AR103078A1 - Derivados de fumagilol - Google Patents

Derivados de fumagilol

Info

Publication number
AR103078A1
AR103078A1 ARP150104152A ARP150104152A AR103078A1 AR 103078 A1 AR103078 A1 AR 103078A1 AR P150104152 A ARP150104152 A AR P150104152A AR P150104152 A ARP150104152 A AR P150104152A AR 103078 A1 AR103078 A1 AR 103078A1
Authority
AR
Argentina
Prior art keywords
independently selected
substituted
heteroaryl
halo
alkyl
Prior art date
Application number
ARP150104152A
Other languages
English (en)
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 AR103078A1 publication Critical patent/AR103078A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558Heterocyclic 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
    • C07F9/65586Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/155Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/192Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/216Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/336Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/397Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/64Sulfonylureas, e.g. glibenclamide, tolbutamide, chlorpropamide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/662Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/665Phosphorus compounds having oxygen as a ring hetero atom, e.g. fosfomycin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/683Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22Hormones
    • A61K38/28Insulins
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs 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)
  • Engineering & Computer Science (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Zoology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Hematology (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

Reivindicación 1: Un compuesto de fórmula (1), un estereoisómero de este o una sal farmacéuticamente aceptable del compuesto o estereoisómero, donde: R¹ y R² se seleccionan cada uno independientemente de fenilo, heteroarilo C₃₋₅, -OR⁴, y -N(R⁴)R⁵, donde cada fenilo y heteroarilo C₃₋₅ está independientemente sustituido con entre 0 y 3 Rᵃ, y cada heteroarilo C₃₋₅ tiene átomos de 5 ó 6 anillos de los cuales 1 ó 2 son heteroátomos que se seleccionan independientemente de N, O, y S; cada Rᵃ se selecciona independientemente de halo, -CN, R³, y R⁴; cada R³ se selecciona independientemente de -OR⁴, -N(R⁴)R⁵, -NR⁴C(O)R⁶, -NR⁴C(O)OR⁵, -C(O)OR⁴, -C(O)N(R⁴)R⁵, -C(O)N(R⁴)OR⁵, -C(O)N(R⁴)S(O)₂R⁶, -N(R⁴)S(O)₂R⁶, -SR⁴, -S(O)R⁶, -S(O)₂R⁶, y -S(O)₂N(R⁴)R⁵; cada R⁴ y R⁵ se selecciona independientemente de (a) alquilo C₁₋₆, alquenilo C₂₋₆, y alquinilo C₂₋₆ cada uno sustituido con entre 0 y 3 Rᵇ, y (b) cicloalquilo C₃₋₈-(CH₂)ₘ-, heterociclilo C₂₋₆-(CH₂)ₘ-, arilo C₆₋₁₄-(CH₂)ₘ-, y heteroarilo C₁₋₉-(CH₂)ₘ-, cada uno sustituido con entre 0 y 3 Rᶜ; cada R⁶ se selecciona independientemente de (a) alquilo C₁₋₆, que está sustituido con entre 0 y 3 Rᵇ, y (b) cicloalquilo C₃₋₈-(CH₂)ₘ-, heterociclilo C₂₋₆-(CH₂)ₘ-, arilo C₆₋₁₄-(CH₂)ₘ-, y heteroarilo C₁₋₉-(CH₂)ₘ-, cada uno sustituido con entre 0 y 3 Rᵈ; cada Rᵇ se selecciona independientemente de halo, -CN, y R⁷; cada Rᶜ se selecciona independientemente de (a) halo, -CN, y R⁷, y (b) alquilo C₁₋₆, alquenilo C₂₋₆, y alquinilo C₂₋₆, cada uno sustituido con entre 0 y 3 Rᵇ; cada Rᵈ se selecciona independientemente de (a) halo, -CN, y R⁷, y (b) alquilo C₁₋₆, que está sustituido con entre 0 y 3 Rᵇ; cada R⁷ se selecciona independientemente de -OR⁸, -N(R⁸)R⁹, -NR⁸C(O)R⁹, -NR⁸C(O)OR⁹, -C(O)OR⁸, -C(O)N(R⁸)R⁹, -C(O)N(R⁸)OR⁹, -C(O)N(R⁸)S(O)₂R⁹, -N(R⁸)S(O)₂R⁹, -SR⁸, -S(O)R⁸, -S(O)₂R⁸, y -S(O)₂N(R⁸)R⁹; cada R⁸ y R⁹ se selecciona independientemente de alquilo C₁₋₆, cicloalquilo C₃₋₈-(CH₂)ₘ-, y heterociclilo C₂₋₆-(CH₂)ₘ-, cada uno sustituido con entre 0 y 3 sustituyentes que se seleccionan independientemente de halo y -CN; y cada m se selecciona independientemente de 0, 1, 2, 3, y 4; donde cada resto heteroarilo que se enumera en R⁴, R⁵, y R⁶ tiene independientemente de 1 a 4 heteroátomos que se seleccionan independientemente de N, O y S, y cada resto heterociclilo que se enumera en R⁴, R⁵, R⁶, y R⁸ tiene independientemente de 1 a 4 heteroátomos que se seleccionan independientemente de N, O, y S.
ARP150104152A 2014-12-19 2015-12-17 Derivados de fumagilol AR103078A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201462094823P 2014-12-19 2014-12-19

Publications (1)

Publication Number Publication Date
AR103078A1 true AR103078A1 (es) 2017-04-12

Family

ID=55071249

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP150104152A AR103078A1 (es) 2014-12-19 2015-12-17 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
KR20210005100A (ko) * 2018-04-20 2021-01-13 더 유니버시티 오브 버몬트 앤드 스테이트 애그리컬쳐 칼리지 선택된 환자에서 심혈관 질환을 치료하기 위한 조성물 및 방법

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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
CO2017007189A2 (es) 2017-10-20
DOP2017000138A (es) 2017-07-31
KR20170099973A (ko) 2017-09-01
EA201791398A1 (ru) 2017-10-31
US9827255B2 (en) 2017-11-28
EP3233870A1 (en) 2017-10-25
ES2702026T3 (es) 2019-02-27
CN107207547A (zh) 2017-09-26
US10328089B2 (en) 2019-06-25
JP2018500329A (ja) 2018-01-11
EP3233870B1 (en) 2018-10-31
CR20170332A (es) 2017-10-05
PE20171141A1 (es) 2017-08-09
WO2016100778A1 (en) 2016-06-23
MX2017007926A (es) 2017-09-27
TW201636342A (zh) 2016-10-16
IL252908A0 (en) 2017-08-31
PH12017501134A1 (en) 2017-11-27
UY36450A (es) 2016-07-29
AU2015364477A1 (en) 2017-07-13
US20180050051A1 (en) 2018-02-22
ECSP17045054A (es) 2017-10-31
TN2017000254A1 (en) 2018-10-19
SG11201704985VA (en) 2017-07-28
CA2971282A1 (en) 2016-06-23
BR112017012965A2 (pt) 2018-01-09
US20160175332A1 (en) 2016-06-23
EA032431B1 (ru) 2019-05-31
CL2017001602A1 (es) 2018-03-09

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