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
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 208000015122 neurodegenerative disease Diseases 0.000 title abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 13
- 125000002252 acyl group Chemical group 0.000 abstract 12
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 12
- 125000003396 thiol group Chemical group [H]S* 0.000 abstract 12
- 229910052736 halogen Inorganic materials 0.000 abstract 10
- 150000002367 halogens Chemical group 0.000 abstract 10
- 125000000623 heterocyclic group Chemical group 0.000 abstract 10
- 229910052739 hydrogen Inorganic materials 0.000 abstract 9
- 239000001257 hydrogen Substances 0.000 abstract 9
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 9
- 125000004423 acyloxy group Chemical group 0.000 abstract 8
- 125000003545 alkoxy group Chemical group 0.000 abstract 8
- 125000004104 aryloxy group Chemical group 0.000 abstract 8
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 abstract 8
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 abstract 8
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 7
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 7
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 7
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 7
- 125000004043 oxo group Chemical group O=* 0.000 abstract 6
- 125000001188 haloalkyl group Chemical group 0.000 abstract 4
- 125000005415 substituted alkoxy group Chemical group 0.000 abstract 4
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 4
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000004429 atom Chemical group 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- 101100495911 Arabidopsis thaliana CHR10 gene Proteins 0.000 abstract 1
- 101001043818 Mus musculus Interleukin-31 receptor subunit alpha Proteins 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 238000003776 cleavage reaction Methods 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000004475 heteroaralkyl group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 230000004770 neurodegeneration Effects 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000007017 scission Effects 0.000 abstract 1
- 229940124597 therapeutic agent Drugs 0.000 abstract 1
Classifications
-
- 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 (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1883341B1 (en) | 2005-05-09 | 2020-08-12 | 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 |
| BR122020017678B1 (pt) | 2007-10-02 | 2021-08-03 | Labrador Diagnostics Llc | Sistema para detecção automática de um analito em uma amostra de fluido corporal |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| WO2012071279A1 (en) | 2010-11-23 | 2012-05-31 | 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 |
| TW202208825A (zh) | 2011-01-21 | 2022-03-01 | 美商拉布拉多診斷有限責任公司 | 樣本使用最大化之系統及方法 |
| US9346827B2 (en) | 2011-02-07 | 2016-05-24 | Amgen Inc. | 5-amino-oxazepine and 5-amino-thiazepane compounds as beta secretase antagonists and methods of use |
| US8962859B2 (en) | 2011-02-15 | 2015-02-24 | Amgen Inc. | Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of 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 |
| 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 |
| 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 |
| 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 |
| US8380541B1 (en) | 2011-09-25 | 2013-02-19 | Theranos, Inc. | Systems and methods for collecting and transmitting assay results |
| 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 |
| US20140170735A1 (en) | 2011-09-25 | 2014-06-19 | Elizabeth A. Holmes | Systems and methods for multi-analysis |
| US9296759B2 (en) | 2011-09-21 | 2016-03-29 | Amgen Inc. | Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| US10012664B2 (en) | 2011-09-25 | 2018-07-03 | Theranos Ip Company, Llc | Systems and methods for fluid and component handling |
| US9810704B2 (en) | 2013-02-18 | 2017-11-07 | Theranos, Inc. | Systems and methods for multi-analysis |
| ES2566373T3 (es) * | 2011-10-10 | 2016-04-12 | Astrazeneca Ab | Inhibidores monofluoro beta-secretasa |
| JP2015518048A (ja) | 2012-05-30 | 2015-06-25 | コメンティス， インコーポレイテッド | クロマン化合物 |
| 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 |
| WO2014078314A1 (en) | 2012-11-15 | 2014-05-22 | Amgen Inc. | Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| WO2019060720A1 (en) | 2017-09-25 | 2019-03-28 | Case Western Reserve University | COMPOSITIONS AND METHODS FOR REDUCING SERUM CHOLESTEROL AND PCSK9 |
| WO2020005938A1 (en) | 2018-06-25 | 2020-01-02 | Case Western Reserve University | Compositions and methods for treating tissue injury |
| WO2020061566A1 (en) | 2018-09-21 | 2020-03-26 | Case Western Reserve University | Aldoketo reductase inhibitors and uses thereof |
| 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 |
| CA2662776A1 (en) * | 2006-09-07 | 2008-03-13 | Merck And Co., Inc. | Spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease |
-
2011
- 2011-09-23 UY UY0001033627A patent/UY33627A/es not_active Application Discontinuation
- 2011-09-23 TW TW100134440A patent/TW201219400A/zh unknown
- 2011-09-23 AR ARP110103476A patent/AR083169A1/es unknown
- 2011-09-23 US US13/244,034 patent/US20120083501A1/en not_active Abandoned
- 2011-09-23 WO PCT/US2011/053118 patent/WO2012040641A2/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| WO2012040641A2 (en) | 2012-03-29 |
| US20120083501A1 (en) | 2012-04-05 |
| WO2012040641A3 (en) | 2012-06-07 |
| TW201219400A (en) | 2012-05-16 |
| UY33627A (es) | 2013-04-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |