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1. 发明授权

US11547704B2 Chemical compounds 有权
公开(公告)号：US11547704B2
公开(公告)日：2023-01-10
申请号：US16898667
申请日：2020-06-11
申请人： GlaxoSmithKline Intellectual Property Development Limited
发明人： Jeffrey Michael Axten , Mui Cheung , Michael P. Demartino , Hilary Schenck Eidam , Raghava Reddy Kethiri , Biswajit Kalita
IPC分类号： A61K31/4468 , A61K31/438 , A61K31/439 , A61K31/445 , A61K31/454 , C07D211/32 , C07D211/58 , C07D211/66 , C07D403/12 , C07D417/12 , C07D471/08 , C07D498/10 , C07D211/26 , C07D211/60 , C07D401/04 , C07D211/56 , C07D211/62 , C07D401/12 , C07D209/52 , C07D405/12 , C07D451/04
摘要： The invention is directed to substituted piperidine derivatives. Specifically, the invention is directed to compounds according to Formula IIII: wherein A, B, X, Y, L1, L2, L3, R1, R2, R3, R4, R5, R6, R9, z2, z4, z5, and z6 are as defined herein, and salts thereof. The compounds of the invention are inhibitors of the ATF4 pathway and can be useful in the treatment of cancer, pre-cancerous syndromes and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, spinal cord injury, traumatic brain injury, ischemic stroke, stroke, diabetes, Parkinson disease, Huntington's disease, Creutzfeldt-Jakob Disease, and related prion diseases, progressive supranuclear palsy, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, inflammation, fibrosis, chronic and acute diseases of the liver, chronic and acute diseases of the lung, chronic and acute diseases of the kidney, chronic traumatic encephalopathy (CTE), neurodegeneration, dementia, cognitive impairment, atherosclerosis, ocular diseases, arrhythmias, in organ transplantation and in the transportation of organs for transplantation. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting the ATF4 pathway and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

2. 发明授权

US09879021B2 Compounds as rearranged during transfection (RET) inhibitors 有权
公开(公告)号：US09879021B2
公开(公告)日：2018-01-30
申请号：US15509569
申请日：2015-09-10
申请人： GlaxoSmithKline Intellectual Property Development Limited
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 , C07D471/04 , C07D413/14 , C07D409/12 , C07D405/14 , C07D401/12 , C07D401/14 , C07D221/04 , C07D217/24 , C07D213/69 , C07D213/64 , C07D401/04 , C07D405/12 , C07D413/12
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.

3. 发明授权

US09035063B2 Compounds as rearranged during transfection (RET) inhibitors 有权
公开(公告)号：US09035063B2
公开(公告)日：2015-05-19
申请号：US14564625
申请日：2014-12-09
申请人： GlaxoSmithKline Intellectual Property Development Limited
发明人： Hilary Schenck Eidam , Huiping Amy Guan , Chengde Wu , Mui Cheung
IPC分类号： C07D413/12 , C07D213/69 , C07D213/75 , C07D401/12
CPC分类号： C07D213/69 , C07D213/75 , 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.

4. 发明申请

US20220315556A1 FURIN INHIBITORS 有权
公开(公告)号：US20220315556A1
公开(公告)日：2022-10-06
申请号：US17054491
申请日：2019-05-10
申请人： Glaxosmithkline Intellectual Property Development Limited
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.

5. 发明授权

US08937071B2 Compounds as rearranged during transfection (RET) inhibitors 有权
标题翻译：转染期间重排的化合物（RET）抑制剂
公开(公告)号：US08937071B2
公开(公告)日：2015-01-20
申请号：US14210726
申请日：2014-03-14
申请人： GlaxoSmithKline Intellectual Property Development Limited
发明人： Hilary Schenck Eidam , Kaushik Raha , Zhen Gong , Huiping Amy Guan , Chengde Wu , Haiying Yang , Haiyu Yu , Zhiliu Zhang , Mui Cheung
IPC分类号： C07D413/12 , C07D213/69 , C07D213/75 , C07D401/12
CPC分类号： C07D213/69 , C07D213/75 , 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.
摘要翻译：本发明涉及作为转染（RET）激酶重排的抑制剂的新化合物，含有它们的药物组合物，其制备方法及其在治疗中单独或组合用于胃肠道敏感性标准化的用途，运动性和/或分泌和/或腹部疾病或疾病和/或与RET功能障碍相关疾病相关的治疗或其中RET活性的调节可具有治疗益处，包括但不限于肠易激综合征（IBS）的所有分类，包括腹泻 - 功能性腹胀，功能性腹泻，功能性腹痛，功能性腹痛综合征，慢性特发性便秘，功能性食管障碍，功能性胃十二指肠疾病，功能性肛门直肠疼痛，炎性肠病，增殖性疾病等作为非小细胞肺癌，肝细胞癌，结肠直肠癌，甲状腺髓样癌，滤泡性甲状腺癌，间变性甲状腺癌，甲状腺乳头状癌，脑肿瘤，腹腔癌，实体瘤，其他肺癌，头颈癌，胶质瘤，神经母细胞瘤，Von Hippel-Lindau综合征和肾肿瘤，乳腺癌，输卵管癌，卵巢癌，移行细胞癌，前列腺癌，食管癌和胃食管结，胆管癌，腺癌和任何具有增加的RET激酶活性的恶性肿瘤。

6. 发明授权

US11773078B2 Furin inhibitors 有权
公开(公告)号：US11773078B2
公开(公告)日：2023-10-03
申请号：US17054491
申请日：2019-05-10
申请人： Glaxosmithkline Intellectual Property Development Limited
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.

7. 发明申请

US20210053955A1 GHRELIN O-ACYLTRANSFERASE INHIBITORS 有权
公开(公告)号：US20210053955A1
公开(公告)日：2021-02-25
申请号：US16967262
申请日：2019-02-05
申请人： Glaxosmithkline Intellectual Property Development Limited
发明人： Anish Bandyopadhyay , Mui Cheung , Hilary Schenck Eidam , Hemant Joshi , Dai-Shi Su
IPC分类号： C07D409/12 , C07D491/048
摘要： This invention relates to novel compounds according to Formula (I) which are inhibitors of ghrelin O-acyltransferase (GOAT), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of metabolic disorders (e.g. Prader-Willi syndrome, metabolic syndrome, insulin resistance, impaired glucose tolerance, prediabetes, diabetes mellitus (e.g., type II diabetes mellitus), dysglycemia (e.g., hyperglycemia), obesity (e.g., obesity caused by Prader-Willi syndrome), increased adiposity, poor glycemic control, hyperphagia, impaired satiety, dyslipidemia (e.g., atherogenic dyslipidemia), hepatic steatosis (e.g., non-alcoholic fatty liver disease (e.g., non-alcoholic steatohepatitis))), psychiatric disorders (e.g., eating disorders (e.g., bulimia nervosa, binge eating disorder, night-time eating syndrome), substance related disorders (e.g., addiction disorders (e.g., alcohol, smoking, overeating, or use of illicit drugs))), as well as disorders related to or complications of metabolic or psychiatric disorders (e.g., cardiovascular diseases (e.g., diabetic heart disease (e.g., diabetic cardiomyopathy), heart failure, or hypertension), ischemia (e.g., myocardial ischemia, cerebral ischemia, ischemic stroke), or BMI-related cancers (e.g., pancreatic cancer, gallbladder cancer, esophageal cancer, colorectal cancer, breast cancer etc.).

8. 发明申请

US20180099976A1 NOVEL COMPOUNDS AS REARRANGED DURING TRANSFECTION (RET) INHIBITORS 审中-公开
公开(公告)号：US20180099976A1
公开(公告)日：2018-04-12
申请号：US15837048
申请日：2017-12-11
申请人： GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
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.

