5963-75-7

Upstream product

• 34094-21-8 (3-bromopropyl)cyclohexane 
• 1216963-74-4 lithium acetylide-ethylenediamine complex 
• 147936-56-9 3-cyclohexyl-1-iodopropane 
• 1124-63-6 3-cyclohexylpropan-1-ol 

Downstream Products

• 141345-30-4 9-(2,3,5-tri-O-acetyl-1-β-D-ribofuranosyl)-6-chloro-2-(5-cyclohexyl-1-pentyn-1-yl)purine 
• 4292-92-6 n-pentylcyclohexane 
• 538-68-1 pentylbenzene 
• 141345-15-5 2-(5-cyclohexyl-1-pentyn-1-yl)adenosine 

Relevant academic research and scientific papers

AMINO ALCOHOL DERIVATIVE OR PHOSPHONIC ACID DERIVATIVE AND MEDICINAL COMPOSITION CONTAINING THESE

The present invention relates to amino alcohol derivatives or phosphonic acid derivatives having excellent immunosuppressive activity, pharmacologically acceptable salts thereof or pharmacologically acceptable esters thereof, and to pharmaceutical compositions comprising said compounds as an active ingredient: [wherein, ???R1 and R2 each represent a hydrogen atom, or a protecting group of the amino group; ???R3 represents a hydrogen atom, or a protecting group of the hydroxyl group; ???R4 represents a lower alkyl group; ???n represents an integer of from 1 to 6; ???X represents an oxygen atom or a nitrogen atom unsubstituted or substituted with a lower alkyl group or the like; ???Y represents an ethylene group; ???Z represents a C1-C10 alkylene group; ???R5 represents an aryl group, or an aryl group substituted with substituents; ???R6 and R7 each represents a hydrogen atom; provided that when R5 represents a hydrogen atom, then Z represents a group other than a single bond or a straight chain C1-C10 alkylene group] .

AMINO ALCOHOL DERIVATIVES

The present invention relates to compounds of formula (I) which exhibit excellent immune suppression activity, pharmacologically acceptable salts thereof, esters thereof or other derivatives: wherein R1 and R2 are a hydrogen atom, an amino protecting group; R3 is a hydrogen atom, a hydroxy protecting group; R4 is a lower alkyl group; n is an integer from 1 to 6; X is an ethylene group; Y is a C1-C10 alkylene group, a C1-C10 alkylene group substituted with 1 to 3 substituents selected from substituent group a and b; R5 is an aryl group; R6 and R7 are a hydrogen atom, a group selected from substituent group a; with the proviso when R5 is a hydrogen atom, Y is not a single bond or a straight chain C1-C10 alkylene group.

Amino alcohol derivatives

Compounds of formula (I) which exhibit excellent immune suppression activity, pharmacologically acceptable salts thereof, esters thereof or other derivatives: wherein R1 and R2 are a hydrogen atom, an amino protecting group; R3 is a hydrogen atom, a hydroxy protecting group; R4 is a lower alkyl group; n is an integer from 1 to 6; X is an ethylene group; Y is a C1-C10 alkylene group, a C1-C10 alkylene group substituted with 1 to 3 substituents selected from substituent group a and b; R5 is an aryl group; R6 and R7 are a hydrogen atom, a group selected from substituent group a; with the proviso when R5 is a hydrogen atom, Y is not a single bond or a straight chain C1-C10 alkylene group.

Nucleosides and nucleotides. 107. 2-(cycloalkylalkynyl)adenosines: Adenosine A2 receptor agonists with potent antihypertensive effects

Adenosine receptor-binding profiles in rat brain tissues and antihypertensive effects in spontaneously hypertensive rats (SHR) of a series of 2-(cycloalkylalkynyl)adenosine (2-CAAs) and their congeners are described. The structure-activity relationship of this series of compounds is discussed, focusing on the length of the alkynyl side chain and bulkiness of the terminal cycloalkyl substituents in terms of binding activity and cardiovascular effects. All the 2-CAAs had a preferential affinity for A2 receptors. Of these derivatives, 2-(3-cyclopentyl-1-propyn-1-yl)adenosine (10b) exhibited the most selective affinity for A2 receptors (K(i) ratio: A1/A2 = 70) on the basis of receptor binding. In the C-2 binding region of adenosine, compounds often have potent and/or selective A2 activity from introduction of an acetylenic group at the C-2 position followed by one methylene residue further followed by a hydrophobic substituent such as a cycloalkyl ring at the terminal position of the alkynyl side chain. Intravenous injection of 10b up to 100 μg/kg had a potent hypotensive effect without a marked decrease in heart rate in anesthetized SHR. Compounds 10j-s, with a hydroxyl group in the C-3 position of the alkynyl side chain, had a potent affinity for both A1 and A2 receptors, but they were not highly selective for A2 receptors. These compounds caused a marked bradycardia upon intravenous administration in anesthetized SHR. Oral administration of 10b (0.1-1 mg/kg) had a potent and long-lasting antihypertensive effect in conscious SHR.