EA201791398A1 - Производные фумагиллола - Google Patents

Производные фумагиллола

Info

Publication number
EA201791398A1
EA201791398A1 EA201791398A EA201791398A EA201791398A1 EA 201791398 A1 EA201791398 A1 EA 201791398A1 EA 201791398 A EA201791398 A EA 201791398A EA 201791398 A EA201791398 A EA 201791398A EA 201791398 A1 EA201791398 A1 EA 201791398A1
Authority
EA
Eurasian Patent Office
Prior art keywords
compounds
fumagillalle
derivatives
stereoisomers
formula
Prior art date
Application number
EA201791398A
Other languages
English (en)
Other versions
EA032431B1 (ru
Inventor
Зачариа Черуваллатх
Джон Дэвид Лоусон
Кристофер Макбрайд
Original Assignee
Такеда Фармасьютикал Компани Лимитед
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 Такеда Фармасьютикал Компани Лимитед filed Critical Такеда Фармасьютикал Компани Лимитед
Publication of EA201791398A1 publication Critical patent/EA201791398A1/ru
Publication of EA032431B1 publication Critical patent/EA032431B1/ru

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 System
    • 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

Abstract

Предложены соединения формулы 1их стереоизомеры и фармацевтически приемлемые соли соединений и стереоизомеров, где Rи Rопределены в описании. Данное описание также относится к материалам и методам получения соединений формулы 1, к фармацевтическим композициям, которые содержат их, и к их применению для лечения ожирения и связанных с ним заболеваний, расстройств и патологических состояний, связанных с MetAP2.
EA201791398A 2014-12-19 2015-12-18 Производные фумагиллола EA032431B1 (ru)

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 (2)

Publication Number Publication Date
EA201791398A1 true EA201791398A1 (ru) 2017-10-31
EA032431B1 EA032431B1 (ru) 2019-05-31

Family

ID=55071249

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201791398A EA032431B1 (ru) 2014-12-19 2015-12-18 Производные фумагиллола

Country Status (25)

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

Families Citing this family (1)

* 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

Family Cites Families (26)

* Cited by examiner, † Cited by third party
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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
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US5376645A (en) 1990-01-23 1994-12-27 University Of Kansas Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
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
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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
PL366216A1 (en) 2000-11-01 2005-01-24 Praecis Pharmaceuticals Inc. Therapeutic agents and methods of use thereof for the modulation of angiogenesis
US7087768B2 (en) * 2001-09-27 2006-08-08 Equispharm Co., Ltd. Fumagillol derivatives and preparing method thereof
AU2003230852B2 (en) 2002-04-11 2008-07-10 Children's Medical Center Corporation TNP-470 polymer conjugates and use thereof
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
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
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AU2011239414A1 (en) * 2010-04-15 2012-11-08 The Washington University Prodrug compositions, prodrug nanoparticles, and methods of use thereof
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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
KR20170099973A (ko) 2017-09-01
UY36450A (es) 2016-07-29
US9827255B2 (en) 2017-11-28
SG11201704985VA (en) 2017-07-28
CA2971282A1 (en) 2016-06-23
DOP2017000138A (es) 2017-07-31
CO2017007189A2 (es) 2017-10-20
JP2018500329A (ja) 2018-01-11
CN107207547A (zh) 2017-09-26
TW201636342A (zh) 2016-10-16
ES2702026T3 (es) 2019-02-27
MX2017007926A (es) 2017-09-27
CR20170332A (es) 2017-10-05
EP3233870A1 (en) 2017-10-25
PH12017501134A1 (en) 2017-11-27
CL2017001602A1 (es) 2018-03-09
AR103078A1 (es) 2017-04-12
US10328089B2 (en) 2019-06-25
AU2015364477A1 (en) 2017-07-13
IL252908A0 (en) 2017-08-31
WO2016100778A1 (en) 2016-06-23
ECSP17045054A (es) 2017-10-31
EA032431B1 (ru) 2019-05-31
TN2017000254A1 (en) 2018-10-19
US20180050051A1 (en) 2018-02-22
PE20171141A1 (es) 2017-08-09
BR112017012965A2 (pt) 2018-01-09
US20160175332A1 (en) 2016-06-23
EP3233870B1 (en) 2018-10-31

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Legal Events

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG TJ TM RU