AT396973T - Benzyl ether and benzylamino-beta-secretase inhibitors for treatment of alzheimer's disease - Google Patents

Benzyl ether and benzylamino-beta-secretase inhibitors for treatment of alzheimer's disease

Info

Publication number
AT396973T
AT396973T AT04789263T AT04789263T AT396973T AT 396973 T AT396973 T AT 396973T AT 04789263 T AT04789263 T AT 04789263T AT 04789263 T AT04789263 T AT 04789263T AT 396973 T AT396973 T AT 396973T
Authority
AT
Austria
Prior art keywords
benzylamino
alzheimer
beta
disease
treatment
Prior art date
Application number
AT04789263T
Other languages
German (de)
Inventor
Philippe Nantermet
Hemaka Anthony Rajapakse
Harold Selnick
Original Assignee
Merck & Co Inc
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
Priority to US50836903P priority Critical
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of AT396973T publication Critical patent/AT396973T/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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 heteroatoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00Carboxylic acid nitriles
    • C07C255/49Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/57Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and carboxyl groups, other than cyano groups, bound to the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/01Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/08Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/06Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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 heteroatoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/76Nitrogen atoms to which a second hetero atom is attached
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/16Heterocyclic 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 acylated on ring nitrogen atoms
    • C07D295/18Heterocyclic 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 acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182Radicals derived from carboxylic acids
    • C07D295/192Radicals derived from carboxylic acids from aromatic carboxylic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulfur
    • C07D333/06Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulfur with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/14Radicals substituted by singly bound hetero atoms other than halogen
    • C07D333/20Radicals substituted by singly bound hetero atoms other than halogen by nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/02Systems containing only non-condensed rings with a three-membered ring
AT04789263T 2003-10-03 2004-09-29 Benzyl ether and benzylamino-beta-secretase inhibitors for treatment of alzheimer's disease AT396973T (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
US50836903P true 2003-10-03 2003-10-03

Publications (1)

Publication Number Publication Date
AT396973T true AT396973T (en) 2008-06-15

Family

ID=34421727

Family Applications (1)

Application Number Title Priority Date Filing Date
AT04789263T AT396973T (en) 2003-10-03 2004-09-29 Benzyl ether and benzylamino-beta-secretase inhibitors for treatment of alzheimer's disease

Country Status (9)

Country Link
US (2) US7829597B2 (en)
EP (1) EP1673078B1 (en)
JP (1) JP4649413B2 (en)
CN (1) CN1859904A (en)
AT (1) AT396973T (en)
AU (1) AU2004277981B2 (en)
CA (1) CA2540452A1 (en)
DE (1) DE602004014170D1 (en)
WO (1) WO2005032471A2 (en)

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JP5930573B2 (en) 2007-03-01 2016-06-15 プロビオドルグ エージー A new use of glutaminyl cyclase inhibitors
EP1689713B1 (en) * 2003-11-24 2011-07-27 Merck Sharp & Dohme Corp. Benzylether and benzylamino beta-secretase inhibitors for the treatment of alzheimer s disease
CA2548849A1 (en) 2003-12-19 2005-07-21 Merck & Co., Inc. Phenylamide and pyridylamide beta-secretase inhibitors for the treatment of alzheimer's disease
AU2005236063A1 (en) 2004-04-20 2005-11-03 Merck & Co., Inc. 2, 4, 6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's disease
WO2005103020A1 (en) 2004-04-20 2005-11-03 Merck & Co., Inc. 1,3,5-substituted phenyl derivative compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease
US7714021B2 (en) 2004-06-15 2010-05-11 Merck & Co., Inc. Pyrrolidin-3-yl compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's disease
JP2008520670A (en) * 2004-11-17 2008-06-19 メルク エンド カムパニー インコーポレーテッドMerck & Company Incoporated Macrocyclic tertiary amine β- secretase inhibitors for the treatment of Alzheimer's disease
JP2008520718A (en) * 2004-11-23 2008-06-19 メルク エンド カムパニー インコーポレーテッドMerck & Company Incoporated Useful as β- secretase inhibitors for the treatment of Alzheimer's disease 2,3,4,6-substituted pyridyl derivative compounds
US7951949B2 (en) * 2004-11-23 2011-05-31 Merck, Sharp & Dohme, Corp. Macrocyclic aminopyridyl beta-secretase inhibitors for the treatment of Alzheimer's disease
EP1912963B1 (en) * 2005-08-03 2011-10-12 Merck Sharp & Dohme Corp. Cyclic ketal beta-secretase inhibitors for the treatment of alzheimer's disease
WO2007019078A2 (en) * 2005-08-03 2007-02-15 Merck & Co., Inc. Tricyclic beta-secretase inhibitors for the treatment of alzheimer's disease
AU2006315817A1 (en) * 2005-11-16 2007-05-24 Merck & Co., Inc. Imidazolidinone compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's disease
CA2664130A1 (en) * 2006-09-21 2008-03-27 Merck & Co., Inc. Piperidine and pyrrolidine beta-secretase inhibitors for the treatment of alzheimer's disease
WO2008055945A1 (en) 2006-11-09 2008-05-15 Probiodrug Ag 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases
WO2008065141A1 (en) 2006-11-30 2008-06-05 Probiodrug Ag Novel inhibitors of glutaminyl cyclase
US7960506B2 (en) * 2006-12-14 2011-06-14 Aileron Therapeutics, Inc. Bis-sulfhydryl macrocyclization systems
EP2952522A1 (en) 2007-01-31 2015-12-09 Dana-Farber Cancer Institute, Inc. Stabilized p53 peptides and uses thereof
EP2564862B1 (en) 2007-02-23 2017-08-02 Aileron Therapeutics, Inc. Substituted amino acids for preparing triazole linked macrocyclic peptides
US9656991B2 (en) 2007-04-18 2017-05-23 Probiodrug Ag Inhibitors of glutaminyl cyclase
MX2010009561A (en) * 2008-02-29 2010-09-24 Renovis Inc Amide compounds, compositions and uses thereof.
WO2010033168A2 (en) 2008-09-18 2010-03-25 Renovis, Inc. Amide compounds, compositions and uses thereof
US9181182B2 (en) 2008-10-17 2015-11-10 Akaal Pharma Pty Ltd S1P receptors modulators
WO2010043000A1 (en) 2008-10-17 2010-04-22 Akaal Pharma Pty Ltd S1p receptors modulators and their use thereof
BRPI1006139A2 (en) 2009-01-14 2017-05-30 Aileron Therapeutics Inc peptidomimetic macrocycles
EP2475428B1 (en) 2009-09-11 2015-07-01 Probiodrug AG Heterocylcic derivatives as inhibitors of glutaminyl cyclase
EA025120B1 (en) 2009-10-08 2016-11-30 Мерк Шарп Энд Домэ Корп. Iminothiadiazine dioxide derivatives as bace inhibitors, compositions based thereon, and their use
ES2586231T3 (en) 2010-03-03 2016-10-13 Probiodrug Ag Glutaminyl cyclase inhibitors
CN102791704B (en) 2010-03-10 2015-11-25 前体生物药物股份公司 Glutaminyl cyclase (qc, ec 2.3.2.5) heterocyclic inhibitors
JP5945532B2 (en) 2010-04-21 2016-07-05 プロビオドルグ エージー Benzimidazole derivatives as inhibitors of glutaminyl cyclase
MX355543B (en) 2010-08-13 2018-04-20 Aileron Therapeutics Inc Star Peptidomimetic macrocycles.
US8530670B2 (en) 2011-03-16 2013-09-10 Probiodrug Ag Inhibitors
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JP6450191B2 (en) 2012-02-15 2019-01-09 エイルロン セラピューティクス,インコーポレイテッド Peptide macrocycles
JP6450192B2 (en) 2012-02-15 2019-01-09 エイルロン セラピューティクス,インコーポレイテッド And triazoles crosslinked, and thioether crosslinked peptidomimetic macrocycles
CN104812384A (en) 2012-11-01 2015-07-29 爱勒让治疗公司 Disubstituted amino acids and methods of preparation and use thereof
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EP3461819A1 (en) 2017-09-29 2019-04-03 Probiodrug AG Inhibitors of glutaminyl cyclase

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Also Published As

Publication number Publication date
WO2005032471A2 (en) 2005-04-14
EP1673078A2 (en) 2006-06-28
AU2004277981A1 (en) 2005-04-14
EP1673078B1 (en) 2008-05-28
US20060293380A1 (en) 2006-12-28
WO2005032471A3 (en) 2005-07-07
JP2007507515A (en) 2007-03-29
CA2540452A1 (en) 2005-04-14
EP1673078A4 (en) 2007-04-18
AU2004277981B2 (en) 2009-10-01
CN1859904A (en) 2006-11-08
US8008315B2 (en) 2011-08-30
JP4649413B2 (en) 2011-03-09
US7829597B2 (en) 2010-11-09
US20100210693A1 (en) 2010-08-19
DE602004014170D1 (en) 2008-07-10

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