KR100341982B1 - 프롤릴엔도펩티다제억제제 - Google Patents

프롤릴엔도펩티다제억제제 Download PDF

Info

Publication number
KR100341982B1
KR100341982B1 KR1019960702894A KR19960702894A KR100341982B1 KR 100341982 B1 KR100341982 B1 KR 100341982B1 KR 1019960702894 A KR1019960702894 A KR 1019960702894A KR 19960702894 A KR19960702894 A KR 19960702894A KR 100341982 B1 KR100341982 B1 KR 100341982B1
Authority
KR
South Korea
Prior art keywords
compound
mmol
acid
reaction
pentafluoro
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
KR1019960702894A
Other languages
English (en)
Korean (ko)
Inventor
노턴 피. 피이트
죠셉 피. 버크하트
슈야스 메흐디
Original Assignee
메렐 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 메렐 파마슈티칼스 인크. filed Critical 메렐 파마슈티칼스 인크.
Application granted granted Critical
Publication of KR100341982B1 publication Critical patent/KR100341982B1/ko
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/04—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D277/06—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Neurosurgery (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (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)
  • Enzymes And Modification Thereof (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Pyrrole Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
KR1019960702894A 1993-12-02 1994-11-08 프롤릴엔도펩티다제억제제 Expired - Fee Related KR100341982B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US16110693A 1993-12-02 1993-12-02
US08/161106 1993-12-02
PCT/US1994/012865 WO1995015310A1 (en) 1993-12-02 1994-11-08 Prolyl endopeptidase inhibitors

Publications (1)

Publication Number Publication Date
KR100341982B1 true KR100341982B1 (ko) 2002-11-30

Family

ID=22579844

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019960702894A Expired - Fee Related KR100341982B1 (ko) 1993-12-02 1994-11-08 프롤릴엔도펩티다제억제제

Country Status (19)

Country Link
US (1) US5661167A (enExample)
EP (1) EP0731788B1 (enExample)
JP (1) JPH09506090A (enExample)
KR (1) KR100341982B1 (enExample)
CN (1) CN1136806A (enExample)
AT (1) ATE223894T1 (enExample)
AU (1) AU684861B2 (enExample)
CA (1) CA2177821C (enExample)
DE (1) DE69431359T2 (enExample)
DK (1) DK0731788T3 (enExample)
ES (1) ES2179093T3 (enExample)
HU (1) HUT74687A (enExample)
IL (1) IL111775A (enExample)
NO (1) NO962238D0 (enExample)
NZ (1) NZ276600A (enExample)
PT (1) PT731788E (enExample)
TW (1) TW280818B (enExample)
WO (1) WO1995015310A1 (enExample)
ZA (1) ZA949302B (enExample)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5859031A (en) 1995-06-07 1999-01-12 Gpi Nil Holdings, Inc. Small molecule inhibitors of rotamase enzyme activity
JP4806628B2 (ja) 2003-05-05 2011-11-02 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤
EP1824846A2 (en) 2003-11-03 2007-08-29 Probiodrug AG Novel compounds for the treatment of neurological disorders
WO2005049027A2 (en) 2003-11-03 2005-06-02 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
KR101099206B1 (ko) 2004-02-05 2011-12-27 프로비오드룩 아게 신규한 글루타미닐 시클라제 저해제
US8278345B2 (en) 2006-11-09 2012-10-02 Probiodrug Ag Inhibitors of glutaminyl cyclase
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
EP2481408A3 (en) 2007-03-01 2013-01-09 Probiodrug AG New use of glutaminyl cyclase inhibitors
WO2008128985A1 (en) 2007-04-18 2008-10-30 Probiodrug Ag Thiourea derivatives as glutaminyl cyclase inhibitors
WO2008144748A1 (en) * 2007-05-21 2008-11-27 The Uab Research Foundation Prolyl endopeptidase inhibitors for reducing or preventing neutrophilic inflammation
MX2012002993A (es) 2009-09-11 2012-04-19 Probiodrug Ag Derivados heterociclicos como inhibidores de ciclasa glutaminilo.
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
US8269019B2 (en) 2010-03-10 2012-09-18 Probiodrug Ag Inhibitors
WO2011131748A2 (en) 2010-04-21 2011-10-27 Probiodrug Ag Novel inhibitors
ES2570167T3 (es) 2011-03-16 2016-05-17 Probiodrug Ag Derivados de benzimidazol como inhibidores de glutaminil ciclasa
CA2938369C (en) 2014-01-28 2019-08-06 Spirit Global Energy Solutions, Inc. Down-hole gas and solids separator utilized in production hydrocarbons
PL3461819T3 (pl) 2017-09-29 2020-11-30 Probiodrug Ag Inhibitory cyklazy glutaminylowej

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4518528A (en) * 1983-05-19 1985-05-21 Rasnick David W α Amino fluoro ketones
ZA86746B (en) * 1985-02-04 1986-09-24 Merrell Dow Pharma Novel peptidase inhibitors
DE3712365A1 (de) * 1987-04-11 1988-10-27 Hoechst Ag Neue 2-acylpyrrolidin-derivate, verfahren zu ihrer herstellung, sie enthaltende mittel sowie deren verwendung
US4855303A (en) * 1987-07-01 1989-08-08 Pfizer Inc. Fluorine containing renin inhibitors
JPH0662591B2 (ja) * 1988-12-14 1994-08-17 株式会社ヤクルト本社 新規なチオプロリン誘導体
WO1990012005A1 (fr) * 1989-04-13 1990-10-18 Japan Tobacco Inc. Nouveaux derives aminoacides possedant une activite d'inhibiteur de la prolylendopeptidase

Also Published As

Publication number Publication date
US5661167A (en) 1997-08-26
EP0731788B1 (en) 2002-09-11
DK0731788T3 (da) 2003-01-20
IL111775A0 (en) 1995-01-24
ATE223894T1 (de) 2002-09-15
NZ276600A (en) 1997-09-22
AU1091795A (en) 1995-06-19
CA2177821C (en) 2000-03-28
JPH09506090A (ja) 1997-06-17
DE69431359T2 (de) 2003-07-31
PT731788E (pt) 2003-01-31
HUT74687A (en) 1997-01-28
CA2177821A1 (en) 1995-06-08
ES2179093T3 (es) 2003-01-16
EP0731788A1 (en) 1996-09-18
DE69431359D1 (de) 2002-10-17
WO1995015310A1 (en) 1995-06-08
IL111775A (en) 1998-06-15
HU9601472D0 (en) 1996-07-29
AU684861B2 (en) 1998-01-08
NO962238L (no) 1996-05-31
NO962238D0 (no) 1996-05-31
CN1136806A (zh) 1996-11-27
TW280818B (enExample) 1996-07-11
ZA949302B (en) 1995-08-07

Similar Documents

Publication Publication Date Title
US5496927A (en) Peptidase inhibitors
KR900008004B1 (ko) 펩티다제 억제물의 제조방법
US4518528A (en) α Amino fluoro ketones
AU2003208471B2 (en) Selective dipeptide inhibitors of kallikrein
EP0731788B1 (en) Prolyl endopeptidase inhibitors
US7119073B2 (en) Peptides and their use as inhibitors of hepatitis C virus ns3 protease
US5869454A (en) Arginine keto-amide enzyme inhibitors
US4692458A (en) Anti-hypertensive agents
US4745124A (en) Orally effective anti-hypertensive agents
IE51259B1 (en) Angiotensin converting enzyme inhibitors
HUP0001826A2 (hu) Új trombin inhibitorok
JPH10509727A (ja) Ｎ−末端スルホニル−又はアミノスルホニル基を有する新規のジペプチドのｐ−アミノベンジルアミド
EP0804465B1 (en) Novel elastase inhibitors
US5798377A (en) Thrombin inhibitors
US6693072B2 (en) Elastase inhibitors
US6569876B1 (en) Method and structure for inhibiting activity of serine elastases
US4734420A (en) Anti-hypertensive agents
EP0762887B1 (en) Acylated enol derivatives as prodrugs of elastase inhibitors
US4833152A (en) Anti-hypertensive agents
US4690936A (en) Anti-hypertensive agents
KR19990071822A (ko) α-케토에스테르 및 α-케토아미드의 아실화된 에놀 유도체
KR20060027789A (ko) 프롤릴 올리고펩티다제 억제 활성을 가지는 화합물
EP1140984B1 (en) Selective inhibitors of mmp-12
JPH0532602A (ja) ナフチルメチルアミン誘導体及びこれを含有するレニン阻害剤
US4698355A (en) Anti-hypertensive agents

Legal Events

Date Code Title Description
PA0105 International application

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

R17-X000 Change to representative recorded

St.27 status event code: A-3-3-R10-R17-oth-X000

PG1501 Laying open of application

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

R17-X000 Change to representative recorded

St.27 status event code: A-3-3-R10-R17-oth-X000

A201 Request for examination
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

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-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

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

PG1601 Publication of registration

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

R18-X000 Changes to party contact information recorded

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

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: 20050613

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: 20050613

P22-X000 Classification modified

St.27 status event code: A-4-4-P10-P22-nap-X000