JP2019055968A5 - - Google Patents
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- JP2019055968A5 JP2019055968A5 JP2018214091A JP2018214091A JP2019055968A5 JP 2019055968 A5 JP2019055968 A5 JP 2019055968A5 JP 2018214091 A JP2018214091 A JP 2018214091A JP 2018214091 A JP2018214091 A JP 2018214091A JP 2019055968 A5 JP2019055968 A5 JP 2019055968A5
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- JP
- Japan
- Prior art keywords
- optionally substituted
- salt
- alkyl
- hydrogen
- compound according
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims 63
- 150000003839 salts Chemical class 0.000 claims 62
- 229910052739 hydrogen Inorganic materials 0.000 claims 52
- 239000001257 hydrogen Substances 0.000 claims 52
- 125000000547 substituted alkyl group Chemical group 0.000 claims 50
- 125000000623 heterocyclic group Chemical group 0.000 claims 46
- 125000001072 heteroaryl group Chemical group 0.000 claims 41
- 150000002431 hydrogen Chemical group 0.000 claims 39
- 125000004452 carbocyclyl group Chemical group 0.000 claims 37
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 37
- 125000003107 substituted aryl group Chemical group 0.000 claims 36
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 34
- 150000003573 thiols Chemical class 0.000 claims 13
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 12
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 12
- 229910052736 halogen Inorganic materials 0.000 claims 12
- 150000002367 halogens Chemical group 0.000 claims 12
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 12
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 9
- 125000001181 organosilyl group Chemical group [SiH3]* 0.000 claims 9
- 239000008194 pharmaceutical composition Substances 0.000 claims 9
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 8
- 229910052757 nitrogen Inorganic materials 0.000 claims 8
- -1 amino, substituted Amino Chemical group 0.000 claims 7
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 7
- 208000015181 infectious disease Diseases 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 208000035143 Bacterial infection Diseases 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 5
- 125000003710 aryl alkyl group Chemical group 0.000 claims 4
- 208000022362 bacterial infectious disease Diseases 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 3
- 208000035473 Communicable disease Diseases 0.000 claims 3
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 3
- LCIYFINKFGDAHD-UHFFFAOYSA-N azepane;3-nitrobenzoic acid Chemical compound C1CCCNCC1.OC(=O)C1=CC=CC([N+]([O-])=O)=C1 LCIYFINKFGDAHD-UHFFFAOYSA-N 0.000 claims 3
- 150000001720 carbohydrates Chemical class 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 229910052731 fluorine Inorganic materials 0.000 claims 3
- 239000011737 fluorine Substances 0.000 claims 3
- 125000004475 heteroaralkyl group Chemical group 0.000 claims 3
- 239000001301 oxygen Substances 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000001188 haloalkyl group Chemical group 0.000 claims 2
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 2
- 229920002554 vinyl polymer Polymers 0.000 claims 2
- 125000006706 (C3-C6) carbocyclyl group Chemical group 0.000 claims 1
- 206010060976 Bacillus infection Diseases 0.000 claims 1
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims 1
- 206010061126 Escherichia infection Diseases 0.000 claims 1
- 206010061190 Haemophilus infection Diseases 0.000 claims 1
- 208000030852 Parasitic disease Diseases 0.000 claims 1
- 206010035664 Pneumonia Diseases 0.000 claims 1
- 241000191940 Staphylococcus Species 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000004450 alkenylene group Chemical group 0.000 claims 1
- 229940100198 alkylating agent Drugs 0.000 claims 1
- 239000002168 alkylating agent Substances 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 125000004419 alkynylene group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 150000005676 cyclic carbonates Chemical class 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 208000027096 gram-negative bacterial infections Diseases 0.000 claims 1
- 230000002140 halogenating effect Effects 0.000 claims 1
- 125000004474 heteroalkylene group Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 230000002458 infectious effect Effects 0.000 claims 1
- 230000004968 inflammatory condition Effects 0.000 claims 1
- 125000005647 linker group Chemical group 0.000 claims 1
- 125000000466 oxiranyl group Chemical group 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361808441P | 2013-04-04 | 2013-04-04 | |
| US61/808,441 | 2013-04-04 | ||
| US201361832639P | 2013-06-07 | 2013-06-07 | |
| US61/832,639 | 2013-06-07 | ||
| US201461946604P | 2014-02-28 | 2014-02-28 | |
| US61/946,604 | 2014-02-28 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016506660A Division JP6437523B2 (ja) | 2013-04-04 | 2014-04-04 | マクロライドならびにそれらの調製および使用の方法 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020088633A Division JP7111381B2 (ja) | 2013-04-04 | 2020-05-21 | マクロライドならびにそれらの調製および使用の方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019055968A JP2019055968A (ja) | 2019-04-11 |
| JP2019055968A5 true JP2019055968A5 (enExample) | 2019-06-20 |
| JP6850783B2 JP6850783B2 (ja) | 2021-03-31 |
Family
ID=51659360
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016506660A Active JP6437523B2 (ja) | 2013-04-04 | 2014-04-04 | マクロライドならびにそれらの調製および使用の方法 |
| JP2018214091A Active JP6850783B2 (ja) | 2013-04-04 | 2018-11-14 | マクロライドならびにそれらの調製および使用の方法 |
| JP2020088633A Active JP7111381B2 (ja) | 2013-04-04 | 2020-05-21 | マクロライドならびにそれらの調製および使用の方法 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016506660A Active JP6437523B2 (ja) | 2013-04-04 | 2014-04-04 | マクロライドならびにそれらの調製および使用の方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020088633A Active JP7111381B2 (ja) | 2013-04-04 | 2020-05-21 | マクロライドならびにそれらの調製および使用の方法 |
Country Status (11)
| Country | Link |
|---|---|
| US (3) | US9982005B2 (enExample) |
| EP (2) | EP4095146A1 (enExample) |
| JP (3) | JP6437523B2 (enExample) |
| KR (2) | KR102528984B1 (enExample) |
| CN (2) | CN105246334A (enExample) |
| AU (3) | AU2014248014B2 (enExample) |
| BR (1) | BR112015025159A2 (enExample) |
| CA (2) | CA2908575C (enExample) |
| IL (1) | IL241878B (enExample) |
| MX (2) | MX377459B (enExample) |
| WO (1) | WO2014165792A2 (enExample) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2008316830B2 (en) | 2007-10-25 | 2016-03-17 | Cempra Pharmaceuticals, Inc. | Process for the preparation of macrolide antibacterial agents |
| US9072759B2 (en) | 2008-10-24 | 2015-07-07 | Cempra Pharmaceuticals, Inc. | Biodefenses using triazole-containing macrolides |
| US9937194B1 (en) | 2009-06-12 | 2018-04-10 | Cempra Pharmaceuticals, Inc. | Compounds and methods for treating inflammatory diseases |
| ES2608285T3 (es) | 2009-09-10 | 2017-04-07 | Cempra Pharmaceuticals, Inc. | Procedimientos para el tratamiento de paludismo, tuberculosis y enfermedades por MAC |
| WO2012034058A1 (en) | 2010-09-10 | 2012-03-15 | Cempra Pharmaceuticals, Inc. | Hydrogen bond forming fluoro ketolides for treating diseases |
| IN2014DN08939A (enExample) | 2012-03-27 | 2015-05-22 | Cempra Pharmaceuticals Inc | |
| CN105163785A (zh) | 2013-03-14 | 2015-12-16 | 森普拉制药公司 | 用于治疗呼吸道疾病的方法及其制剂 |
| RU2015138797A (ru) | 2013-03-15 | 2017-04-24 | Семпра Фармасьютикалс, Инк. | Конвергентные способы получения макролидных антибактериальных агентов |
| MX377459B (es) | 2013-04-04 | 2025-03-10 | Harvard College | Macrolidos y metodos para su preparacion y uso. |
| CN105764491A (zh) | 2013-12-09 | 2016-07-13 | 度瑞公司 | 药物活性剂复合物、聚合物复合物,以及包括其的组合物和方法 |
| WO2016057798A1 (en) | 2014-10-08 | 2016-04-14 | President And Fellows Of Harvard College | 14-membered ketolides and methods of their preparation and use |
| MX2017011454A (es) * | 2015-03-06 | 2018-01-23 | Cempra Pharmaceuticals Inc | Procesos para preparar fluorocetólidos. |
| CN107530365A (zh) * | 2015-03-25 | 2018-01-02 | 哈佛大学的校长及成员们 | 具有修饰的脱氧糖胺糖的大环内酯及其用途 |
| CN107531737A (zh) * | 2015-03-25 | 2018-01-02 | 哈佛大学的校长及成员们 | 脱氧糖胺的合成 |
| GB201608236D0 (en) * | 2016-05-11 | 2016-06-22 | Fidelta D O O | Seco macrolide compounds |
| BR112019017223A2 (pt) * | 2017-02-17 | 2020-04-14 | Cempra Pharmaceuticals Inc | macrolídeos contendo triazol e seus usos oftálmicos |
| WO2018201076A2 (en) | 2017-04-28 | 2018-11-01 | Macrolide Pharmaceuticals Inc. | Macrolides with modified desosamine sugars and uses thereof |
| US20220177508A1 (en) * | 2018-11-19 | 2022-06-09 | Zikani Therapeutics, Inc. | C10-Cyclic Substituted 13-Membered Macrolides and Uses Thereof |
| IL283194B2 (en) | 2018-11-19 | 2025-03-01 | Zikani Therapeutics Inc | C10-alkylene substituted 13-membered macrolides and uses thereof |
| CN114591286B (zh) * | 2021-04-12 | 2023-05-23 | 南京大学 | 新型大环内酯化合物acautalides A-C及其制备方法和应用 |
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