CN102596977B - 雷公藤内酯前药 - Google Patents
雷公藤内酯前药 Download PDFInfo
- Publication number
- CN102596977B CN102596977B CN201080031839.1A CN201080031839A CN102596977B CN 102596977 B CN102596977 B CN 102596977B CN 201080031839 A CN201080031839 A CN 201080031839A CN 102596977 B CN102596977 B CN 102596977B
- Authority
- CN
- China
- Prior art keywords
- cancer
- compound
- triptolide
- formula
- purposes
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/665—Phosphorus compounds having oxygen as a ring hetero atom, e.g. fosfomycin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
- C07F9/572—Five-membered rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Oncology (AREA)
- Neurosurgery (AREA)
- Gastroenterology & Hepatology (AREA)
- Pulmonology (AREA)
- Physical Education & Sports Medicine (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US17624909P | 2009-05-07 | 2009-05-07 | |
| US61/176249 | 2009-05-07 | ||
| PCT/US2010/034117 WO2010129918A1 (en) | 2009-05-07 | 2010-05-07 | Triptolide prodrugs |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102596977A CN102596977A (zh) | 2012-07-18 |
| CN102596977B true CN102596977B (zh) | 2016-06-29 |
Family
ID=42244313
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201080031839.1A Active CN102596977B (zh) | 2009-05-07 | 2010-05-07 | 雷公藤内酯前药 |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US8507552B2 (enExample) |
| EP (1) | EP2427467B1 (enExample) |
| JP (3) | JP6000122B2 (enExample) |
| KR (1) | KR101821823B1 (enExample) |
| CN (1) | CN102596977B (enExample) |
| AU (1) | AU2010245669B2 (enExample) |
| BR (1) | BRPI1014802B8 (enExample) |
| CA (2) | CA2760953C (enExample) |
| DK (1) | DK2427467T3 (enExample) |
| EA (1) | EA021135B1 (enExample) |
| ES (1) | ES2552163T3 (enExample) |
| MX (1) | MX2011011776A (enExample) |
| MY (1) | MY160392A (enExample) |
| PL (1) | PL2427467T3 (enExample) |
| PT (1) | PT2427467E (enExample) |
| SG (1) | SG175885A1 (enExample) |
| WO (1) | WO2010129918A1 (enExample) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9150600B2 (en) | 2009-05-07 | 2015-10-06 | Regents Of The University Of Minnesota | Triptolide prodrugs |
| DK3510860T3 (da) | 2012-08-23 | 2021-10-18 | Senestech Inc | Nedsættelse af pattedyrs reproduktive kapacitet |
| WO2014047783A1 (zh) * | 2012-09-25 | 2014-04-03 | 鼎泓国际投资(香港)有限公司 | 含有雷公藤甲素及雷公藤甲素类衍生物和Bcl-2抑制剂的药物组合物及其应用 |
| WO2014167581A2 (en) * | 2013-04-01 | 2014-10-16 | Laurus Labs Private Limited | An improved process for the preparation of triptolide prodrugs |
| JP6931228B2 (ja) * | 2015-09-11 | 2021-09-01 | ワイズ・エー・シー株式会社 | 抗cd26抗体と他の抗癌剤とを組み合わせた癌治療用組成物 |
| CN109942665B (zh) * | 2018-04-02 | 2021-04-06 | 欣凯医药化工中间体(上海)有限公司 | 雷公藤内酯醇衍生物及其制备方法和应用 |
| CN110551171B (zh) * | 2018-05-31 | 2021-07-27 | 欣凯医药化工中间体(上海)有限公司 | 一种雷公藤内酯醇衍生物的制备方法 |
| CN113056474A (zh) * | 2018-09-13 | 2021-06-29 | 米尼阿姆里塔治疗学有限责任公司 | 用于治疗纤维化、nash和nafld的方法中的雷公藤内酯及其前药 |
| WO2021221179A1 (ja) * | 2020-04-28 | 2021-11-04 | 国立大学法人高知大学 | ヒト膵癌オルガノイドを用いたマウスモデルの樹立 |
| US20230303618A1 (en) | 2020-08-21 | 2023-09-28 | Reyoung Corporation | Triptolide conjugates and uses thereof |
| CN115227829B (zh) * | 2022-02-22 | 2023-10-13 | 成都中医药大学 | 酸敏感性适配体雷公藤甲素偶联物及应用 |
| KR102821060B1 (ko) | 2023-03-09 | 2025-06-16 | 미네암리타 테라퓨틱스, 엘엘씨 | 위암의 치료를 위한 약물 조합 |
| KR20250154513A (ko) | 2023-03-09 | 2025-10-28 | 미네암리타 테라퓨틱스, 엘엘씨 | 췌장암 치료용 약물 조합 |
| WO2024187139A1 (en) | 2023-03-09 | 2024-09-12 | Minneamrita Therapeutics Llc | Drug combination for treatment of gastric cancer |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1483731A (zh) * | 2002-09-18 | 2004-03-24 | 成都达远药物有限公司 | 高免疫抑制活性的水溶性雷公藤内酯醇衍生物及其应用 |
| CA2658793A1 (en) * | 2006-07-25 | 2008-02-07 | Daniel Dumas | Quinoline derivatives |
| WO2008108384A1 (ja) * | 2007-03-06 | 2008-09-12 | Eisai R & D Management Co., Ltd. | 安定性が改善されたクロロメチルフォスフェイト誘導体を含む組成物及びその製造方法 |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5843452A (en) | 1992-11-09 | 1998-12-01 | Pharmagenesis, Inc. | Immunotherapy composition and method |
| US5759550A (en) | 1993-05-06 | 1998-06-02 | Pharmagenesis, Inc. | Method for suppressing xenograft rejection |
| US5609991A (en) | 1995-02-10 | 1997-03-11 | Morton International, Inc. | Photoimageable composition having improved alkaline process resistance and tack-free surface for contact imaging |
| US5663335A (en) | 1996-03-01 | 1997-09-02 | Pharmagenesis, Inc. | Immunosuppressive compounds and methods |
| US5962516A (en) | 1997-02-28 | 1999-10-05 | Pharmagenesis, Inc. | Immunosuppressive compounds and methods |
| US6204257B1 (en) * | 1998-08-07 | 2001-03-20 | Universtiy Of Kansas | Water soluble prodrugs of hindered alcohols |
| US6548537B1 (en) | 1998-09-02 | 2003-04-15 | Pharmagenesis, Inc. | Triptolide prodrugs having high aqueous solubility |
| DE69909633T2 (de) * | 1998-09-02 | 2004-05-13 | Pharmagenesis, Inc., Palo Alto | Gut wasserlösliche triptolid-prodrugs |
| AU3365800A (en) | 1999-02-16 | 2000-09-04 | Board Of Trustees Of The Leland Stanford Junior University | Combined therapy of diterpenoid triepoxides and trail for synergistic killing oftumor cells |
| AU5368699A (en) | 1999-04-16 | 2000-11-02 | Chengdu Diao Pharmaceutical Group Company Limited | Derivatives of triptolide, and preparation and uses thereof |
| US6294546B1 (en) | 1999-08-30 | 2001-09-25 | The Broad Of Trustees Of The Leland Stanford Junior University | Uses of diterpenoid triepoxides as an anti-proliferative agent |
| US6620843B2 (en) * | 2001-01-19 | 2003-09-16 | Pharmagenesis | Anticancer treatment using triptolide prodrugs |
| US6569893B2 (en) * | 2001-03-15 | 2003-05-27 | Pharmagenesis, Inc. | Amino acid derivatives of triptolide compounds as immune modulators and anticancer agents |
| UA77033C2 (uk) * | 2001-12-21 | 2006-10-16 | Mgi Gp Inc | Спосіб отримання водорозчинних фосфонооксиметильних похідних спирту та фенолу |
| US7847109B2 (en) | 2002-05-31 | 2010-12-07 | Pharmagenesis, Inc. | Triptolide derivatives for modulation of apoptosis and immunosuppression |
| AU2003297211A1 (en) | 2002-12-17 | 2004-07-22 | Pharmagenesis, Inc. | Triptolide derivatives as immunomodulator and anticancer agents |
| CN1223595C (zh) | 2002-12-27 | 2005-10-19 | 中国科学院上海药物研究所 | 雷公藤内酯醇衍生物及其应用 |
| US6943259B2 (en) | 2003-02-25 | 2005-09-13 | Pharmagenesis, Inc. | Halogenated triptolide derivatives as immunomodulators and anticancer agents |
| WO2005020887A2 (en) | 2003-06-27 | 2005-03-10 | Pharmagenesis, Inc. | Method for treatment of severe acute respiratory syndrome |
| US7820834B2 (en) | 2003-12-24 | 2010-10-26 | Pharmagenesis, Inc. | Triptolide 5,6-derivatives as immunomodulators and anticancer agents |
| JP5252765B2 (ja) | 2003-12-26 | 2013-07-31 | 学校法人東京薬科大学 | 皮脂産生抑制剤及び皮脂腺発達抑制剤、並びに、皮膚外用剤 |
| ATE554758T1 (de) | 2004-03-02 | 2012-05-15 | Pharmagenesis Inc | Triptolid-lacton-ring-derivate als immunmodulatoren und mittel gegen krebs |
| US20070244080A1 (en) | 2004-06-25 | 2007-10-18 | Pharmagenesis, Inc. | Method for Treatment of Inflammatory Disorders Using Triptolide Compounds |
| WO2007025031A2 (en) * | 2005-08-24 | 2007-03-01 | Cephalon, Inc. | Prodrugs of indanone and tetralone compounds |
| CN101049300A (zh) | 2006-04-04 | 2007-10-10 | 中国科学院上海药物研究所 | 包含雷公藤内酯醇衍生物的药物组合物、其剂型和应用 |
| FI20070574A0 (fi) * | 2007-07-30 | 2007-07-30 | Kuopion Yliopisto | Vesiliukoinen propofolin etylideenifosfaatti-aihiolääke |
| WO2009023201A1 (en) | 2007-08-16 | 2009-02-19 | Myelorx Llc | Rigid derivatives of triptolide as anticancer, immune suppressant, anti-fibrosis, and cns protectant agents |
-
2010
- 2010-05-07 CA CA2760953A patent/CA2760953C/en active Active
- 2010-05-07 AU AU2010245669A patent/AU2010245669B2/en active Active
- 2010-05-07 CA CA2964631A patent/CA2964631A1/en not_active Abandoned
- 2010-05-07 PT PT107191884T patent/PT2427467E/pt unknown
- 2010-05-07 DK DK10719188.4T patent/DK2427467T3/en active
- 2010-05-07 BR BRPI1014802A patent/BRPI1014802B8/pt active IP Right Grant
- 2010-05-07 MX MX2011011776A patent/MX2011011776A/es active IP Right Grant
- 2010-05-07 KR KR1020117029123A patent/KR101821823B1/ko active Active
- 2010-05-07 US US13/319,316 patent/US8507552B2/en active Active
- 2010-05-07 PL PL10719188T patent/PL2427467T3/pl unknown
- 2010-05-07 SG SG2011081122A patent/SG175885A1/en unknown
- 2010-05-07 JP JP2012510027A patent/JP6000122B2/ja active Active
- 2010-05-07 WO PCT/US2010/034117 patent/WO2010129918A1/en not_active Ceased
- 2010-05-07 MY MYPI2011005335A patent/MY160392A/en unknown
- 2010-05-07 EA EA201190293A patent/EA021135B1/ru unknown
- 2010-05-07 ES ES10719188.4T patent/ES2552163T3/es active Active
- 2010-05-07 CN CN201080031839.1A patent/CN102596977B/zh active Active
- 2010-05-07 EP EP10719188.4A patent/EP2427467B1/en active Active
-
2014
- 2014-07-03 JP JP2014137661A patent/JP2014185181A/ja not_active Withdrawn
-
2016
- 2016-01-08 JP JP2016002236A patent/JP2016065099A/ja active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1483731A (zh) * | 2002-09-18 | 2004-03-24 | 成都达远药物有限公司 | 高免疫抑制活性的水溶性雷公藤内酯醇衍生物及其应用 |
| CA2658793A1 (en) * | 2006-07-25 | 2008-02-07 | Daniel Dumas | Quinoline derivatives |
| WO2008108384A1 (ja) * | 2007-03-06 | 2008-09-12 | Eisai R & D Management Co., Ltd. | 安定性が改善されたクロロメチルフォスフェイト誘導体を含む組成物及びその製造方法 |
Also Published As
| Publication number | Publication date |
|---|---|
| CA2760953C (en) | 2017-05-30 |
| EP2427467A1 (en) | 2012-03-14 |
| EP2427467B1 (en) | 2015-08-05 |
| PL2427467T3 (pl) | 2016-04-29 |
| EA201190293A1 (ru) | 2012-11-30 |
| CA2760953A1 (en) | 2010-11-11 |
| MY160392A (en) | 2017-03-15 |
| WO2010129918A1 (en) | 2010-11-11 |
| ES2552163T3 (es) | 2015-11-26 |
| WO2010129918A8 (en) | 2011-01-20 |
| JP2014185181A (ja) | 2014-10-02 |
| JP6000122B2 (ja) | 2016-09-28 |
| AU2010245669A1 (en) | 2011-12-01 |
| KR20120015339A (ko) | 2012-02-21 |
| JP2016065099A (ja) | 2016-04-28 |
| US8507552B2 (en) | 2013-08-13 |
| MX2011011776A (es) | 2012-08-03 |
| BRPI1014802B1 (pt) | 2020-09-24 |
| AU2010245669B2 (en) | 2015-11-26 |
| KR101821823B1 (ko) | 2018-01-24 |
| CN102596977A (zh) | 2012-07-18 |
| HK1168107A1 (en) | 2012-12-21 |
| DK2427467T3 (en) | 2015-11-09 |
| CA2964631A1 (en) | 2010-11-11 |
| SG175885A1 (en) | 2011-12-29 |
| JP2012526148A (ja) | 2012-10-25 |
| BRPI1014802B8 (pt) | 2021-05-25 |
| PT2427467E (pt) | 2015-11-19 |
| BRPI1014802A2 (pt) | 2016-04-05 |
| US20120238529A1 (en) | 2012-09-20 |
| EA021135B1 (ru) | 2015-04-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant |