CO5280088A1 - PROTEASA INHIBITORS - Google Patents

PROTEASA INHIBITORS

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Publication number
CO5280088A1
CO5280088A1 CO01029287A CO01029287A CO5280088A1 CO 5280088 A1 CO5280088 A1 CO 5280088A1 CO 01029287 A CO01029287 A CO 01029287A CO 01029287 A CO01029287 A CO 01029287A CO 5280088 A1 CO5280088 A1 CO 5280088A1
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Colombia
Prior art keywords
alkyl
het
group
cycloalkyl
mfi
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Application number
CO01029287A
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Spanish (es)
Inventor
Marquis Robert Wells Jr
Daniel Frank Veber
Ru-Maxwell Yu
David Cummings
Scott Kevin Thompson
Dennis Shinji Yamashita
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Smithkline Beecham Corp
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Publication of CO5280088A1 publication Critical patent/CO5280088A1/en

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    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/02—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D223/06—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings 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
    • C07D223/08—Oxygen atoms
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D421/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having selenium, tellurium, or halogen atoms as ring hetero atoms
    • C07D421/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having selenium, tellurium, or halogen atoms as ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems

Abstract

Un método para inhibir catepsina S que comprende administrar a un animal, particularmente un mamífero, lo más particularmente un ser humano que necesita de ello, una cantidad eficaz de un compuesto de Fórmula I: <EMI FILE="01029287_1" ID="1" IMF=JPEG > en la que:R1 se selecciona del grupo formado por:<EMI FILE="01029287_2" ID="2" IMF=JPEG > R2 se selecciona del grupo formado por: 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)-, R9R11NC(O)-, R9R11NC(S)-, R9(R11)NSO2-,<EMI FILE="01029287_3" ID="3" IMF=JPEG ><EMI FILE="01029287_4" ID="4" IMF=JPEG >R3 se selecciona del grupo formado por: H, alquilo C1-6, cicloalquil C3-6-alquilo C0-6, alquenilo C2-6, alquinilo C2-6, Het-alquilo C0-6, Ar-alquilo C0-6, Ar-Ar-alquilo C0-6, Ar-Het-alquilo C0-6, Het-Ar-alquilo C0-6 y Het-Het-alquilo C0-6;R3 y R' pueden estar unidos dos para formar un anillo de pirrolidina, piperidina o morfolina; R4 se selecciona del grupo formado por 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)-, R5R13NC(O)- y R5R13NC(S)-;R5 se selecciona del grupo formado por H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6 y Het-alquilo C0-6; - 2 -R6 se selecciona del grupo formado por H, alquilo C1-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6 y het-alquilo C0-6;R7 se selecciona del grupo formado por: 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)-, R10R14NC(O)- y R10R14NC(S)-,R8 selecciona del grupo formado por H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, Het-alquilo C0-6 y Ar-alquilo C0-6; R9 se selecciona del grupo formado por: alquilo C1-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6 y Het-alquilo C0-6,R10 se selecciona del grupo formado por: alquilo C1-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6 y Het-alquilo C0-6;R11 se selecciona del grupo formado por H, alquilo C1-6, Ar-alquilo C0-6 y Het-alquilo C0-6; R12 se selecciona del grupo formado por: H, alquilo C1-6, Ar-alquilo C0-6 y Het-alquilo C0-6; R13 se selecciona del grupo formado por: H, alquilo C1-6, Ar-alquilo C0-6 y Het-alquilo C0-6, R14 se selecciona del grupo formado por: H, alquilo C1-6, Ar-alquilo C0-6 y Het-alquilo C0-6; R' se selecciona del grupo formado por: H, alquilo C1-6, Ar-alquilo C0-6 y Het-alquilo C0-6;R´´ se selecciona del grupo formado por: H, alquilo C1-6, Ar-alquilo C0-6 o Het-alquilo C0-6;R'" se selecciona del grupo formado por: H, alquilo C1-6, cicloalquil C3-6-aIquilo C0-6, Ar-alquilo C0-6 y Het-alquilo C0-6;X se selecciona del grupo formado por: CH2, S y O;Z se selecciona del grupo formado por: C(O) y CH2;y sus sales, hidratos y solvatos farmacéuticamente aceptables.1 Un compuesto según la reivindicación 16, en el que alquilo C1-6 se selecciona del grupo formado por: 5-, 6- y 7-alquilo C1-6.A method for inhibiting cathepsin S which comprises administering to an animal, particularly a mammal, most particularly a human being in need thereof, an effective amount of a compound of Formula I: <EMI FILE = "01029287_1" ID = "1" MFI = JPEG> in which: R1 is selected from the group consisting of: <EMI FILE = "01029287_2" ID = "2" MFI = JPEG> R2 is selected from the group consisting of: H, C1-6 alkyl, C3- cycloalkyl 6-C0-6 alkyl, Ar-C0-6 alkyl, Het-C0-6 alkyl, R9C (O) -, R9C (S) -, R9SO2-, R9OC (O) -, R9R11NC (O) -, R9R11NC ( S) -, R9 (R11) NSO2 -, <EMI FILE = "01029287_3" ID = "3" MFI = JPEG> <EMI FILE = "01029287_4" ID = "4" MFI = JPEG> R3 is selected from the group consisting of : H, C1-6 alkyl, C3-6 cycloalkyl-C0-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, Het-C0-6 alkyl, Ar-C0-6 alkyl, Ar-Ar-C0-6 alkyl , Ar-Het-C0-6 alkyl, Het-Ar-C0-6 alkyl and Het-Het-C0-6 alkyl; R3 and R 'can be joined together to form a pyrrolidine, piperidine or morpholine ring; R4 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, R5C (O) -, R5C (S) -, R5SO2-, R5OC (O) -, R5R13NC (O) - and R5R13NC (S) -; R5 is selected from the group consisting of H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6- cycloalkyl C0-6 alkyl, Ar-C0-6 alkyl and Het-C0-6 alkyl; - 2 -R6 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; 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) - , R10R14NC (O) - and R10R14NC (S) -, R8 selects from the group consisting of H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, Het-C0-6 alkyl and Ar-C0-6 alkyl; R9 is selected from the group consisting of: C1-6 alkyl, C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl and Het-C0-6 alkyl, R10 is selected from the group consisting of: C1-6 alkyl, C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl and Het-C0-6 alkyl; R11 is selected from the group consisting of H, C1-6 alkyl, Ar-C0-6 alkyl and Het-C0- alkyl 6; R12 is selected from the group consisting of: H, C1-6 alkyl, Ar-C0-6 alkyl and Het-C0-6 alkyl; R13 is selected from the group consisting of: H, C1-6 alkyl, Ar-C0-6 alkyl and Het-C0-6 alkyl, R14 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, C1-6 alkyl, Ar-C0-6 alkyl and Het-C0-6 alkyl; R' is selected from the group consisting of: H, C1-6 alkyl, Ar-alkyl C0-6 or 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- alkyl 6; X is selected from the group consisting of: CH2, S and O; Z is selected from the group consisting of: C (O) and CH2; and its pharmaceutically acceptable salts, hydrates and solvates. 1 A compound according to claim 16, in which C1-6 alkyl is selected from the group consisting of: 5-, 6- and 7-C1-6 alkyl.

CO01029287A 2000-04-18 2001-04-16 PROTEASA INHIBITORS CO5280088A1 (en)

Applications Claiming Priority (2)

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US19849300P 2000-04-18 2000-04-18
US27381101P 2001-03-07 2001-03-07

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EP (1) EP1278502A4 (en)
JP (1) JP2004526662A (en)
KR (1) KR20020089482A (en)
CN (1) CN1431904A (en)
AR (1) AR032319A1 (en)
AU (1) AU9050701A (en)
BR (1) BR0108954A (en)
CA (1) CA2406829A1 (en)
CO (1) CO5280088A1 (en)
CZ (1) CZ20023460A3 (en)
HK (1) HK1053785A1 (en)
HU (1) HUP0301781A2 (en)
IL (1) IL151087A0 (en)
MX (1) MXPA02010276A (en)
NO (1) NO20025005L (en)
PL (1) PL366040A1 (en)
WO (1) WO2001089451A2 (en)

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KR20080103117A (en) 2002-09-24 2008-11-26 노파르티스 아게 Sphingosine-1-phosphate receptor agonists in the treatment of demyelinating disorders
EP1551823A1 (en) * 2002-10-08 2005-07-13 Merck Frosst Canada Inc. 4-amino-azepan-3-one compounds as cathepsin k inhibitors useful in the treatment of osteoporosis
US7297714B2 (en) * 2003-10-21 2007-11-20 Irm Llc Inhibitors of cathepsin S
US20100292298A1 (en) * 2006-02-21 2010-11-18 Agency For Science, Technology And Research Method and reagents for treating hepatic fibrosis and inflammation
US20100331545A1 (en) * 2007-10-24 2010-12-30 Nippon Chemiphar Co., Ltd. Regulator for signaling toll-like receptor, which comprises cathepsin inhibitor as active ingredient
CN104800196A (en) 2008-06-20 2015-07-29 诺华股份有限公司 Paediatric compositions for treating1 multiple sclerosis
LV15485B (en) * 2018-09-13 2020-06-20 Latvijas Organiskās Sintēzes Institūts Selenophene chromenone hydroxamic acids, their production and use in angiogenesis inhibition

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AU9050701A (en) 2001-12-03
AR032319A1 (en) 2003-11-05
CA2406829A1 (en) 2001-11-29
BR0108954A (en) 2006-05-09
KR20020089482A (en) 2002-11-29
WO2001089451A2 (en) 2001-11-29
EP1278502A2 (en) 2003-01-29
NO20025005L (en) 2002-12-06
CZ20023460A3 (en) 2004-03-17
CN1431904A (en) 2003-07-23
HUP0301781A2 (en) 2003-09-29
HK1053785A1 (en) 2003-11-07
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WO2001089451A3 (en) 2002-04-04
IL151087A0 (en) 2003-04-10

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