PE20040988A1 - Nuevos compuestos de pirazol como inhibidores del factor de crecimiento transformante (tgf) - Google Patents
Nuevos compuestos de pirazol como inhibidores del factor de crecimiento transformante (tgf)Info
- Publication number
- PE20040988A1 PE20040988A1 PE2003000940A PE2003000940A PE20040988A1 PE 20040988 A1 PE20040988 A1 PE 20040988A1 PE 2003000940 A PE2003000940 A PE 2003000940A PE 2003000940 A PE2003000940 A PE 2003000940A PE 20040988 A1 PE20040988 A1 PE 20040988A1
- Authority
- PE
- Peru
- Prior art keywords
- tgf
- inhibitors
- growth factor
- transforming growth
- pyrazole compounds
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- 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
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Dermatology (AREA)
- Hematology (AREA)
- Emergency Medicine (AREA)
- Obesity (AREA)
- Vascular Medicine (AREA)
- Gastroenterology & Hepatology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
SE REFIERE A UN COMPUESTO DE FORMULA Ia, DONDE R1 ES ANILLO SATURADO, INSATURADO O AROMATICO C3-C20, MONO- O BICICLICO, ENTRE OTROS; R3 ES H, HALO, HALOALQUILO C1-C6, ENTRE OTROS; R4 ES H, HALO, HALOALQUILO C1-C6, ENTRE OTROS; S ES 1-5. R6 ES FENILO, HETEROARILO C5-C10, HETEROCICLO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS:4-[3-(6-METILPIRIDIL-2-IL)-1H-PIRAZOL-4-IL-QUINOLINA, 2-(4-BENZO[1,3]DIOXOL-5-IL-1H-PIRAZOL-3-IL)-6-METILPIRIDINA Y 4-(3-PIRIDIN-2-IL-1H-PIRAZOL-4-IL)QUINOLINA; ENTRE OTROS. DICHOS COMPUESTOS SON INHIBIDORES DEL FACTOR DE CRECIMIENTO TRANSFORMADOR (TGF) Y SON UTILES EN LA PREVENCION O TRATAMIENTO DE PATOLOGIAS RELACIONADAS CON TGF TALES COMO CANCER Y ENFERMEDADES FIBROTICAS
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US41214602P | 2002-09-18 | 2002-09-18 | |
US48454303P | 2003-07-02 | 2003-07-02 |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20040988A1 true PE20040988A1 (es) | 2004-12-25 |
Family
ID=32033585
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2003000940A PE20040988A1 (es) | 2002-09-18 | 2003-09-15 | Nuevos compuestos de pirazol como inhibidores del factor de crecimiento transformante (tgf) |
Country Status (27)
Country | Link |
---|---|
US (4) | US6958354B2 (es) |
EP (2) | EP2165708A3 (es) |
JP (1) | JP4519657B2 (es) |
KR (1) | KR20050044807A (es) |
CN (1) | CN1681501A (es) |
AP (1) | AP2005003263A0 (es) |
AR (1) | AR041272A1 (es) |
AT (1) | ATE450258T1 (es) |
AU (1) | AU2003259475A1 (es) |
BR (1) | BR0314302A (es) |
CA (1) | CA2496295C (es) |
CO (1) | CO5550456A2 (es) |
DE (1) | DE60330362D1 (es) |
EA (1) | EA200500377A1 (es) |
EC (1) | ECSP055679A (es) |
ES (1) | ES2335099T3 (es) |
HR (1) | HRP20050247A2 (es) |
IS (1) | IS7698A (es) |
MA (1) | MA27440A1 (es) |
MX (1) | MXPA05002376A (es) |
NO (1) | NO20050838L (es) |
OA (1) | OA12929A (es) |
PA (1) | PA8583201A1 (es) |
PE (1) | PE20040988A1 (es) |
PL (1) | PL375979A1 (es) |
UY (1) | UY27985A1 (es) |
WO (1) | WO2004026306A2 (es) |
Families Citing this family (29)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AP2005003261A0 (en) | 2002-09-18 | 2005-03-31 | Pfizer Prod Inc | Novel oxazole and thiazole compounds as transforming growth factor (TGF) inhibitors. |
AP2005003264A0 (en) | 2002-09-18 | 2005-03-31 | Pfizer Prod Inc | Novel imidazole compounds as transforming growth factor (TGD) inhibitors. |
PL375979A1 (en) * | 2002-09-18 | 2005-12-12 | Pfizer Products Inc. | Pyrazole derivatives as transforming growth factor (tgf) inhibitors |
CL2004000234A1 (es) * | 2003-02-12 | 2005-04-15 | Biogen Idec Inc | Compuestos derivados 3-(piridin-2-il)-4-heteroaril-pirazol sustituidos, antagonistas de aik5 y/o aik4; composicion farmaceutica y uso del compuesto en el tratamiento de desordenes fibroticos como esclerodermia, lupus nefritico, cicatrizacion de herid |
PA8595001A1 (es) | 2003-03-04 | 2004-09-28 | Pfizer Prod Inc | Nuevos compuestos heteroaromaticos condensados que son inhibidores del factor de crecimiento transforante (tgf) |
GB0313915D0 (en) * | 2003-06-16 | 2003-07-23 | Smithkline Beecham Corp | Compounds |
CA2578628A1 (en) * | 2004-08-31 | 2006-03-09 | Biogen Idec Ma Inc. | Pyrimidinylpyrazoles as tgf-beta inhibitors |
WO2006028029A1 (ja) * | 2004-09-07 | 2006-03-16 | Sankyo Company, Limited | 置換ビフェニル誘導体 |
CA2584248A1 (en) * | 2004-10-15 | 2006-04-27 | Biogen Idec Ma Inc. | Methods of treating vascular injuries |
TW200639163A (en) * | 2005-02-04 | 2006-11-16 | Genentech Inc | RAF inhibitor compounds and methods |
CA2629432A1 (en) * | 2005-12-16 | 2007-06-21 | Alcon, Inc. | Control of intraocular pressure using alk5 modulation agents |
PT2089367E (pt) | 2006-10-31 | 2012-02-01 | Pfizer Prod Inc | Compostos de pirazolina como antagonistas dos receptores mineralcorticóides |
AU2008281543A1 (en) * | 2007-08-01 | 2009-02-05 | Pfizer Inc. | Pyrazole compounds and their use as Raf inhibitors |
ES2813875T3 (es) | 2014-01-01 | 2021-03-25 | Medivation Tech Llc | Compuestos y procedimientos de uso |
WO2016160881A1 (en) | 2015-04-01 | 2016-10-06 | Rigel Pharmaceuticals, Inc. | TGF-β INHIBITORS |
WO2016210292A1 (en) | 2015-06-25 | 2016-12-29 | Children's Medical Center Corporation | Methods and compositions relating to hematopoietic stem cell expansion, enrichment, and maintenance |
AU2017235461B2 (en) | 2016-03-15 | 2023-02-23 | Children's Medical Center Corporation | Methods and compositions relating to hematopoietic stem cell expansion |
EP3470409B1 (en) * | 2016-06-13 | 2020-02-12 | Genfleet Therapeutics (Shanghai) Inc. | Benzotriazole-derived alpha and beta-unsaturated amide compound used as tgf-beta ri inhibitor |
EP3532604A4 (en) * | 2016-10-26 | 2020-06-03 | Icahn School of Medicine at Mount Sinai | METHOD FOR INCREASING CELL PROLIFERATION IN PANCREATIC BETA CELLS, TREATMENT METHOD AND COMPOSITION |
BR112019008516A2 (pt) | 2016-11-14 | 2019-07-09 | Jiangsu Hengrui Medicine Co | derivado de 3,4-bipiridil pirazol, e método de preparação para o mesmo e aplicação médica do mesmo |
US11547712B2 (en) | 2017-11-20 | 2023-01-10 | Icahn School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
RU2750702C1 (ru) * | 2017-12-13 | 2021-07-01 | Джинфлит Терапьютикс (Шанхай) Инк. | КРИСТАЛЛИЧЕСКАЯ ФОРМА И СОЛЕВАЯ ФОРМА ИНГИБИТОРА TGF-βRI И СПОСОБ ИХ ПОЛУЧЕНИЯ |
US11788064B2 (en) | 2018-01-05 | 2023-10-17 | Icahn School Of Medicine At Mount Sinai | Method of increasing proliferation of pancreatic beta cells, treatment method, and composition |
CA3093340A1 (en) | 2018-03-20 | 2019-09-26 | Icahn School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
TW202012390A (zh) * | 2018-06-29 | 2020-04-01 | 日商日本歐愛特農業科技股份有限公司 | 新穎之經取代吡唑衍生物 |
US11034669B2 (en) | 2018-11-30 | 2021-06-15 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
TW202039459A (zh) | 2018-12-11 | 2020-11-01 | 美商施萬生物製藥研發 Ip有限責任公司 | Alk5 抑制劑 |
CN110467601B (zh) * | 2019-08-29 | 2021-07-02 | 杭州市西溪医院 | 一种吡唑联吡啶酮类化合物、中间体及其制备方法及应用 |
US11590116B2 (en) | 2019-11-22 | 2023-02-28 | Theravance Biopharma R&D Ip, Llc | Substituted pyridines and methods of use |
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US3492397A (en) | 1967-04-07 | 1970-01-27 | Warner Lambert Pharmaceutical | Sustained release dosage in the pellet form and process thereof |
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JP3734180B2 (ja) * | 1994-12-28 | 2006-01-11 | エーザイ株式会社 | 新規ピラゾール誘導体 |
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US6087381A (en) | 1997-05-22 | 2000-07-11 | G. D. Searle & Company | Pyrazole derivatives as p38 kinase inhibitors |
US5932576A (en) | 1997-05-22 | 1999-08-03 | G. D. Searle & Company | 3(5)-heteroaryl substituted pyrazoles as p38 kinase inhibitors |
JP2002541253A (ja) | 1999-04-09 | 2002-12-03 | スミスクライン・ビーチャム・コーポレイション | トリアリールイミダゾール |
AR029803A1 (es) | 2000-02-21 | 2003-07-16 | Smithkline Beecham Plc | Imidazoles sustituidos con piridilo y composiciones farmaceuticas que las comprenden |
GB0007405D0 (en) | 2000-03-27 | 2000-05-17 | Smithkline Beecham Corp | Compounds |
PE20020506A1 (es) | 2000-08-22 | 2002-07-09 | Glaxo Group Ltd | Derivados de pirazol fusionados como inhibidores de la proteina cinasa |
EP1349851A4 (en) | 2000-11-16 | 2004-09-08 | Smithkline Beecham Corp | COMPOUNDS |
GB0027987D0 (en) | 2000-11-16 | 2001-01-03 | Smithkline Beecham Plc | Compounds |
GB0100762D0 (en) | 2001-01-11 | 2001-02-21 | Smithkline Beecham Plc | Novel use |
ES2237671T3 (es) * | 2001-02-02 | 2005-08-01 | Smithkline Beecham Corporation | Derivados de pirazol contra la sobreexpresion de tgf. |
JP2004521901A (ja) * | 2001-02-02 | 2004-07-22 | グラクソ グループ リミテッド | Tgf阻害剤としてのピラゾール |
GB0102672D0 (en) * | 2001-02-02 | 2001-03-21 | Glaxo Group Ltd | Compounds |
AP2002002460A0 (en) | 2001-03-09 | 2002-06-30 | Pfizer Prod Inc | Novel benzimidazole anti-inflammatory compounds. |
ATE402164T1 (de) | 2001-04-26 | 2008-08-15 | Eisai R&D Man Co Ltd | Stickstoffhaltige verbindung mit kondensiertem ring und pyrazolylgruppe als substituent und medizinische zusammensetzung davon |
AR039241A1 (es) | 2002-04-04 | 2005-02-16 | Biogen Inc | Heteroarilos trisustituidos y metodos para su produccion y uso de los mismos |
AR040726A1 (es) | 2002-07-31 | 2005-04-20 | Smithkline Beecham Corp | Compuesto de 2- fenilpiridin-4-il-heterociclico, composicion farmaceutica que lo comprende y su uso para la fabricacion de un medicamento |
AP2005003264A0 (en) | 2002-09-18 | 2005-03-31 | Pfizer Prod Inc | Novel imidazole compounds as transforming growth factor (TGD) inhibitors. |
AP2005003261A0 (en) | 2002-09-18 | 2005-03-31 | Pfizer Prod Inc | Novel oxazole and thiazole compounds as transforming growth factor (TGF) inhibitors. |
PL375979A1 (en) | 2002-09-18 | 2005-12-12 | Pfizer Products Inc. | Pyrazole derivatives as transforming growth factor (tgf) inhibitors |
CA2497971A1 (en) | 2002-09-18 | 2004-04-01 | Pfizer Products Inc. | Triazole derivatives as transforming growth factor (tgf) inhibitors |
EA200500286A1 (ru) | 2002-09-18 | 2005-08-25 | Пфайзер Продактс Инк. | Новые изотиазольные и изоксазольные соединения в качестве ингибиторов трансформирующего фактора роста (тфр) |
PA8595001A1 (es) | 2003-03-04 | 2004-09-28 | Pfizer Prod Inc | Nuevos compuestos heteroaromaticos condensados que son inhibidores del factor de crecimiento transforante (tgf) |
-
2003
- 2003-09-08 PL PL03375979A patent/PL375979A1/xx not_active Application Discontinuation
- 2003-09-08 WO PCT/IB2003/003933 patent/WO2004026306A2/en active Application Filing
- 2003-09-08 CA CA2496295A patent/CA2496295C/en not_active Expired - Fee Related
- 2003-09-08 EA EA200500377A patent/EA200500377A1/ru unknown
- 2003-09-08 AT AT03797443T patent/ATE450258T1/de not_active IP Right Cessation
- 2003-09-08 BR BR0314302-3A patent/BR0314302A/pt not_active IP Right Cessation
- 2003-09-08 EP EP09177298A patent/EP2165708A3/en not_active Withdrawn
- 2003-09-08 DE DE60330362T patent/DE60330362D1/de not_active Expired - Lifetime
- 2003-09-08 CN CNA038222655A patent/CN1681501A/zh active Pending
- 2003-09-08 ES ES03797443T patent/ES2335099T3/es not_active Expired - Lifetime
- 2003-09-08 MX MXPA05002376A patent/MXPA05002376A/es active IP Right Grant
- 2003-09-08 KR KR1020057004598A patent/KR20050044807A/ko not_active Application Discontinuation
- 2003-09-08 OA OA1200500078A patent/OA12929A/en unknown
- 2003-09-08 AP AP2005003263A patent/AP2005003263A0/xx unknown
- 2003-09-08 EP EP03797443A patent/EP1542684B1/en not_active Expired - Lifetime
- 2003-09-08 JP JP2004568904A patent/JP4519657B2/ja not_active Expired - Fee Related
- 2003-09-08 AU AU2003259475A patent/AU2003259475A1/en not_active Abandoned
- 2003-09-15 PE PE2003000940A patent/PE20040988A1/es not_active Application Discontinuation
- 2003-09-16 AR ARP030103356A patent/AR041272A1/es unknown
- 2003-09-16 UY UY27985A patent/UY27985A1/es not_active Application Discontinuation
- 2003-09-17 PA PA20038583201A patent/PA8583201A1/es unknown
- 2003-09-17 US US10/667,189 patent/US6958354B2/en not_active Expired - Fee Related
-
2005
- 2005-02-16 NO NO20050838A patent/NO20050838L/no unknown
- 2005-02-17 IS IS7698A patent/IS7698A/is unknown
- 2005-03-16 CO CO05024529A patent/CO5550456A2/es not_active Application Discontinuation
- 2005-03-16 EC EC2005005679A patent/ECSP055679A/es unknown
- 2005-03-16 HR HR20050247A patent/HRP20050247A2/hr not_active Application Discontinuation
- 2005-03-18 MA MA28154A patent/MA27440A1/fr unknown
- 2005-09-23 US US11/234,564 patent/US7151110B2/en not_active Expired - Fee Related
-
2006
- 2006-11-08 US US11/557,638 patent/US7638537B2/en not_active Expired - Fee Related
-
2009
- 2009-11-12 US US12/617,027 patent/US20100056571A1/en not_active Abandoned
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