KR100819679B1 - 베타-아밀로이드 펩티드 방출 또는 합성을 억제하는 락탐화합물 - Google Patents

베타-아밀로이드 펩티드 방출 또는 합성을 억제하는 락탐화합물 Download PDF

Info

Publication number
KR100819679B1
KR100819679B1 KR1020037006721A KR20037006721A KR100819679B1 KR 100819679 B1 KR100819679 B1 KR 100819679B1 KR 1020037006721 A KR1020037006721 A KR 1020037006721A KR 20037006721 A KR20037006721 A KR 20037006721A KR 100819679 B1 KR100819679 B1 KR 100819679B1
Authority
KR
South Korea
Prior art keywords
methyl
amino
tetrahydro
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
KR1020037006721A
Other languages
English (en)
Korean (ko)
Other versions
KR20030051846A (ko
Inventor
제임스 에드문드 아우디아
바기즈 존
리 에이치. 라티머
스테이시 레이 맥다니엘
제프리 스코트 니센
유진 디. 토르세트
제이 에스. 텅
Original Assignee
일라이 릴리 앤드 캄파니
엘란 파마슈티칼스, 인크.
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 일라이 릴리 앤드 캄파니, 엘란 파마슈티칼스, 인크. filed Critical 일라이 릴리 앤드 캄파니
Publication of KR20030051846A publication Critical patent/KR20030051846A/ko
Application granted granted Critical
Publication of KR100819679B1 publication Critical patent/KR100819679B1/ko
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/16—Benzazepines; Hydrogenated benzazepines
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal 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)
  • Peptides Or Proteins (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Hydrogenated Pyridines (AREA)
KR1020037006721A 2000-11-17 2001-11-05 베타-아밀로이드 펩티드 방출 또는 합성을 억제하는 락탐화합물 Expired - Fee Related KR100819679B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US24955200P 2000-11-17 2000-11-17
US60/249,552 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 (2)

Publication Number Publication Date
KR20030051846A KR20030051846A (ko) 2003-06-25
KR100819679B1 true KR100819679B1 (ko) 2008-04-04

Family

ID=22943982

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020037006721A Expired - Fee Related KR100819679B1 (ko) 2000-11-17 2001-11-05 베타-아밀로이드 펩티드 방출 또는 합성을 억제하는 락탐화합물

Country Status (33)

Country Link
US (1) US20050261495A1 (enExample)
EP (1) EP1341531B1 (enExample)
JP (1) JP4116437B2 (enExample)
KR (1) KR100819679B1 (enExample)
CN (1) CN1486184A (enExample)
AR (1) AR035927A1 (enExample)
AU (2) AU2002243192B2 (enExample)
BR (1) BR0115427A (enExample)
CA (1) CA2427227C (enExample)
CY (1) CY1106366T1 (enExample)
CZ (1) CZ20031351A3 (enExample)
DE (1) DE60126132T2 (enExample)
DK (1) DK1341531T3 (enExample)
DZ (1) DZ3453A1 (enExample)
EA (1) EA005954B1 (enExample)
EC (1) ECSP034600A (enExample)
ES (1) ES2278804T3 (enExample)
HR (1) HRP20030383B1 (enExample)
HU (1) HU228117B1 (enExample)
IL (2) IL155960A0 (enExample)
MX (1) MXPA03004292A (enExample)
MY (1) MY134559A (enExample)
NO (1) NO324324B1 (enExample)
NZ (1) NZ525854A (enExample)
PE (1) PE20020802A1 (enExample)
PL (1) PL212199B1 (enExample)
PT (1) PT1341531E (enExample)
SI (1) SI1341531T1 (enExample)
SK (1) SK288065B6 (enExample)
TW (1) TWI305204B (enExample)
UA (1) UA74849C2 (enExample)
WO (1) WO2002047671A2 (enExample)
ZA (1) ZA200303789B (enExample)

Families Citing this family (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA74849C2 (en) * 2000-11-17 2006-02-15 Lilly Co Eli Lactam
US7468365B2 (en) 2000-11-17 2008-12-23 Eli Lilly And Company Lactam compound
EP1867636B1 (en) 2005-04-08 2013-06-05 Daiichi Sankyo Company, Limited Pyridylmethylsulfone derivative
WO2006123182A2 (en) 2005-05-17 2006-11-23 Merck Sharp & Dohme Limited Cyclohexyl sulphones for treatment of cancer
JP5198877B2 (ja) * 2006-01-31 2013-05-15 株式会社エーピーアイ コーポレーション ベンゾアゼピノン類の製造方法
CA2676715A1 (en) 2007-02-12 2008-08-21 Merck & Co., Inc. Piperazine derivatives for treatment of ad and related conditions
CL2008002060A1 (es) * 2007-07-16 2008-11-21 Wyeth Corp Compuestos derivados de sulfonamida, inhibidores de la produccion de beta amiloide; metodo de preparacion; composicion farmaceutica; kit farmaceutico; y uso en el tratamiento de enfermedades tales como alzheimer, angiopatia amiloide, sindrome de down, entre otras.
CA2694209C (en) 2007-08-14 2013-09-17 Eli Lilly And Company Azepine derivatives as gamma-secretase inhibitors
TW200920362A (en) 2007-09-11 2009-05-16 Daiichi Sankyo Co Ltd Alkylsulfone derivatives
ES2413504T3 (es) 2007-12-21 2013-07-16 Ligand Pharmaceuticals Inc. Moduladores selectivos del receptor de andrógeno (SARM) y usos de los mismos
EP2291181B9 (en) 2008-04-18 2013-09-11 University College Dublin National University Of Ireland, Dublin Captodiamine for the treatment of depression symptoms
WO2010114780A1 (en) 2009-04-01 2010-10-07 Merck Sharp & Dohme Corp. Inhibitors of akt activity
MY174452A (en) 2009-10-14 2020-04-19 Schering 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
US8518907B2 (en) 2010-08-02 2013-08-27 Merck Sharp & Dohme Corp. RNA interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (CTNNB1) gene expression using short interfering nucleic acid (siNA)
EP3587574B1 (en) 2010-08-17 2022-03-16 Sirna Therapeutics, Inc. Rna interference mediated inhibition of hepatitis b virus (hbv) gene expression using short interfering nucleic acid (sina)
US8946216B2 (en) 2010-09-01 2015-02-03 Merck Sharp & Dohme Corp. 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
US9260471B2 (en) 2010-10-29 2016-02-16 Sirna Therapeutics, Inc. 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
US9023865B2 (en) 2011-10-27 2015-05-05 Merck Sharp & Dohme Corp. 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
EP3919620A1 (en) 2012-05-02 2021-12-08 Sirna Therapeutics, Inc. Short interfering nucleic acid (sina) compositions
EP3970725B1 (en) 2012-09-07 2025-08-20 Massachusetts Eye & Ear Infirmary A gamma secretase inhibitor for treating hearing loss
JP6486272B2 (ja) 2012-09-07 2019-03-20 マサチューセッツ・アイ・アンド・イア・インファーマリー 有毛細胞および／または支持細胞再生のための方法および組成物
JP6280554B2 (ja) 2012-09-28 2018-02-14 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． Ｅｒｋ阻害剤である新規化合物
DK2925888T3 (en) 2012-11-28 2017-12-18 Merck Sharp & Dohme COMPOSITIONS AND METHODS OF CANCER TREATMENT
AR094116A1 (es) 2012-12-20 2015-07-08 Merck Sharp & Dohme Imidazopiridinas sustituidas como inhibidores de hdm2
WO2014120748A1 (en) 2013-01-30 2014-08-07 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as hdm2 inhibitors
US20160067306A1 (en) 2013-04-19 2016-03-10 National University Corporation Hokkaido University Treatment agent for cognitive impairment induced by amyloid beta-protein, therapeutic agent for alzheimer's disease, and treatment method and pathological analysis method related to these
US20160194368A1 (en) 2013-09-03 2016-07-07 Moderna Therapeutics, Inc. Circular polynucleotides
EP3613418A1 (en) 2014-01-17 2020-02-26 Ligand Pharmaceuticals, Inc. 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
EP3458076A4 (en) 2016-05-16 2020-01-22 The General Hospital Corporation HUMAN RESPIRATORY STEM CELLS IN BREEDING LUNG EPITHEL
EP3525785B1 (en) 2016-10-12 2025-08-27 Merck Sharp & Dohme LLC Kdm5 inhibitors
US10947234B2 (en) 2017-11-08 2021-03-16 Merck Sharp & Dohme Corp. PRMT5 inhibitors
EP3706747B1 (en) 2017-11-08 2025-09-03 Merck Sharp & Dohme LLC Prmt5 inhibitors
US11590152B2 (en) 2018-01-26 2023-02-28 Massachusetts Eye And Ear Infirmary Treatment of hearing loss
WO2020033284A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
US11993602B2 (en) 2018-08-07 2024-05-28 Merck Sharp & Dohme Llc PRMT5 inhibitors
EP3833355A4 (en) 2018-08-07 2022-05-11 Merck Sharp & Dohme Corp. PRMT5 INHIBITORS
BR112021020864A2 (pt) 2019-04-19 2021-12-14 Ligand Pharm Inc Formas cristalinas e métodos de produção de formas cristalinas de um composto
US20230108114A1 (en) 2019-12-17 2023-04-06 Merck Sharp & Dohme Llc Prmt5 inhibitors
AU2020408148B2 (en) 2019-12-17 2025-04-24 Merck Sharp & Dohme Llc PRMT5 inhibitors
WO2021126729A1 (en) 2019-12-17 2021-06-24 Merck Sharp & Dohme Corp. Prmt5 inhibitors
CN120225528A (zh) 2022-09-02 2025-06-27 默沙东有限责任公司 依喜替康衍生的拓扑异构酶-1抑制剂药物组合物及其用途
CR20250146A (es) 2022-10-25 2025-05-26 Merck Sharp & Dohme Llc Enlazadores-cargas útiles de adc derivados de exatecán, composiciones farmacéuticas, y usos de los mismos
CN120359051A (zh) 2022-12-14 2025-07-22 默沙东有限责任公司 奥瑞他汀接头-载荷、药物组合物及其用途

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998028268A2 (en) * 1996-12-23 1998-07-02 Elan Pharmaceuticals, Inc. CYCLOALKYL, LACTAM, LACTONE AND RELATED COMPOUNDS AS β-AMYLOID PEPTIDE RELEASE INHIBITORS

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999067219A1 (en) * 1998-06-22 1999-12-29 Elan Pharmaceuticals, Inc. Compounds for inhibiting beta-amyloid peptide release and/or its synthesis
WO2001034571A1 (en) * 1999-11-09 2001-05-17 Eli Lilly And Company β-AMINOACID COMPOUNDS USEFUL FOR INHIBITING β-AMYLOID PEPTIDE RELEASE AND/OR ITS SYNTHESIS
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
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

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998028268A2 (en) * 1996-12-23 1998-07-02 Elan Pharmaceuticals, Inc. CYCLOALKYL, LACTAM, LACTONE AND RELATED COMPOUNDS AS β-AMYLOID PEPTIDE RELEASE INHIBITORS

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
WO 98/28268 A1.*

Also Published As

Publication number Publication date
IL155960A (en) 2009-06-15
DE60126132D1 (de) 2007-03-08
EP1341531A2 (en) 2003-09-10
MXPA03004292A (es) 2004-02-12
NO324324B1 (no) 2007-09-24
SI1341531T1 (sl) 2007-06-30
EA005954B1 (ru) 2005-08-25
NZ525854A (en) 2004-06-25
SK288065B6 (sk) 2013-04-03
CN1486184A (zh) 2004-03-31
AU2002243192B2 (en) 2006-07-20
NO20032236L (no) 2003-07-10
US20050261495A1 (en) 2005-11-24
KR20030051846A (ko) 2003-06-25
MY134559A (en) 2007-12-31
PE20020802A1 (es) 2002-09-10
CA2427227A1 (en) 2002-06-20
CY1106366T1 (el) 2011-10-12
PL362688A1 (en) 2004-11-02
NO20032236D0 (no) 2003-05-16
ES2278804T3 (es) 2007-08-16
DE60126132T2 (de) 2007-10-18
HRP20030383B1 (hr) 2007-12-31
ECSP034600A (es) 2003-06-25
DZ3453A1 (fr) 2002-06-20
PL212199B1 (pl) 2012-08-31
AR035927A1 (es) 2004-07-28
JP2004517090A (ja) 2004-06-10
CZ20031351A3 (cs) 2003-11-12
PT1341531E (pt) 2007-04-30
UA74849C2 (en) 2006-02-15
TWI305204B (en) 2009-01-11
IL155960A0 (en) 2003-12-23
JP4116437B2 (ja) 2008-07-09
WO2002047671A2 (en) 2002-06-20
AU4319202A (en) 2002-06-24
HRP20030383A2 (en) 2005-10-31
HK1059731A1 (en) 2004-07-16
DK1341531T3 (da) 2007-05-14
ZA200303789B (en) 2004-08-16
EA200300580A1 (ru) 2003-10-30
WO2002047671A3 (en) 2003-03-06
HU228117B1 (en) 2012-11-28
HUP0301842A2 (hu) 2003-09-29
HUP0301842A3 (en) 2010-03-29
SK5592003A3 (en) 2003-12-02
BR0115427A (pt) 2003-10-07
CA2427227C (en) 2010-08-17
EP1341531B1 (en) 2007-01-17

Similar Documents

Publication Publication Date Title
KR100819679B1 (ko) 베타-아밀로이드 펩티드 방출 또는 합성을 억제하는 락탐화합물
AU2002243192A1 (en) Lactam compound to inhibit beta-amyloid peptide release or synthesis
KR20030045194A (ko) 락탐 화합물
US7468365B2 (en) Lactam compound
AU2002224321A1 (en) Lactam compound
JP2004521084A5 (enExample)
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
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

R18-X000 Changes to party contact information recorded

St.27 status event code: A-3-3-R10-R18-oth-X000

A201 Request for examination
E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

St.27 status event code: A-1-2-D10-D22-exm-PE0701

GRNT Written decision to grant
PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 4

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 5

R18-X000 Changes to party contact information recorded

St.27 status event code: A-5-5-R10-R18-oth-X000

FPAY Annual fee payment

Payment date: 20130227

Year of fee payment: 6

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 6

R18-X000 Changes to party contact information recorded

St.27 status event code: A-5-5-R10-R18-oth-X000

PN2301 Change of applicant

St.27 status event code: A-5-5-R10-R13-asn-PN2301

St.27 status event code: A-5-5-R10-R11-asn-PN2301

FPAY Annual fee payment

Payment date: 20140227

Year of fee payment: 7

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 7

LAPS Lapse due to unpaid annual fee
PC1903 Unpaid annual fee

St.27 status event code: A-4-4-U10-U13-oth-PC1903

Not in force date: 20150329

Payment event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE

PC1903 Unpaid annual fee

St.27 status event code: N-4-6-H10-H13-oth-PC1903

Ip right cessation event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE

Not in force date: 20150329