AR067236A1 - Inhibidores de proteasas - Google Patents
Inhibidores de proteasasInfo
- Publication number
- AR067236A1 AR067236A1 ARP080101172A ARP080101172A AR067236A1 AR 067236 A1 AR067236 A1 AR 067236A1 AR P080101172 A ARP080101172 A AR P080101172A AR P080101172 A ARP080101172 A AR P080101172A AR 067236 A1 AR067236 A1 AR 067236A1
- Authority
- AR
- Argentina
- Prior art keywords
- formula
- alkyl
- methyl
- compound
- clause
- Prior art date
Links
- 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 title 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 5
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- 125000001153 fluoro group Chemical group F* 0.000 abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- UYFWXTAZASDCCA-BYPYZUCNSA-N (2s)-2-amino-4-fluoro-4-methylpentanoic acid Chemical compound CC(C)(F)C[C@H](N)C(O)=O UYFWXTAZASDCCA-BYPYZUCNSA-N 0.000 abstract 1
- WAMWSIDTKSNDCU-ZETCQYMHSA-N (2s)-2-azaniumyl-2-cyclohexylacetate Chemical compound OC(=O)[C@@H](N)C1CCCCC1 WAMWSIDTKSNDCU-ZETCQYMHSA-N 0.000 abstract 1
- WNXJIVFYUVYPPR-UHFFFAOYSA-N 1,3-dioxolane Chemical compound C1COCO1 WNXJIVFYUVYPPR-UHFFFAOYSA-N 0.000 abstract 1
- 102000004171 Cathepsin K Human genes 0.000 abstract 1
- 108090000625 Cathepsin K Proteins 0.000 abstract 1
- AGPKZVBTJJNPAG-WHFBIAKZSA-N L-isoleucine Chemical compound CC[C@H](C)[C@H](N)C(O)=O AGPKZVBTJJNPAG-WHFBIAKZSA-N 0.000 abstract 1
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 abstract 1
- ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Natural products CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 abstract 1
- 206010027476 Metastases Diseases 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- FYCWLJLGIAUCCL-DMTCNVIQSA-N O-methyl-L-threonine Chemical compound CO[C@H](C)[C@H](N)C(O)=O FYCWLJLGIAUCCL-DMTCNVIQSA-N 0.000 abstract 1
- 208000001132 Osteoporosis Diseases 0.000 abstract 1
- 230000004913 activation Effects 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 210000000988 bone and bone Anatomy 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- AGPKZVBTJJNPAG-UHFFFAOYSA-N isoleucine Natural products CCC(C)C(N)C(O)=O AGPKZVBTJJNPAG-UHFFFAOYSA-N 0.000 abstract 1
- 229960000310 isoleucine Drugs 0.000 abstract 1
- 230000009401 metastasis Effects 0.000 abstract 1
- 201000008482 osteoarthritis Diseases 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000000335 thiazolyl group Chemical group 0.000 abstract 1
Classifications
-
- 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
- C07D491/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Physical Education & Sports Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Compuestos de la formula (1) en donde R2 es la cadena lateral de leucina, isoleucina, ciclohexilglicina, O-metilo treonina, 4-fluoroleucina o 3-metoxivalina; R3 es H, metilo o fluoro; R4 es alquilo C1-6; E es un enlace o tiazolilo, opcionalmente sustituido con metilo o fluoro; n es 0 o 1; o una sal, N-oxido o hidrato aceptable para uso farmacéutico del mismo; que son de utilidad en el tratamiento de trastornos caracterizados por una expresion o activacion inapropiada de catepsina K, tales como osteoporosis, osteoartritis, artritis reumatoide o metástasis osea. Reivindicacion 30: Un compuesto, caracterizado porque es de la formula (2) en donde los grupos Rb definen un cetal, tal como el bis-metilcetal, o juntos definen un cetal cíclico, tal como 1,3-dioxolano, o un derivado N-protegido del mismo. Reivindicacion 31: Un compuesto de acuerdo con la cláusula 30 caracterizado porque es de formula (3). Reivindicacion 32: Un compuesto, caracterizado porque es de la formula (4) en donde R4 representa aIquiIo C1-6, o una sal o éster de alquilo inferior (por ejemplo alquilo C1-6) del mismo. Reivindicacion 33: Un compuesto de acuerdo con la cláusula 32, caracterizado porque es e formula (5).
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0705213A GB0705213D0 (en) | 2007-03-19 | 2007-03-19 | Protease inhibitors |
| GB0712182A GB0712182D0 (en) | 2007-06-25 | 2007-06-25 | Protease inhabitors |
| EP07123740 | 2007-12-20 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR067236A1 true AR067236A1 (es) | 2009-10-07 |
Family
ID=39472105
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080101172A AR067236A1 (es) | 2007-03-19 | 2008-03-19 | Inhibidores de proteasas |
Country Status (3)
| Country | Link |
|---|---|
| AR (1) | AR067236A1 (es) |
| TW (1) | TW200906392A (es) |
| WO (1) | WO2008114054A1 (es) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0817424D0 (en) | 2008-09-24 | 2008-10-29 | Medivir Ab | Protease inhibitors |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK1362052T3 (da) * | 2001-01-17 | 2007-07-09 | Amura Therapeutics Ltd | Inhibitorer af cruzipain og andre cysteinproteaser |
| BRPI0506719A (pt) * | 2004-01-08 | 2007-05-02 | Medivir Ab | composto, composição farmacêutica, e, uso de um composto |
-
2008
- 2008-03-18 WO PCT/GB2008/050193 patent/WO2008114054A1/en not_active Ceased
- 2008-03-19 TW TW097109638A patent/TW200906392A/zh unknown
- 2008-03-19 AR ARP080101172A patent/AR067236A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| TW200906392A (en) | 2009-02-16 |
| WO2008114054A1 (en) | 2008-09-25 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |