US4485107A
Expired / Lapsed
US
⏱️ 0.0 years remaining
[[Bis(aryl)methylene]-1-piperidinyl]alkyl-pyrimidinones
Assignee: Janssen Pharmaceutica NV
•
Filing: 1983-07-27
•
Granted: 1984-11-27
•
Expires: 2003-07-27
Abstract
Abstract Novel [[bis(aryl)methylene]-1-piperidinyl]alkyl-pyrimidinones, wherein the pyrimidinone-ring is embraced within a bicyclic system, being useful compounds in the treatment of psychosomatic disorders.
Inventors
- 👤 Ludo E. J. Kennis
- 👤 Jan Vandenberk
- 👤 Josephus C. Mertens
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-06 10:42
CPC Classifications
C; C07; C07D; C07D495/00; C07D495/02; C07D495/04; C07D471/00; C07D471/02; C07D471/04; A; A61; A61P; A61P25/00; A61P25/28; C07D211/00; C07D211/04; C07D211/06; C07D211/08; C07D211/18; C07D211/30; C07D211/32; C07D211/68; C07D211/70; C07D211/72; C07D211/74; C07D213/00; C07D213/02; C07D213/04; C07D213/24; C07D213/44; C07D213/46; C07D213/50; C07D513/00; C07D513/02; C07D513/04
Claims Analysis
Total Claims: 9
Claim 1
Independent Claim
147 words
A chemical compound having the formula ##STR21## the possible stereochemically isomeric forms and the pharmaceutically acceptable acid-addition salts thereof, wherein: R is hydrogen, hydroxy or lower alkyloxy; R 1 is a member selected from the group consisting of hydrogen and lower alkyl; Alk is a lower alkanediyl radical; X is a member selected from the group consisting of --CH 2 -- and --C(R 2 )═C(R 3 )--, said R 2 and R 3 being each independently hydrogen or lower alkyl; A is a bivalent radical having the formula --CH 2 --CH 2 --, or ##STR22## wherein R 4 and R 5 are each independently selected from the group consisting of hydrogen, halo, amino and lower alkyl; and Ar 1 and Ar 2 are each independently selected from the group consisting of pyridinyl, thienyl and phenyl, being optionally substituted with halo, hydroxy, lower alkyloxy, lower alkyl and trifluoromethyl.
Claim 2
Dependent Claim
147 words
A chemical compound having the formula ##STR21## the possible stereochemically isomeric forms and the pharmaceutically acceptable acid-addition salts thereof, wherein: R is hydrogen, hydroxy or lower alkyloxy; R 1 is a member selected from the group consisting of hydrogen and lower alkyl; Alk is a lower alkanediyl radical; X is a member selected from the group consisting of --CH 2 -- and --C(R 2 )═C(R 3 )--, said R 2 and R 3 being each independently hydrogen or lower alkyl; A is a bivalent radical having the formula --CH 2 --CH 2 --, or ##STR22## wherein R 4 and R 5 are each independently selected from the group consisting of hydrogen, halo, amino and lower alkyl; and Ar 1 and Ar 2 are each independently selected from the group consisting of pyridinyl, thienyl and phenyl, being optionally substituted with halo, hydroxy, lower alkyloxy, lower alkyl and trifluoromethyl.
Claim 3
Dependent Claim
13 words
A chemical compound according to claim 1 wherein Alk is an 1,2-ethanediyl radical.
Claim 4
Dependent Claim
175 words
A pharmaceutical composition in unit dosage form comprising per dosage unit a pharmaceutically acceptable carrier and an amount effective for treating patients suffering from psychosomatic disorders of at least one compound having the formula ##STR23## the possible stereochemically isomeric forms and the pharmaceutically acceptable acid-addition salts thereof, wherein: R is hydrogen, hydroxy or lower alkyloxy; R 1 is a member selected from the group consisting of hydrogen and lower alkyl; Alk is a lower alkanediyl radical; X is a member selected from the group consisting of --CH 2 -- and --C(R 2 )═C(R 3 )--, said R 2 and R 3 being each independently hydrogen or lower alkyl; A is a bivalent radical having the formula --CH 2 --CH 2 --, or ##STR24## wherein R 4 and R 5 are each independently selected from the group consisting of hydrogen, halo, amino and lower alkyl; and Ar 1 and Ar 2 are each independently selected from the group consisting of pyridinyl, thienyl and phenyl, being optionally substituted with halo, hydroxy, lower alkyloxy, lower alkyl and trifluoromethyl.
Claim 5
Dependent Claim
175 words
A pharmaceutical composition in unit dosage form comprising per dosage unit a pharmaceutically acceptable carrier and an amount effective for treating patients suffering from psychosomatic disorders of at least one compound having the formula ##STR23## the possible stereochemically isomeric forms and the pharmaceutically acceptable acid-addition salts thereof, wherein: R is hydrogen, hydroxy or lower alkyloxy; R 1 is a member selected from the group consisting of hydrogen and lower alkyl; Alk is a lower alkanediyl radical; X is a member selected from the group consisting of --CH 2 -- and --C(R 2 )═C(R 3 )--, said R 2 and R 3 being each independently hydrogen or lower alkyl; A is a bivalent radical having the formula --CH 2 --CH 2 --, or ##STR24## wherein R 4 and R 5 are each independently selected from the group consisting of hydrogen, halo, amino and lower alkyl; and Ar 1 and Ar 2 are each independently selected from the group consisting of pyridinyl, thienyl and phenyl, being optionally substituted with halo, hydroxy, lower alkyloxy, lower alkyl and trifluoromethyl.
Claim 6
Dependent Claim
13 words
A pharmaceutical composition according to claim 3 wherein Alk is an 1,2-ethanediyl radical.
Claim 7
Independent Claim
171 words
A method of treating patients suffering from psychosomatic disorders which comprises the systemic administration to said patients of a pharmaceutically acceptable amount of at least one compound having the formula ##STR25## the possible stereochemically isomeric forms and the pharmaceutically acceptable acid-addition salts thereof, wherein: R is hydrogen, hydroxy or lower alkyloxy; R 1 is a member selected from the group consisting of hydrogen and lower alkyl; Alk is a lower alkanediyl radical; X is a member selected from the group consisting of --CH 2 -- and --C(R 2 )═C(R 3 )--, said R 2 and R 3 being each independently hydrogen or lower alkyl; A is a bivalent radical having the formula --CH 2 --CH 2 --, or ##STR26## wherein R 4 and R 5 are each independently selected from the group consisting of hydrogen, halo, amino and lower alkyl; and Ar 1 and Ar 2 are each independently selected from the group consisting of pyridinyl, thienyl and phenyl, being optionally substituted with halo, hydroxy, lower alkyloxy, lower alkyl and trifluoromethyl.
Claim 8
Independent Claim
171 words
A method of treating patients suffering from psychosomatic disorders which comprises the systemic administration to said patients of a pharmaceutically acceptable amount of at least one compound having the formula ##STR25## the possible stereochemically isomeric forms and the pharmaceutically acceptable acid-addition salts thereof, wherein: R is hydrogen, hydroxy or lower alkyloxy; R 1 is a member selected from the group consisting of hydrogen and lower alkyl; Alk is a lower alkanediyl radical; X is a member selected from the group consisting of --CH 2 -- and --C(R 2 )═C(R 3 )--, said R 2 and R 3 being each independently hydrogen or lower alkyl; A is a bivalent radical having the formula --CH 2 --CH 2 --, or ##STR26## wherein R 4 and R 5 are each independently selected from the group consisting of hydrogen, halo, amino and lower alkyl; and Ar 1 and Ar 2 are each independently selected from the group consisting of pyridinyl, thienyl and phenyl, being optionally substituted with halo, hydroxy, lower alkyloxy, lower alkyl and trifluoromethyl.
Claim 9
Dependent Claim
12 words
A method according to claim 5 wherein Alk is an 1,2-ethanediyl radical.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-11-27 | 1988-05-28 | 1988-11-27 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-11-27 | 1992-05-28 | 1992-11-27 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-11-27 | 1996-05-28 | 1996-11-27 | $7700.00 | Window Closed / Lapsed |