ZA200603183B - Novel keto-oxadiazole derivatives as cathepsin inhibitors - Google Patents
Novel keto-oxadiazole derivatives as cathepsin inhibitors Download PDFInfo
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- ZA200603183B ZA200603183B ZA200603183A ZA200603183A ZA200603183B ZA 200603183 B ZA200603183 B ZA 200603183B ZA 200603183 A ZA200603183 A ZA 200603183A ZA 200603183 A ZA200603183 A ZA 200603183A ZA 200603183 B ZA200603183 B ZA 200603183B
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- ZA
- South Africa
- Prior art keywords
- alkyl
- amide
- morpholine
- carboxylic acid
- carbonyl
- Prior art date
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- 239000003112 inhibitor Substances 0.000 title claims description 12
- 102000005600 Cathepsins Human genes 0.000 title claims description 9
- 108010084457 Cathepsins Proteins 0.000 title claims description 9
- ZVTQYRVARPYRRE-UHFFFAOYSA-N oxadiazol-4-one Chemical class O=C1CON=N1 ZVTQYRVARPYRRE-UHFFFAOYSA-N 0.000 title description 2
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- STUHQDIOZQUPGP-UHFFFAOYSA-N morpholin-4-ium-4-carboxylate Chemical compound OC(=O)N1CCOCC1 STUHQDIOZQUPGP-UHFFFAOYSA-N 0.000 claims description 55
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- 150000003839 salts Chemical class 0.000 claims description 18
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- 230000000694 effects Effects 0.000 claims description 13
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Classifications
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- C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
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- C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
- C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
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- C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
- C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
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- C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
- C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
- C07D271/107—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles with two aryl or substituted aryl radicals attached in positions 2 and 5
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- C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
- C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
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- C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
- C07D295/20—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
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- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
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- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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| EP1819667B1 (en) | 2004-12-02 | 2012-10-17 | ViroBay, Inc. | Sulfonamide compounds as cysteine protease inhibitors |
| EP1865940B1 (en) | 2005-03-21 | 2013-02-13 | Virobay, Inc. | Alpha ketoamide compounds as cysteine protease inhibitors |
| JP5215167B2 (ja) | 2005-03-22 | 2013-06-19 | ビロベイ,インコーポレイティド | システインプロテアーゼ阻害剤としてのスルホニル基含有化合物 |
| WO2007137738A1 (de) * | 2006-06-01 | 2007-12-06 | Sanofi-Aventis | Spiro-cyclische nitrile als protease-inhibitoren |
| US7893112B2 (en) | 2006-10-04 | 2011-02-22 | Virobay, Inc. | Di-fluoro containing compounds as cysteine protease inhibitors |
| CA2664878A1 (en) * | 2006-10-04 | 2008-04-10 | Virobay, Inc. | Di-fluoro containing compounds as cysteine protease inhibitors |
| MY162041A (en) | 2007-02-28 | 2017-05-31 | Sanofi Aventis | Imaging probes |
| BRPI0822420A2 (pt) * | 2008-04-01 | 2014-10-07 | Virobay Inc | Composto, composição farmaceutica, e, métodos para tratar uma doença em uma animal e para tratar um paciente que passa por uma tarepia. |
| US7741327B2 (en) | 2008-04-16 | 2010-06-22 | Hoffmann-La Roche Inc. | Pyrrolidinone glucokinase activators |
| CN102264710B (zh) * | 2008-12-19 | 2014-11-05 | 美迪维尔英国有限公司 | 半胱氨酸蛋白酶抑制剂 |
| US7893099B2 (en) * | 2009-06-11 | 2011-02-22 | Hoffman-La Roche Inc. | Cyclopentane derivatives |
| US20110021570A1 (en) | 2009-07-23 | 2011-01-27 | Nancy-Ellen Haynes | Pyridone glucokinase activators |
| 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 |
| US8895497B2 (en) | 2009-12-04 | 2014-11-25 | Dcb-Usa, Llc | Cathepsin S inhibitors |
