WO2001068655A3 - Caprolactam derivatives and uses thereof - Google Patents

Caprolactam derivatives and uses thereof Download PDF

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Publication number
WO2001068655A3
WO2001068655A3 PCT/US2001/007935 US0107935W WO0168655A3 WO 2001068655 A3 WO2001068655 A3 WO 2001068655A3 US 0107935 W US0107935 W US 0107935W WO 0168655 A3 WO0168655 A3 WO 0168655A3
Authority
WO
WIPO (PCT)
Prior art keywords
compounds
caprolactam
caprolactam derivatives
derivatives
src
Prior art date
Application number
PCT/US2001/007935
Other languages
French (fr)
Other versions
WO2001068655A2 (en
Inventor
Pierre Deprez
Dominique Lesuisse
Didier Benard
Original Assignee
Ariad Pharma Inc
Pierre Deprez
Dominique Lesuisse
Didier Benard
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 Ariad Pharma Inc, Pierre Deprez, Dominique Lesuisse, Didier Benard filed Critical Ariad Pharma Inc
Priority to AU2001243601A priority Critical patent/AU2001243601A1/en
Publication of WO2001068655A2 publication Critical patent/WO2001068655A2/en
Publication of WO2001068655A3 publication Critical patent/WO2001068655A3/en

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
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • 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 Table
    • C07F9/02—Phosphorus compounds
    • C07F9/06—Phosphorus compounds without P—C bonds
    • C07F9/08—Esters of oxyacids of phosphorus
    • C07F9/09—Esters of phosphoric acids
    • C07F9/12—Esters of phosphoric acids with hydroxyaryl 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 Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40—Esters thereof
    • C07F9/4003—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4056—Esters of arylalkanephosphonic acids
    • 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 Table
    • 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
    • C07F9/5532—Seven-(or more) 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
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • 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)
  • Biochemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

The invention involves derivatives of caprolactam of the formula (I) in which [A?1], A2 and R1¿ have the meanings indicated in the description, their salts and their prodrugs. The invention also relates to the preparation of such compounds, synthetic intermediates, their use, and in particular, antagonists of the Src SH2 domain and inhibitors of bone resorption and pharmaceutical compounds containing such compounds.
PCT/US2001/007935 2000-03-10 2001-03-12 Caprolactam derivatives and uses thereof WO2001068655A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2001243601A AU2001243601A1 (en) 2000-03-10 2001-03-12 Caprolactam derivatives and uses thereof

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US52324300A 2000-03-10 2000-03-10
US09/523,243 2000-03-10

Publications (2)

Publication Number Publication Date
WO2001068655A2 WO2001068655A2 (en) 2001-09-20
WO2001068655A3 true WO2001068655A3 (en) 2002-08-01

Family

ID=24084232

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/007935 WO2001068655A2 (en) 2000-03-10 2001-03-12 Caprolactam derivatives and uses thereof

Country Status (2)

Country Link
AU (1) AU2001243601A1 (en)
WO (1) WO2001068655A2 (en)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200502221A (en) 2002-10-03 2005-01-16 Astrazeneca Ab Novel lactams and uses thereof
EP1636196A1 (en) 2003-03-14 2006-03-22 AstraZeneca AB Novel lactams and uses thereof
CA2547651C (en) * 2003-12-01 2015-06-23 Cambridge University Technical Services Limited Anti-inflammatory agents
GB2418427A (en) 2004-09-02 2006-03-29 Univ Cambridge Tech Ligands for G-protein coupled receptors
GB2452696B (en) 2007-08-02 2009-09-23 Cambridge Entpr Ltd 3-(2',2'-dimethylpropanoylamino)-tetrahydropyridin-2-one and its use in pharmaceutical compositions
US7662967B2 (en) 2007-08-02 2010-02-16 Cambridge Enterprise Limited Anti-inflammatory compounds and compositions
EP2994143A4 (en) * 2013-05-08 2017-02-01 Board of Regents, The University of Texas System Stat6 inhibitors

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997024339A1 (en) * 1995-12-27 1997-07-10 Ono Pharmaceutical Co., Ltd. Tetrazole derivatives and drugs containing the same as the active ingredient
WO1999031066A1 (en) * 1997-12-18 1999-06-24 Boehringer Ingelheim Pharmaceuticals, Inc. Pyridones as src family sh2 domain inhibitors
FR2781483A1 (en) * 1998-07-21 2000-01-28 Hoechst Marion Roussel Inc Thioazepinone derivatives having Src domain SH2 inhibiting and osteoclast-mediated calcium resorption from bone inhibiting activity, for treatment of osteoporosis

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997024339A1 (en) * 1995-12-27 1997-07-10 Ono Pharmaceutical Co., Ltd. Tetrazole derivatives and drugs containing the same as the active ingredient
WO1999031066A1 (en) * 1997-12-18 1999-06-24 Boehringer Ingelheim Pharmaceuticals, Inc. Pyridones as src family sh2 domain inhibitors
FR2781483A1 (en) * 1998-07-21 2000-01-28 Hoechst Marion Roussel Inc Thioazepinone derivatives having Src domain SH2 inhibiting and osteoclast-mediated calcium resorption from bone inhibiting activity, for treatment of osteoporosis

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
BEAULIEU P L ET AL: "Ligands for the tyrosine kinase p56lck SH2 domain;discovery of potent dipeptide derivatives with monocharge, nonhydrolyzable phosphate replacement", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY. WASHINGTON, US, vol. 42, no. 10, 20 May 1999 (1999-05-20), pages 1757 - 1766, XP002148488, ISSN: 0022-2623 *
CARLSTROM A-S ET AL: "PALLADIUM-CATALYZED SYNTHESIS OF DIDEHYDROAMINO ACID DERIVATIVES", SYNTHESIS, GEORG THIEME VERLAG. STUTTGART, DE, no. 6, 1 June 1989 (1989-06-01), pages 414 - 418, XP000026631, ISSN: 0039-7881 *
NATCHUS M G ET AL: "Design and synthesis of conformationally-constrained MMP inhibitors", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, OXFORD, GB, vol. 8, no. 16, 18 August 1998 (1998-08-18), pages 2077 - 2080, XP004137222, ISSN: 0960-894X *
ROBL J A ET AL: "DUAL METALLOPROTEASE INHIBITORS. 6. INCORPORATION OF BICYCLIC AND SUBSTITUTED MONOCYCLIC AZEPINONES AS DIPEPTIDE SURROGATES IN ANGIOTENSIN-CONVERTING ENZYME/NEUTRAL ENDOPEPTIDASE INHIBITORS", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY. WASHINGTON, US, vol. 39, no. 2, 19 January 1996 (1996-01-19), pages 494 - 502, XP000749701, ISSN: 0022-2623 *
TONG ET AL: "Carboxymethyl-phenylalanine as a replacement for phosphotyrosine in SH2 domain binding", JOURNAL OF BIOLOGICAL CHEMISTRY, AMERICAN SOCIETY OF BIOLOGICAL CHEMISTS, BALTIMORE, MD, US, vol. 273, no. 32, 7 August 1998 (1998-08-07), pages 20238 - 20242, XP002143951, ISSN: 0021-9258 *

Also Published As

Publication number Publication date
AU2001243601A1 (en) 2001-09-24
WO2001068655A2 (en) 2001-09-20

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