461023-63-2

Upstream product

• 111902-61-5 (2R,3R)-3-cyclohexyl-2,3-epoxypropan-1-ol 
• 42134-55-4 3-cyclohexyl-2-propen-1-ol 
• 4484-35-9 3-cyclohexylacrylic acid 
• 705-95-3 3-cyclohexylacrylic acid methyl ester 
• 80542-16-1 D-threo-2-amino-3-cyclohexyl-3-hydroxypropionic acid 
• 674782-28-6 C₃₃H₄₃N₃O₆ 
• 1280013-74-2 C₁₉H₃₃N₃O₃ 
• 1280013-68-4 C₂₆H₃₉N₃O₃ 
• 80542-17-2 (2R,3S)-2-(t-butoxycarbonylamino)-3-cyclohexyl-3-hydroxypropanoic acid 
• 115362-12-4 (-)-(2S,3S)-2,3-epoxy-3-cyclohexyl-1-propanol 
• 1319734-52-5 (4S,5R)-3-benzyl-5-cyclohexyl-2-oxo-oxazolidine-4-carboxylic acid 
• 1280013-87-7 methyl (4R,5R)-3-benzyl-5-cyclohexyl-2-oxo-oxazolidine-4-carboxylate 
• 1280013-86-6 (4R,5R)-3-benzyl-5-cyclohexyl-2-oxo-oxazolidine-4-carboxylic acid 
• 1280013-85-5 (4S,5R)-3-benzyl-5-cyclohexyl-4-(hydroxymethyl)oxazolidin-2-one 

Relevant academic research and scientific papers

Discovery of 4-[4-({(3R)-1-butyl-3-[(R)-cyclohexyl(hydroxy)methyl]-2,5- dioxo-1,4,9-triazaspiro[5.5]undec-9-yl}methyl)phenoxy]benzoic acid hydrochloride: A highly potent orally available CCR5 selective antagonist

Based on the original spirodiketopiperazine design framework, further optimization of an orally available CCR5 antagonist was undertaken. Structural hybridization of the hydroxylated analog 4 derived from one of the oxidative metabolites and the new orally available non-hydroxylated benzoic acid analog 5 resulted in another potent orally available CCR5 antagonist 6a as a clinical candidate. Full details of a structure-activity relationship (SAR) study and ADME properties are presented.

Spirodiketopiperazine-based CCR5 antagonist: Discovery of an antiretroviral drug candidate

Following the discovery that hydroxylated derivative 3 (Fig. 1) was one of the oxidative metabolites of the original lead 1, it was found that hydroxylated compound 4 possesses higher in vitro anti-HIV potency than the corresponding non-hydroxylated compo

TRIAZASPIRO 5.5 UNDECANE DERIVATIVES AND DRUGS COMPRISI NG THE SAME AS THE ACTIVE INGREDIENT

Compounds represented by formula (I) (wherein all of the symbols have the same meanings as defined in specification.), quaternary ammonium salts thereof, N-oxides thereof or salts thereof. The compounds represented by formula (I) are used for prevention a

NOVEL CRYSTALS OF TRIAZASPIRO 5.5 UNDECANE DERIVATIVE

The present invention relates to a new crystal of triazaspiro[5.5]undecane derivatives. The crystal of a non-solvate of (3R)-1-butyl-2,5-dioxo-3-[(1R)-1-hydroxy-1-cyclohexylmethyl]-9-[4-(4-carboxyphenyloxy)phenylmethyl]-1,4,9-triazaspiro[5.5]undecane hydr

DRUGS CONTAINING TRIAZASPIRO 5.5]UNDECANE DERIVATIVES AS THE ACTIVE INGREDIENT

A pharmaceutical composition for prevention and/or treatment for HIV infection or AIDS induced by the infection which comprises, as an active ingredient, a triazaspiro[5.5]undecane derivative, a quaternary ammonium salt thereof, an N-oxide thereof, or a n

TRIAZASPIRO 5.5]UNDECANE DERIVATIVES AND DRUGS CONTAINING THE SAME AS THE ACTIVE INGREDIENT

Triazaspiro[5.5]undecane derivatives of the formula (I), quaternary ammonium salts thereof, N-oxides thereof, non-toxic salts thereof, or pharmaceutical compositions comprising them, as active ingredients (wherein R1 is formula (II) or formula