PE20080155A1 - Compuestos heterociclicos como inhibidores de aspartil-proteasa - Google Patents
Compuestos heterociclicos como inhibidores de aspartil-proteasaInfo
- Publication number
- PE20080155A1 PE20080155A1 PE2007000708A PE2007000708A PE20080155A1 PE 20080155 A1 PE20080155 A1 PE 20080155A1 PE 2007000708 A PE2007000708 A PE 2007000708A PE 2007000708 A PE2007000708 A PE 2007000708A PE 20080155 A1 PE20080155 A1 PE 20080155A1
- Authority
- PE
- Peru
- Prior art keywords
- heterocyclic compounds
- aspartile
- cycloalkyl
- alkylene
- alkyl
- Prior art date
Links
- 150000002391 heterocyclic compounds Chemical class 0.000 title abstract 2
- 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 title 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 229940125373 Gamma-Secretase Inhibitor Drugs 0.000 abstract 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 abstract 1
- 239000003540 gamma secretase inhibitor Substances 0.000 abstract 1
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 abstract 1
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/20—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
-
- 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
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- 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
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D405/04—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 directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D411/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
- C07D411/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D411/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D495/20—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Virology (AREA)
- Hospice & Palliative Care (AREA)
- AIDS & HIV (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Molecular Biology (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
SE REFIERE A COMPUESTOS HETEROCICLICOS DE FORMULA (I) DONDE W ES UN ENLACE, C(=S), S(O), S(O)2, C(=O), ENTRE OTROS; X ES O, N(R5) O C(R6)(R7); U ES UN ENLACE O (C(R3)(R4))b, DONDE b ES 1 O 2; R1, R2 Y R5 SON CADA UNO H, ALQUILO(C1-C20), CICLOALQUILO(C3-C15), ALQUINILO(C2-C15), CN, ENTRE OTROS; R3, R4 Y R6 SON CADA UNO H, ALQUILO(C1-C20), CICLOALQUILO(C3-C15), ALQUENILO(C2-C15), ARILO(C6-C14), ENTRE OTROS; R7 ES ALQUILENO(C1-C20), CICLOALQUILENO(C3-C15), ALQUENILENO(C2-C15), ARILENO(C6-C14), ENTRE OTROS; R30 ES ALQUILENO(C1-C20), CICLOALQUILENO(C3-C15), ALQUINILENO(C2-C15), ARILENO(C6-C14), ENTRE OTROS; R31 ES UN COMPUESTO DE FORMULA (i) O (ii) DONDE T ES UN ENLACE, O-((C(R23)(R23)), S-((C(R23)(R23)), ENTRE OTROS; R23 ES H, ALQUILO(C1-C20), CICLOALQUILO(C3-C15), ALQUENILO(C2-C15), ENTRE OTROS. SON COMPUESTOS PREFERIDOS LOS COMPUESTOS DE FORMULA (a), (b), ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA QUE OPCIONALMENTE CONTIENE UN INHIBIDOR GAMMA SECRETASA, UN INHIBIDOR DE HMG-CoA REDUCTASA, UN AGENTE ANTIINFLAMATORIO NO ESTEROIDE, ENTRE OTROS. DICHOS COMPUESTOS SON INHIBIDORES DE ASPARTIL-PROTEASA SIENDO UTILES EN EL TRATAMIENTO DE LA ENFERMEDAD DE ALZHEIMER
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US81274406P | 2006-06-12 | 2006-06-12 |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20080155A1 true PE20080155A1 (es) | 2008-03-10 |
Family
ID=38713565
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2007000708A PE20080155A1 (es) | 2006-06-12 | 2007-06-07 | Compuestos heterociclicos como inhibidores de aspartil-proteasa |
Country Status (18)
Country | Link |
---|---|
US (2) | US8168641B2 (es) |
EP (2) | EP2644600B1 (es) |
JP (1) | JP2009539983A (es) |
KR (1) | KR20090015967A (es) |
CN (1) | CN101484429A (es) |
AR (1) | AR061264A1 (es) |
AU (1) | AU2007258435A1 (es) |
BR (1) | BRPI0712780A2 (es) |
CA (1) | CA2653650A1 (es) |
CL (1) | CL2007001674A1 (es) |
EC (1) | ECSP088959A (es) |
IL (1) | IL195592A0 (es) |
MX (1) | MX2008015956A (es) |
NO (1) | NO20090144L (es) |
PE (1) | PE20080155A1 (es) |
RU (1) | RU2009100074A (es) |
TW (1) | TW200815365A (es) |
WO (1) | WO2007146225A2 (es) |
Families Citing this family (72)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
US7700603B2 (en) | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
CN101228163A (zh) * | 2005-06-14 | 2008-07-23 | 先灵公司 | 天冬氨酰蛋白酶抑制剂 |
WO2006138265A2 (en) | 2005-06-14 | 2006-12-28 | Schering Corporation | Heterocyclic aspartyl protease inhibitors, preparation and use thereof |
CN101198609A (zh) | 2005-06-14 | 2008-06-11 | 先灵公司 | 天冬氨酰基蛋白酶抑制剂 |
RU2416603C9 (ru) | 2005-10-25 | 2012-06-20 | Сионоги Энд Ко., Лтд. | Производные аминодигидротиазина |
EP2644600B1 (en) | 2006-06-12 | 2017-01-11 | Merck Sharp & Dohme Corp. | Heterocyclic aspartyl protease inhibitors |
TW200815349A (en) | 2006-06-22 | 2008-04-01 | Astrazeneca Ab | New compounds |
US20100016341A1 (en) * | 2006-12-12 | 2010-01-21 | Zhaoning Zhu | Aspartyl protease inhibitors containing a tricyclic ring system |
US8093254B2 (en) | 2006-12-12 | 2012-01-10 | Schering Corporation | Aspartyl protease inhibitors |
US8653067B2 (en) | 2007-04-24 | 2014-02-18 | Shionogi & Co., Ltd. | Pharmaceutical composition for treating Alzheimer's disease |
AU2008245082B8 (en) | 2007-04-24 | 2012-09-13 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives substituted with a cyclic group |
TW200902499A (en) | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
JP2011503002A (ja) | 2007-11-05 | 2011-01-27 | シェーリング コーポレイション | γセクレターゼ調節剤 |
AR072952A1 (es) * | 2008-04-22 | 2010-10-06 | Schering Corp | Compuestos de 2-imino-3-metilpirrolopirimidinona fenilo-sustituida como inhibidores de bace-1, composiciones y su uso |
CN102119161B (zh) | 2008-06-13 | 2015-07-08 | 盐野义制药株式会社 | 具有β分泌酶抑制作用的含硫杂环衍生物 |
US8450308B2 (en) * | 2008-08-19 | 2013-05-28 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
ES2459195T3 (es) * | 2008-09-11 | 2014-05-08 | Amgen Inc. | Compuestos de anillo espiro-tetracíclico como moduladores de beta-secretasa y métodos de uso |
US8703785B2 (en) | 2008-10-22 | 2014-04-22 | Shionogi & Co., Ltd. | 2-aminopyrimidin-4-one and 2-aminopyridine derivatives both having BACE1-inhibiting activity |
TW201020244A (en) | 2008-11-14 | 2010-06-01 | Astrazeneca Ab | New compounds |
CA2753730C (en) | 2009-03-13 | 2020-12-22 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
GB0912777D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydropyrimidone derivatives |
GB0912778D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydro-oxazine derivatives |
AU2013234424B9 (en) * | 2009-10-08 | 2014-07-03 | Merck Sharp & Dohme Llc | Iminothiadiazine dioxide compounds as BACE inhibitors, compositions, and their use |
EP2485591B1 (en) * | 2009-10-08 | 2016-03-23 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
WO2011044185A2 (en) * | 2009-10-08 | 2011-04-14 | Schering Corporation | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
UA108363C2 (uk) * | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
US8557826B2 (en) | 2009-10-08 | 2013-10-15 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions, and their use |
EP2511268B2 (en) | 2009-12-11 | 2021-02-17 | Shionogi & Co., Ltd. | Oxazine derivative |
US8889703B2 (en) | 2010-02-24 | 2014-11-18 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
JP2013522305A (ja) | 2010-03-15 | 2013-06-13 | アムジエン・インコーポレーテツド | β−セクレターゼ調節剤としてのスピロ−四環式環化合物 |
EP2547686B1 (en) | 2010-03-15 | 2014-01-22 | Amgen Inc. | Amino-dihydrooxazine and amino-dihydrothiazine spiro compounds as beta-secretase modulators and their medical use |
US8921363B2 (en) | 2010-08-05 | 2014-12-30 | Amgen Inc. | Derivatives of 1 H-isoindol-3-amine, 1 H-iso-aza-indol-3amine, 3,4-dihydroisoquinolin-1-amine, and 1,4-dihydroisoquinolin-3-amine as beta-secretase inhibitors |
WO2012057248A1 (ja) | 2010-10-29 | 2012-05-03 | 塩野義製薬株式会社 | ナフチリジン誘導体 |
EP2634188A4 (en) | 2010-10-29 | 2014-05-07 | Shionogi & Co | FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE |
US8957083B2 (en) | 2010-11-23 | 2015-02-17 | Amgen Inc. | Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use |
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 |
EP2673279A1 (en) | 2011-02-07 | 2013-12-18 | Amgen Inc. | 5-amino-oxazepine and 5-amino-thiazepane compounds as beta-secretase antagonists and methods of use |
WO2012112462A1 (en) | 2011-02-15 | 2012-08-23 | Amgen Inc. | Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of 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 |
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 |
WO2012139425A1 (en) | 2011-04-13 | 2012-10-18 | Schering Corporation | 5-substituted iminothiazines and their mono-and dioxides as bace inhibitors,compositions,and their use |
TW201247635A (en) | 2011-04-26 | 2012-12-01 | Shionogi & Co | Oxazine derivatives and a pharmaceutical composition for inhibiting BAC1 containing them |
BR112014004181A2 (pt) | 2011-08-22 | 2017-06-13 | Merck Sharp & Dohme | composto, composição farmacêutica, e, método de tratamento, prevenção, e / ou retardo do início de uma doença ou patologia |
WO2013044092A1 (en) | 2011-09-21 | 2013-03-28 | Amgen Inc. | Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
TWI557112B (zh) | 2012-03-05 | 2016-11-11 | 百靈佳殷格翰國際股份有限公司 | β-分泌酶抑制劑 |
CN106902108B (zh) | 2012-03-19 | 2020-07-21 | 巴克老龄化研究所 | App特异性bace抑制剂(asbi)及其用途 |
US10548882B2 (en) * | 2012-06-21 | 2020-02-04 | Astrazeneca Ab | Camsylate salt |
TW201422592A (zh) | 2012-08-27 | 2014-06-16 | Boehringer Ingelheim Int | β-分泌酶抑制劑 |
EP2900650A1 (en) | 2012-09-28 | 2015-08-05 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
EP2908825B1 (en) | 2012-10-17 | 2018-04-18 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
EP2908824B1 (en) | 2012-10-17 | 2018-05-02 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
WO2014065434A1 (en) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
US9725469B2 (en) | 2012-11-15 | 2017-08-08 | Amgen, Inc. | Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
CN104870000A (zh) | 2012-12-20 | 2015-08-26 | 默沙东公司 | 作为bace抑制剂的c5,c6氧杂环稠合的亚胺基噻嗪二氧化物化合物,组合物及其用途 |
US9489013B2 (en) | 2012-12-20 | 2016-11-08 | Merck Sharp & Dohme Corp. | C6-azaspiro iminothiadiazine dioxides as bace inhibitors, compositions, and their use |
EP2934149B1 (en) * | 2012-12-20 | 2019-02-06 | Merck Sharp & Dohme Corp. | C6-azaspiro iminothiadiazine dioxides as bace inhibitors |
US9580396B2 (en) | 2012-12-21 | 2017-02-28 | Merck Sharp & Dohme Corp. | C6-spiro iminothiadiazine dioxides as BACE inhibitors, compositions, and their use |
US10202355B2 (en) | 2013-02-12 | 2019-02-12 | Buck Institute For Research On Aging | Hydantoins that modulate bace-mediated app processing |
CA2902080A1 (en) | 2013-02-25 | 2014-08-28 | Merck Patent Gmbh | 2-amino-3,4-dihydroquinazoline derivatives and the use thereof as cathepsin d inhibitors |
EP3082823B1 (en) | 2013-12-18 | 2020-04-22 | Merck Sharp & Dohme Corp. | Iminothiadiazepane dioxide compounds as bace inhibitors, compositions, and their use |
WO2015094930A1 (en) | 2013-12-18 | 2015-06-25 | Merck Sharp & Dohme Corp. | C-6 spirocarbocyclic iminothiadiazine dioxides as bace inhibitors, compositions, and their use |
ES2942308T3 (es) | 2015-04-21 | 2023-05-31 | Allgenesis Biotherapeutics Inc | Compuestos y su uso como inhibidores de BACE1 |
ES2811329T3 (es) * | 2015-11-25 | 2021-03-11 | UCB Biopharma SRL | Derivados de iminotetrahidropirimidinona como inhibidores de plasmepsina V |
CN105646466A (zh) * | 2016-01-27 | 2016-06-08 | 上海宣创生物科技有限公司 | 一种杂环天冬氨基蛋白酶抑制剂的b晶型及其制备方法 |
CN105541820A (zh) * | 2016-01-27 | 2016-05-04 | 上海宣创生物科技有限公司 | 一种杂环天冬氨基蛋白酶抑制剂的c晶型及其制备方法 |
CN105524054A (zh) * | 2016-01-27 | 2016-04-27 | 上海宣创生物科技有限公司 | 一种杂环天冬氨基蛋白酶抑制剂的a晶型及其制备方法 |
EP3416647A4 (en) | 2016-02-18 | 2019-10-23 | Merck Sharp & Dohme Corp. | N3-SUBSTITUTED IMINOPYRIMIDINONE AS ANTIMALARIAMIDAL |
AU2019387370A1 (en) | 2018-11-30 | 2021-06-10 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
Family Cites Families (72)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6492408B1 (en) | 1999-07-21 | 2002-12-10 | Boehringer Ingelheim Pharmaceuticals, Inc. | Small molecules useful in the treatment of inflammatory disease |
CA2416906A1 (en) | 2000-08-09 | 2002-02-14 | 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 |
US6673821B2 (en) | 2001-10-22 | 2004-01-06 | Enanta Pharmaceuticals, Inc. | Nitrogen heterocycle inhibitors of aspartyl protease |
CN1863797A (zh) | 2003-08-08 | 2006-11-15 | 先灵公司 | 具有苯甲酰胺取代基的环胺bace-1抑制剂 |
MXPA06001558A (es) | 2003-08-08 | 2006-05-15 | Schering Corp | Inhibidores de amina ciclica bace-1 que poseen un sustituyente heterociclico. |
RU2405774C9 (ru) * | 2003-12-15 | 2011-03-20 | Шеринг Корпорейшн | Гетероциклические ингибиторы аспартилпротеазы |
US7592348B2 (en) * | 2003-12-15 | 2009-09-22 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
EP1740573A1 (en) | 2004-04-22 | 2007-01-10 | Eli Lilly And Company | Amides as bace inhibitors |
CN1968945A (zh) * | 2004-06-16 | 2007-05-23 | 惠氏公司 | 用于抑制β分泌酶的氨基-5,5-二苯基咪唑酮衍生物 |
DE602005025363D1 (de) | 2004-07-22 | 2011-01-27 | Schering Corp | Substituierte amide als inhibitoren der beta-sekretase |
DE602005007245D1 (es) | 2004-07-28 | 2008-07-10 | Schering Corp | |
ES2403185T3 (es) | 2004-08-06 | 2013-05-16 | Janssen Pharmaceutica N.V. | Nuevos derivados de 2-amino-quinazolina útiles como inhibidores de ss-secretasa (BACE) |
ATE482936T1 (de) | 2004-08-06 | 2010-10-15 | Janssen Pharmaceutica Nv | Als b-sekretase (bace)-hemmer nützliche 2-amino- chinazolinderivate |
US8436006B2 (en) | 2004-08-06 | 2013-05-07 | Jansssen Pharmaceutica N.V. | 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE) |
WO2006023774A2 (en) * | 2004-08-20 | 2006-03-02 | Imquest Biosciences, Inc. | Plasma or serum fraction for treatment and prevention of viral infections and related conditions |
EP1802587A4 (en) * | 2004-10-15 | 2010-02-17 | Astrazeneca Ab | SUBSTITUTED AMINO BINDINGS AND THEIR APPLICATIONS |
US20090062282A1 (en) | 2004-10-15 | 2009-03-05 | Astrazeneca Ab | Substituted Amino-Pyrimidones and Uses Thereof |
EP2264036A1 (en) | 2005-01-14 | 2010-12-22 | Wyeth LLC (Formerly Known As Wyeth) | Amino-imidazolones for the inhibition of beta-secretase |
CN101228163A (zh) * | 2005-06-14 | 2008-07-23 | 先灵公司 | 天冬氨酰蛋白酶抑制剂 |
CA2610829A1 (en) | 2005-06-14 | 2006-12-28 | Schering Corporation | The preparation and use of compounds as aspartyl protease inhibitors |
AR053902A1 (es) | 2005-06-14 | 2007-05-23 | Schering Corp | Inhibidores de aspartil proteasa heterociclicos macrociclicos |
WO2006138265A2 (en) | 2005-06-14 | 2006-12-28 | Schering Corporation | Heterocyclic aspartyl protease inhibitors, preparation and use thereof |
CA2610617A1 (en) | 2005-06-14 | 2006-12-28 | Schering Corporation | The preparation and use of protease inhibitors |
CN101198609A (zh) | 2005-06-14 | 2008-06-11 | 先灵公司 | 天冬氨酰基蛋白酶抑制剂 |
US7759353B2 (en) * | 2005-06-14 | 2010-07-20 | Schering Corporation | Substituted spiro iminopyrimidinones as aspartyl protease inhibitors, compositions, and methods of treatment |
TW200738683A (en) | 2005-06-30 | 2007-10-16 | Wyeth Corp | Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation |
AU2006266167A1 (en) | 2005-06-30 | 2007-01-11 | Wyeth | Amino-5-(6-membered)heteroarylimidazolone compounds and the use thereof for beta-secretase modulation |
TW200730523A (en) | 2005-07-29 | 2007-08-16 | Wyeth Corp | Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation |
JP2009509957A (ja) | 2005-09-26 | 2009-03-12 | ワイス | β−セクレターゼ阻害剤としてのアミノ−5−[4−(ジフルオロメトキシ)フェニル]−5−フェニルイミダゾロン化合物 |
RU2416603C9 (ru) | 2005-10-25 | 2012-06-20 | Сионоги Энд Ко., Лтд. | Производные аминодигидротиазина |
WO2007050612A1 (en) | 2005-10-25 | 2007-05-03 | Janssen Pharmaceutica N.V. | 2-amino-3,4-dihydro-pyrido[3,4-d]pyrimidine derivatives useful as inhibitors of beta-secretase (bace) |
DE602006016314D1 (de) | 2005-10-27 | 2010-09-30 | Schering Corp | Heterozyklische aspartyl-proteasehemmer |
CN101351460A (zh) | 2005-10-31 | 2009-01-21 | 先灵公司 | 天冬氨酰蛋白酶抑制剂 |
AR058381A1 (es) | 2005-12-19 | 2008-01-30 | Astrazeneca Ab | Compuestos derivados de 2-aminopiridin-4-onas y una composicion farmaceutica |
WO2007078813A2 (en) * | 2005-12-19 | 2007-07-12 | Wyeth | 2-AMINO-5-PIPERIDINYLIMIDAZOLONE COMPOUNDS AND USE THEREOF FOR β-SECRETASE MODULATION |
US7932261B2 (en) | 2006-02-06 | 2011-04-26 | Janssen Pharmaceutica Nv | Macrocycle derivatives useful as inhibitors of β-secretase (BACE) |
WO2007092854A2 (en) | 2006-02-06 | 2007-08-16 | Janssen Pharmaceutica N.V. | 2-AMINO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE) |
US7776882B2 (en) | 2006-02-06 | 2010-08-17 | Baxter Ellen W | 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 |
EP2004630A4 (en) | 2006-04-05 | 2010-05-19 | Astrazeneca Ab | 2-AMINOPYRIMIDIN-4-ONES AND THEIR USE FOR THE TREATMENT OR PREVENTION OF PATHOLOGIES RELATED TO PROTEIN A |
EP2644600B1 (en) | 2006-06-12 | 2017-01-11 | Merck Sharp & Dohme Corp. | Heterocyclic aspartyl protease inhibitors |
TW200815447A (en) | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds IV |
TW200815449A (en) | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds II |
US20080051420A1 (en) | 2006-06-14 | 2008-02-28 | Astrazeneca Ab | New Compounds 317 |
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 |
US8093254B2 (en) | 2006-12-12 | 2012-01-10 | Schering Corporation | Aspartyl protease inhibitors |
US20100016341A1 (en) | 2006-12-12 | 2010-01-21 | Zhaoning Zhu | Aspartyl protease inhibitors containing a tricyclic ring system |
TW200831484A (en) | 2006-12-20 | 2008-08-01 | Astrazeneca Ab | New compounds |
AU2008245082B8 (en) | 2007-04-24 | 2012-09-13 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives substituted with a cyclic group |
US8653067B2 (en) | 2007-04-24 | 2014-02-18 | Shionogi & Co., Ltd. | Pharmaceutical composition for treating Alzheimer's disease |
TW200902499A (en) | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
TW200902503A (en) | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
WO2009005471A1 (en) | 2007-07-05 | 2009-01-08 | Astrazeneca Ab | Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors |
WO2009005470A1 (en) | 2007-07-05 | 2009-01-08 | Astrazeneca Ab | Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors |
JP5450407B2 (ja) | 2007-07-06 | 2014-03-26 | 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 | 置換アミノ−キナゾリノン、前記化合物を含む薬物、それらの使用及び製造方法 |
WO2009091016A1 (ja) | 2008-01-18 | 2009-07-23 | Eisai R & D Management Co., Ltd. | 縮合アミノジヒドロチアジン誘導体 |
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 |
BRPI0906625A2 (pt) | 2008-01-28 | 2015-07-14 | Janssen Pharmaceutica Nv | Derivados de tio-2-amino-quinolina-6-substituída úteis como inibidores da beta-secretase (bace) |
US7786116B2 (en) | 2008-01-29 | 2010-08-31 | Janssen Pharmaceutica N.V. | 2-amino-quinoline derivatives useful as inhibitors of β-secretase (BACE) |
CN101952260B (zh) | 2008-02-18 | 2013-02-13 | 弗·哈夫曼-拉罗切有限公司 | 4,5-二氢-*唑-2-基胺衍生物 |
AU2009217518A1 (en) | 2008-02-28 | 2009-09-03 | Merck Sharp & Dohme Corp. | 2-aminoimidazole beta-secretase inhibitors for the treatment of Alzheimer's disease |
AR072952A1 (es) | 2008-04-22 | 2010-10-06 | Schering Corp | Compuestos de 2-imino-3-metilpirrolopirimidinona fenilo-sustituida como inhibidores de bace-1, composiciones y su uso |
TWI431004B (zh) | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Bace抑制劑 |
CN102119161B (zh) | 2008-06-13 | 2015-07-08 | 盐野义制药株式会社 | 具有β分泌酶抑制作用的含硫杂环衍生物 |
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 |
AU2009277485B2 (en) | 2008-07-28 | 2013-05-02 | Eisai R&D Management Co., Ltd. | Spiroaminodihydrothiazine derivatives |
US8198269B2 (en) | 2008-09-30 | 2012-06-12 | Eisai R&D Management Co., Ltd. | Fused aminodihydrothiazine derivative |
US8703785B2 (en) | 2008-10-22 | 2014-04-22 | Shionogi & Co., Ltd. | 2-aminopyrimidin-4-one and 2-aminopyridine derivatives both having BACE1-inhibiting activity |
WO2010056194A1 (en) | 2008-11-14 | 2010-05-20 | Astrazeneca Ab | 5h-pyrrolo [ 3, 4-b] pyridin derivatives and their use |
US8394807B2 (en) | 2008-11-20 | 2013-03-12 | Purdue Research Foundation | Quinazoline inhibitors of BACE 1 and methods of using |
-
2007
- 2007-06-07 EP EP13163216.8A patent/EP2644600B1/en active Active
- 2007-06-07 CA CA002653650A patent/CA2653650A1/en not_active Abandoned
- 2007-06-07 AR ARP070102455A patent/AR061264A1/es not_active Application Discontinuation
- 2007-06-07 RU RU2009100074/04A patent/RU2009100074A/ru not_active Application Discontinuation
- 2007-06-07 US US11/759,336 patent/US8168641B2/en active Active
- 2007-06-07 EP EP07795971A patent/EP2032542A2/en not_active Withdrawn
- 2007-06-07 WO PCT/US2007/013684 patent/WO2007146225A2/en active Application Filing
- 2007-06-07 PE PE2007000708A patent/PE20080155A1/es not_active Application Discontinuation
- 2007-06-07 KR KR1020087030210A patent/KR20090015967A/ko not_active Withdrawn
- 2007-06-07 AU AU2007258435A patent/AU2007258435A1/en not_active Abandoned
- 2007-06-07 BR BRPI0712780-4A patent/BRPI0712780A2/pt not_active Application Discontinuation
- 2007-06-07 CN CNA2007800218527A patent/CN101484429A/zh active Pending
- 2007-06-07 JP JP2009515439A patent/JP2009539983A/ja active Pending
- 2007-06-07 MX MX2008015956A patent/MX2008015956A/es not_active Application Discontinuation
- 2007-06-08 TW TW096120821A patent/TW200815365A/zh unknown
- 2007-06-08 CL CL2007001674A patent/CL2007001674A1/es unknown
-
2008
- 2008-11-27 IL IL195592A patent/IL195592A0/en unknown
- 2008-12-11 EC EC2008008959A patent/ECSP088959A/es unknown
-
2009
- 2009-01-09 NO NO20090144A patent/NO20090144L/no not_active Application Discontinuation
-
2012
- 2012-03-15 US US13/421,396 patent/US8629155B2/en active Active
Also Published As
Publication number | Publication date |
---|---|
NO20090144L (no) | 2009-03-04 |
WO2007146225A2 (en) | 2007-12-21 |
IL195592A0 (en) | 2009-09-01 |
US20070287692A1 (en) | 2007-12-13 |
WO2007146225A3 (en) | 2008-03-06 |
EP2032542A2 (en) | 2009-03-11 |
