2-amino-4,5-trisubstituted thiazolyl derivatives

Details 2-amino-4,5-trisubstituted thiazolyl derivatives 2-amino-4,5-trisubstituted thiazolyl derivatives

2007-06-19

2007-06-19

Saeed, Kamal A. (Department: 1626)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C514S369000, C514S370000, C548S200000, C548S202000

Reexamination Certificate

active

10486819

ABSTRACT:
This invention concerns the use of a compound of formula (I′), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is halo; C1-6alkyl; C1-6alkylcarbonyl; C1-6alkyloxy -carbonyl; aminocarbonyl; C1-6alkyl substituted with hydroxy, carboxyl, cyano, amino, amino substituted with piperidinyl, amino substituted with C1-4alkyl substituted piperidinyl, mono- or di(C1-6alkyl)amino, aminocarbonyl, mono- or di(C1-6alkyl)aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkyloxy, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl; polyhaloC1-4alkyl; cyano; amino; mono- or di(C1-6alkyl)aminocarbonyl; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; aminoS(═O)2—; mono- or di(C1-6alkyl)aminoS(═O)2; —C(═N—Rx)NRyRz; Q is optionally substituted C3-6cycloalkyl, phenyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, benzthiazolyl, benzoxazolyl, benzimidazolyl, indazolyl, or imidazopyridyl, or Q is a radical of formula (b-1), (b-2), or (b-3), L is optionally substituted phenyl or an optionally substituted monocyclic 5 or 6-membered partially saturated or aromatic heterocycle or a bicyclic partially saturated or aromatic heterocycle; aryl is optionally substituted phenyl; for the manufacture of a medicament for the prevention or the treatment of inflammatory and/or auto-immune diseases mediated through TNF-α and/or IL-12

REFERENCES:
patent: 3933838 (1976-01-01), Manghisi et al.
patent: 4612321 (1986-09-01), Terao et al.
patent: 4649146 (1987-03-01), Takaya et al.
patent: 5000775 (1991-03-01), Grabiak et al.
patent: 3406329 (1985-08-01), None
patent: 154 190 (1985-09-01), None
patent: 790 057 (1997-08-01), None
patent: WO 97/18839 (1997-05-01), None
patent: WO 99/64418 (1999-12-01), None
patent: WO 02/34748 (2001-05-01), None
patent: WO 01/64674 (2003-09-01), None
Nogradi, M., et al, “Dimethyl-β-Cyclodextrin.”Drugs of the Future, 1984, pp. 577-578, vol. 9, No. 8.
Ramchandra, R., et al., “Activity of Acryloyl Thiazoles, Thiazolyl Aminopyrimidines And Thiazolyl Thiopyrimidines on Aspergillus Flavus Link, ex FriesIn Vitro.” Indian bot. Reptri. 1985, pp. 144-147, vol. 2, No. 4.
Corsaro, A., et al., “A Convenient Synthesis Of 2-Alkyl- and 2-Arylamino-4-Aryl-5-Cya Nothiazoles.”Heterocylces, 1985, pp. 2645-2645, vol. 23, No. 10.
Badachikar, R. K. et al., “Antiinflammatory, Analgesic & Antibacterial Activities of 4-(2′-Dialkyl/diarylamino-4′-phenyl-5′-thiazolylcarbonyl)-3-arylsyndnones.”Indian J. of Chem., 1986, pp. 444-446, vol. 25B.
Gawande, N.G., et al., “Synthesis of Thiazolyl-pyrazoline & Isoxazolines from Acrylothiazoles & Their Microbial Activity.”Indian J. Chem., 1987, pp. 351-355. vol. 26B.
Liebscher, J. et al., “Ring Transformations via Bridged 1,3-Dicarbonyl Heteroanalogs; Part II. Synthesis of 4-(w-Aminoalkyl)-thiazoles by a Novel Ring Transformation Reaction of Semicyclic Thioacylamidines with Acidic Methyl Halides.”Synthesis, 1989, pp. 968-970, vol. 12.
Nagatomi, H., et al., “Studies on the Anti-inflammatory Activity and Ulcerogenic Adverse Effect of Thiazoles Derivatives, Expecially 2-Amino-thiazoleacetic Acid Derivatives.”Arzneim-Forsch. 1984, pp. 599-603, vol. 5, No. 34.
Wauve, J.V., et al., “The inhibitory effect of pentamidine on the production of chemotactic cytokines by in vitro stimulated human blood cells.”Inflammatory Res. 1996, pp. 357-363, vol. 45.
Dridi, K., et al., “Reaction of Mercaptoacetate and Halides Containing Activated Methyklenes With Thiocarbamoylimidates: A Novel Approach to the Synthesis Of Aminothiazole Derivatives.”Synthesis Communications, 1998, pp. 167-174, vol. 1, No. 28.
PCT International Search Report dated Jul. 2, 2003 for PCT Appln. No. PCT/EP 02/08955 which relates to U.S. Patent Appln. filed herewith.
Richter, Monika, “Reaction behavior of selected carboxylic acid amides towards heterocumulenes, Synthesis of N-aroyl, (heteroaroyl)guanldines, aroylisothiouress and 2-aminothiazoles”, Z. Chem. (1982), 22(3), 103-4 (XP008006386).

Affiliated with

Also associated with

Rating

2-amino-4,5-trisubstituted thiazolyl derivatives does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with 2-amino-4,5-trisubstituted thiazolyl derivatives, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and 2-amino-4,5-trisubstituted thiazolyl derivatives will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-3887181