ECSP078003A - Inhibidores de aspartil proteasas - Google Patents
Inhibidores de aspartil proteasasInfo
- Publication number
- ECSP078003A ECSP078003A EC2007008003A ECSP078003A ECSP078003A EC SP078003 A ECSP078003 A EC SP078003A EC 2007008003 A EC2007008003 A EC 2007008003A EC SP078003 A ECSP078003 A EC SP078003A EC SP078003 A ECSP078003 A EC SP078003A
- Authority
- EC
- Ecuador
- Prior art keywords
- proteasas
- aspartil
- inhibitors
- compounds
- formula
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 208000010877 cognitive disease Diseases 0.000 abstract 2
- 230000001149 cognitive effect Effects 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 230000004770 neurodegeneration Effects 0.000 abstract 2
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 2
- 102000004580 Aspartic Acid Proteases Human genes 0.000 abstract 1
- 108010017640 Aspartic Acid Proteases Proteins 0.000 abstract 1
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 229940122041 Cholinesterase inhibitor Drugs 0.000 abstract 1
- 239000000556 agonist Substances 0.000 abstract 1
- 239000000544 cholinesterase inhibitor Substances 0.000 abstract 1
- 239000003683 muscarinic M2 receptor antagonist Substances 0.000 abstract 1
- 150000003839 salts Chemical class 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)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (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 revelan compuestos de fórmula I o su estereoisómero, tautómero o sal aceptable para uso farmacéutico, donde j, k, U, W, R, R1, R2, R3, R4, R6, R7 y R7a son según se describieron anteriormente en la memoria descriptiva.Además se revela el método para inhibir la aspartil proteasa, y en particular, los métodos para tratar enfermedades cardiovasculares, enfermedades cognitivas y neurodegenerativas. Además se revelan métodos para tratar enfermedades cognitivas y neurodegenerativas utilizando los compuestos de fórmula I en combinación con un inhibidor de colinesterasa o un agonista m1 o antagonista m2 muscarínico.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US69053705P | 2005-06-14 | 2005-06-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP078003A true ECSP078003A (es) | 2008-01-23 |
Family
ID=37114557
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EC2007008003A ECSP078003A (es) | 2005-06-14 | 2007-12-12 | 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)
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|---|---|---|---|---|
| GB0220581D0 (en) | 2002-09-04 | 2002-10-09 | Novartis Ag | Organic Compound |
| 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 |
| US7763609B2 (en) * | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| PE20060437A1 (es) | 2004-06-18 | 2006-06-08 | Novartis Ag | COMPUESTOS AZA-BICICLONONANOS COMO LIGANDOS COLINERGICOS DE nAChR |
| GB0415746D0 (en) | 2004-07-14 | 2004-08-18 | Novartis Ag | Organic compounds |
| SG162790A1 (en) | 2005-06-14 | 2010-07-29 | Schering 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 |
| ATE482214T1 (de) | 2005-06-14 | 2010-10-15 | Schering Corp | Aspartylproteasehemmer |
| GB0521508D0 (en) * | 2005-10-21 | 2005-11-30 | Novartis Ag | Organic compounds |
| ATE478070T1 (de) | 2005-10-27 | 2010-09-15 | Schering Corp | Heterozyklische aspartyl-proteasehemmer |
| GB0525673D0 (en) * | 2005-12-16 | 2006-01-25 | Novartis Ag | Organic compounds |
| GB0525672D0 (en) * | 2005-12-16 | 2006-01-25 | Novartis Ag | Organic compounds |
| US8168641B2 (en) * | 2006-06-12 | 2012-05-01 | Schering Corporation | Aspartyl protease inhibitors |
| TW200815349A (en) | 2006-06-22 | 2008-04-01 | Astrazeneca Ab | New compounds |
| MX2009006228A (es) * | 2006-12-12 | 2009-06-22 | Schering Corp | Inhibidores de aspartil proteasa. |
| CN101631779A (zh) * | 2006-12-12 | 2010-01-20 | 先灵公司 | 含有三环系统的天冬氨酰蛋白酶抑制剂 |
| TW200902499A (en) | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
| CN101848897A (zh) | 2007-09-06 | 2010-09-29 | 先灵公司 | γ分泌酶调节剂 |
| WO2009061699A1 (en) | 2007-11-05 | 2009-05-14 | Schering Corporation | Gamma secretase modulators |
| CA2708300A1 (en) | 2007-12-11 | 2009-06-18 | 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 |
| AU2009314049B2 (en) | 2008-11-13 | 2015-03-05 | Merck Sharp & Dohme Corp. | Gamma secretase modulators |
| TW201020244A (en) | 2008-11-14 | 2010-06-01 | Astrazeneca Ab | New compounds |
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| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
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| 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 |
| SG191710A1 (en) | 2011-01-21 | 2013-08-30 | Eisai R&D Man Co Ltd | Methods and compounds useful in the synthesis of fused aminodihydrothiazine derivatives |
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| EP2694489B1 (en) | 2011-04-07 | 2017-09-06 | Merck Sharp & Dohme Corp. | C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| US9145426B2 (en) | 2011-04-07 | 2015-09-29 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use |
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| CN104270945B (zh) | 2012-03-19 | 2017-03-29 | 巴克老龄化研究所 | App特异性bace抑制剂(asbi)及其用途 |
| JO3143B1 (ar) | 2012-04-03 | 2017-09-20 | Lilly Co Eli | مركبات تتراهيدرو بيرولو ثيازين |
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| US9000184B2 (en) | 2012-06-20 | 2015-04-07 | Astrazeneca Ab | Cyclohexane-1,2′-naphthalene-1′,2″-imidazol compounds and their use as BACE inhibitors |
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| US9000185B2 (en) | 2012-06-20 | 2015-04-07 | Astrazeneca Ab | Cycloalkyl ether compounds and their use as BACE inhibitors |
| US10548882B2 (en) | 2012-06-21 | 2020-02-04 | Astrazeneca Ab | Camsylate salt |
| EP2908824B1 (en) | 2012-10-17 | 2018-05-02 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
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| HUE031764T2 (en) | 2012-10-26 | 2017-07-28 | Lilly Co Eli | Tetrahydropyrrolothiazine derivatives as BACE inhibitors |
| WO2014099788A1 (en) | 2012-12-21 | 2014-06-26 | Merck Sharp & Dohme Corp. | C5-spiro iminothiadiazine dioxides as bace inhibitors |
| CA2899938C (en) | 2013-02-12 | 2021-10-19 | Buck Institute For Research On Aging | Hydantoins that modulate bace-mediated app processing |
| 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 |
| JO3318B1 (ar) | 2013-06-18 | 2019-03-13 | Lilly Co Eli | مثبطات bace |
| US9745324B2 (en) | 2013-12-18 | 2017-08-29 | 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 |
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-
2006
- 2006-06-12 SG SG201004170-5A patent/SG162790A1/en unknown
- 2006-06-12 PE PE2006000655A patent/PE20070135A1/es not_active Application Discontinuation
- 2006-06-12 MX MX2007016180A patent/MX2007016180A/es active IP Right Grant
- 2006-06-12 US US11/451,541 patent/US7868000B2/en active Active
- 2006-06-12 WO PCT/US2006/022918 patent/WO2006138264A2/en not_active Ceased
- 2006-06-12 JP JP2008516997A patent/JP2008543849A/ja active Pending
- 2006-06-12 EP EP06784807.7A patent/EP1896478B1/en active Active
- 2006-06-12 AR ARP060102461A patent/AR054617A1/es not_active Application Discontinuation
- 2006-06-12 CA CA002609582A patent/CA2609582A1/en not_active Abandoned
- 2006-06-12 TW TW098137006A patent/TW201004961A/zh unknown
- 2006-06-12 KR KR1020077029300A patent/KR20080029965A/ko not_active Withdrawn
- 2006-06-12 BR BRPI0612072-5A patent/BRPI0612072A2/pt not_active IP Right Cessation
- 2006-06-12 RU RU2008100165/04A patent/RU2008100165A/ru not_active Application Discontinuation
- 2006-06-12 AU AU2006259572A patent/AU2006259572A1/en not_active Abandoned
- 2006-06-12 TW TW095120854A patent/TWI332005B/zh active
- 2006-06-12 CN CNA2006800215030A patent/CN101228163A/zh active Pending
-
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 |
|---|---|
| CN101228163A (zh) | 2008-07-23 |
| CA2609582A1 (en) | 2006-12-28 |
| NO20080187L (no) | 2008-03-14 |
| AU2006259572A1 (en) | 2006-12-28 |
| KR20080029965A (ko) | 2008-04-03 |
| TW200716642A (en) | 2007-05-01 |
| WO2006138264A2 (en) | 2006-12-28 |
| RU2008100165A (ru) | 2009-07-20 |
| EP1896478B1 (en) | 2014-05-21 |
| US20070060575A1 (en) | 2007-03-15 |
| US7868000B2 (en) | 2011-01-11 |
| MX2007016180A (es) | 2008-03-07 |
| WO2006138264A3 (en) | 2007-03-01 |
| TW201004961A (en) | 2010-02-01 |
| IL187814A0 (en) | 2008-08-07 |
| JP2008201784A (ja) | 2008-09-04 |
| BRPI0612072A2 (pt) | 2010-10-19 |
| TWI332005B (en) | 2010-10-21 |
| EP1896478A2 (en) | 2008-03-12 |
| JP2008543849A (ja) | 2008-12-04 |
| PE20070135A1 (es) | 2007-03-09 |
| SG162790A1 (en) | 2010-07-29 |
| AR054617A1 (es) | 2007-07-04 |
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