AR080865A1 - Derivados de espirotetrahidronaftaleno, composiciones farmaceuticas que los contienen, proceso de preparacion y uso de los mismos para tratar enfermedades neurodegenerativas,tal como alzheimer. - Google Patents
Derivados de espirotetrahidronaftaleno, composiciones farmaceuticas que los contienen, proceso de preparacion y uso de los mismos para tratar enfermedades neurodegenerativas,tal como alzheimer.Info
- Publication number
- AR080865A1 AR080865A1 ARP110101073A ARP110101073A AR080865A1 AR 080865 A1 AR080865 A1 AR 080865A1 AR P110101073 A ARP110101073 A AR P110101073A AR P110101073 A ARP110101073 A AR P110101073A AR 080865 A1 AR080865 A1 AR 080865A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- acyl
- alkoxy
- heterocycle
- carbocycle
- Prior art date
Links
Classifications
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- 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
- C07D401/14—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 three or more hetero rings
-
- 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
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
- C07D263/62—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems having two or more ring systems containing condensed 1,3-oxazole rings
- C07D263/64—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems having two or more ring systems containing condensed 1,3-oxazole rings linked in positions 2 and 2' by chains containing six-membered aromatic rings or ring systems containing such rings
-
- 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
- C07D403/10—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 linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
-
- 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
- C07D417/10—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 linked by a carbon chain containing aromatic rings
Abstract
Reivindicacion 1: Un compuesto seleccionado desde la formula (1) y esteroisomeros, diaesteroisomeros, enantiomeros, tautomeros y sales farmacéuticamente aceptables de los mismos caracterizados porque W es un enlace o CR10R11; Y es O, S o NR1; Z es CR12R13 o C(=O), proporcionado cuando Z es C(=O) entonces Y es NR1; X1, X2 y X3 se seleccionan independientemente desde CR9 y N, caracterizado porque solamente uno de X1, X2 o X3 puede ser N; R1 se selecciona desde hidrogeno, alquilo, aralquilo, heteroarilo o heteroaralquilo; R2 se selecciona desde hidroxi, halogeno, amino, ciano, nitro, alquilo, alcoxi, acilo, aciloxi, alcoxicarbonilo, sulfonilo, sulfinilo, sulfanilo, ariloxi, un carbociclo o un heterociclo caracterizado porque dicho alquilo, alcoxi, acilo, aciloxi, alcoxicarbonilo, sulfonilo, sulfinilo, sulfanilo, ariloxi, carbociclo y heterociclo se sustituyen opcionalmente con hidroxi, halogeno, amino, ciano, nitro, oxo, alquilo opcionalmente sustituido, alcoxi opcionalmente sustituido, sulfanilo, acilo, alcoxicarbonilo, haloalquilo, carbociclo opcionalmente sustituido o heterociclo; R3 y R4 se seleccionan independientemente desde hidrogeno, halogeno y alquilo, o R3 y R4 juntos forman un grupo oxo; R5 y R6 son independientemente hidrogeno, hidroxi, halogeno, amino, ciano, nitro, alquilo, alcoxi, acilo, aciloxi, alcoxicarbonilo, sulfonilo, sulfinilo, sulfanilo, un carbociclo o un heterociclo caracterizado porque, dicho alquilo, alcoxi, acilo, aciloxi, alcoxicarbonilo, sulfonilo, sulfinilo, sulfanilo, carbociclo y heterociclo se sustituyen opcionalmente con hidroxi, halogeno, amino, ciano, nitro, alquilo, alcoxi, acilo, haloalquilo, un carbociclo opcionalmente sustituido y un heterociclo opcionalmente sustituido, o R5 y R6 juntos forman un carbociclo de 3 a 6 miembros o un heterociclo opcionalmente sustituido con hidroxi, halogeno, amino, ciano, nitro, alquilo, alcoxi, acilo y haloalquilo; R7 y R8 son independientemente hidrogeno, halogeno, amino, ciano, nitro, alquilo, alcoxi, acilo, aciloxi, alcoxicarbonilo, sulfonilo, sulfinilo, sulfanilo, un carbociclo o un heterociclo caracterizado porque dicho alquilo, alcoxi, acilo, aciloxi, alcoxicarbonilo, sulfonilo, sulfinilo, sulfanilo carbociclo y heterociclo se sustituyen opcionalmente con hidroxi, halogeno, amino, ciano, nitro, alquilo, alcoxi, acilo, haloalquilo, un carbociclo y un heterociclo opcionalmente sustituido, o R7 y R8 juntos forman un carbociclo de 3 a 6 miembros o un heterociclo opcionalmente sustituido por hidroxi, halogeno, amino, ciano, nitro, alquilo, alcoxi, acilo y haloalquilo; R9 es independientemente hidrogeno, halogeno, amino, ciano, nitro, alquilo, alcoxi, acilo, aciloxi, alcoxicarbonilo, sulfonilo, sulfinilo, sulfanilo, un carbociclo o un heterociclo caracterizado porque dicho alquilo, alcoxi, acilo, aciloxi, alcoxicarbonilo, sulfonilo, sulfinilo, sulfanilo, carbociclo y heterociclo se sustituyen opcionalmente con hidroxi, halogeno, amino, ciano, nitro, alquilo, alcoxi, acilo y haloalquilo, o R5 y R7 juntos forman un carbociclo de 3 a 4 miembros o heterociclo opcionalmente sustituido por hidroxi, halogeno, amino, ciano, nitro, alquilo, alcoxi, acilo y haloalquilo; cada R9 se selecciona independientemente del hidrogeno, halogeno o metilo; R10 y R11 se seleccionan independientemente desde hidrogeno y alquilo, o R10 y R11 juntos forman el átomo al cual se unen para formar un carbociclo de 3 a 6 miembros o un heterociclo; y R12 y R13 se seleccionan independientemente desde hidrogeno, alquilo y un carbociclo.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US31934110P | 2010-03-31 | 2010-03-31 | |
US201161439723P | 2011-02-04 | 2011-02-04 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR080865A1 true AR080865A1 (es) | 2012-05-16 |
Family
ID=43927953
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP110101073A AR080865A1 (es) | 2010-03-31 | 2011-03-31 | Derivados de espirotetrahidronaftaleno, composiciones farmaceuticas que los contienen, proceso de preparacion y uso de los mismos para tratar enfermedades neurodegenerativas,tal como alzheimer. |
Country Status (3)
Country | Link |
---|---|
US (1) | US20120065195A1 (es) |
AR (1) | AR080865A1 (es) |
WO (1) | WO2011123674A1 (es) |
Families Citing this family (27)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
EP2539322B1 (en) | 2010-02-24 | 2014-01-01 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
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 |
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 |
EP2675810A1 (en) | 2011-02-15 | 2013-12-25 | 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 |
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 |
US9079919B2 (en) * | 2011-05-27 | 2015-07-14 | Hoffmann-La Roche Inc. | Spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines as BACE1 and/or BACE2 inhibitors |
MX2014002113A (es) | 2011-08-22 | 2014-04-25 | Merck Sharp & Dohme | Iminotiazinas sustituidas en 2-espiro y sus mono y bioxidos como inhibidores de enzima de disociacion de proteina precursora amiloide del sitio beta, composiciones, y su uso. |
JP2014526560A (ja) | 2011-09-21 | 2014-10-06 | アムジエン・インコーポレーテツド | β‐セクレターゼ調節因子としてのアミノオキサジン化合物およびアミノジヒドロチアジン化合物および使用方法 |
US9650336B2 (en) | 2011-10-10 | 2017-05-16 | Astrazeneca Ab | Mono-fluoro beta-secretase inhibitors |
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 |
WO2013148851A1 (en) * | 2012-03-27 | 2013-10-03 | Array Biopharma Inc. | Compounds for treating neurodegenerative diseases |
CA2873678A1 (en) | 2012-05-30 | 2013-12-05 | Comentis, Inc. | Chromane compounds |
EP2669286A1 (en) * | 2012-05-31 | 2013-12-04 | Ares Trading S.A. | Spiro tetrahydro-benzothiophen derivatives useful for the treatment of neurodegenerative diseases |
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 |
US9000184B2 (en) | 2012-06-20 | 2015-04-07 | Astrazeneca Ab | Cyclohexane-1,2′-naphthalene-1′,2″-imidazol compounds and their use as BACE inhibitors |
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 |
WO2014052398A1 (en) | 2012-09-28 | 2014-04-03 | Vitae Pharmaceuticals, Inc. | Inhibitor of beta-secretase |
US9725469B2 (en) | 2012-11-15 | 2017-08-08 | Amgen, Inc. | Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
WO2014099788A1 (en) | 2012-12-21 | 2014-06-26 | Merck Sharp & Dohme Corp. | C5-spiro iminothiadiazine dioxides as bace inhibitors |
US10053453B2 (en) | 2014-10-07 | 2018-08-21 | Astrazeneca Ab | Compounds and their use as BACE inhibitors |
CN115322208B (zh) * | 2021-05-10 | 2023-04-11 | 中国药科大学 | 2-氨基噻唑类衍生物及其制备方法和医药用途 |
Family Cites Families (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE2714880A1 (de) | 1977-04-02 | 1978-10-26 | Hoechst Ag | Cephemderivate und verfahren zu ihrer herstellung |
ZA825413B (en) | 1981-08-26 | 1983-06-29 | Pfizer | Thromboxane synthetase inhibitors, processes for their production, and pharmaceutical compositions comprising them |
US5543523A (en) | 1994-11-15 | 1996-08-06 | Regents Of The University Of Minnesota | Method and intermediates for the synthesis of korupensamines |
EP0975608B1 (en) | 1997-04-15 | 2005-06-15 | Genentech, Inc. | Halo-alkoxycarbonyl prodrugs |
WO2008030412A2 (en) * | 2006-09-07 | 2008-03-13 | Merck & Co., Inc. | Spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease |
AU2008277676A1 (en) | 2007-07-16 | 2009-01-22 | Novartis Ag | Heterocyclic compounds useful as MK2 inhibitors |
WO2010021680A2 (en) * | 2008-08-19 | 2010-02-25 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
-
2011
- 2011-03-31 WO PCT/US2011/030769 patent/WO2011123674A1/en active Application Filing
- 2011-03-31 US US13/077,477 patent/US20120065195A1/en not_active Abandoned
- 2011-03-31 AR ARP110101073A patent/AR080865A1/es unknown
Also Published As
Publication number | Publication date |
---|---|
WO2011123674A1 (en) | 2011-10-06 |
US20120065195A1 (en) | 2012-03-15 |
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