AR032319A1 - Metodo para inhibir la catepsina s, 4-amino-azepan-3-onas, metodos de tratamiento que comprenden su administracion y uso de las mismas en la fabricacion de medicamentos - Google Patents

Metodo para inhibir la catepsina s, 4-amino-azepan-3-onas, metodos de tratamiento que comprenden su administracion y uso de las mismas en la fabricacion de medicamentos

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Publication number
AR032319A1
AR032319A1 ARP010101786A ARP010101786A AR032319A1 AR 032319 A1 AR032319 A1 AR 032319A1 AR P010101786 A ARP010101786 A AR P010101786A AR P010101786 A ARP010101786 A AR P010101786A AR 032319 A1 AR032319 A1 AR 032319A1
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Argentina
Prior art keywords
alkyl
het
group
cycloalkyl
azepan
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ARP010101786A
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English (en)
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Smithkline Beecham Corp
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Publication of AR032319A1 publication Critical patent/AR032319A1/es

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    • 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
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    • 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
    • A—HUMAN NECESSITIES
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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

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Abstract

Un método para inhibir la Catepsina S que comprende administrarle a un animal que lo necesita, una cantidad eficaz de una de 4-amino-azepan-3-ona de Formula (1), en la que: R1 se selecciona del grupo formado por las formulas (2), (3) y (4); 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-, formulas(5), (6) y (7); 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; 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 se 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-alquilo 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. Además, se dan a conocer 4-amino-azepan-3-onas, métodos de tratamiento que comprenden su administracion, y uso de las mismas en la fabricacion de medicamentos para el tratamiento o prevencion de enfermedad autoinmune y para la prevencion de lesiones ateroscleroticas; inhibicion de una respuesta asmática, inhibicion de una respuesta alérgica, inhibicion de respuesta inmune contra un organo o tejido trasplantado, o inhibicion de la actividad de elastasa en ateroma.
ARP010101786A 2000-04-18 2001-04-17 Metodo para inhibir la catepsina s, 4-amino-azepan-3-onas, metodos de tratamiento que comprenden su administracion y uso de las mismas en la fabricacion de medicamentos AR032319A1 (es)

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

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AR032319A1 true AR032319A1 (es) 2003-11-05

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EP (1) EP1278502A4 (es)
JP (1) JP2004526662A (es)
KR (1) KR20020089482A (es)
CN (1) CN1431904A (es)
AR (1) AR032319A1 (es)
AU (1) AU9050701A (es)
BR (1) BR0108954A (es)
CA (1) CA2406829A1 (es)
CO (1) CO5280088A1 (es)
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MX (1) MXPA02010276A (es)
NO (1) NO20025005L (es)
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WO2002092563A2 (en) * 2001-05-17 2002-11-21 Smithkline Beecham Corporation Protease inhibitors
US20050030912A1 (en) * 2002-08-22 2005-02-10 Enikia L.L.C. Use of hybrid (HW/DSP/MCU/SW) architectures for powerline OFDM communication field
KR101095807B1 (ko) 2002-09-24 2011-12-21 노파르티스 아게 탈수초성 장애의 치료에 있어서의 스핑고신-1-포스페이트 수용체 아고니스트
US20060166966A1 (en) * 2002-10-08 2006-07-27 Cameron Black 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
WO2007097720A2 (en) * 2006-02-21 2007-08-30 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
CN102076335A (zh) 2008-06-20 2011-05-25 诺瓦提斯公司 用于治疗多发性硬化的儿科组合物
LV15485B (lv) * 2018-09-13 2020-06-20 Latvijas Organiskās Sintēzes Institūts Selenofēnhromenonu hidroksāmskābes, to izgatavošana un izmantošana angioģenēzes inhibīcijā

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TW494094B (en) * 1993-04-29 2002-07-11 Vertex Pharma Peptide analogs as irreversible interleukin-1β protease inhibitors and pharmaceutical compositions comprising the same
DZ2285A1 (fr) * 1996-08-08 2002-12-25 Smithkline Beecham Corp Inhibiteurs de protéase de la cystéine.
KR100630986B1 (ko) * 1998-12-23 2006-10-09 스미스클라인 비참 코포레이션 프로테아제 억제제
NZ520588A (en) * 2000-03-21 2004-06-25 Smithkline Beecham Corp Protease inhibitors
AU2001286983A1 (en) * 2000-09-01 2002-03-13 Smith Kline Beecham Corporation Method of treatment

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JP2004526662A (ja) 2004-09-02
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BR0108954A (pt) 2006-05-09
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PL366040A1 (en) 2005-01-24
KR20020089482A (ko) 2002-11-29
EP1278502A2 (en) 2003-01-29
WO2001089451A3 (en) 2002-04-04
CZ20023460A3 (en) 2004-03-17
HK1053785A1 (zh) 2003-11-07
CA2406829A1 (en) 2001-11-29
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NO20025005D0 (no) 2002-10-17
MXPA02010276A (es) 2003-04-25
EP1278502A4 (en) 2003-05-21
NO20025005L (no) 2002-12-06
CO5280088A1 (es) 2003-05-30
HUP0301781A2 (hu) 2003-09-29

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