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AR021970A1 - PROTEASE INHIBITORS - Google Patents

PROTEASE INHIBITORS

Info

Publication number
AR021970A1
AR021970A1 ARP990106647A ARP990106647A AR021970A1 AR 021970 A1 AR021970 A1 AR 021970A1 AR P990106647 A ARP990106647 A AR P990106647A AR P990106647 A ARP990106647 A AR P990106647A AR 021970 A1 AR021970 A1 AR 021970A1
Authority
AR
Argentina
Prior art keywords
alkyl
group
het
cycloalkyl
independently selected
Prior art date
Application number
ARP990106647A
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 AR021970A1 publication Critical patent/AR021970A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom 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
    • 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
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • 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
    • C07D225/00—Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom
    • C07D225/02—Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom not condensed with other rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)

Abstract

El presente proporciona compuestos de Formula (1) en la que: A se selecciona entre el grupo que consta de C(O) y CH(OH); R1 se selecciona entre el grupoque consta de las formulas (2), (3), (4) y (5); R2 se selecciona entre el grupo que consta de H, alquilo C1-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6,het-alquilo C0-6, R9C(O)-, R9C(S)-, R9SO2-, R9OC(O)-, R9R12NC(O)-, R9R12NC(S)-, R12HNCH(R12)C(O)-, R9OC(O)NR12CH(R12)C(O)-, adamantil-C(O)-, o un grupo deformula (6); R se selecciona entre el grupo que consta de H, alquilo C1-6, Ar-alquilo C0-6, y Het-alquilo C0-6; R se selecciona entre el grupo que constade H, alquilo 1-6, cicloalquil C3-6-alquilo C1-6, Ar-alquilo C0-6, y Het-alquilo C0-6; R3 y R8 se seleccionan independientemente entre el grupo que consta deH, alquenilo C2-6, alquinilo C2-6, Het, Ar o alquilo C1-6 opcionalmente sustituido con OR13, SR13, NR132, R13NC(O)OR5, CO2R13, CO2NR132, N(C=NH)NH2, Het y Ar;R4 se selecciona entre el grupo que consta de H, alquilo C1-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6, Het-alquilo C0-6, R5C(O)-, R5C(S)-, R5SO2-,R5OC(O)-, R5R14NC(O)-, R5R14NC(S)-, R14HNCH(R14)C(O)- y R5OC(O)NR14CH(R14)C(O)-; R5, R9 y R10 se seleccionan independientemente entre el grupo que consta dealquiloC1-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6, y Het-alquilo C0-6; R6 se selecciona entre el grupo que consta de H, alquilo C1-6, Ar-alquiloC0-6 y Het-alquilo C0-6; R7 se selecciona entre el grupo que consta de H, alquilo C1-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6, Het-alquilo C0-6,R10C(O)-, R10C(S)-, R10SO2-, R10OC(O)-, R10R15NC(O)-, R10R15NC(S)-, R15HNCH(R15)C(O)-, y R10OC(O)NR15CH(R15)C(O)-; o R6 y R7 se conectan para formar un anillode pirrolidina, piperidina o morfolina; cada R se selecciona independientemente entre el grupo que consta de H, alquilo C1-6, Ar-alquilo C0-6 y Het-alquiloC0-6; R11 es Ar; R12, R13, R14 y R15 se seleccionan independientemente entre el grupo que consta de H, alquilo C1-6, Ar-alquilo C0-6 y Het-alquilo C0-6; R* seselecciona entre el grupo que consta de H, alquilo C1-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6 y Het-alquilo C0-6; Z se selecciona entre el grupo queThe present provides compounds of Formula (1) in which: A is selected from the group consisting of C (O) and CH (OH); R1 is selected from the group consisting of formulas (2), (3), (4) and (5); R2 is selected from the group consisting of H, C1-6 alkyl, C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl, het-C0-6 alkyl, R9C (O) -, R9C (S) -, R9SO2-, R9OC (O) -, R9R12NC (O) -, R9R12NC (S) -, R12HNCH (R12) C (O) -, R9OC (O) NR12CH (R12) C (O) -, adamantil-C (O) -, or a deformula group (6); R is selected from the group consisting of H, C1-6 alkyl, Ar-C0-6 alkyl, and Het-C0-6 alkyl; R is selected from the group consisting of H, 1-6 alkyl, C3-6 cycloalkyl-C1-6 alkyl, Ar-C0-6 alkyl, and Het-C0-6 alkyl; R3 and R8 are independently selected from the group consisting of H, C2-6 alkenyl, C2-6 alkynyl, Het, Ar or C1-6 alkyl optionally substituted with OR13, SR13, NR132, R13NC (O) OR5, CO2R13, CO2NR132, N (C = NH) NH2, Het and Ar; R4 is selected from the group consisting of H, C1-6 alkyl, C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl, Het-C0- alkyl 6, R5C (O) -, R5C (S) -, R5SO2-, R5OC (O) -, R5R14NC (O) -, R5R14NC (S) -, R14HNCH (R14) C (O) - and R5OC (O) NR14CH (R14) C (O) -; R5, R9 and R10 are independently selected from the group consisting of C1-6 alkyl, C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl, and Het-C0-6 alkyl; R6 is selected from the group consisting of H, C1-6 alkyl, Ar-C0-6 alkyl and Het-C0-6 alkyl; R7 is selected from the group consisting of H, C1-6 alkyl, C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl, Het-C0-6 alkyl, R10C (O) -, R10C (S) -, R10SO2-, R10OC (O) -, R10R15NC (O) -, R10R15NC (S) -, R15HNCH (R15) C (O) -, and R10OC (O) NR15CH (R15) C (O) -; or R6 and R7 are connected to form a pyrrolidine, piperidine or morpholine ring; each R is independently selected from the group consisting of H, C1-6 alkyl, Ar-C0-6 alkyl and Het-C0-6 alkyl; R11 is Ar; R12, R13, R14 and R15 are independently selected from the group consisting of H, C1-6 alkyl, Ar-C0-6 alkyl and Het-C0-6 alkyl; R * is selected from the group consisting of H, C1-6 alkyl, C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl and Het-C0-6 alkyl; Z is selected from the group that

ARP990106647A 1998-12-23 1999-12-21 PROTEASE INHIBITORS AR021970A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US11414398P 1998-12-23 1998-12-23

Publications (1)

Publication Number Publication Date
AR021970A1 true AR021970A1 (en) 2002-09-04

Family

ID=22353596

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP990106647A AR021970A1 (en) 1998-12-23 1999-12-21 PROTEASE INHIBITORS

Country Status (9)

Country Link
EP (1) EP1140897A4 (en)
JP (1) JP2002533452A (en)
AR (1) AR021970A1 (en)
AU (1) AU2713100A (en)
CO (1) CO5180541A1 (en)
DZ (1) DZ2976A1 (en)
HK (1) HK1041690A1 (en)
PE (1) PE20001355A1 (en)
WO (1) WO2000039115A1 (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030144175A1 (en) 1998-12-23 2003-07-31 Smithkline Beecham Corporation Protease inhibitors
AU1474801A (en) 1999-11-10 2001-06-06 Smithkline Beecham Corporation Protease inhibitors
JP2003513972A (en) 1999-11-10 2003-04-15 スミスクライン・ビーチャム・コーポレイション Protease inhibitor
AU1588901A (en) 1999-11-10 2001-06-06 Smithkline Beecham Corporation Protease inhibitors
US7071184B2 (en) 2000-03-21 2006-07-04 Smithkline Beecham Corporation Protease inhibitors
US6982263B2 (en) 2001-06-08 2006-01-03 Boehringer Ingelheim Pharmaceuticals, Inc. Nitriles useful as reversible inhibitors of cysteine proteases
US7087604B2 (en) 2002-03-08 2006-08-08 Bristol-Myers Squibb Company Cyclic derivatives as modulators of chemokine receptor activity
WO2006029154A2 (en) * 2004-09-07 2006-03-16 Smithkline Beecham Corporation Novel compounds
EP1841504B1 (en) 2005-01-13 2014-11-19 Bristol-Myers Squibb Company Substituted biaryl compounds as factor xia inhibitors

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DZ2285A1 (en) * 1996-08-08 2002-12-25 Smithkline Beecham Corp Cysteine protease inhibitors.
AU7288598A (en) * 1997-05-08 1998-11-27 Smithkline Beecham Corporation Protease inhibitors

Also Published As

Publication number Publication date
CO5180541A1 (en) 2002-07-30
EP1140897A4 (en) 2002-04-03
DZ2976A1 (en) 2004-03-15
WO2000039115A1 (en) 2000-07-06
EP1140897A1 (en) 2001-10-10
HK1041690A1 (en) 2002-07-19
JP2002533452A (en) 2002-10-08
AU2713100A (en) 2000-07-31
PE20001355A1 (en) 2001-01-28

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