2-amino-thiazole derivatives, process for their preparation, and their use as antitumor agents

• US 7,037,929 B1
• Filed: 10/27/1999
• Issued: 05/02/2006
• Est. Priority Date: 10/30/1998
• Status: Expired due to Fees

• Current Assignee: Nerviano Medical Sciences SRL (NMS Group SpA)
• Original Assignee: Pharmacia & Upjohn LLC (Pfizer Inc.)
• Inventors: Pevarello, Paolo, Traquandi, Gabriella, Isacchi, Antonella, Vulpetti, Anna, Amici, Raffaella, Villa, Manuela
• Primary Examiner(s): SHAMEEM, GOLAM M
• Application Number:
  US09/807,962
• Time in Patent Office: 2,379 Days
• Field of Search: 548/195, 514/371, 514/252.1, 514/235.5, 544/133, 544/238
• US Class Current: 514/371
• CPC Class Codes: A61K 31/426 1,3-Thiazoles
• CPC Class Codes: A61K 31/427 not condensed and containing further heterocyclic rings
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 13/12 of the kidneys
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 17/16 Emollients or protectives, e.g. against radiation
• CPC Class Codes: A61P 19/02 for joint disorders, e.g. arthritis, arthrosis
• CPC Class Codes: A61P 25/28 for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• CPC Class Codes: A61P 31/12 Antivirals
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 37/00 Drugs for immunological or allergic disorders
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 9/10 for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• CPC Class Codes: C07D 277/46 by carboxylic acids, or sulfur or nitrogen analogues thereof
• CPC Class Codes: C07D 417/12 linked by a chain containing hetero atoms as chain links

Abstract

Compounds which are 2-amino-1,3-thiazole derivatives of formula (I)
wherein R is a halogen atom, a nitro group, an optionally substituted amino group or it is a group, optionally further substituted, selected from i) straight or branched C₁–C₈ alkyl, C₂–C₆ alkenyl or C₂–C₆ alkynyl; ii) C₃–C₆ cycloalkyl; iii) aryl or arylalkyl with from 1 to 8 carbon atoms within the straight or branched alkyl chain; R₁ is an optionally further substituted group selected from: i) straight or branched C₁–C₈ alkyl or C₂–C₆ alkenyl; ii) 3 to 6 membered carbocycle or 5 to 7 membered heterocycle ring; iii) aryl or arylcarbonyl; iv) arylalkyl with from 1 to 8 carbon atoms within the straight or branched alkyl chain; v) arylalkenyl with from 2 to 6 carbon atoms within the straight or branched alkenyl chain; vi) an optionally protected amino acid residue; or a pharmaceutically acceptable salt thereof; are useful for treating cell proliferative disorders associated with an altered cell dependent kinase activity.

Claims

1. A compound which is a 2-amino-1,3-thiazole derivative of formula (I)

wherein R is isopropyl;

R₁ is an optionally further substituted group selected from;

i) straight or branched C₁–

C₈ alkyl or C₂–

C₆ alkenyl;

ii) 3 to 6 membered carbocycle or 5 to 7 membered heterocycle ring;

iii) aryl or arylcarbonyl;

iv) arylalkyl with from 1 to 8 carbon atoms within the straight or branched alkyl chain;

v) arylalkenyl with from 2 to 6 carbon atoms within the straight or branched alkenyl chain;

vi) an optionally protected amino acid residue;

or a pharmaceutically acceptable salt thereof.

2. A compound of formula (I), according to claim 1, wherein R₁ is an optionally substituted group selected from straight or branched C₁–

C₄ alkyl or alkenyl, aryl or arylalkyl with from 1 to 4 carbon atoms within the alkyl chain or it is an optionally protected amino acid residue.

3. A process for producing a compound of formula (I), as defined in claim 1, which process comprises reacting a compound of formula (II)

with a compound of formula (III)

R₁—

COX 

 

(III)

wherein R and R₁ are as defined in claim 1 and X is hydroxy or a suitable leaving group; and

, if desired, converting a 2-amino-1,3-thiazole derivative of formula (I) into another such derivative of formula (I), and/or into a salt thereof.

4. A process according to claim 3 wherein X is hydroxy, bromine or chlorine.

5. A pharmaceutical composition comprising one or more pharmaceutically acceptable carriers and/or diluents and, as the active principle, an effective amount of a compound of formula (I) as defined in claim 1.

