- 4,5-DIHYDRO-OXAZOL-2-YL AMINE DERIVATIVES
-
The present invention relates to a compounds of formula I wherein R1, R1′, R2, R3, R4, X, Ar, and m are as defined in the specification and claims and pharmaceutically active acid addition salts thereof. Compounds of the invention have Asp2 (β-secretase, BACE 1 or Memapsin-2) inhibitory activity and are useful for the treatment of diseases characterized by elevated β-amyloid levels or β-amyloid deposits, particularly Alzheimer's disease.
- -
-
Page/Page column 34
(2009/09/05)
-
- Thrombopoietin Receptor Agonists
-
A compound of the formula (I) useful as promoters of thrombopoiesis and megakaryocytopoiesis, wherein A, B, D, E, W, X, Y, Z, R1 and R2 are defined as above.
- -
-
Page/Page column 18
(2010/11/30)
-
- NEW DISUBSTITUTED PHENYLPIPERIDINES/PIPERAZINES AS MODULATORS OF DOPAMINE NEUROTRANSMISSION
-
The present invention relates to compounds which have therapeutic effects against disorders in the central nervous system, and in particular new 4-(ortho, meta-disubstituted phenyl)-1-alkypiperidines and piperazines. (I) wherein R1, R2, R3 and Y are as de
- -
-
Page/Page column 65
(2008/06/13)
-
- 2-Alkynyl-and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists
-
Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is R1, R2, R3, R4 and R5 are H, alkyl or alkoxyalkyl; R6 is H, alkyl, hydroxyalkyl or —CH2F; R7, R8 and R9 are H, alkyl, alkoxy, alkylthio, alkoxyalkyl, halo or —CF3; and Z is optionally substituted aryl, heteroaryl or heteroaryl-alkyl are disclosed. Also disclosed is the use of compounds of formula I in the treatment of central nervous system diseases, in particular Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them.
- -
-
-
- Lithiations directed by carboxylic acid, fluorine and chlorine: The regioselective synthesis of polysubstituted benzoic acids and acetophenones
-
Lithiation/electrophilic quenching of ortho-lithiated benzoates allows the totally regiocontrolled synthesis of a wide range of 2,3-, 2,3,4-, and 2,3,4,5-polysubstituted benzoic acids and related acetophenones. Elsevier,.
- Moyroud, Joel,Guesnet, Jean-Luc,Bennetau, Bernard,Mortier, Jacques
-
p. 133 - 141
(2007/10/03)
-
- Regiospecific Synthesis of Mixed 2,3-Dihalobenzoic Acids and Related Acetophenones via Ortho-Metalation Reactions
-
Concise general routes to mixed 2,3-dihalobenzoic acids and related acetophenones-based on directed ortho-metalation and ipso-desilylation reactions are described.
- Moyroud, Joel,Guesnet, Jean-Luc,Bennetau, Bernard,Mortier, Jacques
-
p. 881 - 884
(2007/10/02)
-