683269-95-6

Upstream product

• 53292-90-3 trans-4-(tert-butoxycarbonylamino)cyclohexanoic acid 
• 239074-29-4 trans (4-hydroxymethyl-cyclohexyl)-carbamic acid tert-butyl ester 
• 7143-01-3 Methanesulfonic anhydride 
• 24424-99-5 di-tert-butyl dicarbonate 
• 27960-59-4 trans-4-aminocyclohexanecarboxylic acid hydrochloric acid 
• 62456-15-9 methyl trans-4-amino-cyclohexanecarboxylate 
• 146307-51-9 methyl (1R,4R)-4-((tert-butoxycarbonyl)amino)cyclohexane-1-carboxylate 
• 15177-67-0 trans-4-(methoxycarbonyl)cyclohexanecarboxylic acid 
• 124-63-0 methanesulfonyl chloride 

Downstream Products

• 956352-36-6 N-[(trans)-4-(azidomethyl)cyclohexyl]carbamic acid tert-butyl ester 
• 506427-91-4 trans N-tert-butoxycarbonyl-4-{2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]ethyl}-cyclohexylamine 
• 791778-53-5 trans-4-(2-(4-(2,3-dichlorophenyl)piperazin-1-yl)ethyl)cyclohexane-1-amine 
• 215790-29-7 trans-2-(1-(4-(N-tert-butoxycarbonyl)amino)cyclohexyl)acetaldehyde 
• 1313279-47-8 trans-(4-cyanomethyl-cyclohexyl)-carbamic acid tert-butyl ester 
• 1607592-65-3 {1-[trans-4-(cyanomethyl)cyclohexyl]-1H-imidazo[4,5-d]thieno[3,2-b]pyridin-2-yl}acetonitrile trifluoroacetate 
• 1607591-64-9 [trans-4-(2-ethyl-1H-imidazo[4,5-d]thieno[3,2-b]pyridin-1-yl)cyclohexyl]acetonitrile 
• 1607589-82-1 (trans-4-{2-[(1R)-1-hydroxyethyl]-1H-imidazo[4,5-d]thieno[3,2-b]pyridin-1-yl}cyclohexyl)acetonitrile 
• 1607589-86-5 {trans-4-[(6-aminothieno[3,2-b]pyridin-7-yl)amino]cyclohexyl}acetonitrile 
• 1607589-85-4 {trans-4-[(6-nitrothieno[3,2-b]pyridin-7-yl)amino]cyclohexyl}acetonitrile 
• 1607590-75-9 {trans-4-[2-(1-methylazetidin-3-yl)-1H-imidazo[4,5-d]thieno[3,2-b]pyridin-1-yl]cyclohexyl}acetonitrile 
• 1607590-73-7 [trans-4-(2-azetidin-3-yl-1H-imidazo[4,5-d]thieno[3,2-b]pyridin-1-yl)cyclohexyl]acetonitrile 
• 1607590-74-8 tert-butyl 3-{1-[trans-4-(cyanomethyl)cyclohexyl]-1H-imidazo[4,5-d]thieno[3,2-b]pyridin-2-yl}azetidine-1-carboxylate 
• 1607590-72-6 [trans-4-(2-isopropyl-1H-imidazo[4,5-d]thieno[3,2-b]pyridin-1-yl)cyclohexyl]acetonitrile 

Relevant academic research and scientific papers

SSAO INHIBITORS AND USE THEREOF

Provided are a compound of formula (I') or (I), a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of SSAO, a pharmaceutical composition comprising a compound of formula (I') or (I), and a method of treating or preventing a disease in which SSAO plays a role.

