729556-25-6Relevant articles and documents
VLA-4 ANTAGONISTS
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Page/Page column 19-20, (2008/06/13)
Substituted N-[N-(sulphonylphenyl)sulfonyl-prolyl]-phenylalanine derivatives of the present invention are antagonists of the VLA-4 integrin and are useful in the treatment, prevention and suppression of diseases mediated by VLA-4-binding and cell adhesion and activation. Moreover, the compounds of the present invention demonstrate significant receptor occupancy of VLA-4 bearing cells after oral administration and are suitable for once-, twice-, or thrice-a-day oral administration. This invention also relates to compositions containing such compounds and methods of treatment using such compounds.
[C]-FUSED BICYCLIC PROLINE DERIVATIVES AND THEIR USE FOR TREATING ARTHRITIC CONDITIONS
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Page 81-82, (2010/02/09)
This invention relates to a compound which is [c]-fused bicyclic proline derivative, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition comprising the compound or the salt thereof, and methods of treating diseases, including, but
N-arylsulfonyl aza-bicyclic derivatives as potent cell adhesion inhibitors
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, (2008/06/13)
Compounds of Formula I are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.
Process for the preparation of monocyclic, bicyclic and tricyclic aminoacids
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, (2008/06/13)
The invention relates to a process for the preparation of compounds of the formula I STR1 in which R represents hydrogen, alkyl or aralkyl, and R1 to R6 denote identical or different radicals hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, cycloalkenylalkyl, aralkyl or aryl, both being monosubstituted, disubstituted or trisubstituted in the aryl moiety by alkyl, alkoxy, hydroxyl, halogen, nitro, methylenedioxy and/or cyano, or in which two of the radicals R1 to R6, together with the carbon atom(s) bearing them form a monocyclic or bicyclic ring system, and the remaining radicals are hydrogen, which process comprises converting, with an oxidizing agent in the presence of a silver salt, a pyrrolidine derivative of the formula II into a Δ1 -pyrroline derivative of the formula III, reacting the latter with hydrogen cyanide or a metal cyanide to form a nitrile of the formula IV, and subjecting the latter to solvolysis with a compound of the formula ROH.
DIASTEREOSELECTIVE SYNTHESIS OF BICYCLIC AMINO ACIDS VIA RING CONTRACTION OF α-CHLOROLACTAMS
Henning, R.,Urbach, H.
, p. 5339 - 5342 (2007/10/02)
Bicyclic lactams were converted to their α-chloro-derivatives and subjected to ring contraction under basic conditions to give bicyclic acids in diasteroselective fashion.