JP2017506238A - Mtan阻害剤を使用するピロリ菌(h.pylori)感染の治療 - Google Patents
Mtan阻害剤を使用するピロリ菌(h.pylori)感染の治療 Download PDFInfo
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- JP2017506238A JP2017506238A JP2016552328A JP2016552328A JP2017506238A JP 2017506238 A JP2017506238 A JP 2017506238A JP 2016552328 A JP2016552328 A JP 2016552328A JP 2016552328 A JP2016552328 A JP 2016552328A JP 2017506238 A JP2017506238 A JP 2017506238A
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- VKYKSIONXSXAKP-UHFFFAOYSA-N hexamethylenetetramine Chemical compound C1N(C2)CN3CN1CN2C3 VKYKSIONXSXAKP-UHFFFAOYSA-N 0.000 description 1
- FUZZWVXGSFPDMH-UHFFFAOYSA-N hexanoic acid Chemical compound CCCCCC(O)=O FUZZWVXGSFPDMH-UHFFFAOYSA-N 0.000 description 1
- PWDFZWZPWFYFTC-UHFFFAOYSA-M hexyl(triphenyl)phosphanium;bromide Chemical compound [Br-].C=1C=CC=CC=1[P+](C=1C=CC=CC=1)(CCCCCC)C1=CC=CC=C1 PWDFZWZPWFYFTC-UHFFFAOYSA-M 0.000 description 1
- 238000004128 high performance liquid chromatography Methods 0.000 description 1
- XMBWDFGMSWQBCA-UHFFFAOYSA-N hydrogen iodide Chemical compound I XMBWDFGMSWQBCA-UHFFFAOYSA-N 0.000 description 1
- ZMZDMBWJUHKJPS-UHFFFAOYSA-N hydrogen thiocyanate Natural products SC#N ZMZDMBWJUHKJPS-UHFFFAOYSA-N 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-M hydrogensulfate Chemical compound OS([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-M 0.000 description 1
- 230000007062 hydrolysis Effects 0.000 description 1
- 238000006460 hydrolysis reaction Methods 0.000 description 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 description 1
- 125000003037 imidazol-2-yl group Chemical group [H]N1C([*])=NC([H])=C1[H] 0.000 description 1
- 125000002140 imidazol-4-yl group Chemical group [H]N1C([H])=NC([*])=C1[H] 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 150000002500 ions Chemical class 0.000 description 1
- 230000007794 irritation Effects 0.000 description 1
- SUMDYPCJJOFFON-UHFFFAOYSA-N isethionic acid Chemical class OCCS(O)(=O)=O SUMDYPCJJOFFON-UHFFFAOYSA-N 0.000 description 1
- BPHPUYQFMNQIOC-NXRLNHOXSA-N isopropyl beta-D-thiogalactopyranoside Chemical compound CC(C)S[C@@H]1O[C@H](CO)[C@H](O)[C@H](O)[C@H]1O BPHPUYQFMNQIOC-NXRLNHOXSA-N 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
- 238000001819 mass spectrum Methods 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 239000002207 metabolite Substances 0.000 description 1
- QARBMVPHQWIHKH-UHFFFAOYSA-N methanesulfonyl chloride Chemical compound CS(Cl)(=O)=O QARBMVPHQWIHKH-UHFFFAOYSA-N 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 239000004530 micro-emulsion Substances 0.000 description 1
- 150000007522 mineralic acids Chemical class 0.000 description 1
- 238000012544 monitoring process Methods 0.000 description 1
- KVBGVZZKJNLNJU-UHFFFAOYSA-M naphthalene-2-sulfonate Chemical compound C1=CC=CC2=CC(S(=O)(=O)[O-])=CC=C21 KVBGVZZKJNLNJU-UHFFFAOYSA-M 0.000 description 1
- 235000001968 nicotinic acid Nutrition 0.000 description 1
- 239000011664 nicotinic acid Substances 0.000 description 1
- FEMOMIGRRWSMCU-UHFFFAOYSA-N ninhydrin Chemical compound C1=CC=C2C(=O)C(O)(O)C(=O)C2=C1 FEMOMIGRRWSMCU-UHFFFAOYSA-N 0.000 description 1
- 125000004433 nitrogen atom Chemical group N* 0.000 description 1
- 231100000252 nontoxic Toxicity 0.000 description 1
- 230000003000 nontoxic effect Effects 0.000 description 1
- 239000002777 nucleoside Substances 0.000 description 1
- IOQPZZOEVPZRBK-UHFFFAOYSA-N octan-1-amine Chemical compound CCCCCCCCN IOQPZZOEVPZRBK-UHFFFAOYSA-N 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- 150000002894 organic compounds Chemical class 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 125000004430 oxygen atom Chemical group O* 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 239000008188 pellet Substances 0.000 description 1
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 description 1
- JRKICGRDRMAZLK-UHFFFAOYSA-L peroxydisulfate Chemical compound [O-]S(=O)(=O)OOS([O-])(=O)=O JRKICGRDRMAZLK-UHFFFAOYSA-L 0.000 description 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- 150000004714 phosphonium salts Chemical class 0.000 description 1
- 229940075930 picrate Drugs 0.000 description 1
- OXNIZHLAWKMVMX-UHFFFAOYSA-M picrate anion Chemical compound [O-]C1=C([N+]([O-])=O)C=C([N+]([O-])=O)C=C1[N+]([O-])=O OXNIZHLAWKMVMX-UHFFFAOYSA-M 0.000 description 1
- IUGYQRQAERSCNH-UHFFFAOYSA-M pivalate Chemical compound CC(C)(C)C([O-])=O IUGYQRQAERSCNH-UHFFFAOYSA-M 0.000 description 1
- 229950010765 pivalate Drugs 0.000 description 1
- 239000013612 plasmid Substances 0.000 description 1
- 229920000768 polyamine Polymers 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 229920001592 potato starch Polymers 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 238000000425 proton nuclear magnetic resonance spectrum Methods 0.000 description 1
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 description 1
- 238000009877 rendering Methods 0.000 description 1
- 230000029058 respiratory gaseous exchange Effects 0.000 description 1
- YGSDEFSMJLZEOE-UHFFFAOYSA-M salicylate Chemical compound OC1=CC=CC=C1C([O-])=O YGSDEFSMJLZEOE-UHFFFAOYSA-M 0.000 description 1
- 229960001860 salicylate Drugs 0.000 description 1
- 238000005070 sampling Methods 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- AWUCVROLDVIAJX-GSVOUGTGSA-N sn-glycerol 3-phosphate Chemical compound OC[C@@H](O)COP(O)(O)=O AWUCVROLDVIAJX-GSVOUGTGSA-N 0.000 description 1
- 238000002415 sodium dodecyl sulfate polyacrylamide gel electrophoresis Methods 0.000 description 1
- 238000000527 sonication Methods 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 239000011593 sulfur Substances 0.000 description 1
- 125000004434 sulfur atom Chemical group 0.000 description 1
- 230000002459 sustained effect Effects 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 238000004885 tandem mass spectrometry Methods 0.000 description 1
- 230000008685 targeting Effects 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- MONIBTBJQQSCJO-LLVKDONJSA-N tert-butyl (4R)-2,2-dimethyl-4-(pyrazin-2-ylsulfanylmethyl)-1,3-oxazolidine-3-carboxylate Chemical compound CC(C)(C)OC(=O)N1[C@@H](CSC2=CN=CC=N2)COC1(C)C MONIBTBJQQSCJO-LLVKDONJSA-N 0.000 description 1
- MIQSZAFNKLLXIQ-OAHLLOKOSA-N tert-butyl (4R)-4-(benzylsulfanylmethyl)-2,2-dimethyl-1,3-oxazolidine-3-carboxylate Chemical compound CC(C)(C)OC(=O)N1[C@@H](CSCC2=CC=CC=C2)COC1(C)C MIQSZAFNKLLXIQ-OAHLLOKOSA-N 0.000 description 1
- ZNWCQLZLAULYCP-GFCCVEGCSA-N tert-butyl (4R)-4-(butylsulfanylmethyl)-2,2-dimethyl-1,3-oxazolidine-3-carboxylate Chemical compound C(CCC)SC[C@@H]1N(C(OC1)(C)C)C(=O)OC(C)(C)C ZNWCQLZLAULYCP-GFCCVEGCSA-N 0.000 description 1
- YUWRXSYKKBAGSK-OAHLLOKOSA-N tert-butyl (4R)-4-(heptylsulfanylmethyl)-2,2-dimethyl-1,3-oxazolidine-3-carboxylate Chemical compound C(CCCCCC)SC[C@@H]1N(C(OC1)(C)C)C(=O)OC(C)(C)C YUWRXSYKKBAGSK-OAHLLOKOSA-N 0.000 description 1
- RTHZHNTVIYRRAY-CYBMUJFWSA-N tert-butyl (4R)-4-[(4-chlorophenyl)sulfanylmethyl]-2,2-dimethyl-1,3-oxazolidine-3-carboxylate Chemical compound CC(C)(C)OC(=O)N1[C@@H](CSC2=CC=C(Cl)C=C2)COC1(C)C RTHZHNTVIYRRAY-CYBMUJFWSA-N 0.000 description 1
- UGBHYNVXSSREBY-INIZCTEOSA-N tert-butyl (4S)-2,2-dimethyl-4-nonyl-1,3-oxazolidine-3-carboxylate Chemical compound CC1(OC[C@@H](N1C(=O)OC(C)(C)C)CCCCCCCCC)C UGBHYNVXSSREBY-INIZCTEOSA-N 0.000 description 1
- AIAPXCOBLDBIAG-LBPRGKRZSA-N tert-butyl (4S)-2,2-dimethyl-4-pentyl-1,3-oxazolidine-3-carboxylate Chemical compound CCCCC[C@H]1COC(C)(C)N1C(=O)OC(C)(C)C AIAPXCOBLDBIAG-LBPRGKRZSA-N 0.000 description 1
- GXZAPBSEZLVPRL-ZDUSSCGKSA-N tert-butyl (4S)-4-hexyl-2,2-dimethyl-1,3-oxazolidine-3-carboxylate Chemical compound C(CCCCC)[C@@H]1N(C(OC1)(C)C)C(=O)OC(C)(C)C GXZAPBSEZLVPRL-ZDUSSCGKSA-N 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 125000000437 thiazol-2-yl group Chemical group [H]C1=C([H])N=C(*)S1 0.000 description 1
- 125000004495 thiazol-4-yl group Chemical group S1C=NC(=C1)* 0.000 description 1
- 125000004496 thiazol-5-yl group Chemical group S1C=NC=C1* 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- YNJBWRMUSHSURL-UHFFFAOYSA-N trichloroacetic acid Chemical compound OC(=O)C(Cl)(Cl)Cl YNJBWRMUSHSURL-UHFFFAOYSA-N 0.000 description 1
- XMQSELBBYSAURN-UHFFFAOYSA-M triphenyl(propyl)phosphanium;bromide Chemical compound [Br-].C=1C=CC=CC=1[P+](C=1C=CC=CC=1)(CCC)C1=CC=CC=C1 XMQSELBBYSAURN-UHFFFAOYSA-M 0.000 description 1
- JBWKIWSBJXDJDT-UHFFFAOYSA-N triphenylmethyl chloride Chemical compound C=1C=CC=CC=1C(C=1C=CC=CC=1)(Cl)C1=CC=CC=C1 JBWKIWSBJXDJDT-UHFFFAOYSA-N 0.000 description 1
- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 description 1
- ZDPHROOEEOARMN-UHFFFAOYSA-N undecanoic acid Chemical compound CCCCCCCCCCC(O)=O ZDPHROOEEOARMN-UHFFFAOYSA-N 0.000 description 1
- 239000008215 water for injection Substances 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
- 229910052726 zirconium Inorganic materials 0.000 description 1
Images
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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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/90—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
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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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- 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
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- Public Health (AREA)
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- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
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- Pest Control & Pesticides (AREA)
- Agronomy & Crop Science (AREA)
- Engineering & Computer Science (AREA)
- Dentistry (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Description
本出願は、内容が参照により全体として本明細書に組み込まれる2014年2月12日に出願された米国仮特許出願第61/938,755号明細書の利益を主張する。
本発明は、National Institutes of Healthにより授与された助成金番号GM41916のもと、およびNational Institute of Biomedical Imaging and Bioengineering(NIBIB)により授与されたCenter for Synchrotron Biosciences助成金番号P30−EB−009998のもと、政府支援を受けて作製された。政府は、本発明の一定の権利を有する。
である、方法を提供する。
である、方法を提供する。
材料および方法
材料。ピロリ菌(H.pylori)(J99および43504)、肺炎桿菌(K.pneumoniae)、赤痢菌(S.flexneri)、サルモネラ菌(S.enterica)、黄色ブドウ球菌(S.aureus)および緑膿菌(P.aeruginosa)を、American Type Culture Collectionから購入した。脱線維ウマ血液(DHB)を、Hemostat Laboratories(Dixon,CA)から購入した。トリプシンダイズ寒天(TSA)を、Becton Dickinson and Company(Sparks,MD)から購入した。マッコンキー寒天はOxoid LTD(Basingstoke,Hampshire,England)から購入した。キサンチンオキシダーゼおよび5’−メチルチオアデノシンを、Sigma−Aldrich(St Louis,MO)から購入した。残りの材料は入手可能な最高純度で購入した。
ピロリ菌(H.pylori)感染において一般に使用される抗生物質としては、アモキシシリン、メトロニダゾールおよびテトラサイクリンが挙げられる。選択される化合物の抗ピロリ菌(H.pylori)効果を一般に使用されるそれらの抗生物質と比較した。
化合物T.2(ヘキシル−SerMe−イムシリンA)のインビトロ活性
これらの以下の実験は、UNT Health Science Center(研究指揮:William J Weiss,Director of Pre−Clinical Services),Fort Worth,TX,USAにおいて実施した。
以下の実験は、UNT Health Science Center(研究指揮:William J Weiss,Director of Pre−Clinical Services),Fort Worth,TX,USAにおいて実施した。
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Claims (25)
- Rが、Qである、請求項1または2に記載の方法。
- Rが、CH2SQである、請求項1または2に記載の方法。
- Qが、C1〜C9アルキルである、請求項1〜4のいずれか一項に記載の方法。
- Qが、C4〜C7シクロアルキルである、請求項1〜4のいずれか一項に記載の方法。
- Qが、アリールである、請求項1〜4のいずれか一項に記載の方法。
- Qが、ヘテロアリールである、請求項1〜4のいずれか一項に記載の方法。
- Qが、アラルキルである、請求項1〜4のいずれか一項に記載の方法。
- Qが、ハロゲンにより置換されたアリール、ヘテロアリールまたはアラルキルである、請求項1〜4のいずれか一項に記載の方法。
- Rが、QまたはCH2SQであり、Qは、C2〜C9直鎖アルキル、アリール、ヘテロアリール、アラルキル、またはC4〜C7シクロアルキルであり、Qは、1つ以上のハロゲン、OH基および/またはNH2基により任意選択的に置換される、請求項1〜4のいずれか一項に記載の方法。
- 前記ハロゲンが、オルト、メタまたはパラ位において存在する、請求項10または11に記載の方法。
- 前記ハロゲンが、Cl、F、BrまたはIである、請求項1〜12のいずれか一項に記載の方法。
- Qが、C3〜C9直鎖アルキルまたはヘテロアリールである、請求項1〜4のいずれか一項に記載の方法。
- 前記化合物が、ピロリ菌(H.pylori)5’−メチルチオアデノシンヌクレオシダーゼ(MTAN)を阻害するために有効な量で投与される、請求項1〜16のいずれか一項に記載の方法。
- 前記化合物が、ピロリ菌(H.pylori)の増殖を阻害するが、大腸菌(E.coli)、コレラ菌(V.cholerae)、黄色ブドウ球菌(S.aureus)、肺炎桿菌(K.pneumoniae)、赤痢菌(S.flexneri)、サルモネラ菌(S.enterica)および緑膿菌(P.aeruginosa)からなる群から選択される1つ以上の細菌の増殖を阻害しない、請求項1〜17のいずれか一項に記載の方法。
- 前記化合物が、大腸菌(E.coli)、コレラ菌(V.cholerae)、黄色ブドウ球菌(S.aureus)、肺炎桿菌(K.pneumoniae)、赤痢菌(S.flexneri)、サルモネラ菌(S.enterica)および緑膿菌(P.aeruginosa)の全ての増殖を阻害しない、請求項18に記載の方法。
- 前記化合物が、ピロリ菌(H.pylori)の増殖の阻害において、アモキシシリン、メトロニダゾールまたはテトラサイクリンよりも有効である、請求項1〜19のいずれか一項に記載の方法。
- 前記対象が、消化性潰瘍を有する、請求項1〜20のいずれか一項に記載の方法。
- 前記対象が、胃潰瘍または十二指腸潰瘍を有する、請求項1〜21のいずれか一項に記載の方法。
- 前記化合物が経口投与される、請求項1〜23のいずれか一項に記載の方法。
- 請求項24に記載の化合物および薬学的に許容可能な担体を含む医薬組成物。
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PCT/US2015/014778 WO2015123101A1 (en) | 2014-02-12 | 2015-02-06 | Treatment of h. pylori infections using mtan inhibitors |
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US10294233B2 (en) | 2019-05-21 |
AU2015217416A1 (en) | 2016-09-29 |
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