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US 9,751,842 B2Granted
Phthalazine derivatives
AssigneeMarck Patent GmbH
InventorsHans-Peter Buchstaller, Dieter Dorsch, Christina Esdar, Birgitta Leuthner
Life of this patent
Estimating the term…
Abstract
Compounds of the formula I in which R1, X and n have the meanings indicated in Claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.
Claims20
A compound of formula I
- in which
- R1 is H, Hal, CH3, OCH3 or CH2OH,
- X is Ar or Cyc,
- Ar is phenyl, biphenyl or naphthyl, each of which is unsubstituted or mono-, di- or trisubstituted by Hal, NO2, CN, A, [C(R2)2]pOR2, S(O)mR2, [C(R2)2]pN(R2)2, [C(R2)2]pCOOR2, [C(R2)2]pCON(R2)2, [C(R2)2]pSO2N(R2)2, NR2COR2, NR2SO2R2, NR2CON(R2)2, NHCOOA, O[C(R2)2]nN(R2)2, CHO and/or COA,
- R2 is H or A,
- A is unbranched or branched alkyl with 1-10 C-atoms, wherein two adjacent carbon atoms optionally form a double bond and/or one or two non-adjacent CH- and/or CH2-groups are optionally replaced by N-, O- and/or S-atoms and wherein 1-7 H-atoms are optionally replaced by F, Cl and/or OH,
- Cyc is cycloalkyl with 3, 4, 5, 6 or 7 C-atoms,
- Hal is F, Cl, Br or I,
- m is 0, 1 or 2,
- n is 1, 2 or 3, and
- p is 0, 1, 2, 3 or 4,
- or a pharmaceutically acceptable salt, solvate, tautomer or stereoisomer thereof.
9 more elements
A compound, which is one of the following compounds
- No.
- Name
- “A1”
- 2-phenyl-N-phthalazin-1-yl-acetamide
- “A2”
- 2-(3-methoxyphenyl)-N-phthalazin-1-yl-acetamide
- “A3”
- 2-(4-methoxyphenyl)-N-phthalazin-1-yl-acetamide
- “A4”
- 2-(4-ethoxyphenyl)-N-phthalazin-1-yl-acetamide
- “A5”
- N-phthalazin-1-yl-2-(3-trifluoromethoxyphenyl)-acetamide
- “A6”
- 2-(3-cyanophenyl)-N-phthalazin-1-yl-acetamide
- “A7”
- 2-(3-nitrophenyl)-N-phthalazin-1-yl-acetamide
- “A8”
- N-phthalazin-1-yl-2-(4-trifluoromethoxyphenyl)-acetamide
- “A9”
- 2-(4-tert-butylphenyl)-N-phthalazin-1-yl-acetamide
- “A10”
- 2-(2,6-dichlorophenyl)-N-phthalazin-1-yl-acetamide
- “A11”
- 2-(4-ethoxy-phenyl)-N-(5-fluoro-phthalazin-1-yl)-acetamide
- “A12”
- N-(5-fluoro-phthalazin-1-yl)-2-(4-methoxy-phenyl)-acetamide
- “A13”
- 3-cyclohexyl-N-phthalazin-1-yl-propionamide
- “A14”
- 3-phenyl-N-phthalazin-1-yl-propionamide
- “A15”
- 3-cyclopentyl-N-phthalazin-1-yl-propionamide
- “A16”
- 3-(2-chloro-phenyl)-N-phthalazin-1-yl-propionamide
- “A17”
- 3-(2,3-dichloro-phenyl)-N-phthalazin-1-yl-propionamide
- “A18”
- N-(8-methyl-phthalazin-1-yl)-2-phenyl-acetamide
- “A19”
- N-(5-methyl-phthalazin-1-yl)-2-phenyl-acetamide
- “A20”
- 2-(4-methoxy-phenyl)-N-(8-methyl-phthalazin-1-yl)-acetamide
- “A21”
- 2-(4-methoxy-phenyl)-N-(5-methyl-phthalazin-1-yl)-acetamide
- “A22”
- 3-cyclohexyl-N-(8-methyl-phthalazin-1-yl)-propionamide
- “A23”
- 3-phenyl-N-(8-methyl-phthalazin-1-yl)-propionamide
- “A24”
- 3-cyclopentyl-N-(8-methyl-phthalazin-1-yl)-propionamide
- “A25”
- 3-(2-chlorophenyl)-N-(8-methyl-phthalazin-1-yl)-propionamide
- or
- “A26”
- 3-(2,3-dichlorophenyl)-N-(8-methyl-phthalazin-1-yl)-
- propionamide
- or a pharmaceutically acceptable salt, solvate, tautomer or stereoisomer thereof.
54 more elements
Dependencies are inferred from the claim text.