RU2007130558A - Производные аминофенола в качестве селективных модуляторов андрогеновых рецепторов - Google Patents
Производные аминофенола в качестве селективных модуляторов андрогеновых рецепторов Download PDFInfo
- Publication number
- RU2007130558A RU2007130558A RU2007130558/04A RU2007130558A RU2007130558A RU 2007130558 A RU2007130558 A RU 2007130558A RU 2007130558/04 A RU2007130558/04 A RU 2007130558/04A RU 2007130558 A RU2007130558 A RU 2007130558A RU 2007130558 A RU2007130558 A RU 2007130558A
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- RU
- Russia
- Prior art keywords
- compound according
- azabicyclo
- endo
- group
- substituted
- Prior art date
Links
- CDAWCLOXVUBKRW-UHFFFAOYSA-N 2-aminophenol Chemical class NC1=CC=CC=C1O CDAWCLOXVUBKRW-UHFFFAOYSA-N 0.000 title 1
- 239000000849 selective androgen receptor modulator Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 29
- -1 cyano, hydroxy Chemical group 0.000 claims 16
- JFDZBHWFFUWGJE-UHFFFAOYSA-N benzonitrile Chemical compound N#CC1=CC=CC=C1 JFDZBHWFFUWGJE-UHFFFAOYSA-N 0.000 claims 10
- 239000003814 drug Substances 0.000 claims 9
- 229910052736 halogen Inorganic materials 0.000 claims 9
- 150000002367 halogens Chemical class 0.000 claims 9
- 229910052739 hydrogen Inorganic materials 0.000 claims 9
- 239000001257 hydrogen Substances 0.000 claims 9
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 7
- 238000004519 manufacturing process Methods 0.000 claims 7
- 208000024172 Cardiovascular disease Diseases 0.000 claims 6
- 206010060862 Prostate cancer Diseases 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 208000030159 metabolic disease Diseases 0.000 claims 6
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 5
- 125000003710 aryl alkyl group Chemical group 0.000 claims 5
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 5
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 5
- 210000003205 muscle Anatomy 0.000 claims 5
- 208000008589 Obesity Diseases 0.000 claims 4
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 4
- 229910005965 SO 2 Inorganic materials 0.000 claims 4
- MUMGGOZAMZWBJJ-DYKIIFRCSA-N Testostosterone Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 MUMGGOZAMZWBJJ-DYKIIFRCSA-N 0.000 claims 4
- 230000037182 bone density Effects 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 230000003247 decreasing effect Effects 0.000 claims 4
- 235000020824 obesity Nutrition 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 230000001568 sexual effect Effects 0.000 claims 4
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 4
- 125000000547 substituted alkyl group Chemical group 0.000 claims 4
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 4
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 4
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 4
- 208000005494 xerophthalmia Diseases 0.000 claims 4
- 208000019022 Mood disease Diseases 0.000 claims 3
- 125000003342 alkenyl group Chemical group 0.000 claims 3
- 125000000304 alkynyl group Chemical group 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 208000015122 neurodegenerative disease Diseases 0.000 claims 3
- 125000003107 substituted aryl group Chemical group 0.000 claims 3
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- 206010006895 Cachexia Diseases 0.000 claims 2
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 2
- 206010013883 Dwarfism Diseases 0.000 claims 2
- 208000032928 Dyslipidaemia Diseases 0.000 claims 2
- 208000004483 Dyspareunia Diseases 0.000 claims 2
- 201000009273 Endometriosis Diseases 0.000 claims 2
- 208000010228 Erectile Dysfunction Diseases 0.000 claims 2
- 206010053759 Growth retardation Diseases 0.000 claims 2
- 206010020772 Hypertension Diseases 0.000 claims 2
- 206010058359 Hypogonadism Diseases 0.000 claims 2
- 208000030663 Libido disease Diseases 0.000 claims 2
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 2
- 208000007466 Male Infertility Diseases 0.000 claims 2
- 208000002720 Malnutrition Diseases 0.000 claims 2
- 208000006262 Psychological Sexual Dysfunctions Diseases 0.000 claims 2
- 206010039966 Senile dementia Diseases 0.000 claims 2
- 102000001307 androgen receptors Human genes 0.000 claims 2
- 108010080146 androgen receptors Proteins 0.000 claims 2
- 208000007502 anemia Diseases 0.000 claims 2
- 230000037007 arousal Effects 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- 239000000460 chlorine Substances 0.000 claims 2
- 230000003920 cognitive function Effects 0.000 claims 2
- 208000029078 coronary artery disease Diseases 0.000 claims 2
- 230000006735 deficit Effects 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 231100000001 growth retardation Toxicity 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 238000002657 hormone replacement therapy Methods 0.000 claims 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 2
- 230000001771 impaired effect Effects 0.000 claims 2
- 201000001881 impotence Diseases 0.000 claims 2
- 230000001071 malnutrition Effects 0.000 claims 2
- 235000000824 malnutrition Nutrition 0.000 claims 2
- 230000002107 myocardial effect Effects 0.000 claims 2
- KIWSYRHAAPLJFJ-DNZSEPECSA-N n-[(e,2z)-4-ethyl-2-hydroxyimino-5-nitrohex-3-enyl]pyridine-3-carboxamide Chemical compound [O-][N+](=O)C(C)C(/CC)=C/C(=N/O)/CNC(=O)C1=CC=CN=C1 KIWSYRHAAPLJFJ-DNZSEPECSA-N 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 208000015380 nutritional deficiency disease Diseases 0.000 claims 2
- 230000008447 perception Effects 0.000 claims 2
- 230000010412 perfusion Effects 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 208000001076 sarcopenia Diseases 0.000 claims 2
- 201000000980 schizophrenia Diseases 0.000 claims 2
- 230000021595 spermatogenesis Effects 0.000 claims 2
- 230000004083 survival effect Effects 0.000 claims 2
- 229960003604 testosterone Drugs 0.000 claims 2
- 206010046947 vaginismus Diseases 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 208000017194 Affective disease Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims 1
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 1
- 206010022998 Irritability Diseases 0.000 claims 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 1
- 241000699670 Mus sp. Species 0.000 claims 1
- 206010028289 Muscle atrophy Diseases 0.000 claims 1
- 206010068871 Myotonic dystrophy Diseases 0.000 claims 1
- 206010029216 Nervousness Diseases 0.000 claims 1
- 229910019142 PO4 Inorganic materials 0.000 claims 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 1
- 125000004103 aminoalkyl group Chemical group 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 239000013043 chemical agent Substances 0.000 claims 1
- 230000003930 cognitive ability Effects 0.000 claims 1
- 230000001934 delay Effects 0.000 claims 1
- 230000002708 enhancing effect Effects 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 239000003862 glucocorticoid Substances 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 230000003054 hormonal effect Effects 0.000 claims 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 1
- 230000007794 irritation Effects 0.000 claims 1
- 206010025482 malaise Diseases 0.000 claims 1
- 201000000585 muscular atrophy Diseases 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 238000011474 orchiectomy Methods 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 1
- 239000010452 phosphate Substances 0.000 claims 1
- PTMHPRAIXMAOOB-UHFFFAOYSA-L phosphoramidate Chemical compound NP([O-])([O-])=O PTMHPRAIXMAOOB-UHFFFAOYSA-L 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 238000009256 replacement therapy Methods 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 230000035807 sensation Effects 0.000 claims 1
- 125000005415 substituted alkoxy group Chemical group 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
-
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- 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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- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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- 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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- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
- C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
- C07D451/06—Oxygen atoms
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hematology (AREA)
- Physical Education & Sports Medicine (AREA)
- Reproductive Health (AREA)
- Biomedical Technology (AREA)
- Heart & Thoracic Surgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Cardiology (AREA)
- Psychiatry (AREA)
- Obesity (AREA)
- Rheumatology (AREA)
- Gynecology & Obstetrics (AREA)
- Child & Adolescent Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Ophthalmology & Optometry (AREA)
- Pregnancy & Childbirth (AREA)
- Emergency Medicine (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US64284105P | 2005-01-10 | 2005-01-10 | |
| US60/642,841 | 2005-01-10 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2007130558A true RU2007130558A (ru) | 2009-02-20 |
Family
ID=36591321
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2007130558/04A RU2007130558A (ru) | 2005-01-10 | 2006-01-09 | Производные аминофенола в качестве селективных модуляторов андрогеновых рецепторов |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US7585877B2 (https=) |
| EP (1) | EP1836202B1 (https=) |
| JP (1) | JP5203712B2 (https=) |
| KR (1) | KR20070112775A (https=) |
| CN (1) | CN101119993B (https=) |
| AU (1) | AU2006205066B2 (https=) |
| CA (1) | CA2594340C (https=) |
| MX (1) | MX2007008334A (https=) |
| NZ (1) | NZ555974A (https=) |
| RU (1) | RU2007130558A (https=) |
| WO (1) | WO2006076317A2 (https=) |
| ZA (1) | ZA200705458B (https=) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070004679A1 (en) * | 2004-05-17 | 2007-01-04 | Nathalie Schlienger | Androgen receptor modulators and methods of treating disease using the same |
| US20060173037A1 (en) * | 2005-01-10 | 2006-08-03 | Nathalie Schlienger | Aminophenyl derivatives as selective androgen receptor modulators |
| NZ555974A (en) * | 2005-01-10 | 2010-11-26 | Acadia Pharm Inc | Aminophenyl derivatives as selective androgen receptor modulators |
| EP1911743B8 (en) * | 2005-08-01 | 2013-01-16 | Takeda Pharmaceutical Company Limited | Cyclic amine compound |
| UA92083C2 (ru) | 2006-05-19 | 2010-09-27 | Эбботт Леборетриз | Азабициклические алкановые производные, замещенные конденсированным бициклогетероциклом |
| CA2670976C (en) | 2006-11-30 | 2015-01-27 | Atsushi Hasuoka | Cyclic amine compound |
| PL2176220T3 (pl) | 2007-08-07 | 2013-08-30 | Takeda Pharmaceuticals Co | Pochodne pirolidyn-2-onu jako modulatory receptora androgenowego |
| ES2488990T3 (es) | 2008-02-22 | 2014-09-01 | Radius Health, Inc. | Moduladores selectivos del receptor de andrógenos |
| US8268872B2 (en) | 2008-02-22 | 2012-09-18 | Radius Health, Inc. | Selective androgen receptor modulators |
| MX338831B (es) | 2010-02-04 | 2016-05-03 | Radius Health Inc | Moduladores selectivos de receptores de androgenos. |
| EP2568806B1 (en) | 2010-05-12 | 2016-05-11 | Radius Health, Inc. | Therapeutic regimens |
| US8642632B2 (en) | 2010-07-02 | 2014-02-04 | Radius Health, Inc. | Selective androgen receptor modulators |
| US9133182B2 (en) | 2010-09-28 | 2015-09-15 | Radius Health, Inc. | Selective androgen receptor modulators |
| EP2736910B1 (en) * | 2011-07-27 | 2015-08-19 | Novartis AG | Pyrazoline derivatives and their use as selective androgen receptor modulators |
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- 2006-01-09 JP JP2007550547A patent/JP5203712B2/ja not_active Expired - Fee Related
- 2006-01-09 WO PCT/US2006/000733 patent/WO2006076317A2/en not_active Ceased
- 2006-01-09 US US11/329,267 patent/US7585877B2/en not_active Expired - Fee Related
- 2006-01-09 CN CN200680002003.2A patent/CN101119993B/zh not_active Expired - Fee Related
- 2006-01-09 RU RU2007130558/04A patent/RU2007130558A/ru not_active Application Discontinuation
- 2006-01-09 CA CA2594340A patent/CA2594340C/en not_active Expired - Fee Related
- 2006-01-09 AU AU2006205066A patent/AU2006205066B2/en not_active Ceased
- 2006-01-09 MX MX2007008334A patent/MX2007008334A/es not_active Application Discontinuation
- 2006-01-09 KR KR1020077018305A patent/KR20070112775A/ko not_active Withdrawn
- 2006-01-09 EP EP06733660.2A patent/EP1836202B1/en not_active Expired - Lifetime
- 2006-01-09 ZA ZA200705458A patent/ZA200705458B/xx unknown
-
2009
- 2009-06-30 US US12/495,514 patent/US20090270449A1/en not_active Abandoned
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| EP1836202B1 (en) | 2016-12-21 |
| WO2006076317A3 (en) | 2006-11-23 |
| US20090270449A1 (en) | 2009-10-29 |
| AU2006205066B2 (en) | 2012-05-17 |
| CA2594340A1 (en) | 2006-07-20 |
| CA2594340C (en) | 2015-11-10 |
| EP1836202A2 (en) | 2007-09-26 |
| ZA200705458B (en) | 2008-12-31 |
| WO2006076317A2 (en) | 2006-07-20 |
| CN101119993B (zh) | 2015-03-04 |
| NZ555974A (en) | 2010-11-26 |
| KR20070112775A (ko) | 2007-11-27 |
| AU2006205066A1 (en) | 2006-07-20 |
| JP2008526888A (ja) | 2008-07-24 |
| CN101119993A (zh) | 2008-02-06 |
| US20060160845A1 (en) | 2006-07-20 |
| US7585877B2 (en) | 2009-09-08 |
| WO2006076317A9 (en) | 2007-09-27 |
| JP5203712B2 (ja) | 2013-06-05 |
| MX2007008334A (es) | 2007-09-11 |
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