AR078675A1 - Derivados de pirazolo[3,4-d]pirimidina inhibidores de jak quinasas, composiciones farmaceuticas que los comprenden, metodo para prepararlos y uso de los mismos para el tratamiento o profilaxis de trastornos inmunologicos, inflamatorios y autoinmunes. - Google Patents
Derivados de pirazolo[3,4-d]pirimidina inhibidores de jak quinasas, composiciones farmaceuticas que los comprenden, metodo para prepararlos y uso de los mismos para el tratamiento o profilaxis de trastornos inmunologicos, inflamatorios y autoinmunes.Info
- Publication number
- AR078675A1 AR078675A1 ARP100103813A ARP100103813A AR078675A1 AR 078675 A1 AR078675 A1 AR 078675A1 AR P100103813 A ARP100103813 A AR P100103813A AR P100103813 A ARP100103813 A AR P100103813A AR 078675 A1 AR078675 A1 AR 078675A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkynyl
- alkenyl
- same
- optionally substituted
- Prior art date
Links
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 title 1
- 230000001900 immune effect Effects 0.000 title 1
- 208000026278 immune system disease Diseases 0.000 title 1
- 230000002757 inflammatory effect Effects 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 27
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 26
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 25
- 229910052736 halogen Inorganic materials 0.000 abstract 13
- 229910052739 hydrogen Inorganic materials 0.000 abstract 11
- 125000005843 halogen group Chemical group 0.000 abstract 8
- 150000002367 halogens Chemical class 0.000 abstract 5
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 229920006395 saturated elastomer Chemical group 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- YBYIRNPNPLQARY-UHFFFAOYSA-N 1H-indene Chemical group C1=CC=C2CC=CC2=C1 YBYIRNPNPLQARY-UHFFFAOYSA-N 0.000 abstract 1
- 101100160255 Saccharomyces cerevisiae (strain ATCC 204508 / S288c) YLR154C-H gene Proteins 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 abstract 1
- 125000003454 indenyl group Chemical group C1(C=CC2=CC=CC=C12)* 0.000 abstract 1
- 239000002207 metabolite Substances 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 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
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- 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
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
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- 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
- A61K31/495—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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- 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
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- 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
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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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
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P37/00—Drugs for immunological or allergic disorders
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- A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
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- A—HUMAN NECESSITIES
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- A61P5/00—Drugs for disorders of the endocrine system
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- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
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- 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
- C07D403/12—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 chain containing hetero atoms as chain links
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Pulmonology (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Neurology (AREA)
- Reproductive Health (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurosurgery (AREA)
- Gastroenterology & Hepatology (AREA)
- Pain & Pain Management (AREA)
- Surgery (AREA)
- Transplantation (AREA)
- Biomedical Technology (AREA)
- Ophthalmology & Optometry (AREA)
- Emergency Medicine (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Obesity (AREA)
- Oncology (AREA)
- Nutrition Science (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09173535 | 2009-10-20 | ||
| US37535810P | 2010-08-20 | 2010-08-20 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR078675A1 true AR078675A1 (es) | 2011-11-23 |
Family
ID=41531257
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100103813A AR078675A1 (es) | 2009-10-20 | 2010-10-19 | Derivados de pirazolo[3,4-d]pirimidina inhibidores de jak quinasas, composiciones farmaceuticas que los comprenden, metodo para prepararlos y uso de los mismos para el tratamiento o profilaxis de trastornos inmunologicos, inflamatorios y autoinmunes. |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US9242987B2 (enExample) |
| EP (1) | EP2491039A1 (enExample) |
| JP (1) | JP5744887B2 (enExample) |
| KR (1) | KR20120102601A (enExample) |
| CN (1) | CN102666545B (enExample) |
| AR (1) | AR078675A1 (enExample) |
| AU (1) | AU2010309882B2 (enExample) |
| BR (1) | BR112012009327A2 (enExample) |
| CA (1) | CA2775009A1 (enExample) |
| EA (1) | EA022120B1 (enExample) |
| IL (1) | IL218751A0 (enExample) |
| MX (1) | MX2012004020A (enExample) |
| NZ (1) | NZ598907A (enExample) |
| TW (1) | TW201125867A (enExample) |
| WO (1) | WO2011048082A1 (enExample) |
Families Citing this family (70)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| LT2455382T (lt) | 2005-12-13 | 2017-02-10 | Incyte Holdings Corporation | Heteroarilu pakeisti pirolo[2,3-b]piridinai ir prolo[2,3-b]pirimidinai kaip janus kinazės inhibitoriai |
| DK2740731T3 (en) | 2007-06-13 | 2016-04-11 | Incyte Holdings Corp | CRYSTALLINE SALTS OF JANUSKINASEINHIBITOREN (R) -3- (4- (7H-pyrrolo [2,3-d] pyrimidin-4-yl) -1H-pyrazol-1-yl) -3-CYCLOPENTYLPROPANNITRIL |
| BRPI0914404A2 (pt) | 2008-10-31 | 2019-03-06 | Genentech Inc | "compostos, composição farmacêutica e método para tratar ou atenuar a gravidade de uma doença ou condição responsiva à inibição da atividade jak quinase em um paciente" |
| WO2010135621A1 (en) | 2009-05-22 | 2010-11-25 | Incyte Corporation | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors |
| SG177384A1 (en) | 2009-06-29 | 2012-02-28 | Incyte Corp | Pyrimidinones as pi3k inhibitors |
| UA110324C2 (en) | 2009-07-02 | 2015-12-25 | Genentech Inc | Jak inhibitory compounds based on pyrazolo pyrimidine |
| WO2011075643A1 (en) | 2009-12-18 | 2011-06-23 | Incyte Corporation | Substituted heteroaryl fused derivatives as pi3k inhibitors |
| US8765734B2 (en) | 2010-03-10 | 2014-07-01 | Incyte Corporation | Piperidin-4-yl azetidine derivatives as JAK1 inhibitors |
| WO2011130342A1 (en) | 2010-04-14 | 2011-10-20 | Incyte Corporation | FUSED DERIVATIVES AS ΡI3Κδ INHIBITORS |
| AU2011255443B2 (en) | 2010-05-21 | 2014-07-03 | Incyte Holdings Corporation | Topical formulation for a JAK inhibitor |
| WO2011163195A1 (en) | 2010-06-21 | 2011-12-29 | Incyte Corporation | Fused pyrrole derivatives as pi3k inhibitors |
| US9040545B2 (en) | 2010-08-20 | 2015-05-26 | Cellzome Limited | Heterocyclyl pyrazolopyrimidine analogues as selective JAK inhibitors |
| RU2013114352A (ru) | 2010-09-15 | 2014-10-20 | Ф. Хоффманн-Ля Рош Аг | Азабензотиазолы, композиции и способы применения |
| SG190839A1 (en) | 2010-11-19 | 2013-07-31 | Incyte Corp | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| RU2013126041A (ru) | 2010-11-19 | 2014-12-27 | Ф.Хоффманн-Ля Рош Аг | Пиразолопиридины и пиразолопиридины и их применение в качестве ингибиторов tyk2 |
| AR084366A1 (es) | 2010-12-20 | 2013-05-08 | Incyte Corp | N-(1-(fenil sustituido)etil)-9h-purin-6-aminas como inhibidores de pi3k |
| US9108984B2 (en) | 2011-03-14 | 2015-08-18 | Incyte Corporation | Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors |
| WO2012135009A1 (en) | 2011-03-25 | 2012-10-04 | Incyte Corporation | Pyrimidine-4,6-diamine derivatives as pi3k inhibitors |
| WO2012143320A1 (en) | 2011-04-18 | 2012-10-26 | Cellzome Limited | (7h-pyrrolo[2,3-d]pyrimidin-2-yl)amine compounds as jak3 inhibitors |
