AR040955A1 - Analogos de ghrelina - Google Patents
Analogos de ghrelinaInfo
- Publication number
- AR040955A1 AR040955A1 ARP030102647A ARP030102647A AR040955A1 AR 040955 A1 AR040955 A1 AR 040955A1 AR P030102647 A ARP030102647 A AR P030102647A AR P030102647 A ARP030102647 A AR P030102647A AR 040955 A1 AR040955 A1 AR 040955A1
- Authority
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- Argentina
- Prior art keywords
- aib
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- Prior art date
Links
- ODKSFYDXXFIFQN-UHFFFAOYSA-N Arginine Chemical compound OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 abstract 7
- PMMYEEVYMWASQN-UHFFFAOYSA-N dl-hydroxyproline Natural products OC1C[NH2+]C(C([O-])=O)C1 PMMYEEVYMWASQN-UHFFFAOYSA-N 0.000 abstract 5
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Chemical compound CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 abstract 3
- -1 Tle Chemical compound 0.000 abstract 3
- 125000002252 acyl group Chemical group 0.000 abstract 3
- 125000003342 alkenyl group Chemical group 0.000 abstract 3
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 2
- 125000002877 alkyl aryl group Chemical group 0.000 abstract 2
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 108090000765 processed proteins & peptides Proteins 0.000 abstract 2
- 125000003107 substituted aryl group Chemical group 0.000 abstract 2
- 230000001225 therapeutic effect Effects 0.000 abstract 2
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 abstract 1
- 125000003837 (C1-C20) alkyl group Chemical group 0.000 abstract 1
- QNAYBMKLOCPYGJ-UHFFFAOYSA-N D-alpha-Ala Natural products CC([NH3+])C([O-])=O QNAYBMKLOCPYGJ-UHFFFAOYSA-N 0.000 abstract 1
- 101800001586 Ghrelin Proteins 0.000 abstract 1
- 102000012004 Ghrelin Human genes 0.000 abstract 1
- 101100109397 Neurospora crassa (strain ATCC 24698 / 74-OR23-1A / CBS 708.71 / DSM 1257 / FGSC 987) arg-8 gene Proteins 0.000 abstract 1
- 239000000556 agonist Substances 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 150000001413 amino acids Chemical class 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- UCMIRNVEIXFBKS-UHFFFAOYSA-N beta-alanine Chemical compound NCCC(O)=O UCMIRNVEIXFBKS-UHFFFAOYSA-N 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 229950003988 decil Drugs 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- GNKDKYIHGQKHHM-RJKLHVOGSA-N ghrelin Chemical compound C([C@H](NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)CN)COC(=O)CCCCCCC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1N=CNC=1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)C1=CC=CC=C1 GNKDKYIHGQKHHM-RJKLHVOGSA-N 0.000 abstract 1
- 125000001151 peptidyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
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- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
- C07K14/47—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
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- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/575—Hormones
- C07K14/61—Growth hormone [GH], i.e. somatotropin
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- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
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- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/22—Hormones
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- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
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Abstract
La presente comprende análogos de peptidilo que poseen actividad de Ghrelina agonista o antagonista, junto con usos terapéuticos y no terapéuticos de los mismos. Reivindicación 1: Un compuesto conforme a la fórmula: (R2R3)-A1-A2-A3-A4-A5-A6-A7-A8-A9-A10-A11-A12-A13-A14-A15-A16-A17-A18-A19-A20-A21-A22-A23-A24-A25-A26-A27-A28-R1, en donde: A1 es Gly, Aib, Ala, beta-Ala, o Acc; A2 es Ser, Aib, Act, Ala, Acc, Abu, Act, Ava, Thr, o Val; A3 es Ser, Ser(C(O)-R4), Asp(O-R8), Asp(NH-R9); Cys(S-R14), Dap(S(O)2-R10), Dab(S(O)2-R11), Glu(O-R6), Glu(NH-R7), Thr, Thr(C(O)-R5), o HN-CH((CH2)n-N(R12R13))-C(O); A4 es Phe, Acc, Aic, Cha, 2Fua, 1Nal, 2Nal, 2Pal, 3Pal, 4Pal, hPhe, (X1, X2, X3, X4, X5)Phe, Taz, 2Thi, 3Thi, Trp, o Tyr; A5 es Leu, Abu, Acc, Aib, Ala, Cha, lle, hLeu, Nle, Nva, Phe, Tle, o Val; A6 es Ser, Abu, Acc, Act, Aib, Ala, Gly, Thr, o Val; A7 es Pro, Dhp, Dmt, 3Hyp, 4Hyp, Inc, Ktp, Oic, Pip, Thz, Tic, o eliminado; A8 es Glu, Acc, Aib, Arg, Asn, Asp, Dab, Dap, Gln, Lys, Orn, HN-CH((CH2)n-N(R12R13))-C(O), o eliminado; A9 es His, Apc, Aib, Acc, 2Fua, 2Pal, 3Pal, 4Pal, Taz, 2Thi, 3Thi, (X1, X2, X3, X4, X5-)Phe, o eliminado; A10 es Gln, Acc, Aib, Asn, Asp, Glu, o eliminado; A11 es Arg, Apc, hArg, Dab, Dap, Lys, Orn, HN-CH((CH2)n-N(R12R13))-C(O), o eliminado; A12 es Val, Abu, Acc, Aib, Ala, Cha, Nva, Gly, lle, Leu, Nle, Tle, Cha, o eliminado; A13 es Gln, Acc, Aib, Asn, Asp, Glu, o eliminado; A14 es Gln, Acc, Aib, Asn, Asp, Glu, o eliminado; A15 es Arg, hArg, Acc, Aib, Apc, Dab, Dap, Lys, Orn, HN-CH((CH2)n-N(R12R13))-C(O), o eliminado; A16 es, Lys, Acc, Aib, Apc, Arg, hArg, Dab, Dap, Orn, HN-CH((CH2)n-(N(R12R13))-C(O), o eliminado; A17 es Glu, Arg, Asn, Asp, Dab, Dap, Gln, Lys, Orn, HN-CH((CH2)n-N(R12R13))-C(O), o eliminado; A18 es Ser, Abu, Acc, Act, Aib, Ala, Thr, Val, o eliminado; A19 es Lys, Acc, Aib, Apc, Arg, hArg, Dab, Dap, Orn, HN-CH((CH2)n-N(R12R13))-C(O), o eliminado; A20 es Lys, Acc, Aib, Apc, Arg, hArg, Dab, Dap, Orn, HN-CH((CH2)n-N(R12R13))-C(O), o eliminado; A21 es Pro, Dhp, Dmt, Inc, 3Hyp, 4Hyp, Ktp, Oic, Pip, Thz, Tic, o eliminado; A22 es Pro, Dhp, Dmt, 3Hyp, 4Hyp, Inc, Ktp, Oic, Pip, Thz, Tic, o eliminado; A23 es Abu, Acc, Act, Aib, Ala, Apc, Gly, Nva, Val, o eliminado; A24 es Lys, Acc, Aib, Apc, Arg, hArg, Dab, Dap, Orn, HN-CH((CH2)n-N(R12R13))-C(O), o eliminado; A25 es Leu, Abu, Acc, Aib, Ala, Cha, lle, hleu, Nle, Nva, Phe, Tle, Val, o eliminado; A26 es Gln, Aib, Asn, Asp, Glu, o eliminado; A27 es Pro, Dhp, Dmt, 3Hyp, 4Hyp, Inc, Ktp, Oic, Pip, Thz, Tic, o eliminado; A28 es Acc, Aib, Apc, Arg, hArg, Dab, Dap, Lys, Orn, HN-CH((CH2)n-N(R12R13))-C(O), o eliminado; R1 es -OH, -NH2, -alcoxi (C1-30), o NH-X6-CH2-Z0, en donde X6 es un alquilo (C1-12), alquenilo (C2-12), y Z0 es -H, -OH, -CO2H o -C(O)-NH2; R2 y R3 son, cada un en forma independiente para cada aparición, H, alquilo (C1-20) o acilo (C1-20); R4, R5, R6, R7, R8, R9 , R10, R11 y R14 son, cada uno en forma independiente para cada aparición, alquilo (C1-40), alquenilo (C2-40), alquilo (C1-40) sustituido, alquenilo (C2-40) sustituido, alquilarilo, alquilarilo sustituido, arilo o arilo sustituido; R12 y R13 son, cada uno en forma independiente para cada aparición, H, alquilo (C1-40), acilo (C1-40), alquilsulfonilo (C1-30) o -C(NH)-NH2, en donde cuando R12 es acilo (C1-40), alquilsulfonilo (C1-30), o -C(NH)-NH2, entonces R13 es H o alquilo (C1-40); n es, en forma independiente para cada aparición 1, 2, , 3, 4, ó 5; X1, X2, X3, X4 y X5 son, cada uno en forma independiente para cada aparición, H, F, Cl, Br, I, alquilo (C1-10), alquilo (C1-10) sustituido, arilo, arilo sustituido, OH, NH2, NO2, o CN; siempre que el péptido contenga por lo menos un aminoácido seleccionado entre los grupos que consiste en: A2 es Aib, Acc, o Act; A3 es Dap(S(O)2-R10), Dab(S(O)2-R11), Glu(NH-Hexil), o Cys(S-Decil); A5 es Abu, Acc, Aib, Ala, Cha, lle, hLeu, Nle, Nva, Phe, Tle, o Val; A6 es Abu, Acc, Act, Aib, Ala, Gly, Thr, o Val; A7 es Dhp, Dmt, 3Hyp, 4Hyp, Inc, Ktp, Oic, Pip, Thz, o Tic; A8 es Acc, Aib, Arg, Asn, Asp, Dab, Dap, Gln, Lys, Orn, o HN-CH((CH2)n-N(R12R13))-C(O); A9 es Aib, Acc, Apc, 2Fua, 2Pal, 3Pal, 4Pal, Taz, 2Thi, 3Thi, o (X1, X2, X3, X4, X5-)Phe; y A10 es Acc, Aib, Asn, Asp, o Glu; y además, siempre que el péptido no sea (Lys8)hGhrelina(1-8)-NH2 o (Arg8)Hgrelina(1-8)-NH2, o una sal farmacéuticamente aceptable de los mismos.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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US39783402P | 2002-07-23 | 2002-07-23 | |
US42748802P | 2002-11-19 | 2002-11-19 |
Publications (1)
Publication Number | Publication Date |
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AR040955A1 true AR040955A1 (es) | 2005-04-27 |
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ARP030102647A AR040955A1 (es) | 2002-07-23 | 2003-07-23 | Analogos de ghrelina |
ARP090103204A AR073099A2 (es) | 2002-07-23 | 2009-08-20 | Analogos de ghrelina |
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ARP090103204A AR073099A2 (es) | 2002-07-23 | 2009-08-20 | Analogos de ghrelina |
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US (3) | US7589058B2 (es) |
EP (2) | EP2258381A3 (es) |
JP (2) | JP2006515271A (es) |
KR (1) | KR101065471B1 (es) |
AR (2) | AR040955A1 (es) |
AT (1) | ATE496940T1 (es) |
AU (1) | AU2003254119B2 (es) |
BR (1) | BR0312871A (es) |
CA (1) | CA2491946C (es) |
DE (1) | DE60335913D1 (es) |
IL (1) | IL166170A (es) |
MX (1) | MXPA05000908A (es) |
NO (1) | NO334857B1 (es) |
PL (1) | PL212106B1 (es) |
PT (1) | PT1578778E (es) |
RU (3) | RU2315059C2 (es) |
TW (1) | TWI325003B (es) |
WO (1) | WO2004009616A2 (es) |
Families Citing this family (23)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
PT1578778E (pt) | 2002-07-23 | 2011-03-07 | Ipsen Pharma | Análogos de grelina |
CA2566703A1 (en) * | 2004-05-11 | 2005-11-24 | Vishwa Deep Dixit | Methods of inhibiting proinflammatory cytokine expression using ghrelin |
CA2625920C (en) | 2005-09-28 | 2014-12-23 | Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R | Analogs of ghrelin |
