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US 7,582,665 B2Granted
Compounds exhibiting thrombopoietin receptor agonism
AssigneeShionogi & Co., Ltd.
InventorsHiroshi Takemoto, Takeshi Shiota, Masami Takayama
Life of this patent
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Abstract
Pharmaceutical compositions containing as an active ingredient compounds of the general formula (I), prodrugs of the same, pharmaceutically acceptable salts of both, or solvates of them and exhibiting thrombopoietin receptor agonism: X1—Y1-Z1-W1 (I) wherein X1 is optionally substituted aryl, optionally substituted heteroaryl or the like; Y1 is —NRACO—(CH2)0-2— or the like (wherein RA is a hydrogen or the like); Z1 is optionally substituted phenylene or the like; and W1 is a group represeted by the below formula: wherein R1, R2, R3, and R4 are each independently a hydrogen atom, optionally substituted lower alkyl or the like, a broken line ( - - - ) represents the presence or absence of bond.
Claims6
A compound represented by the general formula (III):
- wherein R16 is a hydrogen atom, optionally substituted lower alkyl, carboxy, lower alkyloxycarbonyl, halogen atom, or optionally substituted aminocarbonyl;
- R17, R18, R19, R20, and R21 are each independently a hydrogen atom, optionally substituted lower alkyl by one or more substituent(s) selected from substituent group B, cycloalkyl, optionally substituted alkyoxy by one or more substituent(s) selected from substituent group B, alkylthio, halogen atom, optionally substituted phenyl by one or more halogen atoms, optionally substituted heteroaryl by one or more halogen atoms, or optionally substituted nonaromatic heterocyclic group by one or more halogen atoms;
- substituent group B consists of hydroxy, alkyloxy, halogen atom, carboxy, lower alkyloxycarbonyl, aryloxycarbonyl, optionally substituted amino wherein the substituent is an alkyl, phenyl, non-aromatic heterocyclic group, or heteroaryl;
- or
- R16 and R17 taken together may form —CH2—, —CH2CH2—, —CH2CH2CH2—, —OCH2—, or —SCH2—;
- R31 and R32 are each independently a hydrogen atom, lower alkyl, halogen atom, halo(lower)alkyl, lower alkyloxy, halo(lower)alkyloxy, or hydroxy;
- W3 is represented by the formula:
- wherein R13 is a hydrogen atom, lower alkyl, lower alkyloxy, lower alkylthio, or halogen atom;
- R14 and R15 are each independently a hydrogen atom, or optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl, optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, or optionally substituted non-aromatic heterocyclic group, each substituted by one or more substituent(s) selected from substituent group A;
- substituent group A consists of a halogen atom, halo(lower)alkyl, optionally substituted amino, carboxy, lower alkylthio, lower alkylsilyl, or lower alkyloxy;
- R24 is a hydrogen atom or lower alkyl;
- R25 is lower alkyl, optionally substituted aryl, or optionally substituted non-aromatic heterocyclic group;
- A3 is heteroaryl;
- or pharmaceutically acceptable salts thereof.
11 more elements
A compound represented by the general formula (IV-A):
- wherein R27 is a hydrogen atom, C1-C3 alkyl, trifluoromethyl, or halogen atom;
- R28, R29, and R30 are independently a hydrogen atom, optionally substituted lower alkyl by one or more substituent(s) selected from substituent group B, cycloalkyl, optionally substituted alkyoxy by one or more substituent(s) selected from substituent group B, alkylthio, halogen atom, optionally substituted phenyl by one or more halogen atoms, optionally substituted heteroaryl by one or more halogen atoms, or optionally substituted nonaromatic heterocyclic group by one or more halogen atoms;
- substituent group B consists of hydroxy, alkyloxy, halogen atom, carboxy, lower alkyloxycarbonyl, aryloxycarbonyl, optionally substituted amino wherein the substituent is an alkyl, phenyl, non-aromatic heterocyclic group, or heteroaryl;
- R31 and R32 are each independently a hydrogen atom, lower alkyl, halogen atom, halo(lower)alkyl, lower alkyloxy, halo(lower)alkyloxy, or hydroxy;
- W4 is a group represented by the formula:
- wherein R13 is a hydrogen atom, lower alkyl, lower alkyloxy, lower alkylthie, or halogen atom;
- R14 and R15 are each independently a hydrogen atom, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl, optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, or optionally substituted non-aromatic heterocyclic group, each substituted by one or more substituent(s) selected from substituent group A,
- substituent group A consists of a halogen atom, halo(lower)alkyl, optionally substituted amino, carboxy, lower alkylthio, lower alkylsilyl, or lower alkyloxy;
- R24 is a hydrogen atom or lower alkyl;
- or pharmaceutically acceptable salts thereof.
7 more elements
Dependencies are inferred from the claim text.