PE20070332A1 - HETEROARYL-NITRILE COMPOUNDS SUBSTITUTED AS INHIBITORS OF CYSTEINE PROTEASES - Google Patents
HETEROARYL-NITRILE COMPOUNDS SUBSTITUTED AS INHIBITORS OF CYSTEINE PROTEASESInfo
- Publication number
- PE20070332A1 PE20070332A1 PE2006001056A PE2006001056A PE20070332A1 PE 20070332 A1 PE20070332 A1 PE 20070332A1 PE 2006001056 A PE2006001056 A PE 2006001056A PE 2006001056 A PE2006001056 A PE 2006001056A PE 20070332 A1 PE20070332 A1 PE 20070332A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- heteroaryl
- inhibitors
- alkylen
- phenyl
- Prior art date
Links
- 102000005927 Cysteine Proteases Human genes 0.000 title abstract 2
- 108010005843 Cysteine Proteases Proteins 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 201000004792 malaria Diseases 0.000 abstract 2
- 241000223960 Plasmodium falciparum Species 0.000 abstract 1
- 101000977048 Streptomyces cinnamonensis Uncharacterized protein in mutB 3'region Proteins 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- 150000002430 hydrocarbons Chemical group 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen(.) Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 244000045947 parasite Species 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 229930195734 saturated hydrocarbon Natural products 0.000 abstract 1
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
- A61P33/06—Antimalarials
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/10—Anthelmintics
- A61P33/12—Schistosomicides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Tropical Medicine & Parasitology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
SE REFIERE A COMPUESTOS HETEROARIL-NITRILOS SUSTITUIDOS DE FORMULA (I) EN DONDE R4 ES HALOGENO; R2 ES FENIL-ALQUILEN(C1-C3)-X, PIRIDIL-FENIL-ALQUILEN(C1-C3)-X O FENIL-ALQUILEN(C1-C3)-X-RJ; RJ ES Z -ALQUILEN(C1-C3)-Z O -C(O)Z; X E Y SON INDEPENDIENTEMENTE UN GRUPO HIDROCARBONADO SATURADO MONOCICLICO DE 6 MIEMBROS QUE CONTIENE 1 A 2 ATOMOS DE NITROGENO Y OPCIONALMENTE UN OXIGENO OPCIONALMENTE SUSTITUIDOS CON ALQUILO(C1-C4), OH, ALQUIL(C1-C4)OH, ENTRE OTROS. SON PREFERIDOS: N'-(5-BROMO-2-CIANO-4-PIRIMIDINIL)-N'-(CICLOPENTILMETIL)-4-[(4-METIL-1-PIPERAZINIL)METIL]BENZOHIDRAZIDA, N'-(5-BROMO-2-CIANO-4-PIRIMIDINIL)-N'-(CICLOPENTILMETIL)-4-[(4-HIDROXI-1-PIPERIDINIL)METIL]BENZOHIDRAZIDA, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA Y A UN PROCEDIMIENTO DE PREPARACION. DICHOS COMPUESTOS SON INHIBIDORES DE CISTEINA PROTEASA HALLADAS EN EL PARASITO DEL PALUDISMO PLASMODIUM FALCIPARUM POR LO QUE SON UTILES EN EL TRATAMIENTO DE MALARIAREFERS TO HETEROARYL-NITRILE COMPOUNDS SUBSTITUTED FOR FORMULA (I) WHERE R4 IS HALOGEN; R2 IS PHENYL-ALKYLEN (C1-C3) -X, PYRIDYL-PHENYL-ALKYLEN (C1-C3) -X OR PHENYL-ALKYLEN (C1-C3) -X-RJ; RJ IS Z -ALKYLENE (C1-C3) -Z OR -C (O) Z; X AND Y ARE INDEPENDENTLY A SATURATED SATURATED HYDROCARBON GROUP OF 6 MEMBERS CONTAINING 1 TO 2 NITROGEN ATOMS AND OPTIONALLY AN OPTIONALLY SUBSTITUTE OXYGEN WITH ALKYL (C1-C4), OH, ALKYL (C1-C4), OH, ALKYL (C1-C4), ALKYL (C1-C4). THE PREFERRED ARE: N '- (5-BROMO-2-CYANE-4-PYRIMIDINYL) -N' - (CYCLOPENTILMETIL) -4 - [(4-METHYL-1-PIPERAZINIL) METIL] BENZOHIDRAZIDA, N '- (5-BROMO -2-CYANE-4-PYRIMIDINYL) -N '- (CYCLOPENTILMETIL) -4 - [(4-HYDROXY-1-PIPERIDINYL) METHYL] BENZOHYDRAZIDE, AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION AND A PREPARATION PROCEDURE. SAID COMPOUNDS ARE INHIBITORS OF CYSTEINE PROTEASE FOUND IN THE PARASITE OF MALARIA PLASMODIUM FALCIPARUM SO THEY ARE USEFUL IN THE TREATMENT OF MALARIA
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP05381043 | 2005-09-02 | ||
| EP06110666 | 2006-03-03 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20070332A1 true PE20070332A1 (en) | 2007-05-11 |
Family
ID=37770277
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2006001057A PE20070612A1 (en) | 2005-09-02 | 2006-08-31 | NEW CYSTEINE PROTEASE INHIBITORS |
| PE2006001056A PE20070332A1 (en) | 2005-09-02 | 2006-08-31 | HETEROARYL-NITRILE COMPOUNDS SUBSTITUTED AS INHIBITORS OF CYSTEINE PROTEASES |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2006001057A PE20070612A1 (en) | 2005-09-02 | 2006-08-31 | NEW CYSTEINE PROTEASE INHIBITORS |
Country Status (4)
| Country | Link |
|---|---|
| AR (2) | AR057110A1 (en) |
| PE (2) | PE20070612A1 (en) |
| TW (2) | TW200804351A (en) |
| WO (3) | WO2007025776A2 (en) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20081471A1 (en) * | 2006-10-30 | 2008-12-31 | Glaxo Group Ltd | HETEROARYLNITRILE DERIVATIVES AS CYSTEINE PROTEASE INHIBITORS |
| EP2030621A1 (en) * | 2007-08-21 | 2009-03-04 | Glaxo Group Limited | Novel substituted pyrimidines as cysteine protease inhibitors |
| EP2168600A1 (en) | 2007-06-08 | 2010-03-31 | Nippon Chemiphar Co., Ltd. | Therapeutic or prophylactic agent for cerebral aneurysm |
| EP2216047A4 (en) | 2007-10-24 | 2011-12-28 | Nat Univ Corp Tokyo Med & Dent | REGULATOR FOR SIGNALING THE TOLL LIKE RECEPTOR WITH A CATHEPSIN INHIBITOR AS AN ACTIVE SUBSTANCE |
| DE102008063561A1 (en) * | 2008-12-18 | 2010-08-19 | Bayer Cropscience Ag | Hydrazides, process for their preparation and their use as herbicides and insecticides |
| CN102267964B (en) * | 2011-06-15 | 2014-06-18 | 浙江师范大学 | 3-hydroxy-2,3-dihydro-benzofuran derivatives as well as synthesis method and application thereof |
| EP3778576B1 (en) * | 2018-03-28 | 2024-04-17 | Hanlim Pharmaceutical Co., Ltd. | 2-cyanopyrimidin-4-yl carbamate or urea derivative or salt thereof, and pharmaceutical composition including same |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR036375A1 (en) * | 2001-08-30 | 2004-09-01 | Novartis Ag | PIRROLO [2,3-D] PIRIMIDINE -2- CARBONITRILE COMPOUNDS, A PROCESS FOR THEIR PREPARATION, A PHARMACEUTICAL COMPOSITION AND THE USE OF SUCH COMPOUNDS FOR THE PREPARATION OF MEDICINES |
-
2006
- 2006-08-31 AR ARP060103809A patent/AR057110A1/en not_active Application Discontinuation
- 2006-08-31 WO PCT/EP2006/008580 patent/WO2007025776A2/en active Application Filing
- 2006-08-31 PE PE2006001057A patent/PE20070612A1/en not_active Application Discontinuation
- 2006-08-31 TW TW095132087A patent/TW200804351A/en unknown
- 2006-08-31 TW TW095132088A patent/TW200804352A/en unknown
- 2006-08-31 WO PCT/EP2006/008578 patent/WO2007025774A2/en active Application Filing
- 2006-08-31 AR ARP060103810A patent/AR055624A1/en not_active Application Discontinuation
- 2006-08-31 PE PE2006001056A patent/PE20070332A1/en not_active Application Discontinuation
- 2006-08-31 WO PCT/EP2006/008579 patent/WO2007025775A2/en active Application Filing
Also Published As
| Publication number | Publication date |
|---|---|
| TW200804352A (en) | 2008-01-16 |
| AR055624A1 (en) | 2007-08-29 |
| WO2007025774A2 (en) | 2007-03-08 |
| PE20070612A1 (en) | 2007-06-23 |
| AR057110A1 (en) | 2007-11-14 |
| WO2007025775A2 (en) | 2007-03-08 |
| WO2007025774A3 (en) | 2007-04-26 |
| TW200804351A (en) | 2008-01-16 |
| WO2007025776A3 (en) | 2007-05-03 |
| WO2007025776A2 (en) | 2007-03-08 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FD | Application declared void or lapsed |