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US4428962A Expired / Lapsed US ⏱️ 0.0 years remaining

Indoles in treatment of peptic ulcers

Assignee: Merck Sharp & Dohme LLC
•
Filing: 1981-10-30
•
Granted: 1984-01-31
•
Expires: 2001-10-30
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Abstract

Abstract There are disclosed herein certain indole derivatives which are useful in the treatment of peptic ulcer diseases.

Inventors

  • 👤 James A. Bristol
  • 👤 Chester Puchalski

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-04 22:12
CPC Classifications
C; C07; C07D; C07D209/00; C07D209/02; C07D209/04; C07D209/08

Claims Analysis

Total Claims: 34
Claim 1
Independent Claim 40 words
A compound represented by formula: ##STR13## and pharmaceutically acceptable salts thereof, wherein R' 1 represents hydrogen or methyl; R' 2 represents methyl and R' 3 represents methyl, cyanomethyl, or amino; X' represents hydrogen; and Y' represents phenylmethoxy, 2-phenylethyl or 3-phenyl-1-propenyl.
Claim 2
Dependent Claim 40 words
A compound represented by formula: ##STR13## and pharmaceutically acceptable salts thereof, wherein R' 1 represents hydrogen or methyl; R' 2 represents methyl and R' 3 represents methyl, cyanomethyl, or amino; X' represents hydrogen; and Y' represents phenylmethoxy, 2-phenylethyl or 3-phenyl-1-propenyl.
Claim 3
Dependent Claim 24 words
A compound of claim 1 wherein R' 1 , R' 2 , and R' 3 are each methyl and Y' is phenylmethoxy, i.e. 1,2,3-trimethyl-7-phenylmethoxyindole.
Claim 4
Dependent Claim 24 words
A compound of claim 1 wherein R' 1 is hydrogen, R' 2 and R' 3 are each methyl and Y' is phenylmethoxy, i.e. 2,3-dimethyl-7-phenylmethoxyindole.
Claim 5
Dependent Claim 24 words
A compound of claim 1 wherein R' 1 is hydrogen, R' 2 is methyl, R' 3 is amino and Y' is phenylmethoxy, i.e. 2-methyl-3-amino-7-phenylmethoxyindole.
Claim 6
Dependent Claim 24 words
A compound of claim 1 wherein R' 1 is hydrogen, R' 2 and R' 3 are each methyl and Y' is 2-phenylethyl, i.e. 2,3-dimethyl-7-(2-phenylethyl)indole.
Claim 7
Dependent Claim 24 words
A compound of claim 1 wherein R' 1 is hydrogen, R' 2 and R' 3 are each methyl and Y' is 3-phenyl-1-propenyl, i.e. 2,3-dimethyl-7-(3-phenyl-1-propenyl)indole.
Claim 8
Dependent Claim 24 words
A compound of claim 1 wherein R' 1 is hydrogen, R' 2 is methyl, R' 3 is cyanomethyl and Y' is 2-phenylethyl, i.e. 2-methyl-3-cyanomethyl-7-(2-phenylethyl)indole.
Claim 9
Dependent Claim 24 words
A compound of claim 1 wherein R' 1 is hydrogen, R' 2 is methyl, R' 3 is amino and Y' is 2-phenylethyl, i.e. 2-methyl-3-amino-7-(2-phenylethyl)indole.
Claim 10
Dependent Claim 24 words
A compound of claim 1 wherein R' 1 is hydrogen, R' 2 is methyl R' 3 is cyanomethyl and Y' is 3-phenyl-1-propenyl, i.e. 2-methyl-3-cyanomethyl-7-(3-phenyl-1-propenyl)indole.
Claim 11
Dependent Claim 24 words
A compound of claim 1 wherein R' 1 is hydrogen, R' 2 is methyl, R' 3 is amino, and Y' is 3-phenyl-1-propenyl, i.e. 2-methyl-3-amino-7-(3-phenyl-1-propenyl)indole.
Claim 12
Dependent Claim 34 words
A method for the treatment of the symptoms of peptic ulcer disease in mammals, which comprises administering to a mammal having peptic ulcer disease a therapeutically effective quantity of a compound of claim 1.
Claim 13
Dependent Claim 29 words
A method for the treatment of gastric ulcers in mammals which comprises administering to a mammal having gastric ulcers a therapeutically effective quantity of a compound of claim 1.
Claim 14
Dependent Claim 29 words
A method for the treatment of duodenal ulcers in mammals which comprises administering to a mammal having duodenal ulcers a therapeutically effective quantity of a compound of claim 1.
Claim 15
Dependent Claim 21 words
A method of claim 11 which comprises administering to a mammal having peptic ulcer disease, a therapeutically effecive quantity of 1,2,3-trimethyl-7-phenylmethoxyindole.
Claim 16
Dependent Claim 37 words
A pharmaceutical formulation for use in the treatment of ulcers which comprises a compound of claim 1 in a therapeutically effective amount sufficient to alleviate the symptoms of peptic ulcer disease together with a pharmaceutically acceptable carrier.
Claim 17
Dependent Claim 20 words
A pharmaceutical formulation of claim 15 which comprises a therapeutically effective amount of 1,2,3-trimethyl-7-phenylmethoxyindole together with a pharmaceutically acceptable carrier.
Claim 18
Dependent Claim 10 words
A pharmaceutical formulation of claim 15 suitable for oral administration.
Claim 19
Dependent Claim 21 words
A method of claim 11 which comprises administering to a mammal having peptic ulcer disease, a therapeutically effective quantity of 2,3-dimethyl-7-phenylmethoxyindole.
Claim 20
Dependent Claim 21 words
A method of claim 11 which comprises administering to a mammal having peptic ulcer disease, a therapeutically effective quantity of 2-methyl-3-amino-7-phenylmethoxyindole.
Claim 21
Dependent Claim 21 words
A method of claim 11 which comprises administering to a mammal having peptic ulcer disease, a therapeutically effective quantity of 2,3-dimethyl-7-(2-phenylethyl)indole.
Claim 22
Dependent Claim 21 words
A method of claim 11 which comprises administering to a mammal having peptic ulcer disease, a therapeutically effective quantity of 2,3-dimethyl-7-(3-phenyl-1-propenyl)indole.
Claim 23
Dependent Claim 21 words
A method of claim 11 which comprises administering to a mammal having peptic ulcer disease, a therapeutically effective quantity of 2-methyl-3-cyanomethyl-7-(2-phenylethyl)indole.
Claim 24
Dependent Claim 21 words
A method of claim 11 which comprises administering to a mammal having peptic ulcer disease, a therapeutically effective quantity of 2-methyl-3-amino-7-(2-phenylethyl)indole.
Claim 25
Dependent Claim 21 words
A method of claim 11 which comprises administering to a mammal having peptic ulcer disease, a therapeutically effective quantity of 2-methyl-3-cyanomethyl-7-(3-phenyl-1-propenyl)indole.
Claim 26
Dependent Claim 21 words
A method of claim 11 which comprises administering to a mammal having peptic ulcer disease, a therapeutically effective quantity of 2-methyl-3-amino-7-(3-phenyl-1-propenyl)indole.
Claim 27
Dependent Claim 20 words
A pharmaceutical formulation of claim 15 which comprises a therapeutically effective amount of 2,3-dimethyl-7-phenylmethoxyindole together with a pharmaceutically acceptable carrier.
Claim 28
Dependent Claim 20 words
A pharmaceutical formulation of claim 15 which comprises a therapeutically effective amount of 2-methyl-3-amino-7-phenylmethoxyindole together with a pharmaceutically acceptable carrier.
Claim 29
Dependent Claim 20 words
A pharmaceutical formulation of claim 15 which comprises a therapeutically effective amount of 2,3-dimethyl-7-(2-phenylethyl)-indole together with a pharmaceutically acceptable carrier.
Claim 30
Dependent Claim 20 words
A pharmaceutical formulation of claim 15 which comprises a therapeutically effective amount of 2,3-dimethyl-7-(3-phenyl-1-propenyl)indole together with a pharmaceutically acceptable carrier.
Claim 31
Dependent Claim 20 words
A pharmaceutical formulation of claim 15 which comprises a therapeutically effective amount of 2-methyl-3-cyanomethyl-7-(2-phenylethyl)indole together with a pharmaceutically acceptable carrier.
Claim 32
Dependent Claim 20 words
A pharmaceutical formulation of claim 15 which comprises a therapeutically effective amount of 2-methyl-3-amino-7-(2-phenylethyl)indole together with a pharmaceutically acceptable carrier.
Claim 33
Dependent Claim 20 words
A pharmaceutical formulation of claim 15 which comprises a therapeutically effective amount of 2-methyl-3-cyanomethyl-7-(3-phenyl-1-propenyl)indole together with a pharmaceutically acceptable carrier.
Claim 34
Dependent Claim 20 words
A pharmaceutical formulation of claim 15 which comprises a therapeutically effective amount of 2-methyl-3-amino-7-(3-phenyl-1-propenyl)indole together with a pharmaceutically acceptable carrier.

References Cited (Backward Citations)

US3076814A Cited
US3072530A Cited
US3297717A Cited
US4021448A Cited
DE2727829A1 Cited
GB2035310B Cited
US4285962A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1987-01-30 1987-08-01 1988-01-31 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1991-01-30 1991-08-01 1992-01-31 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1995-01-30 1995-08-01 1996-01-31 $7700.00 Window Closed / Lapsed

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