JP2008535863A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2008535863A5 JP2008535863A5 JP2008505633A JP2008505633A JP2008535863A5 JP 2008535863 A5 JP2008535863 A5 JP 2008535863A5 JP 2008505633 A JP2008505633 A JP 2008505633A JP 2008505633 A JP2008505633 A JP 2008505633A JP 2008535863 A5 JP2008535863 A5 JP 2008535863A5
- Authority
- JP
- Japan
- Prior art keywords
- unsubstituted
- substituted
- hydroxy
- isophthalamide
- phenylbutan
- 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
Links
- 102000003908 Cathepsin D Human genes 0.000 claims description 7
- 108090000258 Cathepsin D Proteins 0.000 claims description 7
- 102000004169 proteins and genes Human genes 0.000 claims description 2
- 108090000623 proteins and genes Proteins 0.000 claims description 2
- -1 alkyl halogen Chemical class 0.000 claims 298
- 150000001875 compounds Chemical class 0.000 claims 94
- QZUPTXGVPYNUIT-UHFFFAOYSA-N isophthalamide Chemical compound NC(=O)C1=CC=CC(C(N)=O)=C1 QZUPTXGVPYNUIT-UHFFFAOYSA-N 0.000 claims 62
- 125000000217 alkyl group Chemical group 0.000 claims 55
- 229910052739 hydrogen Inorganic materials 0.000 claims 52
- 239000001257 hydrogen Substances 0.000 claims 52
- 125000003118 aryl group Chemical group 0.000 claims 46
- 150000002431 hydrogen Chemical class 0.000 claims 44
- 125000000753 cycloalkyl group Chemical group 0.000 claims 43
- 125000001072 heteroaryl group Chemical group 0.000 claims 42
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 37
- 125000004404 heteroalkyl group Chemical group 0.000 claims 30
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 18
- 229910052736 halogen Inorganic materials 0.000 claims 16
- 150000002367 halogens Chemical class 0.000 claims 15
- 125000004474 heteroalkylene group Chemical group 0.000 claims 14
- 102100021257 Beta-secretase 1 Human genes 0.000 claims 13
- 101710150192 Beta-secretase 1 Proteins 0.000 claims 13
- 230000003197 catalytic effect Effects 0.000 claims 13
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 13
- 125000002947 alkylene group Chemical group 0.000 claims 12
- 125000004343 1-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])(*)C([H])([H])[H] 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- 150000001408 amides Chemical class 0.000 claims 9
- 125000006833 (C1-C5) alkylene group Chemical group 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 239000003112 inhibitor Substances 0.000 claims 8
- 125000004076 pyridyl group Chemical group 0.000 claims 7
- 125000005549 heteroarylene group Chemical group 0.000 claims 5
- 102100021277 Beta-secretase 2 Human genes 0.000 claims 4
- 101710150190 Beta-secretase 2 Proteins 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 3
- HIQWWDCRULXYDF-UHFFFAOYSA-N 3-n-[3-hydroxy-4-[(3-methoxyphenyl)methylamino]-1-phenylbutan-2-yl]-5-[methyl(methylsulfonyl)amino]-1-n-(1-phenylethyl)benzene-1,3-dicarboxamide Chemical compound COC1=CC=CC(CNCC(O)C(CC=2C=CC=CC=2)NC(=O)C=2C=C(C=C(C=2)N(C)S(C)(=O)=O)C(=O)NC(C)C=2C=CC=CC=2)=C1 HIQWWDCRULXYDF-UHFFFAOYSA-N 0.000 claims 3
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 238000006467 substitution reaction Methods 0.000 claims 3
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 125000004212 difluorophenyl group Chemical group 0.000 claims 2
- 125000001188 haloalkyl group Chemical group 0.000 claims 2
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-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 1
- 125000006497 3-methoxybenzyl group Chemical group [H]C1=C([H])C(=C([H])C(OC([H])([H])[H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000004207 3-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(OC([H])([H])[H])=C1[H] 0.000 claims 1
- DOMFPIOLTSMHHA-UHFFFAOYSA-N 3-n-[(2,5-dimethyl-1,3-oxazol-4-yl)methyl]-1-n-[3-hydroxy-4-[(3-methoxyphenyl)methylamino]-1-phenylbutan-2-yl]-3-n-methylbenzene-1,3-dicarboxamide Chemical compound COC1=CC=CC(CNCC(O)C(CC=2C=CC=CC=2)NC(=O)C=2C=C(C=CC=2)C(=O)N(C)CC2=C(OC(C)=N2)C)=C1 DOMFPIOLTSMHHA-UHFFFAOYSA-N 0.000 claims 1
- PHYXHGMZAMMKGO-UHFFFAOYSA-N 3-n-[(4-ethyl-1,3-thiazol-2-yl)methyl]-1-n-[3-hydroxy-4-[(3-methoxyphenyl)methylamino]-1-phenylbutan-2-yl]-3-n-methylbenzene-1,3-dicarboxamide Chemical compound CCC1=CSC(CN(C)C(=O)C=2C=C(C=CC=2)C(=O)NC(CC=2C=CC=CC=2)C(O)CNCC=2C=C(OC)C=CC=2)=N1 PHYXHGMZAMMKGO-UHFFFAOYSA-N 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 claims 1
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 claims 1
- 125000000641 acridinyl group Chemical group C1(=CC=CC2=NC3=CC=CC=C3C=C12)* 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000004603 benzisoxazolyl group Chemical group O1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000003354 benzotriazolyl group Chemical group N1N=NC2=C1C=CC=C2* 0.000 claims 1
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000000609 carbazolyl group Chemical group C1(=CC=CC=2C3=CC=CC=C3NC12)* 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 1
- 125000000904 isoindolyl group Chemical group C=1(NC=C2C=CC=CC12)* 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000005344 pyridylmethyl group Chemical group [H]C1=C([H])C([H])=C([H])C(=N1)C([H])([H])* 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 125000005306 thianaphthenyl group Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000005556 thienylene group Chemical group 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- 102000004190 Enzymes Human genes 0.000 description 2
- 108090000790 Enzymes Proteins 0.000 description 2
- 102000001708 Protein Isoforms Human genes 0.000 description 1
- 108010029485 Protein Isoforms Proteins 0.000 description 1
- 230000002797 proteolythic effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US66954105P | 2005-04-08 | 2005-04-08 | |
| US71754105P | 2005-09-14 | 2005-09-14 | |
| PCT/US2006/013342 WO2006110668A1 (en) | 2005-04-08 | 2006-04-10 | Compounds which inhibit beta-secretase activity and methods of use thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008535863A JP2008535863A (ja) | 2008-09-04 |
| JP2008535863A5 true JP2008535863A5 (cg-RX-API-DMAC7.html) | 2010-10-07 |
Family
ID=36698894
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008505633A Ceased JP2008535863A (ja) | 2005-04-08 | 2006-04-10 | β−セクレターゼ活性を阻害する化合物およびその使用方法 |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US7504420B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP1871739A1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP2008535863A (cg-RX-API-DMAC7.html) |
| KR (1) | KR20080015079A (cg-RX-API-DMAC7.html) |
| AU (1) | AU2006235344B2 (cg-RX-API-DMAC7.html) |
| BR (1) | BRPI0607019A2 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2604291A1 (cg-RX-API-DMAC7.html) |
| MX (1) | MX2007012341A (cg-RX-API-DMAC7.html) |
| NZ (1) | NZ562314A (cg-RX-API-DMAC7.html) |
| WO (1) | WO2006110668A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| EP1797052A1 (en) * | 2004-09-17 | 2007-06-20 | Comentis, Inc. | Bicyclic compounds which inhibit beta-secretase activity and methods of use thereof |
| KR20080015079A (ko) | 2005-04-08 | 2008-02-18 | 코멘티스, 인코포레이티드 | 베타 세크레타제 활성을 억제하는 화합물 및 이것의 사용방법 |
| EP2491785A1 (en) | 2006-11-21 | 2012-08-29 | Purdue Research Foundation | Method and compositions for treating HIV infections |
| WO2008072760A1 (ja) * | 2006-12-15 | 2008-06-19 | Sumika Chemtex Company, Limited | オレフィン系共重合体の水性エマルジョン |
| EP2178837A2 (en) * | 2007-07-26 | 2010-04-28 | Comentis, Inc. | Isophthalamide derivatives inhibiting beta-secretase activity |
| MX2010002938A (es) * | 2007-09-24 | 2010-04-01 | Comentis Inc | Derivados de (3-hidroxi-4-amino-butan-2-il)-3-(2-tiazol-2-il-pirro lidin-1-carbonil)benzamida y compuestos relacionados como inhibidores de beta-secretasa para tratar enfermedad de alzheimer. |
| EP2244571A4 (en) | 2008-01-17 | 2014-02-19 | Purdue Research Foundation | SMALL MOLECULAR INHIBITORS OF HIV PROTEASES |
| US8791135B2 (en) * | 2008-07-01 | 2014-07-29 | Purdue Research Foundation | Nonpeptide HIV-1 protease inhibitors |
| US8501961B2 (en) * | 2008-07-09 | 2013-08-06 | Purdue Research Foundation | HIV protease inhibitors and methods for using |
| WO2010042796A1 (en) * | 2008-10-10 | 2010-04-15 | Purdue Research Foundation | Compounds for treatment of alzheimer's disease |
| WO2010042892A1 (en) * | 2008-10-10 | 2010-04-15 | Comentis, Inc. | Pyrrolidine compounds which inhibit beta-secretase activity and methods of use thereof |
| JP2012521421A (ja) * | 2009-03-25 | 2012-09-13 | コメンティス，インコーポレーテッド | β−セクレターゼ活性を阻害するピロリジン化合物及びその使用方法 |
| ES2373834B1 (es) * | 2010-07-30 | 2012-12-27 | Universitat De Valencia | Derivados de etanolaminas difluorobencílicas con actividad antimicrobiana. |
| US20120053200A1 (en) * | 2010-09-01 | 2012-03-01 | Harald Mauser | Bace 2 inhibitors |
| CN102816129B (zh) * | 2011-06-07 | 2015-08-12 | 中国人民解放军军事医学科学院毒物药物研究所 | 异噻唑啉(烷)酮取代的苯二羧酸衍生物及其作为β-分泌酶抑制剂的用途 |
| CN105001300A (zh) * | 2014-04-17 | 2015-10-28 | 复旦大学 | 组织蛋白酶d抑制剂及其制备方法、药物组合物和应用 |
Family Cites Families (74)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4911920A (en) * | 1986-07-30 | 1990-03-27 | Alcon Laboratories, Inc. | Sustained release, comfort formulation for glaucoma therapy |
| FR2588189B1 (fr) * | 1985-10-03 | 1988-12-02 | Merck Sharp & Dohme | Composition pharmaceutique de type a transition de phase liquide-gel |
| US4902505A (en) | 1986-07-30 | 1990-02-20 | Alkermes | Chimeric peptides for neuropeptide delivery through the blood-brain barrier |