6. A compound of formula (I) according to claim 1, whenever appropriate in the form of a pharmaceutically acceptable salt, selected from the group consisting of:

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(3-hydroxyphenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(3-methoxyphenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(3-chlorophenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(4-hydroxyphenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(3,4-dihydroxyphenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(4-hydroxy-3-methoxyphenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(4-methoxyphenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(4-chlorophenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-phenyl-acetamide;

N-(5-isopropyl-thiazol-2-yl)-4-sulfamoyl-benzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-butanamide;

2-[3-(3-chloropropoxy)phenyl]-N-(5-isopropyl-1,3-thiazol-2-yl)acetamide;

2-[3-(2-chloroethoxy)phenyl]-N-(5-isopropyl-1,3-thiazol-2-yl)acetamide;

2-(4-aminophenyl)-N-(5-isopropyl-1,3-thiazol-2-yl)acetamide;

4-amino-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

2-(2-amino-1,3-thiazol-4-yl)-N-(5-isopropyl-1,3-thiazol-2-yl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-{3-[3-(4-morpholinyl)propoxy]phenyl} acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-{3-[3-(4-morpholinyl)ethoxy]phenyl}acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(3-[3-(1-pirrolidinyl)propoxy]phenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-{3-[3-(4-methyl-1-piperazinyl)propoxy]phenyl}acetamide;

2-{3-[2-(dimethylamino)ethoxy]phenyl}-N-(5-isopropyl-1,3-thiazol-2-yl)acetamide;

2-{3-[3-(dimethylamino)propoxy]phenyl}-N-(5-isopropyl-1,3-thiazol-2-yl)acetamide;

N-(5-isopropyl-1,3-thiazol-2.-yl)-2-[3-(2-methoxyethoxy)phenyl]acetamide;

3-chloro-N-(5-isopropyl-1,3-thiazol-2-yl)-4-(4-methyl-piperazinyl)bezamide;

2-anilino-N-(5-isopropyl-1,3-thiazol-2-yl)acetamide;

(R)-N-(5-isopropyl-1,3-thiazol-2-yl)-2-phenylpropanamide;

(S)-N-(5-isopropyl-1,3-thiazol-2-yl)-2-phenylpropanamide;

N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

2,5-dichloro-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

3,5-dichloro-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

3,4-dichloro-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

2,4-dichloro-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

2,3-dichloro-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

3-iodio-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

2-iodio-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

4-iodio-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

3-bromo-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

4-chloro-2-fluoro-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

5-bromo-2-chloro-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

3-chloro-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

2-chloro-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

4-chloro-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

3-fluoro-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

2-fluoro-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

4-fluoro-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

2,4-difluoro-N-(5-isopropyl-1,3-triazol-2-yl)benzamide;

3,4-difluoro-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

2,3,4,5,6-pentafluoro-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-4-methyl-3-nitrobenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-5-methyl-2-nitrobenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-3-methyl-2-nitrobenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-3,5-dimethyl-4-nitrobenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-4-methoxy-2-nitrobenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-3-methoxy-2-nitrobenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-4-methoxy-3-nitrobenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-3-methoxy-4-nitrobenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-3,5-dinitrobenzamide;

5-{[(5-isopropyl-1,3-thiazol-2-yl)amino]carbonyl}-2-nitrophenyl octanoate;

N-(5-isopropyl-1,3-thiazol-2-yl)-3-nitrobenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-nitrobenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-4-nitrobenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-4-(methylsulfonyl)-3-nitrobepzamide;

4-chloro-N-(5-isopropyl-1,3-thiazol-2-yl)-3-nitrobenzamide;

6-chloro-N-(5-isopropyl-1,3-thiazol-2-yl)-3-nitrobenzamide;

4-chloro-N-(5-isopropyl-1,3-thiazol-2-yl)-2-nitrobenzamide;

2-chloro-N-(5-isopropyl-1,3-thiazol-2-yl)-4-nitrobenzamide;

5-chloro-N-(5-isopropyl-1,3-thiazol-2-yl)-2-nitrobenzamide;

2-bromo-N-(5-isopropyl-1,3-thiazol-2-yl)-5-nitrobenzamide;

4-fluoro-N-(5-isopropyl-1,3-thiazol-2-yl)-3-nitrobenzamide;

4-fluoro-N-(5-isopropyl-1,3-thiazol-2-yl)-2-nitrobenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-nitro-4-(trifluoromethyl)benzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-3,5-bis(trifluoromethyl)benzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2,6-bis(trifluoromethyl)benzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(trifluoromethyl)benzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-3-(trifluoromethyl)benzamide;

3-fluoro-N-(5-isopropyl-1,3-thiazol-2-yl)-4-(trifluoromethyl)benzamide;

2-fluoro-N-(5-isopropyl-1,3-thiazol-2-yl)-3-(trifluoromethyl)benzamide;

5-fluoro-N-(5-isopropyl-1,3-thiazol-2-yl)-3-(trifluoromethyl)benzamide;

2-fluoro-N-(5-isopropyl-1,3-thiazol-2-yl)-4-(trifluoromethyl)benzamide;

4-fluoro-N-(5-isopropyl-1,3-thiazol-2-yl)-3-(trifluoromethyl)benzamide;

methyl 4-([(5-isopropyl-1,3-thiazol-2-yl)amino]carbonyl}benzoate;

methyl 2-([(5-isopropyl-1,3-thiazol-2-yl)amino]carbonyl)benzoate;

4-cyano-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

3-cyano-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-3-methylbenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-methylbenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-4-methylbenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-4-vinylbenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-4-(2-phenylethynyl)benzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-3-methoxy-4-methylbenzamide;

2-benzyl-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-phenethylbenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-phenylbenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-4-phenylbenzamide;

4-(tert-butyl)-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-4-isopropylbenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-4-pentylbenzamide;

3-fluoro-N-(5-isopropyl-1,3-thiazol-2-yl)-4-methylbenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-3,4-dimethylbenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-3,5-dimethylbenzamide;

4-acetyl-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-4-(methylsulfonyl)benzamide;

5-(aminosulfonyl)-2,4-dichloro-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

5-(aminosulfonyl)-4-chloro-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

3-fluoro-N-(5-isopropyl-1,3-thiazol-2-yl)-4-methoxybenzamide;

3-chloro-N-(5-isopropyl-1,3-thiazol-2-yl)-4-methoxybenzamide;

5-chloro-N-(5-isopropyl-1,3-thiazol-2-yl)-2-methoxybenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-4-methoxybenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-3-methoxybenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-methoxybenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-3,4-dimethoxybenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-3,5-dimethoxybenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2,4-dimethoxybenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2,3-dimethoxybenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-3-phenoxybenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-phenoxybenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-4-phenoxybenzamide;

2-ethoxy-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

4-ethoxy-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-3,4,5-trimethoxybenzamide;

3,4-diethoxy-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

3,4,5-triethoxy-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-3-methoxy-4-(methoxymethoxy)benzamide;

4-butoxy-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-4-propoxybenzamide;

4-isopropoxy-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-1,3-benzodioxole-5-carboxamide;

4-(benzyloxy)-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

4-(2-cyclohexen-1-yloxy)-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-4(trifluoromethoxy)benzamide;

4-(difluoromethoxy)-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-4(methylsulfanyl)benzamide;

2-[(4-chlorophenyl)sulfinyl)-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-[(4-nitrophenyl)sulfinyl]benzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-4-[(4-methylphenyl)sulfonyl]-3-nitrobenzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-3 [(trifluoromethyl)sulfanyl]benzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-methoxy-4-(methylsulfanyl)benzamide;

2-[(2-cyanophenyl)sulfanyl]-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

N-1,N-1-diethyl-3,6-difluoro-N-2-(5-isopropyl-1,3-thiazol-2-yl)phthalamide;

4-formyl-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

2-formyl-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

4-{[(2,5-dimethoxyanilino)carbonyl]amino}-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

4-(hydroxymethyl)-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

4-{[(5-isopropyl-1,3-thiazol-2-yl)amino]carbonyl}-2-nitrobenzyl acetate;

4-{[(5-isopropyl-1,3-thiazol-2-yl)amino]carbonyl}-2-nitrobenzyl 4-(acetylamino)-3-iodobenzoate;

4-(acetylamino)-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-4-[(2-phenylacetyl)amino]benzamide;

4-(acetylamino)-3-iodo-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

4-amino-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

4-(dimethylamino)-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

3-(dimethylamino)-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

2-(methylamino)-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-[3-(trifluoromethyl)anilino]benzamide;

3-{[(5-bromo-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]amino}-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-4-(1H-pyrrol-1-yl)benzamide;

2,6-dichloro-N-(5-isopropyl-1,3-thiazol-2-yl)isonicotinamide;

2-(4-bromophenyl)-6-(4-iodophenyl)-N-(5-isopropyl-1,3-thiazol-2-yl)isonicotinamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-[3-(trifluoromethyl)anilino)nicotinamide;

2,6-dichloro-N-(5-isopropyl. 1,3-thiazol-2-yl)nicotinamide;

5,6-dichloro-N-(5-isopropyl-1,3-thiazol-2-yl)nicotinamide;

2-chloro-N-(5-isopropyl-1,3-thiazol-2-yl)-6-methylnicotinamide;

2,6-dichloro-5-fluoro-N-(5-isopropyl-1,3-thiazol-2-yl)nicotinamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-phenoxynicotinamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-6-(2,2,2-trifluoroethoxy)nicotinamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2,6-dimethoxynicotinamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-quinoxalinecarboxamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-5-methyl-2-pyrazinecarboxamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-8-quinolinecarboxamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-phenyl-4-quinolinecarboxamjde;

N-(5-isopropyl-1,3-thiazol-2-yl)-5-methyl-1-phenyl-1H-pyrazole-4-carboxamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-5-methyl-1H-pyrazole-3-carboxamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-1H-pyrazole-4-carboxamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-5-methyl-2-phenyl-2H-1,2,3-triazole-4-carboxamide;

2-[(2,1,3-benzoxadiazol-5-yloxy)methyl]-N-(5-isopropyl-1,3-thiazol-2-yl)-4-methyl-1,3-thiazole-5-carboxamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-9H-fluorene-1-carboxamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-7-methoxy-1-benzofrran2-carboxide;

N-(5-isopropyl-1,3-thiazol-2-yl)-1-[(4-methylphenyl)sulfonyl]-1H-pyrrole-3-carboxamide;

2-ethoxy-N-(5-isopropyl-1,3-thiazol-2-yl)-1-naphthamide;

4-fluoro-N-(5-isopropyl-1,3-thiazol-2-yl)-1-naphthamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-naphthamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-9,10-dioxo-9,10-dihydro-2-anthracenecarboxamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-9-oxo-9H-fluorene-4-carboxamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-9-oxo-9H-fluorene-1-carboxamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-8-oxo-5,6,7,8-tetrahydro-2-naphthalenecarboxarmde;

N-(5-isopropyl-1,3-thiazol-2-yl)-1,3-dioxo-1,3-dihydro-2-benzofuran-5-carboxamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-1H-indole-5-carboxamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-1H-indole-4-carboxamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-1-methyl-2-phenyl-1H-indole-5-carboxamide;

2-butyl-N-(5-isopropyl-1,3-thiazol-2-yl)-1-methyl-1H-indole-5-carboxamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-1H-indole-6-carboxamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-5-methoxy-1H-indole-2-carboxamide;

1-allyl-2-butyl-N-(5-isopropyl-1,3-thiazol-2-yl)-1H-indole-5-carboxamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-1-methyl-1H-indole-2-carboxamide;

1-benzyl-N-(5-isopropyl-1,3-thiazol-2-yl)-2-phenyl-1H-indole-5-carboxamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-1H-1,2,3-benzotriazole-5-carboxamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-3,5-dimethyl-4-isoxazo 1-carboxamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-3-thiophenecarboxamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-3-methyl-2-thiophenecarboxarmde;

N-(5-isopropyl-1,3-thiazol-2-yl)-5-methyl-2-thiophenecarboxamide;

5-bromo-N-(5-isopropyl-1,3-thiazol-2-yl)-2-thiophenecarboxamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-3-[(2,3,3-trichloroacryloyl)amino]-2-thiophenecarboxamide;

5-bromo-N-(5-isopropyl-1,3-thiazol-2-yl)-2-furamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-furamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-5-(4-nitrophenyl)-2-furamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-5-(2-nitrophenyl)-2-furamide;

5-(4-chlorophenyl)-N-(5-isopropyl-1,3-thiazol-2-yl)-2-furamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-5-[3-(trifluoromethyl)phenyly2ffiramide;

5-(4-chloro-2-nitrophenyl)-N-(5-isopropyl-1,3-thiazol-2-yl)-2-furamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-5-(4-methyl-2-nitrophenyl)-2-furamide;