9. 发明授权

US10851053B2 Chemical compounds 有权
公开(公告)号：US10851053B2
公开(公告)日：2020-12-01
申请号：US16307513
申请日：2017-06-07
申请人： GlaxoSmithKline Intellectual Property Development Limited
发明人： Jeffrey Michael Axten , Mui Cheung , Anthony William Dean , Michael P. DeMartino , Hilary Schenck Eidam , Biswajit Kalita , Raghava Reddy Kethiri , Rajendra Kristam
IPC分类号： A61K31/403 , A61K31/4025 , A61K31/4015 , A61K31/44 , A61K31/4439 , C07D209/52 , C07D207/26 , C07D207/09 , C07D401/06 , C07D401/12 , C07D401/14 , A61P25/28 , A61P25/00 , A61P35/00 , C07D487/10 , C07D405/06 , C07D405/12 , C07D487/04
摘要： The invention is directed to substituted pyrrolidine derivatives. Specifically, the invention is directed to compounds according to Formula III: wherein A, B, L1, L2, L3, R1, R2, R3, R4, R5, R6, R9, R10, R30, Y1, Y2, z2, z4, z5, and z6 are as defined herein, and salts thereof. The compounds of the invention are inhibitors of the ATF4 pathway and can be useful in the treatment of cancer, pre-cancerous syndromes and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, spinal cord injury, traumatic brain injury, ischemic stroke, stroke, diabetes, Parkinson disease, Huntington's disease, Creutzfeldt-Jakob Disease, and related prion diseases, progressive supranuclear palsy, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, inflammation, fibrosis, chronic and acute diseases of the liver, chronic and acute diseases of the lung, chronic and acute diseases of the kidney, chronic traumatic encephalopathy (CTE), neurodegeneration, dementia, cognitive impairment, atherosclerosis, ocular diseases, arrhythmias, in organ transplantation and in the transportation of organs for transplantation. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting the ATF4 pathway and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

10. 发明申请

US20220213076A1 GHRELIN O-ACYLTRANSFERASE INHIBITORS 有权
公开(公告)号：US20220213076A1
公开(公告)日：2022-07-07
申请号：US17703891
申请日：2022-03-24
申请人： Glaxosmithkline Intellectual Property Development Limited
发明人： Anish Bandyopadhyay , Mui Cheung , Hilary Schenck Eidam , Hemant Joshi , Dai-Shi Su
IPC分类号： C07D409/12 , C07D491/048
摘要： This invention relates to novel compounds according to Formula (I) which are inhibitors of ghrelin O-acyltransferase (GOAT), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of metabolic disorders (e.g. Prader-Willi syndrome, metabolic syndrome, insulin resistance, impaired glucose tolerance, prediabetes, diabetes mellitus (e.g., type II diabetes mellitus), dysglycemia (e.g., hyperglycemia), obesity (e.g., obesity caused by Prader-Willi syndrome), increased adiposity, poor glycemic control, hyperphagia, impaired satiety, dyslipidemia (e.g., atherogenic dyslipidemia), hepatic steatosis (e.g., non-alcoholic fatty liver disease (e.g., non-alcoholic steatohepatitis))), psychiatric disorders (e.g., eating disorders (e.g., bulimia nervosa, binge eating disorder, night-time eating syndrome), substance related disorders (e.g., addiction disorders (e.g., alcohol, smoking, overeating, or use of illicit drugs))), as well as disorders related to or complications of metabolic or psychiatric disorders (e.g., cardiovascular diseases (e.g., diabetic heart disease (e.g., diabetic cardiomyopathy), heart failure, or hypertension), ischemia (e.g., myocardial ischemia, cerebral ischemia, ischemic stroke), or BMI-related cancers (e.g., pancreatic cancer, gallbladder cancer, esophageal cancer, colorectal cancer, breast cancer etc.).

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