JP2003524613A5 - - Google Patents
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- Publication number
- JP2003524613A5 JP2003524613A5 JP2000585198A JP2000585198A JP2003524613A5 JP 2003524613 A5 JP2003524613 A5 JP 2003524613A5 JP 2000585198 A JP2000585198 A JP 2000585198A JP 2000585198 A JP2000585198 A JP 2000585198A JP 2003524613 A5 JP2003524613 A5 JP 2003524613A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- venlafaxine
- acceptable salt
- substantially free
- stereoisomer
- 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.)
- Pending
Links
- PNVNVHUZROJLTJ-MRXNPFEDSA-N 1-[(1s)-2-(dimethylamino)-1-(4-methoxyphenyl)ethyl]cyclohexan-1-ol Chemical class C1=CC(OC)=CC=C1[C@@H](CN(C)C)C1(O)CCCCC1 PNVNVHUZROJLTJ-MRXNPFEDSA-N 0.000 description 28
- 150000003839 salts Chemical class 0.000 description 27
- 238000004519 manufacturing process Methods 0.000 description 15
- 239000003814 drug Substances 0.000 description 13
- 241000124008 Mammalia Species 0.000 description 10
- 239000008194 pharmaceutical composition Substances 0.000 description 10
- KYYIDSXMWOZKMP-HNNXBMFYSA-N 4-[(1r)-2-(dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenol Chemical group C1([C@H](CN(C)C)C2(O)CCCCC2)=CC=C(O)C=C1 KYYIDSXMWOZKMP-HNNXBMFYSA-N 0.000 description 8
- PNVNVHUZROJLTJ-UHFFFAOYSA-N venlafaxine Chemical compound C1=CC(OC)=CC=C1C(CN(C)C)C1(O)CCCCC1 PNVNVHUZROJLTJ-UHFFFAOYSA-N 0.000 description 8
- 238000000034 method Methods 0.000 description 7
- 229960004688 venlafaxine Drugs 0.000 description 7
- 239000002552 dosage form Substances 0.000 description 6
- 206010021639 Incontinence Diseases 0.000 description 5
- 230000002411 adverse Effects 0.000 description 5
- 230000000694 effects Effects 0.000 description 5
- 239000000546 pharmaceutical excipient Substances 0.000 description 5
- 208000002193 Pain Diseases 0.000 description 4
- 239000003638 chemical reducing agent Substances 0.000 description 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 4
- 239000012453 solvate Substances 0.000 description 4
- 208000000044 Amnesia Diseases 0.000 description 3
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 description 3
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 3
- 208000026106 cerebrovascular disease Diseases 0.000 description 3
- 239000003937 drug carrier Substances 0.000 description 3
- 238000001802 infusion Methods 0.000 description 3
- 238000001990 intravenous administration Methods 0.000 description 3
- 239000008101 lactose Substances 0.000 description 3
- 230000037317 transdermal delivery Effects 0.000 description 3
- PNVNVHUZROJLTJ-INIZCTEOSA-N 1-[(1r)-2-(dimethylamino)-1-(4-methoxyphenyl)ethyl]cyclohexan-1-ol Chemical class C1=CC(OC)=CC=C1[C@H](CN(C)C)C1(O)CCCCC1 PNVNVHUZROJLTJ-INIZCTEOSA-N 0.000 description 2
- 208000024827 Alzheimer disease Diseases 0.000 description 2
- 208000031091 Amnestic disease Diseases 0.000 description 2
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 description 2
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 description 2
- 229920002785 Croscarmellose sodium Polymers 0.000 description 2
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 2
- 229920000881 Modified starch Polymers 0.000 description 2
- 208000019022 Mood disease Diseases 0.000 description 2
- 208000008589 Obesity Diseases 0.000 description 2
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 2
- 230000006986 amnesia Effects 0.000 description 2
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 description 2
- 230000005978 brain dysfunction Effects 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 229960001681 croscarmellose sodium Drugs 0.000 description 2
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 208000035475 disorder Diseases 0.000 description 2
- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 description 2
- 230000004064 dysfunction Effects 0.000 description 2
- 208000035231 inattentive type attention deficit hyperactivity disease Diseases 0.000 description 2
- 235000019359 magnesium stearate Nutrition 0.000 description 2
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 2
- 239000008108 microcrystalline cellulose Substances 0.000 description 2
- 229940016286 microcrystalline cellulose Drugs 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 235000020824 obesity Nutrition 0.000 description 2
- 230000004584 weight gain Effects 0.000 description 2
- 235000019786 weight gain Nutrition 0.000 description 2
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 description 1
- 208000017194 Affective disease Diseases 0.000 description 1
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 1
- 208000019901 Anxiety disease Diseases 0.000 description 1
- 206010065559 Cerebral arteriosclerosis Diseases 0.000 description 1
- 206010008111 Cerebral haemorrhage Diseases 0.000 description 1
- 206010008138 Cerebral venous thrombosis Diseases 0.000 description 1
- 208000000094 Chronic Pain Diseases 0.000 description 1
- 208000030814 Eating disease Diseases 0.000 description 1
- 208000027534 Emotional disease Diseases 0.000 description 1
- 208000034347 Faecal incontinence Diseases 0.000 description 1
- 208000019454 Feeding and Eating disease Diseases 0.000 description 1
- 206010019196 Head injury Diseases 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- 208000026139 Memory disease Diseases 0.000 description 1
- 208000019695 Migraine disease Diseases 0.000 description 1
- 208000021384 Obsessive-Compulsive disease Diseases 0.000 description 1
- 208000018737 Parkinson disease Diseases 0.000 description 1
- 206010036618 Premenstrual syndrome Diseases 0.000 description 1
- 206010037211 Psychomotor hyperactivity Diseases 0.000 description 1
- 206010039966 Senile dementia Diseases 0.000 description 1
- 206010066218 Stress Urinary Incontinence Diseases 0.000 description 1
- 208000000921 Urge Urinary Incontinence Diseases 0.000 description 1
- 206010046543 Urinary incontinence Diseases 0.000 description 1
- 230000001668 ameliorated effect Effects 0.000 description 1
- 230000036506 anxiety Effects 0.000 description 1
- 235000010290 biphenyl Nutrition 0.000 description 1
- 239000004305 biphenyl Substances 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 206010008118 cerebral infarction Diseases 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 150000002016 disaccharides Chemical class 0.000 description 1
- 235000014632 disordered eating Nutrition 0.000 description 1
- 229960003638 dopamine Drugs 0.000 description 1
- 206010015037 epilepsy Diseases 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 208000020658 intracerebral hemorrhage Diseases 0.000 description 1
- 201000005851 intracranial arteriosclerosis Diseases 0.000 description 1
- 229960001375 lactose Drugs 0.000 description 1
- 229910052744 lithium Inorganic materials 0.000 description 1
- 210000005171 mammalian brain Anatomy 0.000 description 1
- 230000006984 memory degeneration Effects 0.000 description 1
- 208000023060 memory loss Diseases 0.000 description 1
- 206010027599 migraine Diseases 0.000 description 1
- 150000002772 monosaccharides Chemical class 0.000 description 1
- 210000002569 neuron Anatomy 0.000 description 1
- 208000024449 overflow incontinence Diseases 0.000 description 1
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N phenylbenzene Natural products C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 description 1
- 230000011514 reflex Effects 0.000 description 1
- 201000009032 substance abuse Diseases 0.000 description 1
- 231100000736 substance abuse Toxicity 0.000 description 1
- 208000011117 substance-related disease Diseases 0.000 description 1
- 208000011580 syndromic disease Diseases 0.000 description 1
- 239000003053 toxin Substances 0.000 description 1
- 231100000765 toxin Toxicity 0.000 description 1
- 206010046494 urge incontinence Diseases 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11048898P | 1998-12-01 | 1998-12-01 | |
| US60/110,488 | 1998-12-01 | ||
| US09/450,690 US6342533B1 (en) | 1998-12-01 | 1999-11-30 | Derivatives of (−)-venlafaxine and methods of preparing and using the same |
| US09/450,690 | 1999-11-30 | ||
| PCT/US1999/028303 WO2000032556A1 (en) | 1998-12-01 | 1999-12-01 | Derivatives of (-)-venlafaxine and methods of preparing and using the same |
Related Child Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011001270A Division JP2011093924A (ja) | 1998-12-01 | 2011-01-06 | （−）−ベンラファキシン誘導体並びにその製造方法および使用方法 |
| JP2013172984A Division JP2013256526A (ja) | 1998-12-01 | 2013-08-23 | （−）−ベンラファキシン誘導体並びにその製造方法および使用方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2003524613A JP2003524613A (ja) | 2003-08-19 |
| JP2003524613A5 true JP2003524613A5 (enExample) | 2007-01-25 |
Family
ID=26808068
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000585198A Pending JP2003524613A (ja) | 1998-12-01 | 1999-12-01 | （−）−ベンラファキシン誘導体並びにその製造方法および使用方法 |
| JP2011001270A Pending JP2011093924A (ja) | 1998-12-01 | 2011-01-06 | （−）−ベンラファキシン誘導体並びにその製造方法および使用方法 |
| JP2013172984A Pending JP2013256526A (ja) | 1998-12-01 | 2013-08-23 | （−）−ベンラファキシン誘導体並びにその製造方法および使用方法 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011001270A Pending JP2011093924A (ja) | 1998-12-01 | 2011-01-06 | （−）−ベンラファキシン誘導体並びにその製造方法および使用方法 |
| JP2013172984A Pending JP2013256526A (ja) | 1998-12-01 | 2013-08-23 | （−）−ベンラファキシン誘導体並びにその製造方法および使用方法 |
Country Status (6)
| Country | Link |
|---|---|
| US (9) | US6342533B1 (enExample) |
| EP (2) | EP1953136A1 (enExample) |
| JP (3) | JP2003524613A (enExample) |
| AU (1) | AU774408B2 (enExample) |
| CA (1) | CA2352324C (enExample) |
| WO (1) | WO2000032556A1 (enExample) |
Families Citing this family (54)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7208010B2 (en) | 2000-10-16 | 2007-04-24 | Conor Medsystems, Inc. | Expandable medical device for delivery of beneficial agent |
| US6241762B1 (en) * | 1998-03-30 | 2001-06-05 | Conor Medsystems, Inc. | Expandable medical device with ductile hinges |
| US6342533B1 (en) | 1998-12-01 | 2002-01-29 | Sepracor, Inc. | Derivatives of (−)-venlafaxine and methods of preparing and using the same |
| WO2000076955A1 (en) * | 1999-06-15 | 2000-12-21 | American Home Products Corporation | Enantiomers of o-desmethyl venlafaxine |
| AU5613600A (en) * | 1999-06-15 | 2001-01-02 | American Home Products Corporation | Enantiomers of n-desmethyl venlafaxine |
| US20020035158A1 (en) * | 1999-06-15 | 2002-03-21 | American Home Products Corporation | Enantiomers of N-desmethyl venlafaxine |
| US20020022662A1 (en) * | 1999-06-15 | 2002-02-21 | American Home Products Corporation | Enantiomers of O-desmethyl venlafaxine |
| US6348494B1 (en) * | 2000-11-21 | 2002-02-19 | American Home Products Corporation | Ethers of o-desmethyl venlafaxine |
| US7291646B2 (en) | 1999-11-24 | 2007-11-06 | Wyeth | Ethers of O-desmethyl venlafaxine |
| DZ3282A1 (fr) * | 2000-03-07 | 2001-09-13 | Lilly Co Eli | Traitement du psoriasis |
| DE10042412B4 (de) * | 2000-08-30 | 2005-12-22 | Lts Lohmann Therapie-Systeme Ag | Transdermales therapeutisches System zur Abgabe von Venlafaxin, und seine Verwendung |
| AU9463401A (en) | 2000-10-16 | 2002-04-29 | Conor Medsystems Inc | Expandable medical device for delivery of beneficial agent |
| US20030232890A1 (en) | 2000-11-01 | 2003-12-18 | Sention, Inc. | Methods for treating an impairment in memory consolidation |
| US7619005B2 (en) | 2000-11-01 | 2009-11-17 | Cognition Pharmaceuticals Llc | Methods for treating cognitive impairment in humans with Multiple Sclerosis |
| TWI291871B (en) | 2000-11-01 | 2008-01-01 | Cognition Pharmaceuticals Llc | Pharmaceutical compositions and use of amphetamine compounds for improving memory and learning |
| EP1864967A1 (en) * | 2001-02-12 | 2007-12-12 | Wyeth | Method for preparing O-desmethyl-venlafaxine |
| US7842083B2 (en) * | 2001-08-20 | 2010-11-30 | Innovational Holdings, Llc. | Expandable medical device with improved spatial distribution |
| UA80543C2 (en) * | 2001-12-04 | 2007-10-10 | Wyeth Corp | Method for the preparation of o-desmethylvenlafaxine |
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| WO2003082804A1 (en) | 2002-03-28 | 2003-10-09 | Synthon B.V. | Venlafaxine besylate |
| WO2003082805A1 (en) | 2002-03-28 | 2003-10-09 | Synthon B.V. | Low water-soluble venlafaxine salts |
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| US7470435B2 (en) * | 2003-11-17 | 2008-12-30 | Andrx Pharmaceuticals, Llc | Extended release venlafaxine formulation |
| JP5646126B2 (ja) * | 2003-12-11 | 2014-12-24 | サノビオン ファーマシューティカルズ インクＳｕｎｏｖｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃ． | 鎮静剤と神経伝達物質調節剤の併用、および睡眠の質の向上方法および鬱の治療方法 |
| US20050175698A1 (en) * | 2004-02-06 | 2005-08-11 | Wyeth | Multiparticulate O-desmethylvenlafaxine salts and uses thereof |
| US7417009B2 (en) * | 2004-03-26 | 2008-08-26 | Nalco Company | Paraffin inhibitors |
| US7776358B2 (en) | 2004-07-22 | 2010-08-17 | Synthon Ip Inc. | Extended release venlafaxine besylate tablets |
| US20060193911A1 (en) * | 2005-02-28 | 2006-08-31 | Penwest Pharmaceuticals Co., | Controlled release venlafaxine formulations |
| US20090111818A1 (en) * | 2005-07-06 | 2009-04-30 | Sepracor Inc. | Combinations of Eszopiclone and O-Desmethylvenlafaxine, and Methods of Treatment of Menopause and Mood, Anxiety, and Cognitive Disorders |
| MX2008000248A (es) * | 2005-07-06 | 2008-03-19 | Sepracor Inc | Combinaciones de eszopiclona y un antidepresivo y metodos de tratamiento contra la menopausia y trastornos del estado de animo, la ansiedad y trastornos cognitivos. |
| GT200600397A (es) * | 2005-09-07 | 2007-08-28 | Formulas topicas conteniendo o-desmetil venlafaxina (odv) o sus sales | |
| CA2625832A1 (en) * | 2005-10-19 | 2007-04-26 | Vinod Kumar Kansal | Process for the preparation of highly pure 1-[2-dimethylamino-(4-methoxyphenyl) ethyl]cyclohexanol hydrochloride |
| AU2006328198B2 (en) * | 2005-12-19 | 2013-07-18 | Medizinische Hochschule Hannover | Substituted phenol derivatives as analgesics |
| EP1973866A1 (en) | 2005-12-20 | 2008-10-01 | Synthon B.V. | Process for making desvenlafaxine |
| CN101374552A (zh) * | 2006-01-27 | 2009-02-25 | 旭化成制药株式会社 | 经鼻给药用药剂 |
| TW200806282A (en) * | 2006-05-05 | 2008-02-01 | Wyeth Corp | Solid dosage formulations |
| US20080081067A1 (en) * | 2006-10-03 | 2008-04-03 | Gupta Manishkumar | Sustained release pharmaceutical compositions of venlafaxine and process for preparation thereof |
| US20100094055A1 (en) * | 2007-01-09 | 2010-04-15 | Pharmathen S.A. | Process for the preparation of phenethylamine derivatives |
| ZA200905698B (en) * | 2007-02-21 | 2010-10-27 | Sepracor Inc | Solid forms comprising (-) O-desmethylvenlafaxine and uses thereof |
| CA2702664A1 (en) * | 2007-10-16 | 2009-04-23 | Alphapharm Pty Ltd | Controlled-release pharmaceutical formulation |
| CA2703647A1 (en) | 2007-10-26 | 2009-04-30 | Generics [Uk] Limited | Process for preparing o-desmethylvenlafaxine |
| EP2074993A1 (en) | 2007-12-19 | 2009-07-01 | Biovail Laboratories International S.r.l. | Venlafaxine-containing film-coated modified-release tablets |
| WO2009084037A2 (en) * | 2007-12-20 | 2009-07-09 | Calyx Chemicals And Pharmaceuticals Ltd. | Novel process for preparation of o-desmethylvenlafaxine |
| WO2009144517A1 (en) * | 2008-04-14 | 2009-12-03 | Egis Gyógyszergyár Nyilvánosan Müködö | Process for the preparation of cyclohexanol derivatives |
| CA2749933A1 (en) * | 2009-02-04 | 2010-08-12 | Supernus Pharmaceuticals, Inc. | Formulations of desvenlafaxine |
| CZ303249B6 (cs) | 2010-04-06 | 2012-06-20 | Zentiva, K.S. | Zpusob výroby 4-(2-(substituovaných)-1-(1-hydroxycyklohexyl)ethyl)fenolu O-demethylací jejich methyletheru pomocí nepáchnoucích aromatických thiolu |
| US8933123B2 (en) | 2010-10-08 | 2015-01-13 | Cadila Healthcare Limited | Polymorphic forms of O-desmethyl-venlafaxine succinate |
| CN104529797A (zh) * | 2014-12-05 | 2015-04-22 | 南昌市博泽康医药科技有限公司 | 盐酸文拉法辛手性晶型的制备 |
| CN106692118A (zh) * | 2016-11-18 | 2017-05-24 | 广州军区广州总医院 | 文拉法辛在制备预防或治疗轻型脑损伤后认知功能障碍的药物中的应用 |
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-
1999
- 1999-11-30 US US09/450,690 patent/US6342533B1/en not_active Expired - Lifetime
- 1999-12-01 CA CA2352324A patent/CA2352324C/en not_active Expired - Fee Related
- 1999-12-01 JP JP2000585198A patent/JP2003524613A/ja active Pending
- 1999-12-01 EP EP07120208A patent/EP1953136A1/en not_active Ceased
- 1999-12-01 EP EP99968056A patent/EP1135359A1/en not_active Ceased
- 1999-12-01 WO PCT/US1999/028303 patent/WO2000032556A1/en not_active Ceased
- 1999-12-01 AU AU24749/00A patent/AU774408B2/en not_active Ceased
-
2001
- 2001-12-14 US US10/014,592 patent/US6441048B1/en not_active Expired - Lifetime
-
2002
- 2002-08-19 US US10/222,815 patent/US6911479B2/en not_active Expired - Lifetime
-
2004
- 2004-03-23 US US10/806,423 patent/US20040180952A1/en not_active Abandoned
-
2006
- 2006-05-05 US US11/418,138 patent/US20060199861A1/en not_active Abandoned
- 2006-05-05 US US11/418,137 patent/US20060199860A1/en not_active Abandoned
-
2011
- 2011-01-06 JP JP2011001270A patent/JP2011093924A/ja active Pending
-
2012
- 2012-05-25 US US13/481,584 patent/US8642662B2/en not_active Expired - Fee Related
-
2013
- 2013-08-23 JP JP2013172984A patent/JP2013256526A/ja active Pending
- 2013-12-23 US US14/139,339 patent/US9072700B2/en not_active Expired - Fee Related
-
2015
- 2015-07-01 US US14/789,327 patent/US20150299102A1/en not_active Abandoned
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