13663-23-5Relevant articles and documents
KV11.1-3.1 INHIBITING METHODS AND COMPOSITIONS
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Page/Page column 45, (2020/12/30)
Compounds of formula (I), formula (II), or formula (III) and their use for treating a neurological or psychiatric disorder, or treating symptoms associated with a neurological or psychiatric disorder, mediated by Kv11.1-3.1 containing potassium channels, including schizophrenia, are disclosed.
PROLINE DERIVATIVES
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Page/Page column 43, (2008/06/13)
The invention relates to novel compounds of formula (I), wherein X, Y, R1, R2, R3, R4 and n have the meaning cited in claim 1, are inhibitors of the coagulation factor Xa and can be used for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumours.
Synthesis and biological activity of novel 1,4-diazepane derivatives as factor Xa inhibitor with potent anticoagulant and antithrombotic activity
Koshio, Hiroyuki,Hirayama, Fukushi,Ishihara, Tsukasa,Taniuchi, Yuta,Sato, Kazuo,Sakai-Moritani, Yumiko,Kaku, Seiji,Kawasaki, Tomihisa,Matsumoto, Yuzo,Sakamoto, Shuichi,Tsukamoto, Shin-Ichi
, p. 2179 - 2191 (2007/10/03)
Factor Xa (fXa) is a serine protease involved in the coagulation cascade, which has received great interest as a potential target for the development of new antithrombotic drugs. Herein we report a novel series of fXa inhibitors in which the 1,4-diazepane moiety was designed to interact with the S4 aryl-binding domain of the fXa active site. Compound 13 (YM-96765) showed potent fXa inhibitory activity (IC50=6.8nM) and effective antithrombotic activity without prolonging bleeding time.
CARBONYL COMPOUNDS
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Page/Page column 114, (2008/06/13)
The invention relates to the novel compounds of formula (I), wherein D, E, G, W, X, Y, T, R and R are defined as in claim 1. The inventive compounds inhibit coagulation factor Xa and can be used in the prophylaxis and/or therapy of thrombo-embolic diseases and for treating tumors.
Aminoalkyl-substituted aromatic bicyclic compounds, methods for their preparation and their use as pharmaceuticals
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, (2008/06/13)
The present invention relates to aminoalkyl-substituted aromatic bicyclic compounds of formula I, which are valuable pharmaceutically active compounds that are suitable, for example, for the treatment of obesity, type II diabetes, arteriosclerosis, high blood pressure, paresthesia, depression, anxiety, anxiety neuroses, schizophrenia, disorders associated with the circadian rhythm, and drug abuse, as well as normalizing lipid metabolism.
Indolinones having kinase inhibitory activity
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, (2008/06/13)
The present invention relates to substituted indolinones of general formula [Figure] wherein R1 to R5, and X are defined as in claim 1, the isomers thereof and the salts thereof, particularly the physiologically acceptable salts thereof which have valuable pharmacological properties, particularly an inhibitory effect on various kinases and cycline/CDK complexes and on the proliferation of various tumour cells, pharmaceutical compositions containing these (compounds, their use and processes for preparing them.