1,2,4-thiadiazolium derivatives as melanocortin receptor...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

C548S128000

Reexamination Certificate

active

07319107

ABSTRACT:
The present invention is directed to novel 1,2,4-thiadiazol-2-ium derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention are useful for the treatment of metabolic, CNS and dermatological disorders such as obesity, impaired oral glucose tolerance, elevated blood glucose levels, type II diabetes, Syndrome X, diabetic retinopathy, spinal cord injury, nerve injury, acute neurodegenerative disorders, chronic neurodegenerative disorders, plexopathies, male erectile dysfunction, dry eyes, acne, dry skin, aged skin, seborrheic dermatitis, rosacea, excessive ear wax, meibomian gland disorder, pseudofolliculitis, yeast infections, dandruff, hidradenitis suppurativa, ocular rosacea and eccrine gland disorder.

REFERENCES:
patent: 6294534 (2001-09-01), Nargund et al.
patent: 6410548 (2002-06-01), Nargund et al.
patent: 7049331 (2006-05-01), Eisinger et al.
patent: 131373 (1978-06-01), None
patent: 60-11481 (1985-01-01), None
patent: 2-173165 (1990-07-01), None
patent: WO 99/55679 (1999-11-01), None
patent: WO 99/64002 (1999-12-01), None
patent: WO 00/24725 (2000-05-01), None
patent: WO 01/55107 (2001-08-01), None
Nair et al (1980): STN International CAPLUS database (Columbus, Ohio) Accession No. 1981; 15644.
Abraham, W. et al., “Formamidinyl Isothiocyanates-III Addition of Nucleophilic Partners to Formamidinoyl Isothyiocyanates”, Tetrahedron 29, 1973, pp. 699-705 (Translation).
Barbier, B et al; “Crystal Structure of 2-benzyl-3-phenyl-5-phenylimino-Δ3-1,2,4-thiadiaoline, C21H17N3S”; Z. Kristallogr.NCS (1998), pp. 741-742, vol. 213.
Barnikow, Günter et al; Regarding the oxidative cyclization of imidoyl-thioureas1); Z. Chem., (1972), pp. 130, vol. 12-No. 4.
Chetia, J.P. et al; “One-Pot Synthesis of 2-Aryl-3-phenyl(benzyl)-5-phenylimino-Δ4-1,2,4-thiadiazolines usingN-Chlorosuccinimide”; Synthesis Communications, Jan. 1985, pp. 83-84.
Fawzi, Ahmad B. et al; “SCH-202676: An Allosteric Modulator of Both Agonist and Antagonist Binding to G Protein-Coupled Receptors”; Molecular Pharmacology, (2001), pp. 30-37; vol. 59-No. 1.
Goerdeler, Joachim et al; “Herstellung von Acylheterocumulenen aus fünfgliedrigen Ringen mit Hilfe von Phosphinen”; Chem. Ber. (1974), pp. 502-507; vol. 107.
Goerdeler, Joachim et al; “Herstellung von (N-Alkylbenzimidoyl)- und (N-Arylbenzimidoyl)carbodiimiden; ihre Umlagerung zu Aminochinazolinen und Dihydro-1,3,5-triazinen”; Chem. Ber. (1986), pp. 3737-3748, vol. 119.
Goerdeler, Joachim et al; “Reaktion von Heterocumulenen mit 5-Äthoxy-3-phenylimino-3H-1,2,4-dithiazol”; Chem. Ber. (1976), pp. 848-854, vol. 109.
Goerdeler, Joachim et al; “Reaktionen von 5-Imino-Δ3-1,2,4-thiadiazolinen mit Heterocumulenen (Präparative Gesichtspunkte)”; Chem. Ber. (1979); pp. 517-531, vol. 112.
Goerdeler, Joachim et al; “Über die Zerfallsprodukte von Imino-Δ3-1,2,4-thiadiazolinen”; Chem. Ber. (1979), pp. 1288-1296, vol. 112.
Hagiwara, Kenji et al; Synthesis and Fungicidal Activity of Δ3-1,2,4-Thiadiazolines; Journal of Pesticide Science, (1992), pp. 251-259, vol. 17.
L'abbé, Gerrit et al; “5-Imino-Δ3-1,2,4-thiadiazoline Derivatives with a Linear N-S . . . O Grouping. Synthesis and Crystal Structures”; J Heterocyclic Chem., Nov. 1981, pp. 1309-1317, vol. 18.
Liebscher, Jürgen et al; “Oxidation-assisted synthesis of N-imidoyl-guanidines from N-imidoyl-thioureas”; Z. Chem., (1985), pp. 362-363, vol. 25-No. 10.
Nair, M.D. et al; “Oxidation of N-Phenyl-N-phenylthiocarbamoylbenzamidines with Sulphuryl Chloride & Bromine”; Indian Journal of Chemistry, May 1980, pp. 335-337, vol. 19B.
Neidlein, R. et al; “Zum Reaktionsverhalten Von N-Acyl-S-Chlorisothiocarbamoylchloriden”; Tetrahedron, (1971), pp. 4117-4124, vol. 27.
Wikberg, Jarl E.S.; “Melanocortin receptors: new opportunities in drug recovery”; Exp. Opin. Ther. Patents; (2001), pp. 61-76, vol. 11-No. 1.
Zyabrev, V.S. et al; “Chlorination of Imidoyl Isothiocyanates”; Ukrainskii Khimcheskii Zhurnal; (1995), pp. 55-61, vol. 61-No. 5.
S. Rajappa et al., “A General Synthesis of Thiazoles, Part 3. Comparative Evaluation of Different Functionalised Thioureas as Precursors,” J.C.S. Perkin I, May 1978, pp. 1762-1764.
J. Goerdeler et al, Chem. Ber. 112, pp. 1288-1296 (1979) with English-language translation.
Z. Chem. vol. 25 (1985) No. 10, pp. 362-363 with English-language translation.
J. Goerdeler et al., Chem. Ber. 101, 3475-3490 (1968) with English-language abstract.
Abraham, W. et al., “Formamidinoylisothiocyanate-III. Addition Nucleophiler Partner an Formamidinoylisothiocyanate”, Tetrahedron, vol. 29, No. 5, pp. 699-705, Mar. 1973.
PCT International Search Report, dated Nov. 5, 2002, for PCT Int'l Appln. No. PCT/US02/35365.

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

1,2,4-thiadiazolium derivatives as melanocortin receptor... does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with 1,2,4-thiadiazolium derivatives as melanocortin receptor..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and 1,2,4-thiadiazolium derivatives as melanocortin receptor... will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-2810992

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