摘要:
The present invention relates to a method of treating a patient suffering from a neoplastic disease state comprising administering to said patient an effective antineoplastic amount of a 2′-halomethylidene derivative in conjunctive therapy with an effective antineoplastic amount of a S phase or M-phase specific agent.
摘要:
A process and diastereomeric salts useful for the optical resolution of racemic null-null4-(1,1-dimethylethyl)phenylnull-4-(hydroxydiphenylmethyl)-1-piperidinebutanol, 4-null4-null4-(hydroxydiphenylmethyl)-1-piperidinylnull-1-hydroxybutylnull-null,null-dimethylbenzeneacetic acid and lower alkyl 4-null4-null4-(hydroxydiphenylmethyl)-1-piperidinylnull-1-hydroxybutylnull-null,null-dimethylbenzeneacetates. The process comprises placing into solution a chiral resolving agent, either (null)/(null)-di-paratoluoyltartaric acid or (null)/(null)-mandelic acid, in an amount equimolar to a compound corresponding to the desired enantiomer of the above compound, precipitating the resulting diastereomeric salt between the chiral resolving agent and the target enantiomer and separating the enantiomer.
摘要:
The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula 1 wherein W represents nullC(nullO)null or nullCH(OH)null; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is nullCOOH or nullCOOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are ta to form a second bond between the carbon R1 and R2 or where R1 represented hydrox integer 0.
摘要:
The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula ##STR1## wherein W represents --C(.dbd.O)-- or --CH(OH)--;R.sub.1 represents hydrogen or hydroxy;R.sub.2 represents hydrogen;R.sub.1 and R.sub.2 taken together form a second bond between the carbon atoms bearing R.sub.1 and R.sub.2 ;n is an integer of from 1 to 5;m is an integer 0 or 1;R.sub.3 is --COOH or --COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; andpharmaceutically acceptable salts and individual optical isomers thereof,with the proviso that where R.sub.1 and R.sub.2 are ta to form a second bond between the carbon R.sub.1 and R.sub.2 or where R.sub.1 represented hydroxy integer 0.
摘要:
The present invention provides 4-nitro-.DELTA..sup.4 -3-ketosteroids, their use as steroid C.sub.17-20 lyase and 5.alpha.-reductase inhibitors and to a novel process for preparing a compound of the formula: ##STR1## comprising sequentially: a) reacting a starting compound of the formula ##STR2## with an effective amount of a strong base at an elevated or suitable temperature for a time sufficient to create the corresponding thermodynamic dienolate, followed by addition of a neutral nitrating agent to produce the 4-nitrosteroid; and then;b) reacting the 4-nitrosteroid with a suitable reducing agent.
摘要:
This invention relates to compounds and pharmaceutical compositions, and methods for inhibiting or preventing the amyloid protein deposits in the brain which are associated with Alzheimer's disease and aged Down's syndrome patients. More particularly, it relates to the treatment of Alzheimer's disease.
摘要:
The combination of compounds of formula I and II can be used for the treatment of retroviraI infections. The combination can be used to treat AIDS and ARC and other diseases caused by the retrovirus HTV or other related viruses.
摘要:
Antagonists of neurokinin A which are derivatives of naturally occurring neurokinin A in which the amide bond connecting the two amino acids on the carboxy terminal end is modified are described. The antagonism is confirmed using conventional competitive binding and biochemical assays as well as conventional physiological tests and the use of these derivatives in a variety of conditions in which neurokinin A is implicated is also described.
摘要:
This invention relates to certain novel 2'-halomethylidene, 2'-ethenylidene and 2'-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.
摘要:
The present invention is directed toward a novel process of preparing 2'-exocyclic vinylfluoride derivatives of cytidine analogues for use as ribonucleotide reductase inhibitors.