AR045582A1 - Piridinas pirazinas y pirimidinas heteroarilo fusionadas como ligandos receptores de crf1 - Google Patents
Piridinas pirazinas y pirimidinas heteroarilo fusionadas como ligandos receptores de crf1Info
- Publication number
- AR045582A1 AR045582A1 ARP040103174A ARP040103174A AR045582A1 AR 045582 A1 AR045582 A1 AR 045582A1 AR P040103174 A ARP040103174 A AR P040103174A AR P040103174 A ARP040103174 A AR P040103174A AR 045582 A1 AR045582 A1 AR 045582A1
- Authority
- AR
- Argentina
- Prior art keywords
- optionally substituted
- rings
- mono
- ring
- alkyl
- Prior art date
Links
- 102100038018 Corticotropin-releasing factor receptor 1 Human genes 0.000 title 1
- 101000878678 Homo sapiens Corticotropin-releasing factor receptor 1 Proteins 0.000 title 1
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical compound C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 title 1
- 101000948733 Saccharomyces cerevisiae (strain ATCC 204508 / S288c) Probable phospholipid translocase non-catalytic subunit CRF1 Proteins 0.000 title 1
- 239000003446 ligand Substances 0.000 title 1
- 150000003230 pyrimidines Chemical class 0.000 title 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 12
- 229910052757 nitrogen Inorganic materials 0.000 abstract 10
- 125000001072 heteroaryl group Chemical class 0.000 abstract 8
- 229910052760 oxygen Inorganic materials 0.000 abstract 7
- 229910052717 sulfur Inorganic materials 0.000 abstract 6
- 125000005842 heteroatom Chemical group 0.000 abstract 5
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 150000002431 hydrogen Chemical group 0.000 abstract 5
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 150000002367 halogens Chemical group 0.000 abstract 4
- -1 tri-substituted, 1-naphthyl Chemical group 0.000 abstract 4
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 3
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 3
- 125000001188 haloalkyl group Chemical group 0.000 abstract 3
- 239000001301 oxygen Substances 0.000 abstract 3
- 125000005017 substituted alkenyl group Chemical group 0.000 abstract 3
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 3
- 125000004426 substituted alkynyl group Chemical group 0.000 abstract 3
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 3
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 2
- 125000004644 alkyl sulfinyl group Chemical group 0.000 abstract 2
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 2
- 125000004414 alkyl thio group Chemical group 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- 125000005415 substituted alkoxy group Chemical group 0.000 abstract 2
- 239000011593 sulfur Substances 0.000 abstract 2
- 125000001622 2-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C(*)C([H])=C([H])C2=C1[H] 0.000 abstract 1
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 208000030814 Eating disease Diseases 0.000 abstract 1
- 208000019454 Feeding and Eating disease Diseases 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 208000015114 central nervous system disease Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000005432 dialkylcarboxamide group Chemical group 0.000 abstract 1
- 235000014632 disordered eating Nutrition 0.000 abstract 1
- 230000002526 effect on cardiovascular system Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 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
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed 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
- A61K31/435—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
- A61K31/4353—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 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
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
-
- 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
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Child & Adolescent Psychology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Investigating Or Analysing Biological Materials (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Composiciones farmacéuticas que los comprenden y usos para el tratamiento de desórdenes del SNC, cardiovasculares y de la alimentación. Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable del mismo, en el cual: Ar se elige entre: fenilo que está mono-, di- o tri-sustituido, 1-naftilo y 2-naftilo, cada uno de los cuales está opcionalmente mono-, di- o tri-sustituido y heteroarilo opcionalmente mono-, di- o tri-sustituido, teniendo dicho heteroarilo de 1 a 3 anillos, 5 a 7 miembros de anillo en cada anillo, y, por lo menos uno de dichos anillos, desde 1 hasta aproximadamente 3 heteroátomos seleccionados del grupo formado por N, O y S; R es oxígeno o está ausente; el grupo de fórmula (2), representa un sistema anular de 5 miembros saturado, insaturado o aromático que contiene 0 ó 1 heteroátomos, en el cual: Z1 es CR1, CR1R1', nitrógeno o NR1''; Z2 es nitrógeno, oxígeno, azufre, CR2, CR2R2' o NR2''; Z3 es nitrógeno, oxígeno, azufre, CR3, CR3R3' o NR3''; R1 se elige entre hidrógeno, halógeno, hidroxi, ciano, amino, alquilo opcionalmente sustituido, alquenilo opcionalmente sustituido, alquinilo opcionalmente sustituido, alcoxi opcionalmente sustituido, mono- o di-alquilamino opcionalmente sustituido, cicloalquilo opcionalmente sustituido, (cicloalquil)alquilo opcionalmente sustituido, alquiltio opcionalmente sustituido, alquilsulfinilo opcionalmente sustituido, alquilsulfonilo opcionalmente sustituido, mono- o dialquilcarboxamida opcionalmente sustituida, arilo carbocíclico opcionalmente sustituido y heteroarilo opcionalmente sustituido, teniendo dicho heteroarilo opcionalmente sustituido de 1 a 3 anillos, 5 a 7 miembros de anillo en cada anillo y, en por lo menos uno de dichos anillos, desde 1 hasta aproximadamente 3 heteroátomos seleccionados del grupo formado por N, O y S; R1'' se elige entre alquilo opcionalmente sustituido, alquenilo opcionalmente sustituido, alquinilo opcionalmente sustituido, (cicloalquil)alquilo opcionalmente sustituido y arilo carbocíclico opcionalmente sustituido y heteroarilo opcionalmente sustituido, teniendo dicho heteroarilo opcionalmente sustituido de 1 a 3 anillos, 5 a 7 miembros de anillo en cada anillo y, en por lo menos uno de dichos anillos, desde 1 hasta aproximadamente 3 heteroátomos seleccionados del grupo formado por N, O y S; R2 y R3 se eligen independientemente entre hidrógeno, halógeno, hidroxi, amino, ciano, nitro, alquilo, haloalquilo, alcoxi, aminoalquilo y mono- y di-alquilamino; R1', R2' y R3' se eligen independientemente entre hidrógeno, halógeno, alquilo, haloalquilo y aminoalquilo; R2'' y R3'' se eligen independientemente entre hidrógeno, alquilo, haloalquilo y aminoalquilo; Z4 es nitrógeno o CR4; Z5 es nitrógeno o CR5; donde Z4 y Z5 no son ambos nitrógeno; y R4 y R5 se eligen independientemente entre hidrógeno, halógeno, hidroxi, amino, ciano, nitro, alquilo opcionalmente sustituido, alquenilo opcionalmente sustituido, alquinilo opcionalmente sustituido, alcoxi opcionalmente sustituido, mono- o di-alquilamino opcionalmente sustituido, (cicloalquil)alquilo opcionalmente sustituido, alquiltio opcionalmente sustituido, alquilsulfinilo opcionalmente sustituido, alquilsulfonilo opcionalmente sustituido, mono- o di-alquilcarboxamida opcionalmente sustituida, arilo carbocíclico opcionalmente sustituido y heteroarilo opcionalmente sustituido, teniendo donde dicho heteroarilo opcionalmente sustituido de 1 a 3 anillos, 5 a 7 miembros de anillo en cada anillo y, en por lo menos uno de dichos anillos, desde 1 hasta aproximadamente 3 heteroátomos seleccionados del grupo formado por N, O y S.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US50041403P | 2003-09-05 | 2003-09-05 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR045582A1 true AR045582A1 (es) | 2005-11-02 |
Family
ID=34272952
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040103174A AR045582A1 (es) | 2003-09-05 | 2004-09-03 | Piridinas pirazinas y pirimidinas heteroarilo fusionadas como ligandos receptores de crf1 |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US20050113379A1 (es) |
| EP (1) | EP1680424A2 (es) |
| JP (1) | JP2007504271A (es) |
| KR (1) | KR20060088534A (es) |
| CN (1) | CN1878773A (es) |
| AP (1) | AP2006003559A0 (es) |
| AR (1) | AR045582A1 (es) |
| AU (1) | AU2004270713A1 (es) |
| BR (1) | BRPI0414087A (es) |
| CA (1) | CA2537829A1 (es) |
| CR (1) | CR8274A (es) |
| EA (1) | EA200600372A1 (es) |
| EC (1) | ECSP066408A (es) |
| IL (1) | IL174084A0 (es) |
| MA (1) | MA28086A1 (es) |
| NO (1) | NO20061180L (es) |
| TW (1) | TW200530232A (es) |
| WO (1) | WO2005023806A2 (es) |
| ZA (1) | ZA200601978B (es) |
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| WO2006133261A2 (en) | 2005-06-06 | 2006-12-14 | Intra-Cellular Therapies, Inc. | Organic compounds |
| CN101243090A (zh) * | 2005-08-25 | 2008-08-13 | 霍夫曼-拉罗奇有限公司 | p38 MAP激酶抑制剂及使用它的方法 |
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| US7977359B2 (en) | 2005-11-04 | 2011-07-12 | Amira Pharmaceuticals, Inc. | 5-lipdxygenase-activating protein (FLAP) inhibitors |
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| EP3331876B1 (en) | 2015-08-05 | 2020-10-07 | Vitae Pharmaceuticals, LLC | Modulators of ror-gamma |
| JP6914257B2 (ja) | 2015-11-20 | 2021-08-04 | ヴァイティー ファーマシューティカルズ，エルエルシー | Ｒｏｒ−ガンマのモジュレーター |
| TW202220968A (zh) | 2016-01-29 | 2022-06-01 | 美商維它藥物有限責任公司 | ＲＯＲ－γ調節劑 |
| US10682354B2 (en) | 2016-03-28 | 2020-06-16 | Intra-Cellular Therapies, Inc. | Compositions and methods |
| US9481674B1 (en) | 2016-06-10 | 2016-11-01 | Vitae Pharmaceuticals, Inc. | Dihydropyrrolopyridine inhibitors of ROR-gamma |
| US11077108B2 (en) | 2016-09-07 | 2021-08-03 | The Regents Of The University Of California | Allosteric corticotropin-releasing factor receptor 1 (CRFR1) antagonists that decrease p-tau and improve cognition |
| US11291666B2 (en) | 2016-09-12 | 2022-04-05 | Intra-Cellular Therapies, Inc. | Uses |
| WO2019018975A1 (en) | 2017-07-24 | 2019-01-31 | Vitae Pharmaceuticals, Inc. | INHIBITORS OF ROR GAMMA |
| WO2019023207A1 (en) | 2017-07-24 | 2019-01-31 | Vitae Pharmaceuticals, Inc. | Inhibitors of rorϒ |
| EP3746081A4 (en) | 2018-01-31 | 2021-10-27 | Intra-Cellular Therapies, Inc. | Novel uses |
| CN110437846B (zh) * | 2019-08-30 | 2022-02-25 | 陕西师范大学 | 含炔键的氟取代苯并噁唑液晶化合物及其制备方法 |
| US12410175B2 (en) | 2019-09-03 | 2025-09-09 | Intra-Cellular Therapies, Inc. | Compounds |
| PH12022551623A1 (en) | 2020-01-13 | 2023-11-29 | Verge Analytics Inc | Substituted pyrazolo-pyrimidines and uses thereof |
| US12364695B2 (en) | 2020-06-02 | 2025-07-22 | Intra-Cellular Therapies, Inc. | Methods of treating inflammatory disease |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1142817A (zh) * | 1993-10-12 | 1997-02-12 | 杜邦麦克制药有限公司 | 1n-烷基-n-芳基嘧啶胺及其衍生物 |
| AU716993B2 (en) * | 1995-05-12 | 2000-03-16 | Neurogen Corporation | Novel deazapurine derivatives; a new class of CRF1 specific ligands |
| JP3964478B2 (ja) * | 1995-06-30 | 2007-08-22 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | ヘテロ環含有カルボン酸誘導体及びそれを含有する医薬 |
| JP3621706B2 (ja) * | 1996-08-28 | 2005-02-16 | ファイザー・インク | 置換された６，５―ヘテロ―二環式誘導体 |
| US6310063B1 (en) * | 1998-04-02 | 2001-10-30 | Neurogen Corporation | Aminoalkyl substituted pyrrolo [3,2-E]pyridine and pyrollo [2,3-b]pyrimidine derivatives: modulators of CRF1 receptors |
| WO2002000623A2 (en) * | 2000-06-26 | 2002-01-03 | Neurogen Corporation | Aryl fused substituted 4-oxy-pyridines |
| DE10229777A1 (de) * | 2002-07-03 | 2004-01-29 | Bayer Ag | Indolin-Phenylsulfonamid-Derivate |
| CN1809351A (zh) * | 2003-04-24 | 2006-07-26 | 麦克公司 | Akt活性抑制剂 |
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2004
- 2004-09-03 JP JP2006526210A patent/JP2007504271A/ja active Pending
- 2004-09-03 AP AP2006003559A patent/AP2006003559A0/xx unknown
- 2004-09-03 WO PCT/US2004/028899 patent/WO2005023806A2/en not_active Ceased
- 2004-09-03 AU AU2004270713A patent/AU2004270713A1/en not_active Abandoned
- 2004-09-03 EA EA200600372A patent/EA200600372A1/ru unknown
- 2004-09-03 EP EP04788585A patent/EP1680424A2/en not_active Withdrawn
- 2004-09-03 US US10/933,834 patent/US20050113379A1/en not_active Abandoned
- 2004-09-03 KR KR1020067004564A patent/KR20060088534A/ko not_active Withdrawn
- 2004-09-03 ZA ZA200601978A patent/ZA200601978B/en unknown
- 2004-09-03 AR ARP040103174A patent/AR045582A1/es unknown
- 2004-09-03 BR BRPI0414087-7A patent/BRPI0414087A/pt not_active IP Right Cessation
- 2004-09-03 CA CA002537829A patent/CA2537829A1/en not_active Abandoned
- 2004-09-03 CN CNA2004800327037A patent/CN1878773A/zh active Pending
- 2004-09-06 TW TW093126841A patent/TW200530232A/zh unknown
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2006
- 2006-03-02 IL IL174084A patent/IL174084A0/en unknown
- 2006-03-03 CR CR8274A patent/CR8274A/es unknown
- 2006-03-03 EC EC2006006408A patent/ECSP066408A/es unknown
- 2006-03-14 NO NO20061180A patent/NO20061180L/no not_active Application Discontinuation
- 2006-03-24 US US11/389,646 patent/US20060199823A1/en not_active Abandoned
- 2006-04-05 MA MA28916A patent/MA28086A1/fr unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP1680424A2 (en) | 2006-07-19 |
| JP2007504271A (ja) | 2007-03-01 |
| ECSP066408A (es) | 2006-09-18 |
| NO20061180L (no) | 2006-03-31 |
| IL174084A0 (en) | 2008-02-09 |
| TW200530232A (en) | 2005-09-16 |
| EA200600372A1 (ru) | 2006-08-25 |
| MA28086A1 (fr) | 2006-08-01 |
| US20050113379A1 (en) | 2005-05-26 |
| CN1878773A (zh) | 2006-12-13 |
| US20060199823A1 (en) | 2006-09-07 |
| WO2005023806A2 (en) | 2005-03-17 |
| ZA200601978B (en) | 2007-05-30 |
| BRPI0414087A (pt) | 2006-10-31 |
| AP2006003559A0 (en) | 2006-04-30 |
| CA2537829A1 (en) | 2005-03-17 |
| KR20060088534A (ko) | 2006-08-04 |
| WO2005023806A3 (en) | 2005-06-02 |
| CR8274A (es) | 2008-06-10 |
| AU2004270713A1 (en) | 2005-03-17 |
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