Chemical compounds

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

C514S338000, C514S422000, C514S423000, C514S443000, C546S276700, C548S453000, C548S530000, C549S050000

Reexamination Certificate

active

07547722

ABSTRACT:
The invention relates to a group of novel thieno-pyrrole compounds of Formula (I):wherein: R1, R2, R3, R4and R5are as defined in the specification, which are useful as gonadotrophin releasing hormone antagonists. The invention also relates to pharmaceutical formulations of said compounds, methods of treatment using said compounds and to processes for the preparation of said compounds.

REFERENCES:
patent: 7056942 (2006-06-01), Hildesheim et al.
patent: 4356029 (1991-06-01), None
patent: 4179949 (1992-06-01), None
patent: 4179949 (1992-06-01), None
patent: 97/21435 (1997-06-01), None
patent: 97/21703 (1997-06-01), None
patent: 97/21704 (1997-06-01), None
patent: 97/21707 (1997-06-01), None
patent: 98/55116 (1998-12-01), None
patent: 98/55119 (1998-12-01), None
patent: 98/55123 (1998-12-01), None
patent: 98/55470 (1998-12-01), None
patent: 98/55479 (1998-12-01), None
patent: 99/21553 (1999-05-01), None
patent: 99/21557 (1999-05-01), None
patent: 99/41251 (1999-08-01), None
patent: 99/41252 (1999-08-01), None
patent: 99/51231 (1999-10-01), None
patent: 99/51232 (1999-10-01), None
patent: 99/51233 (1999-10-01), None
patent: 99/51234 (1999-10-01), None
patent: 99/51595 (1999-10-01), None
patent: 99/51596 (1999-10-01), None
patent: 00/04013 (2000-01-01), None
patent: 00/53178 (2000-09-01), None
patent: 00/53179 (2000-09-01), None
patent: 00/53180 (2000-09-01), None
patent: 00/53181 (2000-09-01), None
patent: 00/53185 (2000-09-01), None
patent: 00/53602 (2000-09-01), None
patent: 00/69433 (2000-11-01), None
patent: 02/24703 (2002-03-01), None
patent: 02/66459 (2002-08-01), None
patent: 02/92565 (2002-11-01), None
Ashton et al. Subsituted Indole-5-carboxamides and -acetamides as Potent Nonpeptide GnRH Receptor Antagonist, Biorganic & Medicinal Chemistry Letters, 2001, pp. 1723-1726, vol. 11.
Ashton et al. Potent Nonpeptide GnHR Receptor Antagonists Derived from Substituted Indole-5-carboxamides and -acetamides Bearing a Pyridine Sid-Chain Terminus, Bioorganic & Medicinal Chemistry Letters 2001, pp. 1727-1731, vol. 11.
Ashton et al. Orally Bioavailable, Indole-Based Nonpeptide GnHR Receptor Antagonists with High Potancy and Functional Activity, Bioorganic and medicinal Chemistry Letters, 2001, pp. 2567-2602, vol. 11.
Chu at al. Initial Structure-Activity Relationship of a Novel Class of Nonpeptidyl GnHR Receptor Antagonists: 2-Arylindoles, Bioorganic and Medicinal Chemistry Letters, 2001, pp. 509-513, vol. 11.
Chu et al. SAR Studies of a novel 5-Substituted 2-Arylindoles as Nonpeptidyl GnHR Receptor Antagonists. , Bioorganic and Medicinal Chemistry Letters, 2001, pp. 515-517, vol. 11.
Freidinger, R. M. Nonpeptide ligands for peptide and protein receptors, Current Opinion in Chemical Biology 1999, pp. 395-406, vol. 3.
Goulet, M. T. Gonadotropin Releasing Hormone Antagonists, Annual Reports in Medicinal Chemistry, 1995, pp. 169-178, vol. 30.
Lin et al. 2-(3,5-Dimethylphenyl)tryptamine Derivatives That Bind to the GnHR Receptor, Bioorganic & Medicinal Chemistry Letters, 2001, pp. 1073-1076, vol. 11.
Lin et al. Heterocyclic Derivatives of 2-(3,5-Dimethylphenyl)tryptamine as GnHR Receptor Antagonists, Bioorganic & Medicinal Chemistry Letters, 2001, pp. 1077-1080, vol. 11.
Simoene, J.P., Synthesis of Chiral B-methyl tryptamine-derived GnHR antagonists,Tetrahedron Letters, 2001, pp. 6459-6461, vol. 42.
Walsh, et al., A Convergent Synthesis of (S)-B-methyl-2aryltryptamine based gonadotropin releasing hormone antagonists, Tetrahedron, 2001, pp. 5233-5241, vol. 57.
Young et al. 2-Arylindoles as Gonadortopin Releasing Hormone (GnHR) Antagonists: Optimization of the Tryptamine Side Chain, Bioorganic & Medicinal Chemistry Letters, 2002, pp. 827-832, vol. 12.
Ujjainwalla, F. Total synthesis of 6- and 7-azaindole derived GnHR antagonists, Tetrahedron Letters, 2001, pp. 6441-6445, vol. 42.
Simeone et al. Modification of the Pyridine Moiety of Non-peptidyl Indole GnHR Receptor Antagonists, Bioorganic & Medical Chemistry Letters, 2002, pp. 3329-3332, vol. 12.
Gibbs, J.B. Pharmaceutical Research in Molecular Oncology, Cell, 1994, pp. 193-198, vol. 792.
Wensbo, D. Indoel-3-pyruvic acid Oxime ethers and Thieno analogues by Heck Cyclisation. Application to the Synthesis of Thia Tyrptophans, Tetrahedron, 1996, pp.; 14975-14988, vol. 52(47).
Blair et al. Thieno[3,2-b] and Thieno[2,3-b]pyrrole Bioisosteric Analogues of Hallucinogen and Serotonin Agonist N.N-Dimethyltryptamine, J. Med. Chem 1999, pp. 1106-1111, vol. 42.
Colburn et al Condensed Thiophen Ring Systems. Part 20. Synthesis of 5-Arylthieno-[3.2-b]pyrroles and 5-Arylthieno[3,2-c]pyrazoles, Journal of the Chemical Society Perkins I 1977, pp. 2436-2441.
Humphries et al The Synthesis of 6-substituted Thieno[3,2-b]pyrroles. Analogs of Tryptophan, Tryptamine and Indoleacetic and' The Journal of Organic Chemistry 1972, pp. 3626-3629, vol. 37.
Keemer et al ‘The Synthesis of 6-Substituted Thieno[3,2-b]pyrroles’ The Journal of Organic Chemistry 1968, vol. 33 (4), pp. 1355-1359, vol. 33.
Srinivasan et al ‘A New Synthesis of 5-Arylthieno[2,3-b]pyrroles and 5-Arylthieno[3,2-b]pyrroles’ Synthesis 1973, 313-315.
Synder et al ‘Synthesis of the Thieno[3,2-b]pyrrole System’ Journal of the American Chemical Society 1957, pp. 2556-2559, vol. 79.
Gale et al Preparation and Reactions of 5-CArbethoxythieno[3,2-n]pyrrole and Some of Its Derivatives, The Journal of Organic Chemistry 1964, pp. 2160-2165, vol. 29.
Aoyama, T. Chemical 7 Pharmaceutical Bulletin, 1981, pp. 3249-3255, vol. 11.
Geetha et al Indian Journal of Chemistry, 1979, pp. 163-164, Section B, vol. 17B(2).
Kumar et al Indian Journal of Chemistry, Section B 1979, pp. 541-543, vol. 18B(2).
Kvitko et al Zhurnal Organicheskoi Khimii, 1976, pp. 1574-1585 (+Abstract), vol. 12(7).
Kvitko et al Enemines of formyl derivatives of thio- and selenopyrrolone and synthesis of thieno- ans selenopheno[2,3-b]pyrroles, Khim Geterotsikl Soedin 1973, pp. 565-566 (+Abstract), vol. (4).

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

Chemical compounds does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Chemical compounds, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Chemical compounds will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-4132620

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