PE20120026A1 - 2-metil-1-(fenilsulfonil)-4-piperazin-1-il-1h-benzimidazol como ligando de 5-hidroxitriptamina-6 (5-ht6) - Google Patents
2-metil-1-(fenilsulfonil)-4-piperazin-1-il-1h-benzimidazol como ligando de 5-hidroxitriptamina-6 (5-ht6)Info
- Publication number
- PE20120026A1 PE20120026A1 PE2011001015A PE2011001015A PE20120026A1 PE 20120026 A1 PE20120026 A1 PE 20120026A1 PE 2011001015 A PE2011001015 A PE 2011001015A PE 2011001015 A PE2011001015 A PE 2011001015A PE 20120026 A1 PE20120026 A1 PE 20120026A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- piperazin
- benzimidazole
- methyl
- hydroxy
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 abstract 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical group [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 abstract 3
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical class O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 2
- -1 CYANE Chemical class 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 208000015114 central nervous system disease Diseases 0.000 abstract 1
- GEAXLHPORCRESC-UHFFFAOYSA-N chlorocyclohexatriene Chemical class ClC1=CC=C=C[CH]1 GEAXLHPORCRESC-UHFFFAOYSA-N 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/22—Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms directly attached to ring nitrogen atoms
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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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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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
-
- 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
- A61P25/06—Antimigraine agents
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
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- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P25/24—Antidepressants
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- 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
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- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
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- 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
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- 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
- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D487/08—Bridged systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Child & Adolescent Psychology (AREA)
- Addiction (AREA)
- Anesthesiology (AREA)
- Nutrition Science (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
SE REFIERE A UN COMPUESTO DE FORMULA (I) DONDE: R1a Y R1b SON CADA UNO H, ALQUILO C1-C6, ALQUENILO C2-C6, ALQUINILO C2-C6 SUSTITUIDO CON 0-4 SUSTITUYENTES SELECCIONADOS ENTRE ALQUILO C1-C4, CICLOALQUILO C3-C6; R2 ES H, ALQUILO C1-C4, -CHO, -C(O)(ALQUILO C1-4); R3 ES HIDROXI, HALO, NITRO, CIANO, ENTRE OTROS; R4 ES H, HIDROXI, ALQUILO C1-C6, ENTRE OTROS; R5, R6, R7, R8 Y R9 SON CADA UNO H, HALO, NITRO, CIANO, HIDROXI, ENTRE OTROS; m ES 0-2. SON COMPUESTOS PREFERIDOS: 4-(4-METILPIPERAZIN-1-IL)-1-(NAFTALEN-1-ILSULFONIL)-1H-BENZO[d]IMIDAZOL; 2-METIL-1-(1-NAFTILSULFONIL)-4-PIPERAZIN-1-IL-1H-BENZIMIDAZOL; 1-[(4-CLOROFENIL)SULFONIL]-4-PIPERAZIN-1-IL-1H-BENZIMIDAZOL; ENTRE OTROS. REFERIDA TAMBIEN A UNA COMPOSICON FARMACEUTICA Y METODO DE SINTESIS. DICHO COMPUESTO MODULA LA ACTIVIDAD DE 5-HT6, SIENDO UTIL EN EL TRATAMIENTO DE TRANSTORNOS DEL SISTEMA NERVIOSO CENTRAL
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11329608P | 2008-11-11 | 2008-11-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20120026A1 true PE20120026A1 (es) | 2012-02-12 |
Family
ID=41404503
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2011001015A PE20120026A1 (es) | 2008-11-11 | 2009-11-10 | 2-metil-1-(fenilsulfonil)-4-piperazin-1-il-1h-benzimidazol como ligando de 5-hidroxitriptamina-6 (5-ht6) |
Country Status (42)
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2007003327A (es) * | 2004-09-20 | 2007-06-05 | Xenon Pharmaceuticals Inc | Derivados heterociclicos, y su uso como mediadores de estearoil-coa desaturasa. |
| EP2269610A3 (en) * | 2004-09-20 | 2011-03-09 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors |
| AU2005286648A1 (en) * | 2004-09-20 | 2006-03-30 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors |
| CA2580781A1 (en) * | 2004-09-20 | 2006-03-30 | Xenon Pharmaceuticals Inc. | Bicyclic heterocyclic derivatives and their use as inhibitors of stearoyl-coa-desaturase (scd) |
| CN104557726B (zh) * | 2013-10-19 | 2019-05-24 | 广东东阳光药业有限公司 | 芳杂环类衍生物及其在药物上的应用 |
| CA2953004C (en) | 2014-07-08 | 2023-02-21 | Sunshine Lake Pharma Co., Ltd. | Aromatic heterocyclic derivatives and pharmaceutical applications thereof |
| WO2017052394A1 (en) | 2015-09-23 | 2017-03-30 | Uniwersytet Jagielloński | Imidazopyridine compounds and their use as 5-ht6 receptor ligands |
| EP3530651A1 (en) * | 2018-02-21 | 2019-08-28 | Adamed sp. z o.o. | Indole and benzimidazole derivatives as dual 5-ht2a and 5-ht6 receptor antagonists |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3155008B2 (ja) * | 1994-07-26 | 2001-04-09 | ファイザー・インコーポレーテッド | セロトニンアゴニストおよびアンタゴニストとしての４−インドール誘導体 |
| US5849759A (en) * | 1995-12-08 | 1998-12-15 | Berlex Laboratories, Inc. | Naphthyl-substituted benzimidazole derivatives as anti-coagulants |
| DZ2376A1 (fr) | 1996-12-19 | 2002-12-28 | Smithkline Beecham Plc | Dérivés de sulfonamides nouveaux procédé pour leurpréparation et compositions pharmaceutiques les c ontenant. |
| EP0994862B1 (en) | 1997-07-11 | 2005-06-01 | SmithKline Beecham plc | Sulphonamide derivatives being 5-ht6 receptor antagonists and process for their preparation |
| GB9716656D0 (en) * | 1997-08-07 | 1997-10-15 | Zeneca Ltd | Chemical compounds |
| EP0930302B1 (en) * | 1998-01-16 | 2003-04-02 | F.Hoffmann-La Roche Ag | Benzosulfone derivatives |
| US6251893B1 (en) * | 1998-06-15 | 2001-06-26 | Nps Allelix Corp. | Bicyclic piperidine and piperazine compounds having 5-HT6 receptor affinity |
| BR9912937A (pt) * | 1998-08-10 | 2001-05-08 | Partnership Of Michael E Garst | Pró-drogas de inibidores de bomba de prótons |
| GB9818916D0 (en) * | 1998-08-28 | 1998-10-21 | Smithkline Beecham Plc | Use |
| SE0002754D0 (sv) | 2000-07-21 | 2000-07-21 | Pharmacia & Upjohn Ab | New pharmaceutical combination formulation and method of treatment with the combination |
| SE0003810D0 (sv) * | 2000-10-20 | 2000-10-20 | Pharmacia Ab | Novel compounds their use and preparations |
| CA2422717A1 (en) | 2000-10-20 | 2002-04-25 | Biovitrum Ab | 2-, 3-, 4-, or 5-substituted-n1-(benzensulfonyl)indoles and their use in therapy |
| US7034029B2 (en) * | 2000-11-02 | 2006-04-25 | Wyeth | 1-aryl- or 1-alkylsulfonyl-heterocyclylbenzazoles as 5-hydroxytryptamine-6 ligands |
| AU2002220051B2 (en) * | 2000-11-02 | 2007-05-24 | Wyeth | 1-aryl- or 1-alkylsulfonyl-heterocyclylbenzazoles as 5-hydroxytryptamine-6 ligands |
| CN1321110C (zh) * | 2001-06-15 | 2007-06-13 | 弗·哈夫曼-拉罗切有限公司 | 具有5－ht6受体亲和力的4－哌嗪基吲哚衍生物 |
| ATE331707T1 (de) * | 2001-06-15 | 2006-07-15 | Hoffmann La Roche | 4 piperazinylindolderivate mit affinität zum 5- ht6-rezeptor |
| WO2003026665A1 (en) | 2001-09-26 | 2003-04-03 | Bayer Pharmaceuticals Corporation | 2-phenylamino-4-(5-pyrazolylamino)-pyrimidine derivatives as kinase inhibitors, in particular, src kinase inhibitors |
