US2011288109A1PendingUtilityA1

New compounds

Assignee: STADTMUELLER HEINZPriority: Nov 24, 2008Filed: Nov 24, 2009Published: Nov 24, 2011
Est. expiryNov 24, 2028(~2.3 yrs left)· nominal 20-yr term from priority
A61P 37/06A61P 37/00A61P 35/00C07D 239/47C07D 401/14A61P 29/00A61P 31/00C07D 413/14C07D 417/14C07D 401/12C07D 403/12C07D 405/14
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Claims

Abstract

The present invention includes compounds of general Formula (1), wherein A, X, R 1 and R 2 are defined as in claim 1 , which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.

Claims

exact text as granted — not AI-modified
1 . A compound of the formula (1), 
       
         
           
           
               
               
           
         
         wherein 
         A denotes a group, optionally substituted by one or more identical or different R 1 , selected from among C 6-15 aryl and 5-12 membered heteroaryl; 
         X denotes O, S or CH 2 ; 
         R 1  denotes hydrogen or a group selected from among R a , R b  and R a  substituted by one or more identical or different R c  and/or R b    
         R 2  denotes a group selected from among R a  and R a  substituted by one or more identical or different R b  and/or R c ; 
         each R a  is selected independently of one another from among C 1-6 alkyl, C 3-10 cycloalkyl, C 4-16 cycloalkylalkyl, C 6-10 aryl, C 7-16 arylalkyl, 2-6 membered heteroalkyl, 3-8 membered heterocycloalkyl, 4-14 membered heterocycloalkylalkyl, 5-12 membered heteroaryl and 6-18 membered heteroarylalkyl; 
         each R b  is a suitable group and each is independently selected from among ═O, —OR c , C 1-3 haloalkyloxy, —OCF 3 , ═S, —SR c , ═NR c , ═NOR c , ═NNR c R c , ═NN(R g )C(O)NR c R c , —NR c R c , —ONR c R c , —N(OR c )R c , —N(R g )NR c R c , halogen, —CF 3 , —CN, —NC, —OCN, —SCN, —NO, —NO 2 , ═N 2 , —N 3 , —S(O)R c , —S(O)OR c , —S(O) 2 R c , —S(O) 2 OR c , —S(O)NR c R c , —S(O) 2 NR c R c , —OS(O)R c , —OS(O) 2 R c , —OS(O) 2 OR c , —OS(O)NR c R c , —OS(O) 2 NR c R c , —C(O)R c , —C(O)OR c , —C(O)SR c , —C(O)NR c R c , —C(O)N(R g )NR c R c , —C(O)N(R g )OR c , —C(NR g )NR c R c , —C(NOH)R c , —C(NOH)NR c R c , —OC(O)R c , —OC(O)OR c , —OC(O)SR c , —OC(O)NR c R c , —OC(NR g )NR c R c , —SC(O)R c , —SC(O)OR c , —SC(O)NR c R c , —SC(NR g )NR c R c , —N(R g )C(O)R c , —N[C(O)R c ] 2 , —N(OR g )C(O)R c , —N(R g )C(NR g )R c , —N(R g )N(R g )C(O)R c , —N[C(O)R c ]NR c R c , —N(R g )C(S)R c , —N(R g )S(O)R c , —N(R g )S(O)OR c , —N(R g )S(O) 2 R c , —N[S(O) 2 R c ] 2 , —N(R g )S(O) 2 OR c , —N(R g )S(O) 2 NR c R c , —N(R g )[S(O) 2 ] 2 R c , —N(R g )C(O)OR c , —N(R g )C(O)SR c , —N(R g )C(O)NR c R c , —N(R g )C(O)NR g NR c R c , —N(R g )N(R g )C(O)NR c R c , —N(R g )C(S)NR c R c , —N(R g )C(O)] 2 R c —N(R g )[C(O)] 2 R c , —N{[C(O)] 2 R c } 2 , —N(R g )[C(O)] 2 OR c , —N(R g )[C(O)] 2 NR c R c , —N{[C(O)] 2 OR c } 2 , —N {[C(O)] 2 NR c R c } 2 , —[N(R g )C(O)] 2 OR c , —N(R g )C(NR g )OR c , —N(R g )C(NOH)R c , —N(R g )C(NR g )SR c  and —N(R g )C(NR g )NR c R c , 
         each R c  independently of one another denotes hydrogen or a group optionally substituted by one or more identical or different R d  and/or R e  selected from among C 1-6 alkyl, C 3-10 cycloalkyl, C 4-11 cycloalkylalkyl, C 6-10 aryl, C 7-16 arylalkyl, 2-6 membered heteroalkyl, 3-8 membered heterocycloalkyl, 4-14 membered heterocycloalkylalkyl, 5-12 membered heteroaryl and 6-18 membered heteroarylalkyl; 
         each R d  is a suitable group and each is independently selected from among ═O, —OR e , C 1-3 haloalkyloxy, —OCF 3 , ═S, —SR e , ═NR e , ═NOR e , ═NNR e R e , ═NN(R g )C(O)NR e R e , —NR e R e , —ONR e R e , —N(R g )NR e R e , halogen, —CF 3 , —CN, —NC, —OCN, —SCN, —NO, —NO 2 , ═N 2 , —N 3 , —S(O)R e , —S(O)OR e , —S(O) 2 R e , —S(O) 2 OR e , —S(O)NR e R e , —S(O) 2 NR e R e , —OS(O)R e , —OS(O) 2 R e , —OS(O) 2 OR e , —OS(O)NR e R e , —OS(O) 2 NR e R e , —C(O)R e , —C(O)OR e , —C(O)SR e , —C(O)NR e R e , —C(O)N(R g )NR e R e , —C(O)N(R g )OR e , —C(NR g )NR e R e , —C(NOH)R e , —C(NOH)NR e R e , —OC(O)R e , —OC(O)OR e , —OC(O)SR e , —OC(O)NR e R e , —OC(NR g )NR e R e , —SC(O)R e , —SC(O)OR e , —SC(O)NR e R e , —SC(NR g )NR e R e , —N(R g )C(O)R e , —N[C(O)R e ] 2 , —N(OR g )C(O)R e , —N(R g )C(NR g )R e , —N(R g )N(R g )C(O)R e , —N[C(O)R e ]NR e R e , —N(R g )C(S)R c , —N(R g )S(O)R e , —N(R g )S(O)OR e —N(R g )S(O) 2 R e , —N[S(O) 2 R c ] 2 , —N(R g )S(O) 2 OR e , —N(R g )S(O) 2 NR e R e , —N(R g )[S(O) 2 ] 2 R e , —N(R g )C(O)OR e , —N(R g )C(O)SR e , —N(R g )C(O)NR e R e , —N(R g )C(O)NR g NR e R e , —N(R g )N(R g )C(O)NR e R e , —N(R g )C(S)NR e R e , —[N(R g )C(O)] 2 R e , —N(R g )[C(O)] 2 R e , —N{[C(O)] 2 R e } 2 , —N(R g )[C(O)] 2 OR e , —N(R g )[C(O)] 2 NR e R e , —N{[C(O)] 2 OR e } 2 , —N{[C(O)] 2 NR e R e } 2 , —[N(R g )C(O)] 2 OR e , —N(R g )C(NR g )OR e , —N(R g )C(NOH)R e , —N(R g )C(NR g )SR e  and —N(R g )C(NR g )NR e R e , 
         each R e  independently of one another denotes hydrogen or a group optionally substituted by one or more identical or different R f  and/or R g  selected from among C 1-6 alkyl, C 3-8 cycloalkyl, C 4-11 cycloalkylalkyl, C 6-10 aryl, C 7-16 arylalkyl, 2-6 membered heteroalkyl, 3-8 membered heterocycloalkyl, 4-14 membered heterocycloalkylalkyl, 5-12 membered heteroaryl and 6-18 membered heteroarylalkyl; 
         each R f  is a suitable group and each is independently selected from among halogen and —CF 3 ; and 
         each R g  independently of one another denotes hydrogen, C 1-6 alkyl, C 3-8 cycloalkyl, C 4-11 cycloalkylalkyl, C 6-10 aryl, C 7-16 arylalkyl, 2-6 membered heteroalkyl, 3-8 membered heterocycloalkyl, 4-14 membered heterocycloalkyl, 5-12 membered heteroaryl or 6-18 membered heteroarylalkyl; 
         or a tautomer or salt thereof. 
       
     
     
         2 . A compound according to  claim 1 , wherein A is phenyl or 5-10 membered heteroaryl. 
     
     
         3 . A compound according to  claim 2 , wherein A is phenyl. 
     
     
         4 . A compound according to  claim 1 , wherein X denotes O. 
     
     
         5 . A compound according to  claim 1 , wherein R 2  is a group selected from among C 1-6 alkyl, C 3-8 cycloalkyl, C 6-10 aryl, 3-8 membered heterocycloalkyl and 5-12 membered heteroaryl, optionally substituted by one or more identical or different R b  and/or R c . 
     
     
         6 . A compound according to  claim 5 , wherein R 2  is a group selected from among C 6-10 aryl and 5-12 membered heteroaryl, optionally substituted by one or more identical or different R b  and/or R c . 
     
     
         7 . A compound according to  claim 1 , selected from the group consisting of 
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
       
       or a salt thereof. 
     
     
         8 . A pharmaceutically acceptable salt of a compound according to  claim 1 ,  2 ,  3 ,  4 ,  5 ,  6  or  7 . 
     
     
         9 . (canceled) 
     
     
         10 . A pharmaceutical composition comprising a compound according to  claim 1 ,  2 ,  3 ,  4 ,  5 ,  6  or  7  or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier or diluent. 
     
     
         11 . A method for treating cancer, infections, inflammations and autoimmune disease which comprises administering to a host suffering from such condition a therapeutically effective amount of a compound according to  claim 1 ,  2 ,  3 ,  4 ,  5 ,  6  or  7  or a pharmaceutically acceptable salt thereof. 
     
     
         12 . (canceled)

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