1089280-53-4

Usage

Uses

Used in Pharmaceutical Research:
Tert-butyl 4-(4-amino-3-methoxyphenyl)piperidine-1-carboxylate is used as a building block for the development of potential drug candidates due to its unique molecular structure and properties that can be further modified and derivatized to explore its biological activities and interactions.
Used in Medicinal Chemistry:
In the field of medicinal chemistry, tert-butyl 4-(4-amino-3-methoxyphenyl)piperidine-1-carboxylate is employed as an intermediate in the synthesis of compounds with potential therapeutic applications, leveraging its versatile structure to create new molecules with desired biological effects.
Used in Organic Synthesis:
Tert-butyl 4-(4-amino-3-methoxyphenyl)piperidine-1-carboxylate is utilized as a key intermediate in organic synthesis, allowing for the creation of a variety of organic compounds through its adaptable framework, which can be modified to achieve specific chemical properties and reactivity.
Used in Structure-Activity Relationship Studies:
In the study of structure-activity relationships, tert-butyl 4-(4-amino-3-methoxyphenyl)piperidine-1-carboxylate is used to understand how the molecular structure of a compound influences its biological activity, providing insights into the design of more effective and selective drugs.
Used in Chemical Research:
Tert-butyl 4-(4-amino-3-methoxyphenyl)piperidine-1-carboxylate is applied in chemical research to explore its reactivity, stability, and potential applications in the synthesis of novel compounds, contributing to the advancement of chemical knowledge and technology.

Upstream product

• 321-23-3 4-bromo-2-fluoronitrobenzene 
• 103966-66-1 4-bromo-2-methoxy-1-nitro-benzene 
• 59557-91-4 4-bromo-2-methoxyaniline 
• 375853-82-0 tert-Butyl 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-3,6-dihydro-1(2H)-pyridinecarboxylate 
• 1246533-06-1 tert-butyl 4-(4-amino-3-methoxy-phenyl)-3,6-dihydro-2H-pyridine-1-carboxylate 
• 6627-53-8 1-chloro-3-methoxy-4-nitrobenzene 
• 1233145-65-7 4-(3-methoxy-4-nitro-phenyl)-3,6-dihydro-2H-pyridine-1-carboxylic acid tert-butyl ester 

Downstream Products

• 1124330-14-8 2-methoxy-4-(1-methylpiperidin-4-yl)aniline 
• 1233144-32-5 [2-methoxy-4-(1-methylpiperidin-4-yl)-phenyl][7-(2-methoxyphenyl)pyrrolo[2,1-f][1,2,4]triazin-2-yl]amine 
• 1390657-98-3 tert-butyl 4-(4-((2-(2,6-dichlorobenzyl)-5-oxo-5,6-dihydropyrido[2,3-d]pyridazin-4-yl)amino)-3-methoxyphenyl)piperidine-1-carboxylate 
• 1390657-99-4 tert-butyl 4-(3-methoxy-4-(5-oxo-2-vinyl-5,6-dihydropyrido[3,2-d]pyridazin-4-ylamino)phenyl)piperidine-1-carboxylate 
• 1390658-00-0 tert-butyl 4-(3-methoxy-4-(2-(2-morpholinoethyl)-5-oxo-5,6-dihydropyrido[3,2-d]pyridazin-4-ylamino)phenyl)piperidine-1-carboxylate 
• 1390658-02-2 (E)-tert-butyl 4-(4-(2-(2-cyclopropylvinyl)-5-oxo-5,6-dihydropyrido[3,2-d]pyridazin-4-ylamino)-3-methoxyphenyl)piperidine-1-carboxylate 
• 1390658-03-3 tert-butyl 4-(4-(2-(2-cyclopropylethyl)-5-oxo-5,6-dihydropyrido[3,2-d]pyridazin-4-ylamino)-3-methoxyphenyl)piperidine-1-carboxylate 
• 1390658-08-8 tert-butyl 4-(4-((2-(2-fluorobenzyl)-5-oxo-5,6-dihydropyrido[2,3-d]pyridazin-4-yl)amino)-3-methoxyphenyl)piperidine-1-carboxylate 
• 1390656-28-6 2-(2-fluorobenzyl)-4-{[2-methoxy-4-(piperidin-4-yl)phenyl]amino}pyrido[2,3-d]pyridazin-5(6H)-one 
• 1390658-91-9 tert-butyl 4-(4-((2-(2,5-difluorobenzyl)-5-oxo-5,6-dihydropyrido[2,3-d]pyridazin-4-yl)amino)-3-methoxyphenyl)piperidine-1-carboxylate 
• 1390657-97-2 tert-butyl 4-(4-((2-chloro-5-oxo-5,6-dihydropyrido[2,3-d]pyridazin-4-yl)amino)-3-methoxyphenyl)piperidine-1-carboxylate 
• 1314996-83-2 7-Amino-2-[4-(1-cyclopropylpiperid-4-yl)-2-methoxyphenylamino]-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxamide 
• 1315513-76-8 7-Amino-2-[4-(1-cyclopropylpiperid-4-yl)-2-methoxyphenylamino]-8-(2-hydroxy-2-methylpropyl)-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxamide 
• 1315513-52-0 7-amino-2-{4-[1-(2-chloroethyl)piperid-4-yl]-2-methoxyphenylamino}-8-(2-hydroxy-2-methylpropyl)-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxamide 

Relevant academic research and scientific papers

HETEROCYCLIC COMPOUND

The present invention provides a compound having a CaMKII inhibitory action, which is expected to be useful as an agent for the prophylaxis or treatment of cardiac diseases (particularly catecholaminergic polymorphic ventricular tachycardia, postoperative atrial fibrillation, heart failure, fatal arrhythmia) and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

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.

Tyrosine Kinase Inhibitor And Uses Thereof

Disclosed is a compound of Formula (I) or a pharmaceutically acceptable salt, ester, or solvate thereof, or their stereoisomers, which can be used as tyrosine kinase inhibitor. Also disclosed is a method for preparing the compound, a pharmaceutical composition and a kit comprising the compound, and uses of the compound. The compound can be used as tyrosine kinase inhibitor, or can be used to reduce or inhibit activity of EGFR or mutant thereof, such as EGFR mutant comprising T790M mutation, in a cell, or to treat and/or prevent a disease associated with overactivity of EGFR, such as cancer.

Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase

In the treatment of echinoderm microtubule-associated protein-like 4 (EML4)-anaplastic lymphoma kinase positive (ALK+) non-small-cell lung cancer (NSCLC), secondary mutations within the ALK kinase domain have emerged as a major resistance mechanism to both first- and second-generation ALK inhibitors. This report describes the design and synthesis of a series of 2,4-diarylaminopyrimidine-based potent and selective ALK inhibitors culminating in identification of the investigational clinical candidate brigatinib. A unique structural feature of brigatinib is a phosphine oxide, an overlooked but novel hydrogen-bond acceptor that drives potency and selectivity in addition to favorable ADME properties. Brigatinib displayed low nanomolar IC50s against native ALK and all tested clinically relevant ALK mutants in both enzyme-based biochemical and cell-based viability assays and demonstrated efficacy in multiple ALK+ xenografts in mice, including Karpas-299 (anaplastic large-cell lymphomas [ALCL]) and H3122 (NSCLC). Brigatinib represents the most clinically advanced phosphine oxide-containing drug candidate to date and is currently being evaluated in a global phase 2 registration trial.

5 OXO-5,8-DIHYDROPYRIDO[2,3-d]PYRIMIDINE DERIVATIVES AS CAMKII KINASE INHIBITORS FOR TREATING CARDIOVASCULAR DISEASES

The present invention relates to 5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine derivatives, to their preparation and to their therapeutic use.

BICYCLIC INHIBITORS OF ALK

The present invention relates to compounds of formula (1) or pharmaceutical acceptable salts, wherein R1, X, Y, Z, A, B, G1, and n are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as ALK and methods of treating diseases such as cancer.

BICYCLIC CARBOXAMIDE INHIBITORS OF KINASES

Compounds of formula (I) or pharmaceutical acceptable salts are provided, wherein X1~X5, R1~R3, A, B, Z and n are defined in the description. And compositions containing said compounds, and the uses for inhibitors of kinases such as ALK, and the uses for treating cancer thereof are provided.

Strategies to mitigate the bioactivation of 2-anilino-7-aryl-pyrrolo[2,1-f ][1,2,4]triazines: Identification of orally bioavailable, efficacious ALK inhibitors

Chemical strategies to mitigate cytochrome P450-mediated bioactivation of novel 2,7-disubstituted pyrrolo[2,1-f][1,2,4]triazine ALK inhibitors are described along with synthesis and biological activity. Piperidine-derived analogues showing minimal microsomal reactive metabolite formation were discovered. Potent, selective, and metabolically stable ALK inhibitors from this class were identified, and an orally bioavailable compound (32) with antitumor efficacy in ALK-driven xenografts in mouse models was extensively characterized.

PYRIMIDINE INHIBITORS OF KINASE ACTIVITY

The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts or solvates thereof, wherein G1, R2, R3, R4, R5, n, p, q, Ar1, and Ar2 are defined in the description. The present invention relates also to methods of making said compounds, and compositions comprising said compounds which are useful for inhibiting kinases such as IGF-IR.

Imidazopyridine Kinase Inhibitors

The present invention provides imidazopyridine compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.