HRP20230977T1 - Derivati 3-(((((2s,5r)-2-karbamoil-7-okso-1,6-diazabiciklo[3.2.1]oktan-6- il)oksi)sulfonil)oksi)-2,2-dimetilpropanoata i srodni spojevi kao peroralno primijenjeni predlijekovi inhibitora beta-laktamaze namijenjenih liječenju bakterijskih infekcija - Google Patents
Derivati 3-(((((2s,5r)-2-karbamoil-7-okso-1,6-diazabiciklo[3.2.1]oktan-6- il)oksi)sulfonil)oksi)-2,2-dimetilpropanoata i srodni spojevi kao peroralno primijenjeni predlijekovi inhibitora beta-laktamaze namijenjenih liječenju bakterijskih infekcija Download PDFInfo
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- HRP20230977T1 HRP20230977T1 HRP20230977TT HRP20230977T HRP20230977T1 HR P20230977 T1 HRP20230977 T1 HR P20230977T1 HR P20230977T T HRP20230977T T HR P20230977TT HR P20230977 T HRP20230977 T HR P20230977T HR P20230977 T1 HRP20230977 T1 HR P20230977T1
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- Prior art keywords
- oxy
- oxo
- diazabicyclo
- carbamoyl
- sulfonyl
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- 150000001875 compounds Chemical class 0.000 title claims 25
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 title claims 24
- 208000035143 Bacterial infection Diseases 0.000 title claims 9
- 208000022362 bacterial infectious disease Diseases 0.000 title claims 9
- -1 (2s,5r)-2-carbamoyl-7-oxo-1,6-diazabicyclo[3.2.1]octan-6-yl Chemical group 0.000 title claims 7
- 239000003781 beta lactamase inhibitor Substances 0.000 title claims 2
- 229940126813 beta-lactamase inhibitor Drugs 0.000 title claims 2
- 150000003839 salts Chemical class 0.000 claims 11
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- 239000003782 beta lactam antibiotic agent Substances 0.000 claims 5
- 239000002132 β-lactam antibiotic Substances 0.000 claims 5
- 229940124586 β-lactam antibiotics Drugs 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 239000000825 pharmaceutical preparation Substances 0.000 claims 3
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 2
- 108090000204 Dipeptidase 1 Proteins 0.000 claims 2
- 208000036209 Intraabdominal Infections Diseases 0.000 claims 2
- 102000006635 beta-lactamase Human genes 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 229960004261 cefotaxime Drugs 0.000 claims 2
- AZZMGZXNTDTSME-JUZDKLSSSA-M cefotaxime sodium Chemical compound [Na+].N([C@@H]1C(N2C(=C(COC(C)=O)CS[C@@H]21)C([O-])=O)=O)C(=O)\C(=N/OC)C1=CSC(N)=N1 AZZMGZXNTDTSME-JUZDKLSSSA-M 0.000 claims 2
- WYUSVOMTXWRGEK-HBWVYFAYSA-N cefpodoxime Chemical compound N([C@H]1[C@@H]2N(C1=O)C(=C(CS2)COC)C(O)=O)C(=O)C(=N/OC)\C1=CSC(N)=N1 WYUSVOMTXWRGEK-HBWVYFAYSA-N 0.000 claims 2
- 229960005090 cefpodoxime Drugs 0.000 claims 2
- UNJFKXSSGBWRBZ-BJCIPQKHSA-N ceftibuten Chemical compound S1C(N)=NC(C(=C\CC(O)=O)\C(=O)N[C@@H]2C(N3C(=CCS[C@@H]32)C(O)=O)=O)=C1 UNJFKXSSGBWRBZ-BJCIPQKHSA-N 0.000 claims 2
- 229960004086 ceftibuten Drugs 0.000 claims 2
- 229960004755 ceftriaxone Drugs 0.000 claims 2
- VAAUVRVFOQPIGI-SPQHTLEESA-N ceftriaxone Chemical compound S([C@@H]1[C@@H](C(N1C=1C(O)=O)=O)NC(=O)\C(=N/OC)C=2N=C(N)SC=2)CC=1CSC1=NC(=O)C(=O)NN1C VAAUVRVFOQPIGI-SPQHTLEESA-N 0.000 claims 2
