YU90802A - Derivati nitrila beta-aminokiselina - Google Patents

Derivati nitrila beta-aminokiselina

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Publication number
YU90802A
YU90802A YU90802A YUP90802A YU90802A YU 90802 A YU90802 A YU 90802A YU 90802 A YU90802 A YU 90802A YU P90802 A YUP90802 A YU P90802A YU 90802 A YU90802 A YU 90802A
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YU
Yugoslavia
Prior art keywords
pharmaceutically acceptable
angina pectoris
beta
disease
amino acid
Prior art date
Application number
YU90802A
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English (en)
Inventor
Tobias Gabriel
Michael Pech
Sarmiento Rosa M. Rodriguez
Original Assignee
F. Hoffmann-La Roche Ag.
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Filing date
Publication date
Application filed by F. Hoffmann-La Roche Ag. filed Critical F. Hoffmann-La Roche Ag.
Publication of YU90802A publication Critical patent/YU90802A/sh

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    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/20—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
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    • C07C255/29—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the same saturated acyclic carbon skeleton containing cyano groups and acylated amino groups bound to the carbon skeleton
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    • C07C255/32—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring
    • C07C255/42—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being further bound to other hetero atoms
    • C07C255/44—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being further bound to other hetero atoms at least one of the singly-bound nitrogen atoms being acylated
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    • C07C271/24—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a ring other than a six-membered aromatic ring
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    • C07C311/12—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings
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    • C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/45—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
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    • C07C323/60—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
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    • C07D307/82—Benzo [b] furans; Hydrogenated benzo [b] furans 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 carbon atoms of the hetero ring
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Abstract

Ovaj pronalazak se odnosi na jedinjenje formule (I) u kojoj su R1, R2, R3, R4, R5 i n definisani kao što je dato u opisu i zahtevima i na njegove farmaceutski prihvatljive soli i/ili farmaceutski prihvatljive estre. Ova jedinjenja su prikladna za terapiju bolesti koje su u vezi sa cisteinskim proteazama kao što su osteoporoza, osteoartritis, reumatoidni artritis, metastaza tumora, glomerulonefritis, ateroskleroza, miokardijalni infarkt, angina pektoris, nestabilna angina pektoris, moždani udar (šlog), prskanje krvnih pločica, prolazni ishemični napadi, amauroza fugaks (delimično slepilo), periferna arterijska okluzivna bolest, restenoza posle angioplastike i stavljanja stenta, formiranje aneurizma abdominalne aorte, zapaljenje, autoimuna bolest, malarija, citopatija tkiva očnog dna i respiratorna bolest.[The present invention relates to compound of formula (I) wherein R1, R2, R3, R4, R5 and n are as defined in the description and claims and pharmaceutically acceptable stalts and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment of diseases which are associated with cysteine proteases such as osteoporosis, osteoarthritis, rheumatoid arthritis, tumor metastasis, glomerulonephritis, atherosclerosis, myocardial infarction, angina pectoris, instable angina pectoris, stroke, plaque rupture, transient ischemic attacks, amaurosis fugax, peripheral arterial occlusive disease, restenosis after angioplasty and stent placement, abdominal aortic aneurysm formation, inflammation, autoimmune disease, malaria, ocular fundus tissue cytopathy and respiratory disease.
YU90802A 2000-06-14 2001-06-08 Derivati nitrila beta-aminokiselina YU90802A (sh)

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EP (1) EP1294679B1 (sh)
JP (1) JP3872427B2 (sh)
KR (1) KR20030029057A (sh)
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AU2004251794B2 (en) * 2003-06-30 2010-08-19 Merck Canada Inc. Cathepsin cysteine protease inhibitors
US20080125442A1 (en) * 2005-01-19 2008-05-29 Michael David Percival Cathepsin K Inhibitors and Atherosclerosis
CA2614070C (en) * 2005-07-06 2014-03-25 Merck Frosst Canada Ltd. Cathepsin cysteine protease inhibitors
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