公开(公告)号：US06300353B1

公开(公告)日：2001-10-09

申请号：US09263027

申请日：1999-03-05

申请人： Tadakatsu Hayase ,  Shigeyasu Ichihara ,  Yoshiaki Isshiki ,  Pingli Liu ,  Jun Ohwada ,  Toshiya Sakai ,  Nobuo Shimma ,  Masao Tsukazaki ,  Isao Umeda ,  Toshikazu Yamazaki

发明人： Tadakatsu Hayase ,  Shigeyasu Ichihara ,  Yoshiaki Isshiki ,  Pingli Liu ,  Jun Ohwada ,  Toshiya Sakai ,  Nobuo Shimma ,  Masao Tsukazaki ,  Isao Umeda ,  Toshikazu Yamazaki

IPC分类号： C07D41706

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

摘要： Azole derivatives of the formula I wherein R14, R15 are each independently hydrogen or fluorine, T is a group of the formula: wherein R9 is pyrrolidinyl or a group A—NH—B—, A is hydrogen or straight-chain or branched C1-C5 alkyl; B is straight-chain or branched C1-C4 alkylene, —CH2—CONH—CH2 or —CH2CH2CH2—CH(NH2); and X− is a pharmaceutically acceptable anion; and pharmaceutically acceptable salts of said compounds, and hydrates and solvates of the compounds of formula I and the salts thereof can be used in the production of medicaments for treating fungal infections and mycoses.

摘要翻译： 式I其中R 14，R 15各自独立地为氢或氟的唑衍生物，T为下式的基团：其中R 9为吡咯烷基或A-NH-B-A基团，A为氢或直链或支链C 1 -C 5烷基; B是直链或支链C1-C4亚烷基，-CH2-CONH-CH2或-CH2CH2CH2-CH（NH2）; 和X-是药学上可接受的阴离子;所述化合物的药学上可接受的盐，以及式I化合物及其盐的水合物和溶剂合物可用于生产用于治疗真菌感染和真菌病的药物。

公开(公告)号：US08993582B2

公开(公告)日：2015-03-31

申请号：US13761830

申请日：2013-02-07

申请人： Jiacheng Zhou ,  David Meloni ,  Pingli Liu ,  Brian W. Metcalf ,  Tai-Yuen Yue

发明人： Jiacheng Zhou ,  David Meloni ,  Pingli Liu ,  Brian W. Metcalf ,  Tai-Yuen Yue

IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D487/00 ,  C07D487/04 ,  C07F7/18 ,  C07F7/10

CPC分类号： C07D487/04 ,  C07F5/025 ,  C07F7/083 ,  C07F7/10 ,  C07F7/1892 ,  Y02P20/55

摘要： The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines of Formula III, and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases.

公开(公告)号：US08410265B2

公开(公告)日：2013-04-02

申请号：US12687623

申请日：2010-01-14

申请人： Jiacheng Zhou ,  Pingli Liu ,  Qiyan Lin ,  Brian W. Metcalf ,  David Meloni ,  Yongchun Pan ,  Michael Xia ,  Mei Li ,  Tai-Yuen Yue ,  James D. Rodgers ,  Haisheng Wang

发明人： Jiacheng Zhou ,  Pingli Liu ,  Qiyan Lin ,  Brian W. Metcalf ,  David Meloni ,  Yongchun Pan ,  Michael Xia ,  Mei Li ,  Tai-Yuen Yue ,  James D. Rodgers ,  Haisheng Wang

IPC分类号： C07D487/00

CPC分类号： C07D487/04 ,  C07F5/025 ,  C07F7/083 ,  C07F7/10 ,  C07F7/1892 ,  Y02P20/55

摘要： The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines of Formula III, and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases.

