CN109715630B - β-内酰胺酶抑制剂化合物 - Google Patents

β-内酰胺酶抑制剂化合物 Download PDF

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Publication number
CN109715630B
CN109715630B CN201780057302.4A CN201780057302A CN109715630B CN 109715630 B CN109715630 B CN 109715630B CN 201780057302 A CN201780057302 A CN 201780057302A CN 109715630 B CN109715630 B CN 109715630B
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mmol
methyl
oxo
tert
diazabicyclo
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CN109715630A (zh
Inventor
贾内尔·科米塔-普莱瓦尔
托马斯·佛朗索瓦·杜兰德-雷维尔
利兹·高蒂尔
约翰·奥唐奈
扬·罗梅罗
鲁本·托马斯
杰伦·库涅拉·维尔海连
吴新和
吴晓云
张靖
格雷戈里·S·巴萨拉布
比尔·莫斯
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AstraZeneca AB
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AstraZeneca AB
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D211/78—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • 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
    • A61K31/546—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 containing further heterocyclic rings, e.g. cephalothin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B43/00—Formation or introduction of functional groups containing nitrogen
    • 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
    • C07D471/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/0834—Compounds having one or more O-Si linkage
    • C07F7/0892—Compounds with a Si-O-N linkage
    • 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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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
CN201780057302.4A 2016-09-16 2017-09-15 β-内酰胺酶抑制剂化合物 Active CN109715630B (zh)

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Applications Claiming Priority (5)

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US201662395464P 2016-09-16 2016-09-16
US62/395,464 2016-09-16
US201762456423P 2017-02-08 2017-02-08
US62/456,423 2017-02-08
PCT/US2017/051692 WO2018053215A1 (en) 2016-09-16 2017-09-15 Beta-lactamase inhibitor compounds

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CN114591223B (zh) * 2016-09-16 2025-01-24 恩塔西斯治疗有限公司 β-内酰胺酶抑制剂化合物

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EP3781576B1 (en) 2018-04-20 2024-06-12 Qpex Biopharma, Inc. Boronic acid derivatives and therapeutic uses thereof
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CN110898999A (zh) * 2019-11-26 2020-03-24 中国矿业大学 一种煤焦油基煤泥浮选药剂及其制备方法
CN111790439B (zh) * 2020-07-29 2022-12-27 成都能特科技发展有限公司 一种手性二级胺二苯基膦芳甲酰胺双功能催化剂及其制备方法与应用
EP4146650A4 (en) 2020-09-01 2024-01-17 Ningxia Academy of Agriculture and Forestry Sciences BETA-LACTAMASE INHIBITORS AND THEIR PRODUCTION
CN117157078A (zh) * 2021-04-05 2023-12-01 Qpex生物制药有限公司 头孢布烯给药方案
EP4146651A4 (en) 2021-05-07 2024-06-05 Ningxia Academy of Agriculture and Forestry Sciences SULFONYLAMIDINE SUBSTITUTED COMPOUNDS AND THEIR USE AS BETA-LACTAMASE INHIBITORS
US11814385B2 (en) * 2021-06-25 2023-11-14 University Of South Florida Small molecule inhibitors targeting Clostridioides difficile sporulation
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US20230398101A1 (en) * 2022-06-09 2023-12-14 Fleurir Abx Llc Co-agents as Therapy Against Anaerobic Pathogens
CN118271319B (zh) * 2022-12-30 2025-02-28 成都四面体药物研究有限公司 一种β-内酰胺酶抑制剂含脲双环化合物、其制备方法及其用途
CN118772145B (zh) * 2023-04-04 2025-10-10 上海医药工业研究院有限公司 一种二氮杂双环辛烯化合物的制备方法
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CA3036557A1 (en) 2018-03-22
IL289686B2 (en) 2023-03-01
MX385507B (es) 2025-03-18
KR102537340B1 (ko) 2023-05-26
SI3512851T1 (sl) 2022-11-30
DK3512851T3 (en) 2022-10-17
MX392515B (es) 2025-03-24
MA46242A (fr) 2019-07-24
IL265276B (en) 2022-02-01
KR102667828B1 (ko) 2024-05-20
TW201823207A (zh) 2018-07-01
AU2017325863B2 (en) 2021-08-19
PH12019500558A1 (en) 2019-07-29
KR20190043630A (ko) 2019-04-26
BR112019005053A2 (pt) 2019-06-18
CN114591223A (zh) 2022-06-07
EP3512851A1 (en) 2019-07-24
NZ751016A (en) 2025-02-28
MX2021010077A (es) 2022-05-23
TWI773687B (zh) 2022-08-11
IL265276A (en) 2019-05-30
HUE060282T2 (hu) 2023-02-28
JP2019532928A (ja) 2019-11-14
SMT202200397T1 (it) 2022-11-18
KR20230078830A (ko) 2023-06-02
US20190202832A1 (en) 2019-07-04
WO2018053215A1 (en) 2018-03-22
HRP20221217T1 (hr) 2022-12-23
PH12019500558B1 (en) 2023-09-08
SG11201901658PA (en) 2019-04-29
US10800778B2 (en) 2020-10-13
PL3512851T3 (pl) 2022-11-14
CN114591223B (zh) 2025-01-24
JP6997178B2 (ja) 2022-02-03
PT3512851T (pt) 2022-10-11
LT3512851T (lt) 2022-10-25
JP2022046563A (ja) 2022-03-23
IL289686A (en) 2022-03-01
MX2019003060A (es) 2019-07-08
EP3512851B1 (en) 2022-07-06
ES2927986T3 (es) 2022-11-14
JP7281527B2 (ja) 2023-05-25
AU2017325863A1 (en) 2019-03-14
IL289686B (en) 2022-11-01
CN109715630A (zh) 2019-05-03

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