JP2004535424A5 - - Google Patents
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- Publication number
- JP2004535424A5 JP2004535424A5 JP2003503590A JP2003503590A JP2004535424A5 JP 2004535424 A5 JP2004535424 A5 JP 2004535424A5 JP 2003503590 A JP2003503590 A JP 2003503590A JP 2003503590 A JP2003503590 A JP 2003503590A JP 2004535424 A5 JP2004535424 A5 JP 2004535424A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- optionally substituted
- aryl
- group
- heteroaryl
- 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.)
- Pending
Links
- 229910052799 carbon Inorganic materials 0.000 claims 127
- 125000001424 substituent group Chemical group 0.000 claims 124
- 229910052739 hydrogen Inorganic materials 0.000 claims 113
- 125000000217 alkyl group Chemical group 0.000 claims 98
- 125000001072 heteroaryl group Chemical group 0.000 claims 91
- 125000000753 cycloalkyl group Chemical group 0.000 claims 89
- 125000003118 aryl group Chemical group 0.000 claims 81
- -1 dihydronaphthalyl Chemical group 0.000 claims 63
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 57
- 125000003545 alkoxy group Chemical group 0.000 claims 40
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 34
- 229910052736 halogen Inorganic materials 0.000 claims 34
- 150000002367 halogens Chemical class 0.000 claims 34
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 28
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 28
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 27
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 24
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 24
- 150000001721 carbon Chemical group 0.000 claims 23
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 22
- 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 22
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 22
- 125000000623 heterocyclic group Chemical group 0.000 claims 22
- 229910052801 chlorine Inorganic materials 0.000 claims 20
- 229910052731 fluorine Inorganic materials 0.000 claims 20
- 239000001257 hydrogen Substances 0.000 claims 18
- 125000000304 alkynyl group Chemical group 0.000 claims 17
- 125000004663 dialkyl amino group Chemical group 0.000 claims 16
- 229910052740 iodine Inorganic materials 0.000 claims 16
- 125000004432 carbon atom Chemical group C* 0.000 claims 13
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 12
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 12
- 229910052760 oxygen Inorganic materials 0.000 claims 11
- 206010012289 Dementia Diseases 0.000 claims 10
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 10
- 150000001875 compounds Chemical class 0.000 claims 9
- 125000001637 1-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C(*)=C([H])C([H])=C([H])C2=C1[H] 0.000 claims 8
- YBYIRNPNPLQARY-UHFFFAOYSA-N 1H-indene Natural products C1=CC=C2CC=CC2=C1 YBYIRNPNPLQARY-UHFFFAOYSA-N 0.000 claims 8
- 125000001622 2-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C(*)C([H])=C([H])C2=C1[H] 0.000 claims 8
- 208000024827 Alzheimer disease Diseases 0.000 claims 8
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 8
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 8
- 125000005842 heteroatom Chemical group 0.000 claims 8
- 125000004857 imidazopyridinyl group Chemical group N1C(=NC2=C1C=CC=N2)* 0.000 claims 8
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims 8
- 125000003454 indenyl group Chemical group C1(C=CC2=CC=CC=C12)* 0.000 claims 8
- 229910052757 nitrogen Inorganic materials 0.000 claims 8
- 229910052717 sulfur Inorganic materials 0.000 claims 8
- 125000005329 tetralinyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 claims 8
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 208000010877 cognitive disease Diseases 0.000 claims 6
- 125000005843 halogen group Chemical group 0.000 claims 6
- 208000027061 mild cognitive impairment Diseases 0.000 claims 6
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims 5
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 5
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 claims 5
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 5
- 125000005865 C2-C10alkynyl group Chemical group 0.000 claims 5
- 125000003342 alkenyl group Chemical group 0.000 claims 5
- 125000003282 alkyl amino group Chemical group 0.000 claims 5
- 125000002837 carbocyclic group Chemical group 0.000 claims 5
- 150000002148 esters Chemical class 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 5
- 125000006727 (C1-C6) alkenyl group Chemical group 0.000 claims 4
- 150000001414 amino alcohols Chemical class 0.000 claims 4
- 125000004429 atom Chemical group 0.000 claims 4
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 4
- 125000002047 benzodioxolyl group Chemical group O1OC(C2=C1C=CC=C2)* 0.000 claims 4
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 4
- 125000004619 benzopyranyl group Chemical group O1C(C=CC2=C1C=CC=C2)* 0.000 claims 4
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 4
- 125000004600 benzothiopyranyl group Chemical group S1C(C=CC2=C1C=CC=C2)* 0.000 claims 4
- 125000004622 benzoxazinyl group Chemical group O1NC(=CC2=C1C=CC=C2)* 0.000 claims 4
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 4
- 125000000609 carbazolyl group Chemical group C1(=CC=CC=2C3=CC=CC=C3NC12)* 0.000 claims 4
- 125000004617 chromonyl group Chemical group O1C(=CC(C2=CC=CC=C12)=O)* 0.000 claims 4
- 125000000259 cinnolinyl group Chemical group N1=NC(=CC2=CC=CC=C12)* 0.000 claims 4
- 230000003412 degenerative effect Effects 0.000 claims 4
- 125000005992 dihydrobenzisothiazinyl group Chemical group 0.000 claims 4
- 125000005993 dihydrobenzisoxazinyl group Chemical group 0.000 claims 4
- 125000002541 furyl group Chemical group 0.000 claims 4
- 150000002431 hydrogen Chemical group 0.000 claims 4
- 125000002883 imidazolyl group Chemical group 0.000 claims 4
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 4
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims 4
- 125000003406 indolizinyl group Chemical group C=1(C=CN2C=CC=CC12)* 0.000 claims 4
- 125000005994 isobenzotetrahydrofuranyl group Chemical group 0.000 claims 4
- 125000005995 isobenzotetrahydrothienyl group Chemical group 0.000 claims 4
- 125000005990 isobenzothienyl group Chemical group 0.000 claims 4
- 125000003384 isochromanyl group Chemical group C1(OCCC2=CC=CC=C12)* 0.000 claims 4
- 125000003151 isocoumarinyl group Chemical group C1(=O)OC(=CC2=CC=CC=C12)* 0.000 claims 4
- 125000004594 isoindolinyl group Chemical group C1(NCC2=CC=CC=C12)* 0.000 claims 4
- 125000000904 isoindolyl group Chemical group C=1(NC=C2C=CC=CC12)* 0.000 claims 4
- 125000005956 isoquinolyl group Chemical group 0.000 claims 4
- 125000001786 isothiazolyl group Chemical group 0.000 claims 4
- 125000000842 isoxazolyl group Chemical group 0.000 claims 4
- 125000002757 morpholinyl group Chemical group 0.000 claims 4
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 claims 4
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 4
- 125000002971 oxazolyl group Chemical group 0.000 claims 4
- 125000001484 phenothiazinyl group Chemical group C1(=CC=CC=2SC3=CC=CC=C3NC12)* 0.000 claims 4
- 125000001644 phenoxazinyl group Chemical group C1(=CC=CC=2OC3=CC=CC=C3NC12)* 0.000 claims 4
- 125000004592 phthalazinyl group Chemical group C1(=NN=CC2=CC=CC=C12)* 0.000 claims 4
- 125000004193 piperazinyl group Chemical group 0.000 claims 4
- 125000003386 piperidinyl group Chemical group 0.000 claims 4
- 125000001042 pteridinyl group Chemical group N1=C(N=CC2=NC=CN=C12)* 0.000 claims 4
- 125000000561 purinyl group Chemical group N1=C(N=C2N=CNC2=C1)* 0.000 claims 4
- 125000003373 pyrazinyl group Chemical group 0.000 claims 4
- 125000003226 pyrazolyl group Chemical group 0.000 claims 4
- 125000002098 pyridazinyl group Chemical group 0.000 claims 4
- 125000004076 pyridyl group Chemical group 0.000 claims 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 4
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 4
- 125000001422 pyrrolinyl group Chemical group 0.000 claims 4
- 125000000168 pyrrolyl group Chemical group 0.000 claims 4
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims 4
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 4
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims 4
- 125000006413 ring segment Chemical group 0.000 claims 4
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 4
- 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 claims 4
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 4
- 125000005958 tetrahydrothienyl group Chemical group 0.000 claims 4
- 125000003831 tetrazolyl group Chemical group 0.000 claims 4
- 125000000335 thiazolyl group Chemical group 0.000 claims 4
- 125000001544 thienyl group Chemical group 0.000 claims 4
- 125000004306 triazinyl group Chemical group 0.000 claims 4
- 125000001425 triazolyl group Chemical group 0.000 claims 4
- 125000004933 β-carbolinyl group Chemical group C1(=NC=CC=2C3=CC=CC=C3NC12)* 0.000 claims 4
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 2
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 claims 2
- 125000004211 3,5-difluorophenyl group Chemical group [H]C1=C(F)C([H])=C(*)C([H])=C1F 0.000 claims 2
- 208000005145 Cerebral amyloid angiopathy Diseases 0.000 claims 2
- 206010008111 Cerebral haemorrhage Diseases 0.000 claims 2
- 208000011990 Corticobasal Degeneration Diseases 0.000 claims 2
