PE20070135A1 - Compuestos heterociclicos como inhibidores de aspartil proteasas - Google Patents
Compuestos heterociclicos como inhibidores de aspartil proteasasInfo
- Publication number
- PE20070135A1 PE20070135A1 PE2006000655A PE2006000655A PE20070135A1 PE 20070135 A1 PE20070135 A1 PE 20070135A1 PE 2006000655 A PE2006000655 A PE 2006000655A PE 2006000655 A PE2006000655 A PE 2006000655A PE 20070135 A1 PE20070135 A1 PE 20070135A1
- Authority
- PE
- Peru
- Prior art keywords
- aspartile
- inhibitors
- arylalkyl
- alkyl
- proteases
- Prior art date
Links
- 108091005804 Peptidases Proteins 0.000 title abstract 2
- 239000004365 Protease Substances 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 102000035195 Peptidases Human genes 0.000 title 1
- 150000002391 heterocyclic compounds Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 206010007559 Cardiac failure congestive Diseases 0.000 abstract 1
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 206010019280 Heart failures Diseases 0.000 abstract 1
- 206010020772 Hypertension Diseases 0.000 abstract 1
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 abstract 1
- 230000001149 cognitive effect Effects 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Virology (AREA)
- Physical Education & Sports Medicine (AREA)
- Neurosurgery (AREA)
- Heart & Thoracic Surgery (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- Hospice & Palliative Care (AREA)
- AIDS & HIV (AREA)
- Oncology (AREA)
- Psychiatry (AREA)
- Cardiology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
SE REFIERE A UN COMPUESTO DE FORMULA (I) DONDE j ES 0 O 1; k ES 0 O 1; W ES UN ENLACE, C(=S), S(O), S(O)2, ENTRE OTROS; U ES N O C(R6); R ES 1 A 5 GRUPOS R21 DONDE R21 ES ALQUILO(C1-C20), ARILALQUILO, CICLOALQUILO(C3-C15), ENTRE OTROS; R1 Y R2 SON H, ALQUILO(C1-C20), ARILALQUILO, HETEROARILO DE 5 A 14 MIEMBROS QUE TIENE DE 1 A 4 HETEROATOMOS SELECCIONADOS DE O, S Y N, ENTRE OTROS; R3, R6 Y R7 SON H, ALQUILO(C1-C20), ARILO(C6-C14), ARILALQUILO, ENTRE OTROS; R4 Y R7a SON ALQUILENO(C1-C20), ARILALQUILENO, ARILENO(C6-C14), ENTRE OTROS. SON COMPUESTOS PREFERIDOS LOS COMPUESTOS DE FORMULA (A), (B), ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA ASPARTIL PROTEASA SIENDO UTILES PARA EL TRATAMIENTO DE ENFERMEDADES CARDIOVASCULARES TAL COMO HIPERTENSION, INSUFICIENCIA CARDIACA CONGESTIVA; ENFERMEDADES COGNITIVAS O NEURODEGENERATIVAS TAL COMO LA ENFERMEDAD DE ALZHEIMER
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US69053705P | 2005-06-14 | 2005-06-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20070135A1 true PE20070135A1 (es) | 2007-03-09 |
Family
ID=37114557
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2006000655A PE20070135A1 (es) | 2005-06-14 | 2006-06-12 | Compuestos heterociclicos como inhibidores de aspartil proteasas |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US7868000B2 (es) |
| EP (1) | EP1896478B1 (es) |
| JP (2) | JP2008543849A (es) |
| KR (1) | KR20080029965A (es) |
| CN (1) | CN101228163A (es) |
| AR (1) | AR054617A1 (es) |
| AU (1) | AU2006259572A1 (es) |
| BR (1) | BRPI0612072A2 (es) |
| CA (1) | CA2609582A1 (es) |
| EC (1) | ECSP078003A (es) |
| IL (1) | IL187814A0 (es) |
| MX (1) | MX2007016180A (es) |
| NO (1) | NO20080187L (es) |
| PE (1) | PE20070135A1 (es) |
| RU (1) | RU2008100165A (es) |
| SG (1) | SG162790A1 (es) |
| TW (2) | TW201004961A (es) |
| WO (1) | WO2006138264A2 (es) |
Families Citing this family (70)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0220581D0 (en) | 2002-09-04 | 2002-10-09 | Novartis Ag | Organic Compound |
| US7700603B2 (en) | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7592348B2 (en) | 2003-12-15 | 2009-09-22 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| AR049401A1 (es) * | 2004-06-18 | 2006-07-26 | Novartis Ag | Aza-biciclononanos |
| GB0415746D0 (en) | 2004-07-14 | 2004-08-18 | Novartis Ag | Organic compounds |
| EP1896032B1 (en) | 2005-06-14 | 2012-10-31 | Merck Sharp & Dohme Corp. | The preparation and use of compounds as protease inhibitors |
| AR054620A1 (es) | 2005-06-14 | 2007-07-04 | Schering Corp | Inhibidores de aspartil proteasas |
| EP1896478B1 (en) | 2005-06-14 | 2014-05-21 | Merck Sharp & Dohme Corp. | Aspartyl protease inhibitors |
| GB0521508D0 (en) * | 2005-10-21 | 2005-11-30 | Novartis Ag | Organic compounds |
| WO2007050721A2 (en) | 2005-10-27 | 2007-05-03 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| GB0525672D0 (en) * | 2005-12-16 | 2006-01-25 | Novartis Ag | Organic compounds |
| GB0525673D0 (en) | 2005-12-16 | 2006-01-25 | Novartis Ag | Organic compounds |
| AU2007258435A1 (en) | 2006-06-12 | 2007-12-21 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| TW200815349A (en) | 2006-06-22 | 2008-04-01 | Astrazeneca Ab | New compounds |
| AU2007332754A1 (en) * | 2006-12-12 | 2008-06-19 | Schering Corporation | Aspartyl protease inhibitors |
| EP2061771A1 (en) * | 2006-12-12 | 2009-05-27 | Schering Corporation | Aspartyl protease inhibitors containing a tricyclic ring system |
| TW200902499A (en) | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
| EP2200990A1 (en) | 2007-09-06 | 2010-06-30 | Schering Corporation | Gamma secretase modulators |
| EP2217604A1 (en) | 2007-11-05 | 2010-08-18 | Schering Corporation | Gamma secretase modulators |
| EP2227471A1 (en) | 2007-12-11 | 2010-09-15 | Schering Corporation | Gamma secretase modulators |
| AU2009239536C1 (en) * | 2008-04-22 | 2012-12-13 | Merck Sharp & Dohme Corp. | Phenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use |
| CN102282145A (zh) | 2008-11-13 | 2011-12-14 | 先灵公司 | γ分泌酶调节剂 |
| TW201020244A (en) | 2008-11-14 | 2010-06-01 | Astrazeneca Ab | New compounds |
| EP2379563B1 (en) | 2008-12-22 | 2014-07-16 | Merck Sharp & Dohme Corp. | Gamma secretase modulators |
| CA2747750A1 (en) | 2008-12-22 | 2010-07-01 | Theodros Asberom | Gamma secretase modulators |
| FR2944011B1 (fr) * | 2009-04-03 | 2011-05-20 | Pf Medicament | Derives d'aminocyclobutane ou d'aminocyclobutene, leur procede de preparation et leur utilisation a titre de medicaments. |
| WO2010147973A1 (en) | 2009-06-16 | 2010-12-23 | Schering Corporation | Gamma secretase modulators |
| EP2443119A1 (en) | 2009-06-16 | 2012-04-25 | Schering Corporation | Gamma secretase modulators |
| WO2010147969A2 (en) | 2009-06-16 | 2010-12-23 | Schering Corporation | Gamma secretase modulators |
| GB0912778D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydro-oxazine derivatives |
| GB0912777D0 (en) * | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydropyrimidone derivatives |
| EP2281824A1 (en) | 2009-08-07 | 2011-02-09 | Noscira, S.A. | Furan-imidazolone derivatives, for the treatment of cognitive, neurodegenerative or neuronal diseases or disorders |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| WO2011044185A2 (en) | 2009-10-08 | 2011-04-14 | Schering Corporation | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
| US8563543B2 (en) | 2009-10-08 | 2013-10-22 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| WO2011044184A1 (en) | 2009-10-08 | 2011-04-14 | Schering Corporation | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
| US20120245155A1 (en) * | 2009-12-11 | 2012-09-27 | Shionogi & Co., Ltd. | Fused heterocyclic compound having amino group |
| JP2013542973A (ja) | 2010-11-22 | 2013-11-28 | ノスシラ、ソシエダッド、アノニマ | 神経変性疾患または神経変性状態を治療するためのビピリジンスルホンアミド誘導体 |
| US8415483B2 (en) | 2010-12-22 | 2013-04-09 | Astrazeneca Ab | Compounds and their use as BACE inhibitors |
| GB201100181D0 (en) | 2011-01-06 | 2011-02-23 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| GB201101140D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| GB201101139D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| BR112013016241A2 (pt) | 2011-01-21 | 2016-07-12 | Eisai R&D Man Co Ltd | composto, e, método para fabricar um composto |
| US9221839B2 (en) | 2011-04-07 | 2015-12-29 | Merck Sharp & Dohme Corp. | C5-C6 oxacyclic-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use |
| WO2012138590A1 (en) * | 2011-04-07 | 2012-10-11 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| RU2014111055A (ru) | 2011-08-22 | 2015-09-27 | Мерк Шарп И Доум Корп. | 2-спирозамещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов bace, композиции и их применение |
| WO2013054108A1 (en) | 2011-10-10 | 2013-04-18 | Astrazeneca Ab | Mono-fluoro beta-secretase inhibitors |
| CA2867891C (en) | 2012-03-19 | 2021-09-14 | Buck Institute For Research On Aging | App specific bace inhibitors (asbis) and uses thereof |
| JO3143B1 (ar) | 2012-04-03 | 2017-09-20 | Lilly Co Eli | مركبات تتراهيدرو بيرولو ثيازين |
| WO2013180265A1 (ja) | 2012-06-01 | 2013-12-05 | 武田薬品工業株式会社 | 複素環化合物 |
| US9000185B2 (en) | 2012-06-20 | 2015-04-07 | Astrazeneca Ab | Cycloalkyl ether compounds and their use as BACE inhibitors |
| US9000182B2 (en) | 2012-06-20 | 2015-04-07 | Astrazeneca Ab | 2H-imidazol-4-amine compounds and their use as BACE inhibitors |
| US9000184B2 (en) | 2012-06-20 | 2015-04-07 | Astrazeneca Ab | Cyclohexane-1,2′-naphthalene-1′,2″-imidazol compounds and their use as BACE inhibitors |
| US9000183B2 (en) | 2012-06-20 | 2015-04-07 | Astrazeneca Ab | Cyclohexane-1,2′-indene-1′,2″-imidazol compounds and their use as BACE inhibitors |
| US10548882B2 (en) | 2012-06-21 | 2020-02-04 | Astrazeneca Ab | Camsylate salt |
| WO2014062549A1 (en) | 2012-10-17 | 2014-04-24 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| WO2014062553A1 (en) | 2012-10-17 | 2014-04-24 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| CA2886507C (en) * | 2012-10-26 | 2016-09-20 | Eli Lilly And Company | Bace inhibitors |
| WO2014099788A1 (en) | 2012-12-21 | 2014-06-26 | Merck Sharp & Dohme Corp. | C5-spiro iminothiadiazine dioxides as bace inhibitors |
| ES2769578T3 (es) | 2013-02-12 | 2020-06-26 | Buck Inst Res Aging | Hidantoínas que modulan el procesamiento de APP mediado por BACE |
| TWI593692B (zh) | 2013-03-12 | 2017-08-01 | 美國禮來大藥廠 | 四氫吡咯并噻嗪化合物 |
| TWI639607B (zh) | 2013-06-18 | 2018-11-01 | 美國禮來大藥廠 | Bace抑制劑 |
| WO2015095104A1 (en) | 2013-12-18 | 2015-06-25 | Merck Sharp & Dohme Corp. | Iminothiadiazepane dioxide compounds as bace inhibitors, compositions, and their use |
| AR103680A1 (es) | 2015-02-23 | 2017-05-24 | Lilly Co Eli | Inhibidores selectivos de bace1 |
| CN104761557B (zh) * | 2015-04-08 | 2017-02-22 | 河南师范大学 | 六氢‑1H‑吡咯并[3,4‑d]嘧啶类化合物及其制备方法 |
| AR104241A1 (es) | 2015-04-29 | 2017-07-05 | Lilly Co Eli | Derivados de tetrahidrofuro tiazina como inhibidores de bace1 selectivos |
| WO2017139209A1 (en) * | 2016-02-11 | 2017-08-17 | Merck Sharp & Dohme Corp. | C5-c6-oxacylic fused iminothiazine dioxide compounds bearing an ether linker as bace inhibitors, compositions, and their use |
| CN107892697B (zh) | 2016-12-26 | 2020-11-03 | 郑州泰基鸿诺医药股份有限公司 | 一种[1,3]噻嗪-2-胺类化合物及应用,药物组合物 |
| CA3088000A1 (en) | 2018-02-28 | 2019-09-06 | Japan Tobacco Inc. | Saturated-ring-fused dihydropyrimidinone or dihydrotriazinone compounds and pharmaceutical use thereof |
Family Cites Families (100)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL92011A0 (en) | 1988-10-19 | 1990-07-12 | Abbott Lab | Heterocyclic peptide renin inhibitors |
| AU2436792A (en) | 1991-08-16 | 1993-03-16 | Merck & Co., Inc. | Quinazoline derivatives as inhibitors of hiv reverse transcriptase |
| US5610294A (en) | 1991-10-11 | 1997-03-11 | The Du Pont Merck Pharmaceutical Company | Substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors |
| IT1270008B (it) | 1994-09-23 | 1997-04-16 | Ist Superiore Sanita | Derivati purinici ed 8-azapurinici atti al trattamento terapeutico dell'aids |
| US5889006A (en) | 1995-02-23 | 1999-03-30 | Schering Corporation | Muscarinic antagonists |
| IL117149A0 (en) | 1995-02-23 | 1996-06-18 | Schering Corp | Muscarinic antagonists |
| US5935958A (en) | 1996-07-01 | 1999-08-10 | Schering Corporation | Muscarinic antagonists |
| US5952349A (en) | 1996-07-10 | 1999-09-14 | Schering Corporation | Muscarinic antagonists for treating memory loss |
| US5977138A (en) | 1996-08-15 | 1999-11-02 | Schering Corporation | Ether muscarinic antagonists |
| CA2335477C (en) * | 1998-06-19 | 2010-11-30 | Vertex Pharmaceuticals Incorporated | Sulfonamide inhibitors of aspartyl protease |
| US6066636A (en) | 1998-06-30 | 2000-05-23 | Schering Corporation | Muscarinic antagonists |
| US6492408B1 (en) | 1999-07-21 | 2002-12-10 | Boehringer Ingelheim Pharmaceuticals, Inc. | Small molecules useful in the treatment of inflammatory disease |
| US6294554B1 (en) | 1999-09-22 | 2001-09-25 | Schering Corporation | Muscarinic antagonists |
| US6414161B1 (en) | 2000-08-09 | 2002-07-02 | Boehringer Ingelheim Pharmaceuticals, Inc. | Synthesis of (R)-3-(4-Bromobenzyl)-1-(3,5-dichlorophenyl)-5-iodo-3-methyl-1-H-imidazo[1,2-a]imidazol-2-one |
| JP4012068B2 (ja) | 2000-12-22 | 2007-11-21 | シェーリング コーポレイション | ムスカリンアンタゴニスト |
| AU2002306734A1 (en) | 2001-03-15 | 2002-10-03 | The Johns Hopkins University | Inhibitors of plasmepsins |
| CN1301972C (zh) | 2001-10-10 | 2007-02-28 | 先灵公司 | 作为毒覃碱拮抗剂的哌啶化合物 |
| AR045219A1 (es) | 2003-08-08 | 2005-10-19 | Pharmacopeia Inc | Aminas ciclicas inhibidoras de base - 1 que poseen un sustiuyente heterociclico |
| ATE424383T1 (de) | 2003-08-08 | 2009-03-15 | Schering Corp | Cyclische amine mit benzamidsubstituent als bace- 1-inhibitoren |
| US20050171112A1 (en) | 2003-11-03 | 2005-08-04 | Probiodrug Ag | Combinations useful for the treatment of neuronal disorders |
| US7592348B2 (en) | 2003-12-15 | 2009-09-22 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| CA2548388A1 (en) | 2003-12-15 | 2005-06-30 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7700603B2 (en) | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| EP1740573A1 (en) | 2004-04-22 | 2007-01-10 | Eli Lilly And Company | Amides as bace inhibitors |
| WO2006009655A1 (en) | 2004-06-16 | 2006-01-26 | Wyeth | Diphenylimidazopyrimidine and -imidazole amines as inhibitors of b-secretase |
| MXPA06014793A (es) | 2004-06-16 | 2007-02-16 | Wyeth Corp | Derivados de amino-5, 5-difenilimidazolona para la inhibicion de ??-secretasa. |
| AR049726A1 (es) | 2004-07-22 | 2006-08-30 | Schering Corp | Amidas sustituidas inhibidoras de beta secretasa |
