AR077328A1 - Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos - Google Patents
Derivados de oxazina y su uso en el tratamiento de trastornos neurologicosInfo
- Publication number
- AR077328A1 AR077328A1 ARP100102667A ARP100102667A AR077328A1 AR 077328 A1 AR077328 A1 AR 077328A1 AR P100102667 A ARP100102667 A AR P100102667A AR P100102667 A ARP100102667 A AR P100102667A AR 077328 A1 AR077328 A1 AR 077328A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- thioalkyl
- alkoxy
- halo
- group
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—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
- A61K31/535—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
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
- C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D267/02—Seven-membered rings
- C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
- C07D267/10—Seven-membered rings having the hetero atoms in positions 1 and 4 not condensed with other 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
- 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
- C07D413/12—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 chain containing hetero atoms as chain links
-
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero 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
- C07D417/12—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 chain containing hetero atoms as chain links
-
- 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
- C07D471/02—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 two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Hospice & Palliative Care (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
- Cardiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
La presente se refiere a su preparacion, a su uso médico, y a medicamentos que los comprenden. Reivindicacion 1: Un compuesto de la formula (1), o una sal farmacéuticamente aceptable del mismo: en donde: X es O o S; R1 es hidrogeno; ciano; halogeno; alquilo C1-8; halo-alquilo C1-8; alcoxilo C1-8; halo-alcoxilo C1-8; tioalquilo C1-8; halo-tioalquilo C1-8; alcoxilo C1-8-alquilo C1-8; alcoxilo C1-8-alcoxilo C1-8; alcoxilo C1-8-tioalquilo C1-8; tioalquilo C1-8-alquilo C1-8; tioalquilo C1-8-alcoxilo C1-8; tioalquilo C1-8-tioalquilo C1-8; alquenilo C2-8; o alquinilo C2-8; R2 es un grupo arilo, heteroarilo, o heterociclilo no aromático G1, cuyo grupo G1 está opcionalmente sustituido por 1, 2, 3 o 4 sustituyentes seleccionados independientemente a partir del grupo que consiste en ciano, nitro, amino, amino-carbonilo, halogeno, alquilo C1-8; halo-alquilo C1-8; hidroxilo, alcoxilo C1-8; halo-alcoxilo C1-8; tioalquilo C1-8; halo-tioalquilo C1-8; alcoxilo C1-8-alquilo C1-8; alcoxilo C1-8-alcoxilo C1-8; alcoxilo C1-8-tioalquilo C1-8; tioalquilo C1-8-alquilo C1-8; tioalquilo C1-8-alcoxilo C1-8; tioalquilo C1-8-tioalquilo C1-8; alquenilo C2-8; alquinilo C2-8; alquenoxilo C2-8, alquinoxilo C2-8, y un grupo cicloalquilo C3-8, arilo, heteroarilo, o heterociclilo no aromático G2, cuyo grupo G2 está opcionalmente sustituido por 1, 2, 3 o 4 sustituyentes seleccionados independientemente a partir del grupo que consiste en ciano, aminocarbonilo, halogeno, alquilo C1-8; halo-alquilo C1-8; hidroxilo, alcoxilo C1-8; halo-alcoxilo C1-8; tioalquilo C1-8; halo-tioalquilo C1-8; alcoxilo C1-8-alquilo C1-8; alcoxilo C1-8-alcoxilo C1-8; alcoxilo C1-8-tioalquilo C1-8; tioalquilo C1-8-alquilo C1-8; tioalquilo C1-8-alcoxilo C1-8; tioalquilo C1-8-tioalquilo C1-8; alquenilo C2-8; y alquinilo C2-8; R3 es hidrogeno; ciano; halogeno; alquilo C1-8; halo-alquilo C1-8; alcoxilo C1-8; halo-alcoxilo C1-8; tioalquilo C1-8; halo-tioalquilo C1-8; alcoxilo C1-8-alquilo C1-8; alcoxilo C1-8-alcoxilo C1-8; alcoxilo C1-8-tioalquilo C1-8; tioalquilo C1-8-alquilo C1-8; tioalquilo C1-8-alcoxilo C1-8; tioalquilo C1-8-tioalquilo C1-8; alquenilo C2-8; o alquinilo C2-8; cualquiera de R4 es hidrogeno; ciano; halogeno; alquilo C1-8; halo-alquilo C1-8; alcoxilo C1-8; halo-alcoxilo C1-8; tioalquilo C1-8; halo-tioalquilo C1-8; alcoxilo C1-8-alquilo C1-8; alcoxilo C1-8-alcoxilo C1-8; alcoxilo C1-8-tioalquilo C1-8; tioalquilo C1-8-alquilo C1-8; tioalquilo C1-8-alcoxilo C1-8; tioalquilo C1-8-tioalquilo C1-8; alquenilo C2-8; o alquinilo C2-8; y R5 es hidrogeno; ciano; halogeno; alquilo C1-8; halo-alquilo C1-8; alcoxilo C1-8; halo-alcoxilo C1-8; tioalquilo C1-8; halo-tioalquilo C1-8; alcoxilo C1-8-alquilo C1-8; alcoxilo C1-8-alcoxilo C1-8; alcoxilo C1-8-tioalquilo C1-8; tioalquilo C1-8-alquilo C1-8; tioalquilo C1-8-alcoxilo C1-8; tioalquilo C1-8-tioalquilo C1-8; alquenilo C2-8; o alquinilo C2-8; o R4 y R5, tomados juntos, son -C(H)=C(H)-C(H)=C(H)- o un grupo alquileno C1-8, en cuyo grupo alquileno C1-8, 1 o 2 miembros -CH2- del anillo son opcionalmente reemplazados con miembros hetero del anillo independientemente seleccionados a partir del grupo que consiste en -N(H)-, -N[alquilo C1-8]-, -O-, -S-, -S(=O)- o -S(=O)2-; R6 es hidrogeno; alquilo C1-8; halo-alquilo C1-8; hidroxialquilo C1-8, alcoxilo C1-8-alquilo C1-8; mercapto-alquilo C1-8, tioalquilo C1-8-alquilo C1-8; amino-alquilo C1-8; N-alquilo C1-8-amino-alquilo C1-8; N,N-di-[alquilo C1-8]-aminoalquilo C1-8 con dos fracciones de alquilo C1-8 idénticas o diferentes en la fraccion de N,N-di-[alquilo C1-8]-amino; alquenilo C2-8; o alquinilo C2-8; E1 es -C(R7)-(R8)-; o -C(R7)-(R8)-C(Rg)-(R10)-; E2 es -C(R11)-(R12)-; o -C(R11)-(R12)-C(R13)-(R14)-; cualquiera de cada uno de R7 y R8 se selecciona independientemente a partir del grupo que consiste en hidrogeno, ciano, halogeno, alquilo C1-8, halo-alquilo C1-8, alcoxilo C1-8-alquilo C1-8, y tioalquilo C1-8-alquilo C1-8; o R7 y R8, tomados juntos, son oxo o -CH2-CH2-; cualquiera de cada uno de R9 y R10 se selecciona independientemente a partir del grupo que consiste en hidrogeno, ciano, halogeno, alquilo C1-8, halo-alquilo C1-8, alcoxilo C1-8-alquilo C1-8, y tioalquilo C1-8-alquilo C1-8; o R9 y R10, tomados juntos, son oxo o -CH2-CH2-; cualquiera de cada uno de R11 y R12 se selecciona independientemente a partir del grupo que consiste en hidrogeno, ciano, halogeno, alquilo C1-8, halo-alquilo C1-8, alcoxilo C1-8-alquilo C1-8, y tioalquilo C1-8-alquilo C1-8; o R11 y R12, tomados juntos, son oxo o -CH2-CH2-; y cualquiera de cada uno de R13 y R14 se selecciona independientemente a partir del grupo que consiste en hidrogeno, ciano, halogeno, alquilo C1-8, halo-alquilo C1-8, alcoxilo C1-8-alquilo C1-8, y tioalquilo C1-8-alquilo C1-8; o R13 y R14, tomados juntos, son oxo o -CH2-CH2-.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US22847209P | 2009-07-24 | 2009-07-24 | |
US25891109P | 2009-11-06 | 2009-11-06 | |
US36370210P | 2010-07-13 | 2010-07-13 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR077328A1 true AR077328A1 (es) | 2011-08-17 |
Family
ID=42629546
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP100102667A AR077328A1 (es) | 2009-07-24 | 2010-07-22 | Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos |
Country Status (27)
Country | Link |
---|---|
US (5) | US8207164B2 (es) |
EP (1) | EP2456763B1 (es) |
JP (1) | JP5767214B2 (es) |
KR (2) | KR101422965B1 (es) |
CN (1) | CN102471293B (es) |
AR (1) | AR077328A1 (es) |
AU (1) | AU2010274913B2 (es) |
CA (1) | CA2768980A1 (es) |
CL (1) | CL2012000185A1 (es) |
CO (1) | CO6491058A2 (es) |
CR (1) | CR20120002A (es) |
CU (1) | CU24083B1 (es) |
EA (1) | EA201200174A1 (es) |
EC (1) | ECSP12011622A (es) |
ES (1) | ES2534315T3 (es) |
GT (1) | GT201200016A (es) |
HK (1) | HK1166314A1 (es) |
IL (1) | IL217378A (es) |
MA (1) | MA33450B1 (es) |
MX (1) | MX2012001070A (es) |
NZ (1) | NZ597529A (es) |
PE (1) | PE20121440A1 (es) |
SG (1) | SG177397A1 (es) |
TW (1) | TW201107316A (es) |
UY (1) | UY32799A (es) |
WO (1) | WO2011009943A1 (es) |
ZA (1) | ZA201200155B (es) |
Families Citing this family (65)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
BRPI0617852A2 (pt) | 2005-10-25 | 2011-08-09 | Shionogi & Co | compostos derivados de aminodi-hidrotiazina assim como composições contendo os mesmos |
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 |
AU2008245082B8 (en) | 2007-04-24 | 2012-09-13 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives substituted with a cyclic group |
WO2009151098A1 (ja) | 2008-06-13 | 2009-12-17 | 塩野義製薬株式会社 | βセクレターゼ阻害作用を有する含硫黄複素環誘導体 |
EP2360155A4 (en) | 2008-10-22 | 2012-06-20 | Shionogi & Co | 2-AMINOPYRIDIN-4-ON AND 2-AMINOPYRIDINE DERIVATIVE WITH BACE1-HEMDERING EFFECT |
AR077328A1 (es) * | 2009-07-24 | 2011-08-17 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos |
US8188079B2 (en) * | 2009-08-19 | 2012-05-29 | Hoffman-La Roche Inc. | 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines |
EP2485591B1 (en) | 2009-10-08 | 2016-03-23 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
WO2011044184A1 (en) | 2009-10-08 | 2011-04-14 | Schering Corporation | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
US8569310B2 (en) | 2009-10-08 | 2013-10-29 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions and their use |
UA103272C2 (uk) | 2009-12-11 | 2013-09-25 | Ф. Хоффманн-Ля Рош Аг | 2-аміно-5,5-дифтор-5,6-дигідро-4h-оксазини як інгібітори bace1 і/або bace2 |
RU2012129168A (ru) | 2009-12-11 | 2014-01-20 | Сионоги Энд Ко. Лтд. | Производные оксазина |
JP5600754B2 (ja) * | 2009-12-31 | 2014-10-01 | ノバルティス アーゲー | ピラジン誘導体および神経障害の処置におけるそれらの使用 |
US8497264B2 (en) | 2010-03-15 | 2013-07-30 | Amgen Inc. | Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
US8673894B2 (en) * | 2010-05-07 | 2014-03-18 | Hoffmann-La Roche Inc. | 2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine or 2,3,6,7-tetrahydro-[1,4]oxazepin-5-ylamine compounds |
EP2580200B1 (en) | 2010-06-09 | 2016-09-14 | Janssen Pharmaceutica, N.V. | 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace) |
JP5128019B1 (ja) * | 2010-07-13 | 2013-01-23 | ノバルティス アーゲー | オキサジン誘導体および神経障害の処置におけるその使用 |
US9018219B2 (en) | 2010-10-29 | 2015-04-28 | Shionogi & Co., Ltd. | Fused aminodihydropyrimidine derivative |
AU2011321427A1 (en) | 2010-10-29 | 2013-05-02 | Shionogi & Co., Ltd. | Naphthyridine derivative |
EP2655376B1 (en) | 2010-12-22 | 2017-08-23 | Janssen Pharmaceutica NV | 5,6-DIHYDRO-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) |
US8524897B2 (en) * | 2011-01-12 | 2013-09-03 | Novartis Ag | Crystalline oxazine derivative |
JP2014505688A (ja) * | 2011-01-12 | 2014-03-06 | ノバルティス アーゲー | オキサジン誘導体および神経障害の処置におけるその使用 |
PT2663561E (pt) | 2011-01-13 | 2016-06-07 | Novartis Ag | Derivados heterocíclicos novos e sua utilização no tratamento de distúrbios neurológicos |
MX2013008192A (es) * | 2011-01-13 | 2013-12-16 | Novartis Ag | Inhibidores de bace-2 para tratamiento de transtornos metabolicos. |
US9242943B2 (en) * | 2011-01-18 | 2016-01-26 | Siena Biotech S.P.A. | 1,4 oxazines as BACE1 and/or BACE2 inhibitors |
US8399459B2 (en) | 2011-02-02 | 2013-03-19 | Hoffmann-La Roche Inc. | 1,4 oxazines as BACE1 and/or BACE2 inhibitors |
US8815841B2 (en) * | 2011-02-18 | 2014-08-26 | Hoffmann-La Roche Inc. | 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors |
MX338333B (es) * | 2011-03-01 | 2016-04-11 | Janssen Pharmaceutica Nv | DERIVADOS DE 6,7-DIHIDRO-PIRAZOLO [1,5ª]PIRAZIN-4-ILAMINA UTILES COMO INHIBIDORES DE BETA-SECRETASA (BACE). |
US9067924B2 (en) * | 2011-03-04 | 2015-06-30 | Hoffmann-La Roche Inc. | 1,4 thiazepines/sulfones as BACE1 and/or BACE2 inhibitors |
CN103415521B (zh) | 2011-03-09 | 2016-01-06 | 詹森药业有限公司 | 用作β分泌酶(BACE)抑制剂的3,4-二氢-吡咯并[1,2-a]吡嗪-1-基胺衍生物 |
US8748418B2 (en) * | 2011-03-18 | 2014-06-10 | Hoffmann-La Roche Inc. | 1,4-oxazepines as BACE1 and/or BACE2 inhibitors |
US8877744B2 (en) * | 2011-04-04 | 2014-11-04 | Hoffmann-La Roche Inc. | 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors |
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 |
US8754075B2 (en) | 2011-04-11 | 2014-06-17 | Hoffmann-La Roche Inc. | 1,3-oxazines as BACE1 and/or BACE2 inhibitors |
JP2014514302A (ja) | 2011-04-13 | 2014-06-19 | メルク・シャープ・アンド・ドーム・コーポレーション | Bace阻害薬としての5−置換されたイミノチアジン類およびそれのモノおよびジオキシド、組成物およびそれらの使用 |
JPWO2012147763A1 (ja) | 2011-04-26 | 2014-07-28 | 塩野義製薬株式会社 | オキサジン誘導体およびそれを含有するbace1阻害剤 |
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 |
KR20140041590A (ko) * | 2011-06-07 | 2014-04-04 | 에프. 호프만-라 로슈 아게 | [1,3]옥사진 |
PE20140623A1 (es) * | 2011-06-07 | 2014-05-30 | Hoffmann La Roche | Halogenoalquil-1,3-oxazinas como inhibidores de la bace1 y/o bace2 |
US8927535B2 (en) * | 2011-07-06 | 2015-01-06 | Hoffman-La Roche Inc. | Cyclopropyl-fused-1,3-thiazepines as BACE1 and/or BACE2 inhibitors |
AU2012298983A1 (en) | 2011-08-22 | 2014-02-27 | Merck Sharp & Dohme Corp. | 2-spiro-substituted iminothiazines and their mono-and dioxides as BACE inhibitors, compositions and their use |
WO2013044092A1 (en) | 2011-09-21 | 2013-03-28 | Amgen Inc. | Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
MX2014004479A (es) | 2011-10-13 | 2014-08-01 | Novartis Ag | Derivados de oxazina novedosos y su uso en el tratamiento de enfermedades. |
UA111749C2 (uk) * | 2011-12-05 | 2016-06-10 | Янссен Фармацевтика Нв | Похідні 6-дифторметил-5,6-дигідро-2h-[1,4]оксазин-3-аміну |
ES2582473T3 (es) * | 2011-12-06 | 2016-09-13 | Janssen Pharmaceutica, N.V. | Derivados de 5-(3-aminofenil)-5-alquil-5,6-dihidro-2H-[1,4]oxazin-3-amina para el tratamiento de trastornos en que está implicada la beta-secretasa |
AR089781A1 (es) * | 2012-01-26 | 2014-09-17 | Hoffmann La Roche | Fluorometil-5,6-dihidro-4h-[1,3]oxazinas |
US8338413B1 (en) | 2012-03-07 | 2012-12-25 | Novartis Ag | Oxazine derivatives and their use in the treatment of neurological disorders |
WO2014059185A1 (en) | 2012-10-12 | 2014-04-17 | Amgen Inc. | Amino - dihydrothiazine and amino - dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use |
EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY |
US9725469B2 (en) | 2012-11-15 | 2017-08-08 | Amgen, Inc. | Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
AU2013363151A1 (en) | 2012-12-20 | 2015-06-04 | Merck Sharp & Dohme Corp. | C5, C6 oxacyclic-fused iminothiazine dioxide compounds as BACE inhibitors |
TW201512171A (zh) | 2013-04-19 | 2015-04-01 | Pfizer Ltd | 化學化合物 |
US9751886B2 (en) | 2013-06-12 | 2017-09-05 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-6,7-dihydro[1,2,3]triazolo[1,5-A]pyrazine derivatives as inhibitors of beta-secretase (BACE) |
WO2014198853A1 (en) | 2013-06-12 | 2014-12-18 | Janssen Pharmaceutica Nv | 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace) |
CN105452251B (zh) | 2013-06-12 | 2017-12-26 | 詹森药业有限公司 | 作为β‑分泌酶(BACE)抑制剂的4‑氨基‑6‑苯基‑5,6‑二氢咪唑并[1,5‑A]吡嗪‑3(2H)‑酮衍生物 |
FR3025591B1 (fr) * | 2014-09-05 | 2016-10-14 | Technofan | Dispositif de ventilation, aeronef comportant un tel dispositif de ventilation et procede de surveillance associe |
KR20170095881A (ko) | 2014-12-18 | 2017-08-23 | 얀센 파마슈티카 엔.브이. | 베타―세크레타제의 2,3,4,5―테트라히드로피리딘―6―아민 및 3,4―디히드로―2h―피롤―5―아민 화합물 억제제 |
TW201726651A (zh) * | 2015-09-23 | 2017-08-01 | 健生藥品公司 | 2,3,4,5-四氫吡啶-6-胺衍生物 |
CN109661397A (zh) * | 2016-08-26 | 2019-04-19 | 伊莱利利公司 | 用作选择性bace1抑制剂的1,4-噁嗪类化合物 |
US10159191B2 (en) | 2016-09-23 | 2018-12-25 | Deere & Company | Harvester grain unloader |
CN110018266B (zh) * | 2019-02-15 | 2022-03-04 | 广州市妇女儿童医疗中心 | 一种快速定量分析48种氨基酸的方法 |
CN112250580A (zh) * | 2020-10-28 | 2021-01-22 | 上海昂卓新材料科技有限公司 | 一种2-硝基-2-取代苯基丙烷-1,3-二醇的制备方法 |
Family Cites Families (37)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
NL6911868A (es) | 1968-08-31 | 1970-03-03 | ||
PT72878B (en) | 1980-04-24 | 1983-03-29 | Merck & Co Inc | Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents |
IL112778A0 (en) | 1994-03-04 | 1995-05-26 | Merck & Co Inc | Substituted heterocycles, their preparation and pharmaceutical compositions containing them |
TW200502221A (en) * | 2002-10-03 | 2005-01-16 | Astrazeneca Ab | Novel lactams and uses thereof |
CA2514733A1 (en) | 2003-02-28 | 2004-09-16 | Transform Pharmaceuticals, Inc. | Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen |
AR043633A1 (es) | 2003-03-20 | 2005-08-03 | Schering Corp | Ligandos de receptores de canabinoides |
WO2005063738A1 (ja) | 2003-12-29 | 2005-07-14 | Banyu Pharmaceutical Co.,Ltd | 新規2-へテロアリール置換ベンズイミダゾール誘導体 |
WO2005079802A1 (en) | 2004-02-12 | 2005-09-01 | Merck & Co., Inc. | Bipyridyl amides as modulators of metabotropic glutamate receptor-5 |
TW200624426A (en) * | 2004-09-21 | 2006-07-16 | Lilly Co Eli | BACE inhibitors |
US7888374B2 (en) | 2005-01-28 | 2011-02-15 | Abbott Laboratories | Inhibitors of c-jun N-terminal kinases |
BRPI0617852A2 (pt) | 2005-10-25 | 2011-08-09 | Shionogi & Co | compostos derivados de aminodi-hidrotiazina assim como composições contendo os mesmos |
EP2132177B1 (en) | 2007-03-01 | 2013-07-17 | Novartis AG | Pim kinase inhibitors and methods of their use |
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 |
AU2008245082B8 (en) | 2007-04-24 | 2012-09-13 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives substituted with a cyclic group |
GB0713686D0 (en) | 2007-07-13 | 2007-08-22 | Addex Pharmaceuticals Sa | New compounds 2 |
US20100317850A1 (en) | 2008-01-18 | 2010-12-16 | Yuichi Suzuki | Condensed aminodihydrothiazine derivative |
US20100197688A1 (en) | 2008-05-29 | 2010-08-05 | Nantermet Philippe G | Epha4 rtk inhibitors for treatment of neurological and neurodegenerative disorders and cancer |
WO2009151098A1 (ja) | 2008-06-13 | 2009-12-17 | 塩野義製薬株式会社 | βセクレターゼ阻害作用を有する含硫黄複素環誘導体 |
TW201028381A (en) | 2008-07-14 | 2010-08-01 | Shionogi & Co | Pyridine derivative having ttk inhibition activity |
EP2360155A4 (en) | 2008-10-22 | 2012-06-20 | Shionogi & Co | 2-AMINOPYRIDIN-4-ON AND 2-AMINOPYRIDINE DERIVATIVE WITH BACE1-HEMDERING EFFECT |
US9237972B2 (en) | 2008-12-16 | 2016-01-19 | Kimberly-Clark Worldwide, Inc. | Liquid surfactant compositions that adhere to surfaces and solidify and swell in the presence of water and articles using the same |
US8461160B2 (en) | 2009-05-08 | 2013-06-11 | Hoffmann-La Roche, Inc. | Dihydropyrimidinones |
AR077328A1 (es) | 2009-07-24 | 2011-08-17 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos |
US8188079B2 (en) | 2009-08-19 | 2012-05-29 | Hoffman-La Roche Inc. | 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines |
US20120238557A1 (en) | 2009-11-13 | 2012-09-20 | Shionogi & Co., Ltd. | Aminothiazine or aminooxazine derivative having amino linker |
US7964594B1 (en) | 2009-12-10 | 2011-06-21 | Hoffmann-La Roche Inc. | Amino oxazine derivatives |
RU2012129168A (ru) | 2009-12-11 | 2014-01-20 | Сионоги Энд Ко. Лтд. | Производные оксазина |
UA103272C2 (uk) | 2009-12-11 | 2013-09-25 | Ф. Хоффманн-Ля Рош Аг | 2-аміно-5,5-дифтор-5,6-дигідро-4h-оксазини як інгібітори bace1 і/або bace2 |
US8673894B2 (en) * | 2010-05-07 | 2014-03-18 | Hoffmann-La Roche Inc. | 2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine or 2,3,6,7-tetrahydro-[1,4]oxazepin-5-ylamine compounds |
US20130079349A1 (en) | 2010-06-09 | 2013-03-28 | Janssen Pharmaceutica Nv | 5-amino-3,6-dihydro-1h-pyrazin-2-one derivatives useful as inhibitors of beta-secretase (bace) |
EP2580200B1 (en) | 2010-06-09 | 2016-09-14 | Janssen Pharmaceutica, N.V. | 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace) |
JP5128019B1 (ja) * | 2010-07-13 | 2013-01-23 | ノバルティス アーゲー | オキサジン誘導体および神経障害の処置におけるその使用 |
US8524897B2 (en) | 2011-01-12 | 2013-09-03 | Novartis Ag | Crystalline oxazine derivative |
JP2014505688A (ja) | 2011-01-12 | 2014-03-06 | ノバルティス アーゲー | オキサジン誘導体および神経障害の処置におけるその使用 |
MX2013008192A (es) | 2011-01-13 | 2013-12-16 | Novartis Ag | Inhibidores de bace-2 para tratamiento de transtornos metabolicos. |
PT2663561E (pt) | 2011-01-13 | 2016-06-07 | Novartis Ag | Derivados heterocíclicos novos e sua utilização no tratamento de distúrbios neurológicos |
MX2014004479A (es) | 2011-10-13 | 2014-08-01 | Novartis Ag | Derivados de oxazina novedosos y su uso en el tratamiento de enfermedades. |
-
2010
- 2010-07-22 AR ARP100102667A patent/AR077328A1/es unknown
- 2010-07-22 UY UY0001032799A patent/UY32799A/es not_active Application Discontinuation
- 2010-07-23 NZ NZ597529A patent/NZ597529A/xx not_active IP Right Cessation
- 2010-07-23 PE PE2012000094A patent/PE20121440A1/es not_active Application Discontinuation
- 2010-07-23 KR KR1020127001651A patent/KR101422965B1/ko not_active IP Right Cessation
- 2010-07-23 JP JP2012521053A patent/JP5767214B2/ja not_active Expired - Fee Related
- 2010-07-23 CU CU2012000013A patent/CU24083B1/es not_active IP Right Cessation
- 2010-07-23 US US12/842,360 patent/US8207164B2/en active Active
- 2010-07-23 TW TW099124438A patent/TW201107316A/zh unknown
- 2010-07-23 EA EA201200174A patent/EA201200174A1/ru unknown
- 2010-07-23 ES ES10737870.5T patent/ES2534315T3/es active Active
- 2010-07-23 SG SG2011096823A patent/SG177397A1/en unknown
- 2010-07-23 CN CN201080035169.0A patent/CN102471293B/zh not_active Expired - Fee Related
- 2010-07-23 KR KR1020137033812A patent/KR20140004810A/ko not_active Application Discontinuation
- 2010-07-23 EP EP10737870.5A patent/EP2456763B1/en not_active Revoked
- 2010-07-23 WO PCT/EP2010/060718 patent/WO2011009943A1/en active Application Filing
- 2010-07-23 MA MA34558A patent/MA33450B1/fr unknown
- 2010-07-23 AU AU2010274913A patent/AU2010274913B2/en not_active Ceased
- 2010-07-23 CA CA2768980A patent/CA2768980A1/en not_active Abandoned
- 2010-07-23 MX MX2012001070A patent/MX2012001070A/es active IP Right Grant
-
2012
- 2012-01-05 IL IL217378A patent/IL217378A/en not_active IP Right Cessation
- 2012-01-09 CR CR20120002A patent/CR20120002A/es unknown
- 2012-01-09 ZA ZA2012/00155A patent/ZA201200155B/en unknown
- 2012-01-19 CO CO12007858A patent/CO6491058A2/es active IP Right Grant
- 2012-01-23 CL CL2012000185A patent/CL2012000185A1/es unknown
- 2012-01-24 GT GT201200016A patent/GT201200016A/es unknown
- 2012-01-24 EC EC2012011622A patent/ECSP12011622A/es unknown
- 2012-04-24 US US13/454,751 patent/US20120238560A1/en not_active Abandoned
- 2012-07-16 HK HK12106945.9A patent/HK1166314A1/xx not_active IP Right Cessation
-
2013
- 2013-07-12 US US13/940,354 patent/US20140088084A1/en not_active Abandoned
- 2013-12-20 US US14/136,679 patent/US8846658B2/en active Active
-
2014
- 2014-07-07 US US14/324,883 patent/US20150018338A1/en not_active Abandoned
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
AR077328A1 (es) | Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos | |
AR072906A1 (es) | Nucleosidos modificados utiles como antivirales | |
AR084849A1 (es) | Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos | |
AR072952A1 (es) | Compuestos de 2-imino-3-metilpirrolopirimidinona fenilo-sustituida como inhibidores de bace-1, composiciones y su uso | |
AR078408A1 (es) | Derivados de indol como moduladores de los crac | |
AR080865A1 (es) | Derivados de espirotetrahidronaftaleno, composiciones farmaceuticas que los contienen, proceso de preparacion y uso de los mismos para tratar enfermedades neurodegenerativas,tal como alzheimer. | |
AR063602A1 (es) | Derivados de espiroindolinona, formulaciones farmaceuticas que los contienen y su uso en la obtencion de un medicamento para el tratamiento de trastornos oncologicos. | |
AR089019A1 (es) | Derivados modificados de 4-fenil-piridina | |
AR087668A1 (es) | Derivados de oxazina y su uso en el tratamiento de enfermedades | |
UY32462A (es) | Derivados de bifenilo novedosos para el tratamiento de infección por virus de hepatitis c 644 | |
AR064608A1 (es) | Derivados de pirazolo-quinazolina sustituidos, composiciones farmaceuticas que los contienen. proceso para su preparacion y uso de los mismos como agentes anticancer. | |
AR082885A1 (es) | Compuestos y composiciones para la inhibicion de nampt | |
AR077505A1 (es) | Compuestos de piridina y sus usos | |
AR075729A1 (es) | Derivados de benzofuranilo, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de la obesidad y/o diabetes. | |
AR054560A1 (es) | Espiropiperidina como inhibidores de beta-secretasa para el tratamiento de la enfermedad de alzheimer | |
DOP2007000079A (es) | Compuestos fenil amido heterocíclicos condensados | |
RU2015125591A (ru) | БЕНЗИЛСУЛЬФОНАМИДНЫЕ ПРОИЗВОДНЫЕ КАК МОДУЛЯТОРЫ RORc | |
AR054890A1 (es) | Derivados de quinolina como agentes antibacterianos | |
BR112014023384A2 (pt) | inibidores de bace de di-hidro-tiazina e di-hidro-oxazina espirocíclicos, e composições e usos dos mesmos | |
UY31554A1 (es) | Nuevos inhibidores de acetil coenzima a carboxilasa y usos en tratamientos de obesidad y diabetes mellitus | |
AR082889A1 (es) | Compuestos y composiciones para la inhibicion de nampt | |
AR089568A1 (es) | Compuestos heterociclicos y sus metodos de usos | |
AR082111A1 (es) | Furopiridinas o tienopiridinas condensadas, composiciones farmaceuticas que las contienen utiles para tratar trastornos psicoticos y del sistema nervioso central, y metodo de preparacion de las mismas | |
PE20142081A1 (es) | Inhibidores de quinurenina-3-monooxigenasa, composiciones farmaceuticas y metodo de uso de los mismos | |
AR054000A1 (es) | Compuesto de n-(fenilpropil)-sulfonamida, composicion farmaceutica que lo comprende, su uso para la fabricacion de un medicamento, producto de combinacion que comprende dicho compuesto y metodo para prepararlo |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
FB | Suspension of granting procedure |