157695-16-4

Upstream product

• 619-58-9 4-iodobenzoic acid 
• 118493-85-9 acetamide oxime 
• 51934-41-9 4-iodobenzoic acid ethyl ester 
• 118493-85-9 N-hydroxyacetamidine 
• 22059-22-9 N-hydroxyacetamidine 
• 1711-02-0 4-iodobenzoic acid chloride 

Downstream Products

• 157694-99-0 3-[4-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl)-quinuclidin-3-ol 

Relevant academic research and scientific papers

PIPERAZINYLPHENALKYL LACTAM/AMINE LIGANDS FOR THE 5HT1B RECEPTOR

The present invention relates to novel derivatives, that are compounds of Formula (I), wherein R1, R2, R3, R14, X, Y, n and m are defined herein, their pharmaceutically acceptable salts, pharmaceutical compositions and methods using said compounds in treating or preventing depression, anxiety, obsessive compulsive disorder (OCD) and other disorders for which selective antagonists, inverse agonists and partial agonists of serotonin 1 (5-HT1) receptors, specifically, antagonists of 5-HT1B are useful.

HETEROARYL SUBSTITUTED BIPHENYL DERIVATIVES AS P38 KINASE INHIBITORS

Compounds of formula (I) are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.

QUINUCLIDINE DERIVATIVES AS SQUALENE SYNTHASE INHIBITORS

Compounds of formula (I) in which R is hydrogen or hydroxy; R is hydrogen; or R and R are joined together so that CR-CR is a double bond; Ar is a phenylene moiety and Ar is a heterocyclic moiety; or Ar is a heterocyclic moiety and Ar is a phenyl moiety; and wherein one or both of Ar and Ar may optionally bear one or more substituents independently selected from halogeno, hydroxy, amino, nitro, cyano, carboxy, carbamoyl, (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, (1-6C)alkoxy, (1-6C)alkylamino, di-[(1-6C)alkyl]amino N-(1-6C)alkylcarbamoyl, di-N,N-[(1-6C)alkyl]carbamoyl, (1-6C)alkoxycarbonyl, (1-6C)alkylthio, (1-6C)alkylsulphinyl, (1-6C)alkylsulphonyl, halogeno (1-6C)alkyl, (1-6C)alkanoylamino, ureido, N'-(1-6C)alkylureido, (1-6C)alkanoyl and oxime derivatives thereof and O-(1-6C)alkyl ethers of said oxime derivatives; provided that Ar is not a 6-membered heteroaryl moiety containing one or two nitrogen atoms; when Ar and Ar are both hydrogen, Ar is not an oxadiazole moiety; and their pharmaceutically acceptable salts are inhibitors of squalene synthase and hence useful in treating medical conditions in which a lowering of cholesterol is beneficial. Processes preparing these derivatives, pharmaceutical compositions containing them are also described together with their use in medicine.

Quinuclidine derivatives as squalene synthase inhibitors

Compounds of formula (I) and their pharmaceutically acceptable salts in which R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 are joined together so that CR1 -CR2 is a double bond; X is selected from --CH2 CH2 --, --CH=CH--, --C C--, --CH2 O--, --CH2 NH--, --NHCH2 --, --CH2 CO--, --COCH2 --, --CH2 S-- and --SCH2 --; Ar1 is a phenylene moiety; Ar2 is a heteroaryl moiety; and wherein one or both of Ar1 and Ar2 may optionally bear one or more substituents independently selected from halogeno, hydroxy, amino, nitro, cyano, carboxy, carbamoyl, alkyl, alkenyl, alkynyl, alkoxy, alkylamino, di-alkylamino, N-alkylcarbamoyl, di-N,N-alkylcarbamoyl, alkoxycarbonyl, alkylthio, alkylsulphinyl, alkylsulphonyl, halogeno-alkyl, carboxyalkyl and alkanoylamino; provided that when R1 is hydroxy, X is not selected from --NHCH2 -- and --SCH2 --; are inhibitors of squalene synthase and hence useful in treating medical conditions in which a lowering of cholesterol is beneficial, such as hypercholesterolemia and atherosclerosis. Processes for preparing these derivatives, pharmaceutical compositions containing them are also described together with their use in medicine.

Quinclidine derivatives as squalene synthase inhibitors

Quinuclidine derivatives of formula, and their pharmaceutically acceptable salts, in which: R1 is hydrogen or hydroxy; R2 is hydrogen; pr R1 and R2 are joined together so that CR1 -CR2 is a