Synthesis of Bitopic Ligands as Potent Dopamine D2 Receptor Agonists

In this study, we designed and synthesized twelve bitopic ligands as dopamine D2 receptor (D2R) agonists. The forskolin-induced cAMP accumulation assay revealed that all the finial compounds are able to activate D2R. Furthermore, bitopic ligand N-((trans)-4-(((2,3-dihydro-1H-inden-2-yl)(propyl)amino)methyl)cyclo-hexyl)-1H-pyrrolo[2,3-b]pyridine-2-carboxamide (11 b) showed 21-fold higher potency than lead compound propyl aminoindane (2) and 17-fold higher subtype selectivity for D2R over D4R, indicating that the optimal length of spacer affects the D2R functionality. Molecular modeling study exhibited that 11 b formed an electrostatic interaction and two H-bonds with amino acid Asp114, which contributes significantly to the D2R functional activity. Taken together, we discovered a bitopic ligand 11 b as potent D2R agonist, which may be used as a tool compound for further study.

Generation of highly potent DYRK1A-dependent inducers of human β-Cell replication via Multi-Dimensional compound optimization

Small molecule stimulation of β-cell regeneration has emerged as a promising therapeutic strategy for diabetes. Although chemical inhibition of dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A) is sufficient to enhance β-cell replicat

Discovery of a Gut-Restricted JAK Inhibitor for the Treatment of Inflammatory Bowel Disease

To identify Janus kinase (JAK) inhibitors that selectively target gastrointestinal tissues with limited systemic exposures, a class of imidazopyrrolopyridines with a range of physical properties was prepared and evaluated. We identified compounds with low intrinsic permeability and determined a correlation between permeability and physicochemical properties, clogP and tPSA, for a subset of compounds. This low intrinsic permeability translated into compounds displaying high colonic exposure and low systemic exposure after oral dosing at 25 mg/kg in mouse. In a mouse PK/PD model, oral dosing of lead compound 2 demonstrated dose-dependent inhibition of pSTAT phosphorylation in colonic explants post-oral dose but low systemic exposure and no measurable systemic pharmacodynamic activity. We thus demonstrate the utility of JAK inhibitors with low intrinsic permeability as a feasible approach to develop gut-restricted, pharmacologically active molecules with a potential advantage over systemically available compounds that are limited by systemic on-target adverse events.

FUSED CYCLIC UREA DERIVATIVES AS CRHR2 ANTAGONIST

The present invention relates to fused cyclic urea derivatives which have antagonistic activities against CRHR1 and/or CRHR2, and which are useful in the treatment or prevention of disorders and diseases in which CRHR1 and/or CRHR2 is involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CRHR1 and/or CRHR2 is involved.

IRAK DEGRADERS AND USES THEREOF

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

D2 Dopamine Receptor G Protein-Biased Partial Agonists Based on Cariprazine

Functionally selective G protein-coupled receptor ligands are valuable tools for deciphering the roles of downstream signaling pathways that potentially contribute to therapeutic effects versus side effects. Recently, we discovered both Gi/o-bi

NOVEL JAK1 SELECTIVE INHIBITORS AND USES THEREOF

The new 1H-furo[3,2-b]imidazo[4,5-d]pyridine derivatives are selective Jak1 kinase inhibitors useful in treating disorders related to Jak1 activities such as autoimmune diseases or disorders, inflammatory diseases or disorders, and cancer or neoplastic di

IMIDAZOPYRROLOPYRIDINE AS INHIBITORS OF THE JAK FAMILY OF KINASES

2-((1r,4r)-4-(imidazo[4,5-d]pyrrolo[2,3-b]pyridin-1(6H)-yl)cyclohexyl)acetonitrile compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions mediated by JAK, such as inflammatory bowel disease.

Preparation method of trans-4-Boc-aminocyclohexane acetic acid

The invention discloses a preparation method of trans-4-Boc-aminocyclohexane acetic acid. The preparation method specifically comprises the steps of reducing carboxyl of trans-4-Boc-aminocyclohexane methanoic acid, so as to obtain trans-4-Boc-aminocyclohexane methanol, reacting with sulfonyl chloride, so as to obtain trans-4-Boc-aminocyclohexane methanol sulphonate, generating substitution reaction with cyanide, so as to obtain trans-4-Boc-aminocyclohexane acetonitrile, and finally carrying out cyan hydrolysis, so as to obtain a target product. The raw materials used in the preparation method are cheap and easily available, the yield is high, and a production process is suitable for large-scale production and can be widely applied to the pharmacy field.