CN1159311C - 二氢嘧啶类化合物 - Google Patents

二氢嘧啶类化合物 Download PDF

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Publication number
CN1159311C
CN1159311C CNB998074950A CN99807495A CN1159311C CN 1159311 C CN1159311 C CN 1159311C CN B998074950 A CNB998074950 A CN B998074950A CN 99807495 A CN99807495 A CN 99807495A CN 1159311 C CN1159311 C CN 1159311C
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China
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compound
general formula
represent
group
formula
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Expired - Lifetime
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CNB998074950A
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English (en)
Chinese (zh)
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CN1305471A (zh
Inventor
J��˹�ж��ظ�˹
J·斯托尔特福斯
S·戈尔德曼
��Ĭ����
T·克雷默
K·-H·施莱默
U·尼维纳
A·佩森斯
E·格雷夫
S·洛特曼
K·德雷斯
O·纳贝尔
ض�
J·斯特尔廷
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Bayer Pharma AG
Bayer Intellectual Property GmbH
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Bayer AG
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/20—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D239/22—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to ring carbon 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/84—Nitriles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Saccharide Compounds (AREA)
CNB998074950A 1998-04-18 1999-04-07 二氢嘧啶类化合物 Expired - Lifetime CN1159311C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19817264A DE19817264A1 (de) 1998-04-18 1998-04-18 Neue Dihydropyrimidine
DE19817264.8 1998-04-18

Publications (2)

Publication Number Publication Date
CN1305471A CN1305471A (zh) 2001-07-25
CN1159311C true CN1159311C (zh) 2004-07-28

Family

ID=7864972

Family Applications (1)

Application Number Title Priority Date Filing Date
CNB998074950A Expired - Lifetime CN1159311C (zh) 1998-04-18 1999-04-07 二氢嘧啶类化合物

Country Status (36)

Country Link
US (3) US6696451B1 (OSRAM)
EP (1) EP1080086B1 (OSRAM)
JP (2) JP4590097B2 (OSRAM)
KR (1) KR100636771B1 (OSRAM)
CN (1) CN1159311C (OSRAM)
AR (1) AR018187A1 (OSRAM)
AT (1) ATE223401T1 (OSRAM)
AU (1) AU740318B2 (OSRAM)
BG (1) BG64649B1 (OSRAM)
BR (2) BR9909730B1 (OSRAM)
CA (1) CA2328780C (OSRAM)
CO (1) CO5021127A1 (OSRAM)
CU (1) CU23049A3 (OSRAM)
CZ (1) CZ293482B6 (OSRAM)
DE (2) DE19817264A1 (OSRAM)
DK (1) DK1080086T3 (OSRAM)
ES (1) ES2183548T3 (OSRAM)
GT (1) GT199900056A (OSRAM)
HU (1) HUP0102372A3 (OSRAM)
ID (1) ID27263A (OSRAM)
IL (2) IL138584A0 (OSRAM)
MY (1) MY126527A (OSRAM)
NO (2) NO321985B1 (OSRAM)
NZ (1) NZ507569A (OSRAM)
PE (1) PE20000427A1 (OSRAM)
PL (1) PL193898B1 (OSRAM)
PT (1) PT1080086E (OSRAM)
RU (1) RU2245881C9 (OSRAM)
SI (1) SI1080086T1 (OSRAM)
SK (1) SK286407B6 (OSRAM)
SV (1) SV1999000047A (OSRAM)
TR (1) TR200003011T2 (OSRAM)
TW (1) TW548274B (OSRAM)
UA (1) UA63998C2 (OSRAM)
WO (1) WO1999054326A1 (OSRAM)
ZA (1) ZA200005136B (OSRAM)

Families Citing this family (43)

