MX2009006228A - Inhibidores de aspartil proteasa. - Google Patents
Inhibidores de aspartil proteasa.Info
- Publication number
- MX2009006228A MX2009006228A MX2009006228A MX2009006228A MX2009006228A MX 2009006228 A MX2009006228 A MX 2009006228A MX 2009006228 A MX2009006228 A MX 2009006228A MX 2009006228 A MX2009006228 A MX 2009006228A MX 2009006228 A MX2009006228 A MX 2009006228A
- Authority
- MX
- Mexico
- Prior art keywords
- sup
- formula
- disclosed
- aspartyl protease
- protease inhibitors
- Prior art date
Links
- 239000003696 aspartic proteinase 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
- 239000000544 cholinesterase inhibitor Substances 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000000359 muscarinic M1 receptor agonist Substances 0.000 abstract 1
- 239000003683 muscarinic M2 receptor antagonist Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/14—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
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
-
- 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
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
- A61P33/06—Antimalarials
-
- 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
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Cardiology (AREA)
- Biomedical Technology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Virology (AREA)
- Neurosurgery (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- AIDS & HIV (AREA)
- Psychiatry (AREA)
- Ophthalmology & Optometry (AREA)
- Molecular Biology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Enzymes And Modification Thereof (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Se describen compuestos de la fórmula I: (ver fórmula (I)) o un estereoisómero, tautómero, o un solvato o una sal aceptable farmacéuticamente de dichos compuestos, donde: R1, R2, R3, R4, R14, V, W, X, Y, Z, p y el anillo A se definen conforme a lo descrito en la especificación; además se describen el método para la inhibición de aspartil proteasa, y en particular, los métodos de tratamiento de enfermedades cardiovasculares, enfermedades cognitivas y neurodegenerativas; asimismo, se describen métodos para el tratamiento de enfermedades cognitivas o neurodegenerativas usando los compuestos de la fórmula I en combinación con un inhibidor de colinesterasa o un antagonista m2, o agonista m1 muscarínico.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US87441906P | 2006-12-12 | 2006-12-12 | |
| PCT/US2007/025220 WO2008073365A1 (en) | 2006-12-12 | 2007-12-10 | Aspartyl protease inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2009006228A true MX2009006228A (es) | 2009-06-22 |
Family
ID=39356038
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2009006228A MX2009006228A (es) | 2006-12-12 | 2007-12-10 | Inhibidores de aspartil proteasa. |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US8093254B2 (es) |
| EP (1) | EP2064191B1 (es) |
| JP (1) | JP2010512389A (es) |
| KR (1) | KR20090087487A (es) |
| CN (1) | CN101668751A (es) |
| AR (1) | AR064287A1 (es) |
| AU (1) | AU2007332754A1 (es) |
| CA (1) | CA2672293A1 (es) |
| MX (1) | MX2009006228A (es) |
| TW (1) | TW200831512A (es) |
| WO (1) | WO2008073365A1 (es) |
Families Citing this family (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US7592348B2 (en) | 2003-12-15 | 2009-09-22 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| JP2008543849A (ja) * | 2005-06-14 | 2008-12-04 | シェーリング コーポレイション | アスパルチルプロテアーゼ阻害剤 |
| BRPI0612545A2 (pt) | 2005-06-14 | 2010-11-23 | Schering Corp | compostos inibidores de protease, composições farmacêuticas e uso dos mesmos |
| JP2008543840A (ja) | 2005-06-14 | 2008-12-04 | シェーリング コーポレイション | アスパルチルプロテアーゼインヒビター |
| AU2006307314C1 (en) | 2005-10-25 | 2011-08-25 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivative |
| CA2653650A1 (en) | 2006-06-12 | 2007-12-21 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| EP2147914B1 (en) | 2007-04-24 | 2014-06-04 | Shionogi&Co., Ltd. | Aminodihydrothiazine derivatives substituted with cyclic groups |
