BRPI1014802B8 - profármacos de triptolida. - Google Patents
profármacos de triptolida.Info
- Publication number
- BRPI1014802B8 BRPI1014802B8 BRPI1014802A BRPI1014802A BRPI1014802B8 BR PI1014802 B8 BRPI1014802 B8 BR PI1014802B8 BR PI1014802 A BRPI1014802 A BR PI1014802A BR PI1014802 A BRPI1014802 A BR PI1014802A BR PI1014802 B8 BRPI1014802 B8 BR PI1014802B8
- Authority
- BR
- Brazil
- Prior art keywords
- formula
- compounds
- triptolide prodrugs
- triptolide
- prodrugs
- Prior art date
Links
- DFBIRQPKNDILPW-CIVMWXNOSA-N Triptolide Chemical compound O=C1OCC([C@@H]2C3)=C1CC[C@]2(C)[C@]12O[C@H]1[C@@H]1O[C@]1(C(C)C)[C@@H](O)[C@]21[C@H]3O1 DFBIRQPKNDILPW-CIVMWXNOSA-N 0.000 title abstract 2
- 239000000651 prodrug Substances 0.000 title abstract 2
- 229940002612 prodrug Drugs 0.000 title abstract 2
- YKUJZZHGTWVWHA-UHFFFAOYSA-N triptolide Natural products COC12CC3OC3(C(C)C)C(O)C14OC4CC5C6=C(CCC25C)C(=O)OC6 YKUJZZHGTWVWHA-UHFFFAOYSA-N 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 5
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
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 | |
| US61/176,249 | 2009-05-07 | ||
| PCT/US2010/034117 WO2010129918A1 (en) | 2009-05-07 | 2010-05-07 | Triptolide prodrugs |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| BRPI1014802A2 BRPI1014802A2 (pt) | 2016-04-05 |
| BRPI1014802B1 BRPI1014802B1 (pt) | 2020-09-24 |
| BRPI1014802B8 true BRPI1014802B8 (pt) | 2021-05-25 |
Family
ID=42244313
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI1014802A BRPI1014802B8 (pt) | 2009-05-07 | 2010-05-07 | profármacos de triptolida. |
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 |
| ES2902651T3 (es) * | 2012-08-23 | 2022-03-29 | Senestech Inc | Reducción de la capacidad reproductiva de mamíferos |
| 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 |
| SG11201802915WA (en) * | 2015-09-11 | 2018-05-30 | Ys Ac Co Ltd | Cancer treatment composition combining anti-cd26 antibody and other anticancer agent |
| 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 |
| CA3112171A1 (en) * | 2018-09-13 | 2020-03-19 | Minneamrita Therapeutics, LLC | Triptolide and prodrugs thereof for use in methods to treat fibrosis, nash, and nafld |
| 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 |
| EP4200022A1 (en) | 2020-08-21 | 2023-06-28 | 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 |
| AU2023435819A1 (en) | 2023-03-09 | 2025-10-02 | Minneamrita Therapeutics Llc | Drug combination for treatment of pancreatic cancer |
| WO2024186319A1 (en) | 2023-03-09 | 2024-09-12 | Minneamrita Therapeutics Llc | Drug combination for treatment of gastric cancer |
| AU2025207356A1 (en) | 2024-01-11 | 2026-08-06 | Minneamrita Therapeutics Llc | Triptolide formulations |
Family Cites Families (30)
| 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 |
| JP2002523495A (ja) * | 1998-09-02 | 2002-07-30 | ファーマジェネシス， インコーポレイテッド | 高い水溶性を有するトリプトリドプロドラッグ |
| WO2000048619A1 (en) | 1999-02-16 | 2000-08-24 | The Board Of Trustees Of The Leland Stanford Junior University | Combined therapy of diterpenoid triepoxides and trail for synergistic killing of tumor 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 |
| EP1390358A4 (en) | 2001-03-15 | 2004-06-16 | Pharmagenesis Inc | AMINO ACID DERIVATIVES OF TRIPTOLIDE COMPOUNDS AS IMMUNOMODULATORS AND ANTICROPHES |
| KR101016969B1 (ko) * | 2001-12-21 | 2011-02-25 | 에이자이 아이엔씨. | 알콜 및 페놀의 수용성 포스포노옥시메틸 유도체를제조하는 방법 |
| AU2003243351B2 (en) | 2002-05-31 | 2009-04-30 | Pharmagenesis, Inc. | Triptolide derivatives for modulation of apoptosis and immunosuppression |
| CN100398544C (zh) * | 2002-09-18 | 2008-07-02 | 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 |
| WO2004058246A1 (en) | 2002-12-17 | 2004-07-15 | 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 |
| ES2385716T3 (es) | 2004-03-02 | 2012-07-30 | Pharmagenesis, Inc. | Derivados en el anillo de lactona de triptolida como inmunomoduladores y agentes anticáncer |
| 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 |
| EP2079699A1 (en) * | 2006-07-25 | 2009-07-22 | Envivo Pharmaceuticals, Inc. | Quinoline derivatives |
| CN101622263B (zh) * | 2007-03-06 | 2013-05-29 | 卫材R&D管理有限公司 | 稳定性被改善的含有磷酸氯甲酯衍生物的组合物及其制备方法 |
| 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 CN CN201080031839.1A patent/CN102596977B/zh active Active
- 2010-05-07 JP JP2012510027A patent/JP6000122B2/ja active Active
- 2010-05-07 MX MX2011011776A patent/MX2011011776A/es active IP Right Grant
- 2010-05-07 BR BRPI1014802A patent/BRPI1014802B8/pt active IP Right Grant
- 2010-05-07 AU AU2010245669A patent/AU2010245669B2/en active Active
- 2010-05-07 EP EP10719188.4A patent/EP2427467B1/en active Active
- 2010-05-07 PT PT107191884T patent/PT2427467E/pt unknown
- 2010-05-07 US US13/319,316 patent/US8507552B2/en active Active
- 2010-05-07 DK DK10719188.4T patent/DK2427467T3/en active
- 2010-05-07 MY MYPI2011005335A patent/MY160392A/en unknown
- 2010-05-07 CA CA2760953A patent/CA2760953C/en active Active
- 2010-05-07 SG SG2011081122A patent/SG175885A1/en unknown
- 2010-05-07 KR KR1020117029123A patent/KR101821823B1/ko active Active
- 2010-05-07 WO PCT/US2010/034117 patent/WO2010129918A1/en not_active Ceased
- 2010-05-07 ES ES10719188.4T patent/ES2552163T3/es active Active
- 2010-05-07 PL PL10719188T patent/PL2427467T3/pl unknown
- 2010-05-07 EA EA201190293A patent/EA021135B1/ru unknown
- 2010-05-07 CA CA2964631A patent/CA2964631A1/en not_active Abandoned
-
2014
- 2014-07-03 JP JP2014137661A patent/JP2014185181A/ja not_active Withdrawn
-
2016
- 2016-01-08 JP JP2016002236A patent/JP2016065099A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| EP2427467B1 (en) | 2015-08-05 |
| MX2011011776A (es) | 2012-08-03 |
| BRPI1014802A2 (pt) | 2016-04-05 |
| CA2760953C (en) | 2017-05-30 |
| ES2552163T3 (es) | 2015-11-26 |
| KR101821823B1 (ko) | 2018-01-24 |
| EA201190293A1 (ru) | 2012-11-30 |
| EA021135B1 (ru) | 2015-04-30 |
| JP2016065099A (ja) | 2016-04-28 |
| CN102596977B (zh) | 2016-06-29 |
| EP2427467A1 (en) | 2012-03-14 |
| AU2010245669A1 (en) | 2011-12-01 |
| WO2010129918A8 (en) | 2011-01-20 |
| JP2014185181A (ja) | 2014-10-02 |
| WO2010129918A1 (en) | 2010-11-11 |
| PT2427467E (pt) | 2015-11-19 |
| AU2010245669B2 (en) | 2015-11-26 |
| PL2427467T3 (pl) | 2016-04-29 |
| HK1168107A1 (en) | 2012-12-21 |
| KR20120015339A (ko) | 2012-02-21 |
| JP2012526148A (ja) | 2012-10-25 |
| JP6000122B2 (ja) | 2016-09-28 |
| CN102596977A (zh) | 2012-07-18 |
| SG175885A1 (en) | 2011-12-29 |
| US20120238529A1 (en) | 2012-09-20 |
| BRPI1014802B1 (pt) | 2020-09-24 |
| US8507552B2 (en) | 2013-08-13 |
| CA2964631A1 (en) | 2010-11-11 |
| DK2427467T3 (en) | 2015-11-09 |
| CA2760953A1 (en) | 2010-11-11 |
| MY160392A (en) | 2017-03-15 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] | ||
| B06F | Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette] | ||
| B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] |
Free format text: NOTIFICACAO DE ANUENCIA RELACIONADA COM O ART 229 DA LPI |
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| B06T | Formal requirements before examination [chapter 6.20 patent gazette] | ||
| B07A | Application suspended after technical examination (opinion) [chapter 7.1 patent gazette] | ||
| B09A | Decision: intention to grant [chapter 9.1 patent gazette] | ||
| B16A | Patent or certificate of addition of invention granted [chapter 16.1 patent gazette] |
Free format text: PRAZO DE VALIDADE: 10 (DEZ) ANOS CONTADOS A PARTIR DE 24/09/2020, OBSERVADAS AS CONDICOES LEGAIS. |
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