JP2014518286A5 - - Google Patents
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- Publication number
- JP2014518286A5 JP2014518286A5 JP2014519557A JP2014519557A JP2014518286A5 JP 2014518286 A5 JP2014518286 A5 JP 2014518286A5 JP 2014519557 A JP2014519557 A JP 2014519557A JP 2014519557 A JP2014519557 A JP 2014519557A JP 2014518286 A5 JP2014518286 A5 JP 2014518286A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- alkyl
- substituents
- alkyloxy
- optionally substituted
- 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.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 claims 25
- 125000003545 alkoxy group Chemical group 0.000 claims 24
- 125000001424 substituent group Chemical group 0.000 claims 22
- 229910052739 hydrogen Inorganic materials 0.000 claims 16
- 239000001257 hydrogen Substances 0.000 claims 16
- 125000001153 fluoro group Chemical group F* 0.000 claims 14
- 125000005843 halogen group Chemical group 0.000 claims 13
- 125000004093 cyano group Chemical group *C#N 0.000 claims 12
- 150000002431 hydrogen Chemical class 0.000 claims 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 12
- 125000004076 pyridyl group Chemical group 0.000 claims 11
- 150000001875 compounds Chemical class 0.000 claims 9
- 125000003226 pyrazolyl group Chemical group 0.000 claims 7
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 4
- 206010012289 Dementia Diseases 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- -1 NR 7 R 8 Chemical group 0.000 claims 4
- 125000002757 morpholinyl group Chemical group 0.000 claims 4
- 125000001376 1,2,4-triazolyl group Chemical group N1N=C(N=C1)* 0.000 claims 3
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000002883 imidazolyl group Chemical group 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000002971 oxazolyl group Chemical group 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 102000013455 Amyloid beta-Peptides Human genes 0.000 claims 1
- 108010090849 Amyloid beta-Peptides Proteins 0.000 claims 1
- 208000005145 Cerebral amyloid angiopathy Diseases 0.000 claims 1
- 201000010374 Down Syndrome Diseases 0.000 claims 1
- 206010061216 Infarction Diseases 0.000 claims 1
- 208000009829 Lewy Body Disease Diseases 0.000 claims 1
- 201000002832 Lewy body dementia Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 1
- 206010044688 Trisomy 21 Diseases 0.000 claims 1
- 230000032683 aging Effects 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 208000017004 dementia pugilistica Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 230000007574 infarction Effects 0.000 claims 1
- 208000027061 mild cognitive impairment Diseases 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 230000009529 traumatic brain injury Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11174120.3 | 2011-07-15 | ||
| EP11174120 | 2011-07-15 | ||
| PCT/EP2012/063667 WO2013010904A1 (en) | 2011-07-15 | 2012-07-12 | Novel substituted indole derivatives as gamma secretase modulators |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014518286A JP2014518286A (ja) | 2014-07-28 |
| JP2014518286A5 true JP2014518286A5 (OSRAM) | 2015-08-20 |
| JP6068464B2 JP6068464B2 (ja) | 2017-01-25 |
Family
ID=46506432
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014519557A Expired - Fee Related JP6068464B2 (ja) | 2011-07-15 | 2012-07-12 | γ−セクレターゼ調節剤としての新規な置換インドール誘導体 |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US9115143B2 (OSRAM) |
| EP (1) | EP2731948B1 (OSRAM) |
| JP (1) | JP6068464B2 (OSRAM) |
| KR (1) | KR101913135B1 (OSRAM) |
| CN (1) | CN103874702B (OSRAM) |
| AR (1) | AR087182A1 (OSRAM) |
| AU (1) | AU2012285931B2 (OSRAM) |
| BR (1) | BR112014000713A2 (OSRAM) |
| CA (1) | CA2841102C (OSRAM) |
| EA (1) | EA023045B1 (OSRAM) |
| ES (1) | ES2555167T3 (OSRAM) |
| IL (1) | IL230422B (OSRAM) |
| IN (1) | IN2014MN00258A (OSRAM) |
| MX (1) | MX2014000626A (OSRAM) |
| TW (1) | TWI567079B (OSRAM) |
| WO (1) | WO2013010904A1 (OSRAM) |
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010089292A1 (en) | 2009-02-06 | 2010-08-12 | Ortho-Mcneil-Janssen Pharmaceuticals, Inc | Novel substituted bicyclic heterocyclic compounds as gamma secretase modulators |
| WO2010145883A1 (en) | 2009-05-07 | 2010-12-23 | Ortho-Mcneil-Janssen Pharmaceuticals, Inc | Novel substituted indazole and aza-indazole derivatives as gamma secretase modulators |
| EA021047B1 (ru) | 2009-07-15 | 2015-03-31 | Янссен Фармасьютикалз, Инк. | Замещенные производные триазола и имидазола в качестве модуляторов гамма-секретазы |
| MX2012008260A (es) | 2010-01-15 | 2012-08-17 | Janssen Pharmaceuticals Inc | Novedosos derivados de triazol sustituidos como moduladores de la gamma secretasa. |
| AU2012230348A1 (en) | 2011-03-24 | 2013-08-29 | Cellzome Limited | Novel substituted triazolyl piperazine and triazolyl piperidine derivatives as gamma secretase modulators |
| WO2013010904A1 (en) | 2011-07-15 | 2013-01-24 | Janssen Pharmaceuticals, Inc. | Novel substituted indole derivatives as gamma secretase modulators |
| AU2013261023B2 (en) | 2012-05-16 | 2016-11-24 | Cellzome Limited | Substituted 3, 4 - dihydro - 2H - pyrido [1, 2 -a] pyrazine - 1, 6 - dione derivatives useful for the treatment of (inter alia) Alzheimer's disease |
| EP2738172A1 (en) * | 2012-11-28 | 2014-06-04 | Almirall, S.A. | New bicyclic compounds as crac channel modulators |
| JP6275161B2 (ja) | 2012-12-20 | 2018-02-07 | ヤンセン ファーマシューティカ エヌ.ベー. | γセクレターゼ調節剤としての新規な三環式3,4−ジヒドロ−2H−ピリド[1,2−a]ピラジン−1,6−ジオン誘導体 |
| CA2891755C (en) | 2013-01-17 | 2021-10-26 | Janssen Pharmaceutica Nv | Substituted pyrido-piperazinone derivatives as gamma secretase modulators |
| US10562897B2 (en) | 2014-01-16 | 2020-02-18 | Janssen Pharmaceutica Nv | Substituted 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-diones as gamma secretase modulators |
| GB201506660D0 (en) | 2015-04-20 | 2015-06-03 | Cellcentric Ltd | Pharmaceutical compounds |
| GB201506658D0 (en) | 2015-04-20 | 2015-06-03 | Cellcentric Ltd | Pharmaceutical compounds |
| CA3031675A1 (en) | 2016-07-30 | 2018-02-08 | Bristol-Myers Squibb Company | Dimethoxyphenyl substituted indole compounds as tlr7, tlr8 or tlr9 inhibitors |
| ES2902504T3 (es) | 2016-09-09 | 2022-03-28 | Bristol Myers Squibb Co | Compuestos de indol sustituidos con piridilo |
| JOP20190060A1 (ar) | 2016-09-26 | 2019-03-26 | Chugai Pharmaceutical Co Ltd | مشتق بيرازولو بيريدين له تأثير مساعد لمستقبل glp-1 |
| WO2019028301A1 (en) | 2017-08-04 | 2019-02-07 | Bristol-Myers Squibb Company | INDOLE COMPOUNDS SUBSTITUTED WITH [1,2,4] TRIAZOLO [4,3-A] PYRIDINYL |
| ES2909401T3 (es) | 2017-08-04 | 2022-05-06 | Bristol Myers Squibb Co | Compuestos de indol sustituidos útiles como inhibidores de TLR7/8/9 |
| AU2018348930A1 (en) * | 2017-10-11 | 2020-03-26 | F. Hoffmann-La Roche Ag | Bicyclic compounds for use as RIP 1 kinase inhibitors |
| EP3710440B1 (en) * | 2017-11-14 | 2023-04-05 | Bristol-Myers Squibb Company | Substituted indole compounds |
| US12030878B2 (en) | 2017-12-15 | 2024-07-09 | Bristol-Myers Squibb Company | Substituted indole ether compounds |
| SI3728252T1 (sl) | 2017-12-18 | 2023-11-30 | Bristol-Myers Squibb Company | 4-azaindolne spojine |
| CN111491930B (zh) | 2017-12-19 | 2023-09-26 | 百时美施贵宝公司 | 可用作tlr抑制剂的经取代的吲哚化合物 |
| AU2018392316B2 (en) | 2017-12-19 | 2022-05-12 | Bristol-Myers Squibb Company | Amide substituted indole compounds useful as TLR inhibitors |
| JP7304352B2 (ja) | 2017-12-19 | 2023-07-06 | ブリストル-マイヤーズ スクイブ カンパニー | 6-アザインドール化合物 |
| AU2018390544A1 (en) | 2017-12-20 | 2020-08-06 | Bristol-Myers Squibb Company | Diazaindole compounds |
| AU2018390610A1 (en) | 2017-12-20 | 2020-08-06 | Bristol-Myers Squibb Company | Amino indole compounds useful as TLR inhibitors |
| US11420958B2 (en) | 2017-12-20 | 2022-08-23 | Bristol-Myers Squibb Company | Aryl and heteroaryl substituted indole compounds |
| HUE064554T2 (hu) * | 2018-09-03 | 2024-03-28 | Hoffmann La Roche | Bicikluszos heteroaril származékok |
| EP3628669A1 (en) * | 2018-09-28 | 2020-04-01 | GenKyoTex Suisse SA | Novel compounds as nadph oxidase inhibitors |
| US12172995B2 (en) | 2018-10-24 | 2024-12-24 | Bristol-Myers Squibb Company | Substituted indole and indazole compounds |
| US11998537B2 (en) | 2018-10-24 | 2024-06-04 | Bristol-Myers Squibb Company | Substituted indole dimer compounds |
| PL3894411T3 (pl) | 2018-12-13 | 2024-10-07 | F. Hoffmann-La Roche Ag | Pochodne 7-fenoksy-N-(3-azabicyklo[3.2.1]oktan-8-ylo)-6,7-dihydro-5H-pirolo[1,2-b][1,2,4]triazolo-2-aminy i związki pokrewne jako modulatory gamma-sekretazy do leczenia choroby Alzheimera |
| ES2987832T3 (es) | 2019-05-09 | 2024-11-18 | Bristol Myers Squibb Co | Compuestos de benzimidazolona sustituidos |
| KR20220075381A (ko) | 2019-10-01 | 2022-06-08 | 브리스톨-마이어스 스큅 컴퍼니 | 치환된 비시클릭 헤테로아릴 화합물 |
| WO2021067657A1 (en) | 2019-10-04 | 2021-04-08 | Bristol-Myers Squibb Company | Substituted carbazole compounds |
Family Cites Families (65)
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| DE69321875T2 (de) * | 1992-05-19 | 1999-06-17 | Adir Et Compagnie, Courbevoie | Benzimidezolderivate mit antidiabetischer und Anti-Plättchenklumpungswirkung |
| US5767144A (en) | 1994-08-19 | 1998-06-16 | Abbott Laboratories | Endothelin antagonists |
| US6114334A (en) | 1995-07-13 | 2000-09-05 | Knoll Aktiengesellschaft | Piperazine derivatives as therapeutic agents |
| CN1156445C (zh) | 1999-06-10 | 2004-07-07 | 沃尼尔·朗伯公司 | 采用二氢异吲哚衍生物抑制淀粉样蛋白聚集和使淀粉样蛋白沉积成像的方法 |
| CA2406383A1 (en) | 2000-04-13 | 2001-10-25 | Mayo Foundation For Medical Education And Research | A.beta.42 lowering agents |
| WO2001087845A2 (en) | 2000-05-15 | 2001-11-22 | Fujisawa Pharmaceutical Co., Ltd. | N-containing heterocyclic compounds and their use as 5-ht antagonists |
| DE10109867A1 (de) | 2001-03-01 | 2002-09-05 | Abbott Gmbh & Co Kg | Verwendung von Triazolverbindungen zur Prophylaxe und Therapie neurodegenerativer Erkrankungen, Hirntrauma und zerebraler Ischämie |
| DE10238002A1 (de) | 2002-08-20 | 2004-03-04 | Merck Patent Gmbh | Benzimidazolderivate |
| BRPI0407913A (pt) | 2003-02-27 | 2006-03-01 | Hoffmann La Roche | antagonistas receptores de ccr-3 |
| WO2004110350A2 (en) | 2003-05-14 | 2004-12-23 | Torreypines Therapeutics, Inc. | Compouds and uses thereof in modulating amyloid beta |
| AU2004265101B2 (en) | 2003-08-14 | 2009-06-11 | F. Hoffmann-La Roche Ag | Gabanergic modulators |
| ATE483708T1 (de) | 2004-03-08 | 2010-10-15 | Prosidion Ltd | Pyrrolopyridin-2-carbonsäurehydrazide als inhibitoren von glykogenphosphorylase |
| US7667041B2 (en) | 2004-05-26 | 2010-02-23 | Eisai R&D Management Co., Ltd. | Cinnamide compound |
| KR20070083781A (ko) | 2004-10-26 | 2007-08-24 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 신나미드 화합물의 비정질체 |
| US7893267B2 (en) * | 2005-03-14 | 2011-02-22 | High Point Pharmaceuticals, Llc | Benzazole derivatives, compositions, and methods of use as β-secretase inhibitors |
| US7572807B2 (en) | 2005-06-09 | 2009-08-11 | Bristol-Myers Squibb Company | Heteroaryl 11-beta-hydroxysteroid dehydrogenase type I inhibitors |
| US20070078136A1 (en) | 2005-09-22 | 2007-04-05 | Bristol-Myers Squibb Company | Fused heterocyclic compounds useful as kinase modulators |
| BRPI0616150A2 (pt) | 2005-09-22 | 2011-06-07 | Sanofi Aventis | derivados de amino-alquil-amida como lìquidos receptores de ccr3 |
| WO2007043786A1 (en) | 2005-10-10 | 2007-04-19 | Seiyang Yang | Dynamic-based verification apparatus for verification from electronic system level to gate level, and verification method using the same |
| EP1937767B1 (en) | 2005-10-11 | 2013-05-22 | Chemtura Corporation | Diaromatic amines |
| AR056785A1 (es) | 2005-11-10 | 2007-10-24 | Schering Corp | COMPUESTOS DE IMIDAZO[1,2-A]PIRAZINAS, uTILES COMO INHIBIDORES, REGULADORES O MODULADORES DE PROTEINQUINASAS |
| US20090163482A1 (en) | 2006-03-13 | 2009-06-25 | Mchardy Stanton Furst | Tetralines antagonists of the h-3 receptor |
| GB0606774D0 (en) | 2006-04-03 | 2006-05-10 | Novartis Ag | Organic compounds |
| US7893058B2 (en) | 2006-05-15 | 2011-02-22 | Janssen Pharmaceutica Nv | Imidazolopyrazine compounds useful for the treatment of degenerative and inflammatory diseases |
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| JP2010512390A (ja) | 2006-12-12 | 2010-04-22 | シェーリング コーポレイション | 三環式系を含むアスパルチルプロテアーゼ阻害剤 |
| US20100298314A1 (en) | 2006-12-20 | 2010-11-25 | Schering Corporation | Novel jnk inhibitors |
| WO2008097538A1 (en) | 2007-02-08 | 2008-08-14 | Merck & Co., Inc. | Therapeutic agents |
| CA2676715A1 (en) | 2007-02-12 | 2008-08-21 | Merck & Co., Inc. | Piperazine derivatives for treatment of ad and related conditions |
| CA2676920A1 (en) | 2007-02-12 | 2008-08-21 | Merck & Co., Inc. | Piperidine derivatives |
| MX2009012177A (es) | 2007-05-07 | 2009-11-23 | Schering Corp | Moduladores de gamma-secretasa. |
| MX2009012163A (es) | 2007-05-11 | 2009-12-01 | Hoffmann La Roche | Hetarilanilinas como moduladores para beta-amiloide. |
| WO2008156580A1 (en) | 2007-06-13 | 2008-12-24 | Merck & Co., Inc. | Triazole derivatives for treating alzheimer's disease and related conditions |
| CL2008001914A1 (es) | 2007-06-29 | 2009-07-17 | Schering Corp | Compuestos heterociclicos de nitrogeno y oxigeno,moduladores de gama secretasa, composicion farmaceutica de dichos compuestos; kit farmaceutico y su uso para prevenir o tratar enfermedades asociadas al sistema nervioso central como alzheimer, sindrome de down, enfermedades neurodegenerativas, inhibir el deposito de proteina amiloide. |
| US7935815B2 (en) | 2007-08-31 | 2011-05-03 | Eisai R&D Management Co., Ltd. | Imidazoyl pyridine compounds and salts thereof |
| EP2200990A1 (en) | 2007-09-06 | 2010-06-30 | Schering Corporation | Gamma secretase modulators |
| GB0720444D0 (en) | 2007-10-18 | 2007-11-28 | Glaxo Group Ltd | Novel compounds |
| AU2008333865A1 (en) | 2007-12-06 | 2009-06-11 | Schering Corporation | Gamma secretase modulators |
| US8426595B2 (en) | 2007-12-11 | 2013-04-23 | Xianhai Huang | Gamma secretase modulators |
| RU2010137300A (ru) | 2008-02-22 | 2012-03-27 | Ф. Хоффманн-Ля Рош Аг (Ch) | Модуляторы бета-амилоида |
| US20100137320A1 (en) | 2008-02-29 | 2010-06-03 | Schering Corporation | Gamma secretase modulators |
| WO2010010188A1 (en) | 2008-07-25 | 2010-01-28 | Galapagos Nv | Novel compounds useful for the treatment of degenerative and inflammatory diseases. |
| EP2340243B1 (en) | 2008-10-17 | 2014-10-08 | Boehringer Ingelheim International GmbH | Heteroaryl substituted indole compounds useful as mmp-13 inhibitors |
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| TWI461425B (zh) | 2009-02-19 | 2014-11-21 | Janssen Pharmaceuticals Inc | 作為伽瑪分泌酶調節劑之新穎經取代的苯并唑、苯并咪唑、唑并吡啶及咪唑并吡啶衍生物類 |
| RU2515976C2 (ru) | 2009-02-26 | 2014-05-20 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Азотсодержащие конденсированные гетероциклические соединения и их применение в качестве ингибиторов продукции бета-амилоида |
| JP2012051806A (ja) * | 2009-02-26 | 2012-03-15 | Eisai R & D Management Co Ltd | イミダゾリルピラジン誘導体 |
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| EP2410529A1 (en) | 2009-03-16 | 2012-01-25 | Panasonic Corporation | Application running device |
| US20120029190A1 (en) * | 2009-04-03 | 2012-02-02 | Douglas Burdi | Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof |
| EP2424866A1 (en) * | 2009-04-27 | 2012-03-07 | High Point Pharmaceuticals, LLC | Substituted imidazo[1,2-a]pyridine derivatives, pharmaceutical compositions, and methods of use as -secretase inhibitors |
| WO2010145883A1 (en) | 2009-05-07 | 2010-12-23 | Ortho-Mcneil-Janssen Pharmaceuticals, Inc | Novel substituted indazole and aza-indazole derivatives as gamma secretase modulators |
| JP2010274429A (ja) | 2009-05-26 | 2010-12-09 | Ihi Corp | アライメントステージ |
| EA021047B1 (ru) | 2009-07-15 | 2015-03-31 | Янссен Фармасьютикалз, Инк. | Замещенные производные триазола и имидазола в качестве модуляторов гамма-секретазы |
| MX2012008260A (es) | 2010-01-15 | 2012-08-17 | Janssen Pharmaceuticals Inc | Novedosos derivados de triazol sustituidos como moduladores de la gamma secretasa. |
| TW201307347A (zh) * | 2010-11-01 | 2013-02-16 | Arqule Inc | 經取代苯並-咪唑並-吡啶並-二氮呯化合物 |
| AU2012230348A1 (en) | 2011-03-24 | 2013-08-29 | Cellzome Limited | Novel substituted triazolyl piperazine and triazolyl piperidine derivatives as gamma secretase modulators |
| JP5767393B2 (ja) | 2011-03-31 | 2015-08-19 | ファイザー・インク | 新規二環式ピリジノン |
| WO2013010904A1 (en) | 2011-07-15 | 2013-01-24 | Janssen Pharmaceuticals, Inc. | Novel substituted indole derivatives as gamma secretase modulators |
-
2012
- 2012-07-12 WO PCT/EP2012/063667 patent/WO2013010904A1/en not_active Ceased
- 2012-07-12 KR KR1020147003465A patent/KR101913135B1/ko not_active Expired - Fee Related
- 2012-07-12 CN CN201280034912.XA patent/CN103874702B/zh not_active Expired - Fee Related
- 2012-07-12 ES ES12733754.1T patent/ES2555167T3/es active Active
- 2012-07-12 BR BR112014000713A patent/BR112014000713A2/pt active Search and Examination
- 2012-07-12 MX MX2014000626A patent/MX2014000626A/es unknown
- 2012-07-12 EP EP12733754.1A patent/EP2731948B1/en active Active
- 2012-07-12 IN IN258MUN2014 patent/IN2014MN00258A/en unknown
- 2012-07-12 TW TW101125035A patent/TWI567079B/zh not_active IP Right Cessation
- 2012-07-12 EA EA201490287A patent/EA023045B1/ru not_active IP Right Cessation
- 2012-07-12 JP JP2014519557A patent/JP6068464B2/ja not_active Expired - Fee Related
- 2012-07-12 AU AU2012285931A patent/AU2012285931B2/en not_active Ceased
- 2012-07-12 CA CA2841102A patent/CA2841102C/en not_active Expired - Fee Related
- 2012-07-12 US US14/233,078 patent/US9115143B2/en not_active Expired - Fee Related
- 2012-07-13 AR ARP120102548A patent/AR087182A1/es not_active Application Discontinuation
-
2014
- 2014-01-13 IL IL230422A patent/IL230422B/en active IP Right Grant
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