JP2013510874A5 - - Google Patents
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- Publication number
- JP2013510874A5 JP2013510874A5 JP2012539022A JP2012539022A JP2013510874A5 JP 2013510874 A5 JP2013510874 A5 JP 2013510874A5 JP 2012539022 A JP2012539022 A JP 2012539022A JP 2012539022 A JP2012539022 A JP 2012539022A JP 2013510874 A5 JP2013510874 A5 JP 2013510874A5
- Authority
- JP
- Japan
- Prior art keywords
- crystalline form
- item
- amino
- pentanamide
- methyl
- 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
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- 150000003839 salts Chemical class 0.000 claims description 20
- YNMUTYLWSRFTPX-UHFFFAOYSA-N 2-amino-3-methyl-n-(2-morpholin-4-ylethyl)pentanamide Chemical compound CCC(C)C(N)C(=O)NCCN1CCOCC1 YNMUTYLWSRFTPX-UHFFFAOYSA-N 0.000 claims description 10
- 150000001875 compounds Chemical class 0.000 claims description 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 7
- 208000035475 disorder Diseases 0.000 claims description 7
- 239000000203 mixture Substances 0.000 claims description 5
- 239000008194 pharmaceutical composition Substances 0.000 claims description 5
- YNMUTYLWSRFTPX-QWRGUYRKSA-N (2s,3s)-2-amino-3-methyl-n-(2-morpholin-4-ylethyl)pentanamide Chemical compound CC[C@H](C)[C@H](N)C(=O)NCCN1CCOCC1 YNMUTYLWSRFTPX-QWRGUYRKSA-N 0.000 claims description 4
- 239000012453 solvate Substances 0.000 claims description 4
- 230000007850 degeneration Effects 0.000 claims description 3
- 230000004064 dysfunction Effects 0.000 claims description 3
- YNMUTYLWSRFTPX-GHMZBOCLSA-N (2r,3r)-2-amino-3-methyl-n-(2-morpholin-4-ylethyl)pentanamide Chemical compound CC[C@@H](C)[C@@H](N)C(=O)NCCN1CCOCC1 YNMUTYLWSRFTPX-GHMZBOCLSA-N 0.000 claims description 2
- YNMUTYLWSRFTPX-WDEREUQCSA-N (2r,3s)-2-amino-3-methyl-n-(2-morpholin-4-ylethyl)pentanamide Chemical compound CC[C@H](C)[C@@H](N)C(=O)NCCN1CCOCC1 YNMUTYLWSRFTPX-WDEREUQCSA-N 0.000 claims description 2
- BJCHOJPLNYNFIE-UHFFFAOYSA-N 2-amino-3-methyl-n-(2-morpholin-4-ylethyl)pentanamide;4-methylbenzenesulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1.CC1=CC=C(S(O)(=O)=O)C=C1.CCC(C)C(N)C(=O)NCCN1CCOCC1 BJCHOJPLNYNFIE-UHFFFAOYSA-N 0.000 claims description 2
- ZDIIDLMSRMAYJH-UHFFFAOYSA-N 2-amino-3-methyl-n-(2-morpholin-4-ylethyl)pentanamide;methanesulfonic acid Chemical compound CS(O)(=O)=O.CS(O)(=O)=O.CCC(C)C(N)C(=O)NCCN1CCOCC1 ZDIIDLMSRMAYJH-UHFFFAOYSA-N 0.000 claims description 2
- FWJCDHHQMRIOHC-UHFFFAOYSA-N 2-amino-3-methyl-n-(2-morpholin-4-ylethyl)pentanamide;oxalic acid Chemical compound OC(=O)C(O)=O.CCC(C)C(N)C(=O)NCCN1CCOCC1 FWJCDHHQMRIOHC-UHFFFAOYSA-N 0.000 claims description 2
- FWEGNVRQTFWHQF-UHFFFAOYSA-N 2-amino-3-methyl-n-(2-morpholin-4-ylethyl)pentanamide;sulfo hydrogen sulfate Chemical compound OS(=O)(=O)OS(O)(=O)=O.CCC(C)C(N)C(=O)NCCN1CCOCC1 FWEGNVRQTFWHQF-UHFFFAOYSA-N 0.000 claims description 2
