Deep knowledge on
small-molecule drugs and
the 110,000 global patents
Find generic entry opportunities
Drug patents …
… from Kazakhstan to Kalamazoo
Proactively manage your pharmacy inventory
Manage your formulary budget
Anticipate generic drug launch
Flat-rate pricing for predictable budgeting
Short-term plans for project- or client-based billing
Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing
|Title:||19-nor-vitamin D compounds|
|Abstract:||This invention provides a novel class of vitamin D-related compounds, namely the 1.alpha.-hydroxy-19-nor-vitamin D analogs, as well as a general method for their chemical synthesis. The compounds exhibit pronounced activity in arresting the proliferation of undifferentiated cells, including malignant cells, and in inducing their differentiation, and thus represent novel therapeutic agents for the treatment of malignant and other diseases characterized by the proliferative growth of undifferentiated cells. Formulations for therapeutic use and treatment methods are also provided.|
|Inventor(s):||DeLuca; Hector F. (Deerfield, WI), Schnoes; Heinrich K. (Madison, WI), Perlman; Kato L. (Madison, WI), Sicinski; Rafal R. (Warsaw, PL), Prahl; Jean M. (Madison, WI)|
|Assignee:||Wisconsin Alumni Research Foundation (Madison, WI)|
|Filing Date:||May 16, 1995|
|Claims:||1. A method for inducing cell differentiation in HL-60 leukemia cells which comprises exposing said cells to an effective amount of at least one 19-nor-vitamin D compound sufficient to induce differentiation, said 19-nor-vitamin D compound having the formula ##STR9## where X.sup.1 and X.sup.2 are each selected from hydrogen, acyl, alkylsilyl and alkoxyalkyl, and where R is selected from alkyl, hydrogen, hydroxyalkyl, fluoroalkyl and a side chain of the formula ##STR10## wherein R.sup.1 represents hydrogen, hydroxy or O-acyl, R.sup.2 and R.sup.3 are each selected from alkyl, hydroxyalkyl and fluoroalkyl, or, when taken together represent the group--(CH.sub.2).sub.m --where m is an integer having a value of from 2 to 5, R.sup.4 is selected from hydrogen, hydroxy, fluorine, O-acyl, alkyl, hydroxyalkyl and fluoroalkyl, R.sup.5 is selected from hydrogen, fluorine, alkyl, hydroxyalkyl and fluoroalkyl, or R.sup.4 and R.sup.5 taken together represent double-bonded oxygen, R.sup.6 and R.sup.7 are each selected from hydrogen, hydroxy, O-acyl, fluorine and alkyl, or, R.sup.6 and R.sup.7 taken together form a carbon-carbon double bond, and wherein n is an integer having a value of from 1 to 5 and wherein any of the groups --CH(CH.sub.3)--, --CH(R.sup.7)--, or --CH(R.sup.6)-- at positions 20, 22 and 23, respectively, may be replaced by an oxygen atom, with the proviso that when n is 2 to 5 each R.sup.4 is independently selected from hydrogen, hydroxy, fluorine, O-acyl, alkyl, hydroxyalkyl and fluoroalkyl, and each R.sup.5 is independently selected from hydrogen, fluorine, alkyl, hydroxyalkyl and fluoroalkyl. |
2. The method of claim 1 where the compound in a pharmaceutically acceptable vehicle is administered orally.
3. The method of claim 1 where the compound is administered parenterally.
4. The method of claim 1 where the compound is administered topically.
5. The method of claim 1 where R is a side chain of the formula ##STR11## and X.sup.1 and X.sup.2 are both hydrogen.
6. The method of claim 1 where R is a side chain of the formula ##STR12## and X.sup.1 and X.sup.2 are both hydrogen.
7. The method of claim 1 where R is a side chain of the formula ##STR13## and X.sup.1 and X.sup.2 are both hydrogen.
8. The method of claim 1 where R is a side chain of the formula ##STR14## and X.sup.1 and X.sup.2 are both hydrogen.
Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.