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ATE443043T1 - Phenylcarboxamide als beta-sekretase-hemmer zur behandlung von alzheimer - Google Patents

Phenylcarboxamide als beta-sekretase-hemmer zur behandlung von alzheimer

Info

Publication number
ATE443043T1
ATE443043T1 AT03768700T AT03768700T ATE443043T1 AT E443043 T1 ATE443043 T1 AT E443043T1 AT 03768700 T AT03768700 T AT 03768700T AT 03768700 T AT03768700 T AT 03768700T AT E443043 T1 ATE443043 T1 AT E443043T1
Authority
AT
Austria
Prior art keywords
beta
treatment
alzheimer
phenylcarboxamide
secretase inhibitor
Prior art date
Application number
AT03768700T
Other languages
English (en)
Inventor
Craig Coburn
Shawn Stachel
Joseph VACCA
Original Assignee
Merck & Co Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Application granted granted Critical
Publication of ATE443043T1 publication Critical patent/ATE443043T1/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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/45—Carboxylic acid nitriles having cyano groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C255/46—Carboxylic acid nitriles having cyano groups bound to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of non-condensed rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/57—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and carboxyl groups, other than cyano groups, bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/08—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • 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
    • C07D211/20—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 singly bound oxygen or sulphur atoms
    • C07D211/22—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 singly bound oxygen or sulphur atoms by oxygen 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
    • C07D211/30—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 doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom
    • C07D211/32—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 doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom by oxygen 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
    • C07D211/36—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
    • 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
    • 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
    • C07D211/68—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 one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72—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 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, directly attached to ring carbon atoms
    • C07D211/74—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated

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  • Engineering & Computer Science (AREA)
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  • General Chemical & Material Sciences (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyrrole Compounds (AREA)
AT03768700T 2002-11-12 2003-11-06 Phenylcarboxamide als beta-sekretase-hemmer zur behandlung von alzheimer ATE443043T1 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US42556002P 2002-11-12 2002-11-12
US42555502P 2002-11-12 2002-11-12
PCT/US2003/035316 WO2004043916A1 (en) 2002-11-12 2003-11-06 Phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer's disease

Publications (1)

Publication Number Publication Date
ATE443043T1 true ATE443043T1 (de) 2009-10-15

Family

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Family Applications (1)

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AT03768700T ATE443043T1 (de) 2002-11-12 2003-11-06 Phenylcarboxamide als beta-sekretase-hemmer zur behandlung von alzheimer

Country Status (8)

Country Link
US (2) US7109217B2 (de)
EP (1) EP1562897B1 (de)
JP (1) JP4494212B2 (de)
AT (1) ATE443043T1 (de)
AU (1) AU2003291308B2 (de)
CA (1) CA2505098A1 (de)
DE (1) DE60329316D1 (de)
WO (1) WO2004043916A1 (de)

Families Citing this family (96)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2507484A1 (en) * 2002-11-27 2004-06-17 Elan Pharmaceuticals, Inc. Substituted ureas and carbamates
CA2529994A1 (en) 2003-06-30 2005-01-20 Merck & Co., Inc. N-alkyl phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer's disease
CN1863797A (zh) * 2003-08-08 2006-11-15 先灵公司 具有苯甲酰胺取代基的环胺bace－1抑制剂
CA2546142A1 (en) 2003-11-24 2005-06-09 Merck & Co., Inc. Benzylether and benzylamino beta-secretase inhibitors for the treatment of alzheimer's disease
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
CN100537523C (zh) 2003-12-19 2009-09-09 默克公司 用于治疗阿尔茨海默病的苯基酰胺和吡啶基酰胺类β-分泌酶抑制剂
US20060014737A1 (en) * 2004-03-09 2006-01-19 Varghese John Methods of treatment of amyloidosis using bi-aryl aspartyl protease inhibitors
JP2007528400A (ja) * 2004-03-09 2007-10-11 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 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
CA2558036A1 (en) * 2004-03-09 2005-09-22 Elan Pharmaceuticals, Inc. Substituted hydroxyethylamine aspartyl protease inhibitors
CN1942457A (zh) * 2004-04-20 2007-04-04 默克公司 作为β－促分泌酶抑制剂用于阿尔茨海默氏病的治疗中的1,3,5－取代的苯基衍生化合物
US7968571B2 (en) * 2004-04-20 2011-06-28 Merck, Sharp & Dohme, Corp. 2,4,6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's Disease
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
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
CA2573138A1 (en) 2004-07-09 2006-01-26 Elan Pharmaceuticals Inc. Oxime derivative substituted hydroxyethylamine aspartyl protease inhibitors
US20060128715A1 (en) * 2004-07-09 2006-06-15 Jennifer Sealy Oxime derivative hydroxyethylamine aspartyl-protease inhibitors
AR049726A1 (es) * 2004-07-22 2006-08-30 Schering Corp Amidas sustituidas inhibidoras de beta secretasa
AR050184A1 (es) * 2004-07-28 2006-10-04 Schering Corp Inhibidores macrociclicos de beta-secretasa
US7388007B2 (en) 2004-08-26 2008-06-17 Bristol-Myers Squibb Company Gamma-lactams as beta-secretase inhibitors
CA2577392A1 (en) * 2004-08-27 2006-03-09 Elan Pharmaceuticals, Inc. Methods of treatment of amyloidosis using ethanol cyclicamine derivatives 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
SV2006002232A (es) * 2004-09-21 2006-05-25 Lilly Co Eli Inhibidores bace ref. x-16940
JP2008520670A (ja) * 2004-11-17 2008-06-19 メルク エンド カムパニー インコーポレーテッド アルツハイマー病の治療のための大環状第三アミンβ−セクレターゼ阻害剤
AU2005309708A1 (en) * 2004-11-23 2006-06-01 Merck & Co., Inc. Macrocyclic aminopyridyl beta-secretase inhibitors for the treatment of Alzheimer's disease
US8394837B2 (en) * 2004-11-23 2013-03-12 Merck, Sharp & Dohme, Corp. 2,3,4,6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease
WO2006088694A1 (en) * 2005-02-14 2006-08-24 Wyeth SUBSTITUTED THIENYL AND FURYL ACYLGUANIDINES AS β-SECRETASE MODULATORS
WO2006099352A1 (en) * 2005-03-10 2006-09-21 Bristol-Myers Squibb Company Novel isophthalates as beta-secretase inhibitors
WO2006103038A1 (en) * 2005-03-30 2006-10-05 Boehringer Ingelheim International Gmbh Substituted 1,2-ethylendiamines, medicaments comprising said compound; their use and their method of manufacture
MX2007012341A (es) 2005-04-08 2008-02-12 Comentis Inc Compuestos que inhiben actividad beta-secretasa y metodos de uso de los mismos.
WO2007019111A2 (en) * 2005-08-03 2007-02-15 Merck & Co., Inc. Cyclic ketal beta-secretase inhibitors for the treatment of alzheimer's disease
US20090170830A1 (en) * 2005-08-03 2009-07-02 Nantermet Philippe G Tricyclic Beta-Secretase Inhibitors for the Treatment of Alzheimer's Disease
US7476764B2 (en) 2005-08-04 2009-01-13 Bristol-Myers Squibb Company Phenylcarboxyamides as beta-secretase inhibitors
WO2007017511A2 (de) * 2005-08-11 2007-02-15 Boehringer Ingelheim International Gmbh Verbindungen zur behandlung der alzheimer erkrankung
JP2009504613A (ja) * 2005-08-11 2009-02-05 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング アルツハイマー病の治療用化合物
JP5030781B2 (ja) 2005-09-05 2012-09-19 良明 木曽 βセクレターゼ阻害剤
WO2007047306A1 (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
WO2007049532A1 (ja) 2005-10-25 2007-05-03 Shionogi & Co., Ltd. アミノジヒドロチアジン誘導体
US8003653B2 (en) * 2005-11-16 2011-08-23 Merck. Sharp & Dohme Corp. Imidazolidinone compounds useful as β-secretase inhibitors for the treatment of Alzheimer's disease
US7872009B2 (en) * 2005-11-21 2011-01-18 Amgen Inc. Beta-Secretase modulators and methods of use
AU2006316620B2 (en) 2005-11-21 2011-03-03 Amgen Inc. Beta-secretase modulators and methods of use
US7838676B2 (en) 2005-11-21 2010-11-23 Amgen Inc. Beta-secretase modulators and methods of use
US7745484B2 (en) * 2005-11-21 2010-06-29 Amgen Inc. Beta-secretase modulators and methods of use
WO2008036316A2 (en) * 2006-09-21 2008-03-27 Merck & Co., Inc. Piperidine and pyrrolidine beta-secretase inhibitors for the treatment of alzheimer's disease
EP2089383B1 (de) 2006-11-09 2015-09-16 Probiodrug AG 3-hydroxy-1,5-dihydropyrrol-2-one derivate als inhibitoren von glutaminylcyclase zur behandlung von geschwüren, krebs und anderen krankheiten
JP5523107B2 (ja) 2006-11-30 2014-06-18 プロビオドルグ エージー グルタミニルシクラーゼの新規阻害剤
EP2117540A1 (de) 2007-03-01 2009-11-18 Probiodrug AG Neue verwendung von glutaminyl-cyclase-hemmern
US9656991B2 (en) 2007-04-18 2017-05-23 Probiodrug Ag Inhibitors of glutaminyl cyclase
WO2008133274A1 (ja) 2007-04-24 2008-11-06 Shionogi & Co., Ltd. 環式基で置換されたアミノジヒドロチアジン誘導体
EP2151435A4 (de) 2007-04-24 2011-09-14 Shionogi & Co Pharmazeutische zusammensetzung zur behandlung von morbus alzheimer
WO2008137954A2 (en) * 2007-05-07 2008-11-13 Environmental Packaging Technologies Limited Universal shipping container
TW200901991A (en) 2007-05-25 2009-01-16 Amgen Inc Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use
WO2008147544A1 (en) 2007-05-25 2008-12-04 Amgen Inc. Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use
WO2009042694A1 (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
US7803809B2 (en) 2008-11-12 2010-09-28 Amgen Inc. Substituted pyrano [2,3-b] pyridinamine compounds as beta-secretase modulators and methods of use
JP4520533B2 (ja) 2008-01-18 2010-08-04 エーザイ・アール・アンド・ディー・マネジメント株式会社 縮合アミノジヒドロチアジン誘導体
WO2009151098A1 (ja) 2008-06-13 2009-12-17 塩野義製薬株式会社 βセクレターゼ阻害作用を有する含硫黄複素環誘導体
US8791135B2 (en) 2008-07-01 2014-07-29 Purdue Research Foundation Nonpeptide HIV-1 protease inhibitors
AU2009277485B2 (en) 2008-07-28 2013-05-02 Eisai R&D Management Co., Ltd. Spiroaminodihydrothiazine derivatives
WO2010030954A1 (en) * 2008-09-11 2010-03-18 Amgen Inc. Spiro-tetracyclic ring compounds as betasecretase modulators and methods of use
US20110207723A1 (en) 2008-09-30 2011-08-25 Eisai R&D Management Co., Ltd. Novel fused aminodihydrothiazine derivative
EP2349308A4 (de) * 2008-10-10 2012-09-12 Purdue Research Foundation Verbindungen zur behandlung von morbus alzheimer
JPWO2010047372A1 (ja) 2008-10-22 2012-03-22 塩野義製薬株式会社 Ｂａｃｅ１阻害活性を有する２−アミノピリミジン−４−オンおよび２−アミノピリジン誘導体
EP2376083A4 (de) * 2008-11-20 2012-06-20 Purdue Research Foundation Chinazolin-inhibitoren von bace 1 und anwendungsverfahren
US8859590B2 (en) 2008-12-05 2014-10-14 Purdue Research Foundation Inhibitors of BACE1 and methods for treating Alzheimer's disease
CA2756145A1 (en) * 2009-03-25 2010-09-30 Purdue Research Foundation Pyrrolidine compounds which inhibit beta-secretase activity and methods of use thereof
JPWO2010113848A1 (ja) 2009-03-31 2012-10-11 塩野義製薬株式会社 Ｂａｃｅ１阻害作用を有するイソチオウレア誘導体またはイソウレア誘導体
GB0912777D0 (en) 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydropyrimidone derivatives
GB0912778D0 (en) 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydro-oxazine derivatives
AU2010294214B2 (en) 2009-09-11 2015-05-07 Vivoryon Therapeutics N.V. Heterocylcic derivatives as inhibitors of glutaminyl cyclase
EP2486006A4 (de) * 2009-10-05 2013-05-01 Comentis Inc Sulfonamid-pyrrolidin-verbindungen zur hemmung der beta-sekretase-aktivität und verwendungsverfahren dafür
EP2504315A1 (de) 2009-11-23 2012-10-03 Amgen Inc. Aminoheteroarylverbindungen als beta-sekretase-modulatoren und verwendungsverfahren dafür
EP2504330A1 (de) 2009-11-23 2012-10-03 Amgen Inc. Aminoheteroarylverbindungen als beta-sekretase-modulatoren und verwendungsverfahren dafür
US7964594B1 (en) * 2009-12-10 2011-06-21 Hoffmann-La Roche Inc. Amino oxazine derivatives
UA103272C2 (uk) * 2009-12-11 2013-09-25 Ф. Хоффманн-Ля Рош Аг 2-аміно-5,5-дифтор-5,6-дигідро-4h-оксазини як інгібітори bace1 і/або bace2
US8999980B2 (en) 2009-12-11 2015-04-07 Shionogi & Co., Ltd. Oxazine derivatives
CA2788363A1 (en) 2010-01-19 2011-07-28 Amgen Inc. Amino heteroaryl compounds as beta-secretase modulators and methods of use
JP6026284B2 (ja) 2010-03-03 2016-11-16 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤
KR101790806B1 (ko) 2010-03-10 2017-11-20 프로비오드룩 아게 글루타미닐 사이클라제(ｑｃ, ｅｃ 2.3.2.5)의 헤테로사이클릭 억제제
JP2013522305A (ja) 2010-03-15 2013-06-13 アムジエン・インコーポレーテツド β−セクレターゼ調節剤としてのスピロ−四環式環化合物
JP5584352B2 (ja) 2010-03-15 2014-09-03 アムジエン・インコーポレーテツド β−セクレターゼ調節剤としてのアミノ−ジヒドロオキサジン系およびアミノ−ジヒドロチアジン系スピロ化合物ならびにそれらの医学的用途
WO2011130383A1 (en) * 2010-04-14 2011-10-20 Comentis, Inc. Compounds containing fused rings which inhibit beta-secretase activity and methods of use thereof
WO2011131748A2 (en) 2010-04-21 2011-10-27 Probiodrug Ag Novel inhibitors
US9018219B2 (en) 2010-10-29 2015-04-28 Shionogi & Co., Ltd. Fused aminodihydropyrimidine derivative
CA2816285A1 (en) 2010-10-29 2012-05-03 Shionogi & Co., Ltd. Naphthyridine derivative
GB201100181D0 (en) 2011-01-06 2011-02-23 Eisai Ltd Fused aminodihydrothiazine derivatives
JP5993875B2 (ja) 2011-01-21 2016-09-14 エーザイ・アール・アンド・ディー・マネジメント株式会社 縮合アミノジヒドロチアジン誘導体の合成に有用な方法および化合物
GB201101140D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
GB201101139D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
EP2673279A1 (de) 2011-02-07 2013-12-18 Amgen Inc. 5-amino-oxazepin- und 5-amino-thiazepanverbindungen als beta-sekretase-antagonisten und verwendungsverfahren
DK2686313T3 (en) 2011-03-16 2016-05-02 Probiodrug Ag Benzimidazole derivatives as inhibitors of glutaminyl cyclase
US8883779B2 (en) 2011-04-26 2014-11-11 Shinogi & Co., Ltd. Oxazine derivatives and a pharmaceutical composition for inhibiting BACE1 containing them
EP2758406A1 (de) 2011-09-21 2014-07-30 Amgen Inc. Amino-oxazine und amino-dihydrothiazinverbindungen als beta-sekretase-modulatoren und verwendungsverfahren dafür
EP2912035A4 (de) 2012-10-24 2016-06-15 Shionogi & Co Dihydrooxazin- oder oxazepinderivate mit bace1-hemmender wirkung
US9725469B2 (en) 2012-11-15 2017-08-08 Amgen, Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
DK3461819T3 (da) 2017-09-29 2020-08-10 Probiodrug Ag Inhibitorer af glutaminylcyklase

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IS2334B (is) * 1992-09-08 2008-02-15 Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) Aspartyl próteasi hemjari af nýjum flokki súlfonamíða
US5783701A (en) * 1992-09-08 1998-07-21 Vertex Pharmaceuticals, Incorporated Sulfonamide inhibitors of aspartyl protease
AU691201B2 (en) * 1993-11-01 1998-05-14 Japat Ltd. Endothelin receptor antagonists
IL108583A (en) * 1994-02-07 1997-06-10 Yissum Res Dev Co Galactomannan emulsions and comestible products containing the same
US5831117A (en) 1995-01-20 1998-11-03 G. D. Searle & Co. Method of preparing retroviral protease inhibitor intermediates
DE19650975A1 (de) 1996-12-09 1998-06-10 Basf Ag Neue heterocyclisch substituierte Benzamide und deren Anwendung
HUP0000475A3 (en) * 1996-12-11 2002-11-28 Basf Ag Ketobenzamides as calpain inhibitors
DE19818614A1 (de) 1998-04-20 1999-10-21 Basf Ag Neue substituierte Amide, deren Herstellung und Anwendung
IL138999A0 (en) 1998-04-20 2001-11-25 Basf Ag Novel heterocyclically substituted amides with cysteine protease-inhibiting effect
SK13932000A3 (sk) * 1998-04-20 2001-05-10 Basf Aktiengesellschaft Heterocyklicky substituované amidy, ich príprava a použitie
AU3927699A (en) * 1998-04-20 1999-11-08 Basf Aktiengesellschaft New substituted amides, their production and their use
DE19817461A1 (de) 1998-04-20 1999-10-21 Basf Ag Neue substituierte Benzamide, deren Herstellung und Anwendung
US5986102A (en) * 1998-04-29 1999-11-16 Pharmacopeia, Inc. Hydroxypropylamide peptidomimetics as inhibitors of aspartyl proteases
US6482832B1 (en) * 1998-05-25 2002-11-19 Abbott Laboratories Heterocyclically substituted amides, their production and their use
US6117639A (en) * 1998-08-31 2000-09-12 Vertex Pharmaceuticals Incorporated Fusion proteins, DNA molecules, vectors, and host cells useful for measuring protease activity
GB9925136D0 (en) * 1999-10-22 1999-12-22 Smithkline Beecham Plc Novel treatment
US6468457B2 (en) 1999-12-15 2002-10-22 Lear Corporation Method of manufacturing a vehicle cup holder arm assembly
EP1122736B1 (de) * 2000-01-31 2009-10-28 STMicroelectronics S.r.l. Erzeugung eines Addressenübergangssignals (ATD) für eine synchrone Speicheranordnung
EP1265849B1 (de) 2000-03-23 2006-10-25 Elan Pharmaceuticals, Inc. Verbindungen und verfahren zur behandlung der alzheimerschen krankheit
JP2002037731A (ja) * 2000-05-19 2002-02-06 Takeda Chem Ind Ltd βセクレターゼ阻害剤
ATE302751T1 (de) 2000-06-30 2005-09-15 Elan Pharm Inc 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
IL156268A0 (en) * 2000-12-13 2004-01-04 Wyeth Corp Heterocyclic sulfonamide inhibitors of beta amyloid production
US7247704B2 (en) * 2000-12-18 2007-07-24 Arriva Pharmaceuticals, Inc. Multifunctional protease inhibitors and their use in treatment of disease
JP2004532826A (ja) * 2001-03-19 2004-10-28 スローン−ケッタリング インスティトゥート フォー カンサー リサーチ （ｓ，ｒ，ｒ）−（−）−アクチノニンおよびそのアナログの不斉合成、ならびにそれらの使用
FR2824825B1 (fr) * 2001-05-15 2005-05-06 Servier Lab Nouveaux derives d'alpha-amino-acides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US6562783B2 (en) * 2001-05-30 2003-05-13 Neurologic, Inc. Phosphinylmethyl and phosphorylmethyl succinic and glutauric acid analogs as β-secretase inhibitors
EP1404664A1 (de) * 2001-07-10 2004-04-07 Elan Pharmaceuticals, Inc. Aminodiole für die behandlung von alzheimer
RS50504A (en) * 2001-11-08 2007-04-10 Elan Pharmaceuticals Inc., N,n'-substituted-1,3-diamino-2- hydroxypropane derivatives
CA2477607A1 (en) * 2002-02-27 2003-09-04 Pharmacia & Upjohn Company Substituted hydroxyethylamines
CA2498269A1 (en) * 2002-09-10 2004-03-25 Pharmacia & Upjohn Company Llc Substituted aminoethers for the treatment of alzheimer's disease
JP2005051967A (ja) * 2003-07-31 2005-02-24 Yuasa Corp 予備電源システム及び運転方法

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