US2003083523A1PendingUtilityA1

Amide derivatives

42
Assignee: MITSUBISHI CHEM CORPPriority: Jun 25, 1997Filed: Jun 18, 2002Published: May 1, 2003
Est. expiryJun 25, 2017(expired)· nominal 20-yr term from priority
Inventors:Ryoichi AndoMakoto KawamuraNoriko ChibaKazutoshi Watanabe
C07C 2601/08C07D 307/79C07D 333/60C07C 2601/14C07D 209/18C07D 317/60C07C 237/42
42
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Claims

Abstract

A compound represented by the following general formula (I): wherein X represents R 1 (R 2 )R 3 )C- where R 1 represents a C 3 -C 8 cycloalkyl group, an optionally substituted C 6 -C 14 aryl group, an optionally substituted heterocyclic residue, an optionally substituted C 6 -C 14 aryloxy group, or an optionally substituted C 7 -C 15 arylmethyl group; R 2 and R 3 independently represent hydrogen atom or a C 1 -C 5 alkyl group, or R 2 and R 3 may combine to represent a C 2 -C 7 alkylene group; or X represents R 7 -A- wherein R 7 represents (i) a C1-C10 alkyl group which may optionally be substituted with an optionally substituted C6-C14 aryl group, an optionally substituted fluorenyl group or an optionally substituted heterocyclic group, (ii) an optionally substituted C6-C14 aryl group or (iii) an optionally substituted heterocyclic group, and A represents an oxygen atom or -N-R 8 where R 8 represents hydrogen atom or a C1-C5 alkyl group. Y represents an oxygen atom or a sulfur atom, R 4 and R 5 independently represent hydrogen atom or a C 1 -C 5 alkyl group; and R 6 represents hydrogen atom, a C 1 -C 5 alkyl group which may optionally be substituted with a hydroxyl group, a hydroxyl group or a C 1 -C 5 alkoxy group, provided that the compounds wherein R 7 is a benzyl group, A and Y are an oxygen atom, R 4 and R 5 are hydrogen atom, and R 6 is a propyl group are excluded, or a salt thereof, or a solvate thereof or a hydrate thereof.

Claims

exact text as granted — not AI-modified
What is claimed is:  
     
         1 . A compound represented by the following general formula (I):  
       
         
           
           
               
               
           
         
       
       wherein X represents R 1 (R 2 )(R 3 )C- where R 1  represents a C 3 -C 8  cycloakyl group, an optionally substituted C 5 -C 14  aryl group, an optionally substituted heterocyclic residue wherein the heterocyclic residue is one of furan ring, dihydrofuran ring, tetrahydrofuran ring, pyran ring, dihydropyran ring, tetrahydropyran ring, benzofuran ring, dihydrobenzofuran ring, isobenzofuran ring, chromene ring, chroman ring, isochroman ring, thiophene ring, benzothiophene ring, pyrrole ring, pyrroline ring, pyrrolidine ring, imidazole ring, imidazoline ring, imidazolidine ring, pyrazole ring, pyrazoline ring, pyrazolidine ring, triazole ring, tetrazole ring, pyridine ring, pyridineoxide ring, piperidine ring, pyrazine ring, piperazine ring, pyrimidine ring, pyridazine ring, indoline ring, indole ring, indoline ring, isoindole ring, isoindoline ring, indazole ring, benzimidazole ring, purine ring, quinolizine ring, quinoline ring, phthalazine ring, naphthylidine ring, quinoxaline ring, quinazoline ring, cinnoline ring, pteridine ring, oxazole ring, oxazolidine ring, isoxazole ring, isoxazolidine ring, thiazole ring, thiazylidine ring, isothiazole ring, isothiazolidine ring, dioxane ring, dithian ring, morpholine ring, and thiomorpholine ring, an optionally substituted C 6 -C 14  aryloxy group, or an optionally substituted C 7 -C 15  arylmethyl group; R 2  and R 3  independently represent hydrogen atom or a C 1 -C 5  alkyl group, or R 2  and R 3  may combine to represent a C 2 -C 7  alkylene group; or 
 X represents R 7 -A- wherein R 7  represents (i) a C1-C10 alkyl group which may optionally be substituted with an optionally substituted C6-C14 aryl group, an optionally substituted fluorenyl group or an optionally substituted heterocyclic group, (ii) an optionally substituted C6-C14 aryl group or (iii) an optionally substituted heterocyclic group, and A represents an oxygen atom or -N-R 8  where R 8  represents hydrogen atom or a C1-C5 alkyl group,  
 Y represents an oxygen atom or a sulfur atom,  
 R 4  and R 5  independently represent hydrogen atom or a C 1 -C 5  alkyl group; and R 6  represents hydrogen atom, a C 1 -C 5  alkyl group which may optionally be substituted with a hydroxyl group, a hydroxyl group or a C 1 -C 5  alkoxy group,  
 provided that the compounds wherein R 7  is a benzyl group, A and Y are an oxygen atom, R 4  and R 6  are hydrogen atom, and R 6  is a propyl group are excluded,  
 or a salt thereof, or a solvate thereof or a hydrate thereof.  
 