- YCHHIZJKPWVFDT-UHFFFAOYSA-N 2-amino-3-methyl-n-(2-morpholin-4-ylethyl)pentanamide;sulfuric acid Chemical compound OS(O)(=O)=O.CCC(C)C(N)C(=O)NCCN1CCOCC1 YCHHIZJKPWVFDT-UHFFFAOYSA-N 0.000 claims description 2
- 201000004384 Alopecia Diseases 0.000 claims description 2
- 208000024827 Alzheimer disease Diseases 0.000 claims description 2
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims description 2
- 201000011240 Frontotemporal dementia Diseases 0.000 claims description 2
- 208000023105 Huntington disease Diseases 0.000 claims description 2
- 206010021143 Hypoxia Diseases 0.000 claims description 2
- MSWZJZLWBDBWQL-UUPCJSQJSA-N OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O.OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O.CCC(C)C(N)C(=O)NCCN1CCOCC1 Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O.OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O.CCC(C)C(N)C(=O)NCCN1CCOCC1 MSWZJZLWBDBWQL-UUPCJSQJSA-N 0.000 claims description 2
- 208000018737 Parkinson disease Diseases 0.000 claims description 2
- 208000010886 Peripheral nerve injury Diseases 0.000 claims description 2
- 208000000609 Pick Disease of the Brain Diseases 0.000 claims description 2
- 229920001273 Polyhydroxy acid Polymers 0.000 claims description 2
- 208000006011 Stroke Diseases 0.000 claims description 2
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims description 2
- 208000029028 brain injury Diseases 0.000 claims description 2
- 150000001732 carboxylic acid derivatives Chemical group 0.000 claims description 2
- 206010015037 epilepsy Diseases 0.000 claims description 2
- 208000024963 hair loss Diseases 0.000 claims description 2
- 230000003676 hair loss Effects 0.000 claims description 2
- 230000007954 hypoxia Effects 0.000 claims description 2
- 208000028867 ischemia Diseases 0.000 claims description 2
- 201000006417 multiple sclerosis Diseases 0.000 claims description 2
- 210000005036 nerve Anatomy 0.000 claims description 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 2
- 208000033808 peripheral neuropathy Diseases 0.000 claims description 2
- 208000020431 spinal cord injury Diseases 0.000 claims description 2
- QAOWNCQODCNURD-UHFFFAOYSA-L sulfate group Chemical group S(=O)(=O)([O-])[O-] QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims description 2
- 125000000542 sulfonic acid group Chemical group 0.000 claims description 2
- 238000002054 transplantation Methods 0.000 claims description 2
- 238000001237 Raman spectrum Methods 0.000 description 18
- 238000000634 powder X-ray diffraction Methods 0.000 description 18
- 238000000113 differential scanning calorimetry Methods 0.000 description 9
- 238000001757 thermogravimetry curve Methods 0.000 description 9
- 238000000034 method Methods 0.000 description 5
- 239000013078 crystal Substances 0.000 description 3
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US26067109P | 2009-11-12 | 2009-11-12 | |
| US61/260,671 | 2009-11-12 | ||
| US29427910P | 2010-01-12 | 2010-01-12 | |
| US61/294,279 | 2010-01-12 | ||
| US35079710P | 2010-06-02 | 2010-06-02 | |
| US61/350,797 | 2010-06-02 | ||
| PCT/US2010/056537 WO2011060262A1 (en) | 2009-11-12 | 2010-11-12 | Crystalline forms of neurotrophin mimetic compounds and their salts |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015200793A Division JP2016020380A (ja) | 2009-11-12 | 2015-10-09 | ニューロトロフィン模倣化合物およびこれらの塩の結晶形態 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013510874A JP2013510874A (ja) | 2013-03-28 |
| JP2013510874A5 true JP2013510874A5 (enExample) | 2013-12-19 |
| JP5863663B2 JP5863663B2 (ja) | 2016-02-16 |
Family
ID=43992064
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012539022A Active JP5863663B2 (ja) | 2009-11-12 | 2010-11-12 | ニューロトロフィン模倣化合物およびこれらの塩の結晶形態 |
| JP2015200793A Pending JP2016020380A (ja) | 2009-11-12 | 2015-10-09 | ニューロトロフィン模倣化合物およびこれらの塩の結晶形態 |
| JP2018089165A Active JP6657294B2 (ja) | 2009-11-12 | 2018-05-07 | ニューロトロフィン模倣化合物およびこれらの塩の結晶形態 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015200793A Pending JP2016020380A (ja) | 2009-11-12 | 2015-10-09 | ニューロトロフィン模倣化合物およびこれらの塩の結晶形態 |
| JP2018089165A Active JP6657294B2 (ja) | 2009-11-12 | 2018-05-07 | ニューロトロフィン模倣化合物およびこれらの塩の結晶形態 |
Country Status (9)
| Country | Link |
|---|---|
| US (3) | US9271986B2 (enExample) |
| EP (2) | EP3470402B1 (enExample) |
| JP (3) | JP5863663B2 (enExample) |
| CN (3) | CN104761515B (enExample) |
| AU (1) | AU2010319349B2 (enExample) |
| CA (2) | CA2780940C (enExample) |
| ES (1) | ES2712752T3 (enExample) |
| IN (1) | IN2012DN05142A (enExample) |
| WO (1) | WO2011060262A1 (enExample) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10273219B2 (en) | 2009-11-12 | 2019-04-30 | Pharmatrophix, Inc. | Crystalline forms of neurotrophin mimetic compounds and their salts |
| CN104761515B (zh) | 2009-11-12 | 2018-03-09 | 特罗菲克斯制药股份有限公司 | 神经营养蛋白模拟化合物及其盐的晶型 |
| EP2900646A4 (en) * | 2012-09-27 | 2016-09-21 | Pharmatrophix Inc | CRYSTALLINE FORMS OF NEUROTROPHINMIMETIC COMPOUNDS AND THEIR SALTS |
| WO2016196804A1 (en) * | 2015-06-04 | 2016-12-08 | Balchem Corporation | Hydration control for choline salts |
| US11215532B2 (en) | 2020-05-04 | 2022-01-04 | Ford Global Technologies, Llc | Methods and systems for exhaust gas recirculation system diagnostics |
Family Cites Families (66)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3541130A (en) | 1967-02-06 | 1970-11-17 | Boehringer Sohn Ingelheim | 1-(cyanophenoxy)-2-hydroxy-3-tert.-butylamine propanes |
| US4613676A (en) * | 1983-11-23 | 1986-09-23 | Ciba-Geigy Corporation | Substituted 5-amino-4-hydroxyvaleryl derivatives |
| US4743607A (en) | 1987-05-29 | 1988-05-10 | Merrell Dow Pharmaceuticals Inc. | Cardiotonic tricyclic imidazolones |
| WO1989010744A1 (en) | 1988-05-02 | 1989-11-16 | Naftchi N Eric | Neurologically active compounds |
| US5028622A (en) | 1988-05-06 | 1991-07-02 | Ajinomoto Company, Inc. | Administration of amino acids as treatment for neurodegenerative disorders |
| US5321029A (en) | 1988-11-14 | 1994-06-14 | Beecham-Wuelfing Gmbh & Co.K.G. | Xanthines |
| CA2010531A1 (en) | 1989-03-06 | 1990-09-06 | Werner Neidhart | Amino acid derivatives |
| DK0536671T3 (da) | 1991-10-07 | 1996-08-12 | Hoechst Ag | Carboxylsyreester-beskyttelsesgrupper, en fremgangsmåde til deres fremstilling, kobling til funktionelle grupper samt deres anvendelser |
| US5608067A (en) | 1993-12-09 | 1997-03-04 | Afonso; Adriano | 4-substituted pyrazoloquinoline derivatives |
| GB9402331D0 (en) | 1994-02-07 | 1994-03-30 | Univ Mcgill | Nerve growth factor structural analogs and their uses |
| JPH08119922A (ja) | 1994-10-21 | 1996-05-14 | Torii Yakuhin Kk | o−ピバロイル−チロシン誘導体 |
| AU4117396A (en) * | 1994-11-29 | 1996-06-19 | Novartis Ag | Morpholinoethylamide derivatives |
| JPH1081661A (ja) | 1995-10-23 | 1998-03-31 | Sankyo Co Ltd | ヒドロキサム酸誘導体 |
| CA2250075C (en) | 1996-03-29 | 2008-06-10 | The Trustees Of Boston University | Methods for diagnosing and treating alzheimer's disease |
| US5958875A (en) | 1996-03-29 | 1999-09-28 | The Regents Of The University Of California | Synthetic peptides derivatives with nerve growth factor-like neurotrophic activity |
| AU2645497A (en) | 1996-05-06 | 1997-11-26 | Zeneca Limited | Thio derivatives of hydroxamic acids |
| GB9613547D0 (en) | 1996-06-27 | 1996-08-28 | Pharmacia Spa | Matrix metalloproteinase inhibitors |
| GB9616105D0 (en) | 1996-07-31 | 1996-09-11 | Univ Kingston | TrkA binding site of NGF |
| GB9715962D0 (en) | 1996-08-23 | 1997-10-01 | Zeneca Ltd | Sulfonamides |
| DK0968206T3 (da) | 1997-02-19 | 2007-03-26 | Berlex Inc | N-heterocykliske derivater som NOS-inhibitorer |
| FR2762315B1 (fr) | 1997-04-22 | 1999-05-28 | Logeais Labor Jacques | Derives d'amino-acides inhibiteurs des metalloproteases de la matrice extracellulaire et de la liberation du tnf alpha |
| US6117841A (en) | 1997-05-30 | 2000-09-12 | Warner-Lambert Company | Substituted peptidylamine calcium channel blockers |
| US6342507B1 (en) | 1997-09-05 | 2002-01-29 | Isotechnika, Inc. | Deuterated rapamycin compounds, method and uses thereof |
| US20020022657A1 (en) | 1998-02-11 | 2002-02-21 | Francine Gervais | Methods for modulating neuronal cell death |
| WO1999050264A1 (en) | 1998-03-30 | 1999-10-07 | Kyowa Hakko Kogyo Co., Ltd. | Quinazoline derivatives |
| FR2783519B1 (fr) | 1998-09-23 | 2003-01-24 | Sod Conseils Rech Applic | Nouveaux derives d'amidines, leur preparation, leur application a titre de medicaments et les compositions pharmaceutiques les contenant |
| WO2000027378A2 (en) | 1998-11-06 | 2000-05-18 | Roche Diagnostics Gmbh | Cystine derivatives as therapeutic agents for matrix metalloprotease related diseases |
| WO2000037462A1 (en) | 1998-12-18 | 2000-06-29 | Warner-Lambert Company | Non-peptide nk1 receptors antagonists |
| US6583148B1 (en) | 1999-04-08 | 2003-06-24 | Krenitsky Pharmaceuticals, Inc. | Neurotrophic substituted pyrimidines |
| US6492380B1 (en) | 1999-05-17 | 2002-12-10 | Queen's University At Kingston | Method of inhibiting neurotrophin-receptor binding |
| TWI289557B (en) | 1999-06-17 | 2007-11-11 | Takeda Chemical Industries Ltd | A crystal of a hydrate of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl]-1H-benzimidazole |
| US6858577B1 (en) | 1999-06-29 | 2005-02-22 | Ortho-Mcneil Pharmaceutical, Inc. | Indole peptidomimetics as thrombin receptor antagonists |
| DE19939910A1 (de) | 1999-08-23 | 2001-03-01 | Morphochem Ag | Neue Verbindungen, die Tryptase-Aktivität hemmen |
| WO2001017953A1 (en) | 1999-09-08 | 2001-03-15 | Guilford Pharmaceuticals Inc. | Non-peptidic cyclophilin binding compounds and their use |
| ES2276706T3 (es) | 1999-12-08 | 2007-07-01 | Teijin Limited | Antagonistas del receptor ccr5 de aminas ciclicas. |
| US6881719B2 (en) | 2000-01-18 | 2005-04-19 | Mcgill University | β-turn peptidomimetic cyclic compounds |
| AR028606A1 (es) | 2000-05-24 | 2003-05-14 | Smithkline Beecham Corp | Nuevos inhibidores de mmp-2/mmp-9 |
| US6699989B1 (en) | 2000-08-28 | 2004-03-02 | B. Vithal Shetty | Antiviral and antimicrobial guanidine or biguanidine derivatives |
| AU2002220144A1 (en) | 2000-12-13 | 2002-06-24 | Spelman College | Multiplex coherent raman spectroscopy detector and method |
| MXPA04000334A (es) | 2001-07-11 | 2004-09-28 | Elan Pharm Inc | Compuestos de alquilamida n-(3-amino-2-hidroxi-propil) substituidos. |
| US20040248984A1 (en) | 2001-08-29 | 2004-12-09 | Josef Krieglstein | Use of $g(b)-adrenoceptor agonists for the treatment of neurodegenerative diseases |
| AU2002335824A1 (en) | 2001-10-12 | 2003-04-22 | Case Western Reserve University | Neuronal regeneration |
| EA200400648A1 (ru) | 2001-11-08 | 2005-04-28 | Элан Фармасьютикалз, Инк. | N, n'-замещенные производные 1,3-диамино-2-гидроксипропана |
| KR101027570B1 (ko) * | 2002-05-03 | 2011-04-06 | 이스라엘 인스티튜트 포 바이올로지컬 리서치 | 중추 및 말초 신경계 장애의 치료를 위한 방법 및 조성물, 및 그에 유용한 신규 화합물 |
| UA77526C2 (en) | 2002-06-07 | 2006-12-15 | Sanofi Aventis | Substituted derivatives of 1-piperazineacylpiperidine, a method for the preparation thereof and their use in therapy |
| JP2006503069A (ja) | 2002-09-25 | 2006-01-26 | ジョージア テック リサーチ コーポレイション | 慢性神経疾患におけるケトアミド阻害剤 |
| US20040077635A1 (en) | 2002-10-02 | 2004-04-22 | Qiao Jennifer X. | Lactam-containing diaminoalkyl, beta-aminoacids, alpha-aminoacids and derivatives thereof as factor Xa inhibitors |
| US20040186044A1 (en) | 2002-11-06 | 2004-09-23 | Cosgaya Jose Miguel | Modulation of myelination by interaction with P75 and TRK receptors |
| US20040167183A1 (en) | 2003-02-20 | 2004-08-26 | The Procter & Gamble Company | Phenethylamino sulfamic acids |
| GB0304433D0 (en) | 2003-02-27 | 2003-04-02 | Xceleron Ltd | Improvements relating to chemical libraries |
| US7202269B2 (en) | 2003-10-30 | 2007-04-10 | Janssen Pharmaceutica N.V. | GlyT2 modulators |
| ATE473967T1 (de) | 2003-11-26 | 2010-07-15 | Pfizer Prod Inc | Aminopyrazolderivate als gsk-3-inhibitoren |
| JP2007522129A (ja) | 2004-01-21 | 2007-08-09 | エラン ファーマシューティカルズ,インコーポレイテッド | アスパラギン酸プロテアーゼ阻害薬を用いるアミロイドーシスの処置方法 |
| EP1736465A4 (en) | 2004-03-31 | 2009-06-17 | Ajinomoto Kk | ANILINE DERIVATIVES |
| EP1768955A1 (en) | 2004-07-12 | 2007-04-04 | Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. | Amide derivatives as inhibitors of histone deacetylase |
| JP4194540B2 (ja) | 2004-07-27 | 2008-12-10 | キヤノン株式会社 | 画像形成装置 |
| US20110230479A1 (en) | 2005-04-15 | 2011-09-22 | Longo Frank M | Neurotrophin mimetics and uses thereof |
| EP1871420A4 (en) | 2005-04-15 | 2010-09-22 | Univ North Carolina | PROCESS FOR ENABLING CELL SURVIVAL VIA NEUROTROPHINE MIMETICS |
| EP2526942B1 (en) | 2005-06-08 | 2017-08-09 | The University of North Carolina At Chapel Hill | Methods of facilitating neural cell survival using non-peptide and peptide BDNF neurotrophin mimetics |
| WO2007073505A2 (en) | 2005-12-22 | 2007-06-28 | Hydra Biosciences, Inc. | Trpa1 inhibitors for treating pain |
| WO2008107365A1 (en) * | 2007-03-02 | 2008-09-12 | Medivir Ab | New compounds |
| JP2012519703A (ja) | 2009-03-06 | 2012-08-30 | ザ ユニバーシティ オブ ノース カロライナ アット チャペル ヒル | ニューロトロフィン・ミメティック及びその使用 |
| CN104761515B (zh) | 2009-11-12 | 2018-03-09 | 特罗菲克斯制药股份有限公司 | 神经营养蛋白模拟化合物及其盐的晶型 |
| US10273219B2 (en) | 2009-11-12 | 2019-04-30 | Pharmatrophix, Inc. | Crystalline forms of neurotrophin mimetic compounds and their salts |
| US20120322799A1 (en) | 2009-11-30 | 2012-12-20 | Pharmatrophix, Inc. | Deuterated compounds useful for treating neurodegenerative diseases |
| EP2900646A4 (en) | 2012-09-27 | 2016-09-21 | Pharmatrophix Inc | CRYSTALLINE FORMS OF NEUROTROPHINMIMETIC COMPOUNDS AND THEIR SALTS |
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2010
- 2010-11-12 CN CN201510017717.1A patent/CN104761515B/zh active Active
- 2010-11-12 EP EP18207630.7A patent/EP3470402B1/en active Active
- 2010-11-12 AU AU2010319349A patent/AU2010319349B2/en not_active Ceased
- 2010-11-12 EP EP10830787.7A patent/EP2498782B1/en active Active
- 2010-11-12 US US13/509,470 patent/US9271986B2/en active Active
- 2010-11-12 CN CN201080060921.7A patent/CN102740856B/zh active Active
- 2010-11-12 IN IN5142DEN2012 patent/IN2012DN05142A/en unknown
- 2010-11-12 JP JP2012539022A patent/JP5863663B2/ja active Active
- 2010-11-12 CA CA2780940A patent/CA2780940C/en active Active
- 2010-11-12 WO PCT/US2010/056537 patent/WO2011060262A1/en not_active Ceased
- 2010-11-12 CA CA3125909A patent/CA3125909C/en active Active
- 2010-11-12 CN CN201810315680.4A patent/CN108383804A/zh active Pending
- 2010-11-12 ES ES10830787T patent/ES2712752T3/es active Active
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2015
- 2015-10-09 JP JP2015200793A patent/JP2016020380A/ja active Pending
- 2015-12-17 US US14/972,506 patent/US20160176832A1/en not_active Abandoned
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2017
- 2017-08-21 US US15/682,389 patent/US10532988B2/en active Active
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2018
- 2018-05-07 JP JP2018089165A patent/JP6657294B2/ja active Active