ES2185338T3 - Derivados de fumagilol y procedimientos para su fabricacion. - Google Patents
Derivados de fumagilol y procedimientos para su fabricacion.Info
- Publication number
- ES2185338T3 ES2185338T3 ES99919688T ES99919688T ES2185338T3 ES 2185338 T3 ES2185338 T3 ES 2185338T3 ES 99919688 T ES99919688 T ES 99919688T ES 99919688 T ES99919688 T ES 99919688T ES 2185338 T3 ES2185338 T3 ES 2185338T3
- Authority
- ES
- Spain
- Prior art keywords
- substituted
- fumagilol
- halogen
- unsubstituted
- procedures
- 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.)
- Expired - Lifetime
Links
- 238000004519 manufacturing process Methods 0.000 title 1
- 238000000034 method Methods 0.000 title 1
- 229910052739 hydrogen Chemical group 0.000 abstract 3
- 239000001257 hydrogen Chemical group 0.000 abstract 3
- -1 hydroxy, acetoxy Chemical group 0.000 abstract 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical group [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000000738 acetamido group Chemical group [H]C([H])([H])C(=O)N([H])[*] 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000005530 alkylenedioxy group Chemical group 0.000 abstract 1
- 125000002431 aminoalkoxy group Chemical group 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 abstract 1
- 150000002431 hydrogen Chemical class 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
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
- C07D303/08—Compounds containing oxirane rings with hydrocarbon radicals, substituted by halogen atoms, nitro radicals or nitroso radicals
-
- 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
- C07D303/20—Ethers with hydroxy compounds containing no oxirane rings
- C07D303/22—Ethers with hydroxy compounds containing no oxirane rings with monohydroxy compounds
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
- 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
- C07D407/14—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 three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Epoxy Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Derivado de fumagilol representado por la Fórmula Química 1 o una sal del mismo farmacéuticamente aceptable: en la que, X representa un grupo hidroxi e Y representa un halógeno, o X e Y pueden formar un anillo oxiránico; B representa oxígeno o hidrógeno; y R1, R2, R3, R4 y R5 independientemente representan hidrógeno, hidroxi, acetoxi, amino substituido o no substituido, alquilo substituido o no substituido, aminoalcoxi substituido o no substituido, C1-C6 alcoxi, halógeno, ciano, trifuorometilo, nitro, alquilendioxi, formilo, acetamido o metilenoxicarboxilo, con la condición de que R1, R2, R3, R4 y R5 no representen hidrógeno al mismo tiempo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR19980017636 | 1998-05-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2185338T3 true ES2185338T3 (es) | 2003-04-16 |
Family
ID=19537397
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES99919688T Expired - Lifetime ES2185338T3 (es) | 1998-05-15 | 1999-05-11 | Derivados de fumagilol y procedimientos para su fabricacion. |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US6063812A (es) |
| EP (1) | EP1077964B1 (es) |
| JP (1) | JP3370985B2 (es) |
| KR (1) | KR100357542B1 (es) |
| CN (1) | CN100352810C (es) |
| AU (1) | AU3734699A (es) |
| CA (1) | CA2331873C (es) |
| DE (1) | DE69903279T2 (es) |
| ES (1) | ES2185338T3 (es) |
| WO (1) | WO1999059986A1 (es) |
Families Citing this family (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MXPA03003775A (es) | 2000-11-01 | 2003-07-28 | Praecis Pharm Inc | Peptidos como inhibidores de met-ap2. |
| US7105482B2 (en) | 2000-11-01 | 2006-09-12 | 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 |
| KR100455900B1 (ko) * | 2001-09-27 | 2004-11-12 | 주식회사 아이디알 | 새로운 푸마질롤 유도체 및 그의 제조방법 |
| KR100451485B1 (ko) * | 2002-03-28 | 2004-10-06 | 주식회사종근당 | 푸마질롤 유도체 또는 그 염의 포접 화합물, 및 이를포함하는 약제학적 조성물 |
| KR100552043B1 (ko) * | 2004-02-28 | 2006-02-20 | 주식회사종근당 | 푸마질롤 유도체를 포함하는 비만치료용 조성물 |
| JP2008528574A (ja) * | 2005-01-26 | 2008-07-31 | チョン クン ダン ファーマシューティカル コープ. | フマギロール誘導体またはフマギロール誘導体の製造方法およびこれを含む医薬用組成物 |
| EP1967175A1 (en) | 2007-03-06 | 2008-09-10 | Cognis IP Management GmbH | Use of derivatives of sinapinic acid and compositions comprising such derivatives |
| CA2706914A1 (en) * | 2007-11-28 | 2009-06-11 | Mersana Therapeutics, Inc. | Biocompatible biodegradable fumagillin analog conjugates |
| EP2317845A4 (en) * | 2008-07-18 | 2011-11-09 | Zafgen Inc | METHOD FOR TREATING AN OVERWEIGHT OR FATABLE PERSON |
| US8642650B2 (en) | 2008-12-04 | 2014-02-04 | Zafgen, Inc. | Methods of treating an overweight or obese subject |
| WO2010065877A2 (en) | 2008-12-04 | 2010-06-10 | Zafgen Corporation | Methods of treating an overweight or obese subject |
| AU2010303270A1 (en) | 2009-10-09 | 2012-05-03 | Zafgen Corporation | Sulphone compounds for use in the treatment of obesity |
| US8772333B2 (en) | 2010-01-08 | 2014-07-08 | Zafgen, Inc. | Fumigillol type compounds and methods of making and using same |
| WO2011085198A1 (en) | 2010-01-08 | 2011-07-14 | Zafgen Corporation | Metap-2 inhibitor for use in treating benign prostatic hypertrophy (bph) |
| WO2011088055A2 (en) | 2010-01-12 | 2011-07-21 | Zafgen Corporation | Methods and compositions for treating cardiovascular disorders |
| US20130266578A1 (en) | 2010-04-07 | 2013-10-10 | Thomas E. Hughes | Methods of treating an overweight subject |
| US9895449B2 (en) | 2010-05-25 | 2018-02-20 | Syndevrx, Inc. | Polymer-conjugated MetAP2 inhibitors, and therapeutic methods of use thereof |
| EP2576638B1 (en) | 2010-05-25 | 2020-12-23 | Syndevrx, Inc. | Polymer-conjugated metap2 inhibitors, and therapeutic methods of use thereof |
| US9266896B2 (en) | 2010-07-22 | 2016-02-23 | Zafgen, Inc. | Tricyclic compounds and methods of making and using same |
| PH12013500934A1 (en) * | 2010-11-09 | 2022-10-24 | Zafgen Inc | Crystalline solids of a metap-2 inhibitor and methods of making and using same |
| US20140073691A1 (en) | 2010-11-10 | 2014-03-13 | Zafgen, Inc. | Methods and composition for Treating Thyroid Hormone Related Disorders |
| WO2012075020A1 (en) | 2010-11-29 | 2012-06-07 | Zafgen Corporation | Treatment of obesity using non-daily administration of 6 - 0 - (4 - dimethylaminoethoxy) cinnamoyl fumagillol |
| US20130316994A1 (en) | 2010-11-29 | 2013-11-28 | Zafgen, Inc. | Methods of Reducing Risk of Hepatobiliary Dysfunction During Rapid Weight Loss with METAP-2 Inhibitors |
| US9189078B2 (en) | 2010-12-20 | 2015-11-17 | Apple Inc. | Enhancing keycap legend visibility with optical components |
| MX344238B (es) | 2011-01-26 | 2016-12-07 | Zafgen Inc | Compuestos de tetrazol y métodos para preparar y usar los mismos. |
| MX342257B (es) | 2011-03-08 | 2016-09-21 | Zafgen Inc | Derivados y análogos de oxaspiro [2.5] octano. |
| MX343688B (es) | 2011-05-06 | 2016-11-16 | Zafgen Inc | Compuestos tricíclicos de sulfonamida y pirazolo y métodos para su fabricación y uso. |
| US9187494B2 (en) | 2011-05-06 | 2015-11-17 | Zafgen, Inc. | Aryl-substituted tricyclic sulfonamides as methionyl aminopeptidase 2 modulators |
| EP2705030B1 (en) | 2011-05-06 | 2016-07-27 | Zafgen, Inc. | Partially saturated tricyclic compounds and methods of making and using same |
| EP2763671A2 (en) | 2011-10-03 | 2014-08-13 | Zafgen, Inc. | Methods of treating age related disorders |
| AU2013209719A1 (en) | 2012-01-18 | 2014-08-07 | Zafgen, Inc. | Tricyclic sulfone compounds and methods of making and using same |
| JP6035347B2 (ja) | 2012-01-18 | 2016-11-30 | ザフゲン,インコーポレイテッド | 三環式スルホンアミド化合物ならびにその作製および使用方法 |
| AU2013259760A1 (en) | 2012-05-07 | 2014-11-20 | Zafgen, Inc. | Polymorphic salt of the oxalate salt of 6-O-(4-dimethylaminoethoxy) cinnamoyl fumagillol and methods of making and using same |
| CN104363905A (zh) | 2012-05-08 | 2015-02-18 | 扎夫根股份有限公司 | 用metap2抑制剂治疗下丘脑性肥胖 |
| BR112014027981A2 (pt) | 2012-05-09 | 2017-06-27 | Zafgen Inc | compostos do tipo fumagilol e métodos de produção e utilização dos mesmos |
| CA2890344A1 (en) | 2012-11-05 | 2014-05-08 | Zafgen, Inc. | Tricyclic compounds for use in the treatment and/or control of obesity |
| BR112015010225A2 (pt) | 2012-11-05 | 2017-07-11 | Zafgen Inc | compostos tricíclicos e seus métodos de produção e utilização |
| EA028367B1 (ru) | 2012-11-05 | 2017-11-30 | Зафджен, Инк. | Способы лечения заболеваний печени |
| US9597309B2 (en) | 2013-03-14 | 2017-03-21 | Zafgen, Inc. | Methods of treating renal disease and other disorders |
| MX371095B (es) | 2013-04-10 | 2020-01-16 | Syndevrx Inc | Inhibidores de metionina aminopeptidasa-2 y metodos de tratamiento de la obesidad. |
| TW201636342A (zh) * | 2014-12-19 | 2016-10-16 | 武田藥品工業有限公司 | 煙黴醇衍生物 |
| CN106432255A (zh) | 2015-08-11 | 2017-02-22 | 扎夫根公司 | 烟曲霉素醇螺环化合物和制备和使用其的方法 |
| AR105671A1 (es) | 2015-08-11 | 2017-10-25 | Zafgen Inc | Compuestos heterocíclicos de fumagillol y sus métodos de elaboración y uso |
| KR20250127347A (ko) | 2015-12-10 | 2025-08-26 | 신데브알엑스, 인크. | 푸마길롤 유도체 및 그의 다형체 |
| 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 |
| CN121513211A (zh) | 2018-10-26 | 2026-02-13 | 辛德弗雷克斯公司 | Metap2抑制剂的生物标志物及其应用 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PH26256A (en) * | 1988-08-12 | 1992-04-01 | Fujisawa Pharmaceutical Co | Oxaspiro [2,5] octane derivative |
| CA1329771C (en) * | 1988-09-01 | 1994-05-24 | Shoji Kishimoto | Angiogenesis inhibitory agent |
| ATE97410T1 (de) * | 1989-03-06 | 1993-12-15 | Takeda Chemical Industries Ltd | 6-amino-6-desoxyfumagillole, ihre herstellung und ihre verwendung. |
| US5290807A (en) * | 1989-08-10 | 1994-03-01 | Children's Medical Center Corporation | Method for regressing angiogenesis using o-substituted fumagillol derivatives |
| EP0415294A3 (en) * | 1989-08-31 | 1991-06-12 | Takeda Chemical Industries, Ltd. | Cyclohexanol derivatives, production and use thereof |
| DE69330690T2 (de) * | 1992-01-30 | 2002-06-20 | Takeda Chemical Industries, Ltd. | Verfahren zur Herstellung hoch-wasserlöslicher Zyklodextrinkomplexe |
| EP0799616A1 (en) * | 1996-04-01 | 1997-10-08 | Takeda Chemical Industries, Ltd. | Oral composition comprising a fumagillol derivative |
-
1999
- 1999-05-07 KR KR1019990016320A patent/KR100357542B1/ko not_active Expired - Lifetime
- 1999-05-11 CN CNB998061883A patent/CN100352810C/zh not_active Expired - Lifetime
- 1999-05-11 CA CA002331873A patent/CA2331873C/en not_active Expired - Lifetime
- 1999-05-11 DE DE69903279T patent/DE69903279T2/de not_active Expired - Lifetime
- 1999-05-11 WO PCT/KR1999/000229 patent/WO1999059986A1/en not_active Ceased
- 1999-05-11 AU AU37346/99A patent/AU3734699A/en not_active Abandoned
- 1999-05-11 JP JP2000549605A patent/JP3370985B2/ja not_active Expired - Lifetime
- 1999-05-11 ES ES99919688T patent/ES2185338T3/es not_active Expired - Lifetime
- 1999-05-11 EP EP99919688A patent/EP1077964B1/en not_active Expired - Lifetime
- 1999-05-13 US US09/311,076 patent/US6063812A/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| US6063812A (en) | 2000-05-16 |
| CA2331873C (en) | 2005-12-06 |
| CN1301260A (zh) | 2001-06-27 |
| EP1077964A1 (en) | 2001-02-28 |
| KR19990088113A (ko) | 1999-12-27 |
| JP2002515497A (ja) | 2002-05-28 |
| KR100357542B1 (ko) | 2002-10-18 |
| DE69903279D1 (de) | 2002-11-07 |
| DE69903279T2 (de) | 2003-08-07 |
| WO1999059986A1 (en) | 1999-11-25 |
| CN100352810C (zh) | 2007-12-05 |
| AU3734699A (en) | 1999-12-06 |
| EP1077964B1 (en) | 2002-10-02 |
| JP3370985B2 (ja) | 2003-01-27 |
| CA2331873A1 (en) | 1999-11-25 |
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