JP2015516425A5 - - Google Patents
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- Publication number
- JP2015516425A5 JP2015516425A5 JP2015511606A JP2015511606A JP2015516425A5 JP 2015516425 A5 JP2015516425 A5 JP 2015516425A5 JP 2015511606 A JP2015511606 A JP 2015511606A JP 2015511606 A JP2015511606 A JP 2015511606A JP 2015516425 A5 JP2015516425 A5 JP 2015516425A5
- Authority
- JP
- Japan
- Prior art keywords
- crystalline form
- solution
- powder
- diffraction pattern
- dimethylaminoethoxy
- 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.)
- Withdrawn
Links
- 239000000243 solution Substances 0.000 claims 9
- CEVCTNCUIVEQOY-UHFFFAOYSA-N Fumagillol Natural products O1C(CC=C(C)C)C1(C)C1C(OC)C(O)CCC21CO2 CEVCTNCUIVEQOY-UHFFFAOYSA-N 0.000 claims 6
- -1 cinnamoyl fumagillol Chemical compound 0.000 claims 6
- 238000000634 powder X-ray diffraction Methods 0.000 claims 6
- 238000010438 heat treatment Methods 0.000 claims 5
- 239000013078 crystal Substances 0.000 claims 4
- 238000004519 manufacturing process Methods 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims 3
- IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical compound CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 238000001816 cooling Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 239000002244 precipitate Substances 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 238000000425 proton nuclear magnetic resonance spectrum Methods 0.000 claims 1
- 230000005855 radiation Effects 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 238000007920 subcutaneous administration Methods 0.000 claims 1
- 238000010254 subcutaneous injection Methods 0.000 claims 1
- 239000007929 subcutaneous injection Substances 0.000 claims 1
- 239000000725 suspension Substances 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261643586P | 2012-05-07 | 2012-05-07 | |
| US61/643,586 | 2012-05-07 | ||
| PCT/US2013/039877 WO2013169727A1 (en) | 2012-05-07 | 2013-05-07 | Polymorphic salt of the oxalate salt of 6 - o - ( 4 - dimethylaminoethoxy) cinnarnoyl fumagillol and methods of making and using same |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2015516425A JP2015516425A (ja) | 2015-06-11 |
| JP2015516425A5 true JP2015516425A5 (OSRAM) | 2016-06-23 |
Family
ID=48446683
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015511606A Withdrawn JP2015516425A (ja) | 2012-05-07 | 2013-05-07 | ６−ｏ−（４−ジメチルアミノエトキシ）シンナモイルフマギロールのシュウ酸塩の多形塩ならびにその製造および使用方法 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US9260419B2 (OSRAM) |
| EP (1) | EP2847176A1 (OSRAM) |
| JP (1) | JP2015516425A (OSRAM) |
| KR (1) | KR20150016303A (OSRAM) |
| AU (1) | AU2013259760A1 (OSRAM) |
| BR (1) | BR112014027808A2 (OSRAM) |
| CA (1) | CA2872649A1 (OSRAM) |
| IL (1) | IL235521A (OSRAM) |
| MX (1) | MX2014013525A (OSRAM) |
| WO (1) | WO2013169727A1 (OSRAM) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011085198A1 (en) | 2010-01-08 | 2011-07-14 | Zafgen Corporation | Metap-2 inhibitor for use in treating benign prostatic hypertrophy (bph) |
| WO2011127304A2 (en) | 2010-04-07 | 2011-10-13 | Zafgen Corporation | Methods of treating an overweight subject |
| EP2763671A2 (en) | 2011-10-03 | 2014-08-13 | Zafgen, Inc. | Methods of treating age related disorders |
| EP2846792B1 (en) | 2012-05-08 | 2018-08-15 | Zafgen, Inc. | Treating hypothalamic obesity with metap2 inhibitors |
| JP6177888B2 (ja) | 2012-05-09 | 2017-08-09 | ザフゲン，インコーポレイテッド | フマギロール型化合物ならびにその製造および使用方法 |
| US9597309B2 (en) | 2013-03-14 | 2017-03-21 | Zafgen, Inc. | Methods of treating renal disease and other disorders |
| 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 |
Family Cites Families (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5164410A (en) | 1988-01-09 | 1992-11-17 | Takeda Chemical Industries, Ltd. | Fumagillol derivatives and pharmaceutical compositions thereof |
| PH26256A (en) | 1988-08-12 | 1992-04-01 | Fujisawa Pharmaceutical Co | Oxaspiro [2,5] octane derivative |
| KR0138530B1 (ko) | 1988-09-01 | 1998-05-15 | 우메모또 요시마사 | 푸마길롤 유도체 |
| US5166172A (en) | 1988-09-01 | 1992-11-24 | Takeda Chemical Industries, Ltd. | Fumagillol derivatives and pharmaceutical compositions thereof |
| US5180738A (en) | 1988-09-01 | 1993-01-19 | Takeda Chemical Industries | Fumagillol derivatives and pharmaceutical compositions thereof |
| DE69001187T2 (de) | 1989-03-06 | 1993-07-08 | Takeda Chemical Industries Ltd | 6-epifumagillole, ihre herstellung und ihre verwendung. |
| US5288722A (en) | 1989-03-06 | 1994-02-22 | Takeda Chemical Industries, Ltd. | 6-amino-6-desoxyfumagillols, production and use thereof |
| US6017954A (en) | 1989-08-10 | 2000-01-25 | Children's Medical Center Corp. | Method of treating tumors using O-substituted fumagillol derivatives |
| 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 |
| TW282399B (OSRAM) | 1990-05-25 | 1996-08-01 | Takeda Pharm Industry Co Ltd | |
| DE69330690T2 (de) | 1992-01-30 | 2002-06-20 | Takeda Chemical Industries, Ltd. | Verfahren zur Herstellung hoch-wasserlöslicher Zyklodextrinkomplexe |
| DE69311278T2 (de) | 1992-12-16 | 1997-10-30 | Takeda Chemical Industries Ltd | Stabile pharmazeutische Zubereitung mit Fumagillolderivaten |
| HU224028B1 (hu) | 1995-03-27 | 2005-05-30 | Assistance Publique-Hopitaux De Paris | Fumagillol és származékai alkalmazása bélfertőzések kezelésére szolgáló gyógyszerek előállítására |
| WO1997013509A1 (en) | 1995-10-11 | 1997-04-17 | Fujisawa Pharmaceutical Co., Ltd. | Vascular permeation inhibitor |
| EP0799616A1 (en) | 1996-04-01 | 1997-10-08 | Takeda Chemical Industries, Ltd. | Oral composition comprising a fumagillol derivative |
| WO1998005293A2 (en) | 1996-08-02 | 1998-02-12 | The Children's Medical Center Corporation | Method of regulating the female reproductive system through angiogenesis inhibitors |
| US6207704B1 (en) | 1997-06-09 | 2001-03-27 | Massachusetts Institute Of Technology | Type 2 methionine aminopeptidase [MetAP2] inhibitors and uses thereof |
| JP2002502814A (ja) | 1997-10-31 | 2002-01-29 | チルドレンズ・メディカル・センター・コーポレイション | 血管化した正常組織の大きさおよび増殖の調節のための方法 |
| KR100357541B1 (ko) | 1998-05-15 | 2002-10-18 | 주식회사종근당 | 5-데메톡시 푸마질롤 유도체 및 그 제조방법 |
| KR100357542B1 (ko) | 1998-05-15 | 2002-10-18 | 주식회사종근당 | 푸마질롤 유도체 및 그 제조방법 |
| JP2000116337A (ja) | 1998-10-09 | 2000-04-25 | Nippon Shokuhin Kako Co Ltd | ペットフード |
| US6383471B1 (en) | 1999-04-06 | 2002-05-07 | Lipocine, Inc. | Compositions and methods for improved delivery of ionizable hydrophobic therapeutic agents |
| EE200100558A (et) | 1999-04-28 | 2002-12-16 | Aventis Pharma Deutschland Gmbh | Triarüülhappe derivaat, seda sisaldav farmatseutiline kompositsioon ja ühendi raviotstarbeline kasutamine |
| US6323228B1 (en) | 2000-09-15 | 2001-11-27 | Abbott Laboratories | 3-substituted indole angiogenesis inhibitors |
| AU2002239479B2 (en) | 2000-11-01 | 2006-11-09 | Praecis Pharmaceuticals Incorporated | Peptides as Met-AP2 inhibitors |
| US6548477B1 (en) | 2000-11-01 | 2003-04-15 | Praecis Pharmaceuticals Inc. | Therapeutic agents and methods of use thereof for the modulation of angiogenesis |
