JP5209670B2 - カリウムチャンネル機能のヘテロ環インヒビター - Google Patents
カリウムチャンネル機能のヘテロ環インヒビター Download PDFInfo
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- JP5209670B2 JP5209670B2 JP2010154061A JP2010154061A JP5209670B2 JP 5209670 B2 JP5209670 B2 JP 5209670B2 JP 2010154061 A JP2010154061 A JP 2010154061A JP 2010154061 A JP2010154061 A JP 2010154061A JP 5209670 B2 JP5209670 B2 JP 5209670B2
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- 0 CN(*)S(*)(=O)=O Chemical compound CN(*)S(*)(=O)=O 0.000 description 4
- NQRYJNQNLNOLGT-UHFFFAOYSA-N C1CCNCC1 Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 description 2
- RBFBGAGKJCPYMV-HFTWOUSFSA-N CC(C)(C)OC(N(CC1)CCC1(/C(/N(Cc(cc1)ccc1Cl)N)=N/N)c1ccccc1)=O Chemical compound CC(C)(C)OC(N(CC1)CCC1(/C(/N(Cc(cc1)ccc1Cl)N)=N/N)c1ccccc1)=O RBFBGAGKJCPYMV-HFTWOUSFSA-N 0.000 description 1
- SQTIADDQWCDEOL-UHFFFAOYSA-N CCC1(CCNCC1)NC(c(cccc1)c1OC)=O Chemical compound CCC1(CCNCC1)NC(c(cccc1)c1OC)=O SQTIADDQWCDEOL-UHFFFAOYSA-N 0.000 description 1
- QQYKXLISJDVQBS-UHFFFAOYSA-N CCC1=CCC(CCNC(C(Cc2ccccc2)(CC2)CCN2C2=NC=CCC2)=O)C=C1 Chemical compound CCC1=CCC(CCNC(C(Cc2ccccc2)(CC2)CCN2C2=NC=CCC2)=O)C=C1 QQYKXLISJDVQBS-UHFFFAOYSA-N 0.000 description 1
- RKJVWHJGEAJCAO-UHFFFAOYSA-N CCCS(N(CC1)[IH]CC1(CNC(c1ccccc1OC)=O)c1ccc[s]1)(=O)=O Chemical compound CCCS(N(CC1)[IH]CC1(CNC(c1ccccc1OC)=O)c1ccc[s]1)(=O)=O RKJVWHJGEAJCAO-UHFFFAOYSA-N 0.000 description 1
- HWTVJVGXJUQTTL-UHFFFAOYSA-N CCNC(c1ccccc1OC)=O Chemical compound CCNC(c1ccccc1OC)=O HWTVJVGXJUQTTL-UHFFFAOYSA-N 0.000 description 1
- YSPVHAUJXLGZHP-UHFFFAOYSA-N CCOC(N1CCCCC1)=O Chemical compound CCOC(N1CCCCC1)=O YSPVHAUJXLGZHP-UHFFFAOYSA-N 0.000 description 1
- SEMBPRKPNAEHIO-UHFFFAOYSA-N CCc1ccc(CCNC(C2(CC3=CC=CCC3)CCNCC2)=O)cc1 Chemical compound CCc1ccc(CCNC(C2(CC3=CC=CCC3)CCNCC2)=O)cc1 SEMBPRKPNAEHIO-UHFFFAOYSA-N 0.000 description 1
- KRKRIMYJLRJILS-UHFFFAOYSA-N CN(CCc1ccccc1)C(C(CC1)(CCN1C(CCc1ccccc1)=O)C1=CCCC=C1)=O Chemical compound CN(CCc1ccccc1)C(C(CC1)(CCN1C(CCc1ccccc1)=O)C1=CCCC=C1)=O KRKRIMYJLRJILS-UHFFFAOYSA-N 0.000 description 1
- HGLBLOJVEDHWIL-UHFFFAOYSA-N COc1ccccc1C(NCC(CC1)(CCN1S(NCC(F)(F)F)(=O)=O)c1ccc[s]1)=O Chemical compound COc1ccccc1C(NCC(CC1)(CCN1S(NCC(F)(F)F)(=O)=O)c1ccc[s]1)=O HGLBLOJVEDHWIL-UHFFFAOYSA-N 0.000 description 1
- MACLXMNKIOQBPX-UHFFFAOYSA-N COc1ccccc1C(NCC1(CCNCC1)c1ccc[s]1)=O Chemical compound COc1ccccc1C(NCC1(CCNCC1)c1ccc[s]1)=O MACLXMNKIOQBPX-UHFFFAOYSA-N 0.000 description 1
- CXMCTILHSSNMAO-UHFFFAOYSA-N Clc1ccc(C[n]2nnnc2Cc2ccccc2)cc1 Chemical compound Clc1ccc(C[n]2nnnc2Cc2ccccc2)cc1 CXMCTILHSSNMAO-UHFFFAOYSA-N 0.000 description 1
- IMWGJBWIPLEOCC-UHFFFAOYSA-N NS(N(CC1)CCC1(C(NCc1ccccc1)=O)c1ccccc1)(O)=O Chemical compound NS(N(CC1)CCC1(C(NCc1ccccc1)=O)c1ccccc1)(O)=O IMWGJBWIPLEOCC-UHFFFAOYSA-N 0.000 description 1
- KNNXHJSVWVCZOO-UHFFFAOYSA-N O=C(CC(CC1)(CCN1C(OCc1ccccc1)=O)c1ccccc1)NCc1ccccc1 Chemical compound O=C(CC(CC1)(CCN1C(OCc1ccccc1)=O)c1ccccc1)NCc1ccccc1 KNNXHJSVWVCZOO-UHFFFAOYSA-N 0.000 description 1
- MFEILWXBDBCWKF-UHFFFAOYSA-N O=C(CCc1ccccc1)Cl Chemical compound O=C(CCc1ccccc1)Cl MFEILWXBDBCWKF-UHFFFAOYSA-N 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
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- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/26—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
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- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
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- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
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- C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
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- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
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- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D211/64—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4 having an aryl radical as the second substituent in position 4
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- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/92—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
- C07D211/96—Sulfur atom
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- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
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- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
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- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
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- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
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- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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Description
mおよびpの合計が少なくとも2であるという条件で、mおよびpは独立して0、1、2または3であり;
Qは、NR1、O、S、S(O)またはS(O)2であり;
R1は、
R2は、ヘテロアリール、(ヘテロアリール)アルキル、アリール、(アリール)アルキル、ヘテロシクロ、(ヘテロシクロ)アルキル、アルキル、またはシクロアルキルであって、それらの内のいずれかは場合により独立して1つ以上の基T1、T2またはT3で置換され得て;
Jは、結合;場合により独立して1つ以上の基T1a、T2aもしくはT3aで置換されたC1〜4アルキレン;または、場合により独立して1つ以上の基T1a、T2aもしくはT3aで置換されたC1〜4アルケニレンであり;
R3は、
R4は、H、アルキル、ハロアルキル、アルケニル、アルキニル、シクロアルキル、ヘテロシクロ、アリール、(アリール)アルキル、またはヘテロアリールであって、それらの内のいずれかは場合により独立して1つ以上の基T1b、T2bまたはT3bで置換され得て;
R5は、
(a)−NR6aR7a、シアノ;または、
(b)ヘテロアリール、(ヘテロアリール)アルキル、アリール、(アリール)アルキル、アルキル、シクロアルキル、(シクロアルキル)アルキル、ヘテロシクロ、(ヘテロシクロ)アルキル、もしくはアルキル(それらの内のいずれかは場合により独立して1つ以上の基T1c、T2cまたはT3cで置換され得る)
であり;
R6、R6a、R7、R7a、R8、R8a、R8a1、R8a2およびR8a3は独立して、H、アルキル、ヒドロキシ、アルコキシ、アリールオキシ、ヘテロシクロオキシ、ヘテロアリールオキシ、(ヒドロキシ)アルキル、(アルコキシ)アルキル、(アリールオキシ)アルキル、(ヘテロシクロオキシ)アルキル、(ヘテロアリールオキシ)アルキル、(シアノ)アルキル、(アルケニル)アルキル、(アルキニル)アルキル、シクロアルキル、(シクロアルキル)アルキル、アリール、(アリール)アルキル、ヘテロアリール、(ヘテロアリール)アルキル、ヘテロシクロ、(ヘテロシクロ)アルキル、−C(O)R9、−CO2R9、−C(O)−NR9R10、または−NR9R10であって、その内のいずれかは場合により独立して1つ以上の基T1d、T2dまたはT3dで置換され得るか;
R6およびR7、またはR6aおよびR7aはそれらが結合する窒素原子と組み合わさって、場合により独立して1つ以上の基T1d、T2dまたはT3dで置換される4〜8員のヘテロシクロ環を形成し得るか;
R6またはR7の1つがR8、R8aまたはR9aの内の1つと組み合わさって、場合により独立して1つ以上の基T1d、T2dまたはT3dで置換された、飽和または不飽和の5〜8員環を形成し得るか;あるいは、
R6aまたはR7aの1つがR8a1と組み合わさって、場合により独立して1つ以上の基T1d、T2dまたはT3dで置換された飽和または不飽和の5〜8員環を形成し得て;
R8bは、H、アルキル、アリール、シアノ、ニトロ、アシル、または−SO2(アルキル)であって、該アルキル基およびアリール基は場合により独立して1つ以上の基T1d、T2dまたはT3dで置換され得て;
R8cは、H、アルキル、シクロアルキル、アルケニル、アルキニル、アリール、アリールアルキル、ヘテロシクロ、ヘテロアリール、アルコキシ、またはアリールオキシであって、その内のいずれかは場合により独立して1つ以上の基T1d、T2dまたはT3dで置換され得て;
R8dは、R4、COR4、CO2R4、SO2R4、CONR6R7、またはSO2NR6R7であり;
R9およびR10は独立して、H、アルキル、ヒドロキシ、アルコキシ、アリールオキシ、ヘテロシクロオキシ、ヘテロアリールオキシ、(ヒドロキシ)アルキル、(アルコキシ)アルキル、(アリールオキシ)アルキル、(ヘテロシクロオキシ)アルキル、(ヘテロアリールオキシ)アルキル、シクロアルキル、(シクロアルキル)アルキル、アリール、(アリール)アルキル、ヘテロアリール、(ヘテロアリール)アルキル、ヘテロシクロ、または(ヘテロシクロ)アルキルであって、その内のいずれかは場合により独立して1つ以上の基T1f、T2fまたはT3fで置換され得るか;あるいは、
R9およびR10はそれらが結合する窒素原子と組み合わさって、場合により独立して1つ以上の基T1f、T2fまたはT3fで置換され得る飽和または不飽和の環を形成し得て;
Wは、=NR8a1、=N−CO2R8a1、=N−COR8a1、=N−CN、=N−SO2R8a1、または
X1は、O、S、NR8a2、またはCH2であり;
Z、Z1およびZ2は独立して、=O、=S、=NR8a3、または=N−CNであり;
RXは、いずれかの利用可能な環内炭素原子と結合する1つ以上の任意の置換基であって、独立してTlg、T2gまたはT3gから選ばれ;
Tl−1g、T2−2gおよびT3−3gは各々独立して、
(1)水素またはT6
(ここで、T6は、
(i)アルキル、(ヒドロキシ)アルキル、(アルコキシ)アルキル、アルケニル、アルキニル、シクロアルキル、(シクロアルキル)アルキル、シクロアルケニル、(シクロアルケニル)アルキル、アリール、(アリール)アルキル、ヘテロシクロ、(ヘテロシクロ)アルキル、ヘテロアリール、もしくは(ヘテロアリール)アルキル;
(ii)それ自身同じかもしくは異なる基(i)の1つ以上で置換される基(i);または
(iii)Tl−1g、T2−2gおよびT3−3gの定義における以下の基(2)〜(13)の内の1つ以上(1〜3個が好ましい)によって独立して置換される基(i)もしくは(ii)
である);
(2)−OH、もしくは−OT6;
(3)−SH、もしくは−ST6;
(4)−C(O)tH、−C(O)tT6、もしくは−O−C(O)T6(ここで、tは1または2である);
(5)−SO3H、−S(O)tT6、もしくはS(O)tN(T9)T6;
(6)ハロ;
(7)シアノ;
(8)ニトロ;
(9)−T4−NT7T8;
(10)−T4−N(T9)−T5−NT7T8;
(11)−T4−N(T10)−T5−T6;
(12)−T4−N(T10)−T5−H;または、
(13)オキソ
であり;
T4およびT5は各々独立して、
(1)単結合;
(2)−T11−S(O)t−Tl2−;
(3)−T11−C(O)−T12−;
(4)−T11−C(S)−T12−;
(5)−T11−O−T12−;
(6)−T11−S−T12−;
(7)−T11−O−C(O)−T12−;
(8)−T11−C(O)−O−T12−;
(9)−T11−C(=NR9a)−O−T12−;または、
(10)−T11−C(O)−C(O)−T12−
であり;
T7、T8、T9およびT10は、
(1)各々独立して、水素またはT6の定義において示す基であり;
(2)T7およびT8は一緒になってアルキレンまたはアルケニレンであり得て、それらが結合する原子と一緒になって3〜8員の飽和または不飽和の環(該環は、無置換であるか、またはT1−1g、T2−2gおよびT3−3gの定義において示す1つ以上の基で置換される)を完成し得て;
(3)T7またはT8はT9と一緒になってアルキレンまたはアルケニレンであり得て、それらが結合する窒素原子と一緒になって3〜8員の飽和または不飽和の環(該環は、無置換であるか、またはT1−1g、T2−2gおよびT3−3gの定義において示す1つ以上の基で置換される)を完成し得て;あるいは、
(4)T7およびT8またはT9およびT10はそれらが結合する窒素原子と組み合わさって基−N=CT13T14を形成し得て、ここで、該T13およびT14は各々独立してHまたはT6の定義において示す基であり;そして、
T11およびT12は各々独立して、
(1)単結合;
(2)アルキレン;
(3)アルケニレン;または、
(4)アルキニレン
である。
Qは、NR1またはOであり;
R1は、H、
R2は、アリール、(アリール)アルキル、またはヘテロアリールであって、それらの内のいずれかは場合により独立して1つ以上のT1、T2またはT3で置換され得て;
Jは、結合またはメチレンであり;そして、
R3は、R5、
Qは、NR1であり;
R1は、H、
R2は、アリール、(アリール)アルキル、またはヘテロアリール(特に、アリールはフェニルであり、そしてヘテロアリールはチオフェニルである)であって、その内のいずれかは場合により独立して1つ以上のT1、T2またはT3で置換され得て;
Jは、結合またはメチレンであり;そして、
R3は、R5、
R4は、アルキル、アルケニル、アルキニル、シクロアルキル、ヘテロシクロ、アリール、(アリール)アルキル、ヘテロアリール、または(ヘテロアリール)アルキルであって、それらの内のいずれかは場合により独立して1つ以上のT1b、T2bまたはT3bで置換され得て;
R5は、
(a)−NR6aR7a;または、
(b)アリール、(アリール)アルキル、ヘテロアリール、(ヘテロアリール)アルキル、ヘテロシクロ、もしくは(ヘテロシクロ)アルキル(それらの内のいずれかは場合により独立して1つ以上のT1c、T2cまたはT3cで置換され得る)であり;
R6、R6a、R7およびR7aは独立して、H、アルキル、アルケニル、アルキニル、アリール、(アリール)アルキル、(アルコキシ)アルキル、シクロアルキル、(シクロアルキル)アルキル、(ヒドロキシ)アルキル、ヘテロアリール、(ヘテロアリール)アルキル、ヘテロシクロ、(ヘテロシクロ)アルキル、(アリールオキシ)アルキル、−C(O)R9、−CO2R9、または−C(O)−NR9R10であって、その内のいずれかは場合により独立して1つ以上のT1c、T2cまたはT3cで置換され得るか;あるいは、
R6およびR6a、またはR7およびR7aはそれらが結合する窒素原子と組み合わさって、場合により置換された4〜8員環ヘテロ環(例えば、
R8aは、H、アルキル、または(アリール)アルキルであり;
R8cは、
(a)アルキル、アリール、ヘテロアリール(それらの内のいずれかは場合により独立して1つ以上のT1c、T2cまたはT3cで置換され得る);
(b)−NR9R10、
であり;
Wは、=N−CNであり;
Z1は、=Oまたは=N−CNであり;そして、
T、T1b、T1c、T1d、T2、T2b、T2c、T2d、T3、T3b、T3cおよびT3dは独立して、ハロ、シアノ、アルキル、アリール、(アリール)アルキル、ヘテロアリール、(ヘテロアリール)アルキル、ハロアルキル、−OH、−OT6、−C(O)tT6、−SO2T6、−T4NT7T8、または−T4N(T10)T5−T6である。
を得ることができる。カルボン酸または酸クロリドに加えて、当該分野の当業者は、化合物4のピペリジン窒素原子を多数の他の容易に入手可能な原料物質と反応させて、式Iの化合物を得ることができることを認めるであろう。例えば、化合物4は、酸スカベンジャーの存在下でスルホニルクロリド(例えば、R8SO2Cl)と反応させて、式Iの化合物(式中、QはNR1であって、そしてR1は、式:
を得ることができる。化合物4はイソシアネート(例えば、R7R6NCO)と反応させて、式Iの化合物(式中、QはNR1であって、そしてR1は、式:
本発明の範囲内にある化合物は、電位依存性K+チャンネルのK1サブファミリーを阻害し、そしてこのものは例えば、以下の様々な疾患の治療および/または予防において有用である。該疾患としては例えば、心不整脈(例えば、上室性不整脈、心房性不整脈、心房粗動、心房細動、心臓虚血の合併症、心拍数コントロール薬物としての使用を含む);狭心症(例えば、プリンツメタル(Prinzmetal's)症状、血管攣縮性症状および変形症状の軽減を含む);胃腸管疾患(例えば、逆流性食道炎(esauphagitis)、機能性消化不良、運動障害(例えば、便秘および下痢を含む)、および過敏性大腸症候群を含む);血管および内臓平滑筋の障害(例えば、喘息、慢性閉塞性肺疾患、成人呼吸窮迫症候群、末梢血管疾患(例えば、間欠性跛行(claudication)を含む)、静脈機能不全、インポテンス、大脳および冠状動脈の攣縮、並びにレイノー病を含む);炎症性疾患および免疫学的な疾患(例えば、炎症性腸疾患、関節リウマチ、移植片拒絶反応、喘息、慢性閉塞性肺疾患、のう胞性線維症、およびアテローム硬化症を含む);細胞増殖性疾患(例えば、再狭窄および癌(例えば、白血病を含む);聴覚系の疾患;視覚系の疾患(例えば、黄斑変性症および白内障を含む);糖尿病(例えば、糖尿病網膜症、糖尿病腎障害、および糖尿病神経障害を含む);筋肉障害(例えば、筋緊張症および萎縮病を含む);末梢系神経障害;認知障害;偏頭痛;記憶喪失(例えば、アルツハイマー疾患および痴呆を含む);CNS媒介性運動機能不全(例えば、パーキンソン疾患および運動失調を含む);癲癇;および、他のイオンチャンネル媒介性疾患。
実施例75〜84は、実施例74に記載する通り製造した。
4−[1−(4−クロロ−ベンジル)−1H−テトラゾール−5−イル]-4−フェニル−ピペリジン−1−カルボン酸tert−ブチルエステル
標題化合物:1−[4−(5−フェネチル−[1,2,4]オキサジアゾール−3−イル)−4−フェニル−ピペリジン−1−イル]−3−フェニル−プロパン−1−オンを、実施例94に記載する方法論を用いて製造した。LRMS m/z 466 (M+H)+。
Claims (3)
- 式:
[式中、
mおよびpは独立して共に2であり;
Qは、NR1であり;
R1は、
R2は、アリールであって、これは適宜独立して1つ以上の基T1、T2またはT3で置換され得て;
Jは、結合、または適宜独立して1つ以上の基T1a、T2aもしくはT3aで置換され得るC1〜4アルキレンであり;
R3は、−R5であり;
R4は、アルキルまたはアリールであって、それらの内のいずれかは適宜独立して1つ以上の基T1b、T2bまたはT3bで置換され得て;
R5は、−NR6aR7aであり;
R6aは、インダゾリルであって、それは適宜独立して1つ以上の基T1d、T2dまたはT3dで置換され得て;
R7aは、Hであり;
RXは、Hであり;
Tl、T1a、T1b、T1d、T2、T2a、T2b、T2d、T3、T3a、T3b、またはT3dは各々独立して、水素、アルキル、ハロアルキル、アリール、−OH、−Oアルキル、またはハロであり、ここで、
用語「アルキル」とは、炭素数が1〜12個の直鎖または分枝の炭化水素基を指呼し;
用語「C 1〜4 アルキレン」とは、単結合によって連結した炭素数が1〜4個の直鎖の橋を指呼し;
用語「アリール」とは、芳香族性の単素環式の6〜14員を有する単環、二環、または三環を含有する基、並びにシクロアルキル、シクロアルケニル、ヘテロシクロ、またはヘテロアリール環と縮合したそれらの環を指呼する]。 - Qが、NR1であり;
R4が、アルキルであって、それは適宜独立して1つ以上の基T1b、T2bまたはT3bで置換され得て;
R5が、−NR6aR7aであり;
R6aが、インダゾリルであって、それが適宜独立して1つ以上の基T1d、T2dまたはT3dで置換され得て;そして、
R7aが、Hである、
請求項2記載の化合物。
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- 2003-04-16 JP JP2003585661A patent/JP4729259B2/ja not_active Expired - Fee Related
- 2003-04-16 PL PL03373313A patent/PL373313A1/xx not_active Application Discontinuation
- 2003-04-16 EP EP11157512A patent/EP2371366A1/en not_active Withdrawn
- 2003-04-16 ES ES03719792T patent/ES2388034T3/es not_active Expired - Lifetime
- 2003-04-16 AU AU2003223651A patent/AU2003223651A1/en not_active Abandoned
- 2003-04-16 EP EP10165689A patent/EP2228065B1/en not_active Expired - Lifetime
- 2003-04-16 AT AT03719792T patent/ATE557005T1/de active
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- 2003-04-16 US US10/417,355 patent/US7005436B2/en not_active Expired - Lifetime
- 2003-04-16 WO PCT/US2003/011807 patent/WO2003088908A2/en active Application Filing
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Also Published As
Publication number | Publication date |
---|---|
US20090312307A1 (en) | 2009-12-17 |
AU2003223651A1 (en) | 2003-11-03 |
JP2005529114A (ja) | 2005-09-29 |
PE20040685A1 (es) | 2004-10-08 |
PL373313A1 (en) | 2005-08-22 |
JP4729259B2 (ja) | 2011-07-20 |
IS7502A (is) | 2004-10-12 |
EP2228065B1 (en) | 2012-12-26 |
EP2228065A3 (en) | 2010-12-22 |
ATE557005T1 (de) | 2012-05-15 |
ES2388034T3 (es) | 2012-10-05 |
AR040407A1 (es) | 2005-04-06 |
WO2003088908A2 (en) | 2003-10-30 |
WO2003088908A3 (en) | 2004-05-27 |
AU2003223651A8 (en) | 2003-11-03 |
US7582654B2 (en) | 2009-09-01 |
EP1501467A2 (en) | 2005-02-02 |
US20060014792A1 (en) | 2006-01-19 |
EP1501467A4 (en) | 2009-08-19 |
US7005436B2 (en) | 2006-02-28 |
TW200403058A (en) | 2004-03-01 |
EP2371366A1 (en) | 2011-10-05 |
EP1501467B1 (en) | 2012-05-09 |
US20040110793A1 (en) | 2004-06-10 |
JP2010215666A (ja) | 2010-09-30 |
EP2228065A2 (en) | 2010-09-15 |
NO20044351L (no) | 2004-10-13 |
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