EA201171011A1 - DERIVATIVES OF 6- (6-O-SUBSTITUTED TRIAZOLOPIRIDAZINSULFANIL) BENZOTIAZOLES AND -BENZIMIDAZOLES: OBTAINING, APPLICATION AS MEDICINE AND USING AS INHIBITORS - Google Patents
DERIVATIVES OF 6- (6-O-SUBSTITUTED TRIAZOLOPIRIDAZINSULFANIL) BENZOTIAZOLES AND -BENZIMIDAZOLES: OBTAINING, APPLICATION AS MEDICINE AND USING AS INHIBITORSInfo
- Publication number
- EA201171011A1 EA201171011A1 EA201171011A EA201171011A EA201171011A1 EA 201171011 A1 EA201171011 A1 EA 201171011A1 EA 201171011 A EA201171011 A EA 201171011A EA 201171011 A EA201171011 A EA 201171011A EA 201171011 A1 EA201171011 A1 EA 201171011A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- cycloalkyl
- inhibitors
- triazolopiridazinsulfanil
- benzotiazoles
- benzimidazoles
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
- C07D277/62—Benzothiazoles
- C07D277/68—Benzothiazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
- C07D277/82—Nitrogen atoms
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines 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
- 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
-
- 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
-
- 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
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- 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
-
- 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
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- 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]
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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
-
- 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
- A61P3/08—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
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
- A61P37/08—Antiallergic 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine 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
-
- 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
- A61P9/10—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
-
- 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
Abstract
Настоящее изобретение относится к новым продуктам формулы (I), в которой (II) представляет собой ординарную или двойную связь; Ra представляет собой -O-Z-Rc, где Z представляет собой ординарную связь или необязательно замещенный алкилен, и Rc представляет собой циклоалкил, гетероциклоалкил, арил или гетероарил, необязательно замещенные; Rb представляет собой Н или F; причем, если Rb представляет собой Н, тогда Rc не представляет собой циклоалкил, когда Z представляет собой ординарную связь, и Rc не представляет собой гетероциклоалкил, когда Z представляет собой алкилен; Х представляет собой S, SO или SO; А представляет собой NH или S; W представляет собой Н, алкил, циклоалкил или COR, где R представляет собой циклоалкил, алкил, алкоксил, O-фенил, -О-(СН2)n-фенил, где n=1-4; или NR1R2, где R1 представляет собой Н или alk, и R2 представляет собой Н, циклоалкил или алкил; или же R1, R2 вместе с N образуют цикл, необязательно включающий О, S, N и/или NH; где все эти радикалы являются необязательно замещенными; причем эти продукты находятся во всех изомерных формах и в виде солей, в качестве лекарственных средств, в частности, в качестве ингибиторов MET.The present invention relates to new products of formula (I), in which (II) is an ordinary or double bond; Ra is —O — Z — Rc, where Z is a single bond or optionally substituted alkylene, and Rc is cycloalkyl, heterocycloalkyl, aryl or heteroaryl, optionally substituted; Rb represents H or F; moreover, if Rb is H, then Rc is not cycloalkyl when Z is a single bond, and Rc is not heterocycloalkyl when Z is alkylene; X represents S, SO or SO; A represents NH or S; W represents H, alkyl, cycloalkyl or COR, where R represents cycloalkyl, alkyl, alkoxyl, O-phenyl, —O- (CH2) n-phenyl, where n = 1-4; or NR1R2, where R1 is H or alk, and R2 is H, cycloalkyl or alkyl; or R1, R2 together with N form a cycle optionally including O, S, N and / or NH; where all of these radicals are optionally substituted; moreover, these products are in all isomeric forms and in the form of salts, as medicines, in particular, as MET inhibitors.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR0900512A FR2941950B1 (en) | 2009-02-06 | 2009-02-06 | 6- (6-O-SUBSTITUTED-TRIAZOLOPYRIDAZINE-SULFANYL) BENZOTHIAZOLES AND BENZIMIDAZOLES DERIVATIVES: PREPARATION, APPLICATION AS MEDICAMENTS AND USE AS INHIBITORS OF MET. |
| PCT/FR2010/050178 WO2010089507A1 (en) | 2009-02-06 | 2010-02-04 | Derivatives of 6-(6-o-substituted-triazolopyridazine-sulfanyl) benzothiazoles and benzimidazoles, preparation thereof, use thereof as drugs, and use thereof as met inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| EA201171011A1 true EA201171011A1 (en) | 2012-03-30 |
Family
ID=40872767
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201171011A EA201171011A1 (en) | 2009-02-06 | 2010-02-04 | DERIVATIVES OF 6- (6-O-SUBSTITUTED TRIAZOLOPIRIDAZINSULFANIL) BENZOTIAZOLES AND -BENZIMIDAZOLES: OBTAINING, APPLICATION AS MEDICINE AND USING AS INHIBITORS |
Country Status (19)
| Country | Link |
|---|---|
| EP (1) | EP2393791A1 (en) |
| JP (1) | JP2012517408A (en) |
| KR (1) | KR20110132560A (en) |
| CN (1) | CN102378759A (en) |
| AR (1) | AR075249A1 (en) |
| AU (1) | AU2010212232A1 (en) |
| BR (1) | BRPI1008232A2 (en) |
| CA (1) | CA2750875A1 (en) |
| CL (1) | CL2011001879A1 (en) |
| CO (1) | CO6400223A2 (en) |
| EA (1) | EA201171011A1 (en) |
| FR (1) | FR2941950B1 (en) |
| IL (1) | IL214406A0 (en) |
| MA (1) | MA33107B1 (en) |
| MX (1) | MX2011008319A (en) |
| SG (1) | SG173559A1 (en) |
| TW (1) | TW201031670A (en) |
| UY (1) | UY32420A (en) |
| WO (1) | WO2010089507A1 (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2677698C1 (en) * | 2013-12-09 | 2019-01-21 | Юсб Байофарма Спрл | Triazolopyridazine derivatives as modulators of tnf activity |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2755976B1 (en) | 2011-09-15 | 2018-07-18 | Novartis AG | 6-substituted 3-(quinolin-6-ylthio)-[1,2,4]triazolo[4,3-a]pyridines as c-met tyrosine kinase inhibitors |
| CN104024259B (en) * | 2011-09-27 | 2017-09-26 | 基恩菲特公司 | It is used as the triazolopyridazine derivates of 6 substitutions of Rev Erb activators |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1298125A1 (en) | 2001-09-26 | 2003-04-02 | Aventis Pharma S.A. | Substituted benzimidazole compounds and their use for the treatment of cancer |
| AU2006320580B2 (en) * | 2005-11-30 | 2011-06-23 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-Met and uses thereof |
| MX2008008277A (en) * | 2005-12-21 | 2009-03-04 | Janssen Pharmaceutica Nv | Triazolopyridazines as tyrosine kinase modulators. |
| EP2032578A2 (en) * | 2006-05-30 | 2009-03-11 | Pfizer Products Incorporated | Triazolopyridazine derivatives |
| PE20121506A1 (en) * | 2006-07-14 | 2012-11-26 | Amgen Inc | TRIAZOLOPYRIDINE COMPOUNDS AS C-MET INHIBITORS |
| KR20090071612A (en) * | 2006-10-23 | 2009-07-01 | 에스지엑스 파마슈티컬스, 인코포레이티드 | Bicyclic triazoles as protein kinase modulators |
| PA8792501A1 (en) * | 2007-08-09 | 2009-04-23 | Sanofi Aventis | NEW DERIVATIVES OF 6-TRIAZOLOPIRIDACINA-SULFANIL BENZOTIAZOL AND BENCIMIDAZOL, ITS PREPARATION PROCEDURE, ITS APPLICATION AS MEDICATIONS, PHARMACEUTICAL COMPOSITIONS AND NEW MAIN USE AS MET INHIBITORS. |
-
2009
- 2009-02-06 FR FR0900512A patent/FR2941950B1/en not_active Expired - Fee Related
-
2010
- 2010-02-04 WO PCT/FR2010/050178 patent/WO2010089507A1/en active Application Filing
- 2010-02-04 AU AU2010212232A patent/AU2010212232A1/en not_active Abandoned
- 2010-02-04 CA CA2750875A patent/CA2750875A1/en not_active Abandoned
- 2010-02-04 SG SG2011056488A patent/SG173559A1/en unknown
- 2010-02-04 BR BRPI1008232A patent/BRPI1008232A2/en not_active IP Right Cessation
- 2010-02-04 JP JP2011548751A patent/JP2012517408A/en not_active Withdrawn
- 2010-02-04 EA EA201171011A patent/EA201171011A1/en unknown
- 2010-02-04 EP EP10708278A patent/EP2393791A1/en not_active Withdrawn
- 2010-02-04 MA MA34152A patent/MA33107B1/en unknown
- 2010-02-04 KR KR1020117020677A patent/KR20110132560A/en not_active Application Discontinuation
- 2010-02-04 MX MX2011008319A patent/MX2011008319A/en not_active Application Discontinuation
- 2010-02-04 CN CN2010800155375A patent/CN102378759A/en active Pending
- 2010-02-05 UY UY0001032420A patent/UY32420A/en not_active Application Discontinuation
- 2010-02-05 AR ARP100100317A patent/AR075249A1/en unknown
- 2010-02-05 TW TW099103579A patent/TW201031670A/en unknown
-
2011
- 2011-08-02 IL IL214406A patent/IL214406A0/en unknown
- 2011-08-04 CL CL2011001879A patent/CL2011001879A1/en unknown
- 2011-08-05 CO CO11099127A patent/CO6400223A2/en not_active Application Discontinuation
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2677698C1 (en) * | 2013-12-09 | 2019-01-21 | Юсб Байофарма Спрл | Triazolopyridazine derivatives as modulators of tnf activity |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2010212232A1 (en) | 2011-08-25 |
| FR2941950B1 (en) | 2011-04-01 |
| CN102378759A (en) | 2012-03-14 |
| AR075249A1 (en) | 2011-03-16 |
| CL2011001879A1 (en) | 2012-01-06 |
| KR20110132560A (en) | 2011-12-08 |
| EP2393791A1 (en) | 2011-12-14 |
| JP2012517408A (en) | 2012-08-02 |
| CA2750875A1 (en) | 2010-08-12 |
| IL214406A0 (en) | 2011-09-27 |
| MA33107B1 (en) | 2012-03-01 |
| UY32420A (en) | 2010-09-30 |
| FR2941950A1 (en) | 2010-08-13 |
| SG173559A1 (en) | 2011-09-29 |
| BRPI1008232A2 (en) | 2016-03-08 |
| MX2011008319A (en) | 2012-01-25 |
| CO6400223A2 (en) | 2012-03-15 |
| WO2010089507A1 (en) | 2010-08-12 |
| TW201031670A (en) | 2010-09-01 |
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