公开(公告)号：US20080015184A1

公开(公告)日：2008-01-17

申请号：US11570567

申请日：2005-06-14

Applicant: Tushar Kshirsagar ,  George Griesgraber ,  Sarah Johannessen ,  Azim Celebi ,  Philip Heppner ,  Gregory Lundquist Jr. ,  David Amos ,  Bernhard ZImmermann ,  Scott Langer

Inventor： Tushar Kshirsagar ,  George Griesgraber ,  Sarah Johannessen ,  Azim Celebi ,  Philip Heppner ,  Gregory Lundquist Jr. ,  David Amos ,  Bernhard ZImmermann ,  Scott Langer

IPC: A61K31/437 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61P31/12 ,  A61P35/00 ,  C07D243/08 ,  C07D279/12 ,  C07D401/14 ,  C07D413/14 ,  C07D471/04

CPC classification number: C07D471/04 ,  C07D471/14

Abstract: Imidazopyridine, imidazoquinoline, and imidazonaphthyridine compounds having a urea substituent at the 2-position, pharmaceutical compositions containing the compounds, intermediates, and methods of making and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.

Abstract translation: 咪唑并吡啶，咪唑并喹啉和咪唑并吡啶化合物在2-位上具有尿素取代基，含有化合物的药物组合物，中间体及其制备方法以及这些化合物作为免疫调节剂的用途，用于调节动物中的细胞因子生物合成和治疗 公开了包括病毒和肿瘤疾病在内的疾病。

公开(公告)号：US20070259881A1

公开(公告)日：2007-11-08

申请号：US11570715

申请日：2005-06-17

Applicant: Joseph Dellaria ,  Tushar Kshirsagar ,  Shri Niwas ,  William Moser ,  Joan Moseman ,  Kyle Lindstrom ,  Azim Celebi ,  John Gerster ,  Philip Heppner ,  Joshua Wurst

Inventor： Joseph Dellaria ,  Tushar Kshirsagar ,  Shri Niwas ,  William Moser ,  Joan Moseman ,  Kyle Lindstrom ,  Azim Celebi ,  John Gerster ,  Philip Heppner ,  Joshua Wurst

IPC: A61K31/44 ,  A61K31/437 ,  A61K31/496 ,  A61P31/12 ,  A61P35/00 ,  C07D401/02 ,  C07D401/14 ,  C07D471/02

CPC classification number: C07D471/04

Abstract: Imidazo ring systems, which include, for example, imidazopyridine, imidazoquinoline, 6,7,8,9-tetrahydroimidazoquinoline, imidazonaphthyridine, and 6,7,8,9-tetrahydroimidazonaphthyridine compounds substituted at the 1-position and/or the 2-position, pharmaceutical compositions containing these 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.

Abstract translation: 咪唑环体系，其包括例如咪唑并吡啶，咪唑并喹啉，6,7,8,9-四氢咪唑并喹啉，咪唑并吡啶和6,7,8,9-四氢咪唑并吡啶化合物，其在1-位和/或2-位上被取代 公开了含有这些化合物的药物组合物，制备这些化合物的方法，以及这些化合物用作免疫调节剂的方法，用于诱导动物中的细胞因子生物合成和治疗包括病毒和肿瘤疾病在内的疾病。

公开(公告)号：US20070191604A1

公开(公告)日：2007-08-16

申请号：US11636954

申请日：2006-12-11

Applicant: Alan Cooper ,  Yongqi Deng ,  Gerald Shipps ,  Neng-Yang Shih ,  Hugh Zhu ,  Robert Sun ,  Joseph Kelly ,  Ronald Doll ,  Yang Nan ,  Tong Wang ,  Jagdish Desai ,  James Wang ,  Youhao Dong ,  Vincent Madison ,  Li Xiao ,  Alan Hruza ,  M. Siddiqui ,  Ahmed Samatar ,  Sunil Paliwal ,  Hon-Chung Tsui ,  Azim Celebi ,  Yiji Wu ,  Sobhana Boga

Inventor： Alan Cooper ,  Yongqi Deng ,  Gerald Shipps ,  Neng-Yang Shih ,  Hugh Zhu ,  Robert Sun ,  Joseph Kelly ,  Ronald Doll ,  Yang Nan ,  Tong Wang ,  Jagdish Desai ,  James Wang ,  Youhao Dong ,  Vincent Madison ,  Li Xiao ,  Alan Hruza ,  M. Siddiqui ,  Ahmed Samatar ,  Sunil Paliwal ,  Hon-Chung Tsui ,  Azim Celebi ,  Yiji Wu ,  Sobhana Boga

IPC: C07D417/14 ,  C07D413/14 ,  C07D403/14

CPC classification number: C07D405/14 ,  C07D231/56 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/14

Abstract: Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.

Abstract translation: 公开了式1.0的ERK抑制剂及其药学上可接受的盐和溶剂化物。 Q是可以具有桥或稠合环的哌啶或哌嗪环。 哌啶环可以在环中具有双键。 所有其他取代基如本文所定义。 还公开了使用式1.0化合物治疗癌症的方法。

公开(公告)号：US20070167476A1

公开(公告)日：2007-07-19

申请号：US10596895

申请日：2004-12-22

Applicant: Tushar Kshirsagar ,  George Griesgraber ,  Azim Celebi ,  Philip Heppner

Inventor： Tushar Kshirsagar ,  George Griesgraber ,  Azim Celebi ,  Philip Heppner

IPC: A61K31/4745 ,  C07D487/22

CPC classification number: C07D471/14 ,  C07D471/04

Abstract: Piperazine, [1,4]diazepane, [1,4]diazocane, and [1,5]diazocane fused imidazo ring compounds (i.e., imidazoquinolines, tetrahydroimidazoquinolines, imidazonaphthyridines, tetrahydroimidazonaphthyridines, and imidazopyridines), pharmaceutical compositions containing the compounds, intermediates, methods of making, 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 diseases are disclosed.

Abstract translation: 哌嗪，[1,4]二氮杂环庚烷，[1,4]二氮杂环辛烷和[1,5]二氮辛烷稠合的咪唑环化合物（即咪唑并喹啉，四氢咪唑并喹啉，咪唑并噻嗪，四氢咪唑并萘啶和咪唑并吡啶） 公开了制备方法以及这些化合物作为免疫调节剂用于诱导或抑制动物细胞因子生物合成和治疗包括病毒和肿瘤疾病在内的疾病的方法。