145943-75-5

Usage

Derivative of

Piperazine and propanol

Pharmacological properties

Serotonin receptor agonist

Potential use

Ingredient in pharmaceutical formulations

Industry interest

Pharmaceutical and chemical industries

Upstream product

• 69414-53-5 1-(piperazin-1-yl)ethanone hydrochloride 
• 627-30-5 1-chloro-3-hydroxypropane 
• 13889-98-0 N-acetylpiperidine 
• 627-18-9 1-bromo-3-propanol 

Downstream Products

• 393785-31-4 3-(-4-acetylpiperazino)propyl 4-nitrophenylcarbonate 
• 1240299-99-3 benzyl 4-[4-[3-(4-acetylpiperazin-1-yl)propoxy]phenyl]-5,6-dihydropyridine-1(2H)-carboxylate 
• 1240299-34-6 6-(4-{4-[2-(4-acetylpiperazin-1-yl)ethoxy]phenyl}piperidin-1-yl)-3-(trifluoromethyl)-7,8-dihydro[1,2,4]triazolo[4,3-b]pyridazine napadisylate 
• 1240299-37-9 6-(4-{4-[2-(4-acetylpiperazin-1-yl)ethoxy]phenyl}piperidin-1-yl)-3-(trifluoromethyl)-7,8-dihydro[1,2,4]triazolo[4,3-b]pyridazine fumarate 
• 1240299-36-8 6-(4-{4-[2-(4-acetylpiperazin-1-yl)ethoxy]phenyl}piperidin-1-yl)-3-(trifluoromethyl)-7,8-dihydro[1,2,4]triazolo[4,3-b]pyridazine maleate 
• 1240299-31-3 6-[4-[4-[3-(4-acetylpiperazin-1-yl)propoxy]phenyl]piperidin-1-yl]-3-(trifluoromethyl)-7,8-dihydro[1,2,4]triazolo[4,3-b]pyridazine 
• 1166819-39-1 6-[4-[4-[3-(4-acetylpiperazin-1-yl)propoxy]phenyl]piperidin-1-yl]-3-(trifluoromethyl)[1,2,4]triazolo[4,3-b]pyridazine 
• 1240299-33-5 1-(4-(2-(4-(1-(3-(trifluoromethyl)-7,8-dihydro-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl)phenoxy)ethyl)piperazin-1-yl)ethanone 
• 1240300-00-8 4-[4-[3-(4-acetylpiperazin-1-yl)propoxy]phenyl]piperidine 

Relevant academic research and scientific papers

KRAS G12C INHIBITORS

The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.

KRAS G12C INHIBITORS

The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.

NEW ACETYL COENZYME A CARBOXYLASE (ACC) INHIBITORS AND USES IN TREATMENTS OF OBESITY AND DIABETES MELLITUS - 087

The present invention relates to Acetyl Coenzyme A Carboxylase (ACC) inhibitors according to formula (I), or an enantiomer thereof, or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, E, L, Z and n are as defined herein, to processes for preparing such compounds, to pharmaceutical compositions containing them, to the use of such inhibitors and to methods for th eir therapeutic use, particularly in the treatments of obesity and diabetes mellitus.

Cinnoline compounds

The invention relatest to compounds of the formula (I) wherein either any one of G1, G2, G3, G4 and G5 is nitrogen and the other four are —CH—, or G1, G2, G3, G4 and G5 are all —CH—; Z is —O—, —NH—, —S—, —CH2— or a direct bond; Z is linked to any one of G1, G2, G3 and G4 which is a free carbon atom; n is an integer from 0 to 5; any of the substitutents R1 may be attached at any free carbon atom of the indole, azaindole or indazole group; m is an integer from 0 to 3; Ra represents hydrogen; Rb represents hydrogen or another value as defined herein; R1 represents hydrogen, oxo, hydroxy, halogeno, C1-4alkyl, C1-4alkoxy, C1-4alkoxy, C1-4-alkyl, aminoC1-4alkyl, C1-3alkylaminoC1-4alkyl, di(C1-3alkyl)aminoC1-4alkyl, —C1-5alkyl(ring B) wherein ring B is selected from azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, N-methylpiperazinly, N-ethylpiperazinyl, morpholino and thiomorpholino; R2 represents hydrogen, hydroxy, halogeno, cyano, nitro, trifluoromethyl, C1-3alkyl, C1-3alkoxy, C1-3aklylsulphanyl, —NR3R4 (wherein R3 and R4, which may be the same or different, each represents hydrogen or C1-3alkyl), or R5X1— (wherein R5 and X1 are as defined herein) and salts thereof, processes for the preparation of such compounds, pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof as active ingredient and the use of a compound of formula I in the manufacture of medicament for the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals. The compounds of formula I and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.

8-CHLORO AND 8-METHYLTHIO DERIVATIVES OF 10-PIPERAZINO-10,11-DIHYDRODIBENZOTHIEPINS; NEW COMPOUNDS AND NEW PROCEDURES

The resolution of racemic clorothepin (Ia) was repeated and the water-soluble methanesulfonates of (S)(+)-clorothepin and (R)(-)-clorothepin were prepared which were used in recent studies of the stereoselectivity of action of this neuroleptic agent.Alkylation of the secondary amine VIa with 2-chloroethyl decanoate resulted in noroxyclothepin decanoate IVa whose basically catalyzed ethanolysis afforded smoothly the amino alcohol IIa.Reactions of amines VIa and VIb with 1,2-butene oxide gave the amino alcohols VIIab.Alkylation of the amine VIa with 5-bromopentan-2-oneand the following reduction of the amino ketone IXa formed gave the amino alcohol VIIIa.Amino alcohols IIa and IIIb were transformed by treatment with thionyl chloride to the chloroalkylamines Xa and XIb which were used for the synthesis of mandelates XIIa, XIIIb and benzilates XIVa, XVb derived from noroxyclothepin IIa and oxyprothepin IIIb.A substitution reaction of 2,11-dichloro-10,11-dihydrodibenzothiepin with 1,4-diazabicyclononane led to the clorothepin analogue XVI.From 2-chlorodibenzothiepin-10(11 H)-one XVII via the 11-bromo derivative XVIII the amino ketone XIX was prepared.While its reduction with sodium borohydride gave the cis-amino alcohol XXI, the reduction with diborane gave the trans-amino alcohol XXII.The pharmacological properties of the new piperazine derivatives are described; some of them showed a high degree of neuroleptic activity of various profile.