JP2013523746A - Ｄｇａｔ１阻害剤の使用 - Google Patents
Ｄｇａｔ１阻害剤の使用 Download PDFInfo
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- JP2013523746A JP2013523746A JP2013502706A JP2013502706A JP2013523746A JP 2013523746 A JP2013523746 A JP 2013523746A JP 2013502706 A JP2013502706 A JP 2013502706A JP 2013502706 A JP2013502706 A JP 2013502706A JP 2013523746 A JP2013523746 A JP 2013523746A
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- JP
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- Prior art keywords
- group
- phenyl
- dgat1 inhibitor
- pharmaceutically acceptable
- acceptable salt
- Prior art date
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 37
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- 201000010099 disease Diseases 0.000 claims abstract description 32
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- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 19
- -1 N-methylpiperidinyl group Chemical group 0.000 claims description 52
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- 125000000217 alkyl group Chemical group 0.000 claims description 43
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- 125000000623 heterocyclic group Chemical group 0.000 claims description 29
- 125000003118 aryl group Chemical group 0.000 claims description 27
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- TUBPDBIOKLNJTG-UHFFFAOYSA-N 3-[4-[6-(5-methoxy-1,3,4-oxadiazol-2-yl)-1h-indol-2-yl]-3,5-dimethylphenyl]propanoic acid Chemical compound O1C(OC)=NN=C1C1=CC=C(C=C(N2)C=3C(=CC(CCC(O)=O)=CC=3C)C)C2=C1 TUBPDBIOKLNJTG-UHFFFAOYSA-N 0.000 claims description 2
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- 238000005199 ultracentrifugation Methods 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 210000003462 vein Anatomy 0.000 description 1
- 235000019195 vitamin supplement Nutrition 0.000 description 1
- 125000001834 xanthenyl group Chemical group C1=CC=CC=2OC3=CC=CC=C3C(C12)* 0.000 description 1
- OENHQHLEOONYIE-JLTXGRSLSA-N β-Carotene Chemical compound CC=1CCCC(C)(C)C=1\C=C\C(\C)=C\C=C\C(\C)=C\C=C\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C OENHQHLEOONYIE-JLTXGRSLSA-N 0.000 description 1
Classifications
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
-
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- 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
- A61P3/06—Antihyperlipidemics
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Ophthalmology & Optometry (AREA)
- Hospice & Palliative Care (AREA)
- Child & Adolescent Psychology (AREA)
- Psychiatry (AREA)
- Dermatology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31881410P | 2010-03-30 | 2010-03-30 | |
| US61/318,814 | 2010-03-30 | ||
| PCT/US2011/030234 WO2011123401A1 (en) | 2010-03-30 | 2011-03-29 | Uses of dgat1 inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016114803A Division JP6251321B2 (ja) | 2010-03-30 | 2016-06-08 | Ｄｇａｔ１阻害剤の使用 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013523746A true JP2013523746A (ja) | 2013-06-17 |
| JP2013523746A5 JP2013523746A5 (OSRAM) | 2014-05-15 |
Family
ID=44170024
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013502706A Withdrawn JP2013523746A (ja) | 2010-03-30 | 2011-03-29 | Ｄｇａｔ１阻害剤の使用 |
| JP2016114803A Active JP6251321B2 (ja) | 2010-03-30 | 2016-06-08 | Ｄｇａｔ１阻害剤の使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016114803A Active JP6251321B2 (ja) | 2010-03-30 | 2016-06-08 | Ｄｇａｔ１阻害剤の使用 |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US9061012B2 (OSRAM) |
| EP (1) | EP2552441B1 (OSRAM) |
| JP (2) | JP2013523746A (OSRAM) |
| KR (1) | KR20130073884A (OSRAM) |
| CN (1) | CN102834099B (OSRAM) |
| AU (1) | AU2011235301B2 (OSRAM) |
| BR (1) | BR112012024618A2 (OSRAM) |
| CA (1) | CA2792269A1 (OSRAM) |
| CL (1) | CL2012002716A1 (OSRAM) |
| ES (1) | ES2586127T3 (OSRAM) |
| MA (1) | MA34097B1 (OSRAM) |
| MX (1) | MX2012011333A (OSRAM) |
| NZ (1) | NZ602125A (OSRAM) |
| PH (1) | PH12012501859A1 (OSRAM) |
| RU (1) | RU2012145950A (OSRAM) |
| SG (1) | SG183529A1 (OSRAM) |
| TN (1) | TN2012000458A1 (OSRAM) |
| TW (1) | TW201136916A (OSRAM) |
| WO (1) | WO2011123401A1 (OSRAM) |
| ZA (1) | ZA201206456B (OSRAM) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2021001143A (ja) * | 2019-06-21 | 2021-01-07 | 小林製薬株式会社 | 乳び血漿改善剤 |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR083417A1 (es) | 2010-10-14 | 2013-02-21 | Novartis Ag | Composiciones farmaceuticas que contienen un dgat1 inhibidor |
| CN104254519B (zh) * | 2012-04-25 | 2016-04-20 | 韩国化学研究院 | 贝塔丙氨酸衍生物、药学上允许的盐及包含其作为有效成分的药物组合物 |
| WO2013169648A1 (en) | 2012-05-07 | 2013-11-14 | Novartis Ag | Pharmaceutical combinations comprising a dgat1 inhibtor and a triglyceride lowering drug |
| ES2680599T3 (es) | 2013-02-14 | 2018-09-10 | Ionis Pharmaceuticals, Inc. | Modulación de la expresión de apolipoproteína C-III (ApoCIII) en poblaciones deficientes en lipoproteína lipasa (LPLD) |
| HUE041733T2 (hu) | 2014-03-20 | 2019-05-28 | Cymabay Therapeutics Inc | Intrahepatikus kolesztázisos betegségek kezelése |
| US10272058B2 (en) | 2014-03-20 | 2019-04-30 | Cymabay Therapeutics, Inc. | Treatment of intrahepatic cholestatic diseases |
| CN106470675A (zh) * | 2014-06-26 | 2017-03-01 | 西玛贝医药公司 | 严重高甘油三酯血症的治疗 |
| WO2016181409A1 (en) | 2015-05-11 | 2016-11-17 | Cadila Healthcare Limited | Saroglitazar magnesium for the treatment of chylomicronemia syndrome - |
| WO2017064635A2 (en) | 2015-10-14 | 2017-04-20 | Cadila Healthcare Limited | Pyrrole compound, compositions and process for preparation thereof |
| KR102708681B1 (ko) | 2018-02-13 | 2024-09-26 | 길리애드 사이언시즈, 인코포레이티드 | Pd-1/pd-l1 억제제 |
| JP7527984B2 (ja) * | 2018-03-16 | 2024-08-05 | アンジ ファーマシューティカルズ インコーポレーテッド | 重度の便秘を治療するための組成物及び方法 |
| EP3781556B1 (en) | 2018-04-19 | 2025-06-18 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| CN118221646A (zh) | 2018-07-13 | 2024-06-21 | 吉利德科学公司 | Pd-1/pd-l1抑制剂 |
| KR102635333B1 (ko) | 2018-10-24 | 2024-02-15 | 길리애드 사이언시즈, 인코포레이티드 | Pd-1/pd-l1 억제제 |
| WO2020113041A1 (en) * | 2018-11-30 | 2020-06-04 | Hdl Therapeutics, Inc | Methods for treating lipid-related diseases including xanthomas, carotid artery stenoses, and cerebral atherosclerosis |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2006166742A (ja) * | 2004-12-14 | 2006-06-29 | Japan Health Science Foundation | 高トリグリセリド血症の成因となる２種類のリポタンパクリパーゼ（ｌｐｌ）遺伝子変異及びそれを利用した高トリグリセリド血症を診断するためのｌｐｌ変異検出キット |
