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
- 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)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Rheumatology (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) | MX345830B (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 |
|---|---|---|---|---|
| US8946415B2 (en) | 2012-03-09 | 2015-02-03 | Lexicon Pharmaceuticals, Inc. | Pyrazolo[1,5-a]pyrimidine-based compounds, compositions comprising them, and methods of their use |
| US8969565B2 (en) | 2012-03-09 | 2015-03-03 | Lexicon Pharmaceuticals, Inc. | Imidazo[1,2-b]pyridazine-based compounds, compositions comprising them, and methods of their use |
| US8901305B2 (en) | 2012-07-31 | 2014-12-02 | Bristol-Myers Squibb Company | Aryl lactam kinase inhibitors |
| EP2958924B1 (en) | 2013-02-22 | 2016-12-28 | Bristol-Myers Squibb Company | 5h-chromeno[3,4-c]pyridines as inhibitors of adaptor associated kinase 1 (aak1) |
| 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 |
| WO2015054358A1 (en) | 2013-10-11 | 2015-04-16 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| US9714258B2 (en) | 2014-01-24 | 2017-07-25 | Tp Therapeutics, Inc. | Diaryl macrocycles as modulators of protein kinases |
| EA201691397A1 (ru) * | 2014-01-31 | 2016-11-30 | Бристол-Майерс Сквибб Компани | Хинолиновые ингибиторы киназы |
| 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 |
| KR20240055170A (ko) * | 2014-12-15 | 2024-04-26 | 주식회사 씨엠지제약 | 융합된 고리 헤테로아릴 화합물 및 trk 억제제로서의 이들의 용도 |
| 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 |
| JP6871903B2 (ja) | 2015-07-02 | 2021-05-19 | 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Ｔｕｒｎｉｎｇ Ｐｏｉｎｔ Ｔｈｅｒａｐｅｕｔｉｃｓ，Ｉｎｃ． | プロテインキナーゼのモジュレーターとしてのキラルジアリール大環状分子 |
| WO2017007759A1 (en) | 2015-07-06 | 2017-01-12 | Tp Therapeutics, Inc. | Diaryl macrocycle polymorph |
| PT3733187T (pt) | 2015-07-21 | 2024-11-08 | Turning Point Therapeutics Inc | Macrociclo de diarilo quiral e utilização do mesmo no tratamento do cancro |
| KR20180075630A (ko) * | 2015-11-02 | 2018-07-04 | 얀센 파마슈티카 엔.브이. | [1,2,4]트리아졸로[1,5-a]피리미딘-7-일 화합물 |
| JP2019527230A (ja) | 2016-07-28 | 2019-09-26 | 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Ｔｕｒｎｉｎｇ Ｐｏｉｎｔ Ｔｈｅｒａｐｅｕｔｉｃｓ，Ｉｎｃ． | 大環状キナーゼ阻害剤 |
| CN109890824B (zh) | 2016-11-02 | 2022-05-24 | 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 |
| ES2855032T3 (es) | 2016-11-02 | 2021-09-23 | Janssen Pharmaceutica Nv | Compuestos de [1,2,4]triazolo[1,5-a]pirimidina como inhibidores de PDE2 |
| US10947242B2 (en) * | 2016-11-02 | 2021-03-16 | Janssen Pharmaceutica, Nv | [1,2,4]triazolo[1,5and#8208;A]pyrimidine compounds as PDE2 inhibitors |
| 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 |
| HRP20241197T1 (hr) | 2017-07-28 | 2024-11-22 | Turning Point Therapeutics, Inc. | Makrociklični spojevi i primjene istih |
| ES2994013T3 (en) | 2017-07-28 | 2025-01-15 | Takeda Pharmaceuticals Co | Tyk2 inhibitors and uses thereof |
| DK3724191T3 (da) * | 2017-12-15 | 2022-03-14 | Pyramid Biosciences Inc | 5-(2-(2,5-difluorphenyl)pyrrolidin-1-yl)-3-(1h-pyrazol-1-yl)pyrazol[1,5-a]pyrimidinderivater og lignende forbindelser som trk-kinasehæmmere til cancerbehandling |
| PL3728271T3 (pl) | 2017-12-19 | 2023-01-23 | Turning Point Therapeutics, Inc. | Związki makrocykliczne do leczenia chorób |
| CN109456331B (zh) | 2017-12-22 | 2020-06-05 | 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 |
| EP3744723B1 (en) | 2018-01-23 | 2023-10-18 | Shenzhen TargetRx, Inc. | Substituted pyrazolo[1,5-a]pyrimidine macrocyclic compound |
| TW202028209A (zh) * | 2018-09-27 | 2020-08-01 | 大陸商重慶複創醫藥研究有限公司 | 作為RET激酶抑制劑的取代的咪唑[1,2-a]吡啶和[1,2,4]三唑[1,5-a]吡啶化合物 |
| AU2019360941B2 (en) * | 2018-10-15 | 2025-02-27 | Takeda Pharmaceutical Company Limited | TYK2 inhibitors and uses thereof |
| US11730723B2 (en) | 2020-04-21 | 2023-08-22 | Lexicon Pharmaceuticals, Inc. | Compounds and methods for treating viral infections |
| 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 |
| US11478733B2 (en) | 2020-11-24 | 2022-10-25 | Caterpillar Inc. | Filter interlock with tabs mating with a pedestal or a housing |
| US20250122207A1 (en) * | 2023-09-08 | 2025-04-17 | 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 |
| 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 |
| JP2010504933A (ja) | 2006-09-29 | 2010-02-18 | ノバルティス アーゲー | Ｐｉ３ｋ脂質キナーゼ阻害剤としてのピラゾロピリミジン |
| 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 |
| BRPI0912668A2 (pt) * | 2008-05-13 | 2016-01-26 | Irm Llc | composto e composições como inibidores de quinase |
| ES2900243T3 (es) * | 2008-10-22 | 2022-03-16 | Array Biopharma Inc | Compuestos de pirazolo[1,5-a]pirimidina sustituidos como inhibidores de trk quinasa |
| 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 |
| WO2011087999A1 (en) | 2010-01-14 | 2011-07-21 | Merck Sharp & Dohme Corp. | Pyrazolo[1,5-a]pyrimidines as mark inhibitors |
| PT3409278T (pt) * | 2011-07-21 | 2020-12-18 | Sumitomo Dainippon Pharma Oncology Inc | Inibidores de proteína cinase heterocíclicos |
| US8969565B2 (en) | 2012-03-09 | 2015-03-03 | Lexicon Pharmaceuticals, Inc. | Imidazo[1,2-b]pyridazine-based compounds, compositions comprising them, and methods of their use |
| US8946415B2 (en) | 2012-03-09 | 2015-02-03 | Lexicon Pharmaceuticals, Inc. | Pyrazolo[1,5-a]pyrimidine-based compounds, compositions comprising them, and methods of their use |
| WO2013134336A2 (en) | 2012-03-09 | 2013-09-12 | Lexicon Pharmaceuticals, Inc. | Inhibition of adaptor associated kinase 1 for the treatment of pain |
| 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 US US13/785,355 patent/US8946415B2/en active Active
- 2013-03-05 ES ES13710250.5T patent/ES2676224T3/es active Active
- 2013-03-05 MX MX2014010589A patent/MX345830B/es active IP Right Grant
- 2013-03-05 IN IN7384DEN2014 patent/IN2014DN07384A/en unknown
- 2013-03-05 HU HUE13710250A patent/HUE038786T2/hu unknown
- 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 KR KR1020147028071A patent/KR101965025B1/ko active Active
- 2013-03-05 CA CA2866143A patent/CA2866143C/en active Active
- 2013-03-05 AU AU2013230128A patent/AU2013230128B2/en active Active
- 2013-03-05 TR TR2018/08280T patent/TR201808280T4/tr unknown
- 2013-03-05 NZ NZ630721A patent/NZ630721A/en unknown
- 2013-03-05 RU RU2014140735A patent/RU2014140735A/ru not_active Application Discontinuation
- 2013-03-05 EP EP13710250.5A patent/EP2834243B1/en active Active
- 2013-03-05 CN CN201380012483.0A patent/CN104302649B/zh active Active
- 2013-03-05 WO PCT/US2013/029056 patent/WO2013134228A1/en not_active Ceased
- 2013-03-05 DK DK13710250.5T patent/DK2834243T3/en active
- 2013-03-05 PT PT137102505T patent/PT2834243T/pt unknown
- 2013-03-05 SG SG11201405561RA patent/SG11201405561RA/en unknown
- 2013-03-05 PL PL13710250T patent/PL2834243T3/pl 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
-
2016
- 2016-07-12 US US15/207,677 patent/US20170129896A1/en not_active Abandoned
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