JP2010095546A5 - - Google Patents
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- Publication number
- JP2010095546A5 JP2010095546A5 JP2010020146A JP2010020146A JP2010095546A5 JP 2010095546 A5 JP2010095546 A5 JP 2010095546A5 JP 2010020146 A JP2010020146 A JP 2010020146A JP 2010020146 A JP2010020146 A JP 2010020146A JP 2010095546 A5 JP2010095546 A5 JP 2010095546A5
- Authority
- JP
- Japan
- Prior art keywords
- acylated
- structural formula
- following structural
- compound represented
- amine group
- 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.)
- Granted
Links
- -1 amine compound Chemical class 0.000 claims 4
- 238000000034 method Methods 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 230000010933 acylation Effects 0.000 claims 1
- 238000005917 acylation reaction Methods 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30581401P | 2001-07-16 | 2001-07-16 | |
| US60/305,814 | 2001-07-16 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003513958A Division JP5038582B2 (ja) | 2001-07-16 | 2002-07-16 | Ｕｄｐ−グルコース：ｎ−アシルスフィンゴシングルコシルトランスフェラーゼインヒビターの合成 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013041198A Division JP2013136618A (ja) | 2001-07-16 | 2013-02-13 | Ｕｄｐ−グルコース：ｎ−アシルスフィンゴシングルコシルトランスフェラーゼインヒビターの合成 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010095546A JP2010095546A (ja) | 2010-04-30 |
| JP2010095546A5 true JP2010095546A5 (enExample) | 2010-12-24 |
| JP5227348B2 JP5227348B2 (ja) | 2013-07-03 |
Family
ID=23182463
Family Applications (6)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003513958A Expired - Lifetime JP5038582B2 (ja) | 2001-07-16 | 2002-07-16 | Ｕｄｐ−グルコース：ｎ−アシルスフィンゴシングルコシルトランスフェラーゼインヒビターの合成 |
| JP2005112378A Expired - Lifetime JP4708073B2 (ja) | 2001-07-16 | 2005-04-08 | Ｕｄｐ−グルコース：ｎ−アシルスフィンゴシングルコシルトランスフェラーゼインヒビターの合成 |
| JP2010020146A Expired - Lifetime JP5227348B2 (ja) | 2001-07-16 | 2010-02-01 | Ｕｄｐ−グルコース：ｎ−アシルスフィンゴシングルコシルトランスフェラーゼインヒビターの合成 |
| JP2013041198A Pending JP2013136618A (ja) | 2001-07-16 | 2013-02-13 | Ｕｄｐ−グルコース：ｎ−アシルスフィンゴシングルコシルトランスフェラーゼインヒビターの合成 |
| JP2015097734A Pending JP2015180656A (ja) | 2001-07-16 | 2015-04-20 | Ｕｄｐ−グルコース：ｎ−アシルスフィンゴシングルコシルトランスフェラーゼインヒビターの合成 |
| JP2016218570A Expired - Lifetime JP6182254B2 (ja) | 2001-07-16 | 2016-11-09 | Ｕｄｐ−グルコース：ｎ−アシルスフィンゴシングルコシルトランスフェラーゼインヒビターの合成 |
Family Applications Before (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003513958A Expired - Lifetime JP5038582B2 (ja) | 2001-07-16 | 2002-07-16 | Ｕｄｐ−グルコース：ｎ−アシルスフィンゴシングルコシルトランスフェラーゼインヒビターの合成 |
| JP2005112378A Expired - Lifetime JP4708073B2 (ja) | 2001-07-16 | 2005-04-08 | Ｕｄｐ−グルコース：ｎ−アシルスフィンゴシングルコシルトランスフェラーゼインヒビターの合成 |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013041198A Pending JP2013136618A (ja) | 2001-07-16 | 2013-02-13 | Ｕｄｐ−グルコース：ｎ−アシルスフィンゴシングルコシルトランスフェラーゼインヒビターの合成 |
| JP2015097734A Pending JP2015180656A (ja) | 2001-07-16 | 2015-04-20 | Ｕｄｐ−グルコース：ｎ−アシルスフィンゴシングルコシルトランスフェラーゼインヒビターの合成 |
| JP2016218570A Expired - Lifetime JP6182254B2 (ja) | 2001-07-16 | 2016-11-09 | Ｕｄｐ−グルコース：ｎ−アシルスフィンゴシングルコシルトランスフェラーゼインヒビターの合成 |
Country Status (15)
| Country | Link |
|---|---|
| US (11) | US6855830B2 (enExample) |
| EP (3) | EP2266968B1 (enExample) |
| JP (6) | JP5038582B2 (enExample) |
| AT (2) | ATE555102T1 (enExample) |
| BE (1) | BE2015C029I2 (enExample) |
| BR (3) | BR122015016313B8 (enExample) |
| CA (1) | CA2453978C (enExample) |
| CY (1) | CY2015028I1 (enExample) |
| DK (3) | DK2067775T3 (enExample) |
| ES (3) | ES2399323T3 (enExample) |
| FR (1) | FR15C0036I2 (enExample) |
| IL (3) | IL159905A0 (enExample) |
| LU (1) | LU92717I2 (enExample) |
| PT (3) | PT2266968E (enExample) |
| WO (1) | WO2003008399A1 (enExample) |
Families Citing this family (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1384719A1 (en) * | 1999-07-09 | 2004-01-28 | The Regents of The University of Michigan | Inhibitors of the glucosyl ceramide synthase enzyme useful for the treatment of cancers, sphingolipidosis and microbial infections |
| MY164523A (en) * | 2000-05-23 | 2017-12-29 | Univ Degli Studi Cagliari | Methods and compositions for treating hepatitis c virus |
| CA2434028C (en) | 2001-01-10 | 2010-11-09 | The Regents Of The University Of Michigan | Amino ceramide-like compounds and therapeutic methods of use |
| US7723296B2 (en) | 2001-01-18 | 2010-05-25 | Genzyme Corporation | Methods for introducing mannose-6-phosphate and other oligosaccharides onto glycoproteins and its application thereof |
| EP2266968B1 (en) | 2001-07-16 | 2013-01-09 | Genzyme Corporation | Synthesis of UDP-glucose: N-acylsphingosine glucosyltransferase inhibitors |
| AU2002348261A1 (en) * | 2001-11-26 | 2003-06-10 | Genzyme Corporation | Diastereoselective synthesis of udp-glucose : n-acylsphingosine glucosyltransferase inhibitors |
| US20060217560A1 (en) * | 2002-04-29 | 2006-09-28 | Shayman James A | Amino ceramide-like compounds and therapeutic methods of use |
| US6916802B2 (en) * | 2002-04-29 | 2005-07-12 | Genzyme Corporation | Amino ceramide-like compounds and therapeutic methods of use |
| JP4195411B2 (ja) * | 2004-04-12 | 2008-12-10 | セイコーエプソン株式会社 | 有機エレクトロルミネッセンス装置の製造方法 |
| CA2586761A1 (en) * | 2004-11-10 | 2006-05-18 | Genzyme Corporation | Methods of treating diabetes mellitus |
| CN101151248B (zh) | 2005-01-26 | 2012-06-20 | 阿勒根公司 | 具有镇痛活性和/或免疫刺激物活性的3-芳基-3-羟基-2-氨基丙酸酰胺类、3-杂芳基-3-羟基-2-氨基丙酸酰胺类以及相关化合物 |
| EP2032134B1 (en) * | 2006-05-09 | 2015-06-24 | Genzyme Corporation | Methods of treating fatty liver disease comprising inhibiting glucosphingolipid synthesis |
| CA2675968C (en) | 2007-01-18 | 2019-05-21 | Genzyme Corporation | Oligosaccharides comprising an aminooxy group and conjugates thereof |
| US8173683B2 (en) | 2007-03-06 | 2012-05-08 | Allergan, Inc. | Methods for treating cognitive disorders |
| US20140179925A1 (en) | 2009-09-04 | 2014-06-26 | Allergan, Inc. | Methods for treating cognitive disorders using 3-aryl-3-hydroxy-2-amino-propionic acid amides, 3-heteroaryl-3-hydroxy-2-amino-propionic acid amides and related compounds |
| PT2481407T (pt) | 2007-03-06 | 2018-12-28 | Allergan Inc | Compostos para utilização no tratamento de distúrbios cognitivos |
| US9314466B2 (en) | 2007-03-06 | 2016-04-19 | Allergan, Inc. | Methods for treating cognitive disorders using 1-benzyl-1-hydroxy-2,3-diamino-propyl amines, 3-benzyl-3-hydroxy-2-amino-propionic acid amides and related compounds |
| US8304447B2 (en) * | 2007-05-31 | 2012-11-06 | Genzyme Corporation | 2-acylaminopropoanol-type glucosylceramide synthase inhibitors |
| KR20160085917A (ko) | 2007-10-05 | 2016-07-18 | 젠자임 코포레이션 | 세라마이드 유도체로 다낭성 신장질환을 치료하는 방법 |
| US8168631B2 (en) | 2008-02-05 | 2012-05-01 | Allergan, Inc. | 3-(4-fluorophenyl)-3-hydroxy-2-amino-propionic acid amides and related compounds having analgesic activity |
| WO2010014554A1 (en) | 2008-07-28 | 2010-02-04 | Genzyme Corporation | Glucosylceramide synthase inhibition for the treatment of collapsing glomerulopathy and other glomerular disease |
| US8309593B2 (en) | 2008-10-03 | 2012-11-13 | Genzyme Corporation | 2-acylaminopropoanol-type glucosylceramide synthase inhibitors |
| SI2889043T1 (sl) | 2008-12-16 | 2019-08-30 | Genzyme Corporation | Sintetične vmesne spojine za pripravo konjugatov oligosaharid-protein |
| PL3133070T3 (pl) | 2009-11-27 | 2020-01-31 | Genzyme Corporation | Eliglustat (Genz 112638) jako inhibitor syntazy glukozyloceramidowej do zastosowania w sposobie leczenia choroby Fabry’ego lub choroby Gauchera, przy czym sposób obejmuje dostosowanie indywidualnej dawki terapeutycznej do metabolizmu P450 u pacjenta |
| JP5467146B2 (ja) | 2010-04-16 | 2014-04-09 | 京セラ株式会社 | 無線通信システム、高電力基地局、低電力基地局、及び通信制御方法 |
| EP2699676A1 (en) | 2011-04-22 | 2014-02-26 | Genzyme Corporation | Modified acid alpha glucosidase with accelerated processing |
| US8961959B2 (en) | 2011-10-17 | 2015-02-24 | The Regents Of The University Of Michigan | Glucosylceramide synthase inhibitors and therapeutic methods using the same |
| WO2014150043A1 (en) | 2013-03-15 | 2014-09-25 | Concert Pharmaceuticals Inc. | Inhibitors of the enzyme udp-glucose: n-acyl-sphingosine glucosyltransferase |
| TWI690511B (zh) | 2013-09-20 | 2020-04-11 | 美商拜奧馬林製藥公司 | 用於治療疾病之葡萄糖苷基腦醯胺（ｇｌｕｃｏｓｙｌｃｅｒａｍｉｄｅ）合成酶抑制劑 |
| WO2015059679A1 (en) * | 2013-10-25 | 2015-04-30 | Dr. Reddy's Laboratories Limited | Improved process for the preparation of eliglustat |
| MX376685B (es) | 2013-10-29 | 2025-03-07 | Biomarin Pharm Inc | Derivados de n-(1-hidroxi-3-(pirrolidinil)propan-2-il)pirrolidin-3-carboxamida como inhibidores de glucosilceramida sintasa. |
| US10202340B2 (en) | 2015-02-02 | 2019-02-12 | The Regents Of The University Of Michigan | Glucosylceramide synthase inhibitors and therapeutic methods using the same |
| CN104557851B (zh) * | 2015-02-10 | 2017-04-05 | 苏州明锐医药科技有限公司 | 依鲁司他的制备方法 |
| WO2016166170A1 (en) | 2015-04-14 | 2016-10-20 | Sandoz Ag | Crystalline eliglustat hydrochloride |
| WO2017068496A1 (en) * | 2015-10-20 | 2017-04-27 | Dr. Reddy' S Laboratories Limited | Improved process for the preparation of eliglustat and its salts |
| CN105646442A (zh) * | 2015-10-27 | 2016-06-08 | 北京凯莱天成医药科技有限公司 | 一种依利格鲁司他的制备方法 |
| WO2017178499A1 (en) | 2016-04-11 | 2017-10-19 | Spedding Research Solutions | Inhibitors of glucosylceramide degradation in the treatment of diseases of the motor units |