| WO2009040410A1 (en) * | 2007-09-28 | 2009-04-02 | Novartis Ag | Oxadiazole- and oxazole-substituted benzimidazole- and indole-derivatives as dgat1 inhibitors |
| JP2009514780A (ja) * | 2003-07-10 | 2009-04-09 | “エス．ウー．カー．”ベタイリグングス・ゲーエムベーハー | メタボリックシンドロームの処置のためのホエーパーミエートの使用 |
| JP2009532355A (ja) * | 2006-03-31 | 2009-09-10 | ノバルティス アクチエンゲゼルシャフト | 新規化合物 |
| WO2009119534A1 (ja) * | 2008-03-26 | 2009-10-01 | 第一三共株式会社 | 新規テトラヒドロイソキノリン誘導体 |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1997045439A1 (en) | 1996-05-30 | 1997-12-04 | The Trustees Of Columbia University In The City Of New York | Dna encoding acylcoenzyme a: cholesterol acyltransferase and uses thereof |
| US20030154504A1 (en) | 1998-06-24 | 2003-08-14 | Farese Robert V. | Methods and compositions for modulating carbohydrate metabolism |
| US20030167483A1 (en) | 1998-06-24 | 2003-09-04 | Farese Robert V. | Diacylglycerol O-acyltransferase |
| DE69939426D1 (de) | 1998-06-24 | 2008-10-09 | David Gladstone Inst | Diacylglycerin o-acyltransferase |
| US6344548B1 (en) | 1998-06-24 | 2002-02-05 | The Regents Of The University Of California | Diacylglycerol o-acyltransferase |
| US6100077A (en) | 1998-10-01 | 2000-08-08 | The Trustees Of Columbia University In The City Of New York | Isolation of a gene encoding diacylglycerol acyltransferase |
| US6444427B1 (en) | 2000-07-11 | 2002-09-03 | The Regents Of The University Of California | Polymorphisms in a diacylglycerol acyltransferase gene, and methods of use thereof |
| JP4164645B2 (ja) | 2002-08-09 | 2008-10-15 | 株式会社大塚製薬工場 | Ｄｇａｔ阻害剤 |
| CN1753897A (zh) | 2002-11-22 | 2006-03-29 | 日本烟草产业株式会社 | 稠合双环含氮杂环 |
| US20040185559A1 (en) | 2003-03-21 | 2004-09-23 | Isis Pharmaceuticals Inc. | Modulation of diacylglycerol acyltransferase 1 expression |
| AR044152A1 (es) | 2003-05-09 | 2005-08-24 | Bayer Corp | Derivados de alquilarilo, metodo de preparacion y uso para el tratamiento de la obesidad |
| US7300932B2 (en) | 2003-08-07 | 2007-11-27 | Japan Tobacco Inc. | Pyrrolo[1,2-b]pyridazine derivatives |
| GB0325192D0 (en) | 2003-10-29 | 2003-12-03 | Astrazeneca Ab | Method of use |
| JP2005206492A (ja) | 2004-01-21 | 2005-08-04 | Sankyo Co Ltd | スルホンアミド化合物 |
| AU2005209115A1 (en) | 2004-01-30 | 2005-08-11 | Japan Tobacco Inc. | Anorectic compounds |
| JP2006045209A (ja) | 2004-07-02 | 2006-02-16 | Sankyo Co Ltd | ウレア誘導体 |
| CA2572874A1 (en) | 2004-07-02 | 2006-01-12 | Sankyo Company Limited | Urea derivative |
| WO2006019020A1 (ja) | 2004-08-16 | 2006-02-23 | Sankyo Company, Limited | 置換されたウレア化合物 |
| ES2357015T3 (es) | 2004-10-15 | 2011-04-15 | Bayer Healthcare Llc | Preparación y uso de derivados bifenil-4-ilcarbonilaminoácido para el tratamiento de la obesidad. |
| NZ555683A (en) | 2004-12-14 | 2010-09-30 | Astrazeneca Ab | Oxadiazole derivatives as dgat inhibitors |
-
2011
- 2011-03-29 WO PCT/US2011/030234 patent/WO2011123401A1/en not_active Ceased
- 2011-03-29 ES ES11715329.6T patent/ES2586127T3/es active Active
- 2011-03-29 MX MX2012011333A patent/MX2012011333A/es active IP Right Grant
- 2011-03-29 SG SG2012063848A patent/SG183529A1/en unknown
- 2011-03-29 US US13/637,372 patent/US9061012B2/en active Active
- 2011-03-29 KR KR1020127028214A patent/KR20130073884A/ko not_active Withdrawn
- 2011-03-29 CA CA2792269A patent/CA2792269A1/en not_active Abandoned
- 2011-03-29 PH PH1/2012/501859A patent/PH12012501859A1/en unknown
- 2011-03-29 RU RU2012145950/15A patent/RU2012145950A/ru not_active Application Discontinuation
- 2011-03-29 CN CN201180016229.9A patent/CN102834099B/zh not_active Expired - Fee Related
- 2011-03-29 AU AU2011235301A patent/AU2011235301B2/en not_active Ceased
- 2011-03-29 EP EP11715329.6A patent/EP2552441B1/en active Active
- 2011-03-29 MA MA35264A patent/MA34097B1/fr unknown
- 2011-03-29 JP JP2013502706A patent/JP2013523746A/ja not_active Withdrawn
- 2011-03-29 BR BR112012024618A patent/BR112012024618A2/pt not_active IP Right Cessation
- 2011-03-29 TW TW100110831A patent/TW201136916A/zh unknown
- 2011-03-29 NZ NZ602125A patent/NZ602125A/en not_active IP Right Cessation
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2012
- 2012-08-28 ZA ZA2012/06456A patent/ZA201206456B/en unknown
- 2012-09-24 TN TNP2012000458A patent/TN2012000458A1/en unknown
- 2012-09-28 CL CL2012002716A patent/CL2012002716A1/es unknown
-
2016
- 2016-06-08 JP JP2016114803A patent/JP6251321B2/ja active Active
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2009514780A (ja) * | 2003-07-10 | 2009-04-09 | “エス．ウー．カー．”ベタイリグングス・ゲーエムベーハー | メタボリックシンドロームの処置のためのホエーパーミエートの使用 |
| JP2006166742A (ja) * | 2004-12-14 | 2006-06-29 | Japan Health Science Foundation | 高トリグリセリド血症の成因となる２種類のリポタンパクリパーゼ（ｌｐｌ）遺伝子変異及びそれを利用した高トリグリセリド血症を診断するためのｌｐｌ変異検出キット |
| JP2009532355A (ja) * | 2006-03-31 | 2009-09-10 | ノバルティス アクチエンゲゼルシャフト | 新規化合物 |
| WO2009040410A1 (en) * | 2007-09-28 | 2009-04-02 | Novartis Ag | Oxadiazole- and oxazole-substituted benzimidazole- and indole-derivatives as dgat1 inhibitors |
| WO2009119534A1 (ja) * | 2008-03-26 | 2009-10-01 | 第一三共株式会社 | 新規テトラヒドロイソキノリン誘導体 |
Non-Patent Citations (1)
| Title |
|---|
| JPN5013006252; ＺＨＡＯ: 'ＶＡＬＩＤＡＴＩＯＮ ＯＦ ＤＩＡＣＹＬ ＧＬＹＣＥＲＯＬＡＣＹＬＴＲＡＮＳＦＥＲＡＳＥ Ｉ ＡＳ Ａ ＮＯＶＥＬ ＴＡＲＧＥＴ ＦＯＲ ＴＨＥ ＴＲＥＡＴＭＥＮＴ 以下備考' ＪＯＵＲＮＡＬ ＭＥＤＩＣＡＬ ＣＨＥＭＩＳＴＲＹ Ｖ５１, 20080110, Ｐ３８０-３８３ * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2021001143A (ja) * | 2019-06-21 | 2021-01-07 | 小林製薬株式会社 | 乳び血漿改善剤 |
Also Published As
| Publication number | Publication date |
|---|---|
| ES2586127T3 (es) | 2016-10-11 |
| US20130023495A1 (en) | 2013-01-24 |
| JP6251321B2 (ja) | 2017-12-20 |
| WO2011123401A1 (en) | 2011-10-06 |
| NZ602125A (en) | 2014-01-31 |
| PH12012501859A1 (en) | 2013-01-07 |
| AU2011235301B2 (en) | 2013-07-18 |
| US9061012B2 (en) | 2015-06-23 |
| CN102834099B (zh) | 2015-05-27 |
| TW201136916A (en) | 2011-11-01 |
| JP2016216466A (ja) | 2016-12-22 |
| CN102834099A (zh) | 2012-12-19 |
| MX2012011333A (es) | 2012-11-16 |
| KR20130073884A (ko) | 2013-07-03 |
| SG183529A1 (en) | 2012-10-30 |
| TN2012000458A1 (en) | 2014-01-30 |
| CA2792269A1 (en) | 2011-10-06 |
| MA34097B1 (fr) | 2013-03-05 |
| EP2552441B1 (en) | 2016-05-04 |
| CL2012002716A1 (es) | 2013-01-25 |
| RU2012145950A (ru) | 2014-05-10 |
| BR112012024618A2 (pt) | 2019-09-24 |
| AU2011235301A1 (en) | 2012-10-11 |
| EP2552441A1 (en) | 2013-02-06 |
| ZA201206456B (en) | 2013-05-29 |
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