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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- Prior art keywords
- mmol
- pyrimidin
- compound
- pyrazolo
- pharmaceutically acceptable
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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)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (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 (enExample) | 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 (enExample) |
| EP (1) | EP2834243B1 (enExample) |
| JP (1) | JP6418950B2 (enExample) |
| KR (1) | KR101965025B1 (enExample) |
| CN (1) | CN104302649B (enExample) |
| AR (1) | AR090292A1 (enExample) |
| AU (1) | AU2013230128B2 (enExample) |
| BR (1) | BR112014022000A8 (enExample) |
| CA (1) | CA2866143C (enExample) |
| DK (1) | DK2834243T3 (enExample) |
| ES (1) | ES2676224T3 (enExample) |
| HU (1) | HUE038786T2 (enExample) |
| IL (1) | IL234486A (enExample) |
| IN (1) | IN2014DN07384A (enExample) |
| MX (2) | MX381849B (enExample) |
| NZ (1) | NZ630721A (enExample) |
| PL (1) | PL2834243T3 (enExample) |
| PT (1) | PT2834243T (enExample) |
| RU (1) | RU2014140735A (enExample) |
| SG (1) | SG11201405561RA (enExample) |
| TR (1) | TR201808280T4 (enExample) |
| TW (1) | TW201341386A (enExample) |
| UY (1) | UY34668A (enExample) |
| WO (1) | WO2013134228A1 (enExample) |
| ZA (1) | ZA201406149B (enExample) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102085121B1 (ko) | 2012-03-09 | 2020-03-05 | 렉시컨 파마슈티컬스 인코퍼레이티드 | 이미다조[1,2-b]피리다진계 화합물, 그를 포함하는 조성물 및 그의 용도 |
| RU2014140735A (ru) | 2012-03-09 | 2016-04-27 | Лексикон Фармасьютикалз, Инк. | ПРОИЗВОДНЫЕ ПИРАЗОЛО[1, 5-a]ПИРИМИДИНА, КОМПОЗИЦИИ, СОДЕРЖАЩИЕ УКАЗАННЫЕ СОЕДИНЕНИЯ, И СПОСОБЫ ИХ ПРИМЕНЕНИЯ |
| US8901305B2 (en) | 2012-07-31 | 2014-12-02 | Bristol-Myers Squibb Company | Aryl lactam kinase inhibitors |
| US9708337B2 (en) | 2013-02-22 | 2017-07-18 | Bristol-Myers Squibb Company | Aryl amide-based kinase inhibitors |
| 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 |
| PL3097107T3 (pl) | 2014-01-24 | 2020-01-31 | Turning Point Therapeutics, Inc. | Diarylowe związki makrocykliczne jako modulatory kinaz białkowych |
| MX2016009352A (es) * | 2014-01-31 | 2016-10-13 | Bristol Myers Squibb Co | Inhibidores de quinasa a base de quinolina. |
| 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 |
| US20170239249A1 (en) * | 2014-09-30 | 2017-08-24 | Bristol-Myers Squibb Company | Quinazoline-based kinase inhibitors |
| EP4420732A3 (en) * | 2014-12-15 | 2024-11-27 | CMG Pharmaceutical Co., Ltd. | Fused ring heteroaryl compounds and their use as trk inhibitors |
| WO2016164295A2 (en) | 2015-04-10 | 2016-10-13 | Bristol-Myers Squibb Company | Fused pyridines as kinase inhibitors |
| AU2016287568B2 (en) | 2015-07-02 | 2020-08-20 | Turning Point Therapeutics, Inc. | Chiral diaryl macrocycles as modulators of protein kinases |
| HRP20240780T1 (hr) | 2015-07-06 | 2024-09-13 | Turning Point Therapeutics, Inc. | Polimorf diaril makrocikla |
| KR102772574B1 (ko) | 2015-07-21 | 2025-02-24 | 터닝 포인트 테라퓨틱스, 인크. | 키랄 디아릴 매크로사이클 및 이것의 용도 |
| SG11201803605YA (en) * | 2015-11-02 | 2018-05-30 | Janssen Pharmaceutica Nv | [1,2,4]TRIAZOLO[1,5-a]PYRIMIDIN-7-YL COMPOUND |
| RU2019105587A (ru) | 2016-07-28 | 2020-08-28 | Тёрнинг Поинт Терапьютикс, Инк. | Макроциклические ингибиторы киназ |
| BR112019008604A2 (pt) | 2016-11-02 | 2019-07-09 | Janssen Pharmaceutica Nv | compostos de [1,2,4]triazolo[1,5-a]pirimidina como inibidores de pde2 |
| CN109937202B (zh) | 2016-11-02 | 2022-12-30 | 詹森药业有限公司 | 作为pde2抑制剂的[1,2,4]三唑并[1,5-a]嘧啶化合物 |
| MX385576B (es) * | 2016-11-02 | 2025-03-18 | Janssen Pharmaceutica Nv | Derivados de [1,2,4]triazol[1,5-a]pirimidina como inhibidores 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 |
| MY205416A (en) | 2017-07-28 | 2024-10-21 | Takeda Pharmaceuticals Co | Tyk2 inhibitors and uses thereof |
| JP7224334B2 (ja) | 2017-07-28 | 2023-02-17 | 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 | 大環式化合物およびその使用 |
| JP7321183B2 (ja) * | 2017-12-15 | 2023-08-04 | ピラミッド バイオサイエンシズ インコーポレイテッド | がんを治療するためのｔｒｋキナーゼ阻害物質としての、５－（２－（２，５－ジフルオロフェニル）ピロリジン－１－イル）－３－（１ｈ－ピラゾール－１－イル）ピラゾロ［１，５－ａ］ピリミジン誘導体及び関連する化合物 |
| SI3728271T1 (sl) | 2017-12-19 | 2023-01-31 | Turning Point Therapeutics, Inc. | Makrociklične spojine za zdravljenje bolezni |
| CN111362949B (zh) | 2017-12-22 | 2021-12-21 | 深圳市塔吉瑞生物医药有限公司 | 一种取代的吡唑并[1,5-a]嘧啶化合物及其药物组合物及用途 |
| CN111848622A (zh) | 2018-01-23 | 2020-10-30 | 深圳市塔吉瑞生物医药有限公司 | 取代的吡唑并[1,5-a]嘧啶类的大环化合物 |
| EP3856743A4 (en) * | 2018-09-27 | 2022-06-15 | Fochon Pharmaceuticals, Ltd. | SUBSTITUTED IMIDAZO[1,2-A]PYRIDINE AND [1,2,4]TRIAZOLO[1,5-A]PYRIDINE COMPOUNDS AS RET KINASE INHIBITORS |
| CN113271940A (zh) * | 2018-10-15 | 2021-08-17 | 林伯士拉克许米公司 | Tyk2抑制剂和其用途 |
| EP4138844A1 (en) * | 2020-04-21 | 2023-03-01 | 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 |
| WO2021216441A1 (en) | 2020-04-21 | 2021-10-28 | Lexicon Pharmaceuticals, Inc. | 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 |
| TW202525819A (zh) * | 2023-09-08 | 2025-07-01 | 加拿大商薩泰洛斯生物科學公司 | Ａｐ２相關激酶１抑制劑及其用途 |
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 |
| AU2515992A (en) | 1991-08-20 | 1993-03-16 | 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 |
| WO2009140128A2 (en) * | 2008-05-13 | 2009-11-19 | Irm Llc | Compounds and compositions as kinase inhibitors |
| SG196855A1 (en) * | 2008-10-22 | 2014-02-13 | Array Biopharma Inc | Substituted pyrazolo[1,5-a]pyrimidine compounds as trk kinase inhibitors |
| 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 |
| ES2834093T3 (es) * | 2011-07-21 | 2021-06-16 | Sumitomo Dainippon Pharma Oncology Inc | Inhibidores de proteína quinasa heterocíclicos |
| HUE036040T2 (hu) * | 2012-03-09 | 2018-06-28 | Lexicon Pharmaceuticals Inc | Adaptor-asszociált kináz 1 gátlása fájdalom kezelésére |
| RU2014140735A (ru) | 2012-03-09 | 2016-04-27 | Лексикон Фармасьютикалз, Инк. | ПРОИЗВОДНЫЕ ПИРАЗОЛО[1, 5-a]ПИРИМИДИНА, КОМПОЗИЦИИ, СОДЕРЖАЩИЕ УКАЗАННЫЕ СОЕДИНЕНИЯ, И СПОСОБЫ ИХ ПРИМЕНЕНИЯ |
| KR102085121B1 (ko) | 2012-03-09 | 2020-03-05 | 렉시컨 파마슈티컬스 인코퍼레이티드 | 이미다조[1,2-b]피리다진계 화합물, 그를 포함하는 조성물 및 그의 용도 |
| 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 |
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2013
- 2013-03-05 RU RU2014140735A patent/RU2014140735A/ru not_active Application Discontinuation
- 2013-03-05 ES ES13710250.5T patent/ES2676224T3/es active Active
- 2013-03-05 CN CN201380012483.0A patent/CN104302649B/zh active Active
- 2013-03-05 MX MX2017002117A patent/MX381849B/es unknown
- 2013-03-05 BR BR112014022000A patent/BR112014022000A8/pt not_active Application Discontinuation
- 2013-03-05 JP JP2014561024A patent/JP6418950B2/ja active Active
- 2013-03-05 IN IN7384DEN2014 patent/IN2014DN07384A/en unknown
- 2013-03-05 MX MX2014010589A patent/MX345830B/es active IP Right Grant
- 2013-03-05 AU AU2013230128A patent/AU2013230128B2/en active Active
- 2013-03-05 HU HUE13710250A patent/HUE038786T2/hu unknown
- 2013-03-05 PT PT137102505T patent/PT2834243T/pt unknown
- 2013-03-05 NZ NZ630721A patent/NZ630721A/en unknown
- 2013-03-05 EP EP13710250.5A patent/EP2834243B1/en active Active
- 2013-03-05 WO PCT/US2013/029056 patent/WO2013134228A1/en not_active Ceased
- 2013-03-05 CA CA2866143A patent/CA2866143C/en active Active
- 2013-03-05 DK DK13710250.5T patent/DK2834243T3/en active
- 2013-03-05 KR KR1020147028071A patent/KR101965025B1/ko active Active
- 2013-03-05 SG SG11201405561RA patent/SG11201405561RA/en unknown
- 2013-03-05 US US13/785,355 patent/US8946415B2/en active Active
- 2013-03-05 PL PL13710250T patent/PL2834243T3/pl unknown
- 2013-03-05 TR TR2018/08280T patent/TR201808280T4/tr unknown
- 2013-03-08 TW TW102108283A patent/TW201341386A/zh unknown
- 2013-03-11 UY UY0001034668A patent/UY34668A/es not_active Application Discontinuation
- 2013-03-11 AR ARP130100765A patent/AR090292A1/es unknown
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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
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2016
- 2016-07-12 US US15/207,677 patent/US20170129896A1/en not_active Abandoned
Also Published As
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