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CO4970736A1 - PROTEASE CO-INHIBITORS - Google Patents

PROTEASE CO-INHIBITORS

Info

Publication number
CO4970736A1
CO4970736A1 CO98050517A CO98050517A CO4970736A1 CO 4970736 A1 CO4970736 A1 CO 4970736A1 CO 98050517 A CO98050517 A CO 98050517A CO 98050517 A CO98050517 A CO 98050517A CO 4970736 A1 CO4970736 A1 CO 4970736A1
Authority
CO
Colombia
Prior art keywords
ncn
6alkyl
alkyl
protease
inhibitors
Prior art date
Application number
CO98050517A
Other languages
Spanish (es)
Inventor
Benjamin Christensen Sigfried
Renee Louise Desjarlais
Forster Cornelia Jutta
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 CO4970736A1 publication Critical patent/CO4970736A1/en

Links

Classifications

    • 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
    • C07D277/38—Nitrogen atoms
    • C07D277/44—Acylated amino or imino radicals
    • C07D277/48—Acylated amino or imino radicals by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof, e.g. carbonylguanidines
    • 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
    • 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

Landscapes

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

Abstract

Un compuesto de Fórmula Ien la que :X, X1 , X2 y X3 se seleccionan independientemente entre -H, -alquilo C1-6 , -alquilo C1-6 sustituido con 1-3 radicales flúor, -cicloalquilo C3-7 , -CN, -C(O)R1 , -C(O)OR1 , -C(O)NR1 R2 , -C(NR1 )NR1 R2 , -C(NCN)NR1 R2 , -C(NCN)SR3 , NO2 , -NR1 SO2 R3 , -NR1 C(O)R1 , -NR1 R2 -NR1 (C=NR1 )NR1 R2 , -NR1 C(O)NR1 R2 , -NR1 C(O)R1 , -NR1 C(O)OR3 , -NR1 C(NCN)SR3 , -NR1 C(NCN)NR1 R2 , -NR1 C(O)C(O)NR1 R2 , -NR1 C(O)C(O)R2 , -Cl, -Br, -I, -F, -OR1 , -O(CH2 )q OR3 , -O(CH2 )2 OH, -OC(O)R1 , -O(CH2 )q C(O)NR1 R2 , -O(CH2 )q C(O)R1 , -SR1 , -SO2 NR1 R2 ó -S(O)m R3 ;m es 0, 1 ó 2;q es 1 ó 2;n es de 0 a 2;R1 es -H, -alquilo C1-6 , -CF3 ó -CH2 CF3 ; o cuando R1 y R2 se toman conjuntamente como NR1 R2 , pueden formar conjuntamente con el nitrógeno un anillo de 5 a 7 miembros que se compone de carbono o de carbono y uno o más heteroátomos adicionales seleccionados entre O, N ó S;R2 es H, -alquilo C1-6 , -CF3 ó -CH2 CF3 ;R3 es -alquilo C1-6 , -CF3 ó -CH2 CF3 ; yX4 es -H, -alquilo C1-6 - -cicloalquilo C3-7 , -COAr, -COO-alquilo C1-6 o -COOAr.A compound of Formula I in which: X, X1, X2 and X3 are independently selected from -H, -C1-6alkyl, -C1-6alkyl substituted with 1-3 fluoro radicals, -C3-7cycloalkyl, -CN, -C (O) R1, -C (O) OR1, -C (O) NR1 R2, -C (NR1) NR1 R2, -C (NCN) NR1 R2, -C (NCN) SR3, NO2, -NR1 SO2 R3, -NR1 C (O) R1, -NR1 R2 -NR1 (C = NR1) NR1 R2, -NR1 C (O) NR1 R2, -NR1 C (O) R1, -NR1 C (O) OR3, -NR1 C (NCN) SR3, -NR1 C (NCN) NR1 R2, -NR1 C (O) C (O) NR1 R2, -NR1 C (O) C (O) R2, -Cl, -Br, -I, - F, -OR1, -O (CH2) q OR3, -O (CH2) 2 OH, -OC (O) R1, -O (CH2) q C (O) NR1 R2, -O (CH2) q C (O ) R1, -SR1, -SO2 NR1 R2 or -S (O) m R3; m is 0, 1 or 2; q is 1 or 2; n is 0 to 2; R1 is -H, -C1-6 alkyl , -CF3 or -CH2 CF3; or when R1 and R2 are taken together as NR1 R2, may form together with nitrogen a 5-7 membered ring consisting of carbon or carbon and one or more additional heteroatoms selected from O, N or S; R2 is H , -C1-6 alkyl, -CF3 or -CH2 CF3: R3 is -C1-6 alkyl, -CF3 or -CH2 CF3; and X4 is -H, -C1-6alkyl - -C3-7cycloalkyl, -COAr, -COO-C1-6alkyl or -COOAr.

CO98050517A 1997-09-04 1998-09-03 PROTEASE CO-INHIBITORS CO4970736A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US5752797P 1997-09-04 1997-09-04

Publications (1)

Publication Number Publication Date
CO4970736A1 true CO4970736A1 (en) 2000-11-07

Family

ID=22011125

Family Applications (1)

Application Number Title Priority Date Filing Date
CO98050517A CO4970736A1 (en) 1997-09-04 1998-09-03 PROTEASE CO-INHIBITORS

Country Status (10)

Country Link
EP (1) EP1015438A4 (en)
JP (1) JP2001514257A (en)
AU (1) AU9300298A (en)
CA (1) CA2302361A1 (en)
CO (1) CO4970736A1 (en)
MA (1) MA26540A1 (en)
PE (1) PE115699A1 (en)
SA (1) SA98190653A (en)
WO (1) WO1999011637A1 (en)
ZA (1) ZA988064B (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
EP1232154A4 (en) 1999-11-10 2004-06-23 Smithkline Beecham Corp Protease inhibitors
AU1474801A (en) 1999-11-10 2001-06-06 Smithkline Beecham Corporation Protease inhibitors
AU1588901A (en) 1999-11-10 2001-06-06 Smithkline Beecham Corporation Protease inhibitors
AU4344101A (en) 2000-03-21 2001-10-03 Smithkline Beecham Corp Protease inhibitors
US6699866B2 (en) 2001-04-17 2004-03-02 Sepracor Inc. Thiazole and other heterocyclic ligands for mammalian dopamine, muscarinic and serotonin receptors and transporters, and methods of use thereof
EP1465862A1 (en) 2002-01-17 2004-10-13 SmithKline Beecham Corporation Cycloalkyl ketoamides derivatives useful as cathepsin k inhibitors
KR100962972B1 (en) 2002-07-26 2010-06-09 주식회사유한양행 1-phenylpiperidin-3-one derivatives and preparation method thereof
DE102004008141A1 (en) 2004-02-19 2005-09-01 Abbott Gmbh & Co. Kg Guanidine compounds and their use as binding partners for 5-HT5 receptors

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS59225172A (en) * 1983-06-03 1984-12-18 Yamanouchi Pharmaceut Co Ltd Novel guanidinothiazole derivative and its preparation

Also Published As

Publication number Publication date
SA98190653A (en) 2005-12-03
MA26540A1 (en) 2004-12-20
AU9300298A (en) 1999-03-22
CA2302361A1 (en) 1999-03-11
WO1999011637A1 (en) 1999-03-11
EP1015438A1 (en) 2000-07-05
EP1015438A4 (en) 2000-11-08
ZA988064B (en) 1999-05-28
PE115699A1 (en) 2000-01-13
JP2001514257A (en) 2001-09-11

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