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

Cyclische amine mit benzamidsubstituent als bace- 1-inhibitoren

Info

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

Links

Classifications

    • 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
    • C07D207/09Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • 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 and 4
    • C07D243/08Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D205/00Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04Heterocyclic 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
    • 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
    • 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
    • C07D207/10Heterocyclic 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
    • C07D207/12Oxygen or sulfur 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
    • C07D207/18Heterocyclic 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
    • C07D207/22Heterocyclic 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
    • C07D207/24Oxygen or sulfur atoms
    • C07D207/262-Pyrrolidones
    • CCHEMISTRY; METALLURGY
    • 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
    • C07D209/52Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/08Heterocyclic 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
    • C07D211/18Heterocyclic 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
    • C07D211/26Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/08Heterocyclic 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
    • C07D211/18Heterocyclic 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
    • C07D211/34Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/36Heterocyclic 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
    • C07D211/40Oxygen atoms
    • C07D211/44Oxygen atoms attached in position 4
    • C07D211/46Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/12Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring
    • C07D217/18Aralkyl radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04Heterocyclic 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
    • C07D233/28Heterocyclic 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
    • C07D233/30Oxygen or sulfur atoms
    • C07D233/32One oxygen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/06Heterocyclic 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
    • C07D241/08Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • 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
    • CCHEMISTRY; METALLURGY
    • 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
    • C07D401/10Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • 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
    • CCHEMISTRY; METALLURGY
    • 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • 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
    • C07D403/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • 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
    • C07D409/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • 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
    • C07D409/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/06Heterocyclic 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Indole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
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

Family

ID=34193197

Family Applications (1)

Application Number Title Priority Date Filing Date
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 (72)

