Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1992-06-09
1995-01-03
Berch, Mark L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514215, 514218, 5142285, 5142342, 514258, 540544, 540553, 540575, 540578, 540597, 540603, 544 61, 544127, 544143, 544279, 544280, C07D47104, C07D48704, A61K 31505, A61K 3155
Patent
active
053787005
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a novel fused pyrimidine derivative, in particular, a fused pyrimidine derivative having a substituted amino group at the 2- position of the pyrimidine ring and a substituted amino, oxy, thio, alkyl, alkenyl or arylalkyl group at the 4- position of the pyrimidine ring, and a pharmaceutically acceptable acid addition salt thereof. Further, the invention relates to a pharmaceutical preparation comprising said derivative or said pharmaceutically acceptable acid addition salt, as an active ingredient.
BACKGROUND ART
Among fused pyrimidine compounds, 5,6-dihydro-7H-pyrrolo[2,3-d]pyrimidine derivatives having an amino group at their 2- and 4-positions and a process for producing these compounds are known in the art [see, Yamazaki et al., Synthesis, Vol. 3, 266 (1983)]. Similarly, 5,6,7,8-tetrahydropyrido[2,3-d]pyrimidine derivatives having an amino group at their 2- and 4-positions are known in the art [see, Ibid.; and I. Bitter et al., Heterocycles, Vol. 23, 1167 (1985)]. Further, 5,6,7,8-tetrahydro-9H-pyrimido[4,5-b]azepine derivatives having an amino group at their 2- and 4-positions are also known in the art [see, R. G. Glushkov et al., Khim. -Farm. Zh., Vol. 1, 21 (1967)]. Nevertheless, biological activities of these fused pyrimidines have not been known in the art.
Further, no fused pyrimidine derivatives having a substituted amino group at the 2-position of the pyrimidine ring and a substituted amino, oxy, thio, alkyl, alkenyl or arylalkyl group at its 4-position at the same time, has been disclosed in the prior art, and it is not known that the same have a specific pharmacologic activity.
DISCLOSURE OF THE INVENTION
Our extensive and intensive researches on the fused pyrimidine derivatives resulted in a discovery of the compound defined as the general formula [I] described below which have an excellent pharmacologic activity against hypoxemia associated with respiratory diseases.
Note, the present inventors, in related research, found that some pyrrolo[2,3-d]pyrimidine derivatives have the same pharmacologic activity as the compounds of the present invention, have filed a patent application, which is copending, prior to the filing of this application.
Accordingly, in accordance with the present invention, novel fused pyrimidine derivatives having the general formula [I] described below, and pharmaceutically acceptable acid addition salts thereof, and a process for preparation of the same and pharmaceutical preparations comprising a compound selected from the same, are provided: ##STR4## wherein
R.sup.1 represents a hydrogen atom, or an unsubstituted or substituted alkyl, alkenyl, arylalkyl, arylalkenyl or alkylcarbonyl group;
R.sup.2 and R.sup.3, independently of each other, represent a hydrogen atom, or an unsubstituted or substituted alkyl, alkenyl, arylalkyl, arylalkenyl or alkylcarbonyl group; nitrogen atom to form a saturated 5- to 7- membered ring, which may be constructed with at least one hetero atom selected from N, O and S, with the proviso that either R.sup.2 or R.sup.3 represents a group other than a hydrogen atom;
Y represents a linking group of the formula ##STR5## wherein n is an integer of from 4 to 6, ##STR6## wherein A is a hydrogen atom or alkyl group; and
Z when bonded to a carbon atom on said linking group, represents a hydrogen atom, or carboxylic, amino or hydroxyl group, or an unsubstituted or substituted alkyl, aryl, arylalkyl, alkyloxy, alkylcarbonyloxy, alkyloxycarbonyl, arylcarbonyloxy, arylalkylcarbonyloxy, arylalkenylcarbonyloxy, alkylamino, alkenylamino, arylamino, arylalkylamino or alkylcarbonylamino group; and when bonded to an atom other than said carbon atom of the linking group and represents a hydrogen atom, or an unsubstituted or substituted alkyl, alkenyl, aryl, arylalkyl, arylalkenyl, alkylcarbonyl, arylalkylcarbonyl, arylalkenylcarbonly or arylcarbonyl group; or Y and Z together represent an unsubstituted or substituted alkyl, alkenyl or arylalkyl group; or a 5- to 7- member heterocyclic ring which has a nitr
REFERENCES:
patent: 3631045 (1971-12-01), Kim
Bitter et al. Heterocycles 23, 1167 (1985).
Takahata Synthesis pp. 226-228 (1983).
"An Investigaton of Lactams X: Chemical Synthesis of 9H, Pynimido [4, 5-b] azepin Derivatives from Caprolactam", V. G. Granik, R. G. Grucikof Khim Pharm Zh 1(5), 21-26 (1967) (with partial translation).
Hasegawa Masaichi
Hoshina Kenji
Kadota Takashi
Kataoka Ken-ichiro
Sakuma Yasuji
Berch Mark L.
Teijin Limited
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