1932042-59-5

Upstream product

• 198835-06-2 5-oxo-2-azabicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester 
• 198835-03-9 rac-tert-butyl (1S,4S,5R)-5-hydroxy-2-azabicyclo[2.2.1]heptane-2-carboxylate 
• 542-92-7 cyclopenta-1,3-diene 
• 24424-99-5 di-tert-butyl dicarbonate 
• 1400808-00-5 5-oxo-2-azabicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester 
• 702666-73-7 tert-butyl (1R,4S)-(+)-2-azabicyclo[2.2.1]hept-5-ene-2-carboxylate 
• 79200-56-9 (-)-2-azabicyclo[2.2.1]hept-5-en-3-one 
• 702666-72-6 tert-butyl (1S,4R)-2-azabicyclo[2.2.1]heptan-5-en-2-carboxylate 
• 130931-83-8 (1S,4R)-2-azabicyclo[2,2,1]hept-5-en-3-one 
• 198835-03-9 tert-butyl (1S,4S,5R)-5-hydroxy-2-azabicyclo[2.2.1]heptane-2-carboxylate 
• 188345-71-3 2-(tert-butoxycarbonyl)-2-azabicyclo[2.2.1]hept-5-ene 

Downstream Products

• 1415574-00-3 benzyl 5-({cis-4-[2-(benzyloxy)-2-oxoethyl]cyclohexyl}oxy)-2-azabicyclo[2.2.1]heptane-2-carboxylate 

Relevant academic research and scientific papers

RET inhibitor and pharmaceutical composition and application thereof

The invention belongs to the field of medicines, and relates to an RET inhibitor and a pharmaceutical composition and application thereof. Specifically, the invention relates to a compound as shown in a formula (I), or a stereoisomer, a tautomer, a nitrogen oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug of the compound as shown in the formula (I). The invention also relates to pharmaceutical compositions comprising the compounds, and uses of the compounds and pharmaceutical compositions thereof in the preparation of a medicine which is especially used for the treatment and prevention of RET-related diseases and disorders, including cancers, irritable bowel syndrome and/or pain associated with irritable bowel syndrome.

FXR RECEPTOR AGONIST

The present invention belongs to the technical field of pharmaceuticals, and particularly relates to a compound of formula (I), a pharmaceutically acceptable salt thereof, an ester thereof or a stereoisomer of the compound, the salt or the ester, wherein

Synthesis and biological evaluation of pyrimidine derivatives with diverse azabicyclic ether/amine as novel GPR119 agonist

A class of novel pyrimidine derivatives bearing diverse conformationally restricted azabicyclic ether/amine were designed, synthesized and evaluated for their GPR119 agonist activities against type 2 diabetes. Most compounds exhibited superior hEC50

TRICYCLIC GYRASE INHIBITORS FOR USE AS ANTIBACTERIAL AGENTS

Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. In addition, species of tricyclic gyrase inhibitors compounds are also disclosed herein. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.

Synthesis of novel azanorbornylpurine derivatives

Azanorbornylpurine derivatives were prepared by Mitsunobu reaction of appropriate hydroxyazanorbornane derivative with 6-chloropurine or construction of purine base at azanorbornylamines. The prepared target compounds were evaluated for antiviral activity and effect on neuronal and muscle nicotinic acetylcholine receptors.

TRICYCLIC GYRASE INHIBITORS

Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.

Improved synthesis of monoprotected 5- and 6-amino-2-azanorbornanes

(Chemical Equation Presented) An improved synthesis of Boc-monoprotected 5- and 6-amino-2-azanorbornanes is reported. The synthetic scheme consists of five steps and allows multigram quantities of the title compounds to be obtained. The regio- and stereochemistries of the products are established by two-dimensional NMR experiments. Copyright Taylor & Francis Group, LLC.

Discovery of a nortropanol derivative as a potent and orally active GPR119 agonist for type 2 diabetes

The lead optimization studies of a series of GPR119 agonists incorporating a nortropanol scaffold are described. Extensive structure-activity relationship (SAR) studies of the lead compound 20f led to the identification of compound 36j as a potent, single digit nanomolar GPR119 agonist with high agonist activity. Compound 36j was orally active in lowering blood glucose levels in a mouse oral glucose tolerance test and increased plasma insulin levels in a rat hyperglycemic model. It showed good to excellent pharmacokinetic properties in rats and monkeys and no untoward activities in counter-screen assays. Compound 36j demonstrated an attractive in vitro and in vivo profile for further development.

PIPERAZINO DERIVATIVES AS NEUROKININ ANTAGONISTS

The invention relates to compounds of formula (I) wherein Z, Rc, y, m, u, Ar2, n, X, Rc', l and Ar2 are as described herein. These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.

Heterocyclic compounds

The present invention provides heterocyclic 2-aza-bicyclo[2.2.1]heptane compounds which are useful for modulating a muscarinic ptor.