Oxazolidinone derivatives and pharmaceutical compositions containing them

Oxazolidinone derivatives and pharmaceutical compositions containing them

  • CN 1,143,961 A
  • Filed: 03/14/1995
  • Published: 02/26/1997
  • Est. Priority Date: 03/15/1994
  • Status: Abandoned Application
First Claim
Patent Images

1. st, the oxazolidinone derivative shown by structure formula (I) table:

  • Wherein R is (a) hydrogen atom, 

     

     

    (b)C1-C8Alkyl, 

     

     

    (c)C3-C6Cycloalkyl,(d) amino, 

     

     

    (e)C1-C8Alkyl amino, 

     

     

    (f)C1-C8Dialkyl amido, 

     

     

    (g)C1-C8Alkoxy, or 

     

     

    (h)C1-C8Haloalkyl;

    R1And R3Each and be independently(a) hydrogen atom,(b) halogen atom, 

     

     

    (c)C1-C8Alkyl, 

     

     

    (d)C3-C6Cycloalkyl, 

     

     

    (e)-(CH2)m-OR11, or(f)-C (=O)-R41

    X and Y each and are independently(a) hydrogen atom, or(b) halogen atom;

    R4And R5Each and be independently(a) hydrogen atom, 

     

     

     

    (b)C1-C8Alkyl, 

     

     

     

    (c)C1-C8Alkoxy, 

     

     

     

    (d)C1-C8Alkylthio group, 

     

     

     

    (e)-(CH2)m-OR51

     

     

     

    (f)-O-(CH2)m-OR51

     

     

     

    (g)-NR42R52,(h)-N=CH-NR44R55,(i)-C (=O)-NR42R52, or 

     

     

     

    (j)-(CH2)m- C (=A)-R41, or they are combined together to form:

    (k)=O,(l)=NR43,(m)=S,(n)=CR44R54, or(o) replacing in a arbitrary manner, unsaturated or saturation to have 1-3 heteroatomic 5- or 6- circle heterocycles, hetero atom is selected from nitrogen-atoms, oxygen atom and sulphur atom;

    R11And R12Each and be independently:

    (a) hydrogen atom, 

     

     

     

    (b)C1-C8Alkyl, or(c) methoxy;

    R41It is(a) hydrogen atom, 

     

     

     

    (b)-(CH2)m- OH, 

     

     

     

    (c)C1-C8Alkyl, 

     

     

     

    (d)C1-C8Alkoxy, 

     

     

     

    (e)-O-CH2- O-C (=O)-R11, or 

     

     

     

    (f)-(CH2)m- C (=O)-OR11

    R42And R52Each and be independently:

    (a) hydrogen atom, 

     

     

     

    (b)-(CH2)m-OR11

     

     

     

    (c)C1-C8Alkyl,(d)-C (=O)-R41,(e)-C (=O)-NR11R12

     

     

     

    (f)-(CH2)p- phenyl,(g) thiazol-2-yl, or they are combined together to form pyrrolidinyl, piperidino, piperazinyl, morpholino or thiomorpholine generation, each among them can be by C1-C8Alkyl or-(CH2)m- OH replaces;

    R43It is(a) hydrogen atom, 

     

     

     

    (b)-OR51

     

     

     

    (c)C1-C8Alkyl, 

     

     

     

    (d)C1-C8Alkoxy, 

     

     

     

    (e)-(CH2)p- phenyl 

     

     

     

    (f)-N42R52,(g)-NH-C (=NH)-NH2,(h) [1,2,4] triazole-4-yl, or(i) cyano group;

    R44And R54Each and be independently:

    (a) hydrogen atom, 

     

     

     

    (b)C1-C8Alkyl,(c)-C (=O)-R41, or 

     

     

     

    (d)-(CH2)p- phenyl;

    R51It is(a) hydrogen atom, 

     

     

     

    (b)C1-C8Alkyl,(c) C replaced by one or more hydroxyls1-C8Alkyl, 

     

     

     

    (d)C2-C8Alkenyl, 

     

     

     

    (e)C1-C8Haloalkyl, 

     

     

     

    (f)-(CH2)m-OR11

     

     

     

    (g)-(CH2)m- C (=O)-R41,(h)-C (=O)-(CH2)m-OR44, or(i) tosyl;

    A is(a) oxygen atom, or(b) ethylene ketal;

    - it is double bond or singly-bound;

    M is each and independently 0,1 or 2;

    N is 0 or 1;

    P is each and independently 1,2,3 or 4;

    Moreover, each C in above-mentioned definition1-C8Alkyl, each He independently can be replaced by one or more substituents, and the substituent is selected from halogen atom, hydroxyl, C1-C8Alkoxy, C1-C8Acyloxy, amino, C1-C8Alkyl amino, C1-C8Dialkyl amido ,-CN bases and carboxyl, or their pharmacologically acceptable salt.

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