AR057110A1 - DERIVATIVES OF HETEROARIL-NITRILOS REPLACED WHICH ARE INHIBITORS OF PROTEASES - Google Patents
DERIVATIVES OF HETEROARIL-NITRILOS REPLACED WHICH ARE INHIBITORS OF PROTEASESInfo
- Publication number
- AR057110A1 AR057110A1 ARP060103809A ARP060103809A AR057110A1 AR 057110 A1 AR057110 A1 AR 057110A1 AR P060103809 A ARP060103809 A AR P060103809A AR P060103809 A ARP060103809 A AR P060103809A AR 057110 A1 AR057110 A1 AR 057110A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- 4alkyl
- alkylene
- phenyl
- nrerf
- Prior art date
Links
- 102000035195 Peptidases Human genes 0.000 title 1
- 108091005804 Peptidases Proteins 0.000 title 1
- 239000004365 Protease Substances 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000002947 alkylene group Chemical group 0.000 abstract 6
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 3
- 229920006395 saturated elastomer Polymers 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 125000001183 hydrocarbyl group Chemical group 0.000 abstract 2
- 125000002950 monocyclic group Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 101000749287 Clitocybe nebularis Clitocypin Proteins 0.000 abstract 1
- 101000767029 Clitocybe nebularis Clitocypin-1 Proteins 0.000 abstract 1
- 229940094664 Cysteine protease inhibitor Drugs 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 150000005829 chemical entities Chemical class 0.000 abstract 1
- 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- -1 heteroaryl nitriles Chemical class 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 201000004792 malaria Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 229930195734 saturated hydrocarbon Natural products 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 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
Una entidad química seleccionada de compuestos derivados de heteroaril-nitrilos sustituidos, que son inhibidores de proteasas, de formula (1) en donde: R4 representa halogeno; R2 representa i) -fenil-alquilen C1-3-X, -piridil-fenil-alquilen C1-3-X o fenil-alquilen C1-3-X-Rj, en donde fenilo está opcionalmente sustituido con un grupo seleccionado de halogeno o CF3; o ii) -Y-alquilen C1-3-X o -Y-alquilen C1-3-X-Rj; Y representa un grupo aromatico que comprende un anillo de 5 miembros que tiene uno a cuatro heteroátomos seleccionados de N, O y S, en donde el anillo está opcionalmente fusionado a un anillo fenilo; Rj representa Z, -alquilen C1-4-Z o -C(O)z; X y Z representan, de modo independiente; i) un grupo hidrocarbonado saturado monocíclico de 4 miembros que contiene un átomo de nitrogeno; ii) un grupo hidrocarbonado monocíclico saturado o parcialmente saturado de 5 miembros que contiene un átomo de nitrogeno; o iii) un grupo hidrocarbonado monocíclico saturado, parcialmente saturado o aromático de 6 miembros que contiene uno o dos átomos de nitrogeno y opcionalmente un átomo de oxígeno; en donde X y Z están opcionalmente sustituídos, de modo independiente, con a) un grupo seleccionado de: alquilo C1-4, alquil C1-4-OH, -alquil C1-4-Oalquil C1-4OH, OH, -alquil C1-4-C(O)Oalquilo C1-4, -C(O)Oalquilo C1-4, NRERF, -alquil C1-4-NRERF, -alquil C1-4-NRERF, -NC(O)alquilo C1-3, -NC(O)Oalquilo C1-4 y -C(O)NRERF y b) opcionalmente un grupo adicional que es alquilo C1-4; RE y RF representan, de modo independiente, hidrogeno o alquilo C1-4 o alquenilo C1-4; y sus derivados farmacéuticamente aceptables. Su uso para preparar un medicamento util para el tratamiento de una condicion susceptible de mediacion por un inhibidor de cisteína proteasa, tal como la malaria. Composicion farmacéutica que comprende estos compuestos y procedimientos para su preparacion.A chemical entity selected from compounds derived from substituted heteroaryl nitriles, which are protease inhibitors, of formula (1) wherein: R4 represents halogen; R2 represents i) -phenyl-C1-3-X alkylene, -pyridyl-phenyl-C1-3-X alkylene or phenyl-C1-3-X-Rj alkylene, wherein phenyl is optionally substituted with a group selected from halogen or CF3; or ii) -Y-C1-3-X alkylene or -Y-C1-3-X-Rj alkylene; Y represents an aromatic group comprising a 5-membered ring having one to four heteroatoms selected from N, O and S, wherein the ring is optionally fused to a phenyl ring; Rj represents Z, -C1-4-Z alkylene or -C (O) z; X and Z represent, independently; i) a 4-membered monocyclic saturated hydrocarbon group containing a nitrogen atom; ii) a 5-membered saturated or partially saturated monocyclic hydrocarbon group containing a nitrogen atom; or iii) a 6-membered saturated, partially saturated or aromatic monocyclic hydrocarbon group containing one or two nitrogen atoms and optionally an oxygen atom; wherein X and Z are optionally substituted, independently, with a) a group selected from: C1-4alkyl, C1-4alkyl-OH, -C1-4alkyl-C1-4alkyl, OH, -C1 -alkyl 4-C (O) C 1-4 alkyl, -C (O) C 1-4 alkyl, NRERF, -C 1-4 alkyl-NRERF, -C 1-4 alkyl-NRERF, -NC (O) C 1-3 alkyl, - NC (O) C1-4alkyl and -C (O) NRERF and b) optionally an additional group which is C1-4alkyl; RE and RF independently represent hydrogen or C1-4 alkyl or C1-4 alkenyl; and its pharmaceutically acceptable derivatives. Its use to prepare a drug useful for the treatment of a condition susceptible to mediation by a cysteine protease inhibitor, such as malaria. Pharmaceutical composition comprising these compounds and procedures for their preparation.
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 |
|---|---|
| AR057110A1 true AR057110A1 (en) | 2007-11-14 |
Family
ID=37770277
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060103810A AR055624A1 (en) | 2005-09-02 | 2006-08-31 | CHEMICAL SUBSTANCE SELECTED BETWEEN HETEROARIL - SUBSTITUTED NITRILS, ITS USE TO PREPARE A MEDICINAL PRODUCT, PHARMACEUTICAL COMPOSITIONS THAT INCLUDE IT AND PROCESSES TO PREPARE SUCH SUBSTANCES |
| ARP060103809A AR057110A1 (en) | 2005-09-02 | 2006-08-31 | DERIVATIVES OF HETEROARIL-NITRILOS REPLACED WHICH ARE INHIBITORS OF PROTEASES |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060103810A AR055624A1 (en) | 2005-09-02 | 2006-08-31 | CHEMICAL SUBSTANCE SELECTED BETWEEN HETEROARIL - SUBSTITUTED NITRILS, ITS USE TO PREPARE A MEDICINAL PRODUCT, PHARMACEUTICAL COMPOSITIONS THAT INCLUDE IT AND PROCESSES TO PREPARE SUCH SUBSTANCES |
Country Status (4)
| Country | Link |
|---|---|
| AR (2) | AR055624A1 (en) |
| PE (2) | PE20070332A1 (en) |
| TW (2) | TW200804352A (en) |
| WO (3) | WO2007025774A2 (en) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2030621A1 (en) * | 2007-08-21 | 2009-03-04 | Glaxo Group Limited | Novel substituted pyrimidines as cysteine protease inhibitors |
| AR063420A1 (en) * | 2006-10-30 | 2009-01-28 | Glaxo Group Ltd | DERIVATIVES OF 2-CIANO-4-PIRIMIDINIL SUBSTITUTED, PROCESS OF PREPARATION OF THE SAME, MEDICINES THAT CONTAIN THEM AND ITS USE FOR THE TREATMENT OF THE MALARIA. |
| CN101970007A (en) | 2007-06-08 | 2011-02-09 | 日本化学医药株式会社 | Therapeutic or prophylactic agent for cerebral aneurysm |
| US20100331545A1 (en) | 2007-10-24 | 2010-12-30 | Nippon Chemiphar Co., Ltd. | Regulator for signaling toll-like receptor, which comprises cathepsin inhibitor as active ingredient |
| 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 |
| US11299478B2 (en) | 2018-03-28 | 2022-04-12 | 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 TW TW095132088A patent/TW200804352A/en unknown
- 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/EP2006/008578 patent/WO2007025774A2/en not_active Ceased
- 2006-08-31 WO PCT/EP2006/008580 patent/WO2007025776A2/en not_active Ceased
- 2006-08-31 AR ARP060103809A patent/AR057110A1/en not_active Application Discontinuation
- 2006-08-31 WO PCT/EP2006/008579 patent/WO2007025775A2/en not_active Ceased
- 2006-08-31 TW TW095132087A patent/TW200804351A/en unknown
- 2006-08-31 PE PE2006001057A patent/PE20070612A1/en not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| WO2007025774A2 (en) | 2007-03-08 |
| WO2007025776A3 (en) | 2007-05-03 |
| TW200804351A (en) | 2008-01-16 |
| WO2007025774A3 (en) | 2007-04-26 |
| AR055624A1 (en) | 2007-08-29 |
| WO2007025775A2 (en) | 2007-03-08 |
| WO2007025776A2 (en) | 2007-03-08 |
| PE20070612A1 (en) | 2007-06-23 |
| PE20070332A1 (en) | 2007-05-11 |
| TW200804352A (en) | 2008-01-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |