ES2618630T3 - Composiciones terapéuticas y métodos de uso relacionados - Google Patents
Composiciones terapéuticas y métodos de uso relacionados Download PDFInfo
- Publication number
- ES2618630T3 ES2618630T3 ES10794667.5T ES10794667T ES2618630T3 ES 2618630 T3 ES2618630 T3 ES 2618630T3 ES 10794667 T ES10794667 T ES 10794667T ES 2618630 T3 ES2618630 T3 ES 2618630T3
- Authority
- ES
- Spain
- Prior art keywords
- optionally substituted
- alkyl
- aralkyl
- aryl
- heteroaralkyl
- 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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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/36—Sulfur atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
- C07D213/30—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
- C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D257/04—Five-membered rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
- C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
- C07D263/58—Benzoxazoles; Hydrogenated benzoxazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
- C07D265/34—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
- C07D265/36—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/22—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with hetero atoms directly attached to ring nitrogen atoms
- C07D295/26—Sulfur atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D319/00—Heterocyclic compounds containing six-membered rings having two oxygen atoms as the only ring hetero atoms
- C07D319/10—1,4-Dioxanes; Hydrogenated 1,4-dioxanes
- C07D319/14—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems
- C07D319/16—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems condensed with one six-membered ring
- C07D319/18—Ethylenedioxybenzenes, not substituted on the hetero ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D339/00—Heterocyclic compounds containing rings having two sulfur atoms as the only ring hetero atoms
- C07D339/02—Five-membered rings
- C07D339/06—Five-membered rings having the hetero atoms in positions 1 and 3, e.g. cyclic dithiocarbonates
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Transplantation (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
Un compuesto de fórmula (II)**Fórmula** o una de sus sales farmacéuticamente aceptables, en donde: n es 1 o 2; X es O, S, o cicloalquilenilo; R1 se selecciona entre alquilo opcionalmente sustituido, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, heterociclilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido, un aralquilo opcionalmente sustituido, o heteroaralquilo opcionalmente sustituido; y R2 es quinolinilo opcionalmente sustituido; en donde alquilo opcionalmente sustituido, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, heterociclilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido, un aralquilo opcionalmente sustituido, o heteroaralquilo opcionalmente sustituido es opcionalmente sustituido con uno o más de los siguientes grupos: alquilo; cicloalquilo; haloalquilo; arilo; heteroarilo; aralquilo; heteroaralquilo; heterociclilo; alquenilo; alquinilo; cicloalquenilo; heterocicloalquenilo; alcoxi; haloalcoxi; halo; hidroxi; carboxi; carboxilato; ciano; nitro; amino; alquilamino; SO3H; sulfato; fosfato; metilenodioxi (-O-CH2-O- en donde los oxígenos están unidos a los átomos vecinales); etilenodioxi; oxo; tioxo; imino (alquilo, arilo, aralquilo); S(O)n alquilo (donde n es 0-2); S(O)n arilo (donde n es 0-2); S(O)n heteroarilo (donde n es 0-2); S(O)n heterociclilo (donde n es 0-2); amina (mono-, di-, alquilo, cicloalquilo, aralquilo, heteroaralquilo, arilo, heteroarilo, y combinaciones de los mismos); éster (alquilo, aralquilo, heteroaralquilo, arilo, heteroarilo); amida (mono-, di-, alquilo, aralquilo, heteroaralquilo, arilo, heteroarilo, y combinaciones de los mismos); sulfonamida (mono-, di-, alquilo, aralquilo, heteroaralquilo, y combinaciones de los mismos).
Description
Tabla 1
- Compuesto
- EC50
- imagen12
- A
- A
- A
- imagen13
- A
- imagen14
- B
- imagen15
- A
- A
- B
13
- A
- C
- B
- imagen16
- A
- A
- A
- imagen17
- A
- imagen18
- A
14
- B
- A
- A
- A
- A
- A
- A
15
- B
- A
- A
- imagen19
- A
- imagen20
- A
- A
- A
- C
16
- A
- A
- A
- A
- A
- A
- A
- B
- B
17
Claims (1)
-
imagen1 imagen2 imagen3 imagen4
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US22140609P | 2009-06-29 | 2009-06-29 | |
US221406P | 2009-06-29 | ||
PCT/US2010/040485 WO2011002816A1 (en) | 2009-06-29 | 2010-06-29 | Therapeutic compositions and related methods of use |
Publications (1)
Publication Number | Publication Date |
---|---|
ES2618630T3 true ES2618630T3 (es) | 2017-06-21 |
Family
ID=43411414
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ES10794667.5T Active ES2618630T3 (es) | 2009-06-29 | 2010-06-29 | Composiciones terapéuticas y métodos de uso relacionados |
Country Status (8)
Country | Link |
---|---|
US (1) | US9115086B2 (es) |
EP (1) | EP2448581B1 (es) |
JP (2) | JP5764555B2 (es) |
CA (1) | CA2766873C (es) |
DK (1) | DK2448581T3 (es) |
ES (1) | ES2618630T3 (es) |
PL (1) | PL2448581T3 (es) |
WO (1) | WO2011002816A1 (es) |
Families Citing this family (41)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA2758071C (en) | 2009-04-06 | 2018-01-09 | Agios Pharmaceuticals, Inc. | Pyruvate kinase m2 modulators, therapeutic compositions and related methods of use |
DK2448582T3 (en) | 2009-06-29 | 2017-07-17 | Agios Pharmaceuticals Inc | QUINOLIN-8 SULPHONAMIDE DERIVATIVES WITH ANTICANCER ACTIVITY |
EP2632920A1 (en) | 2010-10-27 | 2013-09-04 | Dynamix Pharmaceuticals Ltd. | Sulfonamides for the modulation of pkm2 |
EP2655350B1 (en) | 2010-12-21 | 2016-03-09 | Agios Pharmaceuticals, Inc. | Bicyclic pkm2 activators |
SI3406251T1 (sl) | 2011-05-03 | 2024-05-31 | Agios Pharmaceuticals, Inc. | Aktivatorji piruvat kinaze za uporabo v terapiji |
WO2012151440A1 (en) | 2011-05-03 | 2012-11-08 | Agios Pharmaceuticals, Inc. | Pyruvate kinase activators for use for increasing lifetime of the red blood cells and treating anemia |
WO2013155223A1 (en) * | 2012-04-10 | 2013-10-17 | The Regents Of The University Of California | Compositions and methods for treating cancer |
KR20150080619A (ko) * | 2012-11-08 | 2015-07-09 | 아지오스 파마슈티컬스 아이엔씨. | 치료적 화합물 및 조성물 |
US9227978B2 (en) | 2013-03-15 | 2016-01-05 | Araxes Pharma Llc | Covalent inhibitors of Kras G12C |
TWI659021B (zh) | 2013-10-10 | 2019-05-11 | 亞瑞克西斯製藥公司 | Kras g12c之抑制劑 |
AU2016245864C1 (en) | 2015-04-10 | 2021-09-09 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
JP6789239B2 (ja) | 2015-04-15 | 2020-11-25 | アラクセス ファーマ エルエルシー | Krasの縮合三環系インヒビターおよびその使用の方法 |
ES2959690T3 (es) | 2015-06-11 | 2024-02-27 | Agios Pharmaceuticals Inc | Procedimientos de uso de activadores de piruvato cinasa |
US10144724B2 (en) | 2015-07-22 | 2018-12-04 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
WO2017053510A1 (en) * | 2015-09-23 | 2017-03-30 | The Scripps Research Institute | Small molecule modulators of cellular lipolysis |
US10647703B2 (en) | 2015-09-28 | 2020-05-12 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
EP3356349A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
EP3356347A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
WO2017058728A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
EP3356339A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
EP3356354A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
EP3356359B1 (en) | 2015-09-28 | 2021-10-20 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
WO2017087528A1 (en) | 2015-11-16 | 2017-05-26 | Araxes Pharma Llc | 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof |
US10822312B2 (en) | 2016-03-30 | 2020-11-03 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use |
US10646488B2 (en) | 2016-07-13 | 2020-05-12 | Araxes Pharma Llc | Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof |
CN110036010A (zh) | 2016-09-29 | 2019-07-19 | 亚瑞克西斯制药公司 | Kras g12c突变蛋白的抑制剂 |
WO2018068017A1 (en) | 2016-10-07 | 2018-04-12 | Araxes Pharma Llc | Heterocyclic compounds as inhibitors of ras and methods of use thereof |
EP3573964A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Benzothiophene and benzothiazole compounds and methods of use thereof |
WO2018140512A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | Fused bicyclic benzoheteroaromatic compounds and methods of use thereof |
EP3573967A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Fused hetero-hetero bicyclic compounds and methods of use thereof |
US11279689B2 (en) | 2017-01-26 | 2022-03-22 | Araxes Pharma Llc | 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1 yl)prop-2-en-1-one derivatives and similar compounds as KRAS G12C modulators for treating cancer |
US11136308B2 (en) | 2017-01-26 | 2021-10-05 | Araxes Pharma Llc | Substituted quinazoline and quinazolinone compounds and methods of use thereof |
SI3448859T1 (sl) | 2017-03-20 | 2020-02-28 | Forma Therapeutics, Inc. | Sestavki pirolopirola kot aktivatorji piruvat kinaze (PKR) |
KR20200010306A (ko) | 2017-05-25 | 2020-01-30 | 아락세스 파마 엘엘씨 | Kras의 공유적 억제제 |
US10736897B2 (en) | 2017-05-25 | 2020-08-11 | Araxes Pharma Llc | Compounds and methods of use thereof for treatment of cancer |
US11639346B2 (en) | 2017-05-25 | 2023-05-02 | Araxes Pharma Llc | Quinazoline derivatives as modulators of mutant KRAS, HRAS or NRAS |
CN110372574A (zh) * | 2018-04-13 | 2019-10-25 | 中国药科大学 | 哌啶类ampk激动剂及其医药用途 |
EP3852791B1 (en) | 2018-09-19 | 2024-07-03 | Novo Nordisk Health Care AG | Activating pyruvate kinase r |
US20200129485A1 (en) | 2018-09-19 | 2020-04-30 | Forma Therapeutics, Inc. | Treating sickle cell disease with a pyruvate kinase r activating compound |
US20220380310A1 (en) * | 2019-07-01 | 2022-12-01 | Ligang Qian | P2x7r antagonists |
WO2022170200A1 (en) | 2021-02-08 | 2022-08-11 | Global Blood Therapeutics, Inc. | 1-(2-sulfonyl-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4h)-yl]-ethanone derivatives as pyruvate kinase (pkr) and pkm2 activators for the treatment of sickle cell disease |
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2010
- 2010-06-29 PL PL10794667T patent/PL2448581T3/pl unknown
- 2010-06-29 ES ES10794667.5T patent/ES2618630T3/es active Active
- 2010-06-29 CA CA2766873A patent/CA2766873C/en not_active Expired - Fee Related
- 2010-06-29 DK DK10794667.5T patent/DK2448581T3/en active
- 2010-06-29 EP EP10794667.5A patent/EP2448581B1/en not_active Not-in-force
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2015
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Also Published As
Publication number | Publication date |
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PL2448581T3 (pl) | 2017-06-30 |
WO2011002816A1 (en) | 2011-01-06 |
CA2766873A1 (en) | 2011-01-06 |
JP2015078232A (ja) | 2015-04-23 |
EP2448581A4 (en) | 2013-02-20 |
JP5764555B2 (ja) | 2015-08-19 |
JP2012532136A (ja) | 2012-12-13 |
EP2448581A1 (en) | 2012-05-09 |
CA2766873C (en) | 2018-08-21 |
DK2448581T3 (en) | 2017-03-13 |
US9115086B2 (en) | 2015-08-25 |
EP2448581B1 (en) | 2016-12-07 |
US20120165324A1 (en) | 2012-06-28 |
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