Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1996-11-27
1998-07-28
Shah, Mukund J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514252, 514275, 544122, 544295, 544297, 544331, 544332, A61K 31535, A61K 31495, C07D41300, C07D40300
Patent
active
057863555
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a novel 4,6-diarylpyrimidine derivative or salt thereof which has excellent neovascular inhibitory action and is therefore useful as a pharmaceutical typified by a therapeutic agent for solid cancer, rheumatism, diabetic retinopathy or psoriasis; its preparation process and a pharmaceutical containing it.
BACKGROUND ART
The blood vessel is a very important organ for animals. In recent years, it has been found that abnormal neovascular formation becomes an incentive to the morbid state or a factor for the worsening of the morbid state in the diseases such as malignant tumor, rheumatism, diabetic retinopathy and psoriasis. From such a viewpoint, there has been an attempt to search for a therapeutic agent for the above-described diseases using neovascular 15(2), 33-36(1994)"!.
The conventional neovascular inhibitor, however, has not sufficient action or has a problem in safety so that it has not come to be used as a pharmaceutical yet.
An object of the present invention is therefore to provide a compound which has excellent neovascular inhibitory activity and is useful as a pharmaceutical typified by a therapeutic agent for solid cancer, rheumatism, diabetic retinopathy or psoriasis.
DISCLOSURE OF THE INVENTION
With the forgoing in view, the present inventors have conducted an extensive investigation. As a result, it has been found that a novel 4,6-diarylpyrimidine derivative represented by the below-described formula (1) has excellent neovascular inhibitory activity and is useful as a pharmaceutical represented by a therapeutic agent for solid cancer, rheumatism, diabetic retinopathy or psoriasis, leading to the completion of the present invention.
The present invention therefore provides a 4,6-diarylpyrimidine derivative represented by the following formula (1): ##STR2## wherein R represents a nitrogen-containing heterocyclic group which may be substituted by one to four lower alkyl groups or a group --N(R.sup.1)R.sup.2, said R.sup.1 and R.sup.2 being the same or different and independently representing a hydrogen atom, a lower alkyl group, a lower acyl group or a lower alkylsulfonyl group; and Ar represents a phenyl, naphthyl or aromatic, nitrogen-containing heterocyclic group which may have one to four substituents; or a salt thereof.
The present invention also provides a pharmaceutical comprising as an effective ingredient a 4,6-diarylpyrimidine derivative represented by the above formula (1) or salt thereof.
The present invention further provides a pharmaceutical composition comprising a 4,6-diarylpyrimidine derivative represented by the above formula (1) or salt thereof and a pharmacologically acceptable carrier.
The present invention further provides the use of a 4,6-diarylpyrimidine derivative represented by the above formula (1) or salt thereof as a pharmaceutical.
The present invention further provides a curative and preventive method for a disease caused by abnormal neovascular formation, which comprises administering an effective amount of a 4,6-diarylpyrimidine derivative represented by the above formula (1) or salt thereof to a mammary animal including a human being.
The present invention further provide a process for the preparation of a 4,6-diarylpyrimidine derivative represented by the above formula (1) or salt thereof.
As a 4,6-diarylpyrimidine derivative analogous to the invention compound, there is a description, for example, of 2-amino-4-(2,4-dimethoxyphenyl)-6-(3,4,5-trimethoxyphenyl)pyrimidine in "J. Heterocyclic Chem., 26, 1069-1071(1989)", which is however different from the invention compound in the substituting sites of three methoxy groups on the benzene ring at the 6-position. It makes no reference to the biological activity of the compound. In addition, in "J. INDIAN CHEM. SOC., 70, 266-267(1993)", there is a description of 2-amino-4-(2,4-dimethoxyphenyl)-6-(3,4-dimethoxyphenyl)pyrimidine, which is however different in the number of methoxy groups. In this literature, it is only described that concerning the biological acti
REFERENCES:
Anjuneyulu, A.S.R. et al. "synthesis and characterization of some new oxygen and nitrogen heterocyclics: Part II 3,5-diarylisoxazoles, pyrazoles and 4,6-diarylpyrimidines" Indian Journal of Chemistry vol. 34B, Nov. 1995, pp. 933-938.
Anjaneyulu et al. (Indian J. Chem., Sect B: Org. Chem. Incl. Med. Chem. (1995), 34 B (11), 933-938.
Ankhiwala (J. Inst. Chemists (India), vol. 62, pp. 115-116, 1990.
Desai et al. (Oriental Journal of Chemistry vol. 9, No. 3 (1993) 262-263.
Mahmoud et al. (Indian J. Chem., Sect. B: Org. Chem. Incl. Med. Chem. (1996), 34 B (11), 915-919, 1995.
Ankhiwala (J. Indian Chem. Soc. (1989), 66 (6), 417-418.
Asao Tetsuji
Kimura Masayasu
Konno Yasuo
Nozaki Kenji
Suzuki Takashi
Kifle Bruck
Shah Mukund J.
Taiho Pharmaceutical Co. Ltd.
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