1401464-09-2Relevant articles and documents
NOVEL INHIBITORS OF AUTOTAXIN
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Page/Page column 30-33, (2022/01/12)
The present invention relates to novel heterocyclic compounds of general formula (I) and their pharmaceutically acceptable salts, enantiomers and their diastereomers that are autotaxin (ATX) inhibitors. Compounds of general formula (I), their pharmaceutically acceptable salts and pharmaceutical composition are useful for the treatment and prophylaxis of conditions or a disorder caused by autotaxin (ATX) activation or increased concentration of lysophosphatidic acid (LPA).
Polycyclic amide derivative as CDK9 inhibitor, and preparation method and application thereof
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Paragraph 0353-0356; 0360-0362, (2021/07/24)
The invention belongs to the technical field of polycyclic amide derivatives, and particularly relates to a polycyclic amide derivative as a CDK9 inhibitor, and a preparation method and application thereof. The polycyclic amide derivative shows excellent CDK9 enzyme inhibitory activity, and can be used for preparing drugs for treating cancers, especially hematologic cancers including acute myeloid leukemia, multiple myeloma, chronic lymphocytic leukemia, follicular lymphoma and the like and solid tumors, such as acute myeloid leukemia, multiple myeloma, chronic lymphocytic leukemia and follicular lymphoma, including breast cancer, prostate cancer, ovarian cancer, hepatocellular carcinoma, pancreatic cancer, kidney cancer, stomach cancer, colorectal cancer, lung cancer and the like.
SUB-TYPE SELECTIVE AZABICYCLOALKANE DERIVATIVES
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, (2008/12/04)
Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide, ketone, and ester compounds prepared from certain azabicycloalkane carboxylic acids. The resulting compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the a4?2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, such as those disorders characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle).