AR077054A1 - Derivados de benzimidazol utiles como moduladores del canal trpm8 - Google Patents
Derivados de benzimidazol utiles como moduladores del canal trpm8Info
- Publication number
- AR077054A1 AR077054A1 ARP100102052A ARP100102052A AR077054A1 AR 077054 A1 AR077054 A1 AR 077054A1 AR P100102052 A ARP100102052 A AR P100102052A AR P100102052 A ARP100102052 A AR P100102052A AR 077054 A1 AR077054 A1 AR 077054A1
- Authority
- AR
- Argentina
- Prior art keywords
- lower alkyl
- group
- heterocycloalkyl
- heteroaryl
- cycloalkyl
- Prior art date
Links
- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical class C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 title 1
- 102000003610 TRPM8 Human genes 0.000 title 1
- 101150111302 Trpm8 gene Proteins 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 25
- 125000003545 alkoxy group Chemical group 0.000 abstract 8
- 125000001072 heteroaryl group Chemical group 0.000 abstract 5
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 5
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 150000002367 halogens Chemical class 0.000 abstract 4
- 125000001424 substituent group Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000001721 carbon Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 150000002431 hydrogen Chemical group 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 150000002829 nitrogen Chemical class 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 208000011580 syndromic disease Diseases 0.000 abstract 1
Classifications
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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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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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
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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
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
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- A—HUMAN NECESSITIES
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- 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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- 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P13/10—Drugs for disorders of the urinary system of the bladder
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- A61P17/06—Antipsoriatics
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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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
- A61P3/08—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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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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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- 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
- A61P9/12—Antihypertensives
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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 to ring carbon atoms
- C07D233/44—Nitrogen atoms not forming part of a nitro radical
- C07D233/52—Nitrogen atoms not forming part of a nitro radical with hetero atoms directly attached to said nitrogen atoms
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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
- C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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
- C07D235/30—Nitrogen atoms not forming part of a nitro radical
-
- 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
- C07D498/06—Peri-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Dermatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Diabetes (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Urology & Nephrology (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Gynecology & Obstetrics (AREA)
- Otolaryngology (AREA)
- Obesity (AREA)
- Vascular Medicine (AREA)
- Hematology (AREA)
- Pregnancy & Childbirth (AREA)
- Ophthalmology & Optometry (AREA)
- Emergency Medicine (AREA)
- Pulmonology (AREA)
- Gastroenterology & Hepatology (AREA)
Abstract
Composiciones y métodos para tratar diferentes enfermedades, síndromes, afecciones y trastornos que incluyen el dolor. Reivindicacion 1: Un compuesto de la formula (1) en donde a es un numero entero de 0 a 3; cada R0 se selecciona independientemente del grupo que consiste de halogeno, hidroxi, ciano, alquilo inferior, alquilo inferior fluorado, alcoxi inferior y alcoxi inferior fluorado; R2 se selecciona del grupo que consiste de hidrogeno, halogeno, hidroxi, ciano, alquilo inferior, alquilo inferior fluorado, alcoxi inferior y alcoxi inferior fluorado; R1 se selecciona del grupo que consiste de alquilo, alquilo inferior sustituido con hidroxi, alquilo inferior halogenado, cicloalquilo-(alquilo inferior)- y fenilo-(alquilo inferior)-; alternativamente, R2 y R1 se toman juntos como en restos (2) o (3); R3 se selecciona del grupo que consiste de alquilo inferior, cicloalquilo, arilo, heteroarilo, heterocicloalquilo, cicloalquilo-(alquilo inferior)-, arilo-(alquilo inferior)-, heteroarilo-(alquilo inferior)- y heterocicloalquilo-(alquilo inferior)-; en donde el cicloalquilo, arilo, heteroarilo o heterocicloalquilo, ya sea solo o como parte de un grupo sustituyente se sustituye opcionalmente con uno o más sustituyentes independientemente seleccionados del grupo que consiste de halogeno, alquilo inferior, alquilo inferior halogenado, alcoxi inferior, alcoxi inferior halogenado, -C(O)OH, -C(O)O-(alquilo inferior) y -C(O)NRARB; en donde RA y RB se seleccionan independientemente del grupo que consiste de hidrogeno y alquilo inferior; alternativamente RA y RB se toman juntos con el átomo de nitrogeno al cual está unidos para formar una estructura de anillo que contiene nitrogeno saturado de 5 a 6 miembros; R4 se selecciona del grupo que consiste de alquilo inferior, cicloalquilo, arilo, heteroarilo, heterocicloalquilo, cicloalquilo-(alquilo inferior)-, arilo-(alquilo inferior)-, heteroarilo-(alquilo inferior)- y heterocicloalquilo-(alquilo inferior)-; en donde el cicloalquilo, arilo, heteroarilo o heterocicloalquilo, solo o como parte de un grupo sustituyente se sustituye opcionalmente con uno o más sustituyentes independientemente seleccionados del grupo que consiste de halogeno, alquilo inferior, alquilo inferior halogenado, alcoxi inferior, alcoxi inferior halogenado y -S-CF3; siempre y cuando R4 sea heteroarilo o heterocicloalquilo, entonces el grupo R4 está unido al N del compuesto de la formula (1) a través de un átomo de carbono; siempre y cuando a sea 0, R1 sea metilo, R2 sea hidrogeno y R4 sea metilo; entonces R3 es diferente de metilo, fenilo o 4-metilfenilo; o una sal farmacéuticamente aceptable de éste.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US18568109P | 2009-06-10 | 2009-06-10 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR077054A1 true AR077054A1 (es) | 2011-07-27 |
Family
ID=42357786
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100102052A AR077054A1 (es) | 2009-06-10 | 2010-06-10 | Derivados de benzimidazol utiles como moduladores del canal trpm8 |
Country Status (10)
| Country | Link |
|---|---|
| US (3) | US8450497B2 (es) |
| EP (1) | EP2440295B1 (es) |
| JP (1) | JP2012529536A (es) |
| CN (1) | CN102802730A (es) |
| AR (1) | AR077054A1 (es) |
| AU (1) | AU2010258713B2 (es) |
| CA (1) | CA2774883A1 (es) |
| RU (1) | RU2011154368A (es) |
| TW (1) | TW201105681A (es) |
| WO (1) | WO2010144679A1 (es) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014143768A1 (en) * | 2013-03-15 | 2014-09-18 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
| ES2635560T3 (es) | 2013-07-08 | 2017-10-04 | Incyte Holdings Corporation | Heterociclos tricíclicos como inhibidores de la proteína NET |
| US9399640B2 (en) | 2013-11-26 | 2016-07-26 | Incyte Corporation | Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors |
| WO2015081189A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| US9309246B2 (en) | 2013-12-19 | 2016-04-12 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| ES2942723T3 (es) | 2014-04-23 | 2023-06-06 | Incyte Holdings Corp | 1H-pirrolo[2,3-C]piridin-7(6H)-onas y pirazolo[3,4-C]piridin-7(6H)-onas como inhibidores de proteínas BET |
| ES2855225T3 (es) | 2014-09-15 | 2021-09-23 | Incyte Corp | Heterociclos tricíclicos para su uso como inhibidores de proteínas BET |
| WO2017075377A1 (en) | 2015-10-29 | 2017-05-04 | Incyte Corporation | Amorphous solid form of a bet protein inhibitor |
| KR20250163425A (ko) | 2016-06-20 | 2025-11-20 | 인사이트 코포레이션 | Bet 저해제의 결정질 고체 형태 |
| WO2018168898A1 (ja) * | 2017-03-15 | 2018-09-20 | 大日本住友製薬株式会社 | 新規ベンズイミダゾロン化合物およびその医薬用途 |
| WO2020038387A1 (zh) * | 2018-08-24 | 2020-02-27 | 杭州阿诺生物医药科技有限公司 | 高活性sting蛋白激动剂 |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6340681B1 (en) | 1999-07-16 | 2002-01-22 | Pfizer Inc | 2-benzimidazolylamine compounds as ORL-1-receptor agonists |
| KR20060087386A (ko) * | 2005-01-28 | 2006-08-02 | 주식회사 대웅제약 | 신규 벤조이미다졸 유도체 및 이를 함유하는 약제학적조성물 |
| US7803790B2 (en) * | 2005-05-09 | 2010-09-28 | Hydra Biosciences, Inc. | Compounds for modulating TRPV3 function |
| EP1983992A4 (en) | 2006-01-19 | 2010-08-18 | Abbott Lab | 2-IMINO-BENZIMIDAZOLES |
| WO2007134107A2 (en) | 2006-05-10 | 2007-11-22 | Janssen Pharmaceutica N.V. | Cold menthol receptor-1 antagonists |
| US20080287398A1 (en) * | 2007-05-02 | 2008-11-20 | Colburn Raymond W | Cold menthol receptor-1 antagonists |
| PA8790401A1 (es) * | 2007-07-18 | 2009-03-31 | Janssen Pharmaceutica Nv | Sulfonamidas como moduladores de trpm8 |
-
2010
- 2010-06-09 TW TW099118639A patent/TW201105681A/zh unknown
- 2010-06-10 WO PCT/US2010/038135 patent/WO2010144679A1/en not_active Ceased
- 2010-06-10 EP EP10724968.2A patent/EP2440295B1/en active Active
- 2010-06-10 RU RU2011154368/04A patent/RU2011154368A/ru not_active Application Discontinuation
- 2010-06-10 US US12/797,712 patent/US8450497B2/en not_active Expired - Fee Related
- 2010-06-10 AR ARP100102052A patent/AR077054A1/es unknown
- 2010-06-10 CA CA2774883A patent/CA2774883A1/en not_active Abandoned
- 2010-06-10 JP JP2012515129A patent/JP2012529536A/ja not_active Withdrawn
- 2010-06-10 CN CN2010800263539A patent/CN102802730A/zh active Pending
- 2010-06-10 AU AU2010258713A patent/AU2010258713B2/en not_active Ceased
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2013
- 2013-04-30 US US13/873,570 patent/US8981113B2/en active Active
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2015
- 2015-02-10 US US14/618,462 patent/US9636345B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| US20150150882A1 (en) | 2015-06-04 |
| US9636345B2 (en) | 2017-05-02 |
| JP2012529536A (ja) | 2012-11-22 |
| US20130245085A1 (en) | 2013-09-19 |
| EP2440295B1 (en) | 2013-07-24 |
| TW201105681A (en) | 2011-02-16 |
| AU2010258713A1 (en) | 2012-01-12 |
| US20110003800A1 (en) | 2011-01-06 |
| WO2010144679A1 (en) | 2010-12-16 |
| AU2010258713B2 (en) | 2014-12-04 |
| RU2011154368A (ru) | 2013-07-20 |
| EP2440295A1 (en) | 2012-04-18 |
| CN102802730A (zh) | 2012-11-28 |
| US8450497B2 (en) | 2013-05-28 |
| US8981113B2 (en) | 2015-03-17 |
| HK1169069A1 (en) | 2013-01-18 |
| CA2774883A1 (en) | 2010-12-16 |
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