Aralkyl-substituted purines and pyrimidines as antianginal bronchodilator agents
    1.
    发明授权
    Aralkyl-substituted purines and pyrimidines as antianginal bronchodilator agents 失效
    ARALKYL取代的脯氨酸和嘌呤类作为抗原递质剂

    公开(公告)号:US3862189A

    公开(公告)日:1975-01-21

    申请号:US38829073

    申请日:1973-08-14

    申请人: WARNER LAMBERT CO

    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.

    摘要翻译: 本发明涉及式I化合物:

    N-(delta-(6-purinylthio)valeryl)amino acids and peptides
    2.
    发明授权
    N-(delta-(6-purinylthio)valeryl)amino acids and peptides 失效
    N-(DELTA-(6-嘌呤基)缬氨酸)氨基酸和肽

    公开(公告)号:US3567705A

    公开(公告)日:1971-03-02

    申请号:US3567705D

    申请日:1967-06-26

    CPC分类号: C07D473/38

    摘要: A COMPOUND OF THE GENERAL FORMULA:

    PURIN-4-YL-S-(CH2)4-CO-NH-(CH2)N-CH(-Y)-CO-R

    WHEREIN:

    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.

    Process for preparing purine compounds by reaction of a carbonitrile with formic acid
    4.
    发明授权
    Process for preparing purine compounds by reaction of a carbonitrile with formic acid 失效
    通过与形成酸反应的碳酸酯制备磷化合物的方法

    公开(公告)号:US3857842A

    公开(公告)日:1974-12-31

    申请号:US20576471

    申请日:1971-12-07

    申请人: SAGAMI CHEM RES

    发明人: ASAI N

    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

    摘要翻译: 制备式WHEREIN X的嘌呤化合物的改进方法是选自氨基和羟基,Y选自氨基和羟基和氢,其可用作 有机化合物的合成,以及制备下式的羧酰胺的方法有用的合成上述化合物的中间体被公开。 这些方法从具有下式的4(5) - 氨基咪唑-5(4) - 腈开始

    (+-)-9-(beta-(3-alpha-amino-2alpha-hydroxy)cyclopentyl)-6-substituted-purines and derivatives thereof
    5.
    发明授权
    (+-)-9-(beta-(3-alpha-amino-2alpha-hydroxy)cyclopentyl)-6-substituted-purines and derivatives thereof 失效
    (±)-9-(BETA-(3-ALPHA-AMINO-2ALPHA-羟基)环戊基)-6-取代的脯氨酸及其衍生物

    公开(公告)号:US3825541A

    公开(公告)日:1974-07-23

    申请号:US22089072

    申请日:1972-01-26

    申请人: UNIV MINNESOTA

    发明人: VINCE R

    CPC分类号: C07D317/72 C07D473/00

    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.

    Purine derivatives having hypocholesterolemic activity
    7.
    发明授权
    Purine derivatives having hypocholesterolemic activity 失效
    具有高脂肪活性的嘌呤衍生物

    公开(公告)号:US3813394A

    公开(公告)日:1974-05-28

    申请号:US2236170

    申请日:1970-03-24

    IPC分类号: C07D473/00 C07D57/38

    CPC分类号: C07D473/00

    摘要: PURINE DERIVATIIVES OF THE FORMULA:

    1-(R5-CO-R4-),2-R3,4,5-(-C(-R1)=A-C(-R2)=N-)IMIDAZOLE

    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.