KR102697360B1 - 유출 펌프 억제제로서의 인돌 유도체 - Google Patents
유출 펌프 억제제로서의 인돌 유도체 Download PDFInfo
- Publication number
- KR102697360B1 KR102697360B1 KR1020197029528A KR20197029528A KR102697360B1 KR 102697360 B1 KR102697360 B1 KR 102697360B1 KR 1020197029528 A KR1020197029528 A KR 1020197029528A KR 20197029528 A KR20197029528 A KR 20197029528A KR 102697360 B1 KR102697360 B1 KR 102697360B1
- Authority
- KR
- South Korea
- Prior art keywords
- alkyl
- mmol
- carbocyclyl
- compound
- halo
- 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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Classifications
-
- 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
-
- 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
-
- 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
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- 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
- 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
- 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
- C07D405/04—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 directly linked by a ring-member-to-ring-member bond
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 |
|---|---|---|---|
| US201762469987P | 2017-03-10 | 2017-03-10 | |
| US62/469,987 | 2017-03-10 | ||
| US201762523154P | 2017-06-21 | 2017-06-21 | |
| US62/523,154 | 2017-06-21 | ||
| PCT/US2018/021848 WO2018165611A1 (en) | 2017-03-10 | 2018-03-09 | Indole derivatives as efflux pump inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20190138790A KR20190138790A (ko) | 2019-12-16 |
| KR102697360B1 true KR102697360B1 (ko) | 2024-08-20 |
Family
ID=62044950
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020197029528A Active KR102697360B1 (ko) | 2017-03-10 | 2018-03-09 | 유출 펌프 억제제로서의 인돌 유도체 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US11993571B2 (https=) |
| EP (1) | EP3592736A1 (https=) |
| JP (1) | JP7323179B2 (https=) |
| KR (1) | KR102697360B1 (https=) |
| CN (1) | CN110770224B (https=) |
| AU (1) | AU2018231120B2 (https=) |
| BR (1) | BR112019018691A2 (https=) |
| CA (1) | CA3061238A1 (https=) |
| IL (1) | IL269210B2 (https=) |
| MX (1) | MX2019010717A (https=) |
| SG (1) | SG11201908351TA (https=) |
| WO (1) | WO2018165611A1 (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 |
| KR102704123B1 (ko) | 2019-11-01 | 2024-09-06 | 에스엘 주식회사 | 차량용 램프 |
| AU2024327693A1 (en) | 2023-08-23 | 2026-04-02 | Taxis Pharmaceuticals, Inc. | Bacterial efflux pump inhibitors |
| TW202525791A (zh) * | 2023-08-29 | 2025-07-01 | 美商梅斯治療股份有限公司 | 溶質載體家族6a成員19(slc6a19)之抑制劑及其使用方法 |
Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007115231A2 (en) | 2006-03-30 | 2007-10-11 | Chemocentryx, Inc. | Cxcr4 modulators |
| WO2008012782A2 (en) * | 2006-07-27 | 2008-01-31 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | Labelled analogues of halobenzamides as radiopharmaceuticals |
| WO2009103552A1 (en) * | 2008-02-22 | 2009-08-27 | Grünenthal GmbH | Substituted indole derivatives |
| WO2012084971A1 (fr) | 2010-12-20 | 2012-06-28 | Centre National De La Recherche Scientifique (Cnrs) | Derives d'indoles en tant qu'agents contre des bacteries a gram negatif et positif |
| WO2014078294A1 (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 |
| WO2016040505A1 (en) * | 2014-09-10 | 2016-03-17 | Epizyme, Inc. | Smyd inhibitors |
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| US3238215A (en) * | 1963-10-17 | 1966-03-01 | Sterling Drug Inc | 1-[(3-, 2-, and 1-indolyl)-lower-alkyl-, lower-alkenyl-, and lower-alkynyl]piperidines |
| US3465080A (en) * | 1968-10-07 | 1969-09-02 | American Cyanamid Co | Therapeutic compositions containing morpholinoalkylene - indoles and methods of administering such in the treatment of depression |
| US3978224A (en) | 1975-07-01 | 1976-08-31 | Schering Corporation | Antimicrobial halo-substituted-2-cyanoethylaminoalkyl-3-phenyl-indoles |
| US4910193A (en) * | 1985-12-16 | 1990-03-20 | Sandoz Ltd. | Treatment of gastrointestinal disorders |
| 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 |
| US5864039A (en) * | 1994-03-30 | 1999-01-26 | Yoshitomi Pharmaceutical Industries, Ltd. | Benzoic acid compounds and use thereof as medicaments |
| US5663152A (en) | 1995-01-19 | 1997-09-02 | Asahi Kasei Kogyo Kabushiki Kaisha | Potentiators for aminoglycosides |
| US6506339B1 (en) * | 1997-02-10 | 2003-01-14 | Biomedical Design, Inc. | Method of sterilization |
| AU2337599A (en) * | 1998-01-23 | 1999-08-09 | Microcide Pharmaceuticals, Inc. | Efflux pump inhibitors |
| 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 |
| CO5251397A1 (es) | 1999-10-08 | 2003-02-28 | Smithkline Beecham Corp | Inhibidores de fab i |
| US6555569B2 (en) | 2000-03-07 | 2003-04-29 | Pfizer Inc. | Use of heteroaryl substituted N-(indole-2-carbonyl-) amides for treatment of infection |
| US7365205B2 (en) * | 2001-06-20 | 2008-04-29 | Daiichi Sankyo Company, Limited | Diamine derivatives |
| HUP0103986A2 (hu) * | 2001-09-28 | 2003-06-28 | Richter Gedeon Vegyészeti Gyár Rt. | Új karbonsavamid szerkezetet tartalmazó piperidinil vegyületek, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények |
| EP1314733A1 (en) * | 2001-11-22 | 2003-05-28 | Aventis Pharma Deutschland GmbH | Indole-2-carboxamides as factor Xa inhibitors |
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| GB0403038D0 (en) * | 2004-02-11 | 2004-03-17 | Novartis Ag | Organic compounds |
| US7994225B2 (en) | 2004-03-17 | 2011-08-09 | Rempex Pharmaceuticals, Inc. | Bacterial efflux pump inhibitors for the treatment of ophthalmic and otic infections |
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| EP2536408A1 (en) | 2010-02-16 | 2012-12-26 | Wockhardt Research Centre | Efflux pump inhibitors |
| EP2394653A1 (en) * | 2010-05-26 | 2011-12-14 | Almirall, S.A. | Topical pharmaceutical compositions comprising mometasone furoate |
| BR112015004666B1 (pt) | 2012-09-07 | 2022-04-26 | Novartis Ag | Derivados de indol carboxamida, seu uso, e composição farmacêutica |
| 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 |
| WO2017023894A1 (en) * | 2015-08-03 | 2017-02-09 | Raze Therapeutics, Inc. | Mthfd2 inhibitors and uses thereof |
| 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 |
| ES2968227T3 (es) * | 2016-12-23 | 2024-05-08 | Aquinnah Pharmaceuticals Inc | Compuestos, composiciones y procedimientos de uso |
| 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 |
| 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 |
| 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 |
| US11845742B2 (en) * | 2017-11-14 | 2023-12-19 | Rutgers, The State University Of New Jersey | Therapeutic compounds and methods to treat infection |
-
2018
- 2018-03-09 CN CN201880030845.1A patent/CN110770224B/zh active Active
- 2018-03-09 BR BR112019018691-3A patent/BR112019018691A2/pt active Search and Examination
- 2018-03-09 WO PCT/US2018/021848 patent/WO2018165611A1/en not_active Ceased
- 2018-03-09 AU AU2018231120A patent/AU2018231120B2/en active Active
- 2018-03-09 KR KR1020197029528A patent/KR102697360B1/ko active Active
- 2018-03-09 MX MX2019010717A patent/MX2019010717A/es unknown
- 2018-03-09 SG SG11201908351T patent/SG11201908351TA/en unknown
- 2018-03-09 EP EP18719686.0A patent/EP3592736A1/en active Pending
- 2018-03-09 US US16/492,901 patent/US11993571B2/en active Active
- 2018-03-09 JP JP2019549454A patent/JP7323179B2/ja active Active
- 2018-03-09 CA CA3061238A patent/CA3061238A1/en active Pending
- 2018-03-09 IL IL269210A patent/IL269210B2/en unknown
Patent Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007115231A2 (en) | 2006-03-30 | 2007-10-11 | Chemocentryx, Inc. | Cxcr4 modulators |
| WO2008012782A2 (en) * | 2006-07-27 | 2008-01-31 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | Labelled analogues of halobenzamides as radiopharmaceuticals |
| WO2009103552A1 (en) * | 2008-02-22 | 2009-08-27 | Grünenthal GmbH | Substituted indole derivatives |
| WO2012084971A1 (fr) | 2010-12-20 | 2012-06-28 | Centre National De La Recherche Scientifique (Cnrs) | Derives d'indoles en tant qu'agents contre des bacteries a gram negatif et positif |
| WO2014078294A1 (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 |
| WO2016040505A1 (en) * | 2014-09-10 | 2016-03-17 | Epizyme, Inc. | Smyd inhibitors |
Also Published As
| Publication number | Publication date |
|---|---|
| IL269210A (en) | 2019-11-28 |
| US20210094912A1 (en) | 2021-04-01 |
| CA3061238A1 (en) | 2018-09-13 |
| EP3592736A1 (en) | 2020-01-15 |
| AU2018231120A1 (en) | 2019-10-31 |
| SG11201908351TA (en) | 2019-10-30 |
| IL269210B1 (en) | 2025-01-01 |
| JP7323179B2 (ja) | 2023-08-08 |
| JP2020510044A (ja) | 2020-04-02 |
| WO2018165611A1 (en) | 2018-09-13 |
| CN110770224A (zh) | 2020-02-07 |
| AU2018231120B2 (en) | 2022-06-23 |
| MX2019010717A (es) | 2019-12-05 |
| BR112019018691A2 (pt) | 2020-04-07 |
| KR20190138790A (ko) | 2019-12-16 |
| US11993571B2 (en) | 2024-05-28 |
| CN110770224B (zh) | 2022-11-18 |
| IL269210B2 (en) | 2025-05-01 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PA0105 | International application |
Patent event date: 20191008 Patent event code: PA01051R01D Comment text: International Patent Application |
|
| PG1501 | Laying open of application | ||
| PA0201 | Request for examination |
Patent event code: PA02012R01D Patent event date: 20210305 Comment text: Request for Examination of Application |
|
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