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WO2004108068A3 - 4-[4-(4-morpholino)anilino]pyrimidine derivatives, method for preparing thereof and antiviral pharmaceutical composition comprising the same - Google Patents

4-[4-(4-morpholino)anilino]pyrimidine derivatives, method for preparing thereof and antiviral pharmaceutical composition comprising the same Download PDF

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Publication number
WO2004108068A3
WO2004108068A3 PCT/KR2004/001297 KR2004001297W WO2004108068A3 WO 2004108068 A3 WO2004108068 A3 WO 2004108068A3 KR 2004001297 W KR2004001297 W KR 2004001297W WO 2004108068 A3 WO2004108068 A3 WO 2004108068A3
Authority
WO
WIPO (PCT)
Prior art keywords
straight
group
branched
branched alkyl
alkyl group
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/KR2004/001297
Other languages
French (fr)
Other versions
WO2004108068A2 (en
Inventor
Jong-Woo Kim
Sang-Wook Lee
Geun-Hyung Lee
Jae-Jin Han
Sang-Jin Park
Eul-Yong Park
Joong-Chul Shin
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
B&C Biopharm Co Ltd
Original Assignee
B&C Biopharm Co Ltd
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.)
Filing date
Publication date
Application filed by B&C Biopharm Co Ltd filed Critical B&C Biopharm Co Ltd
Publication of WO2004108068A2 publication Critical patent/WO2004108068A2/en
Publication of WO2004108068A3 publication Critical patent/WO2004108068A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The present invention relates to 4-[4-(4-morpholino)anilino]pyrimidine derivatives useful as an antiviral agent, and more particularly novel 4-[4-(4-morpholino)anilino]pyrimidine derivatives having an excellent inhibitory effect on replication of Hepatitis C virus (HCV), represented by the following formula I: in which R1 represents C1-C4 straight or branched alkoxy group, -NR2R3 group or 4-(R4)-piperazin-l-yl group; R2 represents hydrogen or C1-C4 straight or branched alkyl group; R3 represents C1-C4 straight or branched alkyl group, C1-C4 straight or branched hydroxyalkyl group, C1-C4 straight or branched alkyl group substituted by C2-C6 straight or branched dialkylamino group or C1-C4 straight or branched alkyl group substituted by heterocyclic ring; R4 represents C1-C4 straight or branched alkoxycarbonylmethyl group, carboxymethyl group or -CH2-CO-NH-R5 group; and R5 represents C1-C4 straight or branched alkyl group, C1-C4 straight or branched hydroxyalkyl group, C3-C6 cycloalkyl group or C1-C4 straight or branched alkyl group substituted by heterocyclic ring; and pharmaceutically acceptable salts thereof, a preparation method thereof, and an antiviral pharmaceutical composition comprising the compound as an effective component. The 4-[4-(4-morpholino)anilino]pyrimidine derivatives according to the present invention have an excellent inhibitory effect on replication of Hepatitis C virus (HCV) and thus can be advantageously used as a therapeutic or prophylactic agent of hepatitis C.
PCT/KR2004/001297 2003-06-04 2004-06-01 4-[4-(4-morpholino)anilino]pyrimidine derivatives, method for preparing thereof and antiviral pharmaceutical composition comprising the same Ceased WO2004108068A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR10-2003-0036072A KR100502395B1 (en) 2003-06-04 2003-06-04 4-[4-(4-Morpholino)anilino]pyrimidine derivatives, method for preparing thereof and antiviral pharmaceutical composition comprising the same
KR10-2003-0036072 2003-06-04

Publications (2)

Publication Number Publication Date
WO2004108068A2 WO2004108068A2 (en) 2004-12-16
WO2004108068A3 true WO2004108068A3 (en) 2005-02-17

Family

ID=33509609

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2004/001297 Ceased WO2004108068A2 (en) 2003-06-04 2004-06-01 4-[4-(4-morpholino)anilino]pyrimidine derivatives, method for preparing thereof and antiviral pharmaceutical composition comprising the same

Country Status (2)

Country Link
KR (1) KR100502395B1 (en)
WO (1) WO2004108068A2 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100700676B1 (en) 2005-06-24 2007-03-28 (주) 비엔씨바이오팜 6- (4-substituted-anilino) pyrimidine derivatives, preparation method thereof and pharmaceutical composition for antiviral comprising the same
JP2010526143A (en) 2007-05-04 2010-07-29 バーテックス ファーマシューティカルズ インコーポレイテッド Combination therapy for the treatment of HCV infection

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6200977B1 (en) * 1998-02-17 2001-03-13 Tularik Inc. Pyrimidine derivatives
US6306860B1 (en) * 1998-05-13 2001-10-23 Dong Wha Pharm. Inc. Co., Ltd. 2,5-pyridinedicarboxylic acid derivatives
US6410726B1 (en) * 2000-01-12 2002-06-25 Tularik Inc. Arylsulfonic acid salts of pyrimidine-based antiviral
US6436943B1 (en) * 1998-04-18 2002-08-20 Bayer Aktiengesellschaft Use of dihydropyrimidines as medicaments, and novel substances

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6200977B1 (en) * 1998-02-17 2001-03-13 Tularik Inc. Pyrimidine derivatives
US6436943B1 (en) * 1998-04-18 2002-08-20 Bayer Aktiengesellschaft Use of dihydropyrimidines as medicaments, and novel substances
US6306860B1 (en) * 1998-05-13 2001-10-23 Dong Wha Pharm. Inc. Co., Ltd. 2,5-pyridinedicarboxylic acid derivatives
US6410726B1 (en) * 2000-01-12 2002-06-25 Tularik Inc. Arylsulfonic acid salts of pyrimidine-based antiviral

Also Published As

Publication number Publication date
KR20040104823A (en) 2004-12-13
WO2004108068A2 (en) 2004-12-16
KR100502395B1 (en) 2005-07-19

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