20951-01-3

Upstream product

• 504-24-5 4-aminopyridine 
• 102-09-0 bis(phenyl) carbonate 
• 1885-14-9 phenyl chloroformate 

Downstream Products

• 1170321-66-0 3-endo-(phenylsulfonyl)-N-(pyridin-4-yl)-8-azabicyclo[3.2.1]octane-8-carboxamide 
• 1394894-40-6 C₂₃H₂₃ClN₄O₂ 
• 14547-74-1 4-methyl-N-(pyridin-4-yl)benzamide 
• 1620290-70-1 4-(3-((5-(([1,1'-biphenyl]-2-yloxy)methyl)-4,5-dihydroisoxazol-3-yl)methyl)ureido)pyridine-1-oxide 
• 1620289-83-9 1-((5-(([1,1'-biphenyl]-2-yloxy)methyl)-4,5-dihydroisoxazol-3-yl)methyl)-3-(pyridin-4-yl)urea 
• 153539-26-5 4-(pyridin-4-yl)semicarbazide 
• 1299487-16-3 1-(4-(1-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)benzyl)piperidin-4-yloxy)phenyl)-3-(pyridin-4-yl)urea 
• 1299487-60-7 1-(4-((1-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)benzyl)piperidin-4-yl)methyl)phenyl)-3-(pyridin-4-yl)urea 
• 1299488-97-3 1-(2-(1-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)benzyl)piperidin-4-yl)-1H-indazol-5-yl)-3-(pyridin-4-yl)urea 
• 1299488-95-1 1-(1-(1-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)benzyl)piperidin-4-yl)-1H-benzo[d]imidazol-5-yl)-3-(pyridin-4-yl)urea 
• 1299488-91-7 1-(1-(1-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)benzyl)piperidin-4-yl)-1H-benzo[d]imidazol-6-yl)-3-(pyridin-4-yl)urea 
• 1299488-82-6 1-(3-fluoro-4-((1-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)benzyl)piperidin-4-yl)(methyl)amino)phenyl)-3-(pyridin-4-yl)urea 

Relevant academic research and scientific papers

Compound for specifically enhancing spatial coupling degree of TRPV4-KCa2.3 complex and application of compound

The invention discloses a compound for specifically enhancing the spatial coupling degree of a TRPV4-KCa2.3 complex and an application of the compound, and belongs to the field of chemical medicines.The compound with the structure represented by the general formula (I) is mainly used for uncoupling TRPV4 and KCa2.3 in hypertensive patients, so that two uncoupled proteins can be recoupled, and thenormal state of the two uncoupled proteins can be recovered. Under the normal condition, according to TRPV4 and KCa2.3, TRPV4 receive signals of calcium ions, due to calcium ion inflow, potassium ionoutflow of a downstream KCa2.3 channel is stimulated, vasodilation is achieved through depolarization, and thus the blood pressure of the hypertensive patients is recovered to the normal level.

ISOINDOLINONE COMPOUNDS

Disclosed herein is a compound or pharmaceutically acceptable salts or stereoisomers thereof of of formula I wherein X1 is linear or branched C1-6 alkyl, C3-6 cycloalkyl, -C1-6 alkyl C3-6 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, C1-6 alkyl C6-10 aryl, C1-6 alkyl 5-10 membered heteroaryl, wherein X1 is unsubstituted or substituted with one or more of halogen, linear or branched C1-6 alkyl, linear or branched C1-6 heteroalkyl, CF3, CHF2, -O-CHF2, -O-(CH2)2-OMe, OCF3, C1-6 alkylamino, -CN, -N(H)C(O)-C1- 6alkyl, -OC(O)-C1-6alkyl, -OC(O)-C1-4alkylamino, -C(O)O-C1-6alkyl, -COOH, - CHO, -C1-6alkylC(O)OH, -C1-6alkylC(O)O-C1-6alkyl, NH2, C1-6 alkoxy or C1-6 alkylhydroxy; X2 is hydrogen, C6-10 aryl, 5-10 membered heteroaryl, -O-(5-10 membered heteroaryl), 4-8 membered heterocycloalkyl, C1-4 alkyl 4-8 membered heterocycloalkyl, -O-(4-8 membered heterocycloalkyl), -O-C1-4 alkyl-(4-8 membered heterocycloalkyl), -OC(O)-C1-4alkyl-4-8 membered heterocycloalkyl or C6 aryloxy, wherein X2 is unsubstituted or substituted with one or more of linear or branched C1-6 alkyl, NH2, NMe2 or 5-6 membered heterocycloalkyl; n is 0, 1 or 2.

