62596-26-3

Upstream product

• 17159-79-4 ethyl 4-oxocyclohexane-1-carboxylate 
• 100-39-0 benzyl bromide 
• 3685-22-1 4-hydroxycyclohexanecarboxylic acid 
• 99-96-7 4-hydroxy-benzoic acid 
• 874-61-3 4-oxocyclohexanecarboxylic acid 
• 123762-06-1 benzyl 4-hydroxycyclohexane-1-carboxylate 
• 216106-48-8 4-oxo-bicyclo[3.1.0]hexane-1-carboxylic acid benzyl ester 
• 91503-67-2 (±)-benzyl cyclohex-3-ene-1-carboxylate 

Downstream Products

• 916736-77-1 benzyl 4-fluoro-cyclohex-3-ene-1-carboxylate 
• 1075221-15-6 4,4-difluoro-1-hydroxycyclohexanecarboxylic acid 
• 1379194-22-5 4,4-difluorocyclohex-1-ene-1-carboxylic acid 
• 916736-78-2 benzyl 4,4-difluoro-1-hydroxycyclohexanecarboxylate 
• 1163729-47-2 4-hydroxy-4-(trifluoromethyl)cyclohexane-1-carboxylic acid 

Relevant academic research and scientific papers

TGF-betaR1 inhibitor and application thereof

The invention belongs to the field of medical chemistry, and particularly relates to a compound serving as a TGF-betaR1 inhibitor and application of the compound. Specifically, the invention providesa compound shown as a formula I or an isomer, a pharmaceutically acceptable salt, a solvate, a crystal or a prodrug thereof, a preparation method of the compounds, a pharmaceutical composition containing the compounds and application of the compounds or the composition to treatment and/or prevention of TGF-betaR1 related diseases, such as cancers, tissue hyperplasia diseases, fibrosis and inflammatory diseases. The compound provided by the invention shows significant inhibitory activity on TGF-betaR1 kinase, and is very expected to become a therapeutic agent for TGF-betaR1 related diseases.

DIHYDROPYRIMIDINE DERIVATIVES AND USES THEREOF IN THE TREATMENT OF HBV INFECTION OR OF HBV-INDUCED DISEASES

The application describes dihydropyrimidine derivatives which are useful in the treatment or prevention of HBV infection or of HBV-induced diseases, more particularly of HBV chronic infection or of diseases induced by HBV chronic infection, as well as pharmaceutical or medical applications thereof.

SUBSTITUTED BICYCLIC COMPOUNDS AS FARNESOID X RECEPTOR MODULATORS

Disclosed are compounds of Formula (I): or a stereoisomer, a tautomer, or a salt or solvate thereof, wherein Q is C2-6 alkenyl or C2-6 alkynyl, each substituted with zero to 2 R1; and the other variables are as defined herein. These compounds modulate the activity of farnesoid X receptor (FXR), for example, as agonists. Also disclosed are pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.

DIHYDROPYRIMIDINE DERIVATIVES AND USES THEREOF IN THE TREATMENT OF HBV INFECTION OR OF HBV-INDUCED DISEASES

Provided herein are dihydropyrimidine derivatives which are useful in the treatment of HBV infection or HBV-induced diseases, as well as pharmaceutical or medical applications thereof.

Tetraoxanes as inhibitors of apicomplexan parasites Plasmodium falciparum and Toxoplasma gondii growth and anti-cancer molecules

New cyclohexylidene 1,2,4,5-tetraoxanes with polar guanidine and urea based groups were synthesized and evaluated for their antimalarial activity against chloroquine resistant and susceptible Plasmodium falciparum strains. The derivatives showed moderate, nM range antimalarial activities and low cytotoxicity. The N-phenylurea derivative 24 exhibited the best resistance indices (RIW2 = 0.44, RITM91C235 = 0.80) and was not toxic against human normal peripheral blood mononuclear cells (IC50 > 200 μM). Seven derivatives were tested in vitro against four human cancer cell lines and they demonstrated high selectivity toward leukaemia K562 cells. One compound, derivative 21 with a primary amino group, was the first tetraoxane tested in vivo against Toxoplasma gondii as another apicomplexan parasite. Subcutaneous administration at a dose of 10 mg kg-1 day-1 for 8 days allowed the survival of 20 % of infected mice, thus demonstrating the high potential of tetraoxanes for the treatment of apicomplexan parasites.

TETRAZOLONES AS INHIBITORS OF FATTY ACID SYNTHASE

Provided herein are tetrazolone FASN inhibitors of the formula (I): or a pharmaceutically acceptable form thereof; wherein the variables RA, RB and RC are defined herein. Also provided herein are pharmaceutical compositions of the compounds provided herein as well as methods of their use for the treatment of various disorders such as hyperproliferative disorders, inflammatory disorders, obesity-related disorders and microbial infections.

Bradykinin B1 receptor antagonists: An α-hydroxy amide with an improved metabolism profile

A series of carbo- and heterocyclic α-hydroxy amide-derived bradykinin B1 antagonists was prepared and evaluated. A 4,4-difluorocyclohexyl α-hydroxy amide was incorporated along with a 2-methyl tetrazole in lieu of an oxadiazole to afford a suitable compound with good pharmacokinetic properties, CNS penetration, and clearance by multiple metabolic pathways.

l-HYDROXYCYCLOALKANECARBOXAMIDE DERIVATIVES AS BRADYKININ ANTAGONISTS

α-Hydroxycycloalkanecarboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, wherein formula (a) is a single or double bond; Rl, R2 and R3 are each independently selected from H, halogen and OH; or Rl and R2 attached to the same carbon atom together represent oxo; R4 is H or methyl; R5 is Cl or F; R6 is selected from -CO2-C1-4alkyl, -O-C1-4alkyl, -O- C1-4haloalkyl, 2-methyltetrazol-5-yl, 5-methyl l,2,4-oxadiazol-3-yl, 3-methyl-1,2,4-oxadiazol-5-yl, 5-halomethyl-l,2,4-oxadiazol-3-yl, 3-halomethyl- l,2,4-oxadiazol-5-yl, tetrazol-5-yl, 5-halomethyl-l,2,3-triazolyl, and 5-methyl-l ,2,3-triazolyl; R7 and R8 are each independently Cl or F; and n is 0 or 1, are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.

SmI2-induced ring expansion reactions of alkyl (n+1)- oxobicyclo[n.1.0]alkane-1-carboxylates

Alkyl 4-oxocycloalkanecarboxylates were prepared in good yield via ring expansion reactions of alkyl (n+1)-oxobicyclo[n.1.0]alkane-1-carboxylates mediated by SmI2-induced single electron transfer in THF/MeOH.

BIS(TRIFLUOROACETYLACETONATO)COBALT(II) CATALYZED OXIDATION-REDUCTION HYDRATION OF OLEFINS SELECTIVE FORMATION OF ALCOHOLS FROM OLEFINS

Various olefins are hydrated with molecular oxygen (oxidant) and a secondary alcohol (reductant) in the presence of a catalytic amount of bis(trifluoroacetylacetonato)cobalt(II) in good yields