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AU4289100A (en) * 1999-03-25 2000-10-16 Bayer Aktiengesellschaft Dihydropyrimidines and their use in the treatment of hepatitis
AU5568400A (en) 1999-06-23 2001-01-09 Ajinomoto Co., Inc. Novel dihydropyrimidine derivatives
AU3009801A (en) * 1999-12-22 2001-07-03 Bayer Aktiengesellschaft Combinations of medicaments for treating viral diseases
DE10012823A1 (de) 2000-03-16 2001-09-20 Bayer Ag Arzneimittel gegen virale Erkrankungen
DE10013125A1 (de) * 2000-03-17 2001-09-20 Bayer Ag Arzneimittel gegen virale Erkrankungen
DE10013126A1 (de) * 2000-03-17 2001-09-20 Bayer Ag Arzneimittel gegen virale Erkrankungen
DE10125131A1 (de) 2001-05-23 2002-12-05 Bayer Ag Verfahren zur Spaltung des Methyl 4-(2-chlor-4-fluorphenyl)-2-(3,5-difluor-2-pyridinyl)-6-methyl-1,4-dihydro-5-pyrmidincarboxylat-Racemats
US20040092735A1 (en) * 2002-11-08 2004-05-13 Orchid Chemicals & Pharmaceuticals Limited Process for the preparation of cefuroxime sodium
CN101104617B (zh) 2006-07-10 2010-06-23 北京摩力克科技有限公司 二氢嘧啶类化合物及其用于制备治疗和预防病毒性疾病的药物的用途
CN101104604B (zh) 2006-07-10 2011-03-02 北京摩力克科技有限公司 光学纯二氢嘧啶类化合物及其用于制备治疗和预防病毒性疾病的药物的用途
RU2452733C2 (ru) * 2007-04-27 2012-06-10 Пэдью Фарма Л.П. Антагонисты trpv1 и их применение
AU2008265397C1 (en) 2007-06-18 2013-08-29 Sunshine Lake Pharma Co., Ltd. Bromo-phenyl substituted thiazolyl dihydropyrimidines
RU2493826C2 (ru) 2007-07-12 2013-09-27 Новартис Аг Пероральные фармацевтические растворы, содержащие телбивудин
US20130267517A1 (en) 2012-03-31 2013-10-10 Hoffmann-La Roche Inc. Novel 4-methyl-dihydropyrimidines for the treatment and prophylaxis of hepatitis b virus infection
MX2015002511A (es) 2012-08-24 2016-03-08 Sunshine Lake Pharma Co Ltd Compuestos de dihidropirimidina y su aplicacion en productos farmaceuticos.
EP2892893B2 (en) 2012-09-10 2019-10-16 F.Hoffmann-La Roche Ag 6-amino acid heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis b virus infection
CN103664899B (zh) * 2012-09-11 2017-06-16 广东东阳光药业有限公司 杂芳基取代的二氢嘧啶类化合物及其在药物中的应用
AU2013342164A1 (en) * 2012-11-09 2015-06-04 Assembly Biosciences, Inc. Alternative uses for HBV assembly effectors
BR102014028162A2 (pt) * 2013-11-12 2015-09-08 Dow Agrosciences Llc processo para fluoração de compostos
KR20160077050A (ko) 2013-11-19 2016-07-01 선샤인 레이크 파르마 컴퍼니 리미티드 다이하이드로피리미딘 화합물 및 이의 약제학적 용도
JP6382977B2 (ja) 2013-11-27 2018-08-29 サンシャイン・レイク・ファーマ・カンパニー・リミテッドＳｕｎｓｈｉｎｅ Ｌａｋｅ Ｐｈａｒｍａ Ｃｏ．，Ｌｔｄ． ジヒドロピリミジン誘導体およびその中間体の製造方法
JP2017512789A (ja) 2014-03-28 2017-05-25 サンシャイン・レイク・ファーマ・カンパニー・リミテッドＳｕｎｓｈｉｎｅ Ｌａｋｅ Ｐｈａｒｍａ Ｃｏ．，Ｌｔｄ． ジヒドロピリミジン化合物及び医薬におけるその適用
AU2015266481B2 (en) * 2014-05-30 2018-06-07 Qilu Pharmaceuticals Co., Ltd. Dihydropyrimido fused ring derivative as HBV inhibitor
CN105153164B (zh) * 2014-05-30 2018-10-30 齐鲁制药有限公司 作为hbv抑制剂的二氢嘧啶并环衍生物
EP3253751B1 (en) 2015-02-07 2020-12-09 Sunshine Lake Pharma Co., Ltd. Complexes and salts of dihydropyrimidine derivatives and their application in pharmaceuticals
WO2019001420A1 (en) * 2017-06-27 2019-01-03 Janssen Pharmaceutica Nv HETEROARYLDIHYDROPYRIMIDINE DERIVATIVES AND METHODS OF TREATING INFECTIONS WITH HEPATITIS B VIRUS
US10759774B2 (en) 2017-09-28 2020-09-01 The Curators Of The University Of Missouri Inhibitors of hepatitis B virus targeting capsid assembly
KR20200083552A (ko) 2017-11-02 2020-07-08 아이쿠리스 게엠베하 운트 코. 카게 B형 간염 바이러스 (hbv)에 활성인 신규 고활성 피라졸로-피페리딘 치환된 인돌-2-카르복스아미드
CN111448199A (zh) 2017-11-02 2020-07-24 艾库里斯有限及两合公司 具有抗乙型肝炎病毒(hbv)活性的新的高活性的氨基-噻唑取代的吲哚-2-甲酰胺
CA3097784A1 (en) * 2018-05-08 2019-11-14 Janssen Sciences Ireland Unlimited Company Dihydropyrimidine derivatives and uses thereof in the treatment of hbv infection or of hbv-induced diseases
US11053235B2 (en) 2018-08-09 2021-07-06 Janssen Sciences Ireland Unlimited Company Substituted 1,4-dihydropyrimidines for the treatment of HBV infection or HBV-induced diseases
AR116947A1 (es) 2018-11-02 2021-06-30 Aicuris Gmbh & Co Kg Derivados de urea 6,7-dihidro-4h-pirazolo[1,5-a]pirazinas-indol-2-carboxamidas activas contra el virus de la hepatitis b (vhb)
UY38437A (es) 2018-11-02 2020-05-29 Aicuris Gmbh & Co Kg Nuevas urea 6,7-dihidro-4h-pirazolo[1,5-a]pirazinas activas contra el virus de la hepatitis b (hbv)
AR116946A1 (es) 2018-11-02 2021-06-30 Aicuris Gmbh & Co Kg Derivados de urea 6,7-dihidro-4h-pirazolo[4,3-c]piridinas activas contra el virus de la hepatitis b (vhb)
UY38435A (es) 2018-11-02 2020-05-29 Aicuris Gmbh & Co Kg Nuevas urea 6,7-dihidro-4h-pirazol[1,5-a] pirazinas activas contra el virus de la hepatitis b (vhb)
US20220009945A1 (en) * 2018-11-02 2022-01-13 Aicuris Gmbh & Co. Kg Novel urea 6,7-dihydro-4h-thiazole[5,4-c]pyridines active against the hepatitis b virus (hbv)
AR117189A1 (es) 2018-11-02 2021-07-21 Aicuris Gmbh & Co Kg Derivados de 6,7-dihidro-4h-pirazolo[1,5-a]pirazin indol-2-carboxamidas activos contra el virus de la hepatitis b (vhb)
JP2022511819A (ja) 2018-12-20 2022-02-01 ヤンセン ファーマシューティカ エヌ．ベー． ヘテロアリールジヒドロピリミジン誘導体及びｂ型肝炎感染症を治療する方法
MX2021013105A (es) 2019-04-30 2021-11-17 Aicuris Gmbh & Co Kg Nuevas oxalil piperazinas activas contra el virus de la hepatitis b (vhb).
SG11202111236UA (en) 2019-04-30 2021-11-29 Aicuris Gmbh & Co Kg Novel indole-2-carboxamides active against the hepatitis b virus (hbv)
US20220227789A1 (en) 2019-04-30 2022-07-21 Aicuris Gmbh & Co. Kg Novel indolizine-2-carboxamides active against the hepatitis b virus (hbv)
PH12021552749A1 (en) 2019-04-30 2022-07-11 Aicuris Gmbh & Co Kg Novel phenyl and pyridyl ureas active against the hepatitis b virus (hbv)
WO2020255016A1 (en) 2019-06-18 2020-12-24 Janssen Sciences Ireland Unlimited Company Combination of hepatitis b virus (hbv) vaccines and dihydropyrimidine derivatives as capsid assembly modulators

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CU23049A3 (es) 2005-06-24
BR9909730B1 (pt) 2012-09-04
DE19817264A1 (de) 1999-10-21
SK15652000A3 (sk) 2001-04-09
ATE223401T1 (de) 2002-09-15
AR018187A1 (es) 2001-10-31
TW548274B (en) 2003-08-21
CZ293482B6 (cs) 2004-05-12
ID27263A (id) 2001-03-22
BR9909730A (pt) 2000-12-19
WO1999054326A8 (de) 1999-12-29
US20070117812A1 (en) 2007-05-24
ZA200005136B (en) 2001-03-02
CZ20003871A3 (cs) 2001-01-17
NO321985B1 (no) 2006-07-31
SK286407B6 (sk) 2008-09-05
MY126527A (en) 2006-10-31
NZ507569A (en) 2002-04-26
HUP0102372A3 (en) 2003-01-28
ES2183548T3 (es) 2003-03-16
JP4590097B2 (ja) 2010-12-01
BG104812A (en) 2001-06-29
CA2328780C (en) 2008-09-23
TR200003011T2 (tr) 2001-01-22
SI1080086T1 (en) 2003-02-28
PL193898B1 (pl) 2007-03-30
EP1080086A1 (de) 2001-03-07
US7514565B2 (en) 2009-04-07
NO20045259L (no) 2000-12-13
PL343481A1 (en) 2001-08-27
RU2245881C2 (ru) 2005-02-10
NO20005215L (no) 2000-12-13
KR20010042788A (ko) 2001-05-25
AU3813399A (en) 1999-11-08
BRPI9917862B8 (pt) 2021-05-25
UA63998C2 (uk) 2004-02-16
CN1305471A (zh) 2001-07-25
BG64649B1 (bg) 2005-10-31
JP2002512243A (ja) 2002-04-23
PT1080086E (pt) 2002-12-31
BRPI9917862A2 (OSRAM) 2010-12-07
DE59902573D1 (en) 2002-10-10
CA2328780A1 (en) 1999-10-28
AU740318B2 (en) 2001-11-01
DK1080086T3 (da) 2002-12-23
CO5021127A1 (es) 2001-03-27
BRPI9917862B1 (pt) 2013-05-07
EP1080086B1 (de) 2002-09-04
JP2010241837A (ja) 2010-10-28
US6696451B1 (en) 2004-02-24
PE20000427A1 (es) 2000-06-25
IL138584A0 (en) 2001-10-31
NO20005215D0 (no) 2000-10-17
WO1999054326A1 (de) 1999-10-28
SV1999000047A (es) 2000-06-23
JP5237332B2 (ja) 2013-07-17
KR100636771B1 (ko) 2006-10-23
GT199900056A (es) 2000-10-07
HUP0102372A2 (hu) 2001-12-28
IL138584A (en) 2006-09-05
US20040167135A1 (en) 2004-08-26
HK1039119A1 (en) 2002-04-12
RU2245881C9 (ru) 2006-02-10
NO329020B1 (no) 2010-07-26

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