- A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia
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Mutants of the FLT3 receptor tyrosine kinase (RTK) with duplications in the juxtamembrane domain (FLT3-ITD) act as drivers of acute myeloid leukemia (AML). Potent tyrosine kinase inhibitors (TKi) of FLT3-ITD entered clinical trials and showed a promising,
- Sellmer, Andreas,Pilsl, Bernadette,Beyer, Mandy,Pongratz, Herwig,Wirth, Lukas,Elz, Sigurd,Dove, Stefan,Henninger, Sven Julian,Spiekermann, Karsten,Polzer, Harald,Klaeger, Susan,Kuster, Bernhard,B?hmer, Frank D.,Fiebig, Heinz-Herbert,Kr?mer, Oliver H.,Mahboobi, Siavosh
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- SYNTHESIS, PHARMACOLOGY AND USE OF NEW AND SELECTIVE FMS-LIKE TYROSINE KINASE 3 (FLT3) FLT3 INHIBITORS
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The present invention relates to small molecule compounds of formula (I) and their use as FLT3 inhibitors for the treatment of various diseases, such as acute myeloid leukemia (AML). The present invention further relates to methods of synthesizing the com
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- TETRAHYDROISOQUINOLINE DERIVATIVES
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The present invention relates to tetrahydroisoquinoline derivatives according to formula (I), which are Positive Allosteric Modulators of D1 and accordingly of benefit as pharmaceutical agents for the treatment of diseases in which D1 receptors play a role.
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- ISOINDOLINE DERIVATIVES
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The present invention relates to isoindoline derivatives according to formula (I), which are Positive Allosteric Modulators of D1 and accordingly of benefit as pharmaceutical agents for the treatment of diseases in which D1 receptors play a role.
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- PROCESS FOR THE PREPARATION OF 2,4-DICHLORO-7H-PYRROLO[2,3H]QUINAZOLINE
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The invention relates to a method of preparing 2,4-dichloro-7H-pyrrolo[2,3-h]quinazoline (II): from 1H-pyrrolo[2,3-h]quinazoline-2,4-dione.
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Page/Page column 6; 10
(2010/03/02)
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- HETEROARYL COMPOUNDS, COMPOSITIONS THEREOF, AND USE THEREOF AS PROTEIN KINASE INHIBITORS
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Provided herein are Heteroaryl Compounds having the following structure: (I) wherein R1, R2, L, X, Y, Z, Q, A and B are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, metabolic conditions and conditions treatable or preventable by inhibition of a kinase pathway comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.
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Page/Page column 179
(2008/12/05)
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- NOVEL TETRAYDROSPIRO{PIPERIDINE-2,7’ -PYRROLO[3,2-b]PYRIDINE DERIVATIVES AND NOVEL INDOLE DERIVATIVES USEFUL IN THE TREATMENT OF 5-HT6 RECEPTOR -RELATED DISORDERS
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The present invention relates to compounds of formula (I): Formula (I) wherein U, P, W1, W2, W3, v, Y, Z, Rm, and Rm’ are as described herein, to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds for the preparation of a medicament against 5-HT6 receptor-related disorders.
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Page/Page column 31
(2008/06/13)
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- A FACILE ONE STEP SYNTHESIS OF 4-AMINOINDOLES FROM 5-HALO-4-OXO-4,5,6,7-TETRAHYDROINDOLES
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Reaction of 5-halo-4-oxo-4,5,6,7-tetrahydroindoles with amines initiates the amination of the carbonyl function and ensuing dehydrohalogenation leads to a successful formation of 4-aminoindoles.
- Matsumoto, Masakatsu,Ishida, Yasuko,Hatanaka, Naoto
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p. 1667 - 1674
(2007/10/02)
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