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US 2016/0244444 A1Published application
Novel tetrahydropyridopyrimidine compound or salt thereof
AssigneeTaiho Pharmaceutical Co., Ltd.
InventorsKazuhisa MINAMIGUCHI, Shigeo OKAJIMA, Shinichi AOKI, Masanori ASAI, Takahiro ASAI, Hiroyoshi YAMANAKA, Suguru DOHI
Life of this patent
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Abstract
To provide a compound having an inhibitory activity for an androgen receptor. A tetrahydropyridopyrimidine compound represented by the following general formula (I) or a pharmaceutically acceptable thereof (in the formula, X and R are as defined in the specification).
Claims21
A tetrahydropyridopyrimidine compound represented by formula (I):
- wherein, in the formula (I),
- X is a halogen atom or a halogeno-C1-3 alkyl group;
- R is a C6-14 aryl group which is substituted with R1 and is optionally substituted simultaneously with R2, or a 5- or 6-membered heteroaryl group which is substituted with R1 and is optionally substituted simultaneously with R2;
- R1 is a hydrogen atom, a phenyl group, a hydroxy-C1-6 alkyl group, a hydroxy-C3-7 cycloalkyl group, a C1-6 alkoxy group which may be substituted with Ra, a C3-7 cycloalkylaminosulfonyl group, a 3- to 7-membered monocyclic heterocycloalkylsulfonyl group, a halogeno-C1-3 alkoxycarbonylamino group, a halogeno-C1-3 alkylcarbonylamino group, a 3- to 7-membered monocyclic heterocycloalkanecarbonyl group substituted with a hydroxy-C1-6 alkyl group, or —(CH2)n—C(═O)—NHRf;
- R2 is a hydrogen atom, a halogen atom, or a halogeno-C1-3 alkyl group;
- Ra is a C1-6 alkylpyrazolyl group, a triazolyl group, a tetrazolyl group, or a C1-6 alkylsulfonylpiperazinyl group;
- Rf is a halogeno-C1-3 alkyl group, a hydroxy-C1-6 alkyl group, a hydroxy-C3-7 cycloalkyl group, a hydroxy-C3-7 cycloalkyl-C1-6 alkyl group, or a C1-6 alkyl group substituted with Rfa;
- Rfa is a C1-6 alkylpyrazolyl group, a halogeno-C1-3 alkylthiazolyl group, an oxadiazolyl group, or a halogeno-C1-3 alkyloxadiazolyl group;
- and
- n is an integer of from 0 to 3,
- or a pharmaceutically acceptable salt thereof.
8 more elements
11-13. (canceled)
15-20. (canceled)
Dependencies are inferred from the claim text.