36218-60-7

Upstream product

• 15177-67-0 trans-4-(methoxycarbonyl)cyclohexanecarboxylic acid 
• 3399-22-2 dimethyl 1,4-cyclohexanedicarboxylate 
• 619-82-9 trans-hexahydroterephthalic acid 

Downstream Products

• 134955-99-0 4-Isopropenyl-cyclohexanecarboxylic acid 
• 183996-95-4 4-Isopropenyl-cyclohexanecarboxylic acid methyl ester 
• 183996-83-0 N-[trans-4-(2-hydroxy-1-methylethyl)cyclohexanecarbonyl]-D-phenylalanine 
• 946530-05-8 trans-N-2-{2-[4-(2-methoxy-phenyl)piperazinyl]ethyl}-N-(2-pyridyl)-N-(4-carboxymethylcyclohexane) carboxamide 
• 1345045-52-4 trans-4-(3-fluoro-pyridine-4-carbonyl)-cyclohexanecarboxylic acid methyl ester 
• 1345045-51-3 trans-4-(3-fluoro-pyridine-2-carbonyl)-cyclohexanecarboxylic acid methyl ester 
• 1345045-64-8 trans-4-(2-benzylsulfanyl-benzoyl)-cyclohexanecarboxylic acid methyl ester 
• 1345045-67-1 trans-4-benzo[d]isothiazol-3-yl-cyclohexanecarboxylic acid methyl ester 
• 1005502-63-5 trans-4-(2-fluoro-benzoyl)-cyclohexanecarboxylic acid methyl ester 
• 946530-07-0 (1r,4r)-4-(hydroxymethyl)-N-(2-(4-(2-methoxyphenyl)piperazin-1-yl)ethyl)-N-(pyridin-2-yl)cyclohexanecarboxamide 

Relevant academic research and scientific papers

Palladium-Catalyzed Migratory Insertion of Carbenes and C-C Cleavage of Cycloalkanecarboxamides

A palladium catalyzed reaction of cycloalkanecarboxamides and diazomalonates or bis(phenylsulfonyl)diazomethane has been developed. The reaction proceeds via carbene migratory insertion and cascade C-C cleavage pathways. Cycloalkanecarboxamides with four to seven membered rings are applicable in the transformation. A series of ring opening products were prepared with moderate yields. The finding provides valuable clues for the development of new reactions involving carbene migratory insertion and the cleavage of unstrained C(sp3)-C(sp3) bonds.

IRAK DEGRADERS AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same.

IRAK DEGRADERS AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same.

SMALL MOLECULE INHIBITORS OF ULK1

The present technology is directed to compounds, compositions, and methods related to inhibition of ULK1 and treatment of cancers therefrom.

IRAK DEGRADERS AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same. The compounds include an IRAK binding moiety capable of binding to IRAK4 and a degradation inducing moiety (DIM). The DIM could be DTM a ligase binding moiety (LBM) or lysine mimetic. The compounds could be useful as IRAK protein kinase inhibitors and applied to IRAK mediated disorders.

ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model

Lysophosphatidic acid (LPA) is a bioactive lipid mediator that elicits a number of biological functions, including smooth muscle contraction, cell motility, proliferation, and morphological change. LPA is endogenously produced by autotaxin (ATX) from extracellular lysophosphatidylcholine (LPC) in plasma. Herein, we report our medicinal chemistry effort to identify a novel and highly potent ATX inhibitor, ONO-8430506 (20), with good oral availability. To enhance the enzymatic ATX inhibitory activity, we designed several compounds by structurally comparing our hit compound with the endogenous ligand LPC. Further optimization to improve the pharmacokinetic profile and enhance the ATX inhibitory activity in human plasma resulted in the identification of ONO-8430506 (20), which enhanced the antitumor effect of paclitaxel in a breast cancer model.

1-(CYCLOALKYL-CARBONYL)PROLINE DERIVATIVE

A compound represented by formula (1) (in the formula: ring-D represents a three- to eight-membered hydrocarbon ring; Ra represents an optionally substituted amino C1-6 alkyl group or the like; Rb1 and Rb2 each independently represent a hydrogen atom, a halogen atom, or the like; Rc represents an optionally substituted C6-10 aryl group or the like; Rd represents a hydrogen atom or the like; and ring-Q represents a (hetero)aryl group or the like which may be substituted with a carboxyl group or the like) or a pharmaceutically acceptable salt thereof exhibits an excellent FXIa inhibitory activity, and is useful as a therapeutic agent against thrombosis or the like.

Cyclohexyl-4H,6H-5-oxa-2,3,10b-triaza-benzo[e]azulenes as V1a antagonists

The present invention provides 4H,6H-5-oxa-2,3,10b-triaza-benzo[e]azulenes, which act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.

PRODRUG BIPYRIDYLAMINOPYRIDINES AS SYK INHIBITORS

The present invention provides compounds of Formula (I), which are prodrugs of trans-4-[(1R)-(6-{[4-(difluoromethyl)pyridin-2-yl]amino}-4-methyl-2,3'-bipyridin-6'-yl)-1-hydroxyethyl]cyclohexanecarboxylic acid, a potent inhibitor of Syk. The compounds are useful in the treatment and prevention of diseases mediated by the enzyme, such as asthma, COPD, rheumatoid arthritis and cancer.

Counterion effects in the preparation of aldehyde-bisulfite adducts

The identification and development of an aldehyde-bisulfite adduct as an isolable starting material in the synthesis of the CETP inhibitor Evacetrapib are described. The physical properties of the sodium and potassium analogs are compared, and the extension of the scope of this study to include an investigation into the solid state properties of a range of sodium and potassium bisulfite adducts of commonly encountered aldehydes is discussed.