CR20170332A - Derivados de fumagilol - Google Patents

Derivados de fumagilol

Info

Publication number
CR20170332A
CR20170332A CR20170332A CR20170332A CR20170332A CR 20170332 A CR20170332 A CR 20170332A CR 20170332 A CR20170332 A CR 20170332A CR 20170332 A CR20170332 A CR 20170332A CR 20170332 A CR20170332 A CR 20170332A
Authority
CR
Costa Rica
Prior art keywords
compounds
fumagilol
derivatives
stereoisomers
formula
Prior art date
Application number
CR20170332A
Other languages
English (en)
Inventor
John David Lawson
Christopher Mcbride
Zacharia Cheruvallath
Original Assignee
Takeda Pharmaceuticals Co
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Takeda Pharmaceuticals Co filed Critical Takeda Pharmaceuticals Co
Publication of CR20170332A publication Critical patent/CR20170332A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65586—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22—Hormones
    • A61K38/28—Insulins
    • 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
    • A61K31/13—Amines
    • A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
    • 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
    • A61K31/495—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
    • A61K31/4985—Pyrazines or piperazines 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
    • A61K31/64—Sulfonylureas, e.g. glibenclamide, tolbutamide, chlorpropamide
    • 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
    • A61K31/66—Phosphorus compounds
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/662—Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/665—Phosphorus compounds having oxygen as a ring hetero atom, e.g. fosfomycin
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/683—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Obesity (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Epoxy Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Se divulgan los compuestos de Fórmula 1, estereoisómeros de estos y sales farmacéuticamente aceptables de los compuestos y estereoisómeros, donde R1 y R2 se definen en la especificación. Esta descripción también se refiere a los materiales y métodos para preparar los compuestos de Fórmula 1, a las composiciones farmacéuticas que los contienen y a su uso para tratar la obesidad y enfermedades relacionadas, trastornos y desórdenes relacionados con MetAP2.
CR20170332A 2014-12-19 2015-12-18 Derivados de fumagilol CR20170332A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462094823P 2014-12-19 2014-12-19
PCT/US2015/066594 WO2016100778A1 (en) 2014-12-19 2015-12-18 Fumagillol derivatives

Publications (1)

Publication Number Publication Date
CR20170332A true CR20170332A (es) 2017-10-05

Family

ID=55071249

Family Applications (1)

Application Number Title Priority Date Filing Date
CR20170332A CR20170332A (es) 2014-12-19 2015-12-18 Derivados de fumagilol

Country Status (25)

Country Link
US (2) US9827255B2 (es)
EP (1) EP3233870B1 (es)
JP (1) JP2018500329A (es)
KR (1) KR20170099973A (es)
CN (1) CN107207547A (es)
AR (1) AR103078A1 (es)
AU (1) AU2015364477A1 (es)
BR (1) BR112017012965A2 (es)
CA (1) CA2971282A1 (es)
CL (1) CL2017001602A1 (es)
CO (1) CO2017007189A2 (es)
CR (1) CR20170332A (es)
DO (1) DOP2017000138A (es)
EA (1) EA032431B1 (es)
EC (1) ECSP17045054A (es)
ES (1) ES2702026T3 (es)
IL (1) IL252908A0 (es)
MX (1) MX2017007926A (es)
PE (1) PE20171141A1 (es)
PH (1) PH12017501134A1 (es)
SG (1) SG11201704985VA (es)
TN (1) TN2017000254A1 (es)
TW (1) TW201636342A (es)
UY (1) UY36450A (es)
WO (1) WO2016100778A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW201636342A (zh) 2014-12-19 2016-10-16 武田藥品工業有限公司 煙黴醇衍生物
EP3781262A4 (en) * 2018-04-20 2022-01-19 The University of Vermont and State Agriculture College COMPOSITIONS AND METHODS OF TREATING CARDIOVASCULAR DISEASE IN SELECTED PATIENTS

Family Cites Families (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PH26256A (en) 1988-08-12 1992-04-01 Fujisawa Pharmaceutical Co Oxaspiro [2,5] octane derivative
EP0359036B1 (en) 1988-09-01 1997-03-26 Takeda Chemical Industries, Ltd. Fumagillol derivatives
US5376645A (en) 1990-01-23 1994-12-27 University Of Kansas Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
KR0166088B1 (ko) 1990-01-23 1999-01-15 . 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도
GB9518953D0 (en) 1995-09-15 1995-11-15 Pfizer Ltd Pharmaceutical formulations
JPH1081631A (ja) * 1996-07-17 1998-03-31 Takeda Chem Ind Ltd 癌転移または再発抑制剤
GB9711643D0 (en) 1997-06-05 1997-07-30 Janssen Pharmaceutica Nv Glass thermoplastic systems
WO1998056372A1 (en) 1997-06-09 1998-12-17 Massachusetts Institute Of Technology TYPE 2 METHIONINE AMINOPEPTIDASE (MetAP2) INHIBITORS AND USES THEROF
DE69824750T2 (de) 1997-10-31 2005-07-07 Children's Medical Center Corp., Boston Methoden zur regulierung der grösse und des wachstums von durchblutetem normalem gewebe
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
EP1330447A2 (en) 2000-11-01 2003-07-30 Praecis Pharmaceuticals Incorporated Peptides as met-ap2 inhibitors
ATE440094T1 (de) 2001-09-27 2009-09-15 Equispharm Co Ltd Fumagillolderivate und verfahren zu deren herstellung
JP4514455B2 (ja) 2002-04-11 2010-07-28 チルドレンズ メディカル センター コーポレーション Ｔｎｐ−４７０ポリマー複合体及びその使用
KR100552043B1 (ko) 2004-02-28 2006-02-20 주식회사종근당 푸마질롤 유도체를 포함하는 비만치료용 조성물
US20100056623A1 (en) * 2005-01-26 2010-03-04 Chong Kun Dang Pharmaceutical Corp. Fumagillol derivatives or method for preparation of fumagillol derivatives, and pharmaceutical compositions comprising the same
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
BRPI0820229A2 (pt) 2007-11-28 2017-05-09 A Stevenson Cheri conjugados de análogos de fumagilina biodegradáveis biocompatíveis
US8299067B2 (en) 2008-03-27 2012-10-30 Versitech Limited 5-demethoxyfumagillol and derivatives thereof
US20120004162A1 (en) 2008-12-04 2012-01-05 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
EP2558072B1 (en) 2010-04-15 2018-09-26 The Washington University Prodrug compositions, prodrug nanoparticles, and methods of use thereof
US20130210821A1 (en) 2010-05-27 2013-08-15 James E. Vath Methods for Treating Obesity
AU2012225531B2 (en) * 2011-03-08 2017-03-30 Zafgen, Inc Oxaspiro (2.5) octane derivatives and analogs
FR2973376B1 (fr) 2011-03-28 2013-05-10 Atlanthera Derives utiles dans le traitement ou la prevention de tumeurs osseuses
TW201636342A (zh) 2014-12-19 2016-10-16 武田藥品工業有限公司 煙黴醇衍生物

Also Published As

Publication number Publication date
CN107207547A (zh) 2017-09-26
TW201636342A (zh) 2016-10-16
EA201791398A1 (ru) 2017-10-31
MX2017007926A (es) 2017-09-27
CL2017001602A1 (es) 2018-03-09
UY36450A (es) 2016-07-29
US20160175332A1 (en) 2016-06-23
CO2017007189A2 (es) 2017-10-20
JP2018500329A (ja) 2018-01-11
PE20171141A1 (es) 2017-08-09
AR103078A1 (es) 2017-04-12
IL252908A0 (en) 2017-08-31
ECSP17045054A (es) 2017-10-31
CA2971282A1 (en) 2016-06-23
KR20170099973A (ko) 2017-09-01
BR112017012965A2 (en) 2018-01-09
US20180050051A1 (en) 2018-02-22
TN2017000254A1 (en) 2018-10-19
EA032431B1 (ru) 2019-05-31
AU2015364477A1 (en) 2017-07-13
ES2702026T3 (es) 2019-02-27
SG11201704985VA (en) 2017-07-28
EP3233870B1 (en) 2018-10-31
DOP2017000138A (es) 2017-07-31
WO2016100778A1 (en) 2016-06-23
PH12017501134A1 (en) 2017-11-27
EP3233870A1 (en) 2017-10-25
US10328089B2 (en) 2019-06-25
US9827255B2 (en) 2017-11-28

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