CA2791417A1 - Heterocyclic inhibitors of histamine receptors for the treatment of disease - Google Patents
Heterocyclic inhibitors of histamine receptors for the treatment of disease Download PDFInfo
- Publication number
- CA2791417A1 CA2791417A1 CA2791417A CA2791417A CA2791417A1 CA 2791417 A1 CA2791417 A1 CA 2791417A1 CA 2791417 A CA2791417 A CA 2791417A CA 2791417 A CA2791417 A CA 2791417A CA 2791417 A1 CA2791417 A1 CA 2791417A1
- Authority
- CA
- Canada
- Prior art keywords
- chosen
- recited
- optionally substituted
- compound
- heterocycloalkyl
- 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
- 238000011282 treatment Methods 0.000 title claims abstract description 40
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title claims description 56
- 201000010099 disease Diseases 0.000 title claims description 33
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- 102000000543 Histamine Receptors Human genes 0.000 title description 15
- 108010002059 Histamine Receptors Proteins 0.000 title description 15
- 125000000623 heterocyclic group Chemical group 0.000 title description 13
- 150000001875 compounds Chemical class 0.000 claims abstract description 269
- 238000000034 method Methods 0.000 claims abstract description 40
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- 125000000753 cycloalkyl group Chemical group 0.000 claims description 79
- 125000003118 aryl group Chemical group 0.000 claims description 74
- 125000001072 heteroaryl group Chemical group 0.000 claims description 71
- 229910052739 hydrogen Inorganic materials 0.000 claims description 68
- 239000001257 hydrogen Substances 0.000 claims description 67
- 125000003545 alkoxy group Chemical group 0.000 claims description 56
- 150000002431 hydrogen Chemical class 0.000 claims description 53
- 125000001188 haloalkyl group Chemical group 0.000 claims description 50
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- 125000004103 aminoalkyl group Chemical group 0.000 claims description 46
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- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 44
- NTYJJOPFIAHURM-UHFFFAOYSA-N Histamine Chemical compound NCCC1=CN=CN1 NTYJJOPFIAHURM-UHFFFAOYSA-N 0.000 claims description 43
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 39
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- 229910052757 nitrogen Inorganic materials 0.000 claims description 39
- 125000002252 acyl group Chemical group 0.000 claims description 37
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 37
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- 229910052736 halogen Inorganic materials 0.000 claims description 37
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 36
- 150000002367 halogens Chemical class 0.000 claims description 36
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 36
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- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 claims description 35
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 34
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- 125000000304 alkynyl group Chemical group 0.000 claims description 32
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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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
- 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
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Transplantation (AREA)
- Otolaryngology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31261510P | 2010-03-10 | 2010-03-10 | |
| US61/312,615 | 2010-03-10 | ||
| PCT/US2011/027817 WO2011112766A2 (en) | 2010-03-10 | 2011-03-10 | Heterocyclic inhibitors of histamine receptors for the treatment of disease |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2791417A1 true CA2791417A1 (en) | 2011-09-15 |
Family
ID=44564108
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2791417A Abandoned CA2791417A1 (en) | 2010-03-10 | 2011-03-10 | Heterocyclic inhibitors of histamine receptors for the treatment of disease |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US8569300B2 (enExample) |
| EP (1) | EP2545058B1 (enExample) |
| JP (1) | JP5888654B2 (enExample) |
| KR (1) | KR20130016253A (enExample) |
| CN (1) | CN102869666B (enExample) |
| AR (1) | AR080496A1 (enExample) |
| AU (1) | AU2011224316B2 (enExample) |
| BR (1) | BR112012022211A2 (enExample) |
| CA (1) | CA2791417A1 (enExample) |
| ES (1) | ES2607125T3 (enExample) |
| IL (1) | IL221829A (enExample) |
| MX (1) | MX2012010404A (enExample) |
| NZ (1) | NZ602041A (enExample) |
| PH (1) | PH12012501783A1 (enExample) |
| RU (1) | RU2012137180A (enExample) |
| TW (1) | TW201200518A (enExample) |
| UY (1) | UY33271A (enExample) |
| WO (1) | WO2011112766A2 (enExample) |
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| WO2013039785A2 (en) * | 2011-09-12 | 2013-03-21 | Kalypsys, Inc. | Heterocyclic inhibitors of histamine receptors for the treatment of disease |
| US9266891B2 (en) | 2012-11-16 | 2016-02-23 | Boehringer Ingelheim International Gmbh | Substituted [1,2,4]triazolo[4,3-A]pyrazines that are BRD4 inhibitors |
| CN105164134B (zh) | 2013-05-02 | 2017-09-22 | 辉瑞大药厂 | 作为pde10抑制剂的咪唑并‑三嗪衍生物 |
| LT3057586T (lt) | 2013-10-18 | 2020-03-10 | Celgene Quanticel Research, Inc. | Bromodomeno inhibitoriai |
| ES2750956T3 (es) | 2014-02-13 | 2020-03-30 | Incyte Corp | Ciclopropilaminas como inhibidores de LSD1 |
| US9527835B2 (en) | 2014-02-13 | 2016-12-27 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| JP6602778B2 (ja) | 2014-02-13 | 2019-11-06 | インサイト・コーポレイション | Ｌｓｄ１阻害剤としてのシクロプロピルアミン類 |
| TW201613860A (en) | 2014-02-13 | 2016-04-16 | Incyte Corp | Cyclopropylamines as LSD1 inhibitors |
| US9695167B2 (en) | 2014-07-10 | 2017-07-04 | Incyte Corporation | Substituted triazolo[1,5-a]pyridines and triazolo[1,5-a]pyrazines as LSD1 inhibitors |
| US9695168B2 (en) | 2014-07-10 | 2017-07-04 | Incyte Corporation | Substituted imidazo[1,5-α]pyridines and imidazo[1,5-α]pyrazines as LSD1 inhibitors |
| WO2016007736A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Imidazopyrazines as lsd1 inhibitors |
| WO2016007727A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| TW201625635A (zh) | 2014-11-21 | 2016-07-16 | 默沙東藥廠 | 作為可溶性鳥苷酸環化酶活化劑之三唑并吡基衍生物 |
| UY36462A (es) | 2014-12-23 | 2016-07-29 | Novartis Ag | Compuestos de triazolopirimidina y usos de los mismos |
| EA201792205A1 (ru) | 2015-04-03 | 2018-02-28 | Инсайт Корпорейшн | Гетероциклические соединения как ингибиторы lsd1 |
| BR112018002553A8 (pt) | 2015-08-12 | 2023-01-24 | Incyte Corp | Sais de um inibidor de lsd1 |
| PE20190377A1 (es) | 2016-04-22 | 2019-03-08 | Incyte Corp | Formulaciones de un inhibidor de lsd 1 |
| CN109790166A (zh) | 2016-06-20 | 2019-05-21 | 诺华股份有限公司 | 咪唑并吡啶化合物用于治疗癌症 |
| EP3472161B1 (en) | 2016-06-20 | 2020-03-25 | Novartis AG | Triazolopyridine compounds and uses thereof |
| KR102519922B1 (ko) | 2016-06-20 | 2023-04-11 | 노파르티스 아게 | 트리아졸로피리미딘 화합물의 결정질 형태 |
| TW201837036A (zh) | 2017-01-10 | 2018-10-16 | 德商拜耳廠股份有限公司 | 作為除害劑之雜環衍生物（一） |
| WO2018130443A1 (de) | 2017-01-10 | 2018-07-19 | Bayer Aktiengesellschaft | Heterocyclen-derivate als schädlingsbekämpfungsmittel |
| IL296456A (en) | 2017-01-23 | 2022-11-01 | Revolution Medicines Inc | Bicyclics as allosteric shp2 inhibitors |
| KR20200036004A (ko) | 2017-08-01 | 2020-04-06 | 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 | Jak 키나아제 억제제로서 피라졸로 및 트리아졸로 비시클릭 화합물 |
| SG11202002941WA (en) * | 2017-10-12 | 2020-04-29 | Revolution Medicines Inc | Pyridine, pyrazine, and triazine compounds as allosteric shp2 inhibitors |
| RU2020123241A (ru) * | 2017-12-15 | 2022-01-17 | Революшн Медсинз, Инк. | Полициклические соединения в качестве аллостерических ингибиторов shp2 |
| KR102614939B1 (ko) * | 2018-02-13 | 2023-12-19 | 블루레이 테라퓨틱스 (상하이) 컴퍼니 리미티드 | 피리미딘-융합고리 화합물 및 그의 제조방법과 용도 |
| CN110655520A (zh) * | 2018-06-29 | 2020-01-07 | 上海青煜医药科技有限公司 | 嘧啶并环化合物及其制备方法和应用 |
| CN115448923B (zh) * | 2018-02-13 | 2024-03-22 | 上海青煜医药科技有限公司 | 嘧啶并环化合物及其制备方法和应用 |
| KR20200139153A (ko) | 2018-02-27 | 2020-12-11 | 인사이트 코포레이션 | A2a / a2b 억제제로서의 이미다조피리미딘 및 트리아졸로피리미딘 |
| CA3100731A1 (en) | 2018-05-18 | 2019-11-21 | Incyte Corporation | Fused pyrimidine derivatives as a2a / a2b inhibitors |
| CA3105721A1 (en) | 2018-07-05 | 2020-01-09 | Incyte Corporation | Fused pyrazine derivatives as a2a / a2b inhibitors |
| WO2020047198A1 (en) | 2018-08-31 | 2020-03-05 | Incyte Corporation | Salts of an lsd1 inhibitor and processes for preparing the same |
| WO2020068729A1 (en) | 2018-09-25 | 2020-04-02 | Incyte Corporation | Pyrazolo[4,3-d]pyrimidine compounds as alk2 abd/or fgfr modulators |
| EP3878853A4 (en) * | 2018-11-07 | 2022-12-14 | Shanghai Ringene BioPharma Co., Ltd. | NITROGEN-CONTAINING FUSED HETEROCYCLIC SHP2 INHIBITOR COMPOUND, METHOD OF PREPARATION AND USE |
| AU2019386036A1 (en) * | 2018-11-30 | 2021-05-27 | Tuojie Biotech (Shanghai) Co., Ltd. | Pyrimidine and five-membered nitrogen heterocycle derivative, preparation method therefor, and medical uses thereof |
| CN113498352A (zh) | 2019-01-23 | 2021-10-12 | 施万生物制药研发Ip有限责任公司 | 作为jak抑制剂的咪唑并[1,5-a]吡啶、1,2,4-三唑并[4,3-a]吡啶和咪唑并[1,5-a]吡嗪 |
| TWI829857B (zh) | 2019-01-29 | 2024-01-21 | 美商英塞特公司 | 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶 |
| EP4019521A4 (en) * | 2019-08-22 | 2023-05-03 | Blueray Therapeutics (Shanghai) Co., Ltd | AZAHETEROARYL COMPOUND AND USE |
| US12065444B2 (en) | 2021-11-19 | 2024-08-20 | Crossignal Therapeutics, Inc. | Substituted tetrazolo[1,5-a]pyrazines and tetrazolo[1,5-c]pyrimidines as adenosine receptor antagonists |
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| US3929812A (en) * | 1974-05-20 | 1975-12-30 | Squibb & Sons Inc | Derivatives of 1H-triazolo {8 4,5-c{9 pyridine-7-carboxylic acids and esters |
| DE4337611A1 (de) * | 1993-11-04 | 1995-05-11 | Boehringer Ingelheim Kg | Neue Benzoylguanidine, ihre Herstellung und ihre Verwendung in Arzneimitteln |
| JPWO2003028732A1 (ja) * | 2001-09-28 | 2005-01-13 | 協和醗酵工業株式会社 | 受容体拮抗剤 |
| US6921762B2 (en) * | 2001-11-16 | 2005-07-26 | Amgen Inc. | Substituted indolizine-like compounds and methods of use |
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| EP1545532A2 (en) | 2002-09-06 | 2005-06-29 | Janssen Pharmaceutica N.V. | Heterocyclic compounds |
| ES2317244T3 (es) * | 2004-06-09 | 2009-04-16 | Glaxo Group Limited | Derivados de pirrolopiridina. |
| EP1970373A1 (en) * | 2005-12-02 | 2008-09-17 | Mitsubishi Tanabe Pharma Corporation | Alicyclic heterocyclic compound |
| US7807671B2 (en) * | 2006-04-25 | 2010-10-05 | Bristol-Myers Squibb Company | Diketo-piperazine and piperidine derivatives as antiviral agents |
| DE602007006010D1 (de) * | 2006-05-31 | 2010-06-02 | Galapagos Nv | Triazolopyrazinverbindungen zur behandlung von degenerations- und entzündungskrankheiten |
| EP2044027A2 (en) * | 2006-07-03 | 2009-04-08 | Vereniging voor christelijk hoger onderwijs, wetenschappelijk onderzoek en patiëntenzorg | Fused bicyclic compounds interacting with the histamine h4 receptor |
| WO2008031556A2 (en) | 2006-09-12 | 2008-03-20 | Ucb Pharma, S.A. | 2 amino-pyrimidine derivatives as h4 receptor antagonists, processes for preparing them and their use in pharmaceutical compositions |
| EP2252619B1 (en) * | 2008-01-11 | 2013-10-09 | Fibrogen, Inc. | Isothiazole-pyridine derivatives as modulators of hif (hypoxia inducible factor) activity |
| KR101589960B1 (ko) * | 2008-02-08 | 2016-01-29 | 바실리어 파마슈티카 아게 | Ｐｄｅ 억제를 통해 중재되는 질환의 치료를 위한 마크로라이드 |
| UY32110A (es) * | 2008-09-10 | 2010-04-30 | Alcon Res Ltd | Inhibidores de aminopirimidina de los receptores de histamina para el tratamiento de una enfermedad |
| CA2735369A1 (en) * | 2008-09-10 | 2010-03-18 | Kalypsys Inc. | Heterocyclic inhibitors of histamine receptors for the treatment of disease |
| ES2475091T3 (es) * | 2009-04-16 | 2014-07-10 | Centro Nacional De Investigaciones Oncol�Gicas (Cnio) | Imidazopirazinas como inhibidores de proteína cinasas |
| EP2789614B1 (en) * | 2009-08-11 | 2017-04-26 | Bristol-Myers Squibb Company | Azaindazoles as Btk kinase modulators and use thereof |
| WO2011075591A1 (en) | 2009-12-17 | 2011-06-23 | Merial Limited | Anti parasitic dihydroazole compounds and compositions comprising same |
| US9073927B2 (en) | 2010-01-22 | 2015-07-07 | Fundacion Centro Nacional De Investigaciones Oncologicas Carlos Iii | Inhibitors of PI3 kinase |
| US20110190269A1 (en) * | 2010-02-01 | 2011-08-04 | Karlheinz Baumann | Gamma secretase modulators |
| WO2011112687A2 (en) | 2010-03-10 | 2011-09-15 | Kalypsys, Inc. | Heterocyclic inhibitors of histamine receptors for the treatment of disease |
-
2011
- 2011-03-07 TW TW100107575A patent/TW201200518A/zh unknown
- 2011-03-10 AU AU2011224316A patent/AU2011224316B2/en not_active Ceased
- 2011-03-10 ES ES11754043.5T patent/ES2607125T3/es active Active
- 2011-03-10 NZ NZ602041A patent/NZ602041A/en not_active IP Right Cessation
- 2011-03-10 EP EP11754043.5A patent/EP2545058B1/en not_active Not-in-force
- 2011-03-10 CA CA2791417A patent/CA2791417A1/en not_active Abandoned
- 2011-03-10 KR KR1020127026253A patent/KR20130016253A/ko not_active Withdrawn
- 2011-03-10 WO PCT/US2011/027817 patent/WO2011112766A2/en not_active Ceased
- 2011-03-10 CN CN201180019492.3A patent/CN102869666B/zh not_active Expired - Fee Related
- 2011-03-10 PH PH1/2012/501783A patent/PH12012501783A1/en unknown
- 2011-03-10 BR BR112012022211A patent/BR112012022211A2/pt active Search and Examination
- 2011-03-10 MX MX2012010404A patent/MX2012010404A/es active IP Right Grant
- 2011-03-10 UY UY0001033271A patent/UY33271A/es not_active Application Discontinuation
- 2011-03-10 RU RU2012137180/04A patent/RU2012137180A/ru not_active Application Discontinuation
- 2011-03-10 US US13/044,661 patent/US8569300B2/en not_active Expired - Fee Related
- 2011-03-10 JP JP2012557231A patent/JP5888654B2/ja not_active Expired - Fee Related
- 2011-03-11 AR ARP110100765A patent/AR080496A1/es not_active Application Discontinuation
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2012
- 2012-09-06 IL IL221829A patent/IL221829A/en not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| CN102869666B (zh) | 2015-09-09 |
| JP2013522222A (ja) | 2013-06-13 |
| US8569300B2 (en) | 2013-10-29 |
| BR112012022211A2 (pt) | 2017-07-18 |
| KR20130016253A (ko) | 2013-02-14 |
| MX2012010404A (es) | 2013-05-20 |
| PH12012501783A1 (en) | 2015-06-26 |
| AU2011224316B2 (en) | 2016-09-15 |
| TW201200518A (en) | 2012-01-01 |
| EP2545058A2 (en) | 2013-01-16 |
| WO2011112766A2 (en) | 2011-09-15 |
| AU2011224316A1 (en) | 2012-09-13 |
| EP2545058A4 (en) | 2013-07-24 |
| ES2607125T3 (es) | 2017-03-29 |
| NZ602041A (en) | 2014-08-29 |
| JP5888654B2 (ja) | 2016-03-22 |
| EP2545058B1 (en) | 2016-08-24 |
| US20110237565A1 (en) | 2011-09-29 |
| CN102869666A (zh) | 2013-01-09 |
| UY33271A (es) | 2011-10-31 |
| IL221829A (en) | 2014-11-30 |
| WO2011112766A3 (en) | 2012-01-19 |
| RU2012137180A (ru) | 2014-04-20 |
| AR080496A1 (es) | 2012-04-11 |
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Legal Events
| Date | Code | Title | Description |
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| EEER | Examination request |
Effective date: 20160309 |
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| FZDE | Discontinued |
Effective date: 20191122 |