CA2995366A1 - Fumagillol heterocyclic compounds and methods of making and using same - Google Patents

Fumagillol heterocyclic compounds and methods of making and using same Download PDF

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Publication number
CA2995366A1
CA2995366A1 CA2995366A CA2995366A CA2995366A1 CA 2995366 A1 CA2995366 A1 CA 2995366A1 CA 2995366 A CA2995366 A CA 2995366A CA 2995366 A CA2995366 A CA 2995366A CA 2995366 A1 CA2995366 A1 CA 2995366A1
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CA
Canada
Prior art keywords
carboxylate
methyl
methoxy
oxaspiro
methylbut
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.)
Abandoned
Application number
CA2995366A
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English (en)
French (fr)
Inventor
Robert Zahler
James E. Vath
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Larimar Therapeutics Inc
Original Assignee
Zafgen Inc
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Filing date
Publication date
Application filed by Zafgen Inc filed Critical Zafgen Inc
Publication of CA2995366A1 publication Critical patent/CA2995366A1/en
Abandoned legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • 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
    • 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
    • A61K31/4025—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
    • 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
    • A61K31/41—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
    • 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
    • A61K31/435—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
    • 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
    • A61K31/435—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
    • 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
    • A61K31/495—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
    • 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
    • A61K31/535—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
    • 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
    • A61K31/535—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
    • 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
    • A61K31/54—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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D405/02—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/08—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing alicyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • 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)
CA2995366A 2015-08-11 2016-08-11 Fumagillol heterocyclic compounds and methods of making and using same Abandoned CA2995366A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
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

Publications (1)

Publication Number Publication Date
CA2995366A1 true CA2995366A1 (en) 2017-02-16

Family

ID=56799580

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2995366A Abandoned CA2995366A1 (en) 2015-08-11 2016-08-11 Fumagillol heterocyclic compounds and methods of making and using same

Country Status (15)

Country Link
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=)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112014027981A2 (pt) 2012-05-09 2017-06-27 Zafgen Inc compostos do tipo fumagilol e métodos de produção e utilização dos mesmos
AR105671A1 (es) * 2015-08-11 2017-10-25 Zafgen Inc Compuestos heterocíclicos de fumagillol y sus métodos de elaboración y uso
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
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
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
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
CN111606836B (zh) * 2020-06-12 2021-01-15 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
GB202011996D0 (en) 2020-07-31 2020-09-16 Adorx Therapeutics Ltd Antagonist compounds

Family Cites Families (90)

* 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
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
US5180738A (en) 1988-09-01 1993-01-19 Takeda Chemical Industries Fumagillol derivatives and pharmaceutical compositions thereof
US5166172A (en) 1988-09-01 1992-11-24 Takeda Chemical Industries, Ltd. 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 (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
US5900431A (en) 1995-03-27 1999-05-04 Sanofi Use of fumagillol and derivatives thereof for preparing medicaments against intestinal infections
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
WO1998056372A1 (en) 1997-06-09 1998-12-17 Massachusetts Institute Of Technology TYPE 2 METHIONINE AMINOPEPTIDASE (MetAP2) INHIBITORS AND USES THEROF
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
EP1177176B1 (en) 1999-04-28 2006-04-19 Aventis Pharma Deutschland GmbH Tri-aryl acid derivatives as ppar receptor ligands
EP1223932A4 (en) 1999-10-01 2003-01-15 Smithkline Beecham Corp COMPOUNDS AND METHODS
US20030220371A1 (en) 2000-04-12 2003-11-27 Kallander Lara S. Compounds and methods
US6323228B1 (en) 2000-09-15 2001-11-27 Abbott Laboratories 3-substituted indole angiogenesis inhibitors
UY26929A1 (es) 2000-09-29 2002-04-26 Abbott Lab Polipéptidos antiangiogénicos y métodos para inhibir la angiogénesis
US6548477B1 (en) 2000-11-01 2003-04-15 Praecis Pharmaceuticals Inc. Therapeutic agents and methods of use thereof for the modulation of angiogenesis
BR0115109A (pt) 2000-11-01 2005-10-18 Praecis Pharm Inc Agentes terapêuticos e métodos de uso dos mesmos para a modulação da angiogênese
JP2004525942A (ja) 2001-03-29 2004-08-26 スミスクライン・ビーチャム・コーポレイション 化合物および方法
US20020183242A1 (en) 2001-04-11 2002-12-05 Jack Henkin Peptide antiangiogenic drugs
EP1436286B1 (en) 2001-09-27 2009-08-19 Equispharm Co., Ltd. Fumagillol derivatives and preparing method thereof
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
EP1512047A4 (en) 2002-06-12 2008-03-05 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
US7491718B2 (en) 2002-10-08 2009-02-17 Abbott Laboratories Sulfonamides having antiangiogenic and anticancer activity
US20040157836A1 (en) 2002-10-08 2004-08-12 Comess Kenneth M. 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
WO2005066197A2 (en) 2003-12-29 2005-07-21 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
EP1781303A4 (en) 2004-06-30 2008-07-02 Combinatorx Inc METHOD AND REAGENTS FOR THE TREATMENT OF METABOLISM DISEASES
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
CN101142210A (zh) 2005-01-26 2008-03-12 株式会社钟根堂 烟曲霉醇衍生物或制备烟曲霉醇衍生物的方法、以及包含该衍生物的药物组合物
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
US20070078172A1 (en) 2005-06-16 2007-04-05 Jenrin Discovery Mao-b inhibitors useful for treating obesity
EP2170402B1 (en) 2007-06-26 2015-03-25 Children's Medical Center Corporation Metap-2 inhibitor polymersomes for therapeutic administration
EP2217283A2 (en) * 2007-11-28 2010-08-18 Mersana Therapeutics, Inc. Biocompatible biodegradable fumagillin analog conjugates
US8299067B2 (en) * 2008-03-27 2012-10-30 Versitech Limited 5-demethoxyfumagillol and derivatives thereof
US8865746B2 (en) 2008-07-18 2014-10-21 Zafgen, Inc. Methods of treating an overweight or obese subject
ES2641471T3 (es) 2008-10-06 2017-11-10 The Johns Hopkins University Compuestos de quinolina como inhibidores de la angiogénesis, metionina aminopeptidasa humana, y SirT1, y procedimientos de tratamiento de trastornos
US8906896B2 (en) 2008-10-24 2014-12-09 Ulrich Bierbach Platinum acridine anti-cancer compounds and methods thereof
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
WO2013055385A2 (en) 2011-10-03 2013-04-18 Zafgen Corporation Methods of treating age related disorders
US8642650B2 (en) 2008-12-04 2014-02-04 Zafgen, Inc. Methods 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
CA2777108A1 (en) 2009-10-09 2011-04-14 Zafgen Corporation Sulphone compounds and methods of making and using same
BR112012016793A2 (pt) 2010-01-08 2018-07-31 Zafgen Corp compostos tipo fumagilol e métodos de fazer e usar os mesmos
US8815309B2 (en) 2010-01-08 2014-08-26 Zafgen, Inc. Methods of treating a subject with benign prostate hyperplasia
WO2011088055A2 (en) 2010-01-12 2011-07-21 Zafgen Corporation Methods and compositions for treating cardiovascular disorders
WO2011127304A2 (en) 2010-04-07 2011-10-13 Zafgen Corporation Methods of treating an overweight subject
US20130210821A1 (en) 2010-05-27 2013-08-15 James E. Vath Methods for Treating Obesity
CN103249735B (zh) 2010-07-22 2016-04-06 扎夫根股份有限公司 三环化合物及其制备和使用方法
US9221787B2 (en) 2010-10-12 2015-12-29 Zafgen, Inc. Sulphonamine 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
WO2012064928A1 (en) 2010-11-10 2012-05-18 Zafgen Corporation Methods and compositions for treating thyroid hormone related disorders
US9173865B2 (en) 2010-11-29 2015-11-03 Zafgen, Inc. Treatment of obesity using non-daily administration of 6-O-(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
WO2012074968A1 (en) 2010-11-29 2012-06-07 Zafgen Corporation Methods of reducing risk of hepatobiliary dysfunction during rapid weight loss with metap-2 inhibitors
MX344238B (es) 2011-01-26 2016-12-07 Zafgen Inc Compuestos de tetrazol y métodos para preparar y usar los mismos.
EP2683706B1 (en) 2011-03-08 2018-02-21 Zafgen, Inc. Oxaspiro [2.5]octane derivatives and analogs
EP2705036B1 (en) 2011-05-06 2015-08-12 Zafgen Inc. Tricyclic sulfonamide compounds and methods of making and using same
CN103764641B (zh) 2011-05-06 2016-10-26 扎夫根股份有限公司 部分饱和的三环化合物及其制备和使用方法
BR112013028666A2 (pt) 2011-05-06 2017-08-08 Zafgen Inc compostos de pirazolo sulfonamida tricícilos e métodos para fazer e usar o mesmo
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
JP2015509102A (ja) 2012-01-18 2015-03-26 ザフゲン，インコーポレイテッド 三環式スルホン化合物並びにその作製および使用方法
MX2014008706A (es) 2012-01-18 2015-03-05 Zafgen Inc Compuestos tricíclicos de sulfonamida y métodos para elaborarlos y usarlos.
BR112014027808A2 (pt) 2012-05-07 2017-06-27 Zafgen Inc sal polimórfico do sal de oxalato de 6-o-(4-dimetilaminoetoxi) cinaroil fumagilol e métodos de produção e utilização do mesmo
MX2014013599A (es) 2012-05-08 2015-05-11 Zafgen Inc Tratamiento de la obesidad hipotalamica con inhibidores de metap2.
BR112014027981A2 (pt) * 2012-05-09 2017-06-27 Zafgen Inc compostos do tipo fumagilol e métodos de produção e utilização dos mesmos
CN105228610A (zh) 2013-03-14 2016-01-06 扎夫根股份有限公司 治疗肾疾病和其它病症的方法
AR105671A1 (es) * 2015-08-11 2017-10-25 Zafgen Inc Compuestos heterocíclicos de fumagillol y sus métodos de elaboración y uso

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