PE69099A1 - PROTEASE INHIBITORS - Google Patents

PROTEASE INHIBITORS

Info

Publication number
PE69099A1
PE69099A1 PE1998000320A PE00032098A PE69099A1 PE 69099 A1 PE69099 A1 PE 69099A1 PE 1998000320 A PE1998000320 A PE 1998000320A PE 00032098 A PE00032098 A PE 00032098A PE 69099 A1 PE69099 A1 PE 69099A1
Authority
PE
Peru
Prior art keywords
alkyl
het
formula
ccero
alkynyl
Prior art date
Application number
PE1998000320A
Other languages
Spanish (es)
Inventor
Stacie Marie Halbert
Scott Kevin Thompson
Daniel Frank Veber
Evelyne Michaud
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 PE69099A1 publication Critical patent/PE69099A1/en

Links

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

Landscapes

  • 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

SE REFIERE A UN DERIVADO DE HETEROCICLOCETOHIDRAZIDAS DE FORMULA (I), SU SAL; DONDE "L" ES ALQUILO C2-C6, Ar-ALQUILO(Ccero-C6), Het-ALQUILO(Ccero-C6), CH(R4)NR5R6, NR4R7, CH(R4)OAr`, ENTRE OTROS; Ar Y Ar' SON FENILO O NAFTILO; Het ES UN HETEROCICLO MONOCICLICO DE 5-7 MIEMBROS O BICICLICO DE 7-10 MIEMBROS SATURADO O INSATURADO CON 1-4 N, O o S; "W" ES C(O), SO2; UNO DE "X", "Y" o "Z" ES N, C=N, C=C, N=N Y LOS OTROS DOS SON CR10 o N, CON TAL QUE DOS SEAN N; R', R1, R2, R5, R8, R9, R0 Y R12 SON H, ALQUILO C1-C6, ALQUENILO C2-C6, ENTRE OTROS; R3 ES ALQUILO C3-C6, Ar, Het, -CH(R17)-N(R16)-CO-R18 o UN GRUPO DE FORMULA (a), ENTRE OTROS; R4, R11 Y R15 SON H, ALQUILO C1-C6, ALQUENILO C2-C6, ENTRE OTROS; R16 ES H o ALQUILO C1-C6, R17 ES ALQUILO C1-C6, ALQUENILO C2-C6 o CICLOALQUILO C3-C11; R18 ES ALQUILO C3-C6, -O-ALQUILO C3-C6, ENTRE OTROS. UN COMPUESTO PREFERIDO ES N-[2-(CIS-2,6-DIMETIL-4-MORFOLINO)TIAZOL-4-ILCARBONIL]-N'-[N-(4-PIRIDINILMETOXICARBONIL)-L-LEUCINIL]HIDRAZIDA. TAMBIEN SE REFIERE A PROCEDIMIENTOS PARA LA PREPARACION. EL COMPUESTO DE FORMULA (I) INHIBE A LA ENZIMA PROTEASA DE CISTEINA O DE SERINA, COMO CATEPSINA K, PUDIENDO SER UTIL PARA EL TRATAMIENTO DE ENFERMEDADES CARACTERIZADAS POR PERDIDA OSEA COMO OSTEOPOROSIS, PERIODONTITIS O ENFERMEDADES CARACTERIZADAS POR LA DEGRADACION EXCESIVA DEL CARTILAGO O MATRIZIT REFERS TO A DERIVATIVE OF HETEROCICLOCETOHIDRAZIDAS DE FORMULA (I), ITS SALT; WHERE "L" IS C2-C6 ALKYL, Ar-ALKYL (Ccero-C6), Het-ALKYL (Ccero-C6), CH (R4) NR5R6, NR4R7, CH (R4) OAr`, AMONG OTHERS; Ar And Ar 'ARE PHENYL OR NAPHTHYL; Het IS A 5-7 MEMBER MONOCYCLIC OR 7-10 MEMBER BICYCLE SATURATED OR UNSATURATED WITH 1-4 N, O or S; "W" ES C (O), SO2; ONE OF "X", "Y" or "Z" IS N, C = N, C = C, N = N AND THE OTHER TWO ARE CR10 or N, AS LONG AS TWO ARE N; R ', R1, R2, R5, R8, R9, R0 AND R12 ARE H, C1-C6 ALKYL, C2-C6 ALKYNYL, AMONG OTHERS; R3 IS C3-C6 ALKYL, Ar, Het, -CH (R17) -N (R16) -CO-R18 or A GROUP OF FORMULA (a), AMONG OTHERS; R4, R11 AND R15 ARE H, C1-C6 ALKYL, C2-C6 ALKYLL, AMONG OTHERS; R16 IS H or C1-C6 ALKYL, R17 IS C1-C6 ALKYL, C2-C6 ALKYNYL or C3-C11 CYCLOALKYL; R18 IS C3-C6 ALKYL, -O-C3-C6 ALKYL, AMONG OTHERS. A PREFERRED COMPOUND IS N- [2- (CIS-2,6-DIMETIL-4-MORFOLINO) TIAZOL-4-ILCARBONIL] -N '- [N- (4-PIRIDINILMETOXICARBONIL) -L-LEUCINIL] HYDRAZIDE. IT ALSO REFERS TO PROCEDURES FOR PREPARATION. THE COMPOUND OF FORMULA (I) INHIBITS THE ENZYME PROTEASE OF CYSTEINE OR SERINE, LIKE CATEPSINE K, MAY BE USEFUL FOR THE TREATMENT OF DISEASES CHARACTERIZED BY OSTEOPOROSIS, PERIODONTITIS OR CHARACTERIAL DISEASES

PE1998000320A 1997-04-29 1998-04-27 PROTEASE INHIBITORS PE69099A1 (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
PE69099A1 true PE69099A1 (en) 1999-09-26

Family

ID=21935831

Family Applications (1)

Application Number Title Priority Date Filing Date
PE1998000320A PE69099A1 (en) 1997-04-29 1998-04-27 PROTEASE INHIBITORS

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
EP1232154A4 (en) 1999-11-10 2004-06-23 Smithkline Beecham Corp Protease inhibitors
US6596715B1 (en) 1999-11-10 2003-07-22 Smithkline Beecham Corporation Protease inhibitors
WO2001040204A1 (en) * 1999-12-03 2001-06-07 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
CA2404206A1 (en) 2000-03-21 2001-09-27 Smithkline Beecham Corporation Protease inhibitors
EP1465862A1 (en) 2002-01-17 2004-10-13 SmithKline Beecham Corporation Cycloalkyl ketoamides derivatives useful as cathepsin k inhibitors
ATE397597T1 (en) * 2002-07-04 2008-06-15 Aventis Pharma Sa NEW THIOPHENACYLHYDRAZINO DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF, THEIR USE AS MEDICINAL PRODUCTS, PHARMACEUTICAL COMPOSITIONS AND NEW APPLICATIONS
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
WO2014031784A1 (en) 2012-08-23 2014-02-27 Alios Biopharma, Inc. Compounds for the treatment of paramoxyvirus viral infections
JP6485817B2 (en) 2013-08-21 2019-03-20 ヤンセン バイオファーマ インク． Antiviral compound
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
HUP9900964A3 (en) * 1995-10-30 2001-02-28 Smithkline Beecham Corp Protease inhibitors and pharmaceutical compositions containing these compounds

Also Published As

Publication number Publication date
ZA983522B (en) 1998-10-29
PL337725A1 (en) 2000-08-28
EP1019046A1 (en) 2000-07-19
CO4940477A1 (en) 2000-07-24
HUP0001294A2 (en) 2001-04-28
MA26487A1 (en) 2004-12-20
WO1998048799A1 (en) 1998-11-05
IL132629A0 (en) 2001-03-19
CA2287989A1 (en) 1998-11-05
TR199902703T2 (en) 2000-02-21
AU7365198A (en) 1998-11-24
EP1019046A4 (en) 2002-11-27
AR012622A1 (en) 2000-11-08
CN1261276A (en) 2000-07-26
NO995268D0 (en) 1999-10-28
HUP0001294A3 (en) 2001-06-28
JP2002504097A (en) 2002-02-05
NO995268L (en) 1999-11-15
BR9809333A (en) 2000-07-04
KR20010020391A (en) 2001-03-15

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