AT402934T - Malonamidderivate as gamma-secretase inhibitors - Google Patents

Malonamidderivate as gamma-secretase inhibitors

Info

Publication number
AT402934T
AT402934T AT04705404T AT04705404T AT402934T AT 402934 T AT402934 T AT 402934T AT 04705404 T AT04705404 T AT 04705404T AT 04705404 T AT04705404 T AT 04705404T AT 402934 T AT402934 T AT 402934T
Authority
AT
Austria
Prior art keywords
malonamidderivate
gamma
secretase inhibitors
secretase
inhibitors
Prior art date
Application number
AT04705404T
Other languages
German (de)
Inventor
Guido Galley
Annick Goergler
Helmut Jacobsen
Eric Kitas
Jens-Uwe Peters
Original Assignee
Hoffmann La Roche
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 EP03002190 priority Critical
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AT402934T publication Critical patent/AT402934T/en

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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/22Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/01Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/45Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C07C233/46Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/47Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/23Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C323/39Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton at least one of the nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom
    • C07C323/40Y being a hydrogen or a carbon atom
    • C07C323/41Y being a hydrogen or an acyclic carbon atom
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44Iso-indoles; Hydrogenated iso-indoles
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    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20Oxygen atoms
    • C07D215/22Oxygen atoms attached in position 2 or 4
    • C07D215/227Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
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    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
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    • C07D217/06Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with the ring nitrogen atom acylated by carboxylic or carbonic acids, or with sulfur or nitrogen analogues thereof, e.g. carbamates
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D223/00Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/18Dibenzazepines; Hydrogenated dibenzazepines
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D243/00Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1,4
    • C07D243/10Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1,4 condensed with carbocyclic rings or ring systems
    • C07D243/121,5-Benzodiazepines; Hydrogenated 1,5-benzodiazepines
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    • C07D243/00Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1,4
    • C07D243/10Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1,4 condensed with carbocyclic rings or ring systems
    • C07D243/141,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
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    • C07D243/00Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1,4
    • C07D243/10Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1,4 condensed with carbocyclic rings or ring systems
    • C07D243/141,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/161,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/181,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/24Oxygen atoms
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    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/281,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/301,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
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    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/06Heterocyclic 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 linked by a carbon chain containing only aliphatic carbon 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
    • C07D405/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
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    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
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    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/06Peri-condensed systems
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    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/08Bridged systems
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/06Peri-condensed systems
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/12Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14The ring being saturated
AT04705404T 2003-02-04 2004-01-27 Malonamidderivate as gamma-secretase inhibitors AT402934T (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP03002190 2003-02-04

Publications (1)

Publication Number Publication Date
AT402934T true AT402934T (en) 2008-08-15

Family

ID=32842686

Family Applications (1)

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AT04705404T AT402934T (en) 2003-02-04 2004-01-27 Malonamidderivate as gamma-secretase inhibitors

Country Status (23)

Country Link
US (1) US7375099B2 (en)
EP (1) EP1592684B1 (en)
JP (1) JP4662914B2 (en)
KR (1) KR100810810B1 (en)
CN (1) CN100480248C (en)
AR (1) AR042996A1 (en)
AT (1) AT402934T (en)
BR (1) BRPI0407262A (en)
CA (1) CA2514267C (en)
CL (1) CL2004000174A1 (en)
CO (1) CO5580761A2 (en)
DE (1) DE602004015415D1 (en)
ES (1) ES2311795T3 (en)
HR (1) HRP20050663A2 (en)
IL (1) IL169691A (en)
MX (1) MXPA05008172A (en)
NO (1) NO20053627L (en)
NZ (1) NZ541324A (en)
PL (1) PL378405A1 (en)
RU (1) RU2330849C2 (en)
TW (1) TWI293070B (en)
WO (1) WO2004069826A1 (en)
ZA (1) ZA200506212B (en)

Families Citing this family (51)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7521481B2 (en) 2003-02-27 2009-04-21 Mclaurin Joanne Methods of preventing, treating and diagnosing disorders of protein aggregation
WO2008104580A1 (en) 2007-03-01 2008-09-04 Probiodrug Ag New use of glutaminyl cyclase inhibitors
RS20060146A (en) * 2003-09-09 2008-06-05 F.Hoffmann-La Roche Ag., Malonamide derivatives blocking the activity of gama-secretase
AU2004283803B2 (en) 2003-10-06 2010-06-24 F. Hoffmann-La Roche Ag Substituted dibenzo-azepine and benzo-diazepine derivatives useful as gamma-secretase inhibitors
US7211573B2 (en) * 2004-12-08 2007-05-01 Hoffmann-La Roche Inc. Malonamide derivatives
JP2008536926A (en) 2005-04-20 2008-09-11 メルク エンド カムパニー インコーポレーテッドMerck & Company Incoporated Benzothiophene derivative
TW200900065A (en) 2007-03-07 2009-01-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives
AR059898A1 (en) 2006-03-15 2008-05-07 Janssen Pharmaceutica Nv Derivatives 3-cyano-pyridone and 1,4-disubstituted use as allosteric modulators of mGluR2 receptors
TW200845978A (en) 2007-03-07 2008-12-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives
AU2007229550B2 (en) 2006-03-27 2012-03-08 F. Hoffmann-La Roche Ag Malonamide derivatives as gamma secretase inhibitors
JP5001372B2 (en) 2006-09-20 2012-08-15 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft 4-oxo-2,3,4,5-tetrahydro-benzo [b] [1,4] diazepine derivatives
US8278345B2 (en) 2006-11-09 2012-10-02 Probiodrug Ag Inhibitors of glutaminyl cyclase
AT554085T (en) 2006-11-30 2012-05-15 Probiodrug Ag New inhibitors of glutaminyl
EP2109604A1 (en) * 2007-02-02 2009-10-21 F. Hoffmann-Roche AG 6-oxo-6,7-dihydro-5h-dibenzo[b,d]azepin-7-yl derivatives
EP2142514B1 (en) 2007-04-18 2014-12-24 Probiodrug AG Thiourea derivatives as glutaminyl cyclase inhibitors
US7579464B2 (en) * 2007-05-25 2009-08-25 Hoffmann-La Roche Inc. Process for preparation of enantiomerically pure compounds
JP5433579B2 (en) 2007-09-14 2014-03-05 ジャンセン ファーマシューティカルズ, インコーポレイテッド. 1,3-disubstituted-4-phenyl-1H-pyridin-2-one
PT2200985E (en) 2007-09-14 2011-07-21 Ortho Mcneil Janssen Pharm 1,3-disubstituted 4-(aryl-x-phenyl)-1h-pyridin-2-ones
TWI475995B (en) 2007-09-14 2015-03-11 Janssen Pharmaceuticals Inc 1',3'-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2h, 1'h-[1,4'] bipyridinyl-2'-ones
JP5433582B2 (en) 2007-11-14 2014-03-05 ジャンセン ファーマシューティカルズ, インコーポレイテッド. Imidazo [1,2-a] pyridine derivatives and their use as positive allosteric modulators of the mGluR2 receptor
AU2009289784B2 (en) 2008-09-02 2012-03-22 Addex Pharma S.A. 3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors
JP5656848B2 (en) 2008-10-16 2015-01-21 ジャンセン ファーマシューティカルズ, インコーポレイテッド. Indole and benzomorpholine derivatives as metabotropic glutamate receptor modulators
US8691813B2 (en) 2008-11-28 2014-04-08 Janssen Pharmaceuticals, Inc. Indole and benzoxazine derivatives as modulators of metabotropic glutamate receptors
MY153913A (en) 2009-05-12 2015-04-15 Janssen Pharmaceuticals Inc 7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
DK2430022T3 (en) 2009-05-12 2013-12-02 Janssen Pharmaceuticals Inc 1,2,4-Triazolo [4,3-a] pyridine derivatives and their use in the treatment or prevention of neurological and psychiatric disorders
KR20120035158A (en) 2009-05-12 2012-04-13 아덱스 파마 에스에이 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
KR101755737B1 (en) 2009-09-11 2017-07-07 프로비오드룩 아게 Heterocyclic derivatives as inhibitors of glutaminyl cyclase
US20110190269A1 (en) * 2010-02-01 2011-08-04 Karlheinz Baumann Gamma secretase modulators
JP6026284B2 (en) 2010-03-03 2016-11-16 プロビオドルグ エージー Inhibitors of glutaminyl cyclase
AU2011226074B2 (en) 2010-03-10 2015-01-22 Probiodrug Ag Heterocyclic inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5)
EP2560953B1 (en) 2010-04-21 2016-01-06 Probiodrug AG Inhibitors of glutaminyl cyclase
WO2012062759A1 (en) 2010-11-08 2012-05-18 Janssen Pharmaceuticals, Inc. 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
JP5852664B2 (en) 2010-11-08 2016-02-03 ジヤンセン・フアーマシユーチカルズ・インコーポレーテツド 1,2,4-Triazolo [4,3-a] pyridine derivatives and their use as positive allosteric modulators of the mGluR2 receptor
AU2011328195B2 (en) 2010-11-08 2015-04-02 Janssen Pharmaceuticals, Inc. 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors
WO2012123563A1 (en) 2011-03-16 2012-09-20 Probiodrug Ag Benz imidazole derivatives as inhibitors of glutaminyl cyclase
TWI530489B (en) 2011-03-22 2016-04-21 Squibb Bristol Myers Co Bis (fluoroalkyl) -1,4-benzodiazepine Boom ketone compound
JO3148B1 (en) 2011-07-27 2017-09-20 Lilly Co Eli Notch pathway signaling inhibitor compound
US20150218103A1 (en) 2012-08-25 2015-08-06 The Johns Hopkins University Gapdh cascade inhibitor compounds and methods of use and treatment of stress induced disorders including mental illness
EP2897954B1 (en) 2012-09-21 2016-10-26 Bristol-Myers Squibb Company Fluoroalkyl-1,4-benzodiazepinone compounds
WO2014047393A1 (en) 2012-09-21 2014-03-27 Bristol-Myers Squibb Company N-substituted bis(fluoroalkyl)-1,4-benzodiazepinone compounds as notch inhibitors
JP2015529251A (en) 2012-09-21 2015-10-05 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company Tricyclic heterocyclic compounds as NOTCH inhibitors
US9273075B2 (en) 2012-09-21 2016-03-01 Bristol-Myers Squibb Company Prodrugs of 1,4-benzodiazepinone compounds
EP2897938B1 (en) 2012-09-21 2017-03-15 Bristol-Myers Squibb Company Fluoroalkyl dibenzodiazepinone compounds
JP2015529253A (en) 2012-09-21 2015-10-05 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company Fluoroalkyl and fluorocycloalkyl 1,4-benzodiazepinone compounds as Notch inhibitors
TWI614238B (en) 2012-09-21 2018-02-11 必治妥美雅史谷比公司 Bis(fluoroalkyl)-1,4-benzodiazepinone compounds and prodrugs thereof
US9187434B2 (en) 2012-09-21 2015-11-17 Bristol-Myers Squibb Company Substituted 1,5-benzodiazepinones compounds
JP2015534554A (en) 2012-09-21 2015-12-03 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company Alkyl, fluoroalkyl-1,4-benzodiazepinone compounds
JP2016515625A (en) 2013-04-04 2016-05-30 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company Combination therapy to treat proliferative diseases
TW201835084A (en) 2013-06-04 2018-10-01 比利時商健生藥品公司 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mglur2 receptors
ES2639746T3 (en) 2013-09-06 2017-10-30 Janssen Pharmaceutica, N.V. Compounds of 1,2,4-triazolo [4,3-a] pyridine type and their use as positive allosteric modulators of mglur2 receptors
EP3461819A1 (en) 2017-09-29 2019-04-03 Probiodrug AG Inhibitors of glutaminyl cyclase

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1993003011A1 (en) * 1991-08-08 1993-02-18 Yamanouchi Pharmaceutical Co., Ltd. Urea derivative
EP1222176A1 (en) * 1999-10-08 2002-07-17 Bristol-Myers Squibb Pharma Company AMINO LACTAM SULFONAMIDES AS INHIBITORS OF A$g(b) PROTEIN PRODUCTION
IL151576D0 (en) 2000-04-03 2003-04-10 Bristol Myers Squibb Pharma Co Cyclic lactams as inhibitors of a-beta protein production
CA2404273A1 (en) 2000-04-11 2001-10-18 Bristol-Myers Squibb Pharma Company Substituted lactams as inhibitors of a.beta. protein production
RS20060146A (en) * 2003-09-09 2008-06-05 F.Hoffmann-La Roche Ag., Malonamide derivatives blocking the activity of gama-secretase

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