JP2013539795A5 - - Google Patents
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- JP2013539795A5 JP2013539795A5 JP2013534053A JP2013534053A JP2013539795A5 JP 2013539795 A5 JP2013539795 A5 JP 2013539795A5 JP 2013534053 A JP2013534053 A JP 2013534053A JP 2013534053 A JP2013534053 A JP 2013534053A JP 2013539795 A5 JP2013539795 A5 JP 2013539795A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkynyl
- alkenyl
- cancer
- atoms
- 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.)
- Pending
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- 125000000623 heterocyclic group Chemical group 0.000 claims 37
- 125000000217 alkyl group Chemical group 0.000 claims 32
- 229910052739 hydrogen Inorganic materials 0.000 claims 23
- 125000003342 alkenyl group Chemical group 0.000 claims 22
- 125000000304 alkynyl group Chemical group 0.000 claims 22
- -1 cycloalkynyl Chemical group 0.000 claims 18
- 229940124597 therapeutic agent Drugs 0.000 claims 18
- 239000012830 cancer therapeutic Substances 0.000 claims 17
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 16
- 125000000753 cycloalkyl group Chemical group 0.000 claims 16
- 125000004404 heteroalkyl group Chemical group 0.000 claims 16
- 229910052731 fluorine Inorganic materials 0.000 claims 15
- 125000003118 aryl group Chemical group 0.000 claims 14
- 125000001072 heteroaryl group Chemical group 0.000 claims 14
- 229910052799 carbon Inorganic materials 0.000 claims 13
- 229910052736 halogen Inorganic materials 0.000 claims 13
- 150000002367 halogens Chemical class 0.000 claims 13
- 125000003545 alkoxy group Chemical group 0.000 claims 12
- 125000004429 atom Chemical group 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 12
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 8
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 7
- 206010028980 Neoplasm Diseases 0.000 claims 7
- 201000011510 cancer Diseases 0.000 claims 7
- 125000004430 oxygen atom Chemical group O* 0.000 claims 7
- 102000001301 EGF receptor Human genes 0.000 claims 6
- 108060006698 EGF receptor Proteins 0.000 claims 6
- 125000003302 alkenyloxy group Chemical group 0.000 claims 6
- 229910052801 chlorine Inorganic materials 0.000 claims 6
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 6
- 125000001424 substituent group Chemical group 0.000 claims 6
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 5
- 125000005842 heteroatom Chemical group 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- 229910052717 sulfur Inorganic materials 0.000 claims 5
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 4
- 229910052794 bromium Inorganic materials 0.000 claims 4
- 229910052740 iodine Inorganic materials 0.000 claims 4
- 239000000126 substance Substances 0.000 claims 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 3
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 125000001188 haloalkyl group Chemical group 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 230000035772 mutation Effects 0.000 claims 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 2
- 229910052698 phosphorus Inorganic materials 0.000 claims 2
- 125000002572 propoxy group Chemical group [*]OC([H])([H])C(C([H])([H])[H])([H])[H] 0.000 claims 2
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 239000005411 L01XE02 - Gefitinib Substances 0.000 claims 1
- 239000005551 L01XE03 - Erlotinib Substances 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229960001433 erlotinib Drugs 0.000 claims 1
- AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 claims 1
- 229960002584 gefitinib Drugs 0.000 claims 1
- XGALLCVXEZPNRQ-UHFFFAOYSA-N gefitinib Chemical compound C=12C=C(OCCCN3CCOCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 XGALLCVXEZPNRQ-UHFFFAOYSA-N 0.000 claims 1
- 230000000762 glandular Effects 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 1
- FADJUGSUYLCNJQ-UHFFFAOYSA-N CC(CCC1)C1=C Chemical compound CC(CCC1)C1=C FADJUGSUYLCNJQ-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US39329110P | 2010-10-14 | 2010-10-14 | |
| US61/393,291 | 2010-10-14 | ||
| PCT/US2011/056457 WO2012051587A1 (en) | 2010-10-14 | 2011-10-14 | Methods for inhibiting cell proliferation in egfr-driven cancers |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013539795A JP2013539795A (ja) | 2013-10-28 |
| JP2013539795A5 true JP2013539795A5 (enExample) | 2014-11-27 |
Family
ID=45938740
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013534053A Pending JP2013539795A (ja) | 2010-10-14 | 2011-10-14 | Ｅｇｆｒ発動性がんの細胞増殖の阻害方法 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US20140024620A1 (enExample) |
| EP (1) | EP2627179A4 (enExample) |
| JP (1) | JP2013539795A (enExample) |
| KR (1) | KR20130139999A (enExample) |
| CN (2) | CN104814970A (enExample) |
| AU (1) | AU2011315831B2 (enExample) |
| BR (1) | BR112013008816A2 (enExample) |
| CA (1) | CA2810900A1 (enExample) |
| EA (1) | EA201390550A1 (enExample) |
| IL (1) | IL225351A0 (enExample) |
| MX (1) | MX2013004086A (enExample) |
| WO (1) | WO2012051587A1 (enExample) |
Families Citing this family (61)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
| EP3210609A1 (en) | 2008-05-21 | 2017-08-30 | Ariad Pharmaceuticals, Inc. | Phosphorous derivatives as kinase inhibitors |
| EP2704572B1 (en) * | 2011-05-04 | 2015-12-30 | Ariad Pharmaceuticals, Inc. | Compounds for inhibiting cell proliferation in egfr-driven cancers |
| AU2013204563B2 (en) * | 2012-05-05 | 2016-05-19 | Takeda Pharmaceutical Company Limited | Compounds for inhibiting cell proliferation in EGFR-driven cancers |
| EP2844642B8 (en) * | 2012-05-05 | 2019-12-25 | Ariad Pharmaceuticals, Inc. | Compounds for inhibiting cell proliferation in egfr-driven cancers |
| CN102977104A (zh) * | 2012-11-26 | 2013-03-20 | 盛世泰科生物医药技术(苏州)有限公司 | 2,4-二氯-7-氢-吡咯并（2,3）嘧啶的合成 |
| US9611283B1 (en) | 2013-04-10 | 2017-04-04 | Ariad Pharmaceuticals, Inc. | Methods for inhibiting cell proliferation in ALK-driven cancers |
| UA115388C2 (uk) * | 2013-11-21 | 2017-10-25 | Пфайзер Інк. | 2,6-заміщені пуринові похідні та їх застосування в лікуванні проліферативних захворювань |
| CN104761544B (zh) * | 2014-01-03 | 2019-03-15 | 北京轩义医药科技有限公司 | Egfr酪氨酸激酶的临床重要突变体的选择性抑制剂 |
| WO2015158310A1 (zh) * | 2014-04-18 | 2015-10-22 | 山东轩竹医药科技有限公司 | 一种酪氨酸激酶抑制剂及其用途 |
| JP6487527B2 (ja) * | 2014-07-04 | 2019-03-20 | チル ファーマシューティカル カンパニー リミテッド | スピロ環アリールリン酸化物及びアリールリン硫化物（ｓｐｉｒｏｃｙｃｌｉｃ ａｒｙｌ ｐｈｏｓｐｈｏｒｕｓ ｏｘｉｄｅ ａｎｄ ａｒｙｌ ｐｈｏｓｐｈｏｒｕｓ ｓｕｌｆｉｄｅ） |
| CN106699810A (zh) * | 2015-11-17 | 2017-05-24 | 清华大学 | 一种含氮杂环化合物及其制备方法与在抑制激酶活性中的应用 |
| EP3381925B1 (en) * | 2015-11-27 | 2020-12-16 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Deuterium-modified brigatinib derivatives, pharmaceutical compositions comprising same, and use thereof |
| CN109071512A (zh) * | 2016-02-03 | 2018-12-21 | 重庆复创医药研究有限公司 | 作为激酶抑制剂的含磷化合物 |
| CN107098887B (zh) * | 2016-02-22 | 2019-08-09 | 复旦大学 | 嘧啶类化合物 |
| WO2017200016A1 (ja) * | 2016-05-17 | 2017-11-23 | 公益財団法人がん研究会 | Ｅｇｆｒ－ｔｋｉ耐性を獲得した肺癌の治療薬 |
| CN109715620B (zh) | 2016-08-29 | 2022-05-06 | 密歇根大学董事会 | 作为alk抑制剂的氨基嘧啶 |
| WO2018102366A1 (en) * | 2016-11-30 | 2018-06-07 | Ariad Pharmaceuticals, Inc. | Anilinopyrimidines as haematopoietic progenitor kinase 1 (hpk1) inhibitors |
| CN110520110A (zh) * | 2017-03-08 | 2019-11-29 | 阿瑞雅德制药公司 | 包含5-氯-n4-[2-(二甲基磷酰基)苯基]-n2-{2-甲氧基-4-[4-(4-甲基哌嗪-1-基)哌啶-1-基]苯基}嘧啶-2,4-二胺的药物制剂 |
| CN113354685B (zh) | 2017-07-19 | 2022-12-20 | 正大天晴药业集团股份有限公司 | 作为egfr激酶抑制剂的芳基磷氧化合物 |
| KR20200072478A (ko) * | 2017-09-08 | 2020-06-22 | 더 리전츠 오브 더 유니버시티 오브 콜로라도, 어 바디 코퍼레이트 | Her-구동된 약물-내성암의 치료 또는 예방을 위한 화합물, 조성물 및 방법 |
| JP7043098B2 (ja) * | 2017-12-21 | 2022-03-29 | 深▲チェン▼市塔吉瑞生物医薬有限公司 | キナーゼ活性を阻害するためのジアニリノピリミジン系化合物 |
| CN110305161A (zh) * | 2018-03-20 | 2019-10-08 | 暨南大学 | 2-氨基嘧啶类化合物及其应用 |
| CN110467638A (zh) * | 2018-05-09 | 2019-11-19 | 北京赛特明强医药科技有限公司 | 一种含有间氯苯胺类取代基的双氨基氯代嘧啶类化合物、制备方法及其应用 |
| CN110467637B (zh) * | 2018-05-09 | 2022-02-18 | 北京赛特明强医药科技有限公司 | 一种含有氧化膦类取代苯胺的双氨基氯代嘧啶类化合物、制备方法及其应用 |
| CN110526941A (zh) * | 2018-05-24 | 2019-12-03 | 北京赛特明强医药科技有限公司 | 一种含有间氯苯胺类取代基的吡咯并嘧啶类化合物、制备方法及其应用 |
| CN111836819A (zh) * | 2018-05-24 | 2020-10-27 | 北京赛特明强医药科技有限公司 | 一种含有芳胺基取代的吡咯并嘧啶类化合物、制备方法及其应用 |
| CN110835320B (zh) * | 2018-08-15 | 2025-12-30 | 江苏奥赛康药业有限公司 | 二氨基嘧啶类化合物及其应用 |
| CA3126976A1 (en) * | 2019-01-18 | 2020-07-23 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Salt of egfr inhibitor, crystal form, and preparation method therefor |
| CN111825719A (zh) * | 2019-04-15 | 2020-10-27 | 北京赛特明强医药科技有限公司 | 一种含有芳胺基取代的吡咯并嘧啶类化合物、制备方法及其应用 |
| CN113166103B (zh) * | 2019-04-26 | 2022-12-16 | 江苏先声药业有限公司 | Egfr抑制剂及其应用 |
| TW202115042A (zh) * | 2019-06-21 | 2021-04-16 | 大陸商江蘇豪森藥業集團有限公司 | 芳基磷氧化物類衍生物抑制劑、其製備方法和應用 |
| US11529350B2 (en) | 2019-07-03 | 2022-12-20 | Sumitomo Pharma Oncology, Inc. | Tyrosine kinase non-receptor 1 (TNK1) inhibitors and uses thereof |
| CN114430739A (zh) * | 2019-07-26 | 2022-05-03 | 贝达药业股份有限公司 | Egfr抑制剂、组合物及其制备方法 |
| WO2021018003A1 (zh) * | 2019-07-26 | 2021-02-04 | 贝达药业股份有限公司 | Egfr抑制剂、组合物及其制备方法 |
| CN112538072B (zh) * | 2019-09-21 | 2024-02-06 | 齐鲁制药有限公司 | 氨基嘧啶类egfr抑制剂 |
| WO2021057882A1 (zh) * | 2019-09-26 | 2021-04-01 | 贝达药业股份有限公司 | Egfr抑制剂、组合物及其制备方法 |
| CN114430741A (zh) * | 2019-10-17 | 2022-05-03 | 贝达药业股份有限公司 | Egfr抑制剂、组合物及其制备方法 |
| AU2020385527B2 (en) * | 2019-11-21 | 2023-04-13 | Tyk Medicines, Inc. | Compound used as EGFR kinase inhibitor and use thereof |
| CN114728932B (zh) * | 2019-11-29 | 2024-11-29 | 江苏先声药业有限公司 | 作为egfr激酶抑制剂的多芳基化合物 |
| PH12022552110A1 (en) * | 2020-02-14 | 2024-01-29 | Betta Pharmaceuticals Co Ltd | Quinolyl phosphine oxide compound, and composition and application thereof |
| AU2021227907A1 (en) * | 2020-02-25 | 2022-09-29 | Dana-Farber Cancer Institute, Inc. | Potent and selective degraders of ALK |
| CN115515949A (zh) * | 2020-03-23 | 2022-12-23 | 齐鲁制药有限公司 | 新型氨基嘧啶类egfr抑制剂 |
| CN111777592B (zh) * | 2020-06-22 | 2021-06-18 | 温州医科大学 | 一种n4-(2,5-二甲氧基苯基)-嘧啶二胺类靶向ddr1抑制剂及其制备和应用 |
| JP2023549074A (ja) * | 2020-10-30 | 2023-11-22 | ブループリント メディシンズ コーポレイション | ピリミジン化合物、組成物、及びその医薬用途 |
| CN116685583A (zh) * | 2020-10-30 | 2023-09-01 | 缆图药品公司 | 嘧啶化合物、组合物及其医药应用 |
| PE20231515A1 (es) * | 2020-10-30 | 2023-09-28 | Blueprint Medicines Corp | Compuestos de pirimidina, composiciones y aplicaciones medicas de esta |
| CN116710444A (zh) * | 2020-10-30 | 2023-09-05 | 缆图药品公司 | 嘧啶化合物、组合物及其医药应用 |
| WO2022127807A1 (zh) * | 2020-12-18 | 2022-06-23 | 江苏豪森药业集团有限公司 | 一种芳基磷氧化物类衍生物自由碱的晶型及其制备方法和应用 |
| WO2022147620A1 (en) * | 2021-01-07 | 2022-07-14 | Ontario Institute For Cancer Research (Oicr) | Thienyl and cycloalkyl aminopyrimidine compounds as inhibitors of nuak kinases, compositions and uses thereof |
| CA3204401A1 (en) * | 2021-01-07 | 2022-07-14 | Rima AL-AWAR | Isoindolinone aminopyrimidine compounds as inhibitors of nuak kinases, compositions and uses thereof |
| WO2022194269A1 (zh) * | 2021-03-19 | 2022-09-22 | 上海齐鲁制药研究中心有限公司 | 新型egfr降解剂 |
| WO2022199589A1 (zh) * | 2021-03-23 | 2022-09-29 | 南京明德新药研发有限公司 | 嘧啶衍生物 |
| WO2022211573A1 (ko) * | 2021-04-01 | 2022-10-06 | 주식회사 테라펙스 | 단백질 키나아제 저해 활성을 갖는 피리미딘 유도체 및 이를 포함하는 치료용 약학 조성물 |
| WO2022227032A1 (en) * | 2021-04-30 | 2022-11-03 | Beigene (Beijing) Co., Ltd. | Egfr degraders and associated methods of use |
| EP4330251A4 (en) * | 2021-04-30 | 2025-03-05 | BeiGene Switzerland GmbH | EGFR DEGRADING AGENTS AND METHODS OF USE THEREOF |
| CN115677772B (zh) * | 2021-07-30 | 2023-08-18 | 浙江大学智能创新药物研究院 | 一种用于egfr激酶抑制剂的化合物、组合物及其应用 |
| WO2024005516A1 (ko) * | 2022-06-28 | 2024-01-04 | 보로노이 주식회사 | 헤테로아릴 유도체 화합물 및 이의 용도 |
| CN115260234A (zh) * | 2022-07-01 | 2022-11-01 | 江苏医药职业学院 | 一种2-氨基-4-氨基芳基磷氧基嘧啶化合物及其制备方法与应用 |
| CN116284001B (zh) * | 2023-01-30 | 2025-06-06 | 中国药科大学 | Dclk1抑制剂、制备方法、药物组合物和应用 |
| CN117187271B (zh) * | 2023-03-07 | 2024-08-27 | 艾博生物科技(上海)有限公司 | 编码激活性EGFR突变肽的免疫调节治疗mRNA组合物 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2432000C (en) * | 2000-12-21 | 2011-03-15 | Glaxo Group Limited | Pyrimidineamines as angiogenesis modulators |
| BRPI0618135A2 (pt) * | 2005-11-03 | 2011-08-16 | Irm Llc | compostos e composições como inibidores da proteìna quinase |
| JO2660B1 (en) * | 2006-01-20 | 2012-06-17 | نوفارتيس ايه جي | Pi-3 inhibitors and methods of use |
| WO2008039359A2 (en) * | 2006-09-25 | 2008-04-03 | Janssen Pharmaceutica N.V. | Bicyclic pyrimidine kinase inhibitors |
| TWI389893B (zh) * | 2007-07-06 | 2013-03-21 | Astellas Pharma Inc | 二（芳胺基）芳基化合物 |
| US7989465B2 (en) * | 2007-10-19 | 2011-08-02 | Avila Therapeutics, Inc. | 4,6-disubstituted pyrimidines useful as kinase inhibitors |
| WO2009109605A1 (en) * | 2008-03-05 | 2009-09-11 | Novartis Ag | Use of pyrimidine derivatives for the treatment of egfr dependent diseases or diseases that have acquired resistance to agents that target egfr family members |
| EA018282B1 (ru) * | 2008-04-07 | 2013-06-28 | Айрм Ллк | Соединения и композиции в качестве ингибиторов протеинкиназы |
| EP3210609A1 (en) * | 2008-05-21 | 2017-08-30 | Ariad Pharmaceuticals, Inc. | Phosphorous derivatives as kinase inhibitors |
| TWI546290B (zh) * | 2008-06-27 | 2016-08-21 | 賽基艾維洛米斯研究股份有限公司 | 雜芳基化合物及其用途 |
| RU2585177C2 (ru) * | 2010-06-23 | 2016-05-27 | Ханми Сайенс Ко., Лтд. | Новые конденсированные пиримидиновые производные для ингибирования тирозинкиназной активности |
| ES2635713T3 (es) * | 2010-11-01 | 2017-10-04 | Celgene Car Llc | Compuestos de heteroarilo y usos de los mismos |
| EP2637502B1 (en) * | 2010-11-10 | 2018-01-10 | Celgene CAR LLC | Mutant-selective egfr inhibitors and uses thereof |
-
2011
- 2011-10-14 MX MX2013004086A patent/MX2013004086A/es not_active Application Discontinuation
- 2011-10-14 US US13/878,744 patent/US20140024620A1/en not_active Abandoned
- 2011-10-14 CA CA2810900A patent/CA2810900A1/en not_active Abandoned
- 2011-10-14 CN CN201510102987.2A patent/CN104814970A/zh active Pending
- 2011-10-14 CN CN201180049813.4A patent/CN103153064B/zh active Active
- 2011-10-14 BR BR112013008816A patent/BR112013008816A2/pt not_active IP Right Cessation
- 2011-10-14 WO PCT/US2011/056457 patent/WO2012051587A1/en not_active Ceased
- 2011-10-14 AU AU2011315831A patent/AU2011315831B2/en active Active
- 2011-10-14 EP EP11833524.9A patent/EP2627179A4/en not_active Withdrawn
- 2011-10-14 KR KR1020137012320A patent/KR20130139999A/ko not_active Withdrawn
- 2011-10-14 JP JP2013534053A patent/JP2013539795A/ja active Pending
- 2011-10-14 EA EA201390550A patent/EA201390550A1/ru unknown
-
2013
- 2013-03-20 IL IL225351A patent/IL225351A0/en unknown
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