CA2174311A1 - Boropeptides renfermant de la pyrrolidine substituee, inhibiteurs de la thrombine - Google Patents

Boropeptides renfermant de la pyrrolidine substituee, inhibiteurs de la thrombine

Info

Publication number
CA2174311A1
CA2174311A1 CA002174311A CA2174311A CA2174311A1 CA 2174311 A1 CA2174311 A1 CA 2174311A1 CA 002174311 A CA002174311 A CA 002174311A CA 2174311 A CA2174311 A CA 2174311A CA 2174311 A1 CA2174311 A1 CA 2174311A1
Authority
CA
Canada
Prior art keywords
compound
formula
methyl
cr6r7
cr8r9
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.)
Abandoned
Application number
CA002174311A
Other languages
English (en)
Inventor
Gregory James Pacofsky
James Russell Pruitt
Patricia Carol Weber
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bristol Myers Squibb Pharma Co
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of CA2174311A1 publication Critical patent/CA2174311A1/fr
Abandoned legal-status Critical Current

Links

Classifications

    • 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
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C07K5/06165—Dipeptides with the first amino acid being heterocyclic and Pro-amino acid; Derivatives thereof
    • 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
    • C07D207/18—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 one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—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 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic System
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/572—Five-membered rings
    • 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
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Abstract

L'invention concerne la découverte de nouveaux analogues d'.alpha.-aminoacide, ainsi que leurs sels et promédicaments acceptables pharmaceutiquement, contenant un noyau de pyrrolidine disubstitué conjugué à un .alpha.-aminoacide, qui sont efficaces en tant qu'inhibiteurs de la thrombine.
CA002174311A 1993-10-07 1994-10-06 Boropeptides renfermant de la pyrrolidine substituee, inhibiteurs de la thrombine Abandoned CA2174311A1 (fr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US13325093A 1993-10-07 1993-10-07
US08/133,250 1993-10-07
US13944393A 1993-10-20 1993-10-20
US08/139,443 1993-10-20

Publications (1)

Publication Number Publication Date
CA2174311A1 true CA2174311A1 (fr) 1995-04-13

Family

ID=26831201

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002174311A Abandoned CA2174311A1 (fr) 1993-10-07 1994-10-06 Boropeptides renfermant de la pyrrolidine substituee, inhibiteurs de la thrombine

Country Status (4)

Country Link
EP (1) EP0722449A1 (fr)
AU (1) AU7922794A (fr)
CA (1) CA2174311A1 (fr)
WO (1) WO1995009859A1 (fr)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA951618B (en) * 1994-03-04 1996-08-27 Lilly Co Eli Antithrombotic agents
US5707966A (en) * 1994-03-04 1998-01-13 Eli Lilly And Company Antithrombotic agents
US5885967A (en) * 1994-03-04 1999-03-23 Eli Lilly And Company Antithrombotic agents
US5602101A (en) * 1994-03-04 1997-02-11 Eli Lilly And Company Antithrombotic agents
CA2143533A1 (fr) * 1994-03-04 1995-09-05 Kenneth D. Kurz Agents antithrombotiques
US5726159A (en) * 1994-03-04 1998-03-10 Eli Lilly And Company Antithrombotic agents
US5705487A (en) * 1994-03-04 1998-01-06 Eli Lilly And Company Antithrombotic agents
US5914319A (en) * 1995-02-27 1999-06-22 Eli Lilly And Company Antithrombotic agents
US5710130A (en) * 1995-02-27 1998-01-20 Eli Lilly And Company Antithrombotic agents
US6638950B2 (en) 2000-06-21 2003-10-28 Bristol-Myers Squibb Pharma Company Piperidine amides as modulators of chemokine receptor activity
US20050288253A1 (en) 2002-09-09 2005-12-29 Trigen Limited Boronic acid salts
JP2006509034A (ja) 2002-09-09 2006-03-16 トライジェン・リミテッド 選択性トロンビン阻害のための非経口製剤に有用なボロン酸塩
CN107011229B (zh) * 2012-01-06 2019-11-05 诺华股份有限公司 杂环化合物和它们的使用方法
WO2014058538A1 (fr) * 2012-08-27 2014-04-17 Merck Sharp & Dohme Corp. Inhibiteurs de thrombine pyrrolidine substituée
US10590084B2 (en) 2016-03-09 2020-03-17 Blade Therapeutics, Inc. Cyclic keto-amide compounds as calpain modulators and methods of production and use thereof
US11292801B2 (en) 2016-07-05 2022-04-05 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
CA3038331A1 (fr) 2016-09-28 2018-04-05 Blade Therapeutics, Inc. Modulateurs de calpain et leurs utilisations therapeutiques

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5187157A (en) * 1987-06-05 1993-02-16 Du Pont Merck Pharmaceutical Company Peptide boronic acid inhibitors of trypsin-like proteases
GB9017694D0 (en) * 1990-08-13 1990-09-26 Sandoz Ltd Improvements in or relating to organic chemistry
GB9024129D0 (en) * 1990-11-06 1990-12-19 Thrombosis Research Trust Inhibitors and substrates of thrombin
EP0503203A1 (fr) * 1991-03-15 1992-09-16 Merrell Dow Pharmaceuticals Inc. Nouveaux inhibiteurs de la thrombine

Also Published As

Publication number Publication date
AU7922794A (en) 1995-05-01
EP0722449A1 (fr) 1996-07-24
WO1995009859A1 (fr) 1995-04-13

Similar Documents

Publication Publication Date Title
EP0145441B1 (fr) Peptides d'acides alpha-aminoboroniques
CA2174311A1 (fr) Boropeptides renfermant de la pyrrolidine substituee, inhibiteurs de la thrombine
EP1050540B1 (fr) Inhibiteurs de dipeptidyl-aminopeptidase de type IV
CA2336597C (fr) Peptides inhibiteurs de l'hepatite c
EP1012180B1 (fr) Analogues de peptides inhibiteurs de l'hepatite c
US7230074B2 (en) Inhibitors of dipeptidyl-aminopeptidase type IV
NZ264128A (en) Thrombin inhibitor or substrate and pharmaceutical compositions
EP0724446A1 (fr) Analogues peptidiques electrophiles servant d'inhibiteurs a des enzymes apparentees a la trypsine
SI9200332A (en) Method for making of prolinboronate ester
WO1995009858A1 (fr) Inhibiteurs de dipeptides d'acide boronique d'enzymes analogues a la trypsine
CA2080474A1 (fr) Inhibiteurs de la dipeptidyl-aminopeptidase de type iv
JPH0381256A (ja) レニン阻害剤
EP0345359B1 (fr) Nouveau derive de l'acide hydroxamique
US5639739A (en) Imidazole containing aminoboronic acids
US5462964A (en) Dipeptide boronic acid inhibitors of trypsin-like enzymes
AU707059B2 (en) Serine protease inhibitors
AU703854B2 (en) Antithrombotic azacycloalkylalkanoyl peptides and pseudopeptides
US5731439A (en) Piperidine containing aminobornic acids
WO1994021650A1 (fr) Acide boronique et ester inhibiteurs de la thrombine
WO2016051289A1 (fr) Préparation pharmaceutique antivirale pour le traitement de l'hépatite c
Hoffmann Synthesis of phosphonic analogues of γ-glutamyl tripeptides and depsipeptides
MXPA01001422A (en) Hepatitis c inhibitor peptides
MXPA00001491A (en) Hepatitis c inhibitor peptide analogues

Legal Events

Date Code Title Description
EEER Examination request
FZDE Dead