Design and development of 1,3,4-oxadiazole derivatives as potential inhibitors of acetylcholinesterase to ameliorate scopolamine-induced cognitive dysfunctions

The novel hybrids bearing 4-aminopyridine (4-AP) tethered with substituted 1,3,4-oxadiazole nucleus were designed, synthesized, and evaluated for their potential AChE inhibitory property along with significant antioxidant potential. The inhibitory potenti

Synthesis and Structure–Activity Relationship Studies of Benzo[b][1,4]oxazin-3(4H)-one Analogues as Inhibitors of Mycobacterial Thymidylate Synthase X

Since the discovery of a flavin-dependent thymidylate synthase (ThyX or FDTS) that is absent in humans but crucial for DNA biosynthesis in a diverse group of pathogens, the enzyme has been pursued for the development of new antibacterial agents against Mycobacterium tuberculosis, the causative agent of the widespread infectious disease tuberculosis (TB). In response to a growing need for more effective anti-TB drugs, we have built upon our previous screening efforts and report herein an optimization campaign of a novel series of inhibitors with a unique inhibition profile. The inhibitors display competitive inhibition toward the methylene tetrahydrofolate cofactor of ThyX, enabling us to generate a model of the compounds bound to their target, thus offering insight into their structure–activity relationships.

4,5-DIHYDROISOXAZOLE DERIVATIVES AS NAMPT INHIBITORS

The present invention provides 4,5-dihydroisoxazole derivatives of formula (I), which may be therapeutically useful, more particularly as NAMPT inhibitors. wherein, ring A, L1, L2, X1, X2, X3, Z, R1, R2, R3, R4, R5, m, n, p and q have the meanings given in the specification and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder, caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPT) in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted 4,5-dihydroisoxazole derivatives of formula (I) or a pharmaceutically acceptable salt thereof or a stereoisomer thereof.

SUBSTITUTED OXAZOLE- AND THIAZOLE-BASED CARBOXAMIDE AND UREA DERIVATIVES AS VANILLOID RECEPTOR LIGANDS II

The invention relates to oxazole and thiazole-based carboxamide and urea derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.

Preparation of substituted semicarbazides from corresponding amines and hydrazines via phenyl carbamates

A simple synthetic procedure for the conversion of amines and hydrazines into substituted semicarbazides was developed. The initial condensation between the desired amine and phenyl chloroformate into phenyl carbamate is followed by the addition of hydrazine under basic conditions. The reaction is tolerable to a variety of functional groups, with mild conditions and high percent yields.

4,5-DIHYDROISOXAZOLE DERIVATIVES AS NAMPT INHIBITORS

The present invention provides substituted 4,5-dihydroisoxazole derivatives of formula (I), which may be therapeutically useful, more particularly NAMPT inhibitors and in which R1 R2, Y, X, "Het" and "p" have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPT) in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted 4,5-dihydroisoxazole derivatives of formula (I) or a pharmaceutically acceptable salts or stereoisomers or N-oxide thereof.

Synthesis and biological evaluation of 4-phenoxy-6,7-disubstituted quinolines possessing semicarbazone scaffolds as selective c-Met inhibitors

Novel quinoline derivatives bearing acyclic semicarbazones were prepared and their chemical structures as well as the relative stereochemistry were confirmed. All the synthesized compounds were evaluated for their c-Met kinase inhibitory activity and their cytotoxicity against the cell lines HT-29, MKN-45, and MDA-MB-231 in vitro. Several potent compounds were further evaluated against A549 cells. Most compounds displayed moderate to excellent activity, and the structure-activity relationship studies identified the most promising compound 35 as a selective c-Met kinase inhibitor (IC50 = 4.3 nM). Compound 35 showed a 3.5- and 18.8-fold increase in cytotoxicity in vitro against HT-29 and A549 cells, respectively, compared to that of foretinib. Poor off-target effects of compound 35 were further confirmed by the antiproliferative activity against the c-Met inhibition less sensitive MDA-MB-231 cell line (IC50 = 0.77 μM). Copyright

Aryl piperazinyl ureas as inhibitors of fatty acid amide hydrolase (FAAH) in rat, dog, and primate

A series of aryl piperazinyl ureas that act as covalent inhibitors of fatty acid amide hydrolase (FAAH) is described. A potent and selective (does not inhibit FAAH-2) member of this class, JNJ-40355003, was found to elevate the plasma levels of three fatt