MA33726B1 - Composes de dioxyde d'iminothiadiazine comme inhibiteurs de bace, compositions et leur utlisation - Google Patents

Composes de dioxyde d'iminothiadiazine comme inhibiteurs de bace, compositions et leur utlisation

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Publication number
MA33726B1
MA33726B1 MA34836A MA34836A MA33726B1 MA 33726 B1 MA33726 B1 MA 33726B1 MA 34836 A MA34836 A MA 34836A MA 34836 A MA34836 A MA 34836A MA 33726 B1 MA33726 B1 MA 33726B1
Authority
MA
Morocco
Prior art keywords
compounds
dioxide compounds
iminotiadiazine
formulations
stereoisomers
Prior art date
Application number
MA34836A
Other languages
Arabic (ar)
English (en)
Inventor
Jack D Scott
Andrew W Stamford
Eric J Gilbert
Jared N Cumming
Ulrich Iserloh
Jeffrey A Misiaszek
Guoqing Li
Original Assignee
Schering Corp
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=MA33726(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Schering Corp filed Critical Schering Corp
Publication of MA33726B1 publication Critical patent/MA33726B1/fr

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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • 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
    • A61K31/54—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
    • 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
    • A61K31/54—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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    • 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
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    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • 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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    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/15—Six-membered rings
    • C07D285/16—Thiadiazines; Hydrogenated thiadiazines
    • C07D285/18—1,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines
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    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
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    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
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    • 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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    • 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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    • C07D495/04—Ortho-condensed systems
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    • 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
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    • C07D213/24—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 having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D239/08—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms directly attached in position 2
    • C07D239/12—Nitrogen atoms not forming part of a nitro radical
    • C07D239/14—Nitrogen atoms not forming part of a nitro radical with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to said nitrogen atoms

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Abstract

Dans ses nombreux modes de réalisation, la présente invention concerne certains composés de dioxyde d'iminothiadiazine, notamment des composés de formule (I): (I) et comprend leurs stéréo-isomères, et les sels pharmaceutiquement acceptables desdits stéréo-isomères des composés, chacun parmi R1, R2, R3, R4, R5, R9, cycle A, cycle B, m, n, p, -L1-,L2-, et L3- étant indépendamment choisi et tel que défini ici. Etonnamment, les nouveaux composés de dioxyde d'iminothiadiazine de l'invention se sont révélés présenter des propriétés qui font espérer qu'elles les rendront avantageux en tant qu'inhibiteurs de BACE et/ou pour le traitement et la prévention de diverses pathologies liées à la production de ²-amyloïde (A²). L'invention concerne également des compositions pharmaceutiques comprenant un ou plusieurs de ces composés (seuls et en combinaison avec un ou plusieurs autres agents actifs), et des procédés pour leur préparation et leur utilisation dans le traitement de pathologies associées à la protéine amyloïde bêta (A²), notamment la maladie d'Alzheimer.
MA34836A 2009-10-08 2012-05-04 Composes de dioxyde d'iminothiadiazine comme inhibiteurs de bace, compositions et leur utlisation MA33726B1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US24968509P 2009-10-08 2009-10-08
PCT/US2010/051553 WO2011044181A1 (fr) 2009-10-08 2010-10-06 Composés de dioxyde d'iminothiadiazine comme inhibiteurs de bace, compositions et leur utilisation

Publications (1)

Publication Number Publication Date
MA33726B1 true MA33726B1 (fr) 2012-11-01

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MA34836A MA33726B1 (fr) 2009-10-08 2012-05-04 Composes de dioxyde d'iminothiadiazine comme inhibiteurs de bace, compositions et leur utlisation

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US (6) US8729071B2 (fr)
EP (2) EP2485736B1 (fr)
JP (4) JP5592494B2 (fr)
KR (3) KR101646424B1 (fr)
CN (2) CN104744403A (fr)
AR (1) AR078534A1 (fr)
AU (1) AU2010303591B2 (fr)
BR (1) BR112012008014B1 (fr)
CA (1) CA2774579C (fr)
CL (1) CL2012000872A1 (fr)
CR (1) CR20120158A (fr)
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