     
     
         2 . The compound according to  claim 1  or a salt thereof, or a solvate thereof or a hydrate thereof, wherein R 4  is hydrogen atom.  
     
     
         3 . The compound according to  claim 1  or a salt thereof, or a solvate thereof or a hydrate thereof, wherein R 5  is hydrogen atom.  
     
     
         4 . The compound according to  claim 3  or a salt thereof, or a solvate thereof or a hydrate thereof, wherein R 6  is a C 1 -C 5  alkyl group.  
     
     
         5 . The compound according to  claim 4  or a salt thereof, or a solvate thereof or a hydrate thereof, wherein R 6  is methyl group.  
     
     
         6 . The compound according to  claim 1  or a salt thereof or a solvate thereof or a hydrate thereof, wherein Y is an oxygen atom.  
     
     
         7 . The compound according to  claim 6  or a salt thereof, or a solvate thereof or a hydrate thereof, wherein X is R 1 (R 2 )(R 3 )C-.  
     
     
         8 . The compound according to  claim 7  or a salt thereof, or a solvate thereof or a hydrate thereof, wherein R 2  and R 3  are hydrogen atoms.  
     
     
         9 . The compound according to  claim 7  or a salt thereof, or a solvate thereof or a hydrate thereof, wherein R 1  is a C 6 -C 14  aryl group which may optionally be substituted.  
     
     
         10 . The compound according to  claim 7  or a salt thereof, or a solvate thereof or a hydrate thereof, wherein R 1  is a residue of a heterocyclic compound which may optionally be substituted.  
     
     
         11 . The compound according to  claim 7  or a salt thereof, or a solvate thereof or a hydrate thereof, wherein R 1  is a C 6 -C 14  aryloxy group which may optionally be substituted.  
     
     
         12 . The compound according to  claim 7  or a salt thereof, or a solvate thereof or a hydrate thereof, wherein R 1  is a C 7 -C 15  arylmethyl group which may optionally be substituted.  
     
     
         13 . The compound according to  claim 1  or a salt thereof, or a solvate thereof or a hydrate thereof, wherein X is R 7 -A-.  
     
     
         14 . The compound according to  claim 13  or a salt thereof, or a solvate thereof or a hydrate thereof, wherein A is an oxygen atom or -N-H.  
     
     
         15 . The compound according to  claim 13  or a salt thereof, or a solvate thereof or a hydrate thereof, wherein R 7  is a C1-C10 alkyl group which may optionally be substituted with an optionally substituted C6-C14 aryl group or an optionally substituted heterocyclic group.  
     
     
         16 . The compound according to  claim 15  or a salt thereof, or a solvate thereof or a hydrate thereof, wherein R 7  is a C1-C5 alkyl group which may optionally be substituted with an optionally substituted C6-C14 aryl group or an optionally substituted heterocyclic group.  
     
     
         17 . The compound according to  claim 16  or a salt thereof, or a solvate thereof or a hydrate thereof, wherein R 7  is a methyl group which may optionally be substituted with an optionally substituted C6-C14 aryl group or an optionally substituted heterocyclic group.  
     
     
         18 . The compound according to  claim 17  or a salt thereof, or a solvate thereof or a hydrate thereof, wherein R 7  is a methyl group which is substituted with an optionally substituted C6-C14 aryl group.  
     
     
         19 . The compound according to  claim 17  or a salt thereof, or a solvate thereof or a hydrate thereof, wherein R 7  is a methyl group which is substituted with an optionally substituted heterocyclic group.  
     
     
         20 . A compound selected from the group consisting of: 
 N-(3-methylcarbamoylphenyl)-3-chlorophenylacetamide;    N-(3-methylcarbamoylphenyl)-4-chlorophenylacetamide;    N-(3-methylcarbamoylphenyl)-3-bromophenylacetamide;    N-(3-methylcarbamoylphenyl)-4-bromophenylacetamide:    N-(3-methylcarbamoylphenyl)-3-methylphenylacetamide;    N-(3-methylcarbamoylphenyl)-4-methylphenylacetamide;    N-(3-methylcarbamoylphenyl)-3-methoxyphenylacetamide;    N-(3-methylcarbamoylphenyl)-4-methoxyphenylacetamide;    N-(3-methylcarbamoylphenyl)-3,4,5-trimethoxyphenylacetamide;    N-(3-methylcarbamoylphenyl)-3-benzyloxyphenylacetamide;    N-(3-methylcarbamoylphenyl)-1-naphthylacetamide;    N-(3-methylcarbamoylphenyl)-2-naphthylacetamide;    N-(3-methylcarbamoylphenyl)-3-inadolylacetamide;    N-(3-methylcarbamoylphenyl)-3-benzothienylacetamide;    N-(3-methylcarbamoylphenyl)-4-benzothienylacetamide;    N-(3-methylcarbamoylphenyl)-3,4-methylenedioxyphenylacetamide;    N-(3-methylcarbamoylphenyl)-2-chlorophenoxyacetamide;    N-(3-methylcarbamoylphenyl)-2,3-chlorophenoxyacetamide;    N-(3-methylcarbamoylpheny)-1-naphthyloxyacetamide;    N-(3-methylcarbamoylphenyl)-2-naphthyloxyacetimide; and    N-(3-methylcarbamoylphenyl)-3-(2-methoxyphenyl)propionamide,    or a pharmaceutically acceptable salt thereof, or a solvate thereof or a hydrate thereof.    
     
     
         21 . A compound selected from the group consisting of: 
 N′-methyl-3-(2-chlorobenzyloxycarbonylamino)benzamide,    N′-methyl-3-(4-chlorobenxyloxycarbonylamino)benzamide;    N′-methyl-3-(2,3-dichlorobenzyloxycarbonylamino)benzamide;    N′-methyl-3-(2,6-dichlorobenzyloxycarbonylamino)benzamide;    N′-methyl-3-(2-bromobenzyloxycarbonylamino)benzamide;    N′-methyl-3-(2-methylbenzyloxycarbonylamino)benzamide;    N′-methyl-3(3-methylbenzyloxycarbonylamino)benzamide;    N-methyl-3-(4-methylbenzyloxycarbonylamino)benzamide;    N′-methyl-3-(1-naphthylmethoxycarbonylamino)benzamide; and    N′-methyl-3-(2-naphthylmethoxycarbonylamino)benzamide;    or a pharmaceutically acceptable salt thereof, or a solvate thereof or a hydrate thereof.    
     
     
         22 . N-(3-methylcarbamoylpheny)-1-naphthylacetamide or a pharmaceutically acceptable salt thereof, or a solvate thereof or a hydrate thereof.  
     
     
         23 . N-(3-methylcarbamoylphenyl)-2-naphthylacetamide or a pharmaceutically acceptable salt thereof, or a solvate thereof or a hydrate thereof.  
     
     
         24 . N-(3-methylcarbamoylphenyl)-3-benzothienylacetamide or a pharmaceutically acceptable salt thereof, or a solvate thereof or a hydrate thereof.  
     
     
         25 . N-(3-methylcarbamoylphenyl)-4-benzothienylacetamide or a pharmaceutically acceptable salt thereof, or a solvate thereof or a hydrate thereof.  
     
     
         26 . N-(3-methylcarbamoylphenyl)-1-naphthyloxyacetamide or a pharmaceutically acceptable salt thereof, or a solvate thereof or a hydrate thereof.  
     
     
         27 . A medicament comprising as an active ingredient a substance selected from the group consisting of a compound according to  claim 1  and a salt thereof, and a solvate thereof and a hydrate thereof.  
     
     
         28 . The medicament according to  claim 27  which is in the form of a pharmaceutical composition comprising said substance as an active ingredient and one or more pharmaceutical additives.  
     
     
         29 . The medicament according to  claim 27  which has antibacterial activity.  
     
     
         30 . The medicament according to  claim 29  which has antibacterial activity against a microorganism belonging to the genus Helicobacter and/or Campylobacter.  
     
     
         31 . The medicament according to  claim 30  which has anti- Helicobacter pylori  activity and/or anti- Campylobacter jejuni  activity.  
     
     
         32 . A process for at least one of preventing and treating a digestive disease, comprising administering the medicament according  claim 27 .  
     
     
         33 . The process of  claim 32 , wherein the digestive disease is one of gastritis, gastric ulcer, gastric cancer, gastric malignant lymphoma, MALT lymphoma, duodenal ulcer, duodenal carcinoma, and enteritis.  
     
     
         34 . A process for preventing recurrence of a digestive disease, comprising administering the medicament according to  claim 27 .  
     
     
         35 . The process of  claim 34 , wherein the digestive disease is one of gastric ulcer and duodenal ulcer.

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