- 125000004404 heteroalkyl group Chemical group 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 208000019206 urinary tract infection Diseases 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- QYIOFABFKUOIBV-UHFFFAOYSA-N 4,5-dimethyl-1,3-dioxol-2-one Chemical group CC=1OC(=O)OC=1C QYIOFABFKUOIBV-UHFFFAOYSA-N 0.000 claims 1
- 241000894006 Bacteria Species 0.000 claims 1
- 206010035664 Pneumonia Diseases 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- TXWOGHSRPAYOML-UHFFFAOYSA-M cyclobutanecarboxylate Chemical compound [O-]C(=O)C1CCC1 TXWOGHSRPAYOML-UHFFFAOYSA-M 0.000 claims 1
- NZNMSOFKMUBTKW-UHFFFAOYSA-M cyclohexanecarboxylate Chemical compound [O-]C(=O)C1CCCCC1 NZNMSOFKMUBTKW-UHFFFAOYSA-M 0.000 claims 1
- YMGUBTXCNDTFJI-UHFFFAOYSA-M cyclopropanecarboxylate Chemical compound [O-]C(=O)C1CC1 YMGUBTXCNDTFJI-UHFFFAOYSA-M 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 1
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000003136 n-heptyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000001280 n-hexyl group Chemical group C(CCCCC)* 0.000 claims 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 229940126085 β‑Lactamase Inhibitor Drugs 0.000 claims 1
Classifications
-
- 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
-
- 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
-
- 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
- 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
-
- 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)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pyrrole Compounds (AREA)
- Cephalosporin Compounds (AREA)
- Medicinal Preparation (AREA)
- Storage Device Security (AREA)
Claims (19)
1. Spoj Formule (1):
[image]
,
ili njegova farmaceutski prihvatljiva sol, naznačen time što
svaki od R5, R6 i R7 je vodik;
A je jednostruka veza;
svakog R1 se neovisno bira između C1-3 alkila, ili svaki R1 zajedno s atomom ugljika na kojeg su vezani tvore C3-6 cikloalkilni prsten;
R2 se bira između jednostruka veza, methane-diil, te ethane-diil;
R3 je -C(O)-O-R4, gdje se R4 bira između C1-10 alkila, C1-10 heteroalkila, C5-10 arilalkila, C3-6 heterocikloalkila, te supstituiranog C4-10 heterocikloalkilalkila; i
heteroalkil se odnosi na alkilna skupina u kojoj se jedan ili više atoma ugljika (i određene asocirane atome vodika) neovisno zamjenjuje jednom ili više istih ili različitih heteroatomskih skupina, koje se bira između -O-, -S-, -NH-, -N(-CH3), -SO- i -SO2-.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što se svakog R1 neovisno bira između C1-3 alkila.
3. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 2, naznačen time što je R2 jednostruka veza.
4. Spoj u skladu s patentnim zahtjevom 1, naznačen time što R4 je C1-10 alkil.
5. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 4, naznačen time što:
R1 je neovisno C1-3 alkil;
R2 je jednostruka veza; i
R4 je C1-10 alkil.
6. Spoj u skladu s patentnim zahtjevom 1, naznačen time što:
svaki R1 je metil;
R2 je jednostruka veza; i
R4 se bira između metila, etila, n-propila, iso-propila, n-butila, n-heksila, n-heptila, -CH2-CH2-O-CH3, benzila, 3-oksetanil, te metil-5-metil-1,3-dioksol-2-on.
