ZA200301818B - Novel piperidine derivatives. - Google Patents

Novel piperidine derivatives. Download PDF

Info

Publication number: ZA200301818B
Authority: ZA; South Africa
Prior art keywords: methyl; amino; phenyl; alkyl; compounds according
Prior art date: 2000-09-08

Application number

ZA200301818A

Other languages

English (en)

Inventor

Jean Ackermann

Alexander Chucholowski

Olivier Morand

Thomas Weller

Johannes Aebi

Henrietta Dehmlow

Sabine Wallabaum

Original Assignee

Hoffmann La Roche

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

2000-09-08

Filing date

2003-03-05

Publication date

2004-06-21

2003-03-05 Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche

2004-06-21 Publication of ZA200301818B publication Critical patent/ZA200301818B/en

Links

150000003053 piperidines Chemical class 0.000 title description 2
150000001875 compounds Chemical class 0.000 claims description 80
-1 aryl- lower-alkyl Chemical group 0.000 claims description 32
238000011282 treatment Methods 0.000 claims description 16
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 13
229910052739 hydrogen Inorganic materials 0.000 claims description 13
239000001257 hydrogen Substances 0.000 claims description 13
238000011321 prophylaxis Methods 0.000 claims description 13
229910052801 chlorine Chemical group 0.000 claims description 12
239000000460 chlorine Chemical group 0.000 claims description 12
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 12
125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 12
ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical group [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims description 11
125000000753 cycloalkyl group Chemical group 0.000 claims description 10
150000002148 esters Chemical class 0.000 claims description 10
125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 10
229910052731 fluorine Inorganic materials 0.000 claims description 10
239000011737 fluorine Substances 0.000 claims description 10
125000001424 substituent group Chemical group 0.000 claims description 10
WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical group [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims description 9
239000002253 acid Substances 0.000 claims description 9
GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Chemical group BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims description 9
229910052794 bromium Inorganic materials 0.000 claims description 9
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 9
150000003839 salts Chemical class 0.000 claims description 9
239000000126 substance Substances 0.000 claims description 9
125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims description 7
125000003118 aryl group Chemical group 0.000 claims description 7
201000010099 disease Diseases 0.000 claims description 7
125000001072 heteroaryl group Chemical group 0.000 claims description 7
WSFSSNUMVMOOMR-BJUDXGSMSA-N methanone Chemical compound O=[11CH2] WSFSSNUMVMOOMR-BJUDXGSMSA-N 0.000 claims description 7
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206010012601 diabetes mellitus Diseases 0.000 claims description 6
239000003814 drug Substances 0.000 claims description 6
229910052736 halogen Inorganic materials 0.000 claims description 6
150000002367 halogens Chemical group 0.000 claims description 6
230000003463 hyperproliferative effect Effects 0.000 claims description 6
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 6
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125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 5
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230000036281 parasite infection Effects 0.000 claims description 5
125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims description 4
125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 4
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125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 4
238000002360 preparation method Methods 0.000 claims description 4
230000001225 therapeutic effect Effects 0.000 claims description 4
125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims description 3
125000004199 4-trifluoromethylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C(F)(F)F 0.000 claims description 3
125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims description 3
125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 3
125000001624 naphthyl group Chemical group 0.000 claims description 3
230000002265 prevention Effects 0.000 claims description 3
229910052717 sulfur Inorganic materials 0.000 claims description 3
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125000004800 4-bromophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Br 0.000 claims description 2
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PPBRXRYQALVLMV-UHFFFAOYSA-N Styrene Chemical group C=CC1=CC=CC=C1 PPBRXRYQALVLMV-UHFFFAOYSA-N 0.000 claims description 2
125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 2
125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 claims description 2
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239000013543 active substance Substances 0.000 claims 2
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Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
- C07D211/40—Oxygen atoms
- C07D211/44—Oxygen atoms attached in position 4
- C07D211/46—Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
- C07D211/40—Oxygen atoms
- C07D211/44—Oxygen atoms attached in position 4
- 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
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- A—HUMAN NECESSITIES
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- 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
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P31/10—Antimycotics
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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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- A—HUMAN NECESSITIES
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- 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
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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
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/20—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
- C07D211/22—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by oxygen atoms
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/26—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/92—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
- C07D211/96—Sulfur atom

Landscapes

Organic Chemistry (AREA)
Chemical & Material Sciences (AREA)
Health & Medical Sciences (AREA)
Veterinary Medicine (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Chemical Kinetics & Catalysis (AREA)
Pharmacology & Pharmacy (AREA)
Public Health (AREA)
General Chemical & Material Sciences (AREA)
General Health & Medical Sciences (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Diabetes (AREA)
Obesity (AREA)
Cardiology (AREA)
Heart & Thoracic Surgery (AREA)
Hematology (AREA)
Vascular Medicine (AREA)
Oncology (AREA)
Communicable Diseases (AREA)
Urology & Nephrology (AREA)
Tropical Medicine & Parasitology (AREA)
Emergency Medicine (AREA)
Endocrinology (AREA)
Gastroenterology & Hepatology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Hydrogenated Pyridines (AREA)
Plural Heterocyclic Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

ZA200301818A 2000-09-08 2003-03-05 Novel piperidine derivatives. ZA200301818B (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
EP00119677		2000-09-08

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ZA200301818B true ZA200301818B (en)	2004-06-21

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US (1)	US6964974B2 (de)
EP (1)	EP1317432B1 (de)
JP (1)	JP2004508354A (de)
KR (1)	KR20030027122A (de)
CN (1)	CN1231466C (de)
AR (1)	AR032634A1 (de)
AT (1)	ATE384047T1 (de)
AU (1)	AU2001285912A1 (de)
BR (1)	BR0113752A (de)
CA (1)	CA2419588C (de)
DE (1)	DE60132468T2 (de)
ES (1)	ES2298253T3 (de)
MX (1)	MXPA03002034A (de)
WO (1)	WO2002020483A1 (de)
ZA (1)	ZA200301818B (de)

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CZ2003451A3 (cs)	2000-08-16	2003-10-15	F. Hoffmann-La Roche Ag	Nové deriváty aminocyklohexanu
EP1458374A2 (de) *	2001-12-14	2004-09-22	Novo Nordisk A/S	Verbindungen und deren verwendung zur senkung der aktivität der hormon-abhängigen lipase
US7012077B2 (en) *	2001-12-20	2006-03-14	Hoffmann-La Roche Inc.	Substituted cyclohexane derivatives
US7906645B2 (en) *	2004-12-24	2011-03-15	Astrazeneca Ab	Heterocyclic compounds as ccr2b antagonists
US10143686B2 (en)	2010-12-27	2018-12-04	The Curators Of The University Of Missouri	Oxidosqualene cyclase as a protein target for anticancer therapeutics
CN104039326A (zh) *	2011-10-20	2014-09-10	密苏里大学学监	用于癌症治疗的酶抑制剂

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US3133061A (en)	1962-11-13	1964-05-12	Sterling Drug Inc	Piperidine carboxamides and derivatives thereof
US3914426A (en) *	1972-11-10	1975-10-21	Pfizer	Piperidinesulfonylurea derivatives for lowering blood sugar levels
SK94393A3 (en)	1992-09-11	1994-08-10	Thomae Gmbh Dr K	Cyclic derivatives of urea, process for their production and their pharmaceutical agents with the content of those
JPH08504194A (ja)	1992-12-01	1996-05-07	メルクエンドカンパニーインコーポレーテッド	フィブリノーゲンレセプターアンタゴニスト
FR2705343B1 (fr)	1993-05-17	1995-07-21	Fournier Ind & Sante	Dérivés de beta,beta-diméthyl-4-pipéridineéthanamine, leur procédé de préparation et leur utilisation en thérapeutique.
GB9310066D0 (en)	1993-05-17	1993-06-30	Zeneca Ltd	Alkyl substituted heterocycles
TW438774B (en)	1993-07-14	2001-06-07	Hoffmann La Roche	Pharmaceutical composition for lowering cholesterol containing phenalkylamines and certain novel phenalkylamines
MA23420A1 (fr)	1994-01-07	1995-10-01	Smithkline Beecham Corp	Antagonistes bicycliques de fibrinogene.
DE4407961A1 (de)	1994-03-10	1995-09-14	Thomae Gmbh Dr K	Imidazolidin-2-one, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
CA2190699A1 (en) *	1995-12-08	1997-06-09	Johannes Aebi	Tertiary amines
DE19614204A1 (de)	1996-04-10	1997-10-16	Thomae Gmbh Dr K	Carbonsäurederivate, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
DE19618970A1 (de)	1996-05-10	1997-11-13	Klinge Co Chem Pharm Fab	Neue Thiazolopyridine
US6025372A (en) *	1997-04-04	2000-02-15	Merck & Co., Inc.	Somatostatin agonists
NZ500354A (en) *	1997-04-14	2001-11-30	Cor Therapeutics Inc	Cyclic diaza compounds as selective factor Xa inhibitors for treating thrombotic related disorders
DE19806713A1 (de)	1998-02-18	1999-08-19	Boehringer Ingelheim Pharma	Neue Urethane, ihre Thio- und Dithioanaloga, deren Salze, diese Verbindungen enthaltende Arzneimittel und deren Verwendung sowie Verfahren zu ihrer Herstellung

2001
- 2001-08-27 US US09/939,872 patent/US6964974B2/en not_active Expired - Fee Related
- 2001-08-29 AT AT01965225T patent/ATE384047T1/de not_active IP Right Cessation
- 2001-08-29 JP JP2002525105A patent/JP2004508354A/ja active Pending
- 2001-08-29 CN CNB018169414A patent/CN1231466C/zh not_active Expired - Fee Related
- 2001-08-29 EP EP01965225A patent/EP1317432B1/de not_active Expired - Lifetime
- 2001-08-29 KR KR10-2003-7003436A patent/KR20030027122A/ko not_active Ceased
- 2001-08-29 BR BR0113752-2A patent/BR0113752A/pt not_active IP Right Cessation
- 2001-08-29 ES ES01965225T patent/ES2298253T3/es not_active Expired - Lifetime
- 2001-08-29 WO PCT/EP2001/009941 patent/WO2002020483A1/en not_active Ceased
- 2001-08-29 MX MXPA03002034A patent/MXPA03002034A/es unknown
- 2001-08-29 DE DE60132468T patent/DE60132468T2/de not_active Expired - Lifetime
- 2001-08-29 AU AU2001285912A patent/AU2001285912A1/en not_active Abandoned
- 2001-08-29 CA CA002419588A patent/CA2419588C/en not_active Expired - Fee Related
- 2001-09-06 AR ARP010104232A patent/AR032634A1/es not_active Application Discontinuation
2003
- 2003-03-05 ZA ZA200301818A patent/ZA200301818B/en unknown

Also Published As

Publication number	Publication date
CN1231466C (zh)	2005-12-14
AU2001285912A1 (en)	2002-03-22
DE60132468D1 (de)	2008-03-06
AR032634A1 (es)	2003-11-19
MXPA03002034A (es)	2003-07-24
US20020068753A1 (en)	2002-06-06
ATE384047T1 (de)	2008-02-15
JP2004508354A (ja)	2004-03-18
EP1317432B1 (de)	2008-01-16
BR0113752A (pt)	2003-07-29
US6964974B2 (en)	2005-11-15
CA2419588C (en)	2009-09-22
WO2002020483A1 (en)	2002-03-14
DE60132468T2 (de)	2009-01-15
WO2002020483A8 (en)	2002-06-06
EP1317432A1 (de)	2003-06-11
CA2419588A1 (en)	2002-03-14
KR20030027122A (ko)	2003-04-03
ES2298253T3 (es)	2008-05-16
CN1468220A (zh)	2004-01-14

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