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

Serving hundreds of leading biopharmaceutical companies globally:

Express Scripts
US Department of Justice
Chinese Patent Office

Generated: May 21, 2018

DrugPatentWatch Database Preview

Details for Patent: 4,820,848

« Back to Dashboard

Title: Substituted aromatic sulfonamides as antiglaucoma agents
Abstract:Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.
Inventor(s): Ponticello; Gerald S. (Lansdale, PA), Habecker; Charles N. (Lansdale, PA)
Assignee: Merck & Co., Inc. (Rahway, NJ)
Filing Date:Apr 04, 1988
Application Number:07/177,211
Claims:1. A process for preparing a compound of structural formula: ##STR30## wherein R.sup.13 is

(a) hydrogen,

(b) phenyl either unsubstituted or substituted with one or more of

(1) hydroxy,

(2) C.sub.1-3 alkoxy,

(3) R.sup.17 R.sup.18 N--C.sub.1-5 alkyl, wherein R.sup.17 and R.sup.18 are independently selected from:

(i) hydrogen or

(ii) C.sub.1-5 alkyl, or taken together with the nitrogen to which they are attached from a heterocycle selected from morpholine, piperidine, pyrrolidine, and piperazine,

(c) --OH,

(d) .dbd.O; or

(e) --NR.sup.17 R.sup.18

R.sup.14 is

(a) hydrogen,

(b) --CN,

(c) phenyl-C.sub.1-3 alkyl, wherein the phenyl is either unsubstituted or substituted with one or more of

(1) hydroxy,

(2) C.sub.1-3 alkoxy,

(3) R.sup.17 R.sup.18 N-C.sub.1-5 alkyl,

which comprises treating a compound of structural formula: ##STR31## with Oxone.RTM. (potassium peroxymonosulfate) in an aqueous ethanolic solution to provide the compound of formula: ##STR32## followed by treatment with an amine of formula R.sup.17 R.sup.18 NH in a C.sub.1-3 alkanol at 12.degree.-30.degree. C. for 5 to 24 hours.

2. The process of claim 1, wherein R.sup.13 and R.sup.14 are both hydrogen.

3. The process of claim 2, wherein 5,6-dihydro-6-methylene-4H-thieno[2,3-b]thiopyrano-2-sulfonamide-7,7-dioxi de is treated with isobutylamine to form ##STR33##

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

Serving hundreds of leading biopharmaceutical companies globally:

Queensland Health
Cantor Fitzgerald
Farmers Insurance

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.