169750-01-0Relevant articles and documents
Discovery of DS34942424: An orally potent analgesic without mu opioid receptor agonist activity
Arita, Tsuyoshi,Asano, Masayoshi,Domon, Yuki,Kubota, Kazufumi,Machinaga, Nobuo,Shimada, Kousei
, (2020/09/04)
We identified (5′S)-10′-fluoro-6′-methyl-5′,6′-dihydro-3′H-spiro[cyclopropane-1,4′-[2,6]diaza[2,5]methano[2,6]benzodiazonin]-7′(1′H)-one, 22b (DS34942424) with a unique and original bicyclic skeleton. 22b showed an orally potent analgesic in the acetic ac
TRIAZOLOPYRIDINE COMPOUNDS AS PIM KINASE INHIBITORS
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Page/Page column 83, (2012/12/13)
Compounds of Formula I: in which R1, R2, R3, R4 and R10 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by PIM-1 and/or PIM-2 and/or PIM-3 kinases.
2 -AMINO-PYRIMIDINE DERIVATIVES AS HISTAMINE H4 ANTAGONISTS
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Page/Page column 54, (2009/07/03)
2-Aminopyrimidine derivatives of formula (I), wherein the meaning of the different substituents are those indicated in the description. These compounds are useful as histamine H4 receptor antagonists.
DIACYLGLYCEROL ACYLTRANSFERASE INHIBITORS
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Page/Page column 43; 44, (2009/01/20)
Provided herein are compounds of the formula (I) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.
Synthesis and structure-activity relationships of retro bis-aminopyrrolidine urea (rAPU) derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Part 2
Hudson, Sarah,Kiankarimi, Mehrak,Rowbottom, Martin W.,Vickers, Troy D.,Wu, Dongpei,Pontillo, Joseph,Ching, Brett,Dwight, Wesley,Goodfellow, Val S.,Schwarz, David,Heise, Christopher E.,Madan, Ajay,Wen, Jenny,Ban, William,Wang, Hua,Wade, Warren S.
, p. 4922 - 4930 (2007/10/03)
The design, synthesis, and SAR of a series of retro bis-aminopyrrolidine ureas are described. Compounds from this series exhibited considerable binding affinity (Ki = 1 nM) and functional activity at MCH-R1, acceptable CYP2D6 inhibition, and good rat brain exposure.
AMIDE DERIVATIVE AND MEDICINE
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Page/Page column 40, (2010/11/23)
The present invention is directed to an amide derivative having excellent BCR-ABL tyrosine kinase inhibitory activity, or a salt thereof. The present invention provides an amide derivative represented by the following general formula [1]: (wherein R1 represents -CH2-R11, etc.; R2 represents alkyl, halogen, haloalkyl, etc.; R3 represents hydrogen, etc.; Het1 represents a group of the formula [6] as above, etc.; and Het2 represents pyrimidinyl, etc.), or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same as an active ingredient. The compound of the present invention is useful as a BCR-ABL tyrosine kinase inhibitor.
Quinolinone-carboxamide compounds
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Page/Page column 17, (2008/06/13)
The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
Indazole-carboxamide compounds
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Page/Page column 22, (2008/06/13)
The invention provides novel indazole-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
5-HT4 receptor agonist compounds
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Page/Page column 19, (2008/06/13)
The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
Quinolinone compounds as 5-HT4 receptor agonists
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Page/Page column 22, (2008/06/13)
The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.