  C07C323/56 ,  C07C323/58 ,  C07C323/59 ,  C07C323/60 ,  C07C323/62 ,  C07C323/65 ,  C07D217/12 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/47 ,  C07D263/60 ,  C07D277/80

CPC classification number: C07C323/56 ,  C07C323/52 ,  C07C323/58 ,  C07C323/59 ,  C07C323/60 ,  C07C323/62 ,  C07C323/65

Abstract: This invention relates to new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-β activity, inhibiting angiogenesis, and treating glutamate abnormalities, diabetic neuropathy, pain, compulsive disorders, prostate diseases, cancers and glaucoma.

Abstract translation: 本发明涉及包含这些化合物的新化合物，药物组合物和诊断试剂盒，以及使用这些化合物抑制NAALADase酶活性的方法，检测NAALADase水平改变，影响神经元活性，影响TGF-β活性，抑制血管生成的疾病，以及 治疗谷氨酸异常，糖尿病性神经病，疼痛，强迫症，前列腺疾病，癌症和青光眼。

公开(公告)号：US20050032830A1

公开(公告)日：2005-02-10

申请号：US10916125

申请日：2004-08-11

Applicant: Joseph Dellaria ,  Kyle Lindstrom ,  Luke Dressel ,  Daniel Duffy ,  Philip Heppner ,  John Jacobsen ,  Joan Moseman ,  William Moser ,  Matthew Radmer ,  Doris Stoermer ,  Bernhard Zimmermann

Inventor： Joseph Dellaria ,  Kyle Lindstrom ,  Luke Dressel ,  Daniel Duffy ,  Philip Heppner ,  John Jacobsen ,  Joan Moseman ,  William Moser ,  Matthew Radmer ,  Doris Stoermer ,  Bernhard Zimmermann

IPC: A61K31/437 ,  A61K31/444 ,  A61K31/506 ,  A61K31/5377 ,  A61P7/00 ,  A61P17/00 ,  A61P17/14 ,  A61P17/16 ,  A61P25/00 ,  A61P31/04 ,  A61P31/12 ,  A61P33/00 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07D471/04 ,  C07D471/14 ,  C07D471/02 ,  A61K31/4745

CPC classification number: C07D471/04

Abstract: Imidazopyridine compounds that contain an ether or thioether functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases. Methods of preparing the compounds and intermediates useful in the preparation of the compounds are also disclosed.

Abstract translation: 在1位含有醚或硫醚官能团的咪唑并吡啶化合物可用作免疫应答调节剂。 本发明的化合物和组合物可以诱导各种细胞因子的生物合成，并且可用于治疗各种病症，包括病毒性疾病和肿瘤性疾病。 还公开了制备可用于制备化合物的化合物和中间体的方法。

公开(公告)号：US06740777B2

公开(公告)日：2004-05-25

申请号：US10156880

申请日：2002-05-30

Applicant: Takashi Tsukamoto ,  Doris Stoermer ,  Dilrukshi Vitharana

Inventor： Takashi Tsukamoto ,  Doris Stoermer ,  Dilrukshi Vitharana

IPC: C02C32100

CPC classification number: C07C323/62 ,  C07C323/56 ,  C07C323/58

Abstract: The present invention relates to new thiolalkyl benzoic acids, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-&bgr; activity, inhibiting angiogenesis, and treating glutamate abnormalities, neuropathy, pain, compulsive disorders, prostate diseases, cancers, glaucoma, retinal disorders, and cancer.

Abstract translation: 本发明涉及新的硫醇烷基苯甲酸，包含这些化合物的药物组合物和诊断试剂，以及使用这些化合物抑制NAALADase酶活性的方法，检测其中NAALADase水平被改变，影响神经元活性，影响TGF-β活性，抑制 血管生成和治疗谷氨酸异常，神经病，疼痛，强迫症，前列腺疾病，癌症，青光眼，视网膜疾病和癌症。

公开(公告)号：US07138543B2

公开(公告)日：2006-11-21

申请号：US10819146

申请日：2004-04-07

Applicant: Takashi Tsukamoto ,  Doris Stoermer ,  Dilrukshi Vitharana

Inventor： Takashi Tsukamoto ,  Doris Stoermer ,  Dilrukshi Vitharana

IPC: C07C321/06 ,  C07C323/04 ,  A61K31/19 ,  A61K31/185 ,  A61K31/195

CPC classification number: C07C323/62 ,  C07C323/56 ,  C07C323/58

Abstract: The present invention relates to new thiolalkyl benzoic acids, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-β activity, inhibiting angiogenesis, and treating glutamate abnormalities, neuropathy, pain, compulsive disorders, prostate diseases, cancers, glaucoma, retinal disorders, and cancer.

公开(公告)号：US06884907B2

公开(公告)日：2005-04-26

申请号：US10141818

申请日：2002-05-10

Applicant: Takashi Tsukamoto ,  Pavel Majer ,  Bunda Hin ,  Weizheng Xu ,  Qun Liu ,  Doris Stoermer

Inventor： Takashi Tsukamoto ,  Pavel Majer ,  Bunda Hin ,  Weizheng Xu ,  Qun Liu ,  Doris Stoermer

IPC: G01N33/58 ,  A61K31/19 ,  A61K31/192 ,  A61K31/194 ,  A61K31/235 ,  A61P3/10 ,  A61P9/00 ,  A61P11/00 ,  A61P13/08 ,  A61P15/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/16 ,  A61P25/22 ,  A61P25/28 ,  A61P27/06 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07C239/18 ,  C07C259/06 ,  C07C317/44 ,  C07C323/60 ,  G01N33/68 ,  C07C61/00 ,  A61K31/16 ,  C07C315/00

CPC classification number: C07C317/44 ,  C07C259/06 ,  C07C323/60

Abstract: This invention relates to new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-β activity, inhibiting angiogenesis, and treating glutamate abnormalities, neuropathy, pain, compulsive disorders, prostate diseases, cancers and glaucoma.

Abstract translation: 本发明涉及包含这些化合物的新化合物，药物组合物和诊断试剂盒，以及使用这些化合物抑制NAALADase酶活性的方法，检测NAALADase水平改变，影响神经元活性，影响TGF-β活性，抑制血管生成的疾病，以及 治疗谷氨酸异常，神经病，疼痛，强迫症，前列腺疾病，癌症和青光眼。

公开(公告)号：US06797718B2

公开(公告)日：2004-09-28

申请号：US10456308

申请日：2003-06-06

Applicant: Joseph F. Dellaria ,  Kyle J. Lindstrom ,  Luke T. Dressel ,  Philip D. Heppner ,  John R. Jacobsen ,  Matthew R. Radmer ,  Doris Stoermer

Inventor： Joseph F. Dellaria ,  Kyle J. Lindstrom ,  Luke T. Dressel ,  Philip D. Heppner ,  John R. Jacobsen ,  Matthew R. Radmer ,  Doris Stoermer

IPC: A61K31437

CPC classification number: C07D471/04

Abstract: Imidazopyridine compounds that contain an ether or thioether functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases. Methods of preparing the compounds and intermediates useful in the preparation of the compounds are also disclosed.

公开(公告)号：US06586623B2

公开(公告)日：2003-07-01

申请号：US10046917

申请日：2002-01-17

Applicant: Takashi Tsukamoto ,  Pavel Majer ,  Doris Stoermer ,  Barbara S. Slusher

Inventor： Takashi Tsukamoto ,  Pavel Majer ,  Doris Stoermer ,  Barbara S. Slusher

IPC: C07C32106

CPC classification number: C07C323/56 ,  C07C323/52 ,  C07C323/58 ,  C07C323/59 ,  C07C323/60 ,  C07C323/62 ,  C07C323/65

Abstract: This invention relates to new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-&bgr; activity, inhibiting angiogenesis, and treating glutamate abnormalities, diabetic neuropathy, pain, compulsive disorders, prostate diseases, cancers and glaucoma.

Abstract translation: 本发明涉及包含这些化合物的新化合物，药物组合物和诊断试剂盒，以及使用这些化合物抑制NAALADase酶活性的方法，检测NAALADase水平改变，影响神经元活性，影响TGF-β活性，抑制血管生成的疾病，以及 治疗谷氨酸异常，糖尿病性神经病，疼痛，强迫症，前列腺疾病，癌症和青光眼。

公开(公告)号：US08951528B2

公开(公告)日：2015-02-10

申请号：US12280472

申请日：2007-02-21

Applicant: Doris Stoermer ,  George W. Griesgraber ,  James D. Mendoza ,  Jason D. Bonk

Inventor： Doris Stoermer ,  George W. Griesgraber ,  James D. Mendoza ,  Jason D. Bonk

IPC: A61K39/44 ,  A61K39/385 ,  A61K47/48 ,  A61K31/4745

CPC classification number: A61K47/48384 ,  A61K31/4745 ,  A61K47/6803 ,  A61K47/6843 ,  A61K47/6849 ,  C07K16/2815 ,  C07K16/2878 ,  C07K16/2887

Abstract: The present invention provides IRM conjugates that includes an IRM moiety and a second active moiety covalently linked to the IRM moiety in which the covalent link does not depend on UV irradiation.

Abstract translation: 本发明提供IRM缀合物，其包括共价连接到IRM部分的IRM部分和第二活性部分，其中共价连接不依赖于UV照射。

公开(公告)号：US08541438B2

公开(公告)日：2013-09-24

申请号：US12974459

申请日：2010-12-21

Applicant: Doris Stoermer ,  Joseph F. Dellaria, Jr. ,  David T. Amos ,  Bernhard M. Zimmermann ,  Luke T. Dressel ,  Jason D. Bonk ,  Matthew R. Radmer

Inventor： Doris Stoermer ,  Joseph F. Dellaria, Jr. ,  David T. Amos ,  Bernhard M. Zimmermann ,  Luke T. Dressel ,  Jason D. Bonk ,  Matthew R. Radmer

IPC: C07D487/16 ,  C07D487/14 ,  A61K31/437

CPC classification number: C07D471/04 ,  A61K31/341 ,  A61K31/351 ,  A61K31/435 ,  A61K31/437 ,  A61K31/445 ,  C07D471/14

Abstract: Imidazo-quinoline, -pyridine, and -naphthyridine ring systems (particularly quinolines, tetrahydroquinolines, pyridines, [1,5]naphthyridines, [1,5]tetrahydronaphthyridines) substituted at the 1-position with a cyclic substituent, pharmaceutical compositions containing the compounds, methods of making these compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.