CO6251262A2 - Nuevos derivados de acido dicarboxilico como agonistas de los receptores de s1p1 - Google Patents
Nuevos derivados de acido dicarboxilico como agonistas de los receptores de s1p1Info
- Publication number
- CO6251262A2 CO6251262A2 CO09143477A CO09143477A CO6251262A2 CO 6251262 A2 CO6251262 A2 CO 6251262A2 CO 09143477 A CO09143477 A CO 09143477A CO 09143477 A CO09143477 A CO 09143477A CO 6251262 A2 CO6251262 A2 CO 6251262A2
- Authority
- CO
- Colombia
- Prior art keywords
- alkyl
- group
- cycloalkyl
- hydrogen
- aryl
- Prior art date
Links
- 102100025750 Sphingosine 1-phosphate receptor 1 Human genes 0.000 title 1
- 101710155454 Sphingosine 1-phosphate receptor 1 Proteins 0.000 title 1
- 239000002253 acid Substances 0.000 title 1
- 239000000556 agonist Substances 0.000 title 1
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 125000002877 alkyl aryl group Chemical group 0.000 abstract 2
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 150000002431 hydrogen Chemical group 0.000 abstract 1
- WCPAKWJPBJAGKN-UHFFFAOYSA-N oxadiazole Chemical group C1=CON=N1 WCPAKWJPBJAGKN-UHFFFAOYSA-N 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
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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
- A61P11/00—Drugs for disorders of the respiratory system
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- 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/16—Central respiratory analeptics
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- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A—HUMAN NECESSITIES
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- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P37/08—Antiallergic agents
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- 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
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- 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
- A61P9/08—Vasodilators for multiple indications
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- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
- C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
- C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Virology (AREA)
- Oncology (AREA)
- Neurology (AREA)
- Communicable Diseases (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Neurosurgery (AREA)
- Heart & Thoracic Surgery (AREA)
- Biomedical Technology (AREA)
- Molecular Biology (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Dermatology (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Psychiatry (AREA)
- Transplantation (AREA)
- Obesity (AREA)
- Hospice & Palliative Care (AREA)
- Emergency Medicine (AREA)
- Otolaryngology (AREA)
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Abstract
1.- El compuesto de la fórmula (I)(I)en donderepresenta un grupo de oxadiazol 1, 2, 4; X1 es un anillo mono-, bi- o triciclíco seleccionado de un grupo heterocíclico, heteroarilo, arilo o un grupo cicloalquilo que incluye opcionalmente uno o más sistemas insaturados; R1 se selecciona del grupo que consiste de hidrógeno, halo, perhaloalquilo, perhaloalcoxi, arilo, arilalquilo, alquilarilo, alquilo, alquenilo, alquinilo, -N(R2)2 y cicloalquilo que opcionalmente comprende uno o más sistemas insaturados; caracterizado porque el grupo arilo puede fusionarse con un anillo que comprende de 2 a 5 átomos seleccionados de un carbono o heteroátomo; además se caracteriza porque cada R1 se sustituye opcionalmente, desde uno hasta el número máximo de posiciones que pueden ser sustituidas, por un sustituyente seleccionado independientemente de un grupo que consiste en halo, -alquilo, -O-alquilo, cicloalquilo, arilo, arilalquilo, alquilarilo y perhaloalquilo; y cada R2 se selecciona independientemente de hidrógeno, -alquilo, -cicloalquilo, -CO-(O)r-alquilo, -CO-(O)r-cicloalquilo, -O-CO-alquilo, -O-CO- cicloalquilo, en donde r es 0 o 1; Y1 representa una unión o Y1 se selecciona de un grupo formado por -O- ; S(O)q-, caracterizado porque q es 0, 1 o 2; y -C=Q-, en donde Q es O, S, N-R' o N-OR', caracterizado porque R' se selecciona de hidrógeno, -alquilo, -alquenilo, -alquinilo, -alcoxi, -cicloalquilo o -perhaloalquilo; cada porción R1-Y1, idéntica o diferente, representa un grupo que está unido a la estructura de anillo cíclico X1 y m es un entero seleccionado de 1 a 9, caracterizado porque m representa el número de posiciones de X1 sustituidas por una porción R1-Y1. Y2 representa una unión o Y2 se selecciona de un grupo compuesto de -O-; -CH2-; -C(O)O-; -C(O)NH-; -S(O)q-, caracterizado porque q es 0, 1 o 2; y -C=Q-, en donde Q es O, S, N-(R')2 o N-OR', caracterizado porque cada R' se selecciona independientemente de hidrógeno, -alquilo, ...
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP07290748A EP2014653A1 (en) | 2007-06-15 | 2007-06-15 | Novel dicarboxylic acid derivatives as S1P1 receptor agonists |
Publications (1)
Publication Number | Publication Date |
---|---|
CO6251262A2 true CO6251262A2 (es) | 2011-02-21 |
Family
ID=38645817
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CO09143477A CO6251262A2 (es) | 2007-06-15 | 2009-12-15 | Nuevos derivados de acido dicarboxilico como agonistas de los receptores de s1p1 |
Country Status (17)
Country | Link |
---|---|
US (1) | US8809539B2 (es) |
EP (2) | EP2014653A1 (es) |
JP (1) | JP5346016B2 (es) |
KR (1) | KR20100040853A (es) |
CN (1) | CN101784535A (es) |
BR (1) | BRPI0811712A2 (es) |
CA (1) | CA2693126A1 (es) |
CO (1) | CO6251262A2 (es) |
EA (1) | EA018826B1 (es) |
IL (1) | IL202741A0 (es) |
MA (1) | MA31447B1 (es) |
MX (1) | MX2009013733A (es) |
NZ (1) | NZ581933A (es) |
TN (1) | TN2009000524A1 (es) |
UA (1) | UA99132C2 (es) |
WO (1) | WO2008152149A1 (es) |
ZA (1) | ZA200908851B (es) |
Families Citing this family (28)
Publication number | Priority date | Publication date | Assignee | Title |
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EP2193126B1 (en) | 2007-10-04 | 2015-06-24 | Merck Serono S.A. | Oxadiazole diaryl compounds |
US8202865B2 (en) * | 2007-10-04 | 2012-06-19 | Merck Serono Sa | Oxadiazole derivatives |
EP2209771A1 (en) * | 2007-11-08 | 2010-07-28 | Pfizer, Inc. | Cyclobutyl carboxylic acid derivatives |
HUE030424T2 (en) | 2008-07-23 | 2017-05-29 | Arena Pharm Inc | Substituted 1,2,3,4-tetrahydrocyclopenta [b] indol-3-ylacetic acid derivatives useful in the treatment of autoimmune and inflammatory disorders |
BRPI0917923B1 (pt) | 2008-08-27 | 2022-04-05 | Arena Pharmaceuticals Inc | Derivado de ácido tricíclico substituído, sua composição, seu uso e processo para preparar a referida composição |
EP2344446A4 (en) | 2008-10-17 | 2012-04-04 | Akaal Pharma Pty Ltd | S1P RECEPTOR MODULATORS |
NZ592748A (en) | 2008-10-17 | 2013-01-25 | Akaal Pharma Pty Ltd | 2-Amino-(oxadiazol-3-yl)-benzofuran derivatives and their use as S1P receptor modulators |
EP2241558A1 (en) * | 2009-04-03 | 2010-10-20 | Merck Serono SA | Oxadiazole derivatives |
WO2011048409A1 (en) | 2009-10-20 | 2011-04-28 | Astrazeneca Ab | Cyclic amine derivatives having beta2 adrenergic receptor agonist and muscarinic receptor antagonist activity |
EP3378854B1 (en) | 2010-01-27 | 2022-12-21 | Arena Pharmaceuticals, Inc. | Processes for the preparation of (r)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid and salts thereof |
JP2013521301A (ja) | 2010-03-03 | 2013-06-10 | アリーナ ファーマシューティカルズ, インコーポレイテッド | S1p1受容体修飾物質およびその結晶形の調製のためのプロセス |
CN103119038B (zh) * | 2010-04-23 | 2016-05-04 | 百时美施贵宝公司 | 作为1-磷酸鞘氨醇1受体激动剂的4-(5-异噁唑基或5-吡唑基-1,2,4-噁二唑基-3-基)扁桃酰胺 |
CA2797668A1 (en) | 2010-04-27 | 2011-11-03 | Allergan, Inc. | 3-(4-((1h-imidazol-1-yl)methyl)phenyl)-5-aryl-1,2,4-oxadiazole derivatives as sphingosine-1 phosphate receptors modulators |
US9050334B2 (en) | 2010-07-16 | 2015-06-09 | Innov88 Llc | MIF inhibitors and their uses |
ES2539256T3 (es) | 2010-07-20 | 2015-06-29 | Bristol-Myers Squibb Company | Compuestos de 3-fenil-1,2,4-oxadiazol sustituidos |
WO2012112841A2 (en) * | 2011-02-18 | 2012-08-23 | Abbott Laboratories | [1,2,4]oxadiazol-3-yl acid salts and crystalline forms and their preparation |
EP2511275A1 (en) * | 2011-04-12 | 2012-10-17 | Bioprojet | Novel piperidinyl monocarboxylic acids as S1P1 receptor agonists |
MX2021011472A (es) | 2015-01-06 | 2022-08-17 | Arena Pharm Inc | Metodos de condiciones de tratamiento relacionadas con el receptor s1p1. |
KR102603199B1 (ko) | 2015-06-22 | 2023-11-16 | 아레나 파마슈티칼스, 인크. | S1p1 수용체-관련 장애에서의 사용을 위한 (r)-2-(7-(4-시클로펜틸-3-(트리플루오로메틸)벤질옥시)-1,2,3,4-테트라히드로시클로-펜타[b]인돌-3-일)아세트산 (화합물 1)의 결정성 l-아르기닌 염 |
WO2018119080A1 (en) * | 2016-12-21 | 2018-06-28 | Cornell University | Compositions and methods for treating hepatic disorders |
WO2018151873A1 (en) | 2017-02-16 | 2018-08-23 | Arena Pharmaceuticals, Inc. | Compounds and methods for treatment of primary biliary cholangitis |
CA3053416A1 (en) | 2017-02-16 | 2018-08-23 | Arena Pharmaceuticals, Inc. | Compounds and methods for treatment of inflammatory bowel disease with extra-intestinal manifestations |
CN107827837B (zh) * | 2017-11-21 | 2021-09-24 | 苏州朗科生物技术股份有限公司 | 鞘氨醇-1-磷酸受体调节剂化合物及其制备方法与应用 |
SG11202006255UA (en) * | 2018-02-02 | 2020-07-29 | Univ Kyoto | Medicine for preventing or treating ophthalmic disease associated with enhanced intraocular neovascularization and/or intraocular vascular permeability |
EP3847158A1 (en) | 2018-09-06 | 2021-07-14 | Arena Pharmaceuticals, Inc. | Compounds useful in the treatment of autoimmune and inflammatory disorders |
CN111803636B (zh) * | 2020-07-22 | 2022-08-30 | 四川大学 | 1-磷酸鞘氨醇受体1作为microRNA-9调控血管生成的药物靶点的应用 |
RU2765464C1 (ru) * | 2021-05-20 | 2022-01-31 | Федеральное государственное бюджетное учреждение науки Институт органической химии им. Н.Д. Зеленского Российской академии наук (ИОХ РАН) | Способ получения эфиров пиперидин-4,4-дикарбоновых кислот |
JP7464075B2 (ja) | 2022-04-20 | 2024-04-09 | 株式会社大林組 | プレストレス構造及びそれを用いたプレキャストコンクリート部材 |
Family Cites Families (5)
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JP2005533058A (ja) * | 2002-06-17 | 2005-11-04 | メルク エンド カムパニー インコーポレーテッド | Edg受容体アゴニストとしての1−((5−アリール−1,2,4−オキサジアゾール−3−イル)ベンジル)アゼチジン−3−カルボキシラートおよび1−((5−アリール−1,2,4−オキサジアゾール−3−イル)ベンジル)ピロリジン−3−カルボキシラート |
WO2004035538A1 (en) * | 2002-10-15 | 2004-04-29 | Merck & Co., Inc. | Process for making azetidine-3-carboxylic acid |
JP4516430B2 (ja) * | 2002-12-20 | 2010-08-04 | メルク・シャープ・エンド・ドーム・コーポレイション | 1−(アミノ)インダン並びに(1,2−ジヒドロ−3−アミノ)−ベンゾフラン、ベンゾチオフェン及びインドール |
TW200538433A (en) * | 2004-02-24 | 2005-12-01 | Irm Llc | Immunosuppressant compounds and compositiions |
PL1650186T3 (pl) * | 2004-10-22 | 2008-11-28 | Bioprojet Soc Civ | Nowe pochodne kwasów dikarboksylowych |
-
2007
- 2007-06-15 EP EP07290748A patent/EP2014653A1/en not_active Withdrawn
-
2008
- 2008-06-16 CN CN200880100811A patent/CN101784535A/zh active Pending
- 2008-06-16 JP JP2010511664A patent/JP5346016B2/ja not_active Expired - Fee Related
- 2008-06-16 US US12/664,718 patent/US8809539B2/en not_active Expired - Fee Related
- 2008-06-16 KR KR1020107000880A patent/KR20100040853A/ko not_active Application Discontinuation
- 2008-06-16 EA EA201000024A patent/EA018826B1/ru not_active IP Right Cessation
- 2008-06-16 MX MX2009013733A patent/MX2009013733A/es active IP Right Grant
- 2008-06-16 CA CA2693126A patent/CA2693126A1/en not_active Abandoned
- 2008-06-16 UA UAA200912896A patent/UA99132C2/ru unknown
- 2008-06-16 WO PCT/EP2008/057571 patent/WO2008152149A1/en active Application Filing
- 2008-06-16 BR BRPI0811712-8A2A patent/BRPI0811712A2/pt not_active IP Right Cessation
- 2008-06-16 NZ NZ581933A patent/NZ581933A/en not_active IP Right Cessation
- 2008-06-16 EP EP08761078.8A patent/EP2170850B1/en active Active
-
2009
- 2009-12-11 ZA ZA200908851A patent/ZA200908851B/xx unknown
- 2009-12-11 TN TNP2009000524A patent/TN2009000524A1/fr unknown
- 2009-12-15 IL IL202741A patent/IL202741A0/en unknown
- 2009-12-15 MA MA32421A patent/MA31447B1/fr unknown
- 2009-12-15 CO CO09143477A patent/CO6251262A2/es not_active Application Discontinuation
Also Published As
Publication number | Publication date |
---|---|
EP2170850A1 (en) | 2010-04-07 |
EA018826B1 (ru) | 2013-11-29 |
KR20100040853A (ko) | 2010-04-21 |
EP2170850B1 (en) | 2014-09-24 |
TN2009000524A1 (en) | 2011-03-31 |
US8809539B2 (en) | 2014-08-19 |
JP2010529977A (ja) | 2010-09-02 |
NZ581933A (en) | 2012-01-12 |
UA99132C2 (ru) | 2012-07-25 |
MA31447B1 (fr) | 2010-06-01 |
BRPI0811712A2 (pt) | 2014-11-04 |
EP2014653A1 (en) | 2009-01-14 |
IL202741A0 (en) | 2010-06-30 |
US20100249187A1 (en) | 2010-09-30 |
CN101784535A (zh) | 2010-07-21 |
EA201000024A1 (ru) | 2010-06-30 |
WO2008152149A1 (en) | 2008-12-18 |
MX2009013733A (es) | 2010-04-22 |
AU2008263817A1 (en) | 2008-12-18 |
JP5346016B2 (ja) | 2013-11-20 |
ZA200908851B (en) | 2010-07-28 |
CA2693126A1 (en) | 2008-12-18 |
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