CN104411710A - 作为ptp-1b抑制剂前体的稠合的芳族膦酸酯衍生物 - Google Patents
作为ptp-1b抑制剂前体的稠合的芳族膦酸酯衍生物 Download PDFInfo
- Publication number
- CN104411710A CN104411710A CN201380020092.3A CN201380020092A CN104411710A CN 104411710 A CN104411710 A CN 104411710A CN 201380020092 A CN201380020092 A CN 201380020092A CN 104411710 A CN104411710 A CN 104411710A
- Authority
- CN
- China
- Prior art keywords
- alkyl
- optionally substituted
- halogen
- aryl
- heteroaryl
- Prior art date
- Legal status (The legal status 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 status listed.)
- Pending
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
- C07F9/6571—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
- C07F9/657163—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms the ring phosphorus atom being bound to at least one carbon atom
- C07F9/657181—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms the ring phosphorus atom being bound to at least one carbon atom the ring phosphorus atom and, at least, one ring oxygen atom being part of a (thio)phosphonic acid derivative
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
- C07F9/6571—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
- C07F9/657163—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms the ring phosphorus atom being bound to at least one carbon atom
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/662—Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/665—Phosphorus compounds having oxygen as a ring hetero atom, e.g. fosfomycin
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
- C07F9/40—Esters thereof
- C07F9/4003—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
- C07F9/4021—Esters of aromatic acids (P-C aromatic linkage)
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
- C07F9/40—Esters thereof
- C07F9/4003—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
- C07F9/4056—Esters of arylalkanephosphonic acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
- C07F9/576—Six-membered rings
- C07F9/58—Pyridine rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261624572P | 2012-04-16 | 2012-04-16 | |
| US61/624572 | 2012-04-16 | ||
| PCT/CA2013/000364 WO2013155600A1 (en) | 2012-04-16 | 2013-04-16 | Fused aromatic phosphonate derivatives as precursors to ptp-1b inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN104411710A true CN104411710A (zh) | 2015-03-11 |
Family
ID=49382741
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201380020092.3A Pending CN104411710A (zh) | 2012-04-16 | 2013-04-16 | 作为ptp-1b抑制剂前体的稠合的芳族膦酸酯衍生物 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20150057220A1 (https=) |
| EP (1) | EP2838906A4 (https=) |
| JP (1) | JP2015519309A (https=) |
| KR (1) | KR20140145624A (https=) |
| CN (1) | CN104411710A (https=) |
| AU (1) | AU2013248880A1 (https=) |
| CA (1) | CA2870488A1 (https=) |
| IL (1) | IL235081A0 (https=) |
| IN (1) | IN2014DN09640A (https=) |
| MX (1) | MX2014012465A (https=) |
| WO (1) | WO2013155600A1 (https=) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2023220833A1 (en) * | 2022-05-19 | 2023-11-23 | Kanyr Pharma Inc. | Combined inhibition of tyrosine phosphatases tcptp and ptp1b and pd-1 blockage immunotherapy in the treatment of cancer |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001070754A1 (en) * | 2000-03-22 | 2001-09-27 | Merck Frosst Canada & Co. | Sulfur substituted aryldifluoromethylphosphonic acids as ptp-1b inhibitors |
| CN102317296A (zh) * | 2007-01-26 | 2012-01-11 | 默克弗罗斯特加拿大有限公司 | 稠合芳烃ptp-1b抑制剂 |
Family Cites Families (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4166452A (en) | 1976-05-03 | 1979-09-04 | Generales Constantine D J Jr | Apparatus for testing human responses to stimuli |
| US4256108A (en) | 1977-04-07 | 1981-03-17 | Alza Corporation | Microporous-semipermeable laminated osmotic system |
| US4265874A (en) | 1980-04-25 | 1981-05-05 | Alza Corporation | Method of delivering drug with aid of effervescent activity generated in environment of use |
| US5545618A (en) | 1990-01-24 | 1996-08-13 | Buckley; Douglas I. | GLP-1 analogs useful for diabetes treatment |
| AU1856997A (en) | 1996-02-02 | 1997-08-22 | Merck & Co., Inc. | Method for raising hdl cholesterol levels |
| AR008789A1 (es) | 1996-07-31 | 2000-02-23 | Bayer Corp | Piridinas y bifenilos substituidos |
| UA65549C2 (uk) | 1996-11-05 | 2004-04-15 | Елі Ліллі Енд Компані | Спосіб регулювання ожиріння шляхом периферійного введення аналогів та похідних glp-1 (варіанти) та фармацевтична композиція |
| AU6452098A (en) | 1997-03-07 | 1998-09-22 | Metabasis Therapeutics, Inc. | Novel purine inhibitors of fructose-1,6-bisphosphatase |
| DE69819311T2 (de) | 1997-03-07 | 2004-07-29 | Metabasis Therapeutics Inc., San Diego | Neue benzimidazol inhibitoren der fructose-1,6-bisphosphatase |
| US6054587A (en) | 1997-03-07 | 2000-04-25 | Metabasis Therapeutics, Inc. | Indole and azaindole inhibitors of fructose-1,6-bisphosphatase |
| US6613942B1 (en) | 1997-07-01 | 2003-09-02 | Novo Nordisk A/S | Glucagon antagonists/inverse agonists |
| AU749271B2 (en) | 1997-07-01 | 2002-06-20 | Agouron Pharmaceuticals, Inc. | Glucagon antagonists/inverse agonists |
| ATE246197T1 (de) | 1998-09-09 | 2003-08-15 | Metabasis Therapeutics Inc | Neue heteroaromatische fructose 1,6- bisphosphatase inhibitoren |
| JP2002534512A (ja) | 1999-01-15 | 2002-10-15 | ノボ ノルディスク アクティーゼルスカブ | 非ペプチドglp−1アゴニスト |
| PT1171465E (pt) | 1999-03-29 | 2004-12-31 | Uutech Ltd | Analogos de petido inibidor gastrico e sua utilizacao para o tratamento de diabetes |
| AU4055400A (en) | 1999-04-02 | 2000-10-23 | Neurogen Corporation | Aryl and heteroaryl fused aminoalkyl-imidazole derivatives and their use as antidiabetics |
| WO2000069810A1 (en) | 1999-05-17 | 2000-11-23 | Novo Nordisk A/S | Glucagon antagonists/inverse agonists |
| RU2269354C2 (ru) | 1999-09-28 | 2006-02-10 | Байер Корпорейшн | Агонисты рецептора-3(r3) пептида-активатора гипофизарной аденилатциклазы(расар) и способы их фармакологического применения |
| WO2002008188A1 (en) | 2000-07-25 | 2002-01-31 | Merck & Co., Inc. | N-substituted indoles useful in the treatment of diabetes |
| WO2002060388A2 (en) | 2001-01-30 | 2002-08-08 | Merck & Co., Inc. | Acyl sulfamides for treatment of obesity, diabetes and lipid disorders |
| UA74912C2 (en) | 2001-07-06 | 2006-02-15 | Merck & Co Inc | Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes |
| SE0102764D0 (sv) | 2001-08-17 | 2001-08-17 | Astrazeneca Ab | Compounds |
| GB0121709D0 (en) | 2001-09-07 | 2001-10-31 | Imp College Innovations Ltd | Food inhibition agent |
| AR040241A1 (es) | 2002-06-10 | 2005-03-23 | Merck & Co Inc | Inhibidores de la 11-beta-hidroxiesteroide deshidrogrenasa 1 para el tratamiento de la diabetes obesidad y dislipidemia |
| WO2004020408A1 (en) | 2002-08-29 | 2004-03-11 | Merck & Co., Inc. | Indoles having anti-diabetic activity |
| WO2004019869A2 (en) | 2002-08-29 | 2004-03-11 | Merck & Co., Inc. | Indoles having anti-diabetic activity |
| JO2397B1 (en) | 2002-12-20 | 2007-06-17 | ميرك شارب اند دوم كوربوريشن | Terazol derivatives as beta-hydroxy steroid dihydrogenase-1 inhibitors |
| JP2007504285A (ja) | 2003-01-17 | 2007-03-01 | メルク エンド カムパニー インコーポレーテッド | N−シクロヘキシルアミノカルボニルベンゼンスルホンアミド誘導体 |
| EP1598349B1 (en) | 2003-02-13 | 2011-07-27 | Msd K.K. | Novel 2-pyridinecarboxamide derivatives |
| NZ541824A (en) | 2003-02-26 | 2010-04-30 | Banyu Pharma Co Ltd | Heteroarylcarbamoylbenzene derivatives as glucokinase activators |
| RU2485135C2 (ru) | 2005-06-13 | 2013-06-20 | Импиэриэл Инноувейшнс Лимитид | Соединения оксинтомодулина (варианты), фармацевтическая композиция на их основе, способы лечения и профилактики ожирения и сопутствующих заболеваний (варианты) и лекарственное средство (варианты) |
| CN101389648B (zh) | 2006-02-22 | 2013-07-17 | 默沙东公司 | 肽胃泌酸调节素衍生物 |
| KR20090005329A (ko) | 2006-03-20 | 2009-01-13 | 머크 앤드 캄파니 인코포레이티드 | 뉴로메딘 u 수용체 효능제 및 이의 용도 |
| AU2007275294A1 (en) | 2006-07-18 | 2008-01-24 | Centocor, Inc. | Human GLP-1 mimetibodies, compositions, methods and uses |
| AU2008216265B2 (en) | 2007-02-15 | 2014-04-03 | Indiana University Research And Technology Corporation | Glucagon/GLP-1 receptor co-agonists |
| AU2008267724A1 (en) | 2007-06-28 | 2008-12-31 | Merck Frosst Canada Ltd | Substituted fused pyrimidines as antagonists of GPR105 activity |
| EP2178537A4 (en) | 2007-07-19 | 2011-08-17 | Merck Sharp & Dohme | BETA-CARBOLIN DERIVATIVES AS ANTIDIBLE COMPOUNDS |
| WO2009042053A2 (en) | 2007-09-21 | 2009-04-02 | Merck & Co., Inc. | Neuromedin u receptor agonists and uses thereof |
-
2013
- 2013-04-16 WO PCT/CA2013/000364 patent/WO2013155600A1/en not_active Ceased
- 2013-04-16 JP JP2015506051A patent/JP2015519309A/ja not_active Withdrawn
- 2013-04-16 AU AU2013248880A patent/AU2013248880A1/en not_active Abandoned
- 2013-04-16 MX MX2014012465A patent/MX2014012465A/es unknown
- 2013-04-16 CN CN201380020092.3A patent/CN104411710A/zh active Pending
- 2013-04-16 US US14/394,503 patent/US20150057220A1/en not_active Abandoned
- 2013-04-16 IN IN9640DEN2014 patent/IN2014DN09640A/en unknown
- 2013-04-16 EP EP13778030.0A patent/EP2838906A4/en not_active Withdrawn
- 2013-04-16 KR KR1020147032070A patent/KR20140145624A/ko not_active Withdrawn
- 2013-04-16 CA CA2870488A patent/CA2870488A1/en not_active Abandoned
-
2014
- 2014-10-07 IL IL235081A patent/IL235081A0/en unknown
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001070754A1 (en) * | 2000-03-22 | 2001-09-27 | Merck Frosst Canada & Co. | Sulfur substituted aryldifluoromethylphosphonic acids as ptp-1b inhibitors |
| CN102317296A (zh) * | 2007-01-26 | 2012-01-11 | 默克弗罗斯特加拿大有限公司 | 稠合芳烃ptp-1b抑制剂 |
Non-Patent Citations (4)
| Title |
|---|
| DIPAM PATEL等: ""Discovery of Orally Active, Potent, and Selective Benzotriazole-Based PTP1B Inhibitors"", 《CHEMMEDCHEM》 * |
| JACQUELINE MONTALIBET等: ""Residues Distant from the Active Site Influence Protein-tyrosine Phosphatase 1B Inhibitor Binding"", 《THE JOURNAL OF BIOLOGICAL CHEMISTRY》 * |
| YONGXIN HAN等: ""Discovery of [(3-bromo-7-cyano-2-naphthyl)(difluoro)- methyl]phosphonic acid, a potent and orally active small molecule PTP1B inhibitor "", 《BIOORGANIC & MEDICINAL CHEMISTRY LETTERS》 * |
| YONGXIN HAN等: ""Discovery of [(3-bromo-7-cyano-2-naphthyl)(difluoro)- methyl]phosphonic acid, a potent and orally active small molecule PTP1B inhibitor "", 《BIOORGANIC & MEDICINAL CHEMISTRY LETTERS》, vol. 18, 29 April 2008 (2008-04-29), pages 3202 - 1 * |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2013155600A1 (en) | 2013-10-24 |
| IN2014DN09640A (https=) | 2015-07-31 |
| IL235081A0 (en) | 2014-12-31 |
| MX2014012465A (es) | 2015-01-12 |
| JP2015519309A (ja) | 2015-07-09 |
| CA2870488A1 (en) | 2013-10-24 |
| US20150057220A1 (en) | 2015-02-26 |
| KR20140145624A (ko) | 2014-12-23 |
| AU2013248880A1 (en) | 2014-11-06 |
| EP2838906A1 (en) | 2015-02-25 |
| EP2838906A4 (en) | 2015-07-15 |
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| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20150311 |