AR012622A1 - PROTEASE INHIBITORS, PROCEDURE FOR THE PREPARATION, PHARMACEUTICAL COMPOSITION THAT UNDERSTANDS THEM AND THE USE OF THE SAME IN THE MANUFACTURE OF A MEDICINAL PRODUCT - Google Patents

PROTEASE INHIBITORS, PROCEDURE FOR THE PREPARATION, PHARMACEUTICAL COMPOSITION THAT UNDERSTANDS THEM AND THE USE OF THE SAME IN THE MANUFACTURE OF A MEDICINAL PRODUCT

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Publication number
AR012622A1
AR012622A1 ARP980101999A ARP980101999A AR012622A1 AR 012622 A1 AR012622 A1 AR 012622A1 AR P980101999 A ARP980101999 A AR P980101999A AR P980101999 A ARP980101999 A AR P980101999A AR 012622 A1 AR012622 A1 AR 012622A1
Authority
AR
Argentina
Prior art keywords
alkyl
6alkyl
het
alkenyl
independently
Prior art date
Application number
ARP980101999A
Other languages
Spanish (es)
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 AR012622A1 publication Critical patent/AR012622A1/en

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Classifications

    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—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
    • C07D277/32—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 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
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • C07D417/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biochemistry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Compuesto que inhiben proteasas de formulas (I), en la que: L es alquilo de C2-6, Ar-alquilo de C0-6, Het-alquilo de C0-6, CH(R4)NR5R6, CH(R4)Ar,CH(R4)OAr o NR4R7; Ar es fenilo o naftilo; Ar es fenilo o naftilo; Het es un anillo heterocíclico monocíclico, estable, de 5 a 7 miembros, o un anilloheterocíclico bicíclico, estable, de 7 a 10 miembros, saturado o insaturado, y que consta de átomos de carbono y de uno a cuatro heteroátomos seleccionadosentre el grupo constituido por N, O y S, estando dicho anillo heterocíclico unido a cualquier heteroátomo o átomo de carbono que dé como resultado unaestructura estable, o cualquier grupo bicíclico en el que cualquiera de dichos anillos heterocíclicos monocíclicos esté fusionado con un anillo bencénico; Wes C(O), SO2; X, Y y Z son, independientemente, N, O, S o CR10 con tal que al menos dos de X, Y y Z sean heteroátomos y al menos uno de X, Y y Z sea N, oque uno de X, Y y Z sea C = N, C = C o N = N, y los otros dos sean CR10 o N,con tal que, además, al menos dos de X, Y y Z sean N; -- indica un enlacesencillo o doble en el heterociclo de cinco miembros; R, R1, R2, R5, R8, R9, R10 y R12 son, independientemente, H, alquilo de C1-6, alquenilo de C2-6-, Ar-alquilo de C0-6 o Het-alquilo de C0-6; R3 es alquilo de C3-6, Ar, Het, CH(R11) Ar, CH(R11)OAr, NR11R12, CH(R11)NR12R13; o formula (II); R4, R11 y R15 son,independientemente, H, alquilo de C1-6, alquenilo de C2-6, cicloalquilo de C3-6-alquilo de C0-6, Ar-alquilo de C0-6 o Het-alquilo de C0-6; R7 es alquilode C1-6, alquenilo de C1-6, cicloalquilo de C3-6-alquilo de C0-6, Ar-alquilo de C0-6, o Het-alquilo de C0-6; R6 y R13 son R14, R14C(O), R14C(S), R14OC(O), oR14OC(O)NR9CH(R15)(CO); y R14 es alquilo de C1-6, alquenilo de C2-6, Ar-alquilo de C0-6, o Het alquilo de C0-6; y sus sales, hidratos y solvatosProtease inhibiting compound of formulas (I), wherein: L is C2-6alkyl, Ar-C0-6alkyl, Het-C0-6alkyl, CH (R4) NR5R6, CH (R4) Ar, CH (R4) OAr or NR4R7; Ar is phenyl or naphthyl; Ar is phenyl or naphthyl; Het is a stable, 5- to 7-membered monocyclic heterocyclic ring, or a stable, 7 to 10 membered, bicyclic heterocyclic ring, saturated or unsaturated, and consisting of carbon atoms and one to four heteroatoms selected from the group consisting of N, O and S, said heterocyclic ring being attached to any heteroatom or carbon atom that results in a stable structure, or any bicyclic group in which any of said monocyclic heterocyclic rings is fused with a benzene ring; Wes C (O), SO2; X, Y, and Z are independently N, O, S, or CR10 provided that at least two of X, Y, and Z are heteroatoms and at least one of X, Y, and Z are N, or that one of X, Y, and Z is C = N, C = C or N = N, and the other two are CR10 or N, provided, furthermore, that at least two of X, Y and Z are N; - indicates a single or double bond in the five-membered heterocycle; R, R1, R2, R5, R8, R9, R10 and R12 are independently H, C1-6 alkyl, C2-6 alkenyl, Ar-C0-6 alkyl or Het-C0-6 alkyl; R3 is C3-6alkyl, Ar, Het, CH (R11) Ar, CH (R11) OAr, NR11R12, CH (R11) NR12R13; or formula (II); R4, R11 and R15 are independently H, C1-6 alkyl, C2-6 alkenyl, C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl or Het-C0-6 alkyl ; R7 is C1-6alkyl, C1-6alkenyl, C3-6cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, or Het-C0-6alkyl; R6 and R13 are R14, R14C (O), R14C (S), R14OC (O), or R14OC (O) NR9CH (R15) (CO); and R14 is C1-6 alkyl, C2-6 alkenyl, Ar-C0-6 alkyl, or Het C0-6 alkyl; and its salts, hydrates and solvates

ARP980101999A 1997-04-29 1998-04-29 PROTEASE INHIBITORS, PROCEDURE FOR THE PREPARATION, PHARMACEUTICAL COMPOSITION THAT UNDERSTANDS THEM AND THE USE OF THE SAME IN THE MANUFACTURE OF A MEDICINAL PRODUCT AR012622A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US4506797P 1997-04-29 1997-04-29

Publications (1)

Publication Number Publication Date
AR012622A1 true AR012622A1 (en) 2000-11-08

Family

ID=21935831

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP980101999A AR012622A1 (en) 1997-04-29 1998-04-29 PROTEASE INHIBITORS, PROCEDURE FOR THE PREPARATION, PHARMACEUTICAL COMPOSITION THAT UNDERSTANDS THEM AND THE USE OF THE SAME IN THE MANUFACTURE OF A MEDICINAL PRODUCT

Country Status (18)

Country Link
EP (1) EP1019046A4 (en)
JP (1) JP2002504097A (en)
KR (1) KR20010020391A (en)
CN (1) CN1261276A (en)
AR (1) AR012622A1 (en)
AU (1) AU7365198A (en)
BR (1) BR9809333A (en)
CA (1) CA2287989A1 (en)
CO (1) CO4940477A1 (en)
HU (1) HUP0001294A3 (en)
IL (1) IL132629A0 (en)
MA (1) MA26487A1 (en)
NO (1) NO995268L (en)
PE (1) PE69099A1 (en)
PL (1) PL337725A1 (en)
TR (1) TR199902703T2 (en)
WO (1) WO1998048799A1 (en)
ZA (1) ZA983522B (en)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU1924699A (en) 1997-12-19 1999-07-12 Smithkline Beecham Corporation Compounds of heteroaryl substituted imidazole, their pharmaceutical compositionsand uses
US6100282A (en) * 1998-01-02 2000-08-08 Hoffman-La Roche Inc. Thiazole derivatives
MA26618A1 (en) * 1998-04-09 2004-12-20 Smithkline Beecham Corp PHARMACEUTICAL COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF MALARIA
US6858617B2 (en) 1998-05-26 2005-02-22 Smithkline Beecham Corporation Substituted imidazole compounds
ES2212657T3 (en) 1998-11-04 2004-07-16 Smithkline Beecham Corporation REPLACED PIRAZINAS PIRIDIN-4-IL OR PIRIMIDIN-4-IL.
CO5150165A1 (en) * 1998-11-13 2002-04-29 Smithkline Beecham Plc PROTEASE INHIBITORS: KATEPSIN K TYPE
US20030144175A1 (en) 1998-12-23 2003-07-31 Smithkline Beecham Corporation Protease inhibitors
WO2001034156A1 (en) 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
WO2001034600A1 (en) 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
EP1232155A4 (en) 1999-11-10 2002-11-20 Smithkline Beecham Corp Protease inhibitors
AU1650501A (en) * 1999-12-03 2001-06-12 Ono Pharmaceutical Co. Ltd. 1,3,4-oxadiazoline derivatives and drugs containing these derivatives as the active ingredient
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
MXPA02009305A (en) 2000-03-21 2003-03-12 Smithkline Beecham Corp Protease inhibitors.
JP2005515254A (en) 2002-01-17 2005-05-26 スミスクライン ビーチャム コーポレーション Cycloalkylketoamide derivatives useful as cathepsin K inhibitors
EP1532134B1 (en) * 2002-07-04 2008-06-04 Aventis Pharma S.A. Novel thiophene acyl hydrazino derivatives, method for preparing same, use thereof as medicines, pharmaceutical compositions and novel use
KR100962972B1 (en) 2002-07-26 2010-06-09 주식회사유한양행 1-phenylpiperidin-3-one derivatives and processes for the preparation thereof
WO2011015524A2 (en) * 2009-08-03 2011-02-10 Bayer Cropscience Ag Fungicide heterocycles derivatives
CA2882088C (en) * 2012-08-23 2021-11-23 Alios Biopharma, Inc. Compounds for the treatment of paramoxyvirus viral infections
SG11201600977XA (en) 2013-08-21 2016-03-30 Alios Biopharma Inc Antiviral compounds
MA41614A (en) 2015-02-25 2018-01-02 Alios Biopharma Inc ANTIVIRAL COMPOUNDS

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0934291A1 (en) * 1995-10-30 1999-08-11 Smithkline Beecham Corporation Protease inhibitors

Also Published As

Publication number Publication date
HUP0001294A3 (en) 2001-06-28
BR9809333A (en) 2000-07-04
KR20010020391A (en) 2001-03-15
NO995268L (en) 1999-11-15
AU7365198A (en) 1998-11-24
ZA983522B (en) 1998-10-29
EP1019046A4 (en) 2002-11-27
PL337725A1 (en) 2000-08-28
PE69099A1 (en) 1999-09-26
WO1998048799A1 (en) 1998-11-05
JP2002504097A (en) 2002-02-05
IL132629A0 (en) 2001-03-19
TR199902703T2 (en) 2000-02-21
NO995268D0 (en) 1999-10-28
EP1019046A1 (en) 2000-07-19
CO4940477A1 (en) 2000-07-24
CA2287989A1 (en) 1998-11-05
MA26487A1 (en) 2004-12-20
HUP0001294A2 (en) 2001-04-28
CN1261276A (en) 2000-07-26

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