TWI754613B - 雜環化合物及其用於預防或治療細菌感染之用途 - Google Patents

雜環化合物及其用於預防或治療細菌感染之用途 Download PDF

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Publication number
TWI754613B
TWI754613B TW105114242A TW105114242A TWI754613B TW I754613 B TWI754613 B TW I754613B TW 105114242 A TW105114242 A TW 105114242A TW 105114242 A TW105114242 A TW 105114242A TW I754613 B TWI754613 B TW I754613B
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TW
Taiwan
Prior art keywords
mmol
oct
diazabicyclo
oxy
alkyl
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TW105114242A
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English (en)
Chinese (zh)
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TW201643165A (zh
Inventor
茱莉安 巴比昂
奧黛莉 卡拉維諾
蘇非 捷斯特
法蘭西斯 查凡羅爾
尼可拉斯 雷克印地
班諾特 里道索爾
史崔特 費德力克 雷
賽巴斯汀 里查
克里斯多夫 賽門
蘇非 沃斯查德
茱莉 布亞斯
蘇非 比里特
法賓 費為爾
佛立克 吉瑞爾丁 雷
克里斯戴爾 奧利維亞
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法商木塔比利斯公司
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Priority claimed from EP15305701.3A external-priority patent/EP3091018A1/en
Application filed by 法商木塔比利斯公司 filed Critical 法商木塔比利斯公司
Publication of TW201643165A publication Critical patent/TW201643165A/zh
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/08Bridged systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/439Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic 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
    • A61K31/542Heterocyclic 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
    • A61K31/545Compounds 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
    • A61K31/546Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against 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)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
TW105114242A 2015-05-07 2016-05-06 雜環化合物及其用於預防或治療細菌感染之用途 TWI754613B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
EP15305701.3A EP3091018A1 (en) 2015-05-07 2015-05-07 Heterocyclic compounds and their use in preventing or treating bacterial infections
EP15305701.3 2015-05-07
EP16305144 2016-02-08
EP16305144.4 2016-02-08

Publications (2)

Publication Number Publication Date
TW201643165A TW201643165A (zh) 2016-12-16
TWI754613B true TWI754613B (zh) 2022-02-11

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Country Link
US (1) US10183943B2 (enExample)
EP (1) EP3292125B1 (enExample)
JP (1) JP6767392B2 (enExample)
KR (1) KR102713561B1 (enExample)
CN (1) CN107580595B (enExample)
AU (1) AU2016257338B2 (enExample)
BR (1) BR112017023359A2 (enExample)
CA (1) CA2983674A1 (enExample)
CL (1) CL2017002803A1 (enExample)
MX (1) MX2017014080A (enExample)
RU (1) RU2741496C2 (enExample)
TW (1) TWI754613B (enExample)
WO (1) WO2016177862A1 (enExample)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20170014135A1 (en) 2015-07-14 2017-01-19 Keith Edward Martin Surgical tool
EP3300736B1 (en) * 2016-09-30 2021-05-05 Mutabilis Composition comprising antibiotic compound and an heterocyclic compound and their use in preventing or treating bacterial infections
EP3301094A1 (en) * 2016-09-30 2018-04-04 Mutabilis Heterocyclic compounds and their use in preventing or treating bacterial infections
EP3357924A1 (en) 2017-02-06 2018-08-08 Mutabilis Novel heterocyclic compounds and their use in preventing or treating bacterial infections
US11905286B2 (en) 2018-08-09 2024-02-20 Antabio Sas Diazabicyclooctanones as inhibitors of serine beta-lactamases
ES2960952T3 (es) 2018-08-09 2024-03-07 Antabio Sas Diazabiciclooctanonas como inhibidores de serina beta-lactamasas

Citations (1)

* Cited by examiner, † Cited by third party
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WO2013150296A1 (en) * 2012-04-02 2013-10-10 Astrazeneca Ab Heterobicyclic compounds as beta-lactamase inhibitors

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FR2812635B1 (fr) * 2000-08-01 2002-10-11 Aventis Pharma Sa Nouveaux composes heterocycliques, preparation et utilisation comme medicaments notamment comme anti- bacteriens
FR2835186B1 (fr) * 2002-01-28 2006-10-20 Aventis Pharma Sa Nouveaux composes heterocycliques, actifs comme inhibiteurs de beta-lactamases
EP2231667B1 (en) * 2008-01-18 2013-09-04 Merck Sharp & Dohme Corp. Beta-lactamase inhibitors
BR112013032974A2 (pt) * 2011-08-30 2016-09-06 Wockhardt Ltd "derivados de 1,6-diazabiciclo [3,2,1]-octan-7-ona, seus usos, e composições farmacêuticas".
SG11201406123TA (en) * 2012-03-30 2014-10-30 Cubist Pharm Inc 1,3,4-OXADIAZOLE AND 1,3,4-THIADIAZOLE β-LACTAMASE INHIBITORS
CN104470906B (zh) 2012-06-04 2016-08-24 爱尔克米亚 作为抵抗紫外线辐射的保护剂的亚氨基化合物
US20140315876A1 (en) * 2013-03-15 2014-10-23 Cubist Pharmaceuticals, Inc. Beta-lactamase inhibitors
BR112016008979B1 (pt) * 2013-10-22 2023-04-25 Wockhardt Limited Composições farmacêuticas compreendendo agentes antibacterianos e seus usos
KR20170132301A (ko) * 2015-03-31 2017-12-01 무타빌리스 신규한 헤테로사이클릭 화합물들 및 세균성 감염의 예방 또는 치료에서 그들의 용도

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013150296A1 (en) * 2012-04-02 2013-10-10 Astrazeneca Ab Heterobicyclic compounds as beta-lactamase inhibitors

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Publication number Publication date
US20180093985A1 (en) 2018-04-05
KR102713561B1 (ko) 2024-10-08
AU2016257338A1 (en) 2017-10-26
RU2017135321A3 (enExample) 2019-08-13
AU2016257338B2 (en) 2020-03-05
BR112017023359A2 (pt) 2018-07-17
EP3292125B1 (en) 2019-09-04
KR20180002650A (ko) 2018-01-08
CL2017002803A1 (es) 2018-05-11
RU2741496C2 (ru) 2021-01-26
NZ736152A (en) 2024-09-27
WO2016177862A1 (en) 2016-11-10
MX2017014080A (es) 2018-07-06
CN107580595A (zh) 2018-01-12
CN107580595B (zh) 2020-09-18
RU2017135321A (ru) 2019-04-10
US10183943B2 (en) 2019-01-22
JP2018515504A (ja) 2018-06-14
JP6767392B2 (ja) 2020-10-14
EP3292125A1 (en) 2018-03-14
TW201643165A (zh) 2016-12-16
CA2983674A1 (en) 2016-11-10

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