TW200944540A - C20-C21 substituted glucocorticoid receptor agonists - Google Patents
C20-C21 substituted glucocorticoid receptor agonists Download PDFInfo
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- TW200944540A TW200944540A TW097149406A TW97149406A TW200944540A TW 200944540 A TW200944540 A TW 200944540A TW 097149406 A TW097149406 A TW 097149406A TW 97149406 A TW97149406 A TW 97149406A TW 200944540 A TW200944540 A TW 200944540A
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- JMPVZWBJWHQJDD-UHFFFAOYSA-N sulfur tetrachloride Chemical compound ClS(Cl)(Cl)Cl JMPVZWBJWHQJDD-UHFFFAOYSA-N 0.000 description 1
- 150000003467 sulfuric acid derivatives Chemical class 0.000 description 1
- 229910021653 sulphate ion Inorganic materials 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 238000010189 synthetic method Methods 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 150000003899 tartaric acid esters Chemical class 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- FPGGTKZVZWFYPV-UHFFFAOYSA-M tetrabutylammonium fluoride Chemical compound [F-].CCCC[N+](CCCC)(CCCC)CCCC FPGGTKZVZWFYPV-UHFFFAOYSA-M 0.000 description 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 description 1
- 125000003507 tetrahydrothiofenyl group Chemical group 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 238000011287 therapeutic dose Methods 0.000 description 1
- 231100001274 therapeutic index Toxicity 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 150000007970 thio esters Chemical class 0.000 description 1
- 150000003567 thiocyanates Chemical class 0.000 description 1
- 229930192474 thiophene Natural products 0.000 description 1
- 210000001541 thymus gland Anatomy 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-M toluene-4-sulfonate Chemical compound CC1=CC=C(S([O-])(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-M 0.000 description 1
- LBLYYCQCTBFVLH-UHFFFAOYSA-M toluenesulfonate group Chemical group C=1(C(=CC=CC1)S(=O)(=O)[O-])C LBLYYCQCTBFVLH-UHFFFAOYSA-M 0.000 description 1
- 239000003053 toxin Substances 0.000 description 1
- 231100000765 toxin Toxicity 0.000 description 1
- 108700012359 toxins Proteins 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
- 238000013518 transcription Methods 0.000 description 1
- 230000035897 transcription Effects 0.000 description 1
- 230000009466 transformation Effects 0.000 description 1
- 230000007704 transition Effects 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
- ITMCEJHCFYSIIV-UHFFFAOYSA-M triflate Chemical compound [O-]S(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-M 0.000 description 1
- 239000012588 trypsin Substances 0.000 description 1
- 208000009999 tuberous sclerosis Diseases 0.000 description 1
- MWOOGOJBHIARFG-UHFFFAOYSA-N vanillin Chemical compound COC1=CC(C=O)=CC=C1O MWOOGOJBHIARFG-UHFFFAOYSA-N 0.000 description 1
- FGQOOHJZONJGDT-UHFFFAOYSA-N vanillin Natural products COC1=CC(O)=CC(C=O)=C1 FGQOOHJZONJGDT-UHFFFAOYSA-N 0.000 description 1
- 235000012141 vanillin Nutrition 0.000 description 1
- 230000002227 vasoactive effect Effects 0.000 description 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 201000010044 viral meningitis Diseases 0.000 description 1
- 230000000007 visual effect Effects 0.000 description 1
- 239000003039 volatile agent Substances 0.000 description 1
- 238000010792 warming Methods 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 239000002023 wood Substances 0.000 description 1
- 229910052727 yttrium Inorganic materials 0.000 description 1
- VWQVUPCCIRVNHF-UHFFFAOYSA-N yttrium atom Chemical compound [Y] VWQVUPCCIRVNHF-UHFFFAOYSA-N 0.000 description 1
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- 239000011701 zinc Substances 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
-
- 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
- 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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- 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
- A61P11/06—Antiasthmatics
-
- 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
- A61P11/10—Expectorants
-
- 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
- A61P17/04—Antipruritics
-
- 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
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
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- 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
-
- 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
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic 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
- A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
- A61P5/44—Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Ophthalmology & Optometry (AREA)
- Virology (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Transplantation (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Diabetes (AREA)
- Otolaryngology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US1613507P | 2007-12-21 | 2007-12-21 |
Publications (1)
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|---|---|
| TW200944540A true TW200944540A (en) | 2009-11-01 |
Family
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| Application Number | Title | Priority Date | Filing Date |
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| TW097149406A TW200944540A (en) | 2007-12-21 | 2008-12-18 | C20-C21 substituted glucocorticoid receptor agonists |
Country Status (11)
| Country | Link |
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| US (1) | US8524697B2 (enExample) |
| EP (1) | EP2245042A1 (enExample) |
| JP (1) | JP2011507878A (enExample) |
| CN (1) | CN101970452A (enExample) |
| AR (1) | AR069804A1 (enExample) |
| CA (1) | CA2710149A1 (enExample) |
| CL (1) | CL2008003803A1 (enExample) |
| MX (1) | MX2010007023A (enExample) |
| PE (1) | PE20091525A1 (enExample) |
| TW (1) | TW200944540A (enExample) |
| WO (1) | WO2009085879A2 (enExample) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009085880A2 (en) * | 2007-12-21 | 2009-07-09 | Schering Corporation | C-21 thioethers as glucocorticoid receptor agonists |
| RU2420270C2 (ru) * | 2009-07-20 | 2011-06-10 | Государственное образовательное учреждение высшего профессионального образования "Северо-Осетинская государственная медицинская академия" Федерального агентства по здравоохранению и социальному развитию | Способ лечения рецидивирующего обструктивного бронхита у детей |
| EP2475676B1 (en) * | 2009-09-11 | 2020-05-27 | Chiesi Farmaceutici S.p.A. | Pregnane derivatives condensed in the 16,17 position with an N-substituted isoxazolidine ring as anti-inflammatory agents |
| CN103087137A (zh) * | 2011-11-07 | 2013-05-08 | 天津金耀集团有限公司 | 一种21位为硫代烃基的糖皮质激素 |
| UA116622C2 (uk) * | 2011-11-11 | 2018-04-25 | Аллерган, Інк. | Похідні 4-прегенен-11ss-17-21-тріол-3,20-діону для лікування хвороб очей |
| EP3309166A3 (en) * | 2013-01-23 | 2018-08-22 | Sphaera Pharma Pvt. Ltd. | 11beta-hydroxy-steroids for use in mitochondria biogenesis and diseases associated with mitochondrial dysfunction or depletion |
| GB201320091D0 (en) * | 2013-11-14 | 2014-01-01 | Univ Manchester | Selective glucocorticoid receptor ligands |
| EP3795578A3 (en) | 2014-07-23 | 2021-05-26 | Sphaera Pharma Pvt. Ltd. | Hydroxysteroid compounds, their intermediates, process of preparation, composition and uses thereof |
| LT3464318T (lt) | 2016-06-02 | 2021-06-25 | Abbvie Inc. | Gliukokortikoidų receptorių agonistas ir jo imunokonjugatai |
| MX394528B (es) * | 2016-11-08 | 2025-03-24 | Regeneron Pharma | Esteroides y conjugados de proteinas de los mismos. |
| WO2018097149A1 (ja) * | 2016-11-24 | 2018-05-31 | 帝人ファーマ株式会社 | スルフィド化合物の製造方法 |
| KR20250008984A (ko) | 2017-05-18 | 2025-01-16 | 리제너론 파마슈티칼스 인코포레이티드 | 사이클로덱스트린 단백질 약물 접합체 |
| WO2019023148A1 (en) | 2017-07-24 | 2019-01-31 | Regeneron Pharmaceuticals, Inc. | ANTI-CD8 ANTIBODIES AND USES THEREOF |
| SG11202004151YA (en) | 2017-11-07 | 2020-06-29 | Regeneron Pharma | Hydrophilic linkers for antibody drug conjugates |
| PE20201286A1 (es) | 2017-12-01 | 2020-11-24 | Abbvie Inc | Agonista del receptor de glucocorticoides e inmunoconjugados de este |
| CA3081559A1 (en) * | 2017-12-01 | 2019-06-06 | Abbvie Inc. | Anti-cd40 antibody drug conjugates |
| CA3086926A1 (en) | 2018-01-08 | 2019-07-11 | Regeneron Pharmaceuticals, Inc. | Steroids and antibody-conjugates thereof |
| SG11202010909RA (en) | 2018-05-09 | 2020-12-30 | Regeneron Pharma | Anti-msr1 antibodies and methods of use thereof |
| CN112851743A (zh) * | 2019-11-27 | 2021-05-28 | 重庆华邦胜凯制药有限公司 | 一种氧化杂质的制备方法 |
| CN112876531A (zh) * | 2019-11-29 | 2021-06-01 | 重庆华邦胜凯制药有限公司 | 一种合成地奈德杂质的方法 |
| JP7706565B2 (ja) | 2021-03-23 | 2025-07-11 | イーライ リリー アンド カンパニー | グルココルチコイド受容体アゴニスト |
| AR125079A1 (es) | 2021-03-23 | 2023-06-07 | Lilly Co Eli | Agonistas de receptores de glucocorticoides sustituidos con carboxi |
| AR125084A1 (es) | 2021-03-23 | 2023-06-07 | Lilly Co Eli | Agonistas del receptor de glucocorticoides novedosos |
| CN114702543B (zh) * | 2022-04-19 | 2023-08-22 | 中国药科大学 | Clascoterone衍生物或其可药用的盐及其制备方法和用途 |
| CN115430392B (zh) * | 2022-08-31 | 2024-04-16 | 江苏诺盟化工有限公司 | 一种苯偶酰的制备方法及专用文丘里喷射器 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US1119082A (en) * | 1914-03-16 | 1914-12-01 | George A Inman | Protector-plate. |
| US3020275A (en) * | 1960-06-07 | 1962-02-06 | American Cyanamid Co | 21-nitrogen substituted steroids of the pregnane series and methods of preparing the same |
| GB1119082A (en) * | 1966-07-11 | 1968-07-10 | Lepetit Spa | New steroids |
| DE1300940B (de) * | 1966-10-13 | 1969-08-14 | Hoechst Ag | Verfahren zur Herstellung von Tetrahydropyranylaethern von Steroiden |
| US4188385A (en) * | 1978-04-05 | 1980-02-12 | Syntex (U.S.A.) Inc. | Thioetianic acid derivatives |
| US4861765A (en) * | 1985-06-26 | 1989-08-29 | Jouveinal | 21-alkyl-, cycloalkyl- or aryl-substituted thio steroids and pharmaceutical compositions containing them |
| ZA866097B (en) * | 1985-09-12 | 1988-03-30 | Upjohn Co | 20-and 21-amino steroids |
| JP2659279B2 (ja) * | 1993-05-17 | 1997-09-30 | アルコン ラボラトリーズ,インコーポレイテッド | 眼科用抗炎症化合物 |
| US5420120A (en) * | 1993-12-17 | 1995-05-30 | Alcon Laboratories, Inc. | Anti-inflammatory glucocorticoid compounds for topical ophthalmic use |
| AU7576001A (en) * | 2000-08-05 | 2002-02-18 | Glaxo Group Ltd | 6.alpha., 9.alpha.-difluoro-17.alpha.-`(2-furanylcarboxyl) oxy]-11.beta.-hydroxy-16.alpha.-methyl-3-oxo-androst-1,4,-diene-17-carbothioic acid s-fluoromethyl ester as an anti-inflammatory agent |
| AU1076802A (en) * | 2000-11-03 | 2002-05-15 | Matrix Therapeutics Ltd | Selective glucocorticoid receptor agonists |
| EP1893220A4 (en) * | 2005-06-14 | 2011-06-15 | Gilead Sciences Inc | SUBSTITUTED PHENYLPHOSPHATES AS MUTUAL PROMO PRODUCTS CONSISTING OF STEROIDS AND BETA-AGONISTS FOR THE TREATMENT OF PULMONARY INFLAMMATION AND BRONCHOCONSTRICTION |
| WO2009085880A2 (en) | 2007-12-21 | 2009-07-09 | Schering Corporation | C-21 thioethers as glucocorticoid receptor agonists |
| US8916136B2 (en) * | 2010-04-23 | 2014-12-23 | Indian Institute Of Technology Bombay | Glucose biosensor system coupled with an anti-inflammatory module and methods for using the same |
-
2008
- 2008-12-18 CN CN2008801273812A patent/CN101970452A/zh active Pending
- 2008-12-18 PE PE2008002140A patent/PE20091525A1/es not_active Application Discontinuation
- 2008-12-18 MX MX2010007023A patent/MX2010007023A/es not_active Application Discontinuation
- 2008-12-18 AR ARP080105525A patent/AR069804A1/es not_active Application Discontinuation
- 2008-12-18 WO PCT/US2008/087300 patent/WO2009085879A2/en not_active Ceased
- 2008-12-18 JP JP2010539762A patent/JP2011507878A/ja active Pending
- 2008-12-18 CL CL2008003803A patent/CL2008003803A1/es unknown
- 2008-12-18 CA CA2710149A patent/CA2710149A1/en not_active Abandoned
- 2008-12-18 TW TW097149406A patent/TW200944540A/zh unknown
- 2008-12-18 EP EP08868864A patent/EP2245042A1/en not_active Withdrawn
- 2008-12-18 US US12/736,063 patent/US8524697B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| WO2009085879A2 (en) | 2009-07-09 |
| MX2010007023A (es) | 2010-09-30 |
| AR069804A1 (es) | 2010-02-17 |
| US8524697B2 (en) | 2013-09-03 |
| EP2245042A1 (en) | 2010-11-03 |
| PE20091525A1 (es) | 2009-09-25 |
| CN101970452A (zh) | 2011-02-09 |
| CL2008003803A1 (es) | 2010-02-19 |
| JP2011507878A (ja) | 2011-03-10 |
| CA2710149A1 (en) | 2009-07-09 |
| US20110182828A1 (en) | 2011-07-28 |
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