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US 9,751,843 B2Granted
Substituted uracils and use thereof
AssigneeBayer Pharma Aktiengesellschaft
InventorsChantal Fürstner, Jens Ackerstaff, Alexander Straub, Heinrich Meier, Hanna Tinel, Katja Zimmermann, Adrian Tersteegen, Dmitry Zubov, Raimund Kast, Jens Schamberger, Martina Schäfer
Life of this patent
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Abstract
Substituted uracil derivatives of the compound of Formula (I), processes for their preparation, their use alone or in combinations for treatment and/or prophylaxis of diseases, and their use for preparing medicaments for treatment and/or prophylaxis of diseases.
Claims10
A compound of the formula (I)
- in which
- R1 represents hydrogen or (C1-C4)-alkyl,
- R2 represents a group of the formula
- where
- * represents the point of attachment to the uracil nitrogen atom,
- A represents —CH2—, —CH2—CH2—, —O—CH2-## or oxygen, in which ## represents the point of attachment to the phenyl ring,
- m represents a number 0, 1 or 2,
- R8 represents hydrogen, halogen, difluoromethyl, trifluoromethyl, (C1-C4)-alkyl, difluoromethoxy, trifluoromethoxy or (C1-C4)-alkoxy,
- R9A represents hydrogen or deuterium,
- R9B represents hydrogen, deuterium or (C1-C4)-alkyl,
- R10 represents hydrogen, halogen, (C1-C4)-alkyl, difluoromethyl, trifluoromethyl, nitro or (C1-C4)-alkylthio,
- R11 represents hydrogen, halogen, (C1-C4)-alkyl, difluoromethyl, trifluoromethyl, nitro or (C1-C4)-alkylthio,
- R12 represents hydrogen or halogen,
- R13 represents hydrogen or halogen,
- R3 represents hydrogen,
- R4 represents hydrogen, halogen, (C1-C4)-alkyl or (C1-C4)-alkoxy,
- R5 represents (C1-C4)-alkyl, (C1-C4)-alkoxy, (C1-C4)-alkylthio, (C1-C4)-alkylsulfinyl, (C1-C4)-alkylsulfonyl or —N(R14R15),
- where (C1-C4)-alkyl may be substituted by 1 or 2 substituents independently of one another selected from the group consisting of halogen, hydroxy, 4- to 7-membered heterocyclyl, (C1-C4)-alkoxy, hydroxycarbonyl, (C1-C4)-alkoxycarbonyl, aminocarbonyl, mono-(C1-C4)-alkylaminocarbonyl and di-(C1-C4)-alkylaminocarbonyl,
- in which 4- to 7-membered heterocyclyl may be substituted by 1 or 2 halogen or oxo substituents,
- where (C1-C4)-alkoxy may be substituted by a substituent independently of one another selected from the group consisting of hydroxy, (C1-C4)-alkoxycarbonyl, amino, mono-(C1-C4)-alkylamino, di-(C1-C4)-alkylamino, aminocarbonyl, mono-(C1-C4)-alkylaminocarbonyl and di-(C1-C4)-alkylaminocarbonyl,
- where
- R14 represents (C1-C4)-alkyl, (C1-C4)-alkoxycarbonyl or (C1-C4)-alkylaminocarbonyl,
- in which (C1-C4)-alkyl may be substituted by hydroxy or (C1-C4)-alkoxy,
- and
- in which (C1-C4)-alkylaminocarbonyl may be substituted by hydroxy or (C1-C4)-alkoxy,
- R15 represents hydrogen or (C1-C4)-alkyl,
- or
- R5 represents 4- to 7-membered heterocyclyl or 5- to 6-membered heteroaryl,
- where 4- to 7-membered heterocyclyl may be substituted by 1 to 3 substituents independently of one another selected from the group consisting of halogen, trifluoromethyl, (C1-C4)-alkyl, hydroxy, oxo, amino and (C1-C4)-alkoxycarbonyl,
- in which (C1-C4)-alkyl may be substituted by 1 or 2 substituents independently of one another selected from the group consisting of halogen, hydroxy and —N(R16R17),
- in which R6 represents hydrogen, (C1-C4)-alkyl or (C1-C4)-alkylcarbonyl,
- in which R17 represents hydrogen or (C1-C4)-alkyl,
- where 5- to 6-membered heteroaryl may be substituted by 1 or 2 substituents independently of one another selected from the group consisting of halogen, trifluoromethyl, (C1-C4)-alkyl, hydroxy, amino and (C1-C4)-alkoxycarbonyl,
- in which (C1-C4)-alkyl may be substituted by 1 or 2 substituents independently of one another selected from the group consisting of halogen, hydroxy and —N(R16R17),
- in which R16 represents hydrogen, (C1-C4)-alkyl or (C1-C4)-alkylcarbonyl,
- in which R17 represents hydrogen or (C1-C4)-alkyl,
- R6 represents hydrogen, halogen, cyano, (C1-C4)-alkyl or (C1-C4)-alkoxy,
- R7 represents hydrogen, halogen, (C1-C4)-alkyl or (C1-C4)-alkoxy, a salt or a solvate thereof, or a solvate of the salt.
35 more elements
Dependencies are inferred from the claim text.