Novel use of peptide class of compound for treating non neuropathic inflammatory pain
AssigneeSchwarz Pharma AG
InventorNorma Selve
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Abstract
The present invention concerns the use of compounds of the Formula (I) for treating different types and symptoms of acute and chronic pain, especially non neuropathic inflammatory pain in mammals. The pain to be treated may be e.g. chronic inflammatory pain, rheumatoid arthritis pain and/or secondary inflammatory osteoarthritic pain. The compounds show an antinociceptive profile and differ from classical analgesics like opioids and non-steroidal anti-inflammatory drugs (NSAIDS) and are useful as specific analgesics.
Claims35
Use of a compound having the Formula (I)
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- wherein
- R is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl, aryl lower alkyl, heterocyclic, heterocyclic lower alkyl, lower alkyl heterocyclic, lower cycloalkyl, lower cycloalkyl lower alkyl, and R is unsubstituted or is substituted with at least one electron withdrawing group or electron donating group;
- R1 is hydrogen or lower alkyl, lower alkenyl, lower alkynyl, aryl lower alkyl, aryl, heterocyclic lower alkyl, heterocyclic, lower cycloalkyl, lower cycloalkyl lower alkyl, each unsubstituted or substituted with an electron donating group or an electron withdrawing group;
- R2 and R3 are independently hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl lower alkyl, halo, heterocyclic, heterocyclic lower alkyl, lower alkyl heterocyclic, lower cycloalkyl, lower cycloalkyl lower alkyl, or Z-Y wherein R2 and R3 may be unsubstituted or substituted with at least one electron withdrawing group or electron donating group;
- and wherein heterocyclic in R2 and R3 is furyl, thienyl, pyrazolyl, pyrrolyl, imidazolyl, indolyl, thiazolyl, oxazolyl, isothiazolyl, isoxazolyl, piperidyl, pyrrolinyl, piperazinyl, quinolyl, triazolyl, tetrazolyl, isoquinolyl, benzofuryl, benzothienyl, morpholinyl, benzoxazolyl, tetrahydrofuryl, pyranyl, indazolyl, purinyl, indolinyl, pyrazolindinyl, imidazolinyl, imidazolindinyl, pyrrolidinyl, furazanyl, N-methylindolyl, methylfuryl, pyridazinyl, pyrimidinyl, pyrazinyl, epoxy, aziridino, oxetanyl or azetidinyl;
- Z is O, S, S(O)2, NR6′;
- or PR4;
- Y is hydrogen, lower alkyl, aryl, aryl lower alkyl, lower alkenyl, lower alkynyl, heterocyclic, heterocyclic lower alkyl, and Y may be unsubstituted or substituted with an electron donating group or an electron withdrawing group, or ZY taken together is NR4NR5R7, NR4OR5, ONR4R7, OPR4R5, PR4OR5, SNR4R7, NR4SR7, SPR4R5, PR4SR7, NR4PR5R6 or PR4NR5R7,
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- R6′ is hydrogen, lower alkyl, lower alkenyl, or lower alkynyl and R4 may be unsubstituted or substituted with an electron withdrawing group or electron donating group;
- R4, R5 and R6 are independently hydrogen, lower alkyl, aryl, aryl lower alkyl, lower alkenyl, or lower alkynyl, wherein R4, R5 and R6 may be unsubstituted or substituted with an electron withdrawing group or an electron donating group;
- and
- R7 is COOR8, COR8, hydrogen, lower alkyl, aryl, aryl lower alkyl, lower alkenyl or lower alkynyl, which R7 may be unsubstituted or substituted with an electron withdrawing group or an electron donating group;
- R8 is hydrogen or lower alkyl, or aryl lower alkyl, and the aryl or alkyl group may be unsubstituted or substituted with an electron withdrawing group or an electron donating group;
- and n is 1-4;
- and a is 1-3,
- or of a pharmaceutically acceptable salt thereof,
- for the preparation of a pharmaceutical composition for the treatment of different types and symptoms of acute and chronic pain, especially non neuropathic inflammatory pain in mammals.
Use of a compound having the Formula (II)
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- wherein
- Ar is phenyl which is unsubstituted or substituted with at least one halo group;
- R3 is lower alkoxy containing 1-3 carbon atoms and R1 is lower alkyl containing 1-3 carbon atoms
- or of a pharmaceutically acceptable salt thereof, for the preparation of a pharmaceutical composition for the treatment of acute and chronic pain, especially non neuropathic inflammatory pain.
Use of a compound in the R configuration having the formula
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- wherein
- Ar is phenyl which is unsubstituted or substituted with at least one halo group;
- R3 is lower alkoxy containing 1-3 carbon atoms and R1 is methyl
- or of a pharmaceutically acceptable salt thereof, for the preparation of a pharmaceutical composition for the treatment of non neuropathic inflammatory pain.
Use of (R)-2-Acetamido-N-benzyl-3-methoxypropionamide or its pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical composition for the treatment of non neuropathic inflammatory pain in mammals.
Use of (R)-2-Acetamide-N-benzyl-3-methoxy-propionamide or its pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical composition for the treatment of chronic inflammatory pain in mammals.
Dependencies are inferred from the claim text.