KR102425959B1 - 박테리아 감염의 치료를 위한 크로만 모노박탐 화합물 - Google Patents

박테리아 감염의 치료를 위한 크로만 모노박탐 화합물 Download PDF

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KR102425959B1
KR102425959B1 KR1020207012234A KR20207012234A KR102425959B1 KR 102425959 B1 KR102425959 B1 KR 102425959B1 KR 1020207012234 A KR1020207012234 A KR 1020207012234A KR 20207012234 A KR20207012234 A KR 20207012234A KR 102425959 B1 KR102425959 B1 KR 102425959B1
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alkyl
unsubstituted
substituted
independently
hydrogen
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KR20200058520A (ko
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테스파예 비프투
시안하이 황
웨이구오 리우
웨이동 판
민 박
알렉산더 파스테르나크
완잉 썬
하이펑 탕
이 장
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머크 샤프 앤드 돔 코포레이션
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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
    • A61K31/42—Oxazoles
    • A61K31/424—Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
    • 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/425—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
    • 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
    • A61K31/425—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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4425—Pyridinium derivatives, e.g. pralidoxime, pyridostigmine
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
KR1020207012234A 2017-10-02 2018-09-27 박테리아 감염의 치료를 위한 크로만 모노박탐 화합물 Active KR102425959B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762566779P 2017-10-02 2017-10-02
US62/566,779 2017-10-02
PCT/US2018/053039 WO2019070492A1 (en) 2017-10-02 2018-09-27 CHROMANE MONOBACTAM COMPOUNDS FOR THE TREATMENT OF BACTERIAL INFECTIONS

Publications (2)

Publication Number Publication Date
KR20200058520A KR20200058520A (ko) 2020-05-27
KR102425959B1 true KR102425959B1 (ko) 2022-07-27

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KR1020207012234A Active KR102425959B1 (ko) 2017-10-02 2018-09-27 박테리아 감염의 치료를 위한 크로만 모노박탐 화합물

Country Status (26)

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US (1) US11433055B2 (enExample)
EP (1) EP3691639B1 (enExample)
JP (1) JP7252948B2 (enExample)
KR (1) KR102425959B1 (enExample)
CN (2) CN111201021B (enExample)
AU (1) AU2018345523B2 (enExample)
CA (1) CA3076022C (enExample)
CL (1) CL2020000860A1 (enExample)
CO (1) CO2020004087A2 (enExample)
CR (1) CR20200148A (enExample)
DO (1) DOP2020000058A (enExample)
EA (1) EA202090604A1 (enExample)
ES (1) ES2968467T3 (enExample)
GE (1) GEP20227406B (enExample)
IL (1) IL273306B (enExample)
JO (1) JOP20200130A1 (enExample)
MA (1) MA50629A (enExample)
MX (1) MX2020003581A (enExample)
NI (1) NI202000023A (enExample)
PE (1) PE20201256A1 (enExample)
PH (1) PH12020550107A1 (enExample)
SA (1) SA520411571B1 (enExample)
SG (1) SG11202002575UA (enExample)
UA (1) UA126000C2 (enExample)
WO (1) WO2019070492A1 (enExample)
ZA (1) ZA202001721B (enExample)

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CN110156697B (zh) * 2019-05-30 2022-05-06 常州沃腾化工科技有限公司 一种1,2-二甲基-1,4,5,6-四氢嘧啶的合成方法
US11753413B2 (en) 2020-06-19 2023-09-12 Incyte Corporation Substituted pyrrolo[2,1-f][1,2,4]triazine compounds as JAK2 V617F inhibitors
US11691971B2 (en) 2020-06-19 2023-07-04 Incyte Corporation Naphthyridinone compounds as JAK2 V617F inhibitors
SI4175719T1 (sl) 2020-07-02 2025-07-31 Incyte Corporation Triciklične sečninske spojine kot zaviralci jak2 v617f
US11767323B2 (en) 2020-07-02 2023-09-26 Incyte Corporation Tricyclic pyridone compounds as JAK2 V617F inhibitors
US11661422B2 (en) 2020-08-27 2023-05-30 Incyte Corporation Tricyclic urea compounds as JAK2 V617F inhibitors
US20240051931A1 (en) * 2020-12-03 2024-02-15 University Of Pittsburgh - Of The Commonwealth System Of Higher Education Hdac inhibitors
WO2022140231A1 (en) 2020-12-21 2022-06-30 Incyte Corporation Deazaguaine compounds as jak2 v617f inhibitors
US11958861B2 (en) 2021-02-25 2024-04-16 Incyte Corporation Spirocyclic lactams as JAK2 V617F inhibitors
AU2021473165B2 (en) * 2021-11-09 2025-05-22 Guangzhou HC New Drug Research Co., Ltd. PHARMACEUTICAL COMPOSITION CONTAINING β-LACTAM COMPOUND AND USE THEREOF
US11932637B2 (en) * 2021-11-18 2024-03-19 Merck Sharp & Dohme Llc Chromane amidine monobactam compounds for the treatment of bacterial infections
JP7671398B2 (ja) * 2021-11-18 2025-05-01 メルク・シャープ・アンド・ドーム・エルエルシー クロマンアミジンモノバクタム抗生物質
US12084430B2 (en) 2022-03-17 2024-09-10 Incyte Corporation Tricyclic urea compounds as JAK2 V617F inhibitors
EP4558137A2 (en) * 2022-07-18 2025-05-28 Merck Sharp & Dohme LLC Chromane amidine monobactam compounds for the treatment of bacterial infections

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WO2008074856A1 (en) 2006-12-21 2008-06-26 Novartis Ag Combination therapy for the treatment of airways disease
WO2015148379A1 (en) 2014-03-24 2015-10-01 Novartis Ag Monobactam organic compounds for the treatment of bacterial infections
WO2017106064A1 (en) 2015-12-15 2017-06-22 Merck Sharp & Dohme Corp. Biaryl monobactam compounds and methods of use thereof for the treatment of bacterial infections
WO2017155765A1 (en) 2016-03-07 2017-09-14 Merck Sharp & Dohme Corp. Bicyclic aryl monobactam compounds and methods of use thereof for the treatment of bacterial infections

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CA2783572C (en) 2005-12-07 2016-08-09 Basilea Pharmaceutica Ag Useful combinations of monobactam antibiotics with beta-lactamase inhibitors
EA031698B1 (ru) 2010-10-11 2019-02-28 Байоджен Интернэшнл Нейросайенз Гмбх Человеческие анти-тау антитела
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SG10201803472QA (en) 2014-10-31 2018-06-28 Abbvie Sarl Substituted chromanes and method of use
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WO2008074856A1 (en) 2006-12-21 2008-06-26 Novartis Ag Combination therapy for the treatment of airways disease
WO2015148379A1 (en) 2014-03-24 2015-10-01 Novartis Ag Monobactam organic compounds for the treatment of bacterial infections
WO2017106064A1 (en) 2015-12-15 2017-06-22 Merck Sharp & Dohme Corp. Biaryl monobactam compounds and methods of use thereof for the treatment of bacterial infections
WO2017155765A1 (en) 2016-03-07 2017-09-14 Merck Sharp & Dohme Corp. Bicyclic aryl monobactam compounds and methods of use thereof for the treatment of bacterial infections

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CO2020004087A2 (es) 2020-04-24
NZ762899A (en) 2024-07-26
AU2018345523B2 (en) 2021-10-21
KR20200058520A (ko) 2020-05-27
MA50629A (fr) 2021-03-31
JP2020536082A (ja) 2020-12-10
EP3691639B1 (en) 2023-11-15
IL273306B (en) 2022-04-01
IL273306A (en) 2020-04-30
EP3691639A1 (en) 2020-08-12
CL2020000860A1 (es) 2020-08-14
SG11202002575UA (en) 2020-04-29
JP7252948B2 (ja) 2023-04-05
US20200297702A1 (en) 2020-09-24
US11433055B2 (en) 2022-09-06
CA3076022A1 (en) 2019-04-11
BR112020006381A2 (pt) 2020-09-24
DOP2020000058A (es) 2020-09-15
GEP20227406B (en) 2022-08-25
CN111201021B (zh) 2024-08-23
ZA202001721B (en) 2023-02-22
EP3691639A4 (en) 2021-03-31
BR112020006381A8 (pt) 2023-04-11
CR20200148A (es) 2020-05-22
PE20201256A1 (es) 2020-11-16
PH12020550107A1 (en) 2020-12-07
MX2020003581A (es) 2020-07-22
UA126000C2 (uk) 2022-07-27
AU2018345523A1 (en) 2020-03-26
NI202000023A (es) 2020-09-24
ES2968467T3 (es) 2024-05-09
CN118496221A (zh) 2024-08-16
JOP20200130A1 (ar) 2020-05-28
CA3076022C (en) 2023-01-17
CN111201021A (zh) 2020-05-26
EA202090604A1 (ru) 2020-10-15
WO2019070492A1 (en) 2019-04-11
SA520411571B1 (ar) 2024-08-27

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