PE20140234A1 - Compuestos de 2-amino-4-ariltiazol como antagonistas de trpa1 - Google Patents
Compuestos de 2-amino-4-ariltiazol como antagonistas de trpa1Info
- Publication number
- PE20140234A1 PE20140234A1 PE2013001454A PE2013001454A PE20140234A1 PE 20140234 A1 PE20140234 A1 PE 20140234A1 PE 2013001454 A PE2013001454 A PE 2013001454A PE 2013001454 A PE2013001454 A PE 2013001454A PE 20140234 A1 PE20140234 A1 PE 20140234A1
- Authority
- PE
- Peru
- Prior art keywords
- compounds
- alkyl
- aryltiazole
- amino
- tetrahydrotieno
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- 239000005557 antagonist Substances 0.000 title abstract 2
- 101000764872 Homo sapiens Transient receptor potential cation channel subfamily A member 1 Proteins 0.000 title 1
- 102100026186 Transient receptor potential cation channel subfamily A member 1 Human genes 0.000 title 1
- WZKSXHQDXQKIQJ-UHFFFAOYSA-N F[C](F)F Chemical group F[C](F)F WZKSXHQDXQKIQJ-UHFFFAOYSA-N 0.000 abstract 2
- 101000740162 Homo sapiens Sodium- and chloride-dependent transporter XTRP3 Proteins 0.000 abstract 2
- 208000002193 Pain Diseases 0.000 abstract 2
- 102100037189 Sodium- and chloride-dependent transporter XTRP3 Human genes 0.000 abstract 2
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical compound [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 2
- TUCNEACPLKLKNU-UHFFFAOYSA-N acetyl Chemical compound C[C]=O TUCNEACPLKLKNU-UHFFFAOYSA-N 0.000 abstract 2
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 2
- 208000000094 Chronic Pain Diseases 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 208000004296 neuralgia Diseases 0.000 abstract 1
- 208000021722 neuropathic pain Diseases 0.000 abstract 1
- 230000003349 osteoarthritic effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- VYDIHCZDHYNHNB-UHFFFAOYSA-N phosphoric acid;pyrimidine Chemical compound OP(O)(O)=O.C1=CN=CN=C1 VYDIHCZDHYNHNB-UHFFFAOYSA-N 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P13/10—Drugs for disorders of the urinary system of the bladder
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- 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
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- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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- C07—ORGANIC CHEMISTRY
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- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
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- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
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- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
- C07F9/65616—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing the ring system having three or more than three double bonds between ring members or between ring members and non-ring members, e.g. purine or analogs
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Pulmonology (AREA)
- Urology & Nephrology (AREA)
- Dermatology (AREA)
- Pain & Pain Management (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Cardiology (AREA)
- Hospice & Palliative Care (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
- Physical Education & Sports Medicine (AREA)
- Otolaryngology (AREA)
- Rheumatology (AREA)
- Vascular Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
SE REFIERE A COMPUESTOS DERIVADOS DE 2-AMINO-4-ARILTIAZOL DE FORMULA (I) DONDE Het ES UN COMPUESTO DE FORMULA (a), (b), ENTRE OTROS, EN DONDE Ra, Rb Y Rd SON CADA UNO H O ALQUILO(C1-C4); R1 ES H; P ES (i), (ii), ENTRE OTROS, EN DONDE R3 ES ALQUILO(C1-C8) O UN ANILLO HETEROCICLICO DE 3 A 15 MIEMBROS; R8 ES H, ALQUILO(C1-C4), ENTRE OTROS; R2 ES HALOGENO, HALOALQUILO(C1-C8) O HALOALCOXI(C1-C8); m ES DE 0 A 5. SON COMPUESTOS PREFERIDOS: DIHIDROGENO FOSFATO DE [2-{[(1,3-DIMETIL-2,4-DIOXO-1,2,3,4-TETRAHIDROTIENO[2,3-d]PIRIMIDIN-5-IL)ACETIL]IMINO}-4-[3-FLUORO-4-(TRIFLUOROMETIL)FENIL]-1,3-TIAZOL-3(2H)-IL]METILO; DIHIDROGENO FOSFATO DE [4-[2,4-DIFLUORO-3-(TRIFLUOROMETIL)FENIL]-2-{[(1,3-DIMETIL-2,4-DIOXO-1,2,3,4-TETRAHIDROTIENO[2,3-d]PIRIMIDIN-5-IL)ACETIL]IMINO}-1,3-TIAZOL-3(2H)-IL]METILO; ENTRE OTROS. TAMBIEN SE REFIERE UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON ANTAGONISTAS DEL RECEPTOR DE POTENCIAL TRANSITORIO DE ANQUIRINA TIPO 1 (TRPA1) SIENDO UTILES EN EL TRATAMIENTO DEL DOLOR CRONICO, DOLOR NEUROPATICO, DOLOR OSTEOARTRITICO
Applications Claiming Priority (8)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN3451MU2010 | 2010-12-20 | ||
| US201061428327P | 2010-12-30 | 2010-12-30 | |
| IN748MU2011 | 2011-03-16 | ||
| US201161466535P | 2011-03-23 | 2011-03-23 | |
| IN1569MU2011 | 2011-05-25 | ||
| US201161495002P | 2011-06-09 | 2011-06-09 | |
| IN2741MU2011 | 2011-09-28 | ||
| US201161552076P | 2011-10-27 | 2011-10-27 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20140234A1 true PE20140234A1 (es) | 2014-03-08 |
Family
ID=46235162
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2013001454A PE20140234A1 (es) | 2010-12-20 | 2011-12-15 | Compuestos de 2-amino-4-ariltiazol como antagonistas de trpa1 |
Country Status (20)
| Country | Link |
|---|---|
| US (3) | US8592398B2 (es) |
| EP (1) | EP2655377B1 (es) |
| JP (1) | JP5694560B2 (es) |
| KR (1) | KR101591153B1 (es) |
| CN (1) | CN103261201B (es) |
| AP (1) | AP3391A (es) |
| AR (1) | AR084294A1 (es) |
| AU (1) | AU2011346763B2 (es) |
| BR (1) | BR112013014692A2 (es) |
| CA (1) | CA2820448A1 (es) |
| CL (1) | CL2013001810A1 (es) |
| EA (1) | EA023141B1 (es) |
| MX (1) | MX336549B (es) |
| MY (1) | MY159059A (es) |
| PE (1) | PE20140234A1 (es) |
| PH (1) | PH12013501290A1 (es) |
| SG (1) | SG191173A1 (es) |
| TW (1) | TWI515199B (es) |
| UA (1) | UA109916C2 (es) |
| WO (1) | WO2012085662A1 (es) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101734955B1 (ko) | 2008-11-07 | 2017-05-12 | 메사추세츠 인스티튜트 오브 테크놀로지 | 아미노알콜 리피도이드 및 그의 용도 |
| EA023141B1 (ru) | 2010-12-20 | 2016-04-29 | Гленмарк Фармасьютикалс С.А. | Соединения 2-амино-4-арилтиазола в качестве антагонистов trpa1 |
| EP2691443B1 (en) | 2011-03-28 | 2021-02-17 | Massachusetts Institute of Technology | Conjugated lipomers and uses thereof |
| EP2742048B1 (en) | 2011-08-09 | 2016-04-27 | Hydra Biosciences, Inc. | Inhibiting transient receptor potential ion channel trpa1 |
| MX363734B (es) | 2011-10-27 | 2019-03-29 | Massachusetts Inst Technology | Derivados de aminoacidos funcionalizados en la terminal n capaces de formar microesferas encapsuladoras de farmaco. |
| CN104203236A (zh) | 2012-01-17 | 2014-12-10 | 味之素株式会社 | 杂环酰胺衍生物和含有其的药物 |
| JP5989900B2 (ja) | 2012-06-08 | 2016-09-07 | グレンマーク ファーマシューティカルズ, エセ.アー. | 2−アミノ−4−アリールチアゾール化合物のアミド及びその塩類 |
| PT2903965T (pt) | 2012-10-01 | 2017-06-06 | Orion Corp | Derivados de n-prop-2-inilcarboxamida e sua utilização como antagonistas de trpa1 |
| US9394308B2 (en) | 2013-01-18 | 2016-07-19 | Merck Sharp & Dohme Corp. | Inhibiting the transient receptor potential A1 ion channel |
| GB201309333D0 (en) * | 2013-05-23 | 2013-07-10 | Agency Science Tech & Res | Purine diones as WNT pathway modulators |
| US9198898B2 (en) | 2013-06-24 | 2015-12-01 | Tigercat Pharma, Inc. | Use of NK-1 receptor antagonists in pruritus |
| US8906951B1 (en) | 2013-06-24 | 2014-12-09 | Tigercat Pharma, Inc. | Use of NK-1 receptor antagonists in pruritus |
| CA2926389A1 (en) | 2013-10-15 | 2015-04-23 | Glenmark Pharmaceuticals S.A. | Pharmaceutical composition comprising a trpa1 antagonist and an analgesic agent |
| WO2015127186A1 (en) * | 2014-02-24 | 2015-08-27 | The Johns Hopkins University | Tmem100 peptides and variants thereof and their use in treating or preventing diseases or conditions |
| WO2016205691A1 (en) | 2015-06-19 | 2016-12-22 | Massachusetts Institute Of Technology | Alkenyl substituted 2,5-piperazinediones and their use in compositions for delivering an agent to a subject or cell |
| FR3037956B1 (fr) * | 2015-06-23 | 2017-08-04 | Servier Lab | Nouveaux derives d'acide amine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| WO2017060488A1 (en) | 2015-10-09 | 2017-04-13 | Almirall, S.A. | New trpa1 antagonists |
| WO2017064068A1 (en) | 2015-10-14 | 2017-04-20 | Almirall, S.A. | New trpa1 antagonists |
| CN108727400B (zh) * | 2017-05-24 | 2021-07-09 | 四川晶华生物科技有限公司 | 一种治疗肿瘤的化合物 |
| US10710994B2 (en) | 2018-03-19 | 2020-07-14 | Genentech, Inc. | Oxadiazole transient receptor potential channel inhibitors |
| CN120285204A (zh) * | 2018-10-23 | 2025-07-11 | G·E·霍格 | 用于治疗肺的组合物和方法 |
| CN114945408B (zh) | 2019-10-15 | 2024-04-16 | 勃林格殷格翰国际有限公司 | 作为trpa1抑制剂的噻吩并嘧啶酮 |
| CA3153618A1 (en) * | 2019-10-15 | 2021-04-22 | Boehringer Ingelheim International Gmbh | Thienopyrimidones as trpa1 inhibitors |
| WO2021216749A1 (en) * | 2020-04-22 | 2021-10-28 | George Edward Hoag | Method for treating viral and bacterial infection through inhalation therapy |
| CN111437275B (zh) * | 2020-05-14 | 2021-03-19 | 黑龙江中医药大学 | 一种用于外科手术后抗炎和镇痛的药物及其应用 |
| US12180223B2 (en) | 2021-04-14 | 2024-12-31 | Boehringer Ingelheim International Gmbh | 3H,4H-thieno[2,3-d]pyrimidin-4-one derivatives as TRPA1 inhibitors |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2518916A1 (en) | 2003-04-03 | 2004-10-21 | Joseph R. Garlich | Pi-3 kinase inhibitor prodrugs |
| TW200720264A (en) * | 2005-04-25 | 2007-06-01 | Lundbeck & Co As H | Pro-drugs of n-thiazol-2-yl-benzamide derivatives |
| TWI610684B (zh) | 2005-12-22 | 2018-01-11 | 海卓勒生物科學公司 | 用於調節trpa1功能之化合物 |
| DK2170309T3 (en) * | 2007-06-22 | 2017-01-09 | Hydra Biosciences Inc | Dioxo-2,6, -2,3-dihydro-1H-purine compounds useful in the treatment of diseases related to activity of TRPA1 channel |
| WO2009118596A2 (en) | 2008-03-26 | 2009-10-01 | Glenmark Pharmaceuticals, S. A. | Phthalimide derivatives as trpa1 modulators |
| WO2009144548A1 (en) | 2008-05-28 | 2009-12-03 | Glenmark Pharmaceuticals S.A. | Imidazo [2,1-b] purine derivatives as trpa1 modulators |
| WO2010004390A1 (en) | 2008-06-17 | 2010-01-14 | Glenmark Pharmaceuticals, S.A. | Quinazoline dione derivatives as trpa1 modulators |
| WO2009158719A2 (en) | 2008-06-27 | 2009-12-30 | Hydra Biosciences, Inc. | Methods and compositions for treating disorders |
| TW201026700A (en) | 2008-12-22 | 2010-07-16 | Hydra Biosciences Inc | Compositions useful for treating disorders related to TRPA1 |
| US8623880B2 (en) * | 2009-03-23 | 2014-01-07 | Glenmark Pharmaceuticals S.A. | Fused pyrimidine-dione derivatives as TRPA1 modulators |
| PT2411397E (pt) | 2009-03-23 | 2013-06-06 | Glenmark Pharmaceuticals Sa | Derivados de isotiazolo-pirimidinadiona como moduladores de trpa1 |
| CN102361874A (zh) | 2009-03-23 | 2012-02-22 | 格兰马克药品股份有限公司 | 作为trpa1调节剂的呋喃并嘧啶二酮衍生物 |
| MX2011009824A (es) | 2009-03-23 | 2012-01-25 | Glenmark Pharmaceuticals Sa | Derivados de pirimidina-diona fusionados como moduladores del trpa1. |
| WO2010125469A1 (en) | 2009-04-29 | 2010-11-04 | Glenmark Pharmaceuticals, S.A. | Pyrimidinedione-fused heterocyclic compounds as trpa1 modulators |
| WO2010132838A1 (en) | 2009-05-14 | 2010-11-18 | Hydra Biosciences, Inc. | Compounds useful for treating disorders related to trpa1 |
| WO2011114184A1 (en) | 2010-03-15 | 2011-09-22 | Glenmark Pharmaceuticals S.A. | Amides of heterocyclic compounds as trpa1 inhibitors |
| WO2011132017A1 (en) | 2010-04-19 | 2011-10-27 | Glenmark Pharmaceuticals S.A. | Pyrido[3,4-d]pyrimidinyl acetamide derivatives as trpa1 modulators |
| EA023141B1 (ru) | 2010-12-20 | 2016-04-29 | Гленмарк Фармасьютикалс С.А. | Соединения 2-амино-4-арилтиазола в качестве антагонистов trpa1 |
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2011
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- 2011-12-15 CN CN201180059690.2A patent/CN103261201B/zh not_active Expired - Fee Related
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- 2011-12-15 EP EP11813377.6A patent/EP2655377B1/en not_active Not-in-force
- 2011-12-15 PH PH1/2013/501290A patent/PH12013501290A1/en unknown
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- 2011-12-15 CA CA2820448A patent/CA2820448A1/en not_active Abandoned
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