Hydrazide derivatives as prostaglandin receptors modulators
AssigneeApplied Research Systems ARS Holding N.V.
InventorsGian Araldi, Yihua Liao, Nadia Brugger
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Abstract
The present invention relates to hydrazide derivatives of Formula I notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such hydrazide derivatives. Said hydrazide derivatives are useful in the treatment of preterm labor, dysmenorrhea, fertility disorders, asthma, hypertension, undesired blood clotting, preelampsia, eclampsia, an eosinophil disorder, undesired bone loss, renal dysfunction, an immune deficiency disorder, ichthyosis, elevated intraocular pressure, infertility, sexual dysfunction, gastric ulcers and inflammatory disorders.
Claims38
A hydrazide derivative of Formula (I):
- as well as its geometrical isomers, its optically active forms as enantiomers, diastereomers and mixtures of these, as well as salts thereof, wherein:
- A is selected from the group consisting of C3-C8 cycloalkyl, heterocycloalkyl, aryl and heteroaryl;
- B is selected from the group consisting of C1-C6 alkylene, C2-C6 alkenylene, and C2-C6 alkynylene;
- R1 is selected from the group consisting of H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C8 cycloalkyl, heterocycloalkyl, aryl C1-C6 alkyl, heteroaryl C1-C6 alkyl, aryl and heteroaryl;
- R2 and R3 are independently selected from the grou, consisting of H, C1-C6 alkyl, C2-C6 alkenyl and C2-C6 alkynyl;
- R4 is selected-from the group consisting of hydrogen and C1-C6 alkyl;
- R5 is selected from the group consisting of hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 heteroalkyl, C3-C8 cycloalkyl, C3-C8 cycloalkyl C1-C6 alkyl, aryl C1-C6 alkyl, heteroaryl C1-C6 alkyl, aryl and heteroaryl;
- and
- n is an integer selected from the group consisting of 1, 2, 3, 4, 5 and 6.
A hydrazide derivative selected from the group consisting of:
- 4-{2-[1-acetyl-2-(3-hydroxyoctyl)hydrazino]ethyl}benzoic acid;
- 4-{2-[1-acetyl-2-(3-hydroxyoctyl)-2-methylhydrazino]ethyl}benzoic acid;
- 4-{2-[1-acetyl-2-(3-hydroxybutyl)hydrazino]ethyl}benzoic acid;
- and
- a pharmaceutically acceptable salt of any of said compounds.
(canceled)
A compound of Formula II:
- as well as its geometrical isomers, its optically active forms as enantiomers, diastereomers and mixtures of these, as well as salts thereof, wherein A, R1, R2, R3 and n are as defined above.
A compound of Formula IV:
- as well as its geometrical isomers, its optically active forms as enantiomers, diastereomers and mixtures of these, as well as salts thereof, wherein A, R1, R2, R3, R5 and n are as defined above.
Dependencies are inferred from the claim text.