Claims
- 1. A compound of the general formula I whereinR1 independently represents one or more, same or different substituents selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, carbamoyl, phenyl, or nitro, provided that when R1 represents one substituent, it is in the ortho position, and when R1 represents more than one substituent, at least one R1 substituent is in the ortho position; and R2 represents one substituent in the ortho position, said substituent being selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, carbamoyl, phenyl, or nitro; R3 represents hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, phenyl, cyano, carboxy, or carbamoyl; R4 represents hydrogen, (C1-C3)alkyl, or allyl; X represents oxygen or sulphur; with the proviso that formula I does not comprise the compound 2,2,2-trifluoro-N-[2-[3-chloro-4-(2-methylbenzoyl)-phenylamino]-phenyl]acetamide wherein R1 is 2-methyl, R2 is 2-chloro, R3 and R4 is hydrogen, and X is oxygen; and a salt thereof with a pharmaceutically acceptable acid, a hydrate or a solvate thereof.
- 2. A compound according to claim 1 wherein independentlyR1 represents one or more, same or different substituents selected from the group consisting of fluoro, chloro, bromo, hydroxy, trifluoromethyl, amino, (C1-C2)alkyl, (C2-C3)alkenyl, (C1-C3)alkoxy, (C1-C3)alkoxycarbonyl, cyano, or —COHH2; R2 represents one or more, same or different substituents selected from the group consisting of hydrogen, fluoro, chloro, bromo, hydroxy, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)alkenyl, (C1-C3)alkoxy; R3 represents one or more, same or different substituents selected from the group consisting of hydrogen, fluoro, chloro, bromo, hydroxy, trifluoromethyl, (C1-C3)alkyl, (C2-C3)alkenyl, (C1-C3)alkoxy, (C1-C3)alkoxycarbonyl, cyano, carboxy, or —CONH2; R4 represents hydrogen, (C1-C2)alkyl, or allyl; X represents oxygen.
- 3. A compound according to any one of claims 1 or 2R1 represents one or more, same or different substituents selected from the group consisting of fluoro, chloro, bromo, hydroxy, methyl, or methoxy; R2 represents one or more, same or different substituents selected from the group consisting of hydrogen, fluoro, chloro, bromo, hydroxy, methyl or methoxy; R3 represents one or more, same or different substituents selected from the group consisting of fluoro, chloro, bromo, hydroxy, methyl, or methoxy; R4 represents hydrogen or (C1-C2)alkyl.
- 4. A compound according to claim 1 R1 is 2-methyl.
- 5. A compound according to claim 1 wherein R2 is 2-Cl.
- 6. A compound according to claim 1 selected from the group consisting of2,2,2-Trifluoro-N-[5-bromo-2-[3-chloro-4-(2-methylbenzoyl)-phenylamino]-phenyl]acetamide (Compound 101), 2,2,2-Trifluoro-N-[2-[3-chloro-4-(2-methylbenzoyl)-phenylamino]-5-fluorophenyl]acetamide (Compound 102), 2,2,2-Trifluoro-N-[5-bromo-2-[3-chloro-4-(4-chloro-2-methylbenzoyl)-phenylamino]phenyl]acetamide (Compound 105), 2,2,2-Trifluoro-N-[5-bromo-2-[3-fluoro-4-(2-methylbenzoyl)-phenylamino]phenyl]acetamide (Compound 106), 2,2,2-Trifluoro-N-[5-bromo-2-[3-chloro-4-(2,4,5-trimethylbenzoyl)-phenylamino]phenyl]acetamide (Compound 107), 2,2,2-Trifluoro-N-[5-bromo-2-[3-chloro-4-(4-fluoro-2-methylbenzoyl)-phenylamino]phenyl]acetamide (Compound 108), 2,2,2-Trifluoro-N-[5-bromo-2-[3-chloro-4-(2,5-dimethylbenzoyl)-phenylamino]phenyl]acetamide (Compound 109), 2,2,2-Trifluoro-N-[5-bromo-2-[3-fluoro-4-(4-methoxy-2-methylbenzoyl)-phenylamino]phenyl]acetamide (Compound 111), and salts thereof with pharmaceutically acceptable acids, hydrates and solvates.
- 7. A pharmaceutical composition containing as an active ingredient a compound according to claim 1 together with a pharmaceutically acceptable carrier and optionally together with a second active ingredient optionally selected from the group consisting of glucocorticoids, vitamin D's, anti-histamines, platelet activating factor (PAF) antagonists, anticolinergic angents, methyl xanthines, β-adrenergic agents, salicylates, indomethacin, flufenamate, naproxen, timegadine, gold salts, penicillamine, serum cholesterol-reducing agents, retinoids, zinc-salts, and salicylazosulfapyridin (Salazopyrin).
- 8. A method for the treatment and/or prophylaxis of asthma, allergy, arthritis, including rheumatoid arthritis and spondyloarthrities, gout, atherosclerosis, chronic inflammatory bowel disease (Crohn's disease), proliferative and inflammatory skin disorder, such as psoriasis, atopic dermatitis, uveitis, septic shock, AIDS, osteoporosis and acne, characterized in administering to a patient suffering from at least one of said diseases an effective amount of one or more compounds according to claim 1 as an active ingredient alone, or if necessary together with a pharmaceutically acceptable carrier, and, optionally, a second active ingredient optionally selected from the group consisting of glucocorticoids, vitamin D's, anti-histamines, platelet activating factor (PAF) antagonists, anticolinergic agents, methyl xanthines, β-adrenergic agents, salicylates, indomethacin, flufenamate, naproxen, timegadine, gold salts, penicillamine, serum cholesterol-reducing agents, retinoids, zinc salts, and salicylazosulfapyridin (Salazopyrin).
Parent Case Info
This application is the national phase under 35 U.S.C. §371 of PCT International Application No. PCT/DK00/00388 which has an International filing date of Jul. 11, 2000, which designated the United States of America and was published in English, which claims benefit of Ser. No. 60/144,169, filed Jul. 16, 1999.
PCT Information
Filing Document |
Filing Date |
Country |
Kind |
PCT/DK00/00388 |
|
WO |
00 |
Publishing Document |
Publishing Date |
Country |
Kind |
WO01/05745 |
1/25/2001 |
WO |
A |
US Referenced Citations (1)
Number |
Name |
Date |
Kind |
6313174 |
Ottosen et al. |
Nov 2001 |
B1 |
Foreign Referenced Citations (1)
Number |
Date |
Country |
9832730 |
Jul 1998 |
WO |
Provisional Applications (1)
|
Number |
Date |
Country |
|
60/144169 |
Jul 1999 |
US |