| CN106349210A (zh) * | 2016-08-24 | 2017-01-25 | 北京阳光诺和药物研究有限公司 | 一种制备酒石酸艾力骨司坦的方法 |
| CN106967042B (zh) * | 2017-03-21 | 2020-08-14 | 浙江奥翔药业股份有限公司 | 依利格鲁司他的合成方法及其中间体化合物 |
| CN108822072B (zh) * | 2017-04-11 | 2021-01-12 | 中国医学科学院药物研究所 | 一种制备伊力格鲁司他的方法 |
| WO2018193090A2 (en) | 2017-04-21 | 2018-10-25 | Amneal Pharmaceuticals Company Gmbh | Process for preparation of eliglustat hemitartrate and intermediates thereof |
| ZA201803719B (en) | 2017-06-05 | 2019-04-24 | Cipla Ltd | Stable solid dispersions of eliglustat hemitartrate |
| WO2019118707A1 (en) | 2017-12-15 | 2019-06-20 | Genzyme Corporation | Methods for treating gaucher disease |
| US12064414B2 (en) | 2017-12-20 | 2024-08-20 | Aizant Drug Research Solutions Private Limited. | Stable amorphous Eliglustat premix and process for the preparation thereof |
| CN111217791B (zh) * | 2018-11-27 | 2024-02-02 | 广东东阳光药业股份有限公司 | 依鲁司他中间体及其制备方法 |
| EP3941917A4 (en) * | 2019-03-22 | 2022-12-21 | Piramal Pharma Limited | IMPROVED PROCESS FOR THE MANUFACTURE OF ELIGLUSTAT AND ITS INTERMEDIATE |
| WO2020193746A1 (en) | 2019-03-28 | 2020-10-01 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for predicting the survival of patients suffering from melanoma |
| JP7698320B2 (ja) | 2019-10-23 | 2025-06-25 | ザ・リージェンツ・オブ・ザ・ユニバーシティ・オブ・ミシガン | グルコシルセラミドシンターゼ阻害剤およびそれを使用する治療方法 |
| WO2021214771A1 (en) | 2020-04-23 | 2021-10-28 | The Israel Institute of Biological Research (IIBR) | Glucosylceramide synthase inhibitors for prevention and treatment of viral diseases |
| WO2021221953A1 (en) | 2020-04-28 | 2021-11-04 | The Regents Of The University Of Michigan | Pyridine inhibitors of glucosylceramide synthase and therapeutic methods using the same |
| CN116120274A (zh) | 2021-11-12 | 2023-05-16 | 曙方(上海)医药科技有限公司 | 依利格鲁司他可药用盐及其晶型 |
| EP4201403A1 (en) | 2021-12-21 | 2023-06-28 | Som Innovation Biotech, S.L. | Compounds tirapazamine and quazinone for use in the treatment of gm2 gangliosidoses |
| WO2026006099A1 (en) | 2024-06-24 | 2026-01-02 | Genzyme Corporation | Eliglustat for the treatment of gaucher disease |
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| GB8311286D0 (en) | 1983-04-26 | 1983-06-02 | Searle & Co | Carboxyalkyl peptide derivatives |
| DE3522475A1 (de) | 1985-06-22 | 1987-01-02 | Kali Chemie Pharma Gmbh | Neue aromatische verbindungen, ihre herstellung und verwendung |
| JPH0416856A (ja) | 1990-05-10 | 1992-01-21 | Canon Inc | 正帯電性非磁性トナー |
| ZA929008B (en) | 1991-12-13 | 1993-05-21 | Bristol Myers Squibb Co | Piperazinyl- and piperidinyl-cyclohexanols. |
| US5707649A (en) | 1993-08-13 | 1998-01-13 | Seikagaku Corporation | Agent for treating neuronal diseases |
| ATE195944T1 (de) | 1994-02-02 | 2000-09-15 | Liposome Co Inc | Pharmazeutisch wirksame verbindungen und liposome und verfahren zu deren herstellung |
| WO1995034530A1 (en) * | 1994-06-10 | 1995-12-21 | Seikagaku Corporation | 2-acylaminopropanol compound and medicinal composition |
| FR2734819B1 (fr) | 1995-05-31 | 1997-07-04 | Adir | Nouveaux composes de la piperazine, de la piperidine et de la 1,2,5,6-tetrahydropyridine, leur procede de preparation et les compositions pharmaceutiques les contenant |
| US5916911A (en) | 1995-09-20 | 1999-06-29 | The Regents Of The University Of Michigan | Amino ceramide--like compounds and therapeutic methods of use |
| US20030073680A1 (en) | 1995-09-20 | 2003-04-17 | The Regents Of The University Of Michigan | Amino ceramide-like compounds and therapeutic methods of use |
| WO2001004108A1 (en) | 1999-07-09 | 2001-01-18 | Regents Of The University Of Michigan | Amino ceramide-like compounds and therapeutic methods of use |
| US6255336B1 (en) | 1995-09-20 | 2001-07-03 | The Regents Of The University Of Michigan | Amino ceramide-like compounds and therapeutic methods of use |
| NO965193L (no) | 1995-12-08 | 1997-06-09 | Seikagaku Kogyo Kk Seikagaku C | Aminalkoholderivat og fremgangsmåte for fremstilling derav |
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| JP4176170B2 (ja) | 1997-06-06 | 2008-11-05 | 生化学工業株式会社 | アミノアルコール誘導体を含む医薬及び異常増殖性疾患治療薬 |
| ES2285852T3 (es) | 1998-07-27 | 2007-11-16 | Johns Hopkins University | Compuestos de diamino-propanol para el tratamiento de la isquemia. |
| EP1384719A1 (en) | 1999-07-09 | 2004-01-28 | The Regents of The University of Michigan | Inhibitors of the glucosyl ceramide synthase enzyme useful for the treatment of cancers, sphingolipidosis and microbial infections |
| CA2434028C (en) | 2001-01-10 | 2010-11-09 | The Regents Of The University Of Michigan | Amino ceramide-like compounds and therapeutic methods of use |
| US20040260099A1 (en) | 2001-01-10 | 2004-12-23 | The Regents Of The University Of Michigan | Amino ceramide-like compounds and therapeutic methods of use |
| US7148251B2 (en) | 2001-01-10 | 2006-12-12 | The Regents Of The University Of Michigan | Amino ceramide-like compounds and therapeutic methods of use |
| US20020198240A1 (en) | 2001-01-10 | 2002-12-26 | Shayman James A. | Amino ceramide - like compounds and therapeutic methods of use |
| EP2266968B1 (en) * | 2001-07-16 | 2013-01-09 | Genzyme Corporation | Synthesis of UDP-glucose: N-acylsphingosine glucosyltransferase inhibitors |
| US6916802B2 (en) | 2002-04-29 | 2005-07-12 | Genzyme Corporation | Amino ceramide-like compounds and therapeutic methods of use |
| US20060217560A1 (en) | 2002-04-29 | 2006-09-28 | Shayman James A | Amino ceramide-like compounds and therapeutic methods of use |
| EP2032134B1 (en) * | 2006-05-09 | 2015-06-24 | Genzyme Corporation | Methods of treating fatty liver disease comprising inhibiting glucosphingolipid synthesis |
-
2002
- 2002-07-16 EP EP10075429A patent/EP2266968B1/en not_active Expired - Lifetime
- 2002-07-16 WO PCT/US2002/022659 patent/WO2003008399A1/en not_active Ceased
- 2002-07-16 JP JP2003513958A patent/JP5038582B2/ja not_active Expired - Lifetime
- 2002-07-16 BR BR122015016313A patent/BR122015016313B8/pt not_active IP Right Cessation
- 2002-07-16 PT PT100754290T patent/PT2266968E/pt unknown
- 2002-07-16 BR BRPI0211379-1 patent/BRPI0211379B8/pt active IP Right Grant
- 2002-07-16 IL IL15990502A patent/IL159905A0/xx unknown
- 2002-07-16 ES ES10075429T patent/ES2399323T3/es not_active Expired - Lifetime
- 2002-07-16 US US10/197,227 patent/US6855830B2/en not_active Expired - Lifetime
- 2002-07-16 EP EP09003291A patent/EP2067775B1/en not_active Expired - Lifetime
- 2002-07-16 AT AT09003291T patent/ATE555102T1/de active
- 2002-07-16 CA CA2453978A patent/CA2453978C/en not_active Expired - Lifetime
- 2002-07-16 AT AT02750099T patent/ATE554082T1/de active
- 2002-07-16 EP EP02750099A patent/EP1409467B1/en not_active Expired - Lifetime
- 2002-07-16 BR BR122015016314A patent/BR122015016314B8/pt not_active IP Right Cessation
- 2002-07-16 PT PT02750099T patent/PT1409467E/pt unknown
- 2002-07-16 DK DK09003291.3T patent/DK2067775T3/da active
- 2002-07-16 ES ES02750099T patent/ES2395122T3/es not_active Expired - Lifetime
- 2002-07-16 ES ES09003291T patent/ES2395463T3/es not_active Expired - Lifetime
- 2002-07-16 DK DK02750099.0T patent/DK1409467T3/da active
- 2002-07-16 DK DK10075429.0T patent/DK2266968T3/da active
- 2002-07-16 PT PT09003291T patent/PT2067775E/pt unknown
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2004
- 2004-01-16 IL IL159905A patent/IL159905A/en active Protection Beyond IP Right Term
- 2004-08-12 US US10/916,824 patent/US7265228B2/en not_active Expired - Lifetime
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2005
- 2005-03-28 US US11/091,836 patent/US7196205B2/en active Active
- 2005-04-08 JP JP2005112378A patent/JP4708073B2/ja not_active Expired - Lifetime
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2007
- 2007-02-05 US US11/702,425 patent/US7615573B2/en not_active Expired - Lifetime
- 2007-08-24 US US11/895,632 patent/US7763738B2/en not_active Expired - Lifetime
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2008
- 2008-08-05 IL IL193244A patent/IL193244A0/en unknown
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2010
- 2010-02-01 JP JP2010020146A patent/JP5227348B2/ja not_active Expired - Lifetime
- 2010-07-06 US US12/830,962 patent/US8138353B2/en not_active Expired - Fee Related
-
2012
- 2012-03-14 US US13/420,108 patent/US8779163B2/en not_active Expired - Lifetime
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2013
- 2013-02-13 JP JP2013041198A patent/JP2013136618A/ja active Pending
-
2014
- 2014-06-26 US US14/315,453 patent/US9546161B2/en not_active Expired - Fee Related
-
2015
- 2015-04-20 JP JP2015097734A patent/JP2015180656A/ja active Pending
- 2015-05-12 BE BE2015C029C patent/BE2015C029I2/fr unknown
- 2015-05-13 LU LU92717C patent/LU92717I2/xx unknown
- 2015-05-13 FR FR15C0036C patent/FR15C0036I2/fr active Active
- 2015-07-08 CY CY2015028C patent/CY2015028I1/el unknown
-
2016
- 2016-11-09 JP JP2016218570A patent/JP6182254B2/ja not_active Expired - Lifetime
- 2016-12-30 US US15/395,329 patent/US20170334888A1/en not_active Abandoned
-
2018
- 2018-11-21 US US16/198,258 patent/US20190322649A1/en not_active Abandoned
-
2020
- 2020-07-23 US US16/937,437 patent/US20210171507A1/en not_active Abandoned