EP1937262B1 (en) * | 2005-09-29 | 2019-05-08 | Ipsen Pharma | Composition for use in treating gastrointestinal dysmotility |
US8992928B2 (en) * | 2006-02-11 | 2015-03-31 | Victor Raso | Isolated monoclonal antibody or antigen-binding fragment that cleaves octanoylated native ghrelin |
ES2424970T3 (es) | 2006-03-10 | 2013-10-10 | Ipsen Pharma | Uso de un agonista de la grelina para mejorar los efectos catabólicos del tratamiento con glucocorticoides |
WO2007108990A2 (en) * | 2006-03-13 | 2007-09-27 | Liat Mintz | Use of ghrelin splice variant for treating cachexia and/or anorexia and/or anorexia-cachexia and/or malnutrition and/or lipodystrophy and/or muscle wasting and/or appetite stimulation |
BRPI0717169C1 (pt) | 2006-09-27 | 2012-12-04 | Ipsen Pharma Sas | análogos de grelina substituìda no n-terminal |
WO2008067831A2 (en) * | 2006-12-05 | 2008-06-12 | Charite Universitätsmedizin - Berlin | Use of ghrelin, an analogue thereof or a pharmaceutically acceptable salt thereof |
TW200916113A (en) | 2007-08-08 | 2009-04-16 | Sod Conseils Rech Applic | Method for inhibiting inflammation and pro-inflammatory cytokine/chemokine expression using a ghrelin analogue |
US8883721B2 (en) * | 2009-05-12 | 2014-11-11 | Mcgill University | Methods of inhibiting the ghrelin/growth hormone secretatogue receptor pathway and uses thereof |
US9724381B2 (en) | 2009-05-12 | 2017-08-08 | The Administrators Of The Tulane Educational Fund | Methods of inhibiting the ghrelin/growth hormone secretatogue receptor pathway and uses thereof |
EP2493910A1 (en) | 2009-10-30 | 2012-09-05 | Tranzyme Pharma, Inc. | Macrocyclic ghrelin receptor antagonists and inverse agonists and methods of using the same |
EP2582715B1 (en) * | 2010-06-16 | 2018-11-28 | The Administrators of the Tulane Educational Fund | Growth hormone secretatogue receptor antagonists and uses thereof |
JP5560248B2 (ja) * | 2011-09-07 | 2014-07-23 | 花王株式会社 | ジペプチド誘導体及びその製造方法 |
JP2015510505A (ja) * | 2012-02-03 | 2015-04-09 | ジーランド ファーマ アクティーゼルスカブ | グレリン類似体 |
AU2013263349B2 (en) | 2012-05-17 | 2016-09-08 | Extend Biosciences, Inc | Carriers for improved drug delivery |
US9119832B2 (en) | 2014-02-05 | 2015-09-01 | The Regents Of The University Of California | Methods of treating mild brain injury |
JP6946182B2 (ja) | 2014-10-22 | 2021-10-06 | エクステンド バイオサイエンシズ インコーポレーテッドExtend Biosciences, Inc | 治療用ビタミンdコンジュゲート |
WO2016065052A1 (en) | 2014-10-22 | 2016-04-28 | Extend Biosciences, Inc. | Insulin vitamin d conjugates |
US9789197B2 (en) | 2014-10-22 | 2017-10-17 | Extend Biosciences, Inc. | RNAi vitamin D conjugates |
WO2017075535A1 (en) | 2015-10-28 | 2017-05-04 | Oxeia Biopharmaceuticals, Inc. | Methods of treating neurodegenerative conditions |
CN108029863B (zh) * | 2018-01-19 | 2021-07-27 | 广州英赛特生物技术有限公司 | 丁酰甘氨酸及其衍生物在制备动物饲料添加剂中的应用 |
Family Cites Families (10)
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GB8821785D0 (en) * | 1988-09-16 | 1988-10-19 | Nycomed As | Peptide compounds |
US5264565A (en) | 1991-01-22 | 1993-11-23 | Affymax Technologies, N.V. | Nucleic acid encoding the D2 /Ml chimeric receptor |
