CA2773854A1 - Pharmaceutically useful heterocycle-substituted lactams - Google Patents
Pharmaceutically useful heterocycle-substituted lactams Download PDFInfo
- Publication number
- CA2773854A1 CA2773854A1 CA2773854A CA2773854A CA2773854A1 CA 2773854 A1 CA2773854 A1 CA 2773854A1 CA 2773854 A CA2773854 A CA 2773854A CA 2773854 A CA2773854 A CA 2773854A CA 2773854 A1 CA2773854 A1 CA 2773854A1
- Authority
- CA
- Canada
- Prior art keywords
- optionally substituted
- compound
- pyrazolo
- alkyl
- lcms
- 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.)
- Abandoned
Links
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- GBABOYUKABKIAF-IWWDSPBFSA-N vinorelbinetartrate Chemical compound C1N(CC=2C3=CC=CC=C3NC=22)CC(CC)=C[C@H]1C[C@]2(C(=O)OC)C1=CC(C23[C@H]([C@@]([C@H](OC(C)=O)[C@]4(CC)C=CCN([C@H]34)CC2)(O)C(=O)OC)N2C)=C2C=C1OC GBABOYUKABKIAF-IWWDSPBFSA-N 0.000 description 1
- 230000009385 viral infection Effects 0.000 description 1
- 230000003612 virological effect Effects 0.000 description 1
- 229950004393 visilizumab Drugs 0.000 description 1
- 229950001212 volociximab Drugs 0.000 description 1
- 229950003511 votumumab Drugs 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 239000003643 water by type Substances 0.000 description 1
- 238000009736 wetting Methods 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
- QDLHCMPXEPAAMD-QAIWCSMKSA-N wortmannin Chemical compound C1([C@]2(C)C3=C(C4=O)OC=C3C(=O)O[C@@H]2COC)=C4[C@@H]2CCC(=O)[C@@]2(C)C[C@H]1OC(C)=O QDLHCMPXEPAAMD-QAIWCSMKSA-N 0.000 description 1
- QDLHCMPXEPAAMD-UHFFFAOYSA-N wortmannin Natural products COCC1OC(=O)C2=COC(C3=O)=C2C1(C)C1=C3C2CCC(=O)C2(C)CC1OC(C)=O QDLHCMPXEPAAMD-UHFFFAOYSA-N 0.000 description 1
- 229950008250 zalutumumab Drugs 0.000 description 1
- XRASPMIURGNCCH-UHFFFAOYSA-N zoledronic acid Chemical compound OP(=O)(O)C(P(O)(O)=O)(O)CN1C=CN=C1 XRASPMIURGNCCH-UHFFFAOYSA-N 0.000 description 1
- 229960004276 zoledronic acid Drugs 0.000 description 1
- 229950001346 zolimomab aritox Drugs 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed 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
- A61K31/435—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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- 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
-
- 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
- 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
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
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- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Rheumatology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Vascular Medicine (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24180609P | 2009-09-11 | 2009-09-11 | |
| US61/241,806 | 2009-09-11 | ||
| US37114710P | 2010-08-05 | 2010-08-05 | |
| US61/371,147 | 2010-08-05 | ||
| PCT/US2010/048441 WO2011031979A1 (en) | 2009-09-11 | 2010-09-10 | Pharmaceutically useful heterocycle-substituted lactams |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2773854A1 true CA2773854A1 (en) | 2011-03-17 |
Family
ID=43732815
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2773854A Abandoned CA2773854A1 (en) | 2009-09-11 | 2010-09-10 | Pharmaceutically useful heterocycle-substituted lactams |
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| Country | Link |
|---|---|
| US (1) | US20110071115A1 (enExample) |
| EP (1) | EP2475652A1 (enExample) |
| JP (1) | JP2013504594A (enExample) |
| KR (1) | KR20120104521A (enExample) |
| CN (1) | CN102625803A (enExample) |
| AU (1) | AU2010292116A1 (enExample) |
| BR (1) | BR112012005550A2 (enExample) |
| CA (1) | CA2773854A1 (enExample) |
| IL (1) | IL218521A0 (enExample) |
| IN (1) | IN2012DN03112A (enExample) |
| MX (1) | MX2012002994A (enExample) |
| SG (1) | SG179083A1 (enExample) |
| WO (1) | WO2011031979A1 (enExample) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| ATE554078T1 (de) | 2007-07-26 | 2012-05-15 | Vitae Pharmaceuticals Inc | Synthese von 11-beta-hydroxysteroid-dehydrogenase-1-hemmern |
| AR069207A1 (es) | 2007-11-07 | 2010-01-06 | Vitae Pharmaceuticals Inc | Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1 |
| EP2229368A1 (en) | 2007-12-11 | 2010-09-22 | Vitae Pharmaceuticals, Inc. | Cyclic urea inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| TW200934490A (en) | 2008-01-07 | 2009-08-16 | Vitae Pharmaceuticals Inc | Lactam inhibitors of 11 &abgr;-hydroxysteroid dehydrogenase 1 |
| EP2252601B1 (en) | 2008-01-24 | 2012-12-19 | Vitae Pharmaceuticals, Inc. | Cyclic carbazate and semicarbazide inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| JP5730021B2 (ja) | 2008-02-15 | 2015-06-03 | ヴァイティー ファーマシューティカルズ，インコーポレイテッド | １１β−ヒドロキシステロイドデヒドロゲナーゼ１の阻害剤としてのシクロアルキルラクタム誘導体 |
| WO2009134387A1 (en) | 2008-05-01 | 2009-11-05 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| NZ588954A (en) | 2008-05-01 | 2012-08-31 | Vitae Pharmaceuticals Inc | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| JP5390610B2 (ja) | 2008-07-25 | 2014-01-15 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | １１β−ヒドロキシステロイドデヒドロゲナーゼ１型の阻害剤の合成 |
| PL2324018T3 (pl) | 2008-07-25 | 2014-02-28 | Boehringer Ingelheim Int | Cykliczne inhibitory dehydrogenazy 11 beta-hydroksysteroidowej typu 1 |
| CA2729998A1 (en) | 2008-07-25 | 2010-01-28 | Boehringer Ingelheim International Gmbh | Inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| EP2393807B1 (en) | 2009-02-04 | 2013-08-14 | Boehringer Ingelheim International GmbH | Cyclic inhibitors of 11 -hydroxysteroid dehydrogenase 1 |
| UA109255C2 (ru) | 2009-04-30 | 2015-08-10 | Берінгер Інгельхайм Інтернешнл Гмбх | Циклические ингибиторы 11бета-гидроксистероиддегидрогеназы 1 |
| WO2011011123A1 (en) | 2009-06-11 | 2011-01-27 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 based on the 1,3 -oxazinan- 2 -one structure |
| WO2011056737A1 (en) | 2009-11-05 | 2011-05-12 | Boehringer Ingelheim International Gmbh | Novel chiral phosphorus ligands |
| EP2576570A1 (en) * | 2010-05-26 | 2013-04-10 | Boehringer Ingelheim International GmbH | 2-oxo-1,2-dihydropyridin-4-ylboronic acid derivatives |
| EP2582698B1 (en) | 2010-06-16 | 2016-09-14 | Vitae Pharmaceuticals, Inc. | Substituted 5-,6- and 7-membered heterocycles, medicaments containing such compounds, and their use |
| WO2011161128A1 (en) | 2010-06-25 | 2011-12-29 | Boehringer Ingelheim International Gmbh | Azaspirohexanones as inhibitors of 11-beta-hsd1 for the treatment of metabolic disorders |
| KR20130137628A (ko) | 2010-11-02 | 2013-12-17 | 베링거 인겔하임 인터내셔날 게엠베하 | 대사 장애를 치료하기 위한 약제학적 병용물 |
| WO2012112568A1 (en) * | 2011-02-14 | 2012-08-23 | The Broad Institute, Inc. | Small molecule inhibitors for treating parasitic infections |
| WO2012170827A2 (en) * | 2011-06-08 | 2012-12-13 | Cylene Pharmaceuticals, Inc. | Pyrazolopyrimidines and related heterocycles as ck2 inhibitors |
| TW201319063A (zh) * | 2011-10-04 | 2013-05-16 | Yakult Honsha Kk | 以四氫噻唑衍生物或其鹽為有效成分之醫藥品 |
| AU2013280644B2 (en) | 2012-06-26 | 2018-08-02 | Jeffrey A. BACHA | Methods for treating tyrosine-kinase-inhibitor-resistant malignancies in patients with genetic polymorphisms or AHI1 dysregulations or mutations employing dianhydrogalactitol, diacetyldianhydrogalactitol, dibromodulcitol, or analogs or derivatives thereof |
| TW201414737A (zh) * | 2012-07-13 | 2014-04-16 | 必治妥美雅史谷比公司 | 作爲激酶抑制劑之咪唑并三□甲腈 |
| JP6437452B2 (ja) | 2013-01-14 | 2018-12-12 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｐｉｍキナーゼ阻害剤として有用な二環式芳香族カルボキサミド化合物 |
| LT2945939T (lt) | 2013-01-15 | 2020-07-27 | Incyte Holdings Corporation | Triazolkarboksamidai ir piridinkarboksamido junginiai, naudotini kaip pim kinazės inhibitoriai |
| CN105121442B (zh) * | 2013-03-28 | 2017-05-17 | 山东轩竹医药科技有限公司 | PI3K和/或mTOR抑制剂的前药 |
| JP2016519684A (ja) | 2013-04-08 | 2016-07-07 | デニス エム ブラウン | 準最適に投与された薬物療法の有効性を改善するための及び／又は副作用を低減するための方法および組成物 |
| EP3036238A1 (en) | 2013-08-23 | 2016-06-29 | Incyte Corporation | Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors |
| US9822124B2 (en) | 2014-07-14 | 2017-11-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors |
| US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
| US9540347B2 (en) | 2015-05-29 | 2017-01-10 | Incyte Corporation | Pyridineamine compounds useful as Pim kinase inhibitors |
| AR105967A1 (es) | 2015-09-09 | 2017-11-29 | Incyte Corp | Sales de un inhibidor de pim quinasa |
| WO2017059251A1 (en) | 2015-10-02 | 2017-04-06 | Incyte Corporation | Heterocyclic compounds useful as pim kinase inhibitors |
| EP3658557B1 (en) | 2017-07-28 | 2024-06-05 | Takeda Pharmaceutical Company Limited | Tyk2 inhibitors and uses thereof |
| TW201924683A (zh) | 2017-12-08 | 2019-07-01 | 美商英塞特公司 | 用於治療骨髓增生性贅瘤的低劑量組合療法 |
| US11071727B2 (en) | 2018-01-26 | 2021-07-27 | Northwestern University | Therapeutic targeting of proteolytic cleavage of the mixed lineage leukemia gene product (MLL1) by taspase1 using kinase inhibitors |
| BR112021007283A2 (pt) * | 2018-10-19 | 2021-07-20 | Senhwa Biosciences, Inc. | método de tratamento de um câncer ou câncer refratário |
| EP3771711A1 (en) | 2019-07-29 | 2021-02-03 | Bayer Animal Health GmbH | Pyrazole derivatives for controlling arthropods |
| MX2022008627A (es) | 2020-01-13 | 2022-11-08 | Verge Analytics Inc | Pirazolo-pirimidinas sustituidas y usos de las mismas. |
| US20240043427A1 (en) | 2020-05-01 | 2024-02-08 | Gilead Sciences, Inc. | Cd73 compounds |
| WO2022261069A1 (en) * | 2021-06-08 | 2022-12-15 | Verge Analytics, Inc. | Methods and treatment of viral infection with substituted pyrazolo-pyrimidines |
| PE20241186A1 (es) * | 2021-10-29 | 2024-06-03 | Gilead Sciences Inc | Compuestos de cd73 |
| CN115160341B (zh) * | 2022-07-18 | 2023-07-18 | 中国医学科学院医学实验动物研究所 | 苯并噁嗪类化合物及其药物用途 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5998424A (en) * | 1997-06-19 | 1999-12-07 | Dupont Pharmaceuticals Company | Inhibitors of factor Xa with a neutral P1 specificity group |
| JP4881558B2 (ja) * | 2002-09-04 | 2012-02-22 | シェーリング コーポレイション | サイクリン依存性キナーゼインヒビターとしてのピラゾロピリミジン |
| CN1880317B (zh) * | 2002-09-04 | 2012-10-10 | 先灵公司 | 作为细胞周期蛋白依赖性激酶抑制剂的吡唑并嘧啶 |
| WO2006049952A1 (en) * | 2004-10-29 | 2006-05-11 | Eli Lilly And Company | Cycloalkyl lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 |
| BRPI0616985B1 (pt) * | 2005-10-06 | 2021-10-26 | Merck Sharp & Dohme Corp. | Composto de pirazolo[1,5-a]pirimidina, e, uso de um composto |
| EP1948663B1 (en) * | 2005-10-21 | 2011-09-14 | Exelixis, Inc. | Pyrazolo-pyrimidines as casein kinase ii (ck2) modulators |
| AU2007268083A1 (en) * | 2006-05-22 | 2007-12-06 | Schering Corporation | Pyrazolo [1, 5-A] pyrimidines as CDK inhibitors |
| US7531539B2 (en) * | 2006-08-09 | 2009-05-12 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| EP2526934B1 (en) * | 2006-09-22 | 2015-12-09 | Pharmacyclics LLC | Inhibitors of bruton's tyrosine kinase |
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2010
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- 2010-09-10 JP JP2012528930A patent/JP2013504594A/ja active Pending
- 2010-09-10 US US12/879,851 patent/US20110071115A1/en not_active Abandoned
- 2010-09-10 WO PCT/US2010/048441 patent/WO2011031979A1/en not_active Ceased
- 2010-09-10 EP EP10816161A patent/EP2475652A1/en not_active Withdrawn
- 2010-09-10 SG SG2012016929A patent/SG179083A1/en unknown
- 2010-09-10 BR BR112012005550A patent/BR112012005550A2/pt not_active IP Right Cessation
- 2010-09-10 AU AU2010292116A patent/AU2010292116A1/en not_active Abandoned
- 2010-09-10 MX MX2012002994A patent/MX2012002994A/es not_active Application Discontinuation
- 2010-09-10 IN IN3112DEN2012 patent/IN2012DN03112A/en unknown
- 2010-09-10 CA CA2773854A patent/CA2773854A1/en not_active Abandoned
- 2010-09-10 KR KR1020127009217A patent/KR20120104521A/ko not_active Withdrawn
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2012
- 2012-03-07 IL IL218521A patent/IL218521A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP2475652A1 (en) | 2012-07-18 |
| KR20120104521A (ko) | 2012-09-21 |
| IN2012DN03112A (enExample) | 2015-09-18 |
| SG179083A1 (en) | 2012-04-27 |
| JP2013504594A (ja) | 2013-02-07 |
| CN102625803A (zh) | 2012-08-01 |
| US20110071115A1 (en) | 2011-03-24 |
| MX2012002994A (es) | 2012-07-17 |
| WO2011031979A1 (en) | 2011-03-17 |
| IL218521A0 (en) | 2012-07-31 |
| BR112012005550A2 (pt) | 2015-09-08 |
| AU2010292116A1 (en) | 2012-05-03 |
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Legal Events
| Date | Code | Title | Description |
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| FZDE | Discontinued |
Effective date: 20130910 |