WO2014133414A3 - Heterocyclic tgr5 bile acid receptor agonists, pharmaceutical composition, methods for the production and use thereof - Google Patents

Heterocyclic tgr5 bile acid receptor agonists, pharmaceutical composition, methods for the production and use thereof Download PDF

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Publication number
WO2014133414A3
WO2014133414A3 PCT/RU2014/000108 RU2014000108W WO2014133414A3 WO 2014133414 A3 WO2014133414 A3 WO 2014133414A3 RU 2014000108 W RU2014000108 W RU 2014000108W WO 2014133414 A3 WO2014133414 A3 WO 2014133414A3
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WO
WIPO (PCT)
Prior art keywords
group
substituted
alkyl
hydrogen
acyl
Prior art date
Application number
PCT/RU2014/000108
Other languages
French (fr)
Russian (ru)
Other versions
WO2014133414A2 (en
Inventor
Андрей Александрович ИВАЩЕНКО
Николай Филиппович САВЧУК
Сергей Евгеньевич ТКАЧЕНКО
Александр Викторович ХВАТ
Original Assignee
Алла Хем Ллс
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.)
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Application filed by Алла Хем Ллс filed Critical Алла Хем Ллс
Publication of WO2014133414A2 publication Critical patent/WO2014133414A2/en
Publication of WO2014133414A3 publication Critical patent/WO2014133414A3/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02—Seven-membered rings
    • C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/12—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • 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
    • 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
    • C07D413/12—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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

1. Compounds of general formula I, or racemic mixtures thereof, or individual optical isomers thereof, or pharmaceutically acceptable salts and/or hydrates thereof, wherein: X is the amino group R'R''N, optionally substituted or unsubstituted with identical substituents R' and R'', or a substituted oxy group; the R'R''N group is a non-aromatic azaheterocycle, preferably azetidine, pyrrolidine, piperidine, morpholine, thiomorpholine, piperazine, homopiperidine or homopiperazine; the amino group substituents R' and R'' are hydrogen, alkyl, substituted alkyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, alkenyl, cycloalkenyl, alkynyl, acyl, aroyl, heteroaroyl, alkylsulphonyl, arylsulphonyl, heteroarylsulphonyl, alkoxycarbonyl, aryloxycarbonyl, araloxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl, heteroarylaminocarbonyl, heterocyclylaminocarbonyl, alkylaminothiocarbonyl, arylaminothiocarbonyl, heteroarylaminothiocarbonyl, heterocyclylaminothiocarbonyl, optionally substituted aminosulphonyl, the R'R''N group may be a non-aromatic azaheterocycle, preferably azetidine, pyrrolidine, piperidine, morpholine, thiomorpholine, piperazine, homopiperidine or homopiperazine; and the substituted oxy group is a hydroxy group in which hydrogen is substituted with alkyl, alkenyl, cycloalkyl, cycloalkenyl, aryl, hetaryl and heterocyclyl, or acyl, or an aminocarbonyl group or an oxycarboyl group; R1a and R1b are hydrogen and alkyl, or R1a and R1b together form a -(CH2)n- polymethylene chain, wherein n=2-5; R1c and R1d are hydrogen and alkyl, or R1c and R1d together form a -(CH2)n- polymethylene chain, wherein n=2-5; R2 is an acyl group, a thioacyl group, a substituted oxycarbonyl group, a substituted amidine group, a substituted aminocarbonyl group, a substituted aminothiocarbonyl group or a sulphonyl group; R3 is hydrogen, C1-C6 alkyl, an alkoxy group, halogen, CF3, CN.
PCT/RU2014/000108 2013-02-26 2014-02-19 Heterocyclic tgr5 bile acid receptor agonists, pharmaceutical composition, methods for the production and use thereof WO2014133414A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
RU2013108339 2013-02-26
RU2013108339/04A RU2543485C2 (en) 2013-02-26 2013-02-26 Heterocyclic tgr5 bile acid receptor agonists, pharmaceutical composition, methods for preparing and using them

Publications (2)

Publication Number Publication Date
WO2014133414A2 WO2014133414A2 (en) 2014-09-04
WO2014133414A3 true WO2014133414A3 (en) 2014-12-18

Family

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PCT/RU2014/000108 WO2014133414A2 (en) 2013-02-26 2014-02-19 Heterocyclic tgr5 bile acid receptor agonists, pharmaceutical composition, methods for the production and use thereof

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RU (1) RU2543485C2 (en)
WO (1) WO2014133414A2 (en)

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* Cited by examiner, † Cited by third party
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RU2594154C2 (en) * 2014-11-10 2016-08-10 федеральное государственное автономное образовательное учреждение высшего образования "Московский физико-технический институт (государственный университет)" CRYSTALLINE FORM OF METHYL ESTER 3-(N-P-TOLYLACETAMIDO) METHYL)-2,3,4,5-TETRAHYDROBENZO[f][1,4]OXAZEPINE-4-CARBOXAMIDE)THIOPHENE-2-CARBOXYLIC ACID, ACTIVE COMPONENT, PHARMACEUTICAL COMPOSITION AND DRUG
EP3350166A4 (en) 2015-09-16 2019-05-01 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
EP3350164A4 (en) * 2015-09-16 2019-03-27 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
DK3350165T3 (en) 2015-09-16 2023-09-25 Organovo Inc Farnesoid X receptor agonists and uses thereof
WO2017049172A1 (en) 2015-09-16 2017-03-23 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
EP3464270B1 (en) 2016-05-24 2022-02-23 Genentech, Inc. Heterocyclic inhibitors of cbp/ep300 and their use in the treatment of cancer
SG11201908330PA (en) 2017-03-15 2019-10-30 Metacrine Inc Farnesoid x receptor agonists and uses thereof
EP3596053B1 (en) 2017-03-15 2023-08-16 Organovo, Inc. Farnesoid x receptor agonists and uses thereof
DK3681885T3 (en) 2017-09-15 2024-04-15 Forma Therapeutics Inc TETRAHYDRO-IMIDAZO-QUINOLINE COMPOUNDS AS CBP/P300 INHIBITORS
CN116178369A (en) 2018-06-29 2023-05-30 福马疗法公司 Inhibition of CREB Binding Protein (CBP)
MX2021003110A (en) 2018-09-18 2021-05-13 Metacrine Inc Farnesoid x receptor agonists and uses thereof.
US11795168B2 (en) 2020-09-23 2023-10-24 Forma Therapeutics, Inc. Inhibiting cyclic amp-responsive element-binding protein (CREB) binding protein (CBP)
US11801243B2 (en) 2020-09-23 2023-10-31 Forma Therapeutics, Inc. Bromodomain inhibitors for androgen receptor-driven cancers

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WO2009080725A1 (en) * 2007-12-21 2009-07-02 Glaxo Group Limited Oxadiazole derivatives active on sphingosine-1-phosphate (sip)
RU2007149337A (en) * 2005-06-01 2009-07-10 Такеда Фармасьютикал Компани Лимитед (Jp) A NEW METHOD FOR TREATING HYPERLIPIDEMIA
WO2010118208A1 (en) * 2009-04-09 2010-10-14 Exelixis, Inc. Benzoxazepin-4- (5h) -yl derivatives and their use to treat cancer

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RU2303597C1 (en) * 2006-05-12 2007-07-27 Иващенко Андрей Александрович Pharmaceutical composition, method for its preparing and using
CN101808646A (en) * 2007-11-30 2010-08-18 阿斯比奥制药株式会社 Agent for improving motor complications or psychiatric symptoms in parkinson's disease

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RU2007149337A (en) * 2005-06-01 2009-07-10 Такеда Фармасьютикал Компани Лимитед (Jp) A NEW METHOD FOR TREATING HYPERLIPIDEMIA
WO2009080725A1 (en) * 2007-12-21 2009-07-02 Glaxo Group Limited Oxadiazole derivatives active on sphingosine-1-phosphate (sip)
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WO2014133414A2 (en) 2014-09-04
RU2013108339A (en) 2014-09-10
RU2543485C2 (en) 2015-03-10

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