EA201791398A1 - Производные фумагиллола - Google Patents
Производные фумагиллолаInfo
- 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
Links
- 150000001875 compounds Chemical class 0.000 abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 208000008589 Obesity Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 239000000463 material Substances 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 230000001575 pathological effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
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)
- Bioinformatics & Cheminformatics (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Engineering & Computer Science (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Zoology (AREA)
- Gastroenterology & Hepatology (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Epoxy Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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.
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)
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)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
PH26256A (en) | 1988-08-12 | 1992-04-01 | Fujisawa Pharmaceutical Co | Oxaspiro [2,5] octane derivative |
DE68927904T2 (de) | 1988-09-01 | 1997-09-04 | Takeda Chemical Industries Ltd | Fumagillol-Derivate |
KR0166088B1 (ko) | 1990-01-23 | 1999-01-15 | . | 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도 |
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 |
GB9711643D0 (en) | 1997-06-05 | 1997-07-30 | Janssen Pharmaceutica Nv | Glass thermoplastic systems |
US6207704B1 (en) | 1997-06-09 | 2001-03-27 | Massachusetts Institute Of Technology | Type 2 methionine aminopeptidase [MetAP2] inhibitors and uses thereof |
CA2307792C (en) | 1997-10-31 | 2007-06-26 | Children's Medical Center Corporation | Method for regulating size and growth of vascularized normal tissue |
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 |
AU2002239479B2 (en) | 2000-11-01 | 2006-11-09 | Praecis Pharmaceuticals Incorporated | Peptides as Met-AP2 inhibitors |
US7087768B2 (en) * | 2001-09-27 | 2006-08-08 | Equispharm Co., Ltd. | Fumagillol derivatives and preparing method thereof |
US7332523B2 (en) | 2002-04-11 | 2008-02-19 | 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 |
WO2006080591A1 (en) * | 2005-01-26 | 2006-08-03 | 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 |
MX2010005857A (es) | 2007-11-28 | 2010-11-22 | Mersana Therapeutics Inc | Conjugados de analogos de fumagillina biodegradables biocompatibles. |
US8299067B2 (en) | 2008-03-27 | 2012-10-30 | Versitech Limited | 5-demethoxyfumagillol and derivatives thereof |
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 |
JP2013527157A (ja) * | 2010-04-15 | 2013-06-27 | ワシントン・ユニバーシティ | プロドラッグ組成物、プロドラッグナノ粒子およびその使用方法 |
US20130210821A1 (en) | 2010-05-27 | 2013-08-15 | James E. Vath | Methods for Treating Obesity |
KR101875988B1 (ko) * | 2011-03-08 | 2018-07-06 | 자프겐 인크. | 옥사스피로[2.5]옥탄 유도체 및 유사체 |
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 |
-
2015
- 2015-12-14 TW TW104141948A patent/TW201636342A/zh unknown
- 2015-12-17 AR ARP150104152A patent/AR103078A1/es unknown
- 2015-12-17 UY UY0001036450A patent/UY36450A/es not_active Application Discontinuation
- 2015-12-18 CA CA2971282A patent/CA2971282A1/en not_active Abandoned
- 2015-12-18 SG SG11201704985VA patent/SG11201704985VA/en unknown
- 2015-12-18 KR KR1020177020240A patent/KR20170099973A/ko unknown
- 2015-12-18 WO PCT/US2015/066594 patent/WO2016100778A1/en active Application Filing
- 2015-12-18 EA EA201791398A patent/EA032431B1/ru not_active IP Right Cessation
- 2015-12-18 PE PE2017001074A patent/PE20171141A1/es not_active Application Discontinuation
- 2015-12-18 CR CR20170332A patent/CR20170332A/es unknown
- 2015-12-18 EP EP15820800.9A patent/EP3233870B1/en active Active
- 2015-12-18 AU AU2015364477A patent/AU2015364477A1/en not_active Abandoned
- 2015-12-18 JP JP2017532117A patent/JP2018500329A/ja active Pending
- 2015-12-18 CN CN201580074539.4A patent/CN107207547A/zh active Pending
- 2015-12-18 US US14/974,033 patent/US9827255B2/en not_active Expired - Fee Related
- 2015-12-18 ES ES15820800T patent/ES2702026T3/es active Active
- 2015-12-18 TN TN2017000254A patent/TN2017000254A1/en unknown
- 2015-12-18 BR BR112017012965A patent/BR112017012965A2/pt not_active Application Discontinuation
- 2015-12-18 MX MX2017007926A patent/MX2017007926A/es unknown
-
2017
- 2017-06-13 DO DO2017000138A patent/DOP2017000138A/es unknown
- 2017-06-14 IL IL252908A patent/IL252908A0/en unknown
- 2017-06-16 PH PH12017501134A patent/PH12017501134A1/en unknown
- 2017-06-19 CL CL2017001602A patent/CL2017001602A1/es unknown
- 2017-07-12 EC ECIEPI201745054A patent/ECSP17045054A/es unknown
- 2017-07-18 CO CONC2017/0007189A patent/CO2017007189A2/es unknown
- 2017-10-27 US US15/796,519 patent/US10328089B2/en not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
EA032431B1 (ru) | 2019-05-31 |
PH12017501134A1 (en) | 2017-11-27 |
ES2702026T3 (es) | 2019-02-27 |
AU2015364477A1 (en) | 2017-07-13 |
CA2971282A1 (en) | 2016-06-23 |
US10328089B2 (en) | 2019-06-25 |
ECSP17045054A (es) | 2017-10-31 |
TN2017000254A1 (en) | 2018-10-19 |
CR20170332A (es) | 2017-10-05 |
AR103078A1 (es) | 2017-04-12 |
TW201636342A (zh) | 2016-10-16 |
UY36450A (es) | 2016-07-29 |
CN107207547A (zh) | 2017-09-26 |
SG11201704985VA (en) | 2017-07-28 |
JP2018500329A (ja) | 2018-01-11 |
EP3233870A1 (en) | 2017-10-25 |
WO2016100778A1 (en) | 2016-06-23 |
CL2017001602A1 (es) | 2018-03-09 |
US9827255B2 (en) | 2017-11-28 |
MX2017007926A (es) | 2017-09-27 |
DOP2017000138A (es) | 2017-07-31 |
IL252908A0 (en) | 2017-08-31 |
US20180050051A1 (en) | 2018-02-22 |
US20160175332A1 (en) | 2016-06-23 |
EP3233870B1 (en) | 2018-10-31 |
KR20170099973A (ko) | 2017-09-01 |
BR112017012965A2 (pt) | 2018-01-09 |
CO2017007189A2 (es) | 2017-10-20 |
PE20171141A1 (es) | 2017-08-09 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
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 |