EA201391724A1 - Новые соединения в качестве ингибиторов диацилглицерин ацилтрансферазы - Google Patents

Новые соединения в качестве ингибиторов диацилглицерин ацилтрансферазы

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Publication number
EA201391724A1
EA201391724A1 EA201391724A EA201391724A EA201391724A1 EA 201391724 A1 EA201391724 A1 EA 201391724A1 EA 201391724 A EA201391724 A EA 201391724A EA 201391724 A EA201391724 A EA 201391724A EA 201391724 A1 EA201391724 A1 EA 201391724A1
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EA
Eurasian Patent Office
Prior art keywords
inhibitors
dgat
obesity
new connections
diseases associated
Prior art date
Application number
EA201391724A
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English (en)
Other versions
EA023239B1 (ru
Inventor
Дунхой Цинь
Хемант Джоши
Рагхурам Тангирала
Зигфрид Бенджамин Кристенсен, IV
Original Assignee
Глэксосмитклайн Интеллекчуал Проперти (No.2) Лимитед
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Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=47217644&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA201391724(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Глэксосмитклайн Интеллекчуал Проперти (No.2) Лимитед filed Critical Глэксосмитклайн Интеллекчуал Проперти (No.2) Лимитед
Publication of EA201391724A1 publication Critical patent/EA201391724A1/ru
Publication of EA023239B1 publication Critical patent/EA023239B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C275/42—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/12—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring
    • C07D217/18—Aralkyl radicals
    • C07D217/20—Aralkyl radicals with oxygen atoms directly attached to the aromatic ring of said aralkyl radical, e.g. papaverine
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • C07D217/04—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • C07D217/24—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • C07D217/26—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
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-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
    • C07D237/20—Nitrogen atoms
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
    • C07C2602/08—One of the condensed rings being a six-membered aromatic ring the other ring being five-membered, e.g. indane
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
    • C07C2602/10—One of the condensed rings being a six-membered aromatic ring the other ring being six-membered, e.g. tetraline

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Данное изобретение относится к новым соединениям, которые являются ингибиторами ацильного кофермента А: диацилглицеринацилтрансфераза 1 (ДГАТ-1), к фармацевтическим композициям, содержащим их, к способам для их получения и к их применению в терапии для профилактики или лечения заболеваний, связанных с дисфункцией ДГАТ-1 или при которых модулирование активности ДГАТ-1 может оказать терапевтическую пользу, включая, но не ограничиваясь ими, ожирение, связанные с ожирением заболевания, гипертриглицеридемию, гиперлипопротеинемию, хиломикронемию, дислипидемию, неалкогольный стеатогепатит, диабет, резистентность к инсулину, метаболический синдром, инфекцию вирусом гепатита С и акне или другие кожные расстройства.
EA201391724A 2011-05-20 2012-05-18 Соединения в качестве ингибиторов диацилглицерин ацилтрансферазы EA023239B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IN1451DE2011 2011-05-20
US201161495049P 2011-06-09 2011-06-09
PCT/US2012/038520 WO2012162127A1 (en) 2011-05-20 2012-05-18 Novel compounds as diacylglycerol acyltransferase inhibitors

Publications (2)

Publication Number Publication Date
EA201391724A1 true EA201391724A1 (ru) 2014-04-30
EA023239B1 EA023239B1 (ru) 2016-05-31

Family

ID=47217644

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201391724A EA023239B1 (ru) 2011-05-20 2012-05-18 Соединения в качестве ингибиторов диацилглицерин ацилтрансферазы

Country Status (19)

Country Link
US (1) US9242929B2 (ru)
EP (1) EP2723332B1 (ru)
JP (1) JP5893724B2 (ru)
KR (1) KR20140033426A (ru)
CN (1) CN103687595B (ru)
AU (1) AU2012259042B2 (ru)
CA (1) CA2836666A1 (ru)
CO (1) CO6811853A2 (ru)
CR (1) CR20130603A (ru)
DO (1) DOP2013000273A (ru)
EA (1) EA023239B1 (ru)
ES (1) ES2572261T3 (ru)
IL (1) IL229487A0 (ru)
MA (1) MA35398B1 (ru)
MX (1) MX2013013565A (ru)
PE (1) PE20140618A1 (ru)
SG (1) SG194976A1 (ru)
WO (1) WO2012162127A1 (ru)
ZA (1) ZA201308569B (ru)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2890901A1 (en) * 2012-11-09 2014-05-15 Glaxosmithkline Llc Novel compounds as diacylglycerol acyltransferase inhibitors
WO2014081995A1 (en) * 2012-11-23 2014-05-30 Glaxosmithkline Llc Novel compounds as diacylglycerol acyltransferase inhibitors
WO2022026380A1 (en) * 2020-07-29 2022-02-03 Board Of Regents, The University Of Texas System Urea inhibitors of micro-rna
CN111747876B (zh) * 2020-08-03 2023-05-26 万华化学集团股份有限公司 一种氧化角黄素制备虾青素的方法

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006045209A (ja) * 2004-07-02 2006-02-16 Sankyo Co Ltd ウレア誘導体
US20070249620A1 (en) * 2004-07-02 2007-10-25 Hitoshi Kurata Urea Derivative
BRPI0610850A2 (pt) * 2005-04-19 2008-12-02 Bayer Pharmaceuticals Corp derivados de Ácido aril alquila, composiÇço farmacÊutica, medicamento, bem como uso dos referidos derivados
ES2430115T3 (es) 2006-03-31 2013-11-19 Novartis Ag Inhibidor de DGAT
GB0625654D0 (en) * 2006-12-21 2007-01-31 Smithkline Beecham Corp Compounds
EP2120911A1 (en) * 2007-02-15 2009-11-25 Prosidion Limited Amide and urea derivatives for the treatment of metabolic diseases
JP2008255024A (ja) * 2007-04-02 2008-10-23 Banyu Pharmaceut Co Ltd ビアリールアミン誘導体
US8394823B2 (en) * 2008-04-11 2013-03-12 Bristol-Myers Squibb Company Triazolopyridine compounds useful as DGAT1 inhibitors
EP2471777A4 (en) 2009-08-28 2013-01-02 Daiichi Sankyo Co Ltd NOVEL TETRAHYDROISOQUINOLINE COMPOUNDS
JP2011088889A (ja) * 2009-09-24 2011-05-06 Daiichi Sankyo Co Ltd 新規テトラヒドロイソキノリン誘導体を含有する医薬
JP2013516402A (ja) * 2009-12-31 2013-05-13 ピラマル エンタープライジーズ リミテッド ジアシルグリセロールアシルトランスフェラーゼの抑制剤
US8314120B2 (en) 2010-03-30 2012-11-20 Abbott Gmbh & Co. Kg Small molecule potentiators of metabotropic glutamate receptors

Also Published As

Publication number Publication date
EP2723332A1 (en) 2014-04-30
CR20130603A (es) 2014-09-09
PE20140618A1 (es) 2014-06-05
JP5893724B2 (ja) 2016-03-23
CA2836666A1 (en) 2012-11-29
CN103687595A (zh) 2014-03-26
ZA201308569B (en) 2014-07-30
KR20140033426A (ko) 2014-03-18
SG194976A1 (en) 2013-12-30
AU2012259042A1 (en) 2013-04-18
MX2013013565A (es) 2014-01-08
DOP2013000273A (es) 2014-04-15
ES2572261T3 (es) 2016-05-31
US9242929B2 (en) 2016-01-26
MA35398B1 (fr) 2014-09-01
US20150307445A1 (en) 2015-10-29
AU2012259042B2 (en) 2015-06-11
WO2012162127A1 (en) 2012-11-29
EA023239B1 (ru) 2016-05-31
JP2014525895A (ja) 2014-10-02
CN103687595B (zh) 2017-05-24
CO6811853A2 (es) 2013-12-16
IL229487A0 (en) 2014-01-30
EP2723332A4 (en) 2014-10-15
EP2723332B1 (en) 2016-03-02

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