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WO1998053814A1 - Composes d'amide heterocycliques utilises en tant qu'inhibiteurs de l'adhesion cellulaire - Google Patents

Composes d'amide heterocycliques utilises en tant qu'inhibiteurs de l'adhesion cellulaire Download PDF

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Publication number
WO1998053814A1
WO1998053814A1 PCT/US1998/010940 US9810940W WO9853814A1 WO 1998053814 A1 WO1998053814 A1 WO 1998053814A1 US 9810940 W US9810940 W US 9810940W WO 9853814 A1 WO9853814 A1 WO 9853814A1
Authority
WO
WIPO (PCT)
Prior art keywords
prolyl
dichlorobenzenesulfonyl
tyrosine
carbonyl
tetrahydroisoquinoline
Prior art date
Application number
PCT/US1998/010940
Other languages
English (en)
Inventor
Philippe L. Durette
William K. Hagmann
Malcolm Maccoss
Sander G. Mills
Richard A. Mumford
Gail M. Van Riper
Jack A. Schmidt
Nancy J. Kevin
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
Priority claimed from GBGB9714314.3A external-priority patent/GB9714314D0/en
Priority claimed from GBGB9800686.9A external-priority patent/GB9800686D0/en
Application filed by Merck & Co., Inc. filed Critical Merck & Co., Inc.
Priority to JP50093499A priority Critical patent/JP2002512625A/ja
Priority to EP98926122A priority patent/EP1001764A4/fr
Priority to CA002291778A priority patent/CA2291778A1/fr
Publication of WO1998053814A1 publication Critical patent/WO1998053814A1/fr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/401—Proline; Derivatives thereof, e.g. captopril
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • 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
    • 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
    • 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
    • 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

Definitions

  • R 1 is 1) Ci-ioalkyl
  • R2 is 1) hydrogen
  • Formula I are those of formula la, lb or Ic.
  • heterocyclyl examples include pyrrolidinyl, piperidinyl, piperazinyl, imidazolidinyl, 2,3-dihydrofuro(2,3-b)pyridyl, benzoxazinyl, tetrahydrohydroquinolinyl, tetrahydroisoquinolinyl, dihydroindolyl, and the like.
  • the term also includes partially unsaturated monocyclic rings that are not aromatic, such as 2- or 4- pyridones attached through the nitrogen or N-substituted-(lH,3H)- pyrimidine-2,4-diones (N-substituted uracils).
  • Halogen includes fluorine, chlorine, bromine and iodine.
  • Step C N-(3.5-Dichlorobenzenesulfonyl)-(L)-prolyl-(L)-4- iodophenylalanine. tert-butyl ester.
  • Step E N- 3.5-dichorobenzenesulfonyl - L -prolyl- L -4- 4 , - fluorobenzoyDphenylalanine
  • Step A 2-Amino-2-norbornanecarboxylic acid, methyl ester hydrochoride. To 25 mL of methanol at 0 °C was added thionyl chloride
  • Step C N-(3.5-DichlorobenzenesulfonyP-(L)-2(S)-methyl-prolyl- (L)-4-(5-((lH.3H)-1.3-dimethylpyrimidine-2.4-dione))phenylalanine
  • the tert-butyl ester of N-(3,5-dichlorobenzenesulfonyl)- (L)-2(S)-methyl-prolyl-(L)-4-(5-((lH,3H)-l,3-dimethylpyrimidine-2,4- dione))-phenylalanine, tert butyl ester (24 mg, 0.035 mmol) was stirred in a solution of trifluoroacetic acid (170 ⁇ L, 2.2 mmol) in methylene chloride (1.0 mL) according to the procedure described in Example 225, Step E to yield the title compound.
  • the CS-1 peptide (Cys-Leu-His-Gly-Pro-Glu-Ile- Leu-Asp-Val-Pro-Ser-Thr), which was synthesized by conventional solid phase chemistry and purified by reverse phase HPLC, was next added to the derivatized BSA at a concentration of 2.5 ⁇ g/ml and allowed to react for 2 hours at room temperature. The plates were washed twice with PBS and stored at 4°C.
  • the cells were incubated at a concentration of 2 x 10 cells/ml in PBS containing a 1 ⁇ M concentration of a fluorogenic esterase substrate (2', 7'-bis-(2-carboxyethyl)-5-(and -6)- carboxyfluorescein, acetoxymethyl ester; BCECF-AM; Molecular Probes Inc., Eugene, Oregon; catalog #B-1150) for 30-60 minutes at 37°C in a 5% CO2/air incubator.
  • the fluorescently labeled Jurkat cells were washed two times in PBS and resuspended in RPMI containing 0.25% BSA at a final concentration of 2.0 x 10 cells/ml.

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Pulmonology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Des composés de formule (I) sont des antagonistes de VLA-4 et/ou de α4β7 et sont, en tant que tels, utiles pour inhiber ou empêcher l'adhésion cellulaire et pour lutter contre des pathologies induites par l'adhésion cellulaire. Ces composés peuvent être formulés sous forme de compositions pharmaceutiques et sont adaptés pour être utilisés dans le traitement de l'asthme, des allergies, des inflammations, de la sclérose en plaques et d'autres maladies inflammatoires et auto-immunes.
PCT/US1998/010940 1997-05-29 1998-05-29 Composes d'amide heterocycliques utilises en tant qu'inhibiteurs de l'adhesion cellulaire WO1998053814A1 (fr)

Priority Applications (3)

Application Number Priority Date Filing Date Title
JP50093499A JP2002512625A (ja) 1997-05-29 1998-05-29 細胞接着阻害薬としての複素環アミド化合物
EP98926122A EP1001764A4 (fr) 1997-05-29 1998-05-29 Composes d'amide heterocycliques utilises en tant qu'inhibiteurs de l'adhesion cellulaire
CA002291778A CA2291778A1 (fr) 1997-05-29 1998-05-29 Composes d'amide heterocycliques utilises en tant qu'inhibiteurs de l'adhesion cellulaire

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US4801797P 1997-05-29 1997-05-29
US60/048,017 1997-05-29
GBGB9714314.3A GB9714314D0 (en) 1997-07-07 1997-07-07 Heterocyclic amide compounds as cell adhesion inhibitors
GB9714314.3 1997-07-07
US6652597P 1997-11-25 1997-11-25
US60/066,525 1997-11-25
GBGB9800686.9A GB9800686D0 (en) 1998-01-14 1998-01-14 Hetrocyclic amide compounds as cell adhesion inhibitors
GB9800686.9 1998-01-14

Publications (1)

Publication Number Publication Date
WO1998053814A1 true WO1998053814A1 (fr) 1998-12-03

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PCT/US1998/010940 WO1998053814A1 (fr) 1997-05-29 1998-05-29 Composes d'amide heterocycliques utilises en tant qu'inhibiteurs de l'adhesion cellulaire

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Country Link
EP (1) EP1001764A4 (fr)
JP (1) JP2002512625A (fr)
CA (1) CA2291778A1 (fr)
WO (1) WO1998053814A1 (fr)

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