AR083169A1 - Compuestos para tratar enfermedades neurodegenerativas - Google Patents
Compuestos para tratar enfermedades neurodegenerativasInfo
- Publication number
- AR083169A1 AR083169A1 ARP110103476A ARP110103476A AR083169A1 AR 083169 A1 AR083169 A1 AR 083169A1 AR P110103476 A ARP110103476 A AR P110103476A AR P110103476 A ARP110103476 A AR P110103476A AR 083169 A1 AR083169 A1 AR 083169A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- carbocycle
- sulfanyl
- alkoxycarbonyl
- Prior art date
Links
Classifications
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
- C07D491/20—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Estos compuestos tricíclicos de la fórmula (1) que inhiben el clivaje de b-secretasa de APP son de utilidad como agentes terapéuticos para el tratamiento de enfermedades neurodegenerativas. Se reivindica el compuesto y composiciones farmacéuticas.Reivindicación 1: Un compuesto seleccionado de la fórmula (1) y sus estereoisómeros, diastereómeros, enantiómeros, tautómeros y sales farmacéuticamente aceptables, en donde: X1 está seleccionado de O, S, S(O), SO2, NR10 y CHR10; X2 está seleccionado de CR5R6, NR7 y O; X3 está seleccionado de CR8R9 y O; X4 está seleccionado de CR11 y N; X5 está seleccionado de CR12R13 y O, en donde dos de X2, X3 y X5 deben contener C; R1 está seleccionado de hidrógeno, alquilo, aralquilo, heteroarilo y heteroaralquilo; R2 y R3 están seleccionados, de modo independiente, de hidrógeno, halógeno y alquilo; R4 está seleccionado de hidrógeno, hidroxi, halógeno, amino, ciano, nitro, alquilo, alcoxi, acilo, aciloxi, alcoxicarbonilo, sulfonilo, sulfinilo, sulfanilo, ariloxi, un carbociclo y un heterociclo, en donde dicho alquilo, alcoxi, acilo, aciloxi, alcoxicarbonilo, sulfonilo, sulfinilo, sulfanilo, ariloxi, carbociclo y heterociclo están opcionalmente sustituidos con hidroxi, halógeno, amino, ciano, nitro, oxo, alquilo opcionalmente sustituido, alcoxi opcionalmente sustituido, sulfanilo, acilo, alcoxicarbonilo, haloalquilo o carbociclo opcionalmente sustituido; R5 y R6 están seleccionados, de modo independiente, de hidrógeno, hidroxi, halógeno, amino, ciano, nitro, alquilo, alcoxi, acilo, aciloxi, alcoxicarbonilo, sulfonilo, sulfinilo, sulfanilo, ariloxi, un carbociclo y un heterociclo, en donde dicho alquilo, alcoxi, acilo, aciloxi, alcoxicarbonilo, sulfonilo, sulfinilo, sulfanilo, ariloxi, carbociclo y heterociclo están opcionalmente sustituidos con hidroxi, halógeno, amino, ciano, nitro, oxo, alquilo opcionalmente sustituido, alcoxi opcionalmente sustituido, sulfanilo, acilo, alcoxicarbonilo, haloalquilo o carbociclo opcionalmente sustituido, o R5 y R6 tomados juntos forman un grupo oxo, o R5 y R6 junto con el átomo al que están unidos forman un carbociclo o heterociclo; R7 está seleccionado de hidrógeno, alquilo, alcoxi, acilo, aciloxi, alcoxicarbonilo, sulfonilo, sulfinilo, sulfanilo, ariloxi, un carbociclo y un heterociclo, en donde dicho alquilo, alcoxi, acilo, aciloxi, alcoxicarbonilo, sulfonilo, sulfinilo, sulfanilo, ariloxi, carbociclo y heterociclo están opcionalmente sustituidos con hidroxi, halógeno, amino, ciano, nitro, oxo, alquilo opcionalmente sustituido, alcoxi opcionalmente sustituido, sulfanilo, acilo, alcoxicarbonilo, haloalquilo o carbociclo opcionalmente sustituido; R8 y R9 están seleccionados, de modo independiente, de hidrógeno, hidroxi, halógeno, amino, ciano, nitro, alquilo, alcoxi, acilo, aciloxi, alcoxicarbonilo, sulfonilo, sulfinilo, sulfanilo, ariloxi, un carbociclo y un heterociclo, en donde dicho alquilo, alcoxi, acilo, aciloxi, alcoxicarbonilo, sulfonilo, sulfinilo, sulfanilo, ariloxi, carbociclo y heterociclo están opcionalmente sustituidos con hidroxi, halógeno, amino, ciano, nitro, oxo, alquilo opcionalmente sustituido, alcoxi opcionalmente sustituido, sulfanilo, acilo, alcoxicarbonilo, haloalquilo o carbociclo opcionalmente sustituido, o R8 y R9 tomados juntos forman un oxo o grupo alquenilo, en donde el enlace doble del grupo alquenilo se une inmediatamente al átomos de carbono al que están unidos R8 y R9, o R8 y R9 junto con el átomo al que están unidos forman un carbociclo o heterociclo; R10 está seleccionado de hidrógeno, halógeno y alquilo; R11 está seleccionado de hidrógeno, halógeno y alquilo; y R12 y R13 están seleccionados, de modo independiente, de hidrógeno y alquilo.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US38629610P | 2010-09-24 | 2010-09-24 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR083169A1 true AR083169A1 (es) | 2013-02-06 |
Family
ID=45874425
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP110103476A AR083169A1 (es) | 2010-09-24 | 2011-09-23 | Compuestos para tratar enfermedades neurodegenerativas |
Country Status (5)
Country | Link |
---|---|
US (1) | US20120083501A1 (es) |
AR (1) | AR083169A1 (es) |
TW (1) | TW201219400A (es) |
UY (1) | UY33627A (es) |