| WO2004035740A2 (en) | 2002-10-15 | 2004-04-29 | Synta Pharmaceuticals Corp. | Aromatic bicyclic heterocyles to modulate 1l - 12 production |
| US7745436B2 (en) | 2004-04-13 | 2010-06-29 | Synta Pharmaceuticals Corporation | Disalt inhibitors of IL-12 production |
| CN101365696A (zh) | 2004-07-28 | 2009-02-11 | Irm责任有限公司 | 作为类固醇激素核受体调节剂的化合物和组合物 |
| US7713954B2 (en) * | 2004-09-30 | 2010-05-11 | Roche Palo Alto Llc | Compositions and methods for treating cognitive disorders |
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2009
- 2009-10-11 UA UAA201105862A patent/UA100192C2/uk unknown
- 2009-11-10 ES ES09752080T patent/ES2389694T3/es active Active
- 2009-11-10 AP AP2011005664A patent/AP2814A/xx active
- 2009-11-10 JP JP2011536412A patent/JP5087171B2/ja not_active Expired - Fee Related
- 2009-11-10 AU AU2009314221A patent/AU2009314221B2/en not_active Ceased
- 2009-11-10 MX MX2011004996A patent/MX2011004996A/es active IP Right Grant
- 2009-11-10 CA CA2740262A patent/CA2740262C/en not_active Expired - Fee Related
- 2009-11-10 PL PL09752080T patent/PL2285784T3/pl unknown
- 2009-11-10 NZ NZ592563A patent/NZ592563A/xx not_active IP Right Cessation
- 2009-11-10 BR BRPI0920682A patent/BRPI0920682A2/pt not_active IP Right Cessation
- 2009-11-10 PT PT09752080T patent/PT2285784E/pt unknown
- 2009-11-10 EA EA201100696A patent/EA018369B1/ru not_active IP Right Cessation
- 2009-11-10 CN CN200980144578.1A patent/CN102209713B/zh not_active Expired - Fee Related
- 2009-11-10 KR KR1020117010610A patent/KR101323417B1/ko not_active Expired - Fee Related
- 2009-11-10 ME MEP-2011-75A patent/ME01129B/me unknown
- 2009-11-10 WO PCT/US2009/063816 patent/WO2010056644A1/en active Application Filing
- 2009-11-10 GE GEAP200912221A patent/GEP20135805B/en unknown
- 2009-11-10 SI SI200930293T patent/SI2285784T1/sl unknown
- 2009-11-10 EP EP09752080A patent/EP2285784B1/en active Active
- 2009-11-10 RS RS20120326A patent/RS52381B/en unknown
- 2009-11-10 DK DK09752080.3T patent/DK2285784T3/da active
- 2009-11-10 MY MYPI2011001681A patent/MY156324A/en unknown
- 2009-11-10 PE PE2011001015A patent/PE20120026A1/es not_active Application Discontinuation
- 2009-11-11 AR ARP090104372A patent/AR074325A1/es not_active Application Discontinuation
- 2009-11-11 SA SA109300673A patent/SA109300673B1/ar unknown
- 2009-11-11 US US12/616,201 patent/US8063053B2/en not_active Expired - Fee Related
- 2009-11-11 TW TW098138260A patent/TWI481605B/zh not_active IP Right Cessation
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2011
- 2011-04-07 IL IL212213A patent/IL212213A0/en not_active IP Right Cessation
- 2011-04-22 TN TN2011000203A patent/TN2011000203A1/fr unknown
- 2011-05-05 ZA ZA2011/03283A patent/ZA201103283B/en unknown
- 2011-05-10 DO DO2011000130A patent/DOP2011000130A/es unknown
- 2011-05-10 NI NI201100093A patent/NI201100093A/es unknown
- 2011-05-10 CL CL2011001050A patent/CL2011001050A1/es unknown
- 2011-05-11 EC EC2011011045A patent/ECSP11011045A/es unknown
- 2011-05-11 CU CU2011000101A patent/CU24020B1/es active IP Right Grant
- 2011-05-11 CR CR20110247A patent/CR20110247A/es unknown
- 2011-05-11 SV SV2011003902A patent/SV2011003902A/es unknown
- 2011-05-11 MA MA33836A patent/MA32788B1/fr unknown
- 2011-05-12 CO CO11058600A patent/CO6440548A2/es active IP Right Grant
- 2011-12-06 HK HK11113150.6A patent/HK1158647A1/xx not_active IP Right Cessation
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2012
- 2012-07-09 HR HRP20120561AT patent/HRP20120561T1/hr unknown
- 2012-08-13 CY CY20121100721T patent/CY1113025T1/el unknown
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