TWI527818B - 三環旋轉酶抑制劑 - Google Patents
三環旋轉酶抑制劑 Download PDFInfo
- Publication number
- TWI527818B TWI527818B TW101108646A TW101108646A TWI527818B TW I527818 B TWI527818 B TW I527818B TW 101108646 A TW101108646 A TW 101108646A TW 101108646 A TW101108646 A TW 101108646A TW I527818 B TWI527818 B TW I527818B
- Authority
- TW
- Taiwan
- Prior art keywords
- compound
- amine
- group
- mmol
- ring
- Prior art date
Links
Classifications
-
- 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
- C07D487/02—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 two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- 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
- C07D487/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Epidemiology (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)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161453011P | 2011-03-15 | 2011-03-15 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TW201245200A TW201245200A (en) | 2012-11-16 |
| TWI527818B true TWI527818B (zh) | 2016-04-01 |
Family
ID=45879060
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW101108646A TWI527818B (zh) | 2011-03-15 | 2012-03-14 | 三環旋轉酶抑制劑 |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US9732083B2 (https=) |
| EP (1) | EP2686320B1 (https=) |
| JP (1) | JP6140083B2 (https=) |
| KR (2) | KR20140059164A (https=) |
| CN (1) | CN103562208B (https=) |
| AR (1) | AR085806A1 (https=) |
| AU (1) | AU2012229997B2 (https=) |
| BR (1) | BR112013023266B8 (https=) |
| CA (1) | CA2829939C (https=) |
| IL (1) | IL228220A (https=) |
| MX (1) | MX345780B (https=) |
| PH (1) | PH12013501800A1 (https=) |
| RU (1) | RU2626979C2 (https=) |
| TW (1) | TWI527818B (https=) |
| WO (1) | WO2012125746A1 (https=) |
| ZA (1) | ZA201307583B (https=) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2686320B1 (en) * | 2011-03-15 | 2016-05-18 | Merck Sharp & Dohme Corp. | Tricyclic gyrase inhibitors |
| EP2807165B1 (en) * | 2012-01-27 | 2019-05-15 | Université de Montréal | Pyrimido[4,5-b]indole derivatives and use thereof in the expansion of hematopoietic stem cells |
| CN105189505B (zh) * | 2012-09-12 | 2019-03-22 | 默克夏普&多梅有限公司 | 用作抗菌剂的三环促旋酶抑制剂 |
| CN103304488B (zh) * | 2013-06-13 | 2015-12-09 | 暨明医药科技（苏州）有限公司 | 光学纯2-（1-羟基乙基）-5-羟基嘧啶的制备方法 |
| CN105899511B (zh) * | 2013-09-11 | 2019-06-07 | 默沙东公司 | 三环促旋酶抑制剂 |
| US20170007615A1 (en) | 2014-02-03 | 2017-01-12 | Biota Europe Ltd | Antibacterial Compounds |
| WO2015150337A1 (en) * | 2014-04-01 | 2015-10-08 | Amakem Nv | Lim kinase inhibitors |
| CA3057431A1 (en) | 2017-03-24 | 2018-09-27 | Taisho Pharmaceutical Co., Ltd. | 2(1h)-quinolinone derivative |
| CN110475777B (zh) * | 2017-03-30 | 2022-04-15 | 豪夫迈·罗氏有限公司 | 用于治疗和预防细菌感染的新吡啶并[2,3-b]吲哚化合物 |
| CN108504647B (zh) * | 2018-03-09 | 2021-11-05 | 中山大学 | 一种dna促旋酶的药物结合口袋及其应用 |
| JP7296992B2 (ja) * | 2018-05-28 | 2023-06-23 | エフ． ホフマン－ラ ロシュ アーゲー | 細菌感染症の処置および予防のための新規オキソキノリジン化合物 |
| WO2020064661A1 (en) * | 2018-09-26 | 2020-04-02 | F. Hoffmann-La Roche Ag | Substituted pyridoindoles for the treatment and prophylaxis of bacterial infection |
| EP3887370B1 (en) * | 2018-11-27 | 2023-01-18 | F. Hoffmann-La Roche AG | Tricyclic compounds for the treatment and prophylaxis of bacterial infection |
| WO2020109191A1 (en) | 2018-11-27 | 2020-06-04 | F. Hoffmann-La Roche Ag | Aryl compounds for the treatment and prophylaxis of bacterial infection |
| WO2020127624A1 (en) | 2018-12-20 | 2020-06-25 | F. Hoffmann-La Roche Ag | Oxopyrido[1,2-a]pyrimidine compounds for the treatment and prophylaxis of bacterial infection |
| CN114763357B (zh) * | 2021-01-15 | 2024-06-18 | 中国科学院上海药物研究所 | 吲哚并嘧啶三环类化合物及其制备方法和用途 |
Family Cites Families (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IN157280B (https=) | 1983-07-15 | 1986-02-22 | Hoechst India | |
| CA1336090C (en) | 1988-08-31 | 1995-06-27 | Isao Hayakawa | Spiro-substituted cyclic amines of quinolone derivatives |
| DE4030059A1 (de) | 1990-09-22 | 1992-03-26 | Bayer Ag | Verfahren zur herstellung von 5-hydroxy-3,4,5,6-tetrahydro-pyrimidin-derivaten |
| DE4032560A1 (de) | 1990-10-13 | 1992-04-16 | Bayer Ag | 7-(2,7-diazabicyclo(3.3.0)octyl)-3-chinolon- und -naphtyridoncarbonsaeure-derivate |
| ES2150941T3 (es) | 1992-04-03 | 2000-12-16 | Upjohn Co | Aminas biciclicas-heterociclicas eficaces farmaceuticamente. |
| US5279359A (en) | 1992-06-26 | 1994-01-18 | Erickson Donald C | Rotary trisorption heat pump |
| US5350791A (en) | 1992-07-02 | 1994-09-27 | Henkel Corporation | Hydrophilicizing treatment for metal objects |
| US5527910A (en) | 1992-12-30 | 1996-06-18 | Cheil Foods & Chemicals, Inc. | Pyridone carboxylic acid compounds and their uses for treating infectious diseases caused by bacteria |
| RU2158127C2 (ru) * | 1994-12-23 | 2000-10-27 | Варнер-Ламберт Компани | Способы ингибирования тирозинкиназы рецептора эпидермального фактора роста, азотсодержащие трициклические соединения, фармацевтическая композиция, предназначенная для введения ингибитора тирозинкиназы рецептора эпидермального фактора роста, например, erb-b2, erb-b3 или erb-b4, и противозачаточная композиция |
| NZ304519A (en) | 1995-03-02 | 2000-01-28 | Upjohn Co | Pydrimido[4,5-b]indoles |
| SI9620103A (sl) * | 1995-07-06 | 1998-10-31 | Novartis Ag | Pirolopirimidini in postopki za njihovo pripravo |
| WO1998029397A1 (en) | 1996-12-27 | 1998-07-09 | Yoshitomi Pharmaceutical Industries, Ltd. | Fused pyrimidine compounds and medicinal use thereof |
| SI0964865T1 (en) | 1997-01-08 | 2003-08-31 | Pharmacia & Upjohn Company | Pharmaceutically active tricyclic amines |
| ATE265847T1 (de) | 1997-07-29 | 2004-05-15 | Upjohn Co | Selbstemulgierbare formulierung enthaltend lipophile verbindungen |
| US6147085A (en) | 1999-04-01 | 2000-11-14 | Neurogen Corporation | Aminoalkyl substituted 9H-pyridino[2,3-b] indole and 9H-pyrimidino[4,5-b] indole derivatives |
| EP1068207A1 (en) | 1998-04-02 | 2001-01-17 | Neurogen Corporation | AMINOALKYL SUBSTITUTED 9H-PYRIDINO 2,3-b]INDOLE AND 9H-PYRIMIDINO 4,5-b]INDOLE DERIVATIVES |
| US6221875B1 (en) | 1998-04-02 | 2001-04-24 | Neurogen Corporation | Substituted 9H-pyridino [2,3-B]indole and 9H-pyrimidino [4,5-B]indole derivatives: selective neuropeptide Y receptor ligands |
| JP2000038350A (ja) | 1998-05-18 | 2000-02-08 | Yoshitomi Pharmaceut Ind Ltd | 糖尿病治療薬 |
| WO2000066585A1 (en) | 1999-04-30 | 2000-11-09 | Neurogen Corporation | 9H-PYRIMIDO[4,5-b]INDOLE DERIVATIVES: CRF1 SPECIFIC LIGANDS |
| SK10572002A3 (sk) | 2000-01-24 | 2003-10-07 | Warner-Lambert Company | 3-Aminochinazolín-2,4-diónové antibakteriálne činidlá |
| FR2816509B1 (fr) | 2000-11-15 | 2004-02-06 | Sod Conseils Rech Applic | Association d'inhibiteurs de calpaine et de piegeurs des formes reactives de l'oxygene |
| JP2005515173A (ja) | 2001-10-31 | 2005-05-26 | バイエル・ヘルスケア・アクチェンゲゼルシャフト | ピリミド［４，５−ｂ］インドール誘導体 |
| CA2466266A1 (en) * | 2001-11-08 | 2003-07-31 | Antex Pharma, Inc. | Novel substituted alkane compounds and uses thereof |
| WO2003057149A2 (en) | 2001-12-28 | 2003-07-17 | Bayer Corporation | 4-substituted fused heteropyrimidines and fused hetero-4-pyrimidones |
| TWI270549B (en) | 2002-12-26 | 2007-01-11 | Taisho Pharmaceutical Co Ltd | Pyrrolopyrimidine and pyrrolopyridine derivatives substituted with cyclic amino group |
| WO2004058764A1 (en) * | 2002-12-27 | 2004-07-15 | Bayer Healthcare Ag | 4-phenyl-pyrimido [4,5-b] indole derivatives |
| JP4845736B2 (ja) | 2003-10-14 | 2011-12-28 | アリゾナ ボード オブ リージェンツ オン ビハーフ ザ ユニバーシティー オブ アリゾナ | プロテインキナーゼ阻害剤 |
| US20090143399A1 (en) | 2003-10-14 | 2009-06-04 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Protein Kinase Inhibitors |
| US20080051414A1 (en) | 2003-10-14 | 2008-02-28 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Protein Kinase Inhibitors |
| US20090099165A1 (en) | 2003-10-14 | 2009-04-16 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Protein Kinase Inhibitors |
| JP2006036762A (ja) | 2004-06-25 | 2006-02-09 | Taisho Pharmaceut Co Ltd | 環状アミノ基で置換されているピロロピリミジン及びピロロピリジン誘導体 |
| JP2007161585A (ja) | 2004-06-25 | 2007-06-28 | Taisho Pharmaceut Co Ltd | 環状アミノ基で置換されているピロロピリミジン及びピロロピリジン誘導体 |
| WO2008007113A2 (en) | 2006-07-14 | 2008-01-17 | Astex Therapeutics Limited | Pharmaceutical combinations |
| CA2604284A1 (en) | 2005-04-28 | 2006-11-02 | Supergen, Inc. | Protein kinase inhibitors |
| EP1749822B1 (en) * | 2005-08-05 | 2008-10-15 | Hybrigenics S.A. | Novel cysteine protease inhibitors and their therapeutic applications |
| US20070049591A1 (en) | 2005-08-25 | 2007-03-01 | Kalypsys, Inc. | Inhibitors of MAPK/Erk Kinase |
| JP2007169216A (ja) | 2005-12-22 | 2007-07-05 | Taisho Pharmaceut Co Ltd | 環状アミノ基で置換されているピロロピリミジン及びピロロピリジン誘導体 |
| US20080207632A1 (en) | 2006-10-31 | 2008-08-28 | Supergen, Inc. | Protein kinase inhibitors |
| US8618121B2 (en) | 2007-07-02 | 2013-12-31 | Cancer Research Technology Limited | 9H-pyrimido[4,5-B]indoles, 9H-pyrido[4',3':4,5]pyrrolo[2,3-D]pyridines, and 9H 1,3,6,9 tetraaza-fluorenes as CHK1 kinase function inhibitors |
| US7982035B2 (en) | 2007-08-27 | 2011-07-19 | Duquesne University Of The Holy Spirit | Tricyclic compounds having antimitotic and/or antitumor activity and methods of use thereof |
| US7960400B2 (en) * | 2007-08-27 | 2011-06-14 | Duquesne University Of The Holy Ghost | Tricyclic compounds having cytostatic and/or cytotoxic activity and methods of use thereof |
| WO2009091476A1 (en) | 2008-01-14 | 2009-07-23 | Irm Llc | Compositions and methods for treating cancers |
| ATE546448T1 (de) * | 2008-08-02 | 2012-03-15 | Janssen Pharmaceutica Nv | Urotensin-ii-rezeptorantagonisten |
| WO2011056739A1 (en) | 2009-11-03 | 2011-05-12 | Glaxosmithkline Llc | Compounds and methods |
| EP2686320B1 (en) * | 2011-03-15 | 2016-05-18 | Merck Sharp & Dohme Corp. | Tricyclic gyrase inhibitors |
| CN105189505B (zh) * | 2012-09-12 | 2019-03-22 | 默克夏普&多梅有限公司 | 用作抗菌剂的三环促旋酶抑制剂 |
| CN105899511B (zh) * | 2013-09-11 | 2019-06-07 | 默沙东公司 | 三环促旋酶抑制剂 |
| WO2016067009A1 (en) * | 2014-10-28 | 2016-05-06 | Redx Pharma Plc | Compounds with activity against bacteria and mycobacteria |
-
2012
- 2012-03-14 EP EP12710633.4A patent/EP2686320B1/en active Active
- 2012-03-14 RU RU2013140798A patent/RU2626979C2/ru active
- 2012-03-14 CN CN201280020849.4A patent/CN103562208B/zh active Active
- 2012-03-14 AR ARP120100830A patent/AR085806A1/es active IP Right Grant
- 2012-03-14 US US13/496,188 patent/US9732083B2/en active Active
- 2012-03-14 JP JP2013558143A patent/JP6140083B2/ja active Active
- 2012-03-14 KR KR1020137026970A patent/KR20140059164A/ko not_active Ceased
- 2012-03-14 KR KR1020197025342A patent/KR102132574B1/ko active Active
- 2012-03-14 WO PCT/US2012/029104 patent/WO2012125746A1/en not_active Ceased
- 2012-03-14 BR BR112013023266A patent/BR112013023266B8/pt active IP Right Grant
- 2012-03-14 PH PH1/2013/501800A patent/PH12013501800A1/en unknown
- 2012-03-14 CA CA2829939A patent/CA2829939C/en active Active
- 2012-03-14 MX MX2013010511A patent/MX345780B/es active IP Right Grant
- 2012-03-14 TW TW101108646A patent/TWI527818B/zh active
- 2012-03-14 AU AU2012229997A patent/AU2012229997B2/en active Active
-
2013
- 2013-09-01 IL IL228220A patent/IL228220A/en active IP Right Grant
- 2013-10-11 ZA ZA2013/07583A patent/ZA201307583B/en unknown
-
2017
- 2017-07-07 US US15/643,760 patent/US10858360B2/en active Active
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