CN108026085A - 烟曲霉素醇杂环化合物以及制备和使用其的方法 - Google Patents

烟曲霉素醇杂环化合物以及制备和使用其的方法 Download PDF

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Publication number
CN108026085A
CN108026085A CN201680054518.0A CN201680054518A CN108026085A CN 108026085 A CN108026085 A CN 108026085A CN 201680054518 A CN201680054518 A CN 201680054518A CN 108026085 A CN108026085 A CN 108026085A
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bases
methyl
azetidine
octane
formic acid
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CN201680054518.0A
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Chinese (zh)
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R·扎赫勒
J·E·瓦特
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Larimar Therapeutics Inc
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Zafgen Inc
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more 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
    • A61K31/33—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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • 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
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
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    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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  • Chemical & Material Sciences (AREA)
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  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
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  • Diabetes (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Child & Adolescent Psychology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Epoxy Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN201680054518.0A 2015-08-11 2016-08-11 烟曲霉素醇杂环化合物以及制备和使用其的方法 Pending CN108026085A (zh)

Applications Claiming Priority (3)

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US201562203742P 2015-08-11 2015-08-11
US62/203,742 2015-08-11
PCT/US2016/046511 WO2017027684A1 (en) 2015-08-11 2016-08-11 Fumagillol heterocyclic compounds and methods of making and using same

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CN108026085A true CN108026085A (zh) 2018-05-11

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US (5) US20180230137A1 (https=)
EP (1) EP3334728A1 (https=)
JP (1) JP2018522929A (https=)
KR (1) KR20180035907A (https=)
CN (1) CN108026085A (https=)
AR (1) AR105671A1 (https=)
AU (1) AU2016306558A1 (https=)
CA (1) CA2995366A1 (https=)
EA (1) EA201890449A1 (https=)
IL (1) IL257443A (https=)
MA (1) MA42612A (https=)
MX (1) MX2018001733A (https=)
PH (1) PH12018500315A1 (https=)
TW (1) TW201718550A (https=)
WO (1) WO2017027684A1 (https=)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109180551A (zh) * 2018-07-17 2019-01-11 宜春学院 一种四元氮杂环中间体的制备方法
CN111606836A (zh) * 2020-06-12 2020-09-01 上海馨远医药科技有限公司 一种R-N-Boc-3-吡咯烷乙酸的制备方法

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013169860A1 (en) 2012-05-09 2013-11-14 Zafgen, Inc. Fumigillol type compounds and methods of making and using same
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
WO2018148638A1 (en) * 2017-02-10 2018-08-16 Zafgen, Inc. Pharmaceutical compositions of metap-2 inhibitors
WO2019118612A1 (en) * 2017-12-12 2019-06-20 Zafgen, Inc. Targeting compounds
WO2019173505A1 (en) * 2018-03-06 2019-09-12 Zafgen, Inc. Methods of treating disorders related to glycemic control
JP2022512826A (ja) 2018-10-26 2022-02-07 シンデブルックス，インコーポレイティド ＭｅｔＡＰ２阻害剤のバイオマーカーとその応用
GB202011996D0 (en) 2020-07-31 2020-09-16 Adorx Therapeutics Ltd Antagonist compounds

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0354787A1 (en) * 1988-08-12 1990-02-14 Fujisawa Pharmaceutical Co., Ltd. Oxaspiro[2,5]octane derivative
WO2009073445A2 (en) * 2007-11-28 2009-06-11 Mersana Therapeutics, Inc. Biocompatible biodegradable fumagillin analog conjugates
CN103534244A (zh) * 2011-03-08 2014-01-22 扎夫根股份有限公司 氧杂螺[2.5]辛烷衍生物及类似物
CN104364251A (zh) * 2012-05-09 2015-02-18 扎夫根股份有限公司 烟曲霉醇型化合物及其制备和使用方法

Family Cites Families (86)

* Cited by examiner, † Cited by third party
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
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
EP0682020A1 (en) 1988-09-01 1995-11-15 Takeda Chemical Industries, Ltd. Fumagillol derivatives useful as angiogenesis inhibitors
ATE87623T1 (de) 1989-03-06 1993-04-15 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
US5290807A (en) 1989-08-10 1994-03-01 Children's Medical Center Corporation Method for regressing angiogenesis using o-substituted fumagillol derivatives
US6017954A (en) 1989-08-10 2000-01-25 Children's Medical Center Corp. Method of treating tumors using O-substituted fumagillol derivatives
EP0415294A3 (en) 1989-08-31 1991-06-12 Takeda Chemical Industries, Ltd. Cyclohexanol derivatives, production and use thereof
TW282399B (https=) 1990-05-25 1996-08-01 Takeda Pharm Industry Co Ltd
ATE205092T1 (de) 1992-01-30 2001-09-15 Takeda Chemical Industries Ltd Verfahren zur herstellung hoch-wasserlöslicher zyklodextrinkomplexe
EP0602586B1 (en) 1992-12-16 1997-06-04 Takeda Chemical Industries, Ltd. Stable pharmaceutical composition of fumagillol derivatives
UA41446C2 (uk) 1995-03-27 2001-09-17 Санофі - Сінтелабо Застосування фумагілолу та його похідних для одержання ліків, призначених для боротьби з кишковими інфекціями, та фармацевтична композиція на їх основі
CA2234401A1 (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
AU3968597A (en) 1996-08-02 1998-02-25 Children's Medical Center Corporation Method of regulating the female reproductive system through angiogenesis inhibitors
US6281245B1 (en) 1996-10-28 2001-08-28 Versicor, Inc. Methods for solid-phase synthesis of hydroxylamine compounds and derivatives, and combinatorial libraries thereof
US6207704B1 (en) 1997-06-09 2001-03-27 Massachusetts Institute Of Technology Type 2 methionine aminopeptidase [MetAP2] inhibitors and uses thereof
US6306819B1 (en) 1997-10-31 2001-10-23 Massachusetts Institute Of Technology Method for regulating size of vascularized normal tissue
US6242494B1 (en) 1998-05-01 2001-06-05 Abbott Laboratories Substituted β-amino acid inhibitors of methionine aminopeptidase-2
KR100357542B1 (ko) 1998-05-15 2002-10-18 주식회사종근당 푸마질롤 유도체 및 그 제조방법
KR100357541B1 (ko) 1998-05-15 2002-10-18 주식회사종근당 5-데메톡시 푸마질롤 유도체 및 그 제조방법
KR100293504B1 (ko) 1998-06-05 2001-07-12 김윤 서방형전립선염치료제조성물
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
PL351470A1 (en) 1999-04-28 2003-04-22 Aventis Pharma Gmbh Tri-aryl acid derivatives as ppar receptor ligands
EP1223932A4 (en) 1999-10-01 2003-01-15 Smithkline Beecham Corp COMPOUNDS AND METHODS
WO2001078723A1 (en) 2000-04-12 2001-10-25 Smithkline Beecham Corporation Compounds and methods
US6323228B1 (en) 2000-09-15 2001-11-27 Abbott Laboratories 3-substituted indole angiogenesis inhibitors
PE20020376A1 (es) 2000-09-29 2002-05-13 Abbott Lab Polipeptidos antiangiogenicos y metodos para inhibir la angiogenesis
US6548477B1 (en) 2000-11-01 2003-04-15 Praecis Pharmaceuticals Inc. Therapeutic agents and methods of use thereof for the modulation of angiogenesis
AU3947902A (en) 2000-11-01 2002-06-03 Praecis Pharm Inc Therapeutic agents and methods of use thereof for the modulation of angiogenesis
EP1379241A1 (en) 2001-03-29 2004-01-14 SmithKline Beecham Corporation Compounds and methods
US20020183242A1 (en) 2001-04-11 2002-12-05 Jack Henkin Peptide antiangiogenic drugs
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
US6877863B2 (en) 2002-06-12 2005-04-12 Silicon Optix Inc. Automatic keystone correction system and method
US6989392B2 (en) 2002-06-18 2006-01-24 Abbott Laboratories 2-Aminoquinolines as melanin concentrating hormone receptor antagonists
US7030262B2 (en) 2002-08-06 2006-04-18 Abbott Laboratories 3-Amino-2-hydroxyalkanoic acids and their prodrugs
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
US7491718B2 (en) 2002-10-08 2009-02-17 Abbott Laboratories Sulfonamides having antiangiogenic and anticancer activity
US20040204472A1 (en) 2003-03-04 2004-10-14 Pharmacia Corporation Treatment and prevention of obesity with COX-2 inhibitors alone or in combination with weight-loss agents
EP1699812A2 (en) 2003-12-29 2006-09-13 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
JP2008505176A (ja) 2004-06-30 2008-02-21 コンビナトアールエックス インコーポレーティッド 代謝障害を治療するための方法および試薬
WO2006010498A2 (en) 2004-07-28 2006-02-02 Bayer Healthcare Ag Diagnostics and therapeutics for diseases associated with methionine aminopeptidase 2 (metap2)
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
JP2010531896A (ja) 2007-06-26 2010-09-30 チルドレンズ メディカル センター コーポレーション 治療的投与のためのＭｅｔＡＰ−２阻害剤ポリマーソーム
US8299067B2 (en) * 2008-03-27 2012-10-30 Versitech Limited 5-demethoxyfumagillol and derivatives thereof
CA2731020A1 (en) 2008-07-18 2010-01-21 Zafgen, Inc. Use of antiangiogenic fumagillins in the treatment of obesity
CN102239149B (zh) 2008-10-06 2015-05-13 约翰·霍普金斯大学 喹啉化合物作为血管新生、人类甲硫氨酰氨肽酶、以及sirt1的抑制剂,以及治疗病症的方法
WO2010048499A1 (en) 2008-10-24 2010-04-29 Wake Forest University Platinum acridine anti-cancer compounds and methods thereof
WO2010065881A2 (en) 2008-12-04 2010-06-10 Zafgen Corporation Methods of treating an overweight or obese subject
WO2013055385A2 (en) 2011-10-03 2013-04-18 Zafgen Corporation Methods of treating age related disorders
US20120010290A1 (en) 2008-12-04 2012-01-12 Vath James E Methods of Treating an Overweight or Obese Subject
US8642650B2 (en) 2008-12-04 2014-02-04 Zafgen, Inc. Methods of treating an overweight or obese subject
US20120004162A1 (en) 2008-12-04 2012-01-05 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.
JP5827239B2 (ja) 2010-01-08 2015-12-02 ザフゲン，インコーポレイテッド フマギロール型化合物並びにその製造方法及び使用方法
US8815309B2 (en) 2010-01-08 2014-08-26 Zafgen, Inc. Methods of treating a subject with benign prostate hyperplasia
US20130023513A1 (en) 2010-01-12 2013-01-24 Hughes Thomas E Methods and Compositions for Treating Cardiovascular Disorders
US20130266578A1 (en) 2010-04-07 2013-10-10 Thomas E. Hughes Methods of treating an overweight subject
WO2011150338A1 (en) 2010-05-27 2011-12-01 Zafgen Corporation Methods of treating obesity
AU2011281037B2 (en) 2010-07-22 2014-11-27 Zafgen, Inc. Tricyclic compounds and methods of making and using same
MX339201B (es) 2010-10-12 2016-05-13 Zafgen Inc Compuestos de sulfonamida y métodos para elaborarlos y usarlos.
PH12013500934A1 (en) 2010-11-09 2022-10-24 Zafgen Inc Crystalline solids of a metap-2 inhibitor and methods of making and using same
WO2012064928A1 (en) 2010-11-10 2012-05-18 Zafgen Corporation Methods and compositions for treating thyroid hormone related disorders
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
AU2011336785A1 (en) 2010-11-29 2013-06-20 Zafgen, Inc Treatment of obesity using non-daily administration of 6-0-(4 - dimethylaminoethoxy) cinnamoyl fumagillol
WO2012075026A1 (en) 2010-11-29 2012-06-07 Zafgen Corporation Methods of treating obesity using an effective dose of a metap-2 inhibitor
WO2012103333A1 (en) 2011-01-26 2012-08-02 Zafgen Corporation Tetrazole compounds and methods of making and using same
SG194812A1 (en) 2011-05-06 2013-12-30 Zafgen Inc Partially saturated tricyclic compounds and methods of making and using same
CN103748094B (zh) 2011-05-06 2016-06-29 扎夫根股份有限公司 三环磺酰胺化合物及其制备和使用方法
US9242997B2 (en) 2011-05-06 2016-01-26 Zafgen, Inc. Tricyclic pyrazole sulphonamide compunds and methods of making and using same
WO2013033430A1 (en) 2011-09-02 2013-03-07 Wake Forest School Of Medicine Targeted delivery and prodrug designs for platinum-acridine anti-cancer compounds and methods thereof
BR112014017673A8 (pt) 2012-01-18 2017-07-11 Zafgen Inc Compostos de sulfonamida tricíclicos e métodos para fazer e usar os mesmos
WO2013109735A1 (en) 2012-01-18 2013-07-25 Zafgen, Inc. Tricyclic sulfone compounds and methods of making and using same
WO2013169727A1 (en) 2012-05-07 2013-11-14 Zafgen, Inc. Polymorphic salt of the oxalate salt of 6 - o - ( 4 - dimethylaminoethoxy) cinnarnoyl fumagillol and methods of making and using same
EP2846792B1 (en) 2012-05-08 2018-08-15 Zafgen, Inc. Treating hypothalamic obesity with metap2 inhibitors
US9597309B2 (en) 2013-03-14 2017-03-21 Zafgen, Inc. Methods of treating renal disease and other disorders
AR105671A1 (es) * 2015-08-11 2017-10-25 Zafgen Inc Compuestos heterocíclicos de fumagillol y sus métodos de elaboración y uso

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0354787A1 (en) * 1988-08-12 1990-02-14 Fujisawa Pharmaceutical Co., Ltd. Oxaspiro[2,5]octane derivative
WO2009073445A2 (en) * 2007-11-28 2009-06-11 Mersana Therapeutics, Inc. Biocompatible biodegradable fumagillin analog conjugates
CN103534244A (zh) * 2011-03-08 2014-01-22 扎夫根股份有限公司 氧杂螺[2.5]辛烷衍生物及类似物
CN104364251A (zh) * 2012-05-09 2015-02-18 扎夫根股份有限公司 烟曲霉醇型化合物及其制备和使用方法

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
CHRISTOPHER, ET AL.,: "Carbamate analogues of fumagillin as potent, targeted inhibitors of methionine aminopeptidase-2,", 《J.MED.CHEM》 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109180551A (zh) * 2018-07-17 2019-01-11 宜春学院 一种四元氮杂环中间体的制备方法
CN111606836A (zh) * 2020-06-12 2020-09-01 上海馨远医药科技有限公司 一种R-N-Boc-3-吡咯烷乙酸的制备方法

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