公开(公告)号：US5741909A

公开(公告)日：1998-04-21

申请号：US789264

申请日：1997-01-28

Applicant: John F. Gerster ,  Stephen L. Crooks ,  Kyle J. Lindstrom

Inventor： John F. Gerster ,  Stephen L. Crooks ,  Kyle J. Lindstrom

IPC: C07D215/42 ,  C07D471/04 ,  C07D413/04

CPC classification number: C07D471/04 ,  C07D215/42

Abstract: 1-substituted, 2-substituted 1H-imidazo�4,5-c!-quinolin-4-amines are disclosed. These compounds function as antiviral agents, they induce biosynthesis of interferon, and they inhibit tumor formation in animal models. This invention also provides intermediates for preparing such compounds, pharmaceutical compositions containing such compounds, and pharmacological methods of using such compounds.

Abstract translation: 1-取代的2-取代的1H-咪唑并[4,5-c] - 喹啉-4-胺。 这些化合物作为抗病毒剂起作用，它们诱导干扰素的生物合成，并且它们抑制动物模型中的肿瘤形成。 本发明还提供了制备此类化合物的中间体，含有这些化合物的药物组合物，以及使用这些化合物的药理学方法。

公开(公告)号：US07148232B2

公开(公告)日：2006-12-12

申请号：US10926385

申请日：2004-08-25

Applicant: John F. Gerster ,  Kyle J. Lindstrom ,  Gregory J. Marszalek

Inventor： John F. Gerster ,  Kyle J. Lindstrom ,  Gregory J. Marszalek

IPC: A61K31/4355 ,  A61K31/4365 ,  C07D42/14 ,  C07D42/04

CPC classification number: C07D513/04 ,  C07D513/14 ,  C07D517/04

Abstract: Thiazolo-, oxazolo- and selenazolo[4,5-c]quinolin-4-amines and analogs thereof are described including methods of manufacture and the use of novel intermediates. The compounds are immunomodulators and induce cytokine biosynthesis, including interferon and/or tumor biosynthesis, necrosis factor, and inhibit the T-helper-type 2 immune response. The compounds are further useful in the treatment of viral and neoplastic diseases.

公开(公告)号：US06797716B2

公开(公告)日：2004-09-28

申请号：US10406181

申请日：2003-04-03

Applicant: John F. Gerster ,  Kyle J. Lindstrom ,  Stephen L. Crooks ,  Philip D. Heppner ,  Gregory J. Marszalek ,  Peter V. Maye ,  Bryon A. Merrill ,  John W. Mickelson ,  Michael J. Rice

Inventor： John F. Gerster ,  Kyle J. Lindstrom ,  Stephen L. Crooks ,  Philip D. Heppner ,  Gregory J. Marszalek ,  Peter V. Maye ,  Bryon A. Merrill ,  John W. Mickelson ,  Michael J. Rice

IPC: A61K31437

CPC classification number: C07D471/04 ,  A61K31/4745 ,  A61K45/06 ,  C07D471/14 ,  A61K2300/00

Abstract: Imidazonaphthyridine and tetrahydroimidazonaphthyridine compounds induce the biosynthesis of cytokines such as interferon and tumor necrosis factor. The compounds exhibit antiviral and antitumor properties. Methods of preparing the compounds and intermediates useful in the preparation of the compounds are also disclosed.

公开(公告)号：US06790961B2

公开(公告)日：2004-09-14

申请号：US10731826

申请日：2003-12-09

Applicant: John F. Gerster ,  Stephen L. Crooks ,  Kyle J. Lindstrom

Inventor： John F. Gerster ,  Stephen L. Crooks ,  Kyle J. Lindstrom

IPC: C07D21538

CPC classification number: C07D471/04

Abstract: A method of preparing intermediates for making 1-substituted, 2-substituted 1H-imidazo[4,5-c]quinolin-4-amines is disclosed.

Abstract translation: 公开了制备1-取代的2-取代的1H-咪唑并[4,5-c]喹啉-4-胺的中间体的方法。

公开(公告)号：US06518280B2

公开(公告)日：2003-02-11

申请号：US09945196

申请日：2001-08-31

Applicant: John F. Gerster ,  Kyle J. Lindstrom

Inventor： John F. Gerster ,  Kyle J. Lindstrom

IPC: C07D47102

CPC classification number: C07D471/14

Abstract: Imidazonaphthyridine compounds that are unsubstituted at the 2-position induce the biosynthesis of cytokines such as interferon and tumor necrosis factor. The compounds exhibit antiviral and antitumor properties. Methods of preparing the compounds and intermediates useful in the preparation of the compounds are also disclosed.

Abstract translation: 在2-位未被取代的咪唑并萘啶化合物诱导细胞因子如干扰素和肿瘤坏死因子的生物合成。 该化合物显示抗病毒和抗肿瘤性质。 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：US06323200B1

公开(公告)日：2001-11-27

申请号：US09593434

申请日：2000-06-14

Applicant: John F. Gerster ,  Kyle J. Lindstrom ,  Gregory J. Marszalek ,  Bryon A. Merrill ,  John W. Mickelson ,  Michael J. Rice

Inventor： John F. Gerster ,  Kyle J. Lindstrom ,  Gregory J. Marszalek ,  Bryon A. Merrill ,  John W. Mickelson ,  Michael J. Rice

IPC: A61K315375

CPC classification number: C07D513/04 ,  C07D513/14 ,  C07D517/04

Abstract: Thiazolo-, oxazolo- and selenazolo[4,5-c]quinolin-4-amines and analogs thereof are described including methods of manufacture and the use of novel intermediates. The compounds are immunomodulators and induce cytokine biosynthesis, including interferon and/or tumor biosynthesis, necrosis factor, and inhibit the T-helper-type 2 immune response. The compounds are further useful in the treatment of viral and neoplastic diseases.

Abstract translation: 描述了噻唑并恶唑并[s]噻唑并[4,5-c]喹啉-4-胺及其类似物，包括制造和使用新型中间体的方法。 这些化合物是免疫调节剂并诱导细胞因子生物合成，包括干扰素和/或肿瘤生物合成，坏死因子，并抑制T辅助2型免疫应答。 该化合物还可用于治疗病毒和肿瘤疾病。

公开(公告)号：US6110929A

公开(公告)日：2000-08-29

申请号：US361544

申请日：1999-07-27

Applicant: John F. Gerster ,  Kyle J. Lindstrom ,  Gregory J. Marszalek ,  Bryon A. Merrill ,  John W. Mickelson ,  Michael J. Rice

Inventor： John F. Gerster ,  Kyle J. Lindstrom ,  Gregory J. Marszalek ,  Bryon A. Merrill ,  John W. Mickelson ,  Michael J. Rice

IPC: A61K31/424 ,  A61K31/429 ,  A61K31/4375 ,  A61K31/4738 ,  A61K31/5377 ,  A61P31/12 ,  A61P35/00 ,  A61P37/02 ,  C07D221/00 ,  C07D263/00 ,  C07D277/00 ,  C07D498/04 ,  C07D498/14 ,  C07D513/04 ,  C07D513/14 ,  C07D517/04 ,  A61K31/44 ,  C07D471/02 ,  C07D487/02 ,  C07D513/02 ,  C07D517/02

CPC classification number: C07D513/04 ,  C07D513/14 ,  C07D517/04

Abstract: Thiazolo-, oxazolo- and selenazolo[4,5-c]quinolin-4-amines and analogs thereof are described including methods of manufacture and the use of novel intermediates. The compounds are immunomodulators and induce cytokine biosynthesis, including interferon and/or tumor biosynthesis, necrosis factor, and inhibit the T-helper-type 2 immune response. The compounds are further useful in the treatment of viral and neoplastic diseases.

公开(公告)号：US5605899A

公开(公告)日：1997-02-25

申请号：US353802

申请日：1994-12-12

Applicant: John F. Gerster ,  Stephen L. Crooks ,  Kyle J. Lindstrom

Inventor： John F. Gerster ,  Stephen L. Crooks ,  Kyle J. Lindstrom

IPC: C07D215/42 ,  C07D471/04 ,  C07D413/06 ,  A61K31/44 ,  A61K31/47

CPC classification number: C07D471/04 ,  C07D215/42

Abstract: 1-substituted, 2-substituted 1H-imidazo[4,5-c]-quinolin-4-amines are disclosed. These compounds function as antiviral agents, they induce biosynthesis of interferon, and they inhibit tumor formation in animal models. This invention also provides intermediates for preparing such compounds, pharmaceutical compositions containing such compounds, and pharmacological methods of using such compounds.

Abstract translation: 1-取代的2-取代的1H-咪唑并[4,5-c] - 喹啉-4-胺。 这些化合物作为抗病毒剂起作用，它们诱导干扰素的生物合成，并且它们抑制动物模型中的肿瘤形成。 本发明还提供了制备此类化合物的中间体，含有这些化合物的药物组合物，以及使用这些化合物的药理学方法。

公开(公告)号：US07598382B2

公开(公告)日：2009-10-06

申请号：US11275553

申请日：2006-01-13

Applicant: David S. Hays ,  Tushar Kshirsagar ,  Philip D. Heppner ,  Bryon A. Merrill ,  Michael E. Danielson ,  John F. Gerster ,  Chad A. Haraldson ,  Sarah Johannessen ,  Maureen A. Kavanagh ,  Kyle J. Lindstrom ,  Michael J. Rice ,  David J. Squire ,  Sarah A. Strong ,  Joshua R. Wurst

Inventor： David S. Hays ,  Tushar Kshirsagar ,  Philip D. Heppner ,  Bryon A. Merrill ,  Michael E. Danielson ,  John F. Gerster ,  Chad A. Haraldson ,  Sarah Johannessen ,  Maureen A. Kavanagh ,  Kyle J. Lindstrom ,  Michael J. Rice ,  David J. Squire ,  Sarah A. Strong ,  Joshua R. Wurst

IPC: C07D471/00

CPC classification number: C07D471/04

Abstract: Aryl substituted imidazoquinoline compounds, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral, and neoplastic, are disclosed.

Abstract translation: 公开了芳基取代的咪唑并喹啉化合物，含有化合物的化合物的药物组合物，中间体和这些化合物作为免疫调节剂的用途，用于诱导或抑制动物中的细胞因子生物合成和治疗包括病毒和肿瘤的疾病。

公开(公告)号：US07038051B2

公开(公告)日：2006-05-02

申请号：US11188418

申请日：2005-07-25

Applicant: John F. Gerster ,  Kyle J. Lindstrom ,  Stephen L. Crooks ,  Philip D. Heppner ,  Gregory J. Marszalek ,  Peter V. Maye ,  Bryon A. Merrill ,  John W. Mickelson ,  Michael J. Rice

Inventor： John F. Gerster ,  Kyle J. Lindstrom ,  Stephen L. Crooks ,  Philip D. Heppner ,  Gregory J. Marszalek ,  Peter V. Maye ,  Bryon A. Merrill ,  John W. Mickelson ,  Michael J. Rice

IPC: C07D471/12 ,  C07D471/00

CPC classification number: C07D471/04 ,  A61K31/4745 ,  A61K45/06 ,  C07D471/14 ,  A61K2300/00

Abstract: Imidazonaphthyridine and tetrahydroimidazonaphthyridine compounds induce the biosynthesis of cytokines such as interferon and tumor necrosis factor. The compounds exhibit antiviral and antitumor properties. Methods of preparing the compounds and intermediates useful in the preparation of the compounds are also disclosed.