AR092538A1 - Inhibidores de girasa triciclica - Google Patents
Inhibidores de girasa triciclicaInfo
- Publication number
- AR092538A1 AR092538A1 ARP130103259A ARP130103259A AR092538A1 AR 092538 A1 AR092538 A1 AR 092538A1 AR P130103259 A ARP130103259 A AR P130103259A AR P130103259 A ARP130103259 A AR P130103259A AR 092538 A1 AR092538 A1 AR 092538A1
- Authority
- AR
- Argentina
- Prior art keywords
- membered
- optionally substituted
- substituent
- formula
- heteroaryl ring
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 125000001424 substituent group Chemical group 0.000 abstract 27
- 229910052760 oxygen Inorganic materials 0.000 abstract 19
- 229910052717 sulfur Inorganic materials 0.000 abstract 19
- 230000002452 interceptive effect Effects 0.000 abstract 14
- 125000003118 aryl group Chemical group 0.000 abstract 13
- 125000001072 heteroaryl group Chemical group 0.000 abstract 13
- 239000000651 prodrug Substances 0.000 abstract 13
- 229940002612 prodrug Drugs 0.000 abstract 13
- 150000001875 compounds Chemical class 0.000 abstract 12
- 125000005842 heteroatom Chemical group 0.000 abstract 11
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 6
- 150000003839 salts Chemical class 0.000 abstract 6
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 4
- 125000006163 5-membered heteroaryl group Chemical group 0.000 abstract 4
- 125000004429 atom Chemical group 0.000 abstract 4
- 229910052757 nitrogen Inorganic materials 0.000 abstract 4
- 125000001183 hydrocarbyl group Chemical group 0.000 abstract 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical group [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 150000001412 amines Chemical class 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 150000002148 esters Chemical class 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 150000003141 primary amines Chemical class 0.000 abstract 2
- 150000003335 secondary amines Chemical class 0.000 abstract 2
- 150000003512 tertiary amines Chemical class 0.000 abstract 2
- NAWXUBYGYWOOIX-SFHVURJKSA-N (2s)-2-[[4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]benzoyl]amino]-4-methylidenepentanedioic acid Chemical compound C1=CC2=NC(N)=NC(N)=C2C=C1CCC1=CC=C(C(=O)N[C@@H](CC(=C)C(O)=O)C(O)=O)C=C1 NAWXUBYGYWOOIX-SFHVURJKSA-N 0.000 abstract 1
- 241000894006 Bacteria Species 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 108010054814 DNA Gyrase Proteins 0.000 abstract 1
- 101100073357 Streptomyces halstedii sch2 gene Proteins 0.000 abstract 1
- 150000001721 carbon Chemical group 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 125000000816 ethylene group Chemical group [H]C([H])([*:1])C([H])([H])[*:2] 0.000 abstract 1
- 239000002271 gyrase inhibitor Substances 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 125000005647 linker group Chemical group 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000004434 sulfur atom Chemical group 0.000 abstract 1
Classifications
-
- 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
-
- 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
- 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
-
- 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
- C07D487/16—Peri-condensed systems
-
- 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
- C07D487/22—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 four or more hetero rings
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D515/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D515/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Communicable Diseases (AREA)
- Pharmacology & Pharmacy (AREA)
- Oncology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261700159P | 2012-09-12 | 2012-09-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR092538A1 true AR092538A1 (es) | 2015-04-22 |
Family
ID=49226575
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP130103259A AR092538A1 (es) | 2012-09-12 | 2013-09-12 | Inhibidores de girasa triciclica |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US10865216B2 (enExample) |
| EP (1) | EP2895488B1 (enExample) |
| JP (1) | JP6460991B2 (enExample) |
| CN (1) | CN105189505B (enExample) |
| AR (1) | AR092538A1 (enExample) |
| TW (1) | TWI639602B (enExample) |
| WO (1) | WO2014043272A1 (enExample) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL2651417T3 (pl) | 2010-12-16 | 2017-08-31 | Calchan Limited | Pochodne pirolopirymidyny hamujące ASK1 |
| PH12013501800A1 (en) * | 2011-03-15 | 2013-10-14 | L Livermore Nat Security Llc | Tricyclic gyrase inhibitors |
| WO2015038661A1 (en) | 2013-09-11 | 2015-03-19 | Trius Therapeutics, Inc. | Tricyclic gyrase inhibitors |
| WO2016067009A1 (en) * | 2014-10-28 | 2016-05-06 | Redx Pharma Plc | Compounds with activity against bacteria and mycobacteria |
| US11725187B2 (en) | 2016-06-01 | 2023-08-15 | Universite De Montreal | Selection of human hematopoetic stem cells using EPCR |
| CN106588731B (zh) * | 2016-12-08 | 2018-06-29 | 河北桑迪亚医药技术有限责任公司 | 环丙基二苯基锍三氟甲磺酸盐的合成方法 |
| RU2019133662A (ru) | 2017-03-24 | 2021-04-26 | Тайсо Фармасьютикал Ко., Лтд. | Производное 2(1h)-хинолинона |
| 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 |
| CN119285538A (zh) | 2017-05-04 | 2025-01-10 | 发现号收购集团 | 作为例如用于保护植物的害虫防治剂的2-{[2-(苯氧基甲基)吡啶-5-基]氧基}乙胺衍生物及相关化合物 |
| US11542248B2 (en) * | 2017-06-08 | 2023-01-03 | Kura Oncology, Inc. | Methods and compositions for inhibiting the interaction of menin with MLL proteins |
| TW201920170A (zh) | 2017-09-20 | 2019-06-01 | 美商庫拉腫瘤技術股份有限公司 | 經取代之menin-mll 抑制劑及使用方法 |
| JP7467358B2 (ja) | 2018-02-20 | 2024-04-15 | ウニヴェルシテ・ドゥ・モントリオール | 免疫応答を媒介するｉｎ ｖｉｖｏでのＮＫ細胞およびＤＣ細胞の拡大 |
| JP7443351B2 (ja) * | 2018-09-26 | 2024-03-05 | エフ． ホフマン－ラ ロシュ アーゲー | 細菌感染症の治療及び予防のための、置換ピリドインドール |
| WO2020085504A1 (ja) | 2018-10-26 | 2020-04-30 | 大鵬薬品工業株式会社 | 光照射ザンドマイヤー反応を用いたクロロアゾールカルボキシレート誘導体の製造方法 |
| 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 |
| WO2020225077A1 (en) * | 2019-05-03 | 2020-11-12 | Idorsia Pharmaceuticals Ltd | Pyrimido[4,5-b]indol derivatives as pdhk1 inhibitors |
| MD4051678T2 (en) | 2019-10-28 | 2026-07-31 | Merck Sharp & Dohme Llc | Small molecule inhibitors of the KRAS G12C mutant |
| WO2021085653A1 (en) | 2019-10-31 | 2021-05-06 | Taiho Pharmaceutical Co., Ltd. | 4-aminobut-2-enamide derivatives and salts thereof |
| EP4067343A4 (en) | 2019-11-29 | 2024-01-03 | Taiho Pharmaceutical Co., Ltd. | NEW PHENOLIC COMPOUND OR SALT THEREOF |
| JP7677983B2 (ja) | 2020-01-23 | 2025-05-15 | マイオフォルテ セラピューティクス，インク． | Ｐｇｄｈ阻害剤、およびその作製と使用の方法 |
| US12702658B2 (en) | 2020-04-24 | 2026-08-11 | Taiho Pharmaceutical Co., Ltd. | Anticancer combination therapy with N-(1-acryloyl-azetidin-3-yl)-2-((1H-indazol-3-yl)amino)methyl)-1H-imidazole-5-carboxamide inhibitor of KRAS-G12C |
| WO2021215544A1 (en) | 2020-04-24 | 2021-10-28 | Taiho Pharmaceutical Co., Ltd. | Kras g12d protein inhibitors |
| WO2022109487A1 (en) | 2020-11-23 | 2022-05-27 | Merck Sharp & Dohme Corp. | Spirocyclic-substituted 6,7-dihydro-pyrano[2,3-d]pyrimidine inhibitors of kras g12c mutant |
| CN112574085A (zh) * | 2020-12-18 | 2021-03-30 | 南通药明康德医药科技有限公司 | 一种5-氨基-2-氮杂螺[3.4]辛烷-2-羧酸叔丁酯的制备方法 |
| CN112552222B (zh) * | 2020-12-18 | 2022-08-23 | 南通药明康德医药科技有限公司 | 一种2-(2-(叔-丁氧羰基)-2-氮杂螺[3.4]辛烷-5-基)乙酸的制备方法 |
| 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 |
| CN113372352B (zh) * | 2021-06-10 | 2022-08-26 | 青岛农业大学 | 吲哚3,4位并九元中环化合物及其制备方法 |
| EP4590658A1 (en) * | 2022-09-21 | 2025-07-30 | Bristol-Myers Squibb Company | Process for the preparation of tert-butyl (2-azabicyclo[2.2.1]heptan-4-yl)carbamate and related compounds |
| WO2024103010A1 (en) * | 2022-11-11 | 2024-05-16 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras proteins |
| EP4709371A1 (en) * | 2023-05-09 | 2026-03-18 | Merck Sharp & Dohme LLC | Small molecule inhibitors of kras g12d mutant |
| KR20260096846A (ko) | 2023-10-20 | 2026-06-24 | 머크 샤프 앤드 돔 엘엘씨 | Kras 단백질의 소분자 억제제 |
| WO2025240742A1 (en) * | 2024-05-15 | 2025-11-20 | Merck Sharp & Dohme Llc | Protein degraders of kras g12d mutant |
| WO2026161671A1 (en) * | 2025-01-23 | 2026-07-30 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras proteins |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IN157280B (enExample) * | 1983-07-15 | 1986-02-22 | Hoechst India | |
| 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 |
| US5279359A (en) | 1992-06-26 | 1994-01-18 | Erickson Donald C | Rotary trisorption heat pump |
| 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 |
| GEP20053429B (en) | 2000-01-24 | 2005-01-25 | Warner Lambert Co | 3-Aminoquinazolin-2,4-Dione, Pharmaceutical Composition Containing Them and Use Thereof as Antibacterial Agents |
| US20090099165A1 (en) | 2003-10-14 | 2009-04-16 | 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 |
| WO2005037825A2 (en) * | 2003-10-14 | 2005-04-28 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Protein kinase inhibitors |
| US20090143399A1 (en) | 2003-10-14 | 2009-06-04 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Protein Kinase Inhibitors |
| US7776855B2 (en) | 2006-07-27 | 2010-08-17 | Janssen Pharmaceutica N.V. | Antimicrobial oxazolidinone prodrugs |
| WO2011032050A2 (en) * | 2009-09-11 | 2011-03-17 | Trius Therapeutics, Inc. | Gyrase inhibitors |
| PH12013501800A1 (en) | 2011-03-15 | 2013-10-14 | L Livermore Nat Security Llc | Tricyclic gyrase inhibitors |
| WO2015038661A1 (en) * | 2013-09-11 | 2015-03-19 | Trius Therapeutics, Inc. | Tricyclic gyrase inhibitors |
-
2013
- 2013-09-11 WO PCT/US2013/059310 patent/WO2014043272A1/en not_active Ceased
- 2013-09-11 US US14/427,611 patent/US10865216B2/en active Active
- 2013-09-11 EP EP13765905.8A patent/EP2895488B1/en active Active
- 2013-09-11 TW TW102132841A patent/TWI639602B/zh active
- 2013-09-11 CN CN201380058803.6A patent/CN105189505B/zh active Active
- 2013-09-11 JP JP2015532025A patent/JP6460991B2/ja active Active
- 2013-09-12 AR ARP130103259A patent/AR092538A1/es active IP Right Grant
Also Published As
| Publication number | Publication date |
|---|---|
| EP2895488A1 (en) | 2015-07-22 |
| CN105189505A (zh) | 2015-12-23 |
| US20150246934A1 (en) | 2015-09-03 |
| JP6460991B2 (ja) | 2019-01-30 |
| WO2014043272A1 (en) | 2014-03-20 |
| EP2895488B1 (en) | 2024-12-11 |
| US10865216B2 (en) | 2020-12-15 |
| TWI639602B (zh) | 2018-11-01 |
| TW201425314A (zh) | 2014-07-01 |
| CN105189505B (zh) | 2019-03-22 |
| JP2015528502A (ja) | 2015-09-28 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration |