BR112014010099A8 - ácido benzóico, derivados de ácidos benzóicos e ácidos carboxílicos heteroarílicos conjugados de hidromorfona, pró-fármacos, métodos de fabricação e uso dos mesmos. - Google Patents
ácido benzóico, derivados de ácidos benzóicos e ácidos carboxílicos heteroarílicos conjugados de hidromorfona, pró-fármacos, métodos de fabricação e uso dos mesmos.Info
- Publication number
- BR112014010099A8 BR112014010099A8 BR112014010099A BR112014010099A BR112014010099A8 BR 112014010099 A8 BR112014010099 A8 BR 112014010099A8 BR 112014010099 A BR112014010099 A BR 112014010099A BR 112014010099 A BR112014010099 A BR 112014010099A BR 112014010099 A8 BR112014010099 A8 BR 112014010099A8
- Authority
- BR
- Brazil
- Prior art keywords
- hydromorphone
- prodrugs
- methods
- acids
- benzoic
- 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
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/485—Morphinan derivatives, e.g. morphine, codeine
-
- 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
- A61K31/60—Salicylic acid; Derivatives thereof
- A61K31/612—Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid
- A61K31/616—Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic acid
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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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0043—Nose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- 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
- A61P11/14—Antitussive agents
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Emergency Medicine (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Molecular Biology (AREA)
- Pain & Pain Management (AREA)
- Addiction (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Physiology (AREA)
- Otolaryngology (AREA)
- Nutrition Science (AREA)
- Dermatology (AREA)
- Psychiatry (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
resumo ácido benzóico, derivados de ácidos benzóicos e ácidos carboxílicos heteroarílicos conjugados de hidromorfona, pró-fármacos, métodos de fabricação e uso dos mesmos a tecnologia presentemente descrita fornece composições que compreendem ácidos carboxílicos arílicos conjugados quimicamente a hidromorfona (4,5-a-epoxi-3-hidroxi-17-metil morfinan-6-ona) para formar novos pró-fármacos/composições de hidromorfona. os pró-fármacos de hidromorfona da presente tecnologia têm efeitos colaterais dominuídos e o potencial para abuso diminuído comparado a hidromorfona não conjugada. a presente tecnologia também fornece métodos de tratar pacientes, kits farmacêuticos e métodos de sintetizar conjugados da presente tecnologia.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201161551600P | 2011-10-26 | 2011-10-26 | |
US201261657201P | 2012-06-08 | 2012-06-08 | |
PCT/US2012/061813 WO2013063204A1 (en) | 2011-10-26 | 2012-10-25 | Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydromorphone, prodrugs, methods of making and use thereof |
Publications (2)
Publication Number | Publication Date |
---|---|
BR112014010099A2 BR112014010099A2 (pt) | 2017-06-27 |
BR112014010099A8 true BR112014010099A8 (pt) | 2018-01-16 |
Family
ID=48168468
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112014010099A BR112014010099A8 (pt) | 2011-10-26 | 2012-10-25 | ácido benzóico, derivados de ácidos benzóicos e ácidos carboxílicos heteroarílicos conjugados de hidromorfona, pró-fármacos, métodos de fabricação e uso dos mesmos. |
Country Status (19)
Country | Link |
---|---|
US (6) | US8816083B2 (pt) |
EP (1) | EP2771002A4 (pt) |
JP (1) | JP5769889B2 (pt) |
KR (1) | KR101589846B1 (pt) |
CN (2) | CN104136031B (pt) |
AR (1) | AR088551A1 (pt) |
AU (1) | AU2012328837B2 (pt) |
BR (1) | BR112014010099A8 (pt) |
CA (1) | CA2856608C (pt) |
CL (1) | CL2014000995A1 (pt) |
CO (1) | CO7010825A2 (pt) |
HK (2) | HK1197191A1 (pt) |
IL (1) | IL231822A0 (pt) |
IN (1) | IN2014DN03009A (pt) |
MX (1) | MX362857B (pt) |
RU (1) | RU2573388C2 (pt) |
SG (1) | SG11201401856VA (pt) |
WO (1) | WO2013063204A1 (pt) |
ZA (1) | ZA201402339B (pt) |
Families Citing this family (19)
Publication number | Priority date | Publication date | Assignee | Title |
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UA102916C2 (uk) | 2009-07-02 | 2013-08-27 | Кемфарм, Інк. | Композиція на основі кон'югату гідрокодону з бензойною кислотою, похідними бензойної кислоти або гетероарилкарбоновою кислотою, проліки, спосіб лікування від зловживань |
US10849981B2 (en) | 2009-07-02 | 2020-12-01 | KemPham, Inc. | Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydrocodone, prodrugs, methods of making and use thereof |
JP5769889B2 (ja) | 2011-10-26 | 2015-08-26 | ケムファーム・インコーポレーテッド | ヒドロモルホンの安息香酸、安息香酸誘導体及びヘテロアリールカルボン酸結合体、そのプロドラッグ、製造法及び使用 |
CN112043835B (zh) * | 2013-12-06 | 2022-10-21 | 韩捷 | 用于含氮和羟基的药物的生物可逆引入基团 |
GB201417529D0 (en) | 2014-10-03 | 2014-11-19 | Isis Innovation | Beta lactamase inhibitors |
CA2967424C (en) | 2014-11-25 | 2023-05-02 | Kempharm, Inc. | Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of oxycodone |
CN106999487A (zh) * | 2014-12-02 | 2017-08-01 | 凯姆制药公司 | 羟吗啡酮的苯甲酸缀合物、苯甲酸衍生物缀合物和杂芳基羧酸缀合物、其前药、制备和使用方法 |
US10017519B2 (en) | 2015-04-27 | 2018-07-10 | 3St Research Llc | Alpha-hydroxy carboxylic acid and derivatives and other GRAS based prodrugs of oxycodone and uses thereof |
US9987269B2 (en) | 2015-04-27 | 2018-06-05 | 3St Research Llc | Alpha-hydroxy carboxylic acid and derivatives and other GRAS-based prodrugs of oxymorphone and uses thereof |
US10449190B2 (en) | 2015-04-27 | 2019-10-22 | John K. Thottathil | Alpha-hydroxy carboxylic acid and derivatives and other GRAS-based prodrugs of opioids and uses thereof |
US10226456B2 (en) | 2015-04-27 | 2019-03-12 | 3St Research Llc | Methods and compositions for preventing opioid abuse |
EP3210630A1 (en) | 2016-02-29 | 2017-08-30 | G.L. Pharma GmbH | Abuse-deterrent pharmaceutical compositions |
EP3231420A1 (en) * | 2016-02-29 | 2017-10-18 | G.L. Pharma GmbH | Abuse-deterrent pharmaceutical compositions |
EP3210596A1 (en) | 2016-02-29 | 2017-08-30 | G.L. Pharma GmbH | Abuse-deterrent pharmaceutical composition |
US20200038383A1 (en) * | 2016-10-14 | 2020-02-06 | Kempharm, Inc. | Immediate-release abuse deterrent compositions or medicaments for treating pain, add, adhd and other syndromes or disorders |
TWI827583B (zh) | 2018-03-08 | 2024-01-01 | 美商英塞特公司 | 作為PI3K-γ抑制劑之胺基吡嗪二醇化合物 |
WO2020010003A1 (en) | 2018-07-02 | 2020-01-09 | Incyte Corporation | AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS |
WO2021097532A1 (en) * | 2019-11-22 | 2021-05-27 | Deakin University | Organic corrosion inhibitors |
WO2021097531A1 (en) * | 2019-11-22 | 2021-05-27 | Deakin University | Polyionic corrosion inhibitors |
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US4668685A (en) * | 1984-07-05 | 1987-05-26 | E.I. Du Pont De Nemours And Company | Substituted benzoate ester prodrug derivatives of 3-hydroxymorphinans, which are analgesics or narcotic antagonists |
US5965161A (en) * | 1994-11-04 | 1999-10-12 | Euro-Celtique, S.A. | Extruded multi-particulates |
BR9607492A (pt) * | 1995-01-16 | 1999-06-29 | Commw Scient Ind Res Org | Conjugados de ácidos graxos de composto terapêutico |
DE19602964A1 (de) * | 1995-12-20 | 1997-07-31 | Nycomed Arzneimittel Gmbh | Neue Morphinderivate, Verfahren zu deren Herstellung und deren Verwendung |
DK1623703T3 (da) | 1999-10-29 | 2011-11-28 | Euro Celtique Sa | Hydrocodonformuleringer med kontrolleret frigivelse |
EP1399161B1 (en) | 2001-06-05 | 2011-04-20 | Control Delivery Systems | Sustained-release analgesic compounds |
US6740641B2 (en) | 2001-07-27 | 2004-05-25 | Euro-Celtique, S.A. | Sugar derivatives of hydromorphone, dihydromorphine and dihydromorphine, compositions thereof and uses for treating or preventing pain |
US7375083B2 (en) | 2003-09-30 | 2008-05-20 | Shire Llc | Pharmaceutical compositions for prevention of overdose or abuse |
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US7661226B2 (en) * | 2005-01-11 | 2010-02-16 | Larson Manufacturing Company | Installation method for a storm door |
CA2648659A1 (en) * | 2006-04-14 | 2007-10-25 | Shire Llc | Compositions and methods for enhancing analgesic potency of covalently bound compounds, attenuating its adverse side effects, and preventing their abuse |
BRPI0712819B8 (pt) | 2006-05-26 | 2021-05-25 | Pharmacofore Inc | composto para liberação controlada de opióides fenólicos, processo para a preparação do referido composto e composição farmacêutica |
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US20090192095A1 (en) | 2008-01-18 | 2009-07-30 | Shire Llc | Amino acid and peptide prodrugs of opioid analgesics with reduced gi side-effects |
AU2010231126A1 (en) | 2009-04-02 | 2011-10-13 | Shire Llc | Novel dicarboxylic acid linked amino acid and peptide prodrugs of opioids and uses thereof |
UA102916C2 (uk) * | 2009-07-02 | 2013-08-27 | Кемфарм, Інк. | Композиція на основі кон'югату гідрокодону з бензойною кислотою, похідними бензойної кислоти або гетероарилкарбоновою кислотою, проліки, спосіб лікування від зловживань |
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WO2011008636A1 (en) * | 2009-07-15 | 2011-01-20 | Mallinckrodt Inc. | 3-oxy-hydromorphone derivatives |
WO2011009015A1 (en) | 2009-07-16 | 2011-01-20 | Mallinckrodt Inc. | (+) - morphinans as antagonists of toll-like receptor 9 and therapeutic uses thereof |
EP2475429B1 (en) | 2009-09-08 | 2015-07-29 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable ketone-modified opioid prodrugs and optional inhibitors thereof |
JP5911484B2 (ja) | 2010-07-16 | 2016-04-27 | マリンクロッド エルエルシー | トール様受容体9のアンタゴニストとしての(+)−モルフィナンおよびその治療的使用 |
US8685916B2 (en) | 2011-03-09 | 2014-04-01 | Signature Therapeutics, Inc. | Opioid prodrugs with heterocyclic linkers |
JP5769889B2 (ja) | 2011-10-26 | 2015-08-26 | ケムファーム・インコーポレーテッド | ヒドロモルホンの安息香酸、安息香酸誘導体及びヘテロアリールカルボン酸結合体、そのプロドラッグ、製造法及び使用 |
-
2012
- 2012-10-25 JP JP2014538982A patent/JP5769889B2/ja not_active Expired - Fee Related
- 2012-10-25 SG SG11201401856VA patent/SG11201401856VA/en unknown
- 2012-10-25 EP EP12843820.7A patent/EP2771002A4/en not_active Withdrawn
- 2012-10-25 RU RU2014121065/04A patent/RU2573388C2/ru not_active IP Right Cessation
- 2012-10-25 CA CA2856608A patent/CA2856608C/en not_active Expired - Fee Related
- 2012-10-25 CN CN201280064641.2A patent/CN104136031B/zh not_active Expired - Fee Related
- 2012-10-25 WO PCT/US2012/061813 patent/WO2013063204A1/en active Application Filing
- 2012-10-25 CN CN201610210323.2A patent/CN105749294A/zh active Pending
- 2012-10-25 IN IN3009DEN2014 patent/IN2014DN03009A/en unknown
- 2012-10-25 KR KR1020147010696A patent/KR101589846B1/ko active IP Right Grant
- 2012-10-25 US US13/660,112 patent/US8816083B2/en active Active
- 2012-10-25 AU AU2012328837A patent/AU2012328837B2/en not_active Ceased
- 2012-10-25 BR BR112014010099A patent/BR112014010099A8/pt not_active Application Discontinuation
- 2012-10-25 MX MX2014004691A patent/MX362857B/es active IP Right Grant
- 2012-10-26 AR ARP120104022A patent/AR088551A1/es unknown
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2014
- 2014-03-28 ZA ZA2014/02339A patent/ZA201402339B/en unknown
- 2014-03-31 IL IL231822A patent/IL231822A0/en unknown
- 2014-04-17 CL CL2014000995A patent/CL2014000995A1/es unknown
- 2014-04-28 CO CO14089601A patent/CO7010825A2/es unknown
- 2014-07-21 US US14/336,549 patent/US9566343B2/en active Active
- 2014-10-28 HK HK14110803A patent/HK1197191A1/xx unknown
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2016
- 2016-10-04 HK HK16111529.9A patent/HK1223279A1/zh unknown
- 2016-12-30 US US15/395,475 patent/US9849185B2/en active Active
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2017
- 2017-11-14 US US15/812,823 patent/US10064956B2/en active Active
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2018
- 2018-08-03 US US16/054,575 patent/US10258696B2/en active Active
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2019
- 2019-03-01 US US16/290,496 patent/US10441661B2/en active Active
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