CN111163774A - 细菌外排泵抑制剂 - Google Patents
细菌外排泵抑制剂 Download PDFInfo
- Publication number
- CN111163774A CN111163774A CN201880045566.2A CN201880045566A CN111163774A CN 111163774 A CN111163774 A CN 111163774A CN 201880045566 A CN201880045566 A CN 201880045566A CN 111163774 A CN111163774 A CN 111163774A
- Authority
- CN
- China
- Prior art keywords
- alkyl
- carbocyclyl
- compound
- group
- salt
- 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.)
- Pending
Links
Classifications
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Indole Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762511851P | 2017-05-26 | 2017-05-26 | |
| US62/511,851 | 2017-05-26 | ||
| US201762523156P | 2017-06-21 | 2017-06-21 | |
| US62/523,156 | 2017-06-21 | ||
| PCT/US2018/034724 WO2018218192A1 (en) | 2017-05-26 | 2018-05-25 | Bacterial efflux pump inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN111163774A true CN111163774A (zh) | 2020-05-15 |
Family
ID=64395990
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201880045566.2A Pending CN111163774A (zh) | 2017-05-26 | 2018-05-25 | 细菌外排泵抑制剂 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US11826357B2 (https=) |
| EP (1) | EP3630109A4 (https=) |
| JP (2) | JP7281822B2 (https=) |
| CN (1) | CN111163774A (https=) |
| WO (1) | WO2018218192A1 (https=) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10836706B2 (en) | 2016-02-24 | 2020-11-17 | Rutgers, The State University Of New Jersey | Bacterial efflux pump inhibitors |
| US10556854B2 (en) | 2016-02-24 | 2020-02-11 | Rutgers, The State University Of New Jersey | Bacterial efflux pump inhibitors |
| US11938114B2 (en) | 2017-03-10 | 2024-03-26 | Rutgers, The State University Of New Jersey | Bacterial efflux pump inhibitors |
| WO2018165612A1 (en) | 2017-03-10 | 2018-09-13 | Rutgers, The State University Of New Jersey | Bacterial efflux pump inhibitors |
| CN110770224B (zh) | 2017-03-10 | 2022-11-18 | 罗格斯新泽西州立大学 | 作为外排泵抑制剂的吲哚衍生物 |
| EP3630109A4 (en) | 2017-05-26 | 2021-03-17 | Rutgers, the State University of New Jersey | BACTERIAL EFFLUX PUMP INHIBITORS |
| WO2019005841A1 (en) | 2017-06-26 | 2019-01-03 | Rutgers, The State University Of New Jersey | THERAPEUTIC COMPOUNDS AND METHODS FOR TREATING INFECTION |
| US11845742B2 (en) | 2017-11-14 | 2023-12-19 | Rutgers, The State University Of New Jersey | Therapeutic compounds and methods to treat infection |
| WO2021203014A1 (en) | 2020-04-03 | 2021-10-07 | Vertex Pharmaceuticals Incorporated | Pyrano[4,3-b]l ndole derivatives as alpha-1 -antitrypsin modulators for treating alpha-1 -antitrypsin deficiency (aatd) |
| US20240239771A1 (en) * | 2020-05-29 | 2024-07-18 | Taxis Pharmaceuticals, Inc. | Bacterial efflux pump inhibitors |
| AU2024327693A1 (en) * | 2023-08-23 | 2026-04-02 | Taxis Pharmaceuticals, Inc. | Bacterial efflux pump inhibitors |
Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3573325A (en) * | 1966-07-29 | 1971-03-30 | Ile De France | N-(1-alkyl-2-pyrrolidylmethyl)-3-alkoxy-(or hydroxy)-indoles-2-carboxamides |
| US3996159A (en) * | 1972-12-13 | 1976-12-07 | Schering Corporation | Antimicrobial compositions |
| US4014883A (en) * | 1973-09-10 | 1977-03-29 | Hoffmann-La Roche Inc. | Indoloquinolines, intermediates and processes |
| WO2003013484A2 (en) * | 2001-08-07 | 2003-02-20 | F. Hoffmann-La Roche Ag | N-monoacylated derivatives of o-phenylenediamines, their six membered heterocyclic analogues and their use as pharmaceutical agents |
| WO2009158375A1 (en) * | 2008-06-25 | 2009-12-30 | Abbott Laboratories | Aza-cylic indole- 2 -carboxamides and methods of use thereof |
| US20120028990A1 (en) * | 2009-04-16 | 2012-02-02 | Msd K.K | 3 aryl or heteroaryl-substituted indole derivative |
Family Cites Families (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR204240A1 (es) | 1972-12-13 | 1975-12-10 | Scherico Ltd | La preparacion de 2-aminoalcohil-3-fenil-indoles |
| US3978224A (en) | 1975-07-01 | 1976-08-31 | Schering Corporation | Antimicrobial halo-substituted-2-cyanoethylaminoalkyl-3-phenyl-indoles |
| US4938949A (en) | 1988-09-12 | 1990-07-03 | University Of New York | Treatment of damaged bone marrow and dosage units therefor |
| WO1992004017A1 (en) | 1990-09-10 | 1992-03-19 | The Upjohn Company | Cis-n-(2-aminocyclohexyl)benzamide and their enantiomers as anticonvulsants |
| US5663152A (en) | 1995-01-19 | 1997-09-02 | Asahi Kasei Kogyo Kabushiki Kaisha | Potentiators for aminoglycosides |
| US6204279B1 (en) | 1998-06-03 | 2001-03-20 | Microcide Pharmaceuticals, Inc. | Peptidomimetic efflux pump inhibitors |
| CA2353557A1 (en) | 1998-12-04 | 2000-06-08 | Influx, Inc. | Inhibitors of multidrug transporters |
| US6730684B1 (en) | 1999-10-08 | 2004-05-04 | Affinium Pharmaceuticals, Inc. | Fab I inhibitors |
| US6555569B2 (en) | 2000-03-07 | 2003-04-29 | Pfizer Inc. | Use of heteroaryl substituted N-(indole-2-carbonyl-) amides for treatment of infection |
| US7829543B2 (en) | 2003-01-07 | 2010-11-09 | Paratek Pharmaceuticals, Inc. | Substituted polyamines as inhibitors of bacterial efflux pumps |
| US7994225B2 (en) | 2004-03-17 | 2011-08-09 | Rempex Pharmaceuticals, Inc. | Bacterial efflux pump inhibitors for the treatment of ophthalmic and otic infections |
| WO2005113579A1 (en) * | 2004-05-21 | 2005-12-01 | Mpex Pharmaceuticals, Inc. | Bacterial efflux pump inhibitors and methods of treating bacterial infections |
| US8143257B2 (en) | 2004-11-23 | 2012-03-27 | Ptc Therapeutics, Inc. | Substituted phenols as active agents inhibiting VEGF production |
| US7855228B2 (en) | 2005-02-10 | 2010-12-21 | The Board Of Trustees Of The Leland Stamford Junior University | Antibiotics targeting MreB |
| DE102006033109A1 (de) * | 2006-07-18 | 2008-01-31 | Grünenthal GmbH | Substituierte Heteroaryl-Derivate |
| EP3192788A1 (en) | 2006-10-03 | 2017-07-19 | Arbutus Biopharma Corporation | Lipid containing formulations |
| CA2682483A1 (en) * | 2007-03-29 | 2008-10-09 | Novartis Ag | 3-imidazolyl-indoles for the treatment of proliferative diseases |
| WO2009110002A1 (en) | 2008-03-05 | 2009-09-11 | Council Of Scientific & Industrial Research | Novel efflux pump inhibitors |
| EP2303852A4 (en) | 2008-06-26 | 2011-12-28 | Glaxosmithkline Llc | ACTIVITY INHIBITORS AKT |
| CA2737038A1 (en) | 2008-09-18 | 2010-03-25 | Evotec Ag | Amide compounds, compositions and uses thereof |
| EA201101451A1 (ru) | 2009-04-03 | 2012-03-30 | Ачиллион Фармасьютикалз, Инк. | Гидрокситиенохинолоны и родственные соединения как противоинфекционные средства |
| EP2536408A1 (en) | 2010-02-16 | 2012-12-26 | Wockhardt Research Centre | Efflux pump inhibitors |
| FR2969150B1 (fr) | 2010-12-20 | 2013-07-26 | Centre Nat Rech Scient | Nouvelles molecules indoliques demontrant des activites antibacteriennes dans une variete de bacteries a gram-negatif et positif dont des bacteries multidrogues-resistantes |
| BR112015004666B1 (pt) * | 2012-09-07 | 2022-04-26 | Novartis Ag | Derivados de indol carboxamida, seu uso, e composição farmacêutica |
| CA2890748A1 (en) | 2012-11-13 | 2014-05-22 | Memorial Sloan-Kettering Cancer Center | Indole compounds and their use as antimicrobials |
| WO2015164482A1 (en) | 2014-04-22 | 2015-10-29 | The Johns Hopkins University | Inhibitors of drug-resistant mycobacterium tuberculosis |
| US9926261B2 (en) * | 2015-03-10 | 2018-03-27 | Rutgers, The State University Of New Jersey | Bacterial efflux pump inhibitors |
| US9950993B2 (en) | 2015-03-13 | 2018-04-24 | Rutgers, The State University Of New Jersey | Bacterial efflux pump inhibitors |
| KR20180011843A (ko) | 2015-06-11 | 2018-02-02 | 바실리어 파마슈티카 인터내셔널 리미티드 | 유출-펌프 억제제 및 이의 치료적 용도 |
| US10836706B2 (en) | 2016-02-24 | 2020-11-17 | Rutgers, The State University Of New Jersey | Bacterial efflux pump inhibitors |
| US10556854B2 (en) | 2016-02-24 | 2020-02-11 | Rutgers, The State University Of New Jersey | Bacterial efflux pump inhibitors |
| US11938114B2 (en) | 2017-03-10 | 2024-03-26 | Rutgers, The State University Of New Jersey | Bacterial efflux pump inhibitors |
| CN110770224B (zh) | 2017-03-10 | 2022-11-18 | 罗格斯新泽西州立大学 | 作为外排泵抑制剂的吲哚衍生物 |
| WO2018165612A1 (en) | 2017-03-10 | 2018-09-13 | Rutgers, The State University Of New Jersey | Bacterial efflux pump inhibitors |
| EP3630109A4 (en) | 2017-05-26 | 2021-03-17 | Rutgers, the State University of New Jersey | BACTERIAL EFFLUX PUMP INHIBITORS |
| WO2019005841A1 (en) | 2017-06-26 | 2019-01-03 | Rutgers, The State University Of New Jersey | THERAPEUTIC COMPOUNDS AND METHODS FOR TREATING INFECTION |
| US20190031624A1 (en) | 2017-07-28 | 2019-01-31 | Rutgers, The State University Of New Jersey | Therapeutic compounds and methods to treat infection |
-
2018
- 2018-05-25 EP EP18806950.4A patent/EP3630109A4/en not_active Withdrawn
- 2018-05-25 CN CN201880045566.2A patent/CN111163774A/zh active Pending
- 2018-05-25 US US16/616,903 patent/US11826357B2/en active Active
- 2018-05-25 WO PCT/US2018/034724 patent/WO2018218192A1/en not_active Ceased
- 2018-05-25 JP JP2020515831A patent/JP7281822B2/ja active Active
-
2022
- 2022-09-02 JP JP2022139960A patent/JP2022169800A/ja active Pending
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3573325A (en) * | 1966-07-29 | 1971-03-30 | Ile De France | N-(1-alkyl-2-pyrrolidylmethyl)-3-alkoxy-(or hydroxy)-indoles-2-carboxamides |
| US3996159A (en) * | 1972-12-13 | 1976-12-07 | Schering Corporation | Antimicrobial compositions |
| US4014883A (en) * | 1973-09-10 | 1977-03-29 | Hoffmann-La Roche Inc. | Indoloquinolines, intermediates and processes |
| WO2003013484A2 (en) * | 2001-08-07 | 2003-02-20 | F. Hoffmann-La Roche Ag | N-monoacylated derivatives of o-phenylenediamines, their six membered heterocyclic analogues and their use as pharmaceutical agents |
| WO2009158375A1 (en) * | 2008-06-25 | 2009-12-30 | Abbott Laboratories | Aza-cylic indole- 2 -carboxamides and methods of use thereof |
| US20120028990A1 (en) * | 2009-04-16 | 2012-02-02 | Msd K.K | 3 aryl or heteroaryl-substituted indole derivative |
Non-Patent Citations (1)
| Title |
|---|
| REGISTRY: "1378007-92-1", 《STN CHEMICAL LIBRARY SUPPLIER:CHEMBRIDGE CORPORATION》 * |
Also Published As
| Publication number | Publication date |
|---|---|
| JP7281822B2 (ja) | 2023-05-26 |
| JP2020527597A (ja) | 2020-09-10 |
| WO2018218192A1 (en) | 2018-11-29 |
| US20200197382A1 (en) | 2020-06-25 |
| JP2022169800A (ja) | 2022-11-09 |
| US11826357B2 (en) | 2023-11-28 |
| EP3630109A1 (en) | 2020-04-08 |
| EP3630109A4 (en) | 2021-03-17 |
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