DK0871454T3 - Phosphorholdige inhibitorer af cystein- og serinprotease - Google Patents

Phosphorholdige inhibitorer af cystein- og serinprotease

Info

Publication number
DK0871454T3
DK0871454T3 DK96923756T DK96923756T DK0871454T3 DK 0871454 T3 DK0871454 T3 DK 0871454T3 DK 96923756 T DK96923756 T DK 96923756T DK 96923756 T DK96923756 T DK 96923756T DK 0871454 T3 DK0871454 T3 DK 0871454T3
Authority
DK
Denmark
Prior art keywords
cysteine
phosphorus
serine protease
containing inhibitors
inhibitors
Prior art date
Application number
DK96923756T
Other languages
Danish (da)
English (en)
Inventor
John P Mallamo
Ron Bihovsky
Ming Tao
Gregory J Wells
Original Assignee
Cephalon 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 US08/679,342 external-priority patent/US5639732A/en
Application filed by Cephalon Inc filed Critical Cephalon Inc
Application granted granted Critical
Publication of DK0871454T3 publication Critical patent/DK0871454T3/da

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/06Phosphorus compounds without P—C bonds
    • C07F9/08Esters of oxyacids of phosphorus
    • C07F9/09Esters of phosphoric acids
    • C07F9/091Esters of phosphoric acids with hydroxyalkyl compounds with further substituents on alkyl
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/30Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
    • C07F9/32Esters thereof
    • C07F9/3205Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/3211Esters of acyclic saturated acids which can have further substituents on alkyl
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/30Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
    • C07F9/32Esters thereof
    • C07F9/3205Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/3247Esters of acids containing the structure -C(=X)-P(=X)(R)(XH) or NC-P(=X)(R)(XH), (X = O, S, Se)
    • C07F9/3252Esters of acids containing the structure -C(=X)-P(=X)(R)(XH) or NC-P(=X)(R)(XH), (X = O, S, Se) containing the structure -C(=X)-P(=X)(R)(XR), (X = O, S, Se)
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/30Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
    • C07F9/32Esters thereof
    • C07F9/3258Esters thereof the ester moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/3264Esters with hydroxyalkyl compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/38Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40Esters thereof
    • C07F9/4003Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4006Esters of acyclic acids which can have further substituents on alkyl
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/38Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40Esters thereof
    • C07F9/4003Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4062Esters of acids containing the structure -C(=X)-P(=X)(XR)2 or NC-P(=X)(XR)2, (X = O, S, Se)
    • C07F9/4065Esters of acids containing the structure -C(=X)-P(=X)(XR)2, (X = O, S, Se)
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/38Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40Esters thereof
    • C07F9/4071Esters thereof the ester moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4075Esters with hydroxyalkyl compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/572Five-membered rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6527Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07F9/6533Six-membered rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6571Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
    • C07F9/657163Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms the ring phosphorus atom being bound to at least one carbon atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6571Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
    • C07F9/6574Esters of oxyacids of phosphorus
    • C07F9/65742Esters of oxyacids of phosphorus non-condensed with carbocyclic rings or heterocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06191Dipeptides containing heteroatoms different from O, S, or N
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • 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)
  • Crystallography & Structural Chemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Cosmetics (AREA)
  • Detergent Compositions (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Peptides Or Proteins (AREA)
DK96923756T 1995-07-17 1996-07-12 Phosphorholdige inhibitorer af cystein- og serinprotease DK0871454T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US149195P 1995-07-17 1995-07-17
US08/679,342 US5639732A (en) 1996-07-10 1996-07-10 Phosphorous-containing cysteine and serine protease inhibitors

Publications (1)

Publication Number Publication Date
DK0871454T3 true DK0871454T3 (da) 2004-03-22

Family

ID=26669094

Family Applications (1)

Application Number Title Priority Date Filing Date
DK96923756T DK0871454T3 (da) 1995-07-17 1996-07-12 Phosphorholdige inhibitorer af cystein- og serinprotease

Country Status (10)

Country Link
EP (1) EP0871454B1 (cg-RX-API-DMAC10.html)
JP (1) JPH11509231A (cg-RX-API-DMAC10.html)
AT (1) ATE253920T1 (cg-RX-API-DMAC10.html)
AU (1) AU6458396A (cg-RX-API-DMAC10.html)
CA (1) CA2226414A1 (cg-RX-API-DMAC10.html)
DE (1) DE69630701T2 (cg-RX-API-DMAC10.html)
DK (1) DK0871454T3 (cg-RX-API-DMAC10.html)
ES (1) ES2210377T3 (cg-RX-API-DMAC10.html)
PT (1) PT871454E (cg-RX-API-DMAC10.html)
WO (1) WO1997003679A1 (cg-RX-API-DMAC10.html)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2271116A1 (en) * 1996-11-13 1998-05-22 Gregory J. Wells Benzothiazo and related heterocyclic group-containing cysteine and serine protease inhibitors
US6312662B1 (en) 1998-03-06 2001-11-06 Metabasis Therapeutics, Inc. Prodrugs phosphorus-containing compounds
JP4741725B2 (ja) 1998-03-06 2011-08-10 メタベイシス・セラピューティクス・インコーポレーテッド リン含有化合物のための新規なプロドラッグ
US6489308B1 (en) 1999-03-05 2002-12-03 Trustees Of University Of Technology Corporation Inhibitors of serine protease activity, methods and compositions for treatment of nitric-oxide-induced clinical conditions
US7205404B1 (en) 1999-03-05 2007-04-17 Metabasis Therapeutics, Inc. Phosphorus-containing prodrugs
AU3731400A (en) 1999-03-05 2000-09-21 Trustees Of University Technology Corporation, The Methods and compositions useful in inhibiting apoptosis
US6506733B1 (en) 1999-03-15 2003-01-14 Axys Pharmaceuticals, Inc. Compounds and compositions as protease inhibitors
IL156577A0 (en) 2000-12-22 2004-01-04 Axys Pharm Inc Selective cathepsin s inhibitors and pharmaceutical compositions containing the same
US7030116B2 (en) 2000-12-22 2006-04-18 Aventis Pharmaceuticals Inc. Compounds and compositions as cathepsin inhibitors
BR0212535A (pt) 2001-09-14 2004-10-19 Aventis Pharma Inc Compostos e composições como inibidores de catepsina
HUP0600339A2 (en) * 2001-10-19 2006-08-28 Ortho Mcneil Pharm Inc Phosphonic acid compounds as inhibitors of serine proteases
US7459461B2 (en) 2001-10-19 2008-12-02 Ortho-Mcneil Pharmaceutical, Inc. Phosphonic acid compounds as inhibitors of serine proteases
US6977256B2 (en) 2001-11-14 2005-12-20 Aventis Pharmaceuticals Inc. Compounds and compositions as cathepsin S inhibitors
US7214668B2 (en) 2002-05-13 2007-05-08 Metabasis Therapeutics, Inc. Phosphonic acid based prodrugs of PMEA and its analogues
NZ536327A (en) 2002-05-13 2007-08-31 Metabasis Therapeutics Inc PMEA and PMPA cyclic producing synthesis
BR0315806A (pt) 2002-10-31 2005-09-13 Metabasis Therapeutics Inc Fosfato diésteres cìclicos de 1,3-propano-1-aril diós e seu uso na preparação de pró-drogas
WO2005019434A2 (en) 2003-08-26 2005-03-03 The Regents Of The University Of Colorado, A Body Corporate Serine protease inhibitors for treatment of bacterial infections
CN103374041B (zh) 2004-06-08 2017-05-10 症变治疗公司 路易斯酸介导的环状酯的合成
EP3105238A4 (en) 2014-02-13 2017-11-08 Ligand Pharmaceuticals, Inc. Prodrug compounds and their uses
CN106687118A (zh) 2014-07-02 2017-05-17 配体药物公司 前药化合物及其用途
CN111788196A (zh) 2018-01-09 2020-10-16 配体药物公司 缩醛化合物及其治疗用途
CN113354679A (zh) * 2021-07-05 2021-09-07 南京恒远科技开发有限公司 一种二硬脂酰磷脂酰甘油钠的制备工艺

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69413167T2 (de) * 1993-06-04 1999-05-06 Vertex Pharmaceuticals Inc., Cambridge, Mass. Peptid-Phosphinyloxymethyl-Ketonen als Inhibitoren von Interleukin-1 beta-konvertierenden Enzymen

Also Published As

Publication number Publication date
AU6458396A (en) 1997-02-18
EP0871454A4 (cg-RX-API-DMAC10.html) 1998-11-25
DE69630701D1 (de) 2003-12-18
PT871454E (pt) 2004-03-31
ATE253920T1 (de) 2003-11-15
JPH11509231A (ja) 1999-08-17
EP0871454A1 (en) 1998-10-21
DE69630701T2 (de) 2004-08-19
ES2210377T3 (es) 2004-07-01
EP0871454B1 (en) 2003-11-12
WO1997003679A1 (en) 1997-02-06
HK1016495A1 (en) 1999-11-05
CA2226414A1 (en) 1997-02-06

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