220220-23-5

Upstream product

• 505-66-8 1,4-Diazacycloheptane 
• 24424-99-5 di-tert-butyl dicarbonate 
• 350-46-9 4-Fluoronitrobenzene 
• 112275-50-0 tert-butyl 1,4-diazepine-1-carboxylate 

Downstream Products

• 441313-14-0 4-(4-aminophenyl)-[1,4]-diazepane-1-carboxylic acid tert-butyl ester 
• 850628-93-2 4-[4-(8-cyclopentyl-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-ylamino)phenyl]-[1,4]-diazepane-1-carboxylic acid tert-butyl ester 
• 714249-31-7 ethyl ({[(7-cyano-2-naphthyl)methyl][4-(4-methyl-1,4-diazepan-1-yl)phenyl]amino}sulfonyl)acetate 
• 714249-34-0 ethyl ({({7-[amino(imino)methyl]-2-naphthyl}methyl)[4-(4-methyl-1,4-diazepan-1-yl)phenyl]amino}sulfonyl)acetate 
• 220220-12-2 7-{[[4-(1,4-diazepan-1-yl)phenyl](methylsulfonyl)amino]methyl}naphthalene-2-carboximidamide 
• 220220-32-6 tert-butyl 4-(4-{[(7-cyano-2-naphthyl)methyl]amino}phenyl)-1,4-diazepane-1-carboxylate 
• 220220-08-6 tert-butyl 4-{4-[[(7-cyano-2-napthyl)methyl](methylsulfonyl)amino]phenyl}-1,4-diazepane-1-carboxylate 
• 286430-94-2 ethyl ({({7-[amino(imino)methyl]-2-naphthyl}methyl)[4-(1,4-diazepan-1-yl)phenyl]amino}sulfonyl)acetate 
• 714249-32-8 ethyl ({[4-(4-butyl-1,4-diazepan-1-yl)phenyl][(7-cyano-2-naphthyl)methyl]amino}sulfonyl)acetate 
• 714249-33-9 ethyl ({[4-(4-benzyl-1,4-diazepan-1-yl)phenyl][(7-cyano-2-naphthyl)methyl]amino}sulfonyl)acetate 
• 286430-88-4 tert-butyl 4-(4-{[(7-cyano-2-napthyl)methyl][(2-ethoxy-2-oxoethyl)sulfonyl]amino}phenyl)-1,4-diazepane-1-carboxylate 
• 220220-41-7 ethyl ({({7-[amino(imino)methyl]-2-naphthyl}methyl)[4-(4-ethanimidoyl-1,4-diazepan-1-yl)phenyl]amino}sulfonyl)acetate 
• 714249-35-1 ethyl ({({7-[amino(imino)methyl]-2-naphthyl}methyl)[4-(4-butyl-1,4-diazepan-1-yl)phenyl]amino}sulfonyl)acetate 

Relevant academic research and scientific papers

LOX INHIBITORS

The disclosure relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, Formula (I) as defined herein. Compounds according to Formula I are pharmacologically effective as lysyl oxidase (LOX) inhibitors and are believed to be useful in the treatment of, for instance, cancer.

MACROCYCLIC COMPOUND SERVING AS WEE1 INHIBITOR AND APPLICATIONS THEREOF

Disclosed in the present invention are a macrocyclic compound serving as a Weel inhibitor, and applications thereof in the preparation of drugs for treating Weel-related diseases. The present invention specifically relates to a compound represented by for

PHENYLAMINOPYRIMIDINE AMIDE AUTOPHAGY INHIBITORS AND METHODS OF USE THEREOF

Described herein are compounds that are inhibitors of autophagy and their use in the treatment of disorders such as cancers.

HETEROCYCLIC COMPOUNDS AND USES THEREOF

Heterocyclic compounds as Wee1 inhibitors are provided. The compounds may find use as therapeutic agents for the treatment of diseases and may find particular use in oncology.

Diacylglycerol Acyltransferase Inhibitors

Provided herein are compounds of the formula (1): as well as pharmaceutically acceptable salts thereof wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type 11 diabetes mellitus and metabolic syndrome.

New 1-aryl-3-substituted propanol derivatives as antimalarial agents

This paper describes the synthesis and in vitro antimalarial activity against a P. falciparum 3D7 strain of some new 1-aryl-3-substituted propanol derivatives. Twelve of the tested compounds showed an IC50 lower than 1 μM. These compounds were

THIENOPYRIDINE DERIVATIVES

The present invention provides a compound promoting osteogenesis. The present invention provides a compound having the following general formula (I) wherein R 1 is H or alkyl, R 2 is R a S-, R a O-, R a NH-, R a (R b )N- or cyclic amino, and R a and R b are alkyl which may be substituted, cycloalkyl which may be substituted, or the like, or a pharmacologically acceptable salt thereof.

UREA DERIVATIVE

The present invention relates to a urea derivative or a pharmacologically acceptable salt thereof having an excellent DGAT inhibitory effect. A urea derivative having the formula: [wherein R 1 is a C 6 -C 10 aryl group which may be independently mono- to pentasubstituted by a group selected from Substituent Group a or others; R 2 is a C 6 -C 10 aryl group which may be independently mono- to pentasubstituted by a group selected from Substituent Group a or others; E is a group having the formula (II) or the formula (III) (wherein R 3 is a hydrogen atom or others; R 4 and R 5 , which are the same or different, are a hydrogen atom or others; X and U, which are the same or different, are a group represented by the formula CH or others; m and n, which are the same or different, are 1 or another number) or others; and A is a group represented by the formula -NH-C(=O)- or others], or a pharmacologically acceptable salt thereof.

NOVEL AZACYCLY-SUBSTITUTED ARYLTHIENOPYRIMIDINONES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS MEDICAMENTS

The invention relates to azacyclyl-substituted arylthienopyrimidinones and their derivatives of formula (I), and their physiologically tolerated salts and physiologically functional derivatives, their preparation, medicaments comprising at least one azacyclyl-substituted arylthienopyrimidinone of the invention or its derivative, and the use of the azacyclyl-substituted aryithienopyrimidinones of the invention and their derivatives as MCH antagonists.

Pyrido[2,3-d]pyrimidin-7-ones as specific inhibitors of cyclin-dependent kinase 4

Inhibition of the cell cycle kinase, cyclin-dependent kinase-4 (Cdk4), is expected to provide an effective method for the treatment of proliferative diseases such as cancer. The pyrido[2,3-d]-pyrimidin-7-one template has been identified previously as a privileged structure for the inhibition of ATP-dependent kinases, and good potency against Cdks has been reported for representative examples. Obtaining selectivity for individual Cdk enzymes, particularly Cdk4, has been challenging. Here, we report that the introduction of a methyl substituent at the C-5 position of the pyrido[2,3-d]pvrimidin-7-one template is sufficient to confer excellent selectivity for Cdk4 vs other Cdks and representative tyrosine kinases. Further optimization led to the identification of highly potent and selective inhibitors of Cdk4 that exhibit potent antiproliferative activity against human tumor cells in vitro. The most selective Cdk4 inhibitors were evaluated for antitumor activity against MDA-MB-435 human breast carcinoma xenografts in mice.