.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Claims for Patent: 5,843,984

« Back to Dashboard

Claims for Patent: 5,843,984

Title: Sulfated benzothiophene derivatives, methods of use and formulations containing same
Abstract:Sulfated benzothiophenes of the formula I ##STR1## wherein R.sup.1 is hydrogen, hydroxy, C.sub.1 -C.sub.4 alkoxy, --OCOO(C.sub.1 -C.sub.6 alkyl), --OCO(C.sub.1 -C.sub.6 alkyl), --OCOAr wherein Ar is phenyl or optionally substituted phenyl, --OSO.sub.2 (C.sub.4 -C.sub.6 straight chain alkyl), or --OSO.sub.3 H; R.sup.2 is R.sup.1, Cl or F; with the proviso that at least one of R.sup.1 or R.sup.2 is --OSO.sub.3 H; R.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; and n is 2 or 3; or a pharmaceutically acceptable salt or solvate thereof.
Inventor(s): Clay; Michael Paul (Greenwood, IN), Frolik; Charles Alan (Indianapolis, IN), Jones; Charles David (Indianapolis, IN), Lindstrom; Terry Donald (Indianapolis, IN)
Assignee: Eli Lilly and Company (Indianapolis, IN)
Application Number:08/843,308
Patent Claims: 1. A compound of formula I ##STR9## wherein R.sup.1 is hydrogen, hydroxy, C.sub.1 -C.sub.4 alkoxy, --OCOO(C.sub.1 -C.sub.6 alkyl), --OCO(C.sub.1 -C.sub.6 alkyl), --OCOAr wherein Ar is phenyl or optionally substituted phenyl, --OSO.sub.2 (C.sub.4 -C.sub.6 straight chain alkyl), or --OSO.sub.3 H;

R.sup.2 is R.sup.1, Cl or F; with the proviso that at least one of R.sup.1 or R.sup.2 is --OSO.sub.3 H;

R.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; and

n is 2 or 3;

or a pharmaceutically acceptable salt or solvate thereof.

2. A compound according to claim 1 wherein R.sup.1 and R.sup.2 each are --OSO.sub.3 H.

3. A compound according to claim 1 wherein R.sup.1 is hydroxy and R.sup.2 is --OSO.sub.3 H.

4. A compound according to claim 1 wherein R.sup.2 is hydroxy and R.sup.1 is --OSO.sub.3 H.

5. A compound according to claim 1 wherein n=2.

6. A compound according to claim 5 wherein R.sup.3 is 1-piperidinyl.

7. A pharmaceutical composition comprising a compound according to claim 1, or a pharmaceutically acceptable salt thereof, and, optionally, an effective amount of estrogen or progestin, in combination with a pharmaceutically acceptable carrier, diluent or excipient.

8. A method for alleviating the symptoms of post-menopausal syndrome comprising administering to a woman in need thereof an effective amount of a compound of claim 1, or a pharmaceutically acceptable salt thereof.

9. A method according to claim 8 wherein the post-menopausal syndrome pathological condition is osteoporosis.

10. A method according to claim 8 wherein the post-menopausal syndrome pathological condition is related to a cardiovascular disease.

11. A method according to claim 10 wherein the cardiovascular disease is hyperlipidemia.

12. A method for inhibiting estrogen-dependent cancer comprising administering to a patient in need thereof an effective amount of a compound of claim 1, or a pharmaceutically acceptable salt thereof.

13. A method for inhibiting uterine fibroid disease comprising administering to a woman in need thereof an effective amount of a compound of claim 1, or a pharmaceutically acceptable salt thereof.

14. A method for inhibiting endometriosis comprising administering to a woman in need thereof an effective amount of a compound of claim 1 or a pharmaceutically acceptable salt thereof.

15. A method for inhibiting aortal smooth muscle cell proliferation comprising administering to a human in need thereof an effective amount of a compound of claim 1, or a pharmaceutically acceptable salt thereof.

16. A method for inhibiting restenosis comprising administering to a human in need thereof an effective amount of a compound of claim 1, or a pharmaceutically acceptable salt thereof.

17. A method for alleviating the symptoms of post-menopausal syndrome comprising the method of claim 8, and further comprising administering to said woman an effective amount of estrogen.

18. A method for alleviating the symptoms of post-menopausal syndrome comprising the method of claim 8, and further comprising administering to said woman an effective amount of progestin.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

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.

`abc