| US4801575A (en) * | 1986-07-30 | 1989-01-31 | The Regents Of The University Of California | Chimeric peptides for neuropeptide delivery through the blood-brain barrier |
| US4743585A (en) | 1986-11-21 | 1988-05-10 | Warner-Lambert Company | Renin inhibitors |
| US4863905A (en) * | 1987-02-04 | 1989-09-05 | Warner-Lambert Company | Renin inhibitors II |
| EP0329295A1 (en) | 1988-02-01 | 1989-08-23 | The Upjohn Company | Renin inhibiting peptides with polar end groups |
| US6407061B1 (en) * | 1989-12-05 | 2002-06-18 | Chiron Corporation | Method for administering insulin-like growth factor to the brain |
| US5624898A (en) * | 1989-12-05 | 1997-04-29 | Ramsey Foundation | Method for administering neurologic agents to the brain |
| DE69212850T2 (de) * | 1991-01-15 | 1997-03-06 | Alcon Lab Inc | Verwendung von Karrageenan in topischen ophthalmologischen Zusammensetzungen |
| US5212162A (en) * | 1991-03-27 | 1993-05-18 | Alcon Laboratories, Inc. | Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions |
| US5120718A (en) * | 1991-06-13 | 1992-06-09 | Abbott Laboratories | Candida acid protease inhibiting compounds |
| US6287792B1 (en) * | 1991-06-17 | 2001-09-11 | The Regents Of The University Of California | Drug delivery of antisense oligonucleotides and peptides to tissues in vivo and to cells using avidin-biotin technology |
| DE4215874A1 (de) | 1992-05-14 | 1993-11-18 | Bayer Ag | Dithiolanylglycinhaltige HIV-Proteaseinhibitoren vom Hydroxyethylenisostertyp |
| MX9308025A (es) | 1992-12-22 | 1994-08-31 | Lilly Co Eli | Compuestos inhibidores de la proteasa del virus dela inmunodeficiencia humana, procedimiento para supreparacion y formulacion farmaceutica que los contiene. |
| US6309853B1 (en) | 1994-08-17 | 2001-10-30 | The Rockfeller University | Modulators of body weight, corresponding nucleic acids and proteins, and diagnostic and therapeutic uses thereof |
| US6693208B2 (en) * | 1999-12-16 | 2004-02-17 | Emisphere Technologies, Inc. | Compounds and compositions for delivering active agents |
| US6753410B2 (en) * | 2000-03-02 | 2004-06-22 | Merck & Co., Inc. | Investigational compounds |
| JP2003530360A (ja) * | 2000-04-12 | 2003-10-14 | インプリクス リミテッド | 薬剤送達のためのペプチド複合体 |
| US6372250B1 (en) * | 2000-04-25 | 2002-04-16 | The Regents Of The University Of California | Non-invasive gene targeting to the brain |
| CA2410680A1 (en) | 2000-06-30 | 2002-01-10 | Elan Pharmaceuticals, Inc. | Compounds to treat alzheimer's disease |
| US6846813B2 (en) | 2000-06-30 | 2005-01-25 | Pharmacia & Upjohn Company | Compounds to treat alzheimer's disease |
| PE20020276A1 (es) * | 2000-06-30 | 2002-04-06 | Elan Pharm Inc | COMPUESTOS DE AMINA SUSTITUIDA COMO INHIBIDORES DE ß-SECRETASA PARA EL TRATAMIENTO DE ALZHEIMER |
| US20040121947A1 (en) * | 2000-12-28 | 2004-06-24 | Oklahoma Medical Research Foundation | Compounds which inhibit beta-secretase activity and methods of use thereof |
| AU2002239727C1 (en) | 2000-12-28 | 2005-12-22 | Oklahoma Medical Research Foundation | Inhibitors of memapsin 2 and use thereof |
| US20030095958A1 (en) * | 2001-04-27 | 2003-05-22 | Bhisetti Govinda R. | Inhibitors of bace |
| US6960664B2 (en) | 2001-05-22 | 2005-11-01 | Pharmacia & Upjohn Company | Aza hydroxylated ethyl amine compounds |
| MXPA03011046A (es) | 2001-06-01 | 2004-06-25 | Elan Pharm Inc | Hidroxialquilaminas. |
| WO2002100410A1 (en) | 2001-06-08 | 2002-12-19 | Elan Pharmaceuticals, Inc. | Methods of treating alzheimer's disease |
| WO2002100399A1 (en) | 2001-06-12 | 2002-12-19 | Elan Pharmaceuticals, Inc. | Macrocycles useful in the treatment of alzheimer's disease |
| WO2002100856A1 (en) | 2001-06-12 | 2002-12-19 | Elan Pharmaceuticals, Inc. | Macrocycles useful in the treatment of alzheimer's disease |
| BR0210683A (pt) | 2001-06-25 | 2004-07-20 | Elan Pharm Inc | Métodos para tratar ou prevenir mal de alzheimer e uma doença distinguida por depósitos de beta-amilóide sobre ou no cérebro, para tratar um paciente que tem, ou para evitar que o paciente adquira uma doença ou condição, para inibir a atividade de beta-secretase, a clivagem de um isotipo de proteìna de precursor de amilóide e a produção de peptìdeo beta-amilóide em uma célula e de uma placa de beta-amilóide em um animal e para produzir um complexo de beta-secretase, uso de um composto e composição |
| DE60234696D1 (de) | 2001-07-11 | 2010-01-21 | Elan Pharm Inc | N-(3-amino-2-hydroxy-propyl)substituierte alkylamidverbindungen |
| US20040266871A1 (en) | 2001-08-28 | 2004-12-30 | Schostarez Heinrich Josef | Methods for treating alzheimer's disease using quinaldoyl-amine derivatives of oxo-and hydroxy-substituted hydrocarbons |
| AU2002356525A1 (en) | 2001-09-24 | 2003-04-07 | Elan Pharmaceuticals, Inc. | Substituted amines for the treatment of neurological disorders |
| EP1432674A2 (en) | 2001-10-04 | 2004-06-30 | Elan Pharmaceuticals, Inc. | Hydroxypropylamines |
| AU2002359301B2 (en) | 2001-10-23 | 2008-07-03 | Comentis, Inc. | Beta-secretase inhibitors and methods of use |
| US20060234944A1 (en) * | 2001-10-23 | 2006-10-19 | Oklahoma Medical Reseach Foundation | Beta-secretase inhibitors and methods of use |
| KR20050044407A (ko) * | 2001-11-08 | 2005-05-12 | 엘란 파마슈티칼스, 인크. | N,n'-치환-1,3-디아미노-2-히드록시프로판 유도체 |
| GEP20074045B (en) | 2001-11-19 | 2007-02-26 | Elan Pharm Inc | (4-phenyl) piperidin-3-yl-phenylcarboxylate derivatives and related compounds as beta-secretase inhibitors for the treatment of alzheimer's disease |
| AU2002356991A1 (en) | 2001-11-21 | 2003-06-10 | Elan Pharmaceuticals, Inc. | Amino acid derivatives useful for the treatment of alzheimer's disease |
| AU2002360508A1 (en) | 2001-12-06 | 2003-06-23 | Elan Pharmaceuticals, Inc. | Substituted hydroxyethylamines |
| CA2472617A1 (en) | 2002-01-04 | 2003-07-17 | Elan Pharmaceuticals, Inc. | Substituted amino carboxamides for the treatment of alzheimer's disease |
| IL163652A0 (en) | 2002-02-27 | 2005-12-18 | Upjohn Co | Substituted hydroxyethylamines |
| WO2003099202A2 (en) | 2002-05-17 | 2003-12-04 | Merck & Co., Inc. | Beta-secretase inhibitors |
| AU2003220115A1 (en) * | 2002-05-20 | 2003-12-12 | Board Of Regents, The University Of Texas System | Methods and compositions for delivering enzymes and nucleic acid molecules to brain, bone, and other tissues |
| WO2003106405A1 (en) | 2002-06-01 | 2003-12-24 | Sunesis Pharmaceuticals, Inc. | Aspartyl protease inhibitors |
| US7557137B2 (en) | 2002-08-05 | 2009-07-07 | Bristol-Myers Squibb Company | Gamma-lactams as beta-secretase inhibitors |
| AU2003262947A1 (en) | 2002-08-30 | 2004-03-19 | Pharmacia And Upjohn Company | Method of preventing or treating atherosclerosis or restenosis |
| PL375747A1 (en) | 2002-09-06 | 2005-12-12 | Elan Pharmaceuticals, Inc. | 1, 3-diamino-2-hydroxypropane prodrug derivatives |
| EP1537072A1 (en) | 2002-09-10 | 2005-06-08 | Pharmacia & Upjohn Company LLC | Substituted aminoethers for the treatment of alzheimer s disease |
| UY27967A1 (es) | 2002-09-10 | 2004-05-31 | Pfizer | Acetil 2-hindroxi-1,3-diaminoalcanos |
| WO2004037179A2 (en) | 2002-10-21 | 2004-05-06 | Pharmacia & Upjohn Company | Substituted peptides useful in the treatment of alzheimer’s disease |
| WO2004043916A1 (en) * | 2002-11-12 | 2004-05-27 | Merck & Co., Inc. | Phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer's disease |
| EP1565428A1 (en) * | 2002-11-27 | 2005-08-24 | Elan Pharmaceuticals, Inc. | Substituted ureas and carbamates |
| US7388079B2 (en) * | 2002-11-27 | 2008-06-17 | The Regents Of The University Of California | Delivery of pharmaceutical agents via the human insulin receptor |
| US20040102369A1 (en) * | 2002-11-27 | 2004-05-27 | The Regents Of The University Of California | Transport of basic fibroblast growth factor across the blood brain barrier |
| GB0228410D0 (en) | 2002-12-05 | 2003-01-08 | Glaxo Group Ltd | Novel Compounds |
| AU2004204692B2 (en) | 2003-01-07 | 2009-07-09 | Merck & Co., Inc. | Macrocyclic beta-secretase inhibitors for treatment of Alzheimer's disease |
| GB0305918D0 (en) | 2003-03-14 | 2003-04-23 | Glaxo Group Ltd | Novel compounds |
| WO2004094384A2 (en) * | 2003-04-21 | 2004-11-04 | Elan Pharmaceuticals, Inc. | (hetero) arylamide 2-hydroxy-3-diaminoalkanes for use in the treatment of alzheimer’s disease |
| GB0309221D0 (en) | 2003-04-23 | 2003-06-04 | Glaxo Group Ltd | Novel compounds |
| EP1648928A2 (en) | 2003-07-11 | 2006-04-26 | Affinium Pharmaceuticals, Inc. | Novel purified polypeptides from staphylococcus aureus |
| MXPA06001559A (es) | 2003-08-08 | 2006-05-15 | Schering Corp | Inhibidores de amina ciclica bace-1 que poseen una benzamida como sustituyente. |
| TW200524910A (en) * | 2003-08-08 | 2005-08-01 | Schering Corp | Cyclic amine BACE-1 inhibitors having a heterocyclic substituent |
| KR100793095B1 (ko) | 2003-10-01 | 2008-01-10 | 주식회사 프로메디텍 | Ｂａｃｅ 저해효능을 가진 신규한 술폰 아미드 유도체 |
| GB0411404D0 (en) | 2004-05-21 | 2004-06-23 | Glaxo Group Ltd | Novel compounds |
| EP1797052A1 (en) | 2004-09-17 | 2007-06-20 | Comentis, Inc. | Bicyclic compounds which inhibit beta-secretase activity and methods of use thereof |
| KR20080015079A (ko) * | 2005-04-08 | 2008-02-18 | 코멘티스, 인코포레이티드 | 베타 세크레타제 활성을 억제하는 화합물 및 이것의 사용방법 |
| US7476764B2 (en) * | 2005-08-04 | 2009-01-13 | Bristol-Myers Squibb Company | Phenylcarboxyamides as beta-secretase inhibitors |
| US20100168070A1 (en) | 2005-08-11 | 2010-07-01 | Niklas Heine | Compounds for the treatment of alzheimer's disease |
| JP2009504612A (ja) | 2005-08-11 | 2009-02-05 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | アルツハイマー病の治療用化合物 |
| WO2007047305A1 (en) * | 2005-10-12 | 2007-04-26 | Elan Pharmaceuticals, Inc. | Methods of treating amyloidosis using cyclopropyl derivative aspartyl protease inhibitors |
| US7838676B2 (en) | 2005-11-21 | 2010-11-23 | Amgen Inc. | Beta-secretase modulators and methods of use |
-
2006
- 2006-04-10 KR KR1020077025947A patent/KR20080015079A/ko not_active Abandoned
- 2006-04-10 EP EP06749671A patent/EP1871739A1/en not_active Withdrawn
- 2006-04-10 AU AU2006235344A patent/AU2006235344B2/en not_active Ceased
- 2006-04-10 JP JP2008505633A patent/JP2008535863A/ja not_active Ceased
- 2006-04-10 MX MX2007012341A patent/MX2007012341A/es active IP Right Grant
- 2006-04-10 CA CA002604291A patent/CA2604291A1/en not_active Abandoned
- 2006-04-10 WO PCT/US2006/013342 patent/WO2006110668A1/en not_active Ceased
- 2006-04-10 NZ NZ562314A patent/NZ562314A/en not_active IP Right Cessation
- 2006-04-10 BR BRPI0607019-1A patent/BRPI0607019A2/pt not_active IP Right Cessation
- 2006-08-09 US US11/463,558 patent/US7504420B2/en not_active Expired - Fee Related
-
2007
- 2007-08-01 US US11/832,540 patent/US20080176939A1/en not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2008535863A5 (cg-RX-API-DMAC7.html) | ||
| JP2010540462A5 (cg-RX-API-DMAC7.html) | ||
| CA2462289C (en) | Heteroaryl substituted tetrazole modulators of metabotropic glutamate receptor-5 | |
| RU2447060C2 (ru) | Ингибиторы сфингозинкиназы | |
| JP4171417B2 (ja) | ジペプチジルペプチダーゼｉｖインヒビターとしてのｎ−置換ピロリジン誘導体 | |
| RU2401265C2 (ru) | Соединения и композиции в качестве ингибиторов протеинкиназы | |
| RU2008117170A (ru) | Пиримидинамидные соединения как ингибиторы pgds | |
| JP2007523905A5 (cg-RX-API-DMAC7.html) | ||
| JP2008509982A5 (cg-RX-API-DMAC7.html) | ||
| JP2009510170A5 (cg-RX-API-DMAC7.html) | ||
| JP2005527625A5 (cg-RX-API-DMAC7.html) | ||
| RU2009133807A (ru) | Соединения амино-5-[замещенного-4-(дифторметокси)фенил]-5-фенилимидазолона в качестве ингибиторов бета-секретазы | |
| RU2018138707A (ru) | Замещенные гетероарилом пиридины и способы применения | |
| RU2007117913A (ru) | 2, 6-замещенные-4-монозамещенный амино-пиримидины как антагонисты рецептора простагландина d2 | |
| CA2478068A1 (en) | Dihydropyrazole compounds useful for treating or preventing cancer | |
| CA2550596A1 (en) | 3-cycloalkylaminopyrrolidine derivatives as modulators of chemokine receptors | |
| MX2013001363A (es) | N- ((6-amino-piridin-3-il)-metil) -heteroaril-carboxamidas como inhibidoras de calicreina de plasma. | |
| RU2008135690A (ru) | Соединения и композиции в качестве ингибиторов протеинкиназы | |
| RU2011147203A (ru) | Гетероароматические и ароматические пиперазинилазетидиниламиды в качестве ингибиторов моноацилглицеринлипазы | |
| CA2482346A1 (en) | Substituted phenylacetamides and their use as glucokinase activators | |
| NZ588652A (en) | Carboxamide compounds for the treatment of metabolic disorders | |
| JP2007508346A5 (cg-RX-API-DMAC7.html) | ||
| JP2013517273A5 (cg-RX-API-DMAC7.html) | ||
| JP2007519695A5 (cg-RX-API-DMAC7.html) | ||
| JP2006500369A5 (cg-RX-API-DMAC7.html) |