| CA2575340A1 (en) | 2004-07-28 | 2006-02-09 | Schering Corporation | Macrocyclic beta-secretase inhibitors |
| ES2349594T3 (es) | 2004-08-06 | 2011-01-05 | Janssen Pharmaceutica Nv | Derivados de 2-amino-quinazolín usados como inhibidores de b-secretase (bace). |
| US8436006B2 (en) | 2004-08-06 | 2013-05-07 | Jansssen Pharmaceutica N.V. | 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE) |
| JP5046932B2 (ja) | 2004-08-06 | 2012-10-10 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | β−セクレターゼ(BACE)のインヒビターとして有用な新規の2−アミノ−キナゾリン誘導体 |
| WO2006044492A2 (en) | 2004-10-14 | 2006-04-27 | Ingenious Targeting Laboratory, Inc. | Methods for generating rat embryo-derived cell lines and genetic modification of rat genome |
| JP2008516945A (ja) | 2004-10-15 | 2008-05-22 | アストラゼネカ・アクチエボラーグ | 置換されたアミノ化合物およびそれらの使用 |
| CN101084198A (zh) | 2004-10-15 | 2007-12-05 | 阿斯利康(瑞典)有限公司 | 取代的氨基-嘧啶酮及其用途 |
| RU2007126570A (ru) | 2005-01-14 | 2009-02-20 | Вайет (Us) | Аминоимидазолоны, применяемые для ингибирования бета-секретазы |
| US7759353B2 (en) | 2005-06-14 | 2010-07-20 | Schering Corporation | Substituted spiro iminopyrimidinones as aspartyl protease inhibitors, compositions, and methods of treatment |
| AR054620A1 (es) | 2005-06-14 | 2007-07-04 | Schering Corp | Inhibidores de aspartil proteasas |
| CN101193859A (zh) | 2005-06-14 | 2008-06-04 | 先灵公司 | 蛋白酶抑制剂的制备和用途 |
| AR053902A1 (es) | 2005-06-14 | 2007-05-23 | Schering Corp | Inhibidores de aspartil proteasa heterociclicos macrociclicos |
| EP1896478B1 (en) | 2005-06-14 | 2014-05-21 | Merck Sharp & Dohme Corp. | Aspartyl protease inhibitors |
| EP1896032B1 (en) | 2005-06-14 | 2012-10-31 | Merck Sharp & Dohme Corp. | The preparation and use of compounds as protease inhibitors |
| US8110682B2 (en) | 2005-06-14 | 2012-02-07 | Schering Corporation | Preparation and use of compounds as aspartyl protease inhibitors |
| TW200738683A (en) | 2005-06-30 | 2007-10-16 | Wyeth Corp | Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation |
| BRPI0613578A2 (pt) | 2005-06-30 | 2012-01-17 | Wyeth Corp | composito da fórmula i; uso de um composto de fórmula i; e composição farmacêutica |
| TW200730523A (en) | 2005-07-29 | 2007-08-16 | Wyeth Corp | Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation |
| CN101273018A (zh) | 2005-09-26 | 2008-09-24 | 惠氏公司 | 用于β分泌酶(BACE)抑制剂的氨基-5-[4-(二氟甲氧基)苯基]-5-苯基咪唑酮化合物 |
| EP1966198B1 (en) | 2005-10-25 | 2011-03-16 | Janssen Pharmaceutica NV | 2-amino-3,4-dihydro-pyrido[3,4-d]pyrimidine derivatives useful as inhibitors of beta-secretase (bace) |
| ES2537898T3 (es) | 2005-10-25 | 2015-06-15 | Shionogi & Co., Ltd. | Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1 |
| WO2007050721A2 (en) | 2005-10-27 | 2007-05-03 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| CA2628264A1 (en) | 2005-10-31 | 2007-05-10 | Schering Corporation | Aspartyl protease inhibitors |
| TW200804290A (en) | 2005-11-15 | 2008-01-16 | Astrazeneca Ab | Compounds and uses thereof |
| EP1951680A4 (en) | 2005-11-15 | 2011-08-10 | Astrazeneca Ab | NOVEL 2-AMINOPYRIMIDINONE DERIVATIVES AND THEIR USE |
| US20080318985A1 (en) | 2005-11-15 | 2008-12-25 | Astrazeneca Ab | Novel 2-Aminopyrimidinone Or 2-Aminopyridinone Derivatives and Their Use |
| TW200734311A (en) | 2005-11-21 | 2007-09-16 | Astrazeneca Ab | New compounds |
| WO2007058601A1 (en) | 2005-11-21 | 2007-05-24 | Astrazeneca Ab | Novel 2-amino-imidazole-4-one compounds and their use in the manufacture of a medicament to be used in the treatment of cognitive impairment, alzheimer’s disease, neurodegeneration and dementia |
| AR058381A1 (es) | 2005-12-19 | 2008-01-30 | Astrazeneca Ab | Compuestos derivados de 2-aminopiridin-4-onas y una composicion farmaceutica |
| JP2009520027A (ja) | 2005-12-19 | 2009-05-21 | ワイス | 2−アミノ−5−ピペリジニルイミダゾロン化合物およびβ−セクレターゼ調節におけるその使用 |
| WO2007092854A2 (en) | 2006-02-06 | 2007-08-16 | Janssen Pharmaceutica N.V. | 2-AMINO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE) |
| WO2007092839A2 (en) | 2006-02-06 | 2007-08-16 | Janssen Pharmaceutica N.V. | Macrocycle derivatives useful as inhibitors of beta-secretase (bace) |
| WO2007092846A2 (en) | 2006-02-06 | 2007-08-16 | Janssen Pharmaceutica N.V. | 2-AMINO-3,4-DIHYDRO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE) |
| WO2007100536A1 (en) | 2006-02-24 | 2007-09-07 | Wyeth | DIHYDROSPIRO[DIBENZO[A,D][7]ANNULENE-5,4'-IMIDAZOL] COMPOUNDS FOR THE INHIBITION OF β-SECRETASE |
| US20090099217A1 (en) | 2006-04-05 | 2009-04-16 | Astex Therapeutics Ltd. | 2-Aminopyrimidin-4-Ones And Their Use For Treating Or Preventing Alpha Beta-Related Pathologies |
| AU2007258435A1 (en) | 2006-06-12 | 2007-12-21 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| TW200815447A (en) | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds IV |
| US20080051420A1 (en) | 2006-06-14 | 2008-02-28 | Astrazeneca Ab | New Compounds 317 |
| TW200815449A (en) | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds II |
| TW200808796A (en) | 2006-06-14 | 2008-02-16 | Astrazeneca Ab | New compounds III |
| TW200815443A (en) | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds I |
| TW200815349A (en) | 2006-06-22 | 2008-04-01 | Astrazeneca Ab | New compounds |
| TW200817406A (en) | 2006-08-17 | 2008-04-16 | Wyeth Corp | Imidazole amines as inhibitors of β-secretase |
| WO2008063114A1 (en) | 2006-11-20 | 2008-05-29 | Astrazeneca Ab | Amino- imidazolones and their use as medicament for treating cognitive impairment alzheimer disease, neurodegeneration and dementia |
| EP2061771A1 (en) * | 2006-12-12 | 2009-05-27 | Schering Corporation | Aspartyl protease inhibitors containing a tricyclic ring system |
| AU2007332754A1 (en) * | 2006-12-12 | 2008-06-19 | Schering Corporation | Aspartyl protease inhibitors |
| TW200831484A (en) | 2006-12-20 | 2008-08-01 | Astrazeneca Ab | New compounds |
| TW200831091A (en) | 2006-12-20 | 2008-08-01 | Astrazeneca Ab | New compounds |
| WO2008076044A1 (en) | 2006-12-20 | 2008-06-26 | Astrazeneca Ab | Novel 2-amino-5, 5-diaryl-imidazol-4-ones |
| PE20090160A1 (es) | 2007-03-20 | 2009-02-11 | Wyeth Corp | COMPUESTOS AMINO-5-[4-(DIFLUOROMETOXI)FENIL SUSTITUIDO]-5-FENILIMIDAZOLONA COMO INHIBIDORES DE ß-SECRETASA |
| AR065814A1 (es) | 2007-03-23 | 2009-07-01 | Wyeth Corp | Derivados de 5-fenilimidazolona,inhibidores de beta-secretasa,composiciones farmaceuticas que los contienen y usos para prevenir y/o tratar trastornos asociados a niveles beta-amiloides elevados. |
| EP2689780A1 (en) | 2007-04-24 | 2014-01-29 | Shionogi & Co., Ltd. | Intermediates for aminodihydrothiazine derivatives substituted with a cyclic group |
| EP2151435A4 (en) | 2007-04-24 | 2011-09-14 | Shionogi & Co | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE |
| TW200902503A (en) | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
| TW200902499A (en) | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
| WO2009005470A1 (en) | 2007-07-05 | 2009-01-08 | Astrazeneca Ab | Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors |
| WO2009005471A1 (en) | 2007-07-05 | 2009-01-08 | Astrazeneca Ab | Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors |
| CA2687750C (en) | 2007-07-06 | 2016-10-18 | Boehringer Ingelheim International Gmbh | Substituted amino-quinazolinones, medicaments comprising said compound, their use and their method of manufacture |
| PT2233474E (pt) | 2008-01-18 | 2015-10-26 | Eisai R&D Man Co Ltd | Derivado de aminodihidrotiazina condensado |
| TW200932218A (en) | 2008-01-22 | 2009-08-01 | Boehringer Ingelheim Int | Substituted amino-benzimidazoles, medicaments comprising said compound, their use and their method of manufacture |
| MX2010008202A (es) | 2008-01-28 | 2010-12-06 | Janssen Pharmaceutica Nv | Derivados de tio-2-aminoquinolina 6-sustituida utiles como inhibidores de beta-secretasa (bace). |
| RU2010136050A (ru) | 2008-01-29 | 2012-03-10 | Янссен Фармацевтика Нв (Be) | 2-аминохинолиновые производные для использования в качестве ингибиторов секретазы (васе) |
| WO2009103626A1 (en) | 2008-02-18 | 2009-08-27 | F. Hoffmann-La Roche Ag | 4, 5-dihydro-oxazol-2-yl amine derivatives |
| AU2009239536C1 (en) | 2008-04-22 | 2012-12-13 | Merck Sharp & Dohme Corp. | Phenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use |
| TWI431004B (zh) | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Bace抑制劑 |
| EP2305672B1 (en) | 2008-06-13 | 2019-03-27 | Shionogi & Co., Ltd. | SULFUR-CONTAINING HETEROCYCLIC DERIVATIVE HAVING ß-SECRETASE-INHIBITING ACTIVITY |
| ES2433223T3 (es) | 2008-07-28 | 2013-12-10 | Eisai R&D Management Co., Ltd. | Derivados de espiroaminodihidrotiazina |
| WO2010013302A1 (ja) | 2008-07-28 | 2010-02-04 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | スピロアミノジヒドロチアジン誘導体 |
| US8198269B2 (en) | 2008-09-30 | 2012-06-12 | Eisai R&D Management Co., Ltd. | Fused aminodihydrothiazine derivative |
| EP2360155A4 (en) | 2008-10-22 | 2012-06-20 | Shionogi & Co | 2-AMINOPYRIDIN-4-ON AND 2-AMINOPYRIDINE DERIVATIVE WITH BACE1-HEMDERING EFFECT |
| US20100125081A1 (en) | 2008-11-14 | 2010-05-20 | Astrazeneca Ab | New compounds 574 |
| EP2376083A4 (en) | 2008-11-20 | 2012-06-20 | Purdue Research Foundation | QUINAZOLIN-BASED BACE-1 INHIBITORS AND METHODS OF USE |
-
2006
- 2006-06-12 EP EP06784807.7A patent/EP1896478B1/en active Active
- 2006-06-12 BR BRPI0612072-5A patent/BRPI0612072A2/pt not_active IP Right Cessation
- 2006-06-12 TW TW098137006A patent/TW201004961A/zh unknown
- 2006-06-12 AU AU2006259572A patent/AU2006259572A1/en not_active Abandoned
- 2006-06-12 AR ARP060102461A patent/AR054617A1/es not_active Application Discontinuation
- 2006-06-12 US US11/451,541 patent/US7868000B2/en active Active
- 2006-06-12 MX MX2007016180A patent/MX2007016180A/es active IP Right Grant
- 2006-06-12 SG SG201004170-5A patent/SG162790A1/en unknown
- 2006-06-12 JP JP2008516997A patent/JP2008543849A/ja active Pending
- 2006-06-12 PE PE2006000655A patent/PE20070135A1/es not_active Application Discontinuation
- 2006-06-12 TW TW095120854A patent/TWI332005B/zh active
- 2006-06-12 KR KR1020077029300A patent/KR20080029965A/ko not_active Withdrawn
- 2006-06-12 WO PCT/US2006/022918 patent/WO2006138264A2/en not_active Ceased
- 2006-06-12 CA CA002609582A patent/CA2609582A1/en not_active Abandoned
- 2006-06-12 CN CNA2006800215030A patent/CN101228163A/zh active Pending
- 2006-06-12 RU RU2008100165/04A patent/RU2008100165A/ru not_active Application Discontinuation
-
2007
- 2007-12-02 IL IL187814A patent/IL187814A0/en unknown
- 2007-12-12 EC EC2007008003A patent/ECSP078003A/es unknown
-
2008
- 2008-01-11 NO NO20080187A patent/NO20080187L/no not_active Application Discontinuation
- 2008-03-05 JP JP2008055596A patent/JP2008201784A/ja not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| TW200716642A (en) | 2007-05-01 |
| CA2609582A1 (en) | 2006-12-28 |
| US20070060575A1 (en) | 2007-03-15 |
| US7868000B2 (en) | 2011-01-11 |
| JP2008201784A (ja) | 2008-09-04 |
| EP1896478B1 (en) | 2014-05-21 |
| TWI332005B (en) | 2010-10-21 |
| ECSP078003A (es) | 2008-01-23 |
| IL187814A0 (en) | 2008-08-07 |
| AU2006259572A1 (en) | 2006-12-28 |
| WO2006138264A3 (en) | 2007-03-01 |
| EP1896478A2 (en) | 2008-03-12 |
| BRPI0612072A2 (pt) | 2010-10-19 |
| RU2008100165A (ru) | 2009-07-20 |
| CN101228163A (zh) | 2008-07-23 |
| TW201004961A (en) | 2010-02-01 |
| MX2007016180A (es) | 2008-03-07 |
| KR20080029965A (ko) | 2008-04-03 |
| NO20080187L (no) | 2008-03-14 |
| JP2008543849A (ja) | 2008-12-04 |
| WO2006138264A2 (en) | 2006-12-28 |
| AR054617A1 (es) | 2007-07-04 |
| SG162790A1 (en) | 2010-07-29 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| PE20070135A1 (es) | Compuestos heterociclicos como inhibidores de aspartil proteasas | |
| PE20070138A1 (es) | Compuestos heterociclicos como inhibidores de aspartil proteasas | |
| PE20070321A1 (es) | Compuestos heterociclicos como inhibidores de proteasas | |
| PE20070798A1 (es) | Compuestos heterociclicos como inhibidores de aspartil proteasas | |
| PE20070115A1 (es) | Derivados de [1,3,5]-triazina como inhibidores de aspartil proteasas | |
| PE20070531A1 (es) | Compuestos heterociclicos como inhibidores de aspartil proteasas | |
| GT200600134A (es) | Compuestos novedosos de derivados de aminosulfonilo | |
| PE20080155A1 (es) | Compuestos heterociclicos como inhibidores de aspartil-proteasa | |
| PE20040164A1 (es) | Mimeticos de glucocorticoides, procedimientos para su preparacion y composiciones farmaceuticas | |
| ATE478044T1 (de) | Biphenylderivate und ihre verwendung bei der behandlung von hepatitis c | |
| PE20070018A1 (es) | Compuestos heterociclicos como inhibidores de aspartil proteasas | |
| AR053405A1 (es) | Derivados de urea sustituidas, composiciones farmaceuticas y metodos para el tratamiento de cardiopatias | |
| ATE433447T1 (de) | Pyrimiidinverbindungen | |
| AR072952A1 (es) | Compuestos de 2-imino-3-metilpirrolopirimidinona fenilo-sustituida como inhibidores de bace-1, composiciones y su uso | |
| NO20083598L (no) | Karbosykliske og heterosykliske arylsulfoner som inhibitorer av gamma-sekretase | |
| EA200500342A1 (ru) | Гетероциклические замещённые пиперазины для лечения шизофрении | |
| EA201100689A1 (ru) | N-сульфонилпирролы и их применение в качестве ингибиторов гистондезацетилазы | |
| AR033379A1 (es) | Compuestos de difenilurea, procedimiento para su preparacion y composiciones farmaceuticas que los contienen | |
| CR10974A (es) | Inhibidores de carboxipeptidasa b plasmatica (divisional) | |
| EA201170344A1 (ru) | Азаиндольные ингибиторы iap | |
| AR058347A1 (es) | Entidades quimias composiciones y metodos | |
| BRPI0610644B8 (pt) | composto e composição farmacêutica que compreende tal composto e um veículo ou diluente farmaceuticamente aceitável. | |
| EA200600605A1 (ru) | Перегруппированные пентанолы, способ их получения и их применение в качестве противовоспалительных средств | |
| ATE449776T1 (de) | Pyrroloä2,3-cüpyridinderivate | |
| ATE543803T1 (de) | 3-ä2-(3-azylamino-2-oxo-2h-pyridin-1- yl)acetylaminoü-4-oxopentansäurederivate und deren verwendung als caspase-inhibitoren |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration | ||
| FD | Application declared void or lapsed |