CA2878819A1 - Tri-salt form of metformin - Google Patents
Tri-salt form of metformin Download PDFInfo
- Publication number
- CA2878819A1 CA2878819A1 CA2878819A CA2878819A CA2878819A1 CA 2878819 A1 CA2878819 A1 CA 2878819A1 CA 2878819 A CA2878819 A CA 2878819A CA 2878819 A CA2878819 A CA 2878819A CA 2878819 A1 CA2878819 A1 CA 2878819A1
- Authority
- CA
- Canada
- Prior art keywords
- compound
- metformin
- subject
- formula
- diabetes
- 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.)
- Abandoned
Links
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- 229960003105 metformin Drugs 0.000 title claims abstract description 52
- 150000001875 compounds Chemical class 0.000 claims abstract description 158
- 150000003839 salts Chemical class 0.000 claims abstract description 72
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- JAZBEHYOTPTENJ-JLNKQSITSA-N all-cis-5,8,11,14,17-icosapentaenoic acid Chemical compound CC\C=C/C\C=C/C\C=C/C\C=C/C\C=C/CCCC(O)=O JAZBEHYOTPTENJ-JLNKQSITSA-N 0.000 claims abstract description 49
- MBMBGCFOFBJSGT-KUBAVDMBSA-N all-cis-docosa-4,7,10,13,16,19-hexaenoic acid Chemical compound CC\C=C/C\C=C/C\C=C/C\C=C/C\C=C/C\C=C/CCC(O)=O MBMBGCFOFBJSGT-KUBAVDMBSA-N 0.000 claims abstract description 32
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- SARHCLAXCDURCW-RSDXMDNYSA-N 3-(diaminomethylidene)-1,1-dimethylguanidine;(5z,8z,11z,14z,17z)-icosa-5,8,11,14,17-pentaenoic acid Chemical compound CN(C)C(=[NH2+])NC(N)=N.CC\C=C/C\C=C/C\C=C/C\C=C/C\C=C/CCCC([O-])=O SARHCLAXCDURCW-RSDXMDNYSA-N 0.000 claims description 7
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- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 1
- 235000017557 sodium bicarbonate Nutrition 0.000 description 1
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- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
- HRZFUMHJMZEROT-UHFFFAOYSA-L sodium disulfite Chemical compound [Na+].[Na+].[O-]S(=O)S([O-])(=O)=O HRZFUMHJMZEROT-UHFFFAOYSA-L 0.000 description 1
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- 239000008109 sodium starch glycolate Substances 0.000 description 1
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- 239000003549 soybean oil Substances 0.000 description 1
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- 239000008223 sterile water Substances 0.000 description 1
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- 125000004426 substituted alkynyl group Chemical group 0.000 description 1
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- WPLOVIFNBMNBPD-ATHMIXSHSA-N subtilin Chemical compound CC1SCC(NC2=O)C(=O)NC(CC(N)=O)C(=O)NC(C(=O)NC(CCCCN)C(=O)NC(C(C)CC)C(=O)NC(=C)C(=O)NC(CCCCN)C(O)=O)CSC(C)C2NC(=O)C(CC(C)C)NC(=O)C1NC(=O)C(CCC(N)=O)NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C1NC(=O)C(=C/C)/NC(=O)C(CCC(N)=O)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)CNC(=O)C(NC(=O)C(NC(=O)C2NC(=O)CNC(=O)C3CCCN3C(=O)C(NC(=O)C3NC(=O)C(CC(C)C)NC(=O)C(=C)NC(=O)C(CCC(O)=O)NC(=O)C(NC(=O)C(CCCCN)NC(=O)C(N)CC=4C5=CC=CC=C5NC=4)CSC3)C(C)SC2)C(C)C)C(C)SC1)CC1=CC=CC=C1 WPLOVIFNBMNBPD-ATHMIXSHSA-N 0.000 description 1
- 150000003460 sulfonic acids Chemical class 0.000 description 1
- 239000011593 sulfur Substances 0.000 description 1
- 125000004434 sulfur atom Chemical group 0.000 description 1
- 239000001117 sulphuric acid Substances 0.000 description 1
- 235000011149 sulphuric acid Nutrition 0.000 description 1
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- 239000004094 surface-active agent Substances 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 230000035488 systolic blood pressure Effects 0.000 description 1
- 230000008685 targeting Effects 0.000 description 1
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- 239000011975 tartaric acid Substances 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
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- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 description 1
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- 230000000699 topical effect Effects 0.000 description 1
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- 125000006168 tricyclic group Chemical group 0.000 description 1
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- GXPHKUHSUJUWKP-UHFFFAOYSA-N troglitazone Chemical compound C1CC=2C(C)=C(O)C(C)=C(C)C=2OC1(C)COC(C=C1)=CC=C1CC1SC(=O)NC1=O GXPHKUHSUJUWKP-UHFFFAOYSA-N 0.000 description 1
- GXPHKUHSUJUWKP-NTKDMRAZSA-N troglitazone Natural products C([C@@]1(OC=2C(C)=C(C(=C(C)C=2CC1)O)C)C)OC(C=C1)=CC=C1C[C@H]1SC(=O)NC1=O GXPHKUHSUJUWKP-NTKDMRAZSA-N 0.000 description 1
- 208000035408 type 1 diabetes mellitus 1 Diseases 0.000 description 1
- 238000009424 underpinning Methods 0.000 description 1
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- 230000002792 vascular Effects 0.000 description 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
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- 239000002676 xenobiotic agent Substances 0.000 description 1
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- 229940051223 zetia Drugs 0.000 description 1
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- 229910021511 zinc hydroxide Inorganic materials 0.000 description 1
- 229940007718 zinc hydroxide Drugs 0.000 description 1
- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/205—Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P3/06—Antihyperlipidemics
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/06—Antiarrhythmics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- 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
- C07C229/04—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 being acyclic and saturated
- C07C229/24—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 being acyclic and saturated having more than one carboxyl group bound to the carbon skeleton, e.g. aspartic acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C277/00—Preparation of guanidine or its derivatives, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
- C07C277/08—Preparation of guanidine or its derivatives, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups of substituted guanidines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
- C07C279/20—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups containing any of the groups, X being a hetero atom, Y being any atom, e.g. acylguanidines
- C07C279/24—Y being a hetero atom
- C07C279/26—X and Y being nitrogen atoms, i.e. biguanides
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Child & Adolescent Psychology (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261669763P | 2012-07-10 | 2012-07-10 | |
| US61/669,763 | 2012-07-10 | ||
| US201261670368P | 2012-07-11 | 2012-07-11 | |
| US201261670376P | 2012-07-11 | 2012-07-11 | |
| US61/670,368 | 2012-07-11 | ||
| US61/670,376 | 2012-07-11 | ||
| US13/841,970 US8765811B2 (en) | 2012-07-10 | 2013-03-15 | Tri-salt form of metformin |
| US13/841,970 | 2013-03-15 | ||
| PCT/US2013/049984 WO2014011814A1 (en) | 2012-07-10 | 2013-07-10 | Tri-salt form of metformin |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2878819A1 true CA2878819A1 (en) | 2014-01-16 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
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| CA2878819A Abandoned CA2878819A1 (en) | 2012-07-10 | 2013-07-10 | Tri-salt form of metformin |
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| EP (1) | EP2872483A4 (enExample) |
| JP (1) | JP2015523382A (enExample) |
| KR (1) | KR20150036235A (enExample) |
| CN (1) | CN104684889A (enExample) |
| AU (1) | AU2013290168A1 (enExample) |
| BR (1) | BR112015000368A2 (enExample) |
| CA (1) | CA2878819A1 (enExample) |
| IL (1) | IL236613A0 (enExample) |
| IN (1) | IN2015KN00076A (enExample) |
| MX (1) | MX2015000408A (enExample) |
| WO (1) | WO2014011814A1 (enExample) |
| ZA (1) | ZA201500274B (enExample) |
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| US8853259B2 (en) * | 2013-02-07 | 2014-10-07 | Banavara L. Mylari | Metformin derivatives for treating diabetes and diabetes complications |
| CA2947741A1 (en) | 2014-05-05 | 2015-11-12 | Thetis Pharmaceuticals Llc | Compositions and methods relating to ionic salts of peptides |
| BR112016029476A2 (pt) * | 2014-06-18 | 2017-08-22 | Thetis Pharmaceuticals Llc | complexos de aminoácido mineral de agentes ativos |
| US20170119841A1 (en) * | 2015-11-04 | 2017-05-04 | Thetis Pharmaceuticals Llc | Amino acid salts of unsaturated fatty acids |
| US10130719B2 (en) | 2016-06-03 | 2018-11-20 | Thetis Pharmaceuticals Llc | Compositions and methods relating to salts of specialized pro-resolving mediators |
