HUP0402344A2 - Helyettesített 2-amino-cikloalkán-karboxamidok, felhasználásuk cisztein-proteáz-inhibitorként, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények - Google Patents

Helyettesített 2-amino-cikloalkán-karboxamidok, felhasználásuk cisztein-proteáz-inhibitorként, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények

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Publication number
HUP0402344A2
HUP0402344A2 HU0402344A HUP0402344A HUP0402344A2 HU P0402344 A2 HUP0402344 A2 HU P0402344A2 HU 0402344 A HU0402344 A HU 0402344A HU P0402344 A HUP0402344 A HU P0402344A HU P0402344 A2 HUP0402344 A2 HU P0402344A2
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Hungary
Prior art keywords
lower alkyl
pyridinyl
heteroaryl
hydrogen atom
alkyl group
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HU0402344A
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English (en)
Inventor
Thomas Gabriel
Nancy Elisabeth Krauss
Taraneh Mirzadegan
Wylie Solad Palmer
David Bernard Smith
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F. Hoffmann-La Roche Ag
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Publication date
Application filed by F. Hoffmann-La Roche Ag filed Critical F. Hoffmann-La Roche Ag
Publication of HUP0402344A2 publication Critical patent/HUP0402344A2/hu

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Abstract

A találmány (I) általános képletű vegyületekre[mely képletben R1jelentése heteroaril-csoport, -(CR'R'')mCO-Ra vagy S(O)p-Ra; ahol R'és R'' jelentése egymástól függetlenül hidrogénatom vagy kisszénatomszámú alkilcsoport; m értéke 0 vagy 1; p értéke 1 vagy 2; Rajelentése heteroaril-, heteroaril-kis szénatomszámú alkil- vagyheteroaril-kis szénatomszámú alkoxicsoport, mimellett a fentidefiníciókban levő heteroarilcsoport jelentése adott esetbenhelyettesített indolil-, piridil-, kinolinil-, izokinolinil-, N-oxo-kinolinil-, N-oxo-izokinolinil-, naftiridinil-, pirazolil-,indazolil-, furo[2,3-b]piridinil-, furo[2,3-c]piridinil-, furo[3,2-c]piridinil-, furo[3,2-b]piridinil-, 1H-pirrolo[3,2-b]piridinil-, 1H-pirrolo[2,3-b]piridinil-, 1H-pirrolo[3,2-c]piridinil-, 1H-pirrolo[2,3-c]piridinil-, IH-pirazolo[3,4-b]piridin, 1H-pirazolo[3,4-c]piridin-,1H-pirazolo[4,3-b]piridin, 1H-pirazolo[4,3-c]piridin, benzotiazolil-,azaindolil-, imidazo[2,1-b]benzotiazolil- vagy indolizinilcsoport; R2jelentése hidrogénatom vagy kis szénatomszámú alkilcsoport; R3jelentése hidrogénatom vagy kis szénatomszámú alkilcsoport; R4jelentése hidrogénatom vagy kis szénatomszámú alkilcsoport; R5jelentése hidrogénatom, kis szénatomszámú alkil-, heteroalkil-,cikloalkil-, cikloalkil-kis szénatomszámú alkil-, kis szénatomszámúalkoxi-karbonil-kis szénatomszámú alkil-, aril-, aralkil-, heteroaril-vagy heteroaril-kis szénatomszámú alkilcsoport; R6 jelentésehidrogénatom vagy kis szénatomszámú alkilcsoport; n értéke 1-3] ésgyógyászatilag alkalmas sóikra és/vagy gyógyászatilag alkalmasésztereikre vonatkozik. A találmány szerinti vegyületek cisztein-proteázokkal társult betegségek kezelésére alkalmazhatók pl. az alábbiindikációkban: osteoporosis, osteoarthritis, reumatoid arthritis,tumor metasztázis; glomerulonephritis, atheroszklerózis, miokardiálisinfarktus, angina pectoris, labilis angina pectoris, stroke,plakkrepedés, átmeneti iskémiás rohamok, amaurosis fugax, perifériásartériás elzáródásos betegség, angioplazia és stent behelyezés utánbekövetkező restenosis, hasi aortás aneurizma képződés, gyulladás,autoimmun betegség, malária, szemfenék szövet citopátia és légzésibetegség. A találmány kiterjed a vegyületek előállítására és ezekettartalmazó gyógyszerkészítményekre is. Ó
HU0402344A 2001-12-04 2002-11-25 Helyettesített 2-amino-cikloalkán-karboxamidok, felhasználásuk cisztein-proteáz-inhibitorként, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények HUP0402344A2 (hu)

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PCT/EP2002/013221 WO2003048123A1 (en) 2001-12-04 2002-11-25 Substituted 2-amino-cycloalkanecarboxamides and their use as cysteine protease inhibitors

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ATE357432T1 (de) 2007-04-15
US6747053B2 (en) 2004-06-08
RU2004120784A (ru) 2005-08-10
EP1453801A1 (en) 2004-09-08
PE20030723A1 (es) 2003-08-29
GT200200253A (es) 2003-07-03
CN1315806C (zh) 2007-05-16
EP1453801B1 (en) 2007-03-21
WO2003048123A1 (en) 2003-06-12
AR037683A1 (es) 2004-12-01
IL161992A0 (en) 2005-11-20
BR0214642A (pt) 2004-11-03
CA2467435A1 (en) 2003-06-12
ZA200404343B (en) 2006-07-26
JP2005517640A (ja) 2005-06-16
DE60219068T2 (de) 2007-12-13
PA8559701A1 (es) 2003-07-28
PL370766A1 (en) 2005-05-30
TW200303861A (en) 2003-09-16
DE60219068D1 (de) 2007-05-03
NO20042719L (no) 2004-06-28
US20030212097A1 (en) 2003-11-13
KR20050044660A (ko) 2005-05-12
AU2002352126A1 (en) 2003-06-17
CN1639119A (zh) 2005-07-13
MXPA04005263A (es) 2004-10-11
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