ThiazolyldihydroindazolesThe present invention relates to novel thiazolyldihydroindazoles of the general formula (I) where the R, R and R radicals are each as defined in the claims and the description, to their tautomers, racemates, enantiomers, diastereomers and mixtures thereof, and where appropriate to their pharmacologically safe acid addition salts, solvates and hydrates, and to processes for preparing these thiazolyldihydroindazoles and to their use as medicaments.General formula (i) compoundwhereinr 1expression hydrogen, co-ch 3, co-ch 2-r 4, co-chme-r 4, co-or 4, co-sr 4, co-nh 2, co-nhr 4r 2expression is selected from following group: c 3-6-cycloalkyl, c 1-4-alkyl-c 3-6-cycloalkyl, c 2-4-thiazolinyl-c 3-6-cycloalkyl, c 2-4-alkynyl-c 3-6-cycloalkyl, c 5-6-cycloalkenyl group, c 1-6alkyl-c 5-6-cycloalkenyl group, c 2-4-thiazolinyl-c 5-6-cycloalkenyl group, c 2-4-alkynyl-c 5-6-cycloalkenyl group, c 5-6-cycloalkynyl radical, c 1-6-alkyl-c 5-6-cycloalkynyl radical, c 2-4-thiazolinyl-c 5-6-cycloalkynyl radical and c 2-4-alkynyl-c 5-6-cycloalkynyl radical, it is optional by one or two group ch 3, f, och 3, oh or nh 2replace; r 3expression is selected from following group: c 6-c 14-aryl, c 1-6-alkyl-c 6-c 14-aryl, c 2-6-thiazolinyl-c 6-c 14-aryl, c 2-6alkynyl-c 6-c 14-aryl, c 5-c 10-heteroaryl, c 1-12-alkyl-c 5-c 10-heteroaryl, c 3- 12-thiazolinyl-c 5-c 10-heteroaryl, c 3-12-alkynyl-c 5-c 10-heteroaryl, c 3-6-cycloalkyl, c 1-6-alkyl-c 3-6-cycloalkyl, c 2-4-thiazolinyl-c 3-6-cycloalkyl, c 2-4-alkynyl-c 3-6-cycloalkyl, c 5-6-cycloalkenyl group, c 1-6-alkyl-c 5-6-cycloalkenyl group, c 2-4-thiazolinyl-c 5-6-cycloalkenyl group, c 2-4-alkynyl-c 5-6-cycloalkenyl group, c 5-6-cycloalkynyl radical, c 1-6-alkyl-c 5-6-cycloalkynyl radical, c 2-4-thiazolinyl-c 5-6-cycloalkynyl radical-and c 2-4-alkynyl-c 5-6-cycloalkynyl radical, it is optional by radicals r 5and three radicals r at the most 6replace; or the optional substituted following formula group of expressionwhereinn, m represent 1 or 2 independently of one another;r 4optional substituted following group: the c that is selected from of expression 1-4-alkyl, c 2-10-thiazolinyl, c 2-10-alkynyl, c 3-6-cycloalkyl-c 1-4-alkyl, c 3-6-cycloalkyl-c 3-10-thiazolinyl, c 3-6-cycloalkyl-c 3-10-alkynyl, c 6-c 14-aryl, c 6-c 14-aryl-c 1-4-alkyl, c 5-c 10-heteroaryl, c 5-c 10-heteroaryl-c 1-4-alkyl-and haloalkyl; r 5expression conr 8r 9, nr 8cor 9, nr 