- 208000032843 Hemorrhage Diseases 0.000 claims 2
- 206010033799 Paralysis Diseases 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 2
- 210000004558 lewy body Anatomy 0.000 claims 2
- 238000004393 prognosis Methods 0.000 claims 2
- 230000000750 progressive effect Effects 0.000 claims 2
- 230000000306 recurrent effect Effects 0.000 claims 2
- 230000002739 subcortical effect Effects 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- 125000002877 alkyl aryl group Chemical group 0.000 claims 1
- 125000005213 alkyl heteroaryl group Chemical group 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 0 BN(*)C(C**)C(C(*)(*)*)O Chemical compound BN(*)C(C**)C(C(*)(*)*)O 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US29742001P | 2001-06-11 | 2001-06-11 | |
| PCT/US2002/019067 WO2002100820A1 (en) | 2001-06-11 | 2002-06-11 | Substituted aminoalcohols useful in treatment of alzheimer's disease |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2004535424A JP2004535424A (ja) | 2004-11-25 |
| JP2004535424A5 true JP2004535424A5 (https=) | 2006-01-05 |
Family
ID=23146237
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003503590A Pending JP2004535424A (ja) | 2001-06-11 | 2002-06-11 | アルツハイマー病の治療に有用な置換アミノアルコール |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US7361688B2 (https=) |
| EP (1) | EP1406862A1 (https=) |
| JP (1) | JP2004535424A (https=) |
| CA (1) | CA2450557A1 (https=) |
| MX (1) | MXPA03011502A (https=) |
| WO (1) | WO2002100820A1 (https=) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2003238007A1 (en) * | 2002-06-11 | 2003-12-22 | Elan Pharmaceuticals, Inc. | Methods of treating alzheimer's disease using aryl alkanoic acid amides |
| US7521481B2 (en) | 2003-02-27 | 2009-04-21 | Mclaurin Joanne | Methods of preventing, treating and diagnosing disorders of protein aggregation |
| WO2004094413A1 (en) * | 2003-04-21 | 2004-11-04 | Elan Pharmaceuticals, Inc. | Phenacyl 2-hydroxy-3-diaminoalkanes |
| JP2007528404A (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 | 置換された尿素およびカルバメート、フェナシル−２−ヒドロキシ−３−ジアミノアルカン、ならびにベンズアミド−２−ヒドロキシ−３−ジアミノアルカ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 |
| WO2006010095A2 (en) | 2004-07-09 | 2006-01-26 | Elan Pharmaceuticals Inc. | Oxime derivative substituted hydroxyethylamine aspartyl protease inhibitors |
| WO2007047305A1 (en) | 2005-10-12 | 2007-04-26 | Elan Pharmaceuticals, Inc. | Methods of treating amyloidosis using cyclopropyl derivative aspartyl protease inhibitors |
| EP1867329A3 (en) * | 2006-06-14 | 2008-05-07 | Speedel Experimenta AG | 5-Amino-4-hydroxy-2-isopropyl-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-8-methylnonanamides as therapeutic compounds |
| CA2676715A1 (en) | 2007-02-12 | 2008-08-21 | Merck & Co., Inc. | Piperazine derivatives for treatment of ad and related conditions |
| EP2291181B9 (en) | 2008-04-18 | 2013-09-11 | University College Dublin National University Of Ireland, Dublin | Captodiamine for the treatment of depression symptoms |
| US12194023B2 (en) | 2018-11-29 | 2025-01-14 | The Research Foundation For The State University Of New York | Compositions and methods for modular control of bioorthogonal ligation |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MY119161A (en) * | 1994-04-18 | 2005-04-30 | Novartis Ag | Delta-amino-gamma-hydroxy-omega-aryl-alkanoic acid amides with enzyme especially renin inhibiting activities |
| EP0702004A2 (de) * | 1994-09-15 | 1996-03-20 | Ciba-Geigy Ag | 2,9-Diamino- und 2-amino-8-carbamoyl-4-hydroxy-alkansäureamid-derivative |
| EP0716077A1 (de) * | 1994-12-08 | 1996-06-12 | Ciba-Geigy Ag | Aromatisch substituierte Omega-Aminoalkansäureamide und Alkansäurediamide und ihre Verwendung als Renininhibitoren |
| US5703129A (en) * | 1996-09-30 | 1997-12-30 | Bristol-Myers Squibb Company | 5-amino-6-cyclohexyl-4-hydroxy-hexanamide derivatives as inhibitors of β-amyloid protein production |
| CA2374610A1 (en) * | 1999-06-28 | 2001-01-04 | Jordan J. N. Tang | Catalytically active recombinant memapsin and methods of use thereof |
| US6407064B2 (en) * | 1999-12-06 | 2002-06-18 | Seikagaku Corporation | Aminoalcohol derivative and medicament comprising the same |
-
2002
- 2002-06-11 JP JP2003503590A patent/JP2004535424A/ja active Pending
- 2002-06-11 US US10/480,599 patent/US7361688B2/en not_active Expired - Fee Related
- 2002-06-11 EP EP02759092A patent/EP1406862A1/en not_active Ceased
- 2002-06-11 WO PCT/US2002/019067 patent/WO2002100820A1/en not_active Ceased
- 2002-06-11 MX MXPA03011502A patent/MXPA03011502A/es not_active Application Discontinuation
- 2002-06-11 CA CA002450557A patent/CA2450557A1/en not_active Abandoned
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