7. Spoj u skladu s patentnim zahtjevom 1, naznačen time što se spoj bira između:
etil-3-(((((1R,2S,5R)-2-karbamoil-7-okso-1,6-diazabiciklo[3.2.1]oktan-6-il)oksi)sulfonil)oksi)-2,2-dimetilpropanoata (3);
benzil-3-(((((1R,2S,5R)-2-karbamoil-7-okso-1,6-diazabiciklo[3.2.1]oktan-6-il)oksi)sulfonil)oksi)-2,2-dimetilpropanoata (4);
metil-3-(((((1R,2S,5R)-2-karbamoil-7-okso-1,6-diazabiciklo[3.2.1]oktan-6-il)oksi)sulfonil)oksi)-2,2-dimetilpropanoata (10);
izopropil-3-(((((1R,2S,5R)-2-karbamoil-7-okso-1,6-diazabiciklo[3.2.1]oktan-6-il)oksi)sulfonil)oksi)-2,2-dimetilpropanoata (11);
heksil-3-(((((1R,2S,5R)-2-karbamoil-7-okso-1,6-diazabiciklo[3.2.1]oktan-6-il)oksi)sulfonil)oksi)-2,2-dimetilpropanoata (12);
heptil-3-(((((1R,2S,5R)-2-karbamoil-7-okso-1,6-diazabiciklo[3.2.1]oktan-6-il)oksi)sulfonil)oksi)-2,2-dimetilpropanoata (13);
tert-butil-3-(((((1R,2S,5R)-2-karbamoil-7-okso-1,6-diazabiciklo[3.2.1]oktan-6-il)oksi)sulfonil)oksi)-2,2-dimetilpropanoata (14);
2-metoksietil-3-(((((1R,2S,5R)-2-karbamoil-7-okso-1,6-diazabiciklo[3.2.1]oktan-6-il)oksi)sulfonil)oksi)-2,2-dimetilpropanoata (15);
oksetan-3-il-3-(((((1R,2S,5R)-2-karbamoil-7-okso-1,6-diazabiciklo[3.2.1]oktan-6-il)oksi)sulfonil)oksi)-2,2-dimetilpropanoata (16);
etil-1-((((((1R,2S,5R)-2-karbamoil-7-okso-1,6-diazabiciklo[3.2.1]oktan-6-il)oksi)sulfonil)oksi)metil)cikloheksankarboksilata (17);
etil-1-((((((1R,2S,5R)-2-karbamoil-7-okso-1,6-diazabiciklo[3.2.1]oktan-6-il)oksi)sulfonil)oksi)metil)ciklopropankarboksilata (18);
etil-1-((((((1R,2S,5R)-2-karbamoil-7-okso-1,6-diazabiciklo[3.2.1]oktan-6-il)oksi)sulfonil)oksi)metil)ciklobutankarboksilata (19);
etil-5-(((((1R,2S,5R)-2-karbamoil-7-okso-1,6-diazabiciklo[3.2.1]oktan-6-il)oksi)sulfonil)oksi)-4,4-dimetilpentanoata (35);
heksil-5-(((((1R,2S,5R)-2-karbamoil-7-okso-1,6-diazabiciklo[3.2.1]oktan-6-il)oksi)sulfonil)oksi)-4,4-dimetilpentanoata (36);
heptil-5-(((((1R,2S,5R)-2-karbamoil-7-okso-1,6-diazabiciklo[3.2.1]oktan-6-il)oksi)sulfonil)oksi)-4,4-dimetilpentanoata (37);
2-metoksietil-5-(((((1R,2S,5R)-2-karbamoil-7-okso-1,6-diazabiciklo[3.2.1]oktan-6-il)oksi)sulfonil)oksi)-4,4-dimetilpentanoata (38);
propil-3-(((((1R,2S,5R)-2-karbamoil-7-okso-1,6-diazabiciklo[3.2.1]oktan-6-il)oksi)sulfonil)oksi)-2,2-dimetilpropanoata (57);
butil-3-(((((1R,2S,5R)-2-karbamoil-7-okso-1,6-diazabiciklo[3.2.1]oktan-6-il)oksi)sulfonil)oksi)-2,2-dimetilpropanoata (58);
(5-metil-2-okso-1,3-dioksol-4-il)metil-3-(((((1R,2S,5R)-2-karbamoil-7-okso-1,6-diazabiciklo[3.2.1]oktan-6-il)oksi)sulfonil)oksi)-2,2-dimetilpropanoata (59);
etil-2-((((((1R,2S,5R)-2-karbamoil-7-okso-1,6-diazabiciklo[3.2.1]oktan-6-il)oksi)sulfonil)oksi)metil)-2-etilbutanoata (61);
farmaceutski prihvatljive sol u skladu s bilo kojim od prethodnog; i
kombinacije u skladu s bilo kojim od prethodnog.
8. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je spoj etil-3-(((((1R,2S,5R)-2-karbamoil-7-okso-1,6-diazabiciklo[3.2.1]oktan-6-il)oksi)sulfonil)oksi)-2,2-dimetilpropanoat (3)
[image]
,
ili njegova farmaceutski prihvatljiva sol.
