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    NOVEL COMPOUNDS AS REARRANGED DURING TRANSFECTION (RET) INHIBITORS
    1.
    发明申请
    NOVEL COMPOUNDS AS REARRANGED DURING TRANSFECTION (RET) INHIBITORS 审中-公开

    公开(公告)号：US20190022078A1

    公开(公告)日：2019-01-24

    申请号：US16145271

    申请日：2018-09-28

    Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

    Inventor： Michael P. DEMARTINO ,  Huiping Amy GUAN

    IPC: A61K31/4439 ,  C07D213/69 ,  A61K31/4412 ,  C07D413/12 ,  C07D401/12

    Abstract: 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.

    NOVEL COMPOUNDS AS REARRANGED DURING TRANSFECTION (RET) INHIBITORS
    2.
    发明申请
    NOVEL COMPOUNDS AS REARRANGED DURING TRANSFECTION (RET) INHIBITORS 审中-公开

    公开(公告)号：US20180147194A1

    公开(公告)日：2018-05-31

    申请号：US15877524

    申请日：2018-01-23

    Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

    Inventor： Michael P. DEMARTINO ,  Huiping Amy GUAN

    IPC: A61K31/4439 ,  C07D213/69 ,  A61K31/4412 ,  C07D413/12 ,  C07D401/12

    CPC classification number: A61K31/4439 ,  A61K31/4412 ,  C07D213/69 ,  C07D401/12 ,  C07D413/12

    Abstract: 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.

    PYRIDONE DERIVATIVES AS REARRANGED DURING TRANSFECTION (RET) KINASE INHIBITORS
    3.
    发明申请
    PYRIDONE DERIVATIVES AS REARRANGED DURING TRANSFECTION (RET) KINASE INHIBITORS 有权

    公开(公告)号：US20170340617A1

    公开(公告)日：2017-11-30

    申请号：US15509613

    申请日：2015-09-09

    Applicant: GlaxoSmithKline Intellectual Property Development Limited

    Inventor： Michael P. DEMARTINO ,  Huiping Amy GUAN

    IPC: A61K31/4439 ,  C07D213/69 ,  A61K31/4412 ,  C07D401/12 ,  C07D413/12

    CPC classification number: A61K31/4439 ,  A61K31/4412 ,  C07D213/69 ,  C07D401/12 ,  C07D413/12

    Abstract: 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.

    CHEMICAL COMPOUNDS
    5.
    发明申请
    CHEMICAL COMPOUNDS 有权

    公开(公告)号：US20210253528A1

    公开(公告)日：2021-08-19

    申请号：US16973587

    申请日：2019-07-08

    Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

    Inventor： Michael P. DEMARTINO ,  Karen Anderson EVANS ,  Israil PENDRAK ,  Joseph E. PERO

    IPC: C07D213/64 ,  C07C271/28 ,  C07C275/30 ,  C07C235/20 ,  C07D207/273 ,  A61K45/06 ,  A61K31/506

    Abstract: The invention is directed to substituted carbon-linked bicycloalkane derivatives. Specifically, the invention is directed to compounds according to Formula (X): wherein C′, D′, L2′, L3′, R2′, R3′, R4′, R5′, R6′, R7′, R8′, z2′, z3′, z4′, z5′, z6′, X1, and X2 are as defined herein; or a salt thereof including a pharmaceutically acceptable salt 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, neurological disorders, pain, 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.

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