DK2850084T3 - Pyrazolforbindelser som SGLT1-inhibitorer - Google Patents

Pyrazolforbindelser som SGLT1-inhibitorer Download PDF

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Publication number
DK2850084T3
DK2850084T3 DK13722231.1T DK13722231T DK2850084T3 DK 2850084 T3 DK2850084 T3 DK 2850084T3 DK 13722231 T DK13722231 T DK 13722231T DK 2850084 T3 DK2850084 T3 DK 2850084T3
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DK
Denmark
Prior art keywords
mmol
methyl
pyrazol
propan
beta
Prior art date
Application number
DK13722231.1T
Other languages
English (en)
Inventor
Fucheng Qu
Nathan Bryan Mantlo
Original Assignee
Lilly Co Eli
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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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=DK2850084(T3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Lilly Co Eli filed Critical Lilly Co Eli
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Publication of DK2850084T3 publication Critical patent/DK2850084T3/da

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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)
  • Biochemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Biotechnology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Genetics & Genomics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Claims (9)

1. Forbindelse med formlen:
hvor X betegner følgende:
eller et farmaceutisk acceptabelt salt deraf.
2. Forbindelse eller salt ifølge krav 1, som er:
3. Forbindelse ifølge krav 2, som er:
4. Forbindelse eller farmaceutisk acceptabelt salt deraf ifølge et af kravene 1-3 til anvendelse ved behandling.
5. Forbindelse eller farmaceutisk acceptabelt salt deraf ifølge et af kravene 1-3 til anvendelse ved behandling af diabetes.
6. Forbindelse eller farmaceutisk acceptabelt salt deraf til anvendelse ifølge krav 5 ved behandling af type 1 diabetes.
7. Forbindelse eller farmaceutisk acceptabelt salt deraf til anvendelse ifølge krav 5 ved behandling af type 2 diabetes.
8. Farmaceutisk sammensætning omfattende en forbindelse eller et farmaceutisk acceptabelt salt deraf ifølge et af kravene 1-3 i kombination med en eller flere farmaceutisk acceptable bærere, fortyndingsmidler eller hjælpestoffer.
9. Farmaceutisk sammensætning ifølge krav 8, yderligere omfattende et eller flere terapeutiske midler.
DK13722231.1T 2012-05-10 2013-05-02 Pyrazolforbindelser som SGLT1-inhibitorer DK2850084T3 (da)

Applications Claiming Priority (3)

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

Publications (1)

Publication Number Publication Date
DK2850084T3 true DK2850084T3 (da) 2016-09-12

Family

ID=48428684

Family Applications (1)

Application Number Title Priority Date Filing Date
DK13722231.1T DK2850084T3 (da) 2012-05-10 2013-05-02 Pyrazolforbindelser som SGLT1-inhibitorer

Country Status (43)

Country Link
US (2) US8697849B2 (da)
EP (1) EP2850084B1 (da)
JP (1) JP6148725B2 (da)
KR (1) KR101685779B1 (da)
AP (1) AP3593A (da)
AR (1) AR090806A1 (da)
AU (1) AU2013259946B2 (da)
BR (1) BR112014026198B1 (da)
CA (1) CA2869323C (da)
CL (1) CL2014002845A1 (da)
CO (1) CO7141429A2 (da)
CR (1) CR20140473A (da)
CY (1) CY1117912T1 (da)
DK (1) DK2850084T3 (da)
DO (1) DOP2014000250A (da)
EA (1) EA024207B1 (da)
EC (1) ECSP14026088A (da)
ES (1) ES2588835T3 (da)
GT (1) GT201400242A (da)
HK (1) HK1202542A1 (da)
HR (1) HRP20160804T1 (da)
HU (1) HUE030414T2 (da)
IL (1) IL235427A (da)
IN (1) IN2014DN07996A (da)
JO (1) JO3136B1 (da)
LT (1) LT2850084T (da)
MA (1) MA37501B1 (da)
ME (1) ME02405B (da)
MX (1) MX357058B (da)
MY (1) MY177326A (da)
NZ (1) NZ700356A (da)
PE (1) PE20142399A1 (da)
PH (1) PH12014502492B1 (da)
PL (1) PL2850084T3 (da)
PT (1) PT2850084T (da)
RS (1) RS55107B1 (da)
SG (1) SG11201407345QA (da)
SI (1) SI2850084T1 (da)
TN (1) TN2014000410A1 (da)
TW (1) TWI579295B (da)
UA (1) UA113086C2 (da)
WO (1) WO2013169546A1 (da)
ZA (1) ZA201407531B (da)

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
AR097890A1 (es) 2013-10-17 2016-04-20 Lilly Co Eli Compuestos de urea
AR098134A1 (es) 2013-11-01 2016-05-04 Lilly Co Eli Compuestos de urea
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
CA3089092A1 (en) * 2018-04-04 2019-10-10 Japan Tobacco Inc. Pyrazole compounds substituted with heteroaryl and pharmaceutical use thereof
MX2022002683A (es) * 2019-09-04 2022-04-07 Japan Tobacco Inc Metodo terapeutico o profilactico para diabetes usando medicamentos combinados.

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100591585B1 (ko) 1999-08-31 2006-06-20 깃세이 야쿠힌 고교 가부시키가이샤 글루코피라노실옥시피라졸 유도체, 그것을 함유하는 의약조성물 및 그 제조 중간체
CA2438593C (en) 2001-02-26 2010-09-21 Kissei Pharmaceutical Co., Ltd. Glucopyranosyloxypyrazole derivatives and medicinal use thereof
CA2448741C (en) 2001-05-30 2010-06-22 Kissei Pharmaceutical Co., Ltd. Glucopyranosyloxypyrazole derivative, medicinal composition containing the same, medicinal use thereof, and intermediate therefor
PL213095B1 (pl) 2002-08-08 2013-01-31 Kissei Pharmaceutical Pochodna pirazolu, kompozycja farmaceutyczna, srodek do leczenia lub hamowania choroby i zastosowanie pochodnej pirazolu
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
US7973012B2 (en) * 2006-05-19 2011-07-05 Taisho Pharmaceutical Co., Ltd C-phenyl glycitol compound
WO2009084531A1 (ja) 2007-12-27 2009-07-09 Kissei Pharmaceutical Co., Ltd. ピラゾール誘導体のモノセバシン酸塩
CA2752212C (en) 2009-02-23 2016-08-16 Taisho Pharmaceutical Co., Ltd. 4-isopropylphenyl glucitol compounds as sglt1 inhibitors
MX2012003400A (es) 2009-10-02 2012-04-10 Sanofi Sa Uso de compuestos con actividad inhibidora de sglt - 1/sglt - 2 para producir medicamentos para el tratamiento de enfermedades oseas.
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
ES2588835T3 (es) 2016-11-07
EP2850084B1 (en) 2016-06-15
HUE030414T2 (en) 2017-05-29
SI2850084T1 (sl) 2016-07-29
AR090806A1 (es) 2014-12-10
LT2850084T (lt) 2016-09-12
ZA201407531B (en) 2016-05-25
WO2013169546A1 (en) 2013-11-14
SG11201407345QA (en) 2014-12-30
MA37501B1 (fr) 2016-11-30
HK1202542A1 (zh) 2015-10-02
EA024207B1 (ru) 2016-08-31
PH12014502492A1 (en) 2015-01-12
KR20150001798A (ko) 2015-01-06
JP6148725B2 (ja) 2017-06-14
PT2850084T (pt) 2016-08-02
EP2850084A1 (en) 2015-03-25
ME02405B (me) 2016-09-20
PH12014502492B1 (en) 2015-01-12
MA37501A1 (fr) 2016-03-31
DOP2014000250A (es) 2014-11-30
TWI579295B (zh) 2017-04-21
RS55107B1 (sr) 2016-12-30
CR20140473A (es) 2014-11-21
IL235427A (en) 2016-06-30
IN2014DN07996A (da) 2015-05-01
EA201491852A1 (ru) 2015-02-27
CO7141429A2 (es) 2014-12-12
CA2869323A1 (en) 2013-11-14
MY177326A (en) 2020-09-11
MX2014013615A (es) 2015-02-12
CN104284894A (zh) 2015-01-14
NZ700356A (en) 2016-06-24
PE20142399A1 (es) 2015-01-22
CN104284894B (zh) 2016-02-17
JO3136B1 (ar) 2017-09-20
US8697849B2 (en) 2014-04-15
MX357058B (es) 2018-06-25
CL2014002845A1 (es) 2015-01-30
UA113086C2 (xx) 2016-12-12
BR112014026198A2 (pt) 2017-06-27
AP3593A (en) 2016-02-15
ECSP14026088A (es) 2015-09-30
TN2014000410A1 (en) 2015-12-21
AP2014008044A0 (en) 2014-11-30
US20140162967A1 (en) 2014-06-12
CY1117912T1 (el) 2017-05-17
US20130303471A1 (en) 2013-11-14
US9296775B2 (en) 2016-03-29
AU2013259946B2 (en) 2015-09-10
TW201406773A (zh) 2014-02-16
KR101685779B1 (ko) 2016-12-12
CA2869323C (en) 2016-03-29
GT201400242A (es) 2015-08-27
AU2013259946A1 (en) 2014-10-16
HRP20160804T1 (hr) 2016-08-12
JP2015516419A (ja) 2015-06-11
BR112014026198B1 (pt) 2021-02-02
PL2850084T3 (pl) 2017-05-31

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