KR101929774B1 - 락탐을 강력한 hdac 억제제로서 보유하는 신규 티오 유도체 및 약제로서 그의 용도 - Google Patents
락탐을 강력한 hdac 억제제로서 보유하는 신규 티오 유도체 및 약제로서 그의 용도 Download PDFInfo
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- KR101929774B1 KR101929774B1 KR1020147003177A KR20147003177A KR101929774B1 KR 101929774 B1 KR101929774 B1 KR 101929774B1 KR 1020147003177 A KR1020147003177 A KR 1020147003177A KR 20147003177 A KR20147003177 A KR 20147003177A KR 101929774 B1 KR101929774 B1 KR 101929774B1
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- oxo
- hexyl
- phenylcarbamoyl
- amino
- ester
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- 0 CN(*)C(CCC*)=O Chemical compound CN(*)C(CCC*)=O 0.000 description 1
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/62—Oxygen or sulfur atoms
- C07D213/69—Two or more oxygen atoms
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- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/05—Dipeptides
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- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
- C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
- C07D205/06—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D205/08—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
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- C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/24—Oxygen or sulfur atoms
- C07D207/26—2-Pyrrolidones
- C07D207/273—2-Pyrrolidones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
- C07D207/277—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/24—Oxygen or sulfur atoms
- C07D207/26—2-Pyrrolidones
- C07D207/273—2-Pyrrolidones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
- C07D207/277—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D207/28—2-Pyrrolidone-5- carboxylic acids; Functional derivatives thereof, e.g. esters, nitriles
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D211/78—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/92—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
- C07D211/94—Oxygen atom, e.g. piperidine N-oxide
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06139—Dipeptides with the first amino acid being heterocyclic
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
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- Neurosurgery (AREA)
- Tropical Medicine & Parasitology (AREA)
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- Proteomics, Peptides & Aminoacids (AREA)
- Oncology (AREA)
- Psychology (AREA)
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- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Gastroenterology & Hepatology (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11181832.4 | 2011-09-19 | ||
| EP11181832 | 2011-09-19 | ||
| PCT/EP2012/068230 WO2013041480A1 (en) | 2011-09-19 | 2012-09-17 | New thio derivatives bearing lactams as potent hdac inhibitors and their uses as medicaments |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20140066993A KR20140066993A (ko) | 2014-06-03 |
| KR101929774B1 true KR101929774B1 (ko) | 2018-12-18 |
Family
ID=46888433
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020147003177A Active KR101929774B1 (ko) | 2011-09-19 | 2012-09-17 | 락탐을 강력한 hdac 억제제로서 보유하는 신규 티오 유도체 및 약제로서 그의 용도 |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US8927533B2 (https=) |
| EP (1) | EP2758371B1 (https=) |
| JP (1) | JP6053795B2 (https=) |
| KR (1) | KR101929774B1 (https=) |
| CN (1) | CN103732577B (https=) |
| AU (1) | AU2012311640B2 (https=) |
| BR (1) | BR112014006600B1 (https=) |
| CA (1) | CA2843211C (https=) |
| DK (1) | DK2758371T3 (https=) |
| EA (1) | EA023171B1 (https=) |
| ES (1) | ES2579321T3 (https=) |
| HU (1) | HUE029687T2 (https=) |
| IL (1) | IL230717A (https=) |
| MX (1) | MX369508B (https=) |
| NZ (1) | NZ620336A (https=) |
| PH (1) | PH12014500249A1 (https=) |
| PL (1) | PL2758371T3 (https=) |
| PT (1) | PT2758371T (https=) |
| UA (1) | UA111231C2 (https=) |
| WO (1) | WO2013041480A1 (https=) |
| ZA (1) | ZA201402790B (https=) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CR20160308A (es) * | 2013-12-03 | 2016-11-08 | Acetylon Pharmaceuticals Inc | Combinaciones de inhibidores de histona deacetilasa y farmacos inmunomoduladores |
| KR102359214B1 (ko) | 2014-04-04 | 2022-02-07 | 델 마 파마슈티컬스 | 폐의 비소세포 암종 및 난소암을 치료하기 위한 디안하이드로갈락티톨 및 이의 유사체 또는 유도체 |
| WO2016201374A1 (en) * | 2015-06-11 | 2016-12-15 | University Of Florida Research Foundation, Incorporated | Sulfanide adenosine derivatives and uses thereof |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| IL326136A (en) | 2023-08-07 | 2026-03-01 | Revolution Medicines Inc | RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| US20250375445A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6511990B1 (en) | 1999-09-08 | 2003-01-28 | Sloan-Kettering Institute For Cancer Research | Class of cytodifferentiating agents and histone deacetylase inhibitors, and methods of use thereof |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT1231477B (it) * | 1989-07-12 | 1991-12-07 | Sigma Tau Ind Farmaceuti | (pirrolidin-2-one-1-il) acetammidi quali attivatori dei processi di apprendimento e della memoria e composizioni farmaceutiche comprendenti tali composti |
| IT1244507B (it) * | 1991-04-11 | 1994-07-15 | Sigma Tau Ind Farmaceuti | Derivati dell'acido piroglutammico quali attivatori dei processi di apprendimento e della memoria e composizioni farmaceutiche comprendenti tali composti |
| ITRM20010464A1 (it) * | 2001-07-31 | 2003-01-31 | Sigma Tau Ind Farmaceuti | Derivati retinoidi ad attivita' antiangiogenica, antitumorale e pro-apoptotica. |
| US7163937B2 (en) * | 2003-08-21 | 2007-01-16 | Bristol-Myers Squibb Company | Cyclic derivatives as modulators of chemokine receptor activity |
| US20080004290A1 (en) * | 2003-11-28 | 2008-01-03 | The University Of Queensland | Anti-Cancer Agents |
| WO2005063259A1 (en) * | 2003-12-19 | 2005-07-14 | Jerini Ag | Compounds for the inhibition of undesired cell proliferation and use thereof |
| JP2007238452A (ja) | 2006-03-03 | 2007-09-20 | Nippon Kayaku Co Ltd | ヒストン脱アセチル化酵素を阻害する新規化合物 |
| EP2100879A1 (en) * | 2008-03-13 | 2009-09-16 | 4Sc Ag | Novel N-substituted tetrahydroisoquinoline/isoindoline hydroxamic acid compounds |
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2012
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2014
- 2014-01-29 IL IL230717A patent/IL230717A/en active IP Right Grant
- 2014-04-16 ZA ZA2014/02790A patent/ZA201402790B/en unknown
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6511990B1 (en) | 1999-09-08 | 2003-01-28 | Sloan-Kettering Institute For Cancer Research | Class of cytodifferentiating agents and histone deacetylase inhibitors, and methods of use thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| HUE029687T2 (en) | 2017-03-28 |
| JP2014531441A (ja) | 2014-11-27 |
| CA2843211A1 (en) | 2013-03-28 |
| MX369508B (es) | 2019-11-11 |
| AU2012311640A1 (en) | 2014-02-13 |
| ZA201402790B (en) | 2015-12-23 |
| BR112014006600B1 (pt) | 2022-04-19 |
| ES2579321T3 (es) | 2016-08-09 |
| IL230717A (en) | 2017-01-31 |
| UA111231C2 (uk) | 2016-04-11 |
| WO2013041480A1 (en) | 2013-03-28 |
| CN103732577A (zh) | 2014-04-16 |
| EA201400365A1 (ru) | 2014-06-30 |
| CN103732577B (zh) | 2017-04-05 |
| EA023171B1 (ru) | 2016-04-29 |
| EP2758371A1 (en) | 2014-07-30 |
| US20140200205A1 (en) | 2014-07-17 |
| EP2758371B1 (en) | 2016-06-15 |
| PL2758371T3 (pl) | 2017-01-31 |
| CA2843211C (en) | 2019-03-12 |
| PT2758371T (pt) | 2016-07-13 |
| JP6053795B2 (ja) | 2016-12-27 |
| IL230717A0 (en) | 2014-03-31 |
| AU2012311640B2 (en) | 2017-04-13 |
| US8927533B2 (en) | 2015-01-06 |
| DK2758371T3 (en) | 2016-08-01 |
| NZ620336A (en) | 2015-07-31 |
| PH12014500249A1 (en) | 2022-11-23 |
| BR112014006600A2 (pt) | 2017-03-28 |
| MX2014003334A (es) | 2014-05-21 |
| KR20140066993A (ko) | 2014-06-03 |
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