PT871454E - Inibidores fosforosos que contem protease de cisteina e de serina - Google Patents

Inibidores fosforosos que contem protease de cisteina e de serina

Info

Publication number
PT871454E
PT871454E PT96923756T PT96923756T PT871454E PT 871454 E PT871454 E PT 871454E PT 96923756 T PT96923756 T PT 96923756T PT 96923756 T PT96923756 T PT 96923756T PT 871454 E PT871454 E PT 871454E
Authority
PT
Portugal
Prior art keywords
cysteine
serine
containing protease
inhibitors containing
phosphorus inhibitors
Prior art date
Application number
PT96923756T
Other languages
English (en)
Portuguese (pt)
Inventor
John P Mallamo
Ron Bihovsky
Gregory J Wells
Ming Tao
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
Publication of PT871454E publication Critical patent/PT871454E/pt

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)
PT96923756T 1995-07-17 1996-07-12 Inibidores fosforosos que contem protease de cisteina e de serina PT871454E (pt)

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
PT871454E true PT871454E (pt) 2004-03-31

Family

ID=26669094

Family Applications (1)

Application Number Title Priority Date Filing Date
PT96923756T PT871454E (pt) 1995-07-17 1996-07-12 Inibidores fosforosos que contem protease de cisteina e de serina

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
DK0871454T3 (da) 2004-03-22
EP0871454A4 (cg-RX-API-DMAC10.html) 1998-11-25
DE69630701D1 (de) 2003-12-18
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

Similar Documents

Publication Publication Date Title
PT871454E (pt) Inibidores fosforosos que contem protease de cisteina e de serina
ATE377006T1 (de) Aus d-aminosäuren abgeleitete cystein- und serinproteasehemmer
DE69832268D1 (en) Peptidyl-2-amino-1hydroxyalkansulfonsäuren als cystein-protease-inhibitoren
MY121222A (en) Prodrugs of thrombin inhibitors
EP0677048A1 (en) CYCLIC SULPHONES AS INHIBITORS RETROVIRAL PROTEASES.
EP1032393A4 (en) QUINOLIN-CONTAINING ALPHA-KETOAMIDE-BASED INHIBITORS OF CYSTEIN AND SERINE PROTEASE
ES2106965T3 (es) Nuevas 4-aza-5alfa-androstan-3-onas 7beta-sustituidas como inhibidores de 5alfa-reductasa.
NO990548D0 (no) Inhibitorer for cystein-protease
ATE214928T1 (de) Thrombininhibitoren
MY113489A (en) Reversible protease inhibitors
ZA916393B (en) Inhibitors of serine proteases
ATE193304T1 (de) Inhibitoren der menschlichen neutrophilenelastase
ATE225772T1 (de) Thrombin-inhibitoren
EA199700087A1 (ru) Способ ингибирования катепсина к
BG101687A (bg) Заместени азетидин-2-они за лечение на атеросклероза
BR9815469A (pt) Inibidores de protease
FI942625A7 (fi) Peptidisiä fosfinyylioksimetyyliketoneja interleukiini-1beta-muuttuvan entsyymin inhibiittoreina
SE9602263D0 (sv) New amino acid derivatives
NO992315L (no) Benzotiazo og beslektet heterosykliske gruppe-inneholdende cystein og serinprotease inhibitorer
MX9305784A (es) N-(aceilaminometil) glutaril amino acidos.
NO20002479D0 (no) Kombinasjon av angiotensinkonverterende enzyminhibitor og et diuretikum for behandling av mikrosirkulatoriske forstyrrelser
CA2342985A1 (en) Hydroxamate-containing cysteine and serine protease inhibitors
ES2168816T3 (es) Cemento de inyeccion que contiene inhibidores de la corrosion.
EA199800200A1 (ru) Ингибиторы пролилэндопептидазы
WO1997008934A3 (en) Aryl acrylic acid derivatives useful as protein tyrosine phosphatase inhibitors