AR083831A1 - Antagonistas del receptor del cgrp de piperidinona carboxamida azaindano - Google Patents
Antagonistas del receptor del cgrp de piperidinona carboxamida azaindanoInfo
- Publication number
- AR083831A1 AR083831A1 ARP110104204A ARP110104204A AR083831A1 AR 083831 A1 AR083831 A1 AR 083831A1 AR P110104204 A ARP110104204 A AR P110104204A AR P110104204 A ARP110104204 A AR P110104204A AR 083831 A1 AR083831 A1 AR 083831A1
- Authority
- AR
- Argentina
- Prior art keywords
- hydrogen
- methyl
- cgrp
- piperidinona
- azaindano
- Prior art date
Links
Classifications
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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
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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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
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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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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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
- A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring 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
- 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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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
- A61P13/10—Drugs for disorders of the urinary system of the bladder
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
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- 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
- A61P25/08—Antiepileptics; Anticonvulsants
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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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
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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
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P9/00—Drugs for disorders of the cardiovascular system
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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
- A61P9/08—Vasodilators for multiple indications
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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
- C07D471/10—Spiro-condensed systems
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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
- C07D471/12—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 three hetero rings
- C07D471/20—Spiro-condensed systems
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Cardiology (AREA)
- Dermatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Obesity (AREA)
- Addiction (AREA)
- Child & Adolescent Psychology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Psychiatry (AREA)
- Emergency Medicine (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La presente se refiere a derivados de piperidinona carboxamida azaindano que son antagonistas de receptores del CGRP y útiles en el tratamiento o prevención de enfermedades en las que está implicado el CGRP, tales como migraña. También se refiere a composiciones farmacéuticas que comprende estos compuestos y al uso de estos compuestos y composiciones en la prevención o tratamiento de dichas enfermedades en las que está implicado el CGRP.Reivindicación 1: Un compuesto de fórmula (1) o una sal farmacéuticamente aceptable del mismo, en la que: X se selecciona entre -C(R8)= o -N=, donde R8 es hidrógeno, F o CN; R1 se selecciona entre el grupo que consiste en: alquilo C1-4, ciclopropilmetilo, ciclobutilmetilo y [1-(trifluorometil)ciclopropil]metilo, cada uno de los cuales está opcionalmente sustituido con uno o más sustituyentes según lo permitido por la valencia independientemente seleccionada entre el grupo que consiste en: F e hidroxi; R2 se selecciona entre hidrógeno y metilo; cuando R2 es hidrógeno entonces R3 se selecciona entre hidrógeno, F o Cl; R4 se selecciona entre hidrógeno, F o Cl; R5 es hidrógeno; R6 se selecciona entre hidrógeno o F; y R7 se selecciona entre hidrógeno, F o Cl; con la excepción de que al menos dos de R3, R4, R6 y R7 deben ser F o Cl amenos que R3 sea F, en cuyo caso R4, R6 y R7 pueden ser todos hidrógeno; y si R4 es Cl, entonces R7 no puede ser Cl; cuando R2 es metilo entonces R3 se selecciona entre hidrógeno, metilo, F, Cl o Br; R4 se selecciona entre hidrógeno, metilo, F o Cl; R5 se selecciona entre hidrógeno o F; R6 se selecciona entre hidrógeno o F; y R7 se selecciona entre hidrógeno, metilo, F o Cl; con la excepción de que si R5 es F, entonces al menos tres de R3, R4, R6 y R7 deben ser F; y si R4 es metilo o Cl, entonces R7 no puede ser metilo o CI.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41307710P | 2010-11-12 | 2010-11-12 | |
| US201061425034P | 2010-12-20 | 2010-12-20 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR083831A1 true AR083831A1 (es) | 2013-03-27 |
Family
ID=45034191
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110104204A AR083831A1 (es) | 2010-11-12 | 2011-11-10 | Antagonistas del receptor del cgrp de piperidinona carboxamida azaindano |
Country Status (42)
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI522355B (zh) * | 2010-11-12 | 2016-02-21 | 默沙東藥廠 | 六氫吡啶酮甲醯胺氮雜茚滿ｃｇｒｐ受體拮抗劑 |
| EP2685826B1 (en) | 2011-03-18 | 2016-02-03 | Merck Sharp & Dohme Corp. | Piperidinone carboxamide spirohydantoin cgrp receptor antagonists |
| US9487523B2 (en) * | 2012-03-14 | 2016-11-08 | Merck Sharp & Dohme Corp. | Process for making CGRP receptor antagonists |
| US9174989B2 (en) * | 2012-05-09 | 2015-11-03 | Merck Sharp & Dohme Corp. | Process for making CGRP receptor antagonists |
| MX2016003394A (es) * | 2013-09-16 | 2016-10-28 | Merck Sharp & Dohme | Formulaciones para antagonistas del receptor del cgrp. |
| WO2015119848A1 (en) * | 2014-02-05 | 2015-08-13 | Merck Sharp & Dohme Corp. | Tablet formulation for cgrp-active compounds |
| FR3030521B1 (fr) * | 2014-12-23 | 2019-07-26 | Galderma Research & Development | Nouveaux composes heterocycliques et leur utilisation en medecine ainsi qu'en cosmetique |
| GB201707938D0 (en) | 2017-05-17 | 2017-06-28 | Univ Sheffield | Compounds |
| US20190374520A1 (en) * | 2018-06-08 | 2019-12-12 | Allergan Pharmaceuticals International Limited | Treatment of migraine |
| GB201908430D0 (en) * | 2019-06-12 | 2019-07-24 | Heptares Therapeutics Ltd | Cgrp antagonist compounds |
| CN110787163B (zh) * | 2019-12-05 | 2020-06-02 | 河北医科大学第二医院 | 一种用于神经保护和促进神经再生的药物组合物及其制剂 |
| CN112353767A (zh) * | 2020-11-16 | 2021-02-12 | 海南锦瑞制药有限公司 | 一种盐酸地尔硫卓和普瑞巴林组合物及其制备方法及其应用 |
| WO2022140537A1 (en) | 2020-12-22 | 2022-06-30 | Allergan Pharmaceuticals International Limited | Treatment of migraine |
| US20240139171A1 (en) | 2021-03-02 | 2024-05-02 | Cgrp Diagnostics Gmbh | Treatment and/or reduction of occurrence of migraine |
| WO2023026205A1 (en) | 2021-08-24 | 2023-03-02 | Cgrp Diagnostics Gmbh | Preventative treatment of migraine |
| WO2023119327A1 (en) * | 2021-12-20 | 2023-06-29 | Msn Laboratories Private Limited, R&D Center | Process for the preparation of a pure amorphous form of ubrogepant |
| WO2023208124A1 (zh) * | 2022-04-29 | 2023-11-02 | 熙源安健医药（上海）有限公司 | 哌啶甲酰胺氮杂茚满类衍生物及其制备方法和用途 |
| WO2024081718A1 (en) | 2022-10-11 | 2024-04-18 | Allergan Pharmaceuticals International Limited | Cgrp receptor antagonist for the treatment of migraine |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| 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 |
| WO2004087649A2 (en) | 2003-03-14 | 2004-10-14 | Merck & Co., Inc. | Benodiazepine spirohydantoin cgrp receptor antagonists |
| US7288559B2 (en) | 2003-03-14 | 2007-10-30 | Merck + Co, Inc. | Carboxamide spirohydantoin CGRP receptor antagonists |
| JO2355B1 (en) * | 2003-04-15 | 2006-12-12 | ميرك شارب اند دوم كوربوريشن | Hereditary calcitonin polypeptide receptor antagonists |
| US8003792B2 (en) * | 2004-09-13 | 2011-08-23 | Merck Sharp & Dohme Corp. | Bicyclic anilide spirolactam CGRP receptor antagonists |
| US7390798B2 (en) * | 2004-09-13 | 2008-06-24 | Merck & Co., Inc. | Carboxamide spirolactam CGRP receptor antagonists |
| JP2008533147A (ja) * | 2005-03-14 | 2008-08-21 | メルク エンド カムパニー インコーポレーテッド | Ｃｇｒｐ受容体拮抗薬 |
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| TWI522355B (zh) * | 2010-11-12 | 2016-02-21 | 默沙東藥廠 | 六氫吡啶酮甲醯胺氮雜茚滿ｃｇｒｐ受體拮抗劑 |
| EP2637656B1 (en) * | 2010-11-12 | 2016-12-14 | Merck Sharp & Dohme Corp. | N-Piperidinone-indane carboxamides as CGRP receptor antagonists |
| EP2654423B1 (en) * | 2010-12-22 | 2016-12-07 | Merck Sharp & Dohme Corp. | Fused heterocyclic azaindane carboxamide cgrp receptor antagonists |
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| EP2685826B1 (en) * | 2011-03-18 | 2016-02-03 | Merck Sharp & Dohme Corp. | Piperidinone carboxamide spirohydantoin cgrp receptor antagonists |
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| US9487523B2 (en) * | 2012-03-14 | 2016-11-08 | Merck Sharp & Dohme Corp. | Process for making CGRP receptor antagonists |
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| US9174989B2 (en) * | 2012-05-09 | 2015-11-03 | Merck Sharp & Dohme Corp. | Process for making CGRP receptor antagonists |
| MX2016003394A (es) * | 2013-09-16 | 2016-10-28 | Merck Sharp & Dohme | Formulaciones para antagonistas del receptor del cgrp. |
| WO2015119848A1 (en) * | 2014-02-05 | 2015-08-13 | Merck Sharp & Dohme Corp. | Tablet formulation for cgrp-active compounds |
| EP3110427A4 (en) * | 2014-02-24 | 2018-05-30 | Urigen Pharmaceuticals, Inc. | Compositions of pentosan polysulfate salts for oral administration and methods of use |
| US20180092899A1 (en) * | 2016-09-30 | 2018-04-05 | Merck Sharp & Dohme Corp. | Method of treating acute migraine with cgrp-active compound |
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- 2011-11-09 TW TW104104475A patent/TWI522355B/zh active
- 2011-11-09 TW TW100140962A patent/TWI487706B/zh active
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- 2011-11-10 PL PL11787987T patent/PL2638042T3/pl unknown
- 2011-11-10 SG SG2013034145A patent/SG190137A1/en unknown
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- 2011-11-10 WO PCT/US2011/060081 patent/WO2012064910A1/en active Application Filing
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- 2011-11-10 PE PE2013000966A patent/PE20140240A1/es active IP Right Grant
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