RU2017133660A - Новые гетероциклические соединения и их применение в профилактике или лечении бактериальных инфекций - Google Patents
Новые гетероциклические соединения и их применение в профилактике или лечении бактериальных инфекций Download PDFInfo
- Publication number
- RU2017133660A RU2017133660A RU2017133660A RU2017133660A RU2017133660A RU 2017133660 A RU2017133660 A RU 2017133660A RU 2017133660 A RU2017133660 A RU 2017133660A RU 2017133660 A RU2017133660 A RU 2017133660A RU 2017133660 A RU2017133660 A RU 2017133660A
- Authority
- RU
- Russia
- Prior art keywords
- nhq
- nhc
- heterocycle
- substituents
- saturated
- Prior art date
Links
- 208000035143 Bacterial infection Diseases 0.000 title claims 4
- 208000022362 bacterial infectious disease Diseases 0.000 title claims 4
- 230000002265 prevention Effects 0.000 title claims 3
- 150000002391 heterocyclic compounds Chemical class 0.000 title 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 39
- 125000005842 heteroatom Chemical group 0.000 claims 25
- 229920006395 saturated elastomer Polymers 0.000 claims 21
- 125000003118 aryl group Chemical group 0.000 claims 19
- 150000001875 compounds Chemical class 0.000 claims 18
- 229910052757 nitrogen Inorganic materials 0.000 claims 18
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 18
- 229910052717 sulfur Inorganic materials 0.000 claims 17
- 125000001424 substituent group Chemical group 0.000 claims 15
- 229910052799 carbon Inorganic materials 0.000 claims 10
- 125000004432 carbon atom Chemical group C* 0.000 claims 10
- 229910052760 oxygen Inorganic materials 0.000 claims 8
- 125000000217 alkyl group Chemical group 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 239000003242 anti bacterial agent Substances 0.000 claims 6
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 6
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 4
- 241000894006 Bacteria Species 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 150000003952 β-lactams Chemical class 0.000 claims 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 125000002619 bicyclic group Chemical group 0.000 claims 2
- ORFOPKXBNMVMKC-DWVKKRMSSA-N ceftazidime Chemical compound S([C@@H]1[C@@H](C(N1C=1C([O-])=O)=O)NC(=O)\C(=N/OC(C)(C)C(O)=O)C=2N=C(N)SC=2)CC=1C[N+]1=CC=CC=C1 ORFOPKXBNMVMKC-DWVKKRMSSA-N 0.000 claims 2
- 229960000484 ceftazidime Drugs 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 125000005348 fluorocycloalkyl group Chemical group 0.000 claims 2
- 125000002950 monocyclic group Chemical group 0.000 claims 2
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims 2
- IZXIZTKNFFYFOF-UHFFFAOYSA-N 2-Oxazolidone Chemical class O=C1NCCO1 IZXIZTKNFFYFOF-UHFFFAOYSA-N 0.000 claims 1
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- 108020004256 Beta-lactamase Proteins 0.000 claims 1
- 229930186147 Cephalosporin Natural products 0.000 claims 1
- 241000192125 Firmicutes Species 0.000 claims 1
- 108010015899 Glycopeptides Proteins 0.000 claims 1
- 102000002068 Glycopeptides Human genes 0.000 claims 1
- 108010028921 Lipopeptides Proteins 0.000 claims 1
- 229930182555 Penicillin Natural products 0.000 claims 1
- 108010040201 Polymyxins Proteins 0.000 claims 1
- 108010034396 Streptogramins Proteins 0.000 claims 1
- 239000004098 Tetracycline Substances 0.000 claims 1
- 229940126575 aminoglycoside Drugs 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
- 239000003781 beta lactamase inhibitor Substances 0.000 claims 1
- 102000006635 beta-lactamase Human genes 0.000 claims 1
- 229940126813 beta-lactamase inhibitor Drugs 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 229940041011 carbapenems Drugs 0.000 claims 1
- 229940124587 cephalosporin Drugs 0.000 claims 1
- 150000001780 cephalosporins Chemical class 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940124307 fluoroquinolone Drugs 0.000 claims 1
- YMAWOPBAYDPSLA-UHFFFAOYSA-N glycylglycine Chemical class [NH3+]CC(=O)NCC([O-])=O YMAWOPBAYDPSLA-UHFFFAOYSA-N 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000003835 ketolide antibiotic agent Substances 0.000 claims 1
- 239000003120 macrolide antibiotic agent Substances 0.000 claims 1
- 229940041033 macrolides Drugs 0.000 claims 1
- 229940126601 medicinal product Drugs 0.000 claims 1
- 229940041009 monobactams Drugs 0.000 claims 1
- 230000003287 optical effect Effects 0.000 claims 1
- 150000002961 penems Chemical class 0.000 claims 1
- 150000002960 penicillins Chemical class 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 229940041153 polymyxins Drugs 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 150000007660 quinolones Chemical class 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 229940041030 streptogramins Drugs 0.000 claims 1
- 125000004434 sulfur atom Chemical group 0.000 claims 1
- ILMRJRBKQSSXGY-UHFFFAOYSA-N tert-butyl(dimethyl)silicon Chemical compound C[Si](C)C(C)(C)C ILMRJRBKQSSXGY-UHFFFAOYSA-N 0.000 claims 1
- 125000001981 tert-butyldimethylsilyl group Chemical group [H]C([H])([H])[Si]([H])(C([H])([H])[H])[*]C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 150000003512 tertiary amines Chemical class 0.000 claims 1
- 235000019364 tetracycline Nutrition 0.000 claims 1
- 150000003522 tetracyclines Chemical class 0.000 claims 1
- 229940040944 tetracyclines Drugs 0.000 claims 1
- 229940126085 β‑Lactamase Inhibitor Drugs 0.000 claims 1
Classifications
-
- 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
- A61K31/435—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
- A61K31/495—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
- A61K31/529—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim forming part of bridged ring 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
- A61K31/54—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Communicable Diseases (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15305473.9 | 2015-03-31 | ||
| EP15305473.9A EP3075733A1 (en) | 2015-03-31 | 2015-03-31 | Novel heterocyclic compounds and their use in preventing or treating bacterial infections |
| EP16305073 | 2016-01-26 | ||
| EP16305073.5 | 2016-01-26 | ||
| PCT/EP2016/056847 WO2016156348A1 (en) | 2015-03-31 | 2016-03-30 | Novel heterocyclic compounds and their use in preventing or treating bacterial infections |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2017133660A true RU2017133660A (ru) | 2019-03-28 |
| RU2017133660A3 RU2017133660A3 (enExample) | 2019-08-22 |
Family
ID=55642467
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2017133660A RU2017133660A (ru) | 2015-03-31 | 2016-03-30 | Новые гетероциклические соединения и их применение в профилактике или лечении бактериальных инфекций |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US10072006B2 (enExample) |
| EP (1) | EP3277686B1 (enExample) |
| JP (1) | JP2018510202A (enExample) |
| KR (1) | KR20170132301A (enExample) |
| CN (1) | CN107531708A (enExample) |
| AU (1) | AU2016239209A1 (enExample) |
| BR (1) | BR112017020796A2 (enExample) |
| CA (1) | CA2980085A1 (enExample) |
| CL (1) | CL2017002451A1 (enExample) |
| MX (1) | MX2017012535A (enExample) |
| RU (1) | RU2017133660A (enExample) |
| TW (1) | TW201643164A (enExample) |
| WO (1) | WO2016156348A1 (enExample) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10183943B2 (en) * | 2015-05-07 | 2019-01-22 | Mutabilis | Heterocyclic compounds and their use in preventing or treating bacterial infections |
| PT3512851T (pt) * | 2016-09-16 | 2022-10-11 | Entasis Therapeutics Ltd | Compostos inibidores de beta-lactamase |
| 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 |
| 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 |
| IL280770B2 (en) | 2018-08-09 | 2024-05-01 | Antabio Sas | Diazabicyclooctanones as inhibitors of serine beta-lactamases |
| CN109942579B (zh) * | 2019-04-18 | 2021-06-22 | 成都千禧莱医药科技有限公司 | β-内酰胺酶抑制剂含脲双环化合物及其制备方法和应用 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2936798B1 (fr) | 2008-10-03 | 2012-09-28 | Novexel | Nouveaux composes heterocycliques azotes, leur preparation et leur utilisation comme medicaments antibacteriens. |
| AR090539A1 (es) | 2012-04-02 | 2014-11-19 | Astrazeneca Ab | COMPUESTOS INHIBIDORES DE b LACTAMASA |
| WO2014141132A1 (en) * | 2013-03-14 | 2014-09-18 | Naeja Pharmaceutical Inc. | NEW HETEROCYCLIC COMPOUNDS AND THEIR USE AS ANTIBACTERIAL AGENTS AND β-LACTAMASE INHIBITORS |
-
2016
- 2016-03-30 TW TW105110140A patent/TW201643164A/zh unknown
- 2016-03-30 RU RU2017133660A patent/RU2017133660A/ru not_active Application Discontinuation
- 2016-03-30 EP EP16712867.7A patent/EP3277686B1/en active Active
- 2016-03-30 AU AU2016239209A patent/AU2016239209A1/en not_active Abandoned
- 2016-03-30 MX MX2017012535A patent/MX2017012535A/es unknown
- 2016-03-30 CN CN201680019934.7A patent/CN107531708A/zh active Pending
- 2016-03-30 BR BR112017020796-6A patent/BR112017020796A2/pt not_active Application Discontinuation
- 2016-03-30 KR KR1020177031505A patent/KR20170132301A/ko not_active Withdrawn
- 2016-03-30 JP JP2017551710A patent/JP2018510202A/ja active Pending
- 2016-03-30 WO PCT/EP2016/056847 patent/WO2016156348A1/en not_active Ceased
- 2016-03-30 CA CA2980085A patent/CA2980085A1/en not_active Abandoned
- 2016-03-30 US US15/563,519 patent/US10072006B2/en active Active
-
2017
- 2017-09-28 CL CL2017002451A patent/CL2017002451A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2016239209A1 (en) | 2017-10-12 |
| CA2980085A1 (en) | 2016-10-06 |
| RU2017133660A3 (enExample) | 2019-08-22 |
| US20180086761A1 (en) | 2018-03-29 |
| EP3277686A1 (en) | 2018-02-07 |
| CN107531708A (zh) | 2018-01-02 |
| TW201643164A (zh) | 2016-12-16 |
| US10072006B2 (en) | 2018-09-11 |
| WO2016156348A1 (en) | 2016-10-06 |
| EP3277686B1 (en) | 2020-07-22 |
| JP2018510202A (ja) | 2018-04-12 |
| MX2017012535A (es) | 2018-07-06 |
| BR112017020796A2 (pt) | 2018-06-26 |
| KR20170132301A (ko) | 2017-12-01 |
| CL2017002451A1 (es) | 2018-04-20 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20200730 |