PE20060647A1 - Compuestos de 2-ciano-pirimidina como inhibidores de catepsina-s - Google Patents
Compuestos de 2-ciano-pirimidina como inhibidores de catepsina-sInfo
- Publication number
- PE20060647A1 PE20060647A1 PE2005000946A PE2005000946A PE20060647A1 PE 20060647 A1 PE20060647 A1 PE 20060647A1 PE 2005000946 A PE2005000946 A PE 2005000946A PE 2005000946 A PE2005000946 A PE 2005000946A PE 20060647 A1 PE20060647 A1 PE 20060647A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- catepsin
- cyano
- inhibitors
- cyane
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- IIHQNAXFIODVDU-UHFFFAOYSA-N pyrimidine-2-carbonitrile Chemical class N#CC1=NC=CC=N1 IIHQNAXFIODVDU-UHFFFAOYSA-N 0.000 title abstract 2
- -1 AMINO Chemical group 0.000 abstract 3
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical group 0.000 abstract 2
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical group [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 208000004296 neuralgia Diseases 0.000 abstract 1
- 208000021722 neuropathic pain Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 150000003254 radicals Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/34—One oxygen atom
- C07D239/36—One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- 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
- C07D413/12—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 linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
SE REFIERE A DERIVADOS DE 2-CIANO-PIRIMIDINA, DE FORMULA (I), EN DONDE R1 ES UN RADICAL DE FORMULA (Ia); A, E Y G SON INDEPENDIENTEMENTE O, S O CH2, CON LA CONDICION DE QUE AL MENOS UNO DE A Y E ES CH2; T ES O, S O UN ENLACE, SI G ES CH2, Y T ES UN ENLACE SI G ES O O S; Ra, Rb, Y Rc SON INDEPENDIENTEMENTE H O ALQUILO; s Y p SON DE 0 A 2; t ES DE 1 A 4; R2 ES HALOGENO, ALQUILO, ARILO, -C(O)-NR4R5, -N(R9)-SO2-R10, ENTRE OTROS; R4 ES ALQUILO(C1-C7) OPCIONALMENTE SUSTITUIDO CON AMINO MONO O DI-SUSTITUIDO, 1-AZA-CICLOALQUILO, PIRROLIDINO, PIPERAZINILO, ENTRE OTROS O ES FENILO, N-ALQUILO, ENTRE OTROS; R5 ES H O ALQUILO; R3 ES H, HALOGENO, Y-R6, NR7R8; X ES HN, ALQUILO(C1-C4)-N, ENTRE OTROS. SON PREFERIDOS: (2-MORFOLIN-4-IL-1-FENIL-ETIL)-AMIDA DEL ACIDO 2-CIANO-4-(CICLOHEXILMETIL-AMINO)-PIRIMIDIN-5-CARBOXILICO, [5-(1-METIL-PIPERIDIN-4-ILOXI)-BIFENIL-2-IL]-AMIDA DEL ACIDO 2-CIANO-4-[(ESPIRO-[2.5]-OCT-6-ILMETIL)-AMINO]-PIRIMIDIN-5-CARBOXILICO, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCESO DE ELABORACION Y COMPOSICIONES FARMACEUTICAS. ESTOS COMPUESTOS SON INHIBIDORES DE LA CATEPSINA-S, POR LO QUE SON UTILES EN EL TRATAMIENTO Y PREVENCION DEL DOLOR NEUROPATICO
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0418353.9A GB0418353D0 (en) | 2004-08-17 | 2004-08-17 | Organic compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20060647A1 true PE20060647A1 (es) | 2006-08-11 |
Family
ID=33042203
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2005000946A PE20060647A1 (es) | 2004-08-17 | 2005-08-15 | Compuestos de 2-ciano-pirimidina como inhibidores de catepsina-s |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US7704996B2 (es) |
| EP (1) | EP1781623A1 (es) |
| JP (1) | JP2008509959A (es) |
| KR (1) | KR20070036183A (es) |
| CN (2) | CN101035768A (es) |
| AR (1) | AR050786A1 (es) |
| AU (1) | AU2005274319A1 (es) |
| BR (1) | BRPI0514383A (es) |
| CA (1) | CA2575826A1 (es) |
| GB (1) | GB0418353D0 (es) |
| GT (1) | GT200500220A (es) |
| MX (1) | MX2007001952A (es) |
| PE (1) | PE20060647A1 (es) |
| RU (1) | RU2007109650A (es) |
| TW (1) | TW200621727A (es) |
| WO (1) | WO2006018284A1 (es) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG170725A1 (en) * | 2006-02-21 | 2011-05-30 | Agency Science Tech & Res | Method and reagents for treating hepatic fibrosis and inflammation |
| JP5441705B2 (ja) * | 2007-10-15 | 2014-03-12 | 武田薬品工業株式会社 | アミド化合物およびその用途 |
| WO2010065704A1 (en) * | 2008-12-04 | 2010-06-10 | Glaxo Group Limited | Method for preparing a spiroindoline and a precursor thereof |
| TWI402072B (zh) * | 2010-10-19 | 2013-07-21 | Lilly Co Eli | 組織蛋白酶ｓ抑制劑化合物 |
| US12350260B2 (en) | 2019-04-05 | 2025-07-08 | Universite De Bretagne Occidentale | Protease-activated receptor-2 inhibitors for the treatment of sensory neuropathy induced by a marine neurotoxic poisoning |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE0201976D0 (sv) * | 2002-06-24 | 2002-06-24 | Astrazeneca Ab | Novel compounds |
| GB0220187D0 (en) * | 2002-08-30 | 2002-10-09 | Novartis Ag | Organic compounds |
-
2004
- 2004-08-17 GB GBGB0418353.9A patent/GB0418353D0/en not_active Ceased
-
2005
- 2005-08-15 PE PE2005000946A patent/PE20060647A1/es not_active Application Discontinuation
- 2005-08-16 CN CNA2005800344018A patent/CN101035768A/zh active Pending
- 2005-08-16 EP EP05782460A patent/EP1781623A1/en not_active Withdrawn
- 2005-08-16 US US11/573,451 patent/US7704996B2/en not_active Expired - Fee Related
- 2005-08-16 RU RU2007109650/04A patent/RU2007109650A/ru not_active Application Discontinuation
- 2005-08-16 WO PCT/EP2005/008896 patent/WO2006018284A1/en not_active Ceased
- 2005-08-16 TW TW094127954A patent/TW200621727A/zh unknown
- 2005-08-16 CA CA002575826A patent/CA2575826A1/en not_active Abandoned
- 2005-08-16 MX MX2007001952A patent/MX2007001952A/es not_active Application Discontinuation
- 2005-08-16 JP JP2007526382A patent/JP2008509959A/ja active Pending
- 2005-08-16 AU AU2005274319A patent/AU2005274319A1/en not_active Abandoned
- 2005-08-16 KR KR1020077003902A patent/KR20070036183A/ko not_active Ceased
- 2005-08-16 GT GT200500220A patent/GT200500220A/es unknown
- 2005-08-16 BR BRPI0514383-7A patent/BRPI0514383A/pt not_active IP Right Cessation
- 2005-08-16 CN CN200910179114A patent/CN101671310A/zh active Pending
- 2005-08-19 AR ARP050103494A patent/AR050786A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2008509959A (ja) | 2008-04-03 |
| RU2007109650A (ru) | 2008-09-27 |
| US7704996B2 (en) | 2010-04-27 |
| EP1781623A1 (en) | 2007-05-09 |
| AU2005274319A1 (en) | 2006-02-23 |
| CN101671310A (zh) | 2010-03-17 |
| KR20070036183A (ko) | 2007-04-02 |
| BRPI0514383A (pt) | 2008-06-10 |
| CA2575826A1 (en) | 2006-02-23 |
| AR050786A1 (es) | 2006-11-22 |
| CN101035768A (zh) | 2007-09-12 |
| TW200621727A (en) | 2006-07-01 |
| US20090048230A1 (en) | 2009-02-19 |
| MX2007001952A (es) | 2007-05-09 |
| GT200500220A (es) | 2006-03-29 |
| WO2006018284A1 (en) | 2006-02-23 |
| GB0418353D0 (en) | 2004-09-22 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |