JP6418950B2 - ピラゾロ［１，５−ａ］ピリミジン系化合物、それを含む組成物、及びそれらを使用する方法 - Google Patents
ピラゾロ［１，５−ａ］ピリミジン系化合物、それを含む組成物、及びそれらを使用する方法 Download PDFInfo
- Publication number
- JP6418950B2 JP6418950B2 JP2014561024A JP2014561024A JP6418950B2 JP 6418950 B2 JP6418950 B2 JP 6418950B2 JP 2014561024 A JP2014561024 A JP 2014561024A JP 2014561024 A JP2014561024 A JP 2014561024A JP 6418950 B2 JP6418950 B2 JP 6418950B2
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- Japan
- Prior art keywords
- mmol
- pyrimidin
- compound
- pyrazolo
- pharmaceutically acceptable
- 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.)
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- 0 *c1ncccc1-c(cn[n]1cc2)c1nc2N1CCN(*)CC1 Chemical compound *c1ncccc1-c(cn[n]1cc2)c1nc2N1CCN(*)CC1 0.000 description 3
- MYZAFXMJEKLFIQ-UHFFFAOYSA-N Bc(cn[n]1cc2)c1nc2N(CC1)CCN1C(OC(C)COC)=O Chemical compound Bc(cn[n]1cc2)c1nc2N(CC1)CCN1C(OC(C)COC)=O MYZAFXMJEKLFIQ-UHFFFAOYSA-N 0.000 description 1
- PJOGGOJBEKHZLT-NSHDSACASA-N CC(C)(C)OC(N1[C@H](CNc(cc[n]2nc3)nc2c3I)CCC1)=O Chemical compound CC(C)(C)OC(N1[C@H](CNc(cc[n]2nc3)nc2c3I)CCC1)=O PJOGGOJBEKHZLT-NSHDSACASA-N 0.000 description 1
- GVKFEXUGJWJKKL-JSGCOSHPSA-N CC(C)C[C@@H](C(N(C)[C@@H](CC1)CN1c(cc[n]1nc2)nc1c2Br)=O)N Chemical compound CC(C)C[C@@H](C(N(C)[C@@H](CC1)CN1c(cc[n]1nc2)nc1c2Br)=O)N GVKFEXUGJWJKKL-JSGCOSHPSA-N 0.000 description 1
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Classifications
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- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/05—Isotopically modified compounds, e.g. labelled
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/002—Heterocyclic compounds
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- General Chemical & Material Sciences (AREA)
- Neurology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Rheumatology (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261608765P | 2012-03-09 | 2012-03-09 | |
| US61/608,765 | 2012-03-09 | ||
| PCT/US2013/029056 WO2013134228A1 (en) | 2012-03-09 | 2013-03-05 | PYRAZOLO[1,5-a]PYRIMIDINE-BASED COMPOUNDS, COMPOSITIONS COMPRISING THEM, AND METHODS OF THEIR USE |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015509535A JP2015509535A (ja) | 2015-03-30 |
| JP2015509535A5 JP2015509535A5 (OSRAM) | 2016-04-21 |
| JP6418950B2 true JP6418950B2 (ja) | 2018-11-07 |
Family
ID=47892052
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014561024A Active JP6418950B2 (ja) | 2012-03-09 | 2013-03-05 | ピラゾロ［１，５−ａ］ピリミジン系化合物、それを含む組成物、及びそれらを使用する方法 |
Country Status (25)
| Country | Link |
|---|---|
| US (3) | US8946415B2 (OSRAM) |
| EP (1) | EP2834243B1 (OSRAM) |
| JP (1) | JP6418950B2 (OSRAM) |
| KR (1) | KR101965025B1 (OSRAM) |
| CN (1) | CN104302649B (OSRAM) |
| AR (1) | AR090292A1 (OSRAM) |
| AU (1) | AU2013230128B2 (OSRAM) |
| BR (1) | BR112014022000A8 (OSRAM) |
| CA (1) | CA2866143C (OSRAM) |
| DK (1) | DK2834243T3 (OSRAM) |
| ES (1) | ES2676224T3 (OSRAM) |
| HU (1) | HUE038786T2 (OSRAM) |
| IL (1) | IL234486A (OSRAM) |