5-[2-chloro-5-(trifluoromethyl)phenyl-N-(5-isopropyl-1,3-thiazol-2-yl)-2-furamide;

tert-butyl (1R)-2-[(5-isopropyl-1,3-thiazol-2-yl)amino]-2-oxo-1-phenylethylcarbamate;

(1R)-2-[(5-isopropyl-1,3-thiazol-2-yl)amino]-2-oxo-1-phenylethyl acetate;

(1S)-2-[(5-isopropyl-1,3-thiazol-2-yl)amino]-2-oxo-1-phenylethyl acetate;

(R,S)-2-fluoro-N-(5-isopropyl-1,3-thiazol-2-yl)-2-phenylacetamide;

(R)-2-fluoro-N-(5-isopropyl-1,3-thiazol-2-yl)-2-phenylacetamide;

(S)-2-fluoro-N-(5-isopropyl-1,3-thiazol-2-yl)-2-phenylacetamide;

2-(acetylamino)-N-(5-isopropyl-1,3-thiazol-2-yl)-2-phenylacetamide;

(R,S)-2-(methoxy)-N-(5-isopropyl-1,3-thiazol-2-yl)-2-phenylacetamide;

(R)-2-(methoxy)-N-(5-isopropyl-1,3-thiazol-2-yl)-2-phenylacetamide;

(S)-2-(methoxy)-N-(5-isopropyl-1,3-thiazo]-2-yl)-2-phenylacetamide;

3,3,3-trifluoro-N-(5-isopropyl-1,3-thiazol-2-yl)-2-methoxy-2-phenylpropanamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(1-naphthyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(2-naphthyl)acetamide;

2-(1H-indol-3-yl)-N-(5-isopropyl-1,3-thiazol-2-yl)acetamide;

2-(1,3-benzodioxol-4-yl)-N-(5-isopropyl-1,3-thiazol-2-yl)acetamide;

2-(2,4-dinitrophenyl)-N-(5-isopropyl-1,3-thiazol-2-yl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(2-methyl-1H-indol-3-yl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(1-methyl-1H-indol-3-yl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(5-methoxy-1H-indol-3-yl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(5-benzyloxy-1H-indol-3-yl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(3-methoxy-2-methyl-1H-indol-3-yl)acetamide;

2-(1H-indol-3-yl)-N-(5-isopropyl-1,3-thiazol-2-yl)-0.2-oxoacetamide;

2-(5-bromo-1H-indol-3-yl)-N-(5-isopropyl-1,3-thiazol-2-yl)acetamide;

2-(5-fluoro-1H-indol-3-yl)-N-(5-isopropyl-1,3-thiazol-2-yl)acetamide;

2-[1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]-N-(5-isopropyl-1,3-thiazol-2-yl)acetamide;

3-(1H-indol-3-yl)-N-(5-isopropyl-1,3-thiazol-2-yl)propanamide;

4-(1H-indol-3-yl)-N-(5-isopropyl-1,3-thiazol-2-yl)butanamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-3-(2-thienyl)propanamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(2-thienyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-oxo-2-(2-thienyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(3-thienyl)acetamide;

2-(5-chloro-1-benzothiophen-3-yl)-N-(5-isopropyl-1,3-thiazol-2-yl)acetamide;

2-(1-benzothiophen-3-yl)-N-(5-isopropyl-1,3-thiazol-2-yl)acetamide;

2-[2-(formylamino)-1,3-thiazol-4-yl]-N-(5-isopropyl-1,3-thiazol-2-yl)-2-(methoxyimino)acetamide;

2-{2-[(2-chloroacetyl)amino]-1,3-thiazol-4-yl}-N-(5-isopropyl-1,3-thiazol-2-yl)-2-(methoxyimino)acetamide;

2-chloro-N-(4-(2-[(5-isopropyl-1,3-thiazol-2-yl)amino]-2-oxoethyl}-1,3-thiazol-2-287.ethyl-2-({[2-[(5-isopropyl-1,3-thiazol-2-yl)amino]-2-oxo-1-(1H-pyrazol-3-yl)ethylidene]amino}oxy)acetate;

2-(2-furyl)-N-(5-isopropyl-1,3-thiazol-2-yl)-2-oxoacetamide;

2-(5-bromo-3-pyridinyl)-N-(5-isopropyl-1,3-thiazol-2-yl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(7-methoxy-2-oxo-2H-chromen-4-yl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-4-phenyl-3-butenamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-4-oxo-4-(4-methyl-phenyl)butanamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-4-(4-nitrophenyl)butanamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-4-phenylbutanamide;

benzyl 4-[(5-isopropyl-1,3-thiazol-2-yl)amino]-4-oxobutylcarbamatemethyl 5-[(5-isopropyl-1,3-thiazol-2-yl)amino]-5-oxopentanoate;

4-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-(5-isopropyl-1,3-thiazol-2-yl)butanamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-4-(4-methoxy-1-naphthyl)-4-oxobutanamide;

3-(2-chlorophenoxy)-N-(5-isopropyl-1,3-thiazol-2-yl)propanamide;

3-(4-methylphenoxy)-N-(5-isopropyl-1,3-thiazol-2-yl)propanamide;

3-cyclopentyl-N-(5-isopropyl-1,3-thiazol-2-yl)propanamide;

3-cyclohexyl-N-(5-isopropyl-1,3-thiazol-2-yl)propanamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-4-methylpentanamide;

3-(4-chlorophenyl)-N-(5-isopropyl-1,3-thiazol-2-yl)propanamide;

3-(4-methoxyphenyl)-N-(5-isopropyl-1,3-thiazol-2-yl)propanamide;

3-chloro-N-(5-isopropyl-1,3-thiazol-2-yl)propanamide;

3-phenyl-N-(5-isopropyl-1,3-thiazol-2-yl)propanamide;

2-cyclohexyl-N-(5-isopropyl-1,3-thiazol-2-yl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-3-methylbutanamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-5-oxo-5-phenylpentanamide;

2-[(5-isopropyl-1,3-thiazol-2-yl)amino]-2-oxoyl-phenylethyl acetate;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-[4-(1-oxo-1,3-dihydro-2H-isoindol-2-yl)phenyl]propanamide;

1-(4-chlorophenyl)-N-(5-isopropyl-1,3-thiazol-2-yl)cyclopentanecarboxamide;

1-phenyl-N-(5-isopropyl-1,3-thiazol-2-yl)cyclopentanecarboxamide;

2-(3-bromo-4-methoxyphenyl)-N-(5-isopropyl 1,3-thiazol-2-yl)acetamide;

2-(2-nitro-4-trifluoromethylphenyl)-N-(5-isopropyl. 1,3-thiazol-2-yl)acetamide;

5-cyclohexyl 1-(4-{2-[(5-isopropyl-1,3-thiazol-2-yl)amino]-2-oxoethyl}benzyl)-(2S)-2-[(tert-butoxycarbonyl)amino]pentanedioate;

2-(5,6-dimethyl-1H-benzimidazol-1-yl)-.N-(5-isopropyl-1,3-thiazol-2-yl)acetamide;

2-[5-(4-chlorophenyl)-2H-1,2,3,4-tetraazol-2-yl]-N-(5-isopropyl-1,3-thiazol-2-yl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-[5-(1-pyrrolidinyl)-2H-1,2,3,4-tetraazol-2-yl]acetamide;

N-(5-isopropyl-1,3-thiiazol-2-yl)-2-(3-methyl-1-benzothiophen-2-yl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-4,4-bis(4-methylphenyl)-3-butenamide;

2-cyclopropyl-N-(5-isopropyl-1,3-thiazol-2-yl)acetamide;

N-{4-bromo-6-[(5-isopropyl-1,3-thiazol-2-yl)amino]-6-oxohexyl}benzamide;

2-cyclopentyl-N-(5-isopropyl-1,3-thiazol-2-yl)acetamide;

benzyl 6-[(5-isopropyl-1,3-thiazol-2-yl)amino)-6-oxohexylcarbamate;

N-1-(5-isopropyl-1,3-thiazol-2-yl)-N-4-(2-propynyl)-2-butenediamide;

4-(2,4-dimethylphenyl)-N-(5-isopropyl-1,3-thiazol-2-yl)-4-oxobutanamide;

4-(4-benzyloxyphenyl)-N-(5-isopropyl-1,3.-thiazol-2-yl)-4-oxobutanamide;

4-(thiphen-2-yl)-N-(5-isopropyl-1,3-thiazol-2-yl)-4-oxobutanamide;

benzyl 2-{[(benzyloxy)carbonyl]amino}-5-[(5-isopropyl-1,3-thiazol-2-yl)amino]-5-oxopentanoate;

4-(1H-indol-3-yl)-N-{3-[(5-isopropyl-1,3-thiazol-2-yl)amino]-3-oxopropyl}butanamide;