| WO2008133273A1 (ja) | 2007-04-24 | 2008-11-06 | Shionogi & Co., Ltd. | アルツハイマー症治療用医薬組成物 |
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| EA020740B1 (ru) | 2008-06-13 | 2015-01-30 | Шионоги & Ко., Лтд. | Серосодержащее гетероциклическое производное, обладающее активностью ингибитора бета-секретазы |
| CN102186841A (zh) | 2008-10-22 | 2011-09-14 | 盐野义制药株式会社 | 具有bace1抑制活性的2-氨基嘧啶-4-酮及2-氨基吡啶衍生物 |
| 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 |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| US8563543B2 (en) | 2009-10-08 | 2013-10-22 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| US8557826B2 (en) | 2009-10-08 | 2013-10-15 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions, and their use |
| EP2485920B1 (en) | 2009-10-08 | 2016-04-27 | Merck Sharp & Dohme Corp. | 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 |
| TWI488852B (zh) | 2009-12-11 | 2015-06-21 | Shionogi & Co | 衍生物 |
| AU2011321427A1 (en) | 2010-10-29 | 2013-05-02 | Shionogi & Co., Ltd. | Naphthyridine derivative |
| EP2634188A4 (en) | 2010-10-29 | 2014-05-07 | Shionogi & Co | FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE |
| GB201100181D0 (en) | 2011-01-06 | 2011-02-23 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| GB201101139D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| GB201101140D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
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| US9145426B2 (en) | 2011-04-07 | 2015-09-29 | 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 |
| CN103608345A (zh) | 2011-04-26 | 2014-02-26 | 盐野义制药株式会社 | 噁嗪衍生物和含有该噁嗪衍生物的bace1抑制剂 |
| 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 |
| CA2867891C (en) | 2012-03-19 | 2021-09-14 | Buck Institute For Research On Aging | App specific bace inhibitors (asbis) and uses thereof |
| US9422277B2 (en) | 2012-10-17 | 2016-08-23 | 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 |
| WO2014065434A1 (en) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
| US9303035B2 (en) | 2012-12-19 | 2016-04-05 | Novartis Ag | Substituted pyrazino[1′,2′:1,2]pyrrolo[3,4-d]pyrimidines, pyrimido[4′,5′:3,4]pyrrolo[2,1-c][1,4]oxazines and pyrimido[4′,5′:3,4]pyrrolo[1,2-d][1,4]oxazepines for inhibiting the CFTR channel |
| US9359381B2 (en) | 2012-12-19 | 2016-06-07 | Novartis Ag | Tricyclic compounds for inhibiting the CFTR channel |
| JP6471100B2 (ja) | 2013-02-12 | 2019-02-13 | バック・インスティテュート・フォー・リサーチ・オン・エイジング | Bace仲介性appプロセシングを調節するヒダントイン |
| 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 |
| CN108299169B (zh) * | 2018-02-02 | 2021-04-30 | 南京杰运医药科技有限公司 | 6-氯-3,4-二氢-2h-1-萘酮的合成方法 |
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-
2007
- 2007-12-10 CN CN200780051123A patent/CN101668751A/zh active Pending
- 2007-12-10 WO PCT/US2007/025220 patent/WO2008073365A1/en not_active Ceased
- 2007-12-10 KR KR1020097013474A patent/KR20090087487A/ko not_active Withdrawn
- 2007-12-10 EP EP07862708.0A patent/EP2064191B1/en active Active
- 2007-12-10 CA CA002672293A patent/CA2672293A1/en not_active Abandoned
- 2007-12-10 JP JP2009541321A patent/JP2010512389A/ja not_active Withdrawn
- 2007-12-10 MX MX2009006228A patent/MX2009006228A/es unknown
- 2007-12-10 AU AU2007332754A patent/AU2007332754A1/en not_active Abandoned
- 2007-12-10 US US12/517,744 patent/US8093254B2/en active Active
- 2007-12-11 AR ARP070105546A patent/AR064287A1/es not_active Application Discontinuation
- 2007-12-11 TW TW096147267A patent/TW200831512A/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AR064287A1 (es) | 2009-03-25 |
| WO2008073365A1 (en) | 2008-06-19 |
| CN101668751A (zh) | 2010-03-10 |
| US8093254B2 (en) | 2012-01-10 |
| KR20090087487A (ko) | 2009-08-17 |
| JP2010512389A (ja) | 2010-04-22 |
| US20100069406A1 (en) | 2010-03-18 |
| AU2007332754A1 (en) | 2008-06-19 |
| TW200831512A (en) | 2008-08-01 |
| EP2064191A1 (en) | 2009-06-03 |
| EP2064191B1 (en) | 2014-06-25 |
| CA2672293A1 (en) | 2008-06-19 |
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