877399-47-8

Usage

Uses

Used in Pharmaceutical Industry:
(R)-5-BroMo-N,N-bis-(tert-butoxycarbonyl)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-2-aMine is used as a key intermediate for the synthesis of vardenafil, a medication for erectile dysfunction. It is crucial in the production process due to its role in creating the final drug product.
Used in Medicinal Chemistry:
In the field of medicinal chemistry, (R)-5-BroMo-N,N-bis-(tert-but-butoxycarbonyl)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-2-aMine is utilized for research and development of new drugs, particularly those targeting phosphodiesterase type 5 inhibitors.
Used in Drug Development:
(R)-5-BroMo-N,N-bis-(tert-butoxycarbonyl)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-2-aMine plays a significant role in drug development, where it is employed to create novel compounds with potential therapeutic applications, especially in the area of erectile dysfunction treatment.
Used in Research on Phosphodiesterase Type 5 Inhibitors:
(R)-5-BroMo-N,N-bis-(tert-butoxycarbonyl)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-2-aMine is also used in research focused on phosphodiesterase type 5 inhibitors, contributing to a better understanding of their mechanism of action and the development of improved treatments for related conditions.

Upstream product

• 15128-82-2 3-hydroxy-2-nitropyridine 
• 877397-65-4 (S)‐1‐(2,6-dichloro-3-fluorophenyl)ethanol 
• 16867-03-1 2-amino-3-hydroxypyridine 
• 24424-99-5 di-tert-butyl dicarbonate 
• 877397-70-1 (R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethyoxyl)-2-nitropyridine 
• 54231-35-5 3-fuoro-2-nitropyridine 
• 330156-50-8 (R)-1-(2,6-dichloro-3-fluorophenyl)ethan-1-ol 
• 1448326-33-7 5-bromo-3-[1 (R)-(2,6-dichloro-3-fluoro-phenyl)-ethoxy]-pyridin-2-ylamine 

Downstream Products

• 877399-48-9 (R)-N,N-bis(tert-butoxycarbonyl)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-2-amine 
• 1613148-03-0 (R)-N,N-bis(tert-butoxycarbonyl)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)pyridin-2-amine 
• 1613148-02-9 3-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-(5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)pyridin-2-amine 
• 1613148-05-2 (R)-N,N-bis(tert-butoxycarbonyl)-5-(6-(tert-butoxycarbonyl)-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-3-yl)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-2-amine 

Relevant academic research and scientific papers

Novel pyridine derivatives having inhibition activity against SHIP2 and pharmaceutical compositions with the components

The present invention relates to a use as a pyridine derivative and/or a SHIP2 inhibitor. More specifically, the present invention relates to: a pyridine derivative of chemical formula I or pharmaceutically acceptable salt thereof; a method for manufacturing compounds thereof; and a pharmaceutical composition containing the compounds as active components. The pyridine derivative and the pharmaceutically acceptable salt thereof are useful as therapeutic agents for diseases related to SHIP2, such as Alzheimerandprime;s dementia, hypertension, cancer, diabetes, etc.COPYRIGHT KIPO 2020

Novel pyridine derivatives having inhibition activity against SHIP2 and pharmaceutical compositions with the components

The present invention relates to a pyridine derivative and/or a use as a SHIP2 inhibitor. The present invention relates to a pyridine derivative of chemical formula I or a pharmaceutically acceptable salt thereof, a method for preparing the compounds, and a pharmaceutical composition containing the compounds as an active ingredient. The pyridine derivative and pharmaceutically acceptable salt thereof is useful as drugs for the treatment of diseases related to SHIP2, such as Alzheimerandprime;s dementia, hypertension, cancer, and diabetes.COPYRIGHT KIPO 2021

Synthesis method of anti-tumor drug crizotinib

The invention relates to a synthesis method of an anti-tumor drug crizotinib. 3-hydroxy-2-aminopyridine is used as a raw material; amino is firstly protected; afterwards, a Mitsunobu reaction, the bromination deprotection and the Suzuki coupling are carried out; finally, the deprotection is carried out to prepare and obtain the crizotinib. According to the method, in the condition that a step is not added, the protection on two nitrogen atoms are simultaneously removed to obtain the crizotinib; the route is used for avoiding the previous scheme that the nitrification is firstly carried out andthen the reduction is carried out; much waste acid and wastewater which are generated by the nitrification of concentrated acid are avoided; meanwhile, the environmental pollution brought by the reduction of iron powder or the high cost of catalytic hydrogenation reduction and the high requirement of a device, are also avoided; when the Suzuki coupling is carried out in the condition that the amino is protected, the strong electron donating effect of the para-position amino of pyridine bromide is avoided; the reaction activity of the bromide is increased; the yield of a Suzuki reaction is also improved, and the method has a series of advantages of being few in step, short in cycle, cheap and easily obtained in raw material, low in cost, lower in requirement on the device, high in processstability, green and environmentally friendly, and the like.

Substituted ring compound and its method and use thereof

The invention provides a substituted cyclic compound as well as a use method and application thereof. The compound is a compound as shown in a formula (I) or stereoisomers, stereomers, tautomers, nitric oxides, solvates, metabolites and pharmaceutically acceptable salts or prodrugs of the compound as shown in the formula (I). The invention further provides a medicament composition containing the compound. The compound and the medicament composition are capable of regulating the activity of protein kinase in a biological sample body and are used for protecting, treating or relieving proliferative diseases of patients. The formula (I) is as shown in the specification.

Substituted alkynyl pyridine compounds and methods of use thereof, and use thereof

The invention provides a substituted alkynylpyridine compound with a structure represented by a formula (I) as described in the specification and a pharmaceutically acceptable salt and a medicinal preparation thereof. The compound is used for adjusting activity of protein kinase and adjusting intercellular or intracellular signal response. The invention also relates to a pharmaceutical composition including the compound provided by the invention and a method of applying the pharmaceutical composition in treating mammals, especially in treating highly proliferative diseases of the mankind.

Combination of a C-Met antagonist and an aminoheteroaryl compound for the treatment of cancer

The invention also relates to a composition comprising an antibody antagonist to c-Met and an aminoheteroaryl compound, particularly as a medicament. The present invention also comprises a pharmaceutical composition comprising said anti c-Met antibody and said aminoheteroaryl compound as combination products for simultaneous, separate or sequential use. The invention relates to the use of the composition of the invention for the treatment of cancer in a mammal.

SUBSTITUTED CYCLIC COMPOUNDS AND METHODS OF USE

The present invention provides novel substituted alkynyl compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.

SUBSTITUTED CYCLIC COMPOUNDS AND METHODS OF USE

The present invention provides novel substituted cyclic compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.

SUBSTITUTED ALKYNYL PYRIDINE COMPOUNDS AND METHODS OF USE

The present invention provides novel substituted alkynyl pyridine compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.