Site News  |   Monitor Keywords  |   Monitor Archive  |   Organizer  |   Account Info  |

Carboxylic acid amides, the preparation thereof, and their use as pharmaceutical compositions

Carboxylic acid amides, the preparation thereof, and their use as pharmaceutical compositions description/claims

This application claims benefit of U.S. Ser. No. 60/437,442, filed Dec. 30, 2002, and U.S. Ser. No. 60/498,788, filed Aug. 29, 2003, and claims priority to German Application No. 102 59 407.4, filed Dec. 19, 2002, and German Application No. 103 35 545.6, filed Aug. 2, 2003, each of which is hereby incorporated by reference in its entirety.

The present invention relates to new substituted carboxylic acid amides of general formula

the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.

The compounds of the above general formula I as well as the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, and their stereoisomers have valuable pharmacological properties, particularly an antithrombotic activity and a factor Xa-inhibiting activity.

The present application thus relates to the new compounds of the above general formula I, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and their use.

In the above general formula I in a 1st embodiment

R1 denotes an amino, C1-5-alkylamino, C3-7-cycloalkylamino or (phenyl-C1-3-alkyl)-amino group which may additionally be substituted in each case at the amino nitrogen atom by a phenylcarbonyl or phenylsulfonyl group or by C1-5-alkyl or C1-5-alkylcarbonyl group optionally substituted in the alkyl moiety by a hydroxy, C1-3-alkyloxy or carboxy group, a group which may be converted in vivo into a carboxy group, an amino, C1-3-alkylamino, di-(C1-3-alkyl)-amino or a 4- to 7-membered cycloalkyleneimino group, while in the above-mentioned substituted C1-5-alkyl group two heteroatoms are separated from one another by at least two carbon atoms, a 4- to 7-membered cycloalkyleneiminocarbonyl or cycloalkyleneiminosulfonyl group, while the cycloalkyleneimino moiety may be substituted in the carbon skeleton by a fluorine, chlorine or bromine atom, one or two C1-3-alkyl, C2-3-alkenyl, C2-3-alkynyl, hydroxy-C1-3-alkyl, C1-3-alkyloxy-C1-3-alkyl, phenyl-C1-3-alkyl, 1,1-diphenyl-C1-3-alkyl, heteroaryl-C1-3-alkyl, amino-C1-3-alkyl, C3-6-cycloalkylamino-C1-3-alkyl, phenylamino-C1-3-alkyl, C1-5-alkylamino-C1-3-alkyl, di-(C1-5-alkyl)-amino-C1-3-alkyl, N—(C3-6-cycloalkyl)-C1-3-alkylamino-C1-3-alkyl, a 4- to 7-membered cycloalkyleneimino-C1-3-alkyl, N—(C1-3-alkylcarbonyl)-C1-3-alkylamino-C1-3-alkyl, carboxy-C1-3-alkyl, C1-3-alkyloxycarbonyl-C1-3-alkyl, aminocarbonyl-C1-3-alkyl, C1-3-alkylaminocarbonyl-C1-3-alkyl, di-(C1-3-alkyl)-aminocarbonyl-C1-3-alkyl, a 4- to 7-membered cycloalkyleneiminocarbonyl-C1-3-alkyl, C1-5-alkyloxycarbonylamino-C1-3-alkyl, C1-3-alkylcarbonylamino-C1-3-alkyl, C1-3-alkylsulfonylamino-C1-3-alkyl, aminocarbonylamino-C1-3-alkyl, C1-3-alkylaminocarbonylamino-C1-3-alkyl, di-(C1-3-alkyl)-aminocarbonylamino-C1-3-alkyl, carboxy, C1-3-alkyloxycarbonyl, benzyloxycarbonyl, C1-3-alkylcarbonyl, aminocarbonyl, C1-3-alkylaminocarbonyl, di-(C1-3-alkyl)-aminocarbonyl, N—(C3-7-cycloalkyl)-C1-5 alkylaminocarbonyl, N-(phenyl-C1-3-alkyl)-C1-5-alkylaminocarbonyl, a 4- to 7-membered cycloalkyleneiminocarbonyl, aminocarbonyl-C1-3-alkylaminocarbonyl, hydroxy, C1-3-alkyloxy, allyloxy, propargyloxy, benzyloxy, amino, C1-3-alkylamino, di-(C1-3-alkyl)-amino, a 4- to 7-membered cycloalkyleneimino, trifluoromethylcarbonylamino, a mono-, di- or trifluoromethylamino, a phenyl or a 5- to 6-membered heteroaryl group, with the proviso that in the substitution of a methylene group adjacent to the imino group two heteroatoms are separated from one another by at least two carbon atoms, and/or a methylene group in the 3 position of a 5-membered cycloalkyleneimino group may be replaced by a sulfur atom, a sulfinyl or sulfonyl group or a methylene group in the 4 position of a 6- or 7-membered cycloalkyleneimino group may be replaced by an oxygen or sulfur atom, a carbonyl, sulfinyl or sulfonyl group or by an —NH— group optionally substituted by a C1-3-alkyl, hydroxy, formyl or C1-3-alkylcarbonyl group, while additionally a methylene group adjacent to the abovementioned optionally substituted —NH— group may be replaced by a carbonyl, sulfinyl or sulfonyl group, with the proviso that

Continue reading about Carboxylic acid amides, the preparation thereof, and their use as pharmaceutical compositions...
Full patent description for Carboxylic acid amides, the preparation thereof, and their use as pharmaceutical compositions

Brief Patent Description - Full Patent Description - Patent Application Claims

Click on the above for other options relating to this Carboxylic acid amides, the preparation thereof, and their use as pharmaceutical compositions patent application.
###


How KEYWORD MONITOR works... a FREE service from FreshPatents
1. Sign up (takes 30 seconds). 2. Fill in the keywords to be monitored.
3. Each week you receive an email with patent applications related to your keywords.  
Start now! - Receive info on patent apps like Carboxylic acid amides, the preparation thereof, and their use as pharmaceutical compositions or other areas of interest.
###


Previous Patent Application:
Thiazole and oxazole-substituted arylamides as p2x3 and p2x2/3 antagonists
Next Patent Application:
Pyrazole compounds that modulate the activity of cdk, gsk and aurora kinases
Industry Class:
Drug, bio-affecting and body treating compositions

###

• Provisional Patent
• Utility Patent

• What Is a Patent?
• What Is a Trademark or Servicemark?
• What Is a Copyright?
• Patent Laws