122450-96-8Relevant articles and documents
LPA RECEPTOR ANTAGONISTS AND USES THEREOF
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, (2021/12/17)
The present disclosure relates generally to compounds that bind to Lysophosphatidic Acid Receptor 1 (LPAR1) and act as antagonists of LPAR1. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of LPAR1, including fibrosis and liver diseases such as non alcoholic steatohepatitis (NASH).
5-(1 H-BENZO[D]IMIDAZO-2-YL)-PYRIDIN-2-AMINE AND 5-(3H-IMIDAZO[4,5-B]PYRIDIN-6-YL)-PYRIDIN-2-AMINE DERIVATIVES AS C-MYC AND P300/CBP HISTONE ACETYLTRANSFERASE INHIBITORS FOR TREATING CANCER
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Page/Page column 175, (2019/04/10)
The invention is directed to substituted 5-(1H-benzo[d]imidazo-2-yl)- pyridin-2-amine and 5-(3H-imidazo[4,5-b]pyridin-6-yl)-pyridin-2-amine derivatives. Specifically, the invention is directed to compounds according to Formula (lb) wherein R', R2', R3', R4', Rs', R6', R7', and X1' are as defined herein; or a salt thereof including a pharmaceutically acceptable salt thereof. The compounds of the invention decrease MYC protein (c-MYC) in cells and/or inhibit p300/CBP histone acetyltransferase and can be useful in the treatment of cardiac hypertrophy, diabetes, obesity and nonalcoholic fatty liver disease, HIV, polycystic kidney disease, inflammatory diseases, ankylosing spondylitis, psoriasis, psoriatic arthritis, rheumatoid arthritis, Crohn's disease, multiple sclerosis, cancer and pre-cancerous syndromes, and diseases associated with dysregulation of Myc or inhibition of p300/CBP histone acetyltransferase. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention still further discloses methods of reducing MYC protein (c-MYC) in cells and inhibiting p300/CBP histone acetyltransferase activity, and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
A 2-amino-thiazole compounds (by machine translation)
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Paragraph 0608-0610, (2016/10/08)
The present invention relates to the technical field of pharmaceutical chemistry, particularly relates to a 2-amino thiazole compound or its pharmaceutically acceptable salts, its preparation method, and pharmaceutical compositions containing such compounds and its application in the preparation of antineoplastic. (by machine translation)
INHIBITORS OF KINASE ACTIVITY WITH 1,2-DI-CYCLYL SUBSTITUTED ALKYNE STRUCTURES
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Page/Page column 93-94, (2009/10/09)
This invention relates to compounds that inhibit protein kinase activity. More particularly, the invention relates to compounds, compositions, and methods fo inhibiting Ret receptor kinase activity, c-Raf kinase activity and/or VEGF receptor kinase activity. These compounds are alkynes substituted by carbocyclic or heterocyclic rings at both ends with further substitutions thereon. They further show in vivo activity against solid tumor disease models.
COMPOUNDS, COMPOSITIONS AND METHODS
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Page/Page column 56-57, (2010/11/24)
Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.
CYCLIC COMPOUNDS CONTAINING ZINC BINDING GROUPS AS MATRIX METALLOPROTEINASE INHIBITORS
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Page/Page column 256; 262, (2010/02/06)
This invention provides compounds defined by Formula I Z-L-R1-Q-D-(V1)m-R2 I or a pharmaceutically acceptable salt thereof, wherein Z, L, R1, Q, D, V1, m, and R2 are as defined in the specification. The invention also provides pharmaceutical compositions comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, as defined in the specification, together with a pharmaceutically acceptable carrier, diluent, or excipient. The invention also provides methods of inhibiting an MMP-13 enzyme in an animal, comprising administering to the animal a compound of Formula I, or a pharmaceutically acceptable salt thereof. The invention also provides methods of treating a disease mediated by an MMP-13 enzyme in a patient, comprising administering to the patient a compound of Formula I, or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides methods of treating diseases such as heart disease, multiple sclerosis, osteo- and rheumatoid arthritis, arthritis other than osteo- or rheumatoid arthritis, cardiac insufficiency, inflammatory bowel disease, heart failure, age-related macular degeneration, chronic obstructive pulmonary disease, asthma, periodontal diseases, psoriasis, atherosclerosis, and osteoporosis in a patient, comprising administering to the patient a compound of Formula I, or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides combinations, comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, together with another pharmaceutically active component as described in the specification.
Substituted pyrido[3,2-b]oxazin-3(4H)-ones: Synthesis and evaluation of antinociceptive activity
Savelon,Bizot-Espiard,Caignard,Pfeiffer,Renard,Viaud,Guillaumet
, p. 133 - 142 (2007/10/03)
A new series of N-substituted pyrido[3,2-b]oxazinones has been synthesized, pharmacologically evaluated, and compared with acetyl salicylic acid. The compound with the maximal combination of safety and analgesic efficacy was 4-{3-[4-(4-fluorophenyl-1-piperazinyl)propyl]}- 2H-pyrido[3,2-b]-1,4-oxazin-3(4H)-one (6c) with ED50 values of 12.5 mg/kg po (mouse: phenylquinone writhing test) and 27.8 mg/kg po (rat: acetic acid writhing test), respectively. Compound 6c proved to be more active than aspirin with a safety index of 5.1.
Pyridazinone and pyrazolone compounds, cardiotonic compositions including same, and their uses
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, (2008/06/13)
This invention relates to substituted pyridooxazinone and naphtheridone pyridazinone and pyrazolone compounds which are useful as cardiotonic agents for the treatment of congestive heart failure, to methods for increasing cardiac contractility using said
Pyridooxazinone-pyridone compounds, cardiotonic compositions including the same, and their uses
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, (2008/06/13)
This invention relates to substituted pyridooxazinone pyridones which are useful as cardiotonic agents for the treatment of congestive heart failure, to methods for increasing cardiac contractility using said compounds, and pharmaceutical compositions including the same.
Naphtheridinone- and pyridooxazinone-pyridone compounds, cardiotonic compositions including same, and their uses
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, (2008/06/13)
This invention relates to substituted pyridooxazinone and naphtheridone pyridones which are useful as cardiotonic agents for the treatment of congestive heart failure, to methods for increasing cardiac contractility using said compounds, and pharmaceutical compositions including the same.