Tripeptides and tripeptide derivatives for the treatment of...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

Reexamination Certificate

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

C530S331000

Reexamination Certificate

active

07129213

ABSTRACT:
The invention relates to the use of specific tripeptides for the treatment of neurodegenerative diseases, and to pharmaceutical compositions comprising the tripeptides. The tripeptide derivatives satisfy the following formula (I): wherein X represents OH, (C1-5) alkoxy, NH2, NH—C1-5-alkyl, N(C1-5alkyl)2; R1is a residue derived from one of the amino acids Phe, Tyr, Trp, Pro, which each may be optionally substituted with one or more (C1-5)alkoxy groups, (C1-5)alkyl groups or halogen atoms, as well as Ala, Val, Leu or Ile; R2is a residue derived from one of the amino acids Gly, Ala, Ile, Val, Ser, Thr, Leu and Pro; Y1and Y2independently from each other represent H or (C1-5)alkyl; R3and R4independently from each other represent H, OH, (C1-5)alkyl or (C1-5)alkoxy, provided that R3and R4are not both OH or (C1-5)alkoxy; and R5represents H, OH, (C1-5)alkyl or (C1-5)alkoxy; or a pharmaceutically acceptable salt thereof.

REFERENCES:
patent: 5091391 (1992-02-01), Aizenman et al.
patent: 5212158 (1993-05-01), Vandai
patent: 5804563 (1998-09-01), Still et al.
patent: 5840838 (1998-11-01), Hensley et al.
patent: 5973111 (1999-10-01), Bemis et al.
patent: 6080848 (2000-06-01), Henrichwark et al.
patent: 6156572 (2000-12-01), Bellamkonda et al.
patent: 6235929 (2001-05-01), Powers
patent: 6846641 (2005-01-01), Wieloch et al.
patent: 0316218 (1989-05-01), None
patent: 0445606 (1991-09-01), None
patent: 0446706 (1991-09-01), None
patent: 0446706 (1991-09-01), None
patent: 10818341 (2000-07-01), None
patent: 1231279 (2002-08-01), None
patent: 04-005240 (1992-01-01), None
patent: 09040577 (1997-02-01), None
patent: 09169797 (1997-06-01), None
patent: WO 88/09604 (1988-12-01), None
patent: WO 92/11850 (1992-07-01), None
patent: WO92/13549 (1992-08-01), None
patent: WO 96/41638 (1996-12-01), None
patent: WO 98/14202 (1998-04-01), None
patent: WO 01/28578 (2001-04-01), None
patent: WO 01/28578 (2001-04-01), None
patent: WO 01/34828 (2001-05-01), None
patent: WO 01/68114 (2001-09-01), None
patent: WO 02/062373 (2002-08-01), None
patent: WO 02/062373 (2002-08-01), None
patent: WO 02/062828 (2002-08-01), None
patent: WO 02/062828 (2002-08-01), None
Kan. Current and future approaches to therapy of Alzheimer's disease. Eur J Med Chem. 1992, vol. 27, pp. 565-570.
Hofman et al. Atherosclerosis, apolipoprotein E, and prevalence of dementia and Alzheimer's disease in the Rotterdam Study. Lancet 1997, vol. 349, pp. 151-154.
Scientists uncover Alzheimer's clues. BBC News, Sunday Jun. 25, 2000. (Accessed online May 3, 2005 at http:/
ews.bbc.co.uk/1/hi/health/803297.stm) pp. 1-3.
Beyer, H., and Walter, W.,Handbook of Organic Chemistry,by S. Hirzel Verlag, Stuttgard (English translation of the 22ndedition ofLehrbuch der Organischen Chemie) (1996), pp. 827-838.
Blundell, T.L., et al., “Knowledge-based protein modelling and design”,Eur. J. Biochem.,172:513-520 (1988).
Chessebeuf, M., et al., “Rat liver epithelial cell cultures in a serum-free medium: primary cultures and derived cell lines expressing differentiated functions”,In Vitro,20(10):780-795 (1984).
Clark, M.C., et al., “Validation of the general purpose Tripos 5.2 force field”,J. Comp. Chem.,10(8):982-1012 (1999).
De Pooter, H., et al., “N-acylamino acids and peptides IV the synthesis of N-cinnamyl-, N-p.coumaryl- and N-caffeyl-glycine and -glycyl-L-phenylalanine”,Bull. Soc. Chim. Belg.,85(9):647-656 (1976). XP008015013.
Faden, A.I., et al., “Novel TRH analog improves motor and cognitive recovery after traumatic brain injury in rodents”,Amer. J. Physiology277(4, pt. 2):R1196-R1204 (1999),Chem. Abstr.132:31033 XP002207513, XP008014976.
Faden, A.I., et al., “Structure-activity relationships of TRH analogs in rat spinal cord injury”,Brain Research, 448:287-293 (1988). XP008015202.
Gasteiger, J., et al., “Iterative partial equalization of orbital electronegativity—a rapid access to atomic charges”,Tetrahedron,36:3219-3238 (1980).
Hagg, T., et al., “Delayed treatment with nerve growth factor reverses the apparent loss of cholinergic neurons after acute brain damage”,Exp. Neurol.,101:303-312 (1988).
Jones, D.T., et al., “A new approach to protein fold recognition”,Nature, 358:86-89 (Jul. 1992).
Jones, D.T., “Protein secondary structure prediction based on position-specific scoring matrices”,J. Mol. Biol., 292(2):195-202 (1999).
Kansy, M., et al. “Physicochemical High Throughput Screening: Parallel Artificial Membrane Permeation Assay in the Description of Passive Absorption Processes”,J. Med. Chem.,41(7):1007-1010 (Mar. 26, 1998).
Khuebachova, M., et al., “Mapping the C terminal epitope of the Alzheimer's disease specific antibody MN423”,J. Immunol. Methods(Elsevier Amsterdam, NL) 262(1-2):205-215 (2002), XP004352190.
Laskowski, R.A., et al., “Procheck: a program to check the stereochemical quality of protein structures”,J. Appl. Cryst.,26:283-291 (1993).
Le Poncin-Lafitte, M., et al., “Sound-avoidance conditioning and a mathematical approach to the description of acquisition performance”,Math. Biosciences,59:249-268 (1982).
Luco, J.M., “Prediction of the brain-blood distribution of a large set of drugs from structurally derived descriptors using partial least-squares (PLS) modeling”,J. Chem.. Inf. Comput. Sci.,39 (2):396-404 (1999).
Parnetti, L., et al., “Posatirelin for the treatment of late-onset Alzheimer's disease: a double-blind multicentre study vs citicoline and ascorbic acid”,Acta Neurol. Scand.92:135-140 (1995).
Varon, S., et al., “Nerve Growth Factor in CNS Repair”,J. Neurotrama,11(5) (1994).
Wang, R., et al., “SCORE: A new empirical method for estimating the binding affinity of a protein-ligand complex”,J. Mol. Model.,4:379-394 (1998).
Weiner, S.J., et al., “A new force field for molecular mechanical simulation of nucleic acids and proteins”,J. Am. Chem. Soc.,106:765-784 (1984).
Wiesman, C., et al., “Crystal structure of nerve growth factor in complex with the ligand-binding domain of the TrkA receptor”,Nature, 401:184 (Sep. 9, 1999).
Faden, A.I., et al., “Effect of TRH analogs on neurologic recovery after experimental spinal trauma,”Neurology,35:1331-1334 (1985).
Geschwind, M., et al., “Detection of apoptotic or necrotic death in neuronal cells by morphological, biochemical, and molecular analysis,” inApoptosis Techniques and Protocols, J. Poirier, ed., 1997, pp. 13-31.
Guiloff, R.J., “Thyrotropin releasing hormone and motorneurone disease”,Reviews in the Neurosciences,1:201-219 (1987).
Kurtz, A.F., “Praktische Diagnostik, inAktuelles Wissen Hoechst, Alzheimer-Patienten erkennen und behandeln,” Hoechst AG, publisher (Munich, Germany, 1995), 68-69.With partial translation.
Rapin, J.R., “Les nootropes: propriétés pharmacologiques du piracétam et indications thérapeutiques,”La Lettre du Pharmacologue,6(5):108-111 (1992).With partial translation.
Sarti, G., et al., “TRH-analogues: A possible treatment for symptoms of dementia in elderly patients?”,Archives of Gerontology and Geriatrics,12:173-177 (1991).
Szirtes, T., et al., “Synthesis of thyrotropin-releasing hormone analogues. 1. Complete dissociation of central nervous system effects from thyrotropin-releasing activity,”J. Med. Chem.27:741-745 (1984).

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

Tripeptides and tripeptide derivatives for the treatment of... does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Tripeptides and tripeptide derivatives for the treatment of..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Tripeptides and tripeptide derivatives for the treatment of... will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-3695614

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.