JP2014506930A5 - - Google Patents
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- JP2014506930A5 JP2014506930A5 JP2013556817A JP2013556817A JP2014506930A5 JP 2014506930 A5 JP2014506930 A5 JP 2014506930A5 JP 2013556817 A JP2013556817 A JP 2013556817A JP 2013556817 A JP2013556817 A JP 2013556817A JP 2014506930 A5 JP2014506930 A5 JP 2014506930A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- optionally substituted
- cancer
- haloalkyl
- hydroxyalkyl
- 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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- 125000000217 alkyl group Chemical group 0.000 claims description 87
- 150000001875 compounds Chemical class 0.000 claims description 50
- 229910052739 hydrogen Inorganic materials 0.000 claims description 32
- 239000001257 hydrogen Substances 0.000 claims description 32
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims description 28
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 28
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 24
- 125000000623 heterocyclic group Chemical group 0.000 claims description 24
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 21
- -1 2-oxo-1,2-dihydropyridinyl Chemical group 0.000 claims description 20
- 125000001072 heteroaryl group Chemical group 0.000 claims description 20
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 20
- 229910052736 halogen Inorganic materials 0.000 claims description 16
- 150000002367 halogens Chemical class 0.000 claims description 16
- 239000000203 mixture Substances 0.000 claims description 15
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 14
- 208000035475 disorder Diseases 0.000 claims description 14
- 230000003463 hyperproliferative effect Effects 0.000 claims description 12
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims description 12
- 150000002431 hydrogen Chemical group 0.000 claims description 11
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 10
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 10
- 206010028980 Neoplasm Diseases 0.000 claims description 8
- 201000011510 cancer Diseases 0.000 claims description 8
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 8
- 125000001188 haloalkyl group Chemical group 0.000 claims description 8
- 125000004043 oxo group Chemical group O=* 0.000 claims description 8
- 125000003386 piperidinyl group Chemical group 0.000 claims description 8
- 125000004076 pyridyl group Chemical group 0.000 claims description 8
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 8
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims description 6
- 102100024193 Mitogen-activated protein kinase 1 Human genes 0.000 claims description 6
- 125000002252 acyl group Chemical group 0.000 claims description 6
- 125000003118 aryl group Chemical group 0.000 claims description 6
- 229910052799 carbon Inorganic materials 0.000 claims description 6
- 230000000694 effects Effects 0.000 claims description 6
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 6
- 208000027866 inflammatory disease Diseases 0.000 claims description 6
- 125000002757 morpholinyl group Chemical group 0.000 claims description 6
- 150000003839 salts Chemical class 0.000 claims description 6
- 125000000335 thiazolyl group Chemical group 0.000 claims description 6
- 125000001425 triazolyl group Chemical group 0.000 claims description 6
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims description 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 4
- 125000004485 2-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])([H])C1([H])* 0.000 claims description 4
- 206010006187 Breast cancer Diseases 0.000 claims description 4
- 208000026310 Breast neoplasm Diseases 0.000 claims description 4
- 206010009944 Colon cancer Diseases 0.000 claims description 4
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 4
- 206010033128 Ovarian cancer Diseases 0.000 claims description 4
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 4
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 4
- 208000024770 Thyroid neoplasm Diseases 0.000 claims description 4
- 125000003545 alkoxy group Chemical group 0.000 claims description 4
- 125000005115 alkyl carbamoyl group Chemical group 0.000 claims description 4
- 125000004429 atom Chemical group 0.000 claims description 4
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims description 4
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims description 4
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 4
- 125000001041 indolyl group Chemical group 0.000 claims description 4
- 230000002401 inhibitory effect Effects 0.000 claims description 4
- 201000005202 lung cancer Diseases 0.000 claims description 4
- 208000020816 lung neoplasm Diseases 0.000 claims description 4
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 4
- 229910052757 nitrogen Inorganic materials 0.000 claims description 4
- 125000001715 oxadiazolyl group Chemical group 0.000 claims description 4
- 125000002971 oxazolyl group Chemical group 0.000 claims description 4
- 201000002528 pancreatic cancer Diseases 0.000 claims description 4
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 4
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 4
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 4
- 201000002510 thyroid cancer Diseases 0.000 claims description 4
- 239000003085 diluting agent Substances 0.000 claims description 3
- 239000003937 drug carrier Substances 0.000 claims description 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 3
- 125000006594 (C1-C3) alkylsulfony group Chemical group 0.000 claims description 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 2
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims description 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims description 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 2
- 208000010507 Adenocarcinoma of Lung Diseases 0.000 claims description 2
- 208000003200 Adenoma Diseases 0.000 claims description 2
- 206010001233 Adenoma benign Diseases 0.000 claims description 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims description 2
- 208000008035 Back Pain Diseases 0.000 claims description 2
- 206010005003 Bladder cancer Diseases 0.000 claims description 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims description 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 2
- 208000017604 Hodgkin disease Diseases 0.000 claims description 2
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims description 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims description 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 2
- 208000034578 Multiple myelomas Diseases 0.000 claims description 2
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims description 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims description 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims description 2
- 208000033833 Myelomonocytic Chronic Leukemia Diseases 0.000 claims description 2
- 206010029260 Neuroblastoma Diseases 0.000 claims description 2
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims description 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims description 2
- 208000015634 Rectal Neoplasms Diseases 0.000 claims description 2
- 206010038389 Renal cancer Diseases 0.000 claims description 2
- 206010039491 Sarcoma Diseases 0.000 claims description 2
- 208000024313 Testicular Neoplasms Diseases 0.000 claims description 2
- 206010057644 Testis cancer Diseases 0.000 claims description 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 2
- 125000004442 acylamino group Chemical group 0.000 claims description 2
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims description 2
- 125000004414 alkyl thio group Chemical group 0.000 claims description 2
- 150000001412 amines Chemical class 0.000 claims description 2
- 239000002246 antineoplastic agent Substances 0.000 claims description 2
- 206010003246 arthritis Diseases 0.000 claims description 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 2
- 125000004104 aryloxy group Chemical group 0.000 claims description 2
- 125000002393 azetidinyl group Chemical group 0.000 claims description 2
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims description 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 2
- 150000001721 carbon Chemical group 0.000 claims description 2
- 201000010902 chronic myelomonocytic leukemia Diseases 0.000 claims description 2
- 208000029742 colonic neoplasm Diseases 0.000 claims description 2
- 125000004966 cyanoalkyl group Chemical group 0.000 claims description 2
- 125000004122 cyclic group Chemical group 0.000 claims description 2
- 229940127089 cytotoxic agent Drugs 0.000 claims description 2
- 230000003325 follicular Effects 0.000 claims description 2
- 208000005017 glioblastoma Diseases 0.000 claims description 2
- 125000004995 haloalkylthio group Chemical group 0.000 claims description 2
- 125000005843 halogen group Chemical group 0.000 claims description 2
- 201000010536 head and neck cancer Diseases 0.000 claims description 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims description 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 2
- 125000002883 imidazolyl group Chemical group 0.000 claims description 2
- 230000005764 inhibitory process Effects 0.000 claims description 2
- 125000001786 isothiazolyl group Chemical group 0.000 claims description 2
- CTAPFRYPJLPFDF-UHFFFAOYSA-N isoxazole Chemical compound C=1C=NOC=1 CTAPFRYPJLPFDF-UHFFFAOYSA-N 0.000 claims description 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims description 2
- 201000010982 kidney cancer Diseases 0.000 claims description 2
- 208000003849 large cell carcinoma Diseases 0.000 claims description 2
- 208000032839 leukemia Diseases 0.000 claims description 2
- 201000005249 lung adenocarcinoma Diseases 0.000 claims description 2
- 201000001441 melanoma Diseases 0.000 claims description 2
- LVWZTYCIRDMTEY-UHFFFAOYSA-N metamizole Chemical compound O=C1C(N(CS(O)(=O)=O)C)=C(C)N(C)N1C1=CC=CC=C1 LVWZTYCIRDMTEY-UHFFFAOYSA-N 0.000 claims description 2
- HRDXJKGNWSUIBT-UHFFFAOYSA-N methoxybenzene Chemical group [CH2]OC1=CC=CC=C1 HRDXJKGNWSUIBT-UHFFFAOYSA-N 0.000 claims description 2
- 208000025113 myeloid leukemia Diseases 0.000 claims description 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 2
- 125000003566 oxetanyl group Chemical group 0.000 claims description 2
- 229910052760 oxygen Inorganic materials 0.000 claims description 2
- 125000004193 piperazinyl group Chemical group 0.000 claims description 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 2
- 206010038038 rectal cancer Diseases 0.000 claims description 2
- 201000001275 rectum cancer Diseases 0.000 claims description 2
- 201000003068 rheumatic fever Diseases 0.000 claims description 2
- 201000000849 skin cancer Diseases 0.000 claims description 2
- 208000000649 small cell carcinoma Diseases 0.000 claims description 2
- 206010041823 squamous cell carcinoma Diseases 0.000 claims description 2
- 125000003107 substituted aryl group Chemical group 0.000 claims description 2
- 229910052717 sulfur Inorganic materials 0.000 claims description 2
- 208000001608 teratocarcinoma Diseases 0.000 claims description 2
- 201000003120 testicular cancer Diseases 0.000 claims description 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 2
- 238000000034 method Methods 0.000 description 11
- 239000008194 pharmaceutical composition Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161447587P | 2011-02-28 | 2011-02-28 | |
| US61/447,587 | 2011-02-28 | ||
| PCT/US2012/027009 WO2012118850A1 (en) | 2011-02-28 | 2012-02-28 | Serine/threonine kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014506930A JP2014506930A (ja) | 2014-03-20 |
| JP2014506930A5 true JP2014506930A5 (enExample) | 2015-04-02 |
| JP6085866B2 JP6085866B2 (ja) | 2017-03-01 |
Family
ID=45852719
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013556817A Active JP6085866B2 (ja) | 2011-02-28 | 2012-02-28 | セリン／トレオニンキナーゼインヒビター |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US9133187B2 (enExample) |
| EP (1) | EP2681215B1 (enExample) |
| JP (1) | JP6085866B2 (enExample) |
| KR (1) | KR101961500B1 (enExample) |
| CN (1) | CN103635472B (enExample) |
| BR (1) | BR112013021896A2 (enExample) |
| CA (1) | CA2828478C (enExample) |
| ES (1) | ES2543050T3 (enExample) |
| MX (1) | MX339873B (enExample) |
| RU (1) | RU2013143839A (enExample) |
| WO (1) | WO2012118850A1 (enExample) |
Families Citing this family (33)
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| KR101961500B1 (ko) | 2011-02-28 | 2019-03-22 | 어레이 바이오파마 인크. | 세린/트레오닌 키나제 억제제 |
| CA2839699A1 (en) | 2011-06-24 | 2012-12-27 | Amgen Inc. | Trpm8 antagonists and their use in treatments |
| AU2012272898A1 (en) | 2011-06-24 | 2013-04-11 | Amgen Inc. | TRPM8 antagonists and their use in treatments |
| RU2014108140A (ru) | 2011-08-04 | 2015-09-10 | Эррэй Биофарма Инк. | Соединение на основе хинозолина в качестве ингибиторов серен-треониновых киназ |
| JP6089045B2 (ja) * | 2011-12-27 | 2017-03-01 | バイオ−ファーム ソリューションズ カンパニー リミテッド | 痛みの緩和または治療に使用するためのフェニルカルバメート化合物 |
| UA116774C2 (uk) | 2012-03-01 | 2018-05-10 | Еррей Біофарма Інк. | Інгібітори серин/треонінкінази |
| US8952009B2 (en) | 2012-08-06 | 2015-02-10 | Amgen Inc. | Chroman derivatives as TRPM8 inhibitors |
| KR20150047597A (ko) | 2012-08-27 | 2015-05-04 | 어레이 바이오파마 인크. | 과증식성 질환의 치료를 위한 세린/트레오닌 키나아제 억제제 |
| BR112015005982A2 (pt) | 2012-09-19 | 2017-07-04 | Novartis Ag | di-hidropirrolidino-pirimidinas como inibidores de quinase |
| RU2015114936A (ru) | 2012-10-16 | 2016-12-10 | Ф. Хоффманн-Ля Рош Аг | Ингибиторы серин/треонинкиназы |
| JPWO2015012328A1 (ja) * | 2013-07-24 | 2017-03-02 | 武田薬品工業株式会社 | 複素環化合物 |
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| JP6449293B2 (ja) | 2013-12-06 | 2019-01-09 | ジェネンテック， インコーポレイテッド | セリン／トレオニンキナーゼ阻害剤 |
| JP6642942B2 (ja) | 2013-12-30 | 2020-02-12 | アレイ バイオファーマ、インコーポレイテッド | セリン／トレオニンキナーゼ阻害剤 |
| BR112016015235A2 (pt) | 2013-12-30 | 2017-08-08 | Genentech Inc | Composto, composição farmacêutica, método de inibição da atividade da proteína quinase erk e método de tratamento |
| CN109072311A (zh) | 2016-04-15 | 2018-12-21 | 豪夫迈·罗氏有限公司 | 用于癌症的诊断和治疗方法 |
| MX382339B (es) * | 2016-05-18 | 2025-03-13 | Mirati Therapeutics Inc | Inhibidores g12c de kras. |
| CN111373055B (zh) | 2017-09-08 | 2024-07-23 | 豪夫迈·罗氏有限公司 | 用于癌症的诊断和治疗方法 |
| ES2967094T3 (es) | 2017-09-29 | 2024-04-26 | Mitsubishi Tanabe Pharma Corp | Compuesto de pirrolidina ópticamente activo y procedimiento de producción del mismo |
