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公开(公告)号:US10294236B2
公开(公告)日:2019-05-21
申请号:US15837048
申请日:2017-12-11
发明人: Mui Cheung , Michael P. Demartino , Hilary Schenck Eidam , Huiping Amy Guan , Donghui Qin , Chengde Wu , Zhen Gong , Haiying Yang , Haiyu Yu , Zhiliu Zhang
IPC分类号: C07D491/048 , C07D409/12 , C07D217/24 , C07D413/14 , C07D405/14 , C07D221/04 , C07D401/14 , C07D471/04 , C07D213/75 , C07D221/00 , C07D401/04 , C07D401/12 , C07D403/04 , C07D405/04 , C07D405/12 , C07D407/12 , C07D413/12 , C07D213/64 , C07D213/65 , C07D213/69
摘要: This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung cancer, hepatocellular carcinoma, colorectal cancer, medullary thyroid cancer, follicular thyroid cancer, anaplastic thyroid cancer, papillary thyroid cancer, brain tumors, peritoneal cavity cancer, solid tumors, other lung cancer, head and neck cancer, gliomas, neuroblastomas, Von Hippel-Lindau Syndrome and kidney tumors, breast cancer, fallopian tube cancer, ovarian cancer, transitional cell cancer, prostate cancer, cancer of the esophagus and gastroesophageal junction, biliary cancer, adenocarcinoma, and any malignancy with increased RET kinase activity.
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公开(公告)号:US10111866B2
公开(公告)日:2018-10-30
申请号:US15877524
申请日:2018-01-23
IPC分类号: A61K31/4439 , A61K31/4412 , C07D213/69 , C07D401/12 , C07D413/12
摘要: This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung cancer, hepatocellular carcinoma, colorectal cancer, medullary thyroid cancer, follicular thyroid cancer, anaplastic thyroid cancer, papillary thyroid cancer, brain tumors, peritoneal cavity cancer, solid tumors, other lung cancer, head and neck cancer, gliomas, neuroblastomas, Von Hippel-Lindau Syndrome and kidney tumors, breast cancer, fallopian tube cancer, ovarian cancer, transitional cell cancer, prostate cancer, cancer of the esophagus and gastroesophageal junction, biliary cancer, adenocarcinoma, and any malignancy with increased RET kinase activity.
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公开(公告)号:US09650364B2
公开(公告)日:2017-05-16
申请号:US14762905
申请日:2014-02-19
发明人: Linda N. Casillas , Adam Kenneth Charnley , Xiaoyang Dong , Pamela A. Haile , Michael P. Demartino , John F. Mehlmann
IPC分类号: C07D403/12 , C07D405/14 , A61K9/20 , A61K9/48
CPC分类号: C07D403/12 , A61K9/2054 , A61K9/4866 , C07D405/14
摘要: Disclosed are compounds that are inhibitors of RIP2 kinase and methods of making and using the same.
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公开(公告)号:US20220315556A1
公开(公告)日:2022-10-06
申请号:US17054491
申请日:2019-05-10
发明人: Jeffrey Michael Axten , Mui Cheung , Michael P. Demartino , Huiping Amy Guan , Yan Hu , Aaron Bayne Miller , Donghui Qin , Chengde Wu , Zhiliu Zhang , Xiaojuan Lin
IPC分类号: C07D401/14 , A61P11/00 , C07D401/12 , C07D211/26 , C07D487/08
摘要: This invention relates to novel compounds according to Formula (I) which are inhibitors of furin, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of fibrotic diseases, including pulmonary fibrosis, renal fibrosis, liver fibrosis, skin fibrosis, ocular fibrosis, cardiac fibrosis, and other miscellaneous fibrotic conditions. The disclosed compounds may also be useful for treating other furin-mediated conditions, including but not limited to, hypertension, cancer, infectious diseases, and genetic disorders (e.g., cystic fibrosis (CF)), and neurodegenerative disorders.
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公开(公告)号:US20190247382A1
公开(公告)日:2019-08-15
申请号:US16376858
申请日:2019-04-05
IPC分类号: A61K31/4439 , A61K31/4412 , C07D213/69
摘要: This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung cancer, hepatocellular carcinoma, colorectal cancer, medullary thyroid cancer, follicular thyroid cancer, anaplastic thyroid cancer, papillary thyroid cancer, brain tumors, peritoneal cavity cancer, solid tumors, other lung cancer, head and neck cancer, gliomas, neuroblastomas, Von Hippel-Lindau Syndrome and kidney tumors, breast cancer, fallopian tube cancer, ovarian cancer, transitional cell cancer, prostate cancer, cancer of the esophagus and gastroesophageal junction, biliary cancer, adenocarcinoma, and any malignancy with increased RET kinase activity.
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公开(公告)号:US09994529B2
公开(公告)日:2018-06-12
申请号:US15431942
申请日:2017-02-14
发明人: Michael Jonathan Bury , Linda N. Casillas , Adam K. Charnley , Michael P. Demartino , Xiaoyang Dong , Patrick M. Eidam , Pamela A. Haile , Robert W. Marquis, Jr. , Joshi M. Ramanjulu , Joseph J. Romano , Ami Lakdawala Shah , Robert R. Singhaus, Jr. , Gren Wang
IPC分类号: C07D239/94 , C07D403/12 , C07D417/12 , C07D417/14 , C07D471/04
CPC分类号: C07D239/94 , C07D403/12 , C07D417/12 , C07D417/14 , C07D471/04
摘要: Disclosed are compounds having the formula: wherein R1, R2, R3, and Z are as defined herein, and methods of making and using the same.
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公开(公告)号:US09216965B2
公开(公告)日:2015-12-22
申请号:US14396559
申请日:2013-09-13
发明人: Linda N. Casillas , Michael P. Demartino , Pamela A. Haile , John F. Mehlmann , Joshi M. Ramanjulu , Robert Singhaus, Jr.
IPC分类号: C07D401/12
CPC分类号: C07D401/12
摘要: Disclosed are compounds having the formula: wherein R1, R2R3, R4 and R5 are as defined herein, and methods of making and using the same.
摘要翻译: 公开了具有下式的化合物:其中R1,R2R3,R4和R5如本文所定义,以及制备和使用它们的方法。
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公开(公告)号:US11773078B2
公开(公告)日:2023-10-03
申请号:US17054491
申请日:2019-05-10
发明人: Jeffrey Michael Axten , Mui Cheung , Michael P. Demartino , Huiping Amy Guan , Yan Hu , Aaron Bayne Miller , Donghui Qin , Chengde Wu , Zhiliu Zhang , Xiaojuan Lin
IPC分类号: C07D401/12 , C07D401/14 , A61P11/00 , C07D211/26 , C07D487/08
CPC分类号: C07D401/14 , A61P11/00 , C07D211/26 , C07D401/12 , C07D487/08
摘要: This invention relates to novel compounds according to Formula (I) which are inhibitors of furin, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of fibrotic diseases, including pulmonary fibrosis, renal fibrosis, liver fibrosis, skin fibrosis, ocular fibrosis, cardiac fibrosis, and other miscellaneous fibrotic conditions. The disclosed compounds may also be useful for treating other furin-mediated conditions, including but not limited to, hypertension, cancer, infectious diseases, and genetic disorders (e.g., cystic fibrosis (CF)), and neurodegenerative disorders.
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公开(公告)号:US20180099976A1
公开(公告)日:2018-04-12
申请号:US15837048
申请日:2017-12-11
发明人: Mui Cheung , Michael P. Demartino , Hilary Schenck Eidam , Huiping Amy Guan , Donghui Qin , Chengde Wu , Zhen Gong , Haiying Yang , Haiyu Yu , Zhiliu Zhang
IPC分类号: C07D491/048 , C07D409/12 , C07D217/24 , C07D413/14 , C07D405/14 , C07D221/04 , C07D213/69 , C07D401/14 , C07D471/04 , C07D413/12 , C07D405/12 , C07D213/64 , C07D401/04 , C07D401/12
CPC分类号: C07D491/048 , C07B2200/13 , C07D213/64 , C07D213/65 , C07D213/69 , C07D213/75 , C07D217/24 , C07D221/00 , C07D221/04 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D471/04
摘要: This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung cancer, hepatocellular carcinoma, colorectal cancer, medullary thyroid cancer, follicular thyroid cancer, anaplastic thyroid cancer, papillary thyroid cancer, brain tumors, peritoneal cavity cancer, solid tumors, other lung cancer, head and neck cancer, gliomas, neuroblastomas, Von Hippel-Lindau Syndrome and kidney tumors, breast cancer, fallopian tube cancer, ovarian cancer, transitional cell cancer, prostate cancer, cancer of the esophagus and gastroesophageal junction, biliary cancer, adenocarcinoma, and any malignancy with increased RET kinase activity.
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公开(公告)号:US09918974B2
公开(公告)日:2018-03-20
申请号:US15509613
申请日:2015-09-09
IPC分类号: A61K31/4412 , C07D413/12 , C07D401/12 , C07D213/69 , A61K31/4439
CPC分类号: A61K31/4439 , A61K31/4412 , C07D213/69 , C07D401/12 , C07D413/12
摘要: This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung cancer, hepatocellular carcinoma, colorectal cancer, medullary thyroid cancer, follicular thyroid cancer, anaplastic thyroid cancer, papillary thyroid cancer, brain tumors, peritoneal cavity cancer, solid tumors, other lung cancer, head and neck cancer, gliomas, neuroblastomas, Von Hippel-Lindau Syndrome and kidney tumors, breast cancer, fallopian tube cancer, ovarian cancer, transitional cell cancer, prostate cancer, cancer of the esophagus and gastroesophageal junction, biliary cancer, adenocarcinoma, and any malignancy with increased RET kinase activity.
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