PE20020064A1 - Derivados nitrilo beta-aminoacidos como inhibidores de cistein proteasas - Google Patents
Derivados nitrilo beta-aminoacidos como inhibidores de cistein proteasasInfo
- Publication number
- PE20020064A1 PE20020064A1 PE2001000541A PE2001000541A PE20020064A1 PE 20020064 A1 PE20020064 A1 PE 20020064A1 PE 2001000541 A PE2001000541 A PE 2001000541A PE 2001000541 A PE2001000541 A PE 2001000541A PE 20020064 A1 PE20020064 A1 PE 20020064A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- cistein
- proteases
- beta
- amino acid
- Prior art date
Links
- -1 NITRILE BETA-AMINO ACID Chemical class 0.000 title abstract 3
- 102000035195 Peptidases Human genes 0.000 title abstract 2
- 108091005804 Peptidases Proteins 0.000 title abstract 2
- 239000004365 Protease Substances 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- 206010002388 Angina unstable Diseases 0.000 abstract 1
- 208000037260 Atherosclerotic Plaque Diseases 0.000 abstract 1
- 241000689227 Cora <basidiomycete fungus> Species 0.000 abstract 1
- 208000001132 Osteoporosis Diseases 0.000 abstract 1
- 208000007814 Unstable Angina Diseases 0.000 abstract 1
- UFIWDKQQDTVKDH-MGPQQGTHSA-N [(1r,2r)-2-[[(s)-cyano-(3-hydroxyphenyl)methyl]carbamoyl]cyclohexyl]carbamic acid Chemical compound OC(=O)N[C@@H]1CCCC[C@H]1C(=O)N[C@H](C#N)C1=CC=CC(O)=C1 UFIWDKQQDTVKDH-MGPQQGTHSA-N 0.000 abstract 1
- 150000001408 amides Chemical class 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 201000004332 intermediate coronary syndrome Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
Classifications
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- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
- C07C311/20—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
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- C—CHEMISTRY; METALLURGY
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- C07C255/00—Carboxylic acid nitriles
- C07C255/01—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms
- C07C255/24—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the same saturated acyclic carbon skeleton
- C07C255/29—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the same saturated acyclic carbon skeleton containing cyano groups and acylated amino groups bound to the carbon skeleton
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- C07C255/01—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms
- C07C255/32—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring
- C07C255/42—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being further bound to other hetero atoms
- C07C255/44—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being further bound to other hetero atoms at least one of the singly-bound nitrogen atoms being acylated
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- C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C271/06—Esters of carbamic acids
- C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
- C07C271/24—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a ring other than a six-membered aromatic ring
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- C—CHEMISTRY; METALLURGY
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- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
- C07C311/12—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings
- C07C311/13—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings the carbon skeleton containing six-membered aromatic rings
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- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/45—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
- C07C311/46—Y being a hydrogen or a carbon atom
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- C—CHEMISTRY; METALLURGY
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- C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
- C07C323/51—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
- C07C323/60—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
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- C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
- C07D307/82—Benzo [b] furans; Hydrogenated benzo [b] furans 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 carbon atoms of the hetero ring
- C07D307/84—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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- C07D317/46—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
- C07D317/48—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
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- C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom 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
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- C07C2601/14—The ring being saturated
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Abstract
SE REFIERE A DERIVADOS DE NITRILO BETA-AMINOACIDOS DE FORMULA I DONDE R1 ES H, ARILO, CORa, SO2Rb; Ra ES ALQUILO, ALCOXILO, CICLOALQUILO, ENTRE OTROS; Rb ES ARILO, ARIL-ALQUILO, HETEROARILO; R2, R3, R4 SON H, ALQUILO; R5 ES H, ALQUILO, CICLOALQUILO, ARILO; n ES 1-2. SON COMPUESTOS PREFERIDOS ESTER BENCILICO DEL ACIDO (1R,2R)-(2-{(S)-[CIANO-(3-HIDROXI-FENIL)-METIL]-CARBAMOIL}-CICLOHEXIL)CARBAMICO; [2-(CIANOMETIL-CARBAMOIL)-CICLOHEXIL]AMIDA DEL ACIDO CIS-5-METOXI-BENZOFURAN-2-CARBOXILICO, ENTRE OTROS; TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. LOS COMPUESTOS PUEDEN SER UTILES PARA EL TRATAMIENTO DE ENFERMEDADES QUE SE ASOCIAN CON CISTEIN PROTEASAS COMO OSTEOPOROSIS, ANGINA DE PECHO INESTABLE, RUPTURA DE LA PLACA ATEROSCLEROTICA
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP00112577 | 2000-06-14 |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20020064A1 true PE20020064A1 (es) | 2002-02-01 |
Family
ID=8168969
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2001000541A PE20020064A1 (es) | 2000-06-14 | 2001-06-08 | Derivados nitrilo beta-aminoacidos como inhibidores de cistein proteasas |
Country Status (29)
Country | Link |
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US (1) | US6462076B2 (es) |
EP (1) | EP1294679B1 (es) |
JP (1) | JP3872427B2 (es) |
KR (1) | KR20030029057A (es) |
CN (1) | CN1324006C (es) |
AR (1) | AR031594A1 (es) |
AT (1) | ATE304997T1 (es) |
AU (2) | AU2001266056B2 (es) |
BR (1) | BR0111733A (es) |
CA (1) | CA2410303C (es) |
DE (1) | DE60113533T2 (es) |
EC (1) | ECSP024383A (es) |
ES (1) | ES2248346T3 (es) |
HK (1) | HK1057539A1 (es) |
HR (1) | HRP20020963A2 (es) |
HU (1) | HUP0300896A3 (es) |
IL (1) | IL153166A0 (es) |
JO (1) | JO2234B1 (es) |
MA (1) | MA26913A1 (es) |
MX (1) | MXPA02012253A (es) |
NO (1) | NO20025823D0 (es) |
NZ (1) | NZ522587A (es) |
PE (1) | PE20020064A1 (es) |
PL (1) | PL359811A1 (es) |
RU (1) | RU2245871C2 (es) |
UY (1) | UY26769A1 (es) |
WO (1) | WO2001096285A1 (es) |
YU (1) | YU90802A (es) |
ZA (1) | ZA200209415B (es) |
Families Citing this family (21)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 (es) | 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 |
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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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