Thiazolyl-dihydro-indazoles
| Title: | Thiazolyl-dihydro-indazoles |
|---|---|
| Patent Number: | 8,207,349 |
| Publication Date: | June 26, 2012 |
| Appl. No: | 12/685213 |
| Application Filed: | January 11, 2010 |
| Abstract: | The present invention encompasses compounds of the general formula (1) [chemical expression included] in which R1 to R3 are defined as in claim 1, which are suitable for treating diseases which are characterized by excessive or anomalous cell proliferation, and their use for producing a pharmaceutical having the abovementioned properties. |
| Inventors: | Betzemeier, Bodo (Biberach, DE); Brandl, Trixi (Basel, CH); Breitfelder, Steffen (Attenweiler, DE); Brueckner, Ralph (Vienna, AT); Gerstberger, Thomas (Vienna, AT); Gmachl, Michael (Vienna, AT); Grauert, Matthias (Biberach, DE); Hilberg, Frank (Vienna, AT); Hoenke, Christoph (Ingelheim am Rhein, DE); Hoffmann, Matthias (Mittelbiberach, DE); Impagnatiello, Maria (Vienna, AT); Kessler, Dirk (Vienna, AT); Klein, Christian (Vienna, AT); Krist, Bernd (Altenmuenster, DE); Maier, Udo (Senden, DE); McConnell, Darryl (Vienna, AT); Reither, Charlotte (Vienna, AT); Scheuerer, Stefan (Warthausen, DE); Schoop, Andreas (Neuried, DE); Schweifer, Norbert (Vienna, AT); Simon, Oliver (Vienna, AT); Steegmaier, Martin (Reutlingen, DE); Steurer, Steffen (Vienna, AT); Waizenegger, Irene (Vienna, AT); Weyer-Czernilofsky, Ulrike (Baden, AT); Zoephel, Andreas (Vienna, AT) |
| Assignees: | Boehringer Ingelheim International GmbH (Ingelheim am Rhein, DE) |
| Claim: | 1. A compound of formula (A) [chemical expression included] wherein X is —CH 3 , —OR 4 or —SR 4 and Y is phenyl, 5-10-membered heteroaryl or the group —C(O)O, and R Y is hydrogen, —NO 2 or C 1-6 alkyl and R 4 is a radical selected from the group consisting of R b and R a wherein R a is optionally substituted by one or more, identical or different, R c and/or R b ; each R a is, independently of each other, selected from the group consisting of 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, 5-10-membered heteroaryl and 6-16-membered heteroarylalkyl; each R b is a suitable radical and in each case selected, independently of each other, from the group consisting of ═O, —OR c , C 1-3 haloalkyloxy, —OCF 3 , ═S, —SR c , ═NR c , ═NOR c , —NR c R c , halogen, —CF3, —CN, —NC, —OCN, —SCN, —NO, —NO 2 , ═N 2 , —N 3 , —S(O)R 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) 2 NR c R c , —C(O)R c , —C(O)OR c , —C(O)NR c R c , —C(O)N(R g)NR c R c , —C(O)N(R g)OR c , —CN(R g)NR c R c , —OC(O)R c , —OC(O)OR c , —OC(O)NR c R c , —OCN(R g)NR c R c , —N(R g)C(O)R c , —N(R g)C(O)R c , —N(R g)C(S)R c , —N(R g)S(O) 2 R c , —N(R g)S(O) 2 NR c R c , —N[S(O) 2 ] 2 R c , —N(R g)C(O)OR c , —N(R g)C(O)NR c R c , and —N(R g)CN(Rg)NR c R c ; each R e is, independently of each other, hydrogen or a radical which is optionally substituted by one or more, identical or different, R d and/or R e and which is selected from the group consisting of 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, 5-10-membered heteroaryl and 6-16-membered heteroarylalkyl, each R d is, independently of each other, hydrogen or a radical which is optionally substituted by one or more, identical or different, R e and/or R f and which is selected from the group consisting of 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, 5-10-membered heteroaryl and 6-16-membered heteroarylalkyl, each R e is a suitable radical and in each case selected, independently of each other, from the group consisting of ═O, —OR f , C 1-3 haloalkyloxy, —OCF 3 , ═S, —SR f , ═NR f , ═NOR f , —NR f R f , halogen, —CF3, —CN, —NC, —OCN, —SCN, —NO, —NO 2 , ═N 2 , —N 3 , —S(O)R f , —S(O) 2 R f , —S(O) 2 OR f , —S(O)NR f R f , —S(O) 2 NR f R f , —OS(O)R f , —OS(O) 2 R f , —OS(O) 2 OR f , —OS(O) 2 NR f R f , —C(O)R f , —C(O)OR f , —C(O)NR f R f , —CN(R g)NR f R f , —OC(O)R f , —OC(O)OR f , —OC(O)NR f R f , —OCN(R g)NR f R f , —N(R g)C(O)R f , —N(R g)C(S)R f , —N(R g)S(O) 2 R f , —N(R g)C(O)O R f , —N(R g)C(O)NR f R f , and —N(R g)CN(R g)NR f R f ; each R f is, independently of each other, hydrogen or a radical which is optionally substituted by one or more, identical or different, R g and is selected from the group consisting of 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, 5-10-membered heteroaryl and 6-16-membered heteroarylalkyl, each R g is, independently of each other, 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 heterocycloalkylalkyl, 5-10-membered heteroaryl and 6-16-membered heteroarylalkyl. |
| Claim: | 2. The compound according to claim 1 , wherein R 4 is —C 1-6 alkyl. |
| Current U.S. Class: | 548/163 |
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| Primary Examiner: | Chu, Yong |
| Attorney, Agent or Firm: | Morris, Michael P. Devlin, Mary-Ellen M. |
| Accession Number: | edspgr.08207349 |
| Database: | USPTO Patent Grants |
| Language: | English |
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