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US 2011/0086864 A1Published application
N-hydroxyamide derivatives and use thereof
AssigneeMerck Serono SA
InventorsDominique Swinnen, Jerome Gonzalez
Life of this patent
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Abstract
The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.
Claims17
An N-hydroxyamide derivative according to Formula (I),
- wherein:
- A is selected from —C(B)— and N;
- B is H or B forms a bond with either R5 or R7;
- R1 is heteroaryl optionally substituted with 1 to 5 substituents independently selected from C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, cycloalkyl, heterocycloalkyl, aryl C1-C6-alkyl, heteroaryl C1-C6-alkyl, cycloalkyl C1-C6-alkyl, heterocycloalkyl C1-C6-alkyl, amino, acyl, acyloxy, acylamino, aminocarbonyl, alkoxycarbonyl, ureido, aryl, carbamate, heteroaryl, sulfinyl, sulfonyl, alkoxy, sulfanyl, halogen, carboxy, trihalomethyl, cyano, hydroxy, mercapto and nitro;
- R2 is H;
- R3 is selected from H, C1-C6 alkyl, C2-C6 alkenyl and C2-C6 alkynyl;
- R4, R5, R6 and R7 are independently selected from H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl;
- or R4 and R7 form together a —CH2— linkage;
- or an enantiomer, diastereomer, racemate, or a pharmaceutically acceptable salt thereof.
6 more elements
A process for the manufacture of a compound of Formula I:
- said process comprising the step of reacting a compound of Formula (IV):
- with a hydroxylamine, H2NO—R8, and thereby forming the compound according to Formula I;
- wherein
- A is selected from —C(B)— and N;
- B is H or B forms a bond with either R5 or R7;
- R1 is heteroaryl optionally substituted with 1 to 5 substituents independently selected from C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, cycloalkyl, heterocycloalkyl, aryl C1-C6-alkyl, heteroaryl C1-C6-alkyl, cycloalkyl C1-C6-alkyl, heterocycloalkyl C1-C6-alkyl, amino, acyl, acyloxy, acylamino, aminocarbonyl, alkoxycarbonyl, ureido, aryl, carbamate, heteroaryl, sulfinyl, sulfonyl, alkoxy, sulfanyl, halogen, carboxy, trihalomethyl, cyano, hydroxy, mercapto and nitro;
- R2 is H;
- R3 is selected from H, C1-C6 alkyl, C2-C6 alkenyl and C2-C6 alkynyl;
- R4, R5, R6 and R7 are independently selected from H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl;
- or R4 and R7 form together a —CH2— linkage;
- and
- R8 is selected from H, t-butyl, benzyl, trialkylsilyl and tetrahydropyranyl.
9 more elements
A compound according to Formula (IV):
- wherein
- A is selected from —C(B)— and N;
- B is H or B forms a bond with either R5 or R7;
- R1 is heteroaryl optionally substituted with 1 to 5 substituents independently selected from C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, cycloalkyl, heterocycloalkyl, aryl C1-C6-alkyl, heteroaryl C1-C6-alkyl, cycloalkyl heterocycloalkyl C1-C6-alkyl, amino, acyl, acyloxy, acylamino, aminocarbonyl, alkoxycarbonyl, ureido, aryl, carbamate, heteroaryl, sulfinyl, sulfonyl, alkoxy, sulfanyl, halogen, carboxy, trihalomethyl, cyano, hydroxy, mercapto and nitro;
- R2 is H;
- R3 is selected from H, C1-C6 alkyl, C2-C6 alkenyl and C2-C6 alkynyl;
- and
- R4, R5, R6 and R7 are independently selected from H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl;
- or R4 and R7 form together a —CH2— linkage;
- or a pharmaceutically acceptable salt thereof.
7 more elements
Dependencies are inferred from the claim text.