| US8500766B2 (en) * | 2009-12-18 | 2013-08-06 | Colgate-Palmolive Company | Oral care implement multiple soft tissue cleaner components |
| US8178689B2 (en) | 2010-06-17 | 2012-05-15 | Hoffman-La Roche Inc. | Tricyclic compounds |
| AU2013305759C1 (en) | 2012-08-23 | 2018-01-18 | Janssen Biopharma, Inc. | Compounds for the treatment of paramoxyvirus viral infections |
| WO2020201572A1 (en) | 2019-04-05 | 2020-10-08 | Université De Bretagne Occidentale | Protease-activated receptor-2 inhibitors for the treatment of sensory neuropathy induced by a marine neurotoxic poisoning |
Family Cites Families (20)
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| FR2381023A1 (fr) | 1977-02-18 | 1978-09-15 | Delalande Sa | Nouveaux oligopeptides trifluoromethyles derives de la l-alanine, leur procede de preparation et leur application en therapeutique |
| FR2605009B1 (fr) * | 1986-06-13 | 1989-06-09 | Ayi Ayicoue | Nouveaux peptides contenant un acide a-amine b-monofluore ou b,b-difluore dans leur structure dont des enkephalines et derives d'enkephalines |
| US5223485A (en) | 1989-01-31 | 1993-06-29 | Abbott Laboratories | Anaphylatoxin-receptor ligands |
| EP0456758A4 (en) * | 1989-01-31 | 1992-07-08 | Abbott Laboratories | Anaphylatoxin-receptor ligands |
| JPH0449298A (ja) * | 1990-06-19 | 1992-02-18 | Univ New York State | 新規なエンケファリン誘導体および鎮痛剤 |
| JP3605158B2 (ja) * | 1994-12-09 | 2004-12-22 | 塩野義製薬株式会社 | Hivプロテアーゼ阻害剤 |
| DE19642591A1 (de) * | 1996-10-15 | 1998-04-16 | Basf Ag | Neue Piperidin-Ketocarbonsäure-Derivate, deren Herstellung und Anwendung |
| ATE421954T1 (de) * | 1997-02-26 | 2009-02-15 | Pfizer | Heteroaryl-hexansäureamid-derivate, ihre herstellung und ihre verwendung als selektive inhibitoren der bindung von mip-1-alpha an seinen ccr1 rezeptor |
| ID20812A (id) * | 1997-07-09 | 1999-03-11 | Takeda Chemical Industries Ltd | Senyawa polyol, produk dan penggunaannya |
| KR20010041905A (ko) * | 1998-03-16 | 2001-05-25 | 시토비아 인크. | 디펩티드 카스파제 억제제 및 이의 용도 |
| GB9812523D0 (en) * | 1998-06-10 | 1998-08-05 | Angeletti P Ist Richerche Bio | Peptide inhibitors of hepatitis c virus ns3 protease |
| TW200404789A (en) | 1999-03-15 | 2004-04-01 | Axys Pharm Inc | Novel compounds and compositions as protease inhibitors |
| HRP20010738B1 (en) | 1999-03-15 | 2005-02-28 | Axys Pharmaceuticals | N-cyanomethyl amides as protease inhibitors |
| EP1372655B1 (en) | 2001-03-02 | 2008-10-01 | Merck Frosst Canada Ltd. | Cathepsin cysteine protease inhibitors |
| GB0107924D0 (en) | 2001-03-29 | 2001-05-23 | Angeletti P Ist Richerche Bio | Inhibitor of hepatitis C virus NS3 protease |
| KR20040015725A (ko) | 2001-06-01 | 2004-02-19 | 액시스 파마슈티컬스 인코포레이티드 | 카텝신 s 억제제로서의 화합물 및 약제학적 조성물 |
| US6982263B2 (en) * | 2001-06-08 | 2006-01-03 | Boehringer Ingelheim Pharmaceuticals, Inc. | Nitriles useful as reversible inhibitors of cysteine proteases |
| WO2003075836A2 (en) | 2002-03-05 | 2003-09-18 | Merck Frosst Canada & Co. | Cathepsin cysteine protease inhibitors |
| WO2003087069A2 (en) * | 2002-04-09 | 2003-10-23 | Eli Lilly And Company | Dipeptidic growth hormone secretagogues |
| WO2003097617A1 (en) * | 2002-05-14 | 2003-11-27 | Axys Pharmaceuticals, Inc. | Cysteine protease inhibitors |
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2004
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- 2004-10-22 BR BRPI0415826-1A patent/BRPI0415826A/pt not_active Application Discontinuation
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Also Published As
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| CA2547591A1 (en) | 2005-05-06 |
| CA2547591C (en) | 2010-08-17 |
| AU2004284089B2 (en) | 2009-11-26 |
| NO20062150L (no) | 2006-05-12 |
| NZ546504A (en) | 2009-01-31 |
| AU2004284089A1 (en) | 2005-05-06 |
| WO2005040142A1 (en) | 2005-05-06 |
| RU2006117788A (ru) | 2007-11-27 |
| US7482448B2 (en) | 2009-01-27 |
| RS20060280A (sr) | 2008-08-07 |
| HK1101871A1 (zh) | 2007-10-26 |
| BRPI0415826A (pt) | 2007-01-02 |
| WO2005040142B1 (en) | 2005-07-14 |
| MA28170A1 (fr) | 2006-09-01 |
| IL175106A0 (en) | 2006-09-05 |
| US20060189657A1 (en) | 2006-08-24 |
| MXPA06004422A (es) | 2006-07-03 |
| WO2005040142A9 (en) | 2005-06-09 |
| JP2007509175A (ja) | 2007-04-12 |
| JP4769192B2 (ja) | 2011-09-07 |
| CN1898219A (zh) | 2007-01-17 |
| KR20070008517A (ko) | 2007-01-17 |
| CN100543017C (zh) | 2009-09-23 |
| EP1682524A1 (en) | 2006-07-26 |
| RU2346943C2 (ru) | 2009-02-20 |
| MEP39608A (en) | 2011-02-10 |
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