.

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: 5,753,646

« Back to Dashboard

Claims for Patent: 5,753,646

Title: Substituted dihydrodibenzo/b,f/azepines, method of their preparation, their use in the treatment of some central nervous system disorders, and pharmaceutical compositions containing them
Abstract:New compounds of general formula I, including all possible stereoisomers, are described ##STR1## wherein: R is hydrogen, alkyl, aminoalkyl, halogenalkyl, aralkyl, cycloalkyl, cycloalkylalkyl, alkoxy, phenyl or substituted phenyl or pyridyl group. A process for their preparation consists of reaction of compound II ##STR2## with an acylating agent.
Inventor(s): Benes; Jan (Oporto, PT), Soares Da Silva; Patricio M. V. A. (Oporto, PT)
Assignee: Portela & Ca., S.A. (Oporto, PT)
Application Number:08/673,819
Patent Claims: 1. A compound of general formula I, or stereoisomer thereof, ##STR5## wherein: I R is hydrogen, alkyl, halogenalkyl, aralkyl, cycloalkyl, cycloalkylalkyl, alkoxy, aryl or pyridyl; the term alkyl means carbon chain, straight or branched, containing from 1 to 18 carbon atoms; the term halogen represents fluorine, chlorine, bromine or iodine; the term cycloalkyl represents an alicyclic saturated group with 3 to 6 carbon atoms; and the term aryl represents unsubstituted phenyl group or phenyl substituted by alkoxy, halogen or nitro group.

2. A compound as defined in claim 1 which is:

(1) 10-acetoxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide

(2) 10-benzoyloxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide

(3) 10-(4-methoxybenzoyloxy)-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide

(4) 10-(3-methoxybenzoyloxy)-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide

(5) 10-(2-methoxybenzoyloxy)-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide

(6) 10-(4-nitrobenzoyloxy)-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide

(7) 10-(3-nitrobenzoyloxy)-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide

(8) 10-(2-nitrobenzoyloxy)-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide

(9) 10-(4-chlorobenzoyloxy)-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide

(10) 10-(3-chlorobenzoyloxy)-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide

(11) 10-(2-acetoxybenzoyloxy)-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide

(12) 10-propionyloxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide

(13) 10-butyryloxy-10, 1-dihydro-5H-dibenz/b,f/azepine-5-carboxamide

(14) 10-pivaloyloxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide

(15) 10-[(2-propyl)pentanoyloxy]-10,11-dihydro-5H--dibenz/b,f/azepine-5-carboxa mide

(16) 10-[(2-ethyl)hexanoyloxy]-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamid e

(17) 10-stearoyloxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide

(18) 10-cyclopentanoyloxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide

(19) 10-cyclohexanoyloxy-10,11 -dihydro-5H-dibenz/b,f/azepine-5-carboxamide

(20) 10-phenylacetoxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide

(21) 10-(4-methoxyphenyl)acetoxy-10,11-dihydro-5H-dibenz/b,f/-azepine-5-carboxa mide

(22) 10-(3-methoxyphenyl)acetoxy-10,11-dihydro-5H-dibenz/b,f/-azepine-5-carboxa mide

(23) 10-(4nitrophenyl)acetoxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide

(24) 10-(3-nitrophenyl)acetoxy-10,11-dihydro-5H-dibenz/b,f/azepine-5carboxamide

(25) 10-nicotinoyloxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide

(26) 10-isonicotinoyloxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide

(27) 10-chloroacetoxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide

(28) 10-bromoacetoxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide

(29) 10-formyloxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide

(30) 10-ethoxycarbonyloxy-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide

(31) 10-(2-chloropropionyloxy)-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamid e.

3. A process for producing a compound having the general formula I of claim 1 comprising ##STR6## with compounds of the general formula III

wherein:

R is the same as defined above for general formula I;

A is hydrogen, halo or --O--CO--R group or --O--CO--OR' group, wherein R' is lower alkyl.

4. The process as defined in claim 3 wherein the reaction is conducted in the presence of at least one condensing agent or base.

5. In a method of treating a subject afflicted with epilepsy, trigeminal neuralgia, affective brain disorder or nervous function alteration in degenerative and post-ischemic disease by administering an effective amount of a pharmaceutical composition containing an active ingredient, the improvement which comprises employing a compound of claim 1 as said active ingredient.

6. The method of claim 5 in which the pharmaceutical composition comprises said compound of claim 1 in admixture with a pharmaceutically acceptable carrier.

7. In a method of treating a subject afflicted with epilepsy, trigeminal neuralgia, affective brain disorder or nervous function alteration in degenerative and post-ischemic disease by administering an effective amount of a pharmaceutical composition containing an active ingredient, the improvement which comprises employing a compound of claim 2 as said active ingredient.

8. The method of claim 7 in which the pharmaceutical composition comprises said compound of claim 1 in admixture with a pharmaceutically acceptable carrier.

9. A pharmaceutical composition comprising a compound according to claim 1 in admixture with a pharmaceutically acceptable carrier.

10. A pharmaceutical composition comprising a compound according to claim 2 in admixture with a pharmaceutically acceptable carrier.
« 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