Pyrazolopyrimidines as CRF receptor antagonists

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

C544S250000, C544S251000

Reexamination Certificate

active

07074797

ABSTRACT:
This invention concerns compounds of formulaincluding the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R1is NR4R5or OR5; R2is C1-6alkyl, C1-6alkyloxy or C1-6alkylthio; R3is hydrogen, C1-6alkyl, C1-6alkylsulfonyl, C1-6alkylsulfoxy or C1-6alkylthio; R4is hydrogen, C1-6alkyl, mono- or di(C3-6cycloalkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxyC1-6alkyl or C1-6alkyloxyC1-6alkyl; R5is C1-8alkyl, mono- or di(C3-6cycloalkyl)methyl, A1CH2, C1-6alkyloxyC1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, C1-6alkylthioC1-6alkyl, morpholinyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, C1-6alkylcarbonylC1-6alkyl, C1-6alkyl substituted with imidazolyl; or a radical of formula —Alk—O—CO—Ar1; or R4and R5taken together with the nitrogen atom to which they are attached may form an optionally substituted pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group; having CRF receptor antagonistic properties; pharmaceutical compositions containing such compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amount of a compound of formula (I).

REFERENCES:
patent: 3920652 (1975-11-01), Springer et al.
patent: 4021556 (1977-05-01), Springer et al.
patent: 5420128 (1995-05-01), Kiyokawa et al.
patent: 5571813 (1996-11-01), R uhter et al.
patent: 5688949 (1997-11-01), Inoue et al.
patent: 5707997 (1998-01-01), Shoji et al.
patent: 5843951 (1998-12-01), Inoue et al.
patent: 5985882 (1999-11-01), Inoue et al.
patent: 6060478 (2000-05-01), Gilligan et al.
patent: 6136809 (2000-10-01), Gilligan et al.
patent: 6372743 (2002-04-01), Darrow et al.
patent: 6664261 (2003-12-01), Chen et al.
patent: 6900217 (2005-05-01), Chen
patent: 2002/0151717 (2002-10-01), Chen
patent: 0 244 097 (1987-11-01), None
patent: 0 691 128 (1996-10-01), None
patent: 591 528 (1998-12-01), None
patent: 42-11753 (1967-07-01), None
patent: 44-30512 (1969-12-01), None
patent: 45-30335 (1970-10-01), None
patent: 61-57587 (1986-03-01), None
patent: 3-204877 (1991-09-01), None
patent: WO 94/13676 (1994-06-01), None
patent: WO 94/13677 (1994-06-01), None
patent: WO 95/33750 (1995-12-01), None
patent: WO 96/28448 (1996-09-01), None
patent: WO 96/35689 (1996-11-01), None
Abstract of Japanese Application No. 45-30335, 1970.
Abstract of Japanese Application No. 3-204877, 1991.
Japan Abstract Publication No. 05017470, dated Jan. 26, 1993.
Japan Abstract Publication No. 07309872, dated Nov. 28, 1995.
Japan Abstract Publication No. 08003167, dated Sep. 1, 1996.
Chem. Abstract, vol. 67, No. 23, Dec. 4, 1967, Abstract No. 108663R.
Chem. Abstract, vol. 105, No. 25, Dec. 22, 1996, Abstract No. 226617e.
Derwent Abstract, Japanese Patent No. 44-30512, 2000.
Derwent Abstract of JP 61-57587 - Acc No. 1986-11678, 1998.
Auzzi et al., “2-Phenylphyrazolo [1,5-a] Purimidin 7-ones. A New Class of Nonsteroidal Antiflammatory Drugs Devoid of Ucerogenic Activity,”J. Med. Chem.26:1706-1709, 1983.
Bruni et al., “Synthesis and Study of the Anti-Inflammatory Properties of Some Pyrazolo [1,5-a] Pyrimidine Derivatives,”J. Pharma. Sci. 82(5), 1993.
Ibrahim et al., “Synthesis of New 3- (Pyrimidin-6-yl) Pyrazolo [1, 5a]n Pyrimidines,”Arch Pharm. (Weinheim) 320:487-191, 1987.
Joshi et al., “Synthesis of Some New Fluorine Containing Pyrazolo [1, 5a] Pyrimidines,”J. f.prakt.Chemie. Band 321, Heft2:341-344, 1979.
Novinson et al., “Novel Heterocyclic Nitrofural Hydrazones. In Vivo Antitrypanosomal Activity,”J. Med. Chem.19(4):512-1516, 1976.
Novinson et al., “3-Halo-5,7-Dimethylpyrazolo [1,5-A]Pyrimidines, A Nonbenzodiazepinoid Class Of Antianxiety Agents Devoid Of Potentiation Of Central Nervous System Depressant Effects Of Ethanol Or Barbiturates,”J. Med. Chem.20(3):386-393, 1977.
Senga et al., “Synthesis and Antishistomal Activity of Certain Pyrazolo [1,5-a] Pyrimidines,”J. Med. Chem.24:610-613, 1981.
Springer et al., “Synthesis and Enzymic Activity of Some Novel Xanthine Oxidasse Inhibitors. 3 Substituted 5, 7-Dihydroxypyrazolo [1,5-a] Pyrimidines,” J. Med. Chem. 19(2):291-296, 1976.

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

Pyrazolopyrimidines as CRF receptor antagonists does not yet have a rating. At this time, there are no reviews or comments for this patent.

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

Rate now

     

Profile ID: LFUS-PAI-O-3539013

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