Title:
チアジアゾールウレア誘導体の使用
Document Type and Number:
Japanese Patent JP2007523922
Kind Code:
A
Abstract:
1,3,4-Thiadiazole derivatives (I) are used to prepare medicaments for preventing or treating diseases in which the inhibition, regulation or modulation of kinase signal transduction plays a role. 1,3,4-Thiadiazole derivatives of formula (I) and their derivatives, solvates, salts and stereoisomers are used to prepare medicaments for preventing or treating diseases in which the inhibition, regulation or modulation of kinase signal transduction plays a role. Ar 1>phenyl, naphthyl, biphenylyl or Het, all optionally substituted with 1-4 of R 1>; Ar 2>phenyl, naphthyl, biphenylyl or Het, all optionally substituted with 1-4 of R 2>; Y : O, S, CHNO 2, C(CN) 2 or NR 4>; Z : O, S, CH 2(CH 2) n, (CH 2) nCHA, CHA(CH 2) n; CO, CHOH, (CHA) nO, (CH 2) nO, O(CHA) n, O(CH 2) n, (CH 2) nS, S(CH 2) n, (CH 2) nNH, NH(CH 2) n, (CH 2) nNA, NA(CH 2) n, CHHal or C(Hal) 2; Het : mono- or bicyclic heteroaryl with 1-4 N, O and/or S atoms; R 1>, R 2>A, Ar', OR 3>, SR 3>, OAr', SAr', N(R 3>) 2, NHAr', Hal, NO 2, CN, (CH 2) nCOOR 3>, (CH 2) nCON(R 3>) 2, COR 3>, SO mA, SO mAr', NHCOA, NHCOAr', NHSO mA. NHSO mAr', SO mN(R 3>) 2, O(CH 2) nN(R 3>) 2, O(CH 2) nNHR 3>, O(CH 2) nNA 2, O(CH 2) nC(Me) 2(CH 2) nN(R 3>) 2, NH(CH 2) n(CH 2) 2(CH 2) nN(R 3>) 2, O(CH 2) nN(R 3>)SO mA, O(CH 2) nN(R 3>)SO mN(R 3>)A, O(CH 2) nN(R 3>)SO mAr', (CH 2) nN(R 3>)SO mA, (CH 2) nN(R 3>)SO mN(R 3>)A, (CH 2) nN(R 3>)SO mAr', O(CH 2) nSO mA, O(CH 2) nSO mN(R 3>)A, O(CH 2) nSO mAr', (CH 2) nSO mA, (CH 2) nSO mN(R 3>)A, (CH 2) nSO mAr', NH(CH 2) nNH 2, NH(CH 2) nNHA, NH(CH 2) nNA 2, NA(CH 2) nNH 2, NA(CH 2) nNHA, NA(CH 2) nNA 2, O(CH 2) nHet 1> or Het 1>; R 3>H, A or (CH 2) nAr'; R 4>H, CN, OH, A, (CH 2) nAr', COR 3>, COAr', SO mA or SO mAr'; Ar' : phenyl optionally substituted with 1-5 of A, Ph, OH, OA, SH, SA, OPh, SPh, NH 2, NHA, NA 2, NHPh, Hal, NO 2, (CH 2) nCOOH, (CH 2) nCOOA, (CH 2) nCONH 2, (CH 2) nCONHA, CHO, COA, SO mA, SO mAPh, NHCOA, NHCOPh, NHSO 2A, NHSO 2Ph or SO 2NH 2; Ph : phenyl optionally substituted with 1-3 of A, Hal, CN, COOR (R is not defined), COOH, NH 2, NO 2, OH or OA; Het 1>monocyclic saturated heterocyclyl with 1-4 N, O and/or S atoms, optionally substituted with 1-3 of Hal, A, OA, (CH 2) nOH, (CH 2) nHal, NH 2, =NH, =NOH, =NOA and/or =O; A : 1-10C alkyl or haloalkyl; Hal : F, Cl, Br or I; n : 0-5; m : 0-2. Independent claims are also included for: (1) new compounds (I), namely 1-(2-methoxy-5-trifluoromethyl-phenyl)-3-(5-pyridin-4-ylmethyl-[1,3,4]thiadiazol-2-yl}-urea, 1-(5-chloro-2-methoxy-4-methyl-phenyl)-3-[5-(3,4-dimethoxybenzyl)-[1,3,4]thiadiazol-2-yl]-urea, 1-[5-(3,4-dimethoxybenzyl)-[1,3,4]thiadiazol-2-yl]-3-(3-trifluoromethoxy-phenyl)-urea, 1-[5-(1-phenyl-ethyl)-[1,3,4]thiadiazol-2-yl]-3-(3-trifluoromethylsulfonyl-phenyl)-urea, 1-[5-(3,4-dimethoxy-benzyl)-[1,3,4]thiadiazol-2-yl]-3-(2-methoxy-5-trifluoromethyl-phenyl)-urea, 1-[5-(1-phenyl-ethyl)-(1,3,4]thiadiazol-2-yl]-3-p-tolyl-urea, 1-(2-methoxy-5-methyl-phenyl)-3-[5-(1-phenyl-ethyl)-[1,3,4]thiadiazol-2-yl]-urea, 1-(3-chloro-4-methyl-phenyl)-3-(5-(1-phenyl-ethyl)-[1,3,4]thiadiazol-2-yl]-urea, 1-(5-chloro-2-methyl-phenyl)-3-[5-(1-phenyl-ethyl)-[1,3,4]thiadiazol-2-yl]-urea, 1-(3-chloro-2-methyl-phenyl)-3-[5-(1-phenyl-ethyl)-[1,3,4]thiadiazol-2-yl]-urea, 1-(5-chloro-2-methoxy-phenyl)-3-[5-(1-phenyl-ethyl)-[1,3,4]thiadiazol-2-yl]-urea, 1-[5-(1-phenyl-ethyl)-[1,3,4]thiadiazol-2-yl]-3-(3-trifluoromethyl-phenyl)-urea, 1-[5-(1-phenyl-ethyl)-[1,3,4]thiadiazol-2-yl]-3-(4-trifluoromethyl-phenyl)-urea, 1-[5-(3,4-dimethoxy-benzyl)-[1,3,4]thiadiazol-2-yl]-3-(2-methoxy-phenyl)-urea, 1-[5-(1-phenyl-ethyl)-[1,3,4]thiadiazol-2-yl]-3-(4-trifluoromethoxy-phenyl)-urea, 1-(4-fluoro-3-trifluoromethyl-phenyl)-3-[5-(1-phenyl-ethyl)-[1,3,4]thiadiazol-2-yl]-urea, 1-(4-chloro-3-trifluoromethyl-phenyl)-3-[5-(1-phenyl-ethyl)-[1,3,4]thiadiazol-2-yl]-urea, 1-[5-(2.3-dimethoxy-benzyl)-[1,3,4]thiadiazol-2-yl]-3-(4-trifluoromethoxy-phenyl)-urea, 1-[5-(2,3-dimethoxy-benzyl)-[1,3,4]thiadiazol-2-yl]-3-(2-trifluoromethoxy-phenyl)-urea, 1-(5-chloro-2,4-dimethoxy-phenyl)-3-[5-(3,4-dimethoxy-benzyl)-[1,3,4]thiadiazol-2-yl]-urea, 1-(2,4-dimethoxy-phenyl) -3-[5-(1-phenyl-ethyl)-[1,3,4]thiadiazol-2-yl]-urea, 1-(3-chloro-4-methoxy-phenyl)-3-[5-(1-phenyl-ethyl)-[1,3,4]thiadiazol-2-yl]-urea, 1-[2-(2-dimethylamino-ethoxy)-5-trifluoromethyl-phenyl]-3-[5-(1-phenyl-ethyl)-[1,3,4]thiadiazol-2-yl]-urea; (2) a process for preparing the new compounds (I); (3) kit comprising a compound (I) and another drug in separate packaging. [Image] ACTIVITY : Cytostatic; Antipsoriatic; Gynecological; Antiinflammatory; Vulnerary; Antiarthritic; Antibacterial; Antiulcer; Virucide; Immunosuppressive; Anti-HIV. No biological data given. MECHANISM OF ACTION : Kinase inhibitor.
Inventors:
Burgdorf Rals
Buchstal Hans Peter
Steaver frank
Anzari Zoheira
Ament christiane
Greiner Hartmut
Grell Matthias
Sielenberg Christian
Zenke frank
Buchstal Hans Peter
Steaver frank
Anzari Zoheira
Ament christiane
Greiner Hartmut
Grell Matthias
Sielenberg Christian
Zenke frank
Application Number:
JP2007500082A
Publication Date:
August 23, 2007
Filing Date:
January 31, 2005
Export Citation:
Assignee:
Merck Patent Gesellschaft mit beschraenkter Haftung
International Classes:
C07D285/12; A61K31/433; A61K31/4439; A61K31/454; A61P13/08; A61P15/08; A61P17/02; A61P17/06; A61P19/02; A61P29/00; A61P31/04; A61P31/16; A61P35/00; A61P37/00; A61P37/02; A61P43/00; C07D285/135; C07D413/12; C07D417/06; C07D417/12
Domestic Patent References:
| JP2006513192A | 2006-04-20 | |||
| JP2006522784A | 2006-10-05 |
Foreign References:
| WO2004058753A1 | 2004-07-15 | |||
| WO2004089929A1 | 2004-10-21 | |||
| WO1999020617A1 | 1999-04-29 |
Attorney, Agent or Firm:
Sadao Kumakura
Nobuo Ogawa
Atsushi Hakoda
Kenji Asai
Koji Hirayama
Nobuo Ogawa
Atsushi Hakoda
Kenji Asai
Koji Hirayama