CN105829288B - 抗菌1h-吲唑及1h-吲哚衍生物 - Google Patents
抗菌1h-吲唑及1h-吲哚衍生物 Download PDFInfo
- Publication number
- CN105829288B CN105829288B CN201480067976.9A CN201480067976A CN105829288B CN 105829288 B CN105829288 B CN 105829288B CN 201480067976 A CN201480067976 A CN 201480067976A CN 105829288 B CN105829288 B CN 105829288B
- Authority
- CN
- China
- Prior art keywords
- base
- methyl
- hydroxyl
- mesyl
- butyramide
- 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.)
- Expired - Fee Related
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
-
- 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
- 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
- C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
-
- 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
- C07D403/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
- C07D405/06—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 carbon chain containing only aliphatic carbon atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Indole Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13198338.9 | 2013-12-19 | ||
| EP13198338 | 2013-12-19 | ||
| PCT/EP2014/078384 WO2015091741A1 (en) | 2013-12-19 | 2014-12-18 | Antibacterial 1h-indazole and 1h-indole derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN105829288A CN105829288A (zh) | 2016-08-03 |
| CN105829288B true CN105829288B (zh) | 2019-01-15 |
Family
ID=49880464
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201480067976.9A Expired - Fee Related CN105829288B (zh) | 2013-12-19 | 2014-12-18 | 抗菌1h-吲唑及1h-吲哚衍生物 |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US9624206B2 (enExample) |
| EP (1) | EP3083567B1 (enExample) |
| JP (1) | JP6407288B2 (enExample) |
| KR (1) | KR20160098503A (enExample) |
| CN (1) | CN105829288B (enExample) |
| AR (1) | AR100032A1 (enExample) |
| AU (1) | AU2014368619B2 (enExample) |
| BR (1) | BR112016014115A8 (enExample) |
| CA (1) | CA2933604A1 (enExample) |
| CL (1) | CL2016001524A1 (enExample) |
| EA (1) | EA030730B1 (enExample) |
| ES (1) | ES2666130T3 (enExample) |
| IL (1) | IL246201A0 (enExample) |
| MA (1) | MA39189A1 (enExample) |
| MX (1) | MX360983B (enExample) |
| PH (1) | PH12016501102A1 (enExample) |
| PL (1) | PL3083567T3 (enExample) |
| SG (1) | SG11201605014YA (enExample) |
| TR (1) | TR201807881T4 (enExample) |
| TW (1) | TW201609641A (enExample) |
| WO (1) | WO2015091741A1 (enExample) |
| ZA (1) | ZA201604968B (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR097617A1 (es) | 2013-09-13 | 2016-04-06 | Actelion Pharmaceuticals Ltd | Derivados antibacterianos del 2h-indazol |
| AR099612A1 (es) | 2014-03-04 | 2016-08-03 | Actelion Pharmaceuticals Ltd | Derivados antibacterianos de 1,2-dihidro-3h-pirrolo[1,2-c]imidazol-3-ona |
| JP2017515906A (ja) | 2014-05-16 | 2017-06-15 | アクテリオン ファーマシューティカルズ リミテッドＡｃｔｅｌｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｌｔｄ | 抗菌性キナゾロン−４（３ｈ）−オン誘導体 |
| KR20170086079A (ko) | 2014-11-19 | 2017-07-25 | 액테리온 파마슈티칼 리미티드 | 항균성 벤조티아졸 유도체 |
| AR105646A1 (es) | 2015-08-11 | 2017-10-25 | Actelion Pharmaceuticals Ltd | Agentes antibacterianos de 1,2-dihidro-3h-pirrolo[1,2-c]imidazol-3-ona sustituida |
| US20190031676A1 (en) * | 2015-08-28 | 2019-01-31 | Idorsia Pharmaceuticals Ltd | Antibacterial annulated pyrrolidin-2-one derivatives |
| AR105848A1 (es) * | 2015-08-31 | 2017-11-15 | Actelion Pharmaceuticals Ltd | Derivados heterocíclicos antibacterianos |
| AR105889A1 (es) | 2015-09-03 | 2017-11-22 | Actelion Pharmaceuticals Ltd | Compuestos antibacterianos 1,2-dihidro-3h-pirrolo[1,2-c]imidazol-3-ona sustituidos |
| AR108488A1 (es) * | 2016-05-17 | 2018-08-22 | Idorsia Pharmaceuticals Ltd | Derivados 6-(buta-1,3-diin-1-il)benzo[d]tiazol |
| TW201906819A (zh) | 2017-05-25 | 2019-02-16 | 日商大正製藥股份有限公司 | 新穎之咪唑衍生物 |
| WO2019086452A1 (en) * | 2017-10-31 | 2019-05-09 | Idorsia Pharmaceuticals Ltd | Antibacterial heteroaromatic compounds |
| CN113666860B (zh) * | 2020-05-14 | 2024-03-15 | 鲁南制药集团股份有限公司 | 一种7-乙基色醇的制备方法 |
| CN119014415B (zh) * | 2024-08-19 | 2025-09-05 | 浙江大学 | 1-甲氧基吲哚在驱避和/或杀灭害虫中的应用 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011045703A2 (en) * | 2009-10-13 | 2011-04-21 | Pfizer Inc. | C-linked hydroxamic acid derivatives useful as antibacterial agents |
| WO2012137099A1 (en) * | 2011-04-08 | 2012-10-11 | Pfizer Inc. | Imidazole, pyrazole, and triazole derivatives useful as antibacterial agents |
| CN103443079A (zh) * | 2011-03-07 | 2013-12-11 | 辉瑞大药厂 | 可用作抗菌剂的氟吡啶酮衍生物 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2478374C (en) | 2002-03-13 | 2009-01-06 | Eli M. Wallace | N3 alkylated benzimidazole derivatives as mek inhibitors |
| DE102004017930A1 (de) | 2004-04-14 | 2005-11-03 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel |
| AU2005295441B2 (en) | 2004-10-18 | 2009-04-23 | Amgen, Inc. | Thiadiazole compounds and methods of use |
| KR100973609B1 (ko) | 2005-03-23 | 2010-08-03 | 에프. 호프만-라 로슈 아게 | ｍＧｌｕＲ2 길항제로서 아세틸렌일-피라졸로-피리미딘유도체 |
| WO2008154642A2 (en) | 2007-06-12 | 2008-12-18 | Achaogen, Inc. | Antibacterial agents |
| EP2432468A2 (en) | 2009-05-20 | 2012-03-28 | Ardea Biosciences, Inc. | Methods of modulating uric acid levels |
| PL2512474T3 (pl) | 2009-12-16 | 2015-03-31 | Pfizer | N-przyłączone pochodne kwasu hydroksamowego użyteczne jako środki przeciwbakteryjne |
| GB2483736B (en) | 2010-09-16 | 2012-08-29 | Aragon Pharmaceuticals Inc | Estrogen receptor modulators and uses thereof |
| MX2013005200A (es) | 2010-11-10 | 2013-06-28 | Achaogen Inc | Derivados de acido hidroxamico y su so en el tratamiento de infecciones bacterianas. |
| JP2014501274A (ja) | 2011-01-03 | 2014-01-20 | ハンミ ファーム． シーオー．， エルティーディー． | Ｇタンパク質共役受容体調節のための新規な二環式化合物 |
| CN103717582B (zh) | 2011-04-08 | 2015-09-30 | 辉瑞大药厂 | 用作抗菌剂的异*唑衍生物 |
| WO2013170030A1 (en) | 2012-05-09 | 2013-11-14 | Achaogen, Inc. | Antibacterial agents |
| WO2013170165A1 (en) | 2012-05-10 | 2013-11-14 | Achaogen, Inc. | Antibacterial agents |
| AR097617A1 (es) | 2013-09-13 | 2016-04-06 | Actelion Pharmaceuticals Ltd | Derivados antibacterianos del 2h-indazol |
| AR099612A1 (es) | 2014-03-04 | 2016-08-03 | Actelion Pharmaceuticals Ltd | Derivados antibacterianos de 1,2-dihidro-3h-pirrolo[1,2-c]imidazol-3-ona |
| JP2017515906A (ja) | 2014-05-16 | 2017-06-15 | アクテリオン ファーマシューティカルズ リミテッドＡｃｔｅｌｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｌｔｄ | 抗菌性キナゾロン−４（３ｈ）−オン誘導体 |
-
2014
- 2014-12-18 TR TR2018/07881T patent/TR201807881T4/tr unknown
- 2014-12-18 CA CA2933604A patent/CA2933604A1/en not_active Abandoned
- 2014-12-18 EA EA201600475A patent/EA030730B1/ru not_active IP Right Cessation
- 2014-12-18 PL PL14812752T patent/PL3083567T3/pl unknown
- 2014-12-18 CN CN201480067976.9A patent/CN105829288B/zh not_active Expired - Fee Related
- 2014-12-18 MA MA39189A patent/MA39189A1/fr unknown
- 2014-12-18 WO PCT/EP2014/078384 patent/WO2015091741A1/en not_active Ceased
- 2014-12-18 MX MX2016007991A patent/MX360983B/es active IP Right Grant
- 2014-12-18 SG SG11201605014YA patent/SG11201605014YA/en unknown
- 2014-12-18 JP JP2016541300A patent/JP6407288B2/ja not_active Expired - Fee Related
- 2014-12-18 AU AU2014368619A patent/AU2014368619B2/en not_active Ceased
- 2014-12-18 US US15/106,790 patent/US9624206B2/en not_active Expired - Fee Related
- 2014-12-18 TW TW103144395A patent/TW201609641A/zh unknown
- 2014-12-18 ES ES14812752.5T patent/ES2666130T3/es active Active
- 2014-12-18 AR ARP140104742A patent/AR100032A1/es unknown
- 2014-12-18 BR BR112016014115A patent/BR112016014115A8/pt not_active Application Discontinuation
- 2014-12-18 KR KR1020167019669A patent/KR20160098503A/ko not_active Ceased
- 2014-12-18 EP EP14812752.5A patent/EP3083567B1/en not_active Not-in-force
-
2016
- 2016-06-09 PH PH12016501102A patent/PH12016501102A1/en unknown
- 2016-06-14 IL IL246201A patent/IL246201A0/en unknown
- 2016-06-16 CL CL2016001524A patent/CL2016001524A1/es unknown
- 2016-07-18 ZA ZA2016/04968A patent/ZA201604968B/en unknown
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011045703A2 (en) * | 2009-10-13 | 2011-04-21 | Pfizer Inc. | C-linked hydroxamic acid derivatives useful as antibacterial agents |
| CN103443079A (zh) * | 2011-03-07 | 2013-12-11 | 辉瑞大药厂 | 可用作抗菌剂的氟吡啶酮衍生物 |
| WO2012137099A1 (en) * | 2011-04-08 | 2012-10-11 | Pfizer Inc. | Imidazole, pyrazole, and triazole derivatives useful as antibacterial agents |
Non-Patent Citations (1)
| Title |
|---|
| Heterocyclic methylsulfone hydroxamic acid LpxC inhibitors as Gram-negative antibacterial agents;Laura A. Mcallister等;《Bioorganic & Medicinal Chemistry Letters》;20120924;第22卷(第22期);6832-6838 * |
Also Published As
| Publication number | Publication date |
|---|---|
| CA2933604A1 (en) | 2015-06-25 |
| JP6407288B2 (ja) | 2018-10-17 |
| BR112016014115A8 (pt) | 2017-12-26 |
| ES2666130T3 (es) | 2018-05-03 |
| CN105829288A (zh) | 2016-08-03 |
| EA030730B1 (ru) | 2018-09-28 |
| IL246201A0 (en) | 2016-08-02 |
| AR100032A1 (es) | 2016-09-07 |
| MX2016007991A (es) | 2016-10-07 |
| PH12016501102A1 (en) | 2016-07-11 |
| TW201609641A (zh) | 2016-03-16 |
| EP3083567B1 (en) | 2018-03-07 |
| TR201807881T4 (tr) | 2018-06-21 |
| AU2014368619A1 (en) | 2016-07-28 |
| WO2015091741A1 (en) | 2015-06-25 |
| MX360983B (es) | 2018-11-22 |
| EA201600475A1 (ru) | 2016-11-30 |
| CL2016001524A1 (es) | 2017-01-27 |
| SG11201605014YA (en) | 2016-07-28 |
| JP2017500336A (ja) | 2017-01-05 |
| EP3083567A1 (en) | 2016-10-26 |
| ZA201604968B (en) | 2018-11-28 |
| MA39189A1 (fr) | 2017-06-30 |
| US20170029411A1 (en) | 2017-02-02 |
| AU2014368619B2 (en) | 2018-11-22 |
| BR112016014115A2 (enExample) | 2017-08-08 |
| KR20160098503A (ko) | 2016-08-18 |
| US9624206B2 (en) | 2017-04-18 |
| PL3083567T3 (pl) | 2018-08-31 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| TA01 | Transfer of patent application right |
Effective date of registration: 20171101 Address after: Swiss A Skei Weil Applicant after: Aidu West Pharmaceutical Co. Ltd. Address before: Swiss A Skei Weil Applicant before: Actelion Pharmaceuticals Ltd. |
|
| TA01 | Transfer of patent application right | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20190115 Termination date: 20201218 |
|
| CF01 | Termination of patent right due to non-payment of annual fee |