| IN (1) | IN2014DN07384A (OSRAM) |
| MX (2) | MX381849B (OSRAM) |
| NZ (1) | NZ630721A (OSRAM) |
| PL (1) | PL2834243T3 (OSRAM) |
| PT (1) | PT2834243T (OSRAM) |
| RU (1) | RU2014140735A (OSRAM) |
| SG (1) | SG11201405561RA (OSRAM) |
| TR (1) | TR201808280T4 (OSRAM) |
| TW (1) | TW201341386A (OSRAM) |
| UY (1) | UY34668A (OSRAM) |
| WO (1) | WO2013134228A1 (OSRAM) |
| ZA (1) | ZA201406149B (OSRAM) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112014022000A8 (pt) | 2012-03-09 | 2021-06-15 | Lexicon Pharmaceuticals Inc | compostos à base de pirazol[1,5-a]pirimidina, seu uso e composições que os compreende |
| EP2822559B1 (en) | 2012-03-09 | 2018-05-02 | Lexicon Pharmaceuticals, Inc. | Imidazo[1,2-b]pyridazine-based compounds, compositions comprising them, and uses thereof |
| US8901305B2 (en) | 2012-07-31 | 2014-12-02 | Bristol-Myers Squibb Company | Aryl lactam kinase inhibitors |
| JP2016509066A (ja) | 2013-02-22 | 2016-03-24 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | アダプター関連キナーゼ１（ａａｋ１）の阻害剤としての５ｈ−クロメノ［３，４−ｃ］ピリジン |
| TW201542550A (zh) * | 2013-09-06 | 2015-11-16 | Lexicon Pharmaceuticals Inc | 吡唑并［１，５－ａ］嘧啶基化合物、包含彼之組合物以及使用彼之方法 |
| ES2678877T3 (es) | 2013-10-11 | 2018-08-20 | Bristol-Myers Squibb Company | Inhibidores de pirrolotriazina quinasa |
| RS59059B1 (sr) | 2014-01-24 | 2019-08-30 | Turning Point Therapeutics Inc | Diaril makrociklična jedinjenja kao modulatori protein kinaza |
| CN106132951B (zh) * | 2014-01-31 | 2019-02-12 | 百时美施贵宝公司 | 基于喹啉的激酶抑制剂 |
| TW201620911A (zh) * | 2014-03-17 | 2016-06-16 | 雷西肯製藥股份有限公司 | 銜接子關聯激酶１之抑制劑、包含其之組成物、及其使用方法 |
| EP3200797A1 (en) * | 2014-09-30 | 2017-08-09 | Bristol-Myers Squibb Company | Quinazoline-based kinase inhibitors |
| HUE067779T2 (hu) * | 2014-12-15 | 2024-11-28 | Cmg Pharmaceutical Co Ltd | Kondenzált gyûrûs heteroaril vegyületek és azok felhasználása TRK inhibitorokként |
| EP3292124B1 (en) | 2015-04-10 | 2019-05-22 | Bristol-Myers Squibb Company | 6h-isochromeno[3,4-c]pyridines and benzo[c][1,7]naphthyridin-6-(5h)-ones as adaptor associated kinase 1 (aak1) inhibitors |
| CN107735399B (zh) | 2015-07-02 | 2021-01-26 | 特普医药公司 | 作为蛋白质激酶的调节剂的手性二芳基大环 |
| PL3319969T3 (pl) | 2015-07-06 | 2024-06-24 | Turning Point Therapeutics, Inc. | Diarylowe polimorfy makrocykliczne |
| RU2020123800A (ru) | 2015-07-21 | 2020-10-02 | Тёрнинг Поинт Терапьютикс, Инк. | Хиральные диарильные макроциклы и их применение |
| CN108349979B (zh) | 2015-11-02 | 2021-04-09 | 詹森药业有限公司 | [1,2,4]三唑并[1,5-a]嘧啶-7-基化合物 |
| AU2017302019A1 (en) | 2016-07-28 | 2019-02-07 | Turning Point Therapeutics, Inc. | Macrocycle kinase inhibitors |
| TWI764950B (zh) * | 2016-11-02 | 2022-05-21 | 比利時商健生藥品公司 | Ｐｄｅ２抑制劑 |
| EA039847B1 (ru) | 2016-11-02 | 2022-03-18 | Янссен Фармацевтика Нв | СОЕДИНЕНИЯ [1,2,4]ТРИАЗОЛО[1,5-a]ПИРИМИДИНА В КАЧЕСТВЕ ИНГИБИТОРОВ PDE2 |
| BR112019008163A2 (pt) | 2016-11-02 | 2019-07-09 | Janssen Pharmaceutica Nv | compostos de [1,2,4]triazolo[1,5-a]pirimidina como inibidores de pde2 |
| TWI808958B (zh) | 2017-01-25 | 2023-07-21 | 美商特普醫葯公司 | 涉及二芳基巨環化合物之組合療法 |
| DK3658557T3 (da) | 2017-07-28 | 2024-07-29 | Takeda Pharmaceuticals Co | Tyk2-inhibitorer og anvendelser deraf |
| KR102645316B1 (ko) | 2017-07-28 | 2024-03-07 | 터닝 포인트 테라퓨틱스, 인크. | 거대환형 화합물 및 이의 용도 |
| MX2020006293A (es) * | 2017-12-15 | 2020-12-03 | Pyramid Biosciences Inc | Derivados de 5-(2-2,5-difluorofenil)pirrolidin-1-il)-3-(1h-pirazol -1-il)pirazolo[1,5-a]pirimidina y compuestos relacionados como inhibidores de trk cinasa para el tratamiento de cancer. |
| JP7194188B2 (ja) | 2017-12-19 | 2022-12-21 | ターニング・ポイント・セラピューティクス・インコーポレイテッド | 疾患を治療するための大環状化合物 |
| JP7150356B2 (ja) * | 2017-12-22 | 2022-10-11 | 深▲チェン▼市塔吉瑞生物医薬有限公司 | 置換ピラゾロ［１，５－ａ］ピリミジン化合物並びにその医薬組成物および使用 |
| EP3744723B1 (en) | 2018-01-23 | 2023-10-18 | Shenzhen TargetRx, Inc. | Substituted pyrazolo[1,5-a]pyrimidine macrocyclic compound |
| US20220041588A1 (en) * | 2018-09-27 | 2022-02-10 | Fochon Pharmaceuticals, Ltd. | Substituted imidazo[1,2-a]pyridine and [1,2,4]triazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
| JP7619951B2 (ja) * | 2018-10-15 | 2025-01-22 | 武田薬品工業株式会社 | Ｔｙｋ２阻害剤およびその使用 |
| CA3175973A1 (en) * | 2020-04-21 | 2021-10-28 | Lexicon Pharmaceuticals, Inc. | 4-(3-(pyridin-3-yl)pyrazolo[1,5-a]pyrimidin-5-yl)piperazine for use in the the treatment of cov-229e or cov-oc43 coronaviruses infections |
| CA3175970A1 (en) | 2020-04-21 | 2021-10-28 | Suma GOPINATHAN | Aak1 inhibitors for use in treating viral infections |
| US11478733B2 (en) | 2020-11-24 | 2022-10-25 | Caterpillar Inc. | Filter interlock with tabs mating with a pedestal or a housing |
| WO2025054448A1 (en) * | 2023-09-08 | 2025-03-13 | Satellos Bioscience Inc. | Ap2 associated kinase 1 inhibitors and uses thereof |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5464764A (en) | 1989-08-22 | 1995-11-07 | University Of Utah Research Foundation | Positive-negative selection methods and vectors |
| WO1993004169A1 (en) | 1991-08-20 | 1993-03-04 | Genpharm International, Inc. | Gene targeting in animal cells using isogenic dna constructs |
| US6194410B1 (en) * | 1998-03-11 | 2001-02-27 | Hoffman-La Roche Inc. | Pyrazolopyrimidine and pyrazolines and process for preparation thereof |
| JP4847275B2 (ja) * | 2005-10-21 | 2011-12-28 | 田辺三菱製薬株式会社 | ピラゾロ［１，５−ａ］ピリミジン化合物 |
| KR20090073121A (ko) | 2006-09-29 | 2009-07-02 | 노파르티스 아게 | Ｐｉ3ｋ 지질 키나제 억제제로서의 피라졸로피리미딘 |
| US20120058997A1 (en) * | 2006-11-06 | 2012-03-08 | Supergen, Inc. | Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors |
| AU2009246687B2 (en) * | 2008-05-13 | 2012-08-09 | Irm Llc | Fused nitrogen containing heterocycles and compositions thereof as kinase inhibitors |
| BRPI0919873B8 (pt) * | 2008-10-22 | 2021-05-25 | Array Biopharma Inc | compostos de pirazol[1,5-a]pirimidina substituídos como inibidores da trk quinase, seus processos de preparação e composições farmacêuticas |
| AR077468A1 (es) * | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| US8865726B2 (en) | 2009-09-03 | 2014-10-21 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyrimidine compounds as mTOR inhibitors |
| EP2523552B1 (en) * | 2010-01-14 | 2015-05-13 | Merck Sharp & Dohme Corp. | Pyrazolo[1,5-a]pyrimidines as mark inhibitors |
| ES2671748T3 (es) * | 2011-07-21 | 2018-06-08 | Tolero Pharmaceuticals, Inc. | Inhibidores heterocíclicos de proteína quinasas |
| BR112014022000A8 (pt) | 2012-03-09 | 2021-06-15 | Lexicon Pharmaceuticals Inc | compostos à base de pirazol[1,5-a]pirimidina, seu uso e composições que os compreende |
| AU2013230066A1 (en) * | 2012-03-09 | 2014-09-25 | Lexicon Pharmaceuticals, Inc. | Inhibition of adaptor associated kinase 1 for the treatment of pain |
| EP2822559B1 (en) | 2012-03-09 | 2018-05-02 | Lexicon Pharmaceuticals, Inc. | Imidazo[1,2-b]pyridazine-based compounds, compositions comprising them, and uses thereof |
| TW201620911A (zh) * | 2014-03-17 | 2016-06-16 | 雷西肯製藥股份有限公司 | 銜接子關聯激酶１之抑制劑、包含其之組成物、及其使用方法 |
-
2013
- 2013-03-05 BR BR112014022000A patent/BR112014022000A8/pt not_active Application Discontinuation
- 2013-03-05 ES ES13710250.5T patent/ES2676224T3/es active Active
- 2013-03-05 HU HUE13710250A patent/HUE038786T2/hu unknown
- 2013-03-05 PL PL13710250T patent/PL2834243T3/pl unknown
- 2013-03-05 DK DK13710250.5T patent/DK2834243T3/en active
- 2013-03-05 PT PT137102505T patent/PT2834243T/pt unknown
- 2013-03-05 IN IN7384DEN2014 patent/IN2014DN07384A/en unknown
- 2013-03-05 CA CA2866143A patent/CA2866143C/en active Active
- 2013-03-05 AU AU2013230128A patent/AU2013230128B2/en active Active
- 2013-03-05 WO PCT/US2013/029056 patent/WO2013134228A1/en not_active Ceased
- 2013-03-05 EP EP13710250.5A patent/EP2834243B1/en active Active
- 2013-03-05 NZ NZ630721A patent/NZ630721A/en unknown
- 2013-03-05 MX MX2017002117A patent/MX381849B/es unknown
- 2013-03-05 JP JP2014561024A patent/JP6418950B2/ja active Active
- 2013-03-05 SG SG11201405561RA patent/SG11201405561RA/en unknown
- 2013-03-05 TR TR2018/08280T patent/TR201808280T4/tr unknown
- 2013-03-05 KR KR1020147028071A patent/KR101965025B1/ko active Active
- 2013-03-05 US US13/785,355 patent/US8946415B2/en active Active
- 2013-03-05 MX MX2014010589A patent/MX345830B/es active IP Right Grant
- 2013-03-05 RU RU2014140735A patent/RU2014140735A/ru not_active Application Discontinuation
- 2013-03-05 CN CN201380012483.0A patent/CN104302649B/zh active Active
- 2013-03-08 TW TW102108283A patent/TW201341386A/zh unknown
- 2013-03-11 AR ARP130100765A patent/AR090292A1/es unknown
- 2013-03-11 UY UY0001034668A patent/UY34668A/es not_active Application Discontinuation
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2014
- 2014-08-21 ZA ZA2014/06149A patent/ZA201406149B/en unknown
- 2014-09-07 IL IL234486A patent/IL234486A/en active IP Right Grant
- 2014-09-11 US US14/483,898 patent/US9403832B2/en active Active
-
2016
- 2016-07-12 US US15/207,677 patent/US20170129896A1/en not_active Abandoned
Also Published As
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