CA2869323C - Pyrazole compounds as sglt1 inhibitors - Google Patents

Pyrazole compounds as sglt1 inhibitors Download PDF

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Publication number
CA2869323C
CA2869323C CA2869323A CA2869323A CA2869323C CA 2869323 C CA2869323 C CA 2869323C CA 2869323 A CA2869323 A CA 2869323A CA 2869323 A CA2869323 A CA 2869323A CA 2869323 C CA2869323 C CA 2869323C
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Canada
Prior art keywords
mmol
compound
pyrazol
propan
beta
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Active
Application number
CA2869323A
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English (en)
French (fr)
Other versions
CA2869323A1 (en
Inventor
Fucheng Qu
Nathan Bryan Mantlo
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Eli Lilly and Co
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Eli Lilly and Co
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=48428684&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CA2869323(C) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Eli Lilly and Co filed Critical Eli Lilly and Co
Publication of CA2869323A1 publication Critical patent/CA2869323A1/en
Application granted granted Critical
Publication of CA2869323C publication Critical patent/CA2869323C/en
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/02Heterocyclic radicals containing only nitrogen as ring hetero atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms 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
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00Processes for the preparation of sugar derivatives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/20Carbocyclic rings
    • C07H15/22Cyclohexane rings, substituted by nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H7/00Compounds containing non-saccharide radicals linked to saccharide radicals by a carbon-to-carbon bond
    • C07H7/06Heterocyclic radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biotechnology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Genetics & Genomics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CA2869323A 2012-05-10 2013-05-02 Pyrazole compounds as sglt1 inhibitors Active CA2869323C (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261645101P 2012-05-10 2012-05-10
US61/645,101 2012-05-10
US201361769221P 2013-02-26 2013-02-26
US61/769,221 2013-02-26
PCT/US2013/039164 WO2013169546A1 (en) 2012-05-10 2013-05-02 Pyrazole compounds as sglt1 inhibitors

Publications (2)

Publication Number Publication Date
CA2869323A1 CA2869323A1 (en) 2013-11-14
CA2869323C true CA2869323C (en) 2016-03-29

Family

ID=48428684

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2869323A Active CA2869323C (en) 2012-05-10 2013-05-02 Pyrazole compounds as sglt1 inhibitors

Country Status (42)

Country Link
US (2) US8697849B2 (forum.php)
EP (1) EP2850084B1 (forum.php)
JP (1) JP6148725B2 (forum.php)
KR (1) KR101685779B1 (forum.php)
AP (1) AP3593A (forum.php)
AR (1) AR090806A1 (forum.php)
AU (1) AU2013259946B2 (forum.php)
BR (1) BR112014026198B1 (forum.php)
CA (1) CA2869323C (forum.php)
CL (1) CL2014002845A1 (forum.php)
CO (1) CO7141429A2 (forum.php)
CR (1) CR20140473A (forum.php)
CY (1) CY1117912T1 (forum.php)
DK (1) DK2850084T3 (forum.php)
DO (1) DOP2014000250A (forum.php)
EA (1) EA024207B1 (forum.php)
EC (1) ECSP14026088A (forum.php)
ES (1) ES2588835T3 (forum.php)
GT (1) GT201400242A (forum.php)
HR (1) HRP20160804T1 (forum.php)
HU (1) HUE030414T2 (forum.php)
IL (1) IL235427A (forum.php)
IN (1) IN2014DN07996A (forum.php)
JO (1) JO3136B1 (forum.php)
LT (1) LT2850084T (forum.php)
MA (1) MA37501B1 (forum.php)
ME (1) ME02405B (forum.php)
MX (1) MX357058B (forum.php)
MY (1) MY177326A (forum.php)
NZ (1) NZ700356A (forum.php)
PE (1) PE20142399A1 (forum.php)
PH (1) PH12014502492B1 (forum.php)
PL (1) PL2850084T3 (forum.php)
PT (1) PT2850084T (forum.php)
RS (1) RS55107B1 (forum.php)
SG (1) SG11201407345QA (forum.php)
SI (1) SI2850084T1 (forum.php)
TN (1) TN2014000410A1 (forum.php)
TW (1) TWI579295B (forum.php)
UA (1) UA113086C2 (forum.php)
WO (1) WO2013169546A1 (forum.php)
ZA (1) ZA201407531B (forum.php)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA113086C2 (xx) * 2012-05-10 2016-12-12 Піразольні сполуки як інгібітори sglt1
TW201425326A (zh) 2012-10-05 2014-07-01 Lilly Co Eli 新穎脲化合物
TWI633113B (zh) 2013-10-17 2018-08-21 美國禮來大藥廠 新穎脲化合物
JO3298B1 (ar) 2013-11-01 2018-09-16 Lilly Co Eli مشتقات جليكوبيرانوسيل-مستبدل و اندول-يوريا و استعمالاتهم كمثبطات sglt
AR098670A1 (es) 2013-11-08 2016-06-08 Lilly Co Eli Inhibidor de sglt1
CN110054657B (zh) 2018-01-18 2021-06-29 亚宝药业集团股份有限公司 吡喃葡萄糖取代的吡唑化合物及其制备方法
TWI805727B (zh) * 2018-04-04 2023-06-21 日商日本煙草產業股份有限公司 經雜芳基取代之吡唑化合物及其醫藥用途
EP4342466A1 (en) * 2019-09-04 2024-03-27 Japan Tobacco Inc. Therapeutic or prophylactic method for diabetes using combination medicine

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60009929T2 (de) 1999-08-31 2005-03-31 Kissei Pharmaceutical Co., Ltd., Matsumoto Glucopyranosyloxypyrazol-derivate, diese enthaltende arzneimittel und zwischenprodukte zu deren herstellung
JP4141258B2 (ja) 2001-02-26 2008-08-27 キッセイ薬品工業株式会社 グルコピラノシルオキシピラゾール誘導体及びその医薬用途
EP1400529A4 (en) 2001-05-30 2007-12-19 Kissei Pharmaceutical GLUCOPYRANOSYLOXYPYRAZOLE DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, AND MEDICINAL AND INTERMEDIARY USE THEREOF
NZ538117A (en) * 2002-08-08 2007-01-26 Kissei Pharmaceutical Pyrazole derivative, medicinal composition containing the same, medicinal use thereof, and intermediate for production thereof
JP2004137245A (ja) 2002-08-23 2004-05-13 Kissei Pharmaceut Co Ltd ピラゾール誘導体、それを含有する医薬組成物、その医薬用途及びその製造中間体
DE102004028241B4 (de) * 2004-06-11 2007-09-13 Sanofi-Aventis Deutschland Gmbh Neue Fluorglykosidderivate von Pyrazolen, diese Verbindungen enthaltende Arzneimittel und Herstellung dieser Arzneimittel
MX2008014512A (es) * 2006-05-19 2008-11-27 Taisho Pharma Co Ltd Compuesto de c-fenil glucitol para el tratamiento de diabetes.
AU2008344436B2 (en) 2007-12-27 2013-08-29 Kissei Pharmaceutical Co., Ltd. Monosebacate of pyrazole derivative
CN102414191B (zh) 2009-02-23 2014-04-16 大正制药株式会社 4-异丙苯基山梨醇化合物作为sglt1抑制剂
BR112012007349A2 (pt) * 2009-10-02 2019-09-24 Sanofi Sa uso de composto com atividade inibidora de sglt-1/sglt-2 para produção de medicamentos para tratamento de doenças ósseas.
US8163704B2 (en) 2009-10-20 2012-04-24 Novartis Ag Glycoside derivatives and uses thereof
UA113086C2 (xx) * 2012-05-10 2016-12-12 Піразольні сполуки як інгібітори sglt1

Also Published As

Publication number Publication date
TN2014000410A1 (en) 2015-12-21
ECSP14026088A (es) 2015-09-30
US20130303471A1 (en) 2013-11-14
CN104284894A (zh) 2015-01-14
ZA201407531B (en) 2016-05-25
US20140162967A1 (en) 2014-06-12
AU2013259946A1 (en) 2014-10-16
CO7141429A2 (es) 2014-12-12
BR112014026198B1 (pt) 2021-02-02
HK1202542A1 (zh) 2015-10-02
JP2015516419A (ja) 2015-06-11
AR090806A1 (es) 2014-12-10
CR20140473A (es) 2014-11-21
JO3136B1 (ar) 2017-09-20
EP2850084B1 (en) 2016-06-15
CL2014002845A1 (es) 2015-01-30
MA37501A1 (fr) 2016-03-31
IL235427A (en) 2016-06-30
MX357058B (es) 2018-06-25
CY1117912T1 (el) 2017-05-17
ME02405B (me) 2016-09-20
RS55107B1 (sr) 2016-12-30
PL2850084T3 (pl) 2017-05-31
BR112014026198A2 (pt) 2017-06-27
PE20142399A1 (es) 2015-01-22
DOP2014000250A (es) 2014-11-30
GT201400242A (es) 2015-08-27
PH12014502492A1 (en) 2015-01-12
PH12014502492B1 (en) 2015-01-12
TWI579295B (zh) 2017-04-21
CN104284894B (zh) 2016-02-17
CA2869323A1 (en) 2013-11-14
HUE030414T2 (en) 2017-05-29
MY177326A (en) 2020-09-11
KR101685779B1 (ko) 2016-12-12
UA113086C2 (xx) 2016-12-12
WO2013169546A1 (en) 2013-11-14
HRP20160804T1 (hr) 2016-08-12
AP2014008044A0 (en) 2014-11-30
MX2014013615A (es) 2015-02-12
LT2850084T (lt) 2016-09-12
AP3593A (en) 2016-02-15
TW201406773A (zh) 2014-02-16
DK2850084T3 (en) 2016-09-12
SG11201407345QA (en) 2014-12-30
MA37501B1 (fr) 2016-11-30
KR20150001798A (ko) 2015-01-06
NZ700356A (en) 2016-06-24
US8697849B2 (en) 2014-04-15
EP2850084A1 (en) 2015-03-25
JP6148725B2 (ja) 2017-06-14
PT2850084T (pt) 2016-08-02
AU2013259946B2 (en) 2015-09-10
ES2588835T3 (es) 2016-11-07
EA201491852A1 (ru) 2015-02-27
IN2014DN07996A (forum.php) 2015-05-01
US9296775B2 (en) 2016-03-29
SI2850084T1 (sl) 2016-07-29
EA024207B1 (ru) 2016-08-31

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