4-{[(5-isopropyl-1,3-thiazol-2-yl)amino]carbonyl}phenyl 4-chlorobenzenesulfonate;

N-(5-isopropyl-1,3-thiazol-2-yl)-4-{[(2-methoxyanilino)carbonyl)amino}benzamide;

4-{[2-(isopropylsulfonyl)acetyl]amino}-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-4-{[2-(phenylsulfanyl)acetyl]amino}benzamide;

4-[(diethylamino)sulfonyl]-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

2-bromo-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

3,5-difluoro-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

3-{[(2-fluoroanilino)carbonyl]amino}-N-(5-isopropyl-1,3-thiazol-2-yl)benzamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-1-phenyl-5-propyl-1H-pyrazole-4-carboxamide;

3-chloro-4-(isopropylsulfonyl)-N-(s-isopropyl-t,3-thiazol-2-yl)-5-(methylsulfanyl)-2-thiophenecarboxamide;

3-iodo-4-(isopropylsulfonyl)-N-(5-isopropyl-1,3-thiazol-2-yl)-5-(methylsulfanyl)-2-thiophenecarboxamide;

2-{[(4-chlorophenyl)sulfonyl]methyl}-N-(5-isopropyl-1,3-thiazol-2-yl)-4-methyl-1,3-thiazole-5-carboxamide;

5-(4-chlorophenyl)-N-(5-isopropyl-1,3-thiazol-2-yl)-2-(trifluoromethyl)-3-furamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(2,3,4,5,6-pentafluorophenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(2-fluorophenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(2-bromophenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(2-chlorophenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(2-nitrophenyl) acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(2-trifluoromethylphenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(2-methoxyphenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(2,5-dimethoxyphenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(2,5-difluorophenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(3,4,5-trimethoxyphenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(2,6-dichlorophenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(2-chloro-6-fluorophenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(3,5-dimethoxyphenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(3,5-difluorophenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(2,5-bistrifluoromethylphenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(4-methylthiophenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(4-methoxyphenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(4-bromophenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(4-chlorophenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(4-fluorophenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(4-nitrophenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(4-trifluoromethylphenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(4-methylphenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(4-dimethylaminophenyl)acetamide;

2-[1,1′

-biphenyl)-4-yl-N-(5-isopropyl-1,3-thiazol-2-yl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(3-trifluoromethylphenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(3-bromophenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(3-chlorophenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(3-nitrophenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(3-methoxyphenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(2,4-dinitrophenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(2,4-dichlorophenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(2,4-difluorophenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(4-benzyloxy-3-methoxyphenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(3,4-dichlorophenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(3,4-difluorophenyl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(3,4-dimethoxyphenyl)acetamide;

2-(2,3-dihydro-1H-inden-5-yl)-N-(5-isopropyl-1,3-thiazol-2-yl)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-1-phenylcyclopropanecarboxamide;

2-cyclopentyl-N-(5-isopropyl-1,3-thiazol-2-yl)-2-phenylacetamide;

2-cyclohexyl-N-(5-isopropyl-1,3-thiazol-2-yl)-2-phenylacetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2,2-diphenylacetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(2-nitrophenoxy)acetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(4-nitrophenyl)propanamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-phenyl)propanamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-(4-isobutylphenyl)propanamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-oxo-2-phenylacetamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-3-methyl-2-phenylpentanamide;

(E,Z)-N-(5-isopropyl-1,3-thiazol-2-yl)-2-phenyl-2-butenamide;

N-(5-isopropyl-1,3-thiazol-2-yl)bicyclo[4.2.0]octa-1,3,5-triene-7-carboxamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-3-oxo-1-indanecarboxamide;

N-(5-isopropyl-1,3-thiazol-2-yl)-2-phenyl)butanamide;

tert-butyl (1S)-2-[(5-isopropyl-1,3-thiazol-2-yl)amino]-1-methyl-2-oxoethylcarbamate;

tert-butyl (1S,2S)-1-{[(5-isopropyl-1,3-thiazol-2-yl)amino]carbonyl}-2-methylbutylcarbamate;

tert-butyl 2-[(5-isopropyl-1,3-thiazol-2-yl)amino]-2-oxoethylcarbamate;

tert-butyl (1S)-5-amino-1-{[(5-isopropyl-1,3-thiazol-2-yl)amino]carbonyl}pentylcarbamate;

tert-butyl 4-[(imino {[(4-methylphenyl)sulfonyl]amino}methyl)amino]-1-{[(5-isopropyl-1,3-thiazol-2-yl)amino]carbonyl}butylcarbamate;

tert-butyl 1-{[(5-isopropyl-1,3-thiazol-2-yl)amino]carbonyl}-3-(tritylamino)propylcarbamate;

tert-butyl (1S)-1-(benzyloxymethyl)-2-[(5-isopropyl-1,3-thiazol-2-yl)amino]-2-oxoethylcarbamate;

tert-butyl (1S)-1-benzyl-2-[(5-isopropyl-1,3-thiazol-2-yl)amino]-2-oxoethylcarbamate;

tert-butyl (1R)-2-[(5-isopropyl-1,3-thiazol-2-yl)amino]-2-oxo-1-(benzylthiomethyl)ethylcarbamate;

benzyl (3S)-3-[(tert-butoxycarbonyl)amino]-4-[(5-isopropyl-1,3-thiazol-2-yl)amino]-4-oxobutanoate;

tert-butyl (2S)-2-{[(5-isopropyl-1,3-thiazol-2-yl)amino]carbonyl)-1-pyrrolidinecarboxylate;

tert-butyl (1S)-1-(1H-indol-3-ylmethyl)-2-[(5-isopropyl-1,3-thiazol-2-yl)amino]-2-oxoethylcarbamate;

tert-butyl (1S)-1-{[(5-isopropyl-1,3-thiazol-2-yl)amino]carbonyl)-3-(methylsulfanyl)propylcarbamate;

tert-butyl (1S)-2-benzyloxy-1-{[(5-isopropyl-1,3-thiazol-2-yl)amino]carbonyl)propylcarbamate;

tert-butyl (1S)-1-(4-benzyloxybenzyl)-2-[(5-isopropyl-1,3-thiazol-2-yl)amino]-2-oxoethylcarbamate;

tert-butyl (1S)-1-{[(5-isopropyl-1,3-thiazol-2-yl)amino7Jcarbonyl)-2-methylpropytcarbamate;

tert-butyl (1S)-1-{[(5-isopropyl-1,3-thiazol-2-.yl)amino]carbonyl)-3-methylbutylcarbamate and;

benzyl (4S)-4-[(tert-butoxycarbonyl)amino]-5-[(5-isopropyl-1,3-thiazol-2-yl)amino]-5-oxopentanoate;

and the pharmaceutically acceptable salts thereof.

7. A compound of formula (I) according to claim 1, wherein R₁ is optionally substituted in any of the free positions by one or more groups selected from the group consisting of halogen, nitro, oxo groups (═

O), carboxy, cyano, alkyl, perfluorinated alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocycyl, amino groups and derivatives thereof, carbonylamino groups and derivatives thereof, oxygen-substituted oximes, hydroxy group and derivatives thereof, carbonyl groups and derivatives thereof and sulfonated derivatives.

8. A compound of formula (I) according to claim 7, wherein said derivatives of amino groups are alkylamino, alkoxycarbonylalkylamino, dialkylamino, arylamino, diarylamino or aryleurido.

9. A compound of formula (I) according to claim 7, wherein said derivatives of carbonylamino groups are hydrogencarbonylamino (HCONH—

), alkylcarbonylamino, alkenylcarbonyl amino, alkenylcarbonylamino, arylcarbonylamino or alkoxycarbonylamino.

10. A compound of formula (I) according to claim 7, wherein said oxygensubstituted oximes are alkoxycarbonylalkoxyimino or alkoxyimino.

11. A compound of formula (I) according to claim 7, wherein said derivatives of hydrocy groups are alkoxy, alkylcarbonyloxy, arylcarbonyloxy or cycloalkenyloxy.

12. A compound of formula (I) according to claim 7, wherein said derivatives of carbonly groups are alkylcarbonyl, arylcarbonyl, alkoxycarbonyl, aryloxycarbonyl cycloalkyloxycarbonyl, alkylaminocarbonyl or dialkylaminocarbonyl.

13. A compound of formula (I) according to claim 1, wherein said sulfonated derivatives are alkylthio, arylthio, alkylsulphonyl, arylsulphonyl, alkylsulphinyl, arylsulphinyl, arylsulphonyloxy, aminosulfonyl, alkylaminosulphonyl or dialkylaminosulphonyl.