AR078732A1 - Compuestos heterociclicos fusionados como moduladores del receptor de la orexina - Google Patents
Compuestos heterociclicos fusionados como moduladores del receptor de la orexinaInfo
- Publication number
- AR078732A1 AR078732A1 ARP100103875A ARP100103875A AR078732A1 AR 078732 A1 AR078732 A1 AR 078732A1 AR P100103875 A ARP100103875 A AR P100103875A AR P100103875 A ARP100103875 A AR P100103875A AR 078732 A1 AR078732 A1 AR 078732A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- group
- alkyl
- unsubstituted
- halo
- Prior art date
Links
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
- C07D471/04—Ortho-condensed systems
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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
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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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/12—Antidiarrhoeals
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
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- 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
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- 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
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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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
- A61P9/06—Antiarrhythmics
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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
- A61P9/10—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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- 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
- 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
- C07D487/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Reproductive Health (AREA)
- Psychiatry (AREA)
- Endocrinology (AREA)
- Hospice & Palliative Care (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Anesthesiology (AREA)
- Psychology (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
Abstract
Dichos compuestos pueden ser utiles en composiciones farmacéuticas y métodos para el tratamiento de estados anormales, trastornos y afecciones mediadas por la actividad de la orexina, tales como insomnio. Reivindicacion 1: Una entidad química que es un compuesto de Formula (1): en donde n es 0-1; R1 es un miembro seleccionado del grupo que consiste de: A) fenilo sustituido o no sustituido con Ra, y sustituido en la posicion orto con Rb; Ra es un miembro seleccionado independientemente del grupo que consiste de: halo, alquilo -C1-4, y alcoxi -C1-4; Rb es un miembro seleccionado del grupo que consiste de: a) halo o alcoxi -C1-4, b) tiofen-2-ilo, 2H-1,2,3-triazol, 1H-1,2,3-triazol-1-ilo, 1H-pirazol-1-ilo, 1H-pirazol-5-ilo, pirimidin-2-ilo, o 3-metil-1,2,4-oxadiazol-5-ilo, y c) fenilo; B) piridina sustituida o no sustituida con uno o dos miembros seleccionados independientemente del grupo que consiste de: alquilo C1-4 y 1H-1,2,3-triazol-1-ilo, en donde los sustituyentes están en una posicion adyacente al punto de union por R1; y C) metiltiazol sustituido con 2-fluorofenilo; R2 es un miembro seleccionado del grupo que consiste de: A) anillo de heteroarilo de 6 miembros que contiene dos miembros de nitrogeno sustituidos o no sustituidos con uno o más miembros seleccionados del grupo que consiste de: -alquilo C1-4, -alcoxi C1-4, -CF3, halo, -N(alquilo C1-4)2, -NH2, y fenilo; B) piridina sustituida o no sustituida con uno o más miembros seleccionados independientemente del grupo que consiste de: -CF3 y alquilo -C1-4; C) quinoxalin-2-ilo o quinolina sustituida o no sustituida con -alquilo C1-4; D) benzooxazol-2-ilo sustituido o no sustituido con halo; y E) 4-metil-6,7-dihidro-5H-ciclopenta[d]pirimidina; y sales aceptables farmacéuticamente de compuestos de la Formula 1.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US25451709P | 2009-10-23 | 2009-10-23 |
Publications (1)
Publication Number | Publication Date |
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AR078732A1 true AR078732A1 (es) | 2011-11-30 |
Family
ID=43221929
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP100103875A AR078732A1 (es) | 2009-10-23 | 2010-10-22 | Compuestos heterociclicos fusionados como moduladores del receptor de la orexina |
Country Status (10)
Country | Link |
---|---|
US (1) | US9062044B2 (es) |
EP (1) | EP2491031B1 (es) |
JP (2) | JP5848251B2 (es) |
AR (1) | AR078732A1 (es) |
CL (1) | CL2010001160A1 (es) |
HK (1) | HK1175462A1 (es) |
PE (1) | PE20110328A1 (es) |
TW (1) | TW201141859A (es) |
UY (1) | UY32967A (es) |
WO (1) | WO2011050202A1 (es) |
Families Citing this family (30)
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WO2011029043A1 (en) | 2009-09-04 | 2011-03-10 | Biogen Idec Ma Inc. | Heteroaryl btk inhibitors |
US9062044B2 (en) * | 2009-10-23 | 2015-06-23 | Janssen Pharmaceutica Nv | Disubstituted octahydropyrrolo[3,4-c]pyrroles as orexin receptor modulators |
TR201910327T4 (tr) | 2009-10-23 | 2019-07-22 | Janssen Pharmaceutica Nv | Oreksin reseptör modülatörleri olarak di-ornatılmış oktahidropirrolo [3,4-c]pirroller. |
WO2012085852A1 (en) | 2010-12-22 | 2012-06-28 | Actelion Pharmaceuticals Ltd | 3,8-diaza-bicyclo[4.2.0]oct-8-yl amides |
US9586962B2 (en) | 2011-04-20 | 2017-03-07 | Janssen Pharmaceutica Nv | Disubstituted octahydropyrrolo [3,4-C] pyrroles as orexin receptor modulators |
DK2776430T3 (en) | 2011-11-08 | 2016-05-09 | Actelion Pharmaceuticals Ltd | 2- (1,2,3-triazol-2-yl) benzamide and 3- (1,2,3-triazol-2-yl) PICOLINAMIDDERIVATER AS orexin receptor antagonists |
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 |
HUE031753T2 (en) | 2012-06-04 | 2017-07-28 | Actelion Pharmaceuticals Ltd | Benzimidazole-proline derivatives |
BR112015007516A2 (pt) | 2012-10-10 | 2017-07-04 | Actelion Pharmaceuticals Ltd | antagonistas do receptor de orexina que são derivados de [orto bi-(hetero-)aril]-[2-(meta bi-(hetero-)aril)- pirrolidin-1-il]-metanona |
CN103012293A (zh) * | 2012-12-13 | 2013-04-03 | 同济大学 | 一种抗失眠药物mk-4305中间体的合成方法 |
US9403813B2 (en) | 2013-03-12 | 2016-08-02 | Actelion Pharmaceuticals Ltd. | Azetidine amide derivatives as orexin receptor antagonists |
TW201444849A (zh) | 2013-03-13 | 2014-12-01 | Janssen Pharmaceutica Nv | 經取代的7-氮雜雙環類及其作為食慾激素受體調節劑之用途 |
TW201444821A (zh) | 2013-03-13 | 2014-12-01 | Janssen Pharmaceutica Nv | 經取代之哌啶化合物及其作為食慾素受體調節劑之用途 |
TWI621618B (zh) | 2013-03-13 | 2018-04-21 | 比利時商健生藥品公司 | 經取代2-氮雜雙環類及其作為食慾素受體調控劑之用途 |
TWI644671B (zh) | 2013-03-14 | 2018-12-21 | 比利時商健生藥品公司 | P2x7調節劑 |
CA2930693A1 (en) | 2013-11-15 | 2015-05-21 | The Board Of Trustees Of The Leland Stanford Junior Unversity | Methods of treating heart failure with agonists of hypocretin receptor 2 |
EP3077391B1 (en) | 2013-12-04 | 2018-08-15 | Idorsia Pharmaceuticals Ltd | Use of benzimidazole-proline derivatives |
JP6663909B2 (ja) | 2014-08-13 | 2020-03-13 | エオラス セラピューティクス, インコーポレイテッド | オレキシンレセプターモジュレーターとしてのジフルオロピロリジン |
US9611262B2 (en) | 2014-09-11 | 2017-04-04 | Janssen Pharmaceutica Nv | Substituted 2-azabicycles and their use as orexin receptor modulators |
WO2017012502A1 (en) | 2015-07-17 | 2017-01-26 | Sunshine Lake Pharma Co., Ltd. | Substituted quinazoline compounds and preparation and uses thereof |
AU2016360245B2 (en) | 2015-11-23 | 2020-07-09 | Sunshine Lake Pharma Co., Ltd. | Octahydropyrrolo [3, 4-c] pyrrole derivatives and uses thereof |
EP3414241B1 (en) | 2016-02-12 | 2022-05-04 | Astrazeneca AB | Halo-substituted piperidines as orexin receptor modulators |
SI3426251T1 (sl) | 2016-03-10 | 2022-07-29 | Janssen Pharmaceutica Nv | Postopki za zdravljenje depresije z antagonisti receptorja oreksina-2 |
PT3619199T (pt) | 2017-05-03 | 2021-10-01 | Idorsia Pharmaceuticals Ltd | Preparação de derivados de ácido 2-([1,2,3]triazol-2-il)- benzoico |
CN113164459B (zh) | 2018-09-28 | 2024-09-03 | 詹森药业有限公司 | 单酰基甘油脂肪酶调节剂 |
JP7413368B2 (ja) | 2018-09-28 | 2024-01-15 | ヤンセン ファーマシューティカ エヌ.ベー. | モノアシルグリセロールリパーゼ調節因子 |
KR20210091726A (ko) * | 2018-11-14 | 2021-07-22 | 얀센 파마슈티카 엔.브이. | 오렉신 수용체 조절제로서의 융합 헤테로사이클릭 화합물을 제조하는 개선된 합성 방법 |
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AU2009307915A1 (en) | 2008-10-21 | 2010-04-29 | Merck Sharp & Dohme Corp. | 2,5-disubstituted piperidine orexin receptor antagonists |
PE20110852A1 (es) | 2008-10-30 | 2011-11-25 | Merck Sharp & Dohme | Antagonistas del receptor de orexina de isonicotinamida |
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GB0823467D0 (en) | 2008-12-23 | 2009-01-28 | Glaxo Group Ltd | Novel Compounds |
US9062044B2 (en) * | 2009-10-23 | 2015-06-23 | Janssen Pharmaceutica Nv | Disubstituted octahydropyrrolo[3,4-c]pyrroles as orexin receptor modulators |
-
2010
- 2010-10-21 US US13/503,298 patent/US9062044B2/en active Active
- 2010-10-21 JP JP2012535386A patent/JP5848251B2/ja not_active Expired - Fee Related
- 2010-10-21 WO PCT/US2010/053611 patent/WO2011050202A1/en active Application Filing
- 2010-10-21 EP EP10773478.2A patent/EP2491031B1/en active Active
- 2010-10-22 PE PE2010000998A patent/PE20110328A1/es not_active Application Discontinuation
- 2010-10-22 CL CL2010001160A patent/CL2010001160A1/es unknown
- 2010-10-22 TW TW099136021A patent/TW201141859A/zh unknown
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- 2010-10-25 UY UY0001032967A patent/UY32967A/es not_active Application Discontinuation
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2013
- 2013-02-27 HK HK13102494.2A patent/HK1175462A1/xx not_active IP Right Cessation
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US20130137672A1 (en) | 2013-05-30 |
JP2013508405A (ja) | 2013-03-07 |
JP5848251B2 (ja) | 2016-01-27 |
TW201141859A (en) | 2011-12-01 |
JP2016102118A (ja) | 2016-06-02 |
HK1175462A1 (en) | 2013-07-05 |
US9062044B2 (en) | 2015-06-23 |
EP2491031B1 (en) | 2013-08-07 |
UY32967A (es) | 2011-04-29 |
EP2491031A1 (en) | 2012-08-29 |
WO2011050202A1 (en) | 2011-04-28 |
PE20110328A1 (es) | 2011-06-09 |
CL2010001160A1 (es) | 2011-03-25 |
JP6170121B2 (ja) | 2017-07-26 |
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