IL156577A0 - Selective cathepsin s inhibitors and pharmaceutical compositions containing the same - Google Patents

Selective cathepsin s inhibitors and pharmaceutical compositions containing the same

Info

Publication number
IL156577A0
IL156577A0 IL15657701A IL15657701A IL156577A0 IL 156577 A0 IL156577 A0 IL 156577A0 IL 15657701 A IL15657701 A IL 15657701A IL 15657701 A IL15657701 A IL 15657701A IL 156577 A0 IL156577 A0 IL 156577A0
Authority
IL
Israel
Prior art keywords
inhibitors
same
pharmaceutical compositions
compositions containing
selective cathepsin
Prior art date
Application number
IL15657701A
Other languages
English (en)
Original Assignee
Axys Pharm Inc
Aventis Pharma 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
Application filed by Axys Pharm Inc, Aventis Pharma Inc filed Critical Axys Pharm Inc
Publication of IL156577A0 publication Critical patent/IL156577A0/xx

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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
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    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/51—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/60—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/06—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D205/08—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
    • 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
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    • 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
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    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/40—Acylated substituent nitrogen atom
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
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    • C07D223/12—Nitrogen atoms not forming part of a nitro radical
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    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
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    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
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    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/56—Benzoxazoles; Hydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C—CHEMISTRY; METALLURGY
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    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
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    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/64—Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
    • C—CHEMISTRY; METALLURGY
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    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
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    • C07D285/08—1,2,4-Thiadiazoles; Hydrogenated 1,2,4-thiadiazoles
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    • 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
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    • 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
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IL15657701A 2000-12-22 2001-12-24 Selective cathepsin s inhibitors and pharmaceutical compositions containing the same IL156577A0 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US25760300P 2000-12-22 2000-12-22
PCT/US2001/050680 WO2002051983A2 (en) 2000-12-22 2001-12-24 Novel compounds and compositions as cathepsin inhibitors

Publications (1)

Publication Number Publication Date
IL156577A0 true IL156577A0 (en) 2004-01-04

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IL15657701A IL156577A0 (en) 2000-12-22 2001-12-24 Selective cathepsin s inhibitors and pharmaceutical compositions containing the same

Country Status (7)

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US (2) US7064123B1 (xx)
EP (1) EP1383748A2 (xx)
JP (2) JP2004523506A (xx)
CA (1) CA2433520A1 (xx)
IL (1) IL156577A0 (xx)
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Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2433520A1 (en) * 2000-12-22 2002-07-04 Axys Pharmaceuticals, Inc. Novel compounds and compositions as cathepsin inhibitors
US7030116B2 (en) * 2000-12-22 2006-04-18 Aventis Pharmaceuticals Inc. Compounds and compositions as cathepsin inhibitors
US7132449B2 (en) 2001-01-17 2006-11-07 Amura Therapeutics Limited Inhibitors of cruzipain and other cysteine proteases
NZ526912A (en) 2001-01-17 2005-02-25 Amura Therapeutics Ltd Inhibitors of cruzipain and other cysteine proteases
DK1362052T3 (da) 2001-01-17 2007-07-09 Amura Therapeutics Ltd Inhibitorer af cruzipain og andre cysteinproteaser
US20040147503A1 (en) * 2002-06-04 2004-07-29 Sheila Zipfeil Novel compounds and compositions as cathepsin inhibitors
IL160819A0 (en) * 2001-09-14 2004-08-31 Aventis Pharma Inc Novel compounds and compositions as cathepsin inhibitors
EP1490062B1 (en) 2002-03-26 2007-12-19 Boehringer Ingelheim Pharmaceuticals Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
US7186864B2 (en) 2002-05-29 2007-03-06 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
US7074806B2 (en) 2002-06-06 2006-07-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
WO2004000838A1 (en) * 2002-06-24 2003-12-31 Axys Pharmaceuticals, Inc. Peptidic compounds as cysteine protease inhibitors
TWI376363B (en) 2002-09-24 2012-11-11 Novartis Ag Pharmaceutical combination for treating demyelinating disease
US7109243B2 (en) 2003-03-24 2006-09-19 Irm Llc Inhibitors of cathepsin S
US7384970B2 (en) 2003-03-24 2008-06-10 Irm Llc Inhibitors of cathepsin S
US7173051B2 (en) 2003-06-13 2007-02-06 Irm, Llc Inhibitors of cathepsin S
US7256207B2 (en) 2003-08-20 2007-08-14 Irm Llc Inhibitors of cathepsin S
UY28526A1 (es) 2003-09-24 2005-04-29 Boehringer Ingelheim Pharma Miméticos de glucocorticoides, métodos de preparación composiciones farmacéuticas y usos de los mismos
US7795272B2 (en) 2004-03-13 2010-09-14 Boehringer Ingelheim Pharmaceutical, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof
CA2592514A1 (en) 2004-12-27 2006-07-06 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
WO2009087379A2 (en) 2008-01-09 2009-07-16 Amura Therapeutics Limited Tetrahydrofuro (3, 2 -b) pyrrol- 3 -one derivatives as inhibitors of cysteine proteinases
EP3011958A1 (en) 2008-06-20 2016-04-27 Novartis AG Paediatric compositions for treating multiple sclerosis
WO2022076383A1 (en) * 2020-10-06 2022-04-14 Lysoway Therapeutics, Inc. Sulfonanilide and benzylsulfonyl derivatives, and compositions and methods thereof

Family Cites Families (88)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS429133Y1 (xx) 1966-05-25 1967-05-17
US5874424A (en) 1995-12-20 1999-02-23 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β converting enzyme
US4482670A (en) 1983-03-14 1984-11-13 Dow Corning Corporation Method of polymerizing polydiorganosiloxane fluid-filler mixture using sulfuric or sulfonic acids
DE3606480A1 (de) 1986-02-28 1987-09-03 Behringwerke Ag Oligopeptidylnitrilderivate, diese enthaltende mittel, verfahren zu ihrer herstellung und ihre verwendung
US5055451A (en) 1986-12-22 1991-10-08 Syntex Inc. Aryloxy and arylacyloxy methyl ketones as thiol protease inhibitors
GB8809316D0 (en) 1987-05-11 1988-05-25 Ici America Inc Heterocyclic ketones
JPS63303868A (ja) 1987-06-03 1988-12-12 Oki Electric Ind Co Ltd 誘電体セラミックスの製造方法
DE3827415A1 (de) 1988-08-12 1990-02-15 Behringwerke Ag Peptidderivate, verfahren zu ihrer herstellung und ihre verwendung
EP0376012A3 (en) 1988-12-27 1992-05-06 American Cyanamid Company Renin inhibitors
EP0419683A4 (en) 1989-04-13 1992-03-11 Japan Tobacco Inc. New amino acid derivatives having prolylendopeptidase inhibitor activity
ATE133407T1 (de) 1990-06-07 1996-02-15 Zeria Pharm Co Ltd Neue arylalkanoylaminderivate und diese enthaltendes arzneimittel
CA2111930A1 (en) 1992-12-25 1994-06-26 Ryoichi Ando Aminoketone derivatives
JPH06192199A (ja) 1992-12-25 1994-07-12 Mitsubishi Kasei Corp ケトン誘導体
IL110525A0 (en) 1993-08-09 1994-11-11 Lilly Co Eli Identification and use of protease inhibitors
HUT74733A (en) 1993-11-09 1997-02-28 Merck & Co Inc Piperidines, pyrrolidines and hexahydro-1h-azepines promote release of growth hormone
IL111785A0 (en) 1993-12-03 1995-01-24 Ferring Bv Dp-iv inhibitors and pharmaceutical compositions containing them
US5714484A (en) 1993-12-08 1998-02-03 Prototek, Inc. α-(1,3-dicarbonylenol ether) methyl ketones as cysteine protease inhibitors
US5486623A (en) 1993-12-08 1996-01-23 Prototek, Inc. Cysteine protease inhibitors containing heterocyclic leaving groups
JPH07228529A (ja) 1994-02-17 1995-08-29 Zeria Pharmaceut Co Ltd コリンエステラーゼ賦活剤
US6143790A (en) 1994-03-10 2000-11-07 G.D. Searle & Co. L-N6 -(1-iminoethyl)lysine derivatives useful as nitric oxide synthase inhibitors
US5847135A (en) 1994-06-17 1998-12-08 Vertex Pharmaceuticals, Incorporated Inhibitors of interleukin-1β converting enzyme
US5498616A (en) 1994-11-04 1996-03-12 Cephalon, Inc. Cysteine protease and serine protease inhibitors
US6015791A (en) 1994-11-21 2000-01-18 Cortech Inc. Serine protease inhibitors-cycloheptane derivatives
US5691368A (en) 1995-01-11 1997-11-25 Hoechst Marion Roussel, Inc. Substituted oxazolidine calpain and/or cathepsin B inhibitors
CZ298197A3 (cs) 1995-03-24 1998-03-18 Arris Pharmaceutical Corporation Reverzibilní inhibitory proteas
US6022861A (en) 1995-06-07 2000-02-08 Cor Therapeutics, Inc. Ketoheterocyclic inhibitors of factor Xa
US6069130A (en) 1995-06-07 2000-05-30 Cor Therapeutics, Inc. Ketoheterocyclic inhibitors of factor Xa
WO1996041638A1 (en) 1995-06-13 1996-12-27 Sanofi Winthrop, Inc. Calpain inhibitors for the treatment of neurodegenerative diseases
US6124333A (en) 1995-06-22 2000-09-26 British Biotech Pharmaceuticals Limited Metalloproteinase inhibitors
WO1997003679A1 (en) 1995-07-17 1997-02-06 Cephalon, Inc. Phosphorous-containing cysteine and serine protease inhibitors
JP2002515860A (ja) 1995-11-28 2002-05-28 セフアロン・インコーポレーテツド システイン及びセリンプロテアーゼのｄ―アミノ酸由来のインヒビター
AU3359697A (en) 1996-07-08 1998-02-02 Yamanouchi Pharmaceutical Co., Ltd. Bone resorption inhibitors
EP0960102A1 (en) 1996-07-08 1999-12-01 Du Pont Pharmaceuticals Company AMIDINOINDOLES, AMIDINOAZOLES, AND ANALOGS THEREOF AS INHIBITORS OF FACTOR Xa AND OF THROMBIN
DZ2285A1 (fr) 1996-08-08 2002-12-25 Smithkline Beecham Corp Inhibiteurs de protéase de la cystéine.
BR9712081B1 (pt) 1996-08-28 2010-12-14 derivado peptÍdico, composto, composiÇço farmacÊutica e composiÇço para ativar o sistema nervoso central.
EP0923535A4 (en) 1996-08-28 2001-01-10 Smithkline Beecham Corp CYSTEINE PROTEASE INHIBITORS
UA56197C2 (uk) 1996-11-08 2003-05-15 Зенека Лімітед Гетероциклічні похідні
GB9624817D0 (en) 1996-11-28 1997-01-15 British Biotech Pharm Metalloproteinase inhibitors
US6004933A (en) 1997-04-25 1999-12-21 Cortech Inc. Cysteine protease inhibitors
PL202226B1 (pl) 1997-11-05 2009-06-30 Novartis Ag Nitryl dipeptydowy, jego zastosowanie lecznicze i zawierająca go kompozycja farmaceutyczna
GB9723407D0 (en) 1997-11-05 1998-01-07 Ciba Geigy Ag Organic compounds
US6114310A (en) 1998-01-23 2000-09-05 Microcide Pharmaceuticals, Inc. Efflux pump inhibitors
JP2003535022A (ja) 1998-06-03 2003-11-25 コーテック インコーポレーテッド セリンプロテアーゼ阻害剤としてのアルファー‐ケトオキサジアゾール含有ペプトイド及び非ペプトイド
US5998390A (en) 1998-09-28 1999-12-07 The Research Foundation Of State University Of New York Combination of bisphosphonate and tetracycline
US6037304A (en) * 1999-01-11 2000-03-14 Saudi Basic Industries Corporation Highly active and selective catalysts for the production of unsaturated nitriles, methods of making and using the same
EP1155010A1 (en) 1999-02-20 2001-11-21 AstraZeneca AB Acetamido acetonitrile derivatives as inhibitors of cathepsin l and/or cathepsin s
AU2560000A (en) 1999-02-20 2000-09-04 Astrazeneca Ab Di- and tripeptide nitrile derivatives as inhibitors of cathepsin l and cathepsin
GB9903861D0 (en) * 1999-02-20 1999-04-14 Zeneca Ltd Chemical compounds
CA2360740A1 (en) 1999-03-02 2000-09-08 Boehringer Ingelheim Pharmaceuticals, Inc. Compounds useful as reversible inhibitors of cathepsin s
TW200404789A (en) 1999-03-15 2004-04-01 Axys Pharm Inc Novel compounds and compositions as protease inhibitors
JP2002539190A (ja) 1999-03-15 2002-11-19 アクシス・ファーマシューティカルズ・インコーポレイテッド プロテアーゼ阻害剤としての新規化合物および組成物
HUP0200503A3 (en) 1999-03-15 2005-06-28 Axys Pharmaceuticals Inc South N-cyanomethyl amides as protease inhibitors and pharmaceutical compositions containing them
GB9907683D0 (en) 1999-04-06 1999-05-26 Synphar Lab Inc Substituted azetidin-2-ones as cysteine protease inhibitors
US20030186962A1 (en) * 2000-11-17 2003-10-02 Martin Quibell Cysteine protease inhibitors
GB9911417D0 (en) 1999-05-18 1999-07-14 Peptide Therapeutics Ltd Furanone derivatives as inhibitors of cathepsin s
US6384032B1 (en) * 1999-06-17 2002-05-07 Shionogi Bioresearch Corp. Inhibitors of IL-12 production
JP2001011037A (ja) 1999-07-01 2001-01-16 Kissei Pharmaceut Co Ltd シクロアルカンカルボン酸アミド誘導体
ATE326454T1 (de) 1999-07-30 2006-06-15 Boehringer Ingelheim Pharma Neue bernsteinsäure derivative als cysteine- protease-inhibitoren
GB9917909D0 (en) 1999-07-31 1999-09-29 Synphar Lab Inc Cysteine protease inhibitors
JP2001055366A (ja) 1999-08-12 2001-02-27 Kissei Pharmaceut Co Ltd ビアリール酢酸アミド誘導体
US6420364B1 (en) 1999-09-13 2002-07-16 Boehringer Ingelheim Pharmaceuticals, Inc. Compound useful as reversible inhibitors of cysteine proteases
US6492362B1 (en) 1999-09-16 2002-12-10 Axys Pharmaceuticals, Inc. Compounds and compositions as cathepsin S inhibitors
GB9925264D0 (en) 1999-10-26 1999-12-29 Zeneca Ltd Chemical compounds
US6797720B2 (en) * 1999-12-03 2004-09-28 Ono Pharmaceutical Co., Ltd. 1,3,4-oxadiazoline derivative and an agent comprising its derivative as active ingredient
US7144901B2 (en) * 1999-12-03 2006-12-05 Ono Pharmaceutical Co.,Ltd. Oxadiazole derivatives and drugs containing these derivatives as the active ingredient
HU227039B1 (en) 2000-01-25 2010-05-28 Egis Gyogyszergyar Nyilvanosan New process for the production of quetiapine and intermediates therefor
WO2001055123A1 (fr) * 2000-01-26 2001-08-02 Ono Pharmaceutical Co., Ltd. Composes cycliques a 5 chainons, contenant de l'azote, et medicaments contenant ces composes comme ingredients actifs
KR20020067937A (ko) * 2000-01-26 2002-08-24 오노 야꾸힝 고교 가부시키가이샤 벤젠 축합 헤테로환 유도체 및 그 유도체를 유효성분으로서 함유하는 약제
GB0003111D0 (en) 2000-02-10 2000-03-29 Novartis Ag Organic compounds
US20030114437A1 (en) * 2002-10-17 2003-06-19 Cummings Maxwell D. Protease inhibitors
DE10023470A1 (de) * 2000-05-12 2001-11-15 Basf Ag Verfahren zur Herstellung von Aldehyden
CN1255405C (zh) * 2000-08-14 2006-05-10 奥索-麦克尼尔药品公司 取代的吡唑
AU2001281255B2 (en) * 2000-08-14 2006-07-20 Ortho-Mcneil Pharmaceutical, Inc. Substituted pyrazoles
PT1309593E (pt) * 2000-08-14 2006-08-31 Ortho Mcneil Pharm Inc Pirazoles substituidos
MXPA03001960A (es) * 2000-09-06 2004-03-18 Johnson & Johnson Un metodo para tratar alergias.
CA2433520A1 (en) * 2000-12-22 2002-07-04 Axys Pharmaceuticals, Inc. Novel compounds and compositions as cathepsin inhibitors
JP2004522738A (ja) 2001-01-17 2004-07-29 アミュラ テラピューティクス リミテッド クルジパインおよび他のシステインプロテアーゼの阻害剤としての環状２−カルボニルアミノケトン
DK1362052T3 (da) 2001-01-17 2007-07-09 Amura Therapeutics Ltd Inhibitorer af cruzipain og andre cysteinproteaser
NZ526912A (en) * 2001-01-17 2005-02-25 Amura Therapeutics Ltd Inhibitors of cruzipain and other cysteine proteases
US7132449B2 (en) 2001-01-17 2006-11-07 Amura Therapeutics Limited Inhibitors of cruzipain and other cysteine proteases
WO2002096892A1 (fr) 2001-05-31 2002-12-05 Ono Pharmaceutical Co., Ltd. Composes derives d'oxadiazole et medicaments contenant ces composes comme ingredient actif
CA2448418A1 (en) * 2001-06-01 2002-12-12 Axys Pharmaceuticals, Inc. Chemical compounds and pharmaceutical compositions as cathepsin s inhibitors
US6982263B2 (en) 2001-06-08 2006-01-03 Boehringer Ingelheim Pharmaceuticals, Inc. Nitriles useful as reversible inhibitors of cysteine proteases
US20030144234A1 (en) * 2001-08-30 2003-07-31 Buxton Francis Paul Methods for the treatment of chronic pain and compositions therefor
IL160819A0 (en) * 2001-09-14 2004-08-31 Aventis Pharma Inc Novel compounds and compositions as cathepsin inhibitors
AU2002340031A1 (en) * 2001-10-02 2003-04-14 Boehringer Ingelheim Pharmaceuticals, Inc. Compounds useful as reversible inhibitors of cysteine proteases
WO2003037892A1 (en) * 2001-10-29 2003-05-08 Boehringer Ingelheim Pharmaceuticals, Inc. Compounds useful as reversible inhibitors of cysteine proteases
TW561657B (en) * 2002-04-19 2003-11-11 Ritek Corp Device for peeling cladding layer of fiber ribbon

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