WO1997005252A2 (en) | 1995-07-26 | 1997-02-13 | Nps Pharmaceuticals, Inc. | Chimeric receptors and methods for identifying compounds active at metabotropic glutamate receptors and the use of such compounds in the treatment of neurological disorders and diseases |
WO1997021730A1 (en) | 1995-12-13 | 1997-06-19 | Merck & Co., Inc. | Growth hormone secretagogue receptor family |
US7368427B1 (en) * | 1998-12-07 | 2008-05-06 | Societe De Conseils De Recherches Et D'applications Scientifiques, Sas | GLP-1 analogues |
DK1795598T3 (da) * | 1999-07-23 | 2010-02-01 | Kenji Kangawa | Hidtil ukendte peptider |
WO2001092292A2 (en) * | 2000-05-30 | 2001-12-06 | Merck & Co., Inc. | Ghrelin analogs |
AU2001283938A1 (en) * | 2000-07-24 | 2002-02-05 | Ardana Bioscience Limited | Ghrelin antagonists |
WO2002083860A2 (en) * | 2001-04-10 | 2002-10-24 | Agensys, Inc. | Nucleic acid and corresponding protein entitled 151p3d4 useful in treatment and detection of cancer |
PT1578778E (pt) | 2002-07-23 | 2011-03-07 | Ipsen Pharma | Análogos de grelina |
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2003
- 2003-07-23 PT PT03765930T patent/PT1578778E/pt unknown
- 2003-07-23 EP EP10181462A patent/EP2258381A3/en not_active Withdrawn
- 2003-07-23 TW TW092120152A patent/TWI325003B/zh not_active IP Right Cessation
- 2003-07-23 KR KR1020057001095A patent/KR101065471B1/ko not_active IP Right Cessation
- 2003-07-23 CA CA2491946A patent/CA2491946C/en not_active Expired - Fee Related
- 2003-07-23 AR ARP030102647A patent/AR040955A1/es not_active Application Discontinuation
- 2003-07-23 EP EP03765930A patent/EP1578778B1/en not_active Expired - Lifetime
- 2003-07-23 RU RU2005104841/04A patent/RU2315059C2/ru not_active IP Right Cessation
- 2003-07-23 PL PL377075A patent/PL212106B1/pl unknown
- 2003-07-23 AU AU2003254119A patent/AU2003254119B2/en not_active Ceased
- 2003-07-23 US US10/522,398 patent/US7589058B2/en not_active Expired - Fee Related
- 2003-07-23 AT AT03765930T patent/ATE496940T1/de not_active IP Right Cessation
- 2003-07-23 DE DE60335913T patent/DE60335913D1/de not_active Expired - Lifetime
- 2003-07-23 JP JP2004523304A patent/JP2006515271A/ja active Pending
- 2003-07-23 RU RU2007124275/04A patent/RU2373220C2/ru not_active IP Right Cessation
- 2003-07-23 WO PCT/US2003/022925 patent/WO2004009616A2/en active Search and Examination
- 2003-07-23 BR BRPI0312871-7A patent/BR0312871A/pt not_active IP Right Cessation
- 2003-07-23 MX MXPA05000908A patent/MXPA05000908A/es active IP Right Grant
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2005
- 2005-01-06 IL IL166170A patent/IL166170A/en active IP Right Grant
- 2005-01-06 NO NO20050083A patent/NO334857B1/no not_active IP Right Cessation
-
2009
- 2009-02-27 JP JP2009046345A patent/JP2009161546A/ja active Pending
- 2009-06-16 US US12/456,429 patent/US8633151B2/en not_active Expired - Fee Related
- 2009-07-14 RU RU2009127162/04A patent/RU2009127162A/ru not_active Application Discontinuation
- 2009-08-20 AR ARP090103204A patent/AR073099A2/es not_active Application Discontinuation
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2014
- 2014-01-17 US US14/157,770 patent/US9133261B2/en not_active Expired - Fee Related
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