JP7382316B2 - ヒト免疫応答をモジュレートするためのイミダゾピリミジンの使用 - Google Patents
ヒト免疫応答をモジュレートするためのイミダゾピリミジンの使用 Download PDFInfo
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- Medicinal Preparation (AREA)
Description
本出願は、35 U.S.C.§119(e)の下、2017年11月14日に出願された米国仮出願第62/586,137号に対して利益を主張するものであり、その内容全体は参照により本明細書に組み込まれる。
本開示は、国立衛生研究所(NIH)/国立アレルギー感染病研究所(NIAID)アジュバント発見プログラム(Adjuvant Discovery Program)によって授与されたHHSN272201400052Cの下での政府の支援によりなされた。政府は、本発明において一定の権利を有する。
ヒト免疫は健康と病気との両方に極めて重要であり、感染性疾患、アレルギー、およびがんを包含する複数の大病において中心的な役割を果たす。動物およびヒトの研究によって、ある小分子が免疫アクチベーターとして働くことが示唆されている。
本明細書に提供されるのは、ヒト免疫応答を増強することにおける使用のためのイミダゾピリミジン化合物である。イミダゾピリミジン化合物の治療的または予防的な使用が記載される。いくつかの態様において、イミダゾピリミジン化合物は、免疫を増強または修飾する剤(immune-enhancing or modifying agents)として単独で使用される。いくつかの態様において、イミダゾピリミジン化合物は、ワクチン組成物におけるアジュバントとして使用される。アジュバントは、防御免疫を最大化するためにワクチンの抗原に対する免疫応答を増強し得、長引かせ(prolong)得、およびモジュレートし(modulate)得る。いくつかの態様において、イミダゾピリミジンをワクチンアジュバントとして使用することは、脆弱な集団(例として、新生児(neonates)、高齢者(elderly)、または免疫無防備状態にある(immunocompromised)個体)において有効な免疫付与を可能にさせる。いくつかの態様において、イミダゾピリミジン化合物は、先天性免疫応答と適応免疫応答との両方を増強する。
R1Aは、置換もしくは非置換のフェニル、または置換もしくは非置換のベンジル、または置換もしくは非置換の6員ヘテロアリールである;
R1は、水素、ハロゲン、置換もしくは非置換のC1~6アルキル、-ORa、または-N(Ra1)2である;
RAの各場合は、ハロゲン、置換もしくは非置換のアルキル、置換もしくは非置換のアルケニル、置換もしくは非置換のアルキニル、置換もしくは非置換のカルボシクリル、置換もしくは非置換のヘテロシクリル、置換もしくは非置換のアリール、置換もしくは非置換のヘテロアリール、-ORa、-N(Ra1)2、-SRa、-CN、-C(=O)Ra、-C(=O)ORa、-C(=O)N(Ra1)2、または-NO2である;
RBの各場合は、ハロゲン、置換もしくは非置換のアルキル、置換もしくは非置換のアルケニル、置換もしくは非置換のアルキニル、置換もしくは非置換のカルボシクリル、置換もしくは非置換のヘテロシクリル、置換もしくは非置換のアリール、置換もしくは非置換のヘテロアリール、-ORa、-N(Ra1)2、-SRa、-CN、-C(=O)Ra、-C(=O)ORa、-C(=O)N(Ra1)2、または-NO2である;
Raの各場合は、独立して、水素、置換もしくは非置換のアシル、置換もしくは非置換のアルキル、置換もしくは非置換のアルケニル、置換もしくは非置換のアルキニル、置換もしくは非置換のカルボシクリル、置換もしくは非置換のヘテロシクリル、置換もしくは非置換のアリール、置換もしくは非置換のヘテロアリール、窒素原子へ付着されているとき窒素保護基、酸素原子へ付着されているとき酸素保護基、または硫黄原子へ付着されているとき硫黄保護基である;
Ra1の各場合は、独立して、水素、置換もしくは非置換のアシル、置換もしくは非置換のアルキル、置換もしくは非置換のアルケニル、置換もしくは非置換のアルキニル、置換もしくは非置換のカルボシクリル、置換もしくは非置換のヘテロシクリル、置換もしくは非置換のアリール、置換もしくは非置換のヘテロアリール、窒素原子へ付着されているとき窒素保護基であるか、あるいは、2個のRa1の場合は、結び合うことで、置換もしくは非置換の複素環式の環または置換もしくは非置換のヘテロアリール環を形成する;
aは、0、1、2、または3である;および
bは、0、1、2、または3である。
R2の各場合は、独立して、水素、ハロゲン、置換もしくは非置換のC1~6アルキル、-ORa、または-N(Ra1)2である;
RCの各場合は、独立して、ハロゲン、置換もしくは非置換のアルキル、置換もしくは非置換のアルケニル、置換もしくは非置換のアルキニル、置換もしくは非置換のカルボシクリル、置換もしくは非置換のヘテロシクリル、置換もしくは非置換のアリール、置換もしくは非置換のヘテロアリール、-ORa、-N(Ra1)2、-SRa、-CN、-C(=O)Ra、-C(=O)ORa、-C(=O)N(Ra1)2、または-NO2である;および
cは、0、1、2、3、4、または5である。
いくつかの態様において、組成物は、ワクチン組成物である。いくつかの態様において、イミダゾピリミジン化合物は、アジュバントである。いくつかの態様において、抗原は、ミョウバン上へ吸着されている。いくつかの態様において、イミダゾピリミジン化合物は、ミョウバン上へ吸着されている。いくつかの態様において、イミダゾピリミジン化合物は、脂質付加されている(lipidated)。
R1Aは、置換もしくは非置換のフェニル、または置換もしくは非置換のベンジル、または置換もしくは非置換の6員ヘテロアリールである;
R1は、水素、ハロゲン、置換もしくは非置換のC1~6アルキル、-ORa、または-N(Ra1)2である;
RAの各場合は、ハロゲン、置換もしくは非置換のアルキル、置換もしくは非置換のアルケニル、置換もしくは非置換のアルキニル、置換もしくは非置換のカルボシクリル、置換もしくは非置換のヘテロシクリル、置換もしくは非置換のアリール、置換もしくは非置換のヘテロアリール、-ORa、-N(Ra1)2、-SRa、-CN、-C(=O)Ra、-C(=O)ORa、-C(=O)N(Ra1)2、または-NO2である;
RBの各場合は、ハロゲン、置換もしくは非置換のアルキル、置換もしくは非置換のアルケニル、置換もしくは非置換のアルキニル、置換もしくは非置換のカルボシクリル、置換もしくは非置換のヘテロシクリル、置換もしくは非置換のアリール、置換もしくは非置換のヘテロアリール、-ORa、-N(Ra1)2、-SRa、-CN、-C(=O)Ra、-C(=O)ORa、-C(=O)N(Ra1)2、または-NO2である;
Raの各場合は、独立して、水素、置換もしくは非置換のアシル、置換もしくは非置換のアルキル、置換もしくは非置換のアルケニル、置換もしくは非置換のアルキニル、置換もしくは非置換のカルボシクリル、置換もしくは非置換のヘテロシクリル、置換もしくは非置換のアリール、置換もしくは非置換のヘテロアリール、窒素原子へ付着されているとき窒素保護基、酸素原子へ付着されているとき酸素保護基、または硫黄原子へ付着されているとき硫黄保護基である;
Ra1の各場合は、独立して、水素、置換もしくは非置換のアシル、置換もしくは非置換のアルキル、置換もしくは非置換のアルケニル、置換もしくは非置換のアルキニル、置換もしくは非置換のカルボシクリル、置換もしくは非置換のヘテロシクリル、置換もしくは非置換のアリール、置換もしくは非置換のヘテロアリール、窒素原子へ付着されているとき窒素保護基であるか、あるいは、2個のRa1の場合は、結び合うことで、置換もしくは非置換の複素環式の環または置換もしくは非置換のヘテロアリール環を形成する;
aは、0、1、2、または3である;および
bは、0、1、2、または3である。
R2の各場合は、独立して、水素、ハロゲン、置換もしくは非置換のC1~6アルキル、-ORa、または-N(Ra1)2である;
RCの各場合は、独立して、ハロゲン、置換もしくは非置換のアルキル、置換もしくは非置換のアルケニル、置換もしくは非置換のアルキニル、置換もしくは非置換のカルボシクリル、置換もしくは非置換のヘテロシクリル、置換もしくは非置換のアリール、置換もしくは非置換のヘテロアリール、-ORa、-N(Ra1)2、-SRa、-CN、-C(=O)Ra、-C(=O)ORa、-C(=O)N(Ra1)2、または-NO2である;および
cは、0、1、2、3、4、または5である。
いくつかの態様において、イミダゾピリミジン化合物は、抗原が単独で投与されたときと比較して、免疫応答速度を増大させる。
いくつかの態様において、対象は、感染性疾患を有するか、またはこれを発症するリスクがある。いくつかの態様において、感染性疾患は、細菌、抗酸菌、真菌、ウイルス、寄生体、またはプリオンによって引き起こされる。いくつかの態様において、感染性疾患は、敗血症である。
いくつかの態様において、対象は、アレルギー性疾患を有するか、またはこれを発症するリスクがある。
いくつかの態様において、対象は、ヒト成年者である。いくつかの態様において、対象は、高齢の個体である。いくつかの態様において、投与は、対象が年齢65歳(65 years of age)より高いときに行われる。いくつかの態様において、対象は、(例として、原発性免疫不全または後天性免疫不全に起因する)免疫無防備状態にある。
添付の図面は、縮尺どおりに描画されることを意図していない。図面中、様々な図において説明されている同一のまたはほぼ(nearly)同一の各構成要素は、同じ(like)数字によって表示される。明確にする目的上、どの構成要素も、図面ごとに標識されているとは限らない。図面中:
本開示のいくつかの側面は、イミダゾピリミジン化合物がヒト白血球のin vitroでの確固たる(robust)活性化を誘導し、かつin vivoでアジュバントとして働くという知見に、少なくとも一部基づく。結果的に、本明細書に提供されるのは、先天性免疫応答および適応免疫応答を包含するヒト免疫応答を修飾することにおける使用のためのイミダゾピリミジン化合物である。いくつかの態様において、イミダゾピリミジン化合物は、ワクチンにおいてアジュバントとして使用される。アジュバントは、防御免疫を最大化するために、ワクチンの抗原に対する免疫応答を増強し得、長引かせ得、かつモジュレートし得る。いくつかの側面において、イミダゾピリミジンをワクチンのアジュバントとして使用することは、脆弱な集団(例として、新生児、高齢者、または免疫無防備状態にある個体)における有効な免疫付与を可能にさせる。いくつかの態様において、イミダゾピリミジン化合物は、感染性疾患、がん、またはアレルギーの処置(予防的または治療的の両方)において使用される。いくつかの態様において、新規イミダゾピリミジン化合物は合成され、使用される。
本開示のいくつかの側面は、抗原およびイミダゾピリミジン化合物を含む組成物を提供する。「イミダゾピリミジン化合物」は、本明細書に使用されるとき、イミダゾピリミジンのコア構造を含むいずれの化合物(それらの類似体、誘導体、薬学的に許容し得る塩、溶媒和物、水和物、多形、共結晶、互変異性体、立体異性体、同位体標識された誘導体、またはプロドラッグを包含する)をも網羅する。いくつかの態様において、イミダゾピリミジンの一般コア構造は、式
R1Aは、置換もしくは非置換のフェニル、または置換もしくは非置換のベンジル、または置換もしくは非置換の6員ヘテロアリールである;
R1は、水素、ハロゲン、置換もしくは非置換のC1~6アルキル、-ORa、または-N(Ra1)2である;
RAの各場合は、ハロゲン、置換もしくは非置換のアルキル、置換もしくは非置換のアルケニル、置換もしくは非置換のアルキニル、置換もしくは非置換のカルボシクリル、置換もしくは非置換のヘテロシクリル、置換もしくは非置換のアリール、置換もしくは非置換のヘテロアリール、-ORa、-N(Ra1)2、-SRa、-CN、-C(=O)Ra、-C(=O)ORa、-C(=O)N(Ra1)2、または-NO2である;
RBの各場合は、ハロゲン、置換もしくは非置換のアルキル、置換もしくは非置換のアルケニル、置換もしくは非置換のアルキニル、置換もしくは非置換のカルボシクリル、置換もしくは非置換のヘテロシクリル、置換もしくは非置換のアリール、置換もしくは非置換のヘテロアリール、-ORa、-N(Ra1)2、-SRa、-CN、-C(=O)Ra、-C(=O)ORa、-C(=O)N(Ra1)2、または-NO2である;
Raの各場合は、独立して、水素、置換もしくは非置換のアシル、置換もしくは非置換のアルキル、置換もしくは非置換のアルケニル、置換もしくは非置換のアルキニル、置換もしくは非置換のカルボシクリル、置換もしくは非置換のヘテロシクリル、置換もしくは非置換のアリール、置換もしくは非置換のヘテロアリール、窒素原子へ付着されているとき窒素保護基、酸素原子へ付着されているとき酸素保護基、または硫黄原子へ付着されているとき硫黄保護基である;
Ra1の各場合は、独立して、水素、置換もしくは非置換のアシル、置換もしくは非置換のアルキル、置換もしくは非置換のアルケニル、置換もしくは非置換のアルキニル、置換もしくは非置換のカルボシクリル、置換もしくは非置換のヘテロシクリル、置換もしくは非置換のアリール、置換もしくは非置換のヘテロアリール、窒素原子へ付着されているとき窒素保護基であるか、あるいは、2個のRa1の場合は、結び合うことで、置換もしくは非置換の複素環式の環または置換もしくは非置換のヘテロアリール環を形成する;
aは、0、1、2、または3である;および
bは、0、1、2、または3である。
いくつかの態様において、R1Aは、置換もしくは非置換のピリジン、置換もしくは非置換のピリミジン、または置換もしくは非置換のピラジンである。
R2の各場合は、独立して、水素、ハロゲン、置換もしくは非置換のC1~6アルキル、-ORa、または-N(Ra1)2である;
RCの各場合は、独立して、ハロゲン、置換もしくは非置換のアルキル、置換もしくは非置換のアルケニル、置換もしくは非置換のアルキニル、置換もしくは非置換のカルボシクリル、置換もしくは非置換のヘテロシクリル、置換もしくは非置換のアリール、置換もしくは非置換のヘテロアリール、-ORa、-N(Ra1)2、-SRa、-CN、-C(=O)Ra、-C(=O)ORa、-C(=O)N(Ra1)2、または-NO2である;および
cは、0、1、2、3、4、または5である。
RCの各場合は、ハロゲン、置換もしくは非置換のアルキル、置換もしくは非置換のアルケニル、置換もしくは非置換のアルキニル、置換もしくは非置換のカルボシクリル、置換もしくは非置換のヘテロシクリル、置換もしくは非置換のアリール、置換もしくは非置換のヘテロアリール、-ORa、-N(Ra1)2、-SRa、-CN、-C(=O)Ra、-C(=O)ORa、-C(=O)N(Ra1)2、または-NO2である;および
cは、0、1、2、3、4、または5である。
「不飽和(の)」または「部分的に不飽和(の)」は、少なくとも1つの二重結合または三重結合を包含する基を指す。「部分的に不飽和」の環系は、不飽和を複数部位に有する環を網羅することをさらに意図するが、芳香族基(例として、アリールまたはヘテロアリール基)を包含することは意図しない。同じく、「飽和(の)」は、二重結合または三重結合を含有しない、すなわちすべて単結合を含有する基を指す。
本明細書に記載の原子、部分(moiety)、または基は原子価が許す限り、そのように明示的に提供されなければ、非置換であっても、または置換されていてもよい。用語「任意に置換されていてもよい」は、置換または非置換を指す。
「アシル」は、-C(=O)Raa、-CHO、-CO2Raa、-C(=O)N(Rbb)2、-C(=NRbb)Raa、-C(=NRbb)ORaa、-C(=NRbb)N(Rbb)2、-C(=O)NRbbSO2Raa、-C(=S)N(Rbb)2、-C(=O)SRaa、または-C(=S)SRaaからなる群から選択される部分を指すが、ここでRaaおよびRbbは、本明細書に定義されるとおりである。
本明細書に記載の組成物は、抗原およびイミダゾピリミジン化合物を含む。「抗原」は、抗体もしくは受容体によって結合される実体、または抗体の産生を誘導する実体を指す。いくつかの態様において、抗原は、抗原に特異的に結合する抗体の産生を増大させる。いくつかの態様において、抗原は、タンパク質またはポリペプチドを含む。かかるタンパク質またはペプチドは、本明細書中「免疫原性ポリペプチド」とも言及される。いくつかの態様において、用語「抗原」は、免疫原性ポリペプチドをコードする核酸(例として、DNAまたはRNA分子)を網羅する。いくつかの態様において、抗原は、微生物病原体からのものである。例えば、抗原は、細菌、ウイルス、菌類、および他の微生物の一部(parts)(外皮(coats)、カプセル、細胞壁、鞭毛、線毛、および毒素)を含んでいてもよい。いくつかの態様において、抗原は、がん特異的抗原である。
本開示の組成物は、抗原およびイミダゾピリミジン化合物を含む。いくつかの態様において、イミダゾピリミジン化合物は、抗原へ抱合されている。いくつかの態様において、イミダゾピリミジン化合物は、抗原へは抱合されていない。いくつかの態様において、イミダゾピリミジン化合物は、脂質付加されている。
本発明の他の側面は、対象における免疫応答を増強する方法を提供する。いくつかの態様において、方法は、有効量の本明細書に記載のイミダゾピリミジン化合物を対象へ投与することを含む(例として、自然免疫応答を増強するために、異種のまたは「訓練された」免疫または先天性記憶の誘導を包含する)。いくつかの態様において、方法は、有効量のイミダゾピリミジン化合物および有効量の抗原を(例として、抗原特異的免疫応答を増強するために)対象へ投与することを含む。いくつかの態様において、イミダゾピリミジン化合物は、抗原とは個別に投与される。いくつかの態様において、イミダゾピリミジン化合物は、抗原の投与に先立ち投与される。いくつかの態様において、イミダゾピリミジン化合物は、抗原の投与後に投与される。いくつかの態様において、イミダゾピリミジン化合物および抗原は、同時に投与される。いくつかの態様において、混和物(admixture)としてのイミダゾピリミジン化合物および抗原。
例1。イミダゾピリミジン化合物の免疫モジュレート活性
ヒト免疫は、健康と病気との両方に重大であって、感染性疾患、アレルギー性疾患、自己免疫疾患、ならびにがん腫瘍性疾患および慢性疾患において中心的役割を果たす。これに関連して、病気を予防および/または処置するためにヒト免疫系をモジュレートするアプローチを開発するという関心が高まっている。感染性疾患は、幼少時期における罹患および死亡の原因の第1位である。免疫付与は、感染性疾患を予防するのに鍵となるストラテジーである。しかしながら、新生子および未成年者の免疫付与は、次善の対応(responses)という結果になることもあって、しばしば複数回のブースター用量を要し、かつ徐々に弱くなる免疫によって限定され得る。アジュバント化(adjuvantation)は、ワクチンで誘導される免疫を増強する鍵となるアプローチである。アジュバントは、防御免疫を最大化させるために、ワクチン抗原に対する免疫応答を増強し得、長引かせ得、かつ増強し得、脆弱な集団において(例として、極めて年少および高齢の者において、または有効なワクチンを欠く疾患のために)有効な免疫付与を潜在的に可能にさせることがある。ワクチンアジュバントはまた、がん免疫治療薬としての潜在力も多いに保っている。アジュバントとして使用されてもよい小分子が報告されている。アレルギーから離れる方向へ免疫応答を向かわせ直す(例として、Th1/Th2バランスを元に戻す)ことにおける実用性もまた、いくつかの分子について実証されている(例として、J Immunol March 15, 1998, 160 (6) 2555-2559;およびAdv Drug Deliv Rev. 2009 Mar 28;61(3):256-62に記載のとおり、参照により本明細書に組み込まれる)。
(1)小分子カテゴリーは、大量生産/使用のための手頃な(affordable)規模拡大(scale up)に応じやすい(amenable to);
(2)化合物の分子足場は、同族体(congeners)/類似体の産生および創出への医薬品化学の視点から相対的に好ましいように見える;
(4)化合物は、確立された他の小分子アジュバント(例として、R848とは異なる)と比べて、別個のパターンのサイトカインを誘導するが、これは別個の活性を示唆する。
表1は、PBMCsにおけるTNF産生を刺激した際の、ベンチマーク化合物R848と比較した例示化合物の活性を提供する。具体的に言うと、TNF産生を、成年者PBMCsを化合物037類似体ファミリーまたは化合物R848で33μMにて18時間刺激した後、ELISAによって測定した。類似体を、R848と比較した中央値パーセンテージTNF産生(TNF%)によって上位から下位までランク付けする(N=3~5)。化合物を、TNF%に従い以下のカテゴリー:高活性-クラスA:TNF%>15%;中(medium)活性-クラスB:1%<TNF%≦15%;低活性-クラスC:TNF%≦1%に分類した。
要旨。
ヒト免疫細胞を堅固に活性化する免疫モジュレーター/アジュバントを同定するため、THP1 NF-κBレポーター細胞に対して試験された~200,000の小分子のスクリーニングを行った。THP-1細胞などの細胞培養株が天然の初代ヒト白血球の応答とは一致しないこともあるという証拠から、より小さな規模の新規ハイスループットスクリーニング方法論もまた採用した。ここで、~9,000の市販の化合物(THP-1スクリーニングからの相対的に高い#のヒットを有する小分子ライブラリプレートに焦点を合わせた)を、3名の異なる成年ヒトドナーからの初代ヒト血液単核細胞およびTNFαLISAアッセイ(PerkinElmerから商業的に購入した)を使用してスクリーニングした。Schildberger et al., Mediators of Inflammation, Volume 2013, Article ID 697972 (2013)を参照。
THP1-Lucia(商標)細胞株をInvivogen(San Diego, CA)から得た。白血病をもつ少年(boy)の血液に由来するヒト単球細胞であるTHP1-Lucia細胞は、NF-kB誘導性Lucレポーター構築物を含有する。これによって、NF-kBの活性化が、分泌されたルシフェラーゼ酵素からの発光を定量することによって測定され得る。THP1-Lucia細胞を、10%非加熱不活性化されたウシ胎仔血清(fetal bovine serum)(FBS)、10mM HEPES、1.0mMピルビン酸ナトリウム、50ug/ml Pen-Strep、および100ug/mL Normocin(商標)で補充されたRPMI 1640中で培養した。一旦培養したら、細胞を、5%CO2および加湿雰囲気をもつ37oCインキュベーター中に保管した。細胞を2~3日ごとに継代し、2.0×106細胞/ml培地の濃度を超えないようにした。
スクリーニングされた化合物ライブラリは、知られている生物活性と、様々な供給源からの商用ライブラリ(例として、ChemDiv、ChemBridge、およびAsinexなどの商用ライブラリ;添付pdfのすべてのライブラリを参照)とを包含した。すべてのライブラリはInstitute of Chemistry and Cell Biology(ICCB)-Longwood(Harvard Medical School)によって所有かつ提供された。
15代と18代との間の継代であって培養培地中に懸濁されたTHP1-Lucia細胞を、Combi液体ディスペンサを使用し30,000細胞/30μl/ウェルにて384ウェル黒色透明底プレート(Corning 3712)中へ分注した。免疫刺激活性が知られているベンチマーク小分子との比較を可能にするため、同じ濃度での細胞を0.3%DMSO中50μM R848、TLR7/8アゴニストで刺激し、細胞が存在しない状態の列24の1つおきのウェルへ多チャネルピペットによって同体積にて加えた。THP1培養培地および2.3%DMSO中の700nM酢酸ミリスチン酸ホルボール(PMA)(知られている末梢血細胞マイトジェン)の5μlを、多チャネルピペットによって列23の1つおきのウェルへ加えた(ウェル中の最終濃度:0.3%DMSO中100nM)。2.3%DMSOをもつTHP1培養培地の5μlを、多チャネルピペットによって列23の残りのウェルへ加えた(最終濃度0.3%DMSO)。100%DMSOに希釈されたライブラリ化合物の100nlアリコートを、Seikoピン移動機を使用しそれらの元の384ウェルプレートからアッセイプレートへ移した。各ライブラリプレートは二通りにピン移動させた(pinned)ものであり、比較のために同一条件をもつ2つのアッセイプレートを生産したことになる。次いでプレートを高湿度条件中5%CO2で37Cにて24時間インキュベートした。インキュベーションの後に10μLの上清を各ウェルから除去し、Vprep液体移動機を使用して白色プレート(Corning 3570)へ移した。THP1培養培地中1:2000に希釈された組み換えLuciタンパク質(Invivogen)の10μLを、空のウェル24Pへ加えた。Combi液体ディスペンサーを使用し、滅菌水中1:3に希釈した50μL/ウェルのQuanti-Luc基質(Invivogen)をアッセイプレートへ加えた。基質を加えた直後に、発光を、PerkinElmer Envisionプレートリーダーを使用して読んだ。
ヒト成年者末梢血を承認されたプロトコルに従って収集した。PBMCsをフィコール密度勾配から血液を単離した。PBMCsを、20%自己血漿および10%DMSOを含有する1mL RPMI中バイアルあたり5×107細胞にて使用するまで-80℃にて保管した。第1日にPBMCsを37℃水浴中3min解凍し、PBSで2度洗浄した。生存率をトリパンブルー染色によって査定し、次いで細胞を6.67×105生存細胞/mL(10%自己血漿をもつDMEM)になるよう再懸濁した。Corning 2712黒色384ウェル細胞培養プレート中1ウェルにつき30μlの細胞を分注した(最終濃度は20,000細胞/ウェルであった)。対照を細胞へ手動で加え、試験化合物をロボットのピン移動によって加えた。次いでプレートを37℃/5%CO2湿度制御インキュベーターにて18時間インキュベートした。アッセイの第2日にプレートを遠心分離し、2μl上清をPerkin Elmerアルファプレート中へ収集した。Perkin Elmer Human TNFαキット(cat# AL208F)を上清からTNFαの存在を検出するために使用した。プレートをEnVision(Perkin Elmer)器械上で走らせて615nmでの光放射を検出した。
二通りにおいて、かつPBMCsの3名のヒト試料のうち≧2つとも、確固たるZスコア>2をもたらした試験化合物をヒットと見なした。
以下のヒット判定の標準操作手順書(SOPs)をTHP-1およびTNFαLISAアッセイのために使用した:
=IF(C2="X",LOG10(E2),"")
=IF(C2="X",ABS(K2-$I$3),"")ここでK2はlog変換されたデータ点であり、およびI3は、そのプレートのその読み出しの中央値の値である。
=中央値(M2:M385)*1.4286
次いで確固たるZスコアを、(ウェル_値-中央値_プレート)/(MAD_プレート*1.4286)として算出し、算出例を下に示す:
=IF($C2="X",((K2-$I$3)/$I$5),"")ここでK2は対数変換ウェルの値であり、I3はその読み出しのプレート実験の中央値であり、およびI5はその読み出しのプレート実験のMADである。
=IF(AND((O2>$I$7),(P2>$J$7),($C2="X")),TRUE,FALSE)ここでO2およびP2は二通りの発光読み出しの確固たるZスコアである一方、I7およびJ7は、発光の確固たるZスコア閾値(2)を表す。「TRUE」は、化合物がこれらヒット基準を満たす場合、列Qに戻すことになる。
=IF(Q2,CONCATENATE(A2,":",B2),"")これにおいてQ2は、化合物のヒットステータス(hit status)を決定するTRUE/FALSE値である一方、A2はプレートIDであり、およびB2はウェルIDである。
ヒトPBMCsおよびDC刺激に由来する上清をTNFにつきELISAによってアッセイした(ThermoFisher Scientific; Waltham, MA, USA)。細胞培養上清中のサイトカインおよびケモカイン発現プロファイル(例として、IFNγ、IL-10、IL-12(p70)、IL-1β、IL-6、IL-8、MIP-1α/CCL3、TNF、およびGM-CSF)を、製造業者の取扱説明書に従いカスタマイズされた9重のMilliplex(登録商標) Human Th17 Magnetic Bead Pane(Millipore, Chicago, IL, USA)lを使用し測定した。アッセイをLuminex(登録商標)100/200(商標)系およびxPOTENT(登録商標)ソフトウェア(Luminex, Austin, TX)上で読み分析した。最小限の閾値を個々の各アッセイにつき最小限検出可能な濃度にて設定し、平均バックグラウンドを上回る3つの標準偏差として定義した。
PBMCsを、フィコール密度勾配を使用し血液から単離した。PBMCsは新鮮なまま使用するか、または20%自己血漿および10%DMSOを含有する1mL RPMI中バイアルあたり5×107細胞にて使用するまで-80℃にて保管するかのいずれかであった。刺激プレートを、0.66μlのDMSOに溶解された化合物(10mM)を丸底96ウェルプレートの各ウェルへ移すことによって調製した。ヒト成年ドナーまたは高齢ドナーから単離されたPBMCsを、105細胞/200μl(10%の乏血小板血漿で補充されたRPMI)の濃度にて再懸濁した。200μlの細胞懸濁液を各ウェルへ移し、33μMの最終化合物濃度をもたらした。18時間のインキュベーション(37℃、5%CO2)後にプレートを遠心分離し(500×g、室温、5分)、上清をさらなる分析のために回収した。
ヒト新生子臍帯血を、パイロジェンフリーのヘパリンを抗凝固薬として使用した帝王切開の直後の正期産児(term newborns)(N=5)から収集した。臍帯血をRPMI 1640培地中1:1(v/v)に希釈した。1マイクロリットルの、指摘された化合物の各々(または対照条件としてのDMSO)を、96ウェル丸底プレート中200マイクロリットルの希釈血液を含有する各ウェルへ11μMの最終濃度にて加えた。次いでプレートを5%CO2の存在下37℃にて加湿されたインキュベーター中18時間インキュベートした。次いでプレートを遠心分離し(500×g、室温、5分)、上清をさらなる分析のために回収した。
C57BL/6およびBALB/cマウスは、Taconic BiosciencesまたはCharles River Laboratoriesから得た。これらをBoston Children’s Hospitalでの動物研究施設中、特定病原体除去条件において収容した。
脾臓を6~8週齢C57BL/6マウスから回収した。脾細胞単離のため、脾臓を70μM漉し器に通してすりつぶしてPBSで洗浄し、赤血球を塩化アンモニウムベースの溶解(lysis)緩衝液(BD Biosciences)中2minのインキュベーションで溶解した(lysed)。次いで細胞を計数し、33μMの最終化合物濃度を獲得するために0.66μlのDMSO溶解(-dissolved)化合物(10mM)をもつ200μlの完全培養培地(RPMI 1640に、10%熱不活性化ウシ胎仔血清[FBS、GE Healtycare HyClone]、50μM 2-メルカプトエタノール、2mM l-グルタミン、100U/ml ペニシリン/ストレプトマイシン[Gibco ThermoFisher Scientific]をプラスして)中1ウェル(丸底96ウェルプレート)あたり2×106個播種した。18時間のインキュベーション(37℃、5%CO2)後、プレートを遠心分離し(500×g、室温、5分)、上清をさらなる分析のために回収した。
免疫付与実験につき、成体マウスを、FluBlokワクチン(Protein Sciences Corp.)の2016~2017年の製剤中に含有される、0.33μgの以下の組み換えインフルエンザウイルス血球凝集素(rHA)の各々:A/Michigan/45/2015(H1N1)、A/Hong Kong/4801/2014(H3N2)、およびB/Brisbane/60/2008を含有する、50μlのワクチンで右大腿後部の筋肉内に(i.m.)免疫した。マウスをプライム・ブーストスケジュール(4週空けて(apart)2回の注射)で免疫した。すべての実験群におけるワクチンを、10%(v/v)DMSO(小分子をDMSOに溶解したところ、小分子で免疫された群は除いた)および5%(v/v)Tween-80で製剤化した。特定の実験群について指摘したとおり、ワクチンをまた、水酸化アルミニウム(100μg)および/または化合物037(100nmol、最終DMSO濃度10%)でも製剤化した。血清をプライムから28日後に収集し(ブースト前(pre-boost)の血液試料)、抗体検出のためブーストから14日後に収集した。rHA特異的IgGをELISAによって定量化した。高結合(High binding)平底96ウェルプレート(Corning Life Sciences)を炭酸塩緩衝液(carbonate buffer)中1μg/ml rHA(pH 9.6)でコーティングし、4℃にて終夜インキュベートし、PBS+BSA 1%(Sigma-Aldrich)で室温にて(RT)1hブロッキングした。次いで、ワクチン接種されたマウスからの血清を、PBS+BSA 1%中、1:100の初期希釈および1:4の段階希釈となるように加え、rtにて2hインキュベートした。次いでプレートを洗浄し、HRP抱合抗マウスIgG(Southern Biotech)とともにrtにて1hインキュベートした。インキュベーションの終わりにプレートを再度洗浄して、テトラメチルベンジジン(BD Biosciences)で5分間現像し、次いで1N H2SO4で停止させた。光学密度を450nmにて、SoftMax Pro Version 5付きVersamaxマイクロプレートリーダー(ともにMolecular Devicesから)で読み、エンドポイント力価を、バックグラウンドの光学密度を3回カットオフ(cutoff)として使用し算出した。
統計的有意性および図形出力は、Prism v. 5.0b(GraphPad Software)およびMicrosoft Excel(Microsoft Corporation, Redmond, WA)を使用して生成した。結果をp値<0.05にて有意であると見なし、かつ以下:*p<0.05、**p<0.01のように指摘した。
本明細書に提供される化合物は、容易に入手可能な出発材料から以下の一般の方法および手順を使用して調製し得る。例えば、式(I)で表される化合物はスキーム1に従って調製し得る。典型的なまたは好ましいプロセス条件(すなわち、反応温度、時間、反応物のモル比率、溶媒、圧力等々)が与えられている場合、他のプロセス条件もまた、そのように述べられない限り使用し得る。最適反応条件は使用される具体的な反応物または溶媒とともに変動することもあるが、かかる条件は、最適化手順により当業者によって決定され得る。
スキーム1-例1の調製
N-(2-メチル-5-(6-メチルイミダゾ[1,2-a]ピリミジン-2-イル)フェニル)-2-フェニルブタンアミド
N-(5-(6-フルオロイミダゾ[1,2-a]ピリミジン-2-イル)-2-メチルフェニル)-2-フェニルブタンアミド
当業者は、わずかな型どおりの実験法を使用し、本明細書に記載の態様の多くの均等物を認識するか、または解明できるであろう。本開示の範囲は、上の記載に限定されることを意図しておらず、むしろ添付のクレームで表されるとおりである。
Claims (18)
- 抗原および式:
を含む、組成物。 - 抗原が、タンパク質またはポリペプチドを含む、および/または抗原が、タンパク質またはポリペプチドをコードする核酸を含む、請求項1に記載の組成物。
- 抗原が、微生物病原体からのものである、請求項1または2に記載の組成物。
- 抗原が、がん特異的抗原である、請求項1~3のいずれか一項に記載の組成物。
- 抗原が、リポ多糖(LPS)を含む、請求項1に記載の組成物。
- 組成物が、ワクチン組成物である、請求項1~5のいずれか一項に記載の組成物。
- (i) 化合物が、アジュバントである;および/または
(ii) 抗原が、ミョウバン上へ吸着されている;および/または
(iii) 化合物が、ミョウバン上へ吸着されている;および/または
(iv) ワクチン組成物が、第2アジュバントをさらに含む、
請求項6に記載の組成物。 - 抗原と、
式:
を含む、ワクチン。 - 有効量の抗原および有効量の式:
を含む、医薬組成物であって、
抗原に対する免疫応答の増強を、これを必要とする対象においてする方法における使用のための、前記医薬組成物。 - 抗原が、請求項1~5のいずれか一項に記載のものである、請求項9に記載の使用のための医薬組成物。
- 化合物が、対象において、抗原が単独で投与されたときと比較して、抗原に対する防御効果を長引かせる、請求項9または10に記載の使用のための医薬組成物。
- 投与が、予防的なものである、請求項9~11のいずれか一項に記載の使用のための医薬組成物。
- 対象が、ヒト新生児、未成年者、成年者、または高齢者である、請求項9~12のいずれか一項に記載の使用のための医薬組成物。
- 対象が、投与時に28日齢未満であるヒト未成年者である、請求項9~13のいずれか一項に記載の使用のための医薬組成物。
- 第2の投与が、対象が6月齢未満であるときに行われる、請求項9~14のいずれか一項に記載の使用のための医薬組成物。
- 対象にワクチン接種をする方法、または疾患の処置を、これを必要とする対象においてする方法における使用のための、請求項1~7のいずれか一項に記載の組成物、または請求項8に記載のワクチン。
- 式:
を含む、医薬組成物であって、
免疫応答の増強を、これを必要とする対象においてする方法における使用のための、前記医薬組成物。 - (i) 免疫応答が、自然免疫応答である;および/または
(ii) 化合物が、末梢血単核球(PBMC)を活性化する;および/または
(iii) 化合物が、パターン認識受容体(PRR)を活性化する、
請求項17に記載の使用のための医薬組成物。
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WO2019099578A1 (en) | 2019-05-23 |
EP3710007A1 (en) | 2020-09-23 |
KR20200088398A (ko) | 2020-07-22 |
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JP2023175686A (ja) | 2023-12-12 |
US11730810B2 (en) | 2023-08-22 |
CN111587114A (zh) | 2020-08-25 |
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