EP1068304A4 - TREATMENT OF PARASITAL DISEASES BY INHIBITING CYSTEIN PROTEASES OF THE PAPAIN OVERFAMILY - Google Patents

TREATMENT OF PARASITAL DISEASES BY INHIBITING CYSTEIN PROTEASES OF THE PAPAIN OVERFAMILY

Info

Publication number
EP1068304A4
EP1068304A4 EP99916517A EP99916517A EP1068304A4 EP 1068304 A4 EP1068304 A4 EP 1068304A4 EP 99916517 A EP99916517 A EP 99916517A EP 99916517 A EP99916517 A EP 99916517A EP 1068304 A4 EP1068304 A4 EP 1068304A4
Authority
EP
European Patent Office
Prior art keywords
inhibition
treatment
cysteine proteases
parasitic diseases
papain superfamily
Prior art date
Legal status (The legal status 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 status listed.)
Withdrawn
Application number
EP99916517A
Other languages
German (de)
English (en)
French (fr)
Other versions
EP1068304A1 (en
Inventor
Scott Kevin Thompson
Daniel Frank Veber
Thaddeus Anthony Tomaszek
David Graham Tew
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
SmithKline Beecham Corp
Original Assignee
SmithKline Beecham Corp
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 SmithKline Beecham Corp filed Critical SmithKline Beecham Corp
Publication of EP1068304A1 publication Critical patent/EP1068304A1/en
Publication of EP1068304A4 publication Critical patent/EP1068304A4/en
Withdrawn legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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 ring carbon atoms
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/273—2-Pyrrolidones 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 other ring carbon atoms
    • 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
    • C12N9/99—Enzyme inactivation by chemical treatment
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/10—Anthelmintics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/10—Anthelmintics
    • A61P33/12—Schistosomicides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C281/00—Derivatives of carbonic acid containing functional groups covered by groups C07C269/00 - C07C279/00 in which at least one nitrogen atom of these functional groups is further bound to another nitrogen atom not being part of a nitro or nitroso group
    • C07C281/06—Compounds containing any of the groups, e.g. semicarbazides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/22—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
    • C07C311/29—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/56—Amides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/20—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
    • C07D295/215—Radicals derived from nitrogen analogues of carbonic acid
    • 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
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D307/18—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
    • C07D307/22—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Genetics & Genomics (AREA)
  • Engineering & Computer Science (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Biomedical Technology (AREA)
  • Molecular Biology (AREA)
  • General Engineering & Computer Science (AREA)
  • Microbiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Pyrrole Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
EP99916517A 1998-04-09 1999-04-08 TREATMENT OF PARASITAL DISEASES BY INHIBITING CYSTEIN PROTEASES OF THE PAPAIN OVERFAMILY Withdrawn EP1068304A4 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US8122198P 1998-04-09 1998-04-09
US81221P 1998-04-09
PCT/US1999/007723 WO1999053039A1 (en) 1998-04-09 1999-04-08 Treatment of parasitic diseases by inhibition of cysteine proteases of the papain superfamily

Publications (2)

Publication Number Publication Date
EP1068304A1 EP1068304A1 (en) 2001-01-17
EP1068304A4 true EP1068304A4 (en) 2001-05-09

Family

ID=22162839

Family Applications (1)

Application Number Title Priority Date Filing Date
EP99916517A Withdrawn EP1068304A4 (en) 1998-04-09 1999-04-08 TREATMENT OF PARASITAL DISEASES BY INHIBITING CYSTEIN PROTEASES OF THE PAPAIN OVERFAMILY

Country Status (17)

Country Link
EP (1) EP1068304A4 (es)
JP (1) JP2002511491A (es)
KR (1) KR20010042535A (es)
CN (1) CN1304447A (es)
AR (1) AR020065A1 (es)
AU (1) AU3482099A (es)
CA (1) CA2327282A1 (es)
CO (1) CO5080800A1 (es)
DZ (1) DZ2752A1 (es)
HU (1) HUP0101513A2 (es)
IL (1) IL138628A0 (es)
MA (1) MA26618A1 (es)
NO (1) NO20005032L (es)
PE (1) PE20000421A1 (es)
PL (1) PL343373A1 (es)
TR (1) TR200002940T2 (es)
WO (1) WO1999053039A1 (es)

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6143742A (en) * 1997-12-11 2000-11-07 Fuisz Technologies Ltd Treatment for necrotizing infections
MA26631A1 (fr) * 1998-05-21 2004-12-20 Smithkline Beecham Corp Composes a fonction bis-aminomethyl-carbonyle nouveaux, procede pour leur preparation et compositions pharmaceutiques les contenant
US6083966A (en) 1998-08-31 2000-07-04 University Of Florida Thiazoline acid derivatives
NZ526880A (en) 1998-09-21 2005-05-27 Univ Florida Antimalarial agents
EP1488791A3 (en) * 1998-09-21 2005-04-06 University Of Florida Research Foundation, Inc. Antimalarial agents
CO5150165A1 (es) * 1998-11-13 2002-04-29 Smithkline Beecham Plc Inhibidores de proteasa: tipo catepsina k
US20030144175A1 (en) 1998-12-23 2003-07-31 Smithkline Beecham Corporation Protease inhibitors
EP1232155A4 (en) 1999-11-10 2002-11-20 Smithkline Beecham Corp PROTEASE INHIBITORS
EP1232154A4 (en) 1999-11-10 2004-06-23 Smithkline Beecham Corp PROTEASE INHIBITORS
US6534498B1 (en) 1999-11-10 2003-03-18 Smithkline Beecham Corporation Protease inhibitors
CN1416346A (zh) 2000-03-21 2003-05-07 史密丝克莱恩比彻姆公司 蛋白酶抑制剂
US6635784B2 (en) 2000-09-29 2003-10-21 Eastman Chemical Company Process for the preparation of enantiomerically-enriched cyclopropylalanine derivates
ES2261341T3 (es) * 2000-11-17 2006-11-16 Medivir Ab Inhibidor de cisteina proteasa.
IL156776A0 (en) 2001-01-17 2004-02-08 Amura Therapeutics Ltd Inhibitors of cruzipain and other cysteine proteases
MXPA03006224A (es) 2001-01-17 2004-10-15 Amura Therapeutics Ltd Inhibidores de cruzipaina y otras proteasas de cisteina.
US7132449B2 (en) 2001-01-17 2006-11-07 Amura Therapeutics Limited Inhibitors of cruzipain and other cysteine proteases
EP1465862A1 (en) 2002-01-17 2004-10-13 SmithKline Beecham Corporation Cycloalkyl ketoamides derivatives useful as cathepsin k inhibitors
US8921521B2 (en) 2003-06-18 2014-12-30 Ocera Therapeutics, Inc. Macrocyclic modulators of the Ghrelin receptor
US7476653B2 (en) * 2003-06-18 2009-01-13 Tranzyme Pharma, Inc. Macrocyclic modulators of the ghrelin receptor
AU2003270473A1 (en) 2003-09-09 2005-04-27 University Of Florida Desferrithiocin derivatives and their use as iron chelators
BRPI0610644B8 (pt) 2005-04-04 2021-05-25 Univ Florida composto e composição farmacêutica que compreende tal composto e um veículo ou diluente farmaceuticamente aceitável.
MX2008001207A (es) * 2005-07-26 2008-03-24 Merck Frosst Canada Ltd Inhibidores de la cisteina proteasa de la familia de la papaina para el tratamiento de enfermedades parasitarias.
NZ579994A (en) 2007-03-15 2011-09-30 Univ Florida Desferrithiocin polyether analogues useful in the treatment of pathological conditions responsive to chelation or sequestration of trivalent metal
US20100305056A1 (en) 2007-11-29 2010-12-02 Merck Frosst Canada Ltd. Cysteine protease inhibitors for the treatment of parasitic disease
WO2009087379A2 (en) 2008-01-09 2009-07-16 Amura Therapeutics Limited Tetrahydrofuro (3, 2 -b) pyrrol- 3 -one derivatives as inhibitors of cysteine proteinases
AU2012352025B2 (en) 2011-12-16 2018-01-18 University Of Florida Research Foundation, Inc. Uses of 4'-desferrithiocin analogs
EP2633855A1 (en) 2012-03-01 2013-09-04 Veterinärmedizinische Universität Wien Protease inhibitors for treating Trichomonas gallinae infections
EP3071201A4 (en) 2013-11-22 2017-04-26 University of Florida Research Foundation, Inc. Desferrithiocin analogs and uses thereof
KR20170140306A (ko) 2015-04-27 2017-12-20 유니버시티 오브 플로리다 리서치 파운데이션, 인코포레이티드 대사적으로 프로그램화된 금속 킬레이트화제 및 그의 용도

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997016433A1 (en) * 1995-10-30 1997-05-09 Smithkline Beecham Corporation Protease inhibitors
WO1998005336A1 (en) * 1996-08-08 1998-02-12 Smithkline Beecham Corporation Inhibitors of cysteine protease

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5776718A (en) * 1995-03-24 1998-07-07 Arris Pharmaceutical Corporation Reversible protease inhibitors
MA26487A1 (fr) * 1997-04-29 2004-12-20 Smithkline Beecham Corp Heterocyclecetohydrazides inhibiteurs de proteases, procede pour leur preparation et compositions pharmaceutiques les contenant .

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997016433A1 (en) * 1995-10-30 1997-05-09 Smithkline Beecham Corporation Protease inhibitors
WO1998005336A1 (en) * 1996-08-08 1998-02-12 Smithkline Beecham Corporation Inhibitors of cysteine protease

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See also references of WO9953039A1 *

Also Published As

Publication number Publication date
WO1999053039A1 (en) 1999-10-21
MA26618A1 (fr) 2004-12-20
NO20005032L (no) 2000-11-16
TR200002940T2 (tr) 2001-02-21
AU3482099A (en) 1999-11-01
IL138628A0 (en) 2001-10-31
EP1068304A1 (en) 2001-01-17
CO5080800A1 (es) 2001-09-25
HUP0101513A2 (hu) 2001-08-28
AR020065A1 (es) 2002-04-10
JP2002511491A (ja) 2002-04-16
PL343373A1 (en) 2001-08-13
KR20010042535A (ko) 2001-05-25
CA2327282A1 (en) 1999-10-21
PE20000421A1 (es) 2000-05-21
NO20005032D0 (no) 2000-10-06
DZ2752A1 (fr) 2003-09-15
CN1304447A (zh) 2001-07-18

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