| WO2012177606A1 (en) | 2011-06-20 | 2012-12-27 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors |
| AU2012288892B2 (en) * | 2011-07-28 | 2016-04-21 | Cellzome Limited | Heterocyclyl pyrimidine analogues as JAK inhibitors |
| WO2013017480A1 (en) | 2011-07-29 | 2013-02-07 | Cellzome Limited | Pyrazolo[4,3-c]pyridine derivatives as jak inhibitors |
| WO2013017479A1 (en) | 2011-07-29 | 2013-02-07 | Cellzome Limited | Pyrazolo[4,3-c]pyridine derivatives as jak inhibitors |
| KR102249236B1 (ko) | 2011-09-02 | 2021-05-10 | 인사이트 홀딩스 코포레이션 | Pi3k 억제제로서 헤테로시클릴아민 |
| UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
| AU2012311504B2 (en) * | 2011-09-20 | 2016-03-24 | Cellzome Limited | Pyrazolo[4,3-C]pyridine derivatives as kinase inhibitors |
| BR112014015723A8 (pt) | 2011-12-23 | 2017-07-04 | Cellzome Ltd | derivados de pirimidino-2,4-diamina como inibidores da quinase |
| CN103193600B (zh) * | 2012-01-07 | 2016-04-06 | 浙江九洲药物科技有限公司 | 卡巴拉汀中间体的制备方法 |
| AU2012367141B2 (en) * | 2012-01-28 | 2016-12-22 | Merck Patent Gmbh | Triazolo[4,5-d]pyrimidine derivatives |
| AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
| US9296725B2 (en) | 2012-05-24 | 2016-03-29 | Cellzome Limited | Heterocyclyl pyrimidine analogues as TYK2 inhibitors |
| NZ748448A (en) | 2012-11-15 | 2019-12-20 | Incyte Holdings Corp | Sustained-release dosage forms of ruxolitinib |
| AP2015008604A0 (en) | 2013-01-23 | 2015-07-31 | Astrazeneca Ab | Chemical compounds |
| EP3489239B1 (en) | 2013-03-06 | 2021-09-15 | Incyte Holdings Corporation | Processes and intermediates for making a jak inhibitor |
| EP3721873A1 (en) | 2013-08-07 | 2020-10-14 | Incyte Corporation | Sustained release dosage forms for a jak1 inhibitor |
| US20160222014A1 (en) * | 2013-09-10 | 2016-08-04 | Asana Biosciences, Llc | Compounds for regulating fak and/or src pathways |
| JP6487426B2 (ja) | 2013-10-17 | 2019-03-20 | ダウ アグロサイエンシィズ エルエルシー | 有害生物防除化合物の調製法 |
| TWI699364B (zh) | 2014-05-23 | 2020-07-21 | 瑞士商赫孚孟拉羅股份公司 | 5-氯-2-二氟甲氧基苯基吡唑并嘧啶化合物、組合物及其使用方法 |
| WO2015184305A1 (en) | 2014-05-30 | 2015-12-03 | Incyte Corporation | TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1 |
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- 2010-10-19 JP JP2012534661A patent/JP5744887B2/ja not_active Expired - Fee Related
- 2010-10-19 CN CN201080058290.5A patent/CN102666545B/zh not_active Expired - Fee Related
- 2010-10-19 EA EA201270572A patent/EA022120B1/ru not_active IP Right Cessation
- 2010-10-19 TW TW099135495A patent/TW201125867A/zh unknown
- 2010-10-19 KR KR1020127009821A patent/KR20120102601A/ko not_active Ceased
- 2010-10-19 AU AU2010309882A patent/AU2010309882B2/en not_active Ceased
- 2010-10-19 WO PCT/EP2010/065700 patent/WO2011048082A1/en not_active Ceased
- 2010-10-19 BR BR112012009327A patent/BR112012009327A2/pt not_active IP Right Cessation
- 2010-10-19 MX MX2012004020A patent/MX2012004020A/es not_active Application Discontinuation
- 2010-10-19 CA CA2775009A patent/CA2775009A1/en not_active Abandoned
- 2010-10-19 NZ NZ598907A patent/NZ598907A/en not_active IP Right Cessation
- 2010-10-19 EP EP10775748A patent/EP2491039A1/en not_active Withdrawn
- 2010-10-19 AR ARP100103813A patent/AR078675A1/es unknown
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2012
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|---|---|
| EA022120B1 (ru) | 2015-11-30 |
| US9242987B2 (en) | 2016-01-26 |
| CN102666545A (zh) | 2012-09-12 |
| TW201125867A (en) | 2011-08-01 |
| CA2775009A1 (en) | 2011-04-28 |
| CN102666545B (zh) | 2016-04-06 |
| US20120252779A1 (en) | 2012-10-04 |
| IL218751A0 (en) | 2012-06-28 |
| AU2010309882A1 (en) | 2012-04-12 |
| BR112012009327A2 (pt) | 2017-06-06 |
| KR20120102601A (ko) | 2012-09-18 |
| JP2013508332A (ja) | 2013-03-07 |
| MX2012004020A (es) | 2012-05-08 |
| NZ598907A (en) | 2014-03-28 |
| AU2010309882B2 (en) | 2016-01-28 |
| EP2491039A1 (en) | 2012-08-29 |
| JP5744887B2 (ja) | 2015-07-08 |
| EA201270572A1 (ru) | 2012-12-28 |
| WO2011048082A1 (en) | 2011-04-28 |
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