ATE387197T1 - Cyanoalkylamino-derivate als protease-hemmer - Google Patents

Cyanoalkylamino-derivate als protease-hemmer

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Publication number
ATE387197T1
ATE387197T1 AT02789611T AT02789611T ATE387197T1 AT E387197 T1 ATE387197 T1 AT E387197T1 AT 02789611 T AT02789611 T AT 02789611T AT 02789611 T AT02789611 T AT 02789611T AT E387197 T1 ATE387197 T1 AT E387197T1
Authority
AT
Austria
Prior art keywords
cyanoalkylamino
derivatives
protease inhibitors
compounds
cysteine protease
Prior art date
Application number
AT02789611T
Other languages
German (de)
English (en)
Inventor
Cameron Black
Sheldon Crane
Dana Davis
Eduardo Setti
Original Assignee
Merck Frosst Canada Ltd
Axys Pharm Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck Frosst Canada Ltd, Axys Pharm Inc filed Critical Merck Frosst Canada Ltd
Application granted granted Critical
Publication of ATE387197T1 publication Critical patent/ATE387197T1/de

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    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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AT02789611T 2001-11-13 2002-11-13 Cyanoalkylamino-derivate als protease-hemmer ATE387197T1 (de)

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Families Citing this family (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6759428B2 (en) 2001-12-04 2004-07-06 Roche Palo Alto Llc Indole nitriles
HUP0402344A2 (hu) 2001-12-04 2005-02-28 F. Hoffmann-La Roche Ag Helyettesített 2-amino-cikloalkán-karboxamidok, felhasználásuk cisztein-proteáz-inhibitorként, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények
CN100430052C (zh) * 2002-03-05 2008-11-05 默克弗罗斯特加拿大有限公司 组织蛋白酶半胱氨酸蛋白酶抑制剂
MXPA04011472A (es) 2002-05-22 2005-02-14 Amgen Inc Derivados de amino-piridina, piridina y piridazina para usarse como ligandos del receptor vaniloide para el tratamiento del dolor.
AR041191A1 (es) 2002-08-08 2005-05-04 Amgen Inc Ligandos del receptor vanilloide y su uso en tratamientos
EP1575576A2 (en) 2002-09-24 2005-09-21 Novartis AG Organic compounds
EP1761485A1 (en) * 2003-06-04 2007-03-14 Schering AG Amidino compounds as cysteine protease inhibitors
JP4690319B2 (ja) 2003-06-30 2011-06-01 メルク フロスト カナダ リミテツド カテプシンシステインプロテアーゼ阻害剤
CA2532948A1 (en) * 2003-07-21 2005-02-17 Novartis Ag Combinations of a cathepsin k inhibitor and a bisphophonate in the treatment of bone metastasis, tumor growth and tumor-induced bone loss
CN1839114A (zh) * 2003-08-21 2006-09-27 默克弗罗斯特加拿大有限公司 组织蛋白酶半胱氨酸蛋白酶抑制剂
PT1663958E (pt) * 2003-09-18 2015-06-01 Virobay Inc Compostos contendo haloalquilo como inibidores de protease de cisteína
AU2005212438A1 (en) 2004-02-11 2005-08-25 Amgen Inc. Vanilloid receptor ligands and their use in treatments
MY139645A (en) 2004-02-11 2009-10-30 Amgen Inc Vanilloid receptor ligands and their use in treatments
AR055283A1 (es) * 2004-11-23 2007-08-15 Merck Frosst Canada Ltd Inhibidores de cisteinproteasa de catepsina
EP1819667B1 (en) * 2004-12-02 2012-10-17 ViroBay, Inc. Sulfonamide compounds as cysteine protease inhibitors
US7301022B2 (en) 2005-02-15 2007-11-27 Amgen Inc. Vanilloid receptor ligands and their use in treatments
US7488848B2 (en) * 2005-03-21 2009-02-10 Virobay, Inc. Alpha ketoamide compounds as cysteine protease inhibitors
US7893093B2 (en) * 2005-03-22 2011-02-22 Virobay, Inc. Sulfonyl containing compounds as cysteine protease inhibitors
CN103172568A (zh) * 2005-07-06 2013-06-26 默克弗罗斯特加拿大有限公司 组织蛋白酶半胱氨酸蛋白酶抑制剂
EP2079683B1 (en) * 2006-10-04 2015-01-21 Virobay, Inc. Di-fluoro containing compounds as cysteine protease inhibitors
US7893112B2 (en) * 2006-10-04 2011-02-22 Virobay, Inc. Di-fluoro containing compounds as cysteine protease inhibitors
US8563573B2 (en) 2007-11-02 2013-10-22 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
EP2240491B1 (en) 2008-01-09 2015-07-15 Amura Therapeutics Limited TETRAHYDROFURO(2,3-b)PYRROL-3-ONE DERIVATIVES AS INHIBITORS OF CYSTEINE PROTEINASES
JP2011525189A (ja) 2008-06-20 2011-09-15 ノバルティス アーゲー 多発性硬化症を治療するための小児科の組成物
US8124764B2 (en) 2008-07-14 2012-02-28 Gilead Sciences, Inc. Fused heterocyclyc inhibitor compounds
WO2010009166A1 (en) 2008-07-14 2010-01-21 Gilead Colorado, Inc. Oxindolyl inhibitor compounds
CA2729909A1 (en) 2008-07-14 2010-01-21 Gilead Sciences, Inc. Imidazolyl pyrimidine inhibitor compounds
CN102123987A (zh) 2008-07-28 2011-07-13 吉里德科学公司 亚环烷基和亚杂环烷基组蛋白脱乙酰酶抑制剂化合物
US8283357B2 (en) 2009-06-08 2012-10-09 Gilead Sciences, Inc. Cycloalkylcarbamate benzamide aniline HDAC inhibitor compounds
KR20120031170A (ko) 2009-06-08 2012-03-30 길리애드 사이언시즈, 인코포레이티드 알카노일아미노 벤즈아미드 아닐린 hdac 저해제 화합물
US7893099B2 (en) * 2009-06-11 2011-02-22 Hoffman-La Roche Inc. Cyclopentane derivatives
US8324417B2 (en) * 2009-08-19 2012-12-04 Virobay, Inc. Process for the preparation of (S)-2-amino-5-cyclopropyl-4,4-difluoropentanoic acid and alkyl esters and acid salts thereof
US8802868B2 (en) 2010-03-25 2014-08-12 Vertex Pharmaceuticals Incorporated Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide
ES2608474T3 (es) 2010-04-22 2017-04-11 Vertex Pharmaceuticals Incorporated Proceso de producción de compuestos indol cycloalkylcarboxamido
JP6182593B2 (ja) 2012-04-20 2017-08-16 アドヴィーナス セラピューティクス リミテッド 置換ヘテロ二環化合物、組成物及び医薬並びにそれらの用途
US9617259B2 (en) * 2013-03-14 2017-04-11 Chdi Foundation, Inc. Histone deacetylase inhibitors and compositions and methods of use thereof
CN103275034B (zh) * 2013-04-16 2015-07-08 南京工业大学 一类小分子cathepsin D抑制剂的制备方法
ES2885181T3 (es) 2014-04-15 2021-12-13 Vertex Pharma Composiciones farmacéuticas para el tratamiento de enfermedades mediadas por el regulador de la conductancia transmembrana de fibrosis quística
KR20250133471A (ko) 2020-02-18 2025-09-05 길리애드 사이언시즈, 인코포레이티드 항바이러스 화합물
TWI883391B (zh) 2020-02-18 2025-05-11 美商基利科學股份有限公司 抗病毒化合物
TWI775313B (zh) 2020-02-18 2022-08-21 美商基利科學股份有限公司 抗病毒化合物
CA3216162A1 (en) 2021-04-16 2022-10-20 Gilead Sciences, Inc. Methods of preparing carbanucleosides using amides
AU2022328698B2 (en) 2021-08-18 2025-02-20 Gilead Sciences, Inc. Phospholipid compounds and methods of making and using the same

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0313847A3 (en) * 1987-10-01 1989-11-29 G.D. Searle & Co. Non-peptidyl alpha-succinamidoacyl aminodiols as anti-hypertensive agents
DE60021254T2 (de) 1999-03-15 2006-04-20 AXYS Pharmaceuticals, Inc., South San Francisco N-cyanomethylamide als protease inhibitoren

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CA2466115A1 (en) 2003-05-22
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