CO5180541A1 - PROTEASE INHIBITORS OF THE 1,3-DIAMINOCETONE TYPE WITH 8-14 MEMBER RING - Google Patents

PROTEASE INHIBITORS OF THE 1,3-DIAMINOCETONE TYPE WITH 8-14 MEMBER RING

Info

Publication number
CO5180541A1
CO5180541A1 CO99078651A CO99078651A CO5180541A1 CO 5180541 A1 CO5180541 A1 CO 5180541A1 CO 99078651 A CO99078651 A CO 99078651A CO 99078651 A CO99078651 A CO 99078651A CO 5180541 A1 CO5180541 A1 CO 5180541A1
Authority
CO
Colombia
Prior art keywords
alkyl
group
het
cycloalkyl
mfi
Prior art date
Application number
CO99078651A
Other languages
Spanish (es)
Inventor
Jr Robert Wells Marquis
Daniel Frank Veber
Original Assignee
Smithkline Beechman 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 Beechman Corp filed Critical Smithkline Beechman Corp
Publication of CO5180541A1 publication Critical patent/CO5180541A1/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

Un compuesto de fórmula I:<EMI FILE="99078651_1" ID="1" IMF=JPEG >en la que:A se selecciona entre el grupo que consta de: C(O) y CH(OH);R1 se selecciona entre el grupo que consta de:<EMI FILE="99078651_2" ID="2" IMF=JPEG >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<EMI FILE="99078651_3" ID="3" IMF=JPEG >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 consta de: H, alquilo C1-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6, y Het-alquilo C0-6,R3 y R8 se seleccionan independientemente entre el grupo que consta de: H, alquenilo C2-6, alquinilo C2-6, Het, Ar o alquilo C1-6 opcionalmenre 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 de:alquilo C1-6, cicloalquiI 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-alquilo C0-6 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)-;oR6 y R7 se conectan para formar un anillo de pirrolidina, piperidina o morfolina; ...A compound of formula I: <EMI FILE = "99078651_1" ID = "1" MFI = JPEG> in which: A is selected from the group consisting of: C (O) and CH (OH); R1 is selected from The group consisting of: <EMI FILE = "99078651_2" ID = "2" MFI = JPEG> 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 <EMI FILE = "99078651_3" ID = "3" MFI = JPEG> R "is selected from the group consisting of: H, C1-6 alkyl, Ar-C0-6 alkyl, and Het-C0-6.R "alkyl" is selected from the group consisting of: H, C1-6 alkyl, C3- cycloalkyl 6-C0-6 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 re the group consisting of: H, C1-6 alkyl, C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl, Het-C0-6 alkyl, 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) -; oR6 and R7 are connected to form a pyrrolidine, piperidine or morpholine ring; ...

CO99078651A 1998-12-23 1999-12-16 PROTEASE INHIBITORS OF THE 1,3-DIAMINOCETONE TYPE WITH 8-14 MEMBER RING CO5180541A1 (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
CO5180541A1 true CO5180541A1 (en) 2002-07-30

Family

ID=22353596

Family Applications (1)

Application Number Title Priority Date Filing Date
CO99078651A CO5180541A1 (en) 1998-12-23 1999-12-16 PROTEASE INHIBITORS OF THE 1,3-DIAMINOCETONE TYPE WITH 8-14 MEMBER RING

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
WO2001034599A1 (en) 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
EP1229914A4 (en) 1999-11-10 2004-06-23 Smithkline Beecham Corp Protease inhibitors
WO2001034600A1 (en) 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
NZ520588A (en) 2000-03-21 2004-06-25 Smithkline Beecham Corp Protease inhibitors
US6982263B2 (en) 2001-06-08 2006-01-03 Boehringer Ingelheim Pharmaceuticals, Inc. Nitriles useful as reversible inhibitors of cysteine proteases
WO2003075853A2 (en) 2002-03-08 2003-09-18 Bristol-Myers Squibb Company Cyclic derivatives as modulators of chemokine receptor activity
EP1796793A4 (en) * 2004-09-07 2009-08-05 Smithkline Beecham Corp Novel compounds
CN101137412B (en) * 2005-01-13 2012-11-07 布里斯托尔-迈尔斯·斯奎布公司 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.
US6369077B1 (en) * 1997-05-08 2002-04-09 Smithkline Beecham Corporation Protease inhibitors

Also Published As

Publication number Publication date
JP2002533452A (en) 2002-10-08
EP1140897A1 (en) 2001-10-10
HK1041690A1 (en) 2002-07-19
AR021970A1 (en) 2002-09-04
PE20001355A1 (en) 2001-01-28
WO2000039115A1 (en) 2000-07-06
EP1140897A4 (en) 2002-04-03
DZ2976A1 (en) 2004-03-15
AU2713100A (en) 2000-07-31

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