JP7412008B2 - ジドブジン及び抗微生物化合物を含む組み合わせ - Google Patents
ジドブジン及び抗微生物化合物を含む組み合わせ Download PDFInfo
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- JP7412008B2 JP7412008B2 JP2020560822A JP2020560822A JP7412008B2 JP 7412008 B2 JP7412008 B2 JP 7412008B2 JP 2020560822 A JP2020560822 A JP 2020560822A JP 2020560822 A JP2020560822 A JP 2020560822A JP 7412008 B2 JP7412008 B2 JP 7412008B2
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- pharmaceutically acceptable
- zidovudine
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- mycobacterium
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- WBYWAXJHAXSJNI-VOTSOKGWSA-M trans-cinnamate Chemical compound [O-]C(=O)\C=C\C1=CC=CC=C1 WBYWAXJHAXSJNI-VOTSOKGWSA-M 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- IEDVJHCEMCRBQM-UHFFFAOYSA-N trimethoprim Chemical compound COC1=C(OC)C(OC)=CC(CC=2C(=NC(N)=NC=2)N)=C1 IEDVJHCEMCRBQM-UHFFFAOYSA-N 0.000 description 1
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
- A61K31/7072—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/429—Thiazoles condensed with heterocyclic ring systems
- A61K31/43—Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems
- A61K31/431—Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems containing further heterocyclic rings, e.g. ticarcillin, azlocillin, oxacillin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/542—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
- A61K31/545—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/66—Phosphorus compounds
- A61K31/665—Phosphorus compounds having oxygen as a ring hetero atom, e.g. fosfomycin
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
Description
(I)mRNAレベル(例:mRNAのレベルの0.0001から50%、例えば1から30%、5から25%又は10から20%);及び/又は
(II)ウリジン(例えば[3H]ウリジン)取り込みレベル(例:[3H]ウリジン取り込みのレベルの0.0005から50%、例えば1から40%、15から35%又は20から30%)
を有する。
グラム陰性球菌、例えば、ナイセリア・ゴノロア(Neisseria gonorrhoeae)、ナイセリア・メニンギティディス(Neisseria meningitidis)、ナイセリア・シネレア(Neisseria cinerea)、ナイセリア・エロンガタ(Neisseria elongata)、ナイセリア・フラベセンス(Neisseria flavescens)、ナイセリア・ラクタミカ(Neisseria lactamica)、ナイセリア・ムコサ(Neisseria mucosa)、ナイセリア・シッカ(Neisseria sicca)、ナイセリア・スブフラバ(Neisseria subflava)及びナイセリア・ウェアベリ(Neisseria weaveri);バチルス科、例えば、バチルス・アントラシス(Bacillus anthracis)、バチルス・スブチリス(Bacillus subtilis)、バチルス・スリンギエンシス(Bacillus thuringiensis)、バチルス・ステアロテルモフィルス(Bacillus stearothermophilus)及びバチルス・セレウス(Bacillus cereus);腸内細菌科、例えば、大腸菌(Escherichia coli)、エンテロバクター属(例えば、エンテロバクター・エロゲネス(Enterobacter aerogenes)、エンテロバクター・アグロメランス(Enterobacter agglomerans)及びエンテロバクター・クロアカ(Enterobacter cloacae))、シトロバクター属(シトロバクター・フレウンジ(Citrob. freundii)及びシトロバクター・ジベルニス(Citrob. divernis)など)、ハフニア属(例えば、ハフニア・アルベイ(Hafnia alvei))、エルウィニア属(例えば、エルウィニア・ペルシシヌス(Erwinia persicinus))、モルガネラ・モルガニ(Morganella morganii)、サルモネラ菌 (サルモネラ・エンテリカ(Salmonella enterica)及びサルモネラ・チフィ(Salmonella typhi))、シゲラ菌(例えば、シゲラ・ジセンテリア(Shigella dysenteriae)、シゲラ・フレクスネリ(Shigella flexneri)、シゲラ・ボイジ(Shigella boydii)及びシゲラ・ソネイ(Shigella sonnei))、クレブシエラ菌(例えば、クレブシエラ・ニューモニエ(Klebs. pneumoniae)、クレブシエラ・オキシトカ(Klebs. oxytoca)、クレブシエラ・オルニトリティカ(Klebs. ornitholytica)、クレブシエラ・プランチコラ(Klebs. planticola)、クレブシエラ・オザナエ(Klebs. ozaenae)、クレブシエラ・テリゲナ(Klebs. terrigena)、クレブシエラ・グラヌロマティス(Klebs. granulomatis)(カリマトバクテリウム・グラヌロマティス(Calymmatobacterium granulomatis))及びクレブシエラ・リノスクレロマティス(Klebs. rhinoscleromatis))、プロテウス属(例えば、プロテウス・ミラビリス(Pr. mirabilis)、プロテウス・レトゲリ(Pr. rettgeri)及びプロテウス・バルガリス(Pr. vulgaris))、プロビデンシア属(例えば、プロビデンシア・アルカリファシエンス(Providencia alcalifaciens)、プロビデンシア・レトゲリ(Providencia rettgeri)及びプロビデンシア・スツアルティ(Providencia stuartii))、セラチア属(例えば、セラチア・マルセセンス(Serratia marcescens)及びセラチア・リキファシエンス(Serratia liquifaciens))並びにエルシニア属(例えば、エルシニア・エンテロコリティカ(Yersinia enterocolitica)、エルシニア・ペスティス(Yersinia pestis)及びエルシニア・シュードツベルクロシス(Yersinia pseudotuberculosis));腸球菌(例えば、エンテロコッカス・アビウム(Enterococcus avium)、エンテロコッカス・カセリフラバス(Enterococcus casseliflavus)、エンテロコッカス・セコラム(Enterococcus cecorum)、エンテロコッカス・ジスパル(Enterococcus dispar)、エンテロコッカス・デュランス(Enterococcus durans)、エンテロコッカス・フェカリス(Enterococcus faecalis)、エンテロコッカス・フェシウム(Enterococcus faecium)、エンテロコッカス・フラベセンス(Enterococcus flavescens)、エンテロコッカス・ガリナルム(Enterococcus gallinarum)、エンテロコッカス・ヒラエ(Enterococcus hirae)、エンテロコッカス・マロドラタス(Enterococcus malodoratus)、エンテロコッカス・ムンドチ(Enterococcus mundtii)、エンテロコッカス・シュードアビウム(Enterococcus pseudoavium)、エンテロコッカス・ラフィノサス(Enterococcus raffinosus)及びエンテロコッカス・ソリタリウス(Enterococcus solitarius));ヘリコバクター属(例えば、ヘリコバクター・ピロリ(Helicobacter pylori)、ヘリコバクター・シナエジ(Helicobacter cinaedi)及びヘリコバクター・フェネリア(Helicobacter fennelliae));アシネトバクター属(例えば、アシネトバクター・バウマニ(A. baumanii)、アシネトバクター・カルコアセチカス(A. calcoaceticus)、アシネトバクター・ヘモリティカス(A. haemolyticus)、アシネトバクター・ジョンソニ(A. johnsonii)、アシネトバクター・ジュニ(A. junii)、アシネトバクター・ルウォフィ(A. lwoffi)及びアシネトバクター・ラジオレシステンス(A. radioresistens));シュードモナス属(例えば、シュードモナス・エルギノーサ(Ps. aeruginosa)、シュードモナス・マルトフィリア(Ps. maltophilia)(ステノトロフォモナス・マルトフィリア(Stenotrophomonas maltophilia))、シュードモナス・アルカリジェネス(Ps. alcaligenes)、シュードモナス・クロロラフィス(Ps. chlororaphis)、シュードモナス・フルオレセンス(Ps. fluorescens)、シュードモナス・ルテオラ(Ps. luteola)、シュードモナス・メンドシナ(Ps. mendocina)、シュードモナス・モンテイリ(Ps. monteilii)、シュードモナス・オリジハビタンス(Ps. oryzihabitans)、シュードモナス・ペルトシノゲナ(Ps. pertocinogena)、シュードモナス・シューダルカリジェネス(Ps. pseudalcaligenes)、シュードモナス・プチダ(Ps. putida)及びシュードモナス・スツゼリ(Ps. stutzeri));バクテリオイデス・フラギリス(Bacteriodes fragilis);ペプトコッカス属(例えば、ペプトコッカス・ニガー(Peptococcus niger));ペプトストレプトコッカス属;クロストリジウム属(例えば、クロストリジウム・ペルフリンゲンス(C. perfringens)、クロストリジウム・ジフィシレ(C. difficile)、クロストリジウム・ボツリナム(C. botulinum)、クロストリジウム・テタニ(C. tetani)、クロストリジウム・アブソナム(C. absonum)、クロストリジウム・アルゲンチネンセ(C. argentinense)、クロストリジウム・バラチ(C. baratii)、クロストリジウム・ビフェルメンタンス(C. bifermentans)、クロストリジウム・ベイジェリンキ(C. beijerinckii)、クロストリジウム・ブチリカム(C. butyricum)、クロストリジウム・カダベリス(C. cadaveris)、クロストリジウム・カルニス(C. carnis)、クロストリジウム・セラタム(C. celatum)、クロストリジウム・クロストリジオフォルム(C. clostridioforme)、クロストリジウム・コクレアリウム(C. cochlearium)、クロストリジウム・コクレアタム(C. cocleatum)、クロストリジウム・ファラックス(C. fallax)、クロストリジウム・ゴニ(C. ghonii)、クロストリジウム・グリコリカム(C. glycolicum)、クロストリジウム・ヘモリティカム(C. haemolyticum)、クロストリジウム・ハスチフォルム(C. hastiforme)、クロストリジウム・ヒストリティカム(C. histolyticum)、クロストリジウム・インドリス(C. indolis)、クロストリジウム・イノカム(C. innocuum)、クロストリジウム・イレグラレ(C. irregulare)、クロストリジウム・レプタム(C. leptum)、クロストリジウム・リモサム(C. limosum)、クロストリジウム・マレノミナタム(C. malenominatum)、クロストリジウム・ノビ(C. novyi)、クロストリジウム・オロチカム(C. oroticum)、クロストリジウム・パラプトリフィカム(C. paraputrificum)、クロストリジウム・ピリフォルム(C. piliforme)、クロストリジウム・プトレファシエンス(C. putrefasciens)、クロストリジウム・ラモサム(C. ramosum)、クロストリジウム・セプチカム(C. septicum)、クロストリジウム・ソルデリ(C. sordelii)、クロストリジウム・スフェノイデス(C. sphenoides)、クロストリジウム・スポロゲネス(C. sporogenes)、クロストリジウム・スブテルミナレ(C. subterminale)、クロストリジウム・シンビオサム(C. symbiosum)及びクロストリジウム・テルチウム(C. tertium));マイコプラズマ属(例えば、マイコプラズマ・ニューモニエ(M. pneumoniae)、マイコプラズマ・ホミニス(M. hominis)、マイコプラズマ・ゲニタリウム(M. genitalium)及びマイコプラズマ・ウレアリチカム(M. urealyticum));マイコバクテリウム属(例えば、マイコバクテリウム・ツベルクロシス(Mycobacterium tuberculosis)、マイコバクテリウム・アビウム(Mycobacterium avium)、マイコバクテリウム・フォルツイタム(Mycobacterium fortuitum)、マイコバクテリウム・マリナム(Mycobacterium marinum)、マイコバクテリウム・カンサシ(Mycobacterium kansasii)、マイコバクテリウム・シェロナエ(Mycobacterium chelonae)、マイコバクテリウム・アブセサス(Mycobacterium abscessus)、マイコバクテリウム・レプラエ(Mycobacterium leprae)、マイコバクテリウム・スメグミティス(Mycobacterium smegmitis)、マイコバクテリウム・アフリカナム(Mycobacterium africanum)、マイコバクテリウム・アルベイ(Mycobacterium alvei)、マイコバクテリウム・アジアチカム(Mycobacterium asiaticum)、マイコバクテリウム・オーラム(Mycobacterium aurum)、マイコバクテリウム・ボヘミカム(Mycobacterium bohemicum)、マイコバクテリウム・ボビス(Mycobacterium bovis)、マイコバクテリウム・ブランデリ(Mycobacterium branderi)、マイコバクテリウム・ブルマエ(Mycobacterium brumae)、マイコバクテリウム・セラタム(Mycobacterium celatum)、マイコバクテリウム・チュベンセ(Mycobacterium chubense)、マイコバクテリウム・コンフルエンティス(Mycobacterium confluentis)、マイコバクテリウム・コンスピカム(Mycobacterium conspicuum)、マイコバクテリウム・クッキ(Mycobacterium cookii)、マイコバクテリウム・フラベセンス(Mycobacterium flavescens)、マイコバクテリウム・ガディウム(Mycobacterium gadium)、マイコバクテリウム・ガストリ(Mycobacterium gastri)、マイコバクテリウム・ゲナベンス(Mycobacterium genavense)、マイコバクテリウム・ゴルドナ(Mycobacterium gordonae)、マイコバクテリウム・ゴージ(Mycobacterium goodii)、マイコバクテリウム・ヘモフィルム(Mycobacterium haemophilum)、マイコバクテリウム・ハシカム(Mycobacterium hassicum)、マイコバクテリウム・イントラセルラレ(Mycobacterium intracellulare)、マイコバクテリウム・インタージェクタム(Mycobacterium interjectum)、マイコバクテリウム・ヘイデルベレンス(Mycobacterium heidelberense)、マイコバクテリウム・レンチフラバム(Mycobacterium lentiflavum)、マイコバクテリウム・マルモエンス(Mycobacterium malmoense)、マイコバクテリウム・ミクロゲニカム(Mycobacterium microgenicum)、マイコバクテリウム・ミクロチ(Mycobacterium microti)、マイコバクテリウム・ムコゲニカム(Mycobacterium mucogenicum)、マイコバクテリウム・ネオオーラム(Mycobacterium neoaurum)、マイコバクテリウム・ノンクロモゲニカム(Mycobacterium nonchromogenicum)、マイコバクテリウム・ペレグリナム(Mycobacterium peregrinum)、マイコバクテリウム・フレイ(Mycobacterium phlei)、マイコバクテリウム・スクロフラセウム(Mycobacterium scrofulaceum)、マイコバクテリウム・シモイデイ(Mycobacterium shimoidei)、マイコバクテリウム・シミアエ(Mycobacterium simiae)、マイコバクテリウム・スズルガイ(Mycobacterium szulgai)、マイコバクテリウム・テラエ(Mycobacterium terrae)、マイコバクテリウム・サーモレジスタビル(Mycobacterium thermoresistabile)、マイコバクテリウム・トリプレックス(Mycobacterium triplex)、マイコバクテ
リウム・トリビアレ(Mycobacterium triviale)、マイコバクテリウム・ツシアエ(Mycobacterium tusciae)、マイコバクテリウム・ウルセランス(Mycobacterium ulcerans)、マイコバクテリウム・バッカエ(Mycobacterium vaccae)、マイコバクテリウム・ウォリンスキ(Mycobacterium wolinskyi)及びマイコバクテリウム・キセノピ(Mycobacterium xenopi));ヘモフィルス属(例えば、ヘモフィルス・インフルエンザ(Haemophilus influenzae)、ヘモフィルス・デュクレイ(Haemophilus ducreyi)、ヘモフィルス・エジプチウス(Haemophilus aegyptius)、ヘモフィルス・パラインフルエンザ(Haemophilus parainfluenzae)、ヘモフィルス・ヘモリティカス(Haemophilus haemolyticus)及びヘモフィルス・パラヘモリティカス(Haemophilus parahaemolyticus));アクチノバチルス属(例えば、アクチノバチルス・アクチノミセテムコミタンス(Actinobacillus actinomycetemcomitans)、アクチノバチルス・エクリ(Actinobacillus equuli)、アクチノバチルス・ホミニス(Actinobacillus hominis)、アクチノバチルス・リグニエレシ(Actinobacillus lignieresii)、アクチノバチルス・スイス(Actinobacillus suis)及びアクチノバチルス・ウレア(Actinobacillus ureae));アクチノミセス属(例えば、アクチノミセス・イスラエリ(Actinomyces israelii));ブルセラ菌(例えば、ブルセラ・アボルタス(Brucella abortus)、ブルセラ・カニス(Brucella canis)、ブルセラ・メリンテンシス(Brucella melintensis)及びブルセラ・スイス(Brucella suis));カンピロバクター属(例えば、カンピロバクター・ジェジュニ(Campylobacter jejuni)、カンピロバクター・コリ(Campylobacter coli)、カンピロバクター・ラリ(Campylobacter lari)及びカンピロバクター・フェタス(Campylobacter fetus));リステリア・モノサイトジェネス(Listeria monocytogenes);ビブリオ属(例えば、ビブリオ・コレラ(Vibrio cholerae)及びビブリオ・パラヘモリティカス(Vibrio parahaemolyticus)、ビブリオ・アルギノリティカス(Vibrio alginolyticus)、ビブリオ・カルチャリア(Vibrio carchariae)、ビブリオ・フルビアリス(Vibrio fluvialis)、ビブリオ・フルニシ(Vibrio furnissii)、ビブリオ・ホリサエ(Vibrio hollisae)、ビブリオ・メトシュニコビ(Vibrio metschnikovii)、ビブリオ・ミミカス(Vibrio mimicus)及びビブリオ・バルニフィカス(Vibrio vulnificus));エリシペロトリックス・ルゾパシア(Erysipelothrix rhusopathiae);コリネバクテリウム属(例えば、コリネバクテリウム・ジフテリア(Corynebacterium diphtheriae)、コリネバクテリウム・ジェイケウム(Corynebacterium jeikeum)及びコリネバクテリウム・ウレアリティカム(Corynebacterium urealyticum));スピロヘータ科、例えば、ボレリア属(例えば、ボレリア・レクレンティス(Borrelia recurrentis)、ボレリア・ブルグドルフェリ(Borrelia burgdorferi)、ボレリア・アフゼリ(Borrelia afzelii)、ボレリア・アンダーソニ(Borrelia andersonii)、ボレリア・ビセッティ(Borrelia bissettii)、ボレリア・ガリニ(Borrelia garinii)、ボレリア・ジャポニカ(Borrelia japonica)、ボレリア・ルシタニエ(Borrelia lusitaniae)、ボレリア・タヌキ(Borrelia tanukii)、ボレリア・タルジ(Borrelia turdi)、ボレリア・バライシアナ(Borrelia valaisiana)、ボレリア・カウカシカ(Borrelia caucasica)、ボレリア・クロシデュラエ(Borrelia crocidurae)、ボレリア・デュトニ(Borrelia duttoni)、ボレリア・グラインゲリ(Borrelia graingeri)、ボレリア・ヘルムシ(Borrelia hermsii)、ボレリア・ヒスパニカ(Borrelia hispanica)、ボレリア・ラチシェウィ(Borrelia latyschewii)、ボレリア・マゾッティ(Borrelia mazzottii)、ボレリア・パルケリ(Borrelia parkeri)、ボレリア・ペルシカ(Borrelia persica)、ボレリア・ツリカタエ(Borrelia turicatae)及びボレリア・ベネズエレンシス(Borrelia venezuelensis))並びにトレポネマ属(トレポネマ・パリダム種パリダム(Treponema pallidum ssp. pallidum)、トレポネマ・パリダム種エンデミカム(Treponema pallidum ssp. endemicum)、トレポネマ・パリダム種ペルテヌ(Treponema pallidum ssp. pertenue)及びトリポネマ・カラテウム(Treponema carateum));パスツレラ属(例えば、パスツレラ・アエロジェネス(Pasteurella aerogenes)、パスツレラ・ベチアエ(Pasteurella bettyae)、パスツレラ・カニス(Pasteurella canis)、パスツレラ・ダグマティス(Pasteurella dagmatis)、パスツレラ・ガリナルム(Pasteurella gallinarum)、パスツレラ・ヘモリティカ(Pasteurella haemolytica)、パスツレラ・マルトシダ・マルトシダ(Pasteurella multocida multocida)、パスツレラ・マルトシダ・ガリシダ(Pasteurella multocida gallicida)、パスツレラ・マルトシダ・セプティカ(Pasteurella multocida septica)、パスツレラ・ニューモトロピカ(Pasteurella pneumotropica)及びパスツレラ・ストマティス(Pasteurella stomatis));ボルデテラ属(例えば、ボルデテラ・ブロンキセプティカ(Bordetella bronchiseptica)、ボルデテラ・ヒンジ(Bordetella hinzii)、ボルデテラ・ホルムセイ(Bordetella holmseii)、ボルデテラ・パラペルツシス(Bordetella parapertussis)、ボルデテラ・ペルツシス(Bordetella pertussis)及びボルデテラ・トレマタム(Bordetella trematum));ノカルジア科、例えば、ノカルジア属(例えば、ノカルジア・アステロイデス(Nocardia asteroides)及びノカルジア・ブラジリエンシス(Nocardia brasiliensis));リケッチア属(例えば、リクセトシ(Ricksettsii)若しくはコキシエラ・ブルネチ(Coxiella burnetii));レジオネラ属(例えば、レジオネラ・アニサ(Legionalla anisa)、レジオネラ・ビルミンガメンシス(Legionalla birminghamensis)、レジオネラ・ボゼマニ(Legionalla bozemanii)、レジオネラ・シンシナチエンシス(Legionalla cincinnatiensis)、レジオネラ・デュモフィ(Legionalla dumoffii)、レジオネラ・フィーレイ(Legionalla feeleii)、レジオネラ・ゴルマニ(Legionalla gormanii)、レジオネラ・ハケリア(Legionalla hackeliae)、レジオネラ・イスラエレンシス(Legionalla israelensis)、レジオネラ・ジョルダニス(Legionalla jordanis)、レジオネラ・ランシンジェンシス(Legionalla lansingensis)、レジオネラ・ロングビーチェ(Legionalla longbeachae)、レジオネラ・マセアチェルニ(Legionalla maceachernii)、レジオネラ・ミクダデイ(Legionalla micdadei)、レジオネラ・オークリッジェンシス(Legionalla oakridgensis)、レジオネラ・ニューモフィラ(Legionalla pneumophila)、レジオネラ・サインテレンシ(Legionalla sainthelensi)、レジオネラ・タクソネンシス(Legionalla tucsonensis)及びレジオネラ・ワドワーシ(Legionalla wadsworthii));モラクセラ・カタラリス(Moraxella catarrhalis);シクロスポラ・カイエタネンシス(Cyclospora cayetanensis);赤痢アメーバ(Entamoeba histolytica);ジアルジア・ランブリア(Giardia lamblia);膣トリコモナス(Trichomonas vaginalis);トキソプラズマ原虫(Toxoplasma gondii);ステノトロフォモナス・マルトフィリア(Stenotrophomonas maltophilia);ブルクホルデリア・セパシア(Burkholderia cepacia);ブルクホルデリア・マレイ(Burkholderia mallei)及びブルクホルデリア・シュードマレイ(Burkholderia pseudomallei);フランシセラ・ツラレンシス(Francisella tularensis);カルドネレラ属(例えば、ガルドネレラ・バギナリス(Gardneralla vaginalis)及びガルドネレラ・モビルンカス(Gardneralla mobiluncus));
ストレプトバチルス・モニリフォルミス(Streptobacillus moniliformis);フラボバクテリア科、例えば、カプノサイトファガ属(例えば、カプノサイトファガ・カニモルサス(Capnocytophaga canimorsus)、カプノサイトファガ・シノデグミ(Capnocytophaga cynodegmi)、カプノサイトファガ・ギンギバリス(Capnocytophaga gingivalis)、カプノサイトファガ・グラヌロサ(Capnocytophaga granulosa)、カプノサイトファガ・ヘモリティカ(Capnocytophaga haemolytica)、カプノサイトファガ・オクラセア(Capnocytophaga ochracea)及びカプノサイトファガ・スプチゲナ(Capnocytophaga sputigena));バルトネラ属(バルトネラ・バシリフォルミス(Bartonella bacilliformis)、バルトネラ・クラリッジア(Bartonella clarridgeiae)、バルトネラ・エリザベータ(Bartonella elizabethae)、バルトネラ・ヘンセラ(Bartonella henselae)、バルトネラ・キンタナ(Bartonella quintana)及びバルトネラ・ビンソニ・アルペンシス(Bartonella vinsonii arupensis));レプトスピラ属(例えば、レプトスピラ・ビフレキサ(Leptospira biflexa)、レプトスピラ・ボルグペテルセニ(Leptospira borgpetersenii)、レプトスピラ・イナダイ(Leptospira inadai)、レプトスピラ・インテロガンス(Leptospira interrogans)、レプトスピラ・キルシュネリ(Leptospira kirschneri)、レプトスピラ・ノグチ(Leptospira noguchii)、レプトスピラ・サンタロサイ(Leptospira santarosai)及びレプトスピラ・ウェイリ(Leptospira weilii));スピリリウム(例えば、スピリリウム・ミヌス(Spirillum minus));バクテロイデス属(例えば、バクテロイデス・カッカエ(Bacteroides caccae)、バクテロイデス・カピロサス(Bacteroides capillosus)、バクテロイデス・コアグランス(Bacteroides coagulans)、バクテロイデス・ジスタソニス(Bacteroides distasonis)、バクテロイデス・エゲルチ(Bacteroides eggerthii)、バクテロイデス・フォルシタス(Bacteroides forsythus)、バクテロイデス・フラギリス(Bacteroides fragilis)、バクテロイデス・メルダエ(Bacteroides merdae)、バクテロイデス・オバタス(Bacteroides ovatus)、バクテロイデス・プトレジニス(Bacteroides putredinis)、バクテロイデス・ピオジェネス(Bacteroides pyogenes)、バクテロイデス・スプランチニカス(Bacteroides splanchinicus)、バクテロイデス・ステルコリス(Bacteroides stercoris)、バクテロイデス・テクタス(Bacteroides tectus)、バクテロイデス・テタイオタオミクロン(Bacteroides thetaiotaomicron)、バクテロイデス・ユニフォルミス(Bacteroides uniformis)、バクテロイデス・ウレオリティカス(Bacteroides ureolyticus)及びバクテロイデス・バルガタス(Bacteroides vulgatus));プレボテラ属(例えば、プレボテラ・ビビア(Prevotella bivia)、プレボテラ・ブッカエ(Prevotella buccae)、プレボテラ・コルポリス(Prevotella corporis)、プレボテラ・デンタリス(Prevotella dentalis)(ミツオケラ・デンタリス(Mitsuokella dentalis))、プレボテラ・デンチコラ(Prevotella denticola)、プレボテラ・ディシエンス(Prevotella disiens)、プレボテラ・エノエカ(Prevotella enoeca)、プレボテラ・ヘパリノリティカ(Prevotella heparinolytica)、プレボテラ・インターメディア(Prevotella intermedia)、プレボテラ・ロエシ(Prevotella loeschii)、プレボテラ・メラニノゲニカ(Prevotella melaninogenica)、プレボテラ・ニグレセンス(Prevotella nigrescens)、プレボテラ・オラリス(Prevotella oralis)、プレボテラ・オリス(Prevotella oris)、プレボテラ・オーロラ(Prevotella oulora)、プレボテラ・タネラエ(Prevotella tannerae)、プレボテラ・ベノラリス(Prevotella venoralis)及びプレボテラ・ズーグレオフォルミス(Prevotella zoogleoformans));ポルフィロモナス属(例えば、ポルフィロモナス・アサカロリティカ(Porphyromonas asaccharolytica)、ポルフィロモナス・カンギンギバリス(Porphyromonas cangingivalis)、ポルフィロモナス・カノリス(Porphyromonas canoris)、ポルフィロモナス・カンサルシ(Porphyromonas cansulci)、ポルフィロモナス・カトニエ(Porphyromonas catoniae)、ポルフィロモナス・サーカムデンタリア(Porphyromonas circumdentaria)、ポルフィロモナス・クレビオリカニス(Porphyromonas crevioricanis)、ポルフィロモナス・エンドドンタリス(Porphyromonas endodontalis)、ポルフィロモナス・ギンギバリス(Porphyromonas gingivalis)、ポルフィロモナス・ギンギビカニス(Porphyromonas gingivicanis)、ポルフィロモナス・レビ(Porphyromonas levii)及びポルフィロモナス・マカカエ(Porphyromonas macacae));フソバクテリウム属(例えば、フソバクテリウム・ゴナディアフォルマンス(F. gonadiaformans)、フソバクテリウム・モルチフェラム(F. mortiferum)、フソバクテリウム・ナビフォルム(F. naviforme)、フソバクテリウム・ネクロジェネス(F. necrogenes)、フソバクテリウム・ネクロフォラム・ネクロフォラム(F. necrophorum necrophorum)、フソバクテリウム・ネクロフォラム・ファンジリフォルム(F. necrophorum fundiliforme)、フソバクテリウム・ヌクレアタム・ヌクレアタム(F. nucleatum nucleatum)、フソバクテリウム・ヌクレアタム・フシフォルム(F. nucleatum fusiforme)、フソバクテリウム・ヌクレアタム・ポリモルファム(F. nucleatum polymorphum)、フソバクテリウム・ヌクレアタム・ビンセンチ(F. nucleatum vincentii)、フソバクテリウム・ペリオドンチカム(F. periodonticum)、フソバクテリウム・ルシ(F. russii)、フソバクテリウム・ウルセランス(F. ulcerans)及びフソバクテリウム・バリウム(F. varium));クラミジア属(例えば、クラミジア・トラコマティス(Chlamydia trachomatis));クリプトスポリジウム属(例えば、クリプトスポリジウム・パルバム(C. parvum)、クリプトスポリジウム・ホミニス(C. hominis)、クリプトスポリジウム・カニス(C. canis)、クリプトスポリジウム・フェリス(C. felis)、クリプトスポリジウム・メレアグリディス(C. meleagridis)及びクリプトスポリジウム・ムリス(C. muris));クラミドフィラ属(例えば、クラミドフィラ・アボルタス(Chlamydophila abortus)(クラミジア・プシタシ(Chlamydia psittaci))、クラミドフィラ・ニューモニエ(Chlamydophila pneumoniae)、(クラミジア・ニューモニエ(Chlamydia pneumoniae))及びクラミドフィラ・プシタシ(Chlamydophila psittaci)(クラミジア・プシタシ(Chlamydia psittaci)));ロイコノストク属(例えば、ロイコノストク・シトレウム(Leuconostoc citreum)、ロイコノストク・クレモリス(Leuconostoc cremoris)、ロイコノストク・デキストラニカム(Leuconostoc dextranicum)、ロイコノストク・ラクティス(Leuconostoc lactis)、ロイコノストク・メセンテロイデス(Leuconostoc mesenteroides)及びロイコノストク・シュードメセンテロイデス(Leuconostoc pseudomesenteroides));ゲメラ属(例えば、ゲメラ・ベルゲリ(Gemella bergeri)、ゲメラ・ヘモリサンス(Gemella haemolysans)、ゲメラ・モルビロラム(Gemella morbillorum)及びゲメラ・サンギニス(Gemella sanguinis));並びにウレアプラズマ属(例えば、ウレアプラズマ・パルバム(Ureaplasma parvum)及びウレアプラズマ・ウレアリティカム(Ureaplasma urealyticum))。
腸内細菌、例えば大腸菌(Escherichia coli)、クレブシエラ菌(例えば、クレブシエラ・ニューモニエ(Klebs. pneumoniae)及びクレブシエラ・オキシトカ(Klebs. oxytoca))並びにプロテウス属(Proteus)(例えば、プロテウス・ミラビリス(Pr. mirabilis)、プロテウス・レトゲリ(Pr. rettgeri)及びプロテウス・バルガリス(Pr. vulgaris));インフルエンザ菌(Haemophilis influenzae);マイコバクテリウム属、例えばマイコバクテリウム・ツベルクロシス(Mycobacterium tuberculosis);及びエンテロバクター属(例えば、エンテロバクター・クロアカ(Enterobacter cloacae))などがある。好ましくは、その細菌は、腸内細菌、例えば大腸菌(Escherichia coli)及びクレブシエラ菌(例えば、クレブシエラ・ニューモニエ(Klebs. pneumoniae)及びクレブシエラ・オキシトカ(Klebs. oxytoca))である。特に好ましいものは、大腸菌(Escherichia coli)及びクレブシエラ・ニューモニエ(Klebs. pneumoniae)(例えば、クレブシエラ・ニューモニエ亜種ニューモニエ(Klebs. pneumoniae subsp. pneumoniae))である。
https://www.medicines.org.uk/emc/product/5749/smpc;
https://www.medicines.org.uk/emc/product/429/smpc;
https://www.medicines.org.uk/emc/product/3602/smpc;
https://www.medicines.org.uk/emc/product/428/smpc;
https://www.medicines.org.uk/emc/product/3601/smpc;
https://www.medicines.org.uk/emc/product/437/smpc;及び
https://www.medicines.org.uk/emc/product/7818/smpc
から入手できる。
https://www.medicines.org.uk/emc/product/4982/smpc;及び
https://www.medicines.org.uk/emc/product/3799/smpc
から入手できる。
https://www.medicines.org.uk/emc/product/5439/smpc;
https://www.medicines.org.uk/emc/product/7219/smpc;及び
https://www.medicines.org.uk/emc/product/7329/smpc
から入手できる。
https://www.medicines.org.uk/emc/product/3998/smpc;
https://www.medicines.org.uk/emc/product/3990/smpc;
https://www.medicines.org.uk/emc/product/5960/smpc;
https://www.medicines.org.uk/emc/product/5960/smpc;
https://www.medicines.org.uk/emc/product/3996/smpc;及び
https://www.medicines.org.uk/emc/product/3997/smpc
から入手できる。
有効成分の生物学的活性(例えば、殺菌活性又は抗微生物活性)を求めるのに用いることができる試験手順としては、
(a)臨床的に潜伏性の細菌に対する殺菌活性;及び
(b)対数期細菌に対する抗微生物活性
を測定する上での当業者に公知のものなどがある。
(1)細菌培養物を静止期まで増殖させる段階;
(2)静止(stationery)期培養物を、増殖細菌を死滅させるのに十分な濃度及び/又は時間で1以上の抗微生物剤で処理することで、表現型的に耐性の下位個体群を選択する段階;
(3)表現型的に耐性の下位個体群のサンプルを1以上の試験化合物又は薬剤とともにインキュベートする段階;及び
(4)表現型的に耐性の下位個体群に対する抗微生物効果を評価する段階
を含むことができる。
実施例1で使用したチェッカーボード法は、Antimicrob Chemo (2013)68, 374-384に詳細に記載されたプロトコールに従った。ジドブジン及びニトロフラントインは、市販の入手先から得た。使用した細菌は、大腸菌(E. coli)k12であり、この大腸菌(E. coli)k12は、グラム陰性菌に対する全ての抗生物質に対して感受性であると思われる感受性株である。この株は、市販の入手先から得たもので、その細菌の対数期増殖を、当技術分野で公知の方法を用いて実施した。
(薬剤AのMIC、組み合わせで試験)/(薬剤AのMIC、単独で試験)+(薬剤BのMIC、組み合わせで試験)/(薬剤BのMIC、単独で試験)
方法及び細菌株は実施例1と同一であった。ジドブジン及びファロペネムは、市販の入手先から得た。本発明の組み合わせの効果を、実施例1と同じ方法で、単独及び組み合わせでの各薬剤についてのMICを計算することで調べた。
方法及び細菌株は実施例1と同一であった。ジドブジン及びメシリナムは、市販の入手先から得た。本発明の組み合わせの効果を、実施例1と同じ方法で、単独及び組み合わせでの各薬剤についてのMICを計算することで調べた。
方法及び細菌株は実施例1と同一であった。ジドブジン及びセファレキシンは、市販の入手先から得た。本発明の組み合わせの効果を、実施例1と同じ方法で、単独及び組み合わせでの各薬剤についてのMICを計算することで調べた。
方法及び細菌株は実施例1と同一であった。ジドブジン及びホスホマイシンは、市販の入手先から得た。本発明の組み合わせの効果を、実施例1と同じ方法で、単独及び組み合わせでの各薬剤についてのMICを計算することで調べた。
Claims (11)
- ジドブジン又はその薬学的に許容される塩及び/又は溶媒和物と、ニトロフラントイン又はその薬学的に許容される塩及び/又は溶媒和物である抗微生物化合物とを含む組み合わせを含むグラム陰性細菌感染の治療薬。
- 前記感染に関連する増殖性微生物を死滅させるための、請求項1に記載の治療薬。
- 前記感染が尿路感染である、請求項1又は2に記載の治療薬。
- 前記細菌感染が大腸菌(E. coli)によって引き起こされる、請求項1~3のいずれか1項に記載の治療薬。
- 前記感染が、前記細菌の薬剤耐性株によって引き起こされる、請求項1~4のいずれか1項に記載の治療薬。
- グラム陰性細菌感染治療のための医薬品の製造における、ニトロフラントイン又はその薬学的に許容される塩及び/又は溶媒和物である抗微生物化合物と組み合わせた、ジドブジン又はその薬学的に許容される塩及び/又は溶媒和物の使用。
- グラム陰性細菌感染治療のための医薬品の製造における、ジドブジン又はその薬学的に許容される塩及び/又は溶媒和物と組み合わせた、ニトロフラントイン又はその薬学的に許容される塩及び/又は溶媒和物である抗微生物化合物の使用。
- 前記細菌感染が大腸菌(E. coli)によって引き起こされる、請求項6又は7に記載の使用。
- 前記感染が、前記細菌の薬剤耐性株によって引き起こされる、請求項6~8のいずれか1項に記載の使用。
- ジドブジン又はその薬学的に許容される塩及び/又は溶媒和物とニトロフラントイン又はその薬学的に許容される塩及び/又は溶媒和物である抗微生物化合物との組み合わせ、及び薬学的に許容される補助剤、希釈剤又は担体を含む、グラム陰性細菌感染の治療のために用いられる医薬組成物。
- グラム陰性細菌感染の治療における同時、別個又は順次使用のための組み合わせ薬剤としての、ジドブジン又はその薬学的に許容される塩及び/又は溶媒和物と、ニトロフラントイン又はその薬学的に許容される塩及び/又は溶媒和物である抗微生物化合物とを含む製品。
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JP2016515542A (ja) | 2013-03-22 | 2016-05-30 | ヘルパービー セラピューティクス リミテッドHelperby Therapeutics Limited | ジドブジンおよびポリミキシンを含む組み合わせ |
JP2017504647A (ja) | 2014-01-30 | 2017-02-09 | ヘルパービー セラピューティクス リミテッドHelperby Therapeutics Limited | 微生物感染の治療のためのジドブジン組み合わせ療法 |
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