公开(公告)号：US08420645B2

公开(公告)日：2013-04-16

申请号：US12469360

申请日：2009-05-20

申请人： Lingkai Weng ,  Lei Qiao ,  Jiacheng Zhou ,  Pingli Liu ,  Yongchun Pan

发明人： Lingkai Weng ,  Lei Qiao ,  Jiacheng Zhou ,  Pingli Liu ,  Yongchun Pan

IPC分类号： A01N43/64 ,  A61K31/53 ,  C07D251/00

CPC分类号： A61K31/53 ,  C07D253/07 ,  C07D401/10 ,  C07D487/04

摘要： The present invention is directed to dihydrochloric acid and dibenzenesulfonic acid salts of the c-Met kinase inhibitor 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)-imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and pharmaceutical compositions thereof, useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. The present invention further relates to processes and intermediates for preparing 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and salts thereof.

摘要翻译： 本发明涉及c-Met激酶抑制剂2-氟-N-甲基-4- [7-（喹啉-6-基甲基） - 咪唑并[1,2-b] [1]的二氯氯酸和二苯磺酸盐 ，2,4]三嗪-2-基]苯甲酰胺及其药物组合物，其可用于治疗与激酶途径失调相关的癌症和其它疾病。 本发明还涉及制备2-氟-N-甲基-4- [7-（喹啉-6-基甲基）咪唑并[1,2-b] [1,2,4]三嗪-2-酮的方法和中间体， 吡啶-2-基]苯甲酰胺及其盐。

公开(公告)号：US20130060026A1

公开(公告)日：2013-03-07

申请号：US13605331

申请日：2012-09-06

申请人： Jiacheng Zhou ,  Yongzhong Wu ,  Pingli Liu ,  Ganfeng Cao

发明人： Jiacheng Zhou ,  Yongzhong Wu ,  Pingli Liu ,  Ganfeng Cao

IPC分类号： C07D487/04 ,  C07D491/113 ,  C07D401/06 ,  C07F7/02

CPC分类号： C07D491/113 ,  C07D401/06 ,  C07D487/04 ,  C07D491/10

摘要： This invention relates to processes and intermediates for making {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, useful in the treatment of diseases related to the activity of Janus kinases (JAK) including inflammatory disorders, autoimmune disorders, cancer, and other diseases.

公开(公告)号：US20100190981A1

公开(公告)日：2010-07-29

申请号：US12687623

申请日：2010-01-14

申请人： Jiacheng Zhou ,  Pingli Liu ,  Qiyan Lin ,  Brian W. Metcalf ,  David Meloni ,  Yongchun Pan ,  Michael Xia ,  Mei Li ,  Tai-Yuen Yue ,  James D. Rodgers ,  Haisheng Wang

发明人： Jiacheng Zhou ,  Pingli Liu ,  Qiyan Lin ,  Brian W. Metcalf ,  David Meloni ,  Yongchun Pan ,  Michael Xia ,  Mei Li ,  Tai-Yuen Yue ,  James D. Rodgers ,  Haisheng Wang

IPC分类号： C07D487/04 ,  C07D231/16 ,  C07F5/02

CPC分类号： C07D487/04 ,  C07F5/025 ,  C07F7/083 ,  C07F7/10 ,  C07F7/1892 ,  Y02P20/55

摘要： The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines of Formula III, and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases.

摘要翻译： 本发明涉及制备式III的手性取代吡唑并吡咯并[2,3-d]嘧啶的方法和相关的合成中间体化合物。 手性取代的吡唑基吡咯并[2,3-d]嘧啶可用作Janus Kinase家族蛋白酪氨酸激酶（JAKs）的抑制剂，用于治疗炎性疾病，骨髓增生性疾病和其他疾病。

公开(公告)号：US06376491B1

公开(公告)日：2002-04-23

申请号：US09464240

申请日：1999-12-15

申请人： Yuhko Aoki ,  Hirosato Ebiike ,  Toshihiko Fujii ,  Kenichi Kawasaki ,  Pingli Liu ,  Miyako Masubuchi ,  Tatsuo Ohtsuka ,  Shinji Tsujii

发明人： Yuhko Aoki ,  Hirosato Ebiike ,  Toshihiko Fujii ,  Kenichi Kawasaki ,  Pingli Liu ,  Miyako Masubuchi ,  Tatsuo Ohtsuka ,  Shinji Tsujii

IPC分类号： A61K31535

CPC分类号： C07D307/79 ,  C07D307/85 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07F9/65517

摘要： The present invention is directed to new bicyclic compounds of the formula [I], and pharmaceutically acceptable salts thereof wherein R1, R2, R3, R4, R5, R6, R7, Q1 Q2 and Q3 are as defined in the claims. The compounds have N-myristoyltransferase inhibitory and antifungal activity.

摘要翻译： 本发明涉及式[I]的新的双环化合物及其药学上可接受的盐，其中R1，R2，R3，R4，R5，R6，R7，Q1 Q2和Q3如权利要求中所定义。 该化合物具有N-肉豆蔻酰转移酶抑制和抗真菌活性。

公开(公告)号：US08901123B2

公开(公告)日：2014-12-02

申请号：US13793864

申请日：2013-03-11

申请人： Lingkai Weng ,  Lei Qiao ,  Jiacheng Zhou ,  Pingli Liu ,  Yongchun Pan

发明人： Lingkai Weng ,  Lei Qiao ,  Jiacheng Zhou ,  Pingli Liu ,  Yongchun Pan

IPC分类号： A01N43/64 ,  A61K31/53 ,  C07D487/00

CPC分类号： A61K31/53 ,  C07D253/07 ,  C07D401/10 ,  C07D487/04

摘要： The present invention is directed to dihydrochloric acid and dibenzenesulfonic acid salts of the c-Met kinase inhibitor 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)-imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and pharmaceutical compositions thereof, useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. The present invention further relates to processes and intermediates for preparing 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and salts thereof.

摘要翻译： 本发明涉及c-Met激酶抑制剂2-氟-N-甲基-4- [7-（喹啉-6-基甲基） - 咪唑并[1,2-b] [1]的二氯氯酸和二苯磺酸盐 ，2,4]三嗪-2-基]苯甲酰胺及其药物组合物，其可用于治疗与激酶途径失调相关的癌症和其它疾病。 本发明还涉及制备2-氟-N-甲基-4- [7-（喹啉-6-基甲基）咪唑并[1,2-b] [1,2,4]三嗪-2-酮的方法和中间体， 吡啶-2-基]苯甲酰胺及其盐。

公开(公告)号：US08796319B2

公开(公告)日：2014-08-05

申请号：US13294711

申请日：2011-11-11

申请人： Andrew P. Combs ,  Eddy W. Yue ,  Richard B. Sparks ,  Wenyu Zhu ,  Jiacheng Zhou ,  Qiyan Lin ,  Lingkai Weng ,  Tai-Yuen Yue ,  Pingli Liu

发明人： Andrew P. Combs ,  Eddy W. Yue ,  Richard B. Sparks ,  Wenyu Zhu ,  Jiacheng Zhou ,  Qiyan Lin ,  Lingkai Weng ,  Tai-Yuen Yue ,  Pingli Liu

IPC分类号： A61K31/4245 ,  C07D413/12 ,  C07D271/08

CPC分类号： A61K31/4245 ,  A61K39/0011 ,  A61K39/3955 ,  C07D271/08 ,  C07D413/04 ,  C07D413/12

摘要： The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives.

公开(公告)号：US20090233903A1

公开(公告)日：2009-09-17

申请号：US12401348

申请日：2009-03-10

申请人： James D. Rodgers ,  Stacey Shepard ,  Yun-Long Li ,  Jiacheng Zhou ,  Pingli Liu ,  David Meloni ,  Michael Xia

发明人： James D. Rodgers ,  Stacey Shepard ,  Yun-Long Li ,  Jiacheng Zhou ,  Pingli Liu ,  David Meloni ,  Michael Xia

IPC分类号： A61K31/519 ,  C07D487/04 ,  A61P35/00

CPC分类号： C07D487/04 ,  B60Q3/76 ,  B60Q3/80 ,  Y10S362/80 ,  Y10S362/802

摘要： The present invention relates to azetidine and cyclobutane derivatives, as well as their compositions, methods of use, and processes for preparation, which are JAK inhibitors useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.

摘要翻译： 本发明涉及氮杂环丁烷和环丁烷衍生物，以及它们的组合物，使用方法和制备方法，其是可用于治疗JAK相关疾病（包括例如炎性和自身免疫性疾病）的JAK抑制剂，以及 作为癌症。