ES2519446T3 - Proceso para la preparación de ácido 4-amino-butírico sustituido con biarilo o derivados del mismo y su uso en la producción de inhibidores de NEP - Google Patents
Proceso para la preparación de ácido 4-amino-butírico sustituido con biarilo o derivados del mismo y su uso en la producción de inhibidores de NEP Download PDFInfo
- Publication number
- ES2519446T3 ES2519446T3 ES07818108.8T ES07818108T ES2519446T3 ES 2519446 T3 ES2519446 T3 ES 2519446T3 ES 07818108 T ES07818108 T ES 07818108T ES 2519446 T3 ES2519446 T3 ES 2519446T3
- Authority
- ES
- Spain
- Prior art keywords
- biaryl
- derivatives
- amino
- preparation
- production
- 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.)
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C227/30—Preparation of optical isomers
- C07C227/32—Preparation of optical isomers by stereospecific synthesis
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C269/00—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C269/06—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups by reactions not involving the formation of carbamate groups
-
- 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
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
- B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
- B01J31/00—Catalysts comprising hydrides, coordination complexes or organic compounds
- B01J31/16—Catalysts comprising hydrides, coordination complexes or organic compounds containing coordination complexes
- B01J31/22—Organic complexes
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C227/14—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof
- C07C227/16—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof by reactions not involving the amino or carboxyl groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C229/34—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C271/06—Esters of carbamic acids
- C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
- C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Hematology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Obesity (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Inorganic Chemistry (AREA)
- Materials Engineering (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Catalysts (AREA)
- Enzymes And Modification Thereof (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Un proceso para producir un compuesto de acuerdo con la fórmula (I) o una sal del mismo, en donde R1 y R1` son independientemente hidrógeno o un grupo protector amina, y R2 es un grupo carboxilo o un grupo éster, que comprende hacer reaccionar un compuesto de acuerdo con la fórmula (ii), o una sal del mismo, en donde R1, R1' y R2 son como se definieron anteriormente, con hidrógeno en presencia de un catalizador de metal de transición y un ligando quiral, en donde el metal de transición se selecciona del grupo 7, 8 o 9 de la tabla periódica.
Description
Claims (1)
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imagen1 imagen2 imagen3 imagen4 imagen5
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP06120576 | 2006-09-13 | ||
EP06120576A EP1903027A1 (en) | 2006-09-13 | 2006-09-13 | Process for preparing biaryl substituted 4-amino-butyric acid or derivatives thereof and their use in the production of NEP inhibitors |
PCT/EP2007/007913 WO2008031567A1 (en) | 2006-09-13 | 2007-09-11 | Process for preparing biaryl substituted 4-amino-butyric acid or derivatives thereof and their use in the production of nep inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
ES2519446T3 true ES2519446T3 (es) | 2014-11-07 |
Family
ID=37814152
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ES07818108.8T Active ES2519446T3 (es) | 2006-09-13 | 2007-09-11 | Proceso para la preparación de ácido 4-amino-butírico sustituido con biarilo o derivados del mismo y su uso en la producción de inhibidores de NEP |
Country Status (29)
Country | Link |
---|---|
US (2) | US20090326066A1 (es) |
EP (2) | EP1903027A1 (es) |
JP (1) | JP5455627B2 (es) |
KR (1) | KR101401118B1 (es) |
CN (1) | CN101516831B (es) |
AU (1) | AU2007296889B2 (es) |
BR (1) | BRPI0716990A2 (es) |
CA (1) | CA2662393C (es) |
CO (1) | CO6190550A2 (es) |
CY (1) | CY1115696T1 (es) |
DK (1) | DK2066618T3 (es) |
ES (1) | ES2519446T3 (es) |
GT (1) | GT200900058A (es) |
HK (1) | HK1131381A1 (es) |
HR (1) | HRP20140984T1 (es) |
IL (1) | IL196925A (es) |
MA (1) | MA30724B1 (es) |
MX (1) | MX2009002746A (es) |
MY (1) | MY146660A (es) |
NO (1) | NO341967B1 (es) |
NZ (1) | NZ574665A (es) |
PL (1) | PL2066618T3 (es) |
PT (1) | PT2066618E (es) |
RU (1) | RU2469019C2 (es) |
SG (1) | SG177205A1 (es) |
SI (1) | SI2066618T1 (es) |
TN (1) | TN2009000077A1 (es) |
WO (1) | WO2008031567A1 (es) |
ZA (1) | ZA200900779B (es) |
Families Citing this family (63)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DK2121578T3 (en) | 2007-01-12 | 2016-12-05 | Novartis Ag | A process for the preparation of 4-biphenyl-4-amino-2-methylpentanoic acid |
PE20091364A1 (es) | 2008-01-17 | 2009-10-13 | Novartis Ag | Proceso para la preparacion de inhibidores de nep |
ES2523734T3 (es) | 2009-05-28 | 2014-12-01 | Novartis Ag | Derivados aminopropiónicos sustituidos como inhibidores de neprilisina |
AR076706A1 (es) | 2009-05-28 | 2011-06-29 | Novartis Ag | Derivados aminobutiricos sustituidos como inhibidores de neprilisina |
JO2967B1 (en) | 2009-11-20 | 2016-03-15 | نوفارتس ايه جي | Acetic acid derivatives of carbamoyl methyl amino are substituted as new NEP inhibitors |
PL2526088T3 (pl) * | 2010-01-22 | 2016-01-29 | Novartis Ag | Produkty pośrednie inhibitorów obojętnej endopeptydazy oraz sposób ich wytwarzania |
AU2011295170B2 (en) * | 2010-08-23 | 2014-12-18 | Novartis Ag | Process for the preparation of intermediates for the manufacture of NEP inhibitors |
SI2609071T1 (sl) * | 2010-08-23 | 2017-01-31 | Novartis Ag | Novi postopek za pripravo intermediatov, uporabnih za izdelavo NEP inhibitorjev |
CN103080077B (zh) * | 2010-08-23 | 2015-06-10 | 诺华股份有限公司 | 用于制造nep抑制剂的中间体的制备工艺 |
US8993631B2 (en) | 2010-11-16 | 2015-03-31 | Novartis Ag | Method of treating contrast-induced nephropathy |
US8673974B2 (en) | 2010-11-16 | 2014-03-18 | Novartis Ag | Substituted amino bisphenyl pentanoic acid derivatives as NEP inhibitors |
AR092278A1 (es) * | 2012-08-31 | 2015-04-08 | Novartis Ag | Proceso de obtencion de derivados n-acilicos de bifenil-alanina e intermediarios relacionados |
US9102635B2 (en) | 2013-02-14 | 2015-08-11 | Novartis Ag | Substituted bisphenyl butanoic acid derivatives as NEP inhibitors with improved in vivo efficacy |
PE20151666A1 (es) | 2013-02-14 | 2015-11-19 | Novartis Ag | Derivados sustituidos del acido bisfenil butanoico fosfonico como inhibidores de la nep |
CN104230865B (zh) * | 2013-06-13 | 2018-01-09 | 上海翰森生物医药科技有限公司 | 联芳基取代的4‑氨基丁酸衍生物及其制备方法和用途 |
JP2016528271A (ja) * | 2013-08-21 | 2016-09-15 | ディーピーエックス ホールディングス ビー.ブイ. | □新規な中間体を経由するビフェニルアラニノールの合成 |
CN105461587A (zh) * | 2014-08-27 | 2016-04-06 | 上海翰森生物医药科技有限公司 | Ahu-377半钙盐晶型及其制备方法和应用 |
CN106458857A (zh) * | 2014-08-27 | 2017-02-22 | 上海翰森生物医药科技有限公司 | AHU‑377结晶型游离酸、半钙盐、α﹣苯乙胺盐及其制备方法和应用 |
WO2016037098A1 (en) | 2014-09-04 | 2016-03-10 | Concert Pharmaceuticals, Inc. | Deuterated sacubitril |
PT3218351T (pt) | 2014-11-14 | 2019-09-26 | Zentiva Ks | Um método para a preparação, isolamento e purificação de formas farmaceuticamente aplicáveis de ahu-377 |
CN104557600B (zh) * | 2015-01-26 | 2016-05-04 | 苏州明锐医药科技有限公司 | 沙库比曲的制备方法 |
TW201632493A (zh) | 2015-02-13 | 2016-09-16 | 諾華公司 | 新穎方法 |
CN105884644B (zh) * | 2015-02-15 | 2020-06-09 | 深圳信立泰药业股份有限公司 | 一种中性内肽酶抑制剂盐优势形态及其制备方法 |
CN106146351B (zh) * | 2015-04-03 | 2020-09-11 | 博瑞生物医药(苏州)股份有限公司 | 制备联芳基取代的4-氨基-丁酸或其衍生物的方法 |
CN106065006B (zh) * | 2015-04-22 | 2020-06-05 | 深圳信立泰药业股份有限公司 | 一种中性内肽酶抑制剂盐晶型及其制备方法 |
CN106187808A (zh) * | 2015-05-08 | 2016-12-07 | 苏州鹏旭医药科技有限公司 | Ahu-377的制备方法、ahu-377中间体及ahu-377中间体的制备方法 |
CN104860894B (zh) * | 2015-06-10 | 2017-05-17 | 北京博全健医药科技有限公司 | 一种抗心衰药lcz696的制备方法 |
CN107980038B (zh) | 2015-07-02 | 2021-04-27 | 诺华股份有限公司 | 沙库巴曲钙盐 |
WO2017009784A1 (en) | 2015-07-14 | 2017-01-19 | Cadila Healthcare Limited | Solid state forms of trisodium salt of valsartan/sacubitril complex and sacubitril |
CN105061263B (zh) * | 2015-08-11 | 2017-03-15 | 苏州楚凯药业有限公司 | 一种nep抑制剂中间体的制备方法 |
CN105085322B (zh) * | 2015-08-15 | 2017-10-03 | 浙江永宁药业股份有限公司 | Ahu‑377中间体的制备方法及其中间体和中间体的制备方法 |
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WO2017033128A1 (en) * | 2015-08-25 | 2017-03-02 | Novartis Ag | Biphenyl-substitued 4-amino-butyric acid derivatives and their use in the synthesis of nep inhibitors |
CN105152980B (zh) * | 2015-09-11 | 2017-03-29 | 浙江永宁药业股份有限公司 | N‑叔丁氧羰基‑(4s)‑(对苯基苯基甲基)‑4‑氨基‑(2r)‑甲基丁酸的手性制备方法 |
WO2017051326A1 (en) | 2015-09-23 | 2017-03-30 | Novartis Ag | New processes and intermediates useful in synthesis of nep inhibitors |
CN105348209B (zh) | 2015-12-09 | 2017-12-26 | 浙江天宇药业股份有限公司 | 一种抗心衰药lcz696的制备方法 |
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EP3386955B1 (en) | 2015-12-10 | 2020-08-05 | Novartis AG | Intermediates for the preparation of sacubitril and their preparation |
BR112018011788A2 (pt) | 2015-12-11 | 2018-12-04 | Zentiva Ks | formas sólidas de éster etílico de ácido (2r,4s)-5-(bifenil-4-il)-4-[(3-carboxipropionil)amino]-2-metil-pentanoico, seus sais e um método de preparação |
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WO2017141193A1 (en) * | 2016-02-16 | 2017-08-24 | Sun Pharmaceutical Industries Limited | Process for the preparation of sacubitril or salts thereof |
CN105924355B (zh) * | 2016-05-11 | 2018-08-17 | 浙江宏元药业有限公司 | 沙库比曲中间体及沙库比曲中间体和沙库比曲的制备方法 |
CN109415308B (zh) | 2016-07-05 | 2022-09-06 | 诺华股份有限公司 | 用于早期沙卡布曲中间体的新方法 |
WO2018033866A1 (en) | 2016-08-17 | 2018-02-22 | Novartis Ag | New processes and intermediates for nep inhibitor synthesis |
CN106380421B (zh) * | 2016-08-26 | 2017-12-08 | 中国科学院上海有机化学研究所 | 沙库必曲的合成方法 |
EP3522886A4 (en) | 2016-10-10 | 2020-02-19 | Laurus Labs Limited | STABLE AMORPHE FORM OF THE SACUBITRIL VALSARTAN TRINATRIUM COMPLEX AND METHOD FOR THE PRODUCTION THEREOF |
CN106631903A (zh) * | 2016-12-16 | 2017-05-10 | 重庆市碚圣医药科技股份有限公司 | 一种lcz‑696关键中间体的制备方法 |
ES2883363T3 (es) * | 2016-12-23 | 2021-12-07 | Novartis Ag | Proceso nuevo para intermedios iniciales de sacubitrilo |
CN107011203B (zh) * | 2017-04-28 | 2019-03-29 | 江苏阿尔法药业有限公司 | 一种lcz696中间体ahu-377的制备方法 |
CN107522628A (zh) * | 2017-09-20 | 2017-12-29 | 吉尔生化(上海)有限公司 | 一种l‑3‑(6‑乙酰基‑2‑萘胺基)‑2‑氨基丙酸的合成方法 |
CN108084058A (zh) * | 2017-12-15 | 2018-05-29 | 江苏中邦制药有限公司 | 一种lcz696中间体的制备方法 |
CN108373423B (zh) * | 2018-04-28 | 2020-10-23 | 成都苑东生物制药股份有限公司 | 一种沙库比曲缬沙坦复合物和/或共晶关键中间体沙库比曲钙的制备方法 |
CN109400504A (zh) * | 2018-12-11 | 2019-03-01 | 重庆三圣实业股份有限公司 | Lcz696中间体非对映异构体的分离纯化方法 |
CN109503404A (zh) * | 2018-12-28 | 2019-03-22 | 凯瑞斯德生化(苏州)有限公司 | 一种lcz-696关键中间体的制备方法 |
CN111748590B (zh) * | 2019-03-29 | 2024-05-28 | 弈柯莱(台州)药业有限公司 | 转氨酶在制备Sacubitril中间体中的应用 |
CN110128298B (zh) * | 2019-06-13 | 2021-08-03 | 南京一心和医药科技有限公司 | 一种沙库巴曲中间体的合成方法 |
CN112574132B (zh) * | 2019-09-30 | 2024-02-27 | 广东东阳光药业股份有限公司 | 一种沙库必曲缬沙坦钠的制备方法 |
CN113135836A (zh) * | 2020-01-20 | 2021-07-20 | 鲁南制药集团股份有限公司 | 一种沙库巴曲钙盐的制备方法 |
CN113321600B (zh) * | 2020-02-28 | 2024-06-14 | 四川科伦药物研究院有限公司 | 制备手性联芳基取代的4-氨基-丁酸及其衍生物的方法 |
CN113387841A (zh) * | 2020-03-13 | 2021-09-14 | 凯特立斯(深圳)科技有限公司 | 一种沙库必曲中间体的合成方法 |
CN111269148B (zh) * | 2020-04-08 | 2022-02-08 | 台州职业技术学院 | 一种沙库比曲中间体的制备方法 |
JP7064527B2 (ja) * | 2020-05-01 | 2022-05-10 | ノバルティス アーゲー | サクビトリルカルシウム塩 |
CN112745246A (zh) * | 2020-12-30 | 2021-05-04 | 重庆市碚圣医药科技股份有限公司 | 一种沙库必曲中间体的纯化方法 |
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-
2006
- 2006-09-13 EP EP06120576A patent/EP1903027A1/en not_active Ceased
-
2007
- 2007-09-11 PT PT78181088T patent/PT2066618E/pt unknown
- 2007-09-11 SG SG2011091998A patent/SG177205A1/en unknown
- 2007-09-11 SI SI200731518T patent/SI2066618T1/sl unknown
- 2007-09-11 AU AU2007296889A patent/AU2007296889B2/en active Active
- 2007-09-11 JP JP2009527735A patent/JP5455627B2/ja active Active
- 2007-09-11 KR KR1020097007380A patent/KR101401118B1/ko active IP Right Grant
- 2007-09-11 CN CN2007800341413A patent/CN101516831B/zh active Active
- 2007-09-11 BR BRPI0716990-6A2A patent/BRPI0716990A2/pt not_active Application Discontinuation
- 2007-09-11 RU RU2009113666/04A patent/RU2469019C2/ru active
- 2007-09-11 DK DK07818108.8T patent/DK2066618T3/da active
- 2007-09-11 CA CA2662393A patent/CA2662393C/en active Active
- 2007-09-11 US US12/438,798 patent/US20090326066A1/en not_active Abandoned
- 2007-09-11 MX MX2009002746A patent/MX2009002746A/es active IP Right Grant
- 2007-09-11 MY MYPI20090644A patent/MY146660A/en unknown
- 2007-09-11 EP EP07818108.8A patent/EP2066618B1/en active Active
- 2007-09-11 WO PCT/EP2007/007913 patent/WO2008031567A1/en active Application Filing
- 2007-09-11 ES ES07818108.8T patent/ES2519446T3/es active Active
- 2007-09-11 PL PL07818108T patent/PL2066618T3/pl unknown
- 2007-09-11 NZ NZ574665A patent/NZ574665A/en not_active IP Right Cessation
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2009
- 2009-02-02 ZA ZA2009/00779A patent/ZA200900779B/en unknown
- 2009-02-05 IL IL196925A patent/IL196925A/en active IP Right Grant
- 2009-03-06 TN TN2009000077A patent/TN2009000077A1/fr unknown
- 2009-03-12 GT GT200900058A patent/GT200900058A/es unknown
- 2009-03-25 NO NO20091242A patent/NO341967B1/no unknown
- 2009-03-30 MA MA31739A patent/MA30724B1/fr unknown
- 2009-04-07 CO CO09035919A patent/CO6190550A2/es not_active Application Discontinuation
- 2009-12-03 HK HK09111344.1A patent/HK1131381A1/xx unknown
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2012
- 2012-10-26 US US13/661,991 patent/US8946481B2/en active Active
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2014
- 2014-10-14 HR HRP20140984TT patent/HRP20140984T1/hr unknown
- 2014-10-15 CY CY20141100841T patent/CY1115696T1/el unknown
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