193902-87-3Relevant academic research and scientific papers
NOVEL INHIBITORS OF MAP4K1
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Page/Page column 67; 74, (2018/12/13)
The invention relates to novel inhibitors of MAP4K1 (HPK1) useful for the treatment of diseases or disorders characterised by dysregulation of the signal transduction pathways associated with MAPK activation, including hyperproliferative diseases, diseases of immune system dysfunction, inflammatory disorders, neurological diseases, and cardiovascular diseases. The invention further relates to pharmaceutical compositions comprising the same and methods of treatment of said diseases and disorders. The inhibitors are of formula (I) wherein the definitions for A, D, E, F, R5, R6, R7, Z, ring Q, n, x and y are as given in the application.
Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation
Ma, Xiaodong,Lv, Xiaoqing,Qiu, Ni,Yang, Bo,He, Qiaojun,Hu, Yongzhou
, p. 7585 - 7596 (2015/12/18)
A series of quinoline derivatives featuring the novelty of introducing intra-molecular hydrogen bonding scaffold (iMHBS) were designed, synthesized and biologically evaluated for their mTOR inhibitory activity, as well as anti-proliferative efficacies aga
BICYCLIC CARBOXAMIDE INHIBITORS OF KINASES
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Page/Page column 97, (2012/08/07)
Compounds of formula (I) or pharmaceutical acceptable salts are provided, wherein X1~X5, R1~R3, A, B, Z and n are defined in the description. And compositions containing said compounds, and the uses for inhibitors of kinases such as ALK, and the uses for treating cancer thereof are provided.
The identification and optimisation of novel and selective diamide neuropeptide Y Y2 receptor antagonists
Lunniss, Gillian E.,Barnes, Ashley A.,Barton, Nick,Biagetti, Matteo,Bianchi, Federica,Blowers, Stephen M.,Caberlotto, Laura,Emmons, Amanda,Holmes, Ian P.,Montanari, Dino,Norris, Ros,Walters, Dewi J.,Watson, Steve P.
scheme or table, p. 4022 - 4025 (2010/03/30)
A novel small molecule NPY Y2 antagonist (3) identified from high throughput screening is described. A subsequent SAR study and optimisation programme based around this molecule is also described, leading to the identification of potent and soluble pyridyl analogue 36.
IMIDAZOQUINOLINES AS LIPID KINASE INHIBITORS
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Page/Page column 72; 73, (2008/06/13)
The invention relates to novel organic compounds of formula (I) processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof - alone or in combination with one or more other pharmaceutically active compounds - for the treatment of an inflammatory or obstructive airway disease, such as asthma, disorders commonly occurring in connection with transplantation, or a proliferative disease, such as a tumor disease.
Amide compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use
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, (2008/06/13)
Amide compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction in order to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.
Fibrinogen receptor antagonists
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, (2008/06/13)
This invention relates to compounds of the formula: which are effective for inhibiting platelet aggregation, pharmaceutical compositions for effecting such activity, and a method for inhibiting platelet aggregation.
