EA027688B1 - Меглуминовая соль 2-((1r,4r)-4-(4-(5-(бензоксазол-2-иламино)пиридин-2-ил)фенил)циклогексил)уксусной кислоты и ее кристаллическая форма и их применение в качестве ингибиторов dgat1 - Google Patents

Меглуминовая соль 2-((1r,4r)-4-(4-(5-(бензоксазол-2-иламино)пиридин-2-ил)фенил)циклогексил)уксусной кислоты и ее кристаллическая форма и их применение в качестве ингибиторов dgat1 Download PDF

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Publication number
EA027688B1
EA027688B1 EA201591300A EA201591300A EA027688B1 EA 027688 B1 EA027688 B1 EA 027688B1 EA 201591300 A EA201591300 A EA 201591300A EA 201591300 A EA201591300 A EA 201591300A EA 027688 B1 EA027688 B1 EA 027688B1
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Eurasian Patent Office
Prior art keywords
crystalline form
cyclohexyl
pyridin
phenyl
diffraction pattern
Prior art date
Application number
EA201591300A
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English (en)
Russian (ru)
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EA201591300A1 (ru
Inventor
Кристина Капаччи-Даниель
Мэрилин Делакрус
Баоцин Гун
Акаш Джейн
Яньсун Лу
Лицзюнь Чжан
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Новартис Аг
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Publication date
Application filed by Новартис Аг filed Critical Новартис Аг
Publication of EA201591300A1 publication Critical patent/EA201591300A1/ru
Publication of EA027688B1 publication Critical patent/EA027688B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
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    • 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
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • 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
    • 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
    • A61P35/00Antineoplastic agents
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/02Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
EA201591300A 2013-01-11 2014-01-10 Меглуминовая соль 2-((1r,4r)-4-(4-(5-(бензоксазол-2-иламино)пиридин-2-ил)фенил)циклогексил)уксусной кислоты и ее кристаллическая форма и их применение в качестве ингибиторов dgat1 EA027688B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361751443P 2013-01-11 2013-01-11
PCT/US2014/011005 WO2014110344A1 (en) 2013-01-11 2014-01-10 Meglumine salt forms of 2-((1 r,4r)-4-(4-(5-(benzoxazol-2-ylamino)pyridin-2-yl)phenyl)cyclohexyl) acetic acid and their use as dgat1 inhibitors

Publications (2)

Publication Number Publication Date
EA201591300A1 EA201591300A1 (ru) 2015-11-30
EA027688B1 true EA027688B1 (ru) 2017-08-31

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EA201591300A EA027688B1 (ru) 2013-01-11 2014-01-10 Меглуминовая соль 2-((1r,4r)-4-(4-(5-(бензоксазол-2-иламино)пиридин-2-ил)фенил)циклогексил)уксусной кислоты и ее кристаллическая форма и их применение в качестве ингибиторов dgat1

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US (2) US8987459B2 (enExample)
EP (1) EP2943488B1 (enExample)
JP (1) JP6302937B2 (enExample)
KR (1) KR20150103747A (enExample)
CN (1) CN104995188B (enExample)
AR (1) AR101523A1 (enExample)
AU (1) AU2014205276B2 (enExample)
BR (1) BR112015016370A2 (enExample)
CA (1) CA2896861A1 (enExample)
EA (1) EA027688B1 (enExample)
ES (1) ES2675398T3 (enExample)
MX (1) MX2015008978A (enExample)
PL (1) PL2943488T3 (enExample)
PT (1) PT2943488T (enExample)
TR (1) TR201808198T4 (enExample)
WO (1) WO2014110344A1 (enExample)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL2943488T3 (pl) * 2013-01-11 2018-09-28 Novartis Ag Postacie soli megluminowej kwasu 2-((1r,4r)-4-(4-(5-(benzoksazol-2-iloamino)pirydyn-2-ylo)fenylo)cykloheksylo)octowego i ich zastosowania jako inhibitory dgat1
KR101684053B1 (ko) * 2015-01-20 2016-12-08 씨제이헬스케어 주식회사 벤즈이미다졸 유도체의 신규 결정형 및 이의 제조방법
AU2019255233A1 (en) * 2018-04-17 2020-11-26 Cardurion Pharmaceuticals, Llc Meglumine salts of thienopyrimidines
WO2022099431A1 (en) * 2020-11-10 2022-05-19 Unity Biotechnology, Inc. Crystalline solid meglumine salt inhibitor of bcl and methods of making and using same

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007126957A2 (en) * 2006-03-31 2007-11-08 Novartis Ag New compounds
WO2013169648A1 (en) * 2012-05-07 2013-11-14 Novartis Ag Pharmaceutical combinations comprising a dgat1 inhibtor and a triglyceride lowering drug

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200303742A (en) 2001-11-21 2003-09-16 Novartis Ag Organic compounds
PL2943488T3 (pl) * 2013-01-11 2018-09-28 Novartis Ag Postacie soli megluminowej kwasu 2-((1r,4r)-4-(4-(5-(benzoksazol-2-iloamino)pirydyn-2-ylo)fenylo)cykloheksylo)octowego i ich zastosowania jako inhibitory dgat1

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007126957A2 (en) * 2006-03-31 2007-11-08 Novartis Ag New compounds
WO2013169648A1 (en) * 2012-05-07 2013-11-14 Novartis Ag Pharmaceutical combinations comprising a dgat1 inhibtor and a triglyceride lowering drug

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
STEFFEN DENZINGER: "A counter ion that fulfils all needs", WORLD PHARMACEUTICAL FRONTIERS, VOL. 2, 2011, GLOBAL TRADE MEDIA, LONDON, UK, London, UK, pages 90, XP055102822, Retrieved from the Internet <URL:http://pages.cdn.pagesuite.com/c/1/c1487298-3c31-4c6e-a19f-b426a152fe0b/page.pdf> [retrieved on 20140218] *

Also Published As

Publication number Publication date
US9242971B2 (en) 2016-01-26
BR112015016370A2 (pt) 2017-07-11
CN104995188B (zh) 2018-09-14
US20140200246A1 (en) 2014-07-17
CA2896861A1 (en) 2014-07-17
KR20150103747A (ko) 2015-09-11
AU2014205276B2 (en) 2016-10-20
TR201808198T4 (tr) 2018-07-23
WO2014110344A1 (en) 2014-07-17
CN104995188A (zh) 2015-10-21
PT2943488T (pt) 2018-06-12
PL2943488T3 (pl) 2018-09-28
MX2015008978A (es) 2015-09-29
AR101523A1 (es) 2016-12-28
EP2943488B1 (en) 2018-03-28
US20150166522A1 (en) 2015-06-18
JP6302937B2 (ja) 2018-03-28
EP2943488A1 (en) 2015-11-18
EA201591300A1 (ru) 2015-11-30
AU2014205276A1 (en) 2015-07-16
ES2675398T3 (es) 2018-07-11
US8987459B2 (en) 2015-03-24
JP2016505017A (ja) 2016-02-18

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG TJ TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): RU