JP4116437B2 - β−アミロイドペプチドの放出および/または合成を阻害するラクタム化合物 - Google Patents

β−アミロイドペプチドの放出および/または合成を阻害するラクタム化合物 Download PDF

Info

Publication number
JP4116437B2
JP4116437B2 JP2002549245A JP2002549245A JP4116437B2 JP 4116437 B2 JP4116437 B2 JP 4116437B2 JP 2002549245 A JP2002549245 A JP 2002549245A JP 2002549245 A JP2002549245 A JP 2002549245A JP 4116437 B2 JP4116437 B2 JP 4116437B2
Authority
JP
Japan
Prior art keywords
methyl
tetrahydro
amino
reaction
formula
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
JP2002549245A
Other languages
English (en)
Japanese (ja)
Other versions
JP2004517090A (ja
JP2004517090A5 (https=
Inventor
ジェイムズ・エドモンド・オーディア
バーゲス・ジョン
リー・エイチ・ラティマー
ステイシー・リー・マクダニエル
ジェフリー・スコット・ニッセン
ユージーン・ディ・ソーセット
ジェイ・エス・トゥン
Original Assignee
イーライ リリー アンド カンパニー
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
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 イーライ リリー アンド カンパニー, 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 filed Critical イーライ リリー アンド カンパニー
Publication of JP2004517090A publication Critical patent/JP2004517090A/ja
Publication of JP2004517090A5 publication Critical patent/JP2004517090A5/ja
Application granted granted Critical
Publication of JP4116437B2 publication Critical patent/JP4116437B2/ja
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D223/00Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/16Benzazepines; Hydrogenated benzazepines
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Animal Behavior & Ethology (AREA)
  • Molecular Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Hydrogenated Pyridines (AREA)
  • Medicinal Preparation (AREA)
JP2002549245A 2000-11-17 2001-11-05 β−アミロイドペプチドの放出および/または合成を阻害するラクタム化合物 Expired - Fee Related JP4116437B2 (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US24955200P 2000-11-17 2000-11-17
PCT/US2001/027799 WO2002047671A2 (en) 2000-11-17 2001-11-05 Lactam compound to inhibit beta-amyloid peptide release or synthesis

Publications (3)

Publication Number Publication Date
JP2004517090A JP2004517090A (ja) 2004-06-10
JP2004517090A5 JP2004517090A5 (https=) 2006-08-17
JP4116437B2 true JP4116437B2 (ja) 2008-07-09

Family

ID=22943982

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2002549245A Expired - Fee Related JP4116437B2 (ja) 2000-11-17 2001-11-05 β−アミロイドペプチドの放出および/または合成を阻害するラクタム化合物

Country Status (33)

Country Link
US (1) US20050261495A1 (https=)
EP (1) EP1341531B1 (https=)
JP (1) JP4116437B2 (https=)
KR (1) KR100819679B1 (https=)
CN (1) CN1486184A (https=)
AR (1) AR035927A1 (https=)
AU (2) AU4319202A (https=)
BR (1) BR0115427A (https=)
CA (1) CA2427227C (https=)
CY (1) CY1106366T1 (https=)
CZ (1) CZ20031351A3 (https=)
DE (1) DE60126132T2 (https=)
DK (1) DK1341531T3 (https=)
DZ (1) DZ3453A1 (https=)
EA (1) EA005954B1 (https=)
EC (1) ECSP034600A (https=)
ES (1) ES2278804T3 (https=)
HR (1) HRP20030383B1 (https=)
HU (1) HU228117B1 (https=)
IL (2) IL155960A0 (https=)
MX (1) MXPA03004292A (https=)
MY (1) MY134559A (https=)
NO (1) NO324324B1 (https=)
NZ (1) NZ525854A (https=)
PE (1) PE20020802A1 (https=)
PL (1) PL212199B1 (https=)
PT (1) PT1341531E (https=)
SI (1) SI1341531T1 (https=)
SK (1) SK288065B6 (https=)
TW (1) TWI305204B (https=)
UA (1) UA74849C2 (https=)
WO (1) WO2002047671A2 (https=)
ZA (1) ZA200303789B (https=)

Families Citing this family (51)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7468365B2 (en) 2000-11-17 2008-12-23 Eli Lilly And Company Lactam compound
UA74849C2 (en) * 2000-11-17 2006-02-15 Lilly Co Eli Lactam
US8114886B2 (en) 2005-04-08 2012-02-14 Daiichi Sankyo Company, Limited Pyridylmethylsulfone derivative
WO2006123182A2 (en) 2005-05-17 2006-11-23 Merck Sharp & Dohme Limited Cyclohexyl sulphones for treatment of cancer
US8258302B2 (en) 2006-01-31 2012-09-04 Api Corporation Method for producing benzazepinone
CA2676715A1 (en) 2007-02-12 2008-08-21 Merck & Co., Inc. Piperazine derivatives for treatment of ad and related conditions
EP2193117A1 (en) * 2007-07-16 2010-06-09 Wyeth a Corporation of the State of Delaware Inhibitors of beta amyloid production
MX2010001754A (es) 2007-08-14 2010-05-14 Lilly Co Eli Derivados de azepina como inhibidores de gamma secretasa.
TW200920362A (en) 2007-09-11 2009-05-16 Daiichi Sankyo Co Ltd Alkylsulfone derivatives
KR101595238B1 (ko) 2007-12-21 2016-02-18 리간드 파마슈티칼스 인코포레이티드 선택적 안드로겐 수용체 조절제(sarm) 및 이의 용도
WO2009128057A2 (en) 2008-04-18 2009-10-22 UNIVERSITY COLLEGE DUBLIN, NATIONAL UNIVERSITY OF IRELAND, DUBLIN et al Psycho-pharmaceuticals
WO2010114780A1 (en) 2009-04-01 2010-10-07 Merck Sharp & Dohme Corp. Inhibitors of akt activity
US8859776B2 (en) 2009-10-14 2014-10-14 Merck Sharp & Dohme Corp. Substituted piperidines that increase p53 activity and the uses thereof
US8999957B2 (en) 2010-06-24 2015-04-07 Merck Sharp & Dohme Corp. Heterocyclic compounds as ERK inhibitors
CA2805265A1 (en) 2010-08-02 2012-02-09 Merck Sharp & Dohme Corp. Rna interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (ctnnb1) gene expression using short interfering nucleic acid (sina)
WO2012024170A2 (en) 2010-08-17 2012-02-23 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF HEPATITIS B VIRUS (HBV) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
WO2012030685A2 (en) 2010-09-01 2012-03-08 Schering Corporation Indazole derivatives useful as erk inhibitors
US9242981B2 (en) 2010-09-16 2016-01-26 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel ERK inhibitors
WO2012040444A2 (en) * 2010-09-24 2012-03-29 Bristol-Myers Squibb Company Treatment of patients with incipient alzheimer's disease
WO2012058210A1 (en) 2010-10-29 2012-05-03 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACIDS (siNA)
EP2654748B1 (en) 2010-12-21 2016-07-27 Merck Sharp & Dohme Corp. Indazole derivatives useful as erk inhibitors
EP2770987B1 (en) 2011-10-27 2018-04-04 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
CN102690231B (zh) * 2012-04-11 2014-07-09 南京友杰医药科技有限公司 治疗阿尔茨海默病潜在药物司马西特的合成方法
WO2013165816A2 (en) 2012-05-02 2013-11-07 Merck Sharp & Dohme Corp. SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS
CA2884309A1 (en) 2012-09-07 2014-03-13 Massachusetts Eye And Ear Infirmary Methods and compositions for regenerating hair cells and/or supporting cells from differentiated cochlear cells or differentiated utricular cells by modulation of notch and cmyc activity
CA2883896C (en) 2012-09-07 2023-03-07 Massachusetts Eye & Ear Infirmary Treating hearing loss
WO2014052563A2 (en) 2012-09-28 2014-04-03 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
ME02925B (me) 2012-11-28 2018-04-20 Merck Sharp & Dohme Kompozicije i postupci za liječenje kancera
TW201429969A (zh) 2012-12-20 2014-08-01 Merck Sharp & Dohme 作爲hdm2抑制劑之經取代咪唑吡啶
WO2014120748A1 (en) 2013-01-30 2014-08-07 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as hdm2 inhibitors
JP6319912B2 (ja) 2013-04-19 2018-05-09 国立大学法人 岡山大学 アミロイドβ蛋白質により誘発される認知障害の治療剤およびアルツハイマー病治療薬、ならびにこれらに関連する治療方法および病態解析方法
US20160194368A1 (en) 2013-09-03 2016-07-07 Moderna Therapeutics, Inc. Circular polynucleotides
EP3094323A4 (en) 2014-01-17 2017-10-11 Ligand Pharmaceuticals Incorporated Methods and compositions for modulating hormone levels
EP3212773B1 (en) 2014-10-29 2021-09-15 Massachusetts Eye and Ear Infirmary Efficient delivery of therapeutic molecules to cells of the inner ear
JP6840774B2 (ja) 2016-05-16 2021-03-10 ザ ジェネラル ホスピタル コーポレイション 肺上皮エンジニアリングにおけるヒト気道幹細胞
US10975084B2 (en) 2016-10-12 2021-04-13 Merck Sharp & Dohme Corp. KDM5 inhibitors
EP3706747B1 (en) 2017-11-08 2025-09-03 Merck Sharp & Dohme LLC Prmt5 inhibitors
US10947234B2 (en) 2017-11-08 2021-03-16 Merck Sharp & Dohme Corp. PRMT5 inhibitors
WO2019148067A1 (en) 2018-01-26 2019-08-01 Massachusetts Eye And Ear Infirmary Treatment of hearing loss
WO2020033282A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
WO2020033288A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
EP3833669A4 (en) 2018-08-07 2022-05-11 Merck Sharp & Dohme Corp. PRMT5 INHIBITORS
US11981701B2 (en) 2018-08-07 2024-05-14 Merck Sharp & Dohme Llc PRMT5 inhibitors
AU2020257397B2 (en) 2019-04-19 2026-02-26 Ligand Pharmaceuticals Inc. Crystalline forms and methods of producing crystalline forms of a compound
US12595248B2 (en) 2019-12-17 2026-04-07 Merck Sharp & Dohme Llc PRMT5 inhibitors
CN115003303B (zh) 2019-12-17 2024-03-08 默沙东公司 Prmt5抑制剂
EP4076460B1 (en) 2019-12-17 2026-01-21 Merck Sharp & Dohme LLC 1,4-dihydro-2h-spiro[isoquinoline-3,4'-piperidine derivatives as prmt5 inhibitors for the treatment of cancer
JP7589247B2 (ja) 2019-12-17 2024-11-25 メルク・シャープ・アンド・ドーム・エルエルシー Prmt5阻害剤
JP2025511436A (ja) 2022-09-02 2025-04-16 メルク・シャープ・アンド・ドーム・エルエルシー エキサテカン由来トポイソメラーゼ-1阻害薬医薬組成物及びその使用
CN120417935A (zh) 2022-10-25 2025-08-01 默沙东有限责任公司 依喜替康衍生的adc接头-载荷及其药物组合物和用途
US20240207425A1 (en) 2022-12-14 2024-06-27 Merck Sharp & Dohme Llc Auristatin linker-payloads, pharmaceutical compositions, and uses thereof

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA002100B1 (ru) * 1996-12-23 2001-12-24 Элан Фармасьютикалз, Инк. ЦИКЛОАЛКИЛЬНЫЕ СОЕДИНЕНИЯ, ЛАКТАМЫ, ЛАКТОНЫ И РОДСТВЕННЫЕ СОЕДИНЕНИЯ, СОДЕРЖАЩИЕ ИХ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ И СПОСОБЫ ИНГИБИРОВАНИЯ ВЫСВОБОЖДЕНИЯ И/ИЛИ СИНТЕЗА β-АМИЛОИДНОГО ПЕПТИДА С ПОМОЩЬЮ УКАЗАННЫХ СОЕДИНЕНИЙ
WO1999067219A1 (en) * 1998-06-22 1999-12-29 Elan Pharmaceuticals, Inc. Compounds for inhibiting beta-amyloid peptide release and/or its synthesis
JP2003513958A (ja) * 1999-11-09 2003-04-15 イーライ・リリー・アンド・カンパニー β−アミロイドペプチド放出および/またはその合成を阻害するために有用なβ−アミノ酸化合物
UA74849C2 (en) * 2000-11-17 2006-02-15 Lilly Co Eli Lactam
CA2425558C (en) * 2000-11-17 2012-01-03 Eli Lilly And Company Lactam compound
UA77165C2 (en) * 2000-11-17 2006-11-15 Lilly Co Eli (n)-((s)-2-hydroxy-3-methyl-butyryl)-1-(l-alaninyl)-(s)-1-amino-3-methyl-4,5,6,7-tetrahydro-2h-3-benzazepin-2-one dihydrate, processes for manufacturing and pharmaceutical composition

Also Published As

Publication number Publication date
EP1341531A2 (en) 2003-09-10
ES2278804T3 (es) 2007-08-16
DE60126132D1 (de) 2007-03-08
CA2427227C (en) 2010-08-17
AR035927A1 (es) 2004-07-28
HRP20030383B1 (hr) 2007-12-31
AU2002243192B2 (en) 2006-07-20
DE60126132T2 (de) 2007-10-18
ECSP034600A (es) 2003-06-25
EP1341531B1 (en) 2007-01-17
HK1059731A1 (en) 2004-07-16
PL362688A1 (en) 2004-11-02
MXPA03004292A (es) 2004-02-12
WO2002047671A3 (en) 2003-03-06
HU228117B1 (en) 2012-11-28
IL155960A0 (en) 2003-12-23
HRP20030383A2 (en) 2005-10-31
TWI305204B (en) 2009-01-11
KR100819679B1 (ko) 2008-04-04
HUP0301842A2 (hu) 2003-09-29
DZ3453A1 (fr) 2002-06-20
BR0115427A (pt) 2003-10-07
NO20032236L (no) 2003-07-10
EA200300580A1 (ru) 2003-10-30
NO20032236D0 (no) 2003-05-16
ZA200303789B (en) 2004-08-16
CN1486184A (zh) 2004-03-31
CA2427227A1 (en) 2002-06-20
SI1341531T1 (sl) 2007-06-30
SK288065B6 (sk) 2013-04-03
PE20020802A1 (es) 2002-09-10
EA005954B1 (ru) 2005-08-25
IL155960A (en) 2009-06-15
KR20030051846A (ko) 2003-06-25
UA74849C2 (en) 2006-02-15
SK5592003A3 (en) 2003-12-02
AU4319202A (en) 2002-06-24
CY1106366T1 (el) 2011-10-12
MY134559A (en) 2007-12-31
JP2004517090A (ja) 2004-06-10
US20050261495A1 (en) 2005-11-24
PL212199B1 (pl) 2012-08-31
NZ525854A (en) 2004-06-25
WO2002047671A2 (en) 2002-06-20
CZ20031351A3 (cs) 2003-11-12
NO324324B1 (no) 2007-09-24
DK1341531T3 (da) 2007-05-14
HUP0301842A3 (en) 2010-03-29
PT1341531E (pt) 2007-04-30

Similar Documents

Publication Publication Date Title
JP4116437B2 (ja) β−アミロイドペプチドの放出および/または合成を阻害するラクタム化合物
AU2002243192A1 (en) Lactam compound to inhibit beta-amyloid peptide release or synthesis
HUE027482T2 (en) Benzylamine derivatives as inhibitors of plasma kallikrein
JP4116431B2 (ja) ラクタム化合物
US7468365B2 (en) Lactam compound
JP2004521084A5 (https=)
AU2002224321A1 (en) Lactam compound
EP1345955B1 (en) Lactam dipeptide and its use in inhibiting beta-amyloid peptide release
HK1059731B (en) Lactam compound to inhibit beta-amyloid peptide release or synthesis
US20040077627A1 (en) Lactam compound

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20041028

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20041028

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20060629

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20070828

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20071121

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20071129

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20071227

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20080318

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20080417

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20110425

Year of fee payment: 3

R150 Certificate of patent or registration of utility model

Free format text: JAPANESE INTERMEDIATE CODE: R150

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20110425

Year of fee payment: 3

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20110425

Year of fee payment: 3

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20120425

Year of fee payment: 4

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20120425

Year of fee payment: 4

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20130425

Year of fee payment: 5

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20140425

Year of fee payment: 6

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees