[go: up one dir, main page]

RU2010134411A - Фенилацетамидное производное - Google Patents

Фенилацетамидное производное Download PDF

Info

Publication number
RU2010134411A
RU2010134411A RU2010134411/04A RU2010134411A RU2010134411A RU 2010134411 A RU2010134411 A RU 2010134411A RU 2010134411/04 A RU2010134411/04 A RU 2010134411/04A RU 2010134411 A RU2010134411 A RU 2010134411A RU 2010134411 A RU2010134411 A RU 2010134411A
Authority
RU
Russia
Prior art keywords
cyclopropyl
lower alkyl
cyclopropylsulfonyl
phenyl
halogen
Prior art date
Application number
RU2010134411/04A
Other languages
English (en)
Inventor
Масахико ХАЯКАВА (JP)
Масахико Хаякава
Йосиюки КИДО (JP)
Йосиюки КИДО
Такахиро НИГАВАРА (JP)
Такахиро Нигавара
Мицуаки ОКУМУРА (JP)
Мицуаки Окумура
Акира КАНАИ (JP)
Акира КАНАИ
Кейсуке МАКИ (JP)
Кейсуке Маки
Нобуаки АМИНО (JP)
Нобуаки АМИНО
Original Assignee
Астеллас Фарма Инк. (Jp)
Астеллас Фарма Инк.
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 Астеллас Фарма Инк. (Jp), Астеллас Фарма Инк. filed Critical Астеллас Фарма Инк. (Jp)
Publication of RU2010134411A publication Critical patent/RU2010134411A/ru

Links

Classifications

    • 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
    • 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
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79—Acids; Esters
    • C07D213/80—Acids; Esters in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/38—Nitrogen atoms
    • C07D231/40—Acylated on said nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/20—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
    • C07D241/28—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms in which said hetero-bound carbon atoms have double bonds to oxygen, sulfur or nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D261/14—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/34—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D263/48—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/38—Nitrogen atoms
    • C07D277/44—Acylated amino or imino radicals
    • C07D277/46—Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/54—Nitrogen and either oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/08—1,2,4-Thiadiazoles; Hydrogenated 1,2,4-thiadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/12—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
    • C07D285/125—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • C07D285/135—Nitrogen atoms
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
    • C07D413/06—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 only aliphatic carbon atoms
    • 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
    • C07D413/02—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
    • C07D413/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

1. Фенилацетамидное производное, представленное следующей формулой (I), или его фармацевтически приемлемая соль ! ! где символы имеют следующие значения: ! R1 представляет собой низший алкил, галоген-низший алкил или циклоалкил, ! R2 представляет собой циклоалкил, ! R3 представляет собой галоген, низший алкил, галоген-низший алкил, -OR0 или -О-галоген-низший алкил, ! R0, одинаковые или отличные друг от друга, каждый представляет собой -Н или низший алкил, ! кольцо А представляет собой гетероарил, который может быть замещенным, ! кольцо В представляет собой арил или гетероарил, который может быть замещенным, или ! , ! где Х, одинаковые или отличные друг от друга, каждый представляет собой -С(R4)(R5)-, -С(О), -О-, S(O)p- или -N(R0)-, ! m равен целому числу от 2 до 7, ! R4 и R5, одинаковые или отличные друг от друга, каждый представляет собой -Н, галоген, низший алкил, галоген-низший алкил, -OR0 или -О-галоген-низший алкил, ! n и p, одинаковые или отличные друг от друга, каждый равен 0, 1 или 2, ! при условии, что ! означает простую связь или двойную связь. ! 2. Соединение по п.1, где n равен 0. ! 3. Соединение по п.2, где R1 представляет собой метил, трифторметил или циклопропил. ! 4. Соединение по п.3, где R2 представляет собой циклопропил. ! 5. Соединение по п.4, где кольцо В представляет собой ! , ! где m равен 4 или 5, ни один или один из X представляет собой -CH(F)-, -CH(OH)-, -C(O)- или -O-, и остальные X представляют собой -CH2-. ! 6. Соединение по п.5, где кольцо A представляет собой пиразолил, тиазолил, тиадиазолил, пиридил или пиразинил, каждый из которых может быть замещен группой(ами), выбранной из группы, состоящей из галогена, циано, низшего алкила, который может быть замещен группой -OR0, -OR0

Claims (17)

1. Фенилацетамидное производное, представленное следующей формулой (I), или его фармацевтически приемлемая соль
Figure 00000001
где символы имеют следующие значения:
R1 представляет собой низший алкил, галоген-низший алкил или циклоалкил,
R2 представляет собой циклоалкил,
R3 представляет собой галоген, низший алкил, галоген-низший алкил, -OR0 или -О-галоген-низший алкил,
R0, одинаковые или отличные друг от друга, каждый представляет собой -Н или низший алкил,
кольцо А представляет собой гетероарил, который может быть замещенным,
кольцо В представляет собой арил или гетероарил, который может быть замещенным, или
Figure 00000002
,
где Х, одинаковые или отличные друг от друга, каждый представляет собой -С(R4)(R5)-, -С(О), -О-, S(O)p- или -N(R0)-,
m равен целому числу от 2 до 7,
R4 и R5, одинаковые или отличные друг от друга, каждый представляет собой -Н, галоген, низший алкил, галоген-низший алкил, -OR0 или -О-галоген-низший алкил,
n и p, одинаковые или отличные друг от друга, каждый равен 0, 1 или 2,
при условии, что
Figure 00000003
означает простую связь или двойную связь.
2. Соединение по п.1, где n равен 0.
3. Соединение по п.2, где R1 представляет собой метил, трифторметил или циклопропил.
4. Соединение по п.3, где R2 представляет собой циклопропил.
5. Соединение по п.4, где кольцо В представляет собой
Figure 00000002
,
где m равен 4 или 5, ни один или один из X представляет собой -CH(F)-, -CH(OH)-, -C(O)- или -O-, и остальные X представляют собой -CH2-.
6. Соединение по п.5, где кольцо A представляет собой пиразолил, тиазолил, тиадиазолил, пиридил или пиразинил, каждый из которых может быть замещен группой(ами), выбранной из группы, состоящей из галогена, циано, низшего алкила, который может быть замещен группой -OR0, -OR0, -O-низшего алкилена-OR0 и -C(O)R0.
7. Соединение по п.6, где
Figure 00000003
представляет собой простую связь.
8. Соединение по п.6, где
Figure 00000003
представляет собой двойную связь.
9. Соединение по п.1, которое выбрано из группы, включающей:
(2E)-2-[3-циклопропил-4-(циклопропилсульфонил)фенил]-N-(5-метилпиразин-2-ил)-3-[(1S)-3-оксоциклопентил]акриламид,
(2E)-2-[3-циклопропил-4-(циклопропилсульфонил)фенил]-N-(1-метил-1H-пиразол-3-ил)-3-[(1S)-3-оксоциклопентил]акриламид,
(2E)-2-[3-циклопропил-4-(циклопропилсульфонил)фенил]-N-(5-фтор-1,3-тиазол-2-ил)-3-[(1S)-3-оксоциклопентил]акриламид,
(2R)-N-(4-ацетил-1,3-тиазол-2-ил)-2-[3-циклопропил-4-(циклопропилсульфонил)фенил]-3-[(1R)-3-оксоциклопентил]пропанамид,
(2R)-2-[3-циклопропил-4-(циклопропилсульфонил)фенил]-N-(5-метилпиридин-2-ил)-3-[(1R)-3-оксоциклопентил]пропанамид,
(2R)-2-[3-циклопропил-4-(циклопропилсульфонил)фенил]-N-(5-метилпиразин-2-ил)-3-[(1R)-3-оксоциклопентил]пропанамид,
(2R)-2-[3-циклопропил-4-(циклопропилсульфонил)фенил]-N-[5-(гидроксиметил)пиразин-2-ил]-3-[(1R)-3-оксоциклопентил]пропанамид,
(2R)-N-(5-хлорпиразин-2-ил)-2-[3-циклопропил-4-(циклопропилсульфонил)фенил]-3-[(1R)-3-оксоциклопентил]пропанамид,
(2R)-2-[3-циклопропил-4-(циклопропилсульфонил)фенил]-N-(5-метоксипиразин-2-ил)-3-[(1R)-3-оксоциклопентил]пропанамид,
(2R)-2-[3-циклопропил-4-(циклопропилсульфонил)фенил]-3-[(1R)-3-гидроксициклопентил]-N-(5-метилпиразин-2-ил)пропанамид,
(2R)-2-[3-циклопропил-4-(циклопропилсульфонил)фенил]-3-[(1R)-3-гидроксициклопентил]-N-(5-метоксипиразин-2-ил)пропанамид,
(2R)-2-[3-циклопропил-4-(циклопропилсульфонил)фенил]-N-[5-(2-гидроксиэтокси)пиразин-2-ил]-3-[(1R)-3-оксоциклопентил]пропанамид и
(2R)-2-[3-циклопропил-4-(циклопропилсульфонил)фенил]-N-[5-(2-гидрокси-2-метилпропокси)пиразин-2-ил]-3-[(1R)-3-оксоциклопентил]пропанамид,
или его фармацевтически приемлемую соль.
10. Фармацевтическая композиция, содержащая соединение или его фармацевтически приемлемую соль по п.1 и фармацевтически приемлемый носитель.
11. Фармацевтическая композиция по п.10, которая представляет собой активатор GK.
12. Фармацевтическая композиция по п.10, которая представляет собой средство для предупреждения и/или лечения диабета.
13. Фармацевтическая композиция по п.12, которая представляет собой средство для предупреждения и/или лечения диабета типа II.
14. Фармацевтическая композиция по п.10, которая представляет собой средство для предупреждения и/или лечения ожирения.
15. Фармацевтическая композиция по п.10, которая представляет собой средство для предупреждения и/или лечения метаболического синдрома.
16. Применение соединения или его фармацевтически приемлемой соли по п.1 для получения активатора GK или средства для предупреждения и/или лечения диабета, ожирения или метаболического синдрома.
17. Способ предупреждения и/или лечения диабета, ожирения или метаболического синдрома, включающий введение пациенту терапевтически эффективного количества соединения или его соли по п.1.
RU2010134411/04A 2008-01-18 2009-01-16 Фенилацетамидное производное RU2010134411A (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2008-008671 2008-01-18
JP2008008671 2008-01-18

Publications (1)

Publication Number Publication Date
RU2010134411A true RU2010134411A (ru) 2012-02-27

Family

ID=40885396

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2010134411/04A RU2010134411A (ru) 2008-01-18 2009-01-16 Фенилацетамидное производное

Country Status (14)

Country Link
US (2) US8329707B2 (ru)
EP (1) EP2236498A4 (ru)
JP (1) JP5287730B2 (ru)
KR (1) KR20100113518A (ru)
CN (1) CN101918363B (ru)
AU (1) AU2009205070A1 (ru)
BR (1) BRPI0906888A2 (ru)
CA (1) CA2712948A1 (ru)
IL (1) IL207016A0 (ru)
MX (1) MX2010007853A (ru)
RU (1) RU2010134411A (ru)
TW (1) TW200942239A (ru)
WO (1) WO2009091014A1 (ru)
ZA (1) ZA201004989B (ru)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5287730B2 (ja) * 2008-01-18 2013-09-11 アステラス製薬株式会社 フェニルアセトアミド誘導体
ME02198B (me) 2008-04-28 2016-02-20 Kyorin Seiyaku Kk Derivati ciklopentilakrilamida
JP2012515760A (ja) 2009-01-20 2012-07-12 ファイザー・インク 置換ピラジノンアミド
CN102146078A (zh) * 2010-02-09 2011-08-10 中国科学院上海药物研究所 一类取代的丙酰胺类化合物、其制备方法及用途
WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
US8530413B2 (en) 2010-06-21 2013-09-10 Sanofi Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments
TW201221505A (en) 2010-07-05 2012-06-01 Sanofi Sa Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament
TW201215388A (en) 2010-07-05 2012-04-16 Sanofi Sa (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments
TW201215387A (en) 2010-07-05 2012-04-16 Sanofi Aventis Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament
US20120149718A1 (en) * 2010-12-14 2012-06-14 Brotherton-Pleiss Christine E Amido Compounds
WO2013037390A1 (en) 2011-09-12 2013-03-21 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
WO2013045413A1 (en) 2011-09-27 2013-04-04 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
BR112015015229B1 (pt) * 2012-12-25 2020-07-07 Hua Medicine processo para a preparação de um composto da fórmula, e, composto
EP2878339A1 (en) 2013-12-02 2015-06-03 Siena Biotech S.p.A. SIP3 antagonists
CN112062754B (zh) * 2020-09-24 2022-06-21 深圳市华先医药科技有限公司 一种合成Dorzagliatin的中间体的制备方法

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6320050B1 (en) 1999-03-29 2001-11-20 Hoffmann-La Roche Inc. Heteroaromatic glucokinase activators
DE60014610T2 (de) 1999-03-29 2006-03-09 F. Hoffmann-La Roche Ag Glukokinase aktivatoren
US6353111B1 (en) 1999-12-15 2002-03-05 Hoffmann-La Roche Inc. Trans olefinic glucokinase activators
DE60108108T2 (de) 2000-05-03 2005-12-08 F. Hoffmann-La Roche Ag Heteroaromatische alkynylphenyl-verbindungen als glukokinase-aktivatoren
DE60106599T2 (de) 2000-05-08 2006-02-09 F. Hoffmann-La Roche Ag Substituierte phenylacetamide und ihre verwendung als glukokinase aktivatoren
ES2307623T3 (es) 2000-05-08 2008-12-01 F. Hoffmann-La Roche Ag Activadores de fenilamida glucokinasa para-amina sustituida.
KR100556323B1 (ko) 2000-07-20 2006-03-03 에프. 호프만-라 로슈 아게 알파-아실 및 알파-헤테로원자-치환된 벤젠 아세트아미드글루코키나제 활성화제
US6369232B1 (en) 2000-08-15 2002-04-09 Hoffmann-La Roche Inc. Tetrazolyl-phenyl acetamide glucokinase activators
KR100545431B1 (ko) 2000-12-06 2006-01-24 에프. 호프만-라 로슈 아게 축합된 이종방향족 글루코키나제 활성화제
RS93604A (en) 2002-04-26 2007-02-05 F. Hoffmann-La Roche Ag., Substituted phenylacetamides and their use as glucokinase activators
NZ539013A (en) 2002-10-03 2007-05-31 Novartis Ag Substituted (thiazol-2-yl) -amide or sulfonamide as glycokinase activators useful in the treatment of type 2 diabetes
MY141521A (en) 2002-12-12 2010-05-14 Hoffmann La Roche 5-substituted-six-membered heteroaromatic glucokinase activators
EP1585739B1 (en) 2003-01-06 2011-04-20 Eli Lilly And Company Substituted arylcyclopropylacetamides as glucokinase activators
AU2003294376A1 (en) 2003-01-06 2004-08-10 Eli Lilly And Company Heteroaryl compounds
PL378117A1 (pl) 2003-02-11 2006-03-06 Prosidion Limited Tricyklopodstawione związki amidowe
JP4621198B2 (ja) 2003-02-11 2011-01-26 プロシディオン・リミテッド トリ（シクロ）置換アミドグルコキナーゼ活性化化合物
MXPA06011365A (es) 2004-04-02 2006-12-15 Novartis Ag Derivados de tiazolo-piridina, composiciones farmaceuticas que los contienen, y metodos para el tratamiento de condiciones mediadas por glucoquinasa.
RU2412192C2 (ru) 2004-04-02 2011-02-20 Новартис Аг Сульфонамидтиазолпиридиновые производные как активаторы глюкокиназы, пригодные для лечения диабета типа 2
CA2563192A1 (en) 2004-04-21 2005-11-03 Prosidion Limited Tri(cyclo) substituted amide compounds
CA2576407A1 (en) 2004-08-12 2006-02-16 Prosidion Limited Substituted phenylacetamides and their use as glucokinase activators
AU2005311269B2 (en) 2004-12-03 2011-11-10 Transtech Pharma, Inc. Heteroaromatic glucokinase activators
JP4033409B1 (ja) 2005-07-11 2008-01-16 田辺三菱製薬株式会社 オキシム誘導体及びその製法
KR20080040046A (ko) 2005-08-31 2008-05-07 아스텔라스세이야쿠 가부시키가이샤 티아졸 유도체
GT200600428A (es) 2005-09-30 2007-05-21 Compuestos organicos
GT200600429A (es) 2005-09-30 2007-04-30 Compuestos organicos
AU2006310474A1 (en) 2005-11-03 2007-05-10 Prosidion Ltd Tricyclo substituted amides
US20080293741A1 (en) 2005-11-03 2008-11-27 Matthew Colin Thor Fyfe Tricyclo Substituted Amides as Glucokinase Modulators
BRPI0618067A2 (pt) 2005-11-03 2011-08-16 Prosidion Ltd composto ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, e, uso e processo para a preparação de um composto ou um sal farmaceuticamente aceitável do mesmo
US7888504B2 (en) 2006-07-06 2011-02-15 Bristol-Myers Squibb Company Glucokinase activators and methods of using same
US7910747B2 (en) 2006-07-06 2011-03-22 Bristol-Myers Squibb Company Phosphonate and phosphinate pyrazolylamide glucokinase activators
WO2008012227A2 (en) * 2006-07-24 2008-01-31 F. Hoffmann-La Roche Ag Pyrazoles as glucokinase activators
TW200831081A (en) 2006-12-25 2008-08-01 Kyorin Seiyaku Kk Glucokinase activator
CA2679971C (en) 2007-03-07 2015-02-17 Teijin Pharma Limited Glucokinase activator
JP5287730B2 (ja) * 2008-01-18 2013-09-11 アステラス製薬株式会社 フェニルアセトアミド誘導体

Also Published As

Publication number Publication date
EP2236498A1 (en) 2010-10-06
JP5287730B2 (ja) 2013-09-11
CA2712948A1 (en) 2009-07-23
EP2236498A4 (en) 2012-02-22
MX2010007853A (es) 2010-10-06
CN101918363A (zh) 2010-12-15
CN101918363B (zh) 2012-09-05
US8329707B2 (en) 2012-12-11
TW200942239A (en) 2009-10-16
KR20100113518A (ko) 2010-10-21
US20130102617A1 (en) 2013-04-25
BRPI0906888A2 (pt) 2015-11-03
WO2009091014A1 (ja) 2009-07-23
US20100286171A1 (en) 2010-11-11
JPWO2009091014A1 (ja) 2011-05-26
IL207016A0 (en) 2010-12-30
AU2009205070A1 (en) 2009-07-23
ZA201004989B (en) 2011-09-28

Similar Documents

Publication Publication Date Title
RU2010134411A (ru) Фенилацетамидное производное
RU2420525C2 (ru) Производные оксимов и их получение
RU2317294C2 (ru) (имидазол-1-илметил)пиридазин в качестве блокатора nmda рецептора
RU2486181C2 (ru) Пиримидилциклопентаны как ингибиторы акт-протеинкиназ
RU2436780C2 (ru) Производные 5-фенилтиазола и их применение в качестве ингибиторов рi3 киназы
RU2401658C2 (ru) Гетероциклические ингибиторы аспартилпротеазы
RU2458920C2 (ru) Новые соединения
RU2403247C2 (ru) Модуляторы никотиновых ацетилхолиновых рецепторов альфа 7 и их терапевтические применения
RU2312106C2 (ru) Замещенные 4-алкоксиоксазолпроизводные в качестве агонистов ppar
RU2020110780A (ru) Ингибитор fgfr и его медицинское применение
RU2017116197A (ru) 2-амино-3,5-дифтор-3,6-диметил-6-фенил-3,4,5,6-тетрагидропиридины как ингибиторы васе1 для лечения болезни альцгеймера
RU2017116196A (ru) 2-амино-6-(дифторметил)-5,5-дифтор-6-фенил-3,4,5,6-тетрагидропиридины как ингибиторы васе1
RU2016150535A (ru) Новые соединения
JP2018517746A5 (ru)
RU2004121161A (ru) Замещенные 2-тио-3,5-дициано-4-фенил-6-аминопиридины и их применение
JP2009530281A5 (ru)
JP2007523155A5 (ru)
JP2020507589A5 (ru)
RU2016133626A (ru) 2-амино-3,5,5-трифтор-3,4,5,6-тетрагидропиридины в качестве ингибиторов bace1 для лечения болезни альцгеймера
RU2011117927A (ru) Карбаматное соединение или его соль
JP2014508128A5 (ru)
JP2010514832A5 (ru)
JP2016040288A5 (ru)
RU2009136592A (ru) Терапевтические агенты
RU2018136888A (ru) Нафтиридины в качестве антагонистов интегрина