MX2016007991A - Derivados antibacteriales de 1h-indazol y 1h-indol. - Google Patents
Derivados antibacteriales de 1h-indazol y 1h-indol.Info
- Publication number
- MX2016007991A MX2016007991A MX2016007991A MX2016007991A MX2016007991A MX 2016007991 A MX2016007991 A MX 2016007991A MX 2016007991 A MX2016007991 A MX 2016007991A MX 2016007991 A MX2016007991 A MX 2016007991A MX 2016007991 A MX2016007991 A MX 2016007991A
- Authority
- MX
- Mexico
- Prior art keywords
- cycloprop
- hydroxymethyl
- halogen
- azetidin
- hydroxyalkyl
- Prior art date
Links
- 230000000844 anti-bacterial effect Effects 0.000 title abstract 2
- BNIFVTPIXGUZCU-UHFFFAOYSA-N 1h-indazole Chemical compound C1=CC=C2C=NNC2=C1.C1=CC=C2C=NNC2=C1 BNIFVTPIXGUZCU-UHFFFAOYSA-N 0.000 title 1
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical class C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 title 1
- -1 trifluoromethoxy, amino Chemical group 0.000 abstract 15
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 150000002367 halogens Chemical class 0.000 abstract 4
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000004567 azetidin-3-yl group Chemical group N1CC(C1)* 0.000 abstract 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 2
- 125000005083 alkoxyalkoxy group Chemical group 0.000 abstract 1
- 125000005133 alkynyloxy group Chemical group 0.000 abstract 1
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004990 dihydroxyalkyl group Chemical group 0.000 abstract 1
- 125000000816 ethylene group Chemical group [H]C([H])([*:1])C([H])([H])[*:2] 0.000 abstract 1
- 125000005113 hydroxyalkoxy group Chemical group 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000004287 oxazol-2-yl group Chemical group [H]C1=C([H])N=C(*)O1 0.000 abstract 1
- 125000006299 oxetan-3-yl group Chemical group [H]C1([H])OC([H])([H])C1([H])* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000005309 thioalkoxy group Chemical group 0.000 abstract 1
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
- A61K31/40—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
-
- 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
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)
Abstract
La invención se refiere a compuestos antibacterianos de la fórmula I (ver Fórmula) en donde X es N o CH; R1 es H o halógeno; R2 es alquiniloxi o el grupo M; R3 es H o halógeno; M es uno de los grupos MA y MB representados a continuación (ver Fórmula) en donde A es un enlace, CH2CH2, CH=CH o C?C; R1A es H o halógeno; R2A es H, alcoxi o halógeno; R3A es H, alcoxi, hidroxialcoxi, alcoxialcoxi, tioalcoxi, trifluorometoxi, amino, hidroxialquilo, 2-hidroxiacetamido, 1-aminociclopropilo, 1-hidroximetil-cicloprop- 1-ilo, 1-((fosfonooxi)metil)ciclopropilo, 1-(((dimetilglicil)oxi)m etil)ciclopropilo, trans-2-hidroximetil-cicloprop-1-ilo, 1,2-dihidroxietilo, 3-hidroxioxetan-3-ilo, 3-(hidroxialquil)oxetan -3-ilo, 3-aminooxetan-3-ilo, 3-hidroxitietan-3-ilo, morfolin-4-ilalcoxi, morfolin-4-il-alquilo, oxazol-2-ilo o [1,2,3]triazol-2-ilo; y R1B es hidroxialquilo, dihidroxialquilo, aminoalquilo, 1-hidroximetil-cicloprop-1-ilo, 1-aminometil-cicloprop-1-ilo, trans-2-hidroximetil-cicloprop-1-ilo , 3-hidroxioxetan-3-ilo, 3-hidroxitietan-3ilo, 1-(2-hidroxiacetil)azetidin-3-ilo, 1-(2-aminoacetil)azetidin-3-ilo , 1-glicilazetidin-3-ilo, 1-(2-amino-2-metilpropanoil)azetidin-3-i lo, 3-(2-aminoacetamido)ciclopentilo, trans-(cis-3,4-dihidroxi)-ci clopent-1-ilo o 3-hidroximetilbiciclo[1,1,1]pentan-1-ilo; y sales de los mismos.
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 |
|---|---|
| MX2016007991A true MX2016007991A (es) | 2016-10-07 |
| MX360983B MX360983B (es) | 2018-11-22 |
Family
ID=49880464
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2016007991A MX360983B (es) | 2013-12-19 | 2014-12-18 | Derivados antibacterianos de 1h-indazol y 1h-indol. |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US9624206B2 (es) |
| EP (1) | EP3083567B1 (es) |
| JP (1) | JP6407288B2 (es) |
| KR (1) | KR20160098503A (es) |
| CN (1) | CN105829288B (es) |
| AR (1) | AR100032A1 (es) |
| AU (1) | AU2014368619B2 (es) |
| BR (1) | BR112016014115A8 (es) |
| CA (1) | CA2933604A1 (es) |
| CL (1) | CL2016001524A1 (es) |
| EA (1) | EA030730B1 (es) |
| ES (1) | ES2666130T3 (es) |
| IL (1) | IL246201A0 (es) |
| MA (1) | MA39189A1 (es) |
| MX (1) | MX360983B (es) |
| PH (1) | PH12016501102A1 (es) |
| PL (1) | PL3083567T3 (es) |
| SG (1) | SG11201605014YA (es) |
| TR (1) | TR201807881T4 (es) |
| TW (1) | TW201609641A (es) |
| WO (1) | WO2015091741A1 (es) |
| ZA (1) | ZA201604968B (es) |
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 |
| US9796686B2 (en) | 2014-05-16 | 2017-10-24 | Idorsia Pharmaceuticals Ltd | Antibacterial quinazoline-4(3H)-one derivatives |
| BR112017010474A2 (pt) | 2014-11-19 | 2017-12-26 | Actelion Pharmaceuticals Ltd | derivados antibacterianos de benzotiazol |
| 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 |
| BR112018073580A2 (pt) * | 2016-05-17 | 2019-03-19 | Idorsia Pharmaceuticals Ltd | derivados de 6-(buta-1,3-diyn-1-il) benzo [d] tiazol |
| WO2018216822A1 (en) | 2017-05-25 | 2018-11-29 | Taisho Pharmaceutical Co., Ltd. | Novel imidazole derivatives |
| 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 |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003077914A1 (en) | 2002-03-13 | 2003-09-25 | Array Biopharma, Inc | 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 |
| EP1809282B1 (en) | 2004-10-18 | 2013-01-09 | Amgen, Inc | Thiadiazole compounds and methods of use |
| BRPI0609719B8 (pt) | 2005-03-23 | 2021-05-25 | Hoffmann La Roche | derivados de acetilenil-pirazol-pirimidina como antagonistas de mgbur2 |
| CA2691987C (en) | 2007-06-12 | 2016-08-16 | Achaogen, Inc. | Antibacterial agents |
| EP2432468A2 (en) | 2009-05-20 | 2012-03-28 | Ardea Biosciences, Inc. | Methods of modulating uric acid levels |
| EP2488489A2 (en) * | 2009-10-13 | 2012-08-22 | Pfizer Inc. | C-linked hydroxamic acid derivatives useful as antibacterial agents |
| US8664401B2 (en) | 2009-12-16 | 2014-03-04 | Pfizer Inc. | 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 |
| EP2638006A1 (en) | 2010-11-10 | 2013-09-18 | Achaogen, Inc. | Hydroxamic acid derivatives and their use in the treatment of bacterial infections |
| EP2661438A4 (en) | 2011-01-03 | 2014-06-11 | Hanmi Pharm Ind Co Ltd | NEW BICYCLIC COMPOUND FOR MODULATING G-PROTEIN-COUPLED RECEPTORS |
| MA34963B1 (fr) * | 2011-03-07 | 2014-03-01 | Pfizer | Derives de fluoro-pyridinone utiles en tant qu'agents antibacteriens |
| CA2830866A1 (en) * | 2011-04-08 | 2012-10-11 | Pfizer Inc. | Imidazole, pyrazole, and triazole derivatives useful as antibacterial agents |
| JP2014510132A (ja) | 2011-04-08 | 2014-04-24 | ファイザー・インク | 抗菌剤として有用なイソオキサゾール誘導体 |
| EP2847162A1 (en) | 2012-05-09 | 2015-03-18 | Achaogen, Inc. | Antibacterial agents |
| EP2847168A1 (en) | 2012-05-10 | 2015-03-18 | 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 |
| US9796686B2 (en) | 2014-05-16 | 2017-10-24 | Idorsia Pharmaceuticals Ltd | Antibacterial quinazoline-4(3H)-one derivatives |
-
2014
- 2014-12-18 US US15/106,790 patent/US9624206B2/en not_active Expired - Fee Related
- 2014-12-18 SG SG11201605014YA patent/SG11201605014YA/en unknown
- 2014-12-18 TW TW103144395A patent/TW201609641A/zh unknown
- 2014-12-18 ES ES14812752.5T patent/ES2666130T3/es active Active
- 2014-12-18 CN CN201480067976.9A patent/CN105829288B/zh not_active Expired - Fee Related
- 2014-12-18 CA CA2933604A patent/CA2933604A1/en not_active Abandoned
- 2014-12-18 BR BR112016014115A patent/BR112016014115A8/pt not_active Application Discontinuation
- 2014-12-18 TR TR2018/07881T patent/TR201807881T4/tr unknown
- 2014-12-18 PL PL14812752T patent/PL3083567T3/pl unknown
- 2014-12-18 AU AU2014368619A patent/AU2014368619B2/en not_active Ceased
- 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
- 2014-12-18 WO PCT/EP2014/078384 patent/WO2015091741A1/en not_active Ceased
- 2014-12-18 EP EP14812752.5A patent/EP3083567B1/en not_active Not-in-force
- 2014-12-18 KR KR1020167019669A patent/KR20160098503A/ko not_active Ceased
- 2014-12-18 AR ARP140104742A patent/AR100032A1/es unknown
- 2014-12-18 MA MA39189A patent/MA39189A1/fr unknown
- 2014-12-18 EA EA201600475A patent/EA030730B1/ru not_active IP Right Cessation
-
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 |
|---|---|
| AU2014368619B2 (en) | 2018-11-22 |
| AR100032A1 (es) | 2016-09-07 |
| US9624206B2 (en) | 2017-04-18 |
| CA2933604A1 (en) | 2015-06-25 |
| ES2666130T3 (es) | 2018-05-03 |
| JP2017500336A (ja) | 2017-01-05 |
| SG11201605014YA (en) | 2016-07-28 |
| TW201609641A (zh) | 2016-03-16 |
| PH12016501102A1 (en) | 2016-07-11 |
| EP3083567A1 (en) | 2016-10-26 |
| JP6407288B2 (ja) | 2018-10-17 |
| EP3083567B1 (en) | 2018-03-07 |
| WO2015091741A1 (en) | 2015-06-25 |
| EA030730B1 (ru) | 2018-09-28 |
| BR112016014115A2 (es) | 2017-08-08 |
| MA39189A1 (fr) | 2017-06-30 |
| BR112016014115A8 (pt) | 2017-12-26 |
| MX360983B (es) | 2018-11-22 |
| AU2014368619A1 (en) | 2016-07-28 |
| CN105829288B (zh) | 2019-01-15 |
| CL2016001524A1 (es) | 2017-01-27 |
| ZA201604968B (en) | 2018-11-28 |
| TR201807881T4 (tr) | 2018-06-21 |
| EA201600475A1 (ru) | 2016-11-30 |
| KR20160098503A (ko) | 2016-08-18 |
| US20170029411A1 (en) | 2017-02-02 |
| IL246201A0 (en) | 2016-08-02 |
| PL3083567T3 (pl) | 2018-08-31 |
| CN105829288A (zh) | 2016-08-03 |
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