CA2863413A1 - Substituted prolines / piperidines as orexin receptor antagonists - Google Patents
Substituted prolines / piperidines as orexin receptor antagonists Download PDFInfo
- Publication number
- CA2863413A1 CA2863413A1 CA2863413A CA2863413A CA2863413A1 CA 2863413 A1 CA2863413 A1 CA 2863413A1 CA 2863413 A CA2863413 A CA 2863413A CA 2863413 A CA2863413 A CA 2863413A CA 2863413 A1 CA2863413 A1 CA 2863413A1
- Authority
- CA
- Canada
- Prior art keywords
- orexin receptor
- piperidines
- receptor antagonists
- substituted prolines
- compounds
- 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.)
- Abandoned
Links
- 229940123730 Orexin receptor antagonist Drugs 0.000 title 1
- 150000003053 piperidines Chemical class 0.000 title 1
- 235000013930 proline Nutrition 0.000 title 1
- 150000003148 prolines Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 108050000742 Orexin Receptor Proteins 0.000 abstract 2
- 102000008834 Orexin receptor Human genes 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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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- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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- A—HUMAN NECESSITIES
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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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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P25/00—Drugs for disorders of the nervous system
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- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D401/12—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D401/14—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
-
- 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
-
- 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
- C07D417/02—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 two hetero rings
- C07D417/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- C07D417/02—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 two hetero rings
- C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D471/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Addiction (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Psychology (AREA)
- Obesity (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Anesthesiology (AREA)
- Cardiology (AREA)
- Hospice & Palliative Care (AREA)
- Reproductive Health (AREA)
- Urology & Nephrology (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261596062P | 2012-02-07 | 2012-02-07 | |
| US61/596,062 | 2012-02-07 | ||
| PCT/US2013/024903 WO2013119639A1 (en) | 2012-02-07 | 2013-02-06 | Substituted prolines / piperidines as orexin receptor antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2863413A1 true CA2863413A1 (en) | 2013-08-15 |
Family
ID=48947950
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2863413A Abandoned CA2863413A1 (en) | 2012-02-07 | 2013-02-06 | Substituted prolines / piperidines as orexin receptor antagonists |
Country Status (18)
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2491038B1 (en) | 2009-10-23 | 2016-04-06 | Janssen Pharmaceutica N.V. | Disubstituted octahy - dropyrrolo [3,4-c]pyrroles as orexin receptor modulators |
| WO2013119639A1 (en) | 2012-02-07 | 2013-08-15 | Eolas Therapeutics, Inc. | Substituted prolines / piperidines as orexin receptor antagonists |
| US9440982B2 (en) | 2012-02-07 | 2016-09-13 | Eolas Therapeutics, Inc. | Substituted prolines/piperidines as orexin receptor antagonists |
| ITMI20120322A1 (it) * | 2012-03-01 | 2013-09-02 | Rottapharm Spa | Composti di 4,4-difluoro piperidina |
| WO2014085208A1 (en) * | 2012-11-27 | 2014-06-05 | Merck Sharp & Dohme Corp. | 2-pyridylamino-4-nitrile-piperidinyl orexin receptor antagonists |
| WO2015018027A1 (en) * | 2013-08-08 | 2015-02-12 | Merck Sharp & Dohme Corp. | Thiazole orexin receptor antagonists |
| JP2017001954A (ja) * | 2013-11-08 | 2017-01-05 | 石原産業株式会社 | 含窒素飽和複素環化合物 |
| JP2017024990A (ja) * | 2013-12-13 | 2017-02-02 | 大正製薬株式会社 | オキサゾリジン及びオキサジナン誘導体 |
| TW201613891A (en) * | 2014-02-12 | 2016-04-16 | Eolas Therapeutics Inc | Substituted prolines / piperidines as orexin receptor antagonists |
| US10221170B2 (en) | 2014-08-13 | 2019-03-05 | Eolas Therapeutics, Inc. | Difluoropyrrolidines as orexin receptor modulators |
| MX2017003254A (es) * | 2014-09-11 | 2017-10-12 | Janssen Pharmaceutica Nv | 2-azabiciclos sustituidos y su uso como moduladores de receptores de orexina. |
| JP2018016544A (ja) * | 2014-12-03 | 2018-02-01 | 持田製薬株式会社 | 新規ジアザビシクロ[2.2.2]オクタン誘導体 |
| CN104557744B (zh) * | 2014-12-23 | 2017-04-12 | 广东东阳光药业有限公司 | 一种三氮唑化合物的制备方法 |
| DK3414241T3 (da) | 2016-02-12 | 2022-08-01 | Astrazeneca Ab | Halogensubstituerede piperidiner som orexinreceptormodulatorer |
| US10828302B2 (en) | 2016-03-10 | 2020-11-10 | Janssen Pharmaceutica Nv | Methods of treating depression using orexin-2 receptor antagonists |
| RU2738646C2 (ru) * | 2016-04-01 | 2020-12-15 | РЕКЬЮРИУМ АйПи ХОЛДИНГС, ЛЛС | Модуляторы эстрогеновых рецепторов |
| SG11201809527UA (en) * | 2016-05-12 | 2018-11-29 | Eisai R&D Man Co Ltd | Methods of treating circadian rhythm sleep disorders |
| GB2558975B (en) * | 2017-09-01 | 2019-01-23 | Chronos Therapeutics Ltd | Substituted 2-azabicyclo[3.1.1]heptane and 2-azabicyclo[3.2.1]octane derivatives as orexin receptor antagonists |
| US11660293B2 (en) * | 2017-09-01 | 2023-05-30 | Chronos Therapeutics Limited | Substituted 2-azabicyclo[3.1.1]heptane and 2-azabicyclo[3.2.1]octane derivatives as orexin receptor antagonists |
| US12187737B2 (en) | 2019-06-04 | 2025-01-07 | Hager Biosciences, Llc | Imidazolo derivatives, compositions and methods as orexin antagonists |
| CA3140173A1 (en) * | 2019-06-04 | 2020-12-10 | Belew Mekonnen | Pyrazole and imidazole derivatives, compositions and methods as orexin antagonists |
| BR112023024311A2 (pt) * | 2021-05-26 | 2024-02-06 | Sumitomo Pharma Co Ltd | Derivado de fenil ureia |
Family Cites Families (146)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5049578A (en) * | 1990-03-09 | 1991-09-17 | E. R. Squibb & Sons, Inc. | 1-aroyl or 1-acyl-2-2pyrrolidinyl-3,5-dihydroxy alkanoic and alkenoic acids, salts, esters and lactones |
| JP4633925B2 (ja) | 1998-05-08 | 2011-02-16 | スミスクライン ビーチャム ピー エル シー | フェニル尿素およびフェニルチオ尿素誘導体 |
| JP2002536447A (ja) | 1999-02-12 | 2002-10-29 | スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー | フェニル尿素およびフェニルチオ尿素誘導体 |
| JP2002536445A (ja) | 1999-02-12 | 2002-10-29 | スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー | オレキシン受容体アンタゴニストとしてのフェニル尿素およびフェニルチオ尿素誘導体 |
| WO2000047576A1 (en) | 1999-02-12 | 2000-08-17 | Smithkline Beecham Plc | Cinnamide derivatives as orexin-1 receptors antagonists |
| JP2003500386A (ja) * | 1999-05-24 | 2003-01-07 | シーオーアール セラピューティクス インコーポレイテッド | Xa因子阻害剤 |
| CA2408343A1 (en) | 2000-05-11 | 2002-11-07 | Banyu Pharmaceutical Co., Ltd. | N-acyltetrahydroisoquinoline derivatives |
| AU2001272476A1 (en) * | 2000-06-16 | 2001-12-24 | Smithkline Beecham Plc | Piperidines for use as orexin receptor antagonists |
| DE60108420T2 (de) | 2000-11-28 | 2005-12-22 | Smithkline Beecham P.L.C., Brentford | Morpholinderivate als antagonisten an orexinrezeptoren |
| WO2002051232A2 (en) | 2000-12-27 | 2002-07-04 | Actelion Pharmaceuticals Ltd. | Novel benzazepines and related heterocyclic derivatives |
| JP2004534026A (ja) * | 2001-05-05 | 2004-11-11 | スミスクライン ビーチャム パブリック リミテッド カンパニー | オレキシン受容体アンタゴニストとしてのn−アロイルサイクリックアミン誘導体 |
| MXPA03010129A (es) * | 2001-05-05 | 2004-03-10 | Smithkline Beecham Plc | N-aroilaminas-ciclicas. |
| GB0115862D0 (en) | 2001-06-28 | 2001-08-22 | Smithkline Beecham Plc | Compounds |
| GB0124463D0 (en) | 2001-10-11 | 2001-12-05 | Smithkline Beecham Plc | Compounds |
| GB0126292D0 (en) | 2001-11-01 | 2002-01-02 | Smithkline Beecham Plc | Compounds |
| GB0127145D0 (en) | 2001-11-10 | 2002-01-02 | Smithkline Beecham | Compounds |
| GB0130335D0 (en) | 2001-12-19 | 2002-02-06 | Smithkline Beecham Plc | Compounds |
| GB0130393D0 (en) | 2001-12-19 | 2002-02-06 | Smithkline Beecham Plc | Compounds |
| GB0130341D0 (en) | 2001-12-19 | 2002-02-06 | Smithkline Beecham Plc | Compounds |
| CA2460051A1 (en) | 2002-07-09 | 2004-01-15 | Actelion Pharmaceuticals Ltd. | 7,8,9,10-tetrahydro-6h-azepino, 6,7,8,9-tetrahydro-pyrido and 2,3-dihydro-2h-pyrrolo[2,1-b]-quinazolinone derivatives |
| WO2004026866A1 (en) * | 2002-09-18 | 2004-04-01 | Glaxo Group Limited | N-aroyl cyclic amines as orexin receptor antagonists |
| ATE496884T1 (de) | 2002-10-11 | 2011-02-15 | Actelion Pharmaceuticals Ltd | Sulphonylaminoessigsaeure derivate und deren verwendung als orexin rezeptor antagoniste |
| GB0225884D0 (en) * | 2002-11-06 | 2002-12-11 | Glaxo Group Ltd | Novel compounds |
| GB0225944D0 (en) | 2002-11-06 | 2002-12-11 | Glaxo Group Ltd | Novel compounds |
| GB0225938D0 (en) | 2002-11-06 | 2002-12-11 | Glaxo Group Ltd | Novel compounds |
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-
2013
- 2013-02-06 WO PCT/US2013/024903 patent/WO2013119639A1/en not_active Ceased
- 2013-02-06 KR KR1020147025072A patent/KR20140124398A/ko not_active Withdrawn
- 2013-02-06 CA CA2863413A patent/CA2863413A1/en not_active Abandoned
- 2013-02-06 MX MX2014009281A patent/MX2014009281A/es unknown
- 2013-02-06 BR BR112014019426A patent/BR112014019426A8/pt not_active IP Right Cessation
- 2013-02-06 HK HK15105691.4A patent/HK1204955A1/xx unknown
- 2013-02-06 AU AU2013217323A patent/AU2013217323A1/en not_active Abandoned
- 2013-02-06 SG SG11201404738QA patent/SG11201404738QA/en unknown
- 2013-02-06 ES ES13746989.6T patent/ES2672732T3/es active Active
- 2013-02-06 CN CN201380018420.6A patent/CN104220065A/zh active Pending
- 2013-02-06 JP JP2014556628A patent/JP6346862B2/ja active Active
- 2013-02-06 RU RU2014136339A patent/RU2014136339A/ru not_active Application Discontinuation
- 2013-02-06 EP EP13746989.6A patent/EP2811997B1/en active Active
- 2013-02-06 NZ NZ628491A patent/NZ628491A/en not_active IP Right Cessation
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2014
- 2014-02-12 US US14/179,432 patent/US9499517B2/en active Active
- 2014-08-07 PH PH12014501784A patent/PH12014501784A1/en unknown
- 2014-08-07 IL IL234025A patent/IL234025A0/en unknown
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2015
- 2015-02-11 AR ARP150100403A patent/AR099466A1/es unknown
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2016
- 2016-10-20 US US15/299,230 patent/US9896452B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| US9896452B2 (en) | 2018-02-20 |
| EP2811997B1 (en) | 2018-04-11 |
| JP2015506382A (ja) | 2015-03-02 |
| WO2013119639A1 (en) | 2013-08-15 |
| US20170101410A1 (en) | 2017-04-13 |
| SG11201404738QA (en) | 2014-10-30 |
| AU2013217323A1 (en) | 2014-08-28 |
| US20140364432A1 (en) | 2014-12-11 |
| ES2672732T3 (es) | 2018-06-15 |
| BR112014019426A8 (pt) | 2017-07-11 |
| HK1204955A1 (zh) | 2015-12-11 |
| EP2811997A1 (en) | 2014-12-17 |
| MX2014009281A (es) | 2015-01-12 |
| CN104220065A (zh) | 2014-12-17 |
| EP2811997A4 (en) | 2015-07-22 |
| KR20140124398A (ko) | 2014-10-24 |
| AR099466A1 (es) | 2016-07-27 |
| PH12014501784A1 (en) | 2014-11-10 |
| RU2014136339A (ru) | 2016-03-27 |
| US9499517B2 (en) | 2016-11-22 |
| IL234025A0 (en) | 2014-09-30 |
| NZ628491A (en) | 2016-06-24 |
| BR112014019426A2 (cg-RX-API-DMAC7.html) | 2017-06-20 |
| JP6346862B2 (ja) | 2018-06-20 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FZDE | Discontinued |
Effective date: 20180206 |