WO (1) | WO2012040641A2 (es) |
Families Citing this family (37)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP3763824A1 (en) | 2005-05-09 | 2021-01-13 | Labrador Diagnostics LLC | Point-of-care fluidic systems and uses thereof |
US8741230B2 (en) | 2006-03-24 | 2014-06-03 | Theranos, Inc. | Systems and methods of sample processing and fluid control in a fluidic system |
RU2540424C2 (ru) | 2007-10-02 | 2015-02-10 | Теранос, Инк. | Патрон для автоматического обнаружения аналита в пробе телесной жидкости и содержащая его система |
UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
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 |
US8415483B2 (en) | 2010-12-22 | 2013-04-09 | Astrazeneca Ab | Compounds and their use as BACE inhibitors |
CN106323876B (zh) | 2011-01-21 | 2020-02-14 | 西拉诺斯知识产权有限责任公司 | 样品使用最大化的系统和方法 |
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 |
EP2694521B1 (en) | 2011-04-07 | 2015-11-25 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
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 |
CA2844988A1 (en) | 2011-08-22 | 2013-02-28 | Merck Sharp & Dohme Corp. | 2-spiro-substituted iminothiazines and their mono- and dioxides as bace inhibitors, compositions, and their use |
US8840838B2 (en) | 2011-09-25 | 2014-09-23 | Theranos, Inc. | Centrifuge configurations |
US8380541B1 (en) | 2011-09-25 | 2013-02-19 | Theranos, Inc. | Systems and methods for collecting and transmitting assay results |
US9268915B2 (en) | 2011-09-25 | 2016-02-23 | Theranos, Inc. | Systems and methods for diagnosis or treatment |
US20140170735A1 (en) | 2011-09-25 | 2014-06-19 | Elizabeth A. Holmes | Systems and methods for multi-analysis |
US9619627B2 (en) | 2011-09-25 | 2017-04-11 | Theranos, Inc. | Systems and methods for collecting and transmitting assay results |
US9632102B2 (en) | 2011-09-25 | 2017-04-25 | Theranos, Inc. | Systems and methods for multi-purpose analysis |
US8475739B2 (en) | 2011-09-25 | 2013-07-02 | Theranos, Inc. | Systems and methods for fluid handling |
US9664702B2 (en) | 2011-09-25 | 2017-05-30 | Theranos, Inc. | Fluid handling apparatus and configurations |
EP2758406A1 (en) | 2011-09-21 | 2014-07-30 | Amgen Inc. | Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
US9810704B2 (en) | 2013-02-18 | 2017-11-07 | Theranos, Inc. | Systems and methods for multi-analysis |
US9250229B2 (en) | 2011-09-25 | 2016-02-02 | Theranos, Inc. | Systems and methods for multi-analysis |
US10012664B2 (en) | 2011-09-25 | 2018-07-03 | Theranos Ip Company, Llc | Systems and methods for fluid and component handling |
WO2013054108A1 (en) * | 2011-10-10 | 2013-04-18 | Astrazeneca Ab | Mono-fluoro beta-secretase inhibitors |
BR112014029597A2 (pt) | 2012-05-30 | 2017-11-07 | Comentis Inc | compostos de cromano |
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 |
US9000182B2 (en) | 2012-06-20 | 2015-04-07 | Astrazeneca Ab | 2H-imidazol-4-amine compounds and their use as BACE inhibitors |
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 |
US9725469B2 (en) | 2012-11-15 | 2017-08-08 | Amgen, Inc. | Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
US11576900B2 (en) | 2017-09-25 | 2023-02-14 | Case Western Reserve University | Compositions and methods of reducing serum cholesterol and PCSK9 |
WO2020005938A1 (en) | 2018-06-25 | 2020-01-02 | Case Western Reserve University | Compositions and methods for treating tissue injury |
EP3852750A4 (en) | 2018-09-21 | 2022-05-11 | Case Western Reserve University | ALDOKETO REDUCTAE INHIBITORS AND THEIR USES |
WO2021061763A1 (en) * | 2019-09-23 | 2021-04-01 | Case Western Reserve University | Aldoketo reductase inhibitors and uses thereof |
US11932655B1 (en) | 2023-10-17 | 2024-03-19 | King Faisal University | 12-bromo-2,16-dioxapentacyclo[7.7.5.01,21.03,8.010,15]henicosa3(8),10,12,14-tetraene-7,20-dione as an antimicrobial compound |
Family Cites Families (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
TW200730523A (en) * | 2005-07-29 | 2007-08-16 | Wyeth Corp | Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation |
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 |
JP2010502705A (ja) * | 2006-09-07 | 2010-01-28 | メルク エンド カムパニー インコーポレーテッド | アルツハイマー病の治療用としてのスピロピペリジンベータセクレターゼ阻害剤 |
-
2011
- 2011-09-23 WO PCT/US2011/053118 patent/WO2012040641A2/en active Application Filing
- 2011-09-23 UY UY0001033627A patent/UY33627A/es not_active Application Discontinuation
- 2011-09-23 US US13/244,034 patent/US20120083501A1/en not_active Abandoned
- 2011-09-23 TW TW100134440A patent/TW201219400A/zh unknown
- 2011-09-23 AR ARP110103476A patent/AR083169A1/es unknown
Also Published As
Publication number | Publication date |
---|---|
WO2012040641A3 (en) | 2012-06-07 |
TW201219400A (en) | 2012-05-16 |
US20120083501A1 (en) | 2012-04-05 |
WO2012040641A2 (en) | 2012-03-29 |
UY33627A (es) | 2013-04-30 |
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