- Fit-for-purpose synthesis of dual leucine zipper kinase (DLK) inhibitor GNE-834
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A practical fit-for-purpose synthesis of dual leucine zipper kinase (DLK) inhibitor GNE-834 (1) was developed. The key C[sbnd]C bond was constructed via a Suzuki–Miyaura cross-coupling of iodopyrazole 2 and pyridine boronic ester 3 to afford ketone 12. Su
- Angelaud, Rémy,Beaudry, Danial,Carrera, Diane E.,Gosselin, Francis,Huestis, Malcolm P.,Liu, Wendy,Siu, Michael,Xu, Jie
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- 2-MORPHOLIN-4,6-DISUBSTITUTED PYRIMIDINE DERIVATIVE, AND PREPARATION METHOD AND PHARMACEUTICAL USE THEREOF
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Disclosed is a 2-morpholin-4,6-disubstituted pyrimidine derivative as shown in formula (I) below, and a pharmaceutically acceptable salt, solvate, stereoisomer or prodrug thereof, and a pharmaceutical composition thereof and a use thereof, wherein the definition of each group is as shown in the description. The compound has a PI3K kinase inhibition activity, and has a relatively high inhibitive ability and a low cytotoxicity against PIK3CA mutant breast cancer cell strains T47D and MCF-7.
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Paragraph 0093; 0109
(2017/11/11)
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- PROCESS FOR THE PREPARATION OF SUBSTITUTED IMIDAZO[4,5-C]QUINOLINE COMPOUNDS, INTERMEDIATES AND POLYMORPHS THEREOF
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The present invention relates to a process for preparation of substituted imidazo[4,5- c]quinoline compounds (the compounds of formula I as described) and intermediates thereof. The present invention also relates to polymorphs of a compound encompassed in the compound of formula I and their use in the treatment of proliferative disorders, particularly cancers.
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- COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES
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The present invention provides compounds of formula I: [INSERT FORMULA HERE] or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a Plasmodium parasite, such as malaria.
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Page/Page column 70; 71; 95
(2014/06/11)
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- Structure guided optimization of a fragment hit to imidazopyridine inhibitors of PI3K
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PI3 kinases are a family of lipid kinases mediating numerous cell processes such as proliferation, migration and differentiation. The PI3 Kinase pathway is often de-regulated in cancer through PI3Kα overexpression, gene amplification, mutations and PTEN p
- Pecchi, Sabina,Ni, Zhi-Jie,Han, Wooseok,Smith, Aaron,Lan, Jiong,Burger, Matthew,Merritt, Hanne,Wiesmann, Marion,Chan, John,Kaufman, Susan,Knapp, Mark S.,Janssen, Johanna,Huh, Kay,Voliva, Charles F.
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p. 4652 - 4656
(2013/08/23)
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- FUSED HETEROARYLS AND THEIR USES
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Provided are certain fused heteroaryls, compositions thereof and methods of use therefor.
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Paragraph 0172; 0173
(2013/07/31)
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- FUSED HETEROARYLS AND THEIR USES
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Provided are certain fused heteroaryls, compositions thereof and methods of use therefor.
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Page/Page column 36-37
(2012/04/04)
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- 1H-IMIDAZO[4, 5-c]QUINOLINONE COMPOUNDS, USEFUL FOR THE TREATMENT OF PROLIFERATIVE DISEASES
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The invention relates to the use of 1 H-imidazo[4,5-c]quinolinone compounds and salts thereof in the treatment of protein and/or lipid kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases; 1 H-imidazo[4,5-c]quinolinone compounds for use in the treatment of protein and/or lipid kinase dependent diseases; a method of treatment against said diseases, comprising administering the 1 H-imidazo[4,5-c]quinolinone compounds to a warm-blooded animal, especially a human; pharmaceutical preparations comprising an 1 H-imidazo[4,5-c]quinolinone compounds, especially for the treatment of a protein and/or lipid kinase dependent disease; novel 1 H-imidazo[4,5-c]quinolinone compounds; and a process for the preparation of the novel 1 H-imidazo[4,5-c]quinolinone compounds.
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- PI3K/M TOR INHIBITORS
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The invention relates to PI3K/mTOR inhibiting compounds consisting of the formula (I): wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; meth
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Page/Page column 147-148
(2010/04/03)
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- 1H-IMIDAZO[4,5-c]QUINOLINONE DERIVATIVES
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The invention relates to the use of 1H-imidazo[4,5-c]quinolinone derivatives and salts thereof in the treatment of protein and/or lipid kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases; 1H-imidazo[4,5-c] quinolinone derivatives for use in the treatment of protein and/or lipid kinase dependent diseases; a method of treatment against said diseases, comprising administering the 1H- imidazo[4,5-c] quinofinone derivatives to a warm-blooded animal, especially a human; pharmaceutical preparations comprising an 1H-imidazo[4,5-c] quinolinone derivative, especially for the treatment of a protein and/or lipid kinase dependent disease; novel 1 H- imidazo[4,5-c] quinolinone derivatives; and a process for the preparation of the novel 1H- imidazo[4,5-c] quinolinone derivatives.
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Page/Page column 135
(2010/12/29)
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- SUBSTITUTED IMIDAZOPYRIDAZINES AS PI3K LIPID KINASE INHIBITORS
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The invention relates to novel compounds of formula (I), as well as other invention embodiments related to these compounds. The compounds are e.g. useful in the treatment of the animal or human body in view of their ability to inhibit protein kinases such as especially PI3 kinase.
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- SUBSTITUTED IMIDAZOPYRIDAZINES AND PYRROLOPYRIMIDINES AS LIPID KINASE INHIBITORS
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The present invention relates to compounds are of the formula I, processes for the preparation thereof, more generally these compounds for use in the treatment of the human or animal body, in the treatment of an inflammatory or obstructive airway disease, disorders commonly occurring in connection with transplantation, or a proliferative disease, which disease responds to an inhibition of kinases of the PI3-kinase-related protein kinase family.
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- 2,4-SUBSTITUTED QUINAZOLINES AS LIPID KINASE INHIBITORS
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The invention relates to compounds of the formula (I), which are appropriate for the treatment of kinase, e.g. PI3K-related, diseases, such as proliferative diseases, inflammatory diseases, obstructive airways disorders and transplantation related disease
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Page/Page column 69
(2008/06/13)
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- PYRAZOLO [3, 4-D] PYRIMIDINE DERIVATIVES USEFUL TO TREAT RESPIRATORY DISORDERS
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The present invention concerns a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, where R1-R3 and Y are defined in the description, and its use in the treatment of disorders in which pi3 kinase is imp
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