JP6757402B2 - ピラジノ［２，３−ｂ］［１，４］オキサジン−３−オン又は関連する環系を含む抗菌剤 - Google Patents
ピラジノ［２，３−ｂ］［１，４］オキサジン−３−オン又は関連する環系を含む抗菌剤 Download PDFInfo
- Publication number
- JP6757402B2 JP6757402B2 JP2018507672A JP2018507672A JP6757402B2 JP 6757402 B2 JP6757402 B2 JP 6757402B2 JP 2018507672 A JP2018507672 A JP 2018507672A JP 2018507672 A JP2018507672 A JP 2018507672A JP 6757402 B2 JP6757402 B2 JP 6757402B2
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- amino
- pyrazino
- fluoro
- alkyl
- Prior art date
- Legal status (The legal status 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 status listed.)
- Expired - Fee Related
Links
- 0 CCNN*C1CC=CCC1 Chemical compound CCNN*C1CC=CCC1 0.000 description 3
- AAAXKCNHSKMIGM-UHFFFAOYSA-N COC(c(c(Br)n1)nc(N2)c1SCC2=O)=O Chemical compound COC(c(c(Br)n1)nc(N2)c1SCC2=O)=O AAAXKCNHSKMIGM-UHFFFAOYSA-N 0.000 description 2
- PKBLSVRHRRJQPQ-HDJSIYSDSA-N COc1cnc(ccc(F)c2CN[C@H](CC3)CC[C@@H]3NCc(cn3)nc(N4)c3OCC4=O)c2n1 Chemical compound COc1cnc(ccc(F)c2CN[C@H](CC3)CC[C@@H]3NCc(cn3)nc(N4)c3OCC4=O)c2n1 PKBLSVRHRRJQPQ-HDJSIYSDSA-N 0.000 description 2
- AETOSEGDBPUISS-UHFFFAOYSA-N C=Cc(nc1N2)cnc1OCC2=O Chemical compound C=Cc(nc1N2)cnc1OCC2=O AETOSEGDBPUISS-UHFFFAOYSA-N 0.000 description 1
- XNWGOMZFJDMOBK-UHFFFAOYSA-N CC(C)(C)OC(NC(CC1)CCC1N(Cc(c(F)ccc1nc2)c1nc2OC)Cc(c1c(cc2)ncc(OC)n1)c2F)=O Chemical compound CC(C)(C)OC(NC(CC1)CCC1N(Cc(c(F)ccc1nc2)c1nc2OC)Cc(c1c(cc2)ncc(OC)n1)c2F)=O XNWGOMZFJDMOBK-UHFFFAOYSA-N 0.000 description 1
- YPLPXRXMYSTYOX-CIUDSAMLSA-N CC(C)(C)OC(N[C@@H](CC[C@@H]1N)C[C@@H]1O)=O Chemical compound CC(C)(C)OC(N[C@@H](CC[C@@H]1N)C[C@@H]1O)=O YPLPXRXMYSTYOX-CIUDSAMLSA-N 0.000 description 1
- YPLPXRXMYSTYOX-IWSPIJDZSA-N CC(C)(C)OC(N[C@H](CC[C@H]1N)C[C@H]1O)=O Chemical compound CC(C)(C)OC(N[C@H](CC[C@H]1N)C[C@H]1O)=O YPLPXRXMYSTYOX-IWSPIJDZSA-N 0.000 description 1
- VMLVROAZOLUKIS-VMGRFDJRSA-N CC(C)(C)OC(N[C@H](CC[C@H]1NCc(c2nc(OC)cnc2cc2)c2F)C[C@@H]1O)=O Chemical compound CC(C)(C)OC(N[C@H](CC[C@H]1NCc(c2nc(OC)cnc2cc2)c2F)C[C@@H]1O)=O VMLVROAZOLUKIS-VMGRFDJRSA-N 0.000 description 1
- GXAISKGVBYUPHZ-MHYOXFMBSA-N CC1C(F)=C(CN[C@H](CC[C@H](C2)NCc(cn3)nc(N4)c3OCC4=O)[C@H]2O)c2nc(OC)cnc2C1 Chemical compound CC1C(F)=C(CN[C@H](CC[C@H](C2)NCc(cn3)nc(N4)c3OCC4=O)[C@H]2O)c2nc(OC)cnc2C1 GXAISKGVBYUPHZ-MHYOXFMBSA-N 0.000 description 1
- HLQYEZYBXZTEMZ-QWHCGFSZSA-N COc(cc1)nc(N2CCN(C[C@@H]3CN)C[C@H]3O)c1C=CC2=O Chemical compound COc(cc1)nc(N2CCN(C[C@@H]3CN)C[C@H]3O)c1C=CC2=O HLQYEZYBXZTEMZ-QWHCGFSZSA-N 0.000 description 1
- SQPUCRXQIOGFJZ-OMOCHNIRSA-N COc1ccc(C=CC(N2CCN(CC3CNCc(nc4N5)cnc4SCC5=O)C[C@H]3O)=O)c2n1 Chemical compound COc1ccc(C=CC(N2CCN(CC3CNCc(nc4N5)cnc4SCC5=O)C[C@H]3O)=O)c2n1 SQPUCRXQIOGFJZ-OMOCHNIRSA-N 0.000 description 1
- SMHFUWABTJHONP-UHFFFAOYSA-N COc1cnc(ccc(F)c2C=O)c2n1 Chemical compound COc1cnc(ccc(F)c2C=O)c2n1 SMHFUWABTJHONP-UHFFFAOYSA-N 0.000 description 1
- BVVCQALGKDETNB-IUPBHXKESA-N COc1cnc(ccc(F)c2CN[C@H](CC[C@H](C3)N)[C@H]3O)c2n1 Chemical compound COc1cnc(ccc(F)c2CN[C@H](CC[C@H](C3)N)[C@H]3O)c2n1 BVVCQALGKDETNB-IUPBHXKESA-N 0.000 description 1
- ZWJBYHFOIVOXPL-NJAPINKUSA-N COc1cnc(ccc(F)c2CN[C@H](CC[C@H](C3)NCc(cn4)nc(N5)c4OCC5=O)[C@H]3O)c2n1 Chemical compound COc1cnc(ccc(F)c2CN[C@H](CC[C@H](C3)NCc(cn4)nc(N5)c4OCC5=O)[C@H]3O)c2n1 ZWJBYHFOIVOXPL-NJAPINKUSA-N 0.000 description 1
- JTPXVCKCLBROOJ-UHFFFAOYSA-N Nc1cncc(Cl)n1 Chemical compound Nc1cncc(Cl)n1 JTPXVCKCLBROOJ-UHFFFAOYSA-N 0.000 description 1
- BZTYGYDSIJOIJQ-UHFFFAOYSA-N O=C1Nc2nc(Cl)cnc2OC1 Chemical compound O=C1Nc2nc(Cl)cnc2OC1 BZTYGYDSIJOIJQ-UHFFFAOYSA-N 0.000 description 1
- AXVPMSMOPJYOCS-UHFFFAOYSA-N O=Cc(nc1N2)cnc1OCC2=O Chemical compound O=Cc(nc1N2)cnc1OCC2=O AXVPMSMOPJYOCS-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed 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
- A61K31/535—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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/007—Pulmonary tract; Aromatherapy
- A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
- A61K9/0075—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
- A61K9/127—Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic 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
- C07D513/02—Heterocyclic 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
- C07D513/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Communicable Diseases (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Dispersion Chemistry (AREA)
- Otolaryngology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562205732P | 2015-08-16 | 2015-08-16 | |
| US62/205,732 | 2015-08-16 | ||
| US201662308928P | 2016-03-16 | 2016-03-16 | |
| US62/308,928 | 2016-03-16 | ||
| PCT/IB2016/054890 WO2017029602A2 (en) | 2015-08-16 | 2016-08-15 | Compounds for use in antibacterial applications |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018523675A JP2018523675A (ja) | 2018-08-23 |
| JP2018523675A5 JP2018523675A5 (enExample) | 2019-09-26 |
| JP6757402B2 true JP6757402B2 (ja) | 2020-09-16 |
Family
ID=57218948
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018507672A Expired - Fee Related JP6757402B2 (ja) | 2015-08-16 | 2016-08-15 | ピラジノ［２，３−ｂ］［１，４］オキサジン−３−オン又は関連する環系を含む抗菌剤 |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US10364254B2 (enExample) |
| EP (1) | EP3334739A2 (enExample) |
| JP (1) | JP6757402B2 (enExample) |
| KR (1) | KR20180038046A (enExample) |
| CN (1) | CN108137616B (enExample) |
| AU (2) | AU2016307969C1 (enExample) |
| CA (1) | CA2995715A1 (enExample) |
| CL (1) | CL2018000403A1 (enExample) |
| CO (1) | CO2018002204A2 (enExample) |
| CR (1) | CR20180111A (enExample) |
| DO (1) | DOP2018000049A (enExample) |
| EA (1) | EA033314B1 (enExample) |
| HK (1) | HK1248680A1 (enExample) |
| IL (1) | IL257265B (enExample) |
| MA (1) | MA42621A (enExample) |
| MX (1) | MX2018002033A (enExample) |
| PE (1) | PE20181143A1 (enExample) |
| PH (1) | PH12018500358A1 (enExample) |
| TW (1) | TW201722965A (enExample) |
| UY (1) | UY36851A (enExample) |
| WO (1) | WO2017029602A2 (enExample) |
| ZA (1) | ZA201800722B (enExample) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UY36851A (es) * | 2015-08-16 | 2017-03-31 | Glaxosmithkline Ip Dev Ltd | Compuestos para uso en aplicaciones antibacterianas |
| WO2019180634A1 (en) | 2018-03-23 | 2019-09-26 | Glaxosmithkline Intellectual Property Development Limited | Synthesis of oxazinone-containing bicyclic aromatic and heteroaromatic aldehydes |
| TW202116782A (zh) | 2019-07-16 | 2021-05-01 | 瑞士商愛杜西亞製藥有限公司 | 喹啉酮衍生物 |
| CN111269247B (zh) * | 2020-03-04 | 2020-11-24 | 河南科技大学第一附属医院 | 具有抑制大肠杆菌作用的噻嗪酮药物分子的制备方法 |
| US20250214980A1 (en) | 2022-03-14 | 2025-07-03 | Slap Pharmaceuticals Llc | Multicyclic compounds |
| IL328905A (en) | 2023-12-21 | 2026-08-01 | Glaxosmithkline Intellectual Property No 4 Ltd | Chemical compounds and their uses |
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| US5827533A (en) | 1997-02-06 | 1998-10-27 | Duke University | Liposomes containing active agents aggregated with lipid surfactants |
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