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

Serving hundreds of leading biopharmaceutical companies globally:

Teva
QuintilesIMS
Farmers Insurance
Queensland Health
US Army
Mallinckrodt
Fish and Richardson
Accenture
Cantor Fitzgerald

Generated: April 25, 2018

DrugPatentWatch Database Preview

Claims for Patent: 5,972,986

« Back to Dashboard

Summary for Patent: 5,972,986
Title: Method of using cyclooxygenase-2 inhibitors in the treatment and prevention of neoplasia
Abstract:This invention relates to the use of cyclooxygenase-2 inhibitors or derivatives thereof in preventing and treating neoplasia. In particular, the invention describes the method of preventing and treating epithelial cell neoplasia in a subject, said method comprising treating the subject with a therapeutically-effective amount of a compound of Formula I. ##STR1## wherein A, R.sup.2 and R.sup.3 are as described in the specification.
Inventor(s): Seibert; Karen (St. Louis, MO), Masferrer; Jaime (Ballwin, MO), Gordon; Gary B (Highland Park, IL)
Assignee: G.D. Searle & Co. (Skokie, IL)
Application Number:08/949,922
Patent Claims: 1. A method of treating a neoplasia in a subject in need thereof by inhibiting the growth associated therewith, said method comprising treating the subject with a therapeutically-effective amount of a compound of Formula II ##STR4## wherein R.sup.4 is C.sub.1-6 -haloalkyl; wherein R.sup.5 is hydrido; and wherein R.sup.6 is phenyl optionally substituted at a substitutable position with one or more radicals selected from the group consisting of halo, C.sub.1-6 -alkylthio, C.sub.1-6 -alkylsulfonyl, cyano, nitro, C.sub.1-6 -haloalkyl, C.sub.1-6 -alkyl, hydroxyl, C.sub.2-6 -alkenyl, C.sub.1-6 -hydroxyalkyl, carboxyl, C.sub.3-6 -cycloalkyl, C.sub.1-6 -alkylamino, di-C.sub.1-6 -alkylamino, C.sub.1-6 -alkoxycarbonyl, aminocarbonyl, C.sub.1-6 -alkoxy, C.sub.1-6 -haloalkoxy, sulfamyl, five or six membered heterocyclic and amino; or a pharmaceutically-acceptable salt or derivative thereof.

2. A method of inhibiting or delaying the onset of a neoplasia selected from the group consisting of adenomatous polyps, gastrointestinal cancer, liver cancer, bladder cancer, cervical cancer, prostate cancer, lung cancer, breast cancer and skin cancer, in a subject in need of such inhibition or delay, the method comprising treating said subject with a therapeutically-effective amount of a compound of Formula II ##STR5## wherein R.sup.4 is C.sub.1-6 -haloalkyl; wherein R.sup.5 is hydrido; and wherein R.sup.6 is phenyl optionally substituted at a substitutable position with one or more radicals selected from the group consisting of halo, C.sub.1-6 -alkylthio, C.sub.1-6 -alkylsulfonyl, cyano, nitro, C.sub.1-6 -haloalkyl, C.sub.1-6 -alkyl, hydroxyl, C.sub.2-6 -alkenyl, C.sub.1-6 -hydroxyalkyl, carboxyl, C.sub.3-6 -cycloalkyl, C.sub.1-6 -alkylamino, di-C.sub.1-6 -alkylamino, C.sub.1-6 -alkoxycarbonyl, aminocarbonyl, C.sub.1-6 -alkoxy, C.sub.1-6 -haloalkoxy, sulfamyl, five or six membered heterocyclic and amino; or a pharmaceutically-acceptable salt or derivative thereof.

3. A method of treating a subject suffering from a neoplastic disease state with a conjunctive therapy, said method comprising treating the subject with a therapeutically-effective amount of a compound of Formula II ##STR6## wherein R.sup.4 is C.sub.1-6 -haloalkyl; wherein R.sup.5 is hydrido; and wherein R.sup.6 is phenyl optionally substituted at a substitutable position with one or more radicals selected from the group consisting of halo, C.sub.1-6 -alkylthio, C.sub.1-6 -alkylsulfonyl, cyano, nitro, C.sub.1-6 -haloalkyl, C.sub.1-6 -alkyl, hydroxyl, C.sub.2-6 -alkenyl, C.sub.1-6 -hydroxyalkyl, carboxyl, C.sub.3-6 -cycloalkyl, C.sub.1-6 -alkylamino, di -C.sub.1-6 -alkyl amino, C.sub.1-6 -alkoxycarbonyl, aminocarbonyl, C.sub.1-6 -alkoxy, C.sub.1-6 -haloalkoxy, sulfamyl, five or six membered heterocyclic and amino; or a pharmaceutically-acceptable salt thereof;

and one or more compounds selected from the group consisting of antibiotic agents, alkylating agents, antimetabolite agents, hormonal agents, immunological agents, interferon agents, miscellaneous agents, metallomatrix proteases (MMP) inhibitors, SOD and .alpha..sub.v .beta..sub.3 inhibitors.

4. The method of claim 1 wherein the compound is selected from compounds, and their pharmaceutically acceptable salts, selected from the group consisting of

4-[5-(4-chlorophenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamid e;

4-[5-phenyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide;

4-[5-(4-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamid e;

4-[5-(4-methoxyphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonami de;

4-[5-(4-chlorophenyl)-3-(difluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide

4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamid e;

4-[3-(difluoromethyl)-5-(4-methylphenyl)-1H-pyrazol-1-yl]benzenesulfonamide ;

4-[3-(difluoromethyl)-5-phenyl-1H-pyrazol-1-yl]benzenesulfonamide;

4-[3-(difluoromethyl)-5-(4-methoxyphenyl)-1H-pyrazol-1-yl]benzenesulfonamid e;

4-[3-(difluoromethyl)-5-(3-fluoro-4-methoxyphenyl)-1H-pyrazol-1-yl]benzenes ulfonamide;

4-[5-(3-fluoro-4-methoxyphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzene sulfonamide; and

4-[5-(4-(N,N-dimethylamino)phenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benz enesulfonamide.

5. The method of claim 4 wherein the compound is 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonami de, or a pharmaceutically-acceptable salt thereof.

6. The method of claim 4 wherein the compound is 4-[5-(4-chlorophenyl)-3-(difluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamid e, or a pharmaceutically-acceptable salt thereof.

7. The method of claim 4 where the compound is 4-[5-(3-fluoro-4-methoxyphenyl)-3-(difluoromethyl)-1H-pyrazol-l-yl]benzene sulfonamide, or a pharmaceutically-acceptable salt thereof.

8. The method of claim 1 wherein the neoplasia is selected from the group consisting of colorectal cancer, gastrointestinal cancer, liver cancer, bladder cancer, cervical cancer, prostate cancer, lung cancer, breast cancer and skin cancer.

9. The method of claim 2 wherein the compound is selected from compounds, and their pharmaceutically acceptable salts, selected from the group consisting of

4-[5-(4-chlorophenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamid e;

4-[5-phenyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide;

4-[5-(4-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamid e;

4-[5-(4-methoxyphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonami de;

4-[5-(4-chlorophenyl)-3-(difluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide ;

4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamid e;

4-[3-(difluoromethyl)-5-(4-methylphenyl)-1H-pyrazol-1-yl]benzenesulfonamide ;

4-[3-(difluoromethyl)-5-phenyl-1H-pyrazol-1-yl]benzenesulfonamide;

4-[3-(difluoromethyl)-5-(4-methoxyphenyl)-1H-pyrazol-1-yl]benzenesulfonamid e;

4-[3-(difluoromethyl)-5-(3-fluoro-4-methoxyphenyl)-1H-pyrazol-1-yl]benzenes ulfonamide;

4-[5-(3-fluoro-4-methoxyphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzene sulfonamide; and

4-[5-(4-(N,N-dimethylamino)phenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benz enesulfonamide.

10. The method of claim 9 wherein the compound is 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonami de, or a pharmaceutically-acceptable salt thereof.

11. The method of claim 9 wherein the compound is 4-[5-(4-chlorophenyl)-3-(difluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamid e, or a pharmaceutically-acceptable salt thereof.

12. The method of claim 9 where the compound is 4-[5-(3-fluoro-4-methoxyphenyl)-3-(difluoromethyl)-1H-pyrazol-1-yl]benzene sulfonamide, or a pharmaceutically-acceptable salt thereof.

13. The method of claim 3 wherein the compound is 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonami de, or a pharmaceutically-acceptable salt thereof.

14. The method of claim 1 wherein the neoplasia is adenomatous polyps.

15. The method of claim 2 wherein the neoplasia is adenomatous polyps.

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

Serving hundreds of leading biopharmaceutical companies globally:

Accenture
Cantor Fitzgerald
McKinsey
Mallinckrodt
Deloitte
Baxter
Healthtrust
US Department of Justice
Teva

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.