US4283410A
Expired / Lapsed
US
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3-Amino or amido-2-(1H-indol-3-yl) propanoic acid derivatives
Assignee: Bayer Corp
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Filing: 1979-12-26
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Granted: 1981-08-11
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Expires: 1999-12-26
Abstract
Abstract Disclosed are compounds characterized by the structural formula: <IMAGE> Various compounds circumscribed by the foregoing formula in which: R is H, CH3 or CH2CH3, R' is H, or <IMAGE> X is H, F or OCH3, Y is H or Cl, and Z is H or <IMAGE> are therapeutically useful as anti-hypertensive agents.
Inventors
- 👤 Robert N. Schut
- 👤 Max E. Safdy
- 👤 Enrique Hong
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 12:22
CPC Classifications
C; C07; C07D; C07D209/00; C07D209/02; C07D209/04; C07D209/10; C07D209/18; C07D209/26; C07D209/20
Claims Analysis
Total Claims: 26
Claim 1
Independent Claim
138 words
3-Amino or amido-2-(1H-indol-3-yl)propanoic acid compounds characterized by the formula: ##STR21## wherein: R is H, CH 3 or CH 2 CH 3 , R' is H or ##STR22## X is H, F or OCH 3 , Y is H or Cl, and Z is H or ##STR23## provided that: (i) when X is F; Y, Z and R' are H and R is H or CH 3 ; (ii) when X is H, Y is Cl, Z is H, R is CH 3 and R' is H; and (iii) when X is OCH 3 ; Y is H provided further that when Z and R' are H, R is CH 3 ; when Z is H and R' is ##STR24## R is H and when Z is ##STR25## R' is ##STR26## and R is CH 2 CH 3 .
Claim 2
Dependent Claim
138 words
3-Amino or amido-2-(1H-indol-3-yl)propanoic acid compounds characterized by the formula: ##STR21## wherein: R is H, CH 3 or CH 2 CH 3 , R' is H or ##STR22## X is H, F or OCH 3 , Y is H or Cl, and Z is H or ##STR23## provided that: (i) when X is F; Y, Z and R' are H and R is H or CH 3 ; (ii) when X is H, Y is Cl, Z is H, R is CH 3 and R' is H; and (iii) when X is OCH 3 ; Y is H provided further that when Z and R' are H, R is CH 3 ; when Z is H and R' is ##STR24## R is H and when Z is ##STR25## R' is ##STR26## and R is CH 2 CH 3 .
Claim 3
Dependent Claim
17 words
The compounds defined by claim 1 in the form of their pharmaceutically acceptable, non-toxic, acid addition salts.
Claim 4
Dependent Claim
29 words
A compound as defined by claim 1 wherein X is OCH 3 , Y is H, Z is ##STR27## R is CH 2 CH 3 and R' is ##STR28##
Claim 5
Dependent Claim
27 words
A compound as defined by claim 1 wherein X is OCH 3 , Y is H, Z is H, R is CH 3 and R' is H.
Claim 6
Dependent Claim
12 words
The hydrochloric acid addition salt of the compound defined by claim 4.
Claim 7
Dependent Claim
26 words
A compound as defined by claim 1 wherein X is OCH 3 , Y is H, Z is H, R is H and R' is ##STR29##
Claim 8
Dependent Claim
25 words
A compound as defined by claim 1 wherein X is H, Y is Cl, Z is H, R is CH 3 and R' is H.
Claim 9
Dependent Claim
12 words
The hydrochloric acid addition salt of the compound defined by claim 7.
Claim 10
Dependent Claim
24 words
A compound as defined by claim 1 wherein X is F, Y is H, Z is H, R is H and R' is H.
Claim 11
Dependent Claim
25 words
A compound as defined by claim 1 wherein X is F, Y is H, Z is H, R is CH 3 and R' is H.
Claim 12
Dependent Claim
12 words
The hydrochloric acid addition salt of the compound defined by claim 10.
Claim 13
Dependent Claim
4 words
Methyl 3-amino-2-(5-methoxy-1H-indol-3-yl) propanoate hydrochloride.
Claim 14
Dependent Claim
4 words
Methyl 3-amino-2-(5-methoxy-1H-indol-3-yl) propanoate hydrochloride.
Claim 15
Independent Claim
156 words
A method of treating hypertension in an individual requiring such treatment which method comprises administering to such individual an anti-hypertensive amount of a compound of the formula: ##STR30## wherein: R is H, CH 3 or CH 2 CH 3 , R' is H or ##STR31## X is H, F or OCH 3 , Y is H or Cl, and Z is H or ##STR32## provided that: (i) when X is F; Y, Z and R' are H and R is H or CH 3 ; (ii) when X is H, Y is Cl, Z is H, R is CH 3 and R' is H; and (iii) when X is OCH 3 ; Y is H provided further that when Z and R' are H, R is CH 3 , when Z is H and R' is ##STR33## R is H and when Z is ##STR34## R' is ##STR35## and R is CH 2 CH 3 .
Claim 16
Independent Claim
156 words
A method of treating hypertension in an individual requiring such treatment which method comprises administering to such individual an anti-hypertensive amount of a compound of the formula: ##STR30## wherein: R is H, CH 3 or CH 2 CH 3 , R' is H or ##STR31## X is H, F or OCH 3 , Y is H or Cl, and Z is H or ##STR32## provided that: (i) when X is F; Y, Z and R' are H and R is H or CH 3 ; (ii) when X is H, Y is Cl, Z is H, R is CH 3 and R' is H; and (iii) when X is OCH 3 ; Y is H provided further that when Z and R' are H, R is CH 3 , when Z is H and R' is ##STR33## R is H and when Z is ##STR34## R' is ##STR35## and R is CH 2 CH 3 .
Claim 17
Dependent Claim
21 words
The method of claim 13 wherein the compound administered is in the form of its pharmaceutically acceptable, non-toxic, acid addition salt.
Claim 18
Dependent Claim
35 words
The method of claim 13 wherein the compound administered is further defined in that X is OCH 3 , Y is H, Z is ##STR36## R is CH 2 CH 3 and R' is ##STR37##
Claim 19
Dependent Claim
33 words
The method of claim 13 wherein the compound administered is further defined in that X is OCH 3 , Y is H, Z is H, R is CH 3 and R' is H.
Claim 20
Dependent Claim
21 words
The method of claim 16 wherein the compound defined therein is administered in the form of its hydrochloric acid addition salt.
Claim 21
Dependent Claim
32 words
The method of claim 13 wherein the compound administered is further defined in that X is OCH 3 , Y is H, Z is H, R is H and R' is ##STR38##
Claim 22
Dependent Claim
31 words
The method of claim 13 wherein the compound administered is further defined in that X is H, Y is Cl, Z is H, R is CH 3 and R' is H.
Claim 23
Dependent Claim
21 words
The method of claim 19 wherein the compound defined therein is administered in the form of its hydrochloric acid addition salt.
Claim 24
Dependent Claim
30 words
The method of claim 13 wherein the compound administered is further defined in that X is F, Y is H, Z is H, R is H and R' is H.
Claim 25
Dependent Claim
31 words
The method of claim 13 wherein the compound administered is further defined in that X is F, Y is H, Z is H, R is CH 3 and R' is H.
Claim 26
Dependent Claim
21 words
The method of claim 22 wherein the compound defined therein is administered in the form of its hydrochloric acid addition salt.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 1984-08-10 | 1985-02-09 | 1985-08-11 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-08-10 | 1989-02-09 | 1989-08-11 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-08-10 | 1993-02-09 | 1993-08-11 | $7700.00 | Window Closed / Lapsed |