JP2008505930A - オキシム誘導体置換ヒドロキシエチルアミン系のアスパラギン酸プロテアーゼ阻害薬 - Google Patents
オキシム誘導体置換ヒドロキシエチルアミン系のアスパラギン酸プロテアーゼ阻害薬 Download PDFInfo
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- JP2008505930A JP2008505930A JP2007520579A JP2007520579A JP2008505930A JP 2008505930 A JP2008505930 A JP 2008505930A JP 2007520579 A JP2007520579 A JP 2007520579A JP 2007520579 A JP2007520579 A JP 2007520579A JP 2008505930 A JP2008505930 A JP 2008505930A
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- Prior art keywords
- phenyl
- alkyl
- butyl
- independently
- hydroxy
- 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.)
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- 0 CC(N[C@@](Cc1cc(F)cc(*)c1)[C@@](CNC(CC1)(CCC1=NOCCO)c1cc(C(C)(C)C)ccc1)O)O Chemical compound CC(N[C@@](Cc1cc(F)cc(*)c1)[C@@](CNC(CC1)(CCC1=NOCCO)c1cc(C(C)(C)C)ccc1)O)O 0.000 description 6
- MRXPRCCLLLSZKG-UHFFFAOYSA-N CC(C)(C)c1cc(C(CC2)(CCC2=NO)NCC(C(Cc2cc(F)cc(F)c2)[n]2nnnc2)O)ccc1 Chemical compound CC(C)(C)c1cc(C(CC2)(CCC2=NO)NCC(C(Cc2cc(F)cc(F)c2)[n]2nnnc2)O)ccc1 MRXPRCCLLLSZKG-UHFFFAOYSA-N 0.000 description 1
- WHNDZOVGCLUGIY-UHFFFAOYSA-N CC(C)(C)c1cc(C(CC2)(CCC2=O)NCC(C(Cc2cc(F)cc(F)c2)N2NN(C)N=C2)O)ccc1 Chemical compound CC(C)(C)c1cc(C(CC2)(CCC2=O)NCC(C(Cc2cc(F)cc(F)c2)N2NN(C)N=C2)O)ccc1 WHNDZOVGCLUGIY-UHFFFAOYSA-N 0.000 description 1
- KINUYGKZQPWLLK-IZZNHLLZSA-N CC(C)(C)c1cccc(C(CC2)(CCC2=O)NC[C@H]([C@H](Cc2cc(F)cc(F)c2)NC(C)=O)O)c1 Chemical compound CC(C)(C)c1cccc(C(CC2)(CCC2=O)NC[C@H]([C@H](Cc2cc(F)cc(F)c2)NC(C)=O)O)c1 KINUYGKZQPWLLK-IZZNHLLZSA-N 0.000 description 1
- AEUGQFVNRZFCND-JEUPEJDTSA-N CC(C)(C)c1cccc(C(CCC2)(CC2=C)NC[C@H](C(Cc2cc(F)cc(F)c2)N)O)c1 Chemical compound CC(C)(C)c1cccc(C(CCC2)(CC2=C)NC[C@H](C(Cc2cc(F)cc(F)c2)N)O)c1 AEUGQFVNRZFCND-JEUPEJDTSA-N 0.000 description 1
- IYJIKWJQEJGBIU-NWDGAFQWSA-N CC(N[C@@H](Cc1cc(F)cc(F)c1)[C@@H](CN)O)=O Chemical compound CC(N[C@@H](Cc1cc(F)cc(F)c1)[C@@H](CN)O)=O IYJIKWJQEJGBIU-NWDGAFQWSA-N 0.000 description 1
- FDGUSMLHSYFMPE-JKSUJKDBSA-N CCCCNC[C@H]([C@H](Cc1cc(F)cc(F)c1)NC(C)=O)O Chemical compound CCCCNC[C@H]([C@H](Cc1cc(F)cc(F)c1)NC(C)=O)O FDGUSMLHSYFMPE-JKSUJKDBSA-N 0.000 description 1
- YFXIWGLRXQSPBX-UHFFFAOYSA-N CCc1cc(C(CC2)(CCC2=C)O)ccc1 Chemical compound CCc1cc(C(CC2)(CCC2=C)O)ccc1 YFXIWGLRXQSPBX-UHFFFAOYSA-N 0.000 description 1
- VUEOKCVXTIYFKY-UHFFFAOYSA-N Cc(ccc(CI)c1)c1F Chemical compound Cc(ccc(CI)c1)c1F VUEOKCVXTIYFKY-UHFFFAOYSA-N 0.000 description 1
- CCMXCWVPIUMJPD-UHFFFAOYSA-N Nc1cc(CCC2OC2)cc(N)c1 Chemical compound Nc1cc(CCC2OC2)cc(N)c1 CCMXCWVPIUMJPD-UHFFFAOYSA-N 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
- C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
- C07D285/08—1,2,4-Thiadiazoles; Hydrogenated 1,2,4-thiadiazoles
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C233/00—Carboxylic acid amides
- C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C233/34—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
- C07C233/35—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
- C07C233/36—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
- C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
- C07C237/20—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton containing six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C251/00—Compounds containing nitrogen atoms doubly-bound to a carbon skeleton
- C07C251/32—Oximes
- C07C251/34—Oximes with oxygen atoms of oxyimino groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
- C07C251/44—Oximes with oxygen atoms of oxyimino groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with the carbon atom of at least one of the oxyimino groups being part of a ring other than a six-membered aromatic ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C251/00—Compounds containing nitrogen atoms doubly-bound to a carbon skeleton
- C07C251/32—Oximes
- C07C251/50—Oximes having oxygen atoms of oxyimino groups bound to carbon atoms of substituted hydrocarbon radicals
- C07C251/54—Oximes having oxygen atoms of oxyimino groups bound to carbon atoms of substituted hydrocarbon radicals of hydrocarbon radicals substituted by singly-bound oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C251/00—Compounds containing nitrogen atoms doubly-bound to a carbon skeleton
- C07C251/72—Hydrazones
- C07C251/84—Hydrazones having doubly-bound carbon atoms of hydrazone groups being part of rings other than six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C255/00—Carboxylic acid nitriles
- C07C255/01—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms
- C07C255/32—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring
- C07C255/42—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being further bound to other hetero atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C255/00—Carboxylic acid nitriles
- C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
- C07C255/58—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
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- 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
- C07D213/24—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 substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/36—Radicals substituted by singly-bound nitrogen atoms
- C07D213/40—Acylated substituent nitrogen atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
- C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D257/04—Five-membered rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/20—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings condensed with carbocyclic rings or ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
- C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
- C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D335/00—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom
- C07D335/04—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D335/06—Benzothiopyrans; Hydrogenated benzothiopyrans
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/10—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/04—Systems containing only non-condensed rings with a four-membered ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
- C07C2601/14—The ring being saturated
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US58620704P | 2004-07-09 | 2004-07-09 | |
US60814304P | 2004-09-09 | 2004-09-09 | |
US65687305P | 2005-03-01 | 2005-03-01 | |
US68113805P | 2005-05-16 | 2005-05-16 | |
PCT/US2005/024469 WO2006010095A2 (en) | 2004-07-09 | 2005-07-11 | Oxime derivative substituted hydroxyethylamine aspartyl protease inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
JP2008505930A true JP2008505930A (ja) | 2008-02-28 |
Family
ID=35462378
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2007520579A Pending JP2008505930A (ja) | 2004-07-09 | 2005-07-11 | オキシム誘導体置換ヒドロキシエチルアミン系のアスパラギン酸プロテアーゼ阻害薬 |
Country Status (5)
Families Citing this family (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
TWI332943B (en) * | 2001-07-10 | 2010-11-11 | Synta Pharmaceuticals Corp | Taxol enhancer compounds |
US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
CA2572775A1 (en) * | 2004-07-09 | 2006-01-26 | Elan Pharmaceuticals, Inc. | Oxime derivative hydroxyethylamine aspartyl-protease inhibitors |
JP2009511589A (ja) * | 2005-10-12 | 2009-03-19 | エラン ファーマシューティカルズ,インコーポレイテッド | アリール−シクロプロピル誘導体のアスパルチルプロテアーゼ阻害剤を使用してアミロイドーシスを治療する方法 |
CA2660524A1 (en) | 2006-08-21 | 2008-02-28 | Synta Pharmaceutical Corp. | Compounds for treating proliferative disorders |
WO2012076165A1 (en) | 2010-12-08 | 2012-06-14 | Grünenthal GmbH | Method for synthesising substituted aminocyclohexanone derivatives |
Citations (6)
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JP2004502669A (ja) * | 2000-06-30 | 2004-01-29 | イーラン ファーマスーティカルズ、インコーポレイテッド | アルツハイマー病を治療するための化合物 |
JP2005511735A (ja) * | 2001-12-06 | 2005-04-28 | イーラン ファーマスーティカルズ、インコーポレイテッド | 置換ヒドロキシエチルアミン |
JP2005520791A (ja) * | 2001-11-08 | 2005-07-14 | イーラン ファーマスーティカルズ、インコーポレイテッド | N,n’−置換−1,3−ジアミノ−2−ヒドロキシプロパン誘導体 |
JP2007528402A (ja) * | 2004-03-09 | 2007-10-11 | エラン ファーマシューティカルズ,インコーポレイテッド | 置換ヒドロキシエチルアミン系のアスパラギン酸プロテアーゼ阻害薬 |
JP2007528400A (ja) * | 2004-03-09 | 2007-10-11 | エラン ファーマシューティカルズ,インコーポレイテッド | 置換ヒドロキシエチルアミン系のアスパラギン酸プロテアーゼ阻害薬 |
JP2008505929A (ja) * | 2004-07-09 | 2008-02-28 | エラン ファーマシューティカルズ,インコーポレイテッド | オキシム誘導体ヒドロキシエチルアミン系のアスパラギン酸プロテアーゼ阻害薬 |
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WO2006010095A3 (en) | 2006-06-08 |
US20090042961A1 (en) | 2009-02-12 |
CA2573138A1 (en) | 2006-01-26 |
EP1773756A2 (en) | 2007-04-18 |
US7385085B2 (en) | 2008-06-10 |
US20070149584A9 (en) | 2007-06-28 |
WO2006010095A2 (en) | 2006-01-26 |
US20060135581A1 (en) | 2006-06-22 |
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