PE20191618A1 - Antibioticos macrociclicos de amplio espectro - Google Patents
Antibioticos macrociclicos de amplio espectroInfo
- Publication number
- PE20191618A1 PE20191618A1 PE2019001675A PE2019001675A PE20191618A1 PE 20191618 A1 PE20191618 A1 PE 20191618A1 PE 2019001675 A PE2019001675 A PE 2019001675A PE 2019001675 A PE2019001675 A PE 2019001675A PE 20191618 A1 PE20191618 A1 PE 20191618A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- independently
- combine
- macrocyclical
- antibiotics
- Prior art date
Links
- 239000003242 anti bacterial agent Substances 0.000 title 1
- 229940088710 antibiotic agent Drugs 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 5
- 150000001875 compounds Chemical class 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 2
- XXJGBENTLXFVFI-UHFFFAOYSA-N 1-amino-methylene Chemical compound N[CH2] XXJGBENTLXFVFI-UHFFFAOYSA-N 0.000 abstract 1
- 241000894006 Bacteria Species 0.000 abstract 1
- 208000035143 Bacterial infection Diseases 0.000 abstract 1
- 230000001580 bacterial effect Effects 0.000 abstract 1
- 208000022362 bacterial infectious disease Diseases 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000001721 carbon Chemical group 0.000 abstract 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- -1 nitro, hydroxyl Chemical group 0.000 abstract 1
- 244000052769 pathogen Species 0.000 abstract 1
- 108090000623 proteins and genes Proteins 0.000 abstract 1
- 102000004169 proteins and genes Human genes 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 108010087967 type I signal peptidase Proteins 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/10—Tetrapeptides
- C07K5/1019—Tetrapeptides with the first amino acid being basic
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/06—Tripeptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/07—Tetrapeptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/08—Peptides having 5 to 11 amino acids
-
- 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
- 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
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D245/00—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms
- C07D245/04—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/10—Tetrapeptides
- C07K5/1002—Tetrapeptides with the first amino acid being neutral
- C07K5/1016—Tetrapeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/04—Linear peptides containing only normal peptide links
- C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
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- 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
Abstract
La presente invencion se refiere a un compuesto de formula (I), en donde R1 y R2 son cada uno independientemente H, alquilo C1-C6, -CH2CH(OH)CH2NH2, entre otros; R3 y R5 son H o - (C1-C6 ) alquilo; R4 es H, -(C1-C6) alquilo, -(C1-C6) alquilo-OH, entre otros; o R3 y R4 se combinan para formar un anillo heterocicloalquilo; o R4 y R5 y el atomo de carbono al que se encuentran unidos forman un anillo ciclopropilo; R6, R7 y R8 son cada uno independientemente H, fluor, entre otros; R9 y R10 son H, - (C1-C6) alquilo, entre otros; R11 y R12 son cada uno independientemente H, -NH2, entre otros; R11 y R18 se combinan para formar un anillo heterocicloalquilo opcionalmente sustituido y R12 es H; R15, R16, R17 y R18 son cada uno independientemente H, - (C1-C6) alquilo, entre otros; X es opcionalmente sustituido -(C1-C6) alquilo-, entre otros; Y es un enlace, -O-, -S-, entre otros; Z es H, halogeno, -NH2, entre otros; R27 y R28 son independientemente halogeno, nitro, hidroxil, entre otros; p y q son 0 a 2; o una sal farmaceuticamente aceptable del mismo. . Dichos compuestos son inhibidores de la peptidasa senal bacteriana de tipo 1 (SpsB), una proteina esencial en bacterias; siendo utiles para tratar infecciones bacterianas cuyos patogenos son resistentes a multiples farmacos. Tambien se refiere a composiciones que los contiene.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2017/073575 | 2017-02-15 | ||
| CNPCT/CN2017/085075 | 2017-05-19 | ||
| PCT/CN2018/076957 WO2018149419A1 (en) | 2017-02-15 | 2018-02-22 | Macrocyclic broad spectrum antibiotics |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20191618A1 true PE20191618A1 (es) | 2019-11-05 |
Family
ID=63169158
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2019001675A PE20191618A1 (es) | 2017-02-15 | 2018-02-22 | Antibioticos macrociclicos de amplio espectro |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US20210198316A9 (es) |
| EP (1) | EP3583096B1 (es) |
| JP (2) | JP7134177B2 (es) |
| KR (1) | KR20190127720A (es) |
| CN (1) | CN110520413B (es) |
| AU (2) | AU2018222093B2 (es) |
| BR (1) | BR112019017003A2 (es) |
| CA (1) | CA3053205A1 (es) |
| CL (1) | CL2019002305A1 (es) |
| CO (1) | CO2019010001A2 (es) |
| CR (2) | CR20190428A (es) |
| IL (1) | IL268483B2 (es) |
| MA (1) | MA47514A (es) |
| MX (2) | MX2019009752A (es) |
| PE (1) | PE20191618A1 (es) |
| PH (1) | PH12019501904A1 (es) |
| SG (2) | SG10202108876TA (es) |
| UA (1) | UA126027C2 (es) |
| WO (1) | WO2018149419A1 (es) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6873993B2 (ja) | 2015-11-20 | 2021-05-19 | アールキューエックス ファーマシューティカルズ，インク． | 大環状広域抗生物質 |
| HRP20231497T1 (hr) | 2019-05-28 | 2024-03-01 | F. Hoffmann-La Roche Ag | Makrociklični antibiotici širokog spektra |
| CN112480007B (zh) * | 2020-12-08 | 2022-11-18 | 宿迁市科莱博生物化学有限公司 | 一种1，3-二甲基-1h-吡唑-4-羧酸的合成方法 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2011224710A1 (en) * | 2010-03-09 | 2012-09-06 | Merck Canada Inc. | Bridged lipoglycopeptides that potentiate the activity of beta-lactam antibacterials |
| RU2013112483A (ru) * | 2010-09-15 | 2014-10-20 | Дзе Скриппс Рисеч Инститьют | Аналоги ариломицина, представляющие собой антибиотики широкого спектра действия |
| WO2012166665A2 (en) * | 2011-05-27 | 2012-12-06 | Rqx Pharmaceuticals, Inc. | Broad spectrum antibiotics |
| CA2867448A1 (en) * | 2012-03-14 | 2013-09-19 | Floyd E. Romesberg | Broad spectrum antibiotic arylomycin analogs |
| WO2014065080A1 (ja) * | 2012-10-23 | 2014-05-01 | 富士電機株式会社 | 半導体装置およびその製造方法 |
| CN103788176A (zh) * | 2012-10-31 | 2014-05-14 | 上海来益生物药物研究开发中心有限责任公司 | 一种arylomycin类化合物及其制备方法和应用 |
| WO2014081886A1 (en) | 2012-11-21 | 2014-05-30 | Rqx Pharmaceuticals, Inc. | Macrocyclic broad spectrum antibiotics |
| US20190067498A1 (en) * | 2017-08-28 | 2019-02-28 | Meng Tao | Light-induced aluminum plating on silicon for solar cell metallization |
| KR20170027721A (ko) * | 2014-05-20 | 2017-03-10 | 알큐엑스 파마슈티컬스, 인크. | 마크로시클릭 광범위 항생제 |
| TWI725075B (zh) * | 2015-11-20 | 2021-04-21 | 美商Ｒｑｘ製藥公司 | 巨環廣效抗生素 |
| JP6873993B2 (ja) * | 2015-11-20 | 2021-05-19 | アールキューエックス ファーマシューティカルズ，インク． | 大環状広域抗生物質 |
| AU2018243724B2 (en) | 2017-03-27 | 2022-07-28 | F. Hoffmann-La Roche Ag | Process for making arylomyin ring analogs |
-
2018
- 2018-02-22 WO PCT/CN2018/076957 patent/WO2018149419A1/en unknown
- 2018-02-22 CN CN201880025278.0A patent/CN110520413B/zh active Active
- 2018-02-22 AU AU2018222093A patent/AU2018222093B2/en active Active
- 2018-02-22 MA MA047514A patent/MA47514A/fr unknown
- 2018-02-22 MX MX2019009752A patent/MX2019009752A/es unknown
- 2018-02-22 SG SG10202108876TA patent/SG10202108876TA/en unknown
- 2018-02-22 CR CR20190428A patent/CR20190428A/es unknown
- 2018-02-22 UA UAA201909231A patent/UA126027C2/uk unknown
- 2018-02-22 CA CA3053205A patent/CA3053205A1/en active Pending
- 2018-02-22 SG SG11201907448RA patent/SG11201907448RA/en unknown
- 2018-02-22 PE PE2019001675A patent/PE20191618A1/es unknown
- 2018-02-22 CR CR20210144A patent/CR20210144A/es unknown
- 2018-02-22 IL IL268483A patent/IL268483B2/en unknown
- 2018-02-22 EP EP18754727.8A patent/EP3583096B1/en active Active
- 2018-02-22 KR KR1020197026779A patent/KR20190127720A/ko active IP Right Grant
- 2018-02-22 BR BR112019017003A patent/BR112019017003A2/pt not_active Application Discontinuation
- 2018-02-22 JP JP2019542369A patent/JP7134177B2/ja active Active
-
2019
- 2019-08-13 US US16/539,947 patent/US20210198316A9/en not_active Abandoned
- 2019-08-14 MX MX2022014485A patent/MX2022014485A/es unknown
- 2019-08-14 CL CL2019002305A patent/CL2019002305A1/es unknown
- 2019-08-15 PH PH12019501904A patent/PH12019501904A1/en unknown
- 2019-09-13 CO CONC2019/0010001A patent/CO2019010001A2/es unknown
-
2022
- 2022-03-11 AU AU2022201724A patent/AU2022201724B9/en active Active
- 2022-08-30 JP JP2022137159A patent/JP7461425B2/ja active Active
- 2022-10-18 US US18/047,624 patent/US20230133667A1/en not_active Abandoned
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