9. Spoj u skladu s patentnim zahtjevom 8, naznačen time što je spoj etil-3-(((((1R,2S,5R)-2-karbamoil-7-okso-1,6-diazabiciklo[3.2.1]oktan-6-il)oksi)sulfonil)oksi)-2,2-dimetilpropanoat (3):
[image]
,
10. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je spoj etil-5-(((((1R,2S,5R)-2-karbamoil-7-okso-1,6-diazabiciklo[3.2.1]oktan-6-il)oksi)sulfonil)oksi)-4,4-dimetilpentanoat (35):
[image]
,
ili njegova farmaceutski prihvatljiva sol.
11. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 10, ili njegovu farmaceutski prihvatljivu sol, i farmaceutski prihvatljivi vehikulum.
12. Farmaceutski pripravak u skladu s patentnim zahtjevom 11, further comprising a β-laktamski antibiotik.
13. Farmaceutski pripravak u skladu s patentnim zahtjevom 12, naznačen time što je β-laktamski antibiotik cefotaksim, cefpodoksim, ceftaz, ceftibuten ili ceftriakson.
14. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 10, ili njegova farmaceutski prihvatljiva sol, namijenjen upotrebi u postupku liječenja bakterijske infekcije kod pacijenta, naznačen time što se postupak sastoji u primjeni na pacijentu kojem je potrebno takvo liječenje terapijski djelotvorne količine spoja u skladu s bilo kojim od patentnih zahtjeva 1 do 10, ili njegove farmaceutski prihvatljive soli, i terapijski djelotvorne količine β-laktamskog antibiotika, gdje je bakterijska infekcija bakterijska infekcija uzrokovana bakterijama koje proizvode β-laktamazu.
15. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 10, ili njegova farmaceutski prihvatljiva sol, namijenjen upotrebi u postupku liječenja bakterijske infekcije kod pacijenta, naznačen time što se postupak sastoji u primjeni na pacijentu kojem je potrebno takvo liječenje terapijski djelotvorne količine spoja u skladu s bilo kojim od patentnih zahtjeva 1 do 10, ili njegove farmaceutski prihvatljive soli, i terapijski djelotvorne količine β-laktamskog antibiotika, gdje je bakterijska infekcija bakterijska infekcija kod koje je inhibitor β-laktamaze djelotvoran u liječenju bakterijske infekcije.
16. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 10, ili njegova farmaceutski prihvatljiva sol, namijenjen upotrebi u postupku inhibiranja enzima β-laktamaze kod pacijenta, naznačen time što se postupak sastoji u primjeni na pacijentu djelotvorne količine spoja u skladu s bilo kojim od patentnih zahtjeva 1 do 10, ili njegove farmaceutske soli.
17. Spoj namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 14 do 16, naznačen time što se primjena sastoji u oralnoj primjeni.
18. Spoj namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 14 ili 15, naznačen time što je β-laktamski antibiotik cefotaksim, cefpodoksim, ceftaz, ceftibuten ili ceftriakson.
19. Spoj namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 14 ili 15, naznačen time što je bakterijska infekcija spolna bolest, pneumonija, komplicirana infekcija mokraćnog sustava, infekcija mokraćnog sustava, komplicirana intraabdominalna infekcija ili intraabdominalna infekcija.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762504523P | 2017-05-10 | 2017-05-10 | |
| US201762551043P | 2017-08-28 | 2017-08-28 | |
| US15/934,497 US10085999B1 (en) | 2017-05-10 | 2018-03-23 | Beta-lactamase inhibitors and uses thereof |
| EP18729223.0A EP3625233B9 (en) | 2017-05-10 | 2018-05-02 | 3-(((((2s,5r)-2-carbamoyl-7-oxo-1,6-diazabicyclo[3.2.1]octan-6-yl)oxy)sulfonyl)oxy)-2,2-dimethylpropanoate derivatives and related compounds as perorally administered profrugs of beta-lactamase inhibitors for treating bacterial infections |
| PCT/US2018/030652 WO2018208557A1 (en) | 2017-05-10 | 2018-05-02 | 3-(((((2s,5r)-2-carbamoyl-7-oxo-1,6-diazabicyclo[3.2.1]octan-6-yl)oxy)sulfonyl)oxy)-2,2-dimethylprop noate derivatives and related compounds as perorally administered profrugs of beta-lactamase inhibitors for treating bacterial infections |
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| Publication Number | Publication Date |
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| HRP20230977T1 true HRP20230977T1 (hr) | 2023-12-08 |
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| HRP20230977TT HRP20230977T1 (hr) | 2017-05-10 | 2018-05-02 | Derivati 3-(((((2s,5r)-2-karbamoil-7-okso-1,6-diazabiciklo[3.2.1]oktan-6- il)oksi)sulfonil)oksi)-2,2-dimetilpropanoata i srodni spojevi kao peroralno primijenjeni predlijekovi inhibitora beta-laktamaze namijenjenih liječenju bakterijskih infekcija |
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| US (5) | US10085999B1 (hr) |
| EP (1) | EP3625233B9 (hr) |
| JP (2) | JP6909924B2 (hr) |
| KR (1) | KR102411517B1 (hr) |
| CN (1) | CN110662746B (hr) |
| AU (2) | AU2018266566B2 (hr) |
| BR (1) | BR112019023598A2 (hr) |
| CA (2) | CA3153583A1 (hr) |
| DK (1) | DK3625233T5 (hr) |
| ES (1) | ES2955871T3 (hr) |
| FI (1) | FI3625233T5 (hr) |
| HR (1) | HRP20230977T1 (hr) |
| HU (1) | HUE062752T2 (hr) |
| IL (2) | IL296379B1 (hr) |
| LT (1) | LT3625233T (hr) |
| MX (2) | MX2019013260A (hr) |
| PL (1) | PL3625233T3 (hr) |
| PT (1) | PT3625233T (hr) |
| RS (1) | RS64547B9 (hr) |
| RU (1) | RU2753401C2 (hr) |
| SG (2) | SG10202102306TA (hr) |
| SI (1) | SI3625233T1 (hr) |
| WO (1) | WO2018208557A1 (hr) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
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| ES2894251T3 (es) | 2016-06-30 | 2022-02-14 | Qpex Biopharma Inc | Derivados de ácido borónico y usos terapéuticos de los mismos |
| US10085999B1 (en) * | 2017-05-10 | 2018-10-02 | Arixa Pharmaceuticals, Inc. | Beta-lactamase inhibitors and uses thereof |
| BR112020006594A2 (pt) * | 2017-10-02 | 2020-12-15 | Arixa Pharmaceuticals, Inc. | Derivados de aztreonam e usos dos mesmos |
| US11180500B2 (en) | 2018-10-01 | 2021-11-23 | Arixa Pharmaceuticals, Inc. | Derivatives of relebactam and uses thereof |
| AU2020237440B2 (en) * | 2019-03-12 | 2022-10-20 | Arixa Pharmaceuticals, Inc. | Crystalline form of an avibactam derivative |
| WO2020219405A1 (en) * | 2019-04-26 | 2020-10-29 | Merck Sharp & Dohme Corp. | Process for the preparation of intermediates useful for making (2s,5r)-7-oxo-n-piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide |
| KR20220054364A (ko) * | 2019-08-29 | 2022-05-02 | 아릭사 파마슈티컬스 인코포레이티드 | 박테리아 감염을 치료하기 위해 경구 투여되는 베타-락탐 항생제 및 아비박탐 유도체의 조합 |
| US20210186983A1 (en) * | 2019-12-20 | 2021-06-24 | Arixa Pharmaceuticals, Inc. | Orally administered combinations of amoxicillin and avibactam derivatives for treating mycobacterial infections |
| CN111943950B (zh) * | 2020-09-10 | 2022-03-29 | 山东安信制药有限公司 | 一种瑞来巴坦的制备方法 |
| BR112023020348A2 (pt) * | 2021-04-05 | 2023-11-21 | Qpex Biopharma Inc | Regimes de dosagem de ceftibuteno |
| CN115448920A (zh) * | 2022-10-14 | 2022-12-09 | 广州楷石医药有限公司 | 一种β-内酰胺酶抑制剂及其应用 |
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