AR013079A1 - Derivados sustituidos de tetrahidrofurano-3-onas, de tetrahidropirano-3- onas y tetrahidrotiofen-3-onas, un procedimiento para su preparacion unacomposicion farmaceutica de un medicamento util como inhibidores de proteasas e intermediarios - Google Patents

Derivados sustituidos de tetrahidrofurano-3-onas, de tetrahidropirano-3- onas y tetrahidrotiofen-3-onas, un procedimiento para su preparacion unacomposicion farmaceutica de un medicamento util como inhibidores de proteasas e intermediarios

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Publication number
AR013079A1
AR013079A1 ARP980102069A ARP980102069A AR013079A1 AR 013079 A1 AR013079 A1 AR 013079A1 AR P980102069 A ARP980102069 A AR P980102069A AR P980102069 A ARP980102069 A AR P980102069A AR 013079 A1 AR013079 A1 AR 013079A1
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AR
Argentina
Prior art keywords
alkyl
onas
het
alkenyl
pharmaceutical composition
Prior art date
Application number
ARP980102069A
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English (en)
Original Assignee
Smithkline Beecham Corp
Smithkline Beecham Plc
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, Smithkline Beecham Plc filed Critical Smithkline Beecham Corp
Publication of AR013079A1 publication Critical patent/AR013079A1/es

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    • 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
    • C07D307/26—Heterocyclic compounds containing five-membered rings having one oxygen 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
    • C07D307/30—Heterocyclic compounds containing five-membered rings having one oxygen 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 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
    • C07D307/32—Oxygen 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/06—Anabolic agents
    • 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
    • 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
    • C07D307/83—Oxygen atoms
    • 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
    • C07D307/86—Benzo [b] furans; Hydrogenated benzo [b] furans with an oxygen atom directly attached in position 7
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/16—Heterocyclic compounds containing six-membered rings having one oxygen 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
    • C07D309/28—Heterocyclic compounds containing six-membered rings having one oxygen 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 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
    • C07D309/30—Oxygen atoms, e.g. delta-lactones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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

Abstract

Derivados sustituidos de tetrahidrofurano-3-onas, de tetrahidropirano-3- onas y tetrahidrotiofen-3-onas, caracterizados porque comprenden un compuestosegun la formula (I) en la que: R1 es R, RC(O), RC(S), RSO2, ROC(O), RRNC(O), o ROC(O)NRCH(R6)C(O); R2 es H, alquilo C1-6, alquenilo C2-6,Ar-alquilo C0-6, o Het-alquilo C0-6; R3 es H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6, o Het-alquiloC0-6; R4 es H, alquilo C1-6, alquenilo C2-6, Ar-alquilo C0-C6, o Het-alquilo C0-6; R5, en cada caso, es independientemente H, alquilo C1-6, alquenilo C2-6,Ar-alquilo C0-6, o Het-alquilo C0-6; R6 es H, alquilo C1-6, alquenilo C2-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6, o Het-alquilo C0-6; Res H,alquilo C1-6, alquenilo C2-6, Ar-alquilo C0-6, o Het-alquilo C0-6; R es alquilo C1-6, Ar-alquilo C0-6, Het-alquilo C0-6, Ar-alquenilo C2-6, oHet-alquenilo C2-6, o Het-alquenilo C2-6; X es O o S; y n es 1, 2 o 3; o una de sus sales faramcéuticamente aceptables, que son inhibidores de cisteínaproteasas, particularmente catepsina K, y son utiles en el tratamietno de enfermedades uno de cuyos factores es la inhibicion de pérdida osea,procedimiento para su preparacion, una composicion farmacéutica que los comprende, el uso de los mismos para la fabricacion de un medicamento eintermediarios.
ARP980102069A 1997-05-06 1998-05-04 Derivados sustituidos de tetrahidrofurano-3-onas, de tetrahidropirano-3- onas y tetrahidrotiofen-3-onas, un procedimiento para su preparacion unacomposicion farmaceutica de un medicamento util como inhibidores de proteasas e intermediarios AR013079A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US4575897P 1997-05-06 1997-05-06

Publications (1)

Publication Number Publication Date
AR013079A1 true AR013079A1 (es) 2000-12-13

Family

ID=21939723

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP980102069A AR013079A1 (es) 1997-05-06 1998-05-04 Derivados sustituidos de tetrahidrofurano-3-onas, de tetrahidropirano-3- onas y tetrahidrotiofen-3-onas, un procedimiento para su preparacion unacomposicion farmaceutica de un medicamento util como inhibidores de proteasas e intermediarios

Country Status (19)

