Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2006-07-11
2006-07-11
Raymond, Richard L. (Department: 1624)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S235800, C514S266210, C514S266230, C514S266300, C544S121000, C544S283000, C544S284000, C544S287000
Reexamination Certificate
active
07074800
ABSTRACT:
The invention relates to the use of compounds of formula (I), wherein ring C is an 8, 9, 10, 12 or 13-membered bicyclic or tricyclic moiety which optionally may contain 1–3 heteroatoms selected independently from O, N and S; Z is —O—, —NH—, —S—, —CH2— or a direct bond; n is 0–5; m is 0–3; R2represents hydrogen, hydroxy, halogeno, cyano, nitro, trifluoromethyl, C1-3alkyl, C1-3alkoxy, C1-3alkylsulphanyl, —NR3R4(wherein R3and R4, which may be the same or different, each represents hydrogen or C1-3alkyl), or R5X1— (wherein X1and R5are as defined herein; R1represents hydrogen, oxo, halogeno, hydroxy, C1-4alkoxy, C1-4alkyl, C1-4alkoxymethyl, C1-4alkanoyl, C1-4haloalkyl, cyano, amino, C2-5alkenyl, C2-5alkynyl, C1-3alkanoyloxy, nitro, C1-4alkanoylamino, C1-4alkoxycarbonyl, C1-4alkylsulphanyl, C1-4alkylsulphinyl, C1-4alkylsulphonyl, carbamoyl, N—C1-4alkylcarbamoyl, N,N-di(C1-4alkylcarbamoyl, aminosulphonyl, N—C1-4alkylaminosulphonyl, N,N-di(C1-4alkyl)aminosulphonyl, N—(C1-4alkylsulphonyl)amino, N—(C1-4alkylsulphonyl)-N—(C1-4alkyl)amino, N,N-di(C1-4alkylsulphonyl)amino, a C3-7alkylene chain joined to two ring C carbon atoms, C1-4alkanoylaminoC1-4alkyl, carboxy or a group R56X10(wherein X10and R56are as defined herein); and salts thereof, in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals, processes for the preparation of such compounds, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient and compounds of formula (I). The compounds of formula (I) and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.
REFERENCES:
patent: 5409930 (1995-04-01), Spada et al.
patent: 5411963 (1995-05-01), Dreikorn et al.
patent: 5480883 (1996-01-01), Spada et al.
patent: 5646153 (1997-07-01), Spada et al.
patent: 5710158 (1998-01-01), Myers et al.
patent: 5714493 (1998-02-01), Myers et al.
patent: 5721237 (1998-02-01), Myers et al.
patent: 5736534 (1998-04-01), Arnold
patent: 5859009 (1999-01-01), Schaper et al.
patent: RE36256 (1999-07-01), Spada et al.
patent: 6046206 (2000-04-01), Pamukcu et al.
patent: 6057320 (2000-05-01), Spada et al.
patent: 6153617 (2000-11-01), Bridges
patent: 6162804 (2000-12-01), Bilodeau et al.
patent: 6225318 (2001-05-01), Sobolov-Jaynes et al.
patent: 6531491 (2003-03-01), Kania et al.
patent: 6645969 (2003-11-01), Myers et al.
patent: 2002/0177601 (2002-11-01), Himmelsbach et al.
patent: 19614718 (1997-10-01), None
patent: 0 326 330 (1989-08-01), None
patent: 0 602 851 (1994-06-01), None
patent: 0 602 851 (1994-06-01), None
patent: 0 837 063 (1998-04-01), None
patent: 1 029 853 (2000-08-01), None
patent: 2 345 486 (2000-07-01), None
patent: 87/04321 (1987-07-01), None
patent: 92/20642 (1992-11-01), None
patent: 95/15758 (1995-06-01), None
patent: 95/19169 (1995-07-01), None
patent: 95/23141 (1995-08-01), None
patent: 95/24190 (1995-09-01), None
patent: 96/29301 (1996-09-01), None
patent: 96/39145 (1996-12-01), None
patent: 97/03069 (1997-01-01), None
patent: 97/17329 (1997-05-01), None
patent: 97/22596 (1997-06-01), None
patent: 97/30034 (1997-08-01), None
patent: 97/42187 (1997-11-01), None
patent: 98/02434 (1998-01-01), None
patent: 98/54093 (1998-12-01), None
patent: 99/06396 (1999-02-01), None
patent: 99/10349 (1999-03-01), None
patent: 99/21859 (1999-05-01), None
patent: 99/28159 (1999-05-01), None
patent: 99/35132 (1999-07-01), None
patent: 99/35146 (1999-07-01), None
patent: 00/06554 (2000-02-01), None
patent: 00/12497 (2000-03-01), None
patent: 00/44728 (2000-08-01), None
patent: 00/55141 (2000-09-01), None
patent: 01/02369 (2001-01-01), None
patent: 01/29025 (2001-04-01), None
Sinyak et al., Chemical Abstracts, vol. 104:199594, 1986.
Karminski et al., Chemical Abstracts, vol. 100:34492, 1984.
Bridges, et al., “Enantoselective Inhibition of the Epidermal Growth Factor Receptor Tyrosine Kinase by 4-(a-Phenethylamino)quinazolines,” Bioorganic & Medicinal Chemistry, vol. 3, No. 12, pp. 1651-1656, 1995.
Gazit et al., Tyrophostins IV-Highly Potent Inhibitors . . . Relationship Study of 4-Anilidoquinazolines, Bioorganic & Medicinal Chemistry, vol. 4, No. 8, 1996, pp. 1203-1207.
Hara et al., On the Amination of Azeheterocycles. A New Procedure for the Introduction of an Amino Group (1), J. Heterocyclic Chem. vol. 19, 1982, pp. 1285-1287.
Karminski et al., The Synthesis of Some Quinazoline Derivatives and Their Biological Properties; J. Environ. Sci. Health, vol. B18, 1983, pp. 599-610.
Sinyak, et al., Synthesis and Biological Properties of Derivatives of 4-Heterylmercaptoquinazoline, Zaporozh'e Medical Institute pp. 103-106, translated from Khimiko-farmatsevticheskii Zhurnal, vol. 20, No. 2, Feb. 1986, 168-171, original article submitted Dec. 29, 1984.
Gibson et al., “Epidermal Growth Factor Receptor Tyrosine Kinase: Structure-Activity Relationships And Antitumour Activity of Novel Quinazolines”, Bioorganic and Medicinal Chemistry Letters, vol. 7, No. 21, 1997, pp. 2723-2728.
Hennequin et al., “Design and Structure-Activity Relationship of a New Class of Potent VEGF Receptor Tyrosine Kinase Inhibitors”, J. Med. Chem., 1999, 42, pp. 5369-5389.
Hennequin Laurent F A
Mckerrecher Darren
Ple Patrick
Stokes Elaine S E
AstraZeneca AB
Morgan & Lewis & Bockius, LLP
LandOfFree
Quinazoline derivatives as angiogenesis inhibitors does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Quinazoline derivatives as angiogenesis inhibitors, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Quinazoline derivatives as angiogenesis inhibitors will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-3529227