HUP0300896A2 - Beta-aminosav-nitril-származékok, eljárás az előállításukra, és ezeket tartalmazó gyógyszerkészítmények - Google Patents

Beta-aminosav-nitril-származékok, eljárás az előállításukra, és ezeket tartalmazó gyógyszerkészítmények

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Publication number
HUP0300896A2
HUP0300896A2 HU0300896A HUP0300896A HUP0300896A2 HU P0300896 A2 HUP0300896 A2 HU P0300896A2 HU 0300896 A HU0300896 A HU 0300896A HU P0300896 A HUP0300896 A HU P0300896A HU P0300896 A2 HUP0300896 A2 HU P0300896A2
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Hungary
Prior art keywords
lower alkyl
aryl
cycloalkyl
hydrogen atom
heteroaryl
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Application number
HU0300896A
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English (en)
Inventor
Tobias Gabriel
Michael Pech
Sarmiento Rosa Maria Rodriguez
Original Assignee
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 HUP0300896A2 publication Critical patent/HUP0300896A2/hu
Publication of HUP0300896A3 publication Critical patent/HUP0300896A3/hu

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Abstract

A találmány (I) általános képletű vegyületekre[mely képletben Rljelentése hidrogénatom, arilcsoport, -CO-Ra vagy -SO2-Rb, ahol Rajelentése kis szénatomszámú alkil-, kis szénatomszámú alkoxi-,cikloalkil-, cikloalkil-(kis szénatomszámú alkil)-, cikloalkil-(kisszénatomszámú alkoxi)-, cikloalkoxi-, aril-, ariloxi-, aril-(kisszénatomszámú alkil)-, aril-(kis szénatomszámú alkoxi)-, ariloxi-(kisszénatomszámnú alkil)-, aril-S-(kis szénatomszámú alkil)-, aril-(kisszénatomszámú alkenil)-, heteroaril-, heteroaril-(kis szénatomszámúalkil)- vagy heteroaril-(kis szénatomszámú alkoxi)-csoport; Rbjelentése aril-, aril-(kis szénatomszámú alkil)- vagy heteroaril-csoport; R2 jelentése hidrogénatom vagy kis szénatomszámúalkilcsoport; R3 jelentése hidrogénatom vagy kis szénatomszámúalkilcsoport; R4 jelentése hidrogénatom vagy kis szénatomszámúalkilcsoport; R5 jelentése hidrogénatom, kis szénatomszámú alkil-,cikloalkil- vagy arilcsoport; n értéke 1 vagy 2] és gyógyászatilagalkalmas sóikra és/vagy gyógyászatilag alkalmas észtereikrevonatkozik. A találmány szerinti vegyületek cisztein-proteázokkaltársult betegségek, pl. az alábbi betegségek kezelésére alkalmazhatók:osteoporosis, osteoarthritis, rheumatoid arthritis; tumormetasztázis,glomerulonephritis, atheroszklerozis, miokardiális infarktus, anginapectoris, labilis angina pectoris, stroke, plaquerepedés, átmenetiiskémás rohamok, amaurosis fugax, perifériás artériális elzáródásosbetegség, angioplasztika és stent áthelyezés utáni restenosis, hasiaortás aneurizmusképződés, gyulladás, autoimmun betegség, malária,szemfenékszövet citopátia és légzési betegség. A találmány kiterjed avegyületek előállítási eljárására és ezeket tartalmazógyógyszerkészítményekre is. Ó
HU0300896A 2000-06-14 2001-06-08 Beta-amino acid nitrile derivatives, process for their preparation and pharmaceutical compositions containing them HUP0300896A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP00112577 2000-06-14
PCT/EP2001/006541 WO2001096285A1 (en) 2000-06-14 2001-06-08 Beta-amino acid nitrile derivatives

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HUP0300896A2 true HUP0300896A2 (hu) 2003-07-28
HUP0300896A3 HUP0300896A3 (en) 2004-09-28

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HU (1) HUP0300896A3 (hu)
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WO (1) WO2001096285A1 (hu)
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GB9916575D0 (en) * 1999-07-15 1999-09-15 Cambridge Combinatorial Ltd Solid phase nitrile synthesis
EP1372655B1 (en) * 2001-03-02 2008-10-01 Merck Frosst Canada Ltd. Cathepsin cysteine protease inhibitors
EP1427696A1 (en) * 2001-09-13 2004-06-16 F. Hoffmann-La Roche Ag Ccr-3 receptor antagonists v
AU2002352126A1 (en) * 2001-12-04 2003-06-17 F. Hoffmann-La Roche Ag Substituted 2-amino-cycloalkanecarboxamides and their use as cysteine protease inhibitors
US6759428B2 (en) * 2001-12-04 2004-07-06 Roche Palo Alto Llc Indole nitriles
AU2003282983A1 (en) * 2002-10-23 2004-05-13 Bristol-Myers Squibb Company Glycinenitrile-based inhibitors of dipeptidyl peptidase iv and methods
EP1633701A1 (en) * 2003-06-02 2006-03-15 F.Hoffmann-La Roche Ag Benzamide nitrile derivatives
WO2005000793A1 (ja) * 2003-06-26 2005-01-06 Taisho Pharmaceutical Co., Ltd. ２位置換シクロアルキルカルボン酸誘導体
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
JP5587790B2 (ja) 2008-01-09 2014-09-10 アミュラ セラピューティクス リミティド 化合物
US7893099B2 (en) * 2009-06-11 2011-02-22 Hoffman-La Roche Inc. Cyclopentane derivatives
KR20140049019A (ko) 2011-07-26 2014-04-24 사노피 ３―헤테로아로일아미노―프로피온산 유도체 및 이의 약제로서의 용도
CN103086923B (zh) * 2013-01-21 2014-04-23 吉林大学 肼腈类组织蛋白酶k抑制剂及其在治疗骨质疏松症方面的应用
CA2923272A1 (en) * 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Cathepsin cysteine protease inhibitors
NO2699580T3 (hu) 2014-01-24 2018-02-24
CN105837479B (zh) * 2016-04-05 2017-10-27 吉林大学 肼腈类组织蛋白酶k抑制剂及其在制备治疗骨关节炎药物中的应用
CN113045491A (zh) * 2019-12-26 2021-06-29 罗欣药业(上海)有限公司 一种仑伐替尼及中间体的制备方法
CN115996923A (zh) 2020-08-26 2023-04-21 四川海思科制药有限公司 一种作为二肽基肽酶1抑制剂的腈衍生物及其用途
JP2023551488A (ja) 2020-12-04 2023-12-08 瑞石生物医薬有限公司 カテプシンｃの小分子阻害剤及びその医薬的使用

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU177576B (en) 1975-06-02 1981-11-28 Chinoin Gyogyszer Es Vegyeszet Process for preparing 2-amino-cyclohexane carboxylic acid,its amides and similar compounds
IT1283467B1 (it) 1996-07-19 1998-04-21 Menarini Farma Ind Derivati di cicloalcani 1,2 sostituiti come inibitori della trombina, procedimento per la loro preparazione e loro impiego in formulazioni
CN1282319A (zh) * 1997-10-09 2001-01-31 小野药品工业株式会社 氨基丁酸衍生物
AU751669B2 (en) 1997-11-05 2002-08-22 Novartis Ag Dipeptide nitriles

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