| US10471963B2 (en) | 2017-04-07 | 2019-11-12 | TuSimple | System and method for transitioning between an autonomous and manual driving mode based on detection of a drivers capacity to control a vehicle |
| US10737695B2 (en) | 2017-07-01 | 2020-08-11 | Tusimple, Inc. | System and method for adaptive cruise control for low speed following |
| CN113105367B (zh) | 2021-03-30 | 2022-08-02 | 广州大学 | 一类二甲双胍盐及其制备方法和应用 |
| CN114349665B (zh) * | 2021-11-30 | 2023-06-09 | 潍坊博创国际生物医药研究院 | 二甲双胍焦谷氨酸晶体及其制备方法与应用 |
| CN116999398A (zh) * | 2022-06-30 | 2023-11-07 | 山东海赜生物科技有限公司 | 一种口服组合物 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
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| WO1999029314A1 (en) * | 1997-12-08 | 1999-06-17 | Bristol-Myers Squibb Company | Novel salts of metformin and method |
| FR2774591B1 (fr) * | 1998-02-12 | 2000-05-05 | Lipha | Composition pharmaceutique comprenant l'association metformine et fibrate et son utilisation pour la preparation de medicaments destines a reduire l'hyperglycemie |
| AU2001213150A1 (en) * | 2000-08-03 | 2002-02-18 | Olga Evgenievna Kolesova | Composition of metformin with succinic acid or salts thereof and method for treating diabetes |
| RU2356247C2 (ru) * | 2003-03-18 | 2009-05-27 | Новартис Аг | Комбинации и композиции, содержащие жирные кислоты и аминокислоты, их применение для предупреждения, замедления прогрессирования или лечения диабета и связанных с диабетом заболеваний и состояний, способ снижения веса тела млекопитающего, набор |
| EP1591114A1 (en) * | 2004-03-12 | 2005-11-02 | Fournier Laboratories Ireland Limited | Use of metformin and orlistat for the treatment or prevention of obesity |
| EP2203418B1 (en) * | 2007-09-21 | 2017-10-25 | HanAll Biopharma Co., Ltd. | N,n-dimethyl imidodicarbonimidic diamide dicarboxylate, method for producing the same and pharmaceutical compositions comprising the same |
| WO2009080022A1 (en) * | 2007-12-20 | 2009-07-02 | Fertin Pharma A/S | Compressed chewing gum tablet |
| JPWO2009151116A1 (ja) * | 2008-06-13 | 2011-11-17 | 持田製薬株式会社 | 非アルコール性脂肪肝炎の予防／改善・治療薬 |
| EP4008327A1 (en) * | 2009-04-29 | 2022-06-08 | Amarin Pharmaceuticals Ireland Limited | Pharmaceutical compositions comprising epa and a cardiovascular agent and methods of using the same |
| MX2013004364A (es) * | 2010-10-19 | 2013-07-02 | Elcelyx Therapeutics Inc | Terapias a base de ligando del receptor quimiosensorial. |
| US8796338B2 (en) * | 2011-01-07 | 2014-08-05 | Elcelyx Therapeutics, Inc | Biguanide compositions and methods of treating metabolic disorders |
| US20120178813A1 (en) * | 2011-01-12 | 2012-07-12 | Thetis Pharmaceuticals Llc | Lipid-lowering antidiabetic agent |
| US8853259B2 (en) * | 2013-02-07 | 2014-10-07 | Banavara L. Mylari | Metformin derivatives for treating diabetes and diabetes complications |
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2013
- 2013-07-10 EP EP13817534.4A patent/EP2872483A4/en not_active Withdrawn
- 2013-07-10 CA CA2878819A patent/CA2878819A1/en not_active Abandoned
- 2013-07-10 AU AU2013290168A patent/AU2013290168A1/en not_active Abandoned
- 2013-07-10 IN IN76KON2015 patent/IN2015KN00076A/en unknown
- 2013-07-10 MX MX2015000408A patent/MX2015000408A/es unknown
- 2013-07-10 JP JP2015521784A patent/JP2015523382A/ja active Pending
- 2013-07-10 WO PCT/US2013/049984 patent/WO2014011814A1/en not_active Ceased
- 2013-07-10 BR BR112015000368A patent/BR112015000368A2/pt not_active IP Right Cessation
- 2013-07-10 KR KR20157002264A patent/KR20150036235A/ko not_active Withdrawn
- 2013-07-10 CN CN201380046842.4A patent/CN104684889A/zh active Pending
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- 2015-01-14 ZA ZA2015/00274A patent/ZA201500274B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN104684889A (zh) | 2015-06-03 |
| EP2872483A1 (en) | 2015-05-20 |
| MX2015000408A (es) | 2015-07-14 |
| IN2015KN00076A (enExample) | 2015-07-31 |
| AU2013290168A1 (en) | 2015-02-05 |
| KR20150036235A (ko) | 2015-04-07 |
| IL236613A0 (en) | 2015-02-26 |
| ZA201500274B (en) | 2017-10-25 |
| BR112015000368A2 (pt) | 2017-06-27 |
| WO2014011814A1 (en) | 2014-01-16 |
| JP2015523382A (ja) | 2015-08-13 |
| EP2872483A4 (en) | 2016-03-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FZDE | Discontinued |
Effective date: 20180710 |