JP6970114B2 - ベンゼンスルホニル非対称尿素とその医学的利用 - Google Patents
ベンゼンスルホニル非対称尿素とその医学的利用 Download PDFInfo
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- JP6970114B2 JP6970114B2 JP2018549890A JP2018549890A JP6970114B2 JP 6970114 B2 JP6970114 B2 JP 6970114B2 JP 2018549890 A JP2018549890 A JP 2018549890A JP 2018549890 A JP2018549890 A JP 2018549890A JP 6970114 B2 JP6970114 B2 JP 6970114B2
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- C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
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Description
本発明は、新規な非対称尿素化合物と、その医学的利用、特にグレリン受容体によって調節される病状を処置するときの医学的利用に関する。
成長ホルモン分泌促進受容体(GHS-R)は、多数の生理学的プロセス(その中には成長ホルモン(GH)放出、代謝、食欲が含まれる)を調節している。グレリン(胃の中にある内分泌細胞によって主に産生されて循環するホルモン)は、その内在性リガンドである。グレリンは28個のアミノ酸からなるペプチドであり、生物活性であるにはアシル側鎖を必要とする(Kojima他、Nature、第402巻、656〜660ページ、1999年)。グレリンは成長ホルモン(GH)の放出を促進することと、中枢に投与されたときと末梢に投与されたときの両方で食事の摂取を増加させることが示されている(Wren他、Endocrinology、第141巻、4325〜4328ページ、2000年)。
本発明の発明者は、精力的な研究と実験を通じ、グレリン受容体に対する逆アゴニスト活性を有する一連の新規な化合物を予期せず発見するに至った。
本発明の化合物、組成物、物品、装置、方法を開示して説明する前に、これらは、特に断わらない限り、具体的な合成法または具体的な処置法に限定されないことや、特に断わらない限り、特定の試薬に限定されないことを理解すべきである。そのためこれらはもちろん変更することができる。本明細書で用いる用語は個々の実施態様を説明することだけを目的としているため、制限することは意図していないことも理解すべきである。
点線は、場合によっては存在する結合を表わし;
Wは、C、N、Oのいずれかであり;
Xは、結合、CO、CR7R8のいずれかであり;
kは0〜2であり;
Rは、C1-6アルキルまたはCy1であり、そのC1-6アルキルまたはCy1は、場合によっては、ハロ、ヘテロアリール、C1-6アルコキシ、C1-6アルキル、ヘテロシクロアルキル、CO2(C1-6アルキル)、CO(C1-6アルキル)から選択された1〜3個の置換基で置換されており;
R1とR2は、それぞれ独立に、H、C1-3アルキル、メトキシ、ハロ、OHのいずれかであり、
あるいはR1とR2は、それらが結合している原子と合わさって5〜6員の環を形成し;
あるいはR1とXは、それらが結合している原子と合わさって5〜6員の環を形成し;
あるいはR1とXとRは、それらが結合している原子と合わさって二環構造を形成し;
R3は、H、C1-3アルキル、メトキシ、ハロ、OH、COOR12、CR13R14OH、COHNR15、シクロアルキル、ヘテロアリールのいずれかであり;
R4は、結合、NR6、CR9R10のいずれかであり;
あるいはR3とR4は、それらが結合している原子と合わさって3〜6員の環を形成し;
R5は、Cy2、CO(C1-6アルキル)、C1-6アルキルのいずれかであり、そのCy2、CO(C1-6アルキル)、C1-6アルキルは、場合によっては、ハロ、C1-6アルキルアミン、COR11、SO2R11、ヘテロシクロアルキル、CO2R11、C1-6ヒドロキシアルキル、ヘテロアリール、CH2CO2R11、C1-6アルコキシ、OH、CN、R11、CH2OSO3H、ベンジル、CH2SO3H、CH2CN、NHCH2シクロアルキルから選択された1〜3個の置換基で置換されており;
R6は、結合、H、CH3のいずれかであり;
R7とR8は、それぞれ独立に、H、C1-3アルキル、CONH2のいずれかであり、そのC1-3アルキルは、場合によってはハロで置換されており;
R9とR10は、それぞれ独立に、HまたはC1-3アルキルであり、そのC1-3アルキルは、場合によってはハロで置換されており;
R11は、H、NH2、場合によっては置換されたC1-6アルキルのいずれかであり;
R12は、HまたはC1-3アルキルであり;
R13とR14は、それぞれ独立に、HまたはC1-3アルキルであり;
R15は、HまたはC1-3アルキルである。
X、W、R1〜R4、kは上に定義した通りであり;
Cy1は、アリール、ヘテロアリール、シクロアルキル、ヘテロシクロアルキルからなる群から選択された環状部分であり、その環状部分は、場合によっては、ハロ、ヘテロアリール、C1-6アルコキシ、C1-6アルキル、ヘテロシクロアルキル、CO2(C1-6アルキル)、CO(C1-6アルキル)から選択された1〜3個の置換基で置換されており;
Cy2は、アリール、ヘテロアリール、シクロアルキル、ヘテロシクロアルキルからなる群から選択された環状部分であり、その環状部分は、場合によっては、ハロ、C1-6アルキルアミン、COR11、SO2R11、ヘテロシクロアルキル、CO2R11、C1-6ヒドロキシアルキル、ヘテロアリール、CH2CO2R11、C1-6アルコキシ、OH、CN、R11、CH2OSO3H、ベンジル、CH2SO3H、CH2CN、NHCH2シクロアルキルから選択された1〜3個の置換基で置換されている。
X、R1〜R4、kは上に定義した通りであり;
点線は、場合によっては存在する結合を表わし;
Uは、C、N、S、Oのいずれかであり;
Bは、5〜7員の環構造または二環構造であり、その5〜7員の環構造または二環構造は、場合によっては、COR11、SO2R11、ヘテロシクロアルキル、CO2R11、C1-6ヒドロキシアルキル、ヘテロアリール、CH2CO2R11、C1-6アルコキシ、OH、CN、R11、CH2OSO3H、ベンジル、CH2SO3H、CH2CNのいずれかで置換されており;
Yは、それぞれ独立にCまたはNであり;
Zは、ハロ、メトキシ、場合によってはハロで置換されたC1-3アルキルのいずれかであり;
R'は、ハロ、ヘテロアリール、C1-6アルコキシ、C1-6アルキル、ヘテロシクロアルキル、CNシクロアルキル、CO2(C1-6アルキル)、CO(C1-6アルキル)のいずれかであり;
あるいは2つのR'は、それらが結合している原子と合わさって5〜6員の環を形成し;
lは0〜3であり;
mは0〜3であり;
nは0〜3である。
H0937の合成
H1027とH1071の合成
H1060の合成
H1148とH1194の合成
1.試験化合物貯蔵溶液:10 mMのデキストロメトルファン(Dtr)を含むDMSO溶液、10 mMのジフェンヒドラミン(DPA)を含むDMSO溶液、10 mMのオメプラゾール(Ome)を含むDMSO溶液、10 mMのベラパミル(Ver)を含むDMSO溶液、10 mMの逆アゴニスト化合物を含むDMSO溶液を、アセトニトリル/水(70/30)を用いてそれぞれ0.25 mM溶液に希釈する。
2.緩衝液:pH7.4の100 mMリン酸カリウム緩衝液(PBS)
3.肝臓ミクロソーム(20 mg/ml):37℃の水浴の中で素早く解凍する
4.2000μlのNADPH再生系(1.3 mM)。使用する前にこの系を氷の上に置く:
330μlの100 mM G6P
1300μlの10 mM NADP
5μlの1200 U/ml G6PD
365μlのPBS緩衝液
5.クエンチ溶液:LC-MS/MS分析のための、ISを含むアセトニトリル。
Claims (23)
- 式(IV):
(ただしこの式において、
点線は、場合によっては存在する結合を表わし;
Xは、結合、CO、または、CR7R8であり;
kは、0〜2であり;
Zは、ハロ、メトキシ、または、ハロで置換されてもよいC1-3アルキルであり;
R1とR2は、それぞれ独立に、H、C1-3アルキル、メトキシ、ハロ、または、OHであり、
あるいはR1とR2は、それらが結合している原子と合わさって5〜6員の環を形成し;
あるいはR1とXは、それらが結合している原子と合わさって5〜6員の環を形成し;
R3は、H、C1-3アルキル、メトキシ、ハロ、OH、COOR12、CR13R14OH、COHNR15、シクロアルキル、または、ヘテロアリールであり;
R4は、結合、または、CR9R10であり;
Uは、C、N、S、またはOであり;
R’は、ハロ、ヘテロアリール、C1-6アルコキシ、C1-6アルキル、ヘテロシクロアルキル、CNシクロアルキル、CO2(C1-6アルキル)、または、CO(C1-6アルキル)であり;
あるいは、2つのR’はそれらが結合している原子と合わさって5〜6員の環を形成し;
R7とR8は、それぞれ独立に、H、C1-3アルキル、CONH2のいずれかであり、そのC1-3アルキルは、場合によってはハロで置換されており;
R9とR10は、それぞれ独立に、HまたはC1-3アルキルであり、そのC1-3アルキルは、場合によってはハロで置換されており;
R12、R13、R14、およびR15は、それぞれ独立に、HまたはC1-3アルキルであり;
R16は、HまたはC1-3アルキルであり;
R17は、H、ハロ、またはC1-3アルキルであり;
lは0〜3であり;
mは0〜3であり;
nは0〜3であ;
pは1〜3である)。 - pが1又は2である、請求項1に記載の化合物。
- グレリン受容体に病態生理学的に関連する疾患を治療および/または予防するための医薬の製造のための、請求項1〜21のいずれか1項に記載の式(IV)の化合物の使用。
- グレリン受容体に病態生理学的に関連する疾患を治療および/または予防するための、請求項1〜21のいずれか1項に記載の式(IV)の化合物を含む医薬組成物。
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