Substituted piperazines

Details Substituted piperazines Substituted piperazines

2007-01-02

2007-01-02

Bernhardt, Emily (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

C514S218000, C514S241000, C514S242000, C514S249000, C514S252110, C514S252020, C514S252190, C514S253060, C514S253090, C514S254010, C514S254020, C514S254030, C514S254040, C514S254060, C514S254070, C540S575000, C544S180000, C544S182000, C544S238000, C544S277000, C544S295000, C544S353000, C544S357000, C544S363000, C544S364000, C544S366000, C544S367000, C544S368000, C544S369000, C544S370000, C544S371000

Reexamination Certificate

active

10460752

ABSTRACT:
Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

REFERENCES:
patent: 3362956 (1968-01-01), Archer
patent: 3478032 (1969-11-01), Arya
patent: 3491098 (1970-01-01), Archer
patent: 3723433 (1973-03-01), Ueno et al.
patent: 3950354 (1976-04-01), Wenselburger et al.
patent: 3994890 (1976-11-01), Fujimura et al.
patent: 4166452 (1979-09-01), Generales, Jr.
patent: 4174393 (1979-11-01), Van Daalen et al.
patent: 4256108 (1981-03-01), Theeuwes
patent: 4265874 (1981-05-01), Bonsen et al.
patent: 4310429 (1982-01-01), Lai
patent: 4442102 (1984-04-01), Heinemann et al.
patent: 4547505 (1985-10-01), Oepen et al.
patent: 4559341 (1985-12-01), Petersen et al.
patent: 4562189 (1985-12-01), Tomcufcik et al.
patent: 4672063 (1987-06-01), Jasserand et al.
patent: 4772604 (1988-09-01), van Wijngaarden et al.
patent: 4880809 (1989-11-01), Sugihara et al.
patent: 4997836 (1991-03-01), Sugihara et al.
patent: 5011928 (1991-04-01), Venero et al.
patent: 5177078 (1993-01-01), Ward et al.
patent: 5215989 (1993-06-01), Baldwin et al.
patent: 5227486 (1993-07-01), Merce-Vidal et al.
patent: 5292739 (1994-03-01), Merce Vidal et al.
patent: 5346896 (1994-09-01), Ward et al.
patent: 5382586 (1995-01-01), Merce Vidal et al.
patent: 5464788 (1995-11-01), Bock et al.
patent: 5580985 (1996-12-01), Lee et al.
patent: 5607936 (1997-03-01), Chiang et al.
patent: 5646151 (1997-07-01), Kruse et al.
patent: 5681954 (1997-10-01), Yamamoto et al.
patent: 5719156 (1998-02-01), Shue et al.
patent: 5756504 (1998-05-01), Bock et al.
patent: 5760028 (1998-06-01), Jadhav et al.
patent: 5760225 (1998-06-01), Yuan
patent: 5780475 (1998-07-01), Baker et al.
patent: 5798359 (1998-08-01), Shue et al.
patent: 5968938 (1999-10-01), Williams et al.
patent: 6043246 (2000-03-01), Fukami et al.
patent: 6114334 (2000-09-01), Kerrigan et al.
patent: 6191159 (2001-02-01), Pinto
patent: 6207665 (2001-03-01), Bauman et al.
patent: 6288083 (2001-09-01), Luly et al.
patent: 6329385 (2001-12-01), Luly et al.
patent: 6384035 (2002-05-01), Hutchings et al.
patent: 6455544 (2002-09-01), Friedhoff et al.
patent: 6469041 (2002-10-01), Yuan
patent: 6492375 (2002-12-01), Snutch
patent: 6518273 (2003-02-01), Chapman et al.
patent: 2002/0022624 (2002-02-01), Dinnell et al.
patent: 2002/0040020 (2002-04-01), Bretenbucher et al.
patent: 2002/0045613 (2002-04-01), Pauls et al.
patent: 2002/0045749 (2002-04-01), Lai
patent: 2002/0049205 (2002-04-01), Li et al.
patent: 2002/0077321 (2002-06-01), Khanna et al.
patent: 2002/0107255 (2002-08-01), Blumberg et al.
patent: 2002/0119961 (2002-08-01), Blumberg et al.
patent: 2003/0087917 (2003-05-01), Starck et al.
patent: 2003/0139425 (2003-07-01), Bauman et al.
patent: 2003/0149021 (2003-08-01), Li et al.
patent: 2004/0162282 (2004-08-01), Pennell et al.
patent: 2005/0256130 (2005-11-01), Pennell et al.
patent: 0 479 546 (1992-04-01), None
patent: 1 006 110 (2000-06-01), None
patent: WO 97/10219 (1997-03-01), None
patent: WO 97/44329 (1997-11-01), None
patent: WO 98/25617 (1998-06-01), None
patent: WO 98/39000 (1998-09-01), None
patent: WO 98/56771 (1998-12-01), None
patent: WO 99/37619 (1999-07-01), None
patent: WO 99/37651 (1999-07-01), None
patent: WO 00/47539 (2000-08-01), None
patent: WO 00/53600 (2000-09-01), None
patent: WO 02/008221 (2002-01-01), None
patent: WO 02/14314 (2002-02-01), None
patent: WO 03/008395 (2003-01-01), None
patent: WO 03/024450 (2003-03-01), None
patent: WO 03/051842 (2003-06-01), None
CHEMCATS Database (Chemical Abstracting Service), Accession No. 2003:2855298, Jan. 1, 2004 for CAS Registry No. 492422-98-7.
CHEMCATS Database (Chemical Abstracting Service), Accession No. 2001:2759474, Oct. 20, 2003 for CAS Registry No. 351986-92-0.
Badran, M. et al., “Indazole derivatives (part III): synthesis of pyrazolo-[1,2-a]indazole-1,9-dione,[1,2,4]triazino[1,2-a]indazole-1,10-dione, 3-(Indazol-1-yl)propionic acid amides and hydrazides possessing potential biological activity”Alex. J. Pharm. Sci.(1999) 13(2):101-106.
Bebernitz, G. et al., “The effect of 1,3-diaryl-[1H]-pyrazole-4-acetamides on glucose utilization in on/ob mice”J. Med. Chem.(2001) 44:2601-2611.
Czarnocka—Janowicz, A. et al., “Synthesis and pharmacological activity of 5-substituted-s-triazole-3-thiols”Pharmazie(1991) 46:109-112.
Database Crossfire Beilstein 'Online! Beilstein Institut zur Forderung der Chemischen Wissenschaften, Frankfurt am Main, DE; Database accession No. BRN 6982047 XP002254060 abstract & VARASI et al., Farmaco Ed. Sci. (1987) 42(6):425-436.
Database Crossfire Beilstein 'Online! Beilstein Institut zur Forderung der Chemischen Wissenschaften, Frankfurt am Main, DE; Database accession No. BRN 1159762 XP002254062 abstract & Zotta et al. FARMACIA (1977) 25:129-134.
Database Crossfire Beilstein 'Online! Beilstein Institut zur Forderung der Chemischen Wissenschaften, Frankfurt am Main, DE; Database accession No. BRN 6000843 XP002254061 abstract & TOJA et al., Heterocycles (1987) 26(8):2129-2138.
Database Crossfire Beilstein 'Online! Beilstein Institut zur Forderung der Chemischen Wissenchaften, Frankfurt am Main, DE; Database accession No. BRN 9229443 XP002254063 abstract & VOVK, et al., Russ. J. Org. Chem. (2001) 37(12).
Devries, M. et al., “On the edge: the physiological and pathophysiological role of chemokines during inflammatory and immunological responses”Sem. Immun.(1999) 11:95-104.
Fischer, F. et al., “Modulation of experimental autoimmune encephalomyelitis: effect of altered peptide ligand on chemokine and chemokine receptor expression”J. Neuroimmun.(2000) 110:195-208.
Foks, H. et al., “Synthesis of new 5-substituted 1,2,4-triazole-3-thione derivatives”Phosphorus, Sulfur and Silicon(2000) 164:67-81.
Hayao, S. et al., “New antihypertensive aminoalkyltetrazoles”J. Med. Chem.(1967) 10:400-402.
Hcaplus: Accession No. 1984:630511, Document No. 101:230511; Japanese Patent No. 59130890, issued Jul. 27, 1984; Abstract, 4 pages.
Hesselgesser, J. et al., “Identification and characterization of small molecule functional antagonists of the CCR1 chemokine receptor”J. Biol. Chem.(1998) 273(25):15687-15692.
Izikson, L. et al., “Resistance to experimental autoimmune encephalomyelitis in mice lacking the CC chemokine receptor (CCR)2”J. Exp. Med.(2000) 192(7):1075-1080.
Kennedy, K. et al., “Role of chemokines in the regulation of Th1/Th2 and autoimmune encephalomyelitis”J. Clin. Immunol.(1999) 19(5):273-279.
Liang, M. et al., “Species selectivity of a small molecule antagonist for the CCR1 chemokine receptor”Eur. J. Pharmacol.(2000) 389:41-49.
Liang, M. et al., “Identification and characterization of a potent, selective, and orally active antagonist of the CC chemokine receptor”J. Biol. Chem.(2000) 275(25):19000-19008.
Ng, H. et al., “Discovery of novel non-peptide CCR1 receptor antagonists”J. Med. Chem.(1999) 42:4680-4694.
Nicolai, E. et al., “Synthesis and angiotensin II receptor antagonist activity of C-linkedpyrazole derivatives”Chem. Pharm. Bull.(1994) 42(8):1617-1630.
Patent Abstracts of Japan, vol. 007, No. 139 (C-171), Jun. 17, 1983 & JP 58 052256 A (Nippon Noyaku KK), Mar. 28, 1983 abstract.
Plater-Zyberk, C. et al., “Effect of a CC chemokine receptor antagonist on collagen induced arthritis in DBA/1 mice”Ummun. Lett.(1997) 57:117-120.
Rottman, J. et al., “Leukocyte recruitment during onset of experimental allergic encephalomyelitis is CCR1 dependent”Eur. J. Immunol.(2000) 30:2372-2377.
SciFinder Report; Piperazine, 1-[(4-nitro-1H-imidazol-1-yl)acetyl]-4-phenyl-(9CI); Registry No. 31270

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