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| US20210008047A1 (en) | 2018-02-13 | 2021-01-14 | Vib Vzw | Targeting minimal residual disease in cancer with rxr antagonists |
| WO2020192750A1 (zh) | 2019-03-28 | 2020-10-01 | 江苏恒瑞医药股份有限公司 | 噻吩并杂环类衍生物、其制备方法及其在医药上的应用 |
| BR112021018924A2 (pt) | 2019-03-29 | 2022-02-01 | Jiangsu Hengrui Medicine Co | Derivado de heterocíclico pirrol, método de preparação do mesmo e aplicação do mesmo em medicamento |
| CN113825757B (zh) | 2019-05-24 | 2023-10-20 | 江苏恒瑞医药股份有限公司 | 取代的稠合双环类衍生物、其制备方法及其在医药上的应用 |
| WO2020238791A1 (zh) * | 2019-05-24 | 2020-12-03 | 江苏恒瑞医药股份有限公司 | 氢化吡啶并嘧啶类衍生物、其制备方法及其在医药上的应用 |
| CN111170929A (zh) * | 2019-12-12 | 2020-05-19 | 北京达因高科儿童药物研究院有限公司 | 一种由末端烯烃制备β-氨基醇的方法 |
| ES3033417T3 (en) * | 2020-09-25 | 2025-08-04 | Janssen Pharmaceutica Nv | Cyclin-dependent kinase 7 (cdk7) non-covalent inhibitors |
| CN116437915B (zh) | 2020-09-29 | 2025-03-18 | 江苏恒瑞医药股份有限公司 | 一种吡咯并杂环类衍生物的晶型及其制备方法 |
| CN115040522B (zh) * | 2022-06-30 | 2024-02-06 | 牡丹江医学院 | 一种用于治疗肺癌的药物及其制备方法 |
| KR20250091232A (ko) * | 2022-10-25 | 2025-06-20 | 투오지에 바이오텍 (상하이) 컴퍼니 리미티드 | 피페리디노피리미딘계 유도체, 이의 제조 방법 및 이의 의학적 응용 |
| IT202200024963A1 (it) * | 2022-12-05 | 2024-06-05 | Angelini Pharma S P A | Composti attivatori dei canali potassio Kv7.2/Kv7.3 |
| TW202535869A (zh) * | 2023-10-23 | 2025-09-16 | 大陸商上海拓界生物醫藥科技有限公司 | 一種含有噻唑基的哌啶并嘧啶類衍生物、其製備方法及其醫藥上的應用 |
| WO2025223512A1 (zh) * | 2024-04-24 | 2025-10-30 | 江苏恒瑞医药股份有限公司 | 一种二氢吡啶并嘧啶衍生物的可药用盐、结晶形式及用途 |
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| JP5611826B2 (ja) | 2007-09-04 | 2014-10-22 | ザ スクリプス リサーチ インスティテュート | タンパク質キナーゼ阻害剤としての置換されたピリミジニル−アミン |
| WO2009061761A2 (en) | 2007-11-06 | 2009-05-14 | E. I. Du Pont De Nemours And Company | Fungicidal heterocyclic amines |
| WO2009146034A2 (en) * | 2008-03-31 | 2009-12-03 | Takeda Pharmaceutical Company Limited | Mapk/erk kinase inhibitors and methods of use thereof |
| WO2009156484A2 (en) | 2008-06-27 | 2009-12-30 | Novartis Ag | Organic compounds |
| EP2361248B1 (en) | 2008-06-27 | 2018-09-19 | Celgene CAR LLC | Heteroaryl compounds and uses thereof |
| WO2010077275A1 (en) | 2008-12-08 | 2010-07-08 | Arena Pharmaceuticals, Inc. | Modulators of the prostacyclin (pgi2) receptor useful for the treatment of disorders related thereto |
| KR101961500B1 (ko) | 2011-02-28 | 2019-03-22 | 어레이 바이오파마 인크. | 세린/트레오닌 키나제 억제제 |
| RU2014108140A (ru) | 2011-08-04 | 2015-09-10 | Эррэй Биофарма Инк. | Соединение на основе хинозолина в качестве ингибиторов серен-треониновых киназ |
| UA116774C2 (uk) | 2012-03-01 | 2018-05-10 | Еррей Біофарма Інк. | Інгібітори серин/треонінкінази |
| KR20150047597A (ko) | 2012-08-27 | 2015-05-04 | 어레이 바이오파마 인크. | 과증식성 질환의 치료를 위한 세린/트레오닌 키나아제 억제제 |
-
2012
- 2012-02-28 KR KR1020137025269A patent/KR101961500B1/ko not_active Expired - Fee Related
- 2012-02-28 BR BR112013021896A patent/BR112013021896A2/pt not_active Application Discontinuation
- 2012-02-28 JP JP2013556817A patent/JP6085866B2/ja active Active
- 2012-02-28 EP EP20120709429 patent/EP2681215B1/en active Active
- 2012-02-28 WO PCT/US2012/027009 patent/WO2012118850A1/en not_active Ceased
- 2012-02-28 CA CA2828478A patent/CA2828478C/en not_active Expired - Fee Related
- 2012-02-28 ES ES12709429.0T patent/ES2543050T3/es active Active
- 2012-02-28 MX MX2013009877A patent/MX339873B/es active IP Right Grant
- 2012-02-28 CN CN201280020897.3A patent/CN103635472B/zh active Active
- 2012-02-28 US US14/002,079 patent/US9133187B2/en active Active
- 2012-02-28 RU RU2013143839/04A patent/RU2013143839A/ru not_active Application Discontinuation
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