336191-15-2Relevant articles and documents
SELF-IMMOLATIVE LINKERS CONTAINING MANDELIC ACID DERIVATIVES, DRUG-LIGAND CONJUGATES FOR TARGETED THERAPIES AND USES THEREOF
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Page/Page column 69; 128, (2015/03/28)
The invention provides a therapeutic drug and targeting conjugate, pharmaceutical compositions containing these conjugates in pharmaceutical composition, and uses of these conjugates in anti-neoplastic and other therapeutic regimens. Also provided are novel intermediates thereof. The conjugates provide a therapeutic drug fragment or prodrug fragment bound to a targeting moiety via a linker which comprises a substrate cleavable by a protease such as Cathepsin B. The targeting moiety is a ligand which targets a cell surface molecule, such as a cell surface receptor on an anti-neoplastic cell. The ligand may function solely as a targeting moiety or may itself have a therapeutic effect. Following administration of the therapeutic drug and targeting conjugate of formula I and exposure of the conjugate to the protease specific for the substrate, the linker is cleaved and the targeting moiety is separated from the conjugate, which causes the drug fragment or prodrug fragment to convert to the drug or prodrug. The recited conjugates are useful in anti-neoplastic therapies. Also provided are methods of making the therapeutic drug and targeting conjugates and intermediates thereof, and kits comprising the therapeutic drug and targeting conjugates.
2-CYANOPYRROLOPYRIMIDINES AND PHARMACEUTICAL USES THEREOF
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Page/Page column 41-42, (2010/02/08)
The invention relates to pyrrolo pyrimidines of formula (I), wherein Y represents -(CH2)t-O- or -(CH2)r-S-, p is 1 or 2, r is 1, 2 or 3, t is 1, 2 or 3, or Y is -(CH2)j- or -CH=CH-, j is 1 or 2; p is 1 or 2, or Y is -(CH2)f-, f is 1 or 2, p is 1, and the further radicals and symbols have the meaning as defined herein; their preparation, their use as pharmaceuticals, pharmaceutical compositions containing them, the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment of neuropathic pain and to a method for the treatment of such a disease in animals, especially in humans.
Pyridyl-containing spirocyclic compounds as inhibitors of fibrinogen-dependent platelet aggregation
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, (2008/06/13)
Disclosed are certain substituted or unsubstituted pyridyl-containing spirocyclic compounds substituted with both basic and acidic functionality, which are useful in inhibiting platelet aggregation, inhibiting the binding of fibrinogen to blood platelets, and preventing or treating thrombosis
Spirocyclic nonpeptide glycoprotein IIb-IIIa antagonists. Part 3: Synthesis and SAR of potent and specific 2,8-diazaspiro[4.5]decanes
Mehrotra, Mukund M.,Heath, Julie A.,Rose, Jack W.,Smyth, Mark S.,Seroogy, Joseph,Volkots, Deborah L.,Ruhter, Gerd,Schotten, Theo,Alaimo, Lisa,Park, Gary,Pandey, Anjali,Scarborough, Robert M.
, p. 1103 - 1107 (2007/10/03)
The synthesis and biological activity of analogues containing spiro piperidinylpyridine and pyrrolidinylpyridine templates are described. The potent activity of these compounds as platelet aggregation inhibitors demonstrates the utility of the spiro structures as central template for nonpeptide RGD mimics.
Serine derived NK1 antagonists 2: A pharmacophore model for arylsulfonamide binding
Elliott,Broughton,Cascieri,Chicchi,Huscroft,Kurtz,MacLeod,Sadowski,Stevenson
, p. 1851 - 1856 (2007/10/03)
Modifications to the spirocyclic aryl sulfonamide portion of serine derived NK1 antagonists allow a partial pharmacophore model to be developed.
