摘要:
The present invention relates to compounds of formula I:
wherein R1 is hydroxy, methoxy, mercapto, hydrazino, substituted hydrazino, chloro, amino, alkylamino, dialkylamino, hydroxyalkylamino, aralkylamino or substituted aralkylamino and R2 is phenylalkyl having 1 to 3 carbon atoms in the alkyl moiety and at least two alkoxy, alkyl, halogen, hydroxy, nitro, amino, substituted amino, aminomethyl, acylamino, carboxy, carboxyalkyl or hydroxymethyl groups in the benzene ring or naphthylalkyl, tetrahydronaphthylalkyl, quinolylalkyl, tetrahydroquinolylalkyl or isoquinolylalkyl, each having 1 to 3 carbon atoms in the alkyl moiety and pharmaceutically acceptable acid addition salts thereof. These compounds are useful as antianginal or bronchial dilator agents.
N IS AN INTEGER FROM 0 TO 5; R IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF: (A) ALKOXY HAVING A STRAIGHT OR BRANCHED CHAIN OF 1 TO 8 CARBON ATOMS; (B) HYDROXY; (C) A RESIDUE OF A PEPTIDICALLY ATTACHED AMINO ACID; (D) A RESIDUE OF A DIPEPTIDE; THE SAID AMINO-ACID AND DIPEPTIDE RESIDUES BEING IN THE FORM OF THEIR FREE CARBOXY ACID; (E) A RESIDUE AS AT (C) AND (D) WHEREIN THE CARBOXY GROUP IS ESTERIFIED WITH AN ALCOHOL, HAVING A STRAIGHT OR BRANCHED CHAIN OF 1 TO 7 CARBON ATOMS; Y IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF: HYDROGEN; ALKYL HAVING A STRAIGHT OR BRANCHED CARBON CHAIN OF 1 TO 5 ATOMS; PHENYL; 3-INDOLYL; -CH2OH, -CH2SH, -(CH2)SCH3 AND -(CH2)MCOR1 M IN THE LAST MEMBER BEING AN INTEGER FROM 1 TO 3 AND R1 BEING ALKOXY HAVING A STRAIGHT OR BRANCHED CHAIN OF 1 TO 8 CARBON ATOMS. AN EXAMPLE IS N-($-(6-PURINYLTHIO)VALERYL)GLYCINE ETHYL ESTER.
THE COMPOUNDS HAVE SHOWN AN ANTINEOPLASTIC EFFECT IN CERTAIN SPECIFIC TRANSPLANTABLE MICE TUMORS. THEY ARE DISTINGUISHED BY THEIR HIGH AFFINITY TO A PARTICULAR ORGAN OR TO THE TISSUE OF A PARTICULAR ORGAN AND THEIR ACUTE AND CHRONICAL TOXICITY IS LOW.
摘要:
An improved process for preparing purine compounds of the formula
WHEREIN X is selected from the group consisting of an amino and a hydroxy group, and Y is selected from the group consisting of an amino and a hydroxy group and hydrogen, which are useful as precursors for the synthesis of organic compounds, as well as a process for preparing a carboxyamide of the formula
USEFUL AS AN INTERMEDIATE FOR THE SYNTHESIS OF THE ABOVE PURINE COMPOUNDS ARE
摘要:
A NEW CLASS OF CHEMICAL COMPOUNDS, ($)-9-(B(3AAMINO-2A-HYDROXY)CYCLOPENTYL) - 6 - SUBSTITUTED - PURINES HAVING THE GENERAL FORMULA:
6-R,9-(2-(HO-),3-X-CYCLOPENTYL)-9H-PURINE
WHEREIN R IS A SUBSTITUENT SELECTED FROM THE GROUP CONSISTING OF HYDROXYL, MERCAPTO, METHYL MERCAPTO, HALOGEN (CHLORINE, BROMINE, FLUORINE AND IODINE) AND SUBSTITUTED AMONO:
R''-N(-R")-
WHEREIN R'' AND R'''' MAY BE THE SAME OR DIFFERENT SUBSTITUENTS AND ARE SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, METHYL, ETHYL, PROPYL AND PHENYL; X IS AN AMINO RADICALOR AMINO ACID; AND ACID SALT DERIVATIVES OF THE SAME, SUCH AS ACETIC, HYDROCHLORIC, SULFURIC, ETC.; AND THE METHOD OF PREPARATION THEREOF. THE INTERMEDIATE ($)-9(B-(3A-AMINO - 2A - HYDROXY)CYCLOPENTYL) - 6 - DIMETHYLAMINOPURINE, OR ANY OF ITS CORRESPONDING 6-SUBSTITUTED DERIVATIVES, LEADS TO THE PREPARATION OF TWO DIASTERIOISOMERS WHEN CONDENSED WITH THE APPROPRIATELY BLOCKED LAMINO ACID. THE SEPARATION OF THESE DIASTERIOISOMERS RESULTS IN THE ISOLATION OF ANTIMICROBIAL AND ANTITUMOR AGENTS.
WHEREIN A IS N OR N$O, R1 IS HYDROGEN, HALOGEN, HYDORYXL, MERCAPTO, LOWER ALKOXY, AR(LOWER)ALKOXY, LOWER AKYTHIO, AMINO, LLLOWER ALKYLAMINO, DI(LOWER)ALKYLAMINO, AR(LOWER)ALKYLAMINO, ACYLAMINO, HYDROXYAMINO, LOWER AKOXYAMINO, AR(LOWER) ALKOXYAMINO OR ARYLOXYAMINO, R2 AND R3 ARE EACH HYDROGEN, HALOGEN, HYDOXYL, MERCAPTO, AMINO, LOWER ALKYL, ARYL, LOWER ALKOXY, AR(LOWER)ALKOXY OR LOWER ALKYLTHIO, R4 IS LOWER ALKYLENE SUBSTITUTED WITH ONE OR MORE HYDROXYIS (BUT NO HYDROXYL GROUP BEING PRESENT AT THE CARBON ATOM ADJACENT TO THE RING NITROGEN ATOM) WHICH MAY BE PROTECTED WITH ACYL, LOWER OR HIGHER ALKOXY, A AR(LOWER)AKYL OR, WHEN A PAIR OF HYDROXYLS EXIST ON THE ALKYLENE GROUP, WHICH LOWER ALKYLIDENE OR AR(LOWER)ALKYLIDENE AND R5 IS HYDROXYL, LOWER OR HIGHER ALKOXY, AMINO, LOWER ALKYLAMINO OR DI(LOWER)ALKYLAMINO, AND THEIR SALTS, WHICH EXIBIT MAKED HYPOCHOLESTEROLEMIC ACTIVITY WHICH EXTREMELY LOW TOXICITY.