AR012374A1 - PROTEASE INHIBITORS, PHARMACEUTICAL COMPOSIONS AND USES FOR THE PREPARATION OF MEDICINES. - Google Patents

PROTEASE INHIBITORS, PHARMACEUTICAL COMPOSIONS AND USES FOR THE PREPARATION OF MEDICINES.

Info

Publication number
AR012374A1
AR012374A1 ARP980101627A ARP980101627A AR012374A1 AR 012374 A1 AR012374 A1 AR 012374A1 AR P980101627 A ARP980101627 A AR P980101627A AR P980101627 A ARP980101627 A AR P980101627A AR 012374 A1 AR012374 A1 AR 012374A1
Authority
AR
Argentina
Prior art keywords
alkyl
het
alkenyl
cycloalkyl
roc
Prior art date
Application number
ARP980101627A
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 AR012374A1 publication Critical patent/AR012374A1/en

Links

Classifications

    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • 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
    • 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

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

Abstract

Compuestos de formula (I), en la cual: X, Y y Z son independientemente N, O, S o CR, con la condicion de que al menos dos de X, Y y Z sonheteroátomos y al menos uno de X, Y y Z es N; o uno de X, Y y Z es C=N, C=C o N=N y los otros dos son CR oN, con la condicion de que X, Y y Z juntoscomprenden al menos dos N, - - - indica un enlace simle o doble; R1 es R, RC(O), RC(S), RSO2, ROC(O), o ROC(O)NRCH(R6)C(O); R2 es H, alquiloC1-6, alquenilo C2-6, Ar-alquilo C0-6, o Het-alquilo c0-6; R3 esH, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquil C3-6-alquilo C0-6, Ar-alquiloC0-6, o Het-alquilo C0-6; R4 es H, alquilo C1-6, alquenilo C2-6, Ar-alquilo C0-6, o Het-alquilo C0-6; R5 es alquilo C1-6, Ar-alquilo C0-6, Het-alquiloC0-6, CH(R6)NRR7, CH(R6)Ar, CH(R6)OAr o NR8R9; cada R6 es independientemente H, alquilo C1-6, alquenilo C2-6, cicloalquil C3-6-alquilo C0-6, Ar-alquiloC0-6, Het-alquilo C0-6; R7 es R, RC(O), RC(S), RSO2, ROC(O), o ROC (O)NRCH(R6)C(O); R8 es H, alquilo C1-6, alquenilo C2-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6, o Het-alquilo C0-6, y R9 es alquilo C1-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6, o Het-alquilo C0-6; oR8 y R9 se combinan para formar un anillo carboxíclico o heterocíclico monocíclico de 3-7 miembros o bicíclico de 7-10 miembros, sustituidoopcionalmente con 1-4 de alquilo C1-6, Ar-alquilo C0-6, Het-alquilo C0-6, alcoxi C1-6, Ar-alcoxi C0-6, Het-alcoxi C0-6, OH, (CH2)1-6NRR, u O(CH2)1-6NRR; R10 es H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6, o Het-alquilo C0-6; cada R esindependientemente H, alquilo C1-6, alquenilo C2-6, Ar-alquilo C0-6, o Het- alquilo C0-6; cada R es independientemente alquilo C1-6, Ar-alquilo C0-6, oCompounds of formula (I), in which: X, Y and Z are independently N, O, S or CR, with the proviso that at least two of X, Y and Z are heteroatoms and at least one of X, Y and Z is N; or one of X, Y and Z is C = N, C = C or N = N and the other two are CR oN, with the proviso that X, Y and Z together comprise at least two N, - - - indicates a bond single or double; R1 is R, RC (O), RC (S), RSO2, ROC (O), or ROC (O) NRCH (R6) C (O); R 2 is H, C 1-6 alkyl, C 2-6 alkenyl, Ar-C 0-6 alkyl, or Het-C 0-6 alkyl; R3 is H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl, or Het-C0-6 alkyl; R4 is H, C1-6 alkyl, C2-6 alkenyl, Ar-C0-6 alkyl, or Het-C0-6 alkyl; R5 is C1-6 alkyl, Ar-C0-6 alkyl, Het-C0-6 alkyl, CH (R6) NRR7, CH (R6) Ar, CH (R6) OAr or NR8R9; each R6 is independently H, C1-6 alkyl, C2-6 alkenyl, C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl, Het-C0-6 alkyl; R7 is R, RC (O), RC (S), RSO2, ROC (O), or ROC (O) NRCH (R6) C (O); R8 is H, C1-6 alkyl, C2-6 alkenyl, C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl, or Het-C0-6 alkyl, and R9 is C1-6 alkyl, C3- cycloalkyl 6-C0-6-alkyl, Ar-C0-6-alkyl, or Het-C0-6-alkyl; oR8 and R9 combine to form a 3-7 membered monocyclic or 7-10 membered bicyclic carboxylic or heterocyclic ring, optionally substituted with 1-4 C1-6 alkyl, Ar-C0-6 alkyl, Het-C0-6 alkyl , C1-6 alkoxy, Ar-C0-6 alkoxy, Het-C0-6 alkoxy, OH, (CH2) 1-6NRR, or O (CH2) 1-6NRR; R10 is H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl, or Het-C0-6 alkyl; each R is independently H, C1-6 alkyl, C2-6 alkenyl, Ar-C0-6 alkyl, or Het-C0-6 alkyl; each R is independently C1-6alkyl, Ar-C0-6alkyl, or

ARP980101627A 1997-04-15 1998-04-08 PROTEASE INHIBITORS, PHARMACEUTICAL COMPOSIONS AND USES FOR THE PREPARATION OF MEDICINES. AR012374A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US4309697P 1997-04-15 1997-04-15
US4453197P 1997-04-23 1997-04-23

Publications (1)

Publication Number Publication Date
AR012374A1 true AR012374A1 (en) 2000-10-18

Family

ID=26720044

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP980101627A AR012374A1 (en) 1997-04-15 1998-04-08 PROTEASE INHIBITORS, PHARMACEUTICAL COMPOSIONS AND USES FOR THE PREPARATION OF MEDICINES.

Country Status (7)

Country Link
EP (1) EP0975612A4 (en)
JP (1) JP2002515902A (en)
AR (1) AR012374A1 (en)
AU (1) AU7252398A (en)
CA (1) CA2285601A1 (en)
CO (1) CO4950541A1 (en)
WO (1) WO1998046582A1 (en)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6723722B1 (en) 1999-06-22 2004-04-20 Takeda Chemical Industries, Ltd. Acylhydrazine derivatives, their production and use
CN1416346A (en) 2000-03-21 2003-05-07 史密丝克莱恩比彻姆公司 Peotease inhibitors
HN2002000136A (en) 2001-06-11 2003-07-31 Basf Ag INHIBITORS OF THE PROTEASE OF HIV VIRUS, COMPOUNDS CONTAINING THEMSELVES, THEIR PHARMACEUTICAL USES AND THE MATERIALS FOR SYNTHESIS
EP1465862A1 (en) 2002-01-17 2004-10-13 SmithKline Beecham Corporation Cycloalkyl ketoamides derivatives useful as cathepsin k inhibitors
WO2012166463A2 (en) * 2011-05-27 2012-12-06 Neosome Life Sciences, LLC Aminooxazole inhibitors of cyclin dependent kinases

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0755937B2 (en) * 1986-07-29 1995-06-14 日本曹達株式会社 Oxa (thia) zolidine derivative, its production method and acaricide
US5244867A (en) * 1989-09-26 1993-09-14 Basf Aktiengesellschaft Oxazole- and thiazolecarboxamides
US5618792A (en) * 1994-11-21 1997-04-08 Cortech, Inc. Substituted heterocyclic compounds useful as inhibitors of (serine proteases) human neutrophil elastase

Also Published As

Publication number Publication date
AU7252398A (en) 1998-11-11
WO1998046582A1 (en) 1998-10-22
JP2002515902A (en) 2002-05-28
EP0975612A4 (en) 2001-06-13
CA2285601A1 (en) 1998-10-22
EP0975612A1 (en) 2000-02-02
CO4950541A1 (en) 2000-09-01

Similar Documents

Publication Publication Date Title
BR0012697A (en) Th2 differentiation inhibitors
TR200201874T2 (en) New compounds and compositions as protease inhibitors.
AR035892A1 (en) DERIVATIVES OF OXAZOL, PROCESS FOR PREPARATION, PHARMACEUTICAL COMPOSITIONS THAT INCLUDE THEM, AND THE USE OF SUCH COMPOUNDS IN THE PREPARATION OF MEDICINES
AR033306A1 (en) COMPOUNDS
CO5721006A2 (en) DERIVATIVES OF PIRAZOLO-QUINAZOLINA, PROCESS FOR ITS PREPARATION AND ITS USE AS QUINASE INHIBITORS
EA200300528A1 (en) 1-ARYL-OR 1-ALKYLSULPHONYLETHETROCYCLYLBENZAZOLES AS LIGANDS 5-HYDROXITRIPTAMINE-6
ES2112650T3 (en) SALTS OF A DERIVATIVE OF INDOL ANTIMIGRAÑA.
AR024060A1 (en) NEW PHARMACEUTICALLY ACTIVE COMPOUNDS
AR070801A1 (en) PYRIMIDIN-PYRIDINE DERIVATIVES
AR039399A1 (en) CHEMICAL COMPOUNDS WITH DOUBLE ACTIVITY, PROCEDURES FOR THE PREPARATION AND PHARMACEUTICAL COMPOSITIONS
AR007898A1 (en) A COMPOUND DERIVED FROM 4-HYDROXY-PIPERIDINE, ITS USE FOR THE PREPARATION OF A MEDICINAL PRODUCT, A PROCEDURE FOR PREPARING IT, AND A MEDICINAL PRODUCT CONTAINING IT.
AR018915A1 (en) INHIBITORS OF DIACIL HYDRAZINIC PROTEASES, PHARMACEUTICAL COMPOSITION THAT INCLUDE IT, USES OF THE SAME FOR THE MANUFACTURE OF A MEDICINAL PRODUCT, A MANUFACTURING MANUFACTURE OF SUCH COMPOUNDS
AR013079A1 (en) SUBSTITUTED DERIVATIVES OF TETRAHIDROFURANO-3-ONAS, TETRAHIDROPIRANO-3- ONAS AND TETRAHIDROTIOFEN-3-ONAS, A PROCEDURE FOR THE PREPARATION OF A PHARMACEUTICAL COMPOSITION OF A MEDICINAL PRODUCT USEFUL AS INTERMEDIATE PROTEIN INHIBITORS
CO4950553A1 (en) 7-TETRAHYDROISOKINOLIN COMPOUNDS AND PROCEDURE FOR THE PREPARATION
AR036864A1 (en) USE OF BENZACEPIN-N-ACETIC ACID COMPOUNDS, AND PROCEDURE FOR THE PREPARATION OF SUCH COMPOUNDS
AR007088A1 (en) 2,4-DIAMINOPYRIMIDINES SUBSTITUTED, INTERMEDIATE COMPOUNDS USED IN ITS PREPARATION, PROCEDURE FOR THE PREPARATION OF SUCH 2,4-DIAMINOPYRIMIDINES CONTAINED, MEDICINES THAT CONTAIN THEM AND EMPLOYMENTS OF SUCH PIRIMIDINES
AR012374A1 (en) PROTEASE INHIBITORS, PHARMACEUTICAL COMPOSIONS AND USES FOR THE PREPARATION OF MEDICINES.
MX9306310A (en) ANTAGONIST COMPOUNDS OF THE 5-HT4 RECEPTOR, PROCEDURE FOR ITS PREPARATION AND PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM
ES2172376B1 (en) NEW DERIVATIVES OF ISOQUINOLEINS, ITS PREPARATION PROCEDURE AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM.
MA33103B1 (en) Derivatives 6 - (substitute 6 - triazolopridzine - sulfanil 5) (A-fluoro-benzotiazole and 5-fluoro-benzimidazole: preparation and use as drugs and as inhibitors)
MD522G2 (en) New thioindol piperidine derivatives processes for preparation thereof, pharmaceutical compositions and use thereof as analgetics
ECSP941050A (en) DERIVATIVES OF BENZOFURANO, PROCESS FOR ITS PREPARATION AND PHARMACEUTICAL COMPOSITION THAT CONTAINS THEM
AR027454A1 (en) DERIVATIVES OF BETA-ALANINA, USEFUL AS RECEIVER ANTAGONISTS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THE USE OF THEM FOR THE PREPARATION OF MEDICINES
CO4970804A1 (en) NEW DERIVATIVES OF VITAMIN D3
UY27910A1 (en) USE OF A SPECIFIC CYCLIC AMINE DERIVATIVE OR ITS PHARMACEUTICALLY ACCEPTABLE SALTS TO TREAT OR PREVENT CARDIAC INSUFFICIENCY