ATE424383T1 - Cyclische amine mit benzamidsubstituent als bace- 1-inhibitoren - Google Patents

Cyclische amine mit benzamidsubstituent als bace- 1-inhibitoren

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Publication number
ATE424383T1
ATE424383T1 AT04779938T AT04779938T ATE424383T1 AT E424383 T1 ATE424383 T1 AT E424383T1 AT 04779938 T AT04779938 T AT 04779938T AT 04779938 T AT04779938 T AT 04779938T AT E424383 T1 ATE424383 T1 AT E424383T1
Authority
AT
Austria
Prior art keywords
bace
inhibitors
cyclic amine
benzamide substituent
benzamide
Prior art date
Application number
AT04779938T
Other languages
English (en)
Inventor
Jared Cumming
Ulrich Iserloh
Andrew Stamford
Corey Strickland
Johannes Voigt
Yusheng Wu
Ying Huang
Yan Xia
Samuel Chackalamannil
Tao Guo
Douglas Hobbs
Thuy Le
Jeffrey Lowrie
Kurt Saionz
Suresh Babu
Original Assignee
Schering Corp
Pharmacopeia Drug Discovery
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
Application filed by Schering Corp, Pharmacopeia Drug Discovery filed Critical Schering Corp
Application granted granted Critical
Publication of ATE424383T1 publication Critical patent/ATE424383T1/de

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic 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
    • C07D207/04—Heterocyclic 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
    • C07D207/08—Heterocyclic 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
    • C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/08—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 not condensed with other rings
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic 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
    • C07D207/04—Heterocyclic 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
    • C07D207/08—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic 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
    • C07D207/04—Heterocyclic 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
    • C07D207/10—Heterocyclic 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 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
    • C07D207/12—Oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic 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
    • C07D207/18—Heterocyclic 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 one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic 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 one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/52—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/26—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/34—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 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
    • C07D211/40—Oxygen atoms
    • C07D211/44—Oxygen atoms attached in position 4
    • C07D211/46—Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/12—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring
    • C07D217/18—Aralkyl radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole 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 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
    • C07D233/30—Oxygen or sulfur atoms
    • C07D233/32—One oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/06—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members
    • C07D241/08—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • C07D401/10—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 carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur 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
    • C07D413/02—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
    • C07D413/06—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 only aliphatic carbon atoms
AT04779938T 2003-08-08 2004-08-04 Cyclische amine mit benzamidsubstituent als bace- 1-inhibitoren ATE424383T1 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US49398703P 2003-08-08 2003-08-08

Publications (1)

Publication Number Publication Date
ATE424383T1 true ATE424383T1 (de) 2009-03-15

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AT04779938T ATE424383T1 (de) 2003-08-08 2004-08-04 Cyclische amine mit benzamidsubstituent als bace- 1-inhibitoren

Country Status (17)

Country Link
US (4) US7662816B2 (de)
EP (1) EP1660443B1 (de)
JP (2) JP4448134B2 (de)
KR (1) KR20060058104A (de)
CN (1) CN1863797A (de)
AR (1) AR045218A1 (de)
AT (1) ATE424383T1 (de)
AU (1) AU2004265298A1 (de)
CA (1) CA2534950A1 (de)
DE (1) DE602004019793D1 (de)
ES (1) ES2323068T3 (de)
IL (1) IL173533A0 (de)
MX (1) MXPA06001559A (de)
PE (1) PE20050729A1 (de)
TW (1) TW200519084A (de)
WO (1) WO2005016876A2 (de)
ZA (1) ZA200601097B (de)

Families Citing this family (68)

* 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
US7592348B2 (en) 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7700603B2 (en) 2003-12-15 2010-04-20 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
WO2005087751A2 (en) * 2004-03-09 2005-09-22 Elan Pharmaceuticals, Inc. Substituted hydroxyethylamine aspartyl protease inhibitors
US20060014737A1 (en) * 2004-03-09 2006-01-19 Varghese John Methods of treatment of amyloidosis using bi-aryl aspartyl protease inhibitors
US20050239790A1 (en) * 2004-03-09 2005-10-27 Varghese John Substituted hydroxyethylamine aspartyl protease inhibitors
US7585885B2 (en) 2004-04-22 2009-09-08 Eli Lilly And Company Pyrrolidine derivatives useful as BACE inhibitors
WO2005108358A2 (en) * 2004-04-22 2005-11-17 Eli Lilly And Company Pyrrolidine derivatives useful as bace inhibitors
AU2005257904A1 (en) 2004-06-15 2006-01-05 Merck Sharp & Dohme Corp. Pyrrolidin-3-yl compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's disease
JP2008505930A (ja) 2004-07-09 2008-02-28 エラン ファーマシューティカルズ，インコーポレイテッド オキシム誘導体置換ヒドロキシエチルアミン系のアスパラギン酸プロテアーゼ阻害薬
CA2572775A1 (en) * 2004-07-09 2006-01-26 Elan Pharmaceuticals, Inc. Oxime derivative hydroxyethylamine aspartyl-protease inhibitors
CA2577392A1 (en) * 2004-08-27 2006-03-09 Elan Pharmaceuticals, Inc. Methods of treatment of amyloidosis using ethanol cyclicamine derivatives aspartyl protease inhibitors
EP1789388A2 (de) * 2004-08-27 2007-05-30 Elan Pharmaceuticals, Inc. Verfahren zur behandlung von amyloidose mit substituierten ethanolcyclicamin-aspartylproteasehemmern
TW200624426A (en) * 2004-09-21 2006-07-16 Lilly Co Eli BACE inhibitors
GB0500683D0 (en) 2005-01-13 2005-02-23 Novartis Ag Organic compounds
US7745470B2 (en) 2005-03-10 2010-06-29 Bristol-Myers Squibb Company Isophthalates as beta-secretase inhibitors
AR054617A1 (es) 2005-06-14 2007-07-04 Schering Corp Derivados de pirrol[3, 4 - d]pirimidina como inhibidores de aspartil proteasas y composiciones farmacéuticas que los comprenden
MX2007016175A (es) 2005-06-14 2008-03-07 Schering Corp Inhibidor de aspartil proteasas.
CA2624904A1 (en) * 2005-10-12 2007-04-26 Elan Pharmaceuticals, Inc. Methods of treating amyloidosis using aryl-cyclopropyl derivative aspartyl protease inhibitors
WO2007047305A1 (en) 2005-10-12 2007-04-26 Elan Pharmaceuticals, Inc. Methods of treating amyloidosis using cyclopropyl derivative aspartyl protease inhibitors
JP2009515964A (ja) 2005-11-16 2009-04-16 メルク エンド カムパニー インコーポレーテッド アルツハイマー病を治療するためのβ−セクレターゼ阻害剤として有用なイミダゾリジノン化合物
GB0526614D0 (en) * 2005-12-30 2006-02-08 Novartis Ag Organic compounds
GB0611064D0 (en) * 2006-06-05 2006-07-12 Novartis Ag Organic compounds
EP2032542A2 (de) 2006-06-12 2009-03-11 Schering Corporation Heterozyklische aspartylproteasehemmer
JP2010512389A (ja) 2006-12-12 2010-04-22 シェーリング コーポレイション アスパルチルプロテアーゼ阻害剤
US7902218B2 (en) 2006-12-12 2011-03-08 Bristol-Myers Squibb Company Substituted tetrahydroisoquinolines as β-secretase inhibitors
MX2010002674A (es) 2007-09-06 2010-03-25 Schering Corp Moduladores de gamma secretasa.
US8299267B2 (en) 2007-09-24 2012-10-30 Comentis, Inc. (3-hydroxy-4-amino-butan-2-yl) -3- (2-thiazol-2-yl-pyrrolidine-1-carbonyl) benzamide derivatives and related compounds as beta-secretase inhibitors for treating
WO2009061699A1 (en) 2007-11-05 2009-05-14 Schering Corporation Gamma secretase modulators
MX2010006378A (es) 2007-12-11 2010-09-07 Schering Corp Moduladores de gamma secretasa.
AU2009239536C1 (en) 2008-04-22 2012-12-13 Merck Sharp & Dohme Corp. Phenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use
EP2349308A4 (de) * 2008-10-10 2012-09-12 Purdue Research Foundation Verbindungen zur behandlung von morbus alzheimer
CA2739875A1 (en) * 2008-10-10 2010-04-15 Comentis, Inc. Pyrrolidine compounds which inhibit beta-secretase activity and methods of use thereof
JP5503663B2 (ja) 2008-11-13 2014-05-28 メルク・シャープ・アンド・ドーム・コーポレーション ガンマセクレターゼモジュレータ
AR074702A1 (es) 2008-12-22 2011-02-02 Schering Corp Moduladores de gamma secretasa y composiciones farmaceuticas que los contienen
JP2012513399A (ja) 2008-12-22 2012-06-14 シェーリング コーポレイション γ−セクレターゼ調節剤
JP2012521421A (ja) * 2009-03-25 2012-09-13 コメンティス，インコーポレーテッド β−セクレターゼ活性を阻害するピロリジン化合物及びその使用方法
WO2010147969A2 (en) 2009-06-16 2010-12-23 Schering Corporation Gamma secretase modulators
EP2443119A1 (de) 2009-06-16 2012-04-25 Schering Corporation Gammasekretasemodulatoren
WO2010147973A1 (en) 2009-06-16 2010-12-23 Schering Corporation Gamma secretase modulators
WO2011044057A1 (en) * 2009-10-05 2011-04-14 Comentis, Inc. Sulfonamido pyrrolidine compounds which inhibit beta-secretase activity and methods of use thereof
US8563543B2 (en) 2009-10-08 2013-10-22 Merck Sharp & Dohme Corp. Iminothiadiazine dioxide compounds as bace 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
EP2485590B1 (de) 2009-10-08 2015-01-07 Merck Sharp & Dohme Corp. Heterozyklische pentafluorsulfur-imin-verbindungen als bace-1-hemmer sowie zusammensetzungen damit und ihre verwendung
WO2012058031A2 (en) * 2010-10-28 2012-05-03 Qr Pharma, Inc. Novel method for preparation of bisnorcymerine and salts thereof
KR20140053855A (ko) 2011-02-08 2014-05-08 메르크 파텐트 게엠베하 관절증의 치료를 위한 아미노스타틴 유도체
EP2694489B1 (de) 2011-04-07 2017-09-06 Merck Sharp & Dohme Corp. C5-c6-oxacyclus-fusionierte thiadiazindioxidverbindungen als bace-hemmer sowie zusammensetzungen daraus und ihre verwendung
BR112013031098A2 (pt) * 2011-06-07 2016-12-06 Hoffmann La Roche halogeno-alquil-1,3 oxazinas como inibidores de bace1 e/ou bace2
WO2013028670A1 (en) 2011-08-22 2013-02-28 Merck Sharp & Dohme Corp. 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use
JP6482458B2 (ja) 2012-03-19 2019-03-13 バック・インスティテュート・フォー・リサーチ・オン・エイジング Ａｐｐ特異性のｂａｃｅ（ａｓｂｉ）およびその使用
CN104507957B (zh) 2012-07-24 2018-12-25 默克专利股份有限公司 用于治疗关节病的羟基他汀衍生物
EA201590197A1 (ru) 2012-08-23 2015-07-30 Алиос Биофарма, Инк. Соединения для лечения парамиксовирусных вирусных инфекций
US9416129B2 (en) 2012-10-17 2016-08-16 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use
US9422277B2 (en) 2012-10-17 2016-08-23 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use
KR102051485B1 (ko) 2013-02-12 2019-12-03 버크 인스티튜트 포 리서치 온 에이징 Bace 매개 app 처리과정을 조절하는 히단토인
US9663475B2 (en) 2013-02-25 2017-05-30 Merck Patent Gmbh 2 amino-3,4-dihydrcquinazoline derivatives and the use thereof as cathepsin D inhibitors
WO2015018472A1 (de) 2013-08-06 2015-02-12 Merck Patent Gmbh Intraartikuläre applikation von pepstatin bei arthrose
BR112016003348B1 (pt) * 2013-08-21 2023-03-07 Alios Biopharma, Inc Compostos antivirais ou sais farmaceuticamente aceitáveis dos mesmos, composição farmacêutica e seus usos
US9745324B2 (en) 2013-12-18 2017-08-29 Merck Sharp & Dohme Corp. Iminothiadiazepane dioxide compounds as BACE inhibitors, compositions, and their use
AU2015219902B2 (en) 2014-02-18 2018-11-22 Nissan Chemical Corporation Alkynyl pyridine-substituted amide compound and pesticide
TWI599358B (zh) 2014-09-16 2017-09-21 美國禮來大藥廠 組合療法
TW201740944A (zh) 2016-03-15 2017-12-01 美國禮來大藥廠 組合療法
AR107774A1 (es) * 2016-03-16 2018-05-30 Lilly Co Eli Terapia de combinación, método para el tratamiento de la enfermedad de alzheimer
JP2019530647A (ja) 2016-08-18 2019-10-24 イーライ リリー アンド カンパニー Ｂａｃｅ−１阻害剤と抗ｎ３ｐｇｌｕ ａベータ抗体の併用療法
AR110470A1 (es) 2016-10-21 2019-04-03 Lilly Co Eli Terapia de combinación para tratar la enfermedad de alzheimer
WO2019057946A1 (en) 2017-09-25 2019-03-28 F. Hoffmann-La Roche Ag MULTI-CYCLIC AROMATIC COMPOUNDS AS D-FACTOR INHIBITORS

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW282460B (de) * 1993-12-28 1996-08-01 Yamanouchi Pharma Co Ltd
HRP990246A2 (en) 1998-08-07 2000-06-30 Du Pont Pharm Co Succinoylamino benzodiazepines as inhibitors of a beta protein production
CN1348442A (zh) 1999-02-26 2002-05-08 默克公司 新的磺胺化合物及其应用
DE60116313T2 (de) 2000-06-30 2006-08-31 Elan Pharmaceuticals, Inc., San Francisco Verbindungen zur behandlung der alzheimerischen krankheit
PE20020276A1 (es) 2000-06-30 2002-04-06 Elan Pharm Inc COMPUESTOS DE AMINA SUSTITUIDA COMO INHIBIDORES DE ß-SECRETASA PARA EL TRATAMIENTO DE ALZHEIMER
US6846813B2 (en) 2000-06-30 2005-01-25 Pharmacia & Upjohn Company Compounds to treat alzheimer's disease
EP1389194A2 (de) 2001-04-27 2004-02-18 Vertex Pharmaceuticals Incorporated Bace-inhibitoren
MXPA04001016A (es) 2001-08-03 2004-05-27 Schering Corp Derivados de sulfonamida como inhibidores de la gamma secretasa.
JP4418671B2 (ja) 2001-08-03 2010-02-17 シェーリング コーポレイション 新規γセクレターゼインヒビター
MXPA04001607A (es) 2001-08-21 2004-07-08 Merck Sharp & Dohme Ciclohexilsulfonas novedosas.
TW200302717A (en) 2002-02-06 2003-08-16 Schering Corp Novel gamma secretase inhibitors
WO2004043916A1 (en) * 2002-11-12 2004-05-27 Merck & Co., Inc. Phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer's disease
WO2005108358A2 (en) * 2004-04-22 2005-11-17 Eli Lilly And Company Pyrrolidine derivatives useful as bace inhibitors
US7585885B2 (en) * 2004-04-22 2009-09-08 Eli Lilly And Company Pyrrolidine derivatives useful as BACE inhibitors
US7745470B2 (en) * 2005-03-10 2010-06-29 Bristol-Myers Squibb Company Isophthalates as beta-secretase inhibitors
JP2009515964A (ja) * 2005-11-16 2009-04-16 メルク エンド カムパニー インコーポレーテッド アルツハイマー病を治療するためのβ−セクレターゼ阻害剤として有用なイミダゾリジノン化合物

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