JP2012529443A5

JP2012529443A5 -

Info

Publication number: JP2012529443A5
Application number: JP2012514336A
Authority: JP
Filing date: 2010-06-10
Publication date: 2016-03-17
Anticipated expiration: 2030-06-10

Description

明細書中に特に明示しない限り、Ｙは、Ｈ、ＯＨ、ＮＨＣＨＯ、ＮＨＣ（＝Ｏ）Ｒ₆、ＯＣ（＝Ｏ）ＣＨ₃、ＯＣ（＝Ｏ）Ｒ₆、ＯＣＨ₃、ＯＣ₂Ｈ₅、ＯＲ₆、ＣＨ₃、Ｃ₂Ｈ₅、Ｒ₆、ＣＨ₃ＳＯ₃、Ｒ₆ＳＯ₃、ＮＯ₂、ＣＮ、ＣＦ₃、Ｃ₂Ｆ₅、Ｃ₃Ｆ₇、ＯＣＦ₃、ＯＣ₂Ｆ₅、ＯＣ₃Ｆ₇、Ｆ、Ｂｒ、Ｉ、Ｃｌ、ならびに置換および非置換アルキルオキシルからなる群から選択され；
は、構造ＮＳ−１、構造ＮＳ−２、構造ＮＳ−３、構造ＮＳ−４、および構造ＮＳ−５：
構造ＮＳ−１構造ＮＳ−２構造ＮＳ−３構造ＮＳ−４構造ＮＳ−５
からなる群から選択され；
Ｘ₁は、Ｈ、ＯＨ、ＯＣＨ₃、ＯＣ₂Ｈ₅、ＯＲ₆、Ｃ（＝Ｏ）ＮＨ₂、ＣＨ₂ＯＣ（＝Ｏ）ＮＨ₂、ＣＨ₂ＯＣ（＝Ｏ）ＣＨ₃、ＣＨ₂ＯＣ（＝Ｏ）Ｒ₆、ＯＣ（＝Ｏ）ＣＨ₃、ＯＣ（＝Ｏ）Ｒ₆、ＣＨ₂ＯＣＨ₃、ＣＨ₃、Ｃ₂Ｈ₅、Ｒ₆、Ｃｌ、Ｆ、Ｂｒ、Ｉ、ＨＣ＝ＣＨＣＨ₃、ＨＣ＝ＣＨ₂、ＣＨ₂ＯＣＨ₃、ＣＨ₂ＯＲ₆、Ｓ（ＣＨ₂）_n−ＮＨＲ₇、構造Ｘ₁−１、構造Ｘ₁−２、構造Ｘ₁−３、構造Ｘ₁−４、構造Ｘ₁−５、構造Ｘ₁−６、構造Ｘ₁−７、構造Ｘ₁−８、構造Ｘ₁−９、構造Ｘ₁−１０、構造Ｘ₁−１１、構造Ｘ₁−１２、構造Ｘ₁−１３、構造Ｘ₁−１４、構造Ｘ₁−１５、構造Ｘ₁−１６、構造Ｘ₁−１７、構造Ｘ₁−１８、構造Ｘ₁−１９、構造Ｘ₁−２０、構造Ｘ₁−２１、構造Ｘ₁−２２、構造Ｘ₁−２３、構造Ｘ₁−２４、構造Ｘ₁−２５、構造Ｘ₁−２６、構造Ｘ₁−２７、構造Ｘ₁−２８、構造Ｘ₁−２９、構造Ｘ₁−３０、構造Ｘ₁−３１、構造Ｘ₁−３２、構造Ｘ₁−３３、構造Ｘ₁−３４、構造Ｘ₁−３５、構造Ｘ₁−３６、構造Ｘ₁−３７、構造Ｘ₁−３８、構造Ｘ₁−３９、構造Ｘ₁−４０、構造Ｘ₁−４１、構造Ｘ₁−４２、構造Ｘ₁−４３、構造Ｘ₁−４４、構造Ｘ₁−４５、構造Ｘ₁−４６、構造Ｘ₁−４７、構造Ｘ₁−４８、構造Ｘ₁−４９、構造Ｘ₁−５０、構造Ｘ₁−５１、構造Ｘ₁−５２、構造Ｘ₁−５３、構造Ｘ₁−５４、構造Ｘ₁−５５、構造Ｘ₁−５６、構造Ｘ₁−５７、構造Ｘ₁−５８、構造Ｘ₁−５９、構造Ｘ₁−６０、構造Ｘ₁−６１、構造Ｘ₁−６２、構造Ｘ₁−６３、構造Ｘ₁−６４、構造Ｘ₁−６５、構造Ｘ₁−６６、構造Ｘ₁−６７、構造Ｘ₁−６８、構造Ｘ₁−６９、構造Ｘ₁−７０、構造Ｘ₁−７１、構造Ｘ₁−７２、構造Ｘ₁−７３、構造Ｘ₁−７４、構造Ｘ₁−７５、構造Ｘ₁−７６、構造Ｘ₁−７７、構造Ｘ₁−７８、構造Ｘ₁−７９、構造Ｘ₁−８０、構造Ｘ₁−８１、および構造Ｘ₁−８２からなる群から選択され；
構造Ｘ₁−１構造Ｘ₁−２構造Ｘ₁−３
構造Ｘ₁−４構造Ｘ₁−５
構造Ｘ₁−６構造Ｘ₁−７構造Ｘ₁−８
構造Ｘ₁−９構造Ｘ₁−１０
構造Ｘ₁−１１構造Ｘ₁−１２
構造Ｘ₁−１３構造Ｘ₁−１４
構造Ｘ₁−１５構造Ｘ₁−１６
構造Ｘ₁−１７構造Ｘ₁−１８
構造Ｘ₁−１９構造Ｘ₁−２０
構造Ｘ₁−２１構造Ｘ₁−２２
構造Ｘ₁−２３構造Ｘ₁−２４
構造Ｘ₁−２５構造Ｘ₁−２６
構造Ｘ₁−２７構造Ｘ₁−２８
構造Ｘ₁−２９構造Ｘ₁−３０
構造Ｘ₁−３１構造Ｘ₁−３２
構造Ｘ₁−３３構造Ｘ₁−３４
構造Ｘ₁−３５構造Ｘ₁−３６
構造Ｘ₁−３７構造Ｘ₁−３８
構造Ｘ₁−３９構造Ｘ₁−４０
構造Ｘ₁−４１構造Ｘ₁−４２構造Ｘ₁−４３
構造Ｘ₁−４４構造Ｘ₁−４５
構造Ｘ₁−４６構造Ｘ₁−４７
構造Ｘ₁−４８構造Ｘ₁−４９
構造Ｘ₁−５０構造Ｘ₁−５１
構造Ｘ₁−５２構造Ｘ₁−５３構造Ｘ₁−５４
構造Ｘ₁−５５構造Ｘ₁−５６構造Ｘ₁−５７
構造Ｘ₁−５８構造Ｘ₁−５９
構造Ｘ₁−６０構造Ｘ₁−６１
構造Ｘ₁−６２構造Ｘ₁−６３構造Ｘ₁−６４
構造Ｘ₁−６５構造Ｘ₁−６６
構造Ｘ₁−６７構造Ｘ₁−６８
構造Ｘ₁−６９構造Ｘ₁−７０

構造Ｘ₁−７１構造Ｘ₁−７２
構造Ｘ₁−７３構造Ｘ₁−７４
構造Ｘ₁−７５構造Ｘ₁−７６
構造Ｘ₁−７７構造Ｘ₁−７８
構造Ｘ₁−７９構造Ｘ₁−８０
構造Ｘ₁−８１構造Ｘ₁−８２、

Ｙと一緒になったＲｓ−は、Ｒ₆ＯＣＨ₂Ｃ（Ｒ₅）＝である、または単独で、Ｒ₆ＯＯＣＣＨ（ＮＨＲ₇）（ＣＨ₂）_nＣ（＝Ｏ）ＮＨ−、Ｒ₆ＯＯＣＣＨ（ＮＨＲ₇）（ＣＨ₂）_nＳＣ（＝Ｏ）ＮＨ−、ＣＦ₃ＳＣＨ₂Ｃ（＝Ｏ）ＮＨ−、ＣＦ₃ＣＨ₂Ｃ（＝Ｏ）ＮＨ−、ＣＨＦ₂ＳＣＨ₂Ｃ（＝Ｏ）ＮＨ−、ＣＨ₂ＦＳＣＨ₂Ｃ（＝Ｏ）ＮＨ−、ＮＨ₂Ｃ（＝Ｏ）ＣＨＦＳ−ＣＨ₂Ｃ（＝Ｏ）ＮＨ−、Ｒ₇ＮＨＣＨ（Ｃ（＝Ｏ）ＯＷ）ＣＨ₂ＳＣＨ₂Ｃ（＝Ｏ）ＮＨ−、Ｒ₇ＮＨＣＨ（Ｌ₁−Ｌ₄−Ｌ₂−Ｗ）ＣＨ₂ＳＣＨ₂Ｃ（＝Ｏ）ＮＨ−、ＣＮＣＨ₂ＳＣＨ₂Ｃ（＝Ｏ）ＮＨ−、ＣＨ₃（ＣＨ₂）_nＣ（＝Ｏ）ＮＨ−、Ｒ₇Ｎ＝ＣＨＮＲ₇ＣＨ₂ＣＨ₂Ｓ−、Ｒ₇Ｎ＝Ｃ（ＮＨＲ₇）ＮＨＣ（＝Ｏ）−、Ｒ₇Ｎ＝Ｃ（ＮＨＲ₇）ＮＨＣ（＝Ｏ）ＣＨ₂、ＣＨ₃Ｃ（Ｃｌ）＝ＣＨＣＨ₂ＳＣＨ₂Ｃ（＝Ｏ）ＮＨ−、（ＣＨ₃）₂Ｃ（ＯＲ₆）−、ＣＮＣＨ₂Ｃ（＝Ｏ）ＮＨ−、ＣＮＣＨ₂ＣＨ₂Ｓ−、Ｒ₇ＨＮ＝ＣＨ（ＮＲ₇）ＣＨ₂ＣＨ₂Ｓ−、ＣＨ₂＝ＣＨＣＨ₂ＳＣＨ₂Ｃ（＝Ｏ）ＮＨ−、ＣＨ₃ＣＨ（ＯＨ）−、ＣＨ₃ＣＨ（ＯＲ₈）−、ＣＨ₃ＣＨ（Ｙ₁）−、（ＣＨ₃）₂ＣＨ−、ＣＨ₃ＣＨ₂−、ＣＨ₃（ＣＨ₂）_nＣＨ＝ＣＨ（ＣＨ₂）_mＣ（＝Ｏ）ＮＨ−、構造Ｒｓ−１、構造Ｒｓ−２、構造Ｒｓ−３、構造Ｒｓ−４、構造Ｒｓ−５、構造Ｒｓ−６、構造Ｒｓ−７、構造Ｒｓ−８、構造Ｒｓ−９、構造Ｒｓ−１０、構造Ｒｓ−１１、構造Ｒｓ−１２、構造Ｒｓ−１３、構造Ｒｓ−１４、構造Ｒｓ−１５、構造Ｒｓ−１６、構造Ｒｓ−１７、構造Ｒｓ−１８、構造Ｒｓ−１９、構造Ｒｓ−２０、構造Ｒｓ−２１、構造Ｒｓ−２２、構造Ｒｓ−２３、構造Ｒｓ−２４、構造Ｒｓ−２５、構造Ｒｓ−２６、構造Ｒｓ−２７、構造Ｒｓ−２８、構造Ｒｓ−２９、構造Ｒｓ−３０、構造Ｒｓ−３１、構造Ｒｓ−３２、構造Ｒｓ−３３、構造Ｒｓ−３４、構造Ｒｓ−３５、構造Ｒｓ−３６、構造Ｒｓ−３７、構造Ｒｓ−３８、構造Ｒｓ−３９、構造Ｒｓ−４０、構造Ｒｓ−４１、構造Ｒｓ−４２、構造Ｒｓ−４３、構造Ｒｓ−４４、構造Ｒｓ−４５、および構造Ｒｓ−４６からなる群から選択され；
構造Ｒｓ−１構造Ｒｓ−２
構造Ｒｓ−３構造Ｒｓ−４
構造Ｒｓ−５構造Ｒｓ−６
構造Ｒｓ−７構造Ｒｓ−８
構造Ｒｓ−９構造Ｒｓ−１０
構造Ｒｓ−１１構造Ｒｓ−１２
構造Ｒｓ−１３構造Ｒｓ−１４
構造Ｒｓ−１５構造Ｒｓ−１６
構造Ｒｓ−１７構造Ｒｓ−１８
構造Ｒｓ−１９構造Ｒｓ−２０
構造Ｒｓ−２１構造Ｒｓ−２２
構造Ｒｓ−２３構造Ｒｓ−２４
構造Ｒｓ−２５構造Ｒｓ−２６
構造Ｒｓ−２７構造Ｒｓ−２８
構造Ｒｓ−２９構造Ｒｓ−３０
構造Ｒｓ−３１構造Ｒｓ−３２
構造Ｒｓ−３３構造Ｒｓ−３４
構造Ｒｓ−３５構造Ｒｓ−３６
構造Ｒｓ−３７構造Ｒｓ−３８
構造Ｒｓ−３９構造Ｒｓ−４０
構造Ｒｓ−４１構造Ｒｓ−４２
構造Ｒｓ−４３構造Ｒｓ−４４
構造Ｒｓ−４５構造Ｒｓ−４６；

Ｗは、Ｈ、置換および非置換アルキル、置換および非置換シクロアルキル、置換および非置換ヘテロシクロアルキル、置換および非置換アルキルオキシ、置換および非置換アルケニル、置換および非置換アルキニル、置換および非置換アリール、置換および非置換ヘテロアリール、プロトン化可能なアミン基、薬学的に許容される置換および非置換第一級アミン基、構造Ｗａ、構造Ｗ−１、構造Ｗ−２、構造Ｗ−３、構造Ｗ−４、構造Ｗ−５、構造Ｗ−６、構造Ｗ−７、構造Ｗ−８、構造Ｗ−９、構造Ｗ−１０、構造Ｗ−１１、構造Ｗ−１２、構造Ｗ−１３、構造Ｗ−１４、構造Ｗ−１５、構造Ｗ−１６、構造Ｗ−１７、および構造Ｗ−１８からなる群から選択され；
構造Ｗａ構造Ｗ−１構造Ｗ−２構造Ｗ−３
構造Ｗ−４構造Ｗ−５構造Ｗ−６
構造Ｗ−７構造Ｗ−８構造Ｗ−９
構造Ｗ−１０構造Ｗ−１１構造Ｗ−１２
構造Ｗ−１３構造Ｗ−１４構造Ｗ−１５
構造Ｗ−１６構造Ｗ−１７構造Ｗ−１８；

Ｚは、ＣＨ₂、Ｓ、ＳＯ、ＳＯ₂、ＮＨ、ＮＲ₆、ＣＨＣＨ₃、ＣＨＣＨ₂ＣＨ₃、ＣＨＲ₆、Ｒ₆、−Ｃ（＝Ｏ）−、およびＯからなる群から選択され；
ＡＡは、任意のアミノ酸を表し；
ｍおよびｎの各々は、独立に、０および整数、例えば、０、１、２、３、４、５、６、７、８、９、１０、１１、１２、１３、１４、１５、１６、１７、１８、１９、２０、．．．からなる群から選択され；
ＨＡは、何もない、および薬学的に許容される酸、例えば、塩酸塩、臭化水素酸塩、ヨウ化水素酸塩、硝酸、硫酸（ｓｕｌｆｕｒｉｃａｃｉｄ）、二硫酸、リン酸、亜リン酸、ホスホン酸、イソニコチン酸、酢酸、乳酸、サリチル酸、クエン酸、酒石酸、パントテン酸、二酒石酸、アスコルビン酸、コハク酸、マレイン酸、ゲンチジン酸、フマル酸、グルコン酸、グルクロン酸（ｇｌｕｃｕｒｏｎｉｃａｃｉｄ）、サッカリン酸、ギ酸、安息香酸、グルタミン酸、メタンスルホン酸、エタンスルホン酸、ベンゼンスルホン酸、ｐ−トルエンスルホン酸、およびパモ酸からなる群から選択され；
Ｒは、何もない、Ｈ、ＣＨ₂Ｃ（＝Ｏ）ＯＲ₆、置換および非置換アルキル、置換および非置換シクロアルキル、置換および非置換ヘテロシクロアルキル、置換および非置換アルコキシル、置換および非置換ペルフルオロアルキル、置換および非置換ハロゲン化アルキル、置換および非置換アルケニル、置換および非置換アルキニル、置換および非置換アリール、ならびに置換および非置換ヘテロアリールからなる群から選択され、ここでＲ中の任意のＣＨ₂は、Ｏ、Ｓ、Ｐ、ＮＲ₆、または任意の他の薬学的に許容される基によりさらに置換されていてもよく；
Ｒ₁〜Ｒ₃は、独立に、Ｈ、置換および非置換アルキル、置換および非置換シクロアルキル、置換および非置換ヘテロシクロアルキル、置換および非置換アルキルオキシル、置換および非置換アルケニル、置換および非置換アルキニル、置換および非置換アリール、ならびに置換および非置換ヘテロアリール残基からなる群から選択され；
Ｒ₅およびＲ₃₅は、独立に、Ｈ、Ｃ（＝Ｏ）ＮＨ₂、ＣＨ₂ＣＨ₂ＯＲ₆、ＣＨ₂ＣＨ₂Ｎ（ＣＨ₃）₂、ＣＨ₂ＣＨ₂Ｎ（ＣＨ₂ＣＨ₃）₂、Ｃｌ、Ｆ、Ｂｒ、Ｉ、置換および非置換アルキル、置換および非置換シクロアルキル、置換および非置換ヘテロシクロアルキル、置換および非置換アルキルオキシル、置換および非置換シクロアルキルオキシル、置換および非置換アリール、置換および非置換ヘテロアリール、置換および非置換アルキルカルボニル、置換および非置換アルキルアミノ、−Ｃ（＝Ｏ）−Ｗ、Ｌ₁−Ｌ₄−Ｌ₂−Ｗ、ならびにＷからなる群から選択され；
Ｒ₆、Ｒ₃₆、およびＲ₄₆は、独立に、Ｈ、Ｆ、Ｃｌ、Ｂｒ、Ｉ、Ｎａ⁺、Ｋ⁺、Ｃ（＝Ｏ）Ｒ₅、２−オキソ−１−イミダゾリジニル、フェニル、５−インダニル、２，３−ジヒドロ−１Ｈ−インデン−５−イル、４−ヒドロキシ−１，５−ナフチリジン−３−イル、置換および非置換アルキル、置換および非置換シクロアルキル、置換および非置換ヘテロシクロアルキル、置換および非置換アルケニル、置換および非置換アルキニル、置換および非置換アルキルオキシル、置換および非置換シクロアルキルオキシル、置換および非置換アリール、置換および非置換ヘテロアリール、−Ｃ（＝Ｏ）−Ｗ、−Ｌ₁−Ｌ₄−Ｌ₂−Ｗ、ならびにＷからなる群から選択され；
Ｒ₇およびＲ₃₇は、独立に、Ｈ、Ｆ、Ｃｌ、Ｂｒ、Ｉ、ＣＨ₃ＮＨＣ（＝Ｏ）ＣＨ₂ＣＨ（ＮＨＲ₈）Ｃ（＝Ｏ）、Ｒ₅Ｎ＝Ｃ（ＮＨＲ₆）ＮＨＣ（＝Ｏ）−、Ｃ（＝Ｏ）ＣＨ₃、Ｃ（＝Ｏ）Ｒ₆、ＰＯ（ＯＲ₅）ＯＲ₆、置換および非置換アルキル、置換および非置換シクロアルキル、置換および非置換ヘテロシクロアルキル、置換および非置換アルキルオキシル、置換および非置換アルケニル、置換および非置換アルキニル、置換および非置換アリール、置換および非置換ヘテロアリール、置換および非置換アルキルカルボニル、置換および非置換アルキルアミノ、Ｌ₁−Ｌ₄−Ｌ₂−Ｗ、ならびにＣ−（＝Ｏ）−Ｗからなる群から選択され；
Ｒ₈およびＲ₃₈は、独立に、Ｈ、Ｆ、Ｃｌ、Ｂｒ、Ｉ、ＣＨ₃、Ｃ₂Ｈ₅、ＣＦ₃、ＣＨ₂ＣＨ₂Ｆ、ＣＨ₂ＣＨ₂Ｃｌ、ＣＨ₂ＣＨ₂Ｂｒ、ＣＨ₂ＣＨ₂Ｉ、ＣＨ₂ＣＨＦ₂、ＣＨ₂ＣＦ₃、ＣＨ₂Ｆ、ＣＨ₂Ｃｌ、ＣＨ₂Ｂｒ、ＣＨ₂Ｉ、ＣＨ₂ＮＲ₆Ｒ₇、ＣＨ（ＮＨＲ₇）ＣＨ₂Ｃ（＝Ｏ）ＮＨ₂、Ｃ₃Ｈ₇、Ｃ₄Ｈ₉、Ｃ₅Ｈ₁₁、Ｒ₆、Ｃ（＝Ｏ）Ｒ₆、Ｃ（＝Ｏ）ＮＨ₂、ＣＨ₂Ｃ（＝Ｏ）ＮＨ₂、ＣＨ₂ＯＣ（＝Ｏ）ＮＨ₂、ＰＯ（ＯＲ₅）ＯＲ₆、Ｃ（ＣＨ₃）₂Ｃ（＝Ｏ）ＯＲ₆、ＣＨ（ＣＨ₃）Ｃ（＝Ｏ）ＯＲ₆、ＣＨ₂Ｃ（＝Ｏ）ＯＲ₆、Ｃ（＝Ｏ）−Ｗ、Ｌ₁−Ｌ₄−Ｌ₂−Ｗ、Ｗ、置換および非置換ペルフルオロアルキル、置換および非置換アルキル、置換および非置換シクロアルキル、置換および非置換ヘテロシクロアルキル、置換および非置換アルコキシル、置換および非置換アルキルアミノ、置換および非置換ペルフルオロアルキル、置換および非置換ハロゲン化アルキル、ならびに置換および非置換アルキルカルボニルからなる群から選択され；
Ｒ₁₁〜Ｒ₁₆は、独立に、何もない、Ｈ、ＣＨ₂Ｃ（＝Ｏ）ＯＲ₁₁、置換および非置換アルキル、置換および非置換シクロアルキル、置換および非置換ヘテロシクロアルキル、置換および非置換アルコキシル、置換および非置換ペルフルオロアルキル、置換および非置換ハロゲン化アルキル、置換および非置換アルケニル、置換および非置換アルキニル、置換および非置換アリール、ならびに置換および非置換ヘテロアリールからなる群から選択され；
Ｘ₂は、Ｈ、Ｃ（＝Ｏ）、Ｃ（＝Ｓ）、ＣＨ₂（ＣＨ₂）_nＯＲ₈、Ｃｌ、Ｆ、Ｂｒ、Ｉ、ＮＯ₂、ＣＮ、ＣＦ₃、Ｃ₂Ｆ₅、Ｃ₃Ｆ₇、ＯＣＦ₃、ＯＣ₂Ｆ₅、ＮＨ₂、ＮＨＲ₆、ＣＨ₃、Ｃ₂Ｈ₅、Ｒ₆、Ｃ（＝Ｏ）ＮＨ₂、ＣＨ₂ＯＣ（＝Ｏ）ＮＨ₂、ＣＨ₂Ｃ（＝Ｏ）ＯＲ₅、ＣＨ₂（ＣＨ₂）_nＮ（ＣＨ₃）₂、ＣＨ₂（ＣＨ₂）_nＳＯ₃Ｒ₅、置換および非置換アルキル、置換および非置換シクロアルキル、置換および非置換ヘテロシクロアルキル、置換および非置換ペルフルオロアルキル、置換および非置換アルキル、置換および非置換アルキルチオ、置換および非置換アルキルアミノ、ならびに置換および非置換アルキルオキシルからなる群から選択され；
Ｘ₃は、Ｈ、Ｎ₃、ＳＯ₃Ｗ、Ｆ、Ｃｌ、Ｂｒ、ＯＨ、ＯＣＨ₃、ＯＲ₆、ＣＨ₃、Ｒ₆、Ｃ（＝Ｏ）、Ｃ（＝Ｓ）、Ｃ（＝Ｏ）ＯＷ、ＯＷ、Ｌ₁−Ｌ₄−Ｌ₂−Ｗ、およびＩからなる群から選択され；
Ｘ₄は、Ｎ、ＣＨ、およびＣＹ₁からなる群から選択され；
Ｘ₅およびＸ₃₅は、独立に、何もない、Ｃ（＝Ｏ）、Ｃ（＝Ｓ）、ＯＣ（＝Ｏ）、ＣＨ₂、ＣＨ、Ｓ、Ｏ、およびＮＲ₅からなる群から選択され；
Ｙ₁、Ｙ₃₁、Ｙ₂、Ｙ₃₂、Ｙ₃、およびＹ₄は、独立に、Ｈ、ＯＨ、ＯＷ、ＯＣ（＝Ｏ）Ｗ、Ｌ₁−Ｌ₄−Ｌ₂−Ｗ、ＯＣ（＝Ｏ）ＣＨ₃、ＣＨ₃、Ｃ₂Ｈ₅、Ｃ₃Ｈ₇、Ｃ₄Ｈ₉、Ｒ₆、ＳＯ₃Ｒ₆、ＣＨ₂ＯＲ₆、ＣＨ₂ＯＣ（＝Ｏ）Ｒ₆、ＣＨ₂Ｃ（＝Ｏ）ＯＲ₈、ＯＣＨ₃、ＯＣ₂Ｈ₅、ＯＲ₆、ＣＨ₃ＳＯ₂、Ｒ₆ＳＯ₂、ＣＨ₃ＳＯ₃、Ｒ₆ＳＯ₃、ＮＯ₂、ＣＮ、ＣＦ₃、ＯＣＦ₃、ＣＨ₂（ＣＨ₂）_nＮＲ₅Ｒ₆、ＣＨ₂（ＣＨ₂）_nＯＲ₆、ＣＨ（Ｃ（＝Ｏ）ＮＨ₂）ＮＨＲ₆、ＣＨ₂Ｃ（＝Ｏ）ＮＨ₂、Ｆ、Ｂｒ、Ｉ、Ｃｌ、ＣＨ＝ＣＨＣ（＝Ｏ）ＮＨＣＨ₂Ｃ（＝Ｏ）ＯＷ、ＣＨ＝ＣＨＣ（＝Ｏ）ＮＨＣＨ₂Ｌ₁−Ｌ₄−Ｌ₂−Ｗ、ＮＲ₈Ｃ（＝Ｏ）Ｒ₅、ＳＯ₂ＮＲ₅Ｒ₈、Ｃ（＝Ｏ）Ｒ₅、ＳＲ₅、置換および非置換ペルフルオロアルキル、置換および非置換アルコキシル、置換および非置換アルキルチオ、置換および非置換アルキルアミノ、置換および非置換ペルフルオロアルキル、置換および非置換ハロゲン化アルキル、ならびに置換および非置換アルキルカルボニルからなる群から選択され；
Ｌ₁は、何もない、Ｏ、Ｓ、−Ｏ−Ｌ₃−、−Ｓ−Ｌ₃−、−Ｎ（Ｌ₃）−、−Ｎ（Ｌ₃）−ＣＨ₂−Ｏ、−Ｎ（Ｌ₃）−ＣＨ₂−Ｎ（Ｌ₅）−、−Ｏ−ＣＨ₂−Ｏ−、−Ｏ−ＣＨ（Ｌ₃）−Ｏ、および−Ｓ−ＣＨ（Ｌ₃）−Ｏ−からなる群から選択され；
Ｌ₂は、何もない、Ｏ、Ｓ、−Ｏ−Ｌ₃−、−Ｓ−Ｌ₃−、−Ｎ（Ｌ₃）−、−Ｎ（Ｌ₃）−ＣＨ₂−Ｏ、−Ｎ（Ｌ₃）−ＣＨ₂−Ｎ（Ｌ₅）−、−Ｏ−ＣＨ₂−Ｏ−、−Ｏ−ＣＨ（Ｌ₃）−Ｏ、−Ｓ−ＣＨ（Ｌ₃）−Ｏ−、−Ｏ−Ｌ₃−、−Ｎ−Ｌ₃−、−Ｓ−Ｌ₃−、−Ｎ（Ｌ₃）−Ｌ₅−、およびＬ₃からなる群から選択され；
Ｌ₄は、Ｃ＝Ｏ、Ｃ＝Ｓ、
および
からなる群から選択され；
Ｌ₁、Ｌ₂、およびＬ₄の各々について、Ｌ₃およびＬ₅は、独立に、何もない、Ｈ、ＣＨ₂Ｃ（＝Ｏ）ＯＬ ₆、置換および非置換アルキル、置換および非置換シクロアルキル、置換および非置換ヘテロシクロアルキル、置換および非置換アリール、置換および非置換ヘテロアリール、置換および非置換アルコキシル、置換および非置換アルキルチオ、置換および非置換アルキルアミノ、置換および非置換ペルフルオロアルキル、ならびに置換および非置換ハロゲン化アルキルからなる群から選択され、ここで任意の炭素または水素は、さらに、独立に、Ｏ、Ｓ、Ｐ、ＮＬ₃、または任意の他の薬学的に許容される基により置換されていてもよく；
Ｌ₆は、独立に、Ｈ、ＯＨ、Ｃｌ、Ｆ、Ｂｒ、Ｉ、置換および非置換アルキル、置換および非置換シクロアルキル、置換および非置換ヘテロシクロアルキル、置換および非置換アリール、置換および非置換ヘテロアリール、置換および非置換アルコキシル、置換および非置換アルキルチオ、置換および非置換アルキルアミノ、置換および非置換ペルフルオロアルキル、ならびに置換および非置換ハロゲン化アルキルからなる群から選択され、ここで任意の炭素または水素は、さらに、独立に、Ｏ、Ｓ、Ｎ、Ｐ（Ｏ）ＯＬ₆、ＣＨ＝ＣＨ、Ｃ≡Ｃ、ＣＨＬ₆、ＣＬ₆Ｌ₇、アリール、ヘテロアリール、または環状基により置換されていてもよく；
Ｌ₇は、独立に、Ｈ、ＯＨ、Ｃｌ、Ｆ、Ｂｒ、Ｉ、置換および非置換アルキル、置換および非置換シクロアルキル、置換および非置換ヘテロシクロアルキル、置換および非置換アリール、置換および非置換ヘテロアリール、置換および非置換アルコキシル、置換および非置換アルキルチオ、置換および非置換アルキルアミノ、置換および非置換ペルフルオロアルキル、ならびに置換および非置換ハロゲン化アルキルからなる群から選択され、ここで任意の炭素または水素は、さらに、独立に、Ｏ、Ｓ、Ｎ、Ｐ（Ｏ）ＯＬ₆、ＣＨ＝ＣＨ、Ｃ≡Ｃ、ＣＨＬ₆、ＣＬ₆Ｌ₇、アリール、ヘテロアリール、または環状基により置換されていてもよく；
任意のＣＨ₂基は、Ｏ、Ｓ、またはＮＨにより置換されていてもよい。
Unless otherwise specified in the specification, Y represents H, OH, NHCHO, NHC (═O) R ₆ , OC (═O) CH ₃ , OC (═O) R ₆ , OCH ₃ , OC ₂ H ₅ , OR ₆ , CH ₃ , C ₂ H ₅ , R ₆ , CH ₃ SO ₃ , R ₆ SO ₃ , NO ₂ , CN, CF ₃ , C ₂ F ₅ , C ₃ F ₇ , OCF ₃ , OC ₂ F ₅ , Selected from the group consisting of OC ₃ F ₇ , F, Br, I, Cl, and substituted and unsubstituted alkyloxyls;
Are structure NS-1, structure NS-2, structure NS-3, structure NS-4, and structure NS-5:
Structure NS-1 Structure NS-2 Structure NS-3 Structure NS-4 Structure NS-5
Selected from the group consisting of;
X ₁ is H, OH, OCH ₃ , OC ₂ H ₅ , OR ₆ , C (═O) NH ₂ , CH ₂ OC (═O) NH ₂ , CH ₂ OC (═O) CH ₃ , CH ₂ OC (= O) R ₆ , OC (═O) CH ₃ , OC (═O) R ₆ , CH ₂ OCH ₃ , CH ₃ , C ₂ H ₅ , R ₆ , Cl, F, Br, I, HC═CHCH _{_{3, HC = CH 2, CH}} 2 OCH 3, CH 2 OR 6, S (CH 2) n -NHR 7, the structure X ₁ -1, the structure X ₁ -2, the structure X ₁ -3, the structure X ₁ -4 , Structure X ₁ -5, structure X ₁ -6, structure X ₁ -7, structure X ₁ -8, structure X ₁ -9, structure X ₁ -10, structure X ₁ -11, structure X ₁ -12, structure X ₁ -13, Structure X ₁ -14, Structure X ₁ -15, Structure X ₁ -16, Structure X ₁ -17, Structure X ₁ -18, Structure X ₁ -19, Structure X ₁ -20, Structure X ₁ -21, structure X ₁ -22, structure ₁ -23, the structure X ₁ -24, structure X ₁ -25, structure X ₁ -26, structure X ₁ -27, structure X ₁ -28, structure X ₁ -29, structure X ₁ -30, structure X ₁ - 31, the structure X ₁ -32, structure X ₁ -33, structure X ₁ -34, structure X ₁ -35, structure X ₁ -36, structure X ₁ -37, structure X ₁ -38, structure X ₁ -39, structure X ₁ -40, structure X ₁ -41, structure X ₁ -42, structure X ₁ -43, structure X ₁ -44, structure X ₁ -45, structure X ₁ -46, structure X ₁ -47, structure X ₁ -48, the structure X ₁ -49, structure X ₁ -50, structure X ₁ -51, structure X ₁ -52, structure X ₁ -53, structure X ₁ -54, structure X ₁ -55, structure X ₁ - 56, the structure X ₁ -57, structure X ₁ -58, structure X ₁ -59, structure X ₁ -60, structure X ₁ -61, structure X ₁ -62, structure X ₁ -63, structure X ₁ -64, Structure X ₁ -65, structure X ₁ -66, structure X ₁ -67, structure X ₁ -68, structure X ₁ -69, structure X ₁ -70, structure X ₁ -71, structure X ₁ -72, structure X ₁ -73, the structure X ₁ -74, structure X ₁ -75, structure X ₁ -76, structure X ₁ -77, structure X ₁ -78, structure X ₁ -79, structure X ₁ -80, structure X ₁ - 81 and selected from the group consisting of the structures X ₁ -82;
Structure X ₁ -1 Structure X ₁ -2 Structure X ₁ -3
Structure X ₁ -4 Structure X ₁ -5
Structure X ₁ -6 structure X ₁ -7 structure X ₁ -8
Structure X ₁ -9 structure X ₁ -10
Structure X ₁ -11 structure X ₁ -12
Structure X ₁ -13 structure X ₁ -14
Structure X ₁ -15 structure X ₁ -16
Structure X ₁ -17 structure X ₁ -18
Structure X ₁ -19 structure X ₁ -20
Structure X ₁ -21 structure X ₁ -22
Structure X ₁ -23 structure X ₁ -24
Structure X ₁ -25 structure X ₁ -26
Structure X ₁ -27 structure X ₁ -28
Structure X ₁ -29 structure X ₁ -30
Structure X ₁ -31 structure X ₁ -32
Structure X ₁ -33 structure X ₁ -34
Structure X ₁ -35 Structure X ₁ -36
Structure X ₁ -37 structure X ₁ -38
Structure X ₁ -39 structure X ₁ -40
Structure X ₁ -41 structure X ₁ -42 structure X ₁ -43
Structure X ₁ -44 structure X ₁ -45
Structure X ₁ -46 structure X ₁ -47
Structure X ₁ -48 structure X ₁ -49
Structure X ₁ -50 structure X ₁ -51
Structure X ₁ -52 Structure X ₁ -53 Structure X ₁ -54
Structure X ₁ -55 Structure X ₁ -56 Structure X ₁ -57
Structure X ₁ -58 structure X ₁ -59
Structure X ₁ -60 structure X ₁ -61
Structure X ₁ -62 structure X ₁ -63 structure X ₁ -64
Structure X ₁ -65 structure X ₁ -66
Structure X ₁ -67 structure X ₁ -68
Structure X ₁ -69 structure X ₁ -70

Structure X ₁ -71 structure X ₁ -72
Structure X ₁ -73 structure X ₁ -74
Structure X ₁ -75 Structure X ₁ -76
Structure X ₁ -77 Structure X ₁ -78
Structure X ₁ -79 structure X ₁ -80
Structure X ₁ -81 structure X ₁ -82,

Rs— taken together with Y is R ₆ OCH ₂ C (R ₅ ) =, or R ₆ OOCCH (NHR ₇ ) (CH ₂ ) _n C (═O) NH—, R ₆ OOCCH alone (NHR ₇ ) (CH ₂ ) _n SC (═O) NH—, CF ₃ SCH ₂ C (═O) NH—, CF ₃ CH ₂ C (═O) NH—, CHF ₂ SCH ₂ C (═O) NH—, CH ₂ FSCH ₂ C (═O) NH—, NH ₂ C (═O) CHFS—CH ₂ C (═O) NH—, R ₇ NHCH (C (═O) OW) CH ₂ SCH ₂ C _{(= O) NH-, R 7} NHCH (L 1 -L 4 -L 2 -W) CH 2 SCH 2 C (= O) NH-, CNCH 2 SCH 2 C (= O) NH-, CH 3 (CH _{_{2) n C (= O)}} NH-, R 7 n = CHNR 7 CH 2 CH 2 S-, R 7 n = C (NHR 7) NHC (= O) -, R 7 n = C (NHR 7) _{HC (= O) CH 2,} CH 3 C (Cl) = CHCH 2 SCH 2 C (= O) NH -, (CH 3) 2 C (OR 6) -, CNCH 2 C (= O) NH-, CNCH ₂ CH ₂ S—, R ₇ HN═CH (NR ₇ ) CH ₂ CH ₂ S—, CH ₂ = CHCH ₂ SCH ₂ C (═O) NH—, CH ₃ CH (OH) —, CH ₃ CH (OR _{_{8) -, CH 3 CH (}} Y 1) -, (CH 3) 2 CH-, CH 3 CH 2 -, CH 3 (CH 2) n CH = CH (CH 2) m C (= O) NH-, Structure Rs-1, Structure Rs-2, Structure Rs-3, Structure Rs-4, Structure Rs-5, Structure Rs-6, Structure Rs-7, Structure Rs-8, Structure Rs-9, Structure Rs-10, Structure Rs-11, Structure Rs-12, Structure Rs-13, Structure Rs-14, Structure Rs-15, Structure Rs-16, Structure Rs-17, Structure Rs- 8, structure Rs-19, structure Rs-20, structure Rs-21, structure Rs-22, structure Rs-23, structure Rs-24, structure Rs-25, structure Rs-26, structure Rs-27, structure Rs- 28, structure Rs-29, structure Rs-30, structure Rs-31, structure Rs-32, structure Rs-33, structure Rs-34, structure Rs-35, structure Rs-36, structure Rs-37, structure Rs- 38, selected from the group consisting of Structure Rs-39, Structure Rs-40, Structure Rs-41, Structure Rs-42, Structure Rs-43, Structure Rs-44, Structure Rs-45, and Structure Rs-46;
Structure Rs-1 Structure Rs-2
Structure Rs-3 Structure Rs-4
Structure Rs-5 Structure Rs-6
Structure Rs-7 Structure Rs-8
Structure Rs-9 Structure Rs-10
Structure Rs-11 Structure Rs-12
Structure Rs-13 Structure Rs-14
Structure Rs-15 Structure Rs-16
Structure Rs-17 Structure Rs-18
Structure Rs-19 Structure Rs-20
Structure Rs-21 Structure Rs-22
Structure Rs-23 Structure Rs-24
Structure Rs-25 Structure Rs-26
Structure Rs-27 Structure Rs-28
Structure Rs-29 Structure Rs-30
Structure Rs-31 Structure Rs-32
Structure Rs-33 Structure Rs-34
Structure Rs-35 Structure Rs-36
Structure Rs-37 Structure Rs-38
Structure Rs-39 Structure Rs-40
Structure Rs-41 Structure Rs-42
Structure Rs-43 Structure Rs-44
Structure Rs-45 structure Rs-46;

W is H, substituted and unsubstituted alkyl, substituted and unsubstituted cycloalkyl, substituted and unsubstituted heterocycloalkyl, substituted and unsubstituted alkyloxy, substituted and unsubstituted alkenyl, substituted and unsubstituted alkynyl, substituted and unsubstituted aryl , Substituted and unsubstituted heteroaryl, protonatable amine groups, pharmaceutically acceptable substituted and unsubstituted primary amine groups, structure Wa, structure W-1, structure W-2, structure W-3, structure W-4, structure W-5, structure W-6, structure W-7, structure W-8, structure W-9, structure W-10, structure W-11, structure W-12, structure W-13, structure Selected from the group consisting of W-14, Structure W-15, Structure W-16, Structure W-17, and Structure W-18;
Structure Wa Structure W-1 Structure W-2 Structure W-3
Structure W-4 Structure W-5 Structure W-6
Structure W-7 Structure W-8 Structure W-9
Structure W-10 Structure W-11 Structure W-12
Structure W-13 Structure W-14 Structure W-15
Structure W-16 structure W-17 structure W-18;

Z _{is, CH 2, S, SO,} SO 2, NH, NR 6, CHCH 3, CHCH 2 CH 3, CHR 6, R 6, -C (= O) -, and consisting of O is selected from the group;
AA represents any amino acid;
Each of m and n is independently 0 and an integer, for example 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20,. . . Selected from the group consisting of;
HA is nothing and a pharmaceutically acceptable acid, such as hydrochloride, hydrobromide, hydroiodide, nitric acid, sulfuric acid, disulfuric acid, phosphoric acid, phosphorous acid Phosphonic acid, isonicotinic acid, acetic acid, lactic acid, salicylic acid, citric acid, tartaric acid, pantothenic acid, tartaric acid, ascorbic acid, succinic acid, maleic acid, gentisic acid, fumaric acid, gluconic acid, glucuronic acid, Selected from the group consisting of saccharic acid, formic acid, benzoic acid, glutamic acid, methanesulfonic acid, ethanesulfonic acid, benzenesulfonic acid, p-toluenesulfonic acid, and pamoic acid;
R is nothing, H, CH ₂ C (═O) OR ₆ , substituted and unsubstituted alkyl, substituted and unsubstituted cycloalkyl, substituted and unsubstituted heterocycloalkyl, substituted and unsubstituted alkoxyl, substituted and unsubstituted Selected from the group consisting of perfluoroalkyl, substituted and unsubstituted alkyl halides, substituted and unsubstituted alkenyl, substituted and unsubstituted alkynyl, substituted and unsubstituted aryl, and substituted and unsubstituted heteroaryl, wherein any of R CH ₂ may be further substituted with O, S, P, NR ₆ , or any other pharmaceutically acceptable group;
R _{1 to} R ₃ are independently H, substituted and unsubstituted alkyl, substituted and unsubstituted cycloalkyl, substituted and unsubstituted heterocycloalkyl, substituted and unsubstituted alkyloxyl, substituted and unsubstituted alkenyl, substituted and unsubstituted Selected from the group consisting of alkynyl, substituted and unsubstituted aryl, and substituted and unsubstituted heteroaryl residues;
R ₅ and R ₃₅ are independently H, C (═O) NH ₂ , CH ₂ CH ₂ OR ₆ , CH ₂ CH ₂ N (CH ₃ ) ₂ , CH ₂ CH ₂ N (CH ₂ CH ₃ ) _2. , Cl, F, Br, I, substituted and unsubstituted alkyl, substituted and unsubstituted cycloalkyl, substituted and unsubstituted heterocycloalkyl, substituted and unsubstituted alkyloxyl, substituted and unsubstituted cycloalkyloxyl, substituted and unsubstituted aryl , Substituted and unsubstituted heteroaryl, substituted and unsubstituted alkylcarbonyl, substituted and unsubstituted alkylamino, —C (═O) —W, L ₁ -L ₄ -L ₂ —W, and W ;
R ₆ , R ₃₆ , and R ₄₆ are independently H, F, Cl, Br, I, Na ⁺ , K ⁺ , C (═O) R ₅ , 2-oxo-1-imidazolidinyl, phenyl, 5- Indanyl, 2,3-dihydro-1H-inden-5-yl, 4-hydroxy-1,5-naphthyridin-3-yl, substituted and unsubstituted alkyl, substituted and unsubstituted cycloalkyl, substituted and unsubstituted heterocycloalkyl Substituted and unsubstituted alkenyl, substituted and unsubstituted alkynyl, substituted and unsubstituted alkyloxyl, substituted and unsubstituted cycloalkyloxyl, substituted and unsubstituted aryl, substituted and unsubstituted heteroaryl, -C (= O) -W, -L ₁ -L ₄ -L ₂ -W, as well as selected from the group consisting of W;
R ₇ and R ₃₇ are independently H, F, Cl, Br, I, CH ₃ NHC (═O) CH ₂ CH (NHR ₈ ) C (═O), R ₅ N═C (NHR ₆ ) NHC (= O) -, C ( = O) CH 3, C (= O) R 6, PO (oR 5) oR 6, substituted and unsubstituted alkyl, substituted and unsubstituted cycloalkyl, substituted and unsubstituted heterocycloalkyl Substituted and unsubstituted alkyloxyl, substituted and unsubstituted alkenyl, substituted and unsubstituted alkynyl, substituted and unsubstituted aryl, substituted and unsubstituted heteroaryl, substituted and unsubstituted alkylcarbonyl, substituted and unsubstituted alkylamino, L _1- Selected from the group consisting of L ₄ -L ₂ -W, and C- (═O) —W;
R ₈ and R ₃₈ are independently H, F, Cl, Br, I, CH ₃ , C ₂ H ₅ , CF ₃ , CH ₂ CH ₂ F, CH ₂ CH ₂ Cl, CH ₂ CH ₂ Br, CH ₂ CH ₂ I, CH ₂ CHF ₂ , CH ₂ CF ₃ , CH ₂ F, CH ₂ Cl, CH ₂ Br, CH ₂ I, CH ₂ NR ₆ R ₇ , CH (NHR ₇ ) CH ₂ C (═O) _{_{_{NH 2, C 3 H 7,}}} C 4 H 9, C 5 H 11, R 6, C (= O) R 6, C (= O) NH 2, CH 2 C (= O) NH 2, CH 2 OC (═O) NH ₂ , PO (OR ₅ ) OR ₆ , C (CH ₃ ) ₂ C (═O) OR ₆ , CH (CH ₃ ) C (═O) OR ₆ , CH ₂ C (═O) OR _{6, C (= O) -W} , L 1 -L 4 -L 2 -W, W, substituted and unsubstituted perfluoroalkyl, substituted and unsubstituted alkyl, substituted and unsubstituted cycloalkyl, substituted and unsubstituted heteroaryl A cycloalkyl, substituted and unsubstituted alkoxyl, substituted and unsubstituted alkylamino, substituted and unsubstituted perfluoroalkyl, substituted and unsubstituted halogenated alkyl, and is selected from the group consisting of substituted and unsubstituted alkylcarbonyl;
R _{11 to} R ₁₆ are independently nothing, H, CH ₂ C (═O) OR ₁₁ , substituted and unsubstituted alkyl, substituted and unsubstituted cycloalkyl, substituted and unsubstituted heterocycloalkyl, substituted and unsubstituted Selected from the group consisting of substituted alkoxyl, substituted and unsubstituted perfluoroalkyl, substituted and unsubstituted alkyl halides, substituted and unsubstituted alkenyl, substituted and unsubstituted alkynyl, substituted and unsubstituted aryl, and substituted and unsubstituted heteroaryl;
X ₂ is H, C (═O), C (═S), CH ₂ (CH ₂ ) _n OR ₈ , Cl, F, Br, I, NO ₂ , CN, CF ₃ , C ₂ F ₅ , C ₃ F ₇ , OCF ₃ , OC ₂ F ₅ , NH ₂ , NHR ₆ , CH ₃ , C ₂ H ₅ , R ₆ , C (═O) NH ₂ , CH ₂ OC (═O) NH ₂ , CH ₂ C (= O) OR ₅ , CH ₂ (CH ₂ ) _n N (CH ₃ ) ₂ , CH ₂ (CH ₂ ) _n SO ₃ R ₅ , substituted and unsubstituted alkyl, substituted and unsubstituted cycloalkyl, substituted and unsubstituted Selected from the group consisting of heterocycloalkyl, substituted and unsubstituted perfluoroalkyl, substituted and unsubstituted alkyl, substituted and unsubstituted alkylthio, substituted and unsubstituted alkylamino, and substituted and unsubstituted alkyloxyl;
X ₃ is H, N ₃ , SO ₃ W, F, Cl, Br, OH, OCH ₃ , OR ₆ , CH ₃ , R ₆ , C (= O), C (= S), C (= O) OW, OW, selected from L ₁ -L ₄ -L ₂ -W, and the group consisting of I;
X ₄ is selected from the group consisting of N, CH, and CY ₁ ;
X ₅ and X ₃₅ are independently selected from the group consisting of nothing, C (═O), C (═S), OC (═O), CH ₂ , CH, S, O, and NR _5. ;
Y ₁ , Y ₃₁ , Y ₂ , Y ₃₂ , Y ₃ , and Y ₄ are independently H, OH, OW, OC (═O) W, L ₁ -L ₄ -L ₂ -W, OC (= _{_{O) CH 3, CH 3,}} C 2 H 5, C 3 H 7, C 4 H 9, R 6, SO 3 R 6, CH 2 OR 6, CH 2 OC (= O) R 6, CH 2 C ( _{_{= O) OR 8, OCH 3}} , OC 2 H 5, OR 6, CH 3 SO 2, R 6 SO 2, CH 3 SO 3, R 6 SO 3, NO 2, CN, CF 3, OCF 3, CH 2 (CH ₂ ) _n NR ₅ R ₆ , CH ₂ (CH ₂ ) _n OR ₆ , CH (C (═O) NH ₂ ) NHR ₆ , CH ₂ C (═O) NH ₂ , F, Br, I, Cl , CH = CHC (= O) NHCH 2 C (= O) OW, CH = CHC (= O) NHCH 2 L 1 -L 4 -L 2 -W, NR 8 C (= O) R 5, SO 2 NR ₅ R ₈ , C (═O) R ₅ , SR ₅ , substituted and non- Selected from the group consisting of substituted perfluoroalkyl, substituted and unsubstituted alkoxyl, substituted and unsubstituted alkylthio, substituted and unsubstituted alkylamino, substituted and unsubstituted perfluoroalkyl, substituted and unsubstituted alkyl halides, and substituted and unsubstituted alkylcarbonyl Is;
L ₁ is nothing, O, S, —OL ₃ —, —SL ₃ —, —N (L ₃ ) —, —N (L ₃ ) —CH ₂ —O, —N (L ₃ ) selected from the group consisting of —CH ₂ —N (L ₅ ) —, —O—CH ₂ —O—, —O—CH (L ₃ ) —O, and —S—CH (L ₃ ) —O—. Is;
L ₂ is nothing, O, S, —OL ₃ —, —SL ₃ —, —N (L ₃ ) —, —N (L ₃ ) —CH ₂ —O, —N (L _{_{_{3) -CH 2 -N (L 5}}} ) -, - O-CH 2 -O -, - O-CH (L 3) -O, -S-CH (L 3) -O -, - O-L 3 _{-, - N-L 3 -} , - S-L 3 -, - N (L 3) -L 5 -, and L ₃ is selected from the group consisting of;
L ₄ is C = O, C = S,
and
Selected from the group consisting of;
For each of L ₁ , L ₂ , and L ₄ , L ₃ and L ₅ are independently nothing, H, CH ₂ C (═O) O L ₆ , substituted and unsubstituted alkyl, substituted and unsubstituted Cycloalkyl, substituted and unsubstituted heterocycloalkyl, substituted and unsubstituted aryl, substituted and unsubstituted heteroaryl, substituted and unsubstituted alkoxyl, substituted and unsubstituted alkylthio, substituted and unsubstituted alkylamino, substituted and unsubstituted perfluoroalkyl, And any carbon or hydrogen independently selected from the group consisting of substituted and unsubstituted alkyl halides, independently, O, S, P, NL ₃ , or any other pharmaceutically acceptable group. Optionally substituted by;
L ₆ is independently H, OH, Cl, F, Br, I, substituted and unsubstituted alkyl, substituted and unsubstituted cycloalkyl, substituted and unsubstituted heterocycloalkyl, substituted and unsubstituted aryl, substituted and unsubstituted Selected from the group consisting of heteroaryl, substituted and unsubstituted alkoxyl, substituted and unsubstituted alkylthio, substituted and unsubstituted alkylamino, substituted and unsubstituted perfluoroalkyl, and substituted and unsubstituted alkyl halides, wherein any carbon or The hydrogen is further independently substituted by O, S, N, P (O) OL ₆ , CH═CH, C≡C, CHL ₆ , CL ₆ L ₇ , aryl, heteroaryl, or a cyclic group. Well;
L ₇ is independently H, OH, Cl, F, Br, I, substituted and unsubstituted alkyl, substituted and unsubstituted cycloalkyl, substituted and unsubstituted heterocycloalkyl, substituted and unsubstituted aryl, substituted and unsubstituted Selected from the group consisting of heteroaryl, substituted and unsubstituted alkoxyl, substituted and unsubstituted alkylthio, substituted and unsubstituted alkylamino, substituted and unsubstituted perfluoroalkyl, and substituted and unsubstituted alkyl halides, wherein any carbon or The hydrogen is further independently substituted by O, S, N, P (O) OL ₆ , CH═CH, C≡C, CHL ₆ , CL ₆ L ₇ , aryl, heteroaryl, or a cyclic group. Well;
Any CH ₂ group may be substituted with O, S, or NH.

Claims

Structure I-6, the structure I-8, the structure I-9, the structure I-10, the structure I-11, the structure I-12, the structure I-13, the structure I-14, the structure I-15, the structure I-16 , Structure I-17, Structure I-18, Structure I-19, Structure I-20, Structure I-21, Structure I-22, Structure I-23, Structure I-24, Structure I-25, Structure I-26 A highly permeable compound having a structure selected from the group consisting of Structure I-27, Structure I-28, Structure I-29, Structure I-30, Structure I-31, Structure I-32 and Structure I-33, The stereoisomer or pharmaceutically acceptable salt thereof :

Structure I-6

Structure I-8 Structure I-9

Structure I-10 Structure I-11

Structure I-12 Structure I-13

Structure I-14 Structure I-15

Structure I-16 Structure I-17

Structure I-18 Structure I-19

Structure I-20 Structure I-21

Structure I-22 Structure I-23

Structure I-26 Structure I-27

Structure I-28 Structure I-29

Structure I-30 Structure I-31

Structure I-32 Structure I-33

W represents the structure W-2;
HA is nothing, hydrochloride, hydrobromide, hydroiodide, nitric acid, sulfuric acid, disulfuric acid, phosphoric acid, phosphorous acid, phosphonic acid, isonicotinic acid, acetic acid, lactic acid, salicylic acid, citric acid Acid, tartaric acid, pantothenic acid, ditartaric acid, ascorbic acid, succinic acid, maleic acid, gentisic acid, fumaric acid, gluconic acid, glucuronic acid, saccharic acid, formic acid, benzoic acid, glutamic acid, methanesulfonic acid, ethanesulfonic acid, benzene Selected from the group consisting of sulfonic acid, p-toluenesulfonic acid, and pamoic acid;
R is nothing, is selected from substituted alkyl and unsubstituted alkyl or Ranaru group;
R ₁ is H, substituted and unsubstituted alkyl, substituted and unsubstituted cycloalkyl, substituted and unsubstituted heterocycloalkyl, substituted and unsubstituted alkyloxyl, substituted and unsubstituted alkenyl, substituted and unsubstituted alkynyl, substituted and unsubstituted Selected from the group consisting of aryl, and substituted and unsubstituted heteroaryl residues;
R ₅ is H, C (═O) NH ₂ , CH ₂ CH ₂ OR ₆ , CH ₂ CH ₂ N (CH ₃ ) ₂ , CH ₂ CH ₂ N (CH ₂ CH ₃ ) ₂ , Cl, F, Br , I, substituted and unsubstituted alkyl, substituted and unsubstituted cycloalkyl, substituted and unsubstituted heterocycloalkyl, substituted and unsubstituted alkyloxyl, substituted and unsubstituted cycloalkyloxyl, substituted and unsubstituted aryl, substituted and unsubstituted hetero aryl, substituted and unsubstituted alkylcarbonyl, substituted and unsubstituted alkylamino, -C (= O) -W, selected L ₁ -L ₄ -L ₂ -W, and from the group consisting of W;
R ₆ is H, F, Cl, Br, I, Na ⁺ , K ⁺ , 2-oxo-1-imidazolidinyl, phenyl, 5-indanyl, 2,3-dihydro-1H-inden-5-yl, 4- Hydroxy-1,5-naphthyridin-3-yl, substituted and unsubstituted alkyl, substituted and unsubstituted cycloalkyl, substituted and unsubstituted heterocycloalkyl, substituted and unsubstituted alkenyl, substituted and unsubstituted alkynyl, substituted and unsubstituted alkyl oxyl, substituted and unsubstituted cycloalkyl oxyl, substituted and unsubstituted aryl, substituted and unsubstituted heteroaryl, -C (= O) -W, -L 1 -L 4 -L 2 -W, and from the group consisting of W Selected;
R ₇ is H, F, Cl, Br, I, CH ₃ NHC (═O) CH ₂ CH (NHR ₈ ) C (═O), R ₅ N═C (NHR ₆ ) NHC (═O) —, C (═O) CH ₃ , C (═O) R ₆ , PO (OR ₅ ) OR ₆ , substituted and unsubstituted alkyl, substituted and unsubstituted cycloalkyl, substituted and unsubstituted heterocycloalkyl, substituted and unsubstituted alkyl Oxyl, substituted and unsubstituted alkenyl, substituted and unsubstituted alkynyl, substituted and unsubstituted aryl, substituted and unsubstituted heteroaryl, substituted and unsubstituted alkylcarbonyl, substituted and unsubstituted alkylamino, L ₁ -L ₄ -L _2- Selected from the group consisting of W, and C-(= O) -W;
R ₈ is H, F, Cl, Br, I, CH ₃ , C ₂ H ₅ , CF ₃ , CH ₂ CH ₂ F, CH ₂ CH ₂ Cl, CH ₂ CH ₂ Br, CH ₂ CH ₂ I, CH _{_{_{_{2 CHF 2, CH 2 CF 3}}}} , CH 2 F, CH 2 Cl, CH 2 Br, CH 2 I, C 3 H 7, C 4 H 9, C 5 H 11, R 6, C (= O) R 6 , C (═O) NH ₂ , CH ₂ C (═O) NH ₂ , CH ₂ OC (═O) NH ₂ , PO (OR ₅ ) OR ₆ , C (CH ₃ ) ₂ C (═O) OR ₆ _{, CH (CH 3) C (} = O) oR 6, CH 2 C (= O) oR 6, C (= O) -W, L 1 -L 4 -L 2 -W, W, substituted and unsubstituted alkyl Substituted and unsubstituted cycloalkyl, substituted and unsubstituted heterocycloalkyl, substituted and unsubstituted perfluoroalkyl, substituted and unsubstituted alkoxyl, substituted and unsubstituted alkylamino , Substituted and unsubstituted perfluoroalkyl, substituted and unsubstituted halogenated alkyl, and is selected from the group consisting of substituted and unsubstituted alkylcarbonyl;
R ₁₁ and R _12, independently, nothing is selected from substituted alkyl and unsubstituted alkyl or Ranaru group, provided that at least one of R _11, R ₁₂ and R is a substituted or unsubstituted alkyl;
X is nothing or CH ₂ or we selected;
X ₅ is selected from the group consisting of nothing, C (═O), OC (═O), CH ₂ , CH, S, O, and NR ₅ ;
Y ₁ , Y ₂ , Y ₃ , and Y ₄ are independently H, OH, OW, OC (═O) W, L ₁ -L ₄ -L ₂ -W, OC (═O) CH ₃ , CH _{_{_{3, C 2 H 5, C}}} 3 H 7, C 4 H 9, R 6, SO 3 R 6, CH 2 OR 6, CH 2 OC (= O) R 6, CH 2 C (= O) OR 8, OCH ₃ , OC ₂ H ₅ , OR ₆ , CH ₃ SO ₂ , R ₆ SO ₂ , CH ₃ SO ₃ , R ₆ SO ₃ , NO ₂ , CN, CF ₃ , OCF ₃ , CH ₂ (CH ₂ ) _n NR ₅ R ₆ , CH ₂ (CH ₂ ) _n OR ₆ , CH (C (═O) NH ₂ ) NHR ₆ , CH ₂ C (═O) NH ₂ , F, Br, I, Cl, CH═CHC (= _{O) NHCH 2 C (= O} ) OW, CH = CHC (= O) NHCH 2 L 1 -L 4 -L 2 -W, NR 8 C (= O) R 5, SO 2 NR 5 R 8, C ( _{_{= O) R 5, SR 5}} , substituted and unsubstituted Perufuru Roarukiru, substituted and unsubstituted alkoxyl, substituted and unsubstituted alkylthio, substituted and unsubstituted alkylamino, substituted and unsubstituted perfluoroalkyl, substituted and unsubstituted halogenated alkyl, and is selected from the group consisting of substituted and unsubstituted alkylcarbonyl, n is selected from the group consisting of 0 and an integer ;
L ₁ is nothing, O, S, —OL ₃ —, —SL ₃ —, —N (L ₃ ) —, —N (L ₃ ) —CH ₂ —O, —N (L ₃ ) selected from the group consisting of —CH ₂ —N (L ₅ ) —, —O—CH ₂ —O—, —O—CH (L ₃ ) —O, and —S—CH (L ₃ ) —O—. Is;
L ₂ is nothing, O, S, —OL ₃ —, —SL ₃ —, —N (L ₃ ) —, —N (L ₃ ) —CH ₂ —O, —N (L _{_{_{3) -CH 2 -N (L 5}}} ) -, - O-CH 2 -O -, - O-CH (L 3) -O, -S-CH (L 3) -O -, - O-L 3 _{-, - N-L 3 -} , - S-L 3 -, - N (L 3) -L 5 -, and L ₃ is selected from the group consisting of;
L ₄ is C = O, C = S,

and

Selected from the group consisting of;
For each of L ₁ , L ₂ , and L ₄ , L ₃ and L ₅ are independently nothing, H, CH ₂ C (═O) O L ₆ , substituted and unsubstituted alkyl, substituted and unsubstituted Cycloalkyl, substituted and unsubstituted heterocycloalkyl, substituted and unsubstituted aryl, substituted and unsubstituted heteroaryl, substituted and unsubstituted alkoxyl, substituted and unsubstituted alkylthio, substituted and unsubstituted alkylamino, substituted and unsubstituted perfluoroalkyl, And carbon or hydrogen may be independently further substituted with O, S, P 2 , or other pharmaceutically acceptable groups. ;
L ₆ is independently H, OH, Cl, F, Br, I, substituted and unsubstituted alkyl, substituted and unsubstituted cycloalkyl, substituted and unsubstituted heterocycloalkyl, substituted and unsubstituted aryl, substituted and unsubstituted Selected from the group consisting of heteroaryl, substituted and unsubstituted alkoxyl, substituted and unsubstituted alkylthio, substituted and unsubstituted alkylamino, substituted and unsubstituted perfluoroalkyl, and substituted and unsubstituted alkyl halides, wherein carbon or hydrogen is further, independently, O, S, N, CH = CH, C≡C, aryl, but it may also be substituted by a heteroaryl or a cyclic group.

A pharmaceutical composition comprising the highly permeable compound of claim 1 and a pharmaceutically acceptable carrier.

The pharmaceutical composition according to claim 2, wherein the pharmaceutically acceptable carrier is polar.

The pharmaceutical composition according to claim 2, wherein the pharmaceutically acceptable carrier is selected from the group consisting of alcohol, acetone, ester, water, and aqueous solution.

A pharmaceutical composition comprising a highly permeable compound according to claim 1, wherein the highly permeable compound according to claim 1 has a biological barrier when the pharmaceutical composition is administered to the biological barrier. The pharmaceutical composition that permeates.

6. A pharmaceutical composition according to claim 5 for treating a condition in a biological subject.

7. The pharmaceutical composition according to claim 6, wherein the condition is selected from the group consisting of pain, injury, and a condition associated with a microorganism.

8. The pharmaceutical composition of claim 7, wherein the condition associated with the microorganism is selected from the group consisting of a condition associated with a bacterium, a condition associated with a protozoan, a condition associated with a fungus, and a condition caused by a virus.

The conditions associated with the bacteria are infection, plague, glandular and pulmonary plague, anthrax, skin anthrax, pulmonary anthrax and gastrointestinal anthrax, Lyme disease, brucellosis, pertussis, acute enteritis, respiratory infections, parrot disease, non Gonococcal urethritis, trachoma, neonatal inclusion conjunctivitis, genopathic lymphogranuloma, pseudomembranous colitis, gas gangrene, food poisoning, anaerobic cellulitis, diphtheria, infant meningitis, hemorrhagic colitis, hemolytic uremic Syndrome, savage disease, pneumonia, bronchitis, peptic ulcer, Legionella disease, Pontiac fever, leptospirosis, listeriosis, leprosy, tuberculosis, mycoplasma pneumonia, gonorrhea, neonatal ophthalmitis, purulent arthritis, meningococcal disease , Waterhouse-Friedelxen syndrome, Rocky mountain spotted fever, typhoid salmonellosis, salmonellosis due to gastroenteritis and total enteritis, bacterial dysentery / bacteria Dysentery, cystitis, meningitis and sepsis, endometritis, otitis media, sinusitis, syphilis, necrotizing fasciitis, streptococcal pharyngitis, scarlet fever, rheumatic fever, impetigo, erysipelas, postpartum fever, And a pharmaceutical composition according to claim 8 selected from the group consisting of cholera.

The infectious disease state is liver, lung, stomach, brain, kidney, heart, ear, eye, nose, mouth, tongue, colon, pancreas, gallbladder, duodenum, rectal stomach, colorectal, intestine, vein, respiratory system, Infection status of organs selected from the group consisting of blood vessels, rectal anus, and pruritus, respiratory infection, upper respiratory tract infection, urinary tract infection, nosocomial infection, Pseudomonas aeruginosa infection, coagulase-positive staphylococci 10. selected from the group consisting of infections, skin infections, poisoning, acute bacterial endocarditis, sepsis, necrotizing pneumonia, implant prosthetic infections, and opportunistic infections due to sepsis and pneumonia The pharmaceutical composition as described.

9. The pharmaceutical composition according to claim 8, wherein the condition associated with the protozoa is selected from the group consisting of malaria, sleeping sickness, and toxoplasmosis.

The condition associated with the fungus is selected from the group consisting of aspergillosis, blastosis, ringworm, candidiasis, coccidioidomycosis, cryptococcosis, histoplasmosis, paracoccidioidomycosis, sporotrichosis, and zygomycosis Item 9. A pharmaceutical composition according to Item 8.

9. The pharmaceutical composition of claim 8, wherein the virus-related condition is selected from the group consisting of influenza, yellow fever, and AIDS.