AR093581A1 - Antibioticos macrociclicos de amplio espectro - Google Patents
Antibioticos macrociclicos de amplio espectroInfo
- Publication number
- AR093581A1 AR093581A1 ARP130104303A ARP130104303A AR093581A1 AR 093581 A1 AR093581 A1 AR 093581A1 AR P130104303 A ARP130104303 A AR P130104303A AR P130104303 A ARP130104303 A AR P130104303A AR 093581 A1 AR093581 A1 AR 093581A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- aryl
- independently
- heteroaryl
- Prior art date
Links
- 239000003242 anti bacterial agent Substances 0.000 title 1
- 229940088710 antibiotic agent Drugs 0.000 title 1
- 238000001228 spectrum Methods 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 14
- 125000001072 heteroaryl group Chemical group 0.000 abstract 13
- 125000003118 aryl group Chemical group 0.000 abstract 9
- 125000000623 heterocyclic group Chemical group 0.000 abstract 9
- 229910052739 hydrogen Inorganic materials 0.000 abstract 7
- 239000001257 hydrogen Substances 0.000 abstract 6
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 6
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 5
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 125000003342 alkenyl group Chemical group 0.000 abstract 4
- 125000000304 alkynyl group Chemical group 0.000 abstract 4
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 3
- ZOXJGFHDIHLPTG-UHFFFAOYSA-N Boron Chemical group [B] ZOXJGFHDIHLPTG-UHFFFAOYSA-N 0.000 abstract 3
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 3
- 229910052799 carbon Inorganic materials 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 3
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 3
- 229910052796 boron Inorganic materials 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 150000003254 radicals Chemical class 0.000 abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 abstract 1
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 abstract 1
- 125000006717 (C3-C10) cycloalkenyl group Chemical group 0.000 abstract 1
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 abstract 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 1
- 241000894006 Bacteria Species 0.000 abstract 1
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 1
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 abstract 1
- 125000004423 acyloxy group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 230000001580 bacterial effect Effects 0.000 abstract 1
- 150000001638 boron Chemical class 0.000 abstract 1
- 229910052794 bromium Inorganic materials 0.000 abstract 1
- 239000004202 carbamide Substances 0.000 abstract 1
- 150000001721 carbon Chemical group 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- -1 cyano, hydroxy Chemical group 0.000 abstract 1
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 1
- VILAVOFMIJHSJA-UHFFFAOYSA-N dicarbon monoxide Chemical group [C]=C=O VILAVOFMIJHSJA-UHFFFAOYSA-N 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 125000003051 glycosyloxy group Chemical group 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 229910052740 iodine Inorganic materials 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000004962 physiological condition Effects 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 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
- 239000012453 solvate Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 1
- 125000003107 substituted aryl group Chemical group 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 125000005309 thioalkoxy group Chemical group 0.000 abstract 1
- 108010087967 type I signal peptidase Proteins 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/55—Protease inhibitors
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/10—Antimycotics
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
- C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
-
- 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
- C07K5/081—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing O or S as heteroatoms, e.g. Cys, Ser
-
- 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
- C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- 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
- A61K38/00—Medicinal preparations containing peptides
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Gastroenterology & Hepatology (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Crystallography & Structural Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261729253P | 2012-11-21 | 2012-11-21 | |
| US201261729249P | 2012-11-21 | 2012-11-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR093581A1 true AR093581A1 (es) | 2015-06-10 |
Family
ID=50728492
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP130104303A AR093581A1 (es) | 2012-11-21 | 2013-11-21 | Antibioticos macrociclicos de amplio espectro |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US9309285B2 (OSRAM) |
| EP (1) | EP2922829B1 (OSRAM) |
| JP (2) | JP6437443B2 (OSRAM) |
| KR (1) | KR20150088292A (OSRAM) |
| CN (1) | CN104903302B (OSRAM) |
| AR (1) | AR093581A1 (OSRAM) |
| BR (1) | BR112015011697A2 (OSRAM) |
| CA (1) | CA2892027A1 (OSRAM) |
| EA (1) | EA201590871A1 (OSRAM) |
| MX (1) | MX2015006340A (OSRAM) |
| TW (1) | TWI631127B (OSRAM) |
| WO (1) | WO2014081886A1 (OSRAM) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10501493B2 (en) | 2011-05-27 | 2019-12-10 | Rqx Pharmaceuticals, Inc. | Broad spectrum antibiotics |
| KR102346455B1 (ko) | 2013-03-15 | 2022-01-04 | 더 트러스티스 오브 더 유니버시티 오브 펜실베니아 | Mpsi 치료를 위한 조성물 및 방법 |
| RU2016146581A (ru) * | 2014-05-20 | 2018-06-21 | АрКьюЭкс ФАРМАСЪЮТИКЛС, ИНК. | Макроциклические антибиотики широкого спектра действия |
| AU2016254226C1 (en) * | 2015-04-30 | 2022-11-24 | Idexx Laboratories, Inc. | Methods for detecting renal disease |
| CR20180232A (es) | 2015-10-27 | 2018-05-31 | Hoffmann La Roche | Macrociclos peptídicos contra acinetobacter baumannii |
| EP3377474B1 (en) * | 2015-11-20 | 2023-08-16 | RQX Pharmaceuticals, Inc. | Macrocyclic broad spectrum antibiotics |
| TWI725075B (zh) * | 2015-11-20 | 2021-04-21 | 美商Rqx製藥公司 | 巨環廣效抗生素 |
| IL268483B2 (en) * | 2017-02-15 | 2024-02-01 | Rqx Pharmaceuticals Inc | Macrocyclic broad spectrum antibiotics |
| EP3388444A1 (en) | 2017-04-10 | 2018-10-17 | F. Hoffmann-La Roche AG | Anti-bacterial peptide macrocycles and use thereof |
| US11505573B2 (en) | 2018-03-28 | 2022-11-22 | Hoffmann-La Roche Inc. | Peptide macrocycles against Acinetobacter baumannii |
| US11819532B2 (en) | 2018-04-23 | 2023-11-21 | Hoffmann-La Roche Inc. | Peptide macrocycles against Acinetobacter baumannii |
| IL295889B2 (en) * | 2019-05-28 | 2025-01-01 | Hoffmann La Roche | Broad-spectrum macrocyclic antibiotic |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5204328A (en) | 1990-06-26 | 1993-04-20 | Merck & Co., Inc. | Peptides having atrial natriuretic factor activity |
| EP0895999A1 (en) * | 1997-08-06 | 1999-02-10 | Pfizer Products Inc. | C-4" substituted macrolide antibiotics |
| US6660832B1 (en) * | 1999-08-20 | 2003-12-09 | Isis Pharmaceuticals, Inc. | Macrocyclic compounds and preparation methods thereof |
| US6951840B2 (en) * | 2001-08-31 | 2005-10-04 | Eli Lilly And Company | Lipoglycopeptide antibiotics |
| DE10226921A1 (de) * | 2002-06-17 | 2003-12-24 | Bayer Ag | Antibakterielle Amid-Makrozyklen |
| CA2530063A1 (en) | 2003-06-26 | 2005-01-06 | Migenix Inc. | Compositions of lipopeptide antibiotic derivatives and methods of use thereof |
| DE10358824A1 (de) * | 2003-12-16 | 2005-07-21 | Bayer Healthcare Ag | Antibakterielle Makrozyklen mit substituiertem Biphenyl |
| DE102005014245A1 (de) | 2005-03-30 | 2006-10-05 | Aicuris Gmbh & Co. Kg | Antibakterielle Amid-Makrozyklen V |
| DE102005014247A1 (de) * | 2005-03-30 | 2006-10-05 | Aicuris Gmbh & Co. Kg | Antibakterielle Amid-Makrozyklen VI |
| BR112012021931A2 (pt) * | 2010-03-09 | 2016-05-31 | Merck Canada Inc | composto, composição farmacêutica, método para tratar uma infecção bacteriana, e, uso de composto |
| WO2011120071A1 (en) | 2010-04-01 | 2011-10-06 | The University Of Queensland | Oxytocin peptide analogues |
| KR20130105659A (ko) * | 2010-09-15 | 2013-09-25 | 더 스크립스 리서치 인스티튜트 | 광범위 스펙트럼 항생제 아릴로마이신 유사체 |
| 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 |
-
2013
- 2013-11-20 CA CA2892027A patent/CA2892027A1/en not_active Abandoned
- 2013-11-20 WO PCT/US2013/071093 patent/WO2014081886A1/en not_active Ceased
- 2013-11-20 CN CN201380069987.6A patent/CN104903302B/zh active Active
- 2013-11-20 JP JP2015544117A patent/JP6437443B2/ja active Active
- 2013-11-20 EA EA201590871A patent/EA201590871A1/ru unknown
- 2013-11-20 EP EP13856377.0A patent/EP2922829B1/en active Active
- 2013-11-20 BR BR112015011697A patent/BR112015011697A2/pt not_active Application Discontinuation
- 2013-11-20 MX MX2015006340A patent/MX2015006340A/es unknown
- 2013-11-20 KR KR1020157016534A patent/KR20150088292A/ko not_active Withdrawn
- 2013-11-21 US US14/086,908 patent/US9309285B2/en active Active
- 2013-11-21 AR ARP130104303A patent/AR093581A1/es unknown
- 2013-11-21 TW TW102142527A patent/TWI631127B/zh not_active IP Right Cessation
-
2018
- 2018-07-18 JP JP2018135357A patent/JP6662960B2/ja active Active
Also Published As
| Publication number | Publication date |
|---|---|
| JP2016501864A (ja) | 2016-01-21 |
| CA2892027A1 (en) | 2014-05-30 |
| US20140142029A1 (en) | 2014-05-22 |
| MX2015006340A (es) | 2015-09-07 |
| TWI631127B (zh) | 2018-08-01 |
| CN104903302A (zh) | 2015-09-09 |
| EP2922829A4 (en) | 2016-11-02 |
| US9309285B2 (en) | 2016-04-12 |
| JP6437443B2 (ja) | 2018-12-12 |
| EA201590871A1 (ru) | 2015-11-30 |
| BR112015011697A2 (pt) | 2017-07-11 |
| EP2922829A1 (en) | 2015-09-30 |
| CN104903302B (zh) | 2019-03-29 |
| KR20150088292A (ko) | 2015-07-31 |
| TW201434848A (zh) | 2014-09-16 |
| JP2018184435A (ja) | 2018-11-22 |
| EP2922829B1 (en) | 2021-08-11 |
| WO2014081886A1 (en) | 2014-05-30 |
| JP6662960B2 (ja) | 2020-03-11 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |