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
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- 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)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Gastroenterology & Hepatology (AREA)
- Epidemiology (AREA)
- Crystallography & Structural Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (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)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Actúan por inhibición de la peptidasa de señal (SpsB) del tipo bacteriano 1, una proteína esencial de las bacterias. También se proveen composiciones farmacéuticas y métodos de tratamiento en los que se utilizan los compuestos. Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1) donde: E¹ es alquilo C₁₋₆, alquenilo C₂₋₇, alquinilo C₂₋₇, cicloalquilo C₃₋₇, heterociclilo, heteroarilo, o arilo; E² es alquenilo C₂₋₇, alquinilo C₂₋₇, cicloalquilo C₃₋₇, heterociclilo, heteroarilo, o arilo; L¹ es una unión, -O-, -S-, -NR⁴-, -C(O)-, -CH₂O-, -OCH₂-, -CH₂S-, -SCH₂-, -CH₂NR⁴-, -NR⁴CH₂-, -NR⁴C(O)-, -C(O)NR⁴-, -NR⁴S(O)₂-, -S(O)₂NR⁴-, -NR⁴C(O)NR⁴-, -NR⁴C(O)O-, -OC(O)NR⁴-, o alquileno C₁₋₄ opcionalmente sustituido con OH, CN, NO₂, halógeno, alquilo C₁₋₆; L² es una unión, o alquileno C₁₋₆ opcionalmente sustituido; X es un resto del grupo de fórmulas (2); donde n4, n5 y n6 son en forma independiente entre sí 1, 2 ó 3; n7 es 0, 1 ó 2; R²¹ᵇ y R²²ᵇ son en forma independiente en cada caso hidrógeno, hidroxi, alquilo C₁₋₆, cicloalquilo C₃₋₇, heteroarilo de entre 5 y 7 miembros, heterociclilo de entre 5 y 7 miembros, o arilo C₆₋₁₀, donde cualquier alquilo, cicloalquilo, heterociclilo, arilo o heteroarilo está opcionalmente sustituido entre 1 y 3 J; R²⁵ es H, OH, ORC, un resto del grupo de fórmulas (3), o NR²⁵ᵃR²⁵ᵇ donde R²⁵ᵃ y R²⁵ᵇ son en forma independiente entre sí H, SO₂-alquilo C₁₋₆, o alquilo opcionalmente sustituido; RB¹ y RB² son en forma independiente entre sí H, alquilo C₁₋₆, cicloalquilo C₃₋₆, ORC, C(=O)N(RC)₂, OC(=O)N(RC)₂, C(=O)ORC, OC(=O)ORC, nitro, trifluorometilo, trifluorometoxi, alcoxi C₁₋₆, tioalcoxi C₁₋₆, N(RC)₂, heterociclilo de entre 5 y 7 miembros o heteroarilo de entre 5 y 7 miembros, o arilo C₆₋₁₀; RC es en forma independiente en cada caso H o alquilo C₁₋₆, y una línea ondulada indica el punto de unión de X a un carbono de fórmula (1) que se une a X; o X es CO₂H, CH₂CO₂H, C(=O)NHCH₂C(=O)H, CH₂C(=O)H, C(=O)N(H)CH(R⁷)B(ORB³)(ORB⁴), ó un resto de fórmula (4), donde R⁷ es H, metilo, etilo, o -CH₂OH; o R⁷ y RB³ junto con el átomo de boro forman un anillo de 5 ó 6 miembros que contiene boro; RB³ y RB⁴ son en forma independiente entre sí H, alquilo C₁₋₆, -CH₂CO₂H, -CH₂CH₂CO₂H; o RB³ y RB⁴ junto con el átomo de boro forman un anillo de 5 ó 6 miembros que contiene boro opcionalmente sustituido; R⁵ es arilo, heteroarilo, o una cadena alquilo lineal o ramificada de aproximadamente 1 - 22 átomos de carbono, donde R⁵ se une al carbono de carbonilo al cual se une directamente o por medio de un O ó NR⁴, para dar una unión amida, carbamato, o urea, respectivamente; que opcionalmente comprende dentro de la cadena o en un extremo de la cadena arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, o un resto de fórmula (5) opcionalmente sustituido donde Z es una unión O, S, NH, CH₂ o CºC; R² y R³ son en forma independiente entre sí nitro, halo, ciano, hidroxi, glicosiloxi, amino, alcoxi C₁₋₄, aciloxi C₁₋₄, alquilo C₁₋₄, o un grupo separable bajo condiciones fisiológicas para dar un compuesto de fórmula (1) donde R² o R³ respectivamente es hidroxi, donde cualquier átomo de carbono está opcionalmente sustituido con J; n1 y n2 son en forma independiente 0 ó 1; n3 y n8 son en forma independiente 0, 1, ó 2; cada m es en forma independiente 0 ó 1; R¹ es hidrógeno o alquilo C₁₋₆ opcionalmente sustituido con entre 1 y 3 J; o R¹ junto con E¹ forman un anillo; R⁴, R⁴, y R⁴ son en forma independiente entre sí en cada caso hidrógeno, o alquilo C₁₋₆ opcionalmente sustituido con entre 1 y 3 J; R⁶ es hidrógeno, o alquilo C₁₋₆ opcionalmente sustituido con entre 1 y 3 J; o R⁶ junto con RA⁴ forman un anillo; RA¹, RA¹, RA², RA³, RA³, RA⁴, RA⁴, RA⁷, RA⁷, RA⁸, RA⁸, RA⁹, RA⁹, RA¹⁰, y RA¹⁰ son en forma independiente en cada caso hidrógeno, alquilo C₁₋₆, cicloalquilo C₃₋₇, heteroarilo de entre 5 y 7 miembros, heterociclilo de entre 5 y 7 miembros, o arilo C₆₋₁₀, donde cualquier alquilo, cicloalquilo, heterociclilo, arilo o heteroarilo está opcionalmente sustituido con entre 1 y 3 J; RA⁶ es amino, alquilo C₁₋₆, cicloalquilo C₃₋₇, heteroarilo de entre 5 y 7 miembros, heterociclilo de entre 5 y 7 miembros, o arilo C₆₋₁₀, donde cualquier alquilo, cicloalquilo, heterociclilo, arilo o heteroarilo está opcionalmente sustituido con entre 1 y 3 J; J es halógeno, R, O, CN, CF₃, OCF₃, (CH₂)₀₋ₚN(R)₂, (CH₂)₀₋ₚSR, (CH₂)₀₋ₚS(O)₂R, (CH₂)₀₋ₚS(O)₂N(R)₂, (CH₂)₀₋ₚSO₃R, (CH₂)₀₋ₚC(O)R, (CH₂)₀₋ₚC(O)O, (CH₂)₀₋ₚC(O)N(R)₂, (CH₂)₀₋ₚOC(O)N(R)₂, (CH₂)₀₋ₚNH-C(O)R, (CH₂)₀₋ₚN(R)SO₂R, (CH₂)₀₋ₚN(R)C(O)O, (CH₂)₀₋ₚN(R)C(O)R, (CH₂)₀₋ₚN(R)C(O)N(R)₂, o (CH₂)₀₋ₚC(=NH)N(R)₂, donde p es 4; cada R es en forma independiente en cada caso hidrógeno, alquilo C₁₋₆, alquenilo C₂₋₇, alquinilo C₂₋₇, cicloalquilo C₃₋₁₀, cicloalquenilo C₃₋₁₀, arilo, o heteroarilo donde cualquier alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, arilo o heteroarilo está opcionalmente sustituido con un sustituyente seleccionado entre F, Cl, Br, I, -CN, -NO₂, -OH, -CF₃, -OCF₃, -OCH₃, -NH₂, -N(alquil C₁₋₄)₂-, -NH-alquilo C₁₋₄, alquilo C₁₋₆, cicloalquilo C₃₋₈, o heteroalquilo C₁₋₆; o una sal o un solvato farmacéuticamente aceptables, o una prodroga del mismo.
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 (es) |
| EP (1) | EP2922829B1 (es) |
| JP (2) | JP6437443B2 (es) |
| KR (1) | KR20150088292A (es) |
| CN (1) | CN104903302B (es) |
| AR (1) | AR093581A1 (es) |
| BR (1) | BR112015011697A2 (es) |
| CA (1) | CA2892027A1 (es) |
| EA (1) | EA201590871A1 (es) |
| MX (1) | MX2015006340A (es) |
| TW (1) | TWI631127B (es) |
| WO (1) | WO2014081886A1 (es) |
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 |
| US10137176B2 (en) | 2013-03-15 | 2018-11-27 | The Trustee Of The University Of Pennsylvania | Compositions and methods for treating MPSI |
| RU2016146581A (ru) | 2014-05-20 | 2018-06-21 | АрКьюЭкс ФАРМАСЪЮТИКЛС, ИНК. | Макроциклические антибиотики широкого спектра действия |
| CA2983943A1 (en) * | 2015-04-30 | 2016-11-03 | Idexx Laboratories, Inc. | Methods for detecting renal disease |
| JP7286317B2 (ja) | 2015-10-27 | 2023-06-05 | エフ． ホフマン－ラ ロシュ アーゲー | Ａｃｉｎｅｔｏｂａｃｔｅｒ ｂａｕｍａｎｎｉｉに対するペプチド大環状分子 |
| 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 |
| CR20210144A (es) * | 2017-02-15 | 2021-05-13 | Genentech Inc | ANTOBIÓTICOS MACROCICLICOS DE AMPLIO ESPECTRO (Divisional 2019-0478) |
| 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 |
| ES2961566T3 (es) * | 2019-05-28 | 2024-03-12 | Hoffmann La Roche | Antibióticos macrocíclicos de amplio espectro |
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 |
| EP1656390A2 (en) | 2003-07-17 | 2006-05-17 | 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 |
| MX2012010381A (es) * | 2010-03-09 | 2012-11-23 | Merck Canada Inc | Lipoglicopeptidos en puente que potencian la actividad de antibacterianos de beta-lactama. |
| US20130130985A1 (en) | 2010-04-01 | 2013-05-23 | Paul Alewood | Oxytocin peptide analogues |
| CN103209700A (zh) * | 2010-09-15 | 2013-07-17 | 斯克里普斯研究所 | 广谱抗生素Arylomycin类似物 |
| TWI642684B (zh) | 2011-05-27 | 2018-12-01 | Ｒｑｘ製藥股份有限公司 | 廣效性抗生素 |
| KR20140140580A (ko) | 2012-03-14 | 2014-12-09 | 더 스크립스 리서치 인스티튜트 | 광범위 항생제 아릴로마이신 유사체 |
-
2013
- 2013-11-20 JP JP2015544117A patent/JP6437443B2/ja active Active
- 2013-11-20 EP EP13856377.0A patent/EP2922829B1/en active Active
- 2013-11-20 EA EA201590871A patent/EA201590871A1/ru unknown
- 2013-11-20 CA CA2892027A patent/CA2892027A1/en not_active Abandoned
- 2013-11-20 BR BR112015011697A patent/BR112015011697A2/pt not_active Application Discontinuation
- 2013-11-20 WO PCT/US2013/071093 patent/WO2014081886A1/en not_active Ceased
- 2013-11-20 MX MX2015006340A patent/MX2015006340A/es unknown
- 2013-11-20 CN CN201380069987.6A patent/CN104903302B/zh active Active
- 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 |
|---|---|
| JP6437443B2 (ja) | 2018-12-12 |
| MX2015006340A (es) | 2015-09-07 |
| EP2922829B1 (en) | 2021-08-11 |
| CN104903302B (zh) | 2019-03-29 |
| TWI631127B (zh) | 2018-08-01 |
| TW201434848A (zh) | 2014-09-16 |
| CN104903302A (zh) | 2015-09-09 |
| US20140142029A1 (en) | 2014-05-22 |
| BR112015011697A2 (pt) | 2017-07-11 |
| EP2922829A1 (en) | 2015-09-30 |
| CA2892027A1 (en) | 2014-05-30 |
| WO2014081886A1 (en) | 2014-05-30 |
| US9309285B2 (en) | 2016-04-12 |
| JP2016501864A (ja) | 2016-01-21 |
| JP6662960B2 (ja) | 2020-03-11 |
| EP2922829A4 (en) | 2016-11-02 |
| EA201590871A1 (ru) | 2015-11-30 |
| KR20150088292A (ko) | 2015-07-31 |
| JP2018184435A (ja) | 2018-11-22 |
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