84983-97-1Relevant articles and documents
COMPOUNDS HAVING ACTIVITY AT NK3 RECEPTOR AND USES THEREOF IN MEDICINE
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Page/Page column 19, (2010/11/30)
The present invention relates to compounds of formula (I), a pharmaceutically acceptable salt or solvate thereof: wherein n, m and p, which may be the same or different, are either 0 or 1. Also disclosed are processes for their preparation, pharmaceutical compositions containing them and their use as medicaments particularly in treating disorders of the central nervous system (CNS).
COMPOUNDS HAVING ACTIVITY AT NK3 RECEPTOR AND USES THEREOF IN MEDICINE
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Page/Page column 28, (2010/11/30)
The invention also relates to compounds of formula (I), a pharmaceutically acceptable salt, solvate or prodrug thereof: wherein R1 is phenyl or cyclohexyl, either of which is optionally substituted by 1, 2 or 3 halogen atoms, which atoms may be the same or different; R2 is C1-6alkyl or C3-6cycloalkyl; n is 1 or 2; R3 is hydrogen, C1-6alkyl or C3-6cycloalkyl; X is -(C=O)- or -SO2-; R4 is C1-6alkyl, C1-6haloalkyl, C1-6alkoxy, C1-6alkoxyC1-6alkyl, C1-6haloalkoxy, amino, monoC1-6alkylamino or diC1-6alkylamino, or R4 is heterocyclyl or carbocyclyl, either of which is optionally substituted independently by one or more halogen, C1-6alkyl, C1-6haloalkyl, C1-6alkoxy or C1-6haloalkoxy; R5 is phenyl or thienyl, either of which is optionally substituted by 1, 2 or 3 halogen atoms; and y is 0, 1 or 2; wherein when y is 1 or 2, Y is a halogen atom, and wherein when y is 2 the halogen atoms may be the same or different. Also disclosed are use of the compounds in treating diseases and conditions mediated by activation of the NK3 receptor, compositions containing the derivatives and processes for their preparation.
COMPOUNDS HAVING ACTIVITY AT NK3 RECEPTOR AND USES THEREOF IN MEDICINE
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Page/Page column 31-32, (2010/11/30)
The present invention relates to compounds of formula (I), a pharmaceutically acceptable salt, solvate or prodrug thereof: wherein R1 is phenyl optionally substituted by 1, 2 or 3 halogen atoms which halogen atoms may be the same or different; R2 is C1-6alkyl, C3-6cycloalkyl or acetyl; X is oxygen or sulphur; a is 1, 2 or 3; b is 0 or 1; c is 0, 1 or 2; R3 is hydrogen or C1-6alkyl; R4 is hydrogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxyC1-6alkyl, C3-6cycloalkyl or C3-6cycloalkylC1-6alkyl; R5 is hydrogen; or R5 and R3, together with the nterconnecting atoms, form a 4, 5 or 6 membered ring; R6 is phenyl or thienyl, either of which is optionally substituted by 1, 2 or 3 halogen atoms, which atoms may be the same or different; and z is 0, 1 or 2; wherein when z is 1 or 2, Z is a halogen atom, and wherein when z is 2 the halogen atoms may be the same or different. Also disclosed are processes for their preparation, pharmaceutical compositions containing them and heir use as medicaments particularly in treating disorders of the Central Nervous System (CNS).
QUINOLINE 4-CARBOXAMIDE DERIVATIVES AND THEIR USE AS NEUROKININ 3 (NK-3) RECEPTOR ANTAGONISTS
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Page/Page column 15-16, (2010/02/10)
The invention relates to novel quinoline derivatives, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments particularly in treating disorders of the central nervous system (CNS).
Synthesis of (S)- and (R)-1-(2-furyl)alkylamines and (S)- and (R)-α- amino acids through the addition of organometallic reagents to imines derived from (S)-Valinol
Alvaro, Giuseppe,Martelli, Gianluca,Savoia, Diego,Zoffoli, Andrea
, p. 1773 - 1777 (2007/10/03)
(S)-1-(2-Furyl)alkylamines were prepared through the addition of organometallic reagents to the imine derived from 2-furaldehyde and (S)- valinol, previous protection of the auxiliary hydroxy group as trimethylsilyl ether, followed by removal of the auxiliary. Then, protection of the primary amine as tosylamide or benzamide and oxidation of the furan ring gave the N- derivatives of (S)-α-amino acids. (R)-N-Benzoylphenylglycine was prepared from the benzaldimine, where the hydroxy group was protected as the tert- butyldimethylsilyl ether, through addition of 2-furyllithium.
Factors influencing the stereoselectivity in the cycloaddition of imino-dienophiles derived from amino ethers, amino alcohols, and amino acid esters
Devine,Reilly,Oh
, p. 5827 - 5830 (2007/10/02)
Imino dienophiles derived from amino ethers, amino alcohols and amino esters undergo Lewis acid promoted cycloaddition with Danishefsky's diene. Cyclic chelation between the imine and oxygen atom increases the stereoselectivity of the reaction.
Asymmetric Induction Reactions. I. Asymmetric Sigmatropic Rearrangements of Sulfur Ylides Derived from Chiral Ketenimines and Trimethylsulfonium Ylide
Hiroi, Kunio,Sato, Shuko
, p. 2331 - 2338 (2007/10/02)
The asymmetric (2,3) sigmatropic rearrangements of 2-alkylamino-3-phenyl-2-pentenyl-methylsulfonium methylides were accomplished by the reaction of ethylphenylketenimines 3 having a chiral carbon next to the nitrogen atom with trimethylsulfonium ylide, and acidic hydrolysis of the imines 4 thus obtained led to optically active 3-methylthiomethyl-3-phenyl-2-pentanone (5).The reaction of ethylphenylketene (-)-menthylimine (3g) with trimethylsulfonium ylide at -78 deg C resulted in the highest optical yield of (R)-(-)-5 in the above sequence.Keywords--asymmetric induction; (2,3) sigmatropic rearrangement; chiral ketenimine; sulfur ylide; trimethylsulfonium ylide
