JP6302937B2 - 2−((1r,4r)−4−(4−(5−(ベンゾオキサゾール−2−イルアミノ)ピリジン−2−イル)フェニル)シクロヘキシル)酢酸のメグルミン塩形態、およびdgat1阻害剤としてのそれらの使用 - Google Patents
2−((1r,4r)−4−(4−(5−(ベンゾオキサゾール−2−イルアミノ)ピリジン−2−イル)フェニル)シクロヘキシル)酢酸のメグルミン塩形態、およびdgat1阻害剤としてのそれらの使用 Download PDFInfo
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- JP6302937B2 JP6302937B2 JP2015552797A JP2015552797A JP6302937B2 JP 6302937 B2 JP6302937 B2 JP 6302937B2 JP 2015552797 A JP2015552797 A JP 2015552797A JP 2015552797 A JP2015552797 A JP 2015552797A JP 6302937 B2 JP6302937 B2 JP 6302937B2
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- ylamino
- cyclohexyl
- phenyl
- pyridin
- powder diffraction
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- ZBMZVLHSJCTVON-UHFFFAOYSA-N sotalol Chemical compound CC(C)NCC(O)C1=CC=C(NS(C)(=O)=O)C=C1 ZBMZVLHSJCTVON-UHFFFAOYSA-N 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 239000004059 squalene synthase inhibitor Substances 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 230000007863 steatosis Effects 0.000 description 1
- 231100000240 steatosis hepatitis Toxicity 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 201000011549 stomach cancer Diseases 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
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- 229960005187 telmisartan Drugs 0.000 description 1
- CXGTZJYQWSUFET-IBGZPJMESA-N tesaglitazar Chemical compound C1=CC(C[C@H](OCC)C(O)=O)=CC=C1OCCC1=CC=C(OS(C)(=O)=O)C=C1 CXGTZJYQWSUFET-IBGZPJMESA-N 0.000 description 1
- 229950004704 tesaglitazar Drugs 0.000 description 1
- 201000003120 testicular cancer Diseases 0.000 description 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
- 229960004605 timolol Drugs 0.000 description 1
- 229960005461 torasemide Drugs 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 239000000196 tragacanth Substances 0.000 description 1
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- 229940116362 tragacanth Drugs 0.000 description 1
- 229960002051 trandolapril Drugs 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- 150000004684 trihydrates Chemical class 0.000 description 1
- 229910052722 tritium Inorganic materials 0.000 description 1
- 201000005112 urinary bladder cancer Diseases 0.000 description 1
- 206010046766 uterine cancer Diseases 0.000 description 1
- 229960001722 verapamil Drugs 0.000 description 1
- SYOKIDBDQMKNDQ-XWTIBIIYSA-N vildagliptin Chemical compound C1C(O)(C2)CC(C3)CC1CC32NCC(=O)N1CCC[C@H]1C#N SYOKIDBDQMKNDQ-XWTIBIIYSA-N 0.000 description 1
- 229960001254 vildagliptin Drugs 0.000 description 1
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Classifications
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- 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
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- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non 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
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- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- A61P9/12—Antihypertensives
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
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- Bioinformatics & Cheminformatics (AREA)
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- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Epidemiology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
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- 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)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361751443P | 2013-01-11 | 2013-01-11 | |
| US61/751,443 | 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 (3)
| Publication Number | Publication Date |
|---|---|
| JP2016505017A JP2016505017A (ja) | 2016-02-18 |
| JP2016505017A5 JP2016505017A5 (enExample) | 2016-12-15 |
| JP6302937B2 true JP6302937B2 (ja) | 2018-03-28 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015552797A Expired - Fee Related JP6302937B2 (ja) | 2013-01-11 | 2014-01-10 | 2−((1r,4r)−4−(4−(5−(ベンゾオキサゾール−2−イルアミノ)ピリジン−2−イル)フェニル)シクロヘキシル)酢酸のメグルミン塩形態、およびdgat1阻害剤としてのそれらの使用 |
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| Country | Link |
|---|---|
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| 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)
| 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 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200303742A (en) | 2001-11-21 | 2003-09-16 | Novartis Ag | Organic compounds |
| RU2456273C2 (ru) * | 2006-03-31 | 2012-07-20 | Новартис Аг | Новые соединения |
| WO2013169648A1 (en) * | 2012-05-07 | 2013-11-14 | Novartis Ag | Pharmaceutical combinations comprising a dgat1 inhibtor and a triglyceride lowering drug |
| 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 |
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2014
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- 2014-01-10 BR BR112015016370A patent/BR112015016370A2/pt not_active IP Right Cessation
- 2014-01-10 EP EP14701273.6A patent/EP2943488B1/en not_active Not-in-force
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- 2014-01-10 ES ES14701273.6T patent/ES2675398T3/es active Active
- 2014-01-10 JP JP2015552797A patent/JP6302937B2/ja not_active Expired - Fee Related
- 2014-01-10 TR TR2018/08198T patent/TR201808198T4/tr unknown
- 2014-01-10 KR KR1020157021323A patent/KR20150103747A/ko not_active Ceased
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- 2014-01-10 AU AU2014205276A patent/AU2014205276B2/en not_active Ceased
- 2014-01-10 CA CA2896861A patent/CA2896861A1/en not_active Abandoned
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- 2014-01-10 WO PCT/US2014/011005 patent/WO2014110344A1/en not_active Ceased
- 2014-01-10 CN CN201480003867.0A patent/CN104995188B/zh not_active Expired - Fee Related
- 2014-01-13 AR ARP140100113A patent/AR101523A1/es unknown
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2015
- 2015-02-24 US US14/630,624 patent/US9242971B2/en not_active Expired - Fee Related
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 |
| EP2943488A1 (en) | 2015-11-18 |
| EA201591300A1 (ru) | 2015-11-30 |
| AU2014205276A1 (en) | 2015-07-16 |
| EA027688B1 (ru) | 2017-08-31 |
| ES2675398T3 (es) | 2018-07-11 |
| US8987459B2 (en) | 2015-03-24 |
| JP2016505017A (ja) | 2016-02-18 |
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