EA201600475A1 - Антибактериальные производные 1h-индазола и 1h-индола - Google Patents
Антибактериальные производные 1h-индазола и 1h-индолаInfo
- Publication number
- EA201600475A1 EA201600475A1 EA201600475A EA201600475A EA201600475A1 EA 201600475 A1 EA201600475 A1 EA 201600475A1 EA 201600475 A EA201600475 A EA 201600475A EA 201600475 A EA201600475 A EA 201600475A EA 201600475 A1 EA201600475 A1 EA 201600475A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- methyl
- halogen
- phosphonooxy
- cycloprop
- cyclopropyl
- Prior art date
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
-
- 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
-
- 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
- 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)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Indole Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Изобретение относится к антибактериальным соединениям формулы Iгде X представляет собой N или CH; Rпредставляет собой H или галоген; Rпредставляет собой алкинилокси или группу M; Rпредставляет собой H или галоген; M представляет собой одну из групп Mи M, представленных нижегде A представляет собой связь, CHCH, CH=CH или C≡C; Rпредставляет собой H или галоген; Rпредставляет собой H, алкокси или галоген; Rпредставляет собой H, алкокси, гидроксиалкокси, алкоксиалкокси, тиоалкокси, трифторметокси, амино, гидроксиалкил, 2-гидроксиацетамидо, 1-аминоциклопропил, 1-гидроксиметилциклопроп-1-ил, 1-((фосфоноокси)метил)циклопропил, 1-(((диметилглицил)окси)метил)циклопропил, транс-2-гидроксиметилциклопроп-1-ил, 1,2-дигидроксиэтил, 3-гидроксиоксетан-3-ил, 3-(гидроксиалкил)оксетан-3-ил, 3-аминооксетан-3-ил, 3-гидрокситиетан-3-ил, морфолин-4-илалкокси, морфолин-4-ил-алкил, оксазол-2-ил или [1,2,3]триазол-2-ил; и Rпредставляет собой гидроксиалкил, дигидроксиалкил, аминоалкил, 1-гидроксиметилциклопроп-1-ил, 1-аминометил-циклопроп-1-ил, транс-2-гидроксиметилциклопроп-1-ил, 3-гидроксиоксетан-3-ил, 3-гидрокситиетан-3-ил, 1-(2-гидроксиацетил)азетидин-3-ил, 1-(2-аминоацетил)азетидин-3-ил, 1-глицилазетидин-3-ил, 1-(2-амино-2-метилпропаноил)азетидин-3-ил, 3-(2-аминоацетамидо)циклопентил, транс-(цис-3,4-дигидрокси)циклопент-1-ил или 3-гидроксиметилбицикло[ 1,1,1]пентан-1-ил; и к их солям.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| 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 |
|---|---|
| EA201600475A1 true EA201600475A1 (ru) | 2016-11-30 |
| EA030730B1 EA030730B1 (ru) | 2018-09-28 |
Family
ID=49880464
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201600475A EA030730B1 (ru) | 2013-12-19 | 2014-12-18 | Антибактериальные производные 1h-индазола и 1h-индола |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US9624206B2 (ru) |
| EP (1) | EP3083567B1 (ru) |
| JP (1) | JP6407288B2 (ru) |
| KR (1) | KR20160098503A (ru) |
| CN (1) | CN105829288B (ru) |
| AR (1) | AR100032A1 (ru) |
| AU (1) | AU2014368619B2 (ru) |
| BR (1) | BR112016014115A8 (ru) |
| CA (1) | CA2933604A1 (ru) |
| CL (1) | CL2016001524A1 (ru) |
| EA (1) | EA030730B1 (ru) |
| ES (1) | ES2666130T3 (ru) |
| IL (1) | IL246201A0 (ru) |
| MA (1) | MA39189A1 (ru) |
| MX (1) | MX360983B (ru) |
| PH (1) | PH12016501102A1 (ru) |
| PL (1) | PL3083567T3 (ru) |
| SG (1) | SG11201605014YA (ru) |
| TR (1) | TR201807881T4 (ru) |
| TW (1) | TW201609641A (ru) |
| WO (1) | WO2015091741A1 (ru) |
| ZA (1) | ZA201604968B (ru) |
Families Citing this family (12)
| 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 |
| EP3143007B1 (en) | 2014-05-16 | 2018-07-11 | Idorsia Pharmaceuticals Ltd | Antibacterial quinazoline-4(3h)-one derivatives |
| TW201625569A (zh) | 2014-11-19 | 2016-07-16 | 艾克泰聯製藥有限公司 | 抗菌性苯并噻唑衍生物 |
| 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 |
| AU2016314963A1 (en) * | 2015-08-28 | 2018-04-19 | 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 |
| MX2018014170A (es) * | 2016-05-17 | 2019-03-14 | 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 |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2407849T3 (es) | 2002-03-13 | 2013-06-14 | Array Biopharma, Inc. | Derivados de bencimidazol alquilados N3 como inhibidores de MEK |
| 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 |
| JP4931823B2 (ja) | 2004-10-18 | 2012-05-16 | アムジエン・インコーポレーテツド | チアジアゾール化合物及び使用方法 |
| PL1863818T3 (pl) | 2005-03-23 | 2010-08-31 | Hoffmann La Roche | Pochodne acetylenylo-pirazolo-pirymidyny jako antagoniści MGLUR2 |
| ES2602615T3 (es) | 2007-06-12 | 2017-02-21 | Achaogen, Inc. | Agentes antibacterianos |
| WO2010135536A2 (en) | 2009-05-20 | 2010-11-25 | Ardea Biosciences, Inc. | Methods of modulating uric acid levels |
| CA2774250C (en) * | 2009-10-13 | 2013-12-17 | Pfizer Inc. | C-linked hydroxamic acid derivatives useful as antibacterial agents |
| CA2782453C (en) | 2009-12-16 | 2015-11-24 | Matthew Frank Brown | N-linked hydroxamic acid derivatives useful as antibacterial agents |
| GB2483736B (en) | 2010-09-16 | 2012-08-29 | Aragon Pharmaceuticals Inc | Estrogen receptor modulators and uses thereof |
| JP2014501716A (ja) | 2010-11-10 | 2014-01-23 | アカオジェン インコーポレイテッド | ヒドロキサム酸誘導体および細菌感染の処置におけるその使用 |
| EP2661438A4 (en) | 2011-01-03 | 2014-06-11 | Hanmi Pharm Ind Co Ltd | NEW BICYCLIC COMPOUND FOR THE MODULATION OF G PROTEIN-COUPLED RECEPTORS |
| SG192766A1 (en) * | 2011-03-07 | 2013-09-30 | Pfizer | Fluoro-pyridinone derivatives useful as antibacterial agents |
| EP2694481B1 (en) | 2011-04-08 | 2015-12-30 | Pfizer Inc | Imidazole, pyrazole, and triazole derivatives useful as antibacterial agents |
| SG193367A1 (en) | 2011-04-08 | 2013-10-30 | Pfizer | Isoxazole derivatives useful as antibacterial agents |
| EP2847162A1 (en) | 2012-05-09 | 2015-03-18 | 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 |
| EP3143007B1 (en) | 2014-05-16 | 2018-07-11 | Idorsia Pharmaceuticals Ltd | Antibacterial quinazoline-4(3h)-one derivatives |
-
2014
- 2014-12-18 SG SG11201605014YA patent/SG11201605014YA/en unknown
- 2014-12-18 AR ARP140104742A patent/AR100032A1/es unknown
- 2014-12-18 KR KR1020167019669A patent/KR20160098503A/ko not_active Application Discontinuation
- 2014-12-18 WO PCT/EP2014/078384 patent/WO2015091741A1/en active Application Filing
- 2014-12-18 CN CN201480067976.9A patent/CN105829288B/zh not_active Expired - Fee Related
- 2014-12-18 US US15/106,790 patent/US9624206B2/en active Active
- 2014-12-18 BR BR112016014115A patent/BR112016014115A8/pt not_active Application Discontinuation
- 2014-12-18 PL PL14812752T patent/PL3083567T3/pl unknown
- 2014-12-18 CA CA2933604A patent/CA2933604A1/en not_active Abandoned
- 2014-12-18 EP EP14812752.5A patent/EP3083567B1/en not_active Not-in-force
- 2014-12-18 ES ES14812752.5T patent/ES2666130T3/es active Active
- 2014-12-18 AU AU2014368619A patent/AU2014368619B2/en not_active Ceased
- 2014-12-18 TR TR2018/07881T patent/TR201807881T4/tr unknown
- 2014-12-18 EA EA201600475A patent/EA030730B1/ru not_active IP Right Cessation
- 2014-12-18 MA MA39189A patent/MA39189A1/fr unknown
- 2014-12-18 TW TW103144395A patent/TW201609641A/zh unknown
- 2014-12-18 MX MX2016007991A patent/MX360983B/es active IP Right Grant
- 2014-12-18 JP JP2016541300A patent/JP6407288B2/ja not_active Expired - Fee Related
-
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
Also Published As
| Publication number | Publication date |
|---|---|
| TR201807881T4 (tr) | 2018-06-21 |
| CN105829288B (zh) | 2019-01-15 |
| MX360983B (es) | 2018-11-22 |
| BR112016014115A8 (pt) | 2017-12-26 |
| BR112016014115A2 (ru) | 2017-08-08 |
| ES2666130T3 (es) | 2018-05-03 |
| IL246201A0 (en) | 2016-08-02 |
| JP2017500336A (ja) | 2017-01-05 |
| PL3083567T3 (pl) | 2018-08-31 |
| KR20160098503A (ko) | 2016-08-18 |
| US20170029411A1 (en) | 2017-02-02 |
| AU2014368619B2 (en) | 2018-11-22 |
| MX2016007991A (es) | 2016-10-07 |
| EP3083567A1 (en) | 2016-10-26 |
| TW201609641A (zh) | 2016-03-16 |
| US9624206B2 (en) | 2017-04-18 |
| MA39189A1 (fr) | 2017-06-30 |
| EP3083567B1 (en) | 2018-03-07 |
| CA2933604A1 (en) | 2015-06-25 |
| PH12016501102A1 (en) | 2016-07-11 |
| WO2015091741A1 (en) | 2015-06-25 |
| CL2016001524A1 (es) | 2017-01-27 |
| AR100032A1 (es) | 2016-09-07 |
| AU2014368619A1 (en) | 2016-07-28 |
| EA030730B1 (ru) | 2018-09-28 |
| JP6407288B2 (ja) | 2018-10-17 |
| SG11201605014YA (en) | 2016-07-28 |
| ZA201604968B (en) | 2018-11-28 |
| CN105829288A (zh) | 2016-08-03 |
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| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
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