1032903-52-8

Upstream product

• 1202858-68-1 1-bromo-5-isopropoxy-2-methyl-4-nitrobenzene 
• 375853-82-0 tert-Butyl 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-3,6-dihydro-1(2H)-pyridinecarboxylate 
• 64695-96-1 1-bromo-5-fluoro-2-methyl-4-nitrobenzene 
• 67-63-0 isopropyl alcohol 
• 112108-73-3 1-chloro-5-fluoro-2-methyl-4-nitrobenzene 
• 452-73-3 2-chloro-4-fluorotoluene 
• 1032903-50-6 1-chloro-2-methyl-4-nitro-5-(propan-2-yloxy)benzene 
• 1032903-51-7 2-(5-isopropoxy-2-methyl-4-nitrophenyl)-4,4,5,5-tetramethyl-1,3,2-dioxide cyclopentaborane 
• 138647-49-1 4-Trifluoromethanesulfonyloxy-3,6-dihydro-2H-pyridine-1-carboxylic acid tert-butyl ester 

Downstream Products

• 1190399-91-7 5-chloro-N²-[2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl]-N⁴-[2-(isopropylsulfonyl)phenyl]pyrimidine-2,4-diamine dihydrochloride 
• 1035230-24-0 5-chloro-N²-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N⁴-((2-isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine 
• 1380575-43-8 5-chloro-N²-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N⁴-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine hydrochloride 
• 1032900-25-6 5-chloro-N²-{5-methyl-4-(piperidin-4-yl)-2-[(propan-2-yl)oxy]phenyl}-N⁴-[2-(propane-2-sulfonyl)phenyl]pyrimidine-2,4-diamine 
• 1032903-64-2 4-(4-{5-chloro-4-[2-(propane-2-sulfonyl)phenylamino]pyrimidin-2-ylamino}-5-isopropoxy-2-methylphenyl)piperidine-1-carboxylic acid tert-butyl ester 

Relevant academic research and scientific papers

METHOD FOR TREATING CANCER BY COMBINATION OF FAK/ALK/ROS1 INHIBITOR AND EGFR INHIBITOR

Provided herein is a method for treating or suppressing a cancer, reducing its severity, lowering its risk or inhibiting its metastasis in an individual. The method comprises administering to the individual a therapeutically effective amount of one or more of a FAK inhibitor, an ALK inhibitor and a ROS1 inhibitor, and a therapeutically effective amount of an EGFR inhibitor. Provided herein is also a pharmaceutical composition or kit comprising one or more of a FAK inhibitor, an ALK inhibitor and a ROS 1 inhibitor, and an EGFR inhibitor.

COMBINATION OF FAK INHIBITOR AND BTK INHIBITOR FOR TREATING A DISEASE

A combination comprising a FAK inhibitor and a BTK inhibitor, a pharmaceutical composition and a kit, and a method for treating a disease such as esophageal cancer using the combination.

CONDENSED-RING PYRIMIDYLAMINO DERIVATIVE, PREPARATION METHOD THEREFOR, AND INTERMEDIATE, PHARMACEUTICAL COMPOSITION AND APPLICATIONS THEREOF

Disclosed are a condensed-ring pyrimidylamino derivative, a preparation method therefor, and an intermediate, a pharmaceutical composition and applications thereof. The method for preparing the condensed-ring pyrimidylamino derivative comprises: in a solvent, in the presence of a palladium-containing catalyst, allowing a compound represented by formula I-a and a compound represented by formula I-b' to have a coupling reaction, and then preparing a compound represented by formula I by means of a deprotection reaction. Also disclosed applications of the condensed-ring pyrimidylamino derivative in the preparation of drugs for preventing, relieving and/or treating tumors or diseases caused by an anaplastic lymphoma kinase. The condensed-ring pyrimidylamino derivative of the present invention has an obvious restraint effect on the anaplastic lymphoma kinase.

Anaplastic lymphoma kinase (ALK) inhibitor, and preparation method and application thereof

The invention relates to a compound as shown in a formula (I) which is described in the specification, and a pharmaceutical composition and a preparation method thereof. The compound can be used as anALK inhibitor for treatment of diseases mediated by ALK. The invention further relates to application of the compound as shown in the formula (I) and the pharmaceutical composition thereof to preparation of drugs used for treating diseases mediated by ALK.

AMINOPYRIMIDINES AS ALK INHIBITORS

The present disclosure provides compounds represented by Formula (I): and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, R1b, R2a, R2b, R3, R4, R5, R6, and R7 are as defined as set forth in the specification. The present disclosure also provides compounds of Formula (I) for use to treat a condition or disorder responsive to inhibition of ALK such as cancer.

PYRIMIDINE DERIVATIVE AND USE THEREOF

The present invention provides a pyrimidine derivative and a use thereof. The pyrimidine derivative is the compound shown in formula I or a pharmaceutically acceptable salt, hydrate, solvate, metabolite or prodrug thereof, wherein, R1, R2, R3, R4 and R5 are, for example, as defined in the specification. The compound can act as an ALK inhibitor, and is for preparing an anti-tumor medicament for suppressing an anaplastic lymphoma kinase.

Novel kinase inhibitors

The present invention relates to a novel kinase inhibitor useful as a medicine for tumor, nerve disorder and mental illness. The purpose of the present invention is to provide a compound having improved blood-aqueous barrier penetrability to neurodegenerative diseases that cancer spreads to brain or progresses in brain. To this end, provided is a compound represented by chemical formula 1 or a pharmaceutically allowable salt thereof.COPYRIGHT KIPO 2017

New synthesis technology of ceritinib intermediate

The purpose of the invention is to provide a new synthesis technology of a ceritinib intermediate. The technology is characterized in that the ceritinib intermediate tert-butyl 4-(4-amino-5-isopropyl-2-methylphenyl)-piperidyl-1-carboxylate is prepared thr

DEUTERATED DIAMINOPYRIMIDINE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SUCH COMPOUNDS

The present invention related to deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds. In particular, disclosed are the deuterated diaminopyrimidine compounds shown as formula (I), and the pharmaceutical compositions comprising such compounds or crystal form, pharmaceutically acceptable salts, hydrates or solvates thereof. The compounds of the present invention can be used for treating and/or preventing protein kinase-associated diseases, such as cell proliferative disease, cancer, immune disease and the like.

Preparation method for ALK inhibitor

The invention provides a preparation method for an ALK inhibitor. The preparation method comprises a step of contacting a compound as shown in a formula 4 with a compound as shown in a formula 12. The method can rapidly and efficiently prepare the target ALK inhibitor and is simple in steps, mild in reaction conditions and low in cost.