US8629155B2 (en) | 2014-01-14 |
US20120232064A1 (en) | 2012-09-13 |
RU2009100074A (ru) | 2010-07-20 |
JP2009539983A (ja) | 2009-11-19 |
EP2644600B1 (en) | 2017-01-11 |
MX2008015956A (es) | 2009-01-09 |
TW200815365A (en) | 2008-04-01 |
ECSP088959A (es) | 2009-01-30 |
AU2007258435A1 (en) | 2007-12-21 |
US8168641B2 (en) | 2012-05-01 |
EP2644600A1 (en) | 2013-10-02 |
CA2653650A1 (en) | 2007-12-21 |
CN101484429A (zh) | 2009-07-15 |
AR061264A1 (es) | 2008-08-13 |
BRPI0712780A2 (pt) | 2012-09-11 |
KR20090015967A (ko) | 2009-02-12 |
CL2007001674A1 (es) | 2008-01-18 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
PE20080155A1 (es) | Compuestos heterociclicos como inhibidores de aspartil-proteasa | |
PE20070135A1 (es) | Compuestos heterociclicos como inhibidores de aspartil proteasas | |
PE20070138A1 (es) | Compuestos heterociclicos como inhibidores de aspartil proteasas | |
PE20060488A1 (es) | Compuestos heterociclicos como inhibidores de aspartil proteasa | |
GT200600134A (es) | Compuestos novedosos de derivados de aminosulfonilo | |
PE20050729A1 (es) | Aminas ciclicas sustituidas por bezamida o piridin-carboxamida como inhibidores de bace-1 | |
ES2182535T3 (es) | Derivados de benzo(b)tiepina-1,-dioxido, procedimiento para su preparacion, medicamentos que contienen estos compuestos y su utilizacion. | |
ECSP12006640A (es) | Inhibidores heterocíclicos de aspartil proteasa | |
PE20061325A1 (es) | Derivados de pirrolidina como inhibidores de la renina | |
PE20070073A1 (es) | Compuestos heterociclicos como inhibidores de proteasas | |
PE20080234A1 (es) | Combinacion antiepileptica que comprende derivados de benzoheteroarilsulfamidas | |
UY27777A1 (es) | Inhibidores de metaloproteinasa de heteroariloxi-aril-espiro-pirimidina-2,4,6-triona n-sustituida | |
UY27774A1 (es) | Inhibidores de metaloproteinas de triaril-oxi-aril-espiropirimidina-2,4,6-triona | |
SV2009003152A (es) | Derivados novedosos de aminopiridina que tiene accion inhibidora selectiva sobre aurora a | |
GT200700036A (es) | Compuestos fenil amido heterociclicos condensados | |
PE20090042A1 (es) | Analogos de ciclopamina | |
CL2011000159A1 (es) | Compuestos derivados de 1,3-oxazin-2-ona, inhibidores de 11beta-hsd1; composicion farmaceutica que los comprende; y su uso en el tratamiento de la diabetes. | |
PE20090365A1 (es) | Imidazopirazinas como inhibidores de proteina quinasa | |
CO6190626A2 (es) | Compuestos y composiciones como inhibidores de proteasa activadora de canal | |
AR072166A1 (es) | Derivado de piperidina y su uso como inhibidor de renina superior | |
DOP2006000045A (es) | Derivados del (1,5-difenil-1h-pirazol-3-il oxadiazol, su preparacion y su aplicacion en terapeutica | |
ECSP088484A (es) | Derivados de quinazolina espirocíclicos como inhibidores de pde7 | |
CO5080735A1 (es) | Agonistas de prostaglandinas | |
AR074053A1 (es) | Derivados de anilina-pirimidina sustituidos con sulfoximina como inhibidores de quinasas dependientes de ciclina (cdk), y composiciones farmaceuticas que los contienen | |
ATE501103T1 (de) | Organische verbindungen |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
FC | Refusal |