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PE20201256A1 - Compuestos monobactamicos cromanos para el tratamiento de infecciones bacterianas - Google Patents

Compuestos monobactamicos cromanos para el tratamiento de infecciones bacterianas

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Publication number
PE20201256A1
PE20201256A1 PE2020000692A PE2020000692A PE20201256A1 PE 20201256 A1 PE20201256 A1 PE 20201256A1 PE 2020000692 A PE2020000692 A PE 2020000692A PE 2020000692 A PE2020000692 A PE 2020000692A PE 20201256 A1 PE20201256 A1 PE 20201256A1
Authority
PE
Peru
Prior art keywords
alkyl
hydrogen
compounds
treatment
bacterial infections
Prior art date
Application number
PE2020000692A
Other languages
English (en)
Inventor
Tesfaye Biftu
Xianhai Huang
Weiguo Liu
Weidong Pan
Min Park
Alexander Pasternak
Wanying Sun
Haifeng Tang
Yi Zang
Original Assignee
Merck Sharp & Dohme
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of PE20201256A1 publication Critical patent/PE20201256A1/es

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    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/42Oxazoles
    • A61K31/424Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/429Thiazoles condensed with heterocyclic ring systems
    • A61K31/43Compounds 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
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/429Thiazoles condensed with heterocyclic ring systems
    • A61K31/43Compounds 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
    • A61K31/431Compounds 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
    • 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
    • A61K31/4425Pyridinium derivatives, e.g. pralidoxime, pyridostigmine
    • 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
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non 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
    • 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
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic 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
    • 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
    • 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • 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

Landscapes

  • 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)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente invencion se refiere a un compuesto de formula (I), o una sal farmaceuticamente aceptable, en donde: T es CH o N, siempre que no mas de dos T, U y V sean N; U y V son CH o N; W es un enlace u O; Q es N o CR3; X es O o CH2; Y es O, S, CH2 o NR8, siempre que cuando Y es O, NR8 o S, X no es O; Z es O, S, CH2 o NH, siempre que cuando Z es O, S o NH, X no es O; A es -C(=NH)-NH, cicloalquilo C3-C7, entre otros; L esta ausente o es R4, NHR4, entre otros; M es R5, NHR5, entre otros; R1 es hidrogeno, alquilo C1-C8, entre otros; R2 es hidrogeno, alquilo C1-C8, cicloalquilo C3-C7, entre otros; R3 es hidrogeno, alquilo C1-C4, entre otros; R8 es hidrogeno, alquilo C1-C4 o cicloalquilo C3-C7; Rb es hidrogeno, alquilo C1-C6, entre otros; Rj es hidrogeno, alquilo C1-C3, entre otros; s y t son 0 a 3. Son compuestos especificos, los compuestos de formulas i) a iv), entre otros. Tambien se refiere a una composicion farmaceutica. Dichos compuestos son analogos monobactamicos novedosos, los cuales son altamente potentes y eficaces contra un amplio rango de bacterias gran-negativas, siendo utiles en el tratamiento de infecciones bacterianas.
PE2020000692A 2017-10-02 2018-09-27 Compuestos monobactamicos cromanos para el tratamiento de infecciones bacterianas PE20201256A1 (es)

Applications Claiming Priority (2)

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

Publications (1)

Publication Number Publication Date
PE20201256A1 true PE20201256A1 (es) 2020-11-16

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PE2020000692A PE20201256A1 (es) 2017-10-02 2018-09-27 Compuestos monobactamicos cromanos para el tratamiento de infecciones bacterianas

Country Status (26)

Country Link
US (1) US11433055B2 (es)
EP (1) EP3691639B1 (es)
JP (1) JP7252948B2 (es)
KR (1) KR102425959B1 (es)
CN (2) CN118496221A (es)
AU (1) AU2018345523B2 (es)
CA (1) CA3076022C (es)
CL (1) CL2020000860A1 (es)
CO (1) CO2020004087A2 (es)
CR (1) CR20200148A (es)
DO (1) DOP2020000058A (es)
EA (1) EA202090604A1 (es)
ES (1) ES2968467T3 (es)
GE (1) GEP20227406B (es)
IL (1) IL273306B (es)
JO (1) JOP20200130A1 (es)
MA (1) MA50629A (es)
MX (1) MX2020003581A (es)
NI (1) NI202000023A (es)
PE (1) PE20201256A1 (es)
PH (1) PH12020550107A1 (es)
SA (1) SA520411571B1 (es)
SG (1) SG11202002575UA (es)
UA (1) UA126000C2 (es)
WO (1) WO2019070492A1 (es)
ZA (1) ZA202001721B (es)

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WO2021257863A1 (en) 2020-06-19 2021-12-23 Incyte Corporation Pyrrolotriazine compounds as jak2 v617f inhibitors
WO2021257857A1 (en) 2020-06-19 2021-12-23 Incyte Corporation Naphthyridinone compounds as jak2 v617f inhibitors
US11767323B2 (en) 2020-07-02 2023-09-26 Incyte Corporation Tricyclic pyridone compounds as JAK2 V617F inhibitors
WO2022006457A1 (en) 2020-07-02 2022-01-06 Incyte Corporation Tricyclic urea compounds as jak2 v617f inhibitors
WO2022046989A1 (en) 2020-08-27 2022-03-03 Incyte Corporation Tricyclic urea compounds as jak2 v617f inhibitors
WO2022120048A1 (en) * 2020-12-03 2022-06-09 University Of Pittsburgh - Of The Commonwealth System Of Higher Education Hdac inhibitors
US11919908B2 (en) 2020-12-21 2024-03-05 Incyte Corporation Substituted pyrrolo[2,3-d]pyrimidine compounds as JAK2 V617F inhibitors
WO2022182839A1 (en) 2021-02-25 2022-09-01 Incyte Corporation Spirocyclic lactams as jak2 v617f inhibitors
JP2024537930A (ja) * 2021-11-09 2024-10-16 インスティテュート オブ メディシナル バイオテクノロジー、チャイニーズ アカデミー オブ メディカル サイエンシーズ β-ラクタム化合物を含む医薬組成物及びその使用
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
EP4433476A1 (en) 2021-11-18 2024-09-25 Merck Sharp & Dohme LLC Chromane amidine monobactam antibiotics
JP2025509672A (ja) 2022-03-17 2025-04-11 インサイト・コーポレイション Jak2 v617f阻害剤としての三環式尿素化合物
WO2024019916A2 (en) * 2022-07-18 2024-01-25 Merck Sharp & Dohme Llc Chromane amidine monobactam compounds for the treatment of bacterial infections

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WO2019070492A1 (en) 2019-04-11
NI202000023A (es) 2020-09-24
DOP2020000058A (es) 2020-09-15
NZ762899A (en) 2024-07-26
UA126000C2 (uk) 2022-07-27
ZA202001721B (en) 2023-02-22
KR102425959B1 (ko) 2022-07-27
AU2018345523B2 (en) 2021-10-21
JP2020536082A (ja) 2020-12-10
GEP20227406B (en) 2022-08-25
SA520411571B1 (ar) 2024-08-27
JOP20200130A1 (ar) 2020-05-28
SG11202002575UA (en) 2020-04-29
EP3691639A4 (en) 2021-03-31
PH12020550107A1 (en) 2020-12-07
CN111201021B (zh) 2024-08-23
CR20200148A (es) 2020-05-22
AU2018345523A1 (en) 2020-03-26
IL273306A (en) 2020-04-30
CA3076022A1 (en) 2019-04-11
EP3691639B1 (en) 2023-11-15
JP7252948B2 (ja) 2023-04-05
CO2020004087A2 (es) 2020-04-24
CN111201021A (zh) 2020-05-26
EA202090604A1 (ru) 2020-10-15
BR112020006381A2 (pt) 2020-09-24
MA50629A (fr) 2021-03-31
CN118496221A (zh) 2024-08-16
US11433055B2 (en) 2022-09-06
IL273306B (en) 2022-04-01
EP3691639A1 (en) 2020-08-12
CL2020000860A1 (es) 2020-08-14
BR112020006381A8 (pt) 2023-04-11
US20200297702A1 (en) 2020-09-24
CA3076022C (en) 2023-01-17
ES2968467T3 (es) 2024-05-09
KR20200058520A (ko) 2020-05-27
MX2020003581A (es) 2020-07-22

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