WO2001027077A3 - Hydroxysulfonylalkylene-, phosphonoalkylene- or difluoro(phosphononon)methyl- substituted benzene, or benzofuran derivatives as non-peptidic cdc25 inhibitors - Google Patents

Hydroxysulfonylalkylene-, phosphonoalkylene- or difluoro(phosphononon)methyl- substituted benzene, or benzofuran derivatives as non-peptidic cdc25 inhibitors Download PDF

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Publication number
WO2001027077A3
WO2001027077A3 PCT/US2000/027361 US0027361W WO0127077A3 WO 2001027077 A3 WO2001027077 A3 WO 2001027077A3 US 0027361 W US0027361 W US 0027361W WO 0127077 A3 WO0127077 A3 WO 0127077A3
Authority
WO
WIPO (PCT)
Prior art keywords
cdc25
phosphononon
phosphonoalkylene
hydroxysulfonylalkylene
peptidic
Prior art date
Application number
PCT/US2000/027361
Other languages
French (fr)
Other versions
WO2001027077A2 (en
Inventor
Neil R Taylor
David Borhani
David Epstein
Johannes Rudolph
Kurt Ritter
Taro Fujimori
Simon Robinson
Jens Eckstein
Andreas Haupt
Nigel Walker
Richard W Dixon
Deborah Choquette
Jill Blanchard
Arthur Kluge
Kollol Pal
Nicholas Bockovich
Jon Come
Mark Hediger
Original Assignee
Basf Ag
Neil R Taylor
David Borhani
David Epstein
Johannes Rudolph
Kurt Ritter
Taro Fujimori
Simon Robinson
Jens Eckstein
Andreas Haupt
Nigel Walker
Richard W Dixon
Deborah Choquette
Jill Blanchard
Arthur Kluge
Kollol Pal
Nicholas Bockovich
Jon Come
Mark Hediger
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 Basf Ag, Neil R Taylor, David Borhani, David Epstein, Johannes Rudolph, Kurt Ritter, Taro Fujimori, Simon Robinson, Jens Eckstein, Andreas Haupt, Nigel Walker, Richard W Dixon, Deborah Choquette, Jill Blanchard, Arthur Kluge, Kollol Pal, Nicholas Bockovich, Jon Come, Mark Hediger filed Critical Basf Ag
Priority to AU10730/01A priority Critical patent/AU1073001A/en
Publication of WO2001027077A2 publication Critical patent/WO2001027077A2/en
Publication of WO2001027077A3 publication Critical patent/WO2001027077A3/en

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    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/14—Hydrolases (3)
    • C12N9/16—Hydrolases (3) acting on ester bonds (3.1)
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/24—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of a carbon skeleton containing six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/82—Benzo [b] furans; Hydrogenated benzo [b] furans 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 carbon atoms of the hetero ring
    • C07D307/84—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D307/85—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
    • 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)]
    • C07F9/3804—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)] not used, see subgroups
    • C07F9/3882—Arylalkanephosphonic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0205—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)3-C(=0)-, e.g. statine or 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
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0207—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)4-C(=0), e.g. 'isosters', replacing two amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/021—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)n-C(=0)-, n being 5 or 6; for n > 6, classification in C07K5/06 - C07K5/10, according to the moiety having normal peptide bonds
    • 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
    • C07K5/10—Tetrapeptides
    • C07K5/1021—Tetrapeptides with the first amino acid being acidic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2299/00—Coordinates from 3D structures of peptides, e.g. proteins or enzymes

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Medicinal Chemistry (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Biomedical Technology (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • General Engineering & Computer Science (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

The present application relates to compounds of the fornula (VII), wherein the substituents R1-R5, X and Y are as defined in the description and to compounds of formula (VIII) or formula (IX) and when R3 is in the ortho position to X, R?3 and R4¿ are taken together with the atoms to which are each attached to form an aromatic heterocyclic ring. The application further relates to polypeptides which comprise the ligand binding domain of Cdc25, crystalline forms of these polypeptides and the use of these crystalline forms to determine the three dimensional structure of the catalytic domain of Cdc25. The invention also relates to the use of the three dimensional structure of the Cdc25 catalytic domain in methods of designing and/or identifying potential inhibitors of Cdc25 activity, for example, compounds which inhibit the binding of a native substrate to the Cdc25 catalytic domain.
PCT/US2000/027361 1999-10-12 2000-10-04 Hydroxysulfonylalkylene-, phosphonoalkylene- or difluoro(phosphononon)methyl- substituted benzene, or benzofuran derivatives as non-peptidic cdc25 inhibitors WO2001027077A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU10730/01A AU1073001A (en) 1999-10-12 2000-10-04 Method of identifying inhibitors of cdc25

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US21932099P 1999-10-12 1999-10-12
US60/219,320 1999-10-12

Publications (2)

Publication Number Publication Date
WO2001027077A2 WO2001027077A2 (en) 2001-04-19
WO2001027077A3 true WO2001027077A3 (en) 2002-05-23

Family

ID=22818812

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2000/027361 WO2001027077A2 (en) 1999-10-12 2000-10-04 Hydroxysulfonylalkylene-, phosphonoalkylene- or difluoro(phosphononon)methyl- substituted benzene, or benzofuran derivatives as non-peptidic cdc25 inhibitors

Country Status (2)

Country Link
AU (1) AU1073001A (en)
WO (1) WO2001027077A2 (en)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2003508049A (en) * 1999-08-31 2003-03-04 ベーアーエスエフ アクツィエンゲゼルシャフト Methods for identifying inhibitors of Cdc25
WO2002070680A1 (en) * 2001-03-01 2002-09-12 Basf Aktiengesellschaft Method of identifying inhibitors of cdc25
US7057052B2 (en) 2002-09-26 2006-06-06 Duke University Heterocyclic quinones as pharmaceutical agents
WO2006129164A1 (en) 2005-05-31 2006-12-07 Pfizer Japan Inc. Substituted aryloxy-n-bicyclomethyl acetamide compounds as vr1 antagonists

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1991015495A1 (en) * 1990-04-02 1991-10-17 Pfizer Inc. Benzylphosphonic acid tyrosine kinase inhibitors
US5177095A (en) * 1990-02-13 1993-01-05 Merck & Co., Inc. Triazole angiotensin II antagonists incorporating a substituted benzyl element
EP0558062A2 (en) * 1992-02-28 1993-09-01 Ono Pharmaceutical Co., Ltd. Phenoxyacetic acid derivatives and pharmaceutical compositions containing them
EP0617001A1 (en) * 1993-03-19 1994-09-28 Merck & Co. Inc. Phenoxyphenylacetic acid derivatives
US5559135A (en) * 1994-09-14 1996-09-24 Merck & Co., Inc. Endothelin antagonists bearing pyridyl amides
WO1998004257A1 (en) * 1996-07-30 1998-02-05 University Of Pittsburgh Phosphatase inhibitors and methods of use thereof

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5177095A (en) * 1990-02-13 1993-01-05 Merck & Co., Inc. Triazole angiotensin II antagonists incorporating a substituted benzyl element
WO1991015495A1 (en) * 1990-04-02 1991-10-17 Pfizer Inc. Benzylphosphonic acid tyrosine kinase inhibitors
EP0558062A2 (en) * 1992-02-28 1993-09-01 Ono Pharmaceutical Co., Ltd. Phenoxyacetic acid derivatives and pharmaceutical compositions containing them
EP0617001A1 (en) * 1993-03-19 1994-09-28 Merck & Co. Inc. Phenoxyphenylacetic acid derivatives
US5559135A (en) * 1994-09-14 1996-09-24 Merck & Co., Inc. Endothelin antagonists bearing pyridyl amides
WO1998004257A1 (en) * 1996-07-30 1998-02-05 University Of Pittsburgh Phosphatase inhibitors and methods of use thereof

Also Published As

Publication number Publication date
AU1073001A (en) 2001-04-23
WO2001027077A2 (en) 2001-04-19

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