8r 9, or 9,-c 1-4-alkyl-conr 8r 9r 6it can be identical or different, expression f, c1, br, oh, cn, cf 3, chf 2, or optional substituted following the group :-o-c that is selected from of expression 1-3-alkyl ,-o-c 3-4-thiazolinyl ,-o-c 3-4-alkynyl, c 1-3-alkyl, c 2-6-thiazolinyl and c 2-3-alkynyl, c 3-6-cycloalkyl-c 1-4-alkyl, c 3-6-cycloalkyl-c 2-4-thiazolinyl, c 3-6-cycloalkyl-c 2-4-alkynyl, c 5-6-cycloalkenyl group-c 1-4-alkyl, c 5-6-cycloalkenyl group-c 3-10-thiazolinyl, c 5-6-cycloalkenyl group-c 2-4-alkynyl, c 6-c 14-aryl-c 1-4-alkyl, c 6-c 14-aryl-c 2-4-thiazolinyl-, c 6-c 14-aryl-c 2-4-alkynyl, c 5-c 10-heteroaryl-c 1-4-alkyl, c 5-c 10-heteroaryl-c 2-4-thiazolinyl-and c 5-c 10-heteroaryl-c 2-4-alkynyl; r 7expression hydrogen, cor 9, conr 8r 9, or be selected from following group: c 1-10-alkyl, c 3-10-thiazolinyl, c 3-10-alkynyl, c 3-6-cycloalkyl-c 1-4-alkyl, c 3-6-cycloalkyl-c 3- 10-thiazolinyl, c 3-6-cycloalkyl-c 3-10-alkynyl, c 5-6-cycloalkenyl group-c 1-4-alkyl, c 5-6-cycloalkenyl group-c 3-10-thiazolinyl, c 5-6-cycloalkenyl group-c 3-10-alkynyl, c 6-c 14-aryl, c 1-10-alkyl-c 6-c 14-aryl, c 2-10-thiazolinyl-c 6-c 14-aryl, c 2-10-alkynyl-c 6-c 14-aryl, c 5-c 10-heteroaryl, c 1-12-alkyl-c 5-c 10-heteroaryl, c 3-12-thiazolinyl-c 5-c 10-heteroaryl-and c 3-12-alkynyl-c 5-c 10-heteroaryl, it is optional by radicals r 14with by radicals r 13replace; r 8expression hydrogen, or optional substituted following group: the c that is selected from 1-10-alkyl, c 3-10-thiazolinyl, c 3-10-alkynyl, c 3-6-cycloalkyl-c 1-4-alkyl, c 3-6-cycloalkyl-c 3-10-thiazolinyl, c 3-6-cycloalkyl-c 3-10-alkynyl, c 5-6-cycloalkenyl group-c 1-4-alkyl, c 5-6-cycloalkenyl group-c 3-10-thiazolinyl, c 5-6-cycloalkenyl group-c 3-10-alkynyl, c 6-c 14-aryl-c 1-4-alkyl, c 6-c 14-aryl-c 3-10-thiazolinyl-with c 6-c 14-aryl-c 3-10-alkynyl, c 5-c 10-heteroaryl, c 5-c 10-heteroaryl-c 1-4-alkyl, c 5-c 10-heteroaryl-c 1-4-thiazolinyl, c 5-c 10-heteroaryl-c 1-4-alkynyl, c 1-4-alkyl-o-c 2-4-alkyl, c 1-4-alkyl-o-c 4-6-thiazolinyl-and c 1-4-alkyl-o-c 4-6-alkynyl-; r 9expression hydrogen, or optional substituted following group: the c that is selected from 1-12-alkyl, c 3-12-thiazolinyl, c 3-12-alkynyl, c 3-6-cycloalkyl-c 1-12-alkyl, c 3-6-cycloalkyl-c 3-12-thiazolinyl, c 3-6-cycloalkyl-c 3-12-alkynyl, c 5-6-cycloalkenyl group-c 1-4-alkyl, c 5-6-cycloalkenyl group-c 3-10-thiazolinyl, c 5-6-cycloalkenyl group-c 3-10-alkynyl, c 6-c 14-aryl-c 1-12-alkyl, c 6-c 14-aryl-c 3- 12-thiazolinyl, c 6-c 14-aryl-c 3-12-alkynyl, c 6-c 14-aryl, c 1-12-alkyl-c 6-c 14-aryl, c 2-12-thiazolinyl-c 6-c 14-aryl, c 2-12-alkynyl-c 6-c 14-aryl, c 5-c 10-heteroaryl, c 5-c 10-heteroaryl-c 1-12-alkyl, c 5-c 10-heteroaryl-c 3-12-thiazolinyl, c 5-c 10-heteroaryl-c 3- 12-alkynyl, c 3-8-cycloalkyl, c 5-8-cycloalkenyl group, nr 11r 12-c 3-8-cycloalkyl, nr 11r 12-c 5-8-cycloalkenyl group-and nr 11r 12-c 5-8-cycloalkynyl radical, or the optional substituted c of expression 3-8-heterocyclylalkyl-(ch 2) qgroup contains at least one nr in this 3-to 8-unit heterocyclic grou...
티아졸릴디하이드로인다졸 본 발명은 화학식 I의 티아졸릴디하이드로인다졸, 이의 토토머, 라세미체, 에난티오머, 부분입체이성체 및 이들의 혼합물, 및 경우에 따라 이의 약리학적으로 안전한 산 부가염, 용매화물 및 수화물; 및 이들 티아졸릴디하이드로인다졸의 제조방법 및 약제로서의 이의 용도에 관한 것이다. 화학식 I  상기 화학식 I에서, R1, R2 및 R3 라디칼은 각각 본원 청구의 범위 및 명세서에서 정의한 바와 같다. 화학식 I의 화합물, 임의로 이의 토토머, 라세미체, 에난티오머, 부분입체이성체 및 이들의 혼합물 형태, 및 임의로 이의 약리학적으로 허용되는 산 부가염, 용매화물 및 수화물. 화학식 I [이미지] 상기 화학식 I에서, R1은 수소, CO-CH3, CO-CH2-R4, CO-CHMe-R4, CO-OR4, CO-SR4, CO-NH2 또는 CO-NHR4이고; R2는 그룹 CH3, F, OCH3, OH 또는 NH2 중 1개 또는 2개에 의해 임의로 치환될 수 있는 C3-6-사이클로알킬, C1-4-알킬-C3-6-사이클로알킬, C2-4-알케닐-C3-6-사이클로알킬, C2-4-알키닐-C3-6-사이클로알킬, C5-6-사이클로알케닐, C1-6-알킬-C5-6-사이클로알케닐, C2-4-알케닐-C5-6-사이클로알케닐, C2-4-알키닐-C5-6-사이클로알케닐, C5-6-사이클로알키닐, C1-6-알킬-C5-6-사이클로알키닐, C2-4-알케닐-C5-6-사이클로알키닐- 및 C2-4-알키닐-C5-6-사이클로알키닐로부터 선택된 그룹이고; R3은 그룹 R5 및 3개 이하의 그룹 R6에 의해 임의로 치환될 수 있는 C6-C14-아릴, C1-6-알킬-C6-C14-아릴, C2-6-알케닐-C6-C14-아릴, C2-6-알키닐-C6-C14-아릴, C5-C10-헤테로아릴, C1-12-알킬-C5-C10-헤테로아릴, C3-12-알케닐-C5-C10-헤테로아릴, C3-12-알키닐-C5-C10-헤테로아릴, C3-6-사이클로알킬, C1-6-알킬-C3-6-사이클로알킬, C2-4-알케닐-C3-6-사이클로알킬, C2-4-알키닐-C3-6-사이클로알킬, C5-6-사이클로알케닐, C1-6-알킬-C5-6-사이클로알케닐, C2-4-알케닐-C5-6-사이클로알케닐, C2-4-알키닐-C5-6-사이클로알케닐, C5-6-사이클로알키닐, C1-6-알킬-C5-6-사이클로알키닐, C2-4-알케닐-C5-6-사이클로알키닐- 및 C2-4-알키닐-C5-6-사이클로알키닐로부터 선택된 그룹, 또는 임의로 치환된 [이미지]이고, 여기서, n 및 m은 서로 독립적으로 1 또는 2이고; R4는 C1-4-알킬, C2-10-알케닐, C2-10-알키닐, C3-6-사이클로알킬-C1-4-알킬, C3-6-사이클로알킬-C3-10-알케닐, C3-6-사이클로알킬-C3-10-알키닐, C6-C14-아릴, C6-C14-아릴-C1-4-알킬, C5-C10-헤테로아릴, C5-C10-헤테로아릴-C1-4-알킬- 및 할로알킬로부터 선택되는 임의로 치환된 그룹이고; R5는 CONR8R9, NR8COR9, NR8R9, OR9 또는 -C1-4-알킬-CONR8R9이고; R6은 동일하거나 상이할 수 있고, F, Cl, Br, OH, CN, CF3, CHF2, 또는 O-C1-3-알킬, O-C3-4-알케닐, O-C3-4-알키닐, C1-3-알킬, C2-6 -알케닐 및 C2-3-알키닐, C3-6-사이클로알킬-C1-4-알킬, C3-6-사이클로알킬-C2-4-알케닐, C3-6-사이클로알킬-C2-4-알키닐, C5-6-사이클로알케닐-C1-4-알킬, C5-6-사이클로알케닐-C3-10-알케닐, C5-6-사이클로알케닐-C2-4-알키닐, C6-C14-아릴-C1-4-알킬, C6-C14-아릴-C2-4-알케닐, C6-C14-아릴-C2-4-알키닐, C5-C10-헤테로아릴-C1-4-알킬, C5-C10-헤테로아릴-C2-4-알케닐- 및 C5-C10-헤테로아릴-C2-4-알키닐로부터 선택된 임의로 치환된 그룹이고; R7은 수소, COR9, CONR8R9, 또는 그룹 R14 및 그룹 R13에 의해 임의로 치환될 수 있는 C1-10-알킬, C3-10-알케닐, C3-10-알키닐, C3-6-사이클로알킬-C1-4-알킬, C3-6-사이클로알킬-C3-10-알케닐, C3-6-사이클로알킬-C3-10-알키닐, C5-6-사이클로알케닐-C1-4-알킬, C5-6-사이클로알케닐-C3-10-알케닐, C5-6-사이클로알케닐-C3-10-알키닐, C6-C14-아릴, C1-10-알킬-C6-C14-아릴, C2-10-알케닐-C6-C14-아릴- ,C2-10-알키닐-C6-C14-아릴, C5-C10-헤테로아릴, C1-12-알킬-C5-C10-헤테로아릴, C3-12-알케닐-C5-C10-헤테로아릴- 및 C3-12-알키닐-C5-C10-헤테로아릴로부터 선택된 그룹이고; R8은 수소, 또는 C1-10-알킬, C3-10-알케닐, C3-10-알키닐, C3-6-사이클로알킬-C1-4-알킬, C3-6-사이클로알킬-C3-10-알케닐, C3-6-사이클로알킬-C3-10-알키닐, C5-6-사이클로알케닐-C1-4-알킬, C5-6-사이클로알케닐-C3-10-알케닐, C5-6-사이클로알케닐-C3-10-알키닐, C6-C14-아릴-C1-4-알킬, C6-C14-아릴-C3-10-알케닐- 및 C6-C14-아릴-C3-10-알키닐, C5-C10-헤테로아릴, C5-C10-헤테로아릴-C1-4-알킬, C5-C10-헤테로아릴-C1-4-알케닐, C5-C10-헤테로아릴-C1-4-알키닐, C1-4-알킬-O-C2-4-알킬, C1-4-알킬-O-C4-6-알케닐- 및 C1-4-알킬-O-C4-6-알키닐-로부터 선택된 임의로 치환된 그룹이고; R9는 수소, 또는 C1-12-알킬, C3-12-알케닐, C3-12-알키닐, C3-6-사이클로알킬-C1-12-알킬, C3-6-사이클로알킬-C3-12-알케닐, C3-6-사이클로알킬-C3-12-알키닐, C5-6-사이클로알케닐-C1-4-알킬, C5-6-사이클로알케닐-C3-10-알케닐, C5-6-사이클로알케닐-C3-10-알키닐, C6-C14-아릴-C1-12-알킬, C6-C14-아릴-C3-12-알케닐, C6-C14-아릴-C3-12-알키닐, C6-C14-아릴, C1-12-알킬-C6-C14-아릴, C2-12-알케닐-C6-C14-아릴, C2-12-알키닐-C6-C14-아릴, C5-C10-헤테로아릴, C5-C10-헤테로아릴-C1-12-알킬, C5-C10-헤테로아릴-C3-12-알케닐, C5-C10-헤테로아릴-C3-12-알키닐, C3-8-사이클로알킬, C5-8-사이클로알케닐, NR11R12-C3-8-사이클로알킬, NR11R12-C5-8-사이클로알케닐- 및 NR11R12-C5-8-사이클로알키닐로부터 선택된 임의로 치환된 그룹, 또는 3원 내지 8원 헤테로사이클릭 그룹 내에 하나 이상의 NR10 그룹을 함유하는 임의로 치환된 C3-8-헤테로사이클로알킬-(CH2)q 그룹이고, 또는 R8과 R9는 함께, O 원자 또는 S(O)p 그룹을 임의로 함유하는 포화 또는 불포화 4원 내지 7원 알킬 브릿지를 형성하고, 여기서 p 및 q는 서로 독립적으로 0, 1 또는 2이고, 또는 NR8R9는 추가의 N 원자를 임의로 함유하고 R10, NR11R12 및 NR11R12C1-4-알킬로부터 선택된 그룹에 의해 임의로 치환된 5원 내지 6원 헤테로사이클릭 그룹 또는 그룹 [이미지]이고, 여기서 z, q, g 및 d는 서로 독립적으로 1, 2 또는 3이고; R10 은 수소, 또는 C1-10-알킬, C3-10-알케닐, C3-10-알키닐, C3-7-사이클로알킬-C1-10-알킬, C3-7-사이클로알킬-C3-10-알케닐, C3-7-사이클로알킬-C3-10-알키닐, C3-7-사이클로알킬, C1-6-알킬-C3-7-사이클로알킬, C2-4-알케닐-C3-7-사이클로알킬, C2-4-알키닐-C3-7-사이클로알킬, 테트라하이드로피라닐 및 (NR4)2CH-C1-10-알킬로부터 선택된 임의로 치환된 그룹이고; R11 및 R12는 동일하거나 상이할 수 있고, 수소, 또는 C1-10-알킬, C3-10-알케닐, C3-10-알키닐, C3-6-사이클로알킬-C1-4-알킬- 및 C3-6-사이클로알킬로부터 선택된 임의로 치환된 그룹이고, 또는 R11과 R12는 함께 헤테로원자를 임의로 함유하는 치환된 4원 내지 7원 알킬 쇄를 형성하고; R13은 F, Cl, Br, OH, CN, CF3, CHF2 또는 C1-4-알킬-O이고; R14는 NR11R12, 또는 3원 내지 8원 헤테로사이클릭 그룹 내에 하나 이상의 NR10 그룹을 함유하는 임의로 치환된 C3-8-헤테로사이클로알킬-(CH2)q 그룹이고, 또는 R13과 R14는 함께 O 원자 또는 S(O)p 그룹을 임의로 함유하는 포화 또는 불포화 4원 내지 7원 알킬 브릿지를 형성한다.