CA3005450A1 - Fumagillol derivatives and polymorphs thereof - Google Patents
Fumagillol derivatives and polymorphs thereof Download PDFInfo
- Publication number
- CA3005450A1 CA3005450A1 CA3005450A CA3005450A CA3005450A1 CA 3005450 A1 CA3005450 A1 CA 3005450A1 CA 3005450 A CA3005450 A CA 3005450A CA 3005450 A CA3005450 A CA 3005450A CA 3005450 A1 CA3005450 A1 CA 3005450A1
- Authority
- CA
- Canada
- Prior art keywords
- fumagill
- trans
- benzenesulfonic acid
- aminocyclohexyl
- acid salt
- 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.)
- Pending
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D303/00—Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
- C07D303/02—Compounds containing oxirane rings
- C07D303/12—Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms
- C07D303/18—Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by etherified hydroxyl radicals
- C07D303/31—Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by etherified hydroxyl radicals in which the oxirane rings are condensed with a carbocyclic ring system having three or more relevant rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
- C07D407/08—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a carbon chain containing alicyclic 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
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/336—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
- C07C309/01—Sulfonic acids
- C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
- C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C65/00—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
- C07C65/01—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups
- C07C65/105—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups polycyclic
- C07C65/11—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups polycyclic with carboxyl groups on a condensed ring system containing two rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D303/00—Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
- C07D303/02—Compounds containing oxirane rings
- C07D303/38—Compounds containing oxirane rings with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D303/46—Compounds containing oxirane rings with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals by amide or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Epoxy Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562265675P | 2015-12-10 | 2015-12-10 | |
| US62/265,675 | 2015-12-10 | ||
| PCT/US2016/065799 WO2017100553A1 (en) | 2015-12-10 | 2016-12-09 | Fumagillol derivatives and polymorphs thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3005450A1 true CA3005450A1 (en) | 2017-06-15 |
Family
ID=57589276
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3005450A Pending CA3005450A1 (en) | 2015-12-10 | 2016-12-09 | Fumagillol derivatives and polymorphs thereof |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US9969722B2 (https=) |
| EP (1) | EP3386956B1 (https=) |
| JP (2) | JP7553224B2 (https=) |
| KR (2) | KR102849342B1 (https=) |
| CN (1) | CN108290853B (https=) |
| AU (1) | AU2016366306B2 (https=) |
| CA (1) | CA3005450A1 (https=) |
| DK (1) | DK3386956T3 (https=) |
| ES (1) | ES2893749T3 (https=) |
| MX (2) | MX2018006904A (https=) |
| WO (1) | WO2017100553A1 (https=) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK2576638T3 (da) | 2010-05-25 | 2021-03-15 | Syndevrx Inc | Polymerkonjugerede metap2-inhibitorer og terapeutiske fremgangsmåder til anvendelse deraf |
| CN105431426A (zh) | 2013-04-10 | 2016-03-23 | 新德发制药有限公司 | Metap2抑制剂和治疗肥胖症的方法 |
| US9969722B2 (en) * | 2015-12-10 | 2018-05-15 | Syndevrx, Inc. | Fumagillol derivatives and polymorphs thereof |
| CN108697807B (zh) | 2016-01-11 | 2021-11-26 | 辛德弗雷克斯公司 | 代谢功能障碍引起的肿瘤的治疗 |
| CN113453721B (zh) | 2018-10-26 | 2025-09-16 | 辛德弗雷克斯公司 | Metap2抑制剂的生物标志物及其应用 |
| WO2024040009A2 (en) * | 2022-08-17 | 2024-02-22 | Primetime Life Sciences, Llc | Inhibitors of methionine aminopeptidase-2 and methods of preparation and uses thereof |
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| GB8500209D0 (en) | 1985-01-04 | 1985-02-13 | Ceskoslovenska Akademie Ved | Synthetic polymeric drugs |
| SE8702550D0 (sv) | 1987-06-18 | 1987-06-18 | Anders Grubb | Cysteinproteashemmare |
| US5166172A (en) | 1988-09-01 | 1992-11-24 | Takeda Chemical Industries, Ltd. | Fumagillol derivatives and pharmaceutical compositions thereof |
| US4997878A (en) | 1988-12-29 | 1991-03-05 | Exxon Research And Engineering Company | Hydrophobically associating polymers containing dimethyl acrylamide functionality |
| US5258453A (en) | 1992-01-21 | 1993-11-02 | University Of Utah | Drug delivery system for the simultaneous delivery of drugs activatable by enzymes and light |
| GB9320781D0 (en) | 1993-10-08 | 1993-12-01 | Erba Carlo Spa | Polymer-bound camptothecin derivatives |
| US20030220233A1 (en) | 1994-01-24 | 2003-11-27 | Neorx Corporation | Radiolabeled annexins |
| TW409058B (en) | 1996-06-06 | 2000-10-21 | Daiichi Seiyaku Co | Method for preparation of a drug complex |
| TW527183B (en) | 1996-06-06 | 2003-04-11 | Daiichi Seiyaku Co | Drug complex |
| US6759509B1 (en) | 1996-11-05 | 2004-07-06 | Bristol-Myers Squibb Company | Branched peptide linkers |
| WO1999011272A1 (en) | 1997-09-02 | 1999-03-11 | Johns Hopkins University School Of Medicine | Vitamin d3 analog loaded polymer formulations for cancer and neurodegenerative disorders |
| US6306819B1 (en) | 1997-10-31 | 2001-10-23 | Massachusetts Institute Of Technology | Method for regulating size of vascularized normal tissue |
| KR100357542B1 (ko) | 1998-05-15 | 2002-10-18 | 주식회사종근당 | 푸마질롤 유도체 및 그 제조방법 |
| HK1040052B (zh) | 1998-05-22 | 2006-09-15 | 第一制药株式会社 | 药物复合物 |
| US6464850B1 (en) | 1998-07-31 | 2002-10-15 | Biowhittaker Molecular Applications, Inc. | Method for producing hydrophilic monomers and uses thereof |
| ID29943A (id) | 1998-10-30 | 2001-10-25 | Daiichi Seiyaku Co | Senyawa dds dan metode pengukurannya |
| EP1222217B1 (en) | 1999-09-08 | 2005-06-15 | Polytherics Limited | Uniform molecular weight polymers |
| US6811788B2 (en) | 2000-01-19 | 2004-11-02 | Baofa Yu | Combinations and methods for treating neoplasms |
| US20070161570A1 (en) | 2000-11-01 | 2007-07-12 | Praecis Pharmaceuticals, Inc. | Methionine aminopeptidase-2 inhibitors and methods of use thereof |
| US6548477B1 (en) | 2000-11-01 | 2003-04-15 | Praecis Pharmaceuticals Inc. | Therapeutic agents and methods of use thereof for the modulation of angiogenesis |
| EP1243276A1 (en) | 2001-03-23 | 2002-09-25 | Franciscus Marinus Hendrikus De Groot | Elongated and multiple spacers containing activatible prodrugs |
| US7091186B2 (en) | 2001-09-24 | 2006-08-15 | Seattle Genetics, Inc. | p-Amidobenzylethers in drug delivery agents |
| EP1436286B1 (en) | 2001-09-27 | 2009-08-19 | Equispharm Co., Ltd. | Fumagillol derivatives and preparing method thereof |
| WO2003070173A2 (en) | 2002-02-15 | 2003-08-28 | Sympore Gmbh | Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof |
| AU2003230852B2 (en) | 2002-04-11 | 2008-07-10 | Children's Medical Center Corporation | TNP-470 polymer conjugates and use thereof |
| US20040001801A1 (en) | 2002-05-23 | 2004-01-01 | Corvas International, Inc. | Conjugates activated by cell surface proteases and therapeutic uses thereof |
| US20040116348A1 (en) | 2002-09-23 | 2004-06-17 | Ying Chau | Polymer-linker-drug conjugates for targeted drug delivery |
| US20040228831A1 (en) | 2003-05-15 | 2004-11-18 | Belinka Benjamin A. | Polymeric conjugates for tissue activated drug delivery |
| CN102321584B (zh) | 2003-12-31 | 2014-01-08 | 宾夕法尼亚州研究基金会 | 预测并克服对卵巢癌化疗的抗性的方法及预测结肠癌发生的方法 |
| US20070287680A1 (en) | 2004-05-10 | 2007-12-13 | University Of Utah Research Foundation | Combined Active and Passive Targeting of Biologically Active Agents |
| US7214664B2 (en) | 2004-12-03 | 2007-05-08 | The Curators Of The University Of Missouri | Peptidyl prodrugs that resist P-glycoprotein mediated drug efflux |
| WO2006084054A2 (en) | 2005-02-02 | 2006-08-10 | Children's Medical Center Corporation | Method of treating angiogenic diseases |
| US7629315B2 (en) | 2005-03-09 | 2009-12-08 | University Of Pittsburgh Of The Commonwealth System Of Higher Education | Compositions for blocking the inhibitory effect of human CRP on human leptin |
| WO2006124711A1 (en) | 2005-05-16 | 2006-11-23 | The Board Of Trustees Of The University Of Illinois | Composition and method for providing localized delivery of a therapeutic agent |
| EP2170402B1 (en) | 2007-06-26 | 2015-03-25 | Children's Medical Center Corporation | Metap-2 inhibitor polymersomes for therapeutic administration |
| WO2009036108A1 (en) | 2007-09-13 | 2009-03-19 | Children's Medical Center Corporation | Methods and compositions for inhibiting vascular leakage |
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| EP2217283A2 (en) | 2007-11-28 | 2010-08-18 | Mersana Therapeutics, Inc. | Biocompatible biodegradable fumagillin analog conjugates |
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| DE102008027574A1 (de) | 2008-06-10 | 2009-12-17 | Merck Patent Gmbh | Neue Pyrrolidinderivate als MetAP-2 Inhibitoren |
| WO2010065877A2 (en) | 2008-12-04 | 2010-06-10 | Zafgen Corporation | Methods of treating an overweight or obese subject |
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| TWI373345B (en) | 2009-02-19 | 2012-10-01 | Academia Sinica | Breast cancer-targeting peptides and use thereof |
| EP2493497A4 (en) | 2009-11-01 | 2013-07-24 | Brigham & Womens Hospital | NOTCH INHIBITION IN THE TREATMENT AND PROPHYLAXIS OF ADIPOSITAS AND METABOLISM SYNDROME |
| WO2011127304A2 (en) | 2010-04-07 | 2011-10-13 | Zafgen Corporation | Methods of treating an overweight subject |
| DK2576638T3 (da) | 2010-05-25 | 2021-03-15 | Syndevrx Inc | Polymerkonjugerede metap2-inhibitorer og terapeutiske fremgangsmåder til anvendelse deraf |
| US20110294952A1 (en) | 2010-05-25 | 2011-12-01 | SynDevRX | Optimized Drug Conjugates |
| US9895449B2 (en) | 2010-05-25 | 2018-02-20 | Syndevrx, Inc. | Polymer-conjugated MetAP2 inhibitors, and therapeutic methods of use thereof |
| PH12013500934A1 (en) | 2010-11-09 | 2022-10-24 | Zafgen Inc | Crystalline solids of a metap-2 inhibitor and methods of making and using same |
| EP2683706B1 (en) | 2011-03-08 | 2018-02-21 | Zafgen, Inc. | Oxaspiro [2.5]octane derivatives and analogs |
| BR112014027981A2 (pt) * | 2012-05-09 | 2017-06-27 | Zafgen Inc | compostos do tipo fumagilol e métodos de produção e utilização dos mesmos |
| CN105431426A (zh) * | 2013-04-10 | 2016-03-23 | 新德发制药有限公司 | Metap2抑制剂和治疗肥胖症的方法 |
| US9969722B2 (en) * | 2015-12-10 | 2018-05-15 | Syndevrx, Inc. | Fumagillol derivatives and polymorphs thereof |
| CN108697807B (zh) | 2016-01-11 | 2021-11-26 | 辛德弗雷克斯公司 | 代谢功能障碍引起的肿瘤的治疗 |
-
2016
- 2016-12-09 US US15/373,874 patent/US9969722B2/en active Active
- 2016-12-09 MX MX2018006904A patent/MX2018006904A/es unknown
- 2016-12-09 JP JP2018529646A patent/JP7553224B2/ja active Active
- 2016-12-09 WO PCT/US2016/065799 patent/WO2017100553A1/en not_active Ceased
- 2016-12-09 DK DK16816157.8T patent/DK3386956T3/da active
- 2016-12-09 CA CA3005450A patent/CA3005450A1/en active Pending
- 2016-12-09 CN CN201680072272.XA patent/CN108290853B/zh active Active
- 2016-12-09 ES ES16816157T patent/ES2893749T3/es active Active
- 2016-12-09 AU AU2016366306A patent/AU2016366306B2/en active Active
- 2016-12-09 EP EP16816157.8A patent/EP3386956B1/en active Active
- 2016-12-09 KR KR1020187019456A patent/KR102849342B1/ko active Active
- 2016-12-09 KR KR1020257027526A patent/KR20250127347A/ko active Pending
-
2018
- 2018-04-06 US US15/946,899 patent/US10287277B2/en active Active
- 2018-06-06 MX MX2023002589A patent/MX2023002589A/es unknown
-
2024
- 2024-05-02 JP JP2024074818A patent/JP7842805B2/ja active Active
Also Published As
| Publication number | Publication date |
|---|---|
| AU2016366306A1 (en) | 2018-05-31 |
| US10287277B2 (en) | 2019-05-14 |
| DK3386956T3 (da) | 2021-10-11 |
| KR20250127347A (ko) | 2025-08-26 |
| US20170166556A1 (en) | 2017-06-15 |
| JP2024103495A (ja) | 2024-08-01 |
| CN108290853A (zh) | 2018-07-17 |
| JP7842805B2 (ja) | 2026-04-08 |
| ES2893749T3 (es) | 2022-02-10 |
| KR20180093995A (ko) | 2018-08-22 |
| US20180291010A1 (en) | 2018-10-11 |
| EP3386956A1 (en) | 2018-10-17 |
| US9969722B2 (en) | 2018-05-15 |
| MX2023002589A (es) | 2023-03-22 |
| KR102849342B1 (ko) | 2025-08-21 |
| AU2016366306B2 (en) | 2021-02-25 |
| JP7553224B2 (ja) | 2024-09-18 |
| CN108290853B (zh) | 2022-05-31 |
| JP2019501898A (ja) | 2019-01-24 |
| WO2017100553A1 (en) | 2017-06-15 |
| HK1258254A1 (zh) | 2019-11-08 |
| MX2018006904A (es) | 2018-08-24 |
| EP3386956B1 (en) | 2021-07-14 |
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