Properties and Exciting Facts About 1350643-72-9

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HETEROCYCLIC COMPOUNDS AND USES THEREOF

Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.

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HETEROCYCLIC COMPOUNDS AND USES THEREOF

Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.

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HETEROCYCLIC COMPOUNDS AND USES THEREOF

Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.

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PROCESSES FOR PREPARING ISOQUINOLINONES AND SOLID FORMS OF ISOQUINOLINONES

Polymorphs of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphs thereof, and pharmaceutical compositions thereof.

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HETEROCYCLIC COMPOUNDS FOR USE IN THE TREATMENT OF PI3K-GAMMA MEDIATED DISORDERS

Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.

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Isoquinoline – Wikipedia,
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Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-gamma Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate

Optimization of isoquinolinone PI3K inhibitors led to the discovery of a potent inhibitor of PI3K-gamma (26 or IPI-549) with >100-fold selectivity over other lipid and protein kinases. IPI-549 demonstrates favorable pharmacokinetic properties and robust inhibition of PI3K-gamma mediated neutrophil migration in vivo and is currently in Phase 1 clinical evaluation in subjects with advanced solid tumors.

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HETEROARYL DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSTION FOR PREVENTING OR TREATING DISEASES ASSOCIATED WITH PI3 KINASES, CONTAINING SAME AS ACTIVE INGREDIENT

The present invention relates to a heteroaryl derivative or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a pharmaceutical composition for preventing or treating diseases associated with PI3 kinases, containing the same as an active ingredient. The heteroaryl derivative according to the present invention has an excellent effect of selectively inhibiting PI3 kinases, thereby being useful in preventing or treating PI3 kinase diseases such as: cancers, autoimmune diseases, and respiratory diseases.

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QUINAZOLINE DERIVATIVE OR ITS SALT AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

The present invention provides a quinazoline derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, a pharmaceutical composition comprising the same and a use thereof. The quinazoline derivative or its pharmaceutically acceptable salt has a selective inhibitory activity against the phosphatidylinositol 3-kinase delta subunit, and therefore can be usefully applied for preventing or treating cancer, along with avoiding side effects such as lymphopenia-associated inflammatory responses.

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Brief introduction of 1350643-72-9

The synthetic route of 1350643-72-9 has been constantly updated, and we look forward to future research findings.

1350643-72-9, (S)-3-(1-Aminoethyl)-8-chloro-2-phenylisoquinolin-1(2H)-one is a isoquinoline compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 100 mg (0.391 mmol) of tert-butyl 4-chloro-5,6-dihydro-7H-pyrrolo [2,3- d] pyrimidine- 7- carboxylate in a 5 mL microwave vial, 129 mg (0.430 mmol) of (S) -3- (1-aminoethyl) -8-chloro-2-phenylisoquinoline-1 (2H) -one obtained in Preparation Example 3 was dissolved in 3 mL of anhydrous toluene , 2.6 mg (0.012 mmol) of palladium (II) acetate (Pd (OAc) 2) 2,2′-bis (diphenylphosphino) -1,1′-binaphthalene ((+ -) – BINAP) 22 mg (0.035 mmol), 178 mg (0.547 mmol) of cesium carbonate (Cs2CO3) was added, and degassing was performed three times using argon gas. And the mixture was stirred at 85 for 15 hours. The reaction mixture was filtered under reduced pressure, and the organic layer was extracted with ethyl acetate and water. The organic layer was dried (Na2SO4), filtered and concentrated. The crude product was dissolved in dichloromethane and purified by column chromatography (SiO2, eluent: hexane – dichloromethane of 33% ethyl acetate) to give tert-butyl (S) -4 – ((1- (8-chloro-1-oxo-2-phenyl-l, 2-dihydroisoquinolin- Yl) ethyl) amino) -5,6-dihydro- 7H-pyrrolo [2,3-d] pyrimidine-7-carboxylate 120 mg (0.469 mmol, 59% yield) was obtained as a pale yellow solid., 1350643-72-9

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Reference£º
Patent; Korea Research Institute of Chemical Technology; Lee, Gay Hyung; Lim, Hee Jong; Cho, Hee Young; Park, Woo Kyu; Jung, Dae Young; (40 pag.)KR2017/74381; (2017); A;,
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Downstream synthetic route of 1350643-72-9

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1350643-72-9, (S)-3-(1-Aminoethyl)-8-chloro-2-phenylisoquinolin-1(2H)-one is a isoquinoline compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 2-cyanoacetyl chloride (5.1 mmol, 1.0 eq) in DCM (10 mL) at 0 C., Compound 1 (1.0 eq) and triethylamine (1.5 eq) were added. The resulting mixture was warmed to RT and stirred for 2 h. The mixture was partitioned between DCM and a saturated aqueous sodium bicarbonate solution. The organic phase was separated, dried with sodium sulfate, pre-adsorbed on silica gel and purified on silica gel column with acetone and DCM to afford nitrile 136. ESI-MS m/z: 366.3 [M+H]+., 1350643-72-9

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Reference£º
Patent; Intellikine LLC; Infinity Pharmaceuticals, Inc.; CASTRO, Alfredo C.; CHAN, Katrina; EVANS, Catherine A.; JANARDANANNAIR, Somarajannair; LESCARBEAU, Andre; LI, Liansheng; LIU, Tao; LIU, Yi; REN, Pingda; SNYDER, Daniel A.; TREMBLAY, Martin R.; US2013/267521; (2013); A1;,
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