Country Link
EP (1) EP1003846A4 (es)
JP (1) JP2001525804A (es)
KR (1) KR20010012256A (es)
CN (1) CN1255161A (es)
AR (1) AR013079A1 (es)
AU (1) AU7562598A (es)
BR (1) BR9809306A (es)
CA (1) CA2288868A1 (es)
CO (1) CO4950618A1 (es)
HU (1) HUP0002247A3 (es)
IL (1) IL132088A0 (es)
NO (1) NO995434D0 (es)
NZ (1) NZ337889A (es)
PE (1) PE71599A1 (es)
PL (1) PL336856A1 (es)
TR (1) TR199902766T2 (es)
UY (1) UY25143A1 (es)
WO (1) WO1998050533A1 (es)
ZA (1) ZA983762B (es)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CO5150165A1 (es) * 1998-11-13 2002-04-29 Smithkline Beecham Plc Inhibidores de proteasa: tipo catepsina k
DZ3083A1 (fr) * 1999-02-19 2004-06-02 Smithkline Beecham Corp Composés nouveaux inhibiteurs de protéases, procédé pour leur préparation et compositions pharmaceutiques les conentant.
GB9911417D0 (en) * 1999-05-18 1999-07-14 Peptide Therapeutics Ltd Furanone derivatives as inhibitors of cathepsin s
EP1232155A4 (en) * 1999-11-10 2002-11-20 Smithkline Beecham Corp PROTEASE INHIBITORS
CA2426271A1 (en) * 2000-10-19 2002-04-25 Naeja Pharmaceutical Inc. Dihydropyrimidine derivatives as cysteine protease inhibitors
WO2002040462A2 (en) * 2000-11-17 2002-05-23 Medivir Uk Limited Cysteine protease inhibitors
ES2261341T3 (es) * 2000-11-17 2006-11-16 Medivir Ab Inhibidor de cisteina proteasa.
NZ526914A (en) * 2001-01-17 2005-02-25 Amura Therapeutics Ltd Cyclic 2-carbonylaminoketones as inhibitors of cruzipain and other cysteine proteases
JP2004520365A (ja) * 2001-01-17 2004-07-08 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
US7132449B2 (en) * 2001-01-17 2006-11-07 Amura Therapeutics Limited Inhibitors of cruzipain and other cysteine proteases
CN1269822C (zh) * 2001-01-17 2006-08-16 阿姆拉医疗有限公司 克鲁兹蛋白酶与其他半胱氨酸蛋白酶的抑制剂
US6841571B2 (en) * 2001-10-29 2005-01-11 Boehringer Ingelheim Pharmaceuticals, Inc. Compounds useful as reversible inhibitors of cysteine proteases
CA2499465A1 (en) * 2002-07-16 2004-01-22 Amura Therapeutics Limited Biologically active compounds
KR100962972B1 (ko) 2002-07-26 2010-06-09 주식회사유한양행 1-페닐피페리딘-3-온 유도체 및 그의 제조방법
NZ545747A (en) 2003-08-06 2010-06-25 Senomyx Inc T1R hetero-oligomeric taste receptors, cell lines that express said receptors, and taste compounds
AU2016206281B2 (en) * 2003-08-06 2017-11-30 Senomyx, Inc. Novel flavors, flavor modifiers, tastants, taste enhancers, umami or sweet tastants, and/or enhancers and use thereof
JP4787765B2 (ja) * 2004-01-08 2011-10-05 メディヴィル・アクチボラグ システインプロテアーゼ阻害剤
WO2007022241A2 (en) * 2005-08-17 2007-02-22 Schering Corporation Novel high affinity quinoline-based kinase ligands
GB0614042D0 (en) 2006-07-14 2006-08-23 Amura Therapeutics Ltd Compounds
US8367709B2 (en) * 2007-06-13 2013-02-05 Bristol-Myers Squibb Company Dipeptide analogs as coagulation factor inhibitors
US7893067B2 (en) 2007-06-27 2011-02-22 Medivir Ab Cysteine protease inhibitors
JP5587790B2 (ja) 2008-01-09 2014-09-10 アミュラ セラピューティクス リミティド 化合物
GB0817424D0 (en) 2008-09-24 2008-10-29 Medivir Ab Protease inhibitors

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3190431B2 (ja) * 1991-07-01 2001-07-23 三菱化学株式会社 ケトン誘導体
JPH05140063A (ja) * 1991-11-19 1993-06-08 Suntory Ltd ジペプチド誘導体及びそれを有効成分とする骨疾患の予防及び治療剤
CA2111930A1 (en) * 1992-12-25 1994-06-26 Ryoichi Ando Aminoketone derivatives
JP2848232B2 (ja) * 1993-02-19 1999-01-20 武田薬品工業株式会社 アルデヒド誘導体
JP3599287B2 (ja) * 1993-04-28 2004-12-08 三菱化学株式会社 スルホンアミド誘導体
US5403952A (en) * 1993-10-08 1995-04-04 Merck & Co., Inc. Substituted cyclic derivatives as novel antidegenerative agents
CN1177293A (zh) * 1995-10-30 1998-03-25 史密丝克莱恩比彻姆公司 抑制组织蛋白酶k的方法
TW448172B (en) * 1996-03-08 2001-08-01 Pharmacia & Upjohn Co Llc Novel hydroxamic acid derivatives useful for the treatment of diseases related to connective tissue degradation
WO1998004539A1 (fr) * 1996-07-29 1998-02-05 Mitsubishi Chemical Corporation Derives heterocycliques oxygenes

Also Published As

Publication number Publication date
AU7562598A (en) 1998-11-27
NO995434L (no) 1999-11-05
NZ337889A (en) 2001-09-28
ZA983762B (en) 1998-11-06
HUP0002247A2 (hu) 2001-05-28
CN1255161A (zh) 2000-05-31
IL132088A0 (en) 2001-03-19
JP2001525804A (ja) 2001-12-11
PE71599A1 (es) 1999-09-15
TR199902766T2 (xx) 2000-02-21
BR9809306A (pt) 2000-07-04
NO995434D0 (no) 1999-11-05
PL336856A1 (en) 2000-07-17
CO4950618A1 (es) 2000-09-01
WO1998050533A1 (en) 1998-11-12
EP1003846A4 (en) 2002-11-13
EP1003846A1 (en) 2000-05-31
KR20010012256A (ko) 2001-02-15
UY25143A1 (es) 1998-11-27
CA2288868A1 (en) 1998-11-12
HUP0002247A3 (en) 2003-01-28

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