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Nor-tropane derivatives, and their application in therapeutics

Assignee: Synthelabo SA
•
Filing: 1981-11-04
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Granted: 1984-02-28
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Expires: 2001-11-04
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Abstract

Abstract Novel 3 beta -aroylamino and 3 beta -heteroaroylamino nor-tropanes and granatanes are provided having the general formula: <IMAGE> Wherein n=1 or 2, R represents a benzyl or a substituted benzyl group and A-CO represents one of a specific range of aroyl groups. The compounds of the invention are useful in the treatment of psychism or digestive troubles.

Inventors

  • 👤 Philippe Dostert
  • 👤 Thierry Imbert
  • 👤 Bernard Bucher

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-07 22:24
CPC Classifications
C; C07; C07D; C07D451/00; C07D451/02; C07D451/04; A; A61; A61P; A61P1/00; A61P1/08; A61P1/12; A61P25/00; A61P25/20; C07C; C07C323/00; C07C65/00; C07C65/21; C07C65/32; C07C65/40; C07D451/14

Claims Analysis

Total Claims: 19
Claim 1
Independent Claim 92 words
A compound having the formula ##STR80## wherein n is 1; R is 3-furylmethyl, benzyl or benzyl in which the ring is substituted with one or two halogens, methyl or cyano; R 1 is methyl or ethyl; R 2 is methoxy or ethoxy; R 3 is hydrogen, bromine, methoxy, nitro, acetyl, methylmercapto or ethylmercapto, with the proviso that when the set (R 3 , n, R) is (H, 1, benzyl) the set (R 1 , R 2 ) is not (CH 3 , OCH 3 ), and pharmacologically acceptable acid addition salts thereof.
Claim 2
Dependent Claim 92 words
A compound having the formula ##STR80## wherein n is 1; R is 3-furylmethyl, benzyl or benzyl in which the ring is substituted with one or two halogens, methyl or cyano; R 1 is methyl or ethyl; R 2 is methoxy or ethoxy; R 3 is hydrogen, bromine, methoxy, nitro, acetyl, methylmercapto or ethylmercapto, with the proviso that when the set (R 3 , n, R) is (H, 1, benzyl) the set (R 1 , R 2 ) is not (CH 3 , OCH 3 ), and pharmacologically acceptable acid addition salts thereof.
Claim 3
Dependent Claim 37 words
A compound as claimed in claim 1 in which R is benzyl or benzyl in which the ring is substituted with one or two halogens, methyl or cyano, and R 3 is hydrogen, bromine, nitro or acetyl.
Claim 4
Dependent Claim 28 words
A compound as claimed in claim 1 in which n is 1; R is ##STR81## R 1 is methyl; R 2 is methoxy and R 3 is hydrogen.
Claim 5
Dependent Claim 28 words
A compound as claimed in claim 1 in which n is 1; R is ##STR82## R 1 is methyl; R 2 is methoxy and R 3 is hydrogen.
Claim 6
Dependent Claim 28 words
A compound as claimed in claim 1 in which n is 1; R is ##STR83## R 1 is methyl; R 2 is methoxy and R 3 is hydrogen.
Claim 7
Dependent Claim 28 words
A compound as claimed in claim 1 in which n is 1; R is ##STR84## R 1 is methyl; R 2 is methoxy; and R 3 is bromine.
Claim 8
Dependent Claim 28 words
A compound as claimed in claim 1 in which n is 1; R is ##STR85## R 1 is ethyl; R 2 is methoxy; and R 3 is hydrogen.
Claim 9
Dependent Claim 28 words
A compound as claimed in claim 1 in which n is 1; R is ##STR86## R 1 is methyl; R 2 is methoxy; and R 3 is hydrogen.
Claim 10
Dependent Claim 28 words
A compound as claimed in claim 1 in which n is 1; R is ##STR87## R 1 is ethyl; R 2 is ethoxy; and R 3 is hydrogen.
Claim 11
Dependent Claim 28 words
A compound as claimed in claim 1 in which n is 1; R is ##STR88## R 1 is methyl; R 2 is methoxy; and R 3 is hydrogen.
Claim 12
Dependent Claim 28 words
A compound as claimed in claim 1 in which n is 1; R is ##STR89## R 1 is methyl; R 2 is methoxy; and R 3 is hydrogen.
Claim 13
Dependent Claim 35 words
A compound having the formula ##STR90## wherein n is 1; R 5 is halogen, methyl or cyano; R 1 is methyl or ethyl; R 2 is methoxy or ethoxy, and pharmacologically acceptable acid salts thereof.
Claim 14
Dependent Claim 35 words
A compound having the formula ##STR90## wherein n is 1; R 5 is halogen, methyl or cyano; R 1 is methyl or ethyl; R 2 is methoxy or ethoxy, and pharmacologically acceptable acid salts thereof.
Claim 15
Dependent Claim 50 words
A compound having the formula ##STR91## wherein n is 1; R 1 is methyl or ethyl; and R 2 is methoxy or ethoxy, with the proviso that the set (R 1 , R 2 ) is not (CH 3 , OCH 3 ), and pharmacologically acceptable acid addition salts thereof.
Claim 16
Dependent Claim 50 words
A compound having the formula ##STR91## wherein n is 1; R 1 is methyl or ethyl; and R 2 is methoxy or ethoxy, with the proviso that the set (R 1 , R 2 ) is not (CH 3 , OCH 3 ), and pharmacologically acceptable acid addition salts thereof.
Claim 17
Dependent Claim 126 words
The compound as claimed in claim 1, in which the set of substituents (n, R 1 , R 2 , R 3 , R) is selected from the group consisting of (1, Et, EtO, H, Benzyl), (1, CH 3 , OCH 3 , OCH 3 , benzyl), (1, Et, CH 3 O, H, Benzyl), (1, CH 3 , EtO, H, benzyl), (1, Et, CH 3 O, CH 3 O, benzyl), (1, CH 3 , OCH 3 , NO 2 , benzyl), (1, CH 3 , OCH 3 , Br, benzyl), (1, CH 3 , OCH 3 , SCH 3 , benzyl), (1, CH 3 , OCH 3 , SC 2 H 5 , benzyl), (1, CH 3 , OCH 3 , COCH 3 , benzyl), ##STR92##
Claim 18
Dependent Claim 24 words
A psychotropic pharmaceutical composition comprising a therapeutically effective amount of a compound as claimed in claim 1, in combination with a pharmaceutically acceptable carrier.
Claim 19
Dependent Claim 31 words
An anti-emetic or anti-constipation pharmaceutical composition for treating the digestive system comprising a therapeutically effective amount of a compound as claimed in claim 1, in combination with a pharmaceutically acceptable carrier.

References Cited (Backward Citations)

US3134782A Cited
GB774858A Cited
CH374679A Cited
US4179567A Cited
US4273778A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1987-02-27 1987-08-29 1988-02-28 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1991-02-27 1991-08-29 1992-02-28 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1995-02-27 1995-08-29 1996-02-28 $7700.00 Window Closed / Lapsed

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