NI201200044A - Compuestos de dióxido de iminotiadiazina como inhibodores de bace , composiciones y su uso - Google Patents

Compuestos de dióxido de iminotiadiazina como inhibodores de bace , composiciones y su uso

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Publication number
NI201200044A
NI201200044A NI201200044A NI201200044A NI201200044A NI 201200044 A NI201200044 A NI 201200044A NI 201200044 A NI201200044 A NI 201200044A NI 201200044 A NI201200044 A NI 201200044A NI 201200044 A NI201200044 A NI 201200044A
Authority
NI
Nicaragua
Prior art keywords
compounds
bace
dioxide compounds
inhibodors
iminotiadiazine
Prior art date
Application number
NI201200044A
Other languages
English (en)
Inventor
D Scott Jacke
W Stamford Andrew
J Gilbert Eric
N Cumming Jared
Iserloh Ulrich
A Misiaszek Jeffrey
Li Guoqing
Original Assignee
Merck Sharp & Dohme
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43857101&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=NI201200044(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of NI201200044A publication Critical patent/NI201200044A/es

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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/549—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 sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
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    • 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
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    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C07C309/30—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/89—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to the ring nitrogen atom
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    • 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
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Abstract

En sus muchas realizaciones, la presente invención proporciona ciertos compuestos de dióxido de iminotiadiazina, incluyendo los compuestos de la Fórmula (I): e incluyen sus estereoisómeros, y las sales farmacéuticamente aceptables de dichos compuestos, estereoisómeros, donde cada uno de R1, R2, R3, R4, R5, R9, el anillo A, el anillo B, m, n, p, -L1, -L2-, y -L3- se selecciona independientemente y según lo definido en esta invención. Se ha descubierto, sorprendentemente, que los compuestos de dióxido de iminotiadiazina novedosos de la invención exhiben propiedades las cuales se espera que los convierta en ventajosos como inhibidores de BACE y/o para el tratamiento y prevención de diversas patologías relacionadas con la producción de Beta-amiloides ("ABeta"). También se describen composiciones farmacéuticas que comprenden uno o más de dichos compuestos (solos y en combinación con uno o más otros agentes activos), y métodos para su preparación y uso en el tratamiento de patologías asociadas con la proteína amiloide beta (ABeta), incluyendo la enfermedad de Alzheimer.
NI201200044A 2009-10-08 2012-03-20 Compuestos de dióxido de iminotiadiazina como inhibodores de bace , composiciones y su uso NI201200044A (es)

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