Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1998-07-22
2000-10-31
Shah, Mukund J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514213, 514253, 514258, 514267, 540476, 540593, 544229, 544250, 544280, A01N 4300, A61K 3150, C07D49100, C07D23900, C07F 502
Patent
active
061403172
DESCRIPTION:
BRIEF SUMMARY
The invention relates to 7H-pyrrolo[2,3-d]pyrimidine derivatives and to processes and novel intermediates for their preparation, to pharmaceutical formulations comprising such derivatives, and to the use of those derivatives as medicaments, and to their use in the preparation of medicaments.
The compounds according to the invention are compounds of formula I ##STR3## wherein R.sub.1 and R.sub.2 are each independently of the other lower alkyl; monohalo-, dihalo- or trihalo-lower alkyl; lower alkoxy; phenyl that is unsubstituted or substituted by halogen, monohalo-, dihalo- or trihalo-lower alkyl, carbamoyl-methoxy, carboxy-methoxy, benzyloxycarbonyl-methoxy, lower alkoxycarbonyl-methoxy, phenyl, amino, amino-lower alkyl, lower alkanoylamino, lower alkoxycarbonylamino, phenyl-lower alkoxycarbonylamino, furoyl, thienylcarbonyl, N-lower alkylamino, N,N-di-lower alkyl-amino, hydroxy, lower alkoxy, lower alkanoyloxy, carboxy, lower alkoxycarbonyl, carbamoyl, N-lower alkyl-carbamoyl, N,N-di-lower alkyl-carbamoyl, cyano, amidino, N-(N',N'-di-lower alkylaminomethylidene)-amino, N-((N',N'-di-lower alkylamino)-(lower alkyl)-methylidene)-amino, guanidino, ureido, N.sup.3 -lower alkylureido, N.sup.3,N.sup.3 -di-lower alkylureido, thioureido, N.sup.3 -lower alkylthioureido, N.sup.3,N.sup.3 -di-lower alkylthioureido, lower alkanesulfonylamino, benzene- or naphthalene-sulfonylamino that is unsubstituted or lower alkyl-substituted at the benzene or naphthalene ring, azido or by nitro; hydrogen; unsubstituted or halo- or lower alkyl-substituted pyridyl; N-benzyl-pyridonium; naphthyl; cyano; carboxy; lower alkoxycarbonyl; carbamoyl; N-lower alkyl-carbamoyl; N,N-di-lower alkyl-carbamoyl; N-benzyl-carbamoyl; formyl; lower alkanoyl; lower alkenyl; lower alkenyioxy; or lower alkyl substituted by halogen, amino, lower alkyiamino, piperazino, di-lower alkylamino, phenylamino or phenyl (each unsubstituted or substituted in the phenyl moiety by halogen, lower alkyl, hydroxy, lower alkanoyloxy, lower alkoxy, carboxy, lower alkoxycarbonyl, carbamoyl, N-lower alkyl-carbamoyl, N,N-di-lower alkyl-carbamoyl, cyano, amidino, amino, amino-lower alkyl, lower alkanoylamino, lower alkylamino, N,N-di-lower alkylamino or by trifluoromethyl), hydroxy, lower alkoxy, cyano, carboxy, lower alkoxycarbonyl, carbamoyl, N-lower alkyl-carbamoyl, N,N-di-lower alkyl-carbamoyl, mercapto or by a radical of the formula R.sub.5 --S(O.sub.q)-- wherein R.sub.5 is lower alkyl and q is 0, 1 or 2, or carbon atoms which is unsubstituted or substituted by lower alkyl, ##STR4## wherein m and n are each independently of the other from 0 to 3, alkyl; amino-lower alkyl; N-lower alkyl-amino-lower alkyl; N,N-di-lower alkylamino-lower alkyl; lower alkenyl; lower alkynyl; tri-lower alkylsilanyl-lower alkynyl; monohalo-, dihalo- or trihalo-lower alkyl; halogen; nitro; hydroxy; lower alkoxy; lower alkanoyloxy; isothiocyanato; phenyl that is unsubstituted or substituted by halogen, nitro, trihalo-lower alkyl, hydroxy or by lower alkyl; thienyi; phenyl-lower alkoxy that is unsubstituted or substituted in the phenyl ring by halogen, nitro, trihalo-lower alkyl, hydroxy or by lower alkyl; carboxy; lower alkoxycarbonyl; carbamoyl; N-lower alkylcarbamoyl; N,N-di-lower alkylcarbamoyl; cyano; amino; N-lower alkylamino; N,N-di-lower alkylamino; azido; benzoylamino that is unsubstituted or substituted in the benzene ring by halogen, nitro, tri-halo-lower alkyl, hydroxy or by lower alkyl; lower alkanoylamino; monohalo-, dihalo- or trihalo-lower alkylcarbonylamino; lower alkanesulfonylamino; trihalo-lower alkanesulfonylamino; lower alkylthio; lower alkylsulfinyl; lower alkanesulfonyl; pyrrol-1-yl; piperidin-1-yl; pyrrolidin-1-yl and lower alkanoyl, or two radicals R.sub.3 together or two radicals R.sub.4 together form lower alkylenedioxy; having at least one saturated bond, it being possible for a further ring hetero atom selected from O and S to be present in addition to the bonding nitrogen atom; dihydropyrrolo-fused carbocyclic ring having from 5 to 9 carbon atoms that is fused to the r
REFERENCES:
patent: 5686457 (1997-11-01), Traxler et al.
patent: 5736534 (1998-04-01), Arnold
Burke, "Protein-Tyrosine Kinases: Potential Targets for Anticancer Drug Development," STEM CELLS, vol. 12, pp. 1-6, 1994.
Thompson et al., J. Med. Chem., vol. 38, pp. 3780-88 (1995).
Spada et al., Exp.Opin.Ther.Patents, vol. 5 (8) pp. 805-817 (1995).
Ramsay et al., Synthetic Communications, vol. 25(24), pp. 4029-4033 (1995).
Gribble et al., Synthesis, pp. 859-860 (1977).
Bold Guido
Frei Jorg
Traxler Peter
Borovian Joseph J.
Novartis AG
Shah Mukund J.
Truong Tamthom N.
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