CN104812748B - 二氢吡唑gpr40调节剂 - Google Patents
二氢吡唑gpr40调节剂 Download PDFInfo
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- CN104812748B CN104812748B CN201380059799.5A CN201380059799A CN104812748B CN 104812748 B CN104812748 B CN 104812748B CN 201380059799 A CN201380059799 A CN 201380059799A CN 104812748 B CN104812748 B CN 104812748B
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- agent
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- 0 *C(N=CC1Cl)=CC1N(CC1)CCC1Oc(cc1)ccc1N(C(CC(O)=O)C1C2*C2)N=C1C(F)(F)F Chemical compound *C(N=CC1Cl)=CC1N(CC1)CCC1Oc(cc1)ccc1N(C(CC(O)=O)C1C2*C2)N=C1C(F)(F)F 0.000 description 15
- WZQOVZJEWJVWIZ-UHFFFAOYSA-N CC(C)(C(C)(C)O1)OB1S1OC(C)(C)C(C)(C)O1 Chemical compound CC(C)(C(C)(C)O1)OB1S1OC(C)(C)C(C)(C)O1 WZQOVZJEWJVWIZ-UHFFFAOYSA-N 0.000 description 1
- FUAQRGIQWOTIER-UHFFFAOYSA-N CCOc(cc1)cc(N(CC2)CC(C)C2Oc(cc2)ccc2N(C(CC(O)=O)C2C)N=C2C(F)(F)F)c1F Chemical compound CCOc(cc1)cc(N(CC2)CC(C)C2Oc(cc2)ccc2N(C(CC(O)=O)C2C)N=C2C(F)(F)F)c1F FUAQRGIQWOTIER-UHFFFAOYSA-N 0.000 description 1
- IETUAHZHKPCSLO-QKKBWIMNSA-N C[C@@H]([C@@H]1CC(O)=O)C(C(F)(F)F)=NN1c(cc1)ccc1OC(CC1)CCN1c(ccc(Cl)c1)c1F Chemical compound C[C@@H]([C@@H]1CC(O)=O)C(C(F)(F)F)=NN1c(cc1)ccc1OC(CC1)CCN1c(ccc(Cl)c1)c1F IETUAHZHKPCSLO-QKKBWIMNSA-N 0.000 description 1
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- 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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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A61P27/02—Ophthalmic agents
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
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- A—HUMAN NECESSITIES
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- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
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- A—HUMAN NECESSITIES
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- 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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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
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- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
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- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs 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
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- C—CHEMISTRY; METALLURGY
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- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
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- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- 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
- C07D417/14—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 three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
- C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
- C07D451/06—Oxygen atoms
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- C07D471/00—Heterocyclic 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
- C07D471/02—Heterocyclic 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
- C07D471/08—Bridged systems
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic 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
- C07D487/08—Bridged systems
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Child & Adolescent Psychology (AREA)
- Ophthalmology & Optometry (AREA)
- Vascular Medicine (AREA)
- Endocrinology (AREA)
- Psychiatry (AREA)
- Dermatology (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Optical Integrated Circuits (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261727262P | 2012-11-16 | 2012-11-16 | |
| US61/727,262 | 2012-11-16 | ||
| US201361777294P | 2013-03-12 | 2013-03-12 | |
| US61/777,294 | 2013-03-12 | ||
| PCT/US2013/070215 WO2014078610A1 (en) | 2012-11-16 | 2013-11-15 | Dihydropyrazole gpr40 modulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN104812748A CN104812748A (zh) | 2015-07-29 |
| CN104812748B true CN104812748B (zh) | 2017-10-24 |
Family
ID=49876965
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201380059799.5A Expired - Fee Related CN104812748B (zh) | 2012-11-16 | 2013-11-15 | 二氢吡唑gpr40调节剂 |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US9133163B2 (enExample) |
| EP (1) | EP2920165B1 (enExample) |
| JP (1) | JP6322203B2 (enExample) |
| KR (1) | KR102204804B1 (enExample) |
| CN (1) | CN104812748B (enExample) |
| AU (1) | AU2013344604B2 (enExample) |
| BR (1) | BR112015010779A2 (enExample) |
| CA (1) | CA2891574A1 (enExample) |
| CY (1) | CY1118365T1 (enExample) |
| DK (1) | DK2920165T3 (enExample) |
| EA (1) | EA026913B1 (enExample) |
| ES (1) | ES2606685T3 (enExample) |
| HR (1) | HRP20161631T1 (enExample) |
| HU (1) | HUE032401T2 (enExample) |
| IL (1) | IL238741A0 (enExample) |
| LT (1) | LT2920165T (enExample) |
| MX (1) | MX358499B (enExample) |
| PL (1) | PL2920165T3 (enExample) |
| PT (1) | PT2920165T (enExample) |
| RS (1) | RS55363B1 (enExample) |
| SG (1) | SG11201503558SA (enExample) |
| SI (1) | SI2920165T1 (enExample) |
| SM (1) | SMT201600410B (enExample) |
| TW (1) | TW201427971A (enExample) |
| UY (1) | UY35143A (enExample) |
| WO (1) | WO2014078610A1 (enExample) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6322204B2 (ja) * | 2012-11-16 | 2018-05-09 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | ジヒドロピラゾールのgpr40モジュレーター |
| EA201690888A1 (ru) | 2013-11-14 | 2016-10-31 | Кадила Хелзкэр Лимитед | Новые гетероциклические соединения |
| HRP20180641T1 (hr) | 2014-05-07 | 2018-06-01 | Bristol-Myers Squibb Company | Pirolidinski gpr40 modulatori za liječenje bolesti kao što je dijabetes |
| BR112016025188A2 (pt) * | 2014-05-07 | 2017-08-15 | Bristol Myers Squibb Co | moduladores de pirrolidina gpr40 para o tratamento de doenças tal como diabetes |
| EP3177282B1 (en) | 2014-08-08 | 2021-10-06 | Merck Sharp & Dohme Corp. | Antidiabetic bicyclic compounds |
| US10968193B2 (en) | 2014-08-08 | 2021-04-06 | Merck Sharp & Dohme Corp. | Antidiabetic bicyclic compounds |
| WO2016019587A1 (en) | 2014-08-08 | 2016-02-11 | Merck Sharp & Dohme Corp. | [7, 6]-fused bicyclic antidiabetic compounds |
| US10100042B2 (en) | 2014-08-08 | 2018-10-16 | Merck Sharp & Dohme Corp. | [5,6]—fused bicyclic antidiabetic compounds |
| EP3604267A4 (en) | 2017-03-31 | 2020-12-16 | Takeda Pharmaceutical Company Limited | Aromatic compound |
| KR102708681B1 (ko) | 2018-02-13 | 2024-09-26 | 길리애드 사이언시즈, 인코포레이티드 | Pd-1/pd-l1 억제제 |
| EP3781556B1 (en) | 2018-04-19 | 2025-06-18 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| CN118221646A (zh) | 2018-07-13 | 2024-06-21 | 吉利德科学公司 | Pd-1/pd-l1抑制剂 |
| KR102635333B1 (ko) | 2018-10-24 | 2024-02-15 | 길리애드 사이언시즈, 인코포레이티드 | Pd-1/pd-l1 억제제 |
| CN115490638A (zh) * | 2022-09-22 | 2022-12-20 | 哈尔滨理工大学 | 5-官能团化吡唑啉及其制备方法 |
| CN115671105B (zh) * | 2022-11-22 | 2023-10-27 | 北京箭牧科技有限公司 | Ly2922470在制备预防或治疗肾脏疾病药物中的应用 |
| CN119431272B (zh) * | 2024-11-13 | 2025-07-25 | 北京斯利安药业有限公司 | (s)-3-甲基-(2-哌啶基苯基)-1-丁胺乙酰谷氨酸盐的制备方法 |
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| EP1637522A1 (en) * | 2004-09-16 | 2006-03-22 | Laboratorios Del Dr. Esteve, S.A. | Substituted pyrazoline compounds for reducing triglycerides in blood |
| EP1743894A1 (en) * | 2005-07-15 | 2007-01-17 | Laboratorios Del Dr. Esteve, S.A. | Heterocyclyl-substituted pyrazoline compounds, their preparation and use as medicaments |
| WO2009115515A1 (en) * | 2008-03-18 | 2009-09-24 | Solvay Pharmaceuticals B.V. | Arylsulfonyl pyrazoline carboxamidine derivatives as 5-ht6 antagonists |
| WO2012068529A2 (en) * | 2010-11-18 | 2012-05-24 | Jenrin Discovery | Cannabinoid receptor antagonists-inverse agonists useful for treating metabolic disorders, including obesity and diabetes |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5614492A (en) | 1986-05-05 | 1997-03-25 | The General Hospital Corporation | Insulinotropic hormone GLP-1 (7-36) and uses thereof |
| EP1513817A1 (en) | 2002-05-24 | 2005-03-16 | Takeda Pharmaceutical Company Limited | 1, 2-azole derivatives with hypoglycemic and hypolipidemic activity |
| PL374860A1 (en) | 2002-07-09 | 2005-11-14 | Bristol-Myers Squibb Company | Substituted heterocyclic derivatives useful as antidiabetic and antiobesity agents and method |
| US7501440B2 (en) | 2003-03-07 | 2009-03-10 | Sanofi-Aventis Deutschland Gmbh | Substituted benzoylureidopyridylpiperidine-and-pyrrolidinecarboxylic acid derivatives, processes for preparing them and their use |
| US6995183B2 (en) | 2003-08-01 | 2006-02-07 | Bristol Myers Squibb Company | Adamantylglycine-based inhibitors of dipeptidyl peptidase IV and methods |
| BRPI0507790A (pt) * | 2004-02-17 | 2007-07-17 | Esteve Labor Dr | composto de pirazolina substituìda, processo para a sua manufatura, medicamentos e seus usos |
| BRPI0508098A (pt) | 2004-02-27 | 2007-07-17 | Amgen Inc | compostos, composições farmacêuticas e métodos para uso no tratamento de distúrbios metabólicos |
| US7517910B2 (en) | 2004-03-30 | 2009-04-14 | Takeda Pharmaceutical Company Limited | Alkoxyphenylpropanoic acid derivatives |
| JP2007284350A (ja) | 2004-07-27 | 2007-11-01 | Takeda Chem Ind Ltd | 糖尿病治療剤 |
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- 2013-11-15 WO PCT/US2013/070215 patent/WO2014078610A1/en not_active Ceased
- 2013-11-15 EA EA201590954A patent/EA026913B1/ru not_active IP Right Cessation
- 2013-11-15 SI SI201330340T patent/SI2920165T1/sl unknown
- 2013-11-15 SG SG11201503558SA patent/SG11201503558SA/en unknown
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- 2013-11-15 LT LTEP13811645.4T patent/LT2920165T/lt unknown
- 2013-11-15 RS RS20161061A patent/RS55363B1/sr unknown
- 2013-11-15 AU AU2013344604A patent/AU2013344604B2/en not_active Ceased
- 2013-11-15 BR BR112015010779A patent/BR112015010779A2/pt not_active Application Discontinuation
- 2013-11-15 EP EP13811645.4A patent/EP2920165B1/en active Active
- 2013-11-15 UY UY0001035143A patent/UY35143A/es not_active Application Discontinuation
- 2013-11-15 TW TW102141762A patent/TW201427971A/zh unknown
- 2013-11-15 US US14/081,094 patent/US9133163B2/en active Active
- 2013-11-15 PT PT138116454T patent/PT2920165T/pt unknown
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- 2013-11-15 CA CA2891574A patent/CA2891574A1/en not_active Abandoned
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Also Published As
| Publication number | Publication date |
|---|---|
| CY1118365T1 (el) | 2017-06-28 |
| MX2015005735A (es) | 2015-09-16 |
| TW201427971A (zh) | 2014-07-16 |
| KR20150082616A (ko) | 2015-07-15 |
| EA026913B1 (ru) | 2017-05-31 |
| US20140142139A1 (en) | 2014-05-22 |
| CA2891574A1 (en) | 2014-05-22 |
| US9133163B2 (en) | 2015-09-15 |
| SI2920165T1 (sl) | 2017-02-28 |
| MX358499B (es) | 2018-08-23 |
| RS55363B1 (sr) | 2017-03-31 |
| BR112015010779A2 (pt) | 2017-07-11 |
| PT2920165T (pt) | 2016-12-20 |
| EP2920165B1 (en) | 2016-09-28 |
| LT2920165T (lt) | 2016-12-12 |
| EP2920165A1 (en) | 2015-09-23 |
| JP6322203B2 (ja) | 2018-05-09 |
| UY35143A (es) | 2014-05-30 |
| SG11201503558SA (en) | 2015-06-29 |
| ES2606685T3 (es) | 2017-03-27 |
| AU2013344604B2 (en) | 2017-07-27 |
| PL2920165T3 (pl) | 2017-04-28 |
| HRP20161631T1 (hr) | 2017-01-13 |
| IL238741A0 (en) | 2015-06-30 |
| AU2013344604A1 (en) | 2015-07-02 |
| SMT201600410B (it) | 2017-01-10 |
| DK2920165T3 (en) | 2017-01-16 |
| EA201590954A1 (ru) | 2015-08-31 |
| CN104812748A (zh) | 2015-07-29 |
| WO2014078610A1 (en) | 2014-05-22 |
| JP2016500063A (ja) | 2016-01-07 |
| KR102204804B1 (ko) | 2021-01-18 |
| HUE032401T2 (en) | 2017-09-28 |
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