| DE60233420D1 (de) | 2001-09-27 | 2009-10-01 | Equispharm Co Ltd | Fumagillolderivate und verfahren zu deren herstellung |
| US6803382B2 (en) | 2001-11-09 | 2004-10-12 | Galderma Research & Development, S.N.C. | Angiogenesis inhibitors and pharmaceutical and cosmetic use thereof |
| KR100451485B1 (ko) | 2002-03-28 | 2004-10-06 | 주식회사종근당 | 푸마질롤 유도체 또는 그 염의 포접 화합물, 및 이를포함하는 약제학적 조성물 |
| US20040067266A1 (en) | 2002-10-07 | 2004-04-08 | Toppo Frank R. | Weight loss compound |
| US20040157836A1 (en) | 2002-10-08 | 2004-08-12 | Comess Kenneth M. | Sulfonamides having antiangiogenic and anticancer activity |
| WO2004078113A2 (en) | 2003-03-04 | 2004-09-16 | Pharmacia Corporation | Treatment and prevention of obesity with cox-2 inhibitors alone or in combination with weight-loss agents |
| US20050239878A1 (en) | 2003-12-29 | 2005-10-27 | Praecis Pharmaceuticals, Inc. | Inhibitors of methionine aminopeptidase-2 and uses thereof |
| KR100552043B1 (ko) * | 2004-02-28 | 2006-02-20 | 주식회사종근당 | 푸마질롤 유도체를 포함하는 비만치료용 조성물 |
| US20060045865A1 (en) | 2004-08-27 | 2006-03-02 | Spherics, Inc. | Controlled regional oral delivery |
| 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 |
| FR2886855B1 (fr) | 2005-06-08 | 2009-07-17 | Agronomique Inst Nat Rech | Utilisation de la fumagilline et de ses derives pour augmenter la biodisponibilite des lactones macrocyliques |
| WO2006138475A2 (en) | 2005-06-16 | 2006-12-28 | Jenrin Discovery | Mao-b inhibitors useful for treating obesity |
| BRPI0820229A2 (pt) | 2007-11-28 | 2017-05-09 | A Stevenson Cheri | conjugados de análogos de fumagilina biodegradáveis biocompatíveis |
| WO2010065877A2 (en) | 2008-12-04 | 2010-06-10 | Zafgen Corporation | Methods of treating an overweight or obese subject |
| WO2010065881A2 (en) | 2008-12-04 | 2010-06-10 | Zafgen Corporation | Methods of treating an overweight or obese subject |
| WO2010065883A2 (en) * | 2008-12-04 | 2010-06-10 | Zafgen Corporation | Method of treating an overweight or obese subject |
| US20120010290A1 (en) | 2008-12-04 | 2012-01-12 | Vath James E | Methods of Treating an Overweight or Obese Subject |
| MX337575B (es) | 2009-10-09 | 2016-03-10 | Zafgen Corp | Compuestos de sulfona y métodos para lafabricación y uso de éstos. |
| WO2011088055A2 (en) * | 2010-01-12 | 2011-07-21 | Zafgen Corporation | Methods and compositions for treating cardiovascular disorders |
| PH12013500934A1 (en) | 2010-11-09 | 2022-10-24 | Zafgen Inc | Crystalline solids of a metap-2 inhibitor and methods of making and using same |
| US8669360B2 (en) * | 2011-08-05 | 2014-03-11 | Boston Scientific Scimed, Inc. | Methods of converting amorphous drug substance into crystalline form |
-
2013
- 2013-05-07 KR KR20147033821A patent/KR20150016303A/ko not_active Withdrawn
- 2013-05-07 JP JP2015511606A patent/JP2015516425A/ja not_active Withdrawn
- 2013-05-07 CA CA 2872649 patent/CA2872649A1/en not_active Abandoned
- 2013-05-07 EP EP13723369.8A patent/EP2847176A1/en not_active Withdrawn
- 2013-05-07 MX MX2014013525A patent/MX2014013525A/es unknown
- 2013-05-07 BR BR112014027808A patent/BR112014027808A2/pt not_active IP Right Cessation
- 2013-05-07 US US14/399,387 patent/US9260419B2/en not_active Expired - Fee Related
- 2013-05-07 WO PCT/US2013/039877 patent/WO2013169727A1/en not_active Ceased
- 2013-05-07 AU AU2013259760A patent/AU2013259760A1/en not_active Abandoned
-
2014
- 2014-11-05 IL IL235521A patent/IL235521A/en active IP Right Grant
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