* 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
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
US7592348B2 (en) 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
US20060014737A1 (en) * 2004-03-09 2006-01-19 Varghese John Methods of treatment of amyloidosis using bi-aryl aspartyl protease inhibitors
CA2558034A1 (en) * 2004-03-09 2005-09-22 Elan Pharmaceuticals, Inc. Substituted hydroxyethylamine aspartyl protease inhibitors
WO2005087752A2 (en) * 2004-03-09 2005-09-22 Elan Pharmaceuticals, Inc. Substituted hydroxyethylamine aspartyl protease inhibitors
US7585885B2 (en) 2004-04-22 2009-09-08 Eli Lilly And Company Pyrrolidine derivatives useful as BACE inhibitors
EP1740573A1 (de) 2004-04-22 2007-01-10 Eli Lilly And Company Amide als bace-inhibitoren
JP2008502684A (ja) 2004-06-15 2008-01-31 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ベータ−セクレターゼ阻害剤として有用なピロリジン−3−イル化合物
US7385085B2 (en) 2004-07-09 2008-06-10 Elan Pharmaceuticals, Inc. Oxime derivative substituted hydroxyethylamine aspartyl protease inhibitors
AU2005265354A1 (en) * 2004-07-09 2006-01-26 Elan Pharmaceuticals, Inc. Oxime derivative hydroxyethylamine aspartyl-protease inhibitors
CA2576782A1 (en) * 2004-08-27 2006-03-09 Elan Pharmaceuticals, Inc. Methods of treatment of amyloidosis using substituted ethanolcyclicamine 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
SV2006002232A (es) 2004-09-21 2006-05-25 Lilly Co Eli Inhibidores bace ref. x-16940
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
JP2008535863A (ja) 2005-04-08 2008-09-04 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化合物およびその使用方法
ATE482214T1 (de) 2005-06-14 2010-10-15 Schering Corp Aspartylproteasehemmer
SG162790A1 (en) 2005-06-14 2010-07-29 Schering Corp Aspartyl protease inhibitors
JP2009511589A (ja) * 2005-10-12 2009-03-19 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 アリール−シクロプロピル誘導体のアスパルチルプロテアーゼ阻害剤を使用してアミロイドーシスを治療する方法
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
US8168641B2 (en) 2006-06-12 2012-05-01 Schering Corporation Aspartyl protease inhibitors
MX2009006228A (es) 2006-12-12 2009-06-22 Schering Corp Inhibidores de aspartil proteasa.
US7902218B2 (en) 2006-12-12 2011-03-08 Bristol-Myers Squibb Company Substituted tetrahydroisoquinolines as β-secretase inhibitors
CN101848897A (zh) 2007-09-06 2010-09-29 先灵公司 γ分泌酶调节剂
CA2699787A1 (en) * 2007-09-24 2009-04-02 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
CA2708300A1 (en) * 2007-12-11 2009-06-18 Schering Corporation Gamma secretase modulators
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
EP2349244A4 (de) * 2008-10-10 2012-09-19 Comentis Inc Bicyclische verbindungen zur hemmung der beta-sekretase-aktivität und verwendungsverfahren dafür
CA2740107A1 (en) * 2008-10-10 2010-04-15 Purdue Research Foundation Compounds for treatment of alzheimer's disease
AU2009314049B2 (en) 2008-11-13 2015-03-05 Merck Sharp & Dohme Corp. Gamma secretase modulators
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
EP2379566A2 (de) 2008-12-22 2011-10-26 Schering Corporation Modulatoren von gamma-sekretase
US20120214802A1 (en) * 2009-03-25 2012-08-23 Bilcer Geoffrey M Pyrrolidine compounds which inhibit beta-secretase activity and methods of use thereof
WO2010147969A2 (en) 2009-06-16 2010-12-23 Schering Corporation Gamma secretase modulators
WO2010147975A1 (en) 2009-06-16 2010-12-23 Schering Corporation Gamma secretase modulators
EP2443118A1 (de) 2009-06-16 2012-04-25 Schering Corporation Gammasekretasemodulatoren
EP2486006A4 (de) * 2009-10-05 2013-05-01 Comentis Inc Sulfonamid-pyrrolidin-verbindungen zur hemmung der beta-sekretase-aktivität und verwendungsverfahren dafür
US8557826B2 (en) 2009-10-08 2013-10-15 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions, and their use
EP2485920B1 (de) 2009-10-08 2016-04-27 Merck Sharp & Dohme Corp. Heterozyklische pentafluorsulfur-imin-verbindungen als bace-1-hemmer sowie zusammensetzungen damit und ihre verwendung
EP2485591B1 (de) 2009-10-08 2016-03-23 Merck Sharp & Dohme Corp. Iminothiadiazindioxinverbindungen als bace-hemmer, zusammensetzungen und ihre verwendung
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
WO2012058031A2 (en) * 2010-10-28 2012-05-03 Qr Pharma, Inc. Novel method for preparation of bisnorcymerine and salts thereof
ES2649964T3 (es) 2011-02-08 2018-01-16 Merck Patent Gmbh Derivados de aminoestatina para el tratamiento de la artrosis
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
AU2012266544A1 (en) * 2011-06-07 2013-11-21 F. Hoffmann-La Roche Ag Halogen-alkyl-1,3 oxazines as BACE1 and/or BACE2 inhibitors
US9181236B2 (en) 2011-08-22 2015-11-10 Merck Sharp & Dohme Corp. 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use
CN104270945B (zh) 2012-03-19 2017-03-29 巴克老龄化研究所 App特异性bace抑制剂(asbi)及其用途
ES2673873T3 (es) 2012-07-24 2018-06-26 Merck Patent Gmbh Derivados de hidroxiestatina para el tratamiento de la artrosis
HK1211589A1 (zh) 2012-08-23 2016-05-27 Alios Biopharma, Inc. 用於治疗副粘病毒病毒性感染的化合物
EP2908824B1 (de) 2012-10-17 2018-05-02 Merck Sharp & Dohme Corp. Tricyclische substituierte thiadiazindioxidverbindungen als bace-hemmer, zusammensetzungen und deren verwendung
WO2014062549A1 (en) 2012-10-17 2014-04-24 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
CA2899938C (en) 2013-02-12 2021-10-19 Buck Institute For Research On Aging Hydantoins that modulate bace-mediated app processing
WO2014127881A1 (de) 2013-02-25 2014-08-28 Merck Patent Gmbh 2-amino-3,4-dihydrc-chinazolin derivate und ihre verwendung als cathepsin d inhibitoren
ES2759060T3 (es) 2013-08-06 2020-05-07 Merck Patent Gmbh Administración intraarticular de pepstatina para la artrosis
HK1225716A1 (zh) 2013-08-21 2017-09-15 Alios Biopharma, Inc. 抗病毒化合物
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
AR107783A1 (es) 2016-03-15 2018-06-06 Lilly Co Eli Terapia de combinación
TW201740954A (zh) * 2016-03-16 2017-12-01 美國禮來大藥廠 組合療法
CN109641052A (zh) 2016-08-18 2019-04-16 伊莱利利公司 BACE-1抑制剂和抗-N3pGlu Aβ抗体的组合疗法
TWI669119B (zh) 2016-10-21 2019-08-21 美國禮來大藥廠 組合療法
JP7368856B2 (ja) 2017-07-25 2023-10-25 トゥルーバインディング,インコーポレイテッド Tim-3とそのリガンドとの相互作用の遮断によるがん治療
WO2019057946A1 (en) 2017-09-25 2019-03-28 F. Hoffmann-La Roche Ag MULTI-CYCLIC AROMATIC COMPOUNDS AS D-FACTOR INHIBITORS
CN120058944A (zh) 2019-01-30 2025-05-30 真和制药有限公司 抗gal3抗体及其用途
JP2023528797A (ja) 2020-05-26 2023-07-06 トゥルーバインディング,インコーポレイテッド ガレクチン-3を遮断することにより炎症性疾患を処置する方法

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
EP1159263A1 (de) 1999-02-26 2001-12-05 Merck & Co., Inc. Sulfonamid-verbindungen und anwendungen davon
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
DE60116313T2 (de) 2000-06-30 2006-08-31 Elan Pharmaceuticals, Inc., San Francisco Verbindungen zur behandlung der alzheimerischen krankheit
WO2002088101A2 (en) 2001-04-27 2002-11-07 Vertex Pharmaceuticals Incorporated Inhibitors of bace
MXPA04001016A (es) 2001-08-03 2004-05-27 Schering Corp Derivados de sulfonamida como inhibidores de la gamma secretasa.
ATE515495T1 (de) 2001-08-03 2011-07-15 Schering Corp Gamma sekretase inhibitoren
HUP0401241A3 (en) 2001-08-21 2008-03-28 Merck Sharp & Dohme Novel cyclohexyl sulphones, process for their preparation and pharmaceutical compositions containing them
TW200302717A (en) 2002-02-06 2003-08-16 Schering Corp Novel gamma secretase inhibitors
ATE443043T1 (de) * 2002-11-12 2009-10-15 Merck & Co Inc Phenylcarboxamide als beta-sekretase-hemmer zur behandlung von alzheimer
US7585885B2 (en) * 2004-04-22 2009-09-08 Eli Lilly And Company Pyrrolidine derivatives useful as BACE inhibitors
EP1740573A1 (de) * 2004-04-22 2007-01-10 Eli Lilly And Company Amide als bace-inhibitoren
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

Also Published As

Publication number Publication date
CA2534950A1 (en) 2005-02-24
US20130004518A1 (en) 2013-01-03
JP2010031045A (ja) 2010-02-12
EP1660443A2 (de) 2006-05-31
MXPA06001559A (es) 2006-05-15
US8278334B2 (en) 2012-10-02
PE20050729A1 (es) 2005-10-01
US9062007B2 (en) 2015-06-23
JP2007501788A (ja) 2007-02-01
AR045218A1 (es) 2005-10-19
WO2005016876A2 (en) 2005-02-24
IL173533A0 (en) 2006-07-05
ES2323068T3 (es) 2009-07-06
CN1863797A (zh) 2006-11-15
ZA200601097B (en) 2007-05-30
US20140128361A1 (en) 2014-05-08
US20050119227A1 (en) 2005-06-02
WO2005016876A3 (en) 2005-09-22
TW200519084A (en) 2005-06-16
AU2004265298A1 (en) 2005-02-24
JP4448134B2 (ja) 2010-04-07
US20100152138A1 (en) 2010-06-17
US8623867B2 (en) 2014-01-07
EP1660443B1 (de) 2009-03-04
DE602004019793D1 (de) 2009-04-16
KR20060058104A (ko) 2006-05-29
US7662816B2 (en) 2010-02-16

Similar Documents

Publication Publication Date Title
ATE424383T1 (de) Cyclische amine mit benzamidsubstituent als bace- 1-inhibitoren
ATE402921T1 (de) Cyclische amine mit einem heterocyclischen substituenten als bace-1-inhibitoren
ATE437876T1 (de) Hexahydropyridoisochinoline als dpp-iv- inhibitoren
ATE452891T1 (de) Pyrimidopyrimidone als kinaseinhibitoren
ATE400271T1 (de) Aryl-pyridinderivate als 11-beta-hsd1-hemmer
ATE404564T1 (de) Diazepinoindolderivate als kinaseinhibitoren
DE602004008303D1 (de) Triazolopyrimidinderivate als inhibitoren von glycogensynthasekinase-3
DE60329282D1 (de) Cyano-pyrrolidine als DPP-IV Inhibitoren
ATE420076T1 (de) Indozolonderivate als 11b-hsd1-inhibitoren
NO20076678L (no) Glutamataggrekanaseinhibitorer
IS8320A (is) N-staðgengnir pýrasólýl-amidýl-bensimidasólýl
ATE540936T1 (de) Substituierte 2-alkyl-chinazolinonderivate als parp-hemmer
ATE520671T1 (de) Pyrimidin-harnstoff-derivate als kinase-hemmer
ATE423121T1 (de) Diphenylimidazopyrimidin- und -imidazolamine als b-sekretase-inhibitoren
ATE401328T1 (de) Verbrückte n-arylsulfonylpiperidine als gamma- sekretaseinhibitoren
DE602004018837D1 (de) Ptidase-iv-inhibitoren
NO20055649D0 (no) Substituert dihydrokinazolin med antiviale egenskaper
DE602004016590D1 (de) Einspritzventil
DE60324208D1 (de) Biarylsulfonamide als mmp-inhibitoren
DE602004019555D1 (de) Heterocyclische 7-aminoalkylidenylchinolone und -naphthyridone
ATE500227T1 (de) Amidderivate
ATE538787T1 (de) Benzimidazol-derivative als raf-kinase-hemmer
DE502004006055D1 (de) 6-arylamino-5-cyano-4-pyrimidinone als pde9a-inhibitoren
ATE402700T1 (de) Glycinamid-derivate als raf-kinase-hemmer
ATE509011T1 (de) Pyrimidinderivate als 11beta-hsd1-inhibitoren

Legal Events

Date Code Title Description
RER Ceased as to paragraph 5 lit. 3 law introducing patent treaties