JP2004520393A - ヘテロ環化号物の薬学的に許容可能な塩 - Google Patents
ヘテロ環化号物の薬学的に許容可能な塩 Download PDFInfo
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- JP2004520393A JP2004520393A JP2002563151A JP2002563151A JP2004520393A JP 2004520393 A JP2004520393 A JP 2004520393A JP 2002563151 A JP2002563151 A JP 2002563151A JP 2002563151 A JP2002563151 A JP 2002563151A JP 2004520393 A JP2004520393 A JP 2004520393A
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- Prior art keywords
- ethoxy
- phenyl
- oxo
- ethyl
- salt
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- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 210
- -1 monoalkylamino Chemical group 0.000 claims description 179
- 125000004943 pyrimidin-6-yl group Chemical group N1=CN=CC=C1* 0.000 claims description 149
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- 238000000034 method Methods 0.000 claims description 35
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- UAPQKLTXQPVJGQ-UHFFFAOYSA-N 3-[4-[2-(1,5-dimethyl-7-oxo-3-propylpyrazolo[4,3-d]pyrimidin-6-yl)ethoxy]phenyl]-2-ethoxypropanoic acid Chemical compound CCCC1=NN(C)C(C2=O)=C1N=C(C)N2CCOC1=CC=C(CC(OCC)C(O)=O)C=C1 UAPQKLTXQPVJGQ-UHFFFAOYSA-N 0.000 claims description 20
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- 150000003626 triacylglycerols Chemical class 0.000 claims description 17
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- 125000003118 aryl group Chemical group 0.000 claims description 16
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- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims description 15
- ZRRNJJURLBXWLL-REWJHTLYSA-N (2r,3r,4r,5s)-6-(octylamino)hexane-1,2,3,4,5-pentol Chemical compound CCCCCCCCNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO ZRRNJJURLBXWLL-REWJHTLYSA-N 0.000 claims description 14
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- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims description 13
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- XBPCUCUWBYBCDP-UHFFFAOYSA-N Dicyclohexylamine Chemical compound C1CCCCC1NC1CCCCC1 XBPCUCUWBYBCDP-UHFFFAOYSA-N 0.000 claims description 12
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- HAMNKKUPIHEESI-UHFFFAOYSA-N aminoguanidine Chemical compound NNC(N)=N HAMNKKUPIHEESI-UHFFFAOYSA-N 0.000 claims description 11
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- 229910052736 halogen Inorganic materials 0.000 claims description 11
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- OTXHZHQQWQTQMW-UHFFFAOYSA-N (diaminomethylideneamino)azanium;hydrogen carbonate Chemical compound OC([O-])=O.N[NH2+]C(N)=N OTXHZHQQWQTQMW-UHFFFAOYSA-N 0.000 claims description 9
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- XAWRDWCILPXSAR-UHFFFAOYSA-N 2-ethoxy-3-[4-[2-(5-ethyl-1-methyl-7-oxo-3-propylpyrazolo[4,3-d]pyrimidin-6-yl)ethoxy]phenyl]propanoic acid Chemical compound CCCC1=NN(C)C(C2=O)=C1N=C(CC)N2CCOC1=CC=C(CC(OCC)C(O)=O)C=C1 XAWRDWCILPXSAR-UHFFFAOYSA-N 0.000 claims description 8
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- WHXSMMKQMYFTQS-UHFFFAOYSA-N Lithium Chemical class [Li] WHXSMMKQMYFTQS-UHFFFAOYSA-N 0.000 claims description 8
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- VTHJTEIRLNZDEV-UHFFFAOYSA-L magnesium dihydroxide Chemical compound [OH-].[OH-].[Mg+2] VTHJTEIRLNZDEV-UHFFFAOYSA-L 0.000 claims description 8
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- 229910001862 magnesium hydroxide Inorganic materials 0.000 claims description 8
- RIWRFSMVIUAEBX-UHFFFAOYSA-N n-methyl-1-phenylmethanamine Chemical compound CNCC1=CC=CC=C1 RIWRFSMVIUAEBX-UHFFFAOYSA-N 0.000 claims description 8
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 claims description 8
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- 125000004183 alkoxy alkyl group Chemical group 0.000 claims description 7
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- BHNOABDGWRVNFJ-ZSCHJXSPSA-N (2s)-2,6-diaminohexanoic acid;2-ethoxy-3-[4-[2-(2-ethyl-6-oxo-4-phenylpyrimidin-1-yl)ethoxy]phenyl]propanoic acid Chemical compound NCCCC[C@H](N)C(O)=O.C1=CC(CC(OCC)C(O)=O)=CC=C1OCCN1C(=O)C=C(C=2C=CC=CC=2)N=C1CC BHNOABDGWRVNFJ-ZSCHJXSPSA-N 0.000 claims description 6
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- WJRONFWTXGGIFO-UHFFFAOYSA-N 2-aminoguanidine;2-ethoxy-3-[4-[2-(2-ethyl-6-oxo-4-phenylpyrimidin-1-yl)ethoxy]phenyl]propanoic acid Chemical compound NN=C(N)N.C1=CC(CC(OCC)C(O)=O)=CC=C1OCCN1C(=O)C=C(C=2C=CC=CC=2)N=C1CC WJRONFWTXGGIFO-UHFFFAOYSA-N 0.000 claims description 6
- CEDOJTDGYCORRG-DDAWSSNUSA-N 3-[4-[2-(1,5-dimethyl-7-oxo-3-propylpyrazolo[4,3-d]pyrimidin-6-yl)ethoxy]phenyl]-2-ethoxypropanoic acid (2R,3R,4R,5S)-6-(octylamino)hexane-1,2,3,4,5-pentol Chemical compound CCCCCCCCNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO.CCCC1=NN(C)C(C2=O)=C1N=C(C)N2CCOC1=CC=C(CC(OCC)C(O)=O)C=C1 CEDOJTDGYCORRG-DDAWSSNUSA-N 0.000 claims description 6
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- CLARZNPYHHNNMG-UHFFFAOYSA-L magnesium 2-ethoxypropanoate Chemical compound [Mg+2].C(C)OC(C(=O)[O-])C.C(C)OC(C(=O)[O-])C CLARZNPYHHNNMG-UHFFFAOYSA-L 0.000 claims description 6
- MWLWFFFRVIAHIN-UHFFFAOYSA-M potassium 2-ethoxypropanoate Chemical compound C(C)OC(C(=O)[O-])C.[K+] MWLWFFFRVIAHIN-UHFFFAOYSA-M 0.000 claims description 6
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- JRZWZCNPHDSCRM-ZSCHJXSPSA-N (2s)-2,6-diaminohexanoic acid;2-ethoxy-3-[4-[2-(2-ethyl-4-oxoquinazolin-3-yl)ethoxy]phenyl]propanoic acid Chemical compound NCCCC[C@H](N)C(O)=O.C1=CC(CC(OCC)C(O)=O)=CC=C1OCCN1C(=O)C2=CC=CC=C2N=C1CC JRZWZCNPHDSCRM-ZSCHJXSPSA-N 0.000 claims description 4
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Classifications
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- 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
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/34—One oxygen atom
- C07D239/36—One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
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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
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/88—Oxygen atoms
- C07D239/90—Oxygen atoms with acyclic radicals attached in position 2 or 3
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
-
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
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- Physical Education & Sports Medicine (AREA)
- Hematology (AREA)
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- Hospice & Palliative Care (AREA)
- Dermatology (AREA)
- Reproductive Health (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US26659501P | 2001-02-05 | 2001-02-05 | |
| IN813CH2001 | 2001-10-04 | ||
| PCT/IB2002/000312 WO2002062798A2 (en) | 2001-02-05 | 2002-02-05 | Salts of pyrimidine derivatives for use against coronary heart disease and atherosclerose |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2004520393A true JP2004520393A (ja) | 2004-07-08 |
| JP2004520393A5 JP2004520393A5 (enExample) | 2005-12-22 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002563151A Withdrawn JP2004520393A (ja) | 2001-02-05 | 2002-02-05 | ヘテロ環化号物の薬学的に許容可能な塩 |
Country Status (4)
| Country | Link |
|---|---|
| EP (1) | EP1363913A2 (enExample) |
| JP (1) | JP2004520393A (enExample) |
| CA (1) | CA2436738A1 (enExample) |
| WO (1) | WO2002062798A2 (enExample) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPWO2004031118A1 (ja) * | 2002-10-03 | 2006-02-09 | 小野薬品工業株式会社 | Ｌｐａ受容体拮抗剤 |
| JP2015510947A (ja) * | 2012-03-22 | 2015-04-13 | トランステック・ファーマ，エルエルシー | 小分子ｇｌｐ１ｒアゴニストのトリス（ヒドロキシメチル）アミノメタン塩ならびにその医薬組成物および使用 |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7041691B1 (en) | 1999-06-30 | 2006-05-09 | Amgen Inc. | Compounds for the modulation of PPARγ activity |
| AU6118001A (en) | 2000-05-03 | 2001-11-12 | Tularik Inc | Combination therapeutic compositions and methods of use |
| US20030171399A1 (en) | 2000-06-28 | 2003-09-11 | Tularik Inc. | Quinolinyl and benzothiazolyl modulators |
| EP1407774A1 (en) * | 2002-09-10 | 2004-04-14 | LION Bioscience AG | 2-Amino-4-quinazolinones as LXR nuclear receptor binding compounds |
| EP1398032A1 (en) * | 2002-09-10 | 2004-03-17 | PheneX Pharmaceuticals AG | 4-Oxo-quinazolines as LXR nuclear receptor binding compounds |
| KR20050122220A (ko) * | 2003-03-25 | 2005-12-28 | 다케다 샌디에고, 인코포레이티드 | 디펩티딜 펩티다제 억제제 |
| US7223761B2 (en) | 2003-10-03 | 2007-05-29 | Amgen Inc. | Salts and polymorphs of a potent antidiabetic compound |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUP0301101A3 (en) * | 1996-12-31 | 2009-03-30 | Reddy S Res Foundation | Novel heterocyclic compounds process for their preparation and pharmaceutical compositions containing them and their use in the treatment of diabetes and related diseases |
| WO1999008501A2 (en) * | 1998-04-23 | 1999-02-25 | Dr. Reddy's Research Foundation | New heterocyclic compounds and their use in medicine, process for their preparation and pharmaceutical compositions containing them |
-
2002
- 2002-02-05 WO PCT/IB2002/000312 patent/WO2002062798A2/en not_active Ceased
- 2002-02-05 JP JP2002563151A patent/JP2004520393A/ja not_active Withdrawn
- 2002-02-05 EP EP02711124A patent/EP1363913A2/en not_active Withdrawn
- 2002-02-05 CA CA002436738A patent/CA2436738A1/en not_active Abandoned
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPWO2004031118A1 (ja) * | 2002-10-03 | 2006-02-09 | 小野薬品工業株式会社 | Ｌｐａ受容体拮抗剤 |
| JP4691988B2 (ja) * | 2002-10-03 | 2011-06-01 | 小野薬品工業株式会社 | Ｌｐａ受容体拮抗剤 |
| JP2015510947A (ja) * | 2012-03-22 | 2015-04-13 | トランステック・ファーマ，エルエルシー | 小分子ｇｌｐ１ｒアゴニストのトリス（ヒドロキシメチル）アミノメタン塩ならびにその医薬組成物および使用 |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2002062798A2 (en) | 2002-08-15 |
| WO2002062798A3 (en) | 2002-12-05 |
| CA2436738A1 (en) | 2002-08-15 |
| EP1363913A2 (en) | 2003-11-26 |
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