AR080524A1 - Compuestos de anillo espiro-tetraciclico como moduladores de beta secretasa, composiciones farmaceuticas que los contienen, proceso de preparacion y uso de los mismos en el tratamiento de la enfermedad de alzheimer y trastornos relacionados. - Google Patents
Compuestos de anillo espiro-tetraciclico como moduladores de beta secretasa, composiciones farmaceuticas que los contienen, proceso de preparacion y uso de los mismos en el tratamiento de la enfermedad de alzheimer y trastornos relacionados.Info
- Publication number
- AR080524A1 AR080524A1 ARP110100822A ARP110100822A AR080524A1 AR 080524 A1 AR080524 A1 AR 080524A1 AR P110100822 A ARP110100822 A AR P110100822A AR P110100822 A ARP110100822 A AR P110100822A AR 080524 A1 AR080524 A1 AR 080524A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- phenyl
- aza
- oxo
- bicyclo
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 238000002360 preparation method Methods 0.000 title 1
- -1 8-oxo-3-aza-bicyclo [3.2.1] oct-3-yl Chemical group 0.000 abstract 20
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 17
- 125000001424 substituent group Chemical group 0.000 abstract 6
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 4
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 4
- 125000005043 dihydropyranyl group Chemical group O1C(CCC=C1)* 0.000 abstract 4
- 125000000842 isoxazolyl group Chemical group 0.000 abstract 4
- 125000002757 morpholinyl group Chemical group 0.000 abstract 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 4
- 125000004193 piperazinyl group Chemical group 0.000 abstract 4
- 125000003226 pyrazolyl group Chemical group 0.000 abstract 4
- 125000004076 pyridyl group Chemical group 0.000 abstract 4
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 4
- 125000005309 thioalkoxy group Chemical group 0.000 abstract 4
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 4
- 125000002393 azetidinyl group Chemical group 0.000 abstract 3
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 abstract 3
- 125000004852 dihydrofuranyl group Chemical group O1C(CC=C1)* 0.000 abstract 3
- 125000002541 furyl group Chemical group 0.000 abstract 3
- 125000003566 oxetanyl group Chemical group 0.000 abstract 3
- 125000004043 oxo group Chemical group O=* 0.000 abstract 3
- 125000003386 piperidinyl group Chemical group 0.000 abstract 3
- 125000004309 pyranyl group Chemical group O1C(C=CC=C1)* 0.000 abstract 3
- 125000003373 pyrazinyl group Chemical group 0.000 abstract 3
- 125000002098 pyridazinyl group Chemical group 0.000 abstract 3
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 3
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 abstract 3
- 125000001412 tetrahydropyranyl group Chemical group 0.000 abstract 3
- 125000000335 thiazolyl group Chemical group 0.000 abstract 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 2
- 125000006559 (C1-C3) alkylamino group Chemical group 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 2
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 abstract 2
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 abstract 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000002720 diazolyl group Chemical group 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000002883 imidazolyl group Chemical group 0.000 abstract 1
- 125000001786 isothiazolyl group Chemical group 0.000 abstract 1
- 125000002971 oxazolyl group Chemical group 0.000 abstract 1
- 125000001113 thiadiazolyl group Chemical group 0.000 abstract 1
- 125000001544 thienyl group Chemical group 0.000 abstract 1
Classifications
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- 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
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
- C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
- C07D221/20—Spiro-condensed ring systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
- C07D295/135—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/10—Spiro-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/20—Spiro-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/10—Spiro-condensed systems
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- C—CHEMISTRY; METALLURGY
- C09—DYES; PAINTS; POLISHES; NATURAL RESINS; ADHESIVES; COMPOSITIONS NOT OTHERWISE PROVIDED FOR; APPLICATIONS OF MATERIALS NOT OTHERWISE PROVIDED FOR
- C09B—ORGANIC DYES OR CLOSELY-RELATED COMPOUNDS FOR PRODUCING DYES, e.g. PIGMENTS; MORDANTS; LAKES
- C09B11/00—Diaryl- or thriarylmethane dyes
- C09B11/28—Pyronines ; Xanthon, thioxanthon, selenoxanthan, telluroxanthon dyes
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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
- A61K31/42—Oxazoles
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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
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
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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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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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
- A61K31/495—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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Reivindicacion 1: Un compuesto de la formula (1) caracterizado porque A1 es CH, CF o N; A2 es CH, CF o N; A3 es CH, CF, OH, OCH3, OCF3 o N; A4 es CH, CF, OH, OCH3, OCF3 o N; A5 es CH, CR1 o N; A6 es CH, CF o N, siempre que no más de uno de A1, A2, A3, A4, A5 y A6 es N; R1 es F, Br o un resto de formula (2); R2 es Cl, Br, CN, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, CN, -Oalquilo C1-6, -Salquilo C1-6, -NHalquilo C1-6, -N(alquilo C1-6)2, -NH-fenilo, -NH-bencilo, fenilo, piridilo, pirimidilo, pirazinilo, piridazinilo, pirazolilo, imidazolilo, oxazolilo, isoxazolilo, tiazolilo, isotiazolilo, diazolilo, tiadiazolilo, tienilo, piranilo, dihidropiranilo, tetrahidropiranilo, furanilo, dihidrofuranilo, tetrahidrofuranilo, pirrolidinilo, piperidinilo, piperazinilo, morfolinilo, azetidinilo, 8-oxo-3-aza-biciclo[3.2.1]oct-3-ilo, aza-biciclo[2.2.1]hept-5-ilo, 2-oxo-7-aza-[3,5]-espironon-7-ilo, ciclohexilo o -Si(CH3)3, en donde el alquilo C1-6, alquenilo C2-6, alquinilo C2-6, -Oalquilo C1-6, -Salquilo C1-6, -NHalquilo C1-6, -N(alquilo C1-6)2, -NH-fenilo, -NH-bencilo, fenilo, piridilo, pirimidilo, pirazinilo, piridazinilo, pirazolilo, isoxazolilo, tiazolilo, piranilo, dihidropiranilo, tetrahidropiranilo, furanilo, dihidrofuranilo, tetrahidrofuranilo, pirrolidinilo, piperidinilo, piperazinilo, morfolinilo, azetidinilo, 8-oxo- 3-aza-biciclo[3.2.1]oct-3-ilo, aza-biciclo[2.2.1]hept-5-ilo, 2-oxo-7-aza-[3,5]-espironon-7-ilo y ciclohexilo son opcionalmente sustituidos, independientemente, con 1-5 sustituyentes de R8; R7 es alquilo C1-6, alquenilo C2-4, alquinilo C2-4, CN, -Oalquilo C1-6, -Salquilo C1-6, -NHalquilo C1-6, -N(alquilo C1-3)2, -NH-fenilo, -NH-bencilo, -O-fenilo o un anillo seleccionado del grupo que consiste de fenilo, piridilo, pirimidilo, pirazinilo, piridazinilo, pirazolilo, isoxazolilo, tiazolilo, piranilo, dihidropiranilo, tetrahidropiranilo, furanilo, dihidrofuranilo, tetrahidrofuranilo, pirrolidinilo, piperidinilo, piperazinilo, morfolinilo, azetidinilo, 8-oxo-3-aza-biciclo[3.2.1]oct-3-ilo, aza-biciclo[2.2.1]hept-5-ilo, 2-oxo-7-aza-[3,5]-espironon-7-ilo y ciclohexilo, en donde el alquilo C1-6, alquenilo C2-4, alquinilo C2-4, -Oalquilo C1-6, -Salquilo C1-6, -NHalquilo C1-6, -N(alquilo C1-3)2, -NH-fenilo, -NH-bencilo, -O-fenilo y el anillo son opcionalmente sustituidos, independientemente, con 1-5 sustituyentes de R8; cada R8, independientemente, es halo, haloalquilo, CN, OH, NO2, NH2, acetilo, -C(O)NHCH3, oxo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6, alquilamino C1-6, dialquilamino C1-6, alcoxilo C1-6, tioalcoxilo C1-6, o un anillo seleccionado a partir del grupo que consiste de piridilo, pirimidilo, fenilo, morfolinilo, pirazolilo, isoxazolilo, dihidropiranilo, pirrolidinilo, piperazinilo, oxetanilo y dioxolilo, en donde cada uno del alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6, alquilamino C1-6, dialquilamino C1-6, alcoxilo C1-6, tioalcoxilo C1-6 y el anillo es opcionalmente sustituido independientemente con 1-5 sustituyentes de F, Cl, Br, CN, CF3, OCF3, NO2, NH2, OH, oxo, metilo, metoxilo, etilo, etoxilo, propilo, propoxilo, isopropilo, isopropoxilo, ciclopropilo, ciclopropilmetoxilo, butilo, butoxilo, isobutoxilo, terc-butoxilo, isobutilo, sec-butilo, terc-butilo, alquilamino C1-3, dialquilamino C1-3, tioalcoxilo C1-3 u oxetanilo; alternativamente, dos sustituyentes R8 adyacentes junto con el mismo átomo al cual están unidos forman un anillo espirocíclico de 3-6 elementos que incluye 0-3 heteroátomos seleccionados de N, O y S, el anillo espirocíclico opcionalmente sustituido con 1-3 sustituyentes de 1-5 sustituyentes de F, Cl, CN, CF3, OCF3, NO2, OH, oxo, metilo, metoxilo, etilo, etoxilo, propilo, propoxilo, isopropilo, isopropoxilo, ciclopropilo, ciclopropilmetoxilo, butilo, butoxilo, isobutoxilo, terc-butoxilo, isobutilo, sec-butilo, terc-butilo, alquilamino C1-3, dialquilamino C1-3, tioalcoxilo C1-3 u oxetanilo; X es O, S o CF2; y Y es CR9R9 en donde cada R9, independientemente, es H, F, alquilo C1-4 o -CH2OCH3.
Applications Claiming Priority (1)
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US31412910P | 2010-03-15 | 2010-03-15 |
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AR080524A1 true AR080524A1 (es) | 2012-04-11 |
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ARP110100822A AR080524A1 (es) | 2010-03-15 | 2011-03-15 | Compuestos de anillo espiro-tetraciclico como moduladores de beta secretasa, composiciones farmaceuticas que los contienen, proceso de preparacion y uso de los mismos en el tratamiento de la enfermedad de alzheimer y trastornos relacionados. |
Country Status (10)
Country | Link |
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US (1) | US8883782B2 (es) |
EP (1) | EP2547685A1 (es) |
JP (1) | JP2013522305A (es) |
AR (1) | AR080524A1 (es) |
AU (1) | AU2011227511B2 (es) |
CA (1) | CA2791281A1 (es) |
MX (1) | MX2012010658A (es) |
TW (1) | TW201144322A (es) |
UY (1) | UY33277A (es) |
WO (1) | WO2011115938A1 (es) |
Families Citing this family (17)
Publication number | Priority date | Publication date | Assignee | Title |
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US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
MX2012010657A (es) * | 2010-03-15 | 2013-02-07 | Amgen Inc | Compuestos de espiro amino-dihidrooxazina y amino-dihidrotiazina como moduladores de beta-secretasa y su uso medico. |
EP2643325A1 (en) | 2010-11-23 | 2013-10-02 | Amgen Inc. | Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use |
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- 2011-03-14 EP EP11710372A patent/EP2547685A1/en not_active Withdrawn
- 2011-03-14 US US13/047,734 patent/US8883782B2/en active Active
- 2011-03-14 JP JP2013500141A patent/JP2013522305A/ja not_active Withdrawn
- 2011-03-14 WO PCT/US2011/028417 patent/WO2011115938A1/en active Application Filing
- 2011-03-14 AU AU2011227511A patent/AU2011227511B2/en not_active Ceased
- 2011-03-14 MX MX2012010658A patent/MX2012010658A/es not_active Application Discontinuation
- 2011-03-14 CA CA2791281A patent/CA2791281A1/en not_active Abandoned
- 2011-03-15 TW TW100108803A patent/TW201144322A/zh unknown
- 2011-03-15 AR ARP110100822A patent/AR080524A1/es not_active Application Discontinuation
- 2011-03-15 UY UY0001033277A patent/UY33277A/es not_active Application Discontinuation
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CA2791281A1 (en) | 2011-09-22 |
TW201144322A (en) | 2011-12-16 |
EP2547685A1 (en) | 2013-01-23 |
WO2011115938A1 (en) | 2011-09-22 |
US20110251190A1 (en) | 2011-10-13 |
US8883782B2 (en) | 2014-11-11 |
AU2011227511B2 (en) | 2014-02-20 |
MX2012010658A (es) | 2012-12-05 |
AU2011227511A1 (en) | 2012-09-20 |
UY33277A (es) | 2011-09-30 |
JP2013522305A (ja) | 2013-06-13 |
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