AR071222A1 - Compuestos heterociclicos espirocondensados - Google Patents
Compuestos heterociclicos espirocondensadosInfo
- Publication number
- AR071222A1 AR071222A1 ARP090101487A ARP090101487A AR071222A1 AR 071222 A1 AR071222 A1 AR 071222A1 AR P090101487 A ARP090101487 A AR P090101487A AR P090101487 A ARP090101487 A AR P090101487A AR 071222 A1 AR071222 A1 AR 071222A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- methyl
- spiro
- plasmodium
- indole
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/20—Spiro-condensed systems
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
- A61P33/06—Antimalarials
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
- C07D487/20—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Tropical Medicine & Parasitology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Los compuestos son utiles en el tratamiento y/o la prevencion de infecciones tales como aquéllas causadas por Plasmodium falciparum, Plasmodium vivax, Plasmodium malariae, Plasmodium ovale, Trypanosoma cruzi y parásitos del género Leishmania, tales como, por ejemplo, Leishmania donovani. La solicitud también se refiere a composiciones farmacéuticas que contienen los compuestos, así como el uso del compuesto para la preparacion de medicamentos. Reivindicacion 1: Un compuesto de la formula (1), o una sal farmacéuticamente aceptable, éster o pro-fármaco del mismo: en donde m es 1 o 2; R1 es H, halogeno, alquilo, halo-alquilo, alcoxilo, amina o arilo opcionalmente sustituido con uno o más sustituyentes; R2 es H, alquilo, aril-alquilo o alcoxi-carbonilo; R3 es H o alquilo; R4 es H, alquilo, hidroxi-alquilo, -COOD, en donde D es un grupo alquilo, o R3 y R4 forman parte de un anillo heterocíclico; R5 es H o alquilo; n es 1, 2 o 3; y A y B se fusionan con, y forman parte de, un areno o heteroareno monocíclico o policíclico insustituido o sustituido; en el entendido de que, si A y B se fusionan con las posiciones 2 y 3 de un indol insustituido, n es 1 o 2, R2 y R3 son H, m es 1, y R1 está en la posicion 6 del espiro-oxindol, entonces, R1, R4 y R5 no son todos H; o si R1 es H, entonces R4 no es metilo cuando R5 es H, y R5 no es metilo cuando R4 es H; o si R1 es Br, entonces R4 y R5 no son ambos H, y R4 no es metilo cuando R5 es H; y R5 no es metilo cuando R4 es H. Reivindicacion 11: (1R,3S)-5',7-dicloro-6-fluoro-3-metil-2,3,4,9-tetrahidro-espiro-[beta-carbolin-1,3'-indol-2'(1'H)-ona. Reivindicacion 12: (1R,3S)-5'-cloro-6-fluoro-3-metil-2,3,4,9-tetrahidro-espiro-[beta-carbolin-1,3'-indol-2'(1'H)-ona.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08155342 | 2008-04-29 | ||
| EP09151117 | 2009-01-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR071222A1 true AR071222A1 (es) | 2010-06-02 |
Family
ID=40613087
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090101487A AR071222A1 (es) | 2008-04-29 | 2009-04-27 | Compuestos heterociclicos espirocondensados |
Country Status (31)
| Country | Link |
|---|---|
| US (2) | US8053442B2 (es) |
| EP (2) | EP2722333A1 (es) |
| JP (2) | JP5438098B2 (es) |
| KR (1) | KR101390081B1 (es) |
| CN (1) | CN102015711B (es) |
| AR (1) | AR071222A1 (es) |
| AU (1) | AU2009242279B2 (es) |
| BR (1) | BRPI0911577B8 (es) |
| CA (1) | CA2719365C (es) |
| CL (1) | CL2009001007A1 (es) |
| CO (1) | CO6300940A2 (es) |
| CY (1) | CY1114874T1 (es) |
| DK (1) | DK2285808T3 (es) |
| EA (1) | EA019601B1 (es) |
| EC (2) | ECSP10010646A (es) |
| ES (1) | ES2447590T3 (es) |
| HK (1) | HK1149935A1 (es) |
| HR (1) | HRP20140151T1 (es) |
| IL (1) | IL208357A (es) |
| JO (1) | JO2904B1 (es) |
| MA (1) | MA32316B1 (es) |
| MX (1) | MX2010011868A (es) |
| MY (2) | MY156601A (es) |
| NZ (1) | NZ588217A (es) |
| PE (1) | PE20091787A1 (es) |
| PL (1) | PL2285808T3 (es) |
| PT (1) | PT2285808E (es) |
| SI (1) | SI2285808T1 (es) |
| TW (1) | TWI442921B (es) |
| WO (1) | WO2009132921A1 (es) |
| ZA (1) | ZA201006752B (es) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2010011868A (es) * | 2008-04-29 | 2010-11-26 | Novartis Ag | Derivados de espiro-indol para el tratamiento de enfermedades parasitarias. |
| CN102584835B (zh) * | 2011-01-17 | 2014-08-27 | 苏州大学 | 一种含吲哚结构的螺杂环化合物及其制备方法 |
| US9139821B2 (en) | 2012-03-23 | 2015-09-22 | Codexis, Inc. | Biocatalysts and methods for synthesizing derivatives of tryptamine and tryptamine analogs |
| EP2828256B1 (en) | 2012-03-23 | 2019-07-03 | Novartis AG | Chemical process for preparing spiroindolones and intermediates thereof |
| CN104185634B (zh) * | 2012-03-23 | 2017-05-03 | 诺华股份有限公司 | 制备螺旋吲哚酮和其中间体的化学工艺 |
| WO2015073555A1 (en) | 2013-11-13 | 2015-05-21 | Codexis, Inc. | Engineered imine reductases and methods for the reductive amination of ketone and amine compounds |
| JP6719463B2 (ja) | 2014-11-25 | 2020-07-15 | コデクシス， インコーポレイテッド | ケトン化合物およびアミン化合物の還元的アミノ化のための操作されたイミンレダクターゼおよび方法 |
| CR20170250A (es) | 2014-12-18 | 2017-07-19 | Hoffmann La Roche | TETRAHIDRO-PIRIDO[3,4-b]INDOLES MODULADORES DE RECEPTORES DE ESTRÓGENOS Y USOS DE LOS MISMOS |
| EA032763B1 (ru) * | 2015-01-23 | 2019-07-31 | Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед | ПРОИЗВОДНОЕ ПИРАЗОЛО[3,4-d]ПИРИМИДИНА И ЕГО ПРИМЕНЕНИЕ ПРИ ЛЕЧЕНИИ ЛЕЙШМАНИОЗА |
| WO2016147205A1 (en) * | 2015-03-13 | 2016-09-22 | Council Of Scientific & Industrial Research | Novel substituted 3-spirophosphoryl pyrazole-2-oxindoles as anti-infectives and process for the synthesis thereof |
| WO2016201440A1 (en) * | 2015-06-12 | 2016-12-15 | The Regents Of The University Of California | Spiroindolinones and therapeutic uses thereof |
| JP2017024992A (ja) * | 2015-07-15 | 2017-02-02 | 公益財団法人微生物化学研究会 | 化合物の製造方法 |
| HRP20230859T1 (hr) | 2018-06-21 | 2023-11-10 | F. Hoffmann - La Roche Ag | Kruti oblici soli tartarata 3-((1r,3r)-1-(2,6-difluoro-4-((1-(3-fluoropropil)azetidin-3-il)amino)fenil)-3-metil-1,3,4,9-tetrahidro-2hpirido[3,4-b]indol-2-il)-2,2-difluoropropan-1-ol, postupak njihove proizvodnje i postupci njihove primjene u liječenju raka |
| CN110590795B (zh) * | 2019-10-10 | 2021-01-22 | 贵州省中国科学院天然产物化学重点实验室(贵州医科大学天然产物化学重点实验室) | 一类多并杂环螺羟吲哚类化合物的合成方法 |
| WO2021186348A1 (en) * | 2020-03-17 | 2021-09-23 | The University Of Buea | Dihydro-spiro[indoline-3:1'-isoquinolin]-2-ones as antimalarial agents |
| CN116273188B (zh) * | 2023-03-01 | 2024-06-25 | 岭南师范学院 | 一种负载金属的多孔有机框架材料在催化Pictet-Spengler反应中的应用 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2663935A1 (fr) * | 1990-06-27 | 1992-01-03 | Adir | Nouveaux 1,2,3,4,5,6-hexahydroazepino [4,5-b] indoles et 1,2,3,4-tetrahydrobethacarbolines, leurs procedes de preparation et les compositions pharmaceutiques qui les contiennent. |
| AU765860B2 (en) * | 1998-07-14 | 2003-10-02 | Hong Kong University Of Science And Technology, The | Antiparasitic artemisinin derivatives (endoperoxides) |
| EA004500B1 (ru) | 1998-12-19 | 2004-04-29 | Янссен Фармацевтика Н.В. | Антигистаминные спиросоединения |
| US20050101623A1 (en) * | 2003-07-23 | 2005-05-12 | Pharmacia Corporation | Beta-carboline compounds and analogues thereof as mitogen-activated protein kinase-activated protein kinase-2 inhibitors |
| MY145694A (en) | 2005-04-11 | 2012-03-30 | Xenon Pharmaceuticals Inc | Spiroheterocyclic compounds and their uses as therapeutic agents |
| KR101050568B1 (ko) | 2006-12-07 | 2011-07-19 | 에프. 호프만-라 로슈 아게 | Ｖ1ａ 수용체 길항제로서의 스피로-피페리딘 유도체 |
| JP2011507910A (ja) * | 2007-12-21 | 2011-03-10 | ユニバーシティー オブ ロチェスター | 真核生物の寿命を変更するための方法 |
| ES2403284T3 (es) | 2008-01-09 | 2013-05-17 | Array Biopharma, Inc. | Pirimidil ciclopentanos como inhibidores de la proteína quinasa AKT |
| MX2010011868A (es) * | 2008-04-29 | 2010-11-26 | Novartis Ag | Derivados de espiro-indol para el tratamiento de enfermedades parasitarias. |
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2009
- 2009-04-01 MX MX2010011868A patent/MX2010011868A/es active IP Right Grant
- 2009-04-01 CN CN2009801149364A patent/CN102015711B/zh active Active
- 2009-04-01 EP EP13185962.1A patent/EP2722333A1/en not_active Withdrawn
- 2009-04-01 AU AU2009242279A patent/AU2009242279B2/en active Active
- 2009-04-01 ES ES09737965.5T patent/ES2447590T3/es active Active
- 2009-04-01 EP EP09737965.5A patent/EP2285808B1/en active Active
- 2009-04-01 SI SI200930847T patent/SI2285808T1/sl unknown
- 2009-04-01 DK DK09737965.5T patent/DK2285808T3/da active
- 2009-04-01 MY MYPI2013001071A patent/MY156601A/en unknown
- 2009-04-01 NZ NZ588217A patent/NZ588217A/xx unknown
- 2009-04-01 JP JP2011506638A patent/JP5438098B2/ja active Active
- 2009-04-01 EA EA201001689A patent/EA019601B1/ru not_active IP Right Cessation
- 2009-04-01 MY MYPI20104473 patent/MY152021A/en unknown
- 2009-04-01 CA CA2719365A patent/CA2719365C/en active Active
- 2009-04-01 BR BRPI0911577A patent/BRPI0911577B8/pt active IP Right Grant
- 2009-04-01 WO PCT/EP2009/053902 patent/WO2009132921A1/en active Application Filing
- 2009-04-01 PL PL09737965T patent/PL2285808T3/pl unknown
- 2009-04-01 PT PT97379655T patent/PT2285808E/pt unknown
- 2009-04-01 KR KR1020107026548A patent/KR101390081B1/ko active IP Right Grant
- 2009-04-27 AR ARP090101487A patent/AR071222A1/es active IP Right Grant
- 2009-04-27 US US12/430,625 patent/US8053442B2/en active Active
- 2009-04-28 JO JO2009149A patent/JO2904B1/en active
- 2009-04-28 TW TW098114086A patent/TWI442921B/zh active
- 2009-04-28 PE PE2009000577A patent/PE20091787A1/es active IP Right Grant
- 2009-04-28 CL CL2009001007A patent/CL2009001007A1/es unknown
-
2010
- 2010-09-21 ZA ZA2010/06752A patent/ZA201006752B/en unknown
- 2010-09-21 IL IL208357A patent/IL208357A/en active IP Right Grant
- 2010-11-19 MA MA33365A patent/MA32316B1/fr unknown
- 2010-11-25 CO CO10148514A patent/CO6300940A2/es active IP Right Grant
- 2010-11-29 EC EC2010010646A patent/ECSP10010646A/es unknown
-
2011
- 2011-04-27 HK HK11104203.2A patent/HK1149935A1/xx unknown
- 2011-07-19 US US13/186,035 patent/US8399453B2/en active Active
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2013
- 2013-12-12 JP JP2013257004A patent/JP2014065729A/ja active Pending
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2014
- 2014-02-18 HR HRP20140151AT patent/HRP20140151T1/hr unknown
- 2014-02-20 CY CY20141100135T patent/CY1114874T1/el unknown
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2017
- 2017-10-13 EC ECIEPI201768127A patent/ECSP17068127A/es unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration |