Back to results
US 2003/0171373 A1Published application
Spiro compounds as inhibitors of fibrinogen-dependent platelet aggregation
AssigneesEli Lilly and Company, Millennium Pharmaceuticals, Inc.
InventorsMatthew J. Fisher, Joseph A. Jakubowski, John J. Masters, Jeffrey T. Mullaney, Michael Paal, Gerd Ruhter, Kenneth J. Ruterbories, Robert M. Scarborough, Theo Schotten, Wolfgang Stenzel
Life of this patent
Estimating the term…
Abstract
This invention relates to certain spirocyclic compounds substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.
Claims22
A compound of formula (I):
- 249
- wherein;
- the spirocycle having (Ai)p, C, and (Bj)q is
- 250
- m is a number from zero to 2;
- R10 is the same or different and is a non-interfering substituent independently selected from alkyl, halosubstituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, arylalkyl, hydroxy, alkoxy, arylalkoxy, amino, substituted amino, carbamoyl, carboxy, acyl, cyano, halo, nitro, or sulfo;
- n is a number from zero to 8;
- R0 is the same or different and is a non-interfering substituent independently selected from alkyl, halosubstituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, arylalkyl, hydroxy, alkoxy, arylalkoxy, amino, substituted amino, carbamoyl, carboxy, acyl, cyano, halo, nitro, or sulfo;
- where Q-(L) is attached at a, and R3 is attached at b;
- the linking group -(L)- is a bond or a substituted or unsubstituted chain selected from the group consisting of CO, CO(C1-C6 alkyl), O(C1-C6 alkyl), NHCO, and C1-C6 alkyl;
- Q is a basic group selected from the group consisting of amino, imino, amidino, hydroxyamidino, N-alkylamidine, N,N′-dialkylamidine, N-arylamidine, aminomethyleneamino, iminomethylamino, guanidino, aminoguanidino, alkylamino, dialkylamino, trialkylamino, alkylideneamino, pyrrolyl, imidazolyl, pyrazolyl, pyridyl, pyrazinyl, pyrimidinyl, indolizinyl, isoindolyl, 3H-indolyl, indolyl, 1H-indazolyl, purinyl, 4H-quinolizinyl, isoquinolyl, quinolyl, phthalazinyl, naphthyridinyl, quinoxalinyl, quinazolinyl, cinnolinyl, amide, thioamide, benzamidino, pteridinyl, 4aH-carbozolyl, carbozolyl, beta-carbolinyl, phenanthridinyl, acridinyl, phenanthrolinyl, phenazinyl, phenarsazinyl, phenothiazinyl, pyrrolinyl, imidazolidinyl, imidazolinyl, pyrazolidinyl, pyrazolinyl, piperidyl, piperazinyl, indolinyl, isoindolinyl, quinuclidinyl, morpholinyl, any of the foregoing radicals substituted on a benzene ring optionally substituted with R20 wherein R20 is hydrogen or halogen, and any of the foregoing radicals substituted by amino, imino, amidino, hydroxyamidino, aminomethyleneamino, iminomethylamino, guanidino, alkylamino, dialkylamino, trialkylamino, tetrahydroisoquinoline, dihydrosioindole, alkylideneamino or
- 251
- R3 is an acidic group selected from the group consisting of CO2R5, (C1-C6 alkyl)CO2R5, CO(C1-C6 alkyl)CO2R5, CONH(C1-C6 alkyl)CO2R5, (C1-C6 alkyl)CH(NHR4)CO2R5, CO(C1-C6 alkyl)CH(NHR4)CO2R5, or CONH(C1-C6 alkyl)CH(NHR4)CO2R5, wherein
- R4 is SO2(C1-C6 alkyl), SO2 aryl, or SO2(substituted aryl);
- and
- R5 is hydrogen, C1-C6 alkyl, aryl, or substituted aryl;
- or a pharmaceutically-acceptable salt, solvate or prodrug thereof.
14 more elements
Dependencies are inferred from the claim text.