TWI450898B - 具有抗腫瘤活性之芳基異唑化合物 - Google Patents
具有抗腫瘤活性之芳基異唑化合物 Download PDFInfo
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- TWI450898B TWI450898B TW098120258A TW98120258A TWI450898B TW I450898 B TWI450898 B TW I450898B TW 098120258 A TW098120258 A TW 098120258A TW 98120258 A TW98120258 A TW 98120258A TW I450898 B TWI450898 B TW I450898B
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- Taiwan
- Prior art keywords
- phenyl
- dihydroxy
- carboxylic acid
- iso
- chloro
- Prior art date
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- -1 Aryl isoxazole compounds Chemical class 0.000 title claims description 156
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- 125000004434 sulfur atom Chemical group 0.000 description 1
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- AYUNIORJHRXIBJ-TXHRRWQRSA-N tanespimycin Chemical compound N1C(=O)\C(C)=C\C=C/[C@H](OC)[C@@H](OC(N)=O)\C(C)=C\[C@H](C)[C@@H](O)[C@@H](OC)C[C@H](C)CC2=C(NCC=C)C(=O)C=C1C2=O AYUNIORJHRXIBJ-TXHRRWQRSA-N 0.000 description 1
- 229950007866 tanespimycin Drugs 0.000 description 1
- 125000000335 thiazolyl group Chemical group 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- 125000003396 thiol group Chemical group [H]S* 0.000 description 1
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- 238000011200 topical administration Methods 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 239000003204 tranquilizing agent Substances 0.000 description 1
- 230000002936 tranquilizing effect Effects 0.000 description 1
- 230000009466 transformation Effects 0.000 description 1
- 238000000844 transformation Methods 0.000 description 1
- 230000007704 transition Effects 0.000 description 1
- ITMCEJHCFYSIIV-UHFFFAOYSA-N triflic acid Chemical compound OS(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-N 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- XSQUKJJJFZCRTK-UHFFFAOYSA-N urea group Chemical group NC(=O)N XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 1
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- 230000009385 viral infection Effects 0.000 description 1
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- 238000005406 washing Methods 0.000 description 1
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Classifications
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- C07—ORGANIC CHEMISTRY
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- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
- C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members 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
- C07D261/18—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
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- 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
- A61K31/42—Oxazoles
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- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P37/02—Immunomodulators
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P9/00—Drugs for disorders of the cardiovascular system
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
- C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members 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
- C07D261/14—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D498/02—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 two hetero rings
- C07D498/04—Ortho-condensed systems
-
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
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- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
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- Biomedical Technology (AREA)
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- Psychology (AREA)
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- Physical Education & Sports Medicine (AREA)
- Transplantation (AREA)
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- Rheumatology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Oncology (AREA)
- Anesthesiology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
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| EP08159692 | 2008-07-04 |
Publications (2)
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| TW201012815A TW201012815A (en) | 2010-04-01 |
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| TW098120258A TWI450898B (zh) | 2008-07-04 | 2009-06-17 | 具有抗腫瘤活性之芳基異唑化合物 |
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| EP (1) | EP2310377B1 (enExample) |
| JP (1) | JP5640002B2 (enExample) |
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| WO (1) | WO2010000748A1 (enExample) |
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Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8236838B2 (en) * | 2008-04-21 | 2012-08-07 | Institute For Oneworld Health | Compounds, compositions and methods comprising isoxazole derivatives |
| US8343976B2 (en) | 2009-04-20 | 2013-01-01 | Institute For Oneworld Health | Compounds, compositions and methods comprising pyrazole derivatives |
| EP3190083B1 (en) | 2010-10-27 | 2020-08-26 | Pixelligent Technologies, LLC | Synthesis, capping and dispersion of nanocrystals |
| KR101275264B1 (ko) * | 2011-08-24 | 2013-06-17 | 포항공과대학교 산학협력단 | 샤프로닌 단백질의 조절 물질 탐색 방법 |
| CN103724269B (zh) * | 2012-10-11 | 2016-12-21 | 中国科学院上海药物研究所 | 苯基1,2-异噁唑或苯基1,2-吡唑类化合物及其用途 |
| WO2015143004A1 (en) * | 2014-03-18 | 2015-09-24 | Synta Pharmaceuticals Corp. | Targeted therapeutics |
| US9855249B2 (en) | 2014-10-02 | 2018-01-02 | Flatley Discovery Lab, Llc | Isoxazole compounds and methods for the treatment of cystic fibrosis |
| CA2972239A1 (en) | 2014-12-23 | 2016-06-30 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| CN104725329B (zh) * | 2015-01-13 | 2017-01-18 | 陕西科技大学 | 一种具有抗肿瘤活性的异恶唑羧酸类化合物及其合成方法 |
| CN107427521B (zh) | 2015-03-27 | 2021-08-03 | 达纳-法伯癌症研究所股份有限公司 | 细胞周期蛋白依赖性激酶的抑制剂 |
| CN104803934B (zh) * | 2015-05-04 | 2018-01-02 | 陕西科技大学 | 一种具有抗肿瘤活性的苯基异噁唑羧酸类化合物及其合成方法与应用 |
| IT201700081419A1 (it) * | 2017-07-18 | 2019-01-18 | Rare Partners Srl | Derivati isossazolici come induttori di emoglobina fetale in precursori eritroidi derivati da pazienti beta-talassemici |
| JP7590185B2 (ja) * | 2018-06-25 | 2024-11-26 | ダナ－ファーバー キャンサー インスティテュート， インコーポレイテッド | Ｔａｉｒｅファミリーキナーゼインヒビターおよびそれらの使用 |
| EP3902542A4 (en) | 2018-12-28 | 2022-09-07 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 and uses thereof |
| CN117105880B (zh) * | 2022-10-17 | 2025-08-26 | 上海康斯维克生物医药有限公司 | 用作诱发抗原特异性反应的脲类化合物、其荧光标记物及制备方法和用途 |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004072051A1 (en) * | 2003-02-11 | 2004-08-26 | Vernalis (Cambridge) Limited | Isoxazole compounds as inhibitors of heat shock proteins |
| WO2007078113A1 (en) * | 2005-12-30 | 2007-07-12 | Sk Holdings Co., Ltd. | Isoxazole derivatives and use thereof |
| WO2007096194A1 (en) * | 2006-02-27 | 2007-08-30 | Novartis Ag | Radio-labeled isoxazole derivatives useful for the labeling and diagnostic of hsp90 functionality |
| TWI288136B (en) * | 2000-02-18 | 2007-10-11 | Kirin Brewery | Novel isoxazole and thiazole compounds and use thereof as drugs |
| TW200844102A (en) * | 2007-03-01 | 2008-11-16 | Novartis Ag | Acid addition salts, hydrates and polymorphs of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide and formulations comprising these forms |
-
2009
- 2009-06-17 TW TW098120258A patent/TWI450898B/zh not_active IP Right Cessation
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- 2009-06-30 EP EP09772448.8A patent/EP2310377B1/en not_active Not-in-force
- 2009-06-30 CA CA2729710A patent/CA2729710A1/en not_active Abandoned
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- 2009-06-30 BR BRPI0913834A patent/BRPI0913834A2/pt not_active IP Right Cessation
- 2009-06-30 KR KR1020117000312A patent/KR20110050615A/ko not_active Ceased
- 2009-06-30 NZ NZ590861A patent/NZ590861A/xx not_active IP Right Cessation
- 2009-06-30 MY MYPI20105887 patent/MY150604A/en unknown
- 2009-06-30 EA EA201170139A patent/EA019793B1/ru not_active IP Right Cessation
- 2009-06-30 CN CN2009801255931A patent/CN102083804A/zh active Pending
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2010
- 2010-12-23 IL IL210200A patent/IL210200A0/en unknown
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2011
- 2011-01-03 ZA ZA2011/00007A patent/ZA201100007B/en unknown
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI288136B (en) * | 2000-02-18 | 2007-10-11 | Kirin Brewery | Novel isoxazole and thiazole compounds and use thereof as drugs |
| WO2004072051A1 (en) * | 2003-02-11 | 2004-08-26 | Vernalis (Cambridge) Limited | Isoxazole compounds as inhibitors of heat shock proteins |
| WO2007078113A1 (en) * | 2005-12-30 | 2007-07-12 | Sk Holdings Co., Ltd. | Isoxazole derivatives and use thereof |
| WO2007096194A1 (en) * | 2006-02-27 | 2007-08-30 | Novartis Ag | Radio-labeled isoxazole derivatives useful for the labeling and diagnostic of hsp90 functionality |
| TW200844102A (en) * | 2007-03-01 | 2008-11-16 | Novartis Ag | Acid addition salts, hydrates and polymorphs of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide and formulations comprising these forms |
Also Published As
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| IL210200A0 (en) | 2011-03-31 |
| US20110245221A1 (en) | 2011-10-06 |
| EP2310377A1 (en) | 2011-04-20 |
| AU2009265745A1 (en) | 2010-01-07 |
| AU2009265745B2 (en) | 2013-07-04 |
| JP2011526594A (ja) | 2011-10-13 |
| MX2010013913A (es) | 2011-03-03 |
| MY150604A (en) | 2014-01-30 |
| ZA201100007B (en) | 2011-10-26 |
| KR20110050615A (ko) | 2011-05-16 |
| TW201012815A (en) | 2010-04-01 |
| US8383616B2 (en) | 2013-02-26 |
| WO2010000748A1 (en) | 2010-01-07 |
| JP5640002B2 (ja) | 2014-12-10 |
| CN102083804A (zh) | 2011-06-01 |
| AR072793A1 (es) | 2010-09-22 |
| CA2729710A1 (en) | 2010-01-07 |
| BRPI0913834A2 (pt) | 2015-10-20 |
| SG192464A1 (en) | 2013-08-30 |
| EA201170139A1 (ru) | 2011-08-30 |
| EA019793B1 (ru) | 2014-06-30 |
| EP2310377B1 (en) | 2015-09-